Merrell Dow Pharmaceuticals

Richardson-merrell Inc.

Norbert L Wiech

John M Kane

Michael G Palfreyman

Hsien C Cheng

Albert A Carr

J Martin Grisar

Thomas R Blohm

Johann M Grisar

Richard C Ursillo

Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.

Lactamimides as calcium antagonists

This invention relates to a new class of compounds having important biochemical and pharmacological properties. More particularly, this invention relates to N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5HT.sub.2 receptor site, and to the processes for their preparation and use.

N-aralkyl-piperidine-methanol derivatives

Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activites associated with calcium antagonists.

The invention relates to a new class of compounds having important biochemical and pharmacological properties. More particularly, this invention relates to N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5HT.sub.2 receptor site, and to the processes for their preparation and use.

Novel chemical compounds for the prophylactic treatment of migraine

Novel chemical compounds

N-aralkyl piperidine methanol derivatives and the uses thereof

A method is provided for treating depression in a patient therefrom and requiring rapid symptomatic relief, which comprises administering to said patient concurrently (a) an effective antidepressant amount of a tricyclic antidepressant or a pharmaceutically effective acid addition salt thereof, and (b) an amount of an .alpha.-adrenergic receptor blocking agent effective to achieve rapid onset of the antidepressant action of (a), whereby the onset of said antidepressant action is achieved within from 1 to 7 days. A pharmaceutical composition is also provided which is especially adapted for use with the foregoing method.

TCA Composition and method for rapid onset antidepressant therapy

Compounds having the formula ##STR1## wherein A is a bond or C.sub.1-4 alkylene; R.sup.1, R.sup.2 and R.sup.3 are independently a halogen atom, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, CF.sub.3, SCF.sub.3 or OCF.sub.3 ; R.sup.4 is a hydrogen atom or C.sub.1-4 alkyl; and n, m and q are independently an integer from 0 to 3; and pharmaceutically acceptable acid addition salts thereof, are useful for the treatment of gastrointestinal hypersecretion.

2-(Diphenylalkylimino)piperidine-3-carboxanilides as inhibitors of

A method of treating gastrointestinal hypersecretions which comprises administering substituted lactamimide derivatives.

Lactamimide inhibitors of gastrointestinal hypersecretion

Novel compounds useful as diuretic agents and anticoagulants are represented by the following formula ##SPC1## Wherein m is a positive whole integer of from 1 to 3; n is a positive whole integer of from 3 to 7; R and R.sup.1 may be the same or different and represent hydrogen, a straight or branched lower alkyl chain of from 1 to 4 carbon atoms, halogen, trifluorometyl, trifluoromethylthio, trifluoromethoxy, phenyl, phenoxy, or lower alkoxy of from 1 to 4 carbon atoms, with the proviso that both R and R' are not hydrogen, and with the proviso that when m is equal to 1, and one of R or R.sup.1 is hydrogen the other of R or R.sup.1 is not lower alkoxy of from 1 to 4 carbon atoms; and pharmaceutically acceptable acid addition salts and individual optical isomers where applicable.

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Cincinnati, OH, United States of America

Norbert L Wiech