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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 115982. Отображено 100.
05-01-2012 дата публикации

Yeast ectopically expressing abnormally processed proteins and uses therefor

Номер: US20120003243A1

Disclosed are yeast ectopically expressing abnormally processed proteins and methods of screening to identify compounds that modulate the function of such abnormally processed proteins in yeast. Compounds identified by such screens can be used to treat or prevent diseases associated with abnormally processed proteins or protein misfolding. Such diseases include Parkinson's Disease, Parkinson's Disease with accompanying dementia, Lewy body dementia, Alzheimer's disease with Parkinsonism, and multiple system atrophy.

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05-01-2012 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20120004216A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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05-01-2012 дата публикации

Organic compounds

Номер: US20120004247A1
Принадлежит: NOVARTIS AG

A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R 1 , R 2 and R 3 are as defined herein.

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05-01-2012 дата публикации

New ccr2 receptor antagonists and uses thereof

Номер: US20120004252A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.

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12-01-2012 дата публикации

Modified Fc Molecules

Номер: US20120009205A1
Принадлежит: AMGEN INC

Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them. A DNA encoding the inventive composition of matter, an expression vector containing the DNA, and a host cell containing the expression vector are also disclosed.

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12-01-2012 дата публикации

Modified Virus Vectors and Methods of Making and Using the Same

Номер: US20120009268A1

The present invention provides AAV capsid proteins (VP1, VP2 and/or VP3) comprising a modification in the amino acid sequence in the three-fold axis loop 4 and virus capsids and virus vectors comprising the modified AAV capsid protein. In particular embodiments, the modification comprises a substitution of one or more amino acids at amino acid positions 585 to 590 (inclusive) of the native AAV2 capsid protein sequence or the corresponding positions of other AAV capsid proteins. The invention also provides methods of administering the virus vectors and virus capsids of the invention to a cell or to a subject in vivo.

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12-01-2012 дата публикации

Recombinant surfactant protein d compositions and methods of use thereof

Номер: US20120010126A1
Принадлежит: Medical Research Council

We describe an rspd(n/CRD) polypeptide, fragment, homologue, variant or derivative thereof for use in a method of treatment or prophylaxis of a disease. A method of treating an individual suffering from a disease or preventing the occurrence of a disease in an individual is also described, in which the method comprises administering to the individual a therapeutically or prophylactically effective amount of an rspd (n/CRD) polypeptide, fragment, homologue, variant or derivative thereof. Preferably, the rspd (n/CRD) polypeptide and nucleic acid comprise SEQ ID NO: 1 and SEQ ID NO: 2, respectively.

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19-01-2012 дата публикации

Methods and compositions for cns delivery of heparan n-sulfatase

Номер: US20120014936A1
Принадлежит: Shire Human Genetics Therapies Inc

The present invention provides, among other things, compositions and methods for CNS delivery of lysosomal enzymes for effective treatment of lysosomal storage diseases. In some embodiments, the present invention includes a stable formulation for direct CNS intrathecal administration comprising a heparan N-sulfatase (HNS) protein, salt, and a polysorbate surfactant for the treatment of Sanfilippo Syndrome Type A.

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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

PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS

Номер: US20120014989A1
Принадлежит: Incyte Corp

The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

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19-01-2012 дата публикации

Modified release formulations containing drug-ion exchange resin complexes

Номер: US20120015030A1
Автор: Ketan Mehta, Yu-Hsing Tu
Принадлежит: Tris Pharma Inc

A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.

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19-01-2012 дата публикации

Enterically coated cysteamine, cystamine and derivatives thereof

Номер: US20120015038A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The disclosure provides oral cysteamine and cystamine formulations useful for treating cystinosis and neurodegenerative diseases and disorders. The formulations provide controlled release compositions that improve quality of life and reduced side-effects.

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19-01-2012 дата публикации

Complement receptor 2 targeted complement modulators

Номер: US20120015871A1

Modulation of the complement system represents a therapeutic modality for numerous pathologic conditions associated with complement activation. In a strategy to prepare complement inhibitors that are targeted to sites of complement activation and disease, compositions comprising a complement inhibitor linked to complement receptor (CR) 2 are disclosed. The disclosed are compositions can be used in methods of treating pathogenic diseases and inflammatory conditions by modulating the complement system.

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19-01-2012 дата публикации

Sulfone Compounds Which Modulate The CB2 Receptor

Номер: US20120015988A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

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19-01-2012 дата публикации

Enzymes and methods for producing omega-3 fatty acids

Номер: US20120016144A1
Принадлежит: Individual

The present invention relates generally to the field of recombinant fatty acid synthesis, particularly in transgenic plants. The application describes genes involved in fatty acid synthesis and provides methods and vectors for the manipulation of fatty acid composition of plant oils. In particular, the invention provides constructs for achieving the integration of multiple heterologous genes involved in fatty acid synthesis into the plant genome, such that the resulting plants produce altered levels of polyunsaturated fatty acids. Also described are methods for enhancing the expression of fatty acid biosynthesis enzymes by co-expressing a silencing suppressor within the plant storage organ.

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26-01-2012 дата публикации

Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System

Номер: US20120020915A1

Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.

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26-01-2012 дата публикации

Genetically engineered clostridial genes, proteins encoded by the engineered genes, and uses thereof

Номер: US20120021002A1
Принадлежит: New York University NYU

The present invention relates to an isolated Clostridial neurotoxin propeptide having a light chain region, a heavy chain region, where the light and heavy chain regions are linked by a disulfide bond, and an intermediate region connecting the light and heavy chain regions. An isolated nucleic acid molecule encoding a Clostridial neurotoxin propeptide is also disclosed. Also disclosed is an isolated, physiologically active Clostridial neurotoxin produced by cleaving a Clostridial neurotoxin propeptide, a vaccine or antidote thereof, and methods of immunizing against or treating for toxic effects of Clostridial neurotoxins. Methods of expressing recombinant physiologically active Clostridial neurotoxins are also disclosed. Also disclosed is a chimeric protein having a heavy chain region of a Clostridial neurotoxin and a protein with therapeutic functionality. A treatment method is also disclosed.

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26-01-2012 дата публикации

Garcinia Mangostana L. and Iridoid Based Formulations

Номер: US20120021079A1
Принадлежит: Individual

Embodiments of the invention relate to fortified food and dietary supplement products, which may be administered to produce desirable physiological improvement. In particular, embodiments of the invention relate to the administration of products enhanced with Garcinia mangostana L. and iridoids.

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26-01-2012 дата публикации

Derivatives of n-(arylamino)sulfonamides as inhibitors of mek

Номер: US20120022076A1
Принадлежит: Individual

This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.

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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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02-02-2012 дата публикации

Hk1-binding proteins

Номер: US20120027686A1
Принадлежит: Dyax Corp

The invention features hK1 binding polypeptides as well as compositions comprising such polypeptides and methods of making and using such polypeptides.

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02-02-2012 дата публикации

Natural marine source phospholipids comprising polyunsaturated fatty acids and their applications

Номер: US20120028922A1
Автор: Fotini Sampalis
Принадлежит: Individual

A phospholipid extract from a marine or aquatic biomass possesses therapeutic properties. The phospholipid extract comprises a variety of phospholipids, fatty acid, metals and a novel flavonoid.

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02-02-2012 дата публикации

Pyrazole compounds as crth2 antagonists

Номер: US20120028938A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L 1 , L 2 , X, L 3 , Y, R 1 and R 2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.

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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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02-02-2012 дата публикации

Pharmaceutical compositions containing fluorinated or perfluorinated carboxylic acids

Номер: US20120029079A1
Принадлежит: CXR Biosciences Ltd

The molecules of formula (I) are useful in treating diabetes, obesity, hypercholesterolaemia, hyperlipidaemia, cancer, inflammation or other conditions in which modulation of lipis of eicosanoid status or functions may be desirable. Formula (I): Z 1 —Z 1 —Z 2 wherein a) Z 1 represents CO 2 H or a derivative thereof; b) Z 2 represents F, H, —CO 2 H or a derivative thereof; and c) X represents fluorinated alkylene; or a solvate thereof, for example a perfluorinated fatty acid or derivative thereof.

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09-02-2012 дата публикации

Treatment of neurotrophic factor mediated disorders

Номер: US20120034193A1
Принадлежит: Phytopharm Ltd

An agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone and glycosylated forms thereof is used to induce self-regulated homeostasis of neurotrophic factors (NFs), for example BDNF and/or GDNF, NFs with limited and manageable side effects in a subject, by modulating NFs in a non-toxic manner under homeostatic control. An effective amount of at least one such agent is administered to the subject, particularly in the treatment or prevention of a range of NF-mediated disorders, particularly neurological, psychiatric, inflammatory, allergic, immune and neoplastic disorders, and in the restoration or normalisation of neuronal and other function in or in relation to any damaged or abnormal tissue, including when assisting tissue (for example, skin, bone, eye and muscle) healing and general skin, bone, eye and muscle health.

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09-02-2012 дата публикации

Compositions and methods for the treatment of immune related diseases

Номер: US20120035073A1
Принадлежит: Individual

The present invention relates to compositions containing novel proteins and methods of using those compositions for the diagnosis and treatment of immune related diseases.

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09-02-2012 дата публикации

Glycolipids as treatment for disease

Номер: US20120035120A1
Автор: Shawn Defrees
Принадлежит: Seneb Biosciences Inc

This invention provides compounds, compositions, and methods for treating a disorder selected from cancer, hyperinsulinemia, hypoglycemia, hyperinsulinemia with hypoglycemia, atypical Parkinson's disease, Huntington's disease, multiple systems atrophy, GM3 synthase deficiency, GM2 synthase deficiency or tauopathy.

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09-02-2012 дата публикации

Substituted dihydropyrazolones and their use

Номер: US20120035151A1
Принадлежит: Bayer Pharma AG

The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.

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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

Plasmalogen compounds, pharmaceutical compositions containing the same and methods for treating diseases of the aging

Номер: US20120035250A1
Принадлежит: Phenomenome Discoveries Inc

Described herein are routes of synthesis and therapeutic uses of 1-alkyl, 2-acyl glycerol derivatives of formula I: which when administered to mammalian biological systems result in increased cellular concentrations of specific sn-2 substituted ethanolamine plasmalogens independent of the ether lipid synthesis capacity of the system. Elevating levels of the specific sn-2 substituted species in this way can cause lowering of membrane cholesterol levels and the lowering of amyloid secretion. These compounds can be used for the treatment or prevention of diseases of aging associated with increased membrane cholesterol, increased amyloid, and decreased plasmalogen levels, such as neurodegeneration (including Alzheimer's disease, Parkinson's disease and age-related macular degeneration), cognitive impairment, dementia, cancer (e.g. prostate, lung, breast, ovarian, and kidney cancers), osteoporosis, bipolar disorder and vascular diseases (such as atherosclerosis, hypercholesterolemia).

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16-02-2012 дата публикации

Combination of pilocarpin and methimazol for treating charcot-marietooth disease and related disorders

Номер: US20120040940A1
Принадлежит: Pharnext SA

The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related peripheral neuropathies. More particularly, the invention relates to combined therapies for treating said disease by affecting simultaneously muscarinic receptor signaling and thyroid hormone pathway in a subject.

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16-02-2012 дата публикации

Thiadiazole and oxadiazole derivatives, preparation thereof and therapeutic use thereof

Номер: US20120040984A1
Принадлежит: SANOFI SA

The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.

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16-02-2012 дата публикации

Method of activating regulatory t cells with alpha-2b adrenergic receptor agonists

Номер: US20120041031A1
Принадлежит: Allergan Inc

Disclosed herein is a method of upregulating regulatory T-cells, and treating diseases that would benefit from such upregulation, by administering an alpha 2 receptor agonist.

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23-02-2012 дата публикации

Engineered anti-il-13 antibodies, compositions, methods and uses

Номер: US20120045438A1
Принадлежит: Centocor Ortho Biotech Inc

The present invention relates to engineered antibodies immuno specific for human interleukin-13 (IL-13) protein or fragment thereof, as well as methods of making and using thereof, including therapeutic indications.

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23-02-2012 дата публикации

TNF-alpha Antagonists Containing IGFBP5

Номер: US20120046217A1

The present invention relates to: TNF-α antagonists containing IGFBP5 protein, variants thereof, or fragments thereof; and the use of the TNF-α antagonists. More specifically, the present invention relates to: a polynucleotide encoding the protein, variants thereof, or fragments thereof; a vector containing the polynucleotide; a transformant containing the vector; and a method for screening a therapeutic agent for TNF-α overexpression-related diseases by checking whether the mutual reaction thereof is facilitated after treating with candidates to the cell expressing the IGFBP5 protein, variants thereof, or fragments thereof, and the TNER1.

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23-02-2012 дата публикации

Treatment of dystrophin family related diseases by inhibition of natural antisense transcript to dmd family

Номер: US20120046345A1
Принадлежит: OPKO CURNA LLC

The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Dystrophin family, in particular, by targeting natural antisense polynucleotides of Dystrophin family. The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of DMD family.

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01-03-2012 дата публикации

Therapeutic peptide-polymer conjugates, particles, compositions, and related methods

Номер: US20120052097A1
Принадлежит: Cerulean Pharma Inc

Described herein are conjugates (e.g., therapeutic peptide-polymer conjugates and protein-polymer conjugates) and particles, which can be used, for example, in the treatment of a disorder such as cancer. Also described herein are mixtures, compositions and dosage forms containing the particles, methods of using the particles (e.g., to treat a disorder), kits including the conjugates (e.g., therapeutic peptide-polymer conjugates and protein-polymer conjugates) and particles, methods of making the conjugates (e.g., therapeutic peptide-polymer conjugates and protein-polymer conjugates) and particles, methods of storing the particles and methods of analyzing the particles.

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01-03-2012 дата публикации

Tri-cyclic pyrazolopyridine kinase inhibitors

Номер: US20120053187A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.

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08-03-2012 дата публикации

Novel kinase modulators

Номер: US20120059001A1

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

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15-03-2012 дата публикации

Delivery system with scaffolds

Номер: US20120063997A1
Принадлежит: REGENTEC Ltd

An injectable, agent delivery system comprising a composition comprising: (i) an injectable scaffold material comprising discrete particles, which are capable of interacting to form a scaffold; and (ii) a carrier comprising an agent for delivery. The product can have a pharmaceutical use or use in cosmetic surgery; in particular it can be used in tissue regeneration or reconstruction. The agent for delivery may be a therapeutically, prophylactically or diagnostically active substance.

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15-03-2012 дата публикации

Method for Treating Psoriatic Arthritis by Administering an Anti-IL-12 Antibody

Номер: US20120063998A1
Принадлежит: Individual

Isolated anti-IL-12 antibodies, nucleic acids encoding antibodies or antibody portions, vectors, host cells, and methods of making are useful for production of antibody or portions for treating and/or diagnosing IL-12 related conditions, diseases, and disorders, such as psoriatic arthritis.

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15-03-2012 дата публикации

Isotopologues of thalidomide

Номер: US20120064004A1
Принадлежит: Celgene Corp

Provided herein are thalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.

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15-03-2012 дата публикации

Therapeutic use of anti-cs1 antibodies

Номер: US20120064083A1
Принадлежит: Abbott Biotherapeutics Corp

The present invention is directed to antagonists of CS1 that bind to and neutralize at least one biological activity of CS1. The invention also includes a pharmaceutical composition comprising such antibodies or antigen-binding fragments thereof. The present invention also provides for a method of preventing or treating disease states, including autoimmune disorders and cancer, in a subject in need thereof, comprising administering into said subject an effective amount of such antagonists.

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15-03-2012 дата публикации

Compounds and their uses 708

Номер: US20120065214A1
Принадлежит: AstraZeneca AB

The present invention relates to pyrazinone derivatives of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

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22-03-2012 дата публикации

Methods of treating inflammation

Номер: US20120070449A1
Принадлежит: Yeda Research and Development Co Ltd

A method of treating an inflammation in a subject in need thereof is disclosed. The method comprising administering to the subject an agent capable of down-regulating an activity or expression of CD151 in a lymphocyte, with the proviso that the agent is not CCL2, thereby treating the inflammation.

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22-03-2012 дата публикации

Method of extraction from withania somnifera and one or more fractions containing pharmacologically active ingredients obtained therefrom

Номер: US20120070521A1
Принадлежит: Bio Ved Pharmaceuticals PVT Ltd

A method of obtaining one or more fractions from a plant material of Withania somnifera (WS) is disclosed. The method includes subjecting the plant material to hydro-alcoholic extraction in presence of a water-insoluble solvent to obtain at least one extract. The method further includes subjecting the at least one extract obtained from the hydro-alcoholic extraction to at least one of de-pigmentation, de-fatting and detoxification process to obtain the one or more fractions. The one or more fractions thus obtained contain Withaferin A in a concentration greater than concentrations of other pharmacologically active ingredients present in the one or more fractions. The one or more fraction thus obtained and one or more compositions containing the one or more fractions are effective in inhibiting proliferation of mammalian cancerous cells.

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22-03-2012 дата публикации

Substituted pyridine derivatives, pharmaceutical compositions, and methods of use to treat oxidative stress

Номер: US20120071505A1
Принадлежит: High Point Pharnaceuticals LLC

Substituted pyridine derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted pyridine derivative, and methods of use in treating inflammation are provided. The substituted pyridine derivatives may control of the activity or the amount or both the activity and the amount of heme-oxygenase.

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22-03-2012 дата публикации

Tetrazole Compounds Which Selectively Modulate The CB2 Receptor

Номер: US20120071529A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

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22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Принадлежит: Aragon Pharmaceuticals Inc

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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29-03-2012 дата публикации

Composition with improved bioavailability of saponin and method for improving the bioavailability of saponin (as amended)

Номер: US20120076874A1
Принадлежит: Amorepacific Corp

The present invention relates to a ginseng mixed composition with improved bioavailability of saponin. Further, the present invention relates to a method for improving saponin bioavailability of a subject comprising: administering to the subject an effective amount of at least one extract selected from a Schizandra chinensis extract and a Liriope platyphylla extract that improves saponin bioavailability in the subject.

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29-03-2012 дата публикации

Methods for Identifying Autophagy Inducing Compounds

Номер: US20120077705A1
Автор: Junying Yuan
Принадлежит: Harvard College

This invention pertains to screening methods for identifying autophagy inducing compounds.

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29-03-2012 дата публикации

Sulfonamide, sulfamate, and sulfamothioate derivatives

Номер: US20120077814A1
Принадлежит: Individual

The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.

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29-03-2012 дата публикации

Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors

Номер: US20120077840A1
Принадлежит: Abbott GmbH and Co KG

The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

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29-03-2012 дата публикации

Pharmaceutical product

Номер: US20120077856A1
Принадлежит: Takeda Pharmaceutical Co Ltd

An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II) wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

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29-03-2012 дата публикации

Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response

Номер: US20120077858A1
Принадлежит: Allergan Inc

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R 1 is selected from the group consisting of CO 2 R 7 and CON(R 7 )SO 2 R 7 wherein R 1 , R 2 , R 3 , R 4 , and R 7 are as defined in the specification. The compounds may be administered to treat DP 1 , FP, EP 1 , EP 3 , TP and/or EP 4 receptor mediated diseases or conditions.

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05-04-2012 дата публикации

Stabilized alpha helical peptides and uses thereof

Номер: US20120082636A1
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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05-04-2012 дата публикации

Soluble il-17ra/rc fusion proteins and related methods

Номер: US20120082668A1
Принадлежит: Zymogenetics Inc

Disclosed are antagonists of IL-17A and IL-17F. The antagonists are based on soluble IL-17RA and IL-17RC fusion proteins, including hybrid soluble receptors comprising portions of both IL-17RC and IL-17RA (“IL-17RC/IL-17RA”). Such antagonists serve to block, inhibit, reduce, antagonize or neutralize the activity of IL-17F, IL-17A, or both IL-17A and IL-17F. Also disclosed are methods of using such antagonists for treating disease, particularly inflammatory diseases mediated at least in part by IL-17A and/or IL-17F.

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05-04-2012 дата публикации

Myostatin binding agents

Номер: US20120083442A1
Принадлежит: AMGEN INC

The present invention provides binding agents comprising peptides capable of binding myostatin and inhibiting its activity. In one embodiment the binding agent comprises at least one myostatin-binding peptide attached directly or indirectly to at least one vehicle such as a polymer or an Fc domain. The binding agents of the present invention produced increased lean muscle mass when administered to animals and decreased fat to muscle ratios. Therapeutic compositions containing the binding agents of the present invention are useful for treating muscle-wasting disorders and metabolic disorders including diabetes and obesity.

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05-04-2012 дата публикации

Novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors

Номер: US20120083494A1

The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular alcohol disorder, drug abuse, growth retardation, cachexia, short-, medium-, and/or long term regulation of energy balance, short-, medium-, and/or long term regulation (stimulation and/or inhibition) of food intake, intake of rewarding food, adipogenesis, adiposity and/or obesity, body weight gain and/or reduction, diabetes, diabetes type I, diabetes type II, tumor cell proliferation, inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).

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05-04-2012 дата публикации

Alpha-2b receptor agonist and anticonvulsant compositions for treating chronic pain

Номер: US20120083508A1
Принадлежит: Allergan Inc

Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an alpha-2B receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed.

