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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 107994. Отображено 100.
05-01-2012 дата публикации

N-oxides of 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives useful as nicotinic acetylcholine receptor ligands

Номер: US20120004214A1
Автор: Dan Peters, Daniel B. Timmermann, Eva Dam Christoffersen
Принадлежит: Neurosearch AS

This invention relates to novel 1,4-diaza-bicyclo[3.2.2]nonyl pyrimidinyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Formula (I) a stereoisomer or a mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein Ar represents an indolyl group, which indolyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano, nitro, amino, alkyl, hydroxy and alkoxy.

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Номер записи: 1
05-01-2012 дата публикации

Novel tetrahydro-quinoline derivatives

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

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

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Номер записи: 2
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: 3
12-01-2012 дата публикации

11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds

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

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

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Номер записи: 4
19-01-2012 дата публикации

PYRROLO[2,3-b]PYRIDIN-4-YL-AMINES AND PYRROLO[2,3-b]PYRIMIDIN-5-YL-AMINES AS JANUS KINASE INHIBITORS

Номер: US20120014989A1
Автор: Andrew P. Combs, Haisheng Wang, James D. Rodgers, Richard B. Sparks
Принадлежит: Incyte Corp

The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.

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Номер записи: 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
26-01-2012 дата публикации

Triazole derivatives for treatment of alzheimer's disease

Номер: US20120022044A1
Автор: Adam J. Schell, Alexey A. Rivkin, Andrew Rosenau, Benito Munoz, Chaomin Li, Christian Fischer, Hua Zhou, Joey Methot, Matthew Christopher, Rachel N. Maccoss, Sam Kattar, Sean P. Ahearn, Stephanie Chichetti, William Colby Brown
Принадлежит: Individual

According to the invention there is provided a compound of formula I or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of Aβ42 and hence are useful in treatment of Alzheimer's disease and related conditions.

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Номер записи: 7
26-01-2012 дата публикации

Bridged compounds as hiv integrase inhibitors

Номер: US20120022045A1
Автор: Boyoung Kim, Dai-Shi Su, H. Marie LOUGHRAN, John Lim, John S. Wai, Mark W. Embrey, Peter D. Williams, Richard C.A. Isaacs, Shankar Venkatraman, Wayne Thompson
Принадлежит: Individual

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, χ3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

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Номер записи: 8
26-01-2012 дата публикации

Histamine h3 inverse agonists and antagonists and methods of use thereof

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

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

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Номер записи: 9
02-02-2012 дата публикации

pH MODULATION METHOD TO DETECT LIGAND-RECEPTOR BINDING

Номер: US20120028823A1
Автор: Aaron D. Robison, Hyunsook Jung, Paul S. Cremer
Принадлежит: TEXAS A&M UNIVERSITY SYSTEM

The present disclosure relates to detecting receptor-ligand binding by measuring local pH modulation using a pH-sensitive fluorophore.

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Номер записи: 10
02-02-2012 дата публикации

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

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

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

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Номер записи: 11
09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

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

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

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Номер записи: 12
23-02-2012 дата публикации

Pyrimido [5,4-d] pyrimidine derivatives for the inhibition of tyrosine kinases

Номер: US20120046270A1
Автор: Andreas Mantoulidis, Peter Ettmayer, Steffen Steurer
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention encompasses compounds of general formula (1), wherein the groups R 1 to R 4 , X 1 , X 2 , X 3 , X 4 , X 5 , Q, L 1 and L 2 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, as well as pharmaceutical preparations and formulations of these compounds.

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Номер записи: 13
23-02-2012 дата публикации

Compounds for treating neuropsychiatric conditions

Номер: US20120046283A1
Автор: Benedikt Vollrath, David Campbell, Sergio G. DURÓN, Warren Wade
Принадлежит: Afraxis Inc

Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions.

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Номер записи: 14
23-02-2012 дата публикации

Crystalization of pharmaceutical compounds

Номер: US20120046297A1
Автор: David R. Weyna, Mazen Hanna, Miranda L. Cheney, Ning SHAN
Принадлежит: Thar Pharmaceuticals Inc

Novel crystalline forms of tadalafil suitable for pharmaceutical compositions in drug delivery systems for humans.

