Abstract: The compounds are of the class of tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones possessing antiretroviral, especially anti-HIV-1, activity. An illustrative compound is (+)-S-4,5,6,7-tetrahydro-9-chloro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4 ,5,1-jk][1,4]benzodiazepine-2(1H)-thione. These compounds are represented by the formula: ##STR1## The application also discloses compositions containing these compounds as active ingredients and methods of treating subjects suffering from retroviral infections by administering said compounds.
Type:
Grant
Filed:
October 5, 1993
Date of Patent:
December 6, 1994
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Michael J. Kukla, Henry J. Breslin, Alfons H. M. Raeymaekers, Josephus L. H. Van Gelder, Paul A. J. Janssen
Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.
Type:
Grant
Filed:
December 1, 1992
Date of Patent:
March 22, 1994
Assignee:
Adir et Compagnie
Inventors:
Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
Abstract: Novel bicyclic tetrahydroxylated pyrrolizidines are disclosed which are inhibitors of glycosidase enzymes. A preferred inhibitor is 1.alpha.,2.alpha.,6.alpha.,7.alpha.,7.alpha..beta.-1,2,6-7-tetrahydroxypyr rolizidine. It is synthesized from D-glycero-D-gulo-heptono-1,4-lactone.