JP2008525526A5 - - Google Patents

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JP2008525526A5
JP2008525526A5 JP2007549530A JP2007549530A JP2008525526A5 JP 2008525526 A5 JP2008525526 A5 JP 2008525526A5 JP 2007549530 A JP2007549530 A JP 2007549530A JP 2007549530 A JP2007549530 A JP 2007549530A JP 2008525526 A5 JP2008525526 A5 JP 2008525526A5
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JP5274842B2 (ja
JP2008525526A (ja
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Priority claimed from PCT/US2005/046938 external-priority patent/WO2006071819A1/en
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JP2007549530A 2004-12-28 2005-12-27 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター(p70S6K、Akt−1およびAkt−2)としての[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジンまたは[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジン化合物 Expired - Fee Related JP5274842B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US64020004P 2004-12-28 2004-12-28
US60/640,200 2004-12-28
PCT/US2005/046938 WO2006071819A1 (en) 2004-12-28 2005-12-27 [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

Publications (3)

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JP2008525526A JP2008525526A (ja) 2008-07-17
JP2008525526A5 true JP2008525526A5 (https=) 2009-03-05
JP5274842B2 JP5274842B2 (ja) 2013-08-28

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JP2007549530A Expired - Fee Related JP5274842B2 (ja) 2004-12-28 2005-12-27 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター(p70S6K、Akt−1およびAkt−2)としての[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジンまたは[1H−ピペラゾ[3,4−d]ピリミジン−4−イル]−ピペラジン化合物

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US (1) US7994172B2 (https=)
EP (1) EP1848719B1 (https=)
JP (1) JP5274842B2 (https=)
AT (1) ATE543821T1 (https=)
AU (1) AU2005322085B2 (https=)
CA (1) CA2590961C (https=)
WO (1) WO2006071819A1 (https=)

