CN101801955B - 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 - Google Patents

作为akt蛋白激酶抑制剂的嘧啶基环戊烷 Download PDF

Info

Publication number
CN101801955B
CN101801955B CN2008801058695A CN200880105869A CN101801955B CN 101801955 B CN101801955 B CN 101801955B CN 2008801058695 A CN2008801058695 A CN 2008801058695A CN 200880105869 A CN200880105869 A CN 200880105869A CN 101801955 B CN101801955 B CN 101801955B
Authority
CN
China
Prior art keywords
dihydro
cyclopenta
piperazine
pyrimidine
ethyl ketone
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN2008801058695A
Other languages
English (en)
Chinese (zh)
Other versions
CN101801955A (zh
Inventor
约瑟夫·本克希克
詹姆斯·F·布莱克
詹姆斯·M·格雷厄姆
马丁·F·亨特曼
尼古拉斯·C·卡兰
伊恩·S·米切尔
斯蒂芬·T·施拉克特
基思·L·斯潘瑟
校登明
徐睿
迈克·韦尔克
梁军
布赖恩·S·萨芬娜
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Array Biopharma Inc
Original Assignee
Genentech Inc
Array Biopharma Inc
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 Genentech Inc, Array Biopharma Inc filed Critical Genentech Inc
Publication of CN101801955A publication Critical patent/CN101801955A/zh
Application granted granted Critical
Publication of CN101801955B publication Critical patent/CN101801955B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • A61P11/08—Bronchodilators
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P33/00—Antiparasitic agents
    • 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
    • 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
    • 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
    • A61P9/10—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
CN2008801058695A 2007-07-05 2008-07-03 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 Active CN101801955B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94813807P 2007-07-05 2007-07-05
US60/948,138 2007-07-05
US2008808P 2008-01-09 2008-01-09
US61/020,088 2008-01-09
PCT/US2008/069144 WO2009006567A2 (en) 2007-07-05 2008-07-03 Pyrimidyl cyclopentanes as akt protein kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201310128477.3A Division CN103396409B (zh) 2007-07-05 2008-07-03 作为akt蛋白激酶抑制剂的嘧啶基环戊烷

Publications (2)

Publication Number Publication Date
CN101801955A CN101801955A (zh) 2010-08-11
CN101801955B true CN101801955B (zh) 2013-05-08

Family

ID=40076864

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201310128477.3A Active CN103396409B (zh) 2007-07-05 2008-07-03 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
CN2008801058695A Active CN101801955B (zh) 2007-07-05 2008-07-03 作为akt蛋白激酶抑制剂的嘧啶基环戊烷

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201310128477.3A Active CN103396409B (zh) 2007-07-05 2008-07-03 作为akt蛋白激酶抑制剂的嘧啶基环戊烷

Country Status (19)

