[go: up one dir, main page]

EA201891620A1 - Ингибиторы взаимодействующей с рецептором протеинкиназы 1 - Google Patents

Ингибиторы взаимодействующей с рецептором протеинкиназы 1

Info

Publication number
EA201891620A1
EA201891620A1 EA201891620A EA201891620A EA201891620A1 EA 201891620 A1 EA201891620 A1 EA 201891620A1 EA 201891620 A EA201891620 A EA 201891620A EA 201891620 A EA201891620 A EA 201891620A EA 201891620 A1 EA201891620 A1 EA 201891620A1
Authority
EA
Eurasian Patent Office
Prior art keywords
inhibitors
receptor
interactivating
proteinkinase
azepinylcarboxamide
Prior art date
Application number
EA201891620A
Other languages
English (en)
Inventor
Энтони А. Эстрада
Цзяньвэнь А. Фэн
Брайан Фокс
Колин Филип Лесли
Джозеф П. Лиссикатос
Альфонсо Поццан
Закари К. Суини
Хавьер Де Висенте Фидальго
Original Assignee
Денали Терапьютикс Инк.
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 Денали Терапьютикс Инк. filed Critical Денали Терапьютикс Инк.
Publication of EA201891620A1 publication Critical patent/EA201891620A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/12—Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems

Landscapes

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

Abstract

Настоящее изобретение в целом относится к производным N-азепинилкарбоксамида и их композициям, а также к их применению в качестве ингибиторов взаимодействующей с рецептором протеинкиназы 1, которая является ключевым регулятором воспаления, апоптоза и некроптоза.
EA201891620A 2016-02-05 2017-02-03 Ингибиторы взаимодействующей с рецептором протеинкиназы 1 EA201891620A1 (ru)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662292202P 2016-02-05 2016-02-05
US201662341019P 2016-05-24 2016-05-24
US201662363775P 2016-07-18 2016-07-18
US201662385217P 2016-09-08 2016-09-08
US201662417219P 2016-11-03 2016-11-03
PCT/US2017/016509 WO2017136727A2 (en) 2016-02-05 2017-02-03 Compounds, compositions and methods

Publications (1)

Publication Number Publication Date
EA201891620A1 true EA201891620A1 (ru) 2019-02-28

Family

ID=58054535

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891620A EA201891620A1 (ru) 2016-02-05 2017-02-03 Ингибиторы взаимодействующей с рецептором протеинкиназы 1

Country Status (24)

Country Link
US (7) US9815850B2 (ru)
EP (1) EP3414239A2 (ru)
JP (2) JP6974331B2 (ru)
KR (1) KR102808827B1 (ru)
CN (4) CN114437105B (ru)
AU (1) AU2017213628B2 (ru)
CA (1) CA3012832A1 (ru)
CL (1) CL2018002081A1 (ru)
CO (1) CO2018008707A2 (ru)
CR (1) CR20180413A (ru)
DO (1) DOP2018000175A (ru)
EA (1) EA201891620A1 (ru)
EC (1) ECSP18066138A (ru)
IL (2) IL287136B2 (ru)
MA (1) MA44007A (ru)
MX (3) MX2018009448A (ru)
MY (1) MY196648A (ru)
NZ (2) NZ745052A (ru)
PH (1) PH12018501583A1 (ru)
SA (1) SA518392146B1 (ru)
SG (2) SG10201913587WA (ru)
TN (1) TN2018000276A1 (ru)
TW (2) TWI781920B (ru)
WO (1) WO2017136727A2 (ru)

Families Citing this family (88)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI648274B (zh) 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 （二）
MY192762A (en) 2015-07-02 2022-09-07 Hoffmann La Roche Bicyclic lactams and methods of use thereof
SMT202200437T1 (it) 2015-07-22 2023-01-13 Enanta Pharm Inc Derivati benzodiazepinaci come inibitori del rsv
US10961258B2 (en) 2015-12-21 2021-03-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
WO2017123884A1 (en) 2016-01-15 2017-07-20 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as rsv inhibitors
MA44007A (fr) 2016-02-05 2018-12-19 Denali Therapeutics Inc Inhibiteurs du récepteur interagissant avec protéine kinase 1
TWI759301B (zh) 2016-05-24 2022-04-01 美商安美基公司 聚乙二醇化卡非佐米化合物
CN114315819A (zh) * 2016-06-16 2022-04-12 戴纳立制药公司 作为用于治疗神经退化性病症的lrrk2抑制剂的嘧啶-2-基氨基-1h-吡唑
WO2018073193A1 (en) 2016-10-17 2018-04-26 F. Hoffmann-La Roche Ag Bicyclic pyridone lactams and methods of use thereof
TW201831478A (zh) 2016-12-02 2018-09-01 瑞士商赫孚孟拉羅股份公司 雙環醯胺化合物及其使用方法
US11072607B2 (en) * 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
CN110809472B (zh) 2017-02-16 2023-05-23 英安塔制药有限公司 用于制备苯二氮䓬衍生物的方法
JP2020509009A (ja) 2017-02-27 2020-03-26 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ キナーゼ阻害剤としての複素環式アミド
WO2018226801A1 (en) 2017-06-07 2018-12-13 Enanta Pharmaceuticals, Inc. Aryldiazepine derivatives as rsv inhibitors
WO2019006295A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
WO2019006291A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
FI3652178T3 (fi) 2017-07-14 2024-03-19 Hoffmann La Roche Bisyklisiä ketoniyhdisteitä ja niiden käyttömenetelmiä
CN107759574B (zh) * 2017-08-29 2020-07-03 南京药石科技股份有限公司 一种5-氟-1h-吡唑-3-甲酸酯中间体及其合成方法
EP3687543B1 (en) 2017-09-29 2024-03-20 Enanta Pharmaceuticals, Inc. Combinations of pharmaceutical agents as rsv inhibitors
KR20200070297A (ko) * 2017-10-11 2020-06-17 에프. 호프만-라 로슈 아게 Rip1 키나아제 억제제로서 사용하기 위한 이환형 화합물
PE20211247A1 (es) * 2017-10-31 2021-07-13 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de usos de los mismos
WO2019094920A1 (en) * 2017-11-13 2019-05-16 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as rsv inhibitors
BR112020009210A2 (pt) 2017-11-13 2020-10-20 Enanta Pharmaceuticals, Inc. processos para a preparação de compostos derivados de benzodiazepin-2-ona e benzoazepin-2-ona
CN108129288B (zh) * 2017-12-27 2021-01-22 上海毕得医药科技股份有限公司 一种反式-3-羟基环丁基甲酸的合成方法
US10975094B2 (en) 2018-04-11 2021-04-13 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
WO2019204537A1 (en) * 2018-04-20 2019-10-24 Genentech, Inc. N-[4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazol e-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs)
PL3788045T3 (pl) * 2018-05-03 2023-10-09 Rigel Pharmaceuticals, Inc. Związki hamujące rip1 oraz sposoby ich wytwarzania i wykorzystania
JOP20200278A1 (ar) * 2018-05-03 2020-11-03 Rigel Pharmaceuticals Inc مركبات تثبيط rip1 وطرق لتحضير واستخدامها
TW202019913A (zh) * 2018-06-26 2020-06-01 中國科學院上海有機化學研究所 細胞壞死抑制劑及其製備方法和用途
WO2020044206A1 (en) 2018-08-29 2020-03-05 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors for use in the treatment cancer
WO2020054670A1 (ja) * 2018-09-10 2020-03-19 科研製薬株式会社 新規ヘテロ芳香族アミド誘導体及びそれを含有する医薬
JP7045526B2 (ja) * 2018-11-02 2022-03-31 中国科学院上海薬物研究所 Ｒｉｐ１キナーゼを阻害する複素環状アミド及びその使用
CN111138448B (zh) * 2018-11-02 2022-08-02 中国科学院上海药物研究所 抑制rip1激酶的杂环酰胺及其用途
EP3670667A1 (en) * 2018-12-19 2020-06-24 Paris Sciences et Lettres - Quartier Latin Identification of cognate pairs of ligands and receptors
CN113302193A (zh) 2019-01-11 2021-08-24 豪夫迈·罗氏有限公司 双环吡咯并三唑酮化合物及其使用方法
WO2020151589A1 (zh) * 2019-01-25 2020-07-30 北京赛特明强医药科技有限公司 酰胺基桥连杂环类化合物、及其组合物与应用
JP7558189B2 (ja) 2019-03-18 2024-09-30 エナンタ ファーマシューティカルズ インコーポレイテッド Ｒｓｖ阻害剤としてのベンゾジアゼピン誘導体
WO2020210246A1 (en) 2019-04-09 2020-10-15 Enanta Pharmaceuticals, Inc, Heterocyclic compounds as rsv inhibitors
KR102750159B1 (ko) * 2019-05-31 2025-01-07 메드샤인 디스커버리 아이엔씨. Rip-1 키나아제 억제제인 바이사이클릭 화합물 및 이의 응용
CN110172068A (zh) * 2019-06-05 2019-08-27 河南龙湖生物技术有限公司 具有抗肿瘤活性的苯并噻唑类化合物及其制备方法和应用
KR20220044330A (ko) * 2019-08-09 2022-04-07 주식회사 비씨켐 수용체-상호작용 단백질-1 키나아제 저해제로서의 융합된 고리 헤테로아릴 화합물
BR112022002378A2 (pt) 2019-09-06 2022-06-14 Rigel Pharmaceuticals Inc Compostos inibitórios de rip1 e métodos para preparação e uso dos mesmos
WO2021046515A1 (en) 2019-09-06 2021-03-11 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase i for the treatment of disease
TW202122388A (zh) * 2019-09-06 2021-06-16 美商雷傑製藥公司 Ｒｉｐ１抑制性化合物和用於製備和使用其之方法
