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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Analgesic N-{2-[N'-(2-furylmethyl and 2-thienyl-methyl)-N'-alkylamino]cycloaliphatic}cyanobenzamides
Patent number: 4192885Abstract: 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: March 8, 1979Date of Patent: March 11, 1980Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz -
Patent number: 4186208Abstract: 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: GrantFiled: January 29, 1979Date of Patent: January 29, 1980Assignee: The Upjohn CompanyInventors: Michael P. Kane, Jacob Szmuszkovicz
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Patent number: 4180522Abstract: 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: GrantFiled: August 16, 1978Date of Patent: December 25, 1979Assignee: The Upjohn CompanyInventors: Michael P. Kane, Jacob Szmuszkovicz
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Patent number: 4179501Abstract: 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: December 18, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4172898Abstract: 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: May 30, 1978Date of Patent: October 30, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4169156Abstract: 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: June 5, 1978Date of Patent: September 25, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4159339Abstract: 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: GrantFiled: May 30, 1978Date of Patent: June 26, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4159340Abstract: 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: GrantFiled: May 15, 1978Date of Patent: June 26, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4157398Abstract: 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 21, 1978Date of Patent: June 5, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4156733Abstract: 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 21, 1978Date of Patent: May 29, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4156014Abstract: 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: GrantFiled: March 13, 1978Date of Patent: May 22, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4156015Abstract: 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: GrantFiled: April 10, 1978Date of Patent: May 22, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4153717Abstract: 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: GrantFiled: May 15, 1978Date of Patent: May 8, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4152459Abstract: 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: GrantFiled: May 10, 1978Date of Patent: May 1, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4148914Abstract: 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 10, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4145435Abstract: 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: GrantFiled: November 12, 1976Date of Patent: March 20, 1979Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4128663Abstract: 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: May 16, 1977Date of Patent: December 5, 1978Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 4098904Abstract: 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: November 12, 1976Date of Patent: July 4, 1978Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 3966736Abstract: 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: GrantFiled: April 7, 1975Date of Patent: June 29, 1976Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz
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Patent number: 3933816Abstract: 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: GrantFiled: September 12, 1974Date of Patent: January 20, 1976Assignee: The Upjohn CompanyInventor: Jacob Szmuszkovicz