Serotonin transport inhibitors

Details Serotonin transport inhibitors Serotonin transport inhibitors

C - Chemistry, Metallurgy

07

D

C07D 493/08 (2006.01) A61K 31/35 (2006.01) C07D 451/02 (2006.01) C07D 495/08 (2006.01)

Patent

CA 2373559

The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders. The compounds of the present invention include those having the structural formula: (see formula I) see formula II) (see formula III) wherein: R1 = COOCH3, COR3, lower alkyl, lower alkenyl, lower alkynyl, CONHR4, or COR6; R2 = is a 6.alpha., 6.beta.; 7.alpha. or 7.beta. substituent, which can be selected from H, OR3, F, Cl, Br, and NHR3; X= CH2, CHY, CYY1, CO, O, S; SO, SO2, or C=CX1Y with the C, O or S atom being a member of the ring; X1 = NR3, CH2, CHY, CYY1, CO, O, S; SO, SO2, or NSO2R3; R3 = H, (CH2)n C6H4Y, CHCH2, lower alkyl, lower, alkenyl or lower alkynyl; Y and Y, = H, Br, Cl, I, F, OH, OCH3, CF3, NO2, NH2, CN, NHCOCH3, N(CH3)2, (CH2)õ CH3, COCH3, or C(CH3)3; R4 = CH3, CH2CH3, or CH3SO2; R6 = morpholinyl or piperidinyl; Ar = phenyl-R5, naphthyl-R5, anthracenyl-R5, phenanthrenyl-R5, or diphenylmethoxy-R5; R5 = Br, Cl, 1, F, OH, OCH3, CF3, NO2, NH2, CN, NHCOCH3, N(CH3)2, (CH2)õ CH3, COCH3, C(CH3)3, 3,4-diCl, 3,4-diOH, 3,4-diOAc, 3,4-diOCH3, 3-OH-4- Cl, 3-OH-4-F, 3-C1-40H, 3-F-4-OH, lower alkynyl; m = 0 or 1; and n 0, 1, 2, 3, 4, or 5; wherein the compound has a SERT/DAT selectivity ratio of at least 3.

L'invention porte sur l'utilisation thérapeutique d'analogues de tropane non aminés qui se lient au transporteur de la sérotonine (SERT) et sont destinés à traiter des troubles neuropsychiatriques. Les composés de la présente invention comprennent ceux qui ont la formule structurelle suivante : (voir formule I) (voir formule II) (voir formule III) dans laquelle : R1 = COOCH3, COR3, alkyle inférieur, alkényle inférieur, alkynyle inférieur, CONHR4, ou COR6; R2 = est un substituant 6.alpha., 6.bêta.; 7.alpha. ou 7.bêta., qui peut être sélectionné à partir de H, OR3, F, Cl, Br et NHR3; X = CH2, CHY, CYY1, CO, O, S; SO, SO2, ou C = CX1Y, l'atome de C, O ou S faisant partie de l'anneau; X1 = NR3, CH2, CHY, CYY1, CO, O, S; SO, SO2, ou NSO2R3; R3 = H, (CH2)n C6H4Y, CHCH2, alkyle inférieur, alkényle inférieur ou alkynyle inférieur; Y et Y, = H, Br, Cl, I, F, OH, OCH3, CF3, NO2, NH2, CN, NHCOCH3, N(CH3)2, (CH2)õ CH3, COCH3, ou C(CH3)3; R4 = CH3, CH2CH3, ou CH3SO2; R6 = morpholinyle ou piperidinyle; Ar = phényle-R5, naphthyle-R5, anthracényle-R5, phénanthrenyle-R5, ou diphe=énylméthoxy-R5; R5 = Br, Cl, 1, F, OH, OCH3, CF3, NO2, NH2, CN, NHCOCH3, N(CH3)2, (CH2)õ CH3, COCH3, C(CH3)3, 3,4-diCl, 3,4-diOH, 3,4-diOAc, 3,4-diOCH3, 3-OH-4- Cl, 3-OH-4-F, 3-C1-40H, 3-F-4-OH, alkynyle inférieur; m = 0 ou 1; et n 0, 1, 2, 3, 4, ou 5; dans laquelle le composé présente un ratio de sélectivité SERT/DAT d'au moins 3.

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