JP2016535031A5 - - Google Patents
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- Publication number
- JP2016535031A5 JP2016535031A5 JP2016526776A JP2016526776A JP2016535031A5 JP 2016535031 A5 JP2016535031 A5 JP 2016535031A5 JP 2016526776 A JP2016526776 A JP 2016526776A JP 2016526776 A JP2016526776 A JP 2016526776A JP 2016535031 A5 JP2016535031 A5 JP 2016535031A5
- Authority
- JP
- Japan
- Prior art keywords
- chlorine
- hydrogen
- methoxy
- represents hydrogen
- fluorine
- 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
- 239000001257 hydrogen Substances 0.000 claims 39
- 229910052739 hydrogen Inorganic materials 0.000 claims 39
- 150000002431 hydrogen Chemical class 0.000 claims 28
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 25
- 229910052801 chlorine Inorganic materials 0.000 claims 25
- 239000000460 chlorine Substances 0.000 claims 25
- -1 methoxy, difluoromethoxy Chemical group 0.000 claims 23
- 229910052731 fluorine Inorganic materials 0.000 claims 15
- 239000011737 fluorine Substances 0.000 claims 15
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 11
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 5
- 125000001424 substituent group Chemical group 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
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims 4
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 4
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 3
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000006002 1,1-difluoroethyl group Chemical group 0.000 claims 2
- 125000005940 1,4-dioxanyl group Chemical group 0.000 claims 2
- 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
- CWJSHJJYOPWUGX-UHFFFAOYSA-N chlorpropham Chemical compound CC(C)OC(=O)NC1=CC=CC(Cl)=C1 CWJSHJJYOPWUGX-UHFFFAOYSA-N 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 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
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000000968 intestinal effect Effects 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- VXPLXMJHHKHSOA-UHFFFAOYSA-N propham Chemical compound CC(C)OC(=O)NC1=CC=CC=C1 VXPLXMJHHKHSOA-UHFFFAOYSA-N 0.000 claims 2
- 230000009424 thromboembolic effect Effects 0.000 claims 2
- 230000001732 thrombotic effect Effects 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 125000004778 2,2-difluoroethyl group Chemical group [H]C([H])(*)C([H])(F)F 0.000 claims 1
- 125000001494 2-propynyl group Chemical group [H]C#CC([H])([H])* 0.000 claims 1
- PRDFNJUWGIQQBW-UHFFFAOYSA-N 3,3,3-trifluoroprop-1-yne Chemical compound FC(F)(F)C#C PRDFNJUWGIQQBW-UHFFFAOYSA-N 0.000 claims 1
- LZPWAYBEOJRFAX-UHFFFAOYSA-N 4,4,5,5-tetramethyl-1,3,2$l^{2}-dioxaborolane Chemical compound CC1(C)O[B]OC1(C)C LZPWAYBEOJRFAX-UHFFFAOYSA-N 0.000 claims 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 1
- VOPWNXZWBYDODV-UHFFFAOYSA-N Chlorodifluoromethane Chemical compound FC(F)Cl VOPWNXZWBYDODV-UHFFFAOYSA-N 0.000 claims 1
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 1
- 208000022873 Ocular disease Diseases 0.000 claims 1
- 238000006069 Suzuki reaction reaction Methods 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 125000001352 cyclobutyloxy group Chemical group C1(CCC1)O* 0.000 claims 1
- 239000012024 dehydrating agents Substances 0.000 claims 1
- 238000010931 ester hydrolysis Methods 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 208000030533 eye disease Diseases 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- NBTOZLQBSIZIKS-UHFFFAOYSA-N methoxide Chemical compound [O-]C NBTOZLQBSIZIKS-UHFFFAOYSA-N 0.000 claims 1
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims 1
- 231100000252 nontoxic Toxicity 0.000 claims 1
- 230000003000 nontoxic effect Effects 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 0 *C(C(N(*)*)=O)N(C=C(*)C(*)=C1)C1=O Chemical compound *C(C(N(*)*)=O)N(C=C(*)C(*)=C1)C1=O 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13190940.0 | 2013-10-30 | ||
| EP13190940 | 2013-10-30 | ||
| EP14186078.3 | 2014-09-24 | ||
| EP14186078 | 2014-09-24 | ||
| PCT/EP2014/073132 WO2015063093A1 (de) | 2013-10-30 | 2014-10-28 | Substituierte oxopyridin-derivate |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016535031A JP2016535031A (ja) | 2016-11-10 |
