Настройки

Укажите год
-

Небесная энциклопедия

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год
Применить Всего найдено 2359. Отображено 100.
05-07-2012 дата публикации

Phosphatidyl oligoglycerols

Номер: US20120172631A1
Автор: Hans-Jorg Eibl
Принадлежит: Max Planck Gesellschaft zur Foerderung der Wissenschaften eV

In order to form liposomes with a longer half-life in blood, use is made of defined compounds with the general formula (A)

Подробнее
Номер записи: 1
10-01-2013 дата публикации

Monomers, polymers, photoresist compositions and methods of forming photolithographic patterns

Номер: US20130011783A1
Автор: Jong Keun Park, Matthias S. Ober, Seung-Hyun Lee, Yi Liu, Young Cheol Bae
Принадлежит: Dow Global Technologies LLC, Rohm and Haas Electronic Materials LLC

Provided are (meth)acrylate monomers containing acetal moieties, polymers containing a unit formed from such a monomer and photoresist compositions containing such a polymer. The monomers, polymers and photoresist compositions are useful in forming photolithographic patterns. Also provided are substrates coated with the photoresist compositions, methods of forming photolithographic patterns and electronic devices. The compositions, methods and coated substrates find particular applicability in the manufacture of semiconductor devices.

Подробнее
Номер записи: 2
21-02-2013 дата публикации

Aromatic monomers deriving from glycerol units, process for their preparation and use thereof for the preparation of water-soluble conjugated polymers

Номер: US20130046072A1
Автор: Andrea Pellegrino, Giuliana Schimperna, Maria Caldararo, Riccardo Po'
Принадлежит: Eni Spa

Monomers having formula (I) and process for their synthesis which comprises the etherification reaction of a halogen-derivative (Z═Cl, Br, I) having formula (III) with the hydroxyl group of the glycerol derivative (IV), according to the following scheme:(Formula III, IV & I) (III) (IV) (I)

Подробнее
Номер записи: 3
21-03-2013 дата публикации

Method for Producing (2R)-2-Fluoro-2-C-Methyl-D-Ribono-y-Lactone Precursor

Номер: US20130072699A1
Автор: Ishii Akihiro, Nagura Hirokatsu, Tsuruta Hideyuki
Принадлежит: CENTRAL GLASS COMPANY, LIMITED

In the presence invention, a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is produced in the form of a ring-opened fluorinated compound by reaction of a 1,2-diol with sulfuryl fluoride (SOF) in the presence of an organic base and, optionally, a fluoride ion source. The production method of the present invention secures less number of process steps as compared to the conventional production method (shortening of three steps: cyclic sulfurous esterification, oxidation and ring-opening fluorination to one step) and satisfies the requirements for industrial production (high yield and high reproductivity). The thus-obtained (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor is useful as an important intermediate for the synthesis of 2′-deoxy-2′-fluoro-2′-C-methylcytidine with antivirus activity. The present invention relates to a method for producing a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor.There have been reported some methods for production of (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursors. In any of these production methods, the stereoselective introduction of a fluorine atom to 2-position is a significant problem. Ring-opening fluorination of a cyclic sulfuric ester is known as a fluorine atom introduction technique suitable for mass-scale production (see Patent Documents 1 and 2 and Non-Patent Document 1). Using this technique, it is feasible to produce a (2R)-2-fluoro-2-C-methyl-D-ribono-γ-lactone precursor in the form of a ring-opened fluorinated compound in three steps (first step: cyclic sulfurous esterification, second step: oxidation, third step: ring-opening fluorination) from a 1,2-diol substrate (see Scheme 1 where Me is a methyl group; Et is an ethyl group; X is a proton, a protonated organic base, a metal cation, a tetraalkylammonium or a tris(dialkylamino)sulfonium; and Bz is a benzoyl group). There is also reported a modified production method for producing a ring-opened fluorinated compound in two steps (first step: ...

Подробнее
Номер записи: 4
30-05-2013 дата публикации

DIOXOLANE COMPOUND, LIQUID CRYSTAL COMPOSITION, LIQUID CRYSTAL ELEMENT, AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20130134353A1
Автор: Ishitani Tetsuji, Kato Momoko, Kawata Yuko, Niikura Yasuhiro
Принадлежит: SEMICONDUCTOR ENGERGY LABORATORY CO., LTD

A novel dioxolane compound represented by the general formula (G1) is provided. In the general formula (G1), Rand Rseparately represent any of hydrogen, an alkylene group having 1 to 6 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, an aryl group having 6 to 12 carbon atoms, and an alkylene group having 1 to 20 carbon atoms and a phenyl group as a substituent; aand aseparately represent any of an alkylene group having 1 to 4 carbon atoms and a single bond; Arand Arseparately represent an aryl group having 6 to 16 carbon atoms; and Rto Rseparately represent any of hydrogen, an alkylene group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, and an aryl group having 6 to 12 carbon atoms. 2. The dioxolane compound according to claim 1 , wherein each of aand ais a methylene group.3. The dioxolane compound according to claim 1 , wherein Rand Rare bonded to each other to form a ring.4. A liquid crystal composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the dioxolane compound according to ; and'}a nematic liquid crystal,wherein the liquid crystal composition exhibits a blue phase.5. The liquid crystal composition according to claim 4 , wherein a proportion of the dioxolane compound included in the liquid crystal composition is lower than or equal to 15 wt %.6. A liquid crystal display device comprising the dioxolane compound according to .7. The liquid crystal display device according to claim 6 , wherein the liquid crystal composition comprises an organic resin.9. The dioxolane compound according to claim 8 , wherein Rand Rbonded to each other to form a cyclohexyl ring.10. A liquid crystal composition comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'the dioxolane compound according to ; and'}a nematic liquid crystal,wherein the liquid crystal composition exhibits a blue phase.11. The liquid crystal composition according to claim 10 , wherein a proportion of the dioxolane compound included in the liquid ...

Подробнее
Номер записи: 5
11-07-2013 дата публикации

PROCESS FOR PRODUCING DIOXOLANE

Номер: US20130178638A1
Автор: Mastroianni Sergio
Принадлежит: Rhodia Operations

A process is described for producing dioxolane from crude glycerol obtained from raw materials such as the crude glycerol obtained during production of biodiesel or glycerol obtained during conversion of fats or oils. Further, the described method can dissolve the glycerol in an organic solvent and form an insoluble phase including salts included in the crude glycerol, and then react the glycerol obtained with an aldehyde or a ketone. 1. A process for producing dioxolane , the process comprising the following steps:(a) bringing together crude glycerol and at least one organic solvent comprising from 1 carbon atom to 10 carbon atoms and comprising at least one of a ketone, an aldehyde, an alcohol, an acetal and/or a ketal function, so as to form a liquid phase comprising the-glycerol dissolved in the solvent(s) and to also form an insoluble phase;(b) separating the insoluble phase and the liquid phase;(c) optionally separating the solvent and the glycerol from the liquid phase;(d) adding to the liquid phase or to the glycerol (if step (c) is carried out) a catalyst, and optionally a ketone or an aldehyde, so as to form a dioxolane by catalyzed reaction between the glycerol and the ketone or the aldehyde; and(e) recovering the dioxolane.2. The process as defined by claim 1 , wherein the crude glycerol originates from a renewable raw material.3. The process as defined by claim 1 , wherein the crude glycerol is obtained during production of biodiesel or obtained during conversion of a fat or an oil.4. The process as defined by claim 1 , wherein the ketone is selected from the group consisting of an acetone claim 1 , a cyclohexanone claim 1 , a methylcylohexanone claim 1 , a cyclopentanone claim 1 , a methylcyclopentanone and a methyl isobutyl ketone.5. The method as defined by claim 1 , wherein the aldehyde is selected from the group consisting of a formaldehyde claim 1 , an acetaldehyde and a furfuraldehyde.6. The method as defined by claim 1 , wherein the alcohol is ...

Подробнее
Номер записи: 6
18-07-2013 дата публикации

Process for the Preparation of 1-ARYL-PYRAZOL-3-ONE Intermediates Useful in the Synthesis of SIGMA Receptors Inhibitors

Номер: US20130184472A1
Автор: Ariza Piquer Javier, Bartra Sanmartí Martí, Berenguer Maimó Ramón, Garcia Gomez Jorge, Medrano Rupérez Jorge
Принадлежит: ESTEVE QUIMICA, S.A.

The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors. 4. The process according to claim 1 , wherein the compound of formula (IV) is obtained by reacting a salt of the compound of formula (IV) with a base.5. The process according to claim 1 , where the reaction of a salt of compound of the formula (IV) with a base is performed in the same reaction mixture of .6. The process according to claim 1 , wherein the coupling agent in step a1) is a carbodiimide claim 1 , preferably dicyclohexylcarbodiimide (DCC) claim 1 , diisopropylcarbodiimide (DIC) claim 1 , or N-ethyl-N′-[(3-dimethylamino)propyl]carbodiimide (EDC).7. The process according to claim 1 , wherein the activating agent of the coupling agent in step a1) is selected from 1-hydroxybenzotriazole (HOBt) and 4-dimethylaminopyridine (4-DMAP).8. The process according to claim 1 , wherein the activating agent in step a2) is selected from a halogenating agent claim 1 , Calkyl acid halide claim 1 , aryl acid halide claim 1 , benzyl acid halide claim 1 , Calkyl haloformate claim 1 , aryl haloformate claim 1 , and benzyl haloformate.10. The process according to claim 2 , wherein the cleavage of the ketal or acetal group of compound of formula (V) is performed by acidic treatment in an aqueous medium claim 2 , an organic solvent claim 2 , or a mixture thereof. The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.Psychiatric and neurologic disorders are among the most severe and chronic diseases and conditions. These disorders are also extremely difficult to treat effectively because of the multiplicity of the symptoms and etiologies.Amongst the therapeutic arsenal to combat these psychiatric ...

Подробнее
Номер записи: 7
25-07-2013 дата публикации

Novel Tetrahydronaphalene Antagonists to the Thromboxane A2 (TP) Receptor

Номер: US20130190370A1
Автор: Ballatore Carlo, Brunden Kurt R., Hogan Anne-Marie, Huryn Donna M., Lee Virginia M.Y., PISCITELLI Francesco, Smith Amos B., Trojanowski John Q.
Принадлежит: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA

The present invention relates to TP receptor antagonists, which have the ability to bind to TP receptor and optionally cross the blood brain barrier. The invention also provides compositions and methods for treating a disorder wherein activation of TP receptor is detrimental. 1. A composition comprising a TP receptor antagonist , wherein said antagonist comprises the chemical structures set forth in , a salt thereof , a prodrug thereof , and combinations thereof.2. The composition of claim 1 , wherein said antagonist binds to a TP receptor or a TP-like receptor.3. The composition of claim 1 , wherein said antagonist inhibits activation of a TP receptor or a TP-like receptor.4. The composition of claim 1 , wherein said antagonist is able to cross the blood brain barrier of a mammal.5. The composition of claim 1 , wherein said antagonist is not able to cross the blood brain barrier of a mammal.6. The composition of claim 1 , wherein said antagonist is selected from the group consisting of CNDR-51418 claim 1 , CNDR-51281 claim 1 , CNDR-51354 and CNDR-51414.7. A method of treating a disorder associated with activation of a TP receptor in a mammal in need thereof claim 1 , said method comprising administering to said mammal a therapeutically effective amount of a compound claim 1 , wherein said compound comprises a TP receptor antagonist claim 1 , wherein said antagonist comprises the chemical structures set forth in claim 1 , a salt thereof claim 1 , a prodrug thereof claim 1 , and combinations thereof.8. The method of claim 7 , wherein said antagonist is able to cross the blood brain barrier of said mammal.9. The method of claim 7 , wherein said antagonist is not able to cross the blood brain barrier of said mammal.10. The method of claim 7 , wherein said mammal is a human.11. The method of claim 7 , wherein said disorder associated with activation of a TP receptor is a neurodegenerative disorder.12. The method of claim 11 , wherein said neurodegenerative disorder is ...

Подробнее
Номер записи: 8
15-08-2013 дата публикации

Intermediates and methods for making zearalenone macrolide analogs

Номер: US20130211103A1
Автор: Charles-Andre Lemelin, Francis G. Fang, Hong Du, Jing Li, Kevin (kuo-ming) Wu, Matthew J. Schnaderbeck, Pamela Mcguinness, Roch Boivin, Silvio A. Campagna, Thomas Horstmann, Xiang Niu, Xiaojie (Jeff) Zhu
Принадлежит: Eisai R&D Management Co Ltd

Disclosed herein are methods and intermediates useful in the preparation of macrolides, e.g., compounds of formula (IV) wherein R 1 -R 12 are as defined herein.

Подробнее
Номер записи: 9
03-10-2013 дата публикации

PREPARATION OF (R)-N-(3,4-DIFLUORO-2-(2-FLUORO-4-IODOPHENYLAMINO)-6-METHOXYPHENYL)-1-(2,3-DIHYDROXYPROPYL)CYCLOPROPANE-1-SULFONAMIDE AND (S)- N-(3,4-DIFLUORO-2-(2-FLUORO-4-IODOPHENYLAMINO)-6-METHOXYPHENYL)-1-(2,3-DIHYDROXYPROPYL)CYCLOPROPANE-1-SULFONAMIDE

Номер: US20130261320A1
Автор: MADERNA Andreas, VERNIER Jean Michel
Принадлежит: Ardea Biosciences, Inc.

The present invention relates to the preparation of (R)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide and (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. 5. A process of claim 1 , wherein Rand Rtogether with the carbon atoms to which they are attached form a cyclic 1 claim 1 ,2-diol protecting group.6. The process of claim 5 , wherein the cyclic 1 claim 5 ,2-diol protecting group is a 5-membered cyclic 1 claim 5 ,2-diol protecting group.7. The process of claim 6 , wherein the cyclic 1 claim 6 ,2-diol protecting group is 2 claim 6 ,2-dimethyl-1 claim 6 ,3-dioxolan-4-yl.811-. (canceled)12. A process of claim 2 , wherein Rand Rtogether with the carbon atoms to which they are attached form a cyclic 1 claim 2 ,2-diol protecting group.13. A process of claim 3 , wherein Rand Rtogether with the carbon atoms to which they are attached form a cyclic 1 claim 3 ,2-diol protecting group.14. A process of claim 4 , wherein Rand Rtogether with the carbon atoms to which they are attached form a cyclic 1 claim 4 ,2-diol protecting group.15. The process of claim 12 , wherein the cyclic 1 claim 12 ,2-diol protecting group is a 5-membered cyclic 1 claim 12 ,2-diol protecting group.16. The process of claim 13 , wherein the cyclic 1 claim 13 ,2-diol protecting group is a 5-membered cyclic 1 claim 13 ,2-diol protecting group.17. The process of claim 14 , wherein the cyclic 1 claim 14 ,2-diol protecting group is a 5-membered cyclic 1 claim 14 ,2-diol protecting group.18. The process of claim 12 , wherein the cyclic 1 claim 12 ,2-diol protecting group is 2 claim 12 ,2-dimethyl-1 claim 12 ,3-dioxolan-4-yl.19. The process of claim 13 , wherein the cyclic 1 claim 13 ,2-diol protecting group is 2 claim 13 ,2-dimethyl-1 claim 13 ,3-dioxolan-4-yl.20. The process of claim 14 , wherein the cyclic 1 claim 14 ,2-diol protecting group is 2 claim 14 ,2-dimethyl-1 ...

Подробнее
Номер записи: 10
19-12-2013 дата публикации

PREPARATION OF 2'-FLUORO-2'-ALKYL-SUBSTITUTED OR OTHER OPTIONALLY SUBSTITUTED RIBOFURANOSYL PYRIMIDINES AND PURINES AND THEIR DERIVATIVES

Номер: US20130338349A1
Автор: Chun Byoung-Kwon, Du Jinfa, Rachakonda Suguna, Wang Peiyuan
Принадлежит:

The present invention provides (i) processes for preparing a 2′-deoxy-2′-fluoro-2′-methyl-D-ribonolactone derivatives, (ii) conversion of intermediate lactones to nucleosides with potent anti-HCV activity, and their analogues, and (iii) methods to prepare the anti-HCV nucleosides containing the 2′-deoxy-2′-fluoro-2′-C-methyl-β-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside. 8. The compound of claim 7 , wherein Ris H and Ris methyl. This application a continuation of U.S. patent application Ser. No. 11/225,425, filed Sep. 13, 2005, which claims the benefit of Provisional Patent Application Ser. No. 60/609,783, filed Sep. 14, 2004, Provisional Patent Application Ser. No. 60/610,035, filed Sep. 15, 2004, and Provisional Patent Application Ser. No. 60/666,230, filed Mar. 29, 2005. The entire contents of all of the above-mentioned applications are incorporated herein by reference.The present invention provides (i) processes for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivatives, (ii) conversion of intermediate lactones to nucleosides with potent anti-HCV activity, and their analogues, and (iii) methods to prepare the anti-HCV nucleosides containing the 2′-deoxy-2′-fluoro-2′-C-methyl-β-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.HCV infection has reached epidemic levels worldwide, and has tragic effects on the infected patients. Presently there is no effective treatment for this infection and the only drugs available for treatment of chronic hepatitis C are various forms of alpha interferon (IFN-a), either alone or in combination with ribavirin. However, the therapeutic value of these treatments has been compromised largely due to adverse effects, which highlights the need for development of additional options for treatment.HCV is a small, enveloped virus in the Flaviviridae family, with a positive single-stranded RNA genome of ˜9.6 kb within the nucleocapsid. The genome ...

Подробнее
Номер записи: 11
19-12-2013 дата публикации

PROCESSES AND INTERMEDIATES FOR PREPARING SUBSTITUTED HEXAHYDROFURO [2,3-b] FURANS

Номер: US20130338380A1
Автор: Ghosh Arun K., Martyr Cuthbert D.
Принадлежит: PURDUE RESEARCH FOUNDATION

The invention described herein pertains to processes and compounds useful in the preparation of bis-tetrahydrofurans. The invention described herein also pertains to compounds useful for treating HIV infections. 2. (canceled)5. (canceled)16. The process of wherein the base is a lithium alkoxide claim 1 , a sodium alkoxide claim 1 , a potassium alkoxide claim 1 , a lithium amide claim 1 , a sodium amide claim 1 , a magnesium amide claim 1 , or a potassium amide.17. The process of wherein the inverting step includes converting the free hydroxyl to an ester of a carboxylic acid.18. The process of wherein the reducing agent is selected from the group consisting of a lithium hydridoaluminate and a sodium hydridoaluminate.19. The process of wherein the reducing agent is lithium aluminum hydride or sodium bis(2-methoxyethoxo)-dihydridoaluminate.20. The process of wherein the base is potassium t-butoxide claim 1 , sodium t-amyloxide claim 1 , or lithium hexamethyldisilazide.21. The process of wherein the oxidizing agent is selected from the group consisting of ozone claim 1 , NaIO—RuO claim 1 , and NaIO—OsO.22. The process of wherein the oxidizing agent is ozone.23. (canceled)25. (canceled)27. The process of wherein n is 0.29. The process of wherein n is 0. This application claims the benefit under 35 USC §119(e) of U.S. Provisional Application Ser. No. 61/418,123 filed on Nov. 30, 2010, the entire disclosure of which is incorporated herein by reference.The invention described herein pertains to processes and compounds useful in the preparation of bis-tetrahydrofurans. The invention described herein also pertains to compounds useful for treating HIV infections.In recent years, the bis-tetrahydrofuranyl ligand has become an important ligand in the design of HIV-protease inhibitors. Since its discovery, it has been the salient feature in many drug candidates. Darunavir, (1), the first FDA approved second generation protease inhibitor, is currently being used in the treatment ...

Подробнее
Номер записи: 12
27-02-2014 дата публикации

SULFONATED CARBON SILICA COMPOSITE MATERIAL AND A PROCESS FOR THE PREPARATION THEREOF

Номер: US20140057778A1
Автор: NANDAN DEVAKI, VISWANADHAM NAGABHATLA
Принадлежит: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

The present invention relates to a novel sulfonated carbon silica (SCS) composite material and a process for the preparation thereof. The synthesized SCS composite material on calcination yields the hierarchical mesoporous silica (MS) and further finds application as catalyst in two industrially important reactions namely phenol butylation and glycerol acetalization. 16.-. (canceled)7. A process of preparing a Sulfonated carbon silica (SCS) composite comprising:(a) gradually mixing a saccharide with a silica source and a sulfuric acid to form a reaction mixture, wherein a ratio between saccharide and the silica source is in the range of about 0.385 to about 4.25 and a quantity of the sulphuric acid is in the range of 0.234 to 1.020 M;(b) allowing a hydrolyzing reaction to progress in the mixture reaction by maintaining the reaction mixture at a temperature in the range of about 298 K to 320 K for a period in the range of about 2 to about 5 hours to effect hydrolyzation thereby to obtain a gel;(c) treating the gel thus obtained in step (b) at a temperature in the range of about 350 K to about 423 K for a period in the range of about 12 hours to about 18 hours to obtain a bulk solid mass; and(d) heating the bulk solid mass as obtained in (c) at a temperature in range of about 473 K to about 573 K for a period in the range of about 4 hours to about 8 hours under nitrogen gas to obtain the sulfonated carbon silica (SCS) composite.8. The process according to claim 7 , wherein step (c) comprises treating the gel as obtained in step (b) inside a Teflon-lined autoclave at a temperature in the range of about 350 K to about 423 K for a period in the range of about 12 hours to about 18 hours to obtain bulk solid mass.9. The process according to claim 7 , further comprising washing the sulfonated carbon silica composite at least once.10. The process according to claim 9 , further comprising drying the sulfonated carbon silica composite.11. The process according to claim 9 , ...

Подробнее
Номер записи: 13
06-03-2014 дата публикации

ANTIOXIDANT INFLAMMATION MODULATORS: C-17 HOMOLOGATED OLEANOLIC ACID DERIVATIVES

Номер: US20140066408A1
Автор: GREINER Jack, Jiang Xin, LIU Xiaofeng, SZUCS Stephen S., Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: 614-. (canceled)15. The compound of claim 5 , wherein Y is alkanediylor substituted alkanediyl.1618-. (canceled)19. The compound of claim 5 , wherein Xis ORand Ris absent.20. The compound of claim 4 , wherein Xis hydrogen.21. The compound of claim 5 , wherein Ris —OH.2228-. (canceled)29. The compound of claim 5 , wherein Ris acylor substituted acyl.30. The compound of claim 29 , wherein Ris selected from the group consisting of —C(═O)OH claim 29 , —C(═O)OCH claim 29 , —C(═O)NHCH claim 29 , —C(═O)NHCHCH claim 29 , and —C(═O)NHCHCF.31. The compound of claim 5 , wherein Ris acyloxyor substituted acyloxy.3246-. (canceled)47. The compound of claim 5 , wherein Ris —CN.4850-. (canceled)51. The compound of claim 3 , wherein Ris absent.5253-. (canceled)54. The compound of claim 2 , wherein Rand Rare each methyl.55. The compound of claim 2 , wherein Rand Rare each hydrogen.56. The compound of claim 1 , wherein Rand Rare each hydrogen.57. The compound of claim 1 , wherein Rand Rare each methyl.58. (canceled)59. The compound of claim 5 , wherein the bond between carbons 9 and 11 is a single bond.60. The compound of claim 5 , wherein the bond between carbons 9 and 11 is a double bond.61137-. (canceled)138. A pharmaceutical composition comprising as an active ingredient a compound of and a pharmaceutically acceptable carrier.139146-. (canceled)147. A therapeutic method comprising administering a pharmaceutically effective amount of a compound of to a subject.148. The method of claim 147 , wherein the subject is a human.149. (canceled)150. A method of treating cancer in a subject claim 5 , comprising administering to the subject a pharmaceutically effective amount of a compound of .151173-. (canceled)174. A method of treating or preventing a disease with an inflammatory component in a subject claim 5 , comprising administering to the subject a pharmaceutically effective amount of a ...

Подробнее
Номер записи: 14
03-04-2014 дата публикации

Process for producing ester compound

Номер: US20140094616A1
Автор: Leopold Mpaka LUTETE, Tetsuya Ikemoto, Toshiaki Aikawa
Принадлежит: Sumitomo Chemical Co Ltd

Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R 5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.

Подробнее
Номер записи: 15
10-04-2014 дата публикации

SYNTHESIS PROCESS, AND CRYSTALLINE FORM OF 4- BENZAMIDE HYDROCHLORIDE AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT

Номер: US20140100374A1
Автор: Boiret Mathieu, Gaillard Marina, Lecouve Jean-Pierre, LERESTIF Jean-Michel, Letellier Philippe, Meunier Loic, ROBERT Nicolas
Принадлежит: LES LABORATOIRES SERVIER

Industrial synthesis process for the compound of formula (I): 2. The process according to claim 1 , wherein the reaction mixture obtained at the end of the reaction of the compound of formula (II) with ammonia is subjected to pyrolysis.3. The process according to claim 2 , wherein the pyrolysis is carried out at a temperature greater than or equal to 200° C.4. The process according to claim 2 , wherein the pyrolysis is carried out at a temperature greater than or equal to 280° C.5. The process according to claim 1 , wherein the conversion of the compound of formula (III) into the compound of formula (IV) is carried out in the presence of hydrogen and a metal or metal-containing catalyst.6. The process according to claim 1 , wherein the compound of formula (V) is 4-(3-chloropropoxy)benzamide.7. The process according to claim 1 , wherein the coupling reaction of the compound of formula (IV) with the compound of formula (V) is carried out in the presence of a carbonate claim 1 , an amine or a hydroxide.8. The process according to claim 1 , wherein the coupling reaction of the compound of formula (IV) with the compound of formula (V) is carried out in the presence of potassium carbonate or triethylamine.9. The process according to claim 1 , wherein the coupling reaction of the compound of formula (IV) with the compound of formula (V) is carried out in a polar medium composed of one or more polar solvents selected from water claim 1 , alcohols claim 1 , ketones claim 1 , ethers claim 1 , amides claim 1 , DMSO and acetonitrile.10. The process according to claim 1 , wherein the coupling reaction of the compound of formula (IV) with the compound of formula (V) is carried out in a water/acetonitrile mixture or a water/isopropanol mixture.11. The process according to claim 1 , wherein the salt formation step in the presence of HCl takes place in a solvent selected from water claim 1 , acetone and an alcohol.12. The process according to claim 1 , wherein the salt formation ...

Подробнее
Номер записи: 16
02-01-2020 дата публикации

METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG

Номер: US20200002261A1
Автор: Chambournier Gilles, Endres Gregory William, Fedij Victor, Hering Kirk William, II Thomas James, Krell, MAHMOUD Hussien Mahmoud
Принадлежит: CAYMAN CHEMICAL COMPANY INCORPORATED

The present invention provides processes for preparing a prostacyclin analogue of Formula I 4. The method of claim 3 , wherein the transition metal catalyst comprises a compound or complex either of which comprises copper having a +1 oxidation state.5. The method of claim 4 , wherein the transition metal catalyst comprises CuI.15. The method of claim 14 , further comprising the step of:xxiv) reacting the compound of Formula I with diethanolamine in the presence of an organic solvent to generate the diethanolamine salt of the compound of Formula I.18. The method of claim 17 , wherein the derivatizing reagent comprises 3 claim 17 ,5-dinitrobenzoyl chloride and the alcohol comprises methanol.20. The method of claim 19 , further comprising the step:xlii) recrystallizing the precipitate of step xli). This application is a divisional application of U.S. patent application Ser. No. 15/874,093, filed Jan. 18, 2018, which is a divisional application of U.S. patent application Ser. No. 15/583,457, filed May 1, 2017, now U.S. Pat. No. 9,908,834, issued Mar. 6, 2018, which is a divisional application of U.S. patent application Ser. No. 14/650,234, filed Jun. 5, 2015, which is a 35 U.S.C. § 371 United States National Phase Application of PCT Application Serial No. PCT/US2013/073474, filed Dec. 6, 2013, which claims the benefit of and priority to U.S. provisional application Ser. No. 61/734,672, filed Dec. 7, 2012, and 61/777,882, filed Mar. 12, 2013. The entire contents of the aforementioned disclosures are incorporated herein by reference in their entireties.The present invention relates to processes and intermediates for the preparation of prostacyclin analog that are useful for treating hypertension and other diseases.Prostacyclin derivatives and analogs are useful pharmaceutical compounds possessing activities such as platelet aggregation inhibition, gastric secretion reduction, lesion inhibition, vasodilation, and bronchodilation.Treprostinil is a synthetic prostacyclin ...

Подробнее
Номер записи: 17
04-02-2016 дата публикации

AROMATIC MONOMERS DERIVING FROM GLYCEROL UNITS, PROCESS FOR THEIR PREPARATION AND USE THEREOF FOR THE PREPARATION OF WATER-SOLUBLE CONJUGATED POLYMERS

Номер: US20160031864A1
Автор: "Po Riccardo", Caldararo Maria, Pellegrino Andrea, Schimperna Giuliana
Принадлежит: ENI S.P.A.

Monomers having formula (I) and process for their synthesis which comprises the etherification reaction of a halogen-derivative (Z═Cl, Br, I) having formula (III) with the hydroxyl group of the glycerol derivative (IV), according to the following scheme: 3. The monomers according to claim 2 , wherein Ar is a radical deriving from benzene claim 2 , fluorene claim 2 , thiophene claim 2 , carbazole claim 2 , dithienocyclopentadiene or from phenothiazine.4. The monomers according to claim 2 , wherein Ar′ is a radical deriving from thiophene claim 2 , thieno-thiophene claim 2 , thiazole claim 2 , carbazole claim 2 , dithienocyclopentadiene or from phenothiazine.57-. (canceled)9. The process according to claim 8 , wherein the molar ratios (I):(IX) used are between 1:2 and 1:4.10. The process according to claim 8 , wherein the reaction is carried out at temperatures ranging from 10 to 200° C. claim 8 , preferably from 30 to 150° C.12. The process according to claim 11 , wherein the polymerization reaction is a condensation reaction claim 11 , catalyzed by a derivative of a transition metal claim 11 , selected from palladium claim 11 , in the case of Suzuki claim 11 , Stille and Heck reactions claim 11 , or nickel claim 11 , in the case of a Yamamoto reaction. The present invention relates to aromatic monomers deriving from glycerol units and the process for their preparation as well as their use for the preparation of conjugated polymers/copolymers soluble in water or aqueous mixtures.As is known, photovoltaic devices are devices capable of converting the energy of a light radiation into electric energy. At present, most photovoltaic devices which can be used for practical applications exploit the physico-chemical properties of photoactive materials of the inorganic type, in particular high-purity crystalline silicon. As a result of the high production costs of silicon, scientific research, however, has long been orienting its efforts towards the development of alternative ...

Подробнее
Номер записи: 18
31-01-2019 дата публикации

Method for producing monomers from isomeric mixtures

Номер: US20190031638A1
Автор: BEYER Silvia, DAVE Gaurang, DILLMANN Hans-Jürgen, HARTMANN Patrik, HERZOG Volker, Knebel Joachim, KÖMMELT Sabine, MERBACH Ralf, SCHÜTZ Thorben, Trocha Martin
Принадлежит: Evonik Röhm GmbH

A process produces a (meth)acrylate ester mixture. The process includes reacting a glycerol formal isomer mixture with an alkyl (meth)acrylate in the presence of a catalyst. 1. A process for producing a (meth)acrylate ester mixture , the process comprising:reacting a glycerol formal isomer mixture with an alkyl (meth)acrylate in the presence of a catalyst.2. The process according to claim 1 , whereinthe glycerol formal isomer mixture is a mixture having an isomer ratio of 5-membered ring isomer to 6-membered ring isomer of 20:80 to 70:30.3. The process according to claim 2 , whereina homopolymer, comprising reacted units of at least one (meth)acrylate ester isomer from the (meth)acrylate ester mixture, has a glass transition temperature Tg of from 75° C. and 90° C.4. The process according to claim 1 , whereinthe catalyst is at least one member selected from the group consisting of a titanium alkoxide, a zirconium complex, a tin compound, and a mixture of lithium hydroxide and calcium oxide.5. The process according to claim 1 , whereinsaid reacting is performed at a temperature of from 30° C. and 180° C.67-. (canceled)8. A (meth)acrylate ester mixture obtained by a process according to claim 1 , wherein the (meth)acrylate ester has a vapor pressure of from 0.001 and 5 hPa.9. A process of producing a polymer claim 1 , the process comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'polymerizing the (meth)acrylate ester mixture according to .'}10. A process of producing a coating composition claim 1 , the process comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'polymerizing the (meth)acrylate ester mixture according to to obtain a polymer; and'}adding the polymer to a coating precursor composition to obtain the coating composition. The inversion relates to a process for producing (meth)acrylic esters of isomeric alcohols obtained by reaction of glycerol with formaldehyde (hydroxyl-substituted dioxanes and dioxolanes) in high-yield using titanium-, ...

Подробнее
Номер записи: 19
18-02-2016 дата публикации

BIOCIDE COMPOSITIONS, METHODS OF MANUFACTURE, AND METHODS OF USE

Номер: US20160044914A1
Автор: CUSACK TIMOTHY M., Thakrar Atul C., Yontz Dorie J.
Принадлежит:

A biocide composition comprises a biocide and an adjuvant comprising a ketal having the formula (1) 2. (canceled)3. (canceled)4. The biocide composition of claim 1 , wherein Ris >CH—CH claim 1 , >CH—CHOH claim 1 , >C(CH)CHOH claim 1 , >C(CH)CHOH claim 1 , >C(CHOH) claim 1 , >CH—CH(OH)—CHOH claim 1 , or >CH—(CHOH)—CHOH.5. (canceled)6. (canceled)7. (canceled)9. (canceled)10. (canceled)11. (canceled)12. The biocide composition of claim 1 , wherein the biocide comprises a herbicide claim 1 , an insecticide claim 1 , a fungicide claim 1 , an algicide claim 1 , a moluscicide claim 1 , a miticide claim 1 , a rodenticide claim 1 , an antimicrobial claim 1 , a plant growth regulator claim 1 , or a combination thereof.13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. The biocide composition of claim 1 , further comprising an oil claim 1 , a solvent claim 1 , a surfactant claim 1 , a penetrant claim 1 , water claim 1 , a wetting agent claim 1 , an anti-freeze claim 1 , a preservative claim 1 , stabilizing agent claim 1 , a buffer claim 1 , a rheology modifier claim 1 , an anti-foam agent claim 1 , a crystallization inhibitor claim 1 , a fertilizer claim 1 , or a combination comprising at least one of the foregoing.20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. (canceled)28. (canceled)29. (canceled)30. The biocide composition of claim 1 , wherein the composition is an emulsifiable concentrate claim 1 , a suspension concentrate claim 1 , a suspo-emulsion concentrate claim 1 , a tank mix composition claim 1 , or a ready-to-use liquid composition.31. An emulsifiable concentrate comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the biocide composition of ;'}a surfactant; andoptionally an oil,wherein the emulsifiable concentrate comprises, based on the total weight of the composition:0.01 to 99 weight %, specifically 0.05 to 75 weight %, more specifically 0.1 to 40 weight % of ...

Подробнее
Номер записи: 20
15-02-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180043009A1
Автор: Butler David, Eltepu Laxman, Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure 125-. (canceled)27. A lipid particle comprising a lipid of .28. The lipid particle of claim 27 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.29. The lipid particle of claim 27 , wherein the lipid particle consists essentially of{'claim-ref': {'@idref': 'CLM-00026', 'claim 26'}, 'a. a lipid of ;'}b. a neutral lipid selected from DSPC, DPPC, POPC, DOPE and SM;c. a sterol; andd. PEG-DMG or PEG-DMA,{'b': 26', '5', '25, 'in a molar ratio of about 20-60% lipid of claim :-% neutral lipid:25-55% stero1:0.5-15% PEG-DMG or PEG-DMA.'}30. The lipid particle of claim 27 , further comprising a therapeutic agent.31. The lipid particle of claim 30 , wherein the therapeutic agent is a nucleic acid.32. The lipid particle of claim 31 , wherein the nucleic acid is a plasmid.33. The lipid particle of claim 31 , wherein the nucleic acid is an immunostimulatory oligonucleotide.34. The lipid particle of claim 31 , wherein the nucleic acid is selected from the group consisting of an siRNA claim 31 , an antisense oligonucleotide claim 31 , a microRNA claim 31 , an antagomir claim 31 , an aptamer claim 31 , and a ribozyme.35. The lipid particle of claim 30 , wherein the therapeutic agent is siRNA.36. The lipid particle of claim 30 , wherein the therapeutic agent is mRNA.37. The lipid particle of claim 29 , wherein the sterol is cholesterol.38. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 27 , carrier claim 27 , or diluent.38. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 30 , carrier claim 30 , or diluent. This application is a Continuation application of U.S. application Ser. No. 14/629,991, ...

Подробнее
Номер записи: 21
18-02-2016 дата публикации

METHODS FOR PREPARING SGLT2 INHIBITORS

Номер: US20160046646A1
Автор: Brenek Steven J., Caron Stephane, Nelson Jade D., Webster Mark E., Weekly Rodney Matthew
Принадлежит:

This invention relates to methods for preparing a sodium-glucose transporter 2 (SGLT2) inhibitor, a cocrytalline SGLT2 and (S)-5-oxopyrrolidine-2-carboxylic acid (L-PGA) complex, and intermediates useful in the preparation of the said SGLT2 inhibitor. 4. The method of wherein the hydrogenolysis agent is hydrogen in the presence of palladium.5. The method of wherein the compound is treated using acidic conditions.6. The method of further comprising treating the compound of formula 28a/b with an acid.8. The method of wherein the acid is trifluoroacetic acid and the reducing agent is triethylsilane.10. The method of wherein the halogen metal exchange agent is n-butyllithium or hexyllithium.1115-. (canceled) The present invention relates to methods for preparing certain sodium glucose cotransporter 2 (SGLT2) inhibitors and intermediates useful in the preparation of SGLT2 inhibitors.Obesity is a significant health problem due to its serious medical complications that include co-morbidities such as hypertension, insulin resistance, diabetes, coronary artery disease and heart failure (collectively referred to as Metabolic Syndrome). Obesity and its related co-morbidities continue to cause rising health issues in the developed world and are beginning to affect the developing world as well. The negative health consequences of obesity make it the second leading cause of preventable death in the United States and impart a significant economic and psychosocial effect on society. See, McGinnis M, Foege W H., “Actual Causes of Death in the United States,” 270, 2207-12 (1993). There is a need to identify and develop new medications that treat and/or prevent obesity and its associated co-morbidities, in particular type II (type 2) diabetes.More recently, sodium-glucose co-transport (SGLT) inhibitors, particularly SGLT2 inhibitors, have been shown to block the reabsorption of glucose from the renal filtrate in the glomerulus thereby inducing glucose excretion in the urine. As excess ...

Подробнее
Номер записи: 22
18-02-2016 дата публикации

NOVEL CYCLIC ACETAL, CYCLIC KETAL DIAMINES EPOXY CURING AGENTS AND DEGRADABLE POLYMERS AND COMPOSITES BASED THEREON

Номер: US20160046760A1
Автор: Li Xin, Liang Bo, Qin Bing
Принадлежит:

The present invention provides, among others, compounds of the following formula which can be used as degradable curing agents, methods for preparing the compounds, degradable polymers and reinforced composites, methods for degrading and recycling the polymers and composites. 2. The curing agent of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare the same or different; A and B are the same or different.3. The curing agent of claim 1 , wherein n is 1.4. The curing agent of claim 3 , wherein each of R claim 3 , R claim 3 , R claim 3 , R claim 3 , Rand R claim 3 , independently claim 3 , is hydrogen or lower alkyl.5. The curing agent of claim 4 , wherein each of A and B independently is alkylene claim 4 , cycloalkylene claim 4 , arylene claim 4 , or heteroarylene.8. The method of claim 7 , wherein the catalyst comprises p-toluenesulfonic acid claim 7 , pyridinium p-toluenesulfonic acid claim 7 , sulfuric acid claim 7 , phosphoric acid claim 7 , nitric acid claim 7 , hydrogen chloride claim 7 , molecular sieves claim 7 , sulfonic acid resin claim 7 , or solid super acid.10. The method of claim 9 , wherein the catalyst comprises p-toluenesulfonic acid claim 9 , pyridinium p-toluenesulfonic acid claim 9 , sulfuric acid claim 9 , phosphoric acid claim 9 , nitric acid claim 9 , hydrogen chloride claim 9 , molecular sieves claim 9 , sulfonic acid resin claim 9 , or solid super acid.12. The method of claim 11 , wherein the catalyst comprises p-toluenesulfonic acid claim 11 , pyridinium p-toluenesulfonic acid claim 11 , sulfuric acid claim 11 , phosphoric acid claim 11 , nitric acid claim 11 , hydrogen chloride claim 11 , molecular sieves claim 11 , sulfonic acid resin claim 11 , or solid super acid.14. (canceled)15. The cross-linked polymer of claim 13 , wherein n is 1.16. The cross-linked polymer of claim 15 , wherein each of R claim 15 , R claim 15 , Rand Rindependently is hydrogen or lower alkyl.17. The cross-linked polymer of claim 16 , wherein ...

Подробнее
Номер записи: 23
23-02-2017 дата публикации

NOVEL LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20170050917A1
Автор: Budzik Brian W., Colletti Steven L., DAVIS Jennifer R., Hills Ivory D., SEIFRIED Darla Danile, Stanton Matthew G.
Принадлежит: Sirna Therapeutics, Inc.

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 3. (canceled)4. A lipid nanoparticle comprising of a cationic lipid of to .5. The lipid nanoparticle of claim 5 , wherein the lipid nanoparticle comprises oligonucleotides.6. The lipid nanoparticle of claim 5 , wherein the oligonucleotide are siRNA or mirNA.5. The lipid nanoparticle of wherein the oligonucleotide are siRNA. The present invention relates to novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides, to facilitate the cellular uptake and endosomal escape, and to knockdown target mRNA both in vitro and in vivo.Cationic lipids and the use of cationic lipids in lipid nanoparticles for the delivery of oligonucleotides, in particular siRNA and miRNA, have been previously disclosed. Lipid nanoparticles and use of lipid nanoparticles for the delivery of oligonucleotides, in particular siRNA and miRNA, has been previously disclosed. Oligonucleotides (including siRNA and miRNA) and the synthesis of oligonucleotides has been previously disclosed. (See US patent applications: US 2006/0083780, US 2006/0240554, US 2008/0020058, US 2009/0263407 and US 2009/0285881 and PCT patent applications: WO 2009/086558, WO2009/127060, WO2009/132131, WO2010/042877, WO2010/054384, WO2010/054401, WO2010/054405 and WO2010/054406). See also Semple S. C. et al., Rational design of cationic lipids for siRNA delivery, Nature ...

Подробнее
Номер записи: 24
01-03-2018 дата публикации

AMINATION AND HYDROXYLATION OF ARYLMETAL COMPOUNDS

Номер: US20180057444A1
Автор: GAO HONGYIN, Kürti László, ZHOU Zhe
Принадлежит: William Marsh Rice University

In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions. 1. A method of preparing an aminoaromatic group or a hydroxyaromatic group comprising:(A) admixing a metal aromatic compound with an oxaziridine compound to form a first reaction mixture under conditions sufficient to cause a reaction to obtain an anionic intermediate;(B) admixing a weak acid with the anionic intermediate and the first reaction mixture to obtain a second reaction mixture under conditions sufficient to obtain an aminoaromatic group or a hydroxyaromatic group.2. The method of claim 1 , wherein the metal of the metal aromatic compound is attached to one of the carbon atoms of the aromatic ring.3. The method of claim 1 , wherein the metal of the metal aromatic compound is a magnesium halide or lithium.48-. (canceled)9. The method of claim 1 , wherein the metal aromatic compound is substituted.10. (canceled)11. The method of claim 9 , wherein the metal aromatic compound is substituted with a substituent wherein the substituent is amino claim 9 , aminosulfonyl claim 9 , carboxy claim 9 , cyano claim 9 , halo claim 9 , hydroxy claim 9 , hydroxyamino claim 9 , hydroxysulfonyl claim 9 , mercapto claim 9 , nitro claim 9 , oxo claim 9 , or thio; or acyl claim 9 , alkoxy claim 9 , cycloalkoxy claim 9 , alkenyloxy claim 9 , aryloxy claim 9 , aralkoxy claim 9 , acyloxy claim 9 , cycloalkylalkoxy claim 9 , heterocycloalkylalkoxy claim 9 , heterocycloalkoxy claim 9 , alkylthio claim 9 , cycloalkylthio claim 9 , amido claim 9 , alkylamino claim 9 , dialkylamino claim 9 , alkylsulfonyl claim 9 , arylsulfonyl claim 9 , or a substituted version of these groups ...

Подробнее
Номер записи: 25
08-03-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180064807A1
Автор: Butler David, Eltepu Laxman, Jayaraman Muthusamy, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure: 2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. The cationic lipid of claim 1 , wherein X and Y are O.10. (canceled)11. The cationic lipid of claim 1 , wherein Ais —CH—.12. (canceled)13. (canceled)14. The cationic lipid of claim 1 , wherein Z′ is N(Q).15. (canceled)16. (canceled)17. The cationic lipid of claim 1 , wherein Z′ is alkyl.18. The cationic lipid of claim 1 , wherein Ris alkylamine.19. (canceled)20. (canceled)21. The cationic lipid of claim 1 , wherein Q is alkyl.22. (canceled)23. (canceled)24. (canceled)26. (canceled)27. (canceled)28. (canceled)29. (canceled)30. (canceled)31. (canceled)32. (canceled)33. (canceled)34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)41. (canceled)42. (canceled)43. A lipid particle comprising a compound of .44. (canceled)45. A lipid particle comprising a compound of .46. The lipid particle of claim 43 , wherein the particle further comprises a therapeutic agent.47. The lipid particle of claim 45 , wherein the particle further comprises a therapeutic agent.48. (canceled)49. The lipid particle of claim 46 , wherein the therapeutic agent is a nucleic acid.50. The lipid particle of claim 47 , wherein the therapeutic agent is a nucleic acid.51. (canceled)52. The lipid particle of claim 49 , wherein the nucleic acid is siRNA or mRNA.53. The lipid particle of claim 50 , wherein the nucleic acid is siRNA or mRNA.54. (canceled)55. A method of treating a disease or disorder in a subject in need thereof claim 46 , comprising administering to the subject the lipid particle of .56. A method of treating a disease or disorder in a subject in need thereof claim 47 , comprising administering to the subject the lipid particle of . This application ...

Подробнее
Номер записи: 26
05-06-2014 дата публикации

MEROCYANINE DERIVATIVES

Номер: US20140150380A1
Автор: Ehrsam Larissa, Eichin Kai, Hueglin Dietmar, Kienzle ILona Marion, Marat Xavier, Richard Herve, Schroeder Ute, Winkler Barbara
Принадлежит:

Disclosed are compounds of formula (1) and (2) and/or E/E-, E/Z- or Z/Z geometrical isomer forms thereof; wherein R1-R5, R1-R11 and A are defined as in description. The compounds are used as UV absorbers for protecting household products from photolytic and oxidative degradation, as plastic additives, preferably for food and pharmaceutical packaging applications, for preventing photo-degradation of food by incorporation of the compounds of formula (1′) and/or (2′) into transparent food containers, for protection of UV-A sensitive drugs from photo-degradation by incorporation of UV absorber in transparent blister foils or transparent pharmacy containers, as additives for photographic and printing applications, as additives for electronic applications and protecting the ingredients in agriculture applications. 4. Compounds of formula (1) according to claim 1 , wherein Ris C-Calkyl claim 1 , which is optionally substituted by one or more than one hydroxy.5. Compounds of formula (1) according to claim 1 , wherein{'sub': 6', '1', '12, 'Ris C-Calkyl which is substituted by one or more than one hydroxy;'}{'sub': 1', '2', '4', '22', '1', '2', '2', 'n, 'one of Rand Ris C-Calkyl; or Rand Rtogether with the nitrogen atom linking them form a —(CH)— ring which is optionally interrupted by —O— and/or —NH—; and'}{'sub': 4', '5, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'Rand Rand n are defined as in .'}6. Compounds of formula (2) according to claim 1 , wherein{'sub': 11', '2', 'm', '12, 'Ris a radical of formula (1a) —(CH)—R, wherein'}{'sub': 12', '1', '12', '1', '6', '1', '6, 'Ris C-Calkyl; or C-Calkoxy-C-Calkyl;'}m is a number from 1 to 5; and{'sub': 7', '8', '9', '10, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'R, R, R, Rand A are defined as in .'}7. Compounds according to claim 1 , wherein in formulas (1) and (2){'sub': 1', '2', '7', '8, 'Rand Rand Rand Rrespectively together with the linking nitrogen atom form a piperidyl radical or a morpholinyl radical.'}8. ...

