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).
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Patent number: 5482940Abstract: 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: GrantFiled: April 15, 1993Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Magid A.-M. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., John A. Moyer
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Patent number: 5380725Abstract: 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: GrantFiled: July 14, 1993Date of Patent: January 10, 1995Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 5278160Abstract: 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: GrantFiled: March 10, 1992Date of Patent: January 11, 1994Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., John A. Moyer
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Patent number: 5254552Abstract: 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: GrantFiled: March 16, 1992Date of Patent: October 19, 1993Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, 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: 5106849Abstract: 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: GrantFiled: April 22, 1991Date of Patent: April 21, 1992Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., John A. Moyer
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Patent number: 5010078Abstract: 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: GrantFiled: March 14, 1990Date of Patent: April 23, 1991Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 4988814Abstract: 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: GrantFiled: October 27, 1989Date of Patent: January 29, 1991Assignees: American Home Products Corp., John Wyeth & Bro.Inventors: Magid A. Abou-Gharbia, John P. Yardley, Ian A. Cliffe
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Patent number: 4921958Abstract: 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: GrantFiled: September 27, 1989Date of Patent: May 1, 1990Assignees: American Home Products Corporation, John Wyeth & Brother LimitedInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr., Ian A. Cliffe
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Patent number: 4882432Abstract: 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: GrantFiled: January 9, 1989Date of Patent: November 21, 1989Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
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Patent number: 4798896Abstract: 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: GrantFiled: January 19, 1988Date of Patent: January 17, 1989Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, John P. Yardley, Cesario O. Tio
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Patent number: 4797489Abstract: 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: GrantFiled: December 2, 1987Date of Patent: January 10, 1989Assignee: American Home Products Corp.Inventors: Magid A. Abou-Gharbia, Gary P. Stack, John P. Yardley
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Patent number: 4761501Abstract: 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: GrantFiled: May 22, 1985Date of Patent: August 2, 1988Assignee: American Home Products CorporationInventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
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Patent number: 4754043Abstract: 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: GrantFiled: October 6, 1986Date of Patent: June 28, 1988Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III, John H. Musser, Thomas W. Pattison, John P. Yardley
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Patent number: 4719308Abstract: 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: GrantFiled: October 6, 1986Date of Patent: January 12, 1988Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III, John H. Musser, Thomas W. Pattison, John P. Yardley
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Patent number: 4661596Abstract: 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: GrantFiled: October 3, 1985Date of Patent: April 28, 1987Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III, John H. Musser, Thomas W. Pattison, John P. Yardley
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Patent number: 4611078Abstract: 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: GrantFiled: May 22, 1985Date of Patent: September 9, 1986Assignee: American Home Products CorporationInventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
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Patent number: 4535186Abstract: 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: GrantFiled: October 26, 1983Date of Patent: August 13, 1985Assignee: American Home Products CorporationInventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth
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Patent number: 4272432Abstract: 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: GrantFiled: November 13, 1974Date of Patent: June 9, 1981Assignee: American Home Products CorporationInventors: John P. Yardley, Alan Corbin
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Patent number: 4155935Abstract: 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: GrantFiled: June 29, 1977Date of Patent: May 22, 1979Assignee: American Home Products CorporationInventors: John P. Yardley, Peter B. Russell