MX2016009385A - Inhibidores macrociclicos del factor xia condensados con heterociclicos. - Google Patents
Inhibidores macrociclicos del factor xia condensados con heterociclicos.Info
- Publication number
- MX2016009385A MX2016009385A MX2016009385A MX2016009385A MX2016009385A MX 2016009385 A MX2016009385 A MX 2016009385A MX 2016009385 A MX2016009385 A MX 2016009385A MX 2016009385 A MX2016009385 A MX 2016009385A MX 2016009385 A MX2016009385 A MX 2016009385A
- Authority
- MX
- Mexico
- Prior art keywords
- factor xia
- heterocycles
- condensed
- xia inhibitors
- compounds
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 108010080805 Factor XIa Proteins 0.000 title abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000003827 Plasma Kallikrein Human genes 0.000 abstract 1
- 108090000113 Plasma Kallikrein Proteins 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000009424 thromboembolic effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/18—Bridged systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/08—Bridged systems
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención proporciona compuestos de la Fórmula (Ia) (ver Fórmula) o estereoisómeros, tautómeros o sales de los mismos aceptables desde el punto de vista farmacéutico, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores selectivos del factor XIa o inhibidores duales de FXIa y calicreína plasmática. La presente invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos tromboembólicos y/o inflamatorios mediante su uso.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461933948P | 2014-01-31 | 2014-01-31 | |
| PCT/US2015/013647 WO2015116882A1 (en) | 2014-01-31 | 2015-01-30 | Macrocyclic factor xia inhibitors condensed with heterocycles |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2016009385A true MX2016009385A (es) | 2016-09-16 |
Family
ID=52484569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2016009385A MX2016009385A (es) | 2014-01-31 | 2015-01-30 | Inhibidores macrociclicos del factor xia condensados con heterociclicos. |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US20170057961A1 (es) |
| EP (1) | EP3099688B1 (es) |
| JP (1) | JP6419836B2 (es) |
| CN (1) | CN106459051B (es) |
| AR (1) | AR099228A1 (es) |
| BR (1) | BR112016016741B1 (es) |
| CA (1) | CA2937738C (es) |
| CY (1) | CY1120534T1 (es) |
| DK (1) | DK3099688T3 (es) |
| EA (1) | EA032650B1 (es) |
| ES (1) | ES2655540T3 (es) |
| HR (1) | HRP20172002T1 (es) |
| HU (1) | HUE038060T2 (es) |
| LT (1) | LT3099688T (es) |
| MX (1) | MX2016009385A (es) |
| NO (1) | NO2760821T3 (es) |
| PL (1) | PL3099688T3 (es) |
| PT (1) | PT3099688T (es) |
| RS (1) | RS56785B1 (es) |
| SI (1) | SI3099688T1 (es) |
| SM (1) | SMT201800024T1 (es) |
| TW (1) | TWI703144B (es) |
| UY (1) | UY35972A (es) |
| WO (1) | WO2015116882A1 (es) |
Families Citing this family (25)
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|---|---|---|---|---|
| SI2766346T1 (sl) | 2011-10-14 | 2017-05-31 | Bristol-Myers Squibb Company | Substituirane tetrahidroizokinolinske spojine kot faktor xia inhibitorji |
| WO2014160668A1 (en) | 2013-03-25 | 2014-10-02 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors |
| ES2893251T3 (es) | 2014-01-31 | 2022-02-08 | Bristol Myers Squibb Co | Macrociclos con grupos P2 heterocíclicos como inhibidores del factor XIa |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| 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 |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| NO2721243T3 (es) * | 2014-10-01 | 2018-10-20 | ||
| WO2016205482A1 (en) | 2015-06-19 | 2016-12-22 | 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 |
| EP3328851B1 (en) | 2015-07-29 | 2020-04-22 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties |
| US10214512B2 (en) * | 2015-10-29 | 2019-02-26 | Merck Sharp & Dohme Corp. | Factor XIA inhibitors |
