http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-038240-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_27a71ddaaa2f5a8c228fc6cb3f3b3098 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5383 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-00 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/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D513-04 |
| filingDate | 2003-01-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-038240-A1 |
| titleOfInvention | PIPERIDINE COMPOUND, USE OF THE SAME FOR THE MANUFACTURE OF A MEDICINAL PRODUCT, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND PROCEDURE FOR PREPARATION |
| abstract | Use of a compound of the formula (1) for the manufacture of a medicament useful in the treatment of bacterial infections in mammals, particularly in humans; pharmaceutical composition comprising said compound together with a pharmaceutically acceptable carrier; and procedure to prepare it. Claim 1: A piperidine compound, or one of its pharmaceutically acceptable derivatives, characterized in that it is represented by the formula (1), wherein: one of Z1, Z2, Z3, Z4 and Z5 is N, one is CR1a and the the remaining are CH, or one of Z1, Z2, Z3, Z4 and Z5 is CR1a and the remaining are CH; R1 and R1a are independently hydrogen, 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 C1-6 alkyl groups, acyl or C1-6 alkylsulfonyl, CONH2, hydroxy, C1-6 alkylthio, heterocyclylthio, heterocyclyloxy, arylthio, aryloxy, acylthio, acyloxy or C1-6 alkylsulfonyloxy, C1-6 alkyl substituted with C1-6 alkoxy, halogen, C1-6 alkyl, alkylthio C1-6, trifluoromethyl, trifluoromethoxy, nitro, azido, acyl, acyloxy, acylthio, C1-6 alkylsulfonyl, C1-6 alkylsulfoxide, arylsulfonyl, arylsulfoxide or an amino group, piperidyl, guanidino or amidino optionally N-substituted with one or two groups C1-6 alkyl, acyl or C1-6 alkylsulfonyl; or when Z5 is CR1a, R1a may instead be cyano, hydroxymethyl or carboxy; or R1 and R1a in adjacent positions can together form ethylenedioxy; with the proviso that when neither Z1, Z2, Z3, Z4 and Z5 is N, then R1 is not hydrogen; R2 is hydrogen, 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, C1-4alkyl alkyl , C2-4 alkenyloxy carbonyl, C2-4 alkenyl carbonyl, aminocarbonyl in which the amino group is optionally substituted with hydroxy, C1-4 alkyl, C1-4 hydroxyalkyl, C1-4 alkylcarbonyl, C2-4 alkenyl, C1- alkylsulfonyl 4, trifluoromethylsulfonyl, C2-4 alkenylsulfonyl, C1-4 alkoxycarbonyl, C1-4 alkylcarbonyl, C2-4 alkenyloxycarbonyl or C2-4 alkenyl carbonyl, cyano, tetrazolyl, 2-oxo-oxazolidinyl optionally substituted with R10, 3-hydroxy -3-cyclobutene-1,2-dion-4-yl, 2,4-thiazolidinadion-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 alkylthio, trifluoromethyl, hydroxy optionally substituted with C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxycarbonyl, C1-4 alkylcarbonyl, C2-4 alkenyloxycarbonyl, C2-4 alkenyl carbonyl, oxo, C1-4 alkylsulfonyl, C2-4 alkenylsulfonyl, or C2-4 alkyl aminosulfonyl in which the amino group is optionally substituted with C1-4 alkyl or C2-4 alkenyl; R3 is in position 2, 3 or 4 and is trifluoromethyl or is in position 2 and is oxo; or R3 is in position 3 and is fluorine or amino, in which the amino group is optionally substituted with: hydroxy, C1-6 alkyl sulfonyl, trifluoromethylsulfonyl, C2-6 alkenyl sulfonyl, C1-6 carbonyl alkyl, C2-6 alkenyl carbonyl, C 1-6 alkoxy carbonyl, C 2-6 alkenyloxy carbonyl, C 1-6 alkyl, or C 2-6 alkenyl, wherein a C 1-6 alkyl or C 2-6 alkenyl moiety may be optionally substituted with up to 2 independently selected R 12 groups of: halogen, C1-6 alkylthio, trifluoromethyl, cyano, carboxy, tetrazolyl, 2-oxo-oxazolidinyl, 3-hydroxy-3-cyclobutene-1,2-dion-4-yl, 2,4-thiazolidinedion-5-yl , tetrazol-5-ylaminocarbonyl, 1,2,4-triazol-5-yl optionally substituted with R10, 5-oxo-1,2,4-oxadiazol-3-yl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl , C 2-6 alkenyloxy carbonyl, C 2-6 alkenyl carbonyl, hydroxy optionally substituted with C 1-6 alkyl, C 2-6 alkenyl, C 1-6 alkylcarbonyl, C 1-6 alkenyl carbonyl or aminocarbonyl, wherein the amino group it is optionally substituted with C1-6 alkyl, C2-6 alkenyl, amino optionally mono- or disubstituted with C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, C2-6 alkenyloxycarbonyl, C2-6 alkenylcarbonyl, C1-6 alkyl, C2-6 alkenyl, C1-6 alkylsulfonyl, C2-6 alkenylsulfonyl or aminocarbonyl wherein the amino group is optionally substituted with C1-6 alkyl or C2-6 alkenyl; furthermore, when R3 is disubstituted with a substituent containing hydroxy or amino and substituent containing carboxy, these may together form a cyclic ester or amide bond, respectively; R4 is a group U-R5 where: U is selected from CO, SO2 and CH2 and R5 is an optionally substituted bicyclic or heterocyclic carbocyclic ring system, formula (2) containing up to 4 heteroatoms in each ring in which the ring ( a) is aromatic and ring (b) is non aromatic; X1 is C or N; X2 is N, NR13, O, S (O) x or CR14; X3 and X5 are N or C independently; Y1 is a linker group of 0 to 4 atoms, each of which is independently selected from N, NR13, O, S (O) x, CO and CR14; Y2 is a linking group of 2 to 6 atoms, each atom of Y2 being independently selected from N, NR13, O, S (O) x, CO, CR14 and CR14R15; each R14 and R15 is independently selected from: H, C1-4 alkylthio, halo, C1-4 carboxyalkyl, C1-4 haloalkoxy, C1-4 haloalkyl, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxycarbonyl, formyl , C1-4 alkylcarbonyl, C2-4 alkenyloxycarbonyl, C2-4 alkenylcarbonyl, C1-4 alkylcarbonyloxy, C1-4 alkyl C1-4 alkoxycarbonyl, hydroxy, hydroxy C1-4alkyl, C1-4 mercaptoalkyl, C1- alkoxy 4, trifluoromethoxy, nitro, cyano, carboxy, amino or aminocarbonyl optionally substituted as the corresponding substituents in R3, C1-4 alkylsulfonyl, C2-4 alkenylsulfonyl, or aminosulfonyl in which the amino group is optionally mono or disubstituted with C1- alkyl 4 or C2-4 alkenyl, aryl, arylC 1-4 alkyl, arylC 1-4 alkoxy; each R13 is independently H, trifluoromethyl, C1-4 alkyl optionally substituted with hydroxy, C1-6 alkoxy, C1-6 alkylthio, halo or trifluoromethyl, C2-4 alkenyl, aryl, aryl-C1-4 alkyl, arylcarbonyl, heteroarylcarbonyl, alkoxy C1-4 carbonyl, C1-4 alkyl carbonyl, formyl, C1-6 alkylsulfonyl, or aminocarbonyl in which the amino group is optionally substituted with C1-4 alkoxycarbonyl, C1-4alkyl alkyl, C2-4 alkenyloxycarbonyl, C2 alkenyl -4 carbonyl, C1-4 alkyl or C2-4 alkenyl and optionally more substituted with C1-4 alkyl or C2-4 alkenyl; each x is independently 0, 1 or 2; n is 0 and AB is NR11CO, CO-CR8R9, CR6R7-CO, NHR11SO2, CR6R7-SO2 or CR6R7-CR8R9, with the proviso that R8 and R9 are not optionally hydroxy or amino substituted and R6 and R8 do not represent a bond: or n is 1 and AB is NR11CO, CO-CR8R9, CR6R7-CO, NR11SO2, CONR11, CR6R7-CR8R9, O-CR8R9 or NR11-CR8R9; each of R6, R7, R8 and R9 is independently selected from: hydrogen, C1-6 alkoxy, C1-6 alkylthio, halo, trifluoromethyl, azido, C1-6 alkyl, C2-6 alkenyl, C1-6 alkoxycarbonyl, alkyl C1-6 carbonyl, C2-6 alkenyloxycarbonyl, C2-6 alkenylcarbonyl, hydroxy, amino or aminocarbonyl optionally substituted on the basis of the corresponding substituents on R3, C2-6 alkylsulfonyl, C2-6 alkenylsulfonyl, or aminosulfonyl in which the group amino is optionally substituted with C1-6 alkyl or C2-6 alkenyl; or when n = 1, R6 and R8 together represent a bond and R7 and R9 are as defined above; or R6 and R7 or R8 and R9 together represent oxo; R10 is selected from C1-4 alkyl, C2-4 alkenyl and aryl, any of which may be optionally substituted with a R12 group as defined above, carboxy, aminocarbonyl, wherein the amino group is optionally substituted with hydroxy, alkyl C1-6, C2-6 alkenyl, C1-6 alkylsulfonyl, trifluoromethylsulfonyl, C2-6 alkenyl sulfonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyl, C2-6 alkenyloxycarbonyl or C2-6 alkenyl carbonyl optionally substituted with alkyl C1-6 or C2-6 alkenyl; and R 11 is hydrogen, trifluoromethyl, C 1-6 alkyl, C 2-6 alkenyl, C 1-6 alkoxycarbonyl, C 1-6 alkylcarbonyl, or aminocarbonyl in which the amino group is optionally further substituted by C 1-6 alkoxycarbonyl, C 1-6 alkyl -6 carbonyl or C2-6 alkenyloxy carbonyl, C1-6 alkyl or C2-6 alkenyl and optionally further substituted with C1-6 alkyl or C2-6 alkenyl; or in which one of R3 and R6, R7, R8 or R9 contains a carboxy group and the other contains a hydroxy or amino group can together form a cyclic ester or an amide bond. |
| priorityDate | 2002-01-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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