Ortho-substituted benzoylpyridine, the retrieval method and the drug based on them

 

The invention relates to benzoylpyridine formula I

where R(1) denotes CF3; one of the substituents R(2) and R(3) represents hydrogen; and the other of the substituents R(2) or R(3) represents-CH(CH3)-CH2OH; R(4) denotes methyl, and their pharmaceutically acceptable salts. A method of obtaining benzoylpyridine formula I. Also proposed drug, possess inhibitory activity against Na+/H+-exchange and containing an effective amount benzoylpyridine formula I. Technical result - ortho-substituted benzoylpyridine formula I, having a high efficiency of inhibition of Na+/H+-exchange. 3 S. and 12 C.p. f-crystals.

Description text in facsimile form (see graphic part).

Claims

1. Benzoylpyridine formula I

where R(1) denotes CF3;

one of the substituents R(2) and R(3) denotes hydrogen and the other of the substituents R(2) or R(3) represents-CH(CH3)-CH2OH;

R(4) denotes methyl,

and their pharmaceutically acceptable salts.

2. the t hydrogen; R(4) denotes methyl, and their pharmaceutically acceptable salts.

3. Compound I on p. 1 to obtain drugs for treatment or prevention of disease caused by ischemic conditions.

4. Compound I on p. 1 to obtain drugs for treatment or prevention of heart attack.

5. Compound I on p. 1 to obtain drugs for treatment or prophylaxis of angina.

6. Compound I on p. 1 to obtain drugs for treatment or prophylaxis of ischemic conditions of the heart.

7. Compound I on p. 1 to obtain drugs for treatment or prophylaxis of ischemic conditions of the peripheral and Central nervous system and stroke.

8. Compound I on p. 1 to obtain drugs for treatment or prophylaxis of ischemic conditions of peripheral organs and limbs.

9. Compound I on p. 1 to obtain drugs for the treatment of shock.

10. Compound I on p. 1 to obtain drugs for use in surgical operations and organ transplants.

11. Compound I on p. 1 to obtain medicines for canning and storage trane treatment of diseases in which cell proliferation represents a primary or secondary cause, and consequently to obtain antiatherosclerotic assets, against the late complications of diabetes, against cancerous diseases, fibrotic diseases such as pulmonary fibrosis, liver fibrosis, kidney fibrosis, hyperplasia of the prostate.

13. Compound I on p. 1 to obtain drugs for treatment or prevention of disorders of fat metabolism.

14. The method of obtaining the compounds of formula I on p. 1, characterized in that the compound of formula II

where R(1) no R(4) are specified in paragraph (1; L means easy nucleophile replaced the deleted group,

subjected to interaction with guanidine.

15. Drug, possess inhibitory activity against Na+/H+exchange, characterized in that it contains an effective amount of the compounds of formula I under item 1 or 2.

 

Same patents:

The invention relates to compounds of formula (I)

< / BR>
where R(2) and R(3) independently from each other denote hydrogen, Cl, Br, J, (C1-C8)-alkyl, (C3-C8-cycloalkyl or(5), R(5) - (C1-C8)-alkyl, and one of the two substituents R(2) and R(3) is always hydrogen, however, both Deputy R(2) and R(3) at the same time are not hydrogens, as well as their pharmaceutically acceptable salts

The invention relates to new orthotamine benzoylpyridine formula (1), where R(1) - H, alkyl with 1-8 C-atoms, Xand-(CH2)b-(CF2)c-CF3where a, b, C = 0; one of the two substituents R(2) and R(3) means-O-CO-R(27), respectively, and the other substituents R(2) and R(3) is R(1) where R(27) - alkyl with 1-8 C-atoms; R(4) is hydrogen, alkoxy with 1-4 C-atoms, F, Cl, Br, I; R(5) is hydrogen, and their pharmaceutically acceptable salts

The invention relates to novel ortho-substituted benzoylpyridine formula (1), where R(1) denotes H, halogen, Xand-(CH2)b-(CF2)with-CF3, a, b, C denote the zero, one of the two substituents R(2) and R(3) denotes hydroxyl, and the other of the substituents R(2) and R(3) is R(1), R(4) denotes a1-C4-alkyl, halogen, (CH2)n-(CF2)o-CF3n, mean zero, and their pharmaceutically acceptable salts

The invention relates to substituted guanidines thiophenemethylamine acid of the formula I

< / BR>
where mean:

at least one of the substituents R(1), R(2) and R(3)

- Op-(CH2)s-CqF2q+1, R(40)CO - or R(31)SOk-;

p is zero or 1;

s is zero, 1, 2, 3 or 4;

q 1,2, 3,4, 5, 6, 7 or 8;

k is zero, 1 or 2;

R(40) alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms, perfluoroalkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms,

cycloalkyl with 3, 4, 5, 6, 7 or 8 C-atoms or phenyl which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF, methyl or methoxy;

R(31) alkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms, perfluoroalkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms, cycloalkyl with 3, 4, 5, 6, 7 or 8 C-atoms, or phenyl which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF3, methyl or methoxy;

or

R(31) NR(41)R(42);

R(41)and R(42)

independently from each other hydrogen, alkyl with 1, 2, 3 or 4 C-atoms,

perfluoroalkyl with 1, 2, 3 or 4 C-atoms,

or

R(41)and R(42)

together 4 or 5 methylene groups, of which CH2-group may be replaced by oxygen, S, NH, N-CH3or N-benzyl;

and sootwetstwii-OgaWITHraH2raR(10);

PA zero or 1;

mA zero, 1, 2, 3, 4, 5, 6, 7 or 8;

ga zero or 1;

ha zero, 1, 2, 3 or 4;

R(10) cycloalkyl with 3, 4, 5, 6, 7 or 8 C-atoms or phenyl, where the phenyl is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF3, methyl and methoxy;

R(4) and R(5)

independently from each other hydrogen, F, Cl, Br, I, CN, alkyl with 1, 2, 3, 4, 5, 6,

7 or 8 C-atoms, perfluoroalkyl with 1, 2, 3, 4, 5, 6, 7 or 8 C-atoms, cycloalkyl with 3, 4, 5, 6, 7 or 8 C-atoms or phenyl which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF3, methyl, methoxy and NR(14)R(15);

R(14)R(15)

independently from each other H, alkyl with 1, 2, 3 or 4 C-atoms or perfluoroalkyl of 1, 2, 3 or 4 C-atoms

and their pharmaceutically tolerable salts

The invention relates to phenylselenenyl guanidium alkenylboronic acid of the formula (I)

< / BR>
where T means

< / BR>
moreover, R(A) denotes hydrogen, fluorine, chlorine, bromine, iodine, CN, IT, OR(6), (C1-C4)-alkyl, Or(CH2)aCbF2b+l, (C3-C8-cycloalkyl or NR(7)R(8); where

r denotes zero or 1;

a represents zero, 1, 2, 3 or 4;

b means 1, 2, 3 or 4;

R(6) means (C1-C4)-alkyl, (C1-C4)-perfluoroalkyl, (C3-C6)-alkenyl, (C3-C8-cycloalkyl, phenyl or benzyl;

and the phenyl nucleus is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF3, methyl, metoxygroup and NR(9)R(10);

where

R(9) and R(10) mean hydrogen, (C1-C4)-alkyl or (C1-C4)-perfluoroalkyl;

R(7) and R(8) independently of one another are specified for R(6) the value, or

R(7) and R(8) together mean 4 or 5 methylene groups, of which one CH2group can be replaced by oxygen, sulfur, NH, N-CH3or N-benzyl;

R(B) R(C) and R(D) independently from each other are specified for R(A) mn is od CN, OR(12), (C1-C8)-alkyl, Op(CH2)fCgF2g+l, (C3-C8-cycloalkyl or (C1-C9)heteroaryl;

R denotes zero or 1;

f is zero, 1, 2, 3 or 4;

g means 1, 2, 3, 4, 5, 6, 7 or 8;

R(12) means (C1-C8)-alkyl, (C1-C4)-perfluoroalkyl, (C3-C8)-alkenyl, (C3-C8-cycloalkyl, phenyl or benzyl,

and the phenyl nucleus is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF3, methyl, metoxygroup and NR(13)R(14); where

R(13) and R(14) denote hydrogen, (C1-C4)-alkyl or (C1-C4)-perfluoroalkyl;

R(E) has independently specified for R(F) value;

R(1) independently has a specified T value; or

R(1) means hydrogen, -OkCmH2m+l, -On(CH2)pCqF2q+1, fluorine, chlorine, bromine, iodine, CN, -(C= O)-N=C(NH2)2, -SOrR(17), -SOr2NR(31)R(32), -Ou(CH2)vWITH6H5, -Ou2-(C1-C9-heteroaryl or-Su2-(C1-C9-heteroaryl;

k is zero or 1;

m means zero, 1, 2, 3, 4, 5, 6, 7 or 8;

n denotes zero or 1;

p denotes zero, 1, 2, 3 or 4;

q is 1, 2,with hydrogen, (C1-C8)-alkyl or (C1-C8)-perfluoroalkyl or

R(31) R(32) together form a 4 or 5 methylene groups, of which one CH2group can be replaced by oxygen, sulfur, NH, N-CH3or N-benzyl;

R(17) implies (C1-C8)-alkyl;

u means zero or 1;

u2 means zero or 1;

v means zero, 1, 2, 3 or 4;

and the phenyl nucleus is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, Cl, CF3, methyl, metoxygroup, -(CH2)wNR(21)R(22), NR(18)R(19) and (C1-C9)-heteroaryl;

where

R(18) R(19), R(21) R(22) independently of one another denote (C1-C4)-alkyl or (C1-C4)-perfluoroalkyl;

w is 1, 2, 3 or 4;

moreover, a heterocycle (C1-C9)-heteroaryl not substituted or is substituted by 1-3 substituents selected from the group consisting of F, C1, CF3, methyl or metoxygroup;

