5-ht2 receptor ligands

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 403/04 (2006.01) A61K 31/55 (2006.01) C07D 243/38 (2006.01) C07D 267/20 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07D 498/04 (2006.01) C07D 498/14 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2207613

Described herein are 5-HT2 receptor-selective compounds of formula (I), wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings; X1 is selected from O, S, SO, SO2, C=O, CH2, CH-OH, CH-N(C1-4alkyl)2, C=CHCl, C=CHCN, NH, N- C1-4alkyl and N-acetyl; X2--- is selected from N =, CH2-, CH = and C(O)-; R1 is C1-6alkyl optionally substituted with a substituent selected from OH, halo, C1-4alkyl and C1-4alkoxy; and R2, R3 and R4 are independently selected from H and R1; and acid addition salts, solvates and hydrates thereof. Their use as ligands for serotonin 5-HT2 receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the 5-HT2 receptor is implicated, such as hypertension, thrombosis, migraine, vasospasm, ischemia, depression, anxiety, schizophrenia, sleep disorders and appetite disorders is also described.

L'invention se rapporte à des composés sélectifs par rapport au récepteur 5-HT2, de la formule générale (I), dans laquelle A et B, qui sont indépendamment choisis, représentent des noyaux homo- ou hétérocycliques saturés ou insaturés à 5 ou 6 chaînons, éventuellement substitués; X¿1? est choisi parmi O, S, SO¿2?, SO, C=O, CH¿2?, CH-OH, CH-N(alkyle C¿1-4?)¿2?, C=CHCl, C=CHCN, NH, N-alkyle C¿1-4?, et N-acétyle; X¿2?--- est choisi parmi N =, CH¿2?-, CH = et C(O)-; R¿1? représente alkyle C¿1-6? éventuellement substitué par un substituant choisi parmi OH, halo, alkyle C¿1-4? et alcoxy C¿1-4?; et R¿2?, R¿3? et R¿4? sont indépendamment choisis entre H et R¿1?; et à leurs sels d'addition d'acide, solvates et hydrates. L'invention se rapporte également à l'utilisation de ces composés comme ligands pour l'identification du récepteur 5-HT2 de la sérotonine et dans le cadre d'un programme de criblage de médicaments, ainsi que comme agents pharmaceutiques permettant de traiter des états dans lesquels le récepteur 5-HT2 est impliqué, tels que l'hypertension, les thromboses, la migraine, les vasospasmes, l'ischémie, la dépression, l'anxiété, la schizophrénie, les troubles du sommeil et les troubles de l'appétit.

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