Syntex (u.s.a.) Inc.

David E Clarke

Robin D Clark

Jurg R Pfister

Alam Jahangir

Lawrence Emerson Fisher

David John Morgans, Jr

David Bruce Repke

Todd Richard Elworthy

Helen Y Wu

Eric Brian Sjorgren

The present invention relates to novel .alpha..sub.1 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1;

�3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine,

The present invention relates to novel N-aryloxyalkyl tryptamine .alpha..sub.1 -adrenergic receptor antagonists of the formula I: ##STR1## in which n is 2, 3 or 4; q is 1, 2 or 3; t is 0, 1, 2 or 3; z is 0, 1, 2 or 3; each R.sup.1 and R.sup.2 are independently hydroxy, halogen, cyano, (C.sub.1-8)alkyl, (C.sub.1-8)alkyloxy or trifluoromethyl; and R.sup.2 is hydrogen, (C.sub.1-4)alkyl, fluoro(C.sub.1-4)alkyl, difluoro(C.sub.1-4)alkyl, trifluoro(C.sub.1-4)alkyl, (C.sub.1-4)alkyloxy(C.sub.1-4)alkyl, oxo(C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl or allyl or phenyl(C.sub.1-4)alkyl or heterocyclo(C.sub.1-8)alkyl (optionally substituted with one to two substituents independently selected from (C.sub.1-4)alkyl, (C.sub.1-4)alkyloxy, trifluoromethyl and halogen); R.sup.3 and R.sup.4 are independently hydrogen, (C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl or allyl; and R.sup.5 is hydrogen, (C.sub.1-4)alkyl, (C.sub.1-8)cycloalkyl, (C.sub.1-8)cycloalkylmethyl, allyl, (C.sub.1-4)alkylsulfonyl and aminocarbonyl; with the proviso that when n is 2, t is 0, q is 1, z is 0, 1 or 2, R.sup.5 is hydrogen and R.sup.6 is hydroxy or (C.sub.1-8)alkyloxy then at least one of R.sup.3 and R.sup.4 is not hydrogen; and the pharmaceutically acceptable salts, individual isomers, and mixtures of isomers thereof; their uses as therapeutic agents and the methods of their making.

N-aryloxyalkyl tryptamine .alpha..sub.1 -adrenergic receptor antagonists

Compounds of the Formula (I), (II), or (III): ##STR1## wherein the variables are as defined in the specification and the pharmaceutically acceptable salts thereof, exhibit useful pharmacological properties, and are particularly useful as angiotensin II antagonists.

Substituted indole derivatives

Compound of the Formula (I), (II), or (III): ##STR1## wherein: R.sup.1 is lower alkyl or 2'-(1H-tetrazol-5-yl)biphenyl-4'-ylmethyl;

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Mountain View, CA, United States of America

David E Clarke