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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 43395. Отображено 100.
10-10-2001 дата публикации

ТАБЛЕТКА

Номер: RU0000019762U1

Таблетка, представляющая собой твердую лекарственную форму антигипертензивного препарата, выполненная из фармацевтической композиции, включающей капторил и целевые добавки, отличающаяся тем, что в качестве целевых добавок содержит лактозу, микрокристаллическую целлюлозу, крахмал кукурузный, кислоту стеариновую и стеарат кальция, при следующем соотношении компонентов, мас.%: Каптоприл - 23,125-26,875 Лактоза - 47,7485-55,4915 Микрокристаллическая целлюлоза - 9,25-10,75 Крахмал кукурузный - 9,6015-11,1585 Кислота стеариновая - 1,8-2,2 Стеарат кальция - 0,9-1,1 (19) RU (11) 19 762 (13) U1 (51) МПК A61K 9/20 (2000.01) C07D 207/00 (2000.01) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К СВИДЕТЕЛЬСТВУ (21), (22) Заявка: 2001116993/20 , 28.06.2001 (24) Дата начала отсчета срока действия патента: 28.06.2001 (46) Опубликовано: 10.10.2001 (72) Автор(ы): Нестерук В.В., Сыров К.К. (73) Патентообладатель(и): Нестерук Владимир Викторович, Сыров Кирилл Константинович U 1 1 9 7 6 2 R U Ñòðàíèöà: 1 U 1 (57) Формула полезной модели Таблетка, представляющая собой твердую лекарственную форму антигипертензивного препарата, выполненная из фармацевтической композиции, включающей капторил и целевые добавки, отличающаяся тем, что в качестве целевых добавок содержит лактозу, микрокристаллическую целлюлозу, крахмал кукурузный, кислоту стеариновую и стеарат кальция, при следующем соотношении компонентов, мас.%: Каптоприл - 23,125-26,875 Лактоза - 47,7485-55,4915 Микрокристаллическая целлюлоза - 9,25-10,75 Крахмал кукурузный - 9,6015-11,1585 Кислота стеариновая - 1,8-2,2 Стеарат кальция - 0,9-1,1 1 9 7 6 2 (54) ТАБЛЕТКА R U Адрес для переписки: 121059, Москва, ул.Брянская, 3А, Е.Г.Павельевой (71) Заявитель(и): Нестерук Владимир Викторович, Сыров Кирилл Константинович RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1 RU 19 762 U1

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05-01-2012 дата публикации

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

Номер: US20120004206A1

The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.

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12-01-2012 дата публикации

Acid-free quaternized nitrogen compounds and use thereof as additives in fuels and lubricants

Номер: US20120010112A1
Принадлежит: BASF SE

The present invention relates to novel acid-free quaternized nitrogen compounds, to the preparation thereof and to the use thereof as a fuel and lubricant additive, more particularly as a detergent additive, as a wax antisettling additive (WASA) or as an additive for reducing internal diesel injector deposits (IDID); to additive packages which comprise these compounds; and to fuels and lubricants thus additized. The present invention further relates to the use of these acid-free quaternized nitrogen compounds as a fuel additive for reducing or preventing deposits in the injection systems of direct-injection diesel engines, especially in common-rail injection systems, for reducing the fuel consumption of direct-injection diesel engines, especially of diesel engines with common-rail injection systems, and for minimizing power loss in direct-injection diesel engines, especially in diesel engines with common-rail injection systems.

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12-01-2012 дата публикации

11-Beta-Hydroxysteroid Dehydrogenase Type 1 Active Compounds

Номер: US20120010194A1
Принадлежит: High Point Pharnaceuticals LLC

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

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12-01-2012 дата публикации

Optically active 3-amino-2,5-dioxopyrrolidine-3-carboxylate, process for production of the compound, and use of the compound

Номер: US20120010405A1
Принадлежит: Individual

The present invention provides a compound of the formula (III): wherein R is a C 1-6 alkyl group, as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being a promising therapeutic agent for diabetic complications in a short process, in an economically advantageous manner and in high yields, and the process for preparing the same.

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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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26-01-2012 дата публикации

Pyrrolidine triple reuptake inhibitors

Номер: US20120022125A1
Автор: Jianguo Ma, Liming Shao
Принадлежит: SUNOVION PHARMACEUTICALS INC

In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and/or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

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26-01-2012 дата публикации

Process for Preparing Dithiine-tetracarboxy-diimides

Номер: US20120022270A1
Принадлежит: Bayer CropScience AG

The present invention relates to a new process for preparing dithiine-tetracarboxy-diimides

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26-01-2012 дата публикации

Novel method for producing optically active pyrrolidine compound

Номер: US20120022271A1
Принадлежит: Astellas Pharma Inc

[Object] A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided. [Means for Solution] According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate. [Selected Figure] None

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02-02-2012 дата публикации

3-biphenyl-substituted-3-substituted-4-ketolactam and ketolactone and their utilization as pesticide

Номер: US20120028804A1

The present invention relates to novel 3-biphenyl-substituted, 3-substituted 4-ketolactams and -lactones of the formula (I) in which A, B, Q, G, W, X, Y and Z are as defined in the disclosure, to processes for their preparation, and to their use as pesticides and/or microbicides and/or herbicides.

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02-02-2012 дата публикации

Novel Crystalline Form of Atorvastatin Hemi-calcium Salt, Hydrate Thereof, And Method of Producing The Same

Номер: US20120029207A1
Принадлежит: KYONGBO PHARM

The present invention provides a novel crystalline form of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-mthylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptanoic acid hemi-calcium salt (atorvastatin hemi-calcium salt) of the following formula 1, which is known to be useful as a drug, a hydrate thereof and a preparation method thereof:

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16-02-2012 дата публикации

Dihydrolipoic Acid Derivatives Comprising Nitric Oxide and Therapeutic Uses Thereof

Номер: US20120041025A1
Автор: Sampath Parthasarathy
Принадлежит: Invasc Therapeutics Inc

Compounds are provided that comprise dinitroso-derivatives of dihydrolipoic acid. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating various diseases and disorders, including angina, hypertension, diabetes, dyslipidemia, renal insufficiency, myocardial infarction, stroke, atherosclerosis, and the target organ damage that accompanies these various diseases and disorders, are further provided. The compounds are useful in improving vasodilation, reducing low-density lipoprotein oxidation, and reducing inflammation in a subject.

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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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15-03-2012 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20120065408A1
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

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22-03-2012 дата публикации

Metallo-beta-lactamase inhibitors

Номер: US20120071457A1
Принадлежит: Individual

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

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29-03-2012 дата публикации

Compounds act at multiple prostaglandin receptors giving a general anti-inflammatory response

Номер: US20120077858A1
Принадлежит: Allergan Inc

The present invention provides compounds, that are N-alkyl-2-(1-(5-substituted-2-(3-oxo-3-(trifluoromethylsulfonamido)propyl)benzyl)pyrrolidin-2-yl)oxazole-4-carboxamide wherein the 5 substituent is selected from the group consisting of halo and alkyloxy radicals. The compound may be represented by the following formula wherein R 1 is selected from the group consisting of CO 2 R 7 and CON(R 7 )SO 2 R 7 wherein R 1 , R 2 , R 3 , R 4 , and R 7 are as defined in the specification. The compounds may be administered to treat DP 1 , FP, EP 1 , EP 3 , TP and/or EP 4 receptor mediated diseases or conditions.

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05-04-2012 дата публикации

Ionic liquids, the method for preparing the same and method for removing acetylenes from olefin mixtures using the ionic liquids

Номер: US20120083642A1

There are provided an ionic liquid having ether group(s) in which a copper(I) compound is included, a method for preparing the same, and a method for removing traces amounts of acetylene-based hydrocarbon compounds included in olefin by absorption or extraction using the same. When the disclosed solution is used, oxidation of Cu(I) to Cu(II) is prevented since CuX is stabilized by the ionic liquid. Thus, selective removal efficiency of acetylenic compounds is improved greatly while the removal performance is retained for a long period of time. Further, since the solution according to the present disclosure is applicable as an extractant as well as an absorbent, the associated operation is simple and apparatus cost can be decreased.

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12-04-2012 дата публикации

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

Номер: US20120088797A1
Принадлежит: Takeda Pharmaceutical Co Ltd

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

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19-04-2012 дата публикации

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

Nitrogen-Containing Ligands And Their Use In Atomic Layer Deposition Methods

Номер: US20120108062A1
Принадлежит: Applied Materials Inc

Methods for deposition of elemental metal films on surfaces using metal coordination complexes comprising nitrogen-containing ligands are provided. Also provided are nitrogen-containing ligands useful in the methods of the invention and metal coordination complexes comprising these ligands.

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03-05-2012 дата публикации

Nitrogen-containing aromatic heterocyclyl compound

Номер: US20120108639A1
Принадлежит: Daiichi Sankyo Co Ltd

The present invention provides a compound having excellent regulating action on blood lipid level that is represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein, in one embodiment, A represents a 5-membered nitrogen-containing aromatic heterocyclyl group; R 1 represents COOH; each R 2 represents an alkyl; each R 3 represents an optionally substituted phenyl, an optionally substituted phenylalkyl; m represents 0, 1, 2, or 3; n represents 0 or 1; each of R 4 , R 5 , R 6 , and R 7 represents H, an alkyl; and B represents an optionally substituted naphthyl, an optionally substituted aromatic heterocyclyl, or a group represented by the following formula (II) wherein each of B 1 and B 2 represents an optionally substituted phenyl or an optionally substituted aromatic heterocyclyl.

