Patents by Inventor Guy A. Schiehser
Guy A. Schiehser 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: 7563792Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: GrantFiled: June 27, 2007Date of Patent: July 21, 2009Assignee: Jacobus Pharmaceutical Company, Inc.Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
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Publication number: 20080176852Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: ApplicationFiled: June 27, 2007Publication date: July 24, 2008Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
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Patent number: 7256218Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: GrantFiled: November 18, 2003Date of Patent: August 14, 2007Assignee: Jacobus Pharmaceutical Company, Inc.Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
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Publication number: 20040116428Abstract: Biguanide and dihydrotriazine derivatives, preferably substituted asymmetrical imidodicarbonimidic diamides derived from hydroxylamines, and compositions containing biguanide and dihydrotriazine derivatives are disclosed. In addition, methods of using the biguanide and dihydrotriazine derivatives, inter alia, as antimicrobial agents and methods of using the dihydrotriazine derivatives in biological assays are disclosed. Methods of making the biguanide and dihydrotriazine derivatives are also disclosed.Type: ApplicationFiled: November 18, 2003Publication date: June 17, 2004Inventors: David P. Jacobus, Guy A. Schiehser, Hong-Ming Shieh, Norman P. Jensen, Jacek Terpinski
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Patent number: 5677295Abstract: A compound of the structure ##STR1## wherein X--Y is C.dbd.NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or --OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: May 30, 1996Date of Patent: October 14, 1997Inventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
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Patent number: 5563145Abstract: A compound of the structure ##STR1## wherein X-Y is C=NOR.sup.1 or CHNHOR.sup.2 ; R.sup.1 and R.sup.2 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, cycloalkyl, alkyloxy, alkoxyalkyl, cycloalkylaminoalkyl, cyanoalkyl, fluoroalkyl, trifluoromethylalkyl, trifluoromethyl, ArO--, --(CH.sub.2).sub.m Ar, or --COR.sup.3 ;R.sup.3 is alkyl of 1-6 carbon atoms, --NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.5, or -OR.sup.4 ;R.sup.4 and R.sup.5 are each, independently, alkyl, Ar or if both are present can be taken together to form a 4-7 membered ring;Ar is an aryl or heteroaryl radical which may be optionally substituted; and m=0-6; or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: December 7, 1994Date of Patent: October 8, 1996Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Guy A. Schiehser, Oleg I. Bleyman
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Patent number: 5559122Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: May 24, 1995Date of Patent: September 24, 1996Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5521194Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: May 24, 1995Date of Patent: May 28, 1996Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5508290Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl , or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: May 24, 1995Date of Patent: April 16, 1996Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5508285Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl , or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: May 24, 1995Date of Patent: April 16, 1996Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5491231Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl , or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic N-oxide radical, which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated N-alkyl-heterocyclic N-oxide, which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: November 28, 1994Date of Patent: February 13, 1996Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5468774Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is O;R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido;A is O, S, NR, or a chemical bond;R, if present, is hydrogen or loweralkyl;m is 0-15;n is 3-12;p is 0-15,where m+p=2-15;and the pharmacologically acceptable salts thereof. Also disclosed is a method for treating immunoimmflammatory conditions in mammals which comprises administering to a mammal so afflicted an effective amount of a compound having the formula above wherein X, R.sup.1, R.sup.2, A, R, if present, m and p are as listed above and n=3-12 and m+p=2-15.Type: GrantFiled: March 14, 1995Date of Patent: November 21, 1995Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Craig E. Caufield, Nancie A. Senko, Gregory F. VonBurg
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Patent number: 5420153Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is NR;R is hydrogen or lower alkyl;R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido;A is O, S, NR, or a chemical bond;m is 0-15;n is 0-20;p is 0-15,where m+p.ltoreq.15;and the pharmacologically acceptable salts thereof, which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals, as well as in the modulation of PAF-mediated biological processes, such as embryonic implantation, thus making the compounds useful as antifertility agents.Type: GrantFiled: September 8, 1994Date of Patent: May 30, 1995Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Craig E. Caufield, Nancie A. Senko, Gregory F. VonBurg
