RussianPatents.com

Alkyl sulphonamide quinolines with affinity to nk-3 receptors. RU patent 2421447.

FIELD: chemistry.

SUBSTANCE: compound is ((S)-1-phenyl-propyl)-amide 3-(methane sulphonyl amino)-2-phenyl- quinoline-4-carboxylic acid, stereoisomer, enantiomer or pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition based on the disclosed compound.

EFFECT: novel derivative of methyl sulphonamide quinoline which can be used to modulate the NK-3 receptor.

2 cl, 10 ex

IPC classes for russian patent Alkyl sulphonamide quinolines with affinity to nk-3 receptors. RU patent 2421447. (RU 2421447):

C07D215/52 - with aryl radicals attached in position 2

A61P35 - Antineoplastic agents

A61P3/04 - Anorexiants; Antiobesity agents

A61P25/28 - for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

A61P25/24 - Antidepressants

A61P25/22 - Anxiolytics

A61P25/18 - Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia

A61K31/47 - Quinolines; Isoquinolines

Another patents in same IPC classes:

Application of single dose of cd20-specific binding molecules / 2421242
Invention refers to medicine, namely to arthrology, rheumatology, and can be used for treating rheumatoid arthritis. That is ensured by introducing human CD20 specific small modular immune-pharmaceutical (SMIP) protein in a therapeutically effective amount to the patient. The introduction is single, and the supporting treatment is not performed for approximately three months to two years after the introduction of a first single dose.

Cancer therapy by combination of taxanes and 13-deoxyantracyclines / 2421224
Invention refers drugs, and concerns an anticancer composition containing: a) a therapeutically effective amount of 13-deoxyantracycline of formula specified below and b) a therapeutically effective amount of taxane. Also, there are disclosed pharmaceutical formulation and cancer therapy involving the introduction of the therapeutically effective amount of 13-deoxyantracycline and the therapeutically effective amount of taxane.

Method of differentiated treatment of diffuse large b-cell lymphosarcomas of lymphoid organs in adults / 2421217
Invention refers to medicine, namely to oncohematology and can be used for treatment of diffuse large B-cell lymphosarcomas (DLBCL) of lymphoid organs in adults. The method involves pre-phase chemotherapy of sequential 6-fold block radical chemotherapy A-B-A-B-C-A or A-B-A-B-A-B. The block A is performed by the intravenous introduction of: methotrexate 1500 mg/m2 and vincristine 2 mg on the 1st day, doxorubicine 25 mg/m2 on the 1st and 2nd days, vepezide 100 mg/m2 and cytosar 150 mg/m2 on the 4th and 5th days only, and iphosphamide 800 mg/m2 intravenously, dexamethasone 20 mg in tablets on the 1-5th days. Further, the block B follows by the intravenous introduction of: methotrexate 1500 mg/m2 and vincristine 2 mg on the 1st day, doxorubicine 25 mg/m2 on the 4th and 5th days only, cyclophosphan 200 mg/m2 and dexamethasone 20 mg in tablets on the 1-5th days, then another 2 blocks A and B follow. In the presence of a complete remission, another 2 blocks A-B are required, and in the absence thereof, the block C is performed by the intravenous introduction: methotrexate 1500 mg/m2 and vinblastine 10 mg on the 1st day, cytosar 2000 mg/m2 2 times a day on the 2nd and 3rd days, vepezide 150 mg/m2 on the 3rd, 4th and 5th days, dexamethasone 20 mg in tablets on the 1-5th days, and then in the presence of the complete remission, the block A is performed. The therapeutic course is 4.5-5 months, every 21 days.

Fused proteins binding immunoglobulin domain / 2420537
Offered is a fused protein containing from an amino-terminus to carboxyl terminus: binding domain polypeptide which is bound with a biological target molecule; human one-cysteine "link" region IgGl peptide; immunoglobulin heavy chain CH2 constant region polypeptide and immunoglobulin heavy chain CH3 constant region polypeptide. The fused protein represents mixed monomers and dimers, has ADCC, CDC or both cytotoxicities. Also, described are a pharmaceutical composition and a method of treating a B-cell disorder with using the fused protein.

Pyrazolopyrimidine derivative / 2420530
Invention refers to a compound presented by formula (1), to its salt or hydrate where in formula R1 represents a methylene group, R2 represents a phenyl group which can contain a substitute(s), or a heterocyclic group which can contain a substitute(s), the cycle A represents a 6- or 7-members cycle (where cycle-making atoms of the cycle A different from a sulfur atom in position 6 are carbon atoms), and R3 represents a hydrogen atom, or 1-3 equal or different substitutes used to substitute the cycle A where the possible substitutes are specified in clause 1 of the patent claim. Also, the invention refers to a pharmaceutical composition exhibiting an anticancer activity, on the basis of the compound presented by formula (1).

New histone deacetylase inhibitor class / 2420522
Invention refers to a compound of formula (I) where Q represents a bond, CH-NR3 R4, NR5 or oxygen atom; X represents CH or nitrogen atom; Y represents a bond, CH2, oxygen atom or NR6; Z represents CH or nitrogen atom; R1, R2 represent, independently, hydrogen, halogen; R3, R4 represent, independently, hydrogen, (C1-C6)-alkyl; R5 represents hydrogen, (C1-C6)-alkyl, (CO)R7, SO2- (C1-C6)-alkyl or benzyl; R6 represents hydrogen, (C1-C6)-alkyl; R7 represents (C1-C6)-alkyl, phenyl, benzyl, OR8 or NR9R10; R8 represents (C1-C6)-alkyl; R9 represents hydrogen, (C1-C6)-alkyl; R9 represents hydrogen, (C1-C6)-alkyl; R11, R12 represent, independently, hydrogen or (C1-C6)-alkyl; and to their pharmaceutically acceptable salts; provided when X represents nitrogen atom, Y cannot represent oxygen atom or NR6; and except for the compounds (E)-N-hydroxy-3-(4-{(E)-3-[4-(4-methylpiperazine-1-yl)phenyl]-3-oxopropenyl}phenyl) acrylamide; (E)-N-hydroxy-3-{4-[(E)-3-(4-moropholine-4-ylphenyl)-3-oxopropenyl] phenyl}acrylamide; (E)-3-(3-flour-4-[(E)-3-(4-morpholine-4-ylphenyl)-3-oxopropenyl]phenyl}-N-hydroxyacrylamide. Also, the invention refers to a method for producing the compounds of formula (I), to a pharmaceutical composition, as well as to application of one or more compounds of formula (I), (la), (lb), (Ic).

Method of treating recurrent nasopharynx cancer / 2420333
Invention refers to medicine, namely to oncology, and can be used for treating patients with recurrent nasopharynx cancer. The method involves administration of chemopreparations and gamma-ray teletherapy; the first therapeutic day involves intravenous drop infusion of an automyelosuspension ex temporae incubated with cisplatin at 50 mg/m2 with underlying excessive hydration and forced diuresis; 5-fluorouracil dissolved in normal saline 200 ml is infused the same day at 500 mg/m2. After one day of a pause, gamma-ray teletherapy is performed in a hyperfractionation mode taking into account a residual dose 1.5 Gy of single basic dose twice a day every 5 hours to at 5 o'clock to 65 isoGy of total basic dose. After one week of a pause, the second course of automyelochemotherapy with cisplatin at 100 mg/m2 with underlying excessive hydration and forced diuresis is performed; 5-fluorouracil 500 mg/m2, bleomycine 30 mg/m2 and adriamycin 35 mg/m2 are infused the same day.

Photosensitiser activation method / 2420330
Invention refers to medicine, to a photosensitiser activation method involving selection of photosensitising catalyst nanoparticles from a heterocrystalline mineral capable to catalyse the active oxygen generation, and optical irradiation, particularly infrared, of the nanoparticles. The photosensitiser can be chemically bound with a DNA molecule, or with an acceptable antimetabolic agent.

Method of treating breast cancer / 2420328
Invention refers to medicine, oncology, and can be used in complex treatment of malignant breast tumours. Patient's blood is sampled from a peripheral vein in two containers, 100 ml in each; inductors of an apparatus for physical therapy are placed oppositely on each side of a connector tube of a dropper to expose simultaneously to red light of wave length 670 nm, dose 1-5 J/cm2 and field density 5 mT, frequency 0.3 Hz for 3 minutes. Doxorubicin 50 mg is added to the first container, while Methotrexate 25 mg, cyclopohsphane 600 mg, 5-fluorouracil 750 mg are added to the second container; the contents of the containers is incubated for 40 minutes at temperature 37°C and introduced in the patient on the 1st and 8th days of treatment. On the 3rd, 5th, 10th, 12th and 15th days of treatment, 5-fluorouracil 500 mg mixed with autoblood and incubated as described above is introduced. In 14 days after the last introduction of mixed autoblood and chemopreparation, the therapeutic modalities are repeated in the same order, doses and processing.

Stabilised il-21 compositions / 2420308
Invention relates to medicine and pharmacology and represents pharmaceutical composition, which possesses IL-21 activity, containing IL-21 and sulfate, where IL-21 sequence is selected from the group consisting of SEQ ID No: 1, amino acids from No 30 to No 162 sequence SEQ ID No:1, SEQ ID No:2 and version of any of them, which has identity degree, at least, 80%, and sulfate represents sulfate-ions (SO4 2-) in concentration from 10 mM to 150 mM.

Peptide composition containing propylene glycol optimal for manufacturing and application in injection devices / 2421238
Invention refers to medicine, namely to pharmaceutical compositions containing a peptide and propylene glycol, to methods of preparing such compositions, and also concerns methods of reducing contamination of injection devices by a peptide composition and reducing sediment formation in the production equipment during manufacturing of the peptide composition. The agonist GLP-1 is used as said peptide in the composition.

Oxime derivatives and preparation thereof / 2420525
In formula (I) , the ring A represents 6-members aryl or 5-6-members heteroaryl containing 1-2 heteroatoms selected from nitrogen and sulphur; Q means C3-8 cycloalkyl, 5-6-members heterocycle containing 1 heteroatom selected from oxygen, nitrogen or sulphur, C1-6 alkyl or C2-6 alkenyl; the ring T represents 5, 6, 9 or 10-members heteroaryl or 9-members heterocycle optionally additionally substituted by 1-3 heteroatoms independently selected from nitrogen or sulphur. The values of other substitutes are specified in the patent claim. Also, the invention refers to methods for preparing oxime derivatives of general formula (I), to pharmaceutical compositions containing the compound of the invention as an active ingredient and to applications of the compounds of the invention in preparing a drug.

Compound for treating lipase-mediated diseases / 2420513
Invention relates to novel compounds - benzoquinone derivatives of formula (I): , where each of R1 and R2 is O-C(O)phenyl; where the phenyl is substituted with 1 substitute selected from halide, nitro, C1-C6 alkyl or C1-C6 alkoxy, and pharmaceutically acceptable salts thereof.

Preparations for treating adipose tissue, skin tissue and disorders, and muscular tissue / 2420317
There are offered a prolonged release composition for regional depot fat reduction containing a therapeutically effective amount of at least one glucocorticosteroid in the form of a crystalline microparticle suspension, and a therapeutically effective amount of at least one selective beta-2-adrenergic receptor agonist and a respective combined preparation of the same purpose.

Mammal body weight reduction method / 2420211
Invention relates to therapy and prevention of obesity and may be used for reduction of body weight with both humans and animals. The mammal body weight reduction method envisages addition of a biologically active substances concentrate produced of aspen wood by way of water extraction to the basic ration. For mice the food additive efficient quantity is 0.43-1.71 mg of dry substance of the aspen biologically active substances concentrate (administered daily in two separate doses during a month) per 1 g of live weight. For humans the food additive efficient quantity is 3.6 mg of dry aspen biologically active substances concentrate (administered daily in two separate doses during a month).

Dpp-iv inhibitor containing beta amino group, method for making thereof and pharmaceutical composition containing it for prevention and treatment of diabetes or obesity / 2419615
Invention refers to a compound of formula

Novel piperidine derivatives / 2417985
Invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts thereof where R1 and R2 together denote a group selected form groups of formula (III-1): , where R9 denotes 1) a lower alkyl group, optionally substituted with a halogen atom or lower alkoxy group, 2) an aryl group, 3) an aralkyl group, 4) a heteroarylalkyl group, 5) a heteroaryl group, where the aryl, aralkyl, heteroarylalkyl and heteroaryl groups can be substituted with a halogen atom, lower alkyl group, optionally substituted with a lower alkoxy group or 1-3 halogen atoms, lower alkoxy group, optionally substituted with 1-3 halogen atoms, cyano group, hydroxy group, alkylsulphonyl group, cycloalkylsulphonyl group, aryl group, heteroaryl group, alkylaminocarbonyl group, alkanoyl amino group, alkyl amino group or dialkylamino group; R10 denotes a lower alkyl group, optionally substituted with 1-3 halogen atoms, or a lower alkylsulphonyl group; X9-X12 denotes a carbon atom or a nitrogen atom, where the carbon atom can be independently substituted with a lower alkyl group, optionally substituted with a halogen atom or a lower alkoxy group, lower alkoxy group, optionally substituted with a halogen atom, or a cyano group or a halogen atom; R3 denotes a) a group of formula (II-1): (ii-U where R4 and R5, taken together with a nitrogen atom, form a 5- or 6-member monocyclic ring, where the monocyclic ring may contain a substitute in form of a lower alkyl group, m1 equals 3; or b) a group of formula (II-2): , where R6 denotes a lower alkyl group or cycloalkyl group; m2 equals 1 or 2; X1-X4 all denote carbon atoms, or one of X1-X4 denotes a nitrogen atom and the rest denote carbon atoms; and where "heteroaryl" in each case relates to a 5- or 6-member aromatic ring containing 1-3 heteroatoms selected from a nitrogen atom, oxygen atom and a sulphur atom. The invention also relates to a histamine H3 receptor antagonist or inverse agonist, as well as a preventive or medicinal agent.

Azaindole-2-carboxamide derivatives / 2417226
Invention refers to compounds of formula (I) where R1 is chosen from a group consisting of phenyl, unsubstituted or substituted by one or two groups independently chosen from (lower) alkyl, (lower) phenylalkyl wherein a phenyl ring can be unsubstituted or substituted by one or two groups independently chosen from halogen; R2 represents hydrogen; or R1 and R2 together with nitrogen atom whereto attached, form a saturated 5- or 6-members heterocyclic ring optionally containing an additional oxygen heteroatom, said saturated heterocyclic ring is unsubstituted or substituted by one, two or three groups independently chosen from (lower) alkyl, halogen; R3 is chosen from a group consisting of hydrogen, (lower) alkyl, (lower) hydroxyalkyl, (lower) alkoxyalkyl, (lower) haloalkyl, (lower) cycloalkylalkyl, (lower) cyanoalkyl, (lower) alkylsulfonyl, phenyl unsubstituted or substituted by one or two groups independently chosen from halogen; R4 represents hydrogen or halogen; R5 represents a group chosen from where m represents 0 or 1; n represents 0,1 or 2; X represents CR13R13'; R6, R6', R7, R7', R8,R8', R13, R13' are independently chosen from a group consisting of hydrogen, (lower) alkyl, halogen; p represents 0 or 1; R9 is chosen from (lower) alkyl, cycloalkyl, (lower) cycloalkylalkyl; q represents 0 or 1; R10 represents (lower) alkyl; and to their pharmaceutically acceptable salts, as well as to a pharmaceutical composition exhibiting histamine 3 receptor antagonistic and/or antagonistic activity and based on the compounds of formula I.

Heteroarylbenzamide derivatives applied as glk activators in diabetes treatment / 2415141
Invention refers to the compound 3-{[5-(azetidine-1-ylcarbonyl)pyrazine-2-yl] oxy}-5-{[(1S)-1-methyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazine-5-yl)benzamide or to its pharmaceutically acceptable salt. Also, it refers to a pharmaceutical composition for treating insulin-independent diabetes or obesity containing said compound.

Application of nutrient compositions with phospholipids, sphingolipids and cholesterol / 2414905
Claimed are: nutrient composition, which contains 0.5-20 wt % of phospholipids, 0.1-20 wt % of sphingolipids and 0.005-10 wt % of cholesterol from total lipid content, protein and carbohydrates, intended for child form 36 months for prevention of obesity and/or diabetes, its application for treatment of type two diabetes and/or nutrient regulation of type two diabetes, as well as its application for prevention of disorder development, when age of mentioned child exceeds 36 months, said disorder is selected from group, which consists of type two diabetes, hyperglycemia at starvation, insulin immunity, visceral obesity, hyper-insulinemia, hypertension, cardiovascular diseases, cerebral vessel diseases, arthrosclerosis, dislipidemia, hyperuricemia, fatty liver dystrophy and sleep apnea.

Aryl-izoxazole-4-yl-imidazo[1,5-a]pyridine derivatives / 2420527
Invention refers to aryl-izoxazole-4-yl-imidazo[1,5-a]pyridine derivatives of formula I and to their pharmaceutically acceptable acid addition salts. In formula I , R1 represents hydrogen atom; R2 represents hydrogen atom; R3 represents hydrogen atom, cyano or -(CO)-Ra; Ra represents lower alkoxy or NR'R" where each of R' and R" independently represents hydrogen atom, 6-members heterocycloalkyl with the 1st heteroatom selected from O, or lower alkyl substituted by C3-C7-cycloalkyl. The invention also refers to a drug exhibiting affinity and selectivity to GABA(A) α5-receptor binding sites, containing one or more compounds of formula I and to an application of the compound of the invention in producing the drug exhibiting affinity and selectivity to GABA(A) α5-receptor binding sites.