JP2013510125A5 - - Google Patents

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JP2013510125A5
JP2013510125A5 JP2012537383A JP2012537383A JP2013510125A5 JP 2013510125 A5 JP2013510125 A5 JP 2013510125A5 JP 2012537383 A JP2012537383 A JP 2012537383A JP 2012537383 A JP2012537383 A JP 2012537383A JP 2013510125 A5 JP2013510125 A5 JP 2013510125A5
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alkyl
compound
salt
heteroaromatic
alkoxy
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JP5819840B2 (ja
JP2013510125A (ja
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JP2012537383A 2009-11-05 2010-11-03 ブロモドメイン阻害剤としてのテトラヒドロキノリン誘導体 Expired - Fee Related JP5819840B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0919434.1 2009-11-05
GBGB0919434.1A GB0919434D0 (en) 2009-11-05 2009-11-05 Novel compounds
PCT/EP2010/066701 WO2011054848A1 (en) 2009-11-05 2010-11-03 Thetrahydroquinolines derivatives as bromodomain inhibitors

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JP2013510125A JP2013510125A (ja) 2013-03-21
JP2013510125A5 true JP2013510125A5 (enExample) 2013-11-14
JP5819840B2 JP5819840B2 (ja) 2015-11-24

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JP2012537383A Expired - Fee Related JP5819840B2 (ja) 2009-11-05 2010-11-03 ブロモドメイン阻害剤としてのテトラヒドロキノリン誘導体

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US (1) US8580957B2 (enExample)
EP (1) EP2496558B1 (enExample)
JP (1) JP5819840B2 (enExample)
ES (1) ES2573706T3 (enExample)
GB (1) GB0919434D0 (enExample)
WO (1) WO2011054848A1 (enExample)

