Patents by Inventor Jacob Szmuszkovicz
Jacob Szmuszkovicz 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: 6436954Abstract: Benzo[b]quinolizidine and benzo[f]indolizidine derivatives are provided which are useful for the treatment of Alzheimer's disease, senile dementia or other conditions characterized by memory loss. Pharmaceutical compositions containing these compounds, and methods for their use, are also provided.Type: GrantFiled: March 14, 2001Date of Patent: August 20, 2002Assignees: American Biogenetic Sciences, Inc., University College DublinInventors: Jacob Szmuszkovicz, Ciaran Regan
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Patent number: 4978753Abstract: A 7-phenylpyrimido[1,2-a][1,4]benzodiazepin-3(5H)-ones of the formula II: ##STR1## wherein R.sub.o is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, --COOR in which R is alkyl defined as above, ##STR2## in which n is a number of 1 to 4, R.sub.6 and R.sub.7 are hydrogen or alkyl defined as above or together ##STR3## is selected from the group consisting of pyrrolidino, piperidino, morpholino, and 4-methylpiperazino, and --CH.sub.2 OH; wherein R.sub.1 is selected from the group consisting of hydrogen, hydroxy, acetoxy, propionoxy, succinyloxy, and alkyl esters thereof; wherein R.sub.2, R.sub.3, R.sub.4, and R.sub.Type: GrantFiled: November 2, 1989Date of Patent: December 18, 1990Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4801604Abstract: Certain cis-N-(2-amino-cycloalophatic)benzamides of the formula ##STR1## where m is 0, n is 2, r is alkyl, R.sub.1 and R.sub.2 are taken together with the nitrogen denote a pyrrolidine ring, X and Y are hydrogen or a halogen having an atomic number of from 9 to 35, e.g., cis-3,4-dichloro-N-methyl-n[2-(1-pyrrolidinyl)cyclohexyl]benzamide, and salts thereof, have been found to have CNS seizure blocking or preventing drug action, e.g., anti-convulsant drug properties with little or no analgesic properties.Type: GrantFiled: July 21, 1987Date of Patent: January 31, 1989Assignee: The Upjohn CompanyInventors: Philip F. Vonvoigtlander, Jacob Szmuszkovicz
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Patent number: 4652559Abstract: 2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.Type: GrantFiled: July 22, 1985Date of Patent: March 24, 1987Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4598088Abstract: N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., (1.alpha.,2.beta.)-(.+-.)-3,4-dichloro-N-[2-(2,5-dihydro-1H-pyrrol-1-yl)cy clohexyl]-N-methylbenzeneacetamide, and salts thereof, have useful analgesic activity, low abuse or physical dependence liability properties. Processes for their preparation are disclosed. Pharmaceutical compositions containing such compounds and methods for their use are also disclosed.Type: GrantFiled: May 29, 1985Date of Patent: July 1, 1986Assignee: The Upjohn CompanyInventors: Jacob Szmuszkovicz, John M. McCall, Lester J. Kaplan, Moses W. McMillan
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Patent number: 4590187Abstract: The present invention provides certain novel 4,1-benzoxazepin-2(3H)-ones which are useful as inhibitors of phospholipase A.sub.2 and thus as inhibitors of arachidonate mobilization. These compounds are thus useful whenever it is medically necessary or desirable to inhibit the biosynthesis of the products of the arachidonic acid cascade.Type: GrantFiled: December 19, 1984Date of Patent: May 20, 1986Assignee: The Upjohn CompanyInventors: Donald P. Wallach, deceased, Donald E. Ayer, Jacob Szmuszkovicz
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Patent number: 4540690Abstract: 2-(Phenylmethylene)cycloalkylamines and -azetidines of the formula ##STR1## and acid addition salts thereof, e.g., 1-[2-(phenylmethylene)cyclohexyl]azetidine, and related compounds, which have analgesic, antidepressant and mixed analgesic/antidepressant central nervous system (CNS) activities, and which are useful in treating pain and/or depression in mammals including humans. The invention provides processes for preparing the compounds as well as compositions containing the compounds and methods for using the compounds as analgesic and/or antidepressant drugs for humans and valuable mammalian animals.Type: GrantFiled: August 16, 1982Date of Patent: September 10, 1985Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4466977Abstract: Cis- and trans-N-[2-amino(oxy- or thia group-substituted-cycloaliphatic)]benzeneacetamide and -benzamide compounds, e.g., 3,4-dichloro-N-[4,4-dimethoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzen eacetamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.Type: GrantFiled: November 4, 1982Date of Patent: August 21, 1984Assignee: The Upjohn CompanyInventors: Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4460600Abstract: Cis- and trans-N-[2-amino(adjacenty substituted bis(alkyloxy), bis(alkylthio), alkylthio or mercapto group substituted)-cycloaliphatic]benzeneacetamide and -benzamide compounds, e.g., (.+-.)-(1.alpha.,2.beta.)-4-bromo-N-[3,3-dimethoxy-2-(1-pyrrolidinyl)cyclo hexyl]-N-methylbenzamide, and salts thereof, are provided. These compounds have analgesic properties. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also provided.Type: GrantFiled: November 4, 1982Date of Patent: July 17, 1984Assignee: The Upjohn CompanyInventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4360531Abstract: [2-Amino(substituted cycloaliphatic)]benzeneacetamide and benzamide compounds, e.g., trans-3,4-dichloro-N-methyl-N-[7-(1-pyrrolidinyl)-1,4-dioxaspiro[4.5]dec-8 -yl]benzeneacetamide, have useful analgesic activity and low abuse or physical dependence liability, or are useful as chemical intermediates for producing such analgesic compounds. Processes for their preparation are disclosed. Pharmaceutical compositions and methods of use are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: November 23, 1982Assignee: The Upjohn CompanyInventors: Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4359476Abstract: N-[2-Amino(oxy or thio group) substituted-cycloaliphatic]phenylacetamide and -benzamide compounds, having the oxy- or thio group substituents on a cycloaliphatic ring carbon adjacent to either of the nitrogen bearing carbons of the cycloaliphatic ring, e.g., cis- and trans-4-bromo-N-[3-methoxy-2-(1-pyrrolidinyl)cyclohexyl]-N-methylbenzamide , and trans-3,4-dichloro-N-methyl-N-[7-(1-pyrridolinyl)-1,4-dioxaspiro[4.5]dec-6 -yl]benzeneacetamide, and salts thereof, have useful analgesic activity and low abuse liability in humans and valuable warm blooded animals. Processes for their production and pharmaceutical compositions and method of use are also disclosed.Type: GrantFiled: April 9, 1981Date of Patent: November 16, 1982Assignee: The Upjohn CompanyInventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
