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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 2988. Отображено 100.
21-03-2013 дата публикации

Method and Compounds for the Preparation of Monofluoromethylated Biologically Active Organic Compounds

Номер: US20130072698A1
Автор: Emilia Perpétua Tavares LEITÃO, William Heggie
Принадлежит: Hovione Inter AG

Described are processes for the preparation of monofluoromethylated organic biologically active compounds, such as Fluticasone Propionate and Fluticasone Furoate, in the presence of fluorodecarboxylating reagents such as XeF 2 and BrF 3 .

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Номер записи: 1
28-03-2013 дата публикации

NEURO-PROTECTIVE EFFECTS OF ADELOSTEMMA GRACILLIMUM AND ITS ISOLATED COMPOUNDS

Номер: US20130079293A1
Автор: Guo Shengjun, Ip Fanny Chui-Fun, Ip Nancy Yuk-Yu
Принадлежит: Biotechnology Research Corporation Limited

Isolated compounds from refined fractions and compositions containing the compounds are provided by the present invention. refined fractions and the extraction process thereof are also provided by the present invention. The uses of the compounds and the refined fractions for inhibiting the activities of NMDA receptor or amyloid-beta peptide, for improving memory, and for treating neurodegenerative diseases, neuropathological conditions or epilepsy are further provided by the present invention. 10. The compound of claim 9 , wherein Ris H.11. The compound of claim 9 , wherein{'sup': '1', 'Ris H;'}{'sup': 2', '3, 'each of Rand Rare Me; and'}subscript n is 10.1514. A pharmaceutical composition for treating a neurodegenerative disease or neuropathological condition in a subject claims 1 , the composition comprising a compound of any one of - and a pharmaceutically acceptable carrier or excipient.16Adelostemma gracillimum. A method of preparing a refined fraction claims 1 , the method comprising:{'i': 'Adelostemma gracillimum', 'contacting herb with an alcohol selected from the group consisting of methanol and ethanol, to form an alcohol extract;'}contacting the alcohol extract with an organic solvent to form an organic solvent fraction; and{'i': 'Adelostemma gracillimum', 'contacting the organic solvent fraction with a petroleum ether to form the refined fraction.'}17. The method of claim 16 , further comprising:{'i': 'Adelostemma gracillimum', 'eluting a first fraction of the refined fraction from a resin column with a solution of about 30% ethanol in water;'}eluting a second fraction from the resin column with a solution of about 60% ethanol in water; andeluting a third fraction from the resin column with a solution of about 96% ethanol in water.18Adelostemma gracillimum. An refined fraction prepared by the method of .19Adelostemma gracillimum. An refined fraction prepared by the method of .20Adelostemma gracillimum. A method of improving memory in a subject claim 17 , ...

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Номер записи: 2
09-05-2013 дата публикации

NOVEL POLY(ETHYLENE OXIDE)-BLOCK-POLY(ESTER) BLOCK COPOLYMERS

Номер: US20130116428A1
Автор: LAVASANIFAR Afsaneh, MAHMUD ABDULLAH
Принадлежит: THE GOVERNORS OF THE UNIVERSITY OF ALBERTA

The present invention relates to micelle-forming poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups on the polyester block therein. The biodegradability of these copolymers and their biocompatibilities with a large number of bioactive agents make them suitable as carriers for various bioactive agents. The bioactive agents, such as DNA, RNA, oligonucleotide, protein, peptide, drug and the like, can be coupled to the reactive groups on the polyester block of the copolymer. 125.-. (canceled)27. A compound of formula II as claimed in claim 26 , wherein V is 1 claim 26 , Lis —C(O)—O— and Ris benzyl.28. A compound of formula II as claimed in claim 26 , wherein V is 1 claim 26 , Lis —C(O)—O— and Ris α-cholestryl.29. A compound of formula II as claimed in claim 26 , wherein V is 1 claim 26 , Lis —C(O)—O— and Ris hydrogen.3031.-. (canceled) This application claims the benefit of U.S. provisional patent application No. 60/783,837, filed Mar. 21, 2006.The present invention relates to novel poly(ethylene oxide)-block-poly(ester) block copolymers, particularly poly(ethylene oxide)-block-poly(ester) block copolymers having reactive groups and/or bioactive compounds on the polyester block. The invention also relates to a composition and method of use thereof for delivering bioactive agents.Amphiphilic block copolymers can self-assemble to nanoscopic, core/shell structures in which the hydrophobic core acts as a microreservoir for the encapsulation of drugs, proteins or DNA; and the hydrophilic shell interfaces the media. Among different block copolymers designed for drug delivery, those with polyethylene oxide (PEO), as the shell-forming block, and polyester or poly amino acids (PLAA), as the core-forming block, are of increasing interest. This is owed to the biocompatibility of PEO and potential biodegradability of polyester and PLAA, which make them safe for human administration.It is generally known that poly amino acids (PLAA) structures are ...

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Номер записи: 3
16-05-2013 дата публикации

4-PREGENEN-11BETA-17-21-TRIOL-3,20-DIONE DERIVATIVES

Номер: US20130123223A1
Автор: Edelman Jeffrey L., Malone Thomas C., Nehme Alissar
Принадлежит: ALLERGAN, INC.

The present invention relates to novel 4-pregenen-11β-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation. 3. The compound according to wherein Ris substituted aryl.8. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.12. The method according to wherein the ocular condition is selected from the group consisting of elevated intraocular pressure claim 10 , glaucoma claim 10 , uveitis claim 10 , retinal vein occlusions claim 10 , macular degeneration claim 10 , diabetic retinopathy claim 10 , various forms of macular edema claim 10 , post-surgical inflammation claim 10 , inflammatory conditions of the palpebral and bulbar conjunctiva claim 10 , cornea claim 10 , and anterior segment of the globe claim 10 , such as allergic conjunctivitis claim 10 , ocular rosacea claim 10 , dry eye claim 10 , blepharitis claim 10 , retinal detachment claim 10 , meibomian gland dysfunction claim 10 , superficial punctate keratitis claim 10 , herpes zoster keratitis claim 10 , iritis claim 10 , cyclitis claim 10 , selected infective conjunctivitis claim 10 , corneal injury from chemical claim 10 , radiation claim 10 , or thermal burns claim 10 , penetration of foreign bodies claim 10 , allergy claim 10 , or combinations thereof.13. The method according to wherein the ocular condition is selected from:dry eye, blepharitis, ocular rosacea, meibomian gland dysfunction, uveitis and macular degeneration.14. The method according to wherein the ocular condition is selected from the group consisting of ...

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Номер записи: 4
16-05-2013 дата публикации

Pharamceutical compositions and methods of use 4-pregenen-11beta-17-21-triol-3,20-dione derivatives

Номер: US20130123226A1
Автор: Alissar Nehme, Jeffrey L. Edelman
Принадлежит: Allergan Inc

The present invention relates to pharmaceutical compositions comprising 4-pregenen-11β-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).

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Номер записи: 5
11-07-2013 дата публикации

GLYCOSIDE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20130178431A1
Автор: Hutchinson Charles R., Prudent James R., Shekhani Mohammed S.
Принадлежит:

The present invention provides glycoside compounds, methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and a method for the treatment of hyperproliferative diseases using the same. 15-. (canceled)6. A pharmaceutical composition comprising a compound and at least one pharmaceutically acceptable excipient.7. The pharmaceutical composition of wherein the at least one pharmaceutically acceptable excipient is a cyclodextrin.8. A method of treating a hyperproliferative disease in a subject in need thereof claim 17 , the method comprising administering to the subject a therapeutically effective amount of a compound of .9. A method of treating cancer in a subject in need thereof claim 6 , the method comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition of .1012-. (canceled)13. The method of wherein the cancer is selected from colorectal claim 9 , non-small cell claim 9 , lung claim 9 , ovarian claim 9 , breast claim 9 , colon claim 9 , CNS claim 9 , liver claim 9 , lung claim 9 , and kidney cancers.1416-. (canceled) Cardiac glycosides have been recognized as potential cancer drugs at least since 1999 (Haux, 53:543-8, 1999) and extensive studies of their cytotoxicity in human cancer cells were carried out as early as 2001 (Johansson, et al., 12:475-83, 2001). Interest in the mechanism of inhibition of the cardiac glycosides' target, the inotropic Na,K-ATPases found in the membranes of animal cells, has spawned a considerable body of work (Mijatovic, et al., 1776:32-57, 2007). Extensive medicinal chemistry research directed at finding more potent and less toxic cardiac glycosides through chemical modification of their steroid and sugar portions has also been conducted (Repke, K. R., et al., 30:135-202, 1993; Mudge, et al., 43:847-54, 1978; Repke, K. R. H., Drug Discovery Today. 2:110-16, 1997). Yet despite the synthesis of many different analogs (Repke, K. R., et al., 30:135-202, ...

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Номер записи: 6
18-07-2013 дата публикации

PROCESS FOR PREPARING DELTA-7,9(11) STEROIDS FROM GANODERMA LUCIDUM AND ANALOGS THEREOF

Номер: US20130184244A1
Автор: Kennedy Erin, Minto Robert
Принадлежит: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION

Processes for preparing lanostane triterpenes from the medicinal mushroom , and related compounds are described. Compounds, compositions, and methods for treating cancer are also described. 2. The process of wherein step (b) is performed by oxidative cleavage in the presence of ozone.3. The process of wherein the oxygen containing functional group is selected from the group consisting of hydroxy claim 1 , epoxy claim 1 , carbonyl claim 1 , carboxylic acid claim 1 , and derivatives of each of the foregoing.4. The process of wherein R is alkenyl.5. The process of wherein R is an aldehyde.6. The process of wherein R is an alpha/beta unsaturated carboxylic acid or derivative thereof.7. The process of wherein R is hydroxyalkenyl.8. The process of wherein R is polyhydroxyalkyl.9. The process of wherein one or both of Xand Xor Xand Xare taken together to form CH═C.10. The process of wherein Xand Xare taken together to form C═C.11. (canceled)12. The process of wherein one of Xand X claim 1 , Xand Xor Xand Xare taken together to form an epoxide.13. (canceled)15. The process of wherein Yand Yare taken together to form a ketal.16. (canceled)17. The process of wherein R is optionally substituted aminoalkenyl or optionally substituted aminoalkyl.18. (canceled)19. The process of wherein R is optionally substituted haloalkenyl or optionally substituted haloalkyl.20. (canceled)21. The process of wherein the compound is ganodermanontriol claim 1 , or a stereoisomer thereof.22. The process of wherein the compound is ganodermanontriol.24. The compound of wherein R is selected from the group consisting of alkenyl; aldehyde; an alpha/beta unsaturated carboxylic acid or derivative thereof; hydroxyalkenyl; polyhydroxyalky; optionally substituted aminoalkenyl; optionally substituted aminoalkyl; optionally substituted haloalkenyl; and optionally substituted haloalkyl.2533-. (canceled)34. The compound of wherein one or both of Xand Xor Xand Xare taken together to form CH═C.35. The compound ...

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Номер записи: 7
10-10-2013 дата публикации

AMPHIPHILIC COMPOUNDS

Номер: US20130266656A1
Автор: Chae Pil Seok, GELLMAN Samuel Helmer, Kobilka Brian, Rasmussen Søren
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Bringing membrane proteins into aqueous solution generally requires the use of detergents or other amphiphilic agents. The invention provides a new class of amphiphiles, each of which includes a multi-fused ring system as a lipophilic group. These new amphiphiles confer enhanced stability to a range of membrane proteins in solution relative to conventional detergents, leading to improved structural and functional stability of membrane proteins, including integral membrane proteins. Accordingly, the invention provides new amphiphiles for biochemical manipulations and characterization of membrane proteins. These amphiphiles display favorable behavior with membrane proteins and can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins. 2. The compound of wherein Ris methyl.3. The compound of wherein each Sac is an oxygen-linked monosaccharide.4. The compound of wherein each Sac is an oxygen-linked disaccharide.5. The compound of wherein each Sac is an oxygen-linked trisaccharide.6. The compound of wherein X is NH claim 1 , Y is O claim 1 , Z is H claim 1 , and L is a direct bond.7. The compound of wherein L is —CH— claim 1 , X is O claim 1 , Y is absent claim 1 , and Z is Me.8. The compound of wherein L is a direct bond claim 1 , X is a direct bond claim 1 , Y is absent claim 1 , and Z is H.12. The compound of wherein the optional double bond is present.13. The compound of wherein each Sac is an oxygen-linked monosaccharide.14. The compound of wherein each Sac is an oxygen-linked disaccharide.15. The compound of wherein each Sac is an oxygen-linked trisaccharide.16. The compound of wherein X is NH claim 11 , Y is O claim 11 , Z is H claim 11 , and L is a direct bond.17. The compound of wherein L is —CH— claim 11 , X is O claim 11 , Y is absent claim 11 , and Z is Me.18. The compound of wherein L is a direct bond claim 11 , X is a direct bond claim 11 , Y is absent claim 11 , and ...

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Номер записи: 8
02-01-2014 дата публикации

CONTRACEPTIVE AGENTS

Номер: US20140005132A1
Автор: Blanco Gustavo, Georg Gunda I., Syeda Shameem Sultana
Принадлежит:

The invention provides compounds of formula I, II, III, or IV: 2. The compound of claim 1 , which is a compound of formula (I).3. The compound of claim 1 , which is a compound of formula (II).4. The compound of claim 1 , which is a compound of formula (III).5. The compound of claim 1 , which is a compound of formula (IV).7. The compound of claim 1 , wherein Ris H.8. The compound of claim 1 , wherein Ris H or methoxymethyl.10. The compound of claim 1 , wherein Ris H or methoxymethyl.11. The compound of claim 1 , wherein Ris H.12. The compound of claim 1 , wherein Ris H.13. The compound of claim 1 , wherein Rand Rtaken together form —C(CH)—.16. The compound of claim 1 , wherein X is O.17. The compound of claim 1 , wherein X is ═N—N═C(NH).18. The compound of claim 1 , wherein Y is O.19. The compound of claim 1 , wherein Y is ═N—N═C(NH).20. The compound of claim 1 , wherein Ris —OH claim 1 , morpholino claim 1 , or —O—C(═O)CH(NH)R; and Ris 1-methylethyl or 4-aminobutyl.22. The compound of claim 1 , wherein the compound is not one of the compounds Compound 54 claim 1 , 12 claim 1 , 1 or 1a.23. A compound comprising:a chemical structure of one of Compounds 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 55, 56, 57a, 57b, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 77a, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, or 91.24. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound of formula I, II, III, or IV of , or a pharmaceutically acceptable salt thereof; and'}a pharmaceutically acceptable diluent or carrier having the compound.25. A method for decreasing sperm motility in a mammal comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering the compound of formula I, II, III, or IV of , or a pharmaceutically acceptable ...

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Номер записи: 9
06-02-2014 дата публикации

COMPOSITION FOR TOPICAL SKIN APPLICATION CONTAINING GINSENOSIDE F2 DERIVED FROM HYDROPONIC GINSENG

Номер: US20140039170A1
Автор: CHO Jun Cheol, Kim Dong Hyun, KIM Hyun Hee, LEE Ok Chan, RYU Kwon Real, Yeom Myeong Hun
Принадлежит: AMOREPACIFIC CORPORATION

Beneficial effects are obtained by topically applying ginsenoside F2 to the skin to improve skin conditions, improve water content on the skin surface and related benefits improving skin problems associated with acne or atopy, providing a skin whitening effect, helping control of sebaceous secretion, tightening skin pores, or improving skin complexion through enhanced blood circulation, but also to improve scalp and hair conditions, such as providing an anti-dandruff effect, promoting hair growth, or preventing generation of grey hair. 2. The composition for topical skin application as claimed in claim 1 , wherein the roots and leaves of clean fresh ginseng are produced by a method using an aggregate hydroponic ginseng cultivation system comprising:a) performing a first acclimatization step of storing a ginseng seedling in a storage greenhouse at 15° C. for one or two days after a release and then tentatively planting the ginseng seedling;b) performing a second acclimatization step of storing the tentatively planted ginseng seedling in a greenhouse for one or two days to have the ginseng seedling acclimatized in the environment of the greenhouse and then finally planting the ginseng seedling in a mixed medium formed in a bed with a drainage groove;c) preparing a nutrient solution;d) supplying an appropriate amount of the nutrient solution for the ginseng seedling; ande) harvesting after 4 to 5 months.3. The composition for topical skin application as claimed in claim 1 , wherein the roots and leaves of clean fresh ginseng are produced by a method using an aeroponic ginseng cultivation system comprising:a) performing a first acclimatization step of storing a ginseng seedling in a storage greenhouse at 15° C. for one or two days after a release and then tentatively planting the ginseng seedling;b) performing a second acclimatization step of storing the tentatively planted ginseng seedling in a greenhouse for one or two days to have the ginseng seedling acclimatized in ...

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Номер записи: 10
27-02-2014 дата публикации

Aldosterone induced vascular elastin production

Номер: US20140056916A1
Автор: Aleksander Hinek, Thomas F. Mitts
Принадлежит: Hospital for Sick Children HSC, Human Matrix Sciences LLC

Compositions and methods for inducing the deposition of elastin by administering compositions including a mineralocorticoid, such as, for example, aldosterone and, optionally, a secondary active agent for enhancing or modulating the effect of the mineralocorticoid are described herein.

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Номер записи: 11
27-02-2014 дата публикации

USE OF 3,8,12,14, 17,20-OXO-SUBSTITUTED PREGNENE GLYCOSIDES IN THE PREPARATION OF HEALTHCARE PRODUCTS, FOOD ADDITIVES AND PHARMACEUTICALS FOR THE INHIBITION OF APPETITE

Номер: US20140058074A1
Автор: Chen Zhenhua, Liu Shuangzhu, Wang Luoyi, Zhao Weimin
Принадлежит: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

The present invention relates to the use of 3,8,12,14,17,20-oxo-substituted pregnene glycosides having the following formula I in the preparation of healthcare products, food additives and drugs for losing body weight, controlling body weight and inhibiting appetite of human beings or animals, wherein, Ris a saccharide group, and Ris an acyl group. 2. The use according to claim 1 , wherein claim 1 , in formula I claim 1 , the saccharide group is consisted of one or more sugar moieties selected from glucose claim 1 , cymarose claim 1 , diginose claim 1 , mannose claim 1 , xylose claim 1 , rhamnose claim 1 , arabinose claim 1 , and glucuronic acid; and the acyl group is selected from acetyl claim 1 , cinnamoyl claim 1 , 3 claim 1 ,4-dimethyl-2-amylene acyl claim 1 , nicotinoyl claim 1 , and benzoyl.4. A composition in the preparation of healthcare products claim 1 , food additives and pharmaceuticals for losing body weight claim 1 , controlling body weight and inhibiting appetite of human beings or animals claim 1 , wherein claim 1 , the composition contains 3 claim 1 ,8 claim 1 ,12 claim 1 ,14 claim 1 ,17 claim 1 ,20-oxo-substituted pregnene glycosides according to . The present invention relates to the use of natural 3,8,12,14,17,20-oxo-substituted pregnene glycosides for the inhibition of appetite. In particular, the present invention relates to the use of 3,8,12,14,17,20-oxo-substituted pregnene glycosides in the development of healthcare products, food additives and pharmaceuticals for reducing or controlling body weight and inhibiting appetite of human beings or animals, wherein, the 3,8,12,14,17,20-oxo-substituted pregnene glycosides are separated from medicinal and/or edible plant species.Obesity means that the adipose tissue in human body is too much for various reasons and goes beyond the average level of normal human being. Obesity may affect the health of organism and is an important factor inducing serious diseases and death. In the whole world, there are ...

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Номер записи: 12
27-02-2014 дата публикации

Derivatives of allopregnanolone and of epiallopregnanolone and uses thereof for treating a neuropathological condition

Номер: US20140058079A1
Автор: Ayikoe Guy Mensah-Nyagan, Blandine Ressault, Christine Patte-Mensah, Laurence Meyer, Michel Miesch, Omar Taleb, Philippe Geoffroy
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite De Strasbourg

The présent invention relates to novel neurosteroids, especially derivatives of allopregnanolone and of epiallopregnanolone of formula (I) and the uses thereof as médicament for the treatment of neuropathologies, in particular neuropathies induced by the chemotherapy of a cancer. Thèse molécules according to the invention have both preventative and curative effects. The neurosteroids according to the invention may also be of use in the treatment of neurodegenerative disorders, in particular for preventing neuronal cell death. They may thus be used as neuroprotectants and/or as an agent that stimulâtes neuronal prolifération.

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Номер записи: 13
06-03-2014 дата публикации

STEROID COMPOUNDS AS RORyt MODULATORS AND USES THEREOF

Номер: US20140066391A1
Автор: Gin David Y., Huh Jun R., Krout Michael R., Littman Dan R., Manel Nicolas Gabriel Albert, Ryan Daniel A.
Принадлежит:

Steroid compounds are disclosed that have a formula represented by the following: 2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)18. (canceled)20. (canceled)21. (canceled)24. (canceled)25. (canceled)26. (canceled)30. (canceled)31. The method according to claim 29 , wherein Ris alkyl claim 29 , unsubstituted claim 29 , or substituted with halo claim 29 , phenyl claim 29 , hydroxyl or methoxy claim 29 ,alkenyl, unsubstituted, or substituted with alkyl, or phenyl;cycloalkyl, unsubstituted, or substituted with hydroxyl or methoxy; oraryl, unsubstituted, or substituted with substituted or unsubstituted alkyl, substituted or unsubstituted acyl, substituted or unsubstituted acylamino, substituted or unsubstituted alkylamino, substituted or unsubstituted alkylthio, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted alkylarylamino, substituted or unsubstituted amino, substituted or unsubstituted arylalkyl, sulfo, substituted sulfo, substituted sulfonyl, substituted sulfinyl, substituted sulfanyl, substituted or unsubstituted amino sulfonyl, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted arylsulfonyl, azido, substituted or unsubstituted carbamoyl, carboxyl, cyano, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted dialkylamino, halo, nitro, and thiol.32. The method according to claim 29 , wherein Ris H.34. (canceled)35. (canceled)37. (canceled)38. (canceled)39. (canceled)40. The method according claim 35 , wherein z is 1 or 2; and each Ris independently selected from F claim 35 , Br claim 35 , Cl claim 35 , I claim 35 , OH claim 35 , Me claim 35 , Et claim 35 , CF claim 35 , OCF claim 35 , CF claim 35 , NMe claim 35 , OMe claim 35 , OEt claim 35 , NO claim 35 , OPh claim 35 , and SMe.41. (canceled)42. The ...

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Номер записи: 14
27-03-2014 дата публикации

COMPOSITIONS AND METHODS FOR INCREASING TELOMERASE ACTIVITY

Номер: US20140088055A1
Автор: FAUCE Steven, HARLEY Calvin Bruce, KHOR Soo-Peang, LIN Tong, PIROT Zhu Z., RAMASESHAN Mahesh, RAMIYA Premchandran H.
Принадлежит: TELOMERASE ACTIVATION SCIENCES, INC.

The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells. 7. The compound of claim 1 , wherein Xor Xis —OC(O)CH(NH)CH(CH)CHCH.8. The compound of claim 1 , wherein both Xand Xare —OC(O)CH(NH)CH(CH)CHCH.10. The compound of claim 1 , wherein Xis a —OC(O)CH(NH)CH(CH)and Xand Xare OH.11. The compound of claim 1 , wherein Xis —OC(O)CH(NH)CH(CH)CHCHand Xand Xare —OH.12. The compound of claim 1 , wherein Xis —OC(O)CH(NH)CH(CH)and Xand Xare OH.13. The compound of claim 1 , wherein Xis —OC(O)CH(NH)CH(CH)CHCHand Xand Xare OH.15. The compound of wherein the pharmaceutically acceptable salt is hydrochloride salt.16. A compound selected from the group consisting of:2-(L)-amino-3-methyl-butyric acid 6α,16β-dihydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester;2-(L)-amino-3-methyl-butyric acid 6α-(2-amino-3-methyl-butyryloxy)-16β-hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester;2-(L)-tert-butoxycarbonylamino-3-methyl-butyric acid 3b-acetoxy-16b-hydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-6a-yl ester;2-(L),3-dimethyl-pentanoic acid 6α,16β-dihydroxy-17-[5-(1-hydroxy-1-methyl-ethyl)-2-methyl-tetrahydro-furan-2-yl]-4,4,13,14-tetramethyl-tetradecahydro-cyclopropa[9,10]cyclopenta[a]phenanthren-3β-yl ester,2-(L)-Amino-3-methyl-butyric acid, 16β- ...

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Номер записи: 15
03-01-2019 дата публикации

DERIVATIVES OF ALLOPREGNANOLONE AND OF EPIALLOPREGNANOLONE AND USES THEREOF FOR TREATING A NEUROPATHOLOGICAL CONDITION

Номер: US20190002492A1
Автор: Geoffroy Philippe, Mensah-Nyagan Ayikoe Guy, Meyer Laurence, Miesch Michel, Patte-Mensah Christine, Ressault Blandine, Taleb Omar
Принадлежит:

The present invention relates to novel neurosteroids, especially derivatives of allopregnanolone and of epiallopregnanolone of formula (I) and the uses thereof as medicament for the treatment of neuropathologies, in particular neuropathies induced by the chemotherapy of a cancer. These molecules according to the invention have both preventative and curative effects. The neurosteroids according to the invention may also be of use in the treatment of neurodegenerative disorders, in particular for preventing neuronal cell death. They may thus be used as neuroprotectants and/or as an agent that stimulates neuronal proliferation. 2. The derivative according to claim 1 , wherein{'sup': '1', 'Ris a group chosen among the 3-alpha or 3-beta O-allyl groups, the 3-alpha or 3-beta O-propargyl groups, the 3-alpha or 3-beta O-glycol groups, the 3-alpha or 3-beta O-PEG groups, the 3-alpha or 3-beta O-glycol-allyl groups and 3-alpha or 3-beta O-PEG-allyl groups,'}A is a carbon atom substituted by an atom chosen among 5-H alpha and 5-H beta and B is a methylene group; orA and B are carbon atoms forming a 5,6-double bond;C is a carbon atom substituted by an atom chosen among 14-H alpha, 14-H beta, 14-alpha OH and 14-beta OH and D is a methylene group; orC and D are carbon atoms forming a 14,15-double bond;{'sup': 2', '2', '2, 'F is a carbon atom substituted by an atom chosen among 17-H alpha and 17-H beta, and E is a methylene group or a carbon atom substituted by a group chosen among 16-alkyl-alpha, 16-alkyl-beta, 16-OR-alpha and 16-OR-beta, with Ra group chosen among allyl, propargyl, glycol, PEG, glycol-allyl, PEG-allyl, or'}{'sup': 2', '2', '2', '2', '2', '2, 'F is a carbon atom substituted by a group chosen among 17-alkyl-alpha, 17-alkyl-beta, 17-OR-alpha and 17-OR-beta, with Ra group chosen among allyl, propargyl, glycol, PEG, glycol-allyl, PEG-allyl, and E is a methylene group or a carbon atom substituted by a group chosen among 16-alkyl-alpha, 16-alkyl-beta, 16-OR-alpha and ...

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Номер записи: 16
07-01-2021 дата публикации

INHIBITORS OF GLUCOCORTICOID RECEPTOR

Номер: US20210002324A1
Автор: BALBAS Minna Delarae, Du Xiaohui, EKSTEROWICZ John, FANTIN Valeria R., McGee Lawrence R., MEDINA Julio C., REW Yosup, SUN Daqing, YAN Xuelei, ZHOU Haiying, ZHU Liusheng
Принадлежит:

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism. 2. The compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , hydroxy claim 1 , halo claim 1 , carbocyclyl claim 1 , or heteroalkyl.3. The compound of either of or or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris Calkyl or hydrogen.4. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris methyl.5. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris methyl and Rand Rare H.6. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris H.7. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein R claim 1 , R claim 1 , and Rare H.8. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein ring A is monocyclic heteroaryl or monocyclic aryl.9. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein ring A is phenyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , or pyridazinyl.10. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or ...

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Номер записи: 17
20-01-2022 дата публикации

MOGROSIDE COMPOUNDS AND USES THEREOF

Номер: US20220017564A1
Автор: GAN Xian-Wen, YIN Dan-Ting
Принадлежит: FIRMENICH SA

The present disclosure generally relates to various formulations and uses of the compound Isomogroside IV. In some aspects, the disclosure provides compositions that include Isomogroside IV. In some embodiments, the compositions are comestible compositions, including, but not limited to, packaged food and beverage products and tabletop sweeteners. In some aspects, the disclosure provides certain compositions that include such mogroside compounds, such as compositions that include such mogroside compounds and one or more other sweeteners. In some other aspects, the disclosure provides methods of reducing the caloric content of a sweetened article, such as a sweetened food or beverage product. 2. A method of sweetening or enhancing a sweet taste of a comestible composition claim 1 , the method comprising introducing a mogroside compound of to a comestible composition.3. The method of claim 2 , wherein the mogroside compound is present in the comestible composition at a concentration ranging from 1 ppm to 1000 ppm.4. The method of claim 2 , wherein the comestible composition comprises one or more additional sweeteners.5. The method of claim 4 , wherein the one or more additional sweeteners are selected from the group consisting of: sucrose claim 4 , fructose claim 4 , glucose claim 4 , allulose claim 4 , sugar alcohols (such as xylitol and erythritol) claim 4 , sucralose claim 4 , aspartame claim 4 , acesulfame potassium claim 4 , cyclamate claim 4 , steviol glycosides (such as rebaudioside A claim 4 , rebaudioside D claim 4 , rebaudioside E claim 4 , and rebaudioside M) claim 4 , other mogrosides (such as mogroside III claim 4 , mogroside IV claim 4 , mogroside V claim 4 , siamenoside I claim 4 , isomogroside V claim 4 , mogroside IV claim 4 , isomogroside IV claim 4 , mogroside III claim 4 , 11-oxomogroside V claim 4 , and 1 claim 4 ,6-α isomer of siamenoside I) claim 4 , and any combinations thereof.6. The method of claim 2 , wherein the comestible composition ...

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Номер записи: 18
14-01-2021 дата публикации

METHODS AND SYSTEM FOR STIMULATING ROOT EXUDATION IN PLANTS

Номер: US20210007363A1
Автор: Aharoni Asaph, KORENBLUM Elisa
Принадлежит:

Provided is a plant exudate, methods for obtaining a plant exudate by inducing the plant to secrete an exudate and systems for the collection of a plant exudate which include: one or more plant container including at least two discrete compartments each configured to accommodate a split root of a plant, the compartments being a root stimulating compartment including one or more input being in fluid communication with at least a source of a plant root stimulant, and a root exudate harvesting compartment, and a root exudate collection compartment in fluid communication with the root exudate harvesting compartment. 1. A method for obtaining an exudate from a plant root of a plant , the method comprising: providing a plant; splitting a root of the plant into at least two root moieties; placing each root moiety of the plant into a separate container or compartment; stimulating a first root moiety of the plant or an aerial portion of the plant with a stimulant to induce exudation or secretion of an exudate by the first root moiety or by the second root moiety of the plant into the container or compartment of the first root moiety or the second root moiety; and harvesting the exudate from the container or compartment wherein said exudate comprises a metabolite of interest or an intermediate thereof.2. The method of claim 1 , wherein said plant is a member of the Cannabaceae family and said metabolite of interest comprises a cannabinoid claim 1 , a terpenoid claim 1 , or a combination thereof.3. (canceled)4. The method of claim 1 , wherein the concentration of said metabolite of interest claim 1 , is at least 2 times greater than the concentration of said metabolite of interest extracted from an exudate of an analogous root moiety of a non-induced plant of the same species.5. (canceled)6. The method of claim 1 , wherein said obtaining said exudate is obtaining a composition comprising at least 30% w/w exudate.7. The method of claim 1 , wherein said obtaining an exudate is ...

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Номер записи: 19
27-01-2022 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20220024968A1
Автор: Griffin Andrew, Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R, R, R, R, R, R, and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 140-. (canceled)4243-. (canceled)44. The pharmaceutical composition of claim 41 , wherein Ris substituted or unsubstituted C-Calkyl.45. The pharmaceutical composition of claim 41 , wherein Ris —CH claim 41 , —CF claim 41 , —CHCH claim 41 , or —CHOR claim 41 , wherein Ris substituted or unsubstituted C-Calkyl.4647-. (canceled)48. The pharmaceutical composition of claim 41 , wherein each of Rand Ris independently hydrogen or substituted or unsubstituted alkyl.49. (canceled)50. The pharmaceutical composition of claim 41 , wherein each of Rand Ris independently hydrogen claim 41 , —CF claim 41 , or —CH.51. (canceled)52. The pharmaceutical composition of claim 41 , wherein Rand R claim 41 , together with the carbon atom to which they are attached form an oxo group.5354-. (canceled)55. The pharmaceutical composition of claim 41 , wherein Rand Rare hydrogen.56. The pharmaceutical composition of claim 41 , wherein Ris substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl and Ris hydrogen.57. The pharmaceutical composition of claim 41 , wherein Ris substituted or unsubstituted carbocyclyl or substituted or unsubstituted heterocyclyl and Ris hydrogen.5859-. (canceled)6193-. (canceled)95. The pharmaceutical composition of claim 94 , wherein Ris substituted or unsubstituted C-Calkyl.96. The pharmaceutical composition of claim 94 , wherein Ris —CH claim 94 , —CF claim 94 , —CHCH claim 94 , or —CHOR claim 94 , wherein Ris substituted or unsubstituted C-Calkyl.97. The pharmaceutical composition of claim 94 , wherein each of Rand Ris independently hydrogen or substituted or unsubstituted alkyl.98. The pharmaceutical composition of claim 94 , wherein each ...

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Номер записи: 20
16-01-2020 дата публикации

19-NOR C3, 3-DISUBSTITUTED C21-C-BOUND HETEROARYL STEROIDS AND METHODS OF USE THEREOF

Номер: US20200016178A1
Автор: Beresis Richard Thomas, Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): 127-. (canceled)30. The method of claim 28 , wherein Ris —CH claim 28 , —CHCH claim 28 , —CHF claim 28 , —CHF claim 28 , —CF claim 28 , —CHOCH claim 28 , or substituted or unsubstituted cyclopropyl.31. The method of claim 30 , wherein Ris —CH.32. The method of claim 28 , wherein Ris hydrogen.33. The method of claim 28 , wherein Rand Rare both hydrogen.34. The method of claim 28 , wherein represents a single bond claim 28 , and both of Rand Rare hydrogen.35. The method of claim 28 , wherein represents a single bond claim 28 , and both of Rand Rare fluoro.36. The method of claim 28 , wherein at least one of R claim 28 , R claim 28 , R claim 28 , R claim 28 , and Ris substituted or unsubstituted Calkyl claim 28 , —COR claim 28 , —C(═O)R claim 28 , —CN claim 28 , —NO claim 28 , or halogen claim 28 , wherein Ris substituted or unsubstituted Calkyl.37. The method of claim 36 , wherein at least one of R claim 36 , R claim 36 , R claim 36 , R claim 36 , and Ris substituted or unsubstituted —CH.38. The method of claim 28 , wherein R claim 28 , R claim 28 , R claim 28 , R claim 28 , and Rare hydrogen.42. The method of claim 28 , wherein the human subject has a CNS-related disorder.43. The method of claim 42 , wherein the CNS-related disorder is a sleep disorder claim 42 , a mood disorder claim 42 , a schizophrenia spectrum disorder claim 42 , a convulsive disorder claim 42 , a disorder of memory and/or cognition claim 42 , a movement disorder claim 42 , a personality disorder claim 42 , autism spectrum disorder claim 42 , pain claim 42 , traumatic brain injury claim 42 , a vascular disease claim 42 , a substance abuse disorder and/or withdrawal syndrome claim 42 , or tinnitus.44. The method of claim 43 , wherein the mood disorder is depression.45. The method of claim 44 , wherein the depression is postnatal depression.46. The method of claim 43 , wherein the sleep disorder is insomnia.47. The method of ...

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Номер записи: 21
16-01-2020 дата публикации

EXTRACTION OF CANNABINOIDS, CURCUMINOIDS AND GINSENOSIDES

Номер: US20200016508A1
Автор: Hari V., Stockwell John
Принадлежит:

An example method for extracting phytochemical oil from plant parts includes freezing plant parts from at least one of Cannabis sativa, Curcuma longa, Panax ginseng, and Panax quinquefolius. The frozen plant parts are reduced to a plant powder, which is suspended in an aqueous buffer. The aqueous buffer containing the suspended plant powder is incubated with at least one pectinase and at least one cellulose. An aqueous phase of the incubated aqueous buffer is evaporated through steam heating to obtain a steam dried product. Phytochemical oil, which includes at least one of cannabinoids, curcuminoids, and ginsenosides, is extracted from the steam dried product. 1. A method for extracting phytochemical oil from plant parts , comprising:freezing plant parts from at least one of Cannabis sativa, Curcuma longa, Panax ginseng, and Panax quinquefolius;reducing the frozen plant parts to a plant powder;suspending the plant powder in an aqueous buffer;incubating the aqueous buffer containing the suspended plant powder with at least one pectinase and at least one cellulase;evaporating an aqueous phase of the incubated aqueous buffer through steam heating to obtain a steam dried product; andextracting phytochemical oil from the steam dried product, the phytochemical oil including at least one of cannabinoids, curcuminoids, and ginsenosides.2. The method of claim 1 , comprising claim 1 , prior to said freezing:sanitizing the plant parts, the sanitizing including at least one of washing, ultraviolet irradiation, and ozonolysis.3. The method of claim 2 , wherein said washing and disinfecting removes microorganisms from the plant parts.4. The method of claim 3 , wherein said reducing the frozen plant parts to a plant powder comprises pulverizing the frozen plant parts.5. The method of claim 1 , wherein:said freezing comprises cooling the plant parts with dry ice; andsaid reducing is performed while the plant parts are being cooled by the dry ice.6. The method of claim 1 , wherein ...

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Номер записи: 22
16-01-2020 дата публикации

Novel Triterpene-Glycoside as Sweetener or Sweetener Enhancer

Номер: US20200017541A1
Автор: Fotini TSCHIRINTZI, Gregor HETTERLING, Grit KLUGE, Karsten Siems, Sven Jakupovic
Принадлежит: ANALYTICON DISCOVERY GMBH

What claimed is a method of sweetening or enhancing sweetening effect of a composition that is administered orally to an individual by adding a specific triterpene glycoside obtained from Momordica grosvenorii ( Siraitia grosvenori ).

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Номер записи: 23
21-01-2021 дата публикации

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Номер: US20210017218A1
Автор: Beresis Richard Thomas, Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R, R, R, R, R, R, R, R, Rand are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e. g., such for inducing sedation and/or anesthesia. 164-. (canceled)74. The method of claim 66 , wherein A is a 5-10-membered ring.75. The compound of claim 74 , wherein A is phenyl claim 74 , naphthyl claim 74 , furan claim 74 , thiophene claim 74 , thiazole claim 74 , pyrrole claim 74 , imidazole claim 74 , pyrazole claim 74 , or triazole.77. The method of claim 65 , wherein the CNS-related disorder is a sleep disorder claim 65 , a mood disorder claim 65 , a schizophrenia spectrum disorder claim 65 , a convulsive disorder claim 65 , a disorder of memory claim 65 , a disorder of cognition claim 65 , a movement disorder claim 65 , a personality disorder claim 65 , autism spectrum disorder claim 65 , pain claim 65 , traumatic brain injury claim 65 , a vascular disease claim 65 , a substance abuse disorder claim 65 , a substance abuse withdrawal syndrome claim 65 , a neurodegenerative disorder claim 65 , or tinnitus.78. The method of claim 77 , wherein the CNS-related disorder is tremor.79. The method of claim 78 , wherein the tremor is essential tremor.80. The method of claim 66 , wherein the CNS-related disorder is a sleep disorder claim 66 , a mood disorder claim 66 , a schizophrenia spectrum disorder claim 66 , a convulsive disorder claim 66 , a disorder of memory claim 66 , a disorder of cognition claim 66 , a movement disorder claim 66 , a personality disorder claim 66 , autism spectrum disorder claim 66 , pain claim 66 , traumatic brain injury claim 66 , a vascular disease claim 66 , a substance abuse disorder claim 66 , a substance abuse withdrawal syndrome claim ...

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Номер записи: 24
21-01-2021 дата публикации

INHIBITORS OF GLUCOCORTICOID RECEPTOR

Номер: US20210017219A1
Автор: BALBAS Minna Delarae, Du Xiaohui, EKSTEROWICZ John, FANTIN Valeria R., McGee Lawrence R., MEDINA Julio C., REW Yosup, SUN Daqing, YAN Xuelei, ZHOU Haiying, ZHU Liusheng
Принадлежит:

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer. 2. The compound of or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein R is hydrogen claim 1 , alkyl claim 1 , haloalkyl claim 1 , hydroxy claim 1 , halo claim 1 , carbocyclyl claim 1 , or heteroalkyl.3. The compound of or or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris Calkyl or hydrogen.4. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris methyl.5. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris H.6. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein ring A is monocyclic heteroaryl or monocyclic aryl.7. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein ring A is phenyl claim 1 , pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , or pyridazinyl.8. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein ring A is phenyl.9. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris Calkyl.10. The compound of any one of - or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Ris Calkyl.11. The compound of any ...

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Номер записи: 25
17-04-2014 дата публикации

System and Method for Diagnosis and Treatment

Номер: US20140107086A1
Автор: Myron Rapkin, Neil David THEISE, Randice Lisa Altschul, Rebecca O'brien
Принадлежит: POP TEST CORTISOL LLC

This invention relates to a low cost rapid response diagnostic system to determine cortisol levels in patients selected as potential candidates for GCR (glucocorticoid receptor) antagonist therapy utilizing a GCR antagonist, such as ORG 34517. The rapid, sensitive, and inexpensive test can be used to determine patients who have non-normal cortisol production or disordered circadian rhythms as a method for selecting subjects for GCR antagonist therapy for whom it is likely to have beneficial and/or therapeutic effects, and can also be used to monitor changes in cortisol levels in response to treatment.

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Номер записи: 26
28-01-2021 дата публикации

HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF

Номер: US20210024572A1
Автор: DUGAR Sundeep, Mahajan Dinesh, SCHREINER George Frederic
Принадлежит:

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. 4. (canceled)5. The compound of claim 3 , wherein the compound is selected from the group consisting of:xiii. (10R,11S,13S,17S)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid;xiv. (10R,11S,13S,17S)-11-hydroxy-N,N,10,13-tetramethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxamide;xv. (10R,11S,13S,17S)-17-acetyl-1-hydroxy-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;xvi. (10R,11S,13S,17S)-11-hydroxy-17-((R)-1-hydroxyethyl)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;xxxiii. (10R,11S,13S,17S)-11,17-dihydroxy-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;xxxiv. (10R,11S,13S)-11-hydroxy-10,13-dimethyl-7,8,9,10,11,12,13,14,15,16-decahydro-3H-cyclopenta[a]phenanthrene-3,17(6H)-dione;xli. (10R,11S,13S,17S)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxamide;xlii. (10R,11S,13S,17S)-11-hydroxy-17-(hydroxymethyl)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;xliii. (10R,11S,13S,17S)-17-((dimethylamino)methyl)-11-hydroxy-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;lvi. (8S,9S,10R,11S,13S,14S,Z)-11-hydroxy-17-(hydroxyimino)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;lvii. (8S,9S,10R,11S,13S,14S)-17-amino-11-hydroxy-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one;lviii. (8S,9S,10R,11S,13S,14S)-11-hydroxy-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one; andlix. (8S,9S, ...

