Method for the treatment and prevention of cardiovascular diseases

 

(57) Abstract:

The invention relates to medicine. A method for treatment and prevention of cardiovascular disease with intradermal introduction of a suspension of living cells attenuated streptokinase Museum strains of symbiotic bacteria in a dose of 50-100 MMT, twice - prophylactic, triple and more on the background of traditional therapy in the treatment of cardiovascular diseases. The method increases the concentration in the blood of streptokinase - activator of fibrinolysis. 1 Il.

The invention relates to the field of medicine and biology and can be used for the prevention and treatment of cardiovascular diseases (CVD), including coronary heart disease (CHD) and brain heart attack condition, and the defeat of limb arteries (atherosclerosis, thromboangiitis obliterans).

The greatest efficiency of the present method may be to prevent the occurrence of acute cardiovascular conditions associated with depression of fibrinolysis quick action and spontaneous intravascular thrombosis (myocardial infarction, stroke, and others).

There is a method of treatment of cardiovascular diseases using BA.(1).

The main disadvantages of the known methods is the inability to resolve the depression of fibrinolysis quick action and to prevent the occurrence of spontaneous intravascular thrombosis (myocardial infarction, stroke, and others), as well as their inadequate therapeutic efficacy.

The invention is aimed at solving problems: increasing the efficiency of the method by reducing mortality from CVD, components for Russia in the last 30 years up to 50% of all deaths. (3).

This is achieved by preventing the occurrence of acute cardiovascular conditions associated with spontaneous intravascular thrombosis (myocardial infarction, stroke, heart attack condition, and others), due to the depression of fibrinolysis emergency actions.

The application of this invention can be shown in case of breach of circulatory processes, including microcirculation.

These objectives are achieved by increasing the concentration in the blood and lymph bacterial fibrinolytic enzyme streptokinase (entered when restoring a bacteria carrier streptokinase strains of symbiotic bacteria) - activator of fibrinolysis extraneous element emergency enzymatic fibrinolysis - system plasmin engaged in the human body lightning catalytic decomposition of a drop of blood fibrin clots, blood clots and reduce blood viscosity.

The plasmin system constantly maintains in the blood line of the liquid state of the blood and improves its rheological properties (shear thinning), which prevents spontaneous intravascular thrombosis and significantly improves hemodynamics and blood flow just microcapillary channel.

Fibrinolytic system plasmin is an enzyme system great potential forces which in the presence of blood and lymph bacterial enzyme streptokinase up to 98% of fibrinolysis quick action. (2).

Biological regularities of the process of blood coagulation and fibrinolysis system with the inclusion of the enzyme streptokinase presented in the fundamental work of Czech scientists Raska K. and J. Rotta (4) - (see drawing).

Recovery of bacteria carrier streptokinasetreated bacteria and the normal microflora of the human body, created in the process of evolution and lost during the wide use of antibiotics, is achieved by vnutri beetnik bacteria, producing permanent as their metabolites: enzyme streptokinase - activator plasmin system; enzyme lipoproteins, demoralizing blood cholesterol and other necessary enzymes that regulate homeostasis.

The proposed method is as follows. The patient intradermally usually in the forearm impose a suspension of living cells attenuated streptokinase Museum strains of symbiotic bacteria in sterile saline at a dose of 50-100 MMT - twice with the preventive purpose, three-and more - in the treatment of chronic CVD on the background of traditional therapy with intervals between doses.

Contraindications: acute myocardial infarction, unstable angina.

Examples of specific performance.

Example 1. Patient E., 44 years.

The diagnosis of CHD. Angina, II functional class. Postinfarction cardiosclerosis (25.03.99). Ventricular premature beats. N. I.

Complained of retrosternal pain on mild exertion, weakness, fatigue. 25.03.99, suffered acute transmural peredneperegorodochnoj myocardial infarction with the spread on the top left Zheludok

Objectively: the patient is in satisfactory condition. HR - 66 in minutes BP - 120/80 mm RT.art., T 36,5oC. muffled heart sounds. The vesicular breath.

