JP2014521700A5 - - Google Patents
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- JP2014521700A5 JP2014521700A5 JP2014524151A JP2014524151A JP2014521700A5 JP 2014521700 A5 JP2014521700 A5 JP 2014521700A5 JP 2014524151 A JP2014524151 A JP 2014524151A JP 2014524151 A JP2014524151 A JP 2014524151A JP 2014521700 A5 JP2014521700 A5 JP 2014521700A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- alkyl
- halogen
- substituted
- methyl
- 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.)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161515404P | 2011-08-05 | 2011-08-05 | |
| US61/515,404 | 2011-08-05 | ||
| PCT/US2012/049698 WO2013022814A1 (en) | 2011-08-05 | 2012-08-06 | Cyclic p1 linkers as factor xia inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014521700A JP2014521700A (ja) | 2014-08-28 |
| JP2014521700A5 true JP2014521700A5 (enExample) | 2015-10-01 |
| JP6113727B2 JP6113727B2 (ja) | 2017-04-12 |
Family
ID=46964007
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014524151A Active JP6113727B2 (ja) | 2011-08-05 | 2012-08-06 | 第xia因子阻害剤としての環状p1リンカー |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US8901115B2 (enExample) |
| EP (2) | EP3070087B1 (enExample) |
| JP (1) | JP6113727B2 (enExample) |
| CN (2) | CN103702999B (enExample) |
| AR (1) | AR088423A1 (enExample) |
| ES (2) | ES2563445T3 (enExample) |
| TW (1) | TW201319068A (enExample) |
| WO (1) | WO2013022814A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2789622C (en) | 2010-02-11 | 2018-04-03 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
| 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 |
| 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 |
| SI2766346T1 (sl) | 2011-10-14 | 2017-05-31 | Bristol-Myers Squibb Company | Substituirane tetrahidroizokinolinske spojine kot faktor xia inhibitorji |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| LT2882734T (lt) * | 2012-08-03 | 2016-12-12 | Bristol-Myers Squibb Company | Dihidropiridonai, kaip xia faktoriaus slopikliai |
| PT2880026T (pt) | 2012-08-03 | 2017-05-03 | Bristol Myers Squibb Co | Dihidropiridona p1 como inibidores de fator xia |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| EP2906551B1 (en) | 2012-10-12 | 2018-02-28 | Bristol-Myers Squibb Company | Crystalline forms of a factor xia inhibitor |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2978751B1 (en) | 2013-03-25 | 2018-12-05 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles 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 | ||
| KR20240017118A (ko) * | 2014-01-31 | 2024-02-06 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 헤테로시클릭 P2' 기를 갖는 마크로사이클 |
| EP3104701B1 (en) | 2014-02-11 | 2019-01-30 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| WO2015123093A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| US9868727B2 (en) | 2014-07-28 | 2018-01-16 | 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 |
| NO2721243T3 (enExample) | 2014-10-01 | 2018-10-20 | ||
| MX385021B (es) * | 2014-12-10 | 2025-03-14 | Ono Pharmaceutical Co | Derivado de dihidroindolizinona. |
| JP6742348B2 (ja) * | 2015-06-19 | 2020-08-19 | 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ジアミド大員環 |
| US10676477B2 (en) | 2015-07-29 | 2020-06-09 | Bristol-Myers Squibb Company | Factor XIa macrocycle inhibitors bearing a non-aromatic P2' group |
| JP6629958B2 (ja) | 2015-07-29 | 2020-01-15 | ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company | アルキルまたはシクロアルキルP2’基を担持する大員環の第XIa因子阻害剤 |
| MX387515B (es) | 2015-10-29 | 2025-03-18 | Merck Sharp & Dohme Llc | Inhibidores de factor xia. |
| 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 |
| WO2017151746A1 (en) | 2016-03-02 | 2017-09-08 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| EP3301094A1 (en) * | 2016-09-30 | 2018-04-04 | Mutabilis | Heterocyclic compounds and their use in preventing or treating bacterial infections |
| CN110062757B (zh) * | 2017-01-18 | 2022-03-04 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
| WO2019011166A1 (zh) * | 2017-07-14 | 2019-01-17 | 四川科伦博泰生物医药股份有限公司 | 大环酰胺化合物及其药物组合物和用途 |
| WO2019204447A1 (en) | 2018-04-17 | 2019-10-24 | The Regents Of The University Of Michigan | Inhibitors of platelet function and methods for use of the same |
