Method for treating chronic occluding diseases in arteries of inferior limbs
FIELD: medicine, surgery.
SUBSTANCE: medicinal mixture consisting of 10 ml 0.25%-novocaine, 1 ml 1%-emoxypin and 64 c.u. lidase should be injected strictly subcutaneously per 1 ml for each point of injection into the center of plantar surface of nail phalanx of every toe, and for the first inter-toe space - subcutaneously in plantar and rear directions, then, after injections, it is necessary to carry out massage in area if injection with stretching and stroking movements in proximal direction for 10-15 sec, moreover curative seances should be performed every other day , the course being of 5-10 procedures, at repeating this course 3-6 mo later. The present innovation enables to activate transcapillary exchange due to pathogenetically proved impact onto surface and deep lymphatic network of inferior limbs.
EFFECT: higher efficiency of therapy.
1 cl, 2 ex
The invention relates to medicine, in particular for surgery and medical treatment of chronic occlusive arterial diseases of the lower extremities (HOSANK).
Closest to the proposed method of treatment, HOSANK is the method lies in the catheterization lymphatic vessels on the rear foot in the first interdigital interval, the fixation in the vessel lumen polyurethane catheter, through which the subsequent by means of injection dosing medication is injected mixture comprising 0.5% solution of novocaine, 1% solution of nicotinic acid, 2% solution of papaverine, heparin .
However, this method has some drawbacks:
technical complexity and invasiveness of the method.
- the impossibility of carrying out treatment in outpatient conditions;
- the need for holding infusion of special equipment (dispenser injection);
- high probability of injury catheterized vessel directly catheter when the physical movements of the patient or in excess of the speed of infusion;
- the presence of a catheter attached to the rear foot of the patient, significantly restricts his physical activity;
- high probability of formation of bedsores and infection designated standing of the catheter, especially in patients with impaired peripheral kovoor is to be placed;
- if the specified method of introducing a drug mixture is a therapeutic effect only on deep network of lymphatic system of the lower extremities, while in the pathological process in HOSANK involved as deep and surface network of the lymphatic system of the lower extremities.
A new technical challenge - improving the efficiency of treatment of patients by expanding the area of impact of drugs and reduce the number of complications.
The task to solve a new method for the treatment of chronic occlusive arterial diseases of the lower extremities, which consists in the introduction of medicinal mixtures containing novocaine, to the foot area, and medicinal mixture consisting of 10 ml of 0.25% novocaine, 1 ml of 1% emoxipin and 64 UE lidz, enter strictly intradermally in a volume of 1 ml for each point of introduction into the center of the plantar surface of the ungual phalanx of each toe, and in the first interdigital period subcutaneously into the plantar and dorsal directions, then after the injections, make massage the injection zone in the form of kneading and stroking in the proximal direction of movements in for 10-15 seconds, and healing sessions carried out through the day rate of 5-10 treatments, with a repetition rate of 3-6 months, also when expressed pain syndrome or is technote extremities, introduction medicinal mixture is performed, starting with 0.5 ml of gradually bringing to 1 ml on each point of injection.
The method of introduction is as follows.
1. Foot, dorsal and plantar surfaces, from the end of the phalanx to the middle third of the metatarsal treated according to the method of Grassia-Philonchikova.
2. The plantar surface of the nail phalanx squeeze two fingers for 2-3 seconds until the white spot.
3. The injection needle is injected to the depth of its cut in the skin and produce a drug in a volume of 0.5 to 1 ml, focusing on the sensations of the patient, before the formation of the "lemon peel", while the injectable needle according to the principle of “dry” prick.
4. After removal of the needle perform massage kneading and stroking in the proximal direction of motion at each point of injection for 10-15 seconds.
5. In the first interdigital period of injection is performed in dorsal and plantar directions strictly subcutaneously.
Manipulation is done correctly, if at the injection site appears a white patch on the type of "lemon peel" (this suggests that the introduction made intradermally), and when removing the needle there is no appearance of blood.
Typically, patients feel numbness toes for 5 to 20 minutes, and the ATEM slight feeling of itching, lasting from 20 minutes to 2 hours, turning into a feeling of warmth all over the foot and up depending on the severity of the pathological process. To preserve the sense of heat also depends on the severity of the pathological process and lasts from 2 hours after the first manipulation to 6 months after treatment.
The proposed regime is chosen based on the study of literature data on normal and pathological human normal and pathological histology of the human pharmacokinetics and farmakodinamika drugs in humans [2, 3, 4, 5] and the observation of 37 patients who on the ground of submitted complaints, anamnesis, objective and instrumental examination was diagnosed, “Obliterating atherosclerosis of vessels of lower extremities”, with different severity of insufficiency of blood circulation (classification A.V. Pokrovsky-the Fountain): stage IIA - 6 persons, IIB-IIIa - 23, IIIB - 7 people one patient with critical ischemia. The efficacy was assessed on the basis of clinical data, changes the distance of painless ways and data rheovasography.
1. The introduction: the introduction of medicinal mixture intradermally justified by the presence of severe network shunt vessels of the skin, providing the hell is a cotton transcapillary exchange between tissues. In particular, the described techniques - cutaneous vessels perform the role of a heat exchanger. Additional blood flow to the skin not only helps to get rid of the feeling of freezing feet and shins, but in later to provide additional blood supply to the skeletal muscles that are most affected by hypoxia. This conclusion can be considered to be pathogenetically justified due to the fact that the skin is able to maintain a significant amount of blood and, if necessary, to put her skeletal muscles.
2. The necessity of introduction of the mixture into the plantar surface of the toes justified the highest concentration in this area of arteriovenous anastomoses and free nerve endings forming thermoreceptors in the skin of the plantar surface of the toes. In addition, the method allows adequate outflow through the lymphatic capillaries, the terminal which blindly end up in the deep layer of the epidermis, which is a trigger in the treatment of HOSANK. And you cannot ignore the fact that lymphovenous insufficiency is one of the components of the pathogenesis of HOSANK and lymph capillary is one of the important components of structural and functional unit of any organ, including the skin and skeletal muscles.
3. The composition of a medicinal mixture is justified by the fact that the mode is in, first of all, is a local anesthetic and a solvent for lidzy when intradermal.
The emoxipin is an antioxidant having antihypoxic, angioprotective and antiaggregatory activity. The drug successfully used for diseases accompanied by increased lipid peroxidation and hypoxia. This is especially important because in the pathogenesis of HOSANK free-radical oxidation plays an important role.
Lydasum - preparation with the most pronounced lymphotropism property, is able to penetrate through the wall of the lymphatic capillary and to accelerate the absorption of medicinal substances, in particular substances with macromolecular structure and not able to penetrate the vascular wall (the so-called buffer property lidz).
4. The need for massage the area of injection drug mixture is justified by the fact that the lymphatic capillary deprived of the muscle layer and the mechanical movement promote a more rapid and deep penetration of the mixture from interstice in lymphatic capillaries.
5. The need for 5-10 procedures related to the fact that the holding is less than 5 procedures does not provide a stable clinical effect and holding more than 10 treatments are not advisable because of the excessive drug load organisms is the patient. Procedures through the day most optimally, because the injected mixture has a cumulative effect and completely removed from the injection zone for at least 36 hours. In addition, most patients suffering from HOSANK, there is swelling of the affected tissues, and excessive voltage tissues with the introduction of drug compound causes pain.
Clinical example 1
Patient K., born in 1930, was admitted for treatment complaining of freezing and numbness of both feet and legs, pain in them when walking 100 metres. According to the patient, the above complaints concerned about 6-7 years. Were outpatients regularly. On examination, the skin of both feet and legs pale, cold to the touch, the coat is missing, ripple saved on the femoral artery on both sides, below - no. On the basis of complaints and physical examination data, laboratory and instrumental examination diagnosis: “Obliterating atherosclerosis of vessels of both lower extremities, occlusion BPS on both sides, KHAN III and stage”. When reovazograficheskie study of the lower extremities: reovazograficheskie index (RI) to the right (legs) - 33, left 56. Venous outflow is obstructed. The value of peripheral vascular resistance (SAR) is increased. Appointed following the traditional course of treatment:
inside the military drip the solution reopoligliukina, pentoxifylline physiological solution;
- blockade of sympathetic ganglia L 3-L 4;
blockages in the calf muscles of both legs with the introduction of antihypoxic cocktail;
Further appointed endolymphatic introduction described above medicinal mixture. Given the lack of swelling of the feet and lower sensitivity of the fingers, the patient with the first procedure introduced 1 ml of the mixture in each point of injection. After the procedure the patient has noted the emergence of itching of the feet and lower third of the leg. After 20 minutes the itching was replaced by feelings tide of heat to the toes, persisting for 2 hours. The third procedure is itching minor, for 3-5 minutes, a feeling of warmth in the feet remains on during the day, noted a significant improvement when walking, increasing painless ways to 150 meters. For the obtained effect is made even 3 procedures on the background of traditional treatment. At the time of discharge remained complaints to moderate pain in the calf muscles during intensive walk more than 200 metres, passing quickly when you stop. Your feet and legs warm, the sensitivity of the skin of the feet have recovered. Reovazograficheskie index on the left - 60, the right - 53. Venous return to normal. The value of SAR is reduced.
Clinical example 2p> Patient S., born in 1945, was admitted for treatment complaining of freezing and severe pain in both feet and legs when walking up to 50 meters. Moves with the help of a cane, and in the far distance accompanied by relatives. According to the patient, the above complaints concerned about 10 years. History: frostbite of the feet about 12 years ago. Were outpatients, irregularly. From the proposed 7 years ago surgical treatment refused. On examination: skin, legs pale, pasty, feet cyanotic, cold to the touch, toes palpation painful, especially pronounced painful reaction to the compression of the fingers. The peripheral pulse is not detected. On the basis of complaints and physical examination data, laboratory and instrumental examination diagnosis: "Obliterating atherosclerosis of vessels of both lower extremities. Occlusion of the iliac-femoral segment on both sides. KHAN IIIB stage". When reovazograficheskie study of the lower extremities: RI at the level of the tibia on the right 10, left - 18. Venous outflow is obstructed. The value of PSS raised.
Assigned to traditional treatment and advanced treatment according to the proposed method. During the first procedure, the patient complained of increased pain in fingers during injection of a medicinal mixture. For this reason, the volume of the mixture was limited to 0.5 ml. The pain disappeared immediately after removing the needle. During the following three procedures administered amount of the mixture was brought to 1 ml Should be noted that for the first time itchy toes appeared after 3 treatments and a slight appearance of heat after 5 treatments, then the patient noted a slight decrease in pain when walking. The pronounced appearance of heat in the feet appeared after 7 treatments, the patient was more than 50 meters. Upon completion of the course of treatment of the foot and lower leg warm, palpation finger painless, takes place independently with a cane over 100 meters. At the time of discharge continued complaints of pain in the legs, the compressive nature of going after the rest. RI on the left and 40 right - 22. Venous return to normal. The value of SAR is reduced.
Thus, the proposed method can improve the effectiveness of treatment of HOSANK in patients of all ages, different degrees of arterial insufficiency due to pathogenetically reasonable impact on the superficial and deep lymphatic network of the lower extremities with subsequent activation of transcapillary exchange.
Advantages of the method:
- the method is not technically difficult and traumatic;
- easily performed in outpatient conditions;
- does not limit the physical activity of the patient;
- allows vazdeistva is to be as deep, and on the superficial lymphatic network of the lower extremities;
- used medicinal mixture pathogenetically substantiated;
for administration of medicinal mixture does not require special equipment.
Sources of information used in the preparation of the description
1. Lokhvitski SV, Gulyaev AU, Kudinov S. Kaliev Lymph vasodilator therapy obliterating diseases of lower limb arteries // problems of sanogenic and pathogenic effects of the environmental impact on the internal environment of the organism. Mat. IV-th international. the Symposium. and V-th scientific-the practical. Conf., ]. The 70th anniversary of academician Y. I. Borodin and the 60th anniversary of Kyrgyztelecom. - Bishkek, 1999. 1. - S-199.
2. Agadzhanyan N.A., tel LINA, tsyrkin VI, Chesnokov S.A. Physiology. M: Mecnica, 2003. - S-267.
3. Bunny INC., Churilov, L.P. Fundamentals of General pathology. - SPb., 1999. - ALBI. - C - 226.
4. Mashkovsky PPM Medicines. P.II. - M.: Medicine, 1994. - P.71, 215.
5. Alimbekov EG, Chelysheva Y.A. Histology. M.: Publishing house GEOTAR-Med, 2001. - S-502.
1. A method for the treatment of chronic occlusive arterial diseases of the lower extremities, which consists in the introduction of medicinal mixtures containing novocaine, to the foot area, wherein the drug mixture consisting of 10 ml of 0.25% novocaine, 1 ml of 1% emoxipin and 64 UE lidz, impose strict is intradermally at 1 ml per point of introduction into the center of the plantar surface of the ungual phalanx of each toe, and in the first interdigital period subcutaneously into the plantar and dorsal directions after injections produce massage the area of injection kneading and stroking in the proximal direction movements within 10-15 s, and healing sessions carried out through the day rate of 5-10 treatments, with a repetition rate of 3-6 months.
