1<i>H</i>-Cyclopentapyrimidine-2,4(1<i>H</i>,3<i>H</i>)-dione-Related Ionotropic Glutamate Receptors Ligands. Structure−Activity Relationships and Identification of Potent and Selective iGluR5 Modulators
作者:Stefania Butini、Darryl S. Pickering、Elena Morelli、Salvatore Sanna Coccone、Francesco Trotta、Meri De Angelis、Egeria Guarino、Isabella Fiorini、Giuseppe Campiani、Ettore Novellino、Arne Schousboe、Jeppe K. Christensen、Sandra Gemma
DOI:10.1021/jm800865a
日期:2008.10.23
AMPA receptor partial agonist. Modifying the cyclopentane ring of (S)-1, we developed two of the most potent and selective functional antagonists (5 and 7) for kainate receptor (KA-R) subunit iGluR5. Derivatives 5 and 7, with their unique pharmacological profile, may lead to a better understanding of the different roles and modes of action of iGluR1-5 subunits, paving the way for the synthesis of new
The invention provides compounds of formula I:
or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I, and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula I.
Furo (3,4-d) pyrimidine-2, 4-dione derivatives and intermediates thereof
申请人:ORTHO PHARMACEUTICAL CORPORATION
公开号:EP0244175A2
公开(公告)日:1987-11-04
The synthesis of furo[3,4-d]pyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and furo[3,4-d]pyrimidine-2,4-dione derivatives are general vasodilating agents and antihypertensive agents. The compounds are useful as cardiovascular agents.