[go: up one dir, main page]

CN114401964A - 一类具有brd4抑制活性的化合物、其制备方法及用途 - Google Patents

一类具有brd4抑制活性的化合物、其制备方法及用途 Download PDF

Info

Publication number
CN114401964A
CN114401964A CN202080062423.XA CN202080062423A CN114401964A CN 114401964 A CN114401964 A CN 114401964A CN 202080062423 A CN202080062423 A CN 202080062423A CN 114401964 A CN114401964 A CN 114401964A
Authority
CN
China
Prior art keywords
substituted
unsubstituted
alkyl
group
halogen
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.)
Granted
Application number
CN202080062423.XA
Other languages
English (en)
Other versions
CN114401964B (zh
Inventor
夏林
耿美玉
李乐平
丁健
沈爱军
刘红椿
杨浩然
李亚磊
张敏敏
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.)
Shanghai Haihe Pharmaceutical Co Ltd
Original Assignee
Shanghai Haihe Pharmaceutical Co Ltd
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 Shanghai Haihe Pharmaceutical Co Ltd filed Critical Shanghai Haihe Pharmaceutical Co Ltd
Publication of CN114401964A publication Critical patent/CN114401964A/zh
Application granted granted Critical
Publication of CN114401964B publication Critical patent/CN114401964B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • 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
    • A61K31/4355—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 oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • 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
    • A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

本发明公开了一种具有BRD4抑制活性的化合物、其制备方法及用途。本发明的具有BRD4抑制活性的化合物，结构如式I所示，各取代基的定义如说明书和权利要求书所述。本发明的化合物，具有很高的溴结构域蛋白抑制活性，特别是靶向BRD4的抑制活性，可用于治疗或/和预防由溴结构域蛋白介导的相关疾病。

Description

PCT国内申请，说明书已公开。

Claims (11)

  1. PCT国内申请，权利要求书已公开。
CN202080062423.XA 2019-10-08 2020-09-24 一类具有brd4抑制活性的化合物、其制备方法及用途 Active CN114401964B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019109513693 2019-10-08
CN201910951369.3A CN112625036A (zh) 2019-10-08 2019-10-08 一类具有brd4抑制活性的化合物、其制备方法及用途
PCT/CN2020/117478 WO2021068755A1 (zh) 2019-10-08 2020-09-24 一类具有brd4抑制活性的化合物、其制备方法及用途

Publications (2)

Publication Number Publication Date
CN114401964A true CN114401964A (zh) 2022-04-26
CN114401964B CN114401964B (zh) 2024-10-01

Family

ID=75283242

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201910951369.3A Pending CN112625036A (zh) 2019-10-08 2019-10-08 一类具有brd4抑制活性的化合物、其制备方法及用途
CN202080062423.XA Active CN114401964B (zh) 2019-10-08 2020-09-24 一类具有brd4抑制活性的化合物、其制备方法及用途

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201910951369.3A Pending CN112625036A (zh) 2019-10-08 2019-10-08 一类具有brd4抑制活性的化合物、其制备方法及用途

Country Status (10)

Country Link
US (1) US20240150343A1 (zh)
EP (1) EP4043462A4 (zh)
JP (1) JP7405468B2 (zh)
KR (1) KR20220110175A (zh)
CN (2) CN112625036A (zh)
AU (1) AU2020362763B2 (zh)
IL (1) IL291947A (zh)
MX (1) MX2022004143A (zh)
TW (1) TWI864112B (zh)
WO (1) WO2021068755A1 (zh)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
CN115667237A (zh) * 2020-07-17 2023-01-31 成都苑东生物制药股份有限公司 作为bet抑制剂的新型杂环化合物
CN113121531B (zh) * 2021-04-20 2023-06-13 上海药明康德新药开发有限公司 N杂吲哚类化合物、其合成方法和医药上的用途
WO2022226172A1 (en) * 2021-04-21 2022-10-27 The Regents Of The University Of California Compositions and methods for treating neurodegenerative diseases
CN113402515B (zh) * 2021-05-12 2022-05-27 四川大学华西医院 一种吲哚类化合物及其制备方法和用途
JP2024523491A (ja) 2021-06-29 2024-06-28 タイ セラピューティクス リミテッド がんの治療に有用なピロロピリドン誘導体
CN117050074B (zh) * 2022-05-05 2025-08-12 中国药科大学 一类吡啶联咪唑并吡啶化合物及其制备方法与用途
CN115819412B (zh) * 2022-05-30 2025-03-14 成都苑东生物制药股份有限公司 一种n-杂环bet溴结构域抑制剂的合成方法及其中间体
WO2025014200A1 (ko) * 2023-07-07 2025-01-16 주식회사 티움바이오 화합물 및 이를 포함하는 약학 조성물

