21076-14-2Relevant academic research and scientific papers
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 (2004)
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.
New thiadiazoles and their use as phosphodiesterase-7 inhibitors
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Page 24, (2010/01/31)
The invention provides 1,3,4-thiadiazoles having the following formula (I): in which,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, the process for their preparation and their use for the manufacture of a medicament for the treatment of disorders for which a treatment by a PDE7 inhibitor is relevant.
