Patent ID: 6071935
Filing Date: 2000-06-06
Classification: A61P,C07D

Abstract:
A compound of the formula ##STR6## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 and R.sub.2 are independently selected from the group consisting of --(CH.sub.2).sub.p (5-10 membered heterocyclyl), --(CH.sub.2).sub.p (C.sub.6 -C.sub.10 aryl), allyl, propargyl and C.sub.1 -C.sub.6 alkyl wherein p is 0 to 3, said alkyl and the alkyl moieties of said R.sub.1 and R.sub.2 groups are optionally substituted by 1 to 3 R.sub.9 substituents, and the aryl and heterocyclyl moieties of said R.sub.1 and R.sub.2 groups are optionally substituted by 1 to 3 substituents independently selected from halo and R.sub.9 ;R.sub.3 is --(CH.sub.2)m(1- or 2-adamantyl), --(CH.sub.2).sub.m (C.sub.3 -C.sub.10 cycloalkyl), --(CH.sub.2)m(C.sub.6 -C.sub.10 aryl), C.sub.1 -C.sub.10 alkyl, ##STR7## wherein m is 0 to 6, said cycloalkyl and alkyl optionally contain 1 or 2 double or triple bonds;X.sub.1, X.sub.2, and X.sub.3 are each independently C.sub.1 -C.sub.7 alkylene optionally containing 1 or 2 double or triple bonds, X.sub.4 is a bond or C.sub.1 -C.sub.7 alkylene optionally containing 1 or 2 double or triple bonds, and, in formula (Ib), the X.sub.4 moiety is attached to the X.sub.1 moiety at any available carbon in the X.sub.1 moiety;R.sub.4 is C.sub.6 -C.sub.10 aryl, 5-10 membered heterocyclyl or C.sub.1 -C.sub.6 alkyl wherein each of said R.sub.4 groups is optionally substituted by 1 to 3 R.sub.5 substituents;each R.sub.5 is independently selected from the group consisting of halo, nitro, cyano, phenyl, --C(O)OR.sub.6, --SO.sub.2 NR.sub.6 R.sub.7, --NR.sub.6 R.sub.8, --C(O)R.sub.6, --OR.sub.6, --C(O)NR.sub.6 R.sub.8, --OC(O)NR.sub.6 R.sub.8, --NR.sub.8 C(O)NR.sub.8 R.sub.6, --NR.sub.8 C(O)R.sub.6, --NR.sub.8 C(O)O(C.sub.1 -C.sub.4 alkyl), --C(NR.sub.8)NR.sub.8 R.sub.6, --C(NCN)NR.sub.8 R.sub.6, --C(NCN)S(C.sub.1 -C.sub.4 alkyl), --NR.sub.8 C(NCN)S(C(O)-C.sub.4 alkyl), --NR.sub.8 C(NCN)NR.sub.8 R.sub.6, --NR.sub.8 SO.sub.2 (C.sub.1 -C.sub.4 alkyl), --S(O).sub.n (C.sub.1 -C.sub.4 alkyl) wherein n is 0 to 2,--NR.sub.8 C(O)C(O)NR.sub.8 R.sub.6, --NR.sub.8 C(O)C(O)R8, thiazolyl, imidazolyl, oxazolyl, pyrazolyl, triazolyl, tetrazolyl, and C.sub.1 -C.sub.4 alkyl optionally substituted by 1 to 3 fluoro substituents;each R.sub.6 and R.sub.7 is independently hydrogen or C.sub.1 -C.sub.4 alkyl;each R.sub.8 is independently R.sub.6 or --OR.sub.6 ; and,each R.sub.9 is independently selected from cyano, R.sub.6, --OR.sub.6, --OC(O)R.sub.6, --C(O)OR.sub.6, --C(O)NR.sub.6 R.sub.7, --NR.sub.6 R.sub.7, --NR.sub.6 R.sub.8, --SO.sub.2 NR.sub.6 R.sub.7, and C.sub.1 -C.sub.4 alkyl substituted by hydroxy.