MX2014012741A - Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria. - Google Patents
Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria.Info
- Publication number
- MX2014012741A MX2014012741A MX2014012741A MX2014012741A MX2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A MX 2014012741 A MX2014012741 A MX 2014012741A
- Authority
- MX
- Mexico
- Prior art keywords
- inhibitors
- imidazothiadiazole
- platelet aggregation
- par4
- activated receptor
- Prior art date
Links
Classifications
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- 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
- C07D513/04—Ortho-condensed 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
- A61K31/433—Thidiazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- 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
- 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
- C07D487/04—Ortho-condensed 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
- A61K31/495—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
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
Abstract
La presente invención se refiere a compuestos de imidazotiadiazol de la Fórmula (I): (ver Fórmula) en donde W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 y X4 son como se definen en la presente, o un estereoisómero, tautómero, una sal farmacéuticamente aceptable, éster de profármaco o forma de solvato del mismo, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores de la agregación plaquetaria y, por lo tanto, se pueden usar como medicamentos para tratar o prevenir trastornos tromboembólicos.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261638567P | 2012-04-26 | 2012-04-26 | |
PCT/US2013/037884 WO2013163241A1 (en) | 2012-04-26 | 2013-04-24 | Imidazothiadiazole and imidazopyridazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2014012741A true MX2014012741A (es) | 2015-04-13 |
Family
ID=48225151
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2014012741A MX2014012741A (es) | 2012-04-26 | 2013-04-24 | Derivados de imidazotiadiazol e imidazopirazina como inhibidores del receptor 4 activado de proteasa (par4) para tratamiento de agregacion plaquetaria. |
Country Status (14)
Country | Link |
---|---|
US (1) | US9518064B2 (es) |
EP (1) | EP2855489B1 (es) |
JP (1) | JP6101343B2 (es) |
KR (1) | KR20150003766A (es) |
CN (1) | CN104640869B (es) |
AU (1) | AU2013251680A1 (es) |
BR (1) | BR112014026651A8 (es) |
CA (1) | CA2871599A1 (es) |
EA (1) | EA201491954A1 (es) |
ES (1) | ES2617879T3 (es) |
IL (1) | IL235141A0 (es) |
MX (1) | MX2014012741A (es) |
SG (1) | SG11201406733QA (es) |
WO (1) | WO2013163241A1 (es) |
Families Citing this family (24)
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NZ631027A (en) | 2012-04-26 | 2016-03-31 | Bristol Myers Squibb Co | Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (par4) inhibitors for treating platelet aggregation |
US9862730B2 (en) | 2012-04-26 | 2018-01-09 | Bristol-Myers Squibb Company | Imidazothiadiazole derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation |
WO2015124570A1 (en) | 2014-02-18 | 2015-08-27 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical composition for the treatment of influenza a virus infection |
CN106459028A (zh) | 2014-03-24 | 2017-02-22 | 拜耳作物科学股份公司 | 作为杀真菌剂的苯基哌啶羧酰胺衍生物 |
US9598419B1 (en) | 2014-06-24 | 2017-03-21 | Universite De Montreal | Imidazotriazine and imidazodiazine compounds |
US9617279B1 (en) | 2014-06-24 | 2017-04-11 | Bristol-Myers Squibb Company | Imidazooxadiazole compounds |
ES2929208T3 (es) | 2015-02-26 | 2022-11-25 | Univ Montreal | Compuestos de imidazotiadiazol como inhibidores de PAR4 |
