KR101650956B1 - Ａｋｔ 단백질 키나제 억제제로서의 피리미딜 시클로펜탄 - Google Patents

Ａｋｔ 단백질 키나제 억제제로서의 피리미딜 시클로펜탄 Download PDF

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KR101650956B1
KR101650956B1 KR1020107002558A KR20107002558A KR101650956B1 KR 101650956 B1 KR101650956 B1 KR 101650956B1 KR 1020107002558 A KR1020107002558 A KR 1020107002558A KR 20107002558 A KR20107002558 A KR 20107002558A KR 101650956 B1 KR101650956 B1 KR 101650956B1
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pyrimidin
cyclopenta
piperazin
dihydro
methyl
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Expired - Fee Related
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KR20100044819A (ko
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조세프 벵시크
제임스 에프. 블레이크
제임스 엠. 그레이엄
마틴 에프. 헨트먼
니콜라스 씨. 캘런
이언 에스. 미첼
스티븐 티. 슐락터
키스 엘. 스펜서
뎅밍 샤오
루이 수
마이크 웰치
준 리앙
브라이언 에스. 사피나
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어레이 바이오파마 인크.
제넨테크, 인크.
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    • 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
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    • A61P13/08—Drugs for disorders of the urinary system of the prostate
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    • 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
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    • 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

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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
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  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Virology (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
KR1020107002558A 2007-07-05 2008-07-03 Ａｋｔ 단백질 키나제 억제제로서의 피리미딜 시클로펜탄 Expired - Fee Related KR101650956B1 (ko)

Applications Claiming Priority (4)

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

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KR1020157020046A Division KR20150089099A (ko) 2007-07-05 2008-07-03 Ａｋｔ 단백질 키나제 억제제로서의 피리미딜 시클로펜탄

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KR20100044819A KR20100044819A (ko) 2010-04-30
KR101650956B1 true KR101650956B1 (ko) 2016-08-24

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KR1020107002558A Expired - Fee Related KR101650956B1 (ko) 2007-07-05 2008-07-03 Ａｋｔ 단백질 키나제 억제제로서의 피리미딜 시클로펜탄

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US (1) US8618097B2 (enExample)
EP (1) EP2170863B1 (enExample)
JP (2) JP5628028B2 (enExample)
KR (2) KR20150089099A (enExample)
CN (2) CN101801955B (enExample)
AR (1) AR067413A1 (enExample)
AU (1) AU2008272830B8 (enExample)
BR (1) BRPI0813999A2 (enExample)
CA (1) CA2692502C (enExample)
CO (1) CO6251283A2 (enExample)
CR (1) CR11229A (enExample)
EC (1) ECSP109937A (enExample)
ES (1) ES2551352T3 (enExample)
MA (1) MA31679B1 (enExample)
NZ (1) NZ582692A (enExample)
RU (1) RU2486181C2 (enExample)
SG (1) SG185274A1 (enExample)
TW (1) TWI450720B (enExample)
WO (1) WO2009006567A2 (enExample)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2729424T3 (es) 2006-09-20 2019-11-04 Aerie Pharmaceuticals Inc Inhibidores de Rho cinasa
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
EP2242755B1 (en) 2008-01-08 2012-09-12 Array Biopharma, Inc. Pyrrolopyridines as kinase inhibitors
WO2009089462A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors
CA2711692A1 (en) * 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
WO2009089459A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
JP5512545B2 (ja) * 2008-01-09 2014-06-04 アレイ バイオファーマ、インコーポレイテッド Ａｋｔタンパク質キナーゼ阻害剤としてのピリミジルシクロペンタン類
EP2242757B1 (en) 2008-01-09 2012-08-01 Array Biopharma, Inc. Pyrazolopyridines as kinase inhibitors
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
CA2760562C (en) 2009-05-01 2016-07-19 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
KR20130058672A (ko) 2010-04-16 2013-06-04 제넨테크, 인크. ＰＩ3Ｋ/ＡＫＴ 키나제 경로 억제제 효능에 대한 예측 바이오마커로서의 ＦＯＸＯ３ａ
RU2635193C2 (ru) 2011-04-01 2017-11-09 Дженентек, Инк. Биомаркеры для прогнозирования чувствительности к противоопухолевой терапии
HUE051254T2 (hu) 2012-05-17 2021-03-01 Genentech Inc Egy AKT-gátló pirimidin-ciklopentán vegyület amorf formája, annak kompozíciói és eljárásai
US9452990B2 (en) 2012-06-20 2016-09-27 Novartis Ag Complement pathway modulators and uses thereof
CA2901126C (en) 2013-02-25 2022-01-25 Genentech, Inc. Methods and compositions for detecting and treating drug resistant akt mutant
PT3811943T (pt) 2013-03-15 2023-03-15 Aerie Pharmaceuticals Inc Composto para uso no tratamento de distúrbios oculares
JP6832946B2 (ja) * 2015-11-17 2021-02-24 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 キナーゼ阻害剤およびその中間体の調製方法
US9643927B1 (en) 2015-11-17 2017-05-09 Aerie Pharmaceuticals, Inc. Process for the preparation of kinase inhibitors and intermediates thereof
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment
CN109640966A (zh) 2016-08-31 2019-04-16 爱瑞制药公司 眼用组合物
EP3532464A4 (en) 2016-10-28 2020-07-08 Icahn School of Medicine at Mount Sinai COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER
SG11201908179UA (en) 2017-03-31 2019-10-30 Aerie Pharmaceuticals Inc Aryl cyclopropyl-amino-isoquinolinyl amide compounds
AU2019231689A1 (en) * 2018-03-06 2020-09-24 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (AKT) degradation / disruption compounds and methods of use
MX2020010420A (es) * 2018-04-04 2020-12-11 Arvinas Operations Inc Moduladores de la proteólisis y métodos asociados de uso.
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
WO2020056345A1 (en) 2018-09-14 2020-03-19 Aerie Pharmaceuticals, Inc. Aryl cyclopropyl-amino-isoquinolinyl amide compounds
WO2020198526A2 (en) * 2019-03-27 2020-10-01 St. Jude Children's Research Hospital Small molecule modulators of pank
CA3137916A1 (en) 2019-05-06 2020-11-12 Ichan School Of Medicine At Mount Sinai Heterobifunctional compounds as degraders of hpk1
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
WO2023109540A1 (zh) * 2021-12-17 2023-06-22 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
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto

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
JPS6270A (ja) 1985-03-07 1987-01-06 Sankyo Co Ltd シクロペンタ〔ｄ〕ピリミジン誘導体
WO1990007926A1 (en) 1989-01-20 1990-07-26 Pfizer Inc. 3-(1,2,5,6-tetrahydropyridyl)-pyrrolopyridines
KR100262254B1 (ko) 1992-10-05 2000-07-15 나카히로 마오미 피리미딘 화합물
EP0710654A4 (en) 1993-07-23 1996-08-28 Green Cross Corp TRIAZOLE DERIVATIVE AND ITS PHARMACEUTICAL USE
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
RU2129549C1 (ru) 1994-08-13 1999-04-27 Юхан Корпорейшн Производные пиримидина и способы их получения
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
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
JP2002511092A (ja) 1997-07-01 2002-04-09 ワーナー−ランバート・コンパニー ４−ブロモまたは４−ヨードフェニルアミノベンズヒドロキサム酸誘導体およびそのｍｅｋ阻害剤としての使用
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
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
WO1999051582A1 (en) 1998-03-31 1999-10-14 Kyowa Hakko Kogyo Co., Ltd. Nitrogenous heterocyclic compounds
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
CA2358438A1 (en) 1999-01-07 2000-07-13 David Thomas Dudley Antiviral method using mek inhibitors
DE69924641D1 (de) 1999-01-07 2005-05-12 Warner Lambert Company Llc Mor Behandlung von asthma anhand von mek-inhibitoren
WO2000042002A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors
WO2000042029A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company 1-heterocycle substituted diarylamines
AU2203700A (en) 1999-01-13 2000-08-01 Warner-Lambert Company Benzoheterocycles and their use as mek inhibitors
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
WO2000042003A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
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
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
TR200200205T2 (tr) 1999-07-16 2002-06-21 Warner-Lambert Company MEK inhibitörleri kullanılarak kronik ağrının tedavi edilmesi
EP1202726A2 (en) 1999-07-16 2002-05-08 Warner-Lambert Company Llc Method for treating chronic pain using mek inhibitors
IL147617A0 (en) 1999-07-16 2002-08-14 Warner Lambert Co Method for treating chronic pain using mek inhibitors
KR20020015376A (ko) 1999-07-16 2002-02-27 로즈 암스트롱, 크리스틴 에이. 트러트웨인 Ｍｅｋ 억제제를 사용한 만성 통증의 치료 방법
MXPA02008103A (es) 2000-03-15 2002-11-29 Warner Lambert Co Diarilaminas sustituidas con 5-amida como inhibidores mek.
US6960614B2 (en) 2000-07-19 2005-11-01 Warner-Lambert Company Oxygenated esters of 4-lodo phenylamino benzhydroxamic acids
MXPA03001654A (es) 2000-08-25 2004-09-10 Warner Lambert Co Proceso para la elaboracion del acido n-aril-antranilico y sus derivados.
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
JP2004514718A (ja) 2000-11-02 2004-05-20 アストラゼネカ　アクチボラグ 抗癌剤としての置換キノリン類
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
AR033295A1 (es) 2001-04-30 2003-12-10 Glaxo Group Ltd Compuestos biciclicos de pirimidina, proceso para su obtencion, uso de los mismos para la preparacion de una composicion farmaceutica y dicha composicion farmaceutica
US7115741B2 (en) 2001-09-06 2006-10-03 Levy Daniel E 4-thieno[2,3-D]pyrimidin-4-YL piperazine compounds
US20030187026A1 (en) 2001-12-13 2003-10-02 Qun Li Kinase inhibitors
JP2005526076A (ja) 2002-03-13 2005-09-02 アレイ バイオファーマ、インコーポレイテッド Ｍｅｋ阻害剤としてのｎ３アルキル化ベンズイミダゾール誘導体
MXPA04008893A (es) 2002-03-13 2005-06-20 Array Biopharma Inc Derivados de bencimidazol n3 alquilados como inhibidores de mek.
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
AU2003223467B2 (en) 2002-04-08 2007-10-04 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
JP4451136B2 (ja) 2002-04-08 2010-04-14 メルク エンド カムパニー インコーポレーテッド Ａｋｔ活性阻害薬
CA2481229C (en) 2002-04-08 2010-09-21 Merck & Co., Inc. Substituted pyrazine inhibitors of akt
