UY35975A - Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia - Google Patents
Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xiaInfo
- Publication number
- UY35975A UY35975A UY0001035975A UY35975A UY35975A UY 35975 A UY35975 A UY 35975A UY 0001035975 A UY0001035975 A UY 0001035975A UY 35975 A UY35975 A UY 35975A UY 35975 A UY35975 A UY 35975A
- Authority
- UY
- Uruguay
- Prior art keywords
- inhibitors
- macrociclos
- heterocycles
- groups
- compounds
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 3
- 108010080805 Factor XIa Proteins 0.000 abstract 1
- 102000003827 Plasma Kallikrein Human genes 0.000 abstract 1
- 108090000113 Plasma Kallikrein Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 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
- C07D471/02—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 two hetero rings
- C07D471/08—Bridged systems
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
-
- 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
- A61P9/10—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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
-
- 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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Epidemiology (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
La presente invención proporciona compuestos de la Fórmula (I): o estereoisómeros, tautómeros o sales de aquellos 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 prese nte 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 |
---|---|---|---|
US201461933942P | 2014-01-31 | 2014-01-31 | |
US201462058293P | 2014-10-01 | 2014-10-01 |
Publications (1)
Publication Number | Publication Date |
---|---|
UY35975A true UY35975A (es) | 2015-07-31 |
Family
ID=52484570
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UY0001035971A UY35971A (es) | 2014-01-31 | 2015-01-30 | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
UY0001035975A UY35975A (es) | 2014-01-31 | 2015-01-30 | Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
UY0001035971A UY35971A (es) | 2014-01-31 | 2015-01-30 | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia |
Country Status (31)
Country | Link |
---|---|
US (2) | US20170002006A1 (es) |
EP (4) | EP3099686B1 (es) |
JP (6) | JP6464176B2 (es) |
KR (3) | KR102413453B1 (es) |
CN (4) | CN110845498B (es) |
AU (4) | AU2015210904C1 (es) |
BR (1) | BR112016015717B1 (es) |
CA (1) | CA2937739C (es) |
CL (1) | CL2016001933A1 (es) |
CY (1) | CY1120702T1 (es) |
DK (1) | DK3099687T3 (es) |
EA (1) | EA030222B1 (es) |
ES (3) | ES2687498T3 (es) |
HR (1) | HRP20181339T1 (es) |
HU (1) | HUE040226T2 (es) |
IL (4) | IL307212A (es) |
LT (1) | LT3099687T (es) |
MX (2) | MX2016009230A (es) |
MY (1) | MY190429A (es) |
NZ (2) | NZ723762A (es) |
PE (2) | PE20161069A1 (es) |
PH (2) | PH12016501249A1 (es) |
PL (1) | PL3099687T3 (es) |
PT (1) | PT3099687T (es) |
RS (1) | RS57659B1 (es) |
SG (2) | SG11201606209PA (es) |
SI (1) | SI3099687T1 (es) |
TW (4) | TWI790421B (es) |
UY (2) | UY35971A (es) |
WO (2) | WO2015116885A1 (es) |
ZA (1) | ZA201606011B (es) |
Families Citing this family (42)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB201116559D0 (en) | 2011-09-26 | 2011-11-09 | Univ Leuven Kath | Novel viral replication inhibitors |
SG11201401384UA (en) | 2011-10-14 | 2014-09-26 | Bristol Myers Squibb Co | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
IL307212A (en) * | 2014-01-31 | 2023-11-01 | Bristol Myers Squibb Co | Macrocyclines with P2' heterocyclic groups as factor XIA inhibitors |
EP2913330A1 (en) | 2014-02-27 | 2015-09-02 | Laboratoire Biodim | Condensed derivatives of imidazole useful as pharmaceuticals |