Country Link
US (1) US8618097B2 (OSRAM)
EP (1) EP2170863B1 (OSRAM)
JP (2) JP5628028B2 (OSRAM)
KR (2) KR20150089099A (OSRAM)
CN (2) CN103396409B (OSRAM)
AR (1) AR067413A1 (OSRAM)
AU (1) AU2008272830B8 (OSRAM)
BR (1) BRPI0813999A2 (OSRAM)
CA (1) CA2692502C (OSRAM)
CO (1) CO6251283A2 (OSRAM)
CR (1) CR11229A (OSRAM)
EC (1) ECSP109937A (OSRAM)
ES (1) ES2551352T3 (OSRAM)
MA (1) MA31679B1 (OSRAM)
NZ (1) NZ582692A (OSRAM)
RU (1) RU2486181C2 (OSRAM)
SG (1) SG185274A1 (OSRAM)
TW (1) TWI450720B (OSRAM)
WO (1) WO2009006567A2 (OSRAM)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2068878B1 (en) 2006-09-20 2019-04-10 Aerie Pharmaceuticals, Inc. Rho kinase inhibitors
US8455513B2 (en) 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
WO2009089352A1 (en) 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors
EP2240455B1 (en) 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
EP2240483B8 (en) * 2008-01-09 2013-04-03 Array Biopharma, Inc. Pyrimidyl cyclopentanes as akt protein kinase inhibitors
ES2422733T3 (es) 2008-01-09 2013-09-13 Array Biopharma Inc Pirimidilciclopentanos hidroxilados como inhibidores de proteínas cinasas AKT
US8372842B2 (en) 2008-01-09 2013-02-12 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
ES2426092T3 (es) 2008-01-09 2013-10-21 Array Biopharma, Inc. 5H-Ciclopenta[d]pirimidinas como inhibidores de proteínas cinasas AKT
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
ES2834451T3 (es) 2009-05-01 2021-06-17 Aerie Pharmaceuticals Inc Inhibidores de mecanismo doble para el tratamiento de enfermedades
JP2013528787A (ja) 2010-04-16 2013-07-11 ジェネンテック， インコーポレイテッド Ｐｉ３ｋ／ａｋｔキナーゼ経路インヒビターの効果の予測バイオマーカーとしてのｆｏｘ０３ａ
SG10201507582VA (en) 2011-04-01 2015-10-29 Genentech Inc Biomarkers for predicting sensitivity to cancer treatments
KR102678074B1 (ko) 2012-05-17 2024-06-26 제넨테크, 인크. 무정형 형태의 akt 저해성 피리미디닐 - 사이클로펜탄 화합물, 조성물 및 이들의 방법
US9452990B2 (en) 2012-06-20 2016-09-27 Novartis Ag Complement pathway modulators and uses thereof
KR102182488B1 (ko) 2013-02-25 2020-11-24 제넨테크, 인크. 약물 내성 akt 돌연변이체의 검출 및 치료를 위한 방법 및 조성물
PT3811943T (pt) 2013-03-15 2023-03-15 Aerie Pharmaceuticals Inc Composto para uso no tratamento de distúrbios oculares
US10550087B2 (en) 2015-11-17 2020-02-04 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
US11389441B2 (en) 2016-08-31 2022-07-19 Aerie Pharmaceuticals, Inc. Ophthalmic compositions
CA3041840A1 (en) 2016-10-28 2018-05-03 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating ezh2-mediated cancer
JP2020515583A (ja) 2017-03-31 2020-05-28 アエリエ ファーマシューティカルズ インコーポレイテッド アリールシクロプロピル−アミノ−イソキノリニルアミド化合物
US11472799B2 (en) * 2018-03-06 2022-10-18 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (AKT) degradation / disruption compounds and methods of use
JP7720698B2 (ja) * 2018-04-04 2025-08-08 アルビナス・オペレーションズ・インコーポレイテッド タンパク質分解の調節因子および関連する使用方法
CA3104298A1 (en) 2018-06-21 2019-12-26 Icahn School Of Medicine At Mount Sinai Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use
AU2019337703B2 (en) 2018-09-14 2023-02-02 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
US20220185796A1 (en) * 2019-03-27 2022-06-16 St. Jude Children's Research Hospital Small molecule modulators of pank
CN114423463B (zh) 2019-05-06 2025-09-26 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
US12103924B2 (en) 2020-06-01 2024-10-01 Icahn School Of Medicine At Mount Sinai Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use
CN117677614A (zh) * 2021-12-17 2024-03-08 中国医药研究开发中心有限公司 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途
KR20250151412A (ko) 2023-01-26 2025-10-21 아비나스 오퍼레이션스, 인코포레이티드 세레블론계 kras 분해 단백질 및 이와 관련된 용도

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040009968A1 (en) * 2002-01-25 2004-01-15 Hayley Binch Indazole compounds useful as protein kinase inhibitors
EP1803710A1 (en) * 2004-10-20 2007-07-04 Astellas Pharma Inc. Pyrimidine derivative condensed with non-aromatic ring

