152630-47-2Relevant articles and documents
CONDENSED HETEROCYCLIC COMPOUNDS AS PDE-IV INHIBITORS FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS
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Page 44, (2010/11/30)
The present invention relates to novel heterocyclic compounds that inhibit phosphodiesterase type 4 (PDE4). The compounds are useful for treating inflammatory conditions, diseases of the central nervous system and insulin resistant diabetes , (formula I)
Compounds and method for preparing substituted 4-phenyl-4-cyanocyclohexanoic acids
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Example 6, (2008/06/13)
This invention relates to a method of preparing a compound of the following type by treating a compound of formula (II) with lithium bromide, magnesium bromide and the like.
1,4-Cyclohexanecarboxylates: Potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma
Christensen, Siegfried B.,Guider, Aimee,Forster, Cornelia J.,Gleason, John G.,Bender, Paul E.,Karpinski, Joseph M.,Dewolf Jr., Walter E.,Barnette, Mary S.,Underwood, David C.,Griswold, Don E.,Cieslinski, Lenora B.,Burman, Miriam,Bochnowicz, Steven,Osborn, Ruth R.,Manning, Carol D.,Grous, Marilyn,Hillegas, Leonard M.,Bartus, Joan O'Leary,Dominic Ryan,Eggleston, Drake S.,Curtis Haltiwanger,Torphy, Theodore J.
, p. 821 - 835 (2007/10/03)
Evaluation of a variety of PDE4 inhibitors in a series of cellular and in vivo assays suggested a strategy to improve the therapeutic index of PDE4 inhibitors by increasing their selectivity for the ability to inhibit PDE4 catalytic activity versus the ability to compete for high affinity [3H]rolipram-binding sites in the central nervous system. Use of this strategy led ultimately to the identification of cis-4-cyano-4-[3- (cyclopentyloxy)-4-methoxyphenyl]cyclohexane-1-carboxylic acid (1, SB 207499, Ariflo(TM)), a potent second-generation inhibitor of PDE4 with a decreased potential for side effects versus the archetypic first generation inhibitor, (R)-rolipram.