[go: up one dir, main page]

BR112013020329A2 - compostos heterocíclicos como inibidores da pi3-quinase - Google Patents

compostos heterocíclicos como inibidores da pi3-quinase

Info

Publication number
BR112013020329A2
BR112013020329A2 BR112013020329A BR112013020329A BR112013020329A2 BR 112013020329 A2 BR112013020329 A2 BR 112013020329A2 BR 112013020329 A BR112013020329 A BR 112013020329A BR 112013020329 A BR112013020329 A BR 112013020329A BR 112013020329 A2 BR112013020329 A2 BR 112013020329A2
Authority
BR
Brazil
Prior art keywords
compounds
kinase inhibitors
heterocyclic compounds
formula
treatment
Prior art date
Application number
BR112013020329A
Other languages
English (en)
Inventor
Bohdan Waszkowycz
Brian Safina
Daniel P Sutherlin
Eileen M Seward
Pascal Pierre Alexandre Savy
Robert Heald
Stephen Price
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of BR112013020329A2 publication Critical patent/BR112013020329A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P1/04—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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/40—Heterocyclic compounds containing purine ring systems with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
    • 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
    • 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
    • C07D498/06—Peri-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Obesity (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

compostos heterocíclicos como inibidores da pi3-quinase os compostos de fórmula i, incluindo os estereoisômeros, isômeros geométricos, tautômeros, metabólicos, e sais farmaceuticamente aceitáveis destes, são úteis para a inibição da isoforma delta pi3k, e para o tratamento de doenças mediadas por quinases de lipídeos, tais como inflamação, distúrbios imunológicos, e câncer. os métodos de utilização de compostos de fórmula i para diagnóstico, prevenção, ou tratamento in vitro, in situ e in vivo, dos respectivos distúrbios em células de mamíferos, ou condições patológicas associadas, são revelados.
BR112013020329A 2011-02-09 2012-02-08 compostos heterocíclicos como inibidores da pi3-quinase BR112013020329A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161441014P 2011-02-09 2011-02-09
PCT/EP2012/052090 WO2012107465A1 (en) 2011-02-09 2012-02-08 Heterocyclic compounds as pi3 kinase inhibitors

Publications (1)

Publication Number Publication Date
BR112013020329A2 true BR112013020329A2 (pt) 2016-08-02

Family

ID=45688453

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013020329A BR112013020329A2 (pt) 2011-02-09 2012-02-08 compostos heterocíclicos como inibidores da pi3-quinase

Country Status (10)

