AR017189A1 - Antagonistas del receptor de trombina triciclico sustituido, composicion farmaceutica que lo contiene y su uso para la manufactura de un medicamento - Google Patents
Antagonistas del receptor de trombina triciclico sustituido, composicion farmaceutica que lo contiene y su uso para la manufactura de un medicamentoInfo
- Publication number
- AR017189A1 AR017189A1 ARP980105935A ARP980105935A AR017189A1 AR 017189 A1 AR017189 A1 AR 017189A1 AR P980105935 A ARP980105935 A AR P980105935A AR P980105935 A ARP980105935 A AR P980105935A AR 017189 A1 AR017189 A1 AR 017189A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- heteroarylalkyl
- aryl
- alkyl
- difluoroalkyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic 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
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- 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
-
- 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
- C07D405/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D405/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyridine Compounds (AREA)
Abstract
Antagonista del receptor de trombina tricíclico de la formula I o una sal farmacéuticamente aceptable de los mismos, en donde: la línea punteada simplerepresenta un enlace doble opcional; la línea punteada doble representa un enlace simple opcional;n es 0-2; Q es formula II en donde n1 y n2 sonindependientemente 0-2; o cuando el enlace doble no está presente, Q presenta es heteroarilo R-sustituido o arilo R-sustituido fusionado; R es 1 a 3sustituyentes independientemente seleccionados entre elgrupo que consiste de H, alquiloC1-6, halogeno, hidroxi, amino, alquilo(C1-6)amino, dialquil(C1-6)aminoalcoxi(C1-6), -COR16, -COOR17, -SOR16, -SO2R16, -NR16COR16a, -NR16COOR 16a, -NR16CONR4R5, fluoroalquilo(C1-6), difluoroalquilo(C1-6).trifluoroalqu ilo (C1-6),cicloalquiloC3-6, alqueniloC2-6, arilalquilo(C1-6), arilalquenilo(C2-6) heteroarilalquilo(C1-6), heteroarilalquenilo(C2-6), hidroxialquilo(C1-6), aminoalquilo(C1-6), arilo y tioalquilo(C1-6); R1 y R2 son independientementeseleccionados en tre el grupo que consiste de H, alquiloC1-6, fluoroalquilo(C1-6),difluoroalquilo(C1-6), trifluoroalquilo(C1-6), cicloalquiloC3-6, alqueniloC2-6, arilalquilo(C1-6), arilalquenilo(C2-6), heteroarilalquilo(C1-6)heteroarilalquenilo(C2-6), hidroxialquilo( C1-6), aminoalquilo(C1-6), arilo y tioalquilo(C1-6); o R1 y R2 juntos forman un grupo =O R3 es H, hidroxi, alcoxiC1-6, -SOR16, -SO2R17, -C(O)OR17, -C(O)OR17, -C(O)NR18R19, alquiloC1-6, halogeno, fluoroalquilo(C1-6),difluoroalquilo(C1-6), trifluoroal quilo(C1-6),cicloalquiloC3-6, alqueniloC2-6, arilalquilo(C1-6). arilalquenil(C2-6), heteroarilalquilo(C1-6), heteroarilalquenil(C2-6), hidroxialquilo(C1-6), aminoalquilo(C1-6), arilo o tioalquilo(C1-6); Het es ungrupo heteroaromático mono, bi o tric íclico de 5 a 14 átomos comprendido de 1 a 13 átomos de carbono y 1 a 4heteroátomos independientemente seleccionados del grupo que consiste de N, O y S, en donde un nitrogeno de anillo puede formar un N-oxido oun grupocuaternario con un grupo alquil oC1-4 en donde Het está ligado a B por un miembro anillo de átomo de carbono, y en donde el grupo Het está sustituido con 1 a 4
