| 摘要 |
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows:;wherein R0, R1, R2, R3, R4 and a are defined herein. |
| 主权项 |
1. A method for treating cardiovascular disease aggravated by cold, including peripheral vascular disease, vascular hypertension, pulmonary hypertension, Raynaud's disease, and coronary artery disease, comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formula (I): wherein: a is an integer from 0 to 2; each R0 is independently selected from the group consisting of halogen, C1-2alkyl and fluorinated C1-2alkyl; R2 is hydrogen; R1 is selected from the group consisting of lower alkyl, fluorinated lower alkyl and monocyclic cycloalkyl-(lower alkyl)-; alternatively R2 and R1 are taken together as R3 is phenyl; wherein the phenyl is optionally substituted with a substituent selected from the group consisting of halogen and fluorinated lower alkyl; R4 is selected from the group consisting of benzyl, 4-fluoro-benzyl, 3,4-difluoro-benzyl, 3-chloro-4-fluoro-benzyl, 4-difluoromethyl-benzyl, 3-trifluoromethyl-benzyl, 4-trifluoromethyl-benzyl, 3-trifluoromethoxy-benzyl, 4-trifluoromethoxy-benzyl, 3-fluoro-4-trifluoromethyl-benzyl, 3-trifluoromethyl-4-fluoro-benzyl, 2-fluoro-5-trifluoromethyl-benzyl and 4-trifluoromethyl-thio-benzyl; provided that when a is 0, R1 is methyl, R2 is hydrogen and R4 is methyl; then R3 is other than methyl, phenyl or 4-methylphenyl; or pharmaceutically acceptable salt thereof. |