US10081623B2 (en) | 2014-09-04 | 2018-09-25 | Bristol-Myers Squibb Company | Diamide macrocycles that are FXIa inhibitors |
BR112017006622A2 (pt) | 2014-10-01 | 2018-07-03 | Merck Patent Gmbh | derivados de ácido borônico |
NO2721243T3 (es) * | 2014-10-01 | 2018-10-20 | ||
US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
JOP20160086B1 (ar) | 2015-05-08 | 2021-08-17 | 2 Katholieke Univ Leuven Ku Leuven Research And Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
US10160750B2 (en) | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
JO3703B1 (ar) | 2015-07-09 | 2021-01-31 | Bayer Pharma AG | مشتقات أوكسوبيريدين مستبدلة |
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 |
CN114805365B (zh) | 2015-07-29 | 2024-07-23 | 百时美施贵宝公司 | 携带非芳族p2′基团的因子xia新大环 |
JO3633B1 (ar) | 2015-09-16 | 2020-08-27 | Katholieke Univ Leuven Ku Leuven Research & Development | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JOP20160198B1 (ar) | 2015-09-16 | 2022-03-14 | Janssen Pharmaceuticals Inc | مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
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 |
KR20180073602A (ko) * | 2015-10-29 | 2018-07-02 | 머크 샤프 앤드 돔 코포레이션 | 인자 XIa 억제제 |
JP2019507167A (ja) | 2016-03-02 | 2019-03-14 | 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因子阻害活性を有するジアミド大員環 |
SG11201808270PA (en) | 2016-03-31 | 2018-10-30 | Janssen Pharmaceuticals Inc | Substituted indoline derivatives as dengue viral replication inhibitors |
EP3436435B1 (en) | 2016-03-31 | 2021-05-12 | Janssen Pharmaceuticals, Inc. | Substituted indole derivatives as dengue viral replication inhibitors |
MA44502A (fr) | 2016-04-01 | 2019-02-06 | Janssen Pharmaceuticals Inc | Dérivés d'indole substitués utilisés en tant qu'inhibiteurs de réplication du virus de la dengue |
JOP20170069B1 (ar) | 2016-04-01 | 2021-08-17 | 1 Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
AR109304A1 (es) | 2016-08-10 | 2018-11-21 | Sumitomo Chemical Co | Compuesto de oxadiazol y su uso |
US10143681B2 (en) | 2016-08-22 | 2018-12-04 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
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 |
JOP20180025B1 (ar) | 2017-03-31 | 2021-08-17 | Janssen Pharmaceuticals Inc | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
JOP20180026A1 (ar) | 2017-03-31 | 2019-01-30 | Univ Leuven Kath | مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك |
KR102625991B1 (ko) | 2017-05-22 | 2024-01-16 | 얀센 파마슈티칼즈, 인코포레이티드 | 뎅기 바이러스 복제 억제제로서의 치환 인돌린 유도체 |
KR102625988B1 (ko) | 2017-05-22 | 2024-01-16 | 얀센 파마슈티칼즈, 인코포레이티드 | 뎅기 바이러스 복제 억제제로서의 치환 인돌린 유도체 |
WO2019011166A1 (zh) * | 2017-07-14 | 2019-01-17 | 四川科伦博泰生物医药股份有限公司 | 大环酰胺化合物及其药物组合物和用途 |
TW202104188A (zh) | 2019-04-11 | 2021-02-01 | 美商必治妥美雅史谷比公司 | 製備(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-(二氧甲基)-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)-酮之新穎合成選項 |
MX2021012288A (es) * | 2019-04-11 | 2021-11-12 | Bristol Myers Squibb Co | Rendimiento mejorado de formulaciones solidas amorfas y solubilizadas para lograr concentraciones plasmaticas terapeuticas. |
WO2020211781A1 (zh) | 2019-04-16 | 2020-10-22 | 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 |
US20220281868A1 (en) | 2019-07-23 | 2022-09-08 | Medshine Discovery Inc. | Macrocyclic derivatives as factor xia inhibitors |
TWI749881B (zh) * | 2019-11-21 | 2021-12-11 | 大陸商深圳信立泰藥業股份有限公司 | 二氧代哌類衍生物、其製備方法及其在醫藥上的應用 |
CN112608274B (zh) * | 2020-12-30 | 2022-09-06 | 西南大学 | 一种手性胺化合物的催化合成方法及其化合物 |
CN112876461B (zh) * | 2021-01-20 | 2022-12-30 | 上海零诺生物科技有限公司 | 尼古丁及其中间体的制备方法 |
CN115215867B (zh) * | 2021-04-21 | 2023-12-26 | 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 |
WO2023150591A2 (en) * | 2022-02-03 | 2023-08-10 | D.E. Shaw Research, Llc | Pyridazinone compounds as trpa1 inhibitors |
WO2023240140A1 (en) * | 2022-06-08 | 2023-12-14 | Blossomhill Therapeutics, Inc. | Indazole macrocycles and their use |
Family Cites Families (110)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR1525186A (fr) | 1967-03-29 | 1968-05-17 | Roussel Uclaf | Nouvelles pénicillines et procédé de préparation |
EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | 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 |
WO1996034010A2 (en) | 1995-03-29 | 1996-10-31 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
US5624936A (en) | 1995-03-29 | 1997-04-29 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
US5869682A (en) | 1996-04-03 | 1999-02-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
JP2000507597A (ja) | 1996-04-03 | 2000-06-20 | メルク エンド カンパニー インコーポレーテッド | ファルネシルタンパク質トランスフェラーゼ阻害剤 |
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 |
AP2000001919A0 (en) | 1998-03-19 | 2000-09-30 | Vertex Pharma | Inhibitors of caspases. |
HUP0102514A3 (en) | 1998-05-26 | 2002-03-28 | Warner Lambert Co | Pyrido-pyrimidin and pyrimido-pyrimidin derivatives as inhibitors of cellular proliferation and pharmaceutical compositions thereof |
US6307049B1 (en) | 1998-09-30 | 2001-10-23 | The Procter & Gamble Co. | Heterocyclic 2-substituted ketoamides |
CA2358578A1 (en) | 1999-01-02 | 2000-07-13 | 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 |
WO2000076970A2 (en) | 1999-06-14 | 2000-12-21 | Eli Lilly And Company | Serine protease inhibitors |
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 |
BR0110638A (pt) | 2000-05-11 | 2003-03-25 | Bristol Myers Squibb Co | Análogos de tetraidroisoquinolina úteis como secretagogos de hormÈnio do crescimento |
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 |
WO2003011222A2 (en) * | 2001-07-27 | 2003-02-13 | Merck & Co., Inc. | Thrombin inhibitors |
US6951840B2 (en) | 2001-08-31 | 2005-10-04 | Eli Lilly And Company | Lipoglycopeptide antibiotics |
CN104744461A (zh) | 2001-09-21 | 2015-07-01 | 百时美施贵宝公司 | 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂 |
AU2002357692A1 (en) | 2001-11-09 | 2003-05-26 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
AU2002316317A1 (en) | 2002-06-18 | 2003-12-31 | 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 |
WO2005014533A2 (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 |
EA200700225A1 (ru) | 2004-07-12 | 2008-02-28 | Айдан Фармасьютикалз, Инк. | Аналоги тетрапептида |
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 |
US20070111947A1 (en) | 2005-10-14 | 2007-05-17 | Mcmurry Thomas J | Fibrin targeted therapeutics |
BRPI0618523A2 (pt) | 2005-11-11 | 2011-09-06 | Hoffmann La Roche | compostos de aminas cìclicas fundidas carbocìclicas, composições farmacêuticas e usos dos mesmos |
NZ568595A (en) | 2005-12-14 | 2010-04-30 | Bristol Myers Squibb Co | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors |
US8466295B2 (en) | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
US8163749B2 (en) | 2005-12-14 | 2012-04-24 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
TW200745062A (en) | 2005-12-23 | 2007-12-16 | Bristol Myers Squibb Co | Macrocyclic factor VIIA inhibitors useful as anticoagulants |
CN101389613B (zh) * | 2005-12-23 | 2011-10-12 | 布里斯托尔-迈尔斯.斯奎布公司 | 用作抗凝血药的大环凝血因子viia抑制剂 |
US8410155B2 (en) | 2006-12-15 | 2013-04-02 | 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 |
WO2008157162A1 (en) | 2007-06-13 | 2008-12-24 | Bristol-Myers Squibb Company | Dipeptide analogs as coagulation factor inhibitors |
EP2265601B1 (en) | 2008-03-13 | 2012-02-01 | Bristol-Myers Squibb Company | Pyridazine derivatives as factor xia inhibitors |
WO2010151317A1 (en) | 2009-06-22 | 2010-12-29 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
WO2011002520A2 (en) | 2009-07-02 | 2011-01-06 | 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 |
CN102596933B (zh) * | 2009-09-09 | 2014-09-17 | 杜邦公司 | 除草剂嘧啶酮衍生物 |
CA2789622C (en) * | 2010-02-11 | 2018-04-03 | Bristol-Myers Squibb Company | Macrocycles as factor xia inhibitors |
WO2013009527A2 (en) | 2011-07-08 | 2013-01-17 | 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 |
SG11201401384UA (en) | 2011-10-14 | 2014-09-26 | Bristol Myers Squibb Co | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
US9079929B2 (en) | 2011-10-14 | 2015-07-14 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors |
US9108951B2 (en) | 2011-10-14 | 2015-08-18 | Bristol-Myers Squibb Company | Substituted 5,6,7,8-tetrahydro-1,6-naphthyridines as factor XIa inhibitors |
GB2497806A (en) | 2011-12-21 | 2013-06-26 | Ono Pharmaceutical Co | Pyridinone and pyrimidinone derivatives as factor XIa inhibitors |
IN2014CN04676A (es) * | 2011-12-21 | 2015-09-18 | Ono Pharmaceutical Co | |
EP2807157A1 (en) | 2012-01-27 | 2014-12-03 | Novartis AG | 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors |
WO2013111107A1 (en) | 2012-01-27 | 2013-08-01 | Novartis Ag | Aminopyridine 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 |
ES2698950T3 (es) | 2012-05-10 | 2019-02-06 | Bayer Pharma AG | Anticuerpos capaces de unirse al Factor XI de coagulación y/o a su forma activada, Factor XIa, y usos de los mismos |
GB201209138D0 (en) | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
CN104640843A (zh) | 2012-07-19 | 2015-05-20 | 大日本住友制药株式会社 | 1-(环烷基羰基)脯氨酸衍生物 |
WO2014022767A1 (en) * | 2012-08-03 | 2014-02-06 | Bristol-Myers Squibb Company | Dihydropyridone p1 as factor xia inhibitors |
KR20150038369A (ko) | 2012-08-03 | 2015-04-08 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제제로서의 디히드로피리돈 P1 |
SG11201502605PA (en) | 2012-10-12 | 2015-05-28 | Bristol Myers Squibb Co | Crystalline forms of a factor xia inhibitor |
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 |
EP2934538B1 (en) | 2012-12-19 | 2021-03-31 | 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 |
US9738655B2 (en) | 2013-03-25 | 2017-08-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors |
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 |
WO2015011087A1 (de) | 2013-07-23 | 2015-01-29 | Bayer Pharma Aktiengesellschaft | Substituierte oxopyridin-derivate und ihre verwendung als faktor xia / plasma |
US20160280688A1 (en) | 2013-09-26 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Substituted phenylalanine derivatives |
WO2015044169A1 (de) | 2013-09-26 | 2015-04-02 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
US20160280699A1 (en) | 2013-09-26 | 2016-09-29 | Bayer Pharma Aktiengesellschaft | Substituted phenylalanine derivatives |
SG11201601963TA (en) | 2013-09-26 | 2016-04-28 | Bayer Pharma AG | Substituted phenylalanine derivatives |
WO2015044173A1 (de) | 2013-09-26 | 2015-04-02 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate als faktor xia modulatoren |
EP3049404A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate |
EP3049406A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate und ihre verwendung zur behandlung von thrombotischen / thromboembolischen erkrankungen |
EP3049394A1 (de) | 2013-09-26 | 2016-08-03 | Bayer Pharma Aktiengesellschaft | Substituierte phenylalanin-derivate als faktor xia modulatoren |
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 |
JP6337750B2 (ja) | 2013-11-22 | 2018-06-06 | 小野薬品工業株式会社 | 化合物 |
KR20160107322A (ko) | 2014-01-14 | 2016-09-13 | 다이닛본 스미토모 세이야꾸 가부시끼가이샤 | 축합 5-옥사졸리디논 유도체 |
IL307212A (en) * | 2014-01-31 | 2023-11-01 | Bristol Myers Squibb Co | Macrocyclines with P2' heterocyclic groups as factor XIA inhibitors |
NO2760821T3 (es) | 2014-01-31 | 2018-03-10 | ||
EP3102200B1 (en) | 2014-02-07 | 2023-04-05 | Exithera Pharmaceuticals Inc. | Therapeutic compounds and compositions |
US9944643B2 (en) | 2014-02-11 | 2018-04-17 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
WO2015123091A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
US9663527B2 (en) | 2014-02-11 | 2017-05-30 | 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 |
KR20230042384A (ko) | 2014-03-07 | 2023-03-28 | 바이오크리스트파마슈티컬즈,인코포레이티드 | 인간 혈장 칼리크레인 저해제 |
WO2015160636A1 (en) | 2014-04-16 | 2015-10-22 | Merck Sharp & Dohme Corp. | Factor ixa inhibitors |
US9808445B2 (en) | 2014-04-16 | 2017-11-07 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
GB201409202D0 (en) * | 2014-05-23 | 2014-07-09 | Ffei Ltd | Improvements in imaging microscope samples |
KR20150136294A (ko) | 2014-05-27 | 2015-12-07 | 주식회사 레고켐 바이오사이언스 | 인자 XIa 억제 활성을 가지는 신규한 화합물 |
WO2015183709A1 (en) | 2014-05-28 | 2015-12-03 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
WO2016046157A1 (de) | 2014-09-24 | 2016-03-31 | Bayer Pharma Aktiengesellschaft | Faktor xia hemmende pyridobenzazepin- und pyridobenzazocin-derivate |
NO2721243T3 (es) * | 2014-10-01 | 2018-10-20 | ||
US9453018B2 (en) * | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
CN107001363B (zh) | 2014-12-10 | 2019-06-21 | 小野药品工业株式会社 | 二氢吲嗪酮衍生物 |
US10160750B2 (en) | 2015-06-19 | 2018-12-25 | Bristol-Myers Squibb Company | Diamide macrocycles as factor XIa inhibitors |
-
2015
- 2015-01-30 IL IL307212A patent/IL307212A/en unknown
- 2015-01-30 UY UY0001035971A patent/UY35971A/es not_active Application Discontinuation
- 2015-01-30 SG SG11201606209PA patent/SG11201606209PA/en unknown
- 2015-01-30 RS RS20181028A patent/RS57659B1/sr unknown
- 2015-01-30 JP JP2016549277A patent/JP6464176B2/ja active Active
- 2015-01-30 CN CN201911001057.2A patent/CN110845498B/zh active Active
- 2015-01-30 TW TW109105925A patent/TWI790421B/zh active
- 2015-01-30 EP EP15705428.9A patent/EP3099686B1/en active Active
- 2015-01-30 DK DK15705860.3T patent/DK3099687T3/en active
- 2015-01-30 CN CN201580006495.1A patent/CN105980384B/zh active Active
- 2015-01-30 TW TW104103305A patent/TW201613922A/zh unknown
- 2015-01-30 US US15/115,327 patent/US20170002006A1/en not_active Abandoned
- 2015-01-30 MY MYPI2016702666A patent/MY190429A/en unknown
- 2015-01-30 MX MX2016009230A patent/MX2016009230A/es active IP Right Grant
- 2015-01-30 JP JP2016549279A patent/JP6505727B2/ja active Active
- 2015-01-30 CN CN201580017440.0A patent/CN106132962B/zh active Active
- 2015-01-30 AU AU2015210904A patent/AU2015210904C1/en active Active
- 2015-01-30 SG SG10201908467R patent/SG10201908467RA/en unknown
- 2015-01-30 EP EP15705860.3A patent/EP3099687B1/en active Active
- 2015-01-30 LT LTEP15705860.3T patent/LT3099687T/lt unknown
- 2015-01-30 ES ES15705860.3T patent/ES2687498T3/es active Active
- 2015-01-30 IL IL298983A patent/IL298983B2/en unknown
- 2015-01-30 US US15/115,314 patent/US9777001B2/en active Active
- 2015-01-30 PL PL15705860T patent/PL3099687T3/pl unknown
- 2015-01-30 NZ NZ723762A patent/NZ723762A/en unknown
- 2015-01-30 NZ NZ761182A patent/NZ761182A/en unknown
- 2015-01-30 PT PT15705860T patent/PT3099687T/pt unknown
- 2015-01-30 CN CN202310156065.4A patent/CN116987080A/zh active Pending
- 2015-01-30 ES ES15705428T patent/ES2784841T3/es active Active
- 2015-01-30 TW TW104103366A patent/TWI688564B/zh active
- 2015-01-30 KR KR1020167023481A patent/KR102413453B1/ko active IP Right Grant
- 2015-01-30 PE PE2016001274A patent/PE20161069A1/es unknown
- 2015-01-30 EP EP18174593.6A patent/EP3392249B1/en active Active
