Tetrahydro-gamma-carboline and pharmaceutical composition based on them

 

The invention relates to tetrahydro-gamma carbolines formula (I), where R1, R2D, Alk and n are such as defined in the claims. Also described is a pharmaceutical composition for binding with the receptor 5-HT2, T2aand2based on these compounds. Technical result: received new compounds having valuable biological properties. The invention can be used in medicine. 2 S. and 6 C.p. f-crystals, 9 PL.

Description text in facsimile form (see graphic part).

Claims

1. Tetrahydro-gamma-carboline formula (I)its N-oxide form, pharmaceutically acceptable salt or accession or stereochemical isomeric form, in which R1represents hydrogen, C1-6is alkyl, aryl or C1-6alkyl, substituted aryl; R2represents, each independently, halogen, hydroxy, C1-6alkyl or C1-6alkyloxy; n=0 or 1; Alk is C1-6alcander; D represents a radical of the formula


2. The connection is and.

3. Connection under item 1 or 2, in which R2is halogen, hydroxy, C1-6alkyl or C1-6alkyloxy; n=0 or 1; Alk is C1-4alcander; D represents a radical of formula (a), in which R3represents C1-6alkyl; R4is amino; or R4-R5represents a radical of the formula (a-2) or (a-5), in which one or two hydrogen atoms each independently may be substituted with halogen, C1-6the alkyl, trifluoromethyl, or C1-6alkyloxy, or R4-R5-represents a radical of the formula (a-6), (7), (8), (9), (10) or (11) in which one hydrogen atom may be substituted C1-6the alkyl, or a radical of formula (e), in which X represents S or NR12and R10represents hydrogen, or a radical of formula (f), where X is S or NR12.

4. Connection under item 1 or 2, in which R1represents hydrogen; n=0 or 1; R2represents halogen, C1-6alkyl or C1-6alkoxy; Alk is 1,2-ethandiyl and D represents the radical of formula (a), in which R3represents C1-6alkyl, R4is amino, R5represents C1-6alkyl, or R4-R5- represents a radical of the formula (a-2), (a-5), (6), (7), (8) or (9), in which 2 and R11represents C1-6alkyl.

5. Connection under item 1 or 2, in which R1represents hydrogen; n=0 or 1; R2represents halogen or C1-6alkyl; Alk is 1,2-ethandiyl, and D represents the radical of formula (a), in which R3represents C1-6alkyl, R4and R5taken together, forming a-R4-R5formula (a-2), (a-5), (6), (7) or (8) in which one hydrogen atom may be substituted C1-6the alkyl.

6. Connection on p. 1, in which R1represents hydrogen, methyl, n-butyl, phenyl, benzyl or 4-forfinal.

7. The compound according to any one of paragraphs.1-6, with the ability to bind with the receptors of the 5-HT2, 5HT2aand2.
8. Pharmaceutical composition for binding with the receptor 5-HT2, T2Aand2including pharmaceutically acceptable carrier and as active ingredient a therapeutically effective amount of a compound according to any one of paragraphs.1-6.

 

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< / BR>
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