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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 123042. Отображено 100.
05-01-2012 дата публикации

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

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

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

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Номер записи: 1
05-01-2012 дата публикации

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

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

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

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Номер записи: 2
05-01-2012 дата публикации

NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE

Номер: US20120004213A1
Автор: Alexander Bischoff, Ganesh Prabhu, Hosahalli Subramanya, Kumar Sundaresan, Sandeep N. Raikar, Srinivasa Raju Sammeta
Принадлежит: Forest Laboratories Holdings Ltd

The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.

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Номер записи: 3
05-01-2012 дата публикации

Method of treatment or prophylaxis

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

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

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Номер записи: 4
05-01-2012 дата публикации

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

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

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

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Номер записи: 5
19-01-2012 дата публикации

Compounds for the prevention and treatment of cardiovascular diseases

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

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

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Номер записи: 6
19-01-2012 дата публикации

Taspase1 inhibitors and their uses

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

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

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Номер записи: 7
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).

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Номер записи: 8
26-01-2012 дата публикации

Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System

Номер: US20120020915A1
Автор: Ajay Gupta, Hyman M. Schipper, Jason Z. Vlahakis, Kanji Nakatsu, Moulay Alaoui-Jamali, Walter A. Szarek
Принадлежит: OSTA BIOTECHNOLOGIES Inc, Queens University at Kingston, Sir Mortimer B Davis Jewish General Hospita

Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumour tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.

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Номер записи: 9
26-01-2012 дата публикации

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

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

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

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Номер записи: 10
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: 11
26-01-2012 дата публикации

Fluorine-containing n-alkylsulfonylimide compound, manufacturing method therefor, and method of manufacturing an ionic compound

Номер: US20120022269A1
Автор: Daisuke Takano, Hiroyuki Yatsuyanagi, Takashi Konishi, Tsunetoshi Honda
Принадлежит: Mitsubishi Materials Corp, Mitsubishi Materials Electronic Chemicals Co Ltd

According to the method for producing fluorine-containing N-alkylsulfonylimide compound, the fluorine-containing N-alkylsulfonylimide compound can be produced safely with a high recovery rate by alkylating fluorine-containing sulfonylimide acid or fluorine-containing sulfonylimide acid salt with dialkylsulfuric acid or dialkylcarbonic acid.

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Номер записи: 12
02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1
Автор: David Butler, Jayaprakash K. Narayanannair, Kallanthottathil G. Rajeev, Laxmab Eltepu, Muthiah Manoharan, Muthusamy Jayaraman
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

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Номер записи: 13
02-02-2012 дата публикации

Pyrazole compounds as crth2 antagonists

Номер: US20120028938A1
Автор: Christoph Hoenke, Dieter Wolfgang Hamprecht, Domnic Martyres, Peter Seither, Ralf Anderskewitz, Thorsten Oost, Wolfgang Rist
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to pyrazole compounds of formula (I) and pharmaceutically acceptable salts thereof having CRTH2-activity, wherein W, L 1 , L 2 , X, L 3 , Y, R 1 and R 2 are as defined in the specification and claims, to their use as medicaments and to pharmaceutical formulations, containing said compounds or containing a combination of said compounds with one or more active substances.

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Номер записи: 14
02-02-2012 дата публикации

Synthesis of enone intermediate

Номер: US20120029199A1
Автор: Andrew G. Myers, Jason D. Brubaker
Принадлежит: Harvard College

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

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Номер записи: 15
02-02-2012 дата публикации

Synthesis of substituted-3-aminopyrazoles

Номер: US20120029204A1
Автор: Carmen S. Alvarez, Cory Seth Poker, Kamil Paruch, Kartik M. Keertikar, Marc A. Labroli, Michael P. Dwyer, Timothy J. Guzi
Принадлежит: Schering Corp

The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1′H-4,4′-bispyrazole.

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Номер записи: 16
09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Автор: Johan D. Oslob, Kenneth Barr, Min Zhong, Wang Shen
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

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Номер записи: 17
09-02-2012 дата публикации

Compounds, Compositions, and Methods for the Treatment of Beta-Amyloid Diseases and Synucleinopathies

Номер: US20120035230A1
Автор: Alan D. Snow, F. Michael Hudson, Joel Cummings, Luke A. Esposito, Manfred Weigele, Thomas Lake
Принадлежит: ProteoTech Inc

Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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Номер записи: 18
09-02-2012 дата публикации

Volatile Imidazoles and Group 2 Imidazole Based Metal Precursors

Номер: US20120035351A1
Автор: John Anthony Thomas Norman, Melanie K. Perez, Moo-Sung Kim
Принадлежит: Air Products and Chemicals Inc

Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated

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Номер записи: 19
16-02-2012 дата публикации

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

Номер: US20120041027A1
Автор: David Gwyn Cooper, Graham Walker, Ian Thomson Forbes, Jian Jin, Paul Adrian Wyman, Vincenzo Garzya, Yann Louchart
Принадлежит: Glaxo Group Ltd

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

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Номер записи: 20
23-02-2012 дата публикации

Diacylethylenediamine compound

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

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

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Номер записи: 21
01-03-2012 дата публикации

Nitrogen-containing organic compound, chemically amplified positive resist composition, and patterning process

Номер: US20120052441A1
Автор: Masayoshi Sagehashi, Takeru Watanabe, Tomohiro Kobayashi
Принадлежит: Shin Etsu Chemical Co Ltd

An aralkylcarbamate of imidazole base is effective as the quencher. In a chemically amplified positive resist composition comprising the carbamate, deprotection reaction of carbamate takes place by reacting with the acid generated upon exposure to high-energy radiation, whereby the composition changes its basicity before and after exposure, resulting in a pattern profile with advantages including high resolution, rectangular shape, and minimized dark-bright difference.

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Номер записи: 22
01-03-2012 дата публикации

Compounds, pharmaceutical compositions and methods of use of hydroxamic acid derivatives

Номер: US20120053188A1
Автор: Stephen Gately, Tong Wang
Принадлежит: Translational Genomics Research Institute TGen

The invention encompasses a compound derived from hydroxamic acid that may be used to slow the expansion of cancer cells and thus is effective in the treatment of cancer. Generally, the disclosed compound includes a benzimidazole group coupled to a hydroxyamide of five or more unsubstituted carbon atoms and any pharmaceutically acceptable salts, solvates and chemically protected forms thereof. Also disclosed are pharmacological compositions including the compound and methods of using the compound to slow the expansion of cancer cells as well as methods of using the compound to treat cancer.

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Номер записи: 23
08-03-2012 дата публикации

Prophylactic or therapeutic agent for pulmonary fibrosis

Номер: US20120059020A1
Автор: Kentaro Ueda, Makoto Akashima, Masamichi Takagi, Noboru Hattori
Принадлежит: Shizuoka Coffein Co Ltd

Disclosed is a compound which has an inhibitory activity on plasminogen activator inhibitor-1 (PAI-1) and has a propanedioic acid structure represented by formula (1) [wherein R 1 and R 2 independently represent a hydrogen atom or a linear or branched alkyl group having 1 to 4 carbon atoms; R 3 represents a cyclohexyl group or a phenyl group (provide that the phenyl group may be substituted by a substituent selected from a linear or branched alkyl group having 1 to 4 carbon atoms, a linear or branched alkoxy group having 1 to 4 carbon atoms, and a halogen atom); R 4 represents a linear or branched alkyl group having 1 to 6 carbon atoms or a phenyl group (provide that the phenyl group may be substituted by a substituent selected from a linear or branched alkyl group having 1 to 4 carbon atoms, a linear or branched alkoxy group having 1 to 4 carbon atoms, and a halogen atom); and n represents an integer of 1 to 8]. The compound is useful as a prophylactic or therapeutic agent for pulmonary fibrosis.

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Номер записи: 24
22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Автор: Akihiro Morinaka, Ken Chikauchi, Mizuyo Ida, Takao Abe, Toshiaki Kudo, Yukiko Hiraiwa
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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Номер записи: 25
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.

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Номер записи: 26
22-03-2012 дата публикации

Aminopyrimidinamides As Pest Control Agents

Номер: US20120071496A1
Автор: Angela Becker, Arnd Voerste, Eiichi Shimojo, Eva-Maria Franken, Graham Holmwood, Johannes-Rudolf Jansen, Katsuhiko Shibuya, Markus Heil, Masashi Ataka, Mazen Es-Sayed, Otto Schallner, Peter Lümmen, Sachio Kudo, Silvia Cerezo-Galvez, Simon MAECHLING, Takashi Hashihayata, Teruyuki Ichihara, Ulrich Ebbinghaus-Kintscher, Ulrich Görgens
Принадлежит: Bayer CropScience AG

The present application relates to novel aminopyrimidinamides, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.

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Номер записи: 27
22-03-2012 дата публикации

Compositions and Their Use as Anti-Tumor Agents

Номер: US20120071513A1
Автор: Charles Vacin, David Kanne, Diva Chan, Donald R. James, Gary Look, John Schullek, John Ward, Richard Gless, Tina Lee, X. Michael Wang
Принадлежит: COMPASS PHARMACEUTICALS LLC

The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.

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Номер записи: 28
22-03-2012 дата публикации

Novel solid forms of bendamustine hydrochloride

Номер: US20120071532A1
Автор: Laurent D. Courvoisier, Mark Eddleston, Martin Ian Cooper, Robert E. Mckean
Принадлежит: Cephalon Inc

Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.

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Номер записи: 29
22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
Автор: Andiliy G. Lai, Celine Bonnefous, Jackaline D. Julien, Johnny Y. Nagasawa, Mehmet Kahraman, Nicholas D. Smith, Steven P. Govek
Принадлежит: Aragon Pharmaceuticals Inc

Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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Номер записи: 30
05-04-2012 дата публикации

Ionic liquids, the method for preparing the same and method for removing acetylenes from olefin mixtures using the ionic liquids

Номер: US20120083642A1
Автор: Byoung Sung Ahn, Gyeong Taek Gong, Hoon Sik Kim, Hyun Joo Lee, Jin-Hyung Kim
Принадлежит: Korea Advanced Institute of Science and Technology KAIST

There are provided an ionic liquid having ether group(s) in which a copper(I) compound is included, a method for preparing the same, and a method for removing traces amounts of acetylene-based hydrocarbon compounds included in olefin by absorption or extraction using the same. When the disclosed solution is used, oxidation of Cu(I) to Cu(II) is prevented since CuX is stabilized by the ionic liquid. Thus, selective removal efficiency of acetylenic compounds is improved greatly while the removal performance is retained for a long period of time. Further, since the solution according to the present disclosure is applicable as an extractant as well as an absorbent, the associated operation is simple and apparatus cost can be decreased.