The abdomen is soft, painless. The liver is not increased. Peripheral edema no.

ECG: cicatricial changes in the Antero-septal region of the left ventricle. Exercise test: tolerance to the load average. Threshold load power 120 watts.

Echocardiography: the heart cavity is not expanded. Hypokinesia of the apical and peregrinating segments of the left ventricle. Myocardial contractility is slightly reduced. The ejection fraction of 52%.

The coagulation tests: prothrombin time 14 s, activated partial thromboplastin time 43, fibrinogen 3.8 g/l, Ha-dependent fibrinolysis 5 min, plasma lysis induced by streptokinase, over 10 min; ADP-platelet aggregation 15 C. Conclusion: inhibition of fibrinolysis.

Biomicroscopy of the conjunctiva: a common conjunctival index 14 points. Functional changes in the vascular wall.

With the consent of the patient with 7.10.99, the patient thrice entered the living cells attenuated streptokinase Museum strains of symbiotic bacteria (SS="ptx2">

After the restoration of the microbiocenosis of complaints about chest pain does not show. Notes the decrease in weakness.

The coagulation tests: prothrombin time 14 s, activated partial thromboplastin time 46, fibrinogen 4.3 g/l, Ha-dependent fibrinolysis 7 min; plasma lysis induced by streptokinase, 7 min, ADP-platelet aggregation 16 C. Conclusion: inhibition of fibrinolysis.

Biomicroscopy of the conjunctiva: a common conjunctival index 6 points. Variant rules.

Thus, the restoration of normal microflora disappeared strokes voltage. According to the coagulation occurred activation of fibrinolysis, as evidenced by the decrease in time of the plasma lysis, activated by streptokinase. Improvement of microcirculation processes recorded by conjunctival biomicroscopy in the dynamics.

Example 2. Patient G., aged 52.

The diagnosis of Thromboangiitis obliterans (Buerger's disease). Occlusion of the popliteal artery on the left of the crural arteries to the right of the arteries of the brush on the right. Amputation stump of the left tibia. KHAN III A.

The patient complained of pain, feeling cold in the right foot. Received treatment with acetylserine feet (swelling, the crimson colour of skin, ulcers in the area of the first finger.

Rheovasography: the blood vessels of the right foot is broken, Art. IV (RI - 0,25); the right leg is reduced, Art. I (RI - 0,82).

With the consent of the patient with 13.04.99, has introduced a suspension of living cells attenuated streptokinase Museum strains of symbiotic bacteria (physiological solution). The first intradermal injection at a dose of 50 MMT, the second and subsequent scheme. Complications were observed.

With the re-examination after 9 months. the patient reported a decrease of pain in the right foot. Signs of inflammation are less pronounced. Healed ulcer in the area of the first finger of the right foot.

Rheovasography: the blood vessels of the right foot is broken, Art. III (RI - 0,34); the right leg is reduced, Art. I(RI - 1,02).

According to the days in the dynamics identified improve blood circulation in the area of the right lower limb.

Example 3. Patient D., 71,

The diagnosis of atherosclerosis, combined lesion, ischemic heart disease. Angina, III functional class. Postinfarction cardiosclerosis (1986). Stenosis of the common carotid artery on the left, both subclavian arteries. Stenosis Powszechny artery on the left. Occlusion of PBA with both storonina limbs through a 100 m walk. Were treated with nitrates, inhibitors AFP, calcium antagonists, answered, aspirin.

Objective: heart rate 68 / min, AD - 170/100 mm RT.art., T 35,1oC. Accent of II tone, systolic murmur at the aortic. The vesicular breathing. The abdomen is soft, painless. Peripheral edema is absent. Ripple a.a.tib.post. not determined.

ECG: scars on the back wall, left ventricular hypertrophy.

The coagulation tests: prothrombin time of 14.5 s, activated partial thromboplastin time 37, fibrinogen 6.5 g/l, XIIa-dependent fibrinolysis 7 min; plasma lysis, induced by streptokinase, 158, ADP-platelet aggregation 13 C. Conclusion: hyperfibrinogenemia, giperagregatsiyu platelets.

Rheovasography of the lower extremities: circulatory disorders of organic nature in the legs and feet more to the right. RI in the legs: the left - 0,45; right - of 0.30. RI in feet: left - 0,30; the right to 0.15.

Doppler ultrasound of the lower extremities: stenotic disease of the iliac-femoral segments on both sides, more pronounced on the right. Occlusion of the superficial femoral artery. The blood flow in the area of the rear foot to the right not lazerette.

With 16.02.99, when receiving einwirkung streptokinase Museum strains of symbiotic bacteria (physiological solution) four-fold in a dose of 50-100 MMT intervals between injections. There were no complications.

After treatment the patient has decreased angina to 1-2 times a day. Increased distance traveled without pain in his legs up to 200 meters

The coagulation tests: prothrombin time 14 s, activated partial thromboplastin time 41 s, fibrinogen 4.8 g/l, Ha-dependent fibrinolysis 6 min; ADP-platelet aggregation 13 C. Conclusion: hypersegregated platelets.

Rheovasography of the lower extremities: the blood vessels of the legs and feet is reduced. RI in the legs: the left - 1,0; right - 0,85. RI in feet: left - 0,82; right - of 0.45.

Doppler ultrasound of the lower extremities: there are signs of collateral blood supply in the area of the right foot.

Thus, after the restoration of normal microflora of the patient decreased angina, decreased symptoms of intermittent claudication. Positive changes in the state of hemostasis resulted in reducing the level of fibrinogen and activation of fibrinolysis. According to the days and of Doppler ultrasound of the lower extremities marked improvement in blood supply to the legs and feet with increased collateral circulation.

Example 4. Patient M, the deposits (1991, 1993, 1995, 1996,) encephalopathy. HNMC III senior KHAN II B Art. Chronic bronchitis, the remission phase.

Complained of weakness, dizziness, a feeling of "numbness" in the rear of the right foot. Long received treatment with antiplatelet agents, nicotinic acid. In stationary conditions have been conducted on courses of anticoagulant therapy.

Objective: HR - 72 minutes BP - 130/80 mm RT.article Heart sounds moderately muted. Breathing hard. The abdomen is soft, painless. Peripheral edema no.

Rheoencephalography: pulse blood pressure hemispheric asymmetric (d>s), is reduced; sadacharan region - symmetric reduced. RI hemispheric areas: right - of 0.55; left - 0,40. RI sadacharan area: right - 0,45; left - 0,50.

With the consent of the patient with 20.04.99, was intradermally injected a suspension of living cells attenuated streptokinase Museum strains of symbiotic bacteria (physiological solution) in a specific pattern at a dose of 80-100 MMT three times with intervals between doses.

In the following intradermal injection was repeated after 3 months once. Complications were observed.

As a result of treatment uluchshilos the priori strokes.

According to rheoencephalography in the dynamics of the improvement of the blood supply to the brain. RI hemispheric areas: right - of 0.65; left - 0,65. RI sadacharan area: right - 0,70; left - 0,70.

The preventive effect of intradermal injections.

For patients aged 45-50-60-75 years (over 50 people) who received intradermal dose of 50-100 MMT twice with the preventive purpose, observations were carried out within 10 years. Deviations in health status and functions of the cardiovascular system are not marked. Key indicators: body temperature within 36,3-36,6oWith the pulse - 66-72 beats./min, blood pressure of 120-140/80-90 mm RT. senior formula and blood rheology is normal.

The use of drugs is only occasional.

The use of the proposed method aims to have a significant impact on the prevention of acute thromboembolic States due to spontaneous intravascular thrombosis, caused by depression of fibrinolysis quick action (myocardial infarction, stroke, and others), and to increase the effectiveness of therapy of CVD associated with dysfunction of the vascular system and deep hemodynamic change the Century Fibrinolysis (biochemistry, physiology, pathology processes). - M.: Moscow state University press, 1979.

