AU2016361441B2 - Bicyclic BET bromodomain inhibitors and uses thereof - Google Patents

Bicyclic BET bromodomain inhibitors and uses thereof Download PDF

Info

Publication number
AU2016361441B2
AU2016361441B2 AU2016361441A AU2016361441A AU2016361441B2 AU 2016361441 B2 AU2016361441 B2 AU 2016361441B2 AU 2016361441 A AU2016361441 A AU 2016361441A AU 2016361441 A AU2016361441 A AU 2016361441A AU 2016361441 B2 AU2016361441 B2 AU 2016361441B2
Authority
AU
Australia
Prior art keywords
dimethylisoxazol
quinazolin
chlorobenzyl
amino
methyl
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
AU2016361441A
Other languages
English (en)
Other versions
AU2016361441A1 (en
Inventor
Ajit Jadhav
David J. Maloney
Jeffrey William STROVEL
Daniel Jason URBAN
Shyh Ming YANG
Makoto Yoshioka
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.)
ConverGene LLC
US Department of Health and Human Services
Original Assignee
ConverGene LLC
Government of the United States of America
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 ConverGene LLC, Government of the United States of America filed Critical ConverGene LLC
Publication of AU2016361441A1 publication Critical patent/AU2016361441A1/en
Priority to AU2021209257A priority Critical patent/AU2021209257B2/en
Application granted granted Critical
Publication of AU2016361441B2 publication Critical patent/AU2016361441B2/en
Priority to AU2024201890A priority patent/AU2024201890A1/en
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)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Toxicology (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Psychiatry (AREA)
  • Hematology (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)
AU2016361441A 2015-11-25 2016-11-23 Bicyclic BET bromodomain inhibitors and uses thereof Active AU2016361441B2 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2021209257A AU2021209257B2 (en) 2015-11-25 2021-07-28 Bicyclic BET bromodomain inhibitors and uses thereof
AU2024201890A AU2024201890A1 (en) 2015-11-25 2024-03-22 Bicyclic BET bromodomain inhibitors and uses thereof

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
AU2021209257A Division AU2021209257B2 (en) 2015-11-25 2021-07-28 Bicyclic BET bromodomain inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
AU2016361441A1 AU2016361441A1 (en) 2018-06-21
AU2016361441B2 true AU2016361441B2 (en) 2021-08-12

Family

ID=57543210

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2016361441A Active AU2016361441B2 (en) 2015-11-25 2016-11-23 Bicyclic BET bromodomain inhibitors and uses thereof
AU2021209257A Active AU2021209257B2 (en) 2015-11-25 2021-07-28 Bicyclic BET bromodomain inhibitors and uses thereof
AU2024201890A Pending AU2024201890A1 (en) 2015-11-25 2024-03-22 Bicyclic BET bromodomain inhibitors and uses thereof

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2021209257A Active AU2021209257B2 (en) 2015-11-25 2021-07-28 Bicyclic BET bromodomain inhibitors and uses thereof
AU2024201890A Pending AU2024201890A1 (en) 2015-11-25 2024-03-22 Bicyclic BET bromodomain inhibitors and uses thereof

Country Status (8)

Country Link
US (2) US10508106B2 (https=)
EP (2) EP4050005B1 (https=)
JP (2) JP6882289B2 (https=)
CN (2) CN115806550B (https=)
AU (3) AU2016361441B2 (https=)
CA (1) CA3006300C (https=)
ES (2) ES2918589T3 (https=)
WO (1) WO2017091661A1 (https=)

Families Citing this family (15)

* 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
WO2020219168A1 (en) 2019-04-24 2020-10-29 Convergene, Llc Small molecule bromodomain inhibitors and uses thereof
CA3139018A1 (en) * 2019-05-31 2020-12-03 Chiesi Farmaceutici S.P.A. Amino quinazoline derivatives as p2x3 inhibitors
JP7797204B2 (ja) 2019-05-31 2026-01-13 キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ Ｐ２ｘ３阻害剤としてのピリドピリミジン誘導体
WO2022083657A1 (zh) * 2020-10-20 2022-04-28 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
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
US20240190828A1 (en) * 2021-02-11 2024-06-13 The Medical College Of Wisconsin, Inc. Small Molecule Inhibitors of PBRM1-BD2
KR20230159543A (ko) * 2021-03-26 2023-11-21 메드샤인 디스커버리 아이엔씨. 6-카바메이트로 치환된 헤테로방향족 고리 유도체
JPWO2024043319A1 (https=) * 2022-08-26 2024-02-29
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 (25)

