Patents by Inventor Jerauld S. Skotnicki
Jerauld S. Skotnicki 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: 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: 5250700Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl;R.sup.2 is C.sub.3-7 alkyl or C.sub.3-7 cycloalkyl;R.sup.3 is hydrogen, lower alkyl, carboxyloweralkyl, lower alkoxycarbonyl, lower alkoxycarbonyl loweralkyl, aryl or aralkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, ##STR2## B is a bond, NH or O; Y is O or S;A is a bond or --C.dbd.C--;n is 0-5R.sup.5 may be hydrogen when B is NH, orR.sup.5 is lower alkyl, C.sub.3-8 cycloalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, aralkenyl, aralkenylalkyl, ##STR3## --(CH.sub.2).sub.n NR.sup.1 R.sup.1 or --(CH.sub.2).sub.n het, where het is a 5- or 6-membered, saturated or unsaturated, nitrogen- or sulfur- or oxygen-containing monoheterocycle, optionally substituted with lower alkyl or oxo;R.sup.Type: GrantFiled: December 9, 1992Date of Patent: October 5, 1993Assignee: American Home Products CorporationInventors: Jehan F. Bagli, Louis J. Lombardo, Jerauld S. Skotnicki
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Patent number: 5216162Abstract: There are disclosed compounds of the formula ##STR1## wherein X is R.sup.1, ##STR2## --SO.sub.2 R.sup.1 or --SO.sub.2 R.sup.3 ; R is hydrogen or lower alkyl;R.sup.1 is unsubstituted or substituted pyridyl, indolyl or quinolinyl; or substituted phenyl, thienyl, furyl, benzothienyl or benzofuryl, where the foregoing substituted moieties are substituted with halo, lower alkylcarbonyl, benzoyl, carboxy, lower alkoxycarbonyl, CON(R).sub.2, SO.sub.2 R.sup.3, cyano or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl, phenyl, halo, lower alkoxy, hydroxy or trifluoromethyl;R.sup.3 is lower alkyl or phenyl;Z is --O--, --NNHR.sup.4, --NNHR.sup.1, --NOR.sup.4, --NOR.sup.1, --NOCH.sub.2 R.sup.1, ##STR3## Y is O or S; R.sup.4 is hydrogen, lower alkyl or phenyl;which by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.Type: GrantFiled: August 28, 1992Date of Patent: June 1, 1993Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Robert M. Kearney
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Patent number: 4970316Abstract: There are disclosed compounds of the formula ##STR1## wherein X is O, S, SO, SO.sub.2 or CR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, carboxyl, lower alkoxy carbonyl, lower cycloalkyl, phenyl, anphthyl, pyridyl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing aryl or hetaryl substituents substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, COOR.sup.3, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, SO.sub.3 R.sup.3, SO.sub.2 N(R.sup.3).sub.2, phenylsulfonyl, lower alkyl sulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl;R.sup.4 is halo, morpholino, 4-methylpiperazino, R.sup.5 NNHR.sup.6, R.sup.5 NCH.sub.2 CH.sub.2 OCH.sub.3, or ##STR2## R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.7 and R.sup.Type: GrantFiled: May 3, 1989Date of Patent: November 13, 1990Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman
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Patent number: 4902800Abstract: There are disclosed compounds of the formula: ##STR1## wherein R is phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkenyl, lower alkoxy, carboxy, lower alkoxycarbonyl, hydroxy, amino, mono- or diloweralkylamino, mercapto, lower alkylthio, lower alkylsulfonyl, cyano, nitro or trifluoromethyl; which, by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.Type: GrantFiled: August 17, 1988Date of Patent: February 20, 1990Assignee: American Home Products CorporationInventor: Jerauld S. Skotnicki
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Patent number: 4902685Abstract: There are disclosed compounds of the formula ##STR1## wherein X is CH or NY is CHR.sup.1, NR.sup.2, O or S;R.sup.1 is lower alkenyl, lower alkynyl, or unsubstituted or substituted phenyl, naphthyl, pyridyl, pyrazinyl, pyrimidinyl, quinolyl, quinazolinyl or quinoxalinyl, wherein the substituents are selected from halo, lower alkyl, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkyl sulfonyl, nitro, cyano, trifluoromethyl, hydroxy, mercapto and lower alkylthio; andR.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, or unsubstituted or substituted phenyl, naphthyl, pyridyl, pyrazinyl, pyrimidinyl, quinolyl, quinazolinyl or quinoxalinyl, wherein the substituents are selected from halo, lower alkyl, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, nitro, cyano, trifluoromethyl, hydroxy, mercapto and lower alkylthio, with the proviso that when R.sup.Type: GrantFiled: August 17, 1988Date of Patent: February 20, 1990Assignee: American Home Products CorporationInventor: Jerauld S. Skotnicki
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Patent number: 4894374Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is CHR, NR.sup.1, S or O;R is hydrogen, lower alkenyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl;R.sup.1 is lower alkenyl, pyridyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl; andR.sup.2 and R.sup.Type: GrantFiled: August 17, 1988Date of Patent: January 16, 1990Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Ahmed F. Abdel-Magid
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Patent number: 4851536Abstract: There are disclosed compounds of the formula ##STR1## wherein X is O, S, SO, SO.sub.2 or CR.sup.1 R.sup.2 ;R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, carboxyl, lower alkoxy carbonyl, lower cycloalkyl, phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing aryl or hetaryl substituents substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, COOR.sup.3, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, SO.sub.3 R.sup.3, SO.sub.2 N(R.sup.3).sub.2, phenylsulfonyl, lower alkyl sulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl;R.sup.4 is halo, morpholino, 4-methylpiperazino, R.sup.5 NNHR.sup.6,R.sup.5 NCH.sub.2 CH.sub.2 OCH.sub.3, or ##STR2## R.sup.5 is hydrogen or lower alkyl; R.sup.6 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.7 and R.sup.Type: GrantFiled: April 20, 1988Date of Patent: July 25, 1989Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman
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Patent number: 4826971Abstract: There are disclosed compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1-10 carbon atoms, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, nitro, cyano or lower alkoxycarbonyl;R.sub.2 and R.sub.3 are phenyl or phenyl mono- or di- substituted with halo, lower alkyl, lower alkoxy, nitro, cyano, diloweralkylamino or lower alkoxycarbonyl and R.sub.2 and R.sub.3 may be the same or different; andR.sub.4 is alkyl of 1-10 carbon atoms, phenyl or phenyl mono- or di- substituted with halo, lower alkyl, lower alkoxy, cyano, nitro or lower alkoxycarbonyl;and their use as antifungal agents.Type: GrantFiled: June 28, 1984Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventor: Jerauld S. Skotnicki
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Patent number: 4816464Abstract: There is disclosed a method for the treatment of inflammatory conditions and of collagenase-induced tissue destruction which comprises the administration of a therapeutically effective amount of a compound of the formula ##STR1## wherein R.sup.1 is lower alkyl or lower alkenyl or any of the foregoing optionally substituted with fluoro, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, SR.sup.2 CON(R.sup.2).sub.2, SO.sub.2 R.sup.2, cyano, nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino, R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.6 and R.sup.Type: GrantFiled: June 22, 1987Date of Patent: March 28, 1989Assignee: American Home Products CorporationInventors: Steven C. Gilman, Jerauld S. Skotnicki
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Patent number: 4808612Abstract: There is disclosed a method for the treatment of inflammatory conditions and of collegenase-induced tissue destruction which comprises the administration of a therapeutically effective amount of a compound of the formula ##STR1## wherein R.sup.1 is phenyl or naphthyl, or phenyl or naphthyl substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR.sup.6 and R.sup.Type: GrantFiled: May 7, 1987Date of Patent: February 28, 1989Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman
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Patent number: 4751305Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is pyridl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino, R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, R.sup.4 NCH.sub.2 CH.sub.2 OCH.sub.3, SCH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkylor phenyl; andR.sup.6 and R.sup.Type: GrantFiled: May 7, 1987Date of Patent: June 14, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gillman
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Patent number: 4748246Abstract: There are disclosed compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow, and, by virtue of their ability to inhibit interleukin 1, their use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.Type: GrantFiled: May 7, 1987Date of Patent: May 31, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman, Bruce A. Steinbaugh, John H. Musser
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Patent number: 4728732Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.Type: GrantFiled: November 25, 1985Date of Patent: March 1, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Donald P. Strike
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Patent number: 4728733Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.3 are each individually hydrogen, lower alkyl, carboxy, lower alkoxycarbonyl, cyano, nitro, trifluoromethyl, phenyl or naphthyl; or R.sup.2 and R.sup.3 taken together represent ##STR3## or a 5- or 6- membered unsaturated aza-, diaza-, triaza-, tetraza-, thia-, thiaza-, oxathia-, oxathiaza-, oxa-, dioxa-, oxaza- or oxadiazacyclic moiety; and the dotted line denotes an optional double bond; andR.sup.4 is hydrogen, lower alkyl, phenyl or naphthyl.Type: GrantFiled: November 25, 1985Date of Patent: March 1, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Donald P. Strike
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Patent number: 4728734Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is ##STR2## R.sup.2 and R.sup.Type: GrantFiled: November 25, 1985Date of Patent: March 1, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Donald P. Strike
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Patent number: 4719302Abstract: There are disclosed compounds having the formula ##STR1## wherein R is hydrogen or lower alkyl;R.sup.1 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, phenyl or any of the foregoing substituted with halo;R.sup.2 is hydrogen, carboxy or lower alkoxy carbonyl; andR.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or any of the foregoing substituted with carboxy, methoxycarbonyl, hydroxy, amino, dilower alkyl amino, cyano, nitro or lower alkoxy;and their use as antifungal agents.Type: GrantFiled: March 13, 1987Date of Patent: January 12, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Donald P. Strike, Bruce A. Steinbaugh
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Patent number: 4692517Abstract: There are disclosed novel antibacterial compounds having the formula ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo lower alkyl, aryl of 6-12 carbon atoms, all the said foregoing groups being optionally substituted with carboxy, lower alkoxycarbonyl, phenoxycarbonyl, amino, mono- or di-lower alkyl substituted amino, hydroxy, lower alkoxy, phenoxy, carbamoyl, lower alkyl carbonyl, benzoyl, cyano, nitro, formamido, lower alkanoylamino or benzamido;R.sup.1 is hydrogen, lower alkyl or an alkali metal cation;A is lower alkoxy, lower alkenoxy, lower alkynoxy, aryloxy of 6-12 carbon atoms, di-lower alkyl substituted amino, di-lower alkenyl substituted amino, di-lower alkynyl substituted amino, di-aryl of 6-12 carbon atoms substituted amino, lower alkyl, lower alkenyl, lower alkynyl, aryl of 6-12 carbon atoms.Type: GrantFiled: March 20, 1986Date of Patent: September 8, 1987Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Thomas J. Commons