Families Citing this family (111)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0919431D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
MX373121B (es) 2010-05-14 2020-04-30 Dana Farber Cancer Inst Inc Composiciones y metodos para el tratamiento de leucemia.
US8981083B2 (en) 2010-05-14 2015-03-17 Dana Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
CA2799381A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Male contraceptive compositions and methods of use
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
US9249161B2 (en) 2010-12-02 2016-02-02 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
US9328117B2 (en) 2011-06-17 2016-05-03 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
GB201114103D0 (en) * 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033269A1 (en) * 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
CA2870931A1 (en) 2012-04-20 2013-10-24 Abbvie Inc. Isoindolone derivatives
US9624244B2 (en) 2012-06-06 2017-04-18 Constellation Pharmaceuticals, Inc. Benzo [B] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
AU2012382373A1 (en) 2012-06-12 2014-12-11 Abbvie Inc. Pyridinone and pyridazinone derivatives
US9763956B2 (en) 2012-06-19 2017-09-19 The Broad Institute, Inc. Diagnostic and treatment methods in subjects having or at risk of developing resistance to cancer therapy
WO2014096965A2 (en) 2012-12-21 2014-06-26 Rvx Therapeutics Inc. Novel heterocyclic compounds as bromodomain inhibitors
EP2970312B1 (en) 2013-03-11 2017-11-15 The Regents of The University of Michigan Bet bromodomain inhibitors and therapeutic methods using the same
WO2014140076A1 (en) * 2013-03-14 2014-09-18 Glaxosmithkline Intellectual Property (No.2) Limited 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
US9714946B2 (en) 2013-03-14 2017-07-25 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
KR20150128842A (ko) 2013-03-14 2015-11-18 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 브로모도메인 억제제로서의 퓨로피리딘
CN105407894A (zh) 2013-03-14 2016-03-16 康威基内有限公司 用于抑制含布罗莫结构域的蛋白质的方法和组合物
MX366703B (es) 2013-03-15 2019-07-22 Incyte Holdings Corp Heterociclos tricíclicos como inhibidores de la proteína bet.
CA2901083A1 (en) 2013-04-26 2014-10-30 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
WO2014206150A1 (en) 2013-06-28 2014-12-31 Abbvie Inc. Bromodomain inhibitors
WO2015006193A1 (en) 2013-07-08 2015-01-15 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
AU2014337064B2 (en) 2013-10-18 2019-03-14 Celgene Quanticel Research, Inc. Bromodomain inhibitors
KR20160072261A (ko) 2013-11-08 2016-06-22 다나-파버 캔서 인스티튜트 인크. 브로모도메인 및 엑스트라-말단 (bet) 단백질 저해제를 이용한 암 치료를 위한 조합 요법
WO2015074064A2 (en) * 2013-11-18 2015-05-21 Bair Kenneth W Tetrahydroquinoline compositions as bet bromodomain inhibitors
US9422281B2 (en) 2013-11-18 2016-08-23 Forma Therapeutics, Inc. Benzopiperazine compositions as BET bromodomain inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9108953B2 (en) * 2013-11-26 2015-08-18 Gilead Sciences, Inc. Quinoline derivatives as bromodomain inhibitors
WO2015081203A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
LT3092227T (lt) 2014-01-09 2018-08-10 Orion Corporation Bicikliniai heterocikliniai dariniai kaip bromodomeno inhibitoriai
EA038715B1 (ru) * 2014-01-24 2021-10-08 Селджен Квонтисел Рисёрч, Инк. Ингибиторы бромодомена
KR20160111036A (ko) 2014-01-31 2016-09-23 다나-파버 캔서 인스티튜트 인크. 디아제판 유도체 및 그의 용도
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
US9580430B2 (en) 2014-02-28 2017-02-28 The Regents Of The University Of Michigan 9H-pyrimido[4,5-B]indoles and related analogs as BET bromodomain inhibitors
RU2722179C2 (ru) 2014-02-28 2020-05-28 Тэнша Терапеутикс, Инк. Лечение состояний, ассоциированных с гиперинсулинемией
UA119870C2 (uk) 2014-04-23 2019-08-27 Інсайт Корпорейшн 1H-ПІРОЛО[2,3-c]ПІРИДИН-7(6H)-ОНИ ТА ПІРАЗОЛО[3,4-c]ПІРИДИН-7(6H)-ОНИ ЯК ІНГІБІТОРИ БІЛКІВ BET
CN106687463B (zh) 2014-06-20 2019-04-09 星座制药公司 一种乙酰胺类化合物的晶型
WO2016022970A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
EP3177626A4 (en) 2014-08-08 2017-12-27 Dana Farber Cancer Institute, Inc. Diazepane derivatives and uses thereof
MX373845B (es) 2014-09-12 2020-03-26 Glaxosmithkline Ip No 2 Ltd Derivados de tetrahidroquinolina como inhibidores de bromodominio.
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
UA122130C2 (uk) 2014-10-27 2020-09-25 Тенша Терапеутікс, Інк. Інгібітори бромодомену
EP3227280B1 (en) 2014-12-01 2019-04-24 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
JP2017537946A (ja) 2014-12-11 2017-12-21 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての置換複素環
HK1245247A1 (zh) 2014-12-17 2018-08-24 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
WO2016138332A1 (en) 2015-02-27 2016-09-01 The Regents Of The University Of Michigan 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors
GB201503720D0 (en) 2015-03-05 2015-04-22 Glaxosmithkline Ip No 2 Ltd Chemical compound
GB201504689D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Chemical compounds
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
TW201642860A (zh) * 2015-04-22 2016-12-16 塞爾基因定量細胞研究公司 布羅莫結構域抑制劑
US10702517B2 (en) 2015-04-22 2020-07-07 Celgene Quanticel Research, Inc. Bromodomain inhibitor
WO2016196065A1 (en) 2015-05-29 2016-12-08 Genentech, Inc. Methods and compositions for assessing responsiveness of cancers to bet inhibitors
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
AU2016283020A1 (en) 2015-06-26 2018-01-04 Tensha Therapeutics, Inc. Treatment of nut midline carcinoma
PE20181088A1 (es) 2015-08-10 2018-07-09 Dana Farber Cancer Inst Inc Mecanismo de resistencia a inhibidores de bromodominio bet
HK1249504A1 (zh) 2015-09-02 2018-11-02 Glaxosmithkline Intellectual Property (No. 2) Limited 用作溴结构域抑制剂的吡啶酮二甲酰胺
US11306105B2 (en) 2015-09-11 2022-04-19 Dana-Farber Cancer Institute, Inc. Cyano thienotriazolodiazepines and uses thereof
JP2018526424A (ja) 2015-09-11 2018-09-13 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド アセトアミドチエノトリアゾロジアゼピンおよびこれらの使用
AU2016326864A1 (en) 2015-09-22 2018-03-22 Glaxosmithkline Intellectual Property (No.2) Limited Pyridinone dicarboxamide for use as bromodomain inhibitors
JP6832923B2 (ja) 2015-10-05 2021-02-24 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としての2−オキソ−1,2−ジヒドロピリジン−3,5−ジカルボキサミド化合物
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
CR20180336A (es) 2015-11-25 2018-08-06 Dana Farber Cancer Inst Inc Inhibidores de bromodominio bivalentes y usos de los mismos
ES2882066T3 (es) 2016-02-15 2021-12-01 Univ Michigan Regents 1,4-oxazepinas fusionadas y análogos relacionados como inhibidores de bromodominio BET
CN113788818A (zh) 2016-04-06 2021-12-14 密执安大学评议会 Mdm2蛋白质降解剂
AU2017246453A1 (en) 2016-04-06 2018-11-08 The Regents Of The University Of Michigan Monofunctional intermediates for ligand-dependent target protein degradation
KR20180132680A (ko) 2016-04-07 2018-12-12 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 브로모도메인 억제제로서 벤조[b]푸란
JP6954921B2 (ja) 2016-04-07 2021-10-27 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としてのピリジル誘導体
BR112018070859A2 (pt) 2016-04-12 2019-02-05 Univ Michigan Regents degradantes da proteína de bet
RS60302B1 (sr) 2016-04-15 2020-07-31 Abbvie Inc Inhibitori bromodomena
JP7160688B2 (ja) * 2016-05-24 2022-10-25 ジェネンテック, インコーポレイテッド Cbp/ep300の複素環式インヒビターおよびがんの処置におけるそれらの使用
AU2017269673A1 (en) 2016-05-24 2018-11-22 Glaxosmithkline Intellectual Property (No.2) Limited Pyridine dicarboxamide derivatives as bromodomain inhibitors
AU2017281286B2 (en) 2016-06-20 2021-05-20 Incyte Corporation Crystalline solid forms of a bet inhibitor
GB201614934D0 (en) 2016-09-02 2016-10-19 Glaxosmithkline Intellectual Property (No 2) Ltd Chemical compounds
GB201614939D0 (en) 2016-09-02 2016-10-19 Glaxosmithkline Ip Dev Ltd Crystalline hydrate
GB201614940D0 (en) 2016-09-02 2016-10-19 Glaxosmithkline Intellectual Property (No 2) Ltd Chemical compounds
CN110062759B (zh) 2016-09-13 2022-05-24 密执安大学评议会 作为bet蛋白降解剂的稠合的1,4-氧氮杂䓬
US10975093B2 (en) 2016-09-13 2021-04-13 The Regents Of The University Of Michigan Fused 1,4-diazepines as BET protein degraders
EP3528810A4 (en) * 2016-10-20 2020-06-17 Celgene Quanticel Research, Inc. BROMDOMAIN INHIBITOR
WO2018111805A1 (en) * 2016-12-13 2018-06-21 St. Jude Children's Research Hospital Tetrahydroquinoline-based bromodomain inhibitors
WO2018144789A1 (en) 2017-02-03 2018-08-09 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors
GB201716374D0 (en) * 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
GB201703282D0 (en) 2017-03-01 2017-04-12 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
JOP20190192A1 (ar) 2017-03-01 2019-08-08 Glaxosmithkline Ip No 2 Ltd مشتقات بيرازول بوصفها مثبطات برومودومين
WO2019055444A1 (en) 2017-09-13 2019-03-21 The Regents Of The University Of Michigan DEGRADATION AGENTS OF BROMODOMAIN BET PROTEIN WITH CLEAR BINDERS
GB201716369D0 (en) 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
GB201716392D0 (en) 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
GB201814167D0 (en) 2018-08-31 2018-10-17 Glaxosmithkline Ip No 2 Ltd Compounds
TWI882964B (zh) 2018-09-13 2025-05-11 大陸商恒翼生物醫藥(上海)股份有限公司 Bet 溴結構域(bromodomain)抑制劑之固體形式之製備方法
TWI816880B (zh) * 2018-09-13 2023-10-01 大陸商恒翼生物醫藥(上海)股份有限公司 治療前列腺癌之組合療法
WO2021175432A1 (en) 2020-03-04 2021-09-10 Boehringer Ingelheim International Gmbh Method for administration of an anti cancer agent
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US20240316061A1 (en) 2021-09-17 2024-09-26 Institut Curie Bet inhibitors for treating pab1 deficient cancer
CN119365455A (zh) 2022-04-19 2025-01-24 纽韦卢森公司 对溴结构域有活性的化合物
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
SE0101161D0 (sv) * 2001-03-30 2001-03-30 Astrazeneca Ab New compounds
US20050228016A1 (en) * 2002-06-13 2005-10-13 Enrique Michelotti Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex
EP1435356A1 (en) * 2003-01-06 2004-07-07 Warner-Lambert Company LLC Quinoline derivatives as CRTH2 antagonists
PL1699512T3 (pl) 2003-11-03 2012-11-30 Glaxo Group Ltd Urządzenie do dozowania płynów
WO2006083692A2 (en) * 2005-01-28 2006-08-10 Mount Sinai Schoool Of Medicine Methods of identifying modulators of bromodomains
WO2007084625A2 (en) * 2006-01-19 2007-07-26 Mount Sinai School Of Medicine Novel compounds and methods for inhibiting p53 activity
JP2008156311A (ja) 2006-12-26 2008-07-10 Institute Of Physical & Chemical Research Brd2ブロモドメイン結合剤
WO2009041072A1 (ja) * 2007-09-27 2009-04-02 Kowa Company, Ltd. テトラヒドロキノリン化合物を有効成分とする貧血の予防及び/又は治療剤
EP2239264A4 (en) 2007-12-28 2012-01-11 Mitsubishi Tanabe Pharma Corp ANTITUMORAL MEDIUM
EP2415764A4 (en) * 2009-03-31 2012-08-08 Kowa Co PROPHYLACTIC AND / OR THERAPEUTIC AGENT AGAINST ANEMIA WITH A TETRAHYDROCHINOLINE COMPOUND AS AN ACTIVE SUBSTANCE

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