* 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
EP0393926A1 (en) * 1989-04-12 1990-10-24 Smithkline Beecham Intercredit B.V. 1-Aminoisoquinoline derivatives
WO1993003030A1 (en) * 1991-08-02 1993-02-18 Pfizer Inc. Quinoline derivatives as immunostimulants
EP1012166B1 (en) * 1997-08-29 2003-10-29 Tularik Limited 1-amino-7-isoquinoline derivatives as serine protease inhibitors
EP1430030B1 (en) * 2001-08-27 2005-05-18 AstraZeneca AB N-type calcium channel antagonists for the treatment of pain
WO2006121767A2 (en) * 2005-05-06 2006-11-16 Apath, Llc 4-aminoquinoline compounds for treating virus-related conditions
EP1854789A1 (en) * 2005-02-23 2007-11-14 Shionogi & Co., Ltd. Quinazoline derivative having tyrosine kinase inhibitory activity
WO2008054599A2 (en) * 2006-09-27 2008-05-08 Surface Logix, Inc. Rho kinase inhibitors
WO2008117079A1 (en) * 2007-03-28 2008-10-02 Helperby Therapeutics Limited Antimicrobial compounds based upon 4-aminoquinoline
EP2072502A1 (de) * 2007-12-20 2009-06-24 Bayer Schering Pharma Aktiengesellschaft Sulfoximid-substituierte Chinolin- und Chinazolinderivate als Kinase-Inhibitoren
EP2221301A1 (en) * 2007-11-12 2010-08-25 Banyu Pharmaceutical Co., Ltd. Heteroaryloxy quinazoline derivative
WO2011140442A1 (en) * 2010-05-07 2011-11-10 Glaxo Group Limited Amino-quinolines as kinase inhibitors
WO2012040499A2 (en) * 2010-09-22 2012-03-29 Surface Logix, Inc. Metabolic inhibitors
AU2010339423A1 (en) * 2009-12-31 2012-06-14 Otsuka Pharmaceutical Co., Ltd. Therapeutic compounds and related methods of use
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
WO2013086229A1 (en) * 2011-12-07 2013-06-13 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
EP2650286A1 (en) * 2004-02-19 2013-10-16 Rexahn Pharmaceuticals, Inc. Quinazoline derivatives and therapeutic use thereof
US20140089546A1 (en) * 2012-09-27 2014-03-27 Apple Inc. Interrupt timestamping
WO2014089546A1 (en) * 2012-12-09 2014-06-12 The Scripps Research Institute Targeted covalent probes and inhibitors of proteins containing redox-sensitive cysteines
EP1865958B1 (en) * 2005-03-25 2015-07-08 Surface Logix, Inc. Pharmacokinetically improved compounds
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
WO2015157093A1 (en) * 2014-04-08 2015-10-15 Rigel Pharmaceuticals, Inc. 2,3-disubstituted pyridine compounds as tgf-beta inhibitors and methods of use
WO2015191568A2 (en) * 2014-06-09 2015-12-17 Biomed Valley Discoveries, Inc. Combination therapies using agents that target tumor-associated stroma or tumor cells and tumor vasculature
WO2016120808A1 (en) * 2015-01-28 2016-08-04 Minoryx Therapeutics S.L. Heteroarylaminoisoquinolines, methods for their preparation and therapeutic uses thereof

