Patent ID: 6958354
Filing Date: 2005-10-25
Classification: A61P,C07D

Abstract:
1. A compound of formula (Ia): or a pharmaceutically acceptable salt, tautomer thereof, wherein R 1 is wherein R 2a is independently selected from the group consisting of: (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, C 3 -C 10 )cycloalkyl, (C 5 -C 10 )aryl, (C 1 -C 6 )alkylaryl, amino, carbonyl, carboxyl, (C 2 -C 6 )acid, (C 1 -C 6 )ester, (C 1 -C 6 )alkoxy, nitro, halo, hydroxyl, (C 1 -C 6 )alkoxy(C 1 -C 6 )ester, and where (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, (C 3 -C 10 )cycloalkyl, (C 5 -C 10 )aryl, amino, (C 2 -C 6 )acid, (C 1 -C 6 )ester, and (C 1 -C 6 )alkoxy of R 2a is optionally substituted by at least one moiety independently selected from the group consisting of halo, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, perhalo(C 1 -C 6 )alkyl, phenyl, (C 3 -C 10 )cycloalkyl, formyl, NC—, (C 1 -C 6 )alkyl-(C═O)—, phenyl-(C═O)—, HO—(C═O)—, (C 1 -C 6 )alkyl-O—(C═O)—, (C 1 -C 6 )alkyl-NH—(C═O)—, ((C 1 -C 6 )alkyl) 2 -N—(C═O)—, phenyl-NH—(C═O)—phenyl-[((C 1 -C 6 )alkyl)-N]—(C═O)—, O 2 N—, amino, (C 1 -C 6 )alkylamino, ((C 1 -C 6 )alkyl) 2 -amino, (C 1 -C 6 )alkyl-(C═O)—NH—, (C 1 -C 6 )alkyl-(C═O)—[((C 1 -C 6 )alkyl)-N]—, phenyl-(C═O)—NH—, phenyl-(C═O)—[((C 1 -C 6 )alkyl)-N[—, H 2 N—(C═O)—NH—, (C 1 -C 6 )alkyl-HN—(C═O)—NH—, ((C 1 -C 6 )alkyl) 2 N—(C═O)—NH—, (C 1 -C 6 )alkyl-HN—(C═O)—[((C 1 -C 6 )alkyl)-N]—, ((C 1 -C 6 )alkyl) 2 N—(C═O)—[(C 1 -C 6 )alkyl-N]—, phenyl-(C═O)—NH—, (phenyl) 2 N—(C═O)—NH—, phenyl-HN—(C═O)—[((C 1 -C 6 )alkyl)-N]—, (phenyl-) 2 N—(C═O)—[((C 1 -C 6 alkyl)-N]—, (C 1 -C 6 )alkyl-O—(C═O)—NH—, (C 1 -C 6 )alkyl-O—(C═O)—[((C 1 -C 6 )alkyl)-N]—, phenyl-O—(C═O)—NH—, phenyl-O—(C═O)—[(alkyl)-N]—, (C 1 -C 6 )alkyl-SO 2 NH—, phenyl-SO 2 NH—, (C 1 -C 6 )alkyl-SO 2 —, phenyl-SO 2 —, hydroxy, (C 1 -C 6 )alkoxy, perhalo(C 1 -C 6 )alkoxy, phenoxy, (C 1 -C 6 )alkyl-(C═O)—O—, (C 1 -C 6 )ester-(C 1 -C 6 )alkyl-O—, phenyl-(C═O)—O—, H 2 N—(C═O)—O—, (C 1 -C 6 )alkyl-HN—(C═O)—O—, ((C 1 -C 6 ) alkyl) 2 N—(C═O)—O—, phenyl-HN—(C═O)—O—, and (phenyl) 2 N—(C═O)—O—; each R 3 is independently selected from the group consisting of: hydrogen, halo, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, perhalo(C 