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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 5969. Отображено 100.
02-02-2012 дата публикации

7-azoniabicyclo[2.2.1]heptane derivatives, methods of production, and pharmaceutical uses thereof

Номер: US20120029044A1
Принадлежит: Theron Pharmaceuticals Inc

Muscarinic acetylcholine receptor antagonists and methods of using them for the treatment of muscarinic acetylcholine receptor-mediated diseases, such as pulmonary diseases, are provided.

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29-03-2012 дата публикации

Hepatitis C Virus Inhibitors

Номер: US20120076755A1
Принадлежит: Enanta Pharmaceuticals Inc

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B-W  (I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

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10-05-2012 дата публикации

Porphyrin compounds comprising one or more pyridone moieties

Номер: US20120115901A1
Принадлежит: VENTANA RESEARCH Corp

Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.

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14-06-2012 дата публикации

Heterocyclic Radical or Diradical, The Dimers, Oligomers, Polymers, Dispiro Compounds and Polycycles Thereof, the Use Thereof, Organic Semiconductive Material and Electronic or Optoelectronic Component

Номер: US20120146012A1
Принадлежит: NOVALED GMBH

The present invention relates to heterocyclic radicals or diradicals, the dimers, oligomers, polymers, dispiro compounds and polycycles thereof, to the use thereof, to organic semiconductive materials and to electronic and optoelectronic components.

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18-10-2012 дата публикации

Substituted porphyrins

Номер: US20120264725A1
Принадлежит: Individual

Substituted metalloporphyrin compounds are described, along with pharmaceutical compositions containing the same, and methods of use thereof in protecting cells from oxidant-induced toxicity and pathological conditions such as inflammatory lung disease, neurodegenerative conditions, radiation injury, cancer, diabetes, cardiac conditions and sickle cell disease. Mn(III) porphyrins bearing oxygen atoms within side chains are particularly described.

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15-11-2012 дата публикации

Modified colored pigments

Номер: US20120285347A1
Принадлежит: Cabot Corp

The present invention relates to a modified colored pigment comprising a colored pigment having an attached organic group. The organic group is attached to the colored pigment via at least one carbon atom of a C—C single bond or double bond, wherein the C—C single bond or double bond is not a component of an aromatic system. The organic group further comprises at least one activating group on at least one carbon atom of the C—C single bond or double bond. A method of preparing a modified colored pigment is also disclosed, as are aqueous and non-aqueous dispersions, e.g., including ink jet inks, comprising the modified colored pigments.

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29-11-2012 дата публикации

Copolymer containing fluorenylporphyrin-anthracene, preparation method and application thereof

Номер: US20120302717A1

A copolymer containing fluorenylporphyrin-anthracene is disclosed, which comprises a polymer represented by formula (1), in which R 1 , R 2 , R 3 and R 4 , which may be identical or different, are C 1 -C 16 alkyl, and n is an integer of 1 to 100. A preparation method of the copolymer containing fluorenylporphyrin-anthracene and the application thereof in manufacture of solar cell devices, organic field-effect transistors, organic electroluminescent devices, organic optical storage device, organic nonlinear materials or organic laser devices are also disclosed.

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29-11-2012 дата публикации

Long Wavelength Absorbing Porphyrin Photosensitizers for Dye-Sensitized Solar Cells

Номер: US20120302743A1
Принадлежит: Individual

A long wavelength absorbing porphyrin/metalloporphyrin molecule is provided, made up of a porphyrin macrocycle and an anchor group for attachment to a substrate. A molecular linking element is interposed between the porphyrin macrocycle and the anchor group. The porphyrin/metalloporphyrin molecule also includes an (aminophenyl)amine group, either N,N-(4-aminophenyl)amine or N-phenyl-N-(4-aminophenyl)amine, where an amino moiety of the 4-aminophenyl group is derivatized by an element such as hydrogen, haloalkanes, aromatic hydrocarbons, halogenated aromatic hydrocarbons, heteroarenes, halogenated heteroarenes, or combinations of the above-mentioned elements.

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27-12-2012 дата публикации

Copolymer containing fluorenylporphyrin-benzene, preparation method and use thereof

Номер: US20120329979A1

A copolymer containing fluorenylporphyrin-benzene is disclosed, which comprises a copolymer represented by formula (1), in which R 1 , R 2 , R 3 and R 4 , which may be identical or different, are C 1 -C 16 alkyl, and n is an integer of 1 to 100. The preparation method of said copolymer containing fluorenylporphyrin-benzene and the use thereof in manufacture of solar batteries components, organic field effect transistors, organic electroluminescent components, organic optical storage components, organic non-linear materials or organic laser components are also disclosed.

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18-04-2013 дата публикации

POLYANIONIC MULTIVALENT MACROMOLECULES FOR INTRACELLULAR TARGETING OF PROLIFERATION AND PROTEIN SYNTHESIS

Номер: US20130095035A1
Принадлежит: MIVENION GMBH

The present invention relates generally to methods and compositions for targeting of intracellular molecules involved in proliferation and protein synthesis of activated cells using polyanionic multivalent macromolecules. In particular aspect, multiple sulfate groups linked to polyol are specifically targeted to the cytoplasm and nucleus of proliferating and activated cells. The invention further comprises novel polyanionic macromolecular compounds and formulations. 1. Pharmaceutical composition comprising a sulfated polyglycerol and a therapeutic or diagnostic effector molecule that is covalently conjugated to said sulfated polyglycerol.2. Pharmaceutical composition according to of the formula P(OSOM)(L-G-E)with P is a polyol macromolecule wherein a number n of hydroxyl groups is substituted by sulfate groups OSOM claim 1 , M is a cationic inorganic or organic counter ion to the anionic sulfate group claim 1 , E is therapeutic or diagnostic effector molecule claim 1 , L is a linker or spacer between P and E claim 1 , G is a reactive group for the covalent attachment between L and E claim 1 , and m is a number of 1-100.3. Pharmaceutical composition according to for treating a disease by intracellular uptake of said sulfated polyglycerol and a therapeutic or diagnostic effector molecule into activated cells or proliferative cells and by inhibiting NF-kappaB and/or AP-1 and/or inhibiting TGF-beta synthesis in said cells.4. Conjugate comprising a sulfated polyglycerol and a therapeutic or diagnostic effector molecule that is covalently conjugated to said sulfated polyglycerol.5. Conjugate according to of the formula P(OSOM)(L-G-E)with P is a polyol macromolecule wherein a number n of hydroxyl groups is substituted by sulfate groups OSOM claim 4 , M is a cationic inorganic or organic counter ion to the anionic sulfate group claim 4 , E is therapeutic or diagnostic effector molecule claim 4 , L is a linker or spacer between P and E claim 4 , G is a reactive group for the ...

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25-04-2013 дата публикации

PHOTOCHROMIC MATERIAL

Номер: US20130102775A1
Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

The present invention is a photochromic material formed of a biimidazole compound represented by general formula (1-1): The present invention relates to a photochromic material, and more particularly, to a photochromic material formed of a novel biimidazole compound.Photochromic materials are typically materials that have a function (light modulation function) that enables them to reversibly change color (visible light transmittance) as a result of undergoing an isomerization reaction when irradiated with light, and not only materials prior to being irradiated with light, but also materials formed after being irradiated with light, are referred to as photochromic materials. Consequently, photochromic materials are used as eyeglasses for preventing glare, optical switches as well as display materials such as ink having the ability to switch between display and non-display status. In addition, research is also proceeding on their application to optical discs and other recording materials as well as holograms.Changes in color demonstrated by photochromic materials are typically expressed as a reversible chemical reaction of a material that is induced when the material is irradiated with light. Typical known examples of photochromic materials include spiropyran-based compounds, spirooxadine-based compounds, naphthopyran-based compounds, fulgide-based compounds, and diarylethene-based compounds (see, for example, Non-Patent Document 1). In addition, compounds having a novel structure that demonstrate rapid photoreactivity have also been recently reported (see, for example, Non-Patent Document 2).Photochromic materials are broadly divided into those that exhibit a phenomenon referred to as positive photochromism, which causes these materials to change from an uncolored form to a colored form (colored state) accompanying a structural change when irradiated with light, and those that exhibit a phenomenon referred to as negative photochromism (reverse photochromic materials ...

