CO6551666A2 - Macrociclos como inhibidores del factor de coagulacion (fxia) - Google Patents
Macrociclos como inhibidores del factor de coagulacion (fxia)Info
- Publication number
- CO6551666A2 CO6551666A2 CO12151258A CO12151258A CO6551666A2 CO 6551666 A2 CO6551666 A2 CO 6551666A2 CO 12151258 A CO12151258 A CO 12151258A CO 12151258 A CO12151258 A CO 12151258A CO 6551666 A2 CO6551666 A2 CO 6551666A2
- Authority
- CO
- Colombia
- Prior art keywords
- inhibitors
- macrocicles
- fxia
- compounds
- coagulation factor
- Prior art date
Links
Classifications
-
- 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
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
- C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D225/08—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with two six-membered 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
- C07D471/14—Ortho-condensed systems
-
- 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
- C07D487/06—Peri-condensed 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed 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
- C07D487/12—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 three hetero rings
- C07D487/16—Peri-condensed 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
- C07D487/12—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 three hetero rings
- C07D487/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (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)
- Other In-Based Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se refiere a compuestos de fórmula (I):o un estereoisómero o un tautómero o una sal farmacéuticamente aceptable del mismo, en donde todas las variables son como se han definido en el presente documento. Estos compuestos son inhibidores selectivos del Factor Xla o inhibidores duales de fXla y calicreína de plasma. La presente invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y métodos para tratar trastornos tromboembólicos y/o inflamatorios usando las mismas.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30342310P | 2010-02-11 | 2010-02-11 | |
| US40533810P | 2010-10-21 | 2010-10-21 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO6551666A2 true CO6551666A2 (es) | 2012-10-31 |
Family
ID=43858008
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO12151258A CO6551666A2 (es) | 2010-02-11 | 2012-09-04 | Macrociclos como inhibidores del factor de coagulacion (fxia) |
Country Status (23)
| Country | Link |
|---|---|
| US (9) | US8940720B2 (es) |
| EP (3) | EP3786165A1 (es) |
| JP (3) | JP5844287B2 (es) |
| KR (2) | KR101843542B1 (es) |
| CN (3) | CN102753555B (es) |
| AR (1) | AR080167A1 (es) |
| AU (1) | AU2011215898B2 (es) |
| BR (1) | BR112012019925B1 (es) |
| CA (1) | CA2789622C (es) |
| CL (1) | CL2012002229A1 (es) |
| CO (1) | CO6551666A2 (es) |
| EA (1) | EA020528B1 (es) |
| ES (2) | ES2822130T3 (es) |
| IL (1) | IL221343B (es) |
| MX (1) | MX2012008874A (es) |
| MY (1) | MY162936A (es) |
| NZ (1) | NZ602266A (es) |
| PE (2) | PE20160841A1 (es) |
| PH (1) | PH12012501589A1 (es) |
| SG (1) | SG183153A1 (es) |
| TW (2) | TWI577665B (es) |
| WO (2) | WO2011100401A1 (es) |
| ZA (1) | ZA201206758B (es) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102753555B (zh) * | 2010-02-11 | 2018-01-12 | 百时美施贵宝公司 | 作为因子xia抑制剂的大环类 |
| 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 |
| EP2899183B1 (en) * | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP3309148A1 (en) | 2011-10-14 | 2018-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EA028581B1 (ru) * | 2012-08-03 | 2017-12-29 | Бристол-Маерс Сквибб Компани | ДИГИДРОПИРИДОН Р1 В КАЧЕСТВЕ ИНГИБИТОРОВ ФАКТОРА XIa |
| UY34959A (es) * | 2012-08-03 | 2014-01-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Dihidropiridona p1 como inhibidores del factor xia |
| EP2906541B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| DK2906551T3 (en) | 2012-10-12 | 2018-05-22 | Bristol Myers Squibb Co | CRYSTALLIC FORMS OF A FACTOR XIA INHIBITOR |
| WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine 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 |
| AU2014264973B2 (en) * | 2013-05-06 | 2018-01-18 | Merck Patent Gmbh | Macrocycles as kinase inhibitors |
| WO2015054087A1 (en) | 2013-10-07 | 2015-04-16 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| CN106029076B (zh) | 2013-11-18 | 2019-06-07 | 福马疗法公司 | 作为bet溴域抑制剂的苯并哌嗪组合物 |
| NZ720004A (en) | 2013-11-18 | 2020-03-27 | Forma Therapeutics Inc | Tetrahydroquinoline compositions as bet bromodomain inhibitors |
| UY40230A (es) * | 2014-01-31 | 2023-08-15 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Macrociclos con grupos P2’ heterocíclicos como inhibidores del factor XIa y composiciones farmacéuticas que los comprenden |
| NO2760821T3 (es) * | 2014-01-31 | 2018-03-10 | ||
| EP3102200B1 (en) | 2014-02-07 | 2023-04-05 | Exithera Pharmaceuticals Inc. | Therapeutic compounds and compositions |
| WO2015123091A1 (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 |
| US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
| WO2016015593A1 (en) | 2014-07-28 | 2016-02-04 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
| ES2714283T3 (es) | 2014-09-04 | 2019-05-28 | Bristol Myers Squibb Co | Macrociclos de diamida que son inhibidores de FXIa |
| 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 | ||
| WO2016118403A1 (en) * | 2015-01-20 | 2016-07-28 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
| TWI535452B (zh) * | 2015-01-23 | 2016-06-01 | 長庚醫療財團法人 | 使用抗-cd44中和抗體來治療和/或預防心房顫動 |
| EP3310777B1 (en) | 2015-06-19 | 2019-10-09 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| CN107849026B (zh) * | 2015-07-29 | 2021-01-01 | 百时美施贵宝公司 | 携带烷基或环烷基p2′部分的因子xia大环抑制剂 |
| US10676477B2 (en) | 2015-07-29 | 2020-06-09 | Bristol-Myers Squibb Company | Factor XIa macrocycle inhibitors bearing a non-aromatic P2' group |
| CN105085492A (zh) * | 2015-09-29 | 2015-11-25 | 青岛友诚高新技术有限公司 | 一种可用于制备治疗冠状动脉粥样硬化药物的化合物及其制备方法、用途 |
| 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 |
| US10214512B2 (en) | 2015-10-29 | 2019-02-26 | Merck Sharp & Dohme Corp. | Factor XIA inhibitors |
| EP3423458A1 (en) | 2016-03-02 | 2019-01-09 | Bristol-Myers Squibb Company | Diamide macrocycles having factor xia inhibiting activity |
| AU2017242027B2 (en) * | 2016-04-01 | 2020-10-08 | Recurium Ip Holdings, Llc | Estrogen receptor modulators |
| EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
| EP3601267A1 (en) | 2017-03-21 | 2020-02-05 | Bayer Pharma Aktiengesellschaft | 2-methyl-quinazolines |
| 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 |
| CN109721613B (zh) * | 2017-10-27 | 2021-07-30 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的大环酰胺化合物及其药物组合物和用途 |
| CN109721539B (zh) * | 2017-10-27 | 2021-07-09 | 天津药物研究院有限公司 | 吡唑酰胺类衍生物及其制备方法和用途 |
| CN109867660A (zh) * | 2017-12-01 | 2019-06-11 | 四川科伦博泰生物医药股份有限公司 | 含季铵离子的四氢异喹啉酰胺化合物及其药物用途 |
| BR112020016123A2 (pt) | 2018-02-07 | 2021-02-23 | eXIthera Pharmaceuticals Inc. | compostos e composições terapêuticas |
| GB201805174D0 (en) * | 2018-03-29 | 2018-05-16 | Univ Leeds Innovations Ltd | Compounds |
| CA3097231A1 (en) | 2018-04-18 | 2019-10-24 | Bayer Pharma Aktiengesellschaft | 2-methyl-aza-quinazolines |
| CN109232259B (zh) * | 2018-09-27 | 2021-05-28 | 浙江理工大学 | 一种硝基苯乙酮的制备方法 |
| CN111138366B (zh) * | 2018-11-06 | 2023-03-28 | 天津药物研究院有限公司 | 吡唑氨基甲酰类衍生物、及其制备方法和用途 |
| JP7270770B2 (ja) | 2019-04-16 | 2023-05-10 | チャイナ・リソースズ・バイオファーマシューティカル・カンパニー・リミテッド | XIa因子阻害剤としての大環状誘導体 |
| 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 |
| WO2021121396A1 (zh) * | 2019-12-20 | 2021-06-24 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的三环类化合物及其用途 |
| CN113004284B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的四环类化合物及其用途 |
| CN113004283B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的四环类化合物及其用途 |
| CN115066417B (zh) * | 2019-12-31 | 2025-05-02 | 上海京新生物医药有限公司 | 凝血因子XIa抑制剂 |
| TW202535863A (zh) * | 2020-02-13 | 2025-09-16 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
| CN113943259A (zh) * | 2020-07-17 | 2022-01-18 | 西安禾渼生物医药有限公司 | 一种氨基酸衍生物、其制备方法及应用 |
| US12129265B2 (en) | 2020-07-21 | 2024-10-29 | Ankh Life Sciences Limited | Therapeutic agents and uses thereof |
| CN118373832B (zh) * | 2023-01-20 | 2025-01-28 | 深圳晶蛋生物医药科技有限公司 | 大环类化合物、其药物组合物及其应用 |
| CN116813490B (zh) * | 2023-06-30 | 2025-08-08 | 常州大学 | 可见光驱动非天然氨基酸及其衍生物的合成方法 |
| WO2025117439A1 (en) * | 2023-11-30 | 2025-06-05 | Viva Star Biosciences (Us) Inc. | Macrocycle compounds as inhibitors of nlrp3 activity and therapeutic uses thereof |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3065190D1 (en) | 1979-11-05 | 1983-11-10 | Beecham Group Plc | Enzyme derivatives, and their preparation |
| JPS62103070A (ja) | 1985-10-29 | 1987-05-13 | Mitsui Toatsu Chem Inc | イソオキサゾリン誘導体および植物生長調節剤 |
| 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 |
| 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 |
| 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 |
| US6951840B2 (en) * | 2001-08-31 | 2005-10-04 | Eli Lilly And Company | Lipoglycopeptide antibiotics |
| ES2329881T3 (es) | 2001-09-21 | 2009-12-02 | Bristol-Myers Squibb Company | Compuestos que contienen lactama y derivados de los mismos como inhibidores del factor xa. |
| WO2003106438A1 (en) * | 2002-06-18 | 2003-12-24 | The Scripps Research Institute | Synthesis of diazonamide "a" core |
| CN1160358C (zh) * | 2002-10-09 | 2004-08-04 | 武汉大学 | (8s,18s)-1,4,10,13,16-五氮杂三环[16.3.0.04,8]二十一烷-9,17-二酮及其制备方法和用途 |
| 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 |
| EP1654245A1 (en) | 2003-08-07 | 2006-05-10 | Bayer Pharmaceuticals Corporation | Benzofuran derivatives useful for treating hyper-proliferative disorders |
| US7417063B2 (en) | 2004-04-13 | 2008-08-26 | Bristol-Myers Squibb Company | Bicyclic 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 |
| US7453002B2 (en) | 2004-06-15 | 2008-11-18 | Bristol-Myers Squibb Company | Five-membered heterocycles useful as serine protease inhibitors |
| CN101006063B (zh) * | 2004-06-15 | 2013-07-17 | 布里斯托尔-迈尔斯斯奎布公司 | 用作丝氨酸蛋白酶抑制剂的五元杂环类化合物 |
| JP5236293B2 (ja) | 2005-01-13 | 2013-07-17 | ブリストル−マイヤーズ スクイブ カンパニー | Xia因子阻害剤としての置換ビアリール化合物 |
| 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 |
| US20070111947A1 (en) * | 2005-10-14 | 2007-05-17 | Mcmurry Thomas J | Fibrin targeted therapeutics |
| AR058379A1 (es) * | 2005-12-14 | 2008-01-30 | Bristol Myers Squibb Co | Derivados de arilpropionamida arilacrilamida arilpropinamida o arilmetilurea como inhibidores del factor xia. proceso de obtencion y composiciones farmaceuticas. |
| WO2007070816A2 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Thiophene derivatives as factor xia inhibitors |
| CN101341129B (zh) * | 2005-12-14 | 2011-12-14 | 布里斯托尔-迈尔斯斯奎布公司 | 作为因子xia抑制剂的芳基丙酰胺,芳基丙烯酰胺,芳基丙炔酰胺,或芳基甲基脲类似物 |
| 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 |
| 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 |
| CN101495480B (zh) * | 2006-05-03 | 2013-07-10 | 百时美施贵宝公司 | 作为降钙素基因相关肽受体拮抗剂的受限化合物 |
| US7605126B2 (en) * | 2006-08-11 | 2009-10-20 | Enanta Pharmaceuticals, Inc. | Acylaminoheteroaryl hepatitis C virus protease inhibitors |
| WO2008031508A1 (de) * | 2006-09-13 | 2008-03-20 | Sanofi-Aventis | Tartratderivate als inhibitoren des koagulationsfaktors ixa |
| CN101605779B (zh) * | 2006-12-15 | 2013-11-20 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的芳基丙酰胺、芳基丙烯酰胺、芳基丙炔酰胺或芳基甲基脲类似物 |
| CN101611019A (zh) * | 2006-12-20 | 2009-12-23 | 百时美施贵宝公司 | 可用作抗凝血药的大环凝血因子Ⅶa抑制剂 |
| PE20081775A1 (es) * | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| MX2009012847A (es) | 2007-06-13 | 2009-12-08 | Bristol Myers Squibb Co | Analogos dipeptidicos como inhibidores de factores de coagulacion. |
| EP2197873B1 (en) * | 2007-09-20 | 2014-07-16 | Irm Llc | Compounds and compositions as modulators of gpr119 activity |
| EP2065382A1 (de) | 2007-10-18 | 2009-06-03 | Boehringer Ingelheim Pharma GmbH & Co. KG | CGRP Antagonisten |
| GB0800035D0 (en) | 2008-01-02 | 2008-02-13 | Glaxo Group Ltd | Compounds |
| CN102026996B (zh) | 2008-03-13 | 2015-01-07 | 百时美施贵宝公司 | 作为凝血因子xia抑制剂的哒嗪衍生物 |
| CN102753555B (zh) | 2010-02-11 | 2018-01-12 | 百时美施贵宝公司 | 作为因子xia抑制剂的大环类 |
| 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 |
| EP3309148A1 (en) | 2011-10-14 | 2018-04-18 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2899183B1 (en) | 2011-10-14 | 2018-09-19 | Bristol-Myers Squibb Company | Substituted Tetrahydroisoquinoline Compounds as Factor Xia Inhibitors |
| EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2794597B1 (en) | 2011-12-21 | 2017-11-15 | ONO Pharmaceutical Co., Ltd. | Pyridinone and pyrimidinone derivatives as factor xia 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 |
| GB201209138D0 (en) | 2012-05-24 | 2012-07-04 | Ono Pharmaceutical Co | Compounds |
-
2011
- 2011-02-10 CN CN201180009345.8A patent/CN102753555B/zh active Active
- 2011-02-10 BR BR112012019925-0A patent/BR112012019925B1/pt not_active IP Right Cessation
- 2011-02-10 WO PCT/US2011/024305 patent/WO2011100401A1/en not_active Ceased
- 2011-02-10 PE PE2016000777A patent/PE20160841A1/es active IP Right Grant
- 2011-02-10 KR KR1020127023575A patent/KR101843542B1/ko active Active
- 2011-02-10 PH PH1/2012/501589A patent/PH12012501589A1/en unknown
- 2011-02-10 JP JP2012552984A patent/JP5844287B2/ja active Active
- 2011-02-10 MX MX2012008874A patent/MX2012008874A/es active IP Right Grant
- 2011-02-10 ES ES11704894T patent/ES2822130T3/es active Active
- 2011-02-10 NZ NZ602266A patent/NZ602266A/en not_active IP Right Cessation
- 2011-02-10 EP EP20185503.8A patent/EP3786165A1/en not_active Withdrawn
- 2011-02-10 AU AU2011215898A patent/AU2011215898B2/en not_active Ceased
- 2011-02-10 CN CN201711363263.9A patent/CN107973809B/zh active Active
- 2011-02-10 TW TW104136778A patent/TWI577665B/zh not_active IP Right Cessation
- 2011-02-10 EA EA201270716A patent/EA020528B1/ru not_active IP Right Cessation
- 2011-02-10 PE PE2012001189A patent/PE20121806A1/es active IP Right Grant
- 2011-02-10 JP JP2012552985A patent/JP5841547B2/ja active Active
- 2011-02-10 EP EP11704895.9A patent/EP2534152B1/en active Active
- 2011-02-10 MY MYPI2012003575A patent/MY162936A/en unknown
- 2011-02-10 US US13/024,544 patent/US8940720B2/en active Active
- 2011-02-10 KR KR1020177034126A patent/KR101901545B1/ko active Active
- 2011-02-10 US US13/577,666 patent/US8828983B2/en active Active
- 2011-02-10 WO PCT/US2011/024308 patent/WO2011100402A1/en not_active Ceased
- 2011-02-10 EP EP11704894.2A patent/EP2534154B1/en active Active
- 2011-02-10 TW TW100104487A patent/TWI520965B/zh not_active IP Right Cessation
- 2011-02-10 ES ES11704895.9T patent/ES2674745T3/es active Active
- 2011-02-10 CA CA2789622A patent/CA2789622C/en active Active
- 2011-02-10 CN CN201180018385.9A patent/CN102834397B/zh active Active
- 2011-02-10 SG SG2012057543A patent/SG183153A1/en unknown
- 2011-02-11 AR ARP110100435 patent/AR080167A1/es not_active Application Discontinuation
-
2012
- 2012-08-07 IL IL221343A patent/IL221343B/en active IP Right Grant
- 2012-08-10 CL CL2012002229A patent/CL2012002229A1/es unknown
- 2012-09-04 CO CO12151258A patent/CO6551666A2/es active IP Right Grant
- 2012-09-10 ZA ZA2012/06758A patent/ZA201206758B/en unknown
-
2014
- 2014-07-31 US US14/448,058 patent/US9079918B2/en active Active
- 2014-12-22 US US14/578,846 patent/US9802939B2/en active Active
-
2015
- 2015-06-09 US US14/733,996 patent/US9453029B2/en active Active
- 2015-11-18 JP JP2015225921A patent/JP6294286B2/ja active Active
-
2016
- 2016-08-25 US US15/246,813 patent/US9745313B2/en active Active
-
2017
- 2017-09-28 US US15/718,431 patent/US10487086B2/en active Active
-
2019
- 2019-11-21 US US16/691,099 patent/US11136327B2/en active Active
-
2021
- 2021-10-04 US US17/493,516 patent/US12404274B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CO6551666A2 (es) | Macrociclos como inhibidores del factor de coagulacion (fxia) | |
| MX345763B (es) | Nuevos macrociclos como inhibidores del factor xia. | |
| EA201590284A1 (ru) | Дигидропиридон р1 в качестве ингибиторов фактора xia | |
| EA201590277A1 (ru) | Дигидропиридон р1 в качестве ингибиторов фактора xia | |
| PH12020500195A1 (en) | Pyrimidinones as factor xia inhibitors | |
| CO2017012267A2 (es) | Compuestos de naftiridina como inhibidores de la quinasa jak | |
| UY35971A (es) | Macrociclos con grupos p2? aromáticos como inhibidores del factor xia | |
| EA201490724A1 (ru) | Замещенные соединения тетрагидроизохинолина в качестве ингибиторов фактора xia | |
| EA201691803A1 (ru) | Ингибиторы калликреина плазмы человека | |
| EA201691561A1 (ru) | Макроциклические ингибиторы фактора xia, конденсированные с гетероциклами | |
| EA201790202A1 (ru) | Фталазиноны и изохинолиноны в качестве ингибиторов rock | |
| CO6660497A2 (es) | Derivados del ácido nft-2-ilacético para tratar el sida | |
| CU20140072A7 (es) | Derivados de dihidro-oxazina y dihidro-pirido-oxazina | |
| HK1205506A1 (en) | Protein kinase inhibitors | |
| CO6741219A2 (es) | Inhibidores de catepsina c |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Application granted |