PE20010954A1 - BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINES - Google Patents
BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINESInfo
- Publication number
- PE20010954A1 PE20010954A1 PE2000001365A PE0013652000A PE20010954A1 PE 20010954 A1 PE20010954 A1 PE 20010954A1 PE 2000001365 A PE2000001365 A PE 2000001365A PE 0013652000 A PE0013652000 A PE 0013652000A PE 20010954 A1 PE20010954 A1 PE 20010954A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- preparation
- benzhimidazoles
- medicines
- amidine
- Prior art date
Links
- 239000003814 drug Substances 0.000 title 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Natural products C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 4
- -1 PYRROLIDINE CARBONYL Chemical class 0.000 abstract 3
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 150000001409 amidines Chemical group 0.000 abstract 1
- 150000001412 amines Chemical class 0.000 abstract 1
- 229960004676 antithrombotic agent Drugs 0.000 abstract 1
- ONDMKQWGMAVUNZ-UHFFFAOYSA-N butyl 2-aminoacetate Chemical compound CCCCOC(=O)CN ONDMKQWGMAVUNZ-UHFFFAOYSA-N 0.000 abstract 1
- 229910052731 fluorine Inorganic materials 0.000 abstract 1
- 239000011737 fluorine Substances 0.000 abstract 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
- C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
SE REFIERE A BENCIMIDAZOLES DE FORMULA I, DONDE Ra ES ALQUILO C1-C3 SUSTITUIDO CON FLUOR, PIRROLIDINOCARBONILO, AMINO, ALQUILO C1-C3, ENTRE OTROS; Rb ES ALQUILO C1-C3; Rc ES AMIDINO, CIANO, 1,2,4-OXADIZOL-3-ILO SUSTITUIDO EN POSICION 5 POR ALQUILO C1-C3, FENILO; SON COMPUESTOS PREFERIDOS 2-[4-(N-FENILCARBONIL-AMIDINO)-FENILAMINOMETIL]-1-METIL-5-[1-(n-BUTILOXICARBONILMETILAMINO)-1-(PIRROLIDINOCARBONIL)-ETIL]BENCIMIDAZOL, 2-(4-AMIDINOFENILAMINOMETIL)-1-METIL-5-[1-(TETRAZOL-5-IL-METILAMINO)-1-(PIRROLIDINOCARBONIL)-ETIL]BENCIMIDAZOL, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS I PUEDEN SER UTILES COMO ANTITROMBOTICOSREFERS TO BENZYMIDAZOLES OF FORMULA I, WHERE Ra IS C1-C3 ALKYL SUBSTITUTE WITH FLUORINE, PYRROLIDINE CARBONYL, AMINE, C1-C3 ALKYL, AMONG OTHERS; Rb IS C1-C3 ALKYL; Rc IS AMIDINE, CYANE, 1,2,4-OXADIZOL-3-ILO SUBSTITUTED AT POSITION 5 BY C1-C3 ALKYL, PHENYL; PREFERRED COMPOUNDS ARE 2- [4- (N-PHENYLCARBONYL-AMIDINE) -PHENYLAMINOMETHYL] -1-METHYL-5- [1- (n-BUTYLOXYCARBONYLMETHYLAMINE) -1- (PYRROLIDINOCARBONYL) -ETHYL] BENZIMIDAZOLE, 2- (4-AMIDOMETHYLLINOPHENE ) -1-METHYL-5- [1- (TETRAZOL-5-IL-METHYLAMINE) -1- (PYRROLIDINE CARBONYL) -ETHYL] BENZIMIDAZOLE, AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR PREPARATION. COMPOUNDS I MAY BE USEFUL AS ANTI-THROMBOTICS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19962329A DE19962329A1 (en) | 1999-12-23 | 1999-12-23 | New substituted 2-(phenylaminomethyl)-benzimidazoles, used as thrombin inhibitors, serine protease inhibitors, antithrombotic agents and intermediates |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20010954A1 true PE20010954A1 (en) | 2001-10-09 |
Family
ID=7934028
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2000001365A PE20010954A1 (en) | 1999-12-23 | 2000-12-19 | BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINES |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1244636A1 (en) |
| JP (1) | JP2003519129A (en) |
| AR (1) | AR027050A1 (en) |
| AU (1) | AU2011501A (en) |
| CA (1) | CA2393916A1 (en) |
| DE (1) | DE19962329A1 (en) |
| MX (1) | MXPA02006299A (en) |
| PE (1) | PE20010954A1 (en) |
| UY (1) | UY26492A1 (en) |
| WO (1) | WO2001047896A1 (en) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10125478A1 (en) * | 2001-05-25 | 2002-11-28 | Boehringer Ingelheim Pharma | Treatment or prophylaxis of arterial thrombosis, using 5-quinolinesulfonylamino-benzimidazole derivatives having combined thrombin inhibiting and fibrinogen receptor inhibiting action |
