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 135982. Отображено 100.
05-01-2012 дата публикации

Enterovirus Vaccines for Preventing or Treating Type 1 Diabetes (III)

Номер: US20120003240A1
Автор: Hanna-Riikka Honkanen, Heikki Hyöty, Jeffrey Almond, Malin Flodström-Tullberg, Mikael Knip, Minna Pulkki, Olli Laitinen, Outi Tolonen, Sami Oikarinen, Valerie Lecouturier
Принадлежит: Sanofi Pasteur Inc, Vactech OY

Coxsackie B virus CBV1 has been found to be strongly associated with the risk of contracting type 1 diabetes. A vaccine comprising CBV1, a component thereof or an antibody thereto is provided for use in preventing or treating type 1 diabetes. In addition CBV2 was also found to be diabetogenic.

Подробнее
Номер записи: 1
05-01-2012 дата публикации

Yeast ectopically expressing abnormally processed proteins and uses therefor

Номер: US20120003243A1
Автор: Susan L. Lindquist, Tiago Outeiro
Принадлежит: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCH

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.

Подробнее
Номер записи: 2
05-01-2012 дата публикации

Dpp iv inhibitor formulations

Номер: US20120003313A1
Автор: Anja Kohlrausch, Gerd Seiffert, Patrick Romer
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.

Подробнее
Номер записи: 3
05-01-2012 дата публикации

Method of reducing multi-drug resistance using inositol tripyrophosphate

Номер: US20120003327A1
Автор: Claudine Kieda, Jean-Marie Lehn, Yves Claude Nicolau
Принадлежит: Individual

Inositol trisphosphate (ITPP) causes normalization of tumor vasculature and is a particularly effective cancer therapy when a second chemotherapeutic agent is administered following partial vascularization. ITPP also treats, alone or in combination, multi-drug resistant cancers. ITPP can also be used to reduce the amount of a second chemotherapeutic drug required for anticancer activity. In addition, ITPP enhances immune response and treats hyperproliferative disorders.

Подробнее
Номер записи: 4
05-01-2012 дата публикации

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

Номер: US20120004206A1
Автор: Bryan K. Sorensen, Dariusz Wodka, James T. Link, Marina A. Pliushchev
Принадлежит: Dariusz Wodka, Link James T, Pliushchev Marina A, Sorensen Bryan K

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
Номер записи: 5
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
Автор: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen
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
Номер записи: 6
05-01-2012 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20120004216A1
Автор: Ashvani K. Singh, Lewis R. Makings, Mark T. Miller, Matthew Hamilton, Peter D.J. Grootenhuis, Sara S. Hadida Ruah, Thomas Cleveland
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
Номер записи: 7
05-01-2012 дата публикации

Novel tetrahydro-quinoline derivatives

Номер: US20120004218A1
Автор: HongYing Yun, Li Chen, Lichun Feng, Mengwei Huang, Mingwei Zhou, Yongfu Liu, Yun He
Принадлежит: Hoffmann La Roche Inc

A compound of formula (I) or a pharmaceutically acceptable salt or ester thereof, wherein A 1 to A 3 and R 1 to R 10 have the significance given in claim 1 , can be used as a medicament. These compounds are useful in the treatment or prophylaxis of diseases that are related to AMPK regulation, such as obesity, dyslipidemia, hyperglycemia, type 1 or type 2 diabetes and cancers.

Подробнее
Номер записи: 8
05-01-2012 дата публикации

Organic compounds

Номер: US20120004247A1
Автор: Brian Cox, Robin Alec Fairhurst, Roger John Taylor
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.

Подробнее
Номер записи: 9
05-01-2012 дата публикации

New ccr2 receptor antagonists and uses thereof

Номер: US20120004252A1
Автор: Christofer Tautermann, Christoph Hoenke, Heiner Ebel, Kai Gerlach, Marco Santagostino, Riccardo Giovannini, Rocco Mazzaferro, Sara Frattini, Stefan Scheuerer, Thomas Trieselmann
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.

Подробнее
Номер записи: 10
05-01-2012 дата публикации

Method of treatment or prophylaxis

Номер: US20120004259A1
Автор: Bruce Douglas Wyse, Maree Therese Smith
Принадлежит: SPINIFEX PHARMACEUTICALS PTY LTD

The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT 2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, in vertebrate animals and particularly in human subjects. The AT 2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of neuropathic conditions.

