JP2011500702A - チエノピリミジンおよびピラゾロピリミジン化合物ならびにmTORキナーゼおよびPI3キナーゼ阻害剤としてのその使用 - Google Patents

チエノピリミジンおよびピラゾロピリミジン化合物ならびにmTORキナーゼおよびPI3キナーゼ阻害剤としてのその使用 Download PDF

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JP2011500702A
JP2011500702A JP2010530074A JP2010530074A JP2011500702A JP 2011500702 A JP2011500702 A JP 2011500702A JP 2010530074 A JP2010530074 A JP 2010530074A JP 2010530074 A JP2010530074 A JP 2010530074A JP 2011500702 A JP2011500702 A JP 2011500702A
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phenyl
alkyl
oxa
azabicyclo
pyrazolo
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ザスク アリー
アーロン カプラン ジョシュア
クネラ ヴェーヘイジェン ジェロエン
ジョセフ カラン ケヴィン
ジェームス リチャード デイヴィッド
アイラル−カロウスティアン セミラミス
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ワイス・エルエルシー
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JP2010530074A 2007-10-16 2008-10-15 チエノピリミジンおよびピラゾロピリミジン化合物ならびにmTORキナーゼおよびPI3キナーゼ阻害剤としてのその使用 Withdrawn JP2011500702A (ja)

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US98033207P 2007-10-16 2007-10-16
US2759508P 2008-02-11 2008-02-11
PCT/US2008/079940 WO2009052145A1 (en) 2007-10-16 2008-10-15 Thienopyrimidine and pyrazolopyrimidine compounds and their use as mtor kinase and pi3 kinase inhibitors

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JP2011500702A true JP2011500702A (ja) 2011-01-06
JP2011500702A5 JP2011500702A5 (cg-RX-API-DMAC7.html) 2011-11-24

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2015503546A (ja) * 2011-12-28 2015-02-02 サノフイ Fgf受容体(fgfr)アゴニスト二量体化合物、その製造方法及びその治療上の使用
JP2015512920A (ja) * 2012-04-10 2015-04-30 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、その調製法、中間体、組成物、及び使用
JP2015518010A (ja) * 2012-05-31 2015-06-25 上海 インスティテュート オブ マテリア メディカ、チャイニーズ アカデミー オブ サイエンシーズShanghai Institute Of Materia Medica, Chinese Academy Of Sciences ピロロ[2,1−f][1,2,4]トリアジン系化合物、その製造方法および用途
JP2022519317A (ja) * 2019-02-06 2022-03-22 ベンセラ,インコーポレイティド 局所ホスホイノシチド3-キナーゼ阻害剤

