Patents by Inventor Amedeo Failli
Amedeo Failli has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
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Patent number: 5484790Abstract: 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.Type: GrantFiled: May 24, 1995Date of Patent: January 16, 1996Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Oleg I. Bleyman, Wenling Kao, Magid A. Abou-Gharbia
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Patent number: 5480988Abstract: 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.Type: GrantFiled: August 2, 1994Date of Patent: January 2, 1996Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Oleg I. Bleyman, Wenling Kao, Magid A. Abou-Gharbia
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Patent number: 5446048Abstract: A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, or Ar;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.Type: GrantFiled: September 21, 1994Date of Patent: August 29, 1995Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan, Craig E. Caufield, David C. Hu, Alexander A. Grinfeld
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Patent number: 5420289Abstract: This invention relates to substituted indole derivatives possessing lipoxygenase inhibitory, phospholipase A.sub.2 inhibitory and leukotriene antagonist activity, which are useful as anti-inflammatory, antiallergic and cytoprotective agents.Type: GrantFiled: March 10, 1993Date of Patent: May 30, 1995Assignee: American Home Products CorporationInventors: John H. Musser, Anthony F. Kreft, III, Amedeo A. Failli, Christopher A. Demerson, Uresh S. Shah, James A. Nelson
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Patent number: 5389639Abstract: This invention provides a compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## R.sup.3 is --(CH.sub.2).sub.q CO.sub.2 R.sup.6 ;R.sup.4 is hydrogen, alkyl, or arylalkyl;R.sup.5 is hydrogen or COOR.sup.7 ;R.sup.6 is hydrogen, alkyl, alkenyl, arylalkyl, fluorenylmethyl, or phenyl which is optionally substituted;R.sup.7 is alkyl, alkenyl, arylalkyl, fluorenylmethyl, or phenyl which is optionally substituted;m is 0-4;n is 0-4;p is 1-2;q is 0-4;wherein R.sup.3, R.sup.4, m, and n are independent in each of the ##STR3## subunits when p=2; with the proviso that R.sup.1 and R.sup.2 are not both hydrogen; and further provided that if R.sup.5 is CO.sub.2 R.sup.7, then R.sup.6 is hydrogen; and still further provided that if R.sup.6 is not hydrogen, then R.sup.5 is hydrogen;or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: December 29, 1993Date of Patent: February 14, 1995Assignee: American Home Products CompanyInventors: Amedeo A. Failli, Robert J. Steffan
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Patent number: 5373014Abstract: A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.3 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or --CO.sub.2 R.sup.8 ;R.sup.4 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, Ar, aminoalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, or --CO.sub.2 R.sup.8 ;R.sup.5 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, At, or --CO.sub.2 R.sup.8 ;R.sup.6 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.7 is alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, or Ar;R.sup.8 is hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, arylalkyl, fluorenylmethyl, orAr;Y is O or S;X is .dbd.N--O--(CH.sub.2).sub.f --Z or .dbd.N--O--Ar;Z is hydrogen, alkenyl, alkynyl, alkoxy, cyano, fluoro, trifluoromethyl, --NR.sup.5 R.sup.Type: GrantFiled: October 8, 1993Date of Patent: December 13, 1994Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan, Craig E. Caufield, David C. Hu, Alexander A. Grinfeld
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Patent number: 5364944Abstract: There are disclosed substituted benzoylbenzene-, biphenyl- and 2-oxazole- alkanoic acid derivatives and the pharmacologically acceptable salts thereof as inhibitors of PLA.sub.2 and lipoxygenase, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.Type: GrantFiled: January 6, 1993Date of Patent: November 15, 1994Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
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Patent number: 5346893Abstract: 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.Type: GrantFiled: May 19, 1993Date of Patent: September 13, 1994Assignee: American Home Products CorporationInventors: Amedeo Failli, Wenling Kao, Robert J. Steffan, Robert L. Vogel
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Patent number: 5260299Abstract: 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.Type: GrantFiled: July 21, 1992Date of Patent: November 9, 1993Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Wenling Kao, Robert J. Steffan, Robert L. Vogel
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Patent number: 5252579Abstract: This invention provides a compound of the structure ##STR1## wherein X is selected from the group consisting of --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m S--, --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m O--, --OCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m O--, --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.p --, --OCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.p --, --NR.sup.1 CR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m NR.sup.6 --, --OCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m NR.sup.6 --, --SCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m NR.sup.6 --, --SCR.sup.2 R.sup.3 (CR.sup.4 R.sup.5).sub.m S--, --NOR.sup.1 --, and --NR.sup.1 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are each, independently, hydrogen, alkyl, fluorine, trifluoromethyl, aryl, arylalkyl, or any pair taken together to form a 3-6 membered ring;m=1-6; andp=0-6or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflamatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: February 16, 1993Date of Patent: October 12, 1993Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Amedeo A. Failli, Robert J. Steffan, Robert M. Kearney
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Patent number: 5229516Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O-BwhereinA is C.sub.4 -C.sub.8 alkyl, phenoxyethyl, phenoxyphenyl or a group having the formula ##STR1## wherein ##STR2## R.sup.1 is hydrogen, lower alkyl, phenyl or phenyl substituted with trifluoromethyl;R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring;R.sup.3 is hydrogen or lower alkyl;n is 1-2;B is ##STR3## wherein ##STR4## m is 0-3; R.sup.5 is ##STR5## or phenyl or phenyl substituted by halo, lower alkylthio, lower alkylsulfinyl or lower alkylsulfonyl;R.sup.6 is A(CH.sub.2).sub.n O-- or halo; with the proviso that when R.sup.6 is halo, R.sup.5 is ##STR6## R.sup.7 is lower alkyl; Y is --CH.sub.2 -- or --O--;R.sup.8 is lower alkyl or --(CH.sub.2).sub.m CO.sub.2 R.sup.3 ;R.sup.9 is ##STR7## or --CH.sub.2 R.sup.10 ; R.sup.10 is lower alkyl, phenyl, phenyl substituted with carboxy, halo, loweralkylthio or loweralkylsulfinyl, pyridyl, furanyl or quinolinyl;R.sup.Type: GrantFiled: July 10, 1992Date of Patent: July 20, 1993Assignee: American Home Products CorporationInventors: John H. Musser, Anthony F. Kreft, III, Amedeo A. Failli, Christopher A. Demerson, Uresh S. Shah, James A. Nelson
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Patent number: 5218124Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is a group having the formula ##STR1## wherein X is --N-- or ##STR2## Z is ##STR3## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, with the proviso that when X is --N--, Z is other than ##STR4## R.sup.3 is hydrogen or lower alkyl; n is 1-2;B is ##STR5## wherein Y is OR.sup.5 or N(OH)R.sup.8 ;R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro;R.sup.7 is ##STR6## R.sup.Type: GrantFiled: June 1, 1992Date of Patent: June 8, 1993Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
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Patent number: 5177203Abstract: 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.Type: GrantFiled: March 5, 1992Date of Patent: January 5, 1993Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Wenling Kao, Robert J. Steffan, Robert L. Vogel
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Patent number: 5164399Abstract: A compound of the structure ##STR1## wherein Z is ##STR2## and R.sup.1 is hydrogen, alkyl, or arylalkyl, provided that when R.sup.2 is present, R.sup.1 is absent;R.sup.2 is hydrogen, alkyl, or arylalkyl, provided that when R.sup.1 is present, R.sup.2 is absent;the dotted lines in the pyrazole ring represent double bonds between the 31- and 32-positions and between the 33- and 53-positions when R.sup.1 is present and double bonds between the 31- and 52-positions and between the 32- and 33-positions when R.sup.2 is present;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 antifungal activity is useful in treating fungal infections; and by virtue of its antitumor activity is useful in treating tumors. Intermediates possessing a 31,33-.beta.-dicarbonyl moiety that are useful for the same purposes are also described.Type: GrantFiled: November 18, 1991Date of Patent: November 17, 1992Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan
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Patent number: 5162333Abstract: A compound of the structure ##STR1## wherein R.sup.1 is ##STR2## R.sup.3 is hydrogen, alkyl, arylalkyl, (CH.sub.2).sub.s NR.sup.4 R.sup.5, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenylmethyl, imidazolylmethyl or phenyl which is optionally mono-, di-, or tri-substituted;R.sup.4 is hydrogen, alkyl, or aralkyl;R.sup.2 and R.sup.5 are each independently hydrogen, formyl, alkanoyl, arylalkanoyl, aryloyl, or CO.sub.2 R.sup.6 ;R.sup.6 is alkyl, arylalkyl, allyl, fluorenylmethyl, or phenyl which is optionally mono-, di-, or tri-substituted;m is 0-4; n is 0-4; p is 0-1; q is 0-4; r is 0-4; and s is 0-4; 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 antifungal activity is useful in treating fungal infections; and by virtue of its antitumor activity is useful in treating tumors.Type: GrantFiled: September 11, 1991Date of Patent: November 10, 1992Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan
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Patent number: 5159085Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydroxy, lower alkoxy or lower alkoxyamino;R.sup.1 is hydrogen or A(CH.sub.2).sub.n O--;R.sup.2 is hydrogen or A(CH.sub.2).sub.n O--, with the proviso that one of R.sup.1 and R.sup.2 is hydrogen;n is 1-2;A is phenoxyethyl, phenoxyphenyl or a group having the formula ##STR2## R.sup.3 is hydrogen, lower alkyl or phenyl; R.sup.4 is hydrogen or lower alkyl; orR.sup.3 and R.sup.4 taken together form a benzene ring;R.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or lower alkyl;and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastic cytoprotective agents.Type: GrantFiled: April 4, 1991Date of Patent: October 27, 1992Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser
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Patent number: 5130307Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## with the proviso that R.sup.1 and R.sup.2 are not both hydrogen; R.sup.3 is hydrogen, alkyl, aralkyl, --(CH.sub.2).sub.q CO.sub.2 R.sup.6,--(CH.sub.2).sub.r NR.sup.7 CO.sub.2 R.sup.8, carbamylalkyl, aminoalkyl, hydroxyalkyl, guanylalkyl, mercaptoalkyl, alkylthioalkyl, indolylmethyl, hydroxyphenyklmethyl, imidazoylmethyl or phenyl which is optionally mono-, di-, or tri-substituted with a sustituent selected from alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, amino, or a carboxylic acid;R.sup.4 and R.sup.7 are each, independently, hydrogen, alkyl, or aralkyl;R.sup.5, R.sup.6, and R.sup.Type: GrantFiled: February 19, 1991Date of Patent: July 14, 1992Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Craig E. Caufield, Robert J. Steffan
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Patent number: 5128363Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a trifluoromethoxy substituent in the 5-, 6-, 7-, or 8-position, and methods for their preparation and use, are disclosed. The derivatives are useful anti-inflammatory and analgesic agents.Type: GrantFiled: June 8, 1990Date of Patent: July 7, 1992Assignee: American Home Products CorporationInventor: Amedeo A. Failli
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Patent number: 5120842Abstract: A compound of the structure ##STR1## wherein R.sup.1 is --SiR.sup.3 R.sup.4 R.sup.5 ;R.sup.2 is hydrogen or --SiR.sup.3 R.sup.4 R.sup.5 ; andR.sup.3, R.sup.4, and R.sup.5 are each, independently, alkyl, alkenyl, aralkyl, triphenylmethyl, or phenyl 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. This invention also provides a method of using rapamycin 42-[O-[(1,1-dimethylethyl)-dimethylsilyl] ether for the preparation of 31-substituted rapamycin derivatives.Type: GrantFiled: April 1, 1991Date of Patent: June 9, 1992Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan
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Patent number: 5120726Abstract: A compound of the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl or aralkyl; R.sup.2 is hydrogen, alkyl, cycloalkyl, aralkyl, --COR.sup.3, --CO.sub.2 R.sup.3, --SO.sub.2 R.sup.3, --CONR.sup.4 R.sup.5, --CSNR.sup.4 R.sup.5, --COCONR.sup.4 R.sup.5, or Ar; R.sup.3 is alkyl, aralkyl, or Ar; R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, cycloalkyl, allyl, aralkyl, or Ar;Ar is ##STR2## R.sup.6, R.sup.7, R.sup.8 are each, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, trifluoromethoxy, amino, or a carboxylic acid; X is CH or N; Y is NH, O, or S; 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.Type: GrantFiled: March 8, 1991Date of Patent: June 9, 1992Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Robert J. Steffan