JP2018531954A5 - - Google Patents
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- Publication number
- JP2018531954A5 JP2018531954A5 JP2018521211A JP2018521211A JP2018531954A5 JP 2018531954 A5 JP2018531954 A5 JP 2018531954A5 JP 2018521211 A JP2018521211 A JP 2018521211A JP 2018521211 A JP2018521211 A JP 2018521211A JP 2018531954 A5 JP2018531954 A5 JP 2018531954A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- halo
- nhc
- hydrogen
- 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
- 125000001475 halogen functional group Chemical group 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 241000124008 Mammalia Species 0.000 claims 6
- 230000015572 biosynthetic process Effects 0.000 claims 6
- 125000004043 oxo group Chemical group O=* 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 208000007536 Thrombosis Diseases 0.000 claims 5
- -1 cyano, cyclopropyl Chemical group 0.000 claims 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 239000008280 blood Substances 0.000 claims 3
- 210000004369 blood Anatomy 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000000623 heterocyclic group Chemical group 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 108090000190 Thrombin Proteins 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 2
- IBAHLNWTOIHLKE-UHFFFAOYSA-N cyano cyanate Chemical compound N#COC#N IBAHLNWTOIHLKE-UHFFFAOYSA-N 0.000 claims 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229960004072 thrombin Drugs 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
- 206010047249 Venous thrombosis Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 208000004043 venous thromboembolism Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562248075P | 2015-10-29 | 2015-10-29 | |
| US62/248,075 | 2015-10-29 | ||
| PCT/US2016/058362 WO2017074832A1 (en) | 2015-10-29 | 2016-10-24 | FACTOR XIa INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018531954A JP2018531954A (ja) | 2018-11-01 |
| JP2018531954A5 true JP2018531954A5 (enExample) | 2019-11-28 |
| JP6892858B2 JP6892858B2 (ja) | 2021-06-23 |
Family
ID=58631804
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018521211A Active JP6892858B2 (ja) | 2015-10-29 | 2016-10-24 | 第ＸＩａ因子阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10214512B2 (enExample) |
| EP (1) | EP3368036B1 (enExample) |
| JP (1) | JP6892858B2 (enExample) |
| KR (1) | KR102727485B1 (enExample) |
| CN (1) | CN108430471B (enExample) |
| AU (1) | AU2016344476B2 (enExample) |
| BR (1) | BR112018008506B8 (enExample) |
| CA (1) | CA2998902C (enExample) |
| MA (1) | MA43128A (enExample) |
| MX (1) | MX387515B (enExample) |
| RU (1) | RU2728783C2 (enExample) |
| WO (1) | WO2017074832A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3870171B1 (en) * | 2018-10-25 | 2024-11-20 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| CN113015730A (zh) * | 2018-11-13 | 2021-06-22 | 诺华股份有限公司 | 用于治疗与nlrp活性相关的病症的化合物和组合物 |
| CN113677682B (zh) | 2019-04-16 | 2023-05-30 | 华润生物医药有限公司 | 作为XIa因子抑制剂的大环衍生物 |
| WO2021013209A1 (zh) * | 2019-07-23 | 2021-01-28 | 南京明德新药研发有限公司 | 作为XIa因子抑制剂的大环衍生物 |
| EP4178620B1 (en) | 2020-07-10 | 2026-04-01 | Merck Sharp & Dohme LLC | Plasma kallikrein inhibitors |
| AU2022212785A1 (en) * | 2021-01-28 | 2023-07-27 | Merck Sharp & Dohme Llc | 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 |
| 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 (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004517060A (ja) | 2000-11-07 | 2004-06-10 | ブリストルーマイヤーズ スクイブ カンパニー | セリンプロテアーゼ抑制剤として有用な酸誘導体 |
| EP1332131A2 (en) | 2000-11-07 | 2003-08-06 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| HUP0304058A2 (hu) | 2001-01-30 | 2004-04-28 | Bristol-Myers Squibb Company | Xa faktor szulfonamid-laktám inhibitorok és alkalmazásuk és ezeket tartalmazó gyógyszerkészítmények |
| EP1425015A4 (en) | 2001-08-20 | 2004-12-15 | Bristol Myers Squibb Co | TETRAHYDROQUINOLINE DERIVATIVES FOR USE AS ANTITHROMBOTIC AGENTS |
| US7037911B2 (en) | 2002-06-26 | 2006-05-02 | Bristol-Myers Squibb Company | Amino-bicyclic pyrazinones and pyridinones as coagulation serine protease inhibitors |
| US20040180855A1 (en) | 2003-02-19 | 2004-09-16 | Schumacher William A. | Methods of treating thrombosis with reduced risk of increased bleeding times |
| US7138412B2 (en) | 2003-03-11 | 2006-11-21 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives useful as serine protease inhibitors |
