Patents Represented by Attorney George Tarnowski
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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: 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: 5281608Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl or phenyl;R.sup.1 is hydrogen, lower alkyl, phenyl, halo, hydroxy, lower alkoxy or trifluoromethyl;R.sup.2 is phenyl, phenylloweralkyl, thienyl, furyl, pyrrolyl, pyridyl, benzothienyl, benzofuryl, indolyl, quinolinyl, or any of the foregoing substituted with halo, lower alkyl, lower alkylcarbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl; ##STR2## R.sup.Type: GrantFiled: August 28, 1992Date of Patent: January 25, 1994Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Robert M. Kearney
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Patent number: 5279091Abstract: There are disclosed building enclosure assemblies consisting of panel members, a support means and a clip attachment means, for the construction of fixed or demountable, full or partial, interior or exterior walls, ceilings and floorings, which can meet code-mandated fire-rating and loading requirements, and in which differently sized and shaped panel members can be articulated to one another through the cooperative assembly of the panel members with the support means and clip attachment means.Type: GrantFiled: June 26, 1992Date of Patent: January 18, 1994Inventors: Mark F. Williams, Barbara L. Williams
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Patent number: 5250693Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydrogen or lower alkyl;Y is ##STR2## or a pharmaceutically acceptable salt thereof, and its use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.Type: GrantFiled: December 13, 1991Date of Patent: October 5, 1993Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III, John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak, Annette L. Banker
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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: 5242945Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is --CH.sub.2 R;R is ##STR2## and further when Y=S, R may also be --(CH.sub.2).sub.e CH.sub.3 ; Y is --O--or --S--;R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl;R.sup.3 is indolyl, furyl, phenyl or phenyl optionally mono- or disubstituted independently by alkyl of 1-7 carbon atoms, --C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 CH.sub.3, haloloweralkyl, perfluoroalkyl, lower alkoxy, aryl alkoxy, halo or nitro;R.sup.4 and R.sup.5 are, independently, --COCH.sub.2 R.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, geranyl or CH.sub.2 R.sup.3 ;R.sup.6 is hydrogen or lower alkyl;R.sup.7 is geranyl and any moiety selected from R other than ##STR3## A and B are, independently, --O--, --S-- or --NR.sup.6 --; and a is 0-8;b is 1-10 when Y=S, and 2-10 when Y=O;c is 1-3;d is 0-9; ande is 3-18;which by virtue of their ability to inhibit PLA.sub.Type: GrantFiled: April 12, 1991Date of Patent: September 7, 1993Assignee: American Home Products CorporationInventors: Craig E. Caufield, James M. Rinker
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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: 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: 5216165Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydrogen, halo or trifluoromethyl;R.sup.1 is hydrogen or X;R.sup.2 is hydrogen or X; with the proviso that when R.sup.1 is X, R.sup.2 is hydrogen, and when R.sup.1 is hydrogen, R.sup.2 is X;X is the moiety ##STR2## wherein R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen or ##STR3## R.sup.5 is hydrogen, alkyl of 1-16 carbon atoms, phenyl, phenylloweralkyl or perfluoroloweralkyl;Y is CO or a bond;R.sup.6 is lower alkyl, cycloloweralkyl, arylalkyl, --(CH.sub.2).sub.m -cycloloweralkyl, ##STR4## or --(CH.sub.2).sub.o CONR.sup.8 R.sup.9 or, in the case when Y is CO, phenyl;R.sup.7 is hydrogen or ##STR5## R.sup.8 and R.sup.9 are, independently, hydrogen, lower alkyl, cycloloweralkyl or R.sup.8 and R.sup.Type: GrantFiled: March 20, 1992Date of Patent: June 1, 1993Assignee: American Home Products CorporationInventors: Dominick Mobilio, John H. Musser
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Patent number: 5208344Abstract: There are disclosed compounds of the formula ##STR1## wherein A is alkyl of 3-19 carbon atoms, diloweralkyl allyl, dihaloallyl, diphenylallyl, lower alkynyl, ##STR2## with the proviso that A is not quinolinyl; W is --CR.sub.2 O--, --CH.dbd.CH-- or --CH.dbd.CHCH.sub.2 O--;X is N or CR;Z is ##STR3## --S-- or --O--; R is hydrogen or lower alkyl;Y is ##STR4## 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, optionally substituted by halo;R.sup.3 is --OR, ##STR5## or --NHSO.sub.2 R.sup.4 ; R.sup.4 is phenyl or loweralkyl substituted phenyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.Type: GrantFiled: December 13, 1991Date of Patent: May 4, 1993Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III, John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak, Annette L. Banker
