Patents Represented by Attorney George Tarnowski
  • Patent number: 5420289
    Abstract: 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: Grant
    Filed: March 10, 1993
    Date of Patent: May 30, 1995
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Anthony F. Kreft, III, Amedeo A. Failli, Christopher A. Demerson, Uresh S. Shah, James A. Nelson
  • Patent number: 5364944
    Abstract: 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: Grant
    Filed: January 6, 1993
    Date of Patent: November 15, 1994
    Assignee: American Home Products Corporation
    Inventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
  • Patent number: 5281608
    Abstract: 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: Grant
    Filed: August 28, 1992
    Date of Patent: January 25, 1994
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Robert M. Kearney
  • Patent number: 5279091
    Abstract: 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: Grant
    Filed: June 26, 1992
    Date of Patent: January 18, 1994
    Inventors: Mark F. Williams, Barbara L. Williams
  • Patent number: 5250693
    Abstract: 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: Grant
    Filed: December 13, 1991
    Date of Patent: October 5, 1993
    Assignee: American Home Products Corporation
    Inventors: Anthony F. Kreft, III, John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak, Annette L. Banker
  • Patent number: 5250700
    Abstract: 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: Grant
    Filed: December 9, 1992
    Date of Patent: October 5, 1993
    Assignee: American Home Products Corporation
    Inventors: Jehan F. Bagli, Louis J. Lombardo, Jerauld S. Skotnicki
  • Patent number: 5242945
    Abstract: 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: Grant
    Filed: April 12, 1991
    Date of Patent: September 7, 1993
    Assignee: American Home Products Corporation
    Inventors: Craig E. Caufield, James M. Rinker
  • Patent number: 5229516
    Abstract: 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: Grant
    Filed: July 10, 1992
    Date of Patent: July 20, 1993
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Anthony F. Kreft, III, Amedeo A. Failli, Christopher A. Demerson, Uresh S. Shah, James A. Nelson
  • Patent number: 5218124
    Abstract: 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: Grant
    Filed: June 1, 1992
    Date of Patent: June 8, 1993
    Assignee: American Home Products Corporation
    Inventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
  • Patent number: 5216162
    Abstract: 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: Grant
    Filed: August 28, 1992
    Date of Patent: June 1, 1993
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Robert M. Kearney
  • Patent number: 5216165
    Abstract: 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: Grant
    Filed: March 20, 1992
    Date of Patent: June 1, 1993
    Assignee: American Home Products Corporation
    Inventors: Dominick Mobilio, John H. Musser
  • Patent number: 5208344
    Abstract: 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: Grant
    Filed: December 13, 1991
    Date of Patent: May 4, 1993
    Assignee: American Home Products Corporation
    Inventors: Anthony F. Kreft, III, John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak, Annette L. Banker
  • Patent number: 5194439
    Abstract: 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: Grant
    Filed: September 25, 1991
    Date of Patent: March 16, 1993
    Assignee: John Wyeth & Brother Limited
    Inventors: Ian A. Cliffe, Howard L. Mansell, Richard S. Todd, Alan C. White
  • Patent number: 5191084
    Abstract: 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: Grant
    Filed: May 1, 1991
    Date of Patent: March 2, 1993
    Assignee: American Home Products Corporation
    Inventors: Jehan F. Bagli, Louis J. Lombardo
  • Patent number: 5159085
    Abstract: 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: Grant
    Filed: April 4, 1991
    Date of Patent: October 27, 1992
    Assignee: American Home Products Corporation
    Inventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser
  • Patent number: 5137895
    Abstract: 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: Grant
    Filed: April 29, 1991
    Date of Patent: August 11, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Harry R. Munson, Jr., Gunnar E. Jagdmann, Jr.
  • Patent number: 5124319
    Abstract: 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: Grant
    Filed: October 11, 1991
    Date of Patent: June 23, 1992
    Assignee: American Home Products Corporation
    Inventors: Reinhardt B. Baudy, Horace Fletcher, III, John P. Yardley
  • Patent number: 5124455
    Abstract: 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: Grant
    Filed: August 8, 1990
    Date of Patent: June 23, 1992
    Assignee: American Home Products Corporation
    Inventor: Louis J. Lombardo
  • Patent number: 5112832
    Abstract: 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: Grant
    Filed: August 8, 1990
    Date of Patent: May 12, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: Roger Crossley, Albert Opalko, Robin G. Shepherd
  • Patent number: 5106843
    Abstract: 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: Grant
    Filed: December 19, 1989
    Date of Patent: April 21, 1992
    Assignee: American Home Products Corporation
    Inventors: Terence J. Ward, Janet C. White