406502-37-2Relevant articles and documents
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: Design, synthesis and structure-activity relationship studies
Vergne, Fabrice,Bernardelli, Patrick,Lorthiois, Edwige,Pham, Nga,Proust, Emmanuelle,Oliveira, Chrystelle,Mafroud, Abdel-Kader,Royer, Frederique,Wrigglesworth, Roger,Schellhaas, Jennifer,Barvian, Mark,Moreau, Fran?ois,Idrissi, Moulay,Tertre, Anita,Bertin, Bernadette,Coupe, Magali,Berna, Patrick,Soulard, Patricia
, p. 4607 - 4613 (2007/10/03)
The synthesis and SAR studies of a series of structurally novel small molecule inhibitors of PDE7 are discussed. The best compounds from the series displayed low nanomolar inhibitory activity and are selective versus PDE4.
Thiadiazoles and oxadiazoles and their use as phosphodiesterase-7 inhibitors
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, (2008/06/13)
The invention provides 1,3,4-thiadiazoles and 1,3,4-oxadiazoles having the following Formula I: in which, Y is S or O, R1 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl or a polycyclic group, optionally substituted, R2 is alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl or aryl optionally substituted, R3 is X2—R′3, in which X2 is a binding group and R′3 is cycloalkyl, heterocycloalkyl, cycloalkenyl, aryl, heteroaryl, or a polycyclic group; optionally substituted, or their pharmaceutically acceptable derivatives, a compound of Formula I, for their preparation, and processes for pharmaceutical compositions containing methods of using the compounds for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.