12- and 13-substituted ergoline derivatives

Details 12- and 13-substituted ergoline derivatives 12- and 13-substituted ergoline derivatives

C - Chemistry, Metallurgy

07

D

260/206

C07D 457/12 (2006.01) C07F 7/10 (2006.01)

Patent

CA 1289948

ABSTRACT OF THE DISCLOSURE Novel 12- and 13- substituted ergoline derivatives are suitable, e.g., as psychopharmaceuticals and for hypertension thereapy. The compounds have the formula I Image (I) wherein R1 is in the 12- or 13- position and is OR', SH, SR5, SOR5, C(=X)R6, -CR8R9R10, SO2CF3-, S(CH3)3, CN, Cl or I, R' is H, lower alkyl or C1-5 alkanoyl, R5 is lower alkyl, C6-10 aryl, or C6-10-ar-C1-6-alkyl X is 0 or S, R6 is H, CF3, C6-10 aryl, lower alkyl, amino, amino mono or disubstituted by lower alkyl, or OR7, R7 is hydrogen or lower alkyl, R8 is H, OH, 0-C1-5-alkanoyl, 0- lower alkyl, C6-10-aryl, lower alkyl, amino, or amino substituted by lower alkyl, R9 and R10 are identical or different and each is H, lower alkyl or C6-10-aryl, R2 is lower alkyl R3 is NH-CO-NEt2 or NH-CS-NEt2, C9---C10 and C2---C3 each independently is a CC- single or a C=C-double bond, and the hydrogen atom in the 10- position is in the alpha configuration if C9---C10 is a CC-single bond, and the hydrogen atom in the 3-position is in the alpha- or beta-configuration if C2---C3 is a CC-single bond, or a pharmaceutically acceptable acid addition salt thereof.

518527

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