http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2176645-C2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_634715a790f7ef0163a61e9f364bebcd |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D205-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-60 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-05 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-443 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-395 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D205-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4025 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-397 |
| filingDate | 1996-07-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2001-12-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7e0681f5ca3d4bd91765a62d60474014 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_431aeb056f5b22fa20df063c09d01ebd |
| publicationDate | 2001-12-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2176645-C2 |
| titleOfInvention | Thrombin inhibitors, pharmaceutical composition based on thereof, method of treatment, method of their synthesis (versions) and protected derivative |
| abstract | FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel compounds of the formula (I) where p and q = 0, 1, 2, 3 or 4 independently; R means H, 2,3-epoxypropyl, C 1-6 -alkyl (the latter is possibly substituted or terminated by one or more hydroxy-group), structural fragment of the formula (Ia) where A 1 means C 1-4 4-alkylene and R x means H or when p = 0 then in common with R 2 it means structural fragment of the formula (Ib) where R y means H; R 2 means H, naphthyl, indolyl, C 1-4 -alkyl (the latter group is possibly substituted or terminated by one or more hydroxy-group), C 3-8 -cycloalkyl, phenyl (the two latter groups are possibly substituted with one or more C 1-4 -alkyl, C 1-4 -alkoxy-group, halogen atom, hydroxy-group, nitro-group, methylenedioxy-group, trifluoromethyl-group, N(H)-R 23 or C(O)O-R 24 ) or when p = 0 then in common with R 1 it means structural fragment of the formula (Ib); R 3 means H, naphthyl, indolyl, C 1-6 -alkyl (the latter group is possibly substituted or terminated by one or more hydroxy-group), C 3-8 -cycloalkyl or phenyl (the two latter groups are possibly substituted with one or more C 1-4 -alkyl, C 1-4 -alkoxy-group, halogen atom, hydroxy-group, nitro-group, methylenedioxy-group, trifluoromethyl group, N(H)-R 27 or C(O)O-R 28 ; R 23 and R 27 mean independently H, C 1-4 -alkyl or C(O)-R 29 ; R 24 ,R 28 ,R 29 mean independently H or C 1-4 -alkyl; R 4 means H or C 1-4 -alkyl; Y means C 1-4 -alkylene possibly substituted with C 1-4 -alkyl, methylene or oxo-group; n = 1 or 2; B means structural fragment of the formula (IVa) , (IVb) or (IVc) where R 5 means H; X′ and X 2 mean independently a simple bond or CH 2 ; under condition that when R 1 ,R 2 ,R 4 all mean H, p = 0, Y means (CH 2 ) 2 , n = 1 and: (a) R 3 means unsubstituted phenyl and: (1) B is structural fragment of the formula (IVa) and R 5 means H and then q is not 0 or 1; and (2) B is structural fragment of the formula (IVb) and X′ and X 2 both mean CH 2 and then q is not 0; and (b) R 3 means unsubstituted cyclohexyl group; B means structural fragment of the formula (IVa) and R 5 means H and then q is not 0; or its pharmaceutically acceptable salt. New compounds are useful as competitive inhibitors of trypsin-like proteases, for example, thrombin and especially in treatment of states where inhibition of thrombin is required (for example, in thrombosis) or as anticoagulating agents. Invention describes also a pharmaceutical composition based on thereof, method of patients treatment, method of their synthesis (variants) and protected derivative. EFFECT: new compounds indicated above, improved method of synthesis and treatment, valuable medicinal properties. 44 cl, 61 ex |
| priorityDate | 1995-07-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 243.