EP3262052A1 (en) | 2015-02-26 | 2018-01-03 | Bristol-Myers Squibb Company | Benzothiazole and benzothiophne compounds |
US9789087B2 (en) | 2015-08-03 | 2017-10-17 | Thomas Jefferson University | PAR4 inhibitor therapy for patients with PAR4 polymorphism |
WO2017066863A1 (en) | 2015-10-19 | 2017-04-27 | Universite De Montreal | Heterocyclic compounds as inhibitors of platelet aggregation |
US20190119300A1 (en) * | 2016-04-18 | 2019-04-25 | Vanderbilt University | Substituted and fused 6-membered protease activated receptor 4 (par-4) antagonists |
KR102460385B1 (ko) | 2016-07-14 | 2022-10-27 | 브리스톨-마이어스 스큅 컴퍼니 | 비시클릭 헤테로아릴 치환된 화합물 |
KR102468661B1 (ko) * | 2016-07-14 | 2022-11-17 | 브리스톨-마이어스 스큅 컴퍼니 | Par4 억제제로서의 트리시클릭 헤테로아릴-치환된 퀴놀린 및 아자퀴놀린 화합물 |
CN109689642B (zh) | 2016-07-14 | 2022-04-12 | 百时美施贵宝公司 | 经单环杂芳基取代的化合物 |
CN109689649B (zh) | 2016-07-14 | 2022-07-19 | 百时美施贵宝公司 | 经二环杂芳基取代的化合物 |
JP7294661B2 (ja) * | 2016-12-23 | 2023-06-20 | ミノリックス セラピューティクス エセ.エレ. | 5-[[4-[2-[5-(1-ヒドロキシエチル)-2-ピリジニル]エトキシ]フェニル]メチル]-2,4-チアゾリジンジオンおよびその塩を調製するためのプロセス |
WO2019149205A1 (zh) * | 2018-01-31 | 2019-08-08 | 江苏恒瑞医药股份有限公司 | 苯并杂芳基类衍生物、其制备方法及其在医药上的应用 |
CN110218218B (zh) * | 2018-03-01 | 2022-04-08 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
CN112074523B (zh) * | 2018-05-16 | 2022-08-09 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
CN112074522B (zh) * | 2018-05-16 | 2022-08-26 | 深圳信立泰药业股份有限公司 | 作为用于治疗血小板聚集的蛋白酶激活受体4(par4)抑制剂的化合物 |
CN110627817B (zh) * | 2018-06-25 | 2022-03-29 | 中国药科大学 | 咪唑并环类par4拮抗剂及其医药用途 |
CN111349105B (zh) * | 2018-12-24 | 2023-04-07 | 江苏恒瑞医药股份有限公司 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
CN109651126A (zh) * | 2019-01-17 | 2019-04-19 | 杭州师范大学 | 一种四苯乙烯基羧酸有机配体及其配合物的制备方法 |
CN113150005B (zh) * | 2021-04-09 | 2022-08-30 | 中国药科大学 | 喹喔啉类化合物、制备方法及其在医药上的应用 |
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2013
- 2013-04-24 EP EP13719360.3A patent/EP2855489B1/en active Active
- 2013-04-24 BR BR112014026651A patent/BR112014026651A8/pt not_active IP Right Cessation
- 2013-04-24 MX MX2014012741A patent/MX2014012741A/es unknown
- 2013-04-24 US US14/396,831 patent/US9518064B2/en active Active
- 2013-04-24 SG SG11201406733QA patent/SG11201406733QA/en unknown
- 2013-04-24 WO PCT/US2013/037884 patent/WO2013163241A1/en active Application Filing
- 2013-04-24 EA EA201491954A patent/EA201491954A1/ru unknown
- 2013-04-24 AU AU2013251680A patent/AU2013251680A1/en not_active Abandoned
- 2013-04-24 ES ES13719360.3T patent/ES2617879T3/es active Active
- 2013-04-24 CA CA 2871599 patent/CA2871599A1/en not_active Abandoned
- 2013-04-24 JP JP2015509093A patent/JP6101343B2/ja active Active
- 2013-04-24 CN CN201380033473.5A patent/CN104640869B/zh active Active
- 2013-04-24 KR KR20147030172A patent/KR20150003766A/ko not_active Application Discontinuation
-
2014
- 2014-10-19 IL IL235141A patent/IL235141A0/en unknown
Also Published As
Publication number | Publication date |
---|---|
EA201491954A1 (ru) | 2015-01-30 |
IL235141A0 (en) | 2014-12-31 |
JP6101343B2 (ja) | 2017-03-22 |
US20150119390A1 (en) | 2015-04-30 |
AU2013251680A1 (en) | 2014-11-13 |
CA2871599A1 (en) | 2013-10-31 |
EP2855489B1 (en) | 2017-01-04 |
JP2015514806A (ja) | 2015-05-21 |
US9518064B2 (en) | 2016-12-13 |
BR112014026651A2 (pt) | 2017-06-27 |
CN104640869A (zh) | 2015-05-20 |
BR112014026651A8 (pt) | 2018-01-16 |
ES2617879T3 (es) | 2017-06-20 |
CN104640869B (zh) | 2017-12-12 |
SG11201406733QA (en) | 2014-11-27 |
WO2013163241A1 (en) | 2013-10-31 |
EP2855489A1 (en) | 2015-04-08 |
KR20150003766A (ko) | 2015-01-09 |
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