ECSP088111A - Derivados de 2-oxo-1,2,5,6-tetrahidropiridina inhibidores de la trombina - Google Patents
Derivados de 2-oxo-1,2,5,6-tetrahidropiridina inhibidores de la trombinaInfo
- Publication number
- ECSP088111A ECSP088111A EC2008008111A ECSP088111A ECSP088111A EC SP088111 A ECSP088111 A EC SP088111A EC 2008008111 A EC2008008111 A EC 2008008111A EC SP088111 A ECSP088111 A EC SP088111A EC SP088111 A ECSP088111 A EC SP088111A
- Authority
- EC
- Ecuador
- Prior art keywords
- tetrahydropiridine
- oxo
- derivatives
- thrombin inhibitors
- useful
- Prior art date
Links
- 229940122388 Thrombin inhibitor Drugs 0.000 title 1
- 239000003868 thrombin inhibitor Substances 0.000 title 1
- 108090000190 Thrombin Proteins 0.000 abstract 3
- 229960004072 thrombin Drugs 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 208000005189 Embolism Diseases 0.000 abstract 1
- 102100027612 Kallikrein-11 Human genes 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 101710152431 Trypsin-like protease Proteins 0.000 abstract 1
- 239000003146 anticoagulant agent Substances 0.000 abstract 1
- 229940127219 anticoagulant drug Drugs 0.000 abstract 1
- 230000009286 beneficial effect Effects 0.000 abstract 1
- 230000002860 competitive effect Effects 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D401/14—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 three or more hetero 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
- A61K31/435—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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/73—Unsubstituted amino or imino radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pyridine Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se provee un compuesto de la fórmula (I), en donde R1, R2a, R2b, R3a, R3b, R4, R5a, R5b, R6 a R8, A y G tienen los significados proporcionados en la descripción; estos compuestos son útiles, o como profármacos son útiles, como inhibidores competitivos de las proteasas tipo tripsina, tales como la trombina, y, de este modo, son útiles en particular para el tratamiento de condiciones en donde resulta beneficiosa la inhibición de la trombina (por ej., condiciones, tales como tromboembolias, en donde se requiere o es conveniente la inhibición de la trombina y/o en condiciones en donde es indicada una terapia anticoagulante).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0501413 | 2005-06-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP088111A true ECSP088111A (es) | 2008-02-20 |
Family
ID=37532584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EC2008008111A ECSP088111A (es) | 2005-06-17 | 2008-01-17 | Derivados de 2-oxo-1,2,5,6-tetrahidropiridina inhibidores de la trombina |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US20080207695A1 (es) |
| EP (1) | EP1893601A1 (es) |
| JP (1) | JP2008546684A (es) |
| KR (1) | KR20080021145A (es) |
| CN (1) | CN101243069A (es) |
| AR (1) | AR054512A1 (es) |
| AU (1) | AU2006258300A1 (es) |
| BR (1) | BRPI0612045A2 (es) |
| CA (1) | CA2610428A1 (es) |
| EC (1) | ECSP088111A (es) |
| IL (1) | IL187580A0 (es) |
| MX (1) | MX2007016090A (es) |
| NO (1) | NO20076071L (es) |
| RU (1) | RU2007146731A (es) |
| TW (1) | TW200738675A (es) |
| UY (1) | UY29600A1 (es) |
| WO (1) | WO2006135323A1 (es) |
| ZA (1) | ZA200710564B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8354444B2 (en) | 2008-09-18 | 2013-01-15 | Hoffmann-La Roche Inc. | Substituted pyrrolidine-2-carboxamides |