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03-05-2012 дата публикации

Disubstituted-aminodifluorosulfinium salts, process for preparing same and method of use as deoxofluorination reagents

Номер: US20120108801A1
Принадлежит: OMEGACHEM INC

The invention relates to disubstituted-aminodifluorosulfinium salts represented by the formula (I). Processes for preparing same and methods of use as deoxofluorinating reagent is also provided.

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10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Принадлежит: Kyowa Hakko Kirin Co Ltd

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

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17-05-2012 дата публикации

Substituted carbamoylcycloalkyl acetic acid derivatives as nep

Номер: US20120122764A1
Принадлежит: NOVARTIS AG

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

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17-05-2012 дата публикации

Compounds, Compositions and Methods for Modulating Uric Acid Levels

Номер: US20120122780A1
Принадлежит: Ardea Biociences Inc

Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

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17-05-2012 дата публикации

Novel crystalline form of atorvastatin hemi-calcium salt, hydrate thereof, and method of producing the same

Номер: US20120123132A1
Принадлежит: KYONGBO PHARM

The present invention provides a novel crystalline form of [R-(R * ,R * )]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-mthylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-heptanoic acid hemi-calcium salt (atorvastatin hemi-calcium salt) of the following formula 1, which is known to be useful as a drug, a hydrate thereof and a preparation method thereof:

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24-05-2012 дата публикации

Novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids and their uses as cooling compounds

Номер: US20120129827A1
Автор: Arkadiusz Kazimierski

The present invention relates to novel derivatives of 1-alkyl-6-oxo-piperidine-3-carboxylic acids and 1-alkyl-5-oxo-pyrrolidine-3-carboxylic acids represented by Formula I: wherein n is an integer of 1 or 2; R 1 , R 2 , R 3 , and R 4 are each independently selected from the group consisting of hydrogen and methyl; X is selected from the group consisting of oxygen and nitrogen; and R 5 is hydrogen or a C 1 -C 7 linear or branched acyclic hydrocarbon group, or R 5 together with X form a 3- to 8-membered heterocyclic hydrocarbon group, and their uses as cooling compounds.

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07-06-2012 дата публикации

Soft anticholinergic zwitterions

Номер: US20120141401A1
Автор: Nicholas S. Bodor
Принадлежит: Bodor Nicholas S

Soft anticholinergic zwitterions of the formulas: wherein R 1 and R 2 are both phenyl or one of R 1 and R 2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

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07-06-2012 дата публикации

Pyrrolidine Compounds Which Modulate The CB2 Receptor

Номер: US20120142677A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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07-06-2012 дата публикации

Compounds as bradykinin b1 antagonists

Номер: US20120142695A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

Compounds of the formula I wherein n, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 and X are defined as described in the specification, which are bradykinin B1 antagonists, and their use as medicaments.

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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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28-06-2012 дата публикации

Nitrogen-Based Linkers for Attaching Modifying Groups to Polypeptides and Other Macromolecules

Номер: US20120165275A1
Принадлежит: Affymax Inc

Compounds comprising a peptide moiety, a linker moiety and a water-soluble polymer moiety such as a poly(ethylene glycol) moiety are disclosed. Various linker moieties for use in these compounds are also disclosed, along methods for their synthesis.

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12-07-2012 дата публикации

Rho kinase inhibitors

Номер: US20120178752A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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02-08-2012 дата публикации

IAP BIR domain binding compounds

Номер: US20120195915A1
Принадлежит: Pharmascience Inc

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

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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30-08-2012 дата публикации

Selective calcium channel modulators

Номер: US20120220564A1
Принадлежит: Zalicus Pharmaceuticals Ltd

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an aπl ring as shown in formula (I).

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30-08-2012 дата публикации

Process for reduction of alpha-acyloxy sulfide derivatives

Номер: US20120220784A1
Принадлежит: Scinopharm Singapore Pte Ltd

The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding α-acyloxy sulfides.

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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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06-09-2012 дата публикации

Process for preparing alpha-carboxamide derivatives

Номер: US20120226053A1
Автор: Matthew Allen Zajac
Принадлежит: Convergence Pharmaceuticals Ltd

The present application provides a process for the preparation of α-carboxamide pyrrolidine derivatives of formula (I), wherein R 1 and R 2 are independently hydrogen, C 1-6 alkyl or C 3-6 cycloalkylC 1-6 alkyl; or such R 1 and R 2 , together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R 5 is independently selected from the list consisting of C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; either R 6 or R 7 is —O—R 8 , —OCHR 9 R 8 ,—NCH 2 R 8 or —(CH 2 ) 2 R 8 wherein the other R 6 or R 7 is hydrogen or R 5 ; and wherein R 8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; and R 9 is hydrogen or C 1-3 alkyl.

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13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
Принадлежит: Sarcode Bioscience Inc

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

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13-09-2012 дата публикации

Tri-, tetra-substituted-3-aminopyrrolidine derivative

Номер: US20120232288A1
Принадлежит: Daiichi Pharmaceutical Co Ltd

An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.

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20-09-2012 дата публикации

Luminogen compounds and the use of the same for biosensing and cellular imaging

Номер: US20120237964A1

Provided herein are a luminogen compound of formula (I) including a AIE luminophore moiety conjugated with a maleimide moiety and a use of the same for detecting thiol groups in biomolecules. Also provided is a dye molecule, a biosensor or a bioprobe comprising the luminogen compound of formula (I) in use for detecting thiol groups in biomolecules. The detection method of the present subject matter not only has high thio-selectivity and sensitivity, but also is rapid, convenient and handy.

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18-10-2012 дата публикации

Salt forms of [R-(R*,R*)]-2-(4-flurorophenyl)-beta, delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid

Номер: US20120264934A1
Принадлежит: PFIZER INC

Novel salt forms of [R—(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.

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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

Process of making alpha-aminooxyketone/alpha-aminooxyaldehyde and alpha-hydroxyketone/alpha-hydroxyaldehyde compounds and a process making reaction products from cyclic alpha, beta-unsaturated ketone substrates and nitroso substrates

Номер: US20120302792A1
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY

The present invention is directed to a process of making α-aminooxyketone and α-hydroxyketone compounds. The synthetic pathway generally involves reacting an aldehyde or ketone substrate and a nitroso substrate in the presence of a catalyst of the formula (IV): wherein X a -X c represent independently nitrogen, carbon, oxygen or sulfur and Z represents a 4 to 10-membered ring with or without a substituent and optionally a further step to convert the α-aminooxyketone compound formed to the α-hydroxyketone compound. The present invention results in α-aminooxyketone and α-hydroxyketone compounds with high enantioselectivity and high purity. The present invention is also directed to a catalytic asymmetric O-nitroso Aldol/Michael reaction. The substrates of this reaction are generally cyclic α,β-unsaturated ketone substrate and a nitroso substrate. This methodology generally involves reacting the cyclic α,β-unsaturated ketone substrate and the nitroso substrate in the presence of a proline-based catalyst, to provide a heterocyclic product.

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06-12-2012 дата публикации

3-phenoxymethylpyrrolidine compounds

Номер: US20120309985A1
Принадлежит: Theravance Inc

In one aspect, the invention relates to compounds of formula I: where R 1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

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13-12-2012 дата публикации

Method for Producing Curing Agent Having Acidic Substituent and Unsaturated Maleimide Group, Thermosetting Resin Composition, Prepreg, and Laminate

Номер: US20120316263A1
Принадлежит: Individual

A method for producing a curing agent having an acidic substituent and an unsaturated maleimido group, including reacting, in an organic solvent, a maleimide compound (a) having at least two N-substituted maleimido groups in a molecule thereof with an amine compound (b) having an acidic substituent (represented by formula (I) below); a thermosetting resin composition containing the curing agent (A) produced through the method and a compound (B) which is cured with the curing agent, wherein a cured product of the composition has a glass transition temperature of 200° C. or higher; and a prepreg and a laminated sheet produced therefrom. The thermosetting resin composition can produce a prepreg or laminated sheet exhibiting excellent performance suitable for a printed wiring board for electronic devices and similar devices.

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20-12-2012 дата публикации

Method for Obtaining Novel Derivatives of Naphthalene for the In Vivo Diagnosis of Alzheimer's Disease

Номер: US20120321560A1

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R 1 :-alkylenyl-C(O)NH-alkylenyl-R 3 , -alkylenyl-C(O)O—R 4 , R 3 :—COOH, —OH, —SH, —NH 2 , -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R 4 : H, succinimidyl group, R 2 : —H,-alkyl. In II: R 1 : -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R 2 : -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN) 2 , —HC═CHNO 2 , -alkylenyl-NH 2 , -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

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20-12-2012 дата публикации

Development of Novel Detergents for Use in PCR Systems

Номер: US20120322066A1
Принадлежит: Life Technologies Corp

This disclosure relates to novel detergents for use in various procedures including, for example, nucleic acid amplification reactions such as polymerase chain reaction (PCR). Methods for preparing the modified detergents are also described.

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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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03-01-2013 дата публикации

Cyclic amine bace-1 inhibitors having a benzamide substituent

Номер: US20130004518A1
Принадлежит: Merck Sharp and Dohme LLC

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

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10-01-2013 дата публикации

Cross-linkers and their uses

Номер: US20130011419A1
Принадлежит: Immunogen Inc

Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

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24-01-2013 дата публикации

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

Номер: US20130023539A1
Принадлежит: Euroscreen SA

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

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31-01-2013 дата публикации

Novel maytansinoid derivatives with peptide linker and conjugates thereof

Номер: US20130029900A1
Автор: Wayne C. Widdison
Принадлежит: Immunogen Inc

The invention relates to novel cell-binding agent-cytotoxic agent conjugate having a peptide linkers and more specifically to conjugates of formula (I). The invention also provides novel cytotoxic agents of formula (II), linker compounds represented by formula (III), and drug-linker compounds represented by formula (IV). The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

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14-02-2013 дата публикации

Electroluminescent materials comprising fluorene derivatives

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

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

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14-02-2013 дата публикации

Chemoselective enrichment for compound isolation

Номер: US20130041106A1

Chemoselective isolation of hydroxyl group-containing and carboxyl group-containing compounds is accomplished via formation of polymeric silyl ethers and polymeric siloxyl esters, respectively. Preparation of chemoselective polymeric reagents for capture of hydroxyl group containing compounds and carboxyl group containing compounds is described.

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21-02-2013 дата публикации

Compositions and Methods for Enhancing Proteasome Activity

Номер: US20130045992A1
Принадлежит: Harvard College

Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp 14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

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14-03-2013 дата публикации

MODULATION OF BIOACTIVE EPOXY-FATTY ACID LEVELS BY PHOSPHODIESTERASE INHIBITORS

Номер: US20130065936A1

The present invention provides method for increasing levels of epoxygenated fatty acids by administration of a phosphodiesterase inhibitor. 1. A method of increasing levels of epoxygenated fatty acids in a subject in need thereof comprising administering to the subject an inhibitor of a phosphodiesterase.2. The method of claim 1 , wherein the ratio of epoxygenated fatty acids to dihydroxy fatty acids is increased without changing the levels of dihydroxy fatty acids.3. The method of claim 1 , wherein soluble epoxide hydrolase is not inhibited.4. The method of claim 1 , wherein the inhibitor of phosphodiesterase is an inhibitor of PDE4.5. The method of claim 4 , wherein the inhibitor of PDE4 is selected from the group consisting of rolipram claim 4 , roflumilast claim 4 , cilomilast claim 4 , ariflo claim 4 , HT0712 claim 4 , ibudilast claim 4 , mesembrine claim 4 , pentoxifylline claim 4 , piclamilast claim 4 , and combinations thereof.6. The method of claim 1 , wherein the inhibitor of phosphodiesterase is an inhibitor of PDE5.7. The method of claim 1 , wherein the inhibitor of phosphodiesterase is administered in a subtherapeutic dose.8. The method of claim 1 , further comprising administration of an inhibitor of soluble epoxide hydrolase.9. The method of claim 8 , wherein the inhibitor of soluble epoxide hydrolase is administered in a subtherapeutic dose.10. The method of claim 1 , wherein the epoxygenated fatty acids are cis-epoxyeicosantrienoic acids (“EETs”) claim 1 , epoxides of linoleic acid claim 1 , epoxides of eicosapentaenoic acid (“EPA”) or epoxides of docosahexaenoic acid (“DHA”) claim 1 , or a mixture thereof.11. A method of obtaining analgesic claim 1 , anti-convulsant claim 1 , anti-depressant claim 1 , anti-inflammatory claim 1 , anti-hypertensive claim 1 , cardioprotective claim 1 , organ protective effects in a subject in need thereof claim 1 , comprising administering to the subject an inhibitor of phosphodiesterase.12. A method of reducing claim ...

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21-03-2013 дата публикации

ARALKYL DIAMINE DERIVATIVES AND USES THEREOF AS ANTIDEPRESSANTS

Номер: US20130072488A1

Aralkyl diamine derivative of the following formula, pharmaceutically acceptable salts or uses thereof as antidepressants. The derivatives have triplex inhibiting activities of the reuptake of 5-HT, dopamine and noradrenalin, which can be administered to the patients in need of such treatment in the form of compositions orally or injectedly et al. 2. The compound according to claim 1 , wherein the substituted amino group is an amino group substituted with C-Calkyl or C-Chaloalkyl.3. The compound according to claim 1 , wherein the substituted phenyl or the substituted benzyl has 1-4 substituents on the benzene ring claim 1 , with R claim 1 , Rand Rrepresenting the substituents.4. The compound according to claim 1 , wherein the salt is a pharmaceutically acceptable inorganic or organic salt.5. The compound according to claim 4 , wherein the hydrate contains 0.5-3 molecules of crystal water.6. The compound according to claim 1 , wherein the compound is selected from the group consisting of:VI-1 N,N-diethyl-3-(3,4-dichlorophenyl)-3-(pyrrolidin-1-yl)-propylamine,VI-2 N,N-dimethyl-3-(3,4-dichlorophenyl)-3-(pyrrolidin-1-yl)-propylamine,VI-3 N,N-dimethyl-3-(3,4-dichlorophenyl)-3-(piperazin-1-yl)-propylamine,VI-4 N,N-dimethyl-3-(3,4-dichlorophenyl)-3-morpholinyl-propylamine,VI-5 N-methyl-N-benzyl-3-(3,4-dichlorophenyl)-3-morpholinyl-propylamine,VI-6 4-(3-(3,4-dichlorophenyl)-3-(pyrrolidin-1-yl)propylmorpholine,VI-7 N,N-dimethyl-3-(3,4-dichlorophenyl)-3-piperidyl-propylamine,VI-8 N,N-dimethyl-3-(4-chlorophenyl)-3-morpholinyl-propylamine,VI-9 4-(3-(4-chlorophenyl)-3-(pyrrolidin-1-yl)propylmorpholine,VI-10 N,N-dimethyl-3-(4-methylphenyl)-3-morpholinyl-propylamine,VI-11 4-(3-(4-methylpiperazin-1-yl)-1-(4-methylphenyl)propylmorpholine,VI-12 4-(3-(4-methylphenyl)-3-(morpholinyl)propylpyrrole,VI-13 N,N-dimethyl-3-(benzothiophen-3-yl)-3-(pyrrolidin-1-yl)-propylamine,VI-14 N-methyl-N-benzyl-3-(benzothiophen-3-yl)-3-(pyrrolidin-1-yl)-propylamine,VI-15 N-methyl-3-(benzothiophen-3-yl)-3 ...

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28-03-2013 дата публикации

Novel Isobaric Tandem Mass Tags for Quantitative Proteomics and Peptidomics

Номер: US20130078728A1
Принадлежит:

Compositions and methods of tagging peptides and other molecules using novel isobaric tandem mass tagging reagents, including novel N,N-dimethylated amino acid 8-plex and 16-plex isobaric tandem mass tagging reagents. The tagging reagents comprise: a) a reporter group having at least one atom that is optionally isotopically labeled; b) a balancing group, also having at least one atom that is optionally isotopically labeled, and c) an amine reactive group. The tagging reagents disclosed herein serve as attractive alternatives for isobaric tag for relative and absolute quantitation (iTRAQ) and tandem mass tags (TMTs) due to their synthetic simplicity, labeling efficiency and improved fragmentation efficiency. 2. The method of further comprising identifying one or more fragments of the labeled molecule using mass spectrometry.3. The method of further comprising quantifying amounts of said one or more fragments of the labeled molecule.5. The method of wherein Ris selected from the group consisting of:{'sup': 12', '13, 'a) a methyl group containing one or more deuterium atoms and wherein the carbon is C or C;'}b) hydrogen;c) deuterium;{'sup': '13', 'd) an isopropyl group containing one or more deuterium atoms and one or more C atoms; and'}{'sup': '13', 'e) a butyl group containing one or more deuterium atoms and one or more C atoms.'}6. The method of wherein said molecule is a peptide claim 1 , metabolite or neurotransmitter.7. The method of where labeling the peptide comprises the step of reacting the amine reactive group of the tagging reagent with the N-terminus of the peptide or with an ε-amino group within peptide.8. A method of analyzing a mixture containing target molecules comprising the steps of:a) labeling target molecules within a first sample with a first tagging reagent, thereby generating first labeled target molecules;b) labeling target molecules within at least one additional sample with at least one additional tagging reagent, thereby generating ...

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28-03-2013 дата публикации

HETEROCYCLIC COMPOUND AND p27Kip1 DEGRADATION INHIBITOR

Номер: US20130079306A1
Принадлежит: Individual

A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27 Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.

