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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 491203. Отображено 100.
05-01-2012 дата публикации

Pyrazolo[1,5-a]pyrimidines for antiviral treatment

Номер: US20120003215A1
Автор: Constantine G. Boojamra, David Sperandio, Dustin Siegel, Eugene J. Eisenberg, Hai Yang, Hon Chung Hui, Jay P. Parrish, Kerim Babaoglu, Michael Sangi, Oliver L. Saunders, Richard L. Mackman
Принадлежит: Gilead Sciences Inc

The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.

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Номер записи: 1
05-01-2012 дата публикации

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

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

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

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Номер записи: 2
05-01-2012 дата публикации

Composition Comprising Vascular Endothelial Growth Factor (VEGF) for the Treatment of Hair Loss

Номер: US20120003300A1
Автор: Elliot Isaacs, Toby Cobbledick
Принадлежит: Pangaea Laboratories Ltd

A composition to treat hair loss and enhance hair growth and condition. The composition comprises: i) one or more of VEGF, a VEGF biomimetic peptide, and/or a VEGFR2 receptor agonist; ii) ciclopirox olamine; and iii) a pharmaceutically acceptable carrier.

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Номер записи: 3
05-01-2012 дата публикации

Pharmaceutical Composition Comprising Aliskiren

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

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

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Номер записи: 4
05-01-2012 дата публикации

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.

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Номер записи: 5
05-01-2012 дата публикации

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

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

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

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Номер записи: 6
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.

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Номер записи: 7
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.

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Номер записи: 8
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.

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Номер записи: 9
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.

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Номер записи: 10
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.

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Номер записи: 11
05-01-2012 дата публикации

Method of Inhibition of Respiratory Depression Using Positive Allosteric AMPA Receptor Modulators

Номер: US20120004219A1
Автор: John Greer
Принадлежит: University of Alberta

The invention is directed to a method for alleviating respiratory depression in a subject as a result of disease of pharmacological agents such as opiates, opioids or barbiturates. The invention also discloses pharmaceutical compositions for use with the method, the composition containing in combination, an analgesic, anaesthetic, or a sedative and a positive allosteric AMPA receptor modulator in an amount sufficient to reduce or inhibit respiratory depression caused by the analgesic, anaesthetic, or sedative.

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Номер записи: 12
05-01-2012 дата публикации

Salt of cd 80 antagonist

Номер: US20120004237A1
Автор: Richard Ian MATTHEWS
Принадлежит: MEDIGENE AG

Choline salt of the CD80 antagonist compound 4-(6-fluoro-3-oxo-1,3-dihydro-pyrazolo[4,3-c]cinnolin-2-yl)-N-(2,2-difluoro-ethyl)-benzamide.

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Номер записи: 13
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.

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Номер записи: 14
05-01-2012 дата публикации

Methods of using a methylxanthine compound

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

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

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Номер записи: 15
05-01-2012 дата публикации

Use of the phytocannabinoid cannabidivarin (cbdv) in the treatment of epilepsy

Номер: US20120004251A1
Автор: Ben Whalley, Claire Williams, Gary Stephens, Takashi Futamura
Принадлежит: GW Pharma Ltd, Otsuka Pharmaceutical Co Ltd

This invention relates to the use of the phytocannabinoid cannabidivarin (CBDV) and combinations of the phytocannabinoid CBDV with tetrahydrocannabivarin (THCV) and cannabidiol (CBD) in the treatment of epilepsy. The invention further relates to the use of the phytocannabinoid CBDV in combination with standard anti-epileptic drugs (SAEDs). Preferably the SAED is one of ethosuximide, valproate or phenobarbital.

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Номер записи: 16
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.

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Номер записи: 17
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.

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Номер записи: 18
05-01-2012 дата публикации

Compounds for the treatment of pathologies associated with aging and degenerative disorders

Номер: US20120004263A1
Автор: Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
Принадлежит: University of Pittsburgh

The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.

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Номер записи: 19
05-01-2012 дата публикации

Clathrate, curing agent, cure accelerator, epoxy resin composition, and epoxy resin composition for encapsulation of semiconductor

Номер: US20120004377A1
Автор: Kazuo Ono, Masami Kaneko
Принадлежит: Nippon Soda Co Ltd

It is an object of the present invention to provide a clathrate that suppresses a curing reaction at low temperature to promote an improvement in storage stability (one-component stability), and can effectively cure a resin by heating treatment. A clathrate suitable for the clathrate is a clathrate containing (b1) at least one selected from the group consisting of an aliphatic polyvalent carboxylic acid, 5-nitroisophthalic acid, 5-tert-butylisophthalic acid, 5-hydroxyisophthalic acid, isophthalic acid, and benzophenone-4,4′-dicarboxylic acid; and (b2) at least one selected from the group consisting of an imidazole compound represented by the following formula (I), and 1,8-diazabicyclo[5.4.0]undecene-7, at a molar ratio of 1:1.

