JP6669745B2 - ブロモドメインのインヒビターとしての置換ピロロピリジン - Google Patents

ブロモドメインのインヒビターとしての置換ピロロピリジン Download PDF

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Publication number
JP6669745B2
JP6669745B2 JP2017525078A JP2017525078A JP6669745B2 JP 6669745 B2 JP6669745 B2 JP 6669745B2 JP 2017525078 A JP2017525078 A JP 2017525078A JP 2017525078 A JP2017525078 A JP 2017525078A JP 6669745 B2 JP6669745 B2 JP 6669745B2
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oxo
alkyl
methyl
heterocyclyl
optionally substituted
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JP2017533249A5 (enExample
JP2017533249A (ja
Inventor
ブライアン ケー． アルブレヒト，
ブライアン ケー． アルブレヒト，
スティーブン エフ． ベロン，
スティーブン エフ． ベロン，
ダニエル ジェイ． バーディック，
ダニエル ジェイ． バーディック，
アレクサンドル コート，
アレクサンドル コート，
テリー クローフォード，
テリー クローフォード，
レス エー． デイキン，
レス エー． デイキン，
マイケル チャールズ ヒューイット，
マイケル チャールズ ヒューイット，
ツイ， ビッキー シャオ−ウェイ
ツイ， ビッキー シャオ−ウェイ
イブ レブラン，
イブ レブラン，
スティーブン アール． マグヌソン，
スティーブン アール． マグヌソン，
クリストファー ジー． ナスヴェスチャック，
クリストファー ジー． ナスヴェスチャック，
エフ． アントニー ロメロ，
エフ． アントニー ロメロ，
ヨン タン，
ヨン タン，
アレクサンダー エム． テイラー，
アレクサンダー エム． テイラー，
シューメイ ワン，
シューメイ ワン，
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Constellation Pharmaceuticals Inc
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Constellation Pharmaceuticals Inc
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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JP2017525078A 2014-11-10 2015-11-10 ブロモドメインのインヒビターとしての置換ピロロピリジン Expired - Fee Related JP6669745B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462077707P 2014-11-10 2014-11-10
US62/077,707 2014-11-10
PCT/US2015/060007 WO2016077380A1 (en) 2014-11-10 2015-11-10 Substituted pyrrolopyridines as inhibitors of bromodomain

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JP2017533249A JP2017533249A (ja) 2017-11-09
JP2017533249A5 JP2017533249A5 (enExample) 2018-12-20
JP6669745B2 true JP6669745B2 (ja) 2020-03-18

