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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 3301. Отображено 100.
10-07-2011 дата публикации

УСТАНОВКА ДЛЯ ПОЛУЧЕНИЯ ЦИКЛОГЕКСАНОНА И ЦИКЛОГЕКСАНОЛА

Номер: RU0000106245U1
Автор: Савош Эдуард Кизимирович, Сокол Борис Александрович, Сурба Анатолий Константинович, Таракановский Игорь Викторович
Принадлежит: Открытое акционерное общество "Щекиноазот"

1. Установка для получения циклогексанона и циклогексанола, включающая расположенные в технологической последовательности узел подачи реакционной жидкости, узел охлаждения реакционной жидкости, реактор нейтрализации продуктов окисления, разделительный сосуд первого органического и первого водно-щелочного слоя, узел разложения гидроперекиси циклогексила и оснащенный сепаратором узел отделения второго водно-щелочного слоя, связанный с узлом разложения гидроперекиси и реактором нейтрализации, и снабженный выводом второго органического слоя, отличающаяся тем, что между узлом охлаждения реакционной жидкости и реактором нейтрализации установлены узел отмывки, выполненный в виде смесителя охлажденной реакционной жидкости и воды и разделительный сосуд органического и водно-кислого слоев, который связан с экстрактором водно-кислого слоя и, далее, - с устройством очистки рафината, при этом экстрактор водно-кислого слоя и устройство очистки рафината дополнительно связаны с узлом отмывки реакционной жидкости водой, а устройство очистки рафината снабжено узлом отвода водно-кислого стока. 2. Установка по п.1, отличающаяся тем, что устройство очистки рафината связано с узлом отмывки реакционной жидкости водой через узел ее подачи. 3. Установка по п.1, отличающаяся тем, что разделительный сосуд органического и водно-кислого слоев выполнен в виде сепаратора или отстойника. 4. Установка по п.1, отличающаяся тем, что экстрактор водно-кислого слоя выполнен пульсационным или роторно-дисковым, или насадочным. 5. Установка по п.1, отличающаяся тем, что устройство очистки рафината выполнено в виде насадочной или тарельчатой ректификационной колонны. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 106 245 (13) U1 (51) МПК C07C C07C C07C C07C C07C B01J 27/32 (2006.01) 45/53 (2006.01) 29/50 (2006.01) 35/08 (2006.01) 49/403 (2006.01) 10/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ПОЛЕЗНОЙ МОДЕЛИ К ПАТЕНТУ (21)(22) Заявка: 2010154693/04, 30.12. ...

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Номер записи: 1
29-03-2012 дата публикации

Light-driven rotary molecular motors

Номер: US20120074336A1
Автор: Christine R. Cremo, John H. Frederick, Joseph I. Cline, Stephen L. Gillett, Thomas W. Bell
Принадлежит: Nevada System of Higher Education NSHE

Compounds of Formula ( 1 ) are disclosed: C b is a carbocyclic or heterocyclic group having an atom within the cyclic structure selected from C, N, Si, and C r and singly bound to A. A is CR, COR, CSR, CNR 2 , CCN, CCONR 2 , CNO 2 , CNNAr, CX′, or N. C r is a chromophore having a substantially planar cyclic structure. The compounds function as nanometer-scale rotary molecular motors powered and controlled by light energy. The design of the molecular motor devices is flexible so that the rotary direction, drive light wavelength, and other physical characteristics can be varied. The compounds can be chemically functionalized to allow it to be integrated into or attached to a variety of structures. The device can be used in applications where mechanical power, positional control, and information encoding are to be generated at the size scale of individual molecules.

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Номер записи: 2
18-04-2013 дата публикации

CYCLOHEXANE COMPOUND AND LIQUID CRYSTAL COMPOSITION CONTAINING THE SAME

Номер: US20130092875A1
Автор: Okamoto Kazuo, Shibata Toshihiro
Принадлежит:

The present invention intends to provide a novel cyclohexane compound that can form a liquid crystal composition of which response speed is improved when mixed with a nematic liquid crystal and the like and to provide a specified liquid crystal composition in which a novel cyclohexane compound is mixed. The novel cyclohexane compound is represented by the following formula (1). 5. A liquid crystal composition comprising:{'claim-ref': [{'@idref': 'CLM-00003', 'claim 3'}, {'@idref': 'CLM-00004', 'claim 4'}], 'the liquid crystal composition of mixed with at least one kind of a compound of a compound group of the formula (7) of .'}6. A liquid crystal composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'one or two or more kinds of the cyclohexane compound groups of .'}7. Use of the liquid crystal composition described in in an electrooptical application.8. An electrooptical display device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the liquid crystal composition of encapsulated in a liquid crystal cell.'} The present invention relates to a novel cyclohexane compound and a liquid crystal composition containing the new cyclohexane, and intends to improve the response speed of a liquid crystal display.Many liquid crystal display devices that make use of the optical anisotropy (Δn) (hereinafter, referred to as “Δn” in some cases) or the dielectric constant anisotropy (Δε) (hereinafter, referred to as “Δε” in some cases), which are features of a liquid crystal compound, have been manufactured and have been used in watches, calculators, measurement instruments, instrument panels for vehicles, word processors, electronic diaries, portable telephones, printers, computers, TVs and so on. A liquid crystal compound used in liquid crystal display devices has a specific liquid crystal phase, and the phase mode thereof can be roughly divided into a nematic phase, a smectic phase and a cholesteric phase. Among these, a nematic phase is most widely ...

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Номер записи: 3
25-04-2013 дата публикации

2-methylene-vitamin d analogs and their uses

Номер: US20130102573A1
Автор: Hector F. DeLuca, Izabela Sibilska, Lori A. Plum, Rafal R. Sicinski
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

This invention discloses 2-methylene-vitamin D analogs, and specifically (20S)-25-hydroxy-2-methylene-vitamin D 3 and (20R)-25-hydroxy-2-methylene-vitamin D 3 , as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also have relatively high calcemic activities evidencing use in the treatment of bone diseases.

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Номер записи: 4
09-05-2013 дата публикации

Agent for Treating Parkinson's Disease

Номер: US20130116319A1
Автор: "Ardashov Oleg Vasilevich", "Ilina Irina Viktorovna", Morozova Ekaterina Aleksandrovna, Pavlova Alla Viktorovna, Salahutdinov Nariman Faridovich, Tolstikova Tatiana Genrihovna, Volcho Konstantin Petrovich
Принадлежит: OOO "TOMSKAYA FARMATSEVTICHESKAYA FABRIKA"

The present invention relates to the use of 3-methyl-6-(1-methylethenyl)cyclohex-3-ene-1,2-diol, its isomers and derivatives, as a compound for Parkinson disease treatment, that can be used in medicine. The compound is highly active, low toxic and can be synthesized from available natural compound α-pinene. 2. The method of claim 1 , wherein the neurodegenerative disease comprises Parkinson's disease and/or parkinsonism.5. The method of claim 2 , wherein R1 and R2 are the same.6. The method of claim 2 , wherein the C1-C6 carbonic acid residue is substituted by a halogen atom selected from the group comprising F claim 2 , Cl claim 2 , I claim 2 , and Br.7. The method of claim 2 , wherein the medicinal preparation is suitable for peroral claim 2 , sublingual claim 2 , parenteral or local administration.8. The method of claim 3 , wherein R1 and R2 are the same.9. The method of claim 3 , wherein the C1-C6 carbonic acid residue is substituted by a halogen atom selected from the group comprising F claim 3 , Cl claim 3 , I claim 3 , and Br.10. The method of claim 3 , wherein the medicinal preparation is suitable for peroral claim 3 , sublingual claim 3 , parenteral or local administration.11. The method of claim 4 , wherein R1 and R2 are the same.12. The method of claim 4 , wherein the C1-C6 carbonic acid residue is substituted by a halogen atom selected from the group comprising F claim 4 , Cl claim 4 , I claim 4 , and Br.13. The method of claim 4 , wherein the medicinal preparation is suitable for peroral claim 4 , sublingual claim 4 , parenteral or local administration.14. The method of claim 1 , wherein administering to the patient a daily dose of the compound ranging from about 1 mg to about 500 mg comprises administering the daily dose of the compound as a stand-alone drug therapy or as a component of a form of treatment.15. The method of claim 2 , wherein administering to the patient a daily dose of the compound ranging from about 1 mg to about 500 mg comprises ...

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Номер записи: 5
16-05-2013 дата публикации

Compounds with a Woody Note

Номер: US20130123548A1
Автор: Chanot Jean-Jacques, Muratore Agnés
Принадлежит: V. MANE FILS

The invention relates to the chemistry of fragrances and to the field of perfumery. It relates more particularly to compounds with a woody note, responding to the general formula: 2. The compound according to claim 1 , characterised in that the ring with 6 carbon atoms is saturated.3. The compound according to any claim 1 , characterised in that the ring with 6 carbon atoms has a double bond between carbons C1 and C2 or between carbons C1 and C6.4. The compound according to claim 1 , characterised in that R is selected from: —CHCH claim 1 , —CHCH═CH claim 1 , —CHCHCH claim 1 , —CHCHCHCH claim 1 , —CHCH(CH) claim 1 , —CH(CH)CHCHand —CHCHCH(CH).5. The compound according to claim 1 , characterised in that it is selected from:2-(3,3-dimethylcyclohex-1-enyl)butan-2-ol2-(5,5-dimethylcyclohex-1-enyl)butan-2-ol2-(3,3-dimethylcyclohex-1-enyl)pent-4-en-2-ol2-(5,5-dimethylcyclohex-1-enyl)pent-4-en-2-ol 2-(5,5-dimethylcyclohex-1-enyl)pentan-2-ol', '2-(3,3-dimethylcyclohex-1-enyl)hexan-2-ol', '2-(5,5-dimethylcyclohex-1-enyl)hexan-2-ol', '2-(3,3-dimethylcyclohex-1-enyl)-4-methylpentan-2-ol', '2-(5,5-dimethylcyclohex-1-enyl)-4-methylpentan-2-ol', '2-(3,3-dimethylcyclohex-1-enyl)-3-methylpentan-2-ol', '2-(5,5-dimethylcyclohex-1-enyl)-3-methylpentan-2-ol', '2-(3,3-dimethylcyclohex-1-enyl)-5-methylhexan-2-ol', '2-(5,5-dimethylcyclohex-1-enyl)-5-methylhexan-2-ol', '2-(3,3-dimethylcyclohexyl)butan-2-ol', '2-(3,3-dimethylcyclohexyl)pent-4-en-2-ol', '2-(3,3-dimethylcyclohexyl)pentan-2-ol', '2-(3,3-dimethylcyclohexyl)hexan-2-ol', '2-(3,3-dimethylcyclohexyl)-4-methylpentan-2-ol', '2-(3,3-dimethylcyclohexyl)-5-methylhexan-2-ol., '2-(3,3-dimethylcyclohex-1-enyl)pentan-2-ol'}6. A perfumed composition comprising at least one compound according to .7. The composition according to claim 6 , characterised in that it is a traditional perfume composition.8. The composition according to claim 7 , characterised in that it is selected from: a perfuming concentrate claim 7 , an eau de Cologne claim 7 , ...

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Номер записи: 6
18-07-2013 дата публикации

Process for preparing 5-[1-(4-chlorophenyl)-methylene]-1-hydroxymethyl-2,2-dimethyl-cyclopentanol

Номер: US20130184470A1
Автор: ZIERKE Thomas
Принадлежит:

Process for preparing 5-[1-(4-chlorophenyl)-methylene]-1-hydroxymethyl-2,2-dimethyl-cyclopentanol 18-. (canceled)10. The process according to claim 9 , wherein the reaction a) is carried out at a temperature of (−10) to 40° C.11. The process according to claim 9 , wherein the hydrogenation b) is carried out at a temperature of (−10) to 40° C.12. The process according to claim 9 , wherein the reaction is carried out in a solvent or solvent mixture.13. The process according to claim 12 , wherein catalyst claim 12 , temperature and solvent or solvent mixture is selected such that the diol (Ia) is obtained in an excess relative to the diol (Ib).14. The process according to claim 12 , wherein the hydrogenation is carried out in the presence of a di(C-C-alkyl)formamid claim 12 , di(C-C-alkyl)acetamid or in N-methyl-2-pyrrolidone and palladium is used as catalyst. The present invention relates to a process for preparing diols of the formula (Ia) and (Ib)According to EP-A 359 305, compound (Ia) can be obtained by reacting either the corresponding epoxide (VII) or ester (VIII)wherein Rrepresents a hydrogen atom, an alkyl group or a cycloalkyl group, with a reducing agent, preferably a complex metal hydride, at a temperature from 35° C. to reflux temperature. However, these reagents suffer from being hazardous and expensive. EP-A 359 305 also teaches the use of the diols (Ia) and (Ib) for preparing fungicidal active cyclopentane derivatives such as Metconazole.EP-A 474303 discloses a method of selectively preparing the diol (Ia) from the well obtainable 1-(4-chlorobenzyl)-4,4-dimethyl-cyclohex-1-en-3-on (IX)However, this process requires, besides complex metal hydrides, the use of hydrogen per oxide, which requires challenging safety means in a technical plant.Therefore, it was an object of the present invention to provide a commercial feasible process for preparing the diols of the formula (I) from readily available starting materials, with (Ia) being obtained in an excess ...

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Номер записи: 7
25-07-2013 дата публикации

PROCESS FOR THE PREPARATION OF PROTOESCIGENIN

Номер: US20130190538A1
Автор: GILLER Tomasz, GRUZA Mariusz, GRYNKIEWICZ Grzegorz, JATCZAK Kamil, LASZCZ Marta, ZEGROCKA-STENDEL Oliwia
Принадлежит:

A process for the preparation of protoescigenin by hydrolysis of escin isolated from . The process includes the following steps: a two-step hydrolysis first under acidic and then basic conditions, enrichment of the crude mixture of sapogenins with protoescigenin, an isolation of the mixture of sapogenins in a solid form, and a purification of the obtained solid and isolation of high purity protoescigenin. The invention also relates to protoescigenin monohydrate in a crystalline form and the preparation thereof. Protoescigenin is a polyhydroxy aglycone, which can be used as a synthon in the chemical modifications of naturally occurring saponins. 1Aesculus hippocastanum. A process for the preparation of protoescigenin from escin isolated from the horse chestnut , the process comprising:a) a two-step hydrolysis of escin, consecutively under acidic and basic conditions, resulting in obtaining a crude mixture of sapogenins, b-i) dissolving the hydrolysis product of a) in a three-component mixture of solvents to obtain a clear mono- or bi-layer solution,', 'b-ii) addition of water to the solution obtained in step b-i), until a precipitation of a solid of the pre-purified mixture of sapogenins containing protoescigenin as the major component,, 'b) a process of enrichment of the crude mixture of sapogenins with protoescigenin, wherein said process consists of the following stepsc) isolation of the solid obtained in step b-ii),d) purification of the pre-purified mixture of sapogenins, ande) isolation of protoescigenin.2. The process of claim 1 , wherein the hydrolysis is carried out under acidic and basic conditions without isolation of the intermediate from the reaction mixture.3. The process of claim 1 , wherein the steps a) and b) are carried out without isolation of the intermediate from the reaction mixture.5. The process of claim 4 , wherein component 1 is methanol or propan-2-ol.6. The process of claim 4 , wherein component 3 is selected from a group consisting of ...

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Номер записи: 8
15-08-2013 дата публикации

SYNTHESIS OF BICYCLIC COMPOUNDS AND METHOD FOR THEIR USE AS THERAPEUTIC AGENTS

Номер: US20130210904A1
Автор: BOULANGER Martin J., BRANT Michael G., Bromba Caleb M., Mason Jeremy W., Wulff Jeremy E.
Принадлежит:

Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds. 2. The compound according to where the heteroatom-containing moiety is selected from aldehyde claim 1 , acyl halide claim 1 , carbonate claim 1 , carboxyl claim 1 , carboxylate claim 1 , ether claim 1 , ester claim 1 , hydroxyl claim 1 , ketone claim 1 , silyl ether claim 1 , peroxy claim 1 , hydroperoxy claim 1 , phosphate claim 1 , phosphonate claim 1 , phosphoryl claim 1 , phosphodiester claim 1 , phosphine claim 1 , pyrrole claim 1 , thiol claim 1 , thioether/sulfide claim 1 , disulfide claim 1 , sulfonyl claim 1 , sulfonyl claim 1 , carbonothioyl claim 1 , sulfino claim 1 , sulfo claim 1 , thiocyanate claim 1 , isothiocyanate claim 1 , oxazole claim 1 , oxadiazole claim 1 , imidazole claim 1 , triazole claim 1 , tetrazole claim 1 , amine claim 1 , amide claim 1 , azide claim 1 , azo claim 1 , cyano claim 1 , isocyanate claim 1 , imide claim 1 , nitrile claim 1 , isonitrile claim 1 , nitro claim 1 , nitroso claim 1 , nitromethyl claim 1 , selenol claim 1 , guanidino claim 1 , and substituted guanidino.4. The compound according to where Vis CRR claim 3 , C(R) claim 3 , or C(R) claim 3 , and any one of R claim 3 , R claim 3 , or Rtogether with Rform a lactam or lactone.5. ...

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Номер записи: 9
17-10-2013 дата публикации

FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF

Номер: US20130274240A1
Автор: Ito Hirotsugu, Kobayashi Satoru, Morita Toru, Motomura Takahisa, Nagamori Hironobu, Shinkai Hisashi, Suzawa Koichi
Принадлежит:

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: 217.-. (canceled)18. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , and a pharmaceutically acceptable carrier.1923.-. (canceled)24. A method of inhibiting PDHK in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.25. A method of inhibiting PDHK2 in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.26. A method of decreasing the blood glucose level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.27. A method of decreasing lactate level in a mammal claim 1 , comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof to the mammal.28. A method for the treatment or prophylaxis of diabetes claim 1 , diabetic complications claim 1 , insulin resistance syndrome claim 1 , metabolic syndrome claim 1 , hyperglycemia claim 1 , dyslipidemia claim 1 , atherosclerosis claim 1 , ...

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Номер записи: 10
31-10-2013 дата публикации

6a,7,7-TRIMETHYLDECAHYDRO-1,4-METHANOCYCLOPROPA[de]NAPHTHALEN-1-OL

Номер: US20130287707A1
Автор: Kobayashi Tsuyoshi, Nagano Junko, Yaguchi Yoshihiro, ZAIZEN Kyoko
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

As a novel compound which is excellent in odor quality and has an odor of a very clear and strong woody note, the invention provides a compound represented by the following formula (1): 2. The compound according to claim 1 , which is a (+)-isomer.3. The compound according to claim 1 , which is a (−)-isomer.4. The compound according to claim 1 , which is a mixture of a (+)-isomer and a (−)-isomer.5. The compound according to claim 1 , which is a racemate.6. A method for producing a flavor/fragrance composition claim 1 , comprising mixing the compound according to with a flavor/fragrance component.7. A method for producing a flavor/fragrance composition claim 2 , comprising mixing the compound according to with a flavor/fragrance component.8. A method for producing a flavor/fragrance composition claim 3 , comprising mixing the compound according to with a flavor/fragrance component.9. A method for producing a flavor/fragrance composition claim 4 , comprising mixing the compound according to with a flavor/fragrance component.10. A method for producing a flavor/fragrance composition claim 5 , comprising mixing the compound according to with a flavor/fragrance component.11. A method for producing a perfume claim 5 , a cosmetic claim 5 , a toiletry product claim 5 , a food claim 5 , a beverage claim 5 , an oral cavity composition claim 5 , or a pharmaceutical claim 5 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'mixing the compound according to with a flavor/fragrance component, to thereby obtain a flavor/fragrance composition; and'}incorporating the obtained flavor/fragrance composition into a perfume, a cosmetic, a toiletry product, a food, a beverage, an oral cavity composition, or a pharmaceutical.12. A method for producing a perfume claim 5 , a cosmetic claim 5 , a toiletry product claim 5 , a food claim 5 , a beverage claim 5 , an oral cavity composition claim 5 , or a pharmaceutical claim 5 , the method comprising:{'claim-ref': {'@idref ...