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Номер записи: 15
01-03-2012 дата публикации

Azafluorene derivative and organic light-emitting device using the derivative

Номер: US20120049176A1
Автор: Akihiro Senoo, Hiroki Ohrui, Masanori Muratsubaki, Tetsuya Kosuge
Принадлежит: Canon Inc

A novel azafluorene derivative and an organic light-emitting device having the derivative are provided. The organic light-emitting device includes a pair of electrodes composed of an anode and a cathode one of which is a transparent or semi-transparent electrode, and an organic compound layer interposed between the pair of electrodes. The organic compound layer contains the azafluorene derivative represented by the following general formula (I):

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Номер записи: 16
01-03-2012 дата публикации

Nitrogen-Containing Fused Heterocyclic Compounds and Their use as Beta Amyloid Production Inhibitors

Номер: US20120053171A1
Автор: Daiju Hasegawa, Daisuke Shinmyo, Koichio Ito, Nobuaki Sato, Noritaka Kitazawa, Toru Watanabe, Toshiyuki Uemura
Принадлежит: Eisai R&D Management Co Ltd

A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

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Номер записи: 17
08-03-2012 дата публикации

Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine mch-1 antagonists, methods of making, and use thereof

Номер: US20120058939A9
Автор: Alan John Henderson, Emily Elizabeth FREEMAN, Mark Hadden, Matthew David Surman, Peter R. GUZZO
Принадлежит: Albany Molecular Research Inc

Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.

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Номер записи: 18
08-03-2012 дата публикации

Carbazole and carboline kinase inhibitors

Номер: US20120058988A1
Автор: Ashok Vinayak Purandare, Douglas G. Batt, Harold Mastalerz, Kurt Zimmermann, Qingjie Liu
Принадлежит: Bristol Myers Squibb Co

The present invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof The Formula (I) compounds inhibit tyrosine kinase activity of Jak2, thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

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Номер записи: 19
08-03-2012 дата публикации

Novel kinase modulators

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

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

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Номер записи: 20
15-03-2012 дата публикации

Compounds and their uses 708

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

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

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Номер записи: 21
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: 22
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: 23
29-03-2012 дата публикации

Hepatitis C Virus Inhibitors

Номер: US20120076755A1
Автор: Ce Wang, Hui Cao, LU Ying, Xiaowen Peng, Yao-Ling Qiu, Yat Sun Or
Принадлежит: Enanta Pharmaceuticals Inc

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B-W  (I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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Номер записи: 24
29-03-2012 дата публикации

Substituted Pyrazine (Thio)Pyrans with a Herbicidal Action

Номер: US20120077678A1
Автор: Anja Simon, Anna Aleksandra Michrowska, Bernd Sievernich, Dschun Song, Frank Stelzer, Johannes Hutzler, Julia Major, Klaus Grossmann, Klaus Kreuz, Liliana Parra Rapado, Matthias Witschel, Ricarda Niggeweg, Tao QU, Thomas Ehrhardt, Thomas Seitz, Trevor William Newton, William Karl Moberg
Принадлежит: BASF SE

Substituted pyrazines of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the pyrazines of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one pyrazine compound of the formula I to act on plants, their seed and/or their habitat.

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Номер записи: 25
29-03-2012 дата публикации

Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors

Номер: US20120077840A1
Автор: Falko Ernst Wolter, Marcel Van Gaalen, Margaretha Henrica Maria Bakker, Marjoleen Nijsen, Sean Colm Turner, Wilfried Hornberger
Принадлежит: Abbott GmbH and Co KG

The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

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Номер записи: 26
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: 27
12-04-2012 дата публикации

Bicyclic Compounds and Methods of Making and Using Same

Номер: US20120088793A1
Автор: Boaz Inbal, Gali Golan, Mercedes Lobera, Shomir Ghosh, VINCENT Jacques
Принадлежит: Nanotherapeutics Inc

Disclosed herein are compounds that may be modulators of 5-HT receptors, and methods of making and using same.

