Patents Represented by Attorney George Tarnowski
  • Patent number: 4933365
    Abstract: There is disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals which comprises administering to a mammal so afflicated an effective amount of a compound having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, hydroxy, lower alkyl, lower alkoxy, haloloweralkyl, haloloweralkyl sulfonyl, halo or nitro;R.sup.3 is hydrogen, lower alkyl, or aryl of 7-12 carbon atoms;X is ##STR2## A is --CH.sub.2 --, --O-- or --S--; m is 0-8;n is 0-7, with the proviso that m+n.ltoreq.8;or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: January 25, 1989
    Date of Patent: June 12, 1990
    Assignee: American Home Products Corporation
    Inventors: Lisa A. Marshall, Kurt E. Steiner, Guy A. Schiehser
  • Patent number: 4927934
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is>1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that were R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.
    Type: Grant
    Filed: May 5, 1989
    Date of Patent: May 22, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Usha R. Patel
  • Patent number: 4904786
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is hydrogen or loweralkyl;R.sup.4 hydrogen, lower alkyl, --COOR.sup.3 or ##STR3## R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR4## 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, and as antiinflammatory agents.
    Type: Grant
    Filed: August 11, 1988
    Date of Patent: February 27, 1990
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Dennis M. Kubrak, Anthony F. Kreft, III, Reinhold H. W. Bender
  • Patent number: 4902800
    Abstract: 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: Grant
    Filed: August 17, 1988
    Date of Patent: February 20, 1990
    Assignee: American Home Products Corporation
    Inventor: Jerauld S. Skotnicki
  • Patent number: 4902685
    Abstract: 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: Grant
    Filed: August 17, 1988
    Date of Patent: February 20, 1990
    Assignee: American Home Products Corporation
    Inventor: Jerauld S. Skotnicki
  • Patent number: 4897976
    Abstract: There are disclosed building enclosure assemblies consisting of gypsum-based panel members, a support means and a fire-resistant spline, 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 wind-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 spline.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: February 6, 1990
    Inventors: Mark F. Williams, Barbara L. Williams
  • Patent number: 4895953
    Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 ##STR3## W represents a bond or --O--, --S-- or ##STR4## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR5## R.sup.6 is hydrogen, lower alkyl, --COOR.sup.4 or ##STR6## 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, and as antiinflammatory agents.
    Type: Grant
    Filed: February 15, 1989
    Date of Patent: January 23, 1990
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
  • Patent number: 4894374
    Abstract: 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: Grant
    Filed: August 17, 1988
    Date of Patent: January 16, 1990
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Ahmed F. Abdel-Magid
  • Patent number: 4892943
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 represent the structure ##STR2## R.sup.3 and R.sup.4 are hydrogen, or R.sup.3 and R.sup.4 taken together form a 3-5 membered saturated carbocyclic ring;R.sup.5 and R.sup.6 are hydrogen, or R.sup.5 and R.sup.6 taken together form a 3-6 membered carbocyclic ring or a cyclobutenyl ring; with the proviso that when R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen, n is other than zero;m is 2-4;n is 0-4;X is lower alkylene, vinylene or O;R.sup.7 is unsubstituted or substituted phenyl, 2-pyridinyl, 2-pyrimidinyl, 2-pyrazinyl or 3-pyridazinyl; where the substituents are selected from the group lower alkyl, lower alkoxy, halo, cyano, nitro and trifluoromethyl;and the pharmaceutically acceptable salts thereof and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
    Type: Grant
    Filed: August 26, 1988
    Date of Patent: January 9, 1990
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4889935
    Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R is hydrogen, lower alkyl, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di-lower alkylamino, nitro, hydroxy, carboxy, lower alkoxycarbonyl, lower alkoxy or halo;R.sup.2 is hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other inflammatory conditions.
    Type: Grant
    Filed: June 30, 1989
    Date of Patent: December 26, 1989
    Assignee: American Home Products Corporation
    Inventor: John H. Musser
  • Patent number: 4889936
    Abstract: The invention concerns a process for preparng a thiazolo[3,2-a]benzimidazole of formula I ##STR1## in which formula n is 1 or 2, and R.sub.1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, ##STR2## or a salt thereof wherein n and R, are a defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.
    Type: Grant
    Filed: January 10, 1989
    Date of Patent: December 26, 1989
    Assignee: John Wyeth & Brotyher Limited
    Inventors: Robin G. Shepherd, Sie-Yearl Chai, Maynard E. Lichty, Arnold S. Milowsky
  • Patent number: 4889846
    Abstract: The invention concerns azo compounds of formula ##STR1## or a salt thereof, in which formula R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are each independently hydrogen or lower alkyl, R.sup.7 and R.sup.8 are each independently alkyl of 1 to 7 carbon atom or cycloalkyl of 5 to 7 carbon atoms optionally substituted by lower alkyl which possess anti-inflammatory activity.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: December 26, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4876346
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is N or CR.sup.1Y is O, S, NR.sup.1, CHR.sup.1 or C(R.sup.1).sub.2 when n=O, or N or CR.sup.1 when n=1;p is 0-3;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is H, ##STR2## --SO.sub.2 R.sup.3 or --SO.sub.2 N(R.sup.3).sub.2, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl carbonyl prolinate;R.sup.3 is H, lower alkyl or perfluoro lower alkyl;R.sup.4 is lower alkyl, phenyl, pyridyl or thienyl;R.sup.5 is hydrogen, lower alkyl, phenyl or pyridyl;A is O or NR.sup.1 ;B is OR.sup.1 or N(R.sup.5).sub.2 ;m is 0-2;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.
