Pyrrolidylidene, piperidylidene and hexahydroazepinylidene ureas as CNS
申请人:McNeil Laboratories, Incorporated
公开号:US03998958A1
公开(公告)日:1976-12-21
Compounds of the class of 1-aryl-3-pyrrolidylidene ureas, 1-aryl-3-piperidylidene ureas and 1-aryl-3-hexahydroazepinylidene ureas, useful as central nervous system (CNS) depressants.
The present invention relates to compounds of formula (I)
1
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
and R
7
are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.
Anilide derivatives of the natural trioxane artemisinin were prepared and evaluated for antimalarial efficacy in
Plasmodium berghei
-infected mice. Selected anilides derivatives administered orally as one single-digit dose combined with mefloquine hydrochloride were completely curative, i.e., all 5 of the mice in the particular treatment group had no detectable parasitemia on day 30 post infection, gained as much weight by day 30 post infection as the control mice (no infection), and behaved normally.