Compositions, synthesis and methods for application of phenylcycloalkylmethylamine derivatives

FIELD: pharmacology.

SUBSTANCE: invention relates to new phenylcycloalkylmethylamine derivatives of structural formula (I), or enantiomers or optically active isomers, or pharmaceutically acceptable salts having affinity for the binding of dopamine (DAT), the carrier of norepinephrine (NET) and the serotonin transporter (SERT). The compounds may find use in treatment and/or prevention of obesity, as well as depression 1. In the structural formula (I)

,

n is 1; SP is a spacer, wherein the said spacer is C4 alkylene; X is O or S; R1 and R2 are independently H, C1-6 alkyl, C1-6 alkoxy, halogen; R3 is C1-6 alkyl; R4 is H or C1-6 alkyl; R5 is C1-6 alkyl; and * represents a carbon atom that can be optically active.

EFFECT: improved composition properties.

12 cl, 1 tbl, 86 ex

 



 

Same patents:

FIELD: chemistry.

SUBSTANCE: invention relates to novel substituted cyclohexylmethyl derivatives, having serotonin, noradrenaline or opioid receptor inhibiting activity, optionally in form of cis- or trans-diastereomers or mixture thereof in form of bases or salts with physiologically compatible acids. In formula (1): R2 denotes H or OH; R1 and R2 together denote or =N-OH, R3 denotes a phenyl residue which is unsubstituted or monosubstituted with a halogen atom or a heteroaryl residue selected from a five-member sulphur-containing heteroaryl such as a thienyl residue or an unsubstituted phenyl residue bonded through a C1-C4alkyl group, R4 and R5 independently denote an unsubstituted C1-C3alkyl or R4 and R5 together denote (CH2)3-6, R8 denotes a linear saturated C1-C4 alkyl group bonded with an aryl, which is unsubstituted or monosubstituted with halogen atoms, R9 denotes a saturated C1-C8alkyl; values of radicals R1, m, n, R6, R7, R10-R13 are given in the claim. The invention also relates to methods of producing compounds of formula (I), a medicinal agent containing said compounds, use of compounds of formula (I) to prepare a medicinal agent for anaesthetic treatment during sharp, neuropathic or chronic pain and for treating depression, urinary incontinence, diarrhoea and alcoholism.

EFFECT: high efficiency of using the compounds.

32 cl, 501 ex, 21 tbl

FIELD: medicine, neurology.

SUBSTANCE: the present innovation describes arylalkylamines that specifically affect certain types of receptor-operated Ca2+-canals, their application and pharmaceutical compositions for treating neurological disorders or diseases.

EFFECT: higher efficiency.

55 cl, 29 ex, 11 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, namely to therapy and pharmaceutics, and deals with an influence on the functional activity of a cannabinoid receptor. For this purpose an activated-potentiated form of antibodies to the human cannabinoid receptor is introduced into an organism with the application of an activated-potentiated form of antibodies to an intact molecule or a polypeptide fragment of the human cannabinoid receptor of type I.

EFFECT: method ensures the effective correction of endocannabinoid system impairments with the absence of side effects.

4 cl, 1 tbl, 1 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry and represents a combination of leucine source and ω-3 polyunsaturated fatty acid source applicable in therapeutic or preventive treatment of hypercalcemia.

EFFECT: invention provides extending the range of products applicable in the therapeutic or preventive treatment of hypercalcemia.

19 cl, 8 dwg, 2 tbl, 4 ex

FIELD: food industry.

SUBSTANCE: invention relates to food products having prophylactic effect. The fat-binding composition contains an inclusion complex with a host molecule and a guest molecule. The guest molecule is represented by alpha and beta cyclodextrins. The guest compound may be represented by one or more quantities of compounds from the following list: amino acids, vitamins, flavouring substances and their related compounds, rutin, betanin and their derivative compounds and mixtures. The guest molecule is bound to the host molecule weakly and reversibly so that to enable substitution of the guest compound molecule with a fat molecule in a physiological medium, binding of such fat molecule being virtually irreversible. The proposed fat-binding composition may exist, for instance, in the form of a tablet or powder and may be included into the formula of a food product such as beverage. The proposed fat-binding composition (if prepared in the form of a tablet of powder) may optionally include a component providing for carbon dioxide release , with the composition to be dissolved in fizzy carbonated or still water.

EFFECT: proposed fat-binding composition may be used in a method for binding fat consumed by an animal, such method involving the animal consuming the proposed fat-binding composition or a food product or beverage containing it.

17 cl, 3 dwg, 6 tbl, 13 ex

FIELD: medicine.

SUBSTANCE: treating and/or preventing disorders related to overweight and/or obesity, and to methods for preventing or treating disorders related to overweight and/or obesity, including diabetes mellitus is ensured by using a pharmaceutical combination, which contains metformin or its salts, sibutramine or its salts, as well as microcrystalline cellulose in a daily dose as ingredients: sibutramine or its salts 4-17 mg; metformin or its salts 800-2,700 mg; microcrystalline cellulose (25-153.4), or (153.6-158.4), or (158.6-500) mg. The combined use of metformin, sibutramine and microcrystalline cellulose in the declared relations exhibits a synergetic effect, which enables increasing their therapeutic action.

EFFECT: preventive protection and optimisation of treating the patients with overweight or obesity, including type II diabetes mellitus or metabolic syndrome.

6 cl, 2 tbl

FIELD: medicine.

SUBSTANCE: group of inventions relates to medicine, namely to endocrinology, and deals with the treatment of obesity and accompanying metabolic disorders. For this purpose a medication, which contains an activated-potentiated form of antibodies to a human cannabinoid receptor type I, is introduced.

EFFECT: method makes it possible to provide effective weight reduction and correction of metabolic disorders with the absence of side effects.

6 cl, 7 tbl, 4 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to 2-pyridone compounds, represented by general formula [1], , where A represents benzene ring or pyridine ring, X represents structure, represented by general formula [3], V represents single bond or lower alkylene, W represents single bond, ether bond or lower alkylene, which can include ether bond, or their tautomers or stereoisomers.

EFFECT: obtaining pharmaceutically acceptable salts, which possess excellent activating activity with respect to GK and can be applied as medications.

27 cl, 23 tbl, 371 ex

FIELD: medicine.

SUBSTANCE: invention relates to medicine, namely to endocrinology and cardiology, and deals with the treatment of abdominal obesity in case of metabolic syndrome. For this purpose diet therapy in a combination with metformin is used. The diet of a reduced caloric content - 1200 kkal for women and 1500 kkal for men with the restriction of carbohydrate-containing products and fats is administered. The diet includes carbohydrate-containing products with the glycemic index lower than 40. Metformin is introduced in a dose of 850 mg 2 times per day. When an initial body weight reduces by 5% and the weight stabilises for 2 months, the caloric content of food is increased to a calculated value, determined for the patient by formula for calculating the daily caloric content, recommended by WHO with an account of sex, age, height, weight and physical activity. Carbohydrate-containing products with the glycemic index of 40-69 are introduced into the diet until the weight decreases to a specified level. Intake of metformin is continued for 6 months.

EFFECT: diet therapy mode in a combination with metformin provides the effective reduction and long-term stabilisation of weight in a combination with the correction of metabolic disorders.

3 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to a compound of formula (I) or its pharmaceutically acceptable salts of formula (I), wherein X represents O, S; Y represents O, S; R1 independently represents H, alkyl; G1 represents ethyl; each G2 and G3 are independently specified in H, alkyl, trifluoromethyl, halogen, nitro, amido, cyano and tetrazolyl. The invention also refers to a pharmaceutical composition possessing activating action on peroxisome proliferator activated receptors subtype α, subtype δ and subtype γ and containing an effective amount of the compound of formula (I) or its pharmaceutically acceptable salts. The compounds of formula (I) are applicable for treating or producing a drug preparation for treating or preventing the diseases associated with peroxisome proliferator activated receptors subtype α, subtype δ and subtype γ. The compounds of formula (I) are produced by a reaction of the compound of formula (III) and the compound of formula (IV) when heated in acetonitrile under reflux in the presence of potassium carbonate to produce the compound of formula (II), to saponify the compound of formula (II) in alcoholic solution in the presence of alkali and to acidify the reaction mixture to produce the compound of formula (I). X, Y, R1, G1, G2 and G3 have the above values; R3 represents a leaving group specified in OH, Cl, Br, I, OTs, OMs.

EFFECT: compounds of phenylpropionic acid possessing the activating action on peroxisome proliferator activated receptors (PPARα, δ, γ).

15 cl, 2 ex

FIELD: medicine.

SUBSTANCE: invention represents a method for the inhibition of adipogenesis, which involves a stage, whereat adipocytes are placed into contact with an effective amount of Calebin-A.

EFFECT: extending the range of anti-obesity products.

14 cl, 3 ex, 3 tbl, 7 dwg

FIELD: chemistry.

SUBSTANCE: invention refers to gene engineering, more specifically to producing the peptide GLP-1, modified by an oligosaccharide chain, and can be used in medicine for treating or preventing diseases associated with GLP-1. In the peptide GLP-1 with SEQ ID NO: 2 or SEQ ID NO: 3 two amino acid peptides are substituted by an amino acid modified by a complex bi-antennal oligosaccharide chain, and wherein each of the centres is specified in a group consisting of positions 18, 22, 26, 30, 34 and 36 in the peptide GLP-1 with SEQ ID NO: 2 or SEQ ID NO: 3. The above modified peptide GLP-1 can involve the deletion, substitution or attachment of 1-5 amino acids, except for the amino acids modified by the oligosaccharide chain.

EFFECT: invention enables producing the peptide GLP-1 modified by the oligosaccharide chain, which shows the stronger activity of blood glucose suppression and twice increased half lifetime as compared to GLP-1 with SEQ ID NO: 3.

24 cl, 5 dwg, 6 tbl, 16 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: group of inventions refers to medicine and aims at treating fibromyalgia syndrome. The method of treating fibromyalgia syndrome involves administering a therapeutically effective amount of a substance having structural formula , or its pharmaceutically acceptable salt into a mammal in need thereof, wherein Rx, R1 and R2 represent hydrogen and x is equal to 1. What is also provided is a pharmaceutical composition containing the substance having structural formula (1), or its pharmaceutically acceptable salt.

EFFECT: using the group of inventions provide the effective treatment of fibromyalgia syndrome.

13 cl, 1 tbl, 3 ex

FIELD: medicine.

SUBSTANCE: correcting cognitive disorders in the patients suffering arterial hypertension accompanying type 2 diabetes mellitus is ensured by combining a standard drug therapy with administering the preparation Kudesan 60 mg a day throughout two months.

EFFECT: administering Kudesan in the above dose and regimen provides the effective correction of cognitive disorders in the above group of patients in a combination with improving the cardiovascular function and metabolic processes.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: correcting increased levels of anxiety and depression in the patients with arterial hypertension accompanying type 2 diabetes mellitus is ensured by combining a standard drug treatment and administering Kudesan 60 mg a day for two months.

EFFECT: method provides the effective correction of anxiodepressive conditions in the given category of patients that in turn enables normalising blood pressure more effectively by reducing the negative psychosomatic effect.

1 ex, 2 tbl

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to novel compounds of formula I, possessing ability of binding with delta-opioid receptors. In formula R1 is selected from the group, consisting of i) phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxyl, di(C1-4alkyl), aminocarbonyl, chlorine and fluorine, in such a way that only one di(C1-4alkyl)aminocarbonyl is present; ii) naphthyl; iii) pyridinyl, optionally substituted with one substituent, selected from the group, consisting of C1-4alkyl, C1-4alcoxy, C1-4alkylthio, hydroxy, fluorine, chlorine and cyano; iv) pyrimidin-5-yl; v) furanyl; vi) thienyl; vii) 5-oxo-4,5-dihydro-[1,2,4]oxodiazol-3-yl; and viii) di(C1-2alkyl)aminocarbonyl; Y represents ethyl, vinyl or bond; or Y represents O, when R1 represents optionally substituted phenyl, where substituent represents C1-4alcoxy; R2 represents phenyl, optionally substituted with one-two substituents, independently selected from the group, consisting of C1-4alkyl, C1-4alcoxy, fluorine, chlorine and cyano, trifluoromethoxy and hydroxy; or R2 represents phenyl, substituted with one aminocarbonyl, di(C1-4alkyl)aminocarbonyl, C1-4alcoxycarbonyl or carboxysubstituent; R3 is selected from the group, consisting of i) 3-aminocyclohexyl; ii) 4-aminocyclohexyl; iii) piperidin-3-yl; iv) piperidin-4-yl; v) pyrrolodin-2-yl-methyl, in which pyrrolodin-2-yl is optionally substituted by 3-rd or 4-th position with one or two fluorine-substituents; vi) azetidin-3-yl; vii) 2-(N-methylamino)ethyl; viii) 3-hydroxy-2-aminopropyl; ix) piperidin-3-yl-methyl; x) 1-azabicyclo[2.2.2]octan-3-yl; and xi) 8-azabicyclo[3.2.1]octan-3-yl; or R3 together with Ra and nitrogen atom, which they both are bound to, form piperazinyl, optionally substituted with 4-C1-4alkyl; Ra represents hydrogen, 2-(N-methylamino)ethyl or C1-2alkyl, optionally substituted with azetidin-3-yl.

EFFECT: compounds can be used in treatment of pain in the range from medium to strong, caused by diseases or conditions, such as osteoarthritis, migraine, burn, fibromyalgia, cystitis, rhenite, neuropathic pain, idiopathic neuralgia, toothache, etc.

21 cl, 4 tbl, 26 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: what is presented is a group of inventions concerning a new application of bicyclo[2,2,2]octane-2-carboxylic acid salt. What is presented is using it for treating dysphoria in a person suffering epilepsy for treating alcohol addiction, for reducing the level of hepatic function marker specified in AST (aspartate aminotransferase), ALT (alanine aminotransferase) or bilirubin in the person for reducing an erythrocyte sedimentation rate, as well as for reducing a number or an intensity of epileptic attacks in a daily dose of min 400 mg.

EFFECT: implementing the above applications with no negative effect on patient's behaviour and the functions of the main organs and systems.

19 cl, 6 tbl, 2 ex

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I) and their pharmaceutically acceptable salts, wherein A is thiazolyl, oxazolyl, thienyl, furyl, imidazolyl, pyrazolyl or oxadiazolyl (structures of which are presented in cl.1 of the patent claim), R1 represents C1-6alkyl; R2 represents (i) phenyl substituted by halogen; C1-6alkyl optionally substituted by morpholine or C1-6dialkylamino; C1-6alkoxy optionally substituted by halogen; or heterocyclyl, wherein a heterocyclyl substitute is specified in morpholine; pyrazolyl optionally substituted by C1-6alkyl; piperidinyl; pyrrolidinyl; oxadiazolyl substituted by C1-6alkyl; furyl substituted by C1-6alkyl; dioxydoisothiazolidinyl; triazolyl; tetrazolyl substituted by C1-6alkyl, tridiazolyl substituted by C1-6alkyl; thiazolyl substituted by C1-6alkyl; pyridyl; or pyrazinyl; (ii) substituted or unsubstituted heterocyclyl specified in quinolinyl; pyridyl substituted by C1-6alkoxy or morpholinyl; or benzo [d] [1, 2, 3] triazolyl substituted by C1-6alkyl; R3 represents phenyl substituted by 2 or 3 substitutes specified in halogen; C1-6alkyl; C1-6alkoxy optionally substituted by halogen; hydroxy group; cyano; or -C(=O)ORa, wherein Ra represents phenyl; R4 represents hydrogen, C1-6alkyl or C1-6halogenalkyl. The invention also refers to a pharmaceutical composition containing the compounds of formula (I), a method for PDE10 inhibition, a method of treating neurological disorders, and to intermediate compounds: 2-(4-chlor-3,5-dimethoxyphenyl)furan and 4-(5-methyl-1,3,4-thiadiazol-2-yl)benzaldehyde.

EFFECT: compounds of formula (I) as PDE10 inhibitors.

39 cl, 13 ex, 2 tbl, 77 dwg

FIELD: medicine.

SUBSTANCE: correcting night eating syndrome in the patients with anxiety and depressive disorders is ensured by prescribing agomelatine 25mg a day for the night. The therapeutic course is continued until a long-lasting remission is observed for 6 months and more.

EFFECT: method enables reducing the intensity of night eating syndrome in the patients with an affective pathology by levelling the anxiety and depressive manifestations with improving the sleep quality and minimum side effects.

2 tbl, 2 ex

FIELD: chemistry.

SUBSTANCE: invention relates to 2-bromo-1-(thietanyl-3)imidazole-4,5-dicarboxylic acid derivatives of formula Ia, b where R is COOK (Ia) or (Ib)

EFFECT: obtaining novel heterocyclic compounds having antidepressant activity.

4 cl, 1 tbl, 5 ex

Antidepressant // 2535027

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention relates to medicine, namely to pharmacology, and deals with a synthetic biologically active compound - hydrochloride of 2-(diethylamino)ethyl ether of 9-hydroxy-9H-fluorene carboxylic acid, representing an amyzilum M-cholinoblocker derivative. The said amyzilum derivative has not been described before. The claimed compound possesses low toxicity, its synthesis is simple and available. It is demonstrated that hydrochloride of 2-(diethylamino)ethyl ether of 9-hydroxy-9H-fluorene carboxylic acid, representing the amyzilum M-cholinoblocker derivative demonstrates an expressed antidepressant activity and an anxiolytic action, possesses a sedative, and in high doses a soporific effect, it also positively influences an exploratory ability and memory. In addition, it has been stated that the claimed pharmacological substance in expressiveness of the antidepressant properties surpasses the widely applied tricyclic antidepressant amitriptylinum. The obtained data make it possible to recommend the claimed amyzilum derivative as the antidepressant for the treatment of depression and anxiety disorders.

EFFECT: invention extends an arsenal of pharmacological means, used as depression therapy.

4 tbl

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