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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103974938B (zh) | 2011-10-14 | 2016-11-09 | 百时美施贵宝公司 | 作为因子xia抑制剂的经取代的四氢异喹啉化合物 |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| TWI688564B (zh) | 2014-01-31 | 2020-03-21 | 美商必治妥美雅史谷比公司 | 作為凝血因子xia抑制劑之具有雜環p2'基團之巨環化合物 |
| WO2016036893A1 (en) | 2014-09-04 | 2016-03-10 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
| 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 | ||
| ES2762987T3 (es) | 2015-06-19 | 2020-05-26 | Bristol Myers Squibb Co | Macrociclos de diamida como inhibidores del factor XIA |
| ES2871111T3 (es) | 2015-07-29 | 2021-10-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático |
| KR102086934B1 (ko) * | 2015-07-29 | 2020-03-09 | 브리스톨-마이어스 스큅 컴퍼니 | 알킬 또는 시클로알킬 P2' 모이어티를 갖는 인자 XIa 마크로시클릭 억제제 |
| 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 |
| AU2016344476B2 (en) * | 2015-10-29 | 2020-08-13 | Merck Sharp & Dohme Llc | Factor XIa inhibitors |
| KR20180117156A (ko) | 2016-03-02 | 2018-10-26 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 |
| WO2018039094A1 (en) | 2016-08-22 | 2018-03-01 | Merck Sharp & Dohme Corp. | Pyridine-1-oxide derivatives and their use as 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 |
| AU2018207776B2 (en) | 2017-01-10 | 2021-06-17 | Bayer Aktiengesellschaft | Heterocyclene derivatives as pest control agents |
| MX2019008230A (es) | 2017-01-10 | 2019-10-24 | Bayer Ag | Derivados heterociclicos como agentes de control de plagas. |
| 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 |
| 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 |
| EP3957638B1 (en) * | 2019-04-16 | 2025-01-08 | China Resources Biopharmaceutical Company Limited | Macrocyclic derivatives acting as xia factor inhibitor |
| WO2021007354A1 (en) * | 2019-07-08 | 2021-01-14 | Gary Sharp Innovations, Llc | Compact polarization-based collimators with high contrast |
| JP7286001B2 (ja) * | 2019-07-23 | 2023-06-02 | メッドシャイン ディスカバリー インコーポレイテッド | 第XIa因子阻害剤としての大環状誘導体 |
| 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 |
| TWI877478B (zh) * | 2021-04-21 | 2025-03-21 | 大陸商上海美悦生物科技發展有限公司 | FXIa抑制劑及其藥物組合物、製備方法和用途 |
| 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 |
Family Cites Families (107)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR1525186A (fr) | 1967-03-29 | 1968-05-17 | Roussel Uclaf | Nouvelles pénicillines et procédé de préparation |
| DE3065190D1 (en) | 1979-11-05 | 1983-11-10 | 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 |
| EP0891352A4 (en) | 1996-04-03 | 2001-08-16 | 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. |
| TW557297B (en) | 1997-09-26 | 2003-10-11 | Abbott Lab | Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same |
| KR100898094B1 (ko) | 1998-03-19 | 2009-05-18 | 버텍스 파마슈티칼스 인코포레이티드 | 카스파제의 억제제 |
| 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 |
| AU3043100A (en) | 1999-01-02 | 2000-07-24 | Aventis Pharma Deutschland Gmbh | Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity) |
| 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) |
| DE50008510D1 (de) | 1999-04-09 | 2004-12-09 | Abbott Gmbh & Co Kg | Niedermolekulare inhibitoren von komplementproteasen |
| CA2383008A1 (en) | 1999-06-14 | 2000-12-21 | Amanda Jane Lyons | Compounds |
| 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 |
| CA2408486A1 (en) | 2000-05-11 | 2001-11-15 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs useful as growth hormone secretagogues |
| 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 |
| AU2002322802A1 (en) | 2001-07-27 | 2003-02-17 | Merck And Co., Inc. | Thrombin inhibitors |