Family Cites Families (100)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3885035A (en) 1972-04-05 1975-05-20 Sandoz Ag Method for treating arrhythmia by using 1,4-bis(4 quinazolinyl) piperazines
US3956495A (en) 1973-10-30 1976-05-11 Eli Lilly And Company 2,4-Diaminoquinazolines as antithrombotic agents
US3966936A (en) 1974-02-21 1976-06-29 Pfizer Inc. Piperazino quinazoline bronchodilators
US4060615A (en) 1976-02-18 1977-11-29 Mead Johnson & Company 2-Piperazinyl-6,7-dimethoxyquinazolines
JPS562968A (en) 1979-06-21 1981-01-13 Mitsubishi Yuka Yakuhin Kk Novel pyrimidine derivative
US4749704A (en) 1985-03-07 1988-06-07 Sankyo Company Limited Cyclopenta[d]pyrimidine derivatives and use as antidepressants
MX19185A (es) 1989-01-20 1993-12-01 Pfizer Procedimiento para preparar 3-(1,2,5,6-tretrahidropiridil)-pirrolopiridinas.
WO1994007890A1 (fr) 1992-10-05 1994-04-14 Ube Industries, Ltd. Compose pyrimidine
WO1995003286A1 (en) 1993-07-23 1995-02-02 The Green Cross Corporation Triazole derivative and pharmaceutical use thereof
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
JP2896532B2 (ja) 1994-08-13 1999-05-31 ユーハン コーポレーション 新規なピリミジン誘導体およびその製造方法
US5525625A (en) 1995-01-24 1996-06-11 Warner-Lambert Company 2-(2-Amino-3-methoxyphenyl)-4-oxo-4H-[1]benzopyran for treating proliferative disorders
US7067664B1 (en) 1995-06-06 2006-06-27 Pfizer Inc. Corticotropin releasing factor antagonists
ZA979961B (en) 1996-11-15 1999-05-05 Lilly Co Eli 5-HT1F agonists
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6821963B2 (en) 1997-07-01 2004-11-23 Warner-Lambert Company 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors
AU756586C (en) 1997-07-01 2004-01-29 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
ES2229515T3 (es) 1997-07-01 2005-04-16 Warner-Lambert Company Llc Derivados 4-bromo o 4-yodo del acido fenilamino benzhidroxamico y su uso como inhibidores de la mek.
US6506798B1 (en) 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
US6310060B1 (en) 1998-06-24 2001-10-30 Warner-Lambert Company 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors
ES2356886T3 (es) 1998-03-31 2011-04-14 Kyowa Hakko Kirin Co., Ltd. Compuestos heterocíclicos nitrogenados.
DE19853278A1 (de) 1998-11-19 2000-05-25 Aventis Pharma Gmbh Substituierte 4-Amino-2-aryl-cyclopenta[d]pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate
ATE292462T1 (de) 1999-01-07 2005-04-15 Warner Lambert Co Behandlung von asthma anhand von mek-inhibitoren
EP1140067A1 (en) 1999-01-07 2001-10-10 Warner-Lambert Company Antiviral method using mek inhibitors
WO2000042002A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors
US6545030B1 (en) 1999-01-13 2003-04-08 Warner-Lambert Company 1-heterocycle substituted diarylamines
JP2002534446A (ja) 1999-01-13 2002-10-15 ワーナー−ランバート・カンパニー ４′ヘテロアリールジアリールアミン
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
IL144214A0 (en) 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
US6440966B1 (en) 1999-01-13 2002-08-27 Warner-Lambert Company Benzenesulfonamide derivatives and their use as MEK inhibitors
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
HK1047895A1 (zh) 1999-07-16 2003-03-14 沃尼尔‧朗伯公司 使用mek抑制剂治疗慢性疼痛的方法
CA2377100A1 (en) 1999-07-16 2001-01-25 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
TR200200082T2 (tr) 1999-07-16 2002-04-22 Warner-Lambert Company MEK inhibitörleri kullanılarak kronik ağrının tedavi edilmesi.
CN1358094A (zh) 1999-07-16 2002-07-10 沃尼尔·朗伯公司 用mek抑制剂治疗慢性疼痛的方法
AU2001247372A1 (en) 2000-03-15 2001-09-24 Warner Lambert Company 5-amide substituted diarylamines as mex inhibitors
DZ3401A1 (fr) 2000-07-19 2002-01-24 Warner Lambert Co Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques
IL154507A0 (en) 2000-08-25 2003-09-17 Warner Lambert Co Process for making n-aryl-anthranilic acids and their derivatives
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
EP1337524A1 (en) 2000-11-02 2003-08-27 AstraZeneca AB Substituted quinolines as antitumor agents
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
CA2446514A1 (en) 2001-04-30 2002-11-07 Glaxo Group Limited Fused pyrimidines as antagonists of the corticotropin releasing factor (crf)
WO2003022214A2 (en) 2001-09-06 2003-03-20 Millennium Pharmaceuticals, Inc. Piperazine and homopiperazine compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
TWI338685B (en) 2002-03-13 2011-03-11 Array Biopharma Inc N3 alkylated benzimid azole derivatives as mek inhibitors
PA8569201A1 (es) 2002-03-13 2004-05-21 Array Biopharma Inc "derivados de bencimidazol n3 alquilado como inhibidores de mek" "n3 alkylated benzimimidazole derivatives as mek inhibitors"
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
CA2480880C (en) 2002-04-08 2011-03-22 Merck & Co., Inc. Inhibitors of akt activity
JP4394959B2 (ja) 2002-04-08 2010-01-06 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性の阻害剤