| JP2016535031A5 true JP2016535031A5 (enExample) | 2017-11-30 |
| JP6368367B2 JP6368367B2 (ja) | 2018-08-01 |
Family
ID=51795642
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016526776A Expired - Fee Related JP6368367B2 (ja) | 2013-10-30 | 2014-10-28 | 置換オキソピリジン誘導体 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9765070B2 (enExample) |
| EP (1) | EP3063150B1 (enExample) |
| JP (1) | JP6368367B2 (enExample) |
| CN (1) | CN105849109B (enExample) |
| CA (1) | CA2928867A1 (enExample) |
| ES (1) | ES2659045T3 (enExample) |
| WO (1) | WO2015063093A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2712886T3 (es) | 2014-09-24 | 2019-05-16 | Bayer Pharma AG | Derivados de piridobenzazepina y piridobenzazocina que inhiben el factor XIa |
| EP3197896B1 (de) | 2014-09-24 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| EP3197880B1 (de) | 2014-09-24 | 2018-10-24 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate mit anti-inflammatorischer und anti-thrombotischer wirkung |
| EP3197889B1 (de) | 2014-09-24 | 2018-08-01 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| EP3197872B1 (de) | 2014-09-24 | 2019-01-30 | Bayer Pharma Aktiengesellschaft | (2h)-2-oxopyridine als faktor xia-inhibitoren zur behandlung von thrombotischen erkrankungen |
| 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 |
| EP3371162B1 (en) | 2015-10-29 | 2022-01-26 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
| WO2018039094A1 (en) | 2016-08-22 | 2018-03-01 | Merck Sharp & Dohme Corp. | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| HUE057289T2 (hu) | 2016-08-31 | 2022-05-28 | Jiangsu Hengrui Medicine Co | Oxopikolinamid-származék, annak elõállítási módszere és gyógyszerészeti felhasználása |
| EP3741746A4 (en) | 2018-02-27 | 2020-12-16 | Jiangsu Hengrui Medicine Co., Ltd. | CRYSTAL FORM OF OXOPICOLINAMIDE DERIVATIVE AND MANUFACTURING PROCESS FOR IT |
| KR20200143376A (ko) | 2018-03-13 | 2020-12-23 | 샤이어 휴먼 지네틱 테라피즈 인크. | 혈장 칼리크레인 억제제로서의 치환된 이미다조피리딘 및 이의 용도 |
| IL277811B2 (en) * | 2018-04-10 | 2023-12-01 | Bayer Pharma AG | A consequence of oxopyridine is transformed |
| EP3793559A1 (en) * | 2018-05-17 | 2021-03-24 | Bayer Aktiengesellschaft | Substituted dihydropyrazolo pyrazine carboxamide derivatives |
| CN112004810B (zh) | 2018-07-02 | 2022-04-08 | 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晶型及制备方法 |
| PE20211790A1 (es) | 2018-12-21 | 2021-09-09 | Bayer Ag | Derivados de oxopiridina sustituidos |
| US20220144848A1 (en) | 2018-12-21 | 2022-05-12 | Bayer Aktiengesellschaft | Substituted oxopyridine derivatives |
| ES2987744T3 (es) | 2019-09-18 | 2024-11-18 | Takeda Pharmaceuticals Co | Inhibidores de calicreína plasmática y usos de los mismos |
| WO2021055589A1 (en) * | 2019-09-18 | 2021-03-25 | Shire Human Genetic Therapies, Inc. | Heteroaryl plasma kallikrein inhibitors |
| 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 |
| CN113358792B (zh) * | 2021-06-23 | 2023-02-24 | 北京亚宝生物药业有限公司 | 一种医药物质的hplc含量分析方法 |
| CN116283908A (zh) * | 2023-03-10 | 2023-06-23 | 合肥工业大学 | 一种n-芳香甲基吡啶酮类衍生物及其制备方法与应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0400651A2 (hu) * | 2000-11-07 | 2004-06-28 | Bristol-Myers Squibb Company | Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| 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 |
| WO2008079787A2 (en) | 2006-12-20 | 2008-07-03 | Takeda San Diego, Inc. | Glucokinase activators |
| CN104136431B (zh) * | 2011-12-21 | 2017-03-15 | 小野药品工业株式会社 | 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物 |
| GB2497806A (en) * | 2011-12-21 | 2013-06-26 | Ono Pharmaceutical Co | Pyridinone and pyrimidinone derivatives as factor XIa inhibitors |
-
2014
- 2014-10-28 WO PCT/EP2014/073132 patent/WO2015063093A1/de not_active Ceased
- 2014-10-28 ES ES14789580.9T patent/ES2659045T3/es active Active
- 2014-10-28 EP EP14789580.9A patent/EP3063150B1/de not_active Not-in-force
- 2014-10-28 CA CA2928867A patent/CA2928867A1/en not_active Abandoned
- 2014-10-28 JP JP2016526776A patent/JP6368367B2/ja not_active Expired - Fee Related
- 2014-10-28 US US15/032,212 patent/US9765070B2/en not_active Expired - Fee Related
- 2014-10-28 CN CN201480071585.4A patent/CN105849109B/zh not_active Expired - Fee Related