Claims
- 1. A compound having the formula ##STR6## or a pharmaceutically acceptable salt, ester, amide or prodrug thereof, wherein
- R.sup.100 is selected from the group consisting of hydrogen, hydroxy, halogen, --OR.sup.13 and --OR.sup.14 ;
- R.sup.101 is selected from the group consisting of methyl, ethyl, allyl and propyl;
- R.sup.102 is hydrogen and R.sup.103 is selected from the group consisting of (a) hydrogen, (b) hydroxyl and (c) hydroxyl protected by a hydroxy-protecting group selected from tri(C.sub.1 -C.sub.8 -loweralkyl)silyl, C.sub.1 -C.sub.8 -loweralkyldiarylsilyl, triarylsilyl, tri(arylC.sub.1 -C.sub.12 -alkyl)silyl, triphenylmethyl-dimethylsilyl, trimethylsilylethoxycarbonyl, methylthiomethyoxyethoxycarbonyl, benzenesulfonylethoxycarbonyl, trimethylsilylethoxymethyl and aryl--C(O)-- or, taken together, R.sup.102 and R.sup.103 form a bond; and
- one of R.sup.104 and R.sup.105 is hydrogen, and the other of R.sup.104 and R.sup.105 is a group having the formula ##STR7## where m and n are independently zero, one or two; X is selected from the group consisting of oxygen, --S(O).sub.s -- where s is zero, one or two, --N(R.sup.1)-- and --C(R.sup.2)(R.sup.2')--, or is absent; and
- R.sup.3, R.sup.4 and R.sup.5 are independently selected from the group consisting of
- (a) hydrogen;
- (b) C.sub.1 -C.sub.12 -alkyl;
- (c) halo-C.sub.1 -C.sub.12 -alkyl;
- (d) C.sub.3 -C.sub.8 -cycloalkyl;
- (e) C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.8 alkyl;
- (f) C.sub.2 -C.sub.12 -alkenyl;
- (g) C.sub.2 -C.sub.12 -alkynyl;
- (h) hydroxy-C.sub.1 -C.sub.8 -alkyl;
- (i) hydroxyl-C.sub.1 -C.sub.8 -alkoxy-C.sub.1 -C.sub.12 -alkyl;
- (j) aryl substituted by R.sup.6, R.sup.7 and R.sup.8 wherein R.sup.6, R.sup.7 and R.sup.8 are defined as below;
- (j') aryl-C.sub.1 -C.sub.12 -alkyl substituted by R.sup.6, R.sup.7 and R.sup.8 wherein R.sup.6, R.sup.7 and R.sup.8 are defined as below;
- (k) C.sub.1 -C.sub.8 -alkoxycarbonyl;
- (l) C.sub.1 -C.sub.8 -alkoxycarbonyl-C.sub.1 -C.sub.12 -alkyl;
- (m) carboxy-C.sub.1 -C.sub.8 -alkyl;
- (n) aminoalkyl of the formula {R.sup.403)(R.sup.404)N-C.sub.1 -C.sub.8 -alkyl wherein R.sup.403 and R.sup.404 are independently selected from hydrogen, C.sub.1 -C.sub.8 -alkyl, aryl and aryl-C.sub.1 -C.sub.12 -alkyl or R.sup.403 and R.sup.404, taken together, are --(CH.sub.2).sub.bb -- wherein bb is 2-6;
- (o) C.sub.1 -C.sub.12 -thiolalkyl;
- (q) heterocyclic;
- (r) (heterocyclic)-C.sub.1 -C.sub.12 -alkyl;
- (s) (heterocyclic)-C.sub.1 -C.sub.12 -alkylamino-C.sub.1 -C.sub.8 -alkyl;
- (u) N-mono-C.sub.1 -C.sub.12 -alkylamino-C.sub.1 -C.sub.8 -alkyl or N-mono-C.sub.3 -C.sub.8 -cycloalkylamino-C.sub.1 -C.sub.8 -alkyl;
- (u') N,N-di-(C.sub.1 -C.sub.12 -alkyl)amino-C.sub.1 -C.sub.8 -alkyl or N,N-di-(C.sub.3 -C.sub.8 -cycloalkyl)amino-C.sub.1 -C.sub.8 -alkyl;
- (v) N-mono-C.sub.1 -C.sub.12 -alkylcarboxamido-C.sub.1 -C.sub.8 -alkyl;
- (v') N,N-di-(C.sub.1 -C.sub.12 -alkyl)carboxamido-C.sub.1 -C.sub.8 -alkyl;
- (w) N-monoarylcarboxamido-C.sub.1 -C.sub.8 -alkyl;
- (w') N,N-diarylcarboxamido-C.sub.1 -C.sub.8 -alkyl;
- (x) formyl;
- (x') protected formyl selected from dimethylacetal, diethylacetal, bis-(2,2,2-trichloroethyl)acetal, dibenzylacetal, 1,3-dioxanyl, 5-methylene-1,3-dioxanyl, 5,5-dibromo-1,3-dioxanyl, O-methyl-S-2-[methythiol)ethyl acetal and 1,3-oxathiolanyl;
- (z) (heterocyclic)-C.sub.2 -C.sub.12 -alkenyl; and
- (aa) (heterocyclic)-C.sub.2 -C.sub.12 -alkynyl;
- or, taken together, R.sup.3 and R.sup.5 form a methylene radical --CH.sub.2 --;
- R.sup.1 is selected from the group consisting of
- (a) hydrogen;
- (b) C.sub.1 -C.sub.12 -alkyl;
- (c) halo-C.sub.1 -C.sub.12 -alkyl;
- (d) C.sub.3 -C.sub.8 -cycloalkyl;
- (e) C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.8 -alkyl;
- (f) C.sub.2 -C.sub.12 -alkenyl;
- (g) C.sub.2 -C.sub.12 -alkynyl;
- (h) hydroxy-C.sub.1 -C.sub.8 -alkyl;
- (i) hydroxyl-C.sub.1 -C.sub.8 -alkoxy-C.sub.1 -C.sub.12 -alkyl;
- (j) aryl substituted by R.sup.6, R.sup.7 and R.sup.8 wherein R.sup.6, R.sup.7 and R.sup.8 are independently defined as below;
- (j') aryl-C.sub.1 -C.sub.12 -alkyl substituted by R.sup.6, R.sup.7 and R.sup.8 wherein R.sup.6, R.sup.7 and R.sup.8 are independently defined as below;
- (k) C.sub.1 -C.sub.8 -alkoxycarbonyl;
- (l) C.sub.1 -C.sub.8 -alkoxycarbonyl-C.sub.1 -C.sub.12 -alkyl;
- (m) carboxy-C.sub.1 -C.sub.8 -alkyl;
- (n) aminoalkyl of the formula (R.sup.403)(R.sup.404)N-C.sub.1 -C.sub.8 -alkyl wherein R.sup.403 and R.sup.404 are independently defined as above;
- (o) C.sub.1 -C.sub.12 -thiolalkyl;
- (p) --S(O).sub.x --R.sup.9 where x is one or two and R.sup.9 is selected from the group consisting of C.sub.1 -C.sub.12 alkyl, aryl, and aryl-C.sub.1 -C.sub.12 alkyl;
- (p') C.sub.1 -C.sub.12 -alkyl-C(O)-- or aryl-C(O)--;
- (q) heterocyclic;
- (r) (heterocyclic)-C.sub.1 -C.sub.12 -alkyl;
- (s) (heterocyclic)-C.sub.1 -C.sub.12 -alkylamino-C.sub.1 -C.sub.8 -alkyl;
- (u) N-mono-C.sub.1 -C.sub.12 -alkylamino-C.sub.1 -C.sub.8 -alkyl or N-mono-C.sub.3 -C.sub.8 -cycloalkylamino-C.sub.1 -C.sub.8 -alkyl;
- (u') N, N-di-(C.sub.1 -C.sub.12 -alkyl)amino-C.sub.1 -C.sub.8 -alkyl or N,N-di-(C.sub.3 -C.sub.8 -cycloalkyl)amino-C.sub.1 -C.sub.8 -alkyl;
- (v) N-mono-C.sub.1 -C.sub.12 -alkylcarboxamido-C.sub.1 -C.sub.8 -alkyl;
- (v') N,N-di-(C.sub.1 -C.sub.12 -alkyl)carboxamido-C.sub.1 -C.sub.8 -alkyl;
- (w) N-monoarylcarboxamido-C.sub.1 -C.sub.8 -alkyl;
- (w') N, N-diarylcarboxamido-C.sub.1 -C.sub.8 -alkyl;
- (x) formyl;
- (x') protected formyl selected from dimethylacetal, diethylacetal, bis-(2,2,2-trichloroethyl)acetal, dibenzylacetal, 1,3-dioxanyl, 5-methylene-1,3-dioxanyl, O-methyl-S-2-(methythiol)ethyl acetal and 1,3-oxathiolanyl;
- (y) --P(O)(OR.sup.10)(OR.sup.10') where R.sup.10 and R.sup.10' are independently selected from the group consisting of C.sub.1 -C.sub.8 -loweralkyl, aryl-C.sub.1 -C.sub.12 -alkyl and aryl;
- (z) (heterocyclic)-C.sub.2 -C.sub.12 -alkenyl;
- (aa) (heterocyclic)-C.sub.2 -C.sub.12 -alkynyl;
- (bb) --NHC(O)NH.sub.2 ;
- (cc) nitro; and
- (dd) polyhydroxyl-C.sub.1 -C.sub.12 -alkyl;
- R.sup.2 and R.sup.2' are independently selected from the group consisting of hydrogen, hydroxy, hydroxy-C.sub.1 -C.sub.8 -alkyl, R.sup.402 C(O)N(R.sup.401)-C.sub.1 -C.sub.8 -alkyl wherein R.sup.401 and R.sup.402 are independently selected from hydrogen C.sub.1 -C.sub.8 -alkyl, aryl, aryl-C.sub.1 -C.sub.12 -alkyl and halo-C.sub.1 -C.sub.12 -alkyl or R.sup.401 and R.sup.402, taken together are --(CH.sub.2).sub.aa -- wherein aa is 2-6, --C(O)NH(C.sub.1 -C.sub.8 -alkyl), --C(O)N(C.sub.1 -C.sub.8 -alkyl)(C.sub.1 -C.sub.8 -alkyl), pyrrolidin-1-yl and piperidin-1-yl; or, taken together, R.sup.2 and R.sup.2' are a divalent radical selected from the group consisting of oxo, thiooxo and --O(CH.sub.2).sub.i O--, where i is two, three or four;
- R.sup.6, R.sup.7 and R.sup.8 are independently selected from the group consisting of
- (i) hydrogen;
- (ii) --(C.sub.1 -to-C.sub.7 alkyl);
- (iii) --(C.sub.2 -to-C.sub.6 alkenyl);
- (iv) halogen;
- (v) --(CH.sub.2).sub.m NR.sup.11 R.sup.11' where m is an integer between one and ten, and R.sup.11 and R.sup.11' are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.12 -alkyl, aryl, aryl-C.sub.1 -C.sub.12 -alkyl, heterocyclic, (heterocyclic)-C.sub.1 -C.sub.12 -alkyl, (heterocyclic)-C.sub.2 -C.sub.12 -alkenyl and (heterocyclic)-C.sub.2 -C.sub.12 -alkynyl;
- (vi) --CN;
- (vii) --CHO;
- (viii) mono-, di-, tri- or perhalogenated --C.sub.1 -C.sub.12 -alkyl;
- (ix) --S(O).sub.s R.sup.11 where s is zero, one or two and R.sup.11 is defined as above;
- (x) --C(O)NR.sup.11 R.sup.11' wherein R.sup.11 and R.sup.11' are defined as above;
- (xi) --(CH.sub.2).sub.m OR.sup.11 wherein R.sup.11 is defined as above;
- (xii) --CH(OR.sup.12)(OR.sup.12'), where R.sup.12 and R.sup.12' are independently --(C.sub.1 -to-C.sub.3 alkyl) or, taken together, form an ethylene or propylene bridge;
- (xiii) --(CH.sub.2).sub.m OC(O)R.sup.11 wherein R.sup.11 is defined as above;
- (xiv) --(CH.sub.2).sub.m C(O)OR.sup.11 wherein R.sup.11 Is defined as above;
- (xv) --OR.sup.13, where R.sup.13 is selected from the group consisting of
- (A) --PO(OH)OH,
- (B) --SO.sub.3 H, and
- (C) --C(O)(CH.sub.2).sub.m C(O)OH;
- (xvi) --S(O).sub.t NR.sup.11 R.sup.11', where t is one or two and R.sup.11 and R.sup.11' are defined as above;
- (xvii) --NO.sub.2 ;
- (xviii) --N.sub.3 ; and
- (xviv) guanidino optionally substituted by a radical selected from the group consisting of C.sub.1 -C.sub.8 -loweralkyl, aryl, C.sub.1 -C.sub.12 -alkyl-C(O)--, aryl-C(O)--, arylsulfonyl, C.sub.1 -C.sub.8 -alkoxycarbonyl, aryl-C.sub.1 -C.sub.8 -alkoxycarbonyl, aryloxycarbonyl and C.sub.1 -C.sub.12 -alkylsulfonyl, or any two adjacent R.sup.6, R.sup.7 and R.sup.8 and the atoms to which they are attached form a carbocyclic or heterocyclic ring having between 5 and 7 ring atoms; and
- R.sup.14 is selected from the group consisting of (i) C.sub.1 -C.sub.12 -alkyl-C(O)-- or aryl-C(O)--; (ii) --(C.sub.1 -to-C.sub.7 alkyl); (iii) --(C.sub.2 -to-C.sub.6 alkenyl); (vi) --(CH.sub.2).sub.m NR.sup.11 R.sup.11', where m is an integer between one and ten and R.sup.11 and R.sup.11' are independently defined as above;
- (v) --S(O).sub.s R.sup.11, where s selected from the group consisting of zero, one and two and R.sup.11 is independently defined as above; (vi) --C(O)NR.sup.11 R.sup.11' wherein R.sup.11 and R.sup.11' are independently defined as above; (vii) --(CH.sub.2).sub.m OR.sup.11 wherein R.sup.11 is independently defined as above; (viii) --CH(OR.sup.12)(OR.sup.12') wherein R.sup.12 and R.sup.12' are independently defined as above; (ix) --(CH.sub.2).sub.m OC(O)R.sup.11 wherein R.sup.11 is independently defined as above; (x) --(CH.sub.2).sub.m C(O)OR.sup.11 wherein R.sup.11 is independently defined as above; and (xi) --S(O).sub.t NR.sup.11 R.sup.11', where t is selected from the group consisting of one and two and R.sup.11 and R.sup.11' are independently defined as above:
- wherein at each occurrence aryl Is independently selected from phenyl, 1-naphthyl, 2-naphthyl, fluorenyl, (1,2)-dihydronaphthyl, (1,2.3.4-)-tetrahydronaphthyl, indenyl and indanyl; and at each occurrence heterocyclic is independently selected from (i) an aromatic or non-aromatic 5-, 6- or 7-membered ring having, one, two or three heteroatoms independently selected from oxygen, sulfur and nitrogen, (ii) a bi- or tri-cyclic group comprising six-membered rings and having one, two or three heteroatoms independently selected from oxygen, sulfur and nitrogen or (iii) a 5-membered or 7-membered ring, heterocycle fused to a benzene ring; wherein in any heterocycle any of the nitrogen, sulfur and carbon atoms can be substituted with hydroxy, thiol, oxo or thioxo or any of the nitrogen atoms can be quaternized.
- 2. A compound according to claim 1 wherein R.sup.100 is hydrogen.
- 3. A compound according to claim 1 wherein R.sup.101 is ethyl.