Подробнее
Номер записи: 27
19-03-2015 дата публикации

Dioxlane Derivative, Liquid Crystal Composition, Liquid Crystal Element, and Liquid Crystal Display Device

Номер: US20150076402A1
Автор: Ishitani Tetsuji, Kato Momoko, Kawata Yuko, Niikura Yasuhiro
Принадлежит:

A dioxolane derivative represented by formula (G1) is provided. The explanation of the substituents is given in the specification. The use of the dioxolane derivative enables the production of a liquid crystal composition and a liquid crystal display device including the liquid crystal composition. 2. The compound according to claim 1 ,wherein m and n each represent 1.3. The compound according to claim 1 ,wherein:m and n each represent 1; and{'sup': 3', '4', '3', '4, 'one of Arand Arrepresents a substituted or unsubstituted aryl group having 6 to 12 carbon atoms and the other of Arand Arrepresents a substituted or unsubstituted cycloalkylene group having 3 to 12 carbon atoms.'}4. The compound according to claim 1 ,wherein:m and n each represent 1;{'sup': 3', '4', '3', '4, 'one of Arand Arrepresents a substituted or unsubstituted aryl group having 6 to 12 carbon atoms and the other of Arand Arrepresents a substituted or unsubstituted cycloalkylene group having 3 to 12 carbon atoms; and'}{'sup': '3', 'Rrepresents a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms.'}5. The compound according to claim 1 ,wherein:m and n each represent 1;{'sup': 3', '4', '3', '4, 'one of Arand Arrepresents a substituted or unsubstituted aryl group having 6 to 12 carbon atoms and the other of Arand Arrepresents a substituted or unsubstituted cycloalkylene group having 3 to 12 carbon atoms;'}{'sup': '3', 'Rrepresents a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms;'}{'sup': 1', '2, 'aand aeach represent a single bond; and'}{'sup': 1', '2, 'Arand Areach represent hydrogen.'}6. The compound according to claim 1 ,wherein the compound is optically active.8. A composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound according to ; and'}a liquid crystal.9. A liquid crystal display device comprising the composition according to .12. The compound according to claim 10 ,{'sup': 23', '24, 'wherein Arand Areach represent a ...

Подробнее
Номер записи: 28
19-03-2015 дата публикации

Compounds For The Treatment Of Proliferative Disorders

Номер: US20150080386A1
Автор: Chen Shoujun, Jiang Jun, Kowalczyk Przewloka Teresa, Koya Keizo
Принадлежит:

Disclosed are compounds and pharmaceutical compositions that are useful for treating a subject with a proliferative disorder, such as cancer. The disclosed compounds and pharmaceutical compositions are also useful for treating disorders responsive to Hsp70 induction and/or natural killer induction. 179-. (canceled)81. The method of claim 80 , wherein the Hsp70 responsive disorder is Alzheimers' disease claim 80 , Huntington's disease claim 80 , Parkinson's disease claim 80 , spongiform encephalopathies claim 80 , spinal/bulbar muscular atrophy claim 80 , familial amyotrophic lateral sclerosis claim 80 , atherosclerosis claim 80 , cerebral trauma or spinal trauma.82. The method of claim 80 , wherein the Hsp70 responsive disorder is nerve damage caused by chemotherapy.8384-. (canceled)87. The method of claim 86 , wherein:{'sub': 1', '2, 'Xand Xare both CRR or both O; and'}R, for each occurrence, is independently, —H or a lower alkyl.88. The method of claim 80 , wherein Q is an optionally substituted 5-14 membered heteroaryl group selected from furanyl claim 80 , benzo[1 claim 80 ,3]dioxolyl claim 80 , benzo[1 claim 80 ,4]dioxinyl claim 80 , thienyl claim 80 , pyrrolyl claim 80 , oxazolyl claim 80 , imidazolyl claim 80 , thiazolyl claim 80 , a isoxazolyl claim 80 , quinolinyl claim 80 , pyrazolyl claim 80 , isothiazolyl claim 80 , pyridazinyl claim 80 , pyrimidinyl claim 80 , pyrazinyl claim 80 , a triazinyl claim 80 , triazolyl claim 80 , thiadiazolyl claim 80 , isoquinolinyl claim 80 , indazolyl claim 80 , benzoxazolyl claim 80 , benzofuryl claim 80 , indolizinyl claim 80 , imidazopyridyl claim 80 , tetrazolyl claim 80 , benzimidazolyl claim 80 , benzothiazolyl claim 80 , benzothiadiazolyl claim 80 , benzoxadiazolyl claim 80 , indolyl claim 80 , tetrahydroindolyl claim 80 , azaindolyl claim 80 , imidazopyridyl claim 80 , quinazolinyl claim 80 , purinyl claim 80 , pyrrolo[2 claim 80 ,3]pyrimidinyl claim 80 , pyrazolo[3 claim 80 ,4]pyrimidinyl claim 80 , imidazo[1 ...

Подробнее
Номер записи: 29
19-03-2015 дата публикации

Methods for the manufacture of acetals and ketals, and the acetals and ketals produced thereby

Номер: US20150080585A1
Автор: Andrew J. Louwagie, Brian D. Mullen, Feng Jing, Marc D. Scholten, Steven A. Donen, Vivek Badarinarayana
Принадлежит: Segetis Inc

A method for producing a product that comprises glycerol ketal of ethyl levulinate or propylene glycol ketal of ethyl levulinate comprises reacting either glycerol or propylene glycol with ethyl levulinate in the presence of a homogenous or heterogeneous catalyst system in a reactor system. The ethyl levulinate and either glycerol or propylene glycol are heated to remove water, polyol, and excess ethyl levulinate. The excess ethyl levulinate and polyol is recycled back to the reactor. The product is distilled in a specific fashion and optionally treated by means of a stabilizing agent or acid species removal bed, to obtain a composition comprising glycerol ketal of ethyl levulinate or propylene glycol ketal of ethyl levulinate wherein the composition comprises less than or equal to about 2 wt % contaminants.

Подробнее
Номер записи: 30
05-06-2014 дата публикации

CHIRAL SYNTHESIS OF N--1-[2,3-DIHYDROXY-PROPYL]CYCLOPROPANESULFONAMIDES

Номер: US20140155637A1
Автор: FEY Peter, Mayer Agathe Christine
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-5 methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide. 17. (canceled) The present invention relates to a novel enantioselective method of preparing (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide:N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[(2S)-2,3-dihydroxy-propyl]cyclopropanesulfonamide (hereinafter referred to as “(S)-14”, “BAY 86-9766” or “RDEA 119”) is a highly potent and selective MEK1/2 inhibitor currently under development in clinical trials for treatment of late stage cancer patients refractory or intolerant to other anticancer therapies [ref. 1].The initial synthesis of (S)-14, shown in Scheme A, infra, published in US 2008/0058340 [ref. 2] comprises an osmium catalyzed dihydroxylation of the allyl sulfonamide substituted core followed by chromatographic separation of the enantiomers using a chiral stationary phase: the initial synthesis of (S)-14 provides the target compound as a racemic mixture that needs to be separated by chiral chromatography [ref. 2].In Scheme A, supra, a racemic mixture of the (S)- and (R)-enantiomers of N-{3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl}-1-[2,3-dihydroxy-propyl]cyclopropanesulfonamide is produced which, as seen, must ...

Подробнее
Номер записи: 31
07-04-2016 дата публикации

AMINO LIPIDS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS

Номер: US20160095924A1
Автор: CHEN Jianxin, Ciufolini Marco A., Cullis Pieter R., Hope Michael J., Low Shoud Mui Barbara, Madden Thomas D., Semple Sean C.
Принадлежит:

The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art. 2. (canceled)4. A lipid particle comprising an amino lipid of .5. The lipid particle of claim 4 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing particle aggregation.6. The lipid particle of claim 5 , wherein the lipid particle comprises:(i) DLin-K-C2-DMA;(ii) a neutral lipid selected from DSPC, POPC, DOPE, and SM;(iii) cholesterol; and(iv) a PEG-lipid,in a molar ratio of about 20-60% DLin-K-C2-DMA:5-25% neutral lipid:25-55% Chol:0.5-15% PEG-lipid.7. The lipid particle of claim 4 , further comprising a therapeutic agent.8. The lipid particle of claim 7 , wherein the therapeutic agent is a nucleic acid.9. The lipid particle of claim 8 , wherein the nucleic acid is a plasmid.10. The lipid particle of claim 8 , wherein the nucleic acid is an immunostimulatory oligonucleotide.11. The lipid particle of claim 8 , wherein the nucleic acid is selected from the group consisting of: a siRNA claim 8 , a microRNA claim 8 , an antisense oligonucleotide claim 8 , and a ribozyme.12. The lipid particle of claim 11 , wherein the nucleic acid is a siRNA.13. A pharmaceutical composition comprising the lipid particle of and a pharmaceutically acceptable excipient claim 7 , carrier claim 7 , or diluent.14. A method of modulating the expression of a polypeptide by a cell claim 7 , comprising providing to ...

Подробнее
Номер записи: 32
05-04-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180092971A1
Автор: Ansell Steven, CHEN Jianxin, Eltepu Laxman, Jayaraman Muthusamy, Manoharan Muthiah, Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention 125-. (canceled)27. The lipid of claim 26 , wherein Ris ω-aminoalkyl claim 26 , ω-(substituted)aminoalkyl claim 26 , ω-phosphoalkyl claim 26 , or ω-thiophosphoalkyl.28. The lipid of claim 27 , wherein Ris ω-(substituted)aminoalkyl.29. The lipid of claim 26 , wherein Ris 2-(dimethylamino)ethyl claim 26 , 3-(diisopropylamino)propyl claim 26 , or 3-(N-ethyl-n-isopropylamino)-1-methylpropyl.30. The lipid of claim 26 , wherein Ris H claim 26 , optionally substituted C-Calkyl claim 26 , optionally substituted C-Calkenyl claim 26 , or optionally substituted C-Calkynyl.31. The lipid of claim 26 , wherein Ris alkylaminoalkyl claim 26 , dialkylaminoalkyl claim 26 , or alkylheterocycle.32. The lipid of claim 26 , wherein Rand Rare each optionally substituted C-Calkyl or optionally substituted C-Calkenyl.33. The lipid of claim 26 , wherein Rand Rare each linoleyl.34. A lipid particle comprising a lipid of .35. The lipid particle of claim 34 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.36. The lipid particle of claim 35 , wherein the lipid capable of reducing aggregation is a PEG-lipid.37. The lipid particle of claim 34 , further comprising a therapeutic agent.38. The lipid particle of claim 37 , wherein the therapeutic agent is a nucleic acid.39. The lipid particle of claim 38 , wherein the nucleic acid is selected from the group consisting of an siRNA and an antisense oligonucleotide.40. The lipid particle of claim 37 , wherein the nucleic acid is siRNA.41. The lipid particle of claim 37 , wherein the nucleic acid is mRNA.42. A pharmaceutical composition comprising a lipid of and a pharmaceutically acceptable excipient claim 26 , carrier claim 26 , or diluent.43. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically ...

Подробнее
Номер записи: 33
12-05-2022 дата публикации

WATER-SOLUBLE YNAMIDE COUPLING REAGENT AND PREPARATION METHOD AND USE THEREOF

Номер: US20220144793A1
Автор: Liu Tao, Zhao Junfeng
Принадлежит: Xi'an Easy Peptide Biotechnology Co., Ltd.

The present disclosure discloses a water-soluble ynamide coupling reagent and a method for using the water-soluble ynamide coupling reagent in the synthesis of amide, polypeptide, ester and thioester compound. The ynamide coupling reagent has the structure represented by the following formula (I): 3. The method of claim 2 , wherein in step 1) claim 2 , the solvent I is an organic solvent; the solvent I is preferably at least one selected from the group consisting of dimethyl sulfoxide claim 2 , N claim 2 ,N-dimethylformamide claim 2 , N claim 2 ,N-dimethylacetamide and N-methylpyrrolidone; a molar ratio of N-(2 claim 2 ,2-dimethyl-1 claim 2 ,3-dioxolane-4-ylmethyl)amide having the structure represented by formula (II) to ethylene dichloride is in a range of 1:(0.8-5) claim 2 , preferably 1:(1-3) claim 2 , and more preferably 1:(1.1-2); and/or{'sub': 2', '2', '3', '2', '3', '2', '3', '2, 'in step 2), the alkali is at least one selected from the group consisting of NaH, CaH, t-BuONa, KOH, NaOH, EtONa, EtOLi, CsCO, KCO, NaCO, Ca(OH), LiOH and DBU; the reaction is performed at a temperature of 15-100° C., preferably 20-90° C., and more preferably 25-80° C.; the reaction is performed for 0.2-48 h, preferably 0.5-36 h, and more preferably 1-24 h; the separating is performed by filtration, centrifugation or column chromatography; and a molar ratio of the alkali to N-(2,2-dimethyl-1,3-dioxolane-4-ylmethyl) amide having the structure represented by formula (II) is in a range of (1-10):1, preferably (2-8):1, and more preferably (3-6):1.'}4. A method for using a water-soluble ynamide coupling reagent claim 1 , wherein the water-soluble ynamide coupling reagent of is used in the synthesis of amide claim 1 , polypeptide claim 1 , ester compound or thioester compound.6. The method of claim 5 , wherein in step 1a) claim 5 , the carboxylic acid compound is an organic acid formed by the association of a hydrocarbon group and a carboxyl group; the carboxylic acid compound is ...

Подробнее
Номер записи: 34
16-04-2015 дата публикации

METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE

Номер: US20150105555A1
Автор: Chen Chaoyong, GAGE James, HONG Hao, Liu Shuangyong, LU Jiangping, Zhou Yan
Принадлежит:

Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, introduces a chiral center in an asymmetric synthesis manner, in which a tetrahydrofuran solution containing a samarium catalyst is adopted as a catalyst, and obtains a target compound having a high antimer isomerism value by means of selective catalysis. The yield is improved, raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride. 3. A method for synthesizing sapropterin dihydrochloride according to claim 1 , wherein in Step 2 claim 1 , the Lewis acid is aluminium chloride claim 1 , ferric chloride claim 1 , zinc chloride claim 1 , a boron trifluoride diethyletherate solution claim 1 , zinc bromide claim 1 , or lithium chloride claim 1 , preferably aluminium chloride claim 1 , the boron trifluoride diethyl etherate solution claim 1 , zinc bromide or lithium chloride claim 1 , and optimally the boron trifluoride diethyletherate solution or zinc bromide; the inorganic base is sodium bicarbonate claim 1 , sodium carbonate claim 1 , sodium hydroxide claim 1 , potassium hydroxide claim 1 , potassium carbonate or potassium bicarbonate claim 1 , preferably sodium bicarbonate claim 1 , sodium carbonate claim 1 , potassium carbonate or potassium bicarbonate claim 1 , optimally sodium carbonate; the ratio of the use amount of compound 2 to that of acetone is 1:1 to 3.5 claim 1 , preferably 1:1 to 3; the ratio of the use amount of compound 2 to that of the Lewis acid is 1:0.1 to 0.8 claim 1 , preferably 1:0.1 to 0.6; the ratio of the use amount of compound 2 to that of the inorganic base is 1:0.5 to 2.5 claim 1 , preferably 1:0.5 to 2.4. A method for synthesizing sapropterin dihydrochloride according to claim 1 , wherein in Step 3 claim 1 , the polar solvent is tetrahydrofuran claim 1 , ...

Подробнее
Номер записи: 35
16-04-2015 дата публикации

PRODUCTION METHOD FOR COMPOUND COMPRISING AMINO GROUP AND/OR HYDROXYL GROUP

Номер: US20150105559A1
Автор: Morimoto Hiroyuki, OHSHIMA Takashi, Shimizu Yuhei
Принадлежит: Kyushu University, National University Corporation

Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. HN-A—NH(I) - - -. 2. (canceled)3. The method as claimed in claim 1 , wherein the ammonium salt is an ammonium halide.4. The method as claimed in claim 3 , wherein the substrate compound is an amide claim 3 , the atomic group containing CX is an N-acyl group claim 3 , and the reaction is carried out by eliminating the acyl group to produce a compound having an amino group from said substrate compound.5. The method as claimed in claim 4 , wherein the compound expressed by the formula (I) for the reaction is hydrazine.6. The method as claimed in claim 4 , wherein the compound expressed by the formula (I) for the reaction is the alkylamine.7. The method as claimed in claim 6 , wherein the compound expressed by the formula (I) for the reaction is ethylenediamine.8. The method as claimed in claim 1 , wherein the substrate compound is a cyclic carbamate claim 1 , a chain carbamate claim 1 , a cyclic carbonate claim 1 , a chain carbonate claim 1 , a cyclic urea or a chain urea claim 1 , the atomic group containing CX is carbonyl group claim 1 , and the reaction is carried out by allowing the substrate compound with the alkylamine as the compound expressed by the formula (I) to eliminate the carbonyl group to produce a compound having an amino group and/or a hydroxyl group.9. The method as claimed in claim 1 , wherein the substrate compound ...

Подробнее
Номер записи: 36
21-04-2016 дата публикации

LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS

Номер: US20160106842A1
Автор: Baryza Jeremy Lee, BECKWITH Rohan Eric John, Bowman Keith, BYERS Crystal, Fazal Tanzina, Gamber Gabriel Grant, Lee Cameron Chuck-Munn, TICHKULE Ritesh Bhanudasji, Vargeese Chandra, Wang Shuangxi, West Laura, ZABAWA Thomas, Zhao Junping
Принадлежит:

This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R-R, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues. 221-. (canceled)22. A lipid composition comprising a compound according to or a pharmaceutically acceptable salt thereof.23. The lipid composition according further comprising a biologically active agent.24. The lipid composition according wherein the biologically active agent is a siRNA.2530-. (canceled)31. A pharmaceutical composition comprising the lipid composition according to and a pharmaceutically acceptable carrier or excipient.32. A method for the treatment of a disease or condition comprising administering a therapeutically effective amount of the lipid composition according to to a patient in need of treatment thereof.33. A method for the treatment of a disease or condition comprising administering a therapeutically effective amount of the pharmaceutical composition according to .34. The lipid composition according to wherein the biologically active agent is an mRNA.3540-. (canceled)41. A pharmaceutical composition comprising the lipid composition according to and a pharmaceutically acceptable carrier or excipient.42. A method for the treatment of a disease or condition comprising administering a therapeutically effective amount of the lipid composition according to to a patient in need of treatment thereof.43. A method for the treatment of a disease or condition comprising administering a therapeutically effective amount of the pharmaceutical composition according to .44. A compound according to which is:1-(3,5-bis((Z)-octadec-9-en-1-yloxy)phenyl)-N,N-dimethylmethanamine;1-(3,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)phenyl)-N,N-dimethylmethanamine;2,2′-((3,5-bis((9Z,12Z)-octadeca-9,12-dien-1-yloxy)benzyl)azanediyl)diethanol;1-(3,5-bis((9Z,12Z)- ...

Подробнее
Номер записи: 37
30-04-2015 дата публикации

FUEL COMPOSITIONS COMPRISING HYDROPHOBIC DERIVATIVES OF GLYCERINE

Номер: US20150113860A1
Автор: ASSANELLI Giulio, De Angelis Alberto, POLLESEL PAOLO
Принадлежит: ENI S.P.A.

The object of the present invention relates to a composition that can be used as fuel comprising: at least one hydrocarbon mixture at least one hydrophobic ketal or acetal of glycerine. Said composition can be advantageously used as fuel for diesel or gasoline engines. 2. The composition according to claim 1 , wherein the cyclic ketal and/or acetal having formula (I) or (II) is present in said composition in an amount ranging from 0.5% by volume to 15% by volume.3. The composition according to claim 2 , wherein the cyclic ketal and/or acetal having formula (I) or (II) is present in an amount ranging from 1% by volume to 10% by volume claim 2 , with respect to the total volume of the composition.4. The composition according to claim 1 , wherein the hydrocarbon mixture is selected from gasoil claim 1 , gasoline claim 1 , biodiesel claim 1 , green diesel and mixtures thereof.5. The composition according to claim 1 , wherein claim 1 , in the compounds having formula (I) or (II) claim 1 , Ris selected from H claim 1 , CHand CH claim 1 , and Ris selected from CH claim 1 , CH claim 1 , CHand CH.6. The composition according to claim 1 , wherein claim 1 , in the compounds having formula (I) or (II) claim 1 , Rcontains from 2 to 4 carbon atoms.7. The composition according to claim 1 , wherein claim 1 , in the compounds having formula (I) or (II) claim 1 , Ris ethyl or n-butyl.9. The process according to claim 8 , wherein the transformation in step (1) corresponds to the etherification of glycerine claim 8 , effected by reaction with an alcohol having formula ROH to give the corresponding 3-(RO)-1 claim 8 ,2-propanediol claim 8 , 2-(RO)-1 claim 8 ,3-propanediol or a mixture thereof claim 8 , wherein Ris a linear or branched alkyl containing from 1 to 8 carbon atoms.10. The process according to claim 8 , wherein the transformation in step (1) corresponds to the reduction of glycerine to the corresponding diol claim 8 , effected with hydrogen in the presence of a catalyst to ...

Подробнее
Номер записи: 38
20-04-2017 дата публикации

HYDROPHILIC POLYMER DERIVATIVE HAVING CYCLIC BENZYLIDENE ACETAL LINKER

Номер: US20170107325A1
Автор: TSUBUSAKI Takuma, Yamamoto Yuji
Принадлежит: NOF CORPORATION

A hydrophilic polymer derivative having a cyclic benzylidene acetal linker represented by the following formula (1): 2. The hydrophilic polymer derivative as claimed in claim 1 , wherein s is 1 and t is 0 claim 1 , Rand Rare each a hydrogen atom claim 1 , and a sum (Σσ) of substituent constants (σ) in R claim 1 , Rand P—Zsatisfies −0.30≦Σσ≦1.05.3. The hydrophilic polymer derivative as claimed in claim 1 , wherein s is 1 and t is 0 claim 1 , at least one of Rand Ris the substituent claim 1 , and a sum (Σσ) of substituent constants (σ) in R claim 1 , Rand P—Zsatisfies −1.71≦Σσ≦0.88.4. The hydrophilic polymer derivative as claimed in claim 1 , wherein s is 1 and t is 1 claim 1 , or s is 2 and t is 0 claim 1 , Rand Rare each a hydrogen atom claim 1 , and a sum (Σσ) of substituent constants (σ) in R claim 1 , Rand P—Zsatisfies −0.19≦Σσ≦0.57.5. The hydrophilic polymer derivative as claimed in claim 1 , wherein s is 1 and t is 1 claim 1 , or s is 2 and t is 0 claim 1 , at least one of Rand Ris the substituent claim 1 , and a sum (Σσ) of substituent constants (σ) in R claim 1 , Rand P—Zsatisfies −0.98≦Σσ≦0.48.6. The hydrophilic polymer derivative as claimed in claim 1 , wherein Xis selected from the group consisting of an active ester group claim 1 , an active carbonate group claim 1 , an aldehyde group claim 1 , an isocyanate group claim 1 , an isothiocyanate group claim 1 , an epoxy group claim 1 , a maleimide group claim 1 , a vinyl sulfone group claim 1 , an acryl group claim 1 , a sulfonyloxy group claim 1 , a carboxy group claim 1 , a thiol group claim 1 , a dithiopyridyl group claim 1 , an α-haloacetyl group claim 1 , an alkynyl group claim 1 , an allyl group claim 1 , a vinyl group claim 1 , an amino group claim 1 , an oxyamino group claim 1 , a hydrazide group and an azide group.8. The hydrophilic polymer derivative as claimed in claim 1 , wherein Zand Zare each independently an ether bond claim 1 , an ester bond claim 1 , a carbonate bond claim 1 , a urethane bond ...

