Patent ID: 8236846
Filing Date: 2012-08-07
Classification: A61K,A61P,C07D

Abstract:
1. A compound of formula I: wherein: r is 0, 1 or 2; Ar is selected from: R R 1a is H, —C 1-6 alkyl, —C 1-3 alkylenearyl, —C 1-3 alkyleneheteroaryl, —C 3-7 cycloalkyl, —CH(C 1-4 alkyl)OC(O)R 1aa , —C 0-6 alkylenemorpholine, R 1aa is —O—C 1-6 alkyl, —O—C 3-7 cycloalkyl, —NR 1ab R 1ac ; or —CH(NH 2 )CH 2 COOCH 3 ; R 1ab and R 1ac are independently selected from H, —C 1-6 alkyl, and benzyl, or are taken together as —(CH 2 ) 3-6 —; R 1b is R 1c or —NHC(O)R 1c ; R 1c is —C 1-6 alkyl, —C 0-6 alkylene-O—R 1ca ; —C 1-5 alkylene-NR 1cb R 1cc , —C 0-4 alkylenearyl or —C 0-4 alkyleneheteroaryl; R 1ca is H, —C 1-6 alkyl, or —C 1-6 alkylene-O—C 1-6 alkyl; R 1cb and R 1cc are independently selected from H and —C 1-6 alkyl, or are taken together as —(CH 2 ) 2 —O—(CH 2 ) 2 — or —(CH 2 ) 2 —N[C(O)CH 3 ]—(CH 2 ) 2 —; R 1d is H, R 1c , —C(O)R 1c , or —C(O)NHR 1c ; R 1e is —C 1-4 alkyl or aryl; Y is —N—, Z is —C(R R R X is —C R R 5ea is —O—C 1-6 alkyl, —O—C 3-7 cycloalkyl, —NR 5eb R 5ec , or —CH(NH 2 )CH 2 COOCH 3 ; R 5eb and R 5ec are independently selected from H, —C 1-4 alkyl, and —C 1-3 alkylenearyl, or are taken together as —(CH 2 ) 3-6 —; R 5f is H, —C 1-4 alkyl, —C 0-3 alkylenearyl, —C 1-3 alkylene-NR 5fa R 5fb , or —C 1-3 alkylene(aryl)-C 0-3 alkylene-NR 5fa R 5fb ; R 5fa and R 5fb are independently selected from H and —C 1-4 alkyl; R 5g is H, —C 1-6 alkyl, —C 1-3 alkylenearyl, or —CH 2 —O—(CH 2 ) 2 —O—CH 3 ; R 5h is H or —C 1-4 alkyl; R 5i is H, —C 1-4 alkyl, or —C 0-3 alkylenearyl; and R 5j is —C 1-6 alkyl, aryl, or —CH 2 CH(NH 2 )COOH; R R wherein: each —CH each ring in Ar and each aryl and heteroaryl in R each carbon atom in X is optionally substituted with one or more R each alkyl and each aryl in R and pharmaceutically acceptable salts thereof.