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02-05-2013 дата публикации

HETEROCYCLIC COMPOUNDS CONTAINING AN INDOLE CORE

Номер: US20130109679A1
Принадлежит:

Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention. 1. A compound selected from the group consisting of:N-(2-methoxypyridin-4-yl)-1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide;N-(1-ethyl-1H-benzimidazol-2-yl)-4,4-dimethyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;N-(1-ethyl-1H-benzimidazol-2-yl)-cis-3,4-dimethyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;4R)—N-{1-[3-(dimethylamino)propyl]-1H-benzimidazol-2-yl}-4-methyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;N-(1-ethyl-1H-benzimidazol-2-yl)-5-methyl-1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide;5-methyl-1-oxo-N-[1-(propan-2-yl)-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide;(4R)—N-(1-benzyl-1H-pyrazol-4-yl)-4-methyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;N-(1H-benzimidazol-2-yl)-4,4-dimethyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;(3S,4R)—N-(1-benzyl-1H-pyrazol-4-yl)-3,4-dimethyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;N-(1H-benzimidazol-2-yl)-4-methyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;4,4-dimethyl-N-(1-methyl-1H-benzimidazol-2-yl)-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;N-{1-[3-(dimethylamino)propyl]-1H-benzimidazol-2-yl}-4,4-dimethyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;4-methyl-N-(1-methyl-1H-benzimidazol-2-yl)-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;(5R)-5-methyl-1-oxo-N-[1-(propan-2-yl)-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide;N-(1-ethyl-1H-benzimidazol-2-yl)-4-methyl-1-oxo-1,2,3,4-tetrahydropyrazino[1,2-a]indole-7-carboxamide;N-(1H-benzimidazol-2-yl)-5-methyl-1-oxo-2,3,4,5-tetrahydro-1H-[1,4] ...

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20-06-2013 дата публикации

LIPOMACROCYCLES AND USES THEREOF

Номер: US20130156851A1
Автор: Cui Kunyuan, Liang Dong
Принадлежит:

What is described are macrocyclic compounds formed by reaction of a cyclic compound, which contains an amine, with an epoxide. The macrocyclic compound has the following structure: 2. The macrocyclic compound of claim 1 , comprising at least one amine.5. The macrocyclic compound of claim 4 , comprising a quaternary ammonium or a tertiary amine or both.6. The macrocyclic compound of claim 1 , wherein the cyclic compound is reacted with an amount of epoxide that is proportional to the number of amines in the cyclic compound.7. The macrocyclic compound of claim 1 , wherein the cyclic compound is reacted with an amount of epoxide that is less than the number of amines in the cyclic compound.8. The macrocyclic compound of claim 1 , wherein the cyclic compound is reacted with an amount of epoxide that is proportional to the amount of the cyclic compound.9. The macrocyclic compound of claim 4 , wherein R′ consists an molecular substituent selected from the group consisting of CH2—O—(CH2)9CH3 claim 4 , CH2—O—(CH2)11CH3 claim 4 , CH2—O—(CH2)13CH3 claim 4 , (CH2)9CH3 claim 4 , (CH2)11CH3 claim 4 , (CH2)11CH3 claim 4 , (CH2)13CH3 claim 4 , (CH2)15CH3 and CH2—O—CH(CH2CH3)((CH2)11CH3).10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. The macrocyclic compound according to any of claim 1 , wherein the macrocyclic compound is in a lipid-polynucleotide particle comprising a lipid and a polynucleotide.16. The macrocyclic compound according to any of claim 14 , wherein the polynucleotide is an RNA molecule.17. The macrocyclic compound of claim 16 , wherein the RNA molecule is an siRNA molecule.18. (canceled)19. The macrocyclic compound according to any of claim 1 , wherein the macrocyclic compound is a component of a liposome or a lipid particle.20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. The macrocyclic compound according to any of claim 2 , wherein the macrocyclic compound is in a lipid-polynucleotide particle comprising a lipid and a ...

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27-06-2013 дата публикации

PHOSPHATE ESTERS OF NORIBOGAINE

Номер: US20130165414A1
Принадлежит: DEMERX, INC.

Disclosed herein are phosphate esters of noribogaine and dihydronoribogaine, and esters and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the methods of their use, including in the treatment of addiction and/or pain. 2. The compound of claim 1 , wherein R is a monophosphate.3. The compound of claim 1 , wherein Ris hydrogen.4. The compound of claim 1 , wherein R is a monophosphate and Ris hydrogen.5. A pharmaceutical composition comprising a therapeutically effective amount of the compound of and at least a pharmaceutically acceptable excipient.7. A method for treating pain in a patient which method comprises administering to said patient a therapeutically effective amount of the compound of .8. A method for treating addiction in a patient which method comprises administering to said patient a therapeutically effective amount of the compound of . This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/569,150, filed Dec. 9, 2011, which is incorporated herein by reference in its entirety.This invention is directed to phosphate esters of noribogaine.Noribogaine is a metabolite of ibogaine and is sometimes referred to as 12-hydroxyibogaine. U.S. Pat. No. 2,813,873 claims noribogaine albeit as “12-O-demethylibogaine” while providing an incorrect structural formula for ibogaine. Noribogaine can be depicted by the following formula:Noribogaine and its pharmaceutically acceptable salts have recently received significant attention as a non-addictive alkaloid useful in treating drug dependency (U.S. Pat. No. 6,348,456) and as a potent analgesic (U.S. Pat. No. 7,220,737).Noribogaine is typically administered orally or intravenously and becomes systemically available to the treated patient.This invention is directed in part to phosphate esters of noribogaine and a vicinal dihydro derivative of noribogaine and compositions thereof. The phosphate esters of this invention can be a ...

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27-06-2013 дата публикации

SULFATE ESTERS OF NORIBOGAINE

Номер: US20130165425A1
Принадлежит: DEMERX, INC.

Disclosed herein are sulfate esters of noribogaine or 9,17 dihydronoribogaine, and pharmaceutically acceptable salts of each thereof, pharmaceutical compositions comprising such compounds, and methods of their use, including in treating addiction and/or pain. 2. The compound of claim 1 , wherein Ris hydrogen.3. The compound of claim 1 , wherein Ris SOOR.4. The compound of claim 1 , wherein R is hydrogen.5. The compound of claim 1 , wherein R is SOOR.6. A pharmaceutical composition comprising a compound of and at least one pharmaceutically acceptable excipient.7. A method for treating pain in a patient which method comprises administering to said patient a therapeutically effective amount of the compound of .8. A method for treating addiction in a patient which method comprises administering to said patient a therapeutically effective amount of the compound of . This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application Nos. 61/569,144, filed Dec. 9, 2011, which is incorporated herein by reference in its entirety.This invention is directed to sulfate esters of noribogaine.Noribogaine is a metabolite of ibogaine and is sometimes referred to as 12-hydroxyibogaine. U.S. Pat. No. 2,813,873 claims noribogaine albeit as “12-O-demethylibogaine” while providing an incorrect structural formula for ibogaine. Noribogaine can be depicted by the following formula:Noribogaine and its pharmaceutically acceptable salts have recently received significant attention as a non-addictive alkaloid useful in treating drug dependency (U.S. Pat. No. 6,348,456) and as a potent analgesic (U.S. Pat. No. 7,220,737).Noribogaine is typically administered orally or intravenously and becomes systemically available to the treated patient.This invention is directed to sulfate esters of noribogaine and a vicinal dihydro derivative of noribogaine, and compositions comprising each of them. As used herein, the sulfate esters include pharmaceutically acceptable salts and ...

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27-06-2013 дата публикации

STEREOSELECTIVE TOTAL SYNTHESIS OF NORIBOGAINE

Номер: US20130165647A1
Принадлежит: DEMERX, INC.

This invention relates generally to methods for synthesizing the non-addictive alkaloid noribogaine. 5. The method of claim 1 , wherein greater than 90% of the noribogaine 1 is of the 2R claim 1 , 4S claim 1 , 5S claim 1 , 18R stereochemical configuration.6. The method of claim 1 , wherein greater than 95% of the noribogaine 1 is of the 2R claim 1 , 4S claim 1 , 5S claim 1 , 18R stereochemical configuration.7. The method of claim 1 , wherein greater than 99% of the noribogaine 1 is of the 2R claim 1 , 4S claim 1 , 5S claim 1 , 18R stereochemical configuration.8. The method of claim 1 , wherein the method further comprises the step of separating two or more stereoisomers. This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application Nos. 61/568,568, filed Dec. 8, 2011, which is incorporated herein by reference in its entirety.This invention relates generally to methods for synthesizing the non-addictive alkaloid noribogaine. This invention is further directed to intermediates used in the chiral directed synthesis of noribogaine.Noribogaine is a well known member of the ibogaine family of alkaloids and is sometimes referred to as 12-hydroxyibogaine. U.S. Pat. No. 2,813,873 claims noribogaine albeit as “12-O-demethylibogaine” while providing an incorrect structural formula for ibogaine. The structure of noribogaine has now been determined and found to combine the features of tyrptamine, tetrahydrohavaine and indolazepines. Noribogaine can be depicted by the following formula:where the configuration at the 2, 4, 5, 6 and 18 atoms are 2(R), 4(S), 5(S), 6(S) and 18(R).Noribogaine and its pharmaceutically acceptable salts have recently received significant attention as a non-addictive alkaloid useful in treating drug dependency (U.S. Pat. No. 6,348,456) and as a potent analgesic (U.S. Pat. No. 7,220,737).Conventionally, noribogaine is prepared by the O-demethylation of naturally occurring ibogaine:which is isolated from a shrub of West Africa. ...

