Patent ID: 6777427
Filing Date: 2004-08-17
Classification: A61K,A61P,C07D,C07F

Abstract:
A tetrahydroquinoline compound represented by the following formula (I) or pharmacologically acceptable salts thereof: wherein R1 and R2 each independently represent a hydrogen atom, an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, a nitro group, â€”NR5R6 (wherein R5 and R6 each independently represent a hydrogen atom, an alkyl group having 1-9 carbon atoms, a cycloalkyl group having 3-7 carbon atoms, an aralkyl group having 7-9 carbon atoms which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom and a nitro group, an aryl, furyl or pyridyl group which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom and a nitro group, a formyl group, an aliphatic acyl group having 2-5 carbon atoms, an aliphatic acyloxy group having 2-5 carbon atoms, an aromatic acyl group, an alkylsulfonyl group having 1-4 carbon atoms, an arylsulfonyl group, an alkoxycarbonyl group having 2-5 carbon atoms, a hydroxyoxalyl group, or an alkoxyoxalyl group having 3-7 carbon atoms), a carboxyl group, an alkoxycarbonyl group having 2-5 carbon atoms, an amido group, an alkylamido group having 2-5 carbon atoms, an alkylthio group having 1-4 carbon atoms, an alkylsulfinyl group having 1-4 carbon atoms, an alkylsulfonyl group having 1-4 carbon atoms, a cyano group, a sulfamoyl group, an alkylsulfamoyl group having 1-4 carbon atoms, an amidino group, or an alkyl or alkoxy group having 1-5 carbon atoms which has been substituted by fluorine atom(s);X represents â€”Oâ€”, â€”OCOâ€”, â€”OSO2â€”, â€”Sâ€”, â€”SCOâ€”, â€”SOâ€”, â€”SO2â€”, â€”NR7â€²â€”, â€”NR7COâ€”, â€”NR7SO2â€”, â€”NR7CONHâ€”, â€”NR7CSNHâ€” or â€”NR7COCOâ€” (wherein R7â€² represents an alkyl group having 1-9 carbon atoms, a cycloalkyl group having 3-7 carbon atoms, an aralkyl group having 7-9 carbon atoms which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group, an alkoxyalkyl group having 2-5 carbon atoms, or an aryl, furyl or pyridyl group which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group and R7 represents a hydrogen atom, an alkyl group having 1-9 carbon atoms, a cycloalkyl group having 3-7 carbon atoms, an aralkyl group having 7-9 carbon atoms which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group, an alkoxyalkyl group having 2-5 carbon atoms, or an aryl, furyl or pyridyl group which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group); R3 represents a hydrogen atom, an alkyl group having 1-9 carbon atoms, a cycloalkyl group having 3-7 carbon atoms, an aralkyl group having 7-9 carbon atoms which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group, an alkoxyalkyl group having 2-5 carbon atoms, or an aryl, furyl or pyridyl group which may optionally be substituted by R8 (wherein R8 represents an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom or a nitro group), provided that when X is NR7, R3 and R7 may, together with the nitrogen atom to which they are bonded, form a 3- to 6-membered cyclic amino group or a 4- to 10-membered cyclic imido group; Y represents an alkylene group having 1-9 carbon atoms which may optionally be substituted by alkyl group(s) having 1-9 carbon atoms, cycloalkyl group(s) having 3-7 carbon atoms, hydroxylgroup(s), alkoxy group(s) having 1-9 carbon atoms or â€”NR9R10 (wherein R9 and R10 each independently have the same meaning as R5); Z represents a single bond, â€”Oâ€”, â€”OCOâ€”, â€”OSO2â€”, â€”Sâ€”, â€”SCOâ€”, â€”SOâ€”, â€”SO2â€”, â€”NR11â€”, â€”NR11COâ€”, â€”NR11SO2â€”, â€”NR11CONHâ€”, â€”NR11CSNHâ€”, â€”NR11COOâ€” or â€”NR11COCOâ€” (wherein R11 represents a hydrogen atom, an alkyl group having 1-9 carbon atoms, a cycloalkyl group having 3-7 carbon atoms, an aralkyl group having 7-9 carbon atoms which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group, an alkoxyalkyl group having 2-5 carbon atoms, or an aryl, furyl or pyridyl group which may optionally be substituted by R12 (wherein R12 is an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, a nitro group, an aryl, furyl or pyridyl group which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group, â€”NR13R14 (wherein R13 and R14 each independently have the same meaning as R5), a carboxyl group, an alkoxycarbonyl group having 2-5 carbon atoms, an amido group, an alkylamido group having 2-5 carbon atoms, an alkylthio group having 1-4 carbon atoms, an alkylsulfinyl group having 1-4 carbon atoms, an alkylsulfonyl group having 1-4 carbon atoms, a cyano group, a sulfamoyl group, an alkylsulfamoyl group having 1-4 carbon atoms, or an alkyl or alkoxy group having 1-5 carbon atoms which has been substituted by fluorine atom(s))); and R4 represents a hydrogen atom, an alkyl group having 1-9 carbon atoms, a cycloalkyl group having 3-7 carbon atoms, an aralkyl group having 7-9 carbon atoms which may optionally be substituted by one or more members selected from the group consisting of an alkyl group having 1-9 carbon atoms, an alkoxy group having 1-9 carbon atoms, a halogen atom, and a nitro group, an alkoxy group having 1-9 carbon atoms, an alkoxyalkyl group having 2-5 carbon atoms, a halogen atom, a silyl group substituted by hydrocarbon group(s), or an aryl, furyl or pyridyl group which may optionally be substituted by R15 (wherein R15 independently has the same meaning as R12), provided that when Z is other than a single bond, R4 is not a halogen atom.