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97797997A | 1997-11-25 | 1997-11-25 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR017189A1 true AR017189A1 (es) | 2001-08-22 |
Family
ID=25525702
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP980105935A AR017189A1 (es) | 1997-11-25 | 1998-11-23 | Antagonistas del receptor de trombina triciclico sustituido, composicion farmaceutica que lo contiene y su uso para la manufactura de un medicamento |
Country Status (31)
| Country | Link |
|---|---|
| EP (1) | EP1036072B1 (es) |
| JP (2) | JP3449620B2 (es) |
| KR (1) | KR100393492B1 (es) |
| CN (2) | CN101274929A (es) |
| AR (1) | AR017189A1 (es) |
| AT (1) | ATE266025T1 (es) |
| AU (1) | AU747204B2 (es) |
| BR (1) | BR9812793A (es) |
| CA (1) | CA2309352C (es) |
| CO (1) | CO4990946A1 (es) |
| CZ (1) | CZ298578B6 (es) |
| DE (1) | DE69823694T2 (es) |
| DK (1) | DK1036072T3 (es) |
| ES (1) | ES2219919T3 (es) |
| HK (1) | HK1031726A1 (es) |
| HU (1) | HUP0100607A3 (es) |
| ID (1) | ID24726A (es) |
| IL (1) | IL135797A (es) |
| MY (1) | MY140887A (es) |
| NO (1) | NO322022B1 (es) |
| NZ (1) | NZ504218A (es) |
| PE (1) | PE133799A1 (es) |
| PL (1) | PL195027B1 (es) |
| PT (1) | PT1036072E (es) |
| RU (1) | RU2204557C2 (es) |
| SA (1) | SA99190972B1 (es) |
| SK (1) | SK285153B6 (es) |
| TR (1) | TR200001480T2 (es) |
| TW (1) | TWI236476B (es) |
| WO (1) | WO1999026943A1 (es) |
| ZA (1) | ZA9810685B (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2000229961A (ja) * | 1998-12-11 | 2000-08-22 | Sagami Chem Res Center | ヒドロナフト［２，３−ｃ］フラン誘導体およびその製造方法 |
| AU6731100A (en) | 1999-09-02 | 2001-04-10 | Shionogi & Co., Ltd. | Integrase inhibitors containing aromatic heterocycle derivatives |
| SI1294714T1 (sl) * | 2000-06-15 | 2007-12-31 | Schering Corp | Antagonisti trobinskega receptorja |
| PL359822A1 (en) * | 2000-06-15 | 2004-09-06 | Schering Corporation | Thrombin receptor antagonists |
| US7235567B2 (en) | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
| CA2446924C (en) | 2001-04-19 | 2011-02-08 | Eisai Co., Ltd. | 2-iminopyrrolidine derivatives |
| SG164279A1 (en) | 2002-04-16 | 2010-09-29 | Schering Corp | Tricyclic thrombin receptor antagonists |
| AU2004218187C1 (en) | 2003-02-19 | 2011-04-07 | Eisai R&D Management Co., Ltd. | Methods for producing cyclic benzamidine derivatives |
| JPWO2005108370A1 (ja) | 2004-04-16 | 2008-03-21 | 味の素株式会社 | ベンゼン化合物 |
| DE602005009355D1 (de) * | 2004-05-28 | 2008-10-09 | Schering Corp | Gehinderte himbacinanaloga als thrombinrezeptorantagonisten |
| EP2075250B1 (en) * | 2004-10-08 | 2015-03-04 | Merck Sharp & Dohme Corp. | Thrombin receptor antagonists |
| SI1848705T1 (sl) * | 2005-01-14 | 2010-06-30 | Schering Corp | Eksoselektivne in diastereoselektivne sinteze himbacinskih analogov |
| WO2006076564A1 (en) * | 2005-01-14 | 2006-07-20 | Schering Corporation | Synthesis of himbacine analogs |
| EP2399912B1 (en) * | 2005-01-14 | 2015-02-25 | Merck Sharp & Dohme Corp. | An exo-selective synthesis of himbacine analogs |
| TWI367112B (en) * | 2006-06-30 | 2012-07-01 | Schering Corp | Immediate-release tablet formulations of a thrombin receptor antagonist |