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04-07-2013 дата публикации

USE OF DERIVATIVES OF PENTAPHYRINE AS ANTIMICROBIAL AND DISINFECTANT AGENTS

Номер: US20130172396A1
Принадлежит: UNIVERSITA' DEGLI STUDI DI UDINE

The invention relates to the use of 20-(4-carboxyphenyl)-2,13-dimethyl-3,12-diethyl-[22] pentaphyrine as antibacterial agent in photodynamic treatment. This expanded porphyrin derivatized in position 4 with a carboxyphenyl group proved very active after photo-oxidation both against and . Its high antibacterial activity and its low toxicity make this pentaphyrine particularly useful as antimicrobial agent both for photodynamic therapy against bacterial infections and in the disinfection of microbiologically contaminated liquids. 1. A derivative of pentaphyrine consisting of 20-(4-carboxyphenyl)-2 ,13-dimethyl-3 ,12-diethyl-[22] pentaphyrine , its metallated derivatives and salts thereof having an antimicrobial activity by photodynamic activation.2. The derivative of pentaphyrine according to claim 1 , wherein the metals of the metallated derivatives are selected from Si claim 1 , Ge claim 1 , Lu claim 1 , Yb claim 1 , Ln claim 1 , Al claim 1 , Mn claim 1 , Fe claim 1 , Ru claim 1 , Hg claim 1 , Zn claim 1 , Cu claim 1 , Mg claim 1 , Ni claim 1 , Pd claim 1 , Pt claim 1 , Ag and Au.3. A derivative of pentaphyrine selected from the group consisting of 20-(4-carboxyphenyl)-2 claim 1 ,13-dimethyl-3 claim 1 ,12-diethyl-[22] pentaphyrine claim 1 , its metallated derivatives and salts thereof for use as photodynamically-activated antimicrobial agent In photodynamic treatment.4. A method of treatment of microbial infections by photodynamic therapy comprising the administration in a subject in a need thereof of an effective amount of at least one derivative of pentaphyrine selected from the group consisting of 20-(4-carboxyphenyl)-2 claim 1 ,13-dimethyl-3 claim 1 ,12-diethyl-[22] pentaphyrine claim 1 , its metallated derivatives and salts thereof.5. The method of treatment according to claim 4 , wherein the microbial infections are bacterial infections.6. A method of disinfection comprising the treatment with an effective amount of at least one derivative of pentaphyrine ...

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25-07-2013 дата публикации

Emissive dendrimer composition

Номер: US20130187538A1
Принадлежит: Hewlett Packard Development Co LP

The present disclosure is directed towards emissive dendrimer compositions, luminescence-based pixels, luminescence-based sub-pixels, and associated methods with an emissive dendrimer having various structures as described herein.

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15-08-2013 дата публикации

Organic electroluminescent element

Номер: US20130207097A1

Provided is an organic electroluminescent device (EL device) that uses an indolocarbazole compound. The organic EL device includes an anode, a plurality of organic layers including a phosphorescent light-emitting layer, and a cathode laminated on a substrate, in which at least one organic layer selected from the phosphorescent light-emitting layer, a hole-transporting layer, an electron-transporting layer, and a hole-blocking layer contains an indolocarbazole compound represented by the general formula (1). In the general formula (1), a ring I and a ring II represent rings represented by the formula (1a) and the formula (1b), respectively, each of which are fused to an adjacent ring. X's each represent nitrogen or C—Y and at least one of X's represents nitrogen. Y's each represent hydrogen, an alkyl group, a cycloalkyl group, or an aromatic group. A represents an alkyl group, a cycloalkyl group, or an aromatic group. At least one of Y and A represents an alkyl group or a cycloalkyl group. R's each represent hydrogen, an alkyl group, a cycloalkyl group, an aromatic hydrocarbon group, or an aromatic heterocyclic group.

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15-08-2013 дата публикации

THERMOSTABLE ENZYME TECHNOLOGY FOR ALGAL BIOCONVERSION

Номер: US20130210083A1
Принадлежит:

Thermostable enzyme technology for algal bioconversion The present invention relates to thermostable enzyme systems suitable for use in the production of biofuels and bio-products from algae, and to a method of producing energy feedstocks, stocks, specifically (i) fermentable sugars and (ii) lipid fractions from algae, for the production of biofuels such as bioethanol, biobutanol and bio-oils or biodiesel, as well as other value-added biomolecules (e.g. proteins, peptides, oils, pigments, nucleic acids). 1Talaromyces emersonii. A method of producing fermentable sugars from algal biomass comprising hydrolysing the dried biomass with an enzyme composition , the enzyme composition being derived from which has been grown in the presence of carob powder , or in the presence of a mixture of tea leaves and paper plates , or in the presence of algae and isolating the sugars from the resultant hydrolysate.2. A method as claimed in wherein the algal biomass is dried prior to hydrolysis.3. A method as claimed in wherein the algal biomass does not undergo chemical or extensive mechanical pretreatment prior to hydrolysis.4. A method as claimed in wherein the carob powder claim 1 , or the tea leaves and paper plates are present in the growth medium in an amount of about 2%(w/v).5. A method as claimed in wherein the algae are present in the growth medium in an amount of about 2%(w/v).6. A method as claimed in wherein cultures grown on algae are prepared from cells grown on carob powder or tea leaves and paper plates in the growth medium in an amount of about 2%(w/v).7. A method as claimed in wherein the hydrolysis is carried out for at least 18 hours.8. A method as claimed in wherein the hydrolysis is carried out for at least 6-24 hours.9. A method as claimed in wherein a ratio of enzyme to algal biomass of 0.5mL suitably diluted unconcentrated enzyme system (i.e. fermentation broth) to 50-500 mg algal biomass (dry weight) is used.10Laminaria saccharina, SargussumPalmaria ...

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29-08-2013 дата публикации

PORPHYRIN TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: US20130225545A1
Принадлежит:

Compositions and methods of treating a neurodegenerative disorder are disclosed herein. 2. The compound of claim 1 , wherein the compound has the formula of Formula (II) and M is a metal ion.3. The compound of claim 1 , wherein the compound is the compound of formula II and wherein M is manganese.6. The compound of claim 1 , wherein X claim 1 , X claim 1 , Xand Xare fluorine.10. The compound of claim 9 , wherein R claim 9 , R claim 9 , R claim 9 , and Rare independently a substituted or unsubstituted C-Calkyl.11. The compound of claim 9 , wherein R claim 9 , R claim 9 , R claim 9 , and Rare independently unsubstituted methyl claim 9 , unsubstituted ethyl claim 9 , or unsubstituted propyl.13. The compound of claim 12 , wherein Rand Rare independently substituted or unsubstituted C-Calkyl.14. The compound of claim 12 , wherein Rand Rare independently hydrogen claim 12 , unsubstituted methyl claim 12 , unsubstituted ethyl claim 12 , or unsubstituted propyl.15. The compound of claim 12 , wherein Xand Xare fluorine.16. The compound of claim 1 , wherein Ris —C(X) claim 1 , Ris —C(X) claim 1 , Ris —C(X)and Ris —C(X).17. The compound of claim 16 , wherein X claim 16 , X claim 16 , Xand Xare fluorine.18. A method of treating a neurodegenerative disorder comprising administering to a patient in need thereof an effective amount of a compound of .19. The method of claim 18 , wherein said neurodegenerative disorder is Parkinson's disease claim 18 , Alzheimer's disease claim 18 , Pick's disease claim 18 , Huntington's disease claim 18 , amyotrophic lateral sclerosis claim 18 , prion diseases claim 18 , dystonia claim 18 , dementia with Lewy bodies claim 18 , multiple system atrophy claim 18 , progressive supranuclear palsy claim 18 , Friedreich's Ataxia claim 18 , temporal lobe epilepsy claim 18 , stroke claim 18 , traumatic brain injury claim 18 , or a mitochondrial encephalopathy.20. The method of claim 18 , wherein said neurodegenerative disorder is Parkinson's disease. This ...

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05-09-2013 дата публикации

Pyrido- and pyrimidopyrimidine derivatives as anti-profilerative agents

Номер: US20130231353A1
Принадлежит: Janssen Pharmaceutica NV

The present invention concerns the compounds of formula wherein a 1 -a 2 =a 3 -a 4 represents a divalent radical selected from N—CH═CH—CH, N—CH═N—CH or CH—CH═N—CH; Z represents NH; Y represents —C 3-9 alkyl-, —C 1-5 alkyl-NR 13 —C 1-5 alkyl-, —C 1-6 alkyl-NH—CO— or —CO—NH—C 1-6 alkyl-; X 1 represents —O— or —NR 11 —; X 2 represents —C 1-2 alkyl-, —O—C 1-2 alkyl, —O— or —O—CH 2 —; R 1 represents hydrogen or halo; R 2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C 1-4 alkyloxycarbonyl-, Het 16 -carbonyl- or Ar 5 ; R 3 represents hydrogen; R 4 represents hydroxy, C 1-4 alkyloxy-, Ar 4 —C 1-4 alkyloxy or substituted C 1-4 alkyloxy; R 11 represents hydrogen; R 12 represents hydrogen, C 1-4 alkyl- or C 1-4 alkyl-oxy-carbonyl-; R 13 represents morpholinyl-C 1-4 alkyl; Het 2 represents morpholinyl or piperidinyl optionally substituted with C 1-4 alkyl-, preferably methyl; Het 14 represents morpholinyl; Het 16 represents morpholinyl or pyrrolidinyl; Ar 4 represents phenyl; Ar 5 represents phenyl optionally substituted with cyano.

