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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 63129. Отображено 100.
05-01-2012 дата публикации

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

Номер: US20120003229A1
Принадлежит: Individual

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

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05-01-2012 дата публикации

Triheterocyclic Compounds and Compositions Thereof

Номер: US20120004224A1
Принадлежит: Gemin X Pharmaceuticals Canada Inc

The present invention relates to novel Triheterocyclic Compounds, compositions comprising a Triheterocyclic Compound, and methods useful for treating or preventing cancer or a neoplastic disorder comprising administering a Triheterocyclic Compound. The compounds, compositions, and methods of the invention are also useful for inhibiting the growth of a cancer cell or neoplastic cell, treating or preventing a viral infection, or inhibiting the replication and/or infectivity of a virus.

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05-01-2012 дата публикации

Method of treatment or prophylaxis

Номер: US20120004259A1
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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12-01-2012 дата публикации

Tetrazine monomers and copolymers for use in organic electronic devices

Номер: US20120007026A1
Принадлежит: NATIONAL RESEARCH COUNCIL OF CANADA

Copolymers of formula (I): where each A is S, Se or C═C; each x is an integer from 1 to 4; each R1 is independently H, F, CN or a C 1 -C 20 linear or branched aliphatic group; Ar is one or more substituted or unsubstituted aromatic units; and, n is an integer 5 or greater, can be formed into films or membranes that are useful as active layers in organic electronic device, such as PV solar cells, providing high power conversion efficiencies and good thermal stability. Such copolymers may be synthesized from monomers of formula (II): by Stille or Suzuki coupling reactions. Such monomers may be synthesized by a variation of the Pinner synthesis.

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12-01-2012 дата публикации

Broad spectrum benzothiophene-nitrothiazolide and other antimicrobials

Номер: US20120010187A1

The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.

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12-01-2012 дата публикации

Anthranilic diamide derivatives having cyclic side-chains

Номер: US20120010249A1
Принадлежит: Bayer CropScience AG

The present invention relates to novel anthranilic diamide derivatives of the general formula (I) in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.

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19-01-2012 дата публикации

Pharmaceutical composition for external use

Номер: US20120015997A1
Принадлежит: Nihon Nohyaku Co Ltd, Pola Pharma Inc

Provided is a pharmaceutical composition for external use, including: (i) a compound represented by structural formula (2) and/or a salt thereof; and (ii) N-methyl-2-pyrrolidone.

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26-01-2012 дата публикации

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

Номер: US20120020915A1

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

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26-01-2012 дата публикации

Triazole derivatives for treatment of alzheimer's disease

Номер: US20120022044A1
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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02-02-2012 дата публикации

6 Substituted 2, 3,4,5 Tetrahydro-1H-Benzo[d]Azepines as 5-HT2c Receptor Agonist

Номер: US20120028961A1
Принадлежит: Eli Lilly and Co

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HT 2C receptor agonists for the treatment of 5-HT 2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where: R 6 is —S—R 14 ; and other substituents are as defined in the specification.

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09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

Номер: US20120032158A1
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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09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Принадлежит: Sarcode Bioscience Inc

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

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23-02-2012 дата публикации

Developers and method of coloring lithographic printing members

Номер: US20120045720A1
Принадлежит: Individual

A color contrast image in imaged lithographic printing precursors can be obtained by contacting the imaged precursor with a coloration solution containing a colorless form of a photochromic compound. Residual amounts of this compound attached to the oleophilic surface of the imaged precursor can be changed to its colored form when exposed to UV light. The coloration solution can be an alkaline or acidic developer or an alkaline or acidic solution used separately after development. The coloration solution can also be a gum solution.

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

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

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23-02-2012 дата публикации

3-substituted propanamine compounds

Номер: US20120046312A1
Принадлежит: SK Biopharmaceuticals Co Ltd

Racemic or enantiomerically enriched 3-substituted propanamine compounds represented by the following structural formula (I): or a pharmaceutically acceptable salt thereof are disclosed. Pharmaceutical compositions containing the subject compounds are also disclosed. The subject compounds are useful for the treatment of diseases of the central nervous system, such as depression, anxiety and pain disorders.

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01-03-2012 дата публикации

Azafluorene derivative and organic light-emitting device using the derivative

Номер: US20120049176A1
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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08-03-2012 дата публикации

Di-azetidinyl diamide as monoacylglycerol lipase inhibitors

Номер: US20120058986A1
Принадлежит: Janssen Pharmaceutica NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.

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08-03-2012 дата публикации

Carbazole and carboline kinase inhibitors

Номер: US20120058988A1
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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15-03-2012 дата публикации

Pyridinylcarboxylic Acid Derivatives as Fungicides

Номер: US20120065197A1
Принадлежит: Bayer CropScience AG

Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y 1 , Y 2 , Y 3 , L 1 , L 2 , R G , and R 1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

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22-03-2012 дата публикации

Estrogen receptor modulators and uses thereof

Номер: US20120071535A1
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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29-03-2012 дата публикации

Bicyclic compounds and use as antidiabetics

Номер: US20120077812A1
Принадлежит: Individual

The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds.

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05-04-2012 дата публикации

Photoelectric conversion element, production method thereof, photosensor, imaging device and their driving method

Номер: US20120080585A1
Принадлежит: Fujifilm Corp

To provide a photoelectric conversion element capable of functioning as a photoelectric conversion element when a compound having a specific structure is applied to the photoelectric conversion element, causing the element to exhibit a low dark current, and reducing the range of increase in the dark current even when the element is heat-treated, and an imaging device equipped with such a photoelectric conversion element. A photoelectric conversion element having a photoelectric conversion film which is sandwiched between a transparent electrically conductive film and an electrically conductive film and contains a photoelectric conversion layer and an electron blocking layer, wherein the electron blocking layer contains a compound having, as a substituent, a substituted amino group containing three or more ring structures.

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12-04-2012 дата публикации

Five-membered heterocycles useful as serine protease inhibitors

Номер: US20120088758A1
Принадлежит: Bristol Myers Squibb Co

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

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12-04-2012 дата публикации

Compounds for enzyme inhibition

Номер: US20120088762A1
Принадлежит: Onyx Therapeutics Inc

One aspect of the invention relates to inhibitors that preferentially inhibit immunoproteasome activity over constitutive proteasome activity. In certain embodiments, the invention relates to the treatment of immune related diseases, comprising administering a compound of the invention. In certain embodiments, the invention relates to the treatment of cancer, comprising administering a compound of the invention.

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12-04-2012 дата публикации

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

Номер: US20120088797A1
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.

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19-04-2012 дата публикации

Novel Heterocyclic Compounds as Pesticides

Номер: US20120094837A1
Принадлежит: Bayer CropScience AG

The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects.

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26-04-2012 дата публикации

Novel c-aryl glucoside sglt2 inhibitors and pharmaceutical compositions comprising same

Номер: US20120101051A1
Принадлежит: Green Cross Corp Korea

A novel C-aryl glucoside compound, or a pharmaceutically acceptable salt or a prodrug thereof having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney; and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly, diabetes, are provided.

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03-05-2012 дата публикации

Novel microbiocides

Номер: US20120108645A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

Compounds of formula (I) in which the substituents are as defined in claim 1, are suitable for use as microbiocides.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
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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10-05-2012 дата публикации

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

Номер: US20120115915A1
Принадлежит: Harvard College

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

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17-05-2012 дата публикации

Pyruvate kinase m2 modulators, therapeutic compositions and related methods of use

Номер: US20120122885A1
Принадлежит: Agios Pharmaceuticals Inc

Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

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24-05-2012 дата публикации

Inhibitors of syk and jak protein kinases

Номер: US20120130073A1
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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31-05-2012 дата публикации

Cyclic triazo sodium channel blockers

Номер: US20120135993A1
Принадлежит: University of Greenwich

The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ═NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.

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31-05-2012 дата публикации

Method for preparing 5-chloro-n-(methyl)thiophen-2-carboxamide derivative and intermediate used therein

Номер: US20120136149A1

Disclosed are: a method for preparing a 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin- 1 -yl)phenyl]-1,3-oxazolidin-5-yl}-methyl)thiophene-2-carboxamide derivative, which is a inhibitor of blood coagulation factor Xa, in a high purity and yield; and a novel intermedicate used therein.

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07-06-2012 дата публикации

Light-emitting device material and light-emitting device

Номер: US20120138907A1
Принадлежит: TORAY INDUSTRIES INC

Embodiments provide a light emitting device material characterized by containing an anthracene compound represented by the following general formula. where R 19 to R 37 are a hydrogen atom, alkyl group, cycloalkyl group, heterocyclic group or the like; n is 1 or 2; and A is a heteroarylene group or arylene group. Any one of the R 19 to R 27 and any one of the R 28 to R 37 are used for linking with A. The present teachings allow a light emitting device having high luminous efficiency and excellent durability.

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07-06-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120142732A1
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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21-06-2012 дата публикации

Leaving substituent-containing compound, organic semiconductor material, organic semiconductor film containing the material, organic electronic device containing the film, method for producing film-like product, pi-electron conjugated compound and method for producing the pi-electron conjugated compound

Номер: US20120153271A1
Принадлежит: Ricoh Co Ltd

A leaving substituent-containing compound including a partial structure represented by the following General Formula (I): where a pair of X 1 and X 2 or a pair of Y 1 and Y 2 each represent a hydrogen atom; the other pair each represent a group selected from the group consisting of a halogen atom and a substituted or unsubstituted acyloxy group having one or more carbon atoms; a pair of the acyloxy groups represented by the pair of X 1 and X 2 or the pair of Y 1 and Y 2 may be identical or different, or may be bonded together to form a ring; R 1 to R 4 each represent a hydrogen atom or a substituent; and Q 1 and Q 2 each represent a hydrogen atom, a halogen atom or a monovalent organic group, and may be bonded together to form a ring.

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21-06-2012 дата публикации

Anhydrate Forms Of A Pyridine Derivative

Номер: US20120157450A1

The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.

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28-06-2012 дата публикации

Novel azabicyclohexanes

Номер: US20120165320A1
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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05-07-2012 дата публикации

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

Номер: US20120172599A1
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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12-07-2012 дата публикации

Styryl-triazine derivatives and their therapeutical applications

Номер: US20120178758A1
Принадлежит: California Capital Equity LLC

The invention provides Styryl-Triazine derivatives, and further provides methods of using these compounds to modulate protein kinases and to treat protein kinase mediated diseases.

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19-07-2012 дата публикации

Substituted nicotinamides as kcnq2/3 modulators

Номер: US20120184550A1
Принадлежит: GRUENENTHAL GmbH

Substituted nicotinamides, processes for their preparation, medicaments comprising these compounds and methods of using these compounds to treat pain, epilepsy, urinary incontinence, anxiety, dependency, mania, bipolar disorders, migraine, cognitive diseases, and/or dystonia-associated dyskinesias.

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26-07-2012 дата публикации

Treatment or prophylaxis of proliferative conditions

Номер: US20120190639A1
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.

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02-08-2012 дата публикации

IAP BIR domain binding compounds

Номер: US20120195915A1
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.

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02-08-2012 дата публикации

Sulfoximines as kinase inhibitors

Номер: US20120196902A1
Принадлежит: Allergan Inc

The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

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09-08-2012 дата публикации

NP-1 Antagonists and Their Therapeutic Use

Номер: US20120201749A1
Принадлежит: Ark Therapeutics Ltd

Compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein: W is arylene, heteroarylene or formula (a) each L is independently alkylene, alkenylene, alkynylene, a direct bond, arylene, cycloalkylene, alkylene-arylene, alkylene-C═O or —C═O; each X is independently an N-containing heteroarylene, N-containing cycloalkylene or NR; Y is N-containing heteroaryl, N-containing cycloalkyl, NR 2 , OR 1 , CN or CO 2 R; Z 1 is formula (b); are useful in therapy, particularly in the therapy of neurodegeneration and cancer.

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09-08-2012 дата публикации

Compounds for the treatment of hepatitis c

Номер: US20120201783A1
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.

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09-08-2012 дата публикации

Substituted pyridones as inhibitors of poly(adp-ribose) polymerase (parp)

Номер: US20120202795A1
Принадлежит: Aventis Pharmaceuticals Inc

The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R 1 , R 2 , R 3 and R 4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.

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09-08-2012 дата публикации

Dual small molecule inhibitors of cancer and angiogenesis

Номер: US20120202800A1
Автор: Milton L. Brown

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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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

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

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09-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120202812A1
Принадлежит: Millennium Pharmaceuticals Inc

This invention provides compounds of formula I: wherein R 1 , R 2 , CY, Y 1 , Y 2 , X 1 , X 2 , and X 3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.

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09-08-2012 дата публикации

Processes relating to the alkylation of pyrazoles

Номер: US20120203009A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

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

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16-08-2012 дата публикации

Novel organic electroluminescent compounds and organic electroluminescent device using the same

Номер: US20120206037A1

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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16-08-2012 дата публикации

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

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

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

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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
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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23-08-2012 дата публикации

Viral polymerase inhibitors

Номер: US20120214783A1
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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23-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120214794A1
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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30-08-2012 дата публикации

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

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

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

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30-08-2012 дата публикации

Novel spiropiperidine compounds

Номер: US20120220616A1
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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06-09-2012 дата публикации

Mst1 kinase inhibitors and methods of their use

Номер: US20120225857A1
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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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
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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13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
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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13-09-2012 дата публикации

Use of Indole Derivatives as Nurr-1 Activators for the Application Thereof as a Medicament for the Treatment of Parkinson's Disease

Номер: US20120232070A1
Принадлежит: Laboratories Fournier SAS

Compounds derived from indole, notably useful in therapeutics, selected from: i) the compounds of formula: and ii) the pharmaceutically acceptable salts of the compounds of formula (I); in which R1, R2, R3, R4, R5, R6, R8, R9 and Cy have defined meanings, and the use of such compounds in pharmaceuticals for the treatment of neurodegenerative diseases, particularly Parkinson's disease.

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13-09-2012 дата публикации

Methods of treating emesis using growth hormone secretagogues

Номер: US20120232113A1
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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27-09-2012 дата публикации

Light-emitting element

Номер: US20120242219A1
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A light-emitting element having high external quantum efficiency is provided. A light-emitting element having low drive voltage is provided. Provided is a light-emitting element which includes a light-emitting layer containing a phosphorescent compound, a first organic compound, and a second organic compound between a pair of electrodes. A combination of the first organic compound and the second organic compound forms an exciplex (excited complex). An emission spectrum of the exciplex overlaps with an absorption band located on the longest wavelength side of an absorption spectrum of the phosphorescent compound. A peak wavelength of the emission spectrum of the exciplex is longer than or equal to a peak wavelength of the absorption band located on the longest wavelength side of the absorption spectrum of the phosphorescent compound.

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11-10-2012 дата публикации

Dual-acting pyrazole antihypertensive agents

Номер: US20120259113A1
Принадлежит: Theravance Inc

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

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18-10-2012 дата публикации

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

Номер: US20120264736A1
Принадлежит: Schering Corp

This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

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25-10-2012 дата публикации

Ion channel modulators and methods of use

Номер: US20120270318A1
Принадлежит: Vertex Pharmaceuticals Inc

In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels and/or calcium channels.

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25-10-2012 дата публикации

Adamantyl diamide derivatives and uses of same

Номер: US20120270873A1
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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01-11-2012 дата публикации

Aromatic heterocyclic derivative and organic electroluminescence device using the same

Номер: US20120273766A1
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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01-11-2012 дата публикации

Novel heterocyclic acrylamides and their use as pharmaceuticals

Номер: US20120277207A1
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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08-11-2012 дата публикации

Use of rylene derivatives as photosensitizers in solar cells

Номер: US20120283432A1

Use of rylene derivatives I with the following definition of the variables: X together both —COOM; Y a radical -L-NR 1 R 2   (y1) -L-Z—R 3   (y2) the other radical hydrogen; together both hydrogen; R is optionally substituted (het)aryloxy, (het)arylthio; P is —NR 1 R 2 ; B is alkylene; optionally substituted phenylene; combinations thereof; A is —COOM; —SO 3 M; —PO 3 M 2 ; D is optionally substituted phenylene, naphthylene, pyridylene; M is hydrogen; alkali metal cation; [NR 5 ] 4 + ; L is a chemical bond; optionally indirectly bonded, optionally substituted (het)arylene radical; R 1 , R 2 are optionally substituted (cyclo)alkyl, (het)aryl; together optionally substituted ring comprising the nitrogen atom; Z is —O—; —S—; R 3 is optionally substituted alkyl, (het)aryl; R′ is hydrogen; optionally substituted (cyclo)alkyl, (het)aryl; R 5 is hydrogen; optionally substituted alkyl (het)aryl; m is 0, 1, 2; n, p m=0: 0, 2, 4 where: n+p=2, 4, if appropriate 0; m=1: 0, 2, 4 where: n+p=0, 2, 4; m=2: 0, 4, 6 where: n+p=0, 4, 6, or of mixtures thereof as photosensitizers in solar cells.

