http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-033984-A1
Outgoing Links
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|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
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| filingDate | 2001-07-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-01-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-033984-A1 |
| titleOfInvention | PIRROLIDINE DERIVATIVES, PROCEDURE FOR PREPARATION, PHARMACEUTICAL COMPOSITIONS AND THE USE OF SUCH DERIVATIVES FOR THE MANUFACTURE OF MEDICINES |
| abstract | Pyrrolidine derivatives, which comprise a compound of general formula (1) wherein R 1 is hydrogen, alkylcarbonyl or arylcarbonyl; R2 is alkyl, alkylcycloalkyl, alkylcycloalkylalkyl, cycloalkyl, halogenoalkyl, carboxyalkyl, aminoalkyl, dialkylaminoalkyl, alkoxyalkyl, alkoxycarbonylalkyl, alkynyl, aryl, arylalkyl, arylalkyl (alkoxycarbonyl) alkyl, aryl, arylalkyl, arylcarbonylalkyl, arylcarbonylalkyl, arylcarbonylalkyl, arylcarbonylalkyl, arylcarbonylalkyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, arylcarbonyl, aryl, arylcarbonyl heterocyclyl or heterocyclylalkyl; A is -C (O) -R3, -CH (OH) -R4, or -C (O) -NR5R6, wherein R3 and R4 are independently of the group consisting of alkyl, aryl, arylalkyl, arylalkyl and arylalkyl; R5 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, carboxyalkyl, or arylalkyl; R6 is alkyl, alkylcarbonylalkyl, cyanoalkyl, hydroxyalkyl, hydroxyalkyl (hydroxyalkyl), alkoxycarbonylalkyl, arylcarbonylalkyl, arylaminocarbonylalkyl, aryl (alkyl) aminocarbonyl, aminocarbonillaquilo, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl, cycloalkyl, cycloalkylalkyl, or carboxyalkyl, or R6 is selected from the group consisting of formulas (2), (3) and (4) or -NR5R6 in -C (O) NR5R6 for A represents a saturated ring of 5 or 6 members, optionally substituted with carboxy, alkyloxycarbonyl, hydroxy , alkoxycarbonylalkoxy, phenylalkyl or phenylalkoxycarbonyl, R 7 is hydrogen, alkyl, alkenyl, alkylthioalkyl, aryl, heteroaryl, carboxy alkyl, carboxy, alkoxycarbonylalkyl, arylalkyl, or heteroarylalkyl; or a compound of formula 5, R7a is hydrogen or alkyl; R8 is -OR9 or -NR10R11, wherein R9 is hydrogen, alkyl, arylalkyl; R10 is hydrogen or alkyl; and R11 is alkyl, aryl, heteroaryl, arylalkyl, or the group -NR10R11 represents a 5- or 6-membered ring optionally substituted with carboxy, alkyloxycarbonyl, hydroxy, alkoxycarbonylalkoxy, phenylalkyl or phenylalkoxycarbonyl; R12 is alkyl, aryl, or arylalkyl; Y is -O-, -O-S (O2) -, -O-C (O) - or -O- (C) -NH; m is 0, 1 or 2; X is -SO2, -CO-, -C (O) O-, -SO2NH-, or -C (O) NR13- wherein R13 is hydrogen, alkyl, aryl or carboxyalkyl; and dimeric forms, and / or pharmaceutically acceptable esters, and / or pharmaceutically acceptable salts, and / or pharmaceutically acceptable salts thereof. The compounds are useful as metalloprotease inhibitors, e.g. zinc proteases, in particular zinc hydrolases, and are effective in the treatment of diseases associated with vasoconstriction of increasing incidence. A process for its preparation, pharmaceutical compositions and the use of such derivatives for the manufacture of medicaments for the prophylaxis and treatment of disorders that are caused by the activity of the endothelin converting enzyme (ECE), especially myocardial ischemia, are also described. congestive heart failure, arrhythmia, hypertension, pulmonary hypertension, asthma, cerebral vasospasm, subarachnoidal hemorrhage, pre-eclampsia, kidney diseases, atherosclerosis, Bueger's disease, Takayasu arthritis, diabetic complications, lung cancer, prostate cancer, gastro-testinal disorders, endotoxic shock and septicemia, and for wound healing and menstruation control, glaucoma, graft rejection, diseases associated with cytostatic, ophthalmological and cerebroprotective indications, and organ protection. |
| priorityDate | 2000-07-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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