R(2), R(3), R(4) and R(5) independently of one another are specified for R(1); or

R(1) and R(2) or R(2) and R(3) together mean a group-CH-CH=CH-CH-, which is not substituted or is substituted by 1-3 substituents selected from the group consisting of F, C1, CF3, methyl, metoxygroup, -(CH2)w2NR(24)R(25) and NR(26)R(27);

where
is 1, 2, 3, or 4;

and the molecule contains at least two residue is T, at most three;

and their pharmaceutically acceptable salts

The invention relates to orthotamine benzoylpyridine formula (1), where R(1) denotes R(13)-SOmm denotes the number 2; R(13) denotes alkyl, one of the substituents R(2) and R(3) represents hydrogen; and the other CHR(30)R(31), R(30) represents-(CH2)g-(CHOH)h-(CH2)I-(CHOH)k-R(32), R(32) denotes hydrogen or methyl, g, h, I is equal to zero, k is 1, R(2) and R(3) represents-C(OH)R(33)R(34), R(31), R(33) R(34) denote hydrogen or alkyl, R(4) denotes alkyl, alkoxy, F, Cl, Br, I

The invention relates to compounds of formula (I), where R1, R3-R8 means XYaWZ or X YaWZ', where X Is O; Y - alkylene with 1 to 4 atoms of CH2= 0 , and W is CH2or, if W does not follow directly behind the heteroatom group HUandalso About; Z is-C(=O)R(15) or, if W does not mean Oh, also NR(16)R(17); R(15) is-N=C(NH2)2R(16) and R(17) is hydrogen or alkyl or R(16) and R(17) imply together 4 or 5 methylene groups, of which one CH2-group may be replaced by oxygen or N-(p-chlorophenyl); X' is-C(=O)NR(30); Z' is-C(= O)R(15), N-containing heterocycle with 1-5 C-atoms, and N-containing heterocycle linked through C; the other of R1, R3-R8, which do not fall under the above values, independently of one another denote VpQqU, where V - O, p=0 or 1, q=0, U is hydrogen, alkyl, and one of the substituents R5-R8 are not hydrogen

The invention relates to andinorganic formula I, a method for obtaining medicinal product based on it

The invention relates to new derivatives of fatty acids, which drugs or agrochemicals, with improved performance as it relates to lipophilic derivative of biologically active compounds of the General formula CH3-(CH2)7-CH=CH-(CH2)n-X -, where n is an integer of 7 or 9; X is selected from the group comprising-COO-, -CONH-, -CH2O-, -CH2S-, -CH2O-CO-, -CH2NHCO-, -COS-; lipophilic group SN3-(CH2)7-CH=CH-(CH2)n-X - is CIS - or transconfiguration; And is a fragment of a molecule of biologically active compounds (BAC), non-nucleoside and nucleoside derivative and containing in its structure at least one of functional groups selected from a) alcohol, b) simple broadcast) phenol, (d) amino, (e) thiol, (f) carboxylic acids and (g) of ester carboxylic acid, provided that no connection specified in paragraph 1 of the claims

The invention relates to compounds of formula (I)

< / BR>
where R(2) and R(3) independently from each other denote hydrogen, Cl, Br, J, (C1-C8)-alkyl, (C3-C8-cycloalkyl or(5), R(5) - (C1-C8)-alkyl, and one of the two substituents R(2) and R(3) is always hydrogen, however, both Deputy R(2) and R(3) at the same time are not hydrogens, as well as their pharmaceutically acceptable salts

The invention relates to the cleaning of TETRAFLUOROMETHANE, which is used as a gas for etching or cleaning gas in the production of semiconductor devices

The invention relates to novel ortho-substituted benzoylpyridine formula (1), where R(1) denotes H, halogen, Xand-(CH2)b-(CF2)with-CF3, a, b, C denote the zero, one of the two substituents R(2) and R(3) denotes hydroxyl, and the other of the substituents R(2) and R(3) is R(1), R(4) denotes a1-C4-alkyl, halogen, (CH2)n-(CF2)o-CF3n, mean zero, and their pharmaceutically acceptable salts

The invention relates to medicines, in particular to a mixture of isomers (9)-tetradecanoate

The invention relates to the production of TETRAFLUOROMETHANE used as a solvent, a foaming agent, in the manufacture of foams, as dry provide the Etchant electronic circuits

The invention relates to non-ionic surface-active compositions containing certain combinations of spermatocele, especially useful in detergents
The invention relates to the preparation of polyfluorinated ethers of the formula ROCF2CF2H, where R = CH3or HCF2CF2CH2-

The invention relates to compounds of the formula a-b-D-E-F-G, where the values of the radicals presented in the description in all their stereoisomeric forms and their mixtures in all ratios, and their physiologically acceptable salts
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