WO2021050672A1 (en) * 2019-09-11 2021-03-18 Ohio State Innovation Foundation Kinase inhibitors for the treatment of neurodegenerative diseases
JP2022550099A (ja) 2019-09-27 2022-11-30 ボード オブ レジェンツ，ザ ユニバーシティ オブ テキサス システム 疾患の処置のための受容体相互作用プロテインキナーゼｉの阻害剤
CN114761016A (zh) 2019-10-04 2022-07-15 英安塔制药有限公司 抗病毒杂环化合物
US11505558B1 (en) 2019-10-04 2022-11-22 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
KR20250095767A (ko) * 2019-11-07 2025-06-26 리겔 파마슈티칼스, 인크. 헤테로시클릭 rip1 억제 화합물
US11690850B2 (en) 2019-11-26 2023-07-04 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase I for the treatment of disease
UY39032A (es) 2020-01-24 2021-07-30 Enanta Pharm Inc Compuestos heterocíclicos como agentes antivirales
MX2022010693A (es) * 2020-02-28 2022-09-26 Univ Texas Compuestos, composiciones y metodos para inhibidores de la proteina quinasa que interactua con el receptor i para el tratamiento de enfermedades.
AR121717A1 (es) * 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
CA3173330A1 (en) * 2020-04-17 2021-10-21 Genzyme Corporation Eclitasertib for use in treating conditions involving systemichyperinflammatory response
TW202214617A (zh) 2020-06-02 2022-04-16 法商賽諾菲公司 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途
AR122703A1 (es) 2020-07-01 2022-09-28 Rigel Pharmaceuticals Inc Inhibidores de rip1k
US11534439B2 (en) 2020-07-07 2022-12-27 Enanta Pharmaceuticals, Inc. Dihydroquinoxaline and dihydropyridopyrazine derivatives as RSV inhibitors
WO2022086840A1 (en) 2020-10-19 2022-04-28 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as anti-viral agents
US11976084B2 (en) 2020-11-23 2024-05-07 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
CN114716427B (zh) * 2021-01-07 2024-04-26 成都贝诺科成生物科技有限公司 一种作为rip抑制剂的化合物及其制备方法和用途
WO2022171111A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Heteroaryl-fused bicyclic compound as rip1-kinase inhibitors and uses thereof
WO2022171110A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Fused tricyclic compounds as rip1-kinase inhibitors and uses thereof
JP2024507561A (ja) 2021-02-26 2024-02-20 エナンタ ファーマシューティカルズ インコーポレイテッド 抗ウイルス複素環式化合物
TW202300490A (zh) * 2021-03-11 2023-01-01 美商雷傑製藥公司 雜環rip1激酶抑制劑
JP7651929B2 (ja) 2021-04-19 2025-03-27 住友ゴム工業株式会社 ゴム組成物及びタイヤ
WO2022235605A1 (en) 2021-05-04 2022-11-10 Enanta Pharmaceuticals, Inc. Novel macrocyclic antiviral agents
CN114989156B (zh) * 2021-05-19 2024-07-05 成都贝诺科成生物科技有限公司 一种受体相互作用蛋白抑制剂及其制备方法和用途
TW202321211A (zh) 2021-08-10 2023-06-01 美商艾伯維有限公司 菸鹼醯胺ripk1抑制劑
EP4402139A1 (en) * 2021-09-17 2024-07-24 Bisichem Co., Ltd. Fused heterocyclic rings as ripk1 inhibitors
US11897876B2 (en) 2021-11-11 2024-02-13 Genzyme Corporation Isoxazolidines as RIPK1 inhibitors and use thereof
WO2023086400A1 (en) 2021-11-12 2023-05-19 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
US11858945B2 (en) 2021-11-12 2024-01-02 Enanta Pharmaceuticals, Inc. Alkyne-containing antiviral agents
WO2023086352A1 (en) 2021-11-12 2023-05-19 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
WO2023107419A1 (en) 2021-12-08 2023-06-15 Enanta Pharmaceuticals, Inc. Saturated spirocyclics as antiviral agents
WO2023119210A1 (ko) 2021-12-24 2023-06-29 제일약품주식회사 Ripk1 저해제로서의 신규한 화합물 및 이를 포함하는 약학적 조성물
EP4209213A1 (en) 2022-01-05 2023-07-12 Universität zu Köln Signalling-pathway inhibitor combinations for use in the treatment of cancer diseases
WO2023137007A1 (en) * 2022-01-11 2023-07-20 Enanta Pharmaceuticals, Inc. Processes for the preparation of 4,6,7-trifluoro-1h-indole-2-carboxylic acid
AU2023206890A1 (en) 2022-01-12 2024-08-22 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide
CN116640156A (zh) * 2022-02-22 2023-08-25 上海齐鲁制药研究中心有限公司 Ripk1抑制剂
CN118647617A (zh) 2022-03-16 2024-09-13 江苏恒瑞医药股份有限公司 稠杂环类化合物、其制备方法及其在医药上的应用
US12145942B2 (en) 2022-04-05 2024-11-19 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
AR129003A1 (es) 2022-04-07 2024-07-03 Enanta Pharm Inc Compuestos heterocíclicos antivirales
WO2023211997A1 (en) 2022-04-27 2023-11-02 Enanta Pharmaceuticals, Inc. Antiviral compounds
WO2024170776A1 (en) 2023-02-17 2024-08-22 Universität Zu Köln Triple kinase inhibition for the treatment of type i interferon response associated disorders
WO2025037940A1 (en) * 2023-08-16 2025-02-20 Bisichem Co., Ltd. Pyrazole-1-carboxamides as rip1 kinase inhibitors
CN119528914A (zh) * 2023-08-31 2025-02-28 杭州百诚医药科技股份有限公司 苯并氮杂䓬酮类衍生物及其用途
CN118084889B (zh) * 2024-01-16 2024-09-27 宁夏医科大学 吲哚3-芳基-5-甲酰胺类衍生物及用途
CN117849327A (zh) * 2024-03-06 2024-04-09 军科正源（北京）药物研究有限责任公司 用于检测苏金单抗抗药性抗体的方法

