CN110506044A - 一种brd4抑制剂及其制备和应用 - Google Patents

一种brd4抑制剂及其制备和应用 Download PDF

Info

Publication number
CN110506044A
CN110506044A CN201880024931.1A CN201880024931A CN110506044A CN 110506044 A CN110506044 A CN 110506044A CN 201880024931 A CN201880024931 A CN 201880024931A CN 110506044 A CN110506044 A CN 110506044A
Authority
CN
China
Prior art keywords
substituted
unsubstituted
group
compound
formula
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
CN201880024931.1A
Other languages
English (en)
Other versions
CN110506044B (zh
Inventor
赵玉军
陈德恒
郭德祥
严子琴
周飞龙
耿美玉
丁健
沈爱军
刘红椿
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 Institute of Materia Medica of CAS
Original Assignee
Shanghai Institute of Materia Medica of CAS
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 Institute of Materia Medica of CAS filed Critical Shanghai Institute of Materia Medica of CAS
Publication of CN110506044A publication Critical patent/CN110506044A/zh
Application granted granted Critical
Publication of CN110506044B publication Critical patent/CN110506044B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明涉及一类BRD4蛋白的小分子抑制剂,具体涉及一类具有三氮唑并氮杂结构的小分子化合物、其制备方法、药物组合物和在制备BRD4小分子抑制剂,或预防和/或治疗与BRD4相关的疾病,尤其是癌症,的药物中的用途。

Description

PCT国内申请,说明书已公开。

Claims (12)

  1. PCT国内申请,权利要求书已公开。
CN201880024931.1A 2017-04-13 2018-04-13 一种brd4抑制剂及其制备和应用 Active CN110506044B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710240864.4A CN108727380A (zh) 2017-04-13 2017-04-13 一种brd4抑制剂及其制备和应用
CN2017102408644 2017-04-13
PCT/CN2018/083098 WO2018188660A1 (zh) 2017-04-13 2018-04-13 一种brd4抑制剂及其制备和应用

Publications (2)

Publication Number Publication Date
CN110506044A true CN110506044A (zh) 2019-11-26
CN110506044B CN110506044B (zh) 2022-07-05

Family

ID=63792269

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201710240864.4A Pending CN108727380A (zh) 2017-04-13 2017-04-13 一种brd4抑制剂及其制备和应用
CN201880024931.1A Active CN110506044B (zh) 2017-04-13 2018-04-13 一种brd4抑制剂及其制备和应用

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201710240864.4A Pending CN108727380A (zh) 2017-04-13 2017-04-13 一种brd4抑制剂及其制备和应用

Country Status (2)

Country Link
CN (2) CN108727380A (zh)
WO (1) WO2018188660A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111518045A (zh) * 2019-02-02 2020-08-11 博诺康源(北京)药业科技有限公司 一种具有苯并七元环结构的化合物、其制备方法及用途
CN115043770B (zh) * 2022-07-21 2023-09-08 南京大学 一种吲哚/氮杂吲哚类化合物的光诱导合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011054844A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Condensed azepine derivatives as bromodomain inhibitors
CN102781943A (zh) * 2009-11-05 2012-11-14 葛兰素史密丝克莱恩有限责任公司 苯并二氮杂*溴结构域抑制剂
CN104781259A (zh) * 2012-09-28 2015-07-15 拜耳制药股份公司 抑制bet蛋白的5-芳基三唑并氮杂*

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011054844A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Condensed azepine derivatives as bromodomain inhibitors
CN102781943A (zh) * 2009-11-05 2012-11-14 葛兰素史密丝克莱恩有限责任公司 苯并二氮杂*溴结构域抑制剂
CN104781259A (zh) * 2012-09-28 2015-07-15 拜耳制药股份公司 抑制bet蛋白的5-芳基三唑并氮杂*

Also Published As

Publication number Publication date
CN108727380A (zh) 2018-11-02
WO2018188660A1 (zh) 2018-10-18
CN110506044B (zh) 2022-07-05

Similar Documents

Publication Publication Date Title
TWI736566B (zh) Tlr7/8拮抗劑及其用途
CN109803962B (zh) 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物
CN108347943B (zh) 乙肝核心蛋白调节剂
TWI825398B (zh) Glp-1 受體促效劑、包含該促效劑之醫藥組成物及其製備方法
CN104379574B (zh) 用于抑制abl1、abl2和bcr‑abl1的活性的苯甲酰胺衍生物
EP3057422B1 (en) Quinolinyl modulators of ror(gamma)t
TW201920094A (zh) 雜環化合物及其用途
CN115803030A (zh) 用于kras靶向降解的化合物和方法
EP3510025B1 (en) Heteroaryl inhibitors of pad4
CN113164761A (zh) α-1抗胰蛋白酶的调节剂
CN113286794A (zh) Kras突变蛋白抑制剂
TW201443023A (zh) 作爲rock抑制劑之酞□酮及異喹啉酮
WO2001023383A1 (fr) Composes de quinuclidine et medicaments contenant ces composes comme principe actif
TW201609725A (zh) 作為抗癌劑之新穎三環化合物
CN106459009A (zh) 丙肝病毒抑制剂及其制药用途
CN103619817A (zh) 新颖的二环含氮杂芳基tgr5受体调节剂
CN113302183A (zh) 环脲
JP2017527569A (ja) オレキシン−1受容体の阻害剤としての治療用化合物
TWI773718B (zh) 聚-adp核糖聚合酶(parp)抑制劑
WO2023059581A1 (en) Heterobifunctional compounds and their use in treating disease
CN101668747A (zh) 四氢异喹啉-1-酮衍生物或其盐
CN115413279A (zh) P2x3调节剂
EP3239142A1 (en) Condensed heterocyclic compound
CN110506044B (zh) 一种brd4抑制剂及其制备和应用
CN111801100A (zh) 用于治疗和预防肝癌的7-取代的磺亚氨酰基嘌呤酮化合物和衍生物

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