http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-038172-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c2b9dc89cc4ba060cc73bbf0c90bbb78 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5383 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-538 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-542 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5415 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-498 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 |
| filingDate | 2002-05-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-038172-A1 |
| titleOfInvention | CYCLLOHEXAN AND CYCLLOHEXENE COMPOUND, ITS USE TO PREPARE A PHARMACEUTICAL COMPOSITION, SUCH PHARMACEUTICAL COMPOSITION, PROCEDURE TO PREPARE THE COMPOUND AND INTERMEDIATE COMPOUNDS IN SUCH PROCEDURE |
| abstract | Compound of cyclohexane and cyclohexene of the formula (1) or a pharmaceutically acceptable derivative thereof, wherein: one of Z1, Z2, Z3, Z4 and Z5 is N, one is CR1a and the rest is CH, or one of Z1. Z2, Z3, Z4 and Z5 is CR1a and the rest are CH, Rv and Rw are H or Rv and Rw together are a link; R1 and R1a are independently selected from the group consisting of H, hydroxy, C1-6 alkoxy optionally substituted with C1-6 alkoxy, amino, piperidyl, guanidino or amidino any of which is optionally N-substituted with one or two C1-alkyl groups 6, acyl or (C1-6) alkyl sulfonyl, CONH2, hydroxy, (C1-6) alkyl thio, heterocyclyl, heterocyclyloxy, arylthio, aryloxy, acylthio, acyloxy or (C1-6) alkyl sulfonyloxy; (C1-6) alkyl substituted with C1-6 alkoxy; halogen; C1-6 alkyl, (C1-6) alkyl thio; trifluoromethyl, nitro, azido, acyl, acyloxy, acylthio, (C1-6) alkyl sulfonyl, (C1-6) alkyl sulfoxide; arylsulfonyl; arylsulfoxide or an amino group; Piperidyl, guanidino or amidino optionally N-substituted with one or two (C1-6) alkyl, acyl or (C1-6) sulfonyl groups, or when Z1 is CR1a, R1 and R1a together may represent (C1-2) dioxy alkylene , or when Z5 is CR1a, R1a may be instead of cyano, hydroxymethyl or carboxy, with the proviso that, when Z1, Z2, Z3, Z4 and Z5 are CR1a or CH, then R1 is not H; R2 is H, or C1-4 alkyl or C2-4 alkenyl optionally substituted with 1 to 3 groups selected from: amino optionally substituted with 1 or 2 C1-4 alkyl groups; carboxy; (C1-4) alkoxycarbonyl; (C1-4) alkylcarbonyl; (C2-4) alkenyl oxycarbonyl; (C2-4) alkenyl carbonyl; aminocarbonyl wherein the amino group is optionally substituted with hydroxy, C1-4 alkyl, hydroxy C1-4 alkyl, aminocarbonyl-C1-4 alkyl, C2-4 alkenyl, (C1-4) alkyl sulfonyl, trifluoromethylsulfonyl, alkenyl (C2-4) sulfonyl, (C1-4) alkoxycarbonyl, (C1-4) alkylcarbonyl, (C2-4) alkenyl or oxycarbonyl (C2-4) alkenyl carbonyl; cyano, tetrazolyl; 2-oxo-oxazolidinyl optionally substituted with R10; 3-hydroxy-3-cyclobutene-1,2-dione-4-yl; 2,4-thioazolidinedione-5-yl; tetrazol-5-ylaminocarbonyl; 1,2,4-triazol-5-yl optionally substituted with R10; 5-oxo-1,2,4-oxadiazol-3-yl; halogen; (C1-4) alkyl thio; trifluoromethyl, hydroxy optionally substituted with C1-4 alkyl, C2-4 alkenyl, (C1-4) alkoxycarbonyl, (C1-4) alkylcarbonyl, (C2-4) alkenyl oxycarbonyl, (C2-4) alkenyl carbonyl; oxo; (C1-4) alkyl sulfonyl; (C2-4) alkenyl sulfonyl; or aminosulfonyl wherein the amino group is optionally substituted with C1-4 alkyl or C2-4 alkenyl; R3 is H, or when Rv and Rw are a link, R3 is in position 3 or 4 and when Rv and Rw are not a link, R3 is in position 1, 2, 3 or 4 and R3 is: carboxy; (C1-6) alkoxycarbonyl; aminocarbonyl wherein the amino group is