Sulfadimethoxine kannelirovannye semicolonies cyclic compounds, their use as medicaments, also containing pharmaceutical compositions

 

The invention relates to sulfadimethoxine fused semiclean cyclic compounds of the formula (1)where X(1) denotes-O - or-CH2-; X(2) X(3) mean-CH2-; X(4) means-CH2- or-CHOH-; Y(1), Y(2), Y(3) Y(4) independently of one another mean-CR(12)-; R(12) independently of one another denote hydrogen, F, Cl, Br, J; and (C1-C5)-alkyl, CN, NO2, -Z-CmH2m-R(13); Z denotes O or CONR(14); R(14) means hydrogen or(C1-C3)-alkyl; m is 0, 1, 2, 3, 4 or 5; R(13) means hydrogen or phenyl unsubstituted or substituted by a methoxy group, R(3) means R(17)-CxH2x= 1, 2, 3, 4, 5, where R(17) means hydrogen; or R(3) means phenyl, unsubstituted or substituted by 1 or 2 substituents selected from the group comprising F, Cl, Br, (C1-C2)-alkyl or a methoxy group; R(4) means hydrogen or R(20)-CrH2r, r=1, 2, 3, 4, 5, 6; R(20) means hydrogen; R(5) means hydrogen, in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts. Connection 1 have blocking To+-channel effect and can be used in pharmaceutical compositions to obtain medicines for cured the 2 c. and 15 C.p. f-crystals.

Description text in facsimile form (see graphic part)and

Claims

1. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1)

where X(1) denotes-O - or-CH2-;

X(2) X(3) mean-CH2-;

X(4) means-CH2 - or-NON-;

Y(1), Y(2), Y(3) Y(4) independently of one another mean

-CR(12)-;

R(12) independently of one another denote hydrogen, F, Cl, Br, J,

(C1-C5)-alkyl, CN, NO2,-Z-CmH2m-R(13);

Z means On or CONR(14);

R(14) means hydrogen or(C1-C3)-alkyl;

m denotes zero, 1, 2, 3, 4 or 5;

R(13) denotes hydrogen or phenyl, unsubstituted or substituted by a methoxy group;

R(3) means R(17)-CxH2xx=1,2,3,4,5,

where R(17) means hydrogen, or R(3) means phenyl, unsubstituted or substituted by 1 or 2 substituents selected from the group comprising F, C1, Br, (C1-C2)-alkyl or a methoxy group;

R(4) means hydrogen or R(20)-CrH2rr = 1,2,3,4,5,6;

R(20) means hydrogen;

R(5) means hydrogen,

in all their stereoisomeric forms and mixtures thereof in any ratio, and their fiziologii (1) under item 1, where X(1) denotes-O - or-CH2-;

X(2) X(3) mean-CH2-;

X(4) means-CH2or NON-;

Y(1), Y(2), Y(3) Y(4) independently of one another mean-CR(12)-;

R(12) independently of one another denote hydrogen, F, Cl, Br, J, (C1-C5)-alkyl, CN, NR2, -Z-CmH2m, -R(13);

Z means On or CONR(14);

R(14) means hydrogen or(C1-C3)-alkyl;

m denotes zero, 1, 2, 3, 4 or 5;

R(13) means hydrogen or phenyl unsubstituted or substituted by a methoxy group;

R(3) means R(17)-CxH2x,

where x=1, 2, 3, 4, 5,

where R(17) means hydrogen, or R(3) means phenyl, unsubstituted or substituted by 1 or 2 substituents selected from the group comprising F, Cl, Br, (C1-C2)-alkyl or a methoxy group;

R(4) R means(20)-CrH2r, r= 1, 2, 3, 4, 5, 6;

R(20) means hydrogen;

R(5) means hydrogen,

in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts.

3. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) p. 2, where

X(1) denotes-O - or-CH2-;

X(2) X(3) mean-CH2-;

X(4) means-CH2or NON-;

Y(1), Y(2), Y(3) Y(4) independently of each other oznacza the mH2m-R(13);

Z means On or CONR(14);

R(14) means hydrogen or(C1-C3)-alkyl;

m denotes zero, 1, 2, 3, 4 or 5;

R(13) denotes hydrogen or phenyl, unsubstituted or substituted by a methoxy group;

R(3) means R(17)-CxH2xwhere x= 1, 2, 3, 4, 5;

R(17) means hydrogen;

R(4) R means(20)-CrH2r, r= 1, 2, 3, 4, 5, 6;

R(20) means hydrogen;

R(5) means hydrogen,

in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts.

4. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) under item 3, where

X(1) denotes-O - or-CH2;

X(2) X(3) mean-CH2;

X(4) means-CH2or NON-;

Y(1), Y(2), Y(3) Y(4) independently of one another mean-CR(12)-;

R(12) independently of one another denote hydrogen, F, Cl, Br, J, (C1-C5)-alkyl, CN, NO2;

R(3) means R(17)-CxH2xwhere x= 1, 2, 3, 4, 5;

R(17) means hydrogen;

R(4) R means(20)-CrH2r, r= 1, 2, 3, 4, 5, 6;

R(20) means hydrogen;

R(5) means hydrogen,

in all their stereoisomeric forms and mixtures thereof in any otnoshenijah, as well as their physiologically acceptable salts.

5. Sulfadimethoxine Academy of Sciences of the ut-CH2-;

X(4) means-CH2or NON-;

Y(1), Y(2), Y(3) Y(4) independently of one another mean-CR(12)-;

R(12) independently of one another denote hydrogen, F, Cl, Br, J, (C1-C5)-alkyl, CN, NO2;

R(3) means R(17)-CxH2xwhere x= 1, 2, 3, 4, 5;

R(17) means hydrogen;

R(4) R means(20)-CrH2r, r= 1, 2, 3, 4, 5, 6;

R(20) means hydrogen;

R(5) means hydrogen,

in all their stereoisomeric forms and mixtures thereof in any ratio, and their physiologically acceptable salts.

6. Pharmaceutical composition having a blocking To+- channel effect, containing an effective amount of the compounds of formula (1) according to any one of paragraphs.1-5 and/or its physiologically acceptable salts as the active substance together with pharmaceutically acceptable carriers and additives.

7. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products with blocking To+channel action for the treatment and prevention of mediated+channel diseases.

8. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula is for inhibiting the selection of the acid gastric juice.

9. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products for treatment or prevention of ulcers of the stomach or intestinal tract.

10. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal product for the treatment or prevention of reflux esophagitis.

11. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products for treatment or prevention of diseases associated with diarrhea.

12. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products for treatment or prevention of all types of arrhythmias, including atrial, ventricular and supraventricular arrhythmias.

13. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) lubenia or prevention of cardiac arrhythmias, that can be eliminated by lengthening the action potential.

14. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal product for the treatment or prophylaxis of atrial fibrillation or atrial utter.

15. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products for treatment or prevention of recurrent arrhythmias or prevent sudden death from cardiac arrest due to ventricular fibrillation.

16. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products for the treatment of heart failure.

17. Sulfadimethoxine kannelirovannye semicolonies cyclic compounds of formula (1) according to any one of paragraphs.1-5 and/or their physiologically acceptable salts, suitable for medicinal products for inhibition of stimulated excretion of acid gastric juice is diseases, for treatment or prevention of arrhythmias, including atrial, ventricular and supraventricular arrhythmias, atrial fibrillation and atrial utter and recurrent arrhythmias, or to prevent sudden death from cardiac arrest due to ventricular fibrillation.

 

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