Family Cites Families (170)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US4477464A (en) 1983-02-10 1984-10-16 Ciba-Geigy Corporation Hetero-benzazepine derivatives and their pharmaceutical use
EP0187037A3 (en) 1984-12-21 1988-03-23 Takeda Chemical Industries, Ltd. Piperidine derivatives, their production and use
EP0322779A3 (en) 1987-12-29 1991-05-08 Yoshitomi Pharmaceutical Industries, Ltd. Benzolactam compounds and pharmaceutical uses thereof
JPH0334977A (ja) 1989-06-29 1991-02-14 Yoshitomi Pharmaceut Ind Ltd イミダゾリルベンゾラクタム化合物
IE912064A1 (en) 1990-06-18 1991-12-18 Merck & Co Inc Inhibitors of hiv reverse transcriptase
EP0481614A1 (en) 1990-10-01 1992-04-22 Merck & Co. Inc. Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
US5206235A (en) 1991-03-20 1993-04-27 Merck & Co., Inc. Benzo-fused lactams that promote the release of growth hormone
US5457196A (en) 1991-09-27 1995-10-10 Merrell Dow Pharmaceuticals Inc. 2-substituted indane-2-carboxyalkyl derivatives useful as inhibitors of enkephalinase and ACE
CA2078758C (en) 1991-09-27 2003-12-09 Alan M. Warshawsky 2-substituted indane-2-mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace
JP3358069B2 (ja) 1991-12-24 2002-12-16 武田薬品工業株式会社 三環性複素環類、その製造法及び剤
US5484917A (en) 1993-06-16 1996-01-16 Pfizer Inc. Substituted tetrahydrobenzazepinones
AU4282993A (en) 1992-07-01 1994-01-31 Pfizer Inc. Benzothiazepine and benzoxazepine derivatives as cholecystokinin receptor antagonists
AU679452B2 (en) 1992-08-24 1997-07-03 Merrell Dow Pharmaceuticals Inc. Novel 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase
US5420271A (en) 1992-08-24 1995-05-30 Merrell Dow Pharmaceuticals, Inc. 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase
US5283241A (en) 1992-08-28 1994-02-01 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
JPH07501085A (ja) 1992-09-03 1995-02-02 ベーリンガー　インゲルハイム　コマンディトゲゼルシャフト 新規なアミノ酸誘導体、その製造方法及びこれらの化合物を含む医薬組成物
US5583130A (en) 1992-09-25 1996-12-10 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5317017A (en) 1992-09-30 1994-05-31 Merck & Co., Inc. N-biphenyl-3-amido substituted benzolactams stimulate growth hormone release
US5374721A (en) 1992-10-14 1994-12-20 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
DE69332946T2 (de) 1992-10-16 2004-05-19 Suprex Corp. Automatisierte extrakion mittels eines superkritischen fluidum
GB2272439A (en) 1992-11-13 1994-05-18 Merck & Co Inc Benzo-fused lactams that inhibit the release of growth hormone
US5284841A (en) 1993-02-04 1994-02-08 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
GB9307833D0 (en) 1993-04-15 1993-06-02 Glaxo Inc Modulators of cholecystokinin and gastrin
WO1994026718A1 (en) 1993-05-13 1994-11-24 Yoshitomi Pharmaceutical Industries, Ltd. 3-aminoazepine compound and pharmaceutical use thereof
US5430144A (en) 1993-07-26 1995-07-04 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
ES2081747B1 (es) 1993-09-07 1997-01-16 Esteve Labor Dr Amidas derivadas de tienopirroles, su preparacion y su aplicacion como medicamentos.
US5606054A (en) 1993-12-14 1997-02-25 Merck & Co., Inc. Heterocyclic-fused lactams promote release of growth hormone
DE69510545T2 (de) 1994-04-14 2000-01-13 Glaxo Wellcome Inc Cck oder gastrin modulierende 5-heterocyclicyl-1,5-benzodiazepine
MX9605128A (es) 1994-05-07 1997-08-30 Boehringer Ingelheim Kg Nuevos derivados de aminoacidos, procedimientos para su preparacion y composiciones farmaceuticas que contienen estos compuestos.
IL114955A (en) 1994-08-17 1999-12-22 Novo Nordisk As N-substituted naphthofused lactams and pharmaceutical compositions containing them
GB9420747D0 (en) 1994-10-14 1994-11-30 Glaxo Inc 1,5 benzodiazepine derivatives
GB9420748D0 (en) 1994-10-14 1994-11-30 Glaxo Inc 1,5 benzodiazepine derivatives
GB9420763D0 (en) 1994-10-14 1994-11-30 Glaxo Inc Acetamide derivatives
CA2205463A1 (en) 1994-11-17 1996-05-30 Ciba Specialty Chemicals Holding Inc. Monomers and composition which can be crosslinked and crosslinked polymers
US5587375A (en) 1995-02-17 1996-12-24 Bristol-Myers Squibb Company Azepinone compounds useful in the inhibition of ACE and NEP
US5726171A (en) 1995-06-07 1998-03-10 Merck & Co Inc N-(1-alkyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo B! 1,4!diazepin-3yl)-acetamides
US5700797A (en) 1995-06-07 1997-12-23 Merck & Co, Inc. N-(2,4-dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3-yl)-3-amides
US5691331A (en) 1995-06-07 1997-11-25 Merck & Co., Inc. N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides
ES2193241T3 (es) 1995-06-07 2003-11-01 Merck & Co Inc Nuevas n-2-oxo2.3.4.5-tetrajodrp-1h-1,5-benzodiazepin-3-il)-3-amidas.
EP0761680A3 (en) 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
JP3335362B2 (ja) 1995-09-15 2002-10-15 サノフィ―サンテラボ キノレイン−２（１ｈ）−オン誘導体セロトニンアンタゴニスト
WO1997024339A1 (fr) 1995-12-27 1997-07-10 Ono Pharmaceutical Co., Ltd. Derives de tetrazole et medicaments les contenant a titre d'ingredients actifs