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Patent number: 5385908Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen; R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or R.sup.2 and R.sup.3 may be taken together to form a cycloalkyl ring;R.sup.4 is a heterocyclic radical which may be optionally substituted;R.sup.5 is alkyl or arylalkyl;R.sup.6 and R.sup.7 are taken together to form a saturated heterocyclic ring which may be optionally substituted;k=0-1,m=0-1;n=1-6;with the proviso that R and R.sup.1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: November 22, 1993Date of Patent: January 31, 1995Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5385910Abstract: Compounds of the structure ##STR1## R and R.sup.1 are each, independently, hydrogen, or ##STR2## R.sup.2 and R.sup.3 are each, independently, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.5 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a saturated heterocycle wherein the heterocyclic ring may be optionally mono-, di-, or tri-substituted;m=0-1; andn=0-6;with the proviso that R and R.sup.1 are not both hydrogen, or a pharmaceutically acceptable salt thereof, and ##STR3## R.sup.1 is ##STR4## R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, arylalkyl, or may be taken together to form a cycloalkyl ring;R.sup.4 and R.sup.Type: GrantFiled: November 22, 1993Date of Patent: January 31, 1995Assignee: American Home Products CorporationInventors: Timothy D. Ocain, Guy A. Schiehser
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Patent number: 5385909Abstract: A compound of the structure ##STR1## wherein R and R.sup.1 are each, independently, ##STR2## or hydrogen, R.sup.2 is a heterocyclic radical which may be optionally substituted;n=0-6;with the proviso that R and R.sup.1 are both not hydrogen, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent.Type: GrantFiled: November 22, 1993Date of Patent: January 31, 1995Assignee: American Home Products CorporationInventors: Frances C. Nelson, Guy A. Schiehser
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Patent number: 5366993Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is O, S or NR;R is hydrogen or lower alkyl;R.sup.1 and R.sup.2 are each, independently, hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.20 cycloalkyl, phenylloweralkyl, or substituted phenylloweralkyl substituted by halo, lower alkyl, lower alkoxy, halo lower alkyl, amino, monoloweralkylamino, diloweralkylamino or sulfonamido;A is O, S, NR, or a chemical bond;m is 0-15;n is 0-20;p is 0-15,where m+p.ltoreq.15;and the pharmacologically acceptable salts thereof, which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals, as well as in the modulation of PAF-mediated biological processes, such as embryonic implantation, thus making the compounds useful as antifertility agents.Type: GrantFiled: June 3, 1993Date of Patent: November 22, 1994Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Craig E. Caufield, Nancie A. Senko, Gregory F. VonBurg
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Patent number: 5362718Abstract: A compound of the structure ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen or --CO(CR.sup.3 R.sup.4).sub.b (CR.sup.5 R.sup.6).sub.d CR.sup.7 R.sup.8 R.sup.9 ;R.sup.3 and R.sup.4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or --F;R.sup.5 and R.sup.6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.5 and R.sup.6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with --(CR.sup.3 R.sup.4).sub.f 0R.sup.10 ;R.sup.7 is hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11 ;R.sup.8 and R.sup.9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, --(CR.sup.3 R.sup.4).sub.f OR.sup.10, --CF.sub.3, --F, or --CO.sub.2 R.sup.11, or R.sup.8 and R.sup.Type: GrantFiled: April 18, 1994Date of Patent: November 8, 1994Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Christina L. Leone, Guy A. Schiehser
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Patent number: 5151413Abstract: Derivatives of Rapamycin where the hydroxy group at position 31 and/or 42 are reacted with acetal forming reagents have been shown to have immunosuppressant and antifungal properties. These derivatives are represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, --CH.sub.2 YX, --C(CH.sub.3).sub.2 YX, --CH.sub.2 (CH.sub.3)YX, or L;Y is O or S; X is --CH.sub.3, --(CH.sub.2).sub.n CH.sub.3, --CH.sub.2 C.sub.6 H.sub.6, --(CH.sub.2).sub.2 OCH.sub.3, --CH.sub.2 Cl.sub.3 or --CH.sub.2 CH.sub.2 Si(CH.sub.3).sub.3 and L is selected from tetrahydrofuran-2-yl, tetrahydrothiophen-2-yl, tetrahydrothiopyran-2-yl, tetrahydropyran-2-yl, 4-methoxytetrahydropyran-2-yl, 4-methoxytetrahydrothiopyran-2-yl, or 4-methoxytetrahydrothiopyran-S, S-dioxide-2-yl with a proviso that R.sup.1 and R.sup.2 cannot simultaneously be hydrogen and n is 1-5.Type: GrantFiled: November 6, 1991Date of Patent: September 29, 1992Assignee: American Home Products CorporationInventors: Craig E. Caufield, Guy A. Schiehser
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Patent number: RE44768Abstract: A compound of the structure wherein R1 and R2 are each, independently, hydrogen or —CO(CR3R4)b(CR5R6)dCR7R8R9; R3 and R4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or —F; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4)fOR10, —CF3, —F, or —CO2R11, or R5 and R6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with —(CR3R4)fOR10; R7 is hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4-)fOR10, —CF3, —F, or CO2R11; R8 and R9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, —(CR3R4)fOR10, —CF3, —F, or —CO2R11, or R8 and R9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with —(CR3R4-)fOR10; R10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X isType: GrantFiled: June 28, 2013Date of Patent: February 18, 2014Assignee: Wyeth LLCInventors: Jerauld S. Skotnicki, Christina L. Leone, Guy A. Schiehser