Herbal composition for treating and preventing viral blood disorders, such as diseases caused by human immunodeficiency virus (hiv) or hepatitis c
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a composition for treating or preventing the human immunodeficiency virus (HIV) or hepatitis C. The herbal composition used for treating or preventing the patients infected by the HIV or hepatitis C viruses and containing a herbal ingredient with tannin agents and catechin, and a pharmaceutically acceptable carrier; the herbal ingredient is Agrimonia Eupatoria (GAFT) and/or gambier (Uncaria gambir). A method for preparing the herbal composition for treating or preventing the patients infected by the HIV or hepatitis C viruses.
EFFECT: composition is effective for treating or preventing the patients infected by the HIV or hepatitis C viruses.
12 cl, 6 dwg, 2 tbl
The invention relates to compositions based on plants for the treatment or prophylaxis of viral diseases blood diseases such as caused by the human immunodeficiency virus (HIV) or hepatitis C.
HIV has bilateral (belatedly) developing symptoms related to the disease because they occur only after 2-10 years after infection. During this period, there is no external manifestations of the disease, the media can inadvertently transmit the virus during unprotected sexual contact and infect the blood or passing the disease from mother to child. This large incubation period partially guilty of spreading this disease in the form of an epidemic.
There is currently no vaccine that provides protection from HIV and existing methods of treatment, such as retroviral therapy, have a certain efficiency, but does not provide treatment.
In addition, they are not assigned in the initial period of detection of positive serological reactions, because they have many undesirable secondary effects, such as a certain degree of toxicity.
Among the most frequent and less severe effects may include headaches, nausea and vomiting, weakness, loss of appetite, seizures, fever, burning pain or burning in the hands or feet, diarrhea, and skin problems.
Many side effects are constant the mi and are becoming more and more unacceptable because of their duration. When the above effects continue for a long time, they can become irreversible and very crippling.
Other serious side effects occur over time, they are mainly related to the toxicity of the molecules.
While some side effects are fatal.
- skin or respiratory hypersensitivity to abacavir (Ziagen®);
skin hypersensitivity and hepatitis hypersensitivity to nevirapine (viramune);
acute pancreatitis due to ddl (Videx®).
Known conventional methods of treatment do not have minor deficiencies.
The invention offers a solution to this problem and for this purpose provides a composition for the treatment or prophylaxis of viral diseases of the blood, is effective in reducing viral load of the patient and increase the number of T-lymphocytes subpopulations of CD4, which gives fewer side effects in patients who took them in, or total lack of them.
To achieve this goal using the composition of plant-based for the treatment or prophylaxis of viral diseases of the blood, such as human immunodeficiency virus (HIV) or hepatitis C.
In accordance with this invention, the composition includes a powder sulfur, at least one plant component containing agents tannin and catechin, and pharmaco is logicheskie acceptable carrier.
In accordance with other characteristics, a plant compound that contains the agents of catechin and tannin selected from Agrimonia Eupatoria (GAFT) or Gambarova tree (Uncaria gambir).
In accordance with another characteristic, the composition comprises two different plant components containing agents tannin and catechin.
In this case, these plants are Agrimonia Eupatoria (GAFT) and Gambarova tree (Uncaria gambir).
In addition, the composition additionally includes Nigella.
Moreover, Nigella is present in the form of oil.
Additionally, the composition may contain an antiseptic agent.
Preferably as an antiseptic agent used menthol.
In accordance with another characteristic, the composition comprises covering agent.
This covering agent, in particular, is honey.
As indicated above, the composition according to this invention is completely from natural materials, oils and minerals derived from the earth, mixed in certain proportions. In the course of the experiment, it was proved that this product has no side effects and is composed of any stimulating, sedative or tranquilizing agents
The invention also relates to a method for producing the above composition.
This method includes EB the p mixing, at least one plant component containing agents tannin and catechin, with sulfur powder and a pharmacologically acceptable carrier. Moreover, a plant containing catechin and tannin agents, selected from Agrimonia Eupatoria (GAFT) or Gambarova tree (Uncaria gambir).
In accordance with another variant, use two different plants containing agents tannin and catechin, while these plants are Agrimonia Eupatoria (GAFT) and Gambarova tree (Uncaria gambir).
Optionally, the method comprises the step of adding oil Nigella.
Mainly, Agrimonia Eupatoria (GAFT) used in the form of juice, obtained by distillation. Gambir used in the form of finely ground powder.
In accordance with additional features, the method includes a preliminary step of dissolving crystals of menthol in pure alcohol.
Mainly, pharmacologically acceptable base consists of honey with the appropriate viscosity.
This method is simple to use because, basically, consists of mixing the juice Agrimonia Eupatoria (GAFT), sulfur powder, oil, Nigella, Gambia with a pharmacologically acceptable carrier, which used honey.