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12-09-2013 дата публикации

CDK Inhibitors

Номер: US20130237533A1
Принадлежит: G1 THERAPEUTICS, INC.

Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. 2. The compound of claim 1 , wherein Ris hydrogen or C-Calkyl.3. The compound of having the formula selected from the structures shown in .14. The compound of claim 1 , wherein both of X are N.15. The compound of claim 1 , wherein Ris selected from the structures of .16. The compound of claim 1 , wherein Ris -(alkylene)-heterocyclo claim 1 , -(alkylene)-NRR claim 1 , -(alkylene)-C(O)—NRR claim 1 , -(alkylene)-C(O)—O-alkyl or -(alkylene)-ORany of which may be optionally independently substituted with one or more Rgroups as allowed by valance claim 1 , and wherein two Rgroups bound to the same or adjacent atom may optionally combine to form a ring.21. The compound of claim 17 , wherein each Ris only optionally substituted by C-Calkyl claim 17 , halogen or hydroxy.22. The compound of claim 18 , wherein each Ris only optionally substituted by C-Calkyl claim 18 , halogen or hydroxy.23. The compound of claim 19 , wherein each Ris only optionally substituted by C-Calkyl claim 19 , halogen or hydroxy.24. The compound of claim 20 , wherein each Ris only optionally substituted by C-Calkyl claim 20 , halogen or hydroxy.27. The compound of claim 1 , wherein Ris not further substituted.28. The compound of claim 17 , wherein R* is alkylene claim 17 , -(alkylene)m-O-(alkylene)m- claim 17 , -(alkylene)m-C(O)-(alkylene)m- claim 17 , -(alkylene)m-S(O)2-(alkylene)m- and or -(alkylene)m-NH-(alkylene)m- wherein each m is independently 0 or 1 claim 17 , and wherein any alkylene is not further substituted.29. The compound of claim 18 , wherein R* is alkylene claim 18 , -(alkylene)m-O-(alkylene)m- claim 18 , -(alkylene)m-C(O)-(alkylene)m- claim 18 , -(alkylene)m-S(O)2-(alkylene)m- and or -(alkylene)m-NH-(alkylene)m- wherein each m is independently 0 or 1 claim 18 , and wherein any alkylene is not further substituted.30. The compound of claim 19 , wherein R* is alkylene claim 19 ...

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12-09-2013 дата публикации

CDK INHIBITORS

Номер: US20130237534A1
Принадлежит: G1 THERAPEUTICS, INC.

Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. 2. The compound of claim 1 , wherein Ris hydrogen or C-Calkyl.3. (canceled)4. The compound of claim 1 , wherein Ris selected from any one of the structures of .5. The compound of claim 1 , wherein Ris -(alkylene)-heterocyclo claim 1 , -(alkylene)-NRR claim 1 , -(alkylene)-C(O)—NRR claim 1 , -(alkylene)-C(O)—O-alkyl or -(alkylene)-ORany of which may be optionally independently substituted with one or more Rgroups as allowed by valance claim 1 , and wherein two Rgroups bound to the same or adjacent atom may optionally combine to form a ring.10. The compound of claim 6 , wherein each Ris only optionally substituted by C-Calkyl claim 6 , halogen or hydroxy.11. The compound of claim 7 , wherein each Ris only optionally substituted by C-Calkyl claim 7 , halogen or hydroxy.12. The compound of claim 8 , wherein each Ris only optionally substituted by C-Calkyl claim 8 , halogen or hydroxy.13. The compound of claim 9 , wherein each Ris only optionally substituted by C-Calkyl claim 9 , halogen or hydroxy.16. The compound of claim 1 , wherein Ris not further substituted.17. The compound of claim 6 , wherein R* is an alkylene claim 6 , -(alkylene)-O-(alkylene)- claim 6 , -(alkylene)-C(O)-(alkylene)- claim 6 , -(alkylene)-S(O)-(alkylene)- or -(alkylene)-NH-(alkylene)- wherein each m is independently 0 or 1 claim 6 , and wherein any alkylene is not further substituted.18. The compound of claim 7 , wherein R* is an alkylene claim 7 , -(alkylene)-O-(alkylene)- claim 7 , -(alkylene)-C(O)-(alkylene)- claim 7 , -(alkylene)-S(O)-(alkylene)- or -(alkylene)-NH-(alkylene)- wherein each m is independently 0 or 1 claim 7 , and wherein any alkylene is not further substituted.19. The compound of claim 8 , wherein R* is an alkylene claim 8 , -(alkylene)-O-(alkylene)- claim 8 , -(alkylene)-C(O)-(alkylene)- claim 8 , -(alkylene)-S(O)-(alkylene)- or -(alkylene)-NH-(alkylene)- wherein ...

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12-09-2013 дата публикации

Cdk inhibitors

Номер: US20130237544A1
Принадлежит: G1 Therapeutics Inc

Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.

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03-10-2013 дата публикации

Highly Active Multidentate Catalysts for Efficient Alkyne Metathesis

Номер: US20130261295A1

The invention relates to highly active and selective catalysts for alkyne metathesis. In one aspect, the invention includes a multidentate organic ligand wherein one substrate-binding site of the metal center is blocked. In another aspect, the invention includes N-quaternized or silane-based multidentate organic ligands, capable of binding to metals. In yet another aspect, the invention includes N-quaternized or silane-based multidentate catalysts. The catalysts of the invention show high robustness, strong resistance to small alkyne polymerization and significantly enhanced catalytic activity compared to their corresponding non-quaternized or non-silane-based multidentate catalyst analogues. 2. The compound of claim 1 , wherein Ris N and each G is independently substituted with at least one electron-withdrawing substituent.3. The compound of claim 1 , where Ris selected from the group consisting of N claim 1 ,NH(A) claim 1 , NR(A) claim 1 , B claim 1 , P claim 1 , CH claim 1 , CR claim 1 , SiR and a 1 claim 1 ,3 claim 1 ,5-trivalent phenyl moiety claim 1 , wherein R is optionally substituted alkyl or aryl claim 1 , and A is an anion.8. The compound of claim 7 , wherein M is a transition metal.9. The compound of claim 8 , wherein M is selected from the group consisting of Mo claim 8 , W claim 8 , Re and Ta.10. The compound of claim 7 , wherein Ris N and each G is independently substituted with at least one electron-withdrawing substituent.11. The compound of claim 7 , where Ris selected from the group consisting of N claim 7 ,NH(A) claim 7 , NR(A) claim 7 , B claim 7 , P claim 7 , CH claim 7 , CR claim 7 , SiR and a 1 claim 7 ,3 claim 7 ,5-trivalent phenyl moiety claim 7 , wherein R is optionally substituted alkyl or aryl claim 7 , and A is an anion.12. The compound of claim 7 , wherein G is phenyl claim 7 , naphthyl or anthracenyl.14. The compound of claim 13 , wherein Ris NH(A) or N(R)(A) claim 13 , R is optionally substituted alkyl or aryl claim 13 , and A is an ...

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24-10-2013 дата публикации

NOVEL DRUG TARGETS TO OVERCOME DE NOVO DRUG-RESISTANCE IN MULTIPLE MYELOMA

Номер: US20130281389A1
Принадлежит:

Topoisomerase II alpha (topo IIα) is exported from the cell nucleus in human myeloma cells by a chromosome-maintenance protein-1 (CRM1)-dependent mechanism, resulting in topo II inhibitor resistance. The nuclear export signal (NES) of topo IIα is unique, making it a potential target for small molecule inhibitors. Small molecules NES inhibitors were identified, which inhibited binding of topo IIα to the export receptor CRM1. Inhibition was specific to topo IIα as p53 trafficking was unaffected along with topo IIα protein expression and function (decatenation). These topo IIα-specific nuclear export inhibitors may potentially lead to a new approach in circumventing drug resistance in multiple myeloma. The compounds provide a protocol for treating multiple myeloma or an oncogenic disease. Further, the topoisomerase II nuclear export signal inhibitor may be combined with a topoisomerase II inhibitor. 2. The method of claim 1 , wherein the topoisomerase II nuclear export signal inhibitor is NCI-36400 claim 1 , NCI-35847 claim 1 , NCI-80640 claim 1 , NCI-9138 claim 1 , NCI-155877 claim 1 , NCI-203305 claim 1 , NCI-281703 claim 1 , or NCI-35024.3. The method of claim 2 , wherein the topoisomerase II nuclear export signal inhibitor is NCI-35847 claim 2 , NCI-80640 claim 2 , NCI-9138 claim 2 , or NCI-15587.4. The method of claim 1 , wherein the topoisomerase II nuclear export signal inhibitor is administered at 2 μM to 25 μM.5. The method of claim 1 , further comprising co-administering the topoisomerase II nuclear export signal inhibitor with a topoisomerase II inhibitor.6. The method of claim 5 , wherein the topoisomerase II inhibitor is administered concurrently claim 5 , at between 1.6 to 24 hours after administration of the topoisomerase II nuclear export signal inhibitor claim 5 , or at about 4 hours after administration of the topoisomerase II nuclear export signal inhibitor.7. The method of claim 5 , wherein the topoisomerase II inhibitor is amsacrine claim 5 , ...

