Patents Represented by Attorney, Agent or Law Firm Arnold S. Milowsky
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Patent number: 5194447Abstract: 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.Type: GrantFiled: February 18, 1992Date of Patent: March 16, 1993Assignee: American Home Products CorporationInventor: Wenling Kao
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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: 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: 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
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Patent number: 5118678Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CONH(CR.sup.3 R.sup.4).sub.n --X;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, aralkyl, cycloalkyl, halogen, or trifluoromethyl;X ix hydrogen, lower alkyl, cycloalkyl, trifluoromethyl, nitro, alkoxy, carboalkoxy, aralkyl, halo, dialkylamino, thioalkyl, or Y;Y is a phenyl group which may be optionally mono-, di-, or tri- substituted with a group selected from alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, trifluoromethyl, dialkylamino, or alkylthio;n=0-5;with the proviso that R.sup.1 and R.sup.2 are not both hydrogen and when n=0, X is lower alkyl, cycloalkyl, aralkyl, or Y;or a pharmaceutically acceptable salt thereof when X is dialkylamino, which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host vs.Type: GrantFiled: April 17, 1991Date of Patent: June 2, 1992Assignee: American Home Products CorporationInventors: Wenling Kao, Robert L. Vogel, John H. Musser
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Patent number: 5118677Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each independently, hydrogen or ##STR2## X is --(CH.sub.2).sub.m -- or --Ar--; R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, --(CH.sub.2).sub.n --Ar, --(CH.sub.2).sub.p --NR.sup.5 R.sup.6, or --(CH.sub.2).sub.p --N.sup.+ R.sup.5 R.sup.6 R.sup.7 Y.sup.- ; R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, or --(CH.sub.2).sub.n --Ar; Ar is an optionally substituted group selected from ##STR3## in which the optional substituents are selected from the group consisting of alkyl, aralkyl, alkoxy, cyano, halo, nitro, carbalkoxy, or perfluoroalkyl; R.sup.7 is alkyl; Y is a halide, sulfate, phosphate, or p-toluenesulfonate anion; m=1-6; n=1-6; p=1-6; 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.Type: GrantFiled: May 20, 1991Date of Patent: June 2, 1992Assignee: American Home Products CorporationInventor: Craig E. Caufield
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Patent number: 5118690Abstract: The invention concerns a method for treating pain and/or CNS disorders characterized in that the method uses a compound which acts selectively as an antagonist of gamma aminobutyric acid (GABA) at GABA autoreceptors relative to GABA.sub.A receptors.Type: GrantFiled: October 21, 1991Date of Patent: June 2, 1992Assignee: John Wyeth & Brother LimitedInventors: Michael C. W. Minchin, Alan C. White, John F. White
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Patent number: 5100883Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or ##STR2## R.sup.3 is a mono-, di-, poly-, or per-fluorinated alkyl group with the proviso that R.sup.1 and R.sup.2 are both not hydrogen, 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: April 8, 1991Date of Patent: March 31, 1992Assignee: American Home Products CorporationInventor: Guy A. Schiehser