| CA2667082A1 (en) | 2006-10-04 | 2008-04-10 | Schering Corporation | Bicyclic and tricyclic derivatives as thrombin receptor antagonists |
| ES2527535T3 (es) | 2010-04-16 | 2015-01-26 | Sanofi | Piridil-vinil-pirazolo-quinolinas como inhibidores de PAR1 |
| EP2558465B1 (de) | 2010-04-16 | 2014-12-17 | Sanofi | Trizyklische pyridyl-vinyl-pyrrole als par1-inhibitoren |
| CN108658910B (zh) * | 2017-03-29 | 2020-11-03 | 北京新领先医药科技发展有限公司 | 一种沃拉帕沙中间体1-α的制备方法 |
| CN113387947B (zh) * | 2021-07-12 | 2022-07-01 | 中国科学院成都生物研究所 | 调节雌激素受体合成活性的吡唑并吡啶衍生物 |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL106197A (en) * | 1992-07-30 | 1999-11-30 | Cor Therapeutics Inc | Agagonists for the rhombin receptors and pharmaceutical preparations containing them |
-
1998
- 1998-11-23 KR KR10-2000-7005679A patent/KR100393492B1/ko not_active IP Right Cessation
- 1998-11-23 JP JP2000522101A patent/JP3449620B2/ja not_active Expired - Fee Related
- 1998-11-23 NZ NZ504218A patent/NZ504218A/en unknown
- 1998-11-23 PE PE1998001140A patent/PE133799A1/es not_active Application Discontinuation
- 1998-11-23 AU AU14158/99A patent/AU747204B2/en not_active Ceased
- 1998-11-23 CN CNA2008100835852A patent/CN101274929A/zh active Pending
- 1998-11-23 IL IL13579798A patent/IL135797A/xx not_active IP Right Cessation
- 1998-11-23 ID IDW20000993A patent/ID24726A/id unknown
- 1998-11-23 BR BR9812793-4A patent/BR9812793A/pt not_active Application Discontinuation
- 1998-11-23 EP EP98958039A patent/EP1036072B1/en not_active Expired - Lifetime
- 1998-11-23 DK DK98958039T patent/DK1036072T3/da active
- 1998-11-23 RU RU2000116548/04A patent/RU2204557C2/ru not_active IP Right Cessation
- 1998-11-23 DE DE69823694T patent/DE69823694T2/de not_active Expired - Lifetime
- 1998-11-23 TR TR2000/01480T patent/TR200001480T2/xx unknown
- 1998-11-23 CZ CZ20001856A patent/CZ298578B6/cs not_active IP Right Cessation
- 1998-11-23 ES ES98958039T patent/ES2219919T3/es not_active Expired - Lifetime
- 1998-11-23 AT AT98958039T patent/ATE266025T1/de not_active IP Right Cessation
- 1998-11-23 CN CN98813307A patent/CN1290265A/zh active Pending
- 1998-11-23 WO PCT/US1998/024523 patent/WO1999026943A1/en active IP Right Grant
- 1998-11-23 PL PL98341114A patent/PL195027B1/pl not_active IP Right Cessation
- 1998-11-23 ZA ZA9810685A patent/ZA9810685B/xx unknown
- 1998-11-23 CA CA002309352A patent/CA2309352C/en not_active Expired - Fee Related
- 1998-11-23 CO CO98068933A patent/CO4990946A1/es unknown
- 1998-11-23 TW TW087119396A patent/TWI236476B/zh not_active IP Right Cessation
- 1998-11-23 HU HU0100607A patent/HUP0100607A3/hu unknown
- 1998-11-23 AR ARP980105935A patent/AR017189A1/es active IP Right Grant
- 1998-11-23 PT PT98958039T patent/PT1036072E/pt unknown
- 1998-11-23 SK SK759-2000A patent/SK285153B6/sk not_active IP Right Cessation
- 1998-11-24 MY MYPI98005330A patent/MY140887A/en unknown
-
1999
- 1999-01-10 SA SA99190972A patent/SA99190972B1/ar unknown
-
2000
- 2000-05-24 NO NO20002659A patent/NO322022B1/no not_active IP Right Cessation
-
2001
- 2001-03-16 HK HK01101899A patent/HK1031726A1/xx not_active IP Right Cessation
-
2002
- 2002-10-29 JP JP2002315015A patent/JP2003128670A/ja not_active Withdrawn
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