| US10344039B2 (en) | 2015-10-29 | 2019-07-09 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor XIa inhibitors, pharmaceutically acceptable compositions and their use |
| EP3423458A1 (en) | 2016-03-02 | 2019-01-09 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
| US10143681B2 (en) | 2016-08-22 | 2018-12-04 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| CN110248938A (zh) | 2016-11-23 | 2019-09-17 | 拜耳作物科学股份公司 | 用作农药的2-[3-(烷基磺酰基)-2h-吲唑-2-基]-3h-咪唑并[4,5-b]吡啶衍生物和类似化合物 |
| WO2018130437A1 (de) | 2017-01-10 | 2018-07-19 | Bayer Aktiengesellschaft | Heterocyclen-derivate als schädlingsbekämpfungsmittel |
| JP7098630B2 (ja) | 2017-01-10 | 2022-07-11 | バイエル・アクチエンゲゼルシヤフト | 有害生物防除剤としてのヘテロサイクレン誘導体 |
| WO2018133793A1 (zh) * | 2017-01-18 | 2018-07-26 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
| CN110922412A (zh) * | 2018-09-20 | 2020-03-27 | 复旦大学 | 具有抗精神病作用药物化合物的不对称合成方法 |
| US12018027B2 (en) | 2019-04-16 | 2024-06-25 | China Resources Biopharmaceutical Company Limited | Macrocyclic derivatives acting as XIa factor inhibitor |
| CN114341714A (zh) * | 2019-07-08 | 2022-04-12 | 加里夏普创新有限责任公司 | 具有高对比度的紧凑型基于偏振的准直器 |
| CN114008047B (zh) * | 2019-07-23 | 2023-03-21 | 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 |
| 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 |
| CN117603208A (zh) * | 2021-04-21 | 2024-02-27 | 上海美悦生物科技发展有限公司 | FXIa抑制剂及其药物组合物、制备方法和用途 |
| CN119894901A (zh) * | 2023-06-30 | 2025-04-25 | 深圳信立泰药业股份有限公司 | 一种多取代的大环化合物及其制备方法与应用 |
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2012
- 2012-08-31 NO NO12780535A patent/NO2760821T3/no unknown
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2015
- 2015-01-30 BR BR112016016741-4A patent/BR112016016741B1/pt active IP Right Grant
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- 2015-01-30 DK DK15705427.1T patent/DK3099688T3/en active
- 2015-01-30 PL PL15705427T patent/PL3099688T3/pl unknown
- 2015-01-30 CA CA2937738A patent/CA2937738C/en active Active
- 2015-01-30 CN CN201580017759.3A patent/CN106459051B/zh active Active
- 2015-01-30 RS RS20180033A patent/RS56785B1/sr unknown
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- 2015-01-30 LT LTEP15705427.1T patent/LT3099688T/lt unknown
- 2015-01-30 SM SM20180024T patent/SMT201800024T1/it unknown
- 2015-01-30 SI SI201530121T patent/SI3099688T1/sl unknown
- 2015-01-30 HR HRP20172002TT patent/HRP20172002T1/hr unknown
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- 2015-01-30 EA EA201691561A patent/EA032650B1/ru not_active IP Right Cessation
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| TWI703144B (zh) | 2020-09-01 |
| BR112016016741A2 (es) | 2017-08-08 |
| HUE038060T2 (hu) | 2018-09-28 |
| LT3099688T (lt) | 2017-12-27 |
| TW201615640A (zh) | 2016-05-01 |
| PL3099688T3 (pl) | 2018-03-30 |
| HRP20172002T1 (hr) | 2018-02-09 |
| SMT201800024T1 (it) | 2018-03-08 |
| US20170057961A1 (en) | 2017-03-02 |
| CN106459051B (zh) | 2018-10-16 |
| US20170342071A1 (en) | 2017-11-30 |
| EP3099688A1 (en) | 2016-12-07 |
| ES2655540T3 (es) | 2018-02-20 |
| JP6419836B2 (ja) | 2018-11-07 |
| CY1120534T1 (el) | 2019-07-10 |
| CN106459051A (zh) | 2017-02-22 |
| US10273236B2 (en) | 2019-04-30 |
| DK3099688T3 (en) | 2018-01-15 |
| CA2937738C (en) | 2023-01-17 |
| US20180222907A1 (en) | 2018-08-09 |
| PT3099688T (pt) | 2018-01-15 |
| JP2017504640A (ja) | 2017-02-09 |
| RS56785B1 (sr) | 2018-04-30 |
| EA032650B1 (ru) | 2019-06-28 |
| SI3099688T1 (sl) | 2017-12-29 |
| AR099228A1 (es) | 2016-07-06 |
| EA201691561A1 (ru) | 2017-01-30 |
| WO2015116882A1 (en) | 2015-08-06 |
| UY35972A (es) | 2015-07-31 |
| NO2760821T3 (es) | 2018-03-10 |
| CA2937738A1 (en) | 2015-08-06 |
| BR112016016741B1 (pt) | 2023-01-17 |
| EP3099688B1 (en) | 2017-10-18 |
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