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).

  • Patent number: 6436954
    Abstract: 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: Grant
    Filed: March 14, 2001
    Date of Patent: August 20, 2002
    Assignees: American Biogenetic Sciences, Inc., University College Dublin
    Inventors: Jacob Szmuszkovicz, Ciaran Regan
  • Patent number: 4978753
    Abstract: 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: Grant
    Filed: November 2, 1989
    Date of Patent: December 18, 1990
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4801604
    Abstract: 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: Grant
    Filed: July 21, 1987
    Date of Patent: January 31, 1989
    Assignee: The Upjohn Company
    Inventors: Philip F. Vonvoigtlander, Jacob Szmuszkovicz
  • Patent number: 4652559
    Abstract: 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: Grant
    Filed: July 22, 1985
    Date of Patent: March 24, 1987
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4598088
    Abstract: 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: Grant
    Filed: May 29, 1985
    Date of Patent: July 1, 1986
    Assignee: The Upjohn Company
    Inventors: Jacob Szmuszkovicz, John M. McCall, Lester J. Kaplan, Moses W. McMillan
  • Patent number: 4590187
    Abstract: 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: Grant
    Filed: December 19, 1984
    Date of Patent: May 20, 1986
    Assignee: The Upjohn Company
    Inventors: Donald P. Wallach, deceased, Donald E. Ayer, Jacob Szmuszkovicz
  • Patent number: 4540690
    Abstract: 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: Grant
    Filed: August 16, 1982
    Date of Patent: September 10, 1985
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4466977
    Abstract: 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: Grant
    Filed: November 4, 1982
    Date of Patent: August 21, 1984
    Assignee: The Upjohn Company
    Inventors: Moses W. McMillan, Jacob Szmuszkovicz
  • Patent number: 4460600
    Abstract: 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: Grant
    Filed: November 4, 1982
    Date of Patent: July 17, 1984
    Assignee: The Upjohn Company
    Inventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
  • Patent number: 4360531
    Abstract: [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: Grant
    Filed: April 9, 1981
    Date of Patent: November 23, 1982
    Assignee: The Upjohn Company
    Inventors: Moses W. McMillan, Jacob Szmuszkovicz
  • Patent number: 4359476
    Abstract: 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: Grant
    Filed: April 9, 1981
    Date of Patent: November 16, 1982
    Assignee: The Upjohn Company
    Inventors: Lester J. Kaplan, Moses W. McMillan, Jacob Szmuszkovicz
  • Patent number: 4286106
    Abstract: 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: Grant
    Filed: July 30, 1979
    Date of Patent: August 25, 1981
    Assignee: The Upjohn Company
    Inventors: Michael P. Kane, Jacob Szmuszkovicz
  • Patent number: 4217362
    Abstract: 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: Grant
    Filed: August 3, 1978
    Date of Patent: August 12, 1980
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4215114
    Abstract: 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: Grant
    Filed: March 5, 1979
    Date of Patent: July 29, 1980
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4212878
    Abstract: 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: Grant
    Filed: January 26, 1978
    Date of Patent: July 15, 1980
    Assignee: The Upjohn Company
    Inventors: Daniel Lednicer, Jacob Szmuszkovicz
  • Patent number: 4212888
    Abstract: 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: Grant
    Filed: August 3, 1978
    Date of Patent: July 15, 1980
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4204003
    Abstract: 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: Grant
    Filed: February 9, 1978
    Date of Patent: May 20, 1980
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4199589
    Abstract: 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: Grant
    Filed: February 6, 1979
    Date of Patent: April 22, 1980
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4197308
    Abstract: 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: Grant
    Filed: May 10, 1978
    Date of Patent: April 8, 1980
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: RE30837
    Abstract: 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: Grant
    Filed: September 24, 1980
    Date of Patent: December 29, 1981
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz