Janssen Pharmaceutica Nv

Mcneil Ab

Ortho-mcneil Pharmaceutical Corp.

John E Mills

Neelakandha S Mani

Frank John Villani, Jr

Hua M Zhong

Chennagiri R Pandit

Michael Anthony Letavic

John M Keith

Kiev S Ly

Cynthia Anne Maryanoff

Roy A Olofson

Hua Zhong

Scott Mason Duncan

Georg Feth

Frank J Villani, Jr

Joachim Ernst Berkner

David A Cherry

James D Rodgers

Certain substituted pyridyl amide compounds are histamine Hreceptor modulators useful in the treatment of histamine Hreceptor-mediated diseases.

Substituted pyridyl amide compounds as modulators of the histamine H3 receptor

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Processes are disclosed for making certain compounds of Formula (II): or their pharmaceutically active salts, that are histamine Hreceptor modulators useful in the treatment of histamine Hreceptor-mediated diseases. In one embodiment, the process comprises reacting a compound of formula (7-1): with a compound of formula (B3): in the presence of at least one equivalent of a first base, in a first organic solvent, to give a compound of Formula (II).

The present invention is directed to a one-step process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) 

One step process for the preparation of anticonvulsant derivatives

A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.

Process for producing 1-(5-substituted-2-ethynylphenyl)-2-propanones

Novel compounds, which are aryl-pyrrolyl-imine derivatives of the Formula I ##STR1## and acid addition salts thereof are disclosed; which compounds may be prepared by the acid catalyzed condensation of an imidoyl chloride with a lower alkyl pyrrole-2-acetate; and which compounds are useful as intermediates to form by hydrolysis, the known useful ketone analogs which have anti-inflammatory and analgesic activity; and certain of which compounds have antisecretory, anti-irritable bowel, antidiarrheal and general behavior effect on the CNS properties.

Imidoyl substituted pyrroles

An improved process for preparing fenoctimine, which is 4-(diphenylmethyl)-1-[(octylimino)methyl]piperidine by: (1) reacting dimethylformamide with dimethyl sulfate to form a complex; (2) reacting the resultant dimethylformamide/dimethyl sulfate complex with n-octylamine and optionally with dimethylamine; (3) thereafter treating the reaction with aqueous base to form N,N-dimethyl-N'-octyl-formamidine; and (4) reacting said formamidine, without need for further purification, with 4-(diphenylmethyl) piperidine to obtain 4-(diphenylmethyl)-1-[(octylimino)-methyl]piperidine.

Process for preparation of substituted formamidine and substituted

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Hatfield, PA, United States of America

John E Mills