Families Citing this family (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0418078A8 (pt) 2003-12-23 2018-01-02 Astex Therapeutics Ltd composto ou um seu sal, solvato, tautômero ou n-óxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune em um mamífero e para induzir apoptose em uma célula cancerosa, composição farmacêutica, e, processo para a preparação de um composto
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
EP1902032A1 (en) 2005-06-22 2008-03-26 Astex Therapeutics Limited Pharmaceutical compounds
JP5345842B2 (ja) 2005-06-23 2013-11-20 アステックス・セラピューティクス・リミテッド プロテインキナーゼモジュレーターとしてのピラゾール誘導体を含む医薬組み合わせ
EP2029592A1 (en) * 2006-04-25 2009-03-04 Astex Therapeutics Limited Pharmaceutical compounds
WO2007125321A2 (en) * 2006-04-25 2007-11-08 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
US8063050B2 (en) * 2006-07-06 2011-11-22 Array Biopharma Inc. Hydroxylated and methoxylated pyrimidyl cyclopentanes as AKT protein kinase inhibitors
US8329701B2 (en) 2006-07-06 2012-12-11 Array Biopharma Inc. Dihydrofuro pyrimidines as AKT protein kinase inhibitors
EP2049500B1 (en) * 2006-07-06 2011-09-07 Array Biopharma, Inc. Cyclopenta [d] pyrimidines as akt protein kinase inhibitors
ATE532789T1 (de) 2006-07-06 2011-11-15 Array Biopharma Inc Dihydrothienopyrimidine als akt-proteinkinase- inhibitoren
WO2008061108A2 (en) 2006-11-15 2008-05-22 Forest Laboratories Holdings Limited Phthalazine derivatives
AR064415A1 (es) * 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de pirrolo-piperidinas y purinas,composiciones farmaceuticas que los contienen y usos en trastornos y/o enfermedades mediadas por pka y pkb.
CA2678577A1 (en) * 2007-02-26 2008-09-04 Vitae Pharmaceuticals, Inc. Cyclic urea and carbamate inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
GB0704932D0 (en) 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
UA99284C2 (ru) 2007-05-11 2012-08-10 Елі Ліллі Енд Компані ИНГИБИТОРЫ р70 S6-КИНАЗЫ
US9409886B2 (en) 2007-07-05 2016-08-09 Array Biopharma Inc. Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
CN101918373B (zh) * 2007-07-05 2013-06-05 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
US8846683B2 (en) 2007-07-05 2014-09-30 Array Biopharma, Inc. Pyrimidyl cyclopentanes as Akt protein kinase inhibitors
CN103396409B (zh) 2007-07-05 2015-03-11 阵列生物制药公司 作为akt蛋白激酶抑制剂的嘧啶基环戊烷
EP2183228B1 (en) * 2007-07-26 2014-08-20 Vitae Pharmaceuticals, Inc. CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1
EP2050748A1 (en) * 2007-10-18 2009-04-22 Bayer Schering Pharma Aktiengesellschaft Novel fused pyrimidines
PT2188291E (pt) * 2007-08-14 2012-12-20 Bayer Ip Gmbh Pirimidinas bicíclicas fundidas
PL2201012T3 (pl) 2007-10-11 2014-11-28 Astrazeneca Ab Pochodne pirolo[2,3-d]pirymidyny jako inhibitory kinazy białkowej b
AR069207A1 (es) * 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
CA2708303A1 (en) 2007-12-11 2009-06-18 Vitae Pharmaceuticals, Inc. Cyclic urea inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
TW200934490A (en) * 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
US8841304B2 (en) 2008-01-08 2014-09-23 Array Biopharma, Inc. Pyrrolopyridines as kinase inhibitors
CN101965347B (zh) 2008-01-09 2013-01-02 阵列生物制药公司 作为激酶抑制剂的吡唑并吡啶
US8853216B2 (en) 2008-01-09 2014-10-07 Array Biopharma, Inc. Hydroxylated pyrimidyl cyclopentane as AKT protein kinase inhibitor
NZ586346A (en) 2008-01-09 2012-02-24 Array Biopharma Inc Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors
CA2711782C (en) * 2008-01-09 2017-01-03 Array Biopharma Inc. 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors
WO2009094169A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
ES2494365T3 (es) * 2008-01-30 2014-09-15 Genentech, Inc. Compuestos de pirazolopirimidina que inhiben PI3K y métodos de uso
