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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 25554. Отображено 100.
26-01-2012 дата публикации

3-aminoxalyl-aminobenzamide derivatives and insecticidal and miticidal agents containing same as active ingredient

Номер: US20120022263A1
Принадлежит: Agro Kanesho Co Ltd

The present invention herein provides a 3-aminooxalylaminobenzamide derivative which is used as an insecticide or miticide. The 3-aminooxalylaminobenzamide derivative is one represented by the following general formula [1]: (R 1 and R 2 each represent, for instance, a C 1 to C 3 alkoxy group or a C 1 to C 3 haloalkoxy group; R 3 and R 4 each represent, for instance, a C 1 to C 8 alkyl group or a C 1 to C 8 haloalkyl group; R 5 represents, for instance, a C 1 to C 5 haloalkyl group; R 6 and R 7 each represent, for instance, a hydrogen atom or a C 1 to C 5 alkyl group; Y represents, for instance, a hydrogen atom or a halogen atom; Z represents, for instance, a hydrogen atom; n is an integer ranging from 0 to 4 and m is an integer ranging from 0 to 2).

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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.

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29-03-2012 дата публикации

Process for the preparation of cilastatin and sodium salt

Номер: US20120078009A1

An improved process for preparing Cilastatin Sodium including dissolving Cilastatin acid in a solvent using an organic base, adding sodium salt of a week acid and isolating Cilastatin Sodium.

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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.

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03-05-2012 дата публикации

Cross-Coupled Peptide Nucleic Acids for Detection of Nucleic Acids of Pathogens

Номер: US20120107794A1

The present invention concerns methods for detecting a nucleic acid comprising (i) contacting a solution comprising a first PNA having a first cross-reactive functional group with a substrate having a second PNA affixed thereto, the second PNA having a second first cross-reactive functional group, wherein the first PNA has a reporter molecule attached thereto and the first and second PNAs being complementary to different portions of a target DNA; (ii) contacting a sample suspected of containing the nucleic acid with the first and second PNAs; and (iii) determining the presence of the reporter molecule on the substrate.

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03-05-2012 дата публикации

Novel microbiocides

Номер: US20120108645A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

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

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24-05-2012 дата публикации

Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane

Номер: US20120130127A1
Принадлежит: Mer Pharma GmbH and Co KGaA

Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, an intermediate in the synthesis of 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof, comprising step (iii): (iii) reacting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane with chloroacetonitrile in the presence of an acid, wherein 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane is employed in step (iii) as obtained in the reaction of a methylmagnesium halide with 3,3,5,5-tetramethylcyclohexanone without having been subjected to a purification step.

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28-06-2012 дата публикации

Novel compound and method for preparing the same

Номер: US20120165572A1
Принадлежит: Fujifilm Corp

The invention is directed to a compound represented by the Formula (1) as defined herein, and a method for preparing a compound represented by the Formula (1) which includes: reacting a diamine compound represented by the Formula (2) as defined herein with a methacrylic anhydride or an acrylic anhydride under a condition where an organic acid having a pKa of 2.0 or more is present in an amount of 0.5 to 5.0 moles based on 1 mole of the diamine compound to obtain a reaction mixture; adding phosphoric acid to the reaction mixture; and purifying the reaction mixture by extraction with an organic solvent.

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19-07-2012 дата публикации

Reduction of fused bicyclic impurities in triiodinated x-ray contrast media

Номер: US20120184773A1
Принадлежит: Mallinckrodt LLC

The present disclosure generally relates to an improved process for alkylating a triiodo-substituted arylamide to form a compound suitable for use as an X-ray contrast agent. More particularly, the present disclosure is directed to such a process that limits the formation of fused bicyclic impurities, such as Impurity G, in the alkylation reaction mixture.

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18-10-2012 дата публикации

Photocurable compound

Номер: US20120264963A1
Принадлежит: SAMSUNG ELECTRONICS CO LTD

Disclosed is a compound having a photocurable urethane(meth)acrylate group, its manufacturing method, and a photocurable composition including the compound. The compound is represented by Chemical Formulae 1 to 6. Each of Chemical Formulae 1 to 6 includes a urethane(meth)acrylate group represented by Chemical Formula 1-1 or 1-2.

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08-11-2012 дата публикации

Intermediate compounds and processes for the preparation of tapentadol and related compounds

Номер: US20120283463A1
Принадлежит: Mapi Pharma Ltd

The present invention discloses processes for the preparation of 3-[(1R,2R)-3-(dimethyl-amino)-1-ethyl-2-methyl-propyl]phenol (Tapentadol), salts thereof and related compounds of formula (A), including stereoisomers and pharmaceutically acceptable salts thereof, and to certain intermediates used in such process.

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29-11-2012 дата публикации

Ether-amide compounds and uses thereof

Номер: US20120302791A1
Принадлежит: Individual

Novel ether-amide compounds are described. Uses of the compounds, in particular as solvents, for example in phytosanitary formulations are also described.

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29-11-2012 дата публикации

Process for producing 2-chloro-3,3,3-trifluoropropene

Номер: US20120302803A1
Принадлежит: Daikin Industries Ltd

The present invention provides a process for producing 2-chloro-3,3,3-trifluoropropene represented by the chemical formula: CF 3 CCl═CH 2 , comprising mixing a fluorine-containing alkane, in a liquid state, represented by the formula: CF 3 CH—ClCH 2 X, wherein X is halogen, with an aqueous solution containing at least one metal hydroxide selected from the group consisting of alkali metal hydroxides and alkali earth metal hydroxides in the presence of a catalyst to perform a dehydrohalogenation reaction of the fluorine-containing alkane. According to the present invention, 2-chloro-3,3,3-trifluoropropene (HCFO-1233xf) can be obtained at a very high yield at a relatively low reaction temperature.

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13-12-2012 дата публикации

Fibrillation-resistant insulin and insulin analogues

Номер: US20120316107A1
Автор: Michael Weiss
Принадлежит: CASE WESTERN RESERVE UNIVERSITY

A fibrillation-resistant insulin analogue may be a single-chain insulin analogue or a physiologically acceptable salt thereof, containing an insulin A chain sequence or an analogue thereof and an insulin B chain sequence or an analogue thereof connected by a polypeptide of 4-10 amino acids. The fibrillation-resistant insulin analogue preferably displays less than 1 percent fibrillation with incubation at 37° C. for at least 21 days. A single-chain insulin analogue displays greater in vitro insulin receptor binding than normal insulin while displaying less than or equal binding to IGFR than normal insulin. The fibrillation-resistant insulin may be used to treat a patient using an implantable or external insulin pump, due to its greater fibrillation resistance.

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20-12-2012 дата публикации

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

Номер: US20120321560A1

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

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27-12-2012 дата публикации

Taste Improving Substances

Номер: US20120328536A1
Принадлежит: Quest International Services BV

The present invention relates to taste improvement of foodstuffs, beverages, tobacco products and oral care products, using a substance according to formula (I), edible salts or edible esters thereof: It was found that substances represented by formula (I) are capable of modifying and complementing, the sensory impact of taste imparting substances. Thus, the present taste improving substances are advantageously applied in flavour compositions, foodstuffs, tobacco products and oral care products. Typical examples of taste improving substances according to the present invention include N-(2-hydroxyethyl) 3-hydroxypropionamide; N-(2-hydroxyethyl) 3-hydroxybutyramide; N-(2-hydroxyethyl) 4-hydroxybutyramide; N-(2-hydroxyethyl) N-5-hydroxypentanoylamide; N-(2-hydroxyethyl) 4-hydroxypentanoylamide; N-(2-hydroxyethyl) 3-hydroxypentanoylamide; N-(2-hydroxyethyl) 2-methyl-4-hydroxy-butyramide; N-(2-hydroxyethyl) 2-methyl-3-hydroxybutyramide; N-(2-hydroxyethyl) N-6-hydroxyhexanoylamide; N-(2-hydroxyethyl) 5-hydroxyhexanoylamide; N-(2-hydroxyethyl) 4-hydroxyhexanoylamide; N-(2-hydroxyethyl) 3-hydroxyhexanoylamide; N-(2-hydroxyethyl) 4-hydroxy-2-keto-3-methyl-pentanoylamide; N-(2-hydroxyethyl) 4-hydroxy-2-keto-3-methyl-hexanoylamide and mixtures thereof.

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27-12-2012 дата публикации

Bis-phosphate compound and asymmetric reaction using the same

Номер: US20120330038A1
Принадлежит: API Corp, Tohoku University NUC

A novel bis-phosphate compound is provided which can be applied to a wide range of reactive substrates and reactions as an asymmetric reaction catalyst and can realize an asymmetric reaction affording a high yield and a high enantiomeric excess. The bis-phosphate compound has a tetraaryl skeleton represented by General Formula (1). In an asymmetric reaction, an amidodiene and an unsaturated aldehyde compound are reacted with each other in the presence of the optically active bis-phosphate compound to give an optically active amidoaldehyde. The invention allows a reaction such as an asymmetric Diels-Alder reaction to proceed efficiently, which has been difficult with conventional mono-phosphate compounds. Thus, the invention enables an industrially feasible method for the production of optically active amidoaldehydes, optically active β-amino acid derivatives, optically active diamine compounds, optically active pyrrolidine derivatives and optically active dihydropyran derivatives which are useful as products such as medicines, agricultural chemicals and chemical products as well as synthesis intermediates for such products.

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27-12-2012 дата публикации

Method for producing substituted fluorine-containing olefin

Номер: US20120330072A1
Принадлежит: Daikin Industries Ltd, Osaka University NUC

This invention relates to a method of reacting fluoroolefin with an organic magnesium compound in the presence of a catalyst comprising nickel or palladium so as to efficiently produce fluoroolefin, such as TFE, in which a fluorine (F) atom or atoms bonded to the sp 2 hybridized carbon atom are substituted with an organic group.

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31-01-2013 дата публикации

Process for the preparation of lacosamide

Номер: US20130030216A1
Принадлежит: EUTICALS SPA

A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.

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14-02-2013 дата публикации

Electric Conduction Through Supramolecular Assemblies of Triarylamines

Номер: US20130037307A1
Принадлежит: Universite De Strasbourg

The present invention relates to a method for modifying a surface of a solid conducting material, which comprises a step (E), in which a potential difference is applied between this surface and a surface of another conducting solid material positioned facing it, and wherein, simultaneously, said surface (S) is put into contact with a liquid medium comprising in solution triarylamines (I): while subjecting these triarylamines (I) to electromagnetic radiation, least partly converting them at into triarylammonium radicals. The invention also relates to a conducting device comprising two conducting metal materials, the surfaces of which, (S) and (S′) respectively, are electrically interconnected through an organic material comprising conducting fibrillar organic supramolecular species comprising an association of triarylamines of formula (I).

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21-02-2013 дата публикации

Method for the Hydrolysis of Substituted Formylamines into Substituted Amines

Номер: US20130046111A1
Автор: Mikhail Bobylev
Принадлежит: Individual

An improved method for the synthesis of substituted formylamines and substituted amines via an accelerated Leuckart reaction. The Leuckart reaction is accelerated by reacting formamide or N-alkylformamide and formic acid with an aldehyde or a ketone at a preferred molar ratio that accelerates the reaction. The improved method is applicable to various substituted aldehydes and ketones, including substituted benzaldehydes. An accelerated method for the hydrolysis of substituted formylamines into substituted amines using acid or base and a solvent at an elevated temperature. The improved method is useful for the accelerated synthesis of agrochemicals and pharmaceuticals such as vanillylamine, amphetamine and its analogs, and formamide fungicides.

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21-03-2013 дата публикации

COMPOUNDS WITH BOTH ANALGESIC AND ANTI-HYPERALGESIC EFFICACY

Номер: US20130072533A1
Принадлежит:

The present invention relates to molecules of formula (I), deriving from lipoic acid and camosine, their preparation and use as analgesics. 2. Compounds of formula (I) according to for use as a medicament.3. Compounds according to for use as analgesics.4. Compounds of formula (I) according to for the treatment of neuropathic pain.5. Compositions comprising at least one compound of formula (I) according to and at least one other pharmaceutically acceptable ingredient.6. Process for the preparation of compounds of formula (I) according to starting from lipoic acid and carnosine.8. Compounds of formula (II) as defined in . The present invention relates to the field of organic compounds containing heterocycles having pharmacological efficacy as analgesics.The World Health Organisation (W.H.O.) defines neuropathic pain as: “An unpleasant sensation and a negative-affective emotional experience, associated with actual or potential tissue damage, or described in terms of such damage”. The International Association for the Study of Pain (1ASP) defines it as: “An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described as such”.Neuropathic pain is a significant problem in neurology in that it occurs frequently and is often disabling due to its irritating and chronic character.Examples thereof are: post-herpetic pain, phantom limb pain which can arise after an amputation, pain present in peripheral neuropathy such as with diabetes or AIDS, so-called complex regional pain syndrome or reflex sympathetic dystrophy pain, and pain from lesions of the central nervous system. These latter can be sequelae of stroke, trauma, tumours or due to systemic diseases. In most cases, the pain often present in multiple sclerosis is of such origin. In recent years, interest has focussed on neuropathic pain induced by chemotherapy drugs (vincristine, paclitaxel, oxaliplatin, bortezomib, etc.)The characteristics of this pain vary from patient to ...

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21-03-2013 дата публикации

PYRAZOLECARBOXAMIDE DERIVATIVES AND THEIR USE AS MICROBIOCIDES

Номер: US20130072535A1
Принадлежит: SYNGENTA CROP PROTECTION LLC

Compounds of Formula (I) wherein Ris C-Calkyl or C-Chaloalkyl; Ris C-Calkyl; Ris hydrogen or halogen; Ris hydrogen, C-Calkyl or C-Chalogenalkyl; Ris hydrogen, halogen, C-Calkyl or C-Chalogenalkyl; Ris hydrogen, halogen, C-Calkyl, C-Calkenyl or C-Calkinyl; Ris hydrogen, halogen, C-Calkyl, C-Calkenyl, C-Calkinyl, C-Ccycloalkyl-C-Calkinyl, halophenoxy, halophenyi, C-Chaloalkyl, C-Chaloakoxy, C-Chaloalkenyl, or C-Chaloalkenyloxy; Ris hydrogen, halogen, C-Calkyl, C-Calkenyl or C-Calkinyl; with the provisio that at least one of R, Rand Ris different from hydrogen; n is 0 or 1, are suitable for use as microbriocides. 2. A compound of formula I according to claim 1 , wherein{'sub': '1', 'Ris difluoromethyl, trifluoromethyl or methyl,'}{'sub': '2', 'Ris methyl;'}{'sub': '3', 'Ris hydrogen or fluoro;'}{'sub': '4', 'Ris methyl;'}{'sub': '5', 'Ris hydrogen or methyl;'}n is 0; and{'sub': 6', '7', '8, 'R, Rand Rindependently from each other, are hydrogen or chloro.'}3. A compound of formula I according to claim 2 , wherein{'sub': '5', 'Ris hydrogen.'}4. A compound of formula I according to claim 1 , wherein{'sub': '1', 'Ris difluoromethyl or trifluoromethyl;'}{'sub': '2', 'Ris methyl;'}{'sub': '3', 'Ris hydrogen;'}{'sub': '4', 'Ris methyl;'}{'sub': 6', '7', '8, 'R, Rand Rare, independently from each other, hydrogen or halogen.'}5. A compound of formula I according to claim 4 , wherein R claim 4 , Rand Rare claim 4 , independently from each other claim 4 , hydrogen or chloro claim 4 , with the proviso that at least one of R claim 4 , Rand Ris different from hydrogen.6. A compound of formula I according to claim 1 , wherein{'sub': '5', 'Ris hydrogen.'}7. A compound of formula I according to claim 1 , wherein{'sub': 1', '1', '4, 'Ris C-Chaloalkyl;'}{'sub': 2', '1', '4, 'Ris C-Calkyl;'}{'sub': '3', 'Ris hydrogen;'}{'sub': 4', '1', '4, 'Ris C-Calkyl;'}{'sub': '5', 'Ris hydrogen;'}n is 0 or 1;{'sub': '6', 'Ris hydrogen or halogen;'}{'sub': 7', '8, 'Ris halogen; and Ris hydrogen or ...

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21-03-2013 дата публикации

18ß-GLYCYRRHETINIC ACID DERIVATIVES AND SYNTHETIC METHOD THEREOF

Номер: US20130072694A1
Принадлежит: KAOHSIUNG MEDICAL UNIVERSITY

The present invention provides a chemical compound having the structure being one selected from a group consisting of 2. The method according to further comprising a step of using an isopropylamine solution as the amine solution when Ris CONHCH(CH) claim 1 , and using an aniline solution as the amine solution when Ris CONHCH.3. The method according to further comprising steps of:methylating the 18β-glycyrrhetinic acid to obtain a methylated 18β-glycyrrhetinic acid; andoxidizing the methylated 18β-glycyrrhetinic acid to obtain a second compound.4. The method according to further comprising a step of esterifying the lactone compound to obtain a first derivative of the lactone compound.5. The method according to further comprising a step of cleaving a lactone ring of the lactone compound to obtain a second derivative of the lactone compound.6. The method according to further comprising a step of treating the second derivative with an alcohol solution to obtain a third derivative of the lactone compound.7. The method according to claim 6 , wherein the alcohol solution is one of an isopropyl alcohol solution and a benzyl alcohol solution.8. The method according to further comprising a step of esterifying the second compound with an alcohol solution to obtain a fourth derivative of the lactone compound.9. The method according to further comprising a step of cleaving a lactone ring of the fourth derivative by an acidic solution to obtain a fifth derivative of the lactone compound.13. The method according to claim 12 , wherein the chemical compound with Rbeing one of CONHCH(CH)and CONHCHis obtained by steps of:oxidizing the 18β-glycyrrhetinic acid to form a first compound;treating the first compound with an m-chloroperbenzoic acid to afford a lactone compound; andtreating the lactone compound with an amine solution to obtain the chemical compound being a first derivative of the chemical compound.14. The method according to further comprising a step of using an ...

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21-03-2013 дата публикации

ENANTIOMERICALLY PURE AMINES

Номер: US20130072711A1
Принадлежит: NABRIVA THERAPEUTICS AG

A compound of formula 3. A compound according to claim 1 , wherein PROT and PROT′ together with the nitrogen atom to which are attached form phthalimido-N-yl.4. A compound according to claim 1 ,wherein PROT″ is benzoyl or trityl.7. A compound according to claim 1 , selected from the group consisting of:{(1R,2R,4R)-4-[(tert-Butoxycarbonyl)-amino]-2-hydroxy-cyclohexyl}-benzene-carbothioate,{(1R,2R,4R)-4-[(2,2,2-Trifluoro-acetyl)-amino]-2-hydroxy-cyclohexyl}-benzene-carbothioate,tert-Butyl [(1R,3R,4R)-3-hydroxy-4-tritylsulfanyl-cyclohexyl]-carbamate, and2,2,2-Trifluoro-N-((1R,3R,4R)-3-hydroxy-4-tritylsulfanyl-cyclohexyl)-acetamide.10. A compound of formula II claim 9 , II claim 9 , IIor IIaccording to claim 9 , selected from the group consisting oftert-Butyl (1R,3R,6R)-(7-oxa-bicyclo[4.1.0]hept-3-yl)-carbamate, and2,2,2-Trifluoro-N-(1R,3R,6S)-(7-oxa-bicyclo[4.1.0]hept-3-yl)-acetamide.12. A process according to claim 11 , wherein none of the intermediates obtained in a) to d) is isolated.13. A process according to claim 11 , wherein the reaction a) to e) is performed in a single solvent (system).14. (canceled) The present invention relates to enantiomerically pure amines, such as amino and thio protected hydroxy-mercapto-cyclohexyl amines and production processes thereof.Organic compounds, such as cyclohexyl amines containing an asymmetric carbon atom may exist in the form of enantiomers, diastereoisomers and mixtures thereof, e.g. racemates. Such compounds may exist in the (R)-, (S)- or (R,S)-configuration. For pharmaceutical use it is often vital to have an active compound comprising an asymmetric carbon atom in one of the enantiomerically pure forms, since one isomer may differ, e.g. in several aspects from another isomer, e.g. one isomer may be more active than the other isomer. Separation of isomers is often burdensome. Chromatography which, for example, may be useful for isomeric separation, is on technical scale not easy to carry out and often needs sophisticated ...

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21-03-2013 дата публикации

Process For The Iodination Of Phenolic Derivatives

Номер: US20130072719A1
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to a process for the preparation of iodinated phenols; in particular; it relates to a process including the direct iodination, with suitably activated iodine, of 3,5-disubstituted phenol compounds to the corresponding 3,5-disubstituted-2,4,6-triiodophenols, which are useful intermediates for the synthesis of x-ray contrast media, and to the preparation of the contrast media themselves. 2. The process of wherein claim 1 , within the compounds of formulae 1 and 2 claim 1 , R and R′ represent claim 1 , independently claim 1 , a group of formula —NHRor —NRRwherein each R claim 1 , Rand Ris claim 1 , independently claim 1 , a straight or branched C-Calkyl group optionally substituted by one to three hydroxyl groups.3. The process of wherein claim 2 , within the compounds of formulae 1 and 2 claim 2 , R and R′ represent claim 2 , independently claim 2 , a group selected from:{'sub': '3', '—NHCH,'}{'sub': 2', '2, '—NHCH—CH(OH)—CHOH,'}{'sub': 2', '2, '—NHCH(CHOH), and'}{'sub': 3', '2', '2, '—N(CH)—CH—CH(OH)—CHOH.'}4. The process of wherein the molar ratio between molecular iodine and 3 claim 1 ,5-disubstituted phenol substrate 1 [I/1] is comprised from 1.1 to 1.3 claim 1 , and the molar ratio between iodic acid and 3 claim 1 ,5-disubstituted phenol substrate 1 is comprised from 0.4 to 0.8.5. The process according to wherein the triiodination of the 3 claim 4 ,5-disubstituted phenol substrate 1 with iodine and iodic acid is carried out by using a molar ratio 3 claim 4 ,5-disubstituted phenol substrate:iodine:iodic acid of 1:1.2:0.6.6. The process according to wherein said aqueous medium is water or an aqueous solution.7. The process of comprising: obtaining an aqueous solution of 3 claim 6 ,5-di-substituted phenol substrate of formula 1 claim 6 , or of a salt thereof claim 6 , and adding Iand HIOto said aqueous solution.8. The process according to wherein said aqueous solution of 3 claim 7 ,5-di-substituted phenol substrate is a crude solution ...

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28-03-2013 дата публикации

REACTIVE MONOMER FOR A COATING AND/OR REACTIVE COATING

Номер: US20130078879A1
Принадлежит: ISP Investments Inc.

Disclosed herein are coating solutions comprising a reactive monomer, process and compositions for preparing the same that are suitable for a coating and/or reactive coating. More particularly, the present invention relates to monomers comprising a multifunctional N-vinylformamide crosslinking moiety and their use in coatings. Also disclosed are applications and compositions comprising coating solutions of a reactive monomer and its application in printing processes and inks. 1. A coating composition comprising at least one reactive monomer , wherein said reactive monomer comprises a multifunctional N-vinylformamide crosslinking moiety , a hybrid N-vinylformamide moiety , or combinations thereof.2. The coating composition of wherein the composition is at least one of a reactive solution or a reactive coating.3. The coating composition of wherein the at least one reactive monomer is 1 claim 1 ,8-Di-(N-vinylformamido)-3 claim 1 ,6-dioxyoctane.4. The coating composition of wherein the coating is a UV curable coating claim 1 , a printing ink claim 1 , or a UV printing ink.5. The coating composition of wherein the coating is conductive.6. The coating composition of wherein the coating is applied to at least one of metal claim 1 , plastic claim 1 , glass claim 1 , or textile.7. The coating composition of wherein the metal is selected from the group consisting of steel claim 6 , iron claim 6 , copper claim 6 , brass claim 6 , gold claim 6 , silver claim 6 , and aluminum.8. The coating composition of wherein the plastic is selected from the group consisting of vinyl claim 6 , polyolefin (PE and PP) claim 6 , Tyvec claim 6 , polyester claim 6 , PVDC claim 6 , and nylon.9. The coating composition of further comprising at least one of a fragrance claim 1 , an anionic initiator claim 1 , a cationic initiator claim 1 , a free radical initiator claim 1 , a metal claim 1 , a carbon pigment claim 1 , a carbon nanotube claim 1 , a graphene sheet claim 1 , or a quantum dot.10. The ...

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28-03-2013 дата публикации

Lipid Compounds Targeting VLA-4

Номер: US20130079383A1
Принадлежит: ARROWHEAD RESEARCH CORPORATION

The invention relates to the compounds of formula I: 8. A compound of wherein W is hydrogen and Y is methyl.9. A compound of wherein both W and Y are methyl.10. A compound of wherein Ris an alkyl having 9-20 carbon atoms.11. A compound of wherein Ris an alkyl having 16-20 carbon atoms.12. A compound of wherein Ris an alkyl having 18 carbon atoms.13. A compound of wherein Ris an alkyl having 19 carbon atoms.14. A compound of wherein Ris an alkyl having 20 carbon atoms.15. A compound of wherein n is 9-13.16. A compound of selected from the group consisting of:[2,3-bis(dodecyloxy)propyl][3-[[3-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-1-oxopropyl]amino]propyl]dimethylaminium trifluoroacetate;[2,3-bis(dodecyloxy)propyl][3-[[4-[[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]amino]-1-4-dioxobutyl]amino]propyl]dimethylaminium trifluoroacetate;[[2,3-bis(hexadecyloxy)propyl][3-[[3-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]-1-oxopropyl]amino]propyl]dimethylaminium trifluoroacetate;[2,3-bis(hexadecyloxy)propyl][3-[[4-[[2-2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[3-[[2-[1-[[[(S)-1-carboxy-2-[4-(2,6-dichloro-benzoylamino)phenyl]ethyl]amino]carbonyl]cyclopentyl]ethyl]amino]-3-oxopropyl]oxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]amino]-1,4-dioxobutyl]amino]propyl]dimethylaminium trifluoroacetate;(S)-Alpha-[[[1-[2-[[3-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[4-[[3-[[2,3-bis(hexadecyloxy)propyl]methylamino]propyl]amino]-1,4- ...

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28-03-2013 дата публикации

Branched 3-phenylpropionic acid derivatives and their use

Номер: US20130079412A1
Принадлежит: BAYER PHARMA AKTIENGESELLSCHAFT

The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases. 3. The compound of wherein:{'sup': 1', '2, 'Rand Rboth represent hydrogen,'}{'sup': '3', 'Rrepresents hydrogen or methyl,'}{'sub': '2', 'L represents a bond or represents —CH—,'}{'sup': 4A', '4B, 'claim-text': {'sup': '5', 'Rrepresents hydrogen, fluorine or methyl,'}, 'Rand Rboth represent methyl or are attached to one another and together with the carbon atom to which they are attached form a cyclopropyl or cyclobutyl ring which may be substituted up to two times by fluorine,'}{'sup': '6', 'claim-text': [{'sup': '7', 'Rrepresents hydrogen,'}, {'sup': '8A', 'Rrepresents methyl,'}, {'sup': '8B', 'Rrepresents trifluoromethyl,'}], 'Rrepresents chlorine,'}{'sup': '9', 'Rrepresents fluorine, chlorine, methyl, trifluoromethyl, ethyl, 2,2,2-trifluoroethyl, isopropyl, tert-butyl, cyclopropyl or 2,2-difluorocyclopropyl,'}and{'sup': '10', 'Rrepresents hydrogen, fluorine, methyl or methoxy,'}and salts, solvates and solvates of the salts thereof.5. (canceled)6. (canceled)7. A pharmaceutical composition comprising a compound of and an inert claim 1 , non-toxic claim 1 , pharmaceutically suitable excipient.8. The pharmaceutical composition of further comprising an active compound selected from the group consisting of an organic nitrate claim 1 , an NO donor claim 1 , a cGMP-PDE inhibitor claim 1 , a stimulator of guanylate cyclase claim 1 , an agent having antithrombotic activity claim 1 , an agent lowering blood pressure claim 1 , and an agent altering lipid metabolisms.9. (canceled)10. Method for the treatment and/or prevention of heart failure claim 1 , angina pectoris ...

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28-03-2013 дата публикации

ENHANCED BIMATOPROST OPHTHALMIC SOLUTION

Номер: US20130079414A1
Принадлежит: ALLERGAN, INC.

A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein. 1. A composition comprising about 0.0125% w/v bimatoprost and about 200 ppm benzalkonium chloride , wherein said composition is an aqueous liquid which is formulated for ophthalmic administration.2. (canceled)3. The composition of wherein the concentration of benzalkonium chloride is 200 ppm.4. The composition of having a pH of 7.4 which consists essentially of 0.0125% bimatoprost claim 3 , 200 ppm benzalkonium chloride claim 3 , from 0 to 0.03% EDTA claim 3 , a phosphate buffer claim 3 , NaCl claim 3 , and water.5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. The composition of having a pH of 7.4 which comprises 0.0125% bimatoprost claim 1 , 200 ppm benzalkonium chloride claim 1 , from 0 to 0.03% EDTA claim 1 , a sodium phosphate buffer claim 1 , NaCl and water.11. (canceled)12. A method comprising administering to a mammal suffering from glaucoma or intraocular hypertension a composition comprising about 0.125% w/v bimatoprost and about 200 ppm benzalkonium chloride.13. The composition of comprising from 0.001% to 0.15% EDTA.14. The composition of comprising from 0.01% to 0.1% EDTA.15. The composition of comprising from 0.01% to 0.05% EDTA.16. The composition of comprising 200 ppm BAK.17. The composition of comprising 0.0125% bimatprost. This application claims the benefit of U.S. Provisional Patent Application Ser. No. 61/157,225, filed on Mar. 4, 2009, the entire disclosure of which is incorporated herein by this specific reference.This invention relates to pharmaceutical compositions comprising bimatoprost.Bimatoprost, shown below, is a prostamide marketed commercially for the treatment of glaucoma ...

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28-03-2013 дата публикации

METHOD FOR PREPARING ALKYL LACTATE AND A METHOD FOR PREPARING LACTAMIDE USING THE SAME

Номер: US20130079547A1
Принадлежит: LG CHEM, LTD.

This disclosure relates to a method for preparing alkyl lactate with high yield and high selectivity, comprising the step of reacting glycerol with water or alcohol in the presence of a catalyst. 2. The method according to claim 1 , wherein the catalyst is a homogeneous or heterogeneous catalyst.3. The method according to claim 2 , wherein the homogeneous catalyst is at least one selected from the group consisting of an alkali metal compound having a hydroxyl or alkoxy group claim 2 , a bicarbonate (HCO)-containing metal compound claim 2 , and a carbonate (CO)-containing metal compound.4. The method according to claim 3 , wherein the alkali metal compound having a hydroxyl group is NaOH claim 3 , KOH claim 3 , LiOH or Ba(OH) claim 3 , andthe alkali metal compound having an alkoxy group is NaOR, KOR or LiOR (wherein, R is a substituted or unsubstituted C1-10 alkyl group).5. The method according to claim 2 , wherein the heterogeneous catalyst is a metal compound containing Mg claim 2 , Ca claim 2 , Zr claim 2 , Sn or Ti.6. The method according to claim 5 , wherein the heterogeneous catalyst further comprises at least one selected from the group consisting of an alkali metal compound claim 5 , a hydroxyl group-containing metal compound claim 5 , a bicarbonate-containing metal compound claim 5 , a carbonate-containing metal compound claim 5 , activated clay claim 5 , zeolite claim 5 , active carbon claim 5 , diatomaceous earth claim 5 , bentonite claim 5 , alumina claim 5 , silicalite claim 5 , fly ashes claim 5 , molecular sieve claim 5 , vermiculite claim 5 , perlite claim 5 , π-complex compound adsorbent claim 5 , clay and polymer resin.7. The method according to claim 1 , wherein the reaction is conducted in a batch reactor or tubular reactor.8. The method according to claim 1 , wherein the reaction is conducted at a temperature of 100 to 300° C. and a pressure of 10 to 200 atm for 1 to 20 hours claim 1 , under inert atmosphere.9. The method according to claim 1 , ...

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28-03-2013 дата публикации

SILVER-CATALYZED SYNTHESIS OF AMIDES FROM AMINES AND ALDEHYDES

Номер: US20130079556A1
Принадлежит:

The invention provides a method for producing amides via the reaction of aldehydes and amines with oxygen adsorbed on a metallic silver or silver alloy catalyst. An exemplary reaction is shown in Scheme 1 : (I), (II), (III) 1. A method for preparing an amide comprising reacting an aldehyde and a primary or secondary amine with oxygen adsorbed on a catalyst comprising silver metal or an alloy thereof to produce the amide.4. The method of claim 2 , wherein Rand Rare methyl.5. The method of claim 1 , wherein the aldehyde is formaldehyde.6. The method of claim 1 , wherein the silver alloy is an alloy of silver and gold.7. The method of claim 1 , wherein the source of the adsorbed oxygen is oxygen gas.8. The method of claim 1 , wherein the amine is a primary amine.9. The method of claim 1 , wherein the amine is a secondary amine.10. The method of claim 1 , wherein the catalyst is promoted by a material selected from the group consisting of metal halides claim 1 , carbonates claim 1 , sulfites claim 1 , sulfates claim 1 , nitrites claim 1 , and nitrates claim 1 , transition metal oxoanions claim 1 , lanthanides claim 1 , and alkali and alkaline earth metals.11. The method of claim 1 , wherein the temperatures is from 270 to 1000 K.12. The method of claim 1 , wherein the pressure is from 0.1 atm to 5 atmospheres.13. The method of claim 1 , wherein the catalyst is carried on an inert supporting material. This application claims benefit of U.S. Provisional Application No. 61/336,673, filed Jan. 25, 2010, which is hereby incorporated by reference.This invention was made with U.S. government support under National Science Foundation awards CHE-0513936, PHY-0646094, CHE-0545335, DMR-0820484 and Department of Energy award DE-FG02-84ER13289. The U.S. Government has certain rights in the invention.The invention is in the field of synthetic organic chemistry, and relates specifically to chemical processes involving catalysis, oxidation, and amide synthesis.Amidation is a ...

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11-04-2013 дата публикации

Protein Modification from the Oxidation of Clickable Polyunsaturated Fatty Acid Analogs

Номер: US20130089884A1
Принадлежит: LIFE TECHNOLOGIES CORPORATION

Clickable polyunsaturated fatty acid analogs, methods of using these analogs and kits comprising these analogs. 2. The compound of claim 1 , wherein Xis an alkyne reactive moiety; and Xis selected from the group consisting of an H claim 1 , alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , cycloalkenyl claim 1 , alkoxy claim 1 , aryl claim 1 , aralkyl claim 1 , heteroaryl claim 1 , and heteroaralkyl.3. The compound of claim 1 , wherein Xis azide reactive moiety; and Xis selected from the group consisting of an H claim 1 , alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , cycloalkenyl claim 1 , alkoxy claim 1 , aryl claim 1 , aralkyl claim 1 , heteroaryl claim 1 , and heteroaralkyl.4. The compound of claim 1 , wherein Xis an alkyne reactive moiety; and Xis selected from the group consisting of H claim 1 , alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , cycloalkenyl claim 1 , alkoxy claim 1 , aryl claim 1 , aralkyl claim 1 , heteroaryl claim 1 , and heteroaralkyl.5. The compound of claim 1 , wherein Xis an azide reactive moiety; and Xselected from the group consisting of H claim 1 , alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , cycloalkenyl claim 1 , alkoxy claim 1 , aryl claim 1 , aralkyl claim 1 , heteroaryl claim 1 , and heteroaralkyl.6. The compound of claim 1 , wherein Xand Xare independently selected from the group consisting of an alkyne reactive moiety claim 1 , and azide reactive moiety.9. The method of claim 8 , wherein the modified biomolecule is a modified protein.10. The method of claim 8 , wherein Xis an alkyne reactive moiety; and Xis selected from the group consisting of an H claim 8 , alkyl claim 8 , alkenyl claim 8 , cycloalkyl claim 8 , cycloalkenyl claim 8 , alkoxy claim 8 , aryl claim 8 , aralkyl claim 8 , heteroaryl claim 8 , and heteroaralkyl.11. The method of claim 8 , wherein Xis azide reactive moiety; and Xis selected from the group consisting of an H claim 8 , alkyl claim 8 , alkenyl claim 8 , cycloalkyl claim 8 , ...

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11-04-2013 дата публикации

LYSINE SPECIFIC DEMETHYLASE-1 INHIBITORS AND THEIR USE

Номер: US20130090386A1
Принадлежит:

The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CHC(=0)NH, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH—, —CHCH—, —CHCHCH—, and —CHCHCHCH—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH, —NH(C-Calkyl), —N(C-Calkyl)(C-Calkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer. 1. A compound of Formula 1{'br': None, 'sub': 'X', '(A′)-(A)-(B)—(Z)-(L)-(D)\u2003\u20031'} (A) is heteroaryl or aryl;', {'sub': 2', '2, 'each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CHC(═O)NH, heteroaryl, cyano, sulfonyl, and sulfinyl;'}, 'X is 0, 1, 2, or 3;', '(B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B);', '(Z) is —NH—;', {'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, '(L) is chosen from a single bond, —CH—, —CHCH—, —CHCHCH—, and —CHCHCHCH—; and'}, {'sub': 2', '1', '6', '1', '6', '1', ...

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18-04-2013 дата публикации

WATER/OIL REPELLENT AGENT AND WATER/OIL REPELLENT COMPOSITION

Номер: US20130092047A1
Автор: HOSHINO Taiki
Принадлежит: Asahi Glass Company, Limited

To provide a water/oil repellent agent and a water/oil repellent composition which are capable of imparting sufficient water/oil repellency to the surface of an article and which have low environmental impact. One comprising a reaction product obtained by reacting a fluorinated alcohol or amine having a polyfluoroalkyl moiety having at most 6 carbon atoms with a polyisocyanate compound, which is, when applied to an article, capable of imparting sufficient water/oil repellency, while presenting little environmental impact. When applied to an article, the water/oil repellent composition of the present invention is capable of imparting a high quality water/oil repellency to the article. 2. The water/oil repellent agent according to claim 1 , wherein the reaction product has no isocyanate group.3. The water/oil repellent agent according to claim 1 , wherein the Rin the fluorinated compound (a) is a Cperfluoroalkyl group.5. The water/oil repellent agent according to claim 1 , wherein the polyisocyanate compound (b) is hexamethylene diisocyanate or its modified product.6. The water/oil repellent agent according to claim 1 , which further contains a reaction product of a polyisocyanate compound (b) with a compound (c) having an active hydrogen group reactive with an isocyanate group claim 1 , or a reaction product of a polyisocyanate (b) with the fluorinated compound (a) and a compound (c) having an active hydrogen group reactive with an isocyanate group.7. A water/oil repellent composition which comprises the water/oil repellent agent as defined in and a solvent.8. The water/oil repellent composition according to claim 7 , which has a solid content concentration of from 0.05 to 10 mass %. The present invention relates to a water/oil repellent agent and a water/oil repellent composition.As a method for imparting water/oil repellency to the surface of an article (such as a fiber product), a method of treating the article by means of a water/oil repellent composition ...

