Patents by Inventor John P. Yardley

John P. Yardley 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).

  • Patent number: 5482940
    Abstract: There are disclosed the use of the compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl or 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, or pyrimidinyl wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; and m is the integer from 2 to 5 and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 15, 1993
    Date of Patent: January 9, 1996
    Assignee: American Home Products Corporation
    Inventors: Magid A.-M. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., John A. Moyer
  • Patent number: 5380725
    Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 14, 1993
    Date of Patent: January 10, 1995
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
  • Patent number: 5278160
    Abstract: There are disclosed the use of the compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl or 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, or pyrimidinyl wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; and m is the integer from 2 to 5 and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 10, 1992
    Date of Patent: January 11, 1994
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., John A. Moyer
  • Patent number: 5254552
    Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.The compounds of this invention which demonstrate selectivity at the 5-HT.sub.1A and 5-HT.sub.2 versus D.sub.2 receptor binding sites are useful as potential anxiolytic-antidepressant agents.Compounds of this invention with equal high affinity for the 5-HT.sub.1A and D.sub.2 -receptor binding sites are useful as mixed antipsychotic-anxiolytic agents.
    Type: Grant
    Filed: March 16, 1992
    Date of Patent: October 19, 1993
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, 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: 5106849
    Abstract: There are disclosed the use of the compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl or 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, or pyrimidinyl wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; and m is the integer from 2 to 5 and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 22, 1991
    Date of Patent: April 21, 1992
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., John A. Moyer
  • Patent number: 5010078
    Abstract: There are disclosed compounds of the formula (I) ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 3-noradamantyl, unsubstituted or substituted-2-indolyl, 3-indolyl, 2-benzofuranyl and 3-benzofuranyl wherein the substituents are selected from lower alkyl, lower alkoxy and halo; R.sup.2 is unsubstituted or substituted phenyl, benzyl, pyridinyl, pyrimidinyl or pyrazinyl, wherein the substituents are selected from lower alkyl, lower alkoxy, trifluoromethyl and halo; R.sup.3 is H or lower alkyl of 1 to 3 carbon atoms; n is the integer 0 or 1; m is the integer from 2 to 5; and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 14, 1990
    Date of Patent: April 23, 1991
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
  • Patent number: 4988814
    Abstract: Compounds of the formula: ##STR1## in which R.sup.1 is alkyl; R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene, R.sup.2 and R.sup.3 complete a 5-norbornen-2-yl moiety; X is --CO.sub.2 --, --OCO--, --OCO.sub.2 --, --N(R.sup.7)CO--, --NHNHCO--, --ON(R.sup.7)CO--, --CON(R.sup.7)--, --N(R.sup.7)CO.sub.2 --, --OCON(R.sup.7)-- or --N(R.sup.7)CON(R.sup.8)--, wherein R.sup.7 and R.sup.8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl alkoxy, cyano, nitro or perhalomethyl; R.sup.4 is hydrogen or alkyl; R.sup.5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R.sup.
    Type: Grant
    Filed: October 27, 1989
    Date of Patent: January 29, 1991
    Assignees: American Home Products Corp., John Wyeth & Bro.
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Ian A. Cliffe
  • Patent number: 4921958
    Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; n is 1,2,3,4 or 5; R.sup.1 hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; R.sup.2 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl or 2- or 3-pyrazinyl; R.sup.3 and R.sup.4 are, independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.
    Type: Grant
    Filed: September 27, 1989
    Date of Patent: May 1, 1990
    Assignees: American Home Products Corporation, John Wyeth & Brother Limited
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., Ian A. Cliffe
  • Patent number: 4882432
    Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; X is --O-- or ##STR2## n is 1,2,3 or 4; R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; and R.sup.3 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4-or 5-pyrimidiny; or 2- or 3-pyrazinyl; R.sup.4 and R.sup.5 are independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.
    Type: Grant
    Filed: January 9, 1989
    Date of Patent: November 21, 1989
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
  • Patent number: 4798896
    Abstract: This invention provides a group of antipsychotic/anxiolytic agents of the formula. ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, alkoxy or alkyl;R.sup.2 is hydrogen, phenyl or phenyl substituted with an alkyl, alkoxy, halogen, trifluoromethyl, cyano or nitro group;R.sup.3 and R.sup.4 are hydrogen or, together, complete the benzo ring; andn is 1 to 7;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: January 17, 1989
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Cesario O. Tio
  • Patent number: 4797489
    Abstract: The compounds ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 9-fluorenyl or 1-fluorenyl;n is 0 or 1;m is 1, 2, 3, 4 or 5; andX is ##STR2## where R.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano, nitro or trifluoromethyl, ##STR3## where R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or nitro;or pharmaceutically acceptable salts thereof are useful antidepressant and/or anxiolytic agents.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: January 10, 1989
    Assignee: American Home Products Corp.
