Phenyl pyrazolidinones as bronchodilators and...

C - Chemistry – Metallurgy – 07 – D

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C07D 231/08 (2006.01) C07D 231/20 (2006.01) C07D 231/22 (2006.01) C07D 231/26 (2006.01) C07D 401/02 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2067298

PHENYL PYRAZOLIDINONES AS BRONCHODILATORS AND ANTI-INFLAMMATORY AGENTS Abstract of the Disclosure There are disclosed compounds of the formula Image wherein R1 is hydrogen or lower alkyl; R2 is C3-7 alkyl or C3-7 cycloalkyl; R3 is hydrogen, lower alkyl, carboxyloweralkyl, lower alkoxycarbonyl, lower alkoxycarbonyl loweralkyl, aryl, aralkyl or CONH2; R4 is hydrogen, C1-8 alkyl, Image or Image ; B is a bond, NH or O; Y is O or S; A is a bond or -C=C-; n is 0 - 5 ; R5 is hydrogen when B is NH, or R5 is lower alkyl, C3-8 cycloalkyl; aryl, substituted aryl, aralkyl, substituted aralkyl, aralkenyl, aralkenylalkyl or Image ; and when B is NH, R5 may also represent hydrogen; R6 is hydrogen or halo; the dotted line represents an optional double bond; and the pharmacologically acceptable salts thereof, which by virtue of their ability to selectively inhibit PDE IV, are bronchodilatory and anti-inflammatory and so are useful in the treatment of acute and chronic bronchial asthma and associated pathologies.

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