Piperazine derivatives of theophylline and theobromine

C - Chemistry – Metallurgy – 07 – D

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C07D 473/04 (2006.01) A61K 31/52 (2006.01) C07D 473/06 (2006.01) C07D 473/08 (2006.01) C07D 473/10 (2006.01)

Patent

CA 1274517

25280-FF ABSTRACT OF THE DISCLOSURE New compounds of formulas I and II Image (I) Image (II) and the pharmaceutically acceptable acid addition salts thereof, wherein M is selected from the group consisting of hydrogen, morpholino, benzylamino, di-n-lower alkylamino, n-lower alkylamino and Image wherein Ar is optionally substituted phenyl; Zl1 and Z2 are each independently selected from the group consisting of CH2, CHOB and C=0, wherein B is selected from the group consisting of hydrogen and alkanoyl; Y is oxygen or nothing; n is an integer from 0-4 but cannot be zero when Z1 is CHOB; m is an integer from 0-4 but cannot be zero when Z2 is CHOB; R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy; R4 is lower alkyl; and R5 is hydrogen or lower alkyl, are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold. They are also vasodilators.

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