[go: up one dir, main page]

HUP0400639A2 - Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények - Google Patents

Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0400639A2
HUP0400639A2 HU0400639A HUP0400639A HUP0400639A2 HU P0400639 A2 HUP0400639 A2 HU P0400639A2 HU 0400639 A HU0400639 A HU 0400639A HU P0400639 A HUP0400639 A HU P0400639A HU P0400639 A2 HUP0400639 A2 HU P0400639A2
Authority
HU
Hungary
Prior art keywords
group
so2n
con
ring
condensed
Prior art date
Application number
HU0400639A
Other languages
English (en)
Inventor
David Bebbington
Jean-Damien Charrier
Robert Davies
Simon Everitt
David Kay
Ronald Knegtel
Sanjay Patel
Original Assignee
Vertex Pharmaceuticals Incorporated
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Incorporated filed Critical Vertex Pharmaceuticals Incorporated
Publication of HUP0400639A2 publication Critical patent/HUP0400639A2/hu
Publication of HUP0400639A3 publication Critical patent/HUP0400639A3/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Biotechnology (AREA)

Abstract

A találmány az általános képletű vegyületekre, illetvegyógyszerészetileg elfogadható származékaikra vagy prodrugjaikravonatkozik, amelyek képletében Rx és Ry a közöttük lévő atomokkalegyütt egy kondenzált, telítetlen vagy részlegesen telítetlen; adottesetben legfeljebb három heteroatomot tartalmazó, 5-7 tagú gyűrűtképez, amelyben az Rx és Ry által képezett kondenzált gyűrűben lévőbármely szubsztituálható szénatom oxocsoporttal, -T-R3 vagy L-Z-R3csoporttal, és az Rx és Ry által képezett kondenzált gyűrűben lévőbármely szubsztituálható nitrogénatom -R4 csoporttal szubsztituált; Rl-T- (D gyűrű) csoport; D gyűrű egy, az aril-, heteroaril-,heterociklil- vagy karbociklilcsoportok köréből kiválasztott 5-7 tagúmonociklusos csoportot vagy 8-10 tagú biciklusos csoportot jelent,amely heteroaril- vagy heterociklilcsoport a gyűrűben 1-4 heteroatomottartalmaz; T vegyértékkötés vagy alkilidéncsoport; Z alkilidéncsoport;L oxi-, tio-, szulfinil-, szulfonil-, -N(R6)-SO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, karboni1-, -C(O)O-, -N(R6) -CO-, -N(R6)-C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2N(R6)-, -N(R6)-N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)-C(O)-, -C(R6)2N(R6)C(O)O-, -C(R6)=NN(R6)-, -C(R6)-N-O-C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2N(R6)- vagy -C(R6)2N(R6)-CON(R6)- csoport; R2 és R2'jelentése -R vagy -T-W-R6 csoport, vagy R2 és R2' a közöttük lévőatomokkal együtt egy kondenzált, telítetlen vagy részlegesentelítetlen, adott esetben legfeljebb három heteroatomot tartalmazó, 5-8 tagú gyűrűt képez; R3 halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR,-COCH2COR, nitro-, ciano-, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R7)2, -SO2N(R7)2, -OC(=O)R, -N(R7)COR, -N(R7)COO (adott esetben szubsztituáltalifás), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2, -N(R7)SO2N(R7)2, -N(R4)SO2R vagy -OC(=O)-N(R7)2 csoport; R hidrogénatomvagy adott esetben szubsztituált alifás, aril-, heteroaril- vagyheterociklilcsoport; R5 halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR,nitro-, ciano-, -S(O)R, -S(O)2R, -SR, -N(R4)2, -CON(R4)2, -SO2N(R4)2,-OC(=O)R, -N(R4)COR, -N(R4)CO2 (adott esetben szubsztituált alifás), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R4)CON(R4)2, -N(R4)SO2N(R4)2, -N(R4)SO2R vagy -OC(=O)N(R4)2 csoport; V oxi-, tio-, szulfinil-,szulfonil-, karbonil-, -CO2-, -N(R6)SO2-, -SO2N(R6)-, -N(R6)-, -N(R6)CO-, -N(R6)C(O)O-, -N(R6)CON(R6)-, -N(R6)SO2-N(R6)-, -N(R6)N(R6)-, -C(O)N(R6)-, -OC(O)N(R6)-, -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2N(R6)-, -C(R6)2N(R6)-, -C(R6)2N(R6)C(O)-, -C(R6)2-N(R6)C(O)O-, -C(R6)-NN(R6)-, -C(R6)-N-O-, -C(R6)2N(R6)-N(R6)-, -C(R6)2-N(R6)SO2N(R6)- vagy -C(R6)2N(R6)CON(R6)-csoport; W -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2-SO2N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-, -C(R6)OC(O)-,
HU0400639A 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them HUP0400639A3 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25788700P 2000-12-21 2000-12-21
US28694901P 2001-04-27 2001-04-27
PCT/US2001/049140 WO2002050065A2 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
HUP0400639A2 true HUP0400639A2 (hu) 2004-06-28
HUP0400639A3 HUP0400639A3 (en) 2010-03-29

Family

ID=26946273

Family Applications (5)

Application Number Title Priority Date Filing Date
HU0400638A HUP0400638A2 (hu) 2000-12-21 2001-12-19 Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HU0400641A HUP0400641A3 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
HU0400908A HUP0400908A3 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors, their use and pharmaceutical compositions containing them
HU0400842A HUP0400842A2 (hu) 2000-12-21 2001-12-19 Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HU0400639A HUP0400639A3 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them

Family Applications Before (4)

Application Number Title Priority Date Filing Date
HU0400638A HUP0400638A2 (hu) 2000-12-21 2001-12-19 Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HU0400641A HUP0400641A3 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
HU0400908A HUP0400908A3 (en) 2000-12-21 2001-12-19 Pyrazole compounds useful as protein kinase inhibitors, their use and pharmaceutical compositions containing them
HU0400842A HUP0400842A2 (hu) 2000-12-21 2001-12-19 Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények

Country Status (27)

Country Link
US (16) US20030105090A1 (hu)
EP (10) EP1355905B1 (hu)
JP (19) JP4234435B2 (hu)
KR (8) KR100875091B1 (hu)
CN (6) CN100406454C (hu)
AP (2) AP1588A (hu)
AR (4) AR042169A1 (hu)
AT (9) ATE354573T1 (hu)
AU (7) AU2002234047A1 (hu)
BR (2) BR0116493A (hu)
CA (8) CA2432223C (hu)
CY (1) CY1106297T1 (hu)
DE (8) DE60119776T2 (hu)
DK (3) DK1345922T3 (hu)
ES (7) ES2265446T3 (hu)
HU (5) HUP0400638A2 (hu)
IL (8) IL156368A0 (hu)
MX (8) MXPA03005609A (hu)
MY (1) MY140377A (hu)
NO (5) NO20032671L (hu)
NZ (8) NZ526470A (hu)
PL (2) PL210414B1 (hu)
PT (3) PT1355905E (hu)
RU (1) RU2355688C2 (hu)
SI (2) SI1355905T1 (hu)
TW (2) TWI290551B (hu)
WO (8) WO2002050065A2 (hu)

