1-(3-heteroaromatic or prop-2-enyl)-4-benzylpiperidine, the method of production thereof and pharmaceutical composition based on them

 

The invention relates to 1-(3-heteroaromatic or prop-2-enyl)-4-benzylpiperidine formula (1), where X Is O, NR1, S, or CH2; Y is CH; Z is CH; Y and Z together may denote C= S; R1, R2and R3is hydrogen, R4- fluoride. Also described is a method of obtaining these compounds, pharmaceutical composition for the treatment and prevention of cerebral disorders on the basis of these compounds and method for producing the pharmaceutical composition. Technical result: received new compounds having valuable biological properties. The invention can be used in medicine as a drug for the treatment and prevention of cerebral disorders. 4 S. and 2 C. p. F.-ly, 1 PL.

Tablicy

Claims

1. 1-(3-Heteroaromatic - or prop-2-enyl)-4-benzylpiperidine formula I

in which X represents O, NR1, S, or CH2;

Y is CH;

Z - SN, while Y and Z together may also denote C=C;

R1, R2, R3each N

R4F is selected from the group including

and)6-{3-[4-(4-terbisil)piperidine-1-yl]propenyl}-3H-ridin-1-yl]propenyl}-3H-benzothiazol-2-he;

g)5-{3-[4-(4-terbisil)piperidine-1-yl]propenyl}-1,3-dihydrobenzo-imidazol-2-he;

d)5-{3-[4-(4-terbisil)piperidine-1-yl]propenyl}-1,3-dihydroindol-2-he,

and their physiologically acceptable salts.

2. The method of obtaining compounds of formula I on p. 1, and their salts, characterized in that the compound of formula II

in which L denotes CL, Br, I, HE or reactionsare esterified HE-group;

X, Y, Z, R1, R2and R3have the values listed in paragraph 1,

subjected to interaction with the compound of the formula III

in which R4matter specified in paragraph 1,

or a compound of the formula I, in which X, R1, R2, R3and R4have the values listed in paragraph 1, and Y and Z together denote C=C, hydronaut, or from the compounds of formula I, in which X, R1, R3and R4have the values listed in paragraph 1, Y is CH; Z is CH and R2HE or L’, with L’ Is CL, Br, I or reactionsare esterified HE group otscheplaut water or L H, and/or the compound of formula I by treatment with acid is transferred into one of its salts.

3. A method of obtaining a pharmaceutical composition, characterized in that the compounds of formula I on p. 1 Witkin carrier or auxiliary substance made appropriate dosage form.

4. Pharmaceutical composition for the treatment and prevention of cerebral disorders, characterized in that it contains an effective amount of at least one compound of formula I under item 1 and/or one of its physiologically acceptable salts.

5. The compounds of formula I under item 1 and/or their physiologically acceptable salts as receptor antagonists of amino acids, providing a stimulating effect.

6. The compounds of formula I under item 1 and/or their physiologically acceptable salts as receptor antagonists of amino acids, providing exciting action to combat neurodegenerative diseases, including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease, respectively, Huntington's disease, cerebral ischemia, heart attacks or psychosis.

 

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