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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 38207. Отображено 100.
05-01-2012 дата публикации

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

Номер: US20120003229A1
Принадлежит: Individual

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

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05-01-2012 дата публикации

NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE

Номер: US20120004213A1
Принадлежит: Forest Laboratories Holdings Ltd

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

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12-01-2012 дата публикации

Broad spectrum benzothiophene-nitrothiazolide and other antimicrobials

Номер: US20120010187A1

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

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19-01-2012 дата публикации

Taspase1 inhibitors and their uses

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

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

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26-01-2012 дата публикации

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

Номер: US20120022076A1
Принадлежит: Individual

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

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26-01-2012 дата публикации

Compositions and methods for the treatment of pathological condition(s) related to gpr35 and/or gpr35-herg complex

Номер: US20120022116A1
Принадлежит: Corning Inc

Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject. The compounds having a formula (I), (II) or (III):

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02-02-2012 дата публикации

Derivatives of aminocyclobutane or aminocyclobutene, their method of preparation and their use as medical products

Номер: US20120029013A1
Принадлежит: Pierre Fabre Medicament SA

The present invention concerns compounds of general formula (1), where in:—-a- is a single or double bond, Ar is an aromatic group, substituted or unsubstituted, R1 and R2 each independently or together are: a hydrogen atom or C 1 -C 6 alkyl group, branched or unbranched, saturated or unsaturated, substituted or unsubstituted; the groups R1 and R2 may also form a heterocycle, R3 and R3′ each independently or together are a hydrogen atom or C 1 -C 6 alkyl group, X is an oxygen atom or a sulphur atom, and the addition salts of the compounds of general formula (1) with pharmaceutically acceptable mineral acids or organic acids.

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16-02-2012 дата публикации

Novel Methods for Regeneration of Solvents for Extractive Processes

Номер: US20120037542A1
Принадлежит: AMT International Inc, CPC Corp Taiwan

An improved solvent regeneration system for extractive distillation and liquid-liquid extraction processes capable of effectively removing heavy hydrocarbons and polymeric materials that otherwise develop in a closed solvent loop. The improved process employs a light hydrocarbon displacement agent, which is at least partially soluble in the solvent to squeeze the heavy hydrocarbons and polymeric materials out of the solvent, with virtually no additional energy requirement. It has been demonstrated that the light non-aromatic hydrocarbons in the raffinate stream generated from the extractive distillation or the liquid-liquid extractive process for aromatic hydrocarbons recovery can displace not only the heavy non-aromatic hydrocarbons but also the heavy aromatic hydrocarbons from the extractive solvent, especially when the aromatic hydrocarbons in the solvent are in the C 10+ molecular weight range.

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23-02-2012 дата публикации

Developers and method of coloring lithographic printing members

Номер: US20120045720A1
Принадлежит: Individual

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

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

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

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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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05-04-2012 дата публикации

Novel Compounds, Pharmaceutical Compositions Containing Same, Methods of Use for Same, and Methods for Preparing Same

Номер: US20120083471A1
Принадлежит: JOHNS HOPKINS UNIVERSITY

The present invention relates to novel pharmaceutical compositions containing the same, and methods of use for a variety of therapeutically valuable uses including, but not limited to, treating obesity by inhibiting the activity of Glycerol 3-phosphate acyltransferase (GPAT).

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19-04-2012 дата публикации

Organic Compounds Having Cooling Properties

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

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

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03-05-2012 дата публикации

Novel microbiocides

Номер: US20120108645A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

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

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

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

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10-05-2012 дата публикации

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

Номер: US20120115915A1
Принадлежит: Harvard College

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

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17-05-2012 дата публикации

Libraries of n-substituted-n-phenylethylsulfonamides for drug discovery

Номер: US20120122920A1

New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

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17-05-2012 дата публикации

Process for the preparation of strontium ranelate

Номер: US20120123131A1
Принадлежит: Individual

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

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24-05-2012 дата публикации

Materials for organic electroluminescent devices

Номер: US20120126179A1
Принадлежит: Merck Patent GmBH

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

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24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Принадлежит: Janssen Pharmaceutica NV

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

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07-06-2012 дата публикации

Light-emitting device material and light-emitting device

Номер: US20120138907A1
Принадлежит: TORAY INDUSTRIES INC

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

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07-06-2012 дата публикации

Proteasome inhibitors having chymotrypsin-like activity

Номер: US20120142917A1

Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl 4 . The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.

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07-06-2012 дата публикации

Method for synthesis of secondary alcohols

Номер: US20120142934A1
Принадлежит: National Tsing Hua University NTHU

A method for synthesis of secondary alcohols is provided for pharmaceutical secondary alcohol by addition of organoboronic acids with aldehydes in presence of the cobalt ion and bidentate ligands as the catalyst. In addition, an enantioselective synthesis method for secondary alcohols is also herein provided in the present invention. The present invention has advantages in using less expensive cobalt ion and commercially available chiral ligands as the catalyst, wide scope of organoboronic acids and aldehydes compatible with this catalytic reaction and achieving excellent yields and/or enantiomeric excess.

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14-06-2012 дата публикации

(e)-n-monoalkyl-3-oxo-3-(2-thienyl) propenamine and process for producing the same and process for producing (e,z)-n-monoalkyl-3-oxo-3-(2-thienyl) propenamine

Номер: US20120149917A1
Принадлежит: Sumitomo Seika Chemicals Co Ltd

The present invention provides a process for producing (E)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine represented by Formula (1); wherein R is a C 1-4 alkyl, the method comprising the steps of: maintaining a solution containing (Z)—N-monoalkyl-3-oxo-3-(2-thienyl)propenamine dissolved therein at 25° C. or below to deposit crystals and separating crystals having a particle diameter of 100 μm or less from the deposited crystals; and a process for producing (E,Z)—N-monoalkyl-3-oxo-3-(2-thienyl)propenamine comprising the steps of: reacting an alkali metal salt of β-oxo-β-(2-thienyl)propanal with a monoalkylamine compound; adding a water-insoluble organic solvent to the resulting reaction mixture; adding seed crystals containing (E)-N-monoalkyl-3-oxo-3-(2-thienyl)propenamine to an organic layer obtained by conducting separation; and keeping the resulting mixture at 25° C. or below.

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21-06-2012 дата публикации

Phosphorous derivatives as chemokine receptor modulators

Номер: US20120157413A1
Принадлежит: Allergan Inc

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

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21-06-2012 дата публикации

Novel thiophene compounds for use in therapy

Номер: US20120157516A1
Принадлежит: BioChromix Pharma AB

The present invention relates to novel substituted thiophene derivatives useful in therapy of diseases related to misfolded and aggregated proteins.

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05-07-2012 дата публикации

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

Номер: US20120172599A1
Принадлежит: Individual

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

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02-08-2012 дата публикации

Glycine transporter-1 inhibitors

Номер: US20120195985A1
Принадлежит: AMGEN INC

The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT-1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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09-08-2012 дата публикации

NP-1 Antagonists and Their Therapeutic Use

Номер: US20120201749A1
Принадлежит: Ark Therapeutics Ltd

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

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09-08-2012 дата публикации

Substituted 4-aminocyclohexane derivatives

Номер: US20120202810A1
Принадлежит: GRUENENTHAL GmbH

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

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23-08-2012 дата публикации

Viral polymerase inhibitors

Номер: US20120214783A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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23-08-2012 дата публикации

Heteroaryls and uses thereof

Номер: US20120214794A1
Принадлежит: Millennium Pharmaceuticals Inc

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

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23-08-2012 дата публикации

High Stability Diionic Liquid Salts

Номер: US20120215005A1
Принадлежит: Sigma Aldrich Co LLC

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

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30-08-2012 дата публикации

Guanidine-containing compounds useful as muscarinic receptor antagonists

Номер: US20120219509A1
Принадлежит: Theravance Inc

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

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30-08-2012 дата публикации

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

Номер: US20120220592A1
Принадлежит: Newron Pharmaceuticals SpA

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

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06-09-2012 дата публикации

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

Номер: US20120225890A1
Принадлежит: ProteoTech Inc

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

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13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
Принадлежит: Sarcode Bioscience Inc

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

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01-11-2012 дата публикации

Novel heterocyclic acrylamides and their use as pharmaceuticals

Номер: US20120277207A1
Принадлежит: FAB PHARMA Sas

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

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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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29-11-2012 дата публикации

Thiophene analogues for the treatment or prevention of flavivirus infections

Номер: US20120301430A1
Принадлежит: Vertex Pharmaceuticals Inc

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

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29-11-2012 дата публикации

Novel sulfamides exhibiting neuroprotective action and methods for use thereof

Номер: US20120302546A1

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

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13-12-2012 дата публикации

Chiral Diacylhydrazine Ligands for Modulating the Expression of Exogenous Genes via an Ecdysone Receptor Complex

Номер: US20120316066A1
Принадлежит: Intrexon Corp

The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.

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20-12-2012 дата публикации

Heterocyclic sulfonamides, uses and pharmaceutical compositions thereof

Номер: US20120322823A1
Принадлежит: PFIZER INC

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

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27-12-2012 дата публикации

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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17-01-2013 дата публикации

Synthesis and applications of soluble pentacene precursors and related compounds

Номер: US20130017497A1
Принадлежит: Academia Sinica

The present disclosure relates to methods and systems for synthesis of bridged-hydropentacene, hydroanthracene and hydrotetracene from the precursor compounds pentacene derivatives, tetracene derivatives, and anthracene derivatives. The invention further relates to methods and systems for forming thin films for use in electrically conductive assemblies, such as semiconductors or photovoltaic devices.

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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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14-02-2013 дата публикации

Novel naphthothiophene compound and organic light-emitting device including the same

Номер: US20130037789A1
Принадлежит: Canon Inc

The present invention provides a novel naphthothiophene compound having a high lowest excited triplet level (T1).

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28-02-2013 дата публикации

Inhibitors of flaviviridae viruses

Номер: US20130052161A1
Автор: William J. Watkins
Принадлежит: Gilead Sciences Inc

Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections (e.g. hepatitis C infections), particularly drug resistant Flaviviridae virus infections.

