Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 61082. Отображено 100.
05-01-2012 дата публикации

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

Номер: US20120004206A1

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

Подробнее
05-01-2012 дата публикации

N-oxides of 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives useful as nicotinic acetylcholine receptor ligands

Номер: US20120004214A1
Принадлежит: Neurosearch AS

This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy.

Подробнее
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.

Подробнее
12-01-2012 дата публикации

Monoparamunity inducers based on attenuated rabbit myxomaviruses

Номер: US20120009217A1
Автор: Anton Mayr, Barbara Mayr
Принадлежит: Individual

The present invention relates to monoparamunity inducers based on paramunizing viruses or viral components of a myxomavirus strain from rabbits with typically generalizing disease, to a method for the production thereof and to the use thereof as medicaments for the regulatory optimization of the paramunizing activities for the prophylaxis and therapy of various dysfunctions in humans and animals.

Подробнее
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.

Подробнее
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.

Подробнее
19-01-2012 дата публикации

Sustained release of nutrients in vivo

Номер: US20120015039A1
Принадлежит: NEW WORLD PHARMACEUTICALS LLC

Nutritional compositions delivered in vivo in a time controlled manner sustainable over long periods of time, provide enhancing athletic performance, increased hand/eye coordination and concentration on the task at hand.

Подробнее
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.

Подробнее
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.

Подробнее
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.

Подробнее
26-01-2012 дата публикации

Combination of an insulin and a glp-1-agonist

Номер: US20120021978A1
Принадлежит: Sanofi Aventis Deutschland GmbH

The invention relates to a drug comprising at least one insulin and at least one GLP-1 receptor agonist.

Подробнее
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.

Подробнее
26-01-2012 дата публикации

Compositions and Methods for Induced Brown Fat Differentiation

Номер: US20120022500A1
Принадлежит: Dana Farber Cancer Institute Inc

The invention provides methods and compositions for inducing brown fat cell differentiation through modulation of both Prdm1β and C/EBPβ activity and/or expression. Also provided are methods for preventing or treating obesity or an obesity related disorder in a subject through stimulation of both Prdm1β and C/EBPβ expression and/or activity. Further provided are methods for identifying compounds that are capable of modulating both Prdm1β and C/EBPβ expression and/or activity.

Подробнее
02-02-2012 дата публикации

Methods for treating diabetes

Номер: US20120027729A1
Принадлежит: Tulane University

Transplantation of multipotent stromal cells (MSCs) into diabetic mice lowers blood sugar, increases blood insulin levels, increases the number and size of islets, and improves renal pathology. Accordingly, the invention provides methods for treating or preventing diabetes by administering isolated MSCs. The invention also provides methods for treating or preventing complications which arise from diabetes, including diabetic nephropathy, by transplanting isolated MSCs.

Подробнее
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.

Подробнее
02-02-2012 дата публикации

6 Substituted 2, 3,4,5 Tetrahydro-1H-Benzo[d]Azepines as 5-HT2c Receptor Agonist

Номер: US20120028961A1
Принадлежит: Eli Lilly and Co

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is —S—R 14 ; and other substituents are as defined in the specification.

Подробнее
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.

Подробнее
02-02-2012 дата публикации

Compositions for treating or preventing obesity and insulin resistance disorders

Номер: US20120029065A1
Принадлежит: General Hospital Corp, Harvard College

Provided herein are methods and compositions for modulating the activity or level of a sirtuin, thereby treating or preventing obesity or an insulin resistance disorder, such as diabetes in a subject. Exemplary methods comprise contacting a cell with a sirtuin activating compound or an inhibitory compound to thereby increase or decrease fat accumulation, respectively.

Подробнее
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.

Подробнее
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.

Подробнее
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).

Подробнее
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.

Подробнее
16-02-2012 дата публикации

Benzimidazoles which have activity at m1 receptor and their uses in medicine

Номер: US20120041027A1
Принадлежит: Glaxo Group Ltd

Compounds of formula (I) and salts and solvates are provided: wherein Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.