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Номер записи: 28
26-04-2012 дата публикации

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

Номер: US20120101086A1
Автор: Christian Alan Paul Smethurst, Emmanuel Hubert Demont, Gail Astra Lorraine Seal, James Matthew Bailey, Jason Witherington, John Alexander Brown, Lee Andrew Harrison
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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Номер записи: 29
26-04-2012 дата публикации

Diaza-spiro[5.5]undecanes

Номер: US20120101110A1
Автор: Bernard Lucien Roy, Chetan Pandit, Claudia Betschart, Dirk Behnke, Samuel Hintermann, Sangamesh Badiger, Silvio Ofner, Simona Cotesta
Принадлежит: Individual

The invention relates to compound of the formula I in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.

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Номер записи: 30
26-04-2012 дата публикации

Compounds

Номер: US20120101123A1
Автор: Chengyong Li, Haibo Zhang, Qinghua Meng, Xichen Lin
Принадлежит: Glaxo Group Ltd

The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.

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Номер записи: 31
26-04-2012 дата публикации

1,2,4-oxadiazol derivatives, their pharmaceutical compositions and their use as sphingosine 1-phosphate 1 receptor agonists

Номер: US20120101124A1
Автор: Feng Ren, Xichen Lin, Yugui Si
Принадлежит: Glaxo Group Ltd

1,2,4-Oxadiazol derivatives represented by formula (I) useful as sphingosine 1-phosphate 1 (S1P1) receptor agonists, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders mediated via S1P1 receptor are disclosed.

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Номер записи: 32
03-05-2012 дата публикации

Bait chemistries in hydrogel particles for serum biomarker analysis

Номер: US20120107959A1
Автор: Alessandra Luchini, Davide Tamburro, Lance Liotta, Virginia Espina
Принадлежит: George Mason Intellectual Properties Inc, Istituto Superiore di Sanita ISS

This invention describes the identification of novel organic dye chemistries that can be used as affinity baits to capture proteins and other biomolecules useful in the fields of medical diagnostics, environmental science, toxicology, and infectious disease. Incorporation of unique affinity dye compounds within hydrogel capture particles improves analyte yield and preanalytical precision, and stabilizes the analyte against degradation, while increasing measurement sensitivity. The particles in this invention can be used for routine clinical testing as well as for discovery of low abundance disease biomarkers. Example hydrogel particles containing new high affinity bait chemistries were used to identify a new set of human serum biomarkers.

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Номер записи: 33
03-05-2012 дата публикации

Fused piperidine compound and pharmaceutical containing same

Номер: US20120108581A1
Автор: Hajime Yamada, Hiroyuki Ishiwata, Masanori Ashikawa, Shunji Takemura, Takeshi Doi, Tatsuaki Nishiyama, Toshiharu Morimoto
Принадлежит: Kowa Co Ltd

The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C 10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R 7 , a sulfur atom or an oxygen atom, R 1 , R 2 , R 2′ , R 3 and R 3′ independently represent a hydrogen atom, C 1-6 alkyl group or C 3-6 cycloalkyl group, and R 4 , R 5 and R 6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.

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Номер записи: 34
03-05-2012 дата публикации

Azaquinazolinediones Chymase Inhibitors

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

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

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Номер записи: 35
03-05-2012 дата публикации

Compounds and compositions for treating chemical warfare agent-induced injuries

Номер: US20120108613A1
Автор: Jayhong A. Chong
Принадлежит: Hydra Biosciences LLC

Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

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Номер записи: 36
03-05-2012 дата публикации

N1/n2-lactam acetyl-coa carboxylase inhibitors

Номер: US20120108619A1
Автор: Aaron Smith, David A. Griffith, Robert L. Dow, Scott W. Bagley
Принадлежит: PFIZER INC

The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof; wherein G is R 1 , R 2 and R 3 are as described herein; pharmaceutical compositions thereof; and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.

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Номер записи: 37
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: 38
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: 39
17-05-2012 дата публикации

Radiolabeled cgrp antagonists

Номер: US20120121508A1
Автор: Craig A. Stump, Eric Hostetler, Harold G. Selnick, Ian M. Bell
Принадлежит: Merck Sharp and Dohme LLC

The present invention is directed to radiolabeled CGRP receptor antagonists which are useful for the quantitative imaging of CGRP receptors in mammals.

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Номер записи: 40
17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

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

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

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Номер записи: 41
17-05-2012 дата публикации

Heterocyclic compounds and uses thereof

Номер: US20120122838A1
Автор: Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder, Katrina Chan, Liansheng Li, Pingda Ren, Troy Edward Wilson, Yi Liu
Принадлежит: Infinity Pharmaceuticals Inc, INTELLIKINE LLC

Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.

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Номер записи: 42
17-05-2012 дата публикации

Aurora kinase modulators and method of use

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

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

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Номер записи: 43
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: 44
17-05-2012 дата публикации

Solid forms of sulfonamides and amino acids

Номер: US20120122860A1
Автор: Gary Conard Visor, Guoxian Wu, Hanna Cho, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak
Принадлежит: Plexxikon Inc

Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.

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Номер записи: 45
17-05-2012 дата публикации

Substituted Pyrrolo-Pyrimidine Derivatives, Process for Their Preparation and Their Use as Kinase Inhibitors

Номер: US20120122882A1
Автор: Barbara Valsasina, Helena Posteri, Italo Beria, Maria Gabriella Brasca, Marina Caldarelli, Michele Caruso, Walter Ceccarelli
Принадлежит: Nerviano Medical Sciences SRL

Substituted pyrrolo-pyrimidine derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a dysregulated protein kinase activity, like cancer.

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Номер записи: 46
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: 47
24-05-2012 дата публикации

Azaindazoles as kinase inhibitors and use thereof

Номер: US20120129852A1
Автор: Bin Jiang, Jingwu Duan, Zhonghui Lu
Принадлежит: Bristol Myers Squibb Co

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A 1 , A 2 , A 3 , R 4 are as defined herein.

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Номер записи: 48
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: 49
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: 50
31-05-2012 дата публикации

Novel phenylimidazole derivatives as pde10a enzyme inhibitors

Номер: US20120135987A1
Автор: Andreas Ritzen, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mohamed M. Farah, Morten Langgard
Принадлежит: H Lundbeck AS

This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.

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Номер записи: 51
31-05-2012 дата публикации

Pyridinyl Compounds Useful As Intermediates

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

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

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Номер записи: 52
07-06-2012 дата публикации

Oxazolidinone-quinolone hybrid antibiotics

Номер: US20120142635A1
Автор: Christian Hubschwerlen, Christine Schmitt, Daniel Baeschlin, Jean-Luc Specklin, Michael W. Cappi, Stefan Müller
Принадлежит: Morphochem AG fuer Kombinatorische Chemie

The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:

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Номер записи: 53
07-06-2012 дата публикации

Pyrrolidine Compounds Which Modulate The CB2 Receptor

Номер: US20120142677A1
Автор: Angela Berry, Doris Riether, Eugene Richard Hickey, Lifen Wu, Rajashekhar Betageri, Renee M. Zindell, Someina Khok
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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Номер записи: 54
07-06-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120142732A1
Автор: Courtney A. Cullis, Gang Li, Jianping Guo, Krista E. Granger, Masaaki Hirose, Miho Mizutani, Tricia J. Vos
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula IA or IB: wherein HY, R 1 , R 2 , and G 1 , are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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Номер записи: 55
07-06-2012 дата публикации

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

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

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

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Номер записи: 56
21-06-2012 дата публикации

Novel fused pyridine compounds as casein kinase inhibitors

Номер: US20120157440A1
Автор: Chakrapani Subramanyam, Ramalakshmi Y. Chandrasekaran, Scot R. Mente, Todd W. Butler, Travis T. Wager
Принадлежит: PFIZER INC

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, A, R 4 , n, and R 7 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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Номер записи: 57
28-06-2012 дата публикации

Hydrate of sulfonylurea compound, process for producing the same and suspension formulation containing the same

Номер: US20120165196A1
Автор: Daisaku KAMO, Yu Yanagisawa
Принадлежит: Sumitomo Chemical Co Ltd

The present invention relates to a hydrate of sulfonylurea compound represented by formula (I): having herbicidal activity, a process for producing the same, a suspension formulation containing the same, and the like.

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Номер записи: 58
28-06-2012 дата публикации

Novel azabicyclohexanes

Номер: US20120165320A1
Автор: Gurmeet Kaur, Gurmeet Kaur Nanda, Jagattaran Das, Nishan Singh, Rajseh Jain, Sandeep Kanwar, Sanjay Trehan, Sitaram Kumar Magadi, Sudhir Kumar Sharma
Принадлежит: Panacea Biotec Ltd

The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers including R and S isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof.

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Номер записи: 59
28-06-2012 дата публикации

Quinoline derivatives as pi3 kinase inhibitors

Номер: US20120165321A1
Автор: Carla A. Donatelli, Joelle Lorraine Burgess, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Michael Gerrard Darcy, Nicholas D. Adams, Stanley J. Schmidt, Steven David Knight
Принадлежит: GlaxoSmithKline LLC

Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.

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Номер записи: 60
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: 61
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: 62
05-07-2012 дата публикации

Second-order nonlinear optical compound and nonlinear optical element comprising the same

Номер: US20120172599A1
Автор: Akira Otomo, Hidehisa Tazawa, Hideki Miki, Isao Aoki, Shiyoshi Yokoyama
Принадлежит: Individual

Problem to Be Solved: to provide a chromophore having a far superior nonlinear optical activity to conventional chromophores and to provide a nonlinear optical element comprising said chromophore. Solution: a chromophore comprising a donor structure D, a π-conjugated bridge structure B, and an acceptor structure A, the donor structure D comprising an aryl group substituted with a substituted oxy group; and a nonlinear optical element comprising said chromophore.

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Номер записи: 63
12-07-2012 дата публикации

Lactam compounds useful as protein kinase inhibitors

Номер: US20120178739A1
Автор: Christopher Blackburn, Christopher F. Claiborne, Courtney A. Cullis, Gabriel S. Weatherhead, Matthew Stirling, Michael Patane, Natalie A. Dales, Omar Stradella
Принадлежит: Millennium Pharmaceuticals Inc

The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

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Номер записи: 64
19-07-2012 дата публикации

Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors

Номер: US20120184505A1
Автор: Janeta Popovici-Muller, Kristin E. Rosner, Timothy J. Guzi
Принадлежит: Individual

In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).

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Номер записи: 65
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: 66
02-08-2012 дата публикации

2-Oxo-1-Pyrrolidine Derivatives, Processes for Preparing Them and Their Uses

Номер: US20120196866A1
Автор: Ali Ates, Benoît KENDA, Joël MERCIER, Laurent Turet, PHILIPPE MICHEL, Yannick Quesnel
Принадлежит: UCB PHARMA SA

The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

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Номер записи: 67
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: 68
16-08-2012 дата публикации

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Номер: US20120206037A1
Автор: Bong Ok Kim, Hyuck Joo Kwon, Seung Soo Yoon, Soo Young Lee, Sung Min Kim, Young Gil Kim, Youngg Jun Cho
Принадлежит: Rohm and Haas Electronic Materials Korea Ltd

Provided are a novel organic electroluminescent compound and an organic electroluminescent device using the same. When used as a host material of an organic electroluminescent material of an OLED device, the organic electroluminescent compound disclosed herein exhibits good luminous efficiency and excellent life property as compared to the existing host material. Therefore, it may be used to manufacture OLEDs having very superior operation life.

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Номер записи: 69
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: 70
16-08-2012 дата публикации

Fluorinated aromatic materials and their use in optoelectronics

Номер: US20120208989A1
Автор: Haoran Sun
Принадлежит: University of South Dakota

Fluorinated aromatic materials, their synthesis and their use in optoelectronics. In some cases, the fluorinated aromatic materials are perfluoroalkylated aromatic materials that may include perfluoropolyether substituents.

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Номер записи: 71
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: 72
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: 73
23-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120214794A1
Автор: Brian S. Freeze, Hong Myung Lee, Leo R. Takaoka, Masaaki Hirose, Stepan Vyskocil, Tianlin Xu, Todd B. Sells, Zhan Shi
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula I-A or I-B: wherein HY, G 1 , G 2 , R 2 , R 12 , W 1 , W 2 , n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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Номер записи: 74
30-08-2012 дата публикации

Imidazopyrazine syk inhibitors

Номер: US20120220582A1
Автор: Kevin S. Currie, Scott A. Mitchell
Принадлежит: Gilead Connecticut Inc

Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

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Номер записи: 75
30-08-2012 дата публикации

Heterocyclic compounds and their uses

Номер: US20120220586A1
Автор: Andreas Reichelt, Brian Lucas, Dawei Zhang, Felix Gonzalez Lopez De Turiso, Jason A. Duquette, Jennifer Seganish, Lawrence R. Mcgee, Robert M. Rzasa, Timothy D. Cushing, Xiao He, Xiaolin Hao, Yi Chen, Youngsook Shin
Принадлежит: AMGEN INC

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110δ activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

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Номер записи: 76
30-08-2012 дата публикации

Novel spiropiperidine compounds

Номер: US20120220616A1
Автор: Chafiq Hamdouchi, Jayana Pankaj Lineswala, Pranab Maiti
Принадлежит: Eli Lilly and Co

A compound of the formula: or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition, and a method for treating diabetes.

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Номер записи: 77
06-09-2012 дата публикации

Mst1 kinase inhibitors and methods of their use

Номер: US20120225857A1
Автор: David John AUGERI, Jeffrey Thomas BAGDANOFF, John Anthony GILLERAN, Kenneth Gordon Carson, Konstantin SALOJIN, Leonard Sung, Marianne Carlsen, Simon David Peter BAUGH, Tamas Oravecz, Wei He
Принадлежит: Individual

Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.

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Номер записи: 78
06-09-2012 дата публикации

Heteroarylaminoquinolines as tgf-beta receptor kinase inhibitors

Номер: US20120225875A1
Автор: Alfred Jonczyk, Christiane Amendt, Frank Zenke
Принадлежит: Merck Patent GmBH

Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1 , are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

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Номер записи: 79
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: 80
06-09-2012 дата публикации

[1,5]-Diazocin Derivatives

Номер: US20120225892A1
Автор: Didier Roche, Fabrice Chimienti, Martin Ohsten
Принадлежит: MELLITECH

The present invention relates to compounds of formula (I) compositions, in particular pharmaceutical compositions, and medicaments comprising at least one compound of formula (I). The invention also relates to the use of such a compound for manufacturing a medicament. In particular the medicament and the pharmaceutical composition are intended to treat diseases linked with insulin regulation problems, such as diabetes. This invention aims also to methods for treating or preventing such diseases.

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Номер записи: 81
13-09-2012 дата публикации

Organic compound and photovoltaic device comprising the same

Номер: US20120227802A1
Автор: Alexey Nokel, Pavel Ivan Lazarev, Pavel Khokhlov
Принадлежит: Cryscade Solar Ltd

The present invention provides a organic compound of the general structural formula 1 and photovoltaic device and photovoltaic layer comprising thereof Said organic compound forms rod-like supramolecules and absorbs electromagnetic radiation in at least one predetermined spectral subrange within a wavelength range from 400 to 3000 nm with excitation of electron-hole pairs. The polycyclic core Cor 1 , the bridging group B, and the polycyclic core Cor 2 form a molecular system selected from the list comprising donor-bridge-acceptor-bridge-donor and acceptor-bridge-donor-bridge-acceptor in which a dissociation of excited electron-hole pairs is carried out. A solution of the organic compound or its salt forms a solid photovoltaic layer on a substrate.

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Номер записи: 82
13-09-2012 дата публикации

Compound having a substituted anthracene ring structure and pyridoindole ring structure, and organic electroluminescent device

Номер: US20120228598A1
Автор: Daizou Kanda, Eiji Takahashi, Hiroshi Ohkuma, Kouki Kase, Norimasa Yokoyama, Shuichi Hayashi
Принадлежит: Hodogaya Chemical Co Ltd

The present invention relates to a compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2); and an organic electroluminescent device having a pair of electrodes and at least one organic layer interposed therebetween, in which the compound having a substituted anthracene ring structure and a pyridoindole ring structure, which is represented by the following general formula (1) or the following general formula (2), is used as a constituent material of the aforementioned at least one organic layer.

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Номер записи: 83
13-09-2012 дата публикации

Methods of Treating or Preventing Autoimmune Diseases With 2,4-Pyrimidinediamine Compounds

Номер: US20120230984A1
Автор: Ankush Argade, Catherine Sylvain, Donald G. Payan, Holger Keim, HUI Li, Jeffrey Clough, Rajinder Singh, Somasekhar Bhamidipati
Принадлежит: Rigel Pharmaceuticals Inc

The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

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Номер записи: 84
13-09-2012 дата публикации

Novel opioid antagonists

Номер: US20120231543A1
Автор: Allan James Goodman, Bertrand Le Bourdonnec, Roland E. Dolle
Принадлежит: Adolor Corp

Certain quinolizidine and octahydropyridopyrazine compounds, pharmaceutical compositions, and methods of their use, inter alia, as opioid receptor antagonists are disclosed.

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Номер записи: 85
13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
Автор: Johan Oslob, John Burnier, Kenneth Barr, Min Zhong, Thomas Gadek, Wang Shen
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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Номер записи: 86
13-09-2012 дата публикации

Imidazopyridine derivatives

Номер: US20120232072A1
Автор: Mandar Bhonde, Nilesh Dagia, Pallavi Hanmantrao Mane, Pramod Bhaskar Kumar, Rajiv Sharma, Sanjay Kumar, Sivaramakrishnan Hariharan
Принадлежит: Piramal Life Sciences Ltd

The present invention relates to compounds of formula (I), wherein R a , R b , R c , R d , R e and R f are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PI3K), mammalian target of rapamycin (mTOR), Signal transducer and activator of transcription 3 (STAT 3), tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6) or a combination thereof particularly in the treatment of cancer and inflammation.

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Номер записи: 87
13-09-2012 дата публикации

Quinolizidinone carboxamide m1 receptor positive allosteric modulators

Номер: US20120232076A1
Автор: Ronald K. Chang, Scott D. Kuduk
Принадлежит: Individual

The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

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Номер записи: 88
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: 89
27-09-2012 дата публикации

Mglur4 allosteric potentiators, compositions, and methods of treating neurological dysfunction

Номер: US20120245153A1
Автор: Charles David Weaver, Colleen M. Niswender, Corey R. Hopkins, Craig W. Lindsley, Darren W. Engers, James M. Salovich, P. Jeffrey Conn, Patrick R. Gentry, Rocco D. Gogliotti, Yiu-Yin Cheung
Принадлежит: VANDERBILT UNIVERSITY

Compounds useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) and use thereof.

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Номер записи: 90
27-09-2012 дата публикации

Diphenyl-pyrazolopyridine derivatives, preparation thereof, and use thereof as nuclear receptor not modulators

Номер: US20120245164A1
Автор: Florian Auger, Luc Even
Принадлежит: SANOFI SA

The invention relates to a formula (I), in which R is a hydrogen or halogen atom or a (C1-C6)alkyl group; X is one or more substituents selected from a hydrogen or halogen atom, a (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkoxy, cyano, hydroxy, or hydroxy(C1-C6)alkyl group; Y is a hydrogen or halogen atom or a (C1-C6)alkyl group; R1 is an NR2R3 or OR4 group; R2 and R3 independently are a hydrogen atom, a (C1-C6)alkyl, hydroxy(C1-C6)alkyl or oxo(C1-C6)alkyl group or R2 and R3, together with the nitrogen atom supporting the same, form a heterocycle optionally substituted by a (C1-C6)alkyl, hydroxy or oxo group; and R4 is a (C1-C6)alkyl, hydroxy(C1-C6)alkyl, or oxo(C1-C6)alkyl group, in the base or acid addition salt state. Said formula can be used therapeutically for treating or preventing diseases linked to the nuclear receptors Nurr-1, also known as NR4A2, NOT, TINUR, RNR-1, and HZF3.

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Номер записи: 91
04-10-2012 дата публикации

Bicyclic pyridines and analogs as sirtuin modulators

Номер: US20120252780A1
Автор: Charles Blum, Chi B. Vu, Jeremy S. Disch, Lauren Mcpherson, Mohammed Mahmood Ahmed, Pui Yee Ng, Robert B. Perni
Принадлежит: Charles Blum, Disch Jeremy S, Lauren Mcpherson, Mohammed Mahmood Ahmed, Perni Robert B, Pui Yee Ng, Vu Chi B

Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.

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Номер записи: 92
11-10-2012 дата публикации

Inhibitors of e1 activating enzymes

Номер: US20120258927A1
Автор: Edward J. Olhava, Stepan Vyskocil, Steven P. Langston
Принадлежит: Millennium Pharmaceuticals Inc

This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.

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Номер записи: 93
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: 94
11-10-2012 дата публикации

Substituted N-(1H-Indazol-4-yl)Imidazo[1,2-a]Pyridine-3-Carboxamide Compounds as cFMS Inhibitors

Номер: US20120258952A1
Автор: April L. Kennedy, Bryson Rast, D. David Hennings, Fredrik P. Marmsater, George T. Topalov, James P. Rizzi, Mark C. Munson, Mark Laurence Boys, Martha E. Rodriguez, Matthew David Medina, Michael F. Bradley, Qian Zhao, Robert Kirk Delisle
Принадлежит: Array Biopharma Inc

Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.

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Номер записи: 95
11-10-2012 дата публикации

Novel Process for the Preparation of Paliperidone

Номер: US20120259116A1
Автор: Dattatray Shamrao Metil, Dharmesh Kumar Arvindbhaipatel, Prashant Pandurangpawar, Praveen Raosaheb Supekar, Rajiv Kumar, Santosh Vitthal Pune
Принадлежит: Alkem Laboratories Ltd

The present invention relates to a novel process for the preparation of paliperidone by hydrolysis of 9 -O-acylated paliperidone. In a preferred embodiment of the present invention, Paliperidone Form (II) of purity of about 98 % or more was obtained by basic hydrolysis of 9-O-Acetyl Paliperidone.

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Номер записи: 96
18-10-2012 дата публикации

PROCESS FOR MAKING (R) -3-(2,3-DIHYDROXYPROPYL)-6-FLUORO-5-(2-FLOURO-4-IODOPHENYLAMINO)-8-METHYLPYRIDO[2,3-d]PYRIMIDINE-4,7(3H,8H)-DIONE AND INTERMEDIATES THEREOF

Номер: US20120264967A1
Автор: David Paul Provencal, Jonathon S. Salsbury, Todd Miller, Yuxin Zhao
Принадлежит: Takeda Pharmaceutical Co Ltd

The present invention relates generally to processes of making (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione, intermediates thereof, and a process for making a particular polymorph of (R)-3-(2,3-Dihydroxypropyl)-6-fluoro-5-(2-fluoro-4-iodophenylamino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione.

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Номер записи: 97
25-10-2012 дата публикации

Adamantyl diamide derivatives and uses of same

Номер: US20120270873A1
Автор: Andrew D. White, Dario Doller, Gil Ma, Guiying Li, Hermogenes N. Jimenez, Maojun Guo, Michel Grenon
Принадлежит: H Lundbeck AS

The present invention provides adamantyl-diamide derivatives of formula (I): wherein R 1 and R 2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.

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Номер записи: 98
01-11-2012 дата публикации

Aromatic heterocyclic derivative and organic electroluminescence device using the same

Номер: US20120273766A1
Автор: Kazuki Nishimura, Tomoki Kato
Принадлежит: Idemitsu Kosan Co Ltd

An aromatic heterocyclic derivative represented by the following formula (1), a material for an organic electroluminescence device and an organic electroluminescence device including these:

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Номер записи: 99
01-11-2012 дата публикации

Novel heterocyclic acrylamides and their use as pharmaceuticals

Номер: US20120277207A1
Автор: Alexis Denis, Mayalen Oxoby, Sonia Escaich, Vincent Gerusz
Принадлежит: FAB PHARMA Sas

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

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Номер записи: 100