AR109387A1 - INHIBIDORES DEL FACTOR XIa - Google Patents
INHIBIDORES DEL FACTOR XIaInfo
- Publication number
- AR109387A1 AR109387A1 ARP170102321A ARP170102321A AR109387A1 AR 109387 A1 AR109387 A1 AR 109387A1 AR P170102321 A ARP170102321 A AR P170102321A AR P170102321 A ARP170102321 A AR P170102321A AR 109387 A1 AR109387 A1 AR 109387A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- compounds
- hydroxyl
- independently selected
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente solicitud proporciona compuestos y composiciones farmacéuticas que comprenden uno o más de dichos compuestos, y procedimientos para el uso de dichos compuestos para tratar o prevenir trombosis, embolias, hipercoagulabilidad o cambios fibróticos. Los compuestos son inhibidores del factor XIa selectivos o inhibidores dobles del factor XIa y la calicreína plasmática. Reivindicación 1: Un compuesto de la fórmula (1), en la que X es un resto de fórmula (2) ó (3); R¹ es CF₂H, CF₃, OCF₂H, OCF₃, O(alquilo C₁₋₃) u OCH₂(ciclopropilo); R² es cloro o flúor; R³ es hidrógeno, cloro o flúor; R⁴ es hidrógeno, alquilo C₁₋₃ u O(alquilo C₁₋₃), en el que dichos grupos alquilo están opcionalmente sustituidos con de uno a tres grupos independientemente seleccionados del grupo que consiste en halo e hidroxilo; R⁵ es (C=O)OH o (C=O)O(alquilo C₁₋₆), en el que dichos grupos alquilo están opcionalmente sustituidos con de uno a tres grupos independientemente seleccionados del grupo que consiste en halo e hidroxilo; cada Rˣ está independientemente seleccionado de halo, hidroxilo, ciano, oxo, metilo, etilo, CH₂F, CF₃ o CH₂OH; Rʸ es halo o metilo; m es cero, uno o dos; n es uno, dos, tres o cuatro; p es cero o uno; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662377969P | 2016-08-22 | 2016-08-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR109387A1 true AR109387A1 (es) | 2018-11-28 |
Family
ID=59738512
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170102321A AR109387A1 (es) | 2016-08-22 | 2017-08-22 | INHIBIDORES DEL FACTOR XIa |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US10143681B2 (es) |
| EP (1) | EP3500556B1 (es) |
| AR (1) | AR109387A1 (es) |
| TW (1) | TW201808908A (es) |
| WO (1) | WO2018039094A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112004810B (zh) | 2018-07-02 | 2022-04-08 | 江苏恒瑞医药股份有限公司 | 一种氧代吡啶酰胺类衍生物的晶型及制备方法 |
| 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 |
| CN116134025A (zh) * | 2020-09-17 | 2023-05-16 | 浙江海正药业股份有限公司 | 酰胺膦氧类衍生物及其制备方法和用途 |
| US20230373972A1 (en) | 2020-09-17 | 2023-11-23 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Piperazine derivative, preparation method therefor and use thereof |
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| EP1332131A2 (en) | 2000-11-07 | 2003-08-06 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| AU2002231235A1 (en) | 2000-11-07 | 2002-05-21 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| JP2004518688A (ja) | 2001-01-30 | 2004-06-24 | ブリストル−マイヤーズ スクイブ カンパニー | ファクターＸａ阻害剤のスルホンアミドラクタムおよびその方法 |
| AU2002331707A1 (en) | 2001-08-20 | 2003-03-03 | Bristol-Myers Squibb Company | Tetrahydroquinoline derivatives as antithrombotic agents |
| WO2004002405A2 (en) | 2002-06-26 | 2004-01-08 | Bristol-Myers Squibb Company | Amino-bicyclic pyrazinones and pyridinones |
| 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 |
| US20060074103A1 (en) | 2004-10-06 | 2006-04-06 | Corte James R | Cyclic beta-amino acid derivatives as factor Xa inhibitors |
| ATE405553T1 (de) | 2004-12-08 | 2008-09-15 | Bristol Myers Squibb Co | Heterocyclische verbindungen als inhibitoren von faktor viia |
| PE20061117A1 (es) | 2005-01-10 | 2006-10-13 | Bristol Myers Squibb Co | DERIVADOS DE FENILGLICINAMIDA COMO INHIBIDORES DEL FACTOR VIIa |
| 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 |
