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CN114728917A - 草酰胺类衍生物、其制备方法及其在医药上的应用 - Google Patents

草酰胺类衍生物、其制备方法及其在医药上的应用 Download PDF

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Publication number
CN114728917A
CN114728917A CN202080079342.0A CN202080079342A CN114728917A CN 114728917 A CN114728917 A CN 114728917A CN 202080079342 A CN202080079342 A CN 202080079342A CN 114728917 A CN114728917 A CN 114728917A
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phenyl
amino
mmol
tert
reaction
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CN114728917B (zh
Inventor
吴俊军
陆银锁
肖瑛
吕洋
周鹏
洪泽新
黄艺
王汝欢
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Shenzhen Salubris Pharmaceuticals Co Ltd
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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/56—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having carbon atoms of carboxamide groups bound to carbon atoms of carboxyl groups, e.g. oxamides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C07D257/06—Five-membered rings with nitrogen atoms directly attached to the ring carbon atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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

属于化学药物技术领域，涉及草酰胺类衍生物、其制备方法及其在医药上的应用。具体而言，提供式(I)的化合物或其立体异构体、互变异构体、药学上可接受的盐。这些化合物是选择性因子XIa(Factor XIa，简称FXIa)的抑制剂，还涉及包含这些化合物的药物组合物以及使用该化合物治疗血栓栓塞等疾病的药物中的用途。

Description

PCT国内申请，说明书已公开。

Claims (14)

  1. PCT国内申请，权利要求书已公开。
CN202080079342.0A 2019-12-04 2020-12-03 草酰胺类衍生物、其制备方法及其在医药上的应用 Active CN114728917B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019112271280 2019-12-04
CN201911227128 2019-12-04
PCT/CN2020/133493 WO2021110076A1 (zh) 2019-12-04 2020-12-03 草酰胺类衍生物、其制备方法及其在医药上的应用

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Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117480164B (zh) * 2020-12-11 2024-07-05 上海领泰生物医药科技有限公司 凝血因子XIa抑制剂及其制备方法和应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1745071A (zh) * 2002-12-24 2006-03-08 第一制药株式会社 新型乙二胺衍生物
US20100261645A1 (en) * 2007-09-21 2010-10-14 Sanofi-Aventis (carboxylalkylenephenyl)phenyloxamides, method for the production thereof and use of same as a medicament
CN102325528A (zh) * 2008-12-19 2012-01-18 第一三共株式会社 活化凝血因子X（FXa）抑制剂
US20130203758A1 (en) * 2012-02-06 2013-08-08 Bristol-Myers Squibb Company Compounds for the Treatment of Hepatitis C
WO2016180348A1 (zh) * 2015-05-14 2016-11-17 四川海思科制药有限公司 具有β2受体激动及M受体拮抗活性的含氮杂螺环衍生物及其在医药上的用途
CN107849019A (zh) * 2016-01-22 2018-03-27 四川海思科制药有限公司 一种氮杂环酰胺衍生物及其制备方法和在医药上的用途
CN108026083A (zh) * 2015-06-19 2018-05-11 百时美施贵宝公司 作为因子xia抑制剂的二酰胺大环
WO2019218956A1 (zh) * 2018-05-16 2019-11-21 深圳信立泰药业股份有限公司 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物

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Publication number Priority date Publication date Assignee Title
DE10117823A1 (de) * 2001-04-10 2002-10-17 Merck Patent Gmbh Oxalsäurederivate
EP1864982B1 (en) * 2005-03-31 2012-10-24 Daiichi Sankyo Company, Limited Triamine derivative

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1745071A (zh) * 2002-12-24 2006-03-08 第一制药株式会社 新型乙二胺衍生物
US20100261645A1 (en) * 2007-09-21 2010-10-14 Sanofi-Aventis (carboxylalkylenephenyl)phenyloxamides, method for the production thereof and use of same as a medicament
CN102325528A (zh) * 2008-12-19 2012-01-18 第一三共株式会社 活化凝血因子X（FXa）抑制剂
US20130203758A1 (en) * 2012-02-06 2013-08-08 Bristol-Myers Squibb Company Compounds for the Treatment of Hepatitis C
WO2016180348A1 (zh) * 2015-05-14 2016-11-17 四川海思科制药有限公司 具有β2受体激动及M受体拮抗活性的含氮杂螺环衍生物及其在医药上的用途
CN108026083A (zh) * 2015-06-19 2018-05-11 百时美施贵宝公司 作为因子xia抑制剂的二酰胺大环
CN107849019A (zh) * 2016-01-22 2018-03-27 四川海思科制药有限公司 一种氮杂环酰胺衍生物及其制备方法和在医药上的用途
WO2019218956A1 (zh) * 2018-05-16 2019-11-21 深圳信立泰药业股份有限公司 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
傅焕建，朱莉亚，林紫云: "烟酰胺类和吡啶丙烯酰胺类衍生物的合成及扩血管活性", 药学学报, vol. 01, no. 09, pages 715 - 720 *
李红伟，等: "一种抗凝血药物新型Xa因子抑制剂的合成", 广东化工, vol. 40, no. 11, pages 9 - 10 *
高娜娜，等: "利伐沙班衍生物的合成及Ⅹa因子抑制活性", 中国药科大学学报, vol. 15, no. 05, pages 1 - 7 *

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WO2021110076A1 (zh) 2021-06-10
CN114728917B (zh) 2023-12-08

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