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28-02-2013 дата публикации

Substituted benzofurans, benzothiophenes, benzoselenophenes and indoles and their use as tubulin polymerisation inhibitors

Номер: US20130053351A1
Принадлежит: Bionomics Ltd

The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerisation inhibitors.

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21-03-2013 дата публикации

Propynoic Acid Carbamoyl Methyl-Amides and Pharmaceutical Compositions and Methods Based Thereon

Номер: US20130071328A1
Принадлежит: UNIVERSITY OF SOUTHERN CALIFORNIA

This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2. 4. A compound according to claim 1 , wherein said compound further contains a substituent capable of being used in a biological or medical diagnostic imagining technique to quantify or identify associated biomarker proteins.5. A compound according to claim 3 , wherein said compound further contains a substituent capable of being used in a biological or medical diagnostic imagining technique to quantify or identify associated biomarker proteins.7. A pharmaceutical composition comprising any of the compounds of to and a pharmaceutically acceptable carrier.8. A method for treatment a cancer subject claim 3 , comprising the step of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'administering to a person in need of said treatment method an effective amount of the pharmaceutical composition according to .'}9. A method of claim 8 , where the cancer is: breast cancer claim 8 , ovarian cancer claim 8 , prostate cancer claim 8 , colon cancer claim 8 , brain cancer claim 8 , pancreatic cancer claim 8 , skin cancer claim 8 , lung cancer claim 8 , and multiple myeloma.10. A method for promoting the release and nuclear localization of the transcription factor Nrf2 comprising the step of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'administering an effective amount of the pharmaceutical compositions according to .'}10. A biological or medical diagnostic imaging technique claim 8 , comprising:{'claim-ref': [{'@idref': 'CLM-00004', 'claims 4 ...

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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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28-03-2013 дата публикации

NOVEL ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20130076604A1
Принадлежит: CANON KABUSHIKI KAISHA

Provided are a novel organic compound appropriate for emission of green light and an organic light-emitting device including the organic compound. Provided is a substituted or unsubstituted indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene appropriate for emission of green light. The substituents of the indeno[1,2,3-cd]naphtho[2,3-k]fluoranthene are each independently selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted amino group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocyclic group. 2. The organic compound according to claim 1 , wherein Rto Rare each independently selected from a hydrogen atom and a substituted or unsubstituted aryl group.4. An organic light-emitting device comprising:an anode;a cathode; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an organic compound layer disposed between the anode and the cathode, the organic compound layer containing the organic compound according to .'}5. An organic light-emitting device comprising:an anode;a cathode; and{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'an organic compound layer disposed between the anode and the cathode, the organic compound layer containing the organic compound according to .'}6. The organic light-emitting device according to claim 4 , wherein the organic compound layer is a light-emitting layer.7. The organic light-emitting device according to claim 6 , wherein the organic light-emitting device emits green light.8. A display apparatus having a plurality of pixels claim 4 , each including the organic light-emitting device according to and a switching device connected to the organic light-emitting device.9. An image input apparatus comprising:an image input unit configured to input an image; and{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'a display unit configured to display the image, the display unit having a plurality of pixels, each ...

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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

6,13-DIHALOGEN-5,14-DIHYDROPENTACENE DERIVATIVE AND METHOD FOR PRODUCING 6,13-SUBSTITUTED-5,14-DIHYDROPENTACENE DERIVATIVE USING SAME

Номер: US20130079530A1
Принадлежит:

The present invention provides a 6,13-dihalogen-5,14-dihydropentacene derivative and a method for production thereof. Compounds (b) and (c) are reacted through cross-coupling reaction in the presence of a metal compound and a lithiating agent to synthesize compound (d), which is then halogenated to thereby obtain a 6,13-dihalogen-5,14-dihydropentacene derivative (compound (e)). 2. The derivative according to claim 1 , wherein Xand Xare each an iodine atom.3. The derivative according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand R claim 1 , which may be the same or different claim 1 , are each independently a hydrogen atom; an optionally substituted C-Calkyl group; an optionally substituted C-Caryl group or an optionally substituted silyl group.4. The derivative according to any claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each a hydrogen atom.6. The method according to claim 5 , wherein the organometallic compound is selected from the group consisting of an organolithium compound claim 5 , an organomagnesium compound claim 5 , an organoaluminum compound claim 5 , an organozinc compound claim 5 , an organoboron compound and an organosilyl compound.8. The method according to any claim 5 , wherein the transition metal catalyst comprises a nickel complex or a palladium complex.9. The method according to claim 5 , wherein Aand A claim 5 , which may be the same or different claim 5 , are each independently an optionally substituted C-Calkyl group claim 5 , an optionally substituted C-Calkenyl group claim 5 , an optionally substituted C-Calkynyl group claim 5 , an optionally substituted C-Caryl group or an optionally substituted heteroaryl group.10. The method according to claim 5 , wherein Xand Xare each an iodine atom.11. The method according to claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , R claim 5 , R claim ...

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11-04-2013 дата публикации

Process for the preparation of pteridine derivatives

Номер: US20130090474A1
Принадлежит: Dipharma Francis Srl

The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.

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18-04-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130096106A1

Compounds represented by formula: 3. A compound according to claim 1 , wherein Z is 6-7 membered heterocycle or 6-7 membered cycloalkyl.4. A compound according to claim 1 , wherein Z is cyclohexyl claim 1 , piperidinyl claim 1 , N—(Calkyl)-piperidinyl claim 1 , hexahydrothiopyranyl claim 1 , azepanyl claim 1 , methylazepanyl claim 1 , N—(Calkyl)-piperidinylmethyl claim 1 , tetrahydropyranyl claim 1 , piperidinylmethyl claim 1 , pyridinyl claim 1 , pyridinylmethyl claim 1 , tetrahydrothiopyranyl claim 1 , dioxolanylmethyl or dioxanylmethyl which in each case is unsubstituted or substituted by one or more substituent chosen from halogen claim 1 , nitro claim 1 , nitroso claim 1 , SORf claim 1 , SORf claim 1 , PORcRd claim 1 , CONRgRh claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Caralkyl claim 1 , Caryl claim 1 , Calkyloxy claim 1 , Calkenyloxy claim 1 , Calkynyloxy claim 1 , Caryloxy claim 1 , C(O)Calkyl claim 1 , C(O)Calkenyl claim 1 , C(O)Calkynyl claim 1 , C(O)Caryl claim 1 , C(O)Caralkyl claim 1 , C(O)NHRf claim 1 , Cheterocycle claim 1 , hydroxyl claim 1 , NRgRh claim 1 , C(O)ORf claim 1 , cyano claim 1 , azido claim 1 , amidino or guanido;{'sub': 1-6', '2-6', '2-6', '6-10', '3-10', '3-10', '6-10, 'wherein Rf, Rc, Rd, Rg and Rh in each case is H, Calkyl, Calkenyl, Calkynyl, Caryl, Cheterocycle, Cheteroaralkyl or Caralkyl;'}or Rc and Rd are taken together with the oxygens to form a 5 to 10 membered heterocycle;or Rg and Rh are taken together with the nitrogen to form a 3 to 10 membered heterocycle.5. A compound according to claim 1 , wherein Z is cyclohexyl unsubstituted or substituted by one or more substituent chosen from halogen claim 1 , SORf claim 1 , CONRgRh claim 1 , Calkyl claim 1 , Caralkyl claim 1 , Caryl claim 1 , Calkyloxy claim 1 , C(O)Calkyl claim 1 , Cheterocycle claim 1 , hydroxyl claim 1 , NRgRh claim 1 , C(O)Orf or cyano;{'sub': '1-6', 'wherein Rf, Rg and Rh in each case is H or Calkyl.'}6. A compound according to claim 1 , ...

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18-04-2013 дата публикации

Compounds and Methods for Altering Lifespan of Eukaryotic Organisms

Номер: US20130096175A1
Принадлежит:

Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation. 11.) The compound of claim 1 , wherein the compound is selected from the following: 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[4-(N claim 1 ,N-dimethylamino)phenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-methylphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-(1-methylethyl)phenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[4-chlorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopentanecarbonyl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-isobutyryl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[2-chloro-6-fluorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-propanoyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[3 claim 1 ,4-dimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[3 claim 1 ,4-dimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-acetyl-5-[naphth-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[2 claim 1 ,4-dichlorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-propanoyl-5-[2 claim 1 ,4 claim 1 ,5-trimethoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[4-fluorophenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-benzoyl-5-[fur-2-yl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2-cyclopropanecarbonyl-5-[4-methoxyphenyl]-; 1 claim 1 ,3-cyclohexanedione claim 1 , 2- ...

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18-04-2013 дата публикации

Crystalline rotigotine base and preparation process therefor

Номер: US20130096321A1
Принадлежит: Chemagis Ltd

An isolated and pure crystalline rotigotine base of polymorph Form I, and processes for producing the crystalline rotigotine base are disclosed. Also disclosed is a transdermal patch for the delivery of rotigotine base using the disclosed isolated and pure form of rotigotine base, which can be used in treatment of Parkinson's Disease and other disorders ameliorated or treated by rotigotine, including restless leg syndrome.

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25-04-2013 дата публикации

Cyclohexylamines

Номер: US20130101667A1
Принадлежит: Endo Pharmaceuticals Inc

The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.

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25-04-2013 дата публикации

BIARYL OXYACETIC ACID COMPOUNDS

Номер: US20130102609A1
Принадлежит: LIGAND PHARMACEUTICALS INC.

