Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18F]-fluorobenzyl)piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors
In this study, novel specific PET radioligands containing the 4-(4-fluorobenzyl)piperidine moiety and selectively antagonistic for the NR2B subunit containing NMDA receptors were developed. Two antagonists, RGH-896 (1a) and 4-(4-fluorobenzyl)piperidinyl-1
NOVEL CRYSTALLINE FORM OF 2-[4-(4-FLUORO-BENZYL)-PIPERIDINE-1-YL]-2-OXO-N-(2-OXO-2,3-DIHYDRO-BENZOXAZOL-6-YL)-ACETAMIDE
The present invention relates to a novel crystalline form of 2-[4-(4-fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazol-6-yl)-acetamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.
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(2010/02/17)
NOVEL CRYSTALLINE HYDRATE, AMORPHOUS AND POLYMORPHIC FORMS OF DIHYDRO-BENZOXAZOLE-6-YL-ACETAMIDE DERIVATIVE AND PROCESSES FOR THEM PREPARATION
The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro- benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.
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(2010/09/18)
Oxamides as novel NR2B selective NMDA receptor antagonists
A novel series of oxamides derived from indole-2-carboxamides was identified as potent NR2B selective NMDA receptor antagonists. Several members of this group showed good analgesic activity in the mouse formalin test.