| WO2006089005A2 (en) | 2005-02-17 | 2006-08-24 | Bristol-Myers Squibb Company | Combination of selective factor viia and/or xia and plasma kallikrein inhibitors |
| KR20080004554A (ko) | 2005-04-20 | 2008-01-09 | 얀센 파마슈티카 엔.브이. | 불소화 피리딘 ｎ―옥사이드 트롬빈 모듈레이터 및 질소를함유하는 헤테로아릴의 ｎ―산화 방법 |
| WO2007070818A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| KR20080087817A (ko) | 2005-12-14 | 2008-10-01 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 ｘｉａ 억제제로서 아릴프로피온아미드,아릴아크릴아미드, 아릴프로핀아미드 또는 아릴메틸우레아유사체 |
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| CA2851810C (en) | 2011-10-14 | 2020-01-07 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
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| WO2015044165A1 (de) | 2013-09-26 | 2015-04-02 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
| EP3049390A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
| US20160237067A1 (en) | 2013-09-26 | 2016-08-18 | Bayer Pharma Aktiengesellschaft | Substituted phenylalanine derivatives |
| WO2015044170A1 (de) | 2013-09-26 | 2015-04-02 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate und ihre verwendung zur behandlung von thrombotischen / thromboembolischen erkrankungen |
| US20160229839A1 (en) | 2013-09-27 | 2016-08-11 | Merck Sharp & Dohme Corp. | Factor XIa Inhibitors |
| US20160257668A1 (en) | 2013-10-07 | 2016-09-08 | Merck Sharp & Dohme Corp. | Factor XIa Inhibitors |
| WO2015063093A1 (de) | 2013-10-30 | 2015-05-07 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate |
| CN106103453A (zh) | 2014-01-14 | 2016-11-09 | 大日本住友制药株式会社 | 缩合5‑噁唑烷酮衍生物 |
| RS57659B1 (sr) | 2014-01-31 | 2018-11-30 | Bristol Myers Squibb Co | Makrociklusi sa heterocikličnim p2' grupama kao inhibitori faktora xia |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| ES2945905T3 (es) | 2014-02-07 | 2023-07-10 | Exithera Pharmaceuticals Inc | Compuestos y composiciones terapéuticos |
| EP3104701B1 (en) | 2014-02-11 | 2019-01-30 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3104702B1 (en) | 2014-02-11 | 2022-08-10 | Merck Sharp & Dohme LLC | Factor xia inhibitors |
| US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| WO2015120777A1 (zh) | 2014-02-14 | 2015-08-20 | 四川海思科制药有限公司 | 一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用 |
| EP3134408B1 (en) | 2014-04-22 | 2020-08-12 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| MX2016015484A (es) | 2014-05-28 | 2017-03-23 | Merck Sharp & Dohme | Inhibidores del factor xia. |
| CN105658641B (zh) | 2014-07-25 | 2018-04-17 | 江苏恒瑞医药股份有限公司 | 氮茚‑酰胺类衍生物、其制备方法及其在医药上的应用 |
| WO2016015593A1 (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 |
| US10011585B2 (en) | 2014-07-28 | 2018-07-03 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| US10081623B2 (en) | 2014-09-04 | 2018-09-25 | Bristol-Myers Squibb Company | Diamide macrocycles that are FXIa inhibitors |
| WO2016118403A1 (en) | 2015-01-20 | 2016-07-28 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3283464B1 (en) | 2015-04-16 | 2019-10-23 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| WO2017095760A1 (en) | 2015-12-02 | 2017-06-08 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
-
2017
- 2017-08-21 US US15/681,478 patent/US10143681B2/en active Active
- 2017-08-21 TW TW106128248A patent/TW201808908A/zh unknown
- 2017-08-21 EP EP17758764.9A patent/EP3500556B1/en active Active
- 2017-08-21 WO PCT/US2017/047718 patent/WO2018039094A1/en active Application Filing
- 2017-08-22 AR ARP170102321A patent/AR109387A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2018039094A1 (en) | 2018-03-01 |
| EP3500556B1 (en) | 2023-08-02 |
| US10143681B2 (en) | 2018-12-04 |
| US20180050022A1 (en) | 2018-02-22 |
| TW201808908A (zh) | 2018-03-16 |
| EP3500556A1 (en) | 2019-06-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |