Compounds of the following formula: ##STR00001## wherein X is H or substituted with ##STR00002## with at least one X being substituted; and halo is fluorine, chlorine, bromine, iodine; and stereoisomers and conjugable analogs thereof.

Bornhop; Darryl J.

Bai; Mingfeng

Stella; Nephi

Stern; Eric

Vanderbilt University

University of Washington

Cannabinoid receptor targeted agent

The present invention relates to compounds of the formula ##STR1## in which: X.sub.1 is a group --NR.sub.1 R.sub.2 or a group --OR.sub.2 ;g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are identical or different and are each independently hydrogen, a halogen atom, a (C.sub.1 -C.sub.4)alkyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a nitro or a (C.sub.1 -C.sub.4)alkylthio, with the proviso that at least one of the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and at least one of the substituents w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are other than hydrogen;R.sub.1 is hydrogen or a (C.sub.1 -C.sub.4)alkyl;R.sub.2 is a non-aromatic (C.sub.3 -C.sub.15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C.sub.1 -C.sub.4)alkyl and a (C.sub.1 -C.sub.4)alkoxy;R.sub.3 is hydrogen or a group --CH.sub.2 R.sub.6 ; andR.sub.4 and R.sub.5 are each independently a hydrogen, a (C.sub.1 -C.sub.4)alkyl or a trifluoromethyl;or else R.sub.4 is hydrogen and R.sub.5 and w.sub.6 together constitute an ethylene or trimethylene radical; andR.sub.6 is hydrogen, a (C.sub.1 -C.sub.4)alkyl, a fluorine, a hydroxyl, a (C.sub.1 -C.sub.5)alkoxy, a (C.sub.1 -C.sub.5)alkylthio, a hydroxy(C.sub.1 -C.sub.5)alkoxy, a cyano, a (C.sub.1 -C.sub.5)alkylsulfinyl or a (C.sub.1 -C.sub.5)alkylsulfonyl with the proviso that when the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5 and/or g.sub.6 are a (C.sub.1 -C.sub.4)alkyl R.sub.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.

fluorine/marihuana

Cannabinoid receptor targeted agent

3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity

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