KR101624752B1 - Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 - Google Patents

Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 Download PDF

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KR101624752B1
KR101624752B1 KR1020107017573A KR20107017573A KR101624752B1 KR 101624752 B1 KR101624752 B1 KR 101624752B1 KR 1020107017573 A KR1020107017573 A KR 1020107017573A KR 20107017573 A KR20107017573 A KR 20107017573A KR 101624752 B1 KR101624752 B1 KR 101624752B1
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mmol
compound
compounds
akt
tert
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KR20100103865A (ko
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요셉 벤크식
제임스 에프. 블레이크
니콜라스 씨. 칼란
이안 에스. 미첼
케이트 엘. 스펜서
뎅밍 시아오
루이 슈
크리스틴 샤봇
스티븐 도
준 리앙
브라이언 사피나
비롱 장
제임스 그레이햄
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어레이 바이오파마 인크.
제넨테크, 인크.
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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
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KR1020107017573A 2008-01-09 2009-01-09 Akt 단백질 키나제 저해물질로써의 수산화된 피리미딜 시클로펜탄 Expired - Fee Related KR101624752B1 (ko)

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US2008708P 2008-01-09 2008-01-09
US61/020,087 2008-01-09

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Publication Number Publication Date
KR20100103865A KR20100103865A (ko) 2010-09-28
KR101624752B1 true KR101624752B1 (ko) 2016-05-26

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US (1) US8853216B2 (enExample)
EP (1) EP2240455B1 (enExample)
JP (1) JP5539225B2 (enExample)
KR (1) KR101624752B1 (enExample)
CN (1) CN101932565B (enExample)
AU (1) AU2009204019B2 (enExample)
BR (1) BRPI0907372A2 (enExample)
CA (1) CA2711692A1 (enExample)
CO (1) CO6280510A2 (enExample)
CR (1) CR11591A (enExample)
EC (1) ECSP10010392A (enExample)
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IL (1) IL206607A0 (enExample)
MA (1) MA32343B1 (enExample)
MX (1) MX2010007546A (enExample)
NZ (1) NZ586720A (enExample)
RU (1) RU2520735C2 (enExample)
UA (1) UA100544C2 (enExample)
WO (1) WO2009089453A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
BRPI0813999A2 (pt) * 2007-07-05 2019-10-01 Array Biopharma Inc ciclopentanos de pirimidil como inibidores de akt proteína cinase
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
JP5608097B2 (ja) 2008-01-08 2014-10-15 アレイ バイオファーマ、インコーポレイテッド キナーゼ阻害薬としてのピロロピリジン
EP2250155B1 (en) 2008-01-09 2013-07-03 Array Biopharma, Inc. 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors
US8372842B2 (en) 2008-01-09 2013-02-12 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
KR102123131B1 (ko) * 2012-05-17 2020-06-15 제넨테크, 인크. 하이드록실화 사이클로펜타피리미딘 화합물 및 이의 염의 제조 방법
CN105899492B (zh) * 2013-11-15 2021-08-24 豪夫迈·罗氏有限公司 用于制备嘧啶基环戊烷化合物的方法
US10722484B2 (en) 2016-03-09 2020-07-28 K-Gen, Inc. Methods of cancer treatment

Family Cites Families (87)