CA2481241C (en) 2002-04-08 2010-07-27 Merck & Co., Inc. Fused quinoxaline derivatives as inhibitors of akt activity
WO2003086394A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
EP1503761A1 (en) 2002-05-10 2005-02-09 Neurocrine Biosciences, Inc. Substituted piperazines as melanocortin receptor ligands
AU2003284981B2 (en) 2002-10-30 2009-05-28 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
US20040102360A1 (en) 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
GB0308208D0 (en) 2003-04-09 2003-05-14 Glaxo Group Ltd Chemical compounds
CN1809351A (zh) 2003-04-24 2006-07-26 麦克公司 Akt活性抑制剂
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
EP1663994B1 (en) 2003-08-05 2012-03-07 Vertex Pharmaceuticals Incorporated Tetrahydroquinazoline compounds as inhibitors of voltage-gated ion channels
JP2007501821A (ja) 2003-08-12 2007-02-01 エフ．ホフマン−ラ　ロシュ　アーゲー Ｃｆｒアンタゴニストとしてのテトラヒドロキナゾリン誘導体
EP1666468A4 (en) 2003-09-09 2007-03-21 Ono Pharmaceutical Co CRF ANTAGONISTS AND HETEROBICYCLIC COMPOUNDS
US20050182061A1 (en) 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
PH12012501891A1 (en) 2003-11-21 2013-09-02 Array Biopharma Inc Akt protein kinase inhibitors
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
WO2005113762A1 (en) 2004-05-18 2005-12-01 Pfizer Products Inc. CRYSTAL STRUCTURE OF PROTEIN KINASE B-α (AKT-1) AND USES THEREOF
US20060025074A1 (en) 2004-07-30 2006-02-02 Chih-Ming Liang Bluetooth-based headset
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
TWM266655U (en) 2004-09-23 2005-06-01 Blueexpert Technology Corp Bluetooth earphone device capable of wirelessly receiving and transmitting stereo sound signal and digital information signal
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
ATE543821T1 (de) 2004-12-28 2012-02-15 Exelixis Inc Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen
CA2598956A1 (en) 2005-02-24 2006-08-31 Pfizer Products Inc. Bicyclic heteroaromatic derivatives useful as anticancer agents
US20090029982A1 (en) * 2005-04-28 2009-01-29 Supergen, Inc. Protein kinase inhibitors
EP1881983B1 (en) 2005-05-20 2012-01-11 Vertex Pharmaceuticals, Inc. Pyrrolopyridines useful as inhibitors of protein kinase
HRP20130429T1 (en) 2005-06-10 2013-06-30 Merck Sharp & Dohme Corp. Inhibitors of akt activity
UY29610A1 (es) 2005-06-21 2007-01-31 Cancer Rec Tech Ltd Aril-alquilaminas y heteroaril-alquilaminas como inhibidores de la quinasa proteínica
EP1948659A1 (en) 2005-10-13 2008-07-30 Glaxo Group Limited Pyrrolopyrimidine derivatives as syk inhibitors
WO2007077961A2 (en) 2005-12-28 2007-07-12 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds and their use as mineralocorticoid receptor ligands
JP2009534454A (ja) 2006-04-25 2009-09-24 アステックス、セラピューティックス、リミテッド 医薬化合物
KR20090024834A (ko) 2006-07-05 2009-03-09 인터뮨, 인크. Ｃ형 간염 바이러스 복제의 신규 억제제
NZ573979A (en) 2006-07-06 2012-02-24 Array Biopharma Inc Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CA2655675A1 (en) 2006-07-06 2008-01-10 Glaxo Group Limited Substituted n-phenylmethyl -5-oxo-proline-2-amides as p2x7-receptor antagonists and their methods of use
US8329701B2 (en) 2006-07-06 2012-12-11 Array Biopharma Inc. Dihydrofuro pyrimidines as AKT protein kinase inhibitors
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
UA95641C2 (xx) 2006-07-06 2011-08-25 Эррей Биофарма Инк. Гідроксильовані піримідильні циклопентани як інгібітори акт протеїнкінази$гидроксилированные пиримидильные циклопентаны как ингибиторы акт протеинкиназы
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
US7659270B2 (en) * 2006-08-11 2010-02-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8329159B2 (en) * 2006-08-11 2012-12-11 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2008029907A1 (en) * 2006-09-08 2008-03-13 Kyowa Hakko Bio Co., Ltd. Hypertension-ameliorating agent
US7741347B2 (en) * 2007-05-17 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
MX2009014013A (es) 2007-07-05 2010-01-28 Array Biopharma Inc Pirimidil ciclopentanos como inhibidores de la proteina cinasa akt.
US8629171B2 (en) * 2007-08-08 2014-01-14 Bristol-Myers Squibb Company Crystalline form of methyl ((1S)-1-((25)-2-(5-(4'-(2-((25)-1((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt
EP2240455B1 (en) 2008-01-09 2012-12-26 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
ES2426092T3 (es) 2008-01-09 2013-10-21 Array Biopharma, Inc. 5H-Ciclopenta[d]pirimidinas como inhibidores de proteínas cinasas AKT
ES2422733T3 (es) 2008-01-09 2013-09-13 Array Biopharma Inc Pirimidilciclopentanos hidroxilados como inhibidores de proteínas cinasas AKT
US7704992B2 (en) * 2008-02-13 2010-04-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7906655B2 (en) * 2008-08-07 2011-03-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2010096462A1 (en) * 2009-02-17 2010-08-26 Enanta Pharmaceuticals, Inc Linked diimidazole derivatives
HUE036906T2 (hu) * 2009-05-13 2018-08-28 Antivirális vegyületek