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12-04-2012 дата публикации

Extended release opioid abuse deterrent compositions and methods of making same

Номер: US20120087982A1
Принадлежит: Acura Pharmaceuticals Inc

This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.

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12-04-2012 дата публикации

Compositions for treating cmt and related disorders

Номер: US20120088744A1
Принадлежит: Pharnext SA

The present invention relates to compositions and methods for the treatment of the Charcot-Marie-Tooth disease and related disorders.

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12-04-2012 дата публикации

Chemically modified small molecules

Номер: US20120088745A1
Принадлежит: Individual

Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.

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12-04-2012 дата публикации

Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same

Номер: US20120088746A1
Принадлежит: PFIZER INC

Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

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12-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120088762A1
Принадлежит: Onyx Therapeutics Inc

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

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12-04-2012 дата публикации

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

Номер: US20120088778A1
Принадлежит: vTvx Holdings I LLC

This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

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19-04-2012 дата публикации

Human artificial chromosome (hac) vector

Номер: US20120093785A1
Принадлежит: Kirin Brewery Co Ltd

The present invention relates to a human artificial chromosome (HAC) vector and a method for producing the same. The present invention further relates to a method for introducing foreign DNA using a human artificial chromosome vector and a method for producing a cell which expresses foreign DNA. Furthermore, the present invention relates to a method for producing a protein.

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19-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120094930A1
Принадлежит: Onyx Therapeutics Inc

Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.

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19-04-2012 дата публикации

Mangiferin-Berberine Salt, Manufacturing Method and Use Thereof

Номер: US20120094941A1
Автор: Houlei Teng, Wei Wu
Принадлежит: Hainan Deze Drug Research Co Ltd

The present invention provides a mangiferin-berberine salt and manufacturing method thereof. Otherwise, the present invention also provides the use of mangiferin-berberine salt as AMPK activator.

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19-04-2012 дата публикации

Egfr inhibitors and methods of treating disorders

Номер: US20120094999A1
Принадлежит: Dana Farber Cancer Institute Inc

The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.

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26-04-2012 дата публикации

Humanized antibodies against light and uses thereof

Номер: US20120100074A1
Принадлежит: Teva Biopharmaceuticals USA Inc

The present invention is directed to antigen-binding polypeptides, or variants or derivatives thereof which specifically bind the LIGHT polypeptide. The invention is also directed to methods of making and using such antibodies specifically in the treatment or diagnosis of immune, inflammatory and malignant diseases or conditions (e.g. inflammatory bowel disease; Crohn's disease, ulcerative colitis, multiple sclerosis, rheumatoid arthritis and transplantation).

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26-04-2012 дата публикации

Pharmaceutical formulations of a substituted diaminopurine

Номер: US20120100213A1
Принадлежит: Signal Pharmaceuticals LLC

Provided herein are pharmaceutical formulations, comprising 4-((9-((3S)-tetrahydro-3-furanyl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)-trans-cyclohexanol, including pharmaceutically acceptable salts, solvates, isomers, isotopologues, tautomers and racemic mixtures thereof, and a pharmaceutically acceptable excipient; and their use for treating or preventing disease.

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26-04-2012 дата публикации

Antibodies having altered effector function and methods for making the same

Номер: US20120100575A1
Принадлежит: BIOGEN IDEC MA INC

The invention provides a method of producing aglycosylated Fc-containing polypeptides, such as antibodies, having desired effector function. The invention also provides aglycosylated antibodies produced according to the method as well as methods of using such antibodies as therapeutics.

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26-04-2012 дата публикации

S1p1 agonists comprising a bicyclic n-containing ring

Номер: US20120101083A1
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds of formula (I) having S1P1 agonist activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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26-04-2012 дата публикации

Thiadiazole derivatives and their use for the treatment of disorders mediated by s1p1 receptors

Номер: US20120101086A1
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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26-04-2012 дата публикации

Compounds

Номер: US20120101123A1
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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26-04-2012 дата публикации

1,2,4-oxadiazol derivatives, their pharmaceutical compositions and their use as sphingosine 1-phosphate 1 receptor agonists

Номер: US20120101124A1
Автор: Feng Ren, Xichen Lin, Yugui Si
Принадлежит: Glaxo Group Ltd

1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.

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03-05-2012 дата публикации

Use of LCAT for Treating Anemia and Red Blood Cell Dysfunction

Номер: US20120107298A1
Принадлежит: Alphacore Pharma LLC

Disclosed are methods for treating conditions characterized by anemia or red blood cells dysfunction by administering an agent that increases the level of endogenous LCAT or LCAT activity. Additionally disclosed are methods of treating conditions wherein red blood cells have reduced function in relation to deformability, oxygenation, increased adhesion and aggregability, reduced nitric oxide function, or decreased life-span, increased free cholesterol, or abnormal phospholipid content. Also disclosed are methods for treating conditions characterized by an abnormal concentration of free cholesterol in red blood cells and methods of normalizing the free cholesterol content of red blood cells.

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03-05-2012 дата публикации

Combinations for the Treatment of Diseases involving Cell Proliferation

Номер: US20120107312A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.

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03-05-2012 дата публикации

Substituted phenoxy n-alkylated thiazolidinediones as estrogen related receptor-alpha modulators

Номер: US20120108571A1
Принадлежит: Individual

The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacia, osteoporosis, Paget's disease, periodontal disease, polymyalgia rheumatica, Reiter's syndrome, repetitive stress injury, hyperglycemia, elevated blood glucose level, and insulin resistance.

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03-05-2012 дата публикации

Pharmaceutical formulation containing gelling agent

Номер: US20120108622A1
Принадлежит: Purdue Pharma LP

Disclosed in certain embodiments is a controlled release oral dosage form comprising a therapeutically effective amount of a drug susceptible to abuse together with one or more pharmaceutically acceptable excipients; the dosage form further including a gelling agent in an effective amount to impart a viscosity unsuitable for administration selected from the group consisting of parenteral and nasal administration to a solubilized mixture formed when the dosage form is crushed and mixed with from about 0.5 to about 10 ml of an aqueous liquid; the dosage form providing a therapeutic effect for at least about 12 hours when orally administered to a human patient.

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03-05-2012 дата публикации

Recombinant il-9 antibodies and uses thereof

Номер: US20120109097A1
Принадлежит: MEDIMMUNE LLC

The present invention provides novel antibodies that immunospecifically bind to an IL-9 polypeptide and compositions comprising said antibodies. The present invention also provides methods and compositions preventing, treating, managing, and/or ameliorating diseases and disorders associated with aberrant expression and/or activity of IL 9 or IL-9 receptor or subunits thereof, autoimmune diseases, inflammatory diseases, proliferative diseases, and infections comprising administration of one or more antibodies thereof that immunospecifically bind to an IL-9 polypeptide. The invention also encompasses methods and compositions for diagnosing, monitoring, and prognosing these disorders. The present invention further relates to articles of manufacture and kits comprising antibodies that immunospecifically bind to an IL-9 polypeptide.

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10-05-2012 дата публикации

Method for treating immune disorders

Номер: US20120114555A1
Принадлежит: IMMUNE SYSTEM THERAPEUTICS LTD

The present invention relates to the treatment of B-cell mediated immune disorders such as rheumatoid arthritis, systemic lupus erythromatomus, diabetes mellitus, and multiple sclerosis. In particular, the present invention relates to the treatment of B-cell mediated immune disorders using antibodies which bind to membrane-bound free light chain expressed on the surface of plasma cell precursors.

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10-05-2012 дата публикации

Compositions, methods and kits for enhancing immune response to a respiratory condition

Номер: US20120114608A1
Принадлежит: Individual

Disclosed herein are compositions for treating a respiratory condition, preferably by enhancing immune response in a mammal, the compositions including a therapeutic amount of a probiotic strain of bacteria and a therapeutic amount of an additional component. Also included are methods of treating a respiratory condition, preferably by enhancing immune response, in a mammal. Kits containing the compositions, and instructions for applying the methods are also included. The method includes orally administering to the mammal a therapeutic amount of a probiotic strain of bacteria and a therapeutic amount of an additional component.

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10-05-2012 дата публикации

TGR5 Modulators and Methods of Use Thereof

Номер: US20120115832A1
Автор: Roberto Pellicciari
Принадлежит: Intercept Pharmaceuticals Inc

The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

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10-05-2012 дата публикации

N,n'-diarylurea compounds and n,n'-diarylthiourea compounds as inhibitors of translation initiation

Номер: US20120115915A1
Принадлежит: Harvard College

Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.

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10-05-2012 дата публикации

Human antibodies derived from immunized xenomice

Номер: US20120117669A1
Принадлежит: Abgenix Inc

Fully human antibodies against a specific antigen can be prepared by administering the antigen to a transgenic animal which has been modified to produce such antibodies in response to antigenic challenge, but whose endogenous loci have been disabled. Various subsequent manipulations can be performed to obtain either antibodies per se or analogs thereof.

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17-05-2012 дата публикации

Dry whole milk preparations containing probiotic micro-organisms

Номер: US20120121561A1
Принадлежит: Nestec SA

The present invention relates to the field of nutrition for young children. In particular, the present invention relates to dry whole milk preparations comprising probiotic micro-organisms to be administered to young children older than 12 months. These probiotic micro-organisms may be non-replicating probiotic micro-organisms such as bioactive heat treated probiotic micro-organisms, for example.

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17-05-2012 дата публикации

Antibodies that immunospecifically bind to b lymphocyte stimulator protein

Номер: US20120121606A1
Принадлежит: Human Genome Sciences Inc

The present invention relates to antibodies and related molecules that immunospecifically bind to B Lymphocyte Stimulator. The present invention also relates to methods and compositions for detecting or diagnosing a disease or disorder associated with aberrant B Lymphocyte Stimulator expression or inappropriate function of B Lymphocyte Stimulator comprising antibodies or fragments or variants thereof or related molecules that immunospecifically bind to B Lymphocyte Stimulator. The present invention further relates to methods and compositions for preventing, treating or ameliorating a disease or disorder associated with aberrant B Lymphocyte Stimulator expression or inappropriate B Lymphocyte Stimulator function comprising administering to an animal an effective amount of one or more antibodies or fragments or variants thereof or related molecules that immunospecifically bind to B Lymphocyte Stimulator.

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17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

Номер: US20120122764A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

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17-05-2012 дата публикации

Tricyclic n-heteroaryl-carboxamide derivatives containing a benzimidazole unit, method for preparing same and their therapeutic use

Номер: US20120122852A1
Принадлежит: Sanofi Aventis France

The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R 1 , R 2 and R 3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.

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17-05-2012 дата публикации

New salts

Номер: US20120122883A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.

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17-05-2012 дата публикации

Combination of curcuminoids and mtor inhibitors for the treatment of tauopathies

Номер: US20120122913A1

Methods, uses, compositions, combinations and kits relating to the decrease of Tau protein levels, and prevention and/or treatment of diseases or disorders associated with Tau protein (Tauophathies), such as Alzheimer's disease, using a curcuminoid and a mammalian target rapamycin (mTOR) inhibitor, are described.

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17-05-2012 дата публикации

Use of Ketogenic Compounds for Treatment of Age-Associated Memory Impairment

Номер: US20120122978A1
Автор: Samuel T. Henderson
Принадлежит: Accera Inc

This invention relates to the field of therapeutic agents for the treatment of Age-Associated Memory Impairment (AAMI). In particular, the present invention utilizes compositions comprising at least one compound capable of elevating ketone body concentrations in a mammal (e.g., ketogenic compounds), administered in an amount effective for treatment or prevention of loss of cognitive function caused by reduced neuronal metabolism in AAMI. In one embodiment, the composition includes medium chain triglycerides (MCT). In another embodiment, the compositions are administered in the presence of carbohydrate. The present invention also relates to oral dosage forms, in particular, a nutritional drink comprising at least one compound capable of elevating ketone body concentrations in a mammal.

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17-05-2012 дата публикации

Process for the preparation of strontium ranelate

Номер: US20120123131A1
Принадлежит: Individual

The present invention relates to an improved process for the synthesis of strontium ranelate or hydrates thereof. More particularly, the present invention relates to an effective process for the preparation of a compound of formula III, which is a useful intermediate in the synthesis of strontium ranelate. wherein R 1 and R 2 represents substituted or unsubstituted linear or branched C 1 -C 6 alkyl group or C 3 -C 12 cyclic group.

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24-05-2012 дата публикации

Thienopyrimidines for pharmaceutical compositions

Номер: US20120128686A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

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24-05-2012 дата публикации

Diagnosis and treatment of autoimmune demyelinating diseases

Номер: US20120128698A1
Принадлежит: F Hoffmann La Roche AG

The present invention concerns the diagnosis and treatment of autoimmune demyelinating diseases, such as multiple sclerosis (MS), by means of a CLM-I agonist.

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