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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Применить Всего найдено 3988. Отображено 100.
19-04-2012 дата публикации

Organic Compounds Having Cooling Properties

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

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

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Номер записи: 1
24-05-2012 дата публикации

Piperazinyl derivatives useful as modulators of the neuropeptide y2 receptor

Номер: US20120129870A1
Автор: Chandravadan R. Shah, Dale A. Rudolph, Devin M. Swanson, Jill A. Jablonowski, Victoria D. Wong, Wenying Chai
Принадлежит: Janssen Pharmaceutica NV

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

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Номер записи: 2
07-06-2012 дата публикации

Method for synthesis of secondary alcohols

Номер: US20120142934A1
Автор: Chien-Hong Cheng, Jaganathan Karthikeyan, Pang-Chi Huang
Принадлежит: National Tsing Hua University NTHU

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

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Номер записи: 3
23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Автор: Bernd Nosse, Gerald Juergen Roth, Heike Neubauer, Joerg Kley, Martin Fleck, Niklas Heine, Thorsten Lehmann-Lintz
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

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

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Номер записи: 4
30-08-2012 дата публикации

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

Номер: US20120220592A1
Автор: Alessandra Restivo, Carla Caccia, Cibele Sabido-David, Ermanno Moriggi, Florian Thaler, Laura Faravelli, Mauro Napoletano, Patricia Salvati
Принадлежит: Newron Pharmaceuticals SpA

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

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Номер записи: 5
16-05-2013 дата публикации

MODULATORS OF CENTRAL NERVOUS SYSTEM NEUROTRANSMITTERS

Номер: US20130123253A1
Автор: CASHMAN John
Принадлежит: HUMAN BIOMOLECULAR RESEARCH INSTITUTE

Disclosed are agents having pharmacological activity against cellular receptors and intracellular signaling, particularly receptors and signaling pathways of central nervous system (CNS) neurotransmitters. Also disclosed are related methods and compositions for the treatment or prevention of diseases or disorders using the agents. 3. A compound of claim 2 , wherein G is hydrogen or combined with Rto form a 5-6 membered heterocylcoalkyl containing 1-2 heteroatoms each independently selected from the group consisting of N and 0; and subscript b is 1-3.4. A compound of claim 3 , wherein D is a member selected from the group consisting of optionally substituted phenyl claim 3 , optionally substituted naphthyl and optionally substituted bi-phenyl; and subscript a is 0-3.5. A compound of claim 3 , selected from the group consisting of:2-(aminomethyl)-5-phenyltetrahydrofuran,2-(aminomethyl)-5-(4′-chlorophenyl)tetrahydrofuran,2-(aminomethyl)-5-(4-bromophenyl)tetrahydrofuran,2-(aminomethyl)-5-(4-methoxyphenyl)tetrahydrofuran,2-(aminomethyl)-5-(4′-t-butylphenyl)tetrahydrofuran,trans-2-(aminomethyl)-5-(2′-methoxy-5′-fluorophenyl)tetrahydrofuran,cis-2-(aminomethyl)-5-(2′-methoxy-5-fluorophenyl)tetrahydrofuran,2-(aminomethyl)-5-(3′-fluoro-4′-methylphenyl)tetrahydrofuran,2-(aminomethyl)-5-cyclohexyltetrahydrofuran,2-(aminomethyl)-5-(1′-naphthyl)tetrahydrofuran,2-(aminomethyl)-5-(2′-naphthyl)tetrahydrofuran,2-(aminomethyl)-5-(2′-naphthyl)tetrahydrofuran,2-(aminoethyl)-5-phenyltetrahydrofuran,2-(aminoethyl)-5-(4′-fluorophenyl)tetrahydrofuran,2-(aminoethyl)-5-(4′-bromophenyl)tetrahydrofuran,2-(aminoethyl)-5-(4′-t-butylphenyl)tetrahydrofuran,trans-7 aminoethyl)-5-(2′-methoxy-5′-fluorophenyl)tetrahydrofuran,cis-2-(aminoethyl)-5-(2′-methoxy-5′-fluorophenyl)tetrahydrofuran,2-(aminoethyl)-5-cyclohexyltetrahydrofuran,2-(aminoethyl)-5-(2′-furyl)tetrahydrofuran,2-(aminomethyl)-5-benzyltetrahydrofuran,2-(aminoethyl)-5-benzyltetrahydrofuran,trans-2-(aminomethyl)-5-(2′-methoxy-5′-fluorobenzyl) ...

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Номер записи: 6
23-05-2013 дата публикации

ETHER COMPOUND, ELECTROLYTE COMPOSITION FOR NON-AQUEOUS BATTERY, BINDER COMPOSITION FOR NON-AQUEOUS BATTERY ELECTRODE, SLURRY COMPOSITION FOR NON-AQUEOUS BATTERY ELECTRODE, ELECTRODE FOR NON-AQUEOUS BATTERY AND NON-AQUEOUS BATTERY

Номер: US20130130102A1
Автор: Nakata Natsuko, OKUYAMA Kumi, Sakamoto Kei
Принадлежит: ZEON CORPORATION

An ether compound represented by the following formula and its use: 4. An electrolyte solution composition for a non-aqueous battery claim 1 , comprising an organic solvent claim 1 , an electrolyte dissolved in the organic solvent claim 1 , and the ether compound according to .5. A binder composition for a non-aqueous battery electrode claim 1 , comprising an acrylic-based polymer and the ether compound according to .6. A slurry composition for a non-aqueous battery electrode claim 5 , containing an electrode active material and the binder composition for a non-aqueous battery electrode according to .7. An electrode for a non-aqueous battery claim 5 , comprising a current collector and an electrode active material layer provided on a surface of the current collector claim 5 ,{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'wherein the electrode active material layer is obtained by applying and drying the slurry composition for a non-aqueous battery electrode according to .'}8. A non-aqueous battery claim 5 , comprising a positive electrode claim 5 , a negative electrode claim 5 , and a non-aqueous electrolyte solution claim 5 ,{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'wherein the non-aqueous electrolyte solution is the electrolyte solution composition for a non-aqueous battery according to .'}9. A non-aqueous battery claim 5 , comprising a positive electrode claim 5 , a negative electrode claim 5 , and a non-aqueous electrolyte solution claim 5 ,{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'wherein one or both of the positive electrode and the negative electrode is the electrode for a non-aqueous battery according to .'} The present invention relates to a novel ether compound as well as an electrolyte solution composition for a non-aqueous battery, a binder composition for a non-aqueous battery electrode, a slurry composition for a non-aqueous battery electrode, an electrode for a non-aqueous battery, and a non-aqueous battery, each of which uses the ...

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Номер записи: 7
04-07-2013 дата публикации

PROCESS FOR PREPARING 1, 6-HEXANEDIOL

Номер: US20130172578A1
Автор: Allgeier Alan Martin, Desilva Namal, KOROVESSI EKATERINI, MENNING CARL, Ritter Joachim C., Sengupta Sourav Kumar, Stauffer Christina S.
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Disclosed are processes for preparing 1,6-hexanediol and synthetic intermediates useful in the production of 1,6-hexanediol from renewable biosources. In one embodiment, a process comprises contacting levoglucosenone with hydrogen in the presence of a first hydrogenation catalyst at a first temperature to form product mixture (I); and heating product mixture (I) in the presence of hydrogen and a second hydrogenation catalyst at a second temperature to form product mixture (II) which comprises 1,6-hexanediol. 1. A process comprising:a) contacting levoglucosenone with hydrogen in the presence of a first hydrogenation catalyst at a first temperature between about 25° C. and about 150° C. to form product mixture (I); andb) heating product mixture (I) in the presence of hydrogen and a second hydrogenation catalyst at a second temperature between about 120° C. and about 260° C. to form product mixture (II).2. The process of claim 1 , wherein product mixture (I) comprises one or more of levoglucosenol claim 1 , levoglucosanol claim 1 , tetrahydrofuran 2 claim 1 ,5-dimethanol claim 1 , 2-hydroxymethyltetrahydropyran claim 1 , 1 claim 1 ,2 claim 1 ,5 claim 1 ,6-tetrahydroxyhexane claim 1 , 1 claim 1 ,2 claim 1 ,6-hexanetriol claim 1 , and 2-hydroxymethyl-5-hydroxytetrahydropyran.3. The process of claim 1 , wherein product mixture (II) comprises one or more of 1 claim 1 ,2 claim 1 ,6-hexanetriol claim 1 , tetrahydrofuran 2 claim 1 ,5-dimethanol claim 1 , 2-hydroxymethyl-5-hydroxytetrahydropyran claim 1 , 1 claim 1 ,6-hexanediol claim 1 , 1 claim 1 ,2-hexanediol claim 1 , 1-hexanol claim 1 , and 2-hydroxymethyltetrahydropyran.4. The process of claim 3 , wherein product mixture (II) comprises 1 claim 3 ,6-hexanediol.5. The process of claim 1 , wherein the first hydrogenation catalyst comprises one or more of supported platinum catalysts claim 1 , supported palladium catalysts claim 1 , supported ruthenium catalysts claim 1 , supported nickel catalysts claim 1 , catalysts ...

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Номер записи: 8
04-07-2013 дата публикации

PRODUCTION OF TETRAHYDROFURAN-2, 5-DIMETHANOL FROM ISOSORBIDE

Номер: US20130172586A1
Автор: Desilva Namal, KOROVESSI EKATERINI, MENNING CARL, MURPHY JOSEPH E., Ritter Joachim C., Sengupta Sourav Kumar, Stauffer Christina S.
Принадлежит: E I DU PONT DE NEMOURS AND COMPANY

Disclosed herein are processes comprising contacting isosorbide with hydrogen in the presence of a first hydrogenation catalyst to form a first product mixture comprising tetrahydrofuran-2,5-dimethanol. The processes can further comprise heating the first product mixture in the presence of hydrogen and a second hydrogenation catalyst to form a second product mixture comprising 1,6-hexanediol. The first and second hydrogenation catalysts can be the same or different. 1. A process comprising:a) contacting isosorbide with hydrogen in the presence of a first hydrogenation catalyst at a first temperature between about 150° C. and about 400° C. and at a first pressure between about 500 psi to about 5000 psi to form a first product mixture comprising tetrahydrofuran-2,5-dimethanol.2. The process of claim 1 , wherein the first product mixture further comprises 1 claim 1 ,6-hexanediol.3. The process of claim 1 , further comprising:b) heating the first product mixture in the presence of hydrogen and a second hydrogenation catalyst at a second temperature between about 120° C. and about 350° C. to form a second product mixture comprising 1,6-hexanediol.4. The process of claim 3 , wherein the first and second hydrogenation catalysts are the same.5. The process of claim 1 , wherein the catalyst comprises copper.6. The process of claim 1 , wherein the catalyst comprises CuO.7. The process of claim 1 , wherein the catalyst comprises from 2 weight percent to 98 weight percent CuO claim 1 , and further comprises from 98 weight percent to 2 weight percent of at least one oxide selected from the group consisting of zinc oxide claim 1 , magnesium oxide claim 1 , barium oxide claim 1 , chromium oxide claim 1 , silica claim 1 , alumina claim 1 , zirconium dioxide claim 1 , nickel oxide claim 1 , manganese oxide claim 1 , sodium oxide claim 1 , potassium oxide claim 1 , cerium oxide claim 1 , lanthanum oxide claim 1 , iron oxide claim 1 , silver oxide claim 1 , and cobalt oxide claim 1 , ...

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Номер записи: 9
25-07-2013 дата публикации

APOPTOSIS PROMOTERS

Номер: US20130190488A1
Автор: Bruncko Milan, Ding Hong, Elmore Steven, Kunzer Aaron, Lynch Christopher L., McClellan William, Mitten Michael, Park Cheol-Min, Petros Andrew, Shoemaker Alexander, Song Xiaohong, Tu Noah, Wang Xilu, WENDT Michael
Принадлежит: ABBOTT LABORATORIES

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

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Номер записи: 10
15-08-2013 дата публикации

PURIFICATION OF POSACONAZOLE AND OF POSACONAZOLE INTERMEDIATES

Номер: US20130211086A1
Автор: Bhuta Sachin, De Souza Dominic, Langner Martin, Pise Abhinay C.
Принадлежит: SANDOZ AG

The present invention relates to a process for the preparation of a hydrogen chloride (HCl) salt of a compound of formula (I) wherein Yand Yare independently F or Cl, preferably F, said compound of formula (I) containing the cis-isomer and the trans-isomer, wherein the process comprises (1) providing the compound of formula (I) comprised in a first suitable solvent; and (2) treating the compound of formula (I) comprised in the first suitable solvent with HCl comprised in a second suitable solvent to obtain the HCl salt of the compound of formula (I). 2. The process of claim 1 , wherein the compound of formula (I) provided in (1) contains from 80 to 95% claim 1 , preferably from 85 to 95% of the cis-isomer of formula (II) and from 20 to 5% claim 1 , preferably from 15 to 5% of the trans-isomer of formula (III).4. The process of claim 3 , wherein the method according to which the compound of formula (I) is provided in (1) further comprises(vii) at least partially crystallizing the compound of formula (I) after (vi.2).5. The process of claim 1 , wherein the first suitable solvent in which the compound of formula (I) is comprised is an organic solvent claim 1 , preferably an alcohol and/or a precursor of an alcohol claim 1 , an ether claim 1 , a ketone claim 1 , an ester claim 1 , or a mixture of two or more thereof.6. The process of claim 1 , wherein the first suitable solvent in which the compound of formula (I) is comprised is selected from the group consisting of ethyl acetate claim 1 , isopropyl acetate claim 1 , diethyl ether claim 1 , tetrahydrofuran (THF) claim 1 , methyl tetrahydrofuran claim 1 , dioxane claim 1 , methanol claim 1 , n-propanol claim 1 , 1-butanol claim 1 , 2-butanol claim 1 , 2-methyl-1-butanol claim 1 , 3-methyl-1-butanol claim 1 , acetone claim 1 , 2-butanone claim 1 , and methyl isobutyl ketone (MIBK) claim 1 , and wherein the second solvent is selected from the group consisting of dioxane claim 1 , tetrahydrofuran (THF) claim 1 , diethyl ...

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Номер записи: 11
05-09-2013 дата публикации

Fluorinated monomer of cyclic acetal structure, polymer, resist protective coating composition, resist composition, and patterning process

Номер: US20130231491A1
Автор: Jun Hatakeyama, Kazunori Maeda, Koji Hasegawa, Satoshi SHINACHI, Takeru Watanabe, Takeshi Kinsho, Tomohiro Kobayashi, Yuji Harada
Принадлежит: Shin Etsu Chemical Co Ltd

A fluorinated monomer of cyclic acetal structure has formula (1) wherein R is a C 1 -C 20 alkyl group which may be substituted with halogen or separated by oxygen or carbonyl, and Z is a divalent organic group which forms a ring with alkylenoxy and contains a polymerizable unsaturated group. A polymer derived from the fluorinated monomer may be endowed with appropriate water repellency, water sliding property, lipophilicity, acid lability and hydrolyzability and is useful in formulating a protective coating composition and a resist composition.

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Номер записи: 12
24-10-2013 дата публикации

Novel ruthenium complexes and their uses in processes for formation and/or hydrogenation of esters, amides and derivatives thereof

Номер: US20130281664A1
Автор: Boopathy Gnanaprakasam, Chidambaram Gunanathan, David Milstein, Ekambaram Balaraman, Jing Zhang
Принадлежит: Yeda Research and Development Co Ltd

The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e., synthesis of amides from esters and amines); (8) acylation of alcohols using esters; (9) coupling of alcohols with water to form carboxylic acids; and (10) dehydrogenation of beta-amino alcohols to form pyrazines. The present invention further relates to the novel uses of certain pyridine Ruthenium catalysts.

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Номер записи: 13
31-10-2013 дата публикации

4-(p-QUINONYL)-2-HYDROXYBUTANAMIDE DERIVATIVES FOR TREATMENT OF MITOCHONDRIAL DISEASES

Номер: US20130289034A1
Автор: Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader
Принадлежит: Edison Phamaceuticals Inc

Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.

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Номер записи: 14
07-11-2013 дата публикации

Cyanoenamines and Their use as Fungicides

Номер: US20130298291A1
Автор: Benting Jurgen, Desbordes Philippe, Dubost Christophe, Genix Pierre, Narabu Shinichi, Vors Jean-Pierre, Wachendorff-Neumann Ulrike
Принадлежит: Bayer Intellectual Property GmbH

The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions. 2. A composition for controlling an unwanted microorganism or insect claim 1 , comprising at least one compound according to claim 1 , and one or more extenders and/or surfactants.3. A compound according to claim 1 , capable of being used for controlling unwanted microorganisms and insects.4. A method for controlling an unwanted microorganism claim 1 , comprising applying a compound according to claim 1 , to the microorganisms and/or a habitat thereof.5. A process for preparing a composition for controlling an unwanted microorganism claim 1 , comprising mixing a compound according to claim 1 , with one or more extenders and/or surfactants.6. A compound according to claim 1 , capable of being used for treating transgenic plants.7. A transgenic plant that has been treated with a compound of .8. A method for treating a transgenic plant complying treating said plant with a compound of . The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.In WO 01/85673 arylcyanoenaminones of general formula:are described, wherein K represents an oxygen or sulphur atom, Ar represents an optionally substituted aryl or heteroaryl, X may represent a cyano group, Z represents an optionally substituted phenyl or naphthyl and Y represents an optionally substituted alkyl chain. However, there is no disclosure or suggestion in this documents of any derivative wherein Ar ...

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Номер записи: 15
14-11-2013 дата публикации

Preparation of aminomethyl furans and alkoxymethyl furan derivatives from carbohydrates

Номер: US20130303791A1
Автор: Alexandra Sanborn, Stephen Howard
Принадлежит: Archer Daniels Midland Co

Described herein are single step methods of making various classes of alkylamine derivatives of furan and tetrahydrofuran by simultaneous contact of a sugar with H 2 , an acid catalyst and hydrogenation catalyst in the presence of an alkylamide solvent. The hydrogenation catalyst is a heterogeneous catalyst comprising a metal selected from the group consisting of Pt, Pd, and nickel. The acid catalysts may be homogeneous mineral acid or a heterogeneous acid catalyst on substrate. In a preferred practice the two catalysts are provided on a common heterogeneous bifunctional support. Using similar combinations of acid and hydrogenation catalysts, there is also described single step methods for making furandimethanol by simultaneously contacting a hexose with the two separate catalysts in the presence of H 2 in an aprotic solvent, such as dimethylformamide. With the same catalyst system and similar reaction conditions, 2,5 furan dialkylethers can also be made in a single step when the solvent includes an ROH alcohol.

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Номер записи: 16
28-11-2013 дата публикации

Compounds and therapeutic uses thereof

Номер: US20130317027A1
Автор: Brett R. Murphy, Christophe Hoarau, Dange Vijay Kumar, Daniel Feodore Zigar, Daniel P. Parker, David A. Gerrish, David M. Dastrup, Ian A. Mcalexander, In Chul Kim, J. Adam Willardsen, J. Jay Boniface, Jeffrey W. Lockman, Kraig M. Yager, Matthew Gregory Bursavich, Paul R. Sebahar, Ryan T. Terry-Lorenzo, Se-Ho Kim, Tracey C. Fleischer, Weston R. Judd
Принадлежит: Myrexis, Inc.

The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.

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Номер записи: 17
27-03-2014 дата публикации

NOVEL SUBSTITUTED TETRAHYDRONAPHTHALENES, PROCESS FOR THE PREPARATION THEREOF AND THE USE THEREOF AS MEDICAMENTS

Номер: US20140088077A1
Автор: GOSSEL Matthias, Haack Torsten, Lennig Petra, SCHWINK Lothar, STENGELIN Siegfried
Принадлежит: SANOFI

The invention relates to substituted tetrahydronaphthalenes and derivatives thereof, and also to the physiologically compatible salts and physiologically functional derivatives thereof, to preparation thereof, to medicaments comprising at least one inventive substituted tetrahydronaphthalene or derivative thereof, and to the use of the inventive substituted tetrahydronaphthalenes and derivatives thereof as medicaments. 2. The compound according to claim 1 , wherein:L2 is a bond;or a physiologically compatible salt thereof.4. The compound according to claim 1 , wherein:L3 is a bond, O, or C(R62)(R63)O;or a physiologically compatible salt thereof.5. The compound according to claim 1 , wherein:{'sub': 1', '6, 'B is a 4- to 6-membered nonaromatic ring which includes from 1 to 2 oxygen atoms, where the ring system is optionally substituted by one or more substituents selected from (C-C)-alkyl and hydroxyl;'}or a physiologically compatible salt thereof.11. A pharmaceutical composition comprising the compound according to or a physiologically compatible salt thereof claim 1 , in combination with a pharmacologically acceptable carrier or excipient.12. The pharmaceutical composition according to claim 11 , further comprising one or more active ingredients which are effective in treating a metabolic disorder or a disease associated therewith.13. The pharmaceutical composition according to claim 11 , further comprising one or more antidiabetics.14. The pharmaceutical composition according to claim 11 , further comprising one or more lipid modulators.15. The pharmaceutical composition according to claim 11 , further comprising one or more antiobesity agents.16. A pharmaceutical composition comprising the compound according to or a physiologically compatible salt thereof claim 7 , in combination with a pharmacologically acceptable carrier or excipient.17. A pharmaceutical composition comprising the compound according to or a physiologically compatible salt thereof claim 8 , in ...

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Номер записи: 18
05-01-2017 дата публикации

DIRECT SYNTHESIS OF BIO-BASED ALKYL & FURANIC DIOL ETHERS, ACETATES, ETHER-ACETATES, AND CARBONATES

Номер: US20170001971A1
Автор: Stensrud Kenneth, Venkitasubramanian Padmesh
Принадлежит:

A method of preparing a glycol mono-ether or mono-acetate, or carbonate involving either one of two pathways from alkylene glycols, HMF or its reduction derivative products (i.e., FDM, bHMTHFs), is provided. In particular, according to one pathway, the alkylene glycol, HMF or FDM, bHMTHFs are reacted with a dialkyl carbonate in the presence of a deprotonating agent, in substantial absence of an extrinsic catalyst, to produce an ether, and subsequently reacting the ether with an acid base. According to the other pathway, alkylene glycols are reacted with an acetate donor in the presence of an acid, base, to generate an alkylene monoacetate, and etherified with a carbonate in the presence of a deprotonating agent. 1. A method of preparing a mono-ether from a diol compound , comprising either a first pathway or second pathway , wherein:{'sup': 1', '1', '1', '2', '2', '2, 'sub': '3', 'in the first pathway, the diol compound is contacted with an Rorganic acid in the presence of a Brønsted acid at a temperature and for time sufficient to form a Rmono ester of the diol compound, then the Rmono ester of the diol compound is contacted with a Ralkyl diester of the formula R(CO)Rin the presence of a deprotonating agent at a temperature and for a time sufficient to form the monoester ether; or'}{'sup': 2', '2', '2', '1, 'in the second pathway, the diol compound is contacted with the an Ralkyl diester of the formula R(CO3)Rin the presence of a deprotonating agent at a temperature and for a time sufficient to form a mono ester of the diol compound, then the mono ester of the diol compound is contacted with an Rorganic acid in the presence of a Brønsted acid at a temperature and for time sufficient to form the monoester ether;'}{'sup': 1', '2, 'wherein Rand Rare the same or different alkyl, cyclo-alkyl or aromatic moieties.'}2. The method according to claim 1 , wherein the diol compound is at least one member selected from the group consisting of ethylene glycol (EG) claim 1 , ...

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Номер записи: 19
05-01-2017 дата публикации

N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

Номер: US20170002017A1
Автор: ANDREZ Jean-Christophe, Chowdhury Sultan, DECKER Shannon Marie, DEHNHARDT Christoph Martin, FOCKEN Thilo, GRIMWOOD Michael Edward, HEMEON Ivan William, Jia Qi, LI JUN, Ortwine Daniel F., SAFINA Brian, SHENG Tao, Sun Shaoyi, Sutherlin Daniel P., WILSON Michael Scott, ZENOVA Alla Yurevna
Принадлежит:

The invention provides novel compounds having the general formula: 3. The compound of wherein B is N and Ris absent.4. The compound of wherein B is C.5. The compound of wherein R claim 1 , Rand Rare each independently selected from H claim 1 , F claim 1 , or Cl.6. The compound of wherein Ris H claim 1 , F or Cl; Rand Rare each H; and Ris an optionally substituted group selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —CN claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl claim 1 , and Calkoxy.7. The compound of wherein Ris Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl or —NRR.8. The compound of claim 7 , wherein Ris selected from the group consisting of methyl claim 7 , ethyl claim 7 , propyl claim 7 , trifluoromethyl claim 7 , difluoromethyl claim 7 , monofluoromethyl claim 7 , isopropyl and cyclopropyl.11. The compound of wherein Ris selected from the group consisting of: methyl claim 1 , ethyl claim 1 , tert-butyl claim 1 , dimethylamino claim 1 , methylamino claim 1 , amino claim 1 , morpholino claim 1 , azetidino claim 1 , imidazolyl claim 1 , 3-hydroxyazetidino claim 1 , 3-fluoroazetidino claim 1 , cyclopropyl claim 1 , pyrrolidinyl claim 1 , 3 claim 1 ,3-difluoroazetidino claim 1 , tert-butyl claim 1 , ethyl claim 1 , 2-methoxyethyl claim 1 , 3-methoxyazetidino claim 1 , 2-hydroxyethyl claim 1 , 3-hydroxypyrrolidinyl claim 1 , and N-methylimidazolyl.12. The compound of wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)- is an optionally substituted group selected from the group consisting of Calkylene claim 1 , Calkenylene or Calkynylene.13. The compound of claim 1 , wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)- is selected from the group consisting of —CH— claim 1 , —C(═O)— claim 1 , —C(H)(CH)— claim 1 , —CH—CH— claim 1 , —CH—C(H)(CH)— claim 1 , —C(H)(CH)—C(H)— claim 1 , —CHCHCH— claim 1 , —CH—C(H)(CH)—CH— or —CHCHCHCH—.14. The compound of claim 13 , ...

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Номер записи: 20
07-01-2021 дата публикации

PHENYL CYCLOHEXANONE DERIVATIVES AND METHODS OF MAKING AND USING THEM

Номер: US20210002214A1
Автор: Wainer Irving W.
Принадлежит:

Phenyl cyclohexanone based active agents, pharmaceutical preparations containing such active agents, methods of modifying cellular activity by contacting cells with such active agents, and methods of treating various conditions by administering such active agents to a patient are described. 2. A stereoisomer of a compound of .4. A phenyl cyclohexanone compound of wherein there is a cis stereochemical relationship between the C2 and C6 chiral centers on the cyclohexanone ring.5. A phenyl cyclohexanone compound of wherein the C2 carbon of the cyclohexanone ring is in an S configuration.6. A pharmaceutical composition comprising a phenyl cyclohexanone compound in accordance with and a pharmaceutically acceptable carrier.7. A method of treatment comprising administering a pharmaceutical composition in accordance with to a patient in need of treatment claim 6 , the compound being present in a therapeutically effective amount.8. The method of wherein the compound or composition is administered to a patient in need of treatment for bipolar depression claim 7 , major depressive disorder claim 7 , schizophrenia claim 7 , Alzheimer's dementia claim 7 , amyotrophic lateral sclerosis claim 7 , complex regional pain syndrome (CRPS) claim 7 , chronic pain claim 7 , or neuropathic pain.9. A method of inhibiting MNDA receptor activity comprising contacting cells with a concentration of a compound in accordance with sufficient to inhibit MNDA receptor activity.10. A method of modifying endogenous concentrations of D-Serine comprising contacting cells with a concentration of a compound in accordance with sufficient to modify endogenous concentrations of D-Serine.11. A method of stimulating the activating phosphorylation of mTOR comprising contacting cells with a concentration of a compound in accordance with sufficient to stimulate the activating phosphorylation of mTOR.12. A method of inhibiting nAChR activity comprising contacting cells with a concentration of a compound in ...

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Номер записи: 21
01-01-2015 дата публикации

AMIDE COMPOUND AND USE THEREOF FOR PEST CONTROL

Номер: US20150005348A1
Автор: Awano Tomotsugu, Ihara Hideki, Ohshita Jun
Принадлежит:

An amide compound represented by formula (I) has an excellent pest control effect. (In the formula, Y represents a 3-7 membered saturated heterocyclic ring which contains, as ring-forming components(s), one or more atoms or groups that are selected from the group consisting of an oxygen atom and —S(O)—, the saturated heterocyclic ring may have one to three atoms or groups selected from group D and t represents 0 or the like; x represents a C-Cchain hydrocarbon group having one group that is selected from group A; W represents —CR— or the like; r represents 1 or the like; R, R, R, R, R, R, Rand Rmay be the same or different and each represents a hydrogen atom or the like; and n represents 1 or the like.) 3. The amide compound according to claim 2 , wherein p is 1 claim 2 , or q is 0.4. The amide compound according to claim 2 , wherein p is 2 claim 2 , or q is 1.5. The amide compound according to claim 2 , wherein Yis an oxygen atom.6. The amide compound according to claim 2 , wherein Y is a group represented by the formula (II-a) claim 2 , and Yis an oxygen atom.7. The amide compound according to claim 2 , wherein Y is a group represented by the formula (II-b).8. The amide compound according to claim 1 , wherein{'sup': 8', '1, 'W is —CR—, r is 1, Ris a halogen atom or a hydrogen atom,'}{'sup': '2', 'Ris a C1 to C4 alkyl group optionally having one or more halogen atoms or a hydrogen atom,'}{'sup': '4', 'Ris a C1 to C4 alkyl group optionally having one or more halogen atoms, a halogen atom or a hydrogen atom,'}{'sup': 3', '5', '3', '5', '9', '10', '9', '10, 'sub': 'v', 'Rand Rare the same or different and represent a C1 to C4 alkyl group optionally having one or more halogen atoms, a halogen atom or a hydrogen atom, or Rand Rare taken together to be —(CRR)—, v is 1, Rand Rare the same or different and are a C1 to C4 alkyl group optionally having one or more halogen atoms, a halogen atom or a hydrogen atom,'}{'sup': '8', 'Ris a hydrogen atom, and'}{'sup': 6', '7, 'Rand ...

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Номер записи: 22
12-01-2017 дата публикации

Polymerizable compound, polymer, polymerizable composition, film, and half mirror for displaying projection image

Номер: US20170009138A1
Автор: Daisuke Hayashi, Hiroshi Matsuyama, Masaru Yoshikawa, Shunya Katoh, Yuki Nakazawa
Принадлежит: Fujifilm Corp

The present invention provides a polymerizable compound denoted by Formula (I): in the formula, Z 1 and Z 2 represent an arylene group, and the like, m represents 1 or 2, n represents an integer of 0 or 1, and when m is 2, n is 0, L 1 , L 2 , L 3 , and L 4 each independently represent a linking group such as —C(═O)O— and —OC(═O)—, T 3 represents -Sp 4 -R 4 , X represents —O—, and the like, r represents 1 to 4, Sp 1 , Sp 2 , Sp 3 , Sp 4 , and Sp 5 each independently represent a single bond or a linking group, R 1 and R 2 each independently represent a polymerizable group, and R 3 , R 4 , and R 5 each independently represent a hydrogen atom, a polymerizable group, or the like; a polymerizable composition containing the polymerizable compound described above; a film formed of the polymerizable composition described above; and a half mirror for displaying a projection image including the film described above.

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Номер записи: 23
14-01-2016 дата публикации

PROTOTYPICAL BRAIN PROTECTIVE ACTIVITY OF TETRAHYDRO-N-METHYL-2,2-DIPHENYL-3-FURANOMETHANAMINE (AE37MET)

Номер: US20160009674A1
Автор: Vamvakides Alexandre
Принадлежит:

Tetrahydro-N-methyl-2,2-diphenyl-3-furanomethanamine (AE37Met) is a highly selective ligand of the extrasynaptic NMDA receptors, of the M2 muscarinic autoreceptors and of the sigma-1 (σ1) receptors, with prototypical brain, preventive and therapeutical, protective activity. This invention concerns the prototypical profile of AE37Met and its pharmaceutically acceptable salts, with cytoprotective activity, more specifically for brain glial cells and neurons, against the neuro-degenerative diseases (e.g. Alzheimer's, Huntington's and Parkinson's diseases, depression, brain ischemia/hypoxia, traumatic brain injury and epilepsy), by the highly selective antagonisms, exerced by AE37Met, on the extrasynaptic NMDA glutamatergic receptors [eNMDA(−)] and on the M2 muscarinic cholinergic autoreceptors [M2(−)], associated with a highly selective sigma-1 agonism [σ1(+)]. The above prototypical profile was observed only with AE37Met between the other family members (AE14, AE37 and their enantiomers). 1. A compound comprising an effective amount of a compound selected from the group consisting of tetrahydro-N-methyl-2 ,2-diphenyl-3-furanomethanamine , pharmaceutically acceptable salts of tetrahydro-N-methyl-2 ,2-diphenyl-3-furanomethanamine , enantiomers of tetrahydro-N-methyl-2 ,2-diphenyl-3-furanomethanamine , and combinations thereof , said compound being as prototypical selective antagonists of extrasynaptic N-methyl-D-aspartate receptors , [e NMDA (−)] , of M2 muscarinic autoreceptors of cholinergic neurons [M2 (−)] and selective agonist of sigma-1 receptors [σ1 (+)] , with brain preventive and therapeutical , protective activity.2. A pharmaceutical composition comprising an effective amount of a compound and at least one pharmaceutically acceptable excipient , said compound being selected from the group consisting of tetrahydro-N-methyl-2 ,2-diphenyl-3-furanomethanamine , pharmaceutically acceptable salts of tetrahydro-N-methyl-2 ,2-diphenyl-3-furanomethanamine , enantiomers ...

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Номер записи: 24
10-01-2019 дата публикации

Novel Compounds

Номер: US20190010135A1
Автор: Ebere F. IGBOKO, Feng Ren, Hongfu Lu, Lindong Zhu, Paul Bryan Wren, Ting Yang, Weichun Chen, Xichen Lin, Zhongmiao Xu
Принадлежит: GlaxoSmithKline Intellectual Property Development Ltd

The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.

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Номер записи: 25
09-01-2020 дата публикации

CONVERSION OF BIOMASS

Номер: US20200010440A1
Автор: Cooper Christopher, Khan Jihan, Masterman Thomas Craig, Medoff Marshall
Принадлежит:

Biomass feedstocks (e.g., plant biomass, animal biomass, and municipal waste biomass) are processed to produce useful products, such as fuels. For example, systems are described that can convert feedstock materials to a sugar solution, especially, xylose, which can then be chemically converted to furfural and furfural-derived products. 1. A method for processing biomass , the method comprising:irradiating biomass to reduce the recalcitrance of the biomass;saccharifying the irradiated biomass with one or more enzymes to produce a first sugar composition comprising xylose and glucose;fermenting the first sugar composition to produce a second sugar composition comprising xylose and glucose, wherein the concentration of xylose in the second sugar composition is increased relative to the first sugar composition;isolating the xylose from the second sugar composition;converting the isolated xylose to furfural; andconverting the furfural to a furoic acid.2. The method of claim 1 , wherein isolating the xylose from the second sugar composition comprises one or more isolation method selected from the group consisting of distillation claim 1 , crystallization claim 1 , precipitation claim 1 , sedimentation claim 1 , chromatography claim 1 , centrifugation claim 1 , settling claim 1 , sedimentation claim 1 , and floatation.3. The method of claim claim 1 , 1 wherein the biomass comprises one or more of paper claim 1 , paper product claim 1 , wood claim 1 , wood-related material claim 1 , particle board claim 1 , grass claim 1 , rice hulls claim 1 , bagasse claim 1 , cotton claim 1 , jute claim 1 , hemp claim 1 , flax claim 1 , bamboo claim 1 , wheat straw claim 1 , sisal claim 1 , abaca claim 1 , straw claim 1 , corn cobs claim 1 , corn stover claim 1 , coconut hair claim 1 , algae claim 1 , seaweed claim 1 , altered cellulose claim 1 , regenerated cellulose claim 1 , microbial material claim 1 , municipal waste claim 1 , waste from paper processing claim 1 , newspaper claim 1 , ...

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Номер записи: 26
19-01-2017 дата публикации

PHOSPHONIC ACID CATALYST IN DEHYDRATIVE CYCLIZATION OF 5 AND 6 CARBON POLYOLS WITH IMPROVED COLOR AND PRODUCT ACCOUNTABILITY

Номер: US20170015676A1
Автор: Hagberg Erik, Stensrud Kenneth
Принадлежит:

A process for preparing materials derived from sugar alcohols such that the dehydration products exhibit better accountability and improved color to water-clear or near water-white appearance is described. In particular, the process involves employing a reducing Brønsted acid (e.g., phosphonic acid) for the catalysis of sugar alcohols to their corresponding dehydrated-cyclized products. 1. A method for preparing a cyclic dehydration product from 5 or 6 carbon polyols comprising: reacting a 5 or 6 carbon polyol with a reducing Brønsted acid catalyst in a reaction mixture , at a temperature and for a time sufficient to convert said 5 or 6 carbon polyol to corresponding cyclic dehydration products in a product mixture , wherein at least 70% of the 5 or 6 carbon polyol is converted to the corresponding cyclic dehydration products.2. The method according to claim 1 , further comprising purifying said dehydration products by at least a means selected from the group consisting of chromatography claim 1 , crystallization claim 1 , and distillation.3. The method according to claim 1 , wherein said reducing Brønsted acid catalyst is phosphonic acid.4. The method according to claim 1 , wherein said product mixture has an opacity and color appearance that ranges from translucent claim 1 , with a medium brown to light honey color claim 1 , to transparent claim 1 , clear or near water-white color after completion of said reaction time claim 1 , without being subject to a purifying or decolorizing operation.5. The method according to claim 3 , wherein said product mixture exhibits a color appearance after completion of said reaction time that is lighter and more translucent relative to a product mixture prepared using sulfuric acid catalyst at a catalyst load of ≧0.1 mol % claim 3 , instead of the phosphonic acid catalyst for the same time and temperature.6. The method according to claim 3 , wherein said product mixture exhibits reduced levels of color body formation or ...

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Номер записи: 27
21-01-2016 дата публикации

Pretreatment and fractionation of lignocellulosic biomass

Номер: US20160017540A1
Автор: Anantharam Prasad Dadi, Praveen Paripati
Принадлежит: Suganit Systems Inc

Method and apparatus for enhanced production of sugars and lignin via fractionation of lignocellulosic biomass through ionic liquid pretreatment and mild alkaline treatment. The resulting biomass is easily fractionated and amenable to efficient and rapid enzymatic hydrolysis or acid hydrolysis and catalytic conversion to valuable products with high recovery of the enzymes used in the hydrolysis.

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Номер записи: 28
26-01-2017 дата публикации

Substituted 3-phenylpropylamine derivatives for the treatment of ophthalmic diseases and disorders

Номер: US20170022180A1
Автор: Feng Hong, Mark W. Orme, Ryo Kubota, Vladimir A. Kuksa
Принадлежит: Acucela Inc

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

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Номер записи: 29
04-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160029635A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R1 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.3. A molecule according to wherein R2 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , haloethyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , halo(C)alkyl claim 1 , methoxy claim 1 , ethoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , (C)alkoxy claim 1 , halomethoxy claim 1 , haloethoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , halo(C)alkoxy claim 1 , and halo(C)alkoxy.4. A molecule according to wherein R3 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , NO claim 1 , methyl claim 1 , ethyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , (C)alkyl claim 1 , halomethyl claim 1 , ...

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Номер записи: 30
04-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160029636A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 15-. (canceled)6. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).7. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 38 , 1 claim 38 ,2-dichloropropane claim 38 , 1 claim 38 ,3-dichloropropene claim 38 , 1-methylcyclopropene claim 38 , 1-naphthol claim 38 , 2-(octylthio)ethanol claim 38 , 2 claim 38 ,3 claim 38 ,5-tri-iodobenzoic acid claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-dimethylammonium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-lithium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-potassium claim 38 , 2 claim 38 ,3 claim 38 ,6-TBA-sodium claim 38 , 2 claim 38 ,4 claim 38 ,5-T claim 38 , 2 claim 38 ,4 claim 38 ,5-T-2-butoxypropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-2-ethylhexyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-3-butoxypropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-TB claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butometyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butotyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-butyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isobutyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isoctyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-isopropyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-methyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-pentyl claim 38 , 2 claim 38 ,4 claim 38 ,5-T-sodium claim 38 , 2 claim 38 ,4 claim 38 ,5-T-triethylammonium claim 38 , 2 claim 38 ,4 claim 38 ,5-T-trolamine claim 38 , 2 claim 38 ,4-D claim 38 , 2 claim 38 , ...

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Номер записи: 31
02-02-2017 дата публикации

SYNTHESIS OF R-GLUCOSIDES, SUGAR ALCOHOLS, REDUCED SUGAR ALCOHOLS, AND FURAN DERIVATIVES OF REDUCED SUGAR ALCOHOLS

Номер: US20170029393A1
Автор: Ma Chi-Cheng, Martin Kevin, Stensrud Kenneth
Принадлежит:

Disclosed herein are methods for synthesizing 1,2,5,6-hexanetetrol (HTO), 1,6 hexanediol (HDO) and other reduced polyols from C5 and C6 sugar alcohols or R glycosides. The methods include contacting the sugar alcohol or R-glycoside with a copper catalyst, most desirably a Raney copper catalyst with hydrogen for a time, temperature and pressure sufficient to form reduced polyols having 2 to 3 fewer hydoxy groups than the starting material. When the starting compound is a C6 sugar alcohol such as sorbitol or R-glycoside of a C6 sugar such as methyl glucoside, the predominant product is HTO. The same catalyst can be used to further reduce the HTO to HDO. 1. A method of making 2 ,5-bis(hydroxymethyl)tetrahydrofuran , comprising: contacting a mixture comprising 1 ,2 ,5 ,6-hexanetetrol with an acid catalyst selected from the group consisting of sulfuric acid , phosphonic acid , carbonic acid and a water tolerant non-Bronsted Lewis acid for a time and at a temperature and a pressure sufficient to convert the 1 ,2 ,5 ,6-hexanetetrol to 2 ,5 bis(hydroxymethyl)tetrahydrofuran.2. The method of claim 1 , wherein the non-Bronsted Lewis acid is a triflate compound.3. The method of claim 2 , wherein the triflate compound is selected from the group consisting of bismuth triflate claim 2 , scandium triflate claim 2 , and sulfuric acid.4. (canceled)5. (canceled)6. The method of wherein the wherein the mixture is contacted with the catalyst under vacuum pressure of less than 0.4 psi.7. The method wherein the acid catalyst is sulfuric acid.8. The method of claim 1 , wherein the acid catalyst is the non-Bronsted Lewis acid.9. The method of claim 1 , wherein the acid catalyst is carbonic acid formed by adding of COto the reaction mixture at a pressure sufficient to form carbonic acid.10. (canceled)11. (canceled)12. The method of wherein the mixture further includes 1 claim 1 ,4 claim 1 ,5 hexanetriol and contacting with the acid catalyst further converts the 1 claim 1 ,4 claim 1 ,5 ...

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Номер записи: 32
02-02-2017 дата публикации

Chelate-controlled diastereoselective hydrogenation with heterogeneous catalyst

Номер: US20170029394A1
Автор: Craig Anderson, David Dunn, Howard Winston Tyrrell SUTTON, John Ing Chuan DALY, Lian HUTCHINGS, Matthew Richard GIBBINGS, Patrice Georges Antonin RIBIERE, Sergio Aaron GAMBOA MARTINEZ, Simon Jonathon Grant, Yulia ROGAN
Принадлежит: Thomas Swan and Co Ltd

A catalyst, method of using, and use of a hydrogenation catalyst, preferably palladium on a support, preferably alumina or activated charcoal support. This in the presence of lithium salts, with salts such as the borates being preferred. This provides hydrogenation of precursors to give rise to a stereoselective, such as diastereoselective bias in the product of alkene hydrogenation using the catalyst. This equation, using the preferred substrate, best illustrates the invention:

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Номер записи: 33
02-02-2017 дата публикации

SYNTHESIS OF DERIVATIVES OF DICARBAMATES FROM REDUCTION PRODUCTS OF 2-HYDROXYMETHYL-5-FURUFURAL (HMF)

Номер: US20170029395A1
Автор: Stensrud Kenneth
Принадлежит:

Dicarbamates of the reduction products of 2-hydroxymethyl-5-furfural (HMF) and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The dicarbamates of HMF-reduction products can serve as precursor materials from which various derivative compounds can be synthesized. 2. A chemical compound derived from at least one of the precursor chemical compounds according to claim 1 , said derived chemical compound is a polymer containing said precursor chemical compound as a substituent.5. The method according to claim 4 , wherein said Lewis acid triflate is water-tolerant. The present application claims benefit of priority of U.S. patent application Ser. No. 14/781,364, filed Sep. 20, 2015, which claims priority from International Application No. PCT/US2014/037047, filed May 7,2014, which claims priority from U.S. Provisional Application No. 61/833,951, filed Jun. 12, 2013, the contents of each are herein incorporated.The present invention relates to a synthesis of precursor compounds for polymers. In particular, the present invention pertains to a method for preparing dicarbamates of the reduction products of 2-hydroxymethyl-5-furfural (HMF) (i.e, furan-2,5-dimethanol (FDM) and bis(hydroxymethyl)-tetrahydrofuran (bHMTHF)), and derivative compounds of such dicarbamates.Traditionally, polymers and commodity chemicals have been prepared from petroleum-derived feedstock. As petroleum supplies have become increasingly costly and difficult to access, interest and research has increased to develop renewable or “green” alternative materials from biologically-derived sources for chemicals that will serve as commercially acceptable alternatives to conventional, petroleum-based or -derived counterparts, or for producing the same materials as produced from fossil, non-renewable sources.Carbohydrates or sugars are ubiquitous in agricultural ...

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Номер записи: 34
04-02-2016 дата публикации

SYNTHESIS OF ISOHEXIDE DICARBAMATES AND DERIVATIVES THEREOF

Номер: US20160031842A1
Автор: Stensrud Kenneth
Принадлежит:

Dicarbamates of the reduction products of 2-hydroxymethyl-5-furfural (HMF) and a method of preparing the same are described. The method involves reacting a mixture of an isohexide and a cynate salt in a non-aqueous solvent, with a miscible acid having a pKa of about 3.7 or less. The dicarbamates of HMF-reduction products can serve as precursor materials from which various derivative compounds can be synthesized. 1. A process for preparing dicarbamates of reduction products of HMF , the process comprising: providing a mixture of a HMF-reduction product with a cyanate salt in an inert organic solvent , reacting said mixture with an acid having a pK≦3.7.2. The process according to claim 1 , wherein said acid is added to said reaction mixture of HMF-reduction products at a rate of about 0.03-0.1 stoichiometric equivalents per minute.3. The process according to claim 1 , wherein said HMF-reduction product is at least: a) FDM and b) THF-diols.4. The process according to claim 1 , wherein said organic solvent at least: methylene chloride claim 1 , chloroform claim 1 , carbon tetrachloride claim 1 , benzene claim 1 , toluene claim 1 , xylenes claim 1 , linear and/or branched alkanes claim 1 , tetrahydrofuran claim 1 , 1 claim 1 ,4-dioxane claim 1 , dimethylsulfoxide claim 1 , acetonitrile claim 1 , dimethylformamide claim 1 , acetic acid claim 1 , HMPT claim 1 , nitromethane claim 1 , pyridine claim 1 , N-methyl pyrolidinone claim 1 , dimethylacetamide claim 1 , ethyl acetate claim 1 , acetone claim 1 , methyl tert-butyl ether claim 1 , diethyl ether.5. The process according to claim 1 , wherein said cyanate salt having a cationic counter-ion selected from the group consisting of: Na claim 1 , K claim 1 , Li claim 1 , Ag claim 1 , Hg claim 1 , Al claim 1 , Ca claim 1 , Mg claim 1 , Pb claim 1 , Sn claim 1 , Ti claim 1 , Ni claim 1 , Cs claim 1 , Rb claim 1 , Cu claim 1 , Zn claim 1 , Cd claim 1 , In claim 1 , Co claim 1 , Ga claim 1 , Ba claim 1 , Pd claim 1 , Pt claim 1 , ...

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Номер записи: 35
05-02-2015 дата публикации

Compositions containing tetrahydrofurfuryl and/or alkyl-substituted tetrahydrofurfuryl esters of citric acid

Номер: US20150033985A1
Автор: Kevin M. Lewandowski, Maureen A. Kavanagh
Принадлежит: 3M Innovative Properties Co

Compositions containing tetrahydrofurfuryl and/or alkyl-substituted tetrahydrofurfuryl esters of citric acid are provided. These esters of citric acid can be formed from renewable materials and can be used, for example, as plasticizers for various polymeric materials. The tetrahydrofurfuryl and/or alkyl-substituted tetrahydrofurfuryl esters of citric acid typically have a low odor, have good compatibility with a variety of polymeric materials, and can be used at temperatures often encountered during hot melt processing of polymeric materials.

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Номер записи: 36
31-01-2019 дата публикации

AMINE-CONTAINING CYCLIC HYDROFLUOROETHERS AND METHODS OF USING THE SAME

Номер: US20190031646A1
Автор: Bulinski Michael J., Costello Michael G., Lamanna William M., Smith Sean M., Toso Nicholas A.
Принадлежит:

Described herein is a cyclic fluorinated compound of formula (I) where: L is O, CH, or a covalent bond; X is selected from F or CF, and Y is selected from H, F, or CF, wherein when X is CFthen Y is F and when Y is CFthen X is F, each Ris independently selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from O, N, or combinations thereof; or the two Rgroups are bonded together to form a fluorinated ring structure comprising 4-8 carbon atoms and optionally comprising at least one catenated atom selected from O, N, or combinations thereof; the —CFZ—CHAQ group is bonded to a ring carbon that is alpha to at least one O atom of the ring; A is selected from F, or CF; Z is selected from H, F, or CF; and Q is selected from (i) a F atom, (ii) a Cl atom, (iii) a linear, cyclic, or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from O, N, or combinations thereof, or (iv) a G(R)group, where G is an O atom or a N atom wherein: when Q is a Cl atom, then Z and A are F atoms; when G is O then e is 1, Z is H, F, or CF; A is F; and Ris a linear or branched perfluorinated alkyl group comprising 1-10 carbon atoms and optionally comprising at least one catenated atom selected from O, N, or combinations thereof; when G is N then e is 2, and each Rgroup is independently a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated atom selected from O, N, or combinations thereof or the two Rgroups are bonded together to form a fluorinated ring structure comprising 4-8 carbon atoms and optionally comprising at least one catenated atom selected from O, N, or combinations thereof, with the proviso that when A is CFthen Z is F, and when Z is CFthen A is F. 2. The cyclic fluorinated compound of claim 1 , wherein Q=N(R).3. The cyclic fluorinated compound ...

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Номер записи: 37
11-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160037778A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butomethyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

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Номер записи: 38
11-02-2016 дата публикации

Pesticidal compositions and processes related thereto

Номер: US20160037779A1
Автор: Akshay PATNY, Gerald B. Watson, James E. Hunter, Joshodeep Boruwa, Pravin S. IYER, William C. Lo
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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Номер записи: 39
06-02-2020 дата публикации

A19-144, A2-73 and Certain Anticholinesterase Inhibitor Compositions and Method for Anti-Seizure Therapy

Номер: US20200038365A1
Автор: Durrant Cameron, MISSLING Christopher U.
Принадлежит: ANAVEX LIFE SCIENCES CORP.

This invention concerns a dosage form comprising a therapeutically effective amount of A19-144 or A2-73 and a therapeutically effective amount of at least one AED. This invention further encompasses a method of treating a subject in need of such treatment comprising administering a therapeutically effective amount of A19-144 or A2-73 in conjunction with an therapeutically effective amount of an AED. 1. A method of treating seizures in a subject in need of such treatment comprising administering an therapeutically effective amount of A19-144 or a combination of A19-144 and A2-73 in conjunction with a sub-MED amount of an AED.2. The method of wherein said administering of A19-144 or the combination of A19-144 and A2-73 in conjunction with a sub-MED amount of an AED is co-timely.3. The method of wherein said administering of A19-144 or the combination of A19-144 and A2-73 in conjunction with a sub-MED amount of an AED is coordinated.4. The method of wherein the at least one AED is selected from the group consisting of donepezil claim 1 , memantine claim 1 , galantamine claim 1 , and rivastigmine claim 1 , wherein the sub-MED dose of donepezil is 0.5 mg or less claim 1 , the sub-MED dose of memantine is 0.5 mg or less claim 1 , the sub-MED dose of galantamine is 6 mg or less; and the sub-MED dose of rivastigmine is about 0.5 mg.5. The method of wherein the sub-MED dose and the at least one AED are selected from the group consisting of:less than about 8 mg/day of acetazolamide;less than about 1.5 mg/day for of Clonazepam for an adult, less than about 0.01 mg/kg/day of Clonezepam for a child up to 10 years of age or 30 kg of body weight;less than about 30 (mg) of Clorazepate;less than about 0.1 mg/kg of Lorazepam;less than about 0.2 mg/kg of Midazolam;less than about 7.5 mg/day of Carbamazepine;less than about 0.2 mg/kg of Diazepam;less than about 30 mg/day of Chlordiazepoxide;less than about 5 mg/day for body weight 30 kg or less, and less than about 10 mg/day for body ...

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Номер записи: 40
12-02-2015 дата публикации

SULFONIUM COMPOUNDS, THEIR PREPARATION AND USE

Номер: US20150044509A1
Автор: Kunimoto Kazuhiko, Kura Hisatoshi
Принадлежит: BASF SE

Compounds of the formula (I), (Ia) or (Ib) wherein A, and A is for example (II) is 1 or 2; X is C-Calkylene or CO; Y is for example O, O(CO), O(CO)O, Ris for example hydrogen, d-dsalkyl, C-Ccycloalkyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or C-Cheteroaryl, all of which optionally are substituted; Rand Rfor example are C-Chaloalkylene which is optionally substituted, or Rand Rare phenylene, which optionally is substituted; Ris a group (A) or a group (B); Rand Rfor example are C-Calkyl; or Rand Ror Rand Rtogether form a straight-chain C-Calkylene, Rand Rtogether form a straight-chain C-Calkylene; R, R, Rand Rifor example are C-Calkyl; M for example is C-Calkylene, C-Calkenylene, C-Calkynylene; Rand Rare for example hydrogen, C-Calkyl; R, R, R, Rand Rare for example hydrogen, C-Calkyl, C-Calkenyl, C-Ccycloalkyl, or two radicals Rand R, Rand R, Rand Rand/or Rand Rtogether form a straight-chain C-Calkylene, or Rand Rtogether form 1,2-phenylene, Rand Rfor example are hydrogen, C-Calkyl; R, Rand Rfor example are hydrogen, C-Calkyl; are suitable as thermo-acid generators. 3: A heat-curable composition comprising(a) at least one compound which is capable of undergoing cationic polymerization; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(b) at least one compound of formula I, Ia or Ib according to .'}4: The heat-curable composition according to claim 3 , wherein the compound which is capable of undergoing cationic polymerization has at least one group selected from the group consisting of an epoxy group claim 3 , oxetane group and vinyl ether group.5: The heat-curable composition according to claim 3 , where the compound which is capable of undergoing cationic polymerization is an epoxy resin.6: The heat-curable composition according to claim 3 , further comprising at least one component selected from the group consisting of solvent claim 3 , reactive diluents claim 3 , photoinitiators claim 3 , photoacid generators claim 3 , pigments ...

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Номер записи: 41
18-02-2021 дата публикации

A19-144, A2-73 and Certain Anticholinesterase Inhibitor Compositions and Method for Anti-Seizure Therapy

Номер: US20210046038A1
Автор: Durrant Cameron, MISSLING Christopher U.
Принадлежит: ANAVEX LIFE SCIENCES CORP.

This invention concerns a dosage form comprising a therapeutically effective amount of A19-144 or A2-73 and a therapeutically effective amount of at least one AED. This invention further encompasses a method of treating a subject in need of such treatment comprising administering a therapeutically effective amount of A19-144 or A2-73 in conjunction with any therapeutically effective amount of an AED. 1. A dosage form comprising a therapeutically effective amount of an active , (i) tetrahydro-N-methyl-2,2-diphenyl-3-furanomethanamine, or a pharmaceutically acceptable salt thereof;', '(ii) tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine, or a pharmaceutically acceptable salt thereof; or a combination of (i) and (ii); and, 'wherein the active is'}wherein the therapeutically effective amount is the amount to elicit pharmacological response of reduction in the number of seizures.2. The dosage form of claim 1 , wherein the therapeutically effective amount is 0.5-10 mg/day.3. The dosage form of claim 1 , wherein the dosage form further comprises a pharmaceutical excipient suitable for oral or parenteral administration.4. The dosage form of claim 1 , further comprising a sub-MED amount of at least one anti-epilepsy drug (AED).5. The dosage form of claim 4 , wherein the sub-MED amount of the at least one anti-epilepsy drug (AED) is selected from the group consisting ofless than 5 mg/day of donepezil;less than 0.5 mg/day of memantine;less than 8 mg/day of galantamine;less than 3 mg/day of rivastigmine;less than about 8/day mg of acetazolamide;less than about 1.5 mg/day of Clonazepam for an adult, less than about 0.01 mg/kg/day of Clonazepam for a child up to 10 years of age or 30 kg of body weight;less than about 30 mg/day of Clorazepate;less than about 0.1 mg/kg/day of Lorazepam;less than about 0.2 mg/kg/day of Midazolam;less than about 7.5 mg/day of Carbamazepine;less than about 0.2 mg/kg/day of Diazepam;less than about 30 mg/day of Chlordiazepoxide;less than about ...

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Номер записи: 42
18-02-2016 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20160044925A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 140-. (canceled)41. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).42. A composition according to further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 73 , 1 claim 73 ,2-dichloropropane claim 73 , 1 claim 73 ,3-dichloropropene claim 73 , 1-methylcyclopropene claim 73 , 1-naphthol claim 73 , 2-(octylthio)ethanol claim 73 , 2 claim 73 ,3 claim 73 ,5-tri-iodobenzoic acid claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-dimethylammonium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-lithium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-potassium claim 73 , 2 claim 73 ,3 claim 73 ,6-TBA-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-2-ethylhexyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-3-butoxypropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-TB claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butometyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butotyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-butyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isobutyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isoctyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-isopropyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-methyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-pentyl claim 73 , 2 claim 73 ,4 claim 73 ,5-T-sodium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-triethylammonium claim 73 , 2 claim 73 ,4 claim 73 ,5-T-trolamine claim 73 , 2 claim 73 ,4-D claim 73 , 2 claim ...

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Номер записи: 43
16-02-2017 дата публикации

SYNTHESIS OF R-GLUCOSIDES, SUGAR ALCOHOLS, REDUCED SUGAR ALCOHOLS, AND FURAN DERIVATIVES OF REDUCED SUGAR ALCOHOLS

Номер: US20170044123A1
Автор: Ma Chi-Cheng, Stensrud Kenneth
Принадлежит:

Disclosed herein are methods for synthesizing 1,2,5,6-hexanetetrol (HTO), 1,6 hexanediol (HDO) and other reduced polyols from C5 and C6 sugar alcohols or R glycosides. The methods include contacting the sugar alcohol or R-glycoside with a copper catalyst, most desirably a Raney copper catalyst with hydrogen for a time, temperature and pressure sufficient to form reduced polyols having 2 to 3 fewer hydoxy groups than the starting material. When the starting compound is a C6 sugar alcohol such as sorbitol or R-glycoside of a C6 sugar such as methyl glucoside, the predominant product is HTO. The same catalyst can be used to further reduce the HTO to HDO. 1. A method of making a reduced sugar alcohol including at least one member selected from the group consisting of 1 ,2 ,5-pentanetriol , 1 ,4 ,5-hexanetriol , 1 ,2 ,6-hexanetetrol , and 1 ,2 ,5 ,6 hexanetetrol , comprising ,contacting a solution comprising water and at least 20% wt/wt of a starting compound selected from the group consisting of a sugar alcohol and a R-glycoside of a sugar, wherein R is a methyl or ethyl group, with hydrogen and a Raney copper catalyst for a time and at a temperature and pressure sufficient to produce a mixture containing one or more of the reduced sugar alcohols with a combined selectively yield of at least 50% mol/mol.2. The method of claim 1 , wherein the starting compound is a C6 sugar alcohol selected from the group consisting of sorbitol claim 1 , mannitol claim 1 , ididtol claim 1 , dulcitol claim 1 , talitol claim 1 , and 1 claim 1 ,4-sorbitan and the reduced sugar alcohol is at least one of 1 claim 1 ,4 claim 1 ,5-hexanetriol and 1 claim 1 ,2 claim 1 ,5 claim 1 ,6-hexanetetrol.3. The method of wherein the starting compound is a methyl or ethyl glucoside and reduced sugar alcohol is at least one of 1 claim 1 ,4 claim 1 ,5-hexanetriol and 1 claim 1 ,2 claim 1 ,5 claim 1 ,6-hexanetetrol.4. The method of claim 1 , wherein the temperature is 175° C. to 250° C. and the pressure is ...

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Номер записи: 44
16-02-2017 дата публикации

BIOREFINING COMPOUNDS AND ORGANOCATALYTIC UPGRADING METHODS

Номер: US20170044124A1
Автор: CHEN Eugene Y., LIU Dajiang
Принадлежит: COLORADO STATE UNIVERSITY RESEARCH FOUNDATION

The invention provides new methods for the direct umpolung self-condensation of 5-hydroxymethylfurfural (HMF) by organocatalysis, thereby upgrading the readily available substrate into 5,5′-di(hydroxymethyl) furoin (DHMF). While many efficient catalyst systems have been developed for conversion of plant biomass resources into HMF, the invention now provides methods to convert such nonfood biomass directly into DHMF by a simple process as described herein. The invention also provides highly effective new methods for upgrading other biomass furaldehydes and related compound to liquid fuels. The methods include the organocatalytic self-condensation (umpolung) of biomass furaldehydes into (C-C)furoin intermediates, followed by hydrogenation, etherification or esterification into oxygenated biodiesel, or hydrodeoxygenation by metal-acid tandem catalysis into premium hydrocarbon fuels. 2. The compound of wherein each Ris independently H claim 1 , OH claim 1 , halo claim 1 , alkoxy claim 1 , or acyloxy.3. The compound of wherein Ris OH claim 1 , halo claim 1 , alkoxy claim 1 , or acyloxy.4. The compound of wherein each Ris independently H claim 1 , OH claim 1 , halo claim 1 , alkoxy claim 1 , or acyloxy; and Ris OH claim 1 , halo claim 1 , alkoxy claim 1 , or acyloxy.9. The compound of wherein Ris H claim 8 , OH claim 8 , halo claim 8 , alkoxy claim 8 , or acyloxy.10. The compound of wherein Ris H claim 8 , OH claim 8 , halo claim 8 , alkoxy claim 8 , or acyloxy.11. The compound of wherein Ris H claim 8 , OH claim 8 , halo claim 8 , alkoxy claim 8 , or acyloxy; and Ris H claim 8 , OH claim 8 , halo claim 8 , alkoxy claim 8 , or acyloxy.14. A composition comprising a compound of and one or more (C-C)alkanes.15. The composition of wherein the (C-C)alkane is a (C-C)alkane.16. A composition comprising a compounds of and one or more (C-C)alkanes.17. The composition of wherein the (C-C)alkane is a (C-C)alkane.19. The method of wherein the compound of Formula I is 5 claim 18 ,5′- ...

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Номер записи: 45
15-02-2018 дата публикации

SULFONYLUREAS AND RELATED COMPOUNDS AND USE OF SAME

Номер: US20180044287A1
Автор: "ONeill Luke", COLL Rebecca, Cooper Matthew, ROBERTSON Avril, SCHRODER Kate
Принадлежит:

The present invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity in the inhibition of activation of the NLRP3 inflammasome. Such compounds are useful in the treatment of a wide range of disorders in which the inflammation process, or more specifically the NLRP3 inflammasome, have been implicated as being a key factor. 2. The compound of wherein Ris selected from the group consisting of Cor Ccycloalkyl claim 1 , 5-membered or 6-membered heteroaryl claim 1 , bicyclic heteroaryl wherein at least one ring is heteroaryl claim 1 , phenyl claim 1 , biphenyl claim 1 , phenylheterocyclyl claim 1 , 5-membered or 6-membered heterocyclyl claim 1 , and heterocyclylcycloalkyl claim 1 , all of which may be optionally substituted.3. The compound of or wherein Ris selected from the group consisting of pyrazole claim 1 , furan claim 1 , tetrahydrofuran claim 1 , tetrahydropyran claim 1 , pyran claim 1 , pyrrolidine claim 1 , pyrrole claim 1 , triazole claim 1 , tetrazole claim 1 , imidazole claim 1 , pyridine claim 1 , morpholine claim 1 , piperazine claim 1 , piperidine claim 1 , substituted phenyl claim 1 , phenylheteroaryl claim 1 , phenylheterocyclyl claim 1 , biphenyl claim 1 , quinoline claim 1 , isoquinoline claim 1 , naphthyl claim 1 , pyrazine and pyrimidine claim 1 , all of which may be optionally substituted as appropriate.4. The compound of any one of the preceding claims wherein Ris 5-membered heterocyclyl or heteroaryl claim 1 , each of which may be optionally substituted claim 1 , comprising at least one ring heteroatom selected from N claim 1 , O and S.5. The compound of wherein Ris 5-membered nitrogen heterocyclyl or 5-membered nitrogen heteroaryl claim 4 , each of which may be optionally substituted.6. The compound of or wherein Ris 5-membered heterocyclyl or 5-membered heteroaryl claim 4 , each of which may be optionally substituted claim 4 , comprising at least two ring nitrogen atoms.7. ...

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Номер записи: 46
03-03-2022 дата публикации

New Anionic Surfactants And Detergents And Cleaning Agents Containing Same

Номер: US20220064568A1
Автор: Hausoul Peter, Kipshagen Lukas, Klemmer Anna, Kropf Christian, Palkovits Regina, Schulz Alexander
Принадлежит: Henkel AG & Co. KGaa

An anionic surfactant of general formula (I) in which n and m are, independently of one another, numbers from 0 to 17 and 2 Подробнее

Номер записи: 47
25-02-2021 дата публикации

TRNA SYNTHETASE INHIBITORS

Номер: US20210053997A1
Автор: Baidin Vadim, Kahne Daniel E.
Принадлежит:

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis. 215-. (canceled)1726-. (canceled)28. The compound of claim 27 , wherein at least three of R claim 27 , R claim 27 , R claim 27 , and Rare H.29. The compound of claim 27 , wherein R claim 27 , R claim 27 , Rand Rare each H.30. The compound of claim 27 , wherein Ris H.31. The compound of claim 27 , wherein Ris (C-C)alkyl.32. (canceled)33. The compound of claim 27 , wherein Ris optionally substituted cyclohexyl or cyclohexenyl.34. The compound of claim 27 , wherein Ris optionally substituted cyclohexyl.35. The compound of claim 27 , wherein Ris H.36. The compound of claim 27 , wherein R claim 27 , independently for each occurrence claim 27 , is selected from H and (C-C)alkyl.37. The compound of claim 27 , wherein each occurrence of Ris H.38. The compound of claim 27 , wherein each occurrence of Ris methyl claim 27 , or one Ris methyl or ethyl claim 27 , and the other Ris H.39. The compound of claim 27 , wherein one Ris selected from one of (a)-(d):(a) optionally substituted —C(O)alkyl;{'sub': 3', '10, '(b) optionally substituted —C(O)NH—(C-C)cycloalkyl;'}{'sub': 1', '8, '(c) optionally substituted (C-C)alkyl; or'}(d) optionally substituted cycloalkyl, optionally substituted aryl, or optionally substituted heterocyclyl.40. The compound of claim 39 , wherein one Ris —C(O)CH(NH)CHCHMe.41. (canceled)42. The compound of claim 39 , wherein one Ris —C(O)NH— cyclohexyl claim 39 , optionally substituted with methyl.43. (canceled) .44. The compound of claim 39 , wherein one Ris selected from —CHCH(OH)CHOH claim 39 , —CHC(O)NHCHCOOH claim 39 , —CHC(O)NHCHCOOH claim 39 , —CHCHOMe claim 39 , —CHCOOH claim 39 , —CH(Me)COOH claim 39 , and —CH-furanyl.45. (canceled) . ...

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Номер записи: 48
03-03-2016 дата публикации

POLYMERIZABLE COMPOSITION COMPRISING AN OXIME SULFONATE AS THERMAL CURING AGENT

Номер: US20160060214A1
Автор: Kunimoto Kazuhiko, Kura Hisatoshi, MATSUOKA Yuki, Sameshima Kaori
Принадлежит: BASF SE

The present invention relates to a polymerizable composition comprising at least one ethylenically unsaturated, polymerizable compound and at least one oxime sulfonate compound of the formula I 144-. (canceled)47. The compound of formula I according to claim 45 , where X is S or NRand{'sup': 14', '6', '14a', '8', '9', '10', '11', '4', '5', '6', '7', '8', '9', '10', '11, 'sub': 1', '12', '3', '8', '1', '8', '1', '4', '2, 'claim-text': [{'sub': 2', '12', '3', '8', '1', '8', '1', '4', '2, 'sup': 6', '14a', '8', '9', '10', '11', '4', '5', '6', '7', '8', '9', '10', '11, 'C-C-alkenyl, which may be interrupted by one or more O, S, NRor CO and/or may be substituted by one or more identical or different radicals Rselected from CN, COR, COOR, CONRR, phenyl and C-C-cycloalkyl which may interrupted by one or two CO groups and where the two last-mentioned radicals may be substituted by one or more identical or different radicals selected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COORand CONRR;'}, {'sub': 3', '12', '1', '8, 'sup': 14b', '8', '9', '10', '11, 'C-C-cycloalkyl, which may be interrupted by one or more CO and/or may be substituted by one or more identical or different radicals Rselected from C-C-alkyl, CN, COR, COOR, CONRR;'}, {'sup': 14c', '4', '5', '6', '7', '8', '9', '10', '11, 'sub': 1', '6', '1', '4', '2, 'phenyl, which may be substituted by one or more identical or different radicals Rselected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COOR, CONRRand phenyl,'}, 'or', {'sup': '14', 'two radicals Rtogether may be a divalent bridging group having 1 to 10 atoms between the flanking bonds.'}], 'Ris C-C-alkyl, which may be interrupted by one or more O, S, NRor CO and/or may be substituted by one or more identical or different radicals Rselected from CN, COR, COOR, CONRR, phenyl and C-C-cycloalkyl which may interrupted by one or two CO groups and where the two last-mentioned radicals may be substituted by one or ...

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Номер записи: 49
15-05-2014 дата публикации

SMALL MOLECULE INHIBITORS OF HIV PROTEASES

Номер: US20140135321A1
Автор: Ghosh Arun K.
Принадлежит:

Described herein are compounds, compositions, and methods for treating HIV and related diseases. 2. The pharmaceutical composition of wherein Z is selected from the group consisting of a bond claim 1 , S(O) claim 1 , SO claim 1 , optionally substituted nitrogen claim 1 , and (CRR) claim 1 , where m is 1 to about 3.3. The pharmaceutical composition of wherein X and Y are each independently selected from the group consisting of a bond claim 1 , O claim 1 , S claim 1 , S(O) claim 1 , SO claim 1 , optionally substituted nitrogen claim 1 , and (CRR) claim 1 , where m is 1 to about 3; providing that claim 1 , when X is O then Y is not O or S and when Y is O then X is not O or S.4. The pharmaceutical composition of wherein W claim 1 , X claim 1 , Y claim 1 , and Z are taken together with the attached carbons to form a 5 to 8 membered heterocycle containing 1 or 2 oxygen atoms.5. The pharmaceutical composition of wherein W claim 1 , X claim 1 , Y claim 1 , and Z are taken together with the attached carbons to form a 5 to 8 membered heterocycle containing 1 oxygen and 1 nitrogen atom.6. The pharmaceutical composition of wherein the heterocycle is a tetrahydrofuran claim 1 , dioxolane claim 1 , tetrahydropyran claim 1 , dioxane claim 1 , morpholine claim 1 , oxepane claim 1 , each of which is optionally substituted.7. The pharmaceutical composition of wherein the heterobicycle is a oxabicyclo-[3.2.1]-octane claim 1 , which is optionally substituted.8. The pharmaceutical composition of wherein one of X claim 1 , Y claim 1 , or Z is O or NR claim 1 , where Ris selected from the group consisting of hydrogen claim 1 , alkyl claim 1 , heteroalkyl claim 1 , hydroxy claim 1 , alkoxy claim 1 , arylalkoxy claim 1 , amino claim 1 , alkylthio claim 1 , heterocyclyl claim 1 , heterocyclylalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , arylalkyl claim 1 , heteroarylalkyl claim 1 , and pro-drug moieties claim 1 , each of which is optionally substituted; and the others of X claim 1 , Y ...

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Номер записи: 50
28-02-2019 дата публикации

Oligomeric (TH)FP, production and uses therefor

Номер: US20190062291A1
Автор: David Dunn, Howard Winston Tyrrell SUTTON, Ian Stuart PEARCE, John Ing Chuan DALY, Simon Jonathon Grant
Принадлежит: Thomas Swan and Co Ltd

A method for the isolation of oligomeric 2, 2-difurylpropane (DTHFP) suitable for use on an industrial scale. A method can include using oligomeric 2, 2-difurylpropane, in particular, its use can be as a polar modifier for butadiene and styrene butadiene polymerisation so is to produce rubber. Utilising the material as an alternative to DTHFP in rubber production avoids subsequent leaching of the DTHFP into the environment as the oligomeric 2, 2-difurylpropane (DTHFP) gives rise to much lower levels of leaching.

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Номер записи: 51
12-03-2015 дата публикации

Process for preparation of 3-((2s,5s)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives and intermediates useful thereof

Номер: US20150073157A1
Автор: Boris Gorin, Fabio E.S. Souza, Jason A. BEXRUD, Ricardo Orprecio
Принадлежит: Alphora Research Inc

Discloses is a process for preparation of a compound of formula 7, or a derivative thereof, wherein PG 1 is an alcohol protecting group. Also, disclosed are intermediates and processes for their preparation. The compound of formula 7 can be useful in the preparation of halinchondrin analogs such as Eribulin.

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Номер записи: 52
29-05-2014 дата публикации

PREPARATION OF AMINOMETHYL FURANS AND ALKOXYMETHYL FURAN DERIVATIVES FROM CARBOHYDRATES

Номер: US20140148605A1
Автор: Howard Stephen, Sanborn Alexandra
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

Described herein are single step methods of making various classes of alkylamine derivatives of furan and tetrahydrofuran by simultaneous contact of a sugar with H, an acid catalyst and hydrogenation catalyst in the presence of an alkylamide solvent. The hydrogenation catalyst is a heterogeneous catalyst comprising a metal selected from the group consisting of Pt, Pd, and nickel. The acid catalysts may be homogeneous mineral acid or a heterogeneous acid catalyst on substrate. In a preferred practice the two catalysts are provided on a common heterogeneous bifunctional support. Using similar combinations of acid and hydrogenation catalysts, there is also described single step methods for making furandimethanol by simultaneously contacting a hexose with the two separate catalysts in the presence of Hin an aprotic solvent, such as dimethylformamide. With the same catalyst system and similar reaction conditions, 2,5 furan dialkylethers can also be made in a single step when the solvent includes an ROH alcohol. 123.-. (canceled)25. The method of wherein the organic solvent is a polar aprotic solvent claim 24 , the reaction mixture further includes Hthe temperature is 90-120° C. claim 24 , the pressure is 200-500 psi claim 24 , and the hydroxymethylfuran or tetrahydrofuran derivative is furandimethanol or tetrahydrofuran dimethanol26. The method of wherein the pressure is 400-600 psi claim 25 , and the time is 2-6 hours.27. The method of wherein the polar aprotic solvent comprises dimethylformamide.28. The method of wherein the organic solvent is a C1-C4 alcohol and the hydroxymethylfuran or tetrahydrofuran derivative is a 2 claim 24 ,5-furandiether or a 2 claim 24 ,5-tetrahydrofuran diether29. The method of wherein the temperature is 110-160 C claim 28 , the pressure is greater than 400 psi claim 28 , and the time is 1-4 hours.30. (canceled)31. The method of wherein the hydrogenation catalyst is a heterogeneous catalyst and the acid catalyst is a homogeneous mineral acid ...

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Номер записи: 53
17-03-2016 дата публикации

TETRAHYDROFURAN DERIVATIVES AND USE THEREOF AS PLASTICIZERS

Номер: US20160075671A1
Автор: Bohn Martin A., Breitscheidel Boris, Kindler Alois, LANK Benoit, Wagner Jochen
Принадлежит:

The invention relates to tetrahydrofuran derivatives of general formula (I), wherein X stands for *—(C═O)—O—, *—(CH2)n-O—, or *—(CH2)n-O—(C═O)—, wherein * represents the point of bonding to the tetrahydrofuran ring and n has the value 0, 1, or 2; and R1 and R2 are selected independently of each other from among C4-C5 alkyl and C5-C6 cycloalkyl, wherein the cycloalkyl groups are unsubstituted or can be substituted by at least one C1-C10 alkyl group, a plasticizer composition that contains said tetrahydrofuran derivatives, molding masses that contain a thermoplastic polymer or an elastomer and such a tetrahydrofuran derivative. The invention further relates to a method for producing said tetrahydrofuran derivatives, and to the use of said tetrahydrofuran derivatives 2. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer of the general formula (I) claim 1 , Rand Rare independently selected from an unbranched or branched C-alkyl moiety.3. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer of the general formula (I) claim 1 , Rand Rare independently selected from n-butyl or isobutyl.4. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer of the general formula (I) claim 1 , both of the groups X are *—(C═O)—O—.5. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer that is not of the formula (I) claim 1 , is a plasticizer for a thermoplastic polymer which comprises polyvinyl chloride or consists of polyvinyl chloride.6. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer that is not of the formula (I) claim 1 , is a plasticizer for an elastomer which comprises a natural and/or synthetic rubber or consists of a natural and/or synthetic rubber.7. The polymer or elastomer according to claim 1 , wherein the at least one plasticizer that is not of the formula (I) claim 1 , is plastisol.8. The polymer or elastomer ...

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Номер записи: 54
19-03-2015 дата публикации

NOVEL COMPOUNDS

Номер: US20150080369A1
Автор: Birault Veronique, Campbell Amanda Jennifer, Harrison Stephen, LE Joelle, Shukla Lena
Принадлежит:

The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ. 2. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris H.35-. (canceled)6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris isobutyl.7. (canceled)9. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein r is 1.1011-. (canceled)12. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris CHOH.13. (canceled)14. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein s is 0.1516-. (canceled)17. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein u is 1.18. (canceled)19. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein t is 1 and X is O.20. (canceled)21. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris H.22. (canceled)23. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a heterocycloalkyl selected from tetrahydro-2H-pyran and morpholine.24. (canceled)25. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris unsubstituted.26. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , which is selected from the group consisting of:N-(2,4-dimethylphenyl)-N-(2-methylpropyl)-3-[(oxan-4-ylmethoxy)methyl]benzene-1-sulfonamide;N-(2,4-dimethylphenyl)-N-(2-methylpropyl)-4-[2-(morpholin-4-yl)ethoxy]benzene-1-sulfonamide;2-[(2,4-dimethylphenyl)(2-methylpropyl)sulfamoyl]-5-(oxan-4- ...

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Номер записи: 55
14-03-2019 дата публикации

BIODEGRADABLE COMPOUND, LIPID PARTICLE, COMPOSITION CONTAINING LIPID PARTICLE, AND KIT

Номер: US20190076358A1
Автор: Akahoshi Eiichi, Ishihara Mitsuko, NAITO Katsuyuki
Принадлежит: KABUSHIKI KAISHA TOSHIBA

The compound according to the present embodiment is represented by the following formula (1): 2. The compound according to claim 1 , wherein the L contains an ester structure selected from the group consisting of —C(═O)—O— claim 1 , —O—C(═O)—O— claim 1 , —O—C(═O)—O— claim 1 , —C(═S)—O— claim 1 , —O—C(═S)— claim 1 , —O—C(═S)—O— claim 1 , —S—C(═O)— claim 1 , —C(═O)—S— claim 1 , and —O—P(═O)OR′—O—(wherein R′ is hydrogen claim 1 , a non-cationic aliphatic group claim 1 , or —CHR).8. The compound according to claim 7 , wherein the c1 is a number from 4 to 8.9. The compound according to claim 1 , wherein the longest molecular chain contained in the R has 8 or more atoms.11. A lipid particle comprising the compound according to .12. The lipid particle according to claim 11 , further comprising a membrane-forming lipid and an aggregation-reducing lipid.13. The lipid particle according to claim 12 , wherein the membrane-forming lipid is selected from the group consisting of1,2-dioleoyl-sn-glycero-3-phosphoethanol amine (DOPE),1,2-stearoyl-sn-glycero-3-phosphoethanol amine (DSPE),1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC),1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylcholine (POPC),1,2-di—O—octadecyl-3-trimethylammonium propane (DOTMA),1,2-dioleoyl-3-dimethylammonium propane (DODAP),1,2-dimyristoyl-3-di methylammonium propane (14:0 DAP),1,2-dipalmitoyl-3-dimethylammonium propane (16:0 DAP),1,2-distearoyl-3-dimethylammonium propane (18:0 DAP),N-(4-carboxybenzyl)-N,N-dimethyl-2,3-bis(oleoyloxy)propane (DOBAQ),1,2-dioleoyl-3-trimethylammonium propane (DOTAP),1,2-dioleoyl-sn-glycero-3-phosphochlorine (DOPC),1,2-dilinoleoyl-sn-glycero-3-phosphochlorine (DLPC), 'wherein the aggregation-reducing lipid is a polyethylene glycol (PEG)-modified lipid.', '1,2-dioleoyl-sn-glycero-3-phospho-L-serine (DOPS), cholesterol, and the like; and'}14. The lipid particle according to claim 11 , further comprising an active agent.15. The lipid particle according to claim 14 , wherein the ...

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Номер записи: 56
23-03-2017 дата публикации

METHODS OF PRODUCING COMPOUNDS FROM 5-(HALOMETHYL)FURFURAL

Номер: US20170081470A1
Автор: BISSELL, HIRSCH-WEIL Dimitri A., II John Albert, MASUNO Makoto Nathanael, Smith Ryan L.
Принадлежит: MICROMIDAS, INC.

Provided herein are methods of producing compounds, such as cyclohexanone, hexanediamine, hexanediol, hexamethylenediamine, caprolactam and nylon, from 5-(halomethyl)furfural. 2. A method of producing cyclohexanone , comprising:converting 5-(halomethyl)furfural to hexane-1,5-diol;oxidizing the hexane-1,5-diol to produce 6-hydroxyhexan-2-one; andcyclizing the 6-hydroxyhexan-2-one to produce cyclohexanone.4. A method of producing hexane-1 ,6-diol , comprising:contacting 5-(halomethyl)furfural with an alkanolate or acetate salt to produce 5-(alkoxymethyl)furan-2-carbaldehyde; andreducing the 5-(alkoxymethyl)furan-2-carbaldehyde to produce hexane-1,6-diol.7. The method of claim 6 , wherein the compound of formula (A) and the ammonia are further combined with a copper catalyst to produce the compound of formula (G) and/or a salt thereof.10. A method of producing hexamethylenediamine claim 6 , comprising:converting 5-(halomethyl)furfural to (tetrahydrofuran-2,5-diyl)dimethanamine; andconverting the (tetrahydrofuran-2,5-diyl)dimethanamine to hexamethylenediamine.11. The method of claim 10 , wherein the converting of 5-(halomethyl)furfural to (tetrahydrofuran-2 claim 10 ,5-diyl)dimethanamine comprises:converting the 5-(halomethyl)furfural to (5-(iminomethyl)furan-2-yl)methanamine; andconverting the (5-(iminomethyl)furan-2-yl)methanamine to the (tetrahydrofuran-2,5-diyl)dimethanamine.12. The method of claim 10 , wherein the converting of 5-(halomethyl)furfural to (tetrahydrofuran-2 claim 10 ,5-diyl)dimethanamine comprises:combining the 5-(halomethyl)furfural with ammonia to produce (5-(iminomethyl)furan-2-yl)methanamine; andreducing the (5-(iminomethyl)furan-2-yl)methanamine to produce the (tetrahydrofuran-2,5-diyl)dimethanamine.13. The method of claim 10 , wherein the converting of 5-(halomethyl)furfural to (tetrahydrofuran-2 claim 10 ,5-diyl)dimethanamine comprises:converting the 5-(halomethyl)furfural to (5-(azidomethyl)furan-2-yl)methanimine; andconverting the (5-( ...

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Номер записи: 57
21-03-2019 дата публикации

Conversion of Biomass

Номер: US20190084951A1
Автор: Christopher Cooper, Jihan Khan, Marshall Medoff, Thomas Craig Masterman
Принадлежит: Xyleco Inc

Biomass feedstocks (e.g., plant biomass, animal biomass, and municipal waste biomass) are processed to produce useful products, such as fuels. For example, systems are described that can convert feedstock materials to a sugar solution, especially, xylose, which can then be chemically converted to furfural and furfural-derived products.

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Номер записи: 58
19-06-2014 дата публикации

Pesticidal compositions and processes related thereto

Номер: US20140171309A1
Автор: Akshay PATNY, Gerald B. Watson, James E. Hunter, Joshodeep Boruwa, Pravin S. IYER, William C. Lo
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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Номер записи: 59
07-04-2016 дата публикации

TETRAHYDROFURAN-2,5-DICARBALDEHYDES (DIFORMYL-TETRAHYDROFURAN, DFTHF) AND PROCESS FOR MAKING THE SAME

Номер: US20160096813A1
Автор: Stensrud Kenneth
Принадлежит:

Tetrahydrofuran-(THF)-2,5-dicarbaldehyde and a process of preparing the same are described. The process involves reacting THF-diols in an inert organic solvent with an oxidizing agent at a temperature up to about 50 C. The process can use either HMF or THF-diols as starting materials, and enables a single-step conversion of THF-diols into a precursor material that can be transformed into a multitude of furanic derivative compounds. THF dicarbaldehyde can be modified according to certain reaction processes to generate either new or existing derivative compounds. 1. A process of making a tetrahydrofuran-(THF)-2 ,5-dicarbaldehyde , comprising:providing a reaction mixture containing THF-diols and an inert organic solvent; reacting said THF-diols with an oxidizing agent at a reaction temperature between about 10° C. to about 50° C., in a non-inert atmosphere.2. (canceled)3. The process according to claim 1 , wherein said oxidizing agent exhibits selective reactivity with primary alcohol moieties.4. The process according to claim 1 , wherein said oxidizing agent is not reactive with atmospheric oxygen or water vapor.5. The process according to claim 1 , wherein said oxidizing agent is inhibited from further oxidation of said THF-2 claim 1 ,5-dialdehyde.6. The process according to claim 1 , wherein said oxidizing agent is non-toxic.7. The process according to claim 1 , wherein said reaction temperature is from about 12° C. to about 45° C.8. The process according to claim 1 , wherein a minimum of one equivalent of oxidizing agent is consumed per hydroxyl (OH)-group of said THF-diols.9. The process according to claim 1 , wherein said oxidizing agent is at least one of the following: Dess Martin Periodinane (DMP) claim 1 , Swern oxidation agent (DMSO claim 1 , oxallyl-chloride) claim 1 , pyridinium chloro-chromate (PCC).10. The process according to claim 1 , wherein said THF-diols and THF-2 claim 1 ,5-dicarbaldehyde are present in a 90:10 ratio of cis:trans diastereomers.11. ...

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Номер записи: 60
09-04-2015 дата публикации

DIALLYL ETHERS OF 2,5BIS(HYDROXYMETHYL)TETRAHYDROFURAN AND PROCESSES FOR MAKING THE SAME

Номер: US20150099895A1
Автор: Stensrud Kenneth
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

The diallyl ether derivatives of the cis and trans stereoisomers of 2,5-bis(hydroxymethyl)tetrahydrofuran are produced. These materials are expected to be useful for making a variety of biobased polymers. Processes are further described for producing these diallyl ether derivatives in substantially quantitative yields. 1. (2R , 5S)-2 ,5-bis((allyloxy)methyl)tetrahydrofuran.2. (2S , 5S)-2 ,5-bis((allyloxy)methyl)tetrahydrofuran.3. A process for making a diallyl ether derivative of at least one of the cis and trans stereoisomers of 2 ,5-bis(hydroxymethyl)tetrahydrofuran , comprising reacting at least one of the cis and trans isomers of 2 ,5-bis(hydroxymethyl)tetrahydrofuran with a Brønsted base whose conjugate acid has an acid dissociation constant pKgreater than 16 to form at least one corresponding conjugate base of an isomer of 2 ,5-bis(hydroxymethyl)tetrahydrofuran , then reacting the conjugate base or bases so formed with allyl bromide to form the corresponding diallyl ether derivative.4. A process according to claim 3 , wherein the yield of the diallyl ether derivative or derivatives is substantially quantitative.5. A process as in claim 3 , wherein the Brønsted base whose conjugate acid has an acid dissociation constant pKof at least about 18.6. A process as in claim 5 , wherein potassium t-butoxide is reacted with the at least one of the cis and trans isomers of 2 claim 5 ,5-bis(hydroxymethyl)tetrahydrofuran.76. A process as in any of - claims 3 , which is carried out in a nonaqueous solvent system and in the substantial absence of water.8. A process as in claim 7 , carried out at a temperature of about 25 degrees Celsius or less.9. A process as in claim 8 , carried out at a temperature of about 20 degrees Celsius or less.10. A process as in claim 7 , wherein allyl bromide is added gradually over time.11. A process as in claim 10 , wherein not more than about 13.3 percent of the allyl bromide is added per minute.12. A process for making a diallyl ether ...

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Номер записи: 61
26-03-2020 дата публикации

HYDROXY FORMAMIDE DERIVATIVES AND THEIR USE

Номер: US20200095217A1
Автор: Dowdell Sarah E., Eidam Hilary Schenck, ELBAN Mark, FOX Ryan Michael, Hammond Marlys, Hilfiker Mark A., Hoang Tram H., KALLANDER Lara, LAWHORN Brian Griffin, MANNS Sharada, PHILP Joanne, WASHBURN David G., Ye Guosen
Принадлежит:

Disclosed are compounds having the formula: 2. The method according to claim 1 , wherein the compound of Formula (I):{'sub': 1', '4', '1', '4, 'R1 is selected from the group consisting of H, (C-C) straight chain alkyl, and (C-C) straight chain alkyl substituted with a hydroxy group;'}{'sub': 1', '11', '1', '3', '3', '6', '1', '3', '1', '3', '1', '11', '1', '4', '1', '4, 'R2 is selected from H, (C-C)alkyl, (C-C)alkyl-(C-C)cycloalkyl, (C-C)alkyl-phenyl, and (C-C)alkyl-heterocyclyl, wherein heterocyclyl is a monocyclic ring having 5-6 ring atoms wherein 1-2 of the ring atoms are selected from nitrogen, oxygen and sulfur, and wherein said (C-C)alkyl, cycloalkyl, phenyl, and heterocyclyl are optionally substituted with 1-2 groups independently selected from (C-C)alkyl, (C-C)alkoxy, halo, and cyano; and'} 'c) phenyl, optionally substituted with 1-3 groups independently selected from:', 'R3 is selected from{'sub': 1', '6', '2', '1', '4', '1', '4', '2', '1', '4, 'sup': f', 'g', 'a', 'b', 'a', 'b', 'f', 'g, '(C-C)alkyl, optionally substituted with 1-3 groups independently selected from: fluoro; —COH; —P(O)RR; and —C(O)NRRwherein Rand Rare independently selected from H and (C-C)alkyl, wherein the (C-C)alkyl is optionally substituted with 1-3 groups independently selected from hydroxy, —COH, —C(O)O(C-C)alkyl and —P(O)RR;'}{'sub': '2', 'cyclopropyl, optionally substituted with 1 —COH;'}{'sup': a', 'b', 'a', 'b', 'f', 'g', 'c', 'd', '+', 'c', 'd', 'e, 'sub': 1', '4', '1', '4', '2', '1', '4, '—C(O)NRRwherein Rand Rare independently selected from H and (C-C)alkyl, wherein the (C-C)alkyl is optionally substituted with 1-3 groups independently selected from hydroxy, —COH, —C(O)O(C-C)alkyl, —P(O)RR, NRRand NRRR;'}{'sub': 1', '6', '2', '3', '6, '(C-C)alkoxy, optionally substituted with 1-3 substituents independently selected from halo, hydroxy, —COH, (C-C)cycloalkyl, and pyrrolidinyl;'}{'sub': 3', '6', '2, '(C-C)cycloalkoxy, optionally substituted with 1-3 substituents independently ...

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Номер записи: 62
21-04-2016 дата публикации

Novel Compound

Номер: US20160108023A1
Автор: Alan Robert Steven, Andrew John Williams, Craig Robert Stewart, Iain Alastair Stewart Walters, Mark Richard Ebden, Paula Margaret Tomlin, Stephen Connolly, Thomas Langer
Принадлежит: AstraZeneca AB, Astrazeneca Uk Ltd

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. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.

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Номер записи: 63
19-04-2018 дата публикации

PROFLAVOR DELIVERY ARTICLE

Номер: US20180103667A1
Автор: VAN SLEEUWEN Rutger M.T., WOMACK Gary B.
Принадлежит:

Provided herein are flavor particles containing encapsulated precursors of acetylaldehyde. Also provided herein are methods of making and using the particles. 2. The composition as recited in wherein Rand Rare independently a straight or branched C-Calkyl.3. The composition as recited in wherein Rand Rare independently selected from the group consisting of methyl claim 2 , ethyl claim 2 , propyl claim 2 , and butyl.4. The composition as recited in any one of to wherein n is 1 and x is 2.5. The composition as recited in any one of - wherein n is 2 and x is independently 0 claim 2 , 1 or 2.6. The composition as recited in any one of to wherein n is 3 claim 2 , 4 claim 2 , 5 or 6 and x is independently 0 claim 2 , 1 or 2.7. The composition as recited in selected from the group consisting of bis(1-ethoxyethyl) succinate; bis(1-ethoxyethyl) adipate; bis(1-ethoxyethyl) fumarate; bis(1-propoxyethyl) succinate; bis(1-propoxyethyl) adipate; bis(1-propoxyethyl) fumarate; bis(1-butoxyethyl) succinate; bis(1-butoxyethyl) adipate claim 1 , and bis(1-butoxyethyl) fumarate.8. The composition as recited in wherein the compound is 5-(2-(1-ethoxyethoxy)propan-2-yl)-2-methyl-2-vinyltetrahydrofuran.9. The composition as recited in any one of - wherein the composition is a granule having a size greater than or equal to about 100 micrometers.10. The composition as recited in wherein the granule has a size in a range of about 100 μm up to about 5 mm (millimeters).11. The composition as recited in any one of to wherein the carrier comprises an emulsifier in an amount of from 0% up to about 100% a by weight of the total weight of the carrier.12. A method of releasing acetaldehyde into an aqueous solution comprising delivering a composition as defined in any one of - to the aqueous solution.13. The use of a composition defined by any one of - to confer claim 9 , enhance claim 9 , improve or modify the flavor or aroma of a flavored article.14. A method of making a glass composition comprising ...

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Номер записи: 64
10-07-2014 дата публикации

PIPERAZINE DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO

Номер: US20140194422A1
Автор: Ganesh Thota, Lambeth John David, Smith Susane M., Sun Aiming
Принадлежит: EMORY UNIVERSITY

The disclosure relates to piperazine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidase. 2. The pharmaceutical composition of claim 1 , wherein Z is C═O.3. The pharmaceutical composition of claim 1 , wherein Ris alkyl substituted with amino wherein the amino is substituted with an aryl group optionally substituted with one or more alkoxy.4. The pharmaceutical composition of claim 1 , wherein Ris a heterocyclyl optionally substituted with one or more R;5. The pharmaceutical composition of claim 3 , wherein the heterocyclyl is indolyl claim 3 , quinolinyl claim 3 , or imidazolyl.6. A compound of formula I as in claim 1 , selected from the group consisting of2-((4-acetylphenyl)amino)-1-(4-(4-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(4-methoxyphenyl)-3-methylpiperazin-1-yl)ethanone;2-((4-isopropylphenyl)amino)-1-(4-(4-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(4-ethoxyphenyl)piperazin-1-yl)ethanone;2-((3,4-difluorophenyl)amino)-1-(4-(4-methoxyphenyl)piperazin-1-yl)ethanone;2-((3-fluorophenyl)amino)-1-(4-(4-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(3-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(2-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(4-fluorophenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(2-fluorophenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(pyridin-4-yl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(pyrimidin-2-yl)piperazin-1-yl)ethanone;4-(4-(2-((4-acetylphenyl)amino)acetyl)piperazin-1-yl)benzonitrile;2-((2-fluorophenyl)amino)-1-(4-(4-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-fluorophenyl)amino)-1-(4-(4-methoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(3,4-dimethoxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl)amino)-1-(4-(2-hydroxyphenyl)piperazin-1-yl)ethanone;2-((4-acetylphenyl) ...

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Номер записи: 65
27-04-2017 дата публикации

IMMUNOREGULATORY AGENTS

Номер: US20170112785A1
Автор: JEAN Jaun Carlos, OSIPOV Maksim, POWERS Jay Patrick, SHUNATONA Hunter Paul, WALKER James Ross, ZIBINSKY Mikhail
Принадлежит:

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. 6. The compound of claim 1 , wherein Xis hydrogen.7. The compound of claim 1 , wherein Ris selected from the group consisting of optionally substituted C-Ccycloalkyl and optionally substituted C-Ccycloalkyl-C-Calkyl.8. The compound of claim 1 , wherein Ris selected from the group consisting of optionally substituted 4- to 6-membered cycloheteroalkyl.10. The compound of claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , 1-propyl claim 1 , 2-propyl claim 1 , 1-butyl claim 1 , 2-methylpropyl claim 1 , 3-hydroxypropyl claim 1 , 1-pentyl claim 1 , and 1 claim 1 ,1-dimethylethyl.11. The compound of claim 1 , wherein Xis halogen or C-Chaloalkyl; Xis hydrogen or halogen; and Ris a member selected from the group consisting of optionally substituted C-Calkyl claim 1 , optionally substituted C-Ccycloalkyl claim 1 , optionally substituted C-Ccycloalkyl-C-Calkyl claim 1 , and optionally substituted 3- to 7-membered cycloheteroalkyl; or Rand Rare optionally joined together to form an optionally substituted cyclobutyl claim 1 , cyclopentyl or cycloheptyl.12. The compound of claim 11 , wherein Ris selected from the group consisting of optionally substituted C-Ccycloalkyl and optionally substituted C-Ccycloalkyl-C-Calkyl.13. The compound of claim 11 , wherein Ris selected from the group consisting of optionally substituted 4- to 6-membered cycloheteroalkyl.15. The compound of claim 11 , wherein Ris selected from the group consisting of methyl claim 11 , ethyl claim 11 , 1-propyl claim 11 , 2-propyl claim 11 , 1-butyl claim 11 , 2-methylpropyl claim 11 , ...

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Номер записи: 66
27-04-2017 дата публикации

BENZAMIDE OR BENZAMINE COMPOUNDS USEFUL AS ANTICANCER AGENTS FOR THE TREATMENT OF HUMAN CANCERS

Номер: US20170114062A1
Автор: DeBRABANDER Jef, PARADA Luis
Принадлежит:

The described invention provides small molecule anti-cancer compounds for treating tumors that respond to cholesterol biosynthesis inhibition. The compounds selectively inhibit the cholesterol biosynthetic pathway in tumor-derived cancer cells, but do not affect normally dividing cells. 2. The compound according to claim 1 , wherein:n=1 or 2;{'sup': '3', 'R═H; and'}{'sup': '4', 'Ris selected from the group consisting of H, Me, and propargyl.'}3. The compound according to claim 2 , wherein:{'sup': 1', '2, 'sub': 1', '6', '2', '6', '1', '6, 'Rand Rare independently selected from the group consisting of H, C-Calkyl, C-Calkynyl, C-Chydroxyalkyl, and acyloxyalkyl.'}4. The compound according to claim 3 , wherein:{'sup': '1', 'sub': 2', '2', '3', '2, 'Xis selected from the group consisting of H, F, Cl, CN, NH, NO, N, and SOMe; and'}{'sup': 2', '2', '6, 'X=L-R.'}5. The compound according to claim 1 , wherein the compound is in form of a pharmaceutical composition comprising a therapeutic amount of the compound and a pharmaceutically acceptable carrier.6. A method of treating a cancer in a subject in need thereof claim 5 , comprising administering to the subject the pharmaceutical composition of claim 5 , wherein the therapeutic amount is effective to inhibit tumor growth claim 5 , inhibit tumor proliferation claim 5 , induce cell death claim 5 , or a combination thereof.7. The method according to claim 6 , wherein the therapeutic amount is effective to inhibit a cholesterol biosynthesis pathway.8. The method according to claim 6 , wherein the therapeutic amount is effective to down-regulate SHREBP2 and its target genes.9. The method according to claim 6 , wherein the cancer is a solid brain tumor.10. The method according to claim 9 , wherein the solid brain tumor is a glioma.11. The method according to claim 10 , wherein the glioma is a glioblastoma.12. The method according to claim 9 , wherein the solid brain tumor comprises cancer stem cells.13. The method according to ...

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Номер записи: 67
17-07-2014 дата публикации

Reduction of hmf ethers with metal catalyst

Номер: US20140200299A1
Автор: Alexandra Sanborn, Paul Bloom
Принадлежит: Archer Daniels Midland Co

Methods of making reduced derivatives of hydroxymethyl furfural using metal catalysts are described. The derivatives may have tetrahydrofuran or furan nucleus with alkoxymethyl ether or ester moieties on the 5″ carbon and methanol on the 2′ carbon. Suitable metal catalyst include Raney nickel, a nickel catalyst with a zirconium promoter, a chromite catalyst with a barium, a palladium catalyst, such as palladium on carbon, or a ruthenium catalyst. Also provided are a new class of compounds, which are n-alkoxy hexane diols (i.e., 1,2 or 1,5 hexane diol ethers) and methods of making the same by reduction of furan or tetrahydrofuran derivatives.

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Номер записи: 68
25-08-2022 дата публикации

COMPOUNDS CONTAINING A SULFONIC GROUP AS KAT INHIBITORS

Номер: US20220267260A1
Автор: HARVEY Darren Martin
Принадлежит:

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. 2. The compound according to claim 1 , wherein L is a 3-atom linker.4. The compound according to claim 1 , wherein L is a 4-atom linker.6. (canceled)7. The compound according to claim 1 , wherein L is a 5-atom linker.9. The compound according to claim 1 , wherein Z is optionally substituted Caliphatic.10. (canceled)11. The compound according to claim 1 , wherein Z is —Cy.1214-. (canceled)15. The compound according to claim 1 , wherein Ring B is an optionally substituted 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen claim 1 , oxygen and sulfur.1622-. (canceled)23. The compound according to claim 1 , wherein Ring A is phenyl.24. The compound according to claim 1 , wherein Ring A is a 8-10 membered bicyclic heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen oxygen and sulfur.25. The compound according to claim 1 , wherein Ring A is a 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen claim 1 , oxygen and sulfur.28. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim 1 , and a pharmaceutically acceptable excipient.29. A method of treating a disease or disorder associated with KAT-5 in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a compound or pharmaceutically acceptable salt thereof according to .30. A method of modulating protein acetylation in a subject in need thereof claim 1 , comprising administering to the subject an effective amount of a compound or pharmaceutically acceptable salt thereof according to .31. A method of treating cancer in a subject claim 1 , comprising administering to the subject an effective amount of a compound or pharmaceutically ...

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Номер записи: 69
27-05-2021 дата публикации

LINOLEIC ACID DERIVATIVES, PHARMACEUTICAL COMPOSITION OR FOOD COMPOSITION COMPRISING SAID LINOLEIC ACID DERIVATIVES, AND THEIR USES

Номер: US20210155640A1
Автор: BAYARDON Jerome, HICHAMI Aziz, JUGE Sylvain, KHAN Naim, LOUILLAT-HABERMEYER Marie-Laure, RUGERI Baptiste
Принадлежит:

Disclosed is a linoleic acid derivative of Formula (I) below including a hydrophobic part CHlinked to a polar head part “A”: 2. The linoleic acid derivative according to claim 1 , having a molecular weight ranging from about 300 to about 600 g/mol.3. The linoleic acid derivative according to claim 1 , wherein in A claim 1 , Rand Rare a saturated or unsaturated claim 1 , straight or branched alkyl group containing 1 to 2 carbon atoms claim 1 , or a pharmaceutically/food quality acceptable salt thereof.7. The linoleic acid derivative according to claim 1 , wherein in A claim 1 , Ris H claim 1 , Ris —COCHand Ris H claim 1 , or a pharmaceutically/food quality acceptable salt thereof.8. The linoleic acid derivative according to claim 1 , wherein in A claim 1 , Ris H claim 1 , Ris CH claim 1 , and Ris H claim 1 , or a pharmaceutically/food quality acceptable salt thereof.10. A pharmaceutical composition or food composition comprising claim 1 , respectively claim 1 ,{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'at least one pharmaceutically acceptable carrier and at least one linoleic acid derivative according to , or'}{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'at least one food ingredient and/or at least one food additive and at least one linoleic acid derivative according to .'}11. A method for treatment of a disorder modulated by the GPR120 receptor and/or the CD36 receptor claim 1 , comprising administering to a subject in need thereof a therapeutically effective amount of said linoleic acid derivative of .12. The method according to claim 11 , wherein the disorder modulated by the GPR120 receptor and/or the CD36 receptor is selected from the group consisting of diabetes claim 11 , hyperglycemia claim 11 , impaired glucose tolerance claim 11 , gestational diabetes claim 11 , insulin resistance claim 11 , hyperinsulinemia claim 11 , retinopathy claim 11 , neuropathy claim 11 , nephropathy claim 11 , diabetic kidney disease claim 11 , acute kidney injury ...

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Номер записи: 70
14-05-2015 дата публикации

DIRECT ANTI-MARKOVNIKOV ADDITION OF ACIDS TO ALKENES

Номер: US20150133680A1
Автор: Hamilton David S., Nicewicz David A., Perkowski Andrew J.
Принадлежит:

A method of making an anti-Markovnikov addition product is carried out by reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product; the dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst. Compositions useful for carrying out such methods are also described. 1. A method of making an anti-Markovnikov addition product , comprising:reacting an acid with an alkene or alkyne in a dual catalyst reaction system to the exclusion of oxygen to produce said anti-Markovnikov addition product;said dual catalyst reaction system comprising a single electron oxidation catalyst in combination with a hydrogen atom donor catalyst.2. The method of claim 1 , wherein said anti-Markovnikov addition product is produced regioselectively in a ratio of at least 5:1 of anti-Markovnikov addition product as compared to the corresponding Markovnikov addition product.4. The method of claim 3 , wherein A claim 3 , B claim 3 , and C are each independently selected from the group consisting of halo claim 3 , aryl claim 3 , cyano claim 3 , carboxyl claim 3 , and carbonyl groups.5. The method of claim 1 , wherein said single electron oxidation catalyst is a photocatalyst.6. The method of claim 5 , wherein said photocatalyst comprises a carbocyclic or heterocyclic aromatic compound containing ring nitrogen heteroatoms.7. The method of claim 6 , wherein said photocatalyst comprises an anthracene claim 6 , aza-anthracene or polyaza-anthracene nucleus which is unsubstituted claim 6 , substituted or polysubstituted at any position with halogen claim 6 , and/or with one or more lower alkyl or cycloalkyl radicals claim 6 , and/or with other phenyl substituents.8. The method of claim 5 , wherein said photocatalyst has a reduction potential of about −1.0 V to +0.1 V against a saturated calomel reference electrode in 100 percent acetonitrile ...

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Номер записи: 71
11-05-2017 дата публикации

NEW SIGMA-RECEPTORS LIGANDS WITH ANTI-APOPTOTIC AND/OR PRO-APOPTOTIC PROPERTIES, OVER CELLULAR BIOCHEMICAL MECHANISMS WITH NEUROPROTECTIVE, ANTI-CANCER, ANTI-METASTATIC AND ANTI-(CHRONIC) INFLAMMATORY ACTION

Номер: US20170129864A1
Автор: Vamvakides Alexandre
Принадлежит: ANAVEX LIFE SCIENCES CORP.

The present invention involves new and original sigma receptors ligands: (Mono-or di-alkylaminoalkyl)-γ-butyrolactones, their analogues aminotetrahydrofuranes, the (1-adamantyl) phenyl(s) alkylamines, the N,N Dialkyl α-[(adamantyl-l)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or alkyl phenylamines, their enantiomers or diastereoisomers and their pharmaceutically acceptable salts, with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with anti-cancer, anti-metastatic, anti-(chronic) inflammatory, neuro-protective, anticonvulsive, antidepressive and nooanaleptic or sedative action. 1. A sigma(σ)-receptor ligand with anti-apoptotic and/or pro-apoptotic properties said compound consisting essentially of:a sigma(σ)-receptor ligand compound consisting essentially of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine, enantiomers or diastereoisomers of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine, and pharmacologically acceptable salts of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanomethanamine.24-. (canceled)5. The compound according to wherein said tetrahydro-N claim 1 ,N-dimethyl-2 claim 1 ,2-diphenyl-3-furanomethanamine is a metabolite of said tetrahydro-N claim 1 ,N-dimethyl-2 claim 1 ,2-diphenyl-3-furanomethanamine.6. The compound of wherein said metabolite is tetrahydro-N-methyl-2 claim 5 ,2-diphenyl-3-furanomethanamine This application is a continuation and claims priority to U.S. Ser. No. 12/522,761, filed Jul. 10, 2009, which is a U.S. national phase application under 35 U.S.C. §371 based upon International Application No. PCT/GR2008/000002 filed on Jan. 14, 2008. Additionally, this U.S. national phase application claims the benefit of priority of International Application No. PCT/GR2008/000002 filed on Jan. 14, 2008, and Greece Application No. 20070100020 filed on Jan. 17, 2007. The entire disclosures of the prior applications are incorporated herein by reference. The ...

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Номер записи: 72
31-07-2014 дата публикации

ORGANIC COMPOUNDS

Номер: US20140213594A1
Автор: "DSOUZA Anne-Marie", BAETTIG Urs, Hunt Peter, Press Neil John, WATSON Simon James
Принадлежит: NOVARTIS AG

The present invention relates to compounds of formula (I) 2. The method according to claim 1 , wherein Ris H or C-Calkyl.3. The method according to claim 1 , wherein Ris H or C-Calkyl;{'sup': '2', 'sub': 1', '6, 'Ris C-Calkyl optionally substituted by one or more halogen atoms, CN or OH groups, an ether group containing 2 to 10 carbon atoms and 1 to 3 oxygen atoms, a 4 to 6 membered carbocyclic group optionally substituted by one or more Z groups, or a 4 to 6 membered heterocyclic group optionally substituted by one or more Z groups; or'}{'sup': 1', '2, 'Rand R, together with the carbon atom to which they are attached form a 4 to 6 membered carbocyclic group optionally substituted by one or more Z groups or a 4 to 6 membered heterocyclic group optionally substituted by one or more Z groups.'}4. The method according claim 1 , wherein Ris halogen.5. The method according to claim 1 , wherein Ris H claim 1 , C-Calkyl claim 1 , C-Ccycloalkyl or (C-Calkyl)-C-Ccycloalkyl.6. The method according to claim 1 , wherein Ris C-Calkyl.7. The method according to claim 1 , wherein X is CH.8. The method according to claim 1 , wherein the CXCR2 receptor mediated condition or disease is selected from inflammatory or allergic conditions or diseases claim 1 , particularly severe asthma.9. The method according to claim 1 , wherein the CXCR3 receptor mediated or condition is selected from cancer claim 1 , e.g. ovarian cancer claim 1 , prostate cancer claim 1 , melanoma including metastatic melanoma claim 1 , lung cancer claim 1 , e.g. non small cell lung cancer claim 1 , renal cell carcinoma; tumour angiogenesis claim 1 , ischaemia/reperfusion injury claim 1 , delayed graft function claim 1 , osteoarthritis claim 1 , myeloid metaplasia with myelofibrosis claim 1 , Adenomyosis claim 1 , contact hypersensitivity (skin) and in wound healing.10. The method according to claim 1 , wherein the CXCR3 receptor mediated or condition is selected from acute lung injury (ALI) claim 1 , acute/adult ...

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Номер записи: 73
01-09-2022 дата публикации

DUAL MODULATOR OF MGLUR5 AND 5-HT2A RECEPTOR, AND USE THEREOF

Номер: US20220274939A1
Автор: BAE Mi Seon, Choi Dae Kyu, Choi Jin, HEO Hyun Jin, KIM Hyo Jin, LEE Geon Ho, LEE Han Mi, LEE Yong Seok, PARK Jin Sun, Shim Mi Yon
Принадлежит:

Disclosed are a dual modulator of mGluR5 and 5-HT2AR (5-HT2A receptor), and use thereof. More specifically, disclosed are a compound which acts as modulator of mGluR5 and an antagonist of 5-HT2AR at the same time, and use thereof as therapeutic agent for pain. 2. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein{'sub': 1', '2', '4', '7, 'Xand Xtogether with carbon atom to which they are attached form C-Ccycloalkyl or 4- to 6-membered heterocycloalkyl;'}{'sub': '3', 'Xis CH or N;'}{'sub': 1', '1', '8, 'Ris hydroxy, halo or C-Calkyl;'}{'sub': 2', '1', '8', '1', '5', '1', '5', '1', '5', '1', '5', '3', '6', '1', '5', '3', '6', '1', '5', '1', '5', '1', '5', '1', '5', '1', '8', '1', '8', '1', '8', '1', '8', '1', '5', '1', '5', '1', '5, 'Ris hydroxy, halo, C-Calkyl, C-Calkoxy, 4- to 6-membered heterocycloalkyl, hydroxy-C-Calkyl, halo-C-Calkyl, C-Calkylamino, C-Ccycloalkyl-C-Calkyl, C-Ccycloalkylamino, halo-C-Calkylamino, C-Calkylaminocarbonyl, C-Calkoxycarbonyl-C-Calkyl, carboxy-C-Calkyl, aminocarbonyl-C-Calkyl, hydroxyaminocarbonyl-C-Calkyl, C-Calkylaminocarbonyl-C-Calkyl, di(C-Calkyl)aminocarbonyl-C-Calkyl or pyridyl;'}{'sub': 3', '1', '8, 'Ris deuterium, fluoro or C-Calkyl;'}{'sub': 4', '5', '1', '5, 'Rand Rare each independently halo or C-Calkyl;'}m is an integer of 0 to 2;n is 0 or 1; andl, p and q are each independently an integer of 0 to 2;wherein the heterocycloalkyl has 1 to 3 heteroatoms selected from the group consisting of N and O.3. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the 4- to 7-membered aliphatic ring is cyclobutane claim 1 , cyclopentane claim 1 , cyclohexane or cycloheptane.4. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the 4- to 6-membered heteroaliphatic ring is oxetane claim 1 , tetrahydrofuran claim 1 , tetrahydropyran claim 1 , dioxane or piperidine.5. The compound or pharmaceutically acceptable salt thereof according ...

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Номер записи: 74
17-05-2018 дата публикации

Vinyl Modifier Composition And Processes For Utilizing Such Composition

Номер: US20180134815A1
Автор: Hogan Terrence E., Kiridena Waruna C.B.
Принадлежит: BRIDGESTONE CORPORATION

An oxolanyl compound-containing composition comprising specified amounts of the meso-isomer of one or more of the oxolanyl compounds of specified structure is provided. Also provided are methods for the use of such compositions as vinyl content modifiers in polymerization processes. 125-. (canceled)26. A vinyl content modifier composition comprising 2 ,2-di(2-tetrahydrofuryl)propane , wherein at least 60% by weight of the 2 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.27. The vinyl content modifier composition of claim 26 , wherein at least 65% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.28. The vinyl content modifier composition of claim 26 , wherein at least 75% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.29. The vinyl content modifier composition of claim 26 , wherein at least 99% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.30. The vinyl content modifier composition of claim 26 , wherein 65-99% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.31. The vinyl content modifier composition of claim 26 , wherein 65-87% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.32. The vinyl content modifier composition of claim 26 , wherein at least about 65 to about 75% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.33. The vinyl content modifier composition of claim 26 , wherein about 65 to about 87% by weight of the 2 claim 26 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.35. The vinyl content modifier composition of claim 34 , wherein at least 65% by weight of the 2 claim 34 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.36. The vinyl content modifier composition of claim 34 , wherein at least 75% by weight of the 2 claim 34 ,2-di(2-tetrahydrofuryl)propane is meso-isomer.37. The vinyl content modifier composition of claim 34 , wherein at least 99% by weight of the 2 claim 34 ,2-di(2-tetrahydrofuryl) ...

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Номер записи: 75
26-05-2016 дата публикации

Aminomethyl-Biaryl Derivatives Complement Factor D inhibitors and uses thereof

Номер: US20160145247A1
Автор: Anna Vulpetti, Christine Fang GELIN, David Belanger, Donglei Liu, Edwoge Liliane Jeanne LORTHIOIS, James J. Powers, Keith Jendza, NAN Ji, Nello Mainolfi, Oliver Rogel, Rajeshri Ganesh Karki, Stefan Andreas Randi, Stefanie Flohr, Taeyoung Yoon
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I), a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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Номер записи: 76
02-06-2016 дата публикации

SULFIDE ALKYL COMPOUNDS FOR HBV TREATMENT

Номер: US20160151375A1
Автор: BRAVO Yalda, Chen Austin, Clark Ryan C., Jacintho Jason, Pedram Bijan, Stock Nicholas
Принадлежит:

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris morpholinyl.4. A composition comprising a compound according to claim 1 , or a salt claim 1 , solvate claim 1 , or N-oxide thereof claim 1 , further comprising at least one pharmaceutically acceptable carrier.5. A method of treating an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound according to .6. The method of claim 5 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of an HBV vaccine claim 5 , HBV polymerase inhibitor claim 5 , interferon claim 5 , pegylated interferon claim 5 , viral entry inhibitor claim 5 , viral maturation inhibitor claim 5 , BAY 41-4109 claim 5 , reverse transcriptase inhibitor claim 5 , a TLR-agonist claim 5 , AT-61 ((E)-N-(1-chloro-3-oxo-1-phenyl-3-(piperidin-1-yl)prop-1-en-2-yl)benzamide) claim 5 , and AT-130 ((E)-N-(1-bromo-1-(2-methoxyphenyl)-3-oxo-3-(piperidin-1-yl)prop-1-en-2-yl)-4-nitrobenzamide) claim 5 , and a combination thereof.7. The method of claim 6 , wherein the pegylated interferon is pegylated interferon alpha (IFN-α) claim 6 , pegylated interferon lambda (IFN-λ) claim 6 , or pegylated interferon gamma (IFN-γ).8. The method of claim 6 , wherein the reverse transcriptase inhibitor is at least one of Zidovudine claim 6 , Didanosine claim 6 , Zalcitabine claim 6 , ddA claim 6 , Stavudine claim 6 , Lamivudine claim 6 , Abacavir claim 6 , Emtricitabine claim 6 , Entecavir claim 6 , Apricitabine claim 6 , Atevirapine claim 6 , ribavirin claim 6 , acyclovir claim 6 , famciclovir claim 6 , valacyclovir claim 6 , ...

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Номер записи: 77
15-09-2022 дата публикации

Wdr5-myc inhibitors

Номер: US20220289673A1
Автор: Alex G. Waterson, Alexey Kuznetsov, Changho HAN, Jonathan D. Macdonald, Joseph R. Alvarado, Sameer S. Nikhar, Selena Chacon Simon, Shaun R. Stauffer, Stephen W. Fesik, William P. Tansey
Принадлежит: VANDERBILT UNIVERSITY

Substituted N-phenyl sulfonamide compounds inhibit WDR5-MYC interactions, and the compounds and their pharmaceutical compositions are useful for treating disorders and conditions in a subject, such as cancer cell proliferation.

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Номер записи: 78
16-05-2019 дата публикации

Synthetic Ligands that Modulate the Activity of the RhlR Quorum Sensing Receptor

Номер: US20190144407A1
Автор: BLACKWELL Helen, BOURSIER Michelle E., MOORE Joseph D.
Принадлежит:

RhlR modulators including agonist and antagonists which are useful for modulating QS phenotypes in Gram-negative bacteria. Certain compounds of general formula A-W-HG having various carbocyclic ad heterocyclic head groups (HG) and various tail groups (A), where —W— is —CO—NH—, —SO—NH—, —CO—NH—CH—, or —SO—NH—CH— are RhlR agonists or antagonists. The compounds are useful in methods of modulating quorum sensing in Gram-negative bacteria, particularly in . Compositions including certain RhlR modulators are useful for decreasing the virulence of Gram-negative bacteria. Pharmaceutical compositions comprising certain RhlR modulators are useful for treatment of infections of Gram-negative bacteria. 2. The method of claim 1 , wherein the one or more compound is of formula A-W-HG.3. The method of claim 1 , wherein the one or more compound is of formula AII-L-W-HGII.5. The method of claim 4 , wherein Z represents one halogen substituted on the phenyl ring.6. (canceled)7. (canceled)8. The method of claim 4 , wherein m is 1 and r is 0 or 1.9. (canceled)10. The method of claim 1 , wherein modulation is activation.11. The method of claim 1 , wherein modulation is inhibition.13. (canceled)14. The method of claim 12 , where r is 1.15. The method of claim 12 , wherein W is —CO—NH—CH— claim 12 , or —SO—NH—CH—.17. (canceled)20. (canceled)22. The method of claim 1 , wherein the modulating is activating and HG or HGII is cyclopentyl.24. (canceled)25. (canceled)2735-. (canceled)38. (canceled)39. (canceled)4147-. (canceled) This application is a U.S. National Stage Application under 35 U.S.C. § 371 of International Application No. PCT/US2017/030314, filed Apr. 30, 2017, which claims the benefit of U.S. provisional applications 62/329,942, filed Apr. 29, 2016, and U.S. provisional application 62/376,291, filed Aug. 17, 2016. Each of these applications is hereby incorporated by reference in its entirety.This disclosure was made with government support under GM 109403 awarded by the National ...

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Номер записи: 79
28-08-2014 дата публикации

REDUCTION OF HMF ETHERS WITH METAL CATALYST

Номер: US20140239230A1
Автор: Bloom Paul, Sanborn Alexandra
Принадлежит: ARCHER DANIELS MIDLAND COMPANY

Methods of making reduced derivatives of hydroxymethyl furfural using metal catalysts are described. The derivatives may have tetrahydrofuran or furan nucleus with alkoxymethyl ether or ester moieties on the 5′ carbon and methanol on the 2′ carbon. Suitable metal catalyst include Raney nickel, a nickel catalyst with a zirconium promoter, a chromite catalyst with a barium, a palladium catalyst, such as palladium on carbon, or a ruthenium catalyst. Also provided are a new class of compounds, which are n-alkoxy hexane diols (i.e., 1,2 or 1,5 hexane diol ethers) and methods of making the same by reduction of furan or tetrahydrofuran derivatives. 2. The method of claim 1 , where the source contains at least 40% of the R-5′acyloxymethylfurfural ester as a fraction of dissolved solutes in the source and the desired compound formed is predominantly the (5-acyloxymethyl)-tetrahydrofuran-2-methanol.3. The method of claim 1 , where the source contains at least 40% of the R-5′acyloxymethylfurfural ester as a fraction of dissolved solutes in the source and the desired compound formed is predominantly the (5-acyloxymethyl)-furan-2-methanol.4. The method of claim 1 , where the source contains less than 40% of the R-5′acyloxymethylfurfural ester as a fraction of dissolved solutes in the source and additionally contains at least 20% of at least one compounds selected from the group consisting of alkyl levulinates and humins as a fraction of dissolved solutes in the source and the desired compound formed is predominantly the (5-acyloxymethyl)-furan-2-methanol.5. The method of claim 1 , wherein the temperature is 140-250° C. claim 1 , the pressure is 500-1500 psi claim 1 , the time is 30 min to 14 hours claim 1 , the source is greater than 80% pure claim 1 , and the reaction converts the acyloxymethylfurfural ester to the (5-acyloxymethyl)-tetrahydrofuran-2-methanol compound.6. The method of claim 1 , wherein the temperature is 170-205° C. claim 1 , the source is less than 80% pure ...

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Номер записи: 80
08-06-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170156320A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 81
08-06-2017 дата публикации

LEOLIGIN DERIVATIVES AS SMOOTH MUSCLE CELL PROLIFERATION INHIBITORS

Номер: US20170157301A1
Автор: ATANASOV Atanas, Bernhard David, DIRSCH Verena M., LINDER Thomas, Mihovilovic Marko, SCHWAIGER Stefan, STUPPNER Herrmann
Принадлежит:

A compound of formula (II), and a method of preparation thereof, for use as a smooth muscle cell (SMC) proliferation-inhibiting drug: 2. (canceled)3: The compound of claim 1 , which isisobutyric acid ((2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4,5-trimethoxyphenyl)-tetrahydrofuran-3-yl)methyl ester (2632),(Z)-2-methyl-2-butenoic acid ((2S,3R,4R)-4-(4-butyl benzyl)-2-(3,4-dimethoxyphenyl)tetrahydrofuran-3-yl)methyl ester (3026),((2S,3R,4R)-4-(4-(trifluoromethyl)benzyl)-2-(3,4,5-trimethoxyphenyl)tetrahydrofuran-3-yl)methanol (2760),(Z)-2-methyl-2-butenoic acid ((2S,3R,4R)-4-(4-(tert-butyl)benzyl)-2-(4-fluorophenyl)-tetrahydrofuran-3-yl)methyl ester (3010),(2S,3R,4R)-3-((allyloxy)methyl)-4-(3,4-dimethoxybenzyl)-2-(3,4-dimethoxyphenyl)-tetrahydrofuran (2540),(Z)-2-methyl-2-butenoic acid ((2S,3R,4R)-2-(4-fluorophenyl)-4-(4-(trifluoromethyl)-benzyl)tetrahydrofuran-3-yl)methyl ester (3016),((2S,3R,4R)-2-(3,4-dimethoxyphenyl)-4-(4-methylbenzyl)tetrahydrofuran-3-yl)-methanol (2754),3-methyl-2-butenoic acid ((2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4,5-trimethoxy-phenyl)tetrahydrofuran-3-yl)methyl ester (2755),((2S,3R,4R)-4-benzyl-2-(3,4,5-trimethoxyphenyl)tetrahydrofuran-3-yl)methanol (2756),(Z)-2-methyl-2-butenoic acid ((2S,3R,4R)-2-phenyl-4-(4-(trifluoromethyl)benzyl)-tetrahydrofuran-3-yl)methyl ester (3015),3-methylbutenoic acid ((2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(4-fluorophenyl)-tetrahydrofuran-3-yl)methyl ester (2862),(Z)-2-methyl-2-butenoic acid ((2S,3R,4R)-4-(4-fluorobenzyl)-2-(4-fluorophenyl)-tetrahydrofuran-3-yl)methyl ester (2864),butyric acid ((2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4,5-trimethoxyphenyl)-tetrahydrofuran-3-yl)methyl ester (2629),(E)-2-methyl-2-butenoic acid ((2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4,5-trimethoxyphenyl)tetrahydrofuran-3-yl)methyl ester (2628),(Z)-2-methyl-2-butenoic acid ((2S,3R,4R)-2-(3,4-dimethoxyphenyl)-4-(pyridine-2-yl-methyl)tetrahydrofuran-3-yl)methyl ester (2823),(E)-2-butenoic acid ((2S,3R,4R)-4-(3,4-dimethoxybenzyl)-2-(3,4- ...

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Номер записи: 82
23-05-2019 дата публикации

NOVEL COMPOUND PROMOTING OSTEOBLAST DIFFERENTIATION AND INHIBITING ADIPOCYTE DIFFERENTIATION, PREPARATION METHOD THEREOF AND APPLICATION THEREOF

Номер: US20190152935A1
Автор: BANG Min-hyuk, KIM Hyun Suk, KIM Ki Hyun, LEE YUNMI, PARK Kimoon, YANG Hee-Jin
Принадлежит: SUNG KYUN BIOTECH CO., LTD.

The present disclosure relates to a compound having the activity of promoting osteoblast differentiation and inhibiting adipocyte differentiation and a preparation method thereof. The novel compound of the present disclosure increases the expression of the gene ALP involved in the differentiation of osteoblasts, regulates expression of the genes PPARγ, aP2 and CD36 involved in the differentiation of adipocytes, increases bone mineral density (BMD) in an ovariectomized osteoporosis animal model and decreases adipocytes in the bone marrow. Therefore, it can be used as an active ingredient of a medication or a health functional food useful for metabolic bone disease or obesity. 2. The composition for preventing or treating metabolic bone disease according to claim 1 , wherein each of R claim 1 , R claim 1 , Rand R claim 1 , which may be identical or different from each other claim 1 , is independently selected from a group consisting of C-Calkyl and C-Calkoxy claim 1 , and{'sub': 2', '5, 'each of Rand R, which may be identical or different from each other, is independently selected from a group consisting of hydrogen, hydroxy, halogen and trifluoromethyl.'}4. The composition for preventing or treating metabolic bone disease according to claim 1 , which promotes osteoblast differentiation and inhibits adipocyte differentiation.5. The composition for preventing or treating metabolic bone disease according to claim 4 , which prevents or treats obesity and metabolic bone disease at the same time.7. The health functional food for improving or preventing metabolic bone disease according to claim 6 , wherein each of R claim 6 , R claim 6 , Rand R claim 6 , which may be identical or different from each other claim 6 , is independently selected from a group consisting of C-Calkyl and C-Calkoxy claim 6 , and{'sub': 2', '5, 'each of Rand R, which may be identical or different from each other, is independently selected from a group consisting of hydrogen, hydroxy, halogen and ...

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Номер записи: 83
08-06-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170158674A1
Автор: Brewster William K., CAMPER Debra L., Gundla Rambabu, Gustafson Gary D., Hunter James E., Iyer Pravin S., Joshi Hemant, Lo William C., Lorsbach Beth, Loso Michael R., Mandaleswaran Adiraj, Patny Akshay, Pernich Dan, Sanam Ramadevi, Sparks Thomas C., Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A molecule according to wherein R2 and R4 are selected from F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , and NOand R1 claim 1 , R3 claim 1 , and R5 are H.3. A molecule according to wherein R2 claim 1 , R3 claim 1 , and R4 are selected from F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , CN claim 1 , and NOand R1 claim 1 , and R5 are H.4. A molecule according to wherein R2 claim 1 , R3 claim 1 , and R4 are independently selected from F and Cl and R1 and R5 are H.5. A molecule according to wherein R1 is selected from Cl and H.6. A molecule according to wherein R2 is selected from CF claim 1 , CH claim 1 , Cl claim 1 , F claim 1 , and H.7. A molecule according to wherein R3 is selected from OCH claim 1 , CH claim 1 , F claim 1 , Cl claim 1 , or H.8. A molecule according to wherein R4 is selected from CF claim 1 , CH claim 1 , Cl claim 1 , F claim 1 , and H.9. A molecule according to wherein R5 is selected from F claim 1 , Cl claim 1 , and H.10. A molecule according to wherein R6 is trifluoromethyl.11. A molecule according to wherein R7 is selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , and I.12. A molecule according to wherein R7 is selected from H claim 1 , OCH claim 1 , and OH.13. A molecule according to wherein R8 is selected from CHand H.14. A molecule according to wherein R10 is selected from Cl claim 1 , Br claim 1 , CH claim 1 , and CF.15. A composition comprising a molecule according to and further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and ...

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Номер записи: 84
08-06-2017 дата публикации

PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO

Номер: US20170158675A1
Автор: Boruwa Joshodeep, Hunter James E., Iyer Pravin S., Lo William C., Patny Akshay, Watson Gerald B.
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): 2. A composition according to further comprising:(a) one or more compounds having acaricidal, algicidal, avicidal, bactericidal, fungicidal, herbicidal, insecticidal, molluscicidal, nematicidal, rodenticidal, or virucidal properties; or(b) one or more compounds that are antifeedants, bird repellents, chemosterilants, herbicide safeners, insect attractants, insect repellents, mammal repellents, mating disrupters, plant activators, plant growth regulators, or synergists; or(c) both (a) and (b).3. A composition according to wherein further comprising one or more compounds selected from: (3-ethoxypropyl)mercury bromide claim 1 , 1 claim 1 ,2-dichloropropane claim 1 , 1 claim 1 ,3-dichloropropene claim 1 , 1-methylcyclopropene claim 1 , 1-naphthol claim 1 , 2-(octylthio)ethanol claim 1 , 2 claim 1 ,3 claim 1 ,5-tri-iodobenzoic acid claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-dimethylammonium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-lithium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-potassium claim 1 , 2 claim 1 ,3 claim 1 ,6-TBA-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-2-ethylhexyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-3-butoxypropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-TB claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butometyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butotyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-butyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isobutyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isoctyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-isopropyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-methyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-pentyl claim 1 , 2 claim 1 ,4 claim 1 ,5-T-sodium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-triethylammonium claim 1 , 2 claim 1 ,4 claim 1 ,5-T-trolamine claim 1 , 2 claim 1 ,4-D claim 1 , 2 claim 1 ,4-D-2-butoxypropyl claim 1 , 2 claim 1 ,4-D-2-ethylhexyl claim 1 , 2 claim 1 ,4-D-3- ...

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Номер записи: 85
14-05-2020 дата публикации

DECARBOXYLATIVE CROSS-COUPLING AND APPLICATIONS THEREOF

Номер: US20200148668A1
Автор: MACMILLAN David W.C., ZUO Zhiwei
Принадлежит:

Methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. For example, methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. A method described herein, in some embodiments, comprises providing a reaction mixture including a photoredox catalyst, a transition metal catalyst, a coupling partner and a substrate having a carboxyl group. The reaction mixture is irradiated with a radiation source resulting in cross-coupling of the substrate and coupling partner via a mechanism including decarboxylation, wherein the coupling partner is selected from the group consisting of a substituted aromatic compound and a substituted aliphatic compound. 1. A method of cross-coupling comprising:providing a substrate including a carboxyl group;oxidizing the carboxyl group via a single electron transfer process, wherein the substrate subsequently undergoes decarboxylation to provide a substrate radical; andforming a C—C bond between the substrate radical and a coupling partner selected from the group consisting of a substituted aromatic compound and substituted aliphatic compound.2. The method of claim 1 , wherein the substrate is an aliphatic carboxylic acid.3. The method of claim 1 , wherein the aliphatic carboxylic acid is an amino acid.4. The method of claim 1 , wherein the aliphatic carboxylic acid is a fatty acid.5. The method of claim 1 , wherein the aliphatic carboxylic acid is of formula R—COH claim 1 , wherein Ris selected from the group consisting of -alkyl claim 1 , -cycloalkyl claim 1 , -heteroalkyl claim 1 , -heterocycloalkyl claim 1 , -alkenyl claim 1 , -cycloalkenyl claim 1 , -heteroalkenyl claim 1 , -heterocycloalkenyl claim 1 , -alkynyl claim 1 , -alkyl-aryl claim 1 , -alkyl-heteroaryl claim 1 , -alkyl-alkoxy claim 1 , -alkenyl-aryl claim 1 , - ...

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Номер записи: 86
28-08-2014 дата публикации

HYDROGENOLYSIS OF FURFURYL ALCOHOL TO 1,2-PENTANEDIOL

Номер: US20140243562A1
Автор: Brehme Volker, CLAUS Peter, ECKERT Rene, Lucas Martin, Neumann Manfred, OMEIS Marianne, THEIS Christoph, Wolf Dorit
Принадлежит: Evonik Industries AG

The present invention provides a process for preparing 1,2-pentanediol by reacting furfuryl alcohol with hydrogen in the presence of a catalyst system. The catalyst system contains platinum oxide or contains ruthenium supported on aluminum oxide or activated carbon. The invention also relates to the respective catalysts and processes for producing the catalyst system. 1. A process for preparing 1 ,2-pentanediol , the process comprising:reacting furfuryl alcohol with hydrogen in the presence of a catalyst system to obtain a reaction mixture comprising 1,2-pentanediol; (I) ruthenium and', '(II) a support comprising aluminum oxide;, 'wherein the catalyst system compriseswherein the ruthenium is supported on the aluminum oxide.2. The process according to claim 1 , wherein the aluminum oxide is AlO.3. The process according to claim 1 , wherein a content of the ruthenium is from 0.01 to 30% by weight claim 1 , based on a total weight of the catalyst system.4. The process according to claim 1 , wherein a BET surface area of the catalyst system is from 50 to 250 m/g.5. The process according to claim 1 , wherein an average pore volume of the catalyst system is from 0.2 to 0.8 ml/g.7. The process according to claim 1 , wherein a reaction temperature is from 100° C. to 280° C.8. The process according to claim 1 , wherein a reaction pressure is equal to or greater than 10 bar.9. The process according to claim 1 , wherein the reaction is conducted in a solvent selected from the group consisting of water claim 1 , ethanol claim 1 , tetrahydrofuran and 1 claim 1 ,4-dioxane.10. The process according to claim 1 , wherein a pH of the reaction is from 5.3 to 10.5.11. The process according to claim 1 , wherein the reaction is conducted continuously.12. The process according to claim 1 , wherein the reaction is conducted batchwise.13. The process according to claim 1 , wherein the catalyst system is obtained by a method comprising:a) producing a mixture (i) comprising a ruthenium salt ...

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Номер записи: 87
24-06-2021 дата публикации

Series of Skin-Whitening (Lightening) Compounds

Номер: US20210188751A1
Автор: Hertel Carmen, Liu Jiyun, Nandy Sandip K., Nesterov Alexandre Mikhailovitch, Papmapiya Abeysinghe Arrachchigae
Принадлежит: Unigen, Inc.

The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin. 160-: (canceled)62. The compound of claim 61 , wherein:{'sub': '1', 'Ris H; and'}{'sub': 1', '10, 'R′ is 1 to 3 moieties (R′, R″, R′″) independently selected from the group consisting of a C-Calkoxy group or a hydroxyl group.'}63. A composition comprising the compound of and a pharmaceutically or cosmetically acceptable carrier.64. A composition comprising the compound of and a pharmaceutically or cosmetically acceptable carrier. This application claims the benefit of U.S. Provisional Application Ser. No. 61/082,422, filed Jul. 21, 2008, which is incorporated herein by reference in its entirety.The present invention is directed to novel tyrosinase inhibitors, pharmaceutical, dermatologic and cosmetic compositions comprising such inhibitors, and methods of making and using the same.The color of human skin is determined by the amount and the type of melanin produced by specialized cells, melanocytes, which are located in the basal layers of skin. Melanin, one of the most widely distributed natural pigments, is a homogeneous polyphenol-like biopolymer with a complex structure and color varying from brown to black (eumelanin) and red to yellow (pheomelanin) (Prota G. 1988, 8, 525-556). In human skin, melanin is believed to act as a protective agent against ultraviolet radiation. As such, people living close to equator have darker skin than those living in areas away from the equator.Overproduction of melanin can causes different types of abnormal skin color, hair color, and other dermatological disorders, such as melasma, age spots and sites of actinic damage. Melanin is produced ...

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Номер записи: 88
14-06-2018 дата публикации

ROR GAMMA (RORY) MODULATORS

Номер: US20180162809A1
Автор: CALS Joseph Maria Gerardus Barbara, DE KIMPE Vera, NABUURS Sander Bernardus
Принадлежит:

The present invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof. The compounds can be used as inhibitors of RORy and are useful for the treatment of RORy mediated diseases such as autoimmune and inflammatory diseases. 2. The compound according to wherein all of the positions A in A-Aare carbon.3. The compound according to wherein one of the positions A in A-Ais N claim 1 , the remaining position A being carbon.4. The compound according to wherein either position Aor Ais N and the remaining positions A in A-Aare CR-CR.5. The compound according to wherein either position Aor Ais N and the remaining positions A in A-Aare CR-CR.6. The compound according to wherein R-Rare independently H claim 1 , halogen or methyl.7. The compound according to where Ris C(1-3)alkyl.8. The compound according to wherein Rand Rare both H.9. The compound according to where Ris H.10. The compound according to where Ris C(3-6)cycloalkyl claim 1 , C(3-6)cycloalkylC(1-3)alkyl claim 1 , C(2-5)heterocycloalkyl claim 1 , C(4)heterocycloalkyl-C(1-3)alkyl claim 1 , C(6)aryl claim 1 , C(6)arylC(1-3)alkyl claim 1 , C(1-5)heteroaryl or C(1-5)heteroaryl-C(1-3)alkyl claim 1 , all groups optionally substituted with one or more halogen claim 1 , amino claim 1 , hydroxy claim 1 , cyano claim 1 , C(1-3)alkoxy claim 1 , C(1-3)alkoxycarbonyl claim 1 , (di)C(1-3)alkylamino or C(1-3)alkyl.11. The compound according to where Ris H claim 1 , C(1-6)alkyl claim 1 , C(2-6)alkenyl claim 1 , C(3-6)cycloalkyl claim 1 , C(3-6)cycloalkylC(1-3)alkyl claim 1 , C(4)heterocycloalkyl claim 1 , C(2-5)heterocycloalkylC(1-3)alkyl claim 1 , C(6)aryl claim 1 , C(6)arylC(1-3)alkyl claim 1 , C(1-5)heteroaryl or C(1-5)heteroarylC(1-3)alkyl claim 1 , all groups optionally substituted with one or more halogen claim 1 , amino claim 1 , hydroxy claim 1 , cyano claim 1 , C(1-3)alkoxy claim 1 , C(1-3)alkoxycarbonyl claim 1 , (di)C(1-3)alkylamino or C(1-3)alkyl.12. The compound according to ...

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Номер записи: 89
14-06-2018 дата публикации

COMPOUNDS USEFUL IN THE SYNTHESIS OF HALICHONDRIN B ANALOGS

Номер: US20180162885A1
Автор: Chase Charles E., Endo Atsushi, Fang Francis G.
Принадлежит:

In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate. Exemplary compounds are of formula (I), (II), or (III): 1. (canceled)4. The method of claim 2 , wherein Q is —(CH)OY.5. The method of claim 2 , wherein claim 2 , in the compound of formula (I) claim 2 , Y claim 2 , together with the oxygen to which it is bound claim 2 , is an ester claim 2 , carbonate claim 2 , carbamate claim 2 , sulfonate claim 2 , or ether hydroxyl protecting group.6. The method of claim 2 , wherein claim 2 , in the compound of formula (I) claim 2 , Yis pivaloyl claim 2 , acetyl claim 2 , benzoyl claim 2 , p-bromobenzoyl claim 2 , p-methoxybenzoyl claim 2 , 1-naphthoyl claim 2 , 2-naphthoyl claim 2 , o-phthaloyl claim 2 , benzyl claim 2 , p-methoxybenzyl claim 2 , triphenylmethyl claim 2 , tri(C1-C6 alkyl)silyl claim 2 , tri(C6-C10 aryl or C1-C6 heteroaryl)silyl claim 2 , di(C6-C10 aryl or C1-C6 heteroaryl)(C1-C6 alkyl)silyl claim 2 , or (C6-C10 aryl or C1-C6 heteroaryl)di(C1-C6 alkyl)silyl.7. The method of claim 2 , wherein X is halogen.8. The method of claim 2 , wherein Z is halogen or (C1-C6)alkylsulfonate.9. The method of claim 2 , wherein Z is triflate claim 2 , iodide claim 2 , or bromide.13. The method of claim 2 , wherein claim 2 , in the compound of formula (II) claim 2 ,{'sub': 2', '3', '1, 'Q is —(CH)OY;'}{'sub': '1', 'Y, together with the oxygen atom to which it is bound, is an ester, carbonate, carbamate, sulfonate, or ether hydroxyl protecting group;'}{'sub': 3', '4', '3', '4', '3', '4', '5, 'each of Yand Yis, independently and together with the oxygen atom to which it is bound, an ester, carbonate, carbamate, sulfonate, or ether hydroxyl protecting group, or Yand Ytogether with the oxygen atoms to which they are bound are a cyclic carbonate, cyclic boronate, or cyclic silylene hydroxyl protecting group, or Yand Ytogether are acetal, ketal, or 1,1, ...

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Номер записи: 90
11-09-2014 дата публикации

CATHEPSIN INHIBITORS

Номер: US20140256698A1
Автор: Booth Robert, Dener Jeff, Green Michael
Принадлежит:

The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.

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Номер записи: 91
01-07-2021 дата публикации

A LUBRICANT COMPRISING 2,5-(BISHYDROXYMETHYL) TETRYHYDROFURAN DIALKANOATES

Номер: US20210198590A1
Автор: Bohn Martin Alexander, ECORMIER Muriel, Geyer Karolin, Grabarse Wolfgang, Scherer Markus, Strittmatter Jan
Принадлежит:

A lubricant comprising 2,5-(bishydroxymethyl) tetryhydrofuran dialkanoates This invention relates to a lubricant comprising a THF ester of the formula (I) as defined below. This invention further relates to a use of the THF ester as lubricant; and to a method for reducing friction between moving surfaces comprising the step of contacting the surfaces with the lubricant or with the THF ester. 111.-. (canceled)13. The lubricant according to claim 12 , wherein Rand Rare linear or branched alkyl.14. The lubricant according to claim 12 , wherein Rand Rare selected independently from C-Calkyl.15. The lubricant according to claim 12 , wherein Rand Rare independently selected from the group consisting of hexyl claim 12 , heptyl claim 12 , octyl claim 12 , nonyl claim 12 , decyl claim 12 , undecyl claim 12 , dodecyl claim 12 , tridecyl claim 12 , tetradecyl claim 12 , pentadecyl claim 12 , hexadecyl claim 12 , heptadecyl claim 12 , octadecyl claim 12 , 2-ethylhexyl claim 12 , 2-propyl-heptyl claim 12 , 2-butyloctyl claim 12 , 2-pentylnonyl claim 12 , 2-hexyldecyl claim 12 , isohexyl claim 12 , isoheptyl claim 12 , isooctyl claim 12 , isononyl claim 12 , isodecyl claim 12 , isoundecyl claim 12 , isododecyl claim 12 , isotridecyl claim 12 , isotetradecyl claim 12 , isopentadecyl claim 12 , isohexadecyl claim 12 , isoheptadecyl claim 12 , isooctadecyl and mixtures thereof.16. The lubricant according to claim 12 , wherein Requals R.17. The lubricant according to claim 12 , wherein the THF ester is miscible with a polyalphaolefine having a kinematic viscosity at 100° C. of about 6 cSt.18. The lubricant according to claim 12 , wherein starting materials used for the preparation of the THF ester of the formula (I) originate at least partially from a renewable source.19. The lubricant according to claim 12 , further comprisinga base oil selected from mineral oils, polyalphaolefins, polymerized and interpolymerized olefins, alkyl naphthalenes, alkylene oxide polymers, silicone oils, ...

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Номер записи: 92
06-06-2019 дата публикации

ANIONIC SURFACTANTS AND DETERGENTS AND CLEANING AGENT CONTAINING SAME

Номер: US20190169531A1
Автор: Hausoul Peter, Kipshagen Lukas, Klemmer Anna, Kropf Christian, Palkovits Regina, Schulz Alexander
Принадлежит: Henkel AG & Co. KGaa

An anionic surfactant of general formula (I) in which n and m are, independently of one another, numbers from 0 to 17 and 2 Подробнее

Номер записи: 93
06-06-2019 дата публикации

POLYMERIZABLE COMPOSITION COMPRISING AN OXIME SULFONATE AS THERMAL CURING AGENT

Номер: US20190171099A1
Автор: Kunimoto Kazuhiko, Kura Hisatoshi, MATSUOKA Yuki, Sameshima Kaori
Принадлежит: BASF SE

The present invention relates to a polymerizable composition comprising at least one ethylenically unsaturated, polymerizable compound and at least one oxime sulfonate compound of the formula I 144-. (canceled)47: The compound of formula I according to claim 45 , where{'sup': '14', 'X is S or NRand'}{'sup': 14', '6', '14a', '8', '9', '10', '11', '4', '5', '6', '7', '8', '9', '10', '11, 'sub': 1', '12', '3', '8', '1', '8', '1', '4', '2, 'Ris C-C-alkyl, which may be interrupted by one or more O, S, NRor CO and/or may be substituted by one or more identical or different radicals Rselected from CN, COR, COOR, CONRR, phenyl and C-C-cycloalkyl which may interrupted by one or two CO groups and where the two last-mentioned radicals may be substituted by one or more identical or different radicals selected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COORand CONRR;'}{'sub': 2', '12', '3', '8', '1', '8', '1', '4', '2, 'sup': 6', '14a', '8', '9', '10', '11', '4', '5', '6', '7', '8', '9', '10', '11, 'C-C-alkenyl, which may be interrupted by one or more O, S, NRor CO and/or may be substituted by one or more identical or different radicals Rselected from CN, COR, COOR, CONRR, phenyl and C-C-cycloalkyl which may interrupted by one or two CO groups and where the two last-mentioned radicals may be substituted by one or more identical or different radicals selected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COORand CONRR;'}{'sub': 3', '12', '1', '8, 'sup': 14b', '8', '9', '10', '11, 'C-C-cycloalkyl, which may be interrupted by one or more CO and/or may be substituted by one or more identical or different radicals Rselected from C-C-alkyl, CN, COR, COOR, CONRR;'}{'sup': 14c', '4', '5', '6', '7', '8', '9', '10', '11, 'sub': 1', '8', '1', '4', '2, 'phenyl, which may be substituted by one or more identical or different radicals Rselected from C-C-alkyl, C-C-haloalkyl, F, Cl, Br, I, CN, NO, SR, OR, NRR, COR, COOR, CONRRand phenyl,'}or ...

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Номер записи: 94
18-09-2014 дата публикации

SUBSTITUTED 3-PHENYLPROPYLAMINE DERIVATIVES FOR THE TREATMENT OF OPHTHALMIC DISEASES AND DISORDERS

Номер: US20140275043A1
Автор: Hong Feng, Kubota Ryo, Kuksa Vladimir A., Orme Mark W.
Принадлежит: Acucela Inc.

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted 3-phenylpropylamine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 2. The compound of claim 1 , wherein A is —O—.3. The compound of claim 1 , wherein A is —CH—.4. The compound of claim 1 , wherein Ris OH and Ris H.5. The compound of claim 1 , wherein Rand Rare both hydrogen.6. The compound of claim 1 , wherein Ris hydrogen and Ris C-Calkyl.7. The compound of claim 1 , wherein Ris hydrogen and Ris —C(═O)R.10. A compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , selected from the group consisting of:(R)-3-Amino-1-(3-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)propan-1-ol;3-Amino-1-(3-((tetrahydro-2H-pyran-4-yl)methoxy)phenyl)propan-1-ol;(1R)-3-Amino-1-(3-((tetrahydro-2H-pyran-3-yl)methoxy)phenyl)propan-1-ol;(R)-3-Amino-1-(3-(pyridin-4-ylmethoxy)phenyl)propan-1-ol;(R)-3-Amino-1-(3-(pyridin-3-ylmethoxy)phenyl)propan-1-ol;(R)-3-Amino-1-(3-(pyridin-2-ylmethoxy)phenyl)propan-1-ol;(1R)-3-amino-1-(3-((tetrahydro-2H-thiopyran-3-yl)methoxy)phenyl)propan-1-ol;(R)-3-Amino-1-(3-((tetrahydro-2H-thiopyran-4-yl)methoxy)phenyl)propan-1-ol;(R)-4-((3-(3-Amino-1-hydroxypropyl)phenoxy)methyl)tetrahydro-2H-thiopyran 1,1-dioxide;3-((3-((R)-3-Amino-1-hydroxypropyl)phenoxy)methyl)tetrahydro-2H-thiopyran 1,1-dioxide;(R)-1-(4-((3-(3-amino-1-hydroxypropyl)phenoxy)methyl)piperidin-1-yl)ethanone;(R)-3-Amino-1-(3-((6-methylpyridin-2-yl)methoxy)phenyl)propan-1-ol;(1R)-3-Amino-1-(3-((2,3-dihydrobenzofuran-2-yl)methoxy)phenyl)propan-1-ol;(1R)-3-Amino-1-(3-((tetrahydrofuran-2-yl)methoxy)phenyl)propan-1-ol;(R)-3-Amino-1-(3-(piperidin-4-ylmethoxy)phenyl)propan-1-ol;(R)-3-Amino-1-( ...

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Номер записи: 95
07-07-2016 дата публикации

PROCESS FOR PRODUCTION OF HEXANETRIOL FROM 5-HYDROXYMETHYLFURFURAL

Номер: US20160194298A1
Автор: DIAS ERIC L., HAGEMEYER Alfred, Lavrenko Mayya, Murphy Vincent J., SHOEMAKER James A. W., Sokolovskii Valery
Принадлежит:

Industrial scale conversions of 5-hydroxymethylfurfural to commodity chemicals such as 1,2,6-hexanetriol and 1,6-hexanediol by chemocatalytic conversions using hydrogen and a heterogeneous reduction catalyst are provided. The reactions are suitable for use in continuous flow reactors. Methods of carrying out the conversions are provided, as are product and catalyst compositions. 1. A process for preparing 2 ,5-bis-hydroxymethylfuran (BHMF) from 5-hydroxymethylfurfural (HMF) comprising:reacting the 5-hydroxymethylfurfural (HMF) with hydrogen in a continuous flow reactor in the presence of an organic solvent and a heterogeneous reduction catalyst comprising at least one metal selected from the group consisting of Ni, Co, Cu, Ag, Pt, Pd, Fe and Ru or a combination thereof to form the 2,5-bis-hydroxymethylfuran (BHMF), wherein the process further comprises one or more of (i)-(iii):(i) forming the 2,5-bis-hydroxymethylfuran (BHMF) over an on-stream period of at least 150 hours;(ii) feeding the 5-hydroxymethylfurfural (HMF) through a guard bed comprising a transition metal to the continuous flow reactor;(iii) feeding the 5-hydroxymethylfurfural (HMF) to the continuous flow reactor for an on-stream period of at least 150 hours.2. The process of claim 1 , wherein the 2 claim 1 ,5-bis-hydroxymethylfuran (BHMF) is formed with at least about 90% selectivity and at least 85% conversion of the 5-hydroxymethylfurfural (HMF).3. The process of claim 1 , wherein the organic solvent comprises less than about 25 weight % water.4. The process of claim 1 , wherein the heterogeneous reduction catalyst further comprises a modifier.5. The process of claim 1 , wherein the heterogeneous reduction catalyst further comprises a catalyst support.6. The process of claim 1 , wherein the 5-hydroxymethylfurfural (HMF) is reacted with hydrogen at a temperature in a range of about 50° C. to about 150° C. and at a pressure in a range of about 50 psi to about 2000 psi.7. The process of claim 1 , further ...

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Номер записи: 96
06-07-2017 дата публикации

1-(CYCLOPENT-2-EN-1-YL)-3-(2-HYDROXY-3-(ARYLSULFONYL)PHENYL)UREA DERIVATIVES AS CXCR2 INHIBITORS

Номер: US20170190681A1
Автор: CHEN Weichun, IGBOKO Ebere F., LIN Xichen, LU Hongfu, Ren Feng, WREN Paul Bryan, XU Zhongmiao, Yang Ting, ZHU Lingdong
Принадлежит: Glaxosmithline Intellectual Property Development Limited

The invention relates to 1-(3-sulfonylphenyl)-3-(cyclopent-2-en-1-yl)urea derivatives, and their use in treating or preventing diseases and conditions mediated by the CXCR2 receptor In addition, the invention relates to compositions containing the derivatives and processes for their preparation 2. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris methyl claim 1 , fluoro or chloro3. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris H claim 1 , fluoro or chloro4. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris chloro or cyano5. The compound according to or a pharmaceutically acceptable salt thereof wherein Ris selected from the group consisting of.{'sub': 1-6', '1-3', '1-3', '1-3, 'a) Calkyl optionally substituted by one or more substituents independently selected from the group consisting of fluoro, Calkoxy, Cfluoroalkyl, Cfluoroalkoxy and hydroxy;'}{'sub': 2', 'q, 'claim-text': q is 0, 1 or 2,', {'sub': 2', 'q, 'the —(CH)— linker is optionally substituted by one or more groups independently selected from fluoro and methyl optionally substituted by one or more deuterium,'}, {'sub': 2', 'q, 'the heterocyclyl group is 3, 4, 5 or 6-membered and is attached to the —(CH)— via a ring carbon atom,'}, 'the heterocyclyl is saturated or unsaturated, and', {'sub': 1-3', '1-3', '1-3', '1-3', '1-3', '1-3', '3-6', '2', 'S', '1-3, 'sup': 4c', '4d', '4c', '4d', '4c', '4d, 'wherein the heterocyclyl group is optionally substituted by one or more substituents independently selected from the group consisting of deuterium, Calkyl optionally substituted by one or more deuterium, fluoro, Cfluoroalkyl, hydroxy, Calkoxy, CalkoxyCalkyl, Cfluoroalkoxy, Ccycloalkyl and —(CH)NRR, or two substituents on the heterocyclyl group together with the interconnecting atom(s), form a further 5 or 6-membered ring which further ring is saturated, unsaturated or aromatic when the further ring is ortho- ...

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Номер записи: 97
22-07-2021 дата публикации

CRYSTAL FORMS OF TETRAHYDRO-N,N-DIMETHYL-2,2-DIPHENYL-3-FURANMETHANAMINE HYDROCHLORIDE, PROCESSES OF MAKING SUCH FORMS, AND THEIR PHARMACEUTICAL COMPOSITIONS

Номер: US20210220321A1
Автор: Daintree Linda Sharon, Ledger Daniel Mark, Leonard Lucy Anne, YORK Peter
Принадлежит: ANAVEX LIFE SCIENCES CORP.

Polymorphic forms of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) and a metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73) are disclosed and characterized. Compositions and method for treatment of Alzheimer's disease that includes the polymorphic forms and metabolite of tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride (ANAVEX2-73). 1. A method of making a crystal form of ANAVEX2-73 , comprising crystallizing the ANAVEX2-73 in a supercritical fluid (SCF) environment.2. The method of claim 1 , wherein the supercritical fluid comprises supercritical carbon dioxide.3. The method of claim 1 , wherein the crystallizing comprises:a. making a solution of ANAVEX2-73 in a solvent;b. introducing the solution to the SCF;c. allowing crystallization of ANAVEX2-73 in the SCF environment to form crystals;d. isolating the crystals, thus obtaining the crystal form of ANAVEX2-73.4. The method of claim 3 , wherein the solvent comprises ethanol claim 3 , acetonitrile claim 3 , isopropyl alcohol claim 3 , trifluoroethanol claim 3 , acetone claim 3 , 3-methyl-I-butanol claim 3 , 2-ethoxyethanol claim 3 , 1-propanol claim 3 , dichloromethane claim 3 , dimethyl sulfoxide claim 3 , N claim 3 ,N′-dimethylacetamide claim 3 , dimethylformamide claim 3 , trifluoroethanol claim 3 , 1:9 v/v trifluoroethanol+ethanol claim 3 , 1:1 v/v acetone+ethanol claim 3 , 3-methyl-1-butanol claim 3 , N-methyl-2-pyrrolidone claim 3 , tert-butanol claim 3 , or a combination thereof.5. The method of claim 3 , wherein the SCF environment comprises pressure from about 85 bar to about 200 bar claim 3 , temperature ranging from about 40° C. to about 80° C. claim 3 , and TS flow ranging from about 0.1 g/min to about 1.7 g/min.6. A crystal form produced according to the method of claim 1 , substantially characterized by an X-ray diffraction pattern of claim 1 , claim 1 , or .7. The crystal form of claim 6 , further ...

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Номер записи: 98
13-07-2017 дата публикации

CHELATE-CONTROLLED DIASTEREOSELECTIVE HYDROGENATION WITH HETEROGENEOUS CATALYST

Номер: US20170197929A1
Автор: Anderson Craig, DALY John Ing Chuan, Dunn David, Gamboa Martinez Sergio Aaron, Gibbings Matthew Richard, Grant Simon Jonathon, Hutchings Lian, Ribiere Patrice Georges Antonin, Rogan Yulia, SUTTON Howard Winston Tyrrell
Принадлежит:

A catalyst, method of using, and use of a hydrogenation catalyst, preferably palladium on a support, preferably alumina or activated charcoal support. This in the presence of lithium salts, with salts such as the borates being preferred. This provides hydrogenation of precursors to give rise to a stereoselective, such as diastereoselective bias in the product of alkene hydrogenation using the catalyst. 2. The method of claim 1 , wherein more than 52% meso isomer is produced.3. The method of claim 1 , wherein more than 56% meso isomer is produced.4. The method of claim 1 , wherein the substrate is 2 claim 1 ,2-di(2-furyl)propane and the hydrogenation product is 2 claim 1 ,2′-di(2-tetrahydrofuryl)propane.5. The method of claim 1 , wherein the metal hydrogenation catalyst is selected from the group consisting of platinum claim 1 , palladium claim 1 , ruthenium claim 1 , rhodium and nickel.6. The catalyst composition of claim 5 , wherein the catalyst is palladium.7. The method of claim 1 , wherein the support is selected from the group consisting of carbon claim 1 , alumina claim 1 , silica claim 1 , titanium dioxide claim 1 , calcium carbonate claim 1 , lithium aluminate and barium sulfate.8. The method of claim 7 , wherein the support is selected from the group consisting of carbon and alumina.9. The method of claim 1 , wherein the lithium salt is selected from the group consisting of an organo-carboxylate claim 1 , an organo-sulfate claim 1 , aluminate claim 1 , hydroxide claim 1 , chloride claim 1 , bromide claim 1 , carbonate claim 1 , hydroxide claim 1 , borate and a mixture thereof.10. The method of claim 9 , wherein the lithium salt is selected from the group consisting of lithium tetraborate claim 9 , lithium metaborate claim 9 , and hydrates thereof.11. The method of wherein the method is performed in the presence of a solvent selected from the group consisting of heptane claim 1 , MTBE claim 1 , THF claim 1 , ethyl acetate claim 1 , methanol claim 1 , ethanol ...

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Номер записи: 99
21-07-2016 дата публикации

Synthesis of Diacids, Dialdehydes, or Diamines from THF-Diols

Номер: US20160207894A1
Автор: Stensrud Kenneth
Принадлежит:

A simple and elegant chemical process for the synthesis of oxygenated products, such as acids and aldehydes, or other derivative products, such as amines and nitriles, of cyclic bifunctional molecules made from renewable, bio-based sources such as HMF and/or its reduction product, 2,5-bis(hydroxymethyl)-tetrahydrofuran (bHMTHF) is described. In general, the process involves: a) generating a tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) from bHMTHFs using a sulfonate; b) displacing nucleophilically at least a sulfonate leaving group from the tetrahydrofuran-2,5-diyl-bis(methylene)-bis(sulfonate) to form a THF-dinitrile; and either c) oxidizing the THF-dinitrile with an acid having a pKa of ≦0 to generate a di-acid, or d) reducing partially the THF-dinitrile to generate a di-aldehyde, or e) reducing fully the THF-dinitrile to generate a di-amine. 126-. (canceled)27. A process for preparing either an oxygenated or amine product from 2 ,5-bis(hydroxymethyl)-tetrahydrofuran (bHMTHF) , comprising: a) derivatizing bHMTHF using a sulfonate to generate a tetrahydrofuran-2 ,5-diyl-bis(methylene)-bis(sulfonate); b) displacing at least a sulfonate leaving group from said tetrahydrofuran-2 ,5-diyl-bis(methylene)-bis(sulfonate) with a nucleophile; and either c) hydrolyzing fully with a strong acid having a pKa of ≦0 to generate a di-acid , or d) reducing partially to generate a di-aldehyde , or e) reducing fully to generate a diethyl-amine.28. The process according to claim 27 , wherein said di-acid is a tetrahydrofuran-2 claim 27 ,5-diyl-diacetic acid claim 27 , and said di-aldehyde is a tetrahydrofuran-2 claim 27 ,5-diacet-aldehyde.29. The process according to claim 27 , wherein said sulfonate is at least one of the following: methanesulfonate claim 27 , trifluoromethanesulfonate claim 27 , ethanesulfonate claim 27 , benzenesulfonate claim 27 , and p-toluenesulfonate.30. The process according to claim 27 , wherein said derivatization with said sulfonate involves a ...

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Номер записи: 100