http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-037976-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1f874eb11d4775decc4fd06a6071a4c9 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2603-18 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D493-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D277-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C311-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-497 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D233-88 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/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D233-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D493-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-443 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D233-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 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/A61K31-426 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-425 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4245 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-421 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4188 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4178 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D263-32 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4164 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C311-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-415 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-41 |
| filingDate | 2002-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2004-12-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-037976-A1 |
| titleOfInvention | SULFONAMIDS CONTAINING REPLACED PHENYLL WITH HETEROCICLICAL GROUPS, A PHARMACEUTICAL COMPOSITION, A PRODUCT COMBINED WITH AN ANTIRRETROVIRAL AGENT AND THE USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT. |
| abstract | Claim 1: Sulfonamides containing phenyl substituted with heterocyclic groups having the formula (1) its N-oxide, salt, stereoisomeric form, racemic mixture, pro-drug, ester or metabolite, wherein: R1 and R8 are each , independently, hydrogen, C1-6 alkyl, C2-6 alkenyl, C1-6 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-6 alkyl, aryl, Het1, Het1 C1-6 alkyl, Het2, Het2 alkyl C1-6; R1 can also be a radical of the formula (2) where: R9, R10a and R10b are each independently 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 (C 1-4 alkyl) aminocarbonyl, aminosulfonyl, C 1-4 alkyl (O) t, hydroxy, cyano, halogen or amino, mono- or optionally substituted where the substituents are selected from C 1-4 alkyl, aryl, arylalkyl C1-4, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, Het1, Het2, Het1 C1-4 alkyl and Het2 C1-4 alkyl; where R9, R10a and the carbon atoms to which they are attached can also form a C3-7 cycloalkyl radical; R 11a is hydrogen, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, aryl, aminocarbonyl, mono- or optionally substituted, optionally substituted C 1-4 alkylaminocarboxyloxy, C 1-4 alkyloxycarbonyl, aryloxycarbonyl, Het1 oxycarbonyl, Het2 oxycarbonyl, aryloxycarbonylalkylC 1-4, arylalkylC 1-4 oxycarbonyl, alkylC 1-4 alkyl, cycloalkylcarbonylC3-7, cycloalkyl C3-7 alkyloxycarbonyl C1-4, cycloalkylcarbonyloxyC3-4alkylcarbonyloxycarbonyl C1-4, C1-4 arylalkylcarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, Het1 carbonyl, Het1 carbonyloxy, Het1 C1-4 alkyloxycarbonyl, Het2 carbonyloxy, Het2 C1-4 alkylcarbonyloxy or C1-4 alkyloxycarbonyloxy or C1-4 alkyl optionally substituted with aryl , aryloxy, Het2 or hydroxy; where the substituents in the amino groups are each independently selected from C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, Het1, Het2, Het1 C1 alkyl -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 substituted, optionally, with halogen, hydroxy, C1-4S alkyl (= O) t, aryl, C3-7 cycloalkyl, Het1, Het2, amino, mono- or disubstituted, optionally, where the substituents are selected from C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 alkyl cycloalkyl C1-4, Het1, Het2, Het1 C1-4 alkyl and Het2 C1-4 alkyl; where R11b can be attached to the rest of the molecule by means of a sulfonyl group, 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 group C (= O) or group S (= O) 2 is attached to the NR2 portion; 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, carboxy, mono- or optionally substituted aminocarbonyl, C 3-7 cycloalkyl, C 2-6 alkenyl, C 2-6 alkynyl or C 1-6 alkyl, wherein C 3-7 cycloalkyl, C 2- alkenyl 6, C2-6 alkynyl and C1-6 alkyl may optionally be substituted with a substituent selected from aryl, Het1, Het2, C3-7 cycloalkyl, C1-4 alkyloxycarbonyl, carboxyl, mono- or optionally substituted aminocarbonyl , optionally mono- or disubstituted aminosulfonyl, C1-4alkyl S (= O) t, hydroxy, cyano, optionally mono- or disubstituted amino and halogen, and where the optional substituents on the amino function are selected, so independent 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; t is 0, 1 or 2; each t independently selected is 0, 1 or 2; H aryl is a monocyclic, bicyclic or tricyclic aromatic heterocycle having 3 to 14 members in the ring containing one or more heteroatoms selected from nitrogen, oxygen and sulfur in the ring and which may optionally be substituted at ( 1) one or more carbon atoms by C1-6 alkyl, halogen, hydroxy, mono- or optionally substituted amino, nitro, cyano, C1-6 haloalkyl, carboxyl, C3-7 cycloalkyl, mono- or disubstituted aminocarbonyl optional, methylthio, methylsulfonyl, aryl, - (R7a) nM-R7b, Het1 and Het2; where optional substituents on any amino function are independently selected from R5 and -A-R6; and in (2) a nitrogen atom if present, by hydroxy or -A-R6; A is C1-6 alkanediyl, -C (= O) -, -C (= S) -, -S (= O) 2-, C1-6 alkanediyl -C (= O) -, C1-6 alkanediyl -C (= S) - or C1-6 alkanediyl -S (= O) 2; where for those groups containing a C1-6 alkanediyl portion, the C1-6 alkanediyl portion is attached to the amino group; R5 is hydroxy, C1-6 alkyl, Het1 C1-6 alkyl, amino- C1-6 alkyl where the amino group may be mono- or optionally substituted with C1-4 alkyl; R6 is hydrogen, C1-6 alkyloxy, Het1, Het1 oxy, Het2 oxy, aryl, aryloxy or amino; and, in the case where -A- is different from C1-6 alkanediyl, then, R6 can also be C1-6 alkyl, Het1 C1-4 alkyl, Het1 C1-4 oxyalkyl, Het2 C1-4 alkyl, Het2 C1 oxyalkyl -4, C1-4 arylalkyl, C1-4 aryloxyalkyl or C1-4 aminoalkyl; where each of the amino groups in the definition of R6 may be optionally substituted with one or more substituents selected from C1-4 alkyl, C1-4 alkylcarbonyl, C1-4 alkyloxycarbonyl, aryl, arylcarbonyl, aryloxycarbonyl, Het1, Het2, C1-4 arylalkyl, Het1 C1-4 alkyl or Het2 C1-4 alkyl; R7a is C1-8 alkanediyl optionally substituted by one or more substituents selected from halogen, C1-4 alkylcarbonyl, C1-4 alkyloxycarbonyl, aryl, arylcarbonyl, aryloxycarbonyl, Het1 or Het2; R7b is C1-8 alkyl, optionally substituted with one or more substituents selected from halogen, C1-4 alkylcarbonyl, C1-4 alkyloxycarbonyl, aryl, arylcarbonyl, aryloxycarbonyl, Het1 or Het2; M is defined as -C (= O) -, -OC (= O) -, -C (= O) -O-, -CH2CHOH-, -CHOH-CH2-, -NR8-C (= O) -, - (C = O) -NR8-, -S (= O) 2-, -O-, -S-, -OS (= O) 2-, -S (= O) 2-O-, -NR8- S (= O) 2 or -S (= O) 2-R8-; n is 0 or 1. Manufacture of medicaments as inhibitors of the broad-spectrum HIV protease, the preparation processes, as well as the pharmaceutical compositions comprising them, with another antiretroviral agent. |
| priorityDate | 2001-12-21-04:00^^<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: 84.