| CN113698386B (zh) * | 2020-05-22 | 2022-12-27 | 上海美悦生物科技发展有限公司 | 一种4(1h)-吡啶酮类化合物、其药物组合物和用途 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU698911B2 (en) * | 1995-04-04 | 1998-11-12 | Merck & Co., Inc. | Thrombin inhibitors |
| AU703744B2 (en) * | 1995-06-27 | 1999-04-01 | Merck & Co., Inc. | Pyridinone-thrombin inhibitors |
| CA2252964A1 (en) * | 1996-04-23 | 1997-10-30 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
| US5668289A (en) * | 1996-06-24 | 1997-09-16 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
| US5792779A (en) * | 1997-02-19 | 1998-08-11 | Merck & Co., Inc. | Pyridinone thrombin inhibitors |
| US5866573A (en) * | 1997-04-21 | 1999-02-02 | Merck & Co., Inc. | Pyrazinone thrombin inhibitors |
| UA75093C2 (en) * | 2000-10-06 | 2006-03-15 | Dimensional Pharm Inc | Aminopyridinyl-,aminoguanidinyl-, and alkoxyguanidinesubstituted phenylsubstituted phenylacetamides as protease inhibitors |
| AU2002246675A1 (en) * | 2000-12-18 | 2002-07-30 | Merck And Co., Inc. | Thrombin inhibitors |
| US6946283B2 (en) * | 2001-01-05 | 2005-09-20 | William Marsh Rice University | Ginkgo biloba levopimaradiene synthase |
| JP2004520399A (ja) * | 2001-02-09 | 2004-07-08 | メルク エンド カムパニー インコーポレーテッド | トロンビン阻害剤 |
| SI21097A (sl) * | 2001-12-04 | 2003-06-30 | Univerza V Ljubljani | Inhibitorji trombina |
| AR047521A1 (es) * | 2004-02-06 | 2006-01-25 | Astrazeneca Ab | Compuestos piridin-2-ona utiles como inhibidores de trombina |
-
2006
- 2006-06-14 CN CNA2006800293561A patent/CN101243069A/zh active Pending
- 2006-06-14 JP JP2008516787A patent/JP2008546684A/ja not_active Withdrawn
- 2006-06-14 BR BRPI0612045A patent/BRPI0612045A2/pt not_active IP Right Cessation
- 2006-06-14 CA CA002610428A patent/CA2610428A1/en not_active Abandoned
- 2006-06-14 MX MX2007016090A patent/MX2007016090A/es not_active Application Discontinuation
- 2006-06-14 KR KR1020087001291A patent/KR20080021145A/ko not_active Withdrawn
- 2006-06-14 UY UY29600A patent/UY29600A1/es not_active Application Discontinuation
- 2006-06-14 WO PCT/SE2006/000709 patent/WO2006135323A1/en not_active Ceased
- 2006-06-14 US US11/917,515 patent/US20080207695A1/en not_active Abandoned
- 2006-06-14 RU RU2007146731/04A patent/RU2007146731A/ru not_active Application Discontinuation
- 2006-06-14 EP EP06747902A patent/EP1893601A1/en not_active Withdrawn
- 2006-06-14 AU AU2006258300A patent/AU2006258300A1/en not_active Abandoned
- 2006-06-16 AR ARP060102570A patent/AR054512A1/es not_active Application Discontinuation
- 2006-06-16 TW TW095121779A patent/TW200738675A/zh unknown
-
2007
- 2007-11-22 IL IL187580A patent/IL187580A0/en unknown
- 2007-11-27 NO NO20076071A patent/NO20076071L/no not_active Application Discontinuation
- 2007-12-04 ZA ZA200710564A patent/ZA200710564B/xx unknown
-
2008
- 2008-01-17 EC EC2008008111A patent/ECSP088111A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2007146731A (ru) | 2009-07-27 |
| KR20080021145A (ko) | 2008-03-06 |
| AU2006258300A1 (en) | 2006-12-21 |
| UY29600A1 (es) | 2007-01-31 |
| ZA200710564B (en) | 2008-11-26 |
| IL187580A0 (en) | 2008-03-20 |
| BRPI0612045A2 (pt) | 2018-07-24 |
| WO2006135323A1 (en) | 2006-12-21 |
| CN101243069A (zh) | 2008-08-13 |
| TW200738675A (en) | 2007-10-16 |
| JP2008546684A (ja) | 2008-12-25 |
| EP1893601A1 (en) | 2008-03-05 |
| CA2610428A1 (en) | 2006-12-21 |
| MX2007016090A (es) | 2008-03-10 |
| AR054512A1 (es) | 2007-06-27 |
| US20080207695A1 (en) | 2008-08-28 |
| NO20076071L (no) | 2008-01-08 |
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