Настройки

Укажите год
-

Небесная энциклопедия

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 25771. Отображено 100.
10-11-2014 дата публикации

СЕНСОР ДЛЯ АНАЛИЗА ГЛИЦИНА В ВОДНЫХ РАСТВОРАХ

Номер: RU0000147538U1

Сенсор для определения глицина в водной среде, включающий серебряную поверхность кварцевого резонатора, отличающийся тем, что поверхность модифицирована сульфидом серебра. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 147 538 U1 (51) МПК G01N 31/00 (2006.01) G01N 27/00 (2006.01) C07C 229/08 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ 2014126453/15, 30.06.2014 (24) Дата начала отсчета срока действия патента: 30.06.2014 (45) Опубликовано: 10.11.2014 Бюл. № 31 (54) СЕНСОР ДЛЯ АНАЛИЗА ГЛИЦИНА В ВОДНЫХ РАСТВОРАХ Формула полезной модели Сенсор для определения глицина в водной среде, включающий серебряную поверхность кварцевого резонатора, отличающийся тем, что поверхность модифицирована сульфидом серебра. 1 4 7 5 3 8 Адрес для переписки: 170100, г. Тверь, ул. Желябова, 33, Тверской государственный университет, Управление интеллектуальной собственности (73) Патентообладатель(и): Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Тверской государственный университет" (RU) R U Приоритет(ы): (22) Дата подачи заявки: 30.06.2014 (72) Автор(ы): Рясенский Сергей Станиславович (RU), Феофанова Мариана Александровна (RU), Скобин Михаил Игоревич (RU), Мельников Никита Валерьевич (RU) R U 1 4 7 5 3 8 U 1 U 1 Стр.: 1 RU 5 10 15 20 25 30 35 40 45 147 538 U1 Сенсор для анализа глицина в водных растворах относится к области аналитической химии и может быть использован в химической, микробиологической, фармацевтической промышленности. В качестве ближайшего аналога (прототипа) выбран акустический сенсор для определения глицина и глицил - глицина в водных и спиртовых растворах (В.Ф. Селеменев, А.Н. Зяблов, А.В. Калач. Определение глицина и глицил-глицина в водных и спиртовых растворах с использованием акустического сенсора // Журн. Заводская лаборатория. Диагностика материалов. 2007. №7, т. 73. С. 17-20), состоящий из стеклянного корпуса с подвижным стеклянным колпачком, ...

Подробнее
12-01-2012 дата публикации

Drug Delivery System for Use in the Treatment of Vascular and Vessel-Related Pathologies

Номер: US20120010557A1
Автор: Michal Heger
Принадлежит: ACADEMISCH MEDISCH CENTRUM

The present invention relates to a drug delivery system for use in the treatment of vascular and vessel-related pathologies, comprising a drug delivery platform that comprises at least one compound capable of exerting an effect on the formation and/or maintenance of a thrombus in the vessel to be treated. The platform is preferably formed by liposomes that are sterically stabilized by grafting of poly(ethylene glycol) onto the liposome surface. The liposomes may further comprise photosensitizers and targeting molecules. The liposomes may be thermosensitive. The compound is suitably tranexamic acid. The drug delivery system is preferably used for the treatment of port wine stains.

Подробнее
26-01-2012 дата публикации

Process for the production of carnitine from beta-lactones

Номер: US20120022288A1
Принадлежит: Lonza AG

The invention relates to a method for the production of L-carnitine, wherein a β-lactone, which is a 4-(halomethyl)oxetane-2-one, is converted into carnitine with trimethylamine (TMA), wherein the β-lactone is not subjected to a basic hydrolysis step before being contacted with the trimethylamine. The invention also relates to a carnitine having a unique impurity profile.

Подробнее
16-02-2012 дата публикации

Genetic polymorphisms associated with venous thrombosis, methods of detection and uses thereof

Номер: US20120039864A1

The present invention is based on the discovery of genetic polymorphisms that are associated with coronary heart disease and in particular VT and response to drug treatment. In particular, the present invention relates to nucleic acid molecules containing the polymorphisms, variant proteins encoded by such nucleic acid molecules, reagents for detecting the polymorphic nucleic acid molecules and proteins, and methods of using the nucleic acid and proteins as well as methods of using reagents for their detection.

Подробнее
16-02-2012 дата публикации

Process For The Iodination Of Aromatic Compounds

Номер: US20120041224A1
Принадлежит: BRACCO IMAGING SPA

The present invention relates to a process for the preparation of iodinated anilines; in particular, it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted anilines to the corresponding 3,5-disubstituted-2,4,6-triiodoanilines, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves.

Подробнее
23-02-2012 дата публикации

Methods of reducing the risk of cardiovascular disease in postmenopausal women

Номер: US20120046249A1

The present invention features materials and methods for reducing the risk of cardiovascular disease in postmenopausal or perimenopausal women. More specifically, these methods can be used in women who generally have no apparent cardiovascular disease. We describe herein methods of administering non-antibacterial tetracycline or a sub-antimicrobial amount of antibacterial tetracyclines or tetracycline formulations and their use in reducing the risk that cardiovascular disease will develop in a subject (e.g., in a post- or perimenopausal woman)

Подробнее
23-02-2012 дата публикации

Intermediates in the enantioselective synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid

Номер: US20120046468A1

(S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid or (S)-pregabalin is an anticonvulsive drug. In addition to its use as an anticonvulsive agent, pregabalin has also been indicated as a medicament in the treatment of anxiety, neuropathic pain and pain in patients with fibromyalgia. Provided herein are thioester intermediates in the synthesis of and processes for the synthesis of 3-(aminomethyl)-5-methyl-hexanoic acid in the (R) or (S) configuration.

Подробнее
23-02-2012 дата публикации

Method of preparing an alkylamine derivative

Номер: US20120046494A1
Принадлежит: Kolon Life Science Inc

The present invention provides a method of preparing an alkylamine derivates which hardly generates impurities and enables mass production with high purity.

Подробнее
08-03-2012 дата публикации

nanoparticulate compositions of poorly soluble compounds

Номер: US20120058151A1
Принадлежит: CAPSULUTION PHARMA AG

The present invention relates to a method for the production of a nanoparticulate pharmaceutical composition. The method comprises the steps of a) suspending in water a poorly soluble active ingredient without the presence of a detergent, b) mechanically treating said suspension to obtain particles comprising the active ingredient with an effective average size of less than about 5000 nm, c) contacting said active ingredient or suspension with a first polyelectrolyte during and/or before mechanically treating, d) optionally contacting said suspension with a one or more second or further polyelectrolytes during, before and/or after mechanically treating, e) optionally drying said suspension. The invention also pertains to the pharmaceutical compositions obtained by the method of the invention.

Подробнее
22-03-2012 дата публикации

Treatment of vascularized pigment epithelial detachment with anti-vegf therapy

Номер: US20120070428A1
Принадлежит: Genentech Inc

Methods for treating vascularized pigment epithelial detachment using anti-VEGF agents are disclosed.

Подробнее
29-03-2012 дата публикации

Process for producing granules comprising one or more complexing agent salts

Номер: US20120077727A1
Принадлежит: BASF SE

A process for producing granules containing one or more complexing agent salts of the general formula from an aqueous starting solution, containing the one or more complexing agent salts in a concentration of from 10 to 80% by weight, based on the total weight of the aqueous starting solution, in a jet apparatus.

Подробнее
29-03-2012 дата публикации

Antagonists of pcsk9

Номер: US20120077964A1
Принадлежит: Merck Sharp and Dohme LLC

Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.

Подробнее
12-04-2012 дата публикации

Method for the Generation of Nuclear Hyper-Antipolarization in Solids Without the Use of High Magnetic Fields or Magnetic Resonant Excitation

Номер: US20120087867A1
Принадлежит: Individual

A method of inducing nuclear spin hyper-antipolarization in a solid material is disclosed and described. The solid material can be subjected to an ultralow temperature and a magnetic field. The solid material can include donor nuclei and a carrier material while the material also has both a nuclear spin and an electron spin which are coupled sufficiently to allow an Overhauser effect. The solid material can be subjected at the ultralow temperature to a light source for a time sufficient to induce a substantial nuclear spin antipolarization in the solid material and form a nuclear spin hyper-antipolarized material. The ultralow temperature and light source are controlled so as to be sufficient to drive a non-equilibrium nuclear Overhauser effect of hyperfine coupled electron and nuclear spins. The resulting nuclear spin hyper-antipolarized material can be used for a variety of applications such as medical imaging and quantum computing. These materials can be readily formed relatively quickly and are generally stable at room temperatures.

Подробнее
12-04-2012 дата публикации

Process for the preparation of a iodinating agen

Номер: US20120088926A1
Принадлежит: BRACCO IMAGING SPA

The present invention describes a process for the synthesis of a iodinating agent, being said iodinating agent iodine chloride (ICI.) In particular, the present invention relates to a process for the electrochemical preparation of ICI, as a useful iodinating agent in the preparation of iodinated organic compounds for use as contrast agents or their precursors in the synthesis of the same.

Подробнее
10-05-2012 дата публикации

Optical imaging agents

Номер: US20120114563A1
Принадлежит: General Electric Co

The present invention relates to a method of in vivo optical imaging, of the margins around tumours, which comprises an optical imaging contrast agent. The optical imaging agents comprise conjugates of near-infrared dyes with synthetic polyethylene glycol (PEG) polymers having a molecular weight in the range 15-45 kDa. Also disclosed are optical imaging contrast agents, pharmaceutical compositions and kits.

Подробнее
07-06-2012 дата публикации

Process for preparing pregabalin

Номер: US20120142949A1
Автор: B. S. Pradhan
Принадлежит: HELVETICA IND (P) Ltd

The invention relates to a process for preparing a compound of formula (I): wherein said process comprises hydrogenation of a compound of formula (II); under alkaline conditions, wherein R represents hydrogen or a labile group capable of being converted to hydrogen. The invention also relates to intermediates used in said process, to the use of said intermediates in the preparation of pregabalin and to a process for resolving racemic compounds of formula (I).

Подробнее
07-06-2012 дата публикации

Process to prepare a chelating agent or precursor thereof using a cyanide salt

Номер: US20120142964A1
Принадлежит: Akzo Nobel Chemicals International BV

The present invention relates to a process comprising the reaction of a cyanide with an amino acid and an aldehyde, characterized in that the cyanide is a cyanide salt, the amino acid is aspartic acid and/or glutamic acid in the acidic form, and the process is performed under acidic pH by the addition of between 0 and 1 equivalent of an acid based on the amount of aspartic or glutamic acid.

Подробнее
14-06-2012 дата публикации

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

Номер: US20120149917A1
Принадлежит: Sumitomo Seika Chemicals Co Ltd

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

Подробнее
21-06-2012 дата публикации

Enzyme Treatment of Foodstuffs for Celiac Sprue

Номер: US20120156253A1

Administering an effective dose of glutenase to a Celiac or dermatitis herpetiformis patient reduces levels of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.

Подробнее
28-06-2012 дата публикации

Supplement comprising blackcurrants or boysenberries

Номер: US20120164252A1
Принадлежит: Gibb Holdings Nelson Ltd

The present invention relates to a dietary supplement comprising one or more of processed whole blackcurrants, processed whole boysenberries, one or more natural component extracted from blackcurrants, and one or more natural component extracted from boysenberries. The dietary supplement is particularly, but not exclusively, suitable for animals.

Подробнее
19-07-2012 дата публикации

Heart-slowing drug containing short-acting beta-blocker as teh active ingredient

Номер: US20120184545A1
Принадлежит: Ono Pharmaceutical Co Ltd

The present invention relates to an agent which slows down the heart rate which has an excellent controlling ability in diagnostic imaging comprising a short-acting β-blocker (e.g. landiolol hydrochloride or esmolol hydrochloride). The short-acting β-blocker has a property of slowing down the heart rate and it can temporarily suppress the tachycardia at diagnosis. According to the dose and the method of administration, it can control the period for the heart rate adjustment. Also, the present invention relates to a diagnostic imaging auxiliary comprising a short-acting β-blocker as active ingredient.

Подробнее
26-07-2012 дата публикации

Michael addition reaction product and active energy ray-curable composition

Номер: US20120190846A1
Принадлежит: DIC Corp

The present invention provides a Michael addition reaction product between a specified compound having a group which functions as a Michael donor and a monomer or polymer having a group which functions as a Michael acceptor, a photoinitiator containing the Michael addition reaction product, and an active energy ray-curable composition containing the photoinitiator. The compound having a group functioning as a Michael donor used in the present invention is a phenyl ketone derivative and is characterized by having an amino group or a mercapto group as the group functioning as a Michael donor.

Подробнее
02-08-2012 дата публикации

Ubiquitin interacting motif peptides as cancer therapeutics

Номер: US20120197059A1
Автор: HONG Chen, Yunzhou DONG
Принадлежит: Oklahoma Medical Research Foundation

The present invention involves the use peptides comprising ubiquitin interacting motifs (UIMs) alone or in combination with other agents to treat diseases involving neovascularization, such as cancer.

