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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 47820. Отображено 100.
05-01-2012 дата публикации

Modulators of cytokine mediated signalling pathways and integrin alphavbeta3 receptor antagonists for combination therapy

Номер: US20120003229A1
Автор: Hervé Geneste, Wilfried Hornberger
Принадлежит: Individual

The invention relates to the use of modulators of cytokine mediated signalling pathways in combination with integrin αvβ3 receptor antagonists for the treatment or prevention of diseases, particularly to the use of a pharmaceutical composition, comprising a modulator of cytokine mediated signalling pathways and an integrin αvβ3 receptor antagonist, for the treatment or prevention of inflammatory or autoimmune disorders, particularly for the treatment or prevention of rheumatoid arthritis and to the pharmaceutical composition itself.

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Номер записи: 1
05-01-2012 дата публикации

Pharmaceutical compositions of dextran polymer derivatives

Номер: US20120003282A1
Автор: Corey J. Bloom, Daniel E. Dobry, Daniel T. Smithey, David K. Lyon, David T. Vodak, Dwayne T. Friesen, Michael M. Morgen, Warren K. Miller
Принадлежит: Bend Research Inc

Pharmaceutical compositions are provided comprising an active agent and a dextran polymer derivative. The compositions include from 0.01 to 99 wt % of an active agent and from 1 to 99.99 wt % of a dextran polymer derivative. The dextran polymer derivative is selected from dextran acetate, dextran propionate, dextran succinate, dextran acetate propionate, dextran acetate succinate, dextran propionate succinate, dextran acetate propionate succinate, and mixtures thereof.

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Номер записи: 2
05-01-2012 дата публикации

Nanobead releasing medical devices

Номер: US20120003291A1
Автор: Charles H. Craig, Dennis Orosa, Dudley Jayasinghe, John E. Papp, Lionel G. Hines
Принадлежит: Abbott Cardiovascular Systems Inc

Medical devices comprising nanobeads encapsulating one or more bioactive agents and methods of use thereof are provided.

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Номер записи: 3
05-01-2012 дата публикации

Pharmaceutical Composition Comprising Aliskiren

Номер: US20120003308A1
Автор: Hong Wen, Shoufeng Li, Sonali Bose
Принадлежит: Individual

The invention provides a pharmaceutical oral fixed dose combination of aliskiren and valsartan. It provides compressed bilayer tablets with both a high drug load and suitable physical properties, which can be produced using conventional equipment.

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Номер записи: 4
05-01-2012 дата публикации

Unit doses, aerosols, kits, and methods for treating heart conditions by pulmonary administration

Номер: US20120003318A1
Автор: Carlos A. Schuler, Rangachari Narasimhan
Принадлежит: Incarda Therapeutics Inc

Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.

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Номер записи: 5
12-01-2012 дата публикации

Biomarkers for myocardial ischemia

Номер: US20120009174A1
Автор: Jennifer Van Eyk, QIN Fu, Simon Sheng
Принадлежит: JOHNS HOPKINS UNIVERSITY

This invention relates, e.g., to a method for determining if a subject has myocardial ischemia, comprising (a) providing a blood sample obtained from a subject suspected of having myocardial ischemia; (b) determining in the sample the amount of one or more of the following proteins: (i) Lumican and/or (ii) Extracellular matrix protein 1 and/or (iii) Carboxypeptidase N; and (c) comparing the amount(s) of the protein(s) to a baseline value that is indicative of the amount of the protein in a subject that does not have myocardial ischemia, wherein a statistically significantly increased amount of the protein(s) compared to the baseline value is indicative of myocardial ischemia. Other proteins indicative of myocardial ischemia are also described, as are methods for treating a subject based on a diagnostic procedure of the invention, and kits for carrying out a method of the invention.

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Номер записи: 6
19-01-2012 дата публикации

Kallikrein-inhibitor therapies

Номер: US20120015881A1
Автор: Anthony Williams, Arthur C. Ley, Luigi Bergamaschini, Maria Grazia De Simoni, Robert C. Ladner, Shirish Hirani
Принадлежит: Dyax Corp

Methods are described for preventing or reducing ischemia, e.g., cerebral ischemia, and/or reperfusion injury, e.g., reperfusion injury associated with cerebral ischemia, in a patient.

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Номер записи: 7
19-01-2012 дата публикации

Novel compounds as cannabinoid receptor ligands

Номер: US20120015929A1
Автор: Arturo Perez Medrano, Jennifer M. Frost, Karin Rose Marie Tietje, Meena V. Patel, Sridhar Peddi, Steven P. Latshaw, Teodozyj Kolasa, William A. Carroll, Xueqing Wang
Принадлежит: ABBOTT LABORATORIES

Disclosed herein are compounds of formula (I) wherein R 1 , R 2 , R 3 , R 25a , R 26a , X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.

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Номер записи: 8
26-01-2012 дата публикации

Compositions and methods for the treatment of pathological condition(s) related to gpr35 and/or gpr35-herg complex

Номер: US20120022116A1
Автор: Haibei Hu, Haiyan Sun, Huayun Deng, Mingqian He, Weijun Niu, YE Fang
Принадлежит: Corning Inc

Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject. The compounds having a formula (I), (II) or (III):

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Номер записи: 9
26-01-2012 дата публикации

Use of aminaphtone for the preparation of a medicament for treating arteriopathies

Номер: US20120022155A1
Автор: Raffaella Scorza
Принадлежит: Fondazione IRCCS Ca Granda Ospedale Maggiore Policlinico

The subject of the present invention is the use of aminaphtone for the preparation of a medicament for treating arteriophaties, in particular arteriophaties of a degenerative inflammatory type. Preferably, said medicament is formulated for oral administration

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Номер записи: 10
02-02-2012 дата публикации

Novel compound having 3-heteroarylpyrimidin-4-(3h)-one structure and pharmaceutical preparation containing same

Номер: US20120028983A1
Автор: Gen Watanabe, Hitomi Aoki, Junya Tagashira, Kazuhiro Onogi, Rie Ishida, Ryohei Sekimoto, Seiichi Sato, Tadaaki Ohgiya, Toru Miura
Принадлежит: Kowa Co Ltd

Disclosed is a compound which has both an angiotensin-II receptor antagonistic activity and a PPARγ activation activity and is useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, angina pectoris, cerebrovascular disorders, cerebral circulatory disorders, ischemic peripheral circulatory disorders, renal diseases, arteriosclerosis, inflammatory diseases, type-2 diabetes, diabetic complications, insulin resistance syndrome, syndrome X, metabolic syndrome and hyperinsulinemia. [In the formula, A represents a 5- to 10-membered heteroaryl group; R 1 and R 2 independently represent a C 1-6 alkyl group; and each of R 3 to R 5 is absent or represents H, a halogen atom, OH, NO 2 , a halo-C 1-6 alkyl group, a (substituted) C 1-6 alkoxy group, a (substituted) C 3-6 cycloalkyloxy group, or a 5- to 10-membered heteroaryl group.]