Families Citing this family (376)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6982260B1 (en) 1999-11-22 2006-01-03 Warner-Lambert Company Quinazolines and their use for inhibiting cyclin-dependent kinase enzymes
JP4105947B2 (ja) * 2000-09-15 2008-06-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なトリアゾール化合物
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US20020111353A1 (en) * 2000-12-05 2002-08-15 Mark Ledeboer Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
MXPA03005609A (es) * 2000-12-21 2003-10-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de la proteina cinasa.
ATE325795T1 (de) * 2001-03-23 2006-06-15 Bayer Corp Rho-kinase inhibitoren
CA2442270C (en) 2001-04-10 2009-09-08 Merck & Co., Inc. Inhibitors of akt activity
US7105667B2 (en) * 2001-05-01 2006-09-12 Bristol-Myers Squibb Co. Fused heterocyclic compounds and use thereof
US7138404B2 (en) * 2001-05-23 2006-11-21 Hoffmann-La Roche Inc. 4-aminopyrimidine derivatives
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003026666A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4- (5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, as src kinase inhibitors
PL368347A1 (en) * 2001-09-26 2005-03-21 Pharmacia Italia S.P.A. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions containing them
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
AU2002361846A1 (en) * 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation Quinazoline and quinoline derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
AU2003235798A1 (en) 2002-01-10 2003-07-24 F. Hoffmann-La Roche Ag Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
MXPA04007697A (es) * 2002-02-06 2004-11-10 Vertex Pharma Compuestos de heteroarilo utiles como inhibidores de gsk-3.
ATE468336T1 (de) * 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
WO2003078426A1 (en) * 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azolylaminoazine as inhibitors of protein kinases
AU2003220299A1 (en) * 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
US7223738B2 (en) 2002-04-08 2007-05-29 Merck & Co., Inc. Inhibitors of Akt activity
WO2003104230A1 (ja) 2002-06-07 2003-12-18 協和醱酵工業株式会社 二環性ピリミジン誘導体
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004009602A1 (en) * 2002-07-23 2004-01-29 Smithkline Beecham Corporation Pyrazolopyrimidines as kinase inhibitors
MXPA05001096A (es) 2002-07-29 2005-11-23 Rigel Pharmaceuticals Inc Metodos para tratamiento o prevencion de enfermedades autoinmunes con compuestos de 2,4-diamino-pirimidina.
WO2004013140A1 (en) * 2002-08-02 2004-02-12 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
EP1739087A1 (en) * 2002-08-02 2007-01-03 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
KR101166745B1 (ko) * 2002-09-05 2012-07-23 아방티 파르마 소시에테 아노님 의약으로서의 신규한 아미노인다졸 유도체 및 이를 함유하는 약제학적 조성물
FR2844267B1 (fr) * 2002-09-05 2008-02-15 Aventis Pharma Sa Nouveaux derives d'aminoindazoles a titre de medicaments et compositions pharmaceutiques les renfermant
WO2004030672A1 (en) * 2002-10-02 2004-04-15 Merck Patent Gmbh Use of 4 amino-quinazolines as anti cancer agents
MXPA05003607A (es) * 2002-10-04 2005-11-17 Prana Biotechnology Ltd Compuestos neurologicamente activos.
KR100490893B1 (ko) * 2002-10-11 2005-05-23 (주) 비엔씨바이오팜 2-메톡시-1,3,5-트리아진 유도체, 그 제조방법 및 이를 포함하는 항바이러스용 약학적 조성물
GB0226583D0 (en) * 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
FR2847253B1 (fr) * 2002-11-19 2007-05-18 Aventis Pharma Sa Nouveaux derives de pyridazinones a titre de medicaments et compositions pharmaceutiques les renfermant
US7309701B2 (en) 2002-11-19 2007-12-18 Sanofi-Aventis Deutschland Gmbh Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
US7462613B2 (en) 2002-11-19 2008-12-09 Sanofi-Aventis Deutschland Gmbh Pyridazinone derivatives as pharmaceuticals and pharmaceutical compositions containing them
EA013811B1 (ru) * 2002-11-21 2010-08-30 Новартис Вэксинес Энд Дайэгностикс, Инк. 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака
US7601718B2 (en) * 2003-02-06 2009-10-13 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US7157455B2 (en) * 2003-02-10 2007-01-02 Hoffmann-La Roche Inc. 4-Aminopyrimidine-5-one derivatives
EP1644338A1 (en) * 2003-04-01 2006-04-12 Aponetics AG 2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases
WO2004105764A1 (en) * 2003-06-02 2004-12-09 Astrazeneca Ab (3- ((quinazolin-4-yl) amino )-1h-pyrazol-1-yl) acetamide derivatives and related compounds as aurora kinase inhibitors for the treatment of proliferative diseases such as cancer
WO2004112719A2 (en) 2003-06-19 2004-12-29 Smithkline Beecham Corporation Chemical compounds
TWI372050B (en) * 2003-07-03 2012-09-11 Astex Therapeutics Ltd (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles
US8309562B2 (en) 2003-07-03 2012-11-13 Myrexis, Inc. Compounds and therapeutical use thereof
AU2004253967B2 (en) 2003-07-03 2010-02-18 Cytovia, Inc. 4-arylamino-quinazolines as activators of caspases and inducers of apoptosis
GB0315966D0 (en) * 2003-07-08 2003-08-13 Cyclacel Ltd Compounds
AU2004261459B2 (en) 2003-07-22 2008-06-26 Astex Therapeutics Limited 3, 4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
CA2533474A1 (en) * 2003-07-30 2005-02-10 Shudong Wang 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
HRP20130602T1 (en) 2003-07-30 2013-07-31 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
US20050221357A1 (en) * 2003-09-19 2005-10-06 Mark Shannon Normalization of gene expression data
US7417726B2 (en) * 2003-09-19 2008-08-26 Applied Biosystems Inc. Normalization of data using controls
US20060024690A1 (en) * 2003-09-19 2006-02-02 Kao H P Normalization of data using controls
WO2005030131A2 (en) * 2003-09-23 2005-04-07 Replidyne, Inc Bis-quinazoline compounds for the treatment of bacterial infections
BRPI0415398A (pt) 2003-10-17 2006-12-19 Astrazeneca Ab composto, composição farmacêutica, processo para a preparação da mesma, uso de um composto, método de tratamento de cáncer, e, processo para preparação de um composto
EP1694671A2 (en) * 2003-12-04 2006-08-30 Vertex Pharmaceuticals Incorporated Quinoxalines useful as inhibitors of protein kinases
RU2006124559A (ru) * 2003-12-09 2008-01-20 Вертекс Фармасьютикалз Инкорпорейтед (Us) Производные нафтиридина и применение указанных производныхых в качестве модуляторов мускариновых рецепторов
US7572914B2 (en) 2003-12-19 2009-08-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
TW200530235A (en) 2003-12-24 2005-09-16 Renovis Inc Bicycloheteroarylamine compounds as ion channel ligands and uses thereof
WO2005077938A1 (en) * 2004-02-11 2005-08-25 Amgen Inc. Vanilloid receptor ligands and their use in treatments
EP1723427A2 (en) * 2004-02-26 2006-11-22 Bayer HealthCare AG Diagnostics and therapeutics for diseases associated with glycogen synthase kinase 3 beta (gsk3b)
CA2560111A1 (en) * 2004-03-15 2005-09-22 Takeda Pharmaceutical Company Limited Aminophenylpropanoic acid derivative
CA2562244A1 (en) * 2004-04-07 2005-10-27 Takeda Pharmaceutical Company Limited Cyclic compounds
JP2007533717A (ja) * 2004-04-21 2007-11-22 アストラゼネカ アクチボラグ 化合物
EP1763524A1 (en) * 2004-04-23 2007-03-21 Takeda San Diego, Inc. Indole derivatives and use thereof as kinase inhibitors
EP1751136B1 (en) * 2004-05-07 2014-07-02 Amgen Inc. Nitrogenated heterocyclic derivatives as protein kinase modulators and use for the treatment of angiogenesis and cancer
US7793137B2 (en) 2004-10-07 2010-09-07 Cisco Technology, Inc. Redundant power and data in a wired data telecommunincations network
AU2012200416B2 (en) * 2004-05-14 2014-07-31 Millennium Pharmaceuticals, Inc. "Compounds and methods for inhibiting mitotic progression by inhibition of Aurora kinase"
EP1905773B1 (en) * 2004-05-14 2012-07-18 Millennium Pharmaceuticals, Inc. Compounds and methods for inhibiting mitotic progression by inhibition of aurora kinase
