CN105164122B - 取代的氧代吡啶衍生物及其在治疗心血管病症方面的用途 - Google Patents

取代的氧代吡啶衍生物及其在治疗心血管病症方面的用途 Download PDF

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Publication number
CN105164122B
CN105164122B CN201480025730.5A CN201480025730A CN105164122B CN 105164122 B CN105164122 B CN 105164122B CN 201480025730 A CN201480025730 A CN 201480025730A CN 105164122 B CN105164122 B CN 105164122B
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mmol
methyl
trifluoromethyl
substituted
group
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CN105164122A (zh
Inventor
S.勒里希
A.希利施
J.施特拉斯布格
S.海特迈尔
M.V.施密特
K-H.施莱默
A.特施特根
A.布赫米勒
C.格德斯
M.舍费尔
T.金策尔
H.泰勒
H.希罗克
J.克拉尔
E.希梅内斯努内斯
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Bayer Pharma AG
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Bayer Pharma AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
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    • C07D401/12—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 chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Chemical & Material Sciences (AREA)
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  • 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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  • Pharmacology & Pharmacy (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Epidemiology (AREA)
CN201480025730.5A 2013-03-28 2014-03-27 取代的氧代吡啶衍生物及其在治疗心血管病症方面的用途 Expired - Fee Related CN105164122B (zh)

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EP13161588 2013-03-28
EP13161588.2 2013-03-28
EP13190944.2 2013-10-30
EP13190944 2013-10-30
PCT/EP2014/056135 WO2014154794A1 (de) 2013-03-28 2014-03-27 Substituierte oxopyridin-derivate und ihre verwendung bei der behandlung von herz-kreislauf-erkrankungen

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CN201711458259.0A Expired - Fee Related CN108164513B (zh) 2013-03-28 2014-03-27 取代的氧代吡啶衍生物及其在治疗心血管病症方面的用途

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EP (1) EP2978756B1 (enExample)
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JP6479763B2 (ja) 2013-03-25 2019-03-06 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害剤としての置換アゾール含有のテトラヒドロイソキノリン
TWI633089B (zh) * 2013-03-28 2018-08-21 拜耳製藥股份有限公司 經取代的酮基吡啶衍生物
NO2760821T3 (enExample) 2014-01-31 2018-03-10
ES2687498T3 (es) 2014-01-31 2018-10-25 Bristol-Myers Squibb Company Macrociclos con grupos P2¿ heterocíclicos como inhibidores del factor XIa
WO2015120777A1 (zh) 2014-02-14 2015-08-20 四川海思科制药有限公司 一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用
ES2714283T3 (es) 2014-09-04 2019-05-28 Bristol Myers Squibb Co Macrociclos de diamida que son inhibidores de FXIa
EP3197896B1 (de) 2014-09-24 2019-01-30 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
EP3197889B1 (de) 2014-09-24 2018-08-01 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
WO2016046166A1 (de) 2014-09-24 2016-03-31 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
ES2712886T3 (es) 2014-09-24 2019-05-16 Bayer Pharma AG Derivados de piridobenzazepina y piridobenzazocina que inhiben el factor XIa
EP3197880B1 (de) 2014-09-24 2018-10-24 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate mit anti-inflammatorischer und anti-thrombotischer wirkung
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
CA2979937A1 (en) * 2015-03-19 2016-09-22 Bayer Pharma Aktiengesellschaft Oxo-pyridine-derivatives as factor xia inhibitors for the treatment of thrombosis
JO3703B1 (ar) * 2015-07-09 2021-01-31 Bayer Pharma AG مشتقات أوكسوبيريدين مستبدلة
WO2017037051A1 (de) 2015-09-04 2017-03-09 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
FR3046791B1 (fr) * 2016-01-18 2020-01-10 Adisseo France S.A.S. Procede de preparation d'analogues de la methionine
AU2017317988B2 (en) * 2016-08-31 2020-12-24 Jiangsu Hengrui Medicine Co., Ltd. Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof
CN110193012B (zh) * 2018-02-27 2022-02-08 江苏恒瑞医药股份有限公司 一种氧代吡啶酰胺类衍生物的药物组合物及其制备方法
US11760701B2 (en) 2018-02-27 2023-09-19 The Research Foundation For The State University Of New Yrok Difluoromethoxylation and trifluoromethoxylation compositions and methods for synthesizing same
US11299462B2 (en) 2018-02-27 2022-04-12 Jiangsu Hengrui Medicine Co., Ltd. Crystal form of oxopicolinamide derivative and preparation method therefor
UA126940C2 (uk) 2018-03-15 2023-02-22 Баєр Акціенгезельшафт Спосіб отримання двох похідних 4-{[(2s)-2-{4-[5-хлор-2-(4-хлор-1h-1,2,3-триазол-1-іл)феніл]-5-метоксі-2-оксопіридин-1(2h)-іл}бутаноїл]аміно}-2-фторбензаміду
ES2922533T3 (es) 2018-04-10 2022-09-16 Bayer Pharma AG Un derivado de oxopiridina sustituido
US20220144848A1 (en) 2018-12-21 2022-05-12 Bayer Aktiengesellschaft Substituted oxopyridine derivatives
EP3898633A1 (en) 2018-12-21 2021-10-27 Bayer Aktiengesellschaft Substituted oxopyridine derivatives
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
CN112341377B (zh) * 2019-08-09 2024-05-14 上海美悦生物科技发展有限公司 一种杂环类化合物及其应用
GB201911816D0 (en) * 2019-08-16 2019-10-02 Univ London Queen Mary Treatment
JP7450024B2 (ja) * 2019-09-27 2024-03-14 シェンヅェン サルブリス ファーマシューティカルズ カンパニー リミテッド ＦＸＩａ阻害剤及びその調製方法と医薬用途
CN112940431B (zh) * 2021-02-04 2023-03-10 四川大学 一种激光诱导的荧光发射组合物及图案化荧光发射方法
CN115108977B (zh) * 2021-03-19 2024-11-29 南京正大天晴制药有限公司 一种瑞戈非尼的制备方法
CN114920699B (zh) * 2022-05-31 2024-03-19 甘肃皓天科技股份有限公司 一种制备6-氯-2-甲基-2h-吲唑-5-胺的方法
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
CN116874469B (zh) * 2023-09-06 2023-11-10 成都施贝康生物医药科技有限公司 一种氧代吡啶类化合物、中间体及其制备方法和用途

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