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 2. A compound or salt according to wherein R claim 1 , R claim 1 , Rand Rare each independently selected from hydrogen and methyl.3. (canceled)4. A compound or salt according to claim 1 , wherein Ris selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl and isopropyl.5. (canceled)6. A compound or salt according to claim 1 , wherein Ris selected from aryl and heteroaryl claim 1 , each optionally substituted with one to four substituents independently selected from halogen claim 1 , cyano claim 1 , (C-C) haloalkyl claim 1 , (C-C) alkoxy claim 1 , (C-C) haloalkoxy claim 1 , (C-C) alkyl claim 1 , and (C-C) alkylsulfonyl.9. A compound or salt according to claim 8 , wherein Ris selected from hydrogen claim 8 , methyl claim 8 , fluoro claim 8 , chloro claim 8 , cyano claim 8 , —CFand methoxy; and Ris selected from hydrogen claim 8 , fluoro claim 8 , chloro claim 8 , methyl claim 8 , methoxy claim 8 , cyano claim 8 , —CFand —SOCH.10. A compound or salt according to wherein Rand Rare each independently selected from fluoro claim 9 , chloro claim 9 , methoxy and hydrogen.11. (canceled)13. A compound or salt according to wherein Ris selected from naphthyl claim 6 , pyridinyl and quinolinyl claim 6 , each optionally substituted with one to four substituents independently selected from halogen claim 6 , cyano claim 6 , (C-C) haloalkyl claim 6 , (C-C) alkoxy claim 6 , (C-C) haloalkoxy claim 6 , (C-C) alkyl and alkylsulfonyl.14. A compound or salt according to claim 1 , wherein Rand Rare each hydrogen.15. A compound or salt according to claim 1 , wherein A is selected from phenyl claim 1 , pyridinyl claim 1 , benzimidazolyl claim 1 , quinolinyl claim 1 , indolyl claim 1 , pyrimidinyl and imidazopyridinyl.16. A compound ...

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25-04-2013 дата публикации

ANTIMICROBIAL COMPOUNDS OF 1,4-NAPHTOQUINONE STRUCTURE

Номер: US20130102650A1
Принадлежит:

The present invention relates to a compound having formula (I) wherein: Ris chosen from the group consisting of: phenyl group, possibly substituted, —CH—CH—R′group, R′being chosen from the group consisting of: H, —OH, halogen, alkyl, aryl, CHO, —CN, —NO, —SR, —OR, —NRR, —CONRR, —COOR, and —NHCOR, Rand Rrepresenting independently from each other H, an alkyl group or an aryl group, R′being preferably in para position, and —CH—CO—R′ group, R′ representing an aryl or heteroaryl group, said aryl and heteroaryl groups being possibly substituted, Ris chosen from the group consisting of: —OH and halogen, and R, R, Rand Rare in particular H, for its use for the prevention and/or the treatment of bacterial infections. 3. The compound according to claim 1 , wherein Ris a substituted or unsubstituted phenyl group.4. The compound according to claim 1 , wherein Ris a phenyl group claim 1 , substituted by an aryl group.5. The compound according to claim 1 , wherein Ris chosen from the group consisting of: —CH—CH—R′group and —CH—CO—R′ group claim 1 , R′and R′ being as defined in .7. The compound according to claim 6 , wherein R′is a group in para position having formula —OR′ claim 6 , R′being H or an alkyl group comprising from 1 to 6 carbon atoms.8. The compound according to claim 6 , wherein Ris chosen from the groups having formula —CH—CO—R′ claim 6 , R′ being as defined in .9. The compound according to claim 8 , wherein R′ is a substituted and unsubstituted aryl group.10. The compound for the use according to claim 8 , wherein R′ is a substituted or unsubstituted phenyl group.12. The compound according to claim 11 , wherein R′is a group in para position chosen from the alkyl groups comprising from 1 to 6 carbon atoms claim 11 , and the groups having formula —OR′ claim 11 , R′being chosen from H and alkyl groups comprising from 1 to 6 carbon atoms.13. The compound according to claim 1 , wherein R′ is a substituted and unsubstituted heteroaryl group.15. (canceled)16. The ...

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25-04-2013 дата публикации

Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives

Номер: US20130102794A1
Принадлежит: UCB PHARMA GMBH

The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).

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02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Принадлежит: Tetraphase Pharmaceuticals Inc

The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

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02-05-2013 дата публикации

SALACINOL AND PONKORANOL HOMOLOGUES, DERIVATIVES THEREOF, AND METHODS OF SYNTHESIZING SAME

Номер: US20130109735A1
Принадлежит: SIMON FRASER UNIVERSITY

Salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using said homologies and derivatives. The derivatives include stereoisomers, de-O-sulfonated compounds and congeners of the naturally occurring homologues. Some of the derivatives exhibit enhanced glucosidase inhibitory bioactivity in comparison to the naturally occurring compounds which have been isolated from 5. (canceled)8. (canceled)9. (canceled)13. A method of using a compound as defined in as a glycosidase inhibitor claim 1 , comprising administering said compound to a patient.14. A method for treating diabetes in an affected patient comprising the step of administering to the patient a therapeutically effective amount of a compound as defined in .15. (canceled)16. (canceled) This application claims priority to, and the benefit under 35 U.S.C. §119 of, U.S. provisional patent application No. 61/265,695 filed 1 Dec. 2009 and entitled SALACINOL HOMOLOGUES, DERIVATIVES THEREOF AND METHODS OF SYNTHESIZING SAME, the entirety of which is hereby incorporated by reference.This application relates to salacinol and ponkoranol homologues, derivatives thereof and methods of synthesizing and using same.Glycosidases are enzymes that are involved in the catabolism of glycoproteins and glycoconjugates and the biosynthesis of oligosaccharides. Disruption in regulation of glycosidases can lead to diseases.Over the years, glycosidase inhibitors have received considerable attention in the field of chemical and medicinal researchbecause of their effects on quality control, maturation, transport, secretion of glycoproteins, and cell-cell or cell-virus recognition processes. This principle has potential for many therapeutic applications, such as in the treatment of diabetes, cancer and other viral infections.Bioactive components isolated from medicinal plants that are used in traditional medicine or folk medicine often provide the lead structures for modern drug-discovery programs. For example, ...

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09-05-2013 дата публикации

Novel whitening agents for cellulosic substrates

Номер: US20130116160A1
Принадлежит: Procter and Gamble Co

This invention relates to novel whitening agents for cellulosic substrates. The whitening agents are comprised of at least two components: at least one chromophore component and at least one polymeric component. Suitable chromophore components generally fluoresce blue, red, violet, or purple color when exposed to ultraviolet light, or they may absorb light to reflect these same shades. The whitening agents are further characterized by having a dispersion component value of the Hansen Solubility Parameter of less than or equal to about 17 MPa 0.5 . This invention also relates to laundry care compositions including but not limited to liquid and/or powder laundry detergent formulations and rinse added fabric softening (RAFS) compositions that comprise such whitening agents.

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09-05-2013 дата публикации

BIARYL AMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF

Номер: US20130116227A1
Принадлежит: DAINIPPON SUMITOMO PHARMA CO., LTD.

Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; Ris a substitutable aminosulfonyl group, etc.; Ris a hydrogen atom, etc.; Ris a hydrogen atom, etc.; Ris a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable Calkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R, Rand Rare each independently hydrogen atoms, etc.; Ris a halogen atom, a cyano group, etc.; Rand Rare each independently a hydrogen atom, etc.; and m is an integer such as 0.) 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A is a group of formula (a).3. The compound of either claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —NHCO—.4. The compound of either claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein L is —CONH—.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris [{'sub': '1-6', 'claim-text': [{'sub': '1-6', '(i) amino (in which the amino may be optionally substituted with the same or different 1 to 2 Calkyl),'}, {'sub': '1-6', '(ii) Calkoxy, or'}, '(iii) 4- to 7-membered cyclic amino),, '(a) Calkyl (in which the group may be optionally substituted with'}, {'sub': '1-6', '(b) Calkylcarbonyl,'}, '(c) aminocarbonyl, and', {'sub': '2', '(d) —C(═NH)—NH),'}], '1: aminosulfonyl group (in which the amino may be optionally substituted with the same or different 1 to 2 groups selected from the group consisting of'}{'sub': '1-6', '2: Calkylsulfonyl group, or'}{'sub': '1-6', '3: Calkylsulfonylamino group, or a pharmaceutically acceptable salt thereof.'}6. The compound of claim 5 , wherein Ris aminosulfonyl group claim 5 , or a pharmaceutically acceptable salt thereof.7. The compound of claim ...

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16-05-2013 дата публикации

Styryl-based compound, composition containing styryl-based compound, and organic light emitting diode including styryl-based compound

Номер: US20130119355A1
Принадлежит: Samsung Display Co Ltd

A styryl-based compound represented by Formula 1, a composition containing the styryl-based compound, and an organic light-emitting diode (OLED) including the styryl-based compound: The styryl-based compound may exhibit high heat resistance and thus an OLED including the same may have low driving voltage, high brightness, high efficiency, and long lifetime.

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16-05-2013 дата публикации

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

Номер: US20130121919A1

The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject. 8. A method for screening compounds of Formula (I) , Formula (II) , Formula (III) , or Formula (V) to treat conditions associated with accumulated amyloid-beta peptide deposits , the method comprising:a) administering a HAT Activator compound of Formula (I), Formula (II), Formula (III), or Formula (V) to an animal model of amyloid-beta peptide deposit accumulation; andb) selecting a HAT Activator compound of Formula (I), Formula (II), Formula (III), or Formula (V) that can modulate histone acetylation after administration of the HAT Activator compound in an animal model of amyloid-beta peptide deposit accumulation.9. A method for identifying a histone acetyltransferase (HAT) activator compound of Formula (I) , Formula (II) , Formula (III) , or Formula (V) to treat conditions associated with accumulated amyloid-beta peptide deposits , wherein the method comprises selecting a HAT Activator compound of Formula (I) , Formula (II) , Formula (III) , or Formula (V) having one or more of the following features:{'sub': '50', 'a) the ECof the compound is no more than about 1000 nM;'}b) the histone acetylation activity in vitro targets histone protein H2, H3, and/or H4; andc) the compound penetrates the blood brain barrier; or a combination thereof.10. The method of claim 9 , wherein the compound has a molecular mass less than about 500 Da claim 9 , has a polar surface area less than about 90 Å claim 9 , has less than 8 hydrogen bonds claim 9 , or a combination thereof claim 9 , in order to penetrate the blood brain barrier.12. The method of claim 11 , wherein the subject ...

