http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1654241-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_cf32b60391b469c41e86c353437f5751 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0a70b05f3bdf7f6e9aaf7a41ac3aacdc |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D291-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D285-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-33 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D273-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-33 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D291-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D285-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D273-02 |
| filingDate | 2004-07-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2008-03-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e8a571e45191ccf1e8480816be9beb26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ac24b8808e8f40f671ee4d9e93ab3466 |
| publicationDate | 2008-03-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-1654241-B1 |
| titleOfInvention | Macrocyclic compounds having aspartic protease inhibiting activity and pharmaceutical uses thereof |
| abstract | The present invention relates to macro-cyclic compounds of formula (I), wherein R<SUB>1</SUB>, is (C<SUB>1-8</SUB>)alkyl, (C<SUB>1-4</SUB>)alkoxy(C<SUB>1-4</SUB>)alkyl, hydroxy(C<SUB>1-6</SUB>)alkyl, (C<SUB>1-4</SUB>)alkylthio(C<SUB>1-4</SUB>)alkyl, (C<SUB>1-6</SUB>)alkenyl, (C<SUB>3-7</SUB>)cycloalkyl, (C<SUB>3-7</SUB>)cycloalkyl(C<SUB>1-4</SUB>)alkyl, piperidinyl or pyrrolidinyl, R<SUB>2 </SUB>and R<SUB>4</SUB>, independently, are hydrogen or optionally substituted (C<SUB>1-8</SUB>)alkyl, (C<SUB>3-7</SUB>)cycloalkyl, (C<SUB>3-7</SUB>)cycloalkyl(C<SUB>1-4</SUB>)alkyl, aryl, aryl(C<SUB>1-4</SUB>)alkyl, heteroaryl or heteroaryl(C<SUB>1-4</SUB>)alkyl, or R<SUB>2 </SUB>and R<SUB>4</SUB>, together with the nitrogen to which they are attached, form an optionally substituted piperidino, pyrrolidinyl, morpholino or piperazinyl group, R<SUB>3 </SUB>is hydrogen or (C<SUB>1-4</SUB>)alkyl, X<SUB>1 </SUB>is CH<SUB>2</SUB>, X<SUB>2 </SUB>is CH<SUB>2</SUB>, O, S, CO, COO, OCO, NHCO, CONH, or NR, R being hydrogen or (C<SUB>1-4</SUB>)alkyl, Y is (C<SUB>1-8</SUB>)alkylen or (C<SUB>1-8</SUB>)alkylenoxy(C<SUB>1-6</SUB>)alkylen, (C<SUB>1-8</SUB>)alkenylen or (C<SUB>1-8</SUB>)alkenylenoxy(C<SUB>1-6</SUB>)alkylen, Ar is a phenyl ring optionally mono- di or trisubstituted by, independently, hydroxy or halogen, whereby X<SUB>1</SUB>, and X<SUB>2 </SUB>are in meta or para position to each other, and either Z is CO, AA is a natural or unnatural alpha-amino-acid, and n is 0 or 1, or Z is S0<SUB>2</SUB>, AA is an optionally substituted ethylencarbonyl group (derived from a natural or unnatural alpha-amino acid by replacement of the nitrogen by a methylen group), and n is 1; processes for the preparation of these compounds; pharmaceutical compositions and combinations comprising the same; and their use in the treatment of neurological and vascular disorders related to beta-amyloid generation and/or aggregation. |
| priorityDate | 2003-07-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 365.