Подробнее
09-08-2012 дата публикации

Process for the preparation of a powder comprising one or more complexing agent salts

Номер: US20120202731A1
Принадлежит: BASF SE

A process is proposed for the preparation of a powder comprising one or more complexing agent salts of the general formula starting from an aqueous solution comprising the one or more complexing agent salts in a concentration of from 10 to 80% by weight, based on the total weight of the aqueous solution, in a spray-drying process, comprising an atomization step and a drying step, wherein the atomization step is carried out with the addition of crystalline fine dust of the same complexing agent salt(s) as are present in the aqueous solution, or one or more complexing agent salts different therefrom, with an upper limit for the average particle diameter of the crystalline fine dust which is lower by at least a factor of 2 than the lower limit of the average particle diameter of the powder obtained after the process, in a fraction of from 0.1 to 20% by weight, based on the weight of the powder obtained after the process.

Подробнее
16-08-2012 дата публикации

L-ornithine phenyl acetate and methods of making thereof

Номер: US20120208885A1
Принадлежит: Ocera Therapeutics Inc

Disclosed herein are forms of L-ornithine phenyl acetate and methods of making the same. A crystalline form may, in some embodiments, be Forms I, II, III and V, or mixtures thereof. The crystalline forms may be formulated for treating subjects with liver disorders, such as hepatic encephalopathy. Accordingly, some embodiments include formulations and methods of administering L-ornithine phenyl acetate.

Подробнее
23-08-2012 дата публикации

Cardiomyocytes and methods of producing and purifying cardiomyocytes

Номер: US20120213748A1
Автор: Gabriel Nistor
Принадлежит: Individual

The invention provides methods for producing a culture of cardiomyocytes and cultures of cardiomyocytes. Exemplary methods of producing and cultures of cardiomyocytes include a population of cells including cells having spontaneous and periodic electrical activity, and/or including nodal, sino-atrial or pacemaker cells; immature cardiomyocytes (cardiomyoblasts); mature contractile cardiomyocytes; or a mixed population of two or more of such cells.

Подробнее
23-08-2012 дата публикации

Methods of treating a subject and related particles, polymers and compositions

Номер: US20120213854A1
Автор: Oliver S. Fetzer
Принадлежит: Individual

Described herein are methods for treating a subject with combinations of polymer-agent particles and cyclodextrin polymer agent conjugates. The methods herein may be used to treat subjects identified with cancer, cardiovascular disorders, autoimmune disorders, or inflammatory disorders. Also described herein are compositions, dosage forms, and kits comprising polymer-agent particles and cyclodextrin polymer agent conjugates.

Подробнее
30-08-2012 дата публикации

Stablized Melanocortin Ligands

Номер: US20120220525A1
Автор: Kenneth A. Gruber
Принадлежит: Tensive Controls Inc

Compositions and methods are disclosed for a non-naturally occurring melanocortin ligand comprised of a melanocortin analog coupled to a degradation-resistant C-terminal extension and, optionally, an N-terminal extension, to produce a stable melanocortin ligand having diminished or abolished cardiovascular activity while retaining desired melanocortin regulatory activity.

Подробнее
04-10-2012 дата публикации

Oral lysophilisates containing pvp/va

Номер: US20120252795A1
Автор: Thanh-Tam Nguyen
Принадлежит: Cephalon France SAS

The present invention relates to novel oral pharmaceutical compositions in lyophilized form, in which the dissolution and the bioavailability of the active ingredient that they contain are improved. The compositions according to the invention comprise in particular a polyvinyl acetate/polyvinylpyrrolidone copolymer. The oral lyophilisates according to the invention are particularly suitable for the production of medicaments based on active ingredients which have low solubility or very low solubility in water or which are virtually insoluble in water.

Подробнее
18-10-2012 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20120264945A1
Автор: Thomas Daly
Принадлежит: Thomas Daly

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

Подробнее
15-11-2012 дата публикации

Rare earth nanoparticles

Номер: US20120288535A1

This document provides methods and materials related to rare earth particles such as rare earth nanorods (e.g., inorganic lanthanide hydroxide nanorods). For example, rare earth (e.g., lanthanide) particles such as europium hydroxide nanorods, methods and materials for making rare earth particles (e.g., europium hydroxide nanorods), and methods and materials for using rare earth particles (e.g., europium hydroxide nanorods) as an imaging agent and/or to promote angiogenesis are provided.

Подробнее
22-11-2012 дата публикации

Device and method for combining a treatment agent and a gel

Номер: US20120296312A1
Принадлежит: Abbott Cardiovascular Systems Inc

A method including introducing a treatment agent at a treatment site within a mammalian host; and introducing a bioerodable gel material at the treatment site. An apparatus including a first annular member having a first lumen disposed about a length of the first annular member and a first entry port at a proximal end of the first annular member, and a second annular member coupled to the first annular member having a second lumen disposed about a length of the second annular member and a second entry port at a proximal end of the second annular member, wherein the first annular member and the second annular member are positioned to allow a combining of treatment agents introduced through each annular member at the treatment site.

Подробнее
29-11-2012 дата публикации

Process for preparing aminopolycarboxylates

Номер: US20120302783A1
Принадлежит: BASF SE

What is proposed is a process for preparing aminopolycarboxylates proceeding from the corresponding polyalkanolamines by oxidative dehydrogenation in the presence of a catalyst comprising 1 to 90% by weight of copper, based on the total weight of the catalyst, using a base, which comprises first performing a partial conversion of the polyalkanolamine to a reaction mixture comprising the aminopolycarboxylate at a temperature in the range from 140 to 180° C. until at least 10 to 90 mol % of the polyalkanolamine has been depleted, and then continuing the conversion at elevated temperature.

Подробнее
13-12-2012 дата публикации

METHOD OF RESOLUTION OF (RS)- 1,1'-BI-2-NAPHTHOL FOR OBTAINING ENANTIOMERIC PURE I.E. (S)-(-)-1,1'-BI-2-NAPHTHOL AND/OR (R)-(+)-1,1'-BI-2-NAPHTHOL VIA CO-CRYSTAL FORMATION WITH OPTICALLY ACTIVE DERIVATIVES OF y -AMINO ACIDS

Номер: US20120316361A1
Принадлежит: Lupin Ltd

Novel method for synthesis of optically pure (S)-(−)-1,1′-bi-2-naphthol and/or (R)-(+)-1,1′-bi-2-naphthol via resolution of racemic (RS)-1,1′-bi-2-naphthol through formation of co-crystal with optically active derivatives of γ-amino acids.

Подробнее
20-12-2012 дата публикации

Method of producing beraprost

Номер: US20120323025A1
Принадлежит: Lung LLC

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

Подробнее
27-12-2012 дата публикации

Oral delivery of peptide pharmaceutical compositions

Номер: US20120328666A1
Принадлежит: Unigene Laboratories Inc

Bioavailability of peptide active agents to be administered orally is enhanced by a pharmaceutical composition providing targeted release of the peptide to the intestine by combining the composition with an absorption enhancer. Bioavailability is further significantly increased by administering the composition in an acid-resistant protective vehicle which transports components of the invention through the stomach. The composition may optionally further include a sufficient amount of a pH-lowering agent to lower local intestinal pH. All components are released together into the intestine with the peptide.

Подробнее
03-01-2013 дата публикации

Treatment of vascularized pigment epithelial detachment with anti-vegf therapy

Номер: US20130004486A1
Принадлежит: Genentech Inc

Methods for treating vascularized pigment epithelial detachment using anti-VEGF agents are disclosed.

Подробнее
03-01-2013 дата публикации

Method of treating myocardial injury

Номер: US20130005037A1
Автор: Marc S. Penn
Принадлежит: CLEVELAND CLINIC FOUNDATION

A method of treating a myocardial injury of a subject includes administering a population of at least one of mesenchymal stem cells (MSCs), multipotent adult progenitor cells (MAPCs), embryonic stem cells (ESCs), induced pluripotent stem cells (iPSs), which have down-regulated expression of disabled-2 (Dab2), to the subject.

Подробнее
10-01-2013 дата публикации

Synergists

Номер: US20130012611A1
Принадлежит: SUN CHEMICAL BV

Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C 1.10 -alkyl, R 1 is H or methyl, X is an extender group, n is 0 or an integer between 1 and 12 inclusive, A is a polyol residue wherein the unsubstituted polyol from which the residue is derived has at least y OH groups, and y is an integer>1, can easily be prepared, and are useful as synergists in radiation curing.

Подробнее
17-01-2013 дата публикации

Processes for the preparation of key intermediate for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof

Номер: US20130018065A1
Принадлежит: Lek Pharmaceuticals dd

The present invention relates in general to the field of organic chemistry and in particular to a process for the preparation of 5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-methanesulfonylamino)pyrimidine (RSVL) as well as a process for preparing crystalline 5-((E)-2-((2S,4R)-4-(tert-butyldimethylsilyloxy)-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethanesulfonylamino)pyrimidine (RSVLTBS) useful as key intermediates for the preparation of rosuvastatin or pharmaceutically acceptable salts thereof.

Подробнее
24-01-2013 дата публикации

Carboxylic acid derivatives having an oxazolo[5,4-b]pyridine ring

Номер: US20130023557A1
Принадлежит: SANOFI SA

The invention therefore relates to compounds of the formula I in which X, Y, R 1 , R 2 and R 3 have the given meanings. The compounds of the formula I are suitable, for example, for wound healing.

Подробнее
07-02-2013 дата публикации

Isotopologues of 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9h-purin-2-ylamino]-cyclohexan-1-ol

Номер: US20130034495A1
Принадлежит: Signal Pharmaceuticals LLC

Provided herein are isotopologues of Compound 1, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.

Подробнее
28-02-2013 дата публикации

Use of Gold Nanoclusters in Ameliorating Oxidate Stress and/or Aging

Номер: US20130052270A1

Disclosed herein is the novel use of a gold nanocluser for ameliorating oxidative stress and/or aging of a cultured cell or a subject having an oxidative stress and/or aging condition mediated by a vascular factor. The gold nanocluster has a particle size ranging from about 0.1 to 20 nm, and preferably is dihydrolipoic acid (DHLA) coated gold nanocluster.

Подробнее
28-02-2013 дата публикации

Method for producing a solid with sufficiently low hygroscopicity which comprises glutamic acid-n,n-diacetic acid (glda) or a derivative thereof

Номер: US20130053296A1
Автор: Andreas Baranyai
Принадлежит: BASF SE

The present invention relates to a solid with sufficiently low hygroscopicity which comprises glutamic acid-N,N-diacetic acid (GLDA) or derivatives and/or salts thereof, and a method for its production.

Подробнее
07-03-2013 дата публикации

Novel Gene And Protein Associated With Angiogenesis And Endothelial Cell Specific Apoptosis

Номер: US20130058940A1
Принадлежит: CLEVELAND CLINIC FOUNDATION

This invention provides isolated nucleic acid and amino acid sequences encoding VG5Q, a novel angiogenic growth factor protein with pro-angiogenic activity, a forkhead-associated domain, a G-patch domain; characteristic subcellular localization in an in vitro Matrigel model of angiogenesis: towards the cell periphery in early stages of tubulogenesis, between cells in newly formed endothelial tubes, and no nuclear staining after 24 hours; is expressed in endothelial cells; is secreted during angiogenesis; and interacts with TWEAK. The invention also provides for expression vectors containing nucleic acid sequences encoding VG5Q protein, and host cells containing one or more expression vectors for the recombinant expression of VG5Q. The invention also provides for methods of using VG5Q for the diagnosis and treatment of angiogenesis-mediated diseases or disorders.

Подробнее
21-03-2013 дата публикации

DISPERSANT COMPOSITION

Номер: US20130072704A1
Принадлежит: LUBRIZOL ADVANCED MATERIALS, INC.

The present invention relates to a composition containing a particulate solid, a non-polar organic medium, and a compound obtained/obtainable by reacting an aromatic amine with hydrocarbyl-substituted acylating agent, wherein the hydrocarbyl-substituted acylating agent is selected from the group consisting of an oligomer or polymer from condensation polymerisation of a hydroxy-substituted Ccarboxylic acid into a polyester, an optionally hydroxy-substituted Ccarboxylic acid, a C-hydrocarbyl substituted acylating agent, and a polyolefin-substituted maleic anhydride. The invention further provides compositions for inks, thermoplastics, plasticisers, plastisols, crude grinding and flush. 129-. (canceled)31. The compound of claim 30 , wherein the aromatic amine to hydro-carbyl-substituted acylating agent mole ratio may be in the range of 2:1 to 1:10.32. The compound of claim 30 , wherein the aromatic amine to hydro-carbyl-substituted acylating agent mole ratio may be 1:1 to 1:2.33. The compound of claim 30 , wherein the compound is obtained by reacting an aromatic amine with a hydroxy-substituted Ccarboxylic acid claim 30 , or mixtures thereof.34. The compound of claim 30 , wherein the hydroxy-substituted Ccarboxylic acid is polymerised to form a polyester.35. The composition of claim 34 , wherein the polyester is a polymerisation product of a hydroxy-substituted carboxylic acid of general formula HO—X—COOH claim 34 , wherein X is a divalent saturated or unsaturated aliphatic radical containing at least 4 carbon atoms between the hydroxyl and carboxylic acid groups.36. The compound of claim 34 , wherein the polyester has 4 to 20 repeat units of a hydroxy-substituted Ccarboxylic acid.37. The compound of claim 33 , wherein the hydroxy-substituted Ccarboxylic acid is a mixture of ricinoleic acid and either 12-hydroxystearic acid or 9- and 10-hydroxystearic acids.38. The compound of claim 33 , wherein the hydroxy-substituted Ccarboxylic acid is ricinoleic acid claim 33 , 12- ...