| DE10227666A1 (en) * | 2002-06-20 | 2004-01-08 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | (R) -2- (4-amidinophenylaminomethyl) -1-methyl-5- [1- (carboxymethylamino) -1- (pyrrolidinocarbonyl) ethyl] benzimidazole, its monohydrochloride, process for its preparation and use as a medicament |
| US7169934B2 (en) | 2002-06-20 | 2007-01-30 | Boehringer Ingelheim International Gmbh | (R) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1 (pyrrolidinocarbonyl)-ethyl]-benzimidazole, the monohydrochloride thereof, preparation thereof and the use as pharmaceutical composition |
| PE20040804A1 (en) * | 2002-12-19 | 2004-12-31 | Boehringer Ingelheim Pharma | CARBOXAMID DERIVATIVES AS INHIBITORS OF THE Xa FACTOR |
| US7371743B2 (en) | 2004-02-28 | 2008-05-13 | Boehringer Ingelheim International Gmbh | Carboxylic acid amides, the preparation thereof and their use as medicaments |
| EP1609784A1 (en) * | 2004-06-25 | 2005-12-28 | Boehringer Ingelheim Pharma GmbH & Co.KG | Process for the preparation of 4-(benzimidazolylmethylamino)-benzamidines |
| DE102005061624A1 (en) | 2005-12-21 | 2007-06-28 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Improved process for the preparation of salts of 4- (benzimidazolylmethylamino) -benzamidines |
| DE102005061623A1 (en) | 2005-12-21 | 2007-06-28 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Improved process for the preparation of 4- (benzimidazolylmethylamino) -benzamidines and their salts |
| US10077251B2 (en) | 2012-10-29 | 2018-09-18 | Biophore India Pharmaceuticals Pvt. Ltd. | Process for the synthesis of Dabigatran Etexilate and its intermediates |
| WO2014068587A2 (en) * | 2012-10-29 | 2014-05-08 | Biophore India Pharmaceuticals Pvt. Ltd. | An improved process for the synthesis of dabigatran and its intermediates |
| RU2623439C1 (en) * | 2016-10-14 | 2017-06-26 | федеральное государственное автономное образовательное учреждение высшего образования "Южный федеральный университет" | 1-substituted-3-{[2-(3,5-di-tret-4-hydroxyphenyl)-2-oxoethyl]}-2aminobenzimidazolium bromides with antiplatelet and antioxidant properties |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4129603A1 (en) * | 1991-09-06 | 1993-03-11 | Thomae Gmbh Dr K | CONDENSED 5-LOW HETEROCYCLES, METHOD FOR THE PRODUCTION THEREOF, AND MEDICAMENTS CONTAINING THESE COMPOUNDS |
| EP1060166A1 (en) * | 1998-02-03 | 2000-12-20 | Boehringer Ingelheim Pharma KG | Five-membered, benzo-condensed heterocycles used as antithrombotic agents |
| DE19829964A1 (en) * | 1998-07-04 | 2000-01-05 | Boehringer Ingelheim Pharma | New benzimidazolyl amidine or nitrile compounds, used as thrombin inhibitors, antithrombotic agents or intermediates |
| TWI248435B (en) * | 1998-07-04 | 2006-02-01 | Boehringer Ingelheim Pharma | Benzimidazoles, the preparation thereof and their use as pharmaceutical compositions |
-
1999
- 1999-12-23 DE DE19962329A patent/DE19962329A1/en not_active Withdrawn
-
2000
- 2000-12-16 AU AU20115/01A patent/AU2011501A/en not_active Abandoned
- 2000-12-16 JP JP2001549368A patent/JP2003519129A/en active Pending
- 2000-12-16 EP EP00983342A patent/EP1244636A1/en not_active Withdrawn
- 2000-12-16 WO PCT/EP2000/012841 patent/WO2001047896A1/en not_active Ceased
- 2000-12-16 CA CA002393916A patent/CA2393916A1/en not_active Abandoned
- 2000-12-16 MX MXPA02006299A patent/MXPA02006299A/en unknown
- 2000-12-19 PE PE2000001365A patent/PE20010954A1/en not_active Application Discontinuation
- 2000-12-20 UY UY26492A patent/UY26492A1/en not_active Application Discontinuation
- 2000-12-21 AR ARP000106819A patent/AR027050A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2393916A1 (en) | 2001-07-05 |
| JP2003519129A (en) | 2003-06-17 |
| AR027050A1 (en) | 2003-03-12 |
| WO2001047896A1 (en) | 2001-07-05 |
| MXPA02006299A (en) | 2002-12-09 |
| UY26492A1 (en) | 2001-07-31 |
| EP1244636A1 (en) | 2002-10-02 |
| DE19962329A1 (en) | 2001-06-28 |
| AU2011501A (en) | 2001-07-09 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FD | Application declared void or lapsed |