163705-72-4Relevant academic research and scientific papers
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-asthmatics
Kim, Euikyung,Chun, Hyung-Ok,Jung, Sung-Hak,Kim, Jong Hoon,Lee, Jae-Mok,Suh, Byung-Chul,Xiang, Myung Xik,Rhee, Chung K.
, p. 2355 - 2358 (2007/10/03)
A new series of catechol hydrazines was synthesized and their structure-activity relationship (SAR) was analyzed for developing an effective phosphodiesterase 4 (PDE4) inhibitor as an anti-asthmatic drug candidate. Among the (E)-Analogues tested using in
CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4 inhibitors
Alexander,Warrellow,Eaton,Boyd,Head,Porter,Brown,Reuberson,Hutchinson,Turner,Boyce,Barnes,Mason,Cannell,Taylor,Zomaya,Millican,Leonard,Morphy,Wales,Perry,Allen,Gozzard,Hughes,Higgs
, p. 1451 - 1456 (2007/10/03)
The discovery, synthesis and biological activity of a series of triarylethane phosphodiesterase 4 inhibitors is described. Structure-activity relationship studies are presented for CDP840 (29), a potent, chiral, selective inhibitor of PDE 4 (IC50/su
Phenylpyridyl compounds for inhibiting phosphodiesterase IV and methods of using same
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, (2008/06/13)
PCT No. PCT/US96/00519 Sec. 371 Date Nov. 13, 1997 Sec. 102(e) Date Nov. 13, 1997 PCT Filed Jan. 11, 1996 PCT Pub. No. WO96/21435 PCT Pub. Date Jul. 18, 1996Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improve
1,3-DIHYDRO-1-(PHENYLALKENYL)-2H-IMIDAZOL-2-ONE DERIVATIVES HAVING PDE IV AND CYTOKINE INHIBITING ACTIVITY
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, (2008/06/13)
The present invention concerns the compounds of formula STR1 the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof, wherein R. sup.1 and R. sup. 2 each independently are hydrogen; C
Asymmetric synthesis of CDP840 by Jacobsen epoxidation. An unusual syn selective reduction of an epoxide
Lynch,Choi,Churchill,Volante,Reamer,Ball
, p. 9223 - 9228 (2007/10/03)
An asymmetric synthesis of the PDE IV inhibitor, CDP840 (3) is reported. The absolute stereochemistry was controlled by a Jacobsen epoxidation of the Z triaryl olefin 8 (89% ee) or the E triaryl olefin 9 (48% ee). The disparate results in stereocontrol were interpreted in terms of the 'skewed side-on approach model' proposed by Jacobsen. LiBH4 · BH3 reduction of the epoxides was found to proceed with retention of configuration.
Pheynl or benzyl-substituted rolipram-based compounds for and method of inhibiting phosphodiesterase IV
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, (2008/06/13)
Rolipram-based PDE IV inhibitors containing phenyl- or benzyl-substituted moieties of the formula: STR1 wherein X1 and X2 may be the same or different and each is O or S; R1 is selected from the group consisting of hydroge