3. Oganov, R., Maslennikova, I. Cardiology. - 2000. - 6. - So 40. - S. 4.

4. Raska R., J. Rotta Streptokokove. - Praga, St. zdrav. nakl ad., 1966.

Method for the treatment and prevention of cardiovascular disease, wherein the patient is administered intradermally suspension of living cells attenuated streptokinase Museum strains of symbiotic bacteria in a dose of 50-100 MMT, twice - prophylactic, triple and more on the background of traditional therapy in the treatment of cardiovascular diseases.

 

Same patents:

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 medicine, in particular to pharmaceutical preparations used in the treatment of hypercholesterolemia (primary, combined with hypertriglyceridemia, atherosclerosis
The invention relates to medicine, particularly cardiology, and can be used to prepare for hyperbaric oxygen therapy patients with coronary heart disease

The invention relates to new derivatives of 6-arrepiado[2,3-d]pyrimidine and-naphthiridine, their pharmaceutically acceptable salts, pharmaceutical composition having inhibitory effect of cell proliferation caused by protein tyrosinekinase, and to a method of inhibiting cell proliferation

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

New ketoenamine // 2190599
The invention relates to new ketoenamine formula (1), where R1means phenyl, naphthyl, hinely, pyridyl, chinadoll, Minoxidil, benzothiazyl, isoquinoline, tetrahydroisoquinoline or tetrahydroquinolin, which may be unsubstituted or substituted, R2means hydrogen or alkyl, R3means alkyl, which may carry phenyl ring, X is a bond, -(CH2)m-, -(CH2)m-O-(CH2)0-, -(CH2)n-S-(CH2)m-, -CH= CH-, -CO-CH=CH-, -(CH2)m-NHCO-(CH2)0-, -(CH2)m-CONH-(CH2)0-, -(CH2)m-NHSO2-(CH2)0-, -(CH2)m-SO2NH-(CH2)0-; R4means group OR6, NR7R8; n is a number from 0 to 2

The invention relates to medicine and can be used to obtain therapeutic agents with anti-ischemic activity in the prevention and treatment of ischemic heart disease

New benzamidomethyl // 2189973
The invention relates to new derivatives of benzamidomethyl formula (I), where R1- phenyl, naphthalene, quinoline, isoquinoline, tetrahydroquinoline, tetrahydroisoquinoline, pyridine, hinzelin, cinoxacin, and aromatic and heteroaromatic ring can be substituted by the radicals R4; R2is hydrogen, chlorine, bromine, fluorine, alkyl, -NHCO-naphthyl, -NHSO2- C1-4-alkyl, -O-C1-4-alkyl, -CO-NH - C1-4-alkyl, NO2; R3is a hydrocarbon residue with 1 to 6 carbon atoms, which may carry cycloalkyl, indolenine, phenyl ring, or a residue group-SCH3-; R4- alkyl, -O-C1-4-alkyl, chlorine, fluorine, bromine, iodine, CF3, pyridine; X is a bond, - (CH2)m-, - (CH2)m-O-(CH2)0-, - (CH2)m-S-(CH2)o-, - (CH2)m-SO- (CH2)o-, - (CH2)m-SO2- (CH2)0-, -CH=CH-, -CC-, -CO-CH=CH-, -CH= CH-CO-, - (CH2)m-CO-(CH2)0-, - (CH2)m-NR5CO-(CH2)0-, (R5=H, C1-4-alkyl), - (CH2)m- CONR5-(CH2)0-, - (CH2)m-NHSO2-(CH2)0-, - (CH2)m-SO2NH-(CH2)0-, -N

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 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 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 pharmaceutical industry and relates to agents affecting the cardiovascular system

The invention relates to medicine, in particular to pharmaceutical preparations used in the treatment of hypercholesterolemia (primary, combined with hypertriglyceridemia, atherosclerosis
The invention relates to medicine, particularly cardiology, and can be used to prepare for hyperbaric oxygen therapy patients with coronary heart disease

The invention relates to medicine

The invention relates to medicine and can be used in the treatment of dysbacteriosis
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