US7358258B2 (en) * 2004-05-14 2008-04-15 Vertex Pharmaceuticals Incorporated Prodrugs of an ERK protein kinase inhibitor
KR101748290B1 (ko) * 2004-05-14 2017-06-16 밀레니엄 파머슈티컬스 인코퍼레이티드 아우로라 키나아제의 억제에 의해 유사분열 진행을 억제하기 위한 화합물 및 그 방법
US20050255485A1 (en) * 2004-05-14 2005-11-17 Livak Kenneth J Detection of gene duplications
WO2005112923A2 (en) * 2004-05-20 2005-12-01 Bayer Pharmaceuticals Corporation 5-anilino-4-heteroarylpyrazole derivatives useful for the treatment of diabetes
EP1756673A1 (en) * 2004-05-27 2007-02-28 E.I.Du pont de nemours and company Developer for a photopolymer protective layer
WO2006007532A2 (en) * 2004-07-01 2006-01-19 Synta Pharmaceuticals Corp. 2-substituted heteroaryl compounds
WO2006014420A1 (en) * 2004-07-06 2006-02-09 Angion Biomedica Corporation Quinazoline modulators of hepatocyte growth factor / c-met activity for the treatment of cancer
JP2008510734A (ja) 2004-08-18 2008-04-10 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
US7285569B2 (en) 2004-09-24 2007-10-23 Hoff Hoffmann-La Roche Inc. Tricycles, their manufacture and use as pharmaceutical agents
TW200624431A (en) 2004-09-24 2006-07-16 Hoffmann La Roche Phthalazinone derivatives, their manufacture and use as pharmaceutical agents
MX2007003797A (es) * 2004-09-30 2007-04-23 Tibotec Pharm Ltd 5-heterociclil pirimidinas inhibidoras del virus de inmunodeficiencia humana.
KR20070057798A (ko) * 2004-09-30 2007-06-07 티보텍 파마슈티칼즈 리미티드 Hiv를 저해하는 5-탄소환 또는 복소환으로 치환된피리미딘
RU2410379C2 (ru) * 2004-09-30 2011-01-27 Тиботек Фармасьютикалз Лтд. 5-замещенные пиримидины, ингибирующие вич
US7713973B2 (en) 2004-10-15 2010-05-11 Takeda Pharmaceutical Company Limited Kinase inhibitors
KR20070072562A (ko) * 2004-10-29 2007-07-04 반유 세이야꾸 가부시끼가이샤 오로라 a 선택적 억제 활성을 갖는 신규한 아미노피리딘유도체
US7491720B2 (en) 2004-10-29 2009-02-17 Banyu Pharmaceutical Co., Ltd. Aminopyridine derivatives having Aurora A selective inhibitory action
JP2008519034A (ja) 2004-11-03 2008-06-05 バーテックス ファーマシューティカルズ インコーポレイテッド イオンチャネル調節剤としてのピリミジン誘導体および使用方法
KR20070086188A (ko) 2004-11-17 2007-08-27 미카나 테라퓨틱스, 인크. 키나제 억제제
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
US20060128710A1 (en) * 2004-12-09 2006-06-15 Chih-Hung Lee Antagonists to the vanilloid receptor subtype 1 (VR1) and uses thereof
CA2588220A1 (en) * 2004-12-23 2006-06-29 Pfizer Products Inc. Heteroaromatic derivatives useful as anticancer agents
BRPI0519759A2 (pt) 2004-12-30 2009-03-10 Astex Therapeutics Ltd composiÇÕes farmacÊuticas
CA2590110C (en) 2004-12-30 2014-06-03 Exelixis, Inc. Kinase modulators and method of use
EP1833482A4 (en) 2005-01-03 2011-02-16 Myriad Genetics Inc COMPOUNDS AND ITS THERAPEUTIC USE
US8258145B2 (en) 2005-01-03 2012-09-04 Myrexis, Inc. Method of treating brain cancer
CN101115761B (zh) 2005-01-19 2012-07-18 里格尔药品股份有限公司 2,4-嘧啶二胺化合物的前药及其应用
AR054425A1 (es) * 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
EP1871765B1 (en) * 2005-01-26 2009-12-09 Schering Corporation 3-(indazol-5-yl)-(1,2,4)triazine derivatives and related compounds as protein kinase inhibitors for the treatment of cancer
US8324252B2 (en) 2005-02-04 2012-12-04 Astrazeneca Ab Pyrazolylaminopyridine derivatives useful as kinase inhibitors
DK1853602T3 (da) * 2005-02-16 2010-09-20 Astrazeneca Ab Kemiske forbindelser
AU2006215386B2 (en) * 2005-02-16 2009-06-11 Astrazeneca Ab Chemical compounds
CA2600144A1 (en) * 2005-03-15 2006-09-28 Irm Llc Compounds and compositions as protein kinase inhibitors
WO2006100461A1 (en) * 2005-03-23 2006-09-28 Astrazeneca Ab 2-AZETIDINYL-4-(lH-PYRAZOL-3-YLAMINO)PYRIMIDINES AS INHIBITORS OF INSULIN-LIKE GROWTH FACTOR-I RECEPTOR ACTIVITY
US7402596B2 (en) 2005-03-24 2008-07-22 Renovis, Inc. Bicycloheteroaryl compounds as P2X7 modulators and uses thereof
DK1869032T3 (da) * 2005-04-05 2008-11-10 Astrazeneca Ab Pyrimidindervater til anvendelse som anticancermidler
GB0507347D0 (en) * 2005-04-12 2005-05-18 Astrazeneca Ab Chemical compounds
AU2006233537A1 (en) 2005-04-14 2006-10-19 F. Hoffmann-La Roche Ag Aminopyrazole derivatives, their manufacture and use as pharmaceutical agents
CN101208093A (zh) * 2005-04-27 2008-06-25 阿斯利康(瑞典)有限公司 吡唑-嘧啶衍生物在治疗疼痛中的用途
CN101166732B (zh) * 2005-04-28 2013-04-17 田边三菱制药株式会社 氰基吡啶衍生物及其作为药物的应用
WO2006117212A2 (en) 2005-05-04 2006-11-09 Develogen Aktiengesellschaft Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders
JP5198256B2 (ja) 2005-05-04 2013-05-15 エボテク エージー 縮合複素環式化合物、並びにそれらの組成物及び使用
EP1888561A1 (en) * 2005-05-05 2008-02-20 AstraZeneca AB Pyrazolyl-amino- substituted pyrimidines and their use in the treatment of cancer
WO2006123113A2 (en) * 2005-05-16 2006-11-23 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8193206B2 (en) 2005-06-14 2012-06-05 Taigen Biotechnology Co., Ltd. Pyrimidine compounds
WO2006138304A2 (en) 2005-06-14 2006-12-28 Taigen Biotechnology Pyrimidine compounds
EP1746096A1 (en) 2005-07-15 2007-01-24 4Sc Ag 2-Arylbenzothiazole analogues and uses thereof in the treatment of cancer
WO2007022384A2 (en) * 2005-08-18 2007-02-22 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
WO2007023382A2 (en) * 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
AU2006282896A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
KR101487027B1 (ko) * 2005-09-30 2015-01-28 미카나 테라퓨틱스, 인크. 치환된 피라졸 화합물
UA96427C2 (en) * 2005-09-30 2011-11-10 Мийкана Терапьютикс, Инк. Substituted pyrazole compounds
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
WO2007047978A2 (en) 2005-10-21 2007-04-26 Braincells, Inc. Modulation of neurogenesis by pde inhibition
HRP20120824T1 (hr) 2005-10-28 2012-11-30 Astrazeneca Ab Derivati 4-(3-aminopirazol) pirimidina za uporabu kao inhibitori tirozin kinaze u lijeäśenju karcinoma
WO2007053596A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
NZ567858A (en) * 2005-11-01 2011-08-26 Array Biopharma Inc Pyridine compounds useful as Glucokinase activators
ES2435081T3 (es) * 2005-11-03 2013-12-18 Vertex Pharmaceuticals Incorporated Aminopirimidinas útiles como inhibidores de las cinasas
DE602006021776D1 (de) * 2005-11-16 2011-06-16 Vertex Pharma Als kinaseinhibitoren geeignete aminopyrimidine
US8546404B2 (en) 2005-12-13 2013-10-01 Merck Sharp & Dohme Compounds that are ERK inhibitors
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
WO2007077435A1 (en) 2005-12-30 2007-07-12 Astex Therapeutics Limited Pharmaceutical compounds
US20070213319A1 (en) * 2006-01-11 2007-09-13 Angion Biomedica Corporation Modulators of hepatocyte growth factor/c-Met activity
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
CN101415674A (zh) 2006-02-16 2009-04-22 先灵公司 作为erk抑制剂的吡咯烷衍生物
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
PE20080145A1 (es) 2006-03-21 2008-02-11 Janssen Pharmaceutica Nv Tetrahidro-pirimidoazepinas como moduladores de trpv1
RU2480464C2 (ru) * 2006-03-30 2013-04-27 Тиботек Фармасьютикалз Лтд. 5-амидо-замещенные пиримидины, ингибирующие вич
MX2008012482A (es) * 2006-03-31 2008-10-10 Abbott Lab Compuestos de indazol.
PT2007391E (pt) 2006-04-07 2013-03-11 Novartis Ag Combinação compreendendo: a) um composto de pirimidil-aminobenzamida e b) um inibidor da cinase thr315ile
KR20080109096A (ko) 2006-04-14 2008-12-16 프라나 바이오테크놀로지 리미티드 연령 관련 황반 변성(에이엠디)의 치료 방법
JP5161072B2 (ja) * 2006-04-27 2013-03-13 Msd株式会社 オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
EP2026813A2 (en) 2006-05-09 2009-02-25 Braincells, Inc. 5 ht receptor mediated neurogenesis
EP2382975A3 (en) 2006-05-09 2012-02-29 Braincells, Inc. Neurogenesis by modulating angiotensin
NZ574038A (en) 2006-06-27 2011-12-22 Takeda Pharmaceutical Fused cyclic compounds as GPR40 receptor function modulators, for treating diabetes
EP2043635A2 (en) * 2006-06-29 2009-04-08 Astex Therapeutics Limited Pharmaceutical combinations
JP5523829B2 (ja) 2006-06-29 2014-06-18 アステックス、セラピューティックス、リミテッド 複合薬剤