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US (1) US10150767B2 (enExample)
EP (1) EP3218374B1 (enExample)
JP (1) JP6669745B2 (enExample)
CN (1) CN107108614B (enExample)
MA (1) MA40940A (enExample)
WO (1) WO2016077380A1 (enExample)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA40943A (fr) * 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
JP6639497B2 (ja) * 2014-11-10 2020-02-05 ジェネンテック， インコーポレイテッド ブロモドメインインヒビターおよびその使用
CN107531692B (zh) 2015-01-29 2020-12-25 基因泰克公司 治疗化合物及其用途
EP3265453B1 (en) 2015-03-05 2022-06-29 Boehringer Ingelheim International GmbH New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
AR104259A1 (es) 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio
SG11201808003RA (en) 2016-04-15 2018-10-30 Abbvie Inc Bromodomain inhibitors
WO2017185036A1 (en) 2016-04-22 2017-10-26 Dana Farber Cancer Institute, Inc. Bifunctional molecules for degradation of egfr and methods of use
WO2018130174A1 (zh) * 2017-01-11 2018-07-19 江苏豪森药业集团有限公司 吡咯并[2,3-c]吡啶类衍生物、其制备方法及其在医药上的应用
AU2018209164B2 (en) 2017-01-17 2021-11-04 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
EP3609896A4 (en) * 2017-04-14 2020-11-04 AbbVie Inc. BROMODOMAIN INHIBITORS
CN108976278B (zh) * 2017-06-05 2021-04-06 海创药业股份有限公司 一种嵌合分子及其制备和应用
US11466034B2 (en) * 2017-12-20 2022-10-11 Betta Pharmaceuticals Co., Ltd. Compound functioning as bromodomain protein inhibitor, and composition
EP3750885A4 (en) * 2018-02-06 2021-10-27 Shanghai Haihe Pharmaceutical Co., Ltd. COMPOUND PRESENTING AN INHIBITORING ACTIVITY OF BET, ITS PREPARATION PROCESS AND ITS USE
CN108465108B (zh) * 2018-03-12 2020-07-07 上海宇玫博生物科技有限公司 一种预防或治疗脑胶质瘤的特异性基因靶点
US10442799B1 (en) 2018-04-07 2019-10-15 Fuqiang Ruan Heterocyclic compounds and uses thereof
CN110372693B (zh) * 2018-07-04 2022-05-03 清华大学 一种靶向降解bet蛋白的化合物及其应用
CN110776508B (zh) * 2018-07-27 2021-07-16 海创药业股份有限公司 一种brd4抑制剂及其制备方法和用途
CN110818609A (zh) * 2018-08-11 2020-02-21 中国药科大学 3-乙酰基吲哚类brpf1抑制剂的制备方法及其用途
EP3841115A4 (en) * 2018-08-20 2022-08-24 University of Georgia Research Foundation, Inc. COMPOSITIONS AND METHODS TO INCREASE STAINING OF WHITE FAT TISSUE
CN109125729A (zh) * 2018-09-06 2019-01-04 苏州吉玛基因股份有限公司 与非小细胞肺癌诊疗相关的基因BRD9及其siRNAs和应用
US20220079951A1 (en) * 2018-12-20 2022-03-17 Saint Louis University Bet inhibitors for modulating dux4 expression in fshd
EP3958867B1 (en) * 2019-04-24 2024-06-26 Convergene Llc Small molecule bromodomain inhibitors and uses thereof
GB201905721D0 (en) * 2019-04-24 2019-06-05 Univ Dundee Compounds
US11171132B2 (en) * 2019-10-03 2021-11-09 Globalfoundries U.S. Inc. Bi-directional breakdown silicon controlled rectifiers
CN112625036A (zh) * 2019-10-08 2021-04-09 上海海和药物研究开发股份有限公司 一类具有brd4抑制活性的化合物、其制备方法及用途
WO2022012456A1 (en) * 2020-07-17 2022-01-20 Chengdu Easton Biopharmaceuticals Co., Ltd. Novel heterocyclic compounds as bet inhibitors
TW202237095A (zh) 2020-12-03 2022-10-01 德商艾斯巴赫生物有限公司 Ａｌｃ１抑制劑及與ｐａｒｐｉ之協同性
US20240308998A1 (en) * 2021-06-29 2024-09-19 Tay Therapeutics Limited Pyrrolopyridone derivatives useful in the treatment of cancer
CN115611890B (zh) * 2021-07-15 2024-05-31 成都硕德药业有限公司 一种新型噻吩类bet溴结构域抑制剂、其制备方法及医药用途
TW202330519A (zh) * 2021-09-29 2023-08-01 香港商德琪研發有限公司 作為ｔａｍ抑制劑的吡唑并吡啶化合物
WO2023213833A1 (en) 2022-05-02 2023-11-09 Eisbach Bio Gmbh Use of alc1 inhibitors and synergy with parpi
CN117304205A (zh) * 2022-06-20 2023-12-29 中国科学院广州生物医药与健康研究院 一种苯并咪唑类三元并环化合物、其药学上可接受的盐及其应用
CN117304204A (zh) * 2022-06-20 2023-12-29 中国科学院广州生物医药与健康研究院 一种苯并咪唑类三元并环化合物、其药学上可接受的盐及其应用
WO2024138201A2 (en) * 2022-12-23 2024-06-27 Tay Therapeutics Limited Selective bet inhibitors and uses thereof
WO2024193527A1 (zh) * 2023-03-20 2024-09-26 山东新时代药业有限公司 作为溴结构域抑制剂的吡咯并[2,3-c]吡啶类化合物

