Abstract: A compound of the structure ##STR1## where the substituents are defined in the specification.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.6 R.sup.7).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, --OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each, independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each, independently, hydrogen or alkyl;R.sup.17 is ##STR3## or --C.tbd.C--R.sup.21 ; R.sup.18, R.sup.19, R.sup.20, and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, or --CONH--O--(CR.sup.3 R.sup.4).sub.m Z;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, cycloalkyl, --CF.sub.3, or F;Z is hydrogen, alkyl, --OR.sup.5, --SR.sup.5, --NR.sup.5 R.sup.6, --CN, --CF.sub.3, --OAr, --Ar, or R.sup.7 ;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, or Ar;R.sup.7 is ##STR2## or --C.tbd.C--R.sup.11 ; R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, halogen, or phenyl, wherein the phenyl group may be optionally mono-, di-, or tri-substituted;Ar is an aryl radical that may be optionally mono-, di-, or tri-substituted; andm=1-6;with the proviso that R.sup.1 and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONR.sup.3 (CR.sup.4 R.sup.5).sub.m (CR.sup.4 R.sup.5).sub.n (CR.sup.8 R.sup.9).sub.p NR.sup.10 R.sup.11, or ##STR2## --R.sup.12, or --CONR.sup.3 R.sup.13 ; R.sup.3 is hydrogen, alkyl, or arylalkyl;R.sup.4, R.sup.5, R.sup.8, and R.sup.9 are each, independently, hydrogen, alkyl, p--OH, --CF.sub.3, or --F;R.sup.6 is hydrogen or --OR.sup.13 ;R.sup.7 is hydrogen or alkyl;R.sup.10 is hydrogen, alkyl, or arylalkyl;R.sup.11, R.sup.12, and R.sup.13 are each independently, --(CR.sup.15 R.sup.16).sub.r R.sup.17 ;R.sup.14 is hydrogen, alkyl of 1-6 carbon atoms, tri-(alkyl)silyl, Tri-(alkyl)silyethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, or tetrahydropyranyl;R.sup.15 and R.sup.16 are each independently, hydrogen or alkyl; ##STR3## R.sup.18, R.sup.19, R.sup.20, and R.sup.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2,R.sup.3, R.sup.4, R.sup.5, R.sup.6, B,R.sup.7 and R.sup.8,R.sup.9 and R.sup.10,are each defined in the specification or a pharmaceutically acceptable salt their, of which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, hydrogen, ##STR2## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, alkenyl, alkynyl. --CO.sub.2 R.sup.5, --COR.sup.5, --CN, --NO.sub.2, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --OR.sup.5, --SR.sup.5, or Ar;R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, --CF3, --NR.sup.5 R.sup.6, --CO.sub.2 R.sup.5, --COR.sup.5, CONR.sup.5 R.sup.6, --NO.sub.2, halogen, --OR.sup.5, --SR.sup.5, --CN, --SO.sub.2 R.sup.5, --SO.sub.3 R.sup.5, --SO.sub.2 NR.sup.5 R.sup.6, or Ar;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, or Ar; ##STR3## are each, independently, a 5-7 membered saturated, unsaturated, or partially unsaturated heterocyclic radical, that is optionally fused to a phenyl ring or a cycloalkane or cycloalkene ring, wherein the heterocyclic ring may optionally contain O, S, or NR.sup.8 in the heterocyclic ring, and may be optionally substituted by R.sup.7 ;R.sup.

Abstract: A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen;R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl;Y.sup.- =halide, methanesulfonate, toluene sulfonate or maleate: andZ=oxygen or OH and H.which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: A compound of the structure ##STR1## where the substituents are defined in the main body of the specification which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH.sub.a --{{(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p }.sub.q --B}.sub.r ; --SO.sub.2 R.sup.7 ; --SO.sub.3 H; --CHR.sup.8 O(CH.sub.2).sub.t R.sup.9 ; or ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.10, --SR.sup.10, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.10, --CO.sub.2 R.sup.10, --CONHR.sup.10, --SO.sub.2 R.sup.10, --OSO.sub.3 R.sup.10, --NR.sup.10 R.sup.11, --NHCOR.sup.10, --NHSO.sub.2 R.sup.10, or Ar;X is .dbd.NOR.sup.12 or .dbd.NNR.sup.12 R.sup.13 ;Y is O, .dbd.NOR.sup.12, or .dbd.NNR.sup.12 R.sup.13 ;R.sup.7, R.sup.12, and R.sup.13 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, arylalkyl;R.sup.8, R.sup.9, R.sup.10, and R.sup.

Abstract: A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## or hydrogen; R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen; R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl;Y-=halide, methanesulfonate, toluene sulfonate or maleate; andZ=oxygen or OH and H.which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: The invention concerns compounds of formula (I) ##STR1## where R.sup.1 is alkyl, haloalkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from phenyl, naphthyl and 4-(phenylaza) phenyl wherein said aromatic group is optionally substituted by one or more substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.6) thioalkyl, halo, cyano, nitro, trifuluoromethyl, trifluoromethoxy or R.sup.1 is a heteroaromatic group of 5 to 10 ring atoms containing oxygen, nitrogen and/or sulfur as heteroatom(s) wherein said heteroaromatic group is optionally substituted by one or more substituents selected form C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, --CONH--[(CR.sup.3 R.sup.4).sub.m (--A--(CR.sup.5 R.sup.6).sub.n).sub.p ].sub.q --B; ##STR2## R.sup.3, R.sup.4, R.sup.5, R.sup.6, and B are each, independently, hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, cycloalkyl, --OR.sup.7, --SR.sup.7, halogen, --CN, --NO.sub.2, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.2 R.sup.7, --OSO.sub.3 R.sup.7, --NR.sup.7 R.sup.8, --NHCOR.sup.7, --NHSO.sub.2 R.sup.7, or Ar;R.sup.7 and R.sup.8 are each, independently, hydrogen, alkyl, arylalkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl;R.sup.9 and R.sup.10 are each, independently, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, arylalkyl, --CF.sub.3, --COR.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, --SO.sub.

Abstract: N-arylcarbonyl and N-alkylcarbonyl carbamates of rapamycin of the formula shown below wherein ##STR1## R.sup.1 and R.sup.2 are both ##STR2## and where A is lower alkoxy or aryl or heteroaryl, R.sup.3 is H or methyl and R.sup.4 is C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl possess immunosuppressive and/or antifungal and/or antitumor and/or antiinflammatory activity in vitro and/or inhibit thymocyte proliferation in vivo. These compounds are thus expected to be useful in the treatment of transplantation rejection, autoimmune diseases, fungal infections, cancer, and diseases of inflammation.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONHSO.sub.2 --Ar; andAr is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, or benzodioxolyl; wherein the Ar group may be optionally mono-, di-, or tri-substituted; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen;or a pharmaceutically acceptable salt thereof which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.

Abstract: A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONHSO.sub.2 -Ar; andAr is phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, quinoxalyl, thienyl, thionaphthyl, furyl, benzofuryl, benzodioxyl, benzoxazolyl, benzoisoxazolyl, or benzodioxolyl; wherein the Ar group may be optionally mono-, di, or tri-substituted; with the provision that R.sup.1 and R.sup.2 are not hydrogen; oror a pharmaceutically acceptable salt thereof which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs. graft disease, autoimmune diseases and diseases of inflammation; by virtue of its antitumor activity is useful in treating solid tumors; and by virtue of its antifungal activity is useful in treating fungal infections.

Abstract: A derivative of rapamycin of general formula (I) ##STR1## where R.sup.1 is alkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from the group consisting of phenyl and naphthyl or a heterocyclic moiety selected from the group consisting of thiophenyl and quinolinyl or NHCO.sub.2 R.sup.2 wherein R.sup.2 is lower alkyl containing 1 to 6 carbon atoms or a pharmaceutically acceptable salt thereof, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: A rapamycin dimer of general formula (1) ##STR1## wherein A is --(CH.sub.2).sub.n --, --(CH.sub.2)n--(CH.dbd.CH)--(CH.sub.2).sub.m --, --(CH.sub.2)n--(--C.tbd.C--)--(CH.sub.2).sub.m --, ##STR2## substituted alkyl, substituted alkenyl, substituted alkynyl, and substituted aromatic; n=1-10, m=1-10 and n=m or n .noteq.mor a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: A bicyclic derivative of rapamycin of general formula (1) ##STR1## wherein ##STR2## n=2 to 10, m=2 to 10 andn=m or n.noteq.mor a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.