Sterling Drug Inc.

Denis M Bailey

Mark P Wentland

Virendra Kumar

Thomas E D'Ambra

Ronald G Powles

George Y Lesher

Alan M Ezrin

N-[(alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.

1H-pyrazole-1-(branched)alkanamides as antiarrhythmic agents,

N-[(alkylamino)alkyl]-4,5-diaryl-1H-imidazole-1-acetamides useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of a diaryl imidazole-1-acetic acid with an appropriate diamine.

1H-imidazole-1-acetamides

N-[(alkylamino)alkyl]-4,5-diaryl-1H-pyrazole-1-acetamides, wherein at least one of the aryl substituents is a pyridine, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine.

Pyridinyl-1H-pyrazole-1-alkanamides as antiarrhythmic agents

N-[alkylamino)alkyl]-3,4(or 4,5)-diaryl-1H-pyrazole-1-(branched)alkanamides and pyrazole-1-alkanamines useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine followed by reduction or by reacting the anion of a lower-alkyl ester of a pyrazole-1-acetic acid with an alkylating agent followed by displacement of the ester by an appropriate amine.

1H-pyrazole-1-alkanamines antiarrhythmic compositions and use

N-[(heterocycle)alkyl]-3,4 (or 4,5)-diaryl-1H-pyrazole-1-acetamides and pyrazole-1-propanamides, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic or propanoic acid with an appropriate (heterocycle-alkyl) amine or by reacting a pyrazole-1-acetic or propanoic acid with an appropriate (heterocycle-alkyl)amine.

N-(heterocycle)alkyl)-1H-pyrazole-1-alkanamides as antiarrhythmic

N-[(disubstituted amino)alkyl]-3,4 or 5-aryl-1H-pyrazole-1-acetamides, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic acid with an appropriate diamine.

3,4, or 5-aryl-1H-pyrazole-1-alkanamides as antiarrhythmic agents,

N-[(disubstituted amino)alkyl]-3,4 (or 4,5)-diaryl-1H-pyrazole-1-acetamides and pyrazole-1-propanamides, useful for treating cardiac arrhythmias in mammals, are prepared by reacting a lower-alkyl ester of pyrazole-1-acetic or propanoic acid with an appropriate diamine or by reacting a lower-alkyl ester of a pyrazole-1-acetic or propanoic acid with an .omega.-aminoalkanol, followed by activation of the alcohol and displacement by an appropriate amine.

1H-pyrazole-1-alkanamides, antiarrhythmic compositions and use

N-[1-alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidine)-octanamine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and nonliving surfaces and most especially against pathogenic dental microbes, and a process for perparation, methods of use and compositions thereof are disclosed.

Antimicrobial N-[1-(alkyl or

A method for inhibiting the growth of malignant cells in a mammal, said cells being susceptible to the action of a compound of the formula

Method for treating malignant conditions

Novel lower-alkyl 2-(hydroxyphenylamino)benzoates, useful as inhibitors of lipoxygenase, are of the formula ##STR1## wherein R is hydrogen, lower-alkyl or lower-alkoxy; R' is hydrogen or lower-alkyl; R' is hydrogen, lower-alkyl or halo; and Alk is lower-alkyl. The compounds are prepared by de-etherification of the corresponding alkyl or benzyl ethers.

Compositions containing substituted aminobenzoates and use thereof as

A series of 4-pyridinylaminobenzamides, useful as antihypertensive agents, was prepared from the corresponding 4-pyridinylaminobenzoic acids by reacting the acid chloride of the latter with ammonia or a primary or secondary amine. Alternatively the compounds were prepared by reacting an aminobenzamide with 4-chloropyridine or equivalent reagent.

Antihypertensive pyridylaminobenzamide compounds

N-[1-(alkyl or arylmethyl)-4(1H)-pyridinylidine]-alkanamine and pharmaceutically acceptable acid addition salts thereof, for example, N-(1-octyl-4(1H)-pyridinylidine)octanamine monohydrochloride salt, which are useful as antimicrobial agents, especially on living tissues and nonliving surfaces and most especially against pathogenic dental microbes, and a process for preparation, methods of use and compositions thereof are disclosed.

Antimicrobial (N-1-octyl-4(1H)-pyridinylidine)octanamine and acid

The method of providing cytoprotection of the gastric mucosa in a mammal receiving aspirin perorally which comprises orally administering either prior to or in combination with aspirin a cytoprotectively effective amount of sodium thiosulfate alone or in combination with a pharmaceutically acceptable carrier. Also shown is a composition for providing cytoprotection of the gastric mucosa in a mammal receiving aspirin perorally which comprises aspirin in combination with a cytoprotectively effective amount of sodium thiosulfate.

Gastric cytoprotection with sodium thiosulfate in oral administration of

The method of providing cytoprotection of the gastric mucosa in a mammal receiving aspirin (ASA) perorally which comprises orally administering either prior to or in combination with ASA a cytoprotectively effective amount of 3,3'-thiobis[propanoic acid] (TBPA) or in combination with a pharmaceutically acceptable carrier. Also shown is a composition for providing cytoprotection of the gastric mucosa in a mammal receiving ASA perorally which comprises ASA in combination with a cytoprotectively effective amount of TBPA.

Gastric cytoprotection with 3,3'-thiobis[propanoic acid] in oral

Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R' is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.

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East Greenbush, NY, United States of America

Denis M Bailey