.kappa.-opioid receptor agonist comprising...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 277/66 (2006.01) A61K 31/428 (2006.01) A61P 19/02 (2006.01) A61P 19/06 (2006.01) A61P 25/04 (2006.01) A61P 29/00 (2006.01) A61P 43/00 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2480560

The present invention provides r, opioid receptor agonists comprising 2-phenylbenzothiazoline derivatives. The present invention relates to .kappa. opioid receptor agonists comprising compounds or salts thereof having the chemical structure represented by the general formula [I]. Namely, it is important for exhibition of the .kappa. opioid receptor agonist actions to have an alkyl group having an amino group at a phenyl group of 2-phenylbenzothiazoline as a substituent and to have an acyl group at a nitrogen atom of 2-phenylbenzothiazoline, (see formula I) wherein R is alkyl having the amino group as the substituent; and R1 is acyl.

L'invention porte sur un agoniste du récepteur k-opioïde comprenant un dérivé de 2-phénylbenzothiazoline qui est soit un composé à squelette basique dont la structure chimique est représentée par la formule (I), soit un sel de ce composé. La présence d'un groupe alkyle à substitution amino lié au groupe phényle de 2-phénylbenzothiazoline et la présence d'un groupe acyle lié à l'atome d'azote de 2-phénylbenzothiazoline sont importantes afin de conférer une activité à l'agoniste du récepteur de k-opioïde. (Dans la formule (I), R représente alkyle à substitution amino et R?1¿ représente acyle).

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