Sulfadimethoxine romany and pharmaceutical composition

 

The invention relates to compounds of General formula Iwhere R1and R2) independently from each other hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C-atoms; R3) - R(10)-(CnH2n), where R10- hydrogen, n=0, 1-10,0; R4) - R(13)-CrH2r-Z-CqH2q; where q=0, 1-8; r=0, 1-8; Z IS-CO-NR(14), -OCO-NR(14), -O-CxH2-O-; -O-CxH2-CO-O-; -CO-O-(CxH2)-O-, and connection possible on both sides; x=2, 3 or 4; R14) is hydrogen, alkyl with 1, 2 or 3 C-atoms; R13- hydrogen, -NR(15)R16)=NR(17)NR(15)-R(16), -R(17), phenyl, or N-containing heterocycle with 1-9 C-atoms, and phenyl or N-containing heterocycle unsubstituted or substituted by one Deputy, selected from F, Cl, NO2, NH2, OH, aminosulfonyl; R15and R16) independently from each other hydrogen or alkyl with 1-4 carbon atoms, or R15and R16together denote a chain of 4 or 5 methylene groups, one of which-CH2group can be replaced by-O-, -S-, -NH-, -N(CH3)- or-N(benzyl); R17) - hydrogen; R5) - R(8) independently from each other hydrogen, F, Cl, alkyl with 1-5 carbon atoms; y-CsH+channel, which opens under the action of cyclic adenosine monophosphate (CAMP). 2 C. and 15 C.p. f-crystals, 1 table.

Description text in facsimile form (see graphic part).

Claims

The compounds of formula Iwhere R(l) and R(2) independently from each other hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C-atoms; R(3) - R(10)-(CnH2n), where R(10) is hydrogen; n=0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10; R(4) - R(13) - CrH2r, - Z - CqH2qwhere q=0, 1, 2, 3, 4, 5, 6, 7 or 8, r= 0, 1, 2, 3, 4, 5, 6, 7 or 8, Z denotes-CO-NR(14), -OCO-NR(14), -O-CxH2-O-, -O-CxH2-CO-O-CO-O-(CxH2x)-O, and connection possible on both sides, x= 2, 3 or 4, R(14) is hydrogen, alkyl with 1, 2 or 3 C-atoms, R(13) is hydrogen, -NR(15)R(16), -C(=NR(17))NR(15)R(16), -COOR(17), phenyl, or N-containing heterocycle with 1, 2, 3, 4, 5, 6, 7, 8 or 9 C atoms, and phenyl or N-containing heterocycle metamedium from each other denote hydrogen or alkyl with 1, 2, 3 or 4 C atoms, or R(15) R(16) together imply a chain of 4 or 5 methylene groups, of which one CH2group can be replaced by-O-, -S-, -NH-, -N(CH3)- or-N (benzyl), R(17) is hydrogen; R(5), R(6) R(7) and R(8) independently of one another hydrogen, F, Cl, alkyl with 1, 2, 3, 4 or 5 C atoms; y is CsH2sR(18), where y is-O-, R(18) is hydrogen, phenyl, s=0, 1, 2, 3, 4, 5 or 6; B is hydrogen,
and their physiologically acceptable salts.

2. The compounds of formula I under item 1, in which
R(l) and R(2) independently from each other hydrogen, alkyl with 1, 2, 3, 4, 5 or 6 C-atoms, R(3) - R(10)-(CnH2n); R(10) - H; n=0, 1, 2, R(4) - R(13)-CrH2r- Z - CqH2qq=1, 2, 3, 4, 5, 6, 7 or 8, r=0, 1, 2, 3, 4, 5, 6, 7 or 8, Z denotes-CO-NR(14), -OCO-NR(14), -O-CxH2-O-, -O-CxH2-CO-O-CO-O-(CxH2)-O-, and connection possible on both sides, x = 2, 3 or 4, R(14) is hydrogen, alkyl with 1, 2 or 3 C-atoms, R(13) is hydrogen, -NR(15)R(16), -C(=NR(17))NR(15)R(16), -COOR(17), phenyl, or N-containing heterocycle with 1, 2, 3, 4, 5, 6, 7, 8 or 9 C atoms, and phenyl or N-containing heterocycle unsubstituted or substituted by 1 Deputy selected from F, Cl, NO2, NH2HE aminosulfonyl, R(15) R(16) independently of one another denote hydrogen or alkyl with 1, 2, 3 or 4 C atoms, or R(15) R(16) together imply a chain of 4 or 5 methylene Gorod, R(5), R(6) R(7) and R(8) independently of one another hydrogen, F, Cl, alkyl with 1, 2, 3, 4 or 5 C atoms; y is CsH2sR(18), y is-O-, R(18) is hydrogen, phenyl, s=0, 1, 2, 3, 4, 5 or 6, B is hydrogen, and their physiologically acceptable salts.

3. The compounds of formula I under item 1 or 2, where R(l) and R(2) independently from each other hydrogen, alkyl with 1, 2 or 3 C-atoms, R(3) - R(10)-(CnH2n); R(10) - H; n=0, 1, 2, R(4) - R(13)-CrH2r- Z - CqH2q, q=1, 2, 3, 4, r=0, 1, 2, 3, Z denotes-CO-NR(14), -OCO-NR(14), -O-CxH2x-O-, -O-CxH2-CO-O-CO-O-(CxH2)-O-; and connection possible on both sides, x=2, 3, R(14) is hydrogen, alkyl with 1 or 2 C-atoms, R(13) - -N R(15)R(16), -C(= NR(17))NR(15)R(16), -COOR(17), phenyl, or N-containing heterocycle with 1, 2, 3, 4, 5, 6, 7, 8 or 9 C atoms, and phenyl or N-containing heterocycle unsubstituted or substituted by 1 Deputy selected from F, Cl, NO2, NH2HE aminosulfonyl, R(15) R(16) independently of one another denote hydrogen or alkyl with 1, 2, 3 or 4 C atoms, or R(15) R(16) together imply a chain of 4 or 5 methylene groups, of which one CH2group can be replaced by-O-, -S-, -NH-, -N(CH3)- or-N (benzyl), R(17) is hydrogen, R(5) R(6) independently of one another hydrogen, F, Cl, alkyl with 1, 2, 3, 4 or 5 C-atoms,-Cs-N2sR(18), R(7) and R(8) is hydrogen; y is-O-, R(18)of the formula I on PP.1-3, where R(l) and R(2) - methyl, R(3) denotes methyl or ethyl, R(4) means R(13)-CrH2r-Z-CqH2q, q=1, 2, 3 or 4, r= 0, 1, 2 or 3, Z denotes-CO-NR(14), -OCO-NR(14), x=2 or 3, R(14) is hydrogen or methyl, R(13) - -COOR(17), phenyl, or N-containing heterocycle with 1, 2, 3, 4, 5, 6, 7, 8 or 9 C atoms, moreover phenyl or N-containing heterocycle unsubstituted or substituted by 1 Deputy selected from F, Cl, NO2, NH2HE aminosulfonyl, R(17) is hydrogen, R(5) is hydrogen, alkyl with 1, 2, 3 or 4 C-atoms, F, Cl, R(6) - F, Cl, alkyl with 1, 2, 3, 4 or 5 C-atoms, -y-CsH2s-R(18), R(7) and R(8) is hydrogen, y is-O-, R(18) is hydrogen, phenyl, s=1, 2, 3, 4, 5, B is hydrogen, and their physiologically acceptable salts.

5. The compounds of formula I on p. 1 and their physiologically acceptable salts for use as pharmaceuticals.

6. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication with K+-karavokiros action for the treatment and prevention of diseases associated with K+channels.

7. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are applied to obtain the drug for inhibiting the secretion of acid in the stomach.< the, they are used to receiving medication for the treatment or prevention of stomach ulcers or stomach area.

9. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication for the treatment or prevention of reflux esophagitis.

10. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication for the treatment or prevention of diseases associated with diarrhea.

11. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication for the treatment or prevention of all types of arrhythmias, including atrial, ventricular and supraventricular arrhythmias.

12. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication for the treatment or prevention of cardiac arrhythmias, which can be treated by a potentially long periods.

13. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, Tilletia or atrial same ones.

14. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication for the treatment or prevention of arrhythmia caused by circulation of excitation or inhibition of sudden cardiac arrest due to ventricular fibrillation.

15. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are used to receiving medication for the treatment of heart failure.

16. The compounds of formula I according to one or more paragraphs.1-4 and/or their physiologically acceptable salts, characterized in that they are applied to obtain the drug for inhibition of stimulated acid secretion in the stomach, for the treatment or prevention of stomach ulcers or stomach area, reflux esophagitis, diseases associated with diarrhea, for the treatment or prevention of arrhythmias, including atrial, ventricular and supraventricular arrhythmias, atrial fibrillation and atrial same ones, and arrhythmias caused by circulation of excitation or inhibition of sudden cardiac arrest due to ventricular fibrillation. -
17. Pharmaceutical composition having properties which in at least one connection based on one or more paragraphs. 1-4 and/or its pharmaceutically acceptable salt together with a pharmaceutically acceptable carriers and additives.

 

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