http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-040346-A2
Outgoing Links
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| filingDate | 2003-06-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-03-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-040346-A2 |
| titleOfInvention | INTERMEDIARY COMPOUNDS FOR THE SYNTHESIS OF BENZAMIDO-PIPERIDINAS |
| abstract | A compound of the formula (1), where: Q is C = NH, C = CH2, C = S, SO or SO2; each of each of Y and Z is N or CH, with the proviso that Y and Z cannot be both N; W is a bonding group of a carbon (ie, methylene) or a saturated or unsaturated bonding group of two or three carbons, where each of the above groups W may be optionally substituted with a substituent R7 or two substituents R7 and R6, or W is a bonding group of a carbon that forms, together with a 2, 3, 4 or 5 carbon chain, a 3, 4, 5 or 6 member spiro ring, respectively; or W is a bonding group of a saturated chain of two carbons that forms, together with a separate chain of 1, 2 or 3 carbons, a condensed ring of 3, 4 or 5 members respectively; or W is a binding group of a saturated chain of two carbons, where one of the two carbons of the chain forms, together with a separate chain of 2, 3, 4 or 5 carbons, a 3, 4, 5 spiro ring or 6 members, respectively; R5 and R8 are independently selected from hydrogen, -SO-C1-6 alkyl, -SO2-C1-6 alkyl, -SO-aryl, -SO2-aryl, CF3, halo, phenyl, phenyl-alkyl (C1-2) hydroxy, aryloxy, heteroaryloxy, pyridyl, tetrazolyl, oxazolyl, thiazolyl, (C1-6) alkoxy optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, (C1-6) alkyl optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, and (C1-6) alkyl optionally substituted with one or more substituents, preferably with zero to two substituents selected, independently, from hydroxy, oxo, alkoxy (C1-6), phenyl-C1-3 alkoxy, phenyl, cyano, chlorine, bromine, iodine, NR9R10, NR9COR10, NR9CO2R10, CONR9R10, COR9, and CO2R9; R6 and R7 are independently selected from -SO-C1-6 alkyl, -SO2-C1-6 alkyl, -SO-aryl, -SO2-aryl, CF3, halo, phenyl-C1-2 alkyl ), hydroxy, aryloxy, heteroaryloxy, pyridyl, tetrazolyl, oxazolyl, thiazolyl, (C1-6) alkoxy optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, (C1-6) alkyl optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, and (C1-6) alkyl optionally substituted with one or more substituents, preferably with zero to two substituents selected, independently, from hydroxy, oxo, (C1-) alkoxy 6), phenyl (C1-3) alkoxy, phenyl, cyano, chloro, bromine, iodine, NR9R10, NR9COR10, NR9CO2R10, CONR9R10, COR9 and CO2R9; each R9 and each R10 are independently selected from hydrogen, (C1-6) alkyl, hydroxy (C1-6) alkyl, phenyl and CF3; and wherein the phenyl groups in the definition of R5, R6, R7 and R8 and the phenyl-C1-2 alkyl radical in the definition of R5, R6, R7 and R8 may optionally be substituted with one or more substituents preferably with zero to two substituents, which are independently selected from halo, hydroxy, (C1-6) alkoxy optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, (C1-6) alkyl optionally substituted with one to seven fluorine atoms, preferably zero to three fluorine atoms; and R14 is hydrogen, (C1-6) alkyl or CF3; with the proviso that: (a) R8 cannot be halo, hydroxy, cyano, aryloxy, heteroaryloxy, substituted or unsubstituted (C1-6) alkoxy or methyl substituted with 1-3 fluorine atoms; or one of its pharmaceutically acceptable salts. A compound of the formula T-NH2 is described where T-NH2 is a residue of formula (2) and where p is zero, one or two; R3 is selected from hydrogen, COR9, CO2R9, optionally substituted phenyl, optionally substituted heterocyclic rings, and optionally substituted (C1-8) alkyl where one of the CH2 groups of said (C1-8) alkyl may be optionally replaced with a sulfur, oxygen or carbonyl group and wherein said (C1-8) alkyl may be optionally substituted with one to three substituents, preferably with zero substituents or a substituent, independently selected from hydroxy, oxo, phenyl (C1-3) alkoxy, phenyl, cyano , halo, optionally substituted heterocyclic rings, NR9COR10, NR9CO2R10, CONR9R10, COR9, CO2R9, NR9R10, and (C1-6) alkoxy optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms; and wherein the heterocyclic rings of R3 and the substituent heterocyclic rings on the alkyl groups of R3 are independently selected from the saturated or unsaturated monocyclic rings of 3 to 7 members containing 1 to 4 heteroatoms in the ring, and saturated bicyclic ring or unsaturated 8 to 12 members containing 1 to 4 ring heteroatoms, wherein said heteroatoms are independently selected from oxygen, nitrogen and sulfur