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31-10-2013 дата публикации

Compounds for organic electroluminescent devices

Номер: US20130285036A1
Принадлежит: Merck Patent GmBH

The present invention relates to aromatic nitrogen heterocycles, and to electronic devices, in particular organic electroluminescent devices, which comprise these aromatic nitrogen heterocycles, in particular in a hole-injection layer and/or in a hole-transport layer and/or in a hole-blocking layer and/or in an electron-transport layer and/or in an emitting layer.

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05-12-2013 дата публикации

Porphyrin compounds comprising one or more pyridone moieties

Номер: US20130324714A1
Принадлежит: VENTANA RESEARCH Corp

Various porphyrin compounds comprising one or more pyridone moieties, intermediates thereof, compositions thereof, and, methods of making and using thereof.

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26-12-2013 дата публикации

REVERSAL OF DRUG-INDUCED NEUROMUSCULAR BLOCK USING NOVEL MOLECULAR CONTAINERS

Номер: US20130345273A1
Принадлежит:

Provided are methods for reversing the effects of agents used for muscular immobilization and/or loss of consciousness and/or loss of pain perception. The method comprises administering a composition comprising acyclic CB[n]-type compounds to an individual in need of reversal of the effects of neuromuscular blocking agents and/or anesthetic agents such that the effects of the agent(s) are partially fully reversed. 8) The method of claim 1 , wherein the compound is a salt claim 1 , a partial salt claim 1 , a hydrate claim 1 , a polymorph or a mixture thereof claim 1 , and a stereoisomer and all mixtures thereof.9) The method of claim 1 , wherein the individual is in need of reversal of drug-induced neuromuscular block.10) The method of claim 1 , wherein the individual is in need of reversal of anesthesia.11) The method of claim 1 , wherein the individual is in need of reversal of drug-induced neuromuscular block and anesthesia.12) The method of claim 1 , wherein the individual in need is a human.13) The method of claim 1 , wherein the individual in need is a non-human mammal. This application claims priority to U.S. provisional patent application nos. 61/392,722, filed Oct. 13, 2010, and 61/392,729, filed Oct. 13, 2010, the disclosures of which are incorporated herein by reference.This invention was made with government support under grant no. CHE0615049 awarded by the National Science Foundation. The government has certain rights in the invention.The present invention relates generally to reversal of the effects of agents used to immobilize and anesthetize patients during medical interventions. More particularly, the invention relates to reversal of both, drug-induced neuromuscular block, and anesthesia by administering novel acyclic CB[n]-type container compounds to individuals in need of suchGeneral anesthesia is a drug-induced, reversible condition comprising five behavioral states: hypnosis (loss of consciousness), amnesia, analgesia, and immobility (no movement ...

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02-01-2014 дата публикации

Molecular glasses with functionalizable groups

Номер: US20140005370A1
Автор: Olivier Lebel
Принадлежит: Minister of National Defence of Canada

Disclosed herein is a compound having Formula I: or a salt thereof, in which R 1 , R 2 and R 3 are as defined herein. Also disclosed are processes to prepare compounds of Formula I and use of compounds of Formula I to prepare stable glassy phases.

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09-01-2014 дата публикации

SUBSTITUTED PORPHYRINS

Номер: US20140011794A1
Принадлежит:

The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating cellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods. 2. The method according to claim 1 , wherein said compound inhibits an oxidase.3. The method according to claim 2 , wherein said oxidase is xanthine oxidase.5. The method according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare the same.7. The method according to claim 6 , wherein X is methyl or ethyl.9. The method according to claim 1 , wherein said compound is complexed with a metal selected from the group consisting of manganese claim 1 , iron claim 1 , copper claim 1 , cobalt claim 1 , nickel or zinc.10. The method according to claim 9 , wherein said compound is complexed with manganese. This application is a continuation of U.S. patent application Ser. No. 13/457,232, filed Apr. 26, 2013, which in turn is a continuation of U.S. patent application Ser. No. 12/885,198, filed Sep. 17, 2010, now issued as U.S. Pat. No. 8,217,026, which in turn is a continuation of U.S. patent application Ser. No. 11/424,662, filed Jun. 16, 2006, now issued as U.S. Pat. No. 7,820,644, which in turn is a divisional of U.S. patent application Ser. No. 10/349,171, filed Jan. 23, 2003, now issued as U.S. Pat. No. 7,189,707, which in turn is a continuation of U.S. patent application Ser. No. 09/490,537, filed Jan. 25, 2000, now issued as U.S. Pat. No. 6,544,975, all of which claim the benefit of U.S. Provisional Patent Application No. 60/117,010, filed Jan. 25, 1999, and each of which is incorporated herein in its entirety and for all purposes.This invention was made with Government support under Grant Nos. HL31992 and HL63397 award by the National Institutes of Health. The Government has certain rights in the invention.The present invention ...

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09-01-2014 дата публикации

Targeted Cancer Therapy Conjugates Using Porphyrins and Porphyrin-like Molecules and Various Cytotoxic Agents

Номер: US20140011985A1
Принадлежит: Individual

Disclosed are targeted in-vivo cancer therapeutics based on the creating conjugate combinations of a porphyrin or porphyrin-like molecule or compound used as a delivery vehicle or vector, coupled with a cytotoxic agent that is released upon binding to a tumor site. The families of porphyrin or porphyrin-like molecules or compounds have a high affinity to bind with cancer cells and are organic structures and are not toxic or rejected by the body. The structure includes a binding site for metals and nano-particles. Benefits of the current invention include: accurate, targeted in-vivo radio and therapeutic agents delivered directly to tumor sites. A benefit of targeted therapy is sparing healthy cells and tissue, thus keeping the host patient healthier which enhances the therapeutic effects of reducing and destroying the cancer tumors. An additional benefit is keeping the patient from discomfort of sickness and the side effects of traditional radio and chemo-therapies.

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09-01-2014 дата публикации

PAA NANOPARTICLES FOR TUMOR TREATMENT AND IMAGING

Номер: US20140011989A1
Принадлежит: PHOTOLITEC, LLC

A tetrapyrrolic photosensitizer and imaging compound having a substituent other than hydrogen at its 10 carbon atom which substituent may contain a PAA nanoparticle. 13. A conjugate of the compound of with a PAA nanoparticle.14. The conjugate of where Ris -phenyl-CONHconjugated with a PAA nanoparticle to form —CONH-PAA. Nanoscience is being developed in conjunction with advanced medical science for further precision in diagnosis and treatment. Multidisciplinary biomedical scientific teams including biologists, physicians, mathematicians, engineers and clinicians are working to gather information about the physical properties of intracellular structures upon which biology's molecular machines are built. A new emphasis is being given to moving medical science from laboratory to the bedside and the community. This platform development program brings together an outstanding laboratory that is pioneering biomedical applications of PAA (polyacrylic acid) nanovectors (Kopelman), together with an innovative porphyrin chemistry and a world-class PDT (photodynamic therapy) group at RPCI that is highly experienced in the high volume screening and in vitro/in vivo evaluation of novel compounds, and in developing new therapies from the test tube to FDA approval for clinical use. Although nanoplatforms and nanovectors (i.e. a nanoplatform that delivers a therapeutic or imaging agent) for biomedical applications are still evolving, they show enormous promise for cancer diagnosis and therapy. The approach has been the subject of several recent reviews. Therapeutic examples include nanoparticles (NPs) containing PDT agents, folate receptor-targeted, boron containing dendrimers for neutron capture and NP-directed thermal therapy. Recently, therapeutic and imaging potential of encapsulated, post-loaded and covalently linked photosensitizer-NPs have been evaluated. In PAA NP the post-loading efficiency showed enhanced in vitro/in vivo therapeutic and imaging potential. PAA NP have core ...