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Номер записи: 27
02-02-2017 дата публикации

NOVEL TRITERPENE-GLYCOSIDES AS SWEETENERS OR SWEETENER ENHANCERS

Номер: US20170029458A1
Автор: Hetterling Gregor, Jakupovic Sven, Kluge Grit, Siems Karsten, Tschirintzi Fotini
Принадлежит: ANALYTICON DISCOVERY GMBH

Suggested are triterpene-glycoside compounds, which are obtainable by the extraction of () which are useful as a sweetener or sweetener enhancer in preparations and compositions, especially oral edible compositions. 2. A compound of formula (I) according to claim 1 , wherein{'sub': 1', '2, 'Rand Rare independently of one another and denote hydroxyl or a sugar moiety selected from the group consisting of a monosaccharide, an oligosaccharide and mixtures thereof,'}wherein the monosaccharide and/or the monosaccharide units of the oligosaccharide are selected from the group consisting of glucose, 2-glucopyranosyl-glucose, 3-glucopyranosyl-glucose, 4-glucopyranosyl-glucose, 6-glucopyranosyl-glucose, glucopyranosyl-(1→2)-[glucopyranosyl-(1→6)]-glucose and mixtures thereof, and{'sub': '3', 'wherein in the case of the oligosaccharide, the monosaccharide units of the oligosaccharide are linked via glycosidic bonds to each other, and Rdenote hydrogen, hydroxyl or carbonyl.'}3. A compound of formula (I) according to claim 1 , wherein in the case where Ris an oligosaccharide with 2 monosaccharide units (disaccharide) claim 1 , the monosaccharide units of the disaccharide of Rare linked via glycosidic bonds together claim 1 , which is not a 1→6 linking.4. A compound of formula according to claim 1 , wherein{'sub': '2', 'Ris an oligosaccharide with 2 monosaccharide units (disaccharide), and'}{'sub': '3', 'Rdenote hydrogen or carbonyl.'}5. A compound of formula (I) according to claim 1 , wherein{'sub': '1', 'Rdenotes hydrogen, hydroxyl carbonyl or an oligosaccharide with 2, 3, 4 or 5 monosaccharide units,'}{'sub': '2', 'Ris an oligosaccharide with 2 monosaccharide unit (disaccharide), and'}{'sub': '3', 'Rdenotes hydroxyl.'}6. A compound of formula (I) according to claim 1 , wherein in the case where Ris an oligosaccharide with 3 monosaccharide units (trisaccharide) claim 1 , then{'sub': '1', 'Ris carbonyl, and/or'}{'sub': '3', 'Ris not hydroxyl or carbonyl, or'}{'sub': 3', '1, ' ...

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Номер записи: 28
17-02-2022 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20220048943A1
Автор: Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R, R, and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 2. (canceled)3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted Calkyl.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris unsubstituted Calkyl.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CH claim 1 , —CF claim 1 , —CHOCH claim 1 , —CH(CH)(CF) claim 1 , —CHCH claim 1 , or —CH(CH).6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHor —CHCH.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris unsubstituted Calkyl.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris substituted or unsubstituted ethyl claim 1 , substituted or unsubstituted isopropyl claim 1 , or substituted or unsubstituted tert-butyl.911-. (canceled)12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein represents a single bond.1617-. (canceled)2021-. (canceled)23. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.24. A method of inducing sedation or anesthesia comprising administering to a subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a pharmaceutical composition thereof.25. A method for treating a disorder claim 1 , comprising administering to a subject in need thereof an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or a pharmaceutical composition thereof; wherein the disorder is a gastrointestinal (GI) disorder ...

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Номер записи: 29
11-02-2016 дата публикации

NOVEL MOGROSIDES, COMPOSITIONS AND THEIR PURIFICATION

Номер: US20160039864A1
Автор: CHATURVEDULA VENKATA SAI PRAKASH, Prakash Indra
Принадлежит:

Novel mogrosides and methods for heir purification are provided herein. In addition, compositions comprising said novel mogrosides and methods for preparing the same are provided. The present invention relates generally to novel mogrosides, as well as compositions comprising such novel mogrosides, including consumables. The present invention further extends to methods of purifying such novel mogrosides, methods for preparing compositions (e.g., consumables) comprising such novel mogrosides and methods of enhancing the flavor or sweetness of consumables using these novel mogrosides. 2. The compound of claim 1 , wherein Ris an oligosaccharide.3. The compound of claim 1 , wherein Ris an oligosaccharide comprising from two to five sugars.4. The compound of claim 1 , wherein Ris an oligosaccharide comprising a monosaccharide selected from the group consisting of glyceraldehyde claim 1 , dihydroxyacetone claim 1 , erythrose claim 1 , threose claim 1 , erythrulose claim 1 , arabinose claim 1 , lyxose claim 1 , ribose claim 1 , xylose claim 1 , ribulose claim 1 , xylulose claim 1 , allose claim 1 , altrose claim 1 , galactose claim 1 , glucose claim 1 , gulose claim 1 , idose claim 1 , mannose claim 1 , talose claim 1 , fructose claim 1 , psicose claim 1 , sorbose claim 1 , tagatose claim 1 , mannoheptulose claim 1 , sedoheltulose claim 1 , octolose claim 1 , fucose claim 1 , rhamnose claim 1 , arabinose claim 1 , turanose and sialose.5. The compound of claim 1 , wherein Rcomprises a branched or unbranched oligosaccharide.7. (canceled)8. (canceled)1016.-. (canceled)17. A composition comprising a compound of formula (1).18. The composition of claim 17 , further comprising mogrosides selected from the group consisting of Luo han guo extract claim 17 , by-products of other mogrosides' isolation and purification processes claim 17 , a commercially available Luo han guo extract claim 17 , mogroside IA claim 17 , mogroside IE claim 17 , 11-oxomogroside IA claim 17 , mogroside II ...

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Номер записи: 30
07-02-2019 дата публикации

Method for separating and purifying mogroside v by subcritical water desorption technology

Номер: US20190040097A1
Автор: Minglian Jiang, Wenguo YANG, Yuanyuan Li, Yunfei SONG
Принадлежит: Guilin Layn Natural Ingredients Corp

The invention relates to a method for separating and purifying mogroside V by subcritical water desorption technology. The macroporous adsorption resin enriched with mogroside V is subjected to desorption under a subcritical condition of water using water as a solvent, to give an aqueous solution rich in mogroside V. The method not only improves the content of mogroside V in product, but also effectively removes bitter impurities and residual pesticides, greatly improves the taste adaptability of the product, and improves the safety and quality of the product. The method reduces the processing steps and reduces the use of organic solvents in the prior art, and reduces total production costs.

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Номер записи: 31
13-02-2020 дата публикации

Dihydroartemisinin-steroid conjugate and preparation method and application thereof

Номер: US20200046679A1
Автор: Jinghua Zhang, Zhengwu Shen
Принадлежит: Yunbaiyao Zhengwu Science And Technology (shanghai) Co Ltd

Described is a dihydroartemisinin-steroid conjugate of formula (I), or a pharmaceutically acceptable salt thereof, where position 10 of dihydroartemisinin is linked to the steroid through a linker X. This application further provides a preparation method of the dihydroartemisinin-steroid conjugate and an application of the dihydroartemisinin-steroid conjugate in the preparation of a drug for treating cancer. The dihydroartemisinin-steroid conjugate of the invention exhibits potent inhibitory activity against various tumor cells and low cytotoxicity, moreover, the conjugate is capable of penetrating the blood-brain barrier, having a broad application prospect.

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Номер записи: 32
25-02-2021 дата публикации

Panaxadiol glycoside derivative and preparation method and application thereof

Номер: US20210054019A1
Автор: Jun Zhang, Quanhai Liu
Принадлежит: Suzhou Ji Er Biological Medicine Co Ltd

The invention discloses a panaxadiol glycoside derivative and a preparation method and application thereof. Such compounds show strong anti-inflammatory effects in vitro and in animal model experiments, and thus can be used to prepare anti-inflammatory drugs, especially can be used for treating asthma and COPD. In the experiment, the above-mentioned compounds have obvious effects on asthma and COPD, and the efficacy of the high-dose group is superior than that of dexamethasone and budesonide. Even under the dose much exceeding the therapeutic dose, no obvious affect on blood routine and blood glucoseis observed. It has high industrial prospects in the field of anti-inflammatory drugs, especially in the field for treating asthma and COPD.

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Номер записи: 33
23-02-2017 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS

Номер: US20170051007A1
Автор: "OBrien Rebecca", Altschul Randice Lisa, Arment Anthony R., Kesel Andreas J., Rapkin Myron, Theise Neil David
Принадлежит:

This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease. 3. The pharmaceutical composition of in a dosage form selected from the group consisting of a minicapsule claim 2 , a capsule claim 2 , a tablet claim 2 , an implant claim 2 , a troche claim 2 , a lozenge claim 2 , a minitablet claim 2 , a temporary or permanent suspension claim 2 , an injectable claim 2 , an ovule claim 2 , a suppository claim 2 , a wafer claim 2 , a chewable tablet claim 2 , a quick or fast dissolving tablet claim 2 , an effervescent tablet claim 2 , a buccal or sublingual solid claim 2 , a granule claim 2 , a film claim 2 , a sprinkle claim 2 , a pellet claim 2 , a topical formulation claim 2 , a patch claim 2 , a bead claim 2 , a pill claim 2 , a powder claim 2 , a triturate claim 2 , a smart pill claim 2 , a smart capsule claim 2 , a platelet claim 2 , a strip claim 2 , and a sachet.4. The pharmaceutical composition of in a dosage form for topical application claim 2 , and at least one pharmaceutically acceptable excipient.5. The pharmaceutical composition of in a dosage form for topical application wherein said formulation is in a form selected from the group consisting of: cream claim 2 , lotion claim 2 , gel claim 2 , oil claim 2 , ointment claim 2 , suppository claim 2 , spray claim 2 , foam claim 2 , liniment claim 2 , aerosol claim 2 , buccal and sublingual tablet or a transdermal device or patch for absorption through the skin or mucous membranes.632-. (canceled) This application claims benefit under 35 U.S.C. §119(e) of U.S. Provisional Patent Application No. 62/282,525, filed Aug. 3, 2015; U.S. Provisional Patent Application No. 62/220,583, filed Sep. 18, 2015; U.S. Provisional Patent Application No. 62/241,875, ...

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Номер записи: 34
26-02-2015 дата публикации

4-pregenen-11beta-17-21-triol-3,20-dione derivatives

Номер: US20150057258A1
Автор: Alissar Nehme, Jeffrey L. Edelman, Thomas C. Malone
Принадлежит: Allergan Inc

The present invention relates to novel 4-pregenen-11β-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.

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Номер записи: 35
26-02-2015 дата публикации

TWO CRYSTAL FORMS OF GINSENOSIDE C-K AND METHOD FOR PREPARING SAME

Номер: US20150057440A1
Автор: Bai Hua, Chen Feng, Chen Jinyao, Dai Changliang, Hong Minghuang, Qi Minghui, Ren Guobin, Zhu Wenming
Принадлежит: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

Provided are ginsenoside C-K polymorphic forms and a method for preparing same. The ginsenoside C-K polymorphic forms are crystal form D and crystal form H. 1. A crystal form D of ginsenoside C-K , characterized in that there are diffraction peaks at 2θ values (°) of 6.39 , 12.71 , 13.30 , 15.79 , 16.14 , 16.44 , 20.03 , 20.74 , and 24.29 in the XRPD pattern of said crystal form , wherein the error range of 2θ value is ±0.2°.2. The crystal form D according to claim 1 , wherein the crystal form also has diffraction peaks at 2θ values (°) of 10.66 claim 1 , 11.21 claim 1 , 16.85 claim 1 , 17.27 claim 1 , 19.05 claim 1 , 21.33 claim 1 , 21.65 claim 1 , 22.52 claim 1 , 23.48 claim 1 , 24.93 claim 1 , 25.46 claim 1 , 26.76 claim 1 , 27.99 claim 1 , 29.15 claim 1 , 30.39 claim 1 , and 34.14 claim 1 , wherein the error range of 2θ value is ±0.2.3. The crystal form D according to claim 1 , wherein said crystal form has diffraction peaks of the XRPD pattern substantially as shown in .4. The crystal form D according to claim 1 , wherein said crystal form has an endothermic peak of around 154±5° C. in the DSC pattern.5. A method for preparing the crystal form D according to claim 1 , comprising:(1) dissolving ginsenoside C-K in an organic solvent or a mixed solvent of organic solvent and water, wherein the organic solvent is selected from the group consisting of n-propanol and tetrahydrofuran;(2) adding dropwise water in a volume of 1-4 folds of the organic solvent or the mixed solvent of organic solvent and water in step (1);(3) stirring, filtering the resultant suspension, and drying filter cake under vacuum to obtain the crystal form D of ginsenoside C-K.6. A method for preparing the crystal form D according to claim 1 , comprising:(1) dissolving ginsenoside C-K in a mixed solvent of acetonitrile and water, or a mixed solvent of dimethyl sulfoxide and nitromethane;(2) removing the solvent slowly by evaporation, or removing a portion of the solvent slowly by evaporation, ...

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Номер записи: 36
03-03-2016 дата публикации

AMPHIPHILIC COMPOUNDS

Номер: US20160060290A1
Автор: Chae Pil Seok, GELLMAN Samuel Helmer, Kobilka Brian, Rasmussen Søren
Принадлежит:

Bringing membrane proteins into aqueous solution generally requires the use of detergents or other amphiphilic agents. The invention provides a new class of amphiphiles, each of which includes a multi-fused ring system as a lipophilic group. These new amphiphiles confer enhanced stability to a range of membrane proteins in solution relative to conventional detergents, leading to improved structural and functional stability of membrane proteins, including integral membrane proteins. Accordingly, the invention provides new amphiphiles for biochemical manipulations and characterization of membrane proteins. These amphiphiles display favorable behavior with membrane proteins and can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins. 2. The compound of claim 1 , wherein Ris methyl.3. The compound of claim 1 , wherein each Sac is an oxygen-linked monosaccharide.4. The compound of claim 1 , wherein each Sac is an oxygen-linked disaccharide.5. The compound of claim 1 , wherein each Sac is an oxygen-linked trisaccharide.6. The compound of claim 1 , wherein X is NH claim 1 , Y is O claim 1 , Z is H claim 1 , and L is a direct bond.7. The compound of claim 1 , wherein L is —CH— claim 1 , X is O claim 1 , Y is absent claim 1 , and Z is Me.8. The compound of claim 1 , wherein L is a direct bond claim 1 , X is a direct bond claim 1 , Y is absent claim 1 , and Z is H.11. The compound of claim 1 , wherein the critical micelle concentration (CMC) of the compound in water is about 5 nM to about 100 nM.12. The compound of claim 1 , wherein a plurality of the compounds form a micelle in water comprising about 5 to about 35 molecules of the compound.13. A composition comprising a compound of and an isolated membrane protein.14. A micelle comprising a compound of .15. The micelle of claim 14 , further comprising a polypeptide or a protein.16. A method of solubilizing or stabilizing a membrane ...

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Номер записи: 37
15-05-2014 дата публикации

Novel Ginsenoside With Anti-cancer Activity And The Preparation Method Thereof

Номер: US20140135278A1
Автор: BAI Liping, DONG HANG, JIANG Zhihong, LIU LIANG, WONG Kam Wai, ZHOU Hua
Принадлежит: MACAU UNIVERSITY OF SCIENCE AND TECHNOLOGY

The present invention relates to a novel compound derived from ginsenoside Rh2, the preparation methods and the use thereof in treating cancers. 2. A method of treating cancer comprising administering an effective amount of said ginsenoside compound of to a subject in need thereof.3. The method according to wherein said effective amount ranges from 10-2 claim 2 ,000 mg/kg of said ginsenoside compound per dose.4. The method according to claim 2 , wherein said cancer is selected from a group consisting of lung cancer claim 2 , colon cancer claim 2 , pancreatic cancer claim 2 , nasopharyngeal carcinoma claim 2 , liver cancer claim 2 , breast cancer claim 2 , prostate cancer claim 2 , cervical cancer claim 2 , ovarian cancer claim 2 , bladder cancer claim 2 , acute promyelocytic leukemia (APL) claim 2 , acute myeloid leukemia (AML) claim 2 , acute lymphocytic leukemia (ALL) claim 2 , chronic myelogenous leukemia (CML) claim 2 , non-Hodgkin's lymphoma claim 2 , Hodgkin's disease claim 2 , chronic lymphocytic leukemia (CLL) claim 2 , myelodysplastic syndrome claim 2 , Adult T-cell leukemia (ATL) claim 2 , Burkitt's lymphoma claim 2 , B-cell lymphoma claim 2 , primary malignant lymphocytes claim 2 , B-cell chronic lymphocytic leukemia (B-CLL) claim 2 , human THP-1 leukemia and multiple myeloma.5. Use of said ginsenoside compound according to in the manufacture of a chemotherapeutic agent claim 1 , wherein said chemotherapeutic agent comprises an effective amount of said ginsenoside compound.6. A pharmaceutical composition comprising ginsenoside compound according to admixed with a pharmaceutical carrier suitable for use by oral administration.7. A method of synthesizing ginsenoside compound according to comprising the steps of:a. providing a solution of 20(R)-ginsenoside Rh2;{'sub': '3', 'b. adding mono-persulfate compound and NaHCO;'}c. adding a catalyst solution to the mixture of step (b);d. standing the catalyzed mixture from step (c) for 8-24 hours at room temperature ...

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Номер записи: 38
15-05-2014 дата публикации

OSW-1 ANALOGS AND CONJUGATES, AND USES THEREOF

Номер: US20140135279A1
Автор: Shair Matthew D.
Принадлежит: President and Fellows of Harvard College

Provided are a number of compounds structurally related to OSW-1, a natural compound that binds OSBPs. Also provided are pharmaceutical compositions comprising the OSW-1 analogs, as well as methods for use of these OSW-1 analogs, or pharmaceutically acceptable salts, enantiomers, or stereoisomers thereof in the treatment of atherosclerosis. Alzheimer's disease, and cancer, including p21-deficient cancer. Conjugates of OSW-1 analogs with monoclonal antibodies, including monoclonal antibodies targeted to cancer cells, are also provided. Also provided are pharmaceutical compositions comprising the conjugates, as well as methods for use of these conjugates, in the treatment of cancer, including p21-deficient cancer. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 1 , wherein Ris acetyl.4. The compound of claim 1 , wherein Ris para-methoxybenzoyl or 3-phenylpropanoyl.5. (canceled)6. The compound of claim 1 , wherein Z is O.7. The compound of claim 6 , wherein R is selected from the group consisting of alkyl and 4-nitrophenyl.8. The compound of claim 6 , wherein n is 0.9. The compound of claim 1 , wherein Z is NH.10. The compound of claim 9 , wherein R is an amino group.11. (canceled)12. The compound of claim 10 , wherein n is 6.13. The compound of claim 9 , wherein R is a para-aminoalkylaryl group.14. (canceled)15. The compound of claim 13 , wherein n is 1.16. The compound of claim 9 , wherein n is 1; and R is phenyl.17. The compound of claim 1 , wherein Z is absent.18. The compound of claim 17 , wherein R is an amino group.19. (canceled)20. The compound of claim 18 , wherein n is 2.21. The compound of claim 17 , wherein R is a 1-imidazolyl group.22. The compound of claim 21 , wherein n is 0.23. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Ris tert-butyldimethylsilyl.2425-. (canceled)27. A pharmaceutical composition claim 1 , comprising a compound of ; and a pharmaceutically acceptable carrier.28. A method of ...

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Номер записи: 39
05-03-2015 дата публикации

GINSENOSIDE C-K POLYMORPHIC COMPOUNDS AND METHOD FOR PREPARING SAME

Номер: US20150065699A1
Автор: Bai Hua, Chen Feng, Chen Jinyao, Dai Changliang, Hong Minghuang, Qi Minghui, Ren Guobin, Zhu Wenming
Принадлежит: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

Provided are several types of ginsenoside polymorphic substances and a method for preparing same. In particular, new crystal form A, crystal form B, crystal form C, crystal form E, crystal form F, crystal form I, crystal form K, crystal form L, crystal form M, crystal form N, and crystal form O are involved. 1. A crystal form A of ginsenoside C-K , characterized in that there are diffraction peaks at 2θ values (o) of 5.44 , 7.06 , 8.94 , 11.61 , 13.70 , 14.43 , 15.81 , 17.22 , 17.84 , 18.71 , and 19.01 in the XRPD pattern , wherein the error range of 2θ value is ±0.2.2. The crystal form A according to claim 1 , characterized in that the crystal form A also has diffraction peaks at 2θ values of 9.51 claim 1 , 12.28 claim 1 , 16.14 claim 1 , 20.90 claim 1 , 21.90 claim 1 , 25.68 claim 1 , and 27.71 claim 1 , wherein the error range of 2θ value is ±0.2.34-. (canceled)5. A method for preparing the crystal form A of ginsenoside C-K according to claim 1 , comprising:(1) dissolving ginsenoside C-K in 1-methyl-2-pyrrolidone or a mixed solvent consisting of 1-methyl-2-pyrrolidone and acetone;(2) removing the solvent slowly by evaporation;(3) drying the resultant solid under vacuum to obtain the crystal form A of ginsenoside C-K, or comprising:(1) dissolving ginsenoside C-K in 1-methyl-2-pyrrolidone;(2) adding an anti-solvent dropwise, wherein the anti-solvent is selected from the group consisting of isopropyl ether, water and nitromethane;(3) after stirring for a while, filtering the resultant suspension, and drying the filter cake under vacuum to obtain the crystal form A of ginsenoside C-K.6. (canceled)7. A crystal form B of ginsenoside C-K claim 1 , characterized in that there are diffraction peaks at 2θ values (o) of 5.31 claim 1 , 9.73 claim 1 , 9.89 claim 1 , 10.70 claim 1 , 11.25 claim 1 , 13.83 claim 1 , 16.14 claim 1 , 16.85 claim 1 , and 18.69 in the XRPD pattern claim 1 , wherein the error range of 2θ value is ±0.2.8. The crystal form B according to claim 7 , ...

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Номер записи: 40
17-03-2022 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20220079957A1
Автор: Qian Xiangping
Принадлежит:

Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. 2. At least one chemical entity of wherein Z is OR.3. At least one chemical entity of wherein Ris chosen from optionally substituted alkyl claim 2 , optionally substituted cycloalkyl claim 2 , and optionally substituted heterocycloalkyl.4. At least one chemical entity of wherein Z is NRR.5. At least one chemical entity of wherein Ris chosen from hydrogen claim 4 , optionally substituted alkyl claim 4 , optionally substituted cycloalkyl claim 4 , and optionally substituted heterocycloalkyl claim 4 , and Ris chosen from optionally substituted alkyl claim 4 , optionally substituted cycloalkyl claim 4 , and optionally substituted heterocycloalkyl.6. At least one chemical entity of wherein Ris hydrogen and Ris chosen from optionally substituted alkyl.7. At least one chemical entity of wherein Rand Rare joined together to form a 5- to 7-membered heterocycloalkyl ring.8. At least one chemical entity chosen from compounds I-a-I-f and pharmaceutically acceptable salts thereof.10. At least one chemical entity of wherein Rand Rare each independently chosen from hydrogen and optionally substituted lower alkyl.11. At least one chemical entity of wherein Rand Rare both hydrogen.12. At least one chemical entity of wherein Rand Rare joined together to form a 5- to 7-membered heterocycloalkyl ring.13. At least one chemical entity of any one of to wherein Rand Rare each independently chosen from hydrogen and optionally substituted lower alkyl.14. At least one chemical entity of any one of to wherein n is chosen from 1 claim 9 , 2 claim 9 , and 3.15. At least one chemical entity of wherein n is 1 claim 9 , and Rand Rare joined together to form a 5- to 7-membered heterocycloalkyl ring.16. At least one chemical entity chosen from compounds II-a-II-h and pharmaceutically acceptable salts thereof.18. At least one chemical entity of wherein Ris chosen from hydrogen ...

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Номер записи: 41
28-02-2019 дата публикации

METHODS FOR THE PREPARATION OF OBETICHOLIC ACID AND DERIVATIVES THEREOF

Номер: US20190062367A1
Автор: Galvin Gabriel M
Принадлежит:

The present application relates to a method of preparing a bile acid derivative, or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, comprising direct alkylation at the C-6 position of KLCA. 3. The method of or , wherein the alkylating agent is selected from alkyl halide , alkyl tosylate , alkyl mesylate , sulfonate ester , alkyl oxonium salt , dialkyl sulfate , dialkyl carbonate , and tetraalkylammonium salt.4. The method of claim 3 , wherein the alkylating agent is alkyl halide.5. The method of claim 4 , wherein the alkyl halide is ethyl bromide or ethyl iodide.6. The method of or claim 4 , wherein the alkylation is conducted in an aprotic solvent.7. The method of claim 6 , wherein the aprotic solvent is selected from tetrahydrofuran (THF) claim 6 , ethyl acetate (EtOAc) claim 6 , acetone claim 6 , dimethylformamide (DMF) claim 6 , acetonitrile (MeCN) claim 6 , dimethyl sulfoxide (DMSO) claim 6 , toluene claim 6 , hexane claim 6 , benzene claim 6 , 1 claim 6 ,4-dioxane claim 6 , chloroform claim 6 , dichloromethane (DCM) claim 6 , diethyl ether claim 6 , and methyl test-butyl ether (MTBE).8. The method of or claim 6 , wherein the alkylation is conducted in the presence of a deprotonating agent.9. The method of claim 8 , wherein the deprotonating agent is selected from C-Calkoxide claim 8 , metal hydroxide claim 8 , and metal hydride.10. The method of or claim 8 , further comprising claim 8 , deprotonating Compound 1 before Compound 1 is alkylated.11. The method of claim 10 , wherein the deprotonating agent is selected from C-Calkoxide claim 10 , metal hydroxide claim 10 , and metal hydride.12. The method of or claim 10 , further comprising deprotecting Compound 1 after alkylation of the carbon atom at the C-6 position.13. The method of claim 12 , comprising deprotecting the hydroxyl group at the C-3 position.14. The method of claim 13 , further comprising deprotecting the carboxylic group at the C-24 position claim 13 , wherein the ...

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Номер записи: 42
07-03-2019 дата публикации

METHODS FOR MAKING HIGH INTENSITY SWEETENERS

Номер: US20190071705A1
Автор: Colquitt Justin, Faber Nathan, Manam Rama R., Noriega Chris Edano, PATRON Andrew P., STEGE Justin, ZIELER Helge
Принадлежит:

Provided herein include methods of making mogroside compounds, e.g., Compound 1, compositions (for example host cells) for making the mogroside compounds, and the mogroside compounds made by the methods disclosed herein, and compositions (for example, cell lysates) and recombinant cells comprising the mogroside compounds (e.g., Compound 1). Also provided herein are novel cucurbitadienol synthases and the use thereof. 2. The method of claim 1 , wherein contacting mogroside IIIwith the first enzyme comprises contacting mogroside IIIwith a recombinant host cell that comprises a first gene encoding the first enzyme.3256.-. (canceled)257. The method of claim 2 , wherein the mogroside IIIis present in and/or produced by the recombinant host cell.258. The method of claim 1 , wherein the first enzyme is one or more of UDP glycosyltransferases claim 1 , cyclomaltodextrin glucanotransferases (CGTases) claim 1 , glycotransferases claim 1 , dextransucrases claim 1 , cellulases claim 1 , β-glucosidases claim 1 , amylases claim 1 , transglucosidases claim 1 , pectinases claim 1 , and dextranases.259. The method of claim 258 , wherein the CGTase comprises an amino acid sequence having at least 70% sequence identity to the sequence of any one of SEQ ID NOs: 1 claim 258 , 3 claim 258 , 78-101 claim 258 , 148 claim 258 , and 154.260. The method of claim 258 , wherein the dextransucrase comprises an amino acid sequence having at least 70% sequence identity to any one of the sequences set forth in SEQ ID NOs: 2 claim 258 , 103 claim 258 , 106-110 claim 258 , 156 claim 258 , 159-162 claim 258 , and 896; or wherein the dextransucrase is encoded by a nucleic acid sequence having at least 70% sequence identity to any one of SEQ ID NOs: 104 claim 258 , 105 claim 258 , 157 claim 258 , 158 claim 258 , and 895.261. The method of claim 258 , wherein the transglucosidase comprises an amino acid sequence having at least 70% sequence identity to the sequence of any one of SEQ ID NOs: 163-291 and ...

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Номер записи: 43
05-03-2020 дата публикации

TACCALONOLIDE MICROTUBULE STABILIZERS

Номер: US20200071351A1
Автор: Cichewicz Robert H., Du Lin, LI Jing, Mooberry Susan L., Ola Antonius, Peng Jiangnan, Risinger April L., S.M. Yee Samantha
Принадлежит:

This present disclosure relates to the fields of medicine and pharmaceuticals. In particular, the invention relates to the identification of epoxytaccalonolide microtubule stabilizers for use in inhibiting cell proliferation and disrupting normal cellular microtubule processes leading to cell death. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The compound of claim 1 , wherein Ris acyloxy.3. The compound of claim 1 , wherein C7/C8 are connected with a double bond.4. The compound of claim 1 , wherein Ris a hydroxy or alkyl.15. A composition comprising at least 90% by weight of a compound according to claim 1 , claim 1 , or .16. A composition comprising a compound according to claim 1 , claim 1 , or and a pharmaceutically acceptable carrier therefor.17. A method of treating a hyperproliferative disorder in a patient claim 1 , the method comprising administering to a patient in need thereof an effective amount of a compound according to claim 1 , claim 1 , or or of an effective amount of a composition according to .18. Use of a compound according to claim 1 , claim 1 , or or of a composition according to in the preparation of a medicament for the treatment of a hyperproliferative disorder in a patient.19. A compound according to claim 1 , claim 1 , or for the treatment of a hyperproliferative disorder in a patient.20Tacca. A method of producing a mixture of epoxytaccalonolides claim 1 , said method comprising subjecting a solution of a taccalonolide-containing crude extract of the roots and/or rhizomes of a species in an organic solvent to epoxidation. This application claims the benefit of U.S. Provisional Application No. 62/434,919, filed on Dec. 15, 2016, which is incorporated herein by reference in its entirety.This invention was made with government support under grant no. CA121138, awarded by the National Institutes of Health. The government has certain ...

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Номер записи: 44
24-03-2016 дата публикации

19-nor c3, 3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof

Номер: US20160083417A1
Автор: Albert Jean Robichaud, Boyd L. Harrison, Francesco G. Salituro, Gabriel Martinez Botella, Richard Thomas Beresis
Принадлежит: Sage Therapeutics Inc

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein, , R 1 , R 2 , R 3a , R 3b , R 4a , and R 4b are as defined herein, and A is a carbon bound substituted or unsubstituted 5- to 6-membered heteroaryl ring as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

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Номер записи: 45
26-03-2015 дата публикации

STEROL DERIVATIVES AND USE THEREOF FOR TREATING DISEASES INVOLVING TRANSFORMED ASTROCYTE CELLS OR FOR TREATING MALIGNANT HAEMOPATHIES

Номер: US20150086615A1
Автор: CLARION Ludovic, MERSEL Marcel, Petite Didier
Принадлежит: BETA INNOV

Novel sterol derivatives, the preparation method thereof, pharmaceutical compositions containing them and use thereof for treating diseases involving transformed astrocyte cells or for treating malignant haemopathies. The treatment of glioblastoma multiforme, as well as of other cancers, such as lymphomas, neuroblastomas and melanomas is also described. 122-. (canceled)25. Compound of formula (I) according to claim 23 , in which A represents a —C(O)—Rgroup in which Ris a 2 claim 23 ,2-dimethyl-1 claim 23 ,3-dioxolane group; or a linear or branched C-Calkyl group unsubstituted or substituted with a group selected from OR claim 23 , NHR and SR claim 23 , where R represents hydrogen claim 23 , a linear C-Calkyl or an unsubstituted C-Caryl; a C-Caryl group or a C-Cheteroaryl group claim 23 , which are unsubstituted or substituted with at least one linear or branched C-Calkyl claim 23 , or with at least one group selected from OR claim 23 , NHR and SR claim 23 , where R represents hydrogen claim 23 , a linear C-Calkyl or an unsubstituted C-Caryl; or else a sugar residue.26. Compound of formula (I) according to claim 23 , in which B represents an acyl group in which the alkyl group is C-C claim 23 , in particular acetyl claim 23 , or an alkoxycarbonyl group in which the alkyl group is C-C claim 23 , in particular a tert-butoxycarbonyl group.27. Compound of formula (I) according to claim 23 , in which B can also claim 23 , in particular claim 23 , represent a C-Calkyl group claim 23 , unsubstituted or substituted with at least one group selected from OR claim 23 , NHR and SR claim 23 , as defined above; or a C-Caryl group claim 23 , unsubstituted or substituted with at least one linear or branched C-Calkyl or with at least one group selected from OR claim 23 , NHR and SR claim 23 , where R represents hydrogen claim 23 , a linear C-Calkyl or an unsubstituted C-Caryl.28. Compound of formula (I) claim 23 , characterized in that it is selected from the following compounds:7-(( ...

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Номер записи: 46
21-03-2019 дата публикации

RAMAN TAG

Номер: US20190085019A1
Автор: Dai Mingji
Принадлежит: PURDUE RESEARCH FOUNDATION

A method of forming a probe, wherein the method includes converting cholenic acid into a compound with a terminal alkyne group, wherein the converting the cholenic acid comprises using a sequence, wherein the sequence comprises synthesizing a THP-protection group, LiAlH4 reduction, Dess-Martin oxidation, and Seyferth-Gilbert-Bestmann homologation. 7. The method of further comprising:forming alkyne cholesterol (A-Chol) by removing the THP-protection group;forming phenyl-alkyne cholesterol (PhA-Chol) from the compound with the terminal alkyne group via a palladiumcatalyzed Sonogashira reaction; andforming phenyl-diyne cholesterol (PhDY-Chol) from the compound with the terminal alkyne group via a coppercatalyzed Cadiot-Chodkiewicz reaction.8. The method of claim 1 , further comprising removing the THP-protection group via an acid. The Present U.S. patent application is a continuation of U.S. patent application Ser. No. 15/634,567, filed Jun. 27, 2017, is a continuation of U.S. patent application Ser. No. 14/850,949, filed Sep. 10, 2015, which is related to and claims the priority benefit of U.S. Provisional Patent Application Ser. No. 62/048,484, filed Sep. 10, 2014, the contents of which are hereby incorporated by reference in their entirety into this disclosure.This invention was made with government support under CA182608 awarded by the National Institutes of Health. The government has certain rights in the invention.The present disclosure generally relates to tags for imaging molecules using Raman spectroscopy, and in particular to a method and composition that uses cholesterol mimics to track the location and movement of cholesterol.This section introduces aspects that may help facilitate a better understanding of the disclosure. Accordingly, these statements are to be read in this light and are not to be understood as admissions about what is or is not prior art.An important component of cellular membrane, cholesterol controls physical properties of the membrane ...

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Номер записи: 47
19-06-2014 дата публикации

Orally consumable formulations comprising certain sweet-tasting triterpenes and triterpene glycosides

Номер: US20140170083A1
Автор: Jakob Ley, Katharina Reichelt, Katja Obst, Ludger Wessjohann, Ngo Van Trai, Sabine Wessjohann, The Anh Nguyen, Tran Van Sung
Принадлежит: SYMRISE AG

The invention relates to triterpenes and triterpene glycosides of the formula (I) and/or physiologically acceptable salts thereof, preferably naturally occurring triterpenes and triterpene glycosides from Mycetia balansae and/or physiologically acceptable salts thereof and orally consumable formulations comprising one or a plurality of these triterpenes and triterpene glycosides and/or physiologically acceptable salts thereof. The invention further relates to the use of these triterpenes and triterpene glycosides and/or physiologically acceptable salts thereof, preferably an extract of Mycetia balansae , for generating a sweet impression in an orally consumable formulation or for reinforcing the sweet impression of an orally consumable formulation comprising at least one further, preferably naturally occurring, sweet-tasting substance. Finally, the invention also relates to a method for producing an orally consumable formulation and a method for generating and/or reinforcing a sweet impression of an orally consumable formulation.

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Номер записи: 48
19-03-2020 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20200085846A1
Автор: Qian Xiangping
Принадлежит:

Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. 131.-. (canceled)32. A compound selected from the group consisting of:(R)-(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 2-aminopropanoate;(S)-(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 2-aminopropanoate;(R)-(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 2-amino-3-methylbutanoate;(S)-(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 2-amino-3-methylbutanoate;(R)-(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 2-amino-4-methylpentanoate;(S)-(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl 2-amino-4-methylpentanoate;(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl (2-(pyrrolidin-1-yl)ethyl) carbonate;(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl (2-morpholinoethyl) carbonate;(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl (2-(pyrrolidin-1-yl)ethyl)carbamate;(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl (2-morpholinoethyl)carbamate;(3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5-yl)hexadecahydro-1H-cyclopenta[a]phenanthren-3-yl piperazine-1-carboxylate;4-(((((3S,5R,8R,9S,10S,13R,14S,17R)-14-hydroxy-10,13-dimethyl-17-(2-oxo-2H-pyran-5- ...

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Номер записи: 49
19-03-2020 дата публикации

NUCLEOTIDE AND OLIGONUCLEOTIDE PRODRUGS

Номер: US20200087338A1
Автор: Iyer Radhakrishnan P., Padmanabhan Seetharamaiyer
Принадлежит:

The present invention discloses compounds of formula (I): 2. The method of claim 1 , wherein said compound is administered together with other agents.3. The method of claim 1 , wherein the subject is infected with a resistant strain of HCV. This application is a continuation of U.S. patent application Ser. No. 15/922,581, filed Mar. 15, 2018, which is a continuation of U.S. patent application Ser. No. 14/939,397, filed Nov. 12, 2015, which is a continuation of U.S. patent application Ser. No. 14/186,768, filed on Feb. 21, 2014, which is a continuation of U.S. Pat. No. 8,691,787, filed on Nov. 14, 2011, which is a continuation of U.S. Pat. No. 8,076,303, filed on Dec. 12, 2006, which claims priority to U.S. Provisional Application No. 60/800,294, filed on May 15, 2006, and U.S. Provisional Application No. 60/750,036, filed on Dec. 13, 2005. The contents of each of the foregoing applications are hereby incorporated by reference in their entirety.The invention was supported, in whole or in part by NIH Grant number 5 UO1 AI058270-02/03.The present invention relates to the design, synthesis, and evaluation of prodrug analogs of nucleosides, nucleotides, and oligonucleotides. The compounds, compositions and methods of the present invention are useful for the treatment of hepatitis B virus (HBV) infections and liver diseases associated with HBV. Specifically compounds and compositions related to S-alkyl esters of novel anti-HBV agents phosphorothioate di-, and tri-nucleotides. The compounds and combinations can be administered either alone or in combination with other anti-HBV agents.Acute and chronic liver infections caused by Hepatitis B virus (HBV) constitute a major worldwide public health crisis affecting nearly 2 billion people including 1.7 million in the US (WHO report). There are an estimated 350 million chronic carriers of HBV worldwide. According to the Centers for Disease Control, nearly 3 to 7 million people die each year from complications associated with the ...

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Номер записи: 50
12-05-2022 дата публикации

Novel Mogrosides and Uses of the Same

Номер: US20220142216A1
Автор: Christopher MERCOGLIANDO, Gil Ma, Goran Petrovic, Indra Prakash
Принадлежит: Coca Cola Co

Mogrosides containing non-glucose glycosides are provided herein. Compositions, including consumables comprising the novel mogrosides described herein, are also provided.

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Номер записи: 51
01-04-2021 дата публикации

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

Номер: US20210094981A1
Автор: Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Described herein are steroids of Formula (I): 2. The method of claim 1 , wherein Ris methyl.3. The method of claim 1 , wherein both Rand Rare hydrogen.4. The method of claim 1 , wherein Ris C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , carbocyclyl claim 1 , heterocyclyl claim 1 , C(O)R claim 1 , —C(O)OR claim 1 , or —C(O)NRR.5. The method of claim 4 , wherein Ris —C(O)NRR.6. The method of claim 1 , wherein Ris hydrogen claim 1 , C-Calkyl claim 1 , or —OH.7. The method of claim 6 , wherein Ris hydrogen.8. The method of claim 1 , wherein both Rand Rare hydrogen claim 1 , the between —CRand —CRRis a single bond claim 1 , and both Rand Rare hydrogen.9. The method of claim 1 , wherein Z is —CH—.10. The method of claim 1 , wherein Ris hydrogen and Ris C-Calkyl.12. The method of claim 11 , wherein Ris methyl.13. The method of claim 11 , wherein Ris C-Calkyl claim 11 , C-Calkenyl claim 11 , C-Calkynyl claim 11 , carbocyclyl claim 11 , heterocyclyl claim 11 , —C(I)R claim 11 , —C(O)OR claim 11 , or —C(O)NRR.14. The method of claim 11 , wherein Ris C-Calkyl.15. The method of claim 11 , wherein Ris hydrogen.16. The method of claim 11 , wherein both Rand Rare hydrogen and both Rand Rare hydrogen.19. The method of claim 18 , wherein Ris methyl.20. The method of claim 18 , wherein Ris C-Calkyl claim 18 , C-Calkenyl claim 18 , C-Calkynyl claim 18 , carbocyclyl claim 18 , heterocyclyl claim 18 , —C(O)R claim 18 , —C(O)OR claim 18 , or —C(O)NRR.21. The method of claim 18 , wherein Ris C-Calkyl.22. The method of claim 20 , wherein Ris —C(O)NRR.23. The method of claim 18 , wherein Ris —OH.24. The method of claim 18 , wherein Ris hydrogen.25. The method of claim 18 , wherein both Rand Rare hydrogen and both Rand Rare hydrogen.27. (canceled)28. (canceled)29. (canceled)30. The method of claim 1 , wherein the CNS-related disorder is a major depressive disorder.31. The method of claim 1 , wherein the CNS-related disorder is tremor.32. The method of claim 31 , wherein the ...

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Номер записи: 52
09-04-2015 дата публикации

Glycosylation Reactions Using Phenyl(trifluoroethyl)iodonium Salts

Номер: US20150099870A1
Автор: Bennett Clay S., Chu An-Hsiang A.
Принадлежит:

Provided are methods for the preparation of glycosylation products, including those represented by formula I: 2. The method of claim 1 , wherein Sugar is an optionally protected monosaccharide claim 1 , disaccharide claim 1 , or trisaccharide.3. The method of claim 1 , wherein Sugar is an optionally protected monosaccharide.4. The method of claim 1 , wherein Sugar is a protected glucopyranoside.5. The method of claim 1 , wherein R′ is selected from the group consisting of alkyl claim 1 , cycloalkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , aralkyl claim 1 , and heteroaralkyl; or R′—OH is a steroid or an optionally protected monosaccharide claim 1 , disaccharide claim 1 , trisaccharide claim 1 , or tetrasaccharide.6. The method of claim 1 , wherein R′—OH is cholesterol.7. The method of claim 1 , wherein R′—OH is a protected monosaccharide or disaccharide.8. The method of claim 1 , wherein the OH group of R′—OH that forms a bond to the anomeric carbon atom of Sugar is the C3 or C6 hydroxyl of a protected monosaccharide or disaccharide.10. The method of claim 1 , wherein Ris a phenyl or naphthyl group optionally substituted with one halo claim 1 , alkyl claim 1 , or haloalkyl.11. The method of claim 1 , wherein Ris an unsubstituted phenyl group.12. The method of claim 1 , wherein Rrepresents one or two substituents each independently selected from the group consisting of halo claim 1 , alkyl claim 1 , fluoroalkyl claim 1 , and perfluoroalkyl.13. The method of claim 1 , wherein Ris absent.14. The method of claim 1 , wherein Ris fluoroalkyl.15. The method of claim 1 , wherein Ris 2 claim 1 ,2 claim 1 ,2-trifluoroethyl.16. The method of claim 1 , wherein Xis selected from the group consisting of methanesulfonate claim 1 , trifluoromethanesulfonate claim 1 , benzenesulfonate claim 1 , p-toluenesulfonate claim 1 , bis(methanesulfonyl)amide claim 1 , bis(trifluoromethanesulfonyl)amide claim 1 , bis(benzenesulfonyl)amide claim 1 , (trifluoromethanesulfonyl)( ...

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Номер записи: 53
16-04-2015 дата публикации

SYNTHESIS

Номер: US20150105543A1
Автор: Marshall Philip Andrew, Mason Jennifer Mary, Muscroft-Taylor Andrew Clive, Walker David Millar
Принадлежит: Oncology Research International Limited

The present invention provides an improved synthesis of a class of steroid saponins. Furthermore, the present invention provides a method of selectively discriminating between the C2 and C3 hydroxyl groups of a mono-glycosylated steroid saponin—a key step in the preparation of this class of compounds. Additionally, the present invention provides a range of steroid saponin derivatives, and methods of making them. 2. A method according to wherein the base in step (i) is selected from the group consisting of KCO claim 1 , triethylamine claim 1 , diisopropylethylamine claim 1 , pyridine claim 1 , 4-dimethylaminopyridine claim 1 , and 1 claim 1 ,8-diazabicycloundec-7-ene.3. (canceled)4. A method according to wherein step (i) is carried out in the presence of a solvent claim 1 , wherein the solvent is selected from the group consisting of dichloromethane claim 1 , tetrahydrafuran claim 1 , 1 claim 1 ,2-dioxane claim 1 , dichloroethane claim 1 , chloroform claim 1 , carbon tetrachloride and pyridine.56-. (canceled)7. A method according to wherein step (i) is conducted at a temperature in the range of from −100 to 80° C.89-. (canceled)10. A method according to wherein the temperature of step (i) is initially in the range of −10 to 20° C. claim 7 , and then subsequently increased over the course of the reaction to a temperature in the range of in the range of 10 to 25° C.11. A method according to wherein the acylating agent is an acid anhydride or an acyl halide selected from the group consisting of acetyl chloride claim 1 , propionyl chloride claim 1 , benzoyl chloride claim 1 , 2-chlorobenzoyl chloride claim 1 , 4-chlorobenzoyl chloride claim 1 , 4-nitrobenzoyl chloride and 4-methoxybenzoyl chloride.1214-. (canceled)15. A method according to wherein the ratio of acylating agent to a compound of Formula A is from 3:1 to 1:1.1618-. (canceled)2021-. (canceled)22. A method according to wherein Ris selected from the group consisting of spirostanol aglycones and furostanol ...

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Номер записи: 54
02-06-2022 дата публикации

LIPIDIC ANALOGS OF ANTI-CANCER STEM CELL AGENT

Номер: US20220169673A1
Автор: "OHARA Connor", ABDELFADIEL Elsamani I., AFOSAH Daniel Kwame, BOOTHELLO Rio, Desai Umesh R., GANGJI Rahaman Navaz, MORLA Shravan, Nagarajan Balaji, ONGOLU Ravikumar, PATEL Bhaumik B., SANKARANARAYANAN Viji, SHARON Chetna, SISTLA Jyothi, VERA Alberto
Принадлежит:

A group of specific sulfated flavonoid agents carrying cholesterol modification display promising in vivo anti-cancer activity through selective inhibition of cancer stem cells, and not of adult or hematopoietic stem cells. The compounds exhibit high potency, excellent oral bioavailability and a physiologically relevant therapeutic window. 6. (canceled)7. A method for treating cancer comprising administering to a subject in need thereof a therapeutically effective amount of a compound of .8. The method of claim 7 , wherein the subject in mammalian.9. The method of claim 7 , wherein the subject is human.10. The method of claim 7 , wherein the cancer is selected from the group consisting of colon cancer claim 7 , breast cancer claim 7 , lung cancer claim 7 , liver cancer claim 7 , renal cancer claim 7 , pancreatic cancer and glioma.11. A method of selectively killing or inhibiting the growth of a cancer stem cell comprising contacting the cancer stem cell with effective amount of a compound of .12. The method of claim 11 , wherein the cancer stem cell is mammalian.13. The method of claim 11 , wherein the cancer stem cell is human.14. The method of claim 11 , wherein the cancer stem cell is in vitro.15. The method of claim 11 , wherein the cancer stem cell in in vivo.16. The method of claim 11 , wherein cancer stem cell is of a cancer type selected from the group consisting of colon cancer claim 11 , breast cancer claim 11 , lung cancer claim 11 , liver cancer claim 11 , renal cancer and glioma.18. The method of claim 17 , wherein at least one of steps i) to vi) is conducted under microwave conditions in a batch reactor mode or a flow reactor mode.19. The method of wherein the protecting groups Z and Z′ and Y can be the same or different and are selected from the group consisting of 4-toluenesulfonyl claim 17 , methyl claim 17 , methoxymethyl claim 17 , benzoyl claim 17 , benzyl claim 17 , silyl (e.g. claim 17 , t-butyl-di-methyl-silyl claim 17 , etc.) claim 17 , p- ...

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Номер записи: 55
02-06-2022 дата публикации

METHODS OF PRODUCING MOGROSIDES AND COMPOSITIONS COMPRISING SAME AND USES THEREOF

Номер: US20220170063A1
Автор: BURGER Yosef, COHEN Shahar, DAVIDOVICH-RIKANATI Rachel, DORON-FAIGENBOIM Adi, ITKIN Maxim, KATZIR Nurit, LEWINSOHN Efraim, Oren Elad, Petreikov Marina, Portnoy Vitaly, Schaffer Arthur A., SHEN Shmuel, TADMOR Yaakov
Принадлежит: The State of Israel, Ministry of Agriculture & Rural Development, Agricultural Research Organization

Isolated mogroside and mogrol biosynthetic pathway enzyme polypeptides useful in mogroside biosynthesis are provided. Mogroside biosynthetic pathway enzymes of the invention include squalene epoxidase (SE), epoxy hydratase (EH), cytochrome p450 (Cyp), cucurbitadienol synthase (CDS) and udp-glucosyl-transferase (UGT), Also provided are methods of producing a mogroside using the isolated mogroside and mogrol biosynthetic enzyme polypeptides, the methods comprising contacting a mogrol and/or a glycosylated mogrol (mogroside) with at least one UDP glucose glucosyl transferase (UGT) enzyme polypeptide of the invention catalyzing glucosylation of the mogrol and/or the glucosylated mogrol to produce a mogroside with an additional glucosyl moietie(s), thereby producing the mogroside. Alternatively or additionally provided is a method of synthesizing a mogrol, the method comprising contacting a mogrol precursor substrate with one or more mogrol biosynthetic pathway enzyme polypeptides as described herein catalyzing mogrol synthesis from the mogrol precursor substrate, thereby synthesizing the mogrol. 1. A method of synthesizing a mogrol or mogrol precursor product from a mogrol precursor substrate , the method comprising contacting at least one mogrol precursor substrate with a mogroside pathway enzyme , wherein:(a) when said mogrol precursor product comprises diepoxy squalene and said mogrol precursor substrate comprises squalene or oxidosqualene, said mogroside pathway enzyme comprises a squalene epoxidase polypeptide at least 94% identical to SEQ ID NO: 14 or 89% identical to SEQ ID NO: 16, wherein said polypeptide catalyzes diepoxysqualene synthesis from squalene or oxidosqualene, thereby producing diepoxy squalene,(b) when said mogrol precursor product comprises 3 hydroxy, 24-25 epoxy cucurbitadienol and said mogrol precursor substrate comprises diepoxy squalene, said mogrol pathway enzyme comprises a cucurbitadienol synthetase polypeptide at least 60% homologous or ...

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Номер записи: 56
23-04-2015 дата публикации

Novel Ginsenoside Derivative Compounds And The Use Thereof In Protection Against Ischemia/Reperfusion Injury

Номер: US20150112048A1
Автор: CHAN Wai In, JIANG Zhihong, LIU LIANG, LUO Pei, WANG Jingrong, ZHOU Hua
Принадлежит: Macau University of Science and Tehnology

The present invention provides novel ginsenoside derivative compounds and the use thereof in protection against ischemia/reperfusion injury. 2. The ginsenoside derivative compound according to claim 1 , wherein R3 is represented by formula (II) and comprises stereocenters at C-20 and C-24 claim 1 , said stereocenter being either ‘R’ or ‘S’ in configuration.4. The ginsenoside derivative compound according to claim 2 , wherein said stereocenter at C-20 is ‘R’ in configuration; said compound is 3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-3β claim 2 ,12β claim 2 ,20(R) claim 2 ,24(S)-tetrahydroxydammar-25-ene and 24(R) epimer thereof claim 2 , and presented by formula (V).5. The ginsenoside derivative compound according to claim 1 , wherein R3 is represented by formula (II) and comprises a stereocenter at C-20 claim 1 , said stereocenter being either ‘R’ or ‘S’ in configuration.7. The ginsenoside derivative compound according to claim 5 , wherein said stereocenter is ‘R’ in configuration; said compound is 3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-3β claim 5 ,12β claim 5 ,20(R) claim 5 ,25-tetra-hydroxydammar-23-ene and presented by formula (VI).9. A method of synthesizing ginsenoside derivative compounds comprising steps of:a) providing a ginsenoside starting material;b) mixing said ginsenoside starting material with a stain;c) photosensitizing said mixture;d) filtrating said photosensitized mixturee) adding organophosphorus compound to said filtrate;f) drying the solution of step (e); andg) subjecting the solution of step (f) to combinative column chromatography to obtain said ginsenoside derivative compounds.10. The method according to claim 9 , wherein said step (c) further comprises irradiating the mixture with 400 W lamp under an oxygen atmosphere at room temperature for 10 h.11. The method according to claim 9 , wherein in said step (e) said organophosphorus compound is triphenylphosphine; and said step (e) further comprises stirring said filtrate at ...

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Номер записи: 57
02-04-2020 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS

Номер: US20200101087A1
Автор: "OBrien Rebecca", Altschul Randice Lisa, Arment Anthony, Kesel Andreas J., Rapkin Myron, Theise Neil David
Принадлежит:

This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease. 1. A method of treating a malignancy of the central nervous system in a patient comprising:selecting a patient in need of treating a malignancy of the central nervous system;administering to the patient at least one active agent selected from the group consisting of PT150, PT155, PT156, PT157, PT158, TCY1, combinations thereof, and pharmaceutically acceptable salts thereof,wherein the malignancy of the central nervous system is selected from the group consisting of pancreatic cancer, astrocytomas, oligodendroglioma, glioblastoma, medulloblastoma, brain cancer, neuroblastoma, ganglioneuroblastoma, malignant nerve sheathe tumors, and combinations thereof,thereby treating said malignancy of the central nervous system.2. The method of wherein the active agent is in a pharmaceutical composition comprising:a therapeutically effective amount of one or more of PT150, PT155, PT156, PT157, PT158, TCY1, combinations thereof, and pharmaceutically acceptable salts thereof; andat least one pharmaceutically acceptable excipient.3. The method of wherein the pharmaceutical composition is in a dosage form selected from the group consisting of a minicapsule claim 2 , a capsule claim 2 , a smart capsule claim 2 , a tablet claim 2 , an implant claim 2 , a troche claim 2 , a lozenge claim 2 , a minitablet claim 2 , a temporary or permanent suspension claim 2 , an injectable claim 2 , an ovule claim 2 , a suppository claim 2 , a wafer claim 2 , a chewable tablet claim 2 , a quick or fast dissolving tablet claim 2 , an effervescent tablet claim 2 , a buccal or sublingual solid claim 2 , a granule claim 2 , a film claim 2 , a sprinkle claim 2 , a pellet claim 2 , a ...

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Номер записи: 58
09-06-2022 дата публикации

SERIES OF HALOGENATED TETRACYCLIC TRITERPENE DERIVATIVES AND THEIR PREPARATION AND APPLICATION

Номер: US20220177511A1
Автор: LIU Xia, SUN Qingyan, YUAN Hu, Zhang Weidong
Принадлежит:

The invention provides a series of halogenated tetracyclic triterpene derivatives and their preparation and application. It is represented by the following general structural formula: 5. The preparation method according to is characterized in that: Parikh Doering oxidation described in step a employs sulfur trioxide pyridine complex/dimethyl sulfoxide/triethylamine system and uses solvents selected from dimethyl sulfoxide claim 4 , toluene claim 4 , xylene claim 4 , tetrahydrofuran claim 4 , 2-methyltetrahydrofuran claim 4 , ethyl acetate claim 4 , dichloromethane claim 4 , dichloroethane or chloroform claim 4 , preferably dimethyl sulfoxide or dichloromethane. The molar ratio of compound 5 to sulfur trioxide pyridine is 1:1-1:15 claim 4 , preferably 1:4. The reaction temperature is −20° C.-100° C. claim 4 , preferably 0° C.-30° C. claim 4 , particularly 5° C.-20° C.6. The preparation method according to is characterized in that the cadmium reagent is selected from Jones oxidant claim 4 , pyridinium chlorochromate or pyridinium dichlorochromate. The solvent of the reaction is selected from toluene claim 4 , xylene claim 4 , tetrahydrofuran claim 4 , 2-methyltetrahydrofuran claim 4 , ethyl acetate claim 4 , dichloromethane claim 4 , dichloroethane or chloroform claim 4 , preferably dichloromethane. The molar ratio of compound 5 to the oxidizing agent is 1:1-1:15 claim 4 , preferably 1:2. The reaction temperature is −10° C.-100° C. claim 4 , preferably 10° C.-60° C. claim 4 , particularly 15° C.-25° C.7. The preparation method according to is characterized in that: The Pfitzner-Moffatt oxidation uses a carbodiimide/dimethyl sulfoxide/acid system. The carbodiimide is selected from dicyclohexylimide or 1-ethyl-3(3-dimethylpropylamine) carbodiimide. The acid is selected from orthophosphoric acid claim 4 , dichloroacetic acid and strong acid salt of pyridine (such as pyridine hydrochloride claim 4 , pyridine trifluoroacetate claim 4 , etc.). The solvent is selected from ...

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Номер записи: 59
09-04-2020 дата публикации

CARBONATED BEVERAGE AND METHOD FOR CARBONATION ENHANCEMENT

Номер: US20200109163A1
Автор: Gomez Richard, JAJA-CHIMEDZ Asha, John Thumpalasseril V., KIM Jung-a, Li Xiaodong, SALAS SANTOS Roberto, Tang Xiao-Qing, Wu Hou
Принадлежит:

Compositions and methods for enhancing carbonation effect in food consumables are provided. 3. The method of claim 1 , wherein the compound is β-sitosterol claim 1 , stigmasterol claim 1 , chenodeoxycholic acid or CHAPS.4. The method of claim 1 , wherein the olfactory effective amount is about 1 part per trillion or greater by weight.5. The method of claim 1 , wherein the olfactory effective amount is from about 1 part per billion to about 100 parts per million by weight.6. The method of claim 1 , wherein the carbonated beverage is selected from the group consisting of a carbonated water claim 1 , a mineral water claim 1 , a soda claim 1 , a beer claim 1 , a sparkling wine and a Champagne.9. The carbonated beverage of claim 7 , wherein the compound is R-sitosterol claim 7 , stigmasterol claim 7 , chenodeoxycholic acid or CHAPS. This application is a Continuation-in-Part application of U.S. application Ser. No. 16/083,641, filed Sep. 10, 2018, which is a National Phase Application of PCT/US2017/019903, filed Feb. 28, 2017, which claims benefit of priority from U.S. Provisional Application Ser. No. 62/302,418, filed Mar. 2, 2016 and 62/324,385, filed Apr. 19, 2016, the contents of which are incorporated herein by reference in their entireties.There is an ongoing need in the flavor industry for taste modifying compounds that improve, enhance or modify flavors for food preparations. Those with skill in the art appreciate how differences in the chemical structures of the molecules can result in significant differences in functions. The identification of structural variations and discovery of new compounds enable the creation of new flavors.Phytosterols occur in plants and encompass sterols and stanols. Stanols are saturated forms of corresponding sterols. Phytosterols are steroid compounds similar to cholesterol. They are poorly absorbed and can compete with cholesterol for absorption in the intestine, resulting lower levels of cholesterol. Phytosterol-enriched foods and ...

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Номер записи: 60
03-05-2018 дата публикации

System and Method for Diagnosis and Treatment

Номер: US20180117066A1
Автор: Myron Rapkin, Neil David THEISE, Randice Lisa Altschul, Rebecca O'brien
Принадлежит: Pop Test Oncology LLC

This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease.

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Номер записи: 61
17-07-2014 дата публикации

Method for the Production of Fluoromethyl Esters of Androstan-17 beta Carboxylic Acids

Номер: US20140200341A1
Автор: Leitao Emilia Perpetua Tavares, Maycock Christopher, Ventura Maria Rita
Принадлежит: HOVIONE INTER LIMITED

Described herein are processes for the preparation of monofluoromethylated organic biologically active compounds, starting from protected intermediates and/or reagents to obtain compounds such as fluticasone propionate and fluticasone furoate, in presence of decarboxylating reagents XeFand BrF, or using FCHSH as a reagent. 2. A method according to claim 1 , wherein:{'sub': '1', 'Ris selected from a group consisting of hydroxyl, propionate and furoate; and/or'}{'sub': '2', 'Ris selected from a group consisting of H and methyl; and/or'}{'sub': '3', 'Ris (tert-butylcarboxy)methyl; and/or'}{'sub': '4', 'Ris trifluoroacetate or trichloroacetate; and/or'}{'sub': 1', '2, 'X═X═F; and/or'}{'sub': '3', 'Xis S.'}3. A method according to claim 1 , wherein the fluorodecarboxylating agent is selected from XeFand BrF.4. A method according to claim 1 , wherein the organic biologically active of formula (I) is chosen from a group consisting of Fluticasone claim 1 , Fluticasone Propionate and Fluticasone Furoate.9. A method of making an organic biologically active compound containing a “—CHF” moiety of claim 1 , wherein a compound of formula (III) is used.10. The method according to claim 1 , wherein the organic biologically active compound is a compound of formula (I) as defined in .11. The method according to claim 10 , wherein the compound of formula (I) is Fluticasone claim 10 , Fluticasone Propionate or Fluticasone Furoate.12. A method according to claim 2 , wherein the fluorodecarboxylating agent is selected from XeFand BrF.13. A method according to claim 2 , wherein the organic biologically active of formula (I) is chosen from a group consisting of Fluticasone claim 2 , Fluticasone Propionate and Fluticasone Furoate.14. A method according to claim 3 , wherein the organic biologically active of formula (I) is chosen from a group consisting of Fluticasone claim 3 , Fluticasone Propionate and Fluticasone Furoate.15. A method of making an organic biologically active compound ...

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Номер записи: 62
04-05-2017 дата публикации

HIGH INTENSITY SWEETENERS

Номер: US20170119032A1
Автор: Colquitt Justin, Gonsalves Nicole, Hammaker Jeffrey R., Manam Rama, Noriega Chris Edano, Patron Andrew, Servant Nicole
Принадлежит:

Disclosed herein are compounds having structural Formula (I), or salts thereof. These compounds are useful as sweet tasting agents and/or sweetness enhancers. Also disclosed are compositions comprising the present compounds and methods of increasing the sweet taste of ingestible compositions. Furthermore, methods for preparing the compounds are also disclosed. 12-. (canceled)4. The composition of claim 3 , comprising less than 1% by weight of Mogroside III.5. (canceled)6. (canceled)7. The composition of claim 3 , comprising less than 0.3% by weight of 11-oxo-Mogroside III.811-. (canceled)12. The composition of claim 3 , comprising less than 1% by weight of all isomers of Mogroside I claim 3 , Mogroside II claim 3 , and Mogroside III.1315-. (canceled)16. The composition of claim 3 , comprising less than 1% by weight of 11-oxo-mogrol.1719-. (canceled)20. The composition of claim 3 , comprising greater than 70% by weight of the compound.2124-. (canceled)25. The composition of claim 3 , wherein the compound is in amorphous form.26. The composition of claim 3 , wherein the compound is coating a solid carrier.27. The composition of claim 26 , wherein the solid carrier are particles selected from the group consisting of lactose claim 26 , cellulose claim 26 , microcrystalline cellulose claim 26 , modified food starch claim 26 , gum Arabic claim 26 , maltodextrin claim 26 , modified corn starch claim 26 , dextrose claim 26 , xantham gum claim 26 , carboxymethylcellulose claim 26 , cellulose gel claim 26 , cellulose gum claim 26 , sodium caseinate claim 26 , carrageenan claim 26 , and combinations thereof.28. The composition of claim 25 , wherein the composition is in particulate form.29. The composition of claim 28 , wherein the composition has an average particle size between 50 μm and 300 μm.3031-. (canceled)32. A composition claim 3 , comprising solid particles of the composition of and a liquid carrier.33. The composition of claim 32 , wherein the solid particles are ...

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Номер записи: 63
10-05-2018 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20180125866A1
Автор: Qian Xiangping
Принадлежит:

Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. 131.-. (canceled)33. The method of claim 32 , wherein the subject is a human.34. The method of claim 32 , wherein the compound or the pharmaceutically acceptable salt is administered orally claim 32 , subcutaneously claim 32 , intravenously claim 32 , intranasally claim 32 , transdermally claim 32 , intraperitoneally claim 32 , intramuscularly claim 32 , intrapulmonary claim 32 , vaginally claim 32 , rectally claim 32 , or intraocularly.35. The method of claim 32 , wherein the compound or the pharmaceutically acceptable salt is administered intravenously.36. The method of claim 32 , wherein the compound or the pharmaceutically acceptable salt is administered orally.37. The method of claim 32 , further comprising administering to the subject an additional anti-cancer and/or cytotoxic agent.38. The method of claim 37 , wherein the additional anti-cancer and/or cytotoxic agent is administered simultaneously with the compound or the pharmaceutically acceptable salt.39. The method of claim 32 , wherein the amount of the compound or the pharmaceutically acceptable salt administered is in the range of 0.01 mg to 100 mg per kilogram body weight of the subject.40. The method of claim 32 , wherein amount of the compound of Formula I administered is in the range of about 0.01 mg to 1000 mg.41. The method of claim 32 , wherein Rand Rare each independently chosen from hydrogen and optionally substituted lower alkyl.42. The method of claim 32 , wherein Rand Rare both hydrogen.43. The method of claim 32 , wherein Rand Rare joined together to form a 5- to 7-membered heterocycloalkyl ring.44. The method of claim 32 , wherein each Rand Ris independently chosen from hydrogen and optionally substituted lower alkyl.45. The method of claim 32 , wherein n is chosen from 1 claim 32 , 2 claim 32 , and 3.46. The method of claim 32 , wherein n is 1 claim 32 , and Rand ...

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Номер записи: 64
23-04-2020 дата публикации

COMPOSITION COMPRISING NOVEL GINSENOSIDE

Номер: US20200123194A1
Автор: Hong Yong Deog, Jeong Hyun Woo
Принадлежит: AMOREPACIFIC CORPORATION

The present specification relates to a composition containing novel ginsenoside, (20S,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20,24-epoxy-6a,12b,25-triol, a pharmaceutically acceptable salt thereof, a hydrate or a solvate thereof as an active ingredient. The composition exhibits excellent effects in glycemic control, lipid metabolic control, cholesterol control, anti-obesity and blood circulation improvement. 1. A method for one or more of metabolic control and blood circulation improvement comprising administering to a subject in need thereof an effective amount of (20S ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 ,24-epoxy-6a ,12b ,25-triol , a pharmaceutically acceptable salt thereof , a hydrate or a solvate thereof.3ginseng. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol is extracted from seed.4. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a hydrate or a solvate thereof lowers blood sugar.5. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a hydrate or a solvate thereof inhibits glycolysis in the blood.6. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a hydrate or a solvate thereof promotes cellular uptake of glucose in the blood.7. The method of claim 1 , wherein the method comprises preventing or treating diabetes or diabetic ...

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Номер записи: 65
23-04-2020 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20200123195A1
Автор: Griffin Andrew, Harrison Boyd L., LA Daniel, Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R, R, R, R, R, R, and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 2. The compound of claim 1 , wherein Ris alkyl.36-. (canceled)7. The compound of claim 1 , wherein Ris hydrogen or alkyl.8. The compound of claim 1 , wherein Ris unsubstituted C-Calkyl or C-Chaloalkyl.912-. (canceled)13. The compound of claim 1 , wherein wherein Ris unsubstituted C-Calkyl claim 1 , C-Chaloalkyl claim 1 , carbocyclyl claim 1 , carbocyclylalkyl claim 1 , aralkyl claim 1 , or heterocyclylalkyl.1426-. (canceled)27. The compound of claim 1 , wherein Ris aryl or heteroaryl and Ris hydrogen.28. The compound of claim 1 , wherein Ris carbocyclyl or heterocyclyl and Ris hydrogen.2930-. (canceled)31. The compound of claim 1 , wherein Rand R claim 1 , together with the carbon atom to which they are attached form a 3-8 membered carbocyclic or heterocyclic ring.3233-. (canceled)3540-. (canceled)4247-. (canceled)4836. The compound of claim claim 1 , wherein each of Rand Ris independently hydrogen or alkyl.49. The compound of claim 1 , wherein each of Rand Ris independently hydrogen or C-Chaloalkyl.5059-. (canceled)6162-. (canceled)64. A pharmaceutical composition comprising a compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.65. A method for treating or preventing a disorder described herein claim 1 , comprising administering to a subject in need thereof an effective amount of a compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , or pharmaceutical composition thereof.66. The method according to claim 65 , wherein the disorder is a gastrointestinal (GI) disorder claim 65 , structural disorders affecting the GI claim 65 , anal disorders claim 65 , colon polyps claim 65 , ...

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Номер записи: 66
17-05-2018 дата публикации

POSITIVE ALLOSTERIC MODULATORS OF SWEET TASTE

Номер: US20180132516A1
Автор: BOYLE Sean Michael, RAY Anandasankar
Принадлежит:

The invention provides natural allosteric modulators that are useful as sweet flavor enhancers. The present invention also includes ingestible compositions comprising the present compounds and methods of enhancing the sweet taste of sweeteners and sugars. 1. A composition comprising an isolated sweet taste modulator compound selected from the compounds in Table 1 , and derivatives thereof , wherein said composition further comprises at least one sweetener.2. An ingestible composition comprising a composition of and an acceptable carrier for ingestion.3. The ingestible composition of claim 1 , wherein the sweetener is selected from natural caloric sweeteners claim 1 , natural high-potency sweeteners claim 1 , and synthetic sweeteners.4. The ingestible composition of claim 2 , which has an enhanced sweet taste as compared to an ingestible composition that does not have a compound from Table 1 claim 2 , or a derivative thereof claim 2 , but is otherwise the same.5. The ingestible composition of claim 2 , wherein the ingestible composition is a food claim 2 , beverage claim 2 , pharmaceutical claim 2 , nutraceutical claim 2 , tobacco claim 2 , or oral hygiene/cosmetic product.6. A flavoring concentrate formulation comprising a composition of and a carrier. This application claims the priority benefit of U.S. Provisional Application Ser. No. 62/423,001, filed Nov. 16, 2016, which is incorporated herein by reference in its entirety.Living things use sensory systems to detect important information about the environment in which they live. Taste is a particularly important sensory system, and is one of the most sophisticated forms of chemically-triggered sensations found throughout the animal kingdom.Mammals are believed to have five basic taste modalities: sweet, bitter, sour, salty, and umami (savory). The pleasant taste associated with sweetness is important in industries that produce consumable materials. Natural sugars, such as sucrose, fructose, and glucose, for ...

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Номер записи: 67
09-05-2019 дата публикации

Method for Extracting High-Purity Mogroside V from Siraitia Grosvenorii

Номер: US20190133166A1
Автор: HUANG Huaxue, Long Weian
Принадлежит:

The present application relates to a technique for extracting mogroside V. Provided is a method for extracting high-purity mogroside V from . The specific steps comprise: pre-treatment of a raw material, extraction, centrifugation, enzymolysis, ultrafiltration, nanofiltration, decolorization, concentration, microwave drying, and pulverization. The invention utilizes a membrane-based technique for separation and purification, and only uses pure water as a solvent to eliminate usage of an organic solvent. The method can be easily performed, has a simple process, and provides a safe, environment-friendly, high quality, and low-cost product. The method can be used to realize continuous large-scale industrial production. 1. A preparation method for extracting high-purity mogroside V from Luo Han Guo , characterized in that , the method comprises the following steps:(1) pre-treatment of raw material: crushing a raw material by using a crusher in accordance with the standard of one fresh fruit being broken into 6 to 10 pieces;(2) extraction: by means of continuous countercurrent extraction method, subjecting the raw material obtained in step (1) to hot water continuous countercurrent extraction to extract mogroside V; and passing the extracted liquid through a 200 to 400-mesh stainless steel sieve to obtain a filtrate;(3) centrifugation: subjecting the filtrate obtained in step (2) to centrifugal filtration to obtain a centrifugate;(4) enzymolysis: cooling down the centrifugate obtained in step (3), subsequently delivering it to an enzymolysis tank, and adding an enzyme reagent therein to perform enzymolysis;(5) ultrafiltration: passing the enzymatic centrifugate obtained in step (4) through an ultrafiltration membrane to concentrate to small-volume solution, adding water therein to perform dialysis until the conductivity of the solution meeting the requirement, and obtaining a filtrate;(6) nanofiltration: using a nanofiltration membrane to separate and purify the filtrate ...

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Номер записи: 68
09-05-2019 дата публикации

PHARMACEUTICAL COMPOSITIONS AND METHODS

Номер: US20190134062A1
Автор: "OBrien Rebecca", Altschul Randice Lisa, Arment Anthony, Kesel Andreas J., Rapkin Myron, Theise Neil David
Принадлежит:

This invention relates the use of cortisol blockers (e.g., glucocorticoid receptor [GR] antagonists) for the treating or preventing viral infections, treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease. 1. A method of treating and/or preventing a viral condition in a patient comprising:selecting a patient in need of treating and/or preventing a viral condition;administering to the patient at least one active agent selected from the group consisting of PT150, PT155, PT156, PT157, PT158, TCY1, combinations thereof, and pharmaceutically acceptable salts thereof;administering at least one additional active agent selected from the group consisting of other molecules with potential to bind viral glucocorticoid response elements (GREs), retinazone, RU486, derivatives thereof,wherein the viral condition is to prevent or eliminate acute viral infection, to diminish intensity of viral infection, to diminish length of viral infection, to speed time to resolution and healing of viral infection, to speed time to suppression of viral infection, to increase likelihood of viral eradication, and/or to diminish infectivity of viral infection, with Hepatitis C virus, Bovine Viral Diarrhea virus, Ebola-like viruses, Hepatitis B virus, Mouse mammary tumor virus, Human Immunodeficiency Virus-1 (HIV-1), Varicella-Zoster virus (chicken pox; VZV), Cytomegalovirus (CMV), Human Herpes Virus-6 (HHV-6), Human Herpes Virus-7 (HHV-7), Kaposi's Sarcoma-Associated Herpes virus (or Human Herpes Virus-8; HHV-8), Variola (Small Pox) virus, Vaccinia virus, Cowpox virus, Monkeypox virus.2. A method of treating and/or preventing a viral condition in a patient comprising:selecting the patient in need of treating and/or preventing a viral condition;administering at least one active agent selected from the group consisting of PT150, PT155, PT156, PT157, PT158, TCY1, combinations ...

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Номер записи: 69
07-08-2014 дата публикации

One-pot synthesis of alpha/beta-o-clycolipids

Номер: US20140221633A1
Автор: Jacquelyn Gervay-Hague, Matthew Schombs, Suvarn S. Kulkarni, Wenjun Du
Принадлежит: The Regents of the University of California

The present invention provides a one-pot method of preparing an unprotected α-O-glycolipid. The first step involves contacting a protected α-iodo sugar with a catalyst and a lipid comprising a hydroxy group, under conditions sufficient to prepare a protected α-O-glycolipid. The second step involves deprotecting the protected α-O-glycolipid under conditions sufficient to prepare the unprotected α-O-glycolipid, wherein the contacting and deprotecting steps are performed in a single vessel. The present invention also provides a one-pot method of preparing an unprotected β-O-glycolipid following the steps for the preparation of the unprotected α-O-glycolipid.

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Номер записи: 70
30-04-2020 дата публикации

COMPOSITION FOR ENHANCING EXERCISE ABILITY OR ANTI-FATIGUE COMPRISING NOVEL GINSENOSIDE

Номер: US20200131222A1
Автор: Hong Yong Deog, Jeong Hyun Woo
Принадлежит: AMOREPACIFIC CORPORATION

The present specification relates to a composition containing novel (20S,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20,24-epoxy-6a,12b,25-triol, a pharmaceutically acceptable salt thereof, a hydrate or a solvate thereof as an active ingredient. The composition exhibits an excellent exercise ability enhancing effect and anti-fatigue effect. 1. A method of enhancing exercise ability or anti-fatigue comprising administering to a subject in need thereof an effective amount of (20S ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 ,24-epoxy-6a ,12b ,25-triol , a pharmaceutically acceptable salt thereof , a hydrate or a solvate thereof.3ginseng. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol is extracted from seed.4. The method of claim 1 , wherein the method is for one or more of muscle regeneration promotion claim 1 , muscle augmentation claim 1 , muscle strengthening claim 1 , the prevention or improvement of sarcopenia claim 1 , and fatigue recovery promotion and lactic acid metabolism control.5. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a hydrate claim 1 , or a solvate thereof promotes the production of mitochondria in myocytes.6. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 ,25-triol claim 1 , a pharmaceutically acceptable salt thereof claim 1 , a hydrate claim 1 , or a solvate thereof promotes the fatty acid oxidation in myocytes.7. The method of claim 1 , wherein the (20S claim 1 ,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20 claim 1 ,24-epoxy-6a claim 1 ,12b claim 1 , ...

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Номер записи: 71
24-05-2018 дата публикации

19-NOR C3, 3-DISUBSTITUTED C21-C-BOUND HETEROARYL STEROIDS AND METHODS OF USE THEREOF

Номер: US20180141971A1
Автор: Beresis Richard T., Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert J., Salituro Francesco G.
Принадлежит:

Provided herein are 19-nor C3,3-disubstituted steroids of Formula (I): 3. The method of claim 1 , wherein Ris —CH claim 1 , —CHCH claim 1 , —CHF claim 1 , —CHF claim 1 , —CF claim 1 , —CHOCH claim 1 , or substituted or unsubstituted cyclopropyl.4. The method of claim 3 , wherein Ris —CH.5. The method of claim 1 , wherein Ris —OH claim 1 , —OCH claim 1 , —OCHCH claim 1 , —OCHCHCH claim 1 , —CH claim 1 , —CHCH claim 1 , —CHCHCH claim 1 , substituted or unsubstituted cyclopropyl claim 1 , fluoro claim 1 , or chloro.6. The method of claim 1 , wherein Ris H.7. The method of claim 1 , wherein Rand Rare both hydrogen.8. The method of claim 1 , wherein Rand Rare joined to form ═O (oxo).9. The method of claim 1 , wherein represents a double bond claim 1 , and Ris hydrogen claim 1 , fluoro claim 1 , —CH claim 1 , or —CF.10. The method of claim 1 , wherein represents a single bond claim 1 , and both of Rand Rare hydrogen.11. The method of claim 1 , wherein represents a single bond claim 1 , and both of Rand Rare —CHor —CF.12. The method of claim 1 , wherein represents a single bond claim 1 , and both of Rand Rare fluoro.13. The method of claim 1 , wherein represents a single bond claim 1 , and Ris substituted or unsubstituted Calkyl claim 1 , or halogen claim 1 , and Ris hydrogen.14. The method of claim 13 , wherein Ris fluoro.15. The method of claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris hydrogen.16. The method of claim 1 , wherein at least one of R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris substituted or unsubstituted Calkyl claim 1 , —COR claim 1 , —C(═O)R claim 1 , —CN claim 1 , —NO claim 1 , or halogen claim 1 , wherein Ris substituted or unsubstituted Calkyl.17. The method of claim 16 , wherein at least one of R claim 16 , R claim 16 , R claim 16 , R claim 16 , and Ris substituted or unsubstituted —CH.18. The method of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare hydrogen.22. A method ...

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Номер записи: 72
25-05-2017 дата публикации

COMPOUNDS COMPRISING ONE OR MORE HYDROPHOBIC DOMAINS AND A HYDROPHILIC DOMAIN COMPRISING PEG MOIETIES, USEFUL FOR BINDING CELLS

Номер: US20170146533A1
Автор: Froehlich Thomas, Froehner Stefanie, Heindl Dieter, Josel Hans-Peter
Принадлежит:

The present invention relates to novel compounds comprising one or more hydrophobic domains and a hydrophilic domain comprising PEG moieties, useful for binding cells, as well as uses and compositions related thereto. The compounds are useful for immobilizing and/or stabilizing cells. 1. A compound comprising one or more hydrophobic domains and a hydrophilic domain ,wherein the one or more hydrophobic domains are covalently bound to said hydrophilic domain, andwherein the one or more hydrophobic domains each comprise a linear lipid, a steroid or a hydrophobic vitamin, and {'br': None, 'sub': n', 'k1', 'n', 'k2, 'X1-[A1-(L1)]-Z-[A2-(L1)]-X2 \u2003\u2003(I),'}, 'wherein the hydrophilic domain comprises a compound of Formula (I)wherein{'sub': 2', '2, 'Z is linear polyethylene glycol (PEG) moiety containing 1 to 100 —O—CH—CH— moieties, wherein the polyethylene glycol moiety optionally comprises 1 or more spacer moieties SP connecting two'}{'sub': 2', '2, '—O—CH—CH— moieties, and wherein the linear PEG moiety optionally comprises a linker moiety L3 at one or both ends,'}each L1 is a linker moiety selected independently from each other,each n is either 0 or 1, selected independently from each other,A1 and A2 are bifunctional or trifunctional moieties selected independently from each other, with the proviso that at least one Al or A2 is trifunctional,k1 and k2 are integers between 0 and 10, selected independently from each other, with the proviso that at least one of k1 and k2 is not 0,X1 and X2 are independently selected from hydrogen or a protecting group,L3 is independently selected from a linear alkyl or alkenyl chain with 1 to 10 C atoms, which is optionally (i) interrupted by 1 to 3 N, O or S atoms, and/or (ii) substituted by 1 to 4 hydroxyl, carbonyl, amino or thiol groups,andwherein the one or more hydrophobic domains are covalently bound to said hydrophilic domain via the trifunctional domain(s),or a salt thereof.2. The compound according to claim 1 , wherein Z ...

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Номер записи: 73
07-05-2020 дата публикации

SWEETENING COMPOSITIONS AND PROCESSES FOR PREPARING THEM

Номер: US20200138063A1
Автор: FUSHENG Lan, LYNDON Rex Murray, MILLER Christopher John, SMITH Garth Selwyn
Принадлежит: GUILIN GFS MONK FRUIT CORP.

The invention relates to sweetening compositions obtained from the Luo Han Guo fruit, a member of the Cucurbiticeae family. The compositions are free of bitter-tasting impurities, have a light colour and contain about 16-75% mogroside V and about 30-95% total terpene glycosides on a dry weight basis. A filtered (0.2 μm) solution of the composition in water with a solids content of 1% w/v has an absorbance at 420 nm of about 0.55 or below. Also disclosed is a method of preparing such compositions which includes a heating step to encourage the formation of melanoidins, highly coloured impurities, thereby permitting their removal by filtration providing a lighter coloured product. 1. A sweetening composition , the composition containing from about 16% to about 75% mogroside V and from about 30% to about 95% total terpene glycosides on a dry weight basis , and wherein a filtered (0.2 μm) solution of the composition in water having a solids content of 1% w/v has an absorbance at 420 nm of about 0.55 or below.2. A composition according to claim 1 , wherein the terpene glycosides in the composition are naturally occurring terpene glycosides obtained from fruit of the Cucurbitaceae family.3. (canceled)4. (canceled)5. A composition according to claim 1 , wherein the composition contains from about 20% to about 70% mogroside V and from about 40% to about 90% total terpene glycosides claim 1 , on a dry weight basis.68-. (canceled)9. A composition according to claim 1 , wherein the absorbance at 420 nm of a filtered (0.2 μm) solution of the composition in water having a solids content of 1% w/v is less than about 0.5.1016-. (canceled)17. A sweetening composition comprising:(a) a first component containing from about 16% to about 75% mogroside V and from about 30% to about 95% total terpene glycosides on a dry weight basis, and wherein a filtered solution (0.2 μm) of the first component in water having a solids content of 1% w/v has an absorbance at 420 nm of about 0.55 or below ...

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Номер записи: 74
01-06-2017 дата публикации

METHODS OF EXTRACTION AND PURIFICATION OF LUO HAN GUO MOGROSIDE V, NATURAL SWEETENER COMPOSITIONS THEREWITH AND USES OF SAID COMPOSITION

Номер: US20170150745A1
Автор: Li Cunbiao Kevin, Zhang Yong Luke
Принадлежит:

A method for purifying Mogroside V comprises passing a solution of a pre-prepared primary extract through a multi-column system including a plurality of columns, in series, packed with a porous adsorbent resin to provide at least one column having adsorbed mogrosides and eluting fractions with Mogroside V content from the at least one column having absorbed mogrosides to provide an eluted solution with Mogroside V content. 1Siraitia grosvenori. A method for purifying Mogroside V comprises passing a solution of a pre-prepared primary extract through a multi-column system including a plurality of columns , in series , packed with a porous adsorbent resin to provide at least one column having adsorbed mogrosides and eluting fractions with Mogroside V content from the at least one column having absorbed mogrosides to provide an eluted solution with Mogroside V content (an intermediate Mogroside V extract).2. The method of claim 1 , wherein the plurality of columns is at least two columns.3. The method of claim 1 , wherein the plurality of columns is at least three columns4. The method of claim 1 , wherein the plurality of columns is four columns.5Siraitia grosvenoriSiraitia grosvenori. The method of claim 1 , wherein pre-prepared primary extract is prepared by i) providing fruit of a plant claim 1 , ii) washing and mashing the fruit (while removing seeds) to produce mashed fruit claim 1 , iii) saccharifying the mashed fruit to hydrolyze polysaccharides claim 1 , extracting saccharified matter claim 1 , filtering and concentrating the extract claim 1 , and iv) centrifuging the extract claim 1 , such extract being preparable for passage claim 1 , as a feed liquor claim 1 , through the plurality of columns claim 1 , in series claim 1 , packed with the porous adsorbent resin.6. The method of claim 1 , which comprises further processing of the intermediate Mogroside V extract to remove one or more of colour claim 1 , salt and impurities by a means selected from the group ...

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Номер записи: 75
17-06-2021 дата публикации

GLUCOCORTICOID INHIBITORS FOR TREATMENT OF PROSTATE CANCER

Номер: US20210179660A1
Автор: Arora Vivek, Evans Michael J., Sawyers Charles L., Veach Darren R.
Принадлежит:

The present invention encompasses the recognition that reproducible and detectable changes in the level and or activity of Glucorticoid Receptor (GR) are associated with incidence and/or risk of Castration Resistant Prostrate Cancer (CRPC) and/or doubly resistant prostrate cancer, especially in individuals having prostrate cancer and on antiandrogen therapy, and provides for the use of GR inhibitors to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer. In some embodiments, GR inhibitors also have Androgen Receptors (AR) inhibitory activity and or administered in conjunction with AR Inhibitors. The present invention also provides technologies for identification and/or characterization of agents to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer; in some embodiments such agents alter level and/or activity of a GR. In some embodiments, provided agents show effects on a GR's activity of regulating transcription of one or more target genes. The present invention also provides systems for using such agents, for example to treat and/or reduce risk of CRPC and/or doubly resistant prostrate cancer. 1195-. (canceled)197. The compound of claim 196 , wherein Ris selected from the group consisting of ethyn-1-yl claim 196 , 1-propyn-1-yl claim 196 , 1-butyn-1-yl claim 196 , ethen-1-yl claim 196 , 1-propen-1-yl claim 196 , and 1-buten-1-yl.198. The compound of claim 196 , wherein Ris 1-propyn-1-yl.202. A pharmaceutical composition comprising a compound of claim 196 , or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present application is a divisional application of U.S. patent application Ser. No. 15/103,283, filed Jun. 9, 2016, which is the national phase entry of PCT App. No. PCT/US14/69854, filed Dec. 11, 2014, which claims priority to U.S. Provisional Application No. 61/914,917, filed Dec. 11, 2013, the entirety of each of which is incorporated herein by reference.This invention ...

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Номер записи: 76
17-06-2021 дата публикации

Intermediates for the Synthesis of Bile Acid Derivatives, in Particular of Obeticholic Acid

Номер: US20210179661A1
Автор: Alexander Weymouth-Wilson, Carl OTTER, Ieuan DAVIES, Laura WALLIS, Rhys BATCHELOR, Timothy Evans, Zofia KOMSTA
Принадлежит: Nzp Uk Ltd

The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): wherein: , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.

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Номер записи: 77
09-06-2016 дата публикации

Compounds and methods involving sterols

Номер: US20160159848A1
Автор: Damodaragounder GOPAL, Jerbrena C. Jacobs, Ke-Qing LING, Marco Burello, Roger E. Harrington
Принадлежит: WARSAW ORTHOPEDIC INC

Compounds and methods of synthesizing oxysterols are provided. The compounds and methods provided allow the oxysterol to be safely produced at a high yield. The compounds and methods provided can produce the oxysterol in a stereoselective manner.