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
WO2008089310A2 (en) * 2007-01-18 2008-07-24 Lexicon Pharmaceuticals, Inc. Delta 5 desaturase inhibitors for the treatment of obesity
US20080194557A1 (en) * 2007-01-18 2008-08-14 Joseph Barbosa Methods and compositions for the treatment of pain, inflammation and cancer
EP2152672A1 (en) * 2007-05-24 2010-02-17 Bayer Schering Pharma Aktiengesellschaft Novel sulphoximine-substituted quinazoline and quinazoline derivatives as kinase inhibitors
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
GB0919423D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011156626A1 (en) * 2010-06-09 2011-12-15 Rutgers, 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
GB201106799D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
CA2840627A1 (en) * 2011-06-29 2013-01-03 Otsuka Pharmaceutical Co., Ltd. Quinazolines as therapeutic compounds and related methods of use
US20130281397A1 (en) * 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2014055955A1 (en) * 2012-10-05 2014-04-10 Rigel Pharmaceuticals, Inc. Gdf-8 inhibitors
CA2895129C (en) * 2012-12-20 2022-07-05 Sanford-Burnham Medical Research Institute Quinazoline neurotensin receptor 1 agonists and uses thereof
EA201591746A1 (ru) * 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
JP6461118B2 (ja) * 2013-06-21 2019-01-30 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の置換された二環式化合物
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
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
WO2016022460A1 (en) * 2014-08-03 2016-02-11 H. Lee Moffitt Cancer Center And Research Institute, Inc. Potent dual brd4-kinase inhibitors as cancer therapeutics
EP3072891A1 (en) * 2015-03-24 2016-09-28 Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. New Toll-Like Receptor 9 Antagonists
CN108290855A (zh) * 2015-07-01 2018-07-17 西北大学 被取代的喹唑啉化合物及其调节葡糖脑苷脂酶活性的用途

Patent Citations (25)

* 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
EP0393926A1 (en) * 1989-04-12 1990-10-24 Smithkline Beecham Intercredit B.V. 1-Aminoisoquinoline derivatives
WO1993003030A1 (en) * 1991-08-02 1993-02-18 Pfizer Inc. Quinoline derivatives as immunostimulants
EP1012166B1 (en) * 1997-08-29 2003-10-29 Tularik Limited 1-amino-7-isoquinoline derivatives as serine protease inhibitors
EP1430030B1 (en) * 2001-08-27 2005-05-18 AstraZeneca AB N-type calcium channel antagonists for the treatment of pain
EP2650286A1 (en) * 2004-02-19 2013-10-16 Rexahn Pharmaceuticals, Inc. Quinazoline derivatives and therapeutic use thereof
EP1854789A1 (en) * 2005-02-23 2007-11-14 Shionogi & Co., Ltd. Quinazoline derivative having tyrosine kinase inhibitory activity
EP1865958B1 (en) * 2005-03-25 2015-07-08 Surface Logix, Inc. Pharmacokinetically improved compounds
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
WO2008117079A1 (en) * 2007-03-28 2008-10-02 Helperby Therapeutics Limited Antimicrobial compounds based upon 4-aminoquinoline
EP2221301A1 (en) * 2007-11-12 2010-08-25 Banyu Pharmaceutical Co., Ltd. Heteroaryloxy quinazoline derivative
EP2072502A1 (de) * 2007-12-20 2009-06-24 Bayer Schering Pharma Aktiengesellschaft Sulfoximid-substituierte Chinolin- und Chinazolinderivate als Kinase-Inhibitoren
AU2010339423A1 (en) * 2009-12-31 2012-06-14 Otsuka Pharmaceutical Co., Ltd. Therapeutic compounds and related methods of use
WO2011140442A1 (en) * 2010-05-07 2011-11-10 Glaxo Group Limited Amino-quinolines as kinase 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
WO2013086229A1 (en) * 2011-12-07 2013-06-13 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
US20140089546A1 (en) * 2012-09-27 2014-03-27 Apple Inc. Interrupt timestamping
WO2014089546A1 (en) * 2012-12-09 2014-06-12 The Scripps Research Institute Targeted covalent probes and inhibitors of proteins containing redox-sensitive cysteines
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
WO2015157093A1 (en) * 2014-04-08 2015-10-15 Rigel Pharmaceuticals, Inc. 2,3-disubstituted pyridine compounds as tgf-beta inhibitors and methods of use
WO2015191568A2 (en) * 2014-06-09 2015-12-17 Biomed Valley Discoveries, Inc. Combination therapies using agents that target tumor-associated stroma or tumor cells and tumor vasculature
WO2016120808A1 (en) * 2015-01-28 2016-08-04 Minoryx Therapeutics S.L. Heteroarylaminoisoquinolines, methods for their preparation and therapeutic uses thereof