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28-03-2013 дата публикации

NOVEL SULFONYLPYRROLES

Номер: US20130079347A1
Принадлежит: ALTANA PHARMA AG

Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors. 120-. (canceled)22. A method according to claim 21 , wherein the compound of formula I is selected from the group consisting of1. (E)-N-Hydroxy-3-[1-(toluene-4-sulfonyl)-1-H-pyrrol-3-yl]-acrylamide,2. N-Hydroxy-3-(1-phenylmethanesulfonyl-1H-pyrrol-3-yl)-acrylamide,3. (E)-3-[1-(Biphenyl-4-sulfonyl)-1H-pyrrol-3-yl]-N-hydroxy-acrylamide,4. (E)-3-[1-(4-Dimethylamino-benzenesulfonyl)-1H-pyrrol-3-yl]-N-hydroxy-acrylamide,5. (E)-N-(2-Amino-phenyl)-3-[1-(toluene-4-sulfonyl)-1H-pyrrol-3-yl]-acrylamide,6. (E)-N-(2-Amino-phenyl)-3-(1-phenylmethanesulfonyl-1H-pyrrol-3-yl)-acrylamide,7. (E)-N-(2-Amino-phenyl)-3-[1-(biphenyl-4-sulfonyl)-1H-pyrrol-3-yl]-acrylamide,8. (E)-N-(2-Amino-phenyl)-3-[1-(4-dimethylamino-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylamide,9. (E)-N-Hydroxy-3-(1-[4-(([2-(1H-indol-2-yl)-ethyl]-methyl-amino)-methyl)-benzene sulfonyl]-1H-pyrrol-3-yl)-acrylamide,10. (E)-3-[1-(4-Dimetylaminomethyl-benzenesulfonyl)-1H-pyrrol-3-yl]-N-hydroxy-acrylamide,11. (E)-N-Hydroxy-3-[1-(4-{[(pyridin-3-ylmethyl)-amino]-methyl}-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylamide,12. (E)-N-Hydroxy-3-[1-(4-{[(1H-indol-3-ylmethyl)-amino]-methyl}-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylamide,13. (E)-3-{1-[4-(Benzylamino-methyl)-benzenesulfonyl]-1H-pyrrol-3-yl}-N-hydroxy-acrylamide,14. (E)-N-Hydroxy-3-{1-[4-(isobutylamino-methyl)-benzenesulfonyl]-1H-pyrrol-3-yl}-acrylamide,15. (E)-N-Hydroxy-3-[1-(4-{[(1H-indol-5-ylmethyl)-amino]-methyl}-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylamide,16. (E)-N-Hydroxy-3-[1-(4-{[(pyridin-4-ylmethyl)-amino]-methyl}-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylamide,17. (E)-3-[1-(4-Aminomethyl-benzenesulfonyl)-1H-pyrrol-3-yl]-N-hydroxy-acrylamide,18. (E)-N-Hydroxy-3-[1-(4-pyridin-4-yl-benzenesulfonyl)-1H-pyrrol-3-yl]-acrylamide,19. (E)-N-Hydroxy-3-{1-[4-(1H-pyrazol-4-yl)-benzenesulfonyl]-1H-pyrrol-3-yl}-acrylamide,20. (E)-N ...

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28-03-2013 дата публикации

Substituted Phenylcarbamoyl Alkylamino Arene Compounds and N,N'-BIS-Arylurea Compounds

Номер: US20130079372A1
Принадлежит: MEDIVATION TECHNOLOGIES, INC.

Substituted phenylcarbamoyl alkylamino arenes; substituted phenylthiocarbamyl alkylamino arenes; substituted phenylcarbamoyl alkylamino heteroarenes; substituted phenylthiocarbamyl alkylamino heteroarenes; N-substituted aryl, N′-substituted aryl urea compounds; N-substituted aryl, N′-substituted heteroaryl urea compounds; N-substituted aryl, N′-substituted aryl thiourea compounds and N-substituted aryl, N′-substituted heteroaryl thiourea compounds are provided and may find use as androgen receptor modulators. The compounds may find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer. 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', 'a', 'b, 'sub': 1', '8, '(a) Ris —C-Calkyl-NRR;'}{'sup': 1', 'a', 'b', '2, 'sub': 1', '8, '(b) Ris —C-Calkyl-NRRand Ris halo; or'}{'sup': 1', 'a', 'b', '2, 'sub': 1', '8, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is O;', {'sup': 1', '2, '(iv) Yand Yare both methyl; and'}, '(v) T is C., '(b) Ris —C-Calkyl-NRR, Ris halo, and at least one of (i)-(v) applies3. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein;{'sup': '1', 'sub': 1', '8, '(a) Ris —O—C-Calkyl-NR′R;'}{'sup': 1', 'c', '2, 'sub': 1', '8, '(b) Ris —O—C-Calkyl-NRR and Ris hydrogen; or'}{'sup': 1', 'c', '2, 'sub': 1', '8, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is O;', {'sup': 1', '2, '(iv) Yand Yare both methyl and'}, '(v) T is C, '(c) Ris —O—C-Calkyl-NRR, Ris hydrogen, and at least one of (i)-(v) applies4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', 'e', 'f, '(a) Ris —C(O)NRR;'}{'sup': 1', 'e', 'f', '2, '(b) Ris —C(O)NRRand Ris halo; or'}{'sup': 1', 'e', 'f', '2, 'claim-text': [{'sup': '1', '(i) Wis CN;'}, {'sup': '2', '(ii) Wis perhaloalkyl;'}, '(iii) Z is O;', {'sup': 1', '2, ...

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28-03-2013 дата публикации

ETOMIDATE ANALOGUES THAT DO NOT INHIBIT ADRENOCORTICAL STEROID SYNTHESIS

Номер: US20130079381A1
Принадлежит:

The invention is directed to compounds according to formula (I): where Ris LC(O)OT or LC(O)OLC(O)OT; Ris a substituted or unsubstituted C-Calkyl, C-Calkenyl, or C-Calkynyl, or R; n is an integer from 0 to 5; each Ris independently halogen or R; Rand Rare independently H, halogen, CN or CF; Land Lare each independently a bond, a substituted or unsubstituted C-Calkylene, C-Calkenylene, or C-Calkynylene; and T is H, a substituted or unsubstituted C-Calkyl, C-Calkenyl, or C-Calkynyl, nitrophenol, or cyclopropyl. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and to methods for providing anesthesia in mammals by administering such a pharmaceutical composition. 2. The compound of claim 1 , wherein said compound is present in the form of a pure enantiomer.3. The compound of claim 2 , wherein said enantiomer is the R enantiomer.4. The compound of claim 1 , wherein Ris LC(O)OT.5. The compound of claim 1 , wherein Ris LC(O)OLC(O)OT.6. The compound of claim 1 , wherein Ris selected from the group consisting of CH claim 1 , CHCHand CHCHCH.7. The compound of claim 1 , wherein T is selected from the group consisting of H claim 1 , CH claim 1 , CHCH claim 1 , CHCH(OH)CH claim 1 , and CHCHCH.8. The compound of claim 1 , wherein n is 0 or 1.9. The compound of claim 1 , wherein Ris CH claim 1 , n is 0 claim 1 , Lis a bond claim 1 , and T is H claim 1 , CH claim 1 , CHCH claim 1 , or CHCH(OH)CH.10. The compound of claim 1 , wherein both Rand Rare H.11. The compound of claim 1 , wherein at least one of Rand Ris H and the other is Br or CN.12. The compound of claim 11 , wherein Ris H and Ris Br or CN.13. The compound of claim 11 , wherein Ris Br or CN and Ris H.15. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of and a pharmaceutically acceptable carrier.16. A method for providing anesthesia to a subject comprising administering to said ...

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28-03-2013 дата публикации

Complexes of Ruthenium, Method of Production Thereof And Use Thereof As (Pre)Catalysts of the Metathesis Reaction

Номер: US20130079515A1
Принадлежит: UMICORE AG & CO. KG

The present invention provides ruthenium complexes of the formula 111-. (canceled)13. The complex of claim 12 , wherein X and X′ are chlorine.14. The complex of claim 12 , wherein Ris hydrogen.15. The complex of claim 12 , wherein A is nitrogen.16. The complex of claim 12 , wherein A is carbon with an Rgroup.17. The method for preparing the ruthenium complex of which comprises reacting 8-ethenylquinoline with a Ru carbene catalyst.19. The method of claim 17 , wherein the Ru carbene catalyst comprises an indenylidene residue claim 17 ,20. The method according to claim 17 , wherein the reaction is conducted in the presence of a copper(I) salt.21. The method according to claim 20 , wherein the copper(I) salt is copper(I) chloride.22. The method according to claim 17 , wherein the reaction is performed in a chlorinated solvent claim 17 , an aliphatic solvent claim 17 , a cycloaliphatic solvent or an aromatic hydrocarbon solvent claim 17 , or mixtures thereof.24. An improved process for ring closing metathesis (RCM) claim 12 , wherein the improvement comprise the use of the ruthenium complex of as an initiator or (pre)catalyst.25. An improved process for ring-opening metathesis polymerization (ROMP) claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst.26. An improved process for metathesis of “alkene-alkyne” (ene-yne) type claim 12 , wherein the improvement comprises the use of the ruthenium complex of as an initiator or (pre)catalyst. This application is a continuation application of U.S. patent application Ser. No. 12/303,615, filed Apr. 3, 2009, which in turn is a national stage application of PCT Application No. EP2007/004901, filed Jun. 1, 2007. The disclosures of the above-referenced applications are hereby incorporated by reference into the present disclosure.The invention relates to novel metal complexes with formula 1, whereCompounds of formula 1 occur as two isomers: with formula 1a, in which atoms X ...

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04-04-2013 дата публикации

Method for producing 3-substituted-4-fluoropyrrolidine derivative

Номер: US20130085282A1
Принадлежит: Individual

An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG 1 represents a protecting group for an amino group, R 1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.

