C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/242.01
C07D 471/04 (2006.01)
Patent
CA 1154766
ABSTRACT OF THE DISCLOSURE The invention is nitrogen bridgehead condensed pyrimidine deriva- tives of the general formula Image I pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometric isomers and tautomers thereof - where the upper dotted line stands fro an optionally present carbon-carbon bond, R stands for hydro- gen or C1-4 alkyl, R1 stands for hydrogen or C1-4 alkyl, styryl or carboxy or a derivative thereof or R and R1 together form -(CH=CH)2, when the dotted lines form a further C-C bond and in every other case a single bond is present in the 6, 7-position, R2 stands for hydrogen, C1-4 alkyl or hydroxy, R3 stands for hydrogen, C1- alkyl, aryl, C1-4 alkanoyl, carboxy or derivative thereof or -(CH2)m-COOH or a derivative thereof on the carboxy group and m = 1,2,3, R4 is hydrogen, C? alkyl optionally substituted by hydroxy or carboxy, tri- fluoromethyl, optionally substituted C6-10 aryl, phenyl-C1-3-alkyl or option- ally substituted heterocycle, R5 is hydrogen, C1-4 alkyl, C6-10 aryl, phenyl- C1-3-alkyl, alkanoyl containing C1-4 alkyl or optionally substituted benzoyl or heteroaroyl or R2 and R5 together with the nitrogen which they are at- tached to form a piperidino, pyrrolidino or morpholino ring or R4 and R5 to- gether with the adjacent nitrogen to which they are attached form a group of the general formula -N=C(R6R7) - wherein R6 is hydrogen and R7 stands for optionally substituted phenyl and n = 1. The compounds display antiallergic and anntiasthmatic properties.
318812
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