Farmcampsite for the prevention and treatment of diseases associated with metabolic disorders

 

(57) Abstract:

Usage: in medicine, in particular in pharmacology. The essence of the invention: farmcampsite for the prevention or therapy of diseases associated with metabolic disorders, which contains restored glutathione and at least one anthocyanin compound from the group comprising pelargonidin, peonidin, cyanidin, malvidin, petunidin and delphinidin, with a ratio to the restored glutathione of 1:(0.01 and 0.1) to 1: (3 - -5). This farmcampsite contains tilne derived glutathione from a group that includes an easy-methyl-glutathionyl-(thio)-ether, a simple ethyl-glutathionyl-(thio)-)ether complex mono-acetylglutamine-(thio) ether and complex glutathionyl-(thio) ether monophosphoric acid, and optionally may contain vitamin a in the amount of 10000-50000 units, or-carotene ratio to the restored glutathione 1: (0.005 to 20), and anthocyanin - 1: (0,01-1,5), or selenium ratio to the restored glutathione, comprising (0,0110-3-10010-3):1, and anthocyanin compound - (0,110-3- 510-3: 1) or L-cysteine ratio to the restored glutathione (0.05 to 20:1) and anthocyanin compound (0.1 to 1) :1. Farmcampsite the active substance. 7 C.p. f-crystals.

The invention relates to a therapeutic effect, in particular a drug for the prophylaxis or therapy of metabolic diseases.

The results of scientific research of the past years show that the destructive physical and chemical processes caused by free radicals, for example, chain reaction, and/or activated forms of oxygen, play a growing role in the pathogenesis of many acute and especially chronic diseases, and should be called, for example, arterial and venous diseases, allergies, apaarecida diseases and neoplastic diseases. Reactions of free radicals and activated oxygen species and radicals generated by ionizing radiation in the radiolysis of water, constantly lead to changes and destruction of biomolecules (DNA, RNA, enzymes and structural proteins, unsaturated fatty acids and others) and as a result caused by radicals peroxidative lipid damage and destruction of the membranes of all cells and organs cells. Processes involving radicals play a role in the etiology of all diseases, and often they even are the cause of these diseases, or they continue the R enzymes, having anti-oxidant effect, for example, dismukes peroxide, catalase and peroxidase, which reduces danger of activated forms of oxygen.

Known drug for the prophylaxis or therapy of metabolic diseases, which contains as active substance restored glutathione and/or tilne derived glutathione (see international application published in 1989 under the number WO 89/00427, class A 61 K 37/02).

The effect achieved by using known drugs, is not optimal. In particular the use for therapy restored glutathione as the only active substance can lead to state failure, the reasons for which are:

congenital deficiency of antioxidant enzymes, i.e., the so-called acceptor enzymes (enzymopathies);

insufficient biosynthesis of antioxidant enzymes in different types of cells and, depending on certain unprofitable periods of life (antilopini);

"the deterioration by oxidation restored glutathione in special conditions, for example, in the case of poisoning, inflammation, infections, lack of acceptors, representing enzymes or not representing Enna or radicals peroxosulfates glutathione;

new violations of the biosynthesis of endogenous restored glutathione;

great sport, cachexia, debilitating illness, age.

All of these state failure), which have different causes leading to changes in negative redox potential in all living systems existing in biological spaces, and through the violation of the "redox systems".

Restored glutathione mixed disulfides oxidized glutathione

violations in the system enzymes, especially regarding anti-oxidant and regenerative enzymes to the metabolism of cells, mutations, malignant transformation or cell necrosis.

In addition, known drug for the treatment of wounds, tumors, inflammatory conditions and pathogenic conditions of the vascular system or disorders, the cause of which is the deterioration of lipid or gitignore metabolism (see application DE 27 40 346, class a 61 K 31/35, 1878). This Noah medicine known as an active substance anthocyanidin, for example, cyanidin, peonidin, delphinidin, petunidin, pelargonidin and/or malvidin.

This problem is solved in the proposed drug for the prophylaxis or therapy of metabolic diseases, containing the restored glutathione, due to the fact that it additionally contains at least one anthocyanin compound from the group comprising pelargonidin, peonidin, cyanidin, malvidin, petunidin and delphinidin, with a ratio to the restored glutathione, comprising from 1 (0,01 0,1) to 1 (3-5).

In addition, we offer you the medicine may contain at least one tilne derived glutathione from a group that includes an easy-methyl-glutathionyl-(thio)-ether, a simple ethyl-glutathionyl-(thio)-ether, complex mono - acetyl-glutathionyl-(thio) ether and complex glutathionyl-(thio) ether monophosphoric acid, with a ratio to the restored glutathione and anthocyanin compound, comprising(0,01 0,1) (0,01 0,1) 1.

This problem can be solved in the proposed medicinal product for the prevention or treatment of metabolic diseases, containing at least one tilne derived glutathione from a group that includes an easy-methyl-glutathionyl-(thio)-ether, a simple ethyl-glutathionyl-(thio)-ether, complex mono-acetyl-glutathionyl-(thio)-Epica least one anthocyanin compound from the group including pelargonidin, peonidin, cyanidin, malvidin, petunidin and delphinidin, in relation to toolname derived glutathione equal to 1 (0,01 0,1) to 1 (3-5).

Restored glutathione is a Tripeptide, in its restored form (G SH) present in most human cells and mammalian animals, consisting of three amino acids, namely: glutamic acid, cysteine and glycine, and has the following structural formula:

< / BR>
Restored glutathione ( - -glutamyl-cysteinyl-glycine)

Used according to the invention tirinya glutathione derivatives have the following structural formula:

< / BR>
Simple methyl-glutathionyl-(thio) ether or complex monomethyl-tiefer

< / BR>
Simple ethyl-glutathionyl-(thio) ether or complex monoethyl-tiefer

< / BR>
Complex mono-acetyl-glutathionyl-{thio-ether or complex monoacetyl-thio-ether

< / BR>
Complex glutathionyl-(thio}-ether monophosphoric acid or complex tiefer monophosphoric acid

Anthocyanins are found in many higher plants, where they are responsible for red, purple, blue or bluish-black color of flowers and fruits. They represent a heterocyclic policyleve system is and. Does not contain sugar aglionby components of anthocyanins called antocyanine. They can easily be obtained by hydrolysis of the glycosides present in the normal vegetables and fruits, and they have the following structural formula:

< / BR>
where a value of R1and R2shown in the table

Anthocyanin compounds and restored glutathione and/or its tirinya derivative used for the treatment optimally complement each other depending on the dose of many infringements of cellular functions and many violations of regulatory processes between cells and enzymes. In addition to improving the quality of treatment when combined, restored glutathione and/or its tionally derivatives together with anthocyanin compounds primarily achieved significantly higher performance of the functions of the acceptors. Or preventing the formation of tielnykh radicals (GS), the radical anion of glutathione disulfide (G-S-S-G), and the radicals peroxosulfates-glutathione (G-S O O), or removed toxicity data radicals.

In addition, not only decreases the amount of oxidized glutathione (G-S-S-G) and preventing the formation of radicals glutathione and/or removed their toxicity, the tsya long regeneration removes the toxicity of radical functions. Mutual addition of both groups of substances in the proposed mixture of substances is so optimal that the restored glutathione may again perform all vital functions in genetic terms, in terms of enzymes and in all other respects.

Restored glutathione (G-SH) reacts with, among others quinones, and the formed conjugates of glutathione and hydroquinone, which can samocistici to the appropriate hydrochinone. The conjugation G-SH reduces radical, electrophilic properties of quinones while increasing their hydrophilicity. However, the formation of such conjugates of great importance in relation to toxicology, in cells is limited by the concentration of quinone, and G-SH. This problem is the starting point for the treatment of many diseases, symptomatological respect which is so different. In addition to the new regulation of the physiological behavior of a control loop in all biological relationships and in all cells of living systems the combination of restored glutathione or its tylnej derivatives with anthocyanin compounds is first and foremost a therapeutic effect in the case of induced radical reactions, including chain reactions are the result of the and radiation and others), and if peroxidizable lipids, which is important in pathobiochemical respect phenomenon.

The proposed mixture of substances almost completely prevents the stitching (cross-links) of biomolecules (connective tissue, proteins, DNA, etc.,) in diabetes mellitus and, in particular, when the later syndrome diabetes (prevention education tel Amadori). In addition, it prevents induced peroxidation of lipids and pathogenetically due polyneuropathies degeneration of the peripheral and Central nervous system by preventing the formation of lipofuscin or foci of lipofuscin. In addition, due to the combination of glutathione and anthocyanin compounds prevents the denaturation of proteins in bradytrophic tissues, for example, on the cornea of the eye, the crystalline lens and the vitreous body of the eye.

To further enhance the effectiveness of the proposed medicinal product can be achieved by adding vitamin E (alpha tocopherol acetate) and/or vitamin a and/or b-carotene and/or selenium and/or L-cysteine. The ratio of vitamin E to the restored glutathione and/or toolname derived glutathione amounts (0.1 to 100) 1, and anthocyanin compound (0.5 to 10) 1, soothenol connection -1 (0,01 1,5), the ratio of selenium to the restored glutathione and/or toolname derived glutathione is (0,0110-310010-3) 1, and anthocyanin connection (0,110-3510-3) 1, and the ratio of L-cysteine to the restored glutathione and/or toolname derived glutathione equal to (0.05 to 20) 1 and anthocyanin connection (0,1 -1) 1.

The proposed medicinal product contains vitamin a in the range from 10 000 to 50 000 units.

Depending on the purpose of use (for prophylaxis or therapy) dose of vitamin E per day is preferably 250 to 2000 mg dose of b-carotene 5 150 mg, selenium 50 to 500 g L-cysteine 60 120 mg.

We offer drug using known auxiliary means can be transferred to any liquid or solid preparation.

Especially suitable is the translation offer medicines medicines taken by mouth, and therapeutic dose is typically in the range from 100 mg to 1500 mg per day.

Depending on the purpose of use (for prophylaxis or therapy) dose restored glutathione or Colnago derived glutathione from the specified group is preferably about 10 the tea, if the proposed drug is used for prophylaxis, the ratio of anthocyanin compounds to the restored glutathione and/or toolname derived glutathione is preferably 1 (0,03 0,1). And in that case, if the proposed drug is used for treatment, the ratio of anthocyanin compounds to the restored glutathione and/or toolname derived glutathione is preferably 1 (2 4).

1. Farmcampsite for the prevention and treatment of diseases associated with metabolic disorders, containing reductive glutathione, characterized in that it further comprises at least one anthocyanin compound from the group comprising pelargonidin, peonidin, cyanidin, malvidin, petunidin and delphinidin in relation to reducing glutathione, which accounts for 1 0,01 5.

2. Farmcampsite under item 1, characterized in that it contains at least one tilne derived glutathione from a group that includes an easy-methyl-glutathionyl-(thio)-ether, a simple ethyl-glutathionyl-(thio)-ether complex monoacetyl-glutathionyl(thio) ether and complex glutathionyl-(thio) ether monophosphoric acid at a ratio to restore and 2, characterized in that it contains at least one tilne derived glutathione from a group that includes an easy-methyl-glutathionyl-(thio)-ether, a simple ethyl glutathionyl(thio) ether, complex mono-acetylglutamine-(thio) ether and complex glutathionyl-(thio) ether monophosphoric acid and at least one anthocyanin compound from the group comprising pelargonidin and delphinidin in relation to toolname derived glutathione equal 1 (0,01 0,1) 1 (3 5).

4. Farmcampsite on one of the PP.1 to 3, characterized in that it further contains vitamin E in relation to the restored glutathione and/or toolname derived glutathione, comprising (0.1 to 100) 1, and anthocyanin compound (0.5 to 10) 1.

5. Farmcampsite on one of the PP.1 to 4, characterized in that it additionally contains vitamin a in quantity 10000 50000 IU.

6. Farmcampsite on one of the PP.1 to 5, characterized in that it further contains-carotene in relation to the restored glutathione and/or toolname derived glutathione equal to 1 (0,005 20), and to Antimonopoly connection 1 (0,01 1,5).

7. Farmcampsite on one of the PP.1 to 6, characterized in that it further contains selenium at a ratio of 3) 1, and anthocyanin connection (0,110-3510-3) 1.

8. Farmcampsite on one of the PP.1 to 7, characterized in that it further comprises L-cysteine at a ratio to the restored glutathione and/or toolname derived glutathione, 0.05 20 1 and anthocyanin compound (0.1 to 1) 1.

 

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FIELD: organic synthesis.

SUBSTANCE: invention provides compounds of general formula I:

, where R1 represents -CO-Ra, -SO2-Rb, or aryl optionally substituted by lower alkoxy, wherein Ra represents cycloalkyl, cycloalkyl(lower)alkyl, cycloalkyloxy, aryl, aryloxy, aryl(lower)alkyl, aryl(lower)alkoxy, aryloxy(lower)alkyl, aryl-S-(lower)alkyl, aryl(lower)alkenyl, provided that aryl group can be optionally substituted by halogen, lower alkyl, hydroxy, nitro, cyano, lower alkoxy, phenyl, CF3, cyano(lower)alkyl, lower alkyl-C(O)NH, lower alkyl-CO, and lower alkyl-S; heteroaryl, heteroaryl(lower)alkyl, or heteroaryl(lower)alkoxy, provided that heteroaryl group is 5- or 6-membered ring or bicyclic aromatic group constituted by two 5- or 6-membered rings including 1-3 heteroatoms selected from oxygen, nitrogen, and sulfur and that heteroaryl group can be optionally substituted by lower alkoxy; Rb represents aryl, aryl(lower)alkyl, or heteroaryl, aryl group optionally substituted by halogen, cyano, or lower alkyl-C(O)NH; R2 and R3 represent hydrogen atoms; R4 representshydrogen or lower alkyl; R5 represents hydrogen, lower alkyl, cycloalkyl, benzodioxyl, or aryl optionally substituted by lower alkyl, halogen, lower alkoxy, hydroxy, or (lower)alkyl-C(O)O; n is 1 or 2; and pharmaceutically acceptable salts thereof and/or pharmaceutically acceptable esters thereof. Invention also provides a pharmaceutical composition exhibiting inhibitory activity with regard to cysteine proteases of the cathepsin family, which composition comprises compound of formula I, pharmaceutically acceptable recipient, and/or adjuvant.

EFFECT: increased choice of cysteine protease inhibitors.

34 cl, 1 tbl, 13 ex

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EFFECT: higher efficiency of prophylaxis.

1 cl, 1 ex, 4 tbl

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