The invention, its objectives, advantages and features will become clearer from consideration of the following description and drawings, where:
Table 1 shows the values of viral load, smerenney three patients, which received the composition corresponding to the present invention,
- Fig.1 shows a graph of the changes in viral load over time from the first patient who was given the composition according to the present invention;
- Fig.2 shows a graph of the changes in viral load over time in the second patient, who was given the composition according to the present invention;
- Fig.3 shows a graph of the changes in viral load over time in the third patient, who was given the composition according to the present invention;
- table 2 shows the values of (CD4T lymphocytes, measured over 200 days in three patients;
- Fig.4-6 shows a graph of the time variation of the number of CD4three patients, respectively.
The invention will be described primarily a list of the main ingredients used for its production, and secondly it will be shown how to obtain the composition of these ingredients in accordance with the claimed invention, the method of reception of this composition by the patient and its effectiveness is confirmed by clinical tests on patients. Finally, the last part will be a detailed specification of all the ingredients.
The composition according to this invention consists of ingredients that are listed in the table and in these there is roportaj:
|Ingredients||The mass of the tested compositions, (g)||mass % in the composition to be tested in patients, (mass. %)||The mass range of interest, able to ensure the effectiveness of the compositions (mass %)||Function(s) of the ingredient, considered individually|
|GAFT (Latin name: Agrimonia Eupatoria, name: agrimony pharmacy)||5||0,54||0,54=X<1,05||Two forms of catechins+ and -, +catechin has an antibiotic effect and provides preventive effect against the formation of free radicals|
|Uncaria Gambir, name: Gambarova tree||4||0,43||0,43<X<1||Anti-inflammatory, protivogemorragicheskim|
|Oil Nigella Sativa (Latin name: Nigella Sativa L., name: oil nigella or seed oil black cumin)||5||0,54||0,54=X<0,87||Analgesic, antiseptic, expectorant, and is riseptis (against gram-positive and gram-negative bacteria and organisms), anti spastic, histamine inhibitor, acting as a bronchodilatory|
|Powder dietary sulfur (or sublimated sulphur)||2||0,22||0,19<X<0,27||Energy action at the level of the liver|
|Crystals menthol||1,5||0,16||of 0.15<X<0,18||antiseptic|
|Pure alcohol (95° ethanol)||4||0,43||0,38<X<0,49||the solvent (menthol and oil Nigella Sativas)|
|Pure honey||900||97,67||92,24<X<99,83||Covers composition, antioxidant effect, provides absorption in the stomach|
A method of manufacturing
These ingredients combine in the following way:
1.5 grams of menthol crystals are placed in a container at room te is the temperature and normal pressure.
4 grams of pure alcohol, mainly 95° ethanol is injected into the container to dissolve the crystals of menthol, and then, after dissolution, add oil Nigella.
The resulting mixture defend 5 minutes, then stir to accelerate the dissolution.
2 grams of powder dietary sulfur is introduced into the mixture.
Then add 5 grams of juice GAFT. This juice is prepared in advance, using 1 kg of the dried leaves and stems GAFT, soaked in 3.5 liters of water at room temperature for 20 hours. The mixture was then distil heating at a low temperature and collect pairs in the fridge to get about 2 liters of oil GAFT or juice GAFT.
Alcohol, menthol, sulfur powder and juice GAFT then mixed with 900 grams of honey, which has sufficient viscosity to ensure absorption in the stomach.
4 grams of UNCARIA GAMBIR finely melyat and add to the mixture.
5 grams of oil of nigella cold extraction (NIGELLA SATIVA OIL or NADAB EL BARARAT) is added to the mixture and dissolved therein.
Method of use
About 20 grams of the composition every 6 hours, 4 times a day for at least 12 months, the effect of composition on the patient visible after 40 days after the start of treatment.
The effectiveness of treatment of HIV patients
The first patient
In the first phase, the composition was given to a patient with HIV who have stomach ulcers since 2005, this is the same patient who woman, Kubinka, age about 60 years. In the beginning of the treatment she was on the stage of the disease when developed all the symptoms of the disease, and she was suffering from severe stomach ulcers.
She was given a composition for the treatment of ulcers and after five months of treatment, when the patient had to undergo standard tests before traditional treatment (triple therapy), it was found that the plague is not only fully recovered from, but the level of her CD4was equal to 635 units in mm3blood (before treatment it was less than 500 units in mm3blood and viral load was almost undetectable, which confirmed that the traditional treatment was not necessary.
This patient is alive after administration of the compositions of this invention, in good condition is in Cuba since June 2005 without any treatment.
Five other patients with positive serological reaction, Ukrainians, were treated with the claimed composition.
Their serological status was determined in 1997 and 1998. Three of them were additionally have hepatitis C before treatment of the claimed composition. These five patients were under the constant supervision of their doctors.
It was a preliminary examination of their clinical condition and all were found to symptoms of excitement, fever, muscle pain, pain in the PE the Yeni, fatigue, nausea, vomiting, loss of appetite and headaches.
Different blood samples were analyzed in laboratories at different times since the start of treatment up to 70 days after its completion. There have been three clinical and histological studies first before arrival of the patient to treatment, a month after the end of treatment and two months after treatment.