CA2481241C (en) 2002-04-08 2010-07-27 Merck & Co., Inc. Fused quinoxaline derivatives as inhibitors of akt activity
MXPA04011093A (es) 2002-05-10 2005-02-14 Neurocrine Biosciences Inc Piperazina sustituida como ligandos de receptores de melanocortina.
DE60336576D1 (de) 2002-10-30 2011-05-12 Merck Sharp & Dohme Hemmer der akt aktivität
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
JP2006524254A (ja) 2003-04-24 2006-10-26 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
ATE440825T1 (de) 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
KR20060118398A (ko) 2003-08-05 2006-11-23 버텍스 파마슈티칼스 인코포레이티드 전압 개폐 이온 채널 억제제로서의 축합 피라미딘 화합물
CA2534785A1 (en) 2003-08-12 2005-02-17 Robin Douglas Clark Tetrahydroquinazoline derivatives as cfr antagonists
KR20060072142A (ko) 2003-09-09 2006-06-27 오노 야꾸힝 고교 가부시키가이샤 Ｃｒｆ 길항제 및 이환식 복소환 화합물
US20050182061A1 (en) 2003-10-02 2005-08-18 Jeremy Green Phthalimide compounds useful as protein kinase inhibitors
CN102786482A (zh) 2003-11-21 2012-11-21 阿雷生物药品公司 Akt蛋白激酶抑制剂
US8076338B2 (en) 2004-04-23 2011-12-13 Exelixis, Inc. Kinase modulators and methods of use
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
EP1858902A1 (en) 2005-02-24 2007-11-28 Pfizer Products Incorporated Bicyclic heteroaromatic derivatives useful as anticancer agents
BRPI0609956A2 (pt) * 2005-04-28 2010-05-18 Supergen Inc inibidores de proteìna quinase
US8921376B2 (en) 2005-05-20 2014-12-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
AU2006258124B8 (en) 2005-06-10 2010-01-07 Merck Sharp & Dohme Corp. Inhibitors of Akt activity
AR054485A1 (es) 2005-06-21 2007-06-27 Cancer Rec Tech Ltd ARIL-ALQUILAMINAS Y HETEROARIL-ALQUILAMINAS COMO INHIBIDORES DE PROTEINA QUINASA A Y B, UN PROCESO PARA SU PREPARACION, COMPOSICIONES FARMACEUTICAS QUE LAS CONTIENEN Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO O PROFILAXIS DE ENFERMEDADES ORIGINADAS EN EL CRECIMIENTO ANORMAL DE LA
EA200800664A1 (ru) 2005-10-13 2009-02-27 Глаксо Груп Лимитед Производные пирролопиримидина в качестве ингибиторов syk
CA2635541A1 (en) 2005-12-28 2007-07-12 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds and their use as mineralocorticoid receptor ligands
WO2007125320A1 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
PL2049478T3 (pl) 2006-07-06 2012-09-28 Glaxo Group Ltd Podstawione N-fenylometylo 5-okso-prolino-2-amidy jako antagoniści receptora P2X7 oraz sposoby ich zastosowania
US8063050B2 (en) 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
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
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
ATE493418T1 (de) 2006-07-06 2011-01-15 Array Biopharma Inc Dihydrofuropyrimidine als akt- proteinkinaseinhibitoren
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
ES2372955T3 (es) 2006-07-06 2012-01-30 Array Biopharma, Inc. Ciclopenta[d]pirimidinas como inhibidores de la proteína cinasa akt.
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
US20100190815A1 (en) * 2006-09-08 2010-07-29 Kyowa Hakko Bio Co., Ltd. Hypertension-ameliorating agent
US7741347B2 (en) * 2007-05-17 2010-06-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8377937B2 (en) 2007-07-05 2013-02-19 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
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
WO2009089462A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors
CA2711692A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor
WO2009089459A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
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
BRPI1010795B1 (pt) * 2009-05-13 2018-12-11 Gilead Pharmasset Llc compostos antivirais, seu uso e composição farmacêutica compreendendo os mesmos

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

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