Подробнее
16-02-2012 дата публикации

Method for the manufacture of degarelix

Номер: US20120041172A1
Принадлежит: PolyPeptide Laboratories AS

In a step-wise synthesis of degarelix comprising 0.3% by weight or less of 4-([2(5-hydantoyl)]acetylamino)-phenylalanine analog on (solid support)-NH 2 a step comprises providing a solution of an amino acid or peptide of which the α-amino group is protected by Fmoc; contacting the support with the solution in the presence of reagent for forming a peptide bond between a carboxyl group of the amino acid or peptide and (solid support)-NH 2 ; removing Fmoc by contacting the support with an organic base, in particular piperidine, in an organic solvent. Also disclosed is degarelix of high purity prepared by the method of the invention and the use of Fmoc in the synthesis of degarelix.

Подробнее
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.

Подробнее
23-02-2012 дата публикации

Calcium Formate for Use as a Dietary Supplement

Номер: US20120046252A1
Автор: Hector F. DeLuca
Принадлежит: Individual

A calcium formate composition for oral administration to an individual for the purpose of supplementary dietary calcium is disclosed.

Подробнее
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.

Подробнее
08-03-2012 дата публикации

Anti- integrin antibodies, compositions, methods and uses

Номер: US20120058128A1
Принадлежит: Janssen Biotech Inc

The present invention relates to at least one novel anti-alpha-V subunit antibodies, including isolated nucleic acids that encode at least one anti-alpha-V subunit antibody, alpha-V subunit, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.

Подробнее
08-03-2012 дата публикации

Nutritional composition inducing a postprandial endocrine response

Номер: US20120058938A1
Принадлежит: Nutricia NV

The invention concerns the use of a nutritional composition for the treatment of disorders which are associated with malfunctioning in the uptake and use of food-derived energy in the human body. In particular, the invention concerns the use of a nutritional composition for the treatment of a disorder, which is mediated by a postprandial endocrine or neurological response in a human body, wherein the nutritional composition comprises one or more of a specific protein fraction, a specific carbohydrate fraction and a specific nutritional fiber fraction.

Подробнее
08-03-2012 дата публикации

Neuroprotective iron chelators and pharmaceutical compositions comprising them

Номер: US20120058945A1

Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, e.g., a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, an inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding aging, and prevention and/or treatment of skin aging and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety. The neuroprotective function is imparted to the compound, e.g., by a neuroprotective peptide. A combined antiapoptotic and neuroprotective function is provided by a propargyl group.

Подробнее
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.

Подробнее
08-03-2012 дата публикации

Methods and compositions for modification of a hla locus

Номер: US20120060230A1
Принадлежит: Individual

Disclosed herein are methods and compositions for modulating the expression of a HLA locus or for selectively deleting or manipulating a HLA locus or HLA regulator.

Подробнее
15-03-2012 дата публикации

Crystalline forms of the di-sodium salt of n-(5-chlorosalicyloyl)-8-aminocaprylic acid

Номер: US20120065128A1
Принадлежит: Emisphere Technologies Inc

The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of preparing the same, and methods for facilitating the delivery of active agents with the same.

Подробнее
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.

Подробнее
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.

Подробнее
29-03-2012 дата публикации

Cyclic peptides and uses thereof

Номер: US20120077732A1
Принадлежит: Sydney West Area Health Service SWAHS

The present invention relates to cyclic peptides, comprising alternating D- and L- amino acids and wherein the peptide possesses immunomodulatory activity. The present invention also relates to pharmaceutical compositions comprising the cyclic peptides and to methods for the treatment of disease.

Подробнее
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.

Подробнее
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.

Подробнее
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).

Подробнее
19-04-2012 дата публикации

Implantable liposome embedded matrix composition, uses thereof, and polycaprolactone particles as scaffolds for tissue regeneration

Номер: US20120093914A1
Принадлежит: MOMA THERAPEUTICS

In various embodiments, the present invention describes materials and methods for the local reprogramming of cells in a location where the treatment is applied. The invention can be used to replace lost cells or to restore function to tissue damaged due to disease, injury or genetic defect. In various embodiments, the treatment includes a semisolid hydrogel embedded with liposomes. The liposomes can contain an effector molecule or molecules. When phagocytic cells such as monocytes infiltrate the hydrogel, they encounter the liposomes and incorporate the liposomes carrying the effector molecules into the cells. In some embodiments, the effector molecules can be genetic material encoding the expression of specific proteins such as transcription factors, the expression of which can initiate the reprogramming of the cells. In other embodiments, the effector molecules can induce angiogenesis. In other embodiments, the effector molecules are tumor antigens. The matrix can contain other effector molecules designed to attract specific cells to the matrix. The cells can be released from the matrix as the matrix degrades or by active migration from the matrix. The cells can also remain in the matrix and secret molecules such as proteins and hormones that will diffuse through the matrix material to the surrounding tissue.

Подробнее
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.

Подробнее
19-04-2012 дата публикации

Triglyceride-lowering agent and hyperinsulinism-ameliorating agent

Номер: US20120095043A1
Автор: Taro Aoki, Toru Yokoyama
Принадлежит: Kowa Co Ltd, Nissan Chemical Corp

The present invention is directed to a triglyceride-lowering agent, exhibiting excellent triglyceride-lowering effect and a hyperinsulinemia-ameliorating agent. The triglyceride-lowering agent and hyperinsulinemia-ameliorating agent are characterized by containing a pitavastatin compound, and amlodipine or a salt thereof.

Подробнее
26-04-2012 дата публикации

Regionalised endoderm cells and uses thereof

Номер: US20120100115A1
Принадлежит: University of Edinburgh

The present invention relates to the generation of anterior definitive endoderm (ADE) cells from embryonic stem cells and the differentiation of such cells to, for example, pancreatic or liver cells. The invention also relates to cell lines, cell culture methods, cells markers and the like and their potential uses in a variety of applications.

Подробнее
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.

Подробнее
26-04-2012 дата публикации

Inhibition of secretion from non-neuronal cells

Номер: US20120101027A1
Принадлежит: Syntaxin Ltd

The present invention relates to treatment of disease by inhibition of cellular secretory processes, to agents and compositions therefor, and to manufacture of those agents and compositions. The present invention relates particularly, to treatment of disease dependent upon the exocytotic activity of endocrine cells, exocrine cells, inflammatory cells, cells of the immune system, cells of the cardiovascular system and bone cells.

Подробнее
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.

Подробнее
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.

Подробнее
03-05-2012 дата публикации

INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1

Номер: US20120108578A1

This invention relates to novel compounds of the Formula (I), (Ia 1-10 ), (Ib 1-10 ), (Ic 1-10 ), (Id 1-7 ), (Ie 1-5 ) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.

Подробнее
03-05-2012 дата публикации

N1/n2-lactam acetyl-coa carboxylase inhibitors

Номер: US20120108619A1
Принадлежит: PFIZER INC

The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R 1 , R 2 and R 3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

Подробнее
10-05-2012 дата публикации

Bismuth-containing compounds, coordination polymers, methods for modulating pharmacokinetic properties of biologically active agents, and methods for treating patients

Номер: US20120115823A1
Принадлежит: Synthonics Inc

Bismuth-containing compounds include bismuth and a biologically active agent coordinated to the bismuth. The biologically active agent includes at least one heteroatom configured for coordination with the bismuth. Coordination polymers include a polymer matrix that contains a bismuth-containing compound. Methods for modulating a pharmacokinetic property of a biologically active agent include coordinating the biologically active agent to bismuth to form a bismuth-containing compound, and administering the bismuth-containing compound orally to a patient. Methods for treating Parkinson's disease, methods for treating hypothyroidism, methods for treating ulcerative colitis, and methods for treating cancer each include administering a bismuth-containing compound to a patient.

Подробнее
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.

Подробнее
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.

Подробнее
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.

Подробнее
10-05-2012 дата публикации

Selective inhibitors of cb2 receptor expression and/or activity for the treatment of obesity and obesity-related disorders

Номер: US20120115931A1
Принадлежит: Individual

The invention relates to a method for treating and/or preventing obesity and/or obesity-related disorders by administering to a subject in need thereof a selective inhibitor of cannabinoid type 2 (CB2) receptor expression.

Подробнее
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.

Подробнее
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.

Подробнее
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.

Подробнее
17-05-2012 дата публикации

Pharmaceutical composition for transdermal or transmucous administration

Номер: US20120122829A1
Принадлежит: BESINS Healthcare Luxembourg SARL

The present invention relates to a novel pharmaceutical composition for transdermal or transmucous administration of at least one active substance, and comprising especially a fatty acid as a percutaneous absorption promoter, at least one alcoholic vehicle and also a stabilizer capable of stabilizing the fatty acid in the said pharmaceutical composition.

Подробнее
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.

Подробнее
17-05-2012 дата публикации

Autoantibody production inhibitor

Номер: US20120123099A1
Автор: Masayuki Homma
Принадлежит: Nihon Pharmaceutical Co Ltd

The present invention provides an autoantibody production inhibitor which can specifically suppress the autoantibodies and which can effectively prevent or treat the autoimmune disease of autoantibody type. According to the present invention, there is provided an autoantibody production inhibitor comprising, as an effective ingredient, a fusion protein which consists of a protein (X) containing a site recognized by autoantibodies which are a cause of the autoimmune disease of autoantibody type and a protein (A) containing a fragment which exhibits the antibody-dependent cellular cytotoxicity of the antibody heavy chain constant region.

Подробнее
24-05-2012 дата публикации

Compositions and methods for kinase-mediated cytoprotection and enhanced cellular engraftment and persistence

Номер: US20120128631A1
Автор: Mark A. Sussman

Disclosed are methods of protecting cells, especially non-vascular system, non-hematopoietic cells and tissues, from apoptosis and enhancing their engraftment, survival, and/or persistence by providing enhanced levels of PIM activity for the cell, including PIM-1 activity. Also disclosed are cells that have been engineered to express enhanced levels of PIM kinase, and methods of administering those cells to vertebrates.

Подробнее
24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Принадлежит: Janssen Pharmaceutica NV

The present invention is directed to piperidinyl and piperazinyl derivatives of formula (II) useful as inhibitors of the NPY Y2 receptor, pharmaceutical compositions comprising said compounds, processes for the preparation of said compounds and the use of said compounds for the treatment and/or prevention of disorders, diseases and conditions mediated by the NPY Y2 receptor.

Подробнее
31-05-2012 дата публикации

Organic compounds

Номер: US20120136013A1
Принадлежит: Intra Cellular Therapies Inc

Optionally substituted (5- or 7-amino)-3,4-dihydro-(optionally 4-oxo, 4-thioxo or 4-imino)-1H-pyrrolo[3,4-d]pyrimidin-2(6H)-ones, Compounds of Formula I, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Подробнее
31-05-2012 дата публикации

Fatty acids as anti-inflammatory agents

Номер: US20120136034A1
Принадлежит: University of Pittsburgh

Compounds of formula I and their metabolites are potent mediators of an inflammatory response: (I) where a, b, c, d, e, f, V, W, X, Y, R a , R a′ , R b , R b′ , R c , and R c′ are defined herein. In particular, the compounds of the invention are candidate therapeutics for treating inflammatory conditions.

Подробнее
31-05-2012 дата публикации

Substituted acylanilides and methods of use thereof

Номер: US20120136052A1

This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.

Подробнее
07-06-2012 дата публикации

Treatment of non-proliferative cystic disease

Номер: US20120141506A1
Автор: David L. KLEINBERG
Принадлежит: New York University NYU

The present invention relates generally to the treatment of non-proliferative cystic disease of the breast. More particularly, the present invention relates generally to the treatment of non-proliferative cystic disease of the breast in BRCA1 mutant carriers. Accordingly, the invention relates to the use and application of compounds or agents, including somatostatin analogs, that inhibit insulin-like growth factor I (IGF-I) or insulin-like growth factor I receptor signaling for the treatment of non-proliferative cystic disease of the breast. The invention further relates to the use and application of these compounds or agents for the treatment of non-proliferative cystic disease of the breast in BRCA1 patients. The invention also relates to use of somatostatin analog SOM230 in treatment of non-proliferative cystic disease of the breast and more particularly, to use of somatostatin analog SOM230 in treatment of BRCA1 associated non-proliferative cystic disease.

Подробнее
07-06-2012 дата публикации

Combination of organic compounds

Номер: US20120142638A1
Автор: Randy Lee Webb
Принадлежит: Individual

The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising a therapeutic agent acting on the renin-angiotensin system (RAS) or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be modulated by action on the renin-angiotensin system (RAS), appetency disorders or substance abuse disorders.

Подробнее
07-06-2012 дата публикации

Targetted drug delivery to the bone

Номер: US20120142641A1
Принадлежит: NANYANG TECHNOLOGICAL UNIVERSITY

The present invention relates to a complex of a bisphosphonate compound, methods of preparing such complex and uses thereof.

Подробнее
07-06-2012 дата публикации

Azetidine 2-Carboxamide Derivatives Which Modulate The CB2 Receptor

Номер: US20120142666A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of the formula (I), (II) and (III) 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.

Подробнее
07-06-2012 дата публикации

Pyrrolidine Compounds Which Modulate The CB2 Receptor

Номер: US20120142677A1
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. (I)

Подробнее
07-06-2012 дата публикации

Picolinamide derivatives as ttx-s blockers

Номер: US20120142691A1
Принадлежит: Raqualia Pharma Inc

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

Подробнее
07-06-2012 дата публикации

4-substituted-cyclohexylamino-4-piperidinyl-acetamide antagonists of ccr2

Номер: US20120142733A1
Принадлежит: Janssen Pharmaceutica NV

The present invention comprises compounds of Formula (I). wherein: R 1 , R 2 , R 3 , R 4 , X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).

Подробнее
07-06-2012 дата публикации

Novel oxadiazole derivatives as sphingosine 1-phosphate (s1p) receptor modulators

Номер: US20120142739A1
Принадлежит: Allergan Inc

The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Подробнее
07-06-2012 дата публикации

Novel complexes of fatty acid esters of polyhydroxyalkanes and pyridine carboxy derivatives

Номер: US20120142744A1
Автор: Morten SLOTH WEIDNER
Принадлежит: Astion Dermatology AS

The present invention relates to novel combinations of fatty acid derivatives and pyridine carboxy derivatives, including fatty acid esters with glycerol and 3-carboxy pyridine derivates such as niacinamide. Such combinations have surprisingly shown antiviral and anti-microbial activity and the use for the treatment of inflammatory conditions and infections is disclosed herein.

Подробнее
07-06-2012 дата публикации

Antagonists of the Magnesium Binding Defect as Therapeutic Agents and Methods for Treatment of Abnormal Physiological States

Номер: US20120142781A1
Автор: Ibert Clifton Wells
Принадлежит: Magnesium Diagnostics Inc

This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.

Подробнее
14-06-2012 дата публикации

Product and method for treatment of conditions associated with receptor-desensitization

Номер: US20120148566A1
Принадлежит: NATIONAL JEWISH HEALTH

Particular members of the multisubunit immune recognition receptor (MIRR) family of receptors, specifically, the B cell antigen receptor (BCR), the pre-B cell receptor (pre-BCR), the pro-B cell receptor (pro-BCR), Ig Fc receptors (FcR), and NK receptors, can be physically uncoupled from their associated transducers. The invention describes regulatory compounds and methods for mimicking such dissociation/destabilization for the purposes of receptor desensitization and for treatment of conditions in which receptor desensitization or alternatively, enhanced or prolonged receptor sensitization, is desirable. Compounds and methods for enhancing or prolonging receptor sensitization are also disclosed, as are methods for identifying regulatory compounds suitable for use in the present methods.

Подробнее
14-06-2012 дата публикации

Enzyme inhibitors

Номер: US20120149736A1
Принадлежит: Chroma Therapeutics Ltd

Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent ═CH— or ═N—; W is —CH═CH— Or —CH 2 CH 2 —; R 1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond, —C(═O)—, —S(═O)2—, —C(═O)O—, —C(═O)NR′—, —C(═5)—NR′, —C(═NH)NR′ or —S(═O) 2 NR — wherein R′ is hydrogen or optionally substituted C 1 —C 6 alkyl; L 1 is a divalent radical of formula —(Alk 1 ) m ,(Q) n (Alk 2 ) p — wherein m, n, p, Q, Alk 1 and Alk 2 are as defined in the claims; X 1 represents a bond; —C(═O); or —S(═O) 2 —; —NR 4 C(═O)—, —C(═O)NR 4 —,— NR 4 C(═O)NR 5 —, —NR 4 S(═O) 2 —, or —S(═O) 2 NR 4 — wherein R4 and R5 are independently hydrogen or optionally substituted C 1 -C 6 alkyl; and z is 0 or 1.

Подробнее
21-06-2012 дата публикации

Treatment of menopause-associated symptoms

Номер: US20120157424A1
Принадлежит: Besins Healthcare SA

Described are estradiol-containing pharmaceutical compositions and, and methods using the same to alleviate menopause-related symptoms, such as hot flushes, by topically administering estradiol at low effective doses.

Подробнее
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. ...

Подробнее
05-07-2012 дата публикации

Omega 3 fatty acid formulations

Номер: US20120172431A1
Принадлежит: CENESTRA LLC

The present invention provides highly purified omega-3 fatty acid formulations. Certain formulations provided herein have contain greater than 85% omega-3 fatty acids by weight. Certain other formulations provided herein contain EPA and DHA in a ratio of from about 4.01:1 to about 5:1. The invention also provides methods of using the dosage forms to treat a variety of cardiovascular, autoimmune, inflammatory, and central nervous system disorders by administering a formulation of the invention to a patient in need thereof.

Подробнее
05-07-2012 дата публикации

SOGA Polynucleotides and Polypeptides and Uses Thereof

Номер: US20120174243A1

The present invention relates to the identification of polynucleotides and polypeptides involved in insulin and adiponectin signaling and regulation of glucose production. The invention further relates to the use of the identified polynucleotides and polypeptides, and inhibitors of the polynucleotides and polypeptides, in the regulation of glucose production and the monitoring and treatment of metabolic disorders such as diabetes.

Подробнее
12-07-2012 дата публикации

DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES

Номер: US20120178734A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

Подробнее
12-07-2012 дата публикации

Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use

Номер: US20120178736A1
Принадлежит: Individual

Formula I (Ia and Ib) compounds wherein (i) X 1 is N and X 2 is S, (ii) X 1 is CR 7 and X 2 is S, (iii) X 1 is N and X 2 is NR 2 , or (iv) X 1 is CR 7 and X 2 is 0, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Подробнее
12-07-2012 дата публикации

Treatment of liver disorders with p13k inhibitors

Номер: US20120178767A1
Автор: Roger G. Ulrich
Принадлежит: Gilead Calistoga LLC

The invention provides methods to treat certain liver disorders by administering a compound that inhibits PD K isoforms, particularly the delta isoform. It further provides specific compounds useful for these methods and ways to identify subjects who are particularly suitable for receiving these treatments.

Подробнее
19-07-2012 дата публикации

Methods of promoting fat loss comprising administering an alk7 inhibitor

Номер: US20120183540A1
Автор: Jasbir Seehra, John Knopf
Принадлежит: Acceleron Pharma Inc

The invention relates to ALK7 soluble receptors and their uses as antagonists of the function of certain ligands such as GDF-8 (Myostatin) and GDF-11. The ALK7 soluble receptor of the invention is useful as antagonists of GDF-8 and GDF-11 in the treatment of neuronal diseases or conditions such as stroke, spinal cord injury, and all peripheral nerve diseases. The ALK7 soluble receptor of the invention is also useful as GH (growth hormone) equivalent, and for increasing muscle mass.

Подробнее
19-07-2012 дата публикации

glucocorticoid therapy

Номер: US20120183610A1
Принадлежит: DuoCort Pharma AB

The present invention relates to improved glucocorticoid therapy and to treatment or prevention of a number of disorders that are due to a diminished or disrupted endogenous glucocorticoid secretory pattern. The invention is based on the findings that producing a specific serum Cortisol time profile that mimics the circadian rhythm of Cortisol of a healthy subject in a subject suffering from a diminished or disrupted glucocorticoid secretory pattern gives benefits with respect to reduction of side-effects.

Подробнее
26-07-2012 дата публикации

Oral dosage forms

Номер: US20120189693A1
Принадлежит: Elite Laboratories Inc

Aspects of the present invention are directed to oral dosage forms comprising a compressed microtablet, wherein said microtablet has a major dimension that is between about 0.25 mm and about 1.0 mm and comprises at least about 0.01 weight percent of at least one pharmaceutically active agent that is distributed substantially throughout said microtablet. Additional aspects of the present invention are directed to methods for producing compressed microtablets having a major dimension that is between about 0.25 mm and about 1.0 mm.

Подробнее
26-07-2012 дата публикации

Analogues of Insulin-Like Growth Factor-1 (IGF-1) Having Amino Acid Substitution at Position 59

Номер: US20120190616A1
Принадлежит: Ipsen Pharma SAS

The present invention relates to novel analogues of insulin-like growth factor-1 (IGF-1), pharmaceutical compositions containing said analogues, and the use of said analogues for treatment of IGF-1-receptor mediated conditions, such as short stature, diabetes therapy, neurodegenerative disease treatment, and cartilage repair. More particularly, the present invention relates to novel analogues of IGF-1 having an amino acid substitution at position 59, e.g., (Asn 59 )hIGF-1(1-70)-OH (SEQ ID NO:1), and other substitution(s) as defined herein.

Подробнее
26-07-2012 дата публикации

Androgen composition for treating an opthalmic condition

Номер: US20120190661A1
Принадлежит: Allergan Inc

The disclosure provides compositions for treating an ocular condition. The composition comprises a physiologically effective amount of an androgen, wherein the composition is suitable for topical administration to an eye. The disclosure further provides methods for treating an ocular condition with the disclosed compositions.

Подробнее
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.

Подробнее
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.

Подробнее
09-08-2012 дата публикации

Methods and devices for the sustained release of multiple drugs

Номер: US20120202742A1

The invention relates to an drug delivery device and a method for delivering multiple drugs over a prolonged period of time. The drug delivery device has two or more unitary segments comprising a drug-permeable polymeric substance, wherein at least one of the segments further comprises a pharmaceutically active agent. The invention also relates to a method for the treatment of a benign ovarian secretory disorder in a female mammal, a method of contraception, and a method of relieving the symptoms associated with menopausal, perimenopausal and post-menopausal periods in a woman.

Подробнее
09-08-2012 дата публикации

Management of breakthrough bleeding in extended hormonal contraceptive regimens

Номер: US20120202779A1
Автор: Andreas Sachse
Принадлежит: Bayer Pharma AG

The present invention relates to a flexible extended use regimen for a hormonal contraceptive useful to manage bleeding problems associated with fixed extended use of hormonal contraceptives and to a pharmaceutical package containing the respective hormonal contraceptive.

Подробнее
16-08-2012 дата публикации

Probiotic bifidobacterium strains

Номер: US20120207713A1
Принадлежит: Alimentary Health Ltd

Bifidobacterium strain AH1206 or mutants or variants thereof are immunomodulatory following oral consumption and are useful in the prophylaxis and/or treatment of inflammatory activity for example undesirable gastrointestinal inflammatory activity such as inflammatory bowel disease.

Подробнее
16-08-2012 дата публикации

Pyrrolopyrimidine compounds and their uses

Номер: US20120207763A1
Принадлежит: ASTEX THERAPEUTICS LTD

The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.

Подробнее
16-08-2012 дата публикации

Thieno- and furo-pyrimidine modulators of the histamine h4 receptor

Номер: US20120208793A1
Принадлежит: Individual

Thieno- and furo-pyrimidine compounds are described, which are useful as H 4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H 4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, such as inflammation.

Подробнее
23-08-2012 дата публикации

Methods and compositions for treating autoimmune diseases

Номер: US20120213731A1
Автор: Denise Faustman
Принадлежит: General Hospital Corp

The invention features methods for increasing or maintaining the number of functional cells of a predetermined type, for example, insulin producing cells of the pancreas, blood cells, spleen cells, brain cells, heart cells, vascular tissue cells, cells of the bile duct, or skin cells, in a mammal (e.g., a human patient) that has injured or damaged cells of the predetermined type.

Подробнее
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214782A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Подробнее
23-08-2012 дата публикации

Modified L-Nucleic Acid

Номер: US20120214868A1
Принадлежит: NOXXON PHARMA AG

A modified L-nucleic acid, containing an L-nucleic acid part conjugated to a non-L-nucleic acid part is described. The conjugate has extended retention time in and demonstrates a delayed elimination from an organism.

Подробнее
30-08-2012 дата публикации

Unstructured recombinant polymers and uses thereof

Номер: US20120220011A1
Принадлежит: AMUNIX OPERATING INC

The present invention provides unstructured recombinant polymers (URPs) and proteins containing one or more of the URPs. The present invention also provides microproteins, toxins and other related proteinaceous entities, as well as genetic packages displaying these entities. The present invention also provides recombinant polypeptides including vectors encoding the subject proteinaceous entities, as well as host cells comprising the vectors. The subject compositions have a variety of utilities including a range of pharmaceutical applications.

Подробнее