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014206150A1 (en) * 2013-06-28 2014-12-31 Abbvie Inc. Bromodomain inhibitors
WO2015081203A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
CN107108614A (zh) * 2014-11-10 2017-08-29 基因泰克公司 作为布罗莫结构域抑制剂的取代的吡咯并吡啶
WO2018188047A1 (en) * 2017-04-14 2018-10-18 Abbvie Inc. Bromodomain inhibitors
CN109071534A (zh) * 2016-04-15 2018-12-21 艾伯维公司 布罗莫结构域抑制剂

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI339206B (en) * 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
JPWO2013125543A1 (ja) * 2012-02-20 2015-07-30 武田薬品工業株式会社 複素環化合物
EP2920183B1 (en) * 2012-11-14 2017-03-08 Glaxosmithkline LLC Thieno[3,2-c]pyridin-4(5h)-ones as bet inhibitors
WO2014125408A2 (en) * 2013-02-12 2014-08-21 Aurigene Discovery Technologies Limited Substituted 1h-pyrrolopyridinone derivatives as kinase inhibitors
BR112015022782A2 (pt) * 2013-03-14 2017-07-18 Glaxosmithkline Ip No 2 Ltd composto, composição farmacêutica, combinação, e, uso de um composto
TWI527811B (zh) * 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
US8975417B2 (en) * 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
EP3640241B1 (en) * 2013-10-18 2022-09-28 Celgene Quanticel Research, Inc. Bromodomain inhibitors
US9315501B2 (en) * 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
WO2015081246A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
PL3674302T3 (pl) * 2014-04-23 2023-07-24 Incyte Holdings Corporation 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET
WO2016077375A1 (en) * 2014-11-10 2016-05-19 Genentech, Inc. Bromodomain inhibitors and uses thereof
WO2016123391A1 (en) * 2015-01-29 2016-08-04 Genentech, Inc. Therapeutic compounds and uses thereof
CN108069958A (zh) * 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用
CN110167939B (zh) * 2017-01-11 2021-12-31 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
AU2018277520B2 (en) * 2017-05-31 2022-03-17 Chemocentryx, Inc. 6-5 fused rings as C5a inhibitors
EP3641762B1 (en) * 2017-06-20 2026-02-18 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
TWI713952B (zh) * 2017-12-20 2020-12-21 大陸商貝達藥業股份有限公司 作為溴結構域蛋白質抑制劑的化合物和組合物
CN112236172A (zh) * 2018-01-30 2021-01-15 福宏治疗公司 用于治疗病症的方法和化合物
WO2019151269A1 (ja) * 2018-01-31 2019-08-08 武田薬品工業株式会社 複素環化合物
WO2019153080A1 (en) * 2018-02-06 2019-08-15 Ontario Institute For Cancer Research (Oicr) Inhibitors of the bcl6 btb domain protein-protein interaction and uses thereof
CN110305123B (zh) * 2018-03-27 2021-12-10 海创药业股份有限公司 一种含有金刚烷的化合物及其在治疗癌症中的用途
GB201905721D0 (en) * 2019-04-24 2019-06-05 Univ Dundee Compounds

