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: 4192885
    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: March 8, 1979
    Date of Patent: March 11, 1980
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4186208
    Abstract: A pharmaceutical formulation containing, as active ingredient, a compound of the Formula III: ##STR1## wherein A is a group selected from --(CH.sub.2).sub.2 --; --(CH.sub.2).sub.3 --; --(CH.sub.2).sub.4 --; --(CH.sub.2).sub.5 --; ##STR2## wherein R is ethyl, vinyl, or cyclopropyl; and wherein X is bromo or chloro, or the pharmacologically acceptable acid addition salts for the treatment of depression in warm-blooded animals, including man.
    Type: Grant
    Filed: January 29, 1979
    Date of Patent: January 29, 1980
    Assignee: The Upjohn Company
    Inventors: Michael P. Kane, Jacob Szmuszkovicz
  • Patent number: 4180522
    Abstract: The present specification provides compounds of the formula: ##STR1## wherein A is a group selected from --(CH.sub.2).sub.2 --; --(CH.sub.2).sub.3 --; --(CH.sub.2).sub.4 --; ##STR2## wherein R is ethyl, vinyl, or cyclopropyl; and wherein X is bromo or chloro. These compounds, including the pharmacologically acceptable salts thereof, are disclosed as useful antidepressant agents in warm-blooded animals, particularly man.
    Type: Grant
    Filed: August 16, 1978
    Date of Patent: December 25, 1979
    Assignee: The Upjohn Company
    Inventors: Michael P. Kane, Jacob Szmuszkovicz
  • Patent number: 4179501
    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: December 18, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4172898
    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: May 30, 1978
    Date of Patent: October 30, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4169156
    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: June 5, 1978
    Date of Patent: September 25, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4159339
    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]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: May 30, 1978
    Date of Patent: June 26, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4159340
    Abstract: N-(2-Aminocyclopentyl)-N-acylanilides and their 2-N-oxides of the formula ##STR1## e.g., trans-3,4-dichloro-N-[2-(N-allylamino)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: May 15, 1978
    Date of Patent: June 26, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4157398
    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 21, 1978
    Date of Patent: June 5, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4156733
    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 21, 1978
    Date of Patent: May 29, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4156014
    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]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: March 13, 1978
    Date of Patent: May 22, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4156015
    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-depresssant 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: April 10, 1978
    Date of Patent: May 22, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4153717
    Abstract: Cis- and trans-N-(2-aminocycloaliphatic)benzamide compounds of the formula ##STR1## e.g., N-methyl-N-[2-[(2-furylmethyl)methylamino]cyclohexyl]-3,4-dichlorobenzamid e, 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 15, 1978
    Date of Patent: May 8, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4152459
    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 parmaceutically 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: May 1, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4148914
    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 10, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4145435
    Abstract: Cis- and trans-N-(2-aminocycloaliphatic)-2-arylacetamide derivative compounds of the formula ##STR1## e.g., N-?2-(N', N'-dimethylamino)cyclohexyl!-N-methyl-2-(4-bromophenyl)acetamide and trans-N-methyl-N-?2-(1-pyrrolidinyl)cyclohexyl!acetamide, 2-(3,4-dichlorophenyl) and their pharmaceutically acceptable salts, have been found to have potent analgesic activity, and the preferred compounds have in addition only low to moderate apparent physical dependence liability, compared to morphine and methadone. As analgesics they would be useful also as antitussives. Processes for preparation of these compounds are also disclosed. This invention also includes compositions containing these compounds useful in pharmaceutical dosage unit form for alleviating pain in humans and animals, as well as methods for alleviating pain in animals and humans with these compositions.
    Type: Grant
    Filed: November 12, 1976
    Date of Patent: March 20, 1979
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4128663
    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: May 16, 1977
    Date of Patent: December 5, 1978
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 4098904
    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: November 12, 1976
    Date of Patent: July 4, 1978
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 3966736
    Abstract: 2,9-Dihydro-3H-pyrido[3,2-c]-s-triazolo[4,3-a][1,5]-benzodiazepin-3-ones ##SPC1##Wherein R' and R" are alkyl of 1 to 3 carbon atoms, inclusive; or the group ##EQU1## together is pyrrolidino, piperidino, 4-methylpiperazino or [4-(2-hydroxyethyl)]piperazino; wherein R.sub.2 and R.sub.3 are hydrogen, chloro, bromo, trifluoromethyl, or alkyl defined as above and wherein R.sub.4 is hydrogen, alkyl as defined above or ##EQU2## in which n is the integer 2 or 3 or R', R" or ##EQU3## are defined as above, are obtained by reacting a compound of the formula 1 ##SPC2##Wherein R.sub.2, R.sub.3, R', R", or ##EQU4## are defined as above, with phosphorus pentasulfide to give the corresponding 5-thione compound (II); treating II with an alkyl carbazate to obtain the compound of formula III: ##SPC3##wherein R.sub.2, and R.sub.
    Type: Grant
    Filed: April 7, 1975
    Date of Patent: June 29, 1976
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz
  • Patent number: 3933816
    Abstract: A compound of the formula: ##SPC1##Wherein R, R.sub.0, and R.sub.3 are hydrogen or alkyl of 1 to 3 carbon atoms, inclusive; wherein R.sub.1 and R.sub.2 are alkyl of 1 to 3 carbon atoms, or the group ##EQU1## together is pyrrolidino, piperidino, morpholino and N-methylpiperazino; wherein R.sub.7 is 2-pyridyl or a phenyl radical of the formula ##SPC2##Wherein R.sub.4 is hydrogen, fluoro, or chloro; wherein R.sub.5 is hydrogen or fluoro, with the proviso that R.sub.5 is not fluoro, when R.sub.4 is chloro; and wherein R.sub.6 is hydrogen, chloro, fluoro, bromo, trifluoromethyl, or nitro.The new compounds of formula II have tranquilizing and antianxiety activity and are thus useful to treat mammals and birds.
    Type: Grant
    Filed: September 12, 1974
    Date of Patent: January 20, 1976
    Assignee: The Upjohn Company
    Inventor: Jacob Szmuszkovicz