* 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
DK0664291T3 (da) * 1992-10-05 2000-10-30 Ube Industries Pyrimidinforbindelse
US5750545A (en) * 1993-07-23 1998-05-12 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
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
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
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
JP2002509536A (ja) 1997-07-01 2002-03-26 ワーナー−ランバート・カンパニー 2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用
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
EP1140067A1 (en) 1999-01-07 2001-10-10 Warner-Lambert Company Antiviral method using mek inhibitors
CA2350234A1 (en) 1999-01-07 2000-07-13 Alexander James Bridges Treatment of asthma with 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
AP2001002225A0 (en) * 1999-01-13 2001-09-30 Warner Lambert Co 1-heterocycle substituted diarylamines.
EP1144371B1 (en) 1999-01-13 2005-11-09 Warner-Lambert Company Llc Benzenesulphonamide derivatives and their use as mek inhibitors
ATE311363T1 (de) * 1999-01-13 2005-12-15 Warner Lambert Co Sulfohydroxamsäure and sulfohydroxamate und ihre verwendung als mek-inhibitoren
BR9916857A (pt) 1999-01-13 2001-12-04 Warner Lambert Co 4 heteroaril diarilaminas
IL144214A0 (en) * 1999-01-13 2002-05-23 Warner Lambert Co Benzoheterocycles and their use as mek inhibitors
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
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
JP2003504401A (ja) 1999-07-16 2003-02-04 ワーナー−ランバート・カンパニー Mek阻害剤を用いる慢性疼痛の治療方法
HUP0202381A3 (en) 1999-07-16 2004-12-28 Warner Lambert Co Method for treating chronic pain using mek inhibitors
AU5786000A (en) 1999-07-16 2001-02-05 Warner-Lambert Company Method for treating chronic pain using mek inhibitors
BR0109188A (pt) 2000-03-15 2003-03-18 Warner Lambert Co Diarilaminas 5-amida substituìdas como inibidores de mex
IL153817A0 (en) 2000-07-19 2003-07-31 Warner Lambert Co Oxygenated esters of 4-iodo 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.
AU2002210714A1 (en) 2000-11-02 2002-06-11 Astrazeneca Ab Substituted quinolines as antitumor agents
WO2002083139A1 (en) 2001-04-10 2002-10-24 Merck & Co., Inc. Inhibitors of akt activity
DE60225127T2 (de) * 2001-04-30 2009-02-19 Glaxo Group Ltd., Greenford Kondensierte pyrimidine als antagonisten des 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
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
US7235537B2 (en) * 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
CA2478534A1 (en) 2002-03-13 2003-09-25 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as mek inhibitors
CA2478374C (en) * 2002-03-13 2009-01-06 Eli M. Wallace N3 alkylated benzimidazole derivatives as mek inhibitors
WO2003086403A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
US7273869B2 (en) 2002-04-08 2007-09-25 Merck & Co., Inc. Inhibitors of Akt activity
WO2003086279A2 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
WO2003086394A1 (en) 2002-04-08 2003-10-23 Merck & Co., Inc. Inhibitors of akt activity
MXPA04011093A (es) * 2002-05-10 2005-02-14 Neurocrine Biosciences Inc Piperazina sustituida como ligandos de receptores de melanocortina.
US7399764B2 (en) 2002-10-30 2008-07-15 Merck & Co., Inc. Inhibitors of Akt activity
US20040102360A1 (en) * 2002-10-30 2004-05-27 Barnett Stanley F. Combination therapy
US20040099681A1 (en) * 2002-11-21 2004-05-27 Nice-Pak Products, Inc. Non-planar dispenser for articles
GB0308208D0 (en) * 2003-04-09 2003-05-14 Glaxo Group Ltd Chemical compounds
US7638530B2 (en) 2003-04-24 2009-12-29 Merck & Co., Inc. Inhibitors of Akt activity
ATE440825T1 (de) * 2003-06-06 2009-09-15 Vertex Pharma Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern
AR045445A1 (es) 2003-08-05 2005-10-26 Vertex Pharma Compuestos ihinibidores de canales ionicos regulados por voltaje
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
BRPI0414238A (pt) * 2003-09-09 2006-10-31 Ono Pharmaceutical Co antagonistas de crf e compostos heterobicìclicos
WO2005039564A1 (en) * 2003-10-02 2005-05-06 Vertex Pharmaceuticals Incorporated Phthalimide compounds useful as protein kinase inhibitors
BRPI0416852A (pt) * 2003-11-21 2007-02-27 Array Biopharma Inc inibidores da quinase akt
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
TW200621257A (en) 2004-10-20 2006-07-01 Astellas Pharma Inc Pyrimidine derivative fused with nonaromatic ring
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
US7994172B2 (en) * 2004-12-28 2011-08-09 Exelixis, Inc. [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
EP1858902A1 (en) 2005-02-24 2007-11-28 Pfizer Products Incorporated Bicyclic heteroaromatic derivatives useful as anticancer agents
RU2435769C2 (ru) * 2005-05-20 2011-12-10 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиридины, полезные в качестве ингибиторов протеинкиназы
UY29610A1 (es) 2005-06-21 2007-01-31 Cancer Rec Tech Ltd Aril-alquilaminas y heteroaril-alquilaminas como inhibidores de la quinasa proteínica
US20080004295A1 (en) 2005-10-13 2008-01-03 Gore Paul M Novel compounds
JP2009523701A (ja) 2005-12-28 2009-06-25 武田薬品工業株式会社 縮合複素環化合物およびその用途
EP2013206A1 (en) 2006-04-25 2009-01-14 Astex Therapeutics Limited Pharmaceutical compounds
KR20090024834A (ko) 2006-07-05 2009-03-09 인터뮨, 인크. C형 간염 바이러스 복제의 신규 억제제
WO2008006025A1 (en) * 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrofuro pyrimidines as akt protein kinase inhibitors
SI2049478T1 (sl) 2006-07-06 2012-08-31 Glaxo Group Ltd Substituirani N-fenilmetil-5-okso-prolin-2-amidi kot antagonisti receptorja P2X7 in postopki za njihovo uporabo
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
US7910747B2 (en) 2006-07-06 2011-03-22 Bristol-Myers Squibb Company Phosphonate and phosphinate pyrazolylamide glucokinase activators
TW200808325A (en) 2006-07-06 2008-02-16 Astrazeneca Ab Novel compounds
PL2049500T3 (pl) * 2006-07-06 2012-02-29 Array Biopharma Inc Cyklopenta[d]pirymidyny jako inhibitory kinaz białkowych AKT
GB0613518D0 (en) 2006-07-06 2006-08-16 Phytopharm Plc Chemical compounds
WO2008006039A1 (en) * 2006-07-06 2008-01-10 Array Biopharma Inc. Dihydrothieno pyrimidines as akt protein kinase inhibitors
US8063050B2 (en) * 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
AR061974A1 (es) 2006-07-14 2008-08-10 Novartis Ag Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion
WO2008012635A2 (en) 2006-07-26 2008-01-31 Pfizer Products Inc. Amine derivatives useful as anticancer agents
BRPI0813999A2 (pt) * 2007-07-05 2019-10-01 Array Biopharma Inc ciclopentanos de pirimidil como inibidores de akt proteína cinase
EP2404907B1 (en) 2007-07-05 2015-01-14 Array Biopharma, Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors

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US20100292244A1 (en) 2010-11-18
AU2009204019B2 (en) 2014-02-20
MA32343B1 (fr) 2011-06-01
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ES2401685T8 (es) 2014-11-06
RU2520735C2 (ru) 2014-06-27
UA100544C2 (ru) 2013-01-10
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ECSP10010392A (es) 2010-09-30
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US8853216B2 (en) 2014-10-07
JP2011509306A (ja) 2011-03-24
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NZ586720A (en) 2012-11-30
MX2010007546A (es) 2010-09-30
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