JP2017517512A5 - - Google Patents
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- Publication number
- JP2017517512A5 JP2017517512A5 JP2016569375A JP2016569375A JP2017517512A5 JP 2017517512 A5 JP2017517512 A5 JP 2017517512A5 JP 2016569375 A JP2016569375 A JP 2016569375A JP 2016569375 A JP2016569375 A JP 2016569375A JP 2017517512 A5 JP2017517512 A5 JP 2017517512A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- optionally substituted
- group
- heteroaryl
- cycloalkyl
- 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.)
- Pending
Links
- 125000005843 halogen group Chemical group 0.000 claims 22
- 125000001072 heteroaryl group Chemical group 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 229910052739 hydrogen Inorganic materials 0.000 claims 13
- 239000001257 hydrogen Substances 0.000 claims 13
- 125000001424 substituent group Chemical group 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 8
- 208000007536 Thrombosis Diseases 0.000 claims 6
- 230000015572 biosynthetic process Effects 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 241000124008 Mammalia Species 0.000 claims 3
- 239000008280 blood Substances 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 2
- 206010051055 Deep vein thrombosis Diseases 0.000 claims 1
- 206010014498 Embolic stroke Diseases 0.000 claims 1
- 206010014522 Embolism venous Diseases 0.000 claims 1
- 208000010378 Pulmonary Embolism Diseases 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 208000004043 venous thromboembolism Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462003693P | 2014-05-28 | 2014-05-28 | |
| US62/003,693 | 2014-05-28 | ||
| PCT/US2015/032091 WO2015183709A1 (en) | 2014-05-28 | 2015-05-22 | Factor xia inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017517512A JP2017517512A (ja) | 2017-06-29 |
| JP2017517512A5 true JP2017517512A5 (esLanguage) | 2018-08-02 |
Family
ID=54699606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016569375A Pending JP2017517512A (ja) | 2014-05-28 | 2015-05-22 | 第ｘｉａ因子インヒビター |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9783530B2 (esLanguage) |
| EP (1) | EP3148542B1 (esLanguage) |
| JP (1) | JP2017517512A (esLanguage) |
| KR (1) | KR20170005871A (esLanguage) |
| CN (1) | CN106413710A (esLanguage) |
| AU (1) | AU2015267305A1 (esLanguage) |
| CA (1) | CA2947987A1 (esLanguage) |
| MX (1) | MX2016015484A (esLanguage) |
| RU (1) | RU2016150410A (esLanguage) |
| WO (1) | WO2015183709A1 (esLanguage) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| SI3099687T1 (en) | 2014-01-31 | 2018-08-31 | Bristol-Myers Squibb Company | Macrocycles with hetrocyclic p2' groups as factor xia inhibitors |
| NO2760821T3 (esLanguage) | 2014-01-31 | 2018-03-10 | ||
| US9975874B2 (en) | 2014-07-28 | 2018-05-22 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3189047B1 (en) | 2014-09-04 | 2018-12-26 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| RU2712268C2 (ru) * | 2015-01-20 | 2020-01-28 | Мерк Шарп И Доум Корп. | ИНГИБИТОРЫ ФАКТОРА XIa |
| US10472344B2 (en) | 2015-12-02 | 2019-11-12 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| CN111763171B (zh) * | 2019-04-02 | 2023-12-22 | 上海美悦生物科技发展有限公司 | 一种FXIa凝血因子抑制剂及其药物组合物、制备方法和医药用途 |
| AU2020355830B2 (en) * | 2019-09-27 | 2023-04-13 | Shenzhen Salubris Pharmaceuticals Co. Ltd | FXIa inhibitors and preparation method therefor and pharmaceutical use thereof |
| CN116348109B (zh) * | 2020-09-17 | 2025-01-21 | 浙江海正药业股份有限公司 | 哌嗪类衍生物及其制备方法和用途 |
| US11845748B2 (en) | 2021-03-18 | 2023-12-19 | Janssen Pharmaceutica Nv | Bicyclic pyridine N-oxide derivatives useful as a 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 |
| US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7429604B2 (en) * | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| CN101228129A (zh) * | 2005-04-20 | 2008-07-23 | 詹森药业有限公司 | 氟代吡啶n-氧化物凝血酶调节剂和含氮杂芳基化合物的n-氧化方法 |
| CN101341124A (zh) * | 2005-12-14 | 2009-01-07 | 布里斯托尔-迈尔斯斯奎布公司 | 可用作丝氨酸蛋白酶抑制剂的6元杂环 |
| WO2007109459A2 (en) | 2006-03-21 | 2007-09-27 | Janssen Pharmaceutica, Nv | Pyridines and pyridine n-oxides as modulators of thrombin |
| MX2009012847A (es) * | 2007-06-13 | 2009-12-08 | Bristol Myers Squibb Co | Analogos dipeptidicos como inhibidores de factores de coagulacion. |
| WO2013009527A2 (en) * | 2011-07-08 | 2013-01-17 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
| WO2016018701A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| US9975874B2 (en) | 2014-07-28 | 2018-05-22 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| US9868727B2 (en) | 2014-07-28 | 2018-01-16 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
-
2015
- 2015-05-22 EP EP15800524.9A patent/EP3148542B1/en active Active
- 2015-05-22 US US15/312,839 patent/US9783530B2/en active Active
- 2015-05-22 WO PCT/US2015/032091 patent/WO2015183709A1/en not_active Ceased
- 2015-05-22 KR KR1020167036089A patent/KR20170005871A/ko not_active Withdrawn
- 2015-05-22 AU AU2015267305A patent/AU2015267305A1/en not_active Abandoned
- 2015-05-22 JP JP2016569375A patent/JP2017517512A/ja active Pending
- 2015-05-22 CN CN201580028124.3A patent/CN106413710A/zh active Pending
- 2015-05-22 RU RU2016150410A patent/RU2016150410A/ru not_active Application Discontinuation
- 2015-05-22 MX MX2016015484A patent/MX2016015484A/es unknown
- 2015-05-22 CA CA2947987A patent/CA2947987A1/en not_active Abandoned
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