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16-05-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130123242A1

The present invention provides novel compounds represented by formula I: 197.-. (canceled)101. A compound according to claim 98 , wherein Z is H.102. A compound according to claim 98 , wherein Ris Calkyl claim 98 , Caryl claim 98 , or Cheterocycle claim 98 , which in each case is substituted or unsubstituted.103. A compound according to claim 98 , wherein Ris H claim 98 , Calkyl claim 98 , Caralkyl claim 98 , Cheterocycle claim 98 , or Cheteroaralkyl claim 98 , which in each case is substituted or unsubstituted.104. A compound according to claim 98 , wherein{'sub': 3', '3', '3', '12', '3', 'c', 'd', '13', '14', '1-6', '2-6', '2-6', '6-12', '6-12', '1-6', '2-6', '2-6', '6-12', '1-6', '2-6', '2-6', '6-12', '6-12', '3-10', '13', '14', '12, 'Ris H, or Ris methyl, ethyl, isopropyl, cyclopropyl, cyclohexyl, allyl, piperidinyl, piperazinyl, pyrrolidinyl, azetidinyl, aziridinyl, pyridinyl, piperidinylmethyl, dioxanyl, azepanyl or benzyl, which in each case is unsubstituted or substituted by one or more substituents chosen from halogen, nitro, nitroso, SOR, PORR, CONRR, Calkyl, Calkenyl, Calkynyl, Caralkyl, Caryl, Calkyloxy, Calkenyloxy, Calkynyloxy, Caryloxy, C(O)Calkyl, C(O)Calkenyl, C(O)Calkynyl, C(O)Caryl, C(O)Caralkyl, Cheterocycle, hydroxyl, NRR, C(O)OR, cyano, azido, amidino, and guanido; and'}{'sub': 12', 'c', 'd', '13', '14', '1-12', '2-12', '2-12', '6-14', '3-12', '3-18', '6-18, 'R, R, R, Rand Rare each independently H, Calkyl, Calkenyl, Calkynyl, Caryl, Cheterocycle, Cheteroaralkyl, or Caralkyl,'}{'sub': c', 'd, 'or Rand R, taken together with the oxygens, form a 5 to 10 membered heterocycle,'}{'sub': 13', '14, 'or Rand R, taken together with the nitrogen, form a 3 to 10 membered heterocycle.'}105. A compound according to claim 104 , wherein Ris isopropyl or cyclohexyl claim 104 , which in each case is substituted or unsubstituted.106. A compound according to claim 98 , wherein Ris Calkyl claim 98 , Caryl claim 98 , or Cheterocycle claim 98 , which in each case is ...

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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

CARBOCATALYSTS FOR CHEMICAL TRANSFORMATIONS

Номер: US20130123514A1
Принадлежит: GRAPHEA, INC.

The disclosure relates to catalytically active carbocatalysts, e.g., a graphene oxide or graphite oxide catalyst suitable for use in a variety of chemical transformations. In one embodiment, it relates to a method of catalyzing a chemical reaction of an organic molecule by reacting the organic molecule in the presence of a sufficient amount of graphene oxide or graphite oxide for a time and at a temperature sufficient to allow catalysis of a chemical reaction. According to other embodiments, the reaction may be an oxidation reaction, a hydration reaction, a dehydrogenation reaction, a condensation reaction, or a polymerization reaction. Some reactions may include auto-tandem reactions. The disclosure further provides reaction mixtures containing an organic molecule and graphene oxide or graphite oxide in an amount sufficient to catalyze a reaction of the organic molecule. 1. A method for chemically transforming an organic compound , comprising:(a) contacting the organic compound with a catalytically active carbocatalyst having a surface terminated with one or more peroxide, hydroxyl, aldehyde, or carboxylic acid groups; and(b) transforming the organic compound with the aid of the catalytically active carbocatalyst to form a mixture of a reaction product and a spent or partially spent carbocatalyst.2. The method of claim 1 , wherein the catalytically active carbocatalyst is an oxidized form of graphite.3. The method of claim 2 , wherein the catalytically active carbocatalyst is graphene oxide or graphite oxide.4. The method of claim 1 , wherein the catalytically active carbocatalyst is an oxidized carbon-containing material.5. The method of claim 1 , wherein the catalytically active carbocatalyst is characterized by one or more FT-IR features at about 3150 cm claim 1 ,1685 cm claim 1 , 1280 cm claim 1 , or 1140 cm.629-. (canceled)30. The method of claim 1 , wherein the organic compound has at least one sp-hybridized C—H bond claim 1 , and the transformation involves ...

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23-05-2013 дата публикации

LIGANDS FOR ESTROGEN RELATED RECEPTORS AND METHODS FOR SYNTHESIS OF SAID LIGANDS

Номер: US20130131340A1
Автор: Forman Barry, Yu Donna
Принадлежит:

Estrogen-Related Receptor (ERR) modulating compounds and methods for synthesis of said compounds are described. 2. (canceled)3. The compound of wherein X is S claim 1 , and R is selected from the group consisting of 5-CHand 5-NO claim 1 , and wherein the compound is an estrogen-related receptor (ERR) agonist.4. The compound of wherein X is O claim 1 , and R is selected from the group consisting of 4 claim 1 ,5-CHand 5-CHCH claim 1 , andwherein the compound is an estrogen-related receptor (ERR) agonist.5. (canceled)6. (canceled)7. (canceled)11. The compound of claim 10 , wherein the compound is an ERRα/β/γ agonist.12. The compound of claim 10 , wherein the compound is an ERRβ/γ agonist.13. The compound of wherein the compound is an ERRγ agonist.16. The compound of claim 15 , wherein the compound is an ERRα/β/γ agonist.17. The compound of claim 15 , wherein the compound is an ERRβ/γ agonist.18. The compound of wherein the compound is an ERRγ agonist. This application is a divisional of U.S. patent application Ser. No. 12/475,323, filed May 29, 2009 and now pending, which is a divisional of U.S. patent application Ser. No. 11/336,515, filed Jan. 20, 2006 and issued as U.S. Pat. No. 7,544,838 on Jun. 9, 2009, which claims priority to U.S. Provisional Application No. 60/646,128, filed Jan. 21, 2005, all of which are incorporated herein by reference in their entirety.The present invention relates to ligands and methods for synthesis of said ligands.Metabolic disease, including obesity, diabetes and atherosclerosis, is the leading cause of mortality in industrialized nations. It is estimated that over one-third of the United States population is obese and these individuals are at risk for developing diabetes and atherosclerosis. These disorders are responsible for over 500,000 deaths in the United States each year. The growing incidence of this problem has led to intense interest in identifying new molecular targets and new pharmacologic agents to treat and/or prevent ...

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30-05-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: US20130136719A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , and R 3 are as defined herein, are useful for treating flaviviridae viral infections.

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30-05-2013 дата публикации

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Номер: US20130137690A1
Принадлежит: Individual

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

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30-05-2013 дата публикации

NOVEL AMIDO DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS

Номер: US20130137704A1
Автор: Boléa Christelle
Принадлежит: Addex Pharma, SA

The present invention relates to novel compounds of Formula (I), wherein X, X, X, X, Aand Bare defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. 2. A compound according to claim 1 , which can exist as optical isomers claim 1 , wherein said compound is either the racemic mixture or one or both of the individual optical isomers.3. A compound according to claim 1 , wherein said compound is:N-(3-Chloro-4-(pyrimidin-2-yloxy)phenyl)picolinamideor a pharmaceutically acceptable acid or base addition salt thereof,a stereochemically isomeric form thereof and an N-oxide form thereof.4. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to to and a pharmaceutically acceptable carrier and/or excipient.5. A method of treating or preventing a condition in a mammal claim 1 , including a human claim 1 , the treatment or prevention of which is affected or facilitated by the neuromodulatory effect of mGluR4 allosteric modulators claim 1 , comprising administering to a mammal in need of such treatment or prevention claim 1 , an effective amount of a compound/composition according to to .6. A method of treating or preventing a condition in a mammal claim 1 , including a human claim 1 , the treatment or prevention of which is affected or facilitated by the neuromodulatory effect of mGluR4 positive allosteric modulators claim 1 , comprising administering to a mammal in need of such treatment or prevention claim 1 , an effective amount of a compound/composition according to to .7. A method useful for treating or preventing central nervous system disorders selected from the group consisting of: addiction claim 1 , tolerance or dependence claim 1 , affective disorders claim 1 , such as depression and anxiety claim 1 , psychiatric ...

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06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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06-06-2013 дата публикации

INHIBITORS OF CALCIUM-ACTIVATED CHLORIDE CHANNELS

Номер: US20130143765A1

Provided herein are methods for identifying compounds that are inhibitors of a calcium-activated chloride channel. Aminothiophene and aminothiazole compounds, and compositions comprising these compounds, described herein that inhibit efflux of chloride through a calcium-activated chloride channel are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased chloride and fluid secretion, for example, secretory diarrhea. 425-. (canceled)27. The composition of wherein at least one of Rand Ris not hydrogen.29112.-. (canceled)113. An isolated epithelial cell comprising (i) a calcium-activated chloride channel and (ii) a recombinant cytoplasmic indicator protein that binds halide.114. The epithelial cell of wherein the epithelial cell is an intestinal epithelial cell or a pulmonary epithelial cell.115. The epithelial cell of wherein the intestinal epithelial cell is an HT-29 cell.116. The epithelial cell of wherein the cytoplasmic indicator protein is a yellow fluorescent protein (YFP) mutant.117. The epithelial cell of claim 116 , wherein the YFP mutant is YFP-H148Q/I152L.118. The epithelial cell of wherein the calcium-activated chloride channel is TMEM16A.119. The epithelial cell of wherein TMEM16A is human TMEM16A.120. The epithelial cell of wherein the recombinant cytoplasmic indicator protein is introduced into the cell by a recombinant expression vector that is a viral vector.121. The method of wherein the viral vector is a retroviral vector.122. The method of wherein the retroviral vector is a lentiviral vector.123. A method of identifying an agent that is an inhibitor of a calcium-activated chloride channel comprising:{'claim-ref': {'@idref': 'CLM-00113', 'claim 113'}, '(a) contacting the isolated epithelial cell of and a candidate agent in a test sample to permit interaction between the candidate agent and the cell;'}{'sup': '2', '(b) adding to the test sample (i) at least one ...