US5747235A (en) 1996-01-26 1998-05-05 Eastman Kodak Company Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
JPH09295996A (ja) 1996-03-06 1997-11-18 Takeda Chem Ind Ltd システインプロテアーゼ阻害化合物
US6028195A (en) 1996-06-29 2000-02-22 Samjin Pharmaceutical Co., Ltd. Piperazine derivatives and process for the preparation thereof
DE19638020A1 (de) 1996-09-18 1998-03-19 Solvay Pharm Gmbh Die gastrointestinale Durchblutung fördernde Arzneimittel
AU7624798A (en) 1996-12-06 1998-06-29 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1 beta converting enzyme
JPH10251295A (ja) 1997-03-07 1998-09-22 Ono Pharmaceut Co Ltd テトラゾール誘導体
JP2001515842A (ja) 1997-08-11 2001-09-25 シーオーアール セラピューティクス インコーポレイテッド 選択的Ｘａ因子阻害剤
US6211174B1 (en) 1997-10-31 2001-04-03 Merck & Co., Inc. Naphtho-fused lactams promote release of growth hormone
FR2781483A1 (fr) 1998-07-21 2000-01-28 Hoechst Marion Roussel Inc Derives de thioazepinone, procede de preparation et intermediaires de ce procede, application a titre de medicament et compositions pharmaceutiques les renfermant
DE19858253A1 (de) 1998-12-17 2000-06-21 Aventis Pharma Gmbh Verwendung von Inhibitoren des KQt1-Kanals zur Herstellung eines Medikaments zur Behandlung von Krankheiten, die durch Helminthen und Ektoparasiten hervorgerufen werden
JP2000256318A (ja) 1999-03-02 2000-09-19 Toa Eiyo Ltd 縮合複素環誘導体、その製造法およびそれを含有する医薬品
FR2803594B1 (fr) 2000-01-11 2002-07-19 Centre Nat Rech Scient Oligomeres de mimes contraints non peptidiques de dipeptides ou de tripeptides, et leurs utilisations
US6759404B2 (en) 2000-04-03 2004-07-06 Richard E. Olson Cyclic malonamides as inhibitors of aβ protein production
MXPA02009729A (es) 2000-04-03 2003-03-27 Bristol Myers Squibb Pharma Co Lactamas ciclicas como inhibidores de la produccion de la proteina a-beta.
AU2001255408A1 (en) 2000-04-14 2001-10-30 Corvas International, Inc. Tetrahydro-azepinone derivatives as thrombin inhibitors
RU2002135317A (ru) 2000-04-24 2004-04-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Способ и промежуточные соединения для получения замещенных ацеталей аспарагиновой кислоты
GB0012671D0 (en) 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
CA2379445C (en) 2000-06-01 2007-08-21 Bristol-Myers Squibb Pharma Company Lactams substituted by cyclic succinates as inhibitors of a.beta. protein production
AUPQ969800A0 (en) 2000-08-28 2000-09-21 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyridine compound and pharmaceutical use thereof
AU2001288432A1 (en) 2000-09-01 2002-03-22 Icos Corporation Materials and methods to potentiate cancer treatment
GB0021831D0 (en) * 2000-09-06 2000-10-18 Astrazeneca Ab Chemical compounds
WO2003007945A1 (en) 2001-07-20 2003-01-30 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
EP2335700A1 (en) 2001-07-25 2011-06-22 Boehringer Ingelheim (Canada) Ltd. Hepatitis C virus polymerase inhibitors with a heterobicylic structure
US7294457B2 (en) 2001-08-07 2007-11-13 Boehringer Ingelheim (Canada) Ltd. Direct binding assay for identifying inhibitors of HCV polymerase
WO2003031376A1 (en) 2001-10-12 2003-04-17 Aventis Pharmaceuticals Inc. Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
BR0312204A (pt) 2002-06-27 2005-04-26 Schering Ag Antagonista de receptor ccr5 de quinolina substituìda
US7098235B2 (en) 2002-11-14 2006-08-29 Bristol-Myers Squibb Co. Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds
US7208487B2 (en) 2002-12-13 2007-04-24 Cytokinetics, Incorporated Compounds, compositions and methods
CA2518830A1 (en) 2003-03-14 2004-09-30 Merck & Co., Inc. Carboxamide spirohydantoin cgrp receptor antagonists
DE602004016992D1 (de) 2003-05-02 2008-11-20 Elan Pharm Inc 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazol-3-carbonsäureamid-derivate und verwandte verbindungen als bradykinin b1 rezeptor antagonisten zur behandlung von entzündlichen erkrankungen
JP2005035933A (ja) 2003-07-15 2005-02-10 Takeda Chem Ind Ltd 含窒素縮合複素環化合物の製造方法
ES2567135T3 (es) 2003-08-29 2016-04-20 The Brigham And Women's Hospital, Inc. Derivados de hidantoína como inhibidores de necrosis celular
JP2007532474A (ja) 2003-10-10 2007-11-15 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 セリンプロテアーゼ、特にｈｃｖのｎｓ３−ｎｓ４ａプロテアーゼの阻害剤
US20050256056A1 (en) 2003-12-05 2005-11-17 The Regents Of The University Of California Office Of Technology Transfer University Of California Peptide inhibitors of HIV
US20070010428A1 (en) 2004-09-03 2007-01-11 Mcmurray John S Inhibitors of signal transduction and activator of transcription 3
US7390798B2 (en) 2004-09-13 2008-06-24 Merck & Co., Inc. Carboxamide spirolactam CGRP receptor antagonists
JP4913061B2 (ja) * 2004-10-13 2012-04-11 メルク・シャープ・エンド・ドーム・コーポレイション Ｃｇｒｐ受容体拮抗薬
ATE507880T1 (de) * 2004-10-14 2011-05-15 Merck Sharp & Dohme Cgrp-rezeptorantagonisten
EP1819332B1 (en) 2004-12-02 2009-03-11 Prosidion Limited Pyrrolopyridine-2-carboxylic acid amides