- 4. A compound according to claim 1 wherein R.sup.102 is hydrogen.
- 5. A compound according to claim 1 wherein R.sup.103 is selected from the group consisting of hydrogen and hydroxyl.
- 6. A compound according to claim 1 wherein R.sup.103 is hydroxyl protected by a hydroxy-protecting group selected from tri(C.sub.1 -C.sub.8 -loweralkyl)silyl, C.sub.1 -C.sub.8 -loweralkyldiarylsilyl, triarylsilyl, tri(arylC.sub.1 -C.sub.12 -alkyl)silyl, triphenylmethyl-dimethylsilyl, trimethylsilylethoxycarbonyl, methylthiomethyoxyethoxycarbonyl, benzenesulfonylethoxycarbonyl, trimethylsilylethoxymethyl and aryl-C(O)--.
- 7. A compound according to claim 1 wherein R.sup.104 is hydrogen.
- 8. A compound according to claim 1 wherein m and n are integers independently selected from the group consisting of zero and one.
- 9. A compound according to claim 1 wherein R.sup.105 is a radical having the formula ##STR8## wherein X Is selected from the group consisting of --S(O).sub.s --, --C(R.sup.2)(R.sup.2')-- and --N(R.sup.1)-- wherein n, m, s, R.sup.1, R.sup.2, R.sup.2', R.sup.3, R.sup.4 and R.sup.5 are as defined therein.
- 10. A compound according to claim 9 wherein X is selected from the group consisting of --S(O).sub.s --, --C(R.sup.2)(R.sup.2') and --N(R.sup.1)-- wherein s, R.sup.1, R.sup.2 and R.sup.2' are as defined therein.
- 11. A compound according to claim 9 wherein R.sup.1, R.sup.3, R.sup.4 and R.sup.5 are independently selected from the group consisting of
- (a) hydrogen;
- (b) C.sub.1 -C.sub.12 -alkyl;
- (c) C.sub.3 -C.sub.8 -cycloalkyl;
- (d) C.sub.3 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.8 -alkyl;
- (e) hydroxy-C.sub.1 -C.sub.8 -alkyl;
- (f) hydroxyl-C.sub.1 -C.sub.8 -alkoxy-C.sub.1 -C.sub.12 -alkyl;
- (g) aryl substituted by R.sup.6, R.sup.7 and R.sup.8 ;
- (h) aryl-C.sub.1 -C.sub.12 -alkyl substituted by R.sup.6, R.sup.7 and R.sup.8 ;
- (i) C.sub.1 -C.sub.8 -alkoxycarbonyl;
- (j) C.sub.1 -C.sub.8 -alkoxycarbonyl-C.sub.1 -C.sub.12 alkyl;
- (k) carboxy-C.sub.1 -C.sub.8 -alkyl;
- (l) aminoalkyl of the formula (R.sup.403)(R.sup.404)N-C.sub.1 -C.sub.9 -alkyl wherein R.sup.403 and R.sup.404 are independently selected from hydrogen, C.sub.1 -C.sub.8 -alkyl, aryl and aryl-C.sub.1 -C.sub.12 -alkyl or R.sup.403 and R.sup.404, taken together, are --(CH.sub.2).sub.bb -- wherein bb is 2-6;;
- (m) C.sub.1 -C.sub.12 -thiolalkyl;
- (n) heterocyclic;
- (o) (heterocyclic)-C.sub.1 -C.sub.12 -alkyl;
- (p) (heterocyclic)-C.sub.1 -C.sub.12 -alkylamino-C.sub.1 -C.sub.8 -alkyl;
- (q) C.sub.1 -C.sub.12 -alkyl-C(O)-- or aryl-C(O)--;
- (r) N-mono- or N,N-dialkylaminoalkyl;
- (s) N-mono- or N,N-dialkyl-carboxamidoalkyl;
- (t) N-mono- or N,N-diarylcarboxamidoalkyl; and
- (u) formyl.
- 12. A compound according to claim 9 wherein X is selected from the group consisting of --N(R.sup.1)-- and --C(R.sup.2)(R.sup.2')-- wherein R.sup.2 and R.sup.2' are as defined therein.
- 13. A compound according to claim 9 wherein the total of the integers m and n is an integer selected from the group consisting of zero, one and two.
- 14. A compound of the formula: ##STR9## wherein one of R.sup.104 and R.sup.105 is hydrogen, and the other of R.sup.104 and R.sup.105 is a group having the formula ##STR10## wherein (a) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --(CH.sub.3)N--;
- (b) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --(benzyl)N--;
- (c) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --(phenyl)N--;
- (d) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(tert-butyloxycarbonyl)N--;
- (e) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--[4-nitrobenzyl]N--,
- (f) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(.beta.-naphthylmethyl(N--,
- (g) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--CH.sub.2 --;
- (h) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --(formyl)N--;
- (i) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --C(R.sup.2)(R.sup.2')-- wherein R.sup.2 and R.sup.2' taken together form --O(CH.sub.2).sub.i O-- wherein i=2;
- (j) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(2-hydroxyethyl)N--;
- (k) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=oxygen;
- (l) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(2-(2-hydroxyethoxy)ethyl)N--;
- (m) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(2-pyridyl)N--
- (n) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(2-pyrimidyl)N--;
- (o) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--NH--;
- (p) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=1-(--pyrrolidinocarbonylmethyl)N--;
- (q) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(1-morpholinocarbonylmethyl)N--;
- (r) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --(cyclopentyl)N--;
- (s) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(piperonyl)N--,
- (t) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(4-acetylphenyl)N--;
- (u) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --C(R.sup.2)(R.sup.2')-- wherein R.sup.2 =N-pyrrolino and R.sup.2' =H;
- (v) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(ethoxycarbonyl)N--;
- (w) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(acetyl)N--;
- (x) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(iso-propylaminocarbonylmethyl)N--;
- (y) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X is --C(R.sup.2) (R.sup.2')-- wherein R.sup.2 =hydroxy and R.sup.2' =H;
- (z) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=0; R.sup.4 =R.sup.5 =H; R.sup.3 =hydroxymethyl; and X is --CH.sub.2 --;
- (aa) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.4 =R.sup.5 =H; R.sup.3 =hydroxymethyl; and X is --CH.sub.2 --;
- (bb) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.4 =R.sup.5 =H; R.sup.4 =hydroxymethyl; and X is --CH.sub.2 --;
- (cc) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.4 =R.sup.5 =H; R.sup.3 =2-hydroxyethyl; and X is --CH.sub.2 --;
- (dd) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.5 =H; R.sup.4 =hydroxy; and X is --CH.sub.2 --; or
- (ee) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.4 =R.sup.5 =H; R.sup.3 =hydroxymethyl; and X is --CH.sub.2 --;
- or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.
- 15. A compound of the formula: ##STR11## wherein (a) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =R.sup.104 =dimethylthexylsilyloxy; and R.sup.105 =H;
- (b) R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =dimethylthexyl-silyloxy; and R.sup.105 =H; or
- R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =dimethylthexylsilyloxy; R.sup.104 =OH; R.sub.10 =H.
- 16. A compound of the formula: ##STR12## wherein one of R.sup.104 and R.sup.105 is hydrogen, and the other of R.sup.104 and R.sup.105 is a group having the formula ##STR13## wherein R.sup.100 =H; R.sup.101 =ethyl; R.sup.102 =H; R.sup.103 =OH; R.sup.104 =H; m=0; n=1; R.sup.3 =R.sup.4 =R.sup.5 =H; and X=--(acetyl)N--;
- or a pharmaceutically acceptable salt, ester, amide or prodrug thereof.
Parent Case Info
This application is a continuation of U.S. patent application Ser. No. 08/099,975, filed Jul. 30, 1993, now abandoned, which is a continuation-in-part of the U.S. patent application Ser. No. 08/032,958, filed on Mar. 17, 1993, now abandoned.
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Continuations (1)
|
Number |
Date |
Country |
Parent |
99975 |
Jul 1993 |
|
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
32958 |
Mar 1993 |
|