| US6951840B2 (en) | 2001-08-31 | 2005-10-04 | Eli Lilly And Company | Lipoglycopeptide antibiotics |
| CN110894196A (zh) | 2001-09-21 | 2020-03-20 | 百时美-施贵宝控股爱尔兰无限公司 | 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂 |
| WO2003041641A2 (en) | 2001-11-09 | 2003-05-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
| WO2003106438A1 (en) | 2002-06-18 | 2003-12-24 | The Scripps Research Institute | Synthesis of diazonamide "a" core |
| 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 |
| CA2531796A1 (en) | 2003-08-08 | 2005-02-17 | Transtech Pharma, Inc. | 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 |
| EP2457895A1 (en) | 2004-07-12 | 2012-05-30 | Idun Pharmaceuticals, Inc. | Tetrapeptide analogs |
| 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 |
| 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 |
| WO2007047608A2 (en) | 2005-10-14 | 2007-04-26 | Epix Pharmaceuticals, Inc. | Fibrin targeted therapeutics |
| AU2006311101A1 (en) | 2005-11-11 | 2007-05-18 | F. Hoffmann-La Roche Ag | Carbocyclic fused cyclic amines as inhibitors of the coagulation factor Xa |
| JP2009519966A (ja) | 2005-12-14 | 2009-05-21 | ブリストル−マイヤーズ スクイブ カンパニー | セリンプロテアーゼ阻害剤として有用な6員ヘテロ環 |
| US7626039B2 (en) | 2005-12-14 | 2009-12-01 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, ayrlpropynamide, or arylmethylurea analogs as factor XIa inhibitors |
| WO2007070816A2 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Thiophene derivatives as factor xia inhibitors |
| AR058380A1 (es) | 2005-12-23 | 2008-01-30 | Bristol Myers Squibb Co | Inhibidores del factor viia macrociclicos utiles como anticoagulantes |
| WO2008076805A2 (en) | 2006-12-15 | 2008-06-26 | Bristol-Myers Squibb Company | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor xia inhibitors |
| PE20081775A1 (es) | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| AU2008266228A1 (en) | 2007-06-13 | 2008-12-24 | Bristol-Myers Squibb Company | Dipeptide analogs as coagulation factor inhibitors |
| WO2009114677A1 (en) | 2008-03-13 | 2009-09-17 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
| US8624040B2 (en) | 2009-06-22 | 2014-01-07 | 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 |
| EP2462123B1 (en) | 2009-08-04 | 2013-10-02 | Merck Sharp & Dohme Corp. | 4,5,6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
| EP2534152B1 (en) | 2010-02-11 | 2018-05-02 | 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 |
| ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
| IN2014CN02805A (es) | 2011-10-14 | 2015-07-03 | Bristol Myers Squibb Co | |
| CN103974938B (zh) | 2011-10-14 | 2016-11-09 | 百时美施贵宝公司 | 作为因子xia抑制剂的经取代的四氢异喹啉化合物 |
| CN104136431B (zh) | 2011-12-21 | 2017-03-15 | 小野药品工业株式会社 | 作为凝血因子XIa抑制剂的吡啶酮和嘧啶酮衍生物 |
| GB2497806A (en) | 2011-12-21 | 2013-06-26 | Ono Pharmaceutical Co | Pyridinone and pyrimidinone derivatives as factor XIa inhibitors |
| EP2807156A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | Aminopyridine derivatives as plasma kallikrein inhibitors |
| WO2013111108A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | 5-membered heteroarylcarboxamide 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 |
| EP2847228B1 (en) | 2012-05-10 | 2018-07-25 | Bayer Pharma Aktiengesellschaft | Antibodies capable of binding to the coagulation factor xi and/or its activated form factor xia and uses thereof |
| GB201209138D0 (en) | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
| AU2013291098A1 (en) | 2012-07-19 | 2015-02-05 | Sumitomo Dainippon Pharma Co., Ltd. | 1-(cycloalkyl-carbonyl)proline derivative |
| SG11201500270RA (en) * | 2012-08-03 | 2015-03-30 | Bristol Myers Squibb Co | Dihydropyridone p1 as factor xia inhibitors |
