JP2014530240A5 - - Google Patents
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- Publication number
- JP2014530240A5 JP2014530240A5 JP2014535916A JP2014535916A JP2014530240A5 JP 2014530240 A5 JP2014530240 A5 JP 2014530240A5 JP 2014535916 A JP2014535916 A JP 2014535916A JP 2014535916 A JP2014535916 A JP 2014535916A JP 2014530240 A5 JP2014530240 A5 JP 2014530240A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- alkylene
- conh
- substituted
- 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
- 0 *c1cccc(C2C(N*)=O)c1CCN2C(C=C[C@@](C1F)C([n]2nnnc2)=CC=C1O)=O Chemical compound *c1cccc(C2C(N*)=O)c1CCN2C(C=C[C@@](C1F)C([n]2nnnc2)=CC=C1O)=O 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161547301P | 2011-10-14 | 2011-10-14 | |
| US61/547,301 | 2011-10-14 | ||
| PCT/US2012/059932 WO2013056034A1 (en) | 2011-10-14 | 2012-10-12 | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014530240A JP2014530240A (ja) | 2014-11-17 |
| JP2014530240A5 true JP2014530240A5 (enExample) | 2015-12-03 |
| JP6033318B2 JP6033318B2 (ja) | 2016-11-30 |
Family
ID=47116434
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014535916A Expired - Fee Related JP6033318B2 (ja) | 2011-10-14 | 2012-10-12 | 第ＸＩａ因子阻害剤としての置換テトラヒドロイソキノリン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9079929B2 (enExample) |
| EP (1) | EP2766347B1 (enExample) |
| JP (1) | JP6033318B2 (enExample) |
| CN (1) | CN103987696B (enExample) |
| ES (1) | ES2579832T3 (enExample) |
| IN (1) | IN2014CN02805A (enExample) |
| WO (1) | WO2013056034A1 (enExample) |
Families Citing this family (44)
| 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 |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| WO2013056034A1 (en) | 2011-10-14 | 2013-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2876105A4 (en) | 2012-07-19 | 2016-01-13 | Sumitomo Dainippon Pharma Co Ltd | 1- (CYCLOALKYL-CARBONYL) PROLIN DERIVATIVE |
| 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 |
| BR112015021449B1 (pt) * | 2013-03-05 | 2020-05-05 | Bayer Cropscience Ag | uso de acilsulfonamidas para melhorar a produção da planta |
| EP2978751B1 (en) * | 2013-03-25 | 2018-12-05 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| EP3054944B1 (en) * | 2013-10-07 | 2019-12-04 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| KR20240017118A (ko) | 2014-01-31 | 2024-02-06 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 헤테로시클릭 P2' 기를 갖는 마크로사이클 |
| NO2760821T3 (enExample) | 2014-01-31 | 2018-03-10 | ||
| 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 |
| TN2016000567A1 (en) * | 2014-07-01 | 2018-04-04 | Takeda Pharmaceuticals Co | Heterocyclic compounds and their use as retinoid-related orphan receptor (ror) gamma-t 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 |
| US10414731B2 (en) | 2014-09-24 | 2019-09-17 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| ES2722425T3 (es) * | 2014-09-24 | 2019-08-12 | Bayer Pharma AG | (2H)-2-Oxopiridinas como inhibidores del factor XIa para el tratamiento de enfermedades trombóticas |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| 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 |
| JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
| 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 |
| CN108137549B (zh) * | 2015-08-05 | 2021-07-20 | 百时美施贵宝公司 | 取代的甘氨酸衍生的fxia抑制剂 |
| 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 |
