Настройки

Укажите год
-

Небесная энциклопедия

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год
Применить Всего найдено 93670. Отображено 100.
05-01-2012 дата публикации

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

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

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

Подробнее
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.

Подробнее
Номер записи: 2
05-01-2012 дата публикации

Salt of cd 80 antagonist

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

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

Подробнее
Номер записи: 3
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.

Подробнее
Номер записи: 4
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.

Подробнее
Номер записи: 5
12-01-2012 дата публикации

Choline and tromethamine salt of licofelone

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

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

Подробнее
Номер записи: 6
12-01-2012 дата публикации

Modulation of anxiety through blockade of anandamide hydrolysis

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

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

Подробнее
Номер записи: 7
12-01-2012 дата публикации

Improved chemical synthesis of diazaindoles by chichibabin cyclization

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

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

Подробнее
Номер записи: 8
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.

Подробнее
Номер записи: 9
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.

Подробнее
Номер записи: 10
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.

Подробнее
Номер записи: 11
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.

Подробнее
Номер записи: 12
02-02-2012 дата публикации

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

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

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

Подробнее
Номер записи: 13
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.

Подробнее
Номер записи: 14
23-02-2012 дата публикации

Compounds for the Treatment of Hepatitis C

Номер: US20120046294A1
Автор: John F. Kadow, Richard Pracitto
Принадлежит: Bristol Myers Squibb Co

The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Подробнее
Номер записи: 15
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.

Подробнее
Номер записи: 16
08-03-2012 дата публикации

Novel Indicator Platform

Номер: US20120058503A1
Автор: Alexander Bayer, Christophe Weymuth, Gunter Schabert, Lukas Wick, Urs Spitz
Принадлежит: Biosynth AG

A novel indicator platform comprises a plurality of 1H-lndol-3-yl indicator compounds that are capable of converting to a signalophore compound in response to an external stimulus. In one class of indicator compounds, the resulting signalophores are 2-benzylideneindoline compounds that are formed by an intermolecular Aldol-type process; in a further class of indicator compounds, the resulting signalophores are 10H-indolo[1,2-a]indole compounds that are formed by an intramolecular Aldol-type process. The indicators can be used in a wide array of applications relating, for example, to biological systems or optical data storage.

Подробнее
Номер записи: 17
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.

Подробнее
Номер записи: 18
08-03-2012 дата публикации

Carbazole carboxamide compounds useful as kinase inhibitors

Номер: US20120058996A1
Автор: Andrew J. Tebben, Douglas G. Batt, George V. DeLucca, Qing Shi, Qingjie Liu
Принадлежит: Bristol Myers Squibb Co

Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.

Подробнее
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.

Подробнее
Номер записи: 20
08-03-2012 дата публикации

Diketopyrrolopyrrole polymers for use in organic semiconductor devices

Номер: US20120059140A1
Автор: Hans Jürg Kirner, Marta Fonrodona Turon, Mathias DÜGGELI, Olivier Frédéric AEBISCHER, Pascal Hayoz
Принадлежит: BASF SE

The present invention relates to polymers comprising one or more (repeating) unit(s) of the formula (I) which are characterized in that Ar 1 and Ar 1 ′ are independently of each other are an annulated (aromatic) heterocyclic ring system, containing at least one thiophene ring, which may be optionally substituted by one, or more groups, and their use as organic semiconductor in organic devices, especially in organic photovoltaics (solar cells) and photodiodes, or in a device containing a diode and/or an organic field effect transistor. The polymers according to the invention have excellent solubility in organic solvents and excellent film-forming properties. In addition, high efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when the polymers according to the invention are used in organic field effect transistors, organic photovoltaics (solar cells) and photodiodes.

Подробнее
Номер записи: 21
22-03-2012 дата публикации

N-[(2-azabicyclo[2.1.1]hex-1-yl)-aryl-methyl]-benzamide derivatives, preparation thereof, and therapeutic use thereof

Номер: US20120071536A1
Автор: Abdel-Kader Mafroud, Genevieve Estenne-Bouhtou, Gihad Dargazanli
Принадлежит: SANOFI SA

The invention relates to N-[(2-aza-bicyclo[2.2.1]hex-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C 1 -C 6 )alkyl group, (C 3 -C 7 )-cycloalkyl, optionally substituted by one or more fluorine, (C 3 -C 7 )-cycloalkyl, (C 2 -C 4 )alkenyl, phenyl, (C 1 -C 6 )alkoxy, hydroxy; R 1 is phenyl or naphtyl optionally substituted by one or more halogen, (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, halo-(C 1 -C 6 )alkyl, NR 4 R 5 , (C 1 -C 6 )alkylthio, (C 1 -C 6 )alkyl-SO 2 , phenyl or heteroaryl; R 2 is one or more hydrogen or halogen atoms, halo-(C 1 -C 6 )alkyl, (C 1 -C 6 )alkyl, (C 3 -C 7 )cycloalkyl, (C 3 -C 7 )-cycloalkyl-(C 1 -C 3 )alkyl; R 3 , R 4 and R 5 are independently a hydrogen atom or a (C 1 -C 6 )alkyl group; R 6 is a (C 1 -C 6 )alkyl group; R 3 and R 4 as well as R 3 and R 6 may form, together with the atoms having them, a 5- or 6-member ring; R 4 and R 5 may form together a ring selected from azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, azepine, optionally substituted by a (C 1 -C 6 )alkyl group. The invention also relates to the therapeutic use thereof and to a method for synthesizing same.

Подробнее
Номер записи: 22
29-03-2012 дата публикации

Light-driven rotary molecular motors

Номер: US20120074336A1
Автор: Christine R. Cremo, John H. Frederick, Joseph I. Cline, Stephen L. Gillett, Thomas W. Bell
Принадлежит: Nevada System of Higher Education NSHE

Compounds of Formula ( 1 ) are disclosed: C b is a carbocyclic or heterocyclic group having an atom within the cyclic structure selected from C, N, Si, and C r and singly bound to A. A is CR, COR, CSR, CNR 2 , CCN, CCONR 2 , CNO 2 , CNNAr, CX′, or N. C r is a chromophore having a substantially planar cyclic structure. The compounds function as nanometer-scale rotary molecular motors powered and controlled by light energy. The design of the molecular motor devices is flexible so that the rotary direction, drive light wavelength, and other physical characteristics can be varied. The compounds can be chemically functionalized to allow it to be integrated into or attached to a variety of structures. The device can be used in applications where mechanical power, positional control, and information encoding are to be generated at the size scale of individual molecules.

Подробнее
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.

Подробнее
Номер записи: 24
29-03-2012 дата публикации

Novel salts of sitagliptin

Номер: US20120077760A1
Автор: Ivan Plantan, Lovro Selic
Принадлежит: Lek Pharmaceuticals dd

The present invention relates to novel pharmaceutically acceptable salts of sitagliptin, to processes for their preparation and to pharmaceutical compositions containing them.

Подробнее
Номер записи: 25
29-03-2012 дата публикации

Sulfonamide, sulfamate, and sulfamothioate derivatives

Номер: US20120077814A1
Автор: Emilie D. Smith, James M. Veal, Kenneth H. HUANG, Robert N. Atkinson, Rong Jiang, Zhong Wang
Принадлежит: Individual

The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.

Подробнее
Номер записи: 26
29-03-2012 дата публикации

Chemical compounds

Номер: US20120077828A1
Автор: Dirk A. Heerding, Jeffrey Michael Axten, Jesus Raul Medina, JUN TANG, Seth Wilson Grant, Stuart Paul Romeril
Принадлежит: GlaxoSmithKline LLC

The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R 1 , R 2 , and R 3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

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

Use of inhibitors of bruton's tyrosine kinase (btk)

Номер: US20120087915A1
Автор: David J. Loury, Eric Hedrick, Gwen Fyfe, Joseph J. Buggy, Laurence Elias, Tarak D. Mody
Принадлежит: Pharmacyclics LLC

Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

Подробнее
Номер записи: 28
12-04-2012 дата публикации

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

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

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

Подробнее
Номер записи: 29
19-04-2012 дата публикации

Pyrido [5, 4-d] pyrimidines as cell proliferation inhibitors

Номер: US20120094975A1
Автор: Andreas Mantoulidis, Christian Klein, Georg Dahmann, Irene Waizenegger, Peter Ettmayer, Steffen Steurer, Stephan Karl Zahn
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 1 , X 3 , L 1 and L 2 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by excessive or anomalous cell pro-liferation, and the use thereof in such a treatment.

Подробнее
Номер записи: 30
19-04-2012 дата публикации

Pyrrolopyrrole derivatives, their manufacture and use as semiconductors

Номер: US20120095236A1
Автор: Marta Fonrodona Turon, Mathias Dueggeli, Mathieu G.R. Turbiez, Natalia Chebotareva, Olivier Frédéric AEBISCHER, Pascal Hayoz
Принадлежит: BASF SE

The present invention relates to compounds of the formula (I) wherein the substituents are as defined in claim 1 , and their use as organic semiconductor in organic devices, like diodes, organic field effect transistors and/or solar cells. The compounds of the formula I have excellent solubility in organic solvents. High efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when said compounds are used in semiconductor devices or organic photovoltaic (PV) devices (solar cells).

Подробнее
Номер записи: 31
03-05-2012 дата публикации

Processes for preparing amine salts of sildenafil-analogues and use thereof

Номер: US20120108604A1
Автор: Ing-Jun Chen
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R 1 , R a and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.

Подробнее
Номер записи: 32
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.

Подробнее
Номер записи: 33
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.

Подробнее
Номер записи: 34
10-05-2012 дата публикации

Use of selective gaba a alpha 5 negative allosteric modulators for the treatment of central nervous system conditions

Номер: US20120115839A1
Автор: Andrew Thomas, Maria-Clemencia Hernandez, Rodolfo Gasser
Принадлежит: Hoffmann La Roche Inc

The present invention relates to the pharmaceutical use of selective GABA A α5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.

Подробнее
Номер записи: 35
10-05-2012 дата публикации

Porphyrin compounds comprising one or more pyridone moieties

Номер: US20120115901A1
Автор: Chuchawin Changtong, John L. Lombardi, Robert E. Connors
Принадлежит: VENTANA RESEARCH Corp

Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.

Подробнее
Номер записи: 36
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.

Подробнее
Номер записи: 37
17-05-2012 дата публикации

Aurora kinase modulators and method of use

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

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

Подробнее
Номер записи: 38
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.

Подробнее
Номер записи: 39
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.

Подробнее
Номер записи: 40
31-05-2012 дата публикации

Substituted Esters as Cannabinoid-1 Receptor Modulators

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

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

Подробнее
Номер записи: 41
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.

Подробнее
Номер записи: 42
31-05-2012 дата публикации

Inhibitors of human phosphatidylinositol 3-kinase delta

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

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

Подробнее
Номер записи: 43
31-05-2012 дата публикации

Organic compounds

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

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

Подробнее
Номер записи: 44
07-06-2012 дата публикации

Crystalline compound of 7-[(3r)-3-amino-1-oxo-4-(2, 4, 5-trifluorphenyl)butyl]-5, 6, 7, 8-tetrahydro-3-(tri fluormethyl)-1, 2, 4 -triazolo[4,3-a]pyrazin

Номер: US20120142693A1
Автор: Fritz Blatter, Katharina REICHENBÄCHER
Принадлежит: SANDOZ AG

A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 1 with fumaric acid or a hydrate thereof, where the molar ratio of the compound of formula 1 to fumaric acid is 1:0.6 to 1:1.3 is described.

Подробнее
Номер записи: 45
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.

Подробнее
Номер записи: 46
14-06-2012 дата публикации

Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes

Номер: US20120149637A1
Автор: Ann E. Weber, Jason M. Cox, Ping Chen, Tesfaye Biftu
Принадлежит: Individual

The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Подробнее
Номер записи: 47
21-06-2012 дата публикации

Raf inhibitor compounds and methods of use thereof

Номер: US20120157451A1
Автор: Joachim Rudolph, Li Ren, Stefan Gradl
Принадлежит: Genentech Inc

Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Подробнее
Номер записи: 48
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.

Подробнее
Номер записи: 49
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.

Подробнее
Номер записи: 50
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.

Подробнее
Номер записи: 51
28-06-2012 дата публикации

Inhibitors of b lymphocyte kinase

Номер: US20120165328A1
Автор: David J. Loury, Erik J. Verner, Joseph J. Buggy, Lee Honigberg, Wei Chen
Принадлежит: Pharmacyclics LLC

Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

Подробнее
Номер записи: 52
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.

Подробнее
Номер записи: 53
05-07-2012 дата публикации

4 substituted pyrazolopyrimidines

Номер: US20120172379A1
Автор: Andrew Miller, Juan-Miguel Jimenez
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

Подробнее
Номер записи: 54
12-07-2012 дата публикации

DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-a]IMIDAZOLE-3-CARBOXYLIC ACID AMIDES

Номер: US20120178734A1
Автор: Jennifer A. Kowalski, Matt Aaron Tschantz
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

Подробнее
Номер записи: 55
12-07-2012 дата публикации

Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use

Номер: US20120178736A1
Автор: Brian Safina, Bryan Chan, Daniel P. Sutherlin, David Goldstein, Eileen Mary Seward, Georgette Castanedo, Matthew Lucas, Pascal Pierre Alexandre Savy, Rama KONDRU, Stephen Price, Wylie Palmer, Zachary K. Sweeney
Принадлежит: Individual

Formula I (Ia and Ib) compounds wherein (i) X 1 is N and X 2 is S, (ii) X 1 is CR 7 and X 2 is S, (iii) X 1 is N and X 2 is NR 2 , or (iv) X 1 is CR 7 and X 2 is 0, including stereoisomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Подробнее
Номер записи: 56
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.

Подробнее
Номер записи: 57
12-07-2012 дата публикации

Novel compounds for inhibiting eef-2 kinase activity

Номер: US20120178769A1
Автор: Alexey G. Ryazanov
Принадлежит: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY

The present invention discloses novel compounds for inhibiting eEF2 kinase and methods of use thereof.

Подробнее
Номер записи: 58
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.

Подробнее
Номер записи: 59
19-07-2012 дата публикации

use of inhibitors of bruton's tyrosine kinase (btk)

Номер: US20120183535A1
Автор: David J. Loury, Eric Hedrick, Gwen Fyfe, Joseph J. Buggy, Laurence Elias, Tarak D. Mody
Принадлежит: Pharmacyclics LLC

Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.

Подробнее
Номер записи: 60
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).

Подробнее
Номер записи: 61
19-07-2012 дата публикации

Inhibitors of bruton's tyrosine kinase

Номер: US20120184567A1
Автор: David J. Loury, Erik J. Verner, Joseph J. Buggy, Lee Honigberg, Wei Chen
Принадлежит: Pharmacyclics LLC

Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.

Подробнее
Номер записи: 62
26-07-2012 дата публикации

Compositions and methods for dna sequencing

Номер: US20120190012A1
Автор: Christopher ANDOLINA, Ga-Lai LAW, Nathaniel G. Butlin
Принадлежит: Lumiphore Inc

The invention provides compositions and methods useful in DNA sequencing. In exemplary embodiments, a detectable label such as a luminescent macrocycle is used.

Подробнее
Номер записи: 63
26-07-2012 дата публикации

Treatment or prophylaxis of proliferative conditions

Номер: US20120190639A1
Автор: Saraj Ulhaq, Steven Albert Everett
Принадлежит: UNIVERSITY OF DUNDEE

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

Подробнее
Номер записи: 64
26-07-2012 дата публикации

Substituted pyrazolo-quinazoline derivatives as kinase inhibitors

Номер: US20120190678A1
Автор: Antonella Ermoli, Claudia Piutti, Daniela Faiardi, Francesco Casuscelli
Принадлежит: Nerviano Medical Sciences SRL

The present invention relates to substituted pyrazolo[4,3-h]quinazoline compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular PIM kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.

Подробнее
Номер записи: 65
26-07-2012 дата публикации

Novel Protein Kinase B Inhibitors - 060

Номер: US20120190679A1
Автор: Andrew Leach, Jeffrey James Morris, Paul David Johnson, Richard William Arthur Luke, Zbigniew Stanley Matusiak
Принадлежит: AstraZeneca AB

The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z 1 , Z 2 , R 1 , R 4 , R 5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).

Подробнее
Номер записи: 66
26-07-2012 дата публикации

Process for the preparation of antibiotic compounds

Номер: US20120190842A1
Автор: Shiuan-Ting Chuang, Wei-Hong Tseng, Wen-Hsin Chang
Принадлежит: Savior Lifetec Corp

The present invention relates to a process for the preparation of carbapenem antibiotic compounds, which is useful for intravenous and intramuscular administration.

Подробнее
Номер записи: 67
02-08-2012 дата публикации

IAP BIR domain binding compounds

Номер: US20120195915A1
Автор: Alain Boudreault, Alain Laurent, James Jaquith, Patrick Bureau, Scott Jarvis
Принадлежит: Pharmascience Inc

Disclosed herein is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a prodrug, or a pharmaceutically acceptable salt, or labeled with a detectable label or an affinity tag thereof; wherein R 1 , R 1a , R 100 , R 100a , R 2 , R 200 , W, B, and W 1 are defined herein. Also disclosed are methods of using compounds of Formula I to treat proliferative disorders such as cancer.

Подробнее
Номер записи: 68
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.

Подробнее
Номер записи: 69
09-08-2012 дата публикации

Therapeutic isoxazole compounds

Номер: US20120202786A1
Автор: Alan P. Kaplan, Andrew J. Mcriner, Terence P. Keenan
Принадлежит: Dart Neuroscience Cayman Ltd

The invention provides a compound of formula I: wherein A 1 , A 2 , A 3 , R 1 , X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.

Подробнее
Номер записи: 70
09-08-2012 дата публикации

SUBSTITUTED [(5H-PYRROLO[2,1-c][1,4]BENZODIAZEPIN-11-YL)PIPERAZIN-1-YL]-2,2-DIMETHYLPROPANOIC ACID COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS

Номер: US20120202797A1
Автор: Adam Jan Sanderson, Andrew James Ledgard, Anne Marie Camp, David Andrew Coates, Peter Thaddeus Gallagher
Принадлежит: Eli Lilly and Co

A dual H1/5-HT 2A receptor antagonist of the formula: its uses, and methods for its preparation are described.

Подробнее
Номер записи: 71
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.

Подробнее
Номер записи: 72
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.

Подробнее
Номер записи: 73
16-08-2012 дата публикации

Pyrrolopyrimidine compounds and their uses

Номер: US20120207763A1
Автор: Christopher Thomas Brain, Gebhard Thoma, Moo Je Sung
Принадлежит: ASTEX THERAPEUTICS LTD

The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.

Подробнее
Номер записи: 74
23-08-2012 дата публикации

6,5-heterocyclic propargylic alcohol compounds and uses therefor

Номер: US20120214762A1
Автор: Christian A.G.N. Montalbetti, Jianwen Feng, Pui Leng Loke, Steven Staben
Принадлежит: Genentech Inc

The invention relates to novel compounds of Formula I: wherein A, Y, R 1 , R 2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Подробнее
Номер записи: 75
30-08-2012 дата публикации

Application of quantum dots for nuclear staining

Номер: US20120219948A1
Автор: Adrian E. Murillo, Brian Daniel Kelly, Chol Steven Yun, Christopher A. Bieniarz, Julia Ashworth-Sharpe, Pascal Bamford
Принадлежит: Ventana Medical Systems Inc

Embodiments of a system, method, and kit for visualizing a nucleus are disclosed. A tissue sample is pretreated with a protease to permeabilize the nucleus, and then incubated with a nanoparticle/DNA-binding moiety conjugate. The DNA-binding moiety includes at least one DNA-binding molecule. The conjugate binds to DNA within the nucleus, and the nanoparticle is visualized, thereby visualizing the nucleus. Computer and image analysis techniques are used to evaluate nuclear features such as chromosomal distribution, ploidy, shape, size, texture features, and/or contextual features. The method may be used in combination with other multiplexed tests on the tissue sample, including fluorescence in situ hybridization. Kits for performing the method include a protease enzyme composition, a nanoparticle/DNA-binding moiety conjugate, and a reaction buffer.

Подробнее
Номер записи: 76
30-08-2012 дата публикации

Tricyclic inhibitors of kinases

Номер: US20120220572A1
Автор: Alan S. Florjancic, Julie Miyashiro, Keith W. Woods, Thomas D. Penning, Yunsong Tong
Принадлежит: ABBOTT LABORATORIES

The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R 3 and R 4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.

Подробнее
Номер записи: 77
30-08-2012 дата публикации

Benzodiazepine Bromodomain Inhibitor

Номер: US20120220573A1
Автор: Olivier Mirguet, Romain Luc Marie Gosmini
Принадлежит: GlaxoSmithKline LLC

The present invention relates to a benzodiazepine compound of formula (I), processes for its preparation, pharmaceutical compositions containing such a compound and to its use in therapy.

Подробнее
Номер записи: 78
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.

Подробнее
Номер записи: 79
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.

Подробнее
Номер записи: 80
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.

Подробнее
Номер записи: 81
06-09-2012 дата публикации

Pyrrolo [2,3-d] pyrimidines as non-nucleoside reverse transcriptase inhibitors for treatment of hiv

Номер: US20120226037A1
Автор: Hong Woo Kim, Jean-Luc Girardet, Stephanie Shaw, Yung-Hyo Koh, Zhi Hong
Принадлежит: Ardea Biociences Inc

This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

Подробнее
Номер записи: 82
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.

Подробнее
Номер записи: 83
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.

Подробнее
Номер записи: 84
27-09-2012 дата публикации

Process for the production of a pemetrexed salt

Номер: US20120245349A1
Автор: Huanghsiung Lin, Shanghong Chen
Принадлежит: Scinopharm Taiwan Ltd

A process of making a pemetrexed salt comprising: a) reacting a compound of formula II or an acid salt thereof, wherein each of R 1 and R 2 is independently a C1-C6 alkyl group, with an aqueous basic solution at a temperature of no more than 10° C. to obtain a first mixture comprising the pemetrexed salt; b) isolating the pemetrexed salt from the first mixture.

Подробнее
Номер записи: 85
04-10-2012 дата публикации

Pyrazolo pyrimidine derivatives

Номер: US20120252778A1
Автор: Andrea Vaupel, Berndt Oberhauser, Juraj Velcicky, Klaus Weigand, Rajender Reddy Leleti, Wolfgang Miltz, Yugang Liu, Zhengming Du
Принадлежит: NOVARTIS AG

The present invention relates to pyrazolo pyrimidine derivatives, to methods of preparing these, to combinations and pharmaceutical composition comprising these, and to their use in the treatment of diseases and disorders which may for example involve autoimmune diseases, angiogenesis, pain, and/or inflammatory diseases.

Подробнее
Номер записи: 86
04-10-2012 дата публикации

Heterocyclyl pyrazolopyrimidine analogues as jak inhibitors

Номер: US20120252779A1
Автор: Andrew Ratcliffe, Claudio Dagostin, Cyrille Boussard, Kathryn Bell, Nelly Piton, Nigel Ramsden, Richard John Harrison, Sally Oxenford
Принадлежит: Cellzome Ltd

The invention relates to compounds of formula (I) wherein X 1 to X 5 , Y, Z 1 to Z 3 , and R have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

Подробнее
Номер записи: 87
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).

Подробнее
Номер записи: 88
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.

Подробнее
Номер записи: 89
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.

Подробнее
Номер записи: 90
11-10-2012 дата публикации

Pyrrolo[2,3-d]pyrimidine derivatives: their intermediates and synthesis

Номер: US20120259115A1
Автор: Frank J. Urban, Jennifer L. Rutherford, Joel M. Hawkins, Sally Gut Ruggeri, Teresa M. Makowski
Принадлежит: PFIZER INC

This invention relates to methods and intermediates useful for the synthesis of pyrrolo [2,3-d] pyrimidine compounds. Specifically novel synthetic methods and intermediates for the synthesis of 3-{(3R,4R)-4-methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino}-piperidin-1-yl)-3-oxo-propionitrile and its corresponding citrate salt are disclosed.

Подробнее
Номер записи: 91
18-10-2012 дата публикации

Substituted porphyrins

Номер: US20120264725A1
Автор: Ines Batinic-Haberle, Irwin Fridovich, Ivan Spasojevic
Принадлежит: Individual

Substituted metalloporphyrin compounds are described, along with pharmaceutical compositions containing the same, and methods of use thereof in protecting cells from oxidant-induced toxicity and pathological conditions such as inflammatory lung disease, neurodegenerative conditions, radiation injury, cancer, diabetes, cardiac conditions and sickle cell disease. Mn(III) porphyrins bearing oxygen atoms within side chains are particularly described.

Подробнее
Номер записи: 92
25-10-2012 дата публикации

Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors

Номер: US20120271045A1
Автор: Jean-Damien Charrier, Michael O'donnell, Steven Durrant
Принадлежит: Vertex Pharmaceuticals Inc

A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims. Additionally, the present invention relates to compounds of Structural Formula (I), which are useful as inhibitors of protein kinase.

Подробнее
Номер записи: 93
01-11-2012 дата публикации

Polycyclic ring-fused compound and organic thin film transistor utilizing same

Номер: US20120273770A1
Автор: Hiroaki Nakamura, Hirofumi Kondo, Masahiro Kawamura, Masatoshi Saito, Misa Sunagawa, Naoki Kurihara
Принадлежит: Idemitsu Kosan Co Ltd

A compound for an organic thin film transistor represented by the following formula (1):

Подробнее
Номер записи: 94
08-11-2012 дата публикации

Imidazopyridazinecarbonitriles useful as kinase inhibitors

Номер: US20120283241A1
Автор: Andrew James Nation, Ashvinikumar V. Gavai, Brian E. Fink, Libing Chen, Liqi He, Litai H. Zhang, Soong-Hoon Kim, Yufen Zhao
Принадлежит: Bristol Myers Squibb Co

The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) imidazopyridazines inhibit protein kinase activity thereby making them useful as anticancer agents.

Подробнее
Номер записи: 95
15-11-2012 дата публикации

Modified colored pigments

Номер: US20120285347A1
Автор: Elizabeth G. Burns, James A. Belmont
Принадлежит: Cabot Corp

The present invention relates to a modified colored pigment comprising a colored pigment having an attached organic group. The organic group is attached to the colored pigment via at least one carbon atom of a C—C single bond or double bond, wherein the C—C single bond or double bond is not a component of an aromatic system. The organic group further comprises at least one activating group on at least one carbon atom of the C—C single bond or double bond. A method of preparing a modified colored pigment is also disclosed, as are aqueous and non-aqueous dispersions, e.g., including ink jet inks, comprising the modified colored pigments.

Подробнее
Номер записи: 96
15-11-2012 дата публикации

Kinase inhibitors useful for the treatment of proliferative diseases

Номер: US20120289540A1
Автор: Daniel L. Flynn, Michael D. Kaufman, Peter A. Petillo, William C. Patt
Принадлежит: Deciphera Pharmaceuticals LLC

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

Подробнее
Номер записи: 97
15-11-2012 дата публикации

Nicotinic Acetylcholine Receptor Sub-Type Selective Amides of Diazabicycloalkanes

Номер: US20120289572A1
Автор: Anatoly Mazurov, Lan Miao, Yun-De Xiao
Принадлежит: Targacept Inc

Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

Подробнее
Номер записи: 98
22-11-2012 дата публикации

Inhibitors of bruton's tyrosine kinase

Номер: US20120295885A1
Автор: Francisco Javier Lopez-Tapia, Jutta Wanner, Kshitij C. Thakkar, Rama K. Kondru, Roland Joseph Billedeau, Sung-Sau So, Timothy D. Owens, Yan Lou, Yimin Qian
Принадлежит: Francisco Javier Lopez-Tapia, Jutta Wanner, Kondru Rama K, Owens Timothy D, Roland Joseph Billedeau, Sung-Sau So, Thakkar Kshitij C, Yan Lou, Yimin Qian

This application discloses compounds according to generic Formula I: wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.

Подробнее
Номер записи: 99
22-11-2012 дата публикации

Gabaergic receptor subtype selective ligands and their uses

Номер: US20120295892A1
Автор: Hiteshkumar D. Jain, James M. Cook, Jie Yang, Michael Ming-Jin Poe, Ojas A. Namjoshi, Sundari K. Rallipalli, Terry S. Clayton, Yun Teng Johnson, Zhi-Jian Wang
Принадлежит: UWM Research Foundation Inc

Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.

Подробнее
Номер записи: 100