CN101484426A (zh) * 2006-06-30 2009-07-15 协和发酵麒麟株式会社 Aurora抑制剂
JP2009541480A (ja) * 2006-06-30 2009-11-26 アストラゼネカ アクチボラグ 癌の治療において有用なピリミジン誘導体
CA2656290A1 (en) 2006-07-05 2008-01-10 Exelixis, Inc. Methods of using igf1r and abl kinase modulators
CA2666193A1 (en) 2006-08-08 2008-02-14 Sanofi-Aventis Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
JP2010500352A (ja) * 2006-08-09 2010-01-07 ミレニアム・ファーマシューティカルズ・インコーポレイテッド 有糸分裂の進行を阻止するためのピリドベンゾアゼピン化合物および方法
US7832809B2 (en) * 2006-08-11 2010-11-16 Schlumberger Technology Corporation Degradation assembly shield
JP2008081492A (ja) * 2006-08-31 2008-04-10 Banyu Pharmaceut Co Ltd オーロラa選択的阻害作用を有する新規アミノピリジン誘導体
CA2662491A1 (en) * 2006-09-08 2008-03-13 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
JP2010505961A (ja) * 2006-10-09 2010-02-25 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
WO2008044041A1 (en) 2006-10-12 2008-04-17 Astex Therapeutics Limited Pharmaceutical combinations
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
WO2008053812A1 (fr) * 2006-10-27 2008-05-08 Mitsubishi Tanabe Pharma Corporation Dérivé de cyanopyridine et son utilisation médicale
AU2007317435A1 (en) * 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
CL2007003244A1 (es) 2006-11-16 2008-04-04 Millennium Pharm Inc Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer.
ES2347721T3 (es) * 2006-12-19 2010-11-03 Vertex Pharmaceuticals, Inc. Aminopirimidinas utiles como inhibidores de proteina quinasas.
CA2674185C (en) * 2006-12-29 2017-02-28 Tibotec Pharmaceuticals Ltd. Hiv inhibiting 5,6-substituted pyrimidines
EP2114901B1 (en) * 2006-12-29 2014-04-09 Janssen R&D Ireland Hiv inhibiting 6-substituted pyrimidines
WO2008098058A1 (en) 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
CA2680122A1 (en) 2007-03-05 2008-09-18 Kyowa Hakko Kirin Co., Ltd. Pharmaceutical composition
ES2374335T3 (es) * 2007-03-09 2012-02-15 Vertex Pharmaceuticals Incorporated Aminopirimidinas útiles como inhibidores de proteína quinasas.
WO2008112642A1 (en) * 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
JP2010520887A (ja) 2007-03-09 2010-06-17 バーテックス ファーマシューティカルズ インコーポレイテッド 蛋白キナーゼの阻害剤として有用なアミノピリジン
AU2008228963A1 (en) * 2007-03-20 2008-09-25 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2008117050A1 (en) * 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer
AU2008240313A1 (en) 2007-04-13 2008-10-23 Aj Park Aminopyrimidines useful as kinase inhibitors
WO2008129255A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
WO2008129380A1 (en) 2007-04-18 2008-10-30 Pfizer Products Inc. Sulfonyl amide derivatives for the treatment of abnormal cell growth
JP5389786B2 (ja) * 2007-05-02 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド キナーゼ阻害として有用なアミノピリミジン
CA2688584A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
CA2685876A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
UA99459C2 (en) 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
US20100137398A1 (en) * 2007-05-04 2010-06-03 Novartis Ag Use of hdac inhibitors for the treatment of gastrointestinal cancers
WO2008147626A2 (en) * 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
KR101294731B1 (ko) * 2007-06-04 2013-08-16 삼성디스플레이 주식회사 어레이 기판, 이를 갖는 표시패널 및 이의 제조방법
EP2166849A4 (en) * 2007-06-11 2010-09-15 Miikana Therapeutics Inc SUBSTITUTED PYRAZOL COMPOUNDS
JP2010532756A (ja) * 2007-07-06 2010-10-14 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド mTORC1及びmTORC2の両方の阻害剤を含む組み合わせ抗癌療法
WO2009007753A2 (en) * 2007-07-11 2009-01-15 Astrazeneca Ab 4- (3-aminopyrazole) -pyrimidine derivativee and their use as tyrosine kinase inhibitors for the treatment of cancer
US8415340B2 (en) * 2007-07-25 2013-04-09 Bristol-Myers Squibb Company Triazine kinase inhibitors
WO2009013545A2 (en) * 2007-07-26 2009-01-29 Astrazeneca Ab Chemical compounds
MX2010001137A (es) * 2007-07-31 2010-03-31 Vertex Pharma Procesopara preparar 5-fluoro-1h-pirazol[3,4-b]piridin-3-amina y derivados del mismo.
TW200906818A (en) * 2007-07-31 2009-02-16 Astrazeneca Ab Chemical compounds
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
WO2009027736A2 (en) * 2007-08-27 2009-03-05 Astrazeneca Ab 2,4 diaminopyrimid'lnes for the treatment of myeloproliferative disorders and cancer
EP2727910B1 (en) 2007-09-21 2016-03-16 Array Biopharma, Inc. Pyridin-2-yl-thiourea and Pyridin-2-yl-amine derivatives as intermediates for the preparation of Pyridin-2yl-amino-1,2,4-thiadiazole glucokinase activators
PT2214487E (pt) 2007-10-11 2014-02-20 Glaxosmithkline Llc Novos inibidores de seh e sua utilização
JP5562865B2 (ja) 2007-12-17 2014-07-30 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Trpv1のイミダゾロ−、オキサゾロ−、及びチアゾロピリミジン・モジュレーター
US20090270418A1 (en) * 2008-01-09 2009-10-29 Marianne Sloss Pyrazole pyrazine amine compounds as kinase inhibitors, compositions thereof and methods of treatment therewith
EP2242745A1 (de) * 2008-02-07 2010-10-27 Sanofi-Aventis Neue phenyl-substituierte imidazolidine, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
US8716483B2 (en) * 2008-02-21 2014-05-06 Merck Sharp & Dohme Corp. Compounds that are ERK inhibitors
ES2531398T3 (es) * 2008-02-22 2015-03-13 Msd Kk Nuevos derivados de aminopiridina que tienen una acción inhibidora selectiva de Aurora A
NZ588989A (en) 2008-04-21 2012-03-30 Taigen Biotechnology Co Ltd Heterocyclic compounds comprising pyrimidine, piperazine and amine.
US8844033B2 (en) 2008-05-27 2014-09-23 The Trustees Of Columbia University In The City Of New York Systems, methods, and media for detecting network anomalies using a trained probabilistic model
WO2009150462A1 (en) * 2008-06-11 2009-12-17 Astrazeneca Ab Tricyclic 2,4-diamin0-l,3,5-triazine derivatives useful for the treatment of cancer and myeloproliferative disorders
EP2310372B1 (en) 2008-07-09 2012-05-23 Sanofi Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
ES2432821T3 (es) * 2008-07-31 2013-12-05 Genentech, Inc. Compuestos de pirimidina, composiciones y métodos de utilización
CN102215816A (zh) * 2008-09-03 2011-10-12 沃泰克斯药物股份有限公司 共晶和包含所述共晶的药物制剂
MY156789A (en) * 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
EP2340248B1 (en) * 2008-09-15 2017-05-31 The Regents of The University of California Methods and compositions for modulating ire1, src, and abl activity
KR20110071098A (ko) * 2008-09-30 2011-06-28 아스트라제네카 아베 복소환 jak 키나제 억제제
US8759362B2 (en) * 2008-10-24 2014-06-24 Purdue Pharma L.P. Bicycloheteroaryl compounds and their use as TRPV1 ligands
WO2010056758A1 (en) * 2008-11-12 2010-05-20 Yangbo Feng Quinazoline derivatives as kinase inhibitors
TW201021855A (en) 2008-11-13 2010-06-16 Taigen Biotechnology Co Ltd Lyophilization formulation
WO2010068601A1 (en) 2008-12-08 2010-06-17 Sanofi-Aventis A crystalline heteroaromatic fluoroglycoside hydrate, processes for making, methods of use and pharmaceutical compositions thereof
PA8851101A1 (es) 2008-12-16 2010-07-27 Lilly Co Eli Compuesto amino pirazol
WO2010070060A1 (en) 2008-12-19 2010-06-24 Nerviano Medical Sciences S.R.L. Bicyclic pyrazoles as protein kinase inhibitors
WO2010074724A1 (en) 2008-12-22 2010-07-01 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-cd20 antibodies
US8809343B2 (en) 2008-12-26 2014-08-19 Fudan University Pyrimidine derivative, preparation method and use thereof
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
CN105601619A (zh) * 2009-02-27 2016-05-25 埃姆比特生物科学公司 调控jak激酶的喹唑啉衍生物和其使用方法
CA2660962A1 (en) 2009-03-31 2010-09-30 Astellas Pharma Inc. Novel pharmaceutical composition for treatment of schizophrenia
US8399663B2 (en) 2009-04-03 2013-03-19 Astellas Pharma Inc. Salt of 1,3,5-triazine-2,4,6-triamine derivative
JO3635B1 (ar) 2009-05-18 2020-08-27 Millennium Pharm Inc مركبات صيدلانية صلبة وطرق لانتاجها
EP2440050A4 (en) * 2009-06-08 2013-04-03 California Capital Equity Llc TRIAZINE DERIVATIVES AND THEIR THERAPEUTIC APPLICATION
