Patent ID: 6110922
Filing Date: 2000-08-29
Classification: A61P,C07C,C07D

Abstract:
A compound of the formula ##STR11## or a pharmaceutically-acceptable salt or prodrug thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are independently selected froma. hydrogen,b. halogen,c. alkyl,d. haloalkyl,e. alkoxy,f. cyano,g. nitro,h. carboxaldehyde, andwith the proviso that at least one of R.sub.1 or R.sub.3 is a ""cis-cinnamide"" or a ""trans-cinnamide"", defined as ##STR12## wherein R.sub.8 and R.sub.9 are independently selected from a. hydrogen, andb. alkyl,c. carboxy alkyl,d. alkylaminocarbonyl alkyl, ande. dialkylaminocarbonyl alkyl,R.sub.10 and R.sub.11 are independently selected froma. hydrogen,b. alkyl,c. cycloalkyl,d. alkoxycarbonylalkyl,e. hydroxyalkyl, andf. heterocyclylalkyl,or where NR.sub.10 R.sub.11 is heterocyclyl or substituted heterocyclyl, where substituents are independently selected from1) alkyl,2) alkoxy,3) alkoxyalkyl,4) cycloalkyl,5) aryl,6) heterocyclyl,7) heterocyclylcarbonyl,8) heterocyclylalkylaminocarbonyl,9) hydroxy,10) hydroxyalkyl,11) hydroxyalkoxyalkyl,12) carboxy,13) carboxycarbonyl,14) carboxaldehyde,15) alkoxycarbonyl,16) arylalkoxycarbonyl,17) aminoalkanoyl,18) carboxamido,19) alkoxycarbonylalkyl,20) carboxamidoalkyl,21) alkanoyl,22) hydroxyalkanoyl,23) alkanoyloxy,24) alkanoylamino,25) alkanoyloxyalkyl, and26) alkylsulfonyl,and wherein Ar is a substituted aryl or substituted heteroaryl group, where substitutions are independently selected froma. hydrogen,b. halogen,c. alkyl,d. aryl,e. haloalkyl,f. hydroxy,g. alkoxy,h. alkoxycarbonyl,i. alkoxyalkoxy,j. hydroxyalkyl,k. aminoalkyl,l. alkyl(alkoxycarbonylalkyl)aminoalkyl,m. heterocyclylalkyl,n. substituted heterocyclylalkyl,o. carboxaldehyde,p. carboxaldehyde hydrazone,q. carboxamide,r. alkoxycarbonyl alkyl,s. hydroxycarbonylalkyl (carboxyalkyl),t. cyano,u. amino,v. heterocyclylalkylamino, andw. ""trans-cinnamide"",or a pharmaceutically-acceptable salt or prodrug thereof.