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filingDate 1987-11-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_886d8135578ade84f1ab6905600f9aeb
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publicationDate 1988-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0266989-A2
titleOfInvention Dihydropyridine anti-allergic and anti-inflammatory agents
abstract Compound of the formula:-n wherein R is phenyl or phenyl substituted by one or more substituents selected from nitro, halo, C₁-C₄ alkyl, C₁-C₄ alkoxy, aryl(C₁-C₄ alkoxy), C₁-C₄ alkylthio, C₁-C₄ alkylsulphonyl, hydroxy, trifluormethyl and cyano; R¹ and R² are each independently H or C₁-C₆ alkyl, or the two groups may be joined together to form with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino, morpholino, piperazinyl, N-(C₁-C₄ alkyl)piperazinyl or N-(C₂-C₄ alkanoyl)piperazinyl group; or R² is H or C₁-C₄ alkyl and R¹ is CN, C₃-C₇ cycloalkyl, aryl, heteroaryl, or a C₁-C₄ alkyl group substituted by one or more substituents selected from C₃-C₇ cycloalkyl, C₁-C₄ alkoxycarbonyl, aryl and heteroaryl; R³ is OH, C₁-C₆ alkyloxy, aryl(C₁-C₄ alkoxy), or NR⁴R⁵ wherein each of R⁴ and R⁵ is independently H or C₁-C₆ alkyl, or the two groups may be joined together to form with the nitrogen atom to which they are attached a pyrrolidinyl, piperidino, morpholino, piperazinyl, or N-(C₁-C₄ alkyl)-­piperazinyl group; Y is an alkylene group of from 2 to 8 carbon atoms which may be straight or branched-chain having at least 2 carbon atoms in the chain linking X to the oxygen atom; X is benzimidazol-1-yl or benzimidazol-2-yl, optionally substituted with one or more substituents selected from C₁-C₄ alkyl, C₁-C₄ alkoxy, halo, CF₃ and CN; and their pharmaceutically acceptable salts are antagonists of PAF and are useful in the treatment of allergic, inflammatory and hypersecretory conditions.
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