BRPI1010887A2 (pt) * 2009-06-08 2016-12-27 California Capital Equity Llc derivados de triazina e suas aplicações terapêuticas.
KR20120016676A (ko) * 2009-06-09 2012-02-24 아브락시스 바이오사이언스, 엘엘씨 우레이도페닐치환 트리아진 유도체와 이들의 치료적 용도
JP2012529517A (ja) * 2009-06-09 2012-11-22 アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー ベンジル置換トリアジン誘導体類及びそれらの治療応用
KR20120026613A (ko) * 2009-06-09 2012-03-19 아브락시스 바이오사이언스, 엘엘씨 스티릴-트리아진 유도체와 이들의 치료적 용도
CA2765030C (en) 2009-06-09 2015-10-27 California Capital Equity, Llc Triazine derivatives and their therapeutical applications
EP2443106A1 (en) * 2009-06-18 2012-04-25 Cellzome Limited Heterocyclylaminopyrimidines as kinase inhibitors
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TWI468402B (zh) 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β-類澱粉生成之化合物
US8785608B2 (en) 2009-08-26 2014-07-22 Sanofi Crystalline heteroaromatic fluoroglycoside hydrates, pharmaceuticals comprising these compounds and their use
WO2011034907A2 (en) * 2009-09-16 2011-03-24 Avila Therapeutics, Inc. Protein kinase conjugates and inhibitors
KR102077004B1 (ko) * 2009-11-13 2020-02-13 인튜어티브 서지컬 오퍼레이션즈 인코포레이티드 여분의 닫힘 메커니즘을 구비한 단부 작동기
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
SG181965A1 (en) 2009-12-30 2012-08-30 Avila Therapeutics Inc Ligand-directed covalent modification of protein
SA111320200B1 (ar) * 2010-02-17 2014-02-16 ديبيوفارم اس ايه مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة
WO2011103089A1 (en) 2010-02-19 2011-08-25 Millennium Pharmaceuticals, Inc. Crystalline forms of sodium 4-{[9-chloro-7-(2-fluoro-6--methoxyphenyl)-5h -pyrimido[5,4-d][2]benzazepin-2yl]amino}-2-methoxybenzoate
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2571359A4 (en) * 2010-05-20 2013-10-23 Merck Sharp & Dohme NOVEL PROLYLCARBOXYPEPTIDASE HEMMER
EP2571867B1 (en) 2010-05-21 2015-11-04 Noviga Research AB Novel pyrimidine derivatives
HUE029196T2 (hu) 2010-06-04 2017-02-28 Hoffmann La Roche Aminoprimidin-származékok mint LRRK2 modulátorok
US8933024B2 (en) 2010-06-18 2015-01-13 Sanofi Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
BR112013002164B1 (pt) 2010-07-29 2021-11-09 Oryzon Genomics S.A. Inibidores de desmetilase à base de arilciclopropilamina de lsd1, seus usos, e composição farmacêutica
JP5933554B2 (ja) 2010-09-01 2016-06-15 アムビト ビオスシエンセス コルポラチオン 光学活性のあるピラゾリルアミノキナゾリン及びその医薬組成物及び使用方法
EP2611502A1 (en) * 2010-09-01 2013-07-10 Ambit Biosciences Corporation Adenosine a3 receptor modulating compounds and methods of use thereof
WO2012030914A1 (en) * 2010-09-01 2012-03-08 Ambit Boisciences Corporation 4-azolylaminoquinazoline derivatives and methods of use thereof
EP2663553B1 (en) * 2010-09-01 2015-08-26 Ambit Biosciences Corporation Quinoline and isoquinoline derivatives for use as jak modulators
WO2012030948A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation Quinazoline compounds and methods of use thereof
WO2012030910A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation 2-cycloquinazoline derivatives and methods of use thereof
CN103270030B (zh) * 2010-09-01 2016-01-20 埃姆比特生物科学公司 吡唑基氨基喹唑啉的氢溴酸盐
WO2012059932A1 (en) 2010-11-01 2012-05-10 Aurigene Discovery Technologies Limited 2, 4 -diaminopyrimidine derivatives as protein kinase inhibitors
US8815882B2 (en) 2010-11-10 2014-08-26 Genentech, Inc. Pyrazole aminopyrimidine derivatives as LRRK2 modulators
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
US8710050B2 (en) 2011-03-08 2014-04-29 Sanofi Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2683703B1 (de) 2011-03-08 2015-05-27 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2683701B1 (de) 2011-03-08 2014-12-24 Sanofi Mit benzyl- oder heteromethylengruppen substituierte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
US8901114B2 (en) 2011-03-08 2014-12-02 Sanofi Oxathiazine derivatives substituted with carbocycles or heterocycles, method for producing same, drugs containing said compounds, and use thereof
WO2012120051A1 (de) 2011-03-08 2012-09-13 Sanofi Mit adamantan- oder noradamantan substituierte benzyl-oxathiazinderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2012120050A1 (de) 2011-03-08 2012-09-13 Sanofi Neue substituierte phenyl-oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2012120053A1 (de) 2011-03-08 2012-09-13 Sanofi Verzweigte oxathiazinderivate, verfahren zu deren herstellung, ihre verwendung als medikament sowie sie enthaltendes arzneimittel und deren verwendung
AU2012230229A1 (en) 2011-03-24 2013-10-10 Noviga Research Ab Novel pyrimidine derivatives
CN104024248A (zh) * 2011-08-25 2014-09-03 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸pak1抑制剂
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP5914667B2 (ja) * 2011-09-22 2016-05-11 ファイザー・インク ピロロピリミジンおよびプリン誘導体
WO2013045413A1 (en) 2011-09-27 2013-04-04 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
JP6026544B2 (ja) 2011-09-27 2016-11-16 ノバルティス アーゲー 変異体idhの阻害剤としての3−ピリミジン−4−イル−オキサゾリジン−2−オン類
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
KR20140103972A (ko) 2011-12-22 2014-08-27 에프. 호프만-라 로슈 아게 세린/트레오닌 키나아제 억제제로서의 2,4-다이아민-피리미딘 유도체
US9447051B2 (en) * 2012-02-17 2016-09-20 Abbvie Inc. Diaminopyrimidines and uses thereof
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
TWI485146B (zh) * 2012-02-29 2015-05-21 Taiho Pharmaceutical Co Ltd Novel piperidine compounds or salts thereof
CN104334545A (zh) 2012-03-16 2015-02-04 埃克希金医药品有限公司 3,5-二氨基吡唑激酶抑制剂
US20130303519A1 (en) 2012-03-20 2013-11-14 Millennium Pharmaceuticals, Inc. Methods of treating cancer using aurora kinase inhibitors
SI3459942T1 (sl) 2012-04-24 2021-05-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
RU2641895C2 (ru) * 2012-05-24 2018-01-23 Целльзом Лимитид ГЕТЕРОЦИКЛИЛЬНЫЕ ПИРИМИДИНОВЫЕ АНАЛОГИ В КАЧЕСТВЕ ИНГИБИТОРОВ Tук2
BR112014032346A2 (pt) 2012-06-26 2017-06-27 Del Mar Pharmaceuticals métodos para tratamento de malignidades resistentes ao inibidor de tirosina-quinase em pacientes com polimorfismos genéticos ou desregulações de ahi1 mutações empregando dianidrogalactitol, diacetildianidrogalactitol, dibromodulcitol, ou análogos ou derivados destes
SG11201500005SA (en) * 2012-07-10 2015-01-29 Ares Trading Sa Pyrimidine pyrazolyl derivatives
JP5791817B2 (ja) * 2012-09-19 2015-10-07 大鵬薬品工業株式会社 溶出性及び/又は吸収性が改善された経口投与用医薬組成物
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
CN103059002B (zh) * 2012-12-31 2015-04-22 中山大学 具有Aurora激酶抑制活性的嘧啶衍生物及其制备方法以及应用
CN103191120B (zh) * 2012-12-31 2015-11-25 刘强 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗肿瘤的药物中的用途
CN103202843B (zh) * 2012-12-31 2015-04-29 刘强 一种嘧啶衍生物在制备预防和/或治疗和/或辅助治疗癌症的药物中的用途
CN103910716A (zh) * 2013-01-07 2014-07-09 华东理工大学 2,4-二取代-环烷基[d]嘧啶类化合物及其用途
SG11201507203RA (en) 2013-03-12 2015-10-29 Vertex Pharma Dna-pk inhibitors
PE20151939A1 (es) 2013-03-14 2016-01-08 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
EP3842424B1 (en) 2013-03-15 2024-12-11 The Trustees of Columbia University in the City of New York Map kinase modulators and uses thereof in the tretament of tauopathies
WO2014153509A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase
WO2015003355A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN105764502A (zh) 2013-07-26 2016-07-13 现代化制药公司 改善比生群及其类似物及衍生物的治疗益处的组合方法
WO2015028848A1 (en) * 2013-09-02 2015-03-05 Piramal Enterprises Limited Bicyclic heterocyclic compounds as multi-kinase inhibitors
NZ631142A (en) 2013-09-18 2016-03-31 Axikin Pharmaceuticals Inc Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors
JP6408569B2 (ja) 2013-10-17 2018-10-17 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Dna−pk阻害剤としての(s)−n−メチル−8−(1−((2’−メチル−[4,5’−ビピリミジン]−6−イル)アミノ)プロパン−2−イル)キノリン−4−カルボキサミドおよびその重水素化誘導体の共結晶
ES2676734T3 (es) 2013-10-18 2018-07-24 Syros Pharmaceuticals, Inc. Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
