CN109641886B - 双环bet布罗莫结构域抑制剂及其用途 - Google Patents

双环bet布罗莫结构域抑制剂及其用途 Download PDF

Info

Publication number
CN109641886B
CN109641886B CN201680079771.1A CN201680079771A CN109641886B CN 109641886 B CN109641886 B CN 109641886B CN 201680079771 A CN201680079771 A CN 201680079771A CN 109641886 B CN109641886 B CN 109641886B
Authority
CN
China
Prior art keywords
dimethylisoxazol
chlorobenzyl
quinazolin
alkyl
independently selected
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
CN201680079771.1A
Other languages
English (en)
Chinese (zh)
Other versions
CN109641886A (zh
Inventor
J·W·斯特罗唯尔
吉冈亮
D·J·马隆尼
S·M·杨
A·贾德弗
D·J·厄
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
United States, As Represented By Secretary And Department Of Health And Human Services
ConverGene LLC
Original Assignee
United States, As Represented By Secretary And Department Of Health And Human Services
ConverGene LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by United States, As Represented By Secretary And Department Of Health And Human Services, ConverGene LLC filed Critical United States, As Represented By Secretary And Department Of Health And Human Services
Priority to CN202211334125.9A priority Critical patent/CN115806550B/zh
Publication of CN109641886A publication Critical patent/CN109641886A/zh
Application granted granted Critical
Publication of CN109641886B publication Critical patent/CN109641886B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/10—Spiro-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Toxicology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyridine Compounds (AREA)
CN201680079771.1A 2015-11-25 2016-11-23 双环bet布罗莫结构域抑制剂及其用途 Active CN109641886B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202211334125.9A CN115806550B (zh) 2015-11-25 2016-11-23 双环bet布罗莫结构域抑制剂及其用途

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562259894P 2015-11-25 2015-11-25
US62/259,894 2015-11-25
PCT/US2016/063485 WO2017091661A1 (en) 2015-11-25 2016-11-23 Bicyclic bet bromodomain inhibitors and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN202211334125.9A Division CN115806550B (zh) 2015-11-25 2016-11-23 双环bet布罗莫结构域抑制剂及其用途

Publications (2)

Publication Number Publication Date
CN109641886A CN109641886A (zh) 2019-04-16
CN109641886B true CN109641886B (zh) 2022-11-18

Family

ID=57543210

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201680079771.1A Active CN109641886B (zh) 2015-11-25 2016-11-23 双环bet布罗莫结构域抑制剂及其用途
CN202211334125.9A Active CN115806550B (zh) 2015-11-25 2016-11-23 双环bet布罗莫结构域抑制剂及其用途

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN202211334125.9A Active CN115806550B (zh) 2015-11-25 2016-11-23 双环bet布罗莫结构域抑制剂及其用途

Country Status (8)

Country Link
US (2) US10508106B2 (https=)
EP (2) EP3380469B1 (https=)
JP (2) JP6882289B2 (https=)
CN (2) CN109641886B (https=)
AU (3) AU2016361441B2 (https=)
CA (1) CA3006300C (https=)
ES (2) ES3011058T3 (https=)
WO (1) WO2017091661A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108314680A (zh) * 2017-01-16 2018-07-24 凯惠科技发展(上海)有限公司 一种含芳环化合物、其制备方法、药物组合物及应用
CN109111426B (zh) * 2017-06-23 2021-12-14 中国科学院上海药物研究所 一类稠合双环杂芳基或芳基化合物，及其用途
WO2019201296A1 (zh) * 2018-04-18 2019-10-24 南京明德新药研发有限公司 作为rho激酶抑制剂的吡唑类化合物
EP3620164A1 (en) * 2018-09-05 2020-03-11 Genoscience Pharma SAS Substituted 2,4 diamino-quinoline as new medicament for fibrosis, autophagy and cathepsins b (ctsb), l (ctsl) and d (ctsd) related diseases
EP4424379A3 (en) * 2019-04-24 2024-10-30 Convergene Llc Small molecule bromodomain inhibitors and uses thereof
BR112021022099A2 (pt) * 2019-05-31 2021-12-28 Chiesi Farm Spa Derivados de amino quinazolina como inibidores de p2x3
CN114222741B (zh) * 2019-05-31 2025-12-30 奇斯药制品公司 作为p2x3抑制剂的吡啶并嘧啶类衍生物
EP4234548A4 (en) * 2020-10-20 2024-10-23 Suzhou Zelgen Biopharmaceutical Co., Ltd. SUBSTITUTED BENZO OR PYRIDOPYRIMIDINE AMINE INHIBITOR, ITS PREPARATION METHOD AND ITS APPLICATION
WO2022161461A1 (zh) * 2021-01-29 2022-08-04 江苏先声药业有限公司 Sos1抑制剂及其制备方法和应用
WO2022171018A1 (zh) * 2021-02-09 2022-08-18 苏州泽璟生物制药股份有限公司 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用
EP4291195A4 (en) * 2021-02-11 2025-07-09 Medical College Wisconsin Inc SMALL MOLECULE INHIBITORS OF PBRM1-BD2
CN119630431A (zh) * 2022-08-26 2025-03-14 卫材R&D管理有限公司 抗体药物缀合物
WO2024235225A1 (zh) * 2023-05-15 2024-11-21 苏州泽璟生物制药股份有限公司 取代嘧啶并环类抑制剂及其制备方法和应用
WO2025209570A1 (zh) * 2024-04-03 2025-10-09 北京大学 Bet抑制剂及其应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0393926A1 (en) * 1989-04-12 1990-10-24 Smithkline Beecham Intercredit B.V. 1-Aminoisoquinoline derivatives
EP1012166B1 (en) * 1997-08-29 2003-10-29 Tularik Limited 1-amino-7-isoquinoline derivatives as serine protease inhibitors
WO2011054846A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Imidazo [4, 5-c] quinoline derivates as bromodomain inhibitors
WO2014159837A1 (en) * 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3755332A (en) * 1971-07-01 1973-08-28 Ciba Geigy Corp Substituted 4 indazolaminoquinolines
FI940469L (fi) 1991-08-02 1994-02-01 Pfizer Kinoliinijohdannaisia immunostimulantteina
US7074801B1 (en) * 2001-04-26 2006-07-11 Eisai Co., Ltd. Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof
SE0102858D0 (sv) * 2001-08-27 2001-08-27 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
JP4934432B2 (ja) * 2004-02-19 2012-05-16 レクサン ファーマシューティカルズ インコーポレイテッド キナゾリン誘導体およびキナゾリン誘導体の治療への使用
KR100910333B1 (ko) * 2005-02-23 2009-07-31 시오노기세이야쿠가부시키가이샤 타이로신 키나아제 억제 활성을 갖는 퀴나졸린 유도체
CR9465A (es) * 2005-03-25 2008-06-19 Surface Logix Inc Compuestos mejorados farmacocineticamente
WO2006121767A2 (en) 2005-05-06 2006-11-16 Apath, Llc 4-aminoquinoline compounds for treating virus-related conditions
WO2008054599A2 (en) 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
US20080200458A1 (en) * 2007-01-18 2008-08-21 Joseph Barbosa Methods and compositions for the treatment of body composition disorders
US20080194557A1 (en) * 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
GB0705915D0 (en) * 2007-03-28 2007-05-09 Helperby Therapeutics Ltd New use
EP2152672A1 (en) * 2007-05-24 2010-02-17 Bayer Schering Pharma Aktiengesellschaft Novel sulphoximine-substituted quinazoline and quinazoline derivatives as kinase inhibitors
JP5301456B2 (ja) * 2007-11-12 2013-09-25 Ｍｓｄ株式会社 ヘテロアリールオキシキナゾリン誘導体