    Inventors: Magid A. Abou-Gharbia, Gary P. Stack, John P. Yardley
  • Patent number: 4761501
    Abstract: This application discloses certain substituted phenylacetamides of the formula: ##STR1## in which the dotted line represents optional unsaturation, R.sub.1 is alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen or alkyl; R.sub.5 and R.sub.6, one of which may be hydrogen, are independently, hydroxyl, alkyl, alkoxy, aralkoxy, alkanoyloxy, alkylmercapto, N-protected amino, halo or trifluoromethyl;R.sub.7 is hydrogen or alkyl; andn is one of the integers 0, 1, 2, 3 or 4;which are useful in the production of antidepressant agents.
    Type: Grant
    Filed: May 22, 1985
    Date of Patent: August 2, 1988
    Assignee: American Home Products Corporation
    Inventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
  • Patent number: 4754043
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, where n=1; or Z is O,S, or NR, when n=0; R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;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: October 6, 1986
    Date of Patent: June 28, 1988
    Assignee: American Home Products Corporation
    Inventors: Anthony F. Kreft, III, John H. Musser, Thomas W. Pattison, John P. Yardley
  • Patent number: 4719308
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## Z is CR or N, when n=1; or Z is O, S, or NR, when n=0, R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;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: October 6, 1986
    Date of Patent: January 12, 1988
    Assignee: American Home Products Corporation
    Inventors: Anthony F. Kreft, III, John H. Musser, Thomas W. Pattison, John P. Yardley
  • Patent number: 4661596
    Abstract: There are disclosed compounds of the formula ##STR1## wherein X is --Ch.sub.2 CH.sub.2 --, --CH=CH--, ##STR2## Z is CR or N, when n=1; or Z is O, S, or NR, when n=0; R is hydrogen or loweralkyl;n is 0 or 1;R.sup.1 is hydroxy, amino, loweralkyl sulfonamido, perfluoro loweralkyl sulfonamido or OR;R.sup.2 is hydrogen or loweralkyl;R.sup.3 is hydrogen or loweralkyl; orR.sup.2 and R.sup.3 taken together form a benzene ring; andthe dotted line represents an optional double bond;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: October 3, 1985
    Date of Patent: April 28, 1987
    Assignee: American Home Products Corporation
    Inventors: Anthony F. Kreft, III, John H. Musser, Thomas W. Pattison, John P. Yardley
  • Patent number: 4611078
    Abstract: This application discloses certain substituted phenylacetonitriles of the formula: ##STR1## in which the dotted line represents optional unsaturation, and R.sub.4 is hydrogen or alkyl;R.sub.5 and R.sub.6, one of which may be hydrogen, are ortho or para substituents, independently selected from the group consisting of hydroxyl, alkyl, alkoxy, aralkoxy, alkanoyloxy, alkylmercapto, halo or trifluoromethyl;R.sub.7 is hydrogen or alkyl; andn is one of the integers 0, 1, 2, 3 or 4;which are useful in the production of antidepressant agents.
    Type: Grant
    Filed: May 22, 1985
    Date of Patent: September 9, 1986
    Assignee: American Home Products Corporation
    Inventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
  • Patent number: 4535186
    Abstract: This invention provides a group of hydroxycycloalkanephenethyl amine antidepressant derivatives of the following structural formula: ##STR1## in which A is a moiety of the formula ##STR2## where the dotted line represents optional unsaturation;R.sub.1 is hydrogen or alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen, alkyl, formyl or alkanoyl;R.sub.5 and R.sub.6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl or, taken together, methylenedioxy;R.sub.7 is hydrogen or alkyl; andn is 0, 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 26, 1983
    Date of Patent: August 13, 1985
    Assignee: American Home Products Corporation
    Inventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
  • Patent number: 4272432
    Abstract: The invention embraces the novel nonapeptide L-pyroglutamyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-D-alanyl-L-leucyl -L-arginyl-L-prolinethylamide, intermediates for its production and its use as a claudogenic-interceptive agent.
    Type: Grant
    Filed: November 13, 1974
    Date of Patent: June 9, 1981
    Assignee: American Home Products Corporation
    Inventors: John P. Yardley, Alan Corbin
  • Patent number: 4155935
    Abstract: Reaction of benzalcyclanones with secondary amines affords aminobenzylcyclohexanones, which, upon reduction, yield aminobenzylcyclohexanols having potent analgesic activity. Epimeric aminobenzylcycloalkanols having analgesic activity are prepared by the reaction of C-phenyl nitrones with cycloalkenes to form benzisoxazoles, treatment with alkyl halide to form the corresponding benzisoxazolium halides, followed by hydrogenolysis.
    Type: Grant
    Filed: June 29, 1977
    Date of Patent: May 22, 1979
    Assignee: American Home Products Corporation
    Inventors: John P. Yardley, Peter B. Russell