optionally substituted with hydroxy, C1-6 alkyl, hydroxy C1-6 alkyl, aminocarbonyl C1-6 alkyl, C2-6 alkenyl, (C1-6) sulfonyl, trifuoromethylsulfonyl, alkenyl (C2-6) sulfonyl , (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyl, (C2-6) alkynyl or oxycarbonyl (C2-6) carbonyl and also optionally substituted with C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 aminocarbonylalkyl 6 or C2-6 alkenyl; cyano, tetrazolyl; 2-oxo-oxazolidinyl optionally substituted with R10; 3-hydroxy-3-cyclobutene-1,2-dione-4-yl; 2,4-thiazolidinedione-5-yl; tetrazol-5-ylaminocarbonyl; 1,2,4-triazol-5-yl optionally substituted with R10; or 5-oxo-1,2,4-oxadiazol-3-yl; or C1-4 alkyl or ethenyl optionally substituted with any of the groups listed above for R3 and / or 0 to 2 R12 groups independently selected from halogen, (C1-6) alkyl thio; trifluoromethyl; (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyl; (C2-6) alkenyl oxycarbonyl; (C2-6) alkenyl carbonyl; hydroxy optionally substituted with C1-6 alkyl; C2-6 alkenyl, (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyl, (C2-6) alkynyl oxycarbonyl, (C2-6) alkenyl carbonyl or aminocarbonyl wherein the amino group is optionally substituted with C1- alkyl 6; C2-6 alkenyl, (C1-6) alkylcarbonyl or (C2-6) alkenyl carbonyl; amino optionally mono- or di-substituted with (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyl, (C2-6) alkynyl oxycarbonyl, (C2-6) alkenyl carbonyl, C1-6 alkyl, C2-6 alkenyl , (C1-6) alkyl sulfonyl, (C2-6) alkenyl sulfonyl or aminocarbonyl wherein the amino group is optionally substituted with C1-6 alkyl or C2-6 alkenyl; aminocarbonyl wherein the amino group is optionally substituted with C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 aminocarbonylalkyl, C2-6 alkenyl, alkoxy (C1-6) carbonyl, alkyl (C1-6) carbonyl, alkenyl (C2- 6) oxycarbonyl or (C2-6) alkenyl carbonyl and further optionally substituted with C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 aminocarbonylalkyl or C2-6 alkenyl; oxo, (C1-6) alkyl sulfonyl, (C2-6) alkenyl sulfonyl; or aminosulfonyl wherein the amino group is optionally substituted with C1-6 alkyl or C2-6 alkenyl; or hydroxy optionally substituted with C1-6 alkyl, C2-6 alkenyl, (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyl, (C2-6) alkenyl oxycarbonyl, (C2-6) alkenyl carbonyl or aminocarbonyl wherein the amino group is optionally substituted with C1-6 alkyl, C2-6 alkenyl, (C1-6) alkylcarbonyl (C2-6) alkenyl carbonyl; or amino optionally mono- or di-substituted with (C1-6) alkoxycarbonyl, (C1-6) alkylcarbonyl, (C2-6) alkenyl oxycarbonyl, (C2-6) alkenyl carbonyl, C1-6 alkyl, C2- alkenyl 6, (C1-6) alkyl sulfonyl, (C2-6) alkenyl sulfonyl or aminocarbonyl wherein the amino group is optionally substituted with C1-6 alkyl or C2-6 alkenyl, with the proviso that, when R3 is in position 4 is not hydroxyl or optionally substituted amino; furthermore, when R3 is disubstituted with a hydroxy or amino-containing substituent and a carboxy-containing substituent, these together may optionally form an ester or cyclic amide bond, respectively; R10 is selected from C1-4 alkyl and C2-4 alkenyl any of which may be optionally substituted with an R12 group as defined above; carboxy, aminocarbonyl wherein the amino group is optionally substituted with hydroxy, C1-6 alkyl, C2-6 alkenyl, (C1-6) alkyl sulfonyl, trifluoromethylsulfonyl, alkenyl (C2-6) sulfonyl, alkoxy (C1-6) carbonyl, (C1-6) alkylcarbonyl, (C2-6) alkynyl oxycarbonyl or (C2-6) alkynyl carbonyl and further