US7875627B2 (en) 2004-12-07 2011-01-25 Abbott Laboratories Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof
WO2006071775A2 (en) 2004-12-29 2006-07-06 Elan Pharmaceuticals, Inc. Novel compounds useful for bradykinin b1 receptor antagonism
WO2006079077A2 (en) 2005-01-20 2006-07-27 Acadia Pharmaceuticals Inc. Use of diltiazem or analogs thereof as modulators of ghrelin receptor
WO2006105222A2 (en) 2005-03-25 2006-10-05 Scios Inc. Carboxamide inhibitors of tgfb
EA200701856A1 (ru) 2005-04-01 2008-02-28 Уорнер-Ламберт Компани Ллс Тетрагидропиридоазепин-8-оны и родственные соединения для лечения шизофрении
WO2006113432A2 (en) 2005-04-14 2006-10-26 Smithkline Beecham Corporation Compounds, compositions and methods
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
EA014244B1 (ru) 2005-09-23 2010-10-29 Коли Фармасьютикал Груп, Инк. СПОСОБ ПОЛУЧЕНИЯ 1-Н-ИМИДАЗО[4,5-c]ПИРИДИНОВ И ИХ АНАЛОГОВ
US20090156578A1 (en) 2005-12-05 2009-06-18 PAULS Henry 3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
US8324262B2 (en) 2005-12-20 2012-12-04 The Brigham And Women's Hospital, Inc. Tricyclic necrostatin compounds
GB0605689D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic compounds
WO2007126871A1 (en) 2006-03-29 2007-11-08 Array Biopharma Inc. P38 inhibitors and methods of use thereof
JP2009543762A (ja) 2006-06-09 2009-12-10 メルク エンド カムパニー インコーポレーテッド ナトリウムチャネル遮断薬としてのベンゾアゼピノン
EP2054422B1 (en) 2006-07-20 2017-06-14 Debiopharm International SA Acrylamide derivatives as fab i inhibitors
WO2008011190A1 (en) 2006-07-21 2008-01-24 Vertex Pharmaceuticals Incorporated Cgrp receptor antagonists
US9987277B2 (en) 2006-10-04 2018-06-05 Janssen Sciences Ireland Uc Carboxamide 4-[(4-pyridyl)amino] pryimidines for the treatment of hepatitis C
ES2430821T3 (es) 2006-10-10 2013-11-21 Amgen Inc. Compuestos de N-arilpirazol para usar contra la diabetes
EP1939187A1 (en) * 2006-12-20 2008-07-02 Sanofi-Aventis Substituted heteroaryl pyridopyrimidone derivatives
US9562019B2 (en) 2006-12-21 2017-02-07 Sloan-Kettering Institute For Cancer Research Substituted pyridazines as EGFR and/or KRAS inhibitors
AU2008219723A1 (en) 2007-02-28 2008-09-04 Merck Sharp & Dohme Corp. Substituted benzodiazepinones, benzoxazepinones and benzothiazepinones as sodium channel blockers
WO2008135525A2 (en) 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted azetidines, manufacturing and use thereof as medicaments
US8242150B2 (en) 2007-06-13 2012-08-14 Merck Sharp & Dohme Corp. Triazole derivatives for treating alzheimer'S disease and related conditions
CN101772577A (zh) 2007-08-03 2010-07-07 塞诺菲-安万特股份有限公司 半胱天冬蛋白酶成像探针
WO2009085256A1 (en) 2007-12-27 2009-07-09 Panacos Pharmaceuticals, Inc. Anti-hiv compounds
EP2085399A1 (en) * 2008-01-29 2009-08-05 Sanofi-Aventis substituted arylamide oxazepinopyrimidone derivatives
EP2090578A1 (en) * 2008-01-29 2009-08-19 Sanofi-Aventis Substituted arylamide diazepinopyrimidone derivatives for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3-beta
JP4708443B2 (ja) 2008-01-31 2011-06-22 トヨタ自動車株式会社 作動制御マップおよび白線認識装置
AU2009215731A1 (en) 2008-02-19 2009-08-27 Merck Sharp & Dohme Corp. Imidazobenzazepine CGRP receptor antagonists
WO2009103432A2 (en) 2008-02-21 2009-08-27 Sanofi-Aventis Covalently binding imaging probes
WO2009140549A1 (en) 2008-05-14 2009-11-19 Amgen Inc. Combinations vegf(r) inhibitors and hepatocyte growth factor (c-met) inhibitors for the treatment of cancer
US7884074B2 (en) 2008-05-15 2011-02-08 Ikaria Development Subsidiary Two, LLC Compounds and methods for prevention and/or treatment of inflammation using the same
WO2010013794A1 (en) 2008-07-28 2010-02-04 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
DE102008037790A1 (de) 2008-08-14 2010-02-18 Merck Patent Gmbh Bicyclische Triazolderivate
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
US8088890B2 (en) 2008-09-26 2012-01-03 Fibrex Medical Research & Development Gmbh Peptides and peptidomimetic compounds, the manufacturing thereof as well as their use for preparing a therapeutically and/or preventively active pharmaceutical composition
RU2011119478A (ru) 2008-10-14 2012-11-27 Нин Си Соединения и способы применения
US20110306626A1 (en) 2008-12-17 2011-12-15 Selnick Harold G Imidazolinone derivatives as cgrp receptor antagonists
WO2010083725A1 (zh) 2009-01-20 2010-07-29 山东轩竹医药科技有限公司 含有取代的含氮稠杂环的头孢菌素衍生物
US8624063B2 (en) 2009-06-30 2014-01-07 Wisconsin Alumni Research Foundation Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing
EP2477493A1 (en) 2009-09-16 2012-07-25 Cylene Pharmaceuticals, Inc. Novel tricyclic protein kinase modulators
ES2574927T3 (es) 2009-10-29 2016-06-23 Glaxosmithkline Llc Piridinas bicíclicas y análogos como moduladores de sirtuina
US8481541B2 (en) 2010-03-22 2013-07-09 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
AU2011242465B2 (en) 2010-04-23 2017-01-19 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
