ES2963267T3 - Pirimidinonas como inhibidores del Factor XIa - Google Patents
Pirimidinonas como inhibidores del Factor XIa Download PDFInfo
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- ES2963267T3 ES2963267T3 ES20197284T ES20197284T ES2963267T3 ES 2963267 T3 ES2963267 T3 ES 2963267T3 ES 20197284 T ES20197284 T ES 20197284T ES 20197284 T ES20197284 T ES 20197284T ES 2963267 T3 ES2963267 T3 ES 2963267T3
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- 239000003112 inhibitor Substances 0.000 title abstract description 48
- 108010080805 Factor XIa Proteins 0.000 title abstract description 25
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 title description 8
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 33
- GQHTUMJGOHRCHB-UHFFFAOYSA-N 2,3,4,6,7,8,9,10-octahydropyrimido[1,2-a]azepine Chemical compound C1CCCCN2CCCN=C21 GQHTUMJGOHRCHB-UHFFFAOYSA-N 0.000 claims description 20
- 230000008569 process Effects 0.000 claims description 19
- ARNZYRBXMAGCIZ-UHFFFAOYSA-N 4-[5-chloro-2-[4-(trifluoromethyl)triazol-1-yl]phenyl]-1H-pyrimidin-6-one Chemical compound ClC=1C=CC(=C(C1)C1=CC(=NC=N1)O)N1N=NC(=C1)C(F)(F)F ARNZYRBXMAGCIZ-UHFFFAOYSA-N 0.000 claims description 5
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| US10081623B2 (en) | 2014-09-04 | 2018-09-25 | Bristol-Myers Squibb Company | Diamide macrocycles that are FXIa inhibitors |
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| US10160750B2 (en) | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
| WO2017019821A1 (en) | 2015-07-29 | 2017-02-02 | Bristol-Myers Squibb Company | Factor xia new macrocycle 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 |
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| JOP20160198B1 (ar) | 2015-09-16 | 2022-03-14 | Janssen Pharmaceuticals Inc | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| KR20180117156A (ko) | 2016-03-02 | 2018-10-26 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 |
| WO2017167950A1 (en) | 2016-03-31 | 2017-10-05 | Janssen Pharmaceuticals, Inc. | Substituted indole derivatives as dengue viral replication inhibitors |
| WO2017167953A1 (en) | 2016-03-31 | 2017-10-05 | Janssen Pharmaceuticals, Inc. | Substituted indoline derivatives as dengue viral replication inhibitors |
| EA201892200A1 (ru) | 2016-04-01 | 2019-03-29 | Янссен Фармасьютикалз, Инк. | Замещенные производные соединений индола в качестве ингибиторов репликации вирусов денге |
| JOP20170069B1 (ar) | 2016-04-01 | 2021-08-17 | 1 Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| 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 |
| JOP20180026A1 (ar) | 2017-03-31 | 2019-01-30 | Univ Leuven Kath | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| JOP20180025B1 (ar) | 2017-03-31 | 2021-08-17 | Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
| PE20200604A1 (es) | 2017-05-22 | 2020-03-10 | Janssen Pharmaceuticals Inc | Derivados de indolina sustituidos como inhibidores de la replicacion virica de dengue |
| BR112019024311A2 (pt) | 2017-05-22 | 2020-07-28 | Janssen Pharmaceuticals, Inc. | derivados de indolina substituídos como inibidores da replicação viral do dengue |
| ES2969253T3 (es) * | 2019-04-11 | 2024-05-17 | Bristol Myers Squibb Co | Las opciones sintéticas novedosas hacia la fabricación de (6R,10S)-10-{4-[5-cloro-2-(4-cloro-1H-1,2,3-triazol-1-il)fenil]-6-oxo-1(6H)-pirimidinil}-1-(difluorometil)-6-metil-1,4,7,8,9,10-hexahidro-11,15-(meteno)pirazolo[4,3-b][1,7]diazaciclotetradecin-5(6H)-ona |
| BR112021020257A2 (pt) * | 2019-04-11 | 2021-12-07 | Bristol Myers Squibb Co | Desempenho intensificado de sólido amorfo e formulações solubilizadas para realizar concentrações de plasma terapêutico |
| AU2020257911B2 (en) * | 2019-04-16 | 2023-01-05 | China Resources Biopharmaceutical Company Limited | Macrocyclic derivatives acting as XIa factor inhibitor |
| 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 |
| WO2021057818A1 (zh) * | 2019-09-27 | 2021-04-01 | 深圳信立泰药业股份有限公司 | FXIa抑制剂及其制备方法和医药用途 |
| CN115916780A (zh) * | 2020-04-10 | 2023-04-04 | 百时美施贵宝公司 | (9r,13s)-13-{4-[5-氯-2-(4-氯-1h-1,2,3-三唑-1-基)苯基]-6-氧代-1,6-二氢嘧啶-1-基}-3-(二氟甲基)-9-甲基-3,4,7,15-四氮杂三环[12.3.1.02,6]十八-1(18),2(6),4,14,16-五烯-8-酮的晶型 |
| TW202229280A (zh) * | 2020-10-12 | 2022-08-01 | 美商必治妥美雅史谷比公司 | （６ｒ，１０ｓ）－１０－｛４－［５－氯－２－（４－氯－１ｈ－１，２，３－三唑－１－基）苯基］－６－側氧基－１（６ｈ）－嘧啶基｝－１－（二氟甲基）－６－甲基－１，４，７，８，９，１０－六氫－１１，１５－（亞甲橋基）吡唑并［４，３－ｂ］［１，７］二氮雜環十四炔－５（６ｈ）－酮之製備方法 |
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| 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 |
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| 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 |
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| EA025392B1 (ru) * | 2012-08-03 | 2016-12-30 | Бристол-Маерс Сквибб Компани | Дигидропиридон р1 в качестве ингибиторов фактора xia |
| RS57659B1 (sr) * | 2014-01-31 | 2018-11-30 | Bristol Myers Squibb Co | Makrociklusi sa heterocikličnim p2' grupama kao inhibitori faktora xia |
| NO2760821T3 (US07585860-20090908-C00112.png) * | 2014-01-31 | 2018-03-10 | ||
| NO2721243T3 (US07585860-20090908-C00112.png) * | 2014-10-01 | 2018-10-20 |
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