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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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Форма поиска

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 2841. Отображено 100.
01-11-2012 дата публикации

Processes for making high purity renewable source-based plasticizers and products made therefrom

Номер: US20120277357A1
Принадлежит: Archer Daniels Midland Co

Presently disclosed are high purity unsaturated fatty acid esters with an ester moiety characterized by having from five to seven members in a ring structure, which esters when epoxidized find particular utility as primary plasticizers in flexible polyvinyl halide applications. Also disclosed are processes for making the high purity esters.

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23-05-2013 дата публикации

PROCESSES AND INTERMEDIATES FOR PREPARING STERIC COMPOUNDS

Номер: US20130131359A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

This invention relates to processes and intermediates for the preparation of an alpha-amino beta-hydroxy acid of Formula 1 2. The process of claim 1 , wherein R claim 1 , is C-Calkyl claim 1 , R′is H and R′is —NHRwherein Ris C-Calkyl or C-Ccycloalkyl.3. The process of claim 2 , wherein Ris propyl and Ris cyclopropyl.5. The process of claim 4 , wherein the aminating reagent is an azide salt and the intermediate azido compound is reduced by hydrogenation.7. The process of claim 6 , wherein the oxidizing reagent is t-butyl hydroperoxide.8. The process of claim 6 , wherein the oxidizing reagent includes a chiral reagent.9. The process of claim 8 , wherein the oxidizing reagent is a mixture of samarium (III) isopropoxide claim 8 , triphenyl arsine oxide claim 8 , S-(−)1 claim 8 ,1′-bi-2-naphthol and 4 Å molecular sieves.10. The process of claim 6 , wherein the oxidizing reagent is urea-hydrogen peroxide in the presence of trifluoroacetic anhydride.11. The process of claim 6 , wherein R′is —OE.12. The process of claim 6 , wherein Ris —NHR.13. The process of claim 11 , further comprising hydrolyzing the compound of Formula ii to give an acid and then converting the acid to an amide compound of Formula ii wherein R′is —NHR.15. The process of claim 14 , wherein the compound of Formula 1 is (2S claim 14 ,3S)-3-amino-N-cyclopropyl-2-hydroxyhexanamide.16. The process of claim 14 , wherein the organic acid is L-tartaric acid.17. The process of claim 14 , wherein the organic acid is deoxycholic acid.18. A compound which is N-cyclopropyl-3-propyloxirane-2-carboxamide.19. A compound which is N-cyclopropyl-3-propyloxirane-2-carboxamide.20. A compound which is 3-azido-N-cyclopropyl-2-hydroxyhexanamide.21. A compound which is 3-amino-N-cyclopropyl-2-hydroxyhexanamide claim 14 , L-tartaric acid salt.22. A compound which is 3-amino-N-cyclopropyl-2-hydroxyhexanamide claim 14 , deoxycholic acid salt. This application claims the benefits of U.S. Provisional Application Ser. No. 60/782,976, ...

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20-06-2013 дата публикации

BIOCOMPATIBLE BIODEGRADABLE FUMAGILLIN ANALOG CONJUGATES

Номер: US20130158046A1
Принадлежит: Mersana Therapeutics, Inc

Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog. 124.-. (canceled)2631.-. (canceled)32. A composition comprising the compound or pharmaceutically acceptable salt of the compound of and a pharmaceutically acceptable carrier.3335.-. (canceled)36. A composition comprising a compound or pharmaceutically acceptable salt of the compound of and a pharmaceutically acceptable carrier.37. The composition of claim 36 , wherein the pharmaceutically acceptable carrier is suitable for injectable administration and the composition comprises an injectable dosage form.38. A method of treating cancer claim 25 , comprising administering to a subject in need thereof a compound or a pharmaceutically acceptable salt of a compound of claim 25 , in an amount effective to treat the cancer.39. The method of claim 38 , wherein the cancer is selected from the group consisting of anal claim 38 , astrocytoma claim 38 , leukemia claim 38 , lymphoma claim 38 , head and neck claim 38 , liver claim 38 , testicular claim 38 , cervical claim 38 , sarcoma claim 38 , hemangioma claim 38 , esophageal claim 38 , eye claim 38 , laryngeal claim 38 , mouth claim 38 , mesothelioma claim 38 , skin claim 38 , myeloma claim 38 , oral claim 38 , rectal claim 38 , throat claim 38 , bladder claim 38 , breast claim 38 , uterus claim 38 , ovary claim 38 , prostate claim 38 , lung claim 38 , colon claim 38 , ...

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19-09-2013 дата публикации

MITOCHONDRIAL TARGETED STIMULATORS OF APOPTOSIS

Номер: US20130244325A1
Принадлежит: THE ROCKEFELLER UNIVERSITY

Pro-apoptotic compounds having a tripartite structure: 5. A compound according to of formula A-L-B claim 1 , wherein B is chosen from Bcl2 inhibitors; monoamine oxidase inhibitors; and VDAC inhibitors.11. A method for inducing cell apoptosis comprising a exposing said cell to a compound according to .12. A method for inhibiting tumor growth comprising exposing said tumor to a compound according to . This application claims priority to U.S. Provisional Patent Application No. 61/533,288, filed Sep. 12, 2011, which is hereby incorporated herein by reference in its entirety.The following invention was made with Government support under contract number 5RO1 GM060124-12 awarded by NIH. The Government has certain rights in this invention.The invention relates to compounds that bind to and inhibit Inhibitor of Apoptosis (IAP) Proteins on the mitochondrial outer membrane. Therefore, these compounds are useful to induce apoptosis in cells and to inhibit the growth of tumors.Inhibitor of Apoptosis (IAP) proteins are commonly over-expressed in human tumors and thereby contribute to tumor cell survival. As a result, IAPs have become attractive drug targets in cancer therapy. Several small molecules targeting IAPs are in clinical trials. The design of these compounds is based on a short IAP-binding motif (IBM) that is present in natural IAP-antagonists, such as Reaper/Hid/Grim and mammalian Smac. Derivatives of the Hid IBM have proven most effective. They are reviewed in Vaux, D. L. (2009). 1:79, the contents of which are incorporated herein by reference. Although these IBM-mimetics show some promise, they have some serious limitations. In particular, all available compounds primarily target cIAP1/2, but are poor inhibitors of XIAP. Improved targeting of XIAP would be desirable, since this protein is a potent cell death inhibitor that is over-expressed in human tumors. It has been shown that inactivation of XIAP protects against tumorigenesis in the mouse, and that loss of the ...

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31-10-2013 дата публикации

EPOXY RESIN, EPOXY RESIN COMPOUND COMPRISING THE SAME, AND RADIANT HEAT CIRCUIT BOARD USING THE COMPOUND

Номер: US20130284502A1
Принадлежит: LG INNOTEK CO., LTD.

An epoxy resin compound including an epoxy resin, a hardening agent, and an inorganic filler as a main component is provided. The epoxy resin includes an epoxy resin represented by a chemical formula. Therefore, the epoxy resin having a mesogen structure that increases crystallinity is used, and thus thermal conductivity can be increased. Further, the epoxy resin is used as an insulating material for a printed circuit board, and thus a high radiant heat substrate can be provided. 4. The epoxy resin compound of claim 1 , wherein the inorganic filler is included in 40 wt % to 97 wt % with respect to a total weight of the epoxy resin compound.5. The epoxy resin compound of claim 1 , wherein the inorganic filler includes at least one of alumina claim 1 , boron nitride claim 1 , aluminum nitride claim 1 , crystalline silica and silicon nitride.6. The epoxy resin compound of claim 1 , wherein the epoxy resin is included in 3 wt % to 60 wt % with respect to a total weight of the epoxy resin compound.7. The epoxy resin compound of claim 1 , wherein the epoxy resin further comprises at least one non-crystalline epoxy resin.9. The epoxy resin compound of claim 1 , wherein the epoxy resin represented by Chemical Formula 1 is included in 12 wt % or more with respect to the whole epoxy resin.10. A radiant heat circuit board comprising:a metal plate;an insulating layer formed on the metal plate; anda circuit pattern formed on the insulating layer,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the insulating layer is formed by hardening the epoxy resin compound of .'}11. The radiant heat circuit board of claim 10 , wherein the inorganic filler is included in 40 wt % to 97 wt % with respect to a total weight of the epoxy resin compound.12. The radiant heat circuit board of claim 11 , wherein the inorganic filler includes at least one of alumina claim 11 , boron nitride claim 11 , aluminum nitride claim 11 , crystalline silica and silicon nitride.13. The radiant heat ...

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21-11-2013 дата публикации

TRICYCLIC LACTONES FOR TREATMENT OF CANCER

Номер: US20130310451A1
Принадлежит: Glactone Pharma Development AB

The present invention discloses novel compounds useful for the inhibition of IL-6/STAT signaling and/or PI3K/NF-κB signaling in the treatment of associated diseases or conditions, e.g. cancer. A pharmaceutical composition comprising such novel compounds, its use and a method thereof, is also disclosed. 3. A compound according to claim 1 , wherein R claim 1 , R′ claim 1 , R claim 1 , R′ claim 1 , R claim 1 , R′ claim 1 , Rand R′ are independently selected from the group consisting of H claim 1 , C1-5 alkyl claim 1 , aryl claim 1 , CH2aryl claim 1 , heteroaryl and CH2heteroaryl.4. (canceled)5. A compound according to claim 3 , wherein at least one of R claim 3 , R′ claim 3 , R claim 3 , R′ claim 3 , Rand R′ is selected from the group consisting of C1-5 alkyl claim 3 , aryl claim 3 , CH2aryl claim 3 , heteroaryl and CH2heteroaryl.6. A compound according to claim 5 , wherein at least one of R claim 5 , R′ claim 5 , Rand R′ is selected from the group consisting of C1-5 alkyl claim 5 , aryl claim 5 , CH2aryl claim 5 , heteroaryl and CH2heteroaryl.7. A compound according to claim 6 , wherein at least one of Rand R′ is selected from the group consisting of C1-5 alkyl claim 6 , aryl claim 6 , CH2aryl claim 6 , heteroaryl and CH2heteroaryl.8. (canceled)9. A compound according to claim 1 , wherein Rand R′ are independently selected from the group consisting of H and methyl.10. A compound according to claim 1 , wherein said compound is a compound according to formula (II) and Ris C1-5 alkyl or wherein said compound is a compound according to formula (I) and Ris OH claim 1 , OC1-5 claim 1 , OC1-5 fluoroalkyl claim 1 , or OC(O)C1-5 alkyl.11. A compound according to claim 1 , wherein R claim 1 , R′ claim 1 , R claim 1 , R′ R claim 1 , R′ claim 1 , Rand R′ are independently selected from the group consisting of H claim 1 , C1-5 alkyl claim 1 , aryl claim 1 , CH2aryl claim 1 , heteroaryl and CH2heteroaryl;{'sub': '5', 'R, if present, is OH, NHC0-5 alkyl, NHaryl or NHheteroaryl; and ...

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28-11-2013 дата публикации

COPOLYMERIZABLE SURFACTANTS

Номер: US20130317190A1
Принадлежит: Cognis IP Management GmbH

The invention relates to the use of compounds of the formula (I), R—CH(O—(AO)X)—CH—O—(AO)—CH—CH═CH, where: R denotes an alkyl radical which has 8 to 18 carbon atoms and can be saturated or unsaturated, straight-chain or branched; X denotes a sulfate or phosphate group or hydrogen; (AO) denotes an alkylene oxide unit, selected from the group consisting of ethylene oxide, propylene oxide or butylene oxide; n denotes a number in the range of 0 to 50; and m denotes zero or a number in the range of 1 to 30; as copolymerizable emulsifiers in the emulsion polymerization of olefinically unsaturated monomers. 3. The method of claim 2 , wherein X is a sulfate or phosphate group.4. The method of claim 3 , wherein the sulfate or phosphate group is in partly or wholly neutralized form.5. The method of claim 2 , wherein the degree of alkoxylation n is from 1 to 30.6. The method of claim 5 , wherein the degree of alkoxylation n is from 3 to 10 and (AO) is an ethylene oxide unit.7. A process for preparing a polymer by emulsion polymerization of an olefinically unsaturated monomer claim 1 , which process comprises utilizing said compound (I) according to as a copolymerizable emulsifier.8. The compound of claim 1 , wherein X is a sulfate or phosphate group.9. The compound of claim 8 , wherein the sulfate or phosphate group is in partly or wholly neutralized form.10. The compound of claim 1 , wherein the degree of alkoxylation n is from 1 to 30.11. The compound of claim 10 , wherein the degree of alkoxylation n is from 3 to 10 and (AO) is an ethylene oxide unit.12. The method of claim 2 , wherein the compound of formula (I) is copolymerized in the polymer.13. The method of claim 2 , further comprising initiating the reaction with potassium peroxodisulfate or a redox initiator.14. The method of claim 2 , wherein the compound of formula (I) is in salt form. The present invention lies within the polymer sector and relates to allyl ethers with a specific structure and also to their use as ...

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02-01-2014 дата публикации

NOVEL COMPOUND HAVING alpha-CYANOACRYLATE STRUCTURE, DYE, AND COLORED PHOTOSENSITIVE COMPOSITION

Номер: US20140005292A1
Принадлежит: Adeka Corp

A compound represented by the following general formula (1). In the formula, A represents a benzene ring, a naphthalene ring and the like, wherein these rings may be substituted with a halogen atom and the like, R 1 represents a hydrogen atom and the like, R 2 represents a C 1-35 hydrocarbon group having or not having at least one group selected from an epoxy group, 4-vinylphenyl group and a (meth)acryloyloxy group, or a hydrogen atom, wherein at least one of R 2 with n occurrences is a C 3-35 hydrocarbon group having at least one group selected from an epoxy group, a 4-vinylphenyl group and a (meth)acryloyloxy group, n represents an integer of 1 to 6, and X represents a nitrogen atom, an oxygen atom, a sulfur atom, a phosphorus atom, or an n-valent organic group having 35 or less carbon atoms.

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07-01-2021 дата публикации

Plasticizer composition and resin composition including the same

Номер: US20210002204A1
Принадлежит: LG Chem Ltd

Provided is a plasticizer composition, comprising: a cyclohexane-1,4-diester-based substance of the following Chemical Formula 1; an epoxidized alkyl ester composition comprising one or more compounds of the following Chemical Formula 2; and a citrate-based substance of the following Chemical Formula 3: wherein in Chemical Formula 1 to Chemical Formula 3: R 1 and R 2 each independently are a C8 alkyl group; R 3 is a C8 to C20 alkyl group comprising one or more epoxy groups; and R 4 to R 7 each independently are a C4 to C10 alkyl group.

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12-01-2017 дата публикации

NOVEL CYSTEINE PROTEASE INHIBITORS AND USES THEREOF

Номер: US20170008884A1
Принадлежит:

The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors. 123.-. (canceled)25: The method of claim 24 , wherein the disease is Alzheimer's Disease.27: The method of claim 26 , wherein the disease is Alzheimer's Disease.29: The method of claim 28 , wherein the subject has a neurodegenerative disease.30: The method of claim 29 , wherein the neurodegenerative disease is Alzheimer's Disease.31: The method of claim 24 , wherein the compound is formulated as a pharmaceutical composition.32: The method of claim 31 , wherein the pharmaceutical composition is formulated: as a sterile injectable solution or dispersion claim 31 , for intravenous or oral administration claim 31 , or for transmucosal or transdermal administration.411: The compound of claim (a) claim 31 , wherein the compound is selected from(a) (2S,3 S)-3-((S)-1-(2,6-difluorophenylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2 S,3 S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2R,3R)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3 S)-3-(1-(4-(4-fluorophenyl)thiazol-2-ylamino)-3-(1H-imidazol-4-yl)-1-oxopropan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3 S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-1-oxo-3-(thiazol-4-yl)propan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3 S)-3-((S)-1-(4-(4-ethynylphenyl)thiazol-2-ylamino)-1-oxo-3-(thiazol-4-yl)propan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3 S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-3-(1-methyl-1H-imidazol-4-yl)-1-oxopropan-2-ylcarbamoyl) ...

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14-01-2016 дата публикации

UNSATURATED FATTY ACID ESTER-BASED COMPOSITIONS USEFUL AS PLASTIC ADDITIVES

Номер: US20160009673A1
Принадлежит: Arkema Inc.

Compositions useful as plastic additives may be prepared from renewable resources such as vegetable oils by functionalizing an unsaturated fatty acid ester with epoxy, acyloxy, and optionally alkoxy groups. 1. A compound comprised of a fatty acid ester moiety , wherein the fatty acid ester moiety comprises at least one epoxy group and wherein the fatty acid ester moiety is substituted at least with a first substituent which is a first acyloxy group and with a second substituent which is a second acyloxy group , which may be the same as or different from the first acyloxy group , or an alkoxy group , wherein the first substituent and the second substituent are substituted on adjacent carbon atoms in the fatty acid ester moiety.2. The compound of claim 1 , wherein the fatty acid ester moiety is selected from the group consisting of fatty acid monoesters claim 1 , monoglycerides claim 1 , diglycerides claim 1 , triglycerides claim 1 , and fatty acid esters of polyols other than glycerin.3. The compound of claim 1 , wherein the first acyloxy group is a C2-C24 aliphatic acyloxy group.4. The compound of claim 1 , wherein the first acyloxy group has a structure R—C(═O)—O— claim 1 , wherein R is a straight chain claim 1 , branched or alicyclic claim 1 , saturated or unsaturated hydrocarbyl group containing one to 23 carbon atoms.5. The compound of claim 1 , wherein the first acyloxy group is an acetoxy group.6. The compound of claim 1 , wherein the second substituent is a C2-C24 aliphatic acyloxy group.7. The compound of claim 1 , wherein the second substituent has a structure R—C(═O)—O— claim 1 , wherein R is a straight chain claim 1 , branched or alicyclic claim 1 , saturated or unsaturated hydrocarbyl group containing one to 23 carbon atoms.8. The compound of claim 1 , wherein the second substituent is a C1-C24 alkoxy group.9. The compound of claim 1 , wherein the second substituent has a structure R1—O— claim 1 , wherein R1 is a straight chain claim 1 , branched or ...

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14-01-2021 дата публикации

TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF

Номер: US20210009501A1
Принадлежит: CORSAIR PHARMA, INC.

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension. 123-. (canceled)25. The method of claim 24 , wherein:{'sup': '3', 'sub': 1', '6, 'Rin each occurrence independently is C-Calkyl;'}{'sup': 4', '5', '4', '5, 'sub': 1', '3, 'Rand Rin each occurrence independently are hydrogen or C-Calkyl, or Rand Rand the carbon atom to which they are connected form a cyclopropyl ring;'}{'sup': 6', '3, 'Rin each occurrence independently is hydrogen or R;'}j in each occurrence independently is 0 or 1; andm in each occurrence independently is 1 or 2.28. The method of claim 24 , wherein Ris hydrogen and —ORis derivatized.29. The method of claim 24 , wherein Ris hydrogen and —ORis derivatized.30. The method of claim 24 , wherein both —OR′ and —ORare derivatized claim 24 , optionally with the same group.32. The method of claim 24 , wherein the compound is administered orally.33. The method of claim 24 , wherein the compound is administered parenterally.34. The method of claim 33 , wherein the compound is administered subcutaneously or intravenously.35. The method of claim 24 , wherein the compound is administered topically.36. The method of claim 35 , wherein the compound is administered transdermally or by oral inhalation.37. The method of claim 36 , wherein the compound is administered via a transdermal patch. The present application is a continuation of and claims priority to and the benefit of U.S. application Ser. No. 16/580,828 filed on Sep. 24, 2019, which is a continuation of Ser. No. 16/039,566, filed on Jul. 19, 2018 (now U.S. Pat. No. 10,464,878, granted on Nov. 5, 2019), which is a continuation of Ser. No. 15/617,243 filed Jun. 8, 2017 (now U.S. Pat. No. 10,053,414, granted Aug. 21, 2018), which is a continuation of Ser. No. 15/178,637 filed Jun. 10, ...

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10-01-2019 дата публикации

TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF

Номер: US20190010112A1
Принадлежит:

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension. 120-. (canceled)22. The pharmaceutical composition of claim 21 , which is formulated for transdermal delivery of the compound.23. The pharmaceutical composition of claim 22 , which is configured as a transdermal patch.25. The method of claim 24 , wherein the medical condition is selected from the group consisting of pulmonary hypertension claim 24 , pulmonary fibrosis claim 24 , ischemic diseases claim 24 , peripheral vascular disease claim 24 , peripheral ischemic lesions on the skin claim 24 , critical limb ischemia claim 24 , heart failure claim 24 , atherogenesis claim 24 , inflammatory diseases claim 24 , diabetic neuropathic foot ulcer claim 24 , kidney malfunction and failure claim 24 , tumors claim 24 , cancers claim 24 , and pain associated with each of the preceding conditions.26. The method of claim 25 , wherein the medical condition is pulmonary hypertension.27. The method of claim 26 , wherein the medical condition is pulmonary arterial hypertension.28. The method of claim 24 , wherein the compound is administered topically.29. The method of claim 28 , wherein the compound is administered transdermally.30. The method of claim 29 , wherein the compound is administered via a transdermal patch.31. The method of claim 28 , wherein the compound is administered pulmonarily by oral inhalation.32. The method of claim 24 , wherein the compound is administered orally.33. The method of claim 24 , wherein the compound is administered parenterally.34. The method of claim 33 , wherein the compound is administered subcutaneously or intravenously.35. The method of claim 24 , further comprising administering an additional therapeutic agent.36. The method of claim 35 , wherein the additional ...

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14-01-2021 дата публикации

COALESCING AGENTS FOR WATERBORNE COATINGS

Номер: US20210009844A1
Принадлежит:

Compounds comprising one or more functionalized fatty acid esters, which may be derived from bio-based oils, are used as a low-VOC coalescent agent (i.e., a coalescent agent having a low content of volatile organic compounds) in waterborne coating compositions. The functional group can be epoxide, vicinal diol, hydroxy phosphotriester, hydroxy ester, hydroxyl alkyl ester, hydroxyl benzyl ester, hydroxy ether, hydroxy amino, hydroxy sulfide, hydroxy nitrile, hydroxy amine, terminal alcohol, thiiran, ketone, or cyclic carbonate. The present disclosure also relates to waterborne coating compositions comprising these functionalized fatty acid esters. 1. A coalescent agent for waterborne coatings , wherein the coalescent agent comprises one or more functionalized fatty acid C1-C22 alkyl or benzyl esters , preferably C2-C8 alkyl or benzyl esters , wherein said functionalized fatty acid esters have one or more functional groups per molecule selected from the group consisting of epoxides , excluding coalescent agents of epoxidized fatty acid methyl esters obtained from soybean oil where the alkyl is Cl (methyl epoxy esters derived from soybean oil).2. The coalescent agent of claim 1 , wherein said functionalized fatty acid esters are selected from the group consisting of monoesters claim 1 , fatty acid monoglycerides claim 1 , fatty acid esters of aliphatic mono-alcohols claim 1 , fatty acid esters of aromatic alcohols claim 1 , fatty acid esters of benzyl alcohol claim 1 , fatty acid diesters claim 1 , fatty acid diglycerides claim 1 , fatty acid esters of diols wherein both hydroxyl groups are esterified with fatty acid claim 1 , fatty acid triesters claim 1 , fatty acid triglycerides claim 1 , fatty acid esters of triols other than glycerin in which all three hydroxyl groups are esterified with fatty acid claim 1 , fatty acid esters of polyols containing more than three hydroxyl groups per molecule claim 1 , or mixtures thereof and preferably is a monoester claim 1 , ...

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09-01-2020 дата публикации

PROCESSES FOR PREPARING PARTIALLY FLUORINATED EPOXIDES AND PERFLUORINATED EPOXIDES AND COMPOSITIONS RELATED THERETO

Номер: US20200010439A1
Принадлежит: THE CHEMOURS COMPANY FC, LLC

This application relates to the preparation of partially fluorinated epoxides and perfluorinated epoxides which may be useful in various applications including refrigerants, heat transfer media, high-temperature heat pumps, organic Rankine cycles, fire extinguishing/fire suppression, propellants, foam blowing, solvents, gaseous dielectrics, and/or cleaning fluids. Compositions comprising the fluorinated epoxide compounds are also provided. 2. (canceled)3. (canceled)4. The process of claim 1 , wherein Rand Rare each independently H or F; and Rand Rare each independently selected from partially fluorinated or perfluorinated Calkyl.5. The process of claim 1 , wherein the hypohalite salt is selected from NaOCl claim 1 , KOCl claim 1 , NaOBr claim 1 , and Ca(OCl).6. (canceled)7. The process of claim 1 , wherein the cationic phase transfer catalyst is a quaternary ammonium salt or a quaternary phosphonium salt.8. (canceled)9. The process of claim 1 , the cationic phase transfer catalyst has formula (R)(R)(R)(R)NX or (R)(R)(R)(R)PX claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from Calkyl claim 1 , Ccycloalkyl claim 1 , 4-14 membered heterocycloalkyl claim 1 , Caryl claim 1 , 5-14 membered heteroaryl claim 1 , Ccycloalkyl-Calkylene claim 1 , 4-14 membered heterocycloalkyl-Calkylene claim 1 , Cmembered aryl-Calkylene claim 1 , and 5-14 membered heteroaryl-Calkylene claim 1 , each of which is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 groups independently selected from OH claim 1 , Calkoxy claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Cfluoroalkyl claim 1 , di-(Calkyl)amino claim 1 , Ccycloalkyl claim 1 , 4-14 membered heterocycloalkyl claim 1 , Cmembered aryl claim 1 , and 5-14 membered heteroaryl; and X is an anion.10. The process of claim 1 , wherein the cationic phase transfer catalyst has formula (R)(R)(R)(R)NX claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare eah independently selected ...

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17-01-2019 дата публикации

Selective androgen receptor degrader (sard) ligands and methods of use thereof

Номер: US20190015387A1

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

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18-01-2018 дата публикации

TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF

Номер: US20180016222A1
Принадлежит:

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension. 120-. (canceled)22. The pharmaceutical composition of claim 21 , wherein n is an integer from 1 to 6.24. The pharmaceutical composition of claim 23 , wherein both Rand Rare hydrogen claim 23 , and p is an integer from 1 to 9 or from 1 to 5 (or each occurrence of Rand Ris hydrogen claim 23 , and q is an integer from 0 to 8 or from 0 to 4).27. The pharmaceutical composition of claim 21 , wherein —O—Z—COH is —O-cycloalkyl-COH claim 21 , —O—CH-cycloalkyl-COH claim 21 , —O-cycloalkyl-CH—COH claim 21 , or —O—CH-cycloalkyl-CH—COH claim 21 , and for each of the preceding moieties -cycloalkyl- is:1,2-cyclopropyl (cis or trans); or1,3-cyclobutyl (cis or trans) or 1,2-cyclobutyl (cis or trans); or1,3-cyclopentyl (cis or trans) or 1,2-cyclopentyl (cis or trans); or1,4-cyclohexyl (cis or trans), 1,3-cyclohexyl (cis or trans), or 1,2-cyclohexyl (cis or trans).29. The pharmaceutical composition of claim 21 , which is formulated for transdermal delivery of the compound of Formula (II).30. The pharmaceutical composition of claim 29 , which is configured as a transdermal patch.32. The compound of claim 31 , wherein n is 3 claim 31 , 4 claim 31 , 5 or 6.34. The compound of claim 33 , wherein p is 2 claim 33 , 3 claim 33 , 4 or 5.35. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt claim 31 , solvate claim 31 , hydrate claim 31 , clathrate claim 31 , polymorph or stereoisomer thereof claim 31 , and one or more pharmaceutically acceptable excipients or carriers.36. The pharmaceutical composition of claim 35 , which is formulated for transdermal delivery of the compound.37. A method of treating a medical condition responsive to treatment with treprostinil claim 31 , ...

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22-01-2015 дата публикации

DOCOSAHEXAENOYL ETHANOLAMIDES

Номер: US20150025257A1
Принадлежит: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.

The invention describes novel mono or dihydroxy docosahexaenoic acid (DHA) analogues, their preparation, isolation, identification, purification and uses thereof. 114.-. (canceled)16. The compound of claim 15 , wherein Pand Pare both hydrogen atoms.17. The compound of claim 15 , wherein Z is —C(O)NRR—OH.18. The compound of claim 17 , wherein one Ris H and the second Ris ethyl.20. The purified compound of claim 19 , wherein Pand Pare both hydrogen atoms.21. The purified compound of claim 19 , wherein Z is —C(O)ORand Rof Z is a hydrogen atom.22. The purified compound of claim 19 , wherein Z is —C(O)NRR—OH.23. The purified compound of claim 22 , wherein one Ris H and the second Ris ethyl.24. The compound of claim 15 , wherein the hydrogen atom on one or more hydroxyl containing carbon atoms is substituted with an alkyl group.25. The purified compound of claim 19 , wherein the hydrogen atom on one or more hydroxyl containing carbon atoms is substituted with an alkyl group.26. The compound of claim 15 , wherein the alkyl group is a methyl group.27. The purified compound of claim 19 , wherein the alkyl group is a methyl group.28. The compound of claim 15 , further comprising a pharmaceutically acceptable carrier.29. The compound of claim 19 , further comprising a pharmaceutically acceptable carrier.30. A method to treat or prevent inflammation claim 15 , cancer claim 15 , neurodegeneration claim 15 , memory loss claim 15 , neuroinflammation or traumatic brain injury comprising the step of administering to an individual in need thereof claim 15 , an effective amount of the compound of .31. A method to treat or prevent inflammation claim 19 , cancer claim 19 , neurodegeneration claim 19 , memory loss claim 19 , neuroinflammation or traumatic brain injury comprising the step of administering to an individual in need thereof claim 19 , an effective amount of the compound of .32. A method to treat neural development claim 15 , fetal development claim 15 , homeostasis claim 15 ...

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31-01-2019 дата публикации

ORGANIC COMPOUND, THREE-DIMENSIONAL ORGANIC FRAMEWORK FORMED BY USING ORGANIC COMPOUND, SEPARATION SIEVE AND OPTICAL LAYER, WHICH COMPRISE ORGANIC FRAMEWORK, AND OPTICAL DEVICE COMPRISING OPTICAL LAYER AS OPTICAL AMPLIFICATION LAYER

Номер: US20190031586A1

An organic compound, a three-dimensional organic structure formed by using the organic compound, a separation sieve and an optical layer having the organic structure, and an optical device having the optical layer as an optical amplification layer are provided. The organic structure includes a plurality of organic molecules self-assembled by non-covalent bonding. Each of the unit organic molecules has an aromatic ring, a first pair of substituents being connected to immediately adjacent positions of substitutable positions of the aromatic ring, and a second pair of substituents being connected to immediately adjacent positions of remaining substitutable positions of the aromatic ring. The unit organic molecules are self-assembled by van der Waals interaction, London dispersion interaction or hydrogen bonding between the first and the second pairs of the substituents and by pi-pi interactions between the aromatic rings. 147-. (canceled)48. A three-dimensional organic structure comprising a plurality of unit organic molecules which are self-assembled to form the three-dimensional organic structure ,wherein each of the unit organic molecules has at least one aromatic ring, a first pair of substituents being connected to immediately adjacent positions of substitutable positions of the aromatic ring, and a second pair of substituents being connected to immediately adjacent positions of substitutable positions of the aromatic ring,{'sub': c', 'd', 'e', 'c', 'd', 'e', 'c', 'd', 'e', 'c', 'd', 'e', 'c', 'd', 'e', 'a', 'c', 'd', 'e', '2, 'wherein the substituents have terminal groups, independently, including a group selected from the group consisting of —CRRR, —OH, —COOH, —CHO, —SH, —COCRRR, —COOCRRR, —CR═CRR, —CN, —N═C═O, —C═N═N—CRRR, —C≡CR, —NHCRRR, or —NH,'}wherein the unit organic molecules contained in one layer of the three-dimensional structure are self-assembled by van der Waals interaction, London dispersion interaction or hydrogen bonding between the terminal ...

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09-02-2017 дата публикации

Hydroxamic acids and uses thereof

Номер: US20170036996A1
Принадлежит: Hawaii Biotech Inc

Compounds of formula I are provided: R 1 is an alkoxy or O(CH 2 ) p X, p is an integer from 2 to 3 and X is OH, NH 2 , or CO 2 H, m is an integer from 0 to 5, n is an integer from 0 to 5, each R 2 is independently selected from hydrogen, alkenyl, hydroxyalkyl, alkoxymethyl, heterocyclyl, hetereocyclylmethyl, amino, amido, hydroxamido, any of which may be optionally substituted with one or more of acyl, alkyl, alkoxy, hydroxyalkyl, or halogen, each R 3 is independently selected from hydrogen, halogen, alkyl, alkenyl, carboxy, hydroxymethyl, amido, and at least one of R 2 and R 3 is not hydrogen.

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12-02-2015 дата публикации

Novel Cysteine Protease Inhibitors and Uses Thereof

Номер: US20150045393A1
Принадлежит:

The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors. 10. The compound of claim 1 , wherein the compound is selected from(2S,3S)-3-((S)-1-(2,6-difluorophenylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2R,3R)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-(1-(4-(4-fluorophenyl)thiazol-2-ylamino)-3-(1H-imidazol-4-yl)-1-oxopropan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-1-oxo-3-(thiazol-4-yl)propan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-((S)-1-(4-(4-ethynylphenyl)thiazol-2-ylamino)-1-oxo-3-(thiazol-4-yl)propan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-3-(1-methyl-1H-imidazol-4-yl)-1-oxopropan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-((S)-1-((1-(4-fluorophenyl)-1H-1,2,3-triazol-4-yl)methylamino)-1-oxo-3-(thiazol-4-yl)propan-2-ylcarbamoyl)oxirane-2-carboxylic acid; and(2S,3S)-3-((S)-1-((1-(4-bromophenyl)-1H-1,2,3-triazol-4-yl)methylamino)-1-oxo-3-(thiazol-4-yl)propan-2-ylcarbamoyl)oxirane-2-carboxylic acid.11. The compound of claim 1 , wherein the compound is selected from(2S,3S)-3-((S)-1-(2,6-difluorophenylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-((S)-1-(4-(4-fluorophenyl)thiazol-2-ylamino)-4-methyl-1-oxopentan-2-ylcarbamoyl)oxirane-2-carboxylic acid;(2S,3S)-3-(1-(4-(4-fluorophenyl)thiazol-2-ylamino)-3-(1H-imidazol-4-yl)-1-oxopropan-2-ylcarbamoyl ...

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16-02-2017 дата публикации

Oxaspiro[2.5]Octane Derivatives and Analogs

Номер: US20170044122A1
Принадлежит: Zafgen, Inc.

The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity. 4. The compound of claim 1 , wherein Ris Cstraight saturated alkyl.5. The compound of claim 1 , wherein Ris selected from the group consisting of Cstraight saturated alkyl or Cstraight saturated alkyl.6. The compound of claim 1 , wherein Ris Calkylene substituted on the terminal end by —C(O)OH claim 1 , —C(O)—O-Me claim 1 , or C(O)-Et.8. A pharmaceutically acceptable composition comprising a compound of and a pharmaceutically acceptable excipient.9. A method of treating and/or controlling obesity claim 1 , comprising administering to a patient in need thereof an effective amount of the compound of .10. The method of claim 9 , wherein the patient is a human.11. The method of claim 10 , wherein the patient has a body mass index greater than or equal to about 25 kg/mbefore the administration.12. The method of claim 1 , wherein after administration claim 1 , thioredoxin 1 is not significantly present in the testes of male patient.14. The compound of claim 13 , wherein Z is C. This application is a continuation of U.S. patent application Ser. No. 14/003,906, filed Oct. 29, 2014, which is a national stage filing under U.S.C. §371 of PCT/US2012/028068, filed Mar. 7, 2012, which claims priority to U.S. Provisional Patent Application No. 61/450,301 filed Mar. 8, 2011, all of which are hereby incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or ...

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19-02-2015 дата публикации

AMIDE-LINKED PERFLUOROPOLYETHER THIOL COMPOUNDS AND PROCESSES FOR THEIR PREPARATION AND USE

Номер: US20150051362A1
Принадлежит:

A perfluoropolyether thiol compound comprises a perfluoropolyether segment, at least one mercapto group (—SH), and at least one intervening divalent carbonylimino moiety (—C(═O)—NR—, wherein R is hydrogen or alkyl). The compound can be produced, for example, by a ring-opening reaction of thiolactones with perfluoropolyether-substituted, primary or secondary amines. The compound can be used, for example, as a polymerization chain transfer agent, as an intermediate for the preparation of functional group-containing fluorochemical derivatives such as disulfides, and as a fluorinated surface treatment. 2. A process for preparing a perfluoropolyether thiol compound comprises (a) providing at least one thiolactone compound; (b) providing at least one perfluoropolyether-substituted , primary or secondary amine compound; and (c) combining the thiolactone compound and the perfluoropolyether-substituted , primary or secondary amine compound.3. The process of claim 2 , wherein said thiolactone compound is selected from thiolactone compounds having from 5 to 8 ring members claim 2 , and mixtures thereof4. The process of claim 2 , wherein said thiolactone compound is gamma-butyrothiolactone.5. The process of claim 2 , wherein said perfluoropolyether-substituted claim 2 , primary or secondary amine compound is amide-linked.6. A process comprising polymerizing at least one vinyl monomer in the presence of at least one polymerization initiator and at least one perfluoropolyether thiol compound of formula (II) above claim 2 , wherein R is hydrogen or alkyl; Q is a divalent organic linking group selected from —CHCHCH—[NH—C(═O)]—CHCHCH claim 2 ,{'sub': 2', '2', '2', '3', '2', '2', '2, '—CHCHCH—[N(CH)—C(═O)]—CHCHCH—,'}{'sub': 2', '2', '2', '3', '2', '2', '2', '2', '2', '2, '—CHCHCH—[N(CH)—C(═O)]—CHChCh—S—C(═O)—CHCHCh—,'}{'sub': 2', '2', '2', '2', '2, '—CHCH—[NH—C(═O)]≧CHCHCH—,'}{'sub': 2', '2', '2', '2, '—CHCH—[O—C(═O)]—CHCH—,'}{'sub': 2', '2', '2', '2', '2', 'f, 'claim-ref': {'@idref ...

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08-05-2014 дата публикации

Fungicidal Alkyl-Substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol Compounds

Номер: US20140128255A1
Принадлежит: BASF SE

The present invention relates to the use of alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.

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03-03-2016 дата публикации

PKC-ACTIVATING COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20160060236A1

The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. 1. A method of activating an epsilon isoform of protein kinase C comprising contacting the epsilon isoform of protein kinase C with an effective amount of at least one compound chosen from: a cis-polyunsaturated fatty alcohol in which at least one of the double bonds is replaced by a cyclopropyl group; a cis-polyunsaturated fatty acid in which at least one of the double bonds is replaced by an epoxyl group; a cis-polyunsaturated fatty acid ester in which at least one of the double bonds is replaced by an epoxy group; a cis-polyunsaturated fatty alcohol in which at least one of the double bonds is replaced by an epoxyl group; a cis-monounsaturated fatty acid in which the double bond is replaced by a cyclopropyl group; a cis-monounsaturated fatty acid ester in which the double bond is replaced by a cyclopropyl group; and a cis-monounsaturated fatty alcohol in which the double bond is replaced by a cyclopropyl group.23-. (canceled)4. The method of claim 1 , wherein the at least one compound is a cis-polyunsaturated fatty alcohol in which at least one of the double bonds is replaced by a cyclopropyl group and the polyunsaturated fatty acid from which the fatty alcohol is derived is chosen from arachidonic acid claim 1 , docosapentaenoic acid claim 1 , docosahexaenoic acid claim 1 , eicosapentaenoic acid claim 1 , linoleic acid claim 1 , γ-linoleic acid claim 1 , α-linolenic acid claim 1 , eicosatetraenoic acid claim 1 , adrenic acid claim 1 , and derivatives thereof.510-. (canceled)11. The method of claim 1 , wherein the at least one compound is ...

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28-02-2019 дата публикации

2,3-Epoxy Succinyl Derivative, Preparation Method and Use Thereof

Номер: US20190062290A1

The present invention relates to a 2,3-epoxy succinyl derivative, a preparation method and a use thereof, in particular, the present invention relates to a compound represented by Formula (1), a racemate or an optical isomer thereof, a solvate thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present invention has good inhibitory activity and/or selectivity against cathepsin, especially Cathepsin B, can be used in the treatment of multiple diseases associated with cathepsin, for example, osteoporosis, rheumatoid arthritis and osteoarthritis that are associated with Cathepsin K, Ebola virus infection, a degenerative disease and an autoimmune disease that are associated with Cathepsin L, S, especially Cathepsin B-related tumor diseases, such as gastric cancer, cervical cancer, lung cancer, breast cancer, prostate cancer, bladder cancer, colon cancer, neuroglioma, and melanoma. 2. The compound represented by Formula (1) claim 1 , a racemate or an optical isomer thereof claim 1 , a solvate thereof claim 1 , or a pharmaceutically acceptable salt thereof according to claim 1 ,wherein,{'sub': 1', '1', '10', '3', '10', '2', '10', '2', '10, 'Rrepresents a hydrogen atom, C-Clinear or branched alkyl, C-Ccycloalkyl, C-Clinear or branched alkenyl, C-Clinear or branched alkynyl;'}{'sub': 2', '1', '10', '3', '10', '1', '10', '3', '10', '2', '10', '2', '10', '1', '6', '1', '6', '1', '10', '3', '10', '1', '10', '3', '10', '2', '10', '2', '10', '1', '6', '1', '6', '1', '10', '1', '10', '1', '10', '1', '10', '1', '10, 'Rrepresents a hydrogen atom, C-Clinear or branched alkyl, C-Ccycloalkyl, C-Calkylthio, C-Ccycloalkylthio, C-Clinear or branched alkenyl, C-Clinear or branched alkynyl, aryl, aryl-C-Calkyl, heterocyclyl or heterocyclyl-C-Calkyl, optionally, wherein, the C-Clinear or branched alkyl, C-Ccycloalkyl, C-Calkylthio, C-Ccycloalkylthio, C-Clinear or branched alkenyl, C-Clinear or branched alkynyl, aryl, aryl-C-Calkyl, heterocyclyl or ...

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10-03-2016 дата публикации

METHODS AND COMPOSITIONS FOR WOUND HEALING

Номер: US20160068499A1
Принадлежит:

The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described. 1. A method of promoting wound healing in a subject comprising administering to the subject an epoxy-tigliane compound or a pharmaceutically acceptable salt thereof.2. The method according to wherein the promoting wound healing comprises increasing the rate of wound healing claim 1 , reducing scarring in the wound tissue or both increasing the rate of wound healing and reducing scarring in wound tissue.3. (canceled)4. (canceled)5. The method according to wherein the promoting wound healing comprises improving the cosmetic outcome of the healed wound.6. The method according to wherein the wound is a chronic wound claim 1 , an acute wound or an existing wound.7. The method according to wherein the epoxy-tigliane compound is in the form of a plant extract.8FontaineaHylandia. The method according to wherein the plant extract is obtainable from a plant which is a species or a species.12. The method according to wherein Ris hydrogen and Ris OH or —OC(O)Calkyl claim 9 , —OC(O)Calkenyl or —OC(O)Calkynyl claim 9 , or Rand Rtogether form a carbonyl group.13. The method according to wherein Ris hydrogen or —Calkyl.14. The method according to wherein Rand Rare independently hydrogen or —OH claim 9 , —OC(O)Calkyl claim 9 , —OC(O)Calkenyl or —OC(O)Calkynyl or Rand Rtogether form a double bond or an epoxide.15. The method according to wherein Ris hydrogen or —Calkyl.16. The method according to wherein Ris —OH claim 9 , —OC(O)Calkyl claim 9 , —OC(O)Calkenyl claim 9 , —OC(O)Calkynyl claim 9 , —OC(O)aryl wherein the aryl group is optionally substituted claim 9 , —OC(O) ...

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15-03-2018 дата публикации

METHOD FOR SYNTHESIZING A PRECURSOR OF A SINGLE DAIRY-LACTONE ISOMER

Номер: US20180072693A1
Принадлежит:

This disclosure provides a method for preparing a precursor of a single dairy-lactone isomer, methods of preparing a single dairy-lactone isomer, and to the organoleptic uses thereof. 6. The method according to claim 5 , wherein the dotted line of said molecule of formula (III) represents a single carbon-carbon bond obtained by hydrogenating an α claim 5 ,β-unsaturated lactone.7. The method according to claim 5 , wherein said molecule of formula (III) is obtained by oxidizing a dihydrolevoglucosenone in the presence of a peracid claim 5 , followed by hydrolysis claim 5 , said dihydrolevoglucosenone being obtained by hydrogenating a levoglucosenone.11. A pure isomer of dairy-lactone of Z—R claim 1 , Z—S claim 1 , E-R or E-S conformation obtained by the method according to .12. A pure isomer of dairy-lactone according to claim 11 , wherein the pure isomer of dairy-lactone is of Z—S conformation.13. A use of a pure isomer of dairy-lactone obtained by the method according to claim 1 , as a food flavor.14. The use of a pure isomer of dairy-lactone obtained by the method according to claim 1 , as an odorant molecule to flavor a food or cosmetic product.15. A bakery product comprising a pure isomer of dairy-lactone obtained by the method according to claim 1 , to give a “buttered” note to said bakery product.16. A product based on vegetable milk or animal milk substitute having a pure isomer of dairy-lactone obtained by the method according to claim 1 , to give a “milky” note to said product. This application is a national phase entry under 35 U.S.C. § 371 of International Patent Application PCT/FR2016/050813, filed Apr. 8, 2016, designating the United States of America and published as International Patent Publication WO 2016/162646 A1 on Oct. 13, 2016, which claims the benefit under Article 8 of the Patent Cooperation Treaty to French Patent Application Serial No. 1553112 filed Apr. 10, 2015.This application is in the field of aromatic molecules, their manufacturing ...

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05-06-2014 дата публикации

Tiglien-3-one derivatives

Номер: US20140155479A1
Принадлежит: QBiotics Pty Ltd

The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment.

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05-05-2022 дата публикации

Hydroxy fatty acid synthesis

Номер: US20220135902A1
Принадлежит: US Department of Agriculture USDA

The invention relates to methods for the synthesis of hydroxy fatty acids from unsaturated fatty acids via epoxidation and catalytic hydrogenation.

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14-04-2016 дата публикации

OXIRAN AMINES

Номер: US20160102067A1
Автор: OLSEN Jens Steen
Принадлежит: V-BIOTEK HOLDING APS

Disclosed herein are oxiran amines useful for the treatment of a variety of diseases. The oxiran amines are useful in the manufacture of pharmaceutical compositions. The pharmaceutical composition may be used for the treatment or prevention of a disease caused by a virus having a lipid membrane or the pharmaceutical composition may be used for diseases requiring cell proliferation or immune-regulation. 2. The compound according to claim 1 , wherein Rrepresents a straight or branched alkyl or alkenyl group containing 5 or more carbon atoms.3. The compound according to claim 1 , wherein Rrepresents a straight or branched alkenyl group having 1 to 4 double bonds.4. The compound according to claim 3 , wherein a double bond is located at the third claim 3 , sixth claim 3 , or nineth carbon atom counted from the methyl end of the alkenyl group.7. The composition according to claim 3 , comprising the compound according to any of the to and pharmaceutically acceptable auxiliaries.8. The compound according to claim 1 , for use in a method for treatment of the human or animal body by therapy.9. The compound according to claim 1 , for use in prevention or treatment of a viral infection.10. The compound according to claim 1 , wherein said virus is selected from the group of viruses having a lipid membrane.11. The compound according to claim 1 , wherein the virus is herpes simplex virus (HSV) claim 1 , influenza virus claim 1 , human papilloma virus (HPV) or human immunodeficiency virus (HIV).12. The compound according to for use in proliferating cells.13. The compound according to claim 1 , wherein it is used for treatment of wounds claim 1 , such as a surgical wound or burn claim 1 , diseases in the mouth cavity claim 1 , periodontal disease claim 1 , infection in the eye or the adnexa of the eye claim 1 , cold sores claim 1 , and pharyngitis.14. The compound according to claim 13 , wherein said periodontal disease is selected among gingivitis claim 13 , periodontitis claim 13 ...

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16-04-2015 дата публикации

OXIDATIVE DEGRADATION PRODUCTS OF ATROVASTATIN CALCIUM

Номер: US20150105551A1
Принадлежит:

The present invention relates to oxidative degradation products of atorvastatin calcium and the process of the preparation thereof. The present invention also relates to atorvastatin calcium substantially free of oxidative degradation products and the pharmaceutical compositions containing such atorvastatin calcium. 1. 4-[6-(4-Fluoro-phenyl)-6-hydroxy-1b-isopropyl-6a-phenyl-1a-phenylcarbamoyl-hexahydro-1 ,2-dioxa-5a-aza-cyclopropa[a]inden-3-yl]-3-(R)-hydroxy-butyric acid.2. 4-(4-Fluoro-phenyl)-2 ,4-dihydroxy-2-isopropyl-5-phenyl-3 ,6-dioxa-bicyclo[3.1.0]hexane-1-carboxylic acid phenylamide.3. 4-[1b-(4-Fluoro-phenyl)-6-hydroxy-6-isopropyl-1a-phenyl-6a-phenylcarbamoyl-hexahydro-1 ,2-dioxa-5a-aza-cyclopropa[a]inden-3-yl]-3-(R)-hydroxy-butyric acid.46.-. (canceled)7. A process for the preparation of a compound selected from the group consisting of 4-[6-(4-Fluoro-phenyl)-6-hydroxy-1b-isopropyl-6a-phenyl-1a-phenylcarbamoyl-hexahydro-1 ,2-dioxa-5a-aza-cyclopropa[a]inden-3-yl]-3-(R)-hydroxy-butyric acid , 4-(4-Fluoro-phenyl)-2 ,4-dihydroxy-2-isopropyl-5-phenyl-3 ,6-dioxa-bicyclo[3.1.0]hexane-1-carboxylic acid phenylamide , 4-[1b-(4-Fluoro-phenyl)-6-hydroxy-6-isopropyl-1a-phenyl-6a-phenylcarbamoyl-hexahydro-1 ,2-dioxa-5a-aza-cyclopropa[a]inden-3-yl]-3-(R)-hydroxy-butyric acid and 3-(4-Fluoro-benzoyl)-2-isobutyryl-3-phenyl-oxirane-2-carboxylic acid phenylamide characterized in that a solution of an atorvastatin salt is exposed to sunlight or artificial sunlight.8. The process according to wherein the atorvastatin salt is selected from the group consisting of atorvastatin calcium claim 7 , sodium claim 7 , potassium claim 7 , magnesium and ammonium.9. The process according to wherein it further comprises one or more isolation steps.10. The process according to wherein the isolation step is selected from the group consisting of preparative normal phase and reverse phase chromatography.11. The process according to wherein in preparative normal phase chromatography silica gel or ...

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26-03-2020 дата публикации

TREPROSTINIL DERIVATIVES AND COMPOSITIONS AND USES THEREOF

Номер: US20200095186A1
Принадлежит: CORSAIR PHARMA, INC.

The present disclosure provides treprostinil derivatives that can act as prodrugs of treprostinil. The treprostinil derivatives can be used to treat any conditions responsive to treatment with treprostinil, including pulmonary hypertension, such as pulmonary arterial hypertension. 123-. (canceled)26. The transdermal patch of claim 25 , wherein both Rand Rare hydrogen.29. The transdermal patch of claim 24 , wherein —O—Z—COH is —O-cycloalkyl-COH claim 24 , —O—CH-cycloalkyl-COH claim 24 , —O-cycloalkyl-CH—COH claim 24 , or —O—CH-cycloalkyl-CH—COH claim 24 , and for each of the preceding moieties -cycloalkyl- is:1,2-cyclopropyl (cis or trans); or1,3-cyclobutyl (cis or trans) or 1,2-cyclobutyl (cis or trans); or1,3-cyclopentyl (cis or trans) or 1,2-cyclopentyl (cis or trans); or1,4-cyclohexyl (cis or trans), 1,3-cyclohexyl (cis or trans), or 1,2-cyclohexyl (cis or trans).31. The transdermal patch of claim 24 , further comprising a drug reservoir and a semi-permeable membrane.32. The transdermal patch of claim 24 , further comprising a drug/polymer matrix.33. The transdermal patch of claim 24 , further comprising a chemical permeation enhancer.36. The kit of claim 35 , wherein both Rand Rare hydrogen.39. The kit of claim 34 , wherein —O—Z—COH is —O-cycloalkyl-COH claim 34 , —O—CH-cycloalkyl-COH claim 34 , —O-cycloalkyl-CH—COH claim 34 , or —O—CH-cycloalkyl-CH—COH claim 34 , and for each of the preceding moieties -cycloalkyl- is:1,2-cyclopropyl (cis or trans); or1,3-cyclobutyl (cis or trans) or 1,2-cyclobutyl (cis or trans); or1,3-cyclopentyl (cis or trans) or 1,2-cyclopentyl (cis or trans); or1,4-cyclohexyl (cis or trans), 1,3-cyclohexyl (cis or trans), or 1,2-cyclohexyl (cis or trans).41. The kit of claim 34 , wherein the medical condition is selected from the group consisting of pulmonary hypertension claim 34 , pulmonary fibrosis claim 34 , ischemic diseases claim 34 , peripheral vascular disease claim 34 , peripheral ischemic lesions on the skin claim 34 , critical ...

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04-04-2019 дата публикации

TIGLIEN-3-ONE DERIVATIVES

Номер: US20190099397A1
Принадлежит:

The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment. 124-. (canceled)28. The method according to wherein Rand Rare independently selected from the group consisting of hydrogen claim 25 , hydroxy claim 25 , —OC-Calkyl claim 25 , —OC-Calkenyl claim 25 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl or Rand Rtaken together form a carbonyl group.29. The method according to wherein Rand Rform a double bond or Rand Rare hydrogen or together are —O—.30. The method according to wherein Ris hydrogen or —C-Calkyl.31. The method according to wherein Ris selected from the group consisting of hydroxy claim 25 , —C-Calkyloxy claim 25 , —C-Calkenyloxy claim 25 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl and Ris selected from hydroxy claim 25 , —C-Calkyloxy claim 25 , —C-Calkenyloxy claim 25 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl.32. The method according to wherein Rand Rare independently selected from the group consisting of hydrogen and —C-Calkyl.33. The method according to wherein Rand Rare independently hydrogen claim 25 , hydroxy claim 25 , —OC-Calkyl and —OC-Calkenyl or Rand Rtaken together form a carbonyl group and Ris selected from the group consisting of hydroxy claim 25 , —OC-Calkyl claim 25 , —OC-Calkenyl claim 25 , —OC(O)C-Calkyl and —OC(O)C-Calkenyl.34. The method according to wherein Ris hydroxy claim 25 , —OC-Calkyl claim 25 , —OC-Calkenyl claim 25 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl.35. The method according to wherein Rand Rare each hydroxyl.36. The method according to wherein the compound is selected from:12-tigloyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one;12,13-di-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-tigliaen-3-one;12-(dodeca-2,4,6-trienoyl)-13-(2- ...

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21-04-2016 дата публикации

Epoxy estolide fatty acid alkyl esters useful as biorenewable plasticizers

Номер: US20160108206A1
Принадлежит: University of Minnesota

A composition is described that includes epoxy estolide fatty acid alkyl esters derived from triacylglycerol oil having an unsaturation of greater than 80 Iodine Value (“IV”). The esters are useful as plasticizers for a variety of polymers. Examples of triacylglycerol oils include vegetable oils such as soybean oil, castor oil, canola oil, rapeseed oil, sunflower oil, corn oil, safflower oil, camelina oil, and linseed oil.

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19-04-2018 дата публикации

GRAPHENE COMPOUND AND MANUFACTURING METHOD THEREOF, ELECTROLYTE, AND POWER STORAGE DEVICE

Номер: US20180108944A1
Автор: Yamakaji Masaki
Принадлежит:

To provide a graphene compound having an insulating property and an affinity for lithium ions. To increase the molecular weight of a substituent included in a graphene compound. To provide a graphene compound including a chain group containing an ether bond or an ester bond. To provide a graphene compound including a substituent containing one or more branches. To provide a graphene compound including a substituent including at least one of an ester bond and an amide bond. 6. An electrolyte comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the graphene compound according to ; and'}a lithium salt.7. A power storage device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the graphene compound according to ;'}an exterior body;a positive electrode current collector; anda negative electrode current collector.13. An electrolyte comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'the graphene compound according to ; and'}a lithium salt.14. A power storage device comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'the graphene compound according to ;'}an exterior body;a positive electrode current collector; anda negative electrode current collector.20. A manufacturing method of a graphene compound , comprising the steps of:{'claim-ref': {'@idref': 'CLM-00015', 'claim 15'}, 'manufacturing a first graphene compound by the manufacturing method of a graphene compound according to ;'}forming a second mixture comprising the first graphene compound and a diamine; andfiltering the second mixture to collect a second residue,wherein the second residue comprises a second graphene compound.21. A manufacturing method of a graphene compound , comprising the steps of:{'claim-ref': {'@idref': 'CLM-00015', 'claim 15'}, 'manufacturing a third graphene compound by the manufacturing method of a graphene compound according to ;'}forming a third mixture comprising the third graphene compound and acrylic ester; andfiltering the third mixture to collect ...

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28-04-2016 дата публикации

2, 3-Butanediamide Epoxide Compound and Preparation Method and Use Thereof

Номер: US20160115160A1

Provided are a compound of formula I which can be used as a drug against small RNA virus infections, and optical isomers, pharmaceutically acceptable salts, solvates or hydrates thereof. Also provided are the preparation method of the compound, the method for using the compound for treating bacterial infections and the use of the compound in the preparation of a drug for preventing and/or treating viral diseases caused by small RNA viruses. 2. The compound of formula I according to claim 1 , or optical isomers claim 1 , pharmaceutically acceptable salt claim 1 , solvates or hydrates thereof claim 1 , wherein Y is —N(R)— or hydroxy claim 1 , wherein Ris independently hydrogen or Calkyl claim 1 , preferably hydrogen.3. The compound of formula I according to claim 1 , or optical isomers claim 1 , pharmaceutically acceptable salt claim 1 , solvates or hydrates thereof claim 1 , wherein Ar is aryl or heteroaryl claim 1 , which is optionally and independently mono- or poly-substituted by 1 claim 1 , 2 or 3 R.4. The compound of formula I according to claim 1 , or optical isomers claim 1 , pharmaceutically acceptable salt claim 1 , solvates or hydrates thereof claim 1 , wherein Ris independently hydrogen claim 1 , halogen claim 1 , alkyl claim 1 , alkoxy claim 1 , hydroxy claim 1 , cyano claim 1 , amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , hydroxyalkyl claim 1 , haloalkyl claim 1 , haloalkoxy claim 1 , alkylthio claim 1 , alkoxycarbonyl or nitro;5. The compound of formula I according to claim 1 , or optical isomers claim 1 , pharmaceutically acceptable salt claim 1 , solvates or hydrates thereof claim 1 , wherein Ris aryl or heteroaryl claim 1 , which is optionally and independently mono- or poly-substituted by 1 claim 1 , 2 or 3 substituents claim 1 , and the substituents are independently hydrogen claim 1 , halogen claim 1 , alkyl claim 1 , alkoxy claim 1 , hydroxy claim 1 , amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , haloalkyl claim 1 , ...

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30-04-2015 дата публикации

Method for synthesizing sapropterin dihydrochloride

Номер: US20150119573A1

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

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07-05-2015 дата публикации

CROSS-LINKED GRAPHENE NETWORKS

Номер: US20150122800A1
Принадлежит:

The present invention relates to a method for the production of cross-linked graphene and graphene oxide networks, which are selected from aerogels and xerogels with improved performance and characteristics thereof. The invention is also concerned with graphene and graphene oxide networks, which are selected from aerogels and xerogels produced by such processes and uses thereof. 1. A method of producing an aerogel or xerogel comprising graphene , graphene oxide or a mixture thereof , comprising the steps of: a) dispersing graphene , graphene oxide or a mixture thereof in a solvent compatible therewith; b) cross-linking said graphene , graphene oxide or a mixture thereof via functional groups present on the graphene and/or the graphene oxide , or with a linking molecule comprising at least two functional sites capable of reacting with the surface of said graphene and/or graphene oxide , to form a covalently cross-linked gel network; and c) removing said solvent to produce a cross-linked aerogel or xerogel with a solvent content of less than 10%.2. The method according to claim 1 , wherein said cross-linking is carried out by direct reaction between the surface oxides on the graphene oxide surface.3. The method according to claim 1 , wherein said graphene oxide is oxidised graphene and wherein said cross-linking is carried out with a molecule selected from the group consisting of alkyl diamines claim 1 , aromatic diamines claim 1 , alkyl diols claim 1 , aromatic diols claim 1 , polyols claim 1 , bis-sodium alkoxides claim 1 , dicarboxylic acids claim 1 , di acid chlorides claim 1 , di siloxane halides claim 1 , di siloxane alkoxides and mixtures thereof.4. The method according to claim 2 , wherein said surface oxides are selected from the group consisting of hydroxide claim 2 , carboxylate claim 2 , lactone claim 2 , hydroxyl claim 2 , quinine claim 2 , carboxylic acid groups claim 2 , and mixtures thereof claim 2 , preferably a combination of hydroxide and carboxyl ...

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13-05-2021 дата публикации

FATTY ACID DERIVATIVES AND THEIR USE

Номер: US20210139440A1

This disclosure concerns fatty acid derivatives, pharmaceutical compositions comprising the fatty acid derivatives, and methods of using the fatty acid derivatives, for example, to treat inflammation, chronic itch, chronic pain, an autoimmune disorder, atherosclerosis, a skin disorder, arthritis, a neurodegenerative disorder, or a psychiatric disorder in a subject. In some embodiments, the fatty acid derivative is a compound, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, having a structure according to: 3. The compound of claim 1 , wherein X is from 1-10 carbons in length.4. The compound of claim 1 , wherein X is 6 carbons in length.5. The compound of claim 1 , wherein Z is from 1-10 carbons in length.6. The compound of claim 1 , wherein Z is 4 carbons in length.7. The compound of claim 1 , wherein X and Z together are from 8-14 carbons in length.8. The compound of claim 1 , wherein X and Z together are 10 carbons in length.9. The compound of claim 1 , wherein X and Z are independently alkyl claim 1 , substituted alkenyl claim 1 , or unsubstituted alkenyl.10. The compound of claim 1 , wherein X and Z independently comprise one or more fluoroalkene claim 1 , difluoroalkene claim 1 , and/or bis-allylic deuterium substitutions.11. The compound of claim 1 , having a structure according to any one of formulas (II)-(CII) claim 1 , wherein claim 1 , if present:{'sup': '1', 'Ris hydrogen or lower alkyl;'}{'sup': '2', 'Ris hydrogen or lower alkyl;'}{'sup': '3', 'Ris hydrogen or lower alkyl;'}{'sup': '4', 'Ris lower alkyl, hydroxyl, carboxyl, or amine;'}{'sup': '5', 'Ris hydrogen, lower alkyl, or halide;'}{'sup': '6', 'Ris hydroxyl or substituted thiol;'}{'sup': '7', 'each Ris independently hydrogen or fluoride or not present and the adjacent carbons form alkyne;'}{'sup': '8', 'each Ris independently hydrogen or fluoride; and'}{'sup': '9', 'each Ris independently hydrogen or deuterium.'}12. The compound of claim 11 , wherein each Ris independently ...

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13-05-2021 дата публикации

USES OF FLUORINATED EPOXIDES AND NOVEL MIXTURES THEREOF

Номер: US20210139441A1
Принадлежит: THE CHEMOURS COMPANY FC, LLC

This application relates to compositions comprising one or more partially fluorinated epoxides and/or one or more perfluorinated epoxides which may be useful in applications including refrigerants, air conditioning, heat transfer media, high-temperature heat pumps, organic Rankine cycles, fire extinguishing/fire suppression, propellants, foam blowing, solvents, dielectrics, and/or cleaning fluids. 2. The composition of claim 1 , wherein:{'sup': 1', '4, 'sub': 1-4', '1-4, 'Rand Rare each independently H, Cl, F, a partially fluorinated Calkoxy, or a perfluorinated Calkoxy;'}{'sup': '2', 'sub': 1-10', '1-10, 'Ris H, F, partially fluorinated Calkyl, or perfluorinated Calkyl;'}{'sup': 1', '2', '4, 'wherein at least one of R, R, and Ris not H; and'}{'sup': '3', 'sub': 1-10', '1-10, 'Ris selected from partially fluorinated Calkyl and perfluorinated Calkyl.'}3. The composition of claim 1 , wherein Rand Rare each independently H claim 1 , Cl claim 1 , or F; Ris F claim 1 , CF claim 1 , CFCF claim 1 , CF(CF) claim 1 , CFCFCF claim 1 , CFCFCFCF claim 1 , or CFCFCFCFCF; and Ris CF claim 1 , CFCF claim 1 , CF(CF) claim 1 , CFCFCF claim 1 , CFCFCFCF claim 1 , or CFCFCFCFCF.4. The composition of claim 1 , wherein Rand Rare each independently H claim 1 , Cl claim 1 , F claim 1 , a partially fluorinated Calkoxy claim 1 , or a perfluorinated Calkoxy; and Rand Rare each independently selected from partially fluorinated or perfluorinated Calkylene claim 1 , which together form a monocyclic ring.5. The composition of claim 1 , wherein Rand Rare H; Ris partially fluorinated or perfluorinated Calkylene; and Ris partially fluorinated or perfluorinated Calkylene; wherein said Rand Rare taken together form a 4-6 membered monocyclic ring.6. (canceled)7. The composition of claim 1 , wherein the compound of Formula (I) is selected from:2,3-difluoro-2-(trifluoromethyl)oxirane;2-fluoro-3-(trifluoromethyl)oxirane;2,3-bis(trifluoromethyl)oxirane;2-(trifluoromethyl)-3-(perfluoroethyl)oxirane;2-( ...

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07-05-2015 дата публикации

FUMIGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20150126489A1
Принадлежит: Zafgen, Inc.

The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. 109. A method of treating and/or controlling obesity claims 1 , comprising administering to a patient in need thereof an effective amount of the compound of any one of -.119. A method of inducing weight loss in a patient in need thereof claims 1 , comprising administering to said patient an effective amount of the compound of any one of -.12. The method of or claims 1 , wherein the patient is a human.1312. The method of any one of - claims 11 , wherein the patient has a body mass index greater than or equal to about 25 kg/mbefore the administration.1413. The method of any one of - claims 10 , wherein the compound is administered orally claims 10 , intravenously claims 10 , or subcutaneously.1513. The method of any one of - claims 10 , wherein the compound is administered orally.1615. A pharmaceutical composition comprising a compound of any one of - claims 1 , and a pharmaceutically acceptable carrier.17. The composition of claim 16 , wherein the composition is formulated as a unit dose.18. The method of comprising administering said compound in an amount insufficient to reduce angiogenesis in the patient. This application claims priority to U.S. Provisional Ser. No. 61/644,612 filed May 9, 2012, hereby incorporated by reference in its entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or airplane seats, social difficulties, etc.), these conditions, in particular clinical obesity, affect other aspects of health, i.e., ...

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25-04-2019 дата публикации

Totally bio-based vegetable oil polyol and preparation method and use thereof

Номер: US20190119496A1
Принадлежит:

A method comprises enabling epoxy vegetable oil to react with a compound of a formula III in a second microstructured reactor to obtain the vegetable oil polyol. Compared with the existing technology, the present invention adopts a novel, environment-friendly ring-opening agent, the obtained polyol is novel in structure, high in hydroxyl value, even in distribution and low in viscosity, and can completely replace traditional petrochemical polyol to be applied to the preparation of polyurethane foam materials. 3. The method according to claim 2 , wherein claim 2 , in the step (1) claim 2 , the organic acid is formic acid or acetic acid claim 2 , the catalyst is sulfuric acid or phosphoric acid claim 2 , the stabilizer is ethylenediamine tetraacetic acid claim 2 , the vegetable oil is at least one selected from olive oil claim 2 , peanut oil claim 2 , rapeseed oil claim 2 , cottonseed oil claim 2 , soybean oil claim 2 , palm oil claim 2 , sesame oil claim 2 , sunflower oil claim 2 , linseed oil claim 2 , tung oil claim 2 , safflower oil claim 2 , rice bran oil claim 2 , corn oil and teaseed oil claim 2 , and the mole ratio of double bonds in the vegetable oil to the hydrogen peroxide to the organic acid to the catalyst to the stabilizer is 1:(6-20):(6-20):(0.02-0.4):(0.006-0.2).4. The method according to claim 2 , wherein claim 2 , in the step (1) claim 2 , the first microstructured reactor has a reaction temperature of 60-130° C. claim 2 , a reaction residence time of 5-10 min and a volume of 20-60 mL claim 2 , the vegetable oil is pumped into the micro-channel modular reaction device at a flow rate of 0.5-1.0 mL/min and the mixed solution is pumped into the micro-channel modular reaction device at a flow rate of 3.5-5.0 mL/min.5. The method according to claim 2 , wherein claim 2 , in the step (2) claim 2 , the mole ratio of epoxy groups in the epoxy vegetable oil to the compound of the formula III is 1:(1.5-4.5) claim 2 , the second microstructured reactor has a ...

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10-05-2018 дата публикации

EPOXYCYCLOHEXANE DICARBOXYLIC ACID DIESTER, PLASTICIZER, STABILIZER AND RESIN COMPOSITION

Номер: US20180127390A1
Принадлежит:

The purpose of the present invention is to provide a novel compound which is useful as a plasticizer that has improved heat resistance and cold resistance, while having good inherent plasticization performance as a plasticizer, or which is useful as a stabilizer for chlorine-containing resins. The inventors have found that a novel epoxycyclohexane dicarboxylic acid diester having a specific structure, which has an epoxy group in the molecular structure and has improved cold resistance and heat resistance, enables the achievement of the above-described purpose, and have been able to achieve a novel compound that is useful as a plasticizer and as a stabilizer. 2. The epoxycyclohexane dicarboxylic acid diester according to claim 1 , wherein (i) the alkyl group is mainly composed of an alkyl group having 9 to 11 carbon atoms claim 1 , in which the ratio (molar ratio) of alkyl group having 9 carbon atoms/alkyl group having 10 carbon atoms/alkyl group having 11 carbon atoms is in the range of 10 to 25/35 to 50/30 to 45 claim 1 , or (ii) the alkyl group contains an alkyl group having 9 carbon atoms in an amount of 90% or more (molar ratio) with respect to the total amount of the alkyl groups constituting the dicarboxylic acid diester.3. The epoxycyclohexane dicarboxylic acid diester according to claim 1 , wherein the ratio (molar ratio) of the linear-chain alkyl group in the alkyl groups is 55 to 95%.4. The epoxycyclohexane dicarboxylic acid diester according to claim 1 , wherein the isomer ratio (cis-form/trans form claim 1 , molar ratio) of the oxirane ring and the alkyloxycarbonyl group via the cyclohexane ring measured by proton nuclear magnetic resonance spectroscopy is 5/95 to 35/65.5. A plasticizer for vinyl chloride-based resins claim 1 , comprising the epoxycyclohexane dicarboxylic acid diester according to .6. A vinyl chloride-based resin composition comprising a vinyl chloride-based resin and the plasticizer for vinyl chloride-based resins according to .7. The ...

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31-07-2014 дата публикации

PREPARATION OF NITRILE COMPOUNDS

Номер: US20140213804A1
Принадлежит: DSM IP ASSETS B.V.

The invention relates to novel nitrile compounds according to formula I and II: (I) Formula I wherein: X=—CHor —C≡N, (II) Formula II wherein: X=—CHor —C≡N, each Y is independently chosen from —OH or RC(O)O—, each R is independently chosen from a C1−21 alkyl group. The invention also relates to processes for the preparation of nitrile compounds according to formula I and II and to uses of the nitrile compounds. 3. Nitrile compound according to according to claim 1 , wherein X is —C≡N.4. Nitrile compound according to claim 2 , wherein each Y is independently chosen from —OH and RC(O)O—.5. Nitrile compound according to claim 2 , wherein X is —C≡N.6. Nitrile compound according to claim 2 , wherein X is —CH claim 2 , and either both Y are RC(O)O— or one Y is —OH and one Y is RCO(O)—.7. Nitrile compound according to claim 5 , where one of Y is OH and the other Y is RC(O)O—.8. Nitrile compound according to claim 1 , wherein each R is independently chosen from a C1-C5 alkyl group.9. Nitrile compound according to claim 8 , wherein R is methyl.10. Racemic mixture comprising both enantiomers of a nitrile compound according to .11. Process for the preparation of a nitrile compound according to formula I claim 1 , which comprises at least the step of contacting octadec-9-enenitrile or octadec-9-enedinitrile with hydrogen peroxide under suitable conditions to oxidize the double bond without leading to oxidative carbon-carbon double bond cleavage.12. Use of a compound according to formula I as an intermediate for surfactants or lubricants or as surfactant or lubricant.13. Process for the preparation of a nitrile compound according to formula II claim 1 , that comprises at least the following steps:a. contacting octadec-9-enenitrile or octadec-9-enedinitrile with hydrogen peroxide under suitable conditions to oxidize the double bond without leading to oxidative carbon-carbon double bond cleavage to generate the corresponding C18- nitrile derivatives according to formula I,b. ...

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01-09-2022 дата публикации

FATTY ACID DERIVATIVES AND THEIR USE

Номер: US20220274940A1

This disclosure concerns fatty acid derivatives, pharmaceutical compositions comprising the fatty acid derivatives, and methods of using the fatty acid derivatives, for example, to treat inflammation, chronic itch, chronic pain, an autoimmune disorder, atherosclerosis, a skin disorder, arthritis, a neurodegenerative disorder, or a psychiatric disorder in a subject. In some embodiments, the fatty acid derivative is a compound, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, having a structure according to: 3. The compound of claim 1 , wherein:(i) X is from 1-10 carbons in length; or(ii) Z is from 1-10 carbons in length; or(iii) both (i) and (ii).4. The compound of claim 1 , wherein X and Z together are from 8-14 carbons in length.5. The compound of claim 1 , wherein X and Z are independently alkyl claim 1 , substituted alkenyl claim 1 , or unsubstituted alkenyl.6. The compound of claim 5 , wherein X and Z independently are alkyl claim 5 , alkenyl claim 5 , or halogenated alkenyl.7. The compound of claim 1 , wherein Ris hydrogen.8. The compound of claim 1 , wherein R claim 1 , R claim 1 , and Rare methyl.9. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. The pharmaceutical composition of claim 9 , formulated for topical claim 9 , parenteral claim 9 , or oral administration.11. A method of treating a disease or condition in a subject claim 9 , comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'administering a therapeutically effective amount of the pharmaceutical composition of to a subject having, or suspected of having, the disease or condition,'}wherein the disease or condition is inflammation, chronic itch, chronic pain, an autoimmune disorder, atherosclerosis, a skin disorder, arthritis, a neurodegenerative disorder, or a psychiatric disorder.13. The compound of claim 12 , wherein each Rindependently is hydrogen or fluoride.14. A pharmaceutical composition comprising a ...

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02-05-2019 дата публикации

METHOD FOR PRODUCING N-RETINOYLCYSTEIC ACID ALKYL ESTER

Номер: US20190127322A1
Принадлежит:

A method for producing derivatives of N-retinoylaminoalkane sulfonic acid, the method comprising providing retinoic acid, chloroformate, aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof, cysteinesulfinic acid and alkyl ester thereof, homocysteic acid and alkyl ester thereof, homocysteinesulfinic acid and alkyl esters thereof, taurine and derivatives thereof, and an organic solvent, and a base, mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising a liquid phase, wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase. 1. A method for producing derivatives of N-retinoylaminoalkane sulfonic acid , the method comprising providing retinoic acid , chloroformate , aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof , cysteinesulfinic acid and alkyl ester thereof , homocysteic acid and alkyl ester thereof , homocysteinesulfinic acid and alkyl esters thereof , taurine and derivatives thereof , and an organic solvent , and a base , mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising at least a liquid phase , wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase.2. The method according to claim 1 , wherein the derivatives of N-retinoylaminoalkane sulfonic acid are selected from N-(13-cis-retinoyl)-cysteic acid alkyl ester and N-(all-trans-retinoyl)-cysteic acid alkyl ester claim 1 , the retinoic acid is selected from 13-cis-retinoic acid or all-trans-retinoic acid claim 1 , and the aminoalkane sulfonic acid selected from cysteic acid alkyl ester.3. The method according to claim 1 , wherein the derivatives of N-retinoylaminoalkane sulfonic acid are selected from the sodium salts of N-(13-cis-retinoyl)- ...

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07-08-2014 дата публикации

Primary pvc plasticizers derived from vegetable oils, process for obtaining primary pvc plasticizers derived from vegetable oils and plasticized pvc composition

Номер: US20140221538A1
Принадлежит: Nexoleum Bioderivados Ltda

The present descriptive report refers to a patent of invention of PVC plasticizers composed of epoxidized bioesters of vegetable oil fatty acids obtained by partial transesterification with an alcohol, and glycerin and further acetylation and epoxidation, and PVC compounds plasticized with bioesters resulting from partial transesterification, acetylation and epoxidation, belonging to the technical field of polymer additives that were developed to improve the properties of PVC polymers, in addition to providing a lower cost for renewable compounds, such as those obtained with the use of vegetable oils. The epoxidized bioesters of the present invention are composed by mixtures of epoxidized ethyl esters and acetylated and epoxidized mono, di and triglyceril esters, presenting oxirane index equal to or less than 8. These primary plasticizers provide improvements to the properties of the compounded PVC not foreseen in the state of the art, such as better physical properties at low temperatures, greater flexibility of the final compound, higher mixing efficiency of the resin, improved resistance to aliphatic solvents extraction and improved resistance to UV degradation.

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10-06-2021 дата публикации

1,3-DIPOLAR COMPOUND COMPRISING AN EPOXIDE GROUP

Номер: US20210171670A1

A 1,3-dipolar compound including an epoxide group is provided. The epoxide group is a 3-membered ether ring in which a first member is a carbon atom having an attachment to the dipole of the 1,3-dipolar compound and a second member is a tertiary or quaternary carbon. The use of the 1,3-dipolar compound in the modification of a diene polymer makes it possible to improve the rupture properties of a rubber composition comprising the modified polymer, without the expense of its hysteresis properties, while at the same time improving its implementation. 1. A 1 ,3-dipolar compound including an epoxide group , the epoxide group being a 3-membered ether ring in which a first member is a carbon atom having an attachment to the dipole of the 1 ,3-dipolar compound and a second member is a tertiary or quaternary carbon , and the compound being a nitrile monooxide.3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. The 1 claim 2 ,3-dipolar compound according to claim 2 , in which the substituent group is an alkyl or an aryl.8. (canceled)9. (canceled)10. The 1 claim 1 ,3-dipolar compound according to claim 1 , which comprises a benzene nucleus claim 1 , which benzene nucleus is substituted with the dipole of the 1 claim 1 ,3-dipolar compound.11. The 1 claim 10 ,3-dipolar compound according to claim 10 , in which the benzene nucleus is substituted ortho to the dipole.12. (canceled)13. (canceled)15. The 1 claim 14 ,3-dipolar compound according to claim 14 , in which R1 claim 14 , R3 and R5 each represent a hydrocarbon-based group.16. The 1 claim 14 ,3-dipolar compound according to claim 14 , in which the fifth symbol represents a carbon-based chain interrupted with one or more heteroatoms.17. The 1 claim 14 ,3-dipolar compound according to claim 14 , in which the fifth symbol comprises a —CHO— group claim 14 , the methylene group being attached to the epoxide group.19. A process for modifying a diene polymer via a grafting reaction claim 1 , which comprises the reaction of a ...

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25-05-2017 дата публикации

METHODS AND COMPOSITIONS FOR WOUND HEALING

Номер: US20170144981A1
Принадлежит:

The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described. 127-. (canceled)28. A compound selected from the group consisting of:12-hexanoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 5);12-acetyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 6);12-propanoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 7);12-butanoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 8);12-[(2E,4E)-(6,6-dimethoxyhexa-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 9);12-[(2E,4E)-6-oxohexa-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 10);12-[(2E,4E)-6,7-dihydroxydodeca-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 11);12-[(2E)-4,5-dihydroxy-deca-2-enoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 12);12-tigloyl-13-(2-methylpropanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 13);12-[(2E)-3-methylthioprop-2-enoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 14);12-(2-methylprop-2-enoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 15);12-[(2E,4E)-hexa-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 16);12-[(2E,4E)-8-oxododeca-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound17 ...

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28-08-2014 дата публикации

PROCESS FOR THE PREPARATION OF OSELTAMIVIR AND METHYL 3-EPI-SHIKIMATE

Номер: US20140243537A1

The present invention discloses high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol. The process features incorporation of chirality using sharpless asymmetric epoxidation (AE) and diastereoselective Barbier allylation and construction of cyclohexene carboxylic acid ester core through a ring closing metathesis (RCM) reaction. Further also disclosed herein is synthesis of (−)-methyl 3-epi-shikimate. 2. The process as claimed in claim wherein the solvent is a polar or non-polar solvent; and protic or aprotic solvent is selected from the group consisting of toluene , acetone , ethyl acetate , methanol THF , DCM , and DMSO.3. The process as claimed in claim 1 , wherein the silylating agent used in step (i) is selected from the group consisting of trimethylsilyl (TMS) claim 1 , tert-butyldiphenylsilyl (TBDPS) claim 1 , tert-butyldimethylsilyl (TBS/TBDMS) and triisopropylsilyl (TIPS) claim 1 , [2-(trimethylsilyl)ethoxy]methyl (SEM) claim 1 , and tert-butyl dimethylsilyl chloride (TBSCl).4. The process as claimed in claim 1 , wherein the base used in step (v) is selected from the group comprising consisting of KCOand EtN.5. The process as claimed in claim 1 , wherein protecting agent used in step (iv) is MOMCl (methyl chloromethyl ether).6. (canceled)7. (canceled) The present invention relates to a high yielding enantioselective process for synthesis of Oseltamivir from readily available starting material, cis-1,4-butene diol. The process features incorporation of chirality using sharpless asymmetric epoxidation (AE) and diastereoselective Barbier allylation and construction of cyclohexene carboxylic acid ester core through a ring closing metathesis (RCM) reaction. The present invention also relate to synthesis of (−)-methyl 3-epi-shikimate. More particularly, the present invention relates to compounds of general formula 1 and 2.Influenza, commonly referred to as flu, is an infectious disease ...

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16-06-2016 дата публикации

Manumycin-type metabolite called Colabomycin E which inhibits caspase 1 and creation of interleukins, strain produces the Colabomycin E and a method of a production of the Colabomycin E

Номер: US20160168106A1

A manumycin-type metabolite called Colabomycin E which inhibits caspase 1 and creation of interleukins, strain produces the Colabomycin E and a method of a production of the Colabomycin E. Colabomycin E is a new member of the manumycin-type metabolites produced by the strain Streptomyces aureus SOK1/5-04 deposited in The Czech collection of microorganisms under number CCM8556. The structure of 5 is similar to that of the already known metabolite colabomycin A (3) isolated from Streptomyces griseoflavus . However, the upper polyene chain of 5 is two carbons longer. Therefore, it was named Colabomycin E. Biological activity assays indicated that colabomycin E significantly inhibited IL-1β release from THP-1 cells and might thus potentially act as an anti-inflammatory agent.

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30-05-2019 дата публикации

METHODS AND COMPOSITIONS FOR WOUND HEALING

Номер: US20190161462A1
Принадлежит:

The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds Sand compositions for use in wound healing are also described. 129-. (canceled)30. A method of promoting wound healing in a subject comprising administering to a wound an epoxy-tigliane compound selected from the group consisting of:12-hexanoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 5);12-acetyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 6);12-propanoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 7);12-butanoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 8);12-[(2E,4E)-(6,6-dimethoxyhexa-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 9);12-[(2E,4E)-6-oxohexa-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 10);12-[(2E,4E)-6,7-dihydroxydodeca-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 11);12-[(2E)-4,5-dihydroxy-deca-2-enoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 12);12-tigloyl-13-(2-methylpropanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 13);12-[(2E)-3-methylthioprop-2-enoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 14);12-(2-methylprop-2-enoyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 15);12-[(2E,4E)-hexa-2,4-dienoyl]-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one (Compound 16);12-[(2E,4E)-8- ...

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01-07-2021 дата публикации

TIGLIEN-3-ONE DERIVATIVES

Номер: US20210196668A1
Принадлежит:

The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment 120-. (canceled)24. A pharmaceutical composition according to wherein Rand Rare independently selected from the group consisting of hydrogen claim 21 , hydroxy claim 21 , —OC-Calkyl claim 21 , —OC-Calkenyl claim 21 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl or Rand Rtaken together form a carbonyl group.25. A pharmaceutical composition according to wherein Rand Rform a double bond or Rand Rare hydrogen or together are —O—.26. A pharmaceutical composition according to wherein Ris hydrogen or —C-Calkyl.27. A pharmaceutical composition according to wherein Ris selected from the group consisting of hydroxy claim 21 , —C-Calkyloxy claim 21 , —C-Calkenyloxy claim 21 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl and Ris selected from hydroxy claim 21 , —C-Calkyloxy claim 21 , —C-Calkenyloxy claim 21 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl.28. A pharmaceutical composition according to wherein Rand Rare independently selected from the group consisting of hydrogen and —C-Calkyl.29. A pharmaceutical composition according to wherein Rand Rare independently hydrogen claim 21 , hydroxy claim 21 , —OC-Calkyl and —OC-Calkenyl or Rand Rtaken together form a carbonyl group and Ris selected from the group consisting of hydroxy claim 21 , —OC-Calkyl claim 21 , —OC-Calkenyl claim 21 , —OC(O)C-Calkyl and —OC(O)C-Calkenyl.30. A pharmaceutical composition according to wherein Ris hydroxy claim 21 , —OC-Calkyl claim 21 , —OC-Calkenyl claim 21 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl.31. A pharmaceutical composition according to wherein Rand Rare each hydroxyl.32. A pharmaceutical composition according to wherein the compound is selected from the group consisting of:(12-tigloyl-13-(2- ...

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02-07-2015 дата публикации

FATTY ACID INHIBITORS

Номер: US20150183754A1
Автор: Branchaud Bruce
Принадлежит:

Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein. 2. The compound of claim 1 , wherein the unsaturated or polyunsaturated fatty acid comprises an aliphatic chain having 5 to 23 carbons.3. The compound of claim 1 , wherein the unsaturated or polyunsaturated fatty acid is selected from a glycolipid claim 1 , a glycerolipid claim 1 , a phospholipid and a cholesterol ester.4. The compound of claim 1 , wherein Ris nitro (—NO).5. The compound of claim 1 , wherein the one or more electron withdrawing group is positioned on an alpha carbon of a carbon-carbon double bond of the non-naturally occurring claim 1 , unsaturated or polyunsaturated fatty acid.6. The compound of claim 1 , wherein a carbon-carbon double bond associated with Ris in cis configuration.7. The compound of claim 1 , wherein a carbon-carbon double bond associated with Ris in trans configuration.8. The compound of claim 1 , wherein the unsaturated or polysaturated fatty acid comprises two or more conjugated carbon-carbon double bonds.9. The compound of claim 8 , wherein Ris at any carbon in the two or more conjugated carbon-carbon double bonds.10. The compound of claim 1 , wherein at least Ris positioned at C-9 claim 1 , C-10 claim 1 , C-12 claim 1 , C-13 or a combination thereof.11. The compound of claim 1 , further comprising one or more non-carbon-carbon linkage selected from an ester linkage claim 1 , an ether linkage claim 1 , and a vinyl ether linkage.12. The compound of claim 1 , further comprising one or more functional group other than an electron withdrawing group positioned at any carbon of the unsaturated or polysaturated fatty acid.13. The compound of claim 1 , further comprising a pharmaceutically acceptable carrier claim 1 , excipient claim 1 , or combination thereof.14. The compound of claim 13 , further comprising one ...

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28-05-2020 дата публикации

METHODS FOR MAKING CYCLOHEXENE OXIDE-CONTAINING ESTERS

Номер: US20200165218A1
Принадлежит:

A method of making an ester comprised of at least one cyclohexene oxide moiety is provided, involving the steps of a) esterifying an alcohol with a carboxylic acid-substituted cyclohexene to obtain an intermediate comprised of at least one carboxylate-substituted cyclohexene moiety; and b) epoxidizing the intermediate obtained in step a) with an epoxidizing agent to obtain the ester comprised of at least one cyclohexene oxide moiety. The esters have utility as acid scavengers, plasticizers and reactive resins. 1. A method of making an ester comprised of at least one cyclohexene oxide moiety , comprising:a) esterifying an alcohol with a carboxylic acid-substituted cyclohexene to obtain an intermediate comprised of at least one carboxylate-substituted cyclohexene moiety; andb) epoxidizing the intermediate obtained in step a) with an epoxidizing agent to obtain the ester comprised of at least one cyclohexene oxide moiety.2. The method of claim 1 , wherein the alcohol is a mono-alcohol.3. The method of claim 1 , wherein the alcohol is a C1 to C24 linear or branched aliphatic mono-alcohol or cycloaliphatic mono-alcohol.4. The method of claim 1 , wherein the alcohol is a polyol.5. The method of claim 1 , wherein the alcohol is a polyol selected from the group consisting of ethylene glycol; 1 claim 1 ,2-propylene glycol; 1 claim 1 ,3-propylene glycol; 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- and 1 claim 1 ,4-butanediol; 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- claim 1 , 1 claim 1 ,4- and 1 claim 1 ,5-pentanediol; 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- claim 1 , 1 claim 1 ,4- claim 1 , 1 claim 1 ,5- claim 1 , and 1 claim 1 ,6-hexanediol; 2-methyl-1 claim 1 ,3-propanediol; neopentyl glycol; glycerol; sugars; sugar alcohols claim 1 , pentaerythritol; dipentaerythritol; tripentaerythritol; trimethylolpropane; trimethylolethane; 3-methyl-1 claim 1 ,5-pentanediol; 1 claim 1 ,4-cyclohexanedimethanol; 1 claim 1 ,3-cyclohexanedimethanol; oligomers of ethylene glycol claim 1 , propylene ...

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09-07-2015 дата публикации

PROCESS FOR THE PREPARATION OF KARANJA OIL-BASED EPOXY AND ACYLOXY COMPOUNDS AS LUBRICANT BASESTOCKS

Номер: US20150191441A1
Принадлежит:

The present invention relates to preparation of epoxy karanja oil, epoxy karanja fatty acid methyl esters and their acylated derivatives. Accordingly karanja oil and karanja fatty acid methyl esters were epoxidised using performic acid method. Karanja oil and its fatty acid methyl esters were also hydroxylated to prepare their acyloxy derivatives (C, C& C). Both the epoxy and acyloxy derivatives of karanja oil and its methyl esters were characterized by H NMR and IR studies. The products were evaluated for acid value (A.V.), hydroxyl value (H. V.), iodine value (I. V.), viscosity, viscosity index (V.I.), pour point, flash point and copper strip corrosion and lubricant properties like oxidation stability, air release value, evaporation loss, rust prevention characteristics, hydrolytic stability, foam stability and load carrying capacity and found to be potential base stocks for hydraulic, metal working fluids and other industrial fluids. 2. A process as claimed in claim 1 , wherein epoxy compounds are made in the steps and (b) at 25-80° C. for 0.5-10 hr and further increasing the reaction temperature 80-85° C. for 5-15 hr leads to formation of hydroxylated karanja oil or hydroxyla karanja fatty acid methyl esters.3. A process as claimed in claim 2 , wherein no epoxy components were present either hydroxylated karanja fatty acid methyl esters or in hydroxylated karanja oil4. A process as claimed in claim 1 , wherein concentrated sulphuric acid used in step and (b) is 2% wt of formic acid and hydrogen peroxide.5. A process as claimed in claim 1 , wherein alcohol used in step (b) is selected from group consisting of methanol claim 1 , 2-propanol claim 1 , 1-butanol claim 1 , 2-methyl-1-propanol and ethyl 1-hexanol.6. A process as claimed in claim 1 , wherein acid anhydrides used in step (c) is selec from the group consisting of acetic claim 1 , propionic claim 1 , butyric and hexanoic anhydrides.7. A process as claimed in claim 1 , wherein water azeotrope forming ...

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11-06-2020 дата публикации

TIGLIEN-3-ONE DERIVATIVES

Номер: US20200179325A1
Принадлежит:

The present invention relates to tiglien-3-one compounds and their use in methods of treating or preventing protozoal infections, bacterial infections, parasitic infections and cell proliferative disorders. The tiglien-3-one compounds are also used in methods of controlling pests in humans, animals, plants and the environment 4. The method according to wherein Rand Rare independently selected from the group consisting of hydrogen claim 1 , hydroxy claim 1 , —OC-Calkyl claim 1 , —OC-Calkenyl claim 1 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl or Rand Rtaken together form a carbonyl group.5. The method according to wherein Rand Rform a double bond or Rand Rare hydrogen or together are —O—.6. The method according to wherein le is hydrogen or —C-Calkyl.7. The method according to wherein R″ is selected from the group consisting of hydroxy claim 1 , —C-Calkyloxy claim 1 , —C-Calkenyloxy claim 1 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl and Ris selected from hydroxy claim 1 , —C-Calkyloxy claim 1 , —C-Calkenyloxy claim 1 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl.8. The method according to wherein Rand Rare independently selected from the group consisting of hydrogen and -C-Calkyl.9. The method according to wherein Rand Rare independently hydrogen claim 1 , hydroxy claim 1 , —OC-Calkyl and —OC-Calkenyl or Rand Rtaken together form a carbonyl group and R″ is selected from the group consisting of hydroxy claim 1 , —OC-Calkyl claim 1 , —OC-Calkenyl claim 1 , —OC(O)C-Calkyl and —OC(O)C-Calkenyl.10. The method according to wherein Ris hydroxy claim 1 , —OC-Calkyl claim 1 , —OC-Calkenyl claim 1 , —OC(O)C-Calkyl or —OC(O)C-Calkenyl.11. The method according to wherein Rand Rare each hydroxyl.12. The method according to wherein the compound is selected from:12-tigloyl-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-1-tigliaen-3-one;12,13-di-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20-hexahydroxy-tigliaen-3-one;12-(dodeca-2,4,6-trienoyl)-13-(2-methylbutanoyl)-6,7-epoxy-4,5,9,12,13,20- ...

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30-07-2015 дата публикации

ALICYCLIC EPOXY COMPOUND AND METHOD FOR PRODUCING SAME

Номер: US20150210660A1
Принадлежит: Daicel Corporation

Provided is a novel epoxide that is highly soluble in organic solvents, is lowly volatile, contains a highly reactive epoxy group, and still resists polymerization by itself. 2. The cycloaliphatic epoxide according to claim 1 ,{'sup': 'a', 'sub': 8', '17, 'wherein Ris C-Cbranched chain alkyl.'}3. The cycloaliphatic epoxide according to claim 1 ,{'sup': 1', '11, 'wherein Rto Rare each hydrogen.'}6. The cycloaliphatic epoxide according to claim 2 ,{'sup': 1', '11, 'wherein Rto Rare each hydrogen.'} The present invention relates to cycloaliphatic epoxides (alicyclic epoxy compounds) and methods for producing the same. More specifically, the present invention relates to a cycloaliphatic epoxide that is highly soluble in organic solvents, is lowly volatile, contains a highly reactive epoxy group, and still resists polymerization by itself.Epoxides contain one or more epoxy groups per molecule (in one molecule) and serve a variety of uses. The epoxides are mainly used as principal components to form epoxy resins that are used typically in a variety of structural materials. Their uses, however, have gone beyond this and become wider and wider recently. For example, some epoxides are used as additives to impart a specific function or functions to materials. The epoxides are used as additives typically as a reactive diluent to allow an epoxy resin to have a lower viscosity (see, for example, Patent Literature (PTL) 1); and as a stabilizer (acid scavenger) to scavenge an acid formed in a poly(vinylidene chloride) resin (see, for example, PTL 2).The epoxides to be used as the additives require low volatility. The low volatility is such a property as to resist volatilization even upon heating typically in curing of the epoxy resins or melt molding of the resins. To exhibit functions as a reactive diluent or a stabilizer (acid scavenger) sufficiently, the epoxides further require high reactivity with an epoxy group or an acid and resistance to polymerization by themselves. ...

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28-07-2016 дата публикации

NEMATIC LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY ELEMENT INCLUDING SAME

Номер: US20160215215A1
Принадлежит: DIC CORPORATION

The present invention relates to a nematic liquid crystal composition useful as a liquid crystal display material, the liquid crystal composition having negative dielectric anisotropy (Δ∈), and to a liquid crystal device element including the liquid crystal composition. The liquid crystal composition of the present invention has sufficiently low viscosity (η), sufficiently low rotational viscosity (γ1), a large elastic constant (K), and a negative dielectric anisotropy (Δ∈) whose absolute value is large, without reducing the refractive index anisotropy (Δn) or the nematic-isotropic liquid phase transition temperature (T). Provided is, for example, a VA-mode liquid crystal display element including the liquid crystal composition, the liquid crystal display element having no or minimal display defects and having excellent display quality and a fast response. The liquid crystal display element including the liquid crystal composition of the present invention is useful for an active matrix-addressed liquid crystal display element and used for, for example, a VA- or PSVA-mode liquid crystal display element. 2. The liquid crystal composition according to claim 1 , wherein min general formula (I) represents 1.3. The liquid crystal composition according to claim 2 , wherein ring B1 in general formula (I) represents an unsubstituted 1 claim 2 ,4-phenylene group or a 1 claim 2 ,4-phenylene group substituted with an alkyl group having 1 to 12 carbon atoms claim 2 , a halogenated alkyl group having 1 to 12 carbon atoms claim 2 , an alkoxy group having 1 to 12 carbon atoms claim 2 , a halogenated alkoxy group having 1 to 12 carbon atoms claim 2 , a halogen claim 2 , a cyano group claim 2 , or a nitro group.9. The liquid crystal composition according to claim 1 , wherein the liquid crystal composition has a dielectric anisotropy (Δ∈) of −2.0 to −8.0 at 25° C. claim 1 , a refractive index anisotropy (Δn) of 0.08 to 0.14 at 20° C. claim 1 , a viscosity (η) of 5 to 30 mPa·s at 20° C ...

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18-08-2016 дата публикации

SYNTHESIS PROCESS FOR DIACETYL EPOXY GLYCERYL OLEATE

Номер: US20160237050A1
Принадлежит: GUANGZHOU HAIRMA CHEMICAL (GZ) LTD.

The present invention relates to a process for the synthesis of diacetyl epoxy glyceryl oleate, comprising the steps of: a). esterification of glycerol and oleic acid at 115-190° C. for 1.5-4.5 hours in the presence of an esterification catalyst to obtain glyceryl monooleate; b). acetylation of glyceryl monooleate and an acetylating reagent at 90-160° C. for 2-10 hours in the presence of an acetylation catalyst to obtain diacetyl glyceryl oleate; c). epoxidation of diacetyl glyceryl oleate and hydrogen peroxide at 60-80° C. for 2-4 hours in the presence of an epoxidation catalyst and a weak acid to obtain diacetyl epoxy glyceryl oleate. The prepared diacetyl epoxy glyceryl oleate can be used as plasticizer in plastics, with the advantages of improved stability, good flowability, and high compatibility with plastics. 2. The process according to claim 1 , characterized in that in step a) claim 1 , the weight ratio of glycerol to oleic acid is 1:3.06-3.07.3. The process according to claim 1 , characterized in that in step a) claim 1 , the esterification catalyst is concentrated sulfuric acid claim 1 , concentrated phosphoric acid claim 1 , potassium bisulfate claim 1 , p-toluenesulfonic acid or [emin]BF4 ion liquid claim 1 , and the amount of the esterification catalyst is 0.01-0.04% by weight of the esterification starting material.4. The process according to claim 1 , characterized in that in step b) claim 1 , the acetylating reagent is any one of acetyl chloride claim 1 , glacial acetic acid claim 1 , and acetic anhydride claim 1 , and the amount of said acetylation reagent is 40-50% by weight of the amount of glyceryl monooleate.5. The process according to claim 1 , characterized in that in step b) claim 1 , the acetylation catalyst is at least one of concentrated sulfuric acid claim 1 , concentrated phosphoric acid and NaHSO.HO claim 1 , and the amount of said acetylation catalyst is 0.3-0.6% by weight of the amount of glyceryl monooleate.6. The process according ...

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10-09-2015 дата публикации

METHODS FOR MAKING EPOXIDIZED FATTY ACID ALKYL ESTERS

Номер: US20150252014A1
Принадлежит:

Methods for making epoxidized fatty acid alkyl esters. Such epoxidized fatty acid alkyl esters can be prepared by epoxidizing a natural oil with an acid and a peroxide. Residual acid in the epoxidized natural oil is not neutralized, such as with a base, prior to esterification to produce the epoxidized fatty acid alkyl esters. Epoxidized fatty acid alkyl esters can be employed in plasticizers, either alone or in combination with other plasticizers, such as epoxidized natural oils. Such plasticizers in turn may be used in the formation of polymeric compositions. 1. A process for producing epoxidized fatty acid alkyl esters , said process comprising:(a) epoxidizing a natural oil by contacting said natural oil with an acid and a peroxide to thereby produce an epoxidized reaction mixture comprising epoxidized natural oil, residual acid, residual peroxide, and water;(b) removing a portion of said residual acid, at least a portion of said residual peroxide, and at least a portion of said water from said epoxidized reaction mixture to thereby produce an intermediate reaction mixture; and(c) esterifying at least a portion of said epoxidized natural oil in said intermediate reaction mixture, thereby forming said epoxidized fatty acid alkyl esters,wherein said residual acid is not neutralized prior to said esterifying of step (c).2. A process for producing epoxidized fatty acid alkyl esters , said process consisting essentially of:(a) epoxidizing a natural oil by contacting said natural oil with an acid and a peroxide to thereby produce an epoxidized reaction mixture comprising epoxidized natural oil, residual acid, residual peroxide, and water;(b) removing a portion of said residual acid, at least a portion of said residual peroxide, and at least a portion of said water from said epoxidized reaction mixture to thereby produce an intermediate reaction mixture; and(c) esterifying at least a portion of said epoxidized natural oil in said intermediate reaction mixture, thereby ...

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31-08-2017 дата публикации

PLASTICIZER COMPOSITIONS AND METHODS FOR MAKING PLASTICIZER COMPOSITIONS

Номер: US20170247528A1
Принадлежит:

The present disclosure is directed to a plasticizer composition, polymeric compositions containing the plasticizer composition, and coated conductors comprising the polymeric composition. The plasticizer composition comprises an epoxidized fatty acid alkyl ester having an APHA color value of less than 100, a triepoxide content of at least 6.5 weight percent, and an oxirane oxygen content of at least 5 grams oxirane per 100 grams of epoxidized fatty acid alkyl ester. 1. A plasticizer composition , comprising:an epoxidized fatty acid alkyl ester,wherein said epoxidized fatty acid alkyl ester has an APHA color value of less than 100,wherein said epoxidized fatty acid alkyl ester has a triepoxide content of at least 6.5 weight percent based on the entire weight of said epoxidized fatty acid alkyl ester,wherein said epoxidized fatty acid alkyl ester has an oxirane oxygen content of at least 5 grams oxirane per 100 grams of epoxidized fatty acid alkyl ester.2. The plasticizer composition of claim 1 , wherein said epoxidized fatty acid alkyl ester has a fatty acid dimer content of greater than 0.1 weight percent based on the entire weight of said epoxidized fatty acid alkyl ester claim 1 , wherein said epoxidized fatty acid alkyl ester has an iodine value of 9 or less grams iodine per 100 grams of epoxidized fatty acid alkyl ester.3. The plasticizer composition of claim 1 , wherein said epoxidized fatty acid alkyl ester has a palmitate content of less than 12 weight percent based on the entire weight of said epoxidized fatty acid alkyl ester; wherein said epoxidized fatty acid alkyl ester has a stearate content of less than 5 weight percent based on the entire weight of said epoxidized fatty acid alkyl ester.4. The plasticizer composition of claim 1 , further comprising an epoxidized natural oil.5. The plasticizer composition of claim 1 , wherein said epoxidized fatty acid alkyl ester has a color value of less than 40 APHA; wherein said epoxidized fatty acid alkyl ester ...

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07-09-2017 дата публикации

AMIDE-LINKED PERFLUOROPOLYETHER THIOL COMPOUNDS AND PROCESSES FOR THEIR PREPARATION AND USE

Номер: US20170253570A1
Принадлежит:

A perfluoropolyether thiol compound comprises a perfluoropolyether segment, at least one mercapto group (—SH), and at least one intervening divalent carbonylimino moiety (—C(═O)—NR—, wherein R is hydrogen or alkyl). The compound can be produced, for example, by a ring-opening reaction of thiolactones with perfluoropolyether-substituted, primary or secondary amines. The compound can be used, for example, as a polymerization chain transfer agent, as an intermediate for the preparation of functional group-containing fluorochemical derivatives such as disulfides, and as a fluorinated surface treatment. 1. A process for preparing a perfluoropolyether thiol compound comprises (a) providing at least one thiolactone compound; (b) providing at least one perfluoropolyether-substituted , primary or secondary amine compound; and (c) combining the thiolactone compound and the perfluoropolyether-substituted , primary or secondary amine compound.2. The process of claim 1 , wherein said thiolactone compound is selected from thiolactone compounds having from 5 to 8 ring members claim 1 , and mixtures thereof.3. The process of claim 1 , wherein said thiolactone compound is gamma-butyrothiolactone.4. The process of claim 1 , wherein said perfluoropolyether-substituted claim 1 , primary or secondary amine compound is amide-linked.5. A process comprising polymerizing at least one vinyl monomer in the presence of at least one polymerization initiator and at least one perfluoropolyether thiol compound of formula (II) above claim 1 , wherein R is hydrogen or alkyl; Q is a divalent organic linking group selected from —CHCHCH—[NH—C(═O)]—CHCHCH— claim 1 , —CHCHCH—[N(CH)—C(═O)]—CHCHCH— claim 1 , —CHCHCH—[N(CH)—C(═O)]—CHCHCH—S—C(═O)—CHCHCH— claim 1 , —CHCH—[NH—C(═O)]—CHCHCH— claim 1 , —CHCH—[O—C(═O)]—CHCH— claim 1 , —(CHCHO)—[C(═O)]—CHCH— claim 1 , and combinations thereof; and R′ claim 1 , a claim 1 , x claim 1 , and y are as defined in .6. A process comprising oxidizing at least one ...

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06-08-2020 дата публикации

K-RAS MODULATORS

Номер: US20200247762A1
Принадлежит:

Provided herein, inter alia, are methods and compounds for modulating K-Ras treating cancer. 2. (canceled)5. The compound of claim 1 , wherein the compound is of Formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:Ring A is phenyl;{'sup': 1', '1', '1', '1', '1D', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1C', '1C', '1A', '1B', '1D', '1A', '1D', '1A', '1C', '1A', '1C', '1A', '1C', '1', '1', '1, 'sub': 3', '2', '2', 'n1', 'v1', 'm1', '2', '3', '2', '2, 'Ris independently halogen, —CX, —CHX, —CHX, —CN, —SOR, —SONRR, —NHNRR, —ONRR, —NHC═(O)NHNRR, —NHC(O)NRR, —N(O), —NRR, —C(O)R, —C(O)—OR, —C(O)NRR, —OR, —NRSOR, —NRC(O)R, —NRC(O)OR, —NROR, —OCX, —OCHX, —OCHX, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl; or'}{'sup': '1', 'two adjacent Rsubstituents may optionally be joined to form a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;'}z1 is an integer from 0 to 4;{'sup': 2', '2', '2', '2', '2A', '2A', '2A', '2B, 'sub': 3', '2', '2, 'Ris independently hydrogen, —CX, —CHX, —CHX, —C(O)R, —C(O)OR, —C(O)NRR, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;'}{'sup': '1', 'Lis a bond, substituted or unsubstituted alkylene, or substituted or unsubstituted cycloalkylene;'}{'sup': 3', '3', '3', '3', '3', '3, 'sub': '2', 'Lis a bond, —S(O)—, —N(R)—, —O—, —S—, —C(O)—, —C(O)N(R)—, —N(R)C(O)—, —N(R)C(O)NH—, —NHC(O)N(R)—, —C(O)O—, —OC(O)—, substituted or unsubstituted alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted cycloalkylene, substituted or unsubstituted ...

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06-08-2020 дата публикации

DOCOSAHEXAENOIC ACID ENDOCANNABINOID EPOXIDE DERIVATIVE COMPOSITIONS

Номер: US20200247776A1
Автор: Das Aditi, Roy Jahnabi
Принадлежит:

The present disclosure provides novel compounds derived from docosahexaenoic acid endocamabinoid epoxides having anti-cancer, anti-inflammatory, anti-platelet aggregation and anti-angiogenic properties. Methods of synthesizing and using the compositions are also provided. 3. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen.4. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl , —Calkylene-R , -G , or —Calkylene-G.5. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris —Calkylene-R.6. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein{'sup': 2', '2', '2, 'sub': '1-6', 'Ris -Gor —Calkylene-G, and'}{'sup': 2', 'x2, 'sub': '3-8', 'Gis Ccycloalkyl optionally substituted with 1, 2, 3, or 4 R.'}8. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Rat each occurrence is independently —OH or —NH.11. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of - , or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.12. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in treating cancer.13. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing inflammation in a subject.14. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing platelet aggregation in a subject.15. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing angiogenesis in a subject.16. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in inducing vasoconstriction or vasodilation in a subject.17. Use of a compound of any one of - , or a pharmaceutically acceptable salt thereof , for manufacturing a medicament for treating cancer ...

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06-08-2020 дата публикации

DERIVATIVES OF EPA ENDOCANNABINOID EPOXIDES AS ANTI-INFLAMMATORY, ANTI-CANCEROUS, ANTI-ANGIOGENC AND ANTIPLATELET AGGREGATION COMPOUNDS

Номер: US20200247777A1
Принадлежит:

The present disclosure provides chemical compound derivatives of a class of biological lipid mediators known as endocannabinoids and methods of synthesizing the compositions. These compounds are useful for treating cancer, reducing inflammation, reducing platelet aggregation, and reducing angiogenesis. 3. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris hydrogen.4. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris Calkyl , or —Calkylene-R , -G , or —Calkylene-G.5. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris —Calkylene-R.6. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein{'sup': 2', '2', '2, 'sub': '1-6', 'Ris -Gor —Calkylene-G, and'}{'sup': 2', 'x2, 'sub': '3-8', 'Gis Ccycloalkyl optionally substituted with 1, 2, 3, or 4 R.'}8. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Rat each occurrence is independently —OH or —NH.11. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of - , or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.12. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in treating cancer.13. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing inflammation in a subject.14. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing platelet aggregation in a subject.15. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in reducing angiogenesis in a subject.16. The compound of any one of - , or a pharmaceutically acceptable salt thereof , for use in inducing vasoconstriction or vasodilation in a subject.17. Use of a compound of any one of - , or a pharmaceutically acceptable salt thereof , for ...

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22-09-2016 дата публикации

Functionalized Graphene Barrier Element

Номер: US20160272575A1
Автор: Zheng Shijun
Принадлежит:

Described herein are functionalized graphene compositions that have gas, fluid, and/or vapor resistant properties. Also described are barrier elements based on the aforementioned compositions. Also described is a barrier device that incorporates the barrier element and further comprises a substrate and a protective coating, encompassing the barrier element. 1. A graphene compound comprising an optionally functionalized graphene directly bonded to —NH—R—NHCOR′ or —CO—NH—R—NHCOR′;{'sub': '1-20', 'wherein R is optionally substituted Chydrocarbylene; and'}{'sub': 1-30', '3-30, 'R′ is optionally substituted Chydrocarbyl or Cheteroaryl.'}2. The compound of claim 1 , wherein the optionally functionalized graphene is a reduced graphene oxide.3. The compound of claim 1 , wherein the optionally functionalized graphene is a graphene oxide.4. The compound of claim 1 , having a molar ratio of nitrogen to carbon that is about 0.001 to about 0.2.5. The compound of claim 1 , having a molar ratio of nitrogen to carbon that is about 0.02 to about 0.1.6. The compound of claim 1 , having molar ratio of oxygen to carbon that is about 0.01 to about 1.7. The compound of claim 1 , having molar ratio of oxygen to carbon that is about 0.2 to about 0.8.8. The compound of claim 1 , further represented by a formula CHNO.9. The compound of claim 1 , wherein R is Calkylene.10. The compound of claim 1 , wherein R is Calkylene.11. The compound of claim 1 , wherein R is —(CH)—.12. The compound of claim 1 , wherein R′ is Calkyl.13. The compound of claim 1 , wherein R′ is —CH.14. A barrier element comprising a compound of claim 1 , wherein the barrier element is transparent.15. The barrier element of claim 14 , wherein the barrier element has a gas permeability of less than 0.100 cc/m-day.16. The barrier element of claim 14 , wherein the element has a moisture permeability of less than 10.0 gm/m-day.17. The barrier element of claim 14 , wherein the element has a transparency of at least about 80%.18. ...

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13-08-2020 дата публикации

Rubber composition, heterocycle-modified glycerin fatty acid ester, and production method for heterocycle-modified glycerin fatty acid ester

Номер: US20200255636A1
Принадлежит: Yokohama Rubber Co Ltd

An object of the present invention is to provide a rubber composition having excellent processability, a heterocycle-modified glycerin fatty acid ester, and a production method for the heterocycle-modified glycerin fatty acid ester. The present invention includes: a rubber composition containing a rubber, silica, and a heterocycle-modified glycerin fatty acid ester, in which an epoxy group is modified with a heterocyclic compound having a heterocycle having at least one H-N< bond, where the heterocycle is at least one selected from the group consisting of a piperazine ring, a morpholine ring, and a thiomorpholine ring, and the heterocycle may have a substituent; the heterocycle-modified glycerin fatty acid ester; and a production method therefor.

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05-09-2019 дата публикации

PKC-ACTIVATING COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20190270715A1
Принадлежит: COGNITIVE RESEARCH ENTERPRISES, INC.

The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturted fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono and polyunsaturated fatty acids. 151.. (canceled)54. A pharmaceutical composition comprising methyl-3-(2-((2-((2-((2-((2-((2-ethylcyclopropyl)methyl)cyclopropyl)methy-1)cyclopropyl)methyl)-cyclopropyl)methyl)cyclopropyl)methyl)cyclopropyl)propanoate or a pharmaceutically acceptable salt thereof , and a pharmaceutically acceptable carrier.56. A method of treating a neurological disease selected from the group consisting of Alzheimer's disease , multiple sclerosis , and stroke comprising administering to a patient in need thereof methyl-3-(2-((2-((2-((2-((2-((2-ethylcyclopropyl)methyl)cyclopropyl)methy-1)cyclopropyl)methyl)-cyclopropyl)methyl)cyclopropyl)methyl)cyclopropyl)propanoate or a pharmaceutically acceptable salt thereof.57. The method of wherein the neurological disease is Alzheimer's disease.58. The method of wherein the neurological disease is multiple sclerosis.59. The method of wherein the neurological disease is stroke. This is a continuation application of U.S. Application No. 14/803,762, filed Jul. 20, 2015, which is a divisional application of U.S. application Ser. No. 13/401,459, filed Feb. 21, 2012, now U.S. Pat. No. 9,119,825, which is a continuation of U.S. application Ser. No. 12/510,681, filed Jul. 28, 2009, now U.S. Patent No. 8,163,800, which claims the benefit of U.S. Provisional Application No. 61/084,172, filed Jul. 28, 2008, all of which are incorporated herein by reference.The present invention relates to compositions and methods to activate an isoform of protein kinase C (PKC). The present invention also provides methods for reducing ...

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25-12-2014 дата публикации

WATER DISPERSIBLE, SELF-CROSSLINKABLE PREPOLYMER COMPOSITON

Номер: US20140378607A1
Автор: Pajerski Anthony D.
Принадлежит: LUBRIZOL ADVANCED MATERIALS, INC.

The present invention provides an economical route to environmentally friendly polymeric coatings with a high content of raw materials from renewable resources. These polymeric coatings offer performance characteristics that are competitive with conventional coating systems. The unique polymers on which this invention is based are copolymers of triglyceride oils, such as soybean oil, linseed oil, or another natural oil, with a vinyl compound, such as an acrylate or methacrylate, or a vinyl aromatic monomer. The present invention more specifically discloses a water dispersible, self-crosslinkable prepolymer composition which is comprised of a triglyceride oil having appended thereto (1) hydroxyl groups, (2) epoxy groups, (3) moieties which contain at least one aldehyde group or at least one ketone group, and (4) moieties which contain at least one vinyl and/or substituted vinyl group. In one embodiment of this invention the moiety which contains at least one vinyl group is derived from maleic anhydride. 1. A self-crosslinkable prepolymer composition which is comprised of at least one triglyceride oil having appended thereto (1) hydroxyl groups , (2) moieties , which contain at least one aldehyde group or at least one ketone group , and (3) moieties , which contain at least one vinyl and/or substituted vinyl group.2. The self-crosslinkable prepolymer composition claim 1 , as specified in claim 1 , wherein the triglyceride oil has epoxy groups appended thereto.3. The self-crosslinkable prepolymer composition claim 1 , as specified in claim 1 , further comprising a free carboxylic acid group or an ionized carboxylic acid group.4. (canceled)7. The self-crosslinkable prepolymer claim 6 , as specified in claim 6 , wherein n represents 2 and R represents a methyl group.8. (canceled)10. The self-crosslinkable prepolymer claim 9 , as specified in claim 9 , wherein m represents 0.11. An aqueous self-crosslinkable prepolymer dispersion which is comprised of water and a ...

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11-10-2018 дата публикации

FUMAGILLOL DERIVATIVES AND POLYMORPHS THEREOF

Номер: US20180291010A1
Автор: Petersen John S.
Принадлежит:

The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer. 2. A polymorphic form of fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt characterized by an X-ray powder diffraction pattern including peaks at about 5.6 , 8.9 , and 15.4 degrees 2θ using Cu Kα radiation.3. The polymorphic form of claim 2 , characterized by an X-ray powder diffraction pattern including peaks at about 5.6 claim 2 , 8.9 claim 2 , 11.5 claim 2 , 12.1 claim 2 , 15.4 claim 2 , and 20.9 degrees 2θ using Cu Kα radiation.4. The polymorphic form of claim 2 , characterized by an X-ray powder diffraction pattern including peaks at about 5.6 claim 2 , 8.9 claim 2 , 11.5 claim 2 , 12.1 claim 2 , 15.4 claim 2 , 15.9 claim 2 , 19.7 claim 2 , 20.9 claim 2 , and 23.3 degrees 2θ using Cu Kα radiation.5. The polymorphic form of claim 2 , characterized by an X-ray powder diffraction pattern including peaks at about 5.6 claim 2 , 8.9 claim 2 , 11.5 claim 2 , 12.1 claim 2 , 14.6 claim 2 , 15.4 claim 2 , 15.9 claim 2 , 17.4 claim 2 , 18.1 claim 2 , 19.7 claim 2 , 20.9 claim 2 , and 23.3 degrees 2θ using Cu Kα radiation.610. The polymorphic form of claim 2 , characterized as having an X-ray diffraction pattern substantially similar to that set forth in claim 2 , or D.7. The polymorphic form of claim 2 , characterized by an endothermic onset at about 181° C. and peak at about 186° C. and an exotherm ...

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20-10-2016 дата публикации

HYDROXAMIC ACIDS AND USES THEREOF

Номер: US20160304443A1
Принадлежит:

Compounds of formula I are provided: 2. The compound of claim 1 , wherein Ris an alkoxy in the R-diastereomeric configuration.3. The compound of claim 1 , wherein Ris an alkoxy in the S-diastereomeric configuration.4. The compound of claim 1 , wherein Ris ethoxy or methoxy.5. The compound of claim 1 , wherein m=1 and Ris 4-chloro.6. The compound of claim 1 , wherein m is an integer from 0 to 2.7. The compound of claim 1 , wherein n is an integer from 0 to 4.8. The compound of claim 1 , wherein each Ris a halogen independently selected from the group consisting of fluorine claim 1 , bromine claim 1 , and chlorine.9. The compound of claim 8 , wherein Ris a 4-substituted halogen.10. The compound of claim 1 , wherein the Rheterocyclyl or hetereocyclylmethyl group comprises a morpholine claim 1 , a piperazine claim 1 , an oxirane claim 1 , or a piperidine.12. The compound of claim 11 , wherein Ris methoxy or ethoxy.13. The compound of claim 11 , wherein at least one Ris halogen.14. The compound of claim 11 , wherein X is chlorine.15. The compound of claim 11 , wherein x is fluorine.16. The compound of claim 11 , wherein at least one Ris heterocyclyl or hetereocyclylmethyl.17. The compound of claim 16 , wherein the heterocyclyl or hetereocyclylmethyl group comprises a morpholine claim 16 , a piperazine claim 16 , an oxirane claim 16 , or a piperidine.19. The compound of claim 11 , wherein at least one Ris halogen.20. The compound of claim 11 , wherein at least one Ris hydroxymethyl.21. The compound of claim 11 , wherein at least on Ris heterocyclyl or hetereocyclylmethyl.22. A compound selected from any one of Examples 1 to 52 of Table 1.23. A pharmaceutical composition comprising a compound according to along with a pharmaceutically acceptable carrier.24botulinum. A method of treating a subject exposed to a toxin comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to the subject a pharmaceutical composition comprising a compound according to .'} ...

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10-09-2020 дата публикации

POSITIVE RESIST COMPOSITION AND PATTERNING PROCESS

Номер: US20200285152A1
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

A positive resist composition is provided comprising two onium salts, a base polymer comprising acid labile group-containing recurring units, and an organic solvent. The positive resist composition forms a pattern having PED stability and improved properties including DOF, LWR, and controlled footing profile. 7. A pattern forming process comprising the steps of applying the positive resist composition of to form a resist film on a substrate claim 1 , exposing the resist film to KrF excimer laser claim 1 , ArF excimer laser claim 1 , EB or EUV claim 1 , and developing the exposed resist film in a developer.8. The pattern forming process of wherein the exposing step is carried out by immersion lithography while a liquid having a refractive index of at least 1.0 is held between the resist film and a projection lens.9. The pattern forming process of claim 8 , further comprising the step of forming a protective film on the resist film claim 8 , wherein immersion lithography is carried out while the liquid is held between the protective film and the projection lens. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2019-040330 filed in Japan on Mar. 6, 2019, the entire contents of which are hereby incorporated by reference.This invention relates to a positive resist composition and a pattern forming process.In the recent drive for higher integration and operating speeds of LSI and memory devices, the pattern rule is made drastically finer. The photolithography which is currently on widespread use in the art is approaching the essential limit of resolution determined by the wavelength of a light source.As the light source used in the lithography for resist pattern formation, g-line (436 nm) or i-line (365 nm) from a mercury lamp was widely used in 1980's. Reducing the wavelength of exposure light was believed effective as the means for further reducing the feature size. For the mass production process of 64 MB dynamic ...

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10-09-2020 дата публикации

GRAPHENE COMPOUND AND MANUFACTURING METHOD THEREOF, ELECTROLYTE, AND POWER STORAGE DEVICE

Номер: US20200287239A1
Автор: Yamakaji Masaki
Принадлежит:

To provide a graphene compound having an insulating property and an affinity for lithium ions. To increase the molecular weight of a substituent included in a graphene compound. To provide a graphene compound including a chain group containing an ether bond or an ester bond. To provide a graphene compound including a substituent containing one or more branches. To provide a graphene compound including a substituent including at least one of an ester bond and an amide bond. 6. An electrolyte comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the graphene compound according to ; and'}a lithium salt.7. A power storage device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the graphene compound according to ;'}an exterior body;a positive electrode current collector, anda negative electrode current collector.13. The power storage device according to claim 8 , further comprising a separator. One embodiment of the present invention relates to a graphene compound, a manufacturing method of the graphene compound, an electrolyte, and a power storage device.Note that one embodiment of the present invention is not limited to the above technical field. The technical field of one embodiment of the invention disclosed in this specification and the like relates to an object, a method, or a manufacturing method. Furthermore, one embodiment of the present invention relates to a process, a machine, manufacture, or a composition of matter. Specifically, examples of the technical field of one embodiment of the present invention disclosed in this specification include a semiconductor device, a display device, a light-emitting device, a power storage device, a memory device, a method for driving any of them, and a method for manufacturing any of them.In recent years, a variety of power storage devices, for example, storage batteries such as lithium-ion storage batteries, lithium-ion capacitors, and air cells have been actively developed. In particular, demand for ...

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05-11-2015 дата публикации

Substituted [1,2,4] Triazole Compounds

Номер: US20150313229A1
Принадлежит:

The present invention relates to substituted [1,2,4]triazol compounds of the formula I 114-. (canceled)16. The compound of claim 15 , wherein m is 1 and Ris in ortho- or meta-position.17. The compound of claim 15 , wherein m is 2 claim 15 , 3 or 4 and two of the Rare in 2 claim 15 ,3- claim 15 , 3 claim 15 ,4- claim 15 , 3 claim 15 ,5- or 2 claim 15 ,6-position.18. The compound of claim 15 , wherein m is 2 claim 15 , 3 or 4 and two of the R claim 15 , are in 2 claim 15 ,4-position claim 15 , wherein one (called R-1) of said two substituents is selected from the group consisting of CN claim 15 , NO claim 15 , OH claim 15 , SH claim 15 , C-C-alkyl claim 15 , C-C-alkoxy claim 15 , C-C-alkenyl claim 15 , C-C-alkynyl claim 15 , C-C-cycloalkyl claim 15 , C-C-cycloalkyloxy claim 15 , NH claim 15 , NH(C-C-alkyl) claim 15 , N(C-C-alkyl) claim 15 , NH(C-C-cycloalkyl) claim 15 , N(C-C-cycloalkyl) claim 15 , S(O)(C-C-alkyl) claim 15 , C(═O)(C-C-alkyl) claim 15 , C(═O)(OH) claim 15 , C(═O)(O—C-C-alkyl) claim 15 , C(═O)(NH(C-C-alkyl)) claim 15 , C(═O)(N(C-C-alkyl)) claim 15 , C(═O)(NH(C-C-cycloalkyl)) and C(═O)—(N(C-C-cycloalkyl); wherein each substituent is unsubstituted or further substituted by one claim 15 , two claim 15 , three or four R; and wherein the other one (called R-2) is halogen or selected from the substituents as defined for R-1.19. The compound of claim 15 , wherein Ris Br or F.20. A composition comprising one compound of formula I claim 15 , as defined in claim 15 , an N-oxide or an agriculturally acceptable salt thereof.21. The composition of claim 20 , comprising additionally a further active substance.22. A method for combating harmful fungi claim 15 , comprising treating the fungi or the materials claim 15 , plants claim 15 , the soil or seeds to be protected against fungal attack with an effective amount of at least one compound of formula I claim 15 , as defined in .28. A method for combating harmful fungi claim 20 , comprising treating the fungi or the ...

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18-10-2018 дата публикации

PLASTICIZER COMPOSITION, RESIN COMPOSITION AND METHODS OF PREPARING THE SAME

Номер: US20180298162A1
Принадлежит:

The present invention relates to a plasticizer composition, a resin composition and methods of preparing the same, and provides a plasticizer composition which is environmentally friendly so as to be suitable for use in applications such as a resin for a food wrapping material, exhibits excellent transparency, color and adhesiveness and can maintain or improve mechanical properties such as tensile strength, an elongation rate and hardness when used as a plasticizer of a resin composition, and a resin composition including the same. 3. The plasticizer composition according to claim 1 , wherein Rin Chemical Formula 1 is selected from the group consisting of a butyl group claim 1 , an isobutyl group claim 1 , a pentyl group claim 1 , a hexyl group claim 1 , a heptyl group claim 1 , an isoheptyl group claim 1 , an octyl group claim 1 , a 2-ethylhexyl group claim 1 , a nonyl group claim 1 , an isononyl group claim 1 , a 6-methyloctyl group claim 1 , a decyl group claim 1 , an isodecyl group and a 2-propylheptyl group.4. The plasticizer composition according to claim 1 , wherein Rin Chemical Formula 1 is selected from the group consisting of a butyl group claim 1 , an isobutyl group claim 1 , a 2-ethylhexyl group claim 1 , an isononyl group claim 1 , a 6-methyloctyl group and a 2-propylheptyl group.5. The plasticizer composition according to claim 1 , wherein the epoxidized alkyl ester composition comprises two or more compounds having a different number of carbon atoms in Rof Chemical Formula 1.6. The plasticizer composition according to claim 1 , wherein the epoxidized alkyl ester composition has an oxirane content (O.C.) of 3.5% or more.7. The plasticizer composition according to claim 1 , wherein the epoxidized alkyl ester composition has an oxirane index (O.I.) of 1.0 or more.8. A resin composition comprising:100 parts by weight of a resin; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '5 to 150 parts by weight of the plasticizer composition according to .'}9. ...

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27-10-2016 дата публикации

DOCOSAHEXAENOYL ETHANOLAMIDES

Номер: US20160311761A1
Принадлежит: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.

The invention describes novel mono or dihydroxy docosahexaenoic acid (DHA) analogues, their preparation, isolation, identification, purification and uses thereof. 2. The compound of claim 1 , wherein Pand Pare both hydrogen atoms.3. The compound of claim 1 , wherein Z is —C(O)NRR—OH.4. The compound of claim 3 , wherein one Ris H and the second Ris ethyl claim 3 ,5. The compound of claim 1 , wherein the hydrogen atom on one or more hydroxyl containing carbon atoms is substituted with an alkyl group.6. The compound of claim 5 , wherein the alkyl group is a methyl group.7. The compound of claim 10 , wherein Z is —C(O)ORand Rof Z is a hydrogen atom.8. A method to treat inflammation claim 1 , neurodegeneration claim 1 , memory loss claim 1 , neuroinflammation claim 1 , reperfusion injury or traumatic brain injury comprising the step of administering to an individual in need thereof claim 1 , an effective amount of the compound of .9. A method to treat neural development claim 1 , fetal development claim 1 , homeostasis claim 1 , tissue remodeling claim 1 , or wound repair comprising the step of administering to an individual in need thereof claim 1 , an effective amount of the compound of .10. The compound of claim 1 , further comprising a pharmaceutically acceptable carrier.12. The purified compound of claim 11 , wherein Pand Pare both hydrogen atoms.13. The purified compound of claim 11 , wherein Z is —C(O)ORand Rof Z is a hydrogen atom.14. The purified compound of claim 11 , wherein one Ris H and the second Ris ethyl.15. The purified compound of claim 11 , wherein Z is —C(O)NRR—OH.16. The purified compound of claim 11 , wherein the hydrogen atom on one or more hydroxyl containing carbon atoms is substituted with an alkyl group.17. The purified compound of claim 16 , wherein the alkyl group is a methyl group.18. The compound of claim 11 , further comprising a pharmaceutically acceptable carrier.19. A method to treat inflammation claim 11 , neurodegeneration claim 11 , ...

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03-11-2016 дата публикации

Chemically Modified Graphene

Номер: US20160318980A1

This disclosure relates to graphene derivatives, as well as related devices including graphene derivatives and methods of using graphene derivatives.

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03-10-2019 дата публикации

ELECTROLYTE FOR RECHARGEABLE LITHIUM BATTERY AND RECHARGEABLE LITHIUM BATTERY

Номер: US20190305374A1
Принадлежит:

An electrolyte for a rechargeable lithium battery and a rechargeable lithium battery including the electrolyte, the electrolyte including a non-aqueous organic solvent; a lithium salt; and an additive, wherein the additive includes a compound represented by Chemical Formula 1: 2. The electrolyte for a rechargeable lithium battery as claimed in claim 1 , wherein R is a substituted or unsubstituted C1 to C5 alkyl group or a substituted or unsubstituted C1 to C5 alkoxy group.3. The electrolyte for a rechargeable lithium battery as claimed in claim 1 , wherein the compound represented by Chemical Formula 1 is included in an amount of 0.1 wt % to 3 wt % claim 1 , based on a total weight of the electrolyte for a rechargeable lithium battery.4. The electrolyte for a rechargeable lithium battery as claimed in claim 1 , further comprising an additional additive claim 1 , the additional additive including vinylethylene carbonate claim 1 , fluoroethylene carbonate claim 1 , propenesultone claim 1 , propanesultone claim 1 , lithiumtetrafluoroborate claim 1 , lithium bis(oxalato)borate claim 1 , succinonitrile claim 1 , lithium difluorophosphate claim 1 , or 2-fluoro biphenyl.5. The electrolyte for a rechargeable lithium battery as claimed in claim 4 , wherein the additional additive is included in an amount of 0.1 wt % to 10 wt % claim 4 , based on a total weight of the electrolyte for a rechargeable lithium battery.6. The electrolyte for a rechargeable lithium battery as claimed in claim 4 , wherein the additional additive and the compound represented by Chemical Formula 1 are included in a weight ratio of 5:1 to 1:5.7. A rechargeable lithium battery claim 4 , comprising:a positive electrode;a negative electrode; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the electrolyte as claimed in .'}8. The rechargeable lithium battery as claimed in claim 7 , wherein R is a substituted or unsubstituted C1 to C5 alkyl group or a substituted or unsubstituted C1 to C5 alkoxy group. ...

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10-11-2016 дата публикации

FIVE-MEMBERED CYCLIC BISCARBONATES BEARING AMIDE LINKAGES, THEIR PREPARATION AND THEIR USES FOR THE PREPARATION OF POLYMERS

Номер: US20160326132A1
Принадлежит:

A compound is of formula (I): 2. The compound of formula (I) according to claim 1 , wherein Ais a linear or branched alkylene comprising from 1 to 10 carbon atom(s).3. The compound of formula (I) according to or claim 1 , wherein Ais H or an alkyl radical comprising from 1 to 10 carbon atom(s).4. The compound of formula (I) according to claim 1 , wherein Aand A claim 1 , together with the two nitrogen atoms bearing them claim 1 , form a saturated heterocyclyl group comprising from 5 to 8 members.5. The compound of formula (I) according to claim 1 , wherein Rand R′ are H.10. (canceled)11. A polymer susceptible to be obtained by the polymerisation of a compound of formula (I) according to and of at least one polyamine.14. A method for preparing a poly(hydroxyurethane) claim 1 , comprising a step of polymerisation of a compound of formula (I) according to claim 1 , and of at least one polyamine claim 1 , said step being carried out at a temperature comprised between 60° C. and 150° C. claim 1 , optionally in the presence of a catalyst such as a strong base and/or a nucleophile. The present invention concerns new 5-membered cyclic biscarbonates, their preparation and their uses, in particular for the preparation of polymers such as poly(hydroxyurethane)s (PHUs) and epoxy resins.Polyurethanes (PUs) are produced using (poly)isocyanates. Isocyanates are toxic compounds, manufactured from an amine and phosgene which is also highly toxic when inhaled. The industrial process for the preparation of isocyanates comprises the reaction of an amine with an excess of phosgene leading to isocyanate and a mixture of phosgene and hydrogen chloride.Therefore, finding alternative routes for the synthesis of PUs which avoid the use of isocyanates is of high importance.Several ways are known to produce more sustainable non isocyanate polyurethanes from non-toxic vegetable oil derivatives, such as:Therefore, there is a need to develop these ways of producing non isocyanate polyurethanes, ...

