Pfizer Corporation

Fredric J Vinick

Nicholas A Saccomano

Hiroshi Kondo

John Adams Lowe, Iii

Fumitaka Ito

Arthur A Nagel

Susumu Nakanishi

David L Hageman

Robin W Spencer

W Stephen Faraci

Dihydropyridine derivatives as bradykinin antagonist

A series of aromatic pyrrolidine derivatives and suitable pharmaceutically acceptable salts thereof are disclosed. These compounds are useful as PEP inhibitors in the treatment of Alzheimer's disease, amnesia, dementia, anxiety ischemia, or stroke.

Aromatic pyrrolidine amide prolyl endopeptidase inhibitors

Antidepressant agents having the formula ##STR1## wherein R.sup.1 is a polycycloalkyl group; R.sup.2 is methyl or ethyl, X is O or NH; and Y comprises a 5- or 6-membered heterocyclic ring having one or two nitrogens; or fused bicyclic heterocyclic rings having a total of three nitrogen atoms, one in each ring and one angular nitrogen.

Calcium independent camp phosphodiesterase inhibitor antidepressant

Calcium independent C amp phosphodiesterase inhibitor antidepressant

Antidepressant agents having the formula ##STR1## wherein R.sup.1 is a polycycloalkyl group; R.sup.2 is methyl or ethyl, X is O; and Y comprises a 5-membered heterocyclic ring having one or two nitrogens.

Aryl substituted nitrogen heterocyclic antidepressants

Certain N-substituted nicotinamide compounds having formula (I) below ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is 1-piperidyl, 1-(3-indolyl)ethyl, C.sub.1-4 alkyl, phenyl, 1-(1-phenylethyl), benzyl or mono-substituted benzyl wherein the substituent is methyl, methoxy, chloro or fluoro; and R.sup.2 is bicyclo[2.2.1]hept-2-yl or ##STR2## wherein Y is hydrogen, fluoro or chloro; and X is hydrogen, fluoro, chloro, methoxy, trifluoromethyl, cyano, carboxy, carbo (C.sub.1-4 alkoxy), methylcarbamoyl or dimethylcarbamoyl function as selective inhibitors of calcium-independent phosphodiesterase and are useful as antidepressants.

Antidepressant N-substituted nicotinamide compounds

Process for preparing L-carnosine by reacting L-histidine and tetrahydro-1,3-thiazin-2,4-dione in an aqueous medium at a selected pH and temperature range followed by removal of carbon oxysulfide at acid pH, removal of water and crystallization of product wherein pH adjustments are made with substituted ammonium hydroxides and organic acids having pKa .ltoreq.3.75.

Process for preparing L-carnosine

L-Aspartic acid N-thiocarboxyanhydride is prepared by the reaction of an L-aspartic anhydride addition salt with carbonyl sulfide.

Preparation of L-aspartic acid N-thiocarboxyanhydride

An improved process for the preparation of L-aspartic acid N-thiocarboxyanhydride by the reaction of a 0.75 to 1.25 molar solution of an N-alkoxy-thiocarbonyl L-aspartic acid in a lower alkyl acetate solvent with a phosphorous trihalide. The desired product is substantially insoluble in the lower alkyl acetate solvent and is recovered in pure form without further purification or separation steps.

Process for the preparation of L-aspartic acid N-thiocarboxyanhydride

L-Aspartyl-L-phenylalanine alkyl esters prepared by the reaction of L-aspartic acid N-thiocarboxyanhydride and an appropriate L-phenylalanyl alkyl ester are deodorized by contacting the L-aspartyl-L-phenylalanine alkyl ester in aqueous solution with an effective amount of an alkali metal periodate.

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Waterford, CT, United States of America

Fredric J Vinick