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11-04-2013 дата публикации

GOLD COMPLEXES FOR USE IN THE TREATMENT OF CANCER

Номер: US20130090472A1
Принадлежит: UNIVERSITY OF KWAZULU-NATAL

The invention provides compounds of the Formula (I), in which W is independently selected from W, W, W, W, W, or W represents a pair of substituents independently selected from H, alkyl, aryl or amide in which the amide is optionally part of a linking chain, and the Z—Zbonds (n=4-17; n′=n+1) are optionally of any whole or partial bond order, Y is Yor Y represents a pair of substituents independently selected from H, C--Calkyl, Zor Zaryl, or Y is optionally a bridging structure that may comprise one or more C--Camide, C--Cether, or C--Cester groups, R-Rare independently selected from no substituent, a lone pair of electrons, H, halogen, C-Caryl, C- C-alkyl, amine, C--Calkylamine, C--Camide, nitro, cyano, carboxyl, C--Cester, phosphane, thiol, C--Cthioether, OR′, and suitable pairs of adjacent R groups (R-R) may optionally together form part of a Cor Caryl ring, a Zor Zring, R′ is independently selected from H, C--Calkyl, Zor Zaryl, C--Cester, poly(—CO—), amine, and C--Calkylamine, Z-Zare independently selected from C, N, P, O, and S, and X is a pharmaceutically acceptable anion, for the treatment of cancer. 2. The compound of claim 1 , in which the anion is selected from halide claim 1 , hexafluorophosphate claim 1 , nitrate claim 1 , and triflate.3. The compound of claim 1 , in which Y represents two hydrogen atoms or Y.4. The compound of claim 3 , in which Y is Yand Zand Zare N.5. The compound of claim 4 , in which Z-Zare C.6. The compound of claim 1 , in which R-Rare selected from H claim 1 , C-Calkyl claim 1 , O—C-Calkyl claim 1 , hydroxyl and halogen.7. The compound of claim 6 , in which C-Calkyl is methyl claim 6 , O—C-Calkyl is O-ethyl claim 6 , and halogen is chlorine.8. The compound of claim 1 , in which W is selected from W claim 1 , W claim 1 , WWor W.9. The compound of claim 8 , in which R-Rare selected from H claim 8 , C-Calkyl claim 8 , O—C-Calkyl and halogen.10. The compound of claim 9 , in which C-Calkyl is methyl claim 9 , O—C-Calkyl is O-ethyl and ...

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11-04-2013 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20130090483A1
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

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18-04-2013 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20130096162A1
Принадлежит:

The invention is directed to compounds having the formula: 2. The compound of claim 1 , wherein r is 1.3. (canceled)5. The compound of claim 4 , wherein Ris selected from —COOH claim 4 , —SONHR claim 4 , and tetrazol-5-yl.711-. (canceled)12. The compound of claim 1 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 1 , where Ris —Calkyl.13. The compound of claim 12 , wherein Ris selected from —Calkyl and —O—Calkyl.14. The compound of claim 1 , wherein X is —Calkylene- claim 1 , 1 to 4-CH-moieties in the alkylene are replaced with a —NR—C(O)— or —C(O)—NR— moiety claim 1 , and Ris selected from H and —OH.15. The compound of wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; and —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—.16. The compound of claim 15 , wherein X is selected from —C(O)NH— and —CH—NHC(O)—.17. The compound of claim 1 , wherein Ris selected from —Calkylene-SR claim 1 , —Calkylene-C(O)NRR claim 1 , —Calkylene-NR—C(O)R claim 1 , —NH—Calkylene-P(O)(OR) claim 1 , —Calkylene-P(O)ORR claim 1 , —Calkylene-CHR—COOH claim 1 , and —Calkylene-C(O)NR—CHR—COOH; Ris H claim 1 , Ris —OH claim 1 ...

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18-04-2013 дата публикации

SALALEN LIGANDS AND ORGANOMETALLIC COMPLEXES

Номер: US20130096271A1
Принадлежит: Ramot at Tel-Aviv University Ltd.

Use of homogeneous catalytic systems which include as a pre-catalyst a complex of a Group IV metal and a salalen ligand in the polymerization of alpha-olefins, is disclosed. The alpha-olefin polymers obtained are characterized by controlled levels of tacticity. Also disclosed are novel salalen ligands and novel complexes thereof with Group IV metals. 161-. (canceled)62. A process of polymerizing an alpha-olefin , the process comprising contacting the alpha-olefin with a catalyst system which comprises:(i) a pre-catalyst comprising a Group IV metal atom and a salalen ligand complexed therewith; and(ii) a co-catalyst,thereby producing a polymer of the alpha-olefin.64. The process of claim 62 , wherein said alpha-olefin is propylene.65. The process of claim 62 , wherein said co-catalyst is an aluminoxane.67. The process of claim 63 , wherein R is alkyl.68. The process of claim 63 , wherein at least one of R-Ris an alkyl.69. The process of claim 68 , wherein said alkyl is a bulky alkyl selected from the group consisting of tert-butyl claim 68 , isobutyl claim 68 , isopropyl claim 68 , trityl claim 68 , cumyl and tert-hexyl.70. The process of claim 63 , wherein at least one of R-Ris halogen.71. The process of claim 70 , wherein each of R-Ris halogen.72. The process of claim 70 , wherein at least one of Rand Ris halogen.73. The process of claim 63 , wherein at least one of R-Ris a bulky rigid group.74. The process of claim 73 , wherein at least one of R-Ris selected from the group consisting of aryl claim 73 , heteroaryl claim 73 , cycloalkyl and heteroalicyclic claim 73 , each having at least 7 carbon atoms.75. The process of claim 63 , wherein Ris adamantyl.76. The process of claim 72 , wherein Ris adamantyl.77. A polymer of an alpha-olefin claim 62 , prepared by the process of .78. The polymer of claim 77 , characterized by at least one of:an isotacticity degree of at least 50%;{'sub': 'w', 'a molecular weight of at least M=200,000 grams/mol; and'}a molecular weight ...

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18-04-2013 дата публикации

MESO-BILIVERDIN COMPOSITIONS AND METHODS

Номер: US20130096318A1
Принадлежит: Utah State University

Methods and materials for producing meso-biliverdin are provided where the methods include reacting phycocyanobilin with an amphoteric compound in a solvent to yield meso-biliverdin. 1. A method of producing meso-biliverdin , the method comprising:reacting phycocyanobilin with an amphoteric compound to yield meso-biliverdin.2. The method of claim 1 , wherein the meso-biliverdin comprises meso-biliverdin IXα.3. The method of claim 1 , wherein the meso-biliverdin consists of meso-biliverdin IXα.4. The method of claim 1 , wherein the amphoteric compound is selected from the group consisting of sodium bicarbonate claim 1 , potassium carbonate claim 1 , and sodium carbonate.5. The method of claim 1 , wherein the amphoteric compound comprises sodium bicarbonate or potassium carbonate.6. The method of claim 1 , wherein the phycocyanobilin is reacted with the amphoteric compound in ethanol or tert-butanol.7. The method of claim 5 , wherein the phycocyanobilin is reacted with the sodium bicarbonate or the potassium carbonate in ethanol.8. The method of claim 1 , wherein the amphoteric compound is present in from 1 to 5 folds in weight compared to the phycocyanobilin by weight.9. The method of claim 1 , wherein the amphoteric compound is present in from 2 to 4 folds in weight compared to the phycocyanobilin by weight.10. The method of claim 1 , the method further comprising culturing cyanobacteria claim 1 , rhodophyte claim 1 , cryptophyte claim 1 , or mixture thereof to yield the phycocyanobilin to be reacted with the amphoteric compound.11. The method of claim 10 , wherein the cyanobacteria claim 10 , rhodophyte claim 10 , cryptophyte claim 10 , or mixture thereof are cultured in a culture media comprising waste water.12. A method of producing meso-biliverdin claim 10 , the method comprising:extracting phycocyanobilin from cyanobacteria, rhodophyte, cryptophyte, or mixture thereof; andisomerizing the extracted phycocyanobilin to form meso-biliverdin.13. The method of claim ...

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18-04-2013 дата публикации

PROCESS FOR PREPARATION OF AMISULPRIDE

Номер: US20130096319A1
Принадлежит: Lupin Limited

The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively. 1) A process for the preparation of amisulpride (I) which involves following steps:{'b': '1', ') methylation of 4-amino-salicylic-acid (VI) to 4-amino-2-methoxy methyl benzoate (VII), optionally in the presence of phase transfer catalyst,'}{'b': '2', ') conversion of 4-amino-2-methoxy methyl benzoate (VII) to 4-amino-2-methoxy-5-thiocyano methyl benzoate (VIII),'}{'b': '3', ') ethylation of 4-amino-2-methoxy-5-thiocyano methyl benzoate (VIII) to form 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X),'}the intermediate compound (X) is converted to amisulpiride (I) by two routes (a) or (b):Route (a):{'b': '4', 'i': 'a', ') hydrolysis of 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) to 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX),'}{'b': '4', 'i': 'b', ') oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) with a suitable oxidizing agent in presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV),'}Route (b):{'b': '5', 'i': 'a', ') oxidation of 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) to 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) with a suitable oxidizing agent,'}{'b': '5', 'i': 'b', ') hydrolysis of 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid,(IV and;'}{'b': '6', ') coupling of 2-methoxy-4-amino-5-ethyl-sulfonyl ...

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25-04-2013 дата публикации

Method of manufacturing display apparatus

Номер: US20130100386A1
Принадлежит: SAMSUNG ELECTRONICS CO LTD

In a method of manufacturing a display apparatus, a first substrate including a plurality of pixels is formed, and a black column spacer is formed on the first substrate. A second substrate is formed, and a liquid crystal layer is formed between the first substrate and the second substrate. The black column spacer is formed by coating a photoresist on the first substrate, exposing the photoresist to a first light, developing the exposed photoresist and exposing the developed photoresist to a second light.

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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

Inhibitors of protein prenyltransferases

Номер: US20130102639A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.

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25-04-2013 дата публикации

SUBSTITUTED BIARYL ALKYL AMIDES

Номер: US20130102649A1
Принадлежит: BioTheryX, Inc.