| US9409908B2 (en) * | 2012-08-03 | 2016-08-09 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor XIa inhibitors |
| JP6154473B2 (ja) | 2012-10-12 | 2017-06-28 | 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因子阻害剤の結晶形 |
| US9315519B2 (en) | 2012-10-12 | 2016-04-19 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| WO2014120346A1 (en) | 2012-12-19 | 2014-08-07 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
| GB201300304D0 (en) | 2013-01-08 | 2013-02-20 | Kalvista Pharmaceuticals Ltd | Benzylamine derivatives |
| GB2510407A (en) | 2013-02-04 | 2014-08-06 | Kalvista Pharmaceuticals Ltd | Aqueous suspensions of kallikrein inhibitors for parenteral administration |
| ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
| TWI633089B (zh) | 2013-03-28 | 2018-08-21 | 拜耳製藥股份有限公司 | 經取代的酮基吡啶衍生物 |
| US9475809B2 (en) | 2013-07-23 | 2016-10-25 | Bayer Pharma Aktiengesellschaft | Substituted oxopyridine derivatives and use thereof as factor xia/plasma |
| EP3049404A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
| EP3049403A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
| WO2015044173A1 (de) | 2013-09-26 | 2015-04-02 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate als faktor xia modulatoren |
| EP3049394A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate als faktor xia modulatoren |
| EP3049408A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
| TW201605809A (zh) | 2013-09-26 | 2016-02-16 | 拜耳製藥股份有限公司 | 經取代苯丙胺酸衍生物(一) |
| US20160237044A1 (en) | 2013-09-26 | 2016-08-18 | Bayer Pharma Aktiengesellschaft | Substituted phenylalanine derivatives |
| MA38925B1 (fr) | 2013-09-26 | 2018-09-28 | Bayer Pharma AG | Dérivés de phénylalanine substitués |
| EP3049435A4 (en) | 2013-09-27 | 2017-03-29 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| EP3054944B1 (en) | 2013-10-07 | 2019-12-04 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| JP6337750B2 (ja) | 2013-11-22 | 2018-06-06 | 小野薬品工業株式会社 | 化合物 |
| CA2939326A1 (en) | 2014-01-14 | 2015-07-23 | Sumitomo Dainippon Pharma Co., Ltd. | Condensed 5-oxazolidinone derivative |
| NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
| TWI688564B (zh) | 2014-01-31 | 2020-03-21 | 美商必治妥美雅史谷比公司 | 作為凝血因子xia抑制劑之具有雜環p2'基團之巨環化合物 |
| KR101927114B1 (ko) | 2014-02-07 | 2018-12-10 | 엑시테라 파마슈티컬스 인코퍼레이티드 | 치료 화합물 및 조성물 |
| US9676723B2 (en) | 2014-02-11 | 2017-06-13 | Merck Sharp & Dohme Corp | Factor XIa inhibitors |
| US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| EP3104701B1 (en) | 2014-02-11 | 2019-01-30 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| CN105829298B (zh) | 2014-02-14 | 2019-02-01 | 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 |
| PL3828173T3 (pl) | 2014-03-07 | 2022-12-19 | Biocryst Pharmaceuticals, Inc. | Podstawiane pirazole jako inhibitory ludzkiej kalikreiny osoczowej |
| US9969724B2 (en) | 2014-04-16 | 2018-05-15 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
| WO2015160634A1 (en) | 2014-04-16 | 2015-10-22 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
| KR20150136294A (ko) | 2014-05-27 | 2015-12-07 | 주식회사 레고켐 바이오사이언스 | 인자 XIa 억제 활성을 가지는 신규한 화합물 |
| KR20170005871A (ko) | 2014-05-28 | 2017-01-16 | 머크 샤프 앤드 돔 코포레이션 | 인자 XIa 억제제 |
| ES2712886T3 (es) | 2014-09-24 | 2019-05-16 | Bayer Pharma AG | Derivados de piridobenzazepina y piridobenzazocina que inhiben el factor XIa |
| 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 | ||
| EP3231803B1 (en) | 2014-12-10 | 2020-07-01 | ONO Pharmaceutical Co., Ltd. | Dihydroindolizinone derivative |
| ES2762987T3 (es) | 2015-06-19 | 2020-05-26 | Bristol Myers Squibb Co | Macrociclos de diamida como inhibidores del factor XIA |
-
2012
- 2012-08-31 NO NO12780535A patent/NO2760821T3/no unknown
-
2015
