Patent ID: 6410566
Filing Date: 2002-06-25
Classification: A61K,C07D

Abstract:
A compound of the formula (I) below: a pharmaceutically acceptable acid addition salt thereof or a pharmaceutically acceptable C1-C6 alkyl addition salt thereof,wherein R1 is a phenyl group, a C3-C8 cycloalkyl group, or an aromatic heterocyclic group having 1-3 heteroatoms selected from the group consisting of an oxygen atom, a sulfur atom, a nitrogen atom, or a combination thereof, in which the phenyl or aromatic heterocyclic group may be condensed with a benzene ring or an aromatic heterocyclic group having 1-3 heteroatoms selected from the group consisting of an oxygen atom, a sulfur atom, a nitrogen atom, or a combination thereof, to form a condensed ring, and the phenyl group, C3-C8 cycloalkyl group, aromatic heterocyclic group, or condensed ring may be substituted with one or more of a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a carbamoyl group, a C1-C6 alkyl group, a C3-C8 cycloalkyl group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a C3-C5 alkylene group, a C2-C4 alkylenoxy group, a C1-C3 alkylenedioxy group, a phenyl group, a phenoxy group, a phenylthio group, a benzyl group, a benzyloxy group, a benzoylamino group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a C2-C7 alkanoyloxy group, a C2-C7 alkanoylamino group, a C2-C7 N-alkylcarbamoyl group, a C4-C9 N-cycloalkylcarbamoyl group, a C1-C6 alkylsulfonyl group, a C3-C8 (alkoxycarbonyl)methyl group, a N-phenylcarbamoyl group, a piperidinocarbonyl group, a morpholinocarbonyl group, a 1-pyrrolidinylcarbonyl group, a divalent group represented by the formula: â€”NH(C&boxH;O)Oâ€”, a divalent group represented by the formula: â€”NH(C&boxH;S)Oâ€”, an amino group, a mono(C1-C6 alkyl)amino group, or a di(C1-C6 alkyl)amino group, wherein the substituent for the phenyl group, C3-C8 cycloalkyl group, aromatic heterocyclic group, or condensed ring is optionally substituted with one or more of a halogen atom, a hydroxy group, an amino group, atrifluoromethyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group; R2 is a hydrogen atom, a C1-C6 alkyl group, a C2-C7 alkoxycarbonyl group, a hydroxy group, or a phenyl group, in which the C1-C6 alkyl or phenyl group may be substituted with one or more of a halogen atom, a hydroxy group, a C1-C6 alkyl croup, or a C1-C6 alkoxy group, and when j=0, R2 is not a hydroxy group; j represents an integer of 0-2; k represents an integer of 0-2; m represents an integer of 2-4, with the proviso that the total sum of k and m is 4; n represents 0 or 1; and further with the proviso that when k=2, m=2, n=0 and R1 is an indolyl group, then j=0 and R2 is a hydrogen atom; R3 is a hydrogen atom or a C1-C6 alkyl group optionally substituted with one or two phenyl groups each of which may be substituted with one or more of a halogen atom, a hydroxy group, a C1-C6 alkyl group, or a C1-C6 alkoxy group; R4 and R5 are the same or different from each other and are a hydrogen atom, a hydroxy group, a phenyl group, or a C1-C6 alkyl group, in which the C1-C6 alkyl group is optionally substituted with one or more of a halogen atom, a hydroxy group, a cyano group, a nitro group, a carboxy group, a carbamoyl group, a mercapto group, a guanidino group, a C3-C8 cycloalkyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a phenyl group optionally substituted with one or more of a halogen atom, a hydroxy group, a C1-C6 alkyl group, a C1-C6 alkoxy group, or a benzyloxy group, a phenoxy group, a benzyloxy group, a benzyloxycarbonyl group, a C2-C7 alkanoyl group, a C2-C7, alkoxycarbonyl group, a C2-C7 alkanoyloxy group, a C2-C7 alkanoylamino group, a C2-C7 N-alkylcarbamoyl group, a C1-C6 alkylsulfonyl group, an amino group, a mono(C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group, or an aromatic heterocyclic group having 1-3 of heteroatoms selected from the group consisting of an oxygen atom, a sulfur atom, a nitrogen atom, or a combination thereof and optionally condensed with benzene ring, with the proviso that when one of R4 and R5 is a hydrogen atom, the other is not an isobutyl group, or R4 and R5 taken together form a 3 to 6 membered cyclic hydrocarbon; p represents 0 or 1; q represents 0 or 1; G is a group represented by â€”COâ€”, â€”SO2â€”, â€”COâ€”Oâ€”, â€”NR7â€”COâ€”, â€”COâ€”NR7â€”, â€”NHâ€”COâ€”NHâ€”, â€”NHâ€”CSâ€”NHâ€”, â€”NR7â€”SO2â€”, â€”SO2â€”NR7â€”, â€”NHâ€”COâ€”Oâ€”, or â€”Oâ€”COâ€”NHâ€”, wherein R7 is a hydrogen atom or a C1-C6 alkyl group, or R7 taken together with R5 represents C2-C5 alkylene group; R6 is a phenyl group, a C3-C8 cycloalkyl group, a C3-C8 cycloalkenyl group, a benzyl group, or an aromatic heterocyclic group having 1-3 heteroatoms selected from the group consisting of an oxygen atom, a sulfur atom, a nitrogen atom, or a combination thereof, in which the phenyl, benzyl, or aromatic heterocyclic group may be condensed with a benzene ring or an aromatic heterocyclic group having 1-3 heteroatoms selected from the group consisting of an oxygen atom, a sulfur atom, a nitrogen atom, or a combination thereof, to form a condensed ring, and the phenyl group, C3-C8 cycloalkyl group, C3-C8 cycloalkenyl group, benzyl group, aromatic heterocyclic group, or condensed ring may be substituted with one or more of a halogen atom, a hydroxy group, a mercapto group, a cyano group, a nitro group, a thiocyanato group, a carboxy group, a carbamoyl group, a trifluoromethyl group, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C3-C8 cycloalkyloxy group, a C1C6 alkylthio group, a C1-C3 alkylenedioxy group, a phenyl group, a phenoxy group, a phenylamino group, a benzyl group, a benzoyl group, a phenylsulfinyl group, a phenylsufonyl group, a 3-phenylureido group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a C2-C7, alkanoyloxy group, a C2-C7 alkanoylamino group, a C2-C7 N-alkylcarbamoyl group, a C1-C6 alkylsulfonyl group, a phenylcarbamoyl group, a N,N-di(C1-C6 alkyl) sulfamoyl group, an amino group, a mono(C1-C6 alkyl)amino group, a di(C1-C6 alkyl)amino group, a benzylamino group, a C2-C7 (alkoxycarbonyl)amino group, a C1-C6 (alkylsulfonyl)amino group, or a bis(C1-C6 alkylsulfonyl)amino group, wherein the substituent for the phenyl group, C3-C8 cycloalkyl group, C3-C8 cycloalkenyl group, benzyl group, aromatic heterocyclic group, or condensed ring is optionally substituted with one or more of a halogen atom, a cyano group, a hydroxy group, an amino group, a trifluoromethyl group, a C1-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a mono(C1-C6 alkyl)amino group, or a di(C1-C6 alkyl)amino group with the proviso that when k=2, m=2, n=0, and R1 is an unsubstituted phenyl group, then 1) C1-C6 alkyl group as a substituent for the phenyl group, C3-C8 cycloalkyl group, C3-C8 cycloalkenyl group, benzyl group, aromatic heterocyclic group, or condensed ring in R6 is not substituted with amino group, and 2) R6 is not a benzyl group.