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2264819C (en) * 1996-09-04 2010-03-23 Intertrust Technologies Corp. Trusted infrastructure support systems, methods and techniques for secure electronic commerce, electronic transactions, commerce process control and automation, distributed computing, and rights management
US20030133939A1 (en) 2001-01-17 2003-07-17 Genecraft, Inc. Binding domain-immunoglobulin fusion proteins
US7754208B2 (en) 2001-01-17 2010-07-13 Trubion Pharmaceuticals, Inc. Binding domain-immunoglobulin fusion proteins
DK2298815T3 (en) 2005-07-25 2015-06-15 Emergent Product Dev Seattle B-CELL REDUCTION USING CD37 SPECIFIC AND CD20 SPECIFIC BINDING MOLECULES
CN105837690A (zh) 2006-06-12 2016-08-10 新兴产品开发西雅图有限公司 具有效应功能的单链多价结合蛋白
CA2710194C (en) 2007-12-19 2014-04-22 Amgen Inc. Inhibitors of p13 kinase
RS51975B (sr) 2008-04-11 2012-02-29 Emergent Product Development Seattle Llc. Cd37 imunoterapeutski proizvod i njegova kombinacija sa bifunkcionalnim hemoterapeutskim sredstvom
TW201004963A (en) * 2008-07-03 2010-02-01 Targacept Inc Derivatives of oxabispidine as neuronal nicotinic acetylcholine receptor ligands
WO2010014939A1 (en) * 2008-07-31 2010-02-04 Genentech, Inc. Pyrimidine compounds, compositions and methods of use
CN102224153B (zh) 2008-09-22 2014-04-30 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
TWI378933B (en) 2008-10-14 2012-12-11 Daiichi Sankyo Co Ltd Morpholinopurine derivatives
LT3106463T (lt) 2008-10-22 2018-06-25 Array Biopharma, Inc. Pakeistieji pirazolo[1,5-]pirimidino junginiai kaip trk kinazės slopikliai
EP2385832B1 (en) * 2009-01-08 2015-07-15 Curis, Inc. Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
CA2755554C (en) * 2009-04-17 2013-09-24 Wyeth Llc Pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
MX2011012520A (es) * 2009-05-27 2011-12-12 Hoffmann La Roche Compuestos inhibidores de pi3k de pirimidina biciclicos selectivos para p110 delta y metodos de uso de los mismos.
EP2445346A4 (en) * 2009-06-24 2012-12-05 Genentech Inc OXOHETEROCYCLIC FUSIONED PYRIMIDINE COMPOUNDS AND COMPOSITIONS AND METHOD FOR THEIR USE
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US20110021515A1 (en) * 2009-07-24 2011-01-27 Takeda Pharmaceutical Company Limited Dihyrofuropyrmindine compounds
KR101147550B1 (ko) * 2009-10-22 2012-05-17 한국과학기술연구원 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노[3,2-d]피리미딘 화합물
EP2499143B1 (en) 2009-11-12 2016-03-16 F.Hoffmann-La Roche Ag N7-substituted purine and pyrazolopyrimidine compounds, compositions and methods of use
JP5579864B2 (ja) * 2009-11-12 2014-08-27 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト N−9−置換プリン化合物、組成物及び使用の方法
WO2011078795A1 (en) * 2009-12-21 2011-06-30 S*Bio Pte Ltd Bridged morpholino substituted purines
WO2011090935A1 (en) * 2010-01-19 2011-07-28 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
SG183155A1 (en) 2010-02-03 2012-09-27 Signal Pharm Llc Identification of lkb1 mutation as a predictive biomarker for sensitivity to tor kinase inhibitors
JP2013523807A (ja) 2010-04-05 2013-06-17 ワイス・エルエルシー Pi3kにより誘発される癌のためのバイオマーカー
PT3205654T (pt) 2010-05-20 2019-04-22 Array Biopharma Inc Compostos macrocíclicos como inibidores de cinases trk
US9376664B2 (en) 2010-06-14 2016-06-28 The Scripps Research Institute Reprogramming of cells to a new fate
EA201390766A1 (ru) * 2010-11-24 2013-11-29 Экселиксис, Инк. БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
WO2012099581A1 (en) 2011-01-19 2012-07-26 Takeda Pharmaceutical Company Limited Dihydrofuropyrimidine compounds
CN105039520A (zh) 2011-08-03 2015-11-11 西格诺药品有限公司 作为lkb1状态的预测性生物标志物的基因表达谱的鉴定
JP5985658B2 (ja) * 2012-01-31 2016-09-06 ナンジン アルゲン ファルマ カンパニー リミテッドNanjing Allgen Pharma Co. Ltd. ブルトンチロシンキナーゼ阻害薬としての環状分子
CN103374021B (zh) * 2012-04-21 2015-10-28 通化济达医药有限公司 含有锌结合基的吡啶并嘧啶类HDAC和mTOR抑制剂
WO2013174794A1 (en) 2012-05-23 2013-11-28 F. Hoffmann-La Roche Ag Compositions and methods of obtaining and using endoderm and hepatocyte cells
EP3495367B1 (en) 2012-06-13 2020-09-30 Incyte Holdings Corporation Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
ES2744198T3 (es) 2013-04-17 2020-02-24 Signal Pharm Llc Formulaciones farmacéuticas, procesos, formas sólidas y procedimientos de uso relacionados con 1-etil-7-(2-metil-6-(1H-1,2,4-triazol-3-il)piridin-3-il)-3, 4 dihidropirazino[2,3-b]pirazin-2(1H)-ona
KR102271344B1 (ko) 2013-04-17 2021-07-01 시그날 파마소티칼 엘엘씨 디하이드로피라지노-피라진을 사용한 암의 치료
KR102240356B1 (ko) 2013-04-17 2021-04-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제와 5-치환된 퀴나졸리논 화합물을 포함하는 암 치료용 조합 요법