with the proviso that there cannot be two adjacent oxygen atoms in the ring or two adjacent sulfur atoms in the ring in any of the monocyclic or bicyclic heterocyclic rings and with the proviso that the heterocyclic rings formed by NR9R10 or CONR9R10 must contain at least one nitrogen atom; and wherein the heterocyclic rings of R3 and the heterocyclic rings substituents on the alkyl groups of R3 may be optionally substituted with one or more substituents, preferably with zero, one or two substituents, independently selected, from oxo, hydroxy, thioxo, halo, cyano , phenyl, (CH2) mNR9R10, NR9COR10 (CH2) mOR9, where m is zero, one or two and (C1-6) alkyl optionally substituted with one or more substituents, preferably with zero to two substituents, independently selected from halo, CF3 , methoxy and phenyl; and where the phenyl groups of R3 and phenyl substituents in the R3 alkyl groups may be optionally substituted with one or more substituents, preferably with zero to two substituents, independently selected from the group consisting of halo, cyano, nitro, CF3, (CH2) mNR9R10, where m is zero, one or two, NR9COR10, NR9CO2R10, CONR9R10, CO2NR9R10, COR9, CO2R9, alkyl (C1-6) optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, alkoxy ( C1-6) optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, and (C2-6) alkenyl optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms; each of R1, R2, R11, R12 and R13 is independently selected from hydrogen and (C1-6) alkyl optionally substituted with one or more substituents, preferably with zero, one or two substituents, which are independently selected from hydroxy, oxo, (C1-6) alkoxy and cyano; or R1 and R2, together with the carbon atoms to which they are attached, or R2 and R3, together with the carbon and nitrogen to which they are attached, respectively, form a saturated 5- or 6-membered heterocyclic ring containing one or two heteroatoms that are independently selected from nitrogen, oxygen and sulfur, with the proviso that said ring cannot contain two adjacent oxygen atoms or two adjacent sulfur atoms; or R1 and R2, together with the carbons to which they are attached, form a saturated or unsaturated carbocyclic ring of 5 or 6 members, and wherein said heterocyclic and carbocyclic rings formed by R1 and R2 or by R2 and R3, may be substituted with one or more substituents, preferably with zero substituents or a substituent, independently selected from halo, oxo, NR9R10, (C1-6) alkyl optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms and (C1 alkoxy) -6) optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms; or R12 and R13, together with the carbon atoms to which they are attached, form a saturated 5- or 6-membered heterocyclic ring containing one or two heteroatoms that are independently selected from nitrogen, oxygen and sulfur, with the condition of that said ring cannot contain two adjacent oxygen atoms or two adjacent sulfur atoms, or R12 and R13, together with the carbons to which they are attached, form a saturated or unsaturated carbocyclic ring of 5 or 6 members, and wherein said rings heterocyclic and carbocyclic formed by R12 and R13, may be substituted with one or more substituents, preferably with zero substituents or a substituent, independently selected from NR9R10, halo, phenyl-S-, phenyl-SO-, phenyl-SO2-, oxo, (C1-6) alkoxy optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, and (C1-6) alkyl optionally substituted with one to seven fluorine atoms, preferably mind with zero to three fluorine atoms; with the proviso that no more than one of R1 and R2, R2 and R3, and R12 and R13 can form a ring; R4 is selected from phenyl, 2-, 3- or 4-pyridyl, 2- or 3-thienyl, and pyrimidyl, where R4 may be optionally substituted with one or more substituents, preferably with zero substituents or a substituent, independently selected, between halo, (C1-6) alkyl optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms, (C1-6) alkoxy optionally substituted with one to seven fluorine atoms, preferably with zero to three atoms of fluorine, and (C2-6) alkenyl optionally substituted with one to seven fluorine atoms, preferably with zero to three fluorine atoms; each R9 and each R10 are independently selected from hydrogen, (C1-6) alkyl, hydroxy (C1-6) alkyl, phenyl and CF3; or R9 and R10 when R3 is NR9R10 or CONR9R10, they can form, together with the nitrogen to which they are attached, an optionally substituted heterocyclic ring containing at least one nitrogen atom; or one of its pharmaceutically acceptable salts. A method for treatment |
| priorityDate | 2000-04-10-04:00^^<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: 146.