Country Link
US (1) US8653089B2 (pt)
EP (1) EP2673269A1 (pt)
JP (1) JP5766820B2 (pt)
KR (1) KR20130116358A (pt)
CN (1) CN103476767B (pt)
BR (1) BR112013020329A2 (pt)
CA (1) CA2825028A1 (pt)
MX (1) MX2013008822A (pt)
RU (1) RU2013138835A (pt)
WO (1) WO2012107465A1 (pt)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112013014914B8 (pt) 2010-12-16 2020-08-04 Hoffmann La Roche composto, composição farmacêutica e uso de um composto
WO2013090725A1 (en) * 2011-12-15 2013-06-20 Philadelphia Health & Education Corporation NOVEL PI3K p110 INHIBITORS AND METHODS OF USE THEREOF
WO2013130461A1 (en) * 2012-02-29 2013-09-06 The Scripps Research Institute Wee1 degradation inhibitors
GB201220157D0 (en) * 2012-11-08 2012-12-26 Selvita Sa Substitute tricyclic benzimidazoles as kinase inhibitors
JP6434416B2 (ja) 2012-11-08 2018-12-05 ライゼン・ファーマシューティカルズ・エスアー ＰＤＥ４阻害剤とＰＩ３δ阻害剤または二重ＰＩ３δ−γキナーゼ阻害剤とを含有する薬学的組成物
KR20150087850A (ko) 2012-11-20 2015-07-30 제넨테크, 인크. Egfr 돌연변이체를 함유하는 t790m의 억제제로서의 아미노피리미딘 화합물
AU2013364070B2 (en) 2012-12-21 2016-10-27 Gilead Calistoga Llc Isoquinolinone or quinazolinone phosphatidylinositol 3-kinase inhibitors
NZ708864A (en) 2012-12-21 2016-09-30 Gilead Calistoga Llc Substituted pyrimidine aminoalkyl-quinazolones as phosphatidylinositol 3-kinase inhibitors
CA2903881C (en) 2013-03-15 2021-05-18 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
CA2915129C (en) 2013-06-14 2021-07-27 Gilead Sciences, Inc. Phosphatidylinositol 3-kinase inhibitors
CA2917319A1 (en) 2013-07-08 2015-01-15 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
EA036177B1 (ru) * 2013-08-13 2020-10-09 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Ингибиторы дезоксицитидинкиназы
WO2015030189A1 (ja) * 2013-08-29 2015-03-05 京都薬品工業株式会社 新規芳香族化合物およびその用途
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
FI3674302T3 (fi) 2014-04-23 2023-04-27 Incyte Holdings Corp 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONEJA JA PYRATSOLO[3,4-c]PYRIDIN-7(6H)-ONEJA BET-PROTEIINIEN INHIBIITTOREINA
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN105566329B (zh) * 2014-11-07 2019-02-12 温州医科大学 一种吡唑[5，6-d]并嘧啶类EGFR抑制剂及其抗肿瘤活性
MX2017004782A (es) * 2014-12-11 2017-07-27 Natco Pharma Ltd Derivados de 7-(morfolinil)-2-(n-piperazinil)metiltieno[2,3-c]piri dina como farmacos anticancerigenos.
US9637488B2 (en) 2015-01-29 2017-05-02 Fuqiang Ruan Heterocyclic compounds as inhibitors of class I PI3KS
CN105924433B (zh) * 2015-02-28 2020-12-22 广东东阳光药业有限公司 取代的氨基嘧啶类化合物及其使用方法和用途
SI3277682T1 (sl) 2015-03-30 2019-06-28 Daiichi Sankyo Company, Limited 6-morfolinil-2-pirazolil-9H-purin derivati in njihova uporaba kot PI3K inhibitorji
EP3310786B1 (en) 2015-06-16 2021-03-03 Nanophagix LLC Drug delivery and imaging chemical conjugate, formulations and methods of use thereof
MA42456B1 (fr) 2015-06-25 2021-06-30 Univ Health Network Inhibiteurs de hpk1 et leurs procédés d'utilisation
WO2017042182A1 (en) * 2015-09-08 2017-03-16 F. Hoffmann-La Roche Ag Tricyclic pi3k inhibitor compounds and methods of use
US10590126B2 (en) 2015-10-15 2020-03-17 Thomas Jefferson University Non-selective protease activated receptor 4 ALA120THR isoform antagonist
GB201518456D0 (en) * 2015-10-19 2015-12-02 Galapagos Nv Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory, autoimmune and/or proliferative diseases
AR106520A1 (es) 2015-10-29 2018-01-24 Incyte Corp Forma sólida amorfa de un inhibidor de proteína bet
US10919914B2 (en) 2016-06-08 2021-02-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
DK3472157T3 (da) 2016-06-20 2023-05-01 Incyte Corp Krystallinske faste former af en bet-inhibitor
US10261071B2 (en) * 2016-07-13 2019-04-16 The United States Of America As Represented By The Secretary Of The Navy Volatile organic compounds as diagnostic breath markers for pulmonary oxygen toxicity
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
GB201617630D0 (en) 2016-10-18 2016-11-30 Cellcentric Ltd Pharmaceutical compounds
CN110036109A (zh) 2016-12-02 2019-07-19 第一三共株式会社 新颖的内-β-N-乙酰基氨基葡糖苷酶
EP3551630A4 (en) * 2016-12-07 2020-07-15 Beigene, Ltd. IMIDAZO [1,5-A] PYRAZINE DERIVATIVES AS PI3KDELTA INHIBITORS
ES2944658T3 (es) 2017-09-08 2023-06-23 Beigene Ltd Derivados de imidazo[1,5-a]pirazina como inhibidores de PI3Kdelta
GB201806320D0 (en) 2018-04-18 2018-05-30 Cellcentric Ltd Process
MX2020014129A (es) * 2018-06-21 2021-06-18 Cellestia Biotech Ag Proceso para preparar amino diaril eteres.
JP2021530442A (ja) * 2018-06-28 2021-11-11 ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co., Ltd. 縮合三環系複素環化合物およびその治療上の使用
WO2020038387A1 (zh) * 2018-08-24 2020-02-27 杭州阿诺生物医药科技有限公司 高活性sting蛋白激动剂
BR112021006488A2 (pt) 2018-10-05 2021-07-06 Annapurna Bio Inc compostos e composições para o tratamento de condições associadas com atividade do receptor apj
JP7458406B2 (ja) 2018-12-21 2024-03-29 セルジーン コーポレーション Ｒｉｐｋ２のチエノピリジン阻害剤
CN110054558B (zh) * 2019-05-16 2022-03-25 海门瑞一医药科技有限公司 一种1-三氟甲基环丙烷-1-甲酸的制备方法
TW202146416A (zh) * 2019-12-11 2021-12-16 德商拜耳廠股份有限公司 吡唑并三𠯤
EP4114528A1 (en) * 2020-03-06 2023-01-11 Bayer Aktiengesellschaft Imidazotriazines acting on cancer via inhibition of cdk12
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4334315A1 (en) 2021-05-06 2024-03-13 Bayer Aktiengesellschaft Alkylamide substituted, annulated imidazoles and use thereof as insecticides
WO2025016314A1 (en) * 2023-07-14 2025-01-23 InventisBio Co., Ltd. Compounds, preparation methods and uses thereof

