http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2559273-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-48 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K45-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-46 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 |
| filingDate | 2001-05-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2016-02-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_23da23cc5f6b0fd065a1d7704b76836d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_39c877cd5f3e3d1693817ca5555b717a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8ea1b420cb8f38ead140ed465124a0bc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2b054059f52cf27f56b8162f897ad71e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c993519c4cc61aaa2920228e533f50eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f579a68b8ca43d1c80be69d454c7e4bb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d862e1070f6b798631a5f63a3fc969e5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_365d6c008ac0e8dce16ca0477eba79ba http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5ef7647e0b98b44dd42f7c98bcb3e043 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fd353bc9b009350567061c9d0ce4b4a2 |
| publicationDate | 2016-02-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2559273-T3 |
| titleOfInvention | Pyrimidine prodrugs that inhibit HIV replication |
| abstract | A compound of formula (A1) (A2) N-R1 (I) a form of N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R1 is -S (> = O) -R8; -S (> = O) 2-R8; C1-6alkyl-oxycarbonyl-C1-6alkyl-carbonyl; hydroxycarbonyl-C1-6alkylcarbonyl; aryl1-C1-6alkyl-oxycarbonyl-C1-6alkyl-carbonyl; Het1-C1-6alkyl-oxycarbonyl-C1-6alkyl-carbonyl; R9R10N-C1-6-alkyl-oxycarbonyl-C1-6-alkyl-carbonyl; (A1) (A2) N- is the covalently linked form of the corresponding intermediate of formula (A1) (A2) NH, wherein said intermediate of formula (A1) (A2) NH is a pyrimidine of formula ** Formula ** an N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, in which -a1> = a2-a3> = a4- represents a bivalent radical of formula -CH> = CH- CH> = CH- (a-1); -N> = CH-CH> = CH- (a-2); -N> = CH-N> = CH- (a-3); -N> = CH-CH> = N- (a-4); -N> = N-CH> = CH- (a-5); n is 0, 1, 2, 3 or 4; and in the case that -a1> = a2-a3> = a4- is (a-1), then n can also be 5; each R2 is independently hydroxy, halo, C1-6 alkyl optionally substituted with cyano or -C (> = O) R6, C3-7 cycloalkyl, C2-6 alkenyl optionally substituted with one or more halogen or cyano atoms, C2-6alkynyl optionally substituted with one or more halogen or cyano atoms, C1-6alkyl-oxy, C1-6alkyl-oxycarbonyl, carboxyl, cyano, aminocarbonyl, nitro, amino, mono- or di (C1-6alkyl ) amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S (> = O) pR6, -NH-S (> = O) pR6, -C (> = O) R6, -NHC (> = O) H, -C ( > = O) NHNH2, -NHC (> = O) R6, -C (> = NH) R6 or a radical of the formula in which each A1 is independently N, CH or CR6; and A2 is NH, O, S, or NR6; L is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-7 cycloalkyl, wherein each of said groups may be substituted with one or two substituents independently selected from * C3-cycloalkyl 7, * indolyl or isoindolyl, each optionally substituted with one, two, three or four substituents each independently selected from halo, C1-6 alkyl, hydroxy, C1-6 alkyl-oxy, cyano, aminocarbonyl, nitro, amino, polyhalomethyl, polyhalomethyloxy and C1-6-alkyl-carbonyl, * phenyl, pyridyl, pyrimidinyl, pyrazinyl or pyridazinyl, in which each of said aromatic rings can be optionally substituted with one, two, three, four or five substituents each independently selected of the substituents defined for R2; or L is -X1-R3 or -X2-Alk-R11 where Alk is C1-4 alkane-diyl; R3 and R11 are each independently phenyl, pyridyl, pyrimidinyl, pyrazinyl, or pyridazinyl, wherein each of said aromatic rings may be optionally substituted with one, two, three, four, or five substituents each independently selected from substituents defined in R2; and X1 and X2 are each independently -NR7-, -NH-NH-, -N> = N-, -O-, -C (> = O) -, -CHOH-, -S-, -S (> = O) - or -S (> = O) 2-; Q represents hydrogen, C1-6alkyl, halo, polyhalo-C1-6alkyl or -NR4R5; and R4 and R5 are each independently selected from hydrogen, hydroxy, C1-12 alkyl, C1-12 alkyl-oxy, C1-12 alkylcarbonyl, C1-12 alkyl-oxycarbonyl, C1-12 alkylthiocarbonyl, aryl, amino, mono- or di (C1-12alkyl) amino, mono- or di (C1-12alkyl) aminocarbonyl, in which each of the aforementioned C1-12alkyl groups can be optionally and each individually substituted with one or two substituents each independently selected from hydroxy, C1-6-alkyl-oxy, hydroxy-C1-6-alkyl-oxy, carboxyl, C1-6-alkyl-oxycarbonyl, cyano, amino, imino, mono- or di (C1- alkyl 6) amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S (> = O) pR12, -NH-S (> = O) pR12, - C (> = O) R12, -NHC (> = O) H, -C (> = O) NHNH2, -NHC (> = O) R12, -C (> = NH) R12, aryl and Het; or R4 and R5, taken together, can form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di (C1-12alkyl) aminoalkane C1-4-diyl; R6 is methyl, amino, mono- or dimethylamino or polyhalomethyl; R7 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyl-oxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyl oxycarbonyl, C 1-6 alkyl carbonyloxy; C1-6alkyl-oxy-C1-6alkyl-carbonyl substituted with C1-6alkyl-oxycarbonyl; R8 is C1-6 alkyl, aryl1 or Het1; R9 and R10 are each independently selected from hydrogen, C1-4alkyl, amino-C1-4alkyl, mono- or di (C1-4alkyl) amino-C1-4alkyl; or R9 and R10 are taken together to form a bivalent radical of formula -CH2-CH2-Z-CH2-CH2-, where Z O, NR13, CH2, or a direct bond; R12 is methyl, amino, mono- or dimethylamino or polyhalomethyl; R13 is hydrogen, C1-4alkyl, amino-C1-4alkyl, mono- or di (C1-4alkyl) amino-C1-4alkyl; R14 is methyl, amino, mono- or dimethylamino or polyhalomethyl; Y represents hydrogen, hydroxy, halo, C1-6 alkyl, C3-7 cycloalkyl, C2-6 alkenyl optionally substituted with one or more halogen atoms, C2-6 alkynyl optionally substituted with one or more halogen atoms, C1-6alkyl substituted with cyano or -C (> = O) R14, C1-6alkyl-oxy, C1-6alkyl-oxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di (C1-6alkyl) amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S (> = O) pR14, -NH-S (> = O) pR14, -C (> = O) R14, -NHC (> = O) H, -C (> = O) NHNH2, -NHC (> = O) R14, -C (> = NH) R14 or aryl; p is 1 or 2. |
| priorityDate | 2000-05-08-04:00^^<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: 313.