CN108137549B - 取代的甘氨酸衍生的fxia抑制剂 - Google Patents

取代的甘氨酸衍生的fxia抑制剂 Download PDF

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CN108137549B
CN108137549B CN201680058331.8A CN201680058331A CN108137549B CN 108137549 B CN108137549 B CN 108137549B CN 201680058331 A CN201680058331 A CN 201680058331A CN 108137549 B CN108137549 B CN 108137549B
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substituted
independently selected
occurrence
alkyl
membered heterocyclyl
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CN108137549A (zh
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J.R.科特
W.R.尤因
D.J.P.平托
L.M.史密斯二世
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Bristol Myers Squibb Co
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    • C07—ORGANIC CHEMISTRY
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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 directly attached to ring carbon atoms
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    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
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    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D471/02—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 two hetero rings
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    • C07D471/02—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 two hetero rings
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    • C07D498/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CN201680058331.8A 2015-08-05 2016-08-03 取代的甘氨酸衍生的fxia抑制剂 Active CN108137549B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562201267P 2015-08-05 2015-08-05
US62/201267 2015-08-05
PCT/US2016/045276 WO2017023992A1 (en) 2015-08-05 2016-08-03 Novel substituted glycine derived fxia inhibitors

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CN108137549A CN108137549A (zh) 2018-06-08
CN108137549B true CN108137549B (zh) 2021-07-20

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US (2) US10336730B2 (https=)
EP (1) EP3331872B1 (https=)
JP (1) JP6785838B2 (https=)
KR (1) KR102697816B1 (https=)
CN (1) CN108137549B (https=)
ES (1) ES2754599T3 (https=)
WO (1) WO2017023992A1 (https=)

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CN112047931B (zh) * 2019-06-06 2024-03-08 上海美悦生物科技发展有限公司 FXIa凝血因子抑制剂、其药物组合物和用途
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CN116120240A (zh) * 2019-09-27 2023-05-16 深圳信立泰药业股份有限公司 FXIa抑制剂化合物及其制备方法和医药用途
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CN116133660B (zh) 2020-07-22 2025-05-02 詹森药业有限公司 可用作因子XIa抑制剂的化合物
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TW202227079A (zh) * 2020-10-23 2022-07-16 大陸商深圳信立泰藥業股份有限公司 ＦＸＩａ抑制劑化合物或其鹽的醫藥用途及含有其的藥物組合物
WO2022083706A1 (zh) * 2020-10-23 2022-04-28 深圳信立泰药业股份有限公司 FXIa抑制剂化合物的盐及其制备方法和医药用途
CN112679446A (zh) * 2020-10-26 2021-04-20 都创(上海)医药科技有限公司 一种合成反式-3-(3-氯-2-氟-6-(1h-四氮唑-1-基)苯基)丙烯酸的方法
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
CN112675173B (zh) * 2020-12-25 2022-04-05 华南理工大学 FXIa抑制剂化合物或其盐的医药用途
CN115461330A (zh) * 2021-03-18 2022-12-09 深圳信立泰药业股份有限公司 FXIa抑制剂化合物杂质及其制备方法和用途
CN116283750B (zh) * 2021-09-09 2025-02-07 成都泰和伟业生物科技有限公司 一种杂环酰胺类衍生物及其制备方法和用途
CN116199672A (zh) * 2021-11-30 2023-06-02 成都泰和伟业生物科技有限公司 一种嘧啶酰胺类衍生物及其制备方法和用途
CN116262740A (zh) * 2022-11-18 2023-06-16 成都施贝康生物医药科技有限公司 新型氧代吡啶类化合物及其制备方法和用途
KR20260032556A (ko) 2023-06-30 2026-03-09 심천 사루브리스 퍼머수티칼스 컴퍼니 리미티드 다치환된 거대환식 화합물 및 이의 제조 방법과 용도
CN117164566B (zh) * 2023-09-07 2025-06-06 成都施贝康生物医药科技有限公司 一种氧代哒嗪类化合物及其制备方法和用途
CN117164564B (zh) * 2023-09-07 2025-07-08 成都施贝康生物医药科技有限公司 氧代哒嗪类化合物及其制备方法和用途
CN117164563B (zh) * 2023-09-07 2025-06-10 成都施贝康生物医药科技有限公司 氧代嘧啶类化合物及其制备方法和用途
CN117164562B (zh) * 2023-09-07 2025-06-13 成都施贝康生物医药科技有限公司 一种氧代哒嗪类化合物及其制备方法和用途

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