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 66660. Отображено 100.
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: 1
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: 2
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: 3
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.

Подробнее
Номер записи: 4
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.

Подробнее
Номер записи: 5
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: 6
19-01-2012 дата публикации

(2,5-dioxoimidazolidin-i-yl)-n-hydroxy-acetamides as metalloproteinase inhibitors

Номер: US20120015994A1
Автор: Bertil Samuelsson, Guo-Qiang Lin, Hans Wallberg, Kevin Parkes, Ming-Hua Xu, Piaoyang Sun, Tony Johnson, Xin-Sheng Lei
Принадлежит: Medivir AB

The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).

Подробнее
Номер записи: 7
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: 8
26-01-2012 дата публикации

Use of Simple Amino Acids to Form Porous Particles

Номер: US20120020887A1
Автор: Michael M. Lipp, Ralph W. Niven, Richard P. Batycky
Принадлежит: Individual

Particles having a tap density of less than 0.4 g/cm 3 include a hydrophobic amino acid or salt thereof and a therapeutic, prophylactic or diagnostic agent or any combination thereof. Preferred particles include a phospholipid, have a median geometric diameter between about 5 and about 30 microns and an aerodynamic diameter between about 1 and about 5 microns. The particles can be formed by spray-drying and are useful for delivery to the pulmonary system.

Подробнее
Номер записи: 9
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.

Подробнее
Номер записи: 10
26-01-2012 дата публикации

METHODS FOR TREATING IgE-MEDIATED DISORDER

Номер: US20120020979A1
Автор: Andrea Cerutti, KANG Chen
Принадлежит: CORNELL UNIVERSITY

This invention relates to methods of treating IgE mediated disorders such as allergy and asthma based on activating surface-bound IgD molecules on basophils. The invention also relates to methods of making IgD, as well as methods of screening for antimicrobial agents from IgD-activated basophils.

Подробнее
Номер записи: 11
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.

Подробнее
Номер записи: 12
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.

Подробнее
Номер записи: 13
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.

Подробнее
Номер записи: 14
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.

Подробнее
Номер записи: 15
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: 16
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: 17
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.

Подробнее
Номер записи: 18
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.

Подробнее
Номер записи: 19
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.

Подробнее
Номер записи: 20
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.

Подробнее
Номер записи: 21
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: 22
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: 23
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: 24
09-02-2012 дата публикации

Sphingo-guanidines and their use as inhibitors of sphingosine kinase

Номер: US20120035268A1
Автор: Alicja Bielawska, James Norris, Lina M. Obeld, LIU Xiang, Yusuf A. Hannun, Zdzislaw M. Szulc
Принадлежит: Medical University of South Carolina (MUSC)

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

Подробнее
Номер записи: 25
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: 26
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: 27
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: 28
23-02-2012 дата публикации

Compositions for targeting conducting airway cells comprising adeno-associated virus constructs

Номер: US20120046349A1
Автор: Christie L. Bell, James M. Wilson
Принадлежит: University of Pennsylvania Penn

An artificial AAV capsid comprising a heterologous conducting airway targeting sequence is provided. The artificial AAV is useful as a targeting moiety, for delivery of heterologous molecules which are associated therewith. The artificial AAV is also useful in the generation of AAV vectors having the artificial capsid. Also described are methods of modifying the native tropism and transduction efficiency of vectors by improving and/or ablating their ability to transduce conducting airway cells. Methods of targeting conducting airway cells and delivering therapeutic and other molecules thereto are also provided.

Подробнее
Номер записи: 29
01-03-2012 дата публикации

Use of glycyrrhetinic acid, glycyrrhizic acid and related compounds for prevention and/or treatment of pulmonary fibrosis

Номер: US20120053141A1
Автор: Jianhua Xu, Lurong Zhang, Shanmin Yang, Weijian Zhang
Принадлежит: Individual

The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GLA) and related compounds for prevention and/or treatment of pulmonary fibrosis, in particular, irradiation-induced pulmonary fibrosis. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GLA). The present invention also provides for therapeutic or pharmaceutical compositions comprising a compound of the invention in a form that can be combined with a pharmaceutically acceptable carrier.

Подробнее
Номер записи: 30
01-03-2012 дата публикации

Tri-cyclic pyrazolopyridine kinase inhibitors

Номер: US20120053187A1
Автор: Alex Aronov, Arnaud Le Tiran, David Messersmith, Emilie Porter Huck, Gabriel Martinez Botella, Jon H. Come, Kevin Michael Cottrell, Ronald Lee Grey, Jr., Valerie Marone
Принадлежит: Vertex Pharmaceuticals Inc

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

Подробнее
Номер записи: 31
08-03-2012 дата публикации

Anti- integrin antibodies, compositions, methods and uses

Номер: US20120058128A1
Автор: Jill Giles-Komar, Linda Snyder, Marian T. Nakada, Mohit Trikha
Принадлежит: Janssen Biotech Inc

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

Подробнее
Номер записи: 32
08-03-2012 дата публикации

Macrolides with Anti-Inflammatory Activity

Номер: US20120058963A1
Автор: Antun Hutinec, Dubravko Jelic, Goran Kragol, Marija Ribic, Martina Bosnar, Nikola Marjanovic, Ognjen Culic, Sulejman Alihodzic, Vanja Vela, Vesna Erakovic Haber, Zorica Marusic-Istuk
Принадлежит: Glaxo Group Ltd

The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4″ position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

Подробнее
Номер записи: 33
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: 34
08-03-2012 дата публикации

Combinations comprising antimuscarinic agents and pde4 inhibitors

Номер: US20120059031A1
Автор: Hamish Ryder, Jesus Llenas Calvo, Jordi Gras Escardo, Pio Orviz Diaz
Принадлежит: Individual

A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid.

Подробнее
Номер записи: 35
08-03-2012 дата публикации

Novel crystalline hydrate, amorphous and polymorphic forms of dihydro-benzoxazole-6-yl-acetamide derivative and processes for their preparation

Номер: US20120059034A1
Автор: Ádám DEMETER, Andras Nemes, Ferenc SEBÕK, Gizella Bartane Szalai, László Czibula, Zoltán NÉMET
Принадлежит: Richter Gedeon Nyrt

The invention relates to novel crystalline hydrate, amorphous and crystalline polymorphic forms of 2-[4-(4-Fluoro-benzyl)-piperidine-1-yl]-2-oxo-N-(2-oxo-2,3-dihydro-benzoxazole-6-yl)-acetamide (I) (radiprodil). Processes for the preparation of these forms, compositions containing these forms, and methods of use thereof are also described.

Подробнее
Номер записи: 36
15-03-2012 дата публикации

Il-17 homologous polypeptides and therapeutic uses thereof

Номер: US20120064073A1
Автор: Audrey Goddard, Austin L. Gurney, Colin K. Watanabe, Daniel G. Yansura, Daniel Tumas, Dorothy French, Ellen Fllvaroff, Hanzhong Li, J. Christopher Grimaldi, James Pan, Jian Chen, Kenneth J. Hillan, Melissa A. Starovasnik, Menno Van Lookeren, P. Mickey Williams, Paul J. Godowski, Richard Vandlen, Sarah G. Hymowitz, Sherman Fong, William I. Wood
Принадлежит: Individual

The present invention is directed to novel polypeptides having sequence identity with IL-17, IL-17 receptors and to nucleic acid molecules encoding those polypeptides. Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases.

Подробнее
Номер записи: 37
15-03-2012 дата публикации

Compounds and their uses 708

Номер: US20120065214A1
Автор: Piotr Raubo, Richard Evans, Stephen Brough, Timothy Jon Luker
Принадлежит: AstraZeneca AB

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

Подробнее
Номер записи: 38
15-03-2012 дата публикации

Salts of tiotropium with 10-camphorsulfonic acid

Номер: US20120065226A1
Автор: Helena Modrzejewska, Magdalena Dziedzic-Lysiak, Zbigniew Majka
Принадлежит: Adamed Sp zoo

The present invention relates to novel tiotropium salts with 10-camphorsulphonic acid of formula (I), its optical isomers or their mixtures, their monohydrates, their anhydrous crystalline forms and processes for the preparation thereof, as well as to pharmaceutical compositions containing the same and to the use of novel salts for the treatment of respiratory tract diseases.

Подробнее
Номер записи: 39
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: 40
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: 41
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: 42
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: 43
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: 44
29-03-2012 дата публикации

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

Номер: US20120077858A1
Автор: David F. Woodward, Jenny W. Wang, Jose L. Martos, Jussi J. Kangasmetsa, William R. Carling
Принадлежит: Allergan Inc

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

Подробнее
Номер записи: 45
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: 46
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: 47
05-04-2012 дата публикации

Methods of using il-31 to treat chronic obstructive pulmonary disease (copd)

Номер: US20120083456A1
Автор: Eric M. Chadwick, Janine M. Bilsborough, Sherri L. Mudri
Принадлежит: Zymogenetics Inc

Use of IL-31 agonists, including IL-31, are used to treat agonists are used to treat asthma, airway hyper-responsiveness or allergic rhinitis. The method comprise inhibiting, reducing, limiting or minimizing production of proinflammatory cytokines and include administration of the IL-31 agonist during sensitization or challenge resulting in the asthma, airway hyper-responsiveness or allergic rhinitis state.

Подробнее
Номер записи: 48
12-04-2012 дата публикации

Therapeutic and diagnostic anti-hsp70 antibodies

Номер: US20120087931A1
Автор: Gabriele Multhoff
Принадлежит: Multimmune GmbH

Methods and compositions for the detection, prevention and treatment of infectious diseases, primary and metastatic neoplastic diseases, including, but not limited to human sarcomas and carcinomas are described. In particular, specific antibodies are provided, which are capable of binding an epitope of Hsp70 that is extracellularly localized on diseased tissue and cells, in particular on tumor cells and infected cells.

Подробнее
Номер записи: 49
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: 50
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: 51
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: 52
12-04-2012 дата публикации

1-heterocyclylsulfonyl, 3-aminomethyl, 5- (hetero-) aryl substituted 1-h-pyrrole derivatives as acid secretion inhibitors

Номер: US20120088797A1
Автор: Atsushi Hasuoka, Haruyuki Nishida, Masahiro Kajino
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R 1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R 2 is an optionally substituted C 6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R 3 and R 4 are each a hydrogen atom, or one of R 3 and R 4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R 5 is an alkyl group or a salt thereof.

Подробнее
Номер записи: 53
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: 54
19-04-2012 дата публикации

Egfr inhibitors and methods of treating disorders

Номер: US20120094999A1
Автор: Michael J. Eck, Nathanael S. Gray, Pasi Janne, Wenjun Zhou
Принадлежит: Dana Farber Cancer Institute Inc

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

Подробнее
Номер записи: 55
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: 56
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: 57
26-04-2012 дата публикации

Antibodies having altered effector function and methods for making the same

Номер: US20120100575A1
Автор: Ellen Garber, Frederick R. Taylor
Принадлежит: BIOGEN IDEC MA INC

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

Подробнее
Номер записи: 58
26-04-2012 дата публикации

Inhibition of secretion from non-neuronal cells

Номер: US20120101027A1
Автор: Conrad Padraig Quinn, John Andrew Chaddock, John Robert Purkiss, Keith Alan Foster
Принадлежит: Syntaxin Ltd

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

Подробнее
Номер записи: 59
26-04-2012 дата публикации

Carbonate derivatives for the treatment of cough

Номер: US20120101076A1
Автор: Pierangelo Geppetti, Riccardo Patacchini
Принадлежит: Chiesi Farmaceutici SpA

The invention relates to use of certain quinuclidine carbonate derivatives as cough suppressants, particularly for treating patients with upper respiratory tract infections or asthma.

Подробнее
Номер записи: 60
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: 61
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: 62
26-04-2012 дата публикации

Pure isomers of tritoqualine

Номер: US20120101120A1
Автор: Emile Loria, Gaetan Terrasse, Michalis Nicolaou, Yves Trehin
Принадлежит: Individual

The invention provides an isolated stereoisomer of tritoqualine having the structure of FIG. 2 and FIG. 3.

Подробнее
Номер записи: 63
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: 64
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: 65
03-05-2012 дата публикации

Films and particles

Номер: US20120107365A1
Автор: Aaron Griset, Jesse Wolinsky, Mark Grinstaff, Solomon Azouz, Yolonda Colson
Принадлежит: Boston University, Brigham and Womens Hospital Inc

Described herein are compounds and processes that can be used to prepare polymer-based films, particles, gels and related compositions, and processes for delivery of agents, and other uses.

Подробнее
Номер записи: 66
03-05-2012 дата публикации

Pharmaceutical formulations and methods for treating respiratory tract infections

Номер: US20120107414A1
Автор: David L. Hava, John Hanrahan, Michael M. Lipp, Richard Batycky, Robert W. Clarke
Принадлежит: Pulmatrix Inc

The present invention relates to pharmaceutical formulations for treating a respiratory tract infection or a pulmonary disease in an individual, comprising a calcium salt and a sodium salt, wherein the ratio of Ca +2 to Na + is from about 4:1 (mole:mole) to about 16:1 (mole:mole). The invention also relates to methods of treating (including prophylactically treating) and reducing the spread of a respiratory tract infection, methods of treating (including prophylactically treating) a pulmonary disease or an acute exacerbation of a pulmonary disease, and methods of reducing the spread of an acute exacerbation of a pulmonary disease, comprising administering a pharmaceutical formulation that comprises a calcium salt and a sodium salt.

Подробнее
Номер записи: 67
03-05-2012 дата публикации

Azaquinazolinediones Chymase Inhibitors

Номер: US20120108597A1
Автор: Chuk Chui Man, Hidenori Takahashi, Xin Guo
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.

Подробнее
Номер записи: 68
03-05-2012 дата публикации

Recombinant il-9 antibodies and uses thereof

Номер: US20120109097A1
Автор: Herren Wu, Jeffry D. Watkins, Jennifer Lynne Reed, Julian Davies, Ying Tang
Принадлежит: MEDIMMUNE LLC

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

Подробнее
Номер записи: 69
10-05-2012 дата публикации

TGR5 Modulators and Methods of Use Thereof

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

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

Подробнее
Номер записи: 70
10-05-2012 дата публикации

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors

Номер: US20120116091A1
Автор: Elisabetta Armani, Gabriele Amari, Maurizio Delcanale
Принадлежит: Chiesi Farmaceutici SpA

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Подробнее
Номер записи: 71
10-05-2012 дата публикации

Human antibodies derived from immunized xenomice

Номер: US20120117669A1
Автор: Aya Jakobovits, Daniel G. Brenner, Daniel J. Capon, Raju Kucherlapati, Sue Klapholz
Принадлежит: Abgenix Inc

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

Подробнее
Номер записи: 72
17-05-2012 дата публикации

Dry whole milk preparations containing probiotic micro-organisms

Номер: US20120121561A1
Автор: Annick Mercenier, Guénolée Prioult, Sophie Nutten
Принадлежит: Nestec SA

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

Подробнее
Номер записи: 73
17-05-2012 дата публикации

Biodegradable immunomodulatory formulations and methods for use thereof

Номер: US20120121622A1
Автор: Dino Dina, Gary Van Nest, Karen L. Fearon, Stephen Tuck
Принадлежит: Dynavax Technologies Corp

The invention provides new compositions and methods for immunomodulation of individuals. Immunomodulation is accomplished by administration of immunomodulatory polynucleotide/microcarrier (IMP/MC) complexes. The IMP/MC complexes may be covalently or non-covalently bound, and feature a polynucleotide comprising at least one immunostimulatory sequence bound to a biodegradable microcarrier or nanocarrier.

Подробнее
Номер записи: 74
17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

Номер: US20120122764A1
Автор: Gary Michael Ksander, Muneto Mogi, Nikolaus Schiering, Qian Liu, Rajeshri Ganesh Karki, Robert Sun, Toshio Kawanami
Принадлежит: NOVARTIS AG

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

Подробнее
Номер записи: 75
17-05-2012 дата публикации

Prodrugs and the use thereof

Номер: US20120122820A1
Автор: Claudia Hirth-Dietrich, Hanna Tinel, Hans-Georg Lerchen, Jörg Keldenich, Nicole Diedrichs, Thomas Krahn, Ursula Krenz
Принадлежит: Bayer Schering Pharma AG

The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.

Подробнее
Номер записи: 76
17-05-2012 дата публикации

Aurora kinase modulators and method of use

Номер: US20120122847A1
Автор: Bingfan Du, Hanh Nho Nguyen, Holly Deak, Issac Marx, Karina Romero, Kathleen Panter, Laurie Schenkel, Matthew Martin, Philip Olivieri, Ryan White, Stephanie Geuns-Meyer, Victor Cee, Zihao Hua
Принадлежит: AMGEN INC

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

Подробнее
Номер записи: 77
24-05-2012 дата публикации

Thienopyrimidines for pharmaceutical compositions

Номер: US20120128686A1
Автор: Ian Linney, John Danilewicz, Kay Schreiter, Martin Schneider, Matthias Austen, Phillip Black, Wesley Blackaby
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

Подробнее
Номер записи: 78
24-05-2012 дата публикации

Novel antibody formulation

Номер: US20120128687A1
Автор: Christine Wurth, Michael Adler
Принадлежит: Hoffmann La Roche Inc

Pharmaceutical liquid formulation of an antibody against human OX40L, a process for the preparation and uses of the formulation.

Подробнее
Номер записи: 79
24-05-2012 дата публикации

Infant feeding formulas comprising probiotic micro-organisms

Номер: US20120128726A1
Автор: Annick Mercenier, Guénolée Prioult, Sophie Nutten
Принадлежит: Nestec SA

The present invention relates to the field of infant nutrition. In particular, the present invention relates to infant feeding formulas comprising probiotic micro-organisms. These probiotic micro-organisms may be non-replicating probiotic micro-organisms such as bioactive heat treated probiotic micro-organisms, for example.

Подробнее
Номер записи: 80
24-05-2012 дата публикации

New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders

Номер: US20120129820A1
Автор: Abhya Gupta, Peter Seither
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention provides pharmaceutical compositions comprising one or more CRTH2 antagonists 1 and one or more further active compounds 2.

Подробнее
Номер записи: 81
24-05-2012 дата публикации

Pyridyl-thiazolyl inhibitors of pro-matrix metalloproteinase activation

Номер: US20120129843A1
Автор: Aihua Wang, Brett Andrew Tounge, Joseph Kent Barbay, Kristi Anne Leonard, Michael Hawkins, Umar S.M. Maharoof, Yan Zhang
Принадлежит: Janssen Pharmaceutica NV

This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables R z , Q, J, R 1 , R 3 , R 5 , and R 6 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.

Подробнее
Номер записи: 82
24-05-2012 дата публикации

Stabilized composition comprising at least one adrenergic compound

Номер: US20120129944A1
Автор: Alan J. Baillie, Kenneth MacDonald, Pamela Porteous, Simon Hendry
Принадлежит: ALK AG

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

Подробнее
Номер записи: 83
31-05-2012 дата публикации

Immunosuppressor based on the blockage of tcr-nck interaction

Номер: US20120135041A1
Автор: Aldo Borroto Revuelta, Angel Ramirez Ortiz, Antonio Morreale De Leon, Balbino ALARCÓN SÁNCHEZ, María del Carmen Fäbregas Cleveria, Maria Luz Ortiz
Принадлежит: Consejo Superior de Investigaciones Cientificas CSIC

The present invention relates to a compound of structural formula (I) and its derivatives for use as medicinal drugs. They are preferably immunosuppressive agents, with mechanism of action based on the blockage of TCR-Nck interaction.

Подробнее
Номер записи: 84
31-05-2012 дата публикации

Instant thickener comprising probiotics for hot or cold foods and beverages to be administered to dysphagic patients

Номер: US20120135044A1
Автор: Annick Mercenier, Guénolée Prioult, Sophie Nutten
Принадлежит: Nestec SA

The present invention relates to the fields of hydration and nutrition for dysphagic patients. In particular, the present invention relates to thickeners comprising probiotic microorganisms and to compositions comprising such thickeners. The probiotic micro-organisms may be non-replicating probiotic micro-organisms such as bioactive heat treated probiotic microorganisms.

Подробнее
Номер записи: 85
31-05-2012 дата публикации

Vaccine for mycoplasma infection

Номер: US20120135067A1
Автор: Kazuhiro Matsuda, Koji Ichiyama, Nobuo Nomura, Norio Katayama, Ryo Harasawa, Sachie Matsuda, Yasuo Endo, Yoshichika Arakawa, Yoshihiro Nishida, Yuko Sasaki
Принадлежит: M Bio Technology Inc, National Institute of Infectious Diseases

Disclosed is a vaccine which has a high therapeutic effect on mycoplasma infection and is highly safe. For the purpose of developing effective therapeutic methods for mycoplasma infection, mycoplasma - mimic particles which are effective as a vaccine for mycoplasma infection are provided, and also provided are bacterium-mimic particles including common bacteria. Bacterium-mimic particles such as mycoplasma - mimic particles can be provided by producing liposome particles in which a lipid antigen specific to a pathogenic bacterium such as mycoplasma is contained as a liposome-constituting lipid component. The administration of the mycoplasma - mimic particles enables the induction of a potent immunological activity in living bodies. The mycoplasma - mimic particles can be used as an excellent vaccine for the prevention or treatment of mycoplasma infection.

Подробнее
Номер записи: 86
31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

Номер: US20120135975A1
Автор: Irene E. Whitney, Jeffrey J. Hale, Vincent J. Colandrea, William K. Hagmann
Принадлежит: Merck and Co Inc

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

Подробнее
Номер записи: 87
31-05-2012 дата публикации

Inhibitors of human phosphatidylinositol 3-kinase delta

Номер: US20120135994A1
Автор: Amy Oliver, C. Gregory Sowell, Chanchal Sadhu, Edward A. Kesicki, Jennifer Treiberg, Ken Dick
Принадлежит: Icos Corp

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3Kδ, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity. Methods of using PI3Kδ inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3Kδ inhibitory compounds to inhibit PI3Kδ-mediated processes in vitro and in vivo.

Подробнее
Номер записи: 88
31-05-2012 дата публикации

Organic compounds

Номер: US20120136013A1
Автор: Hailin Zheng, Jun Zhao, Lawrence P. Wennogle, Peng Li
Принадлежит: Intra Cellular Therapies Inc

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

Подробнее
Номер записи: 89
31-05-2012 дата публикации

Fatty acids as anti-inflammatory agents

Номер: US20120136034A1
Автор: Bruce A. Freeman, Francisco J. Schopfer
Принадлежит: University of Pittsburgh

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

Подробнее
Номер записи: 90
31-05-2012 дата публикации

Pyridinyl Compounds Useful As Intermediates

Номер: US20120136158A1
Автор: Alan David Swinamer, Brian Christopher Raudenbush, Brian Nicholas Cook, Can Mao, Christian Harcken, Daniel Kuzmich, Daniel Robert Fandrick, Darren DiSalvo, Hossein Razavi, Jinhua J. Song, Jochen Neu, John Lord, Jonathan Timothy Reeves, Pingrong Liu, Thomas Wai-Ho Lee, Zhulin Tan
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.

Подробнее
Номер записи: 91
07-06-2012 дата публикации

Soft anticholinergic zwitterions

Номер: US20120141401A1
Автор: Nicholas S. Bodor
Принадлежит: Bodor Nicholas S

Soft anticholinergic zwitterions of the formulas: wherein R 1 and R 2 are both phenyl or one of R 1 and R 2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Подробнее
Номер записи: 92
07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Автор: Angelo Ceci, Annette Schuler-Metz, Dieter Wiedenmayer, Henning Priepke, Henri Doods, Ingo Konetzki, Juergen Mack, Norbert Hauel, Rainer Walter
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of the formula I wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.

Подробнее
Номер записи: 93
07-06-2012 дата публикации

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

Номер: US20120142733A1
Автор: James C. Lanter, Nalin Subasinghe, Thomas P. Markotan, Xuqing Zhang, Zhihua Sui
Принадлежит: Janssen Pharmaceutica NV

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

Подробнее
Номер записи: 94
07-06-2012 дата публикации

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

Номер: US20120142739A1
Автор: Evelyn G. Corpuz, Ken Chow, Liming Wang, Wenkui K. Fang, Wha Bin Im
Принадлежит: Allergan Inc

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

Подробнее
Номер записи: 95
07-06-2012 дата публикации

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

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

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

Подробнее
Номер записи: 96
14-06-2012 дата публикации

Polypeptide formulation

Номер: US20120148587A1
Автор: Richard L. Remmele, Jr., Wayne R. Gombotz
Принадлежит: Immunex Corp

The present invention relates to an aqueous pharmaceutical composition suitable for long-term storage of polypeptides containing an Fc domain of an immunoglobulin, methods of manufacture, methods of administration and kits containing same.

Подробнее
Номер записи: 97
14-06-2012 дата публикации

Inhibition of p38 kinase activity using substituted heterocyclic ureas

Номер: US20120149706A1
Автор: Aniko Redman, Bernd Riedl, Holger Paulsen, Holia Hatoum-Mokdad, Jacques Dumas, Jeffrey Johnson, Jill Wood, Robert Sibley, Roger A. Smith, Timothy B. Lowinger, Uday Khire, Wendy Lee, Willian J. SCOTT
Принадлежит: Individual

This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.

Подробнее
Номер записи: 98
14-06-2012 дата публикации

Methods and compositions using racemic, (r)-, and (s)-fexofenadine in combination with leukotriene inhibitors

Номер: US20120149730A1
Автор: Paul D. Rubin
Принадлежит: Individual

Methods and pharmaceutical compositions employing a terfenadine metabolite and a leukotriene inhibitor for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof. Also included are methods and compositions employing a terfenadine metabolite, a leukotriene inhibitor, and a decongestant for the treatment or prevention of inflammation or allergic disorders, such as asthma, or symptoms thereof.

Подробнее
Номер записи: 99
14-06-2012 дата публикации

Enzyme inhibitors

Номер: US20120149736A1
Автор: Alastair David Graham Donald, Andrew James Belfield, Carl Leslie North, David Festus Charles Moffat, Stewart Andrew Wayne Jones
Принадлежит: Chroma Therapeutics Ltd

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

Подробнее
Номер записи: 100