Jacob J Szmuszkovicz

6436954, Aug 20, 2002

Mar 14, 2001

09/744183

Jacob Szmuszkovicz - Kalamazoo MI
Ciaran Regan - Dublin, IE

American Biogenetic Sciences, Inc. - Copiague NY
University College Dublin - Dublin

A61K 31473

514294, 514290, 546 94

Benzo[b]quinolizidine and benzo[f]indolizidine derivatives are provided which are useful for the treatment of Alzheimers disease, senile dementia or other conditions characterized by memory loss. Pharmaceutical compositions containing these compounds, and methods for their use, are also provided.

42861063, Aug 25, 1981

Jul 30, 1979

6/061569

Michael P. Kane - Kalamazoo MI
Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

C07C10375

564220

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.

42040035, May 20, 1980

Feb 9, 1978

5/876349

Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

A61K 31165
C07C10320
C07C10322

424324

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.

41862082, Jan 29, 1980

Jan 29, 1979

6/007127

Michael P. Kane - Kalamazoo MI
Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

C07C10319
C07C10344
A61K 3116
A61K 31165

424324

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.

43605311, Nov 23, 1982

Apr 9, 1981

6/252535

Moses W. McMillan - Portage MI
Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

C07D48700
A61K 3140

424274

[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.

39667367, Jun 29, 1976

Apr 7, 1975

5/565709

Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

C07D47114

260268PC

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. 3 are defined as above and treating III with an alkyl halide of 1 to 3 carbon atoms inclusive, or ##EQU5## in which n, R', R", or ##EQU6## is defined as above, to obtain those compounds of formula IVA in which R. sub. 4 is alkyl or ##EQU7## as defined above.

46525599, Mar 24, 1987

Jul 22, 1985

6/757819

Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

C07D40508
A61K 31395

514210

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.

41928857, Mar 11, 1980

Mar 8, 1979

6/018550

Jacob Szmuszkovicz - Kalamazoo MI

The Upjohn Company - Kalamazoo MI

A61K 3134
A61K 3138
C07D30754
C07D33324

424275

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.