SI3089971T1 (sl) 2014-01-01 2020-11-30 Medivation Technologies Llc Spojine in postopki za uporabo
US10258585B2 (en) 2014-03-13 2019-04-16 Neuroderm, Ltd. DOPA decarboxylase inhibitor compositions
HUE064818T2 (hu) 2014-03-13 2024-04-28 Neuroderm Ltd Dopa dekarboxiláz inhibitor készítmények
WO2015148867A1 (en) * 2014-03-28 2015-10-01 Calitor Sciences, Llc Substituted heteroaryl compounds and methods of use
ES2823825T3 (es) 2014-04-04 2021-05-10 Iomet Pharma Ltd Derivados de indol para su uso en medicina
US20170165230A1 (en) 2014-04-09 2017-06-15 Christopher Rudd Use of gsk-3 inhibitors or activators which modulate pd-1 or t-bet expression to modulate t cell immunity
CN105367555B (zh) * 2014-08-07 2019-06-25 广东东阳光药业有限公司 取代的杂芳基化合物及其组合物和用途
CA2972239A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2016106309A1 (en) 2014-12-23 2016-06-30 Axikin Pharmaceuticals, Inc. 3,5-diaminopyrazole kinase inhibitors
US10227343B2 (en) * 2015-01-30 2019-03-12 Vanderbilt University Isoquiniline and napthalene-substituted compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
JP6861166B2 (ja) 2015-03-27 2021-04-21 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド サイクリン依存性キナーゼの阻害剤
WO2016166604A1 (en) 2015-04-17 2016-10-20 Ludwig Institute For Cancer Research Ltd Plk4 inhibitors
JP6692836B2 (ja) 2015-05-28 2020-05-13 セラヴァンス バイオファーマ アール&ディー アイピー, エルエルシー Jakキナーゼ阻害剤としてのナフチリジン化合物
JP2018135268A (ja) * 2015-06-05 2018-08-30 大日本住友製薬株式会社 新規ヘテロアリールアミノ−3−ピラゾール誘導体およびその薬理学上許容される塩
WO2017015316A1 (en) 2015-07-21 2017-01-26 Millennium Pharmaceuticals, Inc. Administration of aurora kinase inhibitor and chemotherapeutic agents
CA2996978A1 (en) 2015-09-09 2017-03-16 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
JP2018527362A (ja) 2015-09-11 2018-09-20 サンシャイン・レイク・ファーマ・カンパニー・リミテッドSunshine Lake Pharma Co.,Ltd. 置換されたヘテロアリール化合物および使用方法
EA201800367A1 (ru) 2015-12-10 2019-02-28 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Способы лечения болезни хантингтона
CN105503754B (zh) * 2015-12-11 2017-11-17 浙江大学 2‑氨基‑4‑苄基‑6‑吗啉‑1,3,5‑三嗪及其制备和应用
CN105384702B (zh) * 2015-12-11 2018-04-10 浙江大学 三取代均三嗪类化合物及其制备方法
CN105399695B (zh) * 2015-12-11 2019-04-19 浙江大学 三嗪类化合物及其制备方法和用途
EP3390387B1 (en) 2015-12-18 2021-11-17 Bayer Pharma Aktiengesellschaft Heteroarylbenzimidazole compounds
MX390482B (es) 2016-03-14 2025-03-11 Afferent Pharmaceuticals Inc Pirimidinas y variantes de estas, y usos de estas.
JP6902045B2 (ja) 2016-03-25 2021-07-14 アファレント ファーマシューティカルズ インコーポレイテッド ピリミジンおよびそのバリアント、ならびにそのための使用
MX377180B (es) 2016-04-28 2025-03-07 Theravance Biopharma R&D Ip Llc Compuestos de pirimidina como inhibidores de la quinasa jak.
WO2017207534A1 (en) 2016-06-03 2017-12-07 Bayer Pharma Aktiengesellschaft Substituted heteroarylbenzimidazole compounds
US11110108B2 (en) 2016-09-27 2021-09-07 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors
US10858319B2 (en) 2016-10-03 2020-12-08 Iomet Pharma Ltd. Indole derivatives for use in medicine
US10968227B2 (en) * 2016-11-08 2021-04-06 Vanderbilt University Isoquinoline ether compounds as mGluR4 allosteric potentiators, compositions, and methods of treating neurological dysfunction
CN108239071B (zh) * 2016-12-27 2020-12-04 沈阳药科大学 酰胺及硫代酰胺类衍生物及其制备方法和应用
FR3064275B1 (fr) 2017-03-21 2019-06-07 Arkema France Procede de chauffage et/ou climatisation d'un vehicule
EP3630731B1 (en) 2017-05-30 2023-08-09 Basf Se Pyridine and pyrazine compounds for combating phytopathogenic fungi
BR112019025740A2 (pt) 2017-06-05 2020-06-23 Ptc Therapeutics, Inc. Compostos para tratar a doença de huntington
MX2019015580A (es) 2017-06-28 2020-07-28 Ptc Therapeutics Inc Metodos para tratar la enfermedad de huntington.
US11382918B2 (en) 2017-06-28 2022-07-12 Ptc Therapeutics, Inc. Methods for treating Huntington's Disease
CN110582489B (zh) 2017-06-30 2023-10-27 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
KR102469161B1 (ko) 2017-06-30 2022-11-23 베이징 타이드 파마슈티컬 코퍼레이션 리미티드 Rho-관련 단백질 키나아제 억제제, Rho-관련 단백질 키나아제 억제제를 함유하는 약학 조성물, 제조 방법 및 약학 조성물의 용도
ES2930804T3 (es) * 2017-06-30 2022-12-22 Beijing Tide Pharmaceutical Co Ltd Inhibidor de proteína cinasa asociada a RHO, composición farmacéutica que lo comprende, así como método de preparación y uso del mismo
US11440904B2 (en) * 2017-08-28 2022-09-13 Zhihong Chen Substituted pyrimidines, pharmaceutical compositions and therapeutic methods thereof
EP3676264A1 (en) * 2017-08-28 2020-07-08 Acurastem Inc. Pikfyve kinase inhibitors
CN111247142B (zh) 2017-10-27 2022-12-02 施万生物制药研发Ip有限责任公司 作为jak激酶抑制剂的嘧啶化合物
US20200399250A1 (en) * 2017-11-23 2020-12-24 Biomed X Gmbh Pyrimidine Derivatives as Tropomyosin Receptor Kinase A (TRKA) Inhibitors
WO2019113311A1 (en) * 2017-12-06 2019-06-13 Ludwig Institute For Cancer Research Ltd Methods of treating cancer with plk4 inhibitors
JP7399870B2 (ja) 2018-03-27 2023-12-18 ピーティーシー セラピューティクス, インコーポレイテッド ハンチントン病を処置するための化合物
AU2019295632B2 (en) * 2018-06-25 2025-03-06 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
WO2020005882A1 (en) 2018-06-27 2020-01-02 Ptc Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
WO2020005873A1 (en) 2018-06-27 2020-01-02 Ptc Therapeutics, Inc. Heterocyclic and heteroaryl compounds for treating huntington's disease
AU2019294482B2 (en) 2018-06-27 2022-09-01 Ptc Therapeutics, Inc. Heteroaryl compounds for treating Huntington's disease
US20230043863A1 (en) * 2018-11-30 2023-02-09 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Heteroaromatic derivatives for use as regulator, preparation method therefor and use thereof
AU2019413694B2 (en) 2018-12-28 2025-03-20 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
CA3135383A1 (en) 2019-04-24 2020-10-29 Theravance Biopharma R&D Ip, Llc Ester and carbonate pyrimidine compounds as jak kinase inhibitors
US11439641B2 (en) 2019-04-24 2022-09-13 Theravance Biopharma R&D Ip, Llc Pyrimidine JAK inhibitors for the treatment of skin diseases
US20220281842A1 (en) 2019-08-01 2022-09-08 Integral Biosciences Pvt. Ltd. Heterocyclic compounds as kinase inhibitor and uses thereof
US11370803B2 (en) 2019-09-18 2022-06-28 Takeda Pharmaceutical Company Limited Heteroaryl plasma kallikrein inhibitors
ES2987744T3 (es) 2019-09-18 2024-11-18 Takeda Pharmaceuticals Co Inhibidores de calicreína plasmática y usos de los mismos
CN110483493A (zh) * 2019-09-19 2019-11-22 广东工业大学 一种二唑类衍生物及其制备方法和应用
US11331293B1 (en) 2020-11-17 2022-05-17 Neuroderm, Ltd. Method for treatment of Parkinson's disease
US11844754B2 (en) 2020-11-17 2023-12-19 Neuroderm, Ltd. Methods for treatment of Parkinson's disease
US11213502B1 (en) 2020-11-17 2022-01-04 Neuroderm, Ltd. Method for treatment of parkinson's disease
TW202237119A (zh) 2020-12-10 2022-10-01 美商住友製藥腫瘤公司 Alk﹘5抑制劑和彼之用途
JP2024510504A (ja) * 2021-03-17 2024-03-07 武田薬品工業株式会社 血漿カリクレインの多環式インヒビター
CA3213359A1 (en) * 2021-03-26 2022-09-29 Bettina FRANZ Alk-5 inhibitors and uses thereof
CA3217983A1 (en) 2021-05-11 2022-11-17 Chudi Ndubaku Polo like kinase 4 inhibitors
EP4363423A1 (en) 2021-06-28 2024-05-08 Blueprint Medicines Corporation Cdk2 inhibitors
KR102692529B1 (ko) * 2021-07-01 2024-08-08 한국원자력의학원 Mastl-pp2a를 표적화하는 암의 예방 또는 치료용 약학적 조성물
CN116354938B (zh) * 2021-12-28 2024-02-20 沈阳药科大学 一类喹唑啉衍生物与其类似物的制备方法及应用
CN114276302B (zh) * 2022-01-11 2023-07-25 山东百启生物医药有限公司 一种制备2,4-二氨基喹唑啉衍生物的方法
CN116813595B (zh) * 2022-03-28 2025-07-18 上海医药工业研究院有限公司 喹唑啉类衍生物、其制备方法、药物组合物及应用
WO2024003773A1 (en) 2022-07-01 2024-01-04 Pfizer Inc. 2,7-naphthyridine compounds as mastl inhibitors
CN117736198A (zh) * 2022-09-21 2024-03-22 科辉智药生物科技(深圳)有限公司 大环含氮冠醚化合物及其作为蛋白激酶抑制剂的应用
CN115403568B (zh) * 2022-09-21 2023-09-29 中山大学 一种喹唑啉类Aurora A共价抑制剂及其制备方法和应用
WO2024178335A2 (en) * 2023-02-23 2024-08-29 Accutar Biotechnology, Inc. Novel macrocyclic aminopyrazole compounds as cdk2 inhibitors
US12161612B2 (en) 2023-04-14 2024-12-10 Neuroderm, Ltd. Methods and compositions for reducing symptoms of Parkinson's disease

Family Cites Families (102)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) 1964-05-12 J-aminoindazole derivatives
US18436A (en) * 1857-10-20 And saml
US2585906A (en) 1952-02-12 Quaternary salts of pyrimdjines
US3935183A (en) 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3755332A (en) * 1971-07-01 1973-08-28 Ciba Geigy Corp Substituted 4 indazolaminoquinolines
US3998951A (en) * 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
MA18829A1 (fr) 1979-05-18 1980-12-31 Ciba Geigy Ag Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102193L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
SE8102194L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
JPS58124773A (ja) 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc 5−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
EP0136976A3 (de) 1983-08-23 1985-05-15 Ciba-Geigy Ag Verwendung von Phenylpyrimidinen als Pflanzenregulatoren
DE3725638A1 (de) 1987-08-03 1989-02-16 Bayer Ag Neue aryloxy (bzw. thio)aminopyrimidine
JPH0532662A (ja) 1990-11-09 1993-02-09 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
US5714493A (en) * 1991-05-10 1998-02-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5597920A (en) 1992-04-30 1997-01-28 Neurogen Corporation Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
JPH0665237A (ja) 1992-05-07 1994-03-08 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
JP3588116B2 (ja) 1993-10-01 2004-11-10 ノバルティス アクチェンゲゼルシャフト 薬理活性のピリミジンアミン誘導体およびその製造方法
ES2219670T3 (es) 1994-11-10 2004-12-01 Millennium Pharmaceuticals, Inc. Utilizacion de compuestos de pirazola para el tratamiento de la glomerulonefritis, cancer, ateroesclerosis o restenosis.
IL117659A (en) 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
WO1997009325A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
US5935966A (en) 1995-09-01 1999-08-10 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6716575B2 (en) 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
ES2186908T3 (es) 1996-07-13 2003-05-16 Glaxo Group Ltd Compuestos heterociciclos condensados como inhibidores de pproteina-tirosina-quinasas.
JPH10130150A (ja) 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
CA2266519C (en) 1996-10-02 2007-01-23 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
WO1998016502A1 (en) 1996-10-11 1998-04-23 Warner-Lambert Company ASPARTATE ESTER INHIBITORS OF INTERLEUKIN-1β CONVERTING ENZYME
DE19710435A1 (de) * 1997-03-13 1998-09-17 Hoechst Ag Verwendung von Pyrimidinderivaten zur Prävention von Krebs allein oder in Kombination mit anderen therapeutischen Maßnahmen
BR9814817A (pt) 1997-10-10 2002-01-08 Cytovia Inc Inibidores de apoptose de dipeptìdio e o uso dos mesmos
US6267952B1 (en) 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
JP2000026421A (ja) 1998-01-29 2000-01-25 Kumiai Chem Ind Co Ltd ジアリ―ルスルフィド誘導体及び有害生物防除剤
EP1056742B1 (en) 1998-02-17 2003-07-23 Tularik, Inc. Anti-viral pyrimidine derivatives
KR20010041905A (ko) 1998-03-16 2001-05-25 시토비아 인크. 디펩티드 카스파제 억제제 및 이의 용도
AR020590A1 (es) 1998-06-02 2002-05-22 Cadus Pharmaceutical Corp 7-diazapurina-n-6 sustituida, un metodo para su preparacion, composiciones farmaceuticas que la comprenden
US6417185B1 (en) * 1998-06-19 2002-07-09 Chiron Corporation Inhibitors of glycogen synthase kinase 3
WO2000003901A1 (de) * 1998-07-16 2000-01-27 Continental Teves Ag & Co. Ohg Verfahren und vorrichtung zum ermitteln von kritischen fahrzuständen bei im fahrbetrieb befindlichen fahrzeugen
WO2000011003A1 (en) 1998-08-21 2000-03-02 Du Pont Pharmaceuticals Company ISOXAZOLO[4,5-d]PYRIMIDINES AS CRF ANTAGONISTS
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US7262201B1 (en) * 1998-10-08 2007-08-28 Astrazeneca Ab Quinazoline derivatives
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
KR20010108093A (ko) 1999-01-13 2001-12-07 로즈 암스트롱, 크리스틴 에이. 트러트웨인 1-헤테로고리 치환된 디아릴아민
GB9905075D0 (en) * 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
JP4673977B2 (ja) 1999-03-30 2011-04-20 ノバルティス アーゲー 炎症性疾患治療用フタラジン誘導体
JP2003502424A (ja) 1999-06-17 2003-01-21 シオノギ バイオリサーチ コーポレイション Il−12産生の阻害物質
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
CZ2002534A3 (cs) 1999-08-13 2002-07-17 Vertex Pharmaceuticals Incorporated Inhibitory protein-kináz, farmaceutické prostředky, které je obsahují, a jejich pouľití
DE60039059D1 (de) 1999-10-07 2008-07-10 Amgen Inc Triazin-kinase-hemmer
AU1047601A (en) 1999-11-30 2001-06-12 Pfizer Products Inc. 2,4-diaminopyrimidine compounds useful as immunosuppressants
ES2269217T3 (es) 1999-12-02 2007-04-01 Osi Pharmaceuticals, Inc. Compuestos especificos para los receptores a1, a2a y a3 de adenosina y sus usos.
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
CA2396693A1 (en) 1999-12-28 2001-07-05 Stephen T. Wrobleski Cytokine, especially tnf-alpha, inhibitors
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
HUP0202332A2 (en) 2000-02-05 2002-10-28 Vertex Pharma Pyrazole compositions useful as inhibitors of erk
US20030004174A9 (en) * 2000-02-17 2003-01-02 Armistead David M. Kinase inhibitors
GB0004887D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
DE60111509T2 (de) 2000-04-03 2006-05-11 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren von Serin-Proteasen, insbesondere der Hepatitis-C-Virus NS23-Protease
CA2398446A1 (en) 2000-04-18 2001-10-25 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinases
JP3890184B2 (ja) * 2000-05-15 2007-03-07 Necパーソナルプロダクツ株式会社 電源装置及びその電力制御方法、情報処理機器
EP1299381B1 (en) 2000-06-28 2008-05-07 AstraZeneca AB Substituted quinazoline derivatives and their use as inhibitors
AU2001276988B2 (en) 2000-07-21 2007-01-25 Dendreon Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
WO2002018346A1 (en) 2000-08-31 2002-03-07 Pfizer Products Inc. Pyrazole derivatives and their use as protein kinase inhibitors
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE335737T1 (de) 2000-09-15 2006-09-15 Vertex Pharma Isoxazole und ihre verwendung als erk-inhibitoren
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP4105947B2 (ja) 2000-09-15 2008-06-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なトリアゾール化合物
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CN1474815A (zh) 2000-09-20 2004-02-11 Ĭ��ר���ɷ����޹�˾ 4-氨基-喹唑啉
US6641579B1 (en) * 2000-09-29 2003-11-04 Spectrasonics Imaging, Inc. Apparatus and method for ablating cardiac tissue
EP1351691A4 (en) 2000-12-12 2005-06-22 Cytovia Inc SUBSTITUTED 2-ARYL-4-ARYLAMINOPYRIMIDINES AND ANALOGUES AS ACTIVATORS OF CASPASES AND APOPTOSIS INDUCERS, AND USE THEREOF
US6716851B2 (en) 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
DE10061863A1 (de) 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
MXPA03005609A (es) 2000-12-21 2003-10-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de la proteina cinasa.
MY130778A (en) 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
MXPA03008888A (es) 2001-03-29 2005-03-07 Vertex Pharma Inhibidores de n-terminal c-jun cinasas (jnk) y otras proteinas cinasas.
US6642227B2 (en) 2001-04-13 2003-11-04 Vertex Pharmaceuticals Incorporated Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
AU2002305205A1 (en) 2001-04-20 2002-11-05 Jingrong Cao 9-deazaguanine derivatives as inhibitors of gsk-3
EP1404669A2 (en) 2001-05-16 2004-04-07 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
WO2002102800A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
JP4342937B2 (ja) 2001-07-03 2009-10-14 バーテックス ファーマシューティカルズ インコーポレイテッド SrcおよびLckタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
WO2003026666A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4- (5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, as src kinase inhibitors
US6569499B2 (en) * 2001-10-02 2003-05-27 Xerox Corporation Apparatus and method for coating photoreceptor substrates
EP2198867A1 (en) 2001-12-07 2010-06-23 Vertex Pharmaceuticals, Inc. Pyrimidine-based compounds useful as GSK-3 inhibitors
AU2003220299A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
ATE468336T1 (de) 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
WO2003078426A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azolylaminoazine as inhibitors of protein kinases
US6846928B2 (en) 2002-03-15 2005-01-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US20030207873A1 (en) 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
WO2003091246A1 (en) 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
MY141867A (en) 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
WO2004005283A1 (en) 2002-07-09 2004-01-15 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
WO2004013140A1 (en) 2002-08-02 2004-02-12 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of gsk-3
KR101487027B1 (ko) 2005-09-30 2015-01-28 미카나 테라퓨틱스, 인크. 치환된 피라졸 화합물
ES2347721T3 (es) 2006-12-19 2010-11-03 Vertex Pharmaceuticals, Inc. Aminopirimidinas utiles como inhibidores de proteina quinasas.

Also Published As

Publication number Publication date
BR0116411A (pt) 2003-11-11
AU2006201267A1 (en) 2006-04-27
NZ526472A (en) 2004-04-30
EP1345925B1 (en) 2006-05-17
HK1062433A1 (en) 2004-11-05
US7427681B2 (en) 2008-09-23
WO2002050065A3 (en) 2002-10-24
CN1487933A (zh) 2004-04-07
CN1549812A (zh) 2004-11-24
ATE327989T1 (de) 2006-06-15
MXPA03005612A (es) 2003-10-06
KR20030061858A (ko) 2003-07-22
PL210414B1 (pl) 2012-01-31
CA2432131C (en) 2008-07-08
RU2003122209A (ru) 2005-02-10
ATE326463T1 (de) 2006-06-15
CN100408573C (zh) 2008-08-06
US8697698B2 (en) 2014-04-15
HK1060557A1 (en) 2004-08-13
IL156369A (en) 2011-02-28
IL156369A0 (en) 2004-01-04
KR20030061467A (ko) 2003-07-18
US7087603B2 (en) 2006-08-08
SI1355905T1 (sl) 2007-08-31
HUP0400908A3 (en) 2010-03-29
IL156408A0 (en) 2004-01-04
DE60126828D1 (de) 2007-04-05
JP2008189682A (ja) 2008-08-21
AR042398A1 (es) 2005-06-22
US20030055068A1 (en) 2003-03-20
ATE326461T1 (de) 2006-06-15
EP1702920A1 (en) 2006-09-20
MXPA03005611A (es) 2003-10-06
EP1355905B1 (en) 2007-02-21
MXPA03005609A (es) 2003-10-06
AR040925A1 (es) 2005-04-27
NO20032704L (no) 2003-08-21
CN1486312A (zh) 2004-03-31
DE60126828T2 (de) 2007-11-08
CA2432872A1 (en) 2002-06-27
NO20032670D0 (no) 2003-06-12
US20030004164A1 (en) 2003-01-02
RU2355688C2 (ru) 2009-05-20
NZ526468A (en) 2004-03-26
AU2006201267B2 (en) 2010-07-29
CY1106297T1 (el) 2011-10-12
US20030036543A1 (en) 2003-02-20
CN1486311A (zh) 2004-03-31
IL156368A0 (en) 2004-01-04
US6664247B2 (en) 2003-12-16
EP1345928B1 (en) 2007-02-14
EP1345927A1 (en) 2003-09-24
JP2004519479A (ja) 2004-07-02
HK1062565A1 (zh) 2004-11-12
PL363246A1 (en) 2004-11-15
CA2432129C (en) 2008-08-26
JP2004517927A (ja) 2004-06-17
CA2432223A1 (en) 2002-09-06
HUP0400641A2 (hu) 2004-06-28
MXPA03005605A (es) 2003-10-06
EP1345928A2 (en) 2003-09-24
KR100843114B1 (ko) 2008-07-02
US8304414B2 (en) 2012-11-06
KR20030061463A (ko) 2003-07-18
JP2005097322A (ja) 2005-04-14
CA2432872C (en) 2008-09-23
KR100889246B1 (ko) 2009-03-19
NO20032671L (no) 2003-08-18
CA2432799A1 (en) 2002-06-27
WO2002059112A3 (en) 2003-02-06
PT1345922E (pt) 2006-09-29
CA2432222C (en) 2008-07-29
CN100340555C (zh) 2007-10-03
HK1061389A1 (en) 2004-09-17
HK1060347A1 (en) 2004-08-06
WO2002062789A1 (en) 2002-08-15
WO2002059112A2 (en) 2002-08-01
HUP0400908A2 (hu) 2004-07-28
KR100875091B1 (ko) 2008-12-22
KR20030061857A (ko) 2003-07-22
EP1345927B1 (en) 2006-05-17
HK1059776A1 (en) 2004-07-16
ES2266095T3 (es) 2007-03-01
KR20030061468A (ko) 2003-07-18
ES2280313T3 (es) 2007-09-16
AU2002255452B2 (en) 2006-06-08
NZ526474A (en) 2005-10-28
DE60119776T2 (de) 2007-05-16
US20040214814A1 (en) 2004-10-28
DK1353916T3 (da) 2007-01-29
US20030078275A1 (en) 2003-04-24
US7625913B2 (en) 2009-12-01
KR100909665B1 (ko) 2009-07-29
NO328501B1 (no) 2010-03-01
PT1355905E (pt) 2007-05-31
EP1345929B1 (en) 2006-05-17
MXPA03005610A (es) 2003-10-06
KR100947185B1 (ko) 2010-03-15
IL156389A (en) 2011-01-31
HK1060349A1 (en) 2004-08-06
US6989385B2 (en) 2006-01-24
DE60119776D1 (de) 2006-06-22
AU3116602A (en) 2002-07-01
PL363244A1 (en) 2004-11-15
MXPA03005608A (es) 2003-10-06
TWI290551B (en) 2007-12-01
DE60119774T2 (de) 2007-05-16
KR20030061466A (ko) 2003-07-18
NZ526469A (en) 2005-10-28
ATE528303T1 (de) 2011-10-15
KR20030061465A (ko) 2003-07-18
DK1355905T3 (da) 2007-06-18
EP1345925A2 (en) 2003-09-24
NO330527B1 (no) 2011-05-09
NO20032736D0 (no) 2003-06-16
NO20032703L (no) 2003-08-19
CA2432799C (en) 2008-08-19
EP1702920B1 (en) 2011-10-12
US6656939B2 (en) 2003-12-02
DE60119775D1 (de) 2006-06-22
DE60119775T2 (de) 2007-05-10
US20040157893A1 (en) 2004-08-12
CN100406454C (zh) 2008-07-30
DE60120219T2 (de) 2007-04-12
EP1345922A1 (en) 2003-09-24
MXPA03005606A (es) 2003-10-06
JP4160389B2 (ja) 2008-10-01
AU2001297619B2 (en) 2006-06-08
US20030105090A1 (en) 2003-06-05
US20050038023A1 (en) 2005-02-17
US20090312543A1 (en) 2009-12-17
ATE340172T1 (de) 2006-10-15
CN1486310A (zh) 2004-03-31
EP1345929A2 (en) 2003-09-24
WO2002050065A2 (en) 2002-06-27
JP2013213068A (ja) 2013-10-17
EP2264028A1 (en) 2010-12-22
EP1353916A2 (en) 2003-10-22
ES2272567T3 (es) 2007-05-01
US6653301B2 (en) 2003-11-25
JP2008247921A (ja) 2008-10-16
AU2002231166B2 (en) 2008-02-21
PL210066B1 (pl) 2011-11-30
DE60123283T2 (de) 2007-04-12
ES2265446T3 (es) 2007-02-16
ATE326462T1 (de) 2006-06-15
TWI313269B (en) 2009-08-11
US20140187772A1 (en) 2014-07-03
AU2002234047A1 (en) 2002-07-01
DE60119777D1 (de) 2006-06-22
WO2002057259A2 (en) 2002-07-25
JP2008260767A (ja) 2008-10-30
IL209827A0 (en) 2011-02-28
AP1588A (en) 2006-03-06
JP4210520B2 (ja) 2009-01-21
CA2432223C (en) 2008-05-20
HUP0400641A3 (en) 2010-03-29
WO2002050066A3 (en) 2003-01-23
US7982037B2 (en) 2011-07-19
HK1060346A1 (en) 2004-08-06
AR042397A1 (es) 2005-06-22
DE60119777T2 (de) 2007-05-03
PT1353916E (pt) 2007-01-31
NZ526473A (en) 2005-06-24
CA2432303C (en) 2010-04-13
WO2002059111A3 (en) 2003-01-09
JP2008201808A (ja) 2008-09-04
NZ526470A (en) 2006-03-31
AP2003002816A0 (en) 2003-06-30
AP2003002825A0 (en) 2003-09-30
CA2432129A1 (en) 2002-07-25
BR0116493A (pt) 2003-09-30
NZ526475A (en) 2005-06-24
JP5249842B2 (ja) 2013-07-31
US6653300B2 (en) 2003-11-25
JP2004518743A (ja) 2004-06-24
DK1345922T3 (da) 2006-09-18
DE60123283D1 (de) 2006-11-02
NO20032670L (no) 2003-08-15
US20040167141A1 (en) 2004-08-26
CA2432222A1 (en) 2002-08-15
JP2008247920A (ja) 2008-10-16
WO2002066461A1 (en) 2002-08-29
JP2004517926A (ja) 2004-06-17
EP1353916B1 (en) 2006-09-20
CA2432131A1 (en) 2002-08-01
ATE353890T1 (de) 2007-03-15
EP1355905A1 (en) 2003-10-29
MXPA03005607A (es) 2003-10-06
JP2008189687A (ja) 2008-08-21
WO2002059111A2 (en) 2002-08-01
JP2004518703A (ja) 2004-06-24
EP1345926B1 (en) 2006-05-17
CA2432303A1 (en) 2002-08-29
CA2432132C (en) 2008-07-29
JP2009286805A (ja) 2009-12-10
HUP0400638A2 (hu) 2004-06-28
US20030022885A1 (en) 2003-01-30
JP4234435B2 (ja) 2009-03-04
NZ526471A (en) 2005-08-26
HUP0400842A2 (hu) 2004-07-28
IL156389A0 (en) 2004-01-04
CN102250071A (zh) 2011-11-23
JP4160395B2 (ja) 2008-10-01
WO2002057259A3 (en) 2003-04-24
AR042169A1 (es) 2005-06-15
JP2004517894A (ja) 2004-06-17
WO2002050066A2 (en) 2002-06-27
NO20032671D0 (no) 2003-06-12
DE60120219D1 (de) 2006-07-06
US20030004161A1 (en) 2003-01-02
JP2004516291A (ja) 2004-06-03
JP2009155352A (ja) 2009-07-16
US20130096128A1 (en) 2013-04-18
AU2002246754B2 (en) 2006-06-08
WO2002068415A1 (en) 2002-09-06
ES2265450T3 (es) 2007-02-16
HUP0400639A3 (en) 2010-03-29
DE60126658T2 (de) 2007-11-22
US20080287444A1 (en) 2008-11-20
US20040132781A1 (en) 2004-07-08
JP2008222719A (ja) 2008-09-25
US7531536B2 (en) 2009-05-12
NO328537B1 (no) 2010-03-15
TW200716617A (en) 2007-05-01
EP1345922B1 (en) 2006-05-31
KR20030061464A (ko) 2003-07-18
NO20032736L (no) 2003-08-18
SI1353916T1 (sl) 2007-02-28
NO20032703D0 (no) 2003-06-13
IL156407A0 (en) 2004-01-04
ES2265452T3 (es) 2007-02-16
MY140377A (en) 2009-12-31
DE60119774D1 (de) 2006-06-22
DE60126658D1 (de) 2007-03-29
JP4160392B2 (ja) 2008-10-01
CA2432132A1 (en) 2002-08-01
ATE326460T1 (de) 2006-06-15
US6727251B2 (en) 2004-04-27
ES2375491T3 (es) 2012-03-01
CN100436452C (zh) 2008-11-26
NO20032704D0 (no) 2003-06-13
JP2004516292A (ja) 2004-06-03
ATE354573T1 (de) 2007-03-15
EP1345926A2 (en) 2003-09-24

Similar Documents

Publication Publication Date Title
HUP0400639A2 (hu) Pirazolvegyületek mint proteinkináz inhibitorok és ezeket tartalmazó gyógyszerkészítmények
HUP0302411A2 (hu) Proteinkináz inhibitorként alkalmazható pirazolvegyületek és ezeket tartalmazó gyógyszerkészítmények
KR930017900A (ko) 벤즈이미다졸릴 유도체, 이 화합물을 함유하는 약제학적 조성물 및 이의 제조방법
HUP0402065A2 (hu) Heterobiciklikus szerkezetû hepatitis C vírus polimeráz inhibitorok, eljárás az elõállításukra és ezeket tartalmazó gyógyszerkészítmények
HUP0102851A2 (hu) Parazitaellenes artemizinin-származékok (endoperoxidok), eljárás előállításukra és a vegyületeket tartalmazó gyógyászati készítmények
TW200800938A (en) Indole carboxylic acid derivatives exhibiting PGD2 receptor antagonism
DE69110625D1 (de) Oxazolopyridinderivate, Verfahren zu ihrer Herstellung und die sie enthaltenden pharmazeutischen Zusammensetzungen.
HUP0301272A2 (hu) 4-Fenil-piridin-származékok, mint neurokinin-1-receptor antagonisták, eljárás az előállításukra és alkalmazásuk gyógyszerkészítmények előállítására
HUP0303385A2 (hu) Szerotonin újrafelvételt inhibeáló fenoxibenzilamin-származékok, előállítási eljárásuk, alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények
DK1233953T3 (da) Nye benzoethiadiazinderivater, fremgangsmåde til fremstilling heraf og farmaceutiske sammensætninger indeholdende samme
MXPA04005426A (es) Derivados de pirazol de anillos fuisionados.
ATE173251T1 (de) Kondensierte pyrimidinderivate als antitumorverbindungen
AR021968A1 (es) Oximas e hidrazonas sustituidas como antagonistas de neuroquinina
BRPI0211025B1 (pt) um novo composto para o tratamento da impotência
HUP0001050A2 (hu) Gombaellenes hatású, azolgyűrűt tartalmazó aminosav-észterek, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és intermedierjeik
EA200101204A1 (ru) Новые бициклические соединения аминопиразинона, способ их получения и содержащие их фармацевтические композиции
SE0301371D0 (sv) New Compounds
ATE288899T1 (de) Substituierte alkylaminopyridazinonderivate, verfahren zu ihrer herstellung und diese enthaltende pharmazeutische zubereitungen
HUP0202438A2 (hu) Dioxo-tiazolidin-származékok és ezeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
DE60005609D1 (de) Bizyklische Amino-Pyrazinon-Derivate, verfahren zu deren Herstellung und pharmazeutische Zusammensetzungen die diese enthalten
SI1501823T1 (sl) Novi piperidinil-alkilamino-piridazinonski derivati, postopek za njihovo pripravo in farmacevtski sestavki, ki vsebujejo te spojine
EP1433479B8 (en) Appetite-stimulating agents and remedies for anorexia
GB1193534A (en) Novel Benzazocine Derivatives, the Preparation thereof and Compositions Containing the same
Ram et al. TETRAAZAACENAPHTHENE, TETRAAZAPHENALENE
NZ737408B2 (en) Antibacterial compounds

Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees