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US 6,051,580 AGranted
Substituted heterocycles
AssigneeZeneca Limited
InventorsScott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
Life of this patent
Estimating the term…
Abstract
Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.
Claims8
A compound of formula I:
- wherein
- X.sup.j is hydrogen or (C.sub.1 -C.sub.6)alkyl;
- B.sup.j is --N(R.sup.jh)-- and L.sup.j is a hydrocarbon chain selected from trimethylene, 2,2-dimethylprop-1,3-yl or B.sup.j is --N.dbd. and L.sup.j is a hydrocarbon chain in which the 1-position is bound to B.sup.j and L.sup.j is cis,cis-prop-2-en-1-ylidin-3-yl;
- J.sup.j is independently oxygen or sulfur;
- R.sup.jh is independently hydrogen or (C.sub.1 -C.sub.6)alkyl;
- Q.sup.2 is a nitrogen-linked five-membered aromatic ring containing 1-4 nitrogens, which is substituted at a ring position adjacent to the nitrogen-link by a group Q.sup.5 ;
- Q.sup.3 is hydrogen or (C.sub.1 -C.sub.3)alkyl;
- Q.sup.4 is phenyl which may bear one or two substituents independently selected from halo, trifluoromethyl, hydroxy, (C.sub.1 -C.sub.3)alkoxy, (C.sub.1 -C.sub.3)alkyl and methylenedioxy;
- or Q.sup.4 is thienyl, imidazolyl, benzothiophenyl or naphthyl any of which may bear a halo substituent;
- or Q.sup.4 is biphenylyl;
- or Q.sup.4 is carbon-linked indolyl which may bear a benzyl substituent at the 1-position;
- and
- Q.sup.5 is selected from the group consisting of phenyl, benzyl, phenethyl and naphthyl, wherein any phenyl ring or naphthyl may bear one or more substituents selected from (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, methylenedioxy, halogeno, hydroxy, (C.sub.1 -C.sub.4)acyloxy and NR.sup.A R.sup.B in which R.sup.A and R.sup.B are independently hydrogen or (C.sub.1 -C.sub.3)alkyl, or R.sup.A is hydrogen or (C.sub.1 -C.sub.3)alkyl and R.sup.B is (C.sub.1 -C.sub.4)acyl;
- or the N-oxide of the piperidino nitrogen indicated by .DELTA.;
- or a pharmaceutically acceptable salt thereof;
- or a quaternary ammonium salt thereof in which the piperidino nitrogen indicated by .DELTA. is a quadricovalent ammonium nitrogen wherein the fourth radical on the nitrogen R.sup.1 is (C.sub.1 -C.sub.4)alkyl or benzyl and the associated counterion A is a pharmaceutically acceptable anion.
13 more elements
Dependencies are inferred from the claim text.