    Type: Grant
    Filed: May 15, 1986
    Date of Patent: October 24, 1989
    Assignee: American Home Products Corporation
    Inventors: John H. Musser, Anthony F. Kreft, III, Reinhold H. W. Bender
  • Patent number: 4873237
    Abstract: The invention relates to a method of treatment of ulcers or hypersecretion in a mammal which comprises administering a compound of formula ##STR1## or a pharmaceutically acceptable salt thereof wherein --B--B.sup.1 -- represents a chain of formula--(CHR.sup.5).sub.n --CHR.sup.6 -- (Ia)R represents an optionally substituted aryl or heteroaryl radical,R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, or a defined substituent or any adjacent pair of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 together with the carbon atoms to which they are attached complete a five or six membered saturated or unsaturated carbocyclic or heterocyclic ring, said ring being optionally substituted by a defined substituent and said heterocyclic ring having at least one heteroatom selected from oxygen, nitrogen and sulphur;R.sup.5 and R.sup.
    Type: Grant
    Filed: May 22, 1986
    Date of Patent: October 10, 1989
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Patent number: 4870210
    Abstract: There are disclosed compounds of the formula ##STR1## wherein ##STR2## R is hydrogen, lower alkyl, phenyl or benzyl; R.sup.1 is hydrogen, lower alkyl, trifluoromethyl, amino, mono- or di- lower alkylamino, nitro, hydroxy, carboxy, lower alkoxycarbonyl, lower alkoxy or halo;R.sup.2 is hydrogen or lower alkyl;and the pharmaceutically acceptable salts thereof, and their use in the treatment of psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other inflammatory conditions.
    Type: Grant
    Filed: December 18, 1987
    Date of Patent: September 26, 1989
    Assignee: American Home Products Corporation
    Inventor: John H. Musser
  • Patent number: 4857644
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl or phenyl; or R.sup.1 and R.sup.2 taken together represent --(CH.sub.2).sub.4 --or ##STR2## where the dotted line represents an optional double bond; R.sup.3 is hydrogen, lower alkyl, lower alkoxy or halo;R.sup.4 is pyridinyl, pyrimidinyl, pyrazinyl, benzyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, or halo;Z is --SO.sub.2 --or ##STR3## where R.sup.5 is hydrogen or lower alkyl; m is 0-4;n is 0-2; andthe pharmaceutically acceptable salts thereof, and their use as anti-inflammatory agents.
    Type: Grant
    Filed: June 9, 1988
    Date of Patent: August 15, 1989
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4855430
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is>1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that where R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.
    Type: Grant
    Filed: November 12, 1987
    Date of Patent: August 8, 1989
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Usha R. Patel
  • Patent number: 4853333
    Abstract: There is disclosed a DNA transfer vector capable of replication in either a yeast cell or a bacterial cell and having inserted therein a DNA segment coding for human WA rotavirus surface antigen VP7. The transfer vector carrying the foreign DNA is used to transform yeast cells in order to produce the surface antigen VP7 which is capable of eliciting in vivo production of neutralizing antibodies with respect to human WA rotavirus. The surface antigen VP7 so elaborated and its use in a pharmaceutical vaccine composition are also disclosed.
    Type: Grant
    Filed: July 26, 1985
    Date of Patent: August 1, 1989
    Assignee: American Home Products Corporation
    Inventors: Chu-lai Hsiao, Bruce B. Mason, Alan R. Davis
  • Patent number: 4851536
    Abstract: 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: Grant
    Filed: April 20, 1988
    Date of Patent: July 25, 1989
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Steven C. Gilman
  • Patent number: 4845292
    Abstract: There are disclosed compounds of the formula ##STR1## R is --CH.sub.2 OH or --CO.sub.2 R.sup.3 ; R.sup.1 is hydrogen, lower alkyl, lower alkoxy or hydroxybenzyl;R.sup.2 is hydroxyloweralkyl or diloweralkoxyalkyl;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is alkyl of 10-20 carbons atoms, phenylalkyl of 11-18 carbon atoms or phenoxyalkyl of 11-18 carbon atoms; orn is 1-3;or a pharmaceutically acceptable salt thereof, and their use in the prevention and/or treatment of conditions such as allergic rhinitis, allergic bronchial asthma and other naso-bronchial obstructive air-passageway conditions, other immediate hypersensitivity reactions such as allergic conjunctivitis and various inflammatory conditions.
    Type: Grant
    Filed: January 13, 1988
    Date of Patent: July 4, 1989
    Assignee: American Home Products Corporation
    Inventors: William H. McGregor, Lisa A. Marshall, John H. Musser