| WO2017123518A1 (en) * | 2016-01-11 | 2017-07-20 | The Rockefeller University | Aminotriazole immunomodulators for treating autoimmune diseases |
| JP7010834B2 (ja) * | 2016-03-17 | 2022-02-10 | チェックメイト セラピューティクス インコーポレイテッド | ニコチンアミドホスホリボシルトランスフェラーゼ抑制用新規化合物及びこれを含む組成物 |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| CA3031592A1 (en) | 2016-08-31 | 2018-03-08 | Jiangsu Hengrui Medicine Co., Ltd. | Oxopicolinamide derivative, preparation method therefor and pharmaceutical use thereof |
| CN109721539B (zh) * | 2017-10-27 | 2021-07-09 | 天津药物研究院有限公司 | 吡唑酰胺类衍生物及其制备方法和用途 |
| CN109867660A (zh) * | 2017-12-01 | 2019-06-11 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的四氢异喹啉酰胺化合物及其药物用途 |
| WO2019184744A1 (zh) * | 2018-03-28 | 2019-10-03 | 四川科伦博泰生物医药股份有限公司 | 四氢异喹啉类衍生物及其制备方法和用途 |
| WO2020243049A1 (en) * | 2019-05-30 | 2020-12-03 | Merck Sharp & Dohme Corp. | Factor xi activation inhibitors |
| EP4125892A4 (en) * | 2020-04-01 | 2024-04-03 | Merck Sharp & Dohme LLC | Factor xi activation inhibitors |
| EP4149917B1 (en) * | 2020-05-12 | 2025-07-30 | Merck Sharp & Dohme LLC | Factor xi activation inhibitors |
| EP3978487A1 (en) | 2020-09-30 | 2022-04-06 | Origo Biopharma, S.L. | 2-(3-pyridin-2-yl-4-quinolin-4-yl-pyrazol-1-yl)-acetamide derivatives as inhibitors of transforming growth factor-beta receptor i/alk5 |
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|---|---|---|---|---|
| FR1525186A (fr) | 1967-03-29 | 1968-05-17 | Roussel Uclaf | Nouvelles pénicillines et procédé de préparation |
| EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| DE4034829A1 (de) | 1990-11-02 | 1992-05-07 | Merck Patent Gmbh | Cyclopeptide |
| JP3190431B2 (ja) | 1991-07-01 | 2001-07-23 | 三菱化学株式会社 | ケトン誘導体 |
| GB9206757D0 (en) | 1992-03-27 | 1992-05-13 | Ferring Bv | Novel peptide receptor ligands |
| US5624936A (en) | 1995-03-29 | 1997-04-29 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1996034010A2 (en) | 1995-03-29 | 1996-10-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| AU717298B2 (en) | 1996-04-03 | 2000-03-23 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| US5869682A (en) | 1996-04-03 | 1999-02-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| 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 |
| CA2324226C (en) | 1998-03-19 | 2012-06-05 | Vertex Pharmaceuticals Incorporated | Inhibitors of caspases |
| EE200000706A (et) | 1998-05-26 | 2002-06-17 | Warner-Lambert Company | Bitsüklilised pürimidiinid ja bitsüklilised 3,4-dihüdropürimidiinid kui rakkude proliferatsiooni inhibiitorid |
| US6307049B1 (en) | 1998-09-30 | 2001-10-23 | The Procter & Gamble Co. | Heterocyclic 2-substituted ketoamides |
| KR20010101355A (ko) | 1999-01-02 | 2001-11-14 | 로버트 흐라이탁, 미쉘 베스트 | 신규한 말론산 유도체, 이의 제조 방법, 이의 용도 및이를 함유하는 약제학적 조성물(인자 ｘａ 활성 억제) |
| EP1016663A1 (en) | 1999-01-02 | 2000-07-05 | Aventis Pharma Deutschland GmbH | Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity) |
| IL145771A0 (en) | 1999-04-09 | 2002-07-25 | Basf Ag | Low-molecular inhibitors of complement proteases |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| EP1125925A1 (en) | 2000-02-15 | 2001-08-22 | Applied Research Systems ARS Holding N.V. | Amine derivatives for the treatment of apoptosis |
| JP2004507456A (ja) | 2000-05-11 | 2004-03-11 | ブリストル−マイヤーズ スクイブ カンパニー | 成長ホルモン分泌促進薬として有用なテトラヒドロイソキノリン類縁体 |
| SV2003000617A (es) | 2000-08-31 | 2003-01-13 | Lilly Co Eli | Inhibidores de la proteasa peptidomimetica ref. x-14912m |
| 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 |
| EP1427415B1 (en) | 2001-09-21 | 2009-08-12 | Brystol-Myers Squibb Company | Lactam-containing compounds and derivatives thereof as factor xa inhibitors |
| WO2003041641A2 (en) * | 2001-11-09 | 2003-05-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
| 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 |
| WO2005014533A2 (en) | 2003-08-08 | 2005-02-17 | Transtech Pharma, Inc. | Aryl and heteroaryl compounds, compositions, and methods of use |
| US7208601B2 (en) * | 2003-08-08 | 2007-04-24 | Mjalli Adnan M M | Aryl and heteroaryl compounds, compositions, and methods of use |
| 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 |
| BRPI0513310A (pt) | 2004-07-12 | 2008-05-06 | Idun Pharmaceuticals Inc | análogos de tetrapeptìdeo |
| 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 |
| BRPI0612621B8 (pt) | 2005-06-17 | 2017-03-21 | Basf Ag | processo para produzir compostos químicos, e, composto |
| 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 |
| BRPI0716715B1 (pt) | 2006-08-23 | 2021-07-06 | Xenon Pharmaceuticals, Inc | Derivados de 4-(n-azacicloalquil) anilidas como moduladores de canal de potássio, seus usos, produto, composição, comprimido e cápsula |
| 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 |
| EP2265601B1 (en) | 2008-03-13 | 2012-02-01 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| WO2010151317A1 (en) | 2009-06-22 | 2010-12-29 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| US8513433B2 (en) | 2009-07-02 | 2013-08-20 | Angion Biomedica Corp. | Small molecule inhibitors of PARP activity |
| WO2011017296A1 (en) | 2009-08-04 | 2011-02-10 | Schering Corporation | 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
| CA2789622C (en) | 2010-02-11 | 2018-04-03 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
| EP2729150B1 (en) | 2011-07-08 | 2016-09-14 | Merck Sharp & Dohme Corp. | Factor ixa 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 |
| DK2794597T3 (en) | 2011-12-21 | 2018-01-15 | Ono Pharmaceutical Co | PYRIDINON AND PYRIMIDINON DERIVATIVES AS FACTOR XIA INHIBITORS |
| WO2013111108A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
| WO2013111107A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | Aminopyridine derivatives as plasma kallikrein 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 |
| BR112014027952B1 (pt) | 2012-05-10 | 2022-06-21 | Bayer Pharma Aktiengesellschaft | Anticorpos monoclonais humanos capazes de se ligarem ao fator de coagulação xi, seu uso, composição farmacêutica e medicamento os compreendendo, ácido nucleico que o codifica, bem como vetor |
| EP2876105A4 (en) | 2012-07-19 | 2016-01-13 | Sumitomo Dainippon Pharma Co Ltd | 1- (CYCLOALKYL-CARBONYL) PROLIN DERIVATIVE |
| 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 |
-
2012
- 2012-10-12 WO PCT/US2012/059932 patent/WO2013056034A1/en not_active Ceased
- 2012-10-12 CN CN201280061628.1A patent/CN103987696B/zh not_active Expired - Fee Related
- 2012-10-12 ES ES12780357.5T patent/ES2579832T3/es active Active
- 2012-10-12 US US14/350,411 patent/US9079929B2/en active Active
- 2012-10-12 IN IN2805CHN2014 patent/IN2014CN02805A/en unknown
- 2012-10-12 EP EP12780357.5A patent/EP2766347B1/en not_active Not-in-force
- 2012-10-12 JP JP2014535916A patent/JP6033318B2/ja not_active Expired - Fee Related
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