Janssen Pharmaceutica Nv

Janssen Pharmacetuica N.v.

Frans M Van Den Keybus

Georges H Van Daele

Paul A Janssen

Jean-Paul R Bosmans

Marcel A Janssen

Karin J Nuyens

Marc G Verdonck

Georges H Van Daele, Deceased

Peter Jules Van Daele

Marie-Louise Hendrickx

Glenn Kurt Van Daele

Kurt Godfried Van Daele

Marie L Hendrickx, Heiress

Peter Jv Van Daele, Heir

Glenn Kl Van Daele, Heir

Kurt Gce Van Daele, Heir

The present invention concerns novel (2-morpholinylmethyl)benzamide derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sup.2 is hydrogen, halo or C.sub.1-6 alkylsulfonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is a radical of formula R.sup.4 --C(.dbd.O)--Alk-- (a); R.sup.5 --C(.dbd.O)--N(R.sup.6)--Alk-- (b); or R.sup.7 --C(.dbd.O)--O--Alk-- (c); wherein each Alk is independently C.sub.1-12 alkanediyl; R.sup.4 is hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.5 and R.sup.7 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.6 is hydrogen or C.sub.1-6 alkyl; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy. It further relates to pharmaceutical compositions comprising them, processes for preparing said compounds and compositions, and the use thereof as a medicine, in particular in the conditions involving a decreased gastric emptying.

(2-morpholinylmethyl) benzamide derivatives

N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2h-benzopyran,

N- (3-hydroxy-4-piperidinyl) (benzodioxolane, benzodioxane or

N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2-H-benzopyran or

N-(3-hydroxy-4-piperidinyl) (dihydrobenzofuran, dihydro-2H-benzopyran or

N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or

There are disclosed chemical intermediates of the formula: ##STR1## a salt or a stereochemically isomeric form thereof, wherein: wherein one or two hydrogen atoms in the dihydro-1,4-dioxane moiety may be replaced by a C.sub.1-6 alkyl group;

N-(3-hydroxy-4-piperidinyl) dihydrobenzofuran, (dihydro-2H-benzopyran or

N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system are disclosed, wherein the compounds have the formula: ##STR1## A represents a group of the formula: --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 -- wherein one or two hydrogen atoms in the A moiety may be replaced by a C.sub.1-6 alkyl group.

N-(3-hydroxy)-4-piperidinyl) (Dihydrobenzofuran, dihydro-2H-benzopyran

The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.

Method of treating HIV-1 with .alpha.-substituted benzenemethanamine

.alpha.-substituted benzenemethanamine derivatives and pharmaceutical use

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Essen, Belgium

Frans M Van Den Keybus