Thienopyrimidine, the method of production thereof, pharmaceutical composition having the effect of inhibitors of phosphodiesterase v

 

The invention relates to new thienopyrimidine formula I, their pharmaceutically acceptable salts, having the effect of inhibitors of phosphodiesterase V, which can be used to combat diseases of the cardiovascular system and for the treatment and/or therapy of disorders, to pharmaceutical compositions in a form suitable for treatment. The invention also relates to a method of obtaining thienopyrimidines formula I and their pharmaceutically acceptable salts and pharmaceutical compositions based on them. In thienopyrimidine formula I R1and R2both together represent alkylene with 3-5 C-atoms, R3and R4each independently - H, A, OA or Hal; R3and R4together represent alkylene with 3-5 C-atoms, -O-CH2-CH2-, -O-CH2-O - or-O-CH2-CH2-O-; X is one-deputizing Deputy R7, R5or R6; R5- linear or branched alkylene with 1-10 C-atoms; R6- cycloalkylation with 6-12 C-atoms; R7- COOH, cooa, CONH2, CONHA, CON(A)2or CN; And - alkyl with 1-6 C-atoms; Hal Is F, Cl, Br or I; m = 1 or 2; n = 1, 2, or 3. The method of obtaining compounds of formula I and their salts lies in the interaction of the compounds of formula II, where the-line Oh-group, subjected to interaction with the compound of the formula III, where R3, R4and n have the above meanings, followed, if necessary, converting the resulting compounds of the formula I one residue X in the remainder of X, for example, by hydrolysis of the ester groups to COOH groups, or by conversion of COOH-groups in amide or cyano, and/or translation of the compounds of formula I into one of its pharmaceutically acceptable salts. The pharmaceutical composition contains at least one compound of the formula I and /or one of its physiologically acceptable salts. 3 S. and 4 C. p. F.-ly.

Tablicy

Claims

1. The compounds of formula I

where R1and R2both together - alkylene with 3-5 C-atoms;

R3and R4each independently - H, A, OA or Hal, R3and R4both alkylene with 3-5 C-atoms, -O-CH2-CH2-, -O-CH2-O - or-O-CH2-CH2-O-;

X - one-deputizing Deputy R7, R5or R6,where R5- linear or branched alkylen is CN;

And - alkyl with 1-6 C-atoms;

Hal is F, C1, Br or I;

m = 1 or 2;

n = 1, 2, or 3,

and their physiologically acceptable salts.

2. The compounds of formula I on p. 1:

(a)3-[4-(3-chloro-4-methoxybenzylamine)-5,6,7,8-tetrahydro-[1]-benzothieno[2,3-d]pyrimidine-2-yl]propionic acid;

(b)4-[4-(3,4-methylenedioxyphenethylamine)-5,6,7,8-tetrahydro-[1]-benzothieno[2,3-d]pyrimidine-2-yl]butyric acid;

(C)7-[4-(3,4-methylenedioxyphenethylamine)-5,6,7,8-tetrahydro-[1]-benzothieno[2,3-d]pyrimidine-2-yl]heptane acid;

(g)7-[4-(3-chloro-4-methoxybenzylamine)-5,6,7,8-tetrahydro-[1]-benzothieno[2,3-d]pyrimidine-2-yl]heptane acid;

(e)5-[4-(3-chloro-4-methoxybenzylamine)-5,6,7,8-tetrahydro-[1]-benzothieno[2,3-d]pyrimidine-2-yl]valeric acid;

(e)2-{4-[4-(3-chloro-4-methoxybenzylamine)-5,6,7,8-tetrahydro-[1]-benzothieno[2,3-d]pyrimidine-2-yl]cyclohexyl-1-yl}acetic acid;

and their physiologically acceptable salts.

3. The method of obtaining compounds of formula I on p. 1, and their salts, characterized in that

a) compound of formula II

where R1, R2and X have the above meanings;

L - C1, Br, IT, S3or a reactive esterified Oh-group,

subjected to interaction with the compound of the formula III

them if necessary, converting the resulting compounds of the formula I one residue X in the remainder of X, for example, by hydrolysis of the ester groups to COOH groups, or by conversion of COOH-groups in amide or cyano, and/or translation of the compounds of formula I into one of its pharmaceutically acceptable salts.

4. Pharmaceutical composition having the effect of inhibitors of phosphodiesterase V, characterized in that it contains at least one compound of formula I under item 1 and /or one of its physiologically acceptable salts.

5. The compounds of formula I on p. 1 or their physiologically acceptable salts, having the effect of inhibitors of phosphodiesterase V, to combat diseases of the cardiovascular system and for the treatment and/or therapy of disorders of potency.

6. The compounds of formula I on p. 1 and their physiologically acceptable salts as inhibitors of phosphodiesterase V in a form suitable for treatment.

7. The compounds of formula I under item 1 and/or their physiologically acceptable salts, designed to obtain a pharmaceutical composition for p. 4.

 

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< / BR>
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< / BR>
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