| US7129264B2 (en) | 2003-04-16 | 2006-10-31 | Bristol-Myers Squibb Company | Biarylmethyl indolines and indoles as antithromboembolic agents |
| US7417063B2 (en) | 2004-04-13 | 2008-08-26 | Bristol-Myers Squibb Company | Bicyclic heterocycles useful as serine protease inhibitors |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| US20060074103A1 (en) | 2004-10-06 | 2006-04-06 | Corte James R | Cyclic beta-amino acid derivatives as factor Xa inhibitors |
| US7576098B2 (en) | 2004-12-08 | 2009-08-18 | Bristol-Myers Squibb Company | Heterocyclic compounds as inhibitors of factor VIIa |
| AR054321A1 (es) | 2005-01-10 | 2007-06-20 | Bristol Myers Squibb Co | Derivados en fenilglicinamida utiles como anticoagulantes |
| 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 |
| US20060183771A1 (en) | 2005-02-17 | 2006-08-17 | Seiffert Dietmar A | Novel combination of selective factor VIIa and/or factor XIa inhibitors and selective plasma kallikrein inhibitors |
| BRPI0610506A2 (pt) * | 2005-04-20 | 2010-06-29 | Johnson & Johnson | moduladores de trombina de n-óxidos de piridina fluorados e processo para n-oxidação de heteroarilas contendo nitrogênio |
| JP5225098B2 (ja) | 2005-12-14 | 2013-07-03 | ブリストル−マイヤーズ スクイブ カンパニー | 第ＸＩａ因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ |
| AU2006325746A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| US8466295B2 (en) | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
| US7829584B2 (en) * | 2006-03-21 | 2010-11-09 | Janssen Pharmaceutica Nv | Pyridines and pyridine N-oxides as modulators of thrombin |
| ES2546815T3 (es) | 2006-12-15 | 2015-09-28 | Bristol-Myers Squibb Company | Análogos de arilpropilamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor XIa |
| KR20100037600A (ko) | 2007-06-13 | 2010-04-09 | 브리스톨-마이어스 스큅 컴퍼니 | 응고 인자 억제제로서의 디펩티드 유사체 |
| CN102026996B (zh) | 2008-03-13 | 2015-01-07 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的哒嗪衍生物 |
| JP5844287B2 (ja) | 2010-02-11 | 2016-01-13 | 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マクロ環 |
| TW201319068A (zh) * | 2011-08-05 | 2013-05-16 | 必治妥美雅史谷比公司 | 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑 |
| TW201311689A (zh) * | 2011-08-05 | 2013-03-16 | 必治妥美雅史谷比公司 | 作為因子ｘｉａ抑制劑之新穎巨環化合物 |
| LT2766346T (lt) | 2011-10-14 | 2017-06-12 | Bristol-Myers Squibb Company | Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai |
| IN2014CN02806A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| IN2014CN02805A (enExample) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| WO2013093484A1 (en) | 2011-12-21 | 2013-06-27 | Ono Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor xia inhibitors |
| JP2015083542A (ja) | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | ３位置換プロリン誘導体 |
| KR20150038372A (ko) * | 2012-08-03 | 2015-04-08 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 디히드로피리돈 P1 |
| CA2880898A1 (en) * | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
| US9809545B2 (en) | 2013-03-27 | 2017-11-07 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| 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 |
| US9663527B2 (en) * | 2014-02-11 | 2017-05-30 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| US9649309B2 (en) * | 2014-04-11 | 2017-05-16 | The University Of North Carolina At Chapel Hill | Therapeutic uses of selected pyrimidine compounds with anti-Mer tyrosine kinase activity |
| US9453018B2 (en) * | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| US20180162821A1 (en) * | 2016-12-14 | 2018-06-14 | Bristol-Myers Squibb Company | Factor xia macrocycles with novel p1 groups |
-
2016
- 2016-10-24 BR BR112018008506A patent/BR112018008506B8/pt active IP Right Grant
- 2016-10-24 RU RU2018119015A patent/RU2728783C2/ru active
- 2016-10-24 AU AU2016344476A patent/AU2016344476B2/en active Active
- 2016-10-24 MX MX2018005045A patent/MX387515B/es unknown
- 2016-10-24 CA CA2998902A patent/CA2998902C/en active Active
- 2016-10-24 MA MA043128A patent/MA43128A/fr unknown
- 2016-10-24 EP EP16860556.6A patent/EP3368036B1/en active Active
- 2016-10-24 JP JP2018521211A patent/JP6892858B2/ja active Active
- 2016-10-24 CN CN201680059577.7A patent/CN108430471B/zh active Active
- 2016-10-24 KR KR1020187013433A patent/KR102727485B1/ko active Active
- 2016-10-24 WO PCT/US2016/058362 patent/WO2017074832A1/en not_active Ceased
- 2016-10-24 US US15/771,538 patent/US10214512B2/en active Active
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