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014206150A1 (en) * 2013-06-28 2014-12-31 Abbvie Inc. Bromodomain inhibitors
WO2015081203A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
CN107108614A (zh) * 2014-11-10 2017-08-29 基因泰克公司 作为布罗莫结构域抑制剂的取代的吡咯并吡啶
CN109071534A (zh) * 2016-04-15 2018-12-21 艾伯维公司 布罗莫结构域抑制剂
WO2018188047A1 (en) * 2017-04-14 2018-10-18 Abbvie Inc. Bromodomain inhibitors

Also Published As

Publication number Publication date
KR20220110175A (ko) 2022-08-05
EP4043462A4 (en) 2023-11-01
MX2022004143A (es) 2022-07-21
TWI864112B (zh) 2024-12-01
US20240150343A1 (en) 2024-05-09
AU2020362763A1 (en) 2022-04-28
CN114401964B (zh) 2024-10-01
WO2021068755A1 (zh) 2021-04-15
CN112625036A (zh) 2021-04-09
EP4043462A1 (en) 2022-08-17
JP7405468B2 (ja) 2023-12-26
CA3156547A1 (en) 2021-04-15
AU2020362763B2 (en) 2024-02-15
TW202115061A (zh) 2021-04-16
IL291947A (en) 2022-06-01
JP2022551299A (ja) 2022-12-08

Similar Documents

Publication Publication Date Title
CN114401964A (zh) 一类具有brd4抑制活性的化合物、其制备方法及用途
CN114269746A (zh) 一种螺芳环化合物、其制备及应用
CN109715626A (zh) 作为fgfr抑制剂的杂环化合物
CN114222743A (zh) 氧代六元环并嘧啶类化合物，其制法与医药上的用途
CN109983007A (zh) 酰胺类衍生物抑制剂及其制备方法和应用
JP2019522055A5 (zh)
CN105636951A (zh) 酰胺类衍生物及其可药用盐、其制备方法及其在医药上的应用
CN114072396A (zh) 作为dna-pk抑制剂的喹啉和噌啉衍生物
JP2004502756A5 (zh)
RU2019106484A (ru) Гетероциклическое соединение
CN114555588A (zh) 作为axl抑制剂的喹唑啉类化合物
JP2020510091A5 (zh)
CA2430273A1 (en) Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicament, and pharmaceutical preparations comprising them
RU2016110755A (ru) Соединение, ингибирующее активности киназ ВТК и/или JAK3
CA2694270A1 (en) Substituted aryloxazoles and the use thereof
RU2019100164A (ru) Гетероциклическое соединение, используемое как ингибитор fgfr
JP2014503574A5 (zh)
CA2687265A1 (en) P70 s6 kinase inhibitors
CA2436891A1 (en) Ortho-substituted nitrogen-containing bisaryl compounds used as potassium channel inhibitors
MX2020008570A (es) Inhibidores de arginasa y sus metodos de uso.
RU2018111106A (ru) Производные карбоксизамещенных (гетеро)ароматических колец, способ их получения и применение
SA523442662B1 (ar) Apol1 مثبطات لـ وطرق استخدامها
JP2013542267A5 (zh)
CN110267954A (zh) 苯胺取代的1,2-二氢吡咯并[3,4-c]吡啶/嘧啶-3-酮衍生物及用途
CN112135826A (zh) 氨基降茨烷衍生物及其制备方法与应用

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
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40073468

Country of ref document: HK

CB03 Change of inventor or designer information
CB03 Change of inventor or designer information

Inventor after: Xia Lin

Inventor after: Li Leping

Inventor after: Yang Haoran

Inventor before: Xia Lin

Inventor before: Geng Meiyu

Inventor before: Li Leping

Inventor before: Ding Jian

Inventor before: Shen Aijun

Inventor before: Liu Hongchun

Inventor before: Yang Haoran

Inventor before: Li Yalei

Inventor before: Zhang Minmin

GR01 Patent grant
GR01 Patent grant