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Номер записи: 31
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: 32
12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Автор: Cullen L. Cavallaro, Gregory S. Bisacchi, James R. Corte, Joanne M. Smallheer, Jon J. Hangeland, Karen A. Rossi, Mimi L. Quan, Todd J. Friends, Zhong Sun
Принадлежит: Bristol Myers Squibb Co

The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R 3 , R 4 , R 6 , R 11 , X 1 , X 2 , and X 3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.

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Номер записи: 33
12-04-2012 дата публикации

Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors

Номер: US20120088768A1
Автор: Dane Goff, Pingyu Ding, Rajinder Singh, Sacha Holland
Принадлежит: Rigel Pharmaceuticals Inc

Pinane-substituted pyrimidinediamine derivatives and pharmaceutical compositions containing the derivatives are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the derivatives in treating diseases or conditions associated with Axl catalytic activity are also disclosed.

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Номер записи: 34
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.

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Номер записи: 35
19-04-2012 дата публикации

Ionic liquid solvents of perhalide type for metals and metal compounds

Номер: US20120090430A1
Автор: John Holbrey, Robin Don Rogers
Принадлежит: Individual

The present invention relates to a process for dissolving metals in perhalide containing ionic liquids, and to the extraction of metals from mineral ores; the remediation of materials contaminated with heavy, toxic or radioactive metals; and to the removal of heavy and toxic metals from hydrocarbon streams.

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Номер записи: 36
19-04-2012 дата публикации

Organic Compounds Having Cooling Properties

Номер: US20120095042A1
Автор: Stefan Michael Furrer
Принадлежит: Givaudan SA

Provided are compounds of formula (I) wherein m is 0, 1 or 2; R I is a mono- or bicyclic heterocyclic ring system including one, two or three heteroatoms selected from nitrogen, sulphur and oxygen; R 2 is selected from hydrogen, methyl and ethyl; I) R 3 is hydrogen, methyl, or ethyl; and R 4 and R 5 are independently selected from ethyl and isopropyl; and R 3 , R 4 and R 5 together have at least 6 carbon atoms: or II) any two or all of R 3 , R 4 and R 5 form together with the carbon atom to which they are attached 3-para-menthyl, bornyl, or adamantyl; having cooling properties, their use as cooling agent and compositions including them.

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Номер записи: 37
19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1
Автор: David Butler, Kallanthottathil G. Rajeev, Laxman Eltepu, Muthiah Manoharan, Muthusamy Jayaraman, Narayanannair K. Jayaprakash
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

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Номер записи: 38
26-04-2012 дата публикации

Compositions and articles comprising polymerizable ionic liquid mixture, and methods of curing

Номер: US20120101184A1
Автор: Brian N. Holmes, Joel D. Oxman, Joseph D. Rule, Kevin M. Lewandowski, Larry R. Krepski, Peiwang Zhu, Richard L. Severance, Thomas P. Klun, Yizhong Wang
Принадлежит: 3M Innovative Properties Co

Presently described are curable compositions comprising a mixture of at least one (e.g. free-radically) polymerizable ionic liquid and at least one other ethylenically unsaturated monomer, oligomer, or polymer. The polymerizable ionic liquid is characterized as having an air to nitrogen curing exotherm ratio of at least 0.70. Also described are articles and methods of making articles from such curable compositions. A monofunctional polymerizable ionic liquid is also described comprising a non-polymerizable substituted imidazolium cationic group and a polymerizable sulfonate anion.

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Номер записи: 39
03-05-2012 дата публикации

Compound for an organic photoelectric device and organic photoelectric device including the same

Номер: US20120104941A1
Автор: Dong-Min Kang, Ho-Kuk Jung, Mi-Young Chae, Myeong-Soon Kang, Nam-Heon Lee, Nam-Soo Kim, Sung-Hyun Jung
Принадлежит: Cheil Industries Inc

A compound for an organic photoelectric device, an organic photoelectric device, and a display device, the compound being represented by the following Chemical Formula 3a, 3b, or 3c:

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Номер записи: 40
10-05-2012 дата публикации

Material for organic electroluminescence device and organic electroluminescence device using the same

Номер: US20120112629A1
Автор: Chishio Hosokawa, Kazuki Nishimura, Masaki Numata, Tomoki Kato, Toshihiro Iwakuma
Принадлежит: Idemitsu Kosan Co Ltd

Provided are an organic electroluminescence device, which: shows high luminous efficiency; is free of any pixel defect; and has a long lifetime, and a material for an organic electroluminescence device for realizing the device. The material for an organic electroluminescence device is a compound of a specific structure having a π-conjugated heteroacene skeleton crosslinked with a carbon atom, nitrogen atom, or oxygen atom. The organic electroluminescence device has one or more organic thin film layers including a light emitting layer between a cathode and an anode, and at least one layer of the organic thin film layers contains the material for an organic electroluminescence device.

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Номер записи: 41
10-05-2012 дата публикации

Compositions and methods for inhibiting viral and/or bacterial infections

Номер: US20120114639A1
Автор: Michelle Adair Ozbun, Zurab Surviladze
Принадлежит: STC UNM

We describe herein compositions and methods related to inferring with microbial infection. Generally, the compositions include an infection antagonist that inhibits formation of a heparin sulfonated proteoglycan (HSPG)-containing infection complex. Generally, the methods include administering to a subject an amount of a composition as described herein effective to inhibit infection by a microorganism that that infects a host through interactions that involve HSPG.

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Номер записи: 42
10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Автор: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

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Номер записи: 43
10-05-2012 дата публикации

Compounds having antiparasitic or anti-infectious activity

Номер: US20120115904A1
Автор: Aaron Nilsen, Andrii MONASTYRSKYI, David J. Hinrichs, David L. Flanigan, Dennis Kyle, Jane X. Kelly, Jeremy Burrows, Martin J. Smilkstein, Michael K. Riscoe, Richard M. Cross, Rolf W. Winter, Roman Manetsch
Принадлежит: MMV MEDICINES FOR MALARIA VENTURE, Oregon Health Science University, UNIVERSITY OF SOUTH FLORIDA, US Department of Veterans Affairs VA

Compounds of formula I: or formula II: or a pharmaceutically acceptable salt of formula I or formula II, wherein: R 1 is H, hydroxyl, alkoxy, acyl, alkyl, cycloalkyl, aryl, or heteroaryl; R 2 is methyl or haloalkyl; R 4 is hydroxyl, carbonyloxy, or carbonyldioxy; and R 3 is aliphatic, aryl, aralkyl, or alkylaryl; and R 5 , R 6 , R 7 and R 8 are each individually H, halogen, alkoxy, alkyl, haloalkyl, aryl, nitro, cyano, amino, amido, acyl, carboxyl, substituted carboxyl, or —SO 2 R 10 , wherein R 10 is H, alkyl, amino or haloalkyl; provided that in formula I, R 5 and R are not both H or R 6 is not H or methoxy; and in formula II that if R 4 is carbonyldioxy then R 7 is not methoxy.

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Номер записи: 44
10-05-2012 дата публикации

N,n'-diarylurea compounds and n,n'-diarylthiourea compounds as inhibitors of translation initiation

Номер: US20120115915A1
Автор: Bertal Huseyin Aktas, Jose A. Halperin, Michael Chorev
Принадлежит: Harvard College

Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.

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Номер записи: 45
10-05-2012 дата публикации

Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid

Номер: US20120115920A1
Автор: Paul R. Fatheree, Venkat R. Thalladi
Принадлежит: Theravance Inc

The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

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Номер записи: 46
17-05-2012 дата публикации

Compounds, Compositions and Methods for Modulating Uric Acid Levels

Номер: US20120122780A1
Автор: Jean-Luc Girardet, Martha De La Rosa
Принадлежит: Ardea Biociences Inc

Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

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Номер записи: 47
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: 48
17-05-2012 дата публикации

New salts

Номер: US20120122883A1
Автор: Jaroslaw Mazurek, Mihaela Pop
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to new crystalline salt forms of flibanserine which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.

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Номер записи: 49
17-05-2012 дата публикации

No-Carrier-Added Nucleophilic [F-18] Fluorination of Aromatic Compounds

Номер: US20120123120A1
Автор: Jorge R. Barrio, Nagichettiar Satyamurthy
Принадлежит: UNIVERSITY OF CALIFORNIA

Phenyliodonium ylide derivatives substituted with electron donating as well as electron withdrawing groups on the aromatic ring are shown for use as precursors in aromatic nucleophilic substitution reactions. The iodonium ylide group is substituted by nucleophiles such as halide ions to provide the corresponding haloaryl derivatives. No-carrier-added [F-18]fluoride ion exclusively substitutes the iodonium ylide moiety in these derivatives and provides high specific activity F-18 labeled fluoro derivatives. Protected L-dopa-6-iodonium ylide derivative have been synthesized as a precursors for the preparation of no-carrier-added 6-[F-18]fluoro-L-dopa. The iodonium ylide group in this L-dopa.derivative is nucleophilically substituted by no-carrier-added [F-18]fluoride ion to provide a [F-18]fluoro intermediates which upon acid hydrolysis yielded 6-[F-18]fluoro-L-dopa.

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Номер записи: 50
17-05-2012 дата публикации

Process for the preparation of strontium ranelate

Номер: US20120123131A1
Автор: Kapil Ramesh Hire, Koilpillai Joseph Prabahar, Prashant Bhaskarrao Patil, Pravin Bhalchandra Kulkarni
Принадлежит: Individual

The present invention relates to an improved process for the synthesis of strontium ranelate or hydrates thereof. More particularly, the present invention relates to an effective process for the preparation of a compound of formula III, which is a useful intermediate in the synthesis of strontium ranelate. wherein R 1 and R 2 represents substituted or unsubstituted linear or branched C 1 -C 6 alkyl group or C 3 -C 12 cyclic group.

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Номер записи: 51
24-05-2012 дата публикации

Materials for organic electroluminescent devices

Номер: US20120126179A1
Автор: Amir Hossain Parham, Esther Breuning, Susanne Heun
Принадлежит: Merck Patent GmBH

The present invention relates to 4,4′-substituted spirobifluorenes which are suitable, owing to excellent properties, as functional materials in organic electroluminescent devices. In addition, the present invention relates to a process for the preparation of 4,4′-substituted spirobifluorenes and to the use of these compounds in organic electroluminescent devices.

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Номер записи: 52
24-05-2012 дата публикации

Lipid compositions

Номер: US20120128760A1
Автор: David Butler, Kallanthottathil G. Rajeev, Michael E. Jung, Muthiah Manoharan, Muthusamy Jayaraman
Принадлежит: Alnylam Pharmaceuticals Inc

Disclosed herein are lipid compositions comprising a cationic lipid of formula (I), a neutral lipid, a sterol and a PEG or PEG-modified lipid, wherein formula (I) is (F). Also disclosed are methods of producing the cationic lipid of formula (I).

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Номер записи: 53
24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Автор: Chandravadan R. Shah, Dale A. Rudolph, Devin M. Swanson, Jill A. Jablonowski, Victoria D. Wong, Wenying Chai
Принадлежит: Janssen Pharmaceutica NV

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

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Номер записи: 54
24-05-2012 дата публикации

Triterpenoid derivatives useful as antiproliferative agents

Номер: US20120129901A1
Автор: Jorge Antonio Ribeiro Salvador, Marta Cascante Serratosa, Rita Catarina Mendes Dos Santos
Принадлежит: Individual

Formula (I) and (II). The present invention relates to the use of a new lupane derivative of general formula (I) or (II), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, for preventing and/or inhibiting tumor growth and for treating cancer and other proliferative diseases, more particularly for treating leukemia, liver, cervical, colon and prostate cancer. The present invention also relates to the synthesis of these compounds and to pharmaceutical compositions which contain them.

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Номер записи: 55
24-05-2012 дата публикации

Histidinol dehydrogenase inhibitors, and use thereof as medicaments

Номер: US20120129907A1
Автор: Jean-Louis Montero, Jean-Yves Winum, Stephan Kohler
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS

Compounds of general formula (I) below: are characterized in that A represents in particular a C 5 -C 10 heterocyclic group, Y represents in particular a single bond, and B represents in particular an aryl or heteroaryl group.

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Номер записи: 56
24-05-2012 дата публикации

Inhibitors of syk and jak protein kinases

Номер: US20120130073A1
Автор: Anjali Pandey, Brian Kane, Chandrasekar Venkataramani, Jack W. Rose, Mukund Mehrotra, Qing Xu, Shawn M. Bauer, Wolin Huang, Yonghong Song, Zhaozhong Jia
Принадлежит: Portola Pharmaceuticals LLC

The present invention is directed to compounds of formula I-V and tautomers thereof or pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.

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Номер записи: 57
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.

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Номер записи: 58
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.

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Номер записи: 59
31-05-2012 дата публикации

Fungicidal diphenyl-substituted pyridazines

Номер: US20120135995A1
Автор: Paula Louise Sharpe
Принадлежит: EI Du Pont de Nemours and Co

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein R 1 , R 2 , R 3 , R 4a , R 4b , R 5 , W, m and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

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Номер записи: 60
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.

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Номер записи: 61
07-06-2012 дата публикации

Integrin-linked kinase inhibitors

Номер: US20120142702A1
Автор: Ching-Shih Chen, Samuel K. Kulp, Su-Lin Lee
Принадлежит: Ohio State University Research Foundation

A number of compounds and use of the compounds in a method for treating or preventing cancer in a subject by administering to the subject a pharmaceutical composition including a compound of formula I or a pharmaceutically acceptable salt thereof are described. The compounds can also be used to inhibit integrin-linked kinase in a cell, which has an effect on the Akt signaling pathway.

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Номер записи: 62
07-06-2012 дата публикации

Method for production of n-(2-amino-1,2-dicyanovinyl)imidates, method for production of n-(2-amino-1,2-dicyanovinyl)formamidine, and method for production of aminoimidazole derivatives

Номер: US20120142957A1
Автор: Fuminori Komatsu, Mitsuru Takase
Принадлежит: Nippon Soda Co Ltd

A method for producing N-(2-amino-1,2-dicyanovinyl)formamidine, including the steps of reacting an N-(2-amino-1,2-dicyanovinyl)formimidate and ammonia by adding aqueous ammonia to a solution or suspension of an N-(2-amino-1,2-dicyanovinyl)formimidate in ether, or alternatively directly adding an N-(2-amino-1,2-dicyanovinyl)formimidate or adding a solution or suspension of an N-(2-amino-1,2-dicyanovinyl)formimidate in ether to a liquid containing ether and aqueous ammonia.

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Номер записи: 63
14-06-2012 дата публикации

Heterocyclic Radical or Diradical, The Dimers, Oligomers, Polymers, Dispiro Compounds and Polycycles Thereof, the Use Thereof, Organic Semiconductive Material and Electronic or Optoelectronic Component

Номер: US20120146012A1
Автор: Ansgar Werner, Horst Hartmann, Martin Amman, Michael Limmert, Olaf Zeika
Принадлежит: NOVALED GMBH

The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof, to organic semiconductive materials and to electronic and optoelectronic components.

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Номер записи: 64
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.

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Номер записи: 65
21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Автор: Haiqing Yuan, John E. Donello, Michael E. Garst, Richard I. Beard, Veena Viswanath, Xiaoxia Liu
Принадлежит: Allergan Inc

The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

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Номер записи: 66
28-06-2012 дата публикации

Glucagon Receptor Modulators

Номер: US20120165343A1
Автор: Angel Guzman-Perez, Benjamin Dawson STEVENS, Gary Erik Aspnes, Jeffrey Allen Pfefferkorn, Kevin James Filipski, Mary Theresa Didiuk, Meihua Mike Tu
Принадлежит: PFIZER INC

The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R 1 , R 2 , R 3 , A 1 , A 2 , A 3 , A 4 , L, B 1 , B 2 , B 3 and B 4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.

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Номер записи: 67
28-06-2012 дата публикации

Compounds and their use as BACE Inhibitors

Номер: US20120165347A1
Автор: Annika Kers, Britt-Marie Swahn, Fernando Sehgelmeble, Gabor Csjernyik, Karin Kolmodin, Lars Sandberg, Laszlo Rakos, Liselotte Ohberg, Martin Nylof, Peter Soderman, Sofia Karlstrom, Stefan Von Berg
Принадлежит: AstraZeneca AB

The present invention relates to compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.

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Номер записи: 68
05-07-2012 дата публикации

Hsp90 inhibitors

Номер: US20120172321A1
Автор: Erick Co, Huong-Thu Ton-Nu, Jeffrey A. Stafford, John D. Lawson, Prasuna Guntupalli, Wolfgang Reinhard Ludwig Notz, Young K. Chen
Принадлежит: Takeda Pharmaceutical Co Ltd

The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

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Номер записи: 69
05-07-2012 дата публикации

Co-crystals of tramadol and coxibs

Номер: US20120172398A1
Автор: Carlos Ramon Plata Salaman, Nicolas Tesson
Принадлежит: Laboratorios del Dr Esteve SA

The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses in pharmaceutical formulations for the treatment of pain.

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Номер записи: 70
12-07-2012 дата публикации

Pyrimidine derivatives and analogs, preparation method and use thereof

Номер: US20120178915A1
Автор: Lifeng Xu
Принадлежит: Individual

This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X 1 , X 2 , X 3 , X 4 are, independently at each occurrence, C, O, S, Se, N and P elements; R 1 , R 2 , R 3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.

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Номер записи: 71
19-07-2012 дата публикации

Novel n-halamine acrylamide monomers and copolymers thereof for biocidal coatings

Номер: US20120183494A1
Автор: Hasan B. Kocer, Idris CERKEZ, Royall M. Broughton, Shelby D. Worley
Принадлежит: AUBURN UNIVERSITY

Novel acrylamide and methacrylamide hydantoin monomers which can be reacted with other acrylamide, methacrylamide, acrylate, and methacrylate monomers to form copolymers, which upon halogenation, provide oxidative coatings which are biocidal for use with various materials including, but not limited to, textiles, filters, and latex paints.

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Номер записи: 72
19-07-2012 дата публикации

Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent

Номер: US20120184535A1
Автор: Adrian Zarebski, Aleksandra Sabiniarz, Krzysztof Brzózka, Mariusz Millik, Nicolas Beuzen, Renata Windak, Wojciech Czardybon
Принадлежит: Selvita Sp zoo

A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.

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Номер записи: 73
19-07-2012 дата публикации

Novel compounds

Номер: US20120184553A1
Автор: Andrew John Eatherton, Daniele Andreotti, Karamjit Singh Jandu, Oliver James Philps, Paul Bamborough, Paula Louise Nichols
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.

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Номер записи: 74
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: 75
26-07-2012 дата публикации

Diarylthiohydantoin compounds

Номер: US20120190718A1
Автор: Charles L. Sawyers, Chris Tran, Dongwon Yoo, John Wongvipat, Michael E. Jung
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to diarylthiohydantoin compounds and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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Номер записи: 76
26-07-2012 дата публикации

Fused compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor

Номер: US20120190845A1
Автор: Arthur R. Gomtsyan, Chih-Hung Lee, Erol K. Bayburt, Gilles Chamboumier, John R. Koenig, Kirill A. Lukin, Margaret Chi-Ping Hsu, Robert G. Schmidt, Robert M. Leanna, Russell D. Cink
Принадлежит: Bayburt Erol K, Chih-Hung Lee, Cink Russell D, Gilles Chamboumier, Gomtsyan Arthur R, Koenig John R, Leanna Robert M, Lukin Kirill A, Margaret Chi-Ping Hsu, Schmidt Robert G

The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X 1 -X 5 , R 5 -R 8b , Z 1 -Z 2 and Ar 1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.

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Номер записи: 77
26-07-2012 дата публикации

Method for producing 4,6-dialkoxy-2-cyanomethylpyrimidine and synthetic intermediate thereof

Номер: US20120190851A1
Автор: Kentaro Kawazoe
Принадлежит: Ihara Chemical Industry Co Ltd

Disclosed is a method for producing 4,6-dialkoxy-2-cyanomethylpyrimidine and also disclosed is a synthetic intermediate thereof. More specifically disclosed is a method for producing 4,6-dialkoxy-2-cyanomethylpyrimidine represented by general formula (2) (wherein R represents an alkyl group), comprising reacting a t-butyl cyanoacetate derivative represented by general formula (1) (wherein R has the same meaning as described above) in the presence of an acid, and also disclosed is a t-butyl cyanoacetate derivative represented by general formula (1) (wherein R represents an alkylgroup).

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Номер записи: 78
09-08-2012 дата публикации

Phosphorus derivatives as kinase inhibitors

Номер: US20120202776A1
Автор: Anna Kohlmann, David C. Dalgarno, Dong ZOU, Feng Li, Jan Antoinette C. Romero, Jiwei Qi, R. Mathew Thomas, Shuangying Liu, Wei-Sheng Huang, William C. Shakespeare, Xiaotian Zhu, Yihan Wang
Принадлежит: Ariad Pharmaceuticals Inc

The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.

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Номер записи: 79
09-08-2012 дата публикации

Dual small molecule inhibitors of cancer and angiogenesis

Номер: US20120202800A1
Автор: Milton L. Brown
Принадлежит: UNIVERSITY OF VIRGINIA PATENT FOUNDATION

The present invention provides analogs and derivatives of thalidomide which inhibit cancer and angiogenesis. The present invention further provides compounds which disrupt microtubule polymerization. The present further provides methods of treating cancers comprising mutant p53.

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Номер записи: 80
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: 81
09-08-2012 дата публикации

Processes relating to the alkylation of pyrazoles

Номер: US20120203009A1
Автор: Linhua Wang, Maren Fuerst, Ritesh Bharat Sheth
Принадлежит: SYNGENTA CROP PROTECTION LLC

The present invention relates to processes for the preparation of a compound of formula (I) comprising reacting a compound of formula (IV) with a compound of formula III or (IIIA) in the presence of an acid; wherein R 1 is C 1 -C 4 haloalkyl; R 2 is optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; R 3 is methyl or ethyl; R 4 is hydrogen, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl; and n is 0 or 1.

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Номер записи: 82
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: 83
16-08-2012 дата публикации

Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors

Номер: US20120208817A1
Автор: Jian Qiu, Xicheng Sun
Принадлежит: N30 Pharmaceuticals Inc

The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

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Номер записи: 84
23-08-2012 дата публикации

3,4-disubstituted 1h-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators

Номер: US20120213791A1
Автор: Adrian Liam Gill, Alison Jo-Anne Woolford, Andrew James Woodhead, Gary Trewartha, Maria Grazia Carr, Michael Alistair O'brien, Paul Graham Wyatt, Theresa Rachel Early, Valerio Berdini
Принадлежит: ASTEX THERAPEUTICS LTD

The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.

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Номер записи: 85
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214782A1
Автор: Bernd Nosse, Gerald Juergen Roth, Heike Neubauer, Martin Fleck
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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Номер записи: 86
23-08-2012 дата публикации

Viral polymerase inhibitors

Номер: US20120214783A1
Автор: Alexandre Gagnon, Cedrickx Godbout, Jean Rancourt, Julie Naud, Marc-André JOLY, Martin Poirier, Montse Llinas-Brunet, Pasquale Forgione, Pierre L. Beaulieu
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula I: wherein X, R 2 , R 3 , R 3a , R 3b , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

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Номер записи: 87
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Автор: Bernd Nosse, Gerald Juergen Roth, Heike Neubauer, Joerg Kley, Martin Fleck, Niklas Heine, Thorsten Lehmann-Lintz
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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Номер записи: 88
23-08-2012 дата публикации

High Stability Diionic Liquid Salts

Номер: US20120215005A1
Автор: Daniel W. Armstrong, Jared Anderson
Принадлежит: Sigma Aldrich Co LLC

The present invention relates to diionic liquid salts of dicationic or dianionic molecules, as well as solvents comprising diionic liquids and the use of diionic liquids as the stationary phase in a gas chromatographic column.

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Номер записи: 89
30-08-2012 дата публикации

Guanidine-containing compounds useful as muscarinic receptor antagonists

Номер: US20120219509A1
Автор: Craig Husfeld, Li Li, Rick Lee, Yongqi Mu, YuHua Ji
Принадлежит: Theravance Inc

The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R 1-3 , R 5-7 , a, X, Y, Y′, Y″, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

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Номер записи: 90
30-08-2012 дата публикации

2-phenylethylamino derivatives as calcium and/or sodium channel modulators

Номер: US20120220592A1
Автор: Alessandra Restivo, Carla Caccia, Cibele Sabido-David, Ermanno Moriggi, Florian Thaler, Laura Faravelli, Mauro Napoletano, Patricia Salvati
Принадлежит: Newron Pharmaceuticals SpA

2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.

