Smithkline Corporation

Smithkline Beckman Corporation

William D Kingsbury

Robert J Gyurik

Charles Gilvarg

Gregory Gallagher

Roger C Parish

Clifton A Baile

Prodrugs are described whose structures have a oligopeptide chain which is substituted by a nucleophilic chemotherapeutic residue at the .alpha.-position. The products have increased cell membrane permeability and beneficial physico-chemical properties.

Oligopeptide prodrugs

A series of prodrugs is described which have improved antimicrobial activity and physico-chemical properties. The structures of the biologically active ingredients are characterized by having a selected oligopeptide backbone attached, via the .alpha.-carbon of an L-alanyl unit thereof, by means of a disulfide link to the residue of an antimicrobial mercaptan.

Antimicrobial disulfide prodrugs

New anthelmintic compounds, compositions and methods of use are described utilizing 5-cycloalkylthio and oxy-2-carbalkoxyaminobenzimidazole. Methods of preparation involve the reaction of 4-cycloalkylthio- or oxy-o-phenylenediamine with methyl cyanocarbamate in aqueous miscible organic solvents.

5-Cycloalkyl thio- and oxy-2-carbalkoxyaminobenzimidazoles

A method for dephthaloylation of azetidinone compounds which contain a phthalimido group to produce useful aminoazetidinone intermediates comprises reaction with methyl hydrazine at low temperatures.

Intermediate for dephthaloylation of azetidinone compounds

New anthelmintic compositions and methods of use are described utilizing 5-cycloalkylthio and oxy-2-carbalkoxyaminobenzimidazoles as active ingredients.

Methods and compositions using 5-cycloalkylthio- and

4-Sulfanilamidothiazole having antibacterial activity is prepared from the previously unknown 4-aminothiazole.

4-Sulfanilamidothiazole

Compositions and methods for inducing polyphagia or eating in meat producing animals comprise administering orally or preferably by injection an effective but nontoxic subpharmacodynamic quantity of a benzhydryl ether active ingredient. Preferred active ingredients are tropine benzohydryl ether, 3-quinuclidinyl benzohydryl ether or their nontoxic acid addition salts.

Methods for improving the feed intake of meat producing animals

New methyl benzimidazolecarbamate compounds having a heterocyclic thio or oxy moiety at position 5, useful as anthelmintics are described. Methyl-5-(pyridylthio)- and 5-(pyridylmethylthio)-benzimidazolecarbamates are preferred.

Anthelmintic 5-heterocycliothio and oxy-2-carbalkoxyaminobenzimidazles

4-Aminothiazole is prepared in stable useful form by alkaline hydrolysis of 4-trifluoroacetamidothiazole. Also prepared are 4-sulfathiazole and 2-(4-thaizolyl)-indazole.

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West Chester, PA, United States of America

William D Kingsbury