JP5734666B2 (ja) * 2008-02-11 2015-06-17 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1の1,3−オキサアゼパン−2−オン及び1,3−ジアゼパン−2−オン阻害剤
US8598160B2 (en) * 2008-02-15 2013-12-03 Vitae Pharmaceuticals, Inc. Cycloalkyl lactame derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1
JP5538356B2 (ja) * 2008-03-18 2014-07-02 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1型の阻害剤
WO2009134387A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CL2009001059A1 (es) * 2008-05-01 2010-11-12 Boehringer Ingelheim Int Compuestos derivados de 1,3-oxazin-2-ona-3,6 sustituidos, inhibidores de la actividad de la 11-beta-hidroxiesteroide deshidrogenasa i; composicion farmaceutica que los comprende; utiles en el tratamiento de enfermedades tales como diabetes mellitus, entre otras.
CA2723032A1 (en) * 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
AR071236A1 (es) 2008-05-01 2010-06-02 Vitae Pharmaceuticals Inc Inhibidores ciclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
WO2010011314A1 (en) 2008-07-25 2010-01-28 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11 beta-hydroxysteroid dehydrogenase 1
US8846668B2 (en) 2008-07-25 2014-09-30 Vitae Pharmaceuticals, Inc. Inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2743242A1 (en) * 2008-11-11 2010-05-20 Eli Lilly And Company P70 s6 kinase inhibitor and mtor inhibitor combination therapy
AR074072A1 (es) 2008-11-11 2010-12-22 Lilly Co Eli Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme
US8334293B2 (en) 2008-11-11 2012-12-18 Eli Lilly And Company P70 S6 kinase inhibitor and EGFR inhibitor combination therapy
US8653098B2 (en) 2008-11-20 2014-02-18 Genentech, Inc. Pyrazolopyridine PI3K inhibitor compounds and methods of use
CA2744946A1 (en) 2009-02-04 2010-08-12 Boehringer Ingelheim International Gmbh Cyclic inhibitors of 11.beta.-hydroxysteroid dehydrogenase 1
NZ595087A (en) 2009-02-11 2013-03-28 Merck Patent Gmbh Novel amino azaheterocyclic carboxamides
TW201039034A (en) * 2009-04-27 2010-11-01 Chunghwa Picture Tubes Ltd Pixel structure and the method of forming the same
KR20120061771A (ko) * 2009-04-30 2012-06-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
UA109255C2 (ru) 2009-04-30 2015-08-10 Берінгер Інгельхайм Інтернешнл Гмбх Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1
EP2440537A1 (en) 2009-06-11 2012-04-18 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
WO2011002910A1 (en) 2009-07-01 2011-01-06 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CN102471338B (zh) 2009-08-07 2014-07-02 默克专利有限公司 氮杂杂环化合物
PT2473049T (pt) 2009-09-04 2019-03-04 Sunesis Pharmaceuticals Inc Inibidores de tirosina quinase de bruton
MX2012004780A (es) 2009-10-23 2012-08-23 Lilly Co Eli Inhibidores de akt.
US8933072B2 (en) 2010-06-16 2015-01-13 Vitae Pharmaceuticals, Inc. Substituted 5-,6- and 7-membered heterocycles, medicaments containing such compounds, and their use
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための11−β−HSD1のインヒビターとしてのアザスピロヘキサノン
US9586938B2 (en) 2010-07-29 2017-03-07 Merck Patent Gmbh Cyclic amine azaheterocyclic carboxamides
UA110113C2 (xx) 2010-07-29 2015-11-25 Біциклічні азагетероциклічні карбоксаміди
PH12013500808A1 (en) 2010-11-02 2015-10-07 Boehringer Ingelheim Int Pharmaceutical combinations for the treatment of metabolic disorders
PT2643313T (pt) 2010-11-24 2016-10-11 Merck Patent Gmbh Quinazolina carboxamida azetidinas
KR102021157B1 (ko) 2011-04-01 2019-09-11 제넨테크, 인크. Akt 억제제 화합물 및 아비라테론의 조합물, 및 사용 방법
TR201815685T4 (tr) 2011-04-01 2018-11-21 Genentech Inc Kanser tedavisi için akt ve mek inhibe edici bileşiklerin kombinasyonları.
EP2694056B1 (en) 2011-04-01 2019-10-16 AstraZeneca AB Therapeutic treatment
MX346095B (es) 2011-09-12 2017-03-07 Merck Patent Gmbh Nuevas imidazol-aminas como moduladores de la actividad de cinasas.
CN103930407B (zh) * 2011-09-12 2019-02-26 默克专利有限公司 用作激酶活性调节剂的氨基嘧啶衍生物
PH12014500943A1 (en) 2011-11-30 2014-06-30 Astrazeneca Ab Combination treatment of cancer
