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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 28056. Отображено 100.
05-01-2012 дата публикации

Organic semiconductor material and organic thin-film transistor

Номер: US20120001162A1
Принадлежит: Kyushu Institute of Technology NUC

An organic thin-film transistor comprising a gate electrode, a gate insulator layer, an organic semiconductor layer, a source electrode and a drain electrode wherein the organic semiconductor layer consists of the organic semiconductor material having the structure represented by the general formula (1) shown below, and the organic semiconductor layer has crystallinity: wherein L represents a bivalent linker group having the structure consisting of one group or any combination of two or more groups selected from unsubstituted or fluorinated benzene residue, unsubstituted or fluorinated thiophene residue, unsubstituted or fluorinated thienothophene residue; R 1 represents carbonyl group, cyano group or C 1 -C 6 fluorinated alkyl group; R 2 represents halogen atom, cyano group, carbonyl group or acetyl group.

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05-01-2012 дата публикации

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

Номер: US20120003215A1
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.

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09-02-2012 дата публикации

Preparation and application of novel antibacterial and anticancer compounds and their derivatives

Номер: US20120035206A1
Принадлежит: Individual

Novel antibiotic and anticancer compounds of formula I, II, III, IV, derivatives, ostereoisomer, racemic and noracemic mixture of ostereoisomer, or the pharmaceutically acceptable salts or solvates of these compounds are disclosed. The preparation, pharmaceutical composition and biological activity of these compounds are disclosed.

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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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01-03-2012 дата публикации

Conjugated compound, and organic thin film and organic thin film element each comprising same

Номер: US20120049174A1

A conjugated compound having a group represented by formula (I) and/or formula (II). [In the formulas, Ar represents an optionally substituted trivalent aromatic hydrocarbon or optionally substituted trivalent heterocyclic group, and A represents hydrogen, a halogen atom or a monovalent group. When multiple A groups are present they may be the same or different, and at least one A represents an electron-withdrawing group. Ar′ represents an optionally substituted C6 or greater divalent aromatic hydrocarbon or optionally substituted C4 or greater divalent heterocyclic group, and R1 and R2 are the same or different and each represents hydrogen, a halogen atom or a monovalent group, while A′ represents hydrogen, a halogen atom or a monovalent group. When multiple A′ groups are present they may be the same or different, and at least one A′ represents an electron-withdrawing group.]

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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

Sulfonamide, sulfamate, and sulfamothioate derivatives

Номер: US20120077814A1
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.

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29-03-2012 дата публикации

Chemical compounds

Номер: US20120077828A1
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.

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10-05-2012 дата публикации

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

Номер: US20120112629A1
Принадлежит: Idemitsu Kosan Co Ltd

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

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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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17-05-2012 дата публикации

Aurora kinase modulators and method of use

Номер: US20120122847A1
Принадлежит: AMGEN INC

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

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24-05-2012 дата публикации

Thienopyrimidines for pharmaceutical compositions

Номер: US20120128686A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to novel pharmaceutical compositions comprising thienopyrimidine compounds. Moreover, the present invention relates to the use of the thienopyrimidine compounds of the invention for the production of pharmaceutical compositions for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.

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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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28-06-2012 дата публикации

Quinoline derivatives as pi3 kinase inhibitors

Номер: US20120165321A1
Принадлежит: GlaxoSmithKline LLC

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

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12-07-2012 дата публикации

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

Номер: US20120178736A1
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.

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19-07-2012 дата публикации

Organic Semiconductors

Номер: US20120184089A1
Принадлежит: Cambridge Display Technology Ltd

A semiconducting compound comprising the structure: where R1 to R4 independently comprise, but are not limited to, optionally substituted straight, branched or cyclic alkyl chains having 2 to 20 (e.g. 2 to 12) carbon atoms, alkoxy, amino, amido, silyl, alkyl, alkenyl, aryl or hetero aryl; where X1 and X2 independently comprise S, O, NR5 or SiR6R7 where R8 to R7 independently comprise C1 to C5 branched, straight or cyclic alkyl chains; and where Ar1 comprises a heterocyclic ring, and where n is an integer between 1 and 4.

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19-07-2012 дата публикации

Nitrogen-containing heterocyclic compound and salt thereof, and a fungicide for agricultural and horticultural use

Номер: US20120184732A1
Принадлежит: Nippon Soda Co Ltd

The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof, which is useful as an active ingredient of a fungicide for agricultural and horticultural use, having an assured effect and being safely usable.

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16-08-2012 дата публикации

Thieno- and furo-pyrimidine modulators of the histamine h4 receptor

Номер: US20120208793A1
Принадлежит: Individual

Thieno- and furo-pyrimidine compounds are described, which are useful as H 4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H 4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, such as inflammation.

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16-08-2012 дата публикации

Novel heterocyclic aromatic compound and polymer

Номер: US20120208978A1
Принадлежит: Nagase Chemtex Corp

An electrically conductive polymer obtained by oxidative polymerization of a heterocycle-containing aromatic compound as a monomer, wherein the heterocycle-containing aromatic compound is represented by the formula: A-B. In the above formula, A represents a substituted or unsubstituted thiophene ring group, or a substituted or unsubstituted pyrrole ring group; B represents a substituted or unsubstituted hydrocarbon aromatic ring group, a substituted or unsubstituted thiophene ring group, or a substituted or unsubstituted pyrrole ring group; the ring represented by A and the ring represented by B are directly linked; however, A and B represent structures that are different from each other. The compound can be produced by a coupling reaction using a hypervalent iodine reactant.

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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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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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13-09-2012 дата публикации

Organic compound and photovoltaic device comprising the same

Номер: US20120227802A1
Принадлежит: Cryscade Solar Ltd

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

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13-09-2012 дата публикации

Novel compounds and therapeutic use thereof for protein kinase inhibition

Номер: US20120232082A1
Автор: Zhanggui Wu
Принадлежит: Individual

Novel compound having the following formula: (I) wherein Y is N, O, or S. Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.

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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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08-11-2012 дата публикации

Irak inhibitors and uses thereof

Номер: US20120283238A1
Принадлежит: Nimbus Iris Inc

The present invention provides compounds, compositions thereof, and methods of using the same.

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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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15-11-2012 дата публикации

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

Номер: US20120289474A1
Принадлежит: NYCOMED GMBH

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

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06-12-2012 дата публикации

Semiconducting polymers

Номер: US20120305853A1
Принадлежит: Merck Patent GmBH

The invention relates to novel polymers containing repeating units based on benzodithiophene or derivatives thereof, monomers and methods for their preparation, their use as semiconductors in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers.

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20-12-2012 дата публикации

Electroactive materials

Номер: US20120319571A1
Автор: Hong Meng
Принадлежит: EI Du Pont de Nemours and Co

There is provided an electroactive material having Formula I wherein: Q is the same or different at each occurrence and can be O, S, Se, Te, NR, SO, SO 2 , or SiR 3 ; R is the same or different at each occurrence and can be hydrogen, alkyl, aryl, alkenyl, or alkynyl; R 1 through R 8 are the same or different and can be hydrogen, alkyl, aryl, halogen, hydroxyl, aryloxy, alkoxy, alkenyl, alkynyl, amino, alkylthio, phosphino, silyl, —COR, —COOR, —PO 3 R 2 , —OPO 3 R 2 , or CN.

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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

Dihydrothieno pyrimidines as akt protein kinase inhibitors

Номер: US20120329808A1
Принадлежит: Array Biopharma Inc

The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

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27-12-2012 дата публикации

Method for preparing polybiotinylated compounds

Номер: US20120330028A1
Автор: Xavier Lacoux
Принадлежит: Individual

The present invention relates to a novel method for preparing compounds having the formula (I), where X is biotin or Y being biotin or Z being biotin or V being biotin or It also relates to compounds having the formula (I) and their use in clinical and industrial diagnosis.

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10-01-2013 дата публикации

2,4,7-substituted thieno[3,2-d]pyrimidine compounds as protein kinase inhibitors

Номер: US20130012703A1

Disclosed are a 2,4,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,4,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.

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17-01-2013 дата публикации

Chemical compounds

Номер: US20130018038A1
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.

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14-02-2013 дата публикации

Electroluminescent materials comprising fluorene derivatives

Номер: US20130037752A1
Автор: Gene Carl Koch
Принадлежит: Lomox Ltd

OLED compounds of the general structure: B—S-A-S—B in which rod-like nuclei A includes a condensed aromatic ring structure in turn having fluorene ring structures condensed with at least one additional fluorene ring structures wherein the fluorene ring systems provided by the condensed aromatic structure are substituted at the 9-position, and in which the 9-positions of the fluorenes are not susceptible to oxidation.

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21-02-2013 дата публикации

Benzocyanine compounds

Номер: US20130045488A1
Принадлежит: Dyomics GmbH, Pierce Biotechnology Inc

Compounds useful as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.

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28-02-2013 дата публикации

THIENO[3,2-d]PYRIMIDINE DERIVATIVES HAVING INHIBITORY ACTIVITY ON PROTEIN KINASES

Номер: US20130053370A1

The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.

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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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14-03-2013 дата публикации

Compounds Having Semiconducting Properties and Related Compositions and Devices

Номер: US20130062598A1
Принадлежит: Individual

Disclosed are new compounds having semiconducting properties. Such compounds can be processed in solution-phase at a temperature of less than about 50° C. into thin film semiconductors that exhibit high carrier mobility and/or good current modulation characteristics.

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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-alkyl and n-acyl tetrahydro-isoquinoline derivatives, preparation and therapeutic use thereof

Номер: US20130065919A1
Автор: Ryan Hartung, Zhongli Gao
Принадлежит: SANOFI SA

The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). wherein R, R 1 , R 2 , X, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I) and intermediates therefor.

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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

COMPOUND COMPRISING A FIVE-MEMBERED HETERO RING, AN ORGANIC ELECTRICAL ELEMENT USING THE SAME AND A TERMINAL THEREOF

Номер: US20130069049A1
Принадлежит: DUKSAN HIGH METAL CO., LTD.

Disclosed are a compound comprising a five-membered hetero ring, an organic electrical element using the same and a terminal thereof. 2. The compound as claimed in claim 1 , wherein Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , and Rand Reach form a substituted or unsubstituted claim 1 , saturated or unsaturated ring together with an adjacent group.5. An organic electrical element comprising one or more organic material layers comprising the compound as claimed in .6. The organic electrical element as claimed in claim 5 , wherein the organic material layers are formed to comprise the compound by a soluble process.7. The organic electrical element as claimed in claim 5 , wherein the organic electrical element comprises an organic light emitting diode (OLED) having a structure in which a first electrode claim 5 , the one or more organic material layers claim 5 , and a second electrode are sequentially laminated.8. The organic electrical element as claimed in claim 7 , wherein the organic material layers comprise any one of a hole injection layer claim 7 , a hole transport layer claim 7 , a light emitting layer claim 7 , an electron transport layer claim 7 , and an electron injection layer.9. The organic electrical element as claimed in claim 7 , wherein the organic material layers comprise a hole injection layer claim 7 , and the compound is used as a hole transport material in the hole transport layer.10. A terminal comprising a display device claim 7 , which comprises the organic electrical element as claimed in claim 7 , and a control unit for driving the display device.11. The terminal as claimed in claim 10 , wherein the organic electrical element comprises any one of an organic light emitting diode (OLED) claim 10 , an organic solar cell claim 10 , an organic photo conductor (OPC) drum claim 10 , and an organic transistor (organic TFT). The present invention relates to a compound including a five-membered hetero ring, an organic electrical element using the ...

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21-03-2013 дата публикации

5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS

Номер: US20130071352A1
Принадлежит: IDENIX PHARMACEUTICALS, INC.

Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof. 6. The method of claim 1 , wherein Uis S.7. The method of claim 1 , wherein Wis S.8. The method of claim 1 , wherein Wis O.9. The method of claim 1 , wherein Wis N.10. The method of claim 1 , wherein U claim 1 , W claim 1 , Xand Xare C claim 1 , and Vand Vare each independently CR.17. The method of claim 1 , wherein u is 1.18. The method of claim 1 , wherein u is 2.26. The method of claim 1 , wherein Ris —C(O)R claim 1 , —C(O)CH(NRR)R claim 1 , —C(O)CH[N(C(O)R)R]R claim 1 , —C(O)CH[N(C(O)OR)R]R claim 1 , or —C(O)CH[N(C(O)NRR)R]R.27. The method of claim 26 , wherein Ris —C(O)CH[N(C(O)OR)R]R.28. The method of claim 1 , wherein Ris —C(O)R claim 1 , —C(O)CH(NRR)R claim 1 , —C(O)CH[N(C(O)R)R]R claim 1 , —C(O)CH[N(C(O)OR)R]R claim 1 , or —C(O)CH[N(C(O)NRR)R]R.29. The method of claim 28 , wherein Ris —C(O)CH[N(C(O)OR)R]R.30. The method of claim 3 , wherein each Ris independently hydrogen or —C(O)OR.31. The method of claim 1 , wherein each Ris independently hydrogen claim 1 , methyl claim 1 , isopropyl claim 1 , 2-methylpropyl claim 1 , 1-methylpropyl claim 1 , 2-methylthioethyl claim 1 , phenyl claim 1 , benzyl claim 1 , 3-indolylmethyl claim 1 , hydroxymethyl claim 1 , 1-hydroxyethyl claim 1 , sulfhydrylmethyl claim 1 , 4-hydroxybenzyl claim 1 , aminocarbonylmethyl claim 1 , 2-(aminocarbonyl)ethyl claim 1 , carboxymethyl claim 1 , 2-carboxyethyl claim 1 , 4-aminobutyl claim 1 , 3-guanidinopropyl claim 1 , or 5-imidazolylmethyl.32. The method of claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , or butyl.33. The method of claim 1 , wherein Ris hydrogen.34. The method of claim 1 , wherein Rand Rtogether with the C and N atoms to which they ...

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21-03-2013 дата публикации

LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS

Номер: US20130072449A1
Принадлежит: INTERMUNE, INC.

Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided. 5. The compound or pharmaceutically acceptable salt of claim 2 , wherein m=1 claim 2 , and wherein Ris hydrogen and Ris selected from the group consisting of optionally substituted phenyl claim 2 , imidazole claim 2 , pyridine claim 2 , thiazole claim 2 , and oxazole.6. The compound or pharmaceutically acceptable salt thereof of claim 2 , wherein m=1 claim 2 , and wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 2 , an optionally substituted oxetane claim 2 , an optionally substituted beta-lactam claim 2 , an optionally substituted tetrahydropyran claim 2 , an optionally substituted cyclopropyl claim 2 , an optionally substituted cyclobutyl claim 2 , an optionally substituted cyclopentyl claim 2 , or an optionally substituted cyclohexyl.711.-. (canceled)13. (canceled)15. (canceled)18. (canceled)20. (canceled)21. (canceled)22. (canceled)24. The compound or salt thereof of claim 1 , selected from compounds of Table 1 claim 1 , and pharmaceutically acceptable salts thereof.25. The compound or salt thereof of claim 1 , selected from compounds of Table 2 claim 1 , and pharmaceutically acceptable salts thereof.26. The compound or salt thereof of claim 1 , selected from compounds of Table 3 claim 1 , and pharmaceutically acceptable salts thereof.28. The compound or pharmaceutically acceptable salt thereof of claim 27 , wherein Rand Rare joined together with the atom to which they are attached to form an optionally substituted azetidine claim 27 , an optionally substituted oxetane claim 27 , an optionally substituted beta-lactam claim 27 , an optionally substituted tetrahydropyran claim 27 , an optionally ...

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21-03-2013 дата публикации

COMPOUNDS FOR TREATING PROTEIN FOLDING DISORDERS

Номер: US20130072473A1
Принадлежит:

The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis. 112-. (canceled)1427-. (canceled)28. The method of claim 13 , wherein Dis N(R) and wherein each Ris independently selected from the group consisting of hydrogen and optionally substituted C-Calkyl.2932-. (canceled)33. The method of claim 28 , wherein Gis an optionally substituted 5/6-membered fused heteroaryl.34. The method of claim 33 , wherein Gis benzothiazolyl claim 33 , benzoxazolyl claim 33 , benzimidazolyl claim 33 , benzothiophenyl claim 33 , and benzofuranyl claim 33 , each optionally substituted.3646-. (canceled)47. The method of claim 35 , wherein Gis an optionally substituted 5/6-membered fused heteroaryl.48. The method of claim 47 , wherein Gis benzothiazolyl claim 47 , benzoxazolyl claim 47 , benzimidazolyl claim 47 , benzothiophenyl claim 47 , and benzofuranyl claim 47 , each optionally substituted.5065-. (canceled)70. The method of claim 13 , wherein the condition is associated with a dysfunction in the proteostasis of a protein selected from the group consisting of hexosamine A claim 13 , cystic fibrosis transmembrane conductance regulator claim 13 , aspartylglucsaminidase claim 13 , a-galactosidase A claim 13 , cysteine transporter claim 13 , acid ceremidase claim 13 , acid α-L-fucosidase claim 13 , protective protein claim 13 , cathepsin A claim 13 , acid β-glucosidase claim 13 , acid β-galactosidase claim 13 , iduronate 2-sulfatase claim 13 , α-L-iduronidase claim 13 , galactocerebrosidase claim 13 , acid α-mannosidase claim 13 , acid β-mannosidase claim 13 , arylsulfatase B claim 13 , arylsulfatase A claim 13 , N-acetylgalactosamine-6-sulfate sulfatase claim 13 , acid β-galactosidase claim 13 , N-acetylglucosamine-1-phosphotransferase claim 13 , acid sphingmyelinase ...

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21-03-2013 дата публикации

THIENOPYRIDINE ESTER DERIVATIVE CONTAINING CYANO GROUP, PREPARATION METHOD, USE AND COMPOSITION THEREOF

Номер: US20130072521A1

A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation. 2. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is selected from one of the following compounds:I-1: 5-(2-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate;I-2: 5-(3-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate;I-3: 5-(4-cyanobenzyl)-4,5,6,7-tetrahydrothieno [3,2-c]pyridin-2-yl acetate.3. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the pharmaceutically acceptable salt comprises the salt formed by the compound of formula I with an inorganic acid or an organic acid.4. The compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 3 , wherein the pharmaceutically acceptable salt is selected from hydrochlorides claim 3 , hydrobromides claim 3 , hydriodates claim 3 , sulfates claim 3 , hydrosulfates claim 3 , phosphates claim 3 , hydrophosphates claim 3 , acetates claim 3 , propionates claim 3 , butyrates claim 3 , lactates claim 3 , mesylates claim 3 , tosilates claim 3 , maleates claim 3 , benzoates claim 3 , succinates claim 3 , tartrates claim 3 , citrates claim 3 , fumarates claim 3 , taurates claim 3 , gluconates claim 3 , and amino acid salts of the compound of formula I.5. A method for preparing the compound with the structure of formula I or a pharmaceutically acceptable salt thereof according to claim 1 , ...

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21-03-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: US20130072523A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by Formula I: (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R1, R 2 , R 2 ′, R 3 , R 3 ′, R 4 , R 4 ′, R 5′ , R 5′ m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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28-03-2013 дата публикации

Fused Thiazole Derivatives as Kinase Inhibitors

Номер: US20130079330A1
Принадлежит: UCB PHARMA, S.A.

A series of 6,7-dihydro[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. 2. The compound as claimed in wherein Rrepresents Calkyl.3. The compound as claimed in wherein Rrepresents Calkyl.4. The compound as claimed in wherein T represents N—R.5. The compound as claimed in wherein V is carbon.6. The compound as claimed in wherein W is carbon.7. A compound as claimed in wherein Rrepresents hydrogen claim 1 , cyano claim 1 , carboxy claim 1 , Calkoxycarbonyl claim 1 , di(C)alkylaminocarbonyl claim 1 , [(C)alkyl][cyano(C)alkyl]aminocarbonyl claim 1 , [(C)alkoxy(C)alkyl][(C)alkyl]-aminocarbonyl or azetidinylcarbonyl.8. The compound as claimed in wherein Rrepresents hydrogen.9. The compound as claimed in wherein Rrepresents methyl.10. (canceled)11. The pharmaceutical composition comprising a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , in association with a pharmaceutically acceptable carrier.12. (canceled)13. (canceled)14. (canceled)15. A method for the treatment and/or prevention of a disorder for which the administration of a selective PI3K inhibitor is indicated which comprises administering to a patient in need of such treatment an effective amount of a compound of formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt or solvate thereof. The present invention relates to a class of fused thiazole derivatives, and to their use in therapy. More particularly, the invention provides a family of 6,7-dihydro-[1,3]thiazolo[5,4-c]pyridin-4(5H)-one derivatives, which are substituted in the 2-position by a substituted morpholin-4-yl moiety. These compounds are selective ...

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28-03-2013 дата публикации

THIENO (2, 3B) PYRAZINE COMPOUNDS AS B-RAF INHIBITORS

Номер: US20130079341A1
Принадлежит:

The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer. 2. The compound according to wherein X and Y are independently NHCO or CONH.3. The compound according to wherein X is NHCO.4. The compound according to wherein Y is CONH.5. The compound according to wherein the ar ring is (2-5C)heteroaryl substituted with one or more groups selected from (1-6C)alkyl claim 1 , phenyl claim 1 , (di)[(1-4C)alkyl]amino or pyrrolidinyl.7. The compound according to wherein R8 in the phenyl ring is (1-4C)alkyl claim 6 , optionally substituted with one or more CN claim 6 , aminocarbonyl claim 6 , halogen; (1-4C)alkoxy; (di)[(1-4C)alkyl]amino; or (2-5C)heteroaryl.8. The compound according to wherein R8 in the phenyl ring is (1-4C)alkyl claim 7 , optionally substituted with one or more CN or halogen.9. The compound according to wherein R7 claim 6 , R9 claim 6 , R10 and R11 are H.10. The compound according to wherein R1 is H; halogen; hydroxy; CN; amino; (1-2C)alkyl; (1-2C)alkylcarbonyl; (1-2C)alkoxy or (di)[(1-2C)alkyl]amino claim 1 , the alkyl group of which is optionally substituted with hydroxy; andR2 is H; halogen; hydroxy; CN; amino; (1-6C)alkyl; (di)[(1-6C)alkyl]amino, the alkyl group of which is optionally substituted with one or more hydroxy, (di)[(1-4C)alkylamino, (1-6C)alkoxy, (2-5C)heterocycloalkyl, (2-5C)heteroaryl or aryl; (1-4C)alkylcarbonyl; (1-4C)alkoxy, optionally substituted with (di)[(1-4C)alkyl]amino; (2-5C)heterocycloalkyl, optionally substituted with one or more groups selected from hydroxy, amino, (1-6C)alkyloxycarbonylamino) or (1-4C)alkyl, the alkyl optionally substituted with hydroxy; (2-5C)heteroaryl, optionally substituted with halogen, CN, (1-4C)alkoxy, (di)[(1-4C)alkyl]amino or (1-4C)alkyl; phenyl optionally substituted with halogen, CN, (1-4C)alkyl, (1-4C)alkoxy or (di)[(1-4C)alkyl]amino; 2-5C)heteroarylamino; phenylamino; or (2-5C) ...

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28-03-2013 дата публикации

Compounds that modulate intracellular calcium

Номер: US20130079348A1
Принадлежит: CalciMedica Inc

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.

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28-03-2013 дата публикации

NOVEL PIPERIDINO-DIHYDROTHIENOPYRIMIDINE SULFOXIDES AND THEIR USE FOR TREATING COPD AND ASTHMA

Номер: US20130079359A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, 2. The compound of formula I according to claim 1 , wherein R is in the para-position of Ring A claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or an enantiomer or racemate thereof.3. The compound of formula I according to claim 1 , wherein Ring A is selected from the group consisting of phenyl claim 1 , pyridinyl and pyrimidinyl claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or an enantiomer or racemate thereof.4. The compound of formula I according to claim 2 , wherein Ring A is selected from the group consisting of phenyl claim 2 , pyridinyl and pyrimidinyl claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , or an enantiomer or racemate thereof.7. The compound according to claim 1 , wherein S* is in the R-configuration.8. The compound according to claim 1 , wherein S* is in the S-configuration.9. A crystalline anhydrous compound of formula III according to claim 6 , which shows a reflex peak in the X-ray powder diffraction diagram with a d-value of 4.62 Å.10. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 6.82 Å claim 6 , and 10.09 Å.11. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 4.17 Å claim 6 , and 3.66 Å.12. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 6.82 Å claim 6 , 10.09 Å claim 6 , 3.93 Å claim 6 , and 4.94 Å.13. A crystalline anhydrous compound of formula III according to claim 6 , which shows reflex peaks in the X-ray powder diffraction diagram with d-values of 4.62 Å claim 6 , 4.17 Å claim 6 , 3.66 Å claim 6 , 3.73 Å claim 6 , and 18.47 Å.14. A ...

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28-03-2013 дата публикации

ORGANIC COMPOUNDS, PROCESS FOR PREPARING SAME AND USES IN ELECTRONICS

Номер: US20130079529A1
Принадлежит:

The present disclosure relates to novel organic compounds, to the processes for preparing same and to the uses thereof, firstly in the electronics field, in particular in the fields referred to as plastic electronics and molecular electronics, and, secondly, in the coatings field, in particular in the fields of adhesion primers and intelligent coatings. The disclosure also relates to a material comprising a novel compound according to the invention. 2. The compound of formula (I) as claimed in claim 1 , in which:{'sub': '1', 'Rrepresents a hydrogen atom or thiophene;'}{'sub': 2', '2, 'Rrepresents the amino (—NH) group or the aniline group;'}Z represents thiophene;n=1, 2 or 3;m=0 or 1;{'sub': '1', 'wherein, when Rrepresents a hydrogen atom and m=0, then n is other than 1.'}3. The compound of formula (I) as claimed in claim 1 , in which:{'sub': '1', 'Rrepresents a hydrogen atom or thiophene;'}{'sub': 2', '2', '2, 'sup': '+', 'Rrepresents the aniline group, the phenyl group substituted by the diazo (N) group or the phenyl group substituted by the —NOgroup;'}Z represents thiophene;n=1, 2 or 3;m=0 or 1;{'sub': '1', 'wherein, when Rrepresents a hydrogen atom and m=0, then n is other than 1.'}4. The compound of formula (I) as claimed in claim 3 , wherein claim 3 , when m=0 claim 3 , n is other than 1.5. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents a hydrogen atom;'}{'sub': '2', 'Rrepresents the aniline group;'}n=2; andm=0.6. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents thiophene;'}{'sub': '2', 'Rrepresents the aniline group;'}n=1; andm=0.7. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents a hydrogen atom;'}{'sub': '2', 'Rrepresents the aniline group;'}Z represents thiophene;n=1; andm=1.8. The compound of formula (I) as claimed in claim 1 , wherein:{'sub': '1', 'Rrepresents a hydrogen atom;'}{'sub': '2', 'Rrepresents the aniline group;'}n=3; andm=0.9. The ...

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04-04-2013 дата публикации

6-(4-Hydroxy-phenyl)-3-alkyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors

Номер: US20130085128A1
Принадлежит: SANOFI

The present invention relates to pyrazolo[3,4-b]pyridine compounds of the formula I, 10. A pharmaceutical composition comprising the compound of .11. A method of treating a disease associated with diabetes or a diabetic complication claim 1 , comprising administering to a human in need thereof a therapeutically effective amount of the compound of .12. A method of preventing or treating a neuropathy claim 1 , a retinopathy claim 1 , an ischemia claim 1 , inflammation claim 1 , a central nervous system disorder claim 1 , a cardiovascular disease claim 1 , a dermatological disease claim 1 , an autoimmune disease claim 1 , or cancer claim 1 , the method comprising administering to a human in need thereof a therapeutically effective amount of the compound of .13. A method of treating a disease associated with the PKC receptor claim 1 , the method comprising administering to a human in need thereof a therapeutically effective amount of the compound of .14. A method of treating a disease associated with diabetes or a diabetic complication claim 9 , comprising administering to a human in need thereof a therapeutically effective amount of the pharmaceutical composition of .15. A method of preventing or treating a neuropathy claim 9 , a retinopathy claim 9 , an ischemia claim 9 , inflammation claim 9 , a central nervous system disorder claim 9 , a cardiovascular disease claim 9 , a dermatological disease claim 9 , an autoimmune disease claim 9 , or cancer claim 9 , the method comprising administering to a human in need thereof a therapeutically effective amount of the pharmaceutical composition of .16. A method of treating a disease associated with the PKC receptor claim 9 , the method comprising administering to a human in need thereof a therapeutically effective amount of the pharmaceutical composition of . Protein kinase C (PKC) comprises a family of several related isoenzymes that function as serine/threonine kinases. PKC plays an important role in intercellular and ...

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04-04-2013 дата публикации

HETEROCYCLIC COMPOUNDS AND THEIR USES

Номер: US20130085151A1
Автор: Lucas Brian
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 p110 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. 2. A method of treating rheumatoid arthritis claim 1 , ankylosing spondylitis claim 1 , osteoarthritis claim 1 , psoriatic arthritis claim 1 , psoriasis claim 1 , inflammatory diseases and autoimmune diseases claim 1 , inflammatory bowel disorders claim 1 , inflammatory eye disorders claim 1 , inflammatory or unstable bladder disorders claim 1 , skin complaints with inflammatory components claim 1 , chronic inflammatory conditions claim 1 , autoimmune diseases claim 1 , systemic lupus erythematosis (SLE) claim 1 , myestenia gravis claim 1 , rheumatoid arthritis claim 1 , acute disseminated encephalomyelitis claim 1 , idiopathic thrombocytopenic purpura claim 1 , multiples sclerosis claim 1 , Sjoegren's syndrome and autoimmune hemolytic anemia claim 1 , allergic conditions and hypersensitivity claim 1 , ...

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04-04-2013 дата публикации

CRYSTALLINE FORMS OF PRASUGREL SALTS

Номер: US20130085154A1
Принадлежит:

Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets. 1. Crystalline Form 1 of Prasugrel hydrobromide.2. The crystalline Form I of Prasugrel hydrobromide according to claim 1 , characterized by data selected from: an X-ray powder diffraction pattern having peaks at 7.8 claim 1 , 14.4 claim 1 , 16.9 claim 1 , 22.0 and 25.1 degrees two theta±0.2 degrees two theta; an XRPD pattern substantially as depicted in ; a solid-state C MAR spectrum having peaks at 7.1 claim 1 , 11.2 claim 1 , 63.6 claim 1 , 123.7 and 203.4±0.2 ppm; a solid-state C NMR spectrum substantially as depicted in ; and combinations thereof.3. Crystalline Form IA of Prasugrel hydrobromide.4. The crystalline Form IA of Prasugrel hydrobromide according to claim 3 , characterized by data selected from: an X-ray powder diffraction pattern having peaks at 7.9 claim 3 , 8.1 claim 3 , 13.5 claim 3 , 14.6 and 25.2 degrees two theta±0.2 degrees two theta; an XRPD pattern substantially as depicted in ; and combinations thereof.6. The use of at least one crystalline form according to in the manufacture of a pharmaceutical composition.7. The use of a crystalline form according to in the manufacture of prasugrel hydrochloride.8. A crystalline form according to for use as a medicament.9. A crystalline form according to for use as a medicament for inhibiting aggregation of platelets.10. A pharmaceutical composition comprising at least one crystalline form according to claim 1 , and at least one pharmaceutically acceptable excipient.11. A method for inhibiting aggregation of platelets comprising administering a pharmaceutically effective amount of at least one crystalline form according to claim 1 , to a subject in need of such treatment.12. A process for preparing Prasugrel hydrochloride comprising preparing any one of the crystalline forms according to by the process of the ...

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11-04-2013 дата публикации

Inhibitors of Protein Tyrosine Kinase Activity

Номер: US20130090327A1
Принадлежит: METHYLGENE INC.

The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. 5. A composition comprising a compound according to any of to and a pharmaceutically acceptable carrier.6. A method of treating an opthalmic disease , condition or disorder , the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to any of to or a composition thereof , wherein the ophthalmic disease , disorder or condition is selected from the group consisting of (a) a disease , disorder or condition caused by choroidal angiogenesis , (b) diabetic retinopathy and (c) retinal oedema.7. The method according to claim 6 , wherein the ophthalmic disease claim 6 , disorder or condition is age-related macular degeneration. 1. Field of the InventionThis invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling.2. Summary of the Related ArtTyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. ...

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11-04-2013 дата публикации

N3-HETEROARYL SUBSTITUTED TRIAZOLES AND N5-HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS

Номер: US20130090330A1
Принадлежит: Rigel Pharmaceuticals, Inc.

N-Heteroaryl substituted triazoles and N-heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed. 233.-. (canceled)36. The method of wherein the disease or condition is alleviated by the modulation of Axl activity.3744.-. (canceled) This application is a divisional of U.S. patent application Ser. No. 11/966,894, filed Dec. 28, 2007 (now pending); which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 60/975,443, filed Sep. 26, 2007; and U.S. Provisional Patent Application No. 60/882,875, filed Dec. 29, 2006. These applications are incorporated herein by reference in their entireties.This invention is directed to N-heteroaryl substituted triazoles and N-heteroaryl substituted triazoles and pharmaceutical compositions thereof which are useful as inhibitors of the receptor protein tyrosine kinase known as Axl. This invention is also directed to methods of using the compounds and compositions in treating diseases and conditions associated with Axl activity, particularly in treating diseases and conditions associated with angiogenesis and/or cell proliferation.All of the protein kinases that have been identified to date in the human genome share a highly conserved catalytic domain of around 300 aa. This domain folds into a bi-lobed structure in which reside ATP-binding and catalytic sites. The complexity of protein kinase regulation allows many potential mechanisms of inhibition including competition with activating ligands, modulation of positive and negative regulators, interference with protein dimerization, and allosteric or competitive inhibition at the substrate or ATP binding sites.Axl (also known as UFO, ARK, and Tyro7; nucleotide accession numbers NM021913 and NM001699; protein ...

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11-04-2013 дата публикации

PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

Номер: US20130090335A1
Принадлежит:

The invention provides a compound of Formula I, 2. The compound of wherein R is RC(O)— claim 1 , wherein Ris substituted or unsubstituted C-C-alkyl; substituted or unsubstituted C-C-alkenyl claim 1 , preferably C-C-alkenyl claim 1 , and more preferably C-C-alkenyl; substituted or unsubstituted C-C-alkynyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl.3. The compound of wherein R is H or acetyl.5. A pharmaceutical composition comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.6. A pharmaceutical composition for oral administration comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.7. A pharmaceutical composition comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.8. A pharmaceutical composition for oral administration comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.9. A method of treating a PI3K related disease or disorder in a subject in need thereof claim 5 , the method comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of .10. The method of claim 9 , wherein said PI3K related disease or disorder is a cell proliferative disorder.11. The method of wherein the cell proliferative disorder is a cancer.12. The method of claim 11 , wherein the cancer is selected from the group consisting of papilloma claim 11 , blastoglioma claim 11 , Kaposi's sarcoma claim 11 , melanoma claim 11 , non-small cell lung cancer claim 11 , ovarian cancer claim 11 , prostate cancer claim 11 , squamous cell carcinoma claim 11 , astrocytoma claim 11 , head cancer claim 11 , neck cancer claim 11 , bladder cancer claim 11 , breast cancer claim 11 , lung cancer claim 11 , colorectal cancer claim 11 , thyroid cancer claim 11 , pancreatic cancer claim 11 , gastric cancer claim 11 , hepatocellular carcinoma claim 11 , leukemia claim 11 , lymphoma claim ...

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11-04-2013 дата публикации

N-CONTAINING HETEROCYCLIC COMPOUNDS

Номер: US20130090336A1
Принадлежит: YM Biosciences Australia Pty Ltd

The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases. 4. The compound according to claim 1 , wherein A is absent claim 1 , substituted or unsubstituted Calkylene or substituted or unsubstituted divalent Calkoxy and B is absent or S.5. The compound according to claim 1 , wherein R is independently selected from H claim 1 , halogen claim 1 , COR claim 1 , CONRR claim 1 , Ccycloalkyl claim 1 , 5 or 6 membered aryl and 5 to 8 membered heterocyclyls having up to 3 heteroatoms selected from N claim 1 , O claim 1 , S and SO claim 1 , each of which may be substituted with up to 3 substituents independently selected from substituted or unsubstituted Calkyl claim 1 , substituted or unsubstituted 5 to 8 membered heterocyclyls having up to 3 heteroatoms selected from N claim 1 , O claim 1 , S and SO claim 1 , ROH claim 1 , RNHCOR claim 1 , OCF claim 1 , substituted or unsubstituted Calkoxy claim 1 , OH claim 1 , NRR claim 1 , SONRR claim 1 , NRSOR claim 1 , NRCOR claim 1 , CONRR claim 1 , NRCONRR claim 1 , COR claim 1 , CORand/or SORwherein Rand Rare as defined in .6. The compound according to claim 1 , wherein R is independently selected from phenyl unsubstituted or substituted with at least one of NRR claim 1 , NRCOR claim 1 , substituted or unsubstituted Calkoxy claim 1 , substituted or unsubstituted 5 to 8 membered heterocyclyls having up to 3 heteroatoms selected from N claim 1 , O claim 1 , S and SO claim 1 , SONRR claim 1 , NRCONRR claim 1 , NRSOR claim 1 , ROH claim 1 , RNHCOR ...

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11-04-2013 дата публикации

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130090351A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I 2. The compound according claim 1 , wherein{'sub': 1', 'p, 'each A is independently cyclopropyl, cyclohexyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, piperadinyl, phenyl, naphthalenyl, thienyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, indolyl, indazolyl, benzimidazolyl, benzoxazolyl, benzodioxolyl, benzothiazolyl, benzothiadiazolyl, dihydrobenzodioxine, thienofuranyl, thienothienyl, thienopyrrolyl, quinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, or triazolyl; and wherein each A is independently substituted with (R).'}35.-. (canceled)6. The compound according to claim 2 , wherein each A is independently piperazinyl claim 2 , piperadinyl claim 2 , thienyl claim 2 , furanyl claim 2 , pyrrolyl claim 2 , pyrazolyl claim 2 , imidazolyl claim 2 , thiazolyl claim 2 , oxazolyl claim 2 , thiadiazolyl claim 2 , pyrrolidinyl claim 2 , pyridyl claim 2 , pyrimidinyl claim 2 , pyrazinyl claim 2 , pyridazinyl claim 2 , benzoxazolyl claim 2 , benzodioxolyl claim 2 , benzothiazolyl claim 2 , benzothiadiazolyl claim 2 , dihydrobenzodioxinyl claim 2 , thienofuranyl claim 2 , thienothienyl claim 2 , quinolinyl claim 2 , or triazolyl.78.-. (canceled)9. The compound according to claim 1 , wherein B and B′ are independently absent claim 1 , Calkyl or Calkynyl.1011.-. (canceled)1318.-. (canceled)19. The compound according to claim 1 , wherein Ris halogen claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , —C(═O)OR claim 1 , —C(O)NRR claim 1 , hydroxyl claim 1 , cyano claim 1 , or Calkoxy.20. (canceled)21. The compound according to claim 1 , wherein R′ is methyl claim 1 , trifluoromethyl claim 1 , iodo claim 1 , CHOH claim 1 , or NHC(O)CH.22. The compound according to claim 21 , wherein u is 0.23. The compound according to claim 1 , wherein each Ris independently fluoro or methyl.24. The compound according to ...

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11-04-2013 дата публикации

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130090364A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

Compounds represented by formula I 6. The compound according to any one of to , wherein{'sub': 1', 'p, 'each A is independently cyclopropyl, cyclohexyl, pyrrolidinyl, pyrazolidinyl, imidazolidinyl, piperazinyl, piperadinyl, phenyl, naphthalenyl, thienyl, furanyl, pyrrolyl, pyrazolyl, imidazolyl, thiazolyl, thiadiazolyl, oxazolyl, oxadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, indolyl, indazolyl, benzimidazolyl, benzoxazolyl, benzodioxolyl, benzothiazolyl, benzothiadiazolyl, dihydrobenzodioxine, thienofuranyl, thienothienyl, thienopyrrolyl, quinolinyl, quinoxalinyl, quinazolinyl, cinnolinyl, or triazolyl; and wherein each A is independently substituted with (R).'}712.-. (canceled)13. The compound according to claim 1 , wherein B and B′ are independently absent claim 1 , Calkyl or Calkynyl.1416.-. (canceled)1823.-. (canceled)24. The compound according to claim 1 , wherein Ris halogen claim 1 , Calkyl which is unsubstituted or substituted one or more times by R claim 1 , —C(═O)OR claim 1 , —C(O)NRR claim 1 , hydroxyl claim 1 , cyano claim 1 , or Calkoxy.25. The compound according to claim 24 , wherein Ris chloro claim 24 , fluoro claim 24 , bromo claim 24 , methyl claim 24 , ethyl claim 24 , propyl claim 24 , butyl claim 24 , —CHOH claim 24 , difluoromethyl claim 24 , trifluoromethyl claim 24 , —C(═O)OR claim 24 , hydroxyl claim 24 , cyano claim 24 , or methoxy.26. The compound according to claim 1 , wherein R′ is fluoro claim 1 , methyl claim 1 , trifluoromethyl claim 1 , iodo claim 1 , CHOH claim 1 , or NHC(O)CH.27. The compound according to claim 26 , wherein s is 0.28. The compound according to claim 1 , wherein each Ris independently fluoro or methyl.29. The compound according to claim 28 , wherein s is 0.30. The compound according to claim 1 , wherein Rand R′ are H or methyl.3233.-. (canceled)34. The compound according to claim 1 , wherein m and n are independently 1 or 2.35. (canceled)37. The compound according to claim 1 , wherein Rand R′ are each ...

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18-04-2013 дата публикации

COMPOUNDS FOR THE TREATMENT OF CLOSTRIDIUM DIFFICILE-ASSOCIATED DISEASE

Номер: US20130095057A1
Принадлежит:

Disclosed are compounds of formula (I): 2. The compound of wherein Ris: (a) a pyridyl group; or (b) a thiazole group.3. The compound of wherein Ris an optionally substituted aromatic 8-10 membered fused bicyclic ring system in which one or more of the carbon atoms may be replaced by N claim 1 , O claim 1 , S claim 1 , SO or SOand the optional substitution being with one or more substituents selected from halo claim 1 , CN claim 1 , NO claim 1 , R claim 1 , OR claim 1 , N(R) claim 1 , COR claim 1 , COR claim 1 , C(═O)SR claim 1 , SR claim 1 , S(═O)R claim 1 , SOR claim 1 , NRC(═O)R claim 1 , NRCOR claim 1 , OC(═O)NRR claim 1 , NRSOR claim 1 , C(═NR)NRR claim 1 , C(═S)NRR claim 1 , NRC(═NR)NRR claim 1 , NRC(═S)NRR claim 1 , NRC(═O)NRR claim 1 , CONRRand SONRR.4. The compound of wherein R is an optionally substituted aromatic 9-membered bicyclic ring system in which one or more of the carbon atoms may be replaced by N claim 3 , O claim 3 , S claim 3 , SO or SOand the optional substitution being with one or more substituents selected from halo claim 3 , CN claim 3 , NO claim 3 , R claim 3 , OR claim 3 , N(R) claim 3 , COR claim 3 , COR claim 3 , C(═O)SR claim 3 , SR claim 3 , S(═O)R claim 3 , SOR claim 3 , NRC(═O)R claim 3 , NRCOR claim 3 , OC(═O)NRR claim 3 , NRSOR claim 3 , C(═NR)NRR claim 3 , C(═S)NRR claim 3 , NRC(═NR)NRR claim 3 , NRC(═S)NRR claim 3 , NRC(═O)NRR claim 3 , CONRRand SONRR.5. The compound of wherein Ris an optionally substituted aromatic fused 5- and 6-membered bicyclic ring system.6. The compound of wherein Ris: (a) a thienopyridyl group; or (b) a benzothiophene group; or (c) a benzofuran group; or (d) a pyridyl imidazole group; or (e) a benzodioxol group; or (f) an indole group.7. The compound of wherein Ris an optionally substituted aromatic fused 6- and 6-membered bicyclic ring system.8. The compound of wherein Ris: (a) a isoquinolone group; or (b) a quinoxaline group; or (c) an isoquinoline group; or (d) a quinoline group; or (e) a naphthyridine ...

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18-04-2013 дата публикации

COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE

Номер: US20130095193A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. 2. The compound of claim 1 , wherein{'sub': 1-4', '1-4, 'J is halo, Calkyl, or Calkoxy;'}{'sup': '1', 'sub': 'q', 'Jis —(X)—Y;'}{'sub': 1-6', '1-6', '1-3, 'X is Calkyl wherein 0-2 methylene units of said Calkyl are replaced with NH, O, or S; X is optionally substituted with 1-2 occurrences of Calkyl or halo;'}{'sup': '1', 'sub': '1-3', 'or J and Jjoin together to form a 5-7 heterocyclyl having 1-2 heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur; wherein the heterocyclyl is optionally substituted with 1 occurrence of halo or Calkyl;'}{'sup': '4', 'Jis CN or L-Z;'}{'sub': '2', 'L is C(O), S(O), or C(O)NR;'}{'sub': t—', '1-6', '1-6, 'Z is (U)Q or Calkyl wherein 0-2 methylene units of said Calkyl are replaced with O or NR;'}{'sub': '1-2', 'U is Calkyl;'}t is 0 or 1;{'sub': '3-6', 'Q is Ccycloalkyl or 4-6 membered saturated or partially saturated heterocyclyl having 1-2 heteroatoms selected from the group consisting of oxygen, nitrogen, and sulfur; and'}{'sub': '1-4', 'R is H or Calkyl.'}3. The compound of claim 2 , wherein{'sup': '4', 'Jis CN or L-Z;'}{'sup': '5', 'Jis H;'}{'sup': '3', 'sub': '1-6', 'Jis Calkyl;'}{'sub': 1-4', '1-3, 'Y is hydrogen, Calkyl, or a 3-6 membered saturated or partially unsaturated heterocyclyl having 1-2 heteroatoms ...

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18-04-2013 дата публикации

LEAVING SUBSTITUENT-CONTAINING COMPOUND, ORGANIC SEMICONDUCTOR MATERIAL FORMED THEREFROM, ORGANIC ELECTRONIC DEVICE, ORGANIC THIN-FILM TRANSISTOR AND DISPLAY DEVICE USING THE ORGANIC SEMICONDUCTOR MATERIAL, METHOD FOR PRODUCING FILM-LIKE PRODUCT, PI-ELECTRON CONJUGATED COMPOUND AND METHOD FOR PRODUCING THE PI ELECTRON CONJUGATED COMPOUND

Номер: US20130095605A1
Принадлежит: RICOH COMPANY, LTD.

A leaving substituent-containing compound represented by General Formula (I), wherein the leaving substituent-containing compound can be converted to a compound represented by General Formula (Ia) and a compound represented by General Formula (II), by applying energy to the leaving substituent-containing compound, in General Formulas (I), (Ia) and (II), X and Y each represent a hydrogen atom or a leaving substituent, where one of X and Y is the leaving substituent and the other is the hydrogen atom; Qto Qeach represent a hydrogen atom, a halogen atom or a monovalent organic group; Qand Qeach represent a hydrogen atom or a monovalent organic group other than the leaving substituent; and among the monovalent organic groups represented by Qto Q, adjacent monovalent organic groups may be linked together to form a ring. 2: The leaving substituent-comprising compound according to claim 1 , wherein the leaving substituent represented by X or Y is a substituted or unsubstituted ether group or acyloxy group comprising a carbon atom.3: The leaving substituent-comprising compound according to claim 1 , wherein in the General Formula (I) claim 1 , at least one pair selected from (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) and (Q claim 1 , Q) forms a ring structure which optionally has a substituent claim 1 , and one pair optionally forms a ring structure with adjacent pair or pairs.4: The leaving substituent-comprising compound according to claim 1 , wherein in the General Formula (I) claim 1 , at least one pair selected from (Q claim 1 , Q) claim 1 , (Q claim 1 , Q) and (Q claim 1 , Q) forms a ring structure which optionally has a substituent.5: The leaving substituent-comprising compound according to claim 3 , wherein the ring structure is an aryl group or a heteroaryl group.614-. (canceled)16: The method according to claim 15 , wherein the leaving substituent represented by X or Y is a substituted or unsubstituted ether group ...

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18-04-2013 дата публикации

Inhibitors of Protein Tyrosine Kinase Activity

Номер: US20130096088A1
Принадлежит: METHYLGENE INC.

The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. 12. A composition comprising a compound according to and a pharmaceutically acceptable carrier.13. A method of treating an ophthalmic disease claim 1 , condition or disorder claim 1 , the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a composition thereof claim 1 , wherein the ophthalmic disease claim 1 , disorder or condition is selected from the group consisting of (a) a disease claim 1 , disorder or condition caused by choroidal angiogenesis claim 1 , (b) diabetic retinopathy and (c) retinal oedema.14. The method according to claim 13 , wherein the ophthalmic disease claim 13 , disorder or condition is age-related macular degeneration. This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling.Tyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. These tyrosine kinases ...

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18-04-2013 дата публикации

USE OF AMINODIHYDROTHIAZINES FOR THE TREATMENT OR PREVENTION OF DIABETES

Номер: US20130096107A1
Принадлежит: Hoffmann-La Roche Inc.

This invention relates to compounds of formula I, 2. A compound according to claim 1 , wherein Ris halogen.3. A compound according to claim 1 , wherein Ris fluoro.4. A compound according to claim 1 , wherein Ris heteroaryl claim 1 , said heteroaryl being unsubstituted or substituted by one claim 1 , two or three groups selected from the group consisting of C-alkyl claim 1 , halogen claim 1 , halogen-C-alkyl claim 1 , C-alkoxy claim 1 , halogen-C-alkoxy claim 1 , cyano claim 1 , hydroxy-C-alkyl and phenyl.5. A compound according to claim 1 , wherein Ris heteroaryl selected from the group consisting of thienyl claim 1 , oxazolyl claim 1 , thiazolyl claim 1 , pyrazolyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , isoquinolinyl claim 1 , thieno[2 claim 1 ,3-c]pyridyl and benzo[b]thienyl claim 1 , said heteroaryl being unsubstituted or substituted by one claim 1 , two or three groups selected from the group consisting of C-alkyl claim 1 , halogen claim 1 , halogen-C-alkyl and phenyl.6. A compound according to claim 1 , wherein Ris phenyl claim 1 , said phenyl being unsubstituted or substituted by one claim 1 , two or three groups selected from the group consisting of C-alkyl claim 1 , halogen claim 1 , halogen-C-alkyl claim 1 , C-alkoxy claim 1 , halogen-C-alkoxy claim 1 , cyano claim 1 , hydroxy-C-alkyl and phenyl.8. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier and/or adjuvant.10. A method according to wherein:{'sup': '1', 'Ris ethyl; and'}{'sup': '2', 'sub': 1-7', '1-7, 'Ris selected from the group consisting of C-alkyl, halogen, cyano and C-alkoxy.'} This application is a continuation of U.S. application Ser. No. 12/874,336, filed Sep. 2, 2010, and claims the benefit of European Patent Application No. 09170126.8, filed Sep. 11, 2009, and European Patent Application No. 09172068.0, filed Oct. 2, 2009 which are hereby incorporated by reference in their entirety.The present invention is concerned ...

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18-04-2013 дата публикации

Inhibitors of Protein Tyrosine Kinase Activity

Номер: US20130096136A1
Принадлежит: METHYLGENE INC.

The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling. 12. A composition comprising a compound according to and a pharmaceutically acceptable carrier.13. A method of treating an opthalmic disease claim 1 , condition or disorder claim 1 , the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to or a composition thereof claim 1 , wherein the ophthalmic disease claim 1 , disorder or condition is selected from the group consisting of (a) a disease claim 1 , disorder or condition caused by choroidal angiogenesis claim 1 , (b) diabetic retinopathy and (c) retinal oedema.14. The method according to claim 13 , wherein the ophthalmic disease claim 13 , disorder or condition is age-related macular degeneration. This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling.Tyrosine kinases may be classified as growth factor receptor (e.g. EGFR, PDGFR, FGFR and erbB2) or non-receptor (e.g. c-src and bcr-abl) kinases. The receptor type tyrosine kinases make up about 20 different subfamilies. The non-receptor type tyrosine kinases make up numerous subfamilies. These tyrosine kinases have diverse biological ...

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18-04-2013 дата публикации

Tricyclic Compounds Having Antimitotic and/or Antitumor Activity and Methods of Use Thereof

Номер: US20130096146A1
Автор: Gangjee Aleem
Принадлежит:

The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells. 2. The compound of comprising pharmaceutically acceptable salts claim 1 , prodrugs claim 1 , solvates claim 1 , or hydrates thereof.3. The compound of comprising wherein when the C ring is saturated or partially saturated claim 1 , the substituted Rcreates chirality when X is a C and Rand Rare different.4. The compound of comprising stereoisomers thereof.5. The compound of comprising a racemic and/or a diastereoisomeric mixture thereof.7. The compound of comprising pharmaceutically acceptable salts claim 6 , prodrugs claim 6 , solvates claim 6 , or hydrates thereof.8. The compound of comprising wherein when the C ring is saturated or partially saturated claim 6 , the substituted Rcreates chirality when X is a C and Rand Rare different.9. The compound of comprising stereoisomers thereof.10. The compound of comprising a racemic and/or a diastereoisomeric mixture thereof.12. The method of including administering to the patient a therapeutically effective amount of a pharmaceutical salt claim 11 , prodrug claim 11 , solvate claim 11 , or hydrate of said compound of Formula II. This application is a divisional utility patent application claiming priority to pending U.S. Utility patent application Ser. No. 13/151,530, filed on Jun. 2, 2011, which is a divisional application of and claims the benefit of priority to U.S. Utility patent application Ser. No. 12/170,633, filed on Jul. 10, 2008, now U.S. Pat. No. 7,982,035, granted on Jul. 19, 2011, which is a continuation-in-part application of and claims the benefit of priority to U.S. ...

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25-04-2013 дата публикации

FLUORINATED RESORUFIN COMPOUNDS AND THEIR APPLICATION

Номер: US20130102014A1
Принадлежит: LIFE TECHNOLOGIES CORPORATION

The invention provides novel fluorinated resorufin compounds that are of use in a variety of assay formats. Also provided are methods of using the compounds and kits that include a compound of the invention and instructions detailing the use of the compound in one or more assay formats. 2. The compound according to claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , and Ris fluorine.3. The compound according to claim 1 , wherein A is OR claim 1 , E is OR claim 1 , E is OR claim 1 , and Ris hydrogen.46.-. (canceled)7. The compound according to claim 1 , wherein Rand Rare fluorine.8. The compound according to claim 1 , wherein Rand Rare each fluorine.9. The compound according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare each fluorine.10. The compound according to claim 1 , wherein Rand Rare each fluorine and R claim 1 , R claim 1 , Rand Rare hydrogen claim 1 , substituted alkyl claim 1 , unsubstituted alkyl claim 1 , substituted alkoxy claim 1 , unsubstituted alkoxy claim 1 , substituted alkylthio claim 1 , unsubstituted alkylthio claim 1 , substituted aryl claim 1 , unsubstituted aryl claim 1 , substituted heteroaryl claim 1 , or unsubstituted heteroaryl.11. The compound according to claim 1 , wherein Rand Rare each fluorine and R claim 1 , R claim 1 , Rand Rare each hydrogen.12. The compound according to claim 1 , wherein Rand Rare each fluorine and R claim 1 , R claim 1 , Rand Rare hydrogen claim 1 , substituted alkyl claim 1 , unsubstituted alkyl claim 1 , substituted alkoxy claim 1 , unsubstituted alkoxy claim 1 , substituted alkylthio claim 1 , unsubstituted alkylthio claim 1 , substituted aryl claim 1 , unsubstituted aryl claim 1 , substituted heteroaryl claim 1 , or unsubstituted heteroaryl.13. The compound according to claim 1 , wherein Rand Rare each fluorine and R claim 1 , R claim 1 , Rand Rare each hydrogen.1417-. (canceled)18. The compound according to claim 1 , wherein Ris hydrogen claim 1 , substituted alkyl or unsubstituted ...

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25-04-2013 дата публикации

Treatment of cancers having k-ras mutations

Номер: US20130102595A1
Принадлежит: Curis Inc

The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.

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25-04-2013 дата публикации

NOVEL CONDENSED PYRIDINE OR CONDENSED PYRIMIDINE DERIVATIVE, AND MEDICINAL AGENT COMPRISING SAME

Номер: US20130102621A1
Принадлежит: KOWA CO., LTD.

The present invention relates to provision of a novel compound that has an activity of promoting insulin secretion from pancreatic β cells and thus is useful as a prophylaxis and/or therapeutic agent for diseases caused by hyperglycemia such as diabetes mellitus, and 3. The compound of claim 1 ,which is selected from the following compound group, or a salt thereof, or a solvate of the compound or the salt:tert-butyl 4-(4-{[2-fluoro-4-(methylsulfonyl)phenyl]amino}furo[3,2-d]pyrimidin-7-yl)piperidine-1-carboxylate;7-[1-(5-chloropyrimidin-2-yl)piperidin-4-yl]-N-[2-fluoro-4-(methylsulfonyl)phenyl]furo[3,2-d]pyrimidine-4-amine;7-[1-(5-ethylpyrimidin-2-yl)piperidin-4-yl]-N-[2-fluoro-4-(methylsulfonyl)phenyl]furo[3,2-d]pyrimidine-4-amine;N-[2-fluoro-4-(methylsulfonyl)phenyl]-7-[1-(5-fluoropyrimidin-2-yl)piperidin-4-yl]furo[3,2-d]pyrimidine-4-amine7-[1-(5-bromopyrimidin-2-yl)piperidin-4-yl]-N-[2-fluoro-4-(methylsulfonyl)phenyl]furo[3,2-d]pyrimidine-4-amine;N-[2-fluoro-4-(methyl sulfonyl)phenyl]-7-{1-[5-(trifluoromethyl)pyridin-2-yl]piperidin-4-yl}furo[3,2-d]pyrimidine-4-amine;benzyl 4-(4-[2-fluoro-4-(methylsulfonyl)phenyl]amino}furo[3,2-d]pyrimidin-7-yl)piperidine-1-carboxylate;isopropyl 4-(4-{[2-fluoro-4-(methylsulfonyl)phenyl]amino}furo[3,2-d]pyrimidin-7-yl)piperidine-1-carboxylate;ethyl 4-(4-{[2-fluoro-4-(methylsulfonyl)phenyl]amino}furo[3,2-d]pyrimidin-7-yl)piperidine-1-carboxylate;7-(1-{[3,5-bis(trifluoromethyl)phenyl]sulfonyl}piperidin-4-yl)-N-[2-fluoro-4-(methylsulfonyl)phenyl]furo[3,2-d]pyrimidine-4-amine;7-[1-(cyclopropylsulfonyl)piperidin-4-yl]-N-[2-fluoro-4-(methylsulfonyl)phenyl]furo[3,2-c]pyrimidine-4-amine;7-[1-(cyclohexylsulfonyl)piperidin-4-yl]-N-[2-fluoro-4-(methylsulfonyl)phenyl]furo[3,2-d]pyrimidine-4-amine;N-[2-fluoro-4-(methylsulfonyl)phenyl]-7-[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]furo[3,2-d]pyrimidine-4-amine;N-[2-fluoro-4-(methylsulfonyl)phenyl]-7-{1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl}furo[3,2-d]pyrimidine-4-amine;7-[1-(butylsulfonyl) ...

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25-04-2013 дата публикации

Analogues for the treatment or prevention of flavivirus infections

Номер: US20130102629A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R 1 , R 2 , R 2 ′, R 3 , R 3 ′, R 4 , R 4 ′, R 5 , R 5 ′, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

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25-04-2013 дата публикации

METHOD OF MAKING COUPLED HETEROARYL COMPOUNDS VIA REARRANGEMENT OF HALOGENATED HETEROAROMATICS FOLLOWED BY OXIDATIVE COUPLING

Номер: US20130102785A1
Принадлежит: GEORGIA TECH RESEARCH CORPORATION

The inventions disclosed and described herein relate to new and efficient generic methods for making a wide variety of compounds having Formulas (I) and (II) as shown below (Formulas (I) and (II)) wherein HAr is an optionally substituted five or six membered heteroaryl ring, and Hal is a halogen, and Y is a bridging radical, such as S, Se, NRC(O), C(O)C(O), Si(R), SO, SO, PR, BR, C(R)or P(O)R. The synthetic methods employ a “Base-Catalyzed Halogen Dance” reaction to prepare a metallated compound comprising a five or six membered heteroaryl ring comprising a halogen atom, and then oxidatively coupling the reactive intermediate compound. The compounds of Formula (II) and/or oligomer or polymers comprising repeat units having Formula (II) can be useful for making semi-conducting materials, and/or electronic devices comprising those materials. 2. The method of wherein Hal is Br or I.3. The method of wherein HAr is an optionally substituted five membered heteroaryl ring.87. The method of any one of - wherein Ris a C-Caryl or heteroaryl optionally substituted by one to four ring substituents independently selected from halides claims 4 , alkyl claims 4 , alkynyl claims 4 , perfluoroalkyl claims 4 , alkoxide claims 4 , perfluoroalkoxide claims 4 , —Sn(R) claims 4 , —Si(R) claims 4 , —Si(OR)or —B(—OR)wherein each Ris an independently selected alkyl or aryl claims 4 , and each Ris an independently selected alkyl or aryl claims 4 , or the Rgroups together form an optionally substituted alkylene group to form a ring bridging the oxygen atoms.1110. The method of any one of - wherein the strongly basic compound is an alkyl lithium compound.1210. The method of any one of - wherein the strongly basic compound is a lithium dialkylamide compound.1310. The method of any one of - wherein the oxidizing agent is a Cu(II) salt.1410. The method of any one of - wherein the bishalo-bisheteroaryl compound is a 2 claims 1 ,2′-bishalo-1 claims 1 ,1′-bisheteroaryl compound.21. The method of ...

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02-05-2013 дата публикации

MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20130109677A1
Принадлежит:

Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia. 24-. (canceled)6. The compound of claim 5 , wherein m is 0; n is 1; Rand Rare each independently hydrogen claim 5 , optionally substituted C-Calkyl claim 5 , or optionally substituted C-Calkyl; Rand Rare each independently hydrogen or optionally substituted C-Calkyl; Ris hydrogen; and Rand Rare each independently hydrogen claim 5 , halo claim 5 , C-Calkyl claim 5 , aryl claim 5 , heteroaryl claim 5 , heterocyclyl claim 5 , alkoxyl claim 5 , or aminoalkyl claim 5 , each of which is optionally substituted.7. (canceled)8. The compound of claim 5 , wherein Rand Rtogether with the nitrogen atom to which they are attached form a heteroaryl or heterocyclyl claim 5 , each of which is optionally substituted.9. (canceled)10. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an optionally substituted heterocyclyl ring.11. (canceled)12. The compound of claim 5 , wherein Rand Rtogether with the atom to which they are attached form a cycloalkyl or heterocyclyl ring claim 5 , each of which is optionally substituted.13. (canceled)14. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an aryl or cycloalkyl ring claim 5 , each of which is optionally substituted.15. (canceled)16. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an optionally substituted heterocyclyl.17. (canceled)18. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an optionally substituted heterocyclyl and Rand Rtogether with the nitrogen atom to which they are attached form an optionally substituted aryl. ...

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02-05-2013 дата публикации

Small Molecule Inhibitors of Functions of the HIV-1 Matrix Protein

Номер: US20130109698A1
Автор: Simon Cocklin
Принадлежит: Simon Cocklin

The present invention includes a method of inhibiting, suppressing or preventing retroviral infection in a subject in need thereof, comprising administering to the subject a pharmaceutical composition comprising one or more of the compounds of the invention.

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02-05-2013 дата публикации

FAAH Inhibitors

Номер: US20130109721A1
Принадлежит: Ironwood Pharmaceuticals, Inc.

The present disclosure relates to N-benzyl pyrrole compounds of formula (I) useful as inhibitors of the enzyme Fatty Acid Amide Hydrolase (FAAH). The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment or prevention of various disorders. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is an optionally substituted ring selected from the group consisting of phenyl claim 1 , pyridine claim 1 , pyrimidine claim 1 , pyrazine claim 1 , pyridazine claim 1 , pyrrole claim 1 , imidazole claim 1 , pyrazole claim 1 , furan claim 1 , thiophene claim 1 , triazole claim 1 , tetrazole claim 1 , thiazole claim 1 , oxathiazole and oxazole.3. The compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein ring B is an optionally substituted pyridine or an optionally substituted phenyl.45.-. (canceled)6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is selected from the group consisting of 0 and 1.7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Jis independently selected from the group consisting of halogen claim 1 , Calkyl claim 1 , cyclopropyl claim 1 , cyclopropyloxy claim 1 , Chaloalkyl claim 1 , Calkoxy and Chaloalkoxy.8. The compound according to claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein each Jis independently selected from the group consisting of halogen claim 7 , methyl claim 7 , ethyl claim 7 , propyl claim 7 , isopropyl claim 7 , trifluoromethyl claim 7 , methoxy claim 7 , trifluoromethoxy claim 7 , ethoxy claim 7 , propyloxy and isopropyloxy.10. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein p is selected from the group consisting of 0 claim 1 , 1 and 2.11. The compound ...

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02-05-2013 дата публикации

Conjugated fused thiophenes, methods of making conjugated fused thiophenes, and uses thereof

Номер: US20130109821A1
Принадлежит: Corning Inc

Described herein are compositions including heterocyclic organic compounds based on fused thiophene compounds, polymers based on fused thiophene compounds, and methods for making the monomers and polymer along with uses in thin film-based and other devices.

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09-05-2013 дата публикации

NOVEL FUSED PYRIMIDINE DERIVATIVES FOR INHIBITION OF TYROSINE KINASE ACTIVITY

Номер: US20130116213A1
Принадлежит: HANMI SCIENCE CO., LTD.

The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient. 3. The compound of claim 1 , wherein the compound of formula (I) is selected from the group consisting of:N-(3-(2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide;N-(3-(2-(4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide;N-(3-(2-(4-(4-tert-butyl-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(4-(2-fluoro-ethyl)-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(4-(2,2,2-trifluoro-ethyl)-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(4-(2-methoxy-ethyl)-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(4-(2-hydroxy-ethyl)-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(4-hydroxy-4-methyl-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(3,4,5-trimethyl-piperazin-1-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(4-(5-methyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(1-methyl-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-7-ylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(2-methoxy-4-(1-methyl-piperidin-4-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(2-methoxy-4-(1-methyl-piperidin-3-yl)-phenylamino)-thieno[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide;N-(3-(2-(3-fluoro-4-(4-methylpiperazin-1-yl)phenylamino)thieno[3,2-d]pyrimidin-4-yloxy)phenyl)acrylamide;Diethyl(4-((4-(3- ...

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09-05-2013 дата публикации

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

Номер: US20130116233A1
Принадлежит:

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 3. The compound of claim 1 , where Xis selected from O claim 1 , S claim 1 , —X═C(R)— claim 1 , where C(R) is bound to the carbon atom which carries R.4. The compound of claim 1 , where A is selected from A claim 1 , A claim 1 , Aand A.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 5 , where Ris hydrogen or Y-Cyc.7. The compound of claim 1 , where Xis N.8. The compound of claim 1 , where Xis CH.9. The compound of claim 1 , where Xis S.10. The compound of claim 1 , where Xis O.11. The compound of claim 1 , where Xis C(R)═C(R).12. The compound of claim 1 , where Xis N═(CR).13. The compound of claim 11 , where Ris hydrogen or Y-Cyc3.14. The compound of claim 1 , where Xis N═C(R).15. The compound of claim 11 , where Ris hydrogen.16. The compound of claim 1 , where Ris a radical Y-Cyc.17. The compound of claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , C-C-alkyl claim 1 , C-C-fluoroalkyl claim 1 , C-C-alkoxy claim 1 , C-C-fluoroalkoxy claim 1 , cyclopropyl claim 1 , optionally substituted by 1 claim 1 , 2 or 3 methyl groups claim 1 , and fluorinated cyclopropyl.18. The compound of claim 17 , where Ris hydrogen.19. The compound of claim 1 , where A is A.20. The compound of claim 19 , where R claim 19 , Rare selected from hydrogen and fluorine.21. The compound of claim 19 , where Rand Rare claim 19 , independently of each other claim 19 , selected from the group consisting of hydrogen claim 19 , fluorine and methyl.22. The compound of claim 1 , where A is A.23. The compound of claim 1 , where A is ...

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09-05-2013 дата публикации

HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS

Номер: US20130116235A1
Принадлежит: Genentech, Inc.

Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein Xis N.3. The compound of wherein Xis N.4. The compound of wherein Xis N.5. The compound of wherein Xand Xare N claim 1 , Xand Xare N claim 1 , or Xand Xare N.6. The compound of wherein Ris optionally substituted C-Cheteroaryl selected from pyrazolyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , 5-methyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 5-acetyl-4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydropyrazolo[1 claim 1 ,5-a]pyrazin-2-yl claim 1 , 6 claim 1 ,7-dihydro-4H-pyrazolo[5 claim 1 ,1-c][1 claim 1 ,4]oxazin-2-yl claim 1 , and 1-methyl-5-(5-(4-methylpiperazin-1-yl)pyridin-2-yl.7. The compound of wherein Ris —(C-Cheteroaryl)-(C-Cheterocyclyl) where heteroaryl is optionally substituted pyridinyl and heterocyclyl is optionally substituted piperazinyl.8. The compound of wherein Ris phenyl claim 1 , optionally substituted with one or more groups selected from F claim 1 , Cl claim 1 , —CH claim 1 , —S(O)CH claim 1 , cyclopropyl claim 1 , azetidinyl claim 1 , oxetanyl claim 1 , and morpholino.11. The compound of wherein Ris CH.12. The compound of wherein Yis CH and Yis N.13. The compound of wherein Yis N and Yis CH.14. The compound of wherein Yand Yare each CH.15. The compound of wherein Yand Yare each CH claim 1 , and Ris CH.16. The compound of selected from Table 1.17. The compound of selected from Table 218. A pharmaceutical composition comprised of a compound of and a pharmaceutically ...

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09-05-2013 дата публикации

NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A

Номер: US20130116241A1
Принадлежит:

The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. 3. The compound of claim 1 , where Xis selected from O claim 1 , S claim 1 , —X═C(R)— claim 1 , where C(R) is bound to the carbon atom which carries R.4. The compound of claim 1 , where A is selected from A claim 1 , A claim 1 , Aand A.5. The compound of claim 1 , where Xis C—R.6. The compound of claim 5 , where Ris hydrogen or Y-Cyc.7. The compound of claim 1 , where Xis N.8. The compound of claim 1 , where Xis CH.9. The compound of claim 1 , where Xis S.10. The compound of claim 1 , where Xis O.11. The compound of claim 1 , where Xis C(R)═C(R).12. The compound of claim 1 , where Xis N═(CR).13. The compound of claim 11 , where Ris hydrogen or Y-Cyc.14. The compound of claim 1 , where Xis N═C(R).15. The compound of claim 11 , where Ris hydrogen.16. The compound of claim 1 , where Ris a radical Y-Cyc.17. The compound of claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , fluorine claim 1 , C-C-alkyl claim 1 , C-C-fluoroalkyl claim 1 , C-C-alkoxy claim 1 , C-C-fluoroalkoxy claim 1 , cyclopropyl claim 1 , optionally substituted by 1 claim 1 , 2 or 3 methyl groups claim 1 , and fluorinated cyclopropyl.18. The compound of claim 17 , where Ris hydrogen.19. The compound of claim 1 , where A is A.20. The compound of claim 19 , where R claim 19 , Rare selected from hydrogen and fluorine.21. The compound of claim 19 , where Rand Rare claim 19 , independently of each other claim 19 , selected from the group consisting of hydrogen claim 19 , fluorine and methyl.22. The compound of claim 1 , where A is A.23. The compound of claim 1 , where A is ...

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09-05-2013 дата публикации

ALKYLATED PIPERAZINE COMPOUNDS

Номер: US20130116245A1
Принадлежит: Genentech, Inc.

Alkylated piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 2. The compound of wherein X is CR claim 1 , and Ris H3. The compound of wherein X is N.4. The compound of wherein Ris —CHOH.5. The compound of wherein Ris F.6. The compound of wherein Rand Rare H.7. The compound of wherein Ris CH.8. The compound of selected from Table 1.9. The compound of selected from Table 2.10. A pharmaceutical composition comprised of a compound of and a pharmaceutically acceptable carrier claim 1 , glidant claim 1 , diluent claim 1 , or excipient.11. The pharmaceutical composition according to claim 10 , further comprising a therapeutic agent.12. A process for making a pharmaceutical composition which comprises combining a compound of with a pharmaceutically acceptable carrier.13. A method of treating a disease or disorder which comprises administering a therapeutically effective amount of the pharmaceutical composition of to a patient with a disease or disorder selected from immune disorders claim 10 , cancer claim 10 , cardiovascular disease claim 10 , viral infection claim 10 , inflammation claim 10 , metabolism/endocrine function disorders and neurological disorders claim 10 , and mediated by Bruton's tyrosine kinase.14. The method of wherein the disease or disorder is an immune disorder.15. The method of wherein the immune disorder is rheumatoid arthritis.16. The method of wherein the disease or disorder is systemic and local inflammation claim 13 , arthritis claim 13 , inflammation related to immune suppression claim 13 , organ transplant rejection claim 13 , allergies claim 13 , ulcerative colitis ...

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09-05-2013 дата публикации

BICYCLIC PIPERAZINE COMPOUNDS

Номер: US20130116262A1
Принадлежит: Genentech, Inc.

Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. 5. The compound of wherein Xis N claim 1 , Xis CR claim 1 , and Xis CR.6. The compound of wherein Xis CR claim 1 , Xis N claim 1 , and Xis CR.7. The compound of wherein Xis CR claim 1 , Xis CR claim 1 , and Xis N.8. The compound of selected from: Xand Xare N claim 1 , Xand Xare N claim 1 , or Xand Xare N.9. The compound of wherein Ris —CHOH.10. The compound of wherein Xis CR claim 4 , and Ris F.11. The compound of wherein Xand Xare CH.12. The compound of wherein Yis CR claim 1 , and Ris CH.13. The compound of selected from Table 1.14. The compound of selected from Table 2.15. A pharmaceutical composition comprised of a compound of and a pharmaceutically acceptable carrier claim 1 , glidant claim 1 , diluent claim 1 , or excipient.16. The pharmaceutical composition according to claim 15 , further comprising a therapeutic agent.17. A process for making a pharmaceutical composition which comprises combining a compound of with a pharmaceutically acceptable carrier.18. A method of treating a disease or disorder which comprises administering a therapeutically effective amount of the pharmaceutical composition of to a patient with a disease or disorder selected from immune disorders claim 15 , cancer claim 15 , cardiovascular disease claim 15 , viral infection claim 15 , inflammation claim 15 , metabolism/endocrine function disorders and neurological disorders claim 15 , and mediated by Bruton's tyrosine kinase.19. The method of wherein the disease or disorder is an immune disorder.20. The method of wherein the immune disorder is ...

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16-05-2013 дата публикации

Organic Electroluminescent Element, Material for Organic Electroluminescent Element, and Light Emitting Device, Display Device and Illumination Device Each Using the Element

Номер: US20130119359A1
Принадлежит: UDC IRELAND LIMITED

The disclosure relates to organic electroluminescent elements, materials for use in the elements, and devices using the elements, which include a compound represented by the following General Formula (1): 2. The organic electroluminescent element according to claim 1 , wherein in the General Formula (1) Rto Rare each selected from a hydrogen atom claim 1 , an alkyl group claim 1 , an aryl group claim 1 , a heteroaryl group claim 1 , —NYY claim 1 , —OY claim 1 , —SY claim 1 , a halogen atom claim 1 , and a silyl group claim 1 , and{'sup': 1', '4, 'wherein Yto Yeach independently represents an alkyl group, an aryl group or a heteroaryl group, and which may further have substituents.'}6. The organic electroluminescent element according to claim 4 , wherein in the General Formula (3) Land Leach independently represents an arylene group or a heteroarylene group.14. The organic electroluminescent element according to claim 1 , wherein the light emitting layer includes an anthracene-based host material.15. The organic electroluminescent element according to claim 1 , wherein the light emitting layer is formed by a vacuum deposition process.16. The organic electroluminescent element according to claim 1 , wherein the light emitting layer is formed by a wet process.17. A light emitting device comprising the organic electroluminescent element according to .18. A display device comprising the organic electroluminescent element according to .19. An illumination device comprising the organic electroluminescent element according to . This application claims the benefit of priority to Japanese Patent Application No. 2011-250945, filed Nov. 16, 2011, which is incorporated herein by reference in its entirety.The present invention relates to an organic electroluminescent element and a material for an organic electroluminescent element which can be used in the same. The present invention also relates to a light emitting device, a display device, or an illumination device each using ...

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16-05-2013 дата публикации

COMPLIMENTARY POLYMER ELECTROCHROMIC DEVICE

Номер: US20130120821A1
Принадлежит: ASHWIN-USHAS CORPORATION, INC.

A complimentary polymer or “dual-polymer” electrochromic device and methods of preparing the same are provided. 1. A complimentary electrochromic device comprising:(a) a first electrode comprising a cathodically coloring conducting polymeric material, the cathodically coloring conducting polymeric material comprising a substituted or unsubstituted 2,2-dibenzyl-3,4-propylenedioxythiophene monomer;(b) a second electrode comprising an anodically coloring conducting polymeric material;(c) an electrolyte disposed between and in electrochemical communication with the first electrode and the second electrode; andwherein the redox potential of the cathodically coloring conducting polymeric material is substantially matched to the redox potential of the anodically coloring conducting polymeric material such that when one said polymeric material is fully oxidized, the other said polymeric material is fully reduced.2. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene is para substituted with a substituent selected from the group consisting of halo claim 1 , sulfonyl claim 1 , nitro claim 1 , and alkyl.3. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene has a substituent selected from the group consisting of chloro and bromo.4. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene has a substituent selected from the group consisting of n-propyl claim 1 , iso-propyl claim 1 , n-butyl claim 1 , iso-butyl claim 1 , n-pentyl claim 1 , and n-hexyl.5. The electrochromic device of claim 1 , wherein at least one benzyl moiety of the substituted 2 claim 1 ,2-dibenzyl-3 claim 1 ,4-propylenedioxythiophene has an amino substituent.6. The electrochromic device of claim 1 , wherein the ...

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16-05-2013 дата публикации

ACC INHIBITORS AND USES THEREOF

Номер: US20130123231A1
Принадлежит: Nimbus Apollo, Inc.

The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same. 2. The compound according to claim 1 , wherein X is —S—.3. The compound according to claim 2 , wherein Ris methyl or trifluoromethyl.4. The compound according to claim 3 , wherein Ris halogen claim 3 , —C(O)OR claim 3 , —C(O)N(R) claim 3 , or oxazolyl.5. The compound according to claim 3 , wherein Rand Rare taken together to form a 5-6 membered partially unsaturated carbocyclic ring.6. The compound according to claim 3 , wherein Ris tetrazolyl claim 3 , —C(O)OR claim 3 , —C(O)N(R) claim 3 , or —OR.10. A composition comprising a compound according to and a pharmaceutically acceptable carrier claim 1 , adjuvant claim 1 , or vehicle.11. A method of inhibiting ACC in a patient in need thereof claim 10 , comprising administering to said patient the composition according to .12. A method of inhibiting ACC in a biological sample claim 1 , comprising contacting the biological sample with the compound according to .13. A method for treating a metabolic disorder in a patient in need thereof claim 10 , comprising administering to said patient the composition according to .14. The method according to claim 13 , wherein the metabolic disorder is obesity.15. The method according to claim 13 , wherein the metabolic disorder is dyslipidemia or hyperlipidemia.16. The method according to claim 14 , wherein the obesity is a symptom of Prader-Willi syndrome claim 14 , Bardet-Biedl syndrome claim 14 , Cohen syndrome or MOMO syndrome.17. The method according to claim 14 , wherein the obesity is a side effect of the administration of another medication claim 14 , including but not limited to insulin claim 14 , sulfonylureas claim 14 , thiazolidinediones claim 14 , antipsychotics claim 14 , antidepressants claim 14 , steroids claim 14 , anticonvulsants (including phenyloin and valproate) claim 14 , pizotifen claim 14 , or hormonal ...

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16-05-2013 дата публикации

AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS

Номер: US20130123232A1
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: 119.-. (canceled)21. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 20 , a pharmaceutically acceptable excipient claim 20 , and a pharmaceutically acceptable diluent.22. A pharmaceutical composition of claim 21 , wherein the composition is a solid oral dosage form.23. A pharmaceutical composition of claim 21 , wherein the composition is a syrup claim 21 , an elixir claim 21 , or a suspension. This application claims priority to U.S. provisional patent application Nos. 61/171,658 and 61/171,649, each filed Apr. 22, 2009, which are hereby incorporated by reference in their entirety.The research and development of the invention described below was not federally sponsored.has been used for the treatment of pain for many years. Δ-tetrahydrocannabinol is a major active ingredient from and an agonist of cannabinoid receptors (Pertwee, 2008, 153, 199-215). Two cannabinoid G protein-coupled receptors have been cloned, cannabinoid receptor type 1 (CBMatsuda et al., 1990, 346, 561-4) and cannabinoid receptor type 2 (CBMunro et al., 1993, 365, 61-5). CBis expressed centrally in brain areas, such as the hypothalamus and nucleus accumbens as well as peripherally in the liver, gastrointestinal tract, pancreas, adipose tissue, and skeletal muscle (Di Marzo et al., 2007, 18, 129-140). CBis predominantly expressed in immune cells, such as monocytes (Pacher et al., 2008, 294, H1133-H1134), and under certain conditions, also in the brain (Benito et al., 2008, 153, 277-285) and in skeletal (Cavuoto et al., 2007, 364, 105-110) and cardiac (Hajrasouliha et al., 2008, 579, 246-252) muscle. An abundance of pharmacological, anatomical and electrophysiological data, using synthetic agonists, indicate that increased cannabinoid ...

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16-05-2013 дата публикации

NOVEL CCR2 RECEPTOR ANTAGONISTS, METHOD FOR PRODUCING THE SAME, AND USE THEREOF AS MEDICAMENTS

Номер: US20130123241A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases. 2. The compound of formula (I) according to claim 1 ,wherein HET is a group according to formula (IIa),{'sub': 1', '7', '6, 'wherein Ris —H, and wherein Ris —C-aryl,'}{'sub': 7', '3', '1', '6', '1', '6, 'and wherein the ring Ris optionally substituted with one or more groups selected from among —CF, —C-C-alkyl, —O—C-C-alkyl, and -halogen'}{'sub': '16', 'and wherein Ris -hydrogen;'}{'sub': 7', '1', '4, 'or wherein Rand Ron two neighbouring ring atoms together form a —C-alkenylene group, such that an annellated aromatic ring is formed, in which one carbon center may optionally be replaced by 1 nitrogen atom,'}{'sub': 1', '3', '3', '3, 'wherein the resulting annelated ring being optionally substituted by one or more groups selected from among —C-C-alkyl, —CN, —CF, —OCF, and -halogen,'}{'sub': '16', 'and wherein Ris a group selected from -hydrogen, and ═O;'}{'sub': 7', '1', '1, 'or wherein Rand Ron two neighbouring ring atoms together form a —C-alkylene group such that an annellated ring is formed,'}{'sub': 5', '10, 'wherein the resulting annelated ring being optionally substituted by a group of the structure —C-C-aryl,'}{'sub': '16', 'and wherein Ris -hydrogen;'}{'sub': 7', '5', '5', '4', '2', '1', '3', '1', '6', '3', '3', '5', '10, 'or wherein Ris a group selected from among spiro —C-cycloalkenyl, and spiro —C-heterocyclyl, wherein said spirocyclic ring being optionally substituted on two neighbouring ring atoms by a —C-alkenylene group, such that an annellated aromatic ring is formed, wherein the aromatic ring being optionally substituted by one or more groups selected from among —OH, —NH, —C-C-alkyl, —O—C-C-alkyl, —CN, —CF, —OCF, halogen, —C-C- ...

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16-05-2013 дата публикации

COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM

Номер: US20130123265A1
Принадлежит: CalciMedica, Inc.

Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity. 2. The compound of claim 1 , wherein:{'sup': '1', 'Ris hydrogen, methyl, ethyl, n-propyl or iso-propyl.'}3. The compound of or claim 1 , wherein:{'sup': 4', '8, 'sub': 2', '3', '3', '1', '6', '1', '6', '1', '6', '3', '8', '1', '6, 'Ris a phenyl, optionally substituted with at least one substituent selected from F, Cl, Br, I, —CN, —NO, —CF, —OH, —OR, —OCF, C-Calkyl, C-C-fluoroalkyl, C-Cheteroalkyl, C-Ccycloalkyl, and C-Chaloalkyl.'}54. The compound of any of claim 1 , claim 1 , or claim 1 , wherein:{'sup': 4', '8', '9', '9', '9', '9', '9', '8', '9', '9', '9', '8', '9', '8', '9', '9', '8', '8, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'Ris substituted with at least one substituent selected from —NHS(═O)R, —S(═O)N(R), —N(R)S(═O)N(R), —N(R), —N(R)C(═O)R, —N(R)C(═O)N(R), —N(R)C(═O)OR, —COR, —C(═O)R, —OC(═O)N(R), —CON(R), —SR, or —S(═O)R.'}6. The compound of claim 1 , wherein:{'sup': '4', 'Ris selected from phenyl; 2-fluorophenyl; 3-fluorophenyl; 4-fluorophenyl; 2-chlorophenyl; 3-chlorophenyl; 4-chlorophenyl; 2,4-dichlorophenyl; 2,3-dichlorophenyl; 3,4-dichlorophenyl; 3,5-dichlorophenyl; 2-bromophenyl; 3-bromophenyl; 4-bromophenyl; 2-iodophenyl; 3-iodophenyl; 4-iodophenyl; 2-methylphenyl; 3-methylphenyl; 4-methylphenyl; 2,4-dimethylphenyl; 2,3-dimethylphenyl; 3,4-dimethylphenyl; 3,5-dimethylphenyl; 2-trifluoromethylphenyl; 3-trifluoromethylphenyl;'}{'b': '4', 'and -trifluoromethylphenyl.'}76. The compound of - claims 1 , wherein:{'sup': 2', '8, 'sub': 2', '3', '3', '1', '6', '1', '6', '1', '6', '3', '8', '1', '6, 'Ris a phenyl, optionally substituted with at least one ...

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16-05-2013 дата публикации

Crystal of thienopyrimidine derivative

Номер: US20130123279A1
Принадлежит: Aska Pharmaceutical Co Ltd

Crystals are obtained by heating an aqueous suspension of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid. Novel crystals are obtained by adjusting the heating temperature and/or duration.

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23-05-2013 дата публикации

Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections

Номер: US20130129677A1
Принадлежит: Siga Technologies Inc

Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.

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23-05-2013 дата публикации

PYRAZINE KINASE INHIBITORS

Номер: US20130131040A1
Принадлежит: Portola Pharmaceuticals, Inc.

