CN113631559A - 同时具有BET Bromodomain蛋白抑制和PD-L1基因调控作用的化合物 - Google Patents

同时具有BET Bromodomain蛋白抑制和PD-L1基因调控作用的化合物 Download PDF

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CN113631559A
CN113631559A CN202080019562.4A CN202080019562A CN113631559A CN 113631559 A CN113631559 A CN 113631559A CN 202080019562 A CN202080019562 A CN 202080019562A CN 113631559 A CN113631559 A CN 113631559A
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compound
isomer
pharmaceutically acceptable
acceptable salt
och
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CN113631559B (zh
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沈春莉
朱玉川
王廷
吴成德
陈曙辉
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Medshine Discovery Inc
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    • 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
    • C07D495/12—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 three hetero rings
    • C07D495/14—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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

一类同时具有BET Bromodomain蛋白抑制活性和调控PD‑L1基因表达的化合物，及其在制备治疗与BET Bromodomain蛋白抑制剂及PD‑L1基因表达相关肿瘤疾病的药物中的应用。具体公开了式(1)所示化合物、其异构体及其药学上可接受的盐。

Description

PCT国内申请，说明书已公开。

Claims (19)

  1. PCT国内申请，权利要求书已公开。
CN202080019562.4A 2019-03-07 2020-03-06 同时具有BET Bromodomain蛋白抑制和PD-L1基因调控作用的化合物 Active CN113631559B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910172886 2019-03-07
CN2019101728860 2019-03-07
PCT/CN2020/078187 WO2020177762A1 (zh) 2019-03-07 2020-03-06 同时具有BET Bromodomain蛋白抑制和PD-L1基因调控作用的化合物

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CN113631559A true CN113631559A (zh) 2021-11-09
CN113631559B CN113631559B (zh) 2023-05-23

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US (1) US20220177490A1 (zh)
EP (1) EP3936507A4 (zh)
JP (1) JP7292400B2 (zh)
CN (1) CN113631559B (zh)
WO (1) WO2020177762A1 (zh)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022048685A1 (zh) * 2020-09-07 2022-03-10 南京明德新药研发有限公司 苯并四氢呋喃肟类化合物的晶型及其制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5712274A (en) * 1993-09-16 1998-01-27 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and their pharmaceutical use
CN1237180A (zh) * 1996-09-13 1999-12-01 吉富制药株式会社 噻吩并－三唑并二氮杂䓬化合物及其医药用途
CN101910182A (zh) * 2007-12-28 2010-12-08 田边三菱制药株式会社 抗癌剂
WO2011054845A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
WO2018144789A1 (en) * 2017-02-03 2018-08-09 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2016510039A (ja) 2013-02-28 2016-04-04 ワシントン・ユニバーシティＷａｓｈｉｎｇｔｏｎ Ｕｎｉｖｅｒｓｉｔｙ ブロモドメイン阻害剤によるヒトサイトメガロウイルス感染および疾患の治療方法
UA123946C2 (uk) 2015-09-11 2021-06-30 Дана-Фарбер Кенсер Інстітьют, Інк. Ацетамідтієнотриазолодіазепіни й шляхи їх застосування
US20190085404A1 (en) 2016-03-04 2019-03-21 The Board Of Trustees Of The Leland Stanford Junior University Methods of identifying and treating immune checkpoint inhibitor-responsive neoplasms and cells, transgenic animals and kits for use therein
EP3686204A4 (en) * 2017-09-22 2021-05-19 CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. THIENODIAZEPIN DERIVATIVES AND THEIR USES

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5712274A (en) * 1993-09-16 1998-01-27 Yoshitomi Pharmaceutical Industries, Ltd. Thienotriazolodiazepine compounds and their pharmaceutical use
CN1237180A (zh) * 1996-09-13 1999-12-01 吉富制药株式会社 噻吩并－三唑并二氮杂䓬化合物及其医药用途
CN101910182A (zh) * 2007-12-28 2010-12-08 田边三菱制药株式会社 抗癌剂
WO2011054845A1 (en) * 2009-11-05 2011-05-12 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
WO2018144789A1 (en) * 2017-02-03 2018-08-09 The Regents Of The University Of Michigan Fused 1,4-diazepines as bet bromodomain inhibitors

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Publication number Publication date
US20220177490A1 (en) 2022-06-09
WO2020177762A1 (zh) 2020-09-10
CN113631559B (zh) 2023-05-23
JP2022524113A (ja) 2022-04-27
EP3936507A4 (en) 2022-11-23
EP3936507A1 (en) 2022-01-12
JP7292400B2 (ja) 2023-06-16

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