Claims
- 1. A compound of formula I: ##STR41## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is selected from:
- 1) --N.sub.3 ;
- 2) --NHCN;
- 3) --NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 independently, are,
- a) hydrogen,
- b) C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are independently selected from the group consisting of:
- i) hydrogen,
- ii) --OH,
- iii) C.sub.1 -C.sub.6 alkoxy,
- iv) --O--CO--C.sub.1 -C.sub.6 alkyl,
- v) --NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are independently, hydrogen, or C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted with phenyl
- vi) --CONR.sup.10 R.sup.11,
- vii) --CO.sub.2 H,
- viii) --CO--O--C.sub.1 -C.sub.6 alkyl,
- ix) --S--C.sub.1 -C.sub.6 alkyl,
- x) --SO--C.sub.1 -C.sub.6 alkyl,
- xi) --SO.sub.2 --C.sub.1 -C.sub.6 alkyl,
- xii) halo,
- xiii) --C.sub.3 -C.sub.7 -cycloalkyl,
- xiv) phenyl, unsubstituted or substituted with X, Y and Z,
- xv) naphthyl, unsubstituted or substituted with X, Y and Z,
- xvi) --CF.sub.3,
- c) C.sub.3 -C.sub.12 alkenyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above,
- d) C.sub.3 -C.sub.7 cycloalkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above,
- e) phenyl, unsubstituted or substituted with X, Y and Z,
- f) naphthyl, unsubstituted or substituted with X, Y and Z,
- f) --SO.sub.2 -phenyl, wherein phenyl is unsubstituted or substituted with X, Y and Z,
- h) --SO.sub.2 --C.sub.1 -C.sub.6 alkyl,
- i) or where R.sup.6 and R.sup.7 and the N to which they are attached may form a heterocyclic ring, selected from the group consisting of: morpholine, thiomorpholine, piperidine, and piperazine, and where the substituent(s), attached to the carbon atom(s) in the heterocyclic ring is/are independently selected from the group consisting of:
- i) hydrogen,
- ii) --OH,
- iii) C.sub.1 -C.sub.6 alkoxy,
- iv) --O--CO--C.sub.1 -C.sub.6 alkyl,
- v) --NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are independently, hydrogen, or C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted with phenyl,
- vi) --CONR.sup.10 R.sup.11,
- vii) --CO.sub.2 H,
- viii) --CO--O--C.sub.1 -C.sub.6 alkyl,
- ix) --SH,
- x) halo,
- xi) phenyl, unsubstituted or substituted with X, Y and Z,
- xii) naphthyl, unsubstituted or substituted with X, Y and Z,
- xiii) --CF.sub.3 ;
- 4) --N(R.sup.6)CO--O--R.sup.12, wherein R.sup.6 is as defined above and R.sup.12 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above;
- 5) --N(R.sup.6)CO--R.sup.13, wherein R.sup.6 is as defined above and R.sup.13 is
- a) hydrogen,
- b) C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above,
- c) C.sub.3 -C.sub.12 cycloalkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above,
- d) phenyl, unsubstituted or substituted with X, Y and Z,
- e) naphthyl, unsubstituted or substituted with X, Y and Z, or
- f) where R.sup.6 and R.sup.13 and the --NCO-- to which they are attached may form a heterocyclic ring selected from the group consisting of: pyrrolidone, and piperidinone;
- 6) --N(R.sup.14)COCH(R.sup.22)NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 are as defined above, R.sup.14 is selected from the definitions of R.sup.6, and R.sup.22 is
- a) hydrogen,
- b) C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted with R.sup.23 wherein R.sup.23 is selected from the group consisting of:
- i) --OH,
- ii) C.sub.1 -C.sub.6 alkoxy,
- iii) --O--CO--C.sub.1 -C.sub.6 alkyl,
- iv) --SH,
- v) --S--C.sub.1 -C.sub.6 alkyl,
- vi) --NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are as defined above,
- vii) --CO.sub.2 H,
- viii) --CONH.sub.2,
- ix) imidazolyl,
- x) indolyl,
- xi) phenyl, and
- xii) p-hydroxyphenyl, or,
- c) phenyl;
- 7) --N(R.sup.14)CO(CH.sub.2).sub.m NR.sup.6 R.sup.7, wherein m is 0 or 2-6, R.sup.6 and R.sup.7 are as defined above, and R.sup.14 is selected from the definitions of R.sup.6, or where R.sup.14 and R.sup.6 and the --NCO(CH.sub.2).sub.m N-- to which they are attached may form a heterocyclic ring, which is 2-imidazolidone;
- 8) --N.dbd.C(R.sup.14)--NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 are as defined above, and R.sup.14 is selected from the definitions of R.sup.6, and wherein if either R.sup.6 or R.sup.7 are hydrogen, the tautomeric structure --NHC(R.sup.14).dbd.NR.sup.6or7 is also possible;
- 9) --N(R.sup.15).sub.3 +A.sup.-, wherein R.sup.15 is C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted with phenyl or naphthyl, and wherein A.sup.- is a counterion selected from the group consisting of: acetate, adipate, benzoate, benzenesulfonate, bisulfate, butyrate, citrate, camphorate, camphorsulfonate, ethanesulfonate, fumarate, hemisulfate, hemitartrate, heptanoate, hexanoate, hydrochloride, hydrobromide, hydroiodide, methanesulfonate, lactate, maleate, methanesulfonate, 2-naphthalenesulfonate, nitrate oxalate, pamoate, perchlorate, persulfate, picrate, pivalate, propionate, succinate, tartrate, tosylate, and undecanoate;
- 10) ##STR42## wherein R.sup.16 and R.sup.17 are independently, a) hydrogen,
- b) phenyl, unsubstituted or substituted with X, Y and Z,
- c) naphthyl, unsubstituted or substituted with X, Y and Z,
- d) --CN,
- e) --CF.sub.3,
- f) --CO--C.sub.1 -C.sub.6 alkyl, or
- g) --CO--O--C.sub.1 -C.sub.6 alkyl;
- R.sup.2 is selected from:
- 1) phenyl;
- 2) substituted phenyl in which the substituents are X, Y and Z;
- 3) 1- or 2- naphthyl;
- 4) substituted 1- or 2-naphthyl in which the substituents are X, Y and Z;
- 5) biphenyl;
- 6) substituted biphenyl in which the substituents are X, Y and Z;
- R.sup.3 is hydrogen, hydroxy, or C.sub.1 -C.sub.6 alkoxy;
- R.sup.4 is hydrogen, or R.sup.3 and R.sup.4 taken together form a double bond;
- R.sup.5 is methyl, ethyl, propyl or allyl;
- W is O or (H, OH);
- X, Y and Z independently are selected from:
- a) hydrogen,
- b) C.sub.1-7 alkyl,
- c) C.sub.2-6 alkenyl,
- d) halo,
- e) --(CH.sub.2).sub.p --NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are, independently, hydrogen or C.sub.1-6 alkyl, unsubstituted or substituted with phenyl and p is 0 to 2,
- f) --CN,
- g) --CHO,
- h) --CF.sub.3,
- i) --SR.sup.18, wherein R.sup.18 is hydrogen, C.sub.1-6 alkyl, or phenyl,
- j) --SOR.sup.18, wherein R.sup.18 is as defined above,
- k) --SO.sub.2 R.sup.18, wherein R.sup.18 is as defined above,
- l) --CONR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are as defined above,
- m) R.sup.19 O(CH.sub.2).sub.p -- wherein R.sup.19 is hydrogen, C.sub.1-3 alkyl, hydroxy-C.sub.2-3 alkyl, phenyl or naphthyl and p is as defined above;
- n) --CH(OR.sup.20)(OR.sup.21), wherein R.sup.20 and R.sup.21 are C.sub.1-3 alkyl or taken together form an ethyl or propyl bridge,
- o) ##STR43## wherein R.sup.19 and p are as defined above, and p) ##STR44## wherein R.sup.19 and p are as defined above; or any two of X, Y and Z may be joined to form a saturated ring selected from the group consisting of: dihydropyranyl, dihydrofuranyl, dioxolanyl and dioxanyl; and
- n is 1 or 2.
- 2. The compound according to claim 1 wherein the steric configuration of formula I is as defined in formula III: ##STR45##
- 3. The compound according to claim 1 wherein:
- R.sup.1 is selected from:
- 1) --N.sub.3 ;
- 3) --NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 independently, are,
- a) hydrogen,
- b) C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are independently selected from the group consisting of:
- i) hydrogen,
- ii) --OH,
- iii) --O--CO--C.sub.1 -C.sub.6 alkyl,
- iv) --NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are independently, hydrogen, or C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted with phenyl
- v) --CONR.sup.10 R.sup.11,
- vi) --CO.sub.2 H,
- vii) --CO--O--C.sub.1 -C.sub.6 alkyl,
- viii) phenyl, unsubstituted or substituted with X, Y and Z,
- c) C.sub.3 -C.sub.12 alkenyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above;
- 3) --N(R.sup.6)CO--O--R.sup.12, wherein R.sup.6 is as defined above and R.sup.12 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above;
- 4) --N(R.sup.6)CO--R.sup.13, wherein R.sup.6 is as defined above and R.sup.13 is
- a) hydrogen,
- b) C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above,
- c) C.sub.3 -C.sub.12 cycloalkyl, unsubstituted or substituted with R.sup.8 and R.sup.9, wherein R.sup.8 and R.sup.9 are as defined above,
- d) phenyl, unsubstituted or substituted with X, Y and Z,
- 5) --N(R.sup.14)COCH(R.sup.22)NR.sup.6 R.sup.7 wherein R.sup.6 and R.sup.7 are as defined above, R.sup.14 is selected from the definitions of R.sup.6, and R.sup.22 is
- a) hydrogen,
- b) C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted with R.sup.23 wherein R.sup.23 is selected from the group consisting of:
- i) --OH,
- ii) C.sub.1 -C.sub.6 alkoxy,
- iii) --O--CO--C.sub.1 -C.sub.6 alkyl,
- iv) --SH
- v) --S--C.sub.1 -C.sub.6 alkyl,
- vi) --NR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are as defined above,
- vii) --CO.sub.2 H,
- viii) --CONH.sub.2,
- ix) imidazolyl,
- x) indolyl,
- xi) phenyl, and
- xii) p-hydroxyphenyl, or
- c) phenyl,
- 6) --N(R.sup.14)CO(CH.sub.2).sub.m NR.sup.6 R.sup.7, wherein m is 0 or 2-6, R.sup.6 and R.sup.7 are as defined above, and R.sup.14 is selected from the definitions of R.sup.6, or where R.sup.14 and R.sup.6 and the --NCO(CH.sub.2).sub.m N-- to which they are attached may form a heterocyclic ring, which is 2-imidazolidone;
- 7) --N.dbd.C(R.sup.14)--NR.sup.6 R.sup.7, wherein R.sup.6 and R.sup.7 are as defined above, and R.sup.14 is selected from the definitions of R.sup.6, and wherein if either R.sup.6 and R.sup.7 are hydrogen, the tautomeric structure --NHC(R.sup.14).dbd.NR.sup.6or7 is also possible;
- 8) --N(R.sup.15).sub.3.sup.+ A.sup.-, wherein R.sup.15 is C.sub.1 -C.sub.6 alkyl, unsubstituted or substituted with phenyl or naphthyl, and wherein A.sup.- is a counterion selected from the group consisting of: acetate, adipate, benzoate, benzenesulfonate, bisulfate, butyrate, citrate, camphorate, camphorsulfonate, ethanesulfonate, fumarate, hemisulfate, hemitartrate, heptanoate, hexanoate, hydrochloride, hydrobromide, hydroiodide, methanesulfonate, lactate, maleate, methanesulfonate, 2-naphthalenesulfonate, nitrate oxalate, pamoate, perchlorate, persulfate, picrate, pivalate, propionate, succinate, tartrate, tosylate, and undecanoate;
- 9) ##STR46## wherein R.sup.16 and R.sup.17 are independently, a) hydrogen,
- b) phenyl, unsubstituted or substituted with X, Y and Z,
- c) naphthyl, unsubstituted or substituted with X, Y and Z,
- d) --CN,
- e) --CF.sub.3,
- f) --CO--C.sub.1 -C.sub.6 alkyl, or
- g) --CO--O--C.sub.1 -C.sub.6 alkyl;
- R.sup.2 is selected from:
- 1) phenyl;
- 2) substituted phenyl in which the substituents are X, Y and Z;
- 3) 1- or 2-naphthyl;
- 4) substituted 1- or 2-naphthyl in which the substituents are X, Y and Z;
- R.sup.3 is hydrogen or hydroxy;
- R.sup.4 is hydrogen;
- R.sup.5 is ethyl, propyl or allyl;
- W is O or (H, OH);
- X, Y and Z independently are selected from:
- a) hydrogen,
- b) C.sub.1-7 alkyl,
- c) halo,
- d) --CN,
- e) --CHO,
- f) --CF.sub.3,
- g) --CONR.sup.10 R.sup.11, wherein R.sup.10 and R.sup.11 are as defined above,
- h) R.sup.19 O(CH.sub.2).sub.p -wherein R.sup.19 is hydrogen, C.sub.1-3 alkyl, hydroxy-C.sub.2-3 alkyl, phenyl or naphthyl and p is 0 to 2;
- i) --CH(OR.sup.20)(OR.sup.21), wherein R.sup.20 and R.sup.21 are C.sub.1-3 alkyl or taken together form an ethyl or propyl bridge,
- j) ##STR47## wherein R.sup.19 and p are as defined above; k) ##STR48## wherein R.sup.19 and p are as defined above; or any two of X, Y and Z may be joined to form a saturated ring, selected from the group consisting of: dihydropyranyl, dihydrofuranyl, dioxolanyl and dioxanyl; and
- n is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
- 4. A compound which is selected from:
- 17-allyl-1,14-dihydroxy-12-[2'-(4"-amino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-allyl-1-hydroxy-12-[2'-(4"-amino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1,14-dihydroxy-12-[2'-(4"-amino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-phenoxy-3"-aminocyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-dimethylamino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo-[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4'"-methoxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo-[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4'"-hydroxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo-[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-acetylamino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4'"-fluorophenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1,14-dihydroxy-12-[2'-(4"-amino-3"-(4'"-carboxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4'"-trifluoromethylphenoxy)cyclohexyl)-1'-methylvinyl]23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(3'",4'"-dimethoxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-allyl-1,14-dihydroxy-12-[2'-(4"-amino-3"-(4'"-methoxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4'"-methylphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1,14-dihydroxy-12-[2'-(4"-amino-3"-(4'"-methylphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(3'"-methoxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(3'"-hydroxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-N-(2-propenyl)amino-3"-phenoxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone; and
- 17-ethyl-1-hydroxy-12-[2'-(4"-(acetylamino-3"-4'"-methoxyphenoxy)cyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2"'R-hydroxypropyl)amino-3"-phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2"'S-hydroxypropyl)amino-3"-phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2""R-hydroxypropyl)amino-3"-(4"'-methyl)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetra-methyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2""S-hydroxypropyl)amino-3"-(4"'-methyl)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetra-methyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2""R-hydroxypropyl)amino-3"-(4"'-methoxy)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetra-methyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2""S-hydroxypropyl)amino-3"-(4"'-methoxy)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetra-methyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2"'R-hydroxypropyl)amino-3"-allyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-(2"'S-hydroxypropyl)amino-3"-allyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-dimethylamino-3"-(3"-methoxy)phenyloxycyclohexyl)-1'-methylvinyl]23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-azido-3"-(4"'-dimethylamino)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4"'-dimethylamino)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4"'-methyl)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4"'-hydroxymethyl)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4"'-methoxy)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(3"'-methoxy)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4"'-hydroxy)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- 17-ethyl-1-hydroxy-12-[2'-(4"-amino-3"-(4"'-formyl)phenyloxycyclohexyl)-1'-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0.sup.4,9 ]-octacos-18-ene-2,3,10,16-tetraone;
- and pharmaceutically acceptable salts thereof.
- 5. The compound of claim 4 which is: ##STR49##
- 6. The compound of claim 4 which is: ##STR50##
- 7. The compound of claim 4 which is: ##STR51##
- 8. The compound of claim 4 which is: ##STR52##
- 9. The compound of claim 4 which is: ##STR53##
- 10. The compound of claim 4 which is: ##STR54##
- 11. The compound of claim 4 which is: ##STR55##
- 12. The compound of claim 4 which is: ##STR56##
- 13. The compound of claim 4 which is: ##STR57##
- 14. The compound of claim 4 which is: ##STR58##
- 15. The compound of claim 4 which is: ##STR59##
- 16. The compound of claim 4 which is: ##STR60##
Parent Case Info
This application is a continuation-in-part of copending application Ser. No. 07/698,889, filed May 13, 1991 now abandoned.
US Referenced Citations (8)
Foreign Referenced Citations (8)
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Tanaka, et al., J. Am. Chem. Soc., 1987, 109 5031-5033. |
Continuation in Parts (1)
|
Number |
Date |
Country |
Parent |
698889 |
May 1991 |
|