BR112015026021A2 (pt) 2013-04-17 2017-07-25 Signal Pharm Llc terapia de combinação compreendendo um inibidor de tor quinase e n-(3-(5-flúor-2-(4-(2-met-oxietoxi)fenilamino)pirimidin-4-ilamino)fenil)acrilamida para o tratamento de câncer
CN105377260B (zh) 2013-04-17 2020-06-12 西格诺药品有限公司 二氢吡嗪并-吡嗪类化合物在制备治疗癌症的药物中的应用
CN105392499B (zh) 2013-04-17 2018-07-24 西格诺药品有限公司 用于治疗癌症的包含tor激酶抑制剂和胞苷类似物的组合疗法
JP6382947B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ,エルエルシー 前立腺癌を治療するためのジヒドロピラジノ−ピラジン化合物及びアンドロゲン受容体アンタゴニストを含む組合せ療法
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
WO2014193912A1 (en) 2013-05-29 2014-12-04 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
EP3024456A4 (en) 2013-07-26 2017-04-12 Update Pharma Inc. Combinatorial methods to improve the therapeutic benefit of bisantrene
US9745321B2 (en) 2013-09-30 2017-08-29 Shanghai Yingli Pharmaceutical Co., Ltd Fused pyrimidine compound, intermediate, preparation method therefor, and composition and application thereof
FR3015483B1 (fr) * 2013-12-23 2016-01-01 Servier Lab Nouveaux derives de thienopyrimidine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US9763992B2 (en) 2014-02-13 2017-09-19 Father Flanagan's Boys' Home Treatment of noise induced hearing loss
WO2015160880A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
JP6663857B2 (ja) 2014-05-14 2020-03-13 ファイザー・インク ピラゾロピリジンおよびピラゾロピリミジン
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
AU2015346046B2 (en) 2014-11-16 2020-06-25 Array Biopharma, Inc. Crystalline form of (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo(1,5-a)pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
CR20170390A (es) 2015-02-20 2017-10-23 Incyte Holdings Corp Heterociclos biciclicos como inhibidores de fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
EP3352760A4 (en) 2015-09-21 2019-03-06 Aptevo Research and Development LLC CD3-BINDING POLYPEPTIDES
TN2019000271A1 (en) 2015-10-26 2021-01-07 Univ Colorado Regents Point mutations in trk inhibitor-resistant cancer and methods relating to the same
FR3046792B1 (fr) * 2016-01-19 2018-02-02 Les Laboratoires Servier Nouveaux derives d'ammonium, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
TN2018000335A1 (en) 2016-04-04 2020-01-16 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
SI3800189T1 (sl) 2016-05-18 2023-11-30 Loxo Oncology, Inc. Priprava (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo (1,5-a)pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EA202090103A1 (ru) 2017-06-22 2020-04-24 Селджин Корпорейшн Лечение гепатоцеллюлярной карциномы, которая характеризуется вирусной инфекцией гепатита b
CN111683976B (zh) 2018-02-05 2022-11-18 生物辐射实验室股份有限公司 具有阴离子交换-疏水混合模式配体的色谱树脂
CN108358949A (zh) * 2018-03-01 2018-08-03 南京法恩化学有限公司 一种2,4-二氯噻吩并[3,2-d]嘧啶的制备方法
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
US11466004B2 (en) 2018-05-04 2022-10-11 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
CN110850012B (zh) * 2018-08-21 2022-07-08 四川弘远药业有限公司 一种1-(2,3-二氯苯基)哌嗪盐酸盐及其有关物质的检测方法
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WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
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US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
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EP3800188A1 (en) 2019-10-02 2021-04-07 Bayer AG Substituted pyrazolopyrimidines as irak4 inhibitors
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WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含fgfr抑制劑及nectin-4靶向劑之組合療法
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WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Fgfr阻害剤としての三環式ヘテロ環
CN120718043A (zh) * 2024-03-28 2025-09-30 励缔(杭州)医药科技有限公司 具有mTOR抑制活性的有机化合物及其用途

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1277738B1 (en) * 2000-04-27 2011-03-30 Astellas Pharma Inc. Condensed heteroaryl derivatives

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JP2015503546A (ja) * 2011-12-28 2015-02-02 サノフイ Fgf受容体(fgfr)アゴニスト二量体化合物、その製造方法及びその治療上の使用
JP2015512920A (ja) * 2012-04-10 2015-04-30 シャンハイ インリ ファーマシューティカル カンパニー リミティド 縮合ピリミジン化合物、その調製法、中間体、組成物、及び使用
US9499561B2 (en) 2012-04-10 2016-11-22 Shanghai Yingli Pharmaceutical Co., Ltd. Fused pyrimidine compound, and preparation method, intermediate, composition, and uses thereof
JP2015518010A (ja) * 2012-05-31 2015-06-25 上海 インスティテュート オブ マテリア メディカ、チャイニーズ アカデミー オブ サイエンシーズShanghai Institute Of Materia Medica, Chinese Academy Of Sciences ピロロ[2,1−f][1,2,4]トリアジン系化合物、その製造方法および用途
JP2022519317A (ja) * 2019-02-06 2022-03-22 ベンセラ,インコーポレイティド 局所ホスホイノシチド3-キナーゼ阻害剤

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