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Номер записи: 11
05-12-2013 дата публикации

Crystallization of (20R,22R)-2-Methylene-19-Nor-22-Methyl-1alpha,25-Dihydroxyvitamin D3 and Related Precursors

Номер: US20130324752A1
Автор: DeLuca Hector F., Flores Agnieszka, Grzywacz Pawel, Holden Hazel M., Plum Lori A., Thoden James B.
Принадлежит:

Disclosed are methods of purifying the compound (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dto obtain the compound in crystalline form. The methods typically include the steps of dissolving a product containing the compound in a solvent comprising hexane and 2-propanol, cooling the solvent and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of crystals, and recovering the crystals. Certain diol precursors formed during the synthesis of the compound and its diasteromers also may be obtained in crystalline form using ethyl acetate as a solvent. 2. A crystalline form of (20R ,22R)-2-methylene-19-nor-22-methyl-1α ,25-dihydroxyvitamin Dhaving molecular packing arrangement defined by space group C2 and unit cell dimensions a=27.03 Å b=6.47 Å c=17.41 Å α=90° , β=103.35° and γ=90°.3. A three dimensional structure for (20R claim 2 ,22R)-2-methylene-19-nor-22-methyl-1α claim 2 ,25-dihydroxyvitamin Das defined by the molecular packing arrangement set forth in .4. A method of purifying (20R claim 2 ,22R)-2-methylene-19-nor-22-methyl-1α claim 2 ,25-dihydroxyvitamin D claim 2 , comprising the steps of:(a) preparing a solvent comprising hexane;{'sub': '3', '(b) adding a product containing (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dto be purified to said hexane to form a suspension of the product in the hexane;'}(c) adding 2-propanol dropwise to the suspension to form a mixture of the product in the hexane and 2-propanol;{'sub': '3', '(d) heating the mixture to dissolve the product containing (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dto be purified in said mixture;'}{'sub': '3', '(e) cooling said mixture and dissolved product below ambient temperature for a sufficient amount of time to form a precipitate of (20R,22R)-2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin Dcrystals; and'}{'sub': '3', '(f) separating the (20R,22R)-2-methylene-19-nor-22-methyl-1α,25- ...

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Номер записи: 12
19-12-2013 дата публикации

NOVEL ALICYCLIC ALCOHOL

Номер: US20130338403A1
Автор: Ataka Yoshiharu, Fukuda Kazuyuki, Kitamura Mitsuharu
Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

Provided is an alicyclic alcohol compound which can be used as a raw material for a compound perfume, and which has excellent floral-green-like aromas which are crisp and fresh; also provided are a manufacturing method for the same, and a perfume composition which contains the alicyclic alcohol compound. An alicyclic alcohol compound having a specified structure represented by chemical formula (1) has excellent floral-green-like aromas which are crisp and fresh; and a method for manufacturing the alicyclic alcohol compound represented by chemical formula (1) by reacting, in the presence of hydrogen fluoride, 1-isopropyl-4-methylcyclohexene and carbon monoxide, reacting the resulting 4-isopropyl-1-methylcyclohexane carboxylic acid fluoride with alcohol, and, after having acquired a cyclohexane carbonyl compound, reducing the cyclohexane carbonyl compound. The present invention relates to an alicyclic alcohol compound which can be used as a raw material for compounded perfumes, a method for manufacturing the same, and a perfume composition containing said alicyclic alcohol compound.It is known that some of alicyclic alcohol compounds are useful for a raw material for compounded perfumes. For example, Non-patent Document 1 discloses that Mayol having green and muguet-like fragrance, Mugetanol having muguet-like light floral fragrance, Patchone having patchouli-like woody fragrance and the like are useful as a raw material for compounded perfumes.The object of the present invention is to provide a novel alicyclic alcohol compound having floral-green-like fragrance useful for a raw material for compounded perfumes, a method for manufacturing the same and a perfume composition containing said alicyclic alcohol compound.As a result of synthesizing various compounds and studying fragrances thereof, the present inventors have found that the alicyclic alcohol compound represented by the following chemical formula (1) which is a novel compound has excellent floral-green-like ...

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Номер записи: 13
16-01-2014 дата публикации

Blue Curls "Pirzada" and Related Compositions and Methods

Номер: US20140017178A1
Автор: Pirzada Syed Zebe
Принадлежит:

The present disclosure embrace Blue Curls () var. Pirzada and compositions and methods there from. Specifically, the applications provides methods and compositions relating to Blue Curls Pirzada essential oil and floral water. 1. A method for obtaining terpinen-4-ol , comprising(a) growing a Blue Curls ‘Pirzada’ plant; and(b) isolating terpinen-4-ol from Blue Curls ‘Pirzada’.2. The method of claim 1 , wherein said terpinen-4-ol is isolated from gland-tipped epidermal trichomes.3. An essential oil isolated from Blue Curls ‘Pirzada claim 1 ,’ wherein said oil comprises at least about 60% terpinen-4-ol.4. A composition comprising the essential oil of .5. The composition of claim 4 , wherein said composition is a pharmaceutical claim 4 , nutraceutical claim 4 , cosmetic claim 4 , lotion claim 4 , toothpaste claim 4 , or fragrance.6. A method for treating a burn in a subject in need thereof comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'applying terpinen-4-ol isolated by the method of on the burn tissue.'}7. A method for treating a microbial tissue infection in a subject in need thereof comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'applying terpinen-4-ol isolated by the method of on the microbal infected tissue.'}8. The method of claim 7 , wherein said tissue is skin.9. (canceled)10. A method of making the pharmaceutical composition of comprising(a) growing a Blue Curls ‘Pirzada’ plant;(b) isolating terpinen-4-ol from Blue Curls ‘Pirzada’; and(c) combining said terpinen-4-ol into with a carrier.11. A method for increasing terpinen-4-ol content in a plant claim 5 , comprising crossing a plant with a Blue Curls ‘Pirzada’ plant claim 5 , wherein Blue Curls ‘Pirzada’ plant is either the pollen or egg donor.12. (canceled)13. A floral water isolated from Blue Curls ‘Pirzada claim 5 ,’ wherein said floral water comprises at least about 60% terpinen-4-ol.14. A composition comprising the floral water of . The present disclosure relates to var. “ ...

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Номер записи: 14
23-01-2014 дата публикации

Small molecule inhibitors of necroptosis

Номер: US20140024657A1
Автор: Emily S. Hsu, Junying Yuan
Принадлежит: Harvard College

The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.

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Номер записи: 15
06-02-2014 дата публикации

COMPOSITION OF MONOTERPENOIDS HAVING BACTERICIDAL PROPERTIES

Номер: US20140039045A1
Автор: Reynolds Max
Принадлежит:

A composition having bactericidal properties comprising; (a) 30%-80% of at least one compound having the formula (I) and (b) 10% to 40% of at least one compound of formula (II) 2. The composition of claim 1 , wherein the at least one compound of formula 1 is selected from the group consisting of ∝-terpineol claim 1 , β-terpineol claim 1 , γ-terpineol terpinene-4-ol claim 1 , thymol claim 1 , carvacrol claim 1 , carveol claim 1 , perillyl alcohol claim 1 , isopulegol claim 1 , limonene-10-ol claim 1 , and dihydrocarveol.3. The composition of claim 1 , wherein the at least one compound of formula 1 is terpinene-4-ol.4. The composition of claim 3 , wherein the composition comprises from 40% to 70% terpinene-4-ol.5. The composition of claim 1 , having at least two compounds of formula 1.6. The composition of claim 5 , wherein there compounds of formula 1 consist essentially of terpinene-4-ol and ∝-terpineol.7. The composition of comprising between about 40 and about 70% terpinene-4-ol and about 4 to about 15% terpinene-4-ol.9. The composition of claim 1 , wherein the composition comprises at between about 10% to about 40% claim 1 , preferably between about 15% to about 35% claim 1 , preferably between about 20% to about 30% of at least one compound of formula 2.10. The composition of claim 9 , wherein the composition comprises at least two compounds of formula 2 claim 9 , and at least one compound has 2 oxygen atoms and at least one compound has three oxygen atoms claim 9 , wherein the ratio of the at least one compound having two oxygen atoms to the at least one compound having three oxygen atoms is between about 1:1 to 5:1 claim 9 , preferably between about 1.5:1 to about 4:1 claim 9 , most preferably between about 2:1 to about 3:1.11. The composition of claim 9 , wherein the at least one compound of formula 2 comprises between about 1 to about 4% claim 9 , preferably between about 2 to about 3% 2-hydroxy-1 claim 9 ,4-cineole; between about 5% to about 15% claim 9 , ...

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Номер записи: 16
20-02-2014 дата публикации

Triterpene-containing oleogel-forming agent, triterpene-containing oleogel and method for producing a triterpene-containing oleogel

Номер: US20140050790A1
Автор: Armin Scheffler
Принадлежит: Birken AG

The invention relates to an oleogel-forming agent which comprises at least one highly dispersed triterpene. The invention also relates to an oleogel which comprises a nonpolar liquid in an amount ranging from 80% by weight to 99% by weight based on the total weight of the oleogel and an oleogel-forming agent comprising a highly dispersed triterpene in an amount ranging from 1% by weight to 20% by weight based on the total weight of the oleogel. The invention also relates to a method for producing an oleogel.

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Номер записи: 17
27-03-2014 дата публикации

Capsicum variety exhibiting a hyper-accumulation of zeaxanthin and products derived therefrom

Номер: US20140086986A1
Автор: Anthony Van Den Hombergh, Carrie Young, Donald Berdahl, Paul H. Todd, Jr.
Принадлежит: Kalamazoo Holdings Inc

The present invention is concerned with Capsicum plants producing greater than about 0.4% zeaxanthin, by weight in the dried, ripe fruit pod flesh, which plants have been developed from commercially grown Capsicum cultivars by plant breeding techniques. Zeaxanthin is the dominant carotenoid in the dried ripe fruit pod flesh, when measured in non-esterified forms. Alternatively, these plants may be characterized as exhibiting a high pigmentation measured as an ASTA value and further characterized by the predominant presence of zeaxanthin. The zeaxanthin derived from these Capsicum plants can be used in applications that include nutritional supplements, foods, functional foods, cosmetics, animal feeds, aquaculture feeds, and pharmaceuticals.

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Номер записи: 18
01-01-2015 дата публикации

Monomer for hardmask composition and hardmask composition including the monomer and method of forming patterns using the hardmask composition

Номер: US20150001178A1
Автор: Chung-Heon Lee, Go-Un Kim, Hea-Jung KIM, Hyun-Ji SONG, Joon-Young Moon, Seung-Hee Hong, Seung-Wook Shin, Yo-Choul PARK, Yong-Woon YOON, Yoo-Jeong Choi, You-Jung PARK, Young-Min Kim, Yu-Shin Park, Yun-Jun KIM
Принадлежит: Cheil Industries Inc

A monomer for a hardmask composition is represented by the following Chemical Formula 1,

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Номер записи: 19
06-01-2022 дата публикации

SUBSTITUTED POLYFLUORENE COMPOUNDS

Номер: US20220002552A1
Автор: Wang Jing, Xu Xinshe
Принадлежит: BioLegend, Inc.

The present invention provides fluorescent polyfluorene polymers or macromers with unique optical properties that are stable. The polymeric fluorophores are useful in various bioassays formats. The inventive polymers are useful in assays relying on fluorescence resonance energy transfer (FRET) mechanisms where two fluorophores are used. 2. The macromer of claim 1 , wherein the macromer has a molecular weight which is a member selected from the group consisting of about 5 kDa claim 1 , about 6 kDa claim 1 , about 7 kDa claim 1 , about 8 kDa claim 1 , about 9 kDa claim 1 , about 10 kDa claim 1 , about 11 kDa claim 1 , about 12 kDa claim 1 , about 13 kDa claim 1 , about 14 kDa claim 1 , about 15 kDa claim 1 , about 16 kDa claim 1 , about 17 kDa claim 1 , about 18 kDa claim 1 , about 19 kDa claim 1 , about 20 kDa claim 1 , about 21 kDa claim 1 , about 22 kDa claim 1 , about 23 kDa claim 1 , about 24 kDa claim 1 , about 25 kDa claim 1 , about about 26 kDa claim 1 , about 27 kDa claim 1 , about 28 kDa claim 1 , about 29 kDa claim 1 , about 30 kDa claim 1 , about 31 kDa claim 1 , about 32 kDa claim 1 , about 33 kDa claim 1 , about 34 kDa claim 1 , about 35 kDa claim 1 , about 36 kDa claim 1 , about 37 kDa claim 1 , about 38 kDa claim 1 , about 39 kDa claim 1 , about 40 kDa claim 1 , about 41 kDa claim 1 , about 42 kDa claim 1 , about 43 kDa claim 1 , about 44 kDa claim 1 , about 45 kDa claim 1 , about 46 kDa claim 1 , about 47 kDa claim 1 , about 48 kDa claim 1 , about 49 kDa claim 1 , about 50 kDa claim 1 , about 51 kDa claim 1 , about 52 kDa claim 1 , about 53 kDa claim 1 , about 54 kDa claim 1 , about 55 kDa claim 1 , about 56 kDa claim 1 , about 57 kDa claim 1 , about 58 kDa claim 1 , about 59 kDa and about 60 kDa.3. The macromer of claim 1 , wherein Eand/or Eis conjugated to an organic dye.4. The macromer of claim 1 , wherein the macromer has an emission wavelength of about 300 nm to about 500 nm.5. The macromer of claim 1 , wherein each of R claim 1 , R claim 1 , R ...

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Номер записи: 20
13-01-2022 дата публикации

METHOD FOR PRODUCING HETEROCYCLIDENE ACETAMIDE DERIVATIVE

Номер: US20220009898A1
Автор: CAI Xiaofei, Chen Chuan, CHEN Yanliang, GE Yonghui, GU Xiaomin, Li Jie, LIN Jinguang, LUO Jian, SATOH Tsutomu, SHA Chunbo, Sun Baoquan, SUN Fenglai, UCHIDA Hideharu, YE Jiajie, ZHAO BIN
Принадлежит: MOCHIDA PHARMACEUTICAL CO., LTD.

The present invention provides, a novel method for producing a compound represented by formula (I) and a novel method for producing a compound represented by formula (B) or a salt thereof, which are intermediates in the production of formula (I). The present invention relates to a new method for producing (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-((7R)-7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide represented by Formula (I) which is a heterocyclidene acetamide derivative. Furthermore, the present invention relates to a new method for producing (R)-8-amino-1,2,3,4-tetrahydronaphthalen-2-ol represented by Formula (B) or a salt thereof, which is an intermediate useful for producing the compound represented by Formula (I).(E)-2-(7-trifluoromethylchroman-4-ylidene)-N-((7R)-7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide represented by Formula (I) is a transient receptor potential vanilloid 1 (TRPV1) antagonist, and is anticipated as a preventive and/or therapeutic agent for diseases involving the TRPV1 receptor (for example, pain (for example, neuropathic pain, diabetic neuralgia, postoperative pain, osteoarthrosis, rheumatoid arthritis pain, inflammatory pain, cancer pain, migraine and the like), nervous disorders, nerve damage, neurodegeneration, chronic obstructive pulmonary disease, asthma, rhinitis, inflammation of mucous membranes such as in the eyes, nervous skin disease, inflammatory skin disease, allergic disease, urinary incontinence, urge incontinence, overactive bladder, cystitis, pruritus, and the like) (Patent Literature 1).WO 2007/010383 (Patent Literature 1) discloses a method for producing the compound represented by Formula (I). In the document, the compound represented by Formula (I) is produced in steps of to shown in the following (scheme A). A compound represented by Formula (IM-k) is obtained by performing a condensation reaction using 8-amino-3,4-dihydronaphthalen-2(1H)-one (Formula (IM-3)) produced ...

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Номер записи: 21
08-01-2015 дата публикации

Partially halogenated, hydroxylated fullerene and allergen adsorbent using the same

Номер: US20150011802A1
Автор: Ken Kokubo, Takeshi Noguchi
Принадлежит: Osaka University NUC, Totai Co Ltd

Provided are a novel fullerene derivative which can adsorb quickly and efficiently an allergen which may cause a pollen allergy without releasing the allergen again, does not contain a metal or the like which may cause a harmful effect to a human body, and is easily applicable, impregnable, or chemically bondable onto surface of various materials: and a process for producing the same. The fullerene derivative is characterized in that a halogen group and many hydroxyl groups are bonded directly to a fullerene nucleus. In the case that the halogen group is chlorine, the fullerene derivative can be synthesized by a partial hydroxylation of a chlorinated fullerene or a partial chlorination of a hydroxylated fullerene.

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Номер записи: 22
21-01-2016 дата публикации

Compound for forming organic film, and organic film composition using the same, process for forming organic film, and patterning process

Номер: US20160018735A1
Автор: Daisuke Kori, Kazumi Noda, Seiichiro Tachibana, Takeru Watanabe, Toshiharu Yano, Tsutomu Ogihara
Принадлежит: Shin Etsu Chemical Co Ltd

The invention provides a compound for forming an organic film having a partial structure represented by the following formula (vii-2), wherein R 1 represents a linear, branched or cyclic monovalent hydrocarbon group having 1 to 20 carbon atoms, and a methylene group constituting R 1 may be substituted by an oxygen atom; a+b is 1, 2 or 3; c and d are each independently 0, 1 or 2; x represents 0 or 1, when x=0, then a=c=0; L 7 represents a linear, branched or cyclic divalent organic group having 1 to 20 carbon atoms, L 8′ represents the partial structure represented by the following formula (i), 0≦o<1, 0<p≦1 and o+p=1, wherein the ring structures Ar3 represent a substituted or unsubstituted benzene ring or naphthalene ring; R 0 represents a hydrogen atom or a linear, branched or cyclic monovalent organic group having 1 to 30 carbon atoms; and L 0 represents a divalent organic group. There can be provided an organic film composition for forming an organic film having high dry etching resistance as well as advanced filling/planarizing characteristics.

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Номер записи: 23
16-01-2020 дата публикации

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

Номер: US20200017433A1
Автор: Dugan Michael, Flynn Autumn, Jui Nathan, Mays Suzanne, Ortlund Eric
Принадлежит: EMORY UNIVERSITY

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein. 2. The compound of claim 1 , wherein Rand Rare hydrogen claim 1 , Ris 1-phenylvinyl or 1-phenylethyl claim 1 , and Ris phenyl.3. The compound of claim 1 , wherein Ris alkyl terminally substituted with a hydroxy claim 1 , carboxy claim 1 , or phosphate claim 1 , wherein the hydroxy claim 1 , carboxy claim 1 , or phosphate are optionally further substituted with R.5. The compound of claim 1 , wherein Ris hydroxyl claim 1 , alkyl claim 1 , amino claim 1 , aminoalkyl claim 1 , carbamoyl claim 1 , sulphate claim 1 , sulfonate claim 1 , aminosulfonyl claim 1 , phosphate claim 1 , phosphonate claim 1 , or heterocyclyl claim 1 , wherein Ris optionally substituted with R.7. The compound of claim 6 , wherein{'sup': '1', 'a) X is O, and Ris alkanoyl;'}{'sup': '1', 'b) X is —NH—, and Ris alkanoyl;'}{'sup': '1', 'c) X is O, and Ris aminosulfonyl;'}{'sup': '1', 'd) X is —NH—, and Ris aminosulfonyl;'}{'sup': '1', 'e) X is —(C═O)—, Ris amino;'}{'sup': '1', 'f) X is O, Y is —(C═O)—, Ris amino;'}{'sup': '1', 'g) X is O, Y is —(C═O)—, Z is —NH—, and Ris sulfonate; and'}{'sup': '1', 'h) X is O, Y is —(C═O)—, Z is —NH—, and Ris aminosulfonyl.'}8. The compound of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl sulfamide or salt thereof.9. The compound of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl)acetamide or salt thereof.10. A pharmaceutical composition ...

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Номер записи: 24
24-01-2019 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20190023709A1
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (I): 2. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is substituted with one hydrogen;C14 is substituted with one hydrogen;C15 is substituted with two hydrogens;{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 4a', '4b', '7', '3, 'sub': 2', '2', '2', '2', '3', '3, 'Ris hydrogen or alkyl, Ris a direct bond to the carbon to which Ris attached, and Ris —CHNHor —CHN(H)C(O)(CH)CH;'}{'sup': '5', 'Ris alkyl;'}{'sup': '6', 'Ris hydrogen;'}{'sup': '7', 'Ris hydrogen;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain; and'}{'sup': '9', 'each Ris independently hydrogen, alkyl, haloalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl.'}3. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is substituted with one hydrogen;C14 is substituted with one hydrogen;C15 is substituted with two hydrogens;{'sup': '1', 'Ris —OH;'}{'sup': '2', 'sub': '2', 'Ris —CH—OH;'}{'sup': 4a', '4b', '7', '3, 'sub': 2', '2', '2', '2', '3', '3, 'Ris hydrogen or methyl, Ris a direct bond to the carbon to which Ris attached, and Ris —CHNHor —CHN(H)C(O)(CH)CH;'}{'sup': '5', 'Ris methyl;'}{'sup': '6', 'Ris hydrogen; and'}{'sup': '7', 'Ris hydrogen.'}4. The compound of selected from:(1S,3S,4R)-4-((3aS,6S,7R,7aS)-7-(aminomethyl)-3,3a-dimethyl-3a,4,5,6,7,7a-hexahydro-1H-inden-6-yl)-3-(hydroxymethyl)-4-methylcyclohexanol; andN-(((3aR,6S,7R,7aS)-6-((1R,2S,4S)-4-hydroxy-2-(hydroxymethyl)-1-methylcyclohexyl)-3a-methyl-3a,4,5,6,7,7a-hexahydro-1H-inden-7-yl)methyl)pentanamide.6. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is ...

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Номер записи: 25
04-02-2016 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20160031899A1
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., MacRury Thomas B., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (II): wherein A, R, R, Rand Rare described herein, or a stereoisomer, enantiomer or tautomer thereof or mixtures thereof, or a pharmaceutically acceptable salt or solvate thereof, are described herein, as well as other compounds. These compounds have activity as SHIP1 modulators, and thus may be useful in treating a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of the invention are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof. 3. The compound of wherein:{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 3', '8', '9', '11', '8', '9', '12', '8', '9', '9a', '8', '9', '9a', '8', '9', '9a, 'sub': 2', '2', '2, 'Ris —R—N(R)C(O)R, —R—N(R)—R, —R—N(R)C(═NCN)N(R), —R—N(R)C(O)N(R)or —R—N(R)C(S)N(R);'}{'sup': 4a', '4b, 'Rand Rare each independently hydrogen, alkyl, alkenyl or alkynyl;'}{'sup': 4a', '4b', '7, 'or Ris hydrogen, alkyl, alkenyl or alkynyl and Ris a direct bond to the carbon to which Ris attached;'}{'sup': 4a', '4b, 'or Rand Rtogether form alkylidene or haloalkylidene;'}{'sup': 5', '5, 'Ris alkyl or Ris a direct bond to the carbon at C14;'}{'sup': 6', '8', '9', '8', '9, 'sub': '2', 'Ris hydrogen, —R—ORor —R—N(R);'}{'sup': 7', '8', '9', '8', '9', '7', '4b', '7, 'sub': '2', 'Ris hydrogen, —R—OR, —R—N(R), or a direct bond to C15, provided that when Ris a direct bond to C15, Ris not a direct bond to the carbon to which Ris attached;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain;'}{'sup': '9', 'each Ris hydrogen, alkyl, optionally substituted aryl and optionally substituted aralkyl;'}{'sup': '9a', 'each Ris hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl;'}optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, ...

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Номер записи: 26
11-02-2016 дата публикации

PROCESS FOR THE PREPARATION OF 4-(8-(2-CHLOROPHENOXY)-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3-YL)BICYCLO[2.2.1]HEPTAN-1-OL AND NOVEL INTERMEDIATES THEREFOR

Номер: US20160039813A1
Автор: Deerberg Joerg, Hickey Matthew R., Qian Xinhua, Yamamoto Kana, Yang Wendy Wangying, Zhu Keming
Принадлежит:

A process is provided for preparing 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates used in the process. The compound is a 11-beta hydroxysteroid dehydrogenase type I inhibitor which exhibits activity in the treatment of various metabolic diseases. 6. The process as defined in where the oxidation is carried out in the presence of sodium chlorite claim 4 , 2 claim 4 ,2 claim 4 ,6 claim 4 ,6-tetramethylpiperidine-N-oxide and sodium hypochlorite.8. The process as defined in wherein the reaction is carried out under an inert atmosphere at a temperature within the range from about 0 to about 5° C.10. The process as defined in wherein the carboxylic acid is benzoic acid and the reaction is carried out at a temperature within the range from about 105 to 110° C. This application claims priority to U.S. Provisional Application Ser. No. 62/033,695, filed Aug. 6, 2014; the entire content of which is incorporated herein reference.The invention generally relates to novel intermediates and an improved process for the preparation of 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol, a 11-beta hydroxysteroid dehydrogenase type I inhibitor which was recently in clinical trials for the treatment of type 2 diabetes, obesity, and the metabolic syndrome.The steroid hormone cortisol is a key regulator of many physiological processes. However, an excess of cortisol, as occurs in Cushing's Disease, provokes severe metabolic abnormalities including: type 2 diabetes, cardiovascular disease, obesity, and osteoporosis. Many patients with these diseases, however, do not show significant increases in plasma cortisol levels. In addition to plasma cortisol, individual tissues can regulate their glucocorticoid tone via the in situ conversion of inactive cortisone to the active hormone cortisol. Indeed, the normally high plasma concentration of cortisone provides a ready supply of precursor for conversion ...

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Номер записи: 27
09-02-2017 дата публикации

SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-METHYLENE ANALOGS OF CALCITRIOL AND RELATED COMPOUNDS

Номер: US20170036977A1
Автор: DeLuca Hector F., Plum Lori A., Sibilska Izabela K., Sicinski Rafal R.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Disclosed are 2-methylene analogs of vitamin Dand related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1α-hydroxy-2-methylene-vitamin D, (20S)-1α-hydroxy-2-methylene-vitamin D, and (5E)-1α,25-dihydroxy-2-methylene-vitamin D, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders. 2. The compound of claim 1 , wherein Xand Xare t-butyldimethylsilyl.3. The compound of claim 1 , wherein Xand Xare hydrogen.6. A pharmaceutical composition containing an effective amount of the compound of and a pharmaceutically acceptable excipient.7. A method of treating or preventing a bone disease or disorder in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .8. A method for increasing bone strength in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .9. A method of treating or preventing a skin disease claim 1 , disorder claim 1 , or condition in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .10. A method of treating or preventing a cell proliferative disease or disorder in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .11. A method of treating or preventing obesity claim 1 , inhibiting adipocyte differentiation claim 1 , inhibiting SCD-1 gene transcription claim 1 , and/or reducing body fat in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .12. A method of treating secondary hyperparathyroidism of renal osteodystrophy in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount ...

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Номер записи: 28
18-02-2021 дата публикации

Modulators of Liver Receptor Homologue 1 (LRH-1) and Uses

Номер: US20210047258A1
Автор: Dugan Michael, Flynn Autumn, Jui Nathan, Mays Suzanne, Ortlund Eric
Принадлежит:

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein. 4. The method of claim 3 , wherein{'sup': '1', 'a) X is O, and Ris alkanoyl;'}{'sup': '1', 'b) X is —NH—, and Ris alkanoyl;'}{'sup': '1', 'c) X is O, and Ris aminosulfonyl;'}{'sup': '1', 'd) X is —NH—, and Ris aminosulfonyl;'}{'sup': '1', 'e) X is —(C═O)—, Ris amino;'}{'sup': '1', 'f) X is O, Y is —(C═O)—, Ris amino;'}{'sup': '1', 'g) X is O, Y is —(C═O)—, Z is —NH—, and Ris sulfonate; and'}{'sup': '1', 'h) X is O, Y is —(C═O)—, Z is —NH—, and Ris aminosulfonyl.'}5. The method of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl sulfamide or salt thereof.6. The method of claim 1 , wherein the compound is 5-hexyl-4-phenyl-3a-(1-phenylvinyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,3a claim 1 ,6 claim 1 ,6a-hexahydropentalen-1-yl)acetamide or salt thereof.7. The method of claim 1 , wherein the cardiovascular disease is cardiovascular disease is selected from coronary artery disease (CAD) claim 1 , angina claim 1 , myocardial infarction claim 1 , stroke claim 1 , hypertensive heart disease claim 1 , rheumatic heart disease claim 1 , cardiomyopathy claim 1 , heart arrhythmia claim 1 , congenital heart disease claim 1 , valvular heart disease claim 1 , carditis claim 1 , aortic aneurysms claim 1 , peripheral artery disease claim 1 , and venous thrombosis.11. The method of claim 10 , wherein{'sup': '1', 'a) X is O, and Ris alkanoyl;'}{'sup': '1', 'b) X is —NH—, and Ris alkanoyl;'}{'sup': '1', 'c) X is O, and Ris aminosulfonyl;'}{'sup': '1', 'd) X is —NH—, ...

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Номер записи: 29
14-02-2019 дата публикации

Process for Preparing a Mixture of Terpene Alcohols

Номер: US20190047928A1
Автор: BENSON Stefan, GOETZ Roland, Kraus Helmut, Rack Michael, WOLF Bernd
Принадлежит:

The present invention relates to a process for preparing a mixture of terpene alcohols comprising limonene-4-ol and terpinene-4-ol from terpinolene epoxide via an isomerization and/or hydrogenation reaction in the presence of a copper catalyst. 116-. (canceled)18. The process of claim 17 , wherein the copper catalyst comprises copper chromite.19. The process of claim 17 , wherein the copper catalyst comprises at least one promoter selected from the group consisting of alkali metals claim 17 , alkaline earth metals claim 17 , manganese claim 17 , bismuth claim 17 , iron and combinations thereof.20. The process of claim 19 , wherein the promoter is selected from the group consisting of sodium claim 19 , potassium claim 19 , magnesium claim 19 , calcium claim 19 , barium claim 19 , manganese claim 19 , iron and combinations thereof.21. The process of claim 17 , wherein the copper catalyst comprises at least one binder or support material selected from the group consisting of aluminum oxide (AlO) claim 17 , silicon dioxide (SiO) claim 17 , titanium dioxide (TiO) claim 17 , zirconium dioxide (ZrO) claim 17 , sodium silicate claim 17 , calcium silicate claim 17 , magnesium silicate claim 17 , graphite claim 17 , clay claim 17 , zeolite claim 17 , molecular sieves claim 17 , and mixtures thereof.22. The process of claim 17 , wherein the carboxylic acid ester is selected from esters of the general formula RCOORwherein Ris hydrogen or a group selected from C-C-alkyl claim 17 , C-C-cycloalkyl claim 17 , C-C-aryl and C-C-aryl-C-C-alkyl and Ris a group selected from C-C-alkyl claim 17 , C-C-cycloalkyl claim 17 , C-C-aryl and C-C-aryl-C-C-alkyl claim 17 , each of the aforementioned groups optionally being substituted with one or more substituents selected from C-C-alkoxy.23. The process of claim 17 , wherein the carboxylic acid ester is selected from C-C-alkyl acetates.24. The process of claim 17 , wherein the carboxylic acid ester is ethyl acetate.25. The process of claim 17 , ...

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Номер записи: 30
28-02-2019 дата публикации

System and method for producing 1,4-cyclohexanedimethanol and 1,4-cyclohexanedicarboxylic acid from terephthalic acid

Номер: US20190062251A1
Автор: Drow Lionel O&#39;Young, Ketan D. SAMANT, Yik Chung Chan
Принадлежит: Clearwaterbay Chdm Technology Ltd

This invention relates to the continuous production of 1,4-cyclohexane dimethanol (CHDM) and optionally and additionally of 1,4-cyclohexane dicarboxylic acid (CHDA) directly using terephthalic acid (TPA) as the raw material. More specifically, this invention relates to a method and system for continuous production of CHDM and CHDA that features direct use of TPA as feedstock, promotes efficient use of solvent and energy, and provides products with the desired high trans isomer content, by exploiting unexpected features of the thermodynamic phase behavior and the reaction mechanisms.

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Номер записи: 31
08-03-2018 дата публикации

ORGANIC COMPOUNDS

Номер: US20180066003A1
Автор: GEISSER Roger Wilhelm, OETIKER Jurg Daniel, Schröder Fridtjof
Принадлежит:

A process for the hydrogenation of a substrate comprising a carbon heteroatom double bond in the presence of a transition metal complex comprising a tridentate or bisdentate-ligand containing a nitrogen, sulphur and phosphorus atom, of which at least the N- and P- and optionally also the S-atom coordinates with the transition metal. 2. A process according to claim 1 , wherein the nitrogen atom on the tridentate or bisdentate ligand forms part of an amine group or an imine group; the sulphur atom forms part of an aliphatic group or forms part of an aromatic ring; and the phosphorus atom forms part of a phosphine group.3. A process according to or wherein the nitrogen atom-containing group is flanked on one side by the phosphorus atom-containing group claim 1 , and on the other side by the sulphur atom-containing group.6. A process according to any of the preceding claims wherein the metal M is ruthenium or osmium.7. A process according to any of the preceding claims wherein the functional group that is hydrogenated is selected from the group consisting of an ester claim 1 , lactone claim 1 , ketone claim 1 , aldehyde claim 1 , amide claim 1 , lactam and imine.8. A process according to any of the preceding claims wherein the substrate bearing a functional group containing a carbon heteroatom double bond is sclareolide and the hydrogenated product is sclareodiol.11. A complex according to wherein the nitrogen atom on the tridentate or bisdentate ligand forms part of an amine group or an imine group; the sulphur atom forms part of an aliphatic group or forms part of an aromatic ring; and the phosphorus atom forms part of a phosphine group.12. A complex according to or claim 10 , wherein the nitrogen atom-containing group is flanked on one side by the phosphorus atom-containing group claim 10 , and on the other side by the sulphur atom-containing group.15. A complex according to any of the through wherein the metal M is ruthenium or osmium. The present invention relates ...

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Номер записи: 32
10-03-2016 дата публикации

REAGENT AND COMPOSITION OF RESIST

Номер: US20160070165A1
Автор: Enomoto Satoshi
Принадлежит:

Described is a reagent that enhances acid generation of a photoacid generator and a composition containing such reagent. 1. A reagent wherein:a feed of an energy to the reagent or to an acceptor for the reagent receiving the energy generates an intermediate from the reagent; and further whereinthe intermediate enhances generation of acid from a precursor, wherein the intermediate is a ketyl radical.25.-. (canceled)6. The reagent of claim 1 , wherein the feed of energy comprises irradiation with light.7. The reagent of claim 1 , wherein the feed of energy is carried out by irradiation of the reagent with at least one of light of which the wavelength is less than or equal to 15 nm and an electron beam.8. A composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the reagent of ; and'}a first compound that functions as a generation source of acid.9. The composition of claim 8 , further comprising:a second compound that has a bond cleavable by acid.11. (canceled)12. The reagent of claim 10 , wherein:the reagent further includes a second cyclic moiety, andthe first cyclic moiety contains at least two atoms that are also contained in the second cyclic moiety.13. The composition reagent of claim 10 , wherein:the third reagent further includes a third cyclic moiety, andthe first cyclic moiety contains at least two atoms that are also contained in the third cyclic moiety.14. The reagent of claim 10 , wherein the first cyclic moiety is either a six-membered ring or a five-membered ring.15. The reagent of claim 10 , wherein the second cyclic moiety is an aromatic group.16. (canceled)17. The composition of claim 8 , wherein the first compound is an organic salt containing an iodonium ion or a sulfonium ion.18. The reagent of claim 1 , wherein the intermediate is generated by abstracting a hydrogen atom from the reagent.19. The reagent of claim 1 , wherein a difference between at least one of a first oxidation potential of a ground state and a second ...

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Номер записи: 33
15-03-2018 дата публикации

Method for the Conversion of Abienol to Sclarediol

Номер: US20180072644A1
Автор: Schröder Fridtjof
Принадлежит:

A method of selective conversion of Abienol, represented by formula 1, to Sclareodiol, represented by formula 2 2. The method of wherein the ozonolysis is carried out at a temperature above −20° C.3. The method of wherein the ozonolysis and/or the reduction takes place in a flow reactor.4. The method of claim 1 , wherein the ozonolysis and/or reduction takes place in a non-halogenated solvent or a mixture of non-halogenated solvents.5. The method of wherein the non-halogenated solvent is an alcoholic solvent comprising one or more —OH moieties.6. The method of wherein the non-halogenated solvent is ethanol.7. The method of wherein the ozonolysis takes place in a solvent claim 1 , and the reduction takes place in the same solvent.8. The method of claim 1 , wherein a borohydride reducing agent is used in the reduction.9. The method of wherein NaBH4 is used as reducing agent in a concentration of 0.5-5 mol equiv.12. The method of claim 11 , wherein the compound of formula 1 is protected on the OH-function and yields the corresponding compound of formula 2 protected on the OH-function.13. The method of claim 12 , wherein the compound of formula 2 protected on the OH-function is directly cyclized to the compound of formula 3.14. The method of claim 12 , wherein the compound of formula 2 protected on the OH-function claim 12 , is deprotected and subsequently cyclized to the compound of formula 3. This invention relates generally to methods of preparing perfumery raw materials and to key intermediates used in, or prepared during such methods. In particular, this invention relates to a novel method for the preparation of (−)-Sclareodiol 2a (R=H) or a Sclareodiol derivative 2 from Z-(+)-Abienol 1a (R=H, R′=—CH═CH) or an Abienol derivative 1. (−)-Sclareodiol 2a is an important intermediate that can be further cyclized to the compound of formula 3, also known as (−)-Ambrox® ((3aR,5aS,9aS,9bR)-3a,6,6,9a-tetra methyldodecahydro-naphtho[2,1-b]furan), an important base note in ...

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Номер записи: 34
15-03-2018 дата публикации

TRANS-CYCLOHEPTENES AND HETERO-TRANS-CYCLOHEPTENES FOR BIOORTHOGONAL COUPLING

Номер: US20180072761A1
Автор: FANG Yinzhi, Fox Joseph, Zhang Han
Принадлежит: University of Delaware

A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR, CH, CHOH, and CHR; Ris phenyl or CH; Ris phenyl, CH, (CH)CN, or (CH)OH, wherein n is an integer from 1 to 5; Rand Rare each individually selected from the group consisting of H, OH, and CH; and Z and L are not both SiRR; or b) Z is BocN, L is CH, Ris H, and Ris H; or c) Z is C=0, L is CH, Ris H, and Ris H. 2. The substituted trans-cycloheptene according to claim 1 , wherein Z claim 1 , L claim 1 , R claim 1 , and Rare according to any one of combinations a) through l):{'sub': '2', 'sup': a', 'b, 'a) Z is CHOH, L is CH, Ris H, and Ris H;'}{'sub': 2', '2, 'sup': a', 'b, 'b) Z is CHCHOH, L is CH, Ris H, and Ris H;'}{'sub': 2', '2, 'sup': a', 'b, 'c) Z is CH, L is CH, and Ris OH, and Ris H;'}{'sub': '2', 'sup': a', 'b, 'd) Z is CH, L, is CHOH, Ris OH, and Ris H;'}{'sub': '2', 'sup': a', 'b, 'e) Z is BocN, L, is CH, Ris H, and Ris H;'}{'sub': '2', 'sup': a', 'b, 'f) Z is C═O, L is CH, Ris H, and Ris H;'}{'sup': 1', '2', 'a', 'b', '1', '2, 'sub': 2', '3', '2', '3', '2', '4, 'g) Z is SiRR, L is CH, Ris H, Ris H, Ris CH, and Ris either (CH)CN or (CH)OH;'}{'sub': 3', '2', '3', '2', '3', '3, 'sup': a', 'b, 'h) Z is SiCH(CH)OH, L is CH, Ris CH, and Ris CH;'}{'sub': 2', '2, 'sup': a', 'b, 'i) Z is SiPh, L is CH, Ris H, and Ris H;'}{'sub': 3', '2', '2, 'sup': a', 'b, 'j) Z is Si(CH), L is CH, Ris OH, and Ris H;'}{'sub': 2', '2, 'sup': a', 'b, 'k) is CH, L is SiPh, Ris H, and Ris H;'}{'sub': 2', '3', '2', '4, 'sup': a', 'b, 'l) Z is CH, L is SiCH(CH)OH, Ris H, and Ris H.'}3. An adduct of the substituted trans-cycloheptene according to with a molecule selected from the group consisting of tetrazines claim 1 , ketenes claim 1 , conjugated dienes claim 1 , and 1 claim 1 ,3-dipoles.4. The adduct according to claim 3 , wherein the molecule is a tetrazine.5. The adduct according to claim 3 , wherein the molecule is a ketene.6. The adduct according to claim ...

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Номер записи: 35
07-03-2019 дата публикации

Process for synthesis of indenes

Номер: US20190071462A1
Автор: Dermot O&#39;Hare, Jean-Charles BUFFET, THOMAS Arnold, Vichitt Mayalarp
Принадлежит: SCG Chemicals PCL

The present invention relates to a new process for the synthesis of 2,3,4,5,6,7-substituted indenes, which are useful precursors for the formation of certain ansa-metallocene catalysts.

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Номер записи: 36
07-03-2019 дата публикации

LOW GLYCEMIC SUGAR COMPOSITION

Номер: US20190071703A1
Автор: THOMPSON Daryl
Принадлежит:

A composition includes a sugar source and inositol. The sugar source is one more sugars select from the group consisting of glucose, sucrose, sucrolose, tagatose, galactose, high fructose corn syrup, fructose, isoglucose, and rhamnose. The composition of sugar and inositol has an unique properties that prevents or limits the signaling of TNF-α and associated pro-inflammatory cytokines when metabolized by an individual consuming the composition. Accordingly, the composition can be advantageously used to control blood glucose levels, treat diabetes and related conditions as well as treat diseases based on an inflammatory response. 1. A composition consisting of a sugar and inositol.2. The composition of claim 1 , wherein the sugar is sucrose.3. The composition of claim 1 , wherein the sugar is a sugar select from the group consisting of glucose claim 1 , sucrose claim 1 , sucrolose claim 1 , tagatose claim 1 , galactose claim 1 , high fructose corn syrup claim 1 , fructose claim 1 , isoglucose claim 1 , and rhamnose.4. The composition of claim 3 , wherein the sugar is present in around 70% and the inositol is present in approximately 30%.5. The composition of claim 3 , wherein the sugar is present in around 50%.6. A composition consisting essentially of a sugar and inositol with anti-TNF-α effects when administered to a patient in need of treatment therefrom.7. The composition of claim 6 , wherein the sugar is sucrose.8. The composition of claim 6 , wherein the sugar is one more sugars select from the group consisting of glucose claim 6 , sucrose claim 6 , sucrolose claim 6 , tagatose claim 6 , galactose claim 6 , high fructose corn syrup claim 6 , fructose claim 6 , isoglucose claim 6 , and rhamnose.9. The composition of claim 6 , wherein the sugar is present in around 70% and the inositol is present in approximately 30%.10. The composition of claim 6 , wherein the sugar is present in around 50%.1113-. (canceled)14. A method of treating or limiting the occurrence of ...

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Номер записи: 37
26-03-2015 дата публикации

KILLING OF BED BUGS

Номер: US20150087855A1
Автор: BEDOUKIAN Robert H.
Принадлежит: BEDOUKIAN RESEARCH,INC.

Killing of bed bugs is accomplished by bringing the bed bugs into contact with a toxic amount of at least one of the compounds of the structure (I) 3. The method according to wherein the bed bugs are brought into contact with at least two compounds of structure (I).4. The method according to wherein at least one compound of structure (I) is applied to surface of or impregnated into clothing or fabric.5. The method according to wherein at least one compound of structure (I) is applied to detergents claim 1 , fabric softeners or dryer sheets.6. The method according to wherein at least one compound of structure (I) is applied as a topical toxicant formulation in the form of a lotion claim 1 , wipe claim 1 , powder claim 1 , spray or shampoo.7. The method according to wherein at least one compound of structure (I) is applied to furniture claim 1 , building supplies claim 1 , electronic devices claim 1 , cargo or storage areas.7. The method according to wherein at least one compound of structure (I) is selected from the group consisting of 3-methyl-5-propyl-2-cyclohexen-1-one claim 1 , 3-methyl-5-propyl-2-cyclohexen-1-ol and 3-methyl-5-ethyl-2-cyclohexen-1-one for vapor toxicity.8. The method according to wherein at least one compound of structure (I) is selected from the group 3-methyl-5-butyl-2-cyclohexen-1-one claim 1 , 3-methyl-5-pentyl-2-cyclohexen-1-one claim 1 , 3-methyl-5-hexyl-2-cyclohexenone and 3-methyl-5-heptyl-2-cyclohexen-1-one for contact toxicity. This invention relates to compounds used as insecticidal agents to kill bed bugs.Recent data suggests bedbug infestations (Cimex species) of human domiciles are on the rise. At least 92 species of bed bugs have been identified globally, of which at least 16 species are in the North American continent. Generally, bed bugs are parasitic pests with its hosts including humans and various domesticated animals. It is believed that bedbug infestations are becoming more problematic now at least in part because long ...

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Номер записи: 38
26-03-2015 дата публикации

MELANIN PRODUCTION INHIBITOR

Номер: US20150087856A1
Автор: Narukami Toshiaki, Tamai Eiko
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present invention provides a melanin production inhibitor containing a compound having a (2-isopropyl-5-methyl)cyclohexyl group or a (2-isopropenyl-5-methyl)cyclohexyl group. 1. A melanin production inhibitor comprising a compound having a (2-isopropyl-5-methyl)cyclohexyl group or a (2-isopropenyl-5-methyl)cyclohexyl group.3. The melanin production inhibitor according to claim 1 , whereinthe compound having a (2-isopropyl-5-methyl)cyclohexyl group or a (2-isopropenyl-5-methyl)cyclohexyl group is at least one compound selected from5-methyl-(2-isopropenyl)cyclohexanol,3-(2-isopropyl-5-methylcyclohexyloxy)propane-1,2-diol,3-(2-isopropyl-5-methylcyclohexyloxy)propan-1-ol,2-isopropyl-5-methylcyclohexyl 3-hydroxybutyrate,2-(2-(2-isopropyl-5-methylcyclohexyloxy)ethoxy)ethanol,1-(2-isopropyl-5-methylcyclohexyloxy)propan-2-ol, and2-isopropyl-5-methylcyclohexyl 3-oxobutyrate.4. A fragrance composition comprising the melanin production inhibitor according to .5. A skin-whitening agent comprising the melanin production inhibitor according to .6. A cosmetic comprising the melanin production inhibitor according to .7. A skin external agent comprising the melanin production inhibitor according to . The present invention relates to a melanin production inhibitor for inhibiting darkening of the skin due to ultraviolet rays or the like, and a skin-whitening cosmetic which is excellent in skin-whitening effect and is highly safe.When exposed to ultraviolet rays contained in sunlight, ultraviolet lamp, or the like, the skin loses the glow, fine texture, moisture, and the like. Especially when the dermis is damaged by ultraviolet rays, wrinkles and sagging are caused, which cause the so-called photoaging.Active oxygen generated by exposure to ultraviolet rays and various factors released from cells of the skin because of the influence of the active oxygen enhance tyrosinase activity in melanocytes. Melanin, which has a relation to the color tone of the skin, is produced by oxidation ...

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Номер записи: 39
19-06-2014 дата публикации

Phenylcyclohexanol Derivatives As Wax Modifiers And Gelators

Номер: US20140165873A1
Автор: CHOPRA Naveen, Sacripante Guerino G., Wosnick Jordan H.
Принадлежит: XEROX CORPORATION

A compound of the formula 3. (canceled)4. (canceled)5. (canceled)11. The composition of claim 10 , wherein the carrier comprises a member of the group consisting of wax claim 10 , oil claim 10 , solvent claim 10 , water claim 10 , organic liquid claim 10 , inorganic liquid claim 10 , and combinations thereof.12. (canceled)13. (canceled)15. The phase change ink of claim 14 , wherein the carrier comprises at least one wax.16. The phase change ink of claim 14 , wherein the carrier comprises at least one wax having a melting point of 120° C. or higher.17. (canceled)18. (canceled)20. (canceled) In general, phase change inks (sometimes referred to as solid inks or “hot melt inks”) are in the solid phase at ambient temperature, but exist in the liquid phase at the elevated operating temperature of an ink jet printing device. At the jet operating temperature, droplets of liquid ink are ejected from the printing device and, when the ink droplets contact the surface of the recording substrate, either directly or via an intermediate heated transfer belt or drum, they quickly solidify to form a predetermined pattern of solidified ink drops. Phase change inks have also been used in other printing technologies, such as gravure printing.Phase change inks for color printing typically comprise a phase change ink carrier composition which is combined with a phase change ink compatible colorant. In a specific embodiment, a series of colored phase change inks can be formed by combining ink carrier compositions with compatible subtractive primary colorants. The subtractive primary colored phase change inks can comprise four component dyes, namely, cyan, magenta, yellow and black, although the inks are not limited to these four colors. These subtractive primary colored inks can be formed by using a single dye or a mixture of dyes. For example, magenta can be obtained by using a mixture of Solvent Red Dyes or a composite black can be obtained by mixing several dyes. U.S. Pat. No. 4,889, ...

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Номер записи: 40
19-06-2014 дата публикации

C-9 OXYGEN FUNCTIONALIZED LABDANE DERIVATES

Номер: US20140171498A1
Автор: Joshi Swati, Kulkarni Roshan Rajan, Sarkar Dhiman, Sarkar Sampa, Shurpali Ketaki Dilip
Принадлежит: Council of Scientific & Indusrtial Reasearch

This invention relates to diterpenes of general formula (1) belonging to labdane class, isolated from being useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further discloses process for isolation of the fractions containing the same. 18-. (canceled)11Leucas Stelligara.. Compound of formula 1 as claimed in claim 9 , wherein said compound is isolated from12. Compounds of general formula 1 are useful for prevention claim 9 , treatment claim 9 , inhibition or controlling growth and proliferation of tubercular activity in mammals.13Mycobacterium tuberculosis.. Compounds of general formula 1 as claimed in claim 9 , wherein IC50 value is in the range of 5.02 to 9.8 μg/ml against14Mycobacterium tuberculosis.. Compounds of general formula 1 as claimed in claim 9 , wherein IC90 value is in the range of 10.7 to 46.52 μg/ml against15. A process for the extraction of compounds of general formula 1 as claimed in claim 9 , wherein the said process comprising the step of;{'i': 'L. stelligera', 'i. Powdering aerial parts of followed by extraction with acetone at room temperature in the range of 25 to 30° C., filtering acetone solubles and concentrating under reduced pressure in the range of 50-100 mm Hg to obtain a greenish acetone extract,'}ii. separating the extract of step i) by using column chromatography (CC) with gradient increasing polarity of the 10-50% acetone in petroleum ether to obtain 11 fractions (LS-1 to LS-11),iii. subjecting fraction LS7 of step ii) to CC with gradient of acetonitrile from 1% to 3% in chloroform to give 18 sub-fractions (LS7a-r),iv. subjecting sub-fraction LS7i of step iii) to CC in 15% acetone in petroleum ether to give compound 1 and 4,v. subjecting fraction LS4 of step ii) to CC in 6% acetonitrile in chloroform to give 10 (L4a-j) sub-fractions,vi. subjecting fraction L5 of step ii) to CC in 6% acetonitrile in chloroform to give 13(L5a-m) sub-fractions,vii. ...

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Номер записи: 41
19-06-2014 дата публикации

PIMARANE DITERPENES FROM ANISOCHILUS VERTICILLATUS

Номер: US20140171662A1
Автор: Joshi Swati Pramod, Kulkarni Roshan Rajan
Принадлежит: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH

This invention discloses diterpenes class of novel compounds of general formula I from a novel source. More particularly the invention relates to extracts/fractions containing pimarane diterpenes from (Lamiaceae), useful for prevention, treatment, inhibition or controlling growth and proliferation of mycobacterial activity in mammals. The invention further relates to extracts, fractions standardized to diterpenes class of novel compounds useful for the treatment of cancers. 3Anisochilus verticillatus.. The compounds as claimed in claim 1 , wherein said compound is isolated from4. The compound as claimed in are useful for prevention claim 1 , treatment claim 1 , inhibition or controlling growth and proliferation of cancer/tubercular activity in mammals.5. The compounds as claimed in are useful for treating or controlling proliferation of tuberculosis in a mammal.6. The compounds as claimed in claim 1 , wherein % inhibition on Thp-1 cell line of compound 3 is 57.23 at 100 μg/ml.7M. tuberculosis. The compounds of general formula I as claimed in claim 1 , wherein ICvalue of compounds of general formula I against is in the range of 12.5 to 42.92 μg/ml.8. A process for the extraction of compounds of general formula I as claimed in claim 1 , wherein the process comprises the steps of:{'i': 'A. verticillatus', 'i). pulverizing aerial parts of followed by extraction with acetone at room temperature in the range of 25 to 30° C., filtering acetone solubles and concentrating under reduced pressure in the range of 50-100 mm Hg to obtain a greenish acetone extract,'}ii) separating the extract as obtained in step i) by using column chromatography (CC) with increasing polarity of the polar solvent with gradient of acetone from 5% to 50% in pet ether to obtain 18 fractions (AV1-AV18).iii) subjecting fraction AV3 of step ii) to CC with gradient of acetonitrile from 0.5% to 3% in chloroform to collect 8 fractions (AV3a-h),iv) subjecting fraction AV4 of step ii) CC using gradient of ...

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Номер записи: 42
19-03-2020 дата публикации

Methods of making stable and thermally polymerizable vinyl, amino or oligomeric phenoxy benzocyclobutene monomers with improvied curing kinetics

Номер: US20200087429A1
Автор: Colin Hayes, Michael K. Gallagher, Michelle Riener
Принадлежит: Rohm and Haas Electronic Materials LLC

The present invention provides methods of making low energy polymerizable monomers and resins for use in making dielectric materials. The methods comprise deprotecting or deacylating an organic alkali cleavable protecting group containing addition polymerizable, amine containing aromatic monomer or oligoaromatic phenol resin containing an organic alkali cleavable protecting group, such as a C2 to C9 alkanoyl group, preferably, an acyl group, by hydrolyzing to remove the protecting group in organic alkali in a polar solvent containing an excess of alkali C1 to C7 alkoxide and form a hydroxyl functional monomer or resin, followed by; reacting via nucleophilic substitution the resulting hydroxyl functional monomer or resin with an alpha-halide (a-halide) or strong acid conjugate leaving group containing arylcyclobutene compound in a polar solvent, to yield a product an arylcyclobutene-containing addition polymerizable or amine containing aromatic monomer or oligoaromatic phenol resin having an ether linkage from the cyclobutene ring to an aromatic group of the addition polymerizable aromatic monomer, aromatic amine or oligoaromatic phenol.

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Номер записи: 43
12-05-2022 дата публикации

Arthropod controlling composition

Номер: US20220142157A1
Автор: Charles Chappuis, Monica Bandera, Vincent HARRACA
Принадлежит: FIRMENICH SA

Described herein are an arthropod controlling composition including a compound according to a formula (I), methods, and uses to control arthropods as well as arthropod controlling articles including the same.

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Номер записи: 44
30-03-2017 дата публикации

Polymer compound and light emitting device using the same

Номер: US20170092864A1
Автор: Mio SHIRATORI, Tomoyasu Yoshida
Принадлежит: Sumitomo Chemical Co Ltd

A polymer compound comprising a constitutional unit having a group represented by the formula (1): wherein Ring A 1A and Ring R 2A represent an aromatic hydrocarbon ring or a heterocyclic ring and these rings each optionally have a substituent, nA represents an integer of 0 to 5, nB represents an integer of 1 to 5, L A and L B represent an alkylene group, a cycloalkylene group, an arylene group, a divalent heterocyclic ring group, a group represented by —NR′—, an oxygen atom or a sulfur atom, and R′ represents a hydrogen atom, an alkyl group or the like, and Q 1 represents a crosslinkable group.

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Номер записи: 45
30-03-2017 дата публикации

FULLERENE DERIVATIVES

Номер: US20170092866A1
Автор: BERNY Stephane, Blouin Nicolas, JACKSON Edward A., Richter Henning
Принадлежит:

The invention relates to fullerene derivatives of formula I, to mixtures and formulations containing them, to the use of the fullerene derivatives, mixtures and formulations as organic semiconductors in, or for the preparation of electronic devices, especially organic photovoltaic (OPV) devices and organic photodetectors (OPD), and to electronic devices comprising, or being prepared from, these fullerene derivatives, mixtures or formulations. 2. The compound of claim 1 , wherein n is 60 or 70.3. The compound of or claim 1 , wherein Cis a carbon based fullerene or an endohedral fullerene.4. The compound of claim 3 , wherein Cis selected from (C)[5 claim 3 ,6]fullerene claim 3 , (C)[5 claim 3 ,6]fullerene claim 3 , (C)[5 claim 3 ,6]fullerene claim 3 , (C)[5 claim 3 ,6]fullerene claim 3 , (C)[5 claim 3 ,6]fullerene claim 3 , La@C claim 3 , La@C claim 3 , Y@C claim 3 , ScN@C claim 3 , YN@C claim 3 , ScC@Cor a mixture of two or more of the aforementioned fullerenes.5. The compound according to any of to claim 3 , wherein m is 0 and o is 1.6. The compound according to any of to claim 3 , wherein the fullerene Cis substituted at a [6 claim 3 ,6] and/or [5 claim 3 ,6] bond.7. The compound according to any of to claim 3 , wherein Aris a benzene claim 3 , thiophene or naphthalene group that is optionally substituted with one or more groups R.9. The compound according to any of to claim 3 , wherein Rand Rare H.10. The compound according to any of to claim 3 , wherein one of Rand Ris H and the other is different from H.11. The compound according to any of to claim 3 , wherein R claim 3 , Rand Rare H and Ris selected from formulae P-RS-1 to P-RS-7 as defined in claim 3 , preferably from formula P-RS-1 or P-RS-7 wherein preferably k is 0.12. The compound according to claim 11 , wherein n is 60.13. The compound according to any of to claim 11 , wherein Rand Rare H.14. Use of a compound of any of to as electron acceptor or n-type semiconductor in a semiconducting material claim 11 ...

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Номер записи: 46
21-04-2016 дата публикации

Treatment or prevention of neurodegenerative disorders using menthol, linalool and/or icilin

Номер: US20160108004A1
Автор: Henry Markram, Johannes Le Coutre, Maurizio PEZZOLI, Stephanie MICHLIG=GONZALEZ, Susana CAMACHO
Принадлежит: Nestec SA

Compositions for treatment or prevention of neurodegenerative disorders are provided, and the compositions contain a therapeutically effective amount of a compound selected from the group consisting of Menthol, Linalool, Icilin and combinations thereof. Methods for treatment or prevention of neurodegenerative disorders are also provided, and the methods include administering such compositions.

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Номер записи: 47
21-04-2016 дата публикации

TREATMENT OR PREVENTION OF DEPRESSION USING MENTHOL AND/OR ICILIN

Номер: US20160108005A1
Автор: Camacho Susana, Le Coutre Johannes, Markram Henry, MICHLIG-GONZALEZ Stephanie, Pezzoli Maurizio
Принадлежит:

Compositions for treatment or prevention of depression are provided, and the compositions contain a therapeutically effective amount of a compound selected from the group consisting of Menthol, Icilin and combinations thereof. Methods for treatment or prevention of depression are also provided, and the methods include administering such compositions. 1. A method for treating depression comprising administering to an individual having depression a therapeutically effective amount of a compound selected from the group consisting of Menthol , Icilin and combinations thereof.2. The method of wherein the depression is selected from the group consisting of unipolar depression claim 1 , bipolar depression claim 1 , acute depression claim 1 , chronic depression claim 1 , sub-chronic depression claim 1 , dysthymia claim 1 , postpartum depression claim 1 , climacteric depressive symptoms claim 1 , seasonal affective disorders claim 1 , and combinations thereof.3. The method of wherein the composition is administered periodically for at least one year.4. The method of wherein the composition is administered daily.5. The method of wherein the composition is selected from the group consisting of a medicament claim 1 , a food product claim 1 , and a supplement to a food product.6. A method for preventing depression comprising administering to an individual at risk of same a therapeutically effective amount of a compound selected from the group consisting of Menthol claim 1 , Icilin and combinations thereof.7. The method of wherein the depression is selected from the group consisting of unipolar depression claim 6 , bipolar depression claim 6 , acute depression claim 6 , chronic depression claim 6 , sub-chronic depression claim 6 , dysthymia claim 6 , postpartum depression claim 6 , climacteric depressive symptoms claim 6 , seasonal affective disorders claim 6 , and combinations thereof.8. The method of wherein the composition is administered periodically for at least one year.9. ...

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Номер записи: 48
30-04-2015 дата публикации

Use of dicyclohexylmethanol derivatives having antimicrobial properties

Номер: US20150118172A1
Автор: Tatjana Best, Thomas Rudolph
Принадлежит: Merck Patent GmBH

The present invention relates to the use of at least one dicyclohexylmethanol derivative of the formula (I) as antimicrobial active compound or as anti-acne, antidandruff, deodorant or antiperspirant active compound, to preparations comprising these compounds, and to specific dicyclohexylmethanol derivatives and to a process for the preparation thereof.

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Номер записи: 49
26-04-2018 дата публикации

A metal complex catalyst, preparation method thereof, and use thereof in preparing d,l-menthol

Номер: US20180111113A1
Автор: Haidong Yu, Jintao YUAN, Ming Yu, Weikang SHAO, Yuhong Zhang
Принадлежит: Shandong Nhu Pharmaceutical Co ltd, Zhejiang NHU Co Ltd, Zhejiang University ZJU

The present invention discloses a metal complex catalyst, its preparing method and its application in preparing D,L-menthol, the metal complex catalyst includes weight percent elements as follows: 70-85% of Ni, 8-10% of Al, 5-10% of V, and 2-10% of Co. When this metal complex catalyst is applied in preparing D,L-menthol through thymol hydrogenation, it has the characteristics of high reaction activity and quick racemization of chiral compound. Meanwhile, a certain kind of alkali added in isomerization is the key to reducing light constituent byproduct. The whole process comes in good reaction selectivity, simple preparing technology, low production cost, and environment-friendly synthetic route.

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Номер записи: 50
07-05-2015 дата публикации

ANTIMICROBIAL AGENTS

Номер: US20150125402A1
Автор: BEDOUKIAN Robert H.
Принадлежит:

Compounds are used in compositions as antimicrobial agents against microbes, such as for example, , and . Antimicrobial action is obtained by contact of a microorganism with at least one of the compounds of the structure (I); wherein R is a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero or one double bond and a total of from 1 to 11 carbon atoms; Ris —OH, =0 or —OC(0)CHand wherein the compounds of structure (I) contain a total of from 9 to 18 carbon atoms in the compounds. 2Staphylococcus aureus, Staphylococcus epidermidis, Escherichia coli, Pseudomonas aeruginosa, Candida albicansAspergillus brasiliensis.. The method according to wherein the microorganism is selected from the group consisting of claim 1 , and4. The method according to wherein at least one compound of structure (I) is utilized in a formulation selected from the group consisting of liquid cleansers claim 1 , spray cleansers claim 1 , wipes claim 1 , soaps claim 1 , deodorants claim 1 , antiperspirants claim 1 , body sprays claim 1 , mouth drops claim 1 , chewing gums claim 1 , toothpastes claim 1 , mouthwashes claim 1 , mouth sprays and candies.5. The method of wherein the compound of structure (I) is selected from the group consisting of: 3-methyl-5-propyl-2-cyclohexenone claim 1 , 3-methyl-5-butyl-2-cyclohexenone claim 1 , 3-methyl-5-butyl-2-cyclohexenol and 3-methyl-5-heptyl-2-cyclohexenone.6. The method of wherein the at least one compound of structure (I) is contained in a formulation in an amount of from about 10 ppm to about 500 ppm.9. The composition according to wherein the composition is a formulation selected from the group consisting of liquid cleansers claim 7 , spray cleansers claim 7 , wipes claim 7 , soaps claim 7 , deodorants claim 7 , antiperspirants claim 7 , body sprays claim 7 , and oral care products such as claim 7 , mouth drops claim 7 , chewing gums claim 7 , toothpastes claim 7 , mouthwashes claim 7 , mouth sprays and candies.10. The ...

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Номер записи: 51
03-05-2018 дата публикации

AMINE SALTS OF A PROSTACYCLIN ANALOG

Номер: US20180118656A1
Автор: Chambournier Gilles, Endres Gregory William, Fedij Victor, Hering Kirk William, Mahmoud Hussein Mahmoud
Принадлежит: CAYMAN CHEMICAL COMPANY INCORPORATED

The present invention provides amine salts of the prostacyclin analogue of Formula I 3. The method of claim 1 , wherein the organic solvent of step viii) comprises a halogenated organic solvent.4. The method of claim 3 , wherein the halogenated organic solvent comprises dichloromethane claim 3 , chloroform claim 3 , or any combination thereof.6. The method of claim 5 , wherein the base of step ii) comprises an alkyllithium reagent.7. The method of claim 6 , wherein the alkyllithium reagent is sec-butyllithium.8. The method of claim 5 , wherein the organic solvent of step ii) comprises pentane claim 5 , hexane claim 5 , cyclohexane claim 5 , heptane claim 5 , tetrahydrofuran claim 5 , 1 claim 5 ,4-dioxane claim 5 , diethyl ether claim 5 , petro ether claim 5 , methyl-tert-butylether claim 5 , or any combination thereof.9. The method of claim 8 , wherein the organic solvent of step ii) comprises methyl-tert-butylether.11. The method of claim 10 , wherein the reducing agent of step x) comprises a chiral borane compound.12. The method of claim 11 , wherein the chiral borane compound is selected from (R)-1-methyl-3 claim 11 ,3-diphenylhexahydropyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxazaborole claim 11 , (R)-3 claim 11 ,3-diphenylhexahydropyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxazaborole claim 11 , (R)-1-butyl-3 claim 11 ,3-diphenylhexahydropyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxazaborole claim 11 , (R)-tetrahydro-1 claim 11 ,3 claim 11 ,3-triphenyl-1H claim 11 ,3H-pyrrolo[1 claim 11 ,2-c][1 claim 11 ,3 claim 11 ,2]oxaborole claim 11 , (4S)-2-methyl-4 claim 11 ,5 claim 11 ,5-triphenyl-1 claim 11 ,3 claim 11 ,2-oxazaborolidine claim 11 , or any combination thereof.13. The method of claim 10 , wherein the organic solvent of step x) further comprises toluene.16. The method of claim 15 , wherein the oxidizing agent comprises MnOor Dess-Martin periodinane.17. The method of claim 16 , wherein the base of step ii) comprises an alkyllithium ...

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Номер записи: 52
07-05-2015 дата публикации

CYCLIC COMPOUND CONTAINING FUNCTIONAL GROUP OR CONTAINING NO FUNCTIONAL GROUP, AND METHOD FOR PRODUCING SAME

Номер: US20150126779A1
Автор: ISHII Yuuki, Itami Kenichiro, Matsuura Sanae, NAKANISHI Yusuke, Omachi Haruka, Segawa Yasutomo
Принадлежит:

This invention selectively synthesizes a cycloparaphenylene compound having 10, 11, or 13 benzene rings. The invention also synthesizes a cycloparaphenylene compound in which a functional group is introduced into a desired portion. By reacting specific raw materials using a specific reaction, a cyclic compound having 10, 11, or 13 bivalent aromatic hydrocarbon groups, bivalent heterocyclic groups, or derivative groups thereof can be selectively obtained as a pure substance. Further, by a method comprising the step of reacting a specific organic compound containing no functional group with a specific organic compound containing a functional group, it is possible to obtain a cyclic compound containing a functional group in which one or more bivalent aromatic hydrocarbon groups, bivalent heterocyclic groups, or derivative groups thereof of a compound having 10 or more bivalent aromatic hydrocarbon groups, bivalent heterocyclic groups, or derivative groups thereof is substituted with a substituted 1,4-phenylene group. 2. The cyclic compound containing a functional group according to claim 1 , wherein the cyclic compound has 1 group represented by General Formula (2) claim 1 , and 9 or more bivalent aromatic hydrocarbon groups claim 1 , bivalent heterocyclic groups claim 1 , or derivative groups thereof.3. The cyclic compound containing a functional group according to claim 1 , wherein R is a halogen atom.6. The method according to claim 5 , wherein the compound containing no functional group is a compound represented by General Formula (VII-1):{'br': None, 'sup': '2', 'Y—R—Y'}{'sup': '2', 'claim-text': {'br': None, 'sup': '3', 'Y—R—Y'}, 'wherein Ris a bivalent group containing 1 to 3 structural units represented by General Formula (1) and 2 or more bivalent aromatic hydrocarbon groups, bivalent heterocyclic groups, or derivative groups thereof; and Y is as defined above, and the compound containing a functional group is a compound represented by General Formula (VII-2 ...

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Номер записи: 53
14-05-2015 дата публикации

Multicomponent crystals comprising dasatinib and selected co-crystal formers

Номер: US20150133463A1
Автор: Andreas Hafner, Beate Salvador, Bernd Siebenhaar, Fritz Blatter, Marcus Vossen, Martin Szelagiewicz, Tiziana CHIODO, Tobias Hintermann
Принадлежит: BASF SE

Provided are a multicomponent crystalline system (co-crystal), use thereof, as well as a process for obtaining the same. The said multicomponent crystalline system (co-crystal) comprises Dasatinib and a second compound selected from methyM-hydrobenzoate, nicotinamide, ethyl gallate, methyl gallate, propyl gallate, ethyl maltol, vanillin, menthol, or (1R,2S,5R)-(−)-menthol.

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Номер записи: 54
21-05-2015 дата публикации

COMPOUNDS FOR USE IN THE TREATMENT OF AUTOIMMUNE INFLAMMATORY DISEASE

Номер: US20150141523A1
Автор: Frankish Neil, Sheridan Helen
Принадлежит:

A compound of the absolute stereochemical formula 2. The pharmaceutical composition comprising an effective amount of a compound as claimed in and a pharmaceutically acceptable carrier.3. The compound claim 1 , as claimed in for use as a medicament in the prophylaxis or treatment of an autoimmune disease which involves T-cell proliferation or function comprising administering to a subject an effective amount claim 1 , of a compound as claimed in claim 1 ,4. The compound as claimed in for use as a medicament intended for prophylaxis or treatment of inflammatory bowel disease.5. The compound as claimed in for use as a medicament intended for prophylaxis or treatment of ulcerative colitis.6. The compound as claimed in for use as a medicament intended for prophylaxis or treatment of Crohn's disease claim 1 ,7. The method for the prophylaxis or treatment of inflammatory bowel disease claim 1 , comprising administering to a subject sin effective amount of a compound as claimed in .8. The method for the prophylaxis or treatment of ulcerative colitis claim 1 , comprising administering to a subject an effective amount of a compound as claimed in .9. The method for the prophylaxis or treatment of Crohn's disease claim 1 , comprising administering to a subject an effective amount of a compound as claimed in . In WO97/20802A we describe a series of dimeric indane molecules with four different chemical scaffolds. Within this group of molecules we elaborated 2, 2 coupled dimers. The synthesis and biological activity for several 2-alkylated derivatives of this scaffold are presented as is their biological activity. The chemical scaffolds of the indane dimers disclosed in WO97/20802A are quite diverse. Amongst the many compounds disclosed two specific diastereoisomeric molecules [(R,S and S,R)2-Benzyl-2,3-dihydro-1H, 1′H-2,2′-biinden-1-ol and (S,S and R,R)2-Benzyl-2,3-dihydro-1H, 1′H-2,2′-biinden-1-ol] are referred to. Biological data for these diastereoisomers led to the ...

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Номер записи: 55
21-05-2015 дата публикации

TRITERPENOID SAPOGENIN PRODUCTION IN PLANT AND MICROBIAL CULTURES

Номер: US20150141633A1
Автор: Almagro Romero Lorena, Goossens Alain, Moses Tessa, Pollier Jacob
Принадлежит:

The disclosure relates to a method for enhancing the biosynthesis and/or secretion of sapogenins in the culture medium of plant and microbial cell cultures. Further, the disclosure also relates to the identification of novel genes involved in the biosynthesis of sapogenin intermediates, as well as to novel sapogenin compounds. 1. A method for producing triterpenoid sapogenins in the extracellular medium of a eukaryotic cell culture , the method comprising:a. providing eukaryotic cells that synthesize triterpenoid sapogenins under suitable conditions; andb. incubating the cells in culture medium comprising cyclodextrins under the suitable conditions so as to produce the sapogenins in the culture medium.2. The method of claim 1 , wherein the eukaryotic cells are genetically cells engineered to produce triterpenoid sapogenins.3. The method of claim 2 , wherein the eukaryotic cells are selected from the group comprising microbial cells claim 2 , plant cells claim 2 , and algal cells.4Medicago, Panax, Bupleurum, Maesa, Saponaria, Betula, Quillaja, Aesculus, Chenopodium, Hedera, Acacia Centella, Oleander, Avena, ArabidopsisNicotiana.. The method of claim 3 , wherein said cell is a plant cell derived from a plant of the genus selected from the group comprising claim 3 , and5SaccharomycesSchizosaccharomycesPichiaYarrowiaHansenulaCandida. The method of claim 3 , wherein said cell is a yeast cell claim 3 , a cell claim 3 , a cell claim 3 , a cell claim 3 , a cell claim 3 , a cell claim 3 , or a cell.6. The method of claim 5 , wherein said yeast cell is a genetically engineered yeast cell.7. The method of claim 6 , wherein said genetically engineered yeast cell is deficient in expression and/or activity of an enzyme involved in endogenous sterol synthesis.8Dunaliella, ChlorellaChlamydomonas.. The method of claim 3 , wherein said cell is an algae cell derived from algae of the genus selected from the group comprising claim 3 , and9. The method of claim 1 , wherein the ...

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Номер записи: 56
18-05-2017 дата публикации

OPSIN-BINDING LIGANDS, COMPOSITIONS AND METHODS OF USE

Номер: US20170137398A1
Автор: Berman Judd, Cote Jamie B., Frye Leah L., Garvey David S., Greenwood Jeremy R., Larosa Gregory J., Quach Tan
Принадлежит: BIKAM PHARMACEUTICALS, INC.

Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed. 24.-. (canceled)5. The compound of claim 1 , wherein each of Rand Ris independently methyl or ethyl and each of Rand Ris independently hydrogen or methyl.6. The compound of claim 5 , wherein each of each of Rand Ris methyl and each of Rand Ris hydrogen.749.-. (canceled)51. The method of claim 50 , wherein said ophthalmic condition is an ocular protein mislocalization disorder.52. The method of claim 50 , wherein said ophthalmic condition is selected from the group consisting of wet or dry age related macular degeneration (ARMD) claim 50 , retinitis pigmentosa (RP) claim 50 , a retinal or macular dystrophy claim 50 , Stargardt's disease claim 50 , Sorsby's dystrophy claim 50 , autosomal dominant drusen claim 50 , Best's dystrophy claim 50 , peripherin mutation associate with macular dystrophy claim 50 , dominant form of Stargart's disease claim 50 , North Carolina macular dystrophy claim 50 , light toxicity claim 50 , normal vision loss related aging and normal loss of night vision related to aging.53. The method of claim 50 , wherein said ophthalmic condition is retinitis pigmentosa (RP).54. The method of claim 53 , wherein said RP is caused by aberrant opsin-folding.5580.-. (canceled) This application claims priority of U.S. Provisional Application Ser. No. 61/564,401, filed 29 Nov. 2011, Ser. No. 61/561,434, filed 18 Nov. 2011, and Ser. No. 61/627,855, filed 19 Oct. 2011, the disclosures of all ...

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Номер записи: 57
26-05-2016 дата публикации

TOBACCO-DERIVED COMPONENTS AND MATERIALS

Номер: US20160143347A1
Автор: Byrd Crystal Dawn Hege, Dube Michael Francis, Gerardi Anthony Richard
Принадлежит:

The invention provides a method of extracting and isolating certain compounds from tobacco. The resulting isolate can include more than 90% by weight of a given compound and can be used as a flavor component for tobacco material used in smoking articles and smokeless tobacco compositions. Exemplary compounds that may be present in the isolate according to the invention include, but are not limited to, solanone, neophytadiene, megastigmatrienone, β-damascenone, norsolanadione, cis-abienol, α-cembratrienediol, β-cembratrienediol, sucrose esters, and lutein. 1Nicotiana. A method of extracting and isolating compounds from plants of the species , comprising:{'i': 'Nicotiana', 'receiving a plant material of the species;'}contacting the plant material with a solvent for a time and under conditions sufficient to extract one or more desired compounds from the plant material into the solvent;separating the solvent containing the one or more desired compounds from the extracted plant material; andpurifying the solvent containing the one or more desired compounds to provide an isolate comprising at least about 75 percent by weight of the one or more desired compounds, the one or more desired compounds being selected from the group consisting of solanone, neophytadiene, megastigmatrienone, β-damascenone, norsolanadione, cis-abienol, α-cembratrienediol, β-cembratrienediol, sucrose esters, lutein, degradation products thereof, and mixtures thereof.2Nicotiana. The method of claim 1 , wherein the plant material of the species is in a form selected from the group consisting of whole leaf claim 1 , laminae claim 1 , cut filler claim 1 , volume expanded claim 1 , stems claim 1 , cut-rolled stems claim 1 , cut-puffed stems claim 1 , reconstituted tobacco claim 1 , and particulate.3Nicotiana. The method of claim 1 , wherein the plant material of the species is provided in green form.4Nicotiana. The method of claim 1 , wherein the plant material of the species is provided in cured form.5. ...

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Номер записи: 58
09-05-2019 дата публикации

SMALL MOLECULE INHIBITORS OF NECROPTOSIS

Номер: US20190135718A1
Автор: Hsu Emily P., Yuan Junying
Принадлежит:

The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-α induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role. 113-. (canceled)1539-. (canceled)4168-. (canceled)7092-. (canceled)100. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound of claim 14 , or any pharmaceutically acceptable salt or solvate thereof claim 14 , or any stereoisomer thereof.101. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound of claim 40 , or any pharmaceutically acceptable salt or solvate thereof claim 40 , or any stereoisomer thereof.102. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and the compound of claim 69 , or any pharmaceutically acceptable salt or solvate thereof claim 69 , or any stereoisomer thereof.103. A method of treating a condition in a subject claim 14 , said method comprising the step of administering the compound of claim 14 , or any pharmaceutically acceptable salt or solvate thereof claim 14 , or any stereoisomer thereof claim 14 , to said subject in a dosage sufficient to decrease necroptosis.104. A method of treating a condition in a subject claim 40 , said method comprising the step of administering the compound of claim 40 , or any pharmaceutically acceptable salt or solvate thereof claim 40 , or any stereoisomer thereof claim 40 , to said subject in a dosage sufficient to decrease necroptosis.105. A method of treating a condition in a ...

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Номер записи: 59
24-05-2018 дата публикации

A PROCESS FOR THE PREPARATION OF TERPINOLENE EPOXIDE

Номер: US20180141924A1
Автор: BENSON Stefan, GOETZ Roland, Kraus Helmut, NARAYANAN Sukunath, Rack Michael, RISHINARADAMANGALAM Chidambaram, WOLF Bernd
Принадлежит:

The present invention relates to a process for the preparation of terpinolene epoxide by epoxidation of terpinolene. 116.-. (canceled)18. The process according to claim 17 , wherein the halogenated ketone is selected from hexafluoroacetone claim 17 , hexachloroacetone claim 17 , perfluoromethyl isopropyl ketone claim 17 , perfluoromethyl ethyl ketone and any mixture thereof.19. The process according to claim 17 , wherein the halogenated ketone is hexachloroacetone.20. The process according to claim 17 , wherein the reaction is carried out in a non-halogenated inert organic solvent.21. The process according to claim 17 , wherein the non-halogenated inert organic solvent is selected from non-halogenated aliphatic hydrocarbons claim 17 , non-halogenated aromatic hydrocarbons and any mixture thereof.22. The process according to claim 20 , wherein the non-halogenated inert organic solvent is selected from non-halogenated aromatic hydrocarbons and any mixtures thereof.23. The process according to claim 17 , wherein the epoxidation is carried out in the presence of an organic base.24. The process according to claim 23 , wherein the base is selected from tertiary amines claim 23 , pyridine claim 23 , substituted pyridines claim 23 , bicyclic amines and any mixture thereof.25. The process according to claim 23 , wherein the base is pyridine or substituted pyridines.26. The process according to claim 23 , wherein the pH of the reaction mixture is from 3 to 6.27. The process according to claim 17 , wherein the molar ratio of the halogenated ketone to terpinolene is from 0.05:1 to 1:1.28. The process according to claim 17 , wherein the molar ratio of hydrogen peroxide to terpinolene is from 1:1 to 2:1.29. The process according to claim 17 , wherein the epoxidation is carried out at 5 to 40° C.30. The process according to claim 17 , wherein the terpinolene epoxide of formula (I) is further subjected to an epoxide ring opening isomerization leading to limonene-4-ol.31. The ...

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Номер записи: 60
04-06-2015 дата публикации

Control and repellency of bed bugs

Номер: US20150152038A1
Автор: Robert H. Bedoukian
Принадлежит: Bedoukian Research Inc

Control or repellency of bed bugs is accomplished by bringing the bed bugs into contact with at least one of the compounds of the structure (I); wherein R is selected from —OH, —OC(O)R 4 , —OR 6 , —(OR 6 ) 2 , wherein each R 6 is independently selected from an alkyl group containing from 1 to 4 carbon atoms and R 4 is a branched or straight chain saturated or unsaturated hydrocarbyl group with zero to two double bonds and from 1 to 15 carbon atoms; X is O or CH 2 , with the proviso that when X is O R can only be =0; each Z is independently selected from (CH) and (CH 2 ) y is a numeral selected from 1 and 2; R 1 is selected from H or a branched or straight chain saturated or unsaturated hydrocarbyl group with zero to two double bonds and from 1 to 15 carbon atoms. R 2 is selected from H and a branched or straight chain saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 15 carbon atoms. R 3 is selected from H, a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 15 carbon atoms, —(CH 2 ) n OH, —C(O)OR 5 , —CH 2 C(O)OR 7 , —CH 2 C(O)R 8 , —C(O)NR 9 R 10 , —CH 2 C(O)NR 11 R 12 where each of R 5 , R 7 , R 8 , R 9 , R 10 , R 11 and R 12 is independently selected from H and a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 15 carbon atoms, and n is an integer of from 1 to 12; and the bond between the 2 and 3 positions in the ring structure may be a single or a double bond, and wherein the compounds of structure (1) contain from 11 to 20 total carbon atoms, except where R is ═O, X═CH 2 and y is 1 the compounds of structure (I) contain from 13 to 20 total carbon atoms in the compounds, wherein the compounds of structure (1) contain from 11 to 20 total carbon atoms, except where R is ═O, X═CH2 and y is 1 the compounds of structure (I) contain from 13 to 20 total carbon atoms in the compounds, wherein the ...

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Номер записи: 61
31-05-2018 дата публикации

CONTROL AND REPELLENCY OF BITING FLIES, HOUSE FLIES, TICKS, ANTS, FLEAS, BITING MIDGES, COCKROACHES, SPIDERS AND STINK BUGS

Номер: US20180146668A1
Автор: BEDOUKIAN Robert H.
Принадлежит:

Control and repellency of biting flies, house flies, ticks, ants, fleas, biting midges, cockroaches, spiders and stink bugs is obtained by contact of the insects with at least one of the compounds of the structure (I) 2. The method according to wherein the compounds of structure (1) have from 12 to 16 carbon atoms in the compound.3. The method according to wherein the at least one compound of structure (I) is a compound wherein{'sub': 2', '1', '2', '3', '1', '2', '3, 'R is ═O, X is O, y is 1 or 2, each Z is selected from the group consisting of (CH) and (CH), the bond between positions 2 and 3 in the ring is a single bond, one of Rand Ris H or —CHand the other of Rand Ris a hydrocarbyl group containing from 9 to 15 carbon atoms, and Ris H.'}5. The method according to wherein the at least one compound of structure (I) is applied to a surface of or impregnated into clothing or fabric.6. The method according to wherein the at least one compound of structure (I) is applied to the skin in the form of wipes claim 1 , lotions claim 1 , creams claim 1 , oils claim 1 , or sprays.7. The method according to a wherein the at least one compound of structure (I) is applied to cleaning products.8. The method according to wherein the insect is brought into contact with at the least one of the compounds of structure (I) in combination with a compound selected from DEET® (N claim 1 ,N-Diethyl-m-toluamide) and para-menthane-3 claim 1 ,8-diol.9. The method according to wherein the contacting of ticks with the at least one compound of structure (I) produces toxicity to the ticks.10. The method according to wherein the contacting of roaches with the at least one compound of structure (I) produces toxicity to the roaches.11. The method of for obtaining toxicity of the insects wherein the at least one compound of structure (I) contains from 11 to 17 carbon atoms.12. The method of for obtaining toxicity of the insects wherein the at least one compound of structure (I) contains from 11 to 14 ...

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Номер записи: 62
11-06-2015 дата публикации

Process for the production of a mixture comprising cyclohexanone and cyclohexanol from phenol

Номер: US20150158802A1
Автор: Corinne Daguenet, Iris Verschuren, Johan Thomas Tinge, Robert Jan de Korte, Roeland Wilhelmus Theodorus Maria Brands, Wilhelmus Rudolf Maria Martens
Принадлежит: DSM IP ASSETS BV

The present invention provides a process for continuously preparing a mixture of cyclohexanone and cyclohexanol comprising, a) hydrogenating phenol with gaseous hydrogen, in the presence of platinum or palladium, in a hydrogenation reactor, to produce a hydrogenation product stream comprising cyclohexanone, cyclohexanol, phenol and hydrogen; b) cooling the hydrogenation product stream to a temperature such that the fraction of phenol by mass in a first gas phase is lower than the fraction of phenol by mass in a first liquid phase; c) separating the first gas phase from the first liquid phase; d) returning at least part of the first gas phase to the hydrogenation reactor; e) heating the first liquid phase; f) purifying the first liquid phase by distillation; characterized in that heat is transferred from the hydrogenation product stream in step b) to another part of the process by means of in-process heat exchange; a mixture of cyclohexanone and cyclohexanol obtained by the process; and a chemical plant suitable for continuously preparing mixture of cyclohexanone and cyclohexanol according to the process.

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Номер записи: 63
11-06-2015 дата публикации

PREVENTION OR SUPPRESSION OF CYRSTALLISATION OF BORIC ACID PRESENT IN AN AQUEOUS PHASE

Номер: US20150158810A1
Автор: Autissier Laurence, Briere Alix, Longuet Laurence
Принадлежит:

The invention relates to the use of at least one compound comprising at least two hydroxyl functions, the compound being selected from alcohols, aminoalcohols, carboxylic acids and hydroxyacids, for preventing the crystallization of boric acid present in an aqueous phase, or for suppressing this crystallization when this crystallization has already been initiated. 1. A method comprising:using at least one compound comprising at least two hydroxyl functions, the compound being selected from alcohols, aminoalcohols, carboxylic acids, and hydroxyacids, to prevent crystallization of boric acid present in an aqueous phase, or to suppress said crystallization when crystallization has already been initiated.2. The method according to claim 1 , wherein the compound comprising at least two hydroxyl functions includes a total number of carbon atoms which is at most equal to eight.3. The method according to claim 2 , wherein the compound comprising at least two hydroxyl functions includes from 2 to 6 hydroxyl functions.4. The method according to claim 3 , wherein the compound comprising at least two hydroxyl functions is selected from maleic acid claim 3 , 2 claim 3 ,2-dimethylpropane-1 claim 3 ,3-diol claim 3 , 2-amino-2-(hydroxymethyl)-propane-1 claim 3 ,3-diol claim 3 , 2-[bis-(2-hydroxyethyl)-amino]-2-(hydroxymethyl)-propane-1 claim 3 ,3-diol claim 3 , myo-inositol claim 3 , and pentaerythritol.5. The method according to claim 4 , wherein the compound comprising at least two hydroxyl functions is selected from 2-amino-2-(hydroxymethyl)-propane-1 claim 4 ,3-diol claim 4 , 2-[bis-(2-hydroxyethyl)-amino]-2-(hydroxymethyl)-propane-1 claim 4 ,3-diol claim 4 , and pentaerythritol.6. The method according to any of the preceding claim 1 , wherein a mass concentration of boric acid in the aqueous phase is at least equal to a value of a mass solubility of boric acid at a temperature which is exhibited by said aqueous phase containing boric acid.7. The method according to claim 1 , ...

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Номер записи: 64
07-06-2018 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20180155359A9
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., MacRury Thomas B., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (II): 3. The compound of wherein:{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 3', '8', '9', '11', '8', '9', '12', '8', '9', '9a', '8', '9', '9a', '8', '9', '9a, 'sub': 2', '2', '2, 'Ris —R—N(R)C(O)R, —R—N(R)—R, —R—N(R)C(═NCN)N(R), —R—N(R)C(O)N(R)or —R—N(R)C(S)N(R);'}{'sup': 4a', '4b, 'Rand Rare each independently hydrogen, alkyl, alkenyl or alkynyl;'}{'sup': 4a', '4b', '7, 'or Ris hydrogen, alkyl, alkenyl or alkynyl and Ris a direct bond to the carbon to which Ris attached;'}{'sup': 5', '5, 'Ris alkyl or Ris a direct bond to the carbon at C14;'}{'sup': 6', '8', '9', '8', '9, 'sub': '2', 'Ris hydrogen, —R—ORor —R—N(R);'}{'sup': 7', '8', '9', '8', '9', '7', '4b', '7, 'sub': '2', 'Ris hydrogen, —R—OR, —R—N(R), or a direct bond to C15, provided that when Ris a direct bond to C15, Ris not a direct bond to the carbon to which Ris attached;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain;'}{'sup': '9', 'each Ris hydrogen, alkyl, optionally substituted aryl and optionally substituted aralkyl;'}{'sup': '9a', 'each Ris hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl; optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl;'}{'sup': '11', 'Ris optionally substituted heteroaryl; and'}{'sup': '12', 'Ris optionally substituted heterocyclyl.'}4. The compound of wherein:{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 3', '8', '9', '11', '8', '9', '12', '8', '9', '9a', '8', '9', '9a', '8', '9', '9a, 'sub': 2', '2', '2, 'Ris —R—N(R)C(O)R, —R—N(R)—R, —R—N(R)C(═NCN)N(R), —R—N(R)C(O)N(R)or —R—N(R)C(S)N(R);'}{'sup': 4a', '4b, 'Rand Rare each alkyl;'}{'sup': '5', 'Ris a direct bond to the carbon at C14;'}{'sup': '6', 'Ris hydrogen;'}{'sup': '7', 'Ris hydrogen;'}{'sup ...

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Номер записи: 65
28-08-2014 дата публикации

METHODS AND INTERMEDIATES FOR PREPARING MACROLACTAMS

Номер: US20140243519A1
Автор: Baxter Carl, Beutner Gregory L., Cleator Edward, Humphrey Guy, Kuethe Jeffrey T., Yasuda Nobuyoshi, Zhong Yong-Li
Принадлежит:

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applica 11. The method of claim 10 , wherein the reaction uses tri tert-butylphosphine tetra fluoroborate salt in a solvent claim 10 , and Compound 8 is provided as either a dibenzylamine salt or a t-butylamine salt. The present invention relates to process and intermediates that can be used for preparing macrolactams. One use of the methods and intermediates described herein is the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.Hepatitis C virus (HCV) infection is a major health problem. HCV infection leads to chronic liver disease, such as cirrhosis and hepatocellular carcinoma, in a substantial number of infected individuals.Several virally-encoded enzymes are putative targets for therapeutic intervention, including a metalloprotease (NS2-3), a serine protease (NS3), a helicase (NS3), and an RNA-dependent RNA polymerase (NS5B). The NS3 protease is located in the N-terminal domain of the NS3 protein. NS4A provides a cofactor for NS3 activity.Potential treatments for HCV infection are discussed in different references including Balsano, 8(4):307-318, 2008, Rönn et al., 8:533-562, 2008, Sheldon et al., 16(8):1171-1181, 2007, and De Francesco et al., 58:1-16, 2003.Examples of publications describing macrolactam compounds able to inhibit HCV protease activity include: Harper et al., WO2010011566; Liverton et al., WO2009134624; McCauley et al., WO2009108507; Liverton et al., WO2009010804; Liverton et al., WO2008057209; Liverton et al., WO2008051477; Liverton et al., WO2008051514; ...

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Номер записи: 66
25-06-2015 дата публикации

Cycloalkane Oxidation Catalysts and Method to Produce Alcohols and Ketones

Номер: US20150175514A1
Автор: DECAMPO Floryan, HE Mingyuan, Liu Yueming, Wu Peng, Xue Kai, Zhou Wenjuan
Принадлежит:

Disclosed is a method of oxidizing a cycloalkane to form a product mixture containing a corresponding alcohol and ketone, said method comprising contacting a cycloalkane with a hydroperoxide in the presence of a catalytic effective amount of a crystalline MWW-type titanosilicate catalyst. Hydroperoxides may notably be tert-butyl hydroperoxide, tert-amyl hydroperoxide, cumene hydroperoxide, ethylbenzene hydroperoxide, cyclohexyl hydroperoxide, methylcyclohexyl hydroperoxide, tetralin hydroperoxide, isobutylbenzene hydroperoxide, and ethylnaphthalene hydroperoxide. 1. A method of oxidizing a cycloalkane to form a product mixture containing a corresponding alcohol and ketone , said method comprising contacting a cycloalkane with a hydroperoxide in the presence of a catalytically effective amount of a crystalline MWW-type titanosilicate catalyst.2. A method according to claim 1 , in which the hydroperoxide is chosen in the group consisting of: tert-butyl hydroperoxide claim 1 , tert-amyl hydroperoxide claim 1 , cumene hydroperoxide claim 1 , ethylbenzene hydroperoxide claim 1 , cyclohexyl hydroperoxide claim 1 , methylcyclohexyl hydroperoxide claim 1 , tetralin claim 1 , isobutylbenzene hydroperoxide claim 1 , and ethylnaphthalene hydroperoxide.3. A method according to claim 1 , in which the hydroperoxide is added to the cycloalkane at the start of the step of contacting.4. A method according to claim 1 , in which the hydroperoxide is generated in situ by reaction of a cycloalkane with oxygen or an oxygen generator.6. A method according to claim 1 , in which the catalyst further comprises one or more heteroatoms from the group consisting of the elements of Periods IB claim 1 , IVB claim 1 , VB claim 1 , VIB claim 1 , VIIB claim 1 , VIIIB and VA.7. A method according to claim 1 , in which the contacting is at a temperature of between 20 and 200° C.8. A method according to claim 1 , in which pure oxygen claim 1 , air claim 1 , oxygen-enriched air claim 1 , oxygen-depleted ...

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Номер записи: 67
11-09-2014 дата публикации

Opsin-Binding Ligands, Compositions and Methods of Use

Номер: US20140256782A1
Автор: Berman Judd, Cote Jamie B., Frye Leah L., Garvey David S., Greenwood Jeremy R., Larosa Gregory J., Quach Tan
Принадлежит: BIKAM PHARMACEUTICALS, INC.

Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic is visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.

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Номер записи: 68
11-09-2014 дата публикации

Method for Producing Lutein from Tobacco

Номер: US20140256829A1
Автор: Junker Christopher
Принадлежит:

A method for producing lutein from one or more plants of genus is provided. The lutein can be derived inter alia from species biomass. A method such as is described in various embodiments herein also provides articles and compositions that include lutein produced from one or more plants of genus

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Номер записи: 69
11-09-2014 дата публикации

CYCLOHEXANOL, METHOD FOR PRODUCING CYCLOHEXANOL, AND METHOD FOR PRODUCING ADIPIC ACID

Номер: US20140256981A1
Автор: Narisawa Naoki, Tanaka Katsutoshi
Принадлежит: ASAHI KASEI CHEMICALS CORPORATION

A purified cyclohexanol of the present invention has a methylcyclopentanol concentration of 10 to 1000 ppm by weight and a cyclohexylcyclohexene isomer concentration of 15 to 500 ppm by weight. A method for producing cyclohexanol of the present invention comprises: Step 1 of producing a solution (I) containing cyclohexanol, methylcyclopentanol, and water by a hydration reaction of cyclohexene; Step 2 of separating the solution (I) into a water phase and an oil phase; Step 3 of obtaining a partially purified cyclohexanol containing methylcyclopentanol from the oil phase; and Step 4 of separating and removing methylcyclopentanol in the partially purified cyclohexanol so as to obtain a purified cyclohexanol having a methylcyclopentanol concentration of 10 to 1000 ppm by weight and a cyclohexylcyclohexene isomer concentration of 15 to 500 ppm by weight.

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Номер записи: 70
01-07-2021 дата публикации

Method for producing menthol particles stabilized against caking, and storage-stable menthol particles and use thereof

Номер: US20210198169A1
Автор: Gerd Tebben, Gunnar Heydrich, Matthias Rauls, Sebastian WLOCH
Принадлежит: BASF SE

The present invention relates to a process for producing menthol particles stabilized against caking, wherein menthol particles are, following shaping, stored for at least 7 days at a temperature of 0 to 30° C., after which the menthol particles are supplied with a minimum input of mechanical energy. The present invention further relates to storage-stable menthol particles and to the use of said menthol particles in household and consumer goods of all kinds.

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Номер записи: 71
22-06-2017 дата публикации

METHOD FOR SYNTHEZISING CYCLOHEXENONES FOR USE IN THE PERFUME INDUSTRY AND COMPOUNDS OBTAINED THEREBY

Номер: US20170174602A1
Автор: Chanot Jean-Jacques, PLESSIS Caroline
Принадлежит:

Cyclohexenone and cyclohexenol compounds are provided having specific fragrances and remanence properties, along with methods for synthesizing these compounds, including obtaining the compound by condensing a ketone on an α-methylene-aldehyde in order to obtain, by means of a domino reaction, compounds of formula (II) as follows: 2. The compound according to wherein R3 is either a cyclopentyl group substituted by one or more alkyl groups claim 1 , or a cyclopentenyl group substituted by one or more alkyl groups.3. The compound according to wherein R3 is an alkyl or alkenyl group claim 1 , optionally substituted by an aryl.4. The compound according to wherein Z═C(O).5. The compound according to wherein Z═CR4(OR5) with R4 represents a hydrogen or a C1-C8 alkyl or C2-C8 alkenyl group claim 1 , and R5 represents a hydrogen.6. A composition comprising at least one compound of general formula (II) such as defined in claim 1 , in the form of a stereoisomer or of a mixture of stereoisomers claim 1 , or of a racemic mixture.7. The composition according to further comprising at least one additional fragrancing substance.8. The composition according to wherein the compound of formula (II) is present in a concentration of between 0.1 and 99% by weight relative to the total weight of the composition.9. The composition according to wherein the compound of formula (II) is present in a concentration of between 0.1 and 30% by weight relative to the total weight of the composition.10. A fragrant agent or a flavoring agent comprising the compound of and an acceptable fragrant agent or flavoring agent carrier.11. A masking agent of odors and/or flavors comprising the compound of and an acceptable masking agent carrier.12. A pharmaceutical claim 1 , cosmetic claim 1 , or food composition comprising the compound according to in combination with perfuming ingredients claim 1 , flavoring ingredients claim 1 , solvents claim 1 , additives claim 1 , or fixatives.13. A method for conferring ...

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Номер записи: 72
06-06-2019 дата публикации

METHODS OF MAKING STABLE AND THERMALLY POLYMERIZABLE VINYL, AMINO OR OLIGOMERIC PHENOXY BENZOCYCLOBUTENE MONOMERS WITH IMPROVED CURING KINETICS

Номер: US20190169327A1
Автор: Gallagher Michael K., Hayes Colin, Riener Michelle
Принадлежит:

The present invention provides methods of making low energy polymerizable monomers and resins for use in making dielectric materials. The methods comprise deprotecting or deacylating an organic alkali cleavable protecting group containing addition polymerizable, amine containing aromatic monomer or oligoaromatic phenol resin containing an organic alkali cleavable protecting group, such as a Cto Calkanoyl group, preferably, an acyl group, by hydrolyzing to remove the protecting group in organic alkali in a polar solvent containing an excess of alkali Cto Calkoxide and form a hydroxyl functional monomer or resin, followed by; reacting via nucleophilic substitution the resulting hydroxyl functional monomer or resin with an alpha-halide (α-halide) or strong acid conjugate leaving group containing arylcyclobutene compound in a polar solvent, to yield a product an arylcyclobutene-containing addition polymerizable or amine containing aromatic monomer or oligoaromatic phenol resin having an ether linkage from the cyclobutene ring to an aromatic group of the addition polymerizable aromatic monomer, aromatic amine or oligoaromatic phenol. 1. A method of making a monomer or resin composition comprises:{'sub': 1', '7, 'deprotecting or deacylating an organic alkali cleavable protecting group containing aromatic monomer or resin chosen from an addition polymerizable group containing aromatic monomer, an amine containing aromatic monomer, or an oligoaromatic phenol compound containing a phenolic hydroxyl by hydrolyzing it to remove the protecting group in organic alkali in a polar solvent containing an excess of alkali Cto Calkoxide to form an hydroxyl functional addition polymerizable aromatic monomer, hydroxyl functional aromatic amine functional group containing monomer or hydroxyl functional oligoaromatic compound, followed by;'}reacting via nucleophilic substitution the resulting hydroxyl functional addition polymerizable aromatic monomer, aromatic amine functional group ...

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Номер записи: 73
08-07-2021 дата публикации

Shelf life mass polymerizable polycycloolefin compositions as optical materials

Номер: US20210206789A1
Автор: Oleksandr BURTOVYY
Принадлежит: PROMERUS LLC

Embodiments in accordance with the present invention encompass compositions encompassing a latent organo-ruthenium compound and a pyridine compound along with one or more monomers which undergo ring open metathesis polymerization (ROMP) when said composition is exposed to suitable actinic radiation to form a substantially transparent film. Surprisingly, the compositions are very stable at ambient conditions to temperatures up to 80° C. for several days and undergo mass polymerization when subject only to actinic radiation. Accordingly, compositions of this invention are useful in various opto-electronic applications, including as 3D printing materials, coatings, encapsulants, fillers, leveling agents, among others.

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Номер записи: 74
13-06-2019 дата публикации

FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF

Номер: US20190177271A1
Автор: Ito Hirotsugu, Kobayashi Satoru, Morita Toru, Motomura Takahisa, Nagamori Hironobu, Shinkai Hisashi, Suzawa Koichi
Принадлежит:

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: 1. (canceled) The present invention relates to a fluorene compound and a pharmaceutical use thereof. More particularly, the present invention relates to a compound for the prophylaxis or treatment of diabetes, cardiovascular diseases, hyperlactacidemia and cancer based on activation of pyruvate dehydrogenase (PDH) by inhibition of pyruvate dehydrogenase kinase (PDHK), and use thereof. Furthermore, the present invention relates to a compound for the prophylaxis or treatment of diabetic complications (e.g., neuropathy, retinopathy, nephropathy, cataract etc.), brain ischemia, cerebral apoplexy or pulmonary hypertension, and use thereof.In tissue, for reaction using energy, for example, biosynthesis, active biological transport, muscle contraction etc., the energy is supplied by hydrolysis of adenosine triphosphate (ATP). ATP is produced by oxidation of metabolic fuel which yields much energy, such as glucose and free fatty acids. In oxidative tissues such as muscle, ATP is mostly produced from acetyl-CoA that enters citric acid cycle. Acetyl-CoA is produced by oxidation of glucose via glycolytic pathway or β oxidation of free fatty acid. An enzyme that plays a pivotal role in controlling acetyl-CoA production from glucose is PDH. PDH catalyses the oxidation of pyruvate to acetyl-CoA and carbon dioxide with concomitant reduction of nicotinamide adenine dinucleotide (NAD) to NADH.PDH is a multienzyme complex ...

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Номер записи: 75
04-06-2020 дата публикации

Blends containing enantiomerically pure ambrocenide®

Номер: US20200172830A1
Автор: Marcus Eh, Stefan Lambrecht
Принадлежит: SYMRISE AG

The present invention relates in particular to a mixture comprising the compound of formula (Ia) as described herein, wherein the mixture is free or essentially free of the compound of formula (Ib) as described herein, preferably of the compounds of formulae (Ib) and furthermore (Ic) and/or (Id) as described herein. The invention further relates to a method for manufacturing said mixture, fragrance substance compositions containing or consisting of said mixture, perfumed products containing said mixtures or fragrance substance compositions, and various methods and uses for imparting, modifying and/or enhancing certain odour notes.

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Номер записи: 76
15-07-2021 дата публикации

Novel Biphenyl Derivative Compound and Use Thereof

Номер: US20210214324A1
Автор: Kim Bo-kyung, KIM Hwang Suk, LEE Hee-Yoon, LEE Hongsoo, LEE Je Jin, LEE Kong Joo, Seo Ji-wan, SHIN Ji Soo
Принадлежит:

The present disclosure provides a novel biphenyl derivative compound or a pharmaceutically acceptable salt thereof. The biphenyl derivative compound or pharmaceutically acceptable salt thereof according to the present disclosure is a compound that increases Nm23-H1/NDPK activity and can inhibit cancer metastasis and growth. Thus, it exhibits excellent effects not only on the prevention, alleviation and treatment of cancer, but also on the suppression of cancer metastasis. 2. The biphenyl derivative compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the Cto Calkoxy group is any one selected from the group consisting of methoxy claim 1 , ethoxy and propoxy groups.3. The biphenyl derivative compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Rto Rare each independently hydroxy or methoxy.4. The biphenyl derivative compound or pharmaceutically acceptable salt thereof according to claim 3 , wherein each of R claim 3 , R claim 3 , Rand Ris independently hydroxy or methoxy and wherein at least two of R claim 3 , R claim 3 , Rand Rare methoxy groups.5. The biphenyl derivative compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein L is —(C—C)— claim 1 , and each of R claim 1 , R claim 1 , Rand Ris methoxy.7. A pharmaceutical composition for treating or preventing cancer claim 1 , the pharmaceutical composition containing claim 1 , as an active ingredient claim 1 , the biphenyl derivative compound or pharmaceutically acceptable salt thereof according to .8. The pharmaceutical composition of claim 7 , wherein the cancer is cancer selected from the group consisting of breast cancer claim 7 , lung cancer claim 7 , melanoma claim 7 , prostate cancer claim 7 , colorectal cancer claim 7 , bladder cancer claim 7 , bone cancer claim 7 , blood cancer claim 7 , thyroid cancer claim 7 , parathyroid cancer claim 7 , bone marrow cancer claim 7 , rectal cancer claim 7 , throat cancer claim 7 , ...

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Номер записи: 77
07-07-2016 дата публикации

REAGENT FOR ENHANCING GENERATION OF CHEMICAL SPECIES

Номер: US20160194300A1
Автор: Enomoto Satoshi
Принадлежит:

A reagent that enhances acid generation of a photoacid generator and composition containing such reagent is disclosed. 2. (canceled)3. The reagent according to claim 1 , wherein a reaction of the chemical species with a first compound or the precursor regenerates the chemical species.4. (canceled)5. (canceled)6. The reagent according to claim 1 , wherein the intermediate has a reducing character.7. The reagent according to claim 1 , wherein the intermediate is a radical.8. The reagent according to claim 1 , wherein the intermediate discharges at least one of a hydrogen atom and hydrogen ion that have reducing characters.9. The reagent according to claim 1 , wherein the intermediate is a ketyl radical.10. The reagent according to claim 1 , wherein the chemical species is acid.1114.-. (canceled)15. A composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the reagent according to ; and'}the precursor.16. The composition according to claim 15 , further comprising:the first compound.1724.-. (canceled)25. The reagent according to claim 1 , wherein Ris connected to Rthrough at least one bond.26. The reagent according to claim 1 , wherein at least one of Rand Ris an aromatic group.27. The reagent according to claim 1 , wherein the product is formed by oxidation of the intermediate.28. (canceled)29. The reagent according to claim 1 , wherein:the reagent further includes a second cyclic moiety; andthe first cyclic moiety contains at least two atoms which are also contained in the second cyclic moiety.30. (canceled)31. (canceled)32. The reagent according to claim 1 , wherein Ris one of an ester group claim 1 , alkyl group and tetrahydropyranyl group.3335.-. (canceled)36. A method for manufacturing a device claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00015', 'claim 15'}, 'applying a solution of the composition according to to a substrate such that a coating film including the composition is formed on the substrate;'}a first ...

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Номер записи: 78
16-07-2015 дата публикации

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR MODULATORS AND USES THEREOF IN REGULATING BLOOD GLUCOSE LEVELS

Номер: US20150197480A9
Автор: Chein Rong-Jie, KING Klim
Принадлежит:

The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sub': 'A', 'Gis hydrogen, ═O, ═S, —OR″, —SR″, —NR″H, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, a thiocarbamate group, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms, wherein each instance of R″ is independently hydrogen, a cyclic or acyclic, saturated or unsaturated, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 16 carbon atoms;'}{'sub': A1', 'A2', 'A3', 'A4', 'A5', 'A6', 'A7', 'A8', 'A9', 'A10, 'R, R, R, R, R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbons;'}{'sub': A11', 'A12', 'A13', 'A15', 'A16', 'A17, 'R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms;'}{'sub': 'A14', 'Ris halogen, —NR″H, —SR″, —OR″, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, or a thiocarbamate group;'}{'sub': 'A20', 'Ris hydrogen, halogen, or a cyclic or acyclic, substituted ...

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Номер записи: 79
25-09-2014 дата публикации

Cross-Linked Organic Polymer Compositions and Methods for Controlling Cross-Linking Reaction Rate and of Modifying Same to Enhance Processability

Номер: US20140284850A1
Автор: Boland Rodger K., Burgoyne, Das Sudipto, Drake Kerry A., JR. WILLIAM F., Nordquist Andrew F., Song Le, Williams Shawn P.
Принадлежит:

The invention includes a cross-linking composition comprising a cross-linking compound and a cross-linking reaction additive selected from an organic acid and/or an acetate compound, wherein the cross-linking compound has the structure according to formula (IV): 3. The composition according to claim 1 , wherein the arene moiety has a molecular weight of about 1 claim 1 ,000 g/mol to about 9 claim 1 ,000 g/mol.4. The composition according to claim 3 , wherein the arene moiety has a molecular weight of about 2 claim 3 ,000 g/mol to about 7 claim 3 ,000 g/mol.5. The composition according to claim 1 , wherein the cross-linking reaction additive is an organic acid selected from glacial acetic acid claim 1 , formic acid claim 1 , and/or benzoic acid.7. The composition according to claim 6 , wherein the acetate compound is selected from lithium acetate hydrate sodium acetate claim 6 , and/or potassium acetate claim 6 , and salts and derivatives thereof.8. The composition according to claim 1 , wherein the weight percentage ratio of the cross-linking compound to the cross-linking reaction additive is about 10:1 to about 10 claim 1 ,000:1.9. The composition according to claim 8 , wherein the weight percentage ratio of the cross-linking compound to the cross-linking reaction additive is about 20:1 to about 1000:1.10. The composition according to claim 1 , further comprising at least one organic polymer claim 1 , wherein the cross-linking reaction additive is capable of reacting with the cross-linking compound to form a reactive intermediate in the form of an oligomer claim 1 , which reactive intermediate oligomer is capable of cross-linking the organic polymer.11. The organic polymer composition according to claim 10 , wherein the organic polymer is selected from poly(arylene ether)s claim 10 , polysulfones claim 10 , polyethersulfones claim 10 , polyimides claim 10 , polyamides claim 10 , polyureas claim 10 , polyurethanes claim 10 , polyphthalamides claim 10 , polyamide- ...

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Номер записи: 80
18-06-2020 дата публикации

Novel organic solubilisation and/or extraction solvent, extraction method using said solvent, and extracts obtained by said method

Номер: US20200190000A1
Автор: Anne-Sylvie FABIANO TIXIER, Antoine Charles BILY, Farid Chemat, Marc Roller, Natacha ROMBAUT, Simona BIRTIC
Принадлежит: Naturex SA, Universite dAvignon et des Pays de Vaucluse

The invention relates to a novel organic solubilisation and/or extraction solvent comprising at least one compound selected from the group of saturated monocyclic terpenoids, to an extraction method using said solvent, and to extracts obtained by said method. More particularly, the invention relates to a novel use of para-menthane, a saturated terpenoid compound, as a solvent derived from natural substances, and also to a solvent comprising para-menthane.

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Номер записи: 81
26-07-2018 дата публикации

NAPHTHALENE-CONTAINING POLYMERS AND METHODS OF MAKING THE SAME

Номер: US20180208716A1
Автор: MUKARAKATE Calvin, NIMLOS Mark R., PRICE Mariel Jene, WILSON Andrew Nolan
Принадлежит:

The present disclosure relates to a dimer that includes a first hydroxyl-functionalized naphthalene group and a second hydroxyl-functionalized naphthalene group, where the first hydroxyl-functionalized naphthalene group and the second hydroxyl-functionalized naphthalene group are connected by a bridging group. The present disclosure also relates to a polymer synthesized using the dimer, as well as methods for synthesizing both the dimer and the polymer. 1. A dimer comprising:a first hydroxyl-functionalized naphthalene group; anda second hydroxyl-functionalized naphthalene group, wherein:the first hydroxyl-functionalized naphthalene group and the second hydroxyl-functionalized naphthalene group are connected by a bridging group.2. The dimer of claim 1 , wherein the bridging group comprises an aliphatic group.6. A polymer comprising: a first hydroxyl-functionalized naphthalene group; and', 'a second hydroxyl-functionalized naphthalene group, wherein:', 'the first hydroxyl-functionalized naphthalene group and the second hydroxyl-functionalized naphthalene group are connected by a bridging group, wherein:, 'a dimer comprisingthe polymer contains between 2 and 1500 units of the dimer, andthe bridging group comprises an aliphatic group.10. The polymer of claim 7 , wherein the polymer is endcapped with at least one of a hydroxyl group claim 7 , a halogen claim 7 , an amine claim 7 , or an oxygenated aromatic.12. The polymer of claim 6 , further comprising a weight averaged molecular weight claim 6 , M claim 6 , between 3 kDa and 400 kDa.13. The polymer of claim 6 , further comprising a degradation temperature between 150° C. and 500° C.14. The polymer of claim 6 , further comprising a glass transition temperature claim 6 , T claim 6 , between 50° C. and 200° C.15. A method comprising:reacting a precursor molecule with a first bridging molecule to form a dimer, wherein:the precursor molecule comprises a hydroxyl-functionalized naphthalene, andthe first bridging molecule ...

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Номер записи: 82
05-08-2021 дата публикации

METHOD FOR MANUFACTURING ISOPULEGOL

Номер: US20210238115A1
Автор: Kimura Kazuki, KOIKE Ayaka, Komatsuki Yasuhiro, Taira Kazuya
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

A method for manufacturing isopulegol includes the step of diastereoselective ring-closing a citronellal using an aluminum compound of formula (1) below. In formula (1), X represents a halogen atom, Y represents a halogen atom or a hydrogen atom, and Rrepresents a phenyl group or a cycloalkyl group of 5 to 12 carbons. 2. The method for manufacturing isopulegol according to claim 1 , wherein said X is a chlorine atom or a bromine atom.3. The method for manufacturing isopulegol according to claim 1 , wherein said Y is a chlorine atom or a bromine atom.4. The method for manufacturing isopulegol according to claim 1 , wherein said Ris a cyclohexyl group.5. The method for manufacturing isopulegol according to claim 1 , wherein the step of diastereoselective ring-closing a citronellal is performed in the presence of a β-keto ester or a β-diketone.6. The method for manufacturing isopulegol according to claim 5 , wherein the β-keto ester is an acetoacetic acid ester. This application claims priority from Japanese Patent Application No. 2020-013700 filed on Jan. 30, 2020, the entire subject matter of which is incorporated herein by reference.The present invention relates to a method for manufacturing isopulegol.Isopulegol is common as a cooling agent, and one of the reactions to produce isopulegol is the catalytic ring-closing of citronellal. Due to four diastereomers in isopulegol, it is need a selective ring-closing method to produce isopulegol with highly diastereomer ratio, especially, it is need a catalyst for ring-closing of citronellal in a highly normal ratio.Recently, for solving the above problem, a synthetic method has been found with highly normal ratio by aluminum catalyst (Patent Documents 1 to 7).Patent Document 1: US 2015/0315110 A1Patent Document 2: U.S. Pat. No. 8,329,931 B2Patent Document 3: U.S. Pat. No. 8,580,991 B2Patent Document 4: US 2011/0319638 A1Patent Document 5: U.S. Pat. No. 8,329,930 B2Patent Document 6: U.S. Pat. No. 7,550,633 B2Patent ...

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Номер записи: 83
09-10-2014 дата публикации

Process for Preparing Xanthophyll Crystal

Номер: US20140303406A1
Автор: An Xiaodong, Cheng Yuanxin, LIAN Yunhe, Lu Qingguo, QI Lijun, SU Xuehui
Принадлежит: Chenguang Biotech Group Co., Ltd.

Disclosed a process for preparing a xanthophyll crystal, comprising: dissolving the plant extract containing a xanthophyll ester in n-hexane, then filtering the mixture; adding acetone to the filtrate, filtering and collecting a filter cake; mixing the filter cake with soybean oil and ethanol uniformly; saponifying the mixed solution with alkaline aqueous solution; then adding an acidic solution thereto until the mixed solution becomes acidic, concentrating under reduced pressure to obtain a pasty substance; adding n-hexane to the pasty saponified product, standing still and then conducting a solid-liquid separation; washing the resulting solid substance with deionized water; adding a mixed solvent to the washed solid substance, dissolving it with stirring; and then adding n-hexane thereto and standing still to recrystallize. According to the application, organic solvents are used to treat the plant extract and remove non-xanthophyll ester compounds in order to improve the efficiency of the saponification reaction; the saponified solution is concentrated under acidic condition at reduced pressure, then extracted with an organic solvent for saving water; purifying a xanthophyll crystal with a mixed solvent in order to significantly increase the purity of a xanthophyll crystal and proportion of trans-xanthophyll. 1. A process for preparing xanthophyll crystal , comprising the following steps:a) dissolving a plant extract containing a xanthophyll ester in n-hexane, then filtering the mixture;b) adding acetone to the filtrate, standing still, then filtering and collecting a filter cake;c) dissolving the filter cake with soybean oil and ethanol in order to obtain a mixed solution;d) saponifying the mixed solution with an alkaline aqueous solution;e) adding an acidic solution to the saponified solution until the mixed solution becomes acidic, and maintaining the temperature between 40-60° C. during the process of adding the acidic solution;f) recovering the solvent and ...

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Номер записи: 84
27-08-2015 дата публикации

POLYMERIZABLE SPIROBISINDANE MONOMERS AND POLYMERS PREPARED THEREFROM

Номер: US20150239806A1
Автор: Wendland Michael S.
Принадлежит:

Monomers and polymerizable compositions that can be polymerized using a free-radical polymerization reaction are provided. The monomers have two vinyl groups as well as a spirobisindane-type structure. Polymers prepared from the polymerizable compositions are also provided. The polymers can be porous. 2. The compound of claim 1 , wherein each R1 is hydrogen or halo.3. The compound of claim 1 , wherein each R2 and each R3 are alkyl.4. The compound of claim 1 , wherein R4 is hydrogen.5. The compound of claim 1 , wherein the compound is 3 claim 1 ,3 claim 1 ,3′ claim 1 ,3′-tetramethyl-1 claim 1 ,1′-spirobisindan-6 claim 1 ,6′-divinyl.7. The polymerizable composition of claim 6 , wherein the polymerizable composition further comprises a polyvinyl aromatic monomer or a polyvinyl aromatic monomer substituted with one or more alkyl groups.8. The polymerizable composition of claim 7 , wherein the polyvinyl aromatic monomer is divinylbenzene claim 7 , trivinylbenzene claim 7 , divinylbenzene substituted with one or more alkyl groups claim 7 , or trivinylbezene substituted with one or more alkyl groups.9. The polymerizable composition of claim 6 , further comprising up to 25 weight percent of a mono-vinyl aromatic monomer or a mono-vinyl aromatic monomer substituted with one or more alkyl groups.10. The polymerizable composition of claim 9 , wherein polymerizable composition comprises the 1 to 99 weight percent of a monomer of Formula (I) claim 9 , 0 to 25 weight percent of mono-vinyl aromatic monomer claim 9 , and 1 to 99 weight percent of a polyvinyl aromatic monomer claim 9 , wherein the weight percents are based on a total weight of monomers in the polymerizable composition.12. The polymer of claim 11 , wherein the polymerizable composition further comprises a polyvinyl aromatic monomer or a polyvinyl aromatic monomer substituted with one or more alkyl group.13. The polymer of or claim 11 , wherein the polymer is porous.14. The polymer of claim 13 , wherein the polymer is ...

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Номер записи: 85
30-10-2014 дата публикации

CALCIPOTRIOL MONOHYDRATE NANOCRYSTALS

Номер: US20140322331A1
Автор: Petersson Karsten
Принадлежит: LEO PHARMA A/S

Calcipotriol monohydrate nanocrystals prepared by the process disclosed herein may be incorporated in a pharmaceutical composition for use in the prevention or treatment of dermal diseases and conditions. 1. A suspension of calcipotriol monohydrate in the form of nanocrystals of a particle size distribution in the range of 200-600 nm as determined by dynamic light scattering , the suspension further comprising an aqueous phase including a non-ionic , polymeric surfactant in an amount sufficient to prevent formation of aggregates and/or crystal growth of the calcipotriol monohydrate nanocrystals.2. The suspension according to claim 1 , wherein the surfactant is selected from the group consisting of poloxamer or polysorbate surfactants claim 1 , and polyoxyethylene C-24 alkyl ether.3. The suspension according to claim 2 , wherein the poloxamer is selected from the group consisting of poloxamer 124 claim 2 , poloxamer 188 claim 2 , poloxamer 237 claim 2 , poloxamer 338 and poloxamer 407.4. The suspension according to claim 3 , wherein the surfactant is poloxamer 188.5. The suspension according to claim 2 , wherein the polysorbate is selected from the group consisting of polysorbate 20 claim 2 , polysorbate 40 claim 2 , polysorbate 60 claim 2 , polysorbate 61 claim 2 , polysorbate 80 and polysorbate 81.6. The suspension according to claim 2 , wherein the polyoxyethylene C24 alkyl ether is cetomacrogol 1000.7. The suspension according to claim 2 , wherein the amount of surfactant in said aqueous phase is in the range of from about 0.6% to about 1.2% by weight of the suspension.8. The suspension according to claim 1 , wherein the calcipotriol monohydrate nanocrystals have a mean particle size of 200-350 nm claim 1 , 350-400 nm or 400-500 nm as determined by dynamic light scattering.9. A process for preparing a suspension of calcipotriol monohydrate nanocrystals of a particle size distribution in the range of 200-600 nm as determined by dynamic light scattering claim 1 , ...

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Номер записи: 86
30-10-2014 дата публикации

Control and repellency of biting flies, house flies, ticks, ants, fleas, biting midges, cockroaches, spiders and stink bugs

Номер: US20140323561A1
Автор: BEDOUKIAN Robert H.
Принадлежит:

Control and repellency of biting flies, house flies, ticks, ants, fleas, biting midges, cockroaches, spiders and stink bugs is obtained by contact of the insects with at least one of the compounds of the structure (I). 2. The method according to wherein the compounds of structure (1) have from 12 to 16 carbon atoms in the compound.3. The method according to wherein the at least one compound of structure (I) is a compound wherein{'sub': 2', '2', '1', '2', '3', '1', '2', '3, 'R is selected from the group consisting of —OH and ═O, X is CH, y is 1 or 2, each Z is selected from the group consisting of (CH) and (CH), the bond between positions 2 and 3 in the ring is a single bond, one of Rand Ris H or —CHand the other of Rand Ris a hydrocarbyl group containing from 9 to 15 carbon atoms and 0 to 3 double bonds, and Ris H.'}4. The method of wherein the at least one compound of structure (I) is a compound wherein{'sub': 2', '2', '1', '2', '1', '2', '3', '5', '2', '8', '5', '8, 'R is selected from the group consisting of —OH and ═O, X is CH, y is 1 or 2, each Z is selected from (CH) and (CH), the bond between positions 2 and 3 in the ring is a single or double bond, one of Rand Ris H and the other of Rand Ris a hydrocarbyl group containing from 9 to 15 carbon atoms and 0 to 3 double bonds, and Ris selected from the group consisting of —C(O)ORand —CHC(O)Rwhere Rand Rare each selected from a hydrocarbyl group containing from 1 to 6 carbon atoms.'}5. The method according to wherein R is ═O claim 4 , y is 1 claim 4 , the bond between positions 2 and 3 in the ring is a single bond claim 4 , and Rand Rare each —CH.6. The method according to wherein the at least one compound of structure (I) is a compound wherein{'sub': 2', '1', '2', '1', '2', '3', '5', '2', '8', '5', '8, 'R is ═O, X is O, y is 1 or 2, each Z is selected from the group consisting of (CH) and (CH), the bond between positions 2 and 3 of the rings is a single or double bond, one of Rand Ris H and the other of Rand Ris ...

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Номер записи: 87
10-09-2015 дата публикации

NEW ALICYCLIC DIOL COMPOUND AND MANUFACTURING METHOD THEREOF

Номер: US20150251985A1
Автор: Kitamura Mitsuharu
Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

The alicyclic diol compound of the present invention is represented by the following formula (1). The present invention relates to a new alicyclic diol compound having a cyclohexane ring, and a manufacturing method thereof.A polyester resin synthesized from an alicyclic dicarboxylic acid and an alicyclic diol can be applied to use as optical materials, electronic information materials, and medical appliance materials, due to excellence in transparency, heat resistance, weather resistance, gas barrier property, and optical properties.For example, using 1,4-cyclohexane dicarboxylic acid (1,4-CHDA) as alicyclic dicarboxylic acid, and 1,4-cyclohexane dimethanol (1,4-CHDM) as alicyclic diol, a polyester resin excellent in biodegradability (refer to, for example, Patent Document 1), a conductive polyester emitting a less amount of gas (refer to, for example, Patent Document 2), and a polyester having a short foam-disappearing time, suitable for use in medical application (refer to, for example, Patent Document 3) are synthesized. Furthermore, using tricyclo[3.3.1.1]decane dicarboxylic acid as alicyclic dicarboxylic acid, and tricyclo[3.3.1.1]decane diol as alicyclic diol, a polyester resin having small optical anisotropy, excellent in moldability, is synthesized (refer to, for example, Patent Document 4).Japanese Patent Laid-Open No. 2000-290356Japanese Patent Laid-Open No. 2004-124022Japanese Patent Laid-Open No. 2005-298555Japanese Patent No. 3862538An object of the present invention is to provide a new alicyclic diol compound having a cyclohexane ring and a manufacturing method thereof.The present inventor has investigated a method of manufacturing a new alicyclic diol compound represented by the following formula (1) from 4-isopropenyl-1-methyl-1-cyclohexene represented by the following formula (4), and found out that the new alicyclic diol compound represented by the following formula (1) can be manufactured by, for example, reacting 4-isopropenyl-1-methyl-1- ...

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Номер записи: 88
01-08-2019 дата публикации

6-ISOPROPYL-2,4-DIMETHYLCYCLOHEXEN-1-OL COMPOUNDS AS FRAGRANCE INGREDIENTS

Номер: US20190233357A1
Автор: LOVCHIK Martin Alan, ZELENAY Veronika
Принадлежит:

The present invention refers to 6-isopropyl-2,4-dimethylcyclohexen-1-ol derivatives, to a method of their production, and fragrance compositions and fragranced articles comprising them. 2. The compound according to selected from 6-isopropyl-2 claim 1 ,4-dimethylcyclohex-3-en-1-ol claim 1 , 6-isopropyl-2 claim 1 ,4-dimethylcyclohex-4-en-1-ol claim 1 , and mixtures thereof.4. A fragranced article comprising as odorant a compound of formula (I) as defined in claim 1 , or a mixture thereof claim 1 , and a consumer product base.5. The fragranced article according to wherein the consumer product base is selected from fine perfumery claim 5 , household products claim 5 , laundry products claim 5 , fabric care products claim 5 , body care products claim 5 , cosmetic products and air care products.6. A method of improving claim 1 , enhancing or modifying a consumer product base comprising adding to the consumer product base an olfactory acceptable amount of a compound of formula (I) as defined in .7. A fragrance composition comprising a compound of formula (I) as defined in and at least one other compound selected from the group consisting of 2 claim 1 ,4 claim 1 ,7-trimethyloct-6-en-1-ol claim 1 , 2 claim 1 ,4 claim 1 ,7-trimethylocta-2 claim 1 ,6-dien-1-ol claim 1 , 2 claim 1 ,4 claim 1 ,7-trimethylocta-3 claim 1 ,6-dien-1-ol claim 1 , 2 claim 1 ,4 claim 1 ,7-trimethyloctan-1-ol claim 1 , and bis((3-methylbut-2-en-1-yl)oxy)methane.8. The fragrance composition according to wherein the compound of formula (I) is 6-isopropyl-2 claim 7 ,4-dimethylcyclohex-3-en-1-ol. The present invention relates to 6-isopropyl-2,4-dimethylcyclohexen-1-ol derivatives having green, very impactful odor notes, and to their use as flavor and fragrance ingredient and to compositions and products comprising them. It furthermore relates to a method of their production.Green odor characteristics are important scents in perfumery. Albeit a wide range of compounds possessing green odor notes are known, ...

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Номер записи: 89
01-09-2016 дата публикации

Neuroactive enantiomeric 15-, 16- and 17-substituted steroids as modulators for gaba type-a receptors

Номер: US20160251391A9
Автор: Douglas Covey
Принадлежит: Washington University in St Louis WUSTL

The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

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Номер записи: 90
31-08-2017 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20170247389A2
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., MacRury Thomas B., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (II): 3. The compound of wherein:{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 3', '8', '9', '11', '8', '9', '12', '8', '9', '9a', '8', '9', '9a', '8', '9', '9a, 'sub': 2', '2', '2, 'Ris —R—N(R)C(O)R, —R—N(R)—R, —R—N(R)C(═NCN)N(R), —R—N(R)C(O)N(R)or —R—N(R)C(S)N(R);'}{'sup': 4a', '4b, 'Rand Rare each independently hydrogen, alkyl, alkenyl or alkynyl;'}{'sup': 4a', '4b', '7, 'or Ris hydrogen, alkyl, alkenyl or alkynyl and Ris a direct bond to the carbon to which Ris attached;'}{'sup': 5', '5, 'Ris alkyl or Ris a direct bond to the carbon at C14;'}{'sup': 6', '8', '9', '8', '9, 'sub': '2', 'Ris hydrogen, —R—ORor —R—N(R);'}{'sup': 7', '8', '9', '8', '9', '7', '4b', '7, 'sub': '2', 'Ris hydrogen, —R—OR, —R—N(R), or a direct bond to C15, provided that when Ris a direct bond to C15, Ris not a direct bond to the carbon to which Ris attached;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain;'}{'sup': '9', 'each Ris hydrogen, alkyl, optionally substituted aryl and optionally substituted aralkyl;'}{'sup': '9a', 'each Ris hydrogen, alkyl, optionally substituted aryl, optionally substituted aralkyl; optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl;'}{'sup': '11', 'Ris optionally substituted heteroaryl; and'}{'sup': '12', 'Ris optionally substituted heterocyclyl.'}4. The compound of wherein:{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 3', '8', '9', '11', '8', '9', '12', '8', '9', '9a', '8', '9', '9a', '8', '9', '9a, 'sub': 2', '2', '2, 'Ris —R—N(R)C(O)R, —R—N(R)—R, —R—N(R)C(═NCN)N(R), —R—N(R)C(O)N(R)or —R—N(R)C(S)N(R);'}{'sup': 4a', '4b, 'Rand Rare each alkyl;'}{'sup': '5', 'Ris a direct bond to the carbon at C14;'}{'sup': '6', 'Ris hydrogen;'}{'sup': '7', 'Ris hydrogen;'}{'sup ...

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Номер записи: 91
08-08-2019 дата публикации

COMPOSITION FOR RESIST UNDERLAYER FILM FORMATION, RESIST UNDERLAYER FILM AND FORMING METHOD THEREOF, PRODUCTION METHOD OF PATTERNED SUBSTRATE, AND COMPOUND

Номер: US20190243247A1
Автор: Abe Tsubasa, MATSUMURA Yuushi, NAKAFUJI Shin-ya, NOSAKA Naoya, Sakai Kazunori, TAKIMOTO Yoshio, WAKAMATSU Goji
Принадлежит: JSR Corporation

A composition for resist underlayer film formation contains a compound having a group represented by formula (1), and a solvent. Rrepresents an organic group having 2 to 10 carbon atoms and having a valency of (m+n), wherein the carbon atoms include two carbon atoms that are adjacent to each other, with a hydroxy group or an alkoxy group bonding to one of the two carbon atoms, and with a hydrogen atom bonding to another of the two carbon atoms; Lrepresents an ethynediyl group or a substituted or unsubstituted ethenediyl group; Rrepresents a hydrogen atom or a monovalent organic group having 1 to 20 carbon atoms; n is an integer of 1 to 3; * denotes a bonding site to a moiety other than the group represented by the formula (1) in the compound; and m is an integer of 1 to 3. 2. The composition according to claim 1 , wherein a content of oxygen atoms in the compound is no less than 4% by mass.3. The composition according to claim 1 , wherein a hydrogen atom does not bond to the carbon atom to which the hydroxy group or the alkoxy group bonds in the organic group represented by Rin the formula (1).4. The composition according to claim 1 , wherein the compound comprises an aromatic ring.5. The composition according to claim 1 , further comprising an acid generating agent.7. The composition according to claim 1 , wherein a content of the compound in the composition is no less than 1% by mass and no greater than 50% by mass.8. A resist underlayer film formed from the composition according to .9. A method for resist underlayer film formation comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'applying the composition according to directly or indirectly on an upper face side of a substrate to form a coating film; and'}heating the coating film.10. A production method of a patterned substrate comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'forming a resist pattern directly or indirectly on an upper face side of the resist underlayer film obtained by the ...

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Номер записи: 92
07-09-2017 дата публикации

SYNTHESIS AND BIOLOGICAL ACTIVITY OF 2-METHYLENE ANALOGS OF CALCITRIOL AND RELATED COMPOUNDS

Номер: US20170253546A1
Автор: DeLuca Hector F., Plum Lori A., Sibilska Izabela K., Sicinski Rafal R.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Disclosed are 2-methylene analogs of vitamin Dand related compounds, their biological activities, and various pharmaceutical uses for these analogs. Particularly disclosed are 1α-hydroxy-2-methylene-vitamin D, (20S)-1α-hydroxy-2-methylene-vitamin D, and (5E)-1α,25-dihydroxy-2-methylene-vitamin D, their biological activities, and various pharmaceutical uses for these compounds including methods of treating and/or preventing bone diseases and disorders. 2. The compound of claim 1 , wherein Xand Xare t-butyldimethylsilyl.3. The compound of claim 1 , wherein Xand Xare hydrogen.6. A pharmaceutical composition containing an effective amount of the compound of and a pharmaceutically acceptable excipient.7. A method of treating or preventing a bone disease or disorder in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .8. (canceled)9. A method of treating or preventing a skin disease claim 1 , disorder claim 1 , or condition in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .10. A method of treating or preventing a cell proliferative disease or disorder in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .11. A method of treating or preventing obesity claim 1 , inhibiting adipocyte differentiation claim 1 , inhibiting SCD-1 gene transcription claim 1 , and/or reducing body fat in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .12. A method of treating secondary hyperparathyroidism of renal osteodystrophy in a patient in need thereof claim 1 , the method comprising administering to the patient an effective amount of the compound of .15. A pharmaceutical composition containing an effective amount of the compound of and a pharmaceutically acceptable excipient.16. A ...

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Номер записи: 93
07-10-2021 дата публикации

INHIBITION OF RESPIRATORY COMPLEX III BY LIGANDS THAT INTERACT WITH A REGULATORY SWITCH

Номер: US20210309617A1
Автор: Hagras Muhammad, Stuchebrukhov Alexei
Принадлежит: The Regents of the University of California

The present invention provides methods for inhibiting respiratory complex III in a cell. The present invention also provides methods for treating cancer in a subject. 14. The method of claim 1 , wherein the cell is a cancer cell.15. The method of claim 14 , wherein the cancer cell is in a subject.16. The method of claim 15 , further comprising administering to the subject an amount of the compound effective to inhibit respiratory complex III in the cancer cell. The present application is a division of U.S. application Ser. No. 16/531,511, filed Aug. 5, 2019, which is a continuation of International Patent Application No. PCT/US2018/017638, filed Feb. 9, 2018, which claims priority to U.S. Provisional Appln. No. 62/457,684, filed Feb. 10, 2017, the disclosures of which are herein incorporated by reference in their entirety for all purposes.This invention was made with Government support under Grant No. GM054052 awarded by the National Institutes of Health (NIH). The Government has certain rights in the invention.Ideally, a smart anti-cancer drug should discriminate between cancer and normal cells. One of the recently discovered biochemical variations in cancer cells that distinguish them from normal cells is a higher basal level of reactive oxygen species (ROS), which makes the cancer cells more susceptible to ROS-induced apoptosis (Szatrowski and Nathan (1991) 51:794; Kawanishi et al. (2006) 387:365; Toyokuni et al. (1995) 358:1; and Trachootham et al. (2009) 8:579). However, since cancer cells can adapt to such oxidative stress by up-regulating antioxidant production (Tiligada (2006) 13:S115), to make use of such a mechanism, a drug should induce rapid production and accumulation of ROS and trigger apoptosis in cancer cells before anti-oxidant up-regulation takes effect.The mitochondrial electron transport chain (METC) is one of the major sources of ROS in the cell (Adam-Vizi and Chinopoulos (2006) 27:639; and Lenaz (2001) 52:159), and respiratory complex III (also ...

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Номер записи: 94
15-08-2019 дата публикации

PROCESS FOR THE PREPARATION OF TREPROSTINIL

Номер: US20190248725A1
Автор: ALTSACH Tamás, BUZDER-LANTOS Péter, HAVASI Gábor, HORTOBÁGYI Irén, JUHÁSZ Imre, KARDOS Zsuzsanna, LÁSZLÓFI István, NAGYNÉ BORKÓ Ágnes, ROZSUMBERSZKI Imre
Принадлежит: CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT.

Treprostinil is a synthetic prostacyclin derivative with thrombocyte aggregation inhibitory and vasodilatory activity. Treprostinil can be administered in subcutaneous, intravenous, inhalable, or oral forms. Disclosed is a method for the preparation of treprostinil of formula I and its amorphous form, anhydrate form, monohydrate form, and polyhydrate form salts with bases. In the disclosed method, the chiral center in the 3-hydroxyoctyl substituent is formed at the end of the synthesis, so that the method is robust and well scalable. 2. Process as defined in for the preparation of the salts of treprostinil of formula I given with bases claim 1 , wherein as polar solvent Copen-chain or branched organic alcohol claim 1 , is applied.3. Process as defined in for the preparation of the salts of treprostinil of formula I given with bases claim 1 , wherein as for base claim 1 , the solventless organic or inorganic base which contains the cation of the desired salt is applied.4. Process as defined in for the preparation of the salts of treprostinil of formula I given with bases claim 3 , wherein as for base claim 3 , an organic or inorganic base containing alkali metal or alkali earth-metal cation is applied.5. Process as defined in for the preparation of the salts of treprostinil of formula I given with bases claim 4 , wherein as for base sodium carbonate monohydrate claim 4 , sodium hydrogen carbonate claim 4 , sodium methylate claim 4 , or sodium carbonate hydrate is applied.6. Process as defined in for the preparation of the salts of treprostinil of formula I given with bases claim 1 , wherein the reaction mixture is agitated in an inert atmosphere until salt formation proceeds.7. Process as defined in for the preparation of the salts of treprostinil of formula I given with bases claim 1 , wherein as the organic solvent of the crystallisation an ether claim 1 , ester claim 1 , or ketone solvent is applied.8. Process as defined in for the preparation of the salts of ...

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Номер записи: 95
27-11-2014 дата публикации

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR MODULATORS AND USES THEREOF IN REGULATING BLOOD GLUCOSE LEVELS

Номер: US20140350100A1
Автор: Chein Rong-Jie, KING Klim
Принадлежит:

The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sub': 'A', 'Gis hydrogen, ═O, ═S, —OR″, —SR″, —NR″H, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, a thiocarbamate group, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms, wherein each instance of R″ is independently hydrogen, a cyclic or acyclic, saturated or unsaturated, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 16 carbon atoms;'}{'sub': A1', 'A2', 'A3', 'A4', 'A5', 'A6', 'A7', 'A8', 'A9', 'A10, 'R, R, R, R, R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbons;'}{'sub': A11', 'A12', 'A13', 'A15', 'A16', 'A17, 'R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms;'}{'sub': 'A14', 'Ris halogen, —NR″H, —SR″, —OR″, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, or a thiocarbamate group;'}{'sub': 'A20', 'Ris hydrogen, halogen, or a cyclic or acyclic, substituted ...

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Номер записи: 96
22-09-2016 дата публикации

ANTHROPOD REPELLENT CHEMICALS

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

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

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Номер записи: 97
20-09-2018 дата публикации

COCRYSTALS OF NALOXONE AND NALTREXONE

Номер: US20180263973A1
Автор: BARBIER Remi, FRIEDMANN Nadav, SRIRAMBHATLA Vijay, WATT Stephen, Zamloot Michael
Принадлежит: Pain Therapeutics, Inc.

This invention relates to cocrystals of naloxone and of naltrexone and their use as opioid antagonists. The cocrystals of the invention include naloxone isonicotinamide cocrystal, naloxone hydrochloride piperazine cocrystal, naltrexone menthol cocrystal, naltrexone thymine cocrystal, naltrexone 2,5-dihydroxybenzoic acid cocrystal, naltrexone salicylic acid cocrystal, naltrexone hydrochloride piperazine cocrystal and naltrexone hydrochloride sulfathiazole cocrystal. A drug-in¬ adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a cocrystal of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof. Also disclosed is an improved transdermal patch for administering fentanyl or an analog thereof, or for administering a mu opioid agonist, the improvement wherein the transdermal patch contains a cocrystal of the invention in an abuse limiting amount. The improved transdermal patch may be a drug-in-adhesive transdermal patch or a reservoir transdermal patch. 1. A cocrystal of naloxone or a cocrystal of naltrexone selected from the group consisting of naloxone isonicotinamide cocrystal , naloxone hydrochloride piperazine cocrystal , naltrexone menthol cocrystal , naltrexone thymine cocrystal , naltrexone 2 ,5-dihydroxybenzoic acid cocrystal , naltrexone salicylic acid cocrystal , naltrexone hydrochloride piperazine cocrystal and naltrexone hydrochloride sulfathiazole cocrystal.2. A drug-in-adhesive transdermal patch comprising:a backing layer;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an adhesive layer disposed on the backing layer, the adhesive layer comprising a pressure sensitive adhesive, an opioid agonist, and a cocrystal of naloxone or a cocrystal of naltrexone according to or a mixture of the cocrystals; and'}a release layer disposed on the ...

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Номер записи: 98
29-09-2016 дата публикации

Block copolymer

Номер: US20160280832A1
Автор: Eun Young Choi, Je Gwon Lee, Jeong Kyu Lee, Jung Keun Kim, Mi Sook Lee, No Jin Park, Se Jin Ku, Sung Joon Oh, Sung Soo Yoon
Принадлежит: LG Chem Ltd

The present application provides the block copolymers and their application. The present application may provide the block copolymers that have excellent self assembling and phase separation properties and therefore that can be effectively used in various applications. The present application may also provide applications of the block copolymers.

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Номер записи: 99
29-09-2016 дата публикации

Block copolymer

Номер: US20160280835A1
Автор: Je Gwon Lee, Jeong Kyu Lee, Jung Keun Kim, Sung Joon Oh, Sung Soo Yoon, Yeon Joo Kang
Принадлежит: LG Chem Ltd

The present application provides the block copolymers and their application. The present application may provide the block copolymers that have excellent self assembling and phase separation properties and therefore that can be effectively used in various applications. The present application may also provide applications of the block copolymers.

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Номер записи: 100