EP2072502A1 (de) 2007-12-20 2009-06-24 Bayer Schering Pharma Aktiengesellschaft Sulfoximid-substituierte Chinolin- und Chinazolinderivate als Kinase-Inhibitoren
WO2010056758A1 (en) * 2008-11-12 2010-05-20 Yangbo Feng Quinazoline derivatives as kinase inhibitors
US20110135655A1 (en) * 2009-01-13 2011-06-09 PHILADELPHIA HEALTH AND EDUCATION CORPORATION d/b/a Drexel University College of Medicine; Role of PI3K p110 delta Signaling in Retroviral Infection and Replication
AR079814A1 (es) * 2009-12-31 2012-02-22 Otsuka Pharma Co Ltd Compuestos heterociclicos, composiciones farmaceuticas que los contienen y sus usos
EP2566477B1 (en) * 2010-05-07 2015-09-02 GlaxoSmithKline Intellectual Property Development Limited Amino-quinolines as kinase inhibitors
US8933096B2 (en) * 2010-06-09 2015-01-13 Rugers, The State University of New Jersey Antimicrobial agents
AU2011289230B2 (en) 2010-08-13 2014-09-04 Janssen Pharmaceutica Nv 4 - aminoquinazolin- 2 - yl - 1 - pyrrazole - 4 - carboxylic acid compounds as prolyl hydroxylase inhibitors
WO2012040499A2 (en) * 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
WO2012125913A1 (en) * 2011-03-17 2012-09-20 The Trustees Of The University Of Pennsylvania Methods and use of bifunctional enzyme-building clamp-shaped molecules
GB201106799D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
KR20140048216A (ko) 2011-06-29 2014-04-23 오츠카 세이야쿠 가부시키가이샤 치료 화합물로서의 퀴나졸린 및 관련된 사용 방법
EP2788332A1 (en) * 2011-12-07 2014-10-15 Amgen, Inc. Bicyclic aryl and heteroaryl sodium channel inhibitors
US20130225611A1 (en) * 2011-12-09 2013-08-29 The Regents Of The University Of California Compositions and Methods for Reducing Cancer Cell Proliferation and Modulating Importin-Beta Function
US20130281397A1 (en) * 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US9201821B2 (en) * 2012-09-27 2015-12-01 Apple Inc. Interrupt timestamping
KR20150072412A (ko) * 2012-10-05 2015-06-29 리겔 파마슈티칼스, 인크. Gdf-8 억제제
US9977024B2 (en) * 2012-12-09 2018-05-22 The Scripps Research Institute Targeted covalent probes and inhibitors of proteins containing redox-sensitive cysteines
WO2014100501A1 (en) * 2012-12-20 2014-06-26 Sanford-Burnham Medical Research Institute Small molecule agonists of neurotensin receptor 1
EP3010918B1 (en) * 2013-06-21 2018-08-15 Zenith Epigenetics Ltd. Novel substituted bicyclic compounds as bromodomain inhibitors
JP6542212B2 (ja) 2013-07-31 2019-07-10 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新規キナゾリノン
WO2015112739A1 (en) * 2014-01-22 2015-07-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Compounds and method for treating parp1-deficient cancers
CN106536507B (zh) * 2014-04-08 2020-04-07 里格尔药品股份有限公司 作为TGF-β抑制剂的2,3-二取代的吡啶化合物及其使用方法
US11034757B2 (en) * 2014-06-09 2021-06-15 Biomed Valley Discoveries, Inc. Combination therapies using agents that target tumor-associated stroma or tumor cells and tumor vasculature
JP6599908B2 (ja) * 2014-06-25 2019-10-30 サンフォード−バーンハム メディカル リサーチ インスティテュート ニューロテンシン受容体１の小分子アゴニスト
US10106507B2 (en) * 2014-08-03 2018-10-23 H. Lee Moffitt Cancer Center and Research Insitute, Inc. Potent dual BRD4-kinase inhibitors as cancer therapeutics
WO2016120808A1 (en) 2015-01-28 2016-08-04 Minoryx Therapeutics S.L. Heteroarylaminoisoquinolines, methods for their preparation and therapeutic uses thereof
EP3072891A1 (en) * 2015-03-24 2016-09-28 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. New Toll-Like Receptor 9 Antagonists
JP2018525345A (ja) * 2015-07-01 2018-09-06 ノースウェスタン ユニバーシティ 置換キナゾリン化合物及びグルコセレブロシダーゼ活性の調節のためのその使用

