MX2009003758A - Antagonistas del receptor de trombina basados en la unidad triciclica modificada de himbacina. - Google Patents
Antagonistas del receptor de trombina basados en la unidad triciclica modificada de himbacina.Info
- Publication number
- MX2009003758A MX2009003758A MX2009003758A MX2009003758A MX2009003758A MX 2009003758 A MX2009003758 A MX 2009003758A MX 2009003758 A MX2009003758 A MX 2009003758A MX 2009003758 A MX2009003758 A MX 2009003758A MX 2009003758 A MX2009003758 A MX 2009003758A
- Authority
- MX
- Mexico
- Prior art keywords
- himbacine
- receptor antagonists
- thrombin receptor
- antagonists based
- tricyclic unit
- Prior art date
Links
- FMPNFDSPHNUFOS-HQEQRHKESA-N Himbacine Natural products C(/[C@@H]1[C@H]2CCCC[C@@H]2C[C@@H]2C(=O)O[C@H]([C@H]12)C)=C\[C@@H]1CCC[C@H](C)N1C FMPNFDSPHNUFOS-HQEQRHKESA-N 0.000 title 1
- FMPNFDSPHNUFOS-UHFFFAOYSA-N N-Methyl-himandravin Natural products C12C(C)OC(=O)C2CC2CCCCC2C1C=CC1CCCC(C)N1C FMPNFDSPHNUFOS-UHFFFAOYSA-N 0.000 title 1
- FMPNFDSPHNUFOS-LPJDIUFZSA-N himbacine Chemical compound C(/[C@@H]1[C@H]2CCCC[C@@H]2C[C@@H]2C(=O)O[C@H]([C@H]12)C)=C\[C@H]1CCC[C@H](C)N1C FMPNFDSPHNUFOS-LPJDIUFZSA-N 0.000 title 1
- 239000003856 thrombin receptor antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 206010003119 arrhythmia Diseases 0.000 abstract 1
- 230000006793 arrhythmia Effects 0.000 abstract 1
- 229940125692 cardiovascular agent Drugs 0.000 abstract 1
- 239000002327 cardiovascular agent Substances 0.000 abstract 1
- 238000002648 combination therapy Methods 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 201000010235 heart cancer Diseases 0.000 abstract 1
- 208000024348 heart neoplasm Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
Abstract
Se proveen estereoisómeros múltiples de los tricíclicos heterocíclicos sustituidos de la fórmula: (ver fórmula) o una sal, solvato o éster aceptable para uso farmacéutico de dicho compuesto cuyos R y estereoquímica se ilustran en las fórmulas estructurales que se revelan en la presente, así como las composiciones farmacéuticas que los contienen y un método para tratar enfermedades relacionadas con trombosis, ateroesclerosis, restenosis, hipertensión, angina de pecho, arritmia, insuficiencia cardiaca, y cáncer mediante la administración de dichos compuestos; también se reivindica la terapia de combinación con otros agentes cardiovasculares.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US84928406P | 2006-10-04 | 2006-10-04 | |
| PCT/US2007/021259 WO2008060372A2 (en) | 2006-10-04 | 2007-10-02 | Thrombin receptor antagonists based on the modified tricyclic unit of himbacine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2009003758A true MX2009003758A (es) | 2009-04-22 |
Family
ID=39284222
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2009003758A MX2009003758A (es) | 2006-10-04 | 2007-10-02 | Antagonistas del receptor de trombina basados en la unidad triciclica modificada de himbacina. |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20080085923A1 (es) |
| EP (1) | EP2078012A2 (es) |
| JP (1) | JP2010505836A (es) |
