Patent ID: 6274715
Filing Date: 2001-08-14
Classification: A61P,C07H

Abstract:
A compound having the formula: ##STR30##or pharmaceutically acceptable salts and esters thereof, wherein a first substituent, optionally a second substituent, and optionally a third substituent selected from A, B, D and E are independently selected from the group consisting of:(a) C.sub.1 -C.sub.6 alkyl, substituted with one or more substituents selected from the group consisting of:(i) aryl;(ii) substituted-aryl;(iii) heteroaryl;(iv) substituted-heteroaryl;(v) heterocycloalkyl;(vi) hydroxy;(vii) C.sub.1 -C.sub.6 alkoxy;(viii) halogen consisting of Br, Cl, F or I; and(ix) NR.sup.3 R.sup.4, wherein R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1 -C.sub.6 -alkyl, or R.sup.3 and R.sup.4 taken together with a first hetero function, wherein said first hetero function is the nitrogen atom to which R.sup.3 and R.sup.4 are connected, form a non-aromatic 3- to 7-membered ring;said ring optionally containing a second hetero function selected from the group consisting of --O--, --NH--, --N(C.sub.1 -C.sub.6 -alkyl-)-, --N(aryl-C.sub.1 -C.sub.6 -alkyl-)-, --N(substituted-aryl-C.sub.1 -C.sub.6 -alkyl-)-, --N(heteroaryl-C.sub.1 -C.sub.6 -alkyl-)-, --N(substituted-heteroaryl-C.sub.1 -C.sub.6 -alkyl-)-, --S-- and --S(O).sub.n --, wherein n is 1 or 2;(b) C.sub.3 -C.sub.7 -cycloalkyl;(c) aryl;(d) substituted-aryl;(e) heteroaryl;(f) substituted-heteroaryl;(g) heterocycloalkyl; and(h) C.sub.1 -C.sub.6 -alkyl-M--R.sup.5, wherein the C.sub.1 -C.sub.6 -alkyl group is optionally substituted with a substituent in group (a)(i)-(a)(ix), and wherein M is selected from the group consisting of:(aa) --C(O)--NH--;(bb) --NH--C(O)--;(cc) --NH--;(dd) --N(CH.sub.3)--;(ee) --O--;(ff) --S(O).sub.n --, wherein n is 0, 1 or 2;(gg) --C(.dbd.NH)--NH--;(hh) --C(O)--O--;(ii) --O--C(O)--;(jj) --O--C(O)--NH--;(kk) --NH--C(O)--O--; and(ll) --NH--C(O)--NH--;R.sup.5 is selected from the group consisting of:(aaa) C.sub.1 -C.sub.6 -alkyl, optionally substituted with a substituent selected from the group consisting of:(i) aryl;(ii) substituted-aryl;(iii) heteroaryl; and(iv) substituted-heteroaryl;(bbb) aryl;(ccc) substituted-aryl;(ddd) heteroaryl;(eee) substituted-heteroaryl; and(fff) heterocycloalkyl;said optional second and optional third substituents selected from a group (a)-(h) above and further selected from a group consisting of:(i) hydrogen; and(j) C.sub.1 -C.sub.6 -alkyl;a fourth substituent selected from A, B, D and E is hydrogen or C.sub.1 -C.sub.6 -alkyl; R.sup.1 is selected from the group consisting of:(a) hydrogen;(b) --O--C.sub.1 -C.sub.3 -alkyl;(c) --O--C.sub.3 -C.sub.5 -cycloalkyl;(d) --O--C.sub.1 -C.sub.3 -alkyl-C.sub.3 -C.sub.5 -cycloalkyl;(e) --O--C(O)--C.sub.1 -C.sub.3 -alkyl;(f) --O--C(O)--O--C.sub.1 -C.sub.3 -alkyl; and(g) --O--C(O)--NH--C, C.sub.3 -alkyl;R.sup.2 is hydrogen or a hydroxy-protecting group; and Z is hydroxy or protected-hydroxy.