CN113330013A - 杂环化合物盐及其应用 - Google Patents

杂环化合物盐及其应用 Download PDF

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CN113330013A
CN113330013A CN202080008327.7A CN202080008327A CN113330013A CN 113330013 A CN113330013 A CN 113330013A CN 202080008327 A CN202080008327 A CN 202080008327A CN 113330013 A CN113330013 A CN 113330013A
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formula
hydrate
salt
ray powder
powder diffraction
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CN113330013B (zh
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孙晓伟
张倩如
吕硕
张红芬
高园
杨汉煜
郑利刚
刘喜宝
吴希美
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CSPC Zhongqi Pharmaceutical Technology Shijiazhuang Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pulmonology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Otolaryngology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)

Abstract

本发明提供式(A)所示杂环化合物药学上可接受的盐或者所述盐的水合物，所述药学上可接受的盐选自碱金属盐。发明人意外地发现，三种盐中，特别是钠盐、锂盐及两者水合物的溶解度和溶出度相对于式A化合物有明显改善，因此相对于式A化合物更易于成药。本发明还提供式A所示杂环化合物、水合物、其药学上可接受的碱金属盐或者所述碱金属盐的水合物在制备治疗急性肺损伤或急性呼吸窘迫综合征药物中的用途。实验结果表明，上述化合物通过抑制巨噬细胞和嗜中性粒细胞向肺部的渗透，降低肺血管通透性，减少促炎性细胞因子和细胞因子趋化因子的产生和促进IL‑10的产生，极大地缓解了由香烟烟雾CS诱导或LPS诱导的急性肺损伤或急性呼吸窘迫综合征。
Figure DDA0003152551910000011

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。
CN202080008327.7A 2019-01-10 2020-01-10 杂环化合物盐及其应用 Active CN113330013B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201910024238 2019-01-10
CN2019100242380 2019-01-10
CN2019104310264 2019-05-22
CN201910431026 2019-05-22
PCT/CN2020/071515 WO2020143793A1 (zh) 2019-01-10 2020-01-10 杂环化合物盐及其应用

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CN113330013A true CN113330013A (zh) 2021-08-31
CN113330013B CN113330013B (zh) 2022-12-27

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US (1) US20220098197A1 (zh)
EP (1) EP3909952A4 (zh)
JP (1) JP2022517610A (zh)
CN (1) CN113330013B (zh)
WO (1) WO2020143793A1 (zh)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101896178A (zh) * 2007-10-10 2010-11-24 凯米科技公司 作为crth2受体拮抗剂的杂环化合物
CN101932571A (zh) * 2008-01-18 2010-12-29 奥克萨根有限公司 具有crth2拮抗活性的化合物
US20130216552A1 (en) * 2010-07-12 2013-08-22 Ironwood Pharmaceuticals, Inc. Crth2 modulators

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WO1995015973A1 (en) 1993-12-06 1995-06-15 Cytel Corporation Cs-1 peptidomimetics, compositions and methods of using the same
US5510332A (en) 1994-07-07 1996-04-23 Texas Biotechnology Corporation Process to inhibit binding of the integrin α4 62 1 to VCAM-1 or fibronectin and linear peptides therefor
WO1996001644A1 (en) 1994-07-11 1996-01-25 Athena Neurosciences, Inc. Inhibitors of leukocyte adhesion
US5811391A (en) 1994-08-25 1998-09-22 Cytel Corporation Cyclic CS-1 peptidomimetics, compositions and methods of using same
GB9524630D0 (en) 1994-12-24 1996-01-31 Zeneca Ltd Chemical compounds
US6306840B1 (en) 1995-01-23 2001-10-23 Biogen, Inc. Cell adhesion inhibitors
WO1996031206A2 (en) 1995-04-07 1996-10-10 Warner-Lambert Company Flavones and coumarins as agents for the treatment of atherosclerosis
WO1996040781A1 (en) 1995-06-07 1996-12-19 Tanabe Seiyaku Co., Ltd. CYCLIC PEPTIDE INHIBITORS OF β1 AND β2 INTEGRIN-MEDIATED ADHESION
EP0842195A1 (en) 1995-07-06 1998-05-20 Zeneca Limited Peptide inhibitors of fibronectine
US6248713B1 (en) 1995-07-11 2001-06-19 Biogen, Inc. Cell adhesion inhibitors
US20020048610A1 (en) * 2000-01-07 2002-04-25 Cima Michael J. High-throughput formation, identification, and analysis of diverse solid-forms
DE10153737A1 (de) * 2001-10-31 2003-05-28 Boehringer Ingelheim Pharma Kristallines Natriumsalz des Telmisartans, Verfahren zu dessen Herstellung und dessen Verwendung zur Herstellung eines Arzneimittels

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101896178A (zh) * 2007-10-10 2010-11-24 凯米科技公司 作为crth2受体拮抗剂的杂环化合物
CN101932571A (zh) * 2008-01-18 2010-12-29 奥克萨根有限公司 具有crth2拮抗活性的化合物
US20130216552A1 (en) * 2010-07-12 2013-08-22 Ironwood Pharmaceuticals, Inc. Crth2 modulators

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EP3909952A1 (en) 2021-11-17
WO2020143793A1 (zh) 2020-07-16
EP3909952A4 (en) 2023-01-25
US20220098197A1 (en) 2022-03-31
CN113330013B (zh) 2022-12-27

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