SG11201402387WA (en) 2011-12-22 2014-09-26 Merck Patent Gmbh Novel heterocyclic carboxamides as modulators of kinase activity
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
AR091273A1 (es) 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
MX2015002887A (es) * 2012-09-06 2015-07-06 Plexxikon Inc Compuestos y metodos para la modulacion de cinasas, e indicaciones para ello.
WO2014062774A1 (en) * 2012-10-17 2014-04-24 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
AR093511A1 (es) 2012-11-16 2015-06-10 Merck Patent Gmbh Derivados de imidazol-piperidinilo como moduladores de la actividad de cinasas
CA2890288A1 (en) 2012-11-16 2014-05-22 Merck Patent Gmbh Novel heterocyclic derivatives as modulators of kinase activity
US9771330B2 (en) 2012-11-27 2017-09-26 The University Of North Carolina At Chapel Hill Pyrimidine compounds for the treatment of cancer
SG10201800741QA (en) 2012-11-29 2018-03-28 Merck Patent Gmbh BENZO-[d][1,2,3]TRIAZINE COMPOUNDS AND USE AS p70S6K INHIBITORS
USRE48622E1 (en) 2012-12-20 2021-07-06 UCB Biopharma SRL Therapeutically active pyrazolo-pyrimidine derivatives
SG11201504291SA (en) * 2012-12-20 2015-07-30 Ucb Biopharma Sprl Therapeutically active pyrazolo-pyrimidine derivatives
SG11201505999VA (en) 2013-03-11 2015-08-28 Merck Patent Gmbh 6-[4-(1 h-imidazol-2-yl)piperidin-1 -yl]pyrimidin-4-amine derivatives as modulators of kinase activity
CA2944573C (en) 2014-04-03 2022-10-25 Merck Patent Gmbh Combinations of cancer therapeutics
US20150291606A1 (en) 2014-04-11 2015-10-15 The University Of North Carolina At Chapel Hill Mertk-specific pyrrolopyrimidine compounds
US10709708B2 (en) 2016-03-17 2020-07-14 The University Of North Carolina At Chapel Hill Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor
JP7214632B2 (ja) 2016-07-21 2023-01-30 バイオジェン エムエー インク. ブルトン型チロシンキナーゼ阻害剤のコハク酸塩形態および組成物
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
CA3092677A1 (en) * 2018-03-06 2019-09-12 Icahn School Of Medicine At Mount Sinai Serine threonine kinase (akt) degradation / disruption compounds and methods of use
CN110396067B (zh) * 2018-04-25 2022-07-08 复旦大学 1,4-二取代-2-哌嗪酮类化合物及其药物用途
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
CN118908962A (zh) 2019-05-06 2024-11-08 西奈山伊坎医学院 作为hpk1的降解剂的异双功能化合物
GB201918815D0 (en) * 2019-12-19 2020-02-05 Imperial College Innovations Ltd Treatment of cancer
TWI908780B (zh) * 2020-03-17 2025-12-21 大陸商江蘇恆瑞醫藥股份有限公司 稠合二環類衍生物、其製備方法及其在醫藥上的應用
CN113444110B (zh) * 2020-03-25 2023-05-12 江苏恒瑞医药股份有限公司 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用
WO2021216548A1 (en) * 2020-04-21 2021-10-28 University Of Massachusetts Methods and compositions for treatment of age-related macular degeneration
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
WO2022101459A1 (en) 2020-11-16 2022-05-19 Merck Patent Gmbh Kinase inhibitor combinations for cancer treatment
CN117940410A (zh) 2021-09-17 2024-04-26 江苏恒瑞医药股份有限公司 一种稠合二环类衍生物的可药用盐、晶型及其制备方法
CN117122602B (zh) * 2023-09-26 2026-03-20 赣南创新与转化医学研究院 化合物在制备治疗和/或预防脂肪肝病及相关疾病的药物中的用途

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69943144D1 (de) * 1998-03-31 2011-03-03 Kyowa Hakko Kirin Co Ltd Stickstoffenthaltende heterocyclische verbindungen
JP2003252871A (ja) * 2001-03-29 2003-09-10 Tanabe Seiyaku Co Ltd スピロイソキノリン誘導体、その製法およびその合成中間体
JP2004115450A (ja) * 2002-09-27 2004-04-15 Tanabe Seiyaku Co Ltd 医薬組成物
ES2304252T3 (es) * 2003-05-28 2008-10-01 Universita Degli Studi Di Siena Derivados sustituidos en posicion 4 de pirazolo(3,4-d)pirimidina y utilizaciones de los mismos.
CA2546754A1 (en) 2003-11-21 2005-06-09 Array Biopharma Inc. Akt protein kinase inhibitors
KR100843526B1 (ko) 2004-02-27 2008-07-03 에프. 호프만-라 로슈 아게 피라졸의 접합 유도체
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use

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