2. The method according to claim 1, characterized in that when expressed pain syndrome or swelling of extremities introduction medicinal mixture is performed, starting with 0.5 ml, gradually increasing the volume to 1 ml in each point of introduction.
SUBSTANCE: method involves inducing angina pectoris attack on no medicament background. Provoking factor action time is measured to the moment the angina pectoris attack takes place. Nitroglycerine is administered in therapeutic dose to reach rapid relief of symptoms. The provoking factor action is repeated to reproduce attack of the same intensity. Provoking factor action time is measured once more. Prediction coefficient K value is calculated as ratio of the repeated provoking factor action time to the provoking factor action time to the moment the angina pectoris attack takes place. Prognosis is considered to be favorable, unfavorable or uncertain during the nearest year depending on K value.
EFFECT: high accuracy in evaluating coronary reserve.
FIELD: medicine, biochemistry.
SUBSTANCE: invention proposes applying CDP-choline (cytidinediphosphocholine) or its salt as a prophylactic agent for treatment of cerebral ischemia and a method for such prophylactic treatment. Invention found new and unknown early mechanism of action of CDP-choline or its salt: inhibition of activation of caspase cascade being the effectiveness of this effect is high in prophylactic intake of drug.
EFFECT: valuable medicinal properties of agent.
6 cl, 5 dwg, 4 ex
FIELD: medicine, cardiology.
SUBSTANCE: invention relates to treatment of patients with post-infarct cardiosclerosis with circulation insufficiency of functional class 2. Method involves using diltiazem with individual setting doses. Method involves carrying out the simplified 2 h oral tolerance test to glucose. Diltiazem is prescribed in the initial dose 90 mg and in the maintenance dose 45 mg in positive result of test. In negative result of test diltiazem is prescribed in the initial dose 180 mg and in the maintenance dose 90 mg. Method provides enhancing effectiveness in treatment of patients with post-infarct cardiosclerosis with circulation insufficiency due to the more precise individual setting dose of the preparation and reducing frequency in arising adverse effects.
EFFECT: improved method for setting, enhanced effectiveness of treatment.
2 tbl, 2 ex
FIELD: pharmaceutical chemistry.
SUBSTANCE: invention, in particular, relates to prolonged therapeutical form of domestic slow calcium channel blocker, namely ankardin-retard-AZIn (active principle 7,7-ethylenedioxybenzopyran-2,2-dione) in the form of 0.1% solution administered in dose 1 ml in the form of complex with poly(ethylene oxide) 400. Pre-clinical investigations indicated that Ankardin-retard-AZIn was a sufficiently active calcium ion antagonist and, after clinical investigations, it could be applied in medical practice for prevention and treatment of cardiovascular diseases.
EFFECT: extended choice of drugs.
6 tbl, 4 ex
FIELD: medicine, cardiology.
SUBSTANCE: the present innovation deals with decreasing side effects of medicinal preparation of cardiotoxic component. For this purpose it is suggested to apply cariporide to decrease unfavorable impact of macrolide antibiotic, rulide, in particular. The innovation suggested provides the chance to remove side effects of macrolide antibiotic regarding patient's heart under conditions of ischemia and reperfusion.
EFFECT: higher efficiency of application.
FIELD: organic chemistry, pharmaceutical compositions.
SUBSTANCE: invention relates to substituted 3-oxo-1,2,3,4-tetrahydroxinoxalines of general formula 1 , wherein R1 represents substituted sulfanyl or substituted sulfonyl group, containing as substituent optionally substituted C1-C4-alkyl, optionally substituted C3-C8-cycloalkyl, aryl-(C1-C4)alkyl optionally substituted in aril or alkyl group, heterocyclyl-(C1-C4)alkyl optionally substituted in heterocycle or alkyl group; R2 and R3 independently represent hydrogen, halogen, CN, NO2, optionally substituted hydroxyl, optionally substituted amino group, optionally substituted carboxylic group, optionally substituted carbamoyl group, optionally substituted arylcarbonyl group or optionally substituted heterocyclylcarbonyl group; R4 and R5 independently represent hydrogen or inert substituent. Claimed compounds are high effective kaspase-3 inhibitors and are useful in production of pharmaceutical compositions for treatment of diseases associated with excess apoptosis activation, as well as for experimental investigations of apoptosis in vivo and in vitro. Also disclosed are pharmaceutical composition in form of tablets, capsules or injections in pharmaceutically acceptable package, as well as method for production thereof and therapy method.
EFFECT: pharmaceutical composition for apoptosis treatment and investigation.
6 cl, 3 dwg, 8 ex, 1 tbl
SUBSTANCE: method involves using mononuclear autologic marrow fraction containing 6-9x104 mesenchyma cells per 1 ml or autologic mesenchyma trunk cells. The cells are separated from brain bioptate in the amount of 106 cells/kg of patient body mass. The preparations are intracoronarily introduced in fractions at a rate of 3-5 ml/min into the right coronary artery. The introduction is also carried out in intra-arterial mode in jets or in drops.
EFFECT: higher survival rate and life quality of cardiologic patients.
FIELD: new 2,4,6-trimethyl-3-oxypyridine nitrosuccinate and method for production thereof.
SUBSTANCE: claimed compound is useful in medicine as future antiishemic agent with vasodilatation effect and has potent protective action in barotraumatic damages and ballistic wounds due to inhibition of secondary necrosis creation and progress. Compound of present invention is obtained by nitration of malic acid with mixture of sulfuric and nitric acids, separation of nitrohydroxymalic acid and treatment thereof with 2,4,6-trimethyl-3-oxypyridine in alcohol media with subsequent isolation of target product.
EFFECT: new antiishemic agent.
2 cl, 1 ex
SUBSTANCE: the present innovation deals with phospholipid complexes of proanthocyanidine A2 and pharmaceutical compositions upon their basis as antiatherosclerotic agents, those for preventing and treating myocardial and cerebral infarction. Phospholipids of the above-mentioned complex should be preferably chosen out of lecithins, phosphatidyl choline, phosphatidyl ethanolamine, phosphatidyl serine. The innovation provides the preparation to treat the above-mentioned diseases due to decreasing the quantity and burden of atheromatous plaque, decreased obstruction of carotid arteries and decreased thickness of vascular walls.
EFFECT: higher efficiency of prophylaxis and therapy.
9 cl, 11 dwg, 6 ex, 2 tbl
FIELD: organic chemistry, biochemistry, medicine, pharmacy.
SUBSTANCE: invention relates to new aminobenzophenones of the formula (I):
or their pharmaceutically acceptable salts. These compounds elicit properties of inhibitors of cytokines secretion, in particular, 1β-interleukin (IL-1β) and tumor necrosis α-factor (TNF-α) and to secretion of polymorphonuclear superoxide that are useful for treatment of inflammatory diseases, for example, skin diseases, such as psoriasis, atopic dermatitis. In the formula (I) R1 is taken among the group consisting of halogen atom, hydroxy-, mercapto-group, trifluoromethyl, amino-group, (C1-C3)-alkyl, (C2-C3)-olefinic group, (C1-C3)-alkoxy-, (C1-C3)-alkylthio-, (C1-C6)-alkylamino-group, (C1-C3)-alkoxycarbonyl, cyano-group, carbamoyl, phenyl or nitro-group under condition that when R1 means a single substitute then it at ortho-position, and when R1 means more one substitute then at least one substitute of R1 is at ortho-position; R2 means one substitute at ortho-position being indicated substitute is taken among the group consisting of (C1-C3)-alkyl, (C1-C3)-alkoxy-group; R3 means hydrogen, halogen atom, hydroxy-, mercapto-group, trifluoromethyl, amino-group, (C1-C3)-alkyl, (C2-C3)-olefinic group, (C1-C3)-alkoxy-, (C1-C3)-alkylthio-, (C1-C6)-alkylamino-group, (C1-C3)-alkoxycarbonyl, phenyl, cyano-, carboxy-group or carbamoyl; R4 means hydrogen atom or (C1-C3)-alkyl; Q means a bond or -SO2-; Y means (C1-C15)-alkyl, (C3-C10)-carbocyclic group or phenyl being each of them can be substituted optionally with one or some similar or different substitutes designated by the formula R5; R5 means halogen atom, (C1-C4)-alkyl, amino-, (C1-C3)-alkoxy-group, (C1-C3)-alkoxycarbonyl or -COOH; X means oxygen or sulfur atom. Also, invention relates to a pharmaceutical composition and to a method for treatment and/or prophylaxis of inflammatory diseases.
EFFECT: valuable medicinal properties of compounds and composition.
9 cl, 2 sch, 2 tbl, 29 ex
FIELD: medicine, gynecology.