Подробнее
Номер записи: 39
11-04-2019 дата публикации

NOVEL CYCLIC CATIONIC LIPIDS AND METHODS OF USE

Номер: US20190106379A1
Автор: Heyes James, Martin Alan D., Wood Mark
Принадлежит: Arbutus Biopharma Corporation

The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art. 216-. (canceled)1833-. (canceled)3549-. (canceled)50. A lipid particle comprising a cationic lipid of .5157-. (canceled)58. The lipid particle of claim 50 , wherein the particle further comprises a therapeutic agent.5966-. (canceled)67. A pharmaceutical composition comprising a lipid particle of claim 50 , and a pharmaceutically acceptable carrier.68. A method for introducing a therapeutic agent into a cell claim 50 , the method comprising:{'claim-ref': {'@idref': 'CLM-00058', 'claim 58'}, 'contacting the cell with a lipid particle of .'}69. (canceled)70. A method for the in vivo delivery of a therapeutic agent claim 50 , the method comprising:{'claim-ref': {'@idref': 'CLM-00058', 'claim 58'}, 'administering to a mammal a lipid particle of .'}7172-. (canceled)73. A method for treating a disease or disorder in a mammal in need thereof claim 50 , the method comprising:{'claim-ref': {'@idref': 'CLM-00058', 'claim 58'}, 'administering to the mammal a therapeutically effective amount of a lipid particle of .'}7475-. (canceled)76. A lipid particle comprising a cationic lipid of .77. The lipid particle of claim 76 , wherein the particle further comprises a therapeutic agent.78. A pharmaceutical composition comprising a lipid particle of claim 76 , and a pharmaceutically acceptable carrier.79. A method for introducing a ...

Подробнее
Номер записи: 40
11-04-2019 дата публикации

MANNITOL BASED GELATORS FOR OIL SPILLAGE APPLICATIONS

Номер: US20190106399A1
Автор: Nettem Venkateswarlu Choudary, PRAMANIK BHASKAR, RAJU CHINTHALAPATI SIVA KESAVA, Rao Peddy Venkat Chalapathi, Ravishankar Raman, Sriganesh Gandham
Принадлежит:

In accordance with the present subject matter there is provided sugar-based compounds of formula I, methods of making such compounds, gels comprising such compounds, methods of making gels, methods of using such compounds for the containing spill of a hydrocarbon, and methods for reclaiming solvent from gels comprising such compounds. 2. The compound as claimed in claim 1 , wherein Rand Rare C-Calkyl.3. The compound as claimed in claim 1 , wherein Rand Rare C-Calkyl.4. The compound as claimed in claim 1 , wherein Rand Rare Calkyl.5. The compound as claimed in claim 1 , wherein Rand Rare Calkyl.6. The compound as claimed in claim 1 , wherein Rand Rare Calkyl.7. The compound as claimed in claim 1 , wherein Ris Calkyl and Ris Calkyl.8. A method of preparing the compound as claimed in .9. A gel comprising a compound as claimed in and a solvent.10. The gel as claimed in claim 9 , wherein the solvent is selected from water claim 9 , an organic solvent claim 9 , or mixtures thereof.11. A method for producing a gel comprising contacting the compound as claimed in with a solvent.12. The method as claimed in wherein the solvent is selected from water claim 11 , an organic solvent claim 11 , or mixtures thereof.13. The method of claim 11 , wherein the solvent is a hydrocarbon.14. The method of claim 11 , wherein the solvent comprises a mixture of a hydrocarbon and water.15. A method of containing the spill of a hydrocarbon claim 1 , the method comprising contacting the hydrocarbon with the compound as claimed in to obtain a gel.16. A method of reclaiming solvent and a compound as claimed in from the gel as claimed in . The subject matter described herein in general relates to sugar-based compounds that are able to form gels. The subject matter further relates to methods of making the sugar-based compounds, and gels including such compounds. The sugar-based compounds can be used to control hydrocarbon spill by gel formation. The subject matter further relates to methods for ...

Подробнее
Номер записи: 41
30-04-2015 дата публикации

Method for synthesizing sapropterin dihydrochloride

Номер: US20150119573A1
Автор: Chaoyong Chen, Hao Hong, JAMES Gage, Jiangping Lu, Shuangyong Liu, Yan Zhou
Принадлежит: Asymchem Laboratories Fuxin Co Ltd, Asymchem Laboratories Jilin Co Ltd, Asymchem Laboratories Tianjin Co Ltd, Asymchem Life Science Tianjin Co Ltd, Tianjin Asymchem Pharmaceutical Co Ltd

Disclosed is a method for synthesizing sapropterin dihydrochloride. The present disclosure reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediate having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.

Подробнее
Номер записи: 42
30-04-2015 дата публикации

METHOD FOR PRODUCING A SUBSTITUTED BENZOIC ACID COMPOUND

Номер: US20150119586A1
Автор: Adachi Norio, Fukui Fumihiro, Isogai Akihiko, Jonishi Hisayoshi, JUKUROGI Tatsuya, Konishi Hideaki, Okamoto Tomohiro
Принадлежит: ISHIHARA SANGYO KAISHA, LTD.

To provide an industrial method for producing a substituted benzoic acid compound useful as an intermediate of pharmaceutical and agricultural chemicals with high purity and high yield. 2. The production method according to claim 1 , wherein the reaction of the compound represented by the above formula (II) claim 1 , carbon monoxide and the compound represented by the formula R—OH is carried out in the presence of a base and a transition metal catalyst claim 1 , and further as the case requires claim 1 , in the presence of a solvent.3. The production method according to claim 1 , wherein the hydrolysis is carried out in the presence of a base claim 1 , and then the reaction mixture is acidified with an acid.410-. (canceled)12. The compound according to claim 11 , wherein Q is dioxolan-2-yl claim 11 , T is methylsulfonyl claim 11 , X is a chlorine atom claim 11 , Y is a bromine atom claim 11 , and n is 2.14. The compound according to claim 13 , wherein T is methylsulfonyl claim 13 , X is a chlorine atom claim 13 , and Y is a bromine atom.1517-. (canceled)18. The production method according to claim 2 , wherein the hydrolysis is carried out in the presence of a base claim 2 , and then the reaction mixture is acidified with an acid. The present invention relates to a method for producing a substituted benzoic acid compound useful as an intermediate for production of pharmaceutical and agricultural chemicals.Patent Document 1 discloses a method for producing a substituted benzoic acid from 2,4-substituted hydroxybenzoic acid ester as a starting material. This production method has problems such that methyl dichlorobenzoate as a starting material is hardly prepared and is industrially hardly available, anhydrous sodium thiomethoxide used for alkylthiolation of the starting material is industrially hardly available, and the selectivity of the alkylthiolation is low and the yield is low.Patent Document 1: JP-A-2006-16389The object of the present invention is to provide a ...

Подробнее
Номер записи: 43
10-05-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180125985A1
Автор: Butler David, Eltepu Laxman, Jayaraman Muthusamy, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: 5. A lipid particle comprising a lipid of .6. (canceled)7. The lipid particle of claim 5 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.8. The lipid particle of claim 5 , wherein the lipid particle consists essentially of{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. the lipid of ;'}b. a neutral lipid selected from DSPC, DPPC, POPC, DOPE and SM;c. a sterol; andd. PEG-DMG or PEG-DMA,{'b': '1', 'in a molar ratio of about 20-60% lipid of claim :5-25% neutral lipid:25-55% sterol:0.5-15% PEG-DMG or PEG-DMA.'}9. The lipid particle of claim 5 , further comprising a therapeutic agent.10. The lipid particle of claim 9 , wherein the therapeutic agent is a nucleic acid.11. (canceled)12. (canceled)13. The lipid particle of claim 10 , wherein the nucleic acid is selected from the group consisting of an siRNA claim 10 , an antisense oligonucleotide claim 10 , a microRNA claim 10 , an antagomir claim 10 , an aptamer claim 10 , and a ribozyme.14. The lipid particle of claim 13 , wherein the nucleic acid is an siRNA.15. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 9 , carrier claim 9 , or diluent.16. A method of modulating the expression of a target gene in a cell claim 9 , comprising providing to a cell the lipid particle of .17. (canceled)18. (canceled)19. A method of treating a disease or disorder characterized by overexpression of a polypeptide in a subject claim 9 , comprising providing to the subject the lipid particle of .20. A method of treating a disease or disorder characterized by underexpression of a polypeptide in a subject claim 9 , comprising providing to the subject the lipid particle of .2128-. (canceled)29. The lipid ...

Подробнее
Номер записи: 44
21-05-2015 дата публикации

COMPOUNDERS FOR ENHANCING GENERATION OF CHEMICAL SPECIES

Номер: US20150140493A1
Автор: Enomoto Satoshi, SUGA Yusuke
Принадлежит:

A reagent that enhances acid generation of a photoacid generator and composition containing such reagent is disclosed. Also described is a method for manufacturing a device, the method including applying a liquid containing a composition to a member such that a coating film including the composition is formed on the member; and exposing the coating film to at least one of a first electromagnetic ray and a first particle ray such that a first portion of the coating film is exposed to the at least one of the first electromagnetic ray and the first particle ray while a second portion of the coating film is not exposed to the at least one of the first electromagnetic ray and the first particle ray. 1. A reagent characterized in thatthe reagent is able to generate a compounder in at least one of a composition including the reagent, a liquid containing the composition, and a film of the composition; andthe compounder is able to enhance a first chemical species from at least one of the compounder and a substance by an interaction of the compounder with the substance.2. The reagent of claim 1 , wherein the interaction is promoted by an exposure of the composition claim 1 , the liquid and the film to at least one of a first electromagnetic ray and a first particle ray.3. The reagent of claim 1 , wherein the compounder is formed through a reaction of the reagent with a second chemical species generated from the compounder.4. The reagent of claim 1 , wherein:the first chemical species is also generated from the substance without any interaction with the compounder; andthe compounder is formed by a reaction of the reagent with the first chemical species.5. The reagent of claim 1 , wherein the compounder is capable of donating an electron to the substance.6. The reagent of claim 1 , wherein the reagent is able to generate the compounder through processes triggered by supplying energy to the film.7. The reagent of claim 1 , wherein a conjugation length of the compounder is longer ...

Подробнее
Номер записи: 45
21-05-2015 дата публикации

METHOD FOR THE PREPARATION OF THIADIAZOLES

Номер: US20150141655A1
Автор: Bercot Eric A., BIO Matthew, CHAN Johann, Colyer John, FANG Yuanqing, Mennen Steven, Milburn Robert R., Riahi Babak, TEDROW Jason
Принадлежит:

The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles. 2. The process of claim 3 , wherein said salt of substituted 1 claim 3 ,3-dioxolan-4-yl(hydroxy)methanesulfonate is [(4R)-2 claim 3 ,2-dimethyl-1 claim 3 ,3-dioxolan-4-yl](hydroxy)methanesulfonate salt.3. A process for preparing a salt of substituted 1 claim 3 ,3-dioxolan-4-yl(hydroxy)methanesulfonates by the treatment of an aldehyde with a metasulfite salt.4. The process of wherein the [(4R)-2 claim 2 ,2-dimethyl-1 claim 2 ,3-dioxolan-4-yl](hydroxy)methanesulfonate salt is sodium [(4R)-2 claim 2 ,2-dimethyl-1 claim 2 ,3-dioxolan-4-yl](hydroxy)methanesulfonate.5. The process of wherein the aldehyde is the result of oxidative cleavage of 1 claim 2 ,2 claim 2 ,5 claim 2 ,6-di-O-isopropylidene-D-mannitol.6. The process of wherein the temperature is between −15° C. and about 30° C.7. (canceled)8. The process of wherein the oxidative cleavage results from treatment with NaIO claim 5 , or Pb(OAc).9. The process of wherein NaIOis used for the oxidative cleavage.10. The process of comprising treatment with NaIOin an amount of at least about 1 equivalents per mole of the diol employed.11. The process of comprising treatment with NaIOin an amount of about 1.4-1.5 equivalents of NaIO.12. The process of comprising treatment with NaHCO claim 5 , at about 0.3 eq. claim 5 , in the presence of HO.13. The process of wherein the pH of the oxidative cleavage is maintained higher than 0.8.14. (canceled)15. The process of wherein the reaction is maintained at above 35° C.16. The process of wherein the reaction is maintained at a temperature of about 50° C.17. The process of wherein the aldehyde is treated with NaSOin an amount of about 0.5-2 equivalents per mole of the aldehyde employed.18. The process of comprising the use of about 0.5 equivalents of NaSO.2021-. (canceled)23. ...

Подробнее
Номер записи: 46
24-05-2018 дата публикации

METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG

Номер: US20180141889A1
Автор: Chambournier Gilles, Endres Gregory William, Fedij Victor, Hering Kirk William, II Thomas James, Krell, Mahmoud Hussein Mahmoud
Принадлежит: CAYMAN CHEMICAL COMPANY INCORPORATED

The present invention provides processes for preparing a prostacyclin analogue of Formula I 2. The method of claim 1 , wherein the transition metal catalyst of step xv) comprises a compound or complex either of which comprises Cu having a +1 oxidation state.3. The method of claim 2 , wherein the transition metal catalyst of step xv) comprises CuX claim 2 , wherein X is selected from halogen claim 2 , acetate claim 2 , benzoate claim 2 , cyanide claim 2 , hydroxide claim 2 , nitrate claim 2 , or any combination thereof.4. The method of claim 3 , wherein the transition metal catalyst of step xv) comprises CuI.9. The method of claim 8 , wherein the reducing agent of step x) comprises a chiral borane compound.10. The method of claim 9 , wherein the chiral borane compound is selected from (R)-1-methyl-3 claim 9 ,3-diphenylhexahydropyrrolo[1 claim 9 ,2-c][1 claim 9 ,3 claim 9 ,2]oxazaborole claim 9 , (R)-3 claim 9 ,3-diphenylhexahydropyrrolo[1 claim 9 ,2-c][1 claim 9 ,3 claim 9 ,2]oxazaborole claim 9 , (R)-1-butyl-3 claim 9 ,3-diphenylhexahydropyrrolo[1 claim 9 ,2-c][1 claim 9 ,3 claim 9 ,2]oxazaborole claim 9 , (R)-tetrahydro-1 claim 9 ,3 claim 9 ,3-triphenyl-1H claim 9 ,3H-pyrrolo[1 claim 9 ,2-c][1 claim 9 ,3 claim 9 ,2]oxaborole claim 9 , (4S)-2-methyl-4 claim 9 , 5 claim 9 ,5-triphenyl-1 claim 9 ,3 claim 9 ,2-oxazaborolidine claim 9 , or any combination thereof.13. The method of claim 12 , wherein the oxidizing agent of step i) comprises MnOor Dess-Martin periodinane.14. The method of claim 12 , wherein the base of step ii) comprises an alkyllithium reagent.16. The method of claim 15 , wherein the transition metal catalyst comprises a compound or complex either of which comprises copper having a +1 oxidation state.17. The method of claim 16 , wherein the transition metal catalyst comprises CuI.27. The method of claim 26 , further comprising the step of:xxiv) reacting the compound of Formula I with diethanolamine in the presence of an organic solvent to generate the ...

Подробнее
Номер записи: 47
04-06-2015 дата публикации

METHOD OF PREPARING ESTER COMPOUND AND ESTER COMPOUND PREPARED THEREBY

Номер: US20150152036A1
Автор: Choe Yong-Jin, KONG Myungjin, Lee Won Jae
Принадлежит:

This invention relates to a method of preparing an ester compound, including adding carboxylic acid to a mixture of glycerol and acetone in the presence of a sulfuric acid catalyst and applying an ultrasonic wave to induce an esterification reaction, and to an ester compound prepared thereby. 1. A method of preparing an ester compound , comprising adding carboxylic acid to a mixture of glycerol and acetone in presence of a sulfuric acid catalyst and applying an ultrasonic wave to induce an esterification reaction.2. The method of claim 1 , wherein the carboxylic acid is formic acid.3. The method of claim 1 , wherein the method is a one-pot process.4. The method of claim 1 , wherein applying the ultrasonic wave is performed at a power density of 20˜700 W/cm.5. The method of claim 1 , wherein applying the ultrasonic wave is performed at a power density of 70˜500 W/cm.6. The method of claim 1 , wherein applying the ultrasonic wave is performed for 1˜400 min.7. The method of claim 1 , wherein applying the ultrasonic wave is performed for 5˜100 min.8. The method of claim 1 , wherein the acetone is added in an amount of 3˜15 equivalents based on the glycerol.9. The method of claim 1 , wherein the formic acid is added in an amount of 1˜5 equivalents based on the glycerol.10. The method of claim 1 , wherein the esterification reaction is carried out at −20˜10° C.11. The method of claim 1 , wherein the ester is prepared at a yield of 30% or more.12. The method of claim 1 , wherein the ester compound is any one or more selected from the group consisting of (2 claim 1 ,2-dimethyl-1 claim 1 ,3-dioxolan-4-yl)methyl formate claim 1 , 2 claim 1 ,2-dimethyl-1 claim 1 ,3-dioxan-5-yl formate claim 1 , glyceryl formate and 2-hydroxypropane-1 claim 1 ,3-diyl diformate.13. An ester compound prepared by the method of .14. The ester compound of claim 13 , wherein the ester compound is any one or more selected from the group consisting of (2 claim 13 ,2-dimethyl-1 claim 13 ,3-dioxolan-4-yl ...

Подробнее
Номер записи: 48
14-08-2014 дата публикации

Novel Compound

Номер: US20140228339A1
Автор: CONNOLLY Stephen, Ebden Mark Richard, LANGER Thomas, Steven Alan Robert, Stewart Craig Robert, Tomlin Paula Margaret, Walters Iain Alastair Stewart, Williams Andrew John
Принадлежит: AstraZeneca AB

There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. 2. A compound according to of the formula (I).3. A pharmaceutical composition which comprises a compound as claimed in claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.4. A compound as claimed in for use in therapy.5. A compound as claimed in in the manufacture of a medicament for use in therapy.6. A compound as claimed in for the treatment of a chemokine mediated disease state.7. A compound as claimed in for the treatment of asthma claim 1 , allergic rhinitis claim 1 , chronic obstructive pulmonary disease claim 1 , inflammatory bowel disease claim 1 , irritable bowel syndrome claim 1 , osteoarthritis claim 1 , osteoporosis claim 1 , rheumatoid arthritis or psoriasis.8. A method of treating a chemokine mediated disease state in a mammal suffering from claim 1 , or at risk of claim 1 , said disease claim 1 , which comprises administering to a mammal in need of such treatment a therapeutically effective amount of a compound as claimed in .9. A compound as claimed in in a crystalline form.10. A crystalline form as claimed in claim 9 , characterised by an X-ray powder diffraction pattern claim 9 , measured using a wavelength of X-rays 1.5418 Å claim 9 , with at least one peak at 2-Theta (in degrees) selected from 8.5 claim 9 , 9.7 claim 9 , 10.6 claim 9 , 17.1 claim 9 , 19.9 claim 9 , and 21.2.11. A crystalline form as claimed in claim 9 , characterised by an X-ray powder diffraction pattern claim 9 , measured using a wavelength of X-rays 1.5418 Å claim 9 , with at least two or more peaks at 2-Theta (in degrees) selected from 8.5 claim 9 , 9.7 claim 9 , 10.6 claim 9 , 17.1 claim 9 , 19.9 claim 9 , and 21.2.12. ...

Подробнее
Номер записи: 49
14-08-2014 дата публикации

Process for the production of a dioxolane compound from crude glycerol including a liquid-liquid extraction step

Номер: US20140228584A1
Автор: Malheiro Arthur, Rodrigues Edson
Принадлежит: RHODIA POLIAMIDA E ESPECIALIDADES LTDA

A process for the production of dioxolane compounds of formula (I), wherein R1 and R2 independently represent hydrogen or an alkyl chain from 1 to 10 carbon atoms; R3 and R4 independently represent hydrogen, an alkyl chain from 1 to 5 carbon atoms or an alkyl chain from 1 to 5 carbon atoms endowed with one or more hydroxyl groups. Such process comprises successively a reaction step between crude glycerol and aldehyde or ketone and a liquid-liquid extraction step with an extracting ketonic solvent corresponding to formula (II) with A and B independently being an alkyl chain with 2 to 10 carbon atoms, or phenyl, A and B not comprising hydroxyl functions. 2. The process according to claim 1 , wherein at least one of R1 and R2 is selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl claim 1 , isobutyl claim 1 , pentyl claim 1 , and isopentyl.3. The process according to claim 1 , wherein said ketonic solvent for said liquid-liquid extraction step is selected from the group consisting of methyl isobutyl ketone (MIBK) claim 1 , diisobutyl ketone (DIBK) claim 1 , acetophenone claim 1 , and combination thereof.4. The process according to claim 1 , wherein said ketone in said reaction step is at least one ketone selected from the group consisting of acetone claim 1 , cyclohexanone claim 1 , methyl cyclohexanone claim 1 , methyl cyclopentanone claim 1 , methyl isobutyl ketone claim 1 , 4-hydroxy-4-methyl-2-pentanone claim 1 , 2-butanone claim 1 , 3 -butanone claim 1 , diisobutyl ketone claim 1 , 4-methyl-3 -penten-2-one claim 1 , 2-nonanone claim 1 , 2-pentanone claim 1 , 3 -methyl-2-butanone claim 1 , and 1 -phenylethanone.5. The process according to claim 1 , wherein said aldehyde in said reaction step is one or more at least one aldehyde selected from the group consisting of formaldehyde claim 1 , acetaldehyde claim 1 , 2-ethylhexanaL and furfuraldehyde.6. The process according to claim 1 , wherein said dioxolane ...

Подробнее
Номер записи: 50
21-08-2014 дата публикации

NOVEL LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20140235872A1
Автор: Budzik Brian W., Colletti Steven L., DAVIS Jennifer R., Hills Ivory D., SEIFRIED Darla Danile, Stanton Matthew G.
Принадлежит: Sirna Therapeutics, Inc.

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A cationic lipid of Formula A according to claim 1 ,wherein:{'sup': 1', '2, 'Rand Rare each methyl;'}{'sub': 1', '4', '22', '4', '22, 'Lis selected from C-Calkyl and C-Calkenyl; and'}{'sub': 2', '3', '13', '3', '13, 'Lis selected from C-Calkyl and C-Calkenyl;'}or any pharmaceutically acceptable salt or stereoisomer thereof.3. A cationic lipid which is selected from:R—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 2);S—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 1);1-{2-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-1-[(octyloxy)methyl]ethyl}pyrrolidine (Compound 3);(2S)—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-[(5Z)-oct-5-en-1-yloxy]propan-2-amine (Compound 4);1-{2-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-1-[(octyloxy)methyl]ethyl}azetidine (Compound 5);(2S)-1-(hexyloxy)-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 6);(2S)-1-(heptyloxy)-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 7);N,N-dimethyl-1-(nonyloxy)-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 8);N,N-dimethyl-1-[(9Z)-octadec-9-en-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 9);(2S)—N,N-dimethyl-1-[(6Z,9Z,12Z)-octadeca-6,9,12-trien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 10);(2S)-1-[(11Z,14Z)-icosa-11,14-dien-1-yloxy]-N,N-dimethyl-3-(pentyloxy)propan-2-amine (Compound 11);( ...

Подробнее
Номер записи: 51
21-08-2014 дата публикации

Process for the production of a dioxolane compound from crude glycerol

Номер: US20140235878A1
Автор: Malheiro Arthur, Rodrigues Edson
Принадлежит: RHODIA POLIAMIDA E ESPECIALIDADES LTDA

A process for the production of dioxolane compounds of formula (I): 2. The process according to claim 1 , characterized by the wherein at least one of R1 and R2 is selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl claim 1 , isobutyl claim 1 , pentyl claim 1 , and isopentyl.3. The process according to claim 1 , wherein said molar ratio of aldehyde:glycerol or ketone:glycerol is from 4:1 to 15:1.4. Process The process according to claim 1 , wherein said ketone in said reaction is or more of at least one ketone selected from the group consisting of acetone claim 1 , cyclohexanone claim 1 , methyl cyclohexanone claim 1 , methyl cyclopentanone claim 1 , methyl isobutyl ketone claim 1 , 4-hydroxy-4-methyl-2-pentanone claim 1 , 2-butanone claim 1 , 3-butanone claim 1 , diisobutyl ketone claim 1 , 4-methyl-3-penten-2-one claim 1 , 2-nonanone claim 1 , 2-pentanone claim 1 , 3-methyl-2-butanone claim 1 , and 1-phenylethanone.5. The process according to claim 1 , wherein said aldehyde in said reaction is at least one aldehyde selected from the group consisting of formaldehyde claim 1 , acetaldehyde claim 1 , 2-ethylhexanal claim 1 , and furfuraldehyde.6. The process according to claim 1 , wherein said dioxolane compound is a 2-hydrocarbyl-1 claim 1 ,3-dioxolane-4-methanol compound.7. The process according to claim 1 , comprising the steps of:a)—in a reaction vessel, reacting said crude glycerol and said ketone or said aldehyde,b)—allowing decantation, then separating solids, the remaining liquid fraction presenting a light phase and a heavy phase;c)—removing salt from said heavy phase, the remaining portion thereof being optionally returned to the reaction vessel;d)—subjecting said light phase to distillation to separate the dioxolane compound from said ketone or said aldehyde, which are being optionally recycled to the reaction vessel; ande)—subjecting the obtained dioxolane compound from step d) to a further ...

Подробнее
Номер записи: 52
16-06-2016 дата публикации

MODIFIED OLIGOESTERS AND MANUFACTURE METHODS OF THE OLIGOESTERS

Номер: US20160168315A1
Автор: HERNANDEZ GARCIA Hugo Fernando, ILLERA QUINTERO Juan David, PAVONE CORREA Sebastian
Принадлежит: ANHIDRIDOS Y DERIVADOS DE COLOMBIA S.A. ANDERCOL

The present invention relates to a modified oligoester including an oligoester () that in one of its ends has a group that reacts with alcohols or organic acids forming covalent bonds and in one or more of its other terminations has one or more cyclic acetal groups (). In addition, relates to the processes for the production of such modified oligoester, as well as the use of the same in the manufacture of polyester resins, coating compositions, and composite, as well as the process for producing these resins. The scope of the present invention is related to the chemical sector, particularly in what refers to modified oligoesters with cyclic acetal groups. 1. A modified oligoester comprising:{'b': 1', '2, 'an oligoester () containing at least one esterifiable functional group in one terminations and bounded in one or more of the ends of a chain with a cyclic acetal group ().'}31. The modified oligoester according to claim 1 , wherein the oligoester () comes from:{'b': 3', '4', '5, 'an esterification reaction between esterifiables monomers selected from the group consisting of polyols (), carboxylic polyacids (), and hydroxyacids (),'}ordepolymerization of virgin or waste polyesters, including at least one of the following:polyglycolic acid, polylactic acid, polycaprolactone, polyethylene adipate, polyethylene naphthalate, polyethylene terephthalate, polybutylene succinate, polybutylene terephthalate, polytrimethylene terephthalate, polyhydroxybutyrate, and polyhydroxyvalerate.421517. The modified oligoester according to claim 1 , wherein the cyclic acetals () groups come from oligoacetals () or monohydric cyclic acetals ().5151689. The modified oligoester modified according to claim 4 , wherein the oligoacetals () come from the reaction between a triol () with an aldehyde () or a ketone ().6171689. The modified oligoester according to claim 4 , wherein the monohydric cyclic acetals () come from the reaction between a triol () with an () aldehyde or a ketone (). ...

Подробнее
Номер записи: 53
25-06-2015 дата публикации

KETAL AMIDE COMPOUNDS, METHODS OF MAKING, AND APPLICATIONS

Номер: US20150175568A1
Автор: GOETZ Adam E., SCHOLTEN Marc D., SELIFONOV Sergey, ZHOU Ning
Принадлежит:

Disclosed herein are ketal amide compounds. The ketal amide compounds are synthesized by the reaction of ketal acids or ketal esters with amine functional compounds. Also disclosed are methodologies useful to make the ketal amide compounds. Also disclosed herein are formulations and articles containing the ketal amide compounds. 2. The compound of wherein the one or more heteroatoms are independently halogen claim 1 , nitrogen claim 1 , oxygen claim 1 , sulfur claim 1 , silicon claim 1 , or phosphorus.3. The compound of wherein the one or more heteroatoms are in a functional group that is amino claim 2 , carbonate claim 2 , imide claim 2 , amide claim 2 , sulfone claim 2 , sulfonamide claim 2 , urethane claim 2 , mercapto claim 2 , disulfide claim 2 , ether claim 2 , ester claim 2 , phosphate claim 2 , phosphonooxy claim 2 , silane claim 2 , or silyl functional groups claim 2 , or a combination thereof.4. The compound of wherein the polymeric group comprises a surface claim 1 , a layer on top of a surface claim 1 , a particle surface claim 1 , or a porous particle interior.5. The compound of wherein α is 2 and Ris —(CH)— claim 1 , 1 claim 1 ,2-cyclohexyl claim 1 , —(CH)— claim 1 , —CHCHCH(CH)CHC(CH)CH— claim 1 , or —CHCHC(CH)CHCH(CH)CH—.6. The compound of wherein all values of a are 0 claim 1 , 1 claim 1 , or 2.7. The compound of wherein all values of a are 2 and all Rand Rare hydrogen.8. The compound of wherein all Rare methyl.9. The compound of wherein all b are 0 and all Rand Rare hydrogen.10. The compound of wherein all b are 1 claim 1 , all Rare —CHOH claim 1 , all Rare CHCHor CH claim 1 , and all R claim 1 , Rare H.11. The compound of wherein Ris —CH—OH12. The compound of wherein α is 2.15. The compound of wherein the A groups comprise a mixture of saturated and unsaturated fatty acid ester groups.16. A formulation comprising the compound of .17. The formulation of wherein the compound of is a plasticizer claim 1 , a coalescing solvent claim 1 , a cosolvent ...

Подробнее
Номер записи: 54
25-06-2015 дата публикации

SYNTHESIS OF ENT-PROGESTERONE AND INTERMEDIATES THEREOF

Номер: US20150175650A1
Автор: Levy Daniel E., Zhan Xinxi, ZHANG Faliang
Принадлежит:

The present invention relates to the synthesis of ent-progesterone and intermediates thereof. 6. The method for preparing ent-progesterone according to claim 5 , wherein R is —OTs claim 5 , —OMs claim 5 , —OTf claim 5 , —Cl claim 5 , —Br claim 5 , or —I.8. The method for preparing ent-progesterone according to claim 7 , wherein the reaction step comprises a reductive silylation followed by de-silylation and methylation.15. The method for preparing ent-progesterone according to claim 14 , wherein R is —OTs claim 14 , —OMs claim 14 , —OTf claim 14 , —Cl claim 14 , —Br claim 14 , or —I.21. A method for preparing ent-progesterone comprising the step of reacting an enone intermediate compound with triethylsilane and a catalyst to form a silyl enol ether.22. The method for preparing ent-progesterone according to claim 1 , wherein said method has fewer than 17 linear steps.23. The method for preparing ent-progesterone according to claim 1 , wherein said method has fewer than 15 linear steps.24. The method for preparing ent-progesterone according to claim 1 , wherein said method has fewer than 13 linear steps.25. The method for preparing ent-progesterone according to claim 1 , wherein said method has fewer than 12 linear steps.26. The method for preparing ent-progesterone according to claim 2 , wherein said method has fewer than 17 linear steps.27. The method for preparing ent-progesterone according to claim 2 , wherein said method has fewer than 15 linear steps.28. The method for preparing ent-progesterone according to claim 2 , wherein said method has fewer than 13 linear steps.29. The method for preparing ent-progesterone according to claim 2 , wherein said method has fewer than 12 linear steps.30. The method for preparing ent-progesterone according to claim 3 , wherein said method has fewer than 17 linear steps.31. The method for preparing ent-progesterone according to claim 3 , wherein said method has fewer than 15 linear steps.32. The method for preparing ent- ...

Подробнее
Номер записи: 55
01-07-2021 дата публикации

FRAGRANCE AND FLAVOR MATERIALS FROM 1-(2-HYDROXY-4-METHYLCYCLOHEXYL)-ETHANONE

Номер: US20210198229A1
Автор: Dickerson Thalia S., Lankin Michael E., Lombardo Louis J.
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present disclosure is directed to 1-(2-hydroxy-4-methycyclohexyl)-ethanone derivatives having unique and desired flavor and/or fragrance characteristics, as well as the synthesis and application of the derivatives. The compounds of the present disclosure can be employed alone or incorporated as fragrance or flavor ingredients to modify or enhance already existing fragrance compositions, solvents, media, and the like. 2. The compound of claim 1 , wherein Ris one of —OH claim 1 , —NOH—NOR claim 1 , or NOC(O)R; and wherein Ris —OH.5. (canceled)6. (canceled)7. A fragrance composition comprising at least one compound of .8. The fragrance composition of claim 7 , wherein the concentration of the at least one compound is from about 0.001% to about 20% by weight of the fragrance composition.9. The fragrance composition of claim 7 , further comprising one or more compounds selected from the group consisting of one or more aldehydic compound(s) claim 7 , one or more animalic compound(s) claim 7 , one or more balsamic compound(s) claim 7 , one or more citrus compound(s) claim 7 , one or more floral compound(s) claim 7 , one or more fruity compound(s) claim 7 , one or more gourmand compound(s) claim 7 , one or more green compound(s) one or more herbaceous compound(s) one or more marine compound(s) claim 7 , one or more mossy compound(s) claim 7 , one or more musk compound(s) claim 7 , one or more piney compound(s) claim 7 , one or more powdery compound(s) claim 7 , one or more spicy compound(s) and/or one or more woody compound(s) claim 7 , and combinations thereof.10. A flavor composition comprising at least one compound of .11. The flavor composition of claim 10 , wherein the concentration of the at least one compound is from about 0.0001% to about 20% by weight of the flavor composition.12. The flavor composition of claim 10 , further comprising a flavor carrier. This application claims priority to U.S. Provisional Patent Application Ser. No. 62/640,490, filed Mar. 8, ...

Подробнее
Номер записи: 56
06-06-2019 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20190167800A1
Автор: Butler David, Eltepu Laxman, Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure 3. A lipid particle comprising a lipid of .4. (canceled)5. The lipid particle of claim 3 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.6. The lipid particle of claim 3 , wherein the lipid particle consists essentially of{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. a lipid of ;'}b. a neutral lipid selected from DSPC, DPPC, POPC, DOPE and SM;c. a sterol; andd. PEG-DMG,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'in a molar ratio of about 20-60% lipid of : 5-25% neutral lipid:25-55% sterol: 0.5-15% PEG-DMG.'}7. The lipid particle of claim 3 , further comprising a therapeutic agent.8. The lipid particle of claim 7 , wherein the therapeutic agent is a nucleic acid.9. The lipid particle of claim 8 , wherein the nucleic acid is a plasmid.10. The lipid particle of claim 8 , wherein the nucleic acid is an immunostimulatory oligonucleotide.11. The lipid particle of claim 8 , wherein the nucleic acid is selected from the group consisting of an siRNA claim 8 , an antisense oligonucleotide claim 8 , a microRNA claim 8 , an antagomir claim 8 , an aptamer claim 8 , and a ribozyme.12. The lipid particle of claim 11 , wherein the nucleic acid is an siRNA.13. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 7 , carrier claim 7 , or diluent.14. A method of modulating the expression of a target gene in a cell claim 7 , comprising providing to a cell the lipid particle of .15. The method of claim 14 , wherein the therapeutic agent is selected from an siRNA claim 14 , an antagomir claim 14 , an antisense oligonucleotide claim 14 , and a plasmid capable of expressing an siRNA claim 14 , a ribozyme claim 14 , an aptamer or an antisense ...

Подробнее
Номер записи: 57
30-06-2016 дата публикации

DIOXOLANE DERIVATIVE, LIQUID CRYSTAL COMPOSITION, LIQUID CRYSTAL ELEMENT, AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20160185746A1
Автор: Ishitani Tetsuji, Kato Momoko, Kawata Yuko, Niikura Yasuhiro
Принадлежит:

A dioxolane derivative represented by formula (G1) is provided. The explanation of the substituents is given in the specification. The use of the dioxolane derivative enables the production of a liquid crystal composition and a liquid crystal display device including the liquid crystal composition. 3. The compound according to claim 1 ,{'sup': 23', '24, 'wherein Arand Areach represent a substituted or unsubstituted aryl group having 6 to 12 carbon atoms.'}4. The compound according to claim 1 ,wherein:{'sup': 23', '24, 'Arand Areach represent a substituted or unsubstituted aryl group having 6 to 12 carbon atoms;'}{'sup': 1', '2, 'Arand Areach represent hydrogen; and'}{'sup': 1', '2, 'aand aeach represent a single bond.'}5. The compound according to claim 1 ,wherein the compound is optically active.7. A composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound according to ; and'}a liquid crystal.8. A liquid crystal display device comprising the composition according to .10. The compound according to claim 9 ,{'sup': '41', 'wherein Arrepresents a substituted or unsubstituted arylene group having 6 to 12 carbon atoms.'}11. The compound according to claim 9 ,wherein:{'sup': '41', 'Arrepresents a substituted or unsubstituted arylene group having 6 to 12 carbon atoms; and'}{'sup': '3', 'Rrepresents a substituted or unsubstituted alkoxy group having 1 to 6 carbon atoms.'}12. The compound according to claim 9 ,wherein the compound is optically active.14. A composition comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'the compound according to ; and'}a liquid crystal.15. A liquid crystal display device comprising the composition according to . 1. Field of the InventionOne embodiment of the present invention relates to a semiconductor device, a display device, a driving method thereof, or a manufacturing method thereof. In particular, one embodiment of the present invention relates to a novel dioxolane derivative, a liquid crystal ...

Подробнее
Номер записи: 58
04-06-2020 дата публикации

HYDROFORMYLATION PROCESS FOR PRODUCING 1,6-HEXANEDIOL DERIVATIVES

Номер: US20200172458A1
Автор: Ernst Martin, Luyken Hermann, MARION Nicolas, Melder Johann-Peter, Paciello Rocco, PAZICKY Marek
Принадлежит:

The present invention relates to a two-stage hydroformylation process for producing pound of the formula (I) and to a process for producing a compound of the formula (V) comprising the two-stage hydroformylation process for producing a compound of the formula (I) followed by hydrogenation of the compound of the formula (I). 113.-. (canceled)16. The process according to claim 14 , wherein the at least one compound of the formula (II) is butadiene.17. The process according to claim 14 , wherein the molar ratio of the at least one compound of the formula (II) to the at least one alkanol of the formula (III) is in the range from 1:1 to 1:100.18. The process according to claim 14 , wherein the acid used in process step a) has a pK-value relative to water in the range from −14 to 7.19. The process according to claim 15 , wherein the acid used in process step a) has a pK-value relative to water in the range from −2 to 5.20. The process according to claim 14 , wherein the at least one transition metal catalyst TMC 1 used in process step a) comprises at least one transition metal selected from Co claim 14 , Ru claim 14 , Ir claim 14 , Rh claim 14 , Ni claim 14 , Pd and Pt.21. The process according to claim 14 , wherein the at least one transition metal catalyst TMC 1 used in process step a) comprises at least Rh.22. The process according to claim 14 , wherein the at least one transition metal catalyst TMC 2 used in process step c) comprises at least one transition metal selected from Co claim 14 , Ru claim 14 , Ir claim 14 , Rh claim 14 , Ni claim 14 , Pd and. Pt.23. Process according to claim 14 , wherein the at least one transition metal catalyst TMC 1 used in process step a) and the at least one transition metal catalyst TMC 2 used in process step c) both comprise Rh.24. The process according to claim 14 , wherein the at least one transition metal catalyst TMC 1 used in process step a) and the at least one transition metal catalyst TMC 2 used in process step c) each ...

Подробнее
Номер записи: 59
05-07-2018 дата публикации

CLEAVABLE SURFACTANTS

Номер: US20180187127A1
Автор: Hitko Carolyn Woodroofe, Klaubert Dieter, Saveliev Sergei, Simpson Daniel, Uyeda Harry Tetsuo, Wood Keith V.
Принадлежит:

The invention provides surfactant compounds of formulas I-IX, which can be used in methods for aiding the solubilization, digestion, preparation, analysis, and/or characterization of biological material, for example, proteins or cell membranes. The compounds can also aid in the recovery of peptides generated during protein digestion, particularly for in-gel digestion protocol. Additionally, the compounds can improve enzymatic protein deglycosylation without interfering with downstream sample preparation steps and mass spectrometric analysis. The compounds can be specifically useful as digestion aids that can be decomposed by an acid, by heat, or a combination thereof. Decomposition of the surfactants allows for facile separation from isolated samples, and/or allows for analysis of the sample without interfering with the sensitivity of various analytical techniques. 110-. (canceled)12. The method of wherein the biomaterial is in a gel or is bound to a solid support.13. The method of wherein the biomaterial is in an aqueous solution.14. The method wherein the digestion reagent comprises one or more of a protease claim 11 , CNBr claim 11 , or hydroxylamine.15. The method of wherein the protease is a serine protease.16. The method of wherein the serine protease is trypsin or chymotrypsin.17. The method of further comprising decomposing the surfactant compound after protein digestion claim 11 , wherein the degrading optionally comprises contacting the surfactant compound with an acidic solution claim 11 , heating the surfactant compound claim 11 , or a combination thereof.18. The method of wherein the surfactant compound self-hydrolyses in solution after protein digestion.19. The method of further comprising isolating the one or more digested proteins.20. The method of further comprising analyzing the digested proteins claim 11 , wherein the digested proteins are analyzed by mass spectrometry claim 11 , liquid chromatography claim 11 , gel electrophoresis claim 11 , or a ...

Подробнее
Номер записи: 60
14-07-2016 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20160199485A1
Автор: Ansell Steven, CHEN Jianxin, Eltepu Laxman, Jayaraman Muthusamy, Manoharan Muthiah, Rajeev Kallanthottathil G.
Принадлежит: TEKMIRA PHARMACEUTICALS CORPORATION

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure 3. A lipid particle comprising a lipid of .4. (canceled)5. The lipid particle of claim 3 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.6. The lipid particle of claim 5 , wherein the lipid particle consists essentially of{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'a. Lipid of ;'}b. a neutral lipid selected from DSPC, DPPC, POPC, DOPE and SM;c. sterol; andd. PEG-DMG,{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'in a molar ratio of about 20-60% lipid of : 5-25% neutral lipid:25-55% sterol:0.5-15% PEG-DMG or PEG DMA.'}7. The lipid particle of claim 3 , further comprising a therapeutic agent.8. The lipid particle of claim 7 , wherein the therapeutic agent is a nucleic acid.9. The lipid particle of claim 8 , wherein the nucleic acid is a plasmid.10. The lipid particle of claim 8 , wherein the nucleic acid is an immunostimulatory oligonucleotide.11. The lipid particle of claim 8 , wherein the nucleic acid is selected from the group consisting of an siRNA claim 8 , an antisense oligonucleotide claim 8 , a microRNA claim 8 , an antagomir claim 8 , an aptamer claim 8 , and a ribozyme.12. The lipid particle of claim 11 , wherein the nucleic acid is an siRNA.13. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 8 , carrier claim 8 , or diluent.14. A method of modulating the expression of a target gene in a cell claim 7 , comprising providing to a cell the lipid particle of .15. The method of claim 14 , wherein the therapeutic agent is selected from an siRNA claim 14 , an antagomir claim 14 , an antisense oligonucleotide claim 14 , and a plasmid capable of expressing an siRNA claim 14 , a ribozyme claim 14 , an aptamer or an antisense ...

Подробнее
Номер записи: 61
23-07-2015 дата публикации

Trans-2-nonadecyl-4-hydroxymethyl-1,3-dioxolane and method for producing thereof

Номер: US20150203466A1
Автор: CHANG Chi-I, HSU Pang-Kuei, Pan Min-Hsiung, WU Chia-Feng
Принадлежит:

The present invention discloses a method for producing trans-2-nonadecyl-4-hydroxymethyl-1,3-dioxolane comprising mixing alkanes and pyridinium chlorochromat for an oxidation reaction; obtaining a product by the oxidation reaction for processing an aldolization reaction and then purifying for obtaining a trans-2-nonadecyl-4-hydroxymethyl-1,3-dioxolane compound. According to the method of the present invention, it is able to promote the productivity and reduce the cost. 4. The method according to claim 2 , wherein an acidic catalyst is used during the acetalization reaction.5. The method according to claim 2 , wherein the mixture containing the compound of formula (I) can be purified by separation process.6. A method for treating liver disease claim 1 , comprising administering a subject an effective amount of a compound of formula (I) or pharmaceutically acceptable salts thereof according to .7. The method according to claim 6 , wherein the liver disease is liver fibrosis related disease. The present invention relates to a compound and method for producing thereof, especially relates to a trans-2-nonadecyl-4-hydroxymethyl-1,3-dioxolane and method for producing thereof.Liver diseases have apparently become an important concern to modern people. More specifically, the factors like alcohol, medicine, drug or virus can cause the chronic inflammation of liver parenchyma continuously or repeatedly happened. It results in lasting damages, even necrosis, about liver cells and engages the individual in high risks of liver diseases like fatty liver or liver cirrhosis, even has an extremely high risk to become liver cancer. Liver fibrosis is a pathological symptom of chronic liver damage. The main cause lies on proliferation and decomposition of liver fibrillar connective tissues which were under an unbalance status and over-accumulated liver extracellular matrixes when liver cells suffered last and long damages. Liver fibrosis is also an essential process for that the chronic ...

Подробнее
Номер записи: 62
25-09-2014 дата публикации

CROSS-METATHESIS REACTION OF FUNCTIONALIZED AND SUBSTITUTED OLEFINS USING GROUP 8 TRANSITION METAL CARBENE COMPLEXES AS METATHESIS CATALYSTS

Номер: US20140288319A1
Автор: CHATTERJEE Arnab K., CHOI Tae-Lim, Goldberg Steven D., GRUBBS Robert H., LOVE Jennifer A., MORGAN John P., Sanders Daniel P., Scholl Matthias, TOSTE F. Dean, TRNKA Tina M.
Принадлежит: California Institute of Technology

The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand are used to catalyze cross-metathesis reactions to provide a variety of substituted and functionalized olefins, including phosphonate-substituted olefins, directly halogenated olefins, 1,1,2-trisubstituted olefins, and quaternary allylic olefins. The invention further provides a method for creating functional diversity using the aforementioned complexes to catalyze cross-metathesis reactions of a first olefinic reactant, which may or may not be substituted with a functional group, with each of a plurality of different olefinic reactants, which may or may not be substituted with functional groups, to give a plurality of structurally distinct olefinic products. The methodology of the invention is also useful in facilitating the stereoselective synthesis of 1,2-disubstituted olefins in the cis configuration. 27-. (canceled)9. The method of claim 8 , wherein:M is Ru;{'sup': 1', '2, 'sub': 3', '2', '3', '2', '2', '2', '3', '3', '3', '2', '3', '3', '3', '2, 'Xand Xare independently selected from the group consisting of halide, CFCO, CHCO, CFHCO, (CH)CO, (CF)(CH)CO, (CF)(CH)CO, PhO, MeO, EtO, tosylate, mesylate, and trifluoromethanesulfonate;'}{'sup': 1', '2, 'sub': 1', '20', '2', '20, 'Ris hydrogen and Ris selected from the group consisting of C-Calkyl, C-Calkenyl, and aryl;'}L is a neutral electron donor ligand selected from the group consisting of phosphine, phosphite, phosphinite, phosphonite, ether, amine, amide, imine, carboxyl, pyridine, substituted pyridine, imidazole, and substituted imidazole;{'sup': 3', '4, 'Rand Rare aromatic, substituted aromatic, heteroaromatic, substituted heteroaromatic, alicyclic, substituted alicyclic, heteroatom-containing alicyclic, or substituted heteroatom-containing alicyclic, composed of from one ...