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
GB1570494A (en) * 1975-11-28 1980-07-02 Ici Ltd Thienopyrimidine derivatives and their use as pesticides
JPS6216477A (ja) * 1985-07-15 1987-01-24 Maruishi Seiyaku Kk 抗ウイルス活性を有する２−（４−ピリジルアミノメチル）−ベンズイミダゾ−ル誘導体
US4740230A (en) * 1985-09-13 1988-04-26 Idemitsu Kosan Company Limited Triazine derivatives, and herbicides containing the derivatives as the effective component
CA1279648C (en) * 1986-07-11 1991-01-29 Haruo Kuriyama 2-(4-pyridylaminometyl)-benzimidazole derivatives having antiviral activity
US4932998A (en) 1986-09-30 1990-06-12 Idemitsu Kosan Company Limited Triazine derivatives, and herbicides comprising the same as the effective ingredient
WO1988002368A1 (en) * 1986-09-30 1988-04-07 Idemitsu Kosan Company Limited Triazine derivative, production thereof, and herbicide containing same as effective ingredient
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
DE19920936A1 (de) 1999-05-07 2000-11-09 Basf Ag Heterozyklisch substituierte Benzimidazole, deren Herstellung und Anwendung
SE0102315D0 (sv) * 2001-06-28 2001-06-28 Astrazeneca Ab Compounds
US7354932B2 (en) * 2001-12-21 2008-04-08 Anormed, Inc. Chemokine receptor binding heterocyclic compounds with enhanced efficacy
EP1670802A4 (en) 2003-09-18 2010-07-07 Conforma Therapeutics Corp NOVEL HETEROCYCLIC COMPOUNDS AS INHIBITORS OF HSP90 PROTEIN
JP4800216B2 (ja) * 2003-10-24 2011-10-26 エグゼリクシス， インコーポレイテッド ｐ７０Ｓ６キナーゼモジュレーターおよび使用方法
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
JP2007277093A (ja) * 2004-06-21 2007-10-25 Astellas Pharma Inc 三環系化合物
CA2575560A1 (en) 2004-08-02 2006-02-23 Smithkline Beecham Corporation Chemical compounds
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
PT1934174E (pt) 2005-10-07 2011-07-14 Exelixis Inc Azetidinas como inibidores de mek para o tratamento de doenças proliferativas
CA2650295C (en) * 2006-04-26 2015-12-29 Genentech, Inc. Phosphoinositide 3-kinase inhibitor compounds and pharmaceutical compositions containing them
US8802670B2 (en) 2006-04-26 2014-08-12 F. Hoffmann-La Roche Ag Pharmaceutical compounds
HRP20100446T1 (hr) 2006-04-26 2010-09-30 F. Hoffmann-La Roche Ag Derivat tieno[3,2-d]pirimidina koristan kao inhibitor pi3k
HUE035116T2 (hu) * 2006-08-08 2018-05-02 Chugai Pharmaceutical Co Ltd PI3K inhibitor pirimidinszármazékok és alkalmazásuk
WO2008039882A1 (en) 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist
EP2527345B1 (en) * 2006-10-16 2015-12-16 Thesan Pharmaceuticals, Inc. Therapeutic pyrazolyl thienopyridines
AR064154A1 (es) 2006-12-07 2009-03-18 Piramed Ltd Compuestos inhibidores de fodfoinostida 3- quinasas y composiciones farmaceuticas
KR101460816B1 (ko) 2006-12-07 2014-11-12 에프. 호프만-라 로슈 아게 포스포이노시타이드 3-키나제 억제제 화합물 및 그의 사용 방법
WO2008152394A1 (en) 2007-06-12 2008-12-18 F.Hoffmann-La Roche Ag Pharmaceutical compounds
WO2009034386A1 (en) * 2007-09-13 2009-03-19 Astrazeneca Ab Derivatives of adenine and 8-aza-adenine and uses thereof-796
CA2703138A1 (en) 2007-10-26 2009-04-30 F. Hoffmann-La Roche Ag Purine derivatives useful as pi3 kinase inhibitors
GB0725218D0 (en) * 2007-12-24 2008-02-06 Syngenta Ltd Chemical compounds
AU2009248993C1 (en) * 2008-05-23 2013-10-03 Wyeth Llc Triazine compounds as PI3 kinase and mTOR inhibitors
WO2010138589A1 (en) 2009-05-27 2010-12-02 Genentech, Inc. Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
EP2451811A1 (en) * 2009-05-27 2012-05-16 F. Hoffmann-La Roche AG Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
UY33304A (es) * 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
US9062055B2 (en) * 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors

Also Published As

Publication number Publication date
MX2013008822A (es) 2013-10-07
KR20130116358A (ko) 2013-10-23
US20120202785A1 (en) 2012-08-09
EP2673269A1 (en) 2013-12-18
JP5766820B2 (ja) 2015-08-19
CN103476767A (zh) 2013-12-25
CA2825028A1 (en) 2012-08-16
CN103476767B (zh) 2015-06-10
JP2014508145A (ja) 2014-04-03
RU2013138835A (ru) 2015-03-20
WO2012107465A1 (en) 2012-08-16
US8653089B2 (en) 2014-02-18

Similar Documents

Publication Publication Date Title
BR112013020329A2 (pt) compostos heterocíclicos como inibidores da pi3-quinase
BR112013024122A2 (pt) compostos de benzoxazepina seletivos para p110 delta pi3k e métodos de uso
BR112012019635A2 (pt) compostos inibidores de pirido[3,2-d] pirimidina pi3k delta e métodos de uso
PH12014500966A1 (en) Alkylated piperazine compounds as inhibitors of btk activity
MX2014005285A (es) Compuestos biciclicos de piperazina.
UA111756C2 (uk) Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
MX2014005282A (es) Compuestos de 8-fluoroftalazin-1 (2h) -ona.
MX2014014828A (es) Compuestos de 5-azaindazol y metodos de uso.
BR112013014914B8 (pt) composto, composição farmacêutica e uso de um composto
MY160349A (en) Pyridone and aza-pyridone compounds and methods of use
EA201590624A1 (ru) Циклические эфиры пиразол-4-ил-гетероциклил-карбоксамидных соединений и способы их применения
UA116774C2 (uk) Інгібітори серин/треонінкінази
MX2019003468A (es) Derivados de tieno [3,2-d]pirimidina que tienen actividad inhibidora de las cinasas de proteina.
MX2014001239A (es) Compuestos de pirazolo [3,4-c] piridina y metodos de uso.
EA201290957A1 (ru) Пиразол-4-илгетероциклилкарбоксамидные соединения и способы их применения
BR112015029972A2 (pt) composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, método para o tratamento de uma doença, conjunto e utilização de um composto
BRPI0913580B8 (pt) compostos de pirrolopiridinas como inibidores de quinase e composição farmacêutica compreendendo os referidos compostos
MX2011012520A (es) Compuestos inhibidores de pi3k de pirimidina biciclicos selectivos para p110 delta y metodos de uso de los mismos.
MX2016007171A (es) Compuestos de heteroaril piridona y azapiridona con funcionalidad electrofila.
BR112016015235A2 (pt) Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento
BR112015028501A2 (pt) derivados de bipirazol como inibidores de jak
MX2016003861A (es) Nuevos derivados de 1-(4-pirimidinil)-1h-pirrolo[3,2-c]piridina como inhibidores de la cinasa inductora de nf-kappab.
NZ620928A (en) Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
TH151329A (th) ไพริมิดิโนนเป็นสารยับยั้ง pi3k
MA42864A1 (fr) Composes d’éther cyclique-pyrazol-4-yl-heterocyclyl-carboxamide et procédés d'utilisation

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]