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30-11-2017 дата публикации

FUMIGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20170342043A1
Принадлежит:

The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. 12.-. (canceled)4. (canceled)1011.-. (canceled)12. The method of claim 3 , wherein the patient is a human.13. (canceled)14. The method of claim 3 , wherein the compound is administered orally claim 3 , intravenously claim 3 , or subcutaneously.15. The method of claim 3 , wherein the compound is administered orally.1618.-. (canceled)19. The method of claim 5 , wherein the patient is a human.20. The method claim 5 , wherein the compound is administered orally claim 5 , intravenously claim 5 , or subcutaneously.21. The method of claim 5 , wherein the compound is administered orally.22. The method of claim 7 , wherein the patient is a human.23. The method claim 7 , wherein the compound is administered orally claim 7 , intravenously claim 7 , or subcutaneously.24. The method of claim 7 , wherein the compound is administered orally.25. The method of claim 8 , wherein the patient is a human.26. The method claim 8 , wherein the compound is administered orally claim 8 , intravenously claim 8 , or subcutaneously.27. The method of claim 8 , wherein the compound is administered orally.28. The method of claim 9 , wherein the patient is a human.29. The method claim 9 , wherein the compound is administered orally claim 9 , intravenously claim 9 , or subcutaneously.30. The method of claim 9 , wherein the compound is administered orally. This application is a continuation of U.S. patent application Ser. No. 14/399,392, filed Nov. 6, 2014, which is a national stage filing under 35 U.S.C. §371 of PCT/US2013/040080, filed May 8, 2013, which claims priority to U.S. Provisional Ser. No. 61/644,612, filed May 9, 2012, all of which are hereby incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over ...

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22-10-2020 дата публикации

PKC-ACTIVATING COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20200331875A1
Принадлежит: COGNITIVE RESEARCH ENTERPRISES, INC.

The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. 151.-. (canceled)52. A method of treating multiple sclerosis , comprising administering to a patient in need thereof an effective amount of a cyclopropanated polyunsaturated fatty acid (PUFA) ester wherein at least one carbon-carbon unsaturated bond in said PUFA is cyclopropanated.53. The method of claim 52 , wherein the ester is a methyl ester.54. The method of claim 52 , wherein all carbon-carbon unsaturated bonds in said PUFA are cyclopropanated.55. The method of claim 52 , wherein said PUFA is selected from the group consisting of lineoleic acid claim 52 , γ-linolenic acid claim 52 , α-linolenic acid claim 52 , arachidonic acid claim 52 , eicosapentaenoic acid claim 52 , eicosatetraenoic acid claim 52 , docosapentaenoic acid claim 52 , docosahexaenoic acid claim 52 , stearidonic acid claim 52 , and adrenic acid. This is a continuation application of U.S. application Ser. No. 16/400,132, filed May 1, 2019, which is a continuation application of U.S. application Ser. No. 14/803,762, filed Jul. 20, 2015, now U.S. Pat. No. 10,323,011, which is a divisional application of U.S. application Ser. No. 13/401,459, filed Feb. 21, 2012, now U.S. Pat. No. 9,119,825, which is a continuation application of U.S. application Ser. No. 12/510,681, filed Jul. 28, 2009, now U.S. Pat. No. 8,163,800, which claims the benefit of U.S. Provisional Application No. 61/084,172, filed Jul. 28, 2008, all of which are incorporated herein by reference.The present invention relates to compositions and methods to activate an isoform of protein kinase C (PKC). The present ...

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07-12-2017 дата публикации

NANO-HYBRID LUBRICANT AND METHOD THEREOF, AND OIL-BASED DRILLING FLUID

Номер: US20170349802A1
Принадлежит: China University of Petroleum (Beijing)

The present invention relates to the well drilling field in petroleum industry, in particular to a nano-hybrid lubricant and method thereof, and oil-based drilling fluid. The lubricant comprises: graphite oxide and a biquaternary ammonium salt compound of which the cation part is represented by formula (1). The present invention also provides a method for preparation of the lubricant and an oil-based drilling fluid containing the lubricant. The lubricant provided in the present invention can be comprehended as a nano-hybrid material. Thus, oil-based drilling fluids that contain the lucbricant provided in the present invention have lower lubrication coefficient and excellent lubricating property without or with little negative impact on rheological property of the oil fluid, and the lubricant provided in the present invention has excellent thermostability thus suitable for use in operation at a high temperature. 2. The lubricant according to claim 1 , wherein each Rgroup is independently selected from H claim 1 , hydroxyl claim 1 , halogen claim 1 , C1-C4 alkyl claim 1 , C1-C4 alkoxy claim 1 , and C1-C4 hydroxyalkyl; each Rgroup is independently selected from H and C1-C4 alkyl; and each Rgroup is independently selected from H claim 1 , C1-C15 alkyl claim 1 , and C1-C15 hydroxyalkyl.3. The lubricant according to claim 2 , wherein each Rgroup is independently selected from H claim 2 , hydroxyl claim 2 , methyl claim 2 , ethyl claim 2 , methoxy claim 2 , ethoxy claim 2 , hydroxymethyl claim 2 , and hydroxyethyl; each Rgroup is independently selected from H claim 2 , methyl claim 2 , ethyl claim 2 , n-propyl claim 2 , and n-butyl; and each Rgroup is independently selected from H claim 2 , methyl claim 2 , ethyl claim 2 , n-propyl claim 2 , n-butyl claim 2 , n-pentyl claim 2 , n-hexyl claim 2 , n-heptyl claim 2 , n-octyl claim 2 , n-nonyl claim 2 , n-decyl claim 2 , hendecyl claim 2 , and dodecyl.4. The lubricant according to claim 3 , wherein each Rgroup is independently ...

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24-12-2015 дата публикации

PLANT OIL-BASED MATERIALS

Номер: US20150368378A1
Принадлежит: NDSU RESEARCH FOUNDATION

Plant oil-based compounds are provided which possess both low viscosity and high reactive functionality. These compounds are useful in coating and composite applications, as well as related methods. Exemplary compounds can be produced by transesterification of a plant oil triglyceride with a nucleophile reactant, such as a vinyl-functional alcohol, to yield reactive fatty acid-containing monomers. 2. The compound of claim 1 , wherein the fatty acid residue is from a plant oil triglyceride.3. The compound of claim 1 , wherein Ris allyl.4. The compound of claim 2 , wherein the plant oil is selected from the group consisting of soybean oil claim 2 , linseed oil claim 2 , sunflower oil claim 2 , safflower oil claim 2 , canola oil claim 2 , corn oil claim 2 , cashew nut oil claim 2 , olive oil claim 2 , peanut oil claim 2 , palm oil claim 2 , sesame oil claim 2 , cottonseed oil claim 2 , rapeseed oil claim 2 , walnut oil claim 2 , almond oil and coconut oil.5. The compound of claim 4 , wherein the oil is soybean oil.6. The compound of claim 1 , wherein at least one of Rand Rcontains at least one functionality selected from the group consisting of epoxide claim 1 , acrylate claim 1 , methacrylate claim 1 , hydroxyl claim 1 , and cyclic carbonate.7. A composition comprising a plurality of compounds of .8. The composition of claim 7 , wherein the plant oil is soybean oil claim 7 , and wherein for each of the plurality of compounds claim 7 , Ris a fatty acid residue independently selected from a linolenic acid claim 7 , a linoleic acid claim 7 , an oleic acid claim 7 , a stearic acid claim 7 , and a palmitic acid.9. A curable composition comprising at least one compound of .10. The curable composition of comprising a reactive diluent comprising the compound of .12. The method of claim 11 , wherein the nucleophilic reactant is monovalent.13. The method of claim 11 , wherein the nucleophile reactant is an alcohol claim 11 , thiol or amine.14. A polymer or copolymer comprising ...

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13-12-2018 дата публикации

Oxaspiro[2.5]Octane Derivatives and Analogs

Номер: US20180354924A1
Принадлежит:

The invention provides oxaspiro[2.5]octane derivatives and analogs, methods for preparation thereof, intermediates thereto, pharmaceutical compositions, and uses thereof in the treatment of various disorders and conditions, such as overweight and obesity. 116.-. (canceled)19. A pharmaceutically acceptable composition comprising the compound of and a pharmaceutically acceptable excipient.20. A method of treating and/or controlling obesity claim 18 , comprising administering to a patient in need thereof an effective amount of the compound of .21. The method of claim 20 , wherein the patient is a human.22. The method of claim 21 , wherein the patient has a body mass index greater than or equal to about 25 kg/mbefore the administration.23. The method of claim 20 , wherein after administration claim 20 , thioredoxin 1 is not significantly present in the testes of a male patient. This application is a continuation of U.S. patent application Ser. No. 15/068,942, filed Mar. 14, 2016; which is a continuation of U.S. patent application Ser. No. 14/003,906, filed Oct. 29, 2014; which is a national stage filing under U.S.C. § 371 of PCT/US2012/028068, filed Mar. 7, 2012; which claims priority to U.S. Provisional Patent Application No. 61/450,301 filed Mar. 8, 2011; all of which are hereby incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or airplane seats, social difficulties, etc.), these conditions, in particular clinical obesity, affect other aspects of health, i.e., diseases and other adverse health conditions associated with, exacerbated by, or precipitated by being overweight or obese. The ...

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20-12-2018 дата публикации

FUMIGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20180360795A1
Принадлежит:

The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. 18-. (canceled)10. (canceled)11. A method of inducing weight loss in a patient in need thereof claim 9 , comprising administering to said patient an effective amount of the compound of .12. The method of claim 9 , wherein the patient is a human.13. The method of claim 9 , wherein the patient has a body mass index greater than or equal to about 25 kg/mbefore the administration14. The method of claim 9 , wherein the compound is administered orally claim 9 , intravenously claim 9 , or subcutaneously.15. The method of claim 9 , wherein the compound is administered orally.16. (canceled) This application is a continuation of U.S. patent application Ser. No. 15/399,071, filed Jan. 5, 2017, which is a continuation of U.S. patent application Ser. No. 14/399,392, filed Nov. 6, 2014, which is a national stage filing under 35 U.S.C. § 371 of PCT/US2013/040080, filed May 8, 2013, which claims the benefit of and priority to U.S. Provisional Ser. No. 61/644,612, filed May 9, 2012, all of which are hereby incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the age of twenty is considered clinically obese. While being overweight or obese presents problems (for example restriction of mobility, discomfort in tight spaces such as theater or airplane seats, social difficulties, etc.), these conditions, in particular clinical obesity, affect other aspects of health, i.e., diseases and other adverse health conditions associated with, exacerbated by, or precipitated by being overweight or obese. The estimated mortality from obesity-related conditions in the United States is over 300, ...

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19-12-2019 дата публикации

Inhibitors of the n-terminal domain of the androgen receptor

Номер: US20190382335A1

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

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26-12-2019 дата публикации

FUMAGILLOL TYPE COMPOUNDS AND METHODS OF MAKING AND USING SAME

Номер: US20190388380A1
Принадлежит:

The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. 10. A method of treating and/or controlling obesity claim 9 , comprising administering to a patient in need thereof an effective amount of the compound of .11. A method of inducing weight loss in a patient in need thereof claim 9 , comprising administering to said patient an effective amount of the compound of .12. The method of claim 10 , wherein the patient is a human.13. The method of claim 10 , wherein the patient has a body mass index greater than or equal to about 25 kg/mbefore the administration.14. The method claim 10 , wherein the compound is administered orally claim 10 , intravenously claim 10 , or subcutaneously.15. The method of claim 10 , wherein the compound is administered orally.16. A pharmaceutical composition comprising a compound of claim 9 , and a pharmaceutically acceptable carrier.17. The composition of claim 16 , wherein the composition is formulated as a unit dose.18. The method of comprising administering said compound in an amount insufficient to reduce angiogenesis in the patient. This application is a continuation of U.S. patent application Ser. No. 15/869,368, filed Jan. 12, 2018, which is a continuation of U.S. patent application Ser. No. 15/399,071, filed Jan. 5, 2017, which is a continuation of U.S. patent application Ser. No. 14/399,392, filed Nov. 6, 2014, which is a national stage filing under 35 U.S.C. § 371 of PCT/US2013/040080, filed May 8, 2013, which claims the benefit of and priority to U.S. Provisional Ser. No. 61/644,612, filed May 9, 2012, all of which are hereby incorporated by reference in their entirety.Over 1.1 billion people worldwide are reported to be overweight. Obesity is estimated to affect over 90 million people in the United States alone. Twenty-five percent of the population in the United States over the ...

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31-12-2020 дата публикации

PROCESS OF PREPARING A PEPTIDE EPOXYKETONE IMMUNOPROTEASOME INHIBITOR, AND PRECURSORS THEREOF

Номер: US20200407334A1
Принадлежит:

Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound “G”): 2. The method of claim 1 , wherein Xis selected from the group consisting of tosylate claim 1 , triflate claim 1 , acetate claim 1 , naphthalene sulfonate claim 1 , 4-nitrobenzenesulfonate claim 1 , sulfate claim 1 , methylsulfate claim 1 , nitrate claim 1 , fluoride claim 1 , chloride claim 1 , bromide claim 1 , and combinations thereof.3. The method of claim 2 , wherein X is tosylate claim 2 , naphthalene sulfonate claim 2 , or 4-nitrobenzenesulfonate.4. The method of claim 3 , wherein X is tosylate.5. The method of any one of to claim 3 , wherein the aprotic solvent is selected from the group consisting of acetonitrile (“ACN”) claim 3 , dichloromethane (“DCM”) claim 3 , tetrahydrofuran (“THF”) claim 3 , dimethylacetamide (“DMAc”) claim 3 , ethyl acetate (“EtOAc”) claim 3 , isopropyl acetate (“iPrOAc”) claim 3 , dimethylformamide (“DMF”) claim 3 , and combinations thereof.6. The method of claim 5 , wherein the aprotic solvent comprises DCM.7. The method of any one of to claim 5 , wherein the tertiary amine base is selected from the group consisting of N claim 5 ,N-diisopropylethylamine (“DIPEA”) claim 5 , triethylamine (“TEA”) claim 5 , N-methylmorpholine (“NMM”) claim 5 , 2 claim 5 ,2 claim 5 ,6 claim 5 ,6-tetramethylpiperidine (“TMP”) claim 5 , 2 claim 5 ,4 claim 5 ,6-trimethylpyridine (“collidine”) claim 5 , and combinations thereof.8. The method of any one of to claim 5 , wherein the tertiary amine base comprises DIPEA.9. The method of any one of to claim 5 , wherein the molar ratio of the tertiary amine base to compound E is in a range of 1:1 to 4:1.10. The method of any one of to claim 5 , wherein the coupling agent comprises a carbodiimide reagent claim 5 , a phosphonium reagent claim 5 , a uronium reagent claim 5 , an ...

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02-02-2006 дата публикации

Modified vegetable oil-based polyols

Номер: WO2006012344A1
Принадлежит: Pittsburg State University

Methods of making unsaturated modified vegetable oil-based polyols are described. Also described are methods of making oligomeric modified vegetable oil-based polyols. An oligomeric composition having a modified fatty acid triglyceride structure is also described. Also, methods of making a polyol including hydroformylation and hydrogenation of oils in the presence of a catalyst and support are described.

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10-11-2022 дата публикации

PKC-ACTIVATING COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20220356161A1
Принадлежит: Synaptogenix, Inc.

The present invention relates to methods of activate an isoform of protein kinase C (PKC) for the treatment of neurological diseases including Alzheimer's disease and stroke using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. The present invention also relates to methods of reducing neurodegeneration using cyclopropanated or epoxidized derivatives of mono- and polyunsaturated fatty acids. 151.-. (canceled)52. A method of treating multiple sclerosis , comprising administering to a patient in need thereof an effective amount of an epoxidized polyunsaturated fatty acid (PUFA) ester wherein at least one carbon-carbon unsaturated bond in said PUFA is epoxidized.53. The method of claim 52 , wherein the ester is a methyl ester.54. The method of claim 52 , wherein all carbon-carbon unsaturated bonds in said PUFA are epoxidized.55. The method of claim 52 , wherein said PUFA is selected from the group consisting of linoleic acid claim 52 , γ-linolenic acid claim 52 , α-linolenic acid claim 52 , arachidonic acid claim 52 , eicosapentaenoic acid claim 52 , eicosatetraenoic acid claim 52 , docosapentaenoic acid claim 52 , docosahexaenoic acid claim 52 , stearidonic acid claim 52 , and adrenic acid.57. The method of claim 56 , wherein R is methyl.58. The method of claim 52 , wherein the epoxidized polyunsaturated fatty acid (PUFA) ester has any of the following formulas: CH(CH)(CH=CHCH)(CH)COOR or CHCH(CH=CHCH)x(CH)COOR claim 52 , wherein x is 2-6 claim 52 , y is 2-6 claim 52 , and R is alkyl claim 52 , wherein at least one carbon-carbon unsaturated bond in said epoxidized PUFA is epoxidized. This is a continuation application of U.S. application Ser. No. 16/903,551 filed Jun. 17, 2020, which is a continuation application of U.S. application Ser. No. 16/400,132, filed May 1, 2019, now U.S. Pat. No. 10,696,644, which is a continuation application of U.S. application Ser. No. 14/803,762, filed Jul. 20, 2015, now U.S. Pat. No. 10,323,011, which ...

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21-09-2006 дата публикации

Analogues of the azinomycins as anti-tumour agents and as prodrugs

Номер: WO2006097730A1

Compounds of general formula (I) or a salt thereof in which R1 is preferably an aromatic DNA binding subunit are oxidation- activated prodrugs. The compounds are expected to be converted into an epoxide at the alkene to which R2 is attached by cytochrome P450, in particular CYPIBI, expressed at high levels in tumours. R3 preferably comprises a Nitrogen mustard to provide a prodrug which has 2 alkylating groups. The prodrugs are expected to be activated preferentially in tumour cells.

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18-11-1998 дата публикации

Reactive radiation- or thermally-initiated cationically-curable epoxide monomers and compositions made from those monomers

Номер: EP0878471A1

Radiation- or thermally-initiated cationically-curable styrene oxides of the structure

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05-10-1999 дата публикации

Reactive radiation- or thermally-initiated cationically-curable epoxide monomers and compositions made from those monomers

Номер: US5962547A

Radiation- or thermally-initiated cationically-curable styrene oxides of the structure ##STR1## are suitable for use in cationically curable adhesive and coating compositions.

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03-09-1986 дата публикации

Coloured photo-hardenable composition

Номер: EP0088050B1
Принадлежит: Ciba Geigy AG

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30-07-2019 дата публикации

改性感光树脂及其应用

Номер: CN110066391A
Автор: 胡春青, 葛庆余, 钱晓春

本发明提供了一种改性感光树脂及其应用。该改性感光树脂通过原料中的感光性树脂与环氧化合物反应得到,感光性树脂具有如下的结构式I, R 1 选自氢、C 1 ~C 10 的直链烷基、C 3 ~C 10 的支链烷基、C 6 ~C 20 的芳香基和C 1 ~C 10 的烷氧基中的任意一种;m 1 、m 2 各自独立地选自0、1~4中的任意一个整数,n 1 、n 2 各自独立地为0、1~3中的任意一个整数;R 2 选自C 1 ~C 10 的直链烷基、C 3 ~C 10 的支链烷基中的任意一种;A、B各自独立地代表取代基团,n为1~20中的任意一个整数。通过改性,减少了其中的羧酸基团,增加了侧链醇羟基或者环氧基等活性基团,进一步降低了感光性树脂的酸值,提高了反应活性和固化性能。

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11-03-2004 дата публикации

Aza-peptide epoxides

Номер: US20040048327A1
Принадлежит: Georgia Tech Research Corp

The present invention provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the invention include aza-peptide epoxide compositions that inhibit proteases, for example cysteine proteases, either in vivo or in vitro. The disclosed compounds, pharmaceutically acceptable salts, pharmaceutically acceptable derivatives, prodrugs, or combinations thereof can be used to treat disease or pathological conditions related to the activity of proteases associated with a specific disease or condition. Such treatable conditions include viral infections, stroke, neurodegenerative disease, and inflammatory disease, among others.

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