Janssen Pharmaceutica Nv

Marcel A Janssen

Georges H Van Daele

Paul A Janssen

Jean-Paul R Bosmans

Marc G Verdonck

Michael Nicholas Greco

Alfons H Raeymaekers

Eddy J Freyne

Frans M Van Den Keybus

Karin J Nuyens

Victor Karel Sipido

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.

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;

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(=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.

Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1;

Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole

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

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

Pyridine-substituted benzenemethanamine derivatives

.alpha.-substituted benzenemethanamine derivatives and pharmaceutical use

(6,7-dihydro-5H-pyrrolo[1,2-c]imidazolyl-5-yl)- and (5,6,7,8-tetrahydroimidazo[1,5-a]pyridinyl-5-yl) substituted 1H-benzotriazole derivatives, compositions containing the same and methods of treating estrogen dependent disorders.

Pharmacologically active (6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-

Novel antimicrobial compositions comprising a 1-(aryloxyphenyl)piperazine as an active ingredient and a method of combatting the growth of microorganisms by the use of such 1-(aryloxyphenyl)piperazines.

Antimicrobial compositions containing 1-(aryloxyphenyl)piperazines

Compounds of the class of salicylanilides substituted in the 4-position of the anilino moiety with a --CH(CN)-Ar group wherein Ar is phenyl, substituted phenyl, thienyl, halothienyl or naphthalenyl, said salicylanilides being useful as parasiticides.

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Vosselaar, Belgium

Marcel A Janssen