Подробнее
Номер записи: 11
12-01-2012 дата публикации

Modified Fc Molecules

Номер: US20120009205A1
Автор: Colin V. Gegg, Fei Xiong, Kenneth W. Walker, Leslie P. Miranda
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.

Подробнее
Номер записи: 12
12-01-2012 дата публикации

Modified Virus Vectors and Methods of Making and Using the Same

Номер: US20120009268A1
Автор: Aravind Asokan, Richard Jude Samulski
Принадлежит: UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

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.

Подробнее
Номер записи: 13
12-01-2012 дата публикации

Lactoferrin compositions and methods of wound treatment

Номер: US20120010150A1
Автор: Atul Varadhachary, Jose Engelmayer
Принадлежит: Agennix Inc

The present invention relates to lactoferrin compositions and methods of using the compositions to treat wounds. The compositions can be administered alone or in combination with other standard wound healing therapies.

Подробнее
Номер записи: 14
12-01-2012 дата публикации

Synergistic combinations comprising a renin inhibitor for cardiovascular diseases

Номер: US20120010295A1
Автор: Daniel Lucius Vasella, Randy Lee Webb, William Hewitt
Принадлежит: Daniel Lucius Vasella, Randy Lee Webb, William Hewitt

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

Подробнее
Номер записи: 15
12-01-2012 дата публикации

Optically active 3-amino-2,5-dioxopyrrolidine-3-carboxylate, process for production of the compound, and use of the compound

Номер: US20120010405A1
Автор: Daisuke Tanaka, Toshiyuki Negoro
Принадлежит: Individual

The present invention provides a compound of the formula (III): wherein R is a C 1-6 alkyl group, as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being a promising therapeutic agent for diabetic complications in a short process, in an economically advantageous manner and in high yields, and the process for preparing the same.

Подробнее
Номер записи: 16
19-01-2012 дата публикации

Tablet formulation

Номер: US20120012499A1
Автор: Hikaru Fujita, Koichi Wada, Manabu Nakatani, Thomas Friedl
Принадлежит: Novo Nordisk AS

The present invention relates to a pharmaceutical fixed dose combination tablet comprising repaglinide and metformin. The present invention also provides a method of producing said tablet.

Подробнее
Номер записи: 17
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
Автор: Andrew P. Combs, Haisheng Wang, James D. Rodgers, Richard B. Sparks
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
Номер записи: 18
19-01-2012 дата публикации

Complement receptor 2 targeted complement modulators

Номер: US20120015871A1
Автор: Stephen Tomlinson, V. Michael Holers
Принадлежит: MUSC Foundation for Research Development, University of Colorado

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
Номер записи: 19
19-01-2012 дата публикации

Enzymes and methods for producing omega-3 fatty acids

Номер: US20120016144A1
Автор: Anne Maree Mackenzie, Craig Christopher Wood, Dion Matthew Frederick Frampton, James Robertson Petrie, Peter David Nichols, Peter Maged Mansour, Pushkar Shrestha, Qing Liu, Stanley Suresh Robert, Surinder Pal Singh, Susan Irene Ellis Blackburn, Xue-Rong Ziiou
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
Номер записи: 20
26-01-2012 дата публикации

MHC-Less cells

Номер: US20120020885A1
Автор: Edward K.Y. Jung, Elizabeth A. Sweeney, Eric C. Leuthardt, Gary L. McKnight, Lowell L. Wood, JR., Muriel Y. Ishikawa, Roderick A. Hyde, Stephen L. Malaska, Wayne R. Kindsvogel
Принадлежит: SEARETE LLC

The present disclosure relates to compositions, methods, systems, computer-implemented methods, and computer program products thereof that relate to biological cells for delivery of at least one therapeutic agent to a biological tissue or subject.

Подробнее
Номер записи: 21
26-01-2012 дата публикации

Bicyclic piperidine and piperazine derivatives as gpcr modulators for the treatment of obesity, diabetes and other metabolic disorders

Номер: US20120021976A1
Автор: Claire M. Lankin, Craig D. Boyle, Samuel Chackalamannil, Unmesh G. Shah, William J. Greenlee
Принадлежит: Individual

The present invention relates to Bicyclic Piperidine and piperazine Derivatives, compositions comprising a Bicyclic Piperidine and piperazine Derivative, and methods of using the Bicyclic Piperidine and piperazine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.

Подробнее
Номер записи: 22
26-01-2012 дата публикации

Combination of an insulin and a glp-1-agonist

Номер: US20120021978A1
Автор: Barbel Rotthauser, Christopher James Smith, Ulrich Werner
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
Номер записи: 23
26-01-2012 дата публикации

Histamine h3 inverse agonists and antagonists and methods of use thereof

Номер: US20120022050A1
Автор: Kerry L. Spear, Milan Chytil, Qun Kevin Fang, Sharon R. Engel
Принадлежит: SUNOVION PHARMACEUTICALS INC

Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

Подробнее
Номер записи: 24
26-01-2012 дата публикации

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

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

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

Подробнее
Номер записи: 25
26-01-2012 дата публикации

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

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

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

Подробнее
Номер записи: 26
26-01-2012 дата публикации

Compositions and Methods for Induced Brown Fat Differentiation

Номер: US20120022500A1
Автор: Bruce M. Spiegelman, Shingo Kajimura
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
Номер записи: 27
02-02-2012 дата публикации

Hk1-binding proteins

Номер: US20120027686A1
Автор: Andrew Nixon, Anthony Williams, Daniel J. Sexton, Qi-Long Wu, Robert C. Ladner
Принадлежит: Dyax Corp

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

Подробнее
Номер записи: 28
02-02-2012 дата публикации

Methods for treating diabetes

Номер: US20120027729A1
Автор: Darwin J. Prockop, Min Jeong Seo, Ryang Hwa Lee
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
Номер записи: 29
02-02-2012 дата публикации

Apj receptor compounds

Номер: US20120028888A1
Автор: Athan Kuliopulos, Jay Janz, Thomas J. Mcmurry
Принадлежит: ANCHOR THERAPEUTICS Inc

The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and tension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.

Подробнее
Номер записи: 30
02-02-2012 дата публикации

Pyrazole compounds as crth2 antagonists

Номер: US20120028938A1
Автор: Christoph Hoenke, Dieter Wolfgang Hamprecht, Domnic Martyres, Peter Seither, Ralf Anderskewitz, Thorsten Oost, Wolfgang Rist
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
Номер записи: 31
02-02-2012 дата публикации

Bicyclic mglur5 positive allosteric modulators and methods of making and using same

Номер: US20120028955A1
Автор: Alice L. Rodriguez, Carrie K. Jones, Charles David Weaver, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Richard Williams
Принадлежит: Charles David Weaver, Conn P Jeffrey, Jones Carrie K, LINDSLEY Craig W, Niswender Colleen M, Richard Williams, Rodriguez Alice L

In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Подробнее
Номер записи: 32
02-02-2012 дата публикации

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

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

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

Подробнее
Номер записи: 33
02-02-2012 дата публикации

Compositions for treating or preventing obesity and insulin resistance disorders

Номер: US20120029065A1
Автор: David A. Sinclair, Maria Alexander-Bridges
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
Номер записи: 34
02-02-2012 дата публикации

Pharmaceutical compositions containing fluorinated or perfluorinated carboxylic acids

Номер: US20120029079A1
Автор: Charles R. Wolf, Clifford R. Elcombe
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.

Подробнее
Номер записи: 35
09-02-2012 дата публикации

Method of Administering an Antibody

Номер: US20120034243A1
Автор: David Edward Allison, Judith A. Fox, Lee R. Brettman
Принадлежит: Genentech Inc, Millennium Pharmaceuticals Inc

Disclosed is a method for treating a human having a disease associated with leukocyte infiltration of mucosal tissues, comprising administering to said human an effective amount of a human or humanized immunoglobulin or antigen-binding fragment thereof having binding specificity for α4β7 integrin. Preferably, no more than 8 mg immunoglobulin or fragment per kg body weight are administered during a period of about one month.

Подробнее
Номер записи: 36
09-02-2012 дата публикации

Compositions and methods for the treatment of immune related diseases

Номер: US20120035073A1
Автор: Brisdell Hunte, Hilary Clark, Janet K. Jackman, Jill R. Schoenfeld, P. Mickey Williams, Sarah C. Bodary-Winter, Thomas D. Wu, William I. Wood
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
Номер записи: 37
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.

Подробнее
Номер записи: 38
09-02-2012 дата публикации

Substituted dihydropyrazolones and their use

Номер: US20120035151A1
Автор: Friederike Stoll, Hartmut Beck, Ingo Flamme, Mario Jeske, Metin Akbaba
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
Номер записи: 39
09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Автор: Johan D. Oslob, Kenneth Barr, Min Zhong, Wang Shen
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
Номер записи: 40
16-02-2012 дата публикации

Human monoclonal antibody against a costimulatory signal transduction molecule ailim and pharmaceutical use thereof

Номер: US20120039874A1
Автор: Katsunari Tezuka, Nobuaki Hori, Takashi Tsuji
Принадлежит: Japan Tobacco Inc

Immunization of human antibody-producing transgenic mice, which have been created using genetic engineering techniques, with AILIM molecule as an antigen resulted in various human monoclonal antibodies capable of binding to AILIM and capable of controlling a variety of biological reactions (for example, cell proliferation, cytokine production, immune cytolysis, cell death, induction of ADCC, etc.) associated with AILIM-mediated costimulatory signal (secondary signal) transduction. Furthermore, it has been revealed that the human monoclonal antibody is effective to treat and prevent various diseases associated with AILIM-mediated costimulatory signal transduction, being capable of inhibiting the onset and/or advancement of the diseases.

Подробнее
Номер записи: 41
16-02-2012 дата публикации

Thiadiazole and oxadiazole derivatives, preparation thereof and therapeutic use thereof

Номер: US20120040984A1
Автор: Christophe Philippo, Claudie Namane, Eric Nicolai, Eykmar Fett, Patrick Mougenot
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.

Подробнее
Номер записи: 42
16-02-2012 дата публикации

Dihydrolipoic Acid Derivatives Comprising Nitric Oxide and Therapeutic Uses Thereof

Номер: US20120041025A1
Автор: Sampath Parthasarathy
Принадлежит: Invasc Therapeutics Inc

Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.

Подробнее
Номер записи: 43
16-02-2012 дата публикации

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

Номер: US20120041031A1
Автор: Daniel W. Gil, John E. Donello, Lauren M.B. Luhrs, Veena Viswanath
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.

Подробнее
Номер записи: 44
23-02-2012 дата публикации

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

Номер: US20120045438A1
Автор: Alexey V. Teplyakov, Ellen Chi, Gopalan Raghunathan, Hong Mimi Zhou, Jill Giles-Komar, Jill M. Carton, Johan Fransson, Juan C. Almagro, Karyn T. O'neil, Linus Hyun, Ronald V. Swanson, Shanrong Zhao, Wendy Cordier, Yiqing Feng
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
Номер записи: 45
23-02-2012 дата публикации

Policosanol nanoparticles

Номер: US20120045482A1
Автор: Palayakotai R. Raghavan
Принадлежит: NanoRx Inc

The present invention provides nanoparticulate policosanol, and octacosanol formulations including these particles, as a well as methods of using the particles and formulations for treatment and prophylaxis of various diseases and conditions.

Подробнее
Номер записи: 46
23-02-2012 дата публикации

TNF-alpha Antagonists Containing IGFBP5

Номер: US20120046217A1
Автор: Jae-ho Huh, Jae-Ryoung Hwang, Je-Ho Lee
Принадлежит: Sungkyunkwan University Foundation For Corporate Collaboration

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.

Подробнее
Номер записи: 47
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
Номер записи: 48
23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Автор: Hiroki Fukudome, Hiroshi Moritani, Takahiro Nigawara, Takeshi Hanazawa, Tomoaki Kawano, Yasuhiro Yonetoku
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

Подробнее
Номер записи: 49
23-02-2012 дата публикации

Small molecule inhibitors of kynurenine-3-monooxygenase

Номер: US20120046324A1
Автор: Joseph M. Muchowski, Paolo Guidetti, Paul J. Muchowski, Robert Schwarcz
Принадлежит: University of Maryland at Baltimore

The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof.

Подробнее
Номер записи: 50
01-03-2012 дата публикации

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

Номер: US20120052097A1
Автор: Jungyeon Hwang, Oliver S. Fetzer, Patrick Lim Soo, Pei-Sze Ng, Sonke Svenson
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.

Подробнее
Номер записи: 51
01-03-2012 дата публикации

Pharmaceutical composition for diabetic nephropathy and its preparation and application

Номер: US20120053236A1
Автор: Bao He, Dan Tang, Fei GU, Huiquan Cheng, Quan Zhu, Rushang Wang, Tingting Duan, Xiaoling Huang, Xinghua Shi, Yanxia Huang, Zhaoguang Zheng
Принадлежит: GUANGZHOU CONSUN MEDICINE R AND D CO Ltd

The invention relates to application of 4,4′-diphenylmethane-bis(methyl) carbamates (DPMC) extracted and isolated from Cortex Mori and preparation of medicine for diabetic nephropathy. The pharmaceutical composition is made up of DPMC as active ingredient and the normal drug carriers, and the weight percentage of active ingredient is 0.1-99.5%. For the remarkable effect of prevention and cure for diabetic nephropathy and convenience for use, it will be a new facultative drug for patients.

Подробнее
Номер записи: 52
08-03-2012 дата публикации

Therapeutic or prophylactic agent for dyskinesia

Номер: US20120058186A1
Автор: Kotoe Ohta, Suguru Takaki, Yasuhide Horiuch
Принадлежит: TORAY INDUSTRIES INC

The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

Подробнее
Номер записи: 53
08-03-2012 дата публикации

Nutritional composition inducing a postprandial endocrine response

Номер: US20120058938A1
Автор: Mirian Lansink, Robert Johan Joseph Hageman
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
Номер записи: 54
08-03-2012 дата публикации

Neuroprotective iron chelators and pharmaceutical compositions comprising them

Номер: US20120058945A1
Автор: Abraham Warshawsky, Hailin Zheng, Matitiyahu Fridkin, Moussa Youdim, Rivka Warshawsky
Принадлежит: Technion Research and Development Foundation Ltd, Yeda Research and Development Co Ltd

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
Номер записи: 55
08-03-2012 дата публикации

Feedback prodrug

Номер: US20120058960A1
Автор: Geert-Jan Boons, Jun Guo
Принадлежит: University of Georgia Research Foundation Inc UGARF

Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.

Подробнее
Номер записи: 56
08-03-2012 дата публикации

Phosphonate Compounds

Номер: US20120058975A1
Автор: Ganesh D. Kini, James R. Beadle, Karl Y. Hostetler
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.

Подробнее
Номер записи: 57
08-03-2012 дата публикации

Novel kinase modulators

Номер: US20120059001A1
Автор: Govindarajulu Babu, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Swaroop Kumar V.S. Vakkalanka
Принадлежит: Incozen Therapeutics Pvt Ltd, Rhizen Pharmaceuticals SA

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
Номер записи: 58
08-03-2012 дата публикации

Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) an antidiabetic compound for use in the treatment of proliferative diseases

Номер: US20120059005A1
Автор: Carlos Garcia-Echeverria, Jose Baselga, Russillo Michelangelo, Sauveur-Michel Maira, Serena Di Cosimo, Violeta Serra Elizalde, Wolfgang Hackl
Принадлежит: NOVARTIS AG

The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) an insulin sensitivity enhancer compound for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.

Подробнее
Номер записи: 59
08-03-2012 дата публикации

Inhibition of map4k4 through rnai

Номер: US20120059046A1
Автор: Anastasia Khvorova, Joanne Kamens, Tod M Woolf, William Salomon
Принадлежит: RXi Pharmaceuticals Corp

RNAi constructs directed to MAP4K4 that demonstrate unexpectedly high gene silencing activities, and uses thereof are disclosed. The blunt-ended constructs have a double-stranded region of 19-49 nucleotides. The constructs have selective minimal modifications to confer an optimal balance of biological activity, toxicity, stability, and target gene specificity. For example, the strands may be modified (e.g., one or both ends of the sense strand is modified by 2′-O-methyl groups), such that the construct is not cleaved by Dicer or other RNAse III, the antisense strand may also be modified by a 2′-O-methyl group at the penultimate 5′-end nucleotide to greatly reduce off-target silencing.

Подробнее
Номер записи: 60
15-03-2012 дата публикации

Delivery system with scaffolds

Номер: US20120063997A1
Автор: Cheryl Hunter, Kevin Morris Shakessheff, Robin Andrew Quirk
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.

Подробнее
Номер записи: 61
15-03-2012 дата публикации

Methods of Diagnosing Hypophosphatemic Disorders

Номер: US20120064544A1
Автор: Ken White, Michael Econs, Thomas Meitinger, Tim Matthias Strom
Принадлежит: Indiana University Research And Technology Corp, Ludwig Maximilians Universitaet Muenchen LMU

The present invention relates to methods of diagnosing hypophosphatemic disorders.

Подробнее
Номер записи: 62
15-03-2012 дата публикации

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

Номер: US20120065128A1
Автор: Doris C. O'Toole, JoAnne P. Corvino, Nikhil Dhoot, Shingai Majuru, Steven Dinh, William Elliott Bay
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
Номер записи: 63
15-03-2012 дата публикации

Test agent for visceral obesity and use thereof

Номер: US20120066777A1
Автор: Atsunori Kashiwagi, Hiroshi Maegawa, Masatomo Rokushima, Minoru Ikeda, Minoru Suzuki, Shiro Maeda, Tatsuya Takahashi, Tohru Tani, Yoshihiro Kawamura
Принадлежит: RIKEN Institute of Physical and Chemical Research, Shiga University of Medical Science NUC, Shionogi and Co Ltd

Disclosed are: a method for detecting (diagnosing) visceral obesity in a subject; a test agent useful for the method; a method for searching for a substance that can be used as an active ingredient for ameliorating visceral obesity; and an ameliorating agent for visceral obesity or a medicinal agent for preventing a metabolic disease developed as a result of the progression of visceral obesity. As the test agent, a polynucleotide which comprises at least 15 nucleotides and can hybridize with a nucleotide sequence for coiled-coil domain containing protein 3 (CCDC3) gene or a nucleotide sequence complementary to the nucleotide sequence under stringent conditions or an antibody capable of recognizing CCDC3 protein is used.

Подробнее
Номер записи: 64
22-03-2012 дата публикации

Methods of treating inflammation

Номер: US20120070449A1
Автор: Einat Toister, Idit Shachar
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.

Подробнее
Номер записи: 65
22-03-2012 дата публикации

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

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

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

Подробнее
Номер записи: 66
22-03-2012 дата публикации

Protease Stabilized, Pegylated Insulin Analogues

Номер: US20120071402A1
Автор: Peter Madsen, Thomas Børglum KJELDSEN, Thomas Hoeg-Jensen, Tina Møller TAGMOSE
Принадлежит: Novo Nordisk AS

Novel PEGylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. The PEGylation is at B29K.

Подробнее
Номер записи: 67
22-03-2012 дата публикации

Pyrazole oxadiazole derivatives as s1p1 agonists

Номер: US20120071460A1
Автор: Anna Quattropani, Charles Baker-Glenn, Chris KNIGHT, Wesley Blackaby
Принадлежит: MERCK SERONO SA

The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases, wherein R 1 , R 2 and R 3 are as defined in the description.

Подробнее
Номер записи: 68
22-03-2012 дата публикации

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

Номер: US20120071505A1
Автор: Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel, Samuel Victory
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.

Подробнее
Номер записи: 69
29-03-2012 дата публикации

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

Номер: US20120076874A1
Автор: Chan Woong Park, Dae Bang Seo, Hee Young Jeon, Ji Hae Lee, Kyung Mi Joo, Kyung Min Lim, Sang Jun Lee
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.

Подробнее
Номер записи: 70
29-03-2012 дата публикации

Cyclic peptides and uses thereof

Номер: US20120077732A1
Автор: Marina Ali, Nicholas Manolios, Veronika Judit Bender
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
Номер записи: 71
29-03-2012 дата публикации

Novel salts of sitagliptin

Номер: US20120077760A1
Автор: Ivan Plantan, Lovro Selic
Принадлежит: Lek Pharmaceuticals dd

The present invention relates to novel pharmaceutically acceptable salts of sitagliptin, to processes for their preparation and to pharmaceutical compositions containing them.

Подробнее
Номер записи: 72
29-03-2012 дата публикации

Bicyclic compounds and use as antidiabetics

Номер: US20120077812A1
Автор: Andrew J. Carpenter, Christopher R. Conlee, Gregory Peckham, Jing Fang, JUN TANG, Kien S. Du, Subba Reddy Katamreddy
Принадлежит: Individual

The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.

Подробнее
Номер записи: 73
29-03-2012 дата публикации

Chemical compounds

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

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

Подробнее
Номер записи: 74
29-03-2012 дата публикации

Pharmaceutical product

Номер: US20120077856A1
Автор: Masayuki Ii, Tomohiro Kawamoto, Yuji Iizawa
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
Номер записи: 75
05-04-2012 дата публикации

Stabilized alpha helical peptides and uses thereof

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

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

Подробнее
Номер записи: 76
05-04-2012 дата публикации

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

Номер: US20120082668A1
Автор: Gao Zeren, Mark W. Rixon, Steven D. Levin
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.

Подробнее
Номер записи: 77
05-04-2012 дата публикации

Myostatin binding agents

Номер: US20120083442A1
Автор: Hosung Min, Hq Han, Thomas Charles Boone
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.

Подробнее
Номер записи: 78
05-04-2012 дата публикации

Bis-pyridylpyridones as melanin-concentrating hormone receptor antagonists

Номер: US20120083489A1
Автор: Chengde Wu, Chuanning Wang, Di Li, Donghui Qin, Fei Li, Haiyu Yu, Lei Li, Maoyun Lv, MEI Xiao, Shenglin Chen, Shi Lu, Siegfried Benjamin Christensen Iv, Weina Zhang, Xiaojuan Lin, Xing Huang, Zhen Lu, Zhiliu Zhang
Принадлежит: GlaxoSmithKline LLC

The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and diabetes.

Подробнее
Номер записи: 79
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
Автор: Anne-Laure Blayo, Babette Aicher, Gilbert Mueller, Jean Martinez, Jean-Alain Fehrentz, Klaus Paulini, Lars Blumenstein, Matthias Gerlach, Michael Teifel, Peter Schmidt
Принадлежит: Aeterna Zentaris GmbH, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite de Montpellier I, Universite de Montpellier II

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
Номер записи: 80
12-04-2012 дата публикации

Inhibitors of protein tyrosine phosphatases

Номер: US20120088720A1
Автор: Sheng Zhang, Zhong-Yin Zhang
Принадлежит: Indiana University Research And Technology Corp

Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.

Подробнее
Номер записи: 81
12-04-2012 дата публикации

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

Номер: US20120088746A1
Автор: Hirotaka Tanaka, John Kincaid, Kazunari Nakao, Kiran Sahasrabudhe, Maria de los Ángeles ESTIARTE-MARTÍNEZ, Matthew Alexander James Duncton, Matthew Cox, Satoshi Nagayama, Yuji Shishido
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.

Подробнее
Номер записи: 82
12-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120088762A1
Автор: Catherine Sylvain, Francesco Parlati, Guy J. Laidig, Han-Jie Zhou, Kevin D. Shenk, Mark K. Bennett, Mark S. Smyth
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.

Подробнее
Номер записи: 83
12-04-2012 дата публикации

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

Номер: US20120088778A1
Автор: Adnan M.M. Mjalli, Anitha Hari, David R. Jones, Ghassan Qabaja, Kwasi S. Avor, Ramesh Gopalaswamy, Robert C. Andrews, Suparna Gupta, Xiao-Chuan Guo, Xin Chen
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.

Подробнее
Номер записи: 84
12-04-2012 дата публикации

Interlaced method for treating cancer or a precancerous condition

Номер: US20120088807A1
Автор: Andrew J. Krouse, Joel Linden, Lloyd S. Gray, Timothy Macdonald
Принадлежит: TAU THERAPEUTICS LLC

The present invention provides a method for treating a disease or condition in a mammal which comprises the steps of; administering a therapeutically effective amount of a T type calcium channel inhibitor to effectively slow or stop progression of eukaryotic cells through the S, G 2 and M phases of the cell cycle to increase the proportion of the eukaryotic cells in the G 1 phase, stopping administration of the T type calcium channel inhibitor for a period of time, and administering a dosage selected from the group consisting of a dosage of at least one chemotherapeutic agent, a dosage of radiation, and combinations thereof, to kill the proportion of eukaryotic cells progressing past the G 1 phase of the cell cycle after the stopping of the administration of the T type calcium channel inhibitor.

Подробнее
Номер записи: 85
12-04-2012 дата публикации

Satiety-inducing composition

Номер: US20120088830A1
Автор: Annika Viberg, Anthonius Cornelis Van Den Burg, Arjen Sein, Damiet Josephina Petronella Cunera Koenders, Gerardus Johannes Franciscus Smolders
Принадлежит: DSM IP ASSETS BV

The present invention relates to the field of weight management. The invention particularly relates to a method for inducing satiety. In one of its embodiments, the present invention provides a method for inducing satiety in a human or an animal comprising administering to said human or animal an effective amount of a composition comprising a lipid of which at least part is in a crystal form in the small intestine.

Подробнее
Номер записи: 86
19-04-2012 дата публикации

Human artificial chromosome (hac) vector

Номер: US20120093785A1
Автор: Kazuma Tomizuka, Minoru Kakeda, Mitsuo Oshimura, Motonobu Katoh, Yoshimi Kuroiwa
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.

Подробнее
Номер записи: 87
19-04-2012 дата публикации

Treatment of limb ischemia

Номер: US20120093786A1
Автор: Erik Miljan, John Sinden, Paolo Madeddu
Принадлежит: ReNeuron Ltd

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

Подробнее
Номер записи: 88
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
Номер записи: 89
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
Номер записи: 90
26-04-2012 дата публикации

CD86 Antagonist Multi-Target Binding Proteins

Номер: US20120100139A1
Автор: John W. Blankenship, Peter Armstrong Thompson, Peter Robert Baum, Philip Tan, Sateesh Kumar Natarajan
Принадлежит: Emergent Product Development Seattle LLC

This disclosure provides a multi-specific fusion protein composed of a CD86 antagonist binding domain and another binding domain that is an IL-10 agonist, an HLA-G agonist, an HGF agonist, an IL-35 agonist, a PD-1 agonist, a BTLA agonist, a LIGHT antagonist, a GITRL antagonist or a CD40 antagonist. The multi-specific fusion protein may also include an intervening domain that separates the other domains. This disclosure also provides polynucleotides encoding the multi-specific fusion proteins, compositions of the fusion proteins, and methods of using the multi-specific fusion proteins and compositions.

Подробнее
Номер записи: 91
26-04-2012 дата публикации

Stable pharmaceutical composition and methods of using same

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

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

Подробнее
Номер записи: 92
26-04-2012 дата публикации

Pharmaceutical formulations of a substituted diaminopurine

Номер: US20120100213A1
Автор: Anthony Joseph FRANK, Anthony Tutino, Sreenivas S. Bhat, Xiaozhong Liang
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
Номер записи: 93
26-04-2012 дата публикации

Glucose-dependent insulinotropic peptide analogs

Номер: US20120101037A1
Автор: George Ehrlich, Jefferson Wright Tilley, Joseph Swistok, Wajiha Khan, Waleed Danho
Принадлежит: F Hoffmann La Roche AG

The present invention provides compounds which are analogs of glucose-dependent insulinotropic polypeptide (GIP) and pharmaceutically acceptable salts of such compounds. These compounds have activity as agonists of GIP receptor.

Подробнее
Номер записи: 94
26-04-2012 дата публикации

Novel c-aryl glucoside sglt2 inhibitors and pharmaceutical compositions comprising same

Номер: US20120101051A1
Автор: Eun Jung Son, Hee Jeong Seo, Jeongmin Kim, Jinhwa Lee, Kwang-Seop Song, Mi-Soon Kim, Min Ju Kim, Myung Eun Jung, Suk Ho Lee, Suk Youn Kang, Sung-Han Lee
Принадлежит: Green Cross Corp Korea

A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.

Подробнее
Номер записи: 95
26-04-2012 дата публикации

S1p1 agonists comprising a bicyclic n-containing ring

Номер: US20120101083A1
Автор: Christian Alan Paul Smethurst, Emmanuel Hubert Demont, James Matthew Bailey, Jason Witherington, Katherine Louise Jones, Lee Andrew Harrison, Rino Antonio Bit
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.

Подробнее
Номер записи: 96
26-04-2012 дата публикации

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

Номер: US20120101086A1
Автор: Christian Alan Paul Smethurst, Emmanuel Hubert Demont, Gail Astra Lorraine Seal, James Matthew Bailey, Jason Witherington, John Alexander Brown, Lee Andrew Harrison
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
Номер записи: 97
26-04-2012 дата публикации

Compounds

Номер: US20120101123A1
Автор: Chengyong Li, Haibo Zhang, Qinghua Meng, Xichen Lin
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
Номер записи: 98
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.

Подробнее
Номер записи: 99
26-04-2012 дата публикации

Methylphenidate Derivatives and Uses of Them

Номер: US20120101129A1
Автор: David Bar-Or, Nagaraja R. K. Rao
Принадлежит: David Bar-Or, Rao Nagaraja R K

The present invention provides methods of using compounds of formula I: and salts and prodrugs thereof, wherein n, R 1 and R 2 are defined herein. The invention also provides certain novel compounds of formula I and pharmaceutical compositions comprising them.

Подробнее
Номер записи: 100