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15-11-2012 дата публикации

Novel compounds with high therapeutic index

Номер: US20120289471A1
Автор: V. Ravi Chandran
Принадлежит: Signature R&D Holdings LLC

The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

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22-11-2012 дата публикации

Fredericamycin derivatives

Номер: US20120295856A1
Автор: Ulrich Abel, Werner Simon
Принадлежит: ZENTOPHARM GmbH

The invention relates to novel fredericamycin derivatives, to drugs containing said derivatives or the salts thereof, and to the use of the fredericamycin derivatives for treating diseases, especially cancer diseases.

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22-11-2012 дата публикации

Chromone Inhibitors of S-Nitrosoglutathione Reductase

Номер: US20120295966A1
Принадлежит: N30 Pharmaceuticals Inc

The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.

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29-11-2012 дата публикации

Thiophene analogues for the treatment or prevention of flavivirus infections

Номер: US20120301430A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R 1 , X, Y, and Z are as defined herein, are useful for treating flaviviridae viral infections.

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29-11-2012 дата публикации

Novel sulfamides exhibiting neuroprotective action and methods for use thereof

Номер: US20120302546A1

Pharmaceutical compositions of the invention include sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, and any neurodegenerative disease involving glutamate toxicity.

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20-12-2012 дата публикации

Biarylamide inhibitors of leukotriene production

Номер: US20120322795A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R 1a , R 1b , R 2 , R 3 , R 4a and R 4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

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20-12-2012 дата публикации

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Принадлежит: PFIZER INC

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

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27-12-2012 дата публикации

Inhibitors of hepatitis c virus ns5b polymerase

Номер: US20120328569A1
Принадлежит: Individual

Disclosed are compounds of formula (I) that are used as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

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27-12-2012 дата публикации

Cycloalkyl-fused tetrahydroquinolines as crth2 receptor modulators

Номер: US20120329743A1
Принадлежит: Individual

The invention provides certain cycloalkyl-fused tetrahydroquinolines of the Formula (I), and their pharmaceutically acceptable salts and esters, wherein R 1 , R 2 , R 7 , R 8 , R 8a , E, Y, Z, n, u, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH 2 function.

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03-01-2013 дата публикации

Cyclic amine bace-1 inhibitors having a benzamide substituent

Номер: US20130004518A1
Принадлежит: Merck Sharp and Dohme LLC

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is R is —C(O)—N(R 27 )(R 28 ) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a β-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

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03-01-2013 дата публикации

Metalloenzyme inhibitor compounds

Номер: US20130005719A1
Принадлежит: Viamet Pharmaceuticals Inc

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

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24-01-2013 дата публикации

Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disorders as agonists of g-protein coupled receptor 43 (gpr43)

Номер: US20130023539A1
Принадлежит: Euroscreen SA

The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.

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24-01-2013 дата публикации

Catalysts based on heterocyclic-8-anilinoquinoline ligands

Номер: US20130023635A1
Принадлежит: EQUISTAR CHEMICALS LP

A catalyst system useful for polymerizing olefins is disclosed. The catalyst system comprises an activator and a Group 4 metal complex. The complex incorporates a dianionic, tridentate heterocyclic-8-anilinoquinoline ligand. In one aspect, a supported catalyst system is prepared by first combining a boron compound having Lewis acidity with excess alumoxane to produce an activator mixture, followed by combining the activator mixture with a support and the dianionic, tridentate Group 4 metal complex. The Group 4 metal complexes are easy to synthesize, support, and activate, and they enable facile production of high-molecular-weight polyolefins.

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31-01-2013 дата публикации

Compounds, compositions, and methods for controlling biofilms

Номер: US20130029981A1
Принадлежит: Katholieke Universiteit Leuven

The invention relates to substituted 2-aminoimidazoles and their imidazo[1,2- a ]pyrimidinium salts precursors being active against biofilm formation. The invention also relates to imidazo[1,2- a ]pyrimidinium salts bearing an azidoalkyl substituent, and to substituted 2-aminoimidazoles wherein the amino group bears a terminal heterocyclic group such as a triazolyl group which are formed through azide-alkyne Huisgen cycloaddition starting from said imidazo[1,2- a ]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to a class of N-(azidoalkyl)pyrimidin-2-amines useful as starting materials for the synthesis of said imidazo[1,2- a ]pyrimidinium salts bearing an azidoalkyl substituent. The invention also relates to antimicrobial compositions that include a microbial biofilm formation inhibiting amount of such substituted 2-aminoimidazoles or imidazo[1,2- a ]pyrimidinium salts in combination with excipients. Methods for inhibiting or controlling microbial biofilm formation in a plant, a body part of a human or an animal, or a surface with which a human or an animal may come into contact are also disclosed.

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31-01-2013 дата публикации

Novel Compounds

Номер: US20130030031A1
Принадлежит: Glaxo Group Ltd

Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.

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14-02-2013 дата публикации

Novel benzodioxole piperazine compounds

Номер: US20130040948A1
Принадлежит: Hoffmann La Roche Inc

The present invention is concerned with novel dual modulators of the 5-HT 2A and D 3 receptors of formula (I) wherein n, Y, R 1 , R 2 , R 3 , and R 4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.

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14-02-2013 дата публикации

Multisubstituted aromatic compounds as inhibitors of thrombin

Номер: US20130040950A1
Принадлежит: Verseon Corp

There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.

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21-02-2013 дата публикации

Aromatic monomers deriving from glycerol units, process for their preparation and use thereof for the preparation of water-soluble conjugated polymers

Номер: US20130046072A1
Принадлежит: Eni Spa

Monomers having formula (I) and process for their synthesis which comprises the etherification reaction of a halogen-derivative (Z═Cl, Br, I) having formula (III) with the hydroxyl group of the glycerol derivative (IV), according to the following scheme:(Formula III, IV & I) (III) (IV) (I)

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28-02-2013 дата публикации

Compound for electroluminescent device and organic electroluminescent devices using the same

Номер: US20130048956A1
Принадлежит: E Ray Optoelectronics Technology Co Ltd

The present invention provides a compound of formula (I) for an organic electroluminescent device: wherein X 1 , X 2 , X 3 , Y, Ar 1 , Ar 2 , Ar 3 , Ar 4 , Ar 5 , Ar 6 , and Ar 7 are as defined in the description.

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07-03-2013 дата публикации

Maleimide-based compound, and tautomer or stereoisomer thereof, dye for photoelectric conversion, and semiconductor electrode, photoelectric conversion element and photoelectrochemical cell using the same

Номер: US20130056690A1
Принадлежит: NEC Corp

It is an object to provide a maleimide-based compound having excellent photoelectric conversion characteristics, and a tautomer or a stereoisomer thereof, a dye for photoelectric conversion, a semiconductor electrode, a photoelectric conversion element, and a photoelectrochemical cell. In order to accomplish the above-described objects, a dye for photoelectric conversion including at least one compound represented by the following general formula (1) is provided. (In the formula (1), R 1 represents a direct bond, or a substituted or unsubstituted alkylene group. X represents an acidic group. D represents an organic group containing an electron-donating substituent. Z represents a linking group that has at least one hydrocarbon group selected from aromatic rings or heterocyclic rings).

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07-03-2013 дата публикации

Methods of identifying modulators of gpr17

Номер: US20130059899A1

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.

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07-03-2013 дата публикации

Synthesis of substituted pyrazoline carboxamidine derivatives

Номер: US20130060041A1

This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.

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14-03-2013 дата публикации

BIPHOTONIC PHOTOSENSITIZERS, NANOPARTICLES CONTAINING THE SAME AND THEIR USE AS DRUGS

Номер: US20130065849A1
Принадлежит:

The invention relates to compounds of formula (I) 5. Silica nanoparticle claim 1 , comprising at least one photosensitizer constituted by at least a compound according to claim 1 , covalently linked to said nanoparticle claim 1 , and possibly comprising shielding moieties grafted on the surface of said nanoparticle claim 1 , and possibly comprising biotargeting moieties grafted on the surface of said nanoparticle.6. Silica nanoparticle composition claim 1 , constituted by at least one silica nanoparticle comprising at least one photosensitizer constituted by at least a compound according to claim 1 , covalently linked to said nanoparticle claim 1 , and possibly comprising shielding moieties grafted on the surface of said nanoparticle claim 1 , and possibly comprising biotargeting moieties grafted on the surface of said nanoparticle.7. Silica nanoparticle composition according to claim 6 , wherein said silica nanoparticle have an organized porosity.8. Silica nanoparticle composition according to claim 6 , wherein said silica nanoparticle is mesoporous.9. Silica nanoparticle composition according to claim 6 , comprising biotargeting moieties grafted on the surface of said nanoparticle which specifically target neoplastic tissues.10. Silica nanoparticle composition according to claim 6 , comprising shielding moieties grafted on the surface of said nanoparticle claim 6 , and which specifically absorb radiations in the 190 to 600 nm range claim 6 , particularly in the 250 to 500 nm wavelengths.11. Silica nanoparticle composition according to claim 6 , wherein the concentration of said photosensitizer claim 6 , with respect to the total mass of the nanoparticle comprising said photosensitizer claim 6 , ranges from about 0.1 micromole per gram to about 100 micromoles per gram claim 6 , particularly ranges from about 0.5 micromoles per gram to about 30 micromoles per gram claim 6 , particularly ranges from about 1 micromoles per gram to about 10 micromoles per gram.12. ...

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14-03-2013 дата публикации

VLA-4 inhibitory drug

Номер: US20130065882A1
Принадлежит: Individual

This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH 2 ; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A 1 represents a nitrogen atom or C—R 3d wherein R 3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R 1 represents H or a C1-8 alkyl group; R 2 represents H, a halogen, a C1-8 alkoxy

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14-03-2013 дата публикации

SUBSTITUTED N-HETEROARYL BIPYRROLIDINE CARBOXAMIDES, PREPARATION AND THERAPEUTIC USE THEREOF

Номер: US20130065923A1
Принадлежит: SANOFI

The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). 2. The compound according to claim 1 , whereinm and p are 1;X is CO;{'sub': 1', '3, 'Ris CH;'}{'sub': 2', '3, 'Ris CH; and'}{'sub': 3', '1', '4', '3, 'Ris unsubstituted or substituted naphthyl, phenyl, benzyl, thiophenyl, isoxazolyl, cyclopropyl, cyclohexyl, tetrahydropyranyl or piperidinyl, wherein the substituents are selected from the group consisting of halogen, (C-C)alkyl and CHCO; and'}{'sub': '4', 'Ris H,'}or a salt thereof or an enantiomer or a diastereomer thereof.3. The compound according to claim 1 , whereinm and p are 1;{'sub': '2', 'X is SO;'}{'sub': 1', '3, 'Ris CH;'}{'sub': 2', '3, 'Ris CH; and'}{'sub': 3', '1', '4', '3, 'Ris unsubstituted or substituted phenyl, cyclopropyl or cyclohexyl, wherein the substituents are selected from the group consisting of halogen, (C-C)alkyl and CHCO; and'}{'sub': '4', 'Ris H;'}or a salt thereof or an enantiomer or a diastereomer thereof.4. The compound of selected from the group consisting of:tetrahydro-pyran-4-carboxylic acid [2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-amide;tetrahydro-pyran-4-carboxylic acid [5-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-2-yl]-amide;naphthalene-1-carboxylic acid [2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-amide;N-[2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-2-phenyl-acetamide;cyclohexanesulfonic acid [2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-amide;3,4-difluoro-N-[2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-benzenesulfonamide;N-[2-methyl-6-((2S,3′S)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-benzamide;1-acetyl-piperidine-4-carboxylic acid [2-methyl-6-((2S,3′R)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]-amide;5-fluoro-2-methyl-N-[2-methyl-6-((2S,3′R)-2-methyl-[1,3′]bipyrrolidinyl-1′-yl)-pyridin-3-yl]- ...

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14-03-2013 дата публикации

N-piperidinyl acetamide derivatives as calcium channel blockers

Номер: US20130065926A1
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).