- 2015-01-30 KR KR1020227021266A patent/KR102631769B1/ko active IP Right Grant
- 2015-01-30 WO PCT/US2015/013652 patent/WO2015116885A1/en active Application Filing
- 2015-01-30 EP EP21192647.2A patent/EP3988549A1/en active Pending
- 2015-01-30 KR KR1020247003206A patent/KR20240017118A/ko active Application Filing
- 2015-01-30 CA CA2937739A patent/CA2937739C/en active Active
- 2015-01-30 HU HUE15705860A patent/HUE040226T2/hu unknown
- 2015-01-30 SI SI201530317T patent/SI3099687T1/en unknown
- 2015-01-30 UY UY0001035975A patent/UY35975A/es active IP Right Grant
- 2015-01-30 TW TW111149560A patent/TW202340188A/zh unknown
- 2015-01-30 WO PCT/US2015/013654 patent/WO2015116886A1/en active Application Filing
- 2015-01-30 ES ES18174593T patent/ES2893251T3/es active Active
- 2015-01-30 BR BR112016015717-6A patent/BR112016015717B1/pt active IP Right Grant
- 2015-01-30 PE PE2020002136A patent/PE20210470A1/es unknown
- 2015-01-30 EA EA201691471A patent/EA030222B1/ru not_active IP Right Cessation
-
2016
- 2016-06-24 PH PH12016501249A patent/PH12016501249A1/en unknown
- 2016-07-14 MX MX2020012520A patent/MX2020012520A/es unknown
- 2016-07-26 IL IL246964A patent/IL246964B/en active IP Right Grant
- 2016-07-29 CL CL2016001933A patent/CL2016001933A1/es unknown
- 2016-08-30 ZA ZA2016/06011A patent/ZA201606011B/en unknown
-
2018
- 2018-08-23 HR HRP20181339TT patent/HRP20181339T1/hr unknown
- 2018-09-28 CY CY181101000T patent/CY1120702T1/el unknown
-
2019
- 2019-01-07 JP JP2019000516A patent/JP6630004B2/ja active Active
- 2019-03-27 JP JP2019060181A patent/JP6854067B2/ja active Active
- 2019-08-13 AU AU2019216617A patent/AU2019216617B2/en active Active
-
2020
- 2020-01-30 IL IL272377A patent/IL272377B2/en unknown
-
2021
- 2021-02-26 PH PH12021550418A patent/PH12021550418A1/en unknown
- 2021-03-12 JP JP2021039989A patent/JP7325464B2/ja active Active
- 2021-06-15 AU AU2021203968A patent/AU2021203968B2/en active Active
-
2023
- 2023-06-14 AU AU2023203695A patent/AU2023203695A1/en active Pending
- 2023-08-01 JP JP2023125512A patent/JP2023133468A/ja active Pending
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
UY35975A (es) | Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia | |
CO2017003833A2 (es) | Pirimidinonas como inhibidores del factor xia | |
UY34960A (es) | Dihidropiridona p1 como inhibidores del factor xia | |
UY35972A (es) | Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos | |
UY34959A (es) | Dihidropiridona p1 como inhibidores del factor xia | |
CO2017001152A2 (es) | Espirocicloheptanos como inhibidores de la cinasa rho (rock) | |
ECSP17070706A (es) | Inhibidores de bromodominio | |
CU24605B1 (es) | Pirimidin-2-il amino-1h-pirazoles útiles como inhibidores de lrrk2 | |
CL2017001650A1 (es) | Derivados de 5-[(piperazina-1-yl)-3-oxo-propilo]-imidazolidina-2,4-dionan como inhibidores adamts para el tratamiento oesteoartritis. | |
UY36170A (es) | Compuestos de dihidroisoquinolinona sustituida | |
UY34657A (es) | ?derivados macrocíclicos para el tratamiento de enfermedades?. | |
CR20150517A (es) | Inhibidores de la phd de 6-(5-hidroxi-1h-pirazol-1-il) nicotinamida | |
AR103895A1 (es) | Lactamas como inhibidores de rock | |
CU24263B1 (es) | Derivados de imidazopiridazinas inhibidores de quinasa akt, útiles para el tratamiento del cáncer | |
CO2017000011A2 (es) | Derivados de quinolizinona como inhibidores de pi3k | |
SV2016005310A (es) | Derivados de diheterociclo enlazado a cicloalquilo | |
EA201790687A1 (ru) | Хинолинкарбоксамиды для применения в лечении множественной миеломы | |
DOP2016000326A (es) | Compuestos de dihidroisoquinolinona sustituida |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
110 | Patent granted |
Effective date: 20230918 |