| KR (1) | KR20090058583A (es) |
| CN (1) | CN101553484A (es) |
| AR (1) | AR063095A1 (es) |
| AU (1) | AU2007320029A1 (es) |
| CA (1) | CA2666903A1 (es) |
| IL (1) | IL198011A0 (es) |
| MX (1) | MX2009003758A (es) |
| TW (1) | TW200823206A (es) |
| WO (1) | WO2008060372A2 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8227412B2 (en) * | 2007-03-29 | 2012-07-24 | Tsopanoglou Nikos E | Bioactive parstatin peptides and methods of use |
| DK2438060T3 (da) * | 2009-06-04 | 2014-01-13 | Merck Sharp & Dohme | Aktiv metabolit af en trombin-receptor-antagonist |
| EP2488026A4 (en) * | 2009-10-02 | 2013-04-10 | Merck Sharp & Dohme | USE OF A PAR-1 ANTAGONIST IN COMBINATION WITH A P2Y12ADP RECEPTOR ANTAGONIST FOR INHIBITING THROMBOSE |
| CN105777681B (zh) * | 2014-12-17 | 2019-03-01 | 博瑞生物医药（苏州）股份有限公司 | 喜巴辛类似物及其中间体的制备方法 |
| JPWO2016114386A1 (ja) * | 2015-01-15 | 2017-10-19 | 国立研究開発法人国立精神・神経医療研究センター | 進行型免疫性脱髄疾患治療剤 |
| CN105985303B (zh) * | 2015-02-13 | 2020-08-14 | 上海彩迩文生化科技有限公司 | 抗凝血剂的制备方法、中间体及其制备方法 |
| CN106866450B (zh) * | 2017-01-13 | 2019-01-11 | 阜阳欣奕华材料科技有限公司 | 硫酸沃拉帕沙中间体的制备方法 |
| CN110483455A (zh) * | 2019-09-29 | 2019-11-22 | 天津力生制药股份有限公司 | 一种硫酸沃拉帕沙中间体醛基物的合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6063847A (en) * | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
| MXPA02012447A (es) * | 2000-06-15 | 2003-04-25 | Schering Corp | Antagonistas receptores de trombina. |
| AR036832A1 (es) * | 2001-10-18 | 2004-10-06 | Schering Corp | Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos |
| PT1495018E (pt) * | 2002-04-16 | 2008-02-19 | Schering Corp | Antagonistas tricíclicos de receptores de trombina |
-
2007
- 2007-10-02 JP JP2009531440A patent/JP2010505836A/ja not_active Withdrawn
- 2007-10-02 US US11/866,012 patent/US20080085923A1/en not_active Abandoned
- 2007-10-02 AU AU2007320029A patent/AU2007320029A1/en not_active Abandoned
- 2007-10-02 MX MX2009003758A patent/MX2009003758A/es not_active Application Discontinuation
- 2007-10-02 EP EP07867200A patent/EP2078012A2/en not_active Withdrawn
- 2007-10-02 WO PCT/US2007/021259 patent/WO2008060372A2/en not_active Ceased
- 2007-10-02 AR ARP070104357A patent/AR063095A1/es not_active Application Discontinuation
- 2007-10-02 CN CNA2007800433580A patent/CN101553484A/zh active Pending
- 2007-10-02 KR KR1020097008460A patent/KR20090058583A/ko not_active Withdrawn
- 2007-10-02 CA CA002666903A patent/CA2666903A1/en not_active Abandoned
- 2007-10-03 TW TW096137099A patent/TW200823206A/zh unknown
-
2009
- 2009-04-05 IL IL198011A patent/IL198011A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20090058583A (ko) | 2009-06-09 |
| AR063095A1 (es) | 2008-12-30 |
| AU2007320029A1 (en) | 2008-05-22 |
| WO2008060372A3 (en) | 2008-12-24 |
| IL198011A0 (en) | 2009-12-24 |
| JP2010505836A (ja) | 2010-02-25 |
| CN101553484A (zh) | 2009-10-07 |
| US20080085923A1 (en) | 2008-04-10 |
| WO2008060372A2 (en) | 2008-05-22 |
| CA2666903A1 (en) | 2008-05-22 |
| TW200823206A (en) | 2008-06-01 |
| EP2078012A2 (en) | 2009-07-15 |
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