Non-Patent Citations (11)

* Cited by examiner, † Cited by third party
Title
ABOUZID, K. et al., BIOORGANIC & MEDICINAL CHEMISTRY, vol. 16, no. 16, pages 7543 - 7551, (2008-07-20) *
CAS REG NO. 1790268-77-7, STN Entry Date 28 June 2015; Isoquinoline, 1-[4-(methylsulfonyl)-1-piperazinyl]- *
CAS REG NO. 919921-38-3, STN Entry Date 08 February 2007; Quinazoline, 4-(4-methyl-2-phenyl-1-piperazinyl)-2-(trifluoromethyl)- *
CAS REG NO. 920839-33-4, STN Entry Date 14 February 2007; Quinazoline, 4-(4-methyl-2-phenyl-1-piperazinyl)-2-(3-pyridinyl)- *
Chou, Tsui-Fen et al. "Structure-Activity Relationship Study Reveals ML240 and ML241 as Potent and Selective Inhibitors of p97 ATPase", ChemMedChem (2013), 8(2), 297-312 *
GAO, Z-G. et al., MOLECULAR PHARMACOLOGY, 2003, vol. 63, no. 5, pages 1021 - 1031 *
MARVANIA B. et al., EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY., 2014, vol. 83, pages 695 - 708 *
MOYER, M. P. et al., BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1992, vol. 2, no. 12, pages 1589 - 1594 *
STUHLMILLER T. J. et al, CELL REPORTS, 2015, vol. 11, no. 3, pages 390 - 404 *
Van, Hue Thi My et al. European Journal of Medicinal Chemistry (2014), 82, 181-194 *
YANG, S. H. et al., BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, no. 17, 2010, pages 5277 - 5281 *

Also Published As

Publication number Publication date
US11028079B2 (en) 2021-06-08
US20180305344A1 (en) 2018-10-25
EP4050005A1 (en) 2022-08-31
ES2918589T3 (es) 2022-07-19
AU2021209257A1 (en) 2021-08-19
AU2024201890A1 (en) 2024-05-16
CN109641886A (zh) 2019-04-16
JP2021119188A (ja) 2021-08-12
AU2016361441A1 (en) 2018-06-21
US20200223836A1 (en) 2020-07-16
AU2021209257B2 (en) 2023-12-21
CN115806550B (zh) 2025-11-28
ES3011058T3 (en) 2025-04-07
CN115806550A (zh) 2023-03-17
JP6882289B2 (ja) 2021-06-02
WO2017091661A1 (en) 2017-06-01
CA3006300A1 (en) 2017-06-01
EP3380469B1 (en) 2022-03-16
JP2019501140A (ja) 2019-01-17
CN109641886B (zh) 2022-11-18
CA3006300C (en) 2024-02-27
JP7112567B2 (ja) 2022-08-03
US10508106B2 (en) 2019-12-17
EP4050005B1 (en) 2024-12-25
EP3380469A1 (en) 2018-10-03

Similar Documents

Publication Publication Date Title
AU2021209257B2 (en) Bicyclic BET bromodomain inhibitors and uses thereof
JP6983273B2 (ja) リジン特異的なデメチラーゼ−１の阻害剤
TWI671301B (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
EP3080100B1 (en) Inhibitors of lysine specific demethylase-1
RS58024B1 (sr) Biciklični heterociklični derivati kao irak4 inhibitori
AU2009232121A1 (en) Novel HSP90 inhibitory carbazole derivatives, compositions containing same, and use thereof
HK40078733A (en) Bicyclic bet bromodomain inhibitors and uses thereof
HK40078733B (en) Bicyclic bet bromodomain inhibitors and uses thereof
EP3028703B1 (en) Piperidine derivatives as wnt signaling inhibitor
HK1261992B (en) Bicyclic bet bromodomain inhibitors and uses thereof
HK1261992A1 (en) Bicyclic bet bromodomain inhibitors and uses thereof
HK1230202B (en) Inhibitors of lysine specific demethylase-1
HK1230202A1 (en) Inhibitors of lysine specific demethylase-1

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)