CN115996922A - Rho相关蛋白激酶抑制剂的盐、其固体形式及其制备方法和用途 - Google Patents

Rho相关蛋白激酶抑制剂的盐、其固体形式及其制备方法和用途 Download PDF

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CN115996922A
CN115996922A CN202180053323.5A CN202180053323A CN115996922A CN 115996922 A CN115996922 A CN 115996922A CN 202180053323 A CN202180053323 A CN 202180053323A CN 115996922 A CN115996922 A CN 115996922A
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China
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compound
cancer
salt
monohydrochloride
diffraction angles
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CN202180053323.5A
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English (en)
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赵焰平
王红军
冯泽旺
田娜娜
魏来
曹想荣
陈婕
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Beijing Tide Pharmaceutical Co Ltd
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Beijing Tide Pharmaceutical Co Ltd
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Publication of CN115996922A publication Critical patent/CN115996922A/zh
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    • 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
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • C07D403/14—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 three 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
    • A61K31/495—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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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

Abstract

本发明涉及(6‑(4‑((4‑(1H‑吡唑‑4‑基)苯基)氨基)嘧啶‑2‑基)‑1‑甲基‑1H‑吲哚‑2‑基)(3，3‑二氟氮杂环丁烷‑1‑基)甲酮(在下文中称作“化合物A”)的盐及其固体形式，制备所述固体形式的方法、包含所述固体形式的药物组合物，以及所述固体形式用作Rho相关蛋白激酶(ROCK)抑制剂，优选选择性ROCK2抑制剂的用途。

Description

PCT国内申请，说明书已公开。

Claims (10)

  1. PCT国内申请，权利要求书已公开。
CN202180053323.5A 2020-08-31 2021-08-30 Rho相关蛋白激酶抑制剂的盐、其固体形式及其制备方法和用途 Pending CN115996922A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2020112500 2020-08-31
CNPCT/CN2020/112500 2020-08-31
PCT/CN2021/115198 WO2022042712A1 (zh) 2020-08-31 2021-08-30 Rho相关蛋白激酶抑制剂的盐、其固体形式及其制备方法和用途

Publications (1)

Publication Number Publication Date
CN115996922A true CN115996922A (zh) 2023-04-21

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CN202180053323.5A Pending CN115996922A (zh) 2020-08-31 2021-08-30 Rho相关蛋白激酶抑制剂的盐、其固体形式及其制备方法和用途

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Country Link
US (1) US20230312530A1 (zh)
EP (1) EP4206194A1 (zh)
JP (1) JP2023539276A (zh)
KR (1) KR20230061444A (zh)
CN (1) CN115996922A (zh)
AU (1) AU2021332886A1 (zh)
CA (1) CA3191033A1 (zh)
IL (1) IL300938A (zh)
TW (1) TW202214606A (zh)
WO (1) WO2022042712A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN118019530A (zh) * 2021-09-17 2024-05-10 北京泰德制药股份有限公司 治疗病毒感染的方法
WO2023041026A1 (zh) * 2021-09-18 2023-03-23 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂或其溶剂合物的固体形式及其制备方法和用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019001572A1 (zh) * 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho 相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3932404A4 (en) * 2019-03-01 2022-11-30 Beijing Tide Pharmaceutical Co., Ltd. METHODS OF TREATMENT OF FATTY LIVER DISEASE AND/OR STEATOHEPATITIS
AU2020305979A1 (en) * 2019-06-25 2022-02-17 Beijing Tide Pharmaceutical Co., Ltd. Method for treating idiopathic pulmonary fibrosis

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019001572A1 (zh) * 2017-06-30 2019-01-03 北京泰德制药股份有限公司 Rho 相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途

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CA3191033A1 (en) 2022-03-03
AU2021332886A1 (en) 2023-05-11
AU2021332886A9 (en) 2024-05-23
WO2022042712A1 (zh) 2022-03-03
EP4206194A1 (en) 2023-07-05
JP2023539276A (ja) 2023-09-13
TW202214606A (zh) 2022-04-16
IL300938A (en) 2023-04-01
KR20230061444A (ko) 2023-05-08
US20230312530A1 (en) 2023-10-05

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