10 days after the start of treatment, all of the above symptoms, which were in patients with the second stage of the disease had disappeared.
All patients were objectively in good condition, no longer suffered from hepatitis C, increased their muscle mass, no fever, and it was noted that their sexual libido, which hardly existed before treatment, reappeared.
Similar improvements were noted in the results of blood tests. Measurements CD4and viral load were organized at various stages of treatment, and were marked light improve CD4. Similar improvements were found in viral load.
The last three patient
Additional clinical tests were carried out in three other patients in collaboration with recognized international research centres on HIV, located in Paris.
In mid-August 2007, three patients, HIV-infected natives of Lebanon, two men the woman, which have infected each other, started treatment. Both men were on the first stage of the disease, and the 26-year-old woman was chosen by the attending physician as already started on treatment by traditional methods (triple therapy).
Three patients decided to meticulously follow the method of treatment developed for the claimed composition on the recommendation of the above research center, the woman subsequently refused traditional treatment.
Before treatment of the claimed composition, the first blood sample was taken from three patients ("day 0" in tables 1 and 2). The results were transferred to the above centers.
All three patients started taking the claimed composition 19 and August 25, 2007, inside every day 20 grams of the composition, 3-4 times a day with an interval of 6 hours.
A second blood sample was taken on 4 October 2007 and was directly sent to the above research centre for analysis and comparison with previous results.
As a result, as can be seen from table 1, after 40 days the viral load in all patients has drastically reduced: 76% in the first patient, 88% in the second patient and 92% in the third.
Based on these positive results, three patients continued to regularly take the claimed composition is 160 days, thus bringing the total period of treatment up to 200 days, as shown in table 1 and table .
The results of the study blood samples confirmed the effectiveness of the composition in time:
One patient, for example patient No. 1, the reduction in viral load was observed continuously from the beginning to the end of treatment, the viral load decreased by 95% at the end of treatment (200 day).
Patient No. 2 was also observed strong decrease between the beginning of treatment and 40 day treatment, because the number of viral copies per ml of blood decreased by 88% and, subsequently, with 40 days they were kept at a level below 12000 copies, in the end were at 8000 per ml of blood, which showed a reduction of 83% in viral load compared with the beginning of the treatment.
The same methodology has been used in the treatment of patient No. 3 and, as can be seen in figure 2, during the first 40 days occurred a decisive reduction of 92% viral load, and then stabilize at a level below 20000 copies per ml of blood between 40 and 200 days of treatment, at the end was achieved low level of about 5000 copies per ml of blood, which gives a decrease of 94% compared to the beginning of the treatment.
Regarding the change in the number of T lymphocytes in mm3blood, there was a slight increase between the beginning and the end of treatment patient No. 1 because the increase in the number of these lymphocytes 17% was observed between day 0 and 200 in the afternoon. A significantly greater rise was noted in patients # 2 and # 3, because between the beginning of treatment and after treatment patient No. 2 T l is Mazitov in mm 3blood increased by 86% and 78% for the patient No. 3, with a significant increase on day 144 to 102%, and lymphocytes in patient No. 3 reached 930 units in mm3blood at that time.
It is important to note that all the above patients were and remain under medical supervision specialists and this observation is confirmed by their good condition.
In accordance with studies, the effectiveness of the claimed composition can be explained by its effect on the virus.
During the tests, the patients were optimized composition, method of use and method of preparation.
Analyzing the optimization process, you can see that GAFT and sulfur powder are the basic elements for the composition, as if their connection, there is the effect of lowering the viral load and the effect of increasing CD4.
In GAFT were found agents tannin and catechin (paragraph "GAFT" in Chapter Details the main ingredients of the composition").
In Gambira (Uncaria Gambir) agents tannin and catechin were re-discovered.
Gambir containing agents tannin and catechin, therefore, may form instead GAFT with sulfur powder base element for receiving the composition, as if their connection, there is the effect of lowering the viral load and the effect of increasing CD4.
Other plants containing catechin and agents tan is on, as explained in the following section describes the details of the ingredients used, can form a powder sulfur basic items to get at their connection with each other, the effect of reducing viral load and increasing CD4.
Oil Nigella is also an integral element of the composition, substantially included in the process of reducing viral load and increasing CD4.
Composition containing plants GAFT and gambir, in combination with oil and nigella powder sulfur, is the most successful to obtain the effect of reducing viral load and increasing CD4.
Composition containing plants and gambir, in combination with butter and powder, sulfur is the most successful to reduce viral load and increase CD4.
The claimed composition, in General, is effective in treating patients infected by the HIV virus, hepatitis C, and ulcers. It is derived from plants and minerals, which protect it from symptoms of harmful side effects.
The method of preparation of the composition easily reproducible.
During the tests was not disclosed an integral part of the composition or method of preparation. Patients took the song inside immediately after its receipt in the presence of medical personnel. Details of constituent ingredients of the claimed compositions are given below.
1) GAFT or agrimony pharmacy is whether Agrimonia Eupatoria
Agrimonia eupatoria L
Other designations: agrimony pharmacy, Church spire, sticklewort, cocklebur
Botany and geography
Origin: hedges, forests and soils in Europe, North Africa, Western and Northern Asia.
Botanical description: a Perennial herb with a height of 40-60 cm, with reddish hairy stems with large leaves divided into unequal segments - many small yellow flowers, gathered in long clusters - fruit-1-2 achenes enclosed in barbed cupped cavity.
Leaves and inflorescence
Tannins, coumarins, flavanol-3 (largely formed by catechins, quercetin, kaempferol, luteolin, apigenin, various phenolic acids, vitamins B and K
Risks to the human body:
2) Gamberini Uncaria Gambir Section: Plantae
Genre: Rubiales: Rubiaceae
Binary name: Uncaria gambir (W. Hunter) Roxb., 1824
Gambir is a medical plant with toning and astringent properties that are used to treat, among other things, burns, diarrhea, cough, sore throat and ulcers. The plant contains tannic acid and catechin.
2.1 Tannic acid is the
This acid can be obtained as a result of disintegration of tannins under the action of microorganisms.
Tannins are a complex combination of glucose and gallium acid, which is found in oak bark, walnut bark and ink nuts. Tannins makes the skin resistant to rotting, so they are used in leather processing. They are also used in the production of ink.
Catechin is a molecule of the family of flavonoids, a subclass of flavonols.
It is also known as pyrocatechin.
It was originally discovered in the fruit of acacia (Acacia catechu), from which was formed the name; catechin and its many isomers are powerful antioxidants that prevent inflammation and coronary disease.
Catechin is a chiral molecule, which has two symmetric form: (+)-catechin and (-)-catechin. To avoid confusion between the class and the composite, the latter being defined in this context as (+/-)-catechin.
(+)- catechin is an antibiotic and antioxidant, which prevents the formation of free radicals.
Plants, except Gambira rich in catechins and tannic acids:
- the tea Bush (Camellia sinensis): flavonoids from the leaves of the tea Bush are 80% of flavonols i.e., (+)- catechin (C, (-)-apichat the chin EC, (+)- gallocatechin GC and their Gallic esters.
Green, red and black teas are known degree of enzymatic oxidation occurring in the leaves during the process, incorrectly called "fermentation". Flavonoids from green tea, is contained in the fresh leaves, composed by 80% of flavonols, but due to the oxidation of black tea remains 20-30%. Tea is known for a high content of tannin agents.
European grapes (Vitis vinifera): grapes are rich ( + ) - catechin, (-) epicatechin and their Gallic esters, apain-3-gallate. These flavonols are concentrated in the bones, in different doses, depending on the grape variety, soil, harvest, phenolic ripeness. High concentrations are found in the grape varieties Merlot and Cabernet Sauvignon. Grapes are rich in tannin agents.
- The cocoa tree (Theobroma cacao): cocoa beans contain 12-18% polyphenols (%of dry material), of which 35% are in the form of (-)-epicatechin (not fermented grains Forastero). To become cocoa beans must undergo fermentation, drying and roasting. During these operations, a large part of catechins and procyanidolic converted to quinones. In cocoa, flavanols are a big part of polyphenols, first (-)-epicatechin and (+)-catechin, (+)-gallocatechin, and (-)-epigallocatechin (EGC), as well as proanthocyanidin consisting of or 3 units+)-catechin and/or (-)-e is catechin, for example procyanidin B1, B2, B3, B4, B5, C1, and D. High temperature roasting transforms (-)-epicatechin in epimer (-)-catechin. Commercial cocoa from the Ivory Coast contain from 2.2 to 4.8 g/kg epicatechin. Cocoa beans also contain tannin agents:
beans are rich in content of catechin and tannin agents;
- many types of fruits are also rich in catechins and tannin agents:
BlackBerry, of course Vinohrady, then cherries, apricots, raspberries, apples, plums, strawberries, peaches and pears.
3) Powder sulfur.
Other name: sulfuric film
salt or derivative: colloidal sulfur
salt or derivative: precipitated sulfur
salt or derivative: washed sublimated sulfur
Chemical classes sulfur
composition: at least 99.5% sulfur
4) Nigella Sativa (Habbat al Barakah or Nigella or vegetable oil black cumin) Composition
Myristic acid: 5%
Palmitic acid: 11,2-13,7%
Stearic acid: 2.1 to 2.6% of the
Palmitoleic acid: 0,1%
Oleic acid: 20,0-23,7%
Linoleic acid (omega 6): 57,9%
Alpha-linolenic acid (omega 3): 0,2%
Arachnid acid: 1,3%
Oil from Nigella (or Nigella or oil Nigella) - this oil is brown-green with a spicy odor.
The oil must be extracted by a cold method.
Used in crystalline form
Use the: pure
7) Pure honey
The viscosity of honey should be sufficient to ensure the absorption of the composition in the stomach.
1. The composition of plant-based, intended for the treatment or prophylaxis of patients infected with HIV or hepatitis C, characterized in that it includes a sulfur powder, vegetable component containing agents tannin and catechin, and a pharmaceutically acceptable carrier, as a vegetable component choose Agrimonia Eupatoria (GAFT) and/or gambir (Uncaria gambir).
2. The composition according to p. 1, characterized in that it further comprises component Nigella (Nigella).
3. The composition according to p. 2, characterized in that the component Nigella is present in the form of oil.
4. The composition according to p. 1, characterized in that it additionally contains antiseptic agent.
5. The composition according to p. 4, characterized in that as the antiseptic agent used menthol.
6. Composition according to any one of the preceding paragraphs, characterized in that it further includes honey.
7. A method of manufacturing the composition of plant-based, intended for the treatment or prophylaxis of patients infected with the HIV virus or hepatitis C is characterized in that it comprises the step of mixing at least one plant component containing agents tannin and catechin with what oscom sulfur and a pharmaceutically acceptable carrier, at this plant, containing catechin and tannin agents, selected from Agrimonia Eupatoria (GAFT) and/or gambir (Uncaria gambir).
8. The method according to p. 7, characterized in that it comprises the step of adding oil Nigella (nigella).
9. The method according to p. 7, characterized in that Agrimonia Eupatoria (GAFT) used in the form of juice obtained by distillation.
10. The method according to p. 7, characterized in that gambir use melkomolotogo powder.
11. The method according to p. 7, characterized in that it includes a preliminary step of dissolving crystals of menthol in pure alcohol.
12. The method according to p. 7, characterized in that the pharmaceutically acceptable carrier contains honey significant viscosity.
SUBSTANCE: invention relates to the field of biotechnology and cell technology. The claimed invention is aimed at the creation of pluripotent, multipotent and/or self-renewing cells, which are able to start differentiating in a culture into various types of cells and are capable of further differentiation in vivo. The claimed invention is also aimed at the creation of populations of the required differentiating cells, which can be transplanted to patients, genetic modification of endogenic cells and treatment of patients, suffering from diseases, intensity of which can be reduced by means of the said methods.
EFFECT: invention also claims methods of prevention, treatment or retardation of a disease, associated with an infection of immunodeficiency virus.
17 cl, 1 dwg, 13 ex
SUBSTANCE: invention refers to medical and molecular genetics. There are described genetic constructs expressing RNA sequences and genes coding proteins possessing the antiviral activity on human immunodeficiency virus. The genetic constructs contain a sequence coding the human TRIM5a modified protein. The invention can be used in scientific investigations.
EFFECT: presented constructs enable providing the higher expression of the modified gene of the human TRIM5a.
40 cl, 4 dwg, 3 tbl, 13 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a pharmaceutical composition in a tabletted dosage form which contains the first layer containing ritonavir and a polymer in a ratio of 1:1 - 1:6, and the second layer containing darunavir. The first layer is produced by hot extrusion, and the second layer - by direct extrusion or wet granulation. Also, the invention refers to a method for preparing the above pharmaceutical composition, and to a method of treating HIV or AIDS involving administering the above composition.
EFFECT: invention enables overcoming the incompatibility of ritonavir and darunavir, and also provides an optimum dissolution profile of both the active substances.
17 cl, 2 tbl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a pharmaceutical composition for HIV-1 replication inhibition containing a compound of Formula
wherein n is equal to 1 or 2; Ar means phenyl substituted by one substitute specified in a group consisting of OH and NO2, or by two substitutes OR, or thienyl; R1 is specified in a group consisting of R6, C(O)N(R6)2, and C1-C6 alkyl substituted by OR; R2 means H or C1-C6 alkyl; R6 is independently in each specific case specified in H and C1-C6 alkyl; each R independently represents C1-C8 alkyl; or its pharmaceutically acceptable salt, or a compound 1G3, or its pharmaceutically acceptable salt. Also, the invention refers to a method of treating an individual either HIV-1 infected or suffering a high risk of HIV-1 infection involving administration of the above composition, to a method for HIV-1 virus replication inhibition.
EFFECT: what is prepared is the new pharmaceutical composition possessing effective biological properties 1G3.
11 cl, 6 tbl, 1 ex
SUBSTANCE: invention relates to improved method of obtaining pyridine compounds (AA),(BB) and (CC) of respective formulas:
said compounds possess inhibiting action with respect to HIV-integrase. method consists in carrying out the following stages: P-1) bromination of compound of formula (I-I) with obtaining bromine-compound of formula (II-II)
where value R represents -CHO, -CH(OH)2, -CH(OH)(OR4), -CH(OH)-CH2OH or -CH(OR5)(OR6); P1 represents benzyl; P3 represents H or protective group of carboxyl; R4 represents lower alkyl; R5 and R6 independently represent lower alkyl or R5 and R6 can represent alkyl and be connected with formation of 5-, 6- or 7-member ring, P-2) formation of side chain of 2,4-di-fluorophenyl-CH2-NH-C(O)- with application of reagents 2,4-di-fluorophenyl-CH2-NH2 and carbon monoxide, stage of formation of Q ring by means of respective amine, selected from 3-amino-butan-1-ol, 2-amino-propan-1-ol and 2-pyrrolidinyl methylamine, and stage of debenzylation with obtaining compound of formula (AA), (BB) or (CC), where said stage P-2 is carried out after formation of Q ring.
EFFECT: method makes it possible to simplify obtaining target compounds due to carrying out regioselective bromination at the first stage.
6 cl, 3 ex, 7 dwg
SUBSTANCE: invention relates to use of nucleoside derivatives - 1,2,5-oxadiazoles of general structural formula I where R1 and R2 are selected from phenylsulphonyl, substituted with one or more halogen atoms, nitro groups, carboxy groups, alkyl halides, CH3, OCH3, OCF3; X is selected from N or N→O; or R1 and R2 form a group, where R', R", R'" and R'''' are independently selected from hydrogen; halogens; nitro groups, hydroxy group, carboxy group, CH3; CH2Br; OCH3; phenylsulphonyl; phenylthio group; or the following groups: R' and R" can also be merged into one of the following common rings for inhibiting human immunodeficiency virus (HIV) replication. The invention also relates to a pharmaceutical composition based on compounds of formula I and a method of inhibiting HIV-1 subtypes A and B integrase, including forms which are resistant to raltegravir.
EFFECT: detecting novel activity in compounds of formula I, which can be used in medicine as HIV replication inhibitors.
3 cl, 5 tbl, 4 ex
SUBSTANCE: invention relates to compounds of general formula or , where Ar1 represents phenyl group, optionally substituted with one or several identical or non-identical halogen atoms; R1 represents hydrogen atom; R4, R5, R6a, R6b represent hydrogen atoms; Y, Z independently represent linear C1-4 alkylene group, optionally substituted with one linear C1-4 alkyl group; Ar2 stands for condensed with benzene 5-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, substituted with one linear C1-4 alkyl group, or derivative of 5- or 6-membered heterocyclic ring, containing one nitrogen atom and one sulphur atom, condensed with heteroaromatic 6-memebered ring, containing one or two nitrogen atoms, substituted with one linear C1-4 alkyl group, linear C1-4 alkoxygroup or group -NR7R8, where R7 and R8 independently stand for hydrogen atom, linear or branched C1-4 alkyl group, or R7 and R8 together with nitrogen atom form group of general formula , where R2, R3 represent linear C1-4 alkyl groups, A stands for group -CHR12, oxygen atom or group -NR9, where R12 and R9 stand for hydrogen atom or linear C1-4 alkyl group, m has value 1 or 2, n has value 1 or 2, o has value 0 or 1, p has value 0 or 1, Q stands for group -O-, group -N--H or group -N--CO-R10, where R10 stands for linear C1-4 alkyl group or -NH-R11 group, where R11 represents linear C1-4 alkyl group; and to their salts. Invention also relates to methods of obtaining therein and to based on them pharmaceutical composition, possessing antagonistic activity with respect to receptor CCR3.
EFFECT: obtained are novel compounds and based on them pharmaceutical compositions, which can be applied in medicine for obtaining medication, intended for treating asthma, allergic rhinitis, atopic dermatitis, eczema, inflammatory intestinal diseases, ulcerous colitis, Crohn's disease, allergic conjunctivitis, multiple sclerosis or HIV-infection and AIDS-associated diseases.
14 cl, 3 tbl, 26 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: presented group of inventions refers to medicine. What is presented is a pharmaceutical composition representing a tablet formulation containing ritonavir in a first layer and atazanavir in a second layer, and a polymer. What is presented is a method for preparing the above pharmaceutical composition wherein a hot melt of rinonavir is extruded to prepare an extrudate to be placed into the first tablet layer, and atazanavir - into the second layer; the first and second layers are combined providing a single multilayer tablet. What is presented is a composition prepared by the method described above to be used in treating HIV or AIDS, and a method of treating HIV or AIDS.
EFFECT: presented group of inventions is effective in creating the multilayer tablet providing a good bioavailability for ritonavir, wherein atazanavir is not degraded in preparation.
19 cl, 5 tbl, 4 ex
SUBSTANCE: invention relates to novel omega-3 lipid compounds of general formula (I) or to their pharmaceutically acceptable salt, where in formula (I): R1 and R2 are similar or different and can be selected from group of substitutes, consisting of hydrogen atom, hydroxy group, C1-C7alkyl group, halogen atom, C1-C7alkoxy group, C1-C7alkylthio group, C1-C7alkoxycarbonyl group, carboxy group, aminogroup and C1-C7alkylamino group; X represents carboxylic acid or its carbonate, selected from ethylcarboxylate, methylcarboxylate, n-propylcarboxylate, isopropylcarboxylate, n-butylcarboxylate, sec-butylcarboxylate or n-hexylcarboxylate, carboxylic acid in form of triglyceride, diglyceride, 1-monoglyceride or 2-monoglyceride, or carboxamide, selected from primary carboxamide, N-methylcarboxamide, N,N-dimethylcarboxamide, N-ethylcarboxamide or N,N-diethylcarboxamide; and Y stands for C16-C22 alkene with two or more double bonds, which have E- and/or Z-configuration.
EFFECT: described are pharmaceutical and lipid compositions, which contain said compounds, for application as medications, in particular, for treatment and/or prevention of peripheral insulin resistance and/or condition of diabetes, for instance, type 2 diabetes, increased levels of triglycerides and/or levels of non-HDL cholesterol, LDL cholesterol and VLDL cholesterol, hyperlipidemic condition, for instance, hypertriglyceridemia (HTG), obesity or condition of excessive body weight, fatty liver disease, for instance, non-alcoholic fatty liver disease (NAFLD) or inflammatory disease or condition.
60 cl, 3 tbl, 65 ex
SUBSTANCE: there proposed is the method for obtaining vaccine against HIV-1 with the use of method of reverse paning at bacterial virus-presented library of HIV-1 - specific scFv antibodies obtained on the basis of mRNA B-lymphocytes of the patients infected by HIV-1 and enriched via paning on HIV-1 peptides and induced systems of expression of recombinant proteins with eukaryotic glycosylation. There also reviewed is the vaccine against HIV-1 and its use for immunisation of non-infected people against infection and development of HIV infection.
EFFECT: HIV-1 vaccine obtained due to this invention provides the appearance of immune response in organism with formation of HIV-1-specific antibodies.
12 cl, 27 dwg, 9 tbl, 4 ex
SUBSTANCE: group of inventions refers to medicine, namely to hepatology and neurology, and can be used for using rifaximin for preparing a drug preparation for maintaining hepatic encephalopathy (HE) remission in a subject. That is ensured by daily administration of rifaximin into the subject for approximately 12 months or more, or approximately 1095 days or longer, thereby maintaining the HE remission.
EFFECT: group of inventions provides the stable HE remission, as well as a low antibiotic resistance of the patient's bacterial flora.
16 cl, 34 dwg, 28 tbl, 6 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to medicine and can be used as a hepatotrophic, lipotropic agent in gastroenterology, as well as for treating cardiac and cerebral atherosclerosis, in neurology in the lower extremity artery diseases (endarteritis). The agent contains tabletted powders of diisopropylammonium dichloroacetate, microcrystalline cellulose, lactose and excipients presented by Aerosil, Primogel and calcium stearyl fumarate.
EFFECT: agent possesses no toxicity, has the high adsorption properties, the apparent anti-inflammatory action, and provides metabolism and the liver regeneration.
3 tbl, 2 ex
SUBSTANCE: according to a known method of treating the liver disease accompanying type 2 diabetes mellitus involving the baseline therapy of diabetes mellitus and prescribed hepatoprotectors, the above hepatoprotector is presented by Mexicor in a daily therapeutically effective dose of not less than 16 weeks. The therapeutically effective dose of Mexicor makes 100 mg 4 times a day.
EFFECT: higher clinical effectiveness ensured by eliminating the liver disease more prominently, reducing the length of treatment, normalising the liver function test results over a short period of time, and avoiding any side effects.
2 cl, 2 tbl
SUBSTANCE: invention refers to medicine and aims at treating the non-alcoholic fatty liver disease. Increasing a transaminase level to three normal values inclusively requires applying essential phospholipids for 2-3 months twice a year that is followed by using statin 10-20 mg in a combination to ursodeoxycholic acid 15-20 mg/kg for 3-6 months. If the transaminase level exceeds three normal values, the treatment is isolated and includes ursodeoxycholic acid 15-20 mg/kg for 3-6 months.
EFFECT: method enables providing the higher clinical effectiveness of the non-alcoholic fatty liver disease.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to medicine, namely to endocrinology, and can be used for treating non-alcoholic liver disease accompanying type 2 diabetes mellitus. The declared preparation Mexicor provides reducing manifestations of cytolysis and cholestasis, decreasing the steatosis index, enables improving metabolic lipid and glycaemic values and reducing insulin resistance. Mexicor is applied in a daily therapeutically effective dose of 100 mg 4 times a day for at least 16 weeks.
EFFECT: high pharmacological activity of Mexicor has been shown by achieving the pronounced and stable elimination of fatty liver disease that enables reducing the length of treatment with no side effects.
2 cl, 2 tbl
SUBSTANCE: invention refers to medicine, namely to surgery, and describes a method for compensating a disturbed intestinal bile inflow in patients with the external biliary drainage. A method for the deficient bile replacement with the external biliary drainage consists in conducting a background therapy, prescribing a therapeutic formulation containing the following ingredients: ursodeoxycholic acid 12-15 mg/kg/day (up to 20 mg/kg) in 2-3 doses, Eslidin (soya lecithin phospholipids 300 mg; methionine 100 mg, soya oil up to 550 mg) 1 capsule 3 times a day at mealtimes; Milaif 0.2 g 3 times a day.
EFFECT: invention enables improving the patient's health condition and relieving a pain syndrome by a safe and technically easy method.
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to a novel derivative of N-acylanthranilic acid, represented by the following general formula 1, or to its pharmaceutically acceptable salt, in which R1, R2, R3, X1, X2, X3, X4 and A are determined in the invention formula.
EFFECT: invention relates to an inhibitor of collagen production, a medication for treating diseases, associated with the excessive production of collagen, containing N-acylanthranilic acid derivative Formula 1.
SUBSTANCE: hepatoprotective agent based on a lipid fraction from an alcohol extract of perforated thallome ulva - Ulva fenestrate P. et R., containing less than 70% membrane-active lipid components, including not less than 20% essential phospholipids with content of polyunsaturated fatty acids of the n-3 series of not less than 55%.
EFFECT: agent has effective hepatoprotective action, speeds up restoration of stages of metabolic reactions, thereby providing normalisation of biochemical properties of carbohydrate and lipid exchange.
SUBSTANCE: hepatoprotector is used as peptide ACTH (4-7) -PGP (Semax) having the formula Met-Glu-His-Phe-Pro-Gly-Pro.
EFFECT: use of the said peptide with the aim of hepatoprotection under condition of the development of free-radical oxidation of hepatocytes enables to improve the efficiency of treatment of liver diseases accompanied by intensification of free radical oxidation processes.
1 tbl, 1 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to a new compound of formula [I] or to its pharmaceutically acceptable salt, wherein A represents optionally substituted alkyl, wherein the substitute represents identical or different 1-3 groups specified in aryl optionally substituted by 1-3 groups specified in alkyl, halogen, alkoxy and alkanoyl; cycloalkyl optionally substituted by 1-3 groups specified in alkyl and halogen; hydroxy; alkoxy; halogen; an amino group and oxo; an optionally substituted carbocyclic group specified in a mono- and bicyclic group, wherein an aromatic ring and cycloalkyl are condensed; optionally substituted aryl, an optionally substituted completely saturated 5- or 6-merous monocyclic heterocyclic group each of which contains 1 heteroatom specified in nitrogen and oxygen, wherein the substitute of optionally substituted aryl, the optionally substituted carbocyclic group and the optionally substituted heterocyclic group for A represents identical or different 1-3 groups specified in alkyl, optionally substituted hydroxy, alkoxy, cycloalkyl or halogen; cycloalkyl optionally substituted by alkyl or alkoxy; alkoxy optionally substituted by halogen; halogen; hydroxy; oxo; heterocycle; alkyl sulphonyl; and mono- or dialkylcarbamoyl, optionally substituted amino, wherein the substitute represents identical or different 1 or 2 alkyl or aryl, or optionally substituted carbamoyl, wherein the substitute represents identical or different 1 or 2 alkyls optionally substituted by aryl, X represents optionally substituted methylene or -O-, wherein the substitute of optionally substituted methylene for X represents alkoxy or hydroxy, Q represents N or C-R4, L1 represents a single bond, methylene, -CH=CH-, -O-, -CO-, -NR11-, -NR11CO-, -CONR11- or -CH2NR11-, L2 represents a single bond, -CR6R7- or a bivalent 5- or 6-merous completely saturated monocyclic heterocyclic group each of which contains 1 heteroatom specified in nitrogen and oxygen, R1 and R2 are identical or different, and each represents hydrogen, alkyl or halogen, R3 and R4 are identical or different, and each represents hydrogen, alkyl, alkoxy, cyano or halogen, R1 and R3 are optionally bond thereby forming 5- or 6-merous cycloalkane, or a 5- or 6-merous aliphatic heterocycle containing oxygen atom, R5 represents a carboxyl group, an alkoxycarbonyl group or a bioisosteric group of the carboxyl group, R6 and R7 are identical or different, and each represents hydrogen or alkyl, or R6 and R7 are bond thereby forming cycloalkane, R8 represents hydroxy, alkanoylamino or alkyl sulphonylamino, R9 and R10 represent hydrogen or halogen, and R11 represents hydrogen or alkyl. Besides, the invention refers to specific compounds of formula [I], a drug based on the compound of formula [I], using the compound of formula [I], a method of treating based on using the compound of formula [I], and an intermediate compound of formula [II].
EFFECT: there are prepared new compounds possessing the agonist activity on thyroid hormone β receptor.
18 cl, 36 tbl, 344 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention refers to the pharmaceutical industry, particularly to a preparation possessing anti-inflammatory, analgesic and wound-healing action. The preparation possessing the anti-inflammatory, analgesic and wound-healing action represents a mixture of an alcoholate of lilac blossom and plantain leaves with honey and extracted juice of unpeeled pomegranate.
EFFECT: preparation possesses the pronounced anti-inflammatory, analgesic and wound-healing action.