Patents by Inventor Magid A. Abou-Gharbia
Magid A. Abou-Gharbia 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: 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: 4985560Abstract: The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.Type: GrantFiled: January 12, 1990Date of Patent: January 15, 1991Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Magid A. Abou-Gharbia, Gervais Dionne
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Patent number: 4968792Abstract: Disclosed herein are novel benzisothiazole derivatives having pharmacological activity, to a process for preparing them, to pharmaceutical compositions containing them, and to their use in the treatment of a variety of central nervous system disorders.Type: GrantFiled: September 25, 1989Date of Patent: November 6, 1990Assignee: American Home Products CorporationInventors: Gary P. Stack, Magid A. Abou-Gharbia, Thomas D. Golobish
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Patent number: 4957913Abstract: Hypertension in the mammal is controlable by administration of a compound of the formula: ##STR1## wherein R is ##STR2## in which X is methylene, ethylene or ethylidene and Q is alkylene, alkylidene, or Q is a ##STR3## in which the dotted line represents optional unsaturation; n is one of the integers 2,3 or 4;Ar is phenyl or phenyl substituted with halo. trifluoromethyl or alkoxy, or Ar is 2-pyrimidinyl or halopyrimidin-2-yl, 2-pyrazinyl or halo-pyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl or halopyridin-2-yl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 22, 1989Date of Patent: September 18, 1990Assignee: American Home Products Corp.Inventors: Magid A. Abou-Gharbia, Gary P. Stack, Rodney W. Lappe
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Patent number: 4957909Abstract: The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.Type: GrantFiled: January 2, 1990Date of Patent: September 18, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Ronald R. Notvest
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Patent number: 4942234Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.Type: GrantFiled: February 28, 1989Date of Patent: July 17, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
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Patent number: 4940789Abstract: This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, nitro, halo, trifluoromethyl, amino, alkylamino or dialkylamino; R.sup.2 is alkyl; R.sup.4 is alkyl, phenyl or benzyl; n is 0 or 1; m is one of the integers 0,1,2,3,4,5 or 6; and X is alkyl, alkylamino, dialkylamino, alkanoyl or substituted or unsubstituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolyl, morpholinyl, furyl thienyl, pyrrolyl, tetrahydrofuryl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, piperazinyl or perhydropyridminyl, in which the subsitutent is alkyl, alkoxy, halo, trifluoromethyl, cyano, nitro or hydroxy; or a pharmaceutically acceptable salt thereof; and their use in control of degenerative CNS disease states.Type: GrantFiled: October 10, 1989Date of Patent: July 10, 1990Assignee: American Home Products CorporationInventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia
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Patent number: 4937347Abstract: These 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: GrantFiled: May 5, 1989Date of Patent: June 26, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Usha R. Patel
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Patent number: 4927934Abstract: 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: GrantFiled: May 5, 1989Date of Patent: May 22, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Usha R. Patel
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Patent number: 4924008Abstract: The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.Type: GrantFiled: May 4, 1989Date of Patent: May 8, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Ronald R. Notvest
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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: 4910302Abstract: Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring or a substituted benzene ring, in which said substituents are --OH, --OCH.sub.3, alkyl, halo, --CF.sub.3, --NH.sub.2, monoalkylamino, dialkylamino or alkanoylamino; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl or taken together with the carbon atoms to which they are attached, they form a cycloalkane or cycloalkene ring; m is one of the integers 2-5; R.sup.4 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, amino, alkylamino, phenylamino, tolylamino, xylylamino, mesitylamino, methoxyphenylamino, or halophenylamino; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 19, 1988Date of Patent: March 20, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Gary P. Stack
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Patent number: 4900835Abstract: p is one of the integers 2, 3, 4 or 5;q is one of the integers 1, 2 or 3;and ##STR2## where R.sup.4 is hydrogen, alkyl, alkoxy or halo; or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.Type: GrantFiled: April 7, 1989Date of Patent: February 13, 1990Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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Patent number: 4892943Abstract: 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: GrantFiled: August 26, 1988Date of Patent: January 9, 1990Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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Patent number: 4883875Abstract: The compounds: ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or alkyl and R.sup.6 and R.sup.7, taken together, are tetramethylene, pentamethylene or hexamethylene;p is one of the integers 2, 3, 4 or 5;and ##STR2## where R.sup.4 is hydrogen, alkyl, alkoxy or halo;or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.Type: GrantFiled: April 7, 1989Date of Patent: November 28, 1989Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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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: 4873331Abstract: The compounds of the following structural formula posses useful anxiolytic, antidepressant, antipsychotic and learning and memory enhancement properties: ##STR1## in which R.sup.1 is 3-noradamantyl;n is 0 or 1;X is --CO.sub.2 --, --O.sub.2 C-- or --OCO.sub.2 --;m is 1, 2, 3, 4, or 5;andR.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 9, 1988Date of Patent: October 10, 1989Assignee: American Home Products CorporationInventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia
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Patent number: 4857644Abstract: 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: GrantFiled: June 9, 1988Date of Patent: August 15, 1989Assignee: American Home Products CorporationInventor: Magid A. Abou-Gharbia
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Patent number: 4855430Abstract: 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: GrantFiled: November 12, 1987Date of Patent: August 8, 1989Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Usha R. Patel