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US5604241A Substituted benzylaminoquinuclidines as substance P antagonists 失效
取代的苄基氨基奎宁啶作为物质P拮抗剂

Substituted benzylaminoquinuclidines as substance P antagonists
摘要:
Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I ##STR1## and the pharmaceutically-acceptable salts thereof, wherein Ar.sup.1 and Ar.sup.2 are each independently aryl or substituted aryl; R.sup.1 is alkyl having from 1 to 6 carbon atoms;R.sup.2 is hydrogen or alkyl having from 1 to 6 carbon atoms;and either X and Y are taken separately and they are each, independently, hydrogen, dialkylphosphoryl having 2 to carbon atoms, alkyl having from 1 to 6 carbon atoms, alkenyl having from 2 to 6 carbon atoms or alkynyl having from 2 to 6 carbon atoms; or X and Y are taken together and they represent a hydrocarbon chain having 3, 4, or 5 carbon atoms, optionally containing up to 2 double bonds and optionally having 1 or 2 substituents selected from oxo, hydroxy and alkyl having from 1 to 6 carbon atoms; or Y is methoxy when X is ethyl; provided that when X and Y are taken together they are attached to adjacent carbon atoms; and provided that if either X or Y is hydrogen, then the other one must be alkenyl or alkynyl; and provided that when Y is methoxy and X is ethyl, then Y is at the 4-position and X is at the 5-position, Ar.sup.1 or Ar.sup.2 must each be phenyl, R.sup.1 is methyl and R.sup.2 is hydrogen.
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