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Номер записи: 78
07-06-2018 дата публикации

AGROCHEMICAL-FREE SIRAITIA GROSVENORII EXTRACT, AND METHOD FOR PREPARING SAME

Номер: US20180153201A1
Автор: CHI Keika, ITO Yuta, KUNISHIMA Takashi, MURATA Yuji
Принадлежит: Saraya Co., Ltd.

A extract preparation method is provided herein that removes an agrochemical selectively and efficiently from a extract containing the agrochemical. The method further comprises collecting with high yield a glycoside, a substance useful as a sweetener component. 1Siraitia GrosvenoriiSiraitia Grosvenorii. A method for preparing an agrochemical-free extract , comprising the step of treating an agrochemical-containing extract with an activated carbon to remove an agrochemical therein ,wherein the activated carbon used in the activated carbon treatment is at least one activated carbon selected from the group consisting of an activated carbon having an iodine adsorption amount of at least 1500 mg/g, and an activated carbon having a caramel decolorizing ability of at least 85%, and{'i': 'Siraitia Grosvenorii', 'the recovery ratio of glycosides according to the activated carbon treatment is at least 70%, the glycosides being mogroside V, mogroside IV, 11-oxo-mogroside V, and siamenoside I.'}2Siraitia GrosvenoriiSiraitia Grosvenorii. The method according to claim 1 , wherein the total amount of mogroside V claim 1 , mogroside IV claim 1 , 11-oxo-mogroside V claim 1 , and siamenoside I comprised in the agrochemical-free extract is at least 33% by weight per 100% by weight of the agrochemical-free extract.3. The method according to claim 1 , wherein the agrochemical is at least one selected from the group consisting of dimethomorph claim 1 , triadimenol claim 1 , tebuconazole claim 1 , difenoconazole claim 1 , metalaxyl claim 1 , and metalaxyl M.6Siraitia Grosvenorii. The agrochemical-free extract according to claim 5 , wherein the peak which is detected by the HPLC analysis and which is near the retention time of 16 minutes is a peak of a compound having a molecular weight of 358 daltons.7Siraitia Grosvenorii. The agrochemical-free extract according to claim 5 , wherein the agrochemical is dimethomorph claim 5 , triadimenol claim 5 , tebuconazole claim 5 , difenoconazole ...

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Номер записи: 79
23-05-2019 дата публикации

SYSTEM AND METHOD FOR DIAGNOSIS AND TREATMENT

Номер: US20190151335A1
Автор: "OBrien Rebecca", Altschul Randice Lisa, Rapkin Myron, Theise Neil David
Принадлежит:

This invention relates the use of cortisol blockers (glucocorticoid receptor [GR] antagonists) for the treating or preventing treatment resistant prostate cancer, treating or preventing neoplasia, and treating or preventing infection related to acute or chronic injury or disease. 3. The method of claim 1 , wherein the neoplasia is selected from the group consisting of hepatocellular carcinoma claim 1 , esophageal squamous cell carcinoma claim 1 , breast cancer claim 1 , pancreatic cancer claim 1 , squamous cell cancer or adenocarcinoma of the head and neck claim 1 , colorectal cancer claim 1 , renal cancer claim 1 , brain cancer claim 1 , prostate cancer claim 1 , small and non-small cell lung cancer claim 1 , bladder cancer claim 1 , bone or joint cancer claim 1 , uterine cancer claim 1 , cervical cancer claim 1 , multiple myeloma claim 1 , hematopoietic malignancies claim 1 , lymphoma claim 1 , Hodgkin's disease claim 1 , non-Hodgkin's lymphoma claim 1 , skin cancer claim 1 , melanoma claim 1 , squamous cell carcinoma claim 1 , leukemia claim 1 , lung cancer claim 1 , ovarian cancer claim 1 , stomach cancer claim 1 , Kaposi's sarcoma claim 1 , laryngeal cancer claim 1 , endocrine carcinomas claim 1 , cancer of the thyroid gland claim 1 , cancer of the parathyroid gland claim 1 , cancer of the pituitary gland claim 1 , cancer of the adrenal gland claim 1 , and combinations thereof.4. The method of claim 1 , wherein the neoplasia is chemo-resistant ER/GR+ breast cancer.5. The method of wherein said neoplasia-treating therapy is radiation.6. The method of wherein said neoplasia-treating therapy is a radionuclide.7. The method of wherein said neoplasia treating therapy is selected from the group consisting of X-rays claim 1 , gamma rays claim 1 , and other sources of radiation.8. The method of wherein said neoplasia treating therapy is radiation therapy administered as external beam radiation claim 1 , wherein the radiation is directed from a remote source.9. The ...

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Номер записи: 80
22-09-2022 дата публикации

THERAPEUTIC AGENTS AND METHODS

Номер: US20220298203A1
Автор: "OBrien Rebecca", Altschul Randice Lisa, Arment Anthony R., Kesel Andreas J., Rapkin Myron, Theise Neil David
Принадлежит:

The invention provides glucocorticoid receptor antagonists for treatment of infection, neoplasia, and fatty liver disease. 1. A compound selected from the group consisting of:TPR-1, or pharmaceutically acceptable salts thereof;OR-1, or pharmaceutically acceptable salts thereof;MR-1, or pharmaceutically acceptable salts thereof;TCY1, or pharmaceutically acceptable salts thereofKM-1, or pharmaceutically acceptable salts thereof;TCY-1, or pharmaceutically acceptable salts thereof;PT155, or pharmaceutically acceptable salts thereof;PT157, or pharmaceutically acceptable salts thereof;PT158, or pharmaceutically acceptable salts thereof;PT159, or pharmaceutically acceptable salts thereof;PT160, or pharmaceutically acceptable salts thereof;PT162, or pharmaceutically acceptable salts thereof;PT163, or pharmaceutically acceptable salts thereof;PT164, or pharmaceutically acceptable salts thereof;PT165, or pharmaceutically acceptable salts thereof;PT166, or pharmaceutically acceptable salts thereof;PT167, or pharmaceutically acceptable salts thereof,and combinations thereof.2. A pharmaceutical composition comprising a therapeutically effective amount of at least one active agent , wherein the active agent is selected from the group consisting of: TPR-1 , OR-1 , MR-1 , TCY1 , PT150 , PT155 , PT157 , PT158 , PT159 , PT160 , PT162 , PT163 , PT164 , PT165 , PT166 , PT167 , combinations thereof , and pharmaceutically acceptable salts thereof andat least one pharmaceutically acceptable excipient.3. The pharmaceutical composition of claim 2 , in a dosage form selected from the group consisting of a minicapsule claim 2 , a capsule claim 2 , a tablet claim 2 , an implant claim 2 , a troche claim 2 , a lozenge claim 2 , a minitablet claim 2 , a temporary or permanent suspension claim 2 , an injectable claim 2 , an ovule claim 2 , a suppository claim 2 , a wafer claim 2 , a chewable tablet claim 2 , a quick or fast dissolving tablet claim 2 , an effervescent tablet claim 2 , a buccal or ...

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Номер записи: 81
23-05-2019 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20190153021A1
Автор: Chen Lei, Jin Zhendong, MEI Yan, Sha Aashay
Принадлежит: UNIVERSITY OF IOWA RESEARCH FOUNDATION

The invention provides compounds of formula (I): and salts thereof, wherein R, R, R, B, X, Y, and Z have any of the values defined herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing compounds of formula (I) and salts thereof, intermediates useful for preparing compounds of formula (I) and salts thereof, and therapeutic methods for treating cancer using a compound of formula (I) or a pharmaceutically acceptable salt thereof. 2. A compound or salt as described in wherein W is H.3. A compound or salt as described in claim 1 , wherein Ris H.4. A compound or salt as described in claim 1 , wherein Ris H.5. A compound or salt as described in claim 1 , wherein B is H or OH.6. A compound or salt as described in claim 1 , wherein B is H.7. A compound or salt as described in claim 1 , wherein X is acetylamino.8. A compound or salt as described in claim 1 , wherein Y is 4-methoxybenzoylamino.9. A compound or salt as described in claim 1 , any one of - wherein Z is 4-methyl-1-pentyl.10. A pharmaceutical composition comprising a compound of formula (I) as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable diluent or carrier.11. A method for treating cancer in an animal comprising administering a compound of formula (I) as described in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to the animal.1214-. (canceled)15. A compound or salt as described in wherein Z is (C-C)alkyl.16. A compound or salt as described in wherein Y is —NH—(C═O)OR claim 1 , —NH—(C═O)NRR claim 1 , —NH—S(═O)R claim 1 , —NH—(S═O)R claim 1 , or —NRR.17. A compound or salt as described in wherein Y is —NRR.18. A compound or salt as described in wherein each Rand Ris independently H claim 17 , (C-C)alkyl claim 17 , or aryl(C-C)alkyl claim 17 , wherein any C-C)alkyl and aryl(C-C)alkyl of Rand Ris optionally ...

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Номер записи: 82
08-06-2017 дата публикации

HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF

Номер: US20170158730A1
Автор: DUGAR Sundeep, Mahajan Dinesh, SCHREINER George Frederick
Принадлежит: SPHAERA PHARMA PVT. LTD.

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. 5. The compounds as claimed in 1 , selected from the group comprising:i. (10R,11S,13S,17S)-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-11-hydroxy-10,13-dimethyl-3-oxo-1H-cyclopenta[a]phenanthrene-17-carboxylic acid;ii. (3S,8S,9S,10S,11S,13S,14S,17S)-hexadecahydro-3,11-dihydroxy-N,10,13-trimethyl-1H-cyclopenta[a]phenanthrene-17-carboxamide;iii. (3S,8S,9S,10S,11S,13S,14S,17S)—N-(2-aminoethyl)-hexadecahydro-3,11-dihydroxy-10,13-dimethyl-1H-cyclopenta[a]phenanthrene-17-carboxamide;iv. (3S,5R,6R,10R,11S,13S,17S)-hexadecahydro-6-methoxy-10,13-dimethyl-17-(2-methyl-1,3-dioxolan-2-yl)-1H-cyclopenta[a]phenanthrene-3,5,11-triol;v. (4aR,5S,6aS)-5-hydroxy-4a,6a-dimethyl-4,4a,4b,5,6,6a,9,9a,9b,10-decahydro-1H-indeno[5,4-f]quinoline-2,7βH,8H)-dione;vi. (4a′R,5′S,6a'S)-5′-hydroxy-4a′,5′,6a′-trimethyl-3′,4′,4a′,4b′,5′,6′,6a′,8′,9′,9a′,9b′,10′-dodecahydrospiro[[1,3]dioxolane-2,7′-indeno[5,4-f]quinolin]-2′(1′H)-one;vii. (4aR,5S,6aS)-4,4a,4b,5,6,6a,9,9a,9b,10-decahydro-5-hydroxy-4a,6a-dimethyl-1H-indeno[5,4-f]quinoline-2,7βH,8H)-dione;viii. (4aR,5S,6aS)-7-acetyl-4,4a,4b,5,6,6a,7,8,9,9a,9b,10-dodecahydro-5-hydroxy-4a,5,6a-trimethyl-1H-indeno[5,4-f]quinolin-2(3H)-one;ix. (11S)-7,8,9,11,12,13,14,15,16,17-decahydro-3,11-dihydroxy-6H-cyclopenta[a]phenanthrene-17-carboxylic acid;x. (4aR,6aS)-2,3,4,4a,4b,5,6,6a,7,8,9,9a,9b,10-tetradecahydro-4a,6a-dimethyl-2,5-dioxo-1H-indeno[5,4-f]quinoline-7-carboxylic acid;xi. (17S)-17-acetyl-7,8,13,15,16,17-hexahydro-3-hydroxy-1-methyl-6H-cyclopenta [a]phenanthren-11(9H,12H,14H)-one;xii. (13S,17S)-17-acetyl-7,8,13,15,16,17-hexahydro-3-hydroxy-13-methyl-6H-cyclopenta[a]phenanthren-11(9H,12H,14H)-one;xiii. (10R,11S,13S,17S)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid;xiv. (10R,11S,13S,17S)-11-hydroxy-N,N,10,13- ...

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Номер записи: 83
29-09-2022 дата публикации

GLUCOCORTICOID RECEPTOR AGONISTS

Номер: US20220306680A1
Автор: JAMISON James Andrew, Leung Donmienne Doen Mun, WURST Jacqueline Mary
Принадлежит:

The present invention provides a compound of Formula I: 2. The compound of claim 1 , wherein R is hydrogen claim 1 , or a pharmaceutically acceptable salt thereof.3. The compound of claim 1 , wherein R is —P(═O)(OH) claim 1 , or a pharmaceutically acceptable salt thereof.17. A method of treating atopic dermatitis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.18. A method of treating systemic lupus erythematosus in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.19. A method of treating rheumatoid arthritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.20. A method of treating lupus nephritis in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.21. A method of treating inflammatory bowel disease in a patient claim 1 , comprising administering to a patient in need of such treatment an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.22. A pharmaceutical composition claim 1 , comprising a compound or a pharmaceutically acceptable salt thereof claim 1 , according to with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients.23. A process for preparing a pharmaceutical composition claim 1 , comprising admixing a compound or a pharmaceutically acceptable salt thereof according to with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients. The present disclosure provides compounds that are ...

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Номер записи: 84
06-06-2019 дата публикации

NEUROACTIVE STEROIDS, COMPOSITIONS, AND USES THEREOF

Номер: US20190169226A1
Автор: Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Described herein are steroids of Formula (I): 2. The method of claim 1 , wherein Ris methyl.3. The method of claim 1 , wherein both Rand Rare hydrogen.4. The method of claim 1 , wherein Ris C-Calkyl claim 1 , C-Calkenyl claim 1 , C-Calkynyl claim 1 , carbocyclyl claim 1 , heterocyclyl claim 1 , C(O)R claim 1 , —C(O)OR claim 1 , or —C(O)NRR.5. The method of claim 4 , wherein Ris —C(O)NRR.6. The method of claim 1 , wherein Ris hydrogen claim 1 , C-Calkyl claim 1 , or —OH.7. The method of claim 6 , wherein Ris hydrogen.8. The method of claim 1 , wherein both Rand Rare hydrogen claim 1 , the between —CRand —CRRis a single bond claim 1 , and both Rand Rare hydrogen.9. The method of claim 1 , wherein Z is —CH—.10. The method of claim 1 , wherein Ris hydrogen and Ris C-Calkyl.12. The method of claim 11 , wherein Ris methyl.13. The method of claim 11 , wherein Ris C-Calkyl claim 11 , C-Calkenyl claim 11 , C-Calkynyl claim 11 , carbocyclyl claim 11 , heterocyclyl claim 11 , —C(O)R claim 11 , —C(O)OR claim 11 , or —C(O)NRR.14. The method of claim 11 , wherein Ris C-Calkyl.15. The method of claim 11 , wherein Ris hydrogen.16. The method of claim 11 , wherein both Rand Rare hydrogen and both Rand Rare hydrogen.19. The method of claim 18 , wherein Ris methyl.20. The method of claim 18 , wherein Ris C-Calkyl claim 18 , C-Calkenyl claim 18 , C-Calkynyl claim 18 , carbocyclyl claim 18 , heterocyclyl claim 18 , —C(O)R claim 18 , —C(O)OR claim 18 , or —C(O)NRR.21. The method of claim 18 , wherein Ris C-Calkyl.22. The method of claim 20 , wherein Ris —C(O)NRR.23. The method of claim 18 , wherein Ris —OH.24. The method of claim 18 , wherein Ris hydrogen.25. The method of claim 18 , wherein both Rand Rare hydrogen and both Rand Rare hydrogen.27. The method of claim 1 , wherein the CNS-related disorder is a sleep disorder claim 1 , a mood disorder claim 1 , a schizophrenia spectrum disorder claim 1 , a convulsive disorder claim 1 , a disorder of memory and/or cognition claim 1 , a ...

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Номер записи: 85
28-05-2020 дата публикации

ISOTOPICALLY LABELED BILE ACID DERIVATIVES

Номер: US20200165290A1
Автор: Galvin Gabriel, Schaab Kevin, YANIK Mathew
Принадлежит:

The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof. 2. The compound of wherein Ris H.3. The compound of wherein Ris OH.4. The compound of wherein Ris alpha-OH.5. The compound of claim 1 , wherein Ris taurine (—NH(CH)SOH) claim 1 , glycine (—NHCHCOH) claim 1 , or sarcosine (—N(CH)CHCOH). Selective incorporation of isotopes (e.g., deuterium in place of hydrogen) has a unique effect of retaining the biochemical potency and selectivity of physiologically active compounds while modifying metabolic properties to alter their overall therapeutic profile. In some cases, this modification has the potential to have a positive impact on safety, efficacy and tolerability. Isotopically labeled (e.g., deuterated and/or radiolabeled) compounds have been widely studied in clinical and non-clinical settings and used in humans as metabolic or pharmacokinetic probes.Bile acids (BAs) are well known for their role in the solubilization and digestion of lipid-soluble nutrients. Recently, BAs have emerged as signaling molecules with systemic endocrine functions. BAs and derivatives thereof have been shown to modulate several nuclear hormone receptors, notably the farnesoid X receptor (FXR), and are agonists for the G protein-coupled receptor TGR5. Signaling via FXR and TGR5 modulates several metabolic pathways, regulating not only BA synthesis and enterohepatic recirculation, but also triglyceride, cholesterol, glucose and energy homeostasis (Thomas, et al. Nat Rev Drug Discovery, 2008, 7, 678-693).A semi-synthetic bile acid analogue, 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-oic acid (6-ethyl-chenodeoxycholic acid (6-ECDCA) or obeticholic acid (OCA)), disclosed in WO 2002/75298 is a highly potent FXR modulator, which is currently marketed as OCALIVA® for the treatment of primary biliary cholangitis (PBC).Another semi-synthetic bile acid analogue, 3α,7α, 11β-trihydroxy-6α-ethyl-5β-cholan-24-oic acid (compound 100) while ...

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Номер записи: 86
12-07-2018 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20180194797A1
Автор: Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R, R, and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 2. The compound of claim 1 , wherein Ris Calkyl.3. The compound of claim 2 , wherein Ris substituted Calkyl.4. The compound of claim 2 , wherein Ris unsubstituted Calkyl.5. (canceled)6. The compound of claim 1 , wherein Ris methyl or ethyl.7. The compound of claim 1 , wherein Ris Calkyl or carbocyclyl.8. (canceled)9. The compound of claim 1 , wherein Ris carbocyclyl or heterocyclyl.10. The compound of claim 9 , wherein Ris cyclopropyl claim 9 , cyclobutyl claim 9 , cyclopentyl claim 9 , cyclohexyl.11. (canceled)12. (canceled)23. A pharmaceutical composition comprising a compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.24. A method of inducing sedation or anesthesia comprising administering to a subject an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or pharmaceutical composition thereof.25. A method for treating or preventing a disorder described herein claim 1 , comprising administering to a subject in need thereof an effective amount of a compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , or pharmaceutical composition thereof.26. The method according to claim 25 , wherein the disorder is a gastrointestinal (GI) disorder irritable bowel syndrome (IBS) claim 25 , inflammatory bowel disease (IBD) claim 25 , structural disorders affecting the GI claim 25 , anal disorders claim 25 , colon polyps claim 25 , cancer claim 25 , colitis.27. (canceled)28. The method according to claim 26 , wherein the disorder is inflammatory bowel disease claim 26 , cancer claim 26 , diabetes claim 26 , or a sterol synthesis disorder.29. A method for ...

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Номер записи: 87
13-07-2017 дата публикации

SYNTHESIZING PET TRACERS USING [F-18]SULFONYL FLUORIDE AS A SOURCE OF [F-18]FLUORIDE

Номер: US20170197912A1
Автор: Chu Wenhua, Zhou Dong
Принадлежит: WASHINGTON UNIVERSITY

The present disclosure relates to the methods for the preparation of reactive [F-18]fluoride in a form of [F-18]sulfonyl fluoride suitable for efficient radiolabeling without an azeotropic evaporation step by the use of anion exchange resin and sulfonyl chloride, and its applications in the manufacturing of PET radiopharmaceuticals. 1. A method of making [F-18]sulfonyl fluoride without any evaporation step , the method comprising:a) passing an aqueous [F-18]fluoride solution or solvent through a solid phase extraction column comprising an anion-exchange resin so that the [F-18]fluoride is trapped on the resin;b) rinsing the resin with an organic solvent to eliminate the residual water; and{'sub': 2', '2, 'sup': '1', 'claim-text': R is selected from the group consisting of hydrocarbyl, substituted hydrocarbyl, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, arylalkenyl, substituted arylalkenyl, arylalkynyl, substituted arylalkynyl, heteroaryl, substituted heteroaryl, methyl, trifluoromethyl, and combinations thereof; and', {'sup': '1', 'Ris a leaving group.'}], 'c) eluting the [F-18]fluoride with an eluting solution to release the [F-18]fluoride from the anion-exchange resin as [F-18]RSOF which acts as a source of [F-18]fluoride for a labeling reaction, wherein the eluting solution comprises a compound having the formula RSORand an organic solvent, wherein'}2. The method of claim 1 , wherein R is selected from the group consisting of alkyl claim 1 , substituted alkyl claim 1 , cycloalkyl claim 1 , substituted cycloalkyl claim 1 , aryl claim 1 , substituted aryl claim 1 , heteroaryl claim 1 , substituted heteroaryl claim 1 , methyl and trifluoromethyl.3. The method of claim 1 , wherein R is selected from the group consisting of CH claim 1 , CF claim 1 , CH claim 1 , CHCH claim 1 , CFCH claim 1 , NOCH ...

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Номер записи: 88
18-06-2020 дата публикации

MOGROSIDES AND USE THEREOF

Номер: US20200187550A1
Автор: Chow Siew Yin, MARKOSYAN Avetik, RAMANDACH Saravanan
Принадлежит:

The present invention provides a process for preparation of compositions comprising novel mogrosides from fruit of . The compositions have superior organoleptic properties compared to known mogroside compositions and are useful in wider range of consumables including foods and beverages. 2. A composition comprising at least one compound of .3Siraitia grosvenorii. The composition of claim 2 , further comprising mogrosides selected from the group consisting of Luo han guo extract claim 2 , by-products of other mogrosides' isolation and purification processes claim 2 , a commercially available Luo han guo extract claim 2 , mogroside IA claim 2 , mogroside IE claim 2 , 11-oxomogroside IA claim 2 , mogroside II A claim 2 , mogroside II B claim 2 , mogroside II E claim 2 , 7-oxomogroside II E claim 2 , mogroside III claim 2 , 11-deoxymogroside III claim 2 , mogroside IV claim 2 , 11-oxomogroside IV A claim 2 , mogroside V claim 2 , 7-oxomogroside V claim 2 , 11-oxomogroside V claim 2 , isomogroside V claim 2 , mogroside VI claim 2 , mogrol claim 2 , 11-oxomogrol claim 2 , isomogroside claim 2 , siamenoside claim 2 , siamenoside I claim 2 , neomogroside claim 2 , synthetic mogrosides claim 2 , other mogrosides occurring in fruits and combinations thereof.4. The composition of claim 2 , further comprising at least one additional sweetener.5Stevia rebaudianaSiraitia grosvenorii. The composition of claim 4 , wherein the at least one additional sweetener is selected from the group consisting of sucrose claim 4 , glyceraldehyde claim 4 , dihydroxyacetone claim 4 , erythrose claim 4 , threose claim 4 , erythrulose claim 4 , arabinose claim 4 , lyxose claim 4 , ribose claim 4 , xylose claim 4 , ribulose claim 4 , xylulose claim 4 , allose claim 4 , altrose claim 4 , allulose claim 4 , galactose claim 4 , glucose claim 4 , gulose claim 4 , idose claim 4 , mannose claim 4 , talose claim 4 , fructose claim 4 , psicose claim 4 , sorbose claim 4 , tagatose claim 4 , mannoheptulose ...

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Номер записи: 89
29-07-2021 дата публикации

HIGH INTENSITY SWEETENERS

Номер: US20210227863A1
Автор: Colquitt Justin, Gonsalves Nicole, Hammaker Jeffrey R., Manam Rama, Noriega Chris Edano, Patron Andrew, Servant Nicole
Принадлежит:

Disclosed herein are compounds having structural Formula (I), or salts thereof. These compounds are useful as sweet tasting agents and/or sweetness enhancers. Also disclosed are compositions comprising the present compounds and methods of increasing the sweet taste of ingestible compositions. Furthermore, methods for preparing the compounds are also disclosed. 2. The composition of claim 1 , comprising less than 1% by weight of Mogroside III.3. The composition of claim 1 , comprising less than 0.3% by weight of 11-oxo-Mogroside III.4. The composition of claim 1 , comprising less than 1% by weight of all isomers of Mogroside I claim 1 , Mogroside II claim 1 , and Mogroside III.5. The composition of claim 1 , comprising less than 1% by weight of 11-oxo-mogrol.6. The composition of claim 1 , comprising greater than 70% by weight of the compound.7. The composition of claim 1 , wherein the compound is in amorphous form.8. The composition of claim 1 , wherein the compound is coating a solid carrier.9. The composition of claim 8 , wherein the solid carrier are particles selected from the group consisting of lactose claim 8 , cellulose claim 8 , microcrystalline cellulose claim 8 , modified food starch claim 8 , gum Arabic claim 8 , maltodextrin claim 8 , modified corn starch claim 8 , dextrose claim 8 , xantham gum claim 8 , carboxymethylcellulose claim 8 , cellulose gel claim 8 , cellulose gum claim 8 , sodium caseinate claim 8 , carrageenan claim 8 , and combinations thereof.10. The composition of claim 7 , wherein the composition is in particulate form.11. The composition of claim 10 , wherein the composition has an average particle size between 50 μm and 300 μm.12. A composition claim 1 , comprising solid particles of the composition of and a liquid carrier.13. The composition of claim 12 , wherein the solid particles are suspended in the liquid carrier.14. The composition of claim 12 , wherein the liquid carrier is selected from water claim 12 , ethanol claim 12 , ...

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Номер записи: 90
29-07-2021 дата публикации

SEPARATION MEDIUM, USE FOR SEPARATION MEDIUM, STEVIOL GLYCOSIDE SEPARATION METHOD USING SEPARATION MEDIUM, AND STEVIOL GLYCOSIDE PRODUCTION METHOD USING SEPARATION METHOD

Номер: US20210229071A1
Автор: ADACHI Tadashi
Принадлежит: MITSUBISHI CHEMICAL CORPORATION

An object of the present invention is to provide a separation medium and a separation method, ensuring high selectivity and good separation efficiency for specific steviol glycosides. The present invention is related to a separation medium in which polyethyleneimine is immobilized to porous particles of a (meth)acrylic polymer having a crosslinked structure and a hydroxyl group. 18-. (canceled)9. A separation method for steviol glycosides , the method comprising a liquid chromatography step of loading a solution containing two or more types of steviol glycosides to a separation medium and flowing a solvent A through the separation medium , thereby separating at least two types of steviol glycosides included in the steviol glycosides , wherein the separation medium comprises polyethyleneimine immobilized to porous particles of a (meth)acrylic polymer having a crosslinked structure and a hydroxyl group.10. The separation method for steviol glycosides according to claim 9 , wherein the solution containing two or more types of steviol glycosides comprises rebaudioside A claim 9 , and wherein at least one fraction obtained in the liquid chromatography step is a fraction containing rebaudioside A as a main component.11. The separation method for steviol glycosides according to claim 9 , wherein the solvent A comprises alcohols freely miscible with water.12. The separation method for steviol glycosides according to claim 9 , wherein a decolorization of a pigment component in the solution containing two or more types of steviol glycosides is performed during the liquid chromatography step.13. A separation method for steviol glycosides claim 9 , the method comprising an adsorption step of bringing a solution containing two or more types of steviol glycosides and a solvent B into contact with a separation medium to form a steviol glycosides adsorbed separation medium claim 9 , and an elution step of eluting the steviol glycosides from the steviol glycosides adsorbed ...

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Номер записи: 91
06-08-2015 дата публикации

SWEETENING COMPOSITIONS AND PROCESSES FOR PREPARING THEM

Номер: US20150216209A1
Автор: FUSHENG Lan, LYNDON Rex Murray, MILLER Christopher John, SMITH Garth Selwyn
Принадлежит: Waikato Innovation Park

The invention relates to sweetening compositions obtained from the Luo Han Guo fruit, a member of the Cucurbiticeae family. The compositions are free of bitter-tasting impurities, have a light colour and contain about 16-75% mogroside V and about 30-95% total terpene glycosides on a dry weight basis. A filtered (0.2 μm) solution of the composition in water with a solids content of 1% w/v has an absorbance at 420 nm of about 0.55 or below. Also disclosed is a method of preparing such compositions which includes a heating step to encourage the formation of melanoidins, highly coloured impurities, thereby permitting their removal by filtration providing a lighter coloured product. 122-. (canceled)23. A process of preparing a sweetening composition containing terpene glycosides , the process comprising:(a) obtaining a terpene glycoside-containing liquid extract from a fresh plant source material containing terpene glycosides;(b) clarifying the extract;(c) concentrating terpene glycosides in the extract to obtain a purified terpene glycoside-containing solution;(d) heating the purified terpene glycoside-containing solution to a sufficient temperature and for a sufficient time to form melanoidins; and(e) separating melanoidins from terpene glycosides in the solution to obtain a decolourised terpene glycoside-containing solution.24. A process according to claim 23 , further comprising drying the decolourised terpene glycoside-containing solution obtained from step (e) to form a powdered composition.25. A process according to claim 24 , wherein the decolourised terpene glycoside-containing solution is concentrated before drying.26. A process according to claim 23 , wherein the fresh plant source material is a fruit of the Cucurbitaceae family.27. A process according to claim 23 , wherein the fresh plant source material is Luo Han Guo fruit.28. A process according to claim 27 , wherein step (a) comprises contacting macerated Luo Han Guo fruit with hot water claim 27 , at a ...

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Номер записи: 92
09-10-2014 дата публикации

Stereoselective Glycosylation Reactions

Номер: US20140303359A1
Автор: Bennett Clay S., Chu An-Hsiang Adam
Принадлежит: TRUSTEES OF TUFTS COLLEGE

Disclosed is a method for selective synthesis of 1,2-cis-α-linked glycosides which does not require the use of the specialized protecting group patterns normally employed to control diastereoselectivity. Thioglycoside acceptors can be used, permitting iterative oligosaccharide synthesis. The approach eliminates the need for lengthy syntheses of monosaccharides possessing highly specialized and unconventional protecting group patterns. 1. A method of forming a glycosidic bond , comprising:combining a glycosyl sulfide, a sulfoxide, molecular sieves, and a non-nucleophilic base, thereby forming a first reaction mixture;combining a sulfonic anhydride and the first reaction mixture, thereby forming a second reaction mixture;combining tetrabutylammonium iodide (TBAI) and the second reaction mixture, thereby forming a third reaction mixture; andcombining a glycosyl acceptor and the third reaction mixture, thereby forming a glycosidic bond;wherein the glycosidic bond is formed with greater than or equal to 90% stereoselectivity for a particular stereochemical configuration.2. The method of claim 1 , wherein the glycosidic bond is formed with greater than or equal to 95% stereoselectivity for a particular stereochemical configuration.3. The method of claim 1 , wherein the glycosidic bond is formed with greater than or equal to 98% stereoselectivity for a particular stereochemical configuration.4. The method of claim 1 , wherein the glycosidic bond is formed with greater than or equal to 99% stereoselectivity for a particular stereochemical configuration.5. The method of claim 1 , wherein the particular stereochemical configuration is an α linkage.6. The method of claim 1 , wherein said glycosyl sulfide is a glycosyl phenyl sulfide.7. The method of claim 1 , wherein said molecular sieves are 4 Angstrom molecular sieves.8. The method of claim 1 , wherein said sulfoxide is phenyl sulfoxide.9. The method of claim 1 , wherein said sulfonic anhydride is trifluoromethanesulfonic ...

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Номер записи: 93
11-08-2016 дата публикации

PROCESS FOR THE PREPARATION OF ESTETROL

Номер: US20160229885A1
Автор: FERREIRO GIL Juan José, Gallo Nieto Francisco Javier, IGLESIAS RETUERTO Jesús Miguel
Принадлежит: CRYSTAL PHARMA, S.A.U.

The invention relates to a process for obtaining Estetrol or a salt or solvate thereof, the process comprising: a) reacting a compound of formula (IV) or a salt or solvate thereof, wherein Ris a hydroxyl protecting group selected from a silyl ether, an ether, an ester, a carbamate and a carbonate, and Ris a hydroxyl protecting group selected from an ether, with an oxidizing agent selected from OsOor a source of osmium tetroxide to produce Estetrol or a compound of formula (II) or a salt or solvate thereof wherein Ris as defined previously; and b) if a compound of formula (II) is obtained in step a), deprotecting said compound to produce Estetrol. 115.-. (canceled)17. The process according to claim 16 , wherein the oxidizing agent is supported.18. The process according to claim 16 , wherein the oxidizing agent is OsO-PVP (poly(4-vinyl-pyridine)).19. The process according to claim 16 , wherein a co-oxidant is further added.20. The process according to claim 16 , wherein trimethylamine-N-oxide is added as co-oxidant.21. The process according to claim 16 , wherein the 15β claim 16 ,16β-diol isomer is obtained in an amount 3% with respect to the sum of 15β claim 16 ,16β-diol and 15α claim 16 ,16α-diol.22. The process according to claim 16 , wherein the hydroxyl group at position C17 in the compound of formula (IV) is protected by an ether selected from (1-butoxyethyl)ether claim 16 , tetrahydropyranyl (THP) ether claim 16 , phenylthiomethyl (PTM) ether claim 16 , and methoxymethyl (MOM) ether.23. The process according to claim 16 , wherein the hydroxyl group at position C3 in the compound of formula (IV) is protected by an ester.24. The process according to claim 16 , wherein the hydroxyl group at position C3 in the compound of formula (IV) is protected by benzoyl ester.25. The process according to claim 16 , wherein the hydroxyl group at position C3 in the compound of formula (IV) is protected by benzoyl ester and the hydroxyl group at C17 is protected by (1-butoxyethyl ...

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Номер записи: 94
25-07-2019 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS

Номер: US20190224218A1
Автор: Qian Xiangping
Принадлежит:

Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described. 131-. (canceled)33. The method of claim 32 , wherein the subject is a human.34. The method of claim 32 , wherein the compound or the pharmaceutically acceptable salt is administered orally claim 32 , subcutaneously claim 32 , intravenously claim 32 , intranasally claim 32 , transdermally claim 32 , intraperitoneally claim 32 , intramuscularly claim 32 , intrapulmonary claim 32 , vaginally claim 32 , rectally claim 32 , or intraocularly.35. The method of claim 32 , wherein the compound or the pharmaceutically acceptable salt is administered intravenously.36. The method of claim 32 , wherein the compound or the pharmaceutically acceptable salt is administered orally.37. The method of claim 32 , further comprising administering to the subject an additional anti-cancer and/or cytotoxic agent.38. The method of claim 37 , wherein the additional anti-cancer and/or cytotoxic agent is administered simultaneously with the compound or the pharmaceutically acceptable salt.39. The method of claim 32 , wherein the amount of the compound or the pharmaceutically acceptable salt administered is in the range of 0.01 mg to 100 mg per kilogram body weight of the subject.40. The method of claim 32 , wherein the amount of the compound of Formula III administered is in the range of about 0.01 mg to 1000 mg.41. The method of claim 32 , wherein Ris hydrogen or an optionally substituted lower alkyl.42. The method of claim 32 , wherein Ris hydrogen or methyl.43. The method of claim 32 , wherein Ris an optionally substituted alkyl.44. The method of claim 32 , wherein Ris an optionally substituted acyl.45. The method of claim 44 , wherein Ris chosen from acetyl claim 44 , propionyl claim 44 , isobutyryl claim 44 , and pivaloyl.46. The method of claim 32 , wherein Ris an optionally substituted alkoxycarbonyl.47. The method of claim 46 , wherein Ris chosen from optionally ...

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Номер записи: 95
26-08-2021 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20210261598A1
Автор: Harrison Boyd L., Martinez Botella Gabriel, Reid John Gregory, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит:

Compounds are provided according to Formula (I), and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein A, R, and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 4. The compound of claim 2 , wherein p is an integer selected from 0 claim 2 , 1 claim 2 , or 2.5. The compound of claim 2 , wherein p is 0.6. The compound of claim 2 , wherein p is 1.7. The compound of claim 2 , wherein p is 1 and X is halogen.9. The compound of claim 2 , wherein Ris Calkyl.10. The compound of claim 9 , wherein Ris methyl or ethyl.11. (canceled)14. The compound of claim 2 , wherein Z is —C(R)— claim 2 , —O— claim 2 , or —NR—.15. The compound of claim 2 , wherein Ris halogen.16. The compound of claim 2 , wherein Z is —CH— claim 2 , —CF— claim 2 , or —C(CH)—.17. The compound of claim 2 , wherein Z is —O— or —NR—.18. The compound of claim 2 , wherein Z is —NH— claim 2 , —NMe- claim 2 , or —NAc—.19. The compound of claim 2 , wherein Z is —CH—.20. The compound of claim 2 , wherein Z is —C(CH)—.21. The compound of claim 2 , wherein Z is —CF—.22. The compound of claim 2 , wherein m is 1 claim 2 , n is 2 claim 2 , and Z is —O—.23. The compound of claim 2 , wherein m is 2 and n is 2.24. The compound of claim 2 , wherein m is 3 and n is 1.25. The compound of claim 2 , wherein m is 3 claim 2 , n is 1 claim 2 , and Z is —O—.26. The compound of claim 2 , wherein m is 2 claim 2 , n is 2 claim 2 , and Z is —O— or —NR—.29. A pharmaceutical composition comprising a compound according to claim 1 , and a pharmaceutically acceptable carrier.30. A method of inducing sedation or anesthesia comprising administering to a subject an effective amount of a compound according to or pharmaceutical composition thereof.31. A method for treating or preventing a disorder described herein claim 1 , comprising administering to a subject in need thereof an effective amount of a compound ...

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Номер записи: 96
10-09-2015 дата публикации

IODINE(III)-MEDIATED RADIOFLUORINATION

Номер: US20150252007A1
Автор: Liang Huan, Rotstein Benjamin H., Stephenson Nickeisha A., Vasdev Neil
Принадлежит:

A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using F is described. Processes, intermediates, reagents and radiolabelled compounds are described. 2. The process of claim 1 , wherein step (a) is performed in the presence of an oxidizing agent selected from the group consisting of sodium perborate claim 1 , urea-hydrogen peroxide adduct claim 1 , 1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane bis(tetrafluoroborate) (Selectfluor®) claim 1 , potassium peroxymonosulfate (OXONE®) claim 1 , dimethyldioxirane claim 1 , or meta-chloroperoxybenzoic acid.3. The process of claim 2 , wherein step (a) is performed in the presence of a carboxylate source that is an acetate source or trifluoroacetate source.5. The process of claim 1 , wherein step (b) is carried out in the presence of a base.6. The process of claim 5 , wherein step (b) is carried out in the presence of a carbonate base.10. The process of claim 1 , comprising isolating or purifying the iodonium ylide following step (b).11. The process of claim 1 , wherein said fluoride source of step (c) is a fluoride salt.12. The process of claim 1 , wherein said fluoride source comprises [F] fluoride.13. The process of claim 12 , wherein said fluoride source is tetraethylammonium [F]fluoride.14. The process of claim 1 , comprising isolating or purifying the aromatic fluoride following step (c).19. A process for preparing an aromatic fluoride compound (Ar—F) comprising (c) reacting a compound according to with a fluoride source to form an aromatic fluoride compound.20. The process of claim 19 , wherein said fluoride source of step (c) is a fluoride salt.21. The process of claim 19 , wherein said fluoride source comprises [F] fluoride.22. The process of claim 21 , wherein said fluoride source is tetraethylammonium [F]fluoride. This application claims the benefit of U.S. Provisional Appl. No. 61/949,302, filed Mar. 7, 2014, the disclosure of which is ...

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Номер записи: 97
01-09-2016 дата публикации

5-Beta, 14-Beta-Androstane Derivatives Useful For The Treatment Of Proteinuria, Glomerulosclerosis And Renal Failure

Номер: US20160251392A1
Автор: Bianchi Giuseppe, Ferrandi Mara, Ferrari Patrizia
Принадлежит:

Compound of formula (I), wherein the symbol have the meaning reported in the text; for preparing a medicament for the prevention and/or treatment of proteinuria, glomerulosclerosis or renal failure. 112-. (canceled)14. The method according to claim 13 , wherein the compound is administered in a dose of from 0.05 mg to 20 mg per day.15. The method according to claim 14 , wherein the compound is administered in a dose of from 0.5 mg to 15 mg.16. The method according to claim 15 , wherein the compound is administered in a dose of from 5 mg to 10 mg.17. The method according to claim 16 , wherein the compound is administered) in a single dose schedule.18. The method according to claim 16 , wherein the compound is administered in a multiple dose schedule.19. The method according to claim 13 , wherein the compound is administered to the patient orally claim 13 , intravenously claim 13 , intramuscularly claim 13 , intra-arterially claim 13 , intramedullary claim 13 , intrathecally claim 13 , intraventricularly claim 13 , transdermally claim 13 , transcutaneously claim 13 , subcutaneously claim 13 , intraperitoneally claim 13 , intranasally claim 13 , enterally claim 13 , topically claim 13 , sublingually or rectally. This application is a continuation of U.S. application Ser. No. 13/258,728 filed Sep. 22, 2011, which is a National Stage Entry of International Application Number PCT/EP2010/053571 Filed Mar. 18, 2010, which published as PCT Publication No. WO 2010/108855 on Sep. 30, 2010, which claims the benefit of European Application Number EP 09155834.6 filed Mar. 23, 2009.The foregoing applications, and all documents cited therein or during their prosecution (“appln cited documents”) and all documents cited or referenced in the appln cited documents, and all documents cited or referenced herein (“herein cited documents”), and all documents cited or referenced in herein cited documents, together with any manufacturer's instructions, descriptions, product specifications, ...

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Номер записи: 98
31-08-2017 дата публикации

Neuroactive steroids, compositions, and uses thereof

Номер: US20170247406A1
Автор: Albert Jean Robichaud, Boyd L. Harrison, Francesco G. Salituro, Gabriel Martinez Botella
Принадлежит: Sage Therapeutics Inc

Described herein are steroids of Formula (I): and pharmaceutically acceptable salts thereof; wherein R 1 , R 2a , R 2b , R 3 , R 4 , R 5a , R 5b , R 6 , and Z are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

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Номер записи: 99
15-08-2019 дата публикации

OXYSTEROLS AND METHODS OF USE THEREOF

Номер: US20190248829A1
Автор: Griffin Andrew, Harrison Boyd L., Martinez Botella Gabriel, Robichaud Albert Jean, Salituro Francesco G.
Принадлежит: SAGE THERAPEUTICS, INC.

Compounds are provided according to Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R, R, R, R, and and Rare as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. 2. The compound of claim 1 , wherein Ris hydrogen or substituted or unsubstituted C-Calkyl.3. The compound of claim 1 , wherein Ris C-Chaloalkyl.46-. (canceled)7. The compound of claim 1 , wherein each of Rand Ris independently hydrogen claim 1 , carbocyclyl claim 1 , or heterocyclyl.89-. (canceled)10. The compound of claim 1 , wherein at least one of Rand Ris C-Calkyl claim 1 , carbocyclyl claim 1 , or heterocyclyl; or Rand R claim 1 , together with the carbon atom to which they are attached form a 3-8 membered ring.1128-. (canceled)29. The compound of claim 1 , wherein Rand R claim 1 , together with the carbon atom to which they are attached form a 5-membered ring.3031-. (canceled)32. The compound of claim 1 , wherein Rand R claim 1 , together with the carbon atom to which they are attached form a 6-membered ring.3337-. (canceled)38. The compound of claim 1 , wherein Rand R claim 1 , together with the carbon atom to which they are attached form a 3-8 membered carbocyclic or heterocyclic ring.39. The compound of claim 38 , wherein the carbocyclic or heterocyclic ring is substituted with 1 or 2 halo or alkyl groups.4053-. (canceled)55. A pharmaceutical composition comprising a compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.56. A method for treating or preventing a disorder described herein claim 1 , comprising administering to a subject in need thereof an effective amount of a compound of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , or pharmaceutical composition thereof claim 1 , wherein the disorder is a gastrointestinal (GI) disorder claim 1 , constipation claim 1 , ...

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Номер записи: 100