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 |
|---|---|---|---|---|
| EP3822264A4 (en) | 2018-07-02 | 2021-11-10 | Jiangsu Hengrui Medicine Co., Ltd. | CRYSTALLINE FORMS OF AN OXYPYRIDINE AMIDE DERIVATIVE AND THEIR PREPARATION PROCESS |
| 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 |
| CN116134025B (zh) * | 2020-09-17 | 2025-04-04 | 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 |
| CN116348109B (zh) * | 2020-09-17 | 2025-01-21 | 浙江海正药业股份有限公司 | 哌嗪类衍生物及其制备方法和用途 |
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| 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 |
| EP1425015A4 (en) | 2001-08-20 | 2004-12-15 | Bristol Myers Squibb Co | TETRAHYDROQUINOLINE DERIVATIVES FOR USE AS ANTITHROMBOTIC AGENTS |
| EP1523483A4 (en) | 2002-06-26 | 2006-03-08 | Bristol Myers Squibb Co | AMINO-BICYCLIC PYRAZINONE AND PYRIDINONE FOR INHIBITING THE COOKING OF SERIN PROTEASE |
| 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 |
| ATE479676T1 (de) | 2005-01-10 | 2010-09-15 | Bristol Myers Squibb Co | Als antikoagulanzien verwendbare phenylglycinamid-derivate |
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| 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 |
| MX2007013198A (es) | 2005-04-20 | 2008-03-24 | Johnson & Johnson | Moduladores de trombina de n-oxido de piridina fluorado y procedimiento para n-oxidacion de heteroarilos que contienen nitrogeno. |
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| WO2014160592A2 (en) | 2013-03-27 | 2014-10-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
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| EP3049408A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
| AR097754A1 (es) | 2013-09-26 | 2016-04-13 | Bayer Pharma AG | Derivados sustituidos de fenilalanina |
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| WO2015047973A1 (en) | 2013-09-27 | 2015-04-02 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| US20160257668A1 (en) | 2013-10-07 | 2016-09-08 | Merck Sharp & Dohme Corp. | Factor XIa Inhibitors |
| CA2928867A1 (en) | 2013-10-30 | 2015-05-07 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives |
| AU2014378428A1 (en) | 2014-01-14 | 2016-09-01 | Sumitomo Dainippon Pharma Co., Ltd. | Condensed 5-oxazolidinone derivative |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| UY35971A (es) | 2014-01-31 | 2015-07-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
| JP6382997B2 (ja) | 2014-02-07 | 2018-08-29 | エクセセーラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物および組成物 |
| WO2015123090A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3104703B1 (en) | 2014-02-11 | 2020-11-18 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| US9676723B2 (en) | 2014-02-11 | 2017-06-13 | 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 |
| US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| RU2016150410A (ru) | 2014-05-28 | 2018-06-28 | Мерк Шарп И Доум Корп. | Ингибиторы фактора 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 |
| EP3180317B1 (en) | 2014-07-28 | 2021-04-14 | 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 |
| CN107074821B (zh) | 2014-09-04 | 2020-05-22 | 百时美施贵宝公司 | 为fxia抑制剂的二酰胺大环化合物 |
| BR112017015431A2 (pt) | 2015-01-20 | 2018-01-16 | Merck Sharp & Dohme | composto, composição farmacêutica, métodos para inibir a formação de trombos no sangue ou tratar uma formação de trombos no sangue, para impedir a formação de trombos no sangue, para tratar tromboembolismo venoso e embolia pulmonar, para tratar trombose venosa profunda e para tratar ataque tromboembólico, e, uso de um composto |
| US10081617B2 (en) | 2015-04-16 | 2018-09-25 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| US10472344B2 (en) | 2015-12-02 | 2019-11-12 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
-
2017
- 2017-08-21 TW TW106128248A patent/TW201808908A/zh unknown
- 2017-08-21 WO PCT/US2017/047718 patent/WO2018039094A1/en not_active Ceased
- 2017-08-21 US US15/681,478 patent/US10143681B2/en active Active
- 2017-08-21 EP EP17758764.9A patent/EP3500556B1/en active Active
- 2017-08-22 AR ARP170102321A patent/AR109387A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20180050022A1 (en) | 2018-02-22 |
| WO2018039094A1 (en) | 2018-03-01 |
| TW201808908A (zh) | 2018-03-16 |
| EP3500556A1 (en) | 2019-06-26 |
| EP3500556B1 (en) | 2023-08-02 |
| US10143681B2 (en) | 2018-12-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |