Patent ID: 6448243
Filing Date: 2002-09-10
Classification: A61P,C07D

Abstract:
A 1,4-Substituted cyclic amine derivative (I) represented by the following formula or a pharmacologically acceptable salt thereof: whereinA, B, C, and D are the same or different from one another and each represents methine or nitrogen, provided at least two of them are methine; the bond represented by the following formula: â€ƒrepresents a single or double bond; T represents methine or nitrogen; Y and Z are the same or different from each other and each represents methine, nitrogen, a group represented by the following formula: â€ƒor a group represented by the following formula: â€ƒprovided at least one of them represents nitrogen; R1 and R2 are the same or different from each other and each represents hydrogen, halogeno, hydroxy, lower alkylsulfonylaminoalkyl, lower halogenated-alkylsulfonylaminoalkyl, 2-pyrrolidinon-1-yl, 1-hydroxy-1-(methoxypyridyl)methyl, methoxypyridylcarbonyl, 1,3-propanesultum-2-yl, lower hydroxypiperidylcarbonylalkyl, lower hydroxyallylamidoallkyl, lower halogenated-alkylamidoalkyl, lower dihalogenated-alkylamidoalkyl, lower heteroarylamidoalkyl, lower hydroxyalkylamidoalkyl, optionally substituted amino, nitro, lower alkyl, lower alkoxy, lower acyl, lower alkoxyalkoxy, cyano, lower alkylsulfonyl, sulfonylamido, hydroxy-lower alkyl, hydroxy-lower alkoxy, lower alkoxycarbonylamino, lower alkylsulfonylamino, N-lower alkylalkylsulfonylamino, lower acylamino, optionally substituted aminoalkyl, optionally N-substituted lower acylaminoalkyl, optionally substituted aryl, optionally substituted arylsulfonylamino, lower alkylsulfonyloxy, hydroxyiminomethyl, (2-pyrrolidon-1-yl)methyl, (2-piperidon-1-yl)methyl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, cycloalkylcarbonylaminoalkyl, optionally substituted ureido, optionally substituted ureido-lower alkyl, succinimido, (succinimido-1-yl)-lower alkyl, amido, optionally substituted carbamoyl, optionally substituted carbamoyl-lower alkyl, optionally substituted thiocarbamoyl-lower alkyl, formyl, aromatic acyl, heteroarylcarbonyl, halogenated lower alkyl, (2-imidazolidinon-1-yl)methyl, (2,4-imidazolidinedion-3-yl)methyl, (2-oxazolidon-3-yl)methyl, (glutarimido-1-yl)methyl, optionally substituted heteroarylhydroxyalkyl, cyano-lower alkyl, 1-hydroxy lower cycloalkyl, (2,4-thiazolidinedion-3-yl)methyl, optionally substituted 4-piperidylmethyl, heteroarylacyl, pyrrolidinylcarbonyl-lower alkyl, optionally substituted aminosulfonylalkyl, carboxy-lower alkyl or lower alkylamidoalkyl; or alternatively R1 and R2 together may form optionally substituted alicycle, optionally substituted heterocycle or alkylenedioxy, provided these rings may be substituted; R3 represents hydrogen, halogeno, lower alkyl, hydroxy, hydroxy-lower alkyl, lower alkoxy, formyl, optionally substituted aralkyloxy, hydroxy-lower alkoxy, optionally substituted sulfamoyl or optionally N-substituted sulfamoyl-lower alkyl; R4 represents hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxyalkyl, optionally aryl-substituted aryloxyalkyl or optionally aryl-substituted aralkyloxyalkyl; R5 represents lower alkyl, lower acyl, lower alkoxycarbonyl, aromatic acyl, or a group represented by the following formula: â€”Q1â€”(CH2)sâ€”Q2â€”R6 â€ƒwherein Q1 and Q2 are both single bonds, or one of them is a single bond while the other represents oxygen, carbonyl, a group represented by â€”NHCOâ€”, a group represented by â€”NHSO2â€”, or a group represented by >CHâ€”R7 wherein R7 represents hydroxy, lower alkyl or halogeno: s represents 0 or an integer of 1 to 6; and R6 represents optionally substituted aryl, optionally substituted heteroaryl, optionally substituted benzoheteroaryl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, benzothiazolyl, or cyano; wherein, in the above definitions, â€œheteroarylâ€  is selected from pyridyl, pyrazyl, pyrimidyl, pyrrolyl, imidazolyl, pyrazolyl, quinolyl, isoquinolyl, furyl, thienyl, and thiazolyl; n represents 0 or an integer of 1 to 3, provided that when n represents 0, at least one of A, B, C, and D represents nitrogen, and when n represents 1, more or less than one of A, B, C, D, and T represents nitrogen; m represents 0 or an integer of 1 to 6; and represents an integer of 1 to 3.