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Patent number: 4286106Abstract: The present invention relates to novel organic compounds, useful as antidepressant agents. Further provided are novel methods for the preparation of these compounds and pharmaceutical compositions and methods of use. Particular compounds comprising an aspect of the present invention are N-[.omega.-(dimethylamino)alkyl]-3',4'-dichloropropionanilides.Type: GrantFiled: July 30, 1979Date of Patent: August 25, 1981Assignee: The Upjohn CompanyInventors: Michael P. Kane, Jacob Szmuszkovicz
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Patent number: 4217362Abstract: Anilide derivative compounds of the formula ##STR1## e.g., trans-N-(2-hydroxycyclopentyl)-3',4'-dichloropropionanilide, have been found to possess potent Central Nervous System (CNS) antidepressant properties.These compounds are promising antidepressant drugs which are characterized by less toxicity than imipramine, and long-acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are also disclosed.Type: GrantFiled: August 3, 1978Date of Patent: August 12, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4215114Abstract: Cis - and trans-N-(2-aminocycycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-[(2-furylmethyl)methylamino]-cyclohexyl]-3,4-dichlorobenzami de, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm-blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.Type: GrantFiled: March 5, 1979Date of Patent: July 29, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4212878Abstract: N-[(1-Amino-4-(mono or di-oxygen-group-substituted)cyclohex-1-yl)methyl]phenylacetamide derivatives of the formula 1 ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, P, Q, X and Y are defined in the specification, e.g., 2-(3,4-dichlorophenyl)-N-[[8-(1-pyrrolidinyl)-1,4-dioxaspiro[4.5]dec.-8-yl ]methyl]acetamide, and their pharmacologically acceptable salts, have analgesic drug properties with lower physical dependence liability characteristics than morphine or methadone, for use as analgesic drugs in mammalian animals including humans.Type: GrantFiled: January 26, 1978Date of Patent: July 15, 1980Assignee: The Upjohn CompanyInventors: Daniel Lednicer, Jacob Szmuszkovicz
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Patent number: 4212888Abstract: Anilide derivative compounds of the formula ##STR1## e.g., trans-N-(2-hydroxycyclopentyl)-3',4'-dichloropropionanilide, have been found to possess potent Central Nervous System (CNS) antidepressant properties.These compounds are promising antidepressant drugs which are characterized by less toxicity than imipramine, and long-acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are also disclosed.Type: GrantFiled: August 3, 1978Date of Patent: July 15, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4204003Abstract: N-(2-Aminocyclopentyl)N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(dimethylamino)cyclopentyl]propionanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System anti-depressant properties. Many of them are new.These compounds are promising anti-depressant drugs which are characterized by a better therapeutic ratio than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.Type: GrantFiled: February 9, 1978Date of Patent: May 20, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4199589Abstract: N-(2-aminocycloheptyl)-N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(dimethylamino)cycloheptyl]acrylanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System anti-depressant properties. Many of them are new.These compounds are promising anti-depressant drugs which are characterized by lower toxicity than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.Type: GrantFiled: February 6, 1979Date of Patent: April 22, 1980Inventor: Jacob Szmuszkovicz
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Patent number: 4197308Abstract: Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-(N-pyrrolidinyl)cyclohexyl]-3,4- dichlorobenzamide, and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in warm blooded animals, as well as methods for alleviating pain in animals with these compositions. Processes for preparing the compounds are also disclosed.Type: GrantFiled: May 10, 1978Date of Patent: April 8, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: RE30837Abstract: N-(2-aminocycloheptyl)N-alkanoylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(allylamino)cycloheptyl]propionanilide, and their pharmacologically acceptable salts, have been found to possess potent Central Nervous System antidepressant properties. Many of them are new.These compounds are promising antidepressant drugs which are characterized by lower toxicity than imipramine, and long acting activity which may allow longer durations between administrations, e.g., once a day. Pharmaceutical compositions containing these compounds and a process for treating conditions of depression with these compositions are disclosed.Type: GrantFiled: September 24, 1980Date of Patent: December 29, 1981Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz