Substituted 1-indolylpropyl-4-benzylpiperazine derivatives

Details Substituted 1-indolylpropyl-4-benzylpiperazine derivatives Substituted 1-indolylpropyl-4-benzylpiperazine derivatives

1998-04-28

1999-07-20

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544366, 544367, 544369, 544370, A61K 31495, C07D40314

Patent

active

059256389

ABSTRACT:
formula I, substituted at the 5-position of the indole nucleus by a 1,2,4-triazol-4-yl moiety, and on the methylene linkage of the benzyl moiety by a range of substituted alkyl groups, are selective agonists of 5-HT.sub.1 -like receptors, being potent agonists of the human 5-HT.sub.1D.alpha. receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT.sub.1D.alpha. receptor subtype relative to the 5-HT.sub.1D.beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT.sub.1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT.sub.1D receptor agonists. ##STR1##

REFERENCES:
patent: 5614524 (1997-03-01), Matassa et al.
patent: 5807857 (1998-09-01), Pineiro et al.
patent: 5808064 (1998-09-01), Chen et al.

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