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21-03-2013 дата публикации

ORGANIC NANOFIBER STRUCTURE BASED ON SELF-ASSEMBLED ORGANOGEL, ORGANIC NANOFIBER TRANSISTOR USING THE SAME, AND METHOD OF MANUFACTURING THE ORGANIC NANOFIBER TRANSISTOR

Номер: US20130069040A1
Принадлежит:

An organic nanofiber including a gelled organic semiconductor compound. Also disclosed is an organic semiconductor transistor and a method of manufacturing an organic semiconductor transistor. 1. An organic semiconductor transistor comprising:a substrate;a gate electrode;a source electrode and a drain electrode, each of which are insulated from the gate electrode;an organic semiconductor layer, which is insulated from the gate electrode and electrically connected to the source and drain electrodes; andan insulating layer, which insulates the gate electrode from the source and drain electrodes and the organic semiconductor layer,wherein an organic nanofiber comprising a gelated organic semiconductor compound is disposed on the organic semiconductor layer.2. The organic semiconductor transistor of claim 1 , formed by self-assembly of the gelated organic semiconductor compound in an organic solvent.3. The organic semiconductor transistor of claim 1 , wherein the organic semiconductor layer is formed using bottom contact geometry and the channel layer is formed on the source and drain electrodes claim 1 , or wherein the organic semiconductor layer is formed using top contact geometry and the source and drain electrodes are formed on the channel layer.6. The organic semiconductor transistor of claim 5 , wherein the organic solvent comprises dimethyl sulfoxide. This application is a divisional of U.S. application Ser. No. 12/499,310, filed on Jul. 8, 2009, which claims priority to Korean Patent Application No. 10-2008-0066471, filed on Jul. 9, 2008, and all the benefits accruing therefrom under 35 U.S.C. §119, the contents of which in their entirety are incorporated herein by reference.The patent or application file contains at least one drawing executed in color. Copies of this patent or patent application publication with color drawings will be provided by the Office upon request and payment of the necessary fee.BACKGROUND1. FieldOne or more embodiments relate to an ...

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21-03-2013 дата публикации

PROLYL HYDROXYLASE INHIBITORS

Номер: US20130072487A1
Принадлежит: GlaxoSmithKline LLC

The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) 2. The method according to wherein:X is O;Y is O;{'sup': 1', '4, 'sub': 1-', '10', '2-', '10', '2-', '10', '3', '8', '3', '8', '1-', '10', '5', '8', '5', '8', '1-', '10', '3', '8', '3', '8', '1-', '10', '1-', '10', '1-', '10, 'Rand Rare each independently selected from the group consisting of hydrogen, CCalkyl, CCalkenyl, CCalkynyl, C-Ccycloalkyl, C-Ccycloalkyl-CCalkyl, C-Ccycloalkenyl, C-Ccycloalkenyl-CCalkyl, C-Cheterocycloalkyl, C-Cheterocycloalkyl-CCalkyl, aryl, aryl-CCalkyl, heteroaryl and heteroaryl-CCalkyl;'}{'sup': 2', '7', '8', '9, 'Ris —NRRor —OR;'}{'sup': '3', 'sub': 1-', '4, 'claim-text': [{'sup': 7', '8, 'sub': 1-', '10', '2-', '10', '2-', '10', '3', '8', '3', '8, 'where Rand Rare each independently selected from the group consisting of hydrogen, CCalkyl, CCalkenyl, CCalkynyl, C-Ccycloalkyl, C-Cheterocycloalkyl, aryl and heteroaryl, and'}, {'sup': '9', 'sub': 1-', '10', '3', '6, 'Ris H or a cation, or CCalkyl which is unsubstituted or substituted with one or more substituents independently selected from the group consisting of C-Ccycloalkyl, heterocycloalkyl, aryl and heteroaryl,'}, {'sup': 1', '2', '3', '4', '7', '8', '9', '10', '5', '6', '10', '10', '10', '10', '10', '5', '6', '5', '6', '5', '10', '5', '10', '5', '6', '5', '5', '6', '5', '6', '5', '10', '5', '6', '10, 'sub': 1', '6', '1', '6', '2', '2', '2', '2', '10', '2', '10', '3', '6', '3', '6', '1', '6', '1', '6', '1-', '10', '2-', '10', '2-', '10', '1', '4', '3', '6', '3', '6', '2', '1', '4', '3', '8', '3', '8', '6', '14', '1-', '10', '1-', '10, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'where any carbon or heteroatom of R, R, R, R, R, R, Ris unsubstituted or is substituted with one or more substituents independently selected from C-Calkyl, C-Chaloalkyl, halogen, —OR, —NRR, oxo, cyano, nitro, —C(O)R, —C(O)OR, —SR, —S(O)R, —S(O)R, —NRR, —CONRR, —N(R)C(O)R, —N(R)C(O)OR, —OC(O) ...

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