US20130165446A1 (en) 2010-05-11 2013-06-27 Takashi Fujita Benzo-or pyrido-imidazole derivative
MX2012013560A (es) 2010-05-24 2013-03-05 Univ Vanderbilt 6-metilnicotinamidas sustituidas como moduladores alostéricos positivos de mglur5.
US9029501B2 (en) 2010-11-02 2015-05-12 Rigel Pharmaceuticals, Inc. Method for making macrocycles
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
TWI478908B (zh) 2011-07-01 2015-04-01 Gilead Sciences Inc 作為離子通道調節劑之稠合雜環化合物
WO2013012918A1 (en) 2011-07-19 2013-01-24 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
AR087107A1 (es) 2011-07-27 2014-02-12 Lilly Co Eli Compuesto inhibidor de la señalizacion de la trayectoria notch
WO2013013826A1 (en) 2011-07-27 2013-01-31 Friedrich-Alexander-Universität Erlangen-Nürnberg Necroptosis inhibitors for the treatment of inflammatory diseases of the gastrointestinal tract
US20140357570A1 (en) 2011-10-21 2014-12-04 Massachusetts Eye And Ear Infirmary Compositions comprising necrosis inhibitors, such as necrostatins, alone or in combination, for promoting axon regeneration and nerve function, thereby treating cns disorders
MY165902A (en) 2011-12-02 2018-05-18 Aurigene Discovery Tech Ltd Substituted pyridine derivatives as fabi inhibitors
US9062075B2 (en) 2011-12-02 2015-06-23 Aurigene Discovery Technologies Limited Tetrahydropyridine derivatives as FabI inhibitors
JP2015518504A (ja) 2012-04-03 2015-07-02 スリーエム イノベイティブ プロパティズ カンパニー 光塩基発生剤を含む架橋性組成物
WO2013189241A1 (zh) 2012-06-20 2013-12-27 上海恒瑞医药有限公司 嘧啶二胺类衍生物、其制备方法及其在医药上的应用
TWI520962B (zh) 2012-06-29 2016-02-11 As the c-Met tyrosine kinase inhibitors novel fused pyridine derivatives
KR101704307B1 (ko) 2012-07-13 2017-02-07 에프. 호프만-라 로슈 아게 항증식성 벤조[b]아제핀-2-온
CN104470905B (zh) 2012-08-09 2017-09-12 霍夫曼-拉罗奇有限公司 取代的杂‑氮杂*酮化合物
CN103664904A (zh) 2012-09-07 2014-03-26 李振 一种γ-分泌酶抑制剂及其用途
WO2014072930A2 (en) 2012-11-09 2014-05-15 Aurigene Discovery Technologies Limited Fused pyridine derivatives as antibacterial agents
TWI648274B (zh) 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 （二）
WO2014144547A2 (en) 2013-03-15 2014-09-18 The Regents Of The University Of California Amide derivatives of lactam based n-acylethanolamine acid amidase (naaa) inhibitors
FR3003860B1 (fr) 2013-03-29 2015-11-27 Oreal Composes derives d'iridoides proteges ou non, composition les comprenant, utilisation comme colorant des fibres keratiniques et dispositifs
US20160051629A1 (en) 2013-04-15 2016-02-25 Yeda Research And Development Co. Ltd. Inhibition of rip kinases for treating lysosomal storage diseases
WO2015027137A1 (en) 2013-08-23 2015-02-26 University Of Tennessee Research Foundation Improved synthesis of capuramycin and its analogues
US20160326157A1 (en) 2014-01-06 2016-11-10 President And Fellows Of Harvard College Monobactams and methods of their synthesis and use
WO2015104677A1 (en) 2014-01-10 2015-07-16 Piramal Enterprises Limited Heterocyclic compounds as ezh2 inhibitors
WO2015184257A2 (en) 2014-05-30 2015-12-03 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
US9616047B2 (en) 2014-06-30 2017-04-11 Regents Of University Of Minnesota Inhibitors of beta-catenin in treatment of colorectal cancer
US20170226514A1 (en) 2014-08-13 2017-08-10 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Prevention of tumour metastasis by inhibition of necroptosis
US20170266199A1 (en) 2014-08-21 2017-09-21 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as rip1 kinase inhibitors as medicaments
CN107108512B (zh) 2014-10-10 2021-05-04 基因泰克公司 治疗性化合物及其用途
EP3017825A1 (en) 2014-11-06 2016-05-11 Ludwig-Maximilians-Universität München An inhibitor of the RIPK1-dependent necrosis pathway and a pharmaceutical composition comprising the same
WO2016101885A1 (en) 2014-12-24 2016-06-30 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
AU2015371824B2 (en) 2014-12-24 2019-09-19 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
EP3245198B1 (en) 2015-01-13 2020-03-11 Novartis AG Pyrrolidine derivatives as angiotensin ii type 2 antagonists
CN107207485A (zh) 2015-02-13 2017-09-26 葛兰素史密斯克莱知识产权发展有限公司 (S)‑5‑苄基‑N‑(5‑甲基‑4‑氧代‑2,3,4,5‑四氢苯并[b][1,4]氧氮杂环庚三烯‑3‑基)‑4H‑1,2,4‑三唑‑3‑甲酰胺的晶型
TWI609687B (zh) 2015-04-14 2018-01-01 美國禮來大藥廠 平滑肌肉瘤之標靶性治療
MY192762A (en) * 2015-07-02 2022-09-07 Hoffmann La Roche Bicyclic lactams and methods of use thereof
KR101858346B1 (ko) 2015-07-07 2018-05-16 가톨릭대학교 산학협력단 Ripk 억제제를 유효성분으로 포함하는 면역질환의 예방 또는 치료용 조성물
EP3366684B1 (en) 2015-10-23 2020-09-02 Takeda Pharmaceutical Company Limited Heterocyclic compound
US10961258B2 (en) 2015-12-21 2021-03-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
MA44007A (fr) 2016-02-05 2018-12-19 Denali Therapeutics Inc Inhibiteurs du récepteur interagissant avec protéine kinase 1
CN107043377A (zh) 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 一种tlr7激动剂的三氟乙酸盐、晶型b及其制备方法、药物组合物和用途
CN107043378A (zh) 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 一种吡咯并[3,2-d]嘧啶类化合物的制备方法及其中间体