Подробнее
Номер записи: 63
30-07-2015 дата публикации

Liquid crystal composition, liquid crystal element, and liquid crystal display device

Номер: US20150210924A1
Автор: Sachiko Kawakami, Tetsuji Ishitani, Tomohiro Tamura, Yasuhiro Niikura, Yuko Kawata
Принадлежит: Semiconductor Energy Laboratory Co Ltd

A liquid crystal composition including a dioxolane compound represented by the general formula (G1) as a chiral agent is provided. In the general formula (G1), R 1 and R 2 individually represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, an aryl group having 6 to 12 carbon atoms, and an alkyl group having 1 to 20 carbon atoms and having a phenyl group as a substituent; R 1 and R 2 may be bonded to each other to form a ring; R 3 and R 4 individually represent any of hydrogen, an alkyl group having 1 to 6 carbon atoms, and a cycloalkyl group; and R 5 to R 40 individually represent any of hydrogen, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, and an aryl group having 6 to 12 carbon atoms.

Подробнее
Номер записи: 64
27-06-2019 дата публикации

COALESCING AGENT DERIVED FROM DIOXOLANE DERIVATIVES

Номер: US20190194157A1
Автор: KAEOTHIP SOPHON, PIMOLSIRIPHOL VORAPONG, PORNSURIYASAK PAPAPIDA
Принадлежит: PTT Global Chemical Public Company Limited

The present invention relates to a coalescing agent as represented in structure (I); wherein; n is integer from 1 to 8; Rand Rindependently represent group selected from hydrogen atom, alkyl, alkenyl, alkynyl, phenyl, benzyl groups, or optionally cyclic hydrocarbon containing heteroatom; and Y represents group selected from alkyl, alkenyl, alkynyl, phenyl, benzyl groups, or cyclic hydrocarbon containing heteroatom. The said coalescing agent can be used in coating application with efficacy to provide smooth consistent film with chemical and scratch resistant and has no pungent odour, wherein the preparation method of this compound is simplify and employs less harmful chemicals. 130.-. (canceled)32. The coalescing agent derived from dioxolane derivatives according to claim 31 , wherein n is integer from 1 to 4.33. The coalescing agent derived from dioxolane derivatives according to claim 31 , wherein Rand Rare selected from hydrogen atom or alkyl group containing 1 to 8 carbon atoms claim 31 , Y is selected from alkyl group containing 1 to 4 carbon atoms and cyclic hydrocarbon containing heteroatom.35. The coalescing agent derived from dioxolane derivatives according to claim 34 , wherein Rand Rare selected from hydrogen atom or alkyl group containing 1 to 8 carbon atoms.36. The coalescing agent derived from dioxolane derivatives according to claim 31 , wherein said coalescing agent is prepared from method comprising steps:i) mixing glycerol and aldehyde or ketone compound at ratio of 1:1 to 1:6 using acid as catalyst;ii) mixing the compound obtained from step i) and dicarboxylic acid ester compound at ratio of 1:1 to 1:3 using base as catalyst;37. The coalescing agent derived from dioxolane derivatives according to claim 36 , wherein the aldehyde or ketone compound in the reaction in step i) is selected from 2-ethyl hexanal claim 36 , acetone claim 36 , methyl ethyl ketone claim 36 , or mixture thereof.38. The coalescing agent derived from dioxolane derivatives ...

Подробнее
Номер записи: 65
27-06-2019 дата публикации

Arthropod repellent chemicals

Номер: US20190194158A1
Автор: Anandasankar Ray, Christine Krause Pham, Sean Michael Boyle
Принадлежит: UNIVERSITY OF CALIFORNIA

Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.

Подробнее
Номер записи: 66
18-06-2020 дата публикации

NITROGEN AND DIOXOLANE-CONTAINING HYDROFLUOROETHERS AND METHODS OF USING THE SAME

Номер: US20200190071A1
Автор: Costello Michael G., Lamanna William M., Teverovskiy Georgiy
Принадлежит:

Described herein is dioxolane-containing compound of formula (I) wherein (i) Rfand Rfare independently linear or branched perfluoroalkyi groups having with 1-8 carbon atoms and optionally comprise at least one catenated heteroatom, or (ii) Rfand Rfare bonded together to form a ring structure having 4-6 carbon atoms and optionally comprise one or more catenated heteroatoms; Rfis a linear or branched perfluoroalkyi groups having with 1-3 carbon atoms; and Rand Rare independently selected from H, F, Cl, a linear or branched alkyl group having 1-3 carbon atoms, optionally wherein the alkyl group comprises at least one of: fluorine, chlorine, a hydroxyl group, or a catenated heteroatom; for use in cleaning compositions, as an electrolyte solvent, as a heat transfer fluid, or a vapor phase soldering fluid. There is also provided a method of making the dioxolane-containing compound, comprising: contacting a 1,2-diol compound with a fluorinated ethylenically unsaturated compound in the presence of a base. 2. The dioxolane-containing compound of claim 1 , wherein Rand Rare H.3. The dioxolane-containing compound of claim 1 , wherein Ris CF.4. The dioxolane-containing compound of claim 1 , wherein Rand Rare bonded together to form a 5 claim 1 , 6 claim 1 , or 7 membered ring.5. The dioxolane-containing compound of claim 1 , wherein Rand Rare bonded together to form a 6-membered perfluorinated ring comprising a catenated O atom.6. The dioxolane-containing compound of claim 5 , wherein Rand Rform a morpholine group.7. The dioxolane-containing compound of claim 1 , wherein Rand Rare bonded together to form a 6-membered perfluorinated ring comprising an additional catenated N atom.8. The dioxolane-containing compound of claim 7 , wherein Rand Rform an N-perfluoroalkyl piperizine group.9. The dioxolane-containing compound of claim 1 , wherein Rand Rform a pyrrolidine group.10. The dioxolane-containing compound of claim 1 , wherein Rand Rare independently selected from CF claim 1 , ...

Подробнее
Номер записи: 67
04-08-2016 дата публикации

Method for the preparation of thiadiazoles

Номер: US20160221985A1
Автор: Babak Riahi, Eric A. Bercot, Jason TEDROW, Johann CHAN, John Colyer, Matthew Bio, Robert R. MILBURN, Steven Mennen, Yuanqing Fang
Принадлежит: Individual

The present invention relates to processes for preparing protected glyceraldehydes, such as (hydroxy)methanesulfonates. In addition, the invention relates to thiadiazoles, particularly 3-diooxolanyl-thiadiazoles.

Подробнее
Номер записи: 68
12-08-2021 дата публикации

HYDROPHILIC METAL SURFACE TREATMENT AGENT

Номер: US20210246560A1
Автор: HYUGA Toshio, Nemoto Hisao, YAMADA Shoichi
Принадлежит:

The objective of the present invention is to provide a hydrophilic metal surface treatment agent by which a water-repellent property can be given to a metal surface with suppressing a corrosion and a discolorment of the metal, a method for treating a surface of a metal by using the hydrophilic metal surface treatment agent, a synthetic intermediate compound of a branched glycerol derivative as an active ingredient of the hydrophilic metal surface treatment agent, and a method for efficiently producing the synthetic intermediate compound. The hydrophilic metal surface treatment agent of the present invention is characterized in comprising the branched glycerol derivative represented by the following formula (I) as an active ingredient. 2. The hydrophilic metal surface treatment agent according to claim 1 , comprising water as a solvent.3. The hydrophilic metal surface treatment agent according to claim 2 , wherein a concentration of the branched glycerol derivative represented by the formula (I) is 0.005 mM or more and 5 mM or less.4. The hydrophilic metal surface treatment agent according to claim 2 , wherein a concentration of the branched glycerol derivative represented by the formula (I) is 0.001 mass % or more and 5 mass % or less.5. The hydrophilic metal surface treatment agent according to claim 1 , further comprising an alkaline agent.6. The hydrophilic metal surface treatment agent according to claim 1 , further comprising a surfactant.7. A method for treating a surface of a metal claim 1 , comprising the step of treating the surface of the metal by using the hydrophilic metal surface treatment agent according to .8. The method according to claim 7 , wherein the surface of the metal is treated by immersing the metal in the hydrophilic metal surface treatment agent in liquid form claim 7 , applying the hydrophilic metal surface treatment agent to the surface of the metal claim 7 , or spraying the hydrophilic metal surface treatment agent on the surface of the ...

Подробнее
Номер записи: 69
10-08-2017 дата публикации

METHOD FOR PRODUCING 2-AMINO-SUBSTITUTED BENZALDEHYDE COMPOUND

Номер: US20170226046A1
Автор: Kobayashi Shinichi
Принадлежит: NIPPON SODA CO., LTD.

The present invention provides a method for producing a benzaldehyde in which an amino group is bonded in the 2 position, a halogeno group or an alkoxy group is bonded in the 3 position, and a hydrogen atom, an alkyl group, a halogeno group, an alkoxy group, or a cyano group is bonded independently in each of the 4, 5, and 6 positions, the method including: preparing a benzaldehyde in which a halogeno group or an alkoxy group is bonded in the 3 position, a hydrogen atom is bonded in the 2 position, and a hydrogen atom, an alkyl group, a halogeno group, an alkoxy group, or a cyano group is bonded independently in each of the 4, 5, and 6 positions so that a lithiation reaction is most active at the 2 position; acetal-protecting a formyl group in the benzaldehyde; sequentially performing lithiation, azidation, and amination of the 2 position; and the performing acetal deportection. 1. A method for producing a benzaldehyde in which an amino group is bonded in a 2 position , a halogeno group or an alkoxy group is bonded in a 3 position , and a hydrogen atom , an alkyl group , a halogeno group , an alkoxy group , or a cyano group is bonded independently in each of 4 , 5 , and 6 positions , the method comprising:preparing a benzaldehyde in which the halogeno group or the alkoxy group is bonded in the 3 position, a hydrogen atom is bonded in the 2 position, and the hydrogen atom, the alkyl group, the halogeno group, the alkoxy group, or the cyano group is bonded independently in each of the 4, 5, and 6 positions so that a lithiation reaction is most active at the 2 position (hereinafter, abbreviated as 2-unsubstituted benzaldehyde (I-1));acetal-protecting a formyl group in the 2-unsubstituted benzaldehyde (I-1);sequentially performing lithiation, azidation, and amination of the 2 position; andsubsequently performing acetal deportection.2. A method for producing a benzaldehyde in which an amino group is bonded in a 2 position , a halogeno group or an alkoxy group is bonded ...

Подробнее
Номер записи: 70
18-08-2016 дата публикации

METHOD OF GENERATING LINKAGE-SPECIFIC DI-AND POLYPROTEIN PROBES

Номер: US20160237471A1
Автор: LI Guorui, ZHUANG Zhihao
Принадлежит: Universtiy of Delaware

Deubiquitinating enzyme (DUB) probes are provided that resemble native diubiquitin (diUB) with a similar linkage size and that may contain a Michael acceptor for trapping the DUB active-site cysteine. For example, both K63- and K48-linked diubiquitin probes are generated using a facile chemical ligation method, utilizing the linker compound 3-(2-(bromomethyl)-1,3-dioxolan-2-yl)prop-2-en-1-amine. The diUb probes are capable of labelling DUBs from different families and may be employed to reveal intrinsic linkage specificities of DUBs. 2. The compound of claim 1 , wherein R is —CH═CH— claim 1 , n=2 claim 1 , and X is Br.3. The compound of claim 1 , wherein R is —CHCH— claim 1 , n=2 claim 1 , and X is Br.6. A di- or polyprotein comprising a first polypeptide moiety covalently bonded to a second polypeptide moiety through a linkage having a structure corresponding to —[C(═O)NHCHC(═O)NHCH—R—C(═O)CHSCH]— claim 1 , wherein R is —CHCH— or —CH═CH—.7. The di- or polyprotein of claim 6 , wherein the first polypeptide moiety is a first ubiquitin moiety and the second polypeptide moiety is a second ubiquitin moiety.8. The di- or polyprotein of claim 7 , wherein the linkage links a C-terminus of the first ubiquitin moiety with position 6 claim 7 , 11 claim 7 , 27 claim 7 , 29 claim 7 , 33 claim 7 , 48 or 63 of the second ubiquitin moiety.9. The di- or polyprotein of claim 6 , wherein the linkage links position 75 of the first ubiquitin moiety with position 6 claim 6 , 11 claim 6 , 27 claim 6 , 29 claim 6 , 33 claim 6 , 48 or 63 of the second ubiquitin moiety.10. The di- or polyprotein of claim 7 , wherein the first ubiquitin moiety is a Ubmoiety.11. The di- or polyprotein of claim 7 , wherein the second ubiquitin moiety bears a reporter tag.12. The di- or polyprotein of claim 11 , wherein the reporter tag is selected from the group consisting of affinity tags claim 11 , biotin and fluorophores.13. The di- or polyprotein of claim 11 , wherein the reporter tag is an affinity tag ...

Подробнее
Номер записи: 71
25-08-2016 дата публикации

METHOD FOR PREPARING GLYCIDOL USING GLYCEROL AND GLYCIDOL OBTAINED THEREBY

Номер: US20160244419A1
Автор: AHN Byoung Sung, CHOI Ji Sik, Lee Hye Jin, Lee Hyejeong, Lee Hyun Joo, Lee Sang Deuk
Принадлежит:

A method for preparing glycidol using glycerol includes mixing glycerol with urea in the presence of at least one zinc-based catalyst selected from the group consisting of Zn(NO), ZnCl, ZnO and Zn(OAc)under a pressure of 0.5-10 kPa at a temperature of 100-170° C. to obtain glycerol carbonate; filtering the glycerol carbonate mixed with the zinc-based catalyst through an adsorbent including a polymer resin coordinated with amine groups to separate the zinc-based catalyst and glycerol carbonate from each other; and carrying out reaction of the glycerol carbonate separated from the zinc-based catalyst in the presence of an anion alkali metal salt catalyst that is Na, K, Rb, Cs or a mixture thereof containing at least one anion selected from the group consisting of Cl, Br, I, NO, NO and acetate under a pressure of 0.13-6.67 kPa at a temperature of 140-250° C. to obtain glycidol. 1. A method for preparing glycidol , comprising the steps of:(A) mixing glycerol with urea in the presence of a zinc-based catalyst to obtain glycerol carbonate;(B) filtering the glycerol carbonate mixed with the zinc-based catalyst through an adsorbent including a polymer resin coordinated with amine groups to separate the zinc-based catalyst and glycerol carbonate from each other; and(C) carrying out reaction of the glycerol carbonate separated from the zinc-based catalyst in the presence of an anion alkali metal salt catalyst to obtain glycidol.2. The method for preparing glycidol according to claim 1 , wherein the amine group in step (B) is selected from the group consisting of ethylenediamine claim 1 , diethylenetriamine and triethylenetetramine.3. The method for preparing glycidol according to claim 1 , wherein the polymer resin in step (B) is Merrifield resin or Wang resin.4. The method for preparing glycidol according to claim 1 , wherein the adsorbent in step (B) comprises amine groups present in the polymer resin at a concentration of 1.5-4 mmol/g.5. The method for preparing glycidol ...

Подробнее
Номер записи: 72
23-08-2018 дата публикации

NATURAL PRODUCT ANALOGS INCLUDING AN ANTI-INFLAMMATORY CYANOENONE PHARMACORE AND METHODS OF USE

Номер: US20180237383A1
Автор: "OBRIEN Patrick M.", Anderson Eric, BOLTON Gary L., FERGUSON Deborah A., Jiang Xin, JR. Robert M., KRAL, Visnick Melean
Принадлежит: REATA PHARMACEUTICALS, INC.

This invention provides novel compounds comprising the following anti-inflammatory pharmacore: 2. The compound of claim 1 , wherein Rand Rare each independently hydrogen claim 1 , alkylor substituted alkyl.36-. (canceled)8. The compound of claim 7 , wherein Rand Rare each independently hydrogen claim 7 , alkylor substituted alkyl.915-. (canceled)16. The compound of claim 7 , wherein X is —CN.1718-. (canceled)20173-. (canceled)174. A method of making a compound of claim 1 , comprising:(a) obtaining an organic compound having two to eight five and/or six-membered rings, provided that the organic compounds is not argentatin, betulinic acid, lanostane, oleanic acid, boswellic acid, glycyrrhetinic acid, ursolic acid, or tricyclic-bis-enone;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) reacting the organic compound in a series of one of more steps to obtain a compound according to .'}175. The method of claim 174 , wherein the compound's induction of Nrf2 activity is at least ten times higher than the organic compound's induction of Nrf2 activity.176. The method of claim 174 , wherein the compound's inhibition of NF-κB activity is at least ten times higher than the organic compound's inhibition of NF-κB activity.177. The method of claim 174 , wherein the compound's inhibition of IFNγ induced NO activity is at least ten times higher than the organic compound's inhibition of IFNγ induced NO activity. The present application is a continuation application of U.S. patent application Ser. No. 14/950,557, filed Nov. 24, 2015, now U.S. Pat. No. 9,796,668, which is a divisional application of U.S. patent application Ser. No. 13/552,530, filed Jul. 18, 2012, now U.S. Pat. No. 9,233,998, which is a continuation application of U.S. patent application Ser. No. 12/426,889, filed Apr. 20, 2009, now U.S. Pat. No. 8,258,329, which claims the benefit of priority to U.S. Provisional Application No. 61/046,363, filed Apr. 18, 2008, the entire contents of each of which are ...

Подробнее
Номер записи: 73
10-09-2015 дата публикации

CLEANING, SURFACTANT, AND PERSONAL CARE COMPOSITIONS

Номер: US20150252302A1
Автор: Majeti Satyanarayana, Molitor Erich J., RIETH Lee R.
Принадлежит: SEGETIS, INC.

A cleaning or personal care composition containing at least one of 1,4-pentanediol and a ketal alcohol of formula (1) wherein Ris hydrogen or C1-3 alkyl, each R, R, and Ris independently hydrogen or C1-6 alkyl, Rand Rare each independently hydrogen or C1-6 alkyl, a=0-3, and b=0-1. Ris hydrogen or C1-3 alkyl, each R, R, and Ris independently hydrogen or C1-6 alkyl, each Rand Ris independently hydrogen, C1-6 alkyl optionally substituted with at least one hydroxyl groups, a=1-6, and b=0-2. 2. The composition of claim 1 , wherein Ris methyl claim 1 , R claim 1 , R claim 1 , and Rare each independently hydrogen or C1-3 alkyl claim 1 , Ris hydrogen claim 1 , C1-3 alkyl claim 1 , or —CHOH claim 1 , Ris hydrogen claim 1 , a=1-4 claim 1 , and b=0-1.3. The composition of claim 1 , wherein Ris methyl claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , C1-3 alkyl claim 1 , or —CHOH claim 1 , Ris hydrogen claim 1 , a=2-3 claim 1 , and b=0.4. The composition of claim 1 , wherein Ris methyl claim 1 , Ris hydrogen claim 1 , Ris hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , or —CHOH claim 1 , Ris hydrogen claim 1 , a=3 claim 1 , and b=0.6. The composition of claim 1 , wherein the composition is a cleaning composition claim 1 , and the cleaning component is a cosolvent claim 1 , a plurality of abrasive particles claim 1 , an organic amine claim 1 , an antioxidant claim 1 , a biocide claim 1 , a colorant claim 1 , a corrosion inhibitor claim 1 , a defoamer claim 1 , a dye claim 1 , an enzyme claim 1 , a light stabilizer claim 1 , an odor masking agent claim 1 , a plasticizer claim 1 , a preservative claim 1 , a rust inhibitor claim 1 , a surfactant claim 1 , a thickener claim 1 , a soil suspending agent claim 1 , a builder claim 1 , a chelating agent claim 1 , a bleach claim 1 , a bleach activator claim 1 , a bleach stabilizer claim 1 , a pH control agent claim 1 , a hydrotrope claim 1 , a fabric softener claim 1 , or a combination comprising at least one of the foregoing.7. ...

Подробнее
Номер записи: 74
01-09-2016 дата публикации

SYNTHESIS OF 1-ALKYL-2-AMINO-IMIDAZOL-5-CARBOXYLIC ACID ESTER VIA CALPHA-SUBSTITUTED N-ALKYL-GLYCINE ESTER DERIVATIVES

Номер: US20160251387A1
Автор: BREUNING Marcel Andre, DEBOR Michaela, HAHN Helmut Dieter, Jasper Christian, KRATTIGER Philipp
Принадлежит:

The invention provides an efficient and high yielding process for preparing TH-302, comprising at least one step wherein a dioxolane intermediate is generated in an aqueous layer, resulting in a synthesis that is amenable to scale up conditions. 4. The method of claim 1 , wherein each Ris independently Caliphatic claim 1 , which is optionally substituted.5. The method of claim 4 , wherein each Ris independently methyl or ethyl.6. The method of claim 1 , wherein each Ris independently Caliphatic claim 1 , which is optionally substituted.7. The method of claim 6 , wherein each Ris independently methyl or ethyl.8. The method of claim 1 , wherein III is produced by converting II to III claim 1 , or enolate thereof claim 1 , comprising the step of adding a base claim 1 , a formyl source claim 1 , and one or more solvents.9. The method of claim 8 , wherein the base is a metal hydroxide or an organic salt.10. The method of claim 9 , wherein the base is KOtBu.11. The method of claim 8 , wherein the one or more solvents are THF claim 8 , Methyl-THF claim 8 , toluene claim 8 , xylene claim 8 , ether claim 8 , MTBE claim 8 , cumene claim 8 , aliphatic hydrocarbons or methylene chloride.12. The method of claim 1 , wherein the conversion of III claim 1 , or enolate thereof claim 1 , to V comprises an aqueous extraction of III in the presence of claim 1 , or followed by addition of a water soluble diol claim 1 , wherein V is in an aqueous layer.13. The method of claim 12 , wherein the diol is ethylene glycol.14. The method of claim 12 , further comprising the addition of a water soluble acid.15. The method of claim 14 , wherein the acid is HCl.16. The method of claim 1 , wherein the conversion of V to IV comprises a base and NC—NH.17. The method of claim 16 , wherein the base is NaOAc. Phosphoramidate based alkylators used in cancer therapy, such as Cyclophosphamide and Ifosfamide, are an important subclass of chemotherapeutic alkylators. Cyclophosphamide and Ifosfamide are each ...

Подробнее
Номер записи: 75
15-08-2019 дата публикации

PHOTOINITIATORS WITH PROTECTED CARBONYL GROUP

Номер: US20190248757A1
Автор: Abuelyaman Ahmed S., Chou Shih-Hung, Gong Tao, Homnick Paul J., Mahoney Wayne S., Oxman Joel D., Volp Kelly A.
Принадлежит:

Disclosed are of the protected photoinitiators of the formula: wherein Aryl1 is an aromatic or heteroaromatic ring; Aryl2 is an aromatic ring; each Ris an alkyl, an aryl, an electron donating group or an electron withdrawing group, and subscript a is 0 to 3; each Ris an alkyl, an aryl, an electron donating group or an electron withdrawing group, and subscript b is 0 to 3; Prot is a protected carbonyl group. 3. The protected photoinitiator_of wherein Arylis selected from phenyl and napthyl.4. The protected photoinitiator of wherein Prot is a cyclic or acyclic ketal.5. The protected photoinitiator of wherein Prot is selected from thioketals claim 1 , dithioketals claim 1 , O-substituted cyanohydrins claim 1 , substituted hydrazones claim 1 , oxazolidines claim 1 , imidazolidines and thiazolidines protecting groups.6. The protected photoinitiator of having at least one electron-donating Ror Rgroups.7. The protected photoinitiator of having at least one electron-withdrawing Ror Rgroups.8. A polymerizable composition comprising at least one free-radically polymerizable monomer claim 1 , and the protected photoinitiator of .9. The polymerizable composition of wherein the monomer is a (meth)acrylate monomer.10. The polymerizable composition of wherein the monomer is a multifunctional (meth)acrylate monomer.11. The polymerizable composition of comprisingi. up to 100 parts by weight, preferably 85 to 99.5 parts by weight of an (meth)acrylic acid ester;ii. 0 to 15 parts by weight, preferably 0.5 to 15 parts by weight of an acid functional ethylenically unsaturated monomer;iii. 0 to 15 parts by weight of a non-acid functional, ethylenically unsaturated polar monomer;iv. 0 to 5 parts by weight vinyl monomer;v. 0 to 100 parts by weight of a multifunctional (meth)acrylate, preferably 50 to 100 parts by weight, relative to i-iv, wherein the sum of I. to Vii is 100%.12. The polymerizable composition of comprising a reactive oligomer having pendent polymerizable groups comprising:a) ...