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Номер записи: 91
30-08-2012 дата публикации

Amino Acid Compounds

Номер: US20120220642A1
Автор: Alexander Nikolaidis, Ronald Kramer
Принадлежит: Thermolife International LLC

Methods for increasing the bioabsorption of amino acids and for preventing the development of nitrate tolerances in a human or animal are disclosed. The methods include administering to the human or animal a pharmaceutically effective amount of an amino acid compound consisting essentially of a nitrate or nitrite of an amino acid selected from the group consisting of Aspartic Acid, Cysteine, Glycine, Lysine, Methionine, Proline, Tyrosine, Phenylalanine, Carnitine, Taurine, and Betaine.

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Номер записи: 92
06-09-2012 дата публикации

Compositions and methods useful for treating diseases

Номер: US20120225851A1
Автор: Andrew F. Kolodziej, Michael H. Cardone, Xiang Y. Yu
Принадлежит: Eutropics Pharmaceuticals Inc

The present invention relates to a chemotherapeutic cancer treatment in which compounds of Formula Ia′, Ib′, Ic′, or II′ (referred to as a group as BH3Is) are administered to a mammal for the treatment of B-cell Lymphoma or other hematopoietic cancers, including diseases associated with MCL-1. In another aspect, the invention provides a method for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more compounds selected from the group consisting of compounds or Formula Ia, Ib, Ic, or II in combination with other therapies, for example, a class of therapeutics known as 26S proteosome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with pharmaceutical compositions comprising one or more compounds of Formula Ia′, Ib′, Ic′, or II′. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.

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Номер записи: 93
06-09-2012 дата публикации

Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as alzheimer's disease, type 2 diabetes and parkinson's disease

Номер: US20120225890A1
Автор: Alan D. Snow, Beth Nguyen, Charlotte Coffen, David L. Coffen, David Larsen, Gerardo Castillo, Lesley Larsen, Rex T. Weavers, Stephen Lorimer, Thomas Lake, Virginia Sanders
Принадлежит: ProteoTech Inc

Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially Aβ amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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Номер записи: 94
13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
Автор: William J. Polvino, William R. Mann
Принадлежит: Helsinn Therapeutics Us Inc

The present invention relates to methods of treating or preventing emesis and improving a subject's ASAS score by administering to the subject an effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.

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Номер записи: 95
20-09-2012 дата публикации

Iodine radiolabelling method

Номер: US20120237444A1
Автор: Michelle Avory
Принадлежит: Individual

The present invention provides a novel method of labelling biological targeting molecules (BTMs) of interest with radioiodine. Also provided are novel radioiodinated BTMs prepared using the method, as well as radiopharmaceutical compositions comprising such radioiodinated BTMs. The invention also provides radioiodinated intermediates useful in the method, as well as in vivo imaging methods using the radioiodinated BTMs.

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Номер записи: 96
04-10-2012 дата публикации

Heterocyclic GTP Cyclohydrolase 1 Inhibitors For the Treatment of Pain

Номер: US20120252791A1
Автор: Julian Blagg
Принадлежит: Individual

The present invention relates to the field of small molecule heterocyclic inhibitors of GTP cyclohydrolase (GCH-I), or a tautomer, prodrug, or pharmaceutically acceptable salt thereof. The invention also features pharmaceutical compositions of the compounds and the medical use of these compounds for the treatment or prevention of pain (e.g., inflammatory pain, nociceptive pain, functional pain, or neuropathic pain).

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Номер записи: 97
04-10-2012 дата публикации

Compounds, compositions, and methods for the treatment of beta-amyloid diseases and synucleinopathies

Номер: US20120252858A1
Автор: Alan D. Snow, F. Michael Hudson, Joel Cummings, Lesley Larsen, Luke A. Esposito, Manfred Weigele, Thomas Lake
Принадлежит: ProteoTech Inc

Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of β-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.

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Номер записи: 98
11-10-2012 дата публикации

Novel antiplatelet agent

Номер: US20120258951A1
Автор: Hiroshi Sato, Kazushi Sato, Kazutoshi Yokoyama
Принадлежит: Mitsubishi Tanabe Pharma Corp

The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR 1d , X b1 -X b5 are the same or different, and are nitrogen or carbon, R 1a -R 1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R 2 is an optionally substituted aryl or an optionally substituted heteroaryl, R 3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.

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Номер записи: 99
11-10-2012 дата публикации

Dual-acting pyrazole antihypertensive agents

Номер: US20120259113A1
Автор: Brooke BLAIR, Melissa Fleury, Michael Wilson, Paul R. Fatheree, Robert Murray Mckinnell, Roland Gendron, Ryan Hudson
Принадлежит: Theravance Inc

In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R 3 , R 4 and R 5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT 1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

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Номер записи: 100