Azocine analgesics and method for their preparation

C - Chemistry – Metallurgy – 07 – D

Patent

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260/237.8

C07D 221/22 (2006.01) C07D 491/08 (2006.01)

Patent

CA 1126727

ABSTRACT OF THE DISCLOSURE Novel azocine derivatives and a method for their preparation are disclosed. The compounds display analgesic effects in mammals. The compounds have the formula Image wherein R is hydrogen, straight or branched chain alkyl of from 1 to 8 carbon atoms, straight or branched chain alkenyl of from 2 to 6 carbon atoms, straight or branched chain alkynyl of from 2 to 6 carbon atoms, cycloalkyl containing 3 to 7 carbon atoms, cycloalkyl- alkyl containing 4 to 8 carbon atoms, 2- or 3-furyl- methyl optionally substituted by 1 to 3 methyl groups, 2- or 3-tetrahydrofurylmethyl optionally substituted by 1 to 3 methyl groups or Image wherein n is an integer of 1 to 3, Ra is hydrogen, monohalo, or dihalo, and Rb is hydrogen, hydroxy, methyl trifluoromethyl, mono-, di- or trialkoxy of 1 to 3 carbon atoms, alkanoyloxy of from 1 to 6 carbon atoms or Ra and Rb together form a methylenedioxy group; R1 is hydroxy or alkoxy of from 1 to 6 carbon atoms; R2 is hydrogen or alkoxy of from 1 to 6 carbon atoms; R1 and R2 when taken together may form a methylenedioxy group; R3 is alkoxy of from 1 to 6 carbon atoms or benzyloxy; and the pharmacologically acceptable salts thereof.

339827

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