Подробнее
Номер записи: 76
01-10-2015 дата публикации

PROCESS FOR PREPARATION OF ROFLUMILAST

Номер: US20150274667A1
Автор: Chen Yi-Jing, Chu Guo-dong, Kuo Shen-Chun, Pikul Stanislaw
Принадлежит:

The present invention provides novel processes for the preparation of N-substituted benzamides having the formula VIc: 2. The compound of claim 1 , wherein Rand Rare independently selected from the group consisting of Ccycloalkylmethyl and Calkyl which is partially or completely substituted with fluorine.5. The compound of claim 4 , wherein{'sup': 1', '2, 'sub': 1-6', '3-7', '1-4, 'Rand Rare independently selected from the group consisting of Calkyl; Ccycloalkylmethyl; and Calkyl which is partially or completely substituted with fluorine; and'}{'sup': 4', '5, 'sub': '1-6', 'Rand Rare independently selected from the group consisting of Calkyl groups.'} This application claims priority from International application Serial Number PCT/CN2012/072020, filed on Mar. 7, 2012, the entire content of which is hereby incorporated by reference.Not ApplicableNot ApplicablePhosphodiesterases (PDEs) are a family of enzymes that metabolize 3′,5′ cyclic nucleotides to 5′ nucleoside monophosphates, thereby regulating the activity of second messengers such as cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Phosphodiesterase type 4 (PDE4), which is a subfamily of cAMP-specific PDE, has generated interest as a target for the development of novel anti-asthmatic and anti-inflammatory compounds. PDE4 is known to exist in at least four isoforms, each of which is encoded by a distinct gene. Each of the four known PDE4 gene products is believed to play varying roles in over forty allergic and/or inflammatory responses. Inhibition of PDE4, and in particular the inhibition of specific isoforms that produce detrimental responses, can beneficially affect allergy and inflammation symptoms. Practical and economical methods providing novel PDE4 inhibitors are therefore highly desirable.Roflumilast (CAS 162401-32-3) is a member of a class of fluoroalkoxy-substituted benzamides developed by BYK Gulden Lomberg Chemische Fabrik GmbH (see, for example, U.S. Pat. No. 5,712 ...

Подробнее
Номер записи: 77
22-09-2016 дата публикации

ANTHROPOD REPELLENT CHEMICALS

Номер: US20160272612A1
Автор: BOYLE Sean Michael, KRAUSE PHAM Christine, RAY Anandasankar
Принадлежит: The Regents of the University of California

Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof. 2. The composition of claim 1 , wherein the compounds are selected from the group consisting of 4-methylcyclohexene claim 1 , ethyl cyclopentenolone claim 1 , 3 claim 1 ,4-Dihydro-2H-pyran claim 1 , and lemon hexadiene.3. The composition of claim 1 , wherein the alkyl is a C-Calkyl claim 1 , the alkenyl is a C-Calkenyl claim 1 , the alkoxy is a C-Calkoxy claim 1 , the aldehyde group is a C-Caldehyde group claim 1 , the ester group a C-Cester group claim 1 , or any combination thereof.5. The composition claim 1 , wherein the arthropod repellant compounds are selected from the group consisting of 1 claim 1 ,2-epoxyhexane claim 1 , 1-methyl-1 claim 1 ,4-cyclohexadiene claim 1 , 1-ethyl-2-pyrrolidone claim 1 , 2-isobutyl-4-methyl-1 claim 1 ,3-dioxolane claim 1 , 2-methyl tetrahydrofuran claim 1 , 3 claim 1 ,4-Dihydro-2H-pyran claim 1 , 4-hydroxy-2 claim 1 ,5-dimethyl-3(2H)-furanone claim 1 , 4-methyl cyclohexene claim 1 , dihydropyran claim 1 , ethyl cyclopentenolone claim 1 , isopropyl quinoline claim 1 , methyl 2-(4-tert-butylphenyl)acetate and nerol oxide.6. The composition claim 1 , comprising two or more of the arthropod repellant compounds ...

Подробнее
Номер записи: 78
29-08-2019 дата публикации

ACID LABILE SURFACTANTS

Номер: US20190263774A1
Автор: Brousmiche Darryl W.
Принадлежит:

This invention relates to an acid labile surfactant. In particular, the surfactants of the present invention include a dioxolane or dioxane functional group which enables the surfactant to hydrolyze in an acidic environment. Surfactants of this type can be utilized to enhance protein solubilization/enzyme digestion. Following hydrolysis to destroy the surfactant (which may chromatographic issues), there are generally two components formed—a hydrophilic one, and a hydrophobic one. By altering the chemistry of the hydrolysable linker, the polarity of the hydrophobic residue can be altered, allowing it to be solubilized by significantly less organic solvent, and to minimize the potential loss of peptide material and to expand the chromatographic conditions that can be utilized. 2. The method of claim 1 , wherein Ris selected from a group consisting of —RSO claim 1 , —RORSO claim 1 , —R(OCHCH)SO claim 1 , —RCOO claim 1 , —RORCOO claim 1 , —RCONCHCHCOO claim 1 , —R(OCHCH)OP(OH)O claim 1 , —ROP(OH)O claim 1 , —ROP(OH)O claim 1 , —RORP(OH)O claim 1 , —ROROP(OH)O claim 1 , —RN(CH) claim 1 , —RN(R) claim 1 , —RORN(R) claim 1 , —RN(CH)CHCOO claim 1 , —RN(CH)RSO; wherein R claim 1 , R claim 1 , and Rare each claim 1 , independently claim 1 , lower alkyl claim 1 , lower alkenyl claim 1 , lower alkynyl claim 1 , substituted lower alkyl claim 1 , substituted lower alkenyl claim 1 , or substituted lower alkynyl; n is 1 to 6.3. The method of claim 1 , wherein Ris selected from a group consisting of —RSO claim 1 , —RORSO claim 1 , —R(OCHCH)SO.4. The method of comprising the further step of degrading the surfactant after protein solubilization or enzyme digestion.5. The method of wherein the step of degrading the surfactant after protein solubilization or enzyme digestion comprises contacting the surfactant with an acidic solution.6. The method of comprising the further step of purifying the sample.8. The method of claim 7 , wherein Ris selected from a group consisting of —RSO claim ...

Подробнее
Номер записи: 79
27-09-2018 дата публикации

Nucleator composition comprising sorbitol acetal, sorbitol diacetal and sorbitol triacetal

Номер: US20180273545A1
Автор: Wenlin Zhao
Принадлежит: GCH Technology Co Ltd

The present invention provides a nucleator composition comprising sorbitol acetal, sorbitol diacetal, and sorbitol triacetal. The nucleator composition can improve the nucleation performance of a polymer, increase transparency, glossiness, flexural modulus and tensile strength of polymer films, polymer sheets and polymer moulding articles, and increase heat distortion temperature and dimensional stability of polymer articles.

Подробнее
Номер записи: 80
20-08-2020 дата публикации

CLEAVABLE SURFACTANTS

Номер: US20200263110A1
Автор: Hitko Carolyn Woodroofe, Klaubert Dieter, Saveliev Sergei, Simpson Daniel, Uyeda Harry Tetsuo, Wood Keith V.
Принадлежит:

The invention provides surfactant compounds of formulas I-IX, which can be used in methods for aiding the solubilization, digestion, preparation, analysis, and/or characterization of biological material, for example, proteins or cell membranes. The compounds can also aid in the recovery of peptides generated during protein digestion, particularly for in-gel digestion protocol. Additionally, the compounds can improve enzymatic protein deglycosylation without interfering with downstream sample preparation steps and mass spectrometric analysis. The compounds can be specifically useful as digestion aids that can be decomposed by an acid, by heat, or a combination thereof. Decomposition of the surfactants allows for facile separation from isolated samples, and/or allows for analysis of the sample without interfering with the sensitivity of various analytical techniques. 131-. (canceled)33. The compound of claim 32 , wherein Q is (C-C)alkyl.34. The compound of claim 33 , wherein Q is optionally substituted with hydroxy.35. The compound of claim 32 , wherein X is NH claim 32 , and Z is O.36. The compound of claim 32 , wherein M is H or Na.37. The compound of claim 32 , wherein L is a direct bond.38. The compound of claim 32 , wherein Ris (C-C)alkyl.39. The compound of claim 32 , wherein Ris (C-C)alkyl.40. The compound of claim 32 , wherein Rand Rare each (C-C)alkyl.41. The compound of claim 32 , wherein Rand Rare each methyl.42. The compound of claim 32 , wherein:{'sub': 2', '3, 'Q is (C-C)alkyl, which is unsubstituted or substituted with hydroxy;'}X is NH, and Z is O;M is H or Na;L is a direct bond;{'sup': '1', 'sub': 4', '20, 'Ris unsubstituted (C-C)alkyl; and'}{'sup': 2', '3, 'sub': 1', '6, 'Rand Rare each unsubstituted (C-C)alkyl.'}43. The compound of claim 42 , wherein:{'sup': '1', 'sub': 10', '14, 'Ris unsubstituted (C-C)alkyl; and'}{'sup': 2', '3, 'Rand Rare each methyl.'}461. A composition comprising a gel and a compound of claim .47. The composition of claim 46 , ...

Подробнее
Номер записи: 81
15-10-2015 дата публикации

METHOD OF PREPARATION OF ALPHA GALACTOSYL CERAMIDES COMPOUNDS

Номер: US20150291646A1
Автор: SERRA Vincent
Принадлежит: ABIVAX

The present invention relates to a method of preparation of α-galactosyl ceramides compounds of formula (I): 2. Method according to , wherein the compound of formula (I) is obtained from the compound of formula (IV) via deprotection of protecting groups PG , PG , PGand PG′ , and coupling with a compound of formula RCOCl (VII) , wherein Ris as defined in .6. Method according to claim 5 , comprising after step b′) a step c′) of coupling of the compound of formula (VI) with a compound of formula RCOCl (VII) claim 5 , in the presence of a base claim 5 ,said step c′) providing a compound of formula (I).7. Method according to claim 1 , wherein LG is a trichloroacetimidate group.8. Method according to claim 1 , wherein Ris a linear saturated C-Calkyl group.9. Method according to claim 1 , wherein Ris a linear saturated C-Calkyl group.10. Method according to claim 1 , wherein:{'sub': 3', '3, 'Ris an acyl group, preferably of formula —C(O)CH; and'}{'sub': '4', 'Ris H.'}11. Method according to claim 1 , wherein protecting group PGis a benzyl group.12. Method according to claim 1 , wherein protecting group PGis a carboxybenzyl group.13. Method according to claim 1 , wherein the protecting groups PGand PG′form together with the two oxygen atoms to which they are connected claim 1 , an isopropylidene acetal group. The present invention relates to a method of preparation of a class of 6″-deoxy-6-amino α-galactosyl ceramides.The interests lying in α-galactosyl ceramides compounds (also called α-GCs compounds) are well explained in WO 2007/118234, inter alia. α-GCs compounds have been found to effectively stimulate natural killer T (NKT) cells, both in vitro and in vivo. NKT cells have been implicated in suppression of autoimmunity and graft rejection, promotion of resistance to pathogens, and promotion of tumor immunity.A natural glycolipid molecule, termed KRN7000, is known to stimulate NKT cells when loaded into CD1d tetramers. However, supplies of KRN7000, which is derived from ...

Подробнее
Номер записи: 82
06-10-2016 дата публикации

DEGRADABLE ISOCYANATE COMPOUNDS AND APPLICATIONS THEREOF

Номер: US20160289412A1
Автор: Li Xin, Liang Bo, Qin Bing
Принадлежит: ADESSO ADVANCED MATERIALS WUXI CO., LTD.

Degradable isocyanate compounds, methods for making these compounds, and uses of these compounds for preparing degradable cross-linked polymers and composite materials are provided. 1. An isocyanate compound having at least two isocyanate groups , wherein each of the isocyanate groups is bonded via a linker to a linear or cyclic oxy-carbohydro moiety that contains oxygen atoms not less than the isocyanate groups and optionally contains one or more heteroatoms each independently being S or N; each of the linker is alkylene , heteroalkylene , alkenylene , heteroalkyl , alkynylene , heteroalkynlene , arylene , or heteroaryl; the linear oxy-carbohydro moiety is alkyl , alkenyl , or alkynyl optionally substituted in the main chain with one or more heteroatoms , and is connected via oxo to each of the linkers that link the isocyanate groups to the oxy-carbohydro moiety; and the cyclic oxy-carbohydro is saturated , unsaturated , or aromatic ring or fused ring containing at least one oxygen atom in the ring and optionally contain an oxygen in a ring substituent that is bonded to the linker with a isocyanate group.3. The isocyanate of claim 2 , wherein m is 1; each of R claim 2 , R claim 2 , Rand Ris independently hydrogen or alkyl; or each A and B independently is alkylene or alkenylene.5. The isocyanate compound of claim 4 , wherein each of Rand Rindependently is hydrogen or alkyl; or claim 4 , Rand R claim 4 , together with the carbon atom to which they are bonded claim 4 , form a 3-6 membered ring optionally containing one or more heteroatoms each of which is independently S claim 4 , O claim 4 , or N; n is 1; or each of Rand Rindependently is alkylene claim 4 , alkylene-hetero-alkylene claim 4 , or alkenylene.6. The isocyanate compound of claim 1 , wherein the isocyante compound is of Formula (III):{'br': None, 'sub': 9', 'p', '10', 'q, '(R)R(—O—R—N═C═O)\u2003\u2003 (III)'} [{'sub': '10', 'R and the oxygen atoms (each between R and R) together constitute the linear or ...

Подробнее
Номер записи: 83
05-10-2017 дата публикации

Poly(ADP-Ribose) Polymerase 1 Inhibitors Structurally Unrelated to NAD

Номер: US20170283402A1
Автор: Tulin Alexei
Принадлежит:

Compounds that are not related to NAD, and which target PARP1-histone H4 interaction are provided, as well as compositions of these compounds, and methods for specific inhibition of poly(ADP-ribose) polymerase 1 (PARP-1) using these compounds are provided. These PARP-1 inhibitors may be used to treat cancer in which PARP-1 activation or biologic activity plays a role, including prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma, among others. 3. The compound of claim 2 , wherein the R1 comprises —(CH)—.4. (canceled)67-. (canceled)8. The compound of claim 2 , wherein the R1 comprises —(CH)O(CH)—.10. The compound of claim 2 , wherein the R1 comprises —(CH)—.13. The compound of claim 12 , wherein R1 comprises —(CH)—.1518-. (canceled)19. The compound of claim 12 , wherein R1 comprises —(CH)O(CH)—.21. (canceled)22. The compound of claim 12 , wherein R1 comprises —(CH)—.24. (canceled)26. (canceled)27. A composition claim 1 , comprising the compound of and a carrier.28. The composition of claim 27 , wherein the carrier is a pharmaceutically acceptable carrier.3054-. (canceled)5667-. (canceled)69. (canceled)70. The method of wherein:the cancer patient is a prostate cancer patient and the cancer is prostate cancer;the cancer patient is a breast cancer patient and the cancer is breast cancer;the cancer patient is a kidney cancer patient and the cancer is kidney cancer;the cancer patient is an ovarian cancer patient and the cancer is ovarian cancer;the cancer patient is a glioblastoma patient and the cancer is glioblastoma;the cancer patient is a lymphoma patient and the cancer is lymphoma; orthe cancer patient is a leukemia patient and the cancer is leukemia.7194-. (canceled) This application claims priority to U.S. Provisional Application No. 62/059,201, which was filed on Oct. 3, 2014, the contents of which are incorporated by reference herein, in their entirety and for all purposes.The inventions described herein were made, ...

Подробнее
Номер записи: 84
12-09-2019 дата публикации

Cyclic Ketals As Fragrance Precursor Compounds

Номер: US20190276469A1
Автор: SAUF Silvia, Schaefer Sascha
Принадлежит: Henkel AG & Co. KGaa

The invention is directed to the field of pro-fragrances used in detergents and cleaning agents, cosmetic agents and air fresheners, for example. The invention relates to particular cyclic ketals used as pro-fragrances. The invention also relates to detergents and cleaning agents, cosmetic agents and air fresheners containing ketals of the type. The invention further relates to a method for creating a long-lasting fragrance on surfaces and for repelling insects. 2. The compound according to claim 1 , characterized in that R claim 1 , Rand Rare hydrogen and Ris a substituted alkyl or heteroalkyl functional group having 2 to 6 carbon atoms and optionally one or more oxygen atoms.4. The compound according to claim 3 , characterized in that{'sub': 1', '2', '4', '1', '2', '4, '(1) R, R, R, R′, R′ and R′ are hydrogen; and/or'}(2) all instances of n equal 0 or 1.6. The compound according to claim 1 , characterized in that Ra and Rb and the C atom to which they are bonded and/or Ra′ claim 1 , Rb′ and the C atom to which they are bonded are together a functional group derived from a fragrance ketone claim 1 , the fragrance ketone being selected from the group consisting of Buccoxime; isojasmone; methyl beta-naphthyl ketone; musk indanone; tonalide/Musk Plus; alpha-damascone; beta-damascone; delta-damascone; gamma-damascone; damascenone; damask rose; methyl dihydrojasmonate (hedione); menthone; carvone; camphor; fenchone; alpha-ionone; beta-ionone; gamma-methylionone; fleuramone; dihydrojasmone; cis-jasmone; Iso E Super (1-(1 claim 1 ,2 claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6 claim 1 ,7 claim 1 ,8-octahydro-2 claim 1 ,3 claim 1 ,8 claim 1 ,8 claim 1 ,-tetramethyl-2-naphthyl)ethan-1-one); methyl cedrenyl ketone; methyl cedrylone; acetophenone; methylacetophenone; para-methoxyacetophenone; methyl beta-naphthyl ketone; benzylacetone; benzophenone; para-hydroxyphenylbutanone; celery ketone or livescone; 6-isopropyldecahydro-2-naphtone; dimethyl octenone; frescomenthe; 4-(1- ...

Подробнее
Номер записи: 85
11-10-2018 дата публикации

Process For Preparing Aminotetrahydropyrans

Номер: US20180290995A1
Автор: Maragni Paolo, Verzini Massimo
Принадлежит:

The present invention relates to a process for preparing 3-amino tetrahydropyrans and, more particularly, to an improved method for synthesizing a 2,3,5-substituted tetrahydropyran derivative, intermediate being used in the preparation of dipeptidyl peptidase-IV enzyme inhibitors (DPP-4 inhibitors). 2. The process according to claim 1 , wherein said basic species is selected from the group consisting of alkaline hydroxides claim 1 , alkaline alkoxides claim 1 , carbonates and tertiary amines.3. The process according to claim 1 , wherein said catalyst is an organometallic complex of Cu(II) or Cu(I) with a chiral ligand.4. The process according to claim 3 , wherein said chiral ligand is N-[(1S claim 3 ,2S claim 3 ,4S)-1 claim 3 ,7 claim 3 ,7-trimethylbicyclo[2.2.1]hept-2-yl]-2-Pyridinemethanamine (Ligand F) or 2 claim 3 ,4-di-tert-butyl-6-((E)-((R)-(6-methoxy-quinolin-4-yl)((2R claim 3 ,4S claim 3 ,8R)-8-vinyl-quinuclidin-2-yl)-methyl-imino)-methyl)-phenol (Ligand G).5. The process according to claim wherein step a is carried out in an organic solvent selected from the group consisting of methanol claim 3 , ethanol claim 3 , acetonitrile claim 3 , diethoxyethane claim 3 , 2 claim 3 ,2-dimethoxypropane claim 3 , 1 claim 3 ,2-dimethoxyethane claim 3 , dioxane claim 3 , THF and toluene.6. The process according to claim 1 , wherein step a is carried out at a temperature ranging from −20° C. to 20° C.8. The process according to claim 1 , wherein each of Rand Ris a methyl group claim 1 , or claim 1 , wherein Rand R claim 1 , when taken together claim 1 , form a cyclohexyl group.9. The process according to claim 1 , wherein Ar is 2 claim 1 ,5-difluorophenyl.11. The process according to claim 10 , wherein Z is a tosyl group and Z′ is a tetrahydropyranyl group.13. The process of claim 1 , wherein the compound of formula (I) is omarigliptin.15. A compound having formula:1-(2,5-difluorophenyl)-2-nitro-3-((S)-1,4-dioxaspiro[4.5]decan-2-yl)propan-1-ol (IV);1-(2,4,5-trifluorophenyl ...

Подробнее
Номер записи: 86
19-10-2017 дата публикации

METHODS OF SYNTHESIZING A PROSTACYCLIN ANALOG

Номер: US20170297995A1
Автор: Chambournier Gilles, Endres Gregory William, Fedij Victor, Hering Kirk William, II Thomas James, Krell, Mahmoud Hussein Mahmoud
Принадлежит: CAYMAM CHEMICAL COMPANY INCORPORATED

The present invention provides processes for preparing a prostacyclin analogue of Formula (I) or a pharmaceutically acceptable salt thereof, wherein Ris a linear or branched Calkyl. The processes of the present invention comprise steps that generate improved yields and fewer byproducts than traditional methods. The processes of the present invention employ reagents (e.g., the oxidizing reagent) that are less toxic that those used in the traditional methods (e.g., oxalyl chloride). Many of the processes of the present invention generate intermediates with improved e.e. and chemical purity; thereby eliminating the need of additional chromatography steps. And, the processes of the present invention are scalable to generate commercial quantities of the final compound. 1103.-. (canceled)105. The compound of claim 104 , wherein Ris methyl claim 104 , ethyl claim 104 , propyl claim 104 , iso-propyl claim 104 , butyl claim 104 , sec-butyl claim 104 , or tert-butyl.107. The compound of claim 104 , wherein Ris methyl and the —OSi(R)group is108117-. (canceled) This application is a divisional application of U.S. patent application Ser. No. 14/650,234, filed Jun. 5, 2015, which is a 35 U.S.C. §371 United States National Phase Application of PCT Application Serial No. PCT/US2013/073474, filed Dec. 6, 2013, which claims the benefit of and priority to U.S. provisional application Ser. Nos. 61/734,672, filed Dec. 7, 2012, and 61/777,882, filed Mar. 12, 2013. The entire contents of the aforementioned disclosures are incorporated herein by reference in their entirety.The present invention relates to processes and intermediates for the preparation of prostacyclin analog that are useful for treating hypertension and other diseases.Prostacyclin derivatives and analogs are useful pharmaceutical compounds possessing activities such as platelet aggregation inhibition, gastric secretion reduction, lesion inhibition, vasodilation, and bronchodilation.Treprostinil is a synthetic prostacyclin ...

Подробнее
Номер записи: 87
10-09-2020 дата публикации

HALOGENATED HETEROALKENYL- AND HETEROALKYL-FUNCTIONALIZED ORGANIC COMPOUNDS AND METHODS FOR PREPARING SUCH COMPOUNDS

Номер: US20200283351A1
Автор: Chen Benjamin bin, CLARKSON Lucy M., Liu Haiming, Miller Jay Fingeret, POLSZ Craig A., Syvret Robert G.
Принадлежит:

A method for synthesizing halogenated organic compounds, such as halogenated alkenyl group-containing and halogenated alkyl group-containing compounds having a heteroatom (e.g., O,N.S) coupled to a carbon atom of a halogenated alkenyl or halogenated alkyl group, involves reacting a halogenated olefin such as a chloro-substituted trifluoropropenyl compound with an active hydrogen-containing organic compound such as an alcohol (e.g., an aliphatic monoalcohol, aliphatic polyalcohol, or a phenolic compound), a primary amine, a secondary amine or a thiol. 1. A method of making a halogenated organic compound , comprising reacting an active hydrogen-containing organic compound selected from the group consisting of alcohols , primary amines , secondary amines and thiols with a halogenated olefin containing a carbon-carbon double bond , wherein at least one carbon of the carbon-carbon double bond is substituted with at least one substituent selected from the group consisting of halogens and halogenated alkyl groups , to produce the halogenated organic compound.2. The method of claim 1 , wherein the halogenated olefin contains one or more fluorine atoms.3. The method of claim 1 , wherein the halogenated organic compound is a halogenated heteroalkenyl-functionalized organic compound.4. The method of claim 1 , wherein the halogenated organic compound is a halogenated heteroalkyl-functionalized organic compound.5. The method of claim 1 , wherein the halogenated olefin has a fluorinated alkyl group substituted on one carbon of the carbon-carbon double bond.6. The method of claim 1 , wherein the halogenated olefin has a perfluorinated alkyl group substituted on one carbon of the carbon-carbon double bond.7. The method of claim 1 , wherein the halogenated olefin has a structure in accordance with formula (1):{'br': None, 'sup': 1', '2', '3', '4, 'CXX═CXX\u2003\u2003(1)'}{'sup': 1', '2', '3', '4', '1', '2', '3', '4, 'wherein X, X, Xand Xare independently selected from the group ...

Подробнее
Номер записи: 88
18-10-2018 дата публикации

LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS

Номер: US20180296677A1
Автор: Baryza Jeremy Lee, BECKWITH Rohan Eric John, Bowman Keith, BYERS Crystal, Fazal Tanzina, Gamber Gabriel Grant, Lee Cameron Chuck-Munn, TICHKULE Ritesh Bhanudasji, Vargeese Chandra, Wang Shuangxi, West Laura Ellen, ZABAWA Thomas, Zhao Junping
Принадлежит:

This invention provides for a compound of formula (I): 7. The method of claim 1 , wherein the composition comprises one or more of a helper lipid claim 1 , a neutral lipid claim 1 , and a stealth lipid.8. The method of claim 7 , wherein the helper lipid is cholesterol claim 7 , the neutral lipid is DSPC claim 7 , and the stealth lipid is PEG-DMG claim 7 , S010 claim 7 , or S011.9. The method of claim 3 , wherein the composition comprises one or more of a helper lipid claim 3 , a neutral lipid claim 3 , and a stealth lipid.10. The method of claim 9 , wherein the helper lipid is cholesterol claim 9 , the neutral lipid is DSPC claim 9 , and the stealth lipid is PEG-DMG claim 9 , S010 claim 9 , or S011.11. The method of claim 5 , wherein the composition comprises one or more of a helper lipid claim 5 , a neutral lipid claim 5 , and a stealth lipid.12. The method of claim 11 , wherein the helper lipid is cholesterol claim 11 , the neutral lipid is DSPC claim 11 , and the stealth lipid is PEG-DMG claim 11 , S010 claim 11 , or S011.13. The method of claim 1 , wherein the composition is in a form of a lipid nanoparticle.14. The method of claim 3 , wherein the composition is in a form of a lipid nanoparticle.15. The method of claim 5 , wherein the composition is in a form of a lipid nanoparticle.16. The method of claim 8 , wherein the stealth lipid is PEG-DMG.17. The method of claim 10 , wherein the stealth lipid is PEG-DMG.18. The method of claim 12 , wherein the stealth lipid is PEG-DMG.19. The method of claim 8 , wherein the lipid composition has a molar ratio of about 40/about 38/about 10/about 2 of the compound of formula (I)/cholesterol/DSPC/PEG-DMG claim 8 , S010 claim 8 , or S011 claim 8 , respectively.20. The method of claim 10 , wherein the lipid composition has a molar ratio of about 40/about 38/about 10/about 2 of the compound of (9Z claim 10 , 9′Z claim 10 , 12Z claim 10 , 12′Z)-((5-((dimethylamino)methyl)-1 claim 10 ,3-phenylene)bis(oxy))bis(butane-4 claim 10 , ...

Подробнее
Номер записи: 89
05-11-2015 дата публикации

NOVEL LOW MOLECULAR WEIGHT CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY

Номер: US20150315112A1
Автор: Budzik Brian W., Colletti Steven L., DAVIS Jennifer R., Hills Ivory D., SEIFRIED Darla Danile, Stanton Matthew G.
Принадлежит:

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA. 2. A cationic lipid of Formula A according to claim 1 ,wherein:{'sup': 1', '2, 'Rand Rare each methyl;'}{'sub': 1', '4', '22', '4', '22, 'Lis selected from C-Calkyl and C-Calkenyl; and'}{'sub': 2', '3', '13', '3', '13, 'Lis selected from C-Calkyl and C-Calkenyl;'}or any pharmaceutically acceptable salt or stereoisomer thereof.3. A cationic lipid which is selected from:R—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 2);S—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 1);1-{2-[(9412Z)-octadeca-9,12-dien-1-yloxy]-1-[(actyloxy)methyl]ethyl}pyrrolidine (Compound 3);(2S)—N,N-dimethyl-1-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-3-[(5Z)-oct-5-en-1-yloxy]propan-2-amine (Compound 4);1-{2-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]-1-[(octyloxy)methyl]ethyl}azetidine (Compound 5);(2S)-1-(hexyloxy)-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 6);(2S)-1-(heptyloxy)-N,N-dimethyl-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 7);N,N-dimethyl-1-(nonyloxy)-3-[(9Z,12Z)-octadeca-9,12-dien-1-yloxy]propan-2-amine (Compound 8);N,N-dimethyl-1-[(9Z)-octadec-9-en-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 9);(2 S)—N,N-dim ethyl-1-[(6Z,9Z,12Z)-octadeca-6,9,12-trien-1-yloxy]-3-(octyloxy)propan-2-amine (Compound 10);(2S)-1-[(11Z,14Z)-icosa-11,14-dien-1-yloxy]-N,N-dimethyl-3-(pentyloxy)propan-2-amine (Compound 11 ...

Подробнее
Номер записи: 90
17-09-2020 дата публикации

HYDROPHILIC POLYMER DERIVATIVE HAVING CYCLIC BENZYLIDENE ACETAL LINKER

Номер: US20200291178A1
Автор: TSUBUSAKI Takuma, Yamamoto Yuji
Принадлежит: NOF CORPORATION

A hydrophilic polymer derivative having a cyclic benzylidene acetal linker represented by the following formula (1):

Подробнее
Номер записи: 91
03-11-2016 дата публикации

Sulfamate Derivative Compounds for Use in Treating or Alleviating Pain

Номер: US20160318894A1
Автор: Choi Yong Moon
Принадлежит:

The present invention relates to sulfamate derivative compounds and a composition for treating and/or alleviating pain containing the sulfamate derivative compounds or a pharmaceutically acceptable salt thereof as an active ingredient. More specifically, the present invention relates to a pharmaceutical composition for treating or alleviating pain containing a sulfamate derivative compound and/or a pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or alleviation of pain comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or alleviation of pain; and a use of the sulfamate derivative compound or the pharmaceutically acceptable salt thereof in treating and/or alleviating pain, are provided. 2. The method according to claim 1 , Rand Rare each independently hydrogen or methyl.3. The method according to claim 1 , m and n are each independently an integer of 0-2.4. The method according to claim 1 , wherein the compound is selected from the group consisting of:(1) (5-(2-chlorophenyl)-2,2-dimethyl-1,3-dioxolan-4-yl)methylsulfamate;(2) (5-(2-chlorophenyl)-2-methyl-1,3-dioxolan-4-yl) methyl sulfamate;(3) (5-(2-chlorophenyl)-2,2-diethyl-1,3-dioxolan-4-yl)methyl sulfamate;(4) (3-(2-chlorophenyl)-1,4-dioxaspiro[4,4]nonan-2-yl)methyl sulfamate;(5) (3-(2-chlorophenyl)-1,4-dioxaspiro[4,5]decan-2-yl)methyl sulfamate;(6) (5-(2-chlorophenyl)-2-phenyl-1,3-dioxolan-4-yl)methyl sulfamate;(7) (5-(2-fluorophenyl)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl sulfamate;(8) (5-(2-fluorophenyl)-2-methyl-1,3-dioxolan-4-yl) methyl sulfamate;(9) (5-(2-fluorophenyl)-2,2-diethyl-1,3-dioxolan-4-yl)methyl sulfamate;(10) (3-(2-fluorophenyl)-1,4-dioxaspiro[4,4]nonan-2-yl)methyl sulfamate;(11) (3-(2-fluorophenyl)-1,4-dioxaspiro[4,5]decan-2-yl)methyl sulfamate;(12) (5-(2-fluorophenyl)-2-phenyl-1,3-dioxolan-4-yl)methyl sulfamate;(13) (5-(2-iodophenyl)-2 ...

Подробнее
Номер записи: 92
02-11-2017 дата публикации

AMYLOID BINDING AGENTS

Номер: US20170315137A1
Автор: Theodorakis Emmanuel A., Yang Jerry
Принадлежит:

There are provided compounds and methods for the detection of amyloids and treatment of diseases related to amyloids including Alzheimer's disease and other related amyloid-based neurodegenerative diseases. 116-. (canceled)19. The method of claim 17 , wherein x is an integer from 1 to 10.21. The method according to claim 20 , wherein Ris independently unsubstituted alkyl.23. The method of claim 17 , wherein said amyloid peptide is AP peptide claim 17 , prion claim 17 , protein claim 17 , α-synuclein claim 17 , or superoxide dismutase.24. The method of claim 23 , wherein said amyloid peptide forms part of an amyloid.28. The method of claim 26 , wherein Rand Rare optionally joined together to form an R-substituted or unsubstituted heterocycloalkyl.29. The method of claim 26 , wherein said R-substituted or unsubstituted heterocycloalkyl is substituted or unsubstituted piperidinyl.30. The method of claim 26 , wherein y is 2 and z is 0. This application is a divisional of U.S. patent application Ser. No. 14/572,465, filed Dec. 16, 2014, which is a continuation of U.S. patent application Ser. No. 13/515,239, filed Aug. 9, 2012, now U.S. Pat. No. 8,940,918, which is a National Stage Entry of International Patent Application No. PCT/US2010/059952, filed Dec. 10, 2010, which claims priority to U.S. Provisional Patent Application No. 61/285,470, filed Dec. 10, 2009, the disclosures of which are incorporated by reference herein in their entirety and for all purposes.This invention was made with government support under Grant No. 1E21RR025358 awarded by National Institutes of Health (NIH). The government has certain rights in the invention.Alzheimer's disease (AD) is characterized by a progressive loss of cognitive function and constitutes the most common and fatal neurodegenerative disorder. Genetic and clinical evidence supports the hypothesis that accumulation of amyloid deposits in the brain plays an important role in the pathology of the disease. This event is associated ...

Подробнее
Номер записи: 93
01-11-2018 дата публикации

Lipid derivative in which hydrophilic polymer is bound through cyclic benzylidene acetal linker

Номер: US20180312633A1
Автор: Masaki Ota, Takuma Tsubusaki, Yuji Yamamoto
Принадлежит: NOF Corp

A lipid derivative in which a hydrophilic polymer is bound through a cyclic benzylidene acetal linker, and which can accurately control a hydrolysis rate in the weakly acidic environment of a living body to detach the hydrophilic polymer from a lipid membrane structure. The lipid derivative is represented by formula (1): wherein, R 1 and R 6 are each independently a hydrogen atom or a hydrocarbon group; R 2 , R 3 , R 4 and R 5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; R 7 is a hydrocarbon group having from 8 to 24 carbon atoms, an acyl group having from 8 to 24 carbon atoms, a cholesterol derivative, a glycerolipid, a phospholipid or a sphingolipid; P is a hydrophilic polymer; s is 1 or 2, t is 0 or 1, and s+t is 1 or 2; and Z 1 and Z 2 are each independently a selected divalent spacer.

Подробнее
Номер записи: 94
10-10-2019 дата публикации

ANTIBODY-DRUG CONJUGATE HAVING CYCLIC BENZYLIDENE ACETAL LINKER

Номер: US20190309102A1
Автор: TSUBUSAKI Takuma, Yamamoto Yuji
Принадлежит: NOF CORPORATION

An antibody-drug conjugate having a cyclic benzylidene acetal linker represented by formula (1) or formula (2), wherein Y is an antibody; D is a drug; Rand Rare each independently a hydrogen atom or a hydrocarbon group; R, R, Rand Rare each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; s is 1 or 2, t is 0 or 1, and s+t is 1 or 2; w is an integer of 1 to 20; and Zand Zare each independently a selected divalent spacer: 2. The compound as claimed in claim 1 , wherein Xis selected from the group consisting of an active ester group claim 1 , an active carbonate group claim 1 , an aldehyde group claim 1 , an isocyanate group claim 1 , an isothiocyanate group claim 1 , an epoxy group claim 1 , a maleimide group claim 1 , a vinyl sulfone group claim 1 , an acryl group claim 1 , a sulfonyloxy group claim 1 , a carboxyl group claim 1 , a thiol group claim 1 , a dithiopyridyl group claim 1 , an α-haloacetyl group claim 1 , an alkynyl group claim 1 , an allyl group claim 1 , a vinyl group claim 1 , an amino group claim 1 , an oxyamino group claim 1 , a hydrazide group claim 1 , an azide group and a hydroxyl group.5. The compound as claimed in claim 4 , wherein Xis selected from the group consisting of an active ester group claim 4 , an active carbonate group claim 4 , an aldehyde group claim 4 , an isocyanate group claim 4 , an isothiocyanate group claim 4 , an epoxy group claim 4 , a maleimide group claim 4 , a vinyl sulfone group claim 4 , an acryl group claim 4 , a sulfonyloxy group claim 4 , a carboxy group claim 4 , a thiol group claim 4 , a dithiopyridyl group claim 4 , an α-haloacetyl group claim 4 , an alkynyl group claim 4 , an allyl group claim 4 , a vinyl group claim 4 , an amino group claim 4 , an oxyamino group claim 4 , a hydrazide group claim 4 , an azide group and a hydroxyl group.7. The compound as claimed in claim 1 , wherein Zand Zare each independently an ether group claim 1 , an ester group claim 1 , a carbonate ...

Подробнее
Номер записи: 95
17-11-2016 дата публикации

STABILIZED LEVULINIC ESTER KETALS

Номер: US20160332983A1
Автор: BADARINARAYANA Vivek, Hall Eric S., Leibig Cora M., MULLEN Brian D., Tjossas Matthew J.
Принадлежит:

The invention describes methods of preparation and compositions of plasticizers. The plasticizers include at least 2 alkyl ketal ester moieties and have a molecular weight of greater than 300. In one aspect, the alkyl ketal ester moieties are levulinic ester ketals. Certain compositions contain at least one of an antioxidant, a UV stabilizer, a thermal stabilizer or mixtures thereof, present in the composition from about 0.01 to about 5.0 percent by weight of the total composition. 1. A process to prepare a plasticizer in at least a 90% yield , wherein the plasticizer has a molecular weight of greater than 300 with at least 2 alkyl ketal ester moieties , comprising the step:contacting under reaction conditions, an alkyl ketal ester, a multihydric hydrocarbyl moiety, or a monohydric alkyl ketal ester;a catalyst; andan antioxidant, a thermal stabilizer or mixtures thereof, wherein a plasticizer comprising at least 2 alkyl ketal ester moieties is obtained with a molecular weight of greater than 300 and is produced in at least a 90% yield.3. The process of claim 2 , wherein the plasticizer is the compound of formula (IV) wherein Ris a C4 alkyl.4. The process of claim 3 , wherein each a=2 and each b=0. This application is a Divisional of U.S. application Ser. No. 13/648,252, filed Oct. 9, 2012, which claims the benefit under 35 U.S.C. 119(e) to U.S. Provisional Patent Application No. 61/545,849, filed Oct. 11, 2011. The disclosures of which are incorporated by reference herein.The invention relates generally to the preparation of stabilized alkyl ketal ester plasticizers having at least 2 alkyl ketal ester moieties, such as those derived from levulinic acid, with a molecular weight of greater than 300 and compositions thereof.Many known chemical products such as surfactants, plasticizers, solvents, and polymers are currently manufactured from non-renewable, expensive, petroleum-derived or natural gas-derived feedstock compounds. High raw material costs and uncertainty of ...

Подробнее
Номер записи: 96
30-11-2017 дата публикации

KETAL ESTER COMPOUNDS AND USES THEREOF

Номер: US20170342045A1
Автор: Molitor Erich J., MULLEN Brian D., Yontz Dorie J.
Принадлежит:

The invention describes methods of preparation and compositions of plasticizers. The ketal diester products described are useful as components of polymer compositions. The products are excellent plasticizers for a variety of polymers, such as poly(vinylchloride) plastisols. 2. The compound of claim 1 , wherein Rcomprises 2 to 4 carbon atoms.3. The compound of claim 1 , wherein Rcomprises 8 to 12 carbon atoms.4. The compound of claim 1 , wherein Rcomprises 14 to 18 carbon atoms.5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. The compound of claim 1 , wherein Rcomprises 13-17 carbon atoms.15. The compound of claim 1 , wherein Ris an aryl group.19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. The compound of claim 1 , wherein Ris a benzyl and Rcomprises 12 carbon atoms.29. (canceled)34. A mixture comprising two or more compounds of .35. A plasticizer composition comprising a compound of .36. A composition comprising:(a) a polymer; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) a compound or mixture of compounds of .'} The invention relates generally to alkyl ketal esters as well as their method of making and using. The alkyl ketal esters have use as plasticizers in polymeric formulations.Many known chemical products such as surfactants, plasticizers, solvents, and polymers are currently manufactured from non-renewable, expensive, petroleum-derived or natural gas-derived feedstock compounds. Phthalate esters, particularly, dioctyl phthalate ester, di(2-ethylhexyl) phthalate ester, and diisononyl phthalate ester are industrially significant plasticizers useful for plasticizing many formulations; more common formulations include those containing poly(vinyl chloride) (PVC). Recent regulatory pressure has targeted phthalates (United States Environmental Protection Agency Report: Phthalates Action Plan—Dec. 30, 2009) for replacement due to the risks ...

Подробнее
Номер записи: 97
08-12-2016 дата публикации

PROCESS FOR THE INDUSTRIAL SYNTHESIS OF SORDIDIN

Номер: US20160355526A1
Автор: DUFOUR Samuel, LEJEUNE Valérie, SEVESTRE Hubert
Принадлежит:

The present invention relates to a process for preparing sordidin, comprising a step of preparing 4-(2-ethyl-1,3-dioxolan-2-yl)pentan-2-one by means of a reaction in which 2-ethyl-2-(pent-4-en-2-yl)-1,3-dioxolane is oxidized in the presence of a catalyst chosen from the group comprising organometallic complexes of transition metals. 2. Process according to claim 1 , wherein the oxidation reaction is carried out in the presence of an oxidising agent chosen from air claim 1 , oxygen-enriched air claim 1 , oxygen Oand hydroperoxides with the general formula R—OOH wherein R can be a hydrogen atom claim 1 , a linear or branched C-Calkyl group claim 1 , particularly a terbutyl group or a cumyl aromatic group.3. Process according to wherein the catalyst is chosen from organometallic complexes of transition metals with a Ni claim 1 , Rh claim 1 , Ir claim 1 , Pd claim 1 , Co or Pt base.4. Process according to wherein the catalyst is chosen from Palladium (II) compounds such as PdCl claim 1 , Pd(Acetate) claim 1 , Pd(Acetate)(triflate) claim 1 , Pd(OH)or PdBr claim 1 , from Nickel (II) compounds such as Ni(Acetate) claim 1 , NiClor NiBr claim 1 , from the Cobalt compounds such as Co(No) claim 1 , CoCl claim 1 , CoBror Co(Acetate)or from Rhodium (III) compounds such as Rh(Cl) or Rh(ClO)5. Process according to wherein the catalyst is complexed by a ligand chosen from amines claim 1 , phosphines and phtalocyanines.6. Process according to wherein a catalyst regenerator is added.7. Process according to claim 6 , wherein the catalyst regenerator is chosen from copper or iron-based regenerators such as CuCl claim 6 , CuCl2 claim 6 , CuBr claim 6 , CuBr2 claim 6 , CuAcetate claim 6 , FeCl2 claim 6 , FeCl3.8. Process according to wherein the catalyst is Pd(Acetate).9. Process according to wherein the oxidation reaction of compound 3 into compound 4 is carried out in the presence of at least one solvent chosen from water claim 1 , alcoholic solvents claim 1 , acidic solvents claim 1 , ...

Подробнее
Номер записи: 98
17-12-2015 дата публикации

SOLVENT SYSTEM AND COMPOSITIONS THEREWITH

Номер: US20150361281A1
Автор: NASCIMENTO Ronaldo, SILVA Suelbi
Принадлежит: RHODIA POLIAMIDA E ESPECIALIDADES LTDA

The present invention relates to a solvent system characterized by the fact that is comprises one or more dioxolane-derived esters of formula I 2. The solvent system according to characterized by the fact that R1 claim 1 , R2 and R3 are selected from the group consisting of methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , sec-butyl claim 1 , n-pentyl claim 1 , isopentyl claim 1 , sec-pentyl claim 1 , cyclopentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , 2-methylpentyl claim 1 , 3-methylpentyl and phenyl claim 1 , and wherein n is either 1 or 2.3. The solvent system according to claim 1 , wherein R1 is methyl claim 1 , R2 is selected from the group consisting of methyl claim 1 , isobutyl and phenyl claim 1 , R3 is selected from the group consisting of methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl and isobutyl and wherein n=1.4. The solvent system according to characterized by the fact that the solvent system comprise at least a dioxolane-derived ester being 2 claim 1 ,2-dimethyl-1 claim 1 ,3-dioxolane-4-methanol acetate.6. A method for solubilizing grease or oily compounds claim 1 , active ingredients such as pesticides claim 1 , herbicides claim 1 , fungicides claim 1 , pharmaceutical intermediates or active principles claim 1 , polymers and additives such as antioxidants claim 1 , plasticizers claim 1 , excipients claim 1 , rheology modifiers claim 1 , and preservatives using the solvent system according to7. A method for preparing a coating compositions comprising using the solvent system according to .8. A method for preparing a paints based on acrylic claim 7 , nitrocellulose claim 7 , polyester claim 7 , polyol polyester claim 7 , epoxy claim 7 , alkyd claim 7 , melamine claim 7 , maleic claim 7 , phenolic resins or isocyanate-based paint as well as in polyurethane-based paint comprising using the solvent system according to .9. (canceled)11. The method ...

Подробнее
Номер записи: 99
07-12-2017 дата публикации

CATIONIC LIPID

Номер: US20170349532A1
Автор: Era Tomohiro, Kuboyama Takeshi, Naoi Tomoyuki, Yagi Nobuhiro
Принадлежит: KYOWA HAKKO KIRIN CO., LTD.

The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) 128-. (canceled)30. The method according to claim 29 , wherein the cationic lipid forms a complex between a combination of the cationic lipid with a neutral lipid and/or a polymer and the nucleic acid.31. The method according to claim 29 , wherein the nucleic acid is a nucleic acid having an activity of suppressing the expression of the target gene by utilizing RNA interference (RNAi).32. The method according to claim 31 , wherein the target gene is a gene associated with tumor or inflammation.33. A method for introducing the nucleic acid into a cell by using the composition obtained by the method according to .34. The method according to claim 33 , wherein the cell is a cell at a tumor or inflammation site of a mammal.35. The method according to claim 33 , wherein the cell is a cell in the liver claim 33 , lungs claim 33 , kidneys or spleen of a mammal.36. The method according to claim 33 , wherein the method of the introduction into a cell is a method of introduction into a cell by intravenous administration.37. A method for treating cancer or inflammatory disease claim 32 , comprising a step of administering the composition obtained by the method according to .38. The method according to claim 37 , wherein the method of administration is intravenous administration.39. A medicament comprising the composition obtained by the method according to .40. The medicament according to claim 39 , which is for intravenous administration. The present invention relates to a novel cationic lipid that allows, for example, nucleic acid to be easily introduced into cells, and to a novel composition comprising the cationic lipid, and the like.Cationic lipids are amphiphilic molecules that generally contain a lipophilic region containing one or more hydrocarbon groups, and a hydrophilic region containing at least one positively charged polar head ...

Подробнее
Номер записи: 100