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20-06-2013 дата публикации

CALIXARENE COMPOUND AND PHOTORESIST COMPOSITION COMPRISING SAME

Номер: US20130157195A1
Принадлежит: Rohm and Haas Electronic Materials LLC

A molecular glass compound includes (A) a tetrameric reaction product of a specific aromatic compound having at least one hydroxy group, and a specific polycyclic or fused polycyclic aromatic aldehyde; and (B) an acid-removable protecting group as an adduct with the hydroxy group of the aromatic compound and/or a hydroxy group of the polycyclic or fused polycyclic aromatic aldehyde. A photoresist composition including the molecular glass compound, and a coated substrate including a layer of the photoresist composition are also disclosed. 2. The molecular glass compound of claim 1 , wherein the aromatic compound of formula (I) is resorcinol claim 1 , pyrogallol claim 1 , 3-methoxyphenol claim 1 , or 3-ethoxyphenol.3. The molecular glass compound of claim 1 , wherein Arof Formula (II) is a Caryl claim 1 , Cheteroaryl claim 1 , Chaloaryl claim 1 , Cheterohaloaryl claim 1 , Caralkyl claim 1 , or Chaloaralkyl.5. The molecular glass compound of claim 1 , wherein the acid-removable protecting group is the adduct of a vinyl ether claim 1 , a tertiary alkyl ester claim 1 , a tertiary alkyl carbonyl claim 1 , or a combination comprising at least one of the foregoing.7. A photoresist claim 1 , comprising the molecular glass compound of .8. A photoresist claim 1 , comprising the molecular glass compound of claim 1 , a solvent claim 1 , and a photoacid generator.9. A coated substrate claim 8 , comprising: (a) a substrate having one or more layers to be patterned on a surface thereof; and (b) a layer of a photoresist composition of over the one or more layers to be patterned.10. A method of forming a patterned substrate claim 9 , comprising exposing the coated substrate of to activating radiation.11. The method of claim 10 , wherein exposure is with e-beam and/or EUV radiation. This application is a nonprovisional filing of provisional application 61/538,672, filed Sep. 23, 2011, the content of which is incorporated herein by reference in its entirety.Design rules for advanced ...

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20-06-2013 дата публикации

NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY

Номер: US20130157982A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to claim 1 , wherein:{'sup': 1', '10, 'Ris N or C—R;'}{'sup': '2', 'Ris optionally substituted aromatic heterocycle or optionally substituted cycloalkenyl;'}{'sup': 3', '11', '12', '13', '14, 'Ris O, N—R, CH—Ror S, —CR═CR—, —C(O) or —C≡C—;'}{'sup': '4', 'Ris H, optionally substituted aromatic heterocycle, optionally substituted non-aromatic heterocycle, optionally substituted cycloalkyl, optionally substituted cycloalkenyl or optionally substituted aryl;'}{'sup': '5', 'sub': 1-3', '1-3, 'Ris H, halogen, hydroxyl, —OCalkyl, or Calkyl;'}{'sup': '6', 'sub': 1-3', '1-3, 'Ris H, Calkyl, halogen, hydroxyl or —OCalkyl;'}{'sup': '7', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': '8', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': 9', '15, 'sub': 3', '2', '2', '3-6', '2, 'Ris —OPOH, —COOH, —P(O)(OH), —Calkyl, —S(O)OH, —P(O)MeOH, —P(O)(H)OH or —OR;'}{'sup': '10', 'sub': 1-6', '1-3, 'Ris H, Calkyl, halogen, hydroxyl or —OCalkyl;'}{'sup': '11', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '12', 'sub': 1-3', '1-3, 'Ris H, Calkyl, halogen, hydroxyl, —OCalkyl or amino;'}{'sup': '13', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '14', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '15', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': 16', '17, 'L is CHR, O, S, NRor —C(O)—;'}a is 0, 1, 2, 3, 4 or 5;b is 0, 1, 2, 3, 4 or 5;c is 0 or 1;d is 0, 1, 2 or 3;{'sup': '16', 'sub': 1-3', '1-3, 'Ris H, Calkyl, —OCalkyl, halogen, hydroxyl or amino, and'}{'sup': '17', 'sub': '1-3', 'Ris H or Calkyl;'}with the provisos:{'sup': 3', '11', '17, 'a). when Ris O, N—R, or S, and b is 0 or 1 then L is not O, S, or NR; and'}{'sup': '9', 'sub': 3', '2', '2', '2, 'b). when Ris —OPOH, —COOH, —P(O)(OH), —S(O)OH, —P(O)MeOH or —P(O)(H)OH'}then d is not 0; and{'sup': 9', '15, 'c). when Ris ORthen d is not ...

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20-06-2013 дата публикации

METHODS FOR TREATING OR PREVENTING CANCER AND NEURODEGENERATIVE DISEASES

Номер: US20130158017A1
Автор: Li Yueming, Zhu Lei

Provided are methods of treating or preventing a neurodegenerative disease comprising administering to a subject having a neurodegenerative disease an effective amount of a compound of Formula I: 218-. (canceled)21. (canceled)23. The method of claim 20 , wherein each Ris H.24. (canceled)25. The method of claim 20 , wherein v is 1 and X is in the 5-position of the thiopheno group.26. The method of claim 20 , wherein p is 1 and Ris in the 4-position of the phenyl group.2830-. (canceled)34. The method of claim 31 , wherein each Ris H.35. The method of claim 31 , wherein Ris H or methyl.36. The method of claim 31 , wherein Ris methyl.37. The method of claim 31 , wherein q is 0.38. The method of claim 31 , wherein v is 1 and X is in the 5-position of the thiopheno group.41. The method of claim 31 , wherein the neurodegenerative disease is Alzheimer's disease claim 31 , Parkinson's disease claim 31 , ALS claim 31 , or MS.42. The method of claim 31 , wherein the neurodegenerative disease is Alzheimer's disease. This application claims priority to U.S. Provisional Patent Application Ser. No. 61/139,751, filed Dec. 22, 2008, the entire content of which is incorporated herein by reference.The invention relates to methods of treatment or prevention of cancer and neurodegenerative diseases comprising administering an effective amount of a Sulfonamide-Based Compound to a subject.Alzheimer's disease (AD) is the most prevalent form of dementia. It is a neurodegenerative disorder, clinically characterized by progressive loss of memory and general cognitive function, and pathologically characterized by the deposition of extracellular proteinaceous plaques in the cortical and associative brain regions of sufferers. These plaques mainly comprise fibrillar aggregates of beta-amyloid peptide (Aβ). Aβ is formed from amyloid precursor protein (APP). APP is a ubiquitous membrane-spanning (type 1) glycoprotein, of which three major isoforms (APP695, APP751, and APP770) are known, that ...

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20-06-2013 дата публикации

Acrylamide Compounds And Use Thereof For Inhibiting Apoptosis

Номер: US20130158022A1
Принадлежит: CHINESE PLA GENERAL HOSPITAL

The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis. 4. The compound according to having any one of the following structures claim 1 , or their isomers claim 1 , pharmaceutically acceptable salts and solvates:(1) (2E)-3-(2-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(2) (2E)-3-(3-thienyl)-N-[1-(8-quinolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(3) (2E)-3-(2-thienyl)-N-[1-(4-tolylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(4) (2E)-3-(2-thienyl)-N-[1-(2-methoxyanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(5) (2E)-3-(2-thienyl)-N-(1-benzylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(6) (2E)-3-(2-thienyl)-N-(1-cyclohexylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(7) (2E)-3-(2-thienyl)-N-[1-isopropylaminothioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(8) (2E)-3-(2-thienyl)-N-[1-(2-fluoroanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(9) (2E)-3-(2-thienyl)-N-[1-(3-isopropoxypropylamino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(10) (2E)-3-(2-thienyl)-N-[1-(2-methoxyformylanilino)thioformylamino-2,2,2-trichloroethyl]-2-acrylamide;(11) (2E)-3-(2-thienyl)-N-(1-cycloheptylaminothioformylamino-2,2,2-trichloroethyl)-2-acrylamide;(12) (2E)-3-(2-thienyl)-N-[1-(1-morpholinyl)thioformylamino-2,2,2- ...

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20-06-2013 дата публикации

TG2 INHIBITORS AND USES THEREOF

Номер: US20130158087A1

Methods and compounds for treating cancer, dmg resistance and/or metastasis are described herein. These methods and compounds can inhibit the expression of aberrant TG2 expression and/or inhibit the binding of GTP to TG2, and thereby prevent the induction of epithelial to mesenchymal transition of cancer cells, and a stem cell-like phenotype. 76. Use of the compound of , , or for the manufacture of a medicament for treating cancer.83. The method of , , or , wherein the compound treats cancer. This patent application claims priority to U.S. Patent Application Ser. No. 61/356,961 filed on Jun. 21, 2010 which is incorporated by reference herein in its entiretyThis invention is related to modulation of aberrant expression of TG2 and/or inhibition of GTP binding to TG2 to treat cancer, metastasis, drug resistance and other oncogenic properties.None.None.This disclosure includes a sequence listing submitted as a text file pursuant to 37 C.F.R., §1.52(e)(v) named sequence listing.txt, created on Jun. 16, 2010, with a size of 22,111 bytes, which is incorporated herein by reference. The attached sequence descriptions and Sequence Listing comply with the rules governing nucleotide and/or amino acid sequence disclosures in patent applications as set forth in 37 C.F.R. §§1.821-1.825.Epithelial-to-mesenchymal transition (“EMT”) is a complex dynamic process that occurs during embryonic development for reprogramming of epithelial cells. Downregulation of E-cadherin, which occurs during EMT, results in the loss of homotypic adhesion. Reactivation of EMT during adult life has been associated with various pathological conditions. For example, EMT promotes the detachment of cancer cells from the primary tumor and facilitates migration through the acquisition of stem cell like properties, including loss of cellular polarity and adhesion. Metastasis and resistance to systemic therapies pose major clinical challenges to the treatment of breast and other cancers. Identification of tumor- ...

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27-06-2013 дата публикации

BIPHENYL AND PHENYL-PYRIDINE AMIDES AS P2X3 AND P2X2/3 ANTAGONISTS

Номер: US20130165443A1
Принадлежит:

Compounds of the formula I: 2. The compound of claim 1 , wherein R claim 1 , Rand Rare hydrogen.3. The compound of claim 2 , wherein Ris phenyl substituted at the 4-position with methyl or halo and optionally substituted at the 2-position with halo.4. The compound of claim 2 , wherein Ris 4-methyl-phenyl.5. The compound of claim 2 , wherein Ris pyridin 2-yl substituted with methyl or halo at the 5-position.6. The compound of claim 2 , wherein Ris 5-methyl-pyridin-2-yl.8. The compound of claim 7 , wherein Ris hydrogen.9. The compound of claim 7 , wherein Ris methyl.10. The compound of claim 7 , wherein Ris: Calkyl; Calkyloxy-Calkyl; hydroxy-Calkyl; Calkylsulfanyl-Calkyl; Calkylsulfonyl-Calkyl; amino-Calkyl; N—Calkyl-amino-Calkyl; N claim 7 ,N-di-Calkyl-amino-Calkyl; Ccycloalkyl; optionally substituted phenyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.11. The compound of claim 7 , wherein Ris: Calkyloxy-Calkyl; hydroxy-Calkyl; heteroaryl claim 7 , or heterocyclyl-Calkyl.12. The compound of claim 7 , wherein Ris methoxymethyl.13. The compound of claim 7 , wherein Ris hydroxymethyl.14. The compound of claim 7 , wherein Ris heteroaryl selected from pyridinyl claim 7 , pyrimidinyl claim 7 , or pyrazinyl claim 7 , each of which may be optionally substituted once or twice with methyl.15. The compound of claim 7 , wherein Ris hydroxymethyl claim 7 , methoxymethyl claim 7 , pyrazin-2-yl or 5-methyl-pyrazin-2-yl.16. The compound of claim 7 , wherein Ris Calkyl claim 7 , Ccycloalkyl or Ccycloalkyl-Calkyl.17. The compound of claim 7 , wherein Ris isopropyl claim 7 , isobutyl or tert butyl.18. The compound of claim 1 , wherein said compound is selected from:4-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;5-Methyl-thiophene-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Furan-2-carboxylic acid [5-(2-methoxy-1-methyl-ethylcarbamoyl)-4′-methyl-biphenyl-3-yl]-amide;Thiophene-2- ...

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27-06-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130165460A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '2', 'Ris methyl, isopropyl, 2-hydroxyethyl, methylpropionate, 2-methylpyridine, 3-methylpyridine, ethylacetate, N,N-dimethylpropanamide, N-isopropylpropanamide, N-(propan-2-yl)propanamide, propanamide hydroxycyclopent-3-yl, ethyl, N,N-dimethylacetamide, N-methylacetamide, 2-aminoethyl, H-imidazol-2-ylmethyl, 1H-imidazol-4-ylmethyl or ethyl-acetamide.'}6. A compound according to claim 1 , wherein:{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen.'}7. A compound according to claim 1 , wherein:{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris halogen, CN or —OCalkyl; and'}{'sup': '8', 'Ris H.'}8. A compound according to claim 1 , wherein:{'sup': '2', 'Ris methyl, isopropyl, 2-hydroxyethyl, methylpropionate, 2-methylpyridine, 3-methylpyridine, ethylacetate, N,N-dimethylpropanamide, N-isopropylpropanamide, N-(propan-2-yl)propanamide, propanamide hydroxycyclopent-3-yl, ethyl, N,N-dimethylacetamide, N-methylacetamide, 2-aminoethyl, H-imidazol-2-ylmethyl, 1H-imidazol-4-ylmethyl or ethyl-acetamide;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', ' ...

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27-06-2013 дата публикации

Antiviral Drugs for Treatment of Arenavirus Infection

Номер: US20130165493A1
Принадлежит: Siga Technologies, Inc,

Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, and Pichinde), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever). 167-. (canceled)68. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient and a pharmaceutically effective amount of a compound or a pharmaceutically-acceptable salt thereof , selected from the group consisting of2-Phenyl-cyclopropanecarboxylic acid [1-(4-amino-phenyl)-eth-(E)-ylidene]-hydrazide;Cyclopropanecarboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2-Phenyl-cyclopropanecarboxylic acid [1-(2,4-dimethoxy-phenyl)-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-p-tolyl-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-biphenyl-4-yl-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-(3,4-dimethoxy-phenyl)-eth-(E)-ylidene]-hydrazide;Furan-2-carboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2,4-Dichloro-N-(4-[1-[(2-Phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-benzamide;2-Phenyl-cyclopropanecarboxylic acid [1-(2-hydroxy-phenyl)-eth-(E)-ylidene]-hydrazide;Thiophene-2-carboxylic acid (4-[1-[(2-phenyl-cyclopropanecarbonyl)-hydrazono]-ethyl]-phenyl)-amide;2-Phenyl-cyclopropanecarboxylic acid [1-(4-dimethylamino-phenyl)-eth-(E)-ylidene]-hydrazide;2-Phenyl-cyclopropanecarboxylic acid [1-(4-methoxy- ...

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04-07-2013 дата публикации

SULFONAMIDE COMPOUNDS

Номер: US20130172339A1
Принадлежит: KANCERA AB

A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer. 119-. (canceled)21. The compound of claim 20 , wherein A is O or S; or a pharmaceutically acceptable salt claim 20 , hydrate claim 20 , solvate claim 20 , or N-oxide thereof.22. The compound of claim 21 , wherein A is S; or a pharmaceutically acceptable salt claim 21 , hydrate claim 21 , solvate claim 21 , or N-oxide thereof.23. The compound of claim 21 , wherein{'sup': '1', 'Ris selected from H; halogen; and C1-C6 alkyl optionally substituted with at least one halogen; and'}{'sup': 2', '3', '6', '6, 'Rand Rform, together with the carbon atoms to which they are attached, a benzene ring, optionally substituted with at least one R; or a 5- or 6-membered heteroaromatic or heterocyclic ring, optionally substituted with at least one R; or'}{'sup': 1', '2', '6', '6, 'Rand Rform, together with the carbon atoms to which they are attached, a benzene ring optionally substituted with at least one R; or a 5- or 6-membered heteroaromatic or heterocyclic ring, optionally substituted with at least one R; and'}{'sup': '3', 'Ris selected from H; halogen; C1-C6 alkyl optionally substituted with at least one halogen;'}or a pharmaceutically acceptable salt, hydrate, solvate, or N-oxide thereof.24. The compound of claim 21 , wherein{'sup': '1', 'Ris selected from H; halogen; and C1-C6 alkyl optionally substituted with at least one halogen;'}{'sup': 2', '3', '6', '6', '6, 'claim-text': [{'sup': 2', '3, 'at least one of Rand Ris selected from said phenyl, heteroaryl, arylsulfonyl and heteroarylsulfonyl, and'}, {'sup': 2', '3, 'when L is (a), neither Rnor Ris unsubstituted phenyl;'}], 'Rand Rare independently selected from H; halogen; C1-C6 alkyl optionally substituted with at least one halogen; phenyl optionally substituted with at least one R; 5- or 6-membered heteroaryl optionally substituted with at ...

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04-07-2013 дата публикации

2-Alkyl-Cycloalk(en)yl-Carboxamides

Номер: US20130172367A1
Принадлежит: Bayer CropScience AG

Novel -alkylcycloalk(en)ylcarboxamides of the formula (I) 3. Composition for controlling unwanted microorganisms claim 1 , characterized in that it comprises at least one 2-alkylcycloalk(en)ylcarboxamide of the formula (I) according to claim 1 , in addition to extenders and/or surfactants.4. Use of 2-alkylcycloalk(en)ylcarboxamides of the formula (I) according to for controlling unwanted microorganisms.5. Method for controlling unwanted microorganisms claim 1 , characterized in that 2-alkyl-cycloalk(en)ylcarboxamides of the formula (I) according to are applied to the microorganisms and/or their habitat.6. Process for preparing compositions for controlling unwanted microorganisms claim 1 , characterized in that 2-alkylcycloalk(en)ylcarboxamides of the formula (I) according to are mixed with extenders and/or surfactants. The present invention relates to novel 2-alkylcycloalk(en)ylcarboxamides, to a plurality of processes for their preparation and to their use for controlling unwanted microorganisms.It is already known that numerous carboxamides have fungicidal properties (cf., for example, WO 98/03495, WO 98/03486 and EP-A 0 589 313). Thus, some 2-alkylcycloalkylcarboxamides are already known, such as, for example, N-(2-sec-butylcyclohexyl)-2-methyl-4,5-dihydrofuran-3-carboxamide from WO 98/03495, N-[2(2-ethylbutyl)cyclohexyl]-5-fluoro-1,3-dimethyl-1H-pyrazole-4-carboxamide from WO 98/03486 and N-2-sec-butylcyclohexyl)-2-methyl-4-(trifluoromethyl)-1,3-thiazole-5-carboxamide from EP-A 0 589 313. The activity of these compounds is good; however, in some cases, for example at low application rates, it is unsatisfactory.This invention now provides novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I)in whichRrepresents hydrogen, halogen, hydroxyl, cyano, C-C-alkyl, C-C-haloalkyl, C-C-haloalkoxy or C-C-haloalkylthio having in each case 1 to 5 halogen atoms,Furthermore, it has been found that 2-alkylcycloalk(en)ylcarboxamides of the formula (I) are obtained whenR—X  ( ...

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11-07-2013 дата публикации

CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DIODE INCLUDING THE SAME

Номер: US20130175509A1
Принадлежит:

Embodiments of the present invention are directed to a condensed-cyclic compound and an OLED including the same. 5. The condensed-cyclic compound of claim 1 , wherein Xin Formula 2 is N(R) claim 1 , B(R) claim 1 , or Si(R)(R) claim 1 , wherein Rand Rare each independently hydrogen claim 1 , deuterium claim 1 , a halogen atom claim 1 , a hydroxyl group claim 1 , a cyano group claim 1 , a nitro group claim 1 , an amino group claim 1 , an amidino group claim 1 , hydrazine claim 1 , hydrazone claim 1 , a carboxylic acid group or a salt thereof claim 1 , a sulfonic acid group or a salt thereof claim 1 , a phosphoric acid group or a salt thereof claim 1 , a substituted or unsubstituted C-Calkyl group claim 1 , a substituted or unsubstituted C-Calkenyl group claim 1 , a substituted or unsubstituted C-Calkynyl group claim 1 , a substituted or unsubstituted phenyl group claim 1 , a substituted or unsubstituted pentalenyl claim 1 , a substituted or unsubstituted indenyl claim 1 , a substituted or unsubstituted naphthyl group claim 1 , a substituted or unsubstituted azulenyl claim 1 , a substituted or unsubstituted heptalenyl claim 1 , a substituted or unsubstituted indacenyl claim 1 , a substituted or unsubstituted acenaphthyl group claim 1 , a substituted or unsubstituted fluorenyl group claim 1 , a substituted or unsubstituted phenalenyl group claim 1 , a substituted or unsubstituted phenanthrenyl group claim 1 , a substituted or unsubstituted anthryl group claim 1 , a substituted or unsubstituted fluoranthenyl group claim 1 , a substituted or unsubstituted triphenylenyl group claim 1 , a substituted or unsubstituted pyrenyl group claim 1 , a substituted or unsubstituted chrysenyl group claim 1 , a substituted or unsubstituted naphthacenyl group claim 1 , a substituted or unsubstituted picenyl group claim 1 , a substituted or unsubstituted perylenyl group claim 1 , a substituted or unsubstituted pentaphenyl group claim 1 , a substituted or unsubstituted hexacenyl group ...

