CN111263763A - 一种三并环化合物的结晶 - Google Patents

一种三并环化合物的结晶 Download PDF

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Publication number
CN111263763A
CN111263763A CN201880053356.8A CN201880053356A CN111263763A CN 111263763 A CN111263763 A CN 111263763A CN 201880053356 A CN201880053356 A CN 201880053356A CN 111263763 A CN111263763 A CN 111263763A
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crystal
compound
formula
ray powder
organic solvent
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CN201880053356.8A
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CN111263763B (zh
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刘世岚
王大海
梁贵柏
汪洪林
胡国平
黎健
其他发明人请求不公开姓名
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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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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)
  • Immunology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本申请涉及一种三并环化合物的结晶，具体涉及(S)‑8‑(4,4‑二氟环己基)‑8H‑噻吩并[3,4]吡咯并[1,5‑a]咪唑的晶体、其制备方法、其晶体组合物、药物组合物及其用途。本申请式I化合物的晶体的X‑射线粉末衍射光谱用2θ值表示在约11.49°、15.05°、20.14°、21.53°或21.79°处有衍射峰。本申请式I化合物的晶体在物性、安全性及代谢稳定性方面都较高且有较好的IDO抑制作用，其药用价值较高。

Description

PCT国内申请，说明书已公开。

Claims (15)

  1. PCT国内申请，权利要求书已公开。
CN201880053356.8A 2017-08-18 2018-08-17 一种三并环化合物的结晶 Active CN111263763B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2017107142473 2017-08-18
CN201710714247 2017-08-18
PCT/CN2018/100988 WO2019034139A1 (zh) 2017-08-18 2018-08-17 一种三并环化合物的结晶

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CN111263763A true CN111263763A (zh) 2020-06-09
CN111263763B CN111263763B (zh) 2021-02-19

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US (1) US11236107B2 (zh)
EP (1) EP3670518A4 (zh)
CN (1) CN111263763B (zh)
WO (1) WO2019034139A1 (zh)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103547579A (zh) * 2011-04-15 2014-01-29 新联基因公司 用作ido抑制剂的稠合咪唑衍生物
WO2016059412A1 (en) * 2014-10-15 2016-04-21 Redx Pharma Plc 6,7-heterocyclic fused 5h-pyrrolo[1,2-c]imidazole derivatives and their use as indoleamine 2,3-dioxygenase (ido) and/or tryptophan 2,3-dioxygenase (td02) modulators
CN105884828A (zh) * 2015-02-16 2016-08-24 上海迪诺医药科技有限公司 多环化合物、其药物组合物及应用
WO2017140274A1 (zh) * 2016-02-19 2017-08-24 正大天晴药业集团股份有限公司 作为免疫调节剂的三并环化合物

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103547579A (zh) * 2011-04-15 2014-01-29 新联基因公司 用作ido抑制剂的稠合咪唑衍生物
WO2016059412A1 (en) * 2014-10-15 2016-04-21 Redx Pharma Plc 6,7-heterocyclic fused 5h-pyrrolo[1,2-c]imidazole derivatives and their use as indoleamine 2,3-dioxygenase (ido) and/or tryptophan 2,3-dioxygenase (td02) modulators
CN105884828A (zh) * 2015-02-16 2016-08-24 上海迪诺医药科技有限公司 多环化合物、其药物组合物及应用
WO2017140274A1 (zh) * 2016-02-19 2017-08-24 正大天晴药业集团股份有限公司 作为免疫调节剂的三并环化合物

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EP3670518A4 (en) 2021-01-06
WO2019034139A1 (zh) 2019-02-21
US11236107B2 (en) 2022-02-01
EP3670518A1 (en) 2020-06-24
CN111263763B (zh) 2021-02-19
US20200255449A1 (en) 2020-08-13

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