1 -C 6 )alkyl, phenyl, (C 3 -C 10 )cycloalkyl, hydroxy, (C-C 6 )alkoxy, perhalo(C 1 -C 6 )alkoxy, phenoxy, (C 3 -C 10 )cycloalkyl-O—, (C 1 -C 6 )alkyl-S—, (C 1 -C 6 )alkyl-SO 2 —, (C 1 -C 6 )alkyl-NH—SO 2 —, O 2 N—, NC—, amino, Ph(CH 2 ) 1-6 6 HN—, (C 1 -C 6 )alkyl HN—, (C 1 -C 6 )alkylamino, [(C 1 -C 6 )alkyl] 2 -amino, (C 1 -C 6 )alkyl-SO 2 —NH—, amino(C═O)—, aminoO 2 S—, (C 1 -C 6 )alkyl-(C═O)—NH—, (C 1 -C 6 )alkyl-(C═O)—[(((C 1 -C 6 )alkyl)-N]—, phenyl-(C═O)—NH—, phenyl-(C═O)—[((C 1 -C 6 )alkyl)-N]—, (C 1 -C 6 )alkyl-(C═O)—, phenyl-(C═O)—, (C 3 -C 10 )cycloalkyl-(C═O)—, HO—(C═O)—, (C 1 -C 6 )alkyl-O—(C═O)—, H 2 N(C═O)—, (C 1 -C 6 )alkyl-NH—(C═O)—, [(C 1 -C 6 )alkyl] 2 -N—(C═O)—, phenyl-NH—(C═O)—, phenyl-[((C 1 -C 6 )alkyl)-N]—(C═O)—, (C 3 -C 10 )cycloalkyl-NH—(C═O)— and (C 1 -C 6 )alkyl-(C═O)—O—; where alkyl, alkenyl, alkynyl, phenyl, cycloalkyl, alkoxy, phenoxy, amino of R 3 is optionally substituted by at least one substituent independently selected from (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo, H 2 N—, Ph(CH 2 ) 1-6 HN—, and (C 1 -C 6 )alkylHN—; s is an integer from one to five; R 4 is selected from the group consisting of: hydrogen, halo, halo(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, perhalo(C 1 -C 6 )alkyl, phenyl, (C 3 -C 10 )cycloalkyl, hydroxy, (C 1 -C 6 )alkoxy, perhalo(C 1 -C 6 )alkoxy, phenoxy, (C 3 -C 10 )cycloalkyl-O—, (C 1 -C 6 )alkyl-S—, (C 1 -C 6 )alkyl-SO 2 —, (C 1 -C 6 )alkyl-NH—SO 2 —, O 2 N—, NC—, amino, Ph(CH 2 ) 1-6 NH—, alkylNH—, (C 1 -C 6 )alkylamino, [(C 1 -C 6 )alkyl] 2 -amino, (C 1 -C 6 )alkyl-SO 2 —NH—, amino(C═O)—, aminoSO 2 —, (C 1 -C 6 )alkyl-(C═O)—NH—, (C 1 -C 6 )alkyl-(C═O)—((C 1 -C 6 )alkyl)-N]—, phenyl-(C═O)—NH—, phenyl-(C═O)—((C 1 -C 6 )alkyl)-N]—, (C 1 -C 6 )alkyl-(C═O)—, phenyl-(C═O)—, cycloalkyl-(C═O)—, HO—(C═O)—, (C 1 -C 6 )alkyl-O—(C═O)—, H 2 N(C═O)—, (C 1 -C 6 )alkyl-NH—(C═O)—, ((C 1 -C 6 )alkyl) 2 -N—(C═O)—, phenyl-NH—(C═O)—, phenyl-((C 1 -C 6 )alkyl)-N]—(C═O)—, (C 3 -C 10 )cycloalkyl-NH—(C═O)—and (C 1 -C 6 )alkyl-(C═O)—O—, where alkyl, alkenyl, alkynyl, phenyl, cycloalkyl, alkoxy, phenoxy, and amino of R 4 is optionally substituted by at least one substituent independently