Patent ID: 6750230
Filing Date: 2004-06-15
Classification: A61K,A61P,C07D

Abstract:
A compound of the formula Ib or a pharmaceutically acceptable salt or solvate thereof, whereineither (i) R1 is H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl, benzyl, halo, â€”CN, â€”OR7, â€”CO2R5, â€”CONR5R5, â€”OCONR5R5, â€”NR5CO2R7, â€”NR5R5, â€”NR5COR5, â€”NR5COâ€”(C1-C6 alkylene)-OR5, â€”NR5CONR5R5, â€”NR5SO2R7 or R6, said C1-C6 alkyl, C3-C7 cycloalkyl, phenyl and benzyl being optionally substituted by halo, â€”CN, â€”OR5, â€”OR8, â€”CO2R5, â€”CONR5R5, â€”OCONR5R5, â€”NR5CO2R7, â€”NR5R5, â€”NR8R9, â€”NR5COR6, â€”NR5COR6, â€”NR5COR8, â€”SO2NR5R5, â€”NR5CONR5R5, â€”NR5SO2R7 or R6 and R2 is â€”Yâ€”Z, or, R1 and R2, when taken together, represent unbranched C3-C4 alkylene, optionally wherein one methylene group of said C3-C4 alkylene is replaced by an oxygen atom or a nitrogen atom, said nitrogen atom being optionally substituted by R5 or R8, and R3 is H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl, benzyl, â€”CN, halo, â€”OR7, â€”CO2R5, â€”CONR5R5, â€”OCONR5R5, â€”NR5CO2R7, â€”NR5R5, â€”NR5COR5, â€”NR5CONR5R5, â€”NR5SO2R7 or R6, said C1-C6 alkyl, C3-C7 cycloalkyl, phenyl and benzyl being optionally substituted by halo, â€”CN, â€”OR5, â€”CO2R5, â€”CONR5R5, â€”OCONR5R5, â€”NR5CO2R7, â€”NR5R5, â€”NR5COR5, â€”SO2NR5R5, â€”NR5CONR5R5, â€”NR5SO2R7 or R6, or (ii) R1 and R3 are each independently C1-C6 alkyl, C3-C7 cycloalkyl or halo-(C1-C6 alkyl), and R2 is H, provided that (a) for definition (i), R1 and R3 are not both H, (b) for definition (i), R1 and R3 are not both optionally substituted phenyl, as defined therein, (c) for definition (i), when R1 and R3 are both methyl, R2 is not phenyl or methyl, and (d) for definition (ii), R1 and R3 are not both methyl; Y is a direct bond or C1-C3 alkylene; Z is R10 or, where Y is C1-C6 alkylene, Z is â€”NR5COR10, â€”NR5CONR5R10, â€”NR5CONR5COR10 or â€”NR5SO2R10; R4 is dichloro-substituted phenyl; each R1 is independently either H, C1-C6 alkyl, C3-C7 cycloalkyl, fluoro-(C1-C6)-alkyl, phenyl or benzyl, or, when two such groups are attached to the same nitrogen atom, those two groups taken together with the nitrogen atom to which they are attached represent piperidinyl said piperidinyl being optionally substituted by C1-C6 alkyl or C3-C7 cycloalkyl; R6 is a four to six-membered, aromatic, partially unsaturated or saturated non-heterocyclic group, said non-heterocyclic group being optionally substituted by â€”OR5, â€”NR5R5, â€”CN, oxo, C1-C6 alkyl, C3-C7 cycloalkyl, â€”COR7 or halo; R7 is C1-C6 alkyl, C3-C7 cycloalkyl, fluoro-(C1-C6)-alkyl, phenyl or benzyl; R8 is C1-C6 alkyl substituted by phenyl or pyridyl, said phenyl and pyridyl being optionally substituted by halo, â€”CN, â€”CONR5R5, â€”SO2NR5R5, â€”NR5SO2R7, â€”NR5R5, â€”(C1-C6 alkylene)-NR5R5, C1-C6 alkyl, fluoro-(C1-C6)-alkyl, C3-C7 cycloalkyl or C1-C6 alkoxy; R9 is H, C1-C6 alkyl or C3-C7 cycloalkyl, said C1-C6 alkyl and C3-C7 cycloalkyl being optionally substituted by â€”OR5, â€”NR5R5, â€”NR5COR5, â€”CONR5R5 or R6; R10 is (a) benzyl or C-linked R6, said benzyl being optionally substituted by halo, â€”OR5, â€”OR12, â€”CN, â€”CO2R7, â€”CONR5R5, â€”OCONR5R5, â€”C(&boxH;NR5)NR5OR5, â€”CONR5NR5R5, â€”OCONR5CO2R7, â€”NR5R5, â€”NR5R12, â€”NR5COR5, â€”NR5CO2R7, â€”NR5CONR5R5, â€”NR5COCONR5R5, â€”NR5SO2R7, â€”SO2NR5R5 or R6, or (b) when R1 and R3 are each independently C1-C6 alkyl, C3-C7 cycloalkyl or halo-(C1-C6 alkyl), R10 is phenyl, C1-C6 alkyl or C3-C7 cycloalkyl each being optionally substituted by halo, â€”OR5, â€”OR12, â€”CN, â€”CO2R7, â€”CONR5R5, â€”OCONR5R5, â€”C(&boxH;NR5)NR5OR5, â€”CONR5NR5R5, â€”OCONR5CO2R7, â€”NR5R5, â€”NR5R12, â€”NR5COR5, â€”NR5CO2R7, â€”NR5CONR5R5, â€”NR5COCONR5R5, â€”NR5SO2R7, â€”SO2NR5R5 or R6; X is â€”CH2â€”, â€”CHR11â€”, â€”COâ€”, â€”Sâ€”, â€”SOâ€” or â€”SO2â€”; R11 is C1-C6 alkyl, C3-C7 cycloalkyl, fluoro-(C1-C6)-alkyl or C1-C6 alkoxy; and R12 is C1-C6 alkyl substituted by R6, â€”OR5, â€”CONR5R5, â€”NR5COR5 or â€”NR5R5.