- 2015-01-30 CN CN201580017759.3A patent/CN106459051B/zh active Active
- 2015-01-30 ES ES15705427.1T patent/ES2655540T3/es active Active
- 2015-01-30 HR HRP20172002TT patent/HRP20172002T1/hr unknown
- 2015-01-30 EA EA201691561A patent/EA032650B1/ru not_active IP Right Cessation
- 2015-01-30 BR BR112016016741-4A patent/BR112016016741B1/pt active IP Right Grant
- 2015-01-30 WO PCT/US2015/013647 patent/WO2015116882A1/en not_active Ceased
- 2015-01-30 HU HUE15705427A patent/HUE038060T2/hu unknown
- 2015-01-30 LT LTEP15705427.1T patent/LT3099688T/lt unknown
- 2015-01-30 RS RS20180033A patent/RS56785B1/sr unknown
- 2015-01-30 TW TW104103315A patent/TWI703144B/zh active
- 2015-01-30 JP JP2016549270A patent/JP6419836B2/ja active Active
- 2015-01-30 PT PT157054271T patent/PT3099688T/pt unknown
- 2015-01-30 SI SI201530121T patent/SI3099688T1/sl unknown
- 2015-01-30 DK DK15705427.1T patent/DK3099688T3/en active
- 2015-01-30 EP EP15705427.1A patent/EP3099688B1/en active Active
- 2015-01-30 UY UY0001035972A patent/UY35972A/es active IP Right Grant
- 2015-01-30 CA CA2937738A patent/CA2937738C/en active Active
- 2015-01-30 US US15/115,319 patent/US20170057961A1/en not_active Abandoned
- 2015-01-30 AR ARP150100295A patent/AR099228A1/es unknown
- 2015-01-30 PL PL15705427T patent/PL3099688T3/pl unknown
- 2015-01-30 MX MX2016009385A patent/MX2016009385A/es active IP Right Grant
- 2015-01-30 SM SM20180024T patent/SMT201800024T1/it unknown
-
2017
- 2017-08-18 US US15/680,729 patent/US20170342071A1/en not_active Abandoned
- 2017-12-29 CY CY20171101357T patent/CY1120534T1/el unknown
-
2018
- 2018-04-06 US US15/946,837 patent/US10273236B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2015116882A1 (en) | 2015-08-06 |
| HUE038060T2 (hu) | 2018-09-28 |
| BR112016016741B1 (pt) | 2023-01-17 |
| RS56785B1 (sr) | 2018-04-30 |
| SI3099688T1 (sl) | 2017-12-29 |
| DK3099688T3 (en) | 2018-01-15 |
| SMT201800024T1 (it) | 2018-03-08 |
| TW201615640A (zh) | 2016-05-01 |
| HRP20172002T1 (hr) | 2018-02-09 |
| NO2760821T3 (es) | 2018-03-10 |
| JP6419836B2 (ja) | 2018-11-07 |
| US20170057961A1 (en) | 2017-03-02 |
| ES2655540T3 (es) | 2018-02-20 |
| TWI703144B (zh) | 2020-09-01 |
| PL3099688T3 (pl) | 2018-03-30 |
| CN106459051B (zh) | 2018-10-16 |
| EP3099688B1 (en) | 2017-10-18 |
| AR099228A1 (es) | 2016-07-06 |
| US20180222907A1 (en) | 2018-08-09 |
| LT3099688T (lt) | 2017-12-27 |
| EA032650B1 (ru) | 2019-06-28 |
| CA2937738A1 (en) | 2015-08-06 |
| PT3099688T (pt) | 2018-01-15 |
| US20170342071A1 (en) | 2017-11-30 |
| EP3099688A1 (en) | 2016-12-07 |
| UY35972A (es) | 2015-07-31 |
| CY1120534T1 (el) | 2019-07-10 |
| EA201691561A1 (ru) | 2017-01-30 |
| US10273236B2 (en) | 2019-04-30 |
| JP2017504640A (ja) | 2017-02-09 |
| CN106459051A (zh) | 2017-02-22 |
| BR112016016741A2 (es) | 2017-08-08 |
| CA2937738C (en) | 2023-01-17 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PH12021550418A1 (en) | Macrocycles with hetrocyclic p2` groups as factor xia inhibitors | |
| PH12020500195A1 (en) | Pyrimidinones as factor xia inhibitors | |
| MX2016009385A (es) | Inhibidores macrociclicos del factor xia condensados con heterociclicos. | |
| MX2015000892A (es) | Dihidropiridona p1 como inhibidores del factor xia. | |
| MX2015000919A (es) | Dihidropiridona p1 como inhibidores del factor xia. | |
| PH12012501589A1 (en) | Macrocycles as factor xia inhibitors | |
| PH12015502248A1 (en) | 6-(5-hydroxy-1h-pyrazol-1-yl)nicotinamide derivatives and their use as phd inhibitors | |
| EA201490418A1 (ru) | Новые макроциклические соединения в качестве ингибиторов фактора xia | |
| HK1217492A1 (zh) | 作爲刺猬信号通路抑制剂的杂环化合物 | |
| TH170796A (th) | พิริมิดีนในฐานะเป็นตัวยับยั้งแฟคเตอร์ xia |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |