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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 58535. Отображено 100.
05-01-2012 дата публикации

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

Номер: US20120003229A1
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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05-01-2012 дата публикации

Pharmaceutical compositions of dextran polymer derivatives

Номер: US20120003282A1
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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05-01-2012 дата публикации

Nanobead releasing medical devices

Номер: US20120003291A1
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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05-01-2012 дата публикации

Pharmaceutical Composition Comprising Aliskiren

Номер: US20120003308A1
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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05-01-2012 дата публикации

Methods of using a methylxanthine compound

Номер: US20120004248A1
Принадлежит: Deutschman Clifford S, Levy Richard J

The invention relates to compositions and methods for treating various diseases or medical conditions by administering a methylxanthine compound. Specifically, the invention relates to compositions and methods for treating cytochrome oxidase (CcOX) mediated diseases or medical conditions by administering compositions comprising a methyl xanthine compound.

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12-01-2012 дата публикации

Biomarkers for myocardial ischemia

Номер: US20120009174A1
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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12-01-2012 дата публикации

Synergistic combinations comprising a renin inhibitor for cardiovascular diseases

Номер: US20120010295A1

The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.

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19-01-2012 дата публикации

Il-1beta binding antibodies and fragments thereof

Номер: US20120014967A1
Принадлежит: Xoma Technology Ltd USA

An IL-1β binding antibody or IL-1β binding fragment thereof comprising the amino acid sequence of SEQ ID NO: 2, and related nucleic acids, vectors, cells, and compositions, as well as method of using same to treat or prevent a disease, and a method of preparing an affinity matured IL-1β binding polypeptide. IL-1β binding antibodies or IL-1β binding fragments thereof are provided which have desirable affinity and potency.

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19-01-2012 дата публикации

Novel compounds as cannabinoid receptor ligands

Номер: US20120015929A1
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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19-01-2012 дата публикации

Method for Synthesizing Pirfenidone

Номер: US20120016133A1
Принадлежит: Intermune Inc

A process for synthesizing pirfenidone from bromobenzene having less than about 0.15% by weight dibromobenze is disclosed. Also disclosed are processes of synthesizing pirfenidone without using ethyl acetate or n-butanol, and pirfenidone having controlled levels of ethyl acetate, n-butanol, di(5-methyl-2-pyridinone)benzenes, and other impurities having specified retention times. Also disclosed are formulated dosage forms including the disclosed pirfenidone.

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26-01-2012 дата публикации

Method of mitigating adverse drug events using omega-3 fatty acids as a parenteral therapeutic drug vehicle

Номер: US20120022001A1
Автор: David F. Driscoll
Принадлежит: STABLE SOLUTIONS LLC

A method of parenterally administering a composition, the method including parenterally administering to a person a composition including at least one omega-3 fatty acid and at least one drug, wherein the at least one omega-3 fatty acid source and the at least one drug are administered simultaneously.

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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
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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26-01-2012 дата публикации

Heterocyclic antagonists of prostaglandin d2 receptors

Номер: US20120022119A1
Принадлежит: Amira Pharmaceuticals Inc

Described herein are heteroaryl compounds that are antagonists of PGD 2 receptors. Also described are pharmaceutical compositions and medicaments that include the heteroaryl compounds described. Also described herein are methods of using such antagonists of PGD 2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

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26-01-2012 дата публикации

Short Interfering Ribonucleic Acid (siRNA) for Oral Administration

Номер: US20120022139A1
Принадлежит: NOVARTIS AG

Short interfering ribonucleic acid (siRNA) for oral administration, said siRNA comprising two separate RNA strands that are complementary to each other over at least 15 nucleotides, wherein each strand is 49 nucleotides or less, and wherein at least one of which strands contains at least one chemical modification.

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26-01-2012 дата публикации

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

Номер: US20120022155A1
Автор: Raffaella Scorza

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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02-02-2012 дата публикации

Short Interfering Ribonucleic Acid (siRNA) for Oral Administration

Номер: US20120029052A1
Принадлежит: NOVARTIS AG

Short interfering ribonucleic acid (siRNA) for oral administration, said siRNA comprising two separate RNA strands that are complementary to each other over at least 15 nucleotides, wherein each strand is 49 nucleotides or less, and wherein at least one of which strands contains at least one chemical modification.

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09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

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09-02-2012 дата публикации

Dual targeting of mir-208 and mir-499 in the treatment of cardiac disorders

Номер: US20120035243A1
Автор: Eric Olson, Eva Van Rooij
Принадлежит: University of Texas System

The present invention provides a method of treating or preventing cardiac disorders in a subject in need thereof by inhibiting the expression or function of both miR-499 and miR-208 in the heart cells of the subject. In particular, specific protocols for administering inhibitors of the two miRNAs that achieve efficient, long-term suppression are disclosed. In addition, the invention provides a method for treating or preventing musculoskeletal disorders in a subject in need thereof by increasing the expression or activity of both miR-208 and miR-499 in skeletal muscle cells of the subject.

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09-02-2012 дата публикации

Sphingo-guanidines and their use as inhibitors of sphingosine kinase

Номер: US20120035268A1

The presently disclosed subject matter provides compounds of the formula: (1) and pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and R 8 are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting sphingosine kinase, and their use in the treatment and/or prevention of diseases and/or conditions associated with undesirable ceramidase or sphingosine kinase activity, including, but not limit cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, immunological disorders, asthma, atopic dermatitis, wound healing, and other proliferative diseases.

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16-02-2012 дата публикации

Compound of salvianolic acid l, preparation method and use thereof

Номер: US20120041062A1
Принадлежит: Tianjin Tasly Pharmaceutical Co Ltd

The present invention relates to a new compound of salvianolic acid L, its preparation method, a pharmaceutical composition containing the salvianolic acid L, and its use for preparing a medicament for treating cardio-cerebrovascular diseases.

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23-02-2012 дата публикации

Methods of reducing the risk of cardiovascular disease in postmenopausal women

Номер: US20120046249A1

The present invention features materials and methods for reducing the risk of cardiovascular disease in postmenopausal or perimenopausal women. More specifically, these methods can be used in women who generally have no apparent cardiovascular disease. We describe herein methods of administering non-antibacterial tetracycline or a sub-antimicrobial amount of antibacterial tetracyclines or tetracycline formulations and their use in reducing the risk that cardiovascular disease will develop in a subject (e.g., in a post- or perimenopausal woman)

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23-02-2012 дата публикации

Coating Comprising An Elastin-Based Copolymer

Номер: US20120046640A1
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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01-03-2012 дата публикации

Splice-region antisense composition and method

Номер: US20120053228A1
Принадлежит: AVI Biopharma Inc

Antisense compositions targeted against an mRNA sequence coding for a selected protein, at a region having its 5′ end from 1 to about 25 base pairs downstream of a normal splice acceptor junction in the preprocessed mRNA, are disclosed. The antisense compound is RNase-inactive, and is preferably a phosphorodiamidate-linked morpholino oligonucleotide. Such targeting is effective to inhibit natural mRNA splice processing, produce splice variant mRNAs, and inhibit normal expression of the protein.

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08-03-2012 дата публикации

Modulation of drug release rate from electrospun fibers

Номер: US20120058100A1
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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15-03-2012 дата публикации

Genetic modification of targeted regions of the cardiac conduction system

Номер: US20120065253A1
Принадлежит: MEDTRONIC INC

Disclosed are methods and systems for preventing or treating cardiac dysfunction, particularly cardiac pacing dysfunction by genetic modification of the conduction system of the heart. In one embodiment, the invention provides a method of genetically modifying the cells by delivering to the cells one or more coding sequence in a genetic construct capable of modifying the expression of ion channels of the cells.

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15-03-2012 дата публикации

Cyclodextrin-based polymers for therapeutics delivery

Номер: US20120065368A1
Принадлежит: Cerulean Pharma Inc

The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distributing kits containing or relating to the polymeric compounds described herein.

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15-03-2012 дата публикации

Dual targeting antibody of novel form, and use thereof

Номер: US20120065380A1
Принадлежит: Pharmabcine Inc

The present invention relates to: a dual targeting antibody of a novel form having a water-soluble ligand fused to the N-terminus of a heavy chain or light chain of an antibody; a DNA encoding the dual targeting antibody; a recombinant expression vector containing the DNA; a host cell which is transformed with the recombinant expression vector; a method for preparing the dual targeting antibody by culturing the host cell; and a pharmaceutical composition including the dual targeting antibody.

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15-03-2012 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20120065408A1
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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22-03-2012 дата публикации

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

Номер: US20120070403A1
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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22-03-2012 дата публикации

Flavonoid hydrogel

Номер: US20120070433A1

There is provided methods for producing a hydrogel comprising conjugates of a hydrogel forming agent and a flavonoid including a method for producing a hydrogel that is capable of adhesion of cells and which comprises enzymatically cross-linked conjugates of a hydrogel forming agent and a flavonoid. There is also provided a method for producing a hydrogel comprising conjugates of a hydrogel forming agent and a flavonoid without the addition of an exogenous peroxide or peroxidase or without the addition of an exogenous peroxide. Hydrogels produced by such methods and methods of using the hydrogels are also described herein.

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22-03-2012 дата публикации

Method and Formulation for Treating Resistance to Antihypertensives and Related Conditions

Номер: US20120070501A1
Автор: Moshe Laudon, Nava Zisapel
Принадлежит: Neurim Pharmaceuticals 1991 Ltd

A method for the prevention or treatment of symptoms of hypertension in a patient who is resistant to antihypertensive effects of an antihypertensive compound administered in the absence of melatonin comprises administering to said patient melatonin in an amount effective to ameliorate or prevent symptoms of hypertension in said patient.

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29-03-2012 дата публикации

Antibodies to troponin i and methods of use thereof

Номер: US20120076803A1
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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29-03-2012 дата публикации

Prophylactic agent for renal failure

Номер: US20120077735A1
Принадлежит: Individual

The present invention provides an agent having a suppressive action against kidney glomerular disease and renal arteriosclerosis, a prophylactic agent for renal failure containing the above described agent, and functional foods expected to have a prophylactic effect for renal failure. The agent for preventing kidney glomerular disease and renal arteriosclerosis comprises Xaa Pro Pro as an active ingredient.

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12-04-2012 дата публикации

Acetylsalicylic acid salts

Номер: US20120088742A1
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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12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
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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19-04-2012 дата публикации

Treatment of limb ischemia

Номер: US20120093786A1
Принадлежит: ReNeuron Ltd

The present invention uses neural stem cells in the manufacture of a medicament for the treatment of a patient suffering peripheral arterial disease. The invention is particularly suited for treating limb ischemia or Buerger's disease.

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19-04-2012 дата публикации

GNA1870-Based Vesicle Vaccines for Broad Spectrum Protection Against Diseases Caused by Neisseria Meningitidis

Номер: US20120093867A1
Принадлежит: Individual

The present invention generally provides methods and compositions for eliciting an immune response against Neisseria spp. bacteria in a subject, particularly against a Neisseria meningitidis serogroup B strain.

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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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19-04-2012 дата публикации

Par-1 antagonism in fed or antacid-dosed patients

Номер: US20120095052A1
Принадлежит: Schering Corp

Disclosed are methods of inhibiting a PAR-1 receptor in a patient who has recently ingested food or an antacid comprising the step of administering an effective amount and/or the bisulfate salt thereof.

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26-04-2012 дата публикации

Stable pharmaceutical composition and methods of using same

Номер: US20120100208A1
Автор: Mehar Manku
Принадлежит: Amarin Pharma Inc

The present invention relates to, inter alia, pharmaceutical compositions comprising a polyunsaturated fatty acid and to methods of using the same to treat or prevent cardiovascular-related diseases.

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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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03-05-2012 дата публикации

Method of Inhibiting Smooth Muscle Cell Proliferation by Using Reconstituted HDL

Номер: US20120108495A1

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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03-05-2012 дата публикации

Azaquinazolinediones Chymase Inhibitors

Номер: US20120108597A1
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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03-05-2012 дата публикации

Methods and compositions involving (s)-bucindolol

Номер: US20120108617A1
Принадлежит: Arca Biopharma Inc

Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I).

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03-05-2012 дата публикации

Nitrogen-containing aromatic heterocyclyl compound

Номер: US20120108639A1
Принадлежит: Daiichi Sankyo Co Ltd

The present invention provides a compound having excellent regulating action on blood lipid level that is represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein, in one embodiment, A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R 1 represents COOH; each R 2 represents an alkyl; each R 3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R 4 , R 5 , R 6 , and R 7 represents H, an alkyl; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B 1 and B 2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.

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10-05-2012 дата публикации

Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid

Номер: US20120115920A1
Принадлежит: Theravance Inc

The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

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10-05-2012 дата публикации

Pharmaceutical agent for preventing cell death

Номер: US20120115927A1
Автор: Futoshi Shibasaki, Li Chen

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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10-05-2012 дата публикации

Protective action of serofendic acid on cardiac muscle

Номер: US20120115951A1
Принадлежит: Eisai R&D Management Co Ltd

A cardiac myocyte protective agent, comprising a compound represented by the formula (Ia) below, a pharmaceutically acceptable salt thereof, or a solvate thereof:

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10-05-2012 дата публикации

One pot process for preparing 2-butyl-3-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro [4, 4] non-1-en-4-one (irbesartan)

Номер: US20120116093A1
Принадлежит: CTX Life Sciences Pvt Ltd

A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1,3-Diazaspiro[4,4]Non-1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent.

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17-05-2012 дата публикации

Treatment of oncostatin m receptor beta mediated heart failure

Номер: US20120121579A1

The present invention relates to an inhibitor of the oncostatin M receptor β or an inhibitor of an activator of the oncostatin M receptor β for use in the treatment and/or prevention of heart failure. The present invention also relates to a method of treating and/or preventing heart failure comprising administering a pharmaceutically effective amount of an inhibitor of the oncostatin M receptor β or an inhibitor of an activator of the oncostatin M receptor β to a subject in need thereof. Further, the present invention also relates to methods of identifying a compound suitable as a lead compound and/or as a medicament for the treatment and/or prevention of heart failure.

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17-05-2012 дата публикации

Composition for Use in the Prevention and Treatment of Cardiovascular Diseases

Номер: US20120121732A1
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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17-05-2012 дата публикации

Diagnostic agent for ischemic heart disease risk group

Номер: US20120122777A1
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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17-05-2012 дата публикации

Compounds, Compositions and Methods for Modulating Uric Acid Levels

Номер: US20120122780A1
Принадлежит: Ardea Biociences Inc

Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

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17-05-2012 дата публикации

Prodrugs and the use thereof

Номер: US20120122820A1
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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17-05-2012 дата публикации

Aurora kinase modulators and method of use

Номер: US20120122847A1
Принадлежит: AMGEN INC

The present invention relates to chemical compounds having a general formula I wherein A 1-8 , D′, L 1 , L 2 , R 1 , R 6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.

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17-05-2012 дата публикации

Perhexiline for use in the treatment of hypertrophic cardiomyopathy (hcm)

Номер: US20120122925A1
Принадлежит: Heart Metabolics Ltd

The invention relates to perhexiline, or a pharmaceutically acceptable salt thereof, for use in the treatment of hypertrophic cardiomyopathy, as well as to a method of treating HCM, which comprises administering to an animal in need thereof an effective amount of perhexiline, or a pharmaceutically acceptable salt thereof, to treat said HCM. The invention further relates to a treatment programme for treating HCM, which involves the co-use or co-administration of perhexiline with one or more other compounds that are advantageous in treating HCM or the symptoms thereof.

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24-05-2012 дата публикации

Inhibition of ApoE Cleavage Activity in the Treatment of ApoE-Related Disorders

Номер: US20120129782A1
Принадлежит: J David Gladstone Institutes

The present invention provides methods for treating apoE-related disorders. The methods generally involve administering an effective amount of an agent that inhibits activity of an enzyme that cleaves apoE.

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24-05-2012 дата публикации

Stabilized composition comprising at least one adrenergic compound

Номер: US20120129944A1
Принадлежит: ALK AG

A stabilised composition comprising at least one adrenergic compound and at least one antioxidant selected from the group consisting of a bisulfite, a metabisulfite and a sulfite compound.

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07-06-2012 дата публикации

Pharmaceutical composition including a dha ester to be administered parenterally

Номер: US20120141563A1
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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07-06-2012 дата публикации

Treatment of 'iq motif containing gtpase activating protein' (iqgap) related diseases by inhibition of natural antisense transcript to iqgap

Номер: US20120142610A1
Принадлежит: OPKO CURNA LLC

The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of ‘IQ motif containing GTPase activating protein’ (IQGAP), in particular, by targeting natural antisense polynucleotides of ‘IQ motif containing GTPase activating protein’ (IQGAP). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of IQGAP.

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07-06-2012 дата публикации

Bicyclic compound

Номер: US20120142714A1
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

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14-06-2012 дата публикации

Pharmaceutical composition for preventing, stabilising and/or inhibiting blood and lymph vascularization

Номер: US20120149758A1
Автор: Salman Al Mahmood
Принадлежит: GENE SIGNAL INTERNATIONAL

A pharmaceutical composition including as active agent, an antisens oligonucleotide having the sequence SEQ ID NO: 1, wherein the antisens oligonucleotide is in a concentration from about 0.40 mg/ml to about 2 mg/ml and the use thereof for preventing, stabilizing and/or inhibiting blood and lymph vascularization.

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21-06-2012 дата публикации

Targeting agent to newly formed blood vessels

Номер: US20120156132A1
Принадлежит: Fujifilm Corp, KYOTO UNIVERSITY

It is an object of the present invention to provide a targeting agent that enables drug delivery to a neovascular site and the imaging of such a neovascular site, utilizing the effect of the agent to accumulate in the neovascular site. The present invention provides a targeting agent to a neovascular site, which comprises a gelatin-like protein.

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21-06-2012 дата публикации

Microbubbles and methods for oxygen delivery

Номер: US20120156300A1

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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21-06-2012 дата публикации

Pharmaceutical glp-1 compositions having an improved release profile

Номер: US20120157382A1
Принадлежит: Hoffmann La Roche Inc

This invention relates to sustained release liquid pharmaceutical compositions containing a peptide analogue of glucagon-like peptide-1 or salts thereof having an improved release profile. The invention also relates to methods for preparing such compositions.

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28-06-2012 дата публикации

Angiogenically effective unit dose of fgf and method of administering

Номер: US20120165245A1
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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28-06-2012 дата публикации

Tetrahydroquinoxaline urea derivatives, preparation thereof, and therapeutic use thereof

Номер: US20120165337A1
Принадлежит: SANOFI SA

The invention relates to compounds of formula (I), where: A is a bond, an oxygen atom, or an -CH 2 — group; Ar 1 is a phenyl or heteroaryl group; Ar 2 is a phenyl, heteroaryl, or heterocycloalkyl group; R 1a,b,c and R2a,b,c are a hydrogen or halogen atom, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally substituted by one or more halogen atoms, or an —OR 5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR 6 R 7 , —CO-halogenoalkyl, —COOR 5 , alkyl-COOR 5 , —O-alkyl-COOR 5 , —SO 2 -alkyl, —SO 2 -cycloalkyl, —SO 2 -alkyl-cycloalkyl, —SO 2 -alkyl-OR 5 , —SO 2 -alkyl-COOR 5 , —SO 2 -alkyl-NR 6 R 7 , —SO 2 -halogenoalkyl, alkyl-SO 2 -alkyl, —SO 2 —NR 6 R 7 , —SO 2 -alkyl-O-alkyl-OR 5 , —CONR 6 R 7 , -alkyl-CONR 6 R 7 , or -alkyl-NR 6 R 7 group, or further R 1a , R 1b , and R 1c are bonded to R 2a , R 2b , R 2c , respectively, as well as to the carbon atom having same, and are -alkyl-O—; R 3 is a hydrogen atom or an alkyl group; R 4 is a ONR 6 R 7 group, a hydroxyalkyl group substituted by a halogenoalkyl group, or an lkyl-NH—SO 2 -alkyl, NH—SO 2 -alkyl, —O—SO 2 —NR 6 R 7 , -alkyl-CO—NR 6 R 7 , —O-alkyl-CO—NR 6 R 7 , -alkyl-NR 6 R 7 , —O—CO—NR 6 R 7 , -alkyl-heteroaryl, a heteroaryl group optionally substituted by an alkyl, alkoxy-imino, or —NH—NH—CO-alkyl group, with the proviso that R 4 is in the cis position when it is the ONR 6 R 7 group and that R 6 and R 7 are each hydrogen, or an lkyl or lkyl-phenyl group; R 5 is hydrogen, an lkyl group, or lkyl-phenyl; R 6 and R 7 , identical or different, are each a hydrogen atom, an alkyl group, alkoxy, or an alkyl-phenyl group; and R 8 is a hydrogen atom or an O 2 -alkyl group, or a group of formula -Het, where B can be absent or be a bond, an oxygen atom, or a O— or O 2 —(CH 2 ) n group, with n being equal to 0, 1, or 2, and where Het is a heteroaryl or heterocycloaryl optionally substituted by the alkyl, —SO 2 -alkyl, and —COOR 5 groups. ...

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05-07-2012 дата публикации

Arginase Inhibitors and Methods of Use Thereof

Номер: US20120171116A1
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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12-07-2012 дата публикации

Stable combinations of amlodipine besylate and benazepril hydrochloride

Номер: US20120177706A1
Автор: Fanny Leska, Mali Kadosh
Принадлежит: Teva Pharmaceutical Industries LTD

The present invention provides a pharmaceutical composition comprising benazepril and amlodipine wherein the benazepril and the amlodipine are not physically separated from one another, and methods for making the same.

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12-07-2012 дата публикации

Cyanoisoquinoline compounds and methods of use thereof

Номер: US20120178755A1
Принадлежит: Fibrogen Inc

The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions. The cyanoisoquinoline compounds of the invention have the following structure:

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12-07-2012 дата публикации

Styryl-triazine derivatives and their therapeutical applications

Номер: US20120178758A1
Принадлежит: California Capital Equity LLC

The invention provides Styryl-Triazine derivatives, and further provides methods of using these compounds to modulate protein kinases and to treat protein kinase mediated diseases.

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19-07-2012 дата публикации

Pharmaceutical composition containing as an active ingredient 5-methyl-1-phenyl-2-(1h)-pyridone

Номер: US20120183615A1
Принадлежит: Shionogi and Co Ltd

A tablet characterized by comprising 5-methyl-1-phenyl-2-(1H)-pyridone as the main ingredient and, based on the main ingredient, 10 to 50 wt. % excipient, 5 to 40 wt. % disintegrator, 1 to 10 wt. % binder, 0.5 to 5 wt. % lubricant, 2 to 6 wt. % coating basis, and 0.05 to 3 wt. % light-shielding agent, wherein the odor or bitterness of the 5-methyl-1-phenyl-2-(1H)-pyridone is masked and the light stability is improved.

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19-07-2012 дата публикации

[1,4]-benzodiazepines as vasopressin v2 receptor antagonists

Номер: US20120184537A1
Принадлежит: Shire Movetis NV

The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the invention are directed to the use of said [1,4]-benzodiazepine derivatives in therapy based on the capability of said compounds to interfere with the binding of the peptide hormone, vasopressin, to its receptors. In particular as vasopressin V2 receptor antagonists and therefore useful for treating involving increased vascular resistance, cardiac insufficiency, and water retention.

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19-07-2012 дата публикации

Heart-slowing drug containing short-acting beta-blocker as teh active ingredient

Номер: US20120184545A1
Принадлежит: Ono Pharmaceutical Co Ltd

The present invention relates to an agent which slows down the heart rate which has an excellent controlling ability in diagnostic imaging comprising a short-acting β-blocker (e.g. landiolol hydrochloride or esmolol hydrochloride). The short-acting β-blocker has a property of slowing down the heart rate and it can temporarily suppress the tachycardia at diagnosis. According to the dose and the method of administration, it can control the period for the heart rate adjustment. Also, the present invention relates to a diagnostic imaging auxiliary comprising a short-acting β-blocker as active ingredient.

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26-07-2012 дата публикации

Angiogenesis inhibitors

Номер: US20120190659A1

Compounds of Structural Formula I or pharmaceutically acceptable salts thereof, are effective inhibitors of angiogenesis:

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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
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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09-08-2012 дата публикации

Methods and Devices for Sustained In-Vivo Release Of an Active Agent

Номер: US20120201800A1
Принадлежит: Aciont Inc

The present invention includes methods and devices for providing sustained in-vivo release of an active agent to a subject. In some aspects, such release may be achieved by reacting an active agent in-vivo with a depot forming agent in order to form a sustained release active agent depot inside the subject. The depot can then release the active agent over a sustained period of time.

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09-08-2012 дата публикации

Production of encapsulated nanoparticles at commercial scale

Номер: US20120202694A1
Принадлежит: Iceutica Pty Ltd

The present invention relates to methods for producing particles of a biologically active material using dry milling processes as well as compositions comprising such materials, medicaments produced using said biologically active materials in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of said biologically active materials administered by way of said medicaments.

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09-08-2012 дата публикации

Novel salts and polymorphs of desazadesferrithiocin polyether analogues as metal chelation agents

Номер: US20120202857A1
Принадлежит: FerroKin BioScience Inc

Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.

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23-08-2012 дата публикации

Compositions and methods for therapeutic membrane repair

Номер: US20120213737A1

Disclosed herein are compositions comprising PTRF polypeptides, nucleic acids, and PTRF binding proteins useful for tissue regeneration and the treatment and prevention of disorders relating to cell membrane damage and repair.

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23-08-2012 дата публикации

Cardiomyocytes and methods of producing and purifying cardiomyocytes

Номер: US20120213748A1
Автор: Gabriel Nistor
Принадлежит: Individual

The invention provides methods for producing a culture of cardiomyocytes and cultures of cardiomyocytes. Exemplary methods of producing and cultures of cardiomyocytes include a population of cells including cells having spontaneous and periodic electrical activity, and/or including nodal, sino-atrial or pacemaker cells; immature cardiomyocytes (cardiomyoblasts); mature contractile cardiomyocytes; or a mixed population of two or more of such cells.

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23-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120214794A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula I-A or I-B: wherein HY, G 1 , G 2 , R 2 , R 12 , W 1 , W 2 , n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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06-09-2012 дата публикации

Antibiotic formulations, unit doses, kits, and methods

Номер: US20120225835A1
Принадлежит: Bayer Healthcare AG

An aqueous or powder composition includes anti-gram-negative antibiotic or salt thereof being present at an amount ranging from about 100 mg/ml to about 200 mg/ml. Another aqueous or powder composition includes anti-gram-positive antibiotic or salt thereof being present at a concentration ranging from about 0.6 to about 0.9 of the water solubility limit, at 25° C. and 1.0 atmosphere, of the anti-gram-positive antibiotic or salt thereof. Other embodiments include unit doses, kits, and methods.

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06-09-2012 дата публикации

Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors

Номер: US20120225875A1
Принадлежит: Merck Patent GmBH

Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1 , are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

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13-09-2012 дата публикации

Polypeptides that bind tissue inhibitor of metalloproteinase type three (timp-3), compositions and methods

Номер: US20120231013A1
Принадлежит: AMGEN INC

The present invention relates to TIMP-3 binding compositions, methods of producing such compositions, and methods of using such compositions, including in the treatment of various conditions.

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13-09-2012 дата публикации

Novel compounds and therapeutic use thereof for protein kinase inhibition

Номер: US20120232082A1
Автор: Zhanggui Wu
Принадлежит: Individual

Novel compound having the following formula: (I) wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.

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20-09-2012 дата публикации

Combretum laurifolium mart. extract and methods of extracting and using such extract

Номер: US20120237619A1
Принадлежит: SelvaMedica LLC

A method of inhibiting COX-2, inhibiting NF-Kappa B activation, treating inflammation, or treating cancer may comprise administering a therapeutically effective amount of an extract of Combretum laurifolium Mart. to a patient. A medicament as described herein may comprise a pharmaceutically acceptable vehicle and a therapeutically effective amount of an extract of Combretum laurifolium Mart. suspended in the vehicle. A method of making an extract of Combretum laurifolium Mart. may comprise creating a component solution by treating Combretum laurifolium Mart. material with an extractor and a solvent and producing an extract by at least partially removing liquid from the component solution. An extract of Combretum laurifolium Mart. may comprise components extracted using various solvents.

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20-09-2012 дата публикации

Antithrombotic dual inhibitors comprising a biotin residue

Номер: US20120238512A1
Принадлежит: MSD Oss BV

The present invention relates compounds of the formula (I) oligosaccharide-spacer-A (I), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising two to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is an essentially pharmacologically inactive flexible linking residue having a chain length of 10 to 70 atoms; A is the residue —CH[NH—SO 2 —R 1 ] [CO—NR 2 —CH(4-benzamidine)-CO—NR 3 R 4 ], wherein R1 is phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, (iso)quinolinyl, tetrahydro(iso)quinolinyl, 3,4-dihydro-1H-isoquinolinyl, chromanyl or the camphor group, which groups may optionally be substituted with one or more substituents selected from (1-8C)alkyl or (1-8C)alkoxy; and wherein R 2 and R 3 are independently H or (1-8C)alkyl; R 4 is (-8C)alkyl or (3-8C)cycloalkyl; or R 3 and R 4 together with the nitrogen atom to which they are bonded are a nonaromatic (4-8)membered ring optionally containing another heteroatom, the ring optionally being substituted with (1-8C)alkyl or SO2-(I-8C)alkyl; or a pharmaceutically acceptable salt thereof a prodrug or solvate thereof; wherein the compound of formula I further comprises at least one covalent bond with a biotin residue or an analogue thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombosis or other thrombin-related diseases. The antithrombotic activity of the compound of this invention can be neutralized in case of emergency upon administration of avidin, streptavidin and analogues thereof having high biotin affinity.

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27-09-2012 дата публикации

Polypeptides having modulatory effects on cells

Номер: US20120245092A1
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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27-09-2012 дата публикации

Oxadiazole inhibitors of leukotriene production

Номер: US20120245162A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 -R 5 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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04-10-2012 дата публикации

Co-Administration of An Agent Linked to an Internalization Peptide With an Anti-Inflammatory

Номер: US20120252731A1
Принадлежит: NoNO Inc

The invention provides methods of delivering pharmacologic agents linked to an internalization peptide, in which an inflammatory response inducible by the internalization peptide is inhibited by co-administration of an anti-inflammatory or by linking the internalization peptide to biotin or similar molecule. Such methods are premised in part on the results described in the examples whereby administration of a pharmacological agent linked to tat at high dosages is closely followed by an inflammatory response, which includes mast cell degranulation, histamine release and the typical sequelae of histamine release, such as redness, heat, swelling, and hypotension.

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04-10-2012 дата публикации

Oral lysophilisates containing pvp/va

Номер: US20120252795A1
Автор: Thanh-Tam Nguyen
Принадлежит: Cephalon France SAS

The present invention relates to novel oral pharmaceutical compositions in lyophilized form, in which the dissolution and the bioavailability of the active ingredient that they contain are improved. The compositions according to the invention comprise in particular a polyvinyl acetate/polyvinylpyrrolidone copolymer. The oral lyophilisates according to the invention are particularly suitable for the production of medicaments based on active ingredients which have low solubility or very low solubility in water or which are virtually insoluble in water.

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18-10-2012 дата публикации

Coating Comprising An Elastin-Based Copolymer

Номер: US20120263759A1
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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01-11-2012 дата публикации

Method of Treatment and Screening Method

Номер: US20120276012A1
Принадлежит: Oxford University Innovation Ltd

A method for the prevention or treatment of a cardiovascular disease comprising increasing the intracellular creatine concentration in myocardial cells, in particular by up-regulating the creatine transporter. Also described are screening methods for identifying substances to be used in the prevention or treatment of a cardiovascular disease.

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01-11-2012 дата публикации

Methods of Treating a Hyperproliferative Disorder or Inhibiting Cell Growth in a Mammal

Номер: US20120277277A1
Принадлежит: Array Biopharma Inc

Disclosed are methods for inhibiting abnormal cell growth or treating hyperproliferative diseases in mammals, comprising administering to a mammal in heed thereof a pharmaceutical composition comprising 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxy-ethoxy)-amide, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of an anti-tumour agent or in combination with radiation therapy.

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08-11-2012 дата публикации

Compounds with Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof

Номер: US20120282180A1
Принадлежит: Siemens Medical Solutions USA Inc

The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the inhibitors of matrix-metalloproteinases (MMPs) of the invention and of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention.

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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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08-11-2012 дата публикации

Methods and compositions for the induction of hypothermia

Номер: US20120282227A1
Автор: Laurence M. Katz

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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15-11-2012 дата публикации

Rare earth nanoparticles

Номер: US20120288535A1

This document provides methods and materials related to rare earth particles such as rare earth nanorods (e.g., inorganic lanthanide hydroxide nanorods). For example, rare earth (e.g., lanthanide) particles such as europium hydroxide nanorods, methods and materials for making rare earth particles (e.g., europium hydroxide nanorods), and methods and materials for using rare earth particles (e.g., europium hydroxide nanorods) as an imaging agent and/or to promote angiogenesis are provided.

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15-11-2012 дата публикации

Kinase inhibitors useful for the treatment of proliferative diseases

Номер: US20120289540A1
Принадлежит: Deciphera Pharmaceuticals LLC

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

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