CN111757871A - 一种Caspase抑制剂的结晶 - Google Patents

一种Caspase抑制剂的结晶 Download PDF

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Publication number
CN111757871A
CN111757871A CN201980016202.6A CN201980016202A CN111757871A CN 111757871 A CN111757871 A CN 111757871A CN 201980016202 A CN201980016202 A CN 201980016202A CN 111757871 A CN111757871 A CN 111757871A
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compound
formula
crystalline
ray powder
crystal
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CN201980016202.6A
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CN111757871B (zh
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吴松亮
牟剑锋
贺海鹰
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本申请涉及一种caspase抑制剂的结晶，更具体而言涉及(S)‑3‑((S)‑2‑(5‑(2‑氯苯基)异噁唑‑3‑甲酰胺基)丙酰胺基)‑4‑氧代‑5‑(2,3,5,6‑四氟苯氧基)戊酸的结晶，其制备方法、其结晶组合物、药物组合物及其用途。本申请式Ⅰ‑A化合物的结晶稳定性高、吸湿性小，在物理性质、安全性及代谢稳定性方面具备优势，有较高的成药价值。

Description

PCT国内申请，说明书已公开。

Claims (32)

  1. PCT国内申请，权利要求书已公开。
CN201980016202.6A 2018-03-13 2019-03-13 一种Caspase抑制剂的结晶 Active CN111757871B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201810206043 2018-03-13
CN2018102060433 2018-03-13
CN2018108035810 2018-07-20
CN201810803581 2018-07-20
PCT/CN2019/077939 WO2019174589A1 (zh) 2018-03-13 2019-03-13 一种Caspase抑制剂的结晶

Publications (2)

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CN111757871A true CN111757871A (zh) 2020-10-09
CN111757871B CN111757871B (zh) 2022-04-12

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CN201980016202.6A Active CN111757871B (zh) 2018-03-13 2019-03-13 一种Caspase抑制剂的结晶

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US (1) US11091450B2 (zh)
EP (1) EP3766873A4 (zh)
CN (1) CN111757871B (zh)
AU (1) AU2019233195A1 (zh)
CA (1) CA3093728A1 (zh)
WO (1) WO2019174589A1 (zh)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1313846A (zh) * 1998-07-02 2001-09-19 伊邓药品公司 作为ICE/ced－3族半胱氨酸蛋白酶抑制剂的C端修饰的草氨酰二肽

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6184244B1 (en) 1996-12-16 2001-02-06 Idun Pharmaceuticals, Inc. C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases
AU755273B2 (en) * 1998-03-16 2002-12-05 Cytovia, Inc. Dipeptide caspase inhibitors and the use thereof
WO2017053864A1 (en) * 2015-09-23 2017-03-30 Intracellular Technologies, Llc Cysteine protease inhibitors
EP3456711A4 (en) * 2016-05-11 2019-10-16 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREFOR
US11434212B2 (en) * 2017-01-23 2022-09-06 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Bicyclic compound as a caspase inhibitor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1313846A (zh) * 1998-07-02 2001-09-19 伊邓药品公司 作为ICE/ced－3族半胱氨酸蛋白酶抑制剂的C端修饰的草氨酰二肽

Also Published As

Publication number Publication date
WO2019174589A1 (zh) 2019-09-19
CN111757871B (zh) 2022-04-12
US11091450B2 (en) 2021-08-17
EP3766873A1 (en) 2021-01-20
AU2019233195A1 (en) 2020-09-24
CA3093728A1 (en) 2019-09-19
US20210002235A1 (en) 2021-01-07
EP3766873A4 (en) 2021-12-15

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