http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1098651-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_ae340e00572753c0a042ff8b0f6dca49 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0406 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0455 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K51-0459 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-205 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K51-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-205 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-495 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K9-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 |
| filingDate | 1999-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2003-01-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d352ae067184895810ea9a880dea907b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b743c460312d42a88032995f03a47c13 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_72a1e32ede00a6d6263460c6ab2509e2 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ebedcffb00689fd2dde0602d970f0f50 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d5f9382d315f32bc014f053c539b6b09 |
| publicationDate | 2003-01-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-1098651-B1 |
| titleOfInvention | Novel urokinase inhibitors |
| abstract | Sulfonyl-substituted 3-amidino-phenylalanine derivatives (I) are used for the diagnosis, therapy or prevention of diseases associated with urokinase (UK) or UK receptors. Use of amidines of formula (I) (as the racemate or the D- or L-isomer) or their salts is claimed for the preparation of a composition for the diagnosis, therapy or prevention of diseases associated with UK or UK receptors. R1 = (i) OH, OR4 or NR5R6; (ii) 2- or 3-(COR7)-pyrrolidino, 2-, 3- or 4-(COR7)-piperidino (all optionally further substituted) or optionally 2-, 3- or 4-substituted piperidyl (all optionally having a fused aromatic or cycloaliphatic ring in the 2,3- or 3,4-position relative to the heteroatom); (iii) 4-(R8)-piperazino, COX, CONR'R'', CSNR'R'', SO2Y or (CH2)mX' (where the (CH2)m chain is optionally branched); or (iv) aralkyl, 5-8C cycloaliphatic ring, heteroaryl or heterocycloaliphatic group (all optionally ring substituted); R4 = optionally substituted 1-8C alkyl, 3-8C cycloalkyl or aralkyl; R5, R6 = arbitrary residues; R7 = OH, OR4, NR5R6 or 4-(R8)-piperazino; R8 = 1-6C alkyl, aryl, phenoxycarbonyl or benzyloxycarbonyl (all optionally substituted); or optionally unsaturated 1-6C alkoxy; X = H or (all optionally substituted) alkyl, aryl, heteroaryl or cycloalkyl; R', R'' = H or 1-4C alkyl; or R'' may also be aryl if R' = H; or NR'R'' = 5-7 membered heterocycloaliphatic ring, optionally containing a further heteroatom; Y = 1-8C alkyl, aryl, heteroaryl, aryloxy or heteroaryloxy (all optionally substituted); or NH2 or mono- or di-(1-3C alkyl)-amino; m = 1-8; X' = OH (optionally etherified by 1-4C alkyl, aralkyl, aryl or 1-4C hydroxyalkyl; or acylated by 2-7C alkanoyl), halo or tri-(1-3C alkyl)-amino (where the N may be part of a 5-7 membered ring optionally containing a further S heteroatom); R2 = optionally substituted phenyl; R3 = H or 1-4C alkyl; n = 0 or 1. Independent claims are included for: (1) N alpha -(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-D,L-phenylalanine-4-eth oxycarbonyl-piperazide (Ia), the corresponding L-enantiomer and their salts; (2) the use of compounds of formula R2-Z (II) or their salts for the preparation of a composition for targeting lymph cells; (3) a method for inhibiting UK in living organisms (especially humans) by adminstration of (I); and (4) a method for targeting lymph tissue in living organisms by administration of (II). Z = arbitrary group. |
| priorityDate | 1998-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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