Подробнее
21-03-2013 дата публикации

Method for optimising gene expression using synonymous codon optimisation

Номер: US20130074218A1
Автор: Ian Hector Frazer
Принадлежит: University of Queensland UQ

The present invention discloses a method for modulating the quality of a selected phenotype that is displayed by an organism or part thereof and that results from the expression of a polypeptide-encoding polynucleotide by replacing at least one codon of that polynucleotide with a synonymous codon that has a higher or lower preference of usage by the organism or part thereof to produce the selected phenotype than the codon it replaces. The present invention is also directed to the use of a codon-modified polynucleotide so constructed for modulating the quality of a selected phenotype displayed by an organism or part thereof.

Подробнее
28-03-2013 дата публикации

NOVEL DERIVATIVES OF MESALAZINE, PROCESS OF THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF INTESTINAL INFLAMMATORY DISEASES

Номер: US20130079399A1
Автор: LABRUZZO Carla
Принадлежит: SOFAR SPA

The present invention refers to the compounds corresponding to the following general formula (I): 3. 5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof , preferably hydrochloride salt.4. Method for treating acute or chronic intestinal inflammatory diseases claim 1 , comprising the administration to a patient in need of such treatment a compound according to claim 1 , wherein said acute or chronic intestinal inflammatory diseases are preferably selected from among IBD claim 1 , IBS claim 1 , ulcerative colitis claim 1 , Crohn's disease claim 1 , diverticular disease claim 1 , more preferably IBD.5. Method for treating according to claim 4 , wherein said acute or chronic intestinal inflammatory diseases are acute intestinal inflammatory diseases.6. Method for treating according to claim 4 , wherein said acute or chronic intestinal inflammatory diseases are chronic intestinal inflammatory diseases.7. Method for treating according to claim 6 , wherein said chronic intestinal inflammatory diseases are in a remission phase.8. A compound according to claim 2 , characterised in that it is administered enterally claim 2 , preferably orally and/or rectally claim 2 , or topically claim 2 , preferably through anal application.9. Pharmaceutical composition containing a compound according to claim 2 , and at least one physiologically acceptable excipient.10. Pharmaceutical composition according to selected from among tablet claim 9 , capsule claim 9 , granule claim 9 , microgranule claim 9 , suspension or aqueous solution claim 9 , enema claim 9 , suppository claim 9 , gel and rectal foam.13. Process according to claim 11 , wherein the step a) is conducted in an aprotic polar solvent and/or in a mixture of said solvent with HO preferably in a molar ratio comprised between 1:1 and 3:1 claim 11 , more preferably 2:1.14. Process according to claim 11 , wherein said mixture is constituted by dioxane and water claim 11 , preferably in a 2:1 molar ratio ...

Подробнее
11-04-2013 дата публикации

PROCESS FOR THE PREPARATION OF ISOSERINE DERIVATIVES

Номер: US20130090493A1
Принадлежит: INDENA S.P.A

This invention relates to a “one pot” process for the preparation of isoserine derivatives in high diastereoselective way. The process according to the invention includes the steps of reacting a protected glycidic acid with imines to yield isoserines protected both at the —OH and at the —COOH groups, deprotection of the obtained intermediates to isoserines or isoserine 1-4C— alkyl esters. Pure threo derivatives as the main isomer are obtained. 2. A process according to wherein the reacting step between compounds 3 and 4 is catalyzed by protic or Lewis acids.3. A process according to wherein the reacting step is catalyzed by Lewis acids selected from InCland SnCland MgBr.4. A process according to wherein the reacting step temperature is in the range from −40 to −30° C.5. A process according to wherein the reacting step is carried out in aprotic polar solvents selected from dimethylformamide claim 2 , acetonitrile claim 2 , dichloromethane claim 2 , chloroform claim 2 , tetrahydrofuran claim 2 , preferably Acetonitrile and dichloromethane.6. A process according to wherein the alcoholyzing step is performed using an alcohol ROH in presence of trimethylsilyl chloride.7. A process according to which is performed as “one pot reaction” without isolating the intermediates to give the final pure threo diastereoisomers by crystallization.8. A process according to comprising:{'sup': 1', '2, 'sub': '2', 'generating in situ imine 4 from the aldehyde (RCHO) and an amine (RNH), in acetonitrile at room temperature and in presence of molecular sieves or by distillation of the azeotropic mixture acetonitrile/water;'}adding silyl derivative 3 at −30° C. followed by addition of the catalyst to obtain a crude reaction mixture; and{'sup': '3', 'treating the crude reaction mixture with trimethylsilyl chloride in alcohol and isolation of the pure diastereoisomer (2R*,3S*)-1 (where Ris an (C1-C4)-alkyl group) after crystallization.'}9. A process according to claim 8 , wherein said amine is ...

Подробнее
18-04-2013 дата публикации

AMINO ACID GROUP-MODIFIED ORGANOPOLYSILOXANE AND SILANE, AMINO ACID GROUP-CONTAINING COMPOUND, AND PRODUCTION METHOD THEREOF

Номер: US20130096340A1
Автор: MORIYA Hiroyuki
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

An amino acid-modified organopolysiloxane is provided. It has an amino acid derivative bonded to at least one silicon atom of the organopolysiloxane segment constituting the backbone of the organopolysiloxane via an amide bond represented by the following general formula (1): 3. A method according to wherein the compound represented by the general formula (13) is an aliphatic amine containing 6 to 32 carbon atoms.4. A method according to wherein the compound represented by the general formula (13) is a higher aliphatic amine containing 12 to 32 carbon atoms.5. A method according to wherein the compound represented by the general formula (13) is a hydroxy aliphatic amine containing 6 to 32 carbon atoms.6. A method according to wherein the compound represented by the general formula (14) is pyroglutamine acid. The present application is a 37 C.F.R. §1.53(b) divisional of, and claims priority to, U.S. application Ser. No. 13/584,166, filed Aug. 13, 2012. Application Ser. No. 13/584,166 is a divisional of, and claims priority to, U.S. application Ser. No. 12/965,203, filed Dec. 10, 2010. Priority is also claimed to Japanese Patent Application No. 2009-281099 filed Dec. 11, 2009, Japanese Patent Application No. 2009-281114 filed on Dec. 11, 2009 and Japanese Patent Application No. 2009-281126 filed on Dec. 11, 2009. The entire contents of each of these applications is hereby incorporated by reference.This invention relates to an amino acid-modified organopolysiloxane and silane, an amino acid group-containing compound, and production method thereof.Various compounds and methods have been investigated for use in producing an amino acid-modified or a peptide-modified silicone and for use in its production method.For example, in the case of a silicone modified with an amino acid derivative represented by the following formula:the silicone has a structure in which the amino group and the carboxy group of the amino acid have been protected. In addition, this silicone has been ...

Подробнее
25-04-2013 дата публикации

ANTIMICROBIAL COMPOUNDS OF 1,4-NAPHTOQUINONE STRUCTURE

Номер: US20130102650A1
Принадлежит:

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

Подробнее
02-05-2013 дата публикации

Use of dabigatran etexilate for treating patients with pulmonary hypertension

Номер: US20130109722A1
Автор: Martin Feuring
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to a new use of dabigatran etexilate of formula I optionally in the form of the pharmaceutically acceptable salts thereof, as well as new medicament formulations which may be used for this purpose.

Подробнее
09-05-2013 дата публикации

NOVEL COMPOUNDS

Номер: US20130115179A1
Принадлежит:

The invention relates to novel polyglycerol based UV-filters as well as to topical compositions comprising such novel polyglycerol based UV-filters. Furthermore, the invention relates to the use of such novel polyglycerol based UV-filters to enhance the solubility of butyl methoxydibenzoylmethane or bis-ethylhexyloxyphenol methoxyphenyl triazine in cosmetic oils. 1. Polyglycerol based UV filters obtainable by a process comprising the steps ofa.) ring-opening polymerization of x mol equivalents of glycidol using 1 mol equivalent of a polyol starter unit with y mol equivalents hydroxyl-groups followed byb.) block copolymerization with z×(x+y) mole equivalents of propyleneoxide to form a hyperbranched polyether-polyol backbone carrying (x+y) mol equivalents hydroxyl-groups followed byc.) partial or total esterification of the hydroxyl groups with 2-(4-Diethylamino-2-hydroxybenzoyl)benzoic acidwherein x is an integer from 3-16, y is an integer from 1-6, and z is an integer from 0-10.2. The polyglycerol based UV filter according to claim 1 , wherein 15 to 100% claim 1 , more preferably 30-80% claim 1 , most preferably about 60-75% of the hydroxyl groups of the hyperbranched polyether-polyol backbone are esterified with 2-(4-Diethylamino-2-hydroxybenzoyl)benzoic acid.3. The polyglycerol based UV filter according to claim 1 , wherein the amount of glycidol units x is selected in the range of 3 to 16 mol equivalents per mol equivalent of the polyol starter unit.4. The polyglycerol based UV filter according to claim 1 , wherein the polyol starter unit is trimethylolpropane.5. The polyglycerol based UV filter according to claim 1 , wherein 60-75% of the terminal hydroxyl groups of the hyperbranched polyether-polyol backbone are linked to a 2-(4-Diethylamino-2-hydroxybenzoyl)benzoyl moiety and the residual terminal hydroxyl groups are linked to a capping group.6. The polyglycerol based UV filter according to claim 5 , wherein the capping group is a 2-ethyl hexanoyl claim 5 , ...

Подробнее
09-05-2013 дата публикации

Methods for treating or preventing vascular graft failure

Номер: US20130115256A1
Принадлежит: Moerae Matrix Inc

The described invention provides pharmaceutical compositions and methods for treating or preventing vascular graft failure in a subject in need of such treatment, the method comprising administering a therapeutically effective amount of a composition comprising a polypeptide of amino acid sequence YARAAARQARAKALARQLGVAA (SEQ ID NO: 1) or a functional equivalent thereof, and a pharmaceutically acceptable carrier. The methods also are clinically useful for treating a pre-atherosclerotic intimal hyperplasia condition.

Подробнее
09-05-2013 дата публикации

RFamide-Related Peptides and Methods Thereof

Номер: US20130116184A1
Принадлежит: University of Michigan

Provided herein methods and compositions directed to RFRP-1 polypeptides for modulating cardiac contractile function, for preventing and/or treating cardiac disorders.

Подробнее
09-05-2013 дата публикации

PROCESS AND INTERMEDIATES FOR PREPARING INTEGRASE INHIBITORS

Номер: US20130116437A1
Принадлежит: Gilead Sciences, Inc.

The invention provides synthetic processes and synthetic intermediates that can be used to prepare 4-oxoquinolone compounds having useful integrase inhibiting properties. 19-. (canceled)11. The method of wherein the compound of formula 3 is converted to the compound of formula 4 by treatment with a silane reducing agent in the presence of an acid.12. The method of wherein the silane reducing agent is triethylsilane and the acid is trifluoroacetic acid.19. The method of wherein the compound of formula 9 is converted to the compound of formula 10 by treatment with a base.2023-. (canceled) This application is a continuation of Ser. No. 12/892,682, filed on 28 Sep. 2010, which is a continuation of Ser. No. 11/853,606, filed on 11 Sep. 2007, now U.S. Pat. No. 7,825,252, granted on 2 Nov. 2010, and claims priority under 35 U.S.C. 119(e) from U.S. Provisional Patent Application No. 60/844,020 filed 12 Sep. 2006, and from U.S. Provisional Patent Application No. 60/905,365 filed 7 Mar. 2007.International Patent Application Publication Number WO 2004/046115 provides certain 4-oxoquinolone compounds that are useful as HIV integrase inhibitors. The compounds are reported to be useful as anti-HIV agents.International Patent Application Publication Number WO 2005/113508 provides certain specific crystalline forms of one of these 4-oxoquinolone compounds, 6-(3-chloro-2-fluorobenzyl)-1-[(S)-1-hydroxymethyl-2-methylpropyl]-7-methoxy-4-oxo-1,4-dihydroquinolone-3-carboxylic acid. The specific crystalline forms are reported to have superior physical and chemical stability compared to other physical forms of the compound.There is currently a need for improved methods for preparing the 4-oxoquinolone compounds reported in International Patent Application Publication Number WO 2004/046115 and in International Patent Application Publication Number WO 2005/113508. In particular, there is a need for new synthetic methods that are simpler or less expensive to carry out, that provide an ...

Подробнее
09-05-2013 дата публикации

Process for preparing saturated amino acids or saturated amino esters comprising a metathesis step

Номер: US20130116458A1

The subject matter of the invention is a process for synthesizing a saturated long-chain o.,0)-amino ester (acid) obtained in a first step by cross-metathesis between an acrylic first compound and a monounsaturated second compound comprising at least one nitrile, acid or ester trivalent function, one of these compounds comprising a nitrile function and the other an acid or ester function, in the presence of a ruthenium carbene metathesis catalyst, and in a second step by hydrogenation of the monounsaturated nitrile ester (acid) obtained in the presence of the metathesis catalyst of the preceding stop, acting as a hydrogenation catalyst.

Подробнее
16-05-2013 дата публикации

Imaging Agents

Номер: US20130123618A1
Автор: Mark M. Goodman
Принадлежит: EMORY UNIVERSITY

This invention provides amino acid derivatives useful in detecting and evaluating brain and body tumors, including (1S,2S) anti-2-[ 18 F]FACPC and (1R,2R) anti-2-[ 18 F]FACPC.

Подробнее
23-05-2013 дата публикации

METHODS AND COMPOSITIONS FOR DELIVERY OF ACTIVE AGENTS

Номер: US20130129785A1
Принадлежит: ALNYLAM PHARMACEUTICALS, INC

A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction. 2. The compound of claim 1 , wherein X are Y are alkyl.3. The compound of claim 3 , wherein X and Y are both methyl.4. The compound of claim 1 , wherein Lis a linear alkylene unit.5. The compound of claim 1 , wherein Lis a linear alkylene unit.6. The compound of claim 5 , wherein Lcontains one or more double bonds and one or more cycloalkylene groups.7. The compound of claim 1 , wherein Rand Rare each claim 1 , independently claim 1 , C-Calkyl or C-Calkenyl.8. The compound of claim 7 , wherein one of Rand Ris a linear C-Calkyl or C-Calkenyl group and the other of Rand Ris a branched C-Calkyl or C-Calkenyl group.9. The compound of claim 1 , wherein Z is —C(O)O— claim 1 , —C(O)N(R)— claim 1 , —O(CO)N(R) claim 1 , —C(O)N(R)C(O)O— claim 1 , or —N(R)C(O)N(R)—.10. The compound of claim 1 , wherein Ris H or alkyl.11. The compound of claim 1 , wherein{'sub': 1', '4, 'X and Y are each, independently, C-Calkyl;'}{'sup': 1', '2, 'sub': 2', '10, 'Land Lare each, independently, an C-Clinear or branched alkylene linking unit, which may optionally contain one or more double bonds and further may optionally be interrupted by one or more heteroatoms and/or one or more cycloalkylene groups;'}{'sub': 1', '2', '10', '30, 'Rand Rare each, independently, a C-Caliphatic group, which may optionally contain one or more double bonds, and may optionally be interrupted by one or more heteroatoms and/or one or more cycloalkylene groups;'}{'sup': 3', '3', '3', '3', '3', '3', '3', '3, 'Z is —C(O)O—, —OC(O)—, —C(O)N(R)—, —N(R)C(O)—, —O(CO)N(R), —N(R)C(O)O—, —C(O)N(R)C(O)O—, —OC(O)N(R)C(O)— or —N(R)C(O)N(R)—;'}{'sup': '3', 'sub': 1', '4, 'each occurrence of Ris independently H or C-Calkyl; and'}{'img': [{'@id': 'CUSTOM-CHARACTER-00003', '@ ...

Подробнее
23-05-2013 дата публикации

Esters with Antimicrobial, Bioresistant and Fungal Resistant Properties

Номер: US20130131365A1
Автор: Daly Thomas
Принадлежит:

A bromine/nitro moiety linked into the backbone of an ester or other compound over a wide range of occurrence rates provides antimicrobial, bio-resistant and fungal resistant properties for metal working fluids (MWF)s and other coatings. The moiety can be have the bromo and nitro groups linked to the same or different carbon atoms. The present invention also relates to urethanes, urea, amides, imides, carbonates, ethers, siloxanes, and many other types of linkages essential to MWF bases. 2. The anionic surfactant of where n=n′=7 claim 1 , m=m′=7 claim 1 , and A=Br.3. A metal working fluid base comprising a molecule according to .4. A foaming or anti-foaming agent comprising a molecule according to .6. The molecule of where R═R′=—(CH)CHA=—(CH2)CH.7. A metal working fluid base comprising a molecule according to .8. A surfactant comprising a molecule according to .9. A foaming or anti-foaming agent comprising a molecule according to . This is a continuation of application Ser. No. 13/351,512 filed Jan. 17, 2012 which was a continuation of Ser. No. 12/965,252 filed Dec. 10, 2010 which was a divisional from application Ser. No. 12/287,726 filed Oct. 10, 2008, now abandoned, which was a continuation-in-part of application Ser. No. 11/800,569 filed May 7, 2007, now U.S. Pat. No. 7,439,376 issued Oct. 21, 2008, which was a continuation in part of application Ser. No. 10/603,356 filed Jun. 25, 2003, now abandoned, which claimed priority from U.S. Provisional patent application No. 60/392,007 filed Jun. 26, 2002. Applications Ser. Nos. 13/351,512, 12/965,252, 12/287,726, 11/800,569, 10/603,356 and 60/392,007 are hereby incorporated by reference. This application also incorporates by reference my other patent application Ser. No. 10/350,928 filed Jan. 23, 2003 entitled Polymers with Antimicrobial, Bioresistant and Fungal Resistant Properties.The text of this continuation application is substantially identical to that of grandparent application Ser. No. 10/603,356.1. Field of ...

Подробнее
06-06-2013 дата публикации

(2e)-3-phenyl-n-[2,2,2-trifluoro-1-[[8-quinolineamino)thiomethyl]amino]ethyl]-2-acrylamide and pharmaceutical uses thereof

Номер: US20130143917A1
Принадлежит: CHINESE PLA GENERAL HOSPITAL

The present invention relates to an acrylamide compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate thereof, to a composition comprising the compound or an isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluent, and to a use of the compound or the composition for prophylaxis and/or treatment of a disease or disorder associated with cardiomyocyte apoptosis

Подробнее
13-06-2013 дата публикации

ALKYNE AND ALKENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE-1 RECEPTOR MODULATORS

Номер: US20130150331A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to claim 1 , wherein:{'img': {'@id': 'CUSTOM-CHARACTER-00015', '@he': '3.89mm', '@wi': '6.69mm', '@file': 'US20130150331A1-20130613-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'sup': 14', '15, '“” represents a double bond “—CR═CR—”.'}3. A compound according to claim 1 , wherein:{'sup': '1', 'sub': '2', 'Lis CH.'}4. A compound according to claim 1 , wherein:{'sup': '1', 'Lis O, S or NH.'}7. A compound according to claim 1 , selected from:[3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propyl]phosphonic acid; and3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propanoic acid.8. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.9. A pharmaceutical composition according to claim 8 , wherein the compound is selected from:[3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propyl]phosphonic acid; and3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propanoic acid. This application is a Divisional of U.S. patent application Ser. No. 13/305,398, filed Nov. 28, 2011, which claims the benefit of U.S. Provisional Application Ser. No. 61/419,278 filed Dec. 3, 2010, both of which are hereby incorporated by reference in their entirety.The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of sphingosine-1-phosphate receptors. The invention relates specifically to the use of ...

Подробнее
13-06-2013 дата публикации

Method for treating mechanical allodynia comprising administration of eugenol

Номер: US20130150455A1
Принадлежит: SNU R&DB FOUNDATION

The present invention relates to a pharmaceutical composition for selectively treating mechanical allodynia, which provides eugenol or a pharmaceutically acceptable salt thereof at a concentration lower than that which would inhibit voltage-gated sodium channels (VGSCs), a pharmaceutical composition for blocking hyperpolarization-activated current (I h ), and a transdermal preparation for treating mechanical allodynia comprising the composition. Even though administered at a concentration lower than that which would inhibit VGSCs, the eugenol of the present invention inhibits I h in a cAMP or G-protein coupled receptor (GPCR) independent manner, thereby selectively ameliorating mechanical allodynia. Therefore, when the eugenol of the present invention is formulated into a transdermal preparation to be provided at a concentration lower than that which would inhibit VGSCs, and directly applied to the wound lesion, it can be used as a pharmaceutical composition capable of selectively treating mechanical allodynia.

Подробнее
20-06-2013 дата публикации

Method for Production and Use of Mite Group 1 Proteins

Номер: US20130157310A1
Принадлежит: Merck Patent GmBH

The present invention includes a method to produce a recombinant mite Group 1 protein in a methyltrophic yeast or an Escherichia coli microorganism. The present invention also relates to a recombinant mite Group 1 protein obtained by such a method, such a recombinant protein being able to selectively bind IgE or cause proliferation of a T cell that proliferates in response to a native mite Group 1 protein. Also included in the present invention is the use of such a recombinant mite Group 1 protein to detect mite allergy or to reduce an allergic response to a mite Group 1 protein. The present invention also includes novel mite Group 1 nucleic acid molecules, proteins, recombinant molecules, and recombinant cells, as well as uses thereof.

Подробнее
20-06-2013 дата публикации

Process for Preparing Crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic Acid and Use for Production of Primovist®

Номер: US20130158241A1
Принадлежит: Bayer Intellectual Property GmbH

The invention relates to a method for producing crystalline 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I by saponifying 3,6,9-triaza-3,6,9-tris(tert-butoxycarbonylmethyl)-4-(4-ethoxybenzyl)-undecanedioic acid di-tert-butyl ester of the formula II in an aqueous alkali metal hydroxide solution and using 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid of the formula I for producing the gadolinium complex of 3,6,9-triaza-3,6,9-tris(carboxymethyl)-4-(4-ethoxybenzyl)undecanedioic acid [(Gd-EOB-DTPA)=Primovist®].

Подробнее
20-06-2013 дата публикации

CANCER HEAT THERAPY-ENHANCING AGENT

Номер: US20130158293A1
Принадлежит:

Provided is an enhancer for cancer thermotherapy not combined with photodynamic therapy. Cancer treatment not combined with photodynamic therapy is made available by using, as an enhancer for cancer thermotherapy, 5-aminolevulinic acids represented by formula (1): 2. The enhancer for cancer thermotherapy according to claim 1 , wherein the 5-aminolevulinic acids or a salt thereof are not encapsulated inside a lipid membrane or in an internal aqueous phase thereof. The present invention relates to an enhancer for cancer thermotherapy, and more particularly to an enhancer for cancer thermotherapy not combined with photodynamic therapy (PDT), comprising 5-aminolevulinic acids or a salt thereof.Cancer (malignant tumor) is the most frequent cause of death in Japan, and one out of two Japanese is said to suffer from the disease. In addition, cancer is one of the leading causes of death among other developed countries. Accordingly, development of an effective treatment method for cancer has been a long-lasting goal of most people in the world including Japan. Cancer, however, derives from cells of a patient himself/herself. Thus, an effective therapeutic agent and/or method capable of effectively treating cancer without an adverse effect have not been easily developed, so that a potent therapeutic agent or method has yet to be reported.Examples of current major cancer treatment include surgical treatment, chemotherapy, and radiotherapy. Recently, the treatment has extended to include thermotherapy and photodynamic therapy.The above thermotherapy is a treatment method which takes advantage of the fact that cancer cells are heat-sensitive in nature compared to normal cells, and specifically inhibits proliferation of the cancer cells. That is, when a tissue containing cancer and normal cells is heated at about 42 to 43° C.., homeostasis plays a role in the section of the normal cells to expand blood vessels surrounding the cells, thereby increasing their blood flow and ...

Подробнее
20-06-2013 дата публикации

PROCESS FOR THE PREPARATION OF RACEMIC ALPHA-AMINO ACIDS

Номер: US20130158294A1
Принадлежит:

Process for the preparation of racemic α-amino acids or of glycine, wherein the corresponding α-hydroxycarboxylic acid, selected from hydroxyacetic acid, lactic acid, malic acid, α-hydroxyglutamic acid, isocitric acid, tartronic acid and tartaric acid, or at least one salt of the corresponding α-hydroxycarboxylic acid is reacted in the presence of at least one heterogeneous catalyst which comprises at least one transition metal, in the presence of hydrogen with at least one nitrogen compound (c), where the nitrogen compound (c) is selected from primary and secondary amines and ammonia. 1. A process for the preparation of racemic α-amino acids or of glycine , wherein the corresponding α-hydroxycarboxylic acid , selected from hydroxyacetic acid , lactic acid , malic acid , α-hydroxyglutamic acid , isocitric acid , tartronic acid and tartaric acid , or at least one salt of the corresponding α-hydroxycarboxylic acid is reacted in the presence of at least one heterogeneous catalyst which comprises at least one transition metal , in the presence of hydrogen with at least one nitrogen compound (c) , where nitrogen compound (c) is selected from primary and secondary amines and ammonia.2. The process according to claim 1 , wherein heterogeneous catalysts are selected from Raney metals and transition metal applied to a solid support.3. The process according to or claim 1 , wherein the transition metal is selected from Ni claim 1 , Cu and Co.4. The process according to any one of to claim 1 , wherein the transition metal in the heterogeneous catalyst is present during the process at least for part of the time in oxidation state zero.5. The process according to any one of to claim 1 , wherein the nitrogen compound (c) is selected from ammonia.6. The process according to any one of to claim 1 , which is carried out at a temperature in the range from 150 to 280° C.7. The process according to any one of to claim 1 , wherein the α-hydroxycarboxylic acid is selected from racemic ...

Подробнее
27-06-2013 дата публикации

AMINE ADDUCTS, DERIVATIVES THEREOF, METHODS FOR MAKING SUCH ADDUCTS AND DERIVATIVES, AND METHODS FOR USING SUCH ADDUCTS AND DERIVATIVES

Номер: US20130161014A1
Принадлежит: Rhodia Operations

An amine adduct is made by (1) forming an addition intermediate by heating a mixture comprising at least one diene and at least one unsaturated fatty acyl compound, and reacting the addition intermediate with a diamine to form the amine adduct, or by (2) reacting at least one unsaturated fatty acyl compound with at least one diamine to form an amine intermediate, and heating a mixture of the amidoamine intermediate and at least one diene to form the amine adduct, or by (3) reacting at least one unsaturated fatty tertiary amine compound with at least at least one diene to form the amine adduct. A surfactant composition is derived from the amine adduct and is particularly useful in a method for enhancing the recovery of oil from a reservoir having a production wellbore, comprising introducing an aqueous flooding fluid into the reservoir at one or more locations different from the location of the production wellbore, said fluid comprising the surfactant composition and recovering the oil through the production wellbore. 1. An amine adduct , comprising the product obtained by: '(b) reacting the addition intermediate with a diamine to form the amine adduct, or', '(1)(a) forming an addition intermediate by heating a mixture comprising at least one diene and at least one unsaturated fatty acyl compound, and'} '(b) heating a mixture of the amidoamine intermediate and at least one diene to form the amine adduct, or', '(2)(a) reacting at least one unsaturated fatty acyl compound with at least one diamine to form an amidoamine intermediate, and'}(3) reacting at least one unsaturated fatty tertiary amine compound with at least at least one diene to form the amine adduct.2. The amine adduct of wherein the adduct is an amidoamine product claim 1 , obtained by: '(b) reacting the addition intermediate with a diamine to form the amidoamine product, or', '(1)(a) forming an addition intermediate by heating a mixture comprising at least one diene and at least one unsaturated fatty acyl ...

Подробнее
27-06-2013 дата публикации

Fc FUSION PROTEINS

Номер: US20130164286A1

The embodiments of the invention relate to compositions, methods, and kits comprising a fusion protein. The fusion proteins of the embodiments include monomer polypeptides which in one embodiment have at least a binding domain, an optional hinge region, a collagen-like domain and the Fc domain of a human IgG.

Подробнее
27-06-2013 дата публикации

SYNTHESIS OF OMEGA-AMINO CARBOXYLIC ACIDS AND THEIR ESTERS FROM UNSATURATED FATTY ACID DERIVATIVES

Номер: US20130165685A1
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to a process for preparing omega-amino acids or their esters, which is characterized by the following steps: 1. A process for preparing an omega-amino compound , the process comprising:ozonolysis of an unsaturated fatty acid or fatty acid derivative, to obtain an ozonolysis reaction mixture; andreductive amination of the ozonolysis reaction mixture to obtain an omega-amino compound,wherein the ozonolysis occurs in the presence of a C1 to C5 alcohol in a mixture comprising at least 0.5% by weight of water, based on a total amount of solvent in the mixture.2. The process according to claim 1 , wherein the mixture comprises 1% to 20% by weight of the water claim 1 , based on the total amount of solvent.3. The process according to claim 1 , wherein the mixture comprises 2% to 15% by weight of the water claim 1 , based on the total amount of solvent.4. The process according to claim 1 , wherein the mixture comprises 5% to 10% by weight of the water claim 1 , based on the total amount of solvent claim 1 , with the proviso that the water is present at least in a stoichiometric amount relative to a number of double bonds reacted.54. The process according to claim 1 , comprising ozonization of a fatty acid or fatty acid derivative comprising at least one double bond.6. The process according to claim 1 , wherein the ozonolysis and the reductive amination are occur directly after one another without isolation or workup of the ozonolysis reaction mixture.7. The process according to claim 1 , wherein the unsaturated fatty acid or fatty acid derivative is at least one selected from the group consisting of oleic acid claim 1 , an alkyl oleate claim 1 , undecylenic acid claim 1 , an alkyl undecylenate claim 1 , erucic acid claim 1 , and an alkyl erucate.8. The process according to claim 1 , wherein the reductive amination occurs in the presence of hydrogen and a catalyst.9. The process according to claim 8 , wherein the catalyst is Raney nickel.10. The process ...

Подробнее
27-06-2013 дата публикации

PROCESS FOR PREPARING ONE OR MORE COMPLEXING AGENTS SELECTED FROM METHYLGLYCINEDIACETIC ACID, GLUTAMIC ACID DIACETIC ACID AND SALTS THEREOF

Номер: US20130165689A1
Принадлежит:

Process for preparing one or more complexing agents selected from methylglycinediacetic acid, glutamic acid diacetic acid and salts thereof 2. The process according to claim 1 , wherein the non-activated precursor of the catalyst in question has a degree of crystallization K in the range from 0 to 30%.3. The process according to or claim 1 , wherein the activated catalyst comprises 1 to 50% by weight of copper claim 1 , based on the total weight of the catalyst.4. The process according to claim 3 , wherein the activated catalyst comprises 5 to 40% by weight of copper claim 3 , based on the total weight of the catalyst.5. The process according to claim 4 , wherein the activated catalyst comprises 10 to 30% by weight of copper claim 4 , based on the total weight of the catalyst.6. The process according to any one of to claim 4 , wherein the complexing agent is methylglycinediacetate.7. The process according to any one of to claim 4 , wherein the alkali metal hydroxide selected is sodium hydroxide.8. The process according to any one of to claim 4 , wherein the precursor of the catalyst is prepared by precipitation claim 4 , starting from one or more water-soluble copper salts and one or more water-soluble zirconium salts.9. The process according to claim 8 , wherein the pH at the end of the precipitation of the precursor of the catalyst is in the range from 8 to 14.11. A process for producing a catalyst claim 8 , comprising the following steps(a) provision of an acidic aqueous solution of at least one copper salt and at least one zirconium salt,(b) precipitation of a precursor by increasing the pH, where the pH at the end of the precipitation is in the range from 8 to 12,(c) reduction of the precursor.14. A process for producing a precursor of a catalyst according to or claim 8 , comprising the following steps:(a) provision of an acidic aqueous solution of at least one copper salt and at least one zirconium salt,(b) precipitation of a precursor by increasing the pH, ...

Подробнее
27-06-2013 дата публикации

HOMO- AND HETERO-POLYAMINO-ACID DERIVATIVES OF FULLERENE C60, METHOD FOR PRODUCING SAME, AND PHARMACEUTICAL COMPOSITIONS BASED ON SAID DERIVATIVES

Номер: US20130165691A1
Принадлежит:

The invention relates to the pharmaceutical industry and to medicine, specifically to novel homo- and hetero-polyamino-acid derivatives of fullerene Cof general formula: C(H){NH(CH)COO—}{NH(L)COOH)}, where n=2-5, x=3, L=—(CH), where m=1-5, or —CO(CH)CH(NH)—, where k=1-2, characterized in that the compounds comprise covalently bonded amino-acid groups and polar ionic forms of the amino acids, and also to a method for producing said derivatives, and to the production of pharmaceutical compositions based on same. The method for producing homo- and hetero-polyamino-acid derivatives of fullerene is based on the reaction of a nucleophilic bond of amino acids to fullerene, forming covalently bonded amino-acid derivatives of fullerene, with the subsequent introduction of polar ionic forms of the amino acids. A pharmaceutical composition comprises, as active substance, homo- and hetero-polyamino-acid derivatives of fullerene of formula 1. Homo- and heteropoly(amino acid) derivatives of fullerene of general formula C(H){NH(CH)COO—}{NH(L)COOH)} , wherein n=2-5 , x=3 , L=—(CH) , wherein m=1-5 , or —CO(CH)CH(NH)— , wherein k=1-2 , characterized in that the compounds comprise covalently bonded amino acid groups and polar ionic forms of amino acids.2. Fullerene derivatives according to claim 1 , characterized in that the amino acid groups are moieties of aliphatic amino acids of general formula NH(CH)COOH claim 1 , wherein n=2-5.3. Fullerene derivatives according to claim 1 , characterized in that the polar ionic forms of amino acids are moieties of dicaboxylic amino acid amides of general formula NH(CO)(CH)CH(NH)COOH claim 1 , wherein k=1-2.4. A method for producing the fullerene derivatives according to claim 1 , characterized in that the fullerene derivatives are produced by reacting fullerene with a tenfold molar excess of anhydrous potassium salts of amino acids of general formula NH(CH)COOK claim 1 , wherein n=2-5 claim 1 , in an aromatic organic solvent medium claim 1 , ...

Подробнее
27-06-2013 дата публикации

HYDRATED N-FULLERENE AMINO ACIDS, METHOD FOR PRODUCING THE LATTER, AND PHARMACEUTICAL COMPOSITIONS ON THE BASIS THEREOF

Номер: US20130165692A1
Принадлежит:

The invention relates to the pharmaceutical industry and to medicine, specifically to novel hydrated amino-acid derivatives of fullerene Cof general formula C(H){NH(CH)COOH}.xHO, where C-fullerene, n=5, 6, 7, x=8-10, and also to a method for producing said derivatives, and to the production of pharmaceutical compositions on the basis thereof. Hydrated N-fullerene amino acids are formed in the interaction of fullerene with 15 times the molar excess of anhydrous potassium salts of amino acids in a medium of organic aromatic solvent with slow addition to the resultant suspension of an interphase catalyst and with mixing and heating to a temperature not exceeding 60° C. until the solution is completely decolorized and a solid residue formed, after which the latter is separated out, and then 0.8 M of aqueous solutions of potassium salts of fullerene amino-acid derivatives is treated with a solution of organic or mineral acids, followed by centrifugation, rinsing and drying of the residue. A pharmaceutical composition which exhibits activity against the herpes virus, flu viruses of various origin and HIV, and also anti-tumor and anti-psoriatic activity, comprising, as active substance, an effective quantity of hydrated N-fullerene amino acids. 1. Hydrated N-fullerene amino acids of general formula C(H){NH(CH)COOH}xHO , wherein Cis fullerene; n=5 , 6 , or 7; and x=8 to 10.2. A method for producing the compound according to claim 1 , characterized in that the fullerene is reacted with a 15-fold molar excess of anhydrous potassium salts of amino acids of general formula NH(CH)COOH claim 1 , wherein n=5 claim 1 , 6 claim 1 , or 7 claim 1 , in an aromatic solvent medium claim 1 , comprising a slow addition to the resulting suspension of a phase-transfer catalyst under stirring and heating to a temperature not higher than 60 to 80° C. until the solution is completely decolorized and a solid residue is formed claim 1 , wherein said residue represents potassium salts of the ...

Подробнее
27-06-2013 дата публикации

PROCESS FOR PREPARING 4-AMINO-5-HEXENOIC ACID AND INTERMEDIATES THEREOF

Номер: US20130165693A1
Принадлежит: TARGEON

The present invention relates to a new and competitive process for the preparation of 4-amino-5-hexenoic acid and intermediates thereof. The compound, and compositions containing the compound as an active ingredient, can be used for the treatment and/or prophylaxis of epilepsy and West syndrome. 1. A process for producing 4-amino-5-hexenoic acid using succinimide as raw material , characterized in that it comprises at least a first step a) consisting of reducing said succinimide with a hydride donor in an alcoholic solvent in presence of a protic acid to produce a 5-alkoxy-2-pyrrolidone intermediate.2. A process according to which further comprises the following steps:b) reacting said 5-alkoxy-2-pyrrolidone intermediate with at least 2 equivalents of a vinyl magnesium halide reagent (vinyl Grignard reagent) in a suitable solvent, to form 5-vinyl-2-pyrrolidone; andc) hydrolyzing said 5-vinyl-2-pyrrolidone to form 4-amino-5-hexenoic acid.3. A process according to claim 2 , where the vinyl magnesium halide reagent of step b) is present in the amount of 2 to 3 molar equivalents.4. A process according to claim 2 , where the vinyl magnesium halide reagent of step b) is present in the amount of 2 to 2.5 molar equivalents.5. A process according to claim 2 , wherein steps a) and b) are being undertaken without isolation of the 5-alkoxy-2-pyrrolidone intermediate.6. A process according to claim 2 , wherein steps a) claim 2 , b) and c) are being undertaken without isolation of the 5-alkoxy-2-pyrrolidone or 5-vinyl-2-pyrrolidone intermediates.7. A process according to claim 1 , which further comprises the following steps:b) submitting said 5-alkoxy-2-pyrrolidone intermediate to i) one equivalent of a basic reagent in a suitable solvent, and ii) at least one equivalent of a vinyl magnesium halide reagent (vinyl Grignard reagent), to form 5-vinyl-2-pyrrolidone, the two steps being undertaken in the same reaction vessel, andc) hydrolyzing said 5-vinyl-2-pyrrolidone to 4-amino-5- ...

Подробнее
04-07-2013 дата публикации

PLANT ACTIVATOR

Номер: US20130172189A1
Принадлежит:

A compound useful as a plant activator for activating an endogenous defense system of a plant to control disease damage is provided. A compound represented by the formula: (R)NH—(CH)—N(R)—(CH)—NH(R) (one of Rand Rrepresents a linear Calkanoyl group or alkenoyl group, the other represents hydrogen atom or a protective group of amino group; and Rrepresents hydrogen atom or a protective group of amino group). 1. A compound represented by the following general formula (I): (R)NH—(CH)—N(R)—(CH)—NH(R) (In the formula , one of Rand Rrepresents a linear alkanoyl group having 6 to 18 carbon atoms or a linear alkenoyl group having 6 to 18 carbon atoms (the linear alkanoyl group and the linear alkenoyl group may have 1 to 3 hydroxyl groups , and/or 1 to 3 alkyl groups having 1 to 4 carbon atoms) , the other represents hydrogen atom or a protective group of amino group; and Rrepresents hydrogen atom or a protective group of amino group) , or a salt thereof.2. The compound or a salt thereof according to claim 1 , wherein one of Rand Ris a linear alkanoyl group having 8 to 13 carbon atoms or a linear alkenoyl group having 8 to 13 carbon atoms (the linear alkanoyl group and the linear alkenoyl group may have 1 to 3 hydroxyl groups) claim 1 , the other is hydrogen atom or a protective group of amino group claim 1 , and Ris hydrogen atom or a protective group of amino group.3. The compound or a salt thereof according to claim 1 , wherein one Rand Ris a linear alkanoyl group having 8 to 13 carbon atoms (the linear alkanoyl group may have 1 to 3 hydroxyl groups) claim 1 , the other is hydrogen atom or a protective group of amino group claim 1 , and Ris hydrogen atom or a protective group of amino group.4. The compound or a salt thereof according to claim 1 , wherein the linear alkanoyl group is a linear alkanoyl group having 9 to 12 carbon atoms (the linear alkanoyl group may have 1 or 2 hydroxyl groups).5. The compound or a salt thereof according to claim 1 , wherein the linear ...

Подробнее
11-07-2013 дата публикации

PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF

Номер: US20130178644A1
Принадлежит: EUTICALS S.P.A.

The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process. 130-. (canceled)32. The process according to claim 31 , wherein the halide is bromide and the metal is zinc or magnesium.33. The process according to claim 31 , wherein the ethyl metal halide is ethylmagnesium bromide.34. The process according to claim 32 , wherein the ethyl metal halide is used in a quantity between 1 and 5 equivalents with respect to compound (VIII).35. The process according to claim 31 , wherein the alkylation is carried out at a temperature between 0° C. and the boiling temperature of the solvent.36. The process according to claim 35 , wherein the alkylation is carried out at a temperature between 10 and 30° C.38. The process according to claim 37 , wherein the chiral acid is selected from D(−) mandelic acid claim 37 , D(−) 2-chloromandelic acid claim 37 , D(−) tartaric acid claim 37 , and (2R claim 37 ,3R)-O claim 37 ,O′-dibenzoyl tartaric acid.39. The process according to claim 38 , wherein the chiral acid is D(−) mandelic acid.40. The process according to claim 37 , wherein the polar solvent of step a′) is selected from: water claim 37 , aliphatic ketones and/or aliphatic alcohols claim 37 , used ...

Подробнее
25-07-2013 дата публикации

Dietary Supplement For Vascular Health

Номер: US20130189297A1

The present invention relates to an herbal dietary supplement to promote vascular health. The dietary supplement comprises L-Arginine, L-Citrulline, Ginkgo Biloba, Horse chestnut, Red Yeast Rice and Cayanne Pepper.

Подробнее
25-07-2013 дата публикации

Biotinylated polysaccharides having an antithrombotic activity and improved metabolic stability

Номер: US20130190268A1
Принадлежит: SANOFI SA

The invention relates to novel polysaccharides with an antithrombotic activity, having at least one covalent bond with biotin or a biotin derivative, wherein said covalent bond is resistant to metabolic cleavage and comprises a linkage X selected from the group consisting of —O—, —N(R)—, —N(R)—CO— and —N(R′)—CO—N(R″)—, wherein R is an alkyl group and R′ and R″, which may be identical or different, are, independently of one another, a hydrogen atom or alkyl group.

Подробнее
25-07-2013 дата публикации

CRYSTALLINE FORMS OF 4-[2-(4-METHYLPHENYLSULFANYL)-PHENYL] PIPERIDINE WITH COMBINED SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITION FOR THE TREATMENT OF NEUROPATHIC PAIN

Номер: US20130190352A1
Принадлежит: H. Lundbeck A/S

Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain. 2. The compound according to claim 1 , which compound is the HBr addition salt.34-. (canceled)5. The compound according to claim 1 , which compound is the DL-lactic acid addition salt.67-. (canceled)8. The compound according to claim 1 , which compound is the glutaric acid addition salt (1:1).910-. (canceled)11. The compound according to claim 1 , which compound is the malonic acid addition salt (1:1).12. The compound according to claim 11 , which compound is characterized by peaks in an XRPD at 10.77° claim 11 , 16.70° claim 11 , 19.93° and 24.01°2θ claim 11 , or at 6.08° claim 11 , 10.11° claim 11 , 18.25° and 20.26°2θ.1310. The compound according to claim 11 , which compound is characterised by an XRPD as depicted in or .14. The compound according to which compound is L-aspartic acid addition salt (1:1) or L-aspartic acid addition salt hydrate (1:1).15. The compound according to which compound is glutamic acid addition salt (1:1) or glutamic acid addition salt monohydrate.16. (canceled)17. A pharmaceutical composition comprising a compound according to together with a pharmaceutically acceptable excipient.18. A method of treating a disease selected from chronic pain claim 1 , depression in partial responders claim 1 , treatment resistant depression claim 1 , Alzheimer's disease claim 1 , cognitive impairment claim 1 , ADHD claim 1 , melancholia claim 1 , PTSD claim 1 , hot flushes claim 1 , sleep apnea claim 1 , alcohol claim 1 , nicotine or carbohydrate craving claim 1 , substance abuse claim 1 , alcohol or drug abuse claim 1 , emesis claim 1 , eating disorders claim 1 , IBS claim 1 , affective disorders claim 1 , depression claim 1 , major depressive disorder claim 1 , postnatal depression claim 1 , depression associated with bipolar disorder claim 1 , Alzheimer's disease claim 1 , psychosis or Parkinson's disease claim ...

Подробнее
25-07-2013 дата публикации

PROCESS TO PREPARE 6-CHLORO-3-AMINO-2-(2-HYDROXYPROPYL)-1-AZANAPHTHALENE

Номер: US20130190500A1
Принадлежит: Neuron Systems, Inc.

This invention relates to a process for the preparation of 6-chloro-3-amino-2-(2-hydroxypropyl)-1-azanapthalene. It comprises treating 6-chloro-3-pyridylium-2-ethoxycarbonyl-1-azanaphthanlene bromide with morpholine at about 80° C., followed by treating the product thereof with methylmagnesium chloride. 1. A process for the preparation of 6-chloro-3-amino-2-ethoxycarbonyl-1-azanaphthalene comprising treating 6-chloro-3-pyridylium-2-ethoxycarbonyl-1-azanaphthanlene bromide with morpholine at about 80° C.2. The process of further comprising treating ethyl pyridyliumpyruvate halide with 2-amino-5-chloro-benzaldehyde and pyridine at 80° C. under an inert atmosphere to yield 6-chloro-3-pyridylium-2-ethoxycarbonyl-1-azanapthalene halide.3. A process for the preparation of 6-chloro-3-amino-2-(2-hydroxypropyl)-1-azanapthalene comprising the process of followed by treating the product thereof with methylmagnesium chloride.4. A process for the preparation of 2-amino-5-chloro-benzalehyde comprising treating 5-chloro-2-nitrobenzaldehyde with hydrogen and 3% sulfided platinum. This application claims benefit of U.S. Provisional Application Ser. No. 61/569,358, filed on Dec. 12, 2011. The contents of the prior application are incorporated herein by reference.Compound A (6-chloro-3-amino-2-(2-hydroxypropyl)-1-azanaphthalene) is in early stage clinical trials for the treatment of macular degeneration.Although compound A can be readily prepared by those skilled in the art, more efficient synthetic routes are necessary for the production on a commercial scale. A highly efficient route to compound A is disclosed herein.This invention relates to a process for the preparation of 6-chloro-3-amino-2-ethoxycarbonyl-1-azanaphthalene, which comprises treating 6-chloro-3-pyridylium-2-ethoxycarbonyl-1-azanaphthanlene bromide with morpholine at about 80° C. This process may further comprise treating ethyl pyridyliumpyruvate halide with 2-amino-5-chloro-benzaldehyde and pyridine at 80° C. under ...

Подробнее
25-07-2013 дата публикации

PROCESSES FOR THE SYNTHESIS OF DIARYLTHIOHYDANTOIN AND DIARYLHYDANTOIN COMPOUNDS

Номер: US20130190507A1
Принадлежит:

Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer. 3. The process of claim 1 , wherein X is S.4. The process of claim 1 , wherein Yand Yare both methyl.5. The process of claim 1 , wherein Yand Ytogether with the carbon to which they are attached combine to form a cyclobutyl ring or a cyclopentyl ring.6. The process of claim 1 , wherein Lis a single bond.7. The process of claim 1 , wherein Ris —C(═O)—NHCH.8. The process of claim 1 , wherein Ris —C(═O)—NH.9. The process of claim 1 , wherein Ris F.10. The process of claim 1 , wherein Yand Yare both methyl claim 1 , Ris —C(═O)—NHCH claim 1 , and Ris F.11. The process of claim 1 , wherein Yand Yare both methyl claim 1 , Ris —C(═O)—NH claim 1 , and Ris F.13. The process of claim 12 , wherein X is S.1412. The process of claim 12 , wherein Yand Yare both methyl claim 12 , Ris —C(═O)—OH claim 12 , and Ris F. This patent application is a continuation of Ser. No. 13/580,718 filed Aug. 23, 2012 as a national phase application of PCT/US2011/026135 filed on Feb. 24, 2011, which claims priority to Ser. No. 61/307,796, filed Feb. 24, 2010. Each of these applications is incorporated herein by reference in its entirety.Not applicable.The invention is in the field of cancer therapeutics, such as processes for the synthesis of prostate cancer therapeutics.According to the American Cancer Society, prostate cancer is the most commonly diagnosed cancer among men in the United States, other than skin cancer. The American Cancer Society estimates that approximately 186,000 new cases of prostate cancer were diagnosed, and approximately 29,000 men died of prostate cancer in the United States alone during 2008. Prostate cancer is thus the second-leading cause of cancer death in men in the United States, after lung cancer. ...

Подробнее
25-07-2013 дата публикации

Fluorine Radiolabelling Process

Номер: US20130190529A1
Принадлежит:

The invention relates to a process for producing a process for producing an F-labelled compound, the process comprising treating a compound of formula (I) 4. A process according to wherein said rearomatisation is performed in situ.5. A process according to wherein said rearomatisation comprises the addition of a reagent which effects cleavage of Xfrom the carbon atom of the ring which is para to EDG′ in the compound of formula (IIa) claim 3 , to produce a compound of formula (II) claim 3 , wherein said reagent is an acid claim 3 , base or oxidising agent.613.-. (canceled)1517.-. (canceled)2021.-. (canceled)28. A process according to which further comprises a deprotection step comprising substituting H for said amino protecting group R claim 27 , thereby converting the group —NHRin the compound of formula (IIc″″) or (IId″″) into a —NHgroup.3233.-. (canceled)34. A process according to wherein said rearomatisation is performed in situ.35. A process according to wherein said rearomatisation comprises the addition of a reagent which effects cleavage of Xfrom the carbon atom of the ring which is para to EDG′ in the compound of formula (IIc) or formula (IId) claim 23 , wherein said reagent is an acid claim 23 , base or oxidising agent.3645.-. (canceled)47. A process according to wherein said deprotection step is performed in situ.4851.-. (canceled)52. A process according to wherein the step of treating the compound of formula (I) with [F]fluoride comprises treating the compound of formula (I) with a compound comprising F and a counter cation claim 1 , wherein the counter cation is a quaternary ammonium cation claim 1 , an alkali metal or H.5362.-. (canceled)63. A process according to wherein the oxidant is a hypervalent iodonium (III) reagent or a metal oxide.6466.-. (canceled)67. A process according to wherein the step of treating the compound of formula (I) with [F]fluoride is performed in the presence of an additive claim 1 , wherein the additive is an acid or a crown ...

Подробнее
01-08-2013 дата публикации

Short synthesis of tolterodine, intermediates and metabolites

Номер: US20130197082A1
Автор: Damjan Sterk
Принадлежит: Lek Pharmaceuticals dd

A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.

Подробнее
01-08-2013 дата публикации

ANTIPROLIFERATIVE COMPOUNDS, CONJUGATES THEREOF, METHODS THEREFOR, AND USES THEREOF

Номер: US20130197259A1
Принадлежит: Medarex, Inc.

Antiproliferative compounds having a structure represented by formula (II), where n, R, R, R, R, and Rare as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody: 2. A compound according to claim 1 , wherein Ris H or C-Calkyl.3. A compound according to claim 2 , wherein Ris Me.4. A compound according to claim 1 , wherein Ris H claim 1 , Boc (t-butoxycarbonyl) claim 1 , Troc (2 claim 1 ,2 claim 1 ,2-trichloroethoxy carbonyl) claim 1 , Bpoc ((1-methyl-1-(4-biphenyl)ethoxycarbonyl)) claim 1 , Cbz (benzyloxy carbonyl) claim 1 , Aloc (allyloxycarbonyl) claim 1 , methyl amine claim 1 , or Fmoc (9-fluorenylmethoxycarbonyl).5. A compound according to claim 4 , wherein Ris H or C-Calkyl.6. A compound according to claim 5 , wherein Ris Me. This application is a divisional of application Ser. No. 12/846,493, filed Jul. 29, 2010, now allowed; which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Applications Nos. 61/230,932, filed Aug. 3, 2009; and 61/232,883, filed Aug. 11, 2009; the disclosures of which are incorporated herein by reference.This invention relates to compounds structurally related to the tubulysins, conjugates thereof with a ligand, methods for making and using such compounds and conjugates, and compositions comprising such compounds and conjugates.The tubulysins are cytotoxins originally isolated from cultures of the myxobacteria or , with each organism producing a different mixture of tubulysins (Sasse et al. 2000; Reichenbach et al. 1998). Their crystal structure and biosynthetic pathway have been elucidated (Steinmetz et al. 2004) and their biosynthesis genes have been sequenced (Hoefle et al. 2006b). Pretubulysin, a biosynthetic precursor of the tubulysins, also has been shown to possess significant activity in its own right (Ullrich et al. 2009). (Full citations for the documents cited herein by first author or inventor and year are listed at the end of this specification.)The tubulysins ...

Подробнее
08-08-2013 дата публикации

ANTIPROLIFERATIVE COMPOUNDS, CONJUGATES THEREOF, METHODS THEREFOR, AND USES THEREOF

Номер: US20130204033A1
Принадлежит: Medarex, Inc.

Antiproliferative compounds having a structure represented by formula (II), where n, R, R, R, R, and Rare as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody: 2. A compound according to claim 1 , wherein Rand Rare independently selected from H claim 1 , Boc claim 1 , Troc claim 1 , Bpoc claim 1 , Cbz claim 1 , Aloc claim 1 , methylamine claim 1 , and Fmoc.3. A compound according to claim 2 , wherein Ris H or C-Calkyl.4. A compound according to claim 3 , wherein Ris Me.5. A compound according to claim 1 , wherein Ris H or C-Calkyl.6. A compound according to claim 5 , wherein Ris Me.7. A compound according to claim 1 , wherein Rand Rare different amine protecting groups.8. A compound according to claim 7 , wherein Ris H or C-Calkyl.9. A compound according to claim 8 , wherein Ris Me. This application is a divisional of application Ser. No. 12/846,493, filed Jul. 29, 2010, now allowed; which claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Applications Nos. 61/230,932, filed Aug. 3, 2009; and 61/232,883, filed Aug. 11, 2009; the disclosures of which are incorporated herein by reference.This invention relates to compounds structurally related to the tubulysins, conjugates thereof with a ligand, methods for making and using such compounds and conjugates, and compositions comprising such compounds and conjugates.The tubulysins are cytotoxins originally isolated from cultures of the myxobacteria or , with each organism producing a different mixture of tubulysins (Sasse et al. 2000; Reichenbach et al. 1998). Their crystal structure and biosynthetic pathway have been elucidated (Steinmetz et al. 2004) and their biosynthesis genes have been sequenced (Hoefle et al. 2006b). Pretubulysin, a biosynthetic precursor of the tubulysins, also has been shown to possess significant activity in its own right (Ullrich et al. 2009). (Full citations for the documents cited herein by first author or inventor and year are ...

Подробнее
08-08-2013 дата публикации

PROCESS FOR THE PREPARATION OF A MIXTURE OF CHELATING AGENTS

Номер: US20130204035A1
Принадлежит: KEMIRA OYJ

The present invention relates to a process for the preparation of a mixture of aspartic acid diethoxy succinate and an amino acid derivative of the general formula (I) wherein n is 1-10, m is 0 or 1, and R is hydrogen or an alkali metal or alkaline earth metal ion, comprising reacting maleate with diethanol amine under alkaline conditions in the presence of a lanthanoid catalyst to form aspartic acid diethoxy succinate followed by adding aspartic acid which reacts with unreacted maleate to form imino disuccinic acid, i.e. an amino acid derivative of formula (I) wherein m is 0, or by adding a diamine derivative of the general formula (II) NH2(CH2)nNH2 wherein n is as defined above, which reacts with unreacted maleate to form an amino acid derivative of formula (I) wherein m is 1 and n is as defined above. 2. The process according to wherein the amount of the diethanol amine is substoichiometric in relationship to the amount of the maleate.3. The process according to wherein the molar ratio of diethanol amine to maleate is between 1:3.1 and 1:5 claim 2 , preferably between 1:3.5 and 1:4.4. The process according to wherein maleate and diethanol amine are reacted for a period of time for converting at least 30 mole % of diethanol amine into aspartic acid diethoxy succinate.5. The process according to wherein the molar ratio of the lanthanoid catalyst to maleate is between 1:2.5 to 1:5 claim 1 , preferably between 1:3 and 1:4.6. The process according to wherein lanthanoid catalyst is a lanthanum catalyst including lanthanum(III)oxide and lanthanum(III)salts claim 1 , such as lanthanum carbonate claim 1 , lanthanum maleate claim 1 , lanthanum nitrate claim 1 , lanthanum chloride or lanthanum octanoate.7. The process according to wherein the alkaline conditions are obtained by dissolving maleic anhydride in water and adding an alkali metal compound or alkaline earth metal compound claim 1 , such as an alkali metal hydroxide or carbonate or an alkaline earth metal hydroxide ...

Подробнее
15-08-2013 дата публикации

ANTI-INFECTIVE AND IMMUNOMODULATORY COMPOUNDS

Номер: US20130209515A1
Принадлежит:

The present invention provides pharmaceutical compositions and methods that include the use of anti-infective compounds that potentiate the host-immune response or limit or prevent the expression or activity of individual virulence factors. In addition, the compositions have immunomodulatory activity, and therefore can be used to prime host defenses to prevent or limit bacterial, fungal, and viral viability. In the compositions and methods of the inventions, specific steps of the bacterial-, fungal-, or viral-host interaction are targeted to prevent pathogenesis (e.g., infection). Such an approach should prevent pathogenic organisms from acquiring resistance to the protective anti-infective compounds. 114-. (canceled)16. The method of claim 15 , wherein said compound is 2′-aminoacetophenone.17. The method of claim 15 , wherein said compound is 2′-amino-3-hydroxyacetophenone.18. The method of claim 15 , wherein said disease is a bacterial infection claim 15 , a viral infection claim 15 , an autoimmune disease claim 15 , an allergic condition claim 15 , or cancer.19. The method of claim 18 , wherein said bacterial infection is the result of a Gram-negative bacterium.20Vibrio harveyi, Vibrio cholerae, Vibrio parahaemolyticus, Vibrio alginolyticus, Pseudomonas phosphoreum, Pseudomonas aeruginosa Yersinia enterocolitica, Escherichia coli, Salmonella typhimurium, Haemophilus influenzae, Helicobacter pylori, Bacillus subtilis, Borrelia burgfdorferi, Neisseria meningitidis, Neisseria gonorrhoeae, Yersinia pestis, Campylobacter jejuni, Deinococcus radiodurans, Mycobacterium tuberculosis, Enterococcus faecalis, Streptococcus pneumoniae, Streptococcus pyogenesStaphylococcus aureus.. The method of claim 18 , wherein said bacterial infection is the result of claim 18 , or22. The method of claim 21 , wherein said disease is the result of a bacterial infection claim 21 , fungal infection claim 21 , or viral infection.23. The method of claim 22 , wherein said bacterial infection is ...

Подробнее
15-08-2013 дата публикации

Differentiation of pluripotent cells

Номер: US20130210141A1
Принадлежит: Fujifilm Cellular Dynamics Inc

Provided herein are methods for the in vitro maintenance, expansion, culture, and/or differentiation of pluripotent cells, such as human embryonic stem cells (hESC) or induced pluripotent cells (iPSC), into hematopoietic precursor cells or endothelial cells. The pluripotent cells may be maintained and differentiated under defined conditions; thus, the use of mouse feeder cells or serum is not required in certain embodiments for the differentiation of the pluripotent cells into hematopoietic precursor cells or endothelial cells. The resulting hematopoietic precursor cells may be further differentiated into various myeloid or lymphoid lineages.

Подробнее
15-08-2013 дата публикации

NEW SALT OF A PYRIMIDIN DERIVATIVE

Номер: US20130210848A1
Принадлежит: LABORATORIOS SENOSIAIN S.A. DE C.V.

The present invention relates to a salt of a pyrimidin derivative of the acid (3R,5S,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic, to a method for preparing same and to the use thereof in formulating pharmaceutical formulations. 19-. (canceled)10. (3R ,5S ,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl) pyrimidin-5-yl]-3 ,5-dihydroxihept-6-enoic amino acid salt , wherein the amino acid is lysine and wherein the bond formed between these two entities is a non-covalent bond.11. (3R ,5 S ,6E)-7-[4-(4-fluorophenyl)-2-(N-methylmethanesulfonamide)-6-(propan-2-yl)pyrimidin-5-yl]-3 ,5-dihydroxihept-6-enoic amino acid salt , wherein the amino acid is histidine and wherein the bond formed between these two entities in a non-covalent bond.12. A pharmaceutical composition comprising the salt of claim 10 , in combination with a pharmaceutically acceptable carrier.13. A pharmaceutical composition comprising the salt of claim 11 , in combination with a pharmaceutically acceptable carrier.14. A method of manufacturing a pharmaceutical composition comprising the step of adding the salt of to a pharmaceutically acceptable carrier.15. A method of manufacturing a pharmaceutical composition comprising the step of adding the salt of to a pharmaceutically acceptable carrier.16. The method according to claim 14 , wherein the pharmaceutical compositions are in the form of tablets or capsules.17. A method of manufacturing medicaments for the prevention or treatment of cardiovascular diseases comprising the step of adding the compound of to a pharmaceutically acceptable carrier.18. A process for synthesizing a rosuvastatin-lysine salt claim 10 , comprising the steps:a) subjecting the rosuvastatin calcium salt to a dissociation process; andb) mixing the acid rosuvastatin resulting from the previous step with an aqueous solution containing lysine for forming the salt in the presence of a methanol/ethyl ...

Подробнее
15-08-2013 дата публикации

Synthesis of Cyclopentaquinazolines

Номер: US20130211082A1
Принадлежит: ONYX Pharmaceuticals, Inc.

A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N-{N-{4-[N-((6S)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]benzoyl}-L-γ-glutamyl}-D-glutamic acid (ONX-0801). 1. A process for producing a cyclopentaquinazoline from a 5-amino-6-haloindanone comprising the steps of:(a) acylation of the 5-amino group;(b) cyanide displacement of the 6-halo group;(c) hydrolysis of the nitrile group produced in step (b); and(d) cyclisation of a 5-(N-acylamino)-6-amidoindanone to form a cyclopentaquinazoline ring system.2. A process according to claim 1 , wherein (a) acylation of the 5-amino group comprises reaction of a 5-aminoindanone compound with an acylating agent.3. A process according to wherein the acylating agent is generated in situ by reaction of a carboxylic acid with a coupling agent.4. A process according to wherein the carboxylic acid is a carboxylic acid of formula RCOH claim 3 , wherein R is selected from Ror a protected form thereof claim 3 , and wherein Ris independently selected from hydrogen claim 3 , amino claim 3 , Calkyl claim 3 , Calkoxy claim 3 , fluoroCalkyl claim 3 , hydroxyCalkyl claim 3 , or protected hydroxyCalkyl.5. A process according to claim 3 , wherein the acylating agent is a mixed phosphoric anhydride generated in situ by reaction of the carboxylic acid with a chlorophosphate ester.6. A process according to claim 1 , wherein (b) cyanide displacement of the 6-halo group comprises displacement of the 6-halo group with a cyanide nucleophile selected from zinc cyanide claim 1 , potassium cyanide claim 1 , sodium cyanide claim 1 , and cuprous cyanide claim 1 , optionally in the presence of a catalyst.7. A process according to claim 6 , wherein the catalyst is a palladium or nickel catalyst claim 6 , complexed to a triarylphosphine or bidentate bisphosphine ligand.8. A process according ...

Подробнее
15-08-2013 дата публикации

METHODS OF MAKING L-ORNITHINE PHENYL ACETATE

Номер: US20130211135A1
Принадлежит: OCERA THERAPEUTICS, INC.

Disclosed herein are processes for making L-ornithine phenyl acetate. The process may include, for example, inter-mixing a halide salt of L-ornithine with silver phenyl acetate. The process may also include forming a phenyl acetate salt in situ. The present application also relates to various compositions obtained from these processes, including crystalline forms. 1. A process for making L-ornithine phenyl acetate salt comprising:preparing a solution of phenyl acetate salt by mixing a phenyl acetic acid and a base in a solvent;intermixing L-ornithine benzoate with the solution of phenyl acetate salt; andisolating a composition comprising L-ornithine phenyl acetate.2. The process of claim 1 , further comprising forming L-ornithine benzoate claim 1 , wherein forming L-ornithine benzoate comprises intermixing an L-ornithine salt claim 1 , a benzoate salt and a first solvent to form an intermediate solution.3. The process of claim 2 , further comprising removing at least a portion of a salt from said intermediate solution before intermixing with the phenyl acetate salt claim 2 , wherein said removed salt is not an L-ornithine salt.4. The process of claim 3 , wherein said removed salt comprises an anion derived at least in part from the L-ornithine salt and a cation derived at least in part from the benzoate salt.5. The process of claim 4 , wherein the L-ornithine salt is L-ornithine hydrochloride and said anion is chloride.6. The process of claim 4 , wherein the benzoate salt is silver benzoate and the cation is a silver ion.7. The process of claim 3 , wherein the process further comprises adding hydrochloric acid before said removing at least a portion of the salt.8. The process of claim 3 , wherein at least about 90% by weight of said removed salt is removed.9. The process of claim 1 , further comprising forming L-ornithine benzoate claim 1 , wherein forming L-ornithine benzoate comprises:intermixing an L-ornithine salt, a benzoate salt and a first solvent to form an ...

Подробнее
22-08-2013 дата публикации

Omega 3 fatty acid formulations

Номер: US20130213851A1
Принадлежит: CENESTRA LLC

The present invention provides highly purified omega-3 fatty acid formulations. Certain formulations provided herein have greater than 85% omega-3 fatty acids by weight. Certain other formulations provided herein contain EPA and DHA in a ratio of from about 4.01:1 to about 5:1. The invention also provides methods of using the dosage forms to treat a variety of cardiovascular, autoimmune, inflammatory, and central nervous system disorders by administering a formulation of the invention to a patient in need thereof.

Подробнее
22-08-2013 дата публикации

Purification and isolation of recombinant oxalate degrading enzymes and spray-dried particles containing oxalate degrading enzymes

Номер: US20130216515A1
Принадлежит: OXTHERA INTELLECTUAL PROPERTY AB

The present invention comprises methods and compositions for the reduction of oxalate in humans, and methods for the purification and isolation of recombinant oxalate reducing enzyme proteins. The invention provides methods and compositions for the delivery of oxalate-reducing enzymes in particle compositions. The compositions of the present invention are suitable in methods of treatment or prevention of oxalate-related conditions.

Подробнее
22-08-2013 дата публикации

PHENOXY DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS

Номер: US20130217651A1
Принадлежит: ALLERGAN, INC.

The present invention relates to novel phenoxy derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to wherein Lis CH.3. A compound according to wherein Lis CH.4. A compound according to wherein a is 1 claim 1 , 2 or 3.8. A compound according to selected from:3-[(4-{[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]oxy}benzyl)amino]propanoic acid;3-({4-[3-(3-chlorophenyl)-4-(3,4-dimethylphenyl)butoxy]benzyl}amino)propanoic acid;{3-[(4-{[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]oxy}benzyl)amino]propyl}phosphonic acid;[3-({4-[3-(3-chlorophenyl)-4-(3,4-dimethylphenyl)butoxy]benzyl}amino) propyl]phosphonic acid;3-[(4-{[4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)amino]propanoic acid;3-[(4-{[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)amino]propanoic acid;{3-[(4-{[4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)amino]propyl}phosphonic acid;{3-[(4-{[4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)amino]propyl}phosphonic acid;3-[(4-{[5-(3,4-dimethylphenyl)-4-(3-thienyl)pentyl]oxy}benzyl)amino]propanoic acid;3-[(4-{[5-(3,4-dimethylphenyl)-4-(3-thienyl)pentyl]oxy}benzyl)amino]propyl}phosphonic acid; and3-[(4-{[4-(2,3-difluorophenyl)-5-(3,4-dimethylphenyl)pentyl]oxy}benzyl)amino]propanoic acid.9. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.10. A pharmaceutical composition according to wherein the compound is selected from:3-[(4-{[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]oxy}benzyl)amino]propanoic acid;3-({4-[3-(3-chlorophenyl)-4-(3,4-dimethylphenyl)butoxy]benzyl}amino)propanoic acid;{3-[(4-{[5-(3-chlorophenyl)-6-(3,4-dimethylphenyl)hexyl]oxy}benzyl)amino]propyl}phosphonic acid;[3-({4-[3-(3-chlorophenyl)-4-(3,4- ...

Подробнее
22-08-2013 дата публикации

Sulfinylbenzyl and thiobenzyl derivatives as sphingosine 1-phosphate (s1p) receptor modulators

Номер: US20130217652A1
Принадлежит: Allergan Inc

The present invention relates to novel thiobenzyl and sulfinylbenzyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Подробнее
22-08-2013 дата публикации

METHOD FOR PRODUCING 3,4-DISUBSTITUTED PYRROLIDINE DERIVATIVE

Номер: US20130217893A1
Принадлежит: Kyorin Pharmaceutical Co., Ltd.

The present invention provides an inexpensive and industrially advantageous method for producing an optically active form of an anti-(3S,4R)-3-alkylcarbamoyl-4-hydroxypyrrolidine derivative or it's enantiomer, which is a key intermediate for producing a high-quality optically active form of (3R,4S)-3-alkylaminomethyl-4-fluoropyrrolidine or it's enantiomer useful as an intermediate for producing pharmaceuticals. 4. The production method according to claim 1 , wherein the optically active catalyst in Step A is an optically active ruthenium catalyst having a chiral ligand.5. The production method according to claim 1 , wherein in Step A claim 1 , the chiral ligand in the optically active catalyst is an optically active 2 claim 1 ,2′-bis(diphenylphosphino)-1 claim 1 ,1′-binaphthyl (BINAP) or it's analogue claim 1 , 5 claim 1 ,5′-bis(diphenylphosphino)-4 claim 1 ,4′-bi-1 claim 1 ,3-benzodioxole (SEGPHOS) or it's analogue claim 1 , or (2 claim 1 ,2′-bisdiphenylphosphino)-6 claim 1 ,6′-dimethoxy-1 claim 1 ,1′-biphenyl (MeO-BIPHEP) or it's analogue.6. The production method according to claim 1 , wherein in Step A claim 1 , the chiral ligand in the optically active catalyst is 2 claim 1 ,2′-bis(diphenylphosphino)-1 claim 1 ,1′-binaphthyl (BINAP) or 5 claim 1 ,5′-bis(diphenylphosphino)-4 claim 1 ,4′-bi-1 claim 1 ,3-benzodioxole (SEGPHOS).7. The production method according to claim 1 , wherein the protecting group for the amino group represented by PGis an aralkoxycarbonyl group or an alkoxycarbonyl group.8. The production method according to claim 1 , wherein the protecting group for the amino group represented by PGis an aralkoxycarbonyl group.9. The production method according to claim 1 , wherein the protecting group for the amino group represented by PGis a benzyloxycarbonyl group.10. The production method according to claim 1 , wherein Ris a cyclopropyl group.11. The production method according to claim 1 , wherein the reaction in Step A is carried out under the ...

Подробнее
22-08-2013 дата публикации

CHOLINE ANALOGS AND CHEMICAL SYNTHESIS THEREOF

Номер: US20130217917A1
Принадлежит: VANDERBILT UNIVERSITY

A method of making a betaine aldehyde, comprising ozonizing an allyl trimethylammonium to form the betaine aldehyde. 1. A method of making a betaine aldehyde , comprising ozonizing an allyl trimethylammonium to form the betaine aldehyde.2. The method of claim 1 , wherein the nitrogen atom of the allyl trimethylammonium is isotopically enriched N.3. The method of claim 1 , wherein at least one of the hydrogen atoms of the allyl trimethylammonium is istopically enriched D.4. The method of claim 1 , wherein the allyl trimethylammonium is an allyl trimethylammonium chloride or an allyl trimethylammonium bromide.5. The method of claim 1 , wherein the ozonizing step comprises reacting the ally trimethylammonium with ozone to form a peroxide claim 1 , and reducing the peroxide with dimethyl sulfide to form the betaine aldehyde.6. The method of claim 1 , further comprising synthesizing the allyl trimethylammonium from a trimethylammonium and an allyl.7. The method of claim 6 , wherein the nitrogen atom of the trimethylammonium is isotopically enriched N.8. The method of claim 6 , wherein at least one of the hydrogen atoms of the trimethylammonium is istopically enriched D.9. The method of claim 6 , wherein the trimethylammonium is a trimethylammonium bromide or a trimethylammonium chloride.10. The method of claim 6 , wherein at least one of the hydrogen atoms of the allyl is isotopically enriched D. This patent application is a continuation of U.S. application Ser. No. 13/405,074 filed Feb. 24, 2012, which claims priority to U.S. Provisional Patent Application No. 61/446,391 filed Feb. 24, 2011. The entire content of each of these applications is hereby incorporate by reference.This invention was made with government support under National Institutes of Health grant numbers 1R00CA134749 and 3R00CA134749-02S1. The government has certain rights in the invention.Hyperpolarized MRI offers a sensitivity increase by 4-6 orders of magnitude as compared to conventional MRI. ...

Подробнее
29-08-2013 дата публикации

METHOD FOR PRODUCING CRYSTALLINE 5-AMINOSALICYLIC ACID

Номер: US20130225539A1
Принадлежит: PharmaZell GmbH

The invention relates to a method for producing crystalline 5-aminosalicylic acid with a particularly high tap and/or bulk density. 1. 5-Aminosalicylic acid (5-ASA) , characterized by having a bulk density of from 300 g/l to 700 g/l and grain size distribution of X(10)=1 μm-30 μm , X(50)=15 μm-60 μm , X(90)=35 μm-220 μm.2. 5-Aminosalicylic acid (5-ASA) according to claim 1 , characterized by a tapped density of from 510 g/l to 900 g/l.3. A process for producing the crystalline 5-aminosalicylic acid (5-ASA) as defined in comprising the following steps:(i) crystallizing 5-ASA from an aqueous solution of 5-ASA with or without the addition of protic or aprotic polar solvents in a concentration range of from 0 to 100% at a temperature of from 25° C. to 150° C. and at a pH-value of from 3.0 to 5.0 to form a suspension of 5-ASA; and(ii) wet grinding the suspension in a homogenizer.4. The process according to claim 3 , characterized in that said crystallizing is effected at a temperature of from 60° C. to 120° C.5. The process according to claim 3 , characterized by comprising a further step (iii) of cooling the suspension.6. The process according to claim 3 , characterized by comprising a further step (iv) of separating the 5-ASA crystals from the mother liquor.7. The process according to claim 3 , characterized by comprising a further step (v) of drying the 5-ASA crystals.8. Dosage articles selected from the group consisting of suppositories claim 1 , enemas claim 1 , sachets with micropellets and tablets comprising the 5-aminosalicylic acid (5-ASA) according to .9. Use of the 5-aminosalicylic acid (5-ASA) according to for preparing a dosage form selected from the group consisting of suppositories claim 1 , enemas claim 1 , sachets with micropellets and tablets.10. A pharmaceutical composition comprising the 5-aminosalicylic acid (5-ASA) according to .11. The 5-aminosalicylic acid as defined in for use in therapy and prophylaxis of a disease selected from the group ...

Подробнее
29-08-2013 дата публикации

IMAGING AGENTS

Номер: US20130225828A1
Автор: Goodman Mark M.
Принадлежит: EMORY UNIVERSITY

The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[F]fluorocyclobutyl-1-carboxylic acid (2-[F]FACBC) and 1-amino-2-[]fluoromethylcyclobutyl-1-carboxylic acid (2-[F]FMACBC). The labeled amino acid compounds of the invention are useful as imaging agents in detecting and/or monitoring tumors in a subject by PET or SPECT. 2. The compound of claim 1 , wherein halo is a non-radioactive F claim 1 , Cl claim 1 , Br claim 1 , or I.3. The compound of claim 1 , wherein (CRR)is CH.4. The compound of claim 1 , wherein Ris hydrogen.5. The compound of claim 1 , wherein Ris t-butyl.6. The compound of claim 1 , wherein Ris acyl.7. The compound of claim 6 , wherein acyl is t-butoxycarbonyl.8. A compound di-tert-butyl 2-oxa-3-thia-4-azabicyclo[3.2.0]heptane-4 claim 6 ,5-dicarboxylate 3 claim 6 ,3-dioxide.9. A kit comprising a compound of and a radio isotope labeling reagent.10. The kit of wherein the compound is di-tert-butyl 2-oxa-3-thia-4-azabicyclo[3.2.0]heptane-4 claim 9 ,5-dicarboxylate 3 claim 9 ,3-dioxide.11. The kit of claim 9 , wherein the radio isotope labeling reagent is salt of F. This application is a divisional of U.S. patent application Ser. No. 12/946,027 filed Nov. 15 ...

Подробнее
05-09-2013 дата публикации

Therapeutic Angiogenesis for Treatment of the Spine and Other Tissues

Номер: US20130230454A1
Принадлежит: CARDIOVASCULAR BIOTHERAPEUTICS, INC.

Methods for the diagnosis and treatment of ischemic spinal conditions, degenerative disc disease, back pain and/or other tissue pathologies. Patients with ischemic spine disease can be categorized into subsets that are deemed to have potential to respond to therapy. In particular, therapies are disclosed which involve stimulation of neovascularization so as to increase perfusion of spinal and other anatomies. 1. A method of diagnosing a patient with an ischemic spinal disorder , comprisingobtaining electronic image data of one or more vertebral bodies of the patient;identifying one or more regions of interest in the electronic image data, the one or more regions of interest including electronic image data of at least a portion of an intravertebral microcirculation proximate to an intervertebral endplate;analyzing the one or more regions of interest to obtain one or more perfusion measurements within each region of interest;comparing the one or more perfusion measurements with a predetermined perfusion value; anddiagnosing said patient with said ischemic spinal disorder wherein said one or more perfusion measurements is below said predetermined perfusion value.2. A method of treating a patient having an ischemic spinal disorder comprising:obtaining one or more images of at least a portion of a spine of the patient;analyzing the one or more images with a computing system to quantify a localized perfusion of the intravertebral microcirculation proximate to one or more endplates of one or more intervertebral discs of the patient's spine;identifying at least one intravertebral location where the quantified localized perfusion of the intravertebral circulation indicates hypoperfusion of the intravertebral circulation; andtreating the patient by injecting an angiogenesis inducing compound proximate to the at least one intravertebral location where the quantified localized perfusion of the intravertebral circulation indicates hypoperfusion of the intravertebral circulation. ...

Подробнее