Patent ID: 6127407
Filing Date: 2000-10-03
Classification: A61P,C07C,C07D

Abstract:
A compound having the structural formula: ##STR4## or a pharmaceutically acceptable salt or hydrate thereof, wherein:The bond - - - designates a single or double bond;m is 0, 1, 2, 3 or 4;each n is independently 0, 1, 2, 3, 4 or 5;Y is absent, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkenyl or (C.sub.1 -C.sub.6) alkynyl;R.sub.1 is H, --OR, --SR, --O--C(O)R, --S--C(O)R, --O--C(S)R, --S--C(S)R, or when taken together with R.sub.2 is a .dbd.O, .dbd.S, .dbd.N--OR, a 3-8 membered heterocycloalkyl or a substituted 3-8 membered heterocycloalkyl;R.sub.2 is absent or --H;R.sub.3 is absent or --H;R.sub.4 is --H, --OR', --SR', --NR'.sub.2, --CN, --NO.sub.2, (C.sub.3 -C.sub.8) cycloalkyl, 3-8 membered heterocycloalkyl, --C(O)R', --C(S)R', --C(O)OR', --C(S)OR', --C(O)SR', --C(S)SR', C(O)NR'.sub.2 or --C(S)NR'.sub.2 ;each R.sub.5, R.sub.6 and R.sub.7 is independently selected from the group consisting of halogen, --R', --OR', --SR', --NR'.sub.2, --ONR'.sub.2, --SNR'.sub.2, --NO.sub.2, --CN, --C(O)R', --C(S)R', --C(O)OR', --C(O)SR', --C(S)OR', --CS(S)R', --C(O)NR'.sub.2, --C(S)NR'.sub.2, --C(O)NR'(OR'), --C(S)NR'(OR'); --C(O)NR'(SR'), --C(S)NR'(SR'), --CH(CN).sub.2, --CH[C(O)R'].sub.2, --CH[C(S)R'].sub.2, --CH[C(O)OR'].sub.2, --CH[C(S)OR'].sub.2, --CH[C(O)SR'].sub.2 and --CH[C(S)SR'].sub.2 ; with the following exceptions:when - - - is single bond, R.sub.1 and R.sub.2 when taken together are .dbd.O, Y is absent, R.sub.3 and R4 are H, m=0, n=1; then (a) if R.sub.5 is absent. then R.sub.6 is not Br (para), or OMe (para) or OH (para); (b) if R.sub.5 is OH (para) then R.sub.6 is not --NMe.sub.2 at the para position; orwhen - - - is single bond, both R.sub.1 and R.sub.2 are H, Y is absent, R.sub.3 and R4 both are H, m=0; (a) then n is not 0; and (b) if n is 1, then both R.sub.5 and R.sub.6 are not --NH.sub.2 at para positions; (c) if n is 1, then both R.sub.5 and R.sub.6 are not --OH at the para position; orwhen - - - is double bond, Y, R.sub.2 and R.sub.3 are absent, R.sub.1 and R.sub.4 are H, m=0; (a)then n is not 0; (b) if n is 1, R.sub.5 is absent, then R.sub.6 is not --OMe (para), or Br (para), or --CN (para); orwhen - - - is single bond, R.sub.1 and R.sub.2 taken together are .dbd.O, Y is absent, R.sub.3 is Me, R.sub.4 is 1, m=0, n=1, then both R.sub.5 and R.sub.6 are not --OH at the para position; orwhen - - - is single bond, R.sub.1 and R.sub.2 taken together are .dbd.O, Y is absent, R.sub.3 is --C(O)OEt, R.sub.4 is H, m=0, n=1, R.sub.5 is absent, then R.sub.6 is not --OH at the para position; orwhen - - - is single bond, R.sub.1 is --OH, R.sub.2 is H, Y is absent, R.sub.3 and R.sub.4 are H, m=0, n=1, R.sub.5 is absent, then R.sub.6 is not --Br at the para position; orwhen - - - is single bond, R.sub.1 and R.sub.2 taken together are .dbd.N--OH.HCl, Y is absent, R.sub.3 and R.sub.4 are H, m=0, then n is not 0; andeach R is independently selected from the group consisting of --H, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkenyl, (C.sub.1 -C.sub.6) alkynyl, (C.sub.5 -C.sub.20) aryl, substituted (C.sub.5 -C.sub.20) aryl, (C.sub.6 -C.sub.26) alkaryl and substituted (C.sub.6 -C.sub.26) alkaryl;the heterocycloalkyl substituents are each independently selected from the group consisting of --CN, --NO.sub.2, --NR'.sub.2, --OR', --C(O)NR'.sub.2, --C(S)NR'.sub.2, --C(O)OR', --C(S)OR', --C(O)SR', --C(S)SR' and trihalomethyl;the aryl substituents are each independently selected from the group consisting of halogen, --C(O)R', --C(S)R', --C(O)OR', --C(S)OR', --C(O)SR', --C(S)SR', --C(O)NR'.sub.2, --C(S)NR'.sub.2 and trihalomethyl;each R' is independently selected from the group consisting of --H, (C.sub.1 -C.sub.6) alkyl, (C.sub.1 -C.sub.6) alkenyl and (C.sub.1 -C.sub.6) alkynyl.