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06-02-2014 дата публикации

Switchable special effect substances

Номер: US20140034623A1
Принадлежит: BASF SE

A process for altering the absorption of electromagnetic radiation by one or more compounds of the general formulae (I) wherein these compounds are irradiated with electromagnetic radiation of wavelength from 300 to 750 nm. The use of compounds of the general formula (I) or (II) for marking materials, for example paper or mineral oil, and use of compounds of the general formula (I) or (II) for causing a color change. The use of compounds of the general formula (I) or (II) for laser welding, heat management, as a photoinitiator, as a free-radical scavenger or for detection of oxygen. A process for regulating the absorption or transmission of electromagnetic radiation by a material wherein one or more compounds of the general formula (I) or (II) are contacted with this material and these compounds are irradiated with electromagnetic radiation of wavelength from 300 to 750 nm. Specific compounds of the general formula (I).

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03-04-2014 дата публикации

MOLECULAR CONTAINERS AND METHODS OF MAKING AND USING SAME

Номер: US20140094529A1
Принадлежит: University of Maryland, College Park

Acyclic CB[n]-type compounds, methods of making such compounds, and uses of the compounds. For example, these compounds can be used as nanocontainers to solubilize pharmaceutical agents. Also provided are compositions and methods of using them for therapy or prophylaxis of a wide variety of conditions for which therapy or prophylaxis is desirable. 8) The compound of claim 1 , wherein the compound is a salt claim 1 , a partial salt claim 1 , a hydrate claim 1 , a polymorph or a mixture thereof claim 1 , and a stereoisomer and all mixtures thereof.9) A composition comprising a compound of and a pharmaceutical agent.10) The composition of claim 9 , wherein the pharmaceutical agent is non-covalently complexed to the compound.11) A composition as in claim 10 , wherein the pharmaceutical agent has a solubility of less than 100 μM in an aqueous solvent.12) A method for prophylaxis and/or therapy of a condition in an individual comprising administering to an individual in need of the prophylaxis and/or the therapy a composition comprising a compound of and a pharmaceutical agent claim 1 , wherein subsequent to the administration the therapy and/or the prophylaxis of the condition in the individual occurs. This application claims priority to U.S. provisional patent application Nos. 61/392,722, filed Oct. 13, 2010, and 61/392,729, filed Oct. 13, 2010, the disclosures of which are incorporated herein by reference.This invention was made with government support under grant no. CHE0615049 awarded by the National Science Foundation. The government has certain rights in the invention.The present invention generally relates to molecular containers. More particularly, the present invention relates to acyclic CB[n]-type compounds, and methods of making and using such compounds.Only 1 out of 10,000 novel drug candidates makes it through the drug development pipelines to reach the pharmacy shelves. It is estimated that about 40% of novel drug candidates fail due to low bioavailability ...

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10-04-2014 дата публикации

PROCESS FOR PRODUCING OPTICALLY ACTIVE SUCCINIMIDE DERIVATIVES AND INTERMEDIATES THEREOF

Номер: US20140099681A1
Принадлежит:

A process for producing optically active succinimide derivatives as key intermediates of (3R)-2′-(4-bromo-2-fluorobenzyl)spiro{pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine}-1′,2,3′,5(2′H)-tetraone, which comprises the following reaction steps. 2. The production process according to claim 1 , wherein the enzyme is a pig liver esterase or a rabbit liver esterase.3. The process according to claim 1 , wherein Ris ethyl.4. The production process according to claim 3 , wherein the enzyme is a pig liver esterase or a rabbit liver esterase.6. The process according to claim 5 , wherein Ris ethyl.7. The production process according to claim 5 , wherein Ris benzyloxycarbonylamino claim 5 , Ris ethyl claim 5 , and Ris ethyl.9. The production process according to claim 8 , wherein the enzyme is a pig liver esterase or a rabbit liver esterase.10. The process according to claim 8 , wherein Ris ethyl.11. The production process according to claim 10 , wherein the enzyme is a pig liver esterase or a rabbit liver esterase.13. The process according to claim 12 , wherein Ris ethyl.14. The production process according to claim 12 , wherein Ris benzyloxycarbonylamino claim 12 , Ris ethyl claim 12 , and Ris ethyl.16. The production process according to claim 15 , wherein the enzyme is a pig liver esterase or a rabbit liver esterase.17. The process according to claim 15 , wherein Ris ethyl.18. The production process according to claim 17 , wherein the enzyme is a pig liver esterase or a rabbit liver esterase. This patent application is a divisional of copending U.S. patent application Ser. No. 13/148,263, filed on Aug. 5, 2011, which is the U.S. national phase of International Patent Application No. PCT/JP2010/000695 filed on Feb. 5, 2010, which claims the benefit of Japanese Patent Application No. 2009-025599, filed on Feb. 6, 2009, each of which is incorporated by reference in its entirety herein.Incorporated by reference in its entirety herein is a computer-readable nucleotide/amino acid ...

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07-01-2016 дата публикации

NEW SPIRO[3H-INDOLE-3,2'-PYRROLIDIN]-2(1H)-ONE COMPOUNDS AND DERIVATIVES AS MDM2-P53 INHIBITORS

Номер: US20160000764A1
Принадлежит:

The present invention relates to compounds of formula (I) 3. The compound according to wherein{'sup': 1', 'd1', 'e1, 'sub': 1-6', '3-6', '6-10', '3-6', '6-10, 'claim-text': [{'sup': d1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1', 'e1, 'sub': 2', '2', '1-4, 'each Ris independently selected from the group consisting of —OR, —NRR, halogen, —CN, —C(O)R, —C(O)OR, —C(O)NRR, —S(O)R, —S(O)NRR, —NHC(O)Rand —N(Calkyl)C(O)R;'}, {'sup': 'e1', 'sub': 1-6', '2-6', '2-6', '1-6', '3-6', '4-6', '6-10, 'each Rindependently of one another denotes hydrogen or a group selected from the group consisting of Calkyl, Calkenyl, Calkynyl, Chaloalkyl, Ccycloalkyl, Ccycloalkenyl, Caryl, 5-10 membered heteroaryl and 3-10 membered heterocyclyl; or'}], 'Ris Calkyl, optionally substituted by a group selected from the group consisting of Ccycloalkyl, Caryl and 5-10 membered heteroaryl, wherein this Ccycloalkyl, Caryl and 5-10 membered heteroaryl is optionally substituted by one or more, identical or different Rand/or R;'}{'sup': '1', 'sub': 1-6', '1-6', '1-6, 'Ris selected from the group consisting of Calkoxy-Calkyl and Chaloalkyl;'}or a salt thereof.4. The compound according to claim 1 , wherein{'sup': 2', '3', 'b2', 'c2, 'claim-text': [{'sup': b2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2', 'c2, 'sub': 2', '2', '1-4, 'each Ris independently selected from the group consisting of —OR, —NRR, halogen, —CN, —C(O)R, —C(O)OR, —C(O)NRR, —S(O)R, —S(O)NRR, —NHC(O)Rand —N(Calkyl)C(O)R;'}, {'sup': 'c2', 'sub': 1-6', '2-6', '2-6', '1-6', '3-6', '4-6, 'each Rindependently of one another denotes hydrogen or a group selected from the group consisting of Calkyl, Calkenyl, Calkynyl, Chaloalkyl, Ccycloalkyl, Ccycloalkenyl, phenyl, 5-6 membered heteroaryl and 3-7 membered heterocyclyl;'}], 'one of Rand Ris hydrogen and the other is selected from the group consisting of phenyl and 5-6 membered heteroaryl, wherein this phenyl and 5-6 membered heteroaryl is optionally ...

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03-01-2019 дата публикации

Benzimidazolo[1,2-a]benzimidazole derivatives for organic light emitting diodes

Номер: US20190002469A1
Принадлежит: Idemitsu Kosan Co Ltd

Compounds of formula (I) and their use in electronic devices, especially electroluminescent devices: (I) wherein at least two of the substituents R 1 and R 2 , R 2 and R 3 , R 3 and R 4 , R 5 and R 6 , R 6 and R 7 , or R 7 and R 8 form together one of the following ring systems (IIa), (IIb) (IIc). When used as charge transport material, charge blocker material and/or host material in electroluminescent devices, the compounds of formula (I) may provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices and reduced driving voltage of electroluminescent devices.