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040009968A1 (en) * 2002-01-25 2004-01-15 Hayley Binch Indazole compounds useful as protein kinase inhibitors
EP1803710A1 (en) * 2004-10-20 2007-07-04 Astellas Pharma Inc. Pyrimidine derivative condensed with non-aromatic ring

Also Published As

Publication number Publication date
JP2014028842A (ja) 2014-02-13
SG185274A1 (en) 2012-11-29
RU2486181C2 (ru) 2013-06-27
RU2010103813A (ru) 2011-08-10
TWI450720B (zh) 2014-09-01
NZ582692A (en) 2012-05-25
BRPI0813999A2 (pt) 2019-10-01
CN101801955A (zh) 2010-08-11
US20110015204A1 (en) 2011-01-20
US8618097B2 (en) 2013-12-31
CA2692502C (en) 2016-03-01
KR20150089099A (ko) 2015-08-04
EP2170863B1 (en) 2015-09-02
WO2009006567A2 (en) 2009-01-08
CN103396409B (zh) 2015-03-11
CA2692502A1 (en) 2009-01-08
HK1147255A1 (en) 2011-08-05
MA31679B1 (fr) 2010-09-01
EP2170863A2 (en) 2010-04-07
CN103396409A (zh) 2013-11-20
AR067413A1 (es) 2009-10-07
CR11229A (es) 2010-02-09
AU2008272830B8 (en) 2013-12-12
AU2008272830A1 (en) 2009-01-08
KR101650956B1 (ko) 2016-08-24
CO6251283A2 (es) 2011-02-21
JP5628028B2 (ja) 2014-11-19
ECSP109937A (es) 2010-03-31
JP2010532386A (ja) 2010-10-07
TW200902013A (en) 2009-01-16
AU2008272830B2 (en) 2013-12-05
KR20100044819A (ko) 2010-04-30
ES2551352T3 (es) 2015-11-18
WO2009006567A3 (en) 2009-03-19

Similar Documents

Publication Publication Date Title
CN101801955B (zh) 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
CN101631778B (zh) 作为akt蛋白激酶抑制剂的环戊二烯并[d]嘧啶
AU2008272832B2 (en) Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CN101578273A (zh) 作为akt蛋白激酶抑制剂的羟基化和甲氧基化的环戊二烯并[d]嘧啶
US9409886B2 (en) Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
HK1147255B (en) Pyrimidyl cyclopentanes as akt protein kinase inhibitors
HK1185873A (en) Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
HK1136832B (en) Pyrimidyl cyclopentanes as akt protein kinase inhibitors

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1147255

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1147255

Country of ref document: HK