C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/273, 260/265
C07D 471/04 (2006.01) C07D 453/02 (2006.01) C07D 519/00 (2006.01)
Patent
CA 1321586
ABSTRACT Processes for preparing bicyclic compounds useful as anti-allergic, anti-inflammatory and/or cytoprotective agents are described, together with a process for preparing intermediates therefor. These bicyclic compounds have the general formula: Image (X) wherein W and X are the same or different and each represents -CH= or -N=; R2, R3, R4 and R5 are the same or different and each represents H, alkyl, alkenyl, alkynyl, alkoxyalkyl, hydroxyalkyl, cycloalkyl, acyl- oxyalkyl or -R7-CO2R0 wherein R7 is alkylene and R0 is hydrogen or alkyl, with the provisos that the OH of the hydroxyalkyl group and the acyloxy of the acyloxyalkyl group are not joined to the same carbon atom as another heteroatom and that, when R1, R2 and/or R3 are alkenyl or alkynyl, there is at least one carbon-carbon single bond between the nitrogen atom and the carbon-carbon double or triple bond; or - 2 - one of R2 and R3 is an aryl group or an aromatic heterocyclic group; or R2 and R3, together with the adjacent nitrogen atom, are joined together to rep- resent a ring containing from 2 to 8 carbon atoms; or both of R2 and R3 are joined together to represent a polycyclic hydrocarbon ring; m is an integer of from 0 to 3; n is an integer of from 0 to 2; Q represents an aryl or an aromatic heterocyclic group, each Y substituent is independently selected from hydroxy, alkyl, halogen, NO2 alkoxy, trifluoromethyl, cyano, cycloalkyl, alkenyloxy, alkynyloxy, hydroxyalkyl, -S(O)n-R18 (wherein R18 is alkyl and n is as defined above), -SO2NH2, -CO-R (wherein R represents OH, -NH-R18 or -O-R18 (where R18 is as defined above), -O-B-(O)p-COR19 (wherein B is alkylene, p is 0 or 1, and R19 is as defined above), -NH2, -NHCHO, -NH-CO-R19 (wherein R19 is as defined above, with the proviso that it is not hydroxy), -NH-COCF3, -NH-SO2R18 (wherein R18 is as defined above), and -NHSO2CF3.
581753
Gala Dinesh
Ganguly Ashit K.
Steinman Martin
Gala Dinesh
Ganguly Ashit K.
Schering Corporation
Steinman Martin
Swabey Ogilvy Renault
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