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18-07-2013 дата публикации

COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITION AND METHODS OF MAKING SAME

Номер: US20130183252A1
Принадлежит: Senomyx, Inc.

The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals. 2. The compound of claim 1 , wherein X is selected from the group consisting of hydrogen claim 1 , heteroalkyl claim 1 , substituted heteroalkyl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , heteroarylalkyl claim 1 , substituted heteroarylalkyl claim 1 , CN claim 1 , S(O)R claim 1 , CONRR claim 1 , —COR claim 1 , SONRR claim 1 , NRSOR claim 1 , NRSONRR claim 1 , B(OR)(OR) claim 1 , P(O)(OR)(OR) claim 1 , and P(O)(R)(OR).7. A composition comprising one or more compounds of claim 1 , or a salt claim 1 , hydrate claim 1 , solvate or N oxide thereof claim 1 , and one or more pharmaceutically acceptable carriers.8. The composition of claim 7 , which is a food claim 7 , beverage or medicament for human consumption.9. A coffee or coffee flavored food or beverage or medicament composition that comprises at least one compound of or a salt claim 1 , hydrate claim 1 , solvate or N oxide thereof.10. The composition of claim 9 , which is an instant coffee claim 9 , ground coffee claim 9 , or brewed coffee.11. The composition of claim 9 , which is an instant coffee.12. A food claim 1 , beverage claim 1 , or medicament composition having a bitter taste wherein said bitter taste is alleviated or eliminated by the addition of an effective amount of a compound of or a salt claim 1 , hydrate claim 1 , ...

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18-07-2013 дата публикации

Compounds and methods for the treatment or prevention of flavivirus infections

Номер: US20130183266A1
Принадлежит: Vertex Pharmaceuticals Inc

A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A biological probe comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.

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18-07-2013 дата публикации

THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE

Номер: US20130184222A1
Принадлежит: AGIOS PHARMACEUTICALS, INC

Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here. 2. The compound of claim 1 , wherein Ris 3-fluorophenyl.3. The compound of or claim 1 , wherein:{'sup': '1', 'Ris selected from cyclohexyl, cyclopentyl, cycloheptyl, 3,3-difluorocyclobutyl, 4,4,-difluorocyclohexyl, and bicyclo[2.2.1]heptanyl; and'}{'sup': '4', 'Ris selected from 1-(methylmethoxycarbonylamino)ethyl, 1,2,3,4-tetrahydroquinolin-1-yl, 1-ethoxycarbonylpiperidin-2-yl, 1-ethoxycarbonylpyrrolidin-2-yl, 1H-benzimidazol-1-ylmethyl, 1H-indazol-3-ylmethyl, indolin-1-ylmethyl, 1H-indol-3-ylmethyl, 1H-indol-5-ylmethyl, 1H-pyrrolo[2,3-b]pyridine-3-ylmethyl, 1H-pyrrolo[3,2-b]pyridin-3-ylmethyl, 1-methoxycarbonylpiperidin-2-yl, 1-methoxycarbonylpyrrolidin-2-yl, 2-fluoropyridin-3-ylaminomethyl, 2-imino-4-fluoropyridin-1-ylmethyl, 2-methoxyphenylaminomethyl, 2-methyl-1H-benzimidazol-1-ylmethyl, 2-methylimidazol-1-ylmethyl, 2-trifluoromethyl-1H-imidazol-1-yl, 3-cyanophenylaminomethyl, 3-fluoropyridin-2-ylaminomethyl, 3-methoxyphenylaminomethyl, 4-(1,3,4-oxadiazole-2-yl)phenylaminomethyl, 4-(dimethylaminocarbonyloxy)phenylmethyl, 4,5-dichloroimidazol-1-ylmethyl, 4-cyanophenylaminomethyl, 4-fluorophenylaminomethyl, 4-fluoropyridin-2-ylaminomethyl, 4-hydroxyphenylmethyl, 4-methoxycarbonylmorpholin-3-yl, 4-methoxycarbonylpiperazin-1-ylmethyl, 4-methoxyphenylaminomethyl, 4-methylcarbonyloxyphenylmethyl, 5-fluoropyridin-2-aminomethyl, 5-fluoropyridin-2-oxymethyl, 6-fluoropyridin-3-ylaminomethyl, benzomorpholin-4-ylmethyl, methoxycarbonylaminomethyl, methylmethoxycarbonylaminomethyl, methylphenylaminomethyl, phenylaminomethyl, pyridin-2-oxymethyl, pyridin-2-ylaminomethyl, pyridin-2-yloxymethyl, pyridin-3-oxymethyl, pyridin-3-ylmethyl, pyridin-4-ylmethyl, thiazol-4-ylmethyl, and thien-2-ylmethyl.'}4. The compound of claim 1 , wherein the compound is selected from any one of Compound numbers 104 claim ...

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18-07-2013 дата публикации

Naphthalene Derivative

Номер: US20130184241A1
Принадлежит: KYOTO UNIVERSITY

The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) 2. The compound according to or oxides , esters , prodrugs , pharmaceutically acceptable salts or solvates thereof , wherein R is selected from phenyl , pyridyl , quinolinyl and thiophenyl , and may be unsubstituted or independently of one another substituted with one or more Ra , in which Ra is as defined in .3. The compound according to or oxides , esters , prodrugs , pharmaceutically acceptable salts or solvates thereof , wherein Ra is absent or independently of one another selected from the group consisting of halo , alkyl , substituted alkyl , alkenyl , substituted alkenyl , aryl , substituted aryl , heteroaryl , substituted heteroaryl , heterocyclyl , substituted heterocyclyl , cyano , nitro , acyl , acylamino , alkoxy , substituted alkoxy , carboxyl , carboxyl ester , alkylthio , substituted alkylthio and aminocarbonyl , in which the substituted alkyl , the substituted alkenyl , the substituted aryl , the substituted heteroaryl , the substituted heterocyclyl , the substituted alkoxy or the substituted alkylthio independently of one another refer to the respective groups substituted with one or more substituent Rb or Rc , the substituent Rb and Rc being as defined in .6. The compound according to or oxides , esters , prodrugs , pharmaceutically acceptable salts or solvates thereof , wherein Ra is selected from the group consisting of alkenyl , substituted alkenyl , aryl , substituted aryl , heteroaryl , substituted heteroaryl , cyano , carboxyl ester , alkylthio , substituted alkylthio and aminocarbonyl , in which substituted alkenyl , substituted aryl , substituted heteroaryl , substituted alkylthio independently of one another refer to the respective groups substituted with one or more substituent Rb or Rc , the substituent Rb and Rc being as defined in .7. A pharmaceutical composition comprising the compound according to or ...

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18-07-2013 дата публикации

APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Номер: US20130184278A1
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein. 5. The compound of claim 1 , or therapeutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:4-[4-(cyclohexylmethyl)-4-methoxypiperidin-1-yl]-N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}-4-[4-methoxy-4-(3-methylbenzyl)piperidin-1-yl]benzamide;N-{[5-({(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}-4-[4-(3,3-diphenylprop-2-enyl)piperazin-1-yl]benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-[(4-{[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]benzamide;N-[(4-{acetyl[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-[(4-{methyl[2-(phenylthio)ethyl]amino}piperidin-1-yl)sulfonyl]benzamide;4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;4-(4-{[2-(4-chlorophenyl)cyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-{[5-({(1R)-3-[isopropyl(methyl)amino]-1-[(phenylthio)methyl]propyl}amino)-4-nitrothien-2-yl]sulfonyl}benzamide;N-{[(5Z)-5-(acetylimino)-4-methyl-4,5-dihydro-1,3,4-thiadiazol-2-yl]sulfonyl}-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl}benzamide;N-({5-[(benzoylamino)methyl]thien-2-yl}sulfonyl)-4-{4-[(4′-chloro-1,1′-biphenyl-2-yl)methyl]piperazin-1-yl ...

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18-07-2013 дата публикации

METHOD FOR THE PREPARATION OF RIVORAXABAN

Номер: US20130184457A1
Принадлежит: SANDOZ AG

The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed. 2. The method of using according to claim 1 , wherein Ris selected from methyl claim 1 , phenyl and tolyl. The present invention relates to the use of a compound having the formula (II) for the preparation of a compound having the formula (V). Methods of preparing the compound having the formula (V) using the compound having the formula (II) are also described. Individual reaction steps as well as intermediates are additionally claimed.The compound having the formula (V) has been disclosed in WO 01/47919.It is also known as rivaroxaban and is marketed in a number of countries under the trade designation Xarelto.The compound having the formula (V) acts as an inhibitor of clotting factor Xa and may be used as an agent for the prophylaxis and/or treatment of thromboembolic disorders, especially myocardial infarction, angina pectoris (including unstable angina), reocclusions and restenoses after angioplasty or aortocoronary bypass, stroke, transient ischemic attacks, peripheral arterial occlusive diseases, pulmonary embolisms or deep venous thromboses.One method for preparing the compound having the formula (V) is disclosed in WO 2004/060887. The method disclosed therein uses a brominated compoundas an intermediate which is prepared using hydrobromic acid at elevated temperatures. Hydrobromic acid is corrosive and is therefore undesirable.It was therefore an object of the present invention to provide a method of preparing the compound having the formula (V) which does not require the use of hydrobromic acid.It was a further object of the present invention to provide a method of preparing the compound having the formula (V) which is simpler ...

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25-07-2013 дата публикации

COMPOUNDS AND METHODS FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Номер: US20130190289A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

A compound is represented by Structural Formula (I): 2. (canceled)47-. (canceled)8. The compound of claim 3 , wherein:{'sup': '1', 'sub': 1-6', '1', '6, 'Ris Calkyl optionally substituted with one or more substituents selected from the group consisting of halogen, —CN, —OH, and —O(C-Calkyl);'}{'sup': '2', 'sub': 5', '8', '2', '1', '6', '1', '6', '2', '1', '6', '1', '6', '2', '2', '1', '6', '1', '6', '1', '6', '1', '6', '2', '1', '6', '1', '6', '1', '6', '1', '6', '2', '2', '1', '6', '1', '6', '1', '6', '3-7', '3-7, 'Ris C-Ccycloalkyl optionally substituted with one or more substituents selected from the group consisting of halogen; oxo; —CN; —OH; —NH; —NH(C-Calkyl); —N(C-Calkyl): —OCO(C-Calkyl); —CO(C-Calkyl); —COH; —CO(C-Calkyl); —O(C-Calkyl); —O(C-Chaloalkyl); and a C-Caliphatic group optionally substituted with one or more substituents selected from the group consisting of halogen, oxo, —CN, —OH, —NH, —NH(C-Calkyl), —N(C-Calkyl), —OCO(C-Calkyl), —CO(C-Calkyl), —COH, —CO(C-Calkyl), —O(C-Calkyl), —O(C-Chaloalkyl), Ccycloalkyl, Ccyclo(haloalkyl), and phenyl.'}{'sup': a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a, 'sub': 2', '2', '2', '7', '3-8, 'each Q independently is selected from the group consisting of halogen; cyano; nitro; —OR; —SR; —S(O)R; —SOR; —NRR; —C(O)R; —C(O)OR; —OC(O)R; —NRC(O)R; —C(O)NRR; —NRC(O)NRR; —NRC(O)OR; —NRC(═NR)NRR, —OCONRR; —C(O)NRC(O)OR; —C(═NR)R; —C(═NOR)R; —SONRR; —NRSOR; —NRSONRR; —OP(O)(OR)OR; optionally substituted Ccarbocyclic; 4-8 membered, optionally substituted heterocyclyl; optionally substituted phenyl; and optionally substituted, 5-6 membered heteroaryl;'}{'sup': 1A', '2A', '7A', '9A', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a', 'a, 'sub': 2', '3-8', '3-8, 'each of J, J, J, and Jindependently is halogen, oxo, —CN, —OR, —NRR, —OCOR, —COR, —COR, —NRC(O)R, —C(O)NRR, —NRC(O)NRR, —NRC(O)OR, —OCONRR, Ccycloalkyl, Ccyclo(haloalkyl), or phenyl;'}{'sup': 1B', '2B', '7B', '9B', ...

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25-07-2013 дата публикации

SULFUR DERIVATIVES AS CHEMOKINE RECEPTOR MODULATORS

Номер: US20130190338A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors. 2. A compound according to claim 1 , wherein:{'sup': '5', 'Ris S.'}3. A compound according to claim 1 , wherein:{'sup': '5', 'Ris —S(O)—.'}4. A compound according to claim 1 , wherein:{'sup': '5', 'sub': '2', 'Ris —S(O)—.'}5. A compound according to claim 1 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': 1-6', '3-8', '3-8, 'Ris substituted or unsubstituted Calkyl, substituted or unsubstituted Ccycloalkyl or substituted or unsubstituted Ccycloalkenyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '18', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl or halogen;'}{'sup': '7', 'sub': 1-6', '1-6', '3-8, 'Ris H, halogen, CN, —OCalkyl, substituted or unsubstituted Calkyl or substituted or unsubstituted Ccycloalkyl; and'}{'sup': '8', 'sub': '1-6', 'Ris H, substituted or unsubstituted Calkyl, CN or halogen.'}6. A compound according to claim 5 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'sub': '1-6', 'Ris substituted or unsubstituted Calkyl;'}{'sup': '5', 'sub': '2', 'Ris —S—, —S(O)—, or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '17', 'Ris H;'}{'sup': '18', 'Ris H;'}{'sup': '7', 'sub': '1-6', 'Ris H, halogen or Calkyl; and'}{'sup': '8', 'Ris H or CN.'}7. A compound according to claim 6 , wherein:{'sup': '1', 'Ris H;'}{'sup': '2', 'Ris methyl propionate, methyl-2-benzoic acid, methyl-2-methylbenzoate, methyl-3-methylphenylacetamide, methyl-3-methylphenylsulfonamide, methyl acetic acid, methyl-2-methylphenylcarboxylate or propionic acid;'}{'sup': '5', 'sub': '2', 'Ris —S(O)—, S or —S(O)—;'}{'sup': '6', 'Ris optionally substituted 1-benzofuran;'}{'sup': '7', 'Ris chlorine, ...

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25-07-2013 дата публикации

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Номер: US20130190356A1
Принадлежит: Genentech, Inc.

Compounds of the formula I: 2. The compound of claim 1 , wherein C is a group of formula (i).3. The compound of claim 2 , wherein A is a group of formula (a).4. The compound of claim 3 , wherein B is a group of formula (e).5. The compound of claim 3 , wherein B is a group of formula (f).6. The compound of claim 3 , wherein m is 0.7. The compound of claim 3 , wherein m is 1.8. The compound of claim 3 , wherein Rand Rare hydrogen.9. The compound of claim 3 , wherein Rand Rare hydrogen.10. The compound of claim 3 , wherein Ris: Calkyl; Ccycloalkyl; or Ccycloalkyl-Calkyl; each of which may be optionally substituted one or more times with halo.11. The compound of claim 3 , wherein Ris Calkyl.12. The compound of claim 3 , wherein Ris isobutyl.14. The compound of claim 13 , wherein Ris: —SO—R; —(CH)—C(O)—NRR; —(CH)—SO—NRR; —(CH)—NR—C(O)—R; or —(CH)—NR—SO—R.18. A composition comprising:(a) a pharmaceutically acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) a compound of .'}19. A method for treating arthritis claim 1 , said method comprising administering to a subject in need thereof an effective amount of a compound of . This application claims the benefit under 35 USC §119 of U.S. Provisional Application Ser. No. 61/579,255 filed on Dec. 22, 2011, the disclosure of which is incorporated herein by reference.The invention pertains to compounds that modulate the function of retinoid-receptor related orphan receptor RORc (RORγ) and use of such compounds for treatment of autoimmune diseases.T helper 17 cells (Th17) are interleukin (IL)-17 secreting CD4+ T cells involved in pathogenesis of autoimmune diseases such as rheumatoid arthritis, irritable bowel disease, psoriasis, psoriatic arthritis and spondyloarthridities. The retinoic acid-related orphan receptor γ (RORγ or RORc) is recognized as a transcription factor necessary for Th17 cell differentiation. RORc is an orphan member of the nuclear hormone receptor subfamily that includes RORα (RORa) ...

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25-07-2013 дата публикации

APOPTOSIS PROMOTERS

Номер: US20130190488A1
Принадлежит: ABBOTT LABORATORIES

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member. 19-. (canceled)10. A compound , or a therapeutically acceptable salt thereof , wherein the compound is selected from the group consisting of:N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(5,6-dihydro-1(4H)-pyrimidin-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(2,4-dimenthyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-methyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(4,4-dimethyl-4,5-dihydro-1H-imidazol-1-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((2-(4-chlorophenyl)-1-cyclohexen-1-yl)methyl)piperazin-1-yl(benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)oxy)-3-(trifluoromethyl)benzenesulfonamide;N-(4-(4-((2-(4-chlorophenyl)cyclohept-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-(trifluoromethyl)benzenesulfonamide;4-(((1R)-3-(bis(2-methoxyethyl)amino)-1 ...

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25-07-2013 дата публикации

PHENYLALKYL N-HYDROXYUREAS FOR TREATING LEUKOTRIENE RELATED PATHOLOGIES

Номер: US20130190514A1
Принадлежит: TALLIKUT PHARMACEUTICALS, INC.

The method of treating patients by administering N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea for treatment of leukotriene related pathologies, and compositions for this use. 1. A composition comprising R- and S-enantiomers of N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea or pharmaceutically effective salts thereof wherein the composition comprises less than 2% of the S-enantiomer.2. The composition of claim 1 , wherein the composition comprises less than 1% of the S-enantiomer.3. The composition of claim 1 , wherein the composition consists of R- and S-enantiomers of N-[3-[5-[(4-fluorophenyl)methyl]-2-thienyl]-1-methyl-2-propynyl]-N-hydroxyurea or pharmaceutically effective salts thereof.4. The composition of claim 3 , wherein the composition consists of less than 1% of the S-enantiomer.5. The composition of claim 1 , wherein the composition is provided in a unit dosage form for oral administration and wherein the composition is present in an amount of about 25-100 mg.6. The composition of claim 5 , wherein the composition is present in an amount of about 25 claim 5 , 50 claim 5 , 75 claim 5 , or 100 mg.7. The composition of claim 5 , wherein the composition is present in an amount of about 100 mg.8. The composition of claim 5 , wherein said unit oral dosage form is a tablet or capsule.9. The composition of for use in treating a leukotriene related pathology in a subject in need thereof.10. The composition for use of claim 9 , wherein the subject is a human.11. The composition for use of claim 9 , wherein the pathology is heart attack claim 9 , stroke claim 9 , peripheral arterial disease claim 9 , a cardiovascular disease claim 9 , an inflammatory disease claim 9 , a cancer claim 9 , ischemia induced myocardial injury claim 9 , central nervous system pathology resulting from formation of leukotrienes following stroke or subarachnoid hemorrhage claim 9 , allergy claim 9 , or a fibrotic disease.12. ...

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01-08-2013 дата публикации

Alkaloid aminoester derivatives and medicinal composition thereof

Номер: US20130196978A1
Принадлежит: Chiesi Farmaceutici SpA

Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.

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