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CN114040908A - 一种凝血因子XIa抑制剂的晶型及其制备方法 - Google Patents

一种凝血因子XIa抑制剂的晶型及其制备方法 Download PDF

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Publication number
CN114040908A
CN114040908A CN202080042070.7A CN202080042070A CN114040908A CN 114040908 A CN114040908 A CN 114040908A CN 202080042070 A CN202080042070 A CN 202080042070A CN 114040908 A CN114040908 A CN 114040908A
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China
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degrees
compound
crystal form
ray powder
powder diffraction
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Pending
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CN202080042070.7A
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English (en)
Inventor
张�杰
董吉川
黄河
雷鑫
陈勇
王仲清
罗忠华
黄芳芳
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Sunshine Lake Pharma Co Ltd
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Sunshine Lake Pharma Co Ltd
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Publication of CN114040908A publication Critical patent/CN114040908A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams

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

Abstract

一种凝血因子XIa抑制剂的晶型及其制备方法,所述晶型的X射线粉末衍射图包含2θ角为6.9±0.2°,15.9±0.2°,21.8±0.2°,23.7±0.2°和28.2±0.2°的衍射峰。所述晶型具有较好的性能,稳定性高,可用于制备治疗心血管疾病的药物制剂。

Description

PCT国内申请,说明书已公开。

Claims (12)

  1. PCT国内申请,权利要求书已公开。
CN202080042070.7A 2019-06-25 2020-06-17 一种凝血因子XIa抑制剂的晶型及其制备方法 Pending CN114040908A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019105543308 2019-06-25
CN201910554330 2019-06-25
PCT/CN2020/096572 WO2020259366A1 (zh) 2019-06-25 2020-06-17 一种凝血因子XIa抑制剂的晶型及其制备方法

Publications (1)

Publication Number Publication Date
CN114040908A true CN114040908A (zh) 2022-02-11

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CN202080042070.7A Pending CN114040908A (zh) 2019-06-25 2020-06-17 一种凝血因子XIa抑制剂的晶型及其制备方法

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CN (1) CN114040908A (zh)
WO (1) WO2020259366A1 (zh)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999067215A1 (en) * 1998-06-25 1999-12-29 Bristol-Myers Squibb Company Amidino and guanidino azetidinone tryptase inhibitors
US20040180855A1 (en) * 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
JP2005095167A (ja) * 2003-08-26 2005-04-14 Mitsubishi Chemicals Corp 光学活性環状アミノ酸の製造方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999067215A1 (en) * 1998-06-25 1999-12-29 Bristol-Myers Squibb Company Amidino and guanidino azetidinone tryptase inhibitors
US20040180855A1 (en) * 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
JP2005095167A (ja) * 2003-08-26 2005-04-14 Mitsubishi Chemicals Corp 光学活性環状アミノ酸の製造方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
XINHUA QIAN, ET AL.: "A Stereoselective Synthesis of BMS-262084, an Azetidinone-Based Tryptase Inhibitor", J. ORG. CHEM. *

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WO2020259366A1 (zh) 2020-12-30

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Address after: 523808 No.1, Gongye North Road, Songshanhu Park, Dongguan City, Guangdong Province

Applicant after: Guangdong Dongyangguang Pharmaceutical Co.,Ltd.

Address before: 523808 Songshan Lake Science and Technology Industrial Park, Dongguan City, Guangdong Province

Applicant before: SUNSHINE LAKE PHARMA Co.,Ltd.