JP2016525136A5 - - Google Patents
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- Publication number
- JP2016525136A5 JP2016525136A5 JP2016528481A JP2016528481A JP2016525136A5 JP 2016525136 A5 JP2016525136 A5 JP 2016525136A5 JP 2016528481 A JP2016528481 A JP 2016528481A JP 2016528481 A JP2016528481 A JP 2016528481A JP 2016525136 A5 JP2016525136 A5 JP 2016525136A5
- Authority
- JP
- Japan
- Prior art keywords
- formula
- represents hydrogen
- methyl
- compound
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 claims 14
- -1 methoxy, difluoromethoxy Chemical group 0.000 claims 12
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 9
- 229910052801 chlorine Inorganic materials 0.000 claims 9
- 239000000460 chlorine Substances 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 7
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 6
- 229910052731 fluorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 5
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 5
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 4
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 4
- 229910052794 bromium Inorganic materials 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims 2
- 208000011231 Crohn disease Diseases 0.000 claims 2
- 206010019860 Hereditary angioedema Diseases 0.000 claims 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 2
- 230000006806 disease prevention Effects 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000000968 intestinal effect Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 230000009424 thromboembolic effect Effects 0.000 claims 2
- 230000001732 thrombotic effect Effects 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 208000022873 Ocular disease Diseases 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000012024 dehydrating agents Substances 0.000 claims 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 1
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 239000007800 oxidant agent Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 1
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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016525136A JP2016525136A (ja) | 2016-08-22 |
| JP2016525136A5 true JP2016525136A5 (enExample) | 2017-08-17 |
| JP6410819B2 JP6410819B2 (ja) | 2018-10-24 |
Family
ID=48803476
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (7)
| Country | Link |
|---|---|
| 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)
| 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)
| 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 |
-
2014
- 2014-07-21 US US14/906,771 patent/US9475809B2/en not_active Expired - Fee Related
- 2014-07-21 CA CA2918814A patent/CA2918814C/en not_active Expired - Fee Related
- 2014-07-21 JP JP2016528481A patent/JP6410819B2/ja not_active Expired - Fee Related
- 2014-07-21 WO PCT/EP2014/065608 patent/WO2015011087A1/de not_active Ceased
- 2014-07-21 ES ES14741869.3T patent/ES2633248T3/es active Active
- 2014-07-21 CN CN201480052261.6A patent/CN105555767B/zh not_active Expired - Fee Related
- 2014-07-21 EP EP14741869.3A patent/EP3024822B1/de not_active Not-in-force
-
2016
- 2016-10-24 US US15/332,893 patent/US9918969B2/en not_active Expired - Fee Related
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