Provided are pyrazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity. 2. A compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is H.3. A compound of or claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.4. A compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , isopropyl claim 1 , sec-butyl claim 1 , tert-butyl claim 1 , methyl claim 1 , ethyl claim 1 , CFCH— claim 1 , CHFCH— claim 1 , methoxymethylene claim 1 , methylsulfinylethylene claim 1 , and methylsulfonylethylene.5. A compound of any one of to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Ccycloalkyl claim 1 , CcycloalkylCalkylene claim 1 , aryl claim 1 , arylCalkylene or heteroarylCalkylene each of which is optionally substituted with one to five groups independently selected from halo claim 1 , C-Calkyl claim 1 , and amino.6. A compound of or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris selected from the group consisting of cyclopropyl claim 5 , cyclopropylmethylene claim 5 , phenyl and benzyl.7. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Rand Rare independently selected from the group consisting of Calkyl and Calkoxy.8. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein V is heteroaryl optionally substituted with one to five Rgroups.9. A compound of any one of to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein V is cycloalkyl optionally substituted with one to five Rgroups.10. A compound of any one of to claim 5 , or a ...

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23-05-2013 дата публикации

NOVEL PSYCHOTROPIC AGENTS HAVING GLUTAMATE NMDA ACTIVITY

Номер: US20130131048A1
Принадлежит: Ramot at Tel-Aviv University Ltd.

The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders. 1. A compound , or a salt or stereoisomer thereof , of the general formula L-M-V , whereinL is a central nervous system (CNS) active moiety selected from the group consisting of clozapine and quetiapine;{'sub': 1', '8', '3', '8', '2', '2', '2', 'n', '2', 'n', '2', 'n', '2', '2', 'n', '1', '4', '2', '4', '2', '4, 'M is optionally present and is a linker selected from the group consisting of —NH—, —O—, —S—, C-C-alkylene, C-C-cycloalkylene, —CH—O—CH, —(CH)—O—(CH)—, —(CH—O)—, and —(CHCH—O)—, said alkylene and cycloalkylene being optionally substituted by one or more groups selected from the group consisting of C-Calkyl, C-Calkenyl, and C-Calkynyl;'}V is a modulator of a glutamate N-methyl-D-aspartate (NMDA) receptor selected from the group consisting of an amino acid, an ester of the amino acid, an amide of the amino acid, and an alkylated amine of the amino acid; wherein said amino acid is selected from the group consisting of glycinyl, sarcosinyl, serinyl, and cysteinyl; andn, independently of each other, is an integer from 0 to 3.2. The compound claim 1 , or a salt or stereoisomer thereof claim 1 , according to claim 1 , wherein said linker is selected from the group consisting of —NH— claim 1 , —O— claim 1 , —S— claim 1 , —(CH)— wherein m is an integer between 1 and 8 claim 1 , —(CH—CH═CH—CH)— claim 1 , —(CH═CH—CH—CH)— claim 1 , —(CH—CH═CH—CH—CH—CH)— claim 1 , —(CH—C≡C—CH)— claim 1 , —(C≡C—CH—CH)— claim 1 , —(CH—NH—CH═CH—CH)— claim 1 , —(CH—NH—CH—CH—CH)— claim 1 , —(CH—O—CH—CH)— claim 1 , —(CH)—O—(CH)— claim 1 , —CH—O—CH claim 1 , —(CH—O)— claim 1 , and —(CHCH—O)— wherein n is an integer from 0 to 3 claim 1 , and substituted derivatives thereof.3. The compound claim 1 , or a salt or stereoisomer thereof claim 1 , according to claim 1 , wherein the bonds between M and L and between M and V are non-hydrolizable.5. A ...

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23-05-2013 дата публикации

PYRIDAZINONES AND FURAN-CONTAINING COMPOUNDS

Номер: US20130131062A1
Принадлежит:

The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries. 2. The compound according to claim 1 , wherein 4 claim 1 ,5-dichloro-2-m-tolyl-2H-pyridazin-3-one is specifically excluded.3. The compound according to claim 1 , wherein Rand Rare the same claim 1 , Ris hydrogen claim 1 , halo claim 1 , optionally substituted acyl claim 1 , optionally substituted heterocyclic claim 1 , optionally substituted aryl claim 1 , optionally substituted heteroaryl claim 1 , or optionally substituted hydroxy.4. The compound according to claim 3 , wherein Rand Rare both hydrogen.5. The compound according to claim 3 , wherein Rand Rare both chloro claim 3 , bromo claim 3 , iodo claim 3 , or fluoro.6. The compound according to claim 3 , wherein Rand Rare both optionally substituted hydroxy.7. The compound according to claim 3 , wherein Rand Rare both optionally substituted thio.8. The compound according to claim 3 , wherein Rand Rare both optionally substituted amino.9. The compound according to claim 3 , wherein Rand Rare both optionally substituted aliphatic.10. The compound according to claim 3 , wherein Rand Rare both optionally substituted heterocyclic.11. The compound according to claim 3 , wherein Rand Rare both cyano.12. The compound according to claim 1 , wherein Rand Rare the different claim 1 , Ris hydrogen claim 1 , halo claim 1 , optionally substituted acyl claim 1 , optionally substituted heterocyclic claim 1 , optionally substituted aryl claim 1 , optionally substituted heteroaryl claim 1 , or optionally substituted hydroxy.13. The compound ...

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23-05-2013 дата публикации

1-Aryl or 1- Heteroaryl-Pyrido(B)indoles and Uses Thereof

Номер: US20130131070A1
Автор: Buolamwini John K.
Принадлежит:

Provided are 1-aryl or 1-heteroaryl substituted beta-carboline compounds or indole analogs thereof having the structure: 2. The substituted β-carboline compound of claim 1 ,wherein X is NH;{'sup': '1', 'Ris 1-naphthyl optionally substituted with Br or F; and'}{'sup': 2', '3', '4', '5', '6', '7, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4, 'R, R, R, R, R, and Rare independently H, OH, halogen, CN, C-Calkyl, C-Calkoxy, C-Chaloalkoxy, —C(O)OC-Cester, —(C-C)—SO—NH—(C-C) sulfonamide, or phenyl;'}{'sup': 5', '6', '7', '2', '3', '4', '5', '6', '7', '2', '3', '4', '5', '6', '7, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4, 'wherein, when one of R, R, or Ris C-Calkoxy, then R, R, R, R, R, and Rare independently H, OH, halogen, CN, C-Chaloalkoxy, —C(O)OC-Cester, —C-C—SO—NH—C-Csulfonamide, or phenyl such that at least two of R, R, R, R, R, and Rare other than H.'}3. The substituted β-carboline compound of claim 1 ,wherein X is NH;{'sup': '1', 'Ris 1-dihydroacenaphthenyl optionally substituted with Br or F; and'}{'sup': 2', '3', '4', '5', '6', '7, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4, 'R, R, R, R, R, and Rare independently H, OH, halogen, CN, C-Calkyl, C-Calkoxy, phenyl, C-Chaloalkoxy, —C(O)OC-Cester, —(C-C)—SO—NH—(C-C) sulfonamide, or phenyl.'}4. The substituted β-carboline compound of claim 1 ,{'sub': '3', 'wherein X is N—CH, S, or O;'}{'sup': '1', 'Ris 1-naphthyl or 1-dihydroacenaphthenyl each optionally substituted with Br or F; and'}{'sup': 2', '3', '4', '5', '6', '7, 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '2', '1', '4, 'R, R, R, R, R, and Rare independently H, OH, halogen, CN, C-Calkyl, C-Calkoxy, phenyl, C-Chaloalkoxy, —C(O)OC-Cester, —C-C—SO—NH—C-Csulfonamide or phenyl.'}5. A pharmaceutical composition comprising the substituted β-carboline compound of and a pharmaceutically effective carrier.6. A method for inhibiting proliferation of cells associated with a cell proliferative ...

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06-06-2013 дата публикации

NOVEL COMPOUNDS AND THERAPEUTIC USE THEREOF FOR PROTEIN KINASE INHIBITION

Номер: US20130143887A1
Автор: WU Zhanggui
Принадлежит:

Novel compound having the following formula: 117-. (canceled)19. The method according to claim 18 , wherein the cancer to be treated is selected from the group consisting of lung cancer claim 18 , liver cancer claim 18 , leucocythaemia claim 18 , osteocarcinoma claim 18 , pancreas cancer claim 18 , skin cancer claim 18 , melanoma claim 18 , metrocarcinoma claim 18 , oophoroma claim 18 , rectal carcinoma claim 18 , gastric carcinoma claim 18 , colon cancer claim 18 , breast carcinoma claim 18 , salpinx carcinoma claim 18 , endometrial carcinoma claim 18 , cervix carcinoma claim 18 , vagina carcinoma claim 18 , carcinoma of vulva claim 18 , esophagus carcinoma claim 18 , small intestine carcinoma claim 18 , incretion carcinoma claim 18 , soft tissue sarcoma claim 18 , urethra carcinoma claim 18 , prostatic cancer claim 18 , lymphocytoma claim 18 , bladder cancer claim 18 , nephridium cancer claim 18 , tumors of vertebral column claim 18 , tumors in the neuroglia of the brain claim 18 , and pituitary adenoma. The present application is a divisional application of U.S. application Ser. No. 12/349,888 which claims priority to Chinese Patent application No. CN200810000936.9, filed on Jan. 8, 2008, the entire specification, drawings, and disclosure of which are incorporated herein by reference for all purposes.The invention is directed to compounds, pharmaceutical compositions comprising same, and method using the same to inhibit protein kinase. The invention is further directed to methods of synthesis of the compounds and compositions.A major threat to human health is cancer, and worldwide at least 5 million people die from cancer annually. Most cancers in humans are caused by environmental factors. Although certain methods of cancer treatment are available, such as surgery, radiotherapy, and chemotherapy, the rate of success is still quite limited. Among available methods of treatment, chemotherapy is one of the most effective.One category of cancer chemotherapy agents ...

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13-06-2013 дата публикации

Derivatives of 1-Phenyl-1,5-Dihydro-Benzo[B] [1,4]Diazepine-2,4-Dione as Inhibitors of HIV Replication

Номер: US20130150350A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of formula (I) wherein m, R, R, R, X and Y are defined herein, are useful as inhibitors of HIV replication. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris phenyl.3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris thiophene.4. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 1 and Ris selected from Cl claim 1 , F claim 1 , CHand CF.5. The compound according to claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Ris CF.6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H or (C)alkyl.12. (canceled)13. A pharmaceutical composition comprising a a compound of formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , according to and a pharmaceutically acceptable carrier.14. (canceled)15. A method for treating HIV which comprises administering to a host infected by HIV a therapeutically effective amount of a compound according to . This application claims benefit of U.S. Ser. No. 61/305,108, filed Feb. 16, 2010, herein incorporated by reference.The present invention relates to compounds and their use as inhibitors of capsid assembly, pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of human immunodeficiency virus (HIV) infection.To date, over 20 FDA-approved drugs make up the antiretroviral arsenal against HIV (1). These compounds generally target the viral enzymes or the viral entry process and can be divided within 6 mechanistic classes. The standard of care is a multi-drug therapeutic regime, often referred to as highly active antiretroviral therapy (HAART), where combinations of at least three drugs targeting the virus are administered. Although HAART can successfully restrict viral replication for many years, drug resistance can still ...

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13-06-2013 дата публикации

Acyl Piperazine Derivatives as TTX-S Blockers

Номер: US20130150356A1
Принадлежит: Raqualia Pharma Inc.

The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. 2. The compound as claimed in wherein{'sub': 1', '6', '3', '8, 'R is selected from the group consisting of: (1) C-Calkyl and (2) C-Ccycloalkyl; which may be optionally substituted with 1 to 3 substituents independently selected from the group consisting of'}{'sub': 1', '6', '3', '8', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '8', '0', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '3', '6', '1', '6', '1', '6', '1', '6, 'sup': A', 'B', 'A', 'B, '(1) halogen, (2) C-Calkyl, (3) C-Ccycloalkyl, (4) hydroxy, (5) C-Calkoxy, (6) amino, (7) C-Calkylamino, (8) di(C-Calkyl)amino, (9) hydroxy C-Calkyl, (10) C-Calkylsulfonyl, (11) aminosulfonyl, (12) C-Calkyl C(═O)—, (13) RN(R)C(═O)—, (14) C-Calkylsulfonylamino, (15) C-Ccycloalkyl, (16) RC(═O)N(R)—, and (17) 5 to 10 membered aryl C-Calkyl; wherein said aryl may be optionally substituted with 1 to 5 substituents independently selected from the group consisting of hydroxy, halogen, C-Calkyl, C-Calkoxy, hydroxy C-Calkyl, amino C-Calkyl, C-Chaloalkyl, C-Chaloalkoxy, C-Ccycloalkyl, amino, C-Calkylamino, di(C-Calkyl)amino, C-Calkylthio, and nitro;'}{'sup': 3', '4, 'p is 0, 1, or 2; when p is one or more than one, Rand Rmay be same or different;'}q is 0, or 1; when p is 0, then q is 0;X is —O—;or a prodrug thereof or a pharmaceutically acceptable salt thereof.3. The compound as claimed in wherein R is selected from the group consisting of: (1) C-Calkyl and (2) C-Ccycloalkyl; which ...

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