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03-01-2019 дата публикации

METHODS FOR SYNTHESIZING METAL MESOPORPHYRINS

Номер: US20190002481A1
Принадлежит:

Embodiments describe methods of synthesizing metal mesoporphyrin compounds. In embodiments, a metal mesoporphyrin compound may be formed by hemin transmetallation and subsequent hydrogenation of the tin protoporphyrin IX to form a metal mesoporphyrin. In other embodiments, a method of synthesizing a metal mesoporphyrin compound comprises forming a protoporphyrin methyl ester from hemin and converting the protoporphyrin methyl ester intermediate to a metal mesoporphyrin compound through metal insertion and hydrogenation. In other embodiments, a metal mesoporphyrin compound may be formed from hemin by a hydrogen-free hydrogenation method to form a mesoporphyrin IX intermediate followed by metal insertion and hydrogenation. In embodiments, a method of synthesizing a metal mesoporphyrin compound comprises forming a mesoporphyrin IX dihydrochloride intermediate compound and converting the mesoporphyrin IX intermediate to a metal mesoporphyrin compound through metal insertion. In embodiments, a metal mesoporphyrin compound may be formed directly from hemin without isolation of any intermediates. 1. A method of synthesizing a metal mesoporphyrin compound comprising:hydrogenating hemin with ferrous sulfate, palladium on carbon, and poly(methylhydrosiloxane) in formic acid to form a mesoporphyrin formate: converting the mesoporphyrin formate to a mesoporphyrin IX dihydrochloride intermediate compound;isolating the mesoporphyrin IX dihydrochloride intermediate compound; and inserting a metal into the mesoporphyrin IX dihydrochloride intermediate.2. The method of claim 1 , wherein the metal may be selected from tin claim 1 , iron claim 1 , zinc claim 1 , chromium claim 1 , manganese claim 1 , copper claim 1 , nickel claim 1 , magnesium claim 1 , cobalt claim 1 , platinum claim 1 , gold claim 1 , silver claim 1 , arsenic claim 1 , antimony claim 1 , cadmium claim 1 , gallium claim 1 , germanium claim 1 , and palladium.3. The method of claim 2 , wherein the metal is tin.4. The ...

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05-01-2017 дата публикации

LITHIUM REAGENT COMPOSITION, AND METHOD AND DEVICE FOR QUANTIFYING LITHIUM IONS USING SAME

Номер: US20170003228A1
Принадлежит: METALLOGENICS CO., LTD.

A lithium reagent composition for determining lithium concentration, with which it is possible to instantaneously determine the amount of lithium contained in an aqueous solution, such as a biosample or an environmental sample, by means of a simple colorimeter or ultraviolet-visible spectrophotometer and which renders a visual assessement possible; and a method and device for quantifying lithium ions using the composition. A lithium reagent composition obtained by mixing the compound represented by the structural formula, wherein all of the hydrogen atoms bonded to carbon atoms of tetraphenylporphyrin have been replaced with fluorine atoms, as a chelating agent with a basic organic compound selected from monoethanolamine, diethanolamine, and triethanolamine and producing an aqueous solution thereof that further contains a pH regulator with which the pH has been regulated to 5 or higher; and a method and device for quantifying lithium ions using the composition. 2. The reagent composition for lithium according to claim 1 , in which said pH modifier is selected from acids including hydrochloric acid claim 1 , nitric acid claim 1 , acetic acid claim 1 , phosphoric acid claim 1 , citric acid claim 1 , carbonic acid claim 1 , bicarbonate claim 1 , oxalic acid and hydrochloric acid claim 1 , alkali medicine including sodium hydroxide claim 1 , potassium hydroxide and ammonia claim 1 , and their salts.3. The reagent composition for lithium according to claim 1 , in which said pH modifier is pH buffer.4. The reagent composition for lithium according to claim 3 , in which said pH buffer is selected from citric acid claim 3 , carbonic acid claim 3 , bicarbonate claim 3 , phosphoric acid claim 3 , succinic acid claim 3 , phthalic acid claim 3 , ammonium chloride claim 3 , sodium hydroxide claim 3 , potassium hydroxide claim 3 , as Good buffer claim 3 , MES claim 3 , Bis-Tris claim 3 , ADA claim 3 , PIPES claim 3 , ACES claim 3 , MOPSO claim 3 , BES claim 3 , MOPS claim 3 , TES ...

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01-01-2015 дата публикации

GREEN SULFUR BACTERIA VARIANT AND BACTERIOCHLOROPHYLL

Номер: US20150005490A1
Принадлежит:

Provided is a novel strain permitting genetic engineering of green sulfur bacteria that synthesize bacteriochlorophyll e. Isolated green sulfur bacterium Chlorobaculum limnaeum strain RK-j-1 with accession number NITE BP-1202; isolated transformed Chlorobaculum limnaeum strain obtained by transformation of strain RK-j-1, preferably Chlorobaculum limnaeum dbchU strain with accession number NITE BP-1203 wherein bchU gene is disrupted; a production method of bacteriochlorophyll f containing a step of cultivating Chlorobaculum limnaeum strain dbchU; and bacteriochlorophyll f obtained by the aforementioned production method. 1. An isolated green sulfur bacterium Chlorobaculum limnaeum strain RK-j-1 shown by accession number NITE BP-1202.2. An isolated transformant strain of Chlorobaculum limnaeum obtained by transforming the strain RK-j-1 according to .3. The transformant strain of Chlorobaculum limnaeum according to claim 2 , wherein a bchU gene is disrupted.4. The transformant strain of Chlorobaculum limnaeum according to claim 3 , which is a Chlorobaculum limnaeum strain dbchU shown by accession number NITE BP-1203.5. A production method of bacteriochlorophyll f comprising a step of cultivating the transformant strain of Chlorobaculum limnaeum according to .6. Bacteriochlorophyll f obtained by the production method according to .7. Bacteriochlorophyll f produced by the Chlorobaculum limnaeum strain dbchU according to .10. A reconstituted chlorosome comprising the bacteriochlorophyll f according to as a constituent component.11. A production method of bacteriochlorophyll f comprising a step of cultivating the transformant strain of Chlorobaculum limnaeum according to .12. Bacteriochlorophyll f obtained by the production method according to .15. A reconstituted chlorosome comprising the bacteriochlorophyll f according to as a constituent component.16. A reconstituted chlorosome comprising the bacteriochlorophyll f according to as a constituent component.17. A ...

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01-01-2015 дата публикации

STEREOSELECTIVE TOTAL SYNTHESIS OF NORIBOGAINE

Номер: US20150005492A1
Принадлежит: DEMERX, INC.

This invention relates generally to methods for synthesizing the non-addictive alkaloid noribogaine. 114.-. (canceled)19. The method of claim 15 , wherein greater than 90% of the compound of Formula 1 is of the 2R claim 15 , 4S claim 15 , 5S claim 15 , 18R stereochemical configuration.20. The method of claim 15 , wherein greater than 95% of the compound of Formula 1 is of the 2R claim 15 , 4S claim 15 , 5S claim 15 , 18R stereochemical configuration.21. The method of claim 15 , wherein greater than 99% of the compound of Formula 1 is of the 2R claim 15 , 4S claim 15 , 5S claim 15 , 18R stereochemical configuration.22. The method of claim 15 , wherein the method further comprises the step of separating two or more stereoisomers. This application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/568,568, filed Dec. 8, 2011, which is incorporated herein by reference in its entirety.This invention relates generally to methods for synthesizing the non-addictive alkaloid noribogaine. This invention is further directed to intermediates used in the chiral directed synthesis of noribogaine.Noribogaine is a well known member of the ibogaine family of alkaloids and is sometimes referred to as 12-hydroxyibogaine. U.S. Pat. No. 2,813,873 claims noribogaine albeit as “12-O-demethylibogaine” while providing an incorrect structural formula for ibogaine. The structure of noribogaine has now been determined and found to combine the features of tryptamine, tetrahydrohavaine and indolazepines. Noribogaine can be depicted by the following formula:where the configuration at the 2, 4, 5, 6 and 18 atoms are 2(R), 4(S), 5(S), 6(S) and 18(R).Noribogaine and its pharmaceutically acceptable salts have recently received significant attention as a non-addictive alkaloid useful in treating drug dependency (U.S. Pat. No. 6,348,456) and as a potent analgesic (U.S. Pat. No. 7,220,737).Conventionally, noribogaine is prepared by the O-demethylation of naturally ...

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07-01-2021 дата публикации

ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE

Номер: US20210005825A1
Принадлежит: IDEMITSU KOSAN CO., LTD.

An organic electroluminescence device comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises at least one first compound selected from the compounds represented by formulae (19), (21), (22), and (23), a second compound selected from the compounds represented by formula (3a), and a dopant material selected from the compounds represented by formulae (D1) and (D2) is excellent in its performance. 2. The organic electroluminescence device according to claim 1 , wherein the content of the second compound in the fluorescent emitting layer is less than that of the first compound in the fluorescent emitting layer.3. The organic electroluminescence device according to claim 1 , wherein the content of the second compound in the fluorescent emitting layer is 30% by mass or less based on a total amount of the first compound claim 1 , the second compound claim 1 , and the dopant material.4. The organic electroluminescence device according to claim 1 , wherein the content of the dopant material in the fluorescent emitting layer is 10% by mass or less based on a total amount of the first compound claim 1 , the second compound claim 1 , and the dopant material.10. The organic electroluminescence device according to claim 7 , wherein at least one of R claim 7 , R claim 7 , R claim 7 , R claim 7 , and Rof formula (1) does not form a substituted or unsubstituted ring structure having 3 or more ring atoms.20. The organic electroluminescence device according to claim 7 , wherein Rand Rof formula (1) are bonded to each other to form at least two substituted or unsubstituted ring structures each having 3 or more ring atoms.21. The organic electroluminescence device according to claim 7 , wherein{'sub': 1', '2', '2', '3, 'a pair of Rand Rand a pair of Rand R;'}{'sub': 4', '5', '5', '6, 'a pair of Rand Rand a pair of Rand R;'}{'sub': 5', '6', ...

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07-01-2021 дата публикации

Organic electroluminescence element and electronic apparatus

Номер: US20210005826A1
Принадлежит: Idemitsu Kosan Co Ltd

An organic electroluminescence device comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises a first compound, a second compound having a hole mobility larger than that of the first compound, and a dopant material showing a fluorescent spectrum with a half width of 30 nm or less; and an organic electroluminescence device comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises a first compound, a third compound having an affinity larger than that of the first compound, and a dopant material showing a fluorescent spectrum with a half width of 30 nm or less and the content of the third compound in the fluorescent emitting layer is less than that of the first compound in the fluorescent emitting layer are excellent in their performance.

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02-01-2020 дата публикации

FUSED CYCLIC COMPOUND, AND PREPARATION METHOD AND USE THEREOF

Номер: US20200006668A1
Автор: CHEN Zhi Kuan, Sun Hua
Принадлежит:

The invention relates to a fused cyclic compound having a structure of Formula in the fused cyclic compound by controlling effective conjugation of aromatic and heterocyclic rings. Electron transport performance is balanced while hole performance of fused cyclic compound improves. The compound has high triplet energy level and glass transition temperature. The material molecule isn't prone to crystallization. The compound ensures transfer of energy to a guest material. Adjusting substituents of fused cyclic compound improves electron and hole transport performances, reduces difference between singlet and triplet energy levels, broadens recombination region of carriers, and prevents triplet-triplet exciton annihilation. An organic light-emitting device contains the fused cyclic compound. The compound is used as a host material in a light emitting layer. The energy level of the light emitting layer becomes more matched with adjacent carrier transport layers, reducing driving voltage of the device while increasing the luminescence efficiency of the device. 2. The fused cyclic compound according to claim 1 , wherein{'sub': 1', '2', '1', '30', '2', '30', '2', '30', '3', '30', '1', '30', '1', '30', '6', '60', '3', '30, 'Rand Rare each independently selected from hydrogen, halo, cyano, a C-Csubstituted or unsubstituted alkyl group, a C-Csubstituted or unsubstituted alkenyl group, a C-Csubstituted or unsubstituted alkynyl group, a C-Csubstituted or unsubstituted cycloalkyl group, a C-Csubstituted or unsubstituted alkoxy group, a C-Csubstituted or unsubstituted silyl group, a C-Csubstituted or unsubstituted aryl group, or a C-Csubstituted or unsubstituted heteroaryl group;'}{'sub': 1', '2', '1', '30', '2', '30', '2', '30', '3', '30', '1', '30', '1', '30', '6', '60', '3', '30, 'Arand Arare each independently selected from hydrogen, halo, cyano, a C-Csubstituted or unsubstituted alkyl group, a C-Csubstituted or unsubstituted alkenyl group, a C-Csubstituted or unsubstituted ...

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02-01-2020 дата публикации

FUSED CYCLIC COMPOUND, AND PREPARATION METHOD AND USE THEREOF

Номер: US20200006669A1
Автор: CHEN Zhi Kuan, Sun Hua
Принадлежит:

The invention relates to a fused cyclic compound having a structure of Formula compound by controlling conjugation of aromatic and heterocyclic rings. The electron transport performance balances while hole performance of the fused cyclic compound improves. The compound has high triplet energy level and glass transition temperature. The material molecule isn't prone to crystallization. The compound ensures transfer of energy to a guest material. Adjusting substituents improves electron and hole transport performances, reducing the difference between energy levels, broadening the recombination region of carriers, and preventing triplet-triplet exciton annihilation. The invention also relates to an organic light-emitting device having at least one functional layer containing the fused cyclic compound used as a host material in a light emitting layer. The energy level of the light emitting layer becomes matched with that of the carrier transport layers, reducing the driving voltage of the device while increasing luminescence efficiency of the device. 2. The fused cyclic compound according to claim 1 , wherein{'sub': 1', '2', '1', '30', '2', '30', '2', '30', '3', '30', '1', '30', '1', '30', '6', '60', '3', '30, 'Rand Rare each independently selected from hydrogen, halo, cyano, a C-Csubstituted or unsubstituted alkyl group, a C-Csubstituted or unsubstituted alkenyl group, a C-Csubstituted or unsubstituted alkynyl group, a C-Csubstituted or unsubstituted cycloalkyl group, a C-Csubstituted or unsubstituted alkoxy group, a C-Csubstituted or unsubstituted silyl group, a C-Csubstituted or unsubstituted aryl group, or a C-Csubstituted or unsubstituted heteroaryl group;'}{'sub': 1', '1', '30', '2', '30', '2', '30', '3', '30', '1', '30', '1', '30', '6', '60', '3', '30, 'Aris selected from hydrogen, halo, cyano, a C-Csubstituted or unsubstituted alkyl group, a C-Csubstituted or unsubstituted alkenyl group, a C-Csubstituted or unsubstituted alkynyl group, a C-Csubstituted or ...

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08-01-2015 дата публикации

USE OF CERTAIN METAL-ACCUMULATING PLANTS FOR THE PERFORMANCE OF ORGANIC CHEMISTRY REACTIONS

Номер: US20150011749A1
Принадлежит:

Metal-accumulating plants for preparing compositions including a metal catalyst derived from the plants. The composition is substantially devoid of organic matter. Also, carrying out chemical reactions with the compositions prepared from metal-accumulating plants. 1SedumPotentilla griffithii, Arabis paniculata, Arabis gemmifera, Arabis alpina, GentianaGentiana atuntsiensis, Silene viscidula, Corydalis davidii, Incarvillea deltoides, Corydalis pterygopetala, Picris divaricata, Sonchus asper. A composition comprising at least one metal catalyst , the metal of which has been accumulated after thermal treatment of a plant or part of a plant of the genus or of plants selected from sp. , wherein the metal that has accumulated is at least one metal selected in particular from zinc (Zn) , iron (Fe) or copper (Cu) , said composition being substantially devoid of organic matter , for carrying out reactions of organic synthesis involving said catalyst.2SedumPotentilla griffithii.. The composition according to claim 1 , wherein the plant or the part of a plant is of the genus or of the plant3Sedum jinianum, Sedum plumbizincicola, Sedum alfrediiPotentilla griffithii, Potentilla griffithii, Arabis paniculata, Arabis gemmifera, Arabis alpina, GentianaGentiana atuntsiensis, Silene viscidula, Corydalis davidii, Incarvillea deltoides, Corydalis pterygopetala, Picris divaricata, Sonchus asper. The composition according to claim 1 , wherein the plant or the part of a plant is selected from and sp. claim 1 , in which said at least one metal is selected from zinc (Zn) claim 1 , calcium (Ca) claim 1 , magnesium (Mg) claim 1 , iron (Fe) claim 1 , cadmium (Cd) or copper (Cu) claim 1 , said composition optionally having been previously filtered and/or purified on resin and/or fixed on a support claim 1 , after acid treatment.4. The composition according to claim 3 , wherein the acid treatment is carried out with hydrochloric acid claim 3 , in particular gaseous HCl claim 3 , 1N HCl to 12N ...

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03-02-2022 дата публикации

MACROCYCLIC INHIBITORS OF ALK, TRKA, TRKB, AND ROS1

Номер: US20220033402A1
Принадлежит: Dana-Farber Cancer Institute, Inc.

Disclosed are compounds that inhibit ALK, TRKA, TRKB, TRKC and ROS1. Also disclosed are pharmaceutical compositions containing the compounds and methods of using the compounds to treat disease. 2. The compound of claim 1 , wherein ring A is pyrazole and X and Xare independently C or N.3. The compound of claim 1 , wherein Ris methyl or cyclopropyl claim 1 , or wherein Ris H claim 1 , CN claim 1 , methyl or methoxy claim 1 , or wherein Ris hydrogen claim 1 , methyl claim 1 , CHF claim 1 , ethyl claim 1 , CHCF claim 1 , CHCHF claim 1 , or CHCN.4. (canceled)5. (canceled)6. The compound of claim 1 , wherein Ris hydrogen or methyl claim 1 , or Rand Rtogether with the atoms to which they are bound form a 5-6 membered heterocyclic.33. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt or stereoisomer thereof claim 1 , and a pharmaceutically acceptable carrier.34. The composition of claim 33 , which is in the form of a capsule or a tablet or a liquid.35. (canceled)36. A method of treating