Patent ID: 6127386
Filing Date: 2000-10-03
Classification: A61P,C07D

Abstract:
A compound having the structure ##STR31## or a pharmaceutically acceptable salt or pro-drug thereof wherein n is selected from 1, 2 or 3;R.sup.1 is selected from the group consisting ofhydrogen,allyl, andalkyl of one to six carbon atoms;R.sup.2 is selected from the group consisting ofhydrogen,C.sub.1 -C.sub.3 akylfluorine,chlorine,ethenyl, andphenyl;L is absent or is selected from the group consisting ofalkylene of one to six carbon atoms,--C.tbd.C--(C.sub.0 -C.sub.6 -alkyl)-, ##STR32## where p is one or two, ##STR33## where M is selected from --CH.sub.2 --, and --NH--; and R.sup.3 is selected from the group consisting ofa) hydrogen,b) alkyl of one to eight carbon atoms,c) alkenyl of two to six carbon atomsd) haloalkyl of one to six carbon atoms,e) hydroxyalkyl of one to six carbon atoms,f) alkoxy of one to six carbon atoms,g) amino,h) alkylamino of one to six carbon atoms,h') azacycle attached to L through a nitrogen atom,i) dialkylamino in which the two alkyl groups are independently of one to six carbon atoms,j) phenylk) naphthyl,l) biphenyl,m) furyl,n) thienyl,o) pyridinyl,p) pyrazinyl,q) pyridazinyl,r) pyrimidinyl,s) pyrrolyl,t) pyrazolyl,u) imidazolyl,v) indolyl,w) thiazolyl,x) oxazolyl,y) isoxazolyl,z) thiadiazolyl,aa) oxadiazolyl,bb) quinolinyl,cc) isoquinolinyl, anddd) any of b) or j) through cc) above substituted with one or two substituents independently selected from the group consisting ofalkyl of one to six carbon atoms,haloalkyl of one to six carbon atoms,alkoxy of one to six carbon atoms,alkoxyalkyl in which the alkoxy and alkyl portions are independently of one to six carbon atoms,alkoxyalkoxyl in which the alkoxy portions are independently of one to six carbon atoms,halogen,cyano,hydroxy,amino,alkylamino of one to six carbon atoms,carboxyl, andalkoxycarbonyl of two to six carbon atoms;with the provisos thati) when L is absent, R.sup.3 may not be alkyl of one to eight carbon atoms, amino, alkylamino, dialkylamino, alkoxy of 1-6 carbons, CF.sub.3 or CH.sub.2 OH;ii) when L is absent and R.sup.3 is hydrogen, R.sup.2 is selected from ethenyl, unsubstituted phenyl, and phenyl substituted as defined in dd) above; andiii) when L is alkylene, R.sup.3 may not be hydrogen or alkyl;when L is ##STR34## then R.sup.3 is selected from alkyl of one to eight carbon atoms, h'), i), j), k), l), m), n), o), p), q), bb), and cc) as defined above, or any of i), j), k), l), m), n),o), p), q), bb) and cc) optionally substituted as defined in dd) above;when L is ##STR35## and M is --CH.sub.2 --, then R.sup.3 may not be hydrogen; andvi) f) through y) above may be substituted as defined in z) above by no more than one alkylamino, carboxyl, or alkoxycarbonyl substituent, oralternatively, L-R.sub.3 is selected from --O--CH.sub.2 --R.sub.4, wherein R.sub.4 is selected from the group consisting of(a) CH.sub.3 OCH.sub.2 --,(b) i) through cc) as defined above for R.sup.3.