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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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Форма поиска

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 15023. Отображено 100.
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: 1
12-01-2012 дата публикации

Natriuretic activities

Номер: US20120010142A1
Автор: John C. Burnett, Jr., Timothy M. Olson
Принадлежит: Mayo Foundation for Medical Education and Research

This document provides methods and material related to natriuretic polypeptides. For example, substantially pure polypeptides having a natriuretic peptide activity, nucleic acids encoding polypeptides having a natriuretic peptide activity, host cells containing such nucleic acids, and methods for inducing a natriuretic or diuretic activity within a mammal are provided.

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Номер записи: 2
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: 3
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: 4
26-01-2012 дата публикации

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

Номер: US20120021002A1
Автор: Konstantin Ichtchenko, Philip A. Band
Принадлежит: New York University NYU

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

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Номер записи: 5
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: 6
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: 7
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: 8
02-02-2012 дата публикации

Storage-stable aqueous ophthalmic formulations

Номер: US20120028910A1
Автор: Elisabeth Latour, Harun Takruri, Jean-Philippe Combal
Принадлежит: Fovea Pharmaceuticals SA

Storage-stable, topically ocularly administrable aqueous ophthalmic formulations containing at least one closporine are useful for treating and/or preventing ophthalmic diseases or disorders afflicting humans or animals, notably related to inflammatory conditions, more particularly administrable to the front of the eye and which provide therapeutic effects to the eye as they are effective in stabilizing, enhancing and/or improving a patient's vision.

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Номер записи: 9
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: 10
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.

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Номер записи: 11
29-03-2012 дата публикации

Steroid-sparing methods of treating brain edema

Номер: US20120077744A1
Автор: Lisa Carr, Stephen Evans-Freke
Принадлежит: Neutron Ltd

The present invention relates to therapeutic regimens or protocols designed for the treatment, management or prevention of edema. In particular, the invention pertains to methods of treating or managing edema associated with brain tumors involving the administration of a therapeutically effective amount of corticorelin acetate that achieves a steroid-sparing effect.

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Номер записи: 12
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.

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Номер записи: 13
26-04-2012 дата публикации

Stable pharmaceutical composition and methods of using same

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

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

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Номер записи: 14
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.

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Номер записи: 15
17-05-2012 дата публикации

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

Номер: US20120122852A1
Автор: Andre Malanda, Catherine Gille, David Machnik, Laurent Dubois, Luc Even, Nathalie Rakotoarisoa, Yannick Evanno
Принадлежит: Sanofi Aventis France

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

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Номер записи: 16
24-05-2012 дата публикации

Autologous lymph node transfer in combination with vegf-c or vegf-d growth factor therapy to treat secondary lymphedema and to improve reconstructive surgery

Номер: US20120125348A1
Автор: Anne Saaristo, Kari Alitalo, Tuomas Tammela
Принадлежит: Vegenics Ltd

The present invention provides materials and methods for repairing tissue and using vascular endothelial growth factor C (VEGF-C) genes and/or proteins. Methods and materials related to the use of VEGF-C for the reduction of edema and improvement of skin perfusion is provided. Also provided is are materials and methods for using VEGF-C before, during, and after reconstructive surgery.

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Номер записи: 17
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.

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Номер записи: 18
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.

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Номер записи: 19
07-06-2012 дата публикации

Multimeric peptide conjugates and uses thereof

Номер: US20120141416A1
Автор: Carine Thiot, Christian Che, Michel Demeule
Принадлежит: Angiochem Inc

The present invention relates to multimeric (e.g., dimeric, trimeric) forms of peptide vectors that are capable of crossing the blood-brain barrier (BBB) or efficiently entering particular cell types. These multimeric peptide vectors, when conjugated to agents (e.g., therapeutic agents) are capable of transporting the agents across the BBB or into particular cell types. These compounds are therefore particularly useful in the treatment of neurological diseases.

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Номер записи: 20
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.

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Номер записи: 21
19-07-2012 дата публикации

[1,4]-benzodiazepines as vasopressin v2 receptor antagonists

Номер: US20120184537A1
Автор: Ann Meulemans, Erik Keller, Igor Alexnadrovich Mezine, Karel Lavrijsen, Leen Thielemans, Maarten Van Geffen, Marina Cools
Принадлежит: Shire Movetis NV

The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the invention are directed to the use of said [1,4]-benzodiazepine derivatives in therapy based on the capability of said compounds to interfere with the binding of the peptide hormone, vasopressin, to its receptors. In particular as vasopressin V2 receptor antagonists and therefore useful for treating involving increased vascular resistance, cardiac insufficiency, and water retention.

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Номер записи: 22
19-07-2012 дата публикации

Quinazolinone derivatives useful as vanilloid antagonists

Номер: US20120184571A1
Автор: Andrew James Culshaw, Christopher Thomas Brain, Edward Karol Dziadulewicz, Terance William Hart, Timothy John Ritchie
Принадлежит: NOVARTIS AG

The present invention relates to the use of a quinazolinone compound of the formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 and m are as defined in the specification and in the claims, in free form or in salt form, and, where possible, in acid addition salt form, as a vanilloid.

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Номер записи: 23
09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Автор: Bert Nolte, Birgit Roloff, Hans Schick, Heinz Graubaum, Helmut Sonnenschein, József Bálint, Klaus Linz, Sigrid Ozegowski, Werner Englberger, Wolfgang SHRÖDER
Принадлежит: GRUENENTHAL GmbH

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

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Номер записи: 24
09-08-2012 дата публикации

Methods of treating diseases with proanthocyanidin oligomers such as crofelemer

Номер: US20120202876A1
Автор: Alan S. Verkman, Lukmanee Tradtrantip, Pravin Chaturvedi, Wan Namkung
Принадлежит: Napo Pharmaceuticals Inc, UNIVERSITY OF CALIFORNIA

Disclosed herein are methods of treating diseases including gastrointestinal disorders, such as secretory diarrheas, with the proanthocyanidin oligomer, crofelemer. Also disclosed is the anti-secretory effect of crofelemer on Calcium-activated chloride channels (CaCC) and Cystic fibrosis transmembrane conductance regulator (CFTR).

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Номер записи: 25
16-08-2012 дата публикации

Methods of treating macular edema using antiedema therapeutics

Номер: US20120207682A1
Автор: Paul Ashton
Принадлежит: PSIVIDA US Inc

The invention provides methods of treating macular edema in a patient that include determining whether the patient has been diagnosed with or has experienced symptoms of macular edema for a predetermined period of time. If the patient has been diagnosed with or has experienced symptoms of macular edema for a predetermined period of time, the method of treatment includes administering a therapeutically effective amount of an AED to the patient. If the patient has not been diagnosed with or has experienced symptoms of macular edema for a predetermined period of time, the method of treatment optionally includes treating the patient with a therapy other than an AED. The invention further provides methods of treating macular edema in a patient using methods of and devices for administering an AED.

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Номер записи: 26
16-08-2012 дата публикации

Chemokine receptor antagonists and use thereof

Номер: US20120207765A1
Автор: Hiroshi Ochiai, Masaya Kokubo, Shiro Shibayama, Yoshikazu Takaoka
Принадлежит: Ono Pharmaceutical Co Ltd

A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), a preventive and/or therapeutic agent for cancerous diseases or infections, or an agent for regeneration therapy.

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Номер записи: 27
16-08-2012 дата публикации

Floating microgranules

Номер: US20120207843A1
Автор: Christophe P. Lebon, Pascal J. Suplie
Принадлежит: Debregeas Et Associes Pharma SAS

A floating granule having a solid core, on which an active ingredient is supported, and a compound capable of generating a gas discharge which is constituted by an alkaline agent, characterised in that it does not comprise an acid agent that is capable of generating a gas discharge.

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Номер записи: 28
30-08-2012 дата публикации

Pharmaceutical composition and administrations thereof

Номер: US20120220625A1
Автор: Alfredo Grossi, Christopher R. Young, Fredrick F. Van Goor, Gregor Zlokarnik, Kirk Dinehart, Kirk Overhoff, Marinus Jacobus Verwijs, Martyn Botfield, Patricia Hurter, Peter D.J. Grootenhuis, William Rowe
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

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Номер записи: 29
20-09-2012 дата публикации

Pharmaceutical composition containing irbesartan

Номер: US20120238555A1
Автор: Erela Zisman, Gershon Kolatkar
Принадлежит: Teva Pharmaceuticals USA Inc

This invention relates to pharmaceutical compositions containing irbesartan, providing oral formulations with a high relative amount or concentration of irbesartan. In one embodiment, the present invention provides an oral formulation of irbesartan containing greater than 70% w/w irbesartan. In another embodiment, the invention provides an oral formulation of irbesartan which exhibits a dissolution profile according to which greater than about 85% of the Irbesartan is dissolved within about 30 minutes using USP apparatus 2, placing the tablet in 1000 mL of 0.1N hydrochloric acid at 37° C. with paddle speed of 50 rpm. The formulation can optionally contain at least one additional active ingredient.

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Номер записи: 30
27-09-2012 дата публикации

Extended-release formulation for reducing the frequency of urination and method of use thereof

Номер: US20120244221A1
Автор: David A. Dill
Принадлежит: Wellesley Pharmaceuticals LLC

Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of a pharmaceutical composition comprising an analgesic agent formulated for extended-release.

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Номер записи: 31
15-11-2012 дата публикации

3,4,4A,10B-TETRAHYDRO-1H-THIOPYRANO-[4,3-c] ISOQUINOLINE DERIVATIVES

Номер: US20120289474A1
Автор: Alexander Mann, Armin Hatzelmann, Christian Hesslinger, Christof Zitt, Clemens Braun, Degenhard Marx, Dieter Flockerzi, Harald Ohmer, Hermann Tenor, Raimund KÜLZER, Stefan Fischer, Steffen Weinbrenner, Thomas Maier, Thomas Stengel, Torsten Dunkern, Ulrich Kautz
Принадлежит: NYCOMED GMBH

The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.

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Номер записи: 32
22-11-2012 дата публикации

Rapidly disintegrating tablet in oral cavity

Номер: US20120294940A1
Автор: Katsuji Uemura, Masaaki Sugimoto, Shinya Takatsuka, Toshinobu Komori
Принадлежит: Individual

The present invention provides a method of suppressing the bitter taste of a drug when a rapidly disintegrating tablet in an oral cavity is produced. When a rapidly disintegrating tablet in an oral cavity is produced, the bitter taste of a drug is suppressed by utilizing (a) a granule which contains a drug having a bitter taste and an excipient and in which the bitter taste has not been suppressed and (b) a granule containing a water soluble saccharide.

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Номер записи: 33
22-11-2012 дата публикации

Pharmaceutical composition comprising a glp-1 agonist, an insulin and methionine

Номер: US20120295846A1
Автор: Annika Hagendorf, Gerrit Hauck, Isabell Schoettle, Katrin Tertsch, Verena Siefke-Henzler, Werner Mueller
Принадлежит: Sanofi Aventis Deutschland GmbH

A liquid composition comprising a GLP-1 agonist or/and a pharmacologically tolerable salt thereof, an insulin or/and a pharmacologically tolerable salt thereof, and, optionally, at least one pharmaceutically acceptable excipient, wherein the composition comprises methionine, as add-on therapy with metformin where appropriate.

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Номер записи: 34
20-12-2012 дата публикации

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Автор: Anton F. J. Fliri, Barbara E. Segelstein, Christopher John O'donnell, Jacob Bradley Schwarz, Randall James Gallaschun
Принадлежит: PFIZER INC

The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.

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Номер записи: 35
27-12-2012 дата публикации

Formulations and methods for vascular permeability-related diseases or conditions

Номер: US20120329759A1
Автор: David A. Weber, David M. Kleinman, Mary E. Gerritsen, Thierry Nivaggioli
Принадлежит: Santen Pharmaceutical Co Ltd

Described herein are formulations and methods for treating, inhibiting, preventing, delaying onset, or causing regression of a disease or condition relating to vascular permeability.

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Номер записи: 36
03-01-2013 дата публикации

COMBINATION COMPOSITION, COMPRISING AS ACTIVE INGREDIENTS L-CARNITlNE OR PROPIONYL L-CARNITlNE, FOR THE PREVENTION OR TREATMENT OF CHRONIC VENOUS INSUFFICIENCY

Номер: US20130005670A1
Автор: Aleardo Koverech, Mohamed Ashraf Virmani
Принадлежит: Sigma Tau Industrie Farmaceutiche Riunite SpA

It is described a combination composition comprising as active ingredients L-carnitine or propionyl L-carnitine, troxerutine, diosmine and hesperidine, useful for the prevention and/or treatment of chronic venous diseases.

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Номер записи: 37
03-01-2013 дата публикации

Methods and products for treatment of diseases

Номер: US20130005699A1
Автор: David Bar-Or
Принадлежит: DMI Acquisition Corp

The invention provides a method of treating a disease or condition mediated by vascular hyperpermeability in an animal. The method comprises administering an amount of a danazol compound effective to inhibit vascular hyperpermeability and an amount of a second drug effective to treat the disease or condition. The invention further provides a method of inhibiting vascular hyperpermeability when it is a side effect caused by administration of a drug to, or another treatment of, an animal. The method comprises administration of an amount of a danazol compound effective to inhibit the vascular hyperpermeability. The invention also provides a method of modulating the cytoskeleton of endothelial cells in an animal comprising administering an amount of a danazol compound and an amount of a second drug effective to modulate the cytoskeleton. The present invention also relates to pharmaceutical compositions and kits comprising a danazol compound and a second drug.

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Номер записи: 38
10-01-2013 дата публикации

Synthetic peptide amides

Номер: US20130012448A1
Автор: Claudio D. Schteingart, Derek T. Chalmers, Frédérique Menzaghi, Guangcheng Jiang, Javier Sueiras-Diaz, Robert H. Spencer, Roberta Vezza Alexander, Zhiyong Luo
Принадлежит: Cara Therapeutics Inc

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P 450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.

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Номер записи: 39
17-01-2013 дата публикации

Muteins of tear lipocalin and methods for obtaining the same

Номер: US20130017996A1
Автор: Andreas Hohlbaum, Arne Skerra, Eric Boudreau, Ian Kimber, Kristian Jensen, Martin Huelsmeyer, Rebecca Dearman, Richard Jones, Steffen Schlehuber
Принадлежит: PIERIS AG

The present invention relates to novel muteins derived from human tear lipocalin. The invention also refers to a corresponding nucleic acid molecule encoding such a mutein and to a method for its generation. The invention further refers to a method for producing such a mutein. Finally, the invention is directed to a pharmaceutical composition comprising such a lipocalin mutein as well as to various uses of the mutein.

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Номер записи: 40
24-01-2013 дата публикации

Heteroaryl Derivatives as CFTR Modulators

Номер: US20130023538A1
Автор: Brian Bear, Jinglan Zhou, Mark Miller, Sara Hadida Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance 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: 41
28-02-2013 дата публикации

Compounds and methods for treatment of hypertension

Номер: US20130053366A1
Автор: Andrew Asher Protter, Michael John Green, Rajendra Parasmal Jain, Sarvajit Chakravarty
Принадлежит: Medivation Technologies LLC

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α 2B antagonists. The compounds may also bind to and antagonize adrenergic receptor α 1B . The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.

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Номер записи: 42
14-03-2013 дата публикации

Use of immunesuppressant receptor

Номер: US20130064818A1
Автор: Hideaki Tada, Kimiho Moroe, Tomoyuki Odani
Принадлежит: Ono Pharmaceutical Co Ltd

The present invention relates to use of an antagonist of BIR1 (B cell immunoglobulin receptor 1) related to the present invention, a method for screening the antagonist, in addition to subtype polypeptides of BIR1, the polynucleotide encoding them and antibodies for the polypeptides. BIR1 functions as an immunosuppressive receptor, and the antagonist of BIR1 has immunopotentive activity, which is able to use for preventing and/or treating a cancer, an immunodeficiency disease or an infectious disease.

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Номер записи: 43
21-03-2013 дата публикации

Process for Making Modulators of Cystic Fibrosis Transmembrane Conductance Regulator

Номер: US20130072522A1
Автор: Adam R. Looker, Bobbianna J. Neubert-Langille, Brian R. Krueger, Dahrika Milfred Yap GUERETTE, Fredrick F. Van Goor, Gregor Zlokarnik, John Demattei, Martin Trudeau, Martyn Curtis Botfield, Michael P. Ryan, Peter Diederik Jan Grootenhuis, Stefanie Roeper
Принадлежит: Vertex Pharmaceuticals Inc

The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

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Номер записи: 44
28-03-2013 дата публикации

Compositions and methods for modulating the wnt signaling pathway

Номер: US20130079328A1
Автор: Dai Cheng, DONG Han, Guobao Zhang, Lichun Shen, Rajender Reddy Leleti, Shifeng Pan, Wenqi Gao
Принадлежит: Individual

The present invention relates to compositions and methods for modulating the Wnt signaling pathway, using compounds having Formula (1) and (3): wherein A, B, Y and Z all represent rings, and R 1 , R 2 , R 3 are as defined herein.

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Номер записи: 45
28-03-2013 дата публикации

Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands

Номер: US20130079373A1
Автор: Bernhard Lesch, Gregor Bahrenberg, Jeewoo Lee, Robert Frank, Thomas Christoph
Принадлежит: GRUENENTHAL GmbH

The invention relates to substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

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Номер записи: 46
04-04-2013 дата публикации

Taste masked pharmaceutical composition

Номер: US20130084332A1
Автор: Annette Grave, Martin Folger, Norbert Poellinger, Randolph Seidler, Stefan Lehner
Принадлежит: BOEHRINGER INGELHEIM VETMEDICA GMBH

This application relates to taste masked multi-layered particles an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and comprising a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

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Номер записи: 47
18-04-2013 дата публикации

Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyriodin-2-yl)benzoic acid and administration thereof

Номер: US20130095181A1
Автор: Christopher Ryan Young, Irina Nikolaevna Kadiyala, Marinus Jacobus Verwijs, Ritu Rohit Kaushik, Rossitza Gueorguieva Alargova
Принадлежит: Vertex Pharmaceuticals Inc

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a diluent, a disintegrant, a surfactant, a binder, a glidant and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Methods for treating a patient in need thereof include administering an oral pharmaceutical formulation of Compound 1 to the patient.

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Номер записи: 48
16-05-2013 дата публикации

Heterocyclic compounds, their preparation and therapeutic application

Номер: US20130123271A1
Автор: Caroline Leriche, David Middlemiss
Принадлежит: Fovea Pharmaceuticals SA

The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder.

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Номер записи: 49
23-05-2013 дата публикации

Compositions and methods for treating symptoms of inflammatory related conditions using a combination of an antihistamine and a stimulant

Номер: US20130131026A1
Автор: Mlchael LEIGHTON
Принадлежит: Individual

The present invention relates to compositions containing stimulant and anti-histamine compounds, to methods for treating symptoms related to inflammation using the combination compounds, and to a method for preparing the compositions.

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Номер записи: 50
06-06-2013 дата публикации

Diuretic and natriuretic polypeptides

Номер: US20130143820A1
Автор: Horng H. Chen, John C. Burnett, Jr., Robert D. Simari, Shuchong Pan
Принадлежит: Mayo Foundation for Medical Education and Research

This document provides diuretic and natriuretic polypeptides. For example, this document provides polypeptides having diuretic and/or natriuretic activities. In some cases, a polypeptide provided herein can have diuretic and natriuretic activities, while lacking the ability to lower blood pressure. This document also provides methods and materials for inducing diuretic and/or natriuretic activities within a mammal.

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Номер записи: 51
06-06-2013 дата публикации

Guanidine compound

Номер: US20130143860A1
Автор: Daisuke Suzuki, Hiroyoshi Yamada, Hisashi Mihara, Kousei Yoshihara, Norio Seki, Susumu Yamaki
Принадлежит: Astellas Pharma Inc

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

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Номер записи: 52
11-07-2013 дата публикации

Mango seed herbal medication

Номер: US20130177597A1
Автор: Diana Cherian, Jolly Cherian, Ninan Cherian
Принадлежит: Individual

An herbal composition for treatment of kidney nephrotic syndrome formed of a mixture of the herbs mango seed powder, Mangifera Indicia ; dandelion, Taraxacum officinale ; fennel seed, Foeniculum Vulgare ; spreading hogweed, Boerhavia diffusa ; and nettle plant, Urtica dioica.

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Номер записи: 53
18-07-2013 дата публикации

Modulations of protease activated receptors

Номер: US20130184226A1
Автор: David Paul Fairlie, Jacky Yung Suen, Ligong Liu, Mei Kwan Yau
Принадлежит: University of Queensland UQ

The present invention provides novel compounds of the Formula (1), pharmaceutical compositions comprising such compounds and methods for using such compounds as tools for biological studies or as agents or drugs for modulating Protease Activated Receptor-2 (PAR2) and for treating a subject at risk of—or susceptible to—a disease or disorder, or having a disease or disorder associated with undesirable PAR2 activity.

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Номер записи: 54
18-07-2013 дата публикации

Parenteral solutions containing metolazone

Номер: US20130184296A1
Автор: John Somberg, Vasant Ranade
Принадлежит: Academic Pharmaceuticals Inc

Disclosed herein are parenteral solutions containing 7-halo-1,2,3,4-tetrahydro-3-aryl-6-quinazoline sulfonamide in N,N-dimethylacetamide, polyethylene glycol and D 5 W useful in the treatment of hypertension, heart failure and renal disease leading to edematous states. Also disclosed are methods for preparing such solutions.

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Номер записи: 55
18-07-2013 дата публикации

Metal coordinated compositions

Номер: US20130184447A1
Автор: Thomas Piccariello
Принадлежит: Synthonics Inc

A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.

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Номер записи: 56
25-07-2013 дата публикации

Compounds and methods for treating diabetes

Номер: US20130190294A1
Автор: Andrew Asher Protter, Michael John Green, Rajendra Parasmal Jain, Sarvajit Chakravarty
Принадлежит: Medivation Technologies LLC

Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor α 2A . The compounds may also bind to and are an antagonist of the adrenergic receptor α 2B ; or the compounds are not antagonists of the adrenergic receptor α 2B and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.

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Номер записи: 57
25-07-2013 дата публикации

Bisaryl-bonded aryltriazolones and use thereof

Номер: US20130190330A1
Автор: Axel Kretschmer, Carsten Schmeck, Chantal FÜRSTNER, Elisabeth Pook, Hubert Trübel, Ingo Pluschkell, Joerg Keldenich, Martina Delbeck, Peter Kolkhof
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel bisaryl-linked 5-aryl-1,2,4-triazolone derivatives, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.

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Номер записи: 58
15-08-2013 дата публикации

Method of treating dyspnea associated with acute heart failure

Номер: US20130210730A1
Автор: Dennis Stewart, Elaine Unemori, Gad Cotter, Martha Jo Whitehouse, Sam L. Teichman
Принадлежит: NOVARTIS AG

The disclosure pertains to methods of reducing decompensation through acute intervention including in subjects afflicted with acute decompensated heart failure. Particularly, the disclosure provides methods for treating acute cardiac decompensation by administering a pharmaceutically effective amount of relaxin.

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Номер записи: 59
22-08-2013 дата публикации

Modified beta-lactamases and methods and uses related thereto

Номер: US20130216622A1
Автор: Katja Valimaki, Pertti Koski, Ulla Airaksinen
Принадлежит: PREVABR LLC

The present invention relates to pharmaceuticals and modified beta-lactamases. Specifically, the invention relates to novel recombinant beta-lactamases and pharmaceutical compositions comprising the beta-lactamases. Also, the present invention relates to methods for modifying a beta-lactamase, producing the beta-lactamase and treating or preventing beta-lactam antibiotic induced adverse effects. Furthermore, the present invention relates to the beta-lactamase for use as a medicament and to the use of the beta-lactamase in the manufacture of a medicament for treating or preventing beta-lactam antibiotics induced adverse effects. Still further, the invention relates to a polynucleotide and a host cell comprising the polynucleotide.

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Номер записи: 60
29-08-2013 дата публикации

Delayed-release formulation for reducing the frequency of urination and method of use thereof

Номер: US20130224291A1
Автор: David A. Dill
Принадлежит: Wellesley Pharmaceuticals LLC

Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.

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Номер записи: 61
29-08-2013 дата публикации

Method for treating a pulmonary hypertension condition without companion diagnosis

Номер: US20130224306A1
Автор: David J. PIZZUTI, Hunter Campbell Gillies, Tobias Peschel
Принадлежит: Gilead Sciences Inc

There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.

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Номер записи: 62
05-09-2013 дата публикации

Substituted phenylacetate and phenylpropane amides and use thereof

Номер: US20130231313A1
Автор: Axel Kretschmer, Carsten Schmeck, Chantal FÜRSTNER, Elisabeth Pook, Hubert Trübel, Joerg Keldenich, Martina Delbeck, Peter Kolkhof
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel substituted phenylacetamides and phenylpropanamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.

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Номер записи: 63
12-09-2013 дата публикации

Materials and methods for delivering compositions to selected tissues

Номер: US20130236518A1
Автор: Lignyun Cheng, Michael J. Sailor, William R. Freeman
Принадлежит: UNIVERSITY OF CALIFORNIA

This invention relates to devices, systems and methods for delivering preprogrammed quantities of an active ingredient to a biological system over time without the need for external power or electronics.

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Номер записи: 64
12-09-2013 дата публикации

Aptamer therapeutics useful in the treatment of complement-related disorders

Номер: US20130237589A1
Автор: Charles Wilson, Claude Benedict, David Epstein, Dilara McCauley, James Rottman, Jeffrey Kurz, Markus Kurz, Thomas Greene McCauley
Принадлежит: ARCHEMIX LLC

The invention provides nucleic acid therapeutics and methods for using these nucleic acid therapeutics in the treatment of complement-related disorders.

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Номер записи: 65
19-09-2013 дата публикации

Formulations and methods for lyophilization and lyophilates provided thereby

Номер: US20130245069A1
Автор: Sven Jacobson
Принадлежит: Remedy Pharmaceuticals Inc

The present invention provides compositions, methods for lyophilizing compounds and making pharmaceutical compositions, and kits providing solutions and lyophilized formulations of compounds. The compositions, methods, and kits are particularly useful in pharmaceutical applications involving therapeutic agents that have low solubility at low pH and medium pH values. Certain embodiments provide methods for lyophilizing compounds in liquid solutions, which include the steps of: a) preparing aqueous solutions of a compound of interest in the absence of buffer; b) adjusting the pH to high values of pH in order to increase the solubility of the compound of interest; and c) freeze-drying the solution to provide a lyophilized solid composition. Aqueous solutions including buffer are also disclosed. Lyophilized formulations, including micronized and non-micronized powders, are provided.

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Номер записи: 66
17-10-2013 дата публикации

Ion binding polymers and uses thereof

Номер: US20130272992A1
Автор: Dominique Charmot, Gerrit Klaerner, Han-Ting Chang, Jerry M. Buysse, Mingjun Liu
Принадлежит: Relypsa Inc

The present invention provides methods and compositions for the treatment of ion imbalances. In particular, the invention provides compositions comprising potassium binding polymers and pharmaceutical compositions thereof. Methods of use of the polymeric and pharmaceutical compositions for therapeutic and/or prophylactic benefits are disclosed herein. Examples of these methods include the treatment of hyperkalemia, such as hyperkalemia caused by renal failure and/or the use of hyperkalemia causing drugs.

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Номер записи: 67
24-10-2013 дата публикации

Novel 6-Amino-Morphinan Derivatives, Method of Manufacturing Them and Their Application as Analgesics

Номер: US20130281698A1
Автор: Johannes Schuetz, Peter Kayatz
Принадлежит: AlcaSynn Pharmaceuticals GmbH

This invention provides novel 6-amino-morphinan derivatives, methods of making same, and methods of using same for analgesic purposes. The derivatives of this invention are represented by the following formula:

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Номер записи: 68
24-10-2013 дата публикации

Compounds for the treatment of metabolic disorders

Номер: US20130281705A1
Автор: Shalini Sharma
Принадлежит: Wellstat Therapeutics Corp

Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

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Номер записи: 69
31-10-2013 дата публикации

Combination therapy for treatment of immune disorders

Номер: US20130287775A1
Автор: Brent S. Mckenzie, Daniel J. Cua, Edward P. Bowman, Kathy L. Miller, Katia Boniface, Kristian S. Bak-Jensen, Melanie A. Kleinschek, Rene De Waal Malefyt, Robert A. Kastelein
Принадлежит: Merck Sharp and Dohme LLC

Methods and compositions are provided for the treatment of immune disorders, such as autoimmune diseases, or cancers, involving combination therapy with agents that inhibit the development or maintenance of Th17 cells. Treatment regimens are provided in which an antagonist of a pro-inflammatory cytokine is administered for a time sufficient to alleviate signs and symptoms of an acute phase flare-up of the autoimmune disease, or cancer, and treatment with an antagonist of IL-23 is continued for a longer time to prevent recurrence of the acute event. Antagonists of PGE2 and CD161 are also disclosed for use in treatment of autoimmune, inflammatory and proliferative disorders.

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Номер записи: 70
07-11-2013 дата публикации

Heterocyclic ring compound

Номер: US20130296276A2
Автор: Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai, Osamu Ujikawa
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.

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Номер записи: 71
14-11-2013 дата публикации

Anti-c epsilon mx antibodies capable of binding to human mige on b lymphocytes

Номер: US20130302314A1
Автор: Alfur F. Hung, Jiun-Bo Chen, Pheidias C. Wu, Tsewen Chang
Принадлежит: Academia Sinica

The invention pertains to the generation and utility of antibodies that can bind effectively to CεmX domain on membrane-bound IgE (mIgE) expressed on the surface of human B lymphocytes. The CεmX domain of 52 amino acid residues, located between the CH4 domain and the C-terminal membrane-anchor peptide on human membrane-bound epsilon chain, had been suggested as an antigenic site for immunological targeting of B cells expressing mIgE. Previous reported monoclonal antibodies, including a20, which bind to RADWPGPP (SEQ ID NO:1) peptide at the C-terminal of CεmX, have now been found to bind poorly to mIgE on human B cells. We have discovered that only monoclonal antibodies specific for certain segments, such as GLAGGSAQSQRAPDRVL (SEQ ID NO:2) and HSGQQQGLPRAAGGSVPHPR (SEQ ID NO:3), of CεmX can bind effectively to mIgE on human B cells and hence have the utility for targeting those B cells for the treatment of diseases mediated by IgE.

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Номер записи: 72
21-11-2013 дата публикации

N-(hetero)aryl, 2-(hetero)aryl-substituted acetamides for use as wnt signaling modulators

Номер: US20130310375A1
Автор: Dai Cheng, DONG Han, Guobao Zhang, Shifeng Pan, Wenqi Gao
Принадлежит: IRM LLC

The present invention relates to compositions and methods for modulating the Wnt signaling pathway.

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Номер записи: 73
28-11-2013 дата публикации

Pyridyl Derivatives as CFTR Modulators

Номер: US20130317020A1
Автор: Brian Bear, Jinglan Zhou, Mark Miller, Peter Grootenhuis, Sara Hadida Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance 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: 74
28-11-2013 дата публикации

Pharmaceutical formulations and use thereof in the prevention of stroke, diabetes and/or congestive heart failure

Номер: US20130317047A1
Автор: Anders Ljunggren, Badrudin Rangoonwala, Bernward Scholkens, Gilles Dagenais, Hertzel Gerstein, Norbert Bender, Salim Yusuf
Принадлежит: Aventis Pharma Deutschland GmbH

The present invention relates to use of an inhibitor of the renin-anglotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).

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Номер записи: 75
28-11-2013 дата публикации

Solid Forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide

Номер: US20130317060A1
Автор: Adriana Costache, Christopher R. Young, Mariusz Krawiec, Martin Trudeau, Patricia Hurter, Patrick R. Connelly, William Rowe, Yuchuan Gong, Yushi Feng
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to solid state forms of N—[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

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Номер записи: 76
19-12-2013 дата публикации

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

Номер: US20130338195A1
Автор: Evelyn G. Corpuz, Ken Chow, Liming Wang, Wenkui K. Fang, Wha-Bin Im
Принадлежит: Allergan Inc

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

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Номер записи: 77
09-01-2014 дата публикации

Crystalline form of benzylbenzene sglt2 inhibitor

Номер: US20140011754A9
Автор: Binhua Lv, Brian Seed, Ge Xu, Jacques Y. Roberge, Mengzhuang Cai, Qian Liu
Принадлежит: Theracos Inc

Provided are crystalline forms of a compound having an inhibitory effect on sodium-dependent glucose cotransporter SGLT2. The invention also provides pharmaceutical compositions, methods of preparing the crystalline compound, and methods of using the crystalline compound, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT or SGLT2 inhibition.

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Номер записи: 78
09-01-2014 дата публикации

1,2-disubstituted heterocyclic compounds

Номер: US20140011808A1
Автор: Amy Ripka, Gideon Shapiro, Richard Chesworth
Принадлежит: Envivo Phamaceuticals Inc

1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.

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Номер записи: 79
23-01-2014 дата публикации

Treatment of bone marrow edema (oedema) with polysulfated polysaccharides

Номер: US20140024614A1
Автор: Peter Ghosh
Принадлежит: PARADIGM HEALTH SCIENCES PTY LTD

A method for the treatment of bone marrow edema in a mammal comprising administering an effective amount of a polysulfated polysaccharide including salts thereof, to a mammal in need of such treatment.

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Номер записи: 80
30-01-2014 дата публикации

A1 adenosine receptor antagonists

Номер: US20140031375A1
Автор: Constance Neely Wilson
Принадлежит: Individual

This invention relates to compounds of formula (I), Wherein R 1 -R 4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.

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Номер записи: 81
20-02-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140051724A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, 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: 82
03-04-2014 дата публикации

Therapeutic dll4 binding proteins

Номер: US20140093521A1
Автор: Chung-Ming Hsieh, Erwin R. Boghaert, Jijie Gu, Jonathan A. Hickson, Lorenzo Benatuil, Maria Harris, Susan Morgan-Lappe, Yingchun Li, Yuliya Kutskova, Zhihong Liu
Принадлежит: AbbVie Inc

Improved DLL4 binding proteins are described, including antibodies, CDR-grafted antibodies, human antibodies, and DLL4 binding fragments thereof, proteins that bind DLL4 with high affinity, and DLL4 binding proteins that neutralize DLL4 activity. The DLL4 binding proteins are useful for treating or preventing cancers and tumors and especially for treating or preventing tumor angiogenesis, and/or other angiogenesis-dependent diseases such as ocular neovascularization, or angiogenesis-independent diseases characterized by aberrant DLL4 expression or activity such as autoimmune disorders including multiple sclerosis.

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Номер записи: 83
03-04-2014 дата публикации

Aquaporin modulators and methods of using them for the treatment of edema and fluid imbalance

Номер: US20140094455A1
Автор: Andrea J. Yool, Elton Rodrigues Migliati, Gary A. Flynn, Leslie S. Ritter
Принадлежит: Arizona Board of Regents of University of Arizona

Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.

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Номер записи: 84
10-04-2014 дата публикации

Il-1 binding proteins

Номер: US20140099671A1
Автор: Chengbin Wu, Chung-Ming Hsieh, Dominic J. Ambrosi, Tariq Ghayur
Принадлежит: AbbVie Inc

Proteins that bind IL-1α and IL-1β are described along with their use in compositions and methods for treating, preventing, and diagnosing IL-1-related disorders and for detecting IL-1α and IL-1β in cells, tissues, samples, and compositions.

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Номер записи: 85
10-04-2014 дата публикации

Guanidine compound

Номер: US20140100210A1
Автор: Daisuke Suzuki, Hiroyoshi Yamada, Hisashi Mihara, Kousei Yoshihara, Norio Seki, Susumu Yamaki
Принадлежит: Astellas Pharma Inc

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

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Номер записи: 86
05-01-2017 дата публикации

Therapeutic composition

Номер: US20170000813A1
Автор: Anne T. Moore, Danielle N. RINGHOFF, Gary Lee FEISS, Linda M. Mahoney
Принадлежит: Dermarc LLC

This invention relates to a topical composition for prevention and treatment of viral infections.

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Номер записи: 87
03-01-2019 дата публикации

Heteroaromatic compounds and their use as dopamine d1 ligands

Номер: US20190002439A1
Автор: Amy Beth Dounay, Bruce Nelsen Rogers, Chewah Lee, David Lawrence Firman Gray, Ivan Viktorovich Efremov, Jaclyn Louise Henderson, Jennifer Elizabeth Davoren, Lei Zhang, Michael Aaron Brodney, Michael Eric GREEN, Scot Richard Mente, Steven Victor O'neil
Принадлежит: PFIZER INC

The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.

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Номер записи: 88
05-01-2017 дата публикации

Modulation of prekallikrein (pkk) expression

Номер: US20170002359A1
Автор: Huynh-Hoa Bui, Susan M. Freier
Принадлежит: Ionis Pharmaceuticals Inc

Disclosed herein are antisense compounds and methods for decreasing PKK mRNA and protein expression. Such methods, compounds, and compositions are useful to treat, prevent, or ameliorate PKK-associated diseases, disorders, and conditions.

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Номер записи: 89
07-01-2021 дата публикации

Substituted Aromatic Compounds and Pharmaceutical Uses Thereof

Номер: US20210002202A1
Автор: BIENVENU Jean-Francois, GAGNON Lyne, GROUIX Brigitte, Penney Christopher, PERRON Valérie, ZACHARIE Boulos
Принадлежит:

The present invention relates to substituted aromatic compounds of Formula I and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention or treatment of (i) blood disorders, (ii) renal disorders, a nephropathies, or renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders. 2. The method of claim 1 , wherein Ris straight chain Calkyl claim 1 , Calkyl claim 1 , or C-Calkenyl; and Ris H claim 1 , halogen claim 1 , haloalkyl claim 1 , or OR.3. The method of claim 1 , wherein Ris independently chosen from: H claim 1 , halogen claim 1 , haloalkyl claim 1 , straight chain C-Calkyl claim 1 , or OR; and Ris independently chosen from: H claim 1 , halogen claim 1 , haloalkyl claim 1 , C-Calkyl claim 1 , or OR.4. The method of claim 1 , wherein Ris OR.5. The method of claim 1 , wherein the pharmaceutically acceptable salt is a base addition salt.6. The method of claim 5 , wherein the base addition salt is a metal counterion.7. The method of claim 6 , wherein the metal counterion is sodium claim 6 , magnesium claim 6 , calcium claim 6 , potassium or lithium.8. The method of claim 7 , wherein the metal counterion is sodium.11. The method of claim 1 , wherein the inflammatory-related disease is an immune mediated inflammatory disease or an autoimmune disease.12. The method of claim 1 , wherein the inflammatory-related disease is an autoimmune disease.13. The method of claim 1 , wherein the inflammatory-related disease is selected from the group consisting of arthritis claim 1 , systemic lupus erythematosus (SLE) claim 1 , ITP claim 1 , glomerulonephritis claim 1 , vasculitis claim 1 , psoriatic arthritis claim 1 , psoriasis claim 1 , Crohn's disease claim 1 , inflammatory bowel disease claim 1 , ankylosing spondylitis claim 1 , Sjögren's syndrome claim 1 , Still's disease ...

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Номер записи: 90
01-01-2015 дата публикации

Benzazole Derivatives as Histamine H4 Receptor Ligands

Номер: US20150004181A1
Автор: Denis Danvy, Isabelle Berrebi-Bertrand, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Marc Capet, Nicolas Levoin, Olivier Labeeuw, Philippe Robert, Stéphane Krief, Thierry Calmels, Xavier Billot, Xavier Ligneau
Принадлежит: Bioprojet SC

The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.

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Номер записи: 91
14-01-2016 дата публикации

Apoe peptide dimers and uses thereof

Номер: US20160008424A1
Автор: Dale J. Christensen, Michael P. Vitek
Принадлежит: Cognosci Inc

The present invention provides novel pharmaceutical compositions comprising ApoE-derived peptide dimers. In particular, the ApoE peptide dimers of the invention comprise at least two ApoE mimetic domains and can comprise one or more protein transduction domains. Methods of treating various conditions, such as cancer, inflammatory conditions, and neurodegenerative diseases, by administering the pharmaceutical compositions of the invention are also disclosed.

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Номер записи: 92
08-01-2015 дата публикации

Pharmaceuticals and methods for treating hypoxia and screening methods therefor

Номер: US20150010576A1
Автор: Mircea Ivan, William G. Kaelin, Jr.
Принадлежит: Dana Farber Cancer Institute Inc

Light-generating fusion proteins having a ligand binding site and a light-generating polypeptide moiety and their use as diagnostics, in drug screening and discovery, and as therapeutics, are disclosed. The light-generating fusion protein has a feature where the bioluminescence of the polypeptide moiety changes upon binding of a ligand at the ligand binding site. The ligand may be, for example, an enzyme present in an environment only under certain conditions, e.g., ubiquitin ligase in a hypoxic state, such that the light-generating fusion protein is “turned on” only under such conditions.

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Номер записи: 93
14-01-2016 дата публикации

Crystalline forms of (r)-8-chloro-1-methyl- 2,3,4,5-tetrahydro-1h-3-benzazepine hydrochloride

Номер: US20160009654A1
Автор: James A. Henshilwood, Noah Post, Rajesh Kumar Agarwal, William L. Betts, III, Yuan-Hon Kiang
Принадлежит: Arena Pharmaceuticals Inc

The present invention is directed to crystalline forms of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, compositions containing the same and uses thereof.

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Номер записи: 94
14-01-2016 дата публикации

Tricyclic compound and use thereof

Номер: US20160009677A1
Автор: Jae-Sun Kim, Jaeseung AHN, Je Ho Ryu, Jeong A Lee, Joon Ho Sa, Ju Young Lee, Min-Young Han, Taekyung Yoo
Принадлежит: SK Chemicals Co Ltd

The present invention relates to: a compound selected from the group consisting of a tricyclic compound having the structure of formula I, a pharmaceutically acceptable salt, an isomer, a solvate and a precursor thereof; and a use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases.

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Номер записи: 95
14-01-2021 дата публикации

Diaminopyrimidines as p2x3 and p2x2/3 antagonists

Номер: US20210009531A1
Автор: Alam Jahangir, Chris Allen Broka, Clara Jeou Jen Lin, Daniel Warren Parish, David Scott Carter, Michael Patrick Dillon, Ronald Charles Hawley
Принадлежит: Roche Palo Alto LLC

or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.

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Номер записи: 96
14-01-2021 дата публикации

ANTI-VEGFR-2 ANTIBODY

Номер: US20210009695A1
Автор: LEE Seon-Young, Lee Weon-Sup, Yoo Jin-San
Принадлежит: PharmAbcine Inc.

The present invention relates to a pharmaceutical composition comprising an anti-VEGFR-2 antibody. The pharmaceutical composition of the present invention can treat, prevent, or alleviate cerebral edema. For patients who are administered a steroid agent to treat, prevent, or alleviate cerebral edema, the pharmaceutical composition of the present invention also allows a reduction in the administration dosage and/or duration of administration the steroid agent. In addition, the pharmaceutical composition of the present invention can significantly prolong a survival time of a patient suffering from cerebral edema or glioblastoma. 115-. (canceled)16. A method for treating , preventing , or alleviating cerebral edema , comprising:administering a pharmaceutical composition to a subject in need thereof,wherein the pharmaceutical composition comprises an anti-VEGFR-2 antibody that specifically binds to VEGFR-2 to neutralize an activity of VEGFR-2.17. The method according to claim 16 , wherein the anti-VEGFR-2 antibody comprises:a light chain variable region comprising light chain CDR1 of SEQ ID NO: 1, light chain CDR2 of SEQ ID NO: 2, and light chain CDR3 of SEQ ID NO: 3; anda heavy chain variable region comprising heavy chain CDR1 of SEQ ID NO: 4, heavy chain CDR2 of SEQ ID NO: 5, and heavy chain CDR3 of SEQ ID NO: 6.18. The method according to claim 16 , wherein the anti-VEGFR-2 antibody comprises:a light chain variable region of SEQ ID NO: 7; anda heavy chain variable region of SEQ ID NO: 8.19. The method according to claim 16 , wherein the anti-VEGFR-2 antibody is a TTAC-0001 antibody or an antibody specifically binding to the same epitope as an epitope bound by the TTAC-0001 antibody.20. The method according to claim 16 , wherein the cerebral edema is a glioblastoma surrounding edema.21. The method according to claim 16 , wherein the pharmaceutical composition further comprises one or more selected from the group consisting of osmotic agents claim 16 , diuretics claim ...

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Номер записи: 97
03-02-2022 дата публикации

Substituted cycloalkanes for managing nephrogenic diabetes insipidus

Номер: US20220031639A1
Автор: Ish Khanna, Janet Klein, Jeff Sands, Sivaram Pillarisetti
Принадлежит: Nephrodi Therapeutics Inc

In certain embodiments, this disclosure relates to methods of treating or preventing nephrogenic diabetes insipidus comprising administering an effective amount of a compound of Formula I or derivatives thereof, as described herein, to a subject in need thereof. In certain embodiments, the subject has been diagnosed with nephrogenic diabetes insipidus.

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Номер записи: 98
15-01-2015 дата публикации

Conditioned medium obtained from placental mesenchymal stem cells and use thereof in the therapeutic treatment of preeclampsia

Номер: US20150017122A1
Автор: Alessandro Rolfo, Tullia Todros
Принадлежит: CORION BIOTECH Srl

It is described a conditioned medium (CM) obtainable by culturing, in a liquid culture medium, placental mesenchymal stem cells isolated from the placental tissue of pregnant women not affected by preeclampsia. The conditioned medium of the invention includes at least IL-6, IL-10 and MCP-1 proteins and it is effective for the therapeutic treatment of preeclampsia.

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Номер записи: 99
21-01-2016 дата публикации

Neprilysin inhibitors

Номер: US20160016918A1
Автор: Adam D. Hughes, Melissa Fleury, Roland Gendron
Принадлежит: Theravance Biopharma R&D Ip Llc

In one aspect, the invention relates to compounds having the formula: where R 1 -R 6 , a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

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Номер записи: 100