optionally substituted with C1-6 alkyl or C2-6 alkenyl, (C1-6) alkyl sulfonyl; trifluoromethylsulfonyl, (C2-6) alkenyl sulfonyl; (C1-6) alkoxycarbonyl; (C1-6) alkylcarbonyl, (C2-6) alkenyl oxycarbonyl, and (C2-6) alkenyl carbonyl; R4 is a group -CH2-R51 in which R51 is selected from: C4-8 alkyl; C4-8 hydroxyalkyl, (C1-4) alkoxy-(C4-8) alkyl; (C1-4) alkanoyloxy (C4-8) alkyl; (C3-8) cycloalkyl (C4-8) alkyl, hydroxy-, C1-6- alkoxy- or (C1-6) alkanoyloxy (C3-8) -cycloalkyl (C4-8) alkyl, (C4-8) cyanoalkyl; alkenyl (C4-8); (C4-8) alkynyl; tetrahydrofuryl; mono- or di-C 1-6 alkyl-amino C 1-8 alkyl, acylamino C 1-8 alkyl, C 1-6 alkyl- or acyl aminocarbonyl C 1-8 alkyl; mono- or di-C1-6 alkyl-amino (hydroxy) -C4-8 alkyl; or R4 is a group -U-R52 wherein R52 is a bicyclic system of formula (2) of optionally substituted carbocyclic or heterocyclic rings; containing up to 4 heteroatoms in each ring, in which at least one of the rings (a) and (b) is aromatic; X1 is C or N when it is part of an aromatic ring or CR14 when it is part of a non-aromatic ring; X2 is N, NR13, O, S (O) x, CO or CR14 when it is part of an aromatic or non-aromatic ring or it can also be CR14R15 when it is part of a non-aromatic ring; X3u and X5 are independently N or C; Y1 is a linker group of 0 to 4 atoms and each atom thereof is independently selected from N, NR13, O, S (O) x, CO, and CR14 when it is part of an aromatic or non-aromatic ring or can also be CR14R15 when part of a non-aromatic ring; Y2 is a linker group of 0 to 4 atoms, and each atom of Y2 is independently selected from N, NR13, O, S (O) x, CO, and CR14 when it is part of an aromatic or non-aromatic ring or may also be CR14R15 when part of a non-aromatic ring; each of R14 and R15 is independently selected from H, (C1-4) alkyl thio, halo, carboxy-C1-4 alkyl; haloalkoxy (C1-4); haloalkyl (C1-4); C1-4 alkyl; C2-4 alkenyl; (C1-4) alkoxycarbonyl; formyl; (C1-4) alkylcarbonyl; (C2-4) alkenyl oxycarbonyl; (C2-4) alkenyl carbonyl; (C1-4) alkylcarbonyloxy; (C1-4) alkoxycarbonyl (C1-4) alkyl; hydroxy; C1-4 hydroxyalkyl; mercapto-C1-4 alkyl; C1-4 alkoxy; nitro; cyano; carboxy; amino or aminocarbonyl optionally substituted as in the case of the corresponding substituents in R3; (C1-4) alkyl sulfonyl; (C2-4) alkenyl sulfonyl, or aminosulfonyl wherein the amino group is optionally substituted with C1-4 alkyl or C2-4 alkenyl; aryl; C 1-4 aryl alkyl; aryl (C1-4) alkoxy; each R13 is independently H, trifluoromethyl; C1-4 alkyl optionally substituted with hydroxy, carboxy, (C1-6) alkoxycarbonyl, (C1-6) alkoxy, (C1-6) alkyl thio, halo, or trifluoromethyl; C2-4 alkenyl, aryl, aryl (C1-4) alkyl; arylcarbonyl, heteroarylcarbonyl, (C1-4) alkoxycarbonyl; (C1-4) alkylcarbonyl; formyl, (C1-6) alkyl sulfonyl; or aminocarbonyl wherein the amino group is optionally substituted with (C1-4) alkoxycarbonyl, (C1-4) alkylcarbonyl, (C2-4) alkenyl oxycarbonyl, (C2-4) alkenyl carbonyl, C1-4 alkyl or C2 alkenyl -4 and also optionally substituted with C1-4 alkyl or C2-4 alkenyl; each x is independently 0, 1, or 2; U is CO, SO2 or CH2; or R4 is a group -X1a-X2a-X3a-X4a in which: X1a is CH2, CO, or SO2; X2a is CR14aR15a; X3a is NR13a, O, S, SO2 or SR14aR15a; wherein: each of R14a and R15a is independently selected from the groups listed above for R14 and R15, with the proviso that, R14a and R15a on the same C atom are not both selected from optionally substituted hydroxy and amino opium |
| priorityDate | 2001-05-25-04:00^^<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: 57.