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Номер записи: 11
09-02-2012 дата публикации

Reduced-cholesterol dairy product for use as a medicament

Номер: US20120034308A1
Автор: Daniel Dalemans
Принадлежит: Corman SA

A ruminant reduced-cholesterol dairy product is used as a medicament.

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Номер записи: 12
16-02-2012 дата публикации

Identification of novel antagonist toxins of t-type calcium channel for analgesic purposes

Номер: US20120040909A1
Автор: Emmanuel Bourinet, Fabrice Marger, Joël Nargeot, Michel Lazdunski, Pierre Escoubas
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite de Nice Sophia Antipolis UNSA

A peptide with the following sequence YCQKFLWTCDSERPCCEGLVCRLWCKIN (SEQ ID NO 1) or a derivative thereof, and nucleic acids coding for the peptide having the sequence (SEQ ID NO 1). Also the use of this peptide as an antagonist and/or reverse agonist of T-type calcium channels. A use of the peptide for preparing a drug, in particular an analgesic one.

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Номер записи: 13
23-02-2012 дата публикации

Crystalization of pharmaceutical compounds

Номер: US20120046297A1
Автор: David R. Weyna, Mazen Hanna, Miranda L. Cheney, Ning SHAN
Принадлежит: Thar Pharmaceuticals Inc

Novel crystalline forms of tadalafil suitable for pharmaceutical compositions in drug delivery systems for humans.

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Номер записи: 14
23-02-2012 дата публикации

Coating Comprising An Elastin-Based Copolymer

Номер: US20120046640A1
Автор: Lothar W. Kleiner, Syed F.A. Hossainy, Yiwen Tang
Принадлежит: Abbott Cardiovascular Systems Inc

The present invention is directed to medical devices including coatings. The coatings include a topcoat which includes a copolymer comprising a block of an elastin pentapeptide. The topcoat is over a layer of poly(vinyl alcohol) on a hydrophobic coating or over a porous coating comprising pores or depots that include a bioactive agent.

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Номер записи: 15
08-03-2012 дата публикации

Modulation of drug release rate from electrospun fibers

Номер: US20120058100A1
Автор: Jay C. Sy, V. Prasad Shastri
Принадлежит: Individual

Disclosed are co-electrospun polymeric fibers comprising polymers comprising pharmaceutically active agents and/or biologically active agents and capable of release at a combined release rate. Also disclosed are processes for preparing polymeric fibers capable of release at a combined release rate. Also disclosed are processes of modulating delivery rate of pharmaceutically active agents and/or biologically active agents. Also disclosed are processes of delivering pharmaceutically active agents and/or biologically active agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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Номер записи: 16
15-03-2012 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20120065408A1
Автор: Bertrand M.C. Plouvier, Doug Ta Hung Chou, Grace Jung, James Gee Ken Yee
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

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Номер записи: 17
22-03-2012 дата публикации

Use of g-csf for the extension of the therapeutic time-window of thrombolytic stroke therapy

Номер: US20120070403A1
Автор: Armin Schneider, Marc Fisher
Принадлежит: Sygnis Bioscience GmbH and Co KG

The present invention relates to the use of G-CSF and derivatives thereof for extending the therapeutic window of subsequent thrombolytic treatment of acute stroke, and thereby, allowing the diagnostic examinations which are necessary prior to the thrombolytic treatment in order to avoid hemorrhagic and other severe adverse side effects of the thrombolysis.

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Номер записи: 18
22-03-2012 дата публикации

Composition containing a bean extract for improving blood circulation and increasing vascular health

Номер: US20120070520A1
Автор: Chae Wook Kim, Dae-Bang Seo, Hyun Jung Shin, Jin Kwan Kim, Kyung Mi Joo, Kyung Min Lim, Sang Jun Lee, Yeon Su Jeong, Young-Ho Park, Yung Hyup Joo
Принадлежит: Amorepacific Corp

The present invention relates to a composition containing a bean extract extracted by low-concentration, low-grade alcohol or fractions thereof. The composition exhibits excellent effects in improving blood circulation, improving obesity, and preventing diabetes, hyperlipidemia and the like, and exhibits the effects of alleviating or treating the symptoms of diabetes, hyperlipidemia, and the like. The present invention also relates to a method for improving blood circulation and vascular health.

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Номер записи: 19
29-03-2012 дата публикации

Antibodies to troponin i and methods of use thereof

Номер: US20120076803A1
Автор: Bailin Tu, Dagang Huang, Joan D. Tyner, Lowell J. Tyner, Robert N. Ziemann, Susan E. Brophy
Принадлежит: ABBOTT LABORATORIES

The subject invention relates to antibodies to troponin I as well as methods of use thereof. In particular, such antibodies may be used to detect Troponin I in a patient and may also be used in the diagnosis of, for example, a myocardial infarction or acute coronary syndrome.

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Номер записи: 20
29-03-2012 дата публикации

Chemical compounds

Номер: US20120077828A1
Автор: Dirk A. Heerding, Jeffrey Michael Axten, Jesus Raul Medina, JUN TANG, Seth Wilson Grant, Stuart Paul Romeril
Принадлежит: GlaxoSmithKline LLC

The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R 1 , R 2 , and R 3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

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Номер записи: 21
29-03-2012 дата публикации

Method For Improved Bioactivation Of Pharmaceuticals

Номер: US20120077876A1
Автор: Bernd Clement, Dennis Schade
Принадлежит: Dritte Patentportfolio Beteiligungs GmbH and Co KG

This invention relates to a prodrug comprising a partial structure having the general formula (I) or (II), where R 1 and R 2 are hydrogen, alkyl, or aryl radicals.

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Номер записи: 22
05-04-2012 дата публикации

Stabilized alpha helical peptides and uses thereof

Номер: US20120082636A1
Автор: Gregory Verdine, Loren D. Walensky, Stanley J. Korsmeyer, Susan Korsmeyer
Принадлежит: Individual

Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.

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Номер записи: 23
12-04-2012 дата публикации

Acetylsalicylic acid salts

Номер: US20120088742A1
Автор: Anatolijs Birmans, Anatolijs Misnovs, Antons Lebedevs, Ivars Kalvins, Maris Veveris
Принадлежит: Tetra Sia

Novel betaine salts of acetylsalicylic acid, namely 4-trimethylammoniobutanoate acetylsalicylic acid addition salt (gamma-butyrobetaine acetylsalicylate), L-carnitine acetylsalicylic acid addition salt and 3-(trimethylammonioamino)propanoate (meldonium) acetylsalicylic acid addition salt. Use of meldonium acetylsalicylate as antiplatelet agent for treating various pathologies induced by platelet aggregation, anti-inflammatory and antihyperlipidemic agent.

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Номер записи: 24
12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Автор: Cullen L. Cavallaro, Gregory S. Bisacchi, James R. Corte, Joanne M. Smallheer, Jon J. Hangeland, Karen A. Rossi, Mimi L. Quan, Todd J. Friends, Zhong Sun
Принадлежит: Bristol Myers Squibb Co

The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R 3 , R 4 , R 6 , R 11 , X 1 , X 2 , and X 3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

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Номер записи: 25
19-04-2012 дата публикации

Neutrophil-depleted platelet rich plasma formulations for cardiac treatments

Номер: US20120093941A1
Автор: Allan Kumar Mishra
Принадлежит: Allan Kumar Mishra

Compositions and methods for preparing neutrophil-depleted platelet rich plasma are provided. Generally, these compositions comprise a higher concentration of platelets and depressed concentrations of neutrophils relative to whole blood although white blood cells may be at higher concentrations than whole blood. The concentrations of the platelets and/or the white blood cells may be two to eight times the respective concentrations in whole blood. These compositions may have depressed concentrations of red blood cells and hemoglobin. In some variations, the compositions may be useful to treat damaged connective tissue and/or to slow or stop cardiac apoptosis after a heart attack. The neutrophil-depleted platelet rich plasma composition may be delivered in conjunction with reperfusion therapy.

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Номер записи: 26
26-04-2012 дата публикации

Methods of providing anticoagulation effects in subjects

Номер: US20120101169A1
Автор: Amale Hawi
Принадлежит: Penwest Pharmaceuticals Co

The present invention is directed to methods of providing anticoagulation effects in subjects in need thereof, comprising administering to the subjects at least twice a day compounds of the present invention, stereoisomers, and racemates thereof.

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Номер записи: 27
03-05-2012 дата публикации

Method of Inhibiting Smooth Muscle Cell Proliferation by Using Reconstituted HDL

Номер: US20120108495A1
Автор: Bok Soo Lee, Jeong Euy Park, Ki Yong Kim
Принадлежит: Green Cross Corp Korea, SAMSUNG LIFE PUBLIC WELFARE FOUNDATION

A method of inhibiting smooth muscle cell proliferation comprising administering to a subject a pharmaceutical composition including reconstituted HDL as an active ingredient.

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Номер записи: 28
03-05-2012 дата публикации

Agents and methods for denervation

Номер: US20120108517A1
Автор: Emily A. STEIN, Kondapavulur T. Venkateswara-Rao, Michael A. Evans
Принадлежит: Evans Michael A, Stein Emily A, Venkateswara-Rao Kondapavulur T

Various agents are described to denerve, modulate, or otherwise affect the renal nerves and other neural tissue. Also, various delivery devices are described to deliver an agent locally to the renal nerves. The delivery devices are positioned in the renal artery and penetrate into the wall of the renal artery to deliver the agent to the renal nerves. The delivery devices may be used to deliver the agent according to longitudinal position, radial position, and depth of the renal nerves relative to the renal artery. In addition, various methods are described to denervate, modulate, or otherwise affect the renal nerves and other neural tissue.

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Номер записи: 29
03-05-2012 дата публикации

Azaquinazolinediones Chymase Inhibitors

Номер: US20120108597A1
Автор: Chuk Chui Man, Hidenori Takahashi, Xin Guo
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.

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Номер записи: 30
03-05-2012 дата публикации

Compounds and compositions for treating chemical warfare agent-induced injuries

Номер: US20120108613A1
Автор: Jayhong A. Chong
Принадлежит: Hydra Biosciences LLC

Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

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Номер записи: 31
03-05-2012 дата публикации

Injectable composition containing hydroxychloroquine for local administration for treating hemorrhoids

Номер: US20120108633A1
Автор: Oh-Young Yeo
Принадлежит: Individual

The present invention relates to an injectable composition for local administration for treating hemorrhoids, which contains hydroxychloroquine. Specifically, the composition contains a solution of hydroxychloroquine in physiological saline for injection, together with a local anesthetic and an antioxidant.

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Номер записи: 32
10-05-2012 дата публикации

Pharmaceutical agent for preventing cell death

Номер: US20120115927A1
Автор: Futoshi Shibasaki, Li Chen
Принадлежит: TOKYO METROPOLITAN INSTITUTE OF MEDICAL SCIENCE

Disclosed is a pharmaceutical agent for preventing cell death. The occurrence of cell death can be prevented by inhibiting the function of Int6 protein in an affected area. Then, a pharmaceutical agent comprising a substance capable of inhibiting the function of Int6 protein is prepared. The pharmaceutical agent can be used for preventing cell death.

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Номер записи: 33
17-05-2012 дата публикации

Composition for Use in the Prevention and Treatment of Cardiovascular Diseases

Номер: US20120121732A1
Автор: Hjh Che Anishas Hj. Che Idris, Kalyana Sundram P. Manickam, Mohd Basri Wahid, Nagendran Balasundram, Ravigadevi Sambanthamurthi, Yew Ai TAN
Принадлежит: Palm Oil Research and Development Board

The invention provides a composition the prevention and treatment of cardiovascular disease, wherein said composition compounds obtained from palm oil mill effluents, in particular from vegetative liquor from the milling of palm oil fruit.

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Номер записи: 34
17-05-2012 дата публикации

Diagnostic agent for ischemic heart disease risk group

Номер: US20120122777A1
Автор: Issei Komuro, Kenji Hashimoto, Masao Daimon, Tohru Minamino
Принадлежит: Daiichi Pure Chemicals Co Ltd

The present invention relates to a diagnostic agent for an ischemic heart disease risk group comprising an anti-brain-derived neurotrophic factor antibody as an effective ingredient, to an assay method for an ischemic heart disease risk group performed by measuring a brain-derived neurotrophic factor concentration in blood, and to a suppressive/preventive drug for ischemic heart disease, particularly for post-infarction myocardial remodeling, comprising a brain-derived neurotrophic factor.

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Номер записи: 35
17-05-2012 дата публикации

Prodrugs and the use thereof

Номер: US20120122820A1
Автор: Claudia Hirth-Dietrich, Hanna Tinel, Hans-Georg Lerchen, Jörg Keldenich, Nicole Diedrichs, Thomas Krahn, Ursula Krenz
Принадлежит: Bayer Schering Pharma AG

The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.

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Номер записи: 36
31-05-2012 дата публикации

Cyclic triazo sodium channel blockers

Номер: US20120135993A1
Автор: Dieter Riddall, Karl Franzmann, Laurence Harbige, Michael Leach
Принадлежит: University of Greenwich

The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ═NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.

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Номер записи: 37
07-06-2012 дата публикации

Pharmaceutical composition including a dha ester to be administered parenterally

Номер: US20120141563A1
Автор: Elie Leverd, Elsa Kung, Mathew Leigh, Peter Van Hoogevest
Принадлежит: Pierre Fabre Medicament SA

The present invention relates to a pharmaceutical composition to be parenterally administered, including submicronic ester particles of docosahexaenoic acid, dispersed in an aqueous phase using a mixture of at least two surfactants selected from among a) at least one polyoxyethylene fatty acid ester and b) at least one phospholipid derivative. The present invention also relates to the method for preparing said pharmaceutical composition.

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Номер записи: 38
07-06-2012 дата публикации

Picolinamide derivatives as ttx-s blockers

Номер: US20120142691A1
Автор: Hirohide Noguchi, Mikio Morita, Tadashi Inoue, Yoshimasa Arano
Принадлежит: Raqualia Pharma Inc

The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.

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Номер записи: 39
07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Автор: Angelo Ceci, Annette Schuler-Metz, Dieter Wiedenmayer, Henning Priepke, Henri Doods, Ingo Konetzki, Juergen Mack, Norbert Hauel, Rainer Walter
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of the formula I wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.

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Номер записи: 40
14-06-2012 дата публикации

Compositions and methods for the prevention and treatment of hypertension

Номер: US20120148691A1
Автор: Ming Li, Peng Peng
Принадлежит: Generex Pharmaceuticals Inc

Disclosed herein are compounds, extracts, and active fractions of the plant Geum japonicum and methods for preventing or treating hypertension. The compounds provided herein can be formulated into pharmaceutical compositions and medicaments that are useful in the disclosed methods. Also provided are the use of the compounds and extracts in preparing pharmaceutical formulations and medicaments.

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Номер записи: 41
21-06-2012 дата публикации

Microbubbles and methods for oxygen delivery

Номер: US20120156300A1
Автор: Francis X. Mcgowan, John Kheir, Mark Andrew Borden
Принадлежит: Childrens Medical Center Corp, Columbia University of New York

Compositions containing a carrier and microbubbles encapsulating one or more gases, preferably oxygen, and methods for making and using the compositions are described herein. The microbubbles contain a lipid envelope. The compositions may be administered to a patient to quickly deliver large amounts of oxygen to the patient's blood supply or directly to a tissue in need of oxygen. The compositions may be administered via injection or as a continuous infusion. The compositions contain a concentrated microbubble suspension, where the suspension contains at least 40 mL oxygen/dL suspension. The microbubbles are preferably less than 20 microns in diameter, more preferably less than 15 microns in diameter. The microbubbles described herein may be administered to a patient in an effective amount to increase in oxygen concentration in the patient's blood, and/or one or more tissues or organs.

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Номер записи: 42
28-06-2012 дата публикации

Temperature sensitive hydrogel and block copolymers

Номер: US20120164100A1
Автор: Faquan Zeng, Ren-Ke Li
Принадлежит: UNIVERSITY HEALTH NETWORK

The present disclosure provides temperature sensitive hydrogels and block copolymers, processes for the production thereof, and therapeutic and research compositions employing these copolymers.

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Номер записи: 43
28-06-2012 дата публикации

Angiogenically effective unit dose of fgf and method of administering

Номер: US20120165245A1
Автор: Martha J. Whitehouse, W. Michael Kavanaugh
Принадлежит: Novartis Vaccines and Diagnostics Inc

The present invention provides a unit dose comprising 0.2 μg/kg to 36 μg/kg of a recombinant FGF or an angiogenically active fragment or mutein thereof. Also provided is a pharmaceutical composition comprising an angiogenically effective dose of an FGF or an angiogenically active fragment or mutein thereof, and a pharmaceutically acceptable carrier. Also provided is a method for treating a human patient for coronary artery disease, comprising administering into at least one coronary vessel of said patient a safe and angiogenically effective dose of a recombinant FGF of any of SEQ ID NOS:1-3, 5, 8-10, or 12-14, or an angiogenically active fragment or mutein thereof.

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Номер записи: 44
28-06-2012 дата публикации

Quinoline derivatives as pi3 kinase inhibitors

Номер: US20120165321A1
Автор: Carla A. Donatelli, Joelle Lorraine Burgess, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Michael Gerrard Darcy, Nicholas D. Adams, Stanley J. Schmidt, Steven David Knight
Принадлежит: GlaxoSmithKline LLC

Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.

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Номер записи: 45
28-06-2012 дата публикации

Transdermal drug delivery device including an occlusive backing

Номер: US20120165762A1
Автор: David Kanios, Juan A. Mantelle, Viet Nguyen
Принадлежит: Noven Pharmaceuticals Inc

A transdermal drug delivery system for the topical application of one or more active agents contained in one or more polymeric and/or adhesive carrier layers, proximate to a non-drug containing polymeric backing layer which can control the delivery rate and profile of the transdermal drug delivery system by adjusting the moisture vapor transmission rate of the polymeric backing layer.

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Номер записи: 46
05-07-2012 дата публикации

Arginase Inhibitors and Methods of Use Thereof

Номер: US20120171116A1
Автор: Bhaskara Rao Nallaganchu, Bruce Edward Tomczuk, Gary Lee Olson, Jane Wang, Richard Scott Pottorf
Принадлежит: Corridor Pharmaceuticals Inc

The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.

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Номер записи: 47
12-07-2012 дата публикации

Rho kinase inhibitors

Номер: US20120178752A1
Автор: Daniel Richard Marshall, Erick Richard Roush Young, John David Ginn, Robert Sibley, Ronald John Sorcek, Yunlong Zhang
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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Номер записи: 48
02-08-2012 дата публикации

2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses

Номер: US20120196866A1
Автор: Ali Ates, Benoît KENDA, Joël MERCIER, Laurent Turet, PHILIPPE MICHEL, Yannick Quesnel
Принадлежит: UCB PHARMA SA

The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

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Номер записи: 49
09-08-2012 дата публикации

Coacervate having an ionic polymer mixed with the adhesive protein of a mussel or of a species of the variome thereof

Номер: US20120201748A1
Автор: Bong-Hyuk Choi, Dong Gyun Kang, Hyung Joon Cha, Seonghye Lim, Yoo Seong CHOI, Young Hoon Song
Принадлежит: Academy Industry Foundation of POSTECH

The present invention relates to a coacervate comprising a mussel adhesive protein and an anionic polymer, and more particularly, to a coacervate prepared by mixing a mussel adhesive protein with an anionic polymer, and a novel use thereof. In the present invention, a coacervate prepared by mixing a mussel adhesive protein and an anionic polymer shows a very excellent adhesive strength to various substrates such as cells or metals, and is able to maintain its adhesive strength in the presence of water or under water, thereby being effectively used as an adhesive. Moreover, it has an activity capable of encapsulating bioactive materials, thereby being effectively used as an active component of a composition for delivering bioactive materials.

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Номер записи: 50
09-08-2012 дата публикации

Ureidophenyl substituted triazine derivatives and their therapeutical applications

Номер: US20120202818A1
Автор: Chunlin Tao, Laxman Nallan, Lukasz Koroniak, Neil Desai, Qinwei Wang
Принадлежит: California Capital Equity LLC

The present invention provides Uredophenyl substituted triazine derivatives and provides methods of using these compounds to modulate protein kinases and methods of using these compounds to treat protein kinase mediated diseases and conditions.

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Номер записи: 51
09-08-2012 дата публикации

Methods of treating diseases with proanthocyanidin oligomers such as crofelemer

Номер: US20120202876A1
Автор: Alan S. Verkman, Lukmanee Tradtrantip, Pravin Chaturvedi, Wan Namkung
Принадлежит: Napo Pharmaceuticals Inc, UNIVERSITY OF CALIFORNIA

Disclosed herein are methods of treating diseases including gastrointestinal disorders, such as secretory diarrheas, with the proanthocyanidin oligomer, crofelemer. Also disclosed is the anti-secretory effect of crofelemer on Calcium-activated chloride channels (CaCC) and Cystic fibrosis transmembrane conductance regulator (CFTR).

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Номер записи: 52
16-08-2012 дата публикации

Compositions and methods for treatment of cardiovascular disease

Номер: US20120207822A1
Автор: Stanley Hazen, Zeneng Wang
Принадлежит: CLEVELAND CLINIC FOUNDATION

Provided herein are compositions for the treatment and/or prevention of cardiovascular disease (CVD), and methods of application and use thereof. In particular, the present invention provides treatment and/or prevention of cardiovascular disease with 3,3-dimethyl-1-butanol (DMB) and related compounds, and pharmaceutical formulations thereof. In other embodiments, the present invention provides methods of administering a gut flora targeting antibiotic to a subject prior to a procedure that is associated with a risk of causing thrombosis, heart-attack, and/or platelet hyper-responsiveness.

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Номер записи: 53
16-08-2012 дата публикации

Drug eluting implantable medical device with hemocompatible and/or prohealing topcoat

Номер: US20120209371A1
Автор: Lothar W. Kleiner, Yiwen Tang
Принадлежит: Abbott Cardiovascular Systems Inc

The present invention relates to implantable medical devices coated with polymer having hemocompatible and/or prohealing moieties appended thereto and to their use in the treatment of vascular diseases.

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Номер записи: 54
23-08-2012 дата публикации

Methods for protecting dopaminergic neurons from stress and promoting proliferation and differentiation of oligodendrocyte progenitors by nrg-2

Номер: US20120214737A1
Автор: Mark Marchionni
Принадлежит: Acorda Therapeutics Inc

The invention features methods of treatment and diagnosis using NRG-2 polypeptides, nucleic acid molecules, and antibodies. The invention also provides novel NRG-2 polypeptides and nucleic acid molecules.

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Номер записи: 55
27-09-2012 дата публикации

Means and methods for treating ischemic conditions

Номер: US20120245078A1
Автор: Carola FÖRSTER
Принадлежит: Individual

The present invention relates to a combination of (a) at least one glucocorticoid; and (ba) at least one proteasome inhibitor and/or (bb) at least one nucleic acid encoding a glucocorticoid receptor, said glucocorticoid receptor being resistant to proteasomal degradation, for use in the treatment or prevention of ischemic disorders of the central nervous system. Furthermore provided is at least one proteasome inhibitor and/or at least one nucleic acid encoding a glucocorticoid receptor, said glucocorticoid receptor being resistant to proteasomal degradation, for use in treating or preventing glucocorticoid resistance in ischemic disorders of the central nervous system.

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Номер записи: 56
27-09-2012 дата публикации

Polypeptides having modulatory effects on cells

Номер: US20120245092A1
Автор: Benoit de Chassey, Brian B. Rudkin, Ivan Jacques Mikaelian, Pierre Colas
Принадлежит: ECOLE NORMALE SUPERIEURE DE LYON

The present invention relates to peptides and polypeptides having the sequence SAVTFAVCAL or variants thereof, capable of binding to Calcineurin and/or to NS5A-TP2 and to their use in therapy, as well as to nucleic acid sequences and vectors encoding these peptides and polypeptides, and to cells comprising said polypeptides, nucleic acid sequences or vectors. The invention further relates to the use of the peptides, polypeptides or their derivatives to bring about phenotypic changes in mammalian cells, particularly to up-regulate calcineurin activity. The invention finally relates to a method for intracellular identification of substances which bind to calcineurin and which modulate the physiological effects of calcineurin.

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Номер записи: 57
04-10-2012 дата публикации

Endopeptidase and Neurotoxin Combination Treatment of Multiple Medical Conditions

Номер: US20120251574A1
Автор: Andrew M. Blumenfeld, Mitchell F. Brin
Принадлежит: Allergan Inc

The present specification discloses Clostridial neurotoxins and TEMs, compositions comprising such Clostridial neurotoxins and TEMs, methods of treating a multiple medical disorder in an individual using such compositions, use of such Clostridial neurotoxins and TEMs in manufacturing a medicament for treating a multiple medical disorder, and uses of such Clostridial neurotoxins and TEMs in treating a multiple medical disorder.

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Номер записи: 58
04-10-2012 дата публикации

Method of therapy and diagnosis of atherosclerosis

Номер: US20120252867A1
Автор: Ching-Yu Hu, I-Chung Hsieh, Ku-Chugn Chen, Suh-Hang Juo
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

There is provided a method of therapy of atherosclerosis, by providing microRNA let-7g, an analogue thereof or modified let-7g to organisms to inhibit the expression of lectin-like oxidized low density lipoprotein receptor-1 (LOX-1), and the binding of LOX-1 and oxidized low-density lipoprotein (oxLDL), so as to block the pathogenesis of atherosclerosis. Also, a method of diagnosis of atherosclerosis comprises determining the levels of microRNA let-7g in serum or plasma samples of organisms, in which the levels of microRNA let-7g is estimated in individuals with atherosclerosis as compared to individuals without atherosclerosis.

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Номер записи: 59
11-10-2012 дата публикации

Inhibitors of e1 activating enzymes

Номер: US20120258927A1
Автор: Edward J. Olhava, Stepan Vyskocil, Steven P. Langston
Принадлежит: Millennium Pharmaceuticals Inc

This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

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Номер записи: 60
11-10-2012 дата публикации

Novel antiplatelet agent

Номер: US20120258951A1
Автор: Hiroshi Sato, Kazushi Sato, Kazutoshi Yokoyama
Принадлежит: Mitsubishi Tanabe Pharma Corp

The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR 1d , X b1 -X b5 are the same or different, and are nitrogen or carbon, R 1a -R 1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R 2 is an optionally substituted aryl or an optionally substituted heteroaryl, R 3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.

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Номер записи: 61
11-10-2012 дата публикации

Dual-acting pyrazole antihypertensive agents

Номер: US20120259113A1
Автор: Brooke BLAIR, Melissa Fleury, Michael Wilson, Paul R. Fatheree, Robert Murray Mckinnell, Roland Gendron, Ryan Hudson
Принадлежит: Theravance Inc

In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R 3 , R 4 and R 5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT 1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

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Номер записи: 62
18-10-2012 дата публикации

Coating Comprising An Elastin-Based Copolymer

Номер: US20120263759A1
Автор: Lothar W. Kleiner, Syed F.A. Hossainy, Yiwen Tang
Принадлежит: Abbott Cardiovascular Systems Inc

A copolymer comprising a block of an elastin pentapeptide and method of making and using the copolymer are provided. The copolymer may be used as a coating on a stent. Methods of using a stent coated with the copolymer are also provided.

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Номер записи: 63
25-10-2012 дата публикации

Therapeutic human anti-il-1r1 monoclonal antibody

Номер: US20120269824A1
Автор: Alison Witte, Brian Varnum, Chris Vezina, Francis Hall Martin, Gary Elliott, Haichun Huang, Xueming Qian
Принадлежит: AMGEN INC, Medarex LLC

Antibodies that interact with interleukin-1 receptor type 1 (IL-1R1) are described. Methods of treating IL-1 mediated diseases by administering a pharmaceutically effective amount of antibodies to IL-1R1 are described. Methods of detecting the amount of IL-1R1 in a sample using antibodies to IL-1R1 are described.

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Номер записи: 64
01-11-2012 дата публикации

Lipoxin compounds and their use in treating cell proliferative disorders

Номер: US20120277311A1
Автор: Charles N. Serhan
Принадлежит: Brigham and Womens Hospital Inc

Compounds having the active site of natural lipoxins, but a longer tissue half-life are disclosed. In particular, 15-epi-lipoxins and their use in ameliorating undesired cell proliferation, which characterizes diseases such as cancer, are also disclosed.

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Номер записи: 65
08-11-2012 дата публикации

Method for treating or preventing thrombosis using dabigatran etexilate or a salt thereof with improved safety profile over conventional warfarin therapy

Номер: US20120282187A1
Автор: Paul Anthony REILLY
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

A method for preventing stroke in a patient suffering from atrial fibrillation, wherein the patient has at least one risk factor for major bleeding events, the method comprising administering to the patient 110 mg b.i.d. of dabigatran etexilate, optionally in the form of a pharmaceutically acceptable salt thereof.

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Номер записи: 66
08-11-2012 дата публикации

Methods and compositions for the induction of hypothermia

Номер: US20120282227A1
Автор: Laurence M. Katz
Принадлежит: UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

Provided herein are methods for the induction of hypothermia and the treatment of clinical insults in a subject through the administration of a regulated hypothermic multidrug combination. The compositions or multidrug combinations of the invention comprise a regulated hypothermic compound or a dopamine receptor agonist; a vasoactive compound; and an antiarrhythmic compound or a serotonin 5-HT3 receptor antagonist. Additional agents can be included in the composition including at least one of an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. The invention further recognizes that a two phase delivery of multidrug combinations, a rapid infusion of the composition to induce hypothermia followed by a period of slow infusion to maintain the hypothermic state for a sustained period of time. Using the two phase delivery method of the invention, the composition may comprise ethanol and, optionally, at least one of a vasoactive compound, an antiarrhythmic compound, a serotonin 5-HT3 receptor antagonist, an antioxidant, a vitamin, N-acetylcysteine, and an antihyperglycemic compound. This two phase delivery method can be used to deliver any of the compositions of the invention and provides significant benefits to a patient.

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Номер записи: 67
15-11-2012 дата публикации

Nicotinic Acetylcholine Receptor Sub-Type Selective Amides of Diazabicycloalkanes

Номер: US20120289572A1
Автор: Anatoly Mazurov, Lan Miao, Yun-De Xiao
Принадлежит: Targacept Inc

Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

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Номер записи: 68
15-11-2012 дата публикации

SDF-1 Delivery For Treating Ischemic Tissue

Номер: US20120289585A1
Автор: Joseph Pastore, Marc S. Penn, Rahul Aras, Timothy J. Miller
Принадлежит: Joseph Pastore, Miller Timothy J, Penn Marc S, Rahul Aras

A method of treating a cardiomyopathy in a subject includes administering directly to or expressing locally in a weakened, ischemic, and/or peri-infarct region of myocardial tissue of the subject an amount of SDF-1 effective to cause functional improvement in at least one of the following parameters: left ventricular volume, left ventricular area, left ventricular dimension, cardiac function, 6-minute walk test, or New York Heart Association (NYHA) functional classification.

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Номер записи: 69
22-11-2012 дата публикации

Chromone Inhibitors of S-Nitrosoglutathione Reductase

Номер: US20120295966A1
Автор: Jan Wasley, Jian Qiu, Xicheng Sun
Принадлежит: N30 Pharmaceuticals Inc

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

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Номер записи: 70
29-11-2012 дата публикации

Method Of Reducing Injury To Mammalian Cells

Номер: US20120302504A1
Автор: Michael Tymianski
Принадлежит: NoNO Inc

A method of inhibiting the binding between N-methyl-D-aspartate receptors and neuronal proteins in a neuron is disclosed. The method comprises administering to the neuron an effective inhibiting amount of a peptide replacement agent for the NMDA receptor or neuronal protein interaction domain that effect said inhibition of the NMDA receptor-neuronal protein interaction. The method is of value in reducing the damaging effect of injury to mammalian cells. Postsynaptic density-95 protein (PSD-95) couples neuronal N-methyl-D-aspartate receptors (NMDARs) to pathways mediating excitotoxicity, ischemic and traumatic brain damage. This coupling was disrupted by transducing neurons with peptides that bind to modular domains on either side of the PSD-95/NMDAR interaction complex. This treatment attenuated downstream NMDAR signaling without blocking NMDAR activity, protected cultured cortical neurons from excitotoxic insults, dramatically reduced cerebral infarction volume in rats subjected to transient focal cerebral ischemia, and traumatic brain injury (TBI) in rats.

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Номер записи: 71
06-12-2012 дата публикации

Oral medication for the treatment of hemorrhoids and method of use

Номер: US20120308553A1
Автор: Joseph P. Thornton
Принадлежит: Individual

A natural supplement in the form of an orally ingested tablet for treatment of hemorrhoids. Bromelain and Psyllium (e.g., Psyllium husk powder) are the primary active ingredients in the natural supplement tablet. Optionally, Witch Hazel, in the form of Witch Hazel leaf, for example, may be added to the composition. Secondary ingredients include Dicalcium Phosphate, Cellulose, Croscarmellose Sodium, Stearic Acid and Silicon Dioxide. Based on case studies the natural supplement outperforms over-the-counter and prescribed hemorrhoid medications.

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Номер записи: 72
06-12-2012 дата публикации

Treatment of atrial fibrillation

Номер: US20120309810A1
Автор: Gary T. Elliott
Принадлежит: HUYA Bioscience International

Atrial fibrillation (AF) can be treated or prevented by administering to a subject who suffers from or is at risk of suffering from AF a composition comprised of an amount of an active agent, which is 4 -methoxy-N-( 3,5-bis ( 1 -pyrrolidayl)- 4 -hydroxy benzyl) benzene sulfonamide (sulcardine) or a pharmaceutically acceptable salt thereof, such that the Cmax value the active agent in the subject is in the range from about 1 μM to about 20 μM.

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Номер записи: 73
20-12-2012 дата публикации

Biarylamide inhibitors of leukotriene production

Номер: US20120322795A1
Автор: Angela Berry, Chuk Chui Man, Hidenori Takahashi, Michel Jose Emmanuel, Pui Leng Loke, Stephane De Lombaert, Tina Marie Morwick, Zhidong Chen
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R 1a , R 1b , R 2 , R 3 , R 4a and R 4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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Номер записи: 74
27-12-2012 дата публикации

Pharmaceutical Composition Comprising miRNA-100 And Its Use in the Modulation Of Blood Vessel Growth and Endothelial Inflammation

Номер: US20120328686A1
Автор: Christoph Bode, Felix Hans, Franziska Bluhm, Martin Moser, Sebastian Grundmann
Принадлежит: Individual

Disclosed is a pharmaceutical composition comprising a miRNA-100 molecule or an antagomir thereof or a variant thereof for use as a medicament for the positive or negative modulation of blood vessel growth and vascular inflammation wherein the miRNA-100 or the miRNA antagomir has a homology of at least 85% to any of SEQ ID NO:1, 2, 3 and/or 9.

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Номер записи: 75
27-12-2012 дата публикации

Potent and Selective Mediators of Cholesterol Efflux

Номер: US20120329703A1
Автор: Jan Johansson, John K. Bielicki
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention provides a family of non-naturally occurring polypeptides having cholesterol efflux activity that parallels that of full-length apolipoproteins (e.g., Apo AI and Apo E), and having high selectivity for ABAC1 that parallels that of full-length apolipoproteins. The invention also provides compositions comprising such polypeptides, methods of identifying, screening and synthesizing such polypeptides, and methods of treating, preventing or diagnosing diseases and disorders associated with dyslipidemia, hypercholesterolemia and inflammation.

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Номер записи: 76
27-12-2012 дата публикации

Formulations and methods for vascular permeability-related diseases or conditions

Номер: US20120329759A1
Автор: David A. Weber, David M. Kleinman, Mary E. Gerritsen, Thierry Nivaggioli
Принадлежит: Santen Pharmaceutical Co Ltd

Described herein are formulations and methods for treating, inhibiting, preventing, delaying onset, or causing regression of a disease or condition relating to vascular permeability.

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Номер записи: 77
27-12-2012 дата публикации

Imatinib mesylate oral pharmaceutical composition and process for preparation thereof

Номер: US20120329810A1
Автор: Kali Satya Bhujanga Rao Adibhatla, VENKAIAH CHOWDARY Nannapaneni
Принадлежит: Natco Pharma Ltd

The invention relates to an oral pharmaceutical composition comprising, greater than 80% of Imatinib, by weight based on the total weight of the composition and the process for preparation thereof.

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Номер записи: 78
27-12-2012 дата публикации

Process for the preparation of dronedarone

Номер: US20120330036A1
Автор: Antal Friesz, Mariann Csatarine Nagy
Принадлежит: SANOFI SA

The subject of the present disclosure is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.

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Номер записи: 79
03-01-2013 дата публикации

COMBINATION COMPOSITION, COMPRISING AS ACTIVE INGREDIENTS L-CARNITlNE OR PROPIONYL L-CARNITlNE, FOR THE PREVENTION OR TREATMENT OF CHRONIC VENOUS INSUFFICIENCY

Номер: US20130005670A1
Автор: Aleardo Koverech, Mohamed Ashraf Virmani
Принадлежит: Sigma Tau Industrie Farmaceutiche Riunite SpA

It is described a combination composition comprising as active ingredients L-carnitine or propionyl L-carnitine, troxerutine, diosmine and hesperidine, useful for the prevention and/or treatment of chronic venous diseases.

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Номер записи: 80
03-01-2013 дата публикации

Metalloenzyme inhibitor compounds

Номер: US20130005719A1
Автор: Christopher M. Yates, Gary D. Gustafson, Michael R. Loso, Michael T. Sullenberger, Robert J. Schotzinger, Stephen W. Rafferty, William J. Hoekstra
Принадлежит: Viamet Pharmaceuticals Inc

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

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Номер записи: 81
03-01-2013 дата публикации

Crystalline forms of neurotrophin mimetic compounds and their salts

Номер: US20130005731A1
Автор: Frank M. Longo, Rajgopal Munigeti
Принадлежит: Pharmatrophix Inc

The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.

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Номер записи: 82
10-01-2013 дата публикации

ESTABLISHMENT OF PATIENT- OR PERSON- SPECIFIC CARDIAC MYOCYTE CELL LINES FROM HUMAN INDUCED PLURIPOTENT STEM CELLS (iPSCs)

Номер: US20130011371A1
Автор: Jinsong Shen, Raphael Schiffmann, Xingli Meng
Принадлежит: BAYLOR RESEARCH INSTITUTE

A composition and method for generating patient- or person-specific proliferative and substantially pure cardiac myocyte cell lines from pluripotent stem cells (iPSCs) is described herein. The patient-specific cardiac myocyte cell lines of the present invention find applications in research, drug screening and autologous cell-based therapy. The method of the present invention is simple and reproducible and generates cardiac myocyte cells having high purities and proliferating capacities.

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Номер записи: 83
17-01-2013 дата публикации

Methods and systems for pharmacogenomic treatment of cardiovascular conditions

Номер: US20130018024A1
Автор: Fabio Macciardi, Giuseppe Bianchi, Patrizia Ferrari
Принадлежит: ROSTAQUO SpA

Methods and systems are provided herein that are based on the effects of genetic variations on the biological activities associated to rostafuroxin in an individual. In particular, compositions, methods and systems are herein described that are based on an indentified influence on an individual response to rostafuroxin of one or more polymorphisms in an intergenic or intragenic region of a gene selected from the group consisting of KCNS3, THSD7A, FAM46A, LOC389970, HLA-G, and TTC29, and/or a genetic variation in linkage disequilibrium therewith.

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Номер записи: 84
24-01-2013 дата публикации

Drug delivery system for the prevention of cerebral vasospasm

Номер: US20130022660A1
Автор: Brian A. Leuthner, R. Loch Macdonald
Принадлежит: Edge Therapeutics Inc

The present invention relates to the treatment and prevention of vasospasm. The present invention provides a system for treating a cerebral vasospasm in a human utilizing a pharmaceutical composition and administrating a therapeutically effective amount of the pharmaceutical composition to a predetermined location in close proximity to a cerebral artery within a subarachnoid space wherein the pharmaceutical composition produces a localized pharmacologic effect thereby treating the cerebral vasospasm.

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Номер записи: 85
24-01-2013 дата публикации

Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disorders as agonists of g-protein coupled receptor 43 (gpr43)

Номер: US20130023539A1
Автор: Didier Schils, Hamid R. Hoveyda, Julien Parcq, Ludivine Zoute
Принадлежит: Euroscreen SA

The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.

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Номер записи: 86
31-01-2013 дата публикации

Inhibitors of protein kinases

Номер: US20130029944A1
Автор: Anjali Pandey, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Yonghong Song, Zhaozhong J. Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 87
14-02-2013 дата публикации

Electric Conduction Through Supramolecular Assemblies of Triarylamines

Номер: US20130037307A1
Автор: Bernard Doudin, Emilie Moulin, Frederic Niess, Jean-François Dayden, Nicolas Giuseppone, Vina FARAMARZI
Принадлежит: Universite De Strasbourg

The present invention relates to a method for modifying a surface of a solid conducting material, which comprises a step (E), in which a potential difference is applied between this surface and a surface of another conducting solid material positioned facing it, and wherein, simultaneously, said surface (S) is put into contact with a liquid medium comprising in solution triarylamines (I): while subjecting these triarylamines (I) to electromagnetic radiation, least partly converting them at into triarylammonium radicals. The invention also relates to a conducting device comprising two conducting metal materials, the surfaces of which, (S) and (S′) respectively, are electrically interconnected through an organic material comprising conducting fibrillar organic supramolecular species comprising an association of triarylamines of formula (I).

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Номер записи: 88
21-02-2013 дата публикации

Methods and apparatus for determining formulation orientation of multi-layered pharmaceutical dosage forms

Номер: US20130043612A1
Автор: Johan H. Geerke, Steven F. Stone
Принадлежит: Alza Corp

Rapid and accurate determination of the formulation orientation of multi-layer capsule-shaped tablets with respect to different internal formulation layers proximate to the opposite narrow and rounded ends of the tablets is required. By including an appropriate color scheme in multi-layer osmotic tablets, detection of the formulation orientation is achieved by detecting the color at a spot location on a side of the tablet corresponding to one or another formulation layer or to one or another interface of two formulation layers depending on the formulation orientation of the tablet.

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Номер записи: 89
21-02-2013 дата публикации

Neuroprotective modulation of nmda receptor subtype activities

Номер: US20130045991A1
Автор: Lidong Liu, Tak Pan Wong, Yitao Liu, Yu Tian Wang
Принадлежит: University of British Columbia

In various aspects, the invention provides methods and compositions for modulating NMDA receptor subtype activity, to enhance NR2A-containing NMDA receptor activity relative to NR2B-containing NMDA receptor activity, so as to effect a neuroprotective reduction in excitotoxic NMDA receptor activity

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Номер записи: 90
07-03-2013 дата публикации

Pyrimidine derivatives for the treatment of amyloid-related diseases

Номер: US20130059871A1
Автор: David Christopher Horwell, David Ian Carter Scopes
Принадлежит: Individual

The present invention provides (I) these compounds are useful in prevention and treatment of neurodegenerative disorders, such as Alzheimer's, Parkinson's and Huntington's as well as type II diabetes.

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Номер записи: 91
07-03-2013 дата публикации

Methods of identifying modulators of gpr17

Номер: US20130059899A1
Автор: Andreas Spinrath, Christa E. MÜLLER, Evi Kostenis, Kirsten Ritter, Lucas Peters, Rhalid Akkari, Stephanie Hennen, Younis Baqi
Принадлежит: Rheinische Friedrich Wilhelms Universitaet Bonn

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.

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Номер записи: 92
14-03-2013 дата публикации

Engineered anti-il-23r antibodies

Номер: US20130064817A1
Автор: Leonard G. Presta
Принадлежит: Merck Sharp and Dohme LLC

Antibodies to human IL-23R are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.

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Номер записи: 93
14-03-2013 дата публикации

N-piperidinyl acetamide derivatives as calcium channel blockers

Номер: US20130065926A1
Автор: Hassan A. Pajouhesh, Jason Tan, Lingyun Zhang, Michael Edward Grimwood, Nagasree Chakka, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Yuanxi Zhou
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

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Номер записи: 94
21-03-2013 дата публикации

Mitochondrial Compositions and Uses Thereof

Номер: US20130072462A1
Автор: Shaharyar Khan
Принадлежит: Gencia Corp

The present invention provides a compound of Formula 1a, wherein R 1 is H or phosphate and the double bond is between N′ and C′ or between N 2 and C 1 ; R 2 is a mitochondrial targeting moiety; R 3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R 4 is H or an alkyl, aryl, or heteroaryl group; and R 5 is alkyl, aryl, or heteroaryl; or N′ C′, and N 3 together form a heterocyclic ring containing at least 5 atoms, wherein N 1 , N 3 , and R 1 -R 5 are as defined above, or N 3 and R 5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.

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Номер записи: 95
21-03-2013 дата публикации

Use of rgm and its modulators

Номер: US20130072667A1
Автор: Bernd Stahl, Bernhard K. Mueller, Friedrich Bonhoeffer, Jens S. Anderson, Matthias Mann, Paolo Macchi, Philippe P. Monnier
Принадлежит: Individual

The present invention relates to the use of a modulator of a polypeptide having or comprising an amino acid sequence as disclosed herein or of a functional fragment or derivative thereof or of a polynucleotide encoding said polypeptide or fragment or derivative for the preparation of a pharmaceutical composition for preventing, alleviating or treating diseases or conditions associated with the degeneration or injury of vertebrate nervous tissue, associated with seizures or associated with angiogenic disorders or disorders of the cardio-vascular system.

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Номер записи: 96
28-03-2013 дата публикации

System for use in administering inhaled nitric oxide gas

Номер: US20130074839A1
Автор: James S. Baldassarre, Ralf Rosskamp
Принадлежит: INO THERAPEUTICS LLC

Disclosed are systems for use in administering inhaled nitric oxide gas as a therapeutic treatment, where the systems reduce the risk of inducing an increase in pulmonary capillary wedge pressure leading to pulmonary edema in neonatal patients who have hypoxic respiratory failure and are candidates for inhaled nitric oxide treatment, the system comprising a source of pharmaceutically acceptable nitric oxide gas for inhalation, a delivery device suitable for delivering nitric oxide gas from the source to a term or near-term neonate patient, and instructions for use in operating the system.

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Номер записи: 97
04-04-2013 дата публикации

Taste masked pharmaceutical composition

Номер: US20130084332A1
Автор: Annette Grave, Martin Folger, Norbert Poellinger, Randolph Seidler, Stefan Lehner
Принадлежит: BOEHRINGER INGELHEIM VETMEDICA GMBH

This application relates to taste masked multi-layered particles an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and comprising a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

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Номер записи: 98
11-04-2013 дата публикации

Isoforms of the human sst5 receptor originated by alternative splicing and oligonucleotide pairs to detect them by pcr

Номер: US20130089867A1
Автор: Antonio Jesus Martinez Fuentes, Francisco Gracia-Navarro, Justo Pastor Castano Fuentes, Maria Del Mar Malagon Poyato, Mario Duran Prado, Rafael Vazquez Martinez, Socorro Garcia Navarro
Принадлежит: UNIVERSIDAD DE CORDOBA

The present invention is referred to two human nucleic acids that comprise sequences encoding two new isoforms of the human somatostatin receptor type 5 originated by alternative splicing, named sst5B and sst5C, with possible involvement in tumor processes. In addition, the invention is referred to oligonucleotide pairs allowing their differential detection in several tissues using the PCR technique.

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Номер записи: 99
11-04-2013 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20130090483A1
Автор: Bertrand M. C. Plouvier, Doug Ta Hung Chou, Grace Jung, James Gee Ken Yee
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

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Номер записи: 100