JP6410819B2 - 置換オキソピリジン誘導体および第ＸＩａ因子／血漿としてのその使用 - Google Patents

置換オキソピリジン誘導体および第ＸＩａ因子／血漿としてのその使用 Download PDF

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JP6410819B2
JP6410819B2 JP2016528481A JP2016528481A JP6410819B2 JP 6410819 B2 JP6410819 B2 JP 6410819B2 JP 2016528481 A JP2016528481 A JP 2016528481A JP 2016528481 A JP2016528481 A JP 2016528481A JP 6410819 B2 JP6410819 B2 JP 6410819B2
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mmol
methyl
compound
represents hydrogen
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JP2016525136A (ja
JP2016525136A5 (enExample
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レーリヒ，ズザンネ
ヒリツシユ，アレクサンダー
シユトラスブルガー，ユリア
ハイトマイアー，シユテフアン
シユミツト，マルテイナ・ヴイクトーリア
シユレマー，カール−ハインツ
ブーフミユラー，アンニヤ
ゲルデス，クリストフ
テラー，ヘンリツク
シエーフアー，マルテイナ
テルシユテーゲン，アードリアン
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バイエル ファーマ アクチエンゲゼルシャフト
バイエル ファーマ アクチエンゲゼルシャフト
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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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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
    • 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
    • A61P7/10—Antioedematous agents; Diuretics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2016528481A 2013-07-23 2014-07-21 置換オキソピリジン誘導体および第ＸＩａ因子／血漿としてのその使用 Expired - Fee Related JP6410819B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13177605.6 2013-07-23
EP13177605 2013-07-23
PCT/EP2014/065608 WO2015011087A1 (de) 2013-07-23 2014-07-21 Substituierte oxopyridin-derivate und ihre verwendung als faktor xia / plasma

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JP2016525136A JP2016525136A (ja) 2016-08-22
JP2016525136A5 JP2016525136A5 (enExample) 2017-08-17
JP6410819B2 true JP6410819B2 (ja) 2018-10-24

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JP2016528481A Expired - Fee Related JP6410819B2 (ja) 2013-07-23 2014-07-21 置換オキソピリジン誘導体および第ＸＩａ因子／血漿としてのその使用

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US (2) US9475809B2 (enExample)
EP (1) EP3024822B1 (enExample)
JP (1) JP6410819B2 (enExample)
CN (1) CN105555767B (enExample)
CA (1) CA2918814C (enExample)
ES (1) ES2633248T3 (enExample)
WO (1) WO2015011087A1 (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US9475809B2 (en) * 2013-07-23 2016-10-25 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives and use thereof as factor xia/plasma
NO2760821T3 (enExample) 2014-01-31 2018-03-10
JP6505727B2 (ja) 2014-01-31 2019-04-24 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロ環式ｐ２’基を有する第ｘｉａ因子阻害剤としてのマクロ環
JP6526796B2 (ja) 2014-09-04 2019-06-05 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｆｘｉａ阻害剤であるジアミドマクロ環
WO2016046156A1 (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
WO2016046158A1 (de) 2014-09-24 2016-03-31 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
ES2716417T3 (es) 2014-09-24 2019-06-12 Bayer Pharma AG Derivados de oxopiridina sustituidos con acción antiinflamatoria y antitrombótica
WO2016046166A1 (de) 2014-09-24 2016-03-31 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
JO3703B1 (ar) 2015-07-09 2021-01-31 Bayer Pharma AG مشتقات أوكسوبيريدين مستبدلة
EP3344618A1 (de) 2015-09-04 2018-07-11 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate
WO2017074833A1 (en) 2015-10-29 2017-05-04 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
US10143681B2 (en) 2016-08-22 2018-12-04 Merck Sharp & Dohme Corp. Factor XIa inhibitors
CN106831761B (zh) * 2016-12-14 2019-02-12 浙江工业大学 顺式四氢-1H-吡咯并[3,4-b]吡啶-2,5(3H,6H)-二酮的合成方法
DK3774796T3 (da) 2018-04-10 2022-07-18 Bayer Pharma AG Et substitueret oxopyridinderivat
WO2020127508A1 (en) 2018-12-21 2020-06-25 Bayer Aktiengesellschaft Substituted oxopyridine derivatives
EA202191764A1 (ru) 2018-12-21 2021-10-22 Байер Акциенгезельшафт Замещенные оксопиридиновые производные
CN110105276A (zh) * 2019-06-24 2019-08-09 红河学院 一种2-喹啉酮化合物及其制备方法
CN112778273B (zh) * 2019-11-11 2022-08-23 江西济民可信集团有限公司 环酮并吡啶酮类化合物及其制备方法和用途
CN112778277B (zh) * 2019-11-11 2024-04-02 江西济民可信集团有限公司 环酮并吡啶酮联杂芳环化合物及其制备方法和用途
CN113135930B (zh) * 2020-01-17 2023-11-17 上海济煜医药科技有限公司 呋喃并吡啶酮咪唑化合物及其制备方法和用途
CN113135929B (zh) * 2020-01-17 2024-04-19 江西济民可信集团有限公司 呋喃并吡啶酮酰胺化合物及其制备方法和用途
US11814364B2 (en) 2021-03-18 2023-11-14 Janssen Pharmaceutica Nv Pyridine N-oxide derivatives useful as factor XIa inhibitors
US11919881B2 (en) 2021-03-18 2024-03-05 Janssen Pharmaceutica Nv Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors
US11845748B2 (en) 2021-03-18 2023-12-19 Janssen Pharmaceutica Nv Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0407342A3 (en) * 1989-07-06 1991-07-10 Ciba-Geigy Ag Pyrimidine derivatives
CA2881078C (en) * 2004-06-24 2018-10-02 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
GB0420722D0 (en) * 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
CN101137412B (zh) * 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 用作凝血因子XIa抑制剂的取代的二芳基化合物
ES2365815T3 (es) * 2005-12-14 2011-10-11 Bristol-Myers Squibb Company Análogos de arilpropionamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor xia.
ES2546815T3 (es) * 2006-12-15 2015-09-28 Bristol-Myers Squibb Company Análogos de arilpropilamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor XIa
JP5419706B2 (ja) * 2006-12-20 2014-02-19 タケダ カリフォルニア インコーポレイテッド グルコキナーゼアクチベーター
EP2268636A1 (en) * 2007-12-11 2011-01-05 Schering Corporation Gamma secretase modulators
US8268820B2 (en) * 2009-03-26 2012-09-18 Hoffmann-La Roche Inc. 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds
EP2625170A1 (en) * 2010-10-07 2013-08-14 Takeda Pharmaceutical Company Limited 1,4-oxazepane derivatives
WO2013093484A1 (en) * 2011-12-21 2013-06-27 Ono Pharmaceutical Co., Ltd. Pyridinone and pyrimidinone derivatives as factor xia inhibitors
US9475809B2 (en) * 2013-07-23 2016-10-25 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives and use thereof as factor xia/plasma

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Publication number Publication date
WO2015011087A1 (de) 2015-01-29
CN105555767B (zh) 2018-03-23
CA2918814A1 (en) 2015-01-29
ES2633248T3 (es) 2017-09-20
CA2918814C (en) 2021-10-12
EP3024822B1 (de) 2017-05-03
US20170035739A1 (en) 2017-02-09
EP3024822A1 (de) 2016-06-01
JP2016525136A (ja) 2016-08-22
US9475809B2 (en) 2016-10-25
US20160152613A1 (en) 2016-06-02
CN105555767A (zh) 2016-05-04
US9918969B2 (en) 2018-03-20

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