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18-04-2013 дата публикации

RESUSCITATION FLUID

Номер: US20130095192A1
Автор: SIMPKINS Cuthbert O.
Принадлежит:

A method for treating conditions related to lack of blood supply with a lipid based resuscitation fluid is disclosed. The resuscitation fluid contains a lipid component and an aqueous carrier. The lipid component forms an emulsion with the aqueous carrier. The resuscitation fluid can be used to increase the blood pressure and to carry oxygen to tissues. The resuscitation fluid can also be used for preserving the biological integrity of donor organs for transplantation. 121-. (canceled)22. A resuscitation kit , comprising:a lipid based resuscitation fluid comprising a lipid component and an aqueous carrier; andan oxygenation device.23. The resuscitation kit of claim 22 , wherein said oxygenation device is a container containing an oxygenating gas.24. The resuscitation kit of claim 23 , wherein said oxygenating gas comprises 90-100% (v/v) oxygen.25. The resuscitation kit of claim 23 , wherein said oxygenating gas comprises a mixture of oxygen claim 23 , hydrogen sulfide and carbon monoxide.26. The resuscitation kit of claim 22 , wherein said lipid based resuscitation fluid comprises a lipid emulsion comprising 20% (w/v) purified soybean oil claim 22 , 1.2% (w/v) purified egg phospholipids claim 22 , and 2.25% (w/v) glycerol anhydrous.27. The resuscitation kit of claim 26 , wherein said lipid based resuscitation fluid further comprises approximately 5% (w/v) albumin.28. The resuscitation kit of claim 22 , wherein said oxygenation device comprises an air pump.29. The resuscitation kit of claim 22 , further comprising an intravenous infusion (IV) set.30. The resuscitation kit of claim 22 , wherein said resuscitation fluid further comprises histidine.31. The resuscitation kit of claim 22 , wherein said resuscitation fluid further comprises histidine at a concentration of between 0.01M to 0.2M.32. The resuscitation kit of claim 22 , wherein said resuscitation fluid further comprises at least one additive selected from the group consisting of oncotic agents claim 22 , ...

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25-04-2013 дата публикации

METHODS FOR SELECTIVE SILENCING OF SENSORY NEURONS

Номер: US20130102680A1
Автор: Chuang Huai-hu
Принадлежит: CORNELL UNIVERSITY

The present invention relates to a method of treating hyperalgesia in a subject, which involves administering to a subject an amount of a TRPV1 agonist compound that selectively inhibits hyperactive nociceptive neurons. The present invention also relates to a method of selectively inhibiting hyperactive nociceptive neurons. Also disclosed is a method for reducing the electrical activity of hypersensitive neurons sensitized to TRPV1. The present invention also relates to a method for identifying candidate compounds that selectively inhibit hyperactive nociceptive neurons. Also disclosed is a pharmaceutical composition. 1. A method of treating hyperalgesia in a subject , said method comprising:administering to a subject an amount of a TRPV1 agonist compound, wherein the TRPV1 agonist compound selectively inhibits hyperactive nociceptive neurons in the subject under conditions effective to treat hyperalgesia in the subject.2. The method according to claim 1 , wherein said TRPV1 agonist compound induces Ca influx into a neural cell.3. The method according to claim 1 , wherein said TRPV1 agonist compound induces entry into hyperactive nociceptive neurons via the TRPVI pore of the TRPVI agonist itself and permanently charged Na channel blockers to suppress Na currents in sensory neurons.4. The method according to claim 1 , wherein said TRPV1 agonist compound enters hyperactive nociceptive neurons through an activated TRPV1 pore.5. The method according to claim 1 , wherein said TRPV1 agonist compound is a permeant blocker of the TRPV1 pore in hyperactive nociceptive neurons.6. The method according to claim 1 , wherein said TRPV1 agonist compound is impermeable to a plasma membrane of neurons.7. The method according to claim 1 , wherein said TRPV1 agonist compound is hydrophilic.8. The method according to claim 1 , wherein said TRPV1 agonist compound is a permanently charged capsaicin derivative.9. The method according to claim 8 , wherein said TRPV1 agonist compound is ...

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25-04-2013 дата публикации

Compositions and Methods for Inhibiting an Isoform of Human Manganese Superoxide Dismutase

Номер: US20130102681A1
Автор: Anziano Paul Q.
Принадлежит: Mito Tek, LLC

The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure. 153-. (canceled)54. A method of treating a mitochondrial related disease or condition in an individual comprising administering to the individual a therapeutically effective amount of an isoMnSOD inhibitor.55. The method of wherein said inhibitor comprises a compound of Formula I:{'br': None, 'sup': 1', '2, 'Alk-L-L-D\u2003\u2003I'} [{'sub': 2-100', '2-100, 'sup': '1', 'Alk is Calkenyl or Calkynyl, each optionally substituted by one or more R;'}, {'sup': 1', '2', '2', '2', '2', '2', '3', '2', '3, 'sub': 2', '2, 'Lis O, S, CO, C(O)O, C(O)NR, SO, S(O), S(O)NR, S(O)NR, NR, NRC(O)NR, or NRC(S)NR;'}, {'sup': 2', '4, 'sub': 1-6', '2-6', '2-6, 'Lis absent, Calkylenyl, Calkenylenyl, or Calkynylenyl, each optionally substituted by one or more R;'}, {'sup': '5', 'D is aryl or heteroaryl, each optionally substituted by one or more R;'}, {'sup': 1', '4', '6', '6', '6', '7', '7', '7', '8', '9', '8', '6, 'sub': 1-6', '1-6', '2-6', '2-6', '3-7', '2, 'Rand Rare each, independently, halo, cyano, nitro, Calkyl, Chaloalkyl, Calkenyl, Calkynyl, aryl, heteroaryl, Ccycloalkyl, heterocycloalkyl, S(O)R, S(O)R, C(O)R, OR, SR, C(O)OR, NRRor NRC(O)R;'}, {'sup': 2', '3, 'sub': 1-6', '2-6', '2-6', '1-6', '3-7', '3-7, 'Rand Rare each, independently, H, Calkyl, Calkenyl, Calkynyl, Chaloalkyl, aryl, heteroaryl, Ccycloalkyl, heterocycloalkyl, arylalkyl, heteroarylalkyl; (Ccycloalkyl)alkyl or heterocycloalkylalkyl;'}, {'sup': 5', '12', '12', '13', '14', '15', '12', '13', '14', '15', '14', '15', '14', '15', '14', '12', '13', '14', '15', '13', '14', '15, 'sub': 1-6', '2-6', '2-6', '1-4', '2', '2', '2, 'Ris halo, Calkyl, Calkenyl, Calkynyl, Chaloalkyl, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, CN, NO, OR, SR, C(O)R, C(O)NRR, C(O)OR, OC(O)R, OC(O)NRR, NRR, NRC(O)R, NRC(O)OR, S(O)R, S(O)NRR, S(O)R, or S(O)NRR;'}, ...

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25-04-2013 дата публикации

Substituted Tetracycline Compounds

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

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

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25-04-2013 дата публикации

PROCESS FOR PREPARING FORMAMIDES AND FORMIC ESTERS

Номер: US20130102807A1
Принадлежит: BASF SE

A process for preparing carboxylic acid derivatives of the formula H—(C═O)—R, R is ORor NRR, Ris optionally substituted C-C-alkyl, C-C-cycloalkyl, C-C-heterocyclyl, C-C-aryl or C-C-heteroaryl, substituents are C-C-alkyl, C-C-alkoxy, C-C-cycloalkyl or C-C-aryl; Rand Rare independently hydrogen or optionally substituted C-C-alkyl, C-Ccycloalkyl, C-C-heterocyclyl, C-C-aryl or C-C-heteroaryl, substituents are selected from the group consisting of C-C-alkyl, C-C-cycloalkyl and C-C-aryl or Rand Rtogether with the nitrogen atom form a five- or six-membered ring which optionally comprises one or more heteroatoms selected from O, S and N and bearing the substituent R, Ris hydrogen or C-C-alkyl; by reacting a reaction mixture comprising carbon dioxide, hydrogen and an alcohol of the formula R—OH or an amine of the formula NHRRin the presence of a catalyst comprising gold at a pressure from 0.2 to 30 MPa and a temperature from 20 to 200° C. in a hydrogenation reactor. 114.-. (canceled)15. A process for preparing carboxylic acid derivatives of the general formula (Ia){'br': None, 'H—(C═O)—R\u2003\u2003(Ia),'}where{'sup': 1', '2', '3, 'R is selected from the group consisting of ORand NRR, where'}{'sup': '1', 'sub': 1', '15', '5', '10', '5', '10', '5', '10', '5', '10, 'claim-text': {'sub': 1', '15', '1', '6', '5', '10', '5', '10, 'where the substituents are selected from the group consisting of C-C-alkyl, C-C-alkoxy, C-C-cycloalkyl and C-C-aryl;'}, 'Ris unsubstituted or at least monosubstituted C-C-alkyl, C-C-cycloalkyl, C-C-heterocyclyl, C-C-aryl or C-C-heteroaryl,'}{'sup': 2', '3, 'sub': 1', '15', '5', '10', '5', '10', '5', '10', '5', '10, 'claim-text': [{'sub': 1', '15', '5', '10', '5', '10, 'where the substituents are selected from the group consisting of C-C-alkyl, C-C-cycloalkyl and C-C-aryl'}, 'or', {'sup': 2', '3', '4, 'Rand Rtogether with the nitrogen atom form a five- or six-membered ring which optionally additionally comprises one or more heteroatoms selected from ...

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25-04-2013 дата публикации

PROCESS FOR THE PREPARATION OF LACOSAMIDE

Номер: US20130102811A1
Принадлежит: SUN PHARMACEUTICAL INDUSTRIES LTD

The present invention relates to a novel and improved process for the preparation of lacosamide, wherein the process is a sequential one-pot process. 2. The process as claimed in claim 1 , wherein all the reactions of step a) to d) are carried out in dicholormethane.3. The process as claimed in claim 1 , wherein the condensation of N-Boc-D-serine with benzylamine in step a) is performed using a coupling agent claim 1 , optionally in the presence of catalytic 1-hydroxybenzitriazole4. The process as claimed in claim 3 , wherein the coupling agent is selected from the group consisting of (benzotriazole- 1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate (BOP) claim 3 , is obutyl chloroformate claim 3 , N claim 3 ,N′-dicyclohexylcarbodiimide (DCC) and N-(3-dimethylaminopropyl)-N-ethylcarbodiimide(EDC).5. The process as claimed in claim 1 , wherein methylation of compound of formula I in step b) is carried out using a methylating agent in a biphasic system in presence of a phase transfer catalyst.6. The process as claimed in claim 5 , wherein the methylating agent is selected from the group consisting of dimethyl sulfate claim 5 , methyl triflate claim 5 , and trimethyl phosphate.7. The process as claimed in claim 6 , wherein the methylating agent is dimethyl sulfate.8. The process as claimed in claim 5 , wherein the aqueous phase of the biphasic system contains an inorganic base.9. The process as claimed in claim 8 , wherein the inorganic base is selected from an alkali metal hydroxide claim 8 , carbonate and bicarbonate.10. The process as claimed in claim 5 , wherein the phase transfer catalyst is selected from a quarternized amine salt or a phosphonium salt.11. The process as claimed in claim 10 , wherein quarternized amine salt is selected from the group consisting of sulfate claim 10 , chloride or bromide salts of tetraalkylammonium; benzyltrialkylammonium halides; cetyltrialkylammonium halides and Tweens (polyoxyethylene sorbitan esters) such as Tween®20 ...

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02-05-2013 дата публикации

C7-Fluoro Substituted Tetracycline Compounds

Номер: US20130109657A1
Принадлежит: Tetraphase Pharmaceuticals Inc

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

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02-05-2013 дата публикации

PHENYL-N-ACYL DERIVATIVES OF AMINES AND AMINO ACIDS, A PROCESS FOR THE PREPARATION THEREOF, A PHARMACEUTICAL COMPOSITION AND USE THEREOF

Номер: US20130109880A1

The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating. 2. The process according to claim 1 , wherein 1-1.2 equivalents of diphenylphosphorylazide and triethylamine are used.3. The process according to claim 1 , wherein as amino derivatives tyrosine or phenylalanine esters are used.43. The process according to any one of - claims 1 , wherein as an organic solvent N claims 1 ,N-dimethylformamide or ethylacetate are used.53. The process according to any one of - claims 1 , which is conducted at the temperature ranging from −25° C. to 0° C.7. The process according to claim 6 , wherein as amino derivatives tyrosine or phenylalanine esters are used. This application is a divisional of co-pending U.S. application Ser. No. 11/886,965, filed on Oct. 23, 2008, which is a U.S. National Stage application under 35 U.S.C. §371 of International Application PCT/RU2006/000139 (published as WO 2006/101422 A1), filed Mar. 24, 2006, which claims priority to Application RU 2005108492, filed Mar. 25, 2005. Benefit of the filing date of each of these prior applications is hereby claimed. Each of these prior applications is hereby incorporated by reference in its entirety.The present invention relates to the field of bioorganic chemistry and concerns novel compounds, phenyl-N-acyl derivatives of biogenic amines as well as a process for synthesis of novel and known ...

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09-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF 4-CARBONYL)AMINO]-3-FLUOROPHENOXY}-N-METHYLPYRIDINE-2-CARBOXAMIDE, ITS SALTS AND MONOHYDRATE

Номер: US20130116442A1
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a process for preparing 4-{4-[({[4-chloro-3-(trifluoromethyl)-phenyl]amino}carbonyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide, its salts and monohydrate. 2. The process of for preparing the monohydrate of the compound of the formula (I) wherein the salt of the compound of the formula (I) is then treated with an aqueous basic solution to precipitate the monohydrate of the compound of the formula (I).3. The process of wherein the monohydrate of the compound of the formula (I) precipitates at a temperature of from 35° C. to 45° C.4. The process of or for preparing of the compound of the formula (I) wherein the monohydrate is dried under reduced pressure until the compound of the formula (I) is formed.5. The process of any of to wherein the solution comprising the solved compound of the formula (I) and what from the salt of the compound of the formula (I) precipitates is the reaction mixture or is a separate solution of the compound of the formula (I) prepared after isolation of the compound of the formula (I) from the reaction mixture.6. The process of any of to wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture a protic substance and an acid precursor.7. The process of wherein the acid is generated in situ in the reaction mixture after the compound of the formula (I) is formed by adding to the reaction mixture an alcohol and an acylchloride.8. The process of wherein the alcohol is ethanol and the acylchloride is acetylchloride.11. The process of or wherein the compound of the formula (II) is used in a solution of a suitable organic solvent which solution is prepared by neutralization the hydrochloric acid salt of the compound of the formula (II) with a base.12. The process of any of to wherein the compound of the formula (II) it is solved in a suitable organic solvent claim 7 , treated with an acid which is generated in situ by ...

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16-05-2013 дата публикации

HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF

Номер: US20130121919A1

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

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16-05-2013 дата публикации

TUNABLE LCST POLYMERS AND METHODS OF PREPARATION

Номер: US20130123144A1
Автор: Huang Lihong, Putnam David
Принадлежит: CORNELL UNIVERSITY

Polymer compositions having the chemical structure: as well as monomer compositions for producing said polymers are described. Methods for preparing these polymers and combinatorial libraries of these polymers are also described. 212.-. (canceled)13. The monomer composition of claim 1 , wherein Ris a hydrogen atom or methyl group.14. The monomer composition of claim 1 , wherein subscript n represents an integer of at least 5.15. The monomer composition of claim 1 , wherein subscript m represents an integer of at least 1.16. (canceled)18. The monomer composition of claim 17 , wherein subscript n represents an integer of at least 4.19. The monomer composition of claim 17 , wherein subscript m represents an integer of at least 1.20. (canceled)21. The monomer composition of claim 17 , wherein Y represents an —O— group.22. The monomer composition of claim 17 , wherein Y represents an —S— group.23. The monomer composition of claim 17 , wherein Y represents an —NRR— group.25. The monomer composition of claim 24 , wherein X is —O—.26. The monomer composition of claim 24 , wherein X is —NR—.27. The monomer composition of claim 24 , wherein n is at least 2.28. (canceled)29. The monomer composition of claim 24 , wherein m is at least 1.31. The monomer composition of claim 30 , wherein X is —O—.32. The monomer composition of claim 30 , wherein X is —NR—.33. The monomer composition of claim 30 , wherein n is at least 2.34. (canceled)35. The monomer composition of claim 30 , wherein m is at least 1.36. The monomer composition of claim 30 , wherein at least one of R claim 30 , R claim 30 , and Ris a hydrocarbon group substituted by at least one hydrophilic group.37. The monomer composition of claim 36 , wherein said at least one hydrophilic group is selected from the group consisting of amino claim 36 , imino claim 36 , amido claim 36 , hydroxyl claim 36 , ether claim 36 , polyether claim 36 , carboxyl claim 36 , ester claim 36 , carbamato claim 36 , ureido claim 36 , aldehydro ...

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16-05-2013 дата публикации

AZETIDINYL DIAMIDES AS MONOACYLGLYCEROL LIPASE INHIBITORS

Номер: US20130123233A1
Принадлежит: Janssen Pharmaceutica NV

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: 117.-. (canceled)19. A pharmaceutical composition comprising a compound of and at least one of a pharmaceutically acceptable carrier claim 18 , a pharmaceutically acceptable excipient and a pharmaceutically acceptable diluent.20. A pharmaceutical composition of claim 19 , wherein the composition is a solid oral dosage form.21. A pharmaceutical composition of claim 19 , wherein the composition is a syrup claim 19 , an elixir or a suspension. This application claims priority to U.S. provisional patent application Nos. 61/171,658 and 61/171,649, each filed Apr. 22, 2009, which are hereby incorporated by reference in their entirety.The research and development of the invention described below was not federally sponsored.has been used for the treatment of pain for many years. Δ-tetrahydrocannabinol is a major active ingredient from and an agonist of cannabinoid receptors (Pertwee, 2008, 153, 199-215). Two cannabinoid G protein-coupled receptors have been cloned, cannabinoid receptor type 1 (CBMatsuda et al., Nature, 1990, 346, 561-4) and cannabinoid receptor type 2 (CBMunro et al., 1993, 365, 61-5). CBis expressed centrally in brain areas, such as the hypothalamus and nucleus accumbens as well as peripherally in the liver, gastrointestinal tract, pancreas, adipose tissue, and skeletal muscle (Di Marzo et al., 2007, 18, 129-140). CBis predominantly expressed in immune cells, such as monocytes (Pacher et al., 2008, 294, H1133-H1134), and under certain conditions, also in the brain (Benito et al., 2008, 153, 277-285) and in skeletal (Cavuoto et al., 2007, 364, 105-110) and cardiac (Hajrasouliha et al., 2008, 579, 246-252) muscle. An abundance of pharmacological, anatomical and electrophysiological data, using synthetic agonists, indicate that increased cannabinoid signaling through CB/ ...

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16-05-2013 дата публикации

MODULATOR

Номер: US20130123356A1
Принадлежит: UNIVERSITY COLLEGE LONDON

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, 2. A compound according to wherein Y is selected from CN claim 1 , OH claim 1 , COOR claim 1 , SONRR claim 1 , CONRR claim 1 , where each of Rand Ris independently H or a hydrocarbyl group.3. A compound according to wherein each of R claim 1 , R claim 1 , Rand Ris independently H claim 1 , an alkyl group claim 1 , an aryl group claim 1 , or a cycloalkyl group claim 1 , each of which may be optionally substituted.4. A compound according to wherein Y is selected from OH claim 1 , CN claim 1 , COOR claim 1 , CONRR claim 1 , where each of Rand Ris independently H or an optionally substituted alkyl group.5. A compound according to wherein Y is selected from OH claim 1 , CN claim 1 , COOMe claim 1 , COOH claim 1 , CONH claim 1 , CONHMe and CONMe.6. A compound according to wherein X—Y is selected from{'br': None, 'sub': 2', 'p, '—C≡C—(CH)—Y'}{'br': None, 'sup': 5', '6, 'sub': 2', 'q, '—C(R)═C(R)—(CH)—Y; and'}{'br': None, 'i': 'r', '—C(R5)(R6)C(R8)-(CH2)-Y;'}{'sup': 5', '6', '7', '8, 'wherein each of R, R, R, and Ris independently H or alkyl, and each of p, q and r is independently 2, 3, or 4.'}7. A compound according to wherein X—Y is selected from{'br': None, 'sub': 2', 'p, '—C≡C—(CH)—Y; and'}{'br': None, 'sub': 2', 'q, '—CH═CH—(CH)—Y;'}wherein each of p and q is independently 2, 3 or 4.8. A compound according to wherein X—Y is{'br': None, 'sup': 5', '6, 'sub': 2', 'q, 'i': 'q', 'cis-C(R)═C(R)—(CH)—Y and is 2, 3 or 4.'}9. A compound according to wherein X—Y is —C(Me)-CH—(CH)—Y and r is 2 claim 1 , 3 or 4.10. A compound according to wherein A is phenyl.11. A compound according to wherein Z is ORor NRRand each of Rand Ris independently H claim 1 , an alkyl or a cycloalkyl group claim 1 , each of which may be optionally substituted by one or more OH or halogen groups.12. A compound according to wherein Z is selected from OH claim 1 , OEt claim 1 , NHCHCHF claim 1 , NH- ...