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Номер записи: 20
19-01-2022 дата публикации

Раневая атравматическая повязка для животных

Номер: RU0000208882U1
Автор: Александр Александрович Кролевец, Денис Александрович Григорьев, Дмитрий Олегович Сеин, Олег Борисович Сеин
Принадлежит: Федеральное государственное бюджетное образовательное учреждение высшего образования "Курская государственная сельскохозяйственная академия имени И.И. Иванова"

Полезная модель относится к ветеринарной медицине, в частности, к ветеринарной хирургии, и предназначена для лечения инфицированных ран, язв, пролежней, гнойничковых и трофических поражений кожи и подкожной клетчатки и может использоваться как перевязочное средство. Отличительной особенностью раневой атравматической повязки является то, что ее внутренний рабочий слой, обращенный к раневой поверхности, состоит из мелкоячеистого хлопкового нетканого полотна, предварительно обработанного раствором риванола и тримекаина с последующим высушиванием и нанесением на нее антисептика стимулятора Дорогова второй фракции (АСД-2ф), микрокапсулированного в оболочку из натрий карбоксиметилцеллюлозы. Наружный слой повязки, покрывающий слой микрокапсул, состоит из тонкой пергаментной бумаги и нетканого полотна. При этом свободные от слоя микрокапсул края повязки по периметру склеиваются. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 208 882 U1 (51) МПК A61K 31/00 (2006.01) A61K 9/70 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (52) СПК A61K 31/00 (2021.08); A61K 9/70 (2021.08) (21)(22) Заявка: 2021125236, 25.08.2021 (24) Дата начала отсчета срока действия патента: Дата регистрации: 19.01.2022 (45) Опубликовано: 19.01.2022 Бюл. № 2 2 0 8 8 8 2 R U (54) Раневая атравматическая повязка для животных (57) Реферат: Полезная модель относится к ветеринарной медицине, в частности, к ветеринарной хирургии, и предназначена для лечения инфицированных ран, язв, пролежней, гнойничковых и трофических поражений кожи и подкожной клетчатки и может использоваться как перевязочное средство. Отличительной особенностью раневой атравматической повязки является то, что ее внутренний рабочий слой, обращенный к раневой поверхности, состоит из мелкоячеистого хлопкового нетканого полотна, предварительно Стр.: 1 (56) Список документов, цитированных в отчете о поиске: RU 99711 U1, 27.11.2010. RU 2031648 C1, 27.03.1995. CN 109419810 A, 05.03.2019. PE 20081883 A1, ...

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Номер записи: 21
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.

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Номер записи: 22
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.

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Номер записи: 23
12-01-2012 дата публикации

Cell Penetrating Peptide Conjugates for Delivering of Nucleic Acids into a Cell

Номер: US20120010124A9
Автор: Bertrand Alluis, Jean-Sebastien Fruchart
Принадлежит: Diatos SA

The invention provides cell penetrating peptide-nucleic acid conjugates having the formula P-L-N, wherein P is a cell penetrating peptide, N is a nucleic acid, preferably an oligonucleotide and more preferably a siRNA, and L is a hydrophilic polymer, preferably a polyethylene glycol (PEG)-based linker linking P and N together. Compositions, methods of use and methods for producing such conjugates are also disclosed.

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Номер записи: 24
12-01-2012 дата публикации

Recombinant surfactant protein d compositions and methods of use thereof

Номер: US20120010126A1
Автор: Howard Clark, Kenneth Bannerman Milne Reid, Palaniyar Nadesalingam, Peter Strong
Принадлежит: Medical Research Council

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

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Номер записи: 25
12-01-2012 дата публикации

Novel uses of vegfxxxb

Номер: US20120010138A1
Автор: Andrew Salmon, David Owen Bates, Steven James Harper
Принадлежит: University of Bristol

The invention provides VEGF xxx b, or an agent which selectively promotes the expression of VEGF xxx b in preference to VEGF xxx in cells of a subject or in vitro, or an expression vector system which causes the expression of the VEGF xxx b in a host organism, for use in treating or preventing microvascular hyperpermeability disorders, or in regulating the pro-angiogenic pro-permeability properties of VEGF xxx isoforms, or in supporting epithelial cell survival without increased permeability, or in reducing the nature (for example the number density and/or size) of fenestrations of epithelial filtration membranes in vivo or in vitro.

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Номер записи: 26
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.

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Номер записи: 27
12-01-2012 дата публикации

Tumor necrosis factor inhibiting peptides and uses thereof

Номер: US20120010158A1
Автор: Rahul Jain, Rajesh Jain, Shudhanand Prasad, Shweta Dubey, Vijay Goel, Virendra Kumar Vinayak
Принадлежит: Panacea Biotec Ltd

The present invention relates to Tumor Necrosis Factor-alpha (TNF-alpha or TNF-α) inhibiting peptides and process for the preparation thereof. The present invention further relates to a pharmaceutical composition comprising TNF-alpha inhibiting peptides of the present invention and uses thereof in treating TNF-alpha mediated inflammatory disorders.

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Номер записи: 28
12-01-2012 дата публикации

Broad spectrum benzothiophene-nitrothiazolide and other antimicrobials

Номер: US20120010187A1
Автор: Paul S. Hoffman, Richard L. Guerrant, Thomas Eric Ballard, JR., Timothy L. MacDonald
Принадлежит: UNIVERSITY OF VIRGINIA PATENT FOUNDATION

The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.

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Номер записи: 29
12-01-2012 дата публикации

11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds

Номер: US20120010194A1
Автор: Henrik Sune Andersen, Soren Ebdrup
Принадлежит: High Point Pharnaceuticals LLC

The use of substituted amides for modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11βHSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.

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Номер записи: 30
12-01-2012 дата публикации

Methods of treating neurodegenerative disorders and diseases

Номер: US20120010196A1
Автор: Quingyu QIN, Xiaoning Bl
Принадлежит: WESTERN UNIVERSITY OF HEALTH SCIENCES

This invention is directed to a novel method of treating neurodegenerative disorders and diseases. Another, related aspect of this invention is directed to a screening method of identifying compounds that can be used to treat neurodegenerative disorders and diseases. The foregoing aspects of the invention particularly relate to neurodegenerative disorders and diseases have degeneration of neuronal axons as part of their pathologies. The method of treatment involves administering a pharmaceutical formulation that comprises a compound or mixture of compounds that inhibits one or more intracellular signaling mechanism that regulate axon degeneration or growth cone collapse. The screening method aspect of the invention identifies test compounds that can be used for the treatment or prevention of neurodegenerative disorders based on the test compound's ability to inhibit axon degeneration or growth cone collapse.

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Номер записи: 31
12-01-2012 дата публикации

5-chloro-4-hydroxy-1-methyl-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide, salts and uses thereof

Номер: US20120010239A1
Автор: Ulf Tomas Fristedt
Принадлежит: Teva Pharmaceutical Industries LTD

The subject invention provides 5-chloro-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-3-carboxamide, its salts and uses.

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Номер записи: 32
12-01-2012 дата публикации

Choline and tromethamine salt of licofelone

Номер: US20120010261A1
Автор: Hans-Günter Striegel, Stefan Laufer, Wolfgang Albrecht
Принадлежит: CAIR Biosciences GmbH

The present invention relates to the choline and tromethamine salt of Licofelone.

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Номер записи: 33
12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

Номер: US20120010283A1
Автор: Andrea Duranti, Andrea Tontini, Daniele Piomelli, Giorgio Tarzia, Marco Mor
Принадлежит: Universita degli Studi di Parma, Universita degli Studi di Urbino "Carlo Bo", UNIVERSITY OF CALIFORNIA

Fatty acid amide hydrolase inhibitors of the Formula: are provided wherein X is NH, CH 2 , O, or S; Q is O or S; Z is O or N; R is an aromatic moiety selected from the group consisting of substituted or unsubstituted aryl; substituted or unsubstituted biphenylyl, substituted or unsubstituted naphthyl, and substituted or unsubstituted phenyl; substituted or unsubstituted terphenylyl; substituted or unsubstituted cycloalkyl, heteroaryl, or alkyl; and R 1 and R 2 are independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, and substituted or unsubstituted phenyl, substituted or unsubstituted biphenylyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl; with the proviso that if Z is O, one of R 1 and R 2 is absent, and that if Z is N, optionally R 1 and R 2 may optionally be taken together to form a substituted or unsubstituted N-heterocycle or substituted or unsubstituted heteroaryl with the N atom to which they are each attached. Pharmaceutical compositions comprising the compounds of Formula I and methods of using them to inhibit FAAH and/or treat appetite disorders, glaucoma, pain, insomnia, and neurological and psychological disorders including anxiety disorders, epilepsy, and depression are provided.

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Номер записи: 34
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.

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Номер записи: 35
12-01-2012 дата публикации

Improved chemical synthesis of diazaindoles by chichibabin cyclization

Номер: US20120010409A1
Автор: Franz J. Weiberth, George E. Lee, II Frederick L. Shrimp
Принадлежит: SANOFI SA

An improved synthesis method for making diazaindoles using a Chichibabin cyclization is disclosed. In particular, this method is useful for making the compound of Formula I.

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Номер записи: 36
19-01-2012 дата публикации

Enhanced Natural Colors

Номер: US20120014934A1
Автор: Jeffrey M. Wuagneux, Paul Altaffer, Pi-Yu Hsu
Принадлежит: RFI LLC

A natural color is concentrated to intensify color range and to provide useful amounts of one or more of anti-oxidant, nutritional, and anti-inflammatory compounds derived from one or more pigment sources. In a preferred embodiment, the pigment source is a fruit, a vegetable, a legume, a spice, algae, or a combination thereof.

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Номер записи: 37
19-01-2012 дата публикации

Il-1beta binding antibodies and fragments thereof

Номер: US20120014967A1
Автор: Arnold Horwitz, Gang Chen, Linda Masat, Marina Roell, Mary Haak-Frendscho
Принадлежит: Xoma Technology Ltd USA

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

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Номер записи: 38
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.

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Номер записи: 39
19-01-2012 дата публикации

Modified release formulations containing drug-ion exchange resin complexes

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

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

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Номер записи: 40
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.

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Номер записи: 41
19-01-2012 дата публикации

Compounds for the prevention and treatment of cardiovascular diseases

Номер: US20120015905A1
Автор: Henrik C. Hansen
Принадлежит: Resverlogix Corp

The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

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Номер записи: 42
19-01-2012 дата публикации

Sulfone Compounds Which Modulate The CB2 Receptor

Номер: US20120015988A1
Автор: Christopher Francis Palmer, David Smith Thomson, Doris Riether, Eugene Richard Hickey, Mark Whittaker, Monika Ermann, Patricia Amouzegh, Renee M. Zindell
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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Номер записи: 43
19-01-2012 дата публикации

Taspase1 inhibitors and their uses

Номер: US20120015990A1
Автор: Emily Cheng, James Hsieh
Принадлежит: Washington University in St Louis WUSTL

Provided herein are small molecule inhibitors of Taspase1 and methods of using the small molecule inhibitors of Taspase1 to treat neoplasm in subjects in need thereof.

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Номер записи: 44
19-01-2012 дата публикации

RNAi MOLECULE TARGETING THYMIDYLATE SYNTHASE AND APPLICATION THEREOF

Номер: US20120016012A1
Автор: Cheng Long HUANG, Hiromi Wada
Принадлежит: Delta Fly Pharma Inc

This invention provides a novel RNAi molecule that can significantly potentiate antitumor effects of a 5-FU antitumor agent. The RNAi molecule comprises the nucleotide sequence shown in SEQ ID NO: 2. The invention also provides an antitumor agent comprising such RNAi molecule and a 5-FU antitumor agent.

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Номер записи: 45
19-01-2012 дата публикации

Method for Synthesizing Pirfenidone

Номер: US20120016133A1
Автор: Michael Cyr, Ramachandran Radhakrishnan, Sabine M. Pyles
Принадлежит: Intermune Inc

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

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Номер записи: 46
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.

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Номер записи: 47
26-01-2012 дата публикации

Adverse side-effects associated with administration of anti-hyaluronan agents and methods for ameliorating or preventing the side-effects

Номер: US20120020951A1
Автор: Curtis Thompson, Gregory I. Frost, Harold Michael Shepard, Xiaoming Li
Принадлежит: Individual

Provided herein are methods for ameliorating an adverse effect of systemic administration of a PEG hyaluronan degrading enzyme to a subject. The methods involve systemically administering a PEGylated hyaluronan degrading enzyme, particularly a PEGylated hyaluronidase, such as any of the animal or bacterial hyaluronidases, to the subject and administering an amount of a corticosteroid sufficient to ameliorate the adverse effect. Also provided are method of treating a hyaluronan-associated disease or condition for single-agent therapy or combination therapy.

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Номер записи: 48
26-01-2012 дата публикации

Garcinia Mangostana L. and Iridoid Based Formulations

Номер: US20120021079A1
Автор: Afa Kehaati Palu, Brett Justin West, Claude Jarakae Jensen, Jeffery A. Wasden, Shixin Deng
Принадлежит: Individual

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

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Номер записи: 49
26-01-2012 дата публикации

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

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

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

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Номер записи: 50
26-01-2012 дата публикации

Composition and methods of treatment of bacterial meningitis

Номер: US20120022031A1
Автор: Robert B. Boyd
Принадлежит: NBR PATHFINDER LLC

A diluted solution of ceftiofur sodium is intrathecally or ventricularly delivered to effectively treat bacterial meningitis while maintaining the patient's threshold and reducing the likelihood of seizure.

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Номер записи: 51
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.

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Номер записи: 52
26-01-2012 дата публикации

Thiazole and oxazole-substituted arylamides as p2x3 and p2x2/3 antagonists

Номер: US20120022067A1
Автор: Li Chen, Lichun Feng, Michael Patrick Dillon, Minmin YANG, Ronald Charles Hawley
Принадлежит: Individual

Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R 1 is a group of formula A or formula B, and X, R 2 , R 3 , R 4 , R 5 , R 6 , R a and R b are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X 3 and/or a P2X 2/3 receptor antagonist and methods of making the subject compounds.

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Номер записи: 53
26-01-2012 дата публикации

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

Номер: US20120022076A1
Автор: Andreas Maderna, Dinesh Barawkar, Hassan El Abdellaoul, Jean-Michel Vernier, Varaprasad Chamakura, Zhi Hong
Принадлежит: Individual

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

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Номер записи: 54
26-01-2012 дата публикации

Heterocyclic antagonists of prostaglandin d2 receptors

Номер: US20120022119A1
Автор: Brian Andrew Stearns, Jeffrey Roger Roppe, John Howard Hutchinson, Nicholas Simon Stock, Timothy Parr
Принадлежит: Amira Pharmaceuticals Inc

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

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Номер записи: 55
26-01-2012 дата публикации

Short Interfering Ribonucleic Acid (siRNA) for Oral Administration

Номер: US20120022139A1
Автор: Christian Rene Schnell, Eric Billy, Francois Jean-Charles Natt, Juerg Hunziker
Принадлежит: NOVARTIS AG

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

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Номер записи: 56
26-01-2012 дата публикации

Delayed release, oral dosage compositions that contain amorphous cddo-me

Номер: US20120022156A1
Автор: Colin J. Meyer, Jiang Zhang
Принадлежит: Reata Pharmaceuticals Inc

Pharmaceutical formulations exhibit a desirably low Cmax, among other properties, that contain particles of amorphous bardoxolone methyl, either in pure form or in the form of a solid dispersion, admixed with particles of a hydrophilic binding agent. Such formulations possess the advantage of higher oral bioavailability, relative to formulations based on the crystalline form of bardoxolone methyl.

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Номер записи: 57
26-01-2012 дата публикации

Dosing and monitoring patients on nitrogen-scavenging drugs

Номер: US20120022157A1
Автор: Bruce Scharschmidt
Принадлежит: Ucyclyd Pharma Inc

The invention provides a method for determining a dose and dosing schedule, and making dose adjustments of patients taking PBA prodrugs as nitrogen scavengers to treat nitrogen retention states, including ammonia accumulation disorders as well as chronic renal failure, by measuring urinary excretion of phenylacetylglutamine and/or total urinary nitrogen. The invention provides methods to select an appropriate dosage of a PBA prodrug based on the patient's dietary protein intake, or based on previous treatments administered to the patient. The methods are applicable to selecting or modifying a dosing regimen for a subject receiving an orally administered waste nitrogen scavenging drug, and to monitoring patients receiving such drugs.

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Номер записи: 58
26-01-2012 дата публикации

Recombinant Anti-VLA4 Antibody Molecules

Номер: US20120022236A1
Автор: Frank J. Carr, Philip R. Tempest, Roy R. Lobb
Принадлежит: BIOGEN IDEC MA INC

The present invention disclosed recombinant anti-VLA-4 antibody molecules, including humanized recombinant anti-VLA-4 antibody molecules. These antibodies are useful in the treatment of specific and non-specific inflammation, including asthma and inflammatory bowel disease. In addition, the humanized recombinant anti-VLA-4 antibodies disclosed can be useful in methods of diagnosing and localizing sites of inflammation.

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Номер записи: 59
26-01-2012 дата публикации

Novel method for producing optically active pyrrolidine compound

Номер: US20120022271A1
Автор: Atsushi Ohigashi, TAKASHI KIKUCHI
Принадлежит: Astellas Pharma Inc

[Object] A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided. [Means for Solution] According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate. [Selected Figure] None

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Номер записи: 60
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.

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Номер записи: 61
02-02-2012 дата публикации

Transdermal pharmaceutical preparations

Номер: US20120024743A1
Автор: Endre Mikulásik, Patrik Fazekas
Принадлежит: EGIS PHARMACEUTICALS PLC

The present invention relates to semisolid transdermal pharmaceutical preparation having enhanced stability and bioavailability, wherein the particles are coated by a volatile silicon oil component and the thus obtained suspension is dispersed in a gel or cream base.

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Номер записи: 62
02-02-2012 дата публикации

Cancer therapy based on tumor associated antigens derived from cyclin d1

Номер: US20120027684A1
Автор: Harpreet Singh, Steffen Walter, Toni Weinschenk
Принадлежит: IMMATICS BIOTECHNOLOGIES GMBH

The present invention relates to cyclin D1-derived peptides for use in the improved treatment of cancer in a patient, particularly in the form of a combination therapy using a vaccine. Other aspects relate to the use of the peptides or a combination thereof as a diagnostic tool.

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Номер записи: 63
02-02-2012 дата публикации

Methods for treating adult respiratory distress syndrome

Номер: US20120027742A1
Автор: Jahar Bhattacharya, Sadiqa K. Quadri, Shonit Das
Принадлежит: Columbia University of New York

We have discovered that the activated phosphorylated form of focal adhesion kinase (hereafter “FAKp”) strengthens the microvascular endothelial cell (EC) junctions that form a barrier in pulmonary endothelia, and the increased barrier helps to prevent acute lung injury (ALI) and acute respiratory distress syndrome (ARDS). Thus certain embodiments of the invention are directed to prevention and treatment of ALI and ARDS by administering a therapeutically effective amount of FAKp to subjects at risk of developing or diagnosed as having either ALI or ARDS.

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Номер записи: 64
02-02-2012 дата публикации

Antibody gene transfer and recombinant aav therefor

Номер: US20120027798A1
Автор: Kelly Reed Clark, Philip R. Johnson, Jr.
Принадлежит: Nationwide Childrens Hospital Inc

The present invention relates generally to the use of recombinant adeno-associated viruses (rAAV) for gene delivery and more specifically to the use of rAAV to deliver antibody genes to target cells in mammals. Administration of rAAV encoding antibodies that neutralize the HIV-1 virus is exemplified.

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Номер записи: 65
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.

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Номер записи: 66
02-02-2012 дата публикации

Natural marine source phospholipids comprising polyunsaturated fatty acids and their applications

Номер: US20120028922A1
Автор: Fotini Sampalis
Принадлежит: Individual

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

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Номер записи: 67
02-02-2012 дата публикации

Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases

Номер: US20120028925A1
Автор: Andrew J. Souers, Gerard M. Sullivan, Nathaniel D. Catron, Xilu Wang, Zhi-Fu Tao
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

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Номер записи: 68
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.

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Номер записи: 69
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.

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Номер записи: 70
02-02-2012 дата публикации

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

Номер: US20120028961A1
Автор: Ajay Singh, Andrew Caerwyn Williams, Arundhati S. Deo, Christopher Stanley Galka, Christopher Stephen Siedem, Deyi Zhang, Frantz Victor, John Gordon Allen, Karin Briner, Maria Angeles Martinez-Grau, Matthew Robert Reinhard, Michael John Rodriguez, Michael Philip Cohen, Michael Philip Mazanetz, Michael Wade Tidwell, Richard Gerard Conway, Roger Ryan Rothhaar, Sarah Lynne Hellman, Steven Armen Boyd, Wai-Man Lee
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.

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Номер записи: 71
02-02-2012 дата публикации

Biomarker assays for detecting or measuring inhibition of tor kinase activity

Номер: US20120028972A1
Автор: Jian-hua DING, Lilly Wong, Shuichan Xu
Принадлежит: Signal Pharmaceuticals LLC

Provided herein are methods for detecting and/or measuring the inhibition of TOR kinase activity in a subject and uses associated therewith.

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Номер записи: 72
02-02-2012 дата публикации

Nitroimidazooxazines and their uses in anti-tubercular therapy

Номер: US20120028973A1
Автор: Adrian Blaser, Andrew Mark Thompson, Brian Desmond Palmer, Hamish Scott Sutherland, Iveta Kmentova, William Alexander Denny, Zhenkun Ma
Принадлежит: Global Alliance for TB Drug Development

The present invention relates to novel nitroimidazooxazines, to their preparation, and to their use as drugs for treating Mycobacterium tuberculosis and other microbial infections, either alone or in combination with other anti-infective treatments.

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Номер записи: 73
02-02-2012 дата публикации

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

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

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

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Номер записи: 74
02-02-2012 дата публикации

7-azoniabicyclo[2.2.1]heptane derivatives, methods of production, and pharmaceutical uses thereof

Номер: US20120029044A1
Автор: Gwenaella Rescourio, Jurg R. Pfister, Meenakshi S. Venkatraman, Xiaoming Zhang
Принадлежит: Theron Pharmaceuticals Inc

Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.

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Номер записи: 75
02-02-2012 дата публикации

Short Interfering Ribonucleic Acid (siRNA) for Oral Administration

Номер: US20120029052A1
Автор: Christian Rene Schnell, Eric Billy, Francois Jean-Charles Natt, Juerg Hunziker
Принадлежит: NOVARTIS AG

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

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Номер записи: 76
02-02-2012 дата публикации

Compositions and methods for treating or preventing radiation injury

Номер: US20120029071A1
Автор: Rajesh K. Thimmulappa, Shyam Biswal
Принадлежит: JOHNS HOPKINS UNIVERSITY

The invention provides compositions and methods featuring Nrf2 activators for treating or preventing radiation-associated tissue damage.

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Номер записи: 77
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.

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Номер записи: 78
09-02-2012 дата публикации

Dry powder formulation comprising a phosphodiesterase inhibitor

Номер: US20120031403A1
Автор: Daniela Cocconi, Francesca Schiaretti, Roberto Bilzi
Принадлежит: Chiesi Farmaceutici SpA

Pharmaceutical formulations in the form of inhalable dry powder comprising particles of a phosphodiesterase-4 inhibitor as active ingredient are useful for the prevention and/or treatment of respiratory diseases, such as asthma and COPD.

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Номер записи: 79
09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

Номер: US20120032158A1
Автор: Daniel David Lecloux, YING Wang
Принадлежит: EI Du Pont de Nemours and Co

The present invention is directed to a photoactive device comprising an anode, a cathode, and a photoactive layer, which device further comprises an electron transport and/or anti-quenching layer which minimizes both electron transfer quenching and energy transfer quenching of the photoactive layer.

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Номер записи: 80
09-02-2012 дата публикации

Extracellular matrix compositions for tissue regeneration

Номер: US20120034191A1
Автор: Robert G. Matheny
Принадлежит: Individual

The invention is compositions of extracellular matrix that comprise mammalian extracellular matrix from two or more tissue sources in a mammal. The invention also includes methods of using these compositions to regenerate tissue or generate new tissue at sites of defects or wounds in mammals.

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Номер записи: 81
09-02-2012 дата публикации

Treatment of neurotrophic factor mediated disorders

Номер: US20120034193A1
Автор: Antonia Orsi, Daryl Rees, Patrick Howson, Yaer Hu, Zongqin Xia
Принадлежит: Phytopharm Ltd

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

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Номер записи: 82
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.

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Номер записи: 83
09-02-2012 дата публикации

Methods of treating secondary bone tumors with antibodies against pdgfr alpha

Номер: US20120034244A1
Автор: Alessandro FATATIS, Nathan Graeme DOLLOFF, Nick LOIZOS
Принадлежит: ImClone LLC, Philadelphia Health and Education Corp

The invention provides methods of treating bone cancer, particularly metastatic bone cancer, by administering an IGF-IR antagonist and/or a PDGFRα antagonist. The invention also provides antibodies that bind to human PDGFRα and neutralize activation of the receptor. The invention further provides a methods for neutralizing activation of PDGFRα, and a methods of treating a mammal with a neoplastic disease using the antibodie alone or in combination with other agents.

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Номер записи: 84
09-02-2012 дата публикации

Ophthalmic preparation containing menthyl ester of indomethacin

Номер: US20120034278A1
Автор: Joseph Schwarz, Michael Weisspapir
Принадлежит: Alpharx Inc

There is provided an ophthalmic pharmaceutical preparation comprising menthyl ester of indomethacin as an active ingredient. Also provided are different possible formulations of the ophthalmic preparation, and different methods of treating ophthalmic irritation using the ophthalmic preparation.

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Номер записи: 85
09-02-2012 дата публикации

Prolonged duration local anesthesia with minimal toxicity

Номер: US20120034296A1
Автор: Daniel S. Kohane, Hila Epstein-Barash
Принадлежит: Childrens Medical Center Corp, Massachusetts Institute of Technology

Compositions containing site 1 sodium channel blockers for use as local anesthetics with rapid nerve block, improved potency and efficacy, and no local toxicity have been developed. Liposomes were employed for increased loading of the site 1 sodium channel blocker, producing prolonged duration of block without systemic toxicity. In one embodiment, the compositions contain a site 1 sodium channel blocker alone. In another embodiment, the compositions contain a site 1 sodium channel blocker in combination with a corticosteroid. As demonstrated by the examples, encapsulating site 1 sodium channel blockers in liposomes results in rapid and prolonged nerve block without systemic toxicity, which is enhanced by the addition of a corticosteroid. Fluid liposomes showed more rapid release of STX than did solid ones, and dexamethasone accelerated STX release.

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Номер записи: 86
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.

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Номер записи: 87
09-02-2012 дата публикации

Antibiotic product, use and formulation thereof

Номер: US20120035121A1
Автор: Donald J. Treacy, Jr., Edward M. Rudnic, James D. Isbister, Sandra E. Wassink
Принадлежит: Shionogi Inc

An antibiotic product is comprised of at least two dosages forms, each of which has a different release profile, with the C max for the antibiotic product being reached in less than about twelve hours. In one embodiment, there is an immediate release dosage form, as well as one or more delayed release dosage forms, with each of the dosage forms having a different release profile, wherein each reaches a C max at different times.

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Номер записи: 88
09-02-2012 дата публикации

Combination of compounds for treating or preventing skin diseases

Номер: US20120035123A1
Автор: André Jomard, Laurent Fredon, Olivier Roye
Принадлежит: Galderma Research and Development SNC

A combination of compounds for treating skin diseases and particularly rosacea and ocular rosacea is described. The combination of a compound of the avermectin family or of the mylbemycin family with a compound of the family of the alpha-1 or alpha-2 adrenergic receptor agonists is also described. In addition, a product in the form of a kit including: (a) a first composition containing a compound of the avermectin family or of the mylbemycin family, and (b) a second composition different from the first one and containing a compound of the family of the alpha-1 or alpha-2 adrenergic receptor agonists, as a combination product to be used as a drug for treating and/or preventing skin diseases and particularly rosacea and ocular rosacea, wherein said first and second compositions can be applied simultaneously, separately or with a time delay is described.

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Номер записи: 89
09-02-2012 дата публикации

Ophthalmic compositions and methods for treating ophthalmic conditions

Номер: US20120035148A1
Автор: Scott M. Whitcup
Принадлежит: Allergan Inc

Compositions, and methods of using such compositions, useful for placement, for example injection, into the interior of human or animal eyes are provided. Such compositions include a therapeutic component, such as one or more corticosteroids, a biocompatible polymeric component, and a solvent component.

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Номер записи: 90
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.

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Номер записи: 91
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).

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Номер записи: 92
09-02-2012 дата публикации

Pharmaceutical composition for treating cancer comprising chlorin e6-folic acid conjugate compound and chitosan

Номер: US20120035180A1
Автор: Eun Hee Lee, Hyo Jun Kim, Kye Shin Park
Принадлежит: Diatech Korea Co Ltd

The present invention relates to a pharmaceutical composition for the treatment of cancer comprising a chlorin e6-folic acid conjugate compound and chitosan, and more particularly, to a pharmaceutical composition for photodynamic therapy of solid tumors comprising the novel chlorin e6-folic acid conjugate compound or a pharmaceutically acceptable salt thereof and chitosan, in which the novel compound is prepared by linking chlorin e6 to folic acid, and effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic treatment for malignant tumors.

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Номер записи: 93
09-02-2012 дата публикации

Antiparasitic agent for fish and method of controlling proliferation of fish parasites

Номер: US20120035181A1
Автор: Fumi Kawano, Noritaka Hirazawa
Принадлежит: Nippon Suisan Kaisha Ltd

A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.

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Номер записи: 94
09-02-2012 дата публикации

Compound for the Treatment of Tuberculosis

Номер: US20120035219A1
Автор: David Alan Melnick, Kaveri Das, Shandil Radha
Принадлежит: AstraZeneca AB

(5R)-3-[4-[1-[(2S)-2,3-dihydroxypropanoyl]-3,6-dihydro-2H-pyridin-4-yl]-3,5-difluoro-phenyl]-5-(isoxazol-3-yloxymethyl)oxazolidin-2-one, or a pharmaceutically-acceptable salt, or an in-vivo-hydrolysable ester thereof, for use in the treatment of Mycobacterium tuberculosis.

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Номер записи: 95
09-02-2012 дата публикации

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

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

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

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Номер записи: 96
16-02-2012 дата публикации

Methods of treating pain

Номер: US20120039866A1
Автор: Daniela Salvemini
Принадлежит: St Louis University

The invention relates to methods for treating pain disorders including neuropathic and inflammatory pain and to methods to reduce or eliminate nociceptive tolerance induced by opiate analgesic use by administering an agent that suppresses or blocks S1P biological activity.

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Номер записи: 97
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.

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Номер записи: 98
16-02-2012 дата публикации

Methods Of Immune Modulation

Номер: US20120039945A1
Автор: Gill Diamond, Richard W. Scott
Принадлежит: Polymedix Inc, UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY

The present invention provides compounds and compositions thereof that modulate the immune system.

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Номер записи: 99
16-02-2012 дата публикации

Mini-Hepcidin Peptides and Methods of Using thereof

Номер: US20120040894A1
Автор: Elizabeta Nemeth, Gloria Preza, Piotr Ruchala, Tomas Ganz
Принадлежит: UNIVERSITY OF CALIFORNIA

Disclosed herein are peptides which exhibit hepcidin activity and methods of making and using thereof.

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Номер записи: 100