Alkyl-substituted compounds having dopamine receptor affinity

Details Alkyl-substituted compounds having dopamine receptor affinity Alkyl-substituted compounds having dopamine receptor affinity

C - Chemistry, Metallurgy

07

D

C07D 267/20 (2006.01) A61K 31/55 (2006.01) C07D 243/38 (2006.01) C07D 281/16 (2006.01) C07D 295/02 (2006.01) C07D 295/073 (2006.01) C07D 313/14 (2006.01) C07D 337/14 (2006.01) C07D 401/04 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2207771

Described herein are D4 receptor-selective compounds of general formula (I): wherein: A and B are independently selected, optionally substitued, unsaturated 5- or 6- membered, homo- or heterocyclic rings; X1, is selected from CH2, O, NH, S, C=O, CH-OH, CH-N(C1-4alkyl)2, C=CHCl, C=CHCN, N-C1-4alkyl, N-acetyl, SO2 and SO; X2--- is selected from N=, CH2-, CH= and C(O); Y is selected from N and CH; R1 represents C1-4alkyl; n is 0, 1 or 2; q is 1 or 2; and Z is C5-10alkyl optionally substituted with OH, halo, C1-4alkyl or C1- 4alkoxy and optionally incorporating a heteroatom selected from O, N and S; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.

L'invention se rapporte à des composés sélectifs par rapport au récepteur D4, de la formule générale (I), dans laquelle A et B, qui sont indépendamment choisis, représentent des noyaux homo- ou hétérocycliques insaturés à 5 ou 6 chaînons, éventuellement substitués; X¿1? est choisi parmi CH¿2?, O, NH, S, C=O, CH-OH, CH-N(alkyle C¿1-4?)¿2?, C=CHCI, C=CHCN, N-alkyle C¿1-4?, N-acétyle, SO¿2? et SO; X¿2?--- est choisi parmi N=, CH¿2?-, CH= et C(O); Y est choisi entre N et CH; R¿1? représente alkyle C¿1-4?; n vaut 0, 1 ou 2; q vaut 1 ou 2; et Z représente alkyle C¿5-10? éventuellement substitué par OH, halo, alkyle C¿1-4? ou alcoxy C¿1-4? et contenant éventuellement un hétéroatome choisi parmi O, N et S; et à leurs sels d'addition d'acide, solvates et hydrates. L'utilisation de ces composés comme ligands pour l'identification du récepteur de la dopamine et dans le cadre d'un programme de criblage de médicaments, ainsi que comme agents pharmaceutiques permettant de traiter des états dans lesquels la stimulation du récepteur D4 est impliquée, tels que la schizophrénie, est également décrite.

Affiliated with

Also associated with

Rating

Alkyl-substituted compounds having dopamine receptor affinity does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Alkyl-substituted compounds having dopamine receptor affinity, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Alkyl-substituted compounds having dopamine receptor affinity will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1845039