192703-20-1Relevant articles and documents
Tritiation of the cannabinoid receptor antagonist SR144528 involving lithium aluminum tritide reduction; assessment of the kinetic isotope effect by 3H-NMR
Seltzman, Herbert H.,Foster, Matthew C.,Wyrick, Christopher D.,Burgess, Jason P.,Carroll, F. Ivy
, p. 589 - 596 (2005)
The cannabinoid receptor antagonist SR144528 was synthesized by an approach that enabled the incorporation of high specific activity tritium label while circumventing the lability of the target compound to catalytic hydrogenation. Lithium aluminum tritide
3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity
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, (2008/06/13)
The present invention relates to compounds of the formula STR1 in which: X 1 is a group --NR 1 R 2 or a group --OR 2 ;g 2, g 3, g 4, g 5, g 6 and w 2, w 3, w 4, w 5, w 6 are identical or different and are each independently hydrogen, a halogen atom, a (C 1 -C 4)alkyl, a (C 1 -C 4)alkoxy, a trifluoromethyl, a nitro or a (C 1 -C 4)alkylthio, with the proviso that at least one of the substituents g 2, g 3, g 4, g 5, g 6 and at least one of the substituents w 2, w 3, w 4, w 5, w 6 are other than hydrogen;R 1 is hydrogen or a (C 1 -C 4)alkyl;R 2 is a non-aromatic (C 3 -C 15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C 1 -C 4)alkyl and a (C 1 -C 4)alkoxy;R 3 is hydrogen or a group --CH 2 R 6 ; andR 4 and R 5 are each independently a hydrogen, a (C 1 -C 4)alkyl or a trifluoromethyl;or else R 4 is hydrogen and R 5 and w 6 together constitute an ethylene or trimethylene radical; andR 6 is hydrogen, a (C 1 -C 4)alkyl, a fluorine, a hydroxyl, a (C 1 -C 5)alkoxy, a (C 1 -C 5)alkylthio, a hydroxy(C 1 -C 5)alkoxy, a cyano, a (C 1 -C 5)alkylsulfinyl or a (C 1 -C 5)alkylsulfonyl with the proviso that when the substituents g 2, g 3, g 4, g 5 and/or g 6 are a (C 1 -C 4)alkyl R 6 is only hydrogen;to a process for their preparation and to the pharmaceutical compositions in which they are present.These compounds have a good affinity for the peripheral cannabinoid receptors.