Disclosed herein are substituted biaryl alkyl amide compounds, methods of synthesizing substituted biaryl alkyl amide compounds and methods of treating diseases and/or conditions with substituted biaryl alkyl amide compounds. 2. The compound of claim 1 , wherein n is selected from the group consisting of 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , and 5.3. The compound of claim 2 , wherein n is 2.4. The compound of claim 1 , wherein each Ris halo.5. The compound of claim 4 , wherein each Ris chloro.6. The compound of claim 1 , wherein Z claim 1 , Z claim 1 , Zand Zare each —CH—.7. The compound of claim 1 , wherein Ris (Calkoxy)Calkyl.8. The compound of claim 7 , wherein Ris methoxymethyl or ethoxymethyl.9. The compound of claim 1 , wherein Ris (aryloxy)Calkyl.10. The compound of claim 9 , wherein Ris phenoxymethyl.11. The compound of claim 1 , wherein Ris Cheterocyclyl.12. The compound of claim 11 , wherein Ris selected from optionally substituted tetrahydrofuranyl or optionally substituted pyrrolidinyl.13. The compound of claim 12 , wherein the nitrogen atom in pyrrolidinyl is protected with a t-butyloxycarbonyl (Boc) protecting group.14. The compound of claim 1 , wherein Ris Ccycloalkyl.15. The compound of claim 14 , wherein Ris cyclopentyl.16. The compound of claim 1 , wherein Ris haloalkyl.17. The compound of claim 16 , wherein Ris selected from the group consisting of —CHCl claim 16 , —CHBr claim 16 , —CHCHCl claim 16 , —CHCHBr claim 16 , —CH(Cl)CHand —CH(Br)CH.18. The compound of claim 1 , wherein Ris optionally substituted aminoalkyl.19. The compound of claim 18 , wherein Ris selected from the group consisting of —CHNH claim 18 , —CHNH(Boc) claim 18 , —CH(NH)CH claim 18 , and —CH(Boc-NH)CH.20. The compound of claim 1 , wherein Ris —OH.22. The compound of claim 21 , wherein Ris —OH.23. The compound of claim 1 , wherein Ris selected from the group consisting of —OH claim 1 , —NHR claim 1 , an optionally substituted Calkoxy claim 1 , and an optionally ...

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25-04-2013 дата публикации

THIONATION PROCESS AND A THIONATING AGENT

Номер: US20130102774A1
Принадлежит: Vironova AB

A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product, by use of crystalline PS.2 CHN as a thionating agent. A thionating agent which is crystalline PS.2 CHN. 1. A process for transforming a group >C═O (I) in a compound into a group >C═S (II) or into a tautomeric form of group (II) in a reaction giving a thionated reaction product , by use of crystalline PS.2 CHN as a thionating agent.2. A process according to claim 1 , wherein the thionating agent and the compound are allowed to react with each other in a liquid solvent medium for the compound and for the thionating agent.3. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , a C1-C3 alkylnitrile claim 1 , a cyclic sulfone and/or a C1-C3 dialkylsulfone.4. The process according to claim 1 , wherein the liquid solvent medium comprises pyridine claim 1 , sulfolane claim 1 , dimethyl sulfone and/or acetonitrile.5. The process according to claim 1 , wherein the reaction is performed at a temperature of 60° C. to 180° C.6. The process according to claim 5 , wherein the reaction is performed at temperature of 115° C. to 175° C.7. The process according to claim 1 , wherein the compound comprises a group (I) that is present in an amide function.8. The process according to claim 1 , wherein the compound comprises a group (I) that is present in a ketone function.9. The process according to claim 1 , wherein the thionating agent is used at a molar ratio to the group (I) to be transformed of 1 mole PS.2 CHN per 1-4 moles of group (I).10. The process according to claim 1 , comprising separating the thionated reaction product from the reaction.11. The process according to claim 10 , wherein water is added to the reaction and the thionated reaction product is separated as a solid material claim 10 , by precipitation or crystallization.12. A thionating agent which is ...

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25-04-2013 дата публикации

Substituted Tetracycline Compounds

Номер: US20130102779A1
Автор: Abato Paul
Принадлежит: PARATEK PHARMACEUTICALS, INC.

The present invention pertains to tetracycline compounds of formula (VIIa): 2. The tetracycline compound of claim 1 , wherein Ris oxazolyl.3. The tetracycline compound of claim 2 , wherein oxazolyl is substituted with methyl or isopropyl.4. The tetracycline compound of claim 1 , wherein Ris oxadiazolyl.5. The tetracycline compound of claim 4 , wherein oxadiazolyl is substituted with alkyl.6. The tetracycline compound of claim 1 , wherein Ris isoxazolyl.7. The tetracycline compound of claim 1 , wherein Ris pyrazolyl.8. The tetracycline compound of claim 7 , wherein Ris methylpyrazolyl.9. The tetracycline compound of claim 1 , wherein Ris —CONRR claim 1 , in which Ris hydrogen and Ris hydroxyl claim 1 , hydroyxalkyl claim 1 , alkoxy claim 1 , phenyl claim 1 , or alkyl.10. The tetracycline compound of claim 1 , wherein Ris wherein Ris —CONRR claim 1 , in which Ris alkyl and Ris alkyl or hydroxyl.11. The tetracycline compound of claim 1 , wherein Ris dialkylamino.12. The tetracycline compound of claim 11 , wherein Ris dimethylamino.13. The tetracycline compound of claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , and R is hydrogen.14. The tetracycline compound of claim 13 , wherein Ris dialkylamino.15. The tetracycline compound of claim 14 , wherein Ris dimethylamino.19. A pharmaceutical composition comprising a tetracycline compound of and a pharmaceutically acceptable carrier.20. A method for treating a tetracycline responsive state in a subject claim 1 , comprising administering to said subject an effective amount of a tetracycline compound of claim 1 , such that said subject is treated. This application is a divisional application of U.S. Ser. No. 11/963,540, filed on Dec. 21, 2007 and issued as U.S. Pat. No. 8,318,706 on Nov. 27, 2012, which claims priority to U.S. Provisional Patent Application No. 60/876,313, filed on Dec. 21, 2006 and U.S. Provisional Patent Application No. 60/943,003, filed Jun. 8, 2007. The contents of the foregoing applications ...

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25-04-2013 дата публикации

SYNTHETIC PROCESS FOR AMINOCYCLOHEXYL ETHER COMPOUNDS

Номер: US20130102791A1
Принадлежит: CARDIOME PHARMA CORP.

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed. 15.-. (canceled)7. The method of further comprising optionally protecting the compound of formula (4) and/or the compound of formula (6) before the reaction of compound of formula (4) with the compound of formula (6) and optionally deprotecting the compound of formula (8) after the reaction.9. The method of wherein the suitable conditions comprise activating Q in the presence of a catalytic amount of an acid in an aprotic solvent.12. The method of further comprising optionally protecting the compound of formula (71) and/or the compound of formula (6) before the reaction of compound of formula (71) with the compound of formula (6) and optionally deprotecting the compound of formula (73) after the reaction.14. The method of wherein the suitable conditions comprise activating Q in the presence of a catalytic amount of an acid in an aprotic solvent.17. The method of further comprising optionally protecting the compound of formula (72) and/or the compound of formula (6) before the reaction of compound of formula (72) with the compound of formula (6) and optionally deprotecting the compound of formula (74) after the reaction.19. The method of wherein the suitable conditions comprise activating Q in the presence of a catalytic amount of an acid in an aprotic solvent.2120. The method of any one of claim 16 , claim 16 , and claim 16 , wherein the separation step comprises crystallization claim 16 , kinetic resolution claim 16 , chemical separation claim 16 , enzymatic resolution claim 16 , and/or chromatographic resolution.22. The method of wherein said optional functionalization step comprises formation of acid addition salts of the mixture of the compound of formula (4a) and the compound of formula (5a) or the ...

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02-05-2013 дата публикации

Bile Acid Recycling Inhibitors for Treatment of Hypercholemia and Cholestatic Liver Disease

Номер: US20130108573A1
Принадлежит: Lumena Pharmaceuticals, Inc.

Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof. 1. A method for treating or ameliorating hypercholemia comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the method comprises decreasing at least 20% of serum bile acid or hepatic bile acid levels in the patient.3. The method of claim 1 , wherein less than 10% of the ASBTI is systemically absorbed.5. The method of claim 4 , wherein:q is 1;n is 2;{'sup': 'x', 'sub': 3', '2, 'Ris N(CH);'}{'sup': 7', '8, 'Rand Rare independently H;'}{'sup': 1', '2, 'Rand Ris alkyl;'}{'sup': 3', '4, 'Ris H, and Ris OH;'}{'sup': 5', '6', '9', '9', '9', '9', '9, 'sub': 2', '3', 'Z', 'Z, 'claim-text': wherein z is 1, 2 or 3; each L is independently a substituted or unsubstituted alkyl, a substituted or unsubstituted heteroalkyl, a substituted or unsubstituted alkoxy, a substituted or unsubstituted aminoalkyl group, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted cycloalkyl, or a substituted or unsubstituted heterocycloalkyl; each K is a moiety that prevents systemic absorption;', {'sup': 15', '13', '13', '14', '13', '14', '13', '13', '13', '13', '13', '14', '13', ...

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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

GRP94 INHIBITORS

Номер: US20130109684A1
Принадлежит: University of Kansas

The present disclosure provides a series of compounds which exhibit isoform selective inhibition of GRP94, a homologue of Hsp90 that is localized to the endoplasmic recticulum. Through GRP94 inhibition, these compounds are likely to manifest anti-cancer, anti-inflammatory, anti-metastasis, and immunosuppressive activities, as well as utility in the treatment of neurodegenerative diseases, and diabetes. 4. The compound or pharmaceutically acceptable salt according to whereinV is N;X is CH;Y is CH; andZ is N.5. The compound or pharmaceutically acceptable salt according to wherein Ris F claim 1 , Cl claim 1 , Br claim 1 , or I.6. The compound or pharmaceutically acceptable salt according to wherein Ris Cl;{'sup': '2', 'Ris OH; and'}{'sup': '3', 'Ris OH.'}13. A pharmaceutical composition comprising a compound or salt according to and a pharmaceutically acceptable carrier.14. A method of treating or preventing a GRP94 related disorder in a patient in need thereof comprising administering a therapeutically effective amount of a pharmaceutical composition comprising a compound or salt according to claim 1 , and a pharmaceutically acceptable carrier or excipient to the patient.15. The method according to claim 14 , wherein the GRP94 related disorder is selected from the group consisting of cancer claim 14 , metastasis claim 14 , an inflammatory disorder claim 14 , a neurodegenerative disorder claim 14 , and diabetes. This application claims the benefit of priority to U.S. Provisional Application Ser. No. 61/473,343, filed Apr. 8, 2011, which is hereby incorporated herein by reference.This invention was made with Government support under National Institutes of Health (NIH) Grant Nos. AG18001, GM077480, DK053058 and CA109265, awarded by the National Cancer Institute. The Government has certain rights in this invention.1. Field of the InventionThe present disclosure provides a series of compounds which exhibit isoform selective inhibition of Glucose-related protein 94 (Grp94), ...

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02-05-2013 дата публикации

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

Номер: US20130109698A1
Автор: Simon Cocklin
Принадлежит: Simon Cocklin

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

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02-05-2013 дата публикации

FAAH Inhibitors

Номер: US20130109721A1
Принадлежит: Ironwood Pharmaceuticals, Inc.

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

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02-05-2013 дата публикации

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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02-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF PYRROLINES FROM GAMMA-NITROKETONES. USE OF THE GAMMA-NITROKETONES AS PESTICIDAL AGENTS

Номер: US20130109757A1
Принадлежит: Bayer Intellectual Property GmbH

The invention is directed to method for the preparation of pyrrolines of the general formula (I) 2. The method according to claim 1 , wherein said elevated pressure is in a range from 2 to 100 bar.3. The method according to claim 1 , wherein the transitionmetal catalyst used comprises at least one metal selected from the group consisting of platinum, palladium, cobalt and nickel.4. The method according to claim 3 , wherein Raney-Nickel is used as transition metal catalyst in the presence of an organic sulfur-containing compound.5. The method according to claim 4 , wherein said organic sulfur-containing compound is selected from the group consisting of thiophene claim 4 , tetrahydrothiophene and 2 claim 4 ,2′-thiobisethanol.9. The nitroketone compound of formula (II) according to claim 6 , capable of being used for combating harmful invertebrate pests which occur in the agriculture or which occur in a veterinary field.10. A method for combating one or more harmful invertebrate pests which occur in the agriculture or which occur in a veterinary field comprising using a compound of to combat said pests. The present invention relates to a method (process) for the synthesis of substituted pyrrolines as well as to specific γ-nitroketones which can be used as starting materials in the process according to the invention. Pyrrolines are biological active and can thus be used as pesticides (cf. WO 2009/097992, WO 2009/112275).Several methods for the manufacturing of pyrrolines are known (cf. Cheruku, Srinivasa et al. 44 (2003), 3701-3703 and Moffett and White, J. Org. Chem. 17 (1952) 407-413)). One method is the reductive cyclization of γ-nitroketones using zinc powder together with HCOH-EtOH (1:1) which results in pyrroline N-oxides and pyrrolines (cf. Cheruku, Srinivasa et al. 44 (2003), 3701-3703).The reductive cyclization of a bromine-substituted pyrrole-γ-nitroketone is described by Laha, K. Joydev et al. in 2006, 71, pp. 4092-4102 (therein named as compound 8) using ...

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02-05-2013 дата публикации

HETERO-SUBSTITUTED ACETANILIDE DERIVATIVES AS ANALGESIC AGENTS

Номер: US20130109863A1
Принадлежит: Janssen Pharmaceutica N.V.

Hetero-substituted acetanilide derivatives are disclosed as analgesic agents. The compounds of the invention are useful in methods for treating a disease or condition in a mammal characterized by pain and/or fever. 123-. (canceled)251. A compound of claim wherein Rand Rtaken together form an optionally substituted imidazole and enantiomers , diastereomers , tautomers , or pharmaceutically acceptable salts thereof.26. A compound selected from the group consisting of:pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide;5-Methyl-1H-pyrazole-3-carboxylic acid (4-hydroxy-phenyl)-amide; and3H-Imidazole-4-carboxylic acid (4-hydroxy-phenyl)-amide;and enantiomers, diastereomers, tautomers, or pharmaceutically acceptable salts thereof.27. A compound of claim 26 , wherein the compound is pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide and enantiomers claim 26 , diastereomers claim 26 , tautomers claim 26 , or pharmaceutically acceptable salts thereof.28. A compound of claim 26 , wherein the compound is 5-Methyl-1H-pyrazole-3-carboxylic acid (4-hydroxy-phenyl)-amide and enantiomers claim 26 , diastereomers claim 26 , tautomers claim 26 , or pharmaceutically acceptable salts thereof.30. A composition of claim 29 , wherein Rand Rtaken together form an optionally substituted imidazole and enantiomers claim 29 , diastereomers claim 29 , tautomers claim 29 , or pharmaceutically acceptable salts thereof.31. A composition comprising a compound selected from the group consisting of:pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide;5-Methyl-1H-pyrazole-3-carboxylic acid (4-hydroxy-phenyl)-amide; and3H-Imidazole-4-carboxylic acid (4-hydroxy-phenyl)-amide;and enantiomers, diastereomers, tautomers, or pharmaceutically acceptable salts thereof.32. The composition of wherein the compound is pyridine-2-carboxylic acid (4-hydroxy-phenyl)-amide and enantiomers claim 31 , diastereomers claim 31 , tautomers claim 31 , or pharmaceutically acceptable salts thereof.33. The composition of ...

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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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09-05-2013 дата публикации

3-aminopyrrolidine derivatives as modulators of chemokine receptors

Номер: US20130116230A1
Принадлежит: Incyte Corp

The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.

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16-05-2013 дата публикации

DYE FOR PHOTOELECTRIC CONVERSION, SEMICONDUCTOR ELECTRODE, PHOTOELECTRIC CONVERSION ELEMENT, SOLAR CELL, AND NOVEL PYRROLINE-BASED COMPOUND

Номер: US20130118570A1
Принадлежит: NEC Corporation

Provided is a dye for photoelectric conversion containing at least one or more kind of a compound represented by the following General Formula (1) (in Formula (1), Rand Rrepresent any one of —CN, —SOR, —COOR, and —CONR(R represents a hydrogen atom, a substituted or unsubstituted alkyl group, a cycloalkyl group, or an aryl group); Rrepresents a direct bond or a substituted or unsubstituted alkylene group; X represents an acidic group; and D represents an organic group having an electron donating substituent or a substituted or unsubstituted heterocyclic group). 2. The dye for photoelectric conversion according to claim 1 ,wherein the acidic group is a carboxy group, a hydroxy group, a sulfonic acid group, or a phosphonic acid group.3. The dye for photoelectric conversion according to claim 1 ,wherein the organic group having an electron donating substituent is an aryl group having an electron donating substituent.4. A semiconductor electrode comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a semiconductor layer onto which at least one or more kind of the dye for photoelectric conversion according to has been adsorbed.'}5. The semiconductor electrode according to claim 4 ,wherein the semiconductor layer is constituted with a semiconductor material containing titanium oxide or zinc oxide.6. A photoelectric conversion element using the semiconductor electrode according to .7. A solar cell comprising:{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'the photoelectric conversion element according to .'} The present invention relates to a dye for photoelectric conversion, a semiconductor electrode, a photoelectric conversion element, a solar cell, and a novel pyrroline-based compound.Since a large amount of fossil fuels represented by petroleum have been used so far, the level of COhas increased. Consequently, global warming has become a serious problem, and there is a concern over the depletion of fossil fuels. Accordingly, how the demand for a large amount ...

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16-05-2013 дата публикации

CHEMICAL AND BIOLOGICAL AGENTS FOR THE CONTROL OF MOLLUSCS

Номер: US20130121978A1
Принадлежит: MARRONE BIO INNOVATIONS, INC.

Compositions and methods for controlling molluscs, members of the Gastropoda and Bivalvia classes which includes but is not limited to lactones, lactams, carbamates, amides, and/or carboxylic acid containing compounds as active ingredients and/or compounds derived from and/or . Also provided are methods and compositions for increasing the efficacy of chemical and biological control for invasive molluscs in open waters, power plants, and drinking water treatment facilities under coldwater conditions. 1. A combination comprising at least one or more substances effective for controlling a member of a Gastropoda and Bivalvia class and an inert material.2PseudomonasPseudomonas. The combination according to claim 1 , wherein said substances are derived from a species or cell suspension or toxin derived from a species.3Pseudomonas fluorescensPseudomonas fluorescens.. The combination according to claim 1 , wherein said substances are derived from a or cell suspension derived from4PseudomonasPseudomonas. The combination according to claim 1 , wherein said substances are derived from a strain claim 1 , having the identifying characteristics of ATCC 55799.5Pseudomonas. The combination according to claim 1 , wherein the composition comprises a substance that is a cell suspension comprising cells having the toxin producing characteristics of ATCC 55799.6. The combination of claim 1 , wherein said combination is a composition.7ErwiniaPseudomonas. A method for controlling one or more molluscs in a location where control is desired comprising introducing into said location at least one of (a) a cell suspension or extract derived from sp. Cells; (b) one or more compounds claim 1 , wherein said compounds are lactone claim 1 , lactam claim 1 , carbamate claim 1 , carboxylic acid and/or amide compounds or composition comprising said compounds claim 1 , with the proviso that said compounds are not gamma-octalactone claim 1 , gamma-nonalactone claim 1 , gamma-decanolactone claim 1 , ...

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16-05-2013 дата публикации

DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE

Номер: US20130123243A1
Принадлежит:

This invention is directed to compounds of formula (I): 3. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, cyano, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each independently hydrogen or halo.'}4. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, optionally substituted phenyl, furanyl, thienyl, thiazolyl, or optionally substituted oxazolyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each hydrogen.'}6. A compound according to wherein R an optionally substituted heteroaryl.7. A compound according to wherein R is furanyl claim 6 , oxazoyl claim 6 , pyrazolyl claim 6 , pyridinyl claim 6 , triazolyl claim 6 , thiazolyl claim 6 , or benzothiazolyl claim 6 , each of which is optionally substituted.8. A compound according to wherein:{'sup': 2', '7', '5a', '5b', '5c, 'Rand R, together with the nitrogens to which they are attached and one of R, Rand R, form an optionally substituted 6- to 10-membered bridged N-heterocyclyl.'}10. A compound according to wherein:{'sup': 3', '12', '12', '12, 'Ris a direct bond, —O—, —R—O—, —O—R—, —O—R—O—, or an optionally substituted straight or branched alkylene chain;'}{'sup': 4', '12a, 'Ris a direct bond, —O—R— or an optionally substituted straight or branched alkylene chain;'}{'sup': 8', '13', '10', '13', '10', '13', '10', '11, 'Ris aralkyl optionally substituted with one or more substituents selected from the group consisting of —R—OR, —R—C(═O)ORand —R—C(═O)N(R)R;'}{'sup': 9', '10, 'each Ris independently alkyl, halo or —O—R;'}{'sup': '12', 'Ris an optionally substituted straight ...

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16-05-2013 дата публикации

Non-Fluorescent Quencher Compounds and Biomolecular Assays

Номер: US20130123475A1
Принадлежит: LIFE TECHNOLOGIES CORPORATION

Bis-diazo, triaryl and aryldiazo-N-arylphenazonium quencher moieties, substituted with electron-withdrawing and electron-donating substituents which induce polarity in the delocalized aryl/diazo ring systems, are useful as labels when attached to biomolecules such as polynucleotides, nucleosides, nucleotides and polypeptides. The quencher moieties are non-fluorescent and accept energy transfer from fluorescent reporter labels by any energy-transfer mechanism, such as FRET. 354-. (canceled)56. The compound of claim 55 , wherein the electron-withdrawing groups are each claim 55 , independently of one another claim 55 , selected from NO claim 55 , CN claim 55 , CF claim 55 , COH claim 55 , COR′ claim 55 , C(O)NH claim 55 , N(O)NHR′ claim 55 , C(O)NR′R′ claim 55 , CHO claim 55 , C(O)R′ claim 55 , SOR′ claim 55 , SOCF claim 55 , SOOR′ claim 55 , SOH claim 55 , NO and C-Caryl claim 55 , wherein each R′ is independently H claim 55 , C-Calkyl or C-Caryl.57. The compound of claim 55 , wherein the electron-donating groups are each claim 55 , independently of one another claim 55 , selected from O claim 55 , S claim 55 , NR″R″ claim 55 , NHR″ claim 55 , NH claim 55 , NHC(O)R″ claim 55 , OR″ claim 55 , OH claim 55 , OC(O)R″ claim 55 , SR″ claim 55 , SH claim 55 , Br claim 55 , I claim 55 , Cl claim 55 , F claim 55 , R″ and C-Caryl claim 55 , wherein each R″ is independently H claim 55 , C-Calkyl or C-Caryl.58. The compound of claim 55 , wherein Ris NO.59. The compound of claim 55 , wherein at least one of R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , R claim 55 , Rand Ris OCH.60. The compound of claim 55 , wherein the reactive linking group comprises an electrophile.61. The compound of claim 60 , wherein the electrophile of the reactive linking group is a carboxylic acid or an ester.62. The compound of claim 55 , wherein the reactive linking group is linked to the quencher moiety Q1 ...

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16-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES

Номер: US20130123512A1
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates in part to a process for the preparation of a proline derivative of formula I 3. The process of claim 1 , wherein{'sup': '3', 'sub': 1-7', '1-7, 'Ris halogen-C-alkoxy or a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C-alkyl or halogen.'}6. The process of claim 1 , wherein the transformation in step a) is performed with a sulfonating agent in the presence of an organic solvent at a temperature between −10° C. and 40° C.7. The process of claim 1 , wherein the reaction in step b) is performed in the presence of a base in an organic solvent at a temperature between 10° C. and 90° C.8. The process of claim 1 , wherein the oxidation in step c) is performed with an oxidating agent in the presence of an organic solvent at a temperature between 0° C. and 60° C.9. The process of claim 8 , wherein the oxidating agent is potassium peroxymonosulfate or magnesium monoperoxyphthalate hexahydrate.12. The process of claim 11 , wherein the reaction in step a1) is performed in an organic solvent at temperatures between −10° C. and 25° C.13. The process of claim 11 , wherein the reaction in step b1) is performed with a sulfonating agent claim 11 , in an organic solvent at temperatures between −10° C. and 40° C.14. The process of claim 11 , wherein the reaction in step c1) is performed in the presence of a carboxylate salt NaRCOO claim 11 , wherein Ris C-alkyl or aryl claim 11 , in a solvent at temperatures between 40° C. and 130° C.15. The process of claim 14 , wherein sodium 2-ethylhexenoate is used.18. The process of claim 17 , wherein the reaction in step a2) is performed in an organic solvent at temperatures between −10° C. and 25° C.19. The process of wherein the reaction in step b2) is performed in the presence of an alkali alkyl- or arylcarboxylate salt MRCOO claim 17 , wherein M is selected from the group consisting of Li claim 17 , Na claim 17 , K and Cs and Ris C-alkyl or aryl ...

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23-05-2013 дата публикации

CATIONIC LIPID

Номер: US20130129811A1
Принадлежит:

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 2. The cationic lipid according to claim 1 , wherein Xand Xare combined together to form a single bond or alkylene.3. The cationic lipid according to claim 1 , wherein Lis a single bond claim 1 , Ris a hydrogen atom claim 1 , methyl claim 1 , pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare —O—.4. The cationic lipid according to claim 1 , wherein Lis —CO— or —CO—O— claim 1 , Ris pyrrolidin-3-yl claim 1 , piperidin-3-yl claim 1 , piperidin-4-yl claim 1 , or alkyl having 1 to 6 carbon atoms or alkenyl having 3 to 6 carbon atoms substituted with 1 to 3 substituent(s) claim 1 , which is(are) claim 1 , the same or different claim 1 , amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , hydroxy claim 1 , alkoxy claim 1 , carbamoyl claim 1 , monoalkylcarbamoyl claim 1 , dialkylcarbamoyl claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , wherein at least one of the substituents is amino claim 1 , monoalkylamino claim 1 , dialkylamino claim 1 , trialkylammonio claim 1 , pyrrolidinyl claim 1 , piperidyl or morpholinyl claim 1 , and Land Lare identically —CO—O— or —O—CO—.5. The cationic lipid according to any one of to claim 1 , wherein Xis absent claim 1 , or is methyl.64. The cationic lipid according to any one of to claims 1 , wherein Land Lare —O— or —O—CO— claims 1 , and Rand Rare (Z)-hexadec-6-enyl or (Z)-hexadec ...

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23-05-2013 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20130131137A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

The invention relates to compounds of formula (I) where A, A, A, A, G, R, R, Rand Rare as defined in claim 1; or a salt or JV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests. 2. A compound according to where Ais C—R claim 1 , Ais C—H claim 1 , Ais C—H or nitrogen and Ais C—H or nitrogen;3. A compound according to or where G is oxygen.4. A compound according to any one of to where Ris hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , methylcarbonyl- claim 1 , or methoxycarbonyl-.6. A compound according to any one of to where Ris chlorodifluoromethyl or trifluoromethyl.7. A compound according to any one of to where Ris phenyl or phenyl substituted by one to five R.11. A method of controlling insects claim 1 , acarines claim 1 , nematodes or molluscs which comprises applying to a pest claim 1 , to a locus of a pest claim 1 , or to a plant susceptible to attack by a pest an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in any one of to .12. An insecticidal claim 1 , acaricidal claim 1 , nematicidal or molluscicidal composition comprising an insecticidally claim 1 , acaricidally claim 1 , nematicidally or molluscicidally effective amount of a compound of formula (I) as defined in any one of to .13. An insecticidal claim 12 , acaricidal claim 12 , nematicidal or molluscicidal composition according to comprising an additional compound having biological activity.14. A method of treatment of insect pests in or on animals claim 12 , comprising administering an effective amount of a compound as defined in any one of to claim 12 , or a composition comprising said compound claim 12 , to an ...

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