| 摘要 |
The present invention comprises compounds of Formula (I).;
wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I). |
| 主权项 |
1. A compound of Formula (I) wherein: R1 is 2,3-dihydroindol-3-yl, indol-3-yl, pyridyl, pyrimidyl, pyridazyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, or pyrrolyl; wherein said pyridyl, pyrimidyl, pyridazyl, imidazolyl, oxazolyl, isoxazolyl, thiazolyl, or pyrrolyl is optionally substituted with OCH3, CH3, OCF3, CF3, OCF3, —CN, or C(O)CH3; R2 is H, Cl, CH3, OC(1-4)alkyl, or F; R3 is H, F, Cl, CO2C(1-4)alkyl, C(1-4)alkyl, OC(1-4)alkyl, SC(1-4)alkyl, OCF3, OCH2CF3, —CN, CO2H, C(O)C(1-4)alkyl, C(O)NH2, C(O)NHC(1-4)alkyl, C(O)N(C(1-4)alkyl)2, or CF3; R4 is H, CH3, OC(1-4)alkyl, or F; or R4 may be taken together with R3 and their attached phenyl to form a bicyclic ring selected from the group consisting of 2,3-dihydro-1H-inden-5-yl, 2,3-dihydrobenzofuran-5-yl, 2,2-difluoro-benzo[d][1,3]dioxole-5-yl, 2,2-dimethyl-benzo[d][1,3]dioxole-5-yl, 2,2-difluoro-2,3-dihydrobenzofuran-5-yl, 2,2-dimethyl-2,3-dihydrobenzofuran-5-yl, chroman-6-yl, and 2,3-dihydrobenzo[b][1,4]dioxin-6-yl; X is H, OH, NH2, or F; Y is NH2; Z is NH or —HC═CH—; and tautomers, and pharmaceutically acceptable salts thereof. |