SUBSTANCE: one should perform surgical destruction of endometrioidal heterotopias, antibioticotherapy followed by hormone-modulating therapy. Moreover, it is necessary to irradiate blood through a monofilamentous quartz light guide introduced into patient's elbow vein with the help of He-Ne laser at wave length being 628 nm at 15 min duration during the first 5 procedures and for 30 min during 2 last procedures followed by prescribing GnRH agonists for 7 d at the background of antibioticotherapy, intake of analgetics and vobenzyme beginning since the 1st postoperative day.
EFFECT: higher efficiency of therapy.
SUBSTANCE: the present innovation deals with preventing the development of hypoxia due to introducing ceruloplasmin 1 d before hypoxia. The method enables to exclude the development of allergic reactions.
EFFECT: higher efficiency of hypoxia prevention.
2 ex, 3 tbl
FIELD: veterinary medicine.
SUBSTANCE: poultry's diet during the first and second phases of egg yield should be supplemented with roxazym enzymatic complex at the ratio towards husk-bearing components being 0.007 - 0.009 : 20. The present innovation prevents inflammation of oviducal vagina in laying hens.
EFFECT: higher efficiency of prophylaxis.
FIELD: medicine, pharmacology, pharmacy.
SUBSTANCE: invention relates to the agent comprising the following components: lidazum (16-32 U), proserinum 0.05% solution, 0.00025-0.0005 g; methylprednisolone succinate sodium, 0.02-0.04 g; lidocaine 10% solution, 0.05-0.1 g, and glucose 40% solution, 3-4 ml. Also, invention relates to a method for administration of agent and a method for treatment of inflammatory diseases. Invention provides expanding assortment of medicinal agents and improving the regional transport of medicinal preparations.
EFFECT: improved and valuable properties of agent.
6 cl, 5 ex
FIELD: organic chemistry, biochemistry.
SUBSTANCE: invention relates to substituted derivatives of N-phenyl-2-hydroxy-2-methyl-3,3,3-trifluoropropaneamide of the formula (I): wherein n = 1 or 2; R1 represents chlorine, fluorine, bromine atom, methyl or methoxy-group; R2 is taken among of one the following groups: (i) halogen atom, nitro-, hydroxy- amino- or cyano-group; (ii) -X1-R5 wherein X1 represents -O-, -S-, -SO-, -SO2-, NR6-, -CO-, -CONR6-, -NR6CO- wherein R6 represents hydrogen atom and R5 is taken among (C1-C6)-alkyl optionally substituted with one or some A, and so on; (iii) 4-8-membered heterocyclic group joined by nitrogen atom that represents saturated monocyclic ring comprising 4-8 carbon atoms among that at least one is nitrogen atom and so on; R3 represents (C1-C6)-alkyl optionally substituted with one or some A and so on; A is taken among hydroxy-, amino-group, halogen atom, carboxy-, N-(C1-C4-alkyl)-amino-, N,N-di-(C1-C4-alkyl)-amino-group, carbamoyl and (C1-C6)-alkoxy-group; D is taken among: (i) -Xa-Rc wherein Xa represents -SO2, -CO-, -NRdCO-, -NRd- or -CONRd-; (iv) cyano-group or halogen atom; (v) -XcRf wherein Xc represents -C(O)- and Rf represents 4-8-membered heterocyclic group joined by nitrogen atom that represents saturated monocyclic ring comprising 4-8 carbon atoms among that at least one is nitrogen atom with optionally additional heteroatom taken independently among oxygen atom (O), optionally substituted at ring carbon atom by the hydroxy-group, halogen atom, (C1-C4)-alkoxy-group, (C1-C4)-alkyl or cyano-group; G represents (C1-C6)-alkanoyl; R4 represents hydrogen or fluorine atom; or to its pharmaceutically acceptable salt or its ester hydrolyzed in vivo. Also, invention proposes a method for preparing compound of the formula (I). Also, invention proposes pharmaceutical composition enhancing activity of pyruvate dehydrogenase comprising substituted derivatives of N-phenyl-2-hydroxy-2-methyl-3,3,3-trifluoropropaneamide of the formula (I) or its pharmaceutically acceptable salt or ester hydrolyzed in vivo in combination with pharmaceutically acceptable vehicle or carrier. Invention provides preparing derivatives of N-phenyl-2-hydroxy-2-methyl-3,3,3-trifluoropropaneamide enhancing activity of pyruvate dehydrogenase.
EFFECT: valuable medicinal and biochemical properties of compounds.
14 cl, 1 tbl, 85 ex