Family Cites Families (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU22545A1 (es) 1994-11-18 1999-03-31 Centro Inmunologia Molecular Obtención de un anticuerpo quimérico y humanizado contra el receptor del factor de crecimiento epidérmico para uso diagnóstico y terapéutico
US4943533A (en) 1984-03-01 1990-07-24 The Regents Of The University Of California Hybrid cell lines that produce monoclonal antibodies to epidermal growth factor receptor
DE69025946T2 (de) 1989-09-08 1996-10-17 Univ Duke Modifikationen der struktur des egf-rezeptor-gens in menschlichen glioma
AU661533B2 (en) 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
GB9314893D0 (en) 1993-07-19 1993-09-01 Zeneca Ltd Quinazoline derivatives
ATE207366T1 (de) 1993-12-24 2001-11-15 Merck Patent Gmbh Immunokonjugate
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5654307A (en) 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
ATE176910T1 (de) 1994-07-21 1999-03-15 Akzo Nobel Nv Zyklische keton peroxyde zubereitungen
US5804396A (en) 1994-10-12 1998-09-08 Sugen, Inc. Assay for agents active in proliferative disorders
EP0817775B1 (en) 1995-03-30 2001-09-12 Pfizer Inc. Quinazoline derivatives
GB9508538D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quinazoline derivatives
GB9508565D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quiazoline derivative
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
JPH11507535A (ja) 1995-06-07 1999-07-06 イムクローン システムズ インコーポレイテッド 腫瘍の成長を抑制する抗体および抗体フラグメント類
ATE212993T1 (de) 1995-07-06 2002-02-15 Novartis Erfind Verwalt Gmbh Pyrolopyrimidine und verfahren zu ihrer herstellung
US5760041A (en) 1996-02-05 1998-06-02 American Cyanamid Company 4-aminoquinazoline EGFR Inhibitors
GB9603095D0 (en) 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
EP0892789B2 (en) 1996-04-12 2009-11-18 Warner-Lambert Company LLC Irreversible inhibitors of tyrosine kinases
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
US6002008A (en) 1997-04-03 1999-12-14 American Cyanamid Company Substituted 3-cyano quinolines
UA73073C2 (uk) 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
US6235883B1 (en) 1997-05-05 2001-05-22 Abgenix, Inc. Human monoclonal antibodies to epidermal growth factor receptor
AU7165698A (en) 1997-05-06 1998-11-27 American Cyanamid Company Use of quinazoline compounds for the treatment of polycystic kidney disease
ZA986732B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
ZA986729B (en) 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
TW436485B (en) 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
CN1278176A (zh) 1997-11-06 2000-12-27 美国氰胺公司 喹唑啉衍生物作为用于治疗结肠息肉的酪氨酸激酶抑制剂的应用
EA003786B1 (ru) 1998-11-19 2003-10-30 Варнер Ламберт Компани N-[4-(3-хлор-4-фторфениламино)-7-(3-морфолин-4-илпропокси)хиназолин-6-ил]акриламид - необратимый ингибитор тирозинкиназ
EP1953147A1 (en) 2005-11-21 2008-08-06 Japan Tobacco, Inc. Heterocyclic compound and medicinal application thereof
WO2013097052A1 (en) * 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
US20140094456A1 (en) * 2012-10-02 2014-04-03 Intermune, Inc. Anti-fibrotic pyridinones
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
WO2014125408A2 (en) * 2013-02-12 2014-08-21 Aurigene Discovery Technologies Limited Substituted 1h-pyrrolopyridinone derivatives as kinase inhibitors
EP2970285B1 (en) 2013-03-11 2019-04-17 AbbVie Inc. Fused tetracyclic bromodomain inhibitors
CN105026403B (zh) * 2013-03-12 2018-05-18 艾伯维公司 四环布罗莫结构域抑制剂
CN104211639A (zh) 2013-06-05 2014-12-17 中国科学院上海药物研究所 一类炔基杂环类化合物及其应用
EP3008051A4 (en) 2013-06-12 2017-03-01 Viamet Pharmaceuticals, Inc. Metalloenzyme inhibitor compounds
MX2015017963A (es) * 2013-06-28 2016-11-10 Abbvie Inc Inhibidores de bromodominio.
WO2015081246A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081280A1 (en) * 2013-11-26 2015-06-04 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution
US9399640B2 (en) * 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
RU2692485C2 (ru) 2014-04-02 2019-06-25 Интермьюн, Инк. Противофиброзные пиридиноны
SI3674302T1 (sl) * 2014-04-23 2023-07-31 Incyte Holdings Corporation 1h-pirolo(2,3-c)piridin-7(6h)-oni in pirazolo(3,4-c)piridin-7(6h)-oni kot zaviralci proteinov bet
JP6639497B2 (ja) 2014-11-10 2020-02-05 ジェネンテック， インコーポレイテッド ブロモドメインインヒビターおよびその使用
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
US9763922B2 (en) * 2014-11-27 2017-09-19 Genentech, Inc. Therapeutic compounds and uses thereof
WO2016118951A2 (en) 2015-01-23 2016-07-28 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
CN107531692B (zh) 2015-01-29 2020-12-25 基因泰克公司 治疗化合物及其用途

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