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Patent number: 5194439Abstract: Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.Type: GrantFiled: September 25, 1991Date of Patent: March 16, 1993Assignee: John Wyeth & Brother LimitedInventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
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Patent number: 5191084Abstract: 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 0-5;R.sup.5 is hydrogen when B is NH, orR.sup.5 is lower alkyl, C.sub.3-8 cycloalkyl; aryl, substituted aryl, aralkyl, substituted aralkyl, aralkenyl, aralkenylalkyl or ##STR3## R.sup.6 is hydrogen or halo; the dotted line represents an optional double bond; andthe pharmacologically acceptable salts thereof, which by virtue of their ability to selectively inhibit PDE IV, are bronchodilatory and anti-inflammatory and so are useful in the treatment of acute and chronic bronchial asthma and associated pathologies.Type: GrantFiled: May 1, 1991Date of Patent: March 2, 1993Assignee: American Home Products CorporationInventors: Jehan F. Bagli, Louis J. Lombardo
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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: 5137895Abstract: 3-[N-Aroyl(or thioaryol)aminoalkyl]-3-quinuclidinols corresponding to the formula: ##STR1## wherein X is O or S, and Ar is phenyl, substituted phenyl, indole, indazole or pyrimidine; optical isomers and the pharmaceutically acceptable acid addition salts and solvates thereof. These compounds have gastric emptying, antiemetic, anxiolytic and selective serotonin modulating or inhibiting activity.Type: GrantFiled: April 29, 1991Date of Patent: August 11, 1992Assignee: A. H. Robins Company, IncorporatedInventors: Harry R. Munson, Jr., Gunnar E. Jagdmann, Jr.
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Patent number: 5124319Abstract: The compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl, benzyl or pivaloyloxymethyl;R.sup.1 and R.sup.2 are, independently, hydrogen, lower alkyl, lower alkoxy, trifluoromethyl, trifluoromethoxy, methanesulfonylamino, acetylamino, or halo, or when taken together R.sup.1 and R.sup.2 represent a methylenedioxy grouping;and the pharmacologically acceptable salts thereof are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids.Type: GrantFiled: October 11, 1991Date of Patent: June 23, 1992Assignee: American Home Products CorporationInventors: Reinhardt B. Baudy, Horace Fletcher, III, John P. Yardley
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Patent number: 5124455Abstract: There are disclosed compounds of the formula ##STR1## wherein R is ##STR2## R.sup.1 is hydrogen, lower alkyl or ##STR3## a is 1-3; b is 1-3;c is 0-2;X, Y and Z are each, independently, a bond, O, S. or NH, with the proviso that if one of X or Y is O, S or NH, the other must be a bond;R.sup.2 is amino, loweralkylamino, arylamino, loweralkoxy or aryloxy;R.sup.3 is hydrogen, halo, hydroxy, lower alkoxy, aryloxy, loweralkanoyloxy, amino, lower alkylamino, arylamino or loweralkanoylamino;R.sup.4 and R.sup.5 are each, independently hydrogen or lower alkyl;m is 0-4;n is 1-4; ando is 1-4;and, which by virtue of their ability to selectively inhibit an isoenzyme of 3':5'-cyclic AMP phosphodiesterase located in pulmonary smooth muscle tissue and inflammatory cells, are bronchodilatory and antinflammatory and so are useful in the treatment of acute and chronic bronchial asthma and associated pathologies.Type: GrantFiled: August 8, 1990Date of Patent: June 23, 1992Assignee: American Home Products CorporationInventor: Louis J. Lombardo
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Patent number: 5112832Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.0 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.Type: GrantFiled: August 8, 1990Date of Patent: May 12, 1992Assignee: John Wyeth & Brother LimitedInventors: Roger Crossley, Albert Opalko, Robin G. Shepherd
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Patent number: 5106843Abstract: Aryl ureas and carbamic acid derivatives of formulaA--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including 3,5-dichlorophenylW is O or SY is NH or O andB is a specified saturated azacyclic ring, e.g. tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.Type: GrantFiled: December 19, 1989Date of Patent: April 21, 1992Assignee: American Home Products CorporationInventors: Terence J. Ward, Janet C. White