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16-05-2013 дата публикации

CATIONIC LIPIDS, METHODS FOR PREPARING THE SAME, AND DELIVERY SYSTEMS HAVING ABILITY TO TRANSITION INTO CELLS COMPRISING THE SAME

Номер: US20130123485A1
Принадлежит:

The present invention provides cationic lipids, methods for preparing the same, and delivery systems comprising the same. The present invention can provide cationic lipids which enhance the efficiency of intracellular or in vivo delivery of multiple-anionic target compounds such as drugs, anticancer agents, nucleic acids, etc., have no intracellular toxicity, but show increased stability, methods for preparing the same, and delivery systems comprising the same. 2. The cationic lipid according to claim 1 , wherein each of Rand Ris independently saturated or unsaturated hydrocarbon chain derived from stearate claim 1 , laurate claim 1 , myristate claim 1 , palmitate claim 1 , or oleate.3. The cationic lipid according to claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , or benzyl.4. The cationic lipid of claim 1 , wherein the ligand is mPEG (methoxy end-capped polyethylene glycol) claim 1 , polypropylene glycol claim 1 , or polyoxyethylene.5. The cationic lipid of claim 1 , wherein the ligand is at least one sugar selected from the group consisting of mannitol claim 1 , sorbitol claim 1 , xylitol claim 1 , glucitol claim 1 , dulcitol claim 1 , inositol claim 1 , arabinitol claim 1 , arabitol claim 1 , galactitol claim 1 , iditol claim 1 , alitol claim 1 , fructose claim 1 , sorbose claim 1 , glucose claim 1 , mannose claim 1 , xylose claim 1 , trehalose claim 1 , allose claim 1 , dextrose claim 1 , altrose claim 1 , gulose claim 1 , idose claim 1 , galactose claim 1 , talose claim 1 , ribose claim 1 , arabinose claim 1 , lyxose claim 1 , sucrose claim 1 , maltose claim 1 , lactose claim 1 , lactulose claim 1 , fucose claim 1 , rhamnose claim 1 , melezitose claim 1 , maltotriose claim 1 , and raffinose.7. The delivery system according to claim 6 , wherein each of Rand Ris independently saturated or unsaturated hydrocarbon chain derived from stearate claim 6 , laurate claim 6 , myristate claim 6 , palmitate ...

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16-05-2013 дата публикации

METHOD FOR SYNTHESIZING RARE EARTH METAL EXTRACTANT

Номер: US20130123534A1
Принадлежит:

A rare earth metal extractant containing, as the extractant component, dialkyldiglycol amide acid which is excellent in breaking down light rare earth elements is reacted in diglycolic acid (X mol) and an esterification agent (Y mol) at a reaction temperature of 70° C. or more and for a reaction time of one hour or more such that the mol ratio of Y/X is 2.5 or more, and is subjected to vacuum concentration. Subsequently, a reaction intermediate product is obtained by removing unreacted products and reaction residue. Then a nonpolar or low-polar solvent which is an organic solvent for forming an organic phase during solvent extraction of the rare earth metal and which is capable of dissolving dialkyldiglycol amide acid is added as the reaction solvent, and the reaction intermediate product is reacted with dialkyl amine (Z mol) such that the mol ratio of Z/X is 0.9 or more. 2. A method for synthesizing a rare earth metal extractant according to wherein the esterifying agent is selected from acetic anhydride and trifluoroacetic anhydride.3. A method for synthesizing a rare earth metal extractant according to wherein the organic solvent to form an organic phase during solvent extraction of rare earth metals is selected from the group consisting of toluene claim 1 , xylene claim 1 , hexane claim 1 , isododecane claim 1 , kerosene claim 1 , and higher alcohols.4. A method for synthesizing a rare earth metal extractant according to wherein in the step of reacting diglycolic acid with an esterifying agent claim 1 , the molar ratio of Y/X is in the range: 2.5≦Y/X≦6.5.5. A method for synthesizing a rare earth metal extractant wherein in the step of reacting the reaction intermediate product with a dialkylamine claim 1 , the molar ratio of Z/X is in the range: 0.9≦Z/X≦1.2.6. A method for synthesizing a rare earth metal extractant wherein the reaction solvent is added in such an amount that the dialkyl diglycol amic acid formed after the reactions may be present in a ...

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16-05-2013 дата публикации

Beta-Ketocarbonylquat Compounds and Process for the Preparation thereof

Номер: US20130123535A1
Автор: Herzig Christian
Принадлежит: Wacker Chemie AG

β-ketocarbonylquats contain at least one quaternary ammonium salt group, and may be prepared by the reaction of an alkyl ketene dimer with a tertiary amine group-containing compound also containing a protic group, followed by quaternization. 18.-. (canceled)9. A β-ketocarbonylquat comprising one or more β-ketocarbonyl groups of general formula{'br': None, 'sub': '2', 'R—CH—(C═O)—CHR—(C═O)—\u2003\u2003(I)'}and one or more quaternary ammonium groups, whereinR each, independently, is an aliphatic hydrocarbon radical of 6 to 28 carbon atoms, with the proviso that the β-ketocarbonyl group of formula (I) is bonded to a radical Y, wherein{'sup': '1', 'Y is a divalent radical of the formula —O—, —NH—, —NR—, and'}{'sup': '1', 'Ris a monovalent hydrocarbon radical of 1 to 30 carbon atoms.'}10. The β-ketocarbonylquat of claim 9 , wherein the aliphatic hydrocarbon radical R contains 10-26 carbon atoms.11. The β-ketocarbonylquat of claim 9 , wherein the aliphatic hydrocarbon radical R contains 12-20 carbon atoms.12. The β-ketocarbonylquat of claim 9 , wherein Y is —NH— claim 9 , —NR— claim 9 , or a trivalent radical of the formula =N—.13. The β-ketocarbonylquat of claim 9 , wherein Rcontains 1-18 carbon atoms.14. The β-ketocarbonylquat of claim 9 , having the formula{'br': None, 'sup': 3', '4', '5', '(+)', '2', '(−), 'sub': 'a', '[RRRN—R—]Y—Z X\u2003\u2003(II)'}whereina is 1 or 2, with the proviso that when a is 1, Y is a divalent radical and when a is 2, Y is a trivalent radical,{'sup': '1', 'Y is a divalent radical of formula —O—, —NH—, —NR—, or a trivalent radical of formula =N—,'}{'sup': '(−)', 'Xis a counter-ion to the positive charge on the quaternary nitrogen atom,'} {'br': None, 'sub': '2', 'R—CH—(C═O)—CHR—(C═O)—\u2003\u2003(I)'}, 'Z is a β-ketocarbonyl group of the formula'}R each, independently is an aliphatic hydrocarbon radical of 6 to 28 carbon atoms,{'sup': '1', 'Ris a monovalent hydrocarbon radical of 1 to 30 carbon atoms,'}{'sup': '2', 'sub': 1', '18, 'Ris a ...

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16-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF LACOSAMIDE

Номер: US20130123537A1
Принадлежит:

The present invention relates to an improved process for the preparation of Lacosamide of Formula (I), comprising: O-methylating a compound of Formula (V) or a compound of Formula (XX) or a compound of Formula XXII; in the presence of a methylating agent and a base to produce Lacosamide of Formula (I). 2. The process according to claim 1 , wherein the methylating agent used in O-methylation step is selected from methyl iodide claim 1 , methyl chloride claim 1 , methyl bromide claim 1 , methyl fluoride claim 1 , dimethyl sulfate claim 1 , trimethyl silyldiazomethane claim 1 , dimethyl sulfoxide (DMSO) or mixtures thereof.3. The process according to claim 1 , wherein the base used in O-methylation step is selected from sodium hydroxide claim 1 , potassium hydroxide claim 1 , sodium carbonate claim 1 , potassium carbonate claim 1 , sodium bicarbonate claim 1 , potassium bicarbonate or mixtures thereof.4. The process according to claim 1 , wherein the O-methylation is carried out in the presence of a solvent selected from tetrahydrofuran (THF) claim 1 , dichloromethane (MDC) claim 1 , dimethyl sulfoxide (DMSO) claim 1 , acetonitrile (MeCN) claim 1 , ethyl acetate claim 1 , acetone claim 1 , monoglyme claim 1 , diglyme or mixtures thereof.5. The process according to claim 1 , wherein the O-methylation is optionally carried out in the presence of a phase transfer catalyst (PTC) selected from tetraethylammonium-p-toluenesulfonate claim 1 , tetrapropylammonium trifluoromethane sulfonate claim 1 , tetraphenylphosphonium hexafluoroantimonate claim 1 , acetylpyridinium bromide claim 1 , triphenylmethyl triphenylphosponium chloride claim 1 , benzyltriethylammonium chloride claim 1 , benzyltrimethylammonium chloride claim 1 , benzyltriphenylphosphonium chloride claim 1 , benzytributylammonium chloride claim 1 , butyltriethylammonium bromide claim 1 , butyltriphenylphosphonium bromide claim 1 , cetyltrimethyl ammonium bromide claim 1 , cetyltrimethyl ammonium chloride claim 1 , ...

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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.

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23-05-2013 дата публикации

NOVEL CATIONIC AMPHIPHILES WITH MANNOSE-MIMICKING HEAD-GROUPS AND A PROCESS FOR THE PREPARATION THEREOF

Номер: US20130129758A1

The present invention discloses novel cationic amphiphiles containing mannose-mimicking shikimic and quinic acid head-groups and a process for preparing cationic amphiphiles with mannose-mimicking polar head-groups such as, shikimic and quinic acids. The findings described herein also demonstrate that compounds of the present invention can target model DNA vaccines to antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs), via mannose receptors expressed on the cell surface of APCs. The cationic amphiphiles disclosed herein show enhanced cellular and humoral immune response compared to their mannosyl counterpart in dendritic cell (DC, the most professional APC) based genetic immunization in mice. Cationic amphiphiles with mannose-mimicking quinic and shikimic acid head-groups described in the present invention are likely to find future applications in the field of genetic immunization. 3. The cationic amphiphile of claim 1 , wherein lipophilic Rand Rmoiety is selected from the group consisting of saturated C-Calkyl groups and unsaturated C-Calkenyl groups containing 1 claim 1 , 2 or 3 double bonds.5. The process of claim 4 , wherein saturated or unsaturated aliphatic hydrocarbon chains of said amine have 8-22 carbon atoms.6. The process of claim 4 , wherein the polar aprotic solvent used in step (a) is selected from the group consisting of dichloro methane (DCM) claim 4 , dimethyl formamide (DMF) claim 4 , dimethylsulfoxide claim 4 , pyridine claim 4 , and triethyl amine.7. The process of claim 4 , wherein quaternization of the intermediate hydrophobic amide obtained in step (a) is carried out at a temperature between 25-30° C.8. The process of claim 4 , wherein the organic solvent used as polar eluent in step (c) is selected from the group consisting of methanol claim 4 , ethanol claim 4 , chloroform claim 4 , dichloro methane and ethyl acetate.9. The process of claim 4 , wherein the halide ion exchange resins used in step (c) is selected ...

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23-05-2013 дата публикации

TOPICAL TREATMENT FOR CHEMOTHERAPY INDUCED EYELASH LOSS OR HYPOTRICHOSIS USING PROSTAMIDE F2 ALPHA AGONISTS

Номер: US20130131097A1
Принадлежит: ALLERGAN, INC.

The present invention is directed to compositions and methods for the treatment of post-chemotherapeutic hypotrichosis. More specifically, the present invention is directed to the use of compositions comprising bimatoprost for the treatment of post-chemotherapeutic hypotrichosis which may be applied before, during and after receiving chemotherapeutic treatment. 1) A method of growing eyelashes in chemotherapy patients , the method comprising applying 0.03% w/v bimatoprost to the eyelids before , during , or after chemotherapeutic treatment.2) The method of claim 1 , wherein the 0.03% bimatoprost is applied at least once a day.3) The method of and claim 1 , wherein the method results in eyelashes which are longer claim 1 , thicker or darker compared to patients receiving no treatment.4) The method of claim 2 , wherein the method is applied for at least 6 months after completing chemotherapeutic treatment.5) The method of claim 4 , wherein the method is applied for at least 12 months after completing chemotherapeutic treatment.6) The method of claim 3 , wherein the number of eyelashes increases in comparison to post-chemotherapeutic patients who received no treatment.7) The method of claim 1 , wherein the bimatoprost is added during and after post-chemotherapeutic treatment.8) The method of claim 2 , wherein the method is applied twice a day.9) The method of claim 8 , wherein the bimatoprost is applied to the upper and lower eyelid margin of each eye.10) The method of claim 1 , wherein the method effectively treats post-chemotherapeutic hypotrichosis.11) The method of claim 1 , further comprising the step of administering one selected from the group consisting of Minoxidil® and Propecia®.12) The method of claim 1 , wherein the method results in lower incidence of conjunctival hyperemia claim 1 , punctate keratitis claim 1 , erythema of the eyelid claim 1 , eye pruritis and skin hyperpigmentation than in patients receiving 0.03% w/v bimatoprost for treatment of ...

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23-05-2013 дата публикации

Fluro substituted Omega-Carboxyaryl Diphenyl Urea for the Treatment and Prevention of Diseases and Conditions

Номер: US20130131122A1
Принадлежит: Bayer HealthCare LLC

A compound of Formula (I): 154-. (canceled)562. A compound claim where the methylamide group is substituted with a hydroxyl group.571. A pharmaceutical composition comprising a compound of claim and a physiologically acceptable carrier.581. A pharmaceutical composition for the treatment of a cancerous cell growth comprising a compound of claim and a physiologically acceptable carrier for treating cancer.605. A compound claim where either urea nitrogen atom of the compound of formula I is substituted with a hydroxyl group.627. A compound claim where the pyridine nitrogen atom is in the n-oxide form and the methylamide functionality is substituted with a hydroxyl group. This application is a continuation application of U.S. application Ser. No. 10/895,985 filed Jul. 22, 2004 which claims the benefit of the filing date of U.S. Provisional Application Ser. No. 60/489,102 filed Jul. 23, 2003 and U.S. Provisional Application Ser. No. 60/540,326 filed Feb. 2, 2004.This invention relates to novel compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating diseases and conditions mediated by abnormal VEGFR, PDGFR, raf, p38, and/or flt-3 kinase signaling, either alone or in combination with anti-cancer agents.Activation of the ras signal transduction pathway indicates a cascade of events that have a profound impact on cellular proliferation, differentiation, and transformation. Raf kinase, a downstream effector of ras, is recognized as a key mediator of these signals from cell surface receptors to the cell nucleus (Lowy, D. R.; Willumsen, B. M. 1993, 62, 851; Bos, J. L. 1989, 49, 4682). It has been shown that inhibiting the effect of active ras by inhibiting the raf kinase signaling pathway by administration of deactivating antibodies to raf kinase or by co-expression of dominant negative raf kinase or dominant negative MEK, the substrate of raf kinase, leads to the reversion of transformed cells to the normal ...

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23-05-2013 дата публикации

Process For The Preparation Of Contrast Agents

Номер: US20130131382A1
Принадлежит: BRACCO IMAGING S.P.A.

The present invention relates to a process for the preparation of 5-[(2-hydroxyacyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamidic derivatives comprising the Smiles rearrangement of a suitable precursor, by contact of an aqueous solution of this latter with an anion exchanger solid phase. 4. The process according to claim 1 , wherein the anion exchanger solid phase is a weak anion exchanger resin or a strong anion exchanger resin.5. The process according to any one of or claim 1 , wherein the anion exchanger solid phase is selected from: Amberlite® IRA 400 and Purolite® A830.6. The process according to wherein the aqueous solvent is water.7. The process according to claim 1 , wherein the pH of the reaction is comprised from 6 to 9.9. The process according to claim 8 , wherein the compound of formula (3) is:(R)-2-[[(4-nitrophenyl)sulfonyl)]oxy]propanamide; or2-[[(4-notrophenyl)sulfonyl)]oxy]ethanamide.10. The process according to any one of or claim 8 , wherein the solvent is a mixture of water/dioxane in a ratio of 3:1 by weight. The present invention relates in general to a process for the preparation of 5-[(2-hydroxyacyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamidic derivatives, useful as contrast agents in diagnostic techniques.Contrast agents or contrast media, are substances that can alter the way in which a region is analyzed in medical imaging. In particular, they are able to change the contrast of an organ, an injury, or any other surrounding structure, to make visible such details that otherwise would be difficult to detect or appreciate.Contrast agents are primarily used in the radiological or in the nuclear magnetic resonance diagnostic fields. Depending on the field of application, these derivatives present structural features, such as, in the case of molecules useful as contrast agents for X-rays analysis, the presence of one or more atom with high atomic number (e.g. iodine or barium). Iopamidol (N,N′-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2S)(2- ...

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30-05-2013 дата публикации

PANTHENYL DOCOSAHEXAENEOATE AND ITS USE FOR TREATING AND PREVENTING CARDIOVASCULAR DISEASES

Номер: US20130137768A1
Принадлежит: PIERRE FABRE MEDICAMENT

The present invention relates to the docosahexaenoatepanthenyl of the following formula: It also relates to a method for preparing same and to a pharmaceutical composition comprising same and to the use of same in the treatment or the prevention of cardiovascular diseases, in particular atrial fibrillation. 3. A method for treating a subject in need thereof , comprising the use of an ester as defined in or .4. A pharmaceutical composition comprising the ester of or and a pharmaceutically acceptable excipient.5. A method for preventing and/or treating cardiovascular diseases selected or derived from: auricular , ventricular arrhythmia , tachycardia , fibrillation , diseases represented by defects in electrical conduction in myocardial cells , multiple risk factors for cardiovascular disease selected from: hypertriglyceridemia , hypercholesterolemia , and hypertension , comprising the administration of an effective amount of the ester of or or of the composition of .6. The method of claim 5 , wherein said cardiovascular disease is atrial fibrillation.7. A method for preparing the ester of or claim 5 , comprising the following steps:a) Selective protection of two OH functional groups of panthenol or of D-panthenol by an O-protective group,b) Esterification of the unprotected OH functional group by DHA in the presence of 1-[(1H-imidazol-1-yl)carbonyl]-1H-imidazol and N,N-dimethylpyridin-4-amine,c) Deprotection of the two protected OH functional groups.8. The method of claim 5 , wherein said cardiovascular disease is selected from: refractory arterial hypertension claim 5 , hyperlipidemia claim 5 , and dyslipidemia.9. The method of claim 5 , wherein said cardiovascular disease is mixed dyslipidemia.10. The method of claim 5 , wherein said cardiovascular disease is selected from: sudden death and post-infarction treatment.11. The method of claim 7 , wherein said O-protective group is trimethylchlorosilane. The present invention relates to a monoester of docosahexaenoic ...

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30-05-2013 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF SYSTEMIC AA AMYLOID DISEASES

Номер: US20130137775A1
Принадлежит:

Bis- and tris-dihydroxyaryl compounds their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially AA amyloidosis, and the manufacture of medicaments for such treatment. 1. A pharmaceutical composition comprising 3 ,4-dihydroxybenzoic acid 3 ,4-dihydroxyathlide , an oil and a surfactant.2. The composition of wherein the oil is mixture of Capryol 90 and Labrafac PG.3. The composition of wherein the surfactant is a mixture of Labrasol and Solutol HS 15.4. The composition of where the proportion of oil to surfactant is 30%:70%.5. A method of treating the formation claim 1 , deposition claim 1 , accumulation claim 1 , or persistence of AA amyloid fibrils claim 1 , comprising treating the fibrils with an effective amount of the composition of .6. A method of inhibiting and/or relieving an AA amyloid disease in a mammal suffering therefrom claim 1 , comprising administration to the mammal of a therapeutically effective amount of the composition of .7. The method of claim 1 , wherein the mammal is a human.8. The method of claim 1 , wherein the amount of the composition administered is between 1 mg/Kg/day and 100 mg/Kg/day.9. The method of claim 1 , wherein the amount of composition administered is between 10 mg/Kg/day and 50 mg/Kg/day. This application claims priority under 35 USC 119(e) to U.S. Provisional Application No. 61/592,117 filed Jan. 30, 2012.This application is a continuation-in-part of U.S. application Ser. No. 13/413,417 filed Mar 6, 2012 which is a continuation-in-part of 12/837,721 filed Jul. 16, 2010, now U.S. Pat. No. 8,163,957, issued on Apr. 24, 2012, which claimed the benefit of priority under 35 U.S.C. §120 to, and was a continuation of U.S. application Ser. No. 12/269,017, filed Nov. 11, 2008, now abandoned, which is a continuation of U.S. application Ser. No. 10/452,851, filed May 30, 2003, now a U.S. Pat. No. 7,514,583, issued on Apr. 7, 2009, which claims priority under 35 USC 119(e) ...

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30-05-2013 дата публикации

PROCESS FOR THE PREPARATION OF LINEZOLID

Номер: US20130137864A1
Принадлежит:

The present invention provides an improved process for the preparation of Linezolid of formula (D. The present invention relates to preparation of intermediate (R)—N-[[3-[3-fluoro-4-morpholinyl]phenyl|-2-oxo-5-oxazolidinyl]methanol of formula (II), Linezolid amine of formula (Ia) and their use in the preparation of Linezolid. The present invention further provides process for the preparation of Form I of Linezolid of formula (I). 3. The method of or , wherein said suitable solvent is tetrahydrofuran.4. (canceled)7. The method of or , wherein said acylating agent is acetic anhydride or acetyl chloride.8. The method of or , wherein said ketonic solvent is acetone , methyl iso-butyl ketone , methyl ethyl ketone , or a mixture thereof.9. The method of claim 6 , wherein said crystallization is carried out in n-propanol or methyl iso-butyl ketone.10. A Linezolid of formula (I) obtained by the method of or claim 6 , having content of (R)-enantiomer less than about 0.1% and content of bis-Linezolid less than about 0.15%.11. A Linezolid of formula (I) obtained by the method of or claim 6 , having purity greater than 99%. The present invention provides an improved process for the preparation of Linezolid of formula (I).The present invention relates to preparation of intermediate (R)—N—[[3-[3-fluoro-4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methanol of formula (II), Linezolid amine of formula (Ia) and their use in the preparation of Linezolid.The present invention further provides process for the preparation of Form I of Linezolid of formula (I).Linezolid is chemically known as N—[[(5S)-3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide and marketed by Pfizer in US under brand name Zyvox. Linezolid is a synthetic antibacterial agent of the oxazolidinone class. It is used for the treatment of infections caused by multi-resistant bacteria including streptococci and methicillin-resistantLinezolid was first disclosed in U.S. Pat. No. 5,688,792. The process ...

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06-06-2013 дата публикации

BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS

Номер: US20130143926A1
Принадлежит:

The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R, R, R, R, R, Rand Rare as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90. 2. A compound as claimed in wherein Ris hydroxy.3. A compound as claimed in wherein R claim 1 , R claim 1 , Rand Rare the same or different and represent hydrogen or halogen atoms or hydroxy claim 1 , unsubstituted Calkyl or unsubstituted Calkoxy groups.4. A compound as claimed in wherein either:{'sup': 6', '7', '8', '9', '8', '9, 'sub': 3', '1-4', '1-4, '(i) Rrepresents —CH, Rrepresents —CRR-A wherein Rand Rare the same or different and represent a hydrogen or halogen atom or an unsubstituted Calkyl or Calkoxy group, and A represents a phenyl ring substituted with a group W; or'}{'sup': 6', '7, 'sub': 1-4', '1-4', '1-4', '1-4', '1-4', '1-2, '(ii) Rand R, together with the nitrogen atom to which they are bonded, form a pyrrolidinyl, piperidinyl or isoindolinyl group which is substituted with a group W and is optionally further substituted with 1 or 2 groups which are the same or different and are selected from halogen atoms and unsubstituted Calkyl, Calkoxy, hydroxyl, Chaloalkyl, Chaloalkoxy, Chydroxyalkyl, cyano, nitro, —SR′ and —NR′R″ groups where R′ and R″ are the same or different and represent hydrogen or unsubstituted Calkyl.'}5. A compound as claimed in wherein Alkrepresents a bond claim 1 , an unsubstituted Calkylene group claim 1 , or an unsubstituted —(Calkylene)-NH—(Calkylene)- group.6. A compound as claimed in wherein either:{'sup': 12', '13, 'sub': 1-6', '3-7', '6-10', '1-4', '6-10', '1-4', '3-7, '(i) Rand Rare the same or different and represent hydrogen, Calkyl, Ccarbocyclyl, Caryl, —(Calkyl)-(Caryl), or —(Calkyl)-(Ccarbocyclyl); or'}{'sup': 12', '13, 'sub': '3-7', '(ii) Rand R, together with the carbon atom to which they are bonded, ...

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06-06-2013 дата публикации

TARGETED CORRECTION OF A GENETIC DEFECT IN CANCER THERAPY

Номер: US20130143933A1
Принадлежит: TRT Pharma Inc.

The present document describes a cancer mutation-selective chemosensitizer that comprise compounds for restoring association between mutated keap1 protein and Nrf2 protein, and inhibition of Nrf2 functions. The present document also describes composition of matter containing the compounds, as well as methods of medical treatment for treating diseases such as cancer with the compounds. 3. The mutation-selective chemosensitizer of claim 1 , wherein said compound corrects a Keap1 mutation to restore interaction between a mutated Keap1 protein and said Nrf2 protein.10. A pharmaceutical composition for the inhibition of a Nrf2 protein which comprises a therapeutically effective amount of a compound of formula (I) as defined in claim 1 , in association with a pharmaceutically acceptable carrier.11. A pharmaceutical composition for overcoming drug resistance in cancer chemotherapy and for the inhibition of tumor growth which comprises a therapeutically effective amount of a compound of formula (I) as defined in claim 1 , in association with a pharmaceutically acceptable carrier.12. A method of treating and/or preventing a disease which involves the abnormal activation or expression of a Nrf2 protein comprising administering a therapeutically effective amount of the compound of formula (I) as defined in of .13. A method of treating a cancer in a subject in need thereof comprising administering a therapeutically effective amount of a compound of formula (I) as defined in of .14. The method of claims 13 , wherein said cancer is chosen from liver cancer claims 13 , lung cancer claims 13 , breast cancer claims 13 , prostate cancer claims 13 , colon cancer claims 13 , neuroblastoma or leukemia. This application claims priority of U.S. provisional patent application U.S. 61/557,646, filed 9 Nov. 2011, the specification of which is hereby incorporated by reference.(a) FieldThe subject matter disclosed generally relates to a mutation-selective chemosensitizer for overcoming ...

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06-06-2013 дата публикации

PROCESS FOR RAPID IDENTIFICATION AND PREPARATION OF CRYSTALLINE FORMS

Номер: US20130144077A1
Принадлежит: ALLERGAN, INC.

Disclosed is a method of rapid identification and preparation of a crystalline form of an organic compound by using sub-gram level of said organic compound, comprising the steps of temperature-cycled slurrying, cooling, antisolvent addition and solvent evaporation as the major crystallization steps. 1. A process for the rapid identification and preparation of a crystalline form of an organic compound by using sub-gram level of said organic compound , said process comprising the steps of temperature-cycled slurrying , cooling , antisolvent addition and solvent evaporation as the major crystallization steps.2. The process of claim 1 , which comprising the steps of:(a) Conducting an initial x-ray powder diffraction (XRPD) analysis of a starting sample of said organic compound; thereafter(b) Conducting an initial visual solubility estimation of the organic compound in each of several solvents or a mixture of solvents thereof at ambient or room temperature; thereafter(c) Conducting a solubility estimation of the organic compound in each of a subset of the several solvents of step (b) or a mixture of said solvents at elevated temperature by subjecting a suspension or emulsion of the organic compound in said solvent or solvent mixture to temperature-cycled slurrying for a fixed period of time; and thereafter performing any one of: i) steps (d1) through (d5), (e1), (e2) and (f4); ii) steps (f1) through (f4); iii) steps (d1), (e1), (e2) and (f4); iv) steps (d1), (d2), (e1), (e2) and (f4); and (v) steps (d1) through (d4), (e1), (e2) and (f4) set forth below:(d1) If the sample of the organic compound and solvent/solvent mixture from step (c) remains a clear solution, then cooling the solution of said organic compound in said solvent or solvent mixture to a temperature of about 3° C. to about 6° C. and maintaining said solution at said temperature for a fixed period of time to induce super saturation;(d2) If the sample of the organic compound and the solvent/solvent mixture is ...

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13-06-2013 дата публикации

RATIONALLY IMPROVED ISONIAZID AND ETHIONAMIDE DERIVATIVES AND ACTIVITY THROUGH SELECTIVE ISOTOPIC SUBSTITUTION

Номер: US20130150415A1
Принадлежит:

The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including 144-. (canceled)46. The method according to wherein said NHNHgroup is isotopically labeled with two N atoms.47. The method according to wherein said compound contains at least one isotopically labeled atom selected from the group consisting of carbon-13 claim 45 , nitrogen-15 claim 45 , oxygen-17 and oxygen-18 in the exocyclic acyl hydrazide moiety of the compound.49. The method according to wherein said compound has an isotopically labeled carbon-13 claim 45 , oxygen-17 or oxygen-18 atom.50. The method according to wherein said compound has an isotopically labeled carbon-13 atom.51. The method according to wherein said compound has an isotopically labeled oxygen-17 atom.52. The method according to wherein said compound has an isotopically labeled oxygen-18 atom.53. The method according to wherein said compound has an isotopically labeled carbon-13 atom and an isotopically labeled oxygen-18 atom.54. The method according to wherein said compound has an isotopically labeled nitrogen-15 atom.55MycobacteriumMycobacterium tuberculosis.. The method according to wherein said infection is56. The method according to wherein said infection is latent.57. The method according to wherein said infection is active.58. The method according to wherein said infection is miliary.59. The method according to wherein said infection is extrapulmonary.60. The method according to wherein said infection is renal.62. The method according to wherein said compound is administered in pulmonary dosage form.63. The method according to wherein said compound is administered is oral dosage form.64. The method according to wherein said compound is administered in parenteral dosage form. This application claims the benefit of priority of U.S. provisional application Ser. No. 61/127,150, filed May 9, 2008 ...

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13-06-2013 дата публикации

PROLINE SULFONAMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS

Номер: US20130150424A1
Принадлежит: ACTELION PHARMACEUTICALS LTD.

The present invention relates to (S)-proline sulfonamide compounds of formula (I) 2. A method according to claim 1 , wherein{'sup': '1', 'Rrepresents a group selected from the group consisting of 5-bromo-thiophen-2-yl, 4-chloro-phenyl, 3-chloro-phenyl, 4-bromo-phenyl, 3-bromo-phenyl, 3-chloro-4-methyl-phenyl, 2-bromo-4-methyl-phenyl, 4-bromo-2-methyl-phenyl, 4-vinyl-phenyl, 2,4-dimethylphenyl, 3,4-dichloro-phenyl, 4-bromo-2-chloro-phenyl, 3-methoxy-phenyl, 4-methoxy-phenyl, 4-chloro-2,5-dimethyl-phenyl, 4-n-propyl-phenyl, 2-methoxy-4-methyl-phenyl, 2-methoxy-5-methyl-phenyl, 4-trifluoromethyl-phenyl, 4-methanesulfonyl-phenyl, 2,5-dimethoxy-phenyl, 3,4-dimethoxy-phenyl, naphthalen-1-yl, naphthalen-2-yl, 4-methyl-3,4-dihydro-2H-benzo[1,4]oxazin-7-yl, 2-chloro-5-trifluoromethyl-phenyl, 2-chloro-4-trifluoromethyl-phenyl, and 4-chloro-3-trifluoromethyl-phenyl.'}3. A method according to claim 1 , wherein{'sup': '2', 'Rrepresents a group selected from the group consisting of phenyl, 3-chloro-phenyl, 3-bromo-phenyl, 3-methyl-phenyl, 3-methylthio-phenyl, 2-chloro-5-methyl-phenyl, 4-chloro-3-methyl-phenyl, 2-fluoro-5-methyl-phenyl, 4-fluoro-3-methyl-phenyl, 3-ethyl-phenyl, 3,5-dimethyl-phenyl, 3,4-dimethyl-phenyl, 3,4-dichloro-phenyl, 3,5-dichloro-phenyl, 3-chloro-4-fluoro-phenyl, 3,4-difluoro-phenyl, 3-methoxy-phenyl, 3-cyano-phenyl, 5-chloro-2-methoxy-phenyl, 2-chloro-5-methoxy-phenyl, 3-ethoxy-phenyl, 3-dimethylamino-phenyl, 3-trifluoromethyl-phenyl, 3,5-dimethoxy-phenyl, 1-naphthyl, 3-trifluoromethoxy-phenyl, 3,5-bistrifluoromethyl-phenyl, and indan-5-yl.'}5. A pharmaceutical composition according to claim 4 , wherein{'sup': '1', 'Arrepresents a group selected from the group consisting of 3-chloro-phenyl, 4-bromo-phenyl, 3-bromo-phenyl, 3-chloro-4-methyl-phenyl, 3,4-dichloro-phenyl, 3-methoxy-phenyl, 4-methoxy-phenyl, 3,4-dimethoxy-phenyl, and 4-chloro-3-trifluoromethyl-phenyl;'}or a pharmaceutically acceptable salt thereof.6. A pharmaceutical composition according to ...

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13-06-2013 дата публикации

NOVEL SOLID FORMS OF TACEDINALINE

Номер: US20130150450A1
Принадлежит: THE BROAD INSTITUTE, INC.

Novel solid forms of tacedinaline (4-(acetylamino)-N-(2-aminophenyl)benzamide), including crystalline tacedinaline Forms A, B, and D, a novel crystalline tacedinaline TFA salt, and amorphous tacedinaline, are disclosed. Pharmaceutical compositions comprising crystalline tacedinaline Forms A, B, and D, the novel crystalline tacedinaline TFA salt, and/or amorphous tacedinaline, and methods of treating various conditions by administering those novel solid forms, are also disclosed. 14-. (canceled)5. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering 4-(acetylamino)-N-(2-aminophenyl)benzamide comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject.6. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering a pharmaceutical composition comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject.7. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering 0.001 mg/kg to 50 mg/kg per day of 4-(acetylamino)-N-(2-aminophenyl)benzamide comprising crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject , for at least two consecutive days.8. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising administering up to 0.4 mg/kg per day of 4-(acetylamino)-N-(2-aminophenyl)benzamide crystalline 4-(acetylamino)-N-(2-aminophenyl)benzamide Form A to said subject , for up to 14 consecutive days.9. A method of treating at least one of a neoplastic disease , memory loss , and a cognitive function disorder/impairment in a subject , said method comprising ...

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13-06-2013 дата публикации

PROCESS FOR MAKING CIS-1-CHLORO-3,3,3-TRIFLUOROPROPENE

Номер: US20130150633A1
Принадлежит: HONEYWELL INTERNATIONAL INC.

Disclosed is a process for making cis-1-chloro-3,3,3-trifluoropropene comprising reacting 3,3,3-trifluoropropyne with HCl in a reaction vessel at a yield of at least about 80%. 1. A process for making cis-1-chloro-3 ,3 ,3-trifluoropropene comprising reacting 3 ,3 ,3-trifluoropropyne with HCl in a reaction vessel at a yield of at least about 80%.2. The process of claim 1 , wherein a solvent is used in the reaction vessel.3. The process of claim 2 , wherein the solvent comprises an ionic solvent.4. The process of claim 3 , wherein the ionic solvent comprises one or more solvents with ammonium ions.5. The process of claim 4 , wherein the ionic solvent is selected from the group consisting of salts of 1-alkyl-3-methylimidazolium claim 4 , 1-alkylpyridinium claim 4 , and N-methyl-N-alkylpyrrolidinium claim 4 , and mixtures thereof.6. The process of claim 4 , wherein the ionic solvent comprises 1-butyl-3-methylimidazolium chloride claim 4 ,7. The process of claim 1 , wherein a catalyst is used in the reaction vessel.8. The process of claim 7 , wherein the catalyst is on a support.9. The process of claim 8 , wherein the catalyst support comprises activated carbon.10. The process of claim 7 , wherein the catalysts comprises one or more mineral acids.11. The process of claim 10 , wherein the mineral acid comprises HSO.12. The process of claim 7 , wherein the catalyst comprises a Lewis acid or a mixture of Lewis acids.13. The process of claim 12 , wherein the Lewis acids comprises metal salts or mixtures thereof.14. The process of claim 13 , wherein the metal salts are selected from the group consisting of copper and antimony and mixtures thereof.15. The process of claim 13 , wherein the Lewis acids are selected from the group consisting of CuCl claim 13 , CuCl claim 13 , SbCl claim 13 , ZnCl claim 13 , MgCl claim 13 , AlCl claim 13 , FeCl claim 13 , and the like (MCl).16. The process of claim 13 , wherein the Lewis acid comprises CuCl.17. The process of claim 16 , wherein ...

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13-06-2013 дата публикации

PROCESS FOR 1,1,2-TRICHLORO-3,3,3-TRIFLUOROPROPANE

Номер: US20130150634A1
Принадлежит: HONEYWELL INTERNATIONAL INC.

Disclosed is a process for making the compound 1,1,2-trichloro-3,3,3-trifluoro-propane (233da) by the catalytic fluorination of 1,1,1,2,3,3-hexachloropropane. 233da is a starting material used in the production cis-1-chloro-3,3,3-trifluoropropene (cis-1233zd). 1. A process for making the compound 1 ,1 ,2-trichloro-3 ,3 ,3-trifluoropropane (233da) from 1 ,1 ,1 ,2 ,3 ,3-hexachloropropane comprising the steps:(a) fluorinating a metal catalyst; and(b) fluorinating 1,1,1,2,3,3-hexachloropropane in the presence of the fluorinated metal catalyst, to produce a reaction mixture containing 1,1,2-trichloro-3,3,3-trifluoropropane.2. The process of claim 1 , wherein the metal catalyst is selected from the group consisting of SbCl claim 1 , TiCl claim 1 , SnCl claim 1 , TaCl claim 1 , and NbCl.3. The process of claim 2 , wherein the catalyst comprises SbCl.4. The process of claim 3 , wherein the fluorination of the catalyst is conducted at a temperature of about 90° C. for about two hours.5. The process of claim 4 , wherein the fluorination of the hexachloropropane is conducted at a temperature of about 100° C. for about 15 hours.6. The process of claim 3 , wherein the fluorination of the catalyst is conducted at a temperature of about 70° C. for about two hours.7. The process of claim 6 , wherein the fluorination of the hexachloropropane is conducted at a temperature of about 100° C. for about 20 hours.8. The process of claim 2 , wherein the catalyst comprises TaCl.9. The process of claim 8 , wherein the fluorination of the catalyst is conducted at a temperature of about 90° C. for about two hours.10. The process of claim 9 , wherein the fluorination of the hexachloropropane is conducted at a temperature of about 90° C. for about six hours.11. A process for making the compound 1 claim 9 ,1 claim 9 ,2-trichloro-3 claim 9 ,3 claim 9 ,3-trifluoropropane (233da) from trans-1-chloro-3 claim 9 ,3 claim 9 ,3-trifluoropropene (trans-1233zd) comprising reacting chlorine gas with trans- ...

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20-06-2013 дата публикации

Method of preparing ethacrynic amide derivatives and application thereof

Номер: US20130156701A1
Принадлежит: National Tsing Hua University NTHU

The present invention provides a method for preparing [ 18 F]—N-(4-fluorobutyl)ethacrynic amide which is prepared from radiofluorination and deprotection of the precursor tosylate N-Boc-N-[4-(toluenesulfonyloxy)-butyl)ethacrynic amide], obtained from ethacrynic acid via 6-step synthesis in 39% yield, in a radiochemical yield of 44%, aspecific activity of 48 GBq/μmol and radiochemical purity of 98%. The present invention further provides a composition for positron emission tomography (PET) of an animal models of a tumor liver or a liver disease, comprising [ 18 F]—N-(4-fluorobutyl)ethacrynic amide and a pharmaceutically acceptable carrier.

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20-06-2013 дата публикации

Modafinil Formulations

Номер: US20130156825A1
Принадлежит: CEPHALON, INC.

The invention provides an oral pharmaceutical composition comprising modafinil particles, wherein at least about 5% of said modafinil particles have a diameter greater than 200 microns. 1. An oral pharmaceutical composition comprising modafinil particles , wherein at least about 15% of the cumulative total of said modafinil particles have a diameter of more than about 200 microns and more than about 5% of the cumulative total of said modafinil particles have a diameter of more than about 250 microns.2. The pharmaceutical composition of claim 1 , wherein the median of the cumulative total of modafinil particles is greater than 60 microns.3. The pharmaceutical composition of claim 2 , wherein the median of the cumulative total of modafinil particles is greater than about 80 microns.4. The pharmaceutical composition of claim 1 , wherein the composition comprises 100 milligrams of said modafinil.5. The pharmaceutical composition of claim 1 , wherein said composition comprises about 200 milligrams of said modafinil.6. The pharmaceutical composition of claim 1 , wherein said composition has a dissolution rate in 0.1 N HCl at 37° C. of more than 80% in 30 minutes.7. The pharmaceutical composition of claim 1 , wherein said composition additionally comprises colloidal silicon dioxide claim 1 , crospovidone claim 1 , lactose claim 1 , talc claim 1 , sodium stearyl fumarate and povidone. The invention relates to an oral pharmaceutical composition comprising modafinil. The composition comprises modafinil particles, wherein at least 5% of said modafinil particles have a diameter greater than 200 μ. Still, this composition showed dissolution rate and blood levels (after oral administration) comparable with Provigil® tablets of the same strength.Modafinil, also termed 2-[(diphenylmethyl)sulfinyl]acetamide, is marketed in various countries under brand names such as Provigil®, Modiodal® and Vigil®. It is marketed as tablets containing 100 or 200 milligrams of modafinil. This drug is ...

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20-06-2013 дата публикации

PIPERAZINE-SUBSTITUTED BENZOTHIOPHENES FOR TREATMENT OF MENTAL DISORDERS

Номер: US20130158044A1
Принадлежит: OTSUKA PHARMACEUTICAL CO., LTD.

The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety. 7. The heterocyclic compound of the formula (1) according to selected from the group consisting of:(1) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one,(2) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-1H-quinolin-2-one,(3) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-3,4-dihydro-1H-quinolin-2-one,(4) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one,(5) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1-methyl-3,4-dihydro-1H-quinolin-2-one and(6) 6-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-3,4-dihydro-1H-quinolin-2-one;or a salt thereof.8. The heterocyclic compound of the formula (1) according to selected from the group consisting of:(1) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-3,4-dihydro-2H-isoquinolin-1-one(2) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-2-methyl-3,4-dihydro-2H-isoquinolin-1-one,(3) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-2-methyl-3,4-dihydro-2H-isoquinolin-1-one,(4) 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-3,4-dihydro-2H-isoquinoline-1-one,(5) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-2H-isoquinolin-1-one and(6) 7-[3-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)propoxy]-2-methyl-2H-isoquinolin-1-one;or a salt thereof.9. A pharmaceutical composition comprising a heterocyclic compound of the formula (1) or a salt thereof according to claim 1 , as an active ingredient and a pharmaceutically acceptable carrier.10. The pharmaceutical composition according to for treating or preventing central nervous system disorders.11. The pharmaceutical composition according to for treating or preventing central nervous system disorders selected from the group ...

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20-06-2013 дата публикации

CONJUGATES OF POLYUNSATURATED FATTY ACIDS AND AMINE-CONTAINING COMPOUNDS AND USES THEREOF

Номер: US20130158070A1
Автор: Nassar Taher
Принадлежит:

Novel chemical conjugates derived from unsaturated fatty acids and therapeutically active agents, are disclosed. The chemical conjugates are designed and characterized as COX-2 and/or 5-LOX inhibitors and are useful in the treatment of inflammatory diseases and disorders such as Alzheimer's disease, Parkinson's disease, asthma, osteoarthritis, rheumatoid arthritis, pain, primary dysmenorrhea, Crohn's disease and ulcerative colitis. 140-. (canceled)41. A method for treating dermatitis in a subject in need comprising the step of administering the subject in need docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid linked to a hydroxyproline , thereby treating dermatitis in the subject.42. A method of synthesizing 1-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoyl-4-hydroxy-pyrrolidine-2-carboxylic acid comprising:mixing tetrahydrofurane with decosahexanoic acid;adding triethylcloroformate;adding triethylamine;stirring and filtering;adding a solution of hydroxyproline and NaOH in water;adding strong acid;adding hexane;collecting organic layer; and drying43. The method according to claim 42 , wherein the step of stirring following the addition of the hydroxyproline and NaOH in water solution claim 42 , is for at 12 hours.44. The method according to claim 42 , wherein the step of drying is over anhydrous sulfate.45. A chemical conjugate comprising a first moiety and a second moiety covalently linked therebetween claim 42 , wherein said second moiety is derived from docosa-4 claim 42 ,7 claim 42 ,10 claim 42 ,13 claim 42 ,16 claim 42 ,19-hexaenoic acid claim 42 , and wherein said first moiety is derived from a therapeutically active agent or a derivative thereof claim 42 , each independently having a functional group for forming a covalent bond with said second moiety claim 42 , with the proviso that said first moiety is not hydroxyproline claim 42 , the chemical conjugate being a cyclooxygenase-2 (COX-2) inhibitor.46. The chemical conjugate of claim 45 , being further a 5-lipoxygenase (5-LOX ...

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20-06-2013 дата публикации

COMPOSITIONS AND METHODS FOR INHIBITING BETA AMYLOID SECRETION

Номер: US20130158112A1
Принадлежит:

A pharmaceutical composition for inhibiting amyloid beta peptide in a subject includes a compound having the formula (I): 4. The pharmaceutical composition of claim 2 , where Rand Rare independently selected from H claim 2 , Cl claim 2 , CH claim 2 , OH claim 2 , NO claim 2 , F claim 2 , Br claim 2 , CF claim 2 , or an alkoxy group.5. The pharmaceutical composition of claim 2 , where Z is selected from Cl claim 2 , alkoxy claim 2 , OH claim 2 , CN claim 2 , C(NH)NOH claim 2 , NO claim 2 , NH claim 2 , COEt claim 2 , COOH claim 2 , CONH claim 2 , F claim 2 , CH claim 2 , CHO claim 2 , CF claim 2 , BR claim 2 , I claim 2 , CONHCH claim 2 , NHCOCHand OCHCHOCHCHOH.12. The method of where Rand Rare independently selected from H claim 10 , Cl claim 10 , CH claim 10 , OH claim 10 , NO claim 10 , F claim 10 , Br claim 10 , CFand an alkoxy group.13. The method of claim 10 , where Z is selected from Cl claim 10 , alkoxy claim 10 , OH claim 10 , CN claim 10 , C(NH)NOH claim 10 , NO claim 10 , NH claim 10 , COEt claim 10 , COOH claim 10 , CONH claim 10 , F claim 10 , CH claim 10 , CHO claim 10 , CF claim 10 , BR claim 10 , I claim 10 , CONHCH claim 10 , NHCOCHand OCHCHOCHCHOH.19. The method of where Rand Rare independently selected from H claim 17 , Cl claim 17 , CH claim 17 , OH claim 17 , NO claim 17 , F claim 17 , Br claim 17 , CFand an alkoxy group.20. The method of claim 17 , where Z is selected from Cl claim 17 , alkoxy claim 17 , OH claim 17 , CN claim 17 , C(NH)NOH claim 17 , NO claim 17 , NH claim 17 , COEt claim 17 , COOH claim 17 , CONH claim 17 , F claim 17 , CH claim 17 , CHO claim 17 , CF claim 17 , BR claim 17 , I claim 17 , CONHCH claim 17 , NHCOCHand OCHCHOCHCHOH.23. The method of claim 16 , the pharmaceutical composition promoting neuronal survival in the subject. This application claims priority from U.S. Provisional Application No. 61/498,847, filed Jun. 20, 2011, the subject matter of which is incorporated herein by reference in its entirety.This ...

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27-06-2013 дата публикации

Process for the Preparation of Nateglinide

Номер: US20130165686A1
Принадлежит: CIPLA LIMITED

The present invention relates to a process for the preparation of substantially pure nateglinide of formula (I), substantially free from the cis-isomer and L-enantiomer and preparation of enantiomerically pure nateglinide form B, directly from the hydrolysis of a (−)-N-(trans-4-isopropylcyclohexyl-1-carbonyl)-D-phenylalanine alkyl ester in a ketonic solvent or water or mixture thereof. 2. The process according to claim 1 , wherein Alk is methyl.3. The process according to claim 1 , wherein the hydrolysis is carried out at. a temperature ranging from 0° C. to 30° C.4. The process according claim 1 , wherein the solvent is a mixture of a ketone and water claim 1 , and the ketone:water ratio varies from 5:1 to 1:1.5. The process according to . wherein the solvent comprises acetone and water.6. The process according to claim 1 , wherein the solvent is a 1:1 v/v mixture of acetone and water claim 1 , isolation of the nateglinide comprises drying under vacuum tray driers at a temperature ranging from 70° C. to 90° C. claim 1 , and the nateglinide i.s isolated in polymorphic Form B.8. The process according to claim 8 , wherein the compound (IV) is in the form of an HCl addition salt.9. The process according to claim 7 , wherein the trans-4-isopropyl-cyclobexylcarboxylic acid of formula (III) is in molar excess relative to the compound (IV).10. The process according to claim 7 , wherein the condensing reagent is selected from the group consisting of phenylsilane claim 7 , 1 claim 7 ,1′-carbonyldiimidazole (CDI) claim 7 , benzotriazol-1-yloxytris (dimethylamino) phophonium hexafluorophosphate (BOP) claim 7 , 1-hydroxy benzotriazole hydrate (HOBO claim 7 , PyBOP (Analog of the BOP) claim 7 , 1 claim 7 ,3-dicyclohexylcarbodiimide (DCC) claim 7 , 1 claim 7 ,3-chisopropylcarbodiimide (DIC) claim 7 , N claim 7 ,N-diisopropylethylamine (DIEA) claim 7 , 4-dimethylaminopyridine (DMAP) claim 7 , 1 claim 7 ,4-dithio-L-threitol (DTT) claim 7 , N-ethyl-V-(3-dimethylaminopropyl) ...

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27-06-2013 дата публикации

METHOD FOR PRODUCING A CHLORINATED HYDROCARBON HAVING 3 CARBON ATOMS

Номер: US20130165705A1
Принадлежит: TOKUYAMA CORPORATION

A method of producing a chlorinated hydrocarbon having 3 carbon atoms, comprising a conversion step for converting a chloropropane represented by the following formula (1) into a chloropropane represented by the following formula (2) by reacting it with chlorine in the presence of anhydrous aluminum chloride. 1. A method of producing a chlorinated hydrocarbon having 3 carbon atoms , comprising a conversion step for converting a chloropropane represented by the following formula (1) into a chloropropane represented by the following formula (2) by reacting it with chlorine in the presence of anhydrous aluminum chloride ,{'br': None, 'sub': 3', '(2-m)', 'm', '(3-n)', 'n, 'CCl—CClH—CClh\u2003\u2003(1),'}{'b': '1', 'claim-text': {'br': None, 'sub': 3', '(3-m)', '(m-1)', '(3-n)', 'n, 'CCl—CClH—CClH\u2003\u2003(2),'}, 'In the above formula (), m is 1 or 2, and n is an integer of 0 to 3,'}In the above formula (2), m and n are the same integers as in the formula (1), respectively.2. The method of producing a chlorinated hydrocarbon having 3 carbon atoms according to claim 1 , wherein the conversion step is carried out by putting at least the chloropropane represented by the above formula (1) and anhydrous aluminum chloride into a reactor and then supplying chlorine into the reactor.3. The method of producing a chlorinated hydrocarbon having 3 carbon atoms according to claim 2 , wherein the supply of chlorine into the reactor is started after anhydrous aluminum chloride is dissolved.4. The method of producing a chlorinated hydrocarbon having 3 carbon atoms according to claim 1 , wherein the conversion step is carried out by putting a solution containing at least anhydrous aluminum chloride and the chloropropane represented by the above formula (1) into a reactor and then supplying chlorine into the reactor.5. The method of producing a chlorinated hydrocarbon having 3 carbon atoms according to claim 4 , wherein the solution containing at least anhydrous aluminum chloride and ...

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04-07-2013 дата публикации

USE OF KUKOAMINE A AND KUKOAMINE B

Номер: US20130172421A1
Принадлежит:

The use of Kukoamine A and Kukoamine B in the preparation of drugs for the prevention and treatment of sepsis and autoimmune disease is disclosed. Bacterial endotoxin/lipopolysaccaride (LPS) and unmethylated DNA (CpG DNA) of bacteria, the major pathogen-associated molecular patterns in sepsis and autoimmune disease, are specifically targeted, while the disclosed use directionally isolates lead compounds from traditional Chinese medicine. These measures can overcome the major defects of uncertainty of pharmacological material basis and drug targets of extracts and constituents of traditional Chinese medicine. The disclosed use can help in developing a safe, effective and quality controllable drug for prevention and treatment of sepsis and autoimmune disease so as to help solve the present lack of effective drugs in clinical treatment. 1. Use of Kukoamine A and Kukoamine B in the preparation of drugs for the prevention and treatment of sepsis and autoimmune disease.2Lycii cortex. The use of wherein said Kukoamine A and Kukoamine B are extracted from of traditional Chinese medicine.3Lycii cortexLycium chineseLycium barbarum. The use of wherein said is the dried root bark of Mill. or L of the Solanaceae family.4. The use of wherein said drugs are used for the preparation of drugs for the prevention and treatment of sepsis and autoimmune disease.5. The use of wherein said drugs are used for antagonizing the key factors that lead to sepsis and autoimmune disease claim 1 , bacterial endotoxin/lipopolysaccharide (LPS) and unmethylated DNA (CpG DNA) of bacteria.6. A pharmaceutical composition comprising Kukoamine A and Kukoamine B for use in the prevention and treatment of sepsis and autoimmune disease.7Lycii cortex. The pharmaceutical composition of wherein said Kukoamine A and Kukoamine B are extracted from of traditional Chinese medicine.8Lycii cortexLycium chineseLycium barbarum. The pharmaceutical composition of wherein said is the dried root bark of Mill. or L of the ...

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04-07-2013 дата публикации

PROCESSES FOR MAKING CYCLOPROPYL AMIDE DERIVATIVES AND INTERMEDIATES ASSOCIATED THEREWITH

Номер: US20130172560A1
Автор: Stranne Robert
Принадлежит: AstraZeneca AB

Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition. 3. The process of claim 2 , wherein said base is sodium hydroxide.4. The process of claim 2 , wherein said peroxide is hydrogen peroxide.5. The process of claim 2 , wherein said acidic solution is an aqueous solution of sodium hydrogen sulfate.7. The process of claim 6 , wherein X is Br.8. The process of claim 6 , wherein said metal is zinc.9. The process of claim 6 , wherein said metal cyanide is zinc-(II)-cyanide.10. The process of claim 6 , wherein said catalyst is bis(tri-t-butylphosphine)palladium(0).15. The process of claim 14 , wherein said activating agent is 1 claim 14 ,1′-carbonyldiimidazole.19. The process of claim 18 , wherein the activating agent is a mixture of 1-hydroxybenzotriazole and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride.21. The process of claim 16 , wherein said acid is hydrochloric acid.23. The process of claim 17 , wherein said reducing agent is sodium triacetoxy borohydride. Presented herein are processes for making cyclopropyl amide derivatives of formula I, and/or pharmaceutically acceptable salts thereof, and intermediates associated therewith. At least one cyclopropyl amide derivative of formula I, or pharmaceutically acceptable salt thereof is useful to treat at least one histamine H3 receptor associated condition.The histamine H3 receptor is of current interest in developing new medicaments. The H3 receptor is a presynaptic autoreceptor located both in the central and peripheral nervous systems, the skin, and in organs, such as, for example, the lung, the intestine, probably the spleen, and the gastrointestinal tract. Recent evidence suggests the H3 receptor has intrinsic ...

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04-07-2013 дата публикации

Process for Manufacture of N-acylbiphenyl alanine

Номер: US20130172572A1
Принадлежит:

A novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors. 2. The process according to claim 1 , wherein the alkaline conditions comprise the use of a base selected from triethylamine claim 1 , pyridine claim 1 , N-methylpyrrole claim 1 , N-methylmorpholine claim 1 , sodium bicarbonate claim 1 , sodium carbonate claim 1 , potassium bicarbonate claim 1 , potassium carbonate claim 1 , sodium acetate claim 1 , potassium acetate claim 1 , sodium propionate and potassium propionate.3. The process according to ems claim 1 , wherein the reaction is carried out at a temperature of from of from 80 deg C. to reflux.5. The process according to claim 4 , wherein the reaction is carried out at a temperature of from of from room temperature to reflux.7. The process according to claim 6 , wherein the hydrogenation conditions comprise the use of hydrogen and palladium claim 6 , preferably claim 6 , palladium on charcoal.8. A process for preparing a compound of formula (3) claim 6 , as defined in claim 6 ,comprising the steps of{'claim-ref': [{'@idref': 'CLM-00001', 'claim 1'}, {'@idref': 'CLM-00001', 'claim 1'}], 'i) preparing the compound of formula (1-a), as defined in , according to the process defined in ;'}{'claim-ref': [{'@idref': 'CLM-00004', 'claim 4'}, {'@idref': 'CLM-00004', 'claim 4'}], 'ii) preparing the compound of formula (2-a), as defined in , according to the process defined in ; and'}{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'iii) obtaining the compound of formula (3), according to the process defined in .'}9. A process for preparing a compound of formula (3) claim 6 , as defined in claim 6 ,comprising the steps of{'claim-ref': [{'@idref': 'CLM-00004', 'claim 4'}, {'@idref': 'CLM-00004', 'claim 4'}], 'ii) preparing the compound of formula (2-a), as defined in , according to the process defined in ; and'}{'claim-ref': {'@idref': 'CLM-00006', ...

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04-07-2013 дата публикации

Novel Polymers

Номер: US20130172600A1
Принадлежит: NOVARTIS AG

The invention relates to novel crosslinkable copolymers which are obtainable by (a) copolymerizing at least two different hydrophilic monomers selected from the group consisting of N,N-dimethyl acrylamide (DMA), 2-hydroxyethyl acrylate (HEA), glycidyl methacrylate (GMA), N-vinylpyrrolidone (NVP), acrylic acid (AA) and a C-C-alkoxy polyethylene glycol(meth)acrylate having a weight average molecular weight of from 200 to 1500, and at least one crosslinker comprising two or more ethylenically unsaturated double bonds in the presence of a chain transfer agent having a functional group; and (b) reacting one or more functional groups of the resulting copolymer with an organic compound having an ethylenically unsaturated group. 124-. (canceled)25. A process for manufacturing an actinically crosslinkable prepolymer , comprising:(1) obtaining a reaction mixture comprising a first hydrophilic monomer, at least one polysiloxane-containing crosslinker, a second hydrophilic monomer, and a chain transfer agent having a first functional group and present in an amount to have a desired initial concentration;(2) adjusting the temperature of the reaction mixture in order to start the polymerization reaction;(3) dosing the chain transfer agent to the reaction mixture at a rate sufficient to have a concentration comparable to the desired initial concentration until a desired total amount of the chain transfer agent is added;(4) following the completion of the chain transfer agent dosing maintaining the reaction mixture at the reaction temperature in order to complete the reaction so as to obtain a copolymerization product with first functional groups; and(5) reacting an organic compound with the copolymerization product to form the crosslinkable prepolymer having ethylenically unsaturated groups, wherein the organic compound comprises an ethylenically unsaturated group and a second functional group, wherein the second functional group of the organic compound reacts with one of the ...

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18-07-2013 дата публикации

Labeling Agent and Methods for Simultaneous Sequencing and Quantification of Multiple Peptides and Proteins Using the Same

Номер: US20130183704A1
Принадлежит: POSTECH ACADEMY-INDUSTRY FOUNDATION

The present invention provides a compound that can utilize hydrogen isotope and, at the same time, can quantify multiplexed samples at one time, as well as decreasing the cost for synthesis of the labeling agent. In addition, the present invention provides a novel method for quantitatively analyzing protein and peptide analytes having different quantities form each other using the labeling agent, wherein y-type fragment ions having a high mass which comprises the analyte remained after coupling the labeling agent with the analyte and then removing a part of the labeling agent through tandem mass spectrometry are utilized to conduct the quantitative analysis. 3. The compound according to claim 2 , characterized in that Ris octyl; and Ris heptyl.5. The compound according to claim 1 , characterized in that{'sub': 1', '2, 'Rand Rare'}{'sub': 3', '6', '4', '2', '3', '6', '4', '2', '2, 'CHC≡CCHCHand CDC≡CCHCDCH, respectively;'}{'sub': 3', '6', '4', '2', '3', '6', '4', '2', '2, 'CHC≡CCHCDand CDC≡CCHCHCH, respectively;'}{'sub': 3', '6', '4', '2', '3', '6', '4', '2', '2, 'CDC≡CCHCHand CHC≡CCHCDCH, respectively; or'}{'sub': 3', '6', '4', '2', '3', '6', '4', '2', '2, 'CDC≡CCHCDand CHC≡CCHCHCH, respectively.'}6. The compound according to claim 1 , characterized in that Ris a side chain of any one amino acid residue selected from the group consisting of glycine claim 1 , alanine claim 1 , serine claim 1 , valine claim 1 , leucine claim 1 , isoleucine claim 1 , methionine claim 1 , glutamine claim 1 , asparagine claim 1 , cysteine claim 1 , histidine claim 1 , phenylalanine claim 1 , arginine claim 1 , tyrosine and tryptophan.7. The compound according to claim 1 , characterized in that Ris hydroxy claim 1 , succinimid-N-oxy claim 1 , 3-sulfosuccinimid-N-oxy claim 1 , benzotriazol-1-yl-oxy claim 1 , pentahalobenzyloxy claim 1 , 4-nitrophenoxy or 2-nitrophenoxy.8. The compound according to claim 1 , characterized in that said compound is any one selected from the group consisting ...

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18-07-2013 дата публикации

INSECTICIDAL COMPOUNDS

Номер: US20130184343A1
Принадлежит:

A compound of formula (I): 2. A compound according to wherein Ais C—X—Ror C—R.3. A compound according to wherein Ais C—X—Ror C—R.4. A compound according to wherein Ais C—X—Ror C—R.5. A compound according to wherein Ais C—X—Ror C—R.6. A compound according to wherein one or two of A claim 1 , A claim 1 , Aand Aare C—X—R.7. A compound according to wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl or acetyl.8. A compound according to wherein Ris hydrogen claim 1 , methyl claim 1 , ethyl or acetyl.9. A compound according to wherein Gis oxygen.10. A compound according to wherein Gis oxygen.11. A compound according to wherein each Ris independently hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , allyl claim 1 , phenyl or phenyl mono-substituted by halogen or methyl.12. A compound according to wherein each X is independently oxygen or sulfur.13. A compound according to wherein each Ris independently hydrogen or methyl.14. A compound according to wherein each Ris independently hydrogen claim 1 , fluoro claim 1 , methyl or trifluoromethyl.15. A compound according to any wherein Qis 5-bromo-furan-2-yl claim 1 , 2-bromo-phenyl claim 1 , 5-bromo-pyrid-3-yl claim 1 , 2-chloro-5-nitro-phenyl claim 1 , 2-chloro-phenyl claim 1 , 3-chloro-phenyl claim 1 , 2-chloro-pyrid-3-yl claim 1 , 2-chloro-pyrid-4-yl claim 1 , 6-chloro-pyrid-3-yl claim 1 , 5-chloro-thiophen-2-yl claim 1 , 3-chloro-5-trifluoromethyl-pyrid-2-yl claim 1 , 4-cyano-phenyl claim 1 , 2 claim 1 ,5-dichloro-phenyl claim 1 , 2 claim 1 ,3-difluoro-phenyl claim 1 , 1 claim 1 ,3-dimethyl-pyrazol-5-yl claim 1 , 4-fluoro-phenyl claim 1 , 2-fluoro-pyrid-3-yl claim 1 , 2-fluoro-3-trifluoromethyl-phenyl claim 1 , 2-methyl-phenyl claim 1 , 3-methyl-pyrid-2-yl claim 1 , 2-methylthio-pyrid-3-yl claim 1 , 4-nitro-phenyl claim 1 , phenyl claim 1 , 1 claim 1 ,2 claim 1 ,3-thiadiazol-4-yl and thiophen-2-yl.16. A compound according to wherein Qis a moiety of formula (II).17. A compound according to wherein Qis 2 ...

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18-07-2013 дата публикации

ACID ADDITION SALT OF A NORTRIPTYLINE-GABA CONJUGATE AND A PROCESS OF PREPARING SAME

Номер: US20130184347A1
Принадлежит:

An acid addition salt of a nortriptyline-GABA conjugate, a novel crystalline form of a fumaric acid addition salt of a nortriptyline-GABA conjugate, and processes of preparing the forgoing are disclosed. Uses of the above-indicated forms of a nortriptyline-GABA conjugate in the treatment of CNS disorders, and in the treatment of pain in particular, are also disclosed. Further disclosed in a large-scale process of preparing a nortriptyline-GABA conjugate. 149-. (canceled)50. A fumaric acid addition salt of nortriptyline-4-aminobutyrate.51. A crystalline form of a fumaric acid addition salt of nortriptyline-4-aminobutyrate , characterized by at least one of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 3'}, '(a) an X-Ray Powder Diffraction (XRPD) pattern exhibiting at least four of the peaks shown in ;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, '(b) an infrared spectrum exhibiting at least three of the absorption peaks shown in ; and'}(c) a Differential Scanning calorimetry (DSC) exhibiting an endothermic peak maximum that ranges from 155° C. to 160° C.52. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an X-Ray Powder Diffraction (XRPD) pattern exhibiting at least six of the peaks shown in .53. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an X-Ray Powder Diffraction (XRPD) pattern exhibiting at least seven of the peaks shown in .54. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an X-Ray Powder Diffraction (XRPD) pattern substantially identical to the XRPD pattern shown in .55. The crystalline form of nortriptyline-4-aminobutyrate fumarate of claim 51 , characterized by an infrared spectrum exhibiting at least five of the absorption peaks shown in .56. The crystalline form of a fumaric acid addition salt of nortriptyline-4-aminobutyrate of claim 51 , characterized by an infrared spectrum exhibiting absorption peaks substantially ...

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18-07-2013 дата публикации

PROCESS FOR PREPARATION OF 4-FLUORO-alpha-[2METHYL-L-OXOPROPYL]-gamma-OXO-N-beta-DIPHENYLBENZENE BUTANE AMIDE

Номер: US20130184493A1
Принадлежит: VIJAYASRI ORGANICS LIMITED

A process for preparation of 4-fluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzene butane amide also known as a diketone intermediate of atorvastatin, completely devoid of impurities 3,4-difluoro-α-[2-methyl-1-oxopropyl]-γ-oxo-n-β-diphenylbenzene butane amide; methyl, 2{-2[-(4-fluorophenyl)-2-oxo-1-phenylethyl)]}-4-methyl-3-oxo pentanoate; 1,4-bis(4-fluorophenyl)-2,3-diphenylbutane-1,4-dione, 1-(4-fluorophenyl)-2-phenyl ethanone; 1-(4-fluorophenyl)-2-phenyl ethanone and containing about 0.05% or less of 2-methyl-1-oxopropyl]-γ-oxo-N-β-diphenylbenzene butane amide. In that process the said diketone intermediate of formula 1 is obtained by maintaining temperature −25° C. to 50° C. during Friedel-Crafts acylation, in situ halogenation of formula II in presence of a solvent and nucleophilic substitution from a compound of formula III with formula IV in presence of a base. 2. The process of claim 1 , wherein said Friedel-Crafts condensation is carried out in presence of Lewis acid catalyst to afford said Formula II.3. The process of claim 2 , wherein said lewis acid catalyst is selected from the group comprising FeCl3 claim 2 , SbCl5 claim 2 , BF3 claim 2 , TiCl4 claim 2 , ZnC2 or AlCl3.4. (canceled)5. The process of claim 1 , wherein the inert solvent in step (b) is methylene chloride.6. The process of claim 1 , wherein said halogen is selected from the group consisting of bromine and chlorine.7. The process of claim 1 , wherein said base for nucleophilic substitution of said formula III is eitherone or more inorganic salts selected from the group comprising sodium carbonate, potassium carbonate or cesium carbonate; orone or more organic bases selected from the group comprising triethyl amine or diisopropylethylamine.8. The process of claim 1 , wherein said solvent for nucleophilic substitution of said formula III is selected from the group comprising tetrahydrofuran claim 1 , 1 claim 1 ,2-dimethoxy ethane claim 1 , methylene chloride claim 1 , ethyl acetate claim ...

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25-07-2013 дата публикации

BIS-FATTY ACID CONJUGATES AND THEIR USES

Номер: US20130190327A1
Принадлежит: CATABASIS PHARMACEUTICALS INC

The invention relates to bis-fatty acid conjugates; compositions comprising an effective amount of a bis-fatty acid conjugate; and methods for treating or preventing cancer, a metabolic disease or a neurodegenerative disease comprising the administration of an effective amount of a bis-fatty acid conjugate. 1. A molecular conjugate , directly or indirectly covalently linked wherein the linker comprises at least one amide , comprising two or more fatty acids selected from the group consisting of omega-3 fatty acids , fatty acids that are metabolized in vivo to omega-3 fatty acids , and lipoic acid , with the proviso that the molecular conjugate is not (4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid {2-[2-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-ethylamino]-ethyl}-amide (A); (5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoic acid {2-[2-((5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoylamino)-ethylamino]-ethyl}-amide (B); (4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoic acid {2-[2-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-ethoxy]-ethyl}-amide (C); (5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoic acid {2-[2-((5Z ,8Z ,11Z ,14Z ,17Z)-icosa-5 ,8 ,11 ,14 ,17-pentaenoylamino)-ethoxy]-ethyl}-amide (D); or (S)-2 ,6-Bis-((4Z ,7Z ,10Z ,13Z ,16Z ,19Z)-docosa-4 ,7 ,10 ,13 ,16 ,19-hexaenoylamino)-hexanoic acid (E).2. The molecular conjugate of claim 1 , wherein the fatty acid is selected from the group consisting of all-cis-7 claim 1 ,10 claim 1 ,13-hexadecatrienoic acid claim 1 , α-linolenic acid claim 1 , stearidonic acid claim 1 , eicosatrienoic acid claim 1 , eicosatetraenoic acid claim 1 , eicosapentaenoic acid (EPA) claim 1 , docosapentaenoic acid claim 1 , docosahexaenoic acid (DHA) claim 1 , tetracosapentaenoic acid claim 1 , tetracosahexaenoic acid and lipoic acid.3. The molecular conjugate of claim 2 , wherein the fatty acid is selected from ...

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25-07-2013 дата публикации

NOVEL COMPOUND ACCELERATING SECRETION OF HUMAN-DERIVED ANTI-MICROBIAL PEPTIDE, METHOD FOR PREPARING SAME, AND COMPOSITION HAVING SAME AS ACTIVE INGREDIENT

Номер: US20130190397A1
Принадлежит: NEOPHARM CO., LTD.

Disclosed is a compound having an acceleration effect on the secretion of human β-defensin, LL-37, which is a human-derived anti-microbial peptide, a method for preparing same, and a composition for accelerating the secretion of anti-microbial peptide having same as an active ingredient, and the compound and the composition using same of the present invention enhance the anti-microbial effect and the immunity control effect that the anti-microbial peptide has in the body by accelerating the secretion of the anti-microbial peptide in the body. 18-. (canceled)10. The new compound of claim 9 , wherein the antimicrobial peptides are human β-defensin-2 claim 9 , β-defensin-3 claim 9 , or LL-37.14. The composition of claim 13 , wherein the compound as an active ingredient is contained at 0.001-90 wt %.15. The composition of claim 13 , wherein the composition for promoting secretion of human antimicrobial peptides in vivo is a formulation selected from the group consisting of a liquid phase claim 13 , an emulsion phase claim 13 , a suspension phase claim 13 , a cream phase claim 13 , an ointment phase claim 13 , a gel phase claim 13 , a jelly phase claim 13 , and a spray phase.16. The composition of claim 13 , wherein the composition for promoting secretion of human antimicrobial peptides in vivo is a formulation selected from the group consisting of a tablet claim 13 , a liquid claim 13 , a powder claim 13 , and an injection. This application is a continuation application of PCT International Application No. PCT/KR2010/005759 filed Aug. 27, 2010, the contents of which are incorporated herein by reference in their entirety.The following disclosure relates to a compound for promoting the secretion of human antimicrobial peptides, and more particularly, to a new compound for inducing direct or indirect expression of human β-defensin-2 and -3 and LL-37, which are human antimicrobial peptides, a method for preparing the same, and a composition comprising the same as an active ...

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25-07-2013 дата публикации

QUINOLYLPIPERAZINO SUBSTITUTED THIOLACTONE COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF

Номер: US20130190489A1
Принадлежит:

The present invention provides compounds of general formulae A, useful as potential anti-tubercular agents against H37Rv, and drug-resistant and a process for the preparation thereof. Formula (A). 3. Quinolylpiperazino substituted thiolactone compounds as claimed in is represented by the group of the following compounds:3,5-dimethyl-4-[(5-4-[7-(trifluoromethyl)-4-quinolyl]piperazinopentyl)oxy]-5H-thiophen-2-one (3a).3,5-dimethyl-4-[(6-4-[7-(trifluoromethyl)-4-quinolyl]piperazinohexyl)oxy]-5H-thiophen-2-one (3b)3,5-dimethyl-4-[(8-4-[7-(trifluoromethyl)-4-quinolyl]piperazinooctyl)oxy]-5H-thiophen-2-one (3c).3,5-dimethyl-4-[(9-4-[7-(trifluoromethyl)-4-quinolyl]piperazinononyl)oxy]-5H-thiophen-2-one (3 d).3,5-dimethyl-4-[(10-4-[7-(trifluoromethyl)-4-quinolyl]piperazinodecyl)oxy]-5H-thiophen-2-one (3e).3,5-dimethyl-4-[(12-4-[7-(trifluoromethyl)-4-quinolyl]piperazinododecyl)oxy]-5H-thiophen-2-one (3f).3,5-dimethyl-4-(5-[4-(7-chloro-4-quinolyl)piperazino]pentyloxy)-5H-thiophen-2-one (4a).3,5-dimethyl-4-(6-[4-(7-chloro-4-quinolyl)piperazino]hexyloxy)-5H-thiophen-2-one (4b).3,5-dimethyl-4-(8-[4-(7-chloro-4-quinolyl)piperazino]octyloxy)-5H-thiophen-2-one (4c).3,5-dimethyl-4-(9-[4-(7-chloro-4-quinolyl)piperazino]nonyloxy)-5H-thiophen-2-one (4d).3,5-dimethyl-4-(10-[4-(7-chloro-4-quinolyl)piperazino]decyloxy)-5H-thiophen-2-one (4e).3,5-dimethyl-4-(12-[4-(7-chloro-4-quinolyl)piperazino]dodecyloxy)-5H-thiophen-2-one (4f).3,5-dimethyl-4-[(5-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-ylpentyl)oxy]-5H-thiophen-2-one 5a).3,5-dimethyl-4-[(6-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-ylhexyl)oxy]-5H-thiophen-2-one (5b).3,5-dimethyl-4-[(8-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-yloctyl)oxy]-5H-thiophen-2-one (5c).3,5-dimethyl-4-[(9-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-ylnonyl)oxy]-5H-thiophen-2-one (5d).3,5-dimethyl-4-[(10-4-[7-(trifluoromethyl)-4-quinolyl]-1,4-diazepan-1-yldecyl)oxy]-5H-thiophen-2-one (5e).3,5-dimethyl-4-[(12-4-[7-(trifluoromethyl)-4 ...

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25-07-2013 дата публикации

Process for the preparation of amino acid derivatives

Номер: US20130190533A1
Принадлежит: UCB PHARMA GMBH

The present invention relates to a process of manufacture of compounds of formula (B) wherein R 1 , R 2 and R 3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.

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25-07-2013 дата публикации

Method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane

Номер: US20130190540A1
Принадлежит: Kowa Co Ltd

A method for preparing optically active 1-bromo-1-[3,5-bis(trifluoromethyl)-phenyl]ethane having a high optical purity, which comprises the step of brominating optically active 1-[3,5-bis(trifluoromethyl)phenyl]ethanol by using, as a brominating agent, (a) a combination of a phosphorus halide and hydrogen bromide, (b) a combination of 1,2-dibromo-1,1,2,2-tetrachloroethane and an organic phosphorous compound represented by the general formula (I): P(R 1 )(R 2 )(R 3 ) (in the formula, R 1 , R 2 , and R 3 independently represent a C 6-10 aryl group, a C 6-10 aryloxy group, a C 1-10 alkyl group, a C 1-10 alkoxyl group, a C 3-6 cycloalkyl group, or a C 3-6 cycloalkoxy group), or (c) a combination of N-bromosuccinimide and a dialkyl sulfide.

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25-07-2013 дата публикации

CATALYST SYSTEM, COMPRISING CATALYST PELLETS AND DILUENT BEADS WITH PREDEFINED DIMENSIONS AND PHYSICOCHEMICAL PROPERTIES

Номер: US20130190541A1
Принадлежит: INEOUS EUROPE AG

A catalyst system for use in oxychlorination, the catalyst system comprising catalyst pellets comprising a catalyst carried on a substrate the pellets having length x, breadth y and depth z, intrinsic density P and bulk density p and diluent beads having length x±25%, breadth y±25% and depth z±25%, intrinsic density≧P+25% and a bulk density p ±25%. 132-. (canceled)33. A catalyst system for use in oxychlorination , said catalyst system comprising catalyst pellets comprising a catalyst carried on a first substrate , said catalyst pellets having a length x , breadth y and depth z and bulk density ρ and diluent beads comprising a second substrate different from that of the first substrate said beads having a length x±25% , breadth y±25% depth z±25% and bulk density p±25% and said diluent beads having a thermal conductivity at least 5 times greater than the thermal conductivity of said catalyst pellets.34. A catalyst system as claimed in wherein x is in the range 3 to 7 mm.35. A catalyst system as claimed in wherein y is in the range 4 to 7 mm.36. A catalyst system as claimed in wherein z is in the range 4 to 7 mm.37. A catalyst system as claimed in wherein said catalyst pellets comprise alumina.38. A catalyst system as claimed in wherein said diluent beads comprise graphite.39. A catalyst system as claimed in wherein the thermal conductivity of said diluent beads is less than 50 times greater than the thermal conductivity of said pellets.40. A catalyst system as claimed in wherein said pellets are trigonal prisms or right circular cylinders.41. A catalyst system as claimed in wherein said beads are right circular cylinders having a right circular bore having a diameter in the range 2.0 to 4.0 mm.42. A catalyst system as claimed in wherein the lateral compressive strength of the beads is 2 to 4 times that of the pellets.43. A method of preparing 1 claim 33 ,2-dichloroethane comprising passing ethylene claim 33 , hydrogen chloride and a molecular oxygen containing gas ...

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01-08-2013 дата публикации

Novel Glycine Derivative Capable Of Inhibiting Melanin Formation And Composition Using The Same

Номер: US20130195782A1
Принадлежит: CORUM INC.

The invention provides a glycine derivative, having a structure shown in the following general equation (I): 5. The glycine derivative according to claim 1 , wherein a solution or a buffer solution containing the glycine derivative with addition amount of 0.05˜10 wt % (weight ratio) has light transmittance more than or equal to 97% in the wavelength range of 420˜500 nm.6. The glycine derivative according to claim 5 , wherein the buffer solution comprises citric acid and salts thereof.7. The glycine derivative according to claim 5 , wherein solution or the buffer solution containing the glycine derivative with addition amount of 0.05˜10 wt % (weight ratio) has light transmittance more than or equal to 98% at the specific wavelength 440 nm.9. The composition according to claim 8 , wherein the composition comprises the glycine derivative with addition amount of 0.1˜2 wt % (weight ratio) and has a function of inhibiting melanin formation. 1. Field of the InventionThe present invention is generally related to a glycine derivative, and more particularly to a glycine derivative capable of inhibiting melanin formation and composition using the same.2. Description of the Prior ArtIn general, melanin formation is considered to be related to tyrosinase. Tyrosine naturally exists in epidermal cells and is the precursor or melanin. Melanin formation comprises the following steps tyrosine→Dopa→Dopaquinone→Dopachrome→melanin, melanin is formed and tyrosinase is an important enzyme in the melanin formation process. The hydroxylase activity of tyrosinase catalyzes the reaction of converting tyrosine into dopa and the oxidase activity of tyrosinase catalyzes the reaction of converting dopa into dopaquinone. As long as a substance can effectively act on epidermal cells to inhibit melanogenesis or inhibit the formation of any product in the sequence of melanin formation, the substance can be used as an effective ingredient for skin whitening. The first step to initiate melanin ...

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01-08-2013 дата публикации

GENES FOR BIOSYNTHESIS OF TETRACYCLINE COMPOUNDS AND USES THEREOF

Номер: US20130196953A1
Принадлежит: UNIVERZA V LJUBLJANI

The invention relates to tetracycline products produced by genetically engineered cells, and to therapeutic methods using such tetracyclines. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway. 3. Use of a compound of for the treatment of bacterial or fungal infections claim 1 , treatment of malaria claim 1 , a neurodegenerative disease claim 1 , Parkinson's disease claim 1 , Huntington's claim 1 , disease claim 1 , periodontitis claim 1 , an autoimmune condition claim 1 , multiple sclerosis claim 1 , atherosclerosis claim 1 , rheumatoid arthritis claim 1 , osteoporosis claim 1 , tumour invasion claim 1 , cancer and inflammatory states.4. Use of a compound of for the treatment of bacterial or fungal infections.5. Use of a compound of for the treatment of bacterial or fungal infections claim 2 , treatment of malaria claim 2 , a neurodegenerative disease claim 2 , Parkinson's disease claim 2 , Huntington's claim 2 , disease claim 2 , periodontitis claim 2 , an autoimmune condition claim 2 , multiple sclerosis claim 2 , atherosclerosis claim 2 , rheumatoid arthritis claim 2 , osteoporosis claim 2 , tumour invasion claim 2 , cancer and inflammatory states.6. Use of a compound of for the treatment of bacterial or fungal infections. This application is a divisional of U.S. patent application Ser. No. 12/536,622 filed Aug. 6, 2009, now U.S. Pat. No. 8,361,777, which claims the benefit of EP Application No. 08014141.9 filed Aug. 7, 2008, the entire disclosures of which are incorporated herein by reference.This invention relates to genetically engineered cells, and to proteins and genes useful in the production of tetracycline compounds, to methods of producing tetracycline compounds, and to tetracyclines thereby produced. The present invention is based on the cloning and heterologous expression of genes encoding the chelocardin biosynthetic pathway.Tetracyclines are a large group of drugs with a ...

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01-08-2013 дата публикации

PROCESS FOR MANUFACTURING PERFLUOROOLEFINS BY PYROLYSIS OF PERFLUOROCARBONS IN THE PRESENCE OF HYDROGEN

Номер: US20130197281A1
Принадлежит: 3M INNOVATIVE PROPERTIES COMPANY

A process is described of pyrolyzing at least one perfluorinated hydrocarbon, or a material containing at least one perfluorinated hydrocarbon, in the presence of hydrogen, to yield a reaction mixture containing difluorocarbene. 1. A process comprising pyrolyzing at least one perfluorinated hydrocarbon , or a material containing at least one perfluorinated hydrocarbon , in a pyrolysis zone at a temperature between about 580 K and about 2000 K in the presence of hydrogen to yield a reaction mixture containing difluorocarbene , wherein the hydrogen is present in the pyrolysis zone in a molar ratio from about 0.1 to 8 mol hydrogen per mol of perfluorinated hydrocarbon.2. The process of wherein the pyrolysis is carried at in the pyrolysis zone at a temperature of from about from 600 K to 1100 K.3. The process of further comprising quenching said reaction mixture after it exits the pyrolysis zone to yield a product mixture containing tetrafluoroethene and/or hexafluoropropene and claim 1 , optionally claim 1 , separating tetrafluoroethene and/or hexafluoropropene from said product mixture.4. The process according wherein the perfluorinated hydrocarbon is a gas claim 1 , a liquid claim 1 , or a mixture thereof.5. The process according to wherein the perfluorinated hydrocarbon comprises a straight chain or branched perfluroalkane represented by the formula CF claim 1 , wherein n is an integer of from 2 to 25.6. The process according to claim 1 , wherein the perfluorinated hydrocarbon has a boiling point of not more than 250° C.7. The process according to wherein the pyrolysis is carried out in the absence of added carbon.8. The process according to further comprising quenching the reaction mixture comprising difluorocarbene to yield a product mixture containing tetrafluoroethene and/or hexafluoropropene and feeding back into the pyrolysis zone at least a part of the product mixture after removing tetrafluorethene and/or hexafluoropropene therefrom.9. The process according ...

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08-08-2013 дата публикации

Pharmaceutical Formulation for Histone Deacetylase Inhibitors

Номер: US20130203847A1
Принадлежит: SHAPE PHARMACEUTICALS, INC.

A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein. 2. The pharmaceutical composition of claim 1 , wherein the at least one acidifying agent is selected from the groups consisting of acetic acid claim 1 , dehydro acetic acid claim 1 , ascorbic acid claim 1 , benzoic acid claim 1 , boric acid claim 1 , citric acid claim 1 , edetic acid claim 1 , hydrochloric acid claim 1 , isostearic acid claim 1 , stearic acid claim 1 , lactic acid claim 1 , nitric acid claim 1 , oleic acid claim 1 , phosphoric acid claim 1 , sorbic acid claim 1 , sulfuric acid claim 1 , tartaric acid claim 1 , and undecylenic acid.3. The pharmaceutical composition of claim 2 , wherein the at least one acidifying agent is selected from citric acid claim 2 , acetic acid claim 2 , and phosphoric acid.4. The pharmaceutical composition of claim 1 , wherein the at least one pharmaceutically acceptable non-aqueous solvent is selected from the groups consisting of ethanol claim 1 , acetone claim 1 , benzyl alcohol claim 1 , 2-(2-ethoxyethoxy)ethanol claim 1 , diethylene glycol monoethyl ether claim 1 , glycerin claim 1 , propylene glycol claim 1 , propylene carbonate claim 1 , acetone claim 1 , hexylene glycol claim 1 , isopropyl alcohol claim 1 , polyethylene glycols (PEGs) claim 1 , methoxypolyethylene glycols claim 1 , diethyl sebacate claim 1 , dimethyl isosorbide claim 1 , propylene carbonate claim 1 , dimethyl sulfoxide (DMSO) claim 1 , diisopropyl adipate claim 1 , isopropyl myristate claim 1 , vegetable oils claim 1 , a mineral oil claim 1 , and isopropyl palmitate.5. The pharmaceutical composition of claim 4 , wherein the at least one pharmaceutically acceptable ...

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08-08-2013 дата публикации

Pharmaceutical Dopamine Glycoconjugate Compositions and Methods of Their Preparation and Use

Номер: US20130203855A1
Автор: Christian Samuel T.
Принадлежит: Glycon LLC

Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds and methods of their use. 138-. (canceled)41. Dopamine ribonamide or a pharmaceutically acceptable salt thereof.42. Dopamine ribonamine or a pharmaceutically acceptable salt thereof.44. A process for preparing a compound of claim 39 , comprising:reacting a lactone of a sugar and an optionally substituted phenethylamine, andcollecting the phenethylamide.45. A process of preparing a compound of claim 43 , comprisingreacting a lactone of a sugar and 3-hydroxytyramine, andcollecting the dopamine amide.46. A method of treating neurological dysfunction in a subject comprising administering to the subject a compound of . The present application is a continuation-in-part of U.S. patent application Ser. No. 11/965,444, filed Dec. 27, 2007, which issued as U.S. Pat. No. 8,252,752 on Aug. 28, 2012, which is a continuation of U.S. patent application Ser. No. 10/625,645, filed Jul. 22, 2003, which issued as U.S. Pat. No. 7,345,031 on Mar. 18, 2008. The present application is a continuation-in-part of U.S. patent application Ser. No. 12/913,543, filed Oct. 27, 2010, which is a continuation of U.S. patent application Ser. No. 11/343,266, filed Jan. 30, 2006, which is abandoned and is a continuation of U.S. patent application Ser. No. 09/547,501, filed Apr. 12, 2000, which is abandoned. The foregoing patents and patent applications are incorporated herein by reference in their entirety.The invention relates generally to dopaminergic compositions and methods of their preparation and use for treating neurological diseases including Parkinson's and related diseases.Parkinson's disease reportedly affects one person in fifty over fifty years of age and one in twenty over seventy. A degenerative disease of the nervous system described in 1817 and characterized by progressive loss of nigrostriatal neurons, a shaking palsy with tremor at rest, muscular rigidity and slowness of movement, the possible etiology, the ...

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08-08-2013 дата публикации

Fast-Dissolving Solid Pharmaceutical Form for Treating Bacterial Infections

Номер: US20130203858A1
Принадлежит: Nanocore Biotecnologia S.A.

The present invention relates to solid pharmaceutical compositions that dissolve readily and stably and which are capable of inhibiting or eliminating an infectious process caused by bacteria in warm-blooded animals and aquatic species such as, for example, fish and crustaceans. The invention describes composition for formulations containing antibiotics to be administered by various routes for treating bacterial infections in warm-blooded animals and aquatic animals. The formulation can be intended for human and animal use. 1. A pharmaceutical composition for treatment of infections in warm-blooded animals and aquatic species comprising:(a) at least one drug selected from the group of amphenicol antibiotics or mixture of amphenicols;(b) at least one carrier selected from the group of sugars in concentrations between 20% to 83%, preferably between 60 to 82%;(c) a polyalcohol of low molecular weight; and(d) a surfactant from the group of polysorbates.2. The composition according to wherein the drug from the group of amphenicol be florfenicol.3. The composition according to wherein the drug from the group of amphenicol be thiamphenicol.4. The composition according to wherein the florfenicol is in diluted in the formulation at a concentration of 1% to 50% w/w claim 2 , preferably 10% to 25% w/w.5. The composition according to wherein thiamphenicol is diluted at a concentration of 1% to 50% w/w claim 3 , preferably 10% to 25% w/w claim 3 , more preferably 10% w/w.6. The composition according to wherein the carrier is lactose.7. The composition according to wherein the concentration of lactose is between 20% and 83% w/w.8. The composition according to wherein the polyalcohol is a low molecular weight polyethylene glycol (PEG 400).9. The composition according to wherein the surfactant is polysorbate 80.10. The composition according to wherein an adjuvant is added to increase the fluidity of the powder.11. The composition according to wherein the adjuvant is colloidal ...

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08-08-2013 дата публикации

PROCESSES FOR REDUCING IMPURITIES IN LACOSAMIDE

Номер: US20130204042A1
Принадлежит: RANBAXY LABORATORIES LIMITED

The present invention relates to processes for reducing impurities in lacosamide during the preparation of lacosamide. The invention provides processes for minimizing or removing impurities such as (2R)-2-(acetylamino)-3-(benzylamino)-3-oxopropyl acetate of Formula II or (2R)-2-propanoylamino-N-benzyl-3-methoxypropionamide of Formula III in lacosamide. 2. The process of wherein the lacosamide prepared is substantially free of Impurity-A and/or Impurity-B.4. The process of wherein the lacosamide prepared is substantially free of Impurity-A and/or Impurity-B.5. A process for reducing the content of “Impurity-A” in lacosamide during the preparation of lacosamide that comprises the step of treating D-serine with a protecting reagent wherein the number of moles of the protecting reagent is less than the number of moles of D-serine.6. The process of wherein the lacosamide prepared is substantially free of Impurity-A.8. The process of wherein lacosamide prepared is substantially free of Impurity-B.9. Lacosamide substantially free of Impurity-A and Impurity-B.10. Lacosamide substantially free of Impurity-A.11. Lacosamide substantially free of Impurity-B. The present invention relates to processes for reducing impurities in lacosamide during preparation of lacosamide. The invention provides processes for minimizing or removing impurities such as (2R)-2-(acetylamino)-3-(benzylamino)-3-oxopropyl acetate of Formula II or (2R)-2-propanoylamino-N-benzyl-3-methoxypropionamide of Formula III in lacosamide.Lacosamide (SPM 927, also referred to as harkoseride or ADD 234037), is chemically (R)-2-acetamido-N-benzyl-3-methoxypropionamide and represented by Formula I. It has been reported to be effective for the treatment of pain, epilepsy, fibromyalgia syndrome, osteoarthritis and migraine. It is also known to be useful for the treatment of CNS disorders in humans.Lacosamide is available in the United States market as solution and tablet dosage forms with proprietary name of Vimpat®. ...

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08-08-2013 дата публикации

CATALYST FOR PREPARING VINYL CHLORIDE, METHODS OF PREPARATION AND APPLICATION THEREOF

Номер: US20130204052A1
Автор: Jiang Biao, Zhong Jinguang
Принадлежит:

The present invention discloses a catalyst used in preparing vinyl chloride, its method of preparation, and its applications. Said catalyst used in making vinyl chloride comprises activated carbon as a support, a barium compound and a phosphorus compound supported thereon. The barium compound accounts for 0.2% to 20% of the total mass of the catalyst and the phosphorus compound accounts for 0% to 10% of the total mass of the catalyst based on the mass percentage. A water-soluble barium compound, a water-soluble phosphorus compound, an aqueous polymer monomer, and water are mixed to form a solution or emulsion A. The activated carbon is added into the solution or emulsion A. The activated carbon is removed from water after impregnation, spin-dried, and then the monomers are polymerized. The activated carbon, after polymerization step, is heated to remove water and to decompose and carbonize the polymer. The catalyst after carbonization was activated to obtain a catalyst used in making vinyl chloride. 1. A catalyst for the preparation of vinyl chloride , characterized in that:said catalyst comprises activated carbon as a carrier, a barium compound and a phosphorus compound supported on the carrier, wherein said barium compound has a mass percentage of 0.2% to 20% and said phosphorous compound has a mass percentage of 0% to 10% based on the total mass of the catalyst.2. The catalyst of claim 1 , wherein said barium compound is barium chloride and said phosphorus compound is phosphoric acid.3. A method for preparing a catalyst of used in preparing vinyl chloride claim 1 , characterized in that said method comprising the steps of:(1) mixing a water-soluble barium compound, a water-soluble phosphorus compound, an aqueous polymer monomer, and water to obtain a solution A or an emulsion A;(2) impregnating the activated carbon in the solution A or the emulsion A;(3) polymerizing the aqueous polymeric monomer on the activated carbon after spin-drying;(4) heating the activated ...

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15-08-2013 дата публикации

Novel esteramide compounds, methods for preparing same, and uses thereof

Номер: US20130210634A1
Принадлежит: Rhodia Operations SAS

An esteramide compound of the following formula (I): R 1 OOC-A-CONR 2 R 3   (I) is described, wherein: A is a covalent bond or a methylene group —CH 2 —; R 1 is an optionally substituted, saturated or unsaturated aliphatic or cycloaliphatic hydrocarbon group including from 5 to 36 carbon atoms, R 2 and R 3 , either identical or different, are groups selected from a hydrogen atom, and optionally substituted hydrocarbon groups, preferably including from 1 to 36 carbon atoms, and R 2 and R 3 not being simultaneously hydrogen atoms. Also described, are applications for using the esteramide compound, notably as a solvent.

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15-08-2013 дата публикации

PHOTOLABILE CAGED TRANSITION METAL COMPLEXES AND METHODS OF USING THE SAME

Номер: US20130210793A1
Принадлежит: Duke University

The present invention provides compounds of Formula I: 2. The compound of claim 1 , wherein Z is absent.3. The compound of claim 1 , wherein Z is a transition metal.4. The compound of claim 1 , wherein Z is a transition metal selected from the group consisting of copper claim 1 , platinum claim 1 , iron and zinc.5. The compound of claim 1 , wherein at least one adjacent pair of Rand Rtogether form a heteroaryl selected from the group consisting of pyrimidine claim 1 , thiazole claim 1 , thiophene claim 1 , isoquinoline claim 1 , imidazole claim 1 , and pyrroline.6. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.7. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.8. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.9. The compound of claim 1 , wherein Ris selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.10. The compound of claim 1 , wherein Rand Rtogether form oxo.11. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.12. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , halo claim 1 , and sulfonate.13. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , and halo.14. The compound of claim 1 , wherein each Ris independently selected from the group consisting of: H claim 1 , alkyl claim 1 , alkoxy claim 1 , and halo.16. A composition comprising a compound of in a pharmaceutically acceptable carrier.1718-. ( ...

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15-08-2013 дата публикации

SORAFENIB DIMETHYL SULPHOXIDE SOLVATE

Номер: US20130210865A1
Принадлежит: RANBAXY LABORATORIES LIMITED

The present invention provides dimethyl sulphoxide solvate of 4-(4-{3-[4-chloro-3-(trifluoromethyl)phenyl]ureido}phenoxy)-N-methylpyridine-2-carboxamide, process for its preparation, pharmaceutical composition comprising it and its use for the treatment of cancer. The present invention also provides a novel HPLC method for the identification, quantification and isolation of related substances of sorafenib. 2. Sorafenib dimethyl sulphoxide solvate according to further characterized by X-ray diffraction peaks at d-spacing 5.36 claim 1 , 4.47 claim 1 , 4.44 claim 1 , 3.26 and 3.14 Å.3. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by X-ray diffraction pattern as depicted in .4. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by DSC thermogram having endotherms at about 123.69° C. and about 202.54° C.5. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by DSC thermogram as depicted in .6. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by X-ray diffraction pattern as depicted in and DSC thermogram as depicted in .7. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by TGA as depicted in .8. Sorafenib dimethyl sulphoxide solvate of Formula III characterized by IR spectrum as depicted in .9. Sorafenib dimethyl sulphoxide solvate of Formula III having purity greater than 99% by HPLC.11. The process according to claim 10 , wherein Sorafenib free base of Formula I is contacted with dimethyl sulphoxide at a temperature of about 15° C. to the reflux temperature of dimethyl sulphoxide.13. The process according to claim 12 , wherein the solvent is selected from the group consisting of water claim 12 , chlorinated hydrocarbons claim 12 , alcohols claim 12 , ketones claim 12 , alkyl acetates claim 12 , ethers and mixtures thereof.14. The process according to claim 12 , wherein sorafenib dimethyl sulphoxide solvate of Formula III is contacted with a solvent at a temperature of about −5° C. ...

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