Janssen Pharmaceutica Nv

Tanssen Pharmaceutica N.v.

Jean-Paul R Bosmans

Georges H Van Daele

Paul A Janssen

Marc G Verdonck

Marcel A Janssen

Frans M Van Den Keybus

Willy Joannes Van Laerhoven

Michel A De Cleyn

Georges H Van Daele, Deceased

Joannes Adrianus Schuurkes

Karin J Nuyens

Guy Rosalia Van Lommen

Christopher John Love

Peter Jules Van Daele

Kurt Godfried Van Daele

Marie-Louise Hendrickx

Glenn Kurt Van Daele

Michel Anna Decleyn

Henri Elisabeth D'Haen

Ann Louise Meulemans

Glenn Kurt Van Daele, Heir

Peter Jules Van Daele, Heir

Kurt Godfried Van Daele, Heir

Marie-Louise Hendrickx, Heir

John Christopher Love

2,4-diaminopyrimidine derivates as dopamine D4 receptor antagonist

Esters of 3-hydroxy-piperidinemethanol derivatives

Use of 5HT4 receptor antagonists for overcoming gastrointestinal effects

The present invention is concerned with a novel benzamide derivative for formula (I). ##STR1## Pharmaceutical compositions comprising said novel compounds, processes for preparing compounds and compositions, and the use thereof as a medicine, in particular in the treatment of conditions involving a decreased motility of the intestine are described.

Enterokinetic benzamide

Phenyl-oxo-alkyl-(4-piperidinyl)benzoate derivatives

Method of treating 5-HT.sub.3 -mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) ##STR1## the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.C(Cl)--CH.dbd.CH--(b) or --CH.dbd.CH--C(Cl)=CH-- (c); n represents 2, 3 or 4; R.sup.3 represents hydrogen or methoxy; m represents 1 or 2; R.sup.4 represents hydrogen, amino or C.sub.1-3 -alkylcarbonylamino; and R.sup.5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.

Dimethylbenzofuran and dimethylbenzopyran derivatives and their use as

Prokinetic compounds

A compound for use as a medicine having the formula ##STR1## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cyclo-alkyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom bearing said R.sup.1 and R.sup.2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C.sub.1-4 alkylpiperazinyl group; X is O or S; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl-carbonyl, aminocarbonyl, or hydroxy; R.sup.7 is hydrogen or halo; and R.sup.8, R.sup.9 and R.sup.10 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, hydroxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, (trifluoromethyl)carbonyl, aminocarbonyl, (cyclopropyl)carbonyl or a radical C.sub.1-6 alkyl-(C.dbd.Y)- wherein .dbd.Y represents .dbd.O, .dbd.N--OH, .dbd.N--OCH.sub.3, .dbd.N--NH.sub.2 or .dbd.N--N(CH.sub.3).sub.2 ; provided that (1) R.sup.1 is other than n-propyl when R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 represent hydrogen, R.sup.8 represents 4-ethoxy and X represents oxygen, and (2) X is other than sulfur, when R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9 and R.sup.10 represent hydrogen and R.sup.4 and R.sup.5 represent 3,4-dimethoxy. Novel compounds, pharmaceutical compositions containing said compounds of formula (I), and processes for preparing compositions.

HIV-inhibiting benzeneacetamide derivatives

The present invention is concerned with antiretroviral (e.g. anti-HIV-1) compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifluoromethyl; R.sup.4 is trifluoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical --Alk--R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.

Heterocycle-substituted benzenemethanamine derivatives

The present invention is concerned with antiretroviral (e.g. anti-HIV-1)compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifiuoromethyl; R.sup.4 is trifiuoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical -Alk-R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.

A compound for use as a medicine having the formula ##STR1## a pharmaceutically acceptable acid addition salt form or a stereochemically isomeric form thereof, wherein R.sup.1 and R.sup.2 each independently are hydrogen, C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom bearing said R.sup.1 and R.sup.2 may form a pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl or 4-C.sub.1-4 alkylpiperazinyl group; X is O or S; R.sup.3 is hydrogen or C.sub.1-6 alkyl; R.sup.4, R.sup.5 and R.sup.6 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, trifluoromethyl, cyano, aminomethyl, carboxyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl-carbonyl, aminocarbonyl or hydroxy; R.sup.7 is hydrogen or halo; and R.sup.8, R.sup.9 and R.sup.10 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, nitro, hydroxy, trifluoromethoxy, 2,2,2-trifluoroethoxy, (trifluoromethyl)carbonyl, aminocarbonyl, (cyclopropyl)carbonyl or a radical C.sub.1-6 alkyl-(C.dbd.Y)--wherein .dbd.Y represents .dbd.O, .dbd.N--OH, .dbd.N--OCH.sub.3, .dbd.N--NH.sub.2 or .dbd.N--N(CH.sub.3).sub.2 ; provided that

The present invention is concerned with antiretroviral (e.g. anti-HIV-1) compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifluoromethyl; R.sup.4 is trifluoromethyl or methylcarbonyl; or a radical --C(.dbd.X)--NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical -Alk-R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy;

Growing community of inventors

Edegem, Belgium

Jean-Paul R Bosmans