http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035970-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1f874eb11d4775decc4fd06a6071a4c9 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D493-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4439 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5383 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D263-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-429 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-427 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-424 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-423 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D493-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-04 |
| filingDate | 2002-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-07-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-035970-A1 |
| titleOfInvention | 2-AMINO-BENZOXAZOL SULFONAMID SULFONAMID SPECTRUM OF HIV PROTEASE, PHARMACEUTICAL COMPOSITION, "IN VITRO" METHOD TO INHIBIT THE RETROVIRAL REPLICATION, AND USE OF THESE COMPOUNDS IN THE MANUFACTURE OF MEDICINAL MANUFACTURE |
| abstract | 2-amino-benzoxazol sulfonamides having the formula (1), an N-oxide, salt, stereoisomeric form, racemic mixtures, prodrug, ester or metabolite thereof, in which R1 and R8 are, independently of each other, hydrogen, alkyl C1-6, C2-6 alkenyl, C1-6 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-6 alkyl, aryl, Het1, Het1-C1-6 alkyl, Het2, or Het2-C1-6 alkyl; R1 can also be a radical of formula (R11a) (R11b) NC (R10a) (R10b) -CHR9- in which R9, R10a and R10b are, independently of each other, hydrogen, C1-4 alkyloxycarbonyl, carboxyl, aminocarbonyl, mono - or di (C1-4 alkyl) aminocarbonyl, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, or C1-4 alkyl optionally substituted with aryl, Het1, Het2, C3-7 cycloalkyl, C1-4 alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di (C1-4 alkyl) aminocarbonyl, aminosulfonyl, C1-4S alkyl (O) t, hydroxy, cyano, halogen or optionally mono- or disubstituted amino, where the substituents are independently selected from each other, from the group consisting of C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, Het1, Het2, Het1-C1-4 alkyl and Het2-C1-4 alkyl; whereby R9, R10a and the carbon atoms to which they are attached can also form a C3-7 cycloalkyl radical; when L is -O-C1-6-C-alkanediyl (= O) - or -NR8-C1-6-C-alkanediyl (= O) -, then R9 can also be oxo; R11a is hydrogen, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, aryl, optionally mono- or disubstituted aminocarbonyl, optionally mono- or disubstituted C1-4 -alkylcarbonyloxy, C1-4 alkyloxycarbonyl, aryloxycarbonyl, Het1-oxycarbonyl, Het2 -oxycarbonyl, C 1-4 aryloxycarbonylalkyl, C 1-4 aryl alkoxycarbonyl, C 1-7 alkylcarbonyl, C 3-7 cycloalkylcarbonyl, C 3-7 cycloalkylcarbonyloxy, C 1-4 cycloalkylcarbonyloxy, C 1-4 alkylcarbonyloxy, C1-4, arylcarbonyloxy, aryloxycarbonyloxy, Het1-carbonyl, Het1-carbonyloxy, Het1-C1-4 alkyloxycarbonyloxy, Het2-carbonyloxy, Het2-C1-4alkylcarbonyloxy, or C1-4alkyloxycarbonyloxy C1-4 alkyl optionally substituted with aryl, aryloxy, Het2, halogen or hydroxy; where the substituents in the amino groups are independently selected from each other, from the group consisting of C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, Het1, Het2, Het1-alkyl C1-4 and Het2-C1-4 alkyl; R11b is hydrogen, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, Het1, Het2 or C1-4 alkyl optionally substituted by halogen, hydroxy, C1-4 S (O) t alkyl, aryl, C3 cycloalkyl -7, Het1, Het2, optionally mono- or disubstituted amino, where the substituents, independently from each other, are selected from the group consisting of C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl alkyl C1-4, Het1, Het2, Het1-C1-4 alkyl and Het2-C1-4 alkyl; where R11b can be attached to the rest of the molecule through a sulfonyl group; t is independently from each other 0, 1 or 2; R2 is hydrogen or C1-6 alkyl; L is -C (= O) -, -OC (= O) -, -NR8-C (O) -, -O-C1-6-C-alkanediyl (= O) -, -NR8-C1-6- alkanediyl- C (= O) -, -S (= O) 2-, -OS (= O) 2-, -NR8-S (= O) 2, where either group C (= O) or group S ( = O) 2 is attached to the NR2 portion; and whereby the C1-6 alkanediyl portion is optionally substituted with hydroxy, aryl, Het1 and Het2; R3 is C1-6 alkyl, aryl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl or C1-4 arylalkyl; R 4 is hydrogen, C 1-4 alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di (C 1-4 alkyl) aminocarbonyl, C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 1-6 alkyl optionally substituted with one or more substituents selected, independently from each other, from the group consisting of aryl, Het1, Het2, C3-7 cycloalkyl, C1-4 alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di (C1-4 alkyl) aminocarbonyl, aminosulfonyl, C1-4 alkyl (= O) t, hydroxy, cyano, halogen and optionally mono- or disubstituted amino, where the substituents are independently selected from the group consisting of C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, Het1, Het2, Het1-C1-4 alkyl and Het2-C1-4 alkyl; R5 is hydrogen or C1-6 alkyl; R6 is hydrogen or C1-6 alkyl; pharmaceutical composition, "in vitro" method to inhibit retroviral replication and use of these compounds in the manufacture of drugs. The compounds of formula (1) are used as inhibitors of aspartic protease, in particular of the HIV protease, hence their inhibitory action on the AIDS virus. |
| priorityDate | 2001-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 51.