ES2171945T3 - Derivados aromaticos de amidina que sirven de inhibidores selectivos de la trombina. - Google Patents
Derivados aromaticos de amidina que sirven de inhibidores selectivos de la trombina.Info
- Publication number
- ES2171945T3 ES2171945T3 ES97925316T ES97925316T ES2171945T3 ES 2171945 T3 ES2171945 T3 ES 2171945T3 ES 97925316 T ES97925316 T ES 97925316T ES 97925316 T ES97925316 T ES 97925316T ES 2171945 T3 ES2171945 T3 ES 2171945T3
- Authority
- ES
- Spain
- Prior art keywords
- thrombin
- amidina
- serve
- selective inhibitors
- aromatic derivatives
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 108090000190 Thrombin Proteins 0.000 title abstract 2
- 229960004072 thrombin Drugs 0.000 title abstract 2
- 229940124639 Selective inhibitor Drugs 0.000 title 1
- 101000712605 Theromyzon tessulatum Theromin Proteins 0.000 abstract 1
- 229940122388 Thrombin inhibitor Drugs 0.000 abstract 1
- -1 aromatic amidine Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 230000003389 potentiating effect Effects 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000003868 thrombin inhibitor Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D405/14—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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pyrrole Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
Abstract
LA PRESENTE INVENCION SE REFIERE A UN NUEVO INHIBIDOR DE TROMBINA QUE ES EFECTIVO INCLUSO CUANDO SE ADMINISTRA ORALMENTE. DE MODO ESPECIFICO, LA PRESENTE INVENCION SE REFIERE A UN DERIVADO DE AMIDINA AROMATICO REPRESENTADO POR LA FORMULA (I) Y A LAS SALES DE DICHO DERIVADO, LOS CUALES DESARROLLAN UNA POTENTE ACTIVIDAD DE INHIBICION SELECTIVA FRENTE A LA TROMBINA, EN DONDE, (A), R, R 1 , R 2 , R 3 , A, W, Y Y N SE DEFINEN EN LA DESCRIPCION DE LA INVENCION.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR19960019282 | 1996-05-31 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2171945T3 true ES2171945T3 (es) | 2002-09-16 |
Family
ID=19460481
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES97925316T Expired - Lifetime ES2171945T3 (es) | 1996-05-31 | 1997-05-31 | Derivados aromaticos de amidina que sirven de inhibidores selectivos de la trombina. |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US6201006B1 (es) |
| EP (1) | EP0918768B1 (es) |
| JP (1) | JP3202994B2 (es) |
| KR (1) | KR100469028B1 (es) |
| CN (1) | CN1079396C (es) |
| AT (1) | ATE211741T1 (es) |
| AU (1) | AU3049497A (es) |
| CA (1) | CA2256438C (es) |
| DE (1) | DE69709933T2 (es) |
| ES (1) | ES2171945T3 (es) |
| WO (1) | WO1997045424A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6602864B1 (en) * | 1996-12-13 | 2003-08-05 | Aventis Pharma Deutschland Gmbh | Sulfonic acid or sulfonylamino N-(heteroaralkyl)-azaheterocyclylamide compounds |
| KR19990043605A (ko) * | 1997-11-29 | 1999-06-15 | 이경하 | 선택적 트롬빈 억제제로 유용한 방향족 아미딘유도체 |
| PL343424A1 (en) | 1998-04-10 | 2001-08-13 | Japan Tobacco Inc | Amidine compounds |
| WO2000073269A2 (en) * | 1999-06-02 | 2000-12-07 | Regents Of The University Of Minnesota | Nicotine receptor ligands |
| GB9924155D0 (en) * | 1999-10-12 | 1999-12-15 | Rhone Poulenc Rorer Pharma | Chemical compounds |
| DE60024120T2 (de) * | 1999-08-26 | 2006-07-27 | Aventis Pharmaceuticals Inc. | Substituierte (aminoiminomethyl oder aminomethyl) dihydrobenzofurane und benozopyrane |