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0393926A1 (en) * 1989-04-12 1990-10-24 Smithkline Beecham Intercredit B.V. 1-Aminoisoquinoline derivatives
EP1012166B1 (en) * 1997-08-29 2003-10-29 Tularik Limited 1-amino-7-isoquinoline derivatives as serine protease inhibitors
WO2011054846A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Imidazo [4, 5-c] quinoline derivates as bromodomain inhibitors
WO2014159837A1 (en) * 2013-03-14 2014-10-02 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents;Su Hui Yang，等;《Bioorganic & Medicinal Chemistry Letters》;20100703;第20卷;第5279页 *
The synthesis and biological evaluation of new DNA-directed alkylating agents, phenyl N-mustard-4-anilinoquinoline conjugates containing a urea linker;Bhavin Marvania，等;《European Journal of Medicinal Chemistry》;20140628;第83卷;第697页 *

Also Published As

Publication number Publication date
WO2017091661A1 (en) 2017-06-01
US10508106B2 (en) 2019-12-17
ES2918589T3 (es) 2022-07-19
ES3011058T3 (en) 2025-04-07
EP4050005B1 (en) 2024-12-25
CA3006300C (en) 2024-02-27
EP4050005A1 (en) 2022-08-31
EP3380469A1 (en) 2018-10-03
CN109641886A (zh) 2019-04-16
EP3380469B1 (en) 2022-03-16
CN115806550A (zh) 2023-03-17
US20200223836A1 (en) 2020-07-16
AU2016361441B2 (en) 2021-08-12
JP2021119188A (ja) 2021-08-12
JP7112567B2 (ja) 2022-08-03
AU2016361441A1 (en) 2018-06-21
US11028079B2 (en) 2021-06-08
US20180305344A1 (en) 2018-10-25
CN115806550B (zh) 2025-11-28
JP2019501140A (ja) 2019-01-17
AU2021209257A1 (en) 2021-08-19
CA3006300A1 (en) 2017-06-01
AU2021209257B2 (en) 2023-12-21
JP6882289B2 (ja) 2021-06-02
AU2024201890A1 (en) 2024-05-16

Similar Documents

Publication Publication Date Title
CN109641886B (zh) 双环bet布罗莫结构域抑制剂及其用途
ES2866152T3 (es) Derivados de tirosina amida como inhibidores de la Rho-quinasa
CN107406426B (zh) 作为rock抑制剂的环状脲类
ES2838573T3 (es) Derivados de benzamida ligados como inhibidores potentes de ROCK
AU2017359023B2 (en) 3-substituted propionic acids as alpha v integrin inhibitors
CN107207464B (zh) 被取代的二氢异喹啉酮化合物
CN112243439A (zh) 作为hpk1抑制剂的吡咯并[2,3-b]吡啶或吡咯并[2,3-b]吡嗪及其用途
CN110520423A (zh) 作为激酶抑制剂的氨基三唑并吡啶
CN105073741A (zh) 作为rock抑制剂的酞嗪酮及异喹啉酮
TW201620913A (zh) 作為PARP抑制劑的4H-吡唑並[1,5-α]苯並咪唑化合物的類似物
WO2015104662A1 (en) Indazole compounds as irak4 inhibitors
CN110869361A (zh) 用于治疗心力衰竭的rock的五元氨基杂环和5,6元或6,6元双环氨基杂环抑制剂
CN106488916A (zh) 作为pde抑制剂的新型2,5‑取代的嘧啶类
KR20200083529A (ko) 파르네소이드 x 수용체 조정제로서의 알켄 스피로시클릭 화합물
CN112752757B (zh) 作为rho-激酶抑制剂的酪氨酸酰胺衍生物
CN111918863A (zh) 杂环化合物
WO2021051827A1 (zh) 一种细胞凋亡蛋白抑制剂及其制备方法和用途
HK40078733A (en) Bicyclic bet bromodomain inhibitors and uses thereof
HK40078733B (en) Bicyclic bet bromodomain inhibitors and uses thereof
HK1261992B (en) Bicyclic bet bromodomain inhibitors and uses thereof
HK1261992A1 (en) Bicyclic bet bromodomain inhibitors and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant