Patent ID: 6828344
Filing Date: 2004-12-07
Classification: C07D

Abstract:
A compound of the formulae: wherein:R1 and R1â€² are independently selected from H, halogen, â€”CF3, â€”OH, â€”C1-C10 alkyl, â€”Sâ€” C1-C10 alkyl, C1-C10 alkoxy, â€”CN, â€”NO2, â€”NH2, â€”HN(C1-C6), â€”N(C1-C6)2, phenyl, â€”O-phenyl, â€”S-phenyl, benzyl, â€”O-benzyl, â€”S-benzyl, the phenyl and benzyl rings of these groups being optionally substituted by from 1 to 3 substituents selected from halogen, C1-C6 alkyl, C1-C6 alkoxy, â€”NO2, â€”NH2, â€”CN, â€”CF3, or â€”OH; or a moiety of the formulae: R6 is selected from H, C1-C6 alkyl, C1-C6 alkoxy, â€”C(O)CH3 phenyl, â€”O-phenyl benzyl, â€”O-benzyl, the phenyl and benzyl rings of these groups being optionally substituted by from 1 to 3 substituents selected from halogen, C1-C6 alkyl, C1-C6 alkoxy, â€”NO2, â€”NH2, â€”CN, â€”CF3, or â€”OH; R7 is selected from â€”(CH2)nâ€”COOH, â€”(CH2)nâ€”Nâ€”(C1-C6 alkyl)2, â€”(CH2)nâ€”NHâ€”(C1-C6 alkyl), â€”CF3, C1-C6 alkyl, C3-C5 cycloalkyl, C1-C6 alkoxy, â€”NHâ€”(C1-C6 alkyl), â€”Nâ€”(C1-C6 alkyl)2, pyridinyl, thienyl, furyl, pyrrolyl, quinolyl, (CH2)nphenyl, phenyl, â€”O-phenyl, benzyl, â€”O-benzyl, adamantyl, â€”(CH2)n-phenyl-O-phenyl, â€”(CH2)n-phenyl-CH2-phenyl, â€”(CH2)nâ€”O-phenyl-CH2-phenyl, and â€”(CH2)n-phenylâ€”(Oâ€”CH2-phenyl)2, the rings of these groups being optionally substituted by from 1 to 3 substituents selected from halogen, C1-C6 alkyl, C1-C6 alkoxy, â€”NH2, â€”NO2, â€”CF3, CO2H, or â€”OH; R2 is selected from H, halogen, â€”CF3, â€”OH, â€”C1-C10 alkyl, C1-C10 alkoxy, â€”CHO, â€”CN, â€”NO2, â€”NH2, â€”NHâ€”C1-C6 alkyl, â€”N(C1-C6 alkyl)2, â€”Nâ€”SO2â€”C1-C6 alkyl, or â€”SO2â€”C1-C6 alkyl; R3 is selected from H, â€”CF3, C1-C6 lower alkyl, C1-C6 lower alkoxy, C3-C10 cycloalkyl, â€”C1-C6 alkyl, â€”C3-C10 cycloalkyl, â€”CHO, halogen, and (CH2)nC(O)NH2 R4 is selected from the group of C1-C6 lower alkyl, C1-C6 lower alkoxy, â€”(CH2)nâ€”C3-C6 cycloalkyl, â€”(CH2)nâ€”Sâ€”(CH2)nâ€”C3-C5 cycloalkyl, â€”(CH2)nâ€”Oâ€”(CH2)nâ€”C3-C5 cycloalkyl, and a moiety of the formulae â€”(CH2)nâ€”A, â€”(CH2)nâ€”Sâ€”A, or â€”(CH2)nâ€”Oâ€”A, wherein A is the moiety: â€ƒwherein D is H, C1-C6 lower alkyl, C1-C6 lower alkoxy, or â€”CF3; B and C are phenyl optionally substituted by from 1 to 3, substituents selected from H, halogen, â€”CF3, â€”OH, â€”C1-C6 alkyl, C1-C6 alkoxy, or â€”NO2; n is an integer from 0 to 3; R5 is a moiety selected from the formulae â€”L3â€”M3 wherein L3 is a bridging or linking moiety selected from a chemical bond, â€”(CH2)nâ€”, â€”Sâ€”, â€”Oâ€”, â€”SO2â€”, â€”C(O)â€”, â€”(CH2)nâ€”C(O)â€”, â€”(CH2)nâ€”C(O)â€”(CH2)nâ€”, â€”(CH2)nâ€”Oâ€”(CH2)nâ€”, â€”(CH2)nâ€”Sâ€”(CH2)nâ€”, â€”C(Z)â€”N(R6)â€”, â€”C(Z)â€”N(R6)â€”(CH2)nâ€”, â€”C(O)â€”C(Z)â€”N(R6)â€”, â€”C(O)â€”C(Z)â€”N(R6)â€”(CH2)nâ€”, â€”C(Z)â€”NHâ€”SO2â€”, â€”C(Z)â€”NHâ€”SO2â€”(CH2)nâ€”, â€”(CH2)nâ€”Sâ€”(CH2)nâ€”, â€”(CH2)nâ€”SOâ€”(CH2)nâ€”, â€”(CH2)nâ€”SO2â€”(CH2)nâ€”, or â€”(CH2)nâ€”CH&boxH;CHâ€”(CH2)nâ€”Oâ€”; Z is O or S: M3 is and n is an integer from 0 to 3; R9 is selected from H, halogen, â€”CF3, â€”OH, â€”COOH, â€”(CH2)nâ€”COOH, â€”(CH2)nâ€”C(O)â€”COOH, â€”C1-C16 alkyl, â€”Oâ€”C1-C6 alkyl, â€”NH(C1-C6 alkyl), or â€”N(C1-C6 alkyl)2; n is an integer from 0 to 3; or a pharmaceutically acceptable salt thereof.