Also Published As

Publication number Publication date
JP2022017447A (ja) 2022-01-25
TW202330479A (zh) 2023-08-01
KR102808827B1 (ko) 2025-05-19
JP6974331B2 (ja) 2021-12-01
TWI781920B (zh) 2022-11-01
MA44007A (fr) 2018-12-19
AU2017213628B2 (en) 2021-07-29
US20180022759A1 (en) 2018-01-25
KR20180114910A (ko) 2018-10-19
JP7381543B2 (ja) 2023-11-15
SG10201913587WA (en) 2020-02-27
CL2018002081A1 (es) 2018-12-14
IL287136A (en) 2021-12-01
ECSP18066138A (es) 2018-09-30
US9815850B2 (en) 2017-11-14
CN109071504B (zh) 2022-03-08
MY196648A (en) 2023-04-27
IL287136B2 (en) 2023-09-01
US20180099981A1 (en) 2018-04-12
CN109071504A (zh) 2018-12-21
WO2017136727A3 (en) 2017-09-08
CN118994191A (zh) 2024-11-22
MX2021013226A (es) 2022-01-06
NZ784787A (en) 2025-02-28
IL260674B (en) 2021-10-31
US10604535B2 (en) 2020-03-31
WO2017136727A2 (en) 2017-08-10
CA3012832A1 (en) 2017-08-10
PH12018501583A1 (en) 2019-04-08
EP3414239A2 (en) 2018-12-19
US12358928B2 (en) 2025-07-15
CN114437105A (zh) 2022-05-06
US20170226127A1 (en) 2017-08-10
TWI836679B (zh) 2024-03-21
CO2018008707A2 (es) 2018-08-31
DOP2018000175A (es) 2018-10-15
TN2018000276A1 (en) 2020-01-16
TW201730160A (zh) 2017-09-01
BR112018015410A2 (pt) 2018-12-18
JP2019508407A (ja) 2019-03-28
MX2018009448A (es) 2018-11-21
MX2021013228A (es) 2022-01-18
SA518392146B1 (ar) 2023-02-12
AU2017213628A1 (en) 2018-08-23
SG11201806302RA (en) 2018-08-30
US20230043400A1 (en) 2023-02-09
US9896458B2 (en) 2018-02-20
US20200317691A1 (en) 2020-10-08
CN114437105B (zh) 2024-10-11
US20240150376A1 (en) 2024-05-09
US10131676B2 (en) 2018-11-20
IL287136B1 (en) 2023-05-01
CR20180413A (es) 2018-12-04
NZ745052A (en) 2025-02-28
CN118994190A (zh) 2024-11-22
US20190112318A1 (en) 2019-04-18

Similar Documents

Publication Publication Date Title
EA201891620A1 (ru) Ингибиторы взаимодействующей с рецептором протеинкиназы 1
EA201891910A1 (ru) Гетероарильные ингибиторы pad4
EA201890308A1 (ru) Замещенные азасоединения как ингибиторы irak-4
EA201891024A1 (ru) Соединения-ингибиторы tank-связывающей киназы
EA201890093A1 (ru) Комбинированная терапия гемобластозов антителами к cd38 и ингибиторами сурвивина
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
CR20190566A (es) Inhibidores de quinasay usos de los mismos
EA201890307A1 (ru) Индазольные и азаиндазольные соединения как ингибиторы irak-4
MX2018002986A (es) Compuestos de heteroarilo como inhibidores de cinasas asociadas al receptor de interleucina 1 (irak) y sus usos.
MX2017006266A (es) Compuestos de heteroarilo como inhibidores de cinasas asociadas al receptor de interleucina 1(irak) y sus usos.
EA201790649A1 (ru) Бензилзамещенные индазолы в качестве ингибиторов bub 1
EA201691259A1 (ru) РЕГУЛЯТОРЫ Nrf2
CY1123263T1 (el) Πολυκυκλικες ενωσεις ως αναστολεις κινασης τυροσινης bruton
EA201792021A1 (ru) Ингибитор jak
JO3793B1 (ar) مثبطات تيروزين كاينيز بروتون وأساليب استخدامها
EA201692526A1 (ru) Замещенные [1,2,4]триазольные соединения
MX381487B (es) Ciertos inhibidores de la proteina quinasa.
EA201790785A1 (ru) Производные тетрагидроизохинолина
EA201892430A1 (ru) Синтез индазолов
EA201891347A1 (ru) Аза-бензимидазольные ингибиторы pad4
EA201690844A1 (ru) Ингибиторы gsk-3
EA202090183A1 (ru) Композиции, способы и получение дейтерированного домперидона
EA201692525A1 (ru) Замещенные соединения [1,2,4]триазола и имидазола в качестве фунгицидов
EA201992147A1 (ru) Ингибиторы тирозинкиназы брутона