selected from the group consisting of (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo(C 1 -C 6 )alkyl, halo, H 2 N—, Ph(CH 2 ) 1-6 —NH—, and (C 1 -C 6 )alkylNH—; and R 6 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, phenyl, (C 3 -C 10 )cycloalkyl, (C 1 -C 6 )alkyl-(SO 2 )—, phenyl-(SO 2 )—, H 2 N—(SO 2 )—, (C 1 -C 6 )alkyl-NH—(SO 2 )—, ((C 1 -C 6 )alkyl) 2 N—(SO 2 )—, phenyl-NH—(SO 2 )—, (phenyl) 2 N—(SO 2 )—, (C 1 -C 6 )alkyl-(C═O)—, phenyl-(C═O)—, (C 3 -C 10 )cycloalkyl-(C═O)—, (C 1 -C 6 )alkyl-O—(C═O)—, (C═O)—, (C 3 -C 10 )cycloalkyl-O—(C═O)—, H 2 N—(C═O)—, (C 1 -C 6 )alkyl-NH—(C═O)—, phenyl-NH—(C═O)—, (C 3 -C 10 )cycloalkyl-NH—(C═O)—, ((C 1 -C 6 )alkyl) 2 N—(C═O)—, (phenyl) 2 N—(C═O)—, phenyl-[((C 1 -C 6 )alkyl)-N]—(C═O)—, and (C 3 -C 10 )cycloalkyl-[((C 1 -C 6 )alkyl)-N]—(C═O)—; where alkyl, alkenyl, alkynyl, phenyl, benzyl, cycloalkyl, alkoxy, phenoxy, amino of R 6 is optionally substituted with at least one moiety independently selected from the group consisting of halo, (C 1 -C 6 )alkyl, (C 2 -C 6 )alkenyl, (C 2 -C 6 )alkynyl, perhalo(C 1 -C 6 )alkyl, (C 3 -C 10 )cycloalkyl, phenyl, benzyl, (C 1 -C 6 )alkyl-SO 2 —, formyl, NC—, (C 1 -C 6 )alkyl-(C═O)—, (C 3 C 10 )cycloalkyl-(C═O)—, phenyl-(C═O)—, HO—(C═O)—, (C 1 -C 6 )alkyl-O—(C═O)—, (C 3 -C 10 cycloalkyl-O—(C═O)—, (C 1 -C 6 )alkyl-NH—(C═O)—, (C 3 -C 10 )cycloalkyl-NH—(C═O)—, phenyl-NH—(C═O)—, ((C 1 -C 6 )alkyl) 2 -N—(C═O)—, phenyl-[((C 1 -C 6 )alkyl)-N]—(C═O)—, hydroxy, (C 1 -C 6 )alkoxy, perhalo(C 1 -C 6 )alkoxy, (C 3 -C 10 )cycloalkyl-O—, phenoxy, (C 1 -C 6 )alkyl-(C═O)—O—, (C 3 -C 10 )cycloalkyl-(C═O)—O—, phenyl-(C═O)—O—, O 2 N—, amino, (C 1 -C 6 )alkylamino, ((C 1 -C 6 )alkyl) 2 -amino, formamidyl, (C 1 -C 6 )alkyl-(C═O)—NH—, (C 3 -C 10 )cycloalkyl-(C═O)—NH—, phenyl-(C═O)—NH—, (C 1 -C 6 )alkyl-(C═O)—[((C 1 -C 6 alkyl)-N]—, phenyl-(C═O)—[(C 1 -C 6 )alkyl-N]—, (C 1 -C 6 )alkyl-SO 2 NH—, (C 3 -C 10 )cycloalkyl-SO 2 NH—, phenyl-SO 2 NH—, wherein the phenyl moiety of a R 6 substituent is optionally further substituted with at least one radical independently selected from the group consisting of halo, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, perfluoro(C 1 -C 6 )alkyl and perfluoro(C 1 -C 6 )alkoxy.