| US7361663B2 (en) * | 1999-11-10 | 2008-04-22 | Aventis Pharmaceuticals Inc. | N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa |
| EP1263726B1 (en) * | 1999-11-10 | 2007-09-26 | Sanofi-Aventis Deutschland GmbH | N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor xa |
| JP2007511467A (ja) * | 2003-05-14 | 2007-05-10 | タケダ サン ディエゴ インコーポレイテッド | ジペプチジルペプチダーゼインヒビター |
| JP2005350417A (ja) * | 2004-06-11 | 2005-12-22 | Dai Ichi Seiyaku Co Ltd | 還元的エーテル化法を用いたピロリジン誘導体の製造法 |
| WO2006038119A1 (en) * | 2004-10-08 | 2006-04-13 | Warner-Lambert Company Llc | Stereoselective synthesis of n-protected alkoxy prolines |
| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
| EP2023874A4 (en) * | 2006-06-02 | 2009-07-08 | Bioseek Inc | METHOD FOR IDENTIFYING ACTIVE SUBSTANCES AND THEIR USE FOR THE PREVENTION OF RESTENOSIS |
| EP2085397A1 (en) * | 2008-01-21 | 2009-08-05 | Esteve Quimica, S.A. | Crystalline form of abacavir |
| AU2012252165A1 (en) | 2011-05-09 | 2013-03-21 | Cambridge Enterprise Limited | Methods of modulating micrornas in the treatment of pulmonary arterial hypertension |
| WO2020072580A1 (en) * | 2018-10-02 | 2020-04-09 | Disc Medicine, Inc. | Matriptase 2 inhibitors and uses thereof |
| CN113956192A (zh) * | 2021-11-16 | 2022-01-21 | 上海延安药业(湖北)有限公司 | 一种阿维巴坦中间体的合成方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4258192A (en) * | 1977-12-16 | 1981-03-24 | Mitsubishi Chemical Industries Limited | N2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof |
| JPS5813549A (ja) * | 1981-07-15 | 1983-01-26 | Kowa Co | 新規フエニルエステル類 |
| ZA928276B (en) * | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
| JPH0820532A (ja) * | 1994-07-05 | 1996-01-23 | Dai Ichi Seiyaku Co Ltd | 抗膵炎剤 |
-
1997
- 1997-05-31 CN CN97195005A patent/CN1079396C/zh not_active Expired - Fee Related
- 1997-05-31 US US09/180,675 patent/US6201006B1/en not_active Expired - Fee Related
- 1997-05-31 KR KR1019970022566A patent/KR100469028B1/ko not_active Expired - Fee Related
- 1997-05-31 AU AU30494/97A patent/AU3049497A/en not_active Abandoned
- 1997-05-31 CA CA002256438A patent/CA2256438C/en not_active Expired - Fee Related
- 1997-05-31 ES ES97925316T patent/ES2171945T3/es not_active Expired - Lifetime
- 1997-05-31 JP JP54206597A patent/JP3202994B2/ja not_active Expired - Fee Related
- 1997-05-31 EP EP97925316A patent/EP0918768B1/en not_active Expired - Lifetime
- 1997-05-31 WO PCT/KR1997/000100 patent/WO1997045424A1/en not_active Ceased
- 1997-05-31 DE DE69709933T patent/DE69709933T2/de not_active Expired - Fee Related
- 1997-05-31 AT AT97925316T patent/ATE211741T1/de not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| JP3202994B2 (ja) | 2001-08-27 |
| KR100469028B1 (ko) | 2005-07-07 |
| ATE211741T1 (de) | 2002-01-15 |
| EP0918768A1 (en) | 1999-06-02 |
| CN1079396C (zh) | 2002-02-20 |
| CA2256438C (en) | 2002-10-15 |
| EP0918768B1 (en) | 2002-01-09 |
| CN1219932A (zh) | 1999-06-16 |
| CA2256438A1 (en) | 1997-12-04 |
| WO1997045424A1 (en) | 1997-12-04 |
| US6201006B1 (en) | 2001-03-13 |
| KR970074779A (ko) | 1997-12-10 |
| JP2000504030A (ja) | 2000-04-04 |
| DE69709933D1 (en) | 2002-02-28 |
| AU3049497A (en) | 1998-01-05 |
| DE69709933T2 (de) | 2002-08-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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