- New Antihistaminic Theophylline or Theobromine Derivatives
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A series of 3,4-dihydro-1,3-dimethyl-7--1H-purine-2,6-diones and 3,7-dihydro-3,7-dimethyl-1--1H-purine-2,6-diones was synthesized and evaluated for antihistaminic activity.Some of them displayed good inhibition of both histamine-induced bronchospasm in the anesthetized guinea pig at 10 μ/kg by the intravenous route and of passive cutaneous anaphylaxis in the rat at 10 mg/kg by the oral route.Comparison of the two most active compounds revealed a higher antihistaminic activity with the compounds containing a (phenylthio)propyl group (1 and 2) as compared with that containing a phenoxy group.Compound 2 piperazin-1-yl>-2-hydroxypropyl>-1H-purine-2,6-dione> was selected for clinical trials on the basis of a comparative pharmacological study with chloropheniramine, ketotifen, promethazine, and theophylline.
- Pascal, Jean-Claude,Beranger, Serge,Pinhas, Henri,Poizot, Alain,Desiles, Jean-Pierre
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p. 647 - 652
(2007/10/02)
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- Piperazine derivatives of theobromine
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New compounds of the formula STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein Z1 and Z2 are each independently selected from the group consisting of CH2, CHOB and C=O, wherein B is selected from the group consisting of hydrogen and alkanoyl; Y is oxygen or sulfur; 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; and R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy; are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold.
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- Piperazine derivatives of theophylline
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New compounds of the formula STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein Z1 and Z2 are each independently selected from the group consisting of CH2, CHOB and C=O, wherein B is selected from the group consisting of hydrogen and alkanoyl; Y is oxygen or sulfur; 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; and R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy; are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold.
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- Piperazine derivatives of theophylline
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New compounds of the formula STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein M is selected from the group consisting of hydrogen, morpholino, benzylamino, di-n-lower alkylamine, n-lower alkylamine, and aryl piperazino; Z1 and Z2 are each independently selected from the group consisting of CH2, CHOB and C=O, wherein B is selected from the group consisting of hydrogen and alkanoyl; Y is oxygen or sulfur; 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, or when m is hydrogen; R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy; and R4 and R5 are each independently lower alkyl, with the proviso that both R4 and R5 cannot be methyl when M is hydrogen; 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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- Piperazine alkanols
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This invention relates to variously substituted piperazine derivatives. S compounds possess therapeutically useful vasodilator properties.
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