CN112533929A - 吲哚类大环衍生物、其制备方法及其在医药上的应用 - Google Patents

吲哚类大环衍生物、其制备方法及其在医药上的应用 Download PDF

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Publication number
CN112533929A
CN112533929A CN201980049788.6A CN201980049788A CN112533929A CN 112533929 A CN112533929 A CN 112533929A CN 201980049788 A CN201980049788 A CN 201980049788A CN 112533929 A CN112533929 A CN 112533929A
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compound
general formula
mixture
pharmaceutically acceptable
tautomer
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CN201980049788.6A
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CN112533929B (zh
Inventor
张国宝
费洪博
张晓敏
胡伟民
贺峰
陶维康
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Fujian Shengdi Pharmaceutical Co ltd
Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

涉及吲哚类大环衍生物、其制备方法及其在医药上的应用。具体而言，涉及一种通式(IM)所示的吲哚类大环衍生物、其制备方法及含有该衍生物的药物组合物以及其作为治疗剂，特别是作为MCL‑1抑制剂的用途。其中通式(IM)的各取代基与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (34)

  1. PCT国内申请，权利要求书已公开。
CN201980049788.6A 2018-09-30 2019-09-27 吲哚类大环衍生物、其制备方法及其在医药上的应用 Active CN112533929B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN2018111562176 2018-09-30
CN201811156217 2018-09-30
CN2019102273595 2019-03-25
CN201910227359 2019-03-25
PCT/CN2019/108322 WO2020063792A1 (zh) 2018-09-30 2019-09-27 吲哚类大环衍生物、其制备方法及其在医药上的应用

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CN112533929A true CN112533929A (zh) 2021-03-19
CN112533929B CN112533929B (zh) 2022-09-16

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US (1) US20220041623A1 (zh)
EP (1) EP3858840A4 (zh)
JP (1) JP2022503896A (zh)
KR (1) KR20210070312A (zh)
CN (1) CN112533929B (zh)
AU (1) AU2019347963A1 (zh)
BR (1) BR112021004805A2 (zh)
CA (1) CA3113917A1 (zh)
MX (1) MX2021003655A (zh)
TW (1) TW202014423A (zh)
WO (1) WO2020063792A1 (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114641481A (zh) * 2019-06-21 2022-06-17 詹森药业有限公司 Mcl-1的大环抑制剂
CN115151551A (zh) * 2020-02-21 2022-10-04 詹森药业有限公司 作为mcl-1抑制剂的大环吲哚衍生物
CN115151551B (zh) * 2020-02-21 2024-10-25 詹森药业有限公司 作为mcl-1抑制剂的大环吲哚衍生物

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11691989B2 (en) 2018-11-22 2023-07-04 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic indoles as Mcl-1 inhibitors
BR112022009142A2 (pt) 2019-11-21 2022-07-26 Janssen Pharmaceutica Nv Derivados de indol macrocíclicos como inibidores de mcl-1
BR112022009754A2 (pt) 2019-11-21 2022-08-09 Janssen Pharmaceutica Nv Derivados macrocíclicos de sulfonila como inibidores de mcl-1
EP4051685A4 (en) * 2019-12-18 2024-01-10 Zeno Management, Inc. MACROCYCLIC COMPOUNDS
WO2021197295A1 (zh) * 2020-03-30 2021-10-07 江苏恒瑞医药股份有限公司 一种吲哚类大环衍生物的结晶形式及其制备方法
EP4157852A1 (en) 2020-05-29 2023-04-05 JANSSEN Pharmaceutica NV Macrocyclic 7-pyrazol-5-yl-indole derivatives as inhibitors of mcl-1
JP2023530148A (ja) 2020-06-19 2023-07-13 ヤンセン ファーマシューティカ エヌ．ベー． Ｍｃｌ－１阻害剤としてのｎ－結合大環状４－（ピラゾール－５－イル）－インドール誘導体
US20230234969A1 (en) 2020-06-19 2023-07-27 Janssen Pharmaceutica Nv N-linked macrocyclic 7-(pyrazol-5-yl)-indole derivatives as inhibiors of mcl-1
BR112023000212A2 (pt) 2020-07-08 2023-01-31 Janssen Pharmaceutica Nv Éter macrocíclico contendo derivados de indol como inibidores de mcl-1
CA3200758A1 (en) 2020-12-17 2022-06-23 Janssen Pharmaceutica Nv Branched macrocyclic 4-(pyrazol-5-yl)-indole derivatives as inhibitors of mcl-1
EP4291564A1 (en) 2021-02-12 2023-12-20 JANSSEN Pharmaceutica NV Macrocyclic 1,3-bridged 6-chloro-7-pyrazol-4-yl-1h-indole-2-carboxylate and 6-chloro-7-pyrimidin-5-yl-1h-indole-2-carboxylate derivatives as mcl-1 inhibitors for the treatment of cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101711235A (zh) * 2007-04-16 2010-05-19 雅培制药有限公司 7-未取代的吲哚mcl-1抑制剂
US20170305926A1 (en) * 2016-04-22 2017-10-26 Astrazeneca Ab Mcl-1 inhibitors and methods of use thereof
WO2018178226A1 (en) * 2017-03-31 2018-10-04 Astrazeneca Ab Mcl-1 inhibitors and methods of use thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2705599T3 (es) * 2007-04-16 2019-03-26 Abbvie Inc Indoles sustituidos en la posición 7 como inhibidores de mcl-1
WO2017156181A1 (en) 2016-03-09 2017-09-14 Raze Therapeutics, Inc. 3-phosphoglycerate dehydrogenase inhibitors and uses thereof
US11691989B2 (en) * 2018-11-22 2023-07-04 Ascentage Pharma (Suzhou) Co., Ltd. Macrocyclic indoles as Mcl-1 inhibitors
BR112021025732A2 (pt) * 2019-06-21 2022-04-12 Janssen Pharmaceutica Nv Inibidores macrocíclicos de mcl-1

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101711235A (zh) * 2007-04-16 2010-05-19 雅培制药有限公司 7-未取代的吲哚mcl-1抑制剂
US20170305926A1 (en) * 2016-04-22 2017-10-26 Astrazeneca Ab Mcl-1 inhibitors and methods of use thereof
WO2018178226A1 (en) * 2017-03-31 2018-10-04 Astrazeneca Ab Mcl-1 inhibitors and methods of use thereof

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114641481A (zh) * 2019-06-21 2022-06-17 詹森药业有限公司 Mcl-1的大环抑制剂
CN114641481B (zh) * 2019-06-21 2024-07-30 詹森药业有限公司 Mcl-1的大环抑制剂
CN115151551A (zh) * 2020-02-21 2022-10-04 詹森药业有限公司 作为mcl-1抑制剂的大环吲哚衍生物
CN115151551B (zh) * 2020-02-21 2024-10-25 詹森药业有限公司 作为mcl-1抑制剂的大环吲哚衍生物

Also Published As

Publication number Publication date
KR20210070312A (ko) 2021-06-14
EP3858840A4 (en) 2022-05-04
AU2019347963A1 (en) 2021-05-27
BR112021004805A2 (pt) 2021-06-01
TW202014423A (zh) 2020-04-16
WO2020063792A1 (zh) 2020-04-02
JP2022503896A (ja) 2022-01-12
US20220041623A1 (en) 2022-02-10
CN112533929B (zh) 2022-09-16
EP3858840A1 (en) 2021-08-04
CA3113917A1 (en) 2020-04-02
MX2021003655A (es) 2021-06-23

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