| US12018027B2 (en) | 2019-04-16 | 2024-06-25 | China Resources Biopharmaceutical Company Limited | Macrocyclic derivatives acting as XIa factor inhibitor |
| JP7286001B2 (ja) * | 2019-07-23 | 2023-06-02 | メッドシャイン ディスカバリー インコーポレイテッド | 第XIa因子阻害剤としての大環状誘導体 |
| CN115490708B (zh) * | 2021-06-18 | 2025-01-24 | 苏州亚盛药业有限公司 | 磺酰胺类大环衍生物及其制备方法和用途 |
| AU2024309220A1 (en) * | 2023-06-30 | 2026-01-29 | Shenzhen Salubris Pharmaceuticals Co., Ltd | Polysubstituted macrocyclic compound, and preparation method therefor and use thereof |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| JPH0987280A (ja) * | 1995-09-28 | 1997-03-31 | Yamanouchi Pharmaceut Co Ltd | オキソピペラジン誘導体又はその塩 |
| PE121699A1 (es) | 1997-02-18 | 1999-12-08 | Boehringer Ingelheim Pharma | Heterociclos biciclicos disustituidos como inhibidores de la trombina |
| ZA985247B (en) | 1997-06-19 | 1999-12-17 | Du Pont Merck Pharma | Guanidine mimics as factor Xa inhibitors. |
| WO2000077027A2 (en) | 1999-06-14 | 2000-12-21 | Tularik Limited | Serine protease inhibitors |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| AR035216A1 (es) | 2000-12-01 | 2004-05-05 | Astrazeneca Ab | Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios |
| WO2003011222A2 (en) * | 2001-07-27 | 2003-02-13 | Merck & Co., Inc. | Thrombin inhibitors |
| EP1427415B1 (en) | 2001-09-21 | 2009-08-12 | Brystol-Myers Squibb Company | Lactam-containing compounds and derivatives thereof as factor xa 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 |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered 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 |
| JP5236293B2 (ja) | 2005-01-13 | 2013-07-17 | ブリストル−マイヤーズ スクイブ カンパニー | Xia因子阻害剤としての置換ビアリール化合物 |
| 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 |
| 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 |
| EP1981854B1 (en) | 2005-12-14 | 2011-06-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| CN101389613B (zh) * | 2005-12-23 | 2011-10-12 | 布里斯托尔-迈尔斯.斯奎布公司 | 用作抗凝血药的大环凝血因子viia抑制剂 |
| PE20071132A1 (es) * | 2005-12-23 | 2007-12-14 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| EP2102189B1 (en) | 2006-12-15 | 2015-07-29 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| EP2152664B1 (en) | 2007-06-13 | 2014-09-03 | Bristol-Myers Squibb Company | Dipeptide analogs as coagulation factor inhibitors |
| EP2070899A1 (en) | 2007-12-14 | 2009-06-17 | F. Hoffmann-La Roche Ag | Deprotection of N-BOC compounds |
| EP2265601B1 (en) * | 2008-03-13 | 2012-02-01 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| CA2789622C (en) * | 2010-02-11 | 2018-04-03 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
| 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 |
| 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 |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| SI2766346T1 (sl) | 2011-10-14 | 2017-05-31 | Bristol-Myers Squibb Company | Substituirane tetrahidroizokinolinske spojine kot faktor xia inhibitorji |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| PT2880026T (pt) | 2012-08-03 | 2017-05-03 | Bristol Myers Squibb Co | Dihidropiridona p1 como inibidores de fator xia |
| LT2882734T (lt) | 2012-08-03 | 2016-12-12 | Bristol-Myers Squibb Company | Dihidropiridonai, kaip xia faktoriaus slopikliai |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| EP2906551B1 (en) | 2012-10-12 | 2018-02-28 | Bristol-Myers Squibb Company | Crystalline forms of a factor xia inhibitor |
-
2012
- 2012-08-03 TW TW101128158A patent/TW201319068A/zh unknown
- 2012-08-06 US US14/236,968 patent/US8901115B2/en active Active
- 2012-08-06 EP EP16151754.5A patent/EP3070087B1/en active Active
- 2012-08-06 EP EP12766737.6A patent/EP2739625B1/en active Active
- 2012-08-06 JP JP2014524151A patent/JP6113727B2/ja active Active
- 2012-08-06 CN CN201280037801.4A patent/CN103702999B/zh active Active
- 2012-08-06 CN CN201510648908.8A patent/CN105294701B/zh active Active
- 2012-08-06 WO PCT/US2012/049698 patent/WO2013022814A1/en not_active Ceased
- 2012-08-06 ES ES12766737.6T patent/ES2563445T3/es active Active
- 2012-08-06 ES ES16151754T patent/ES2733096T3/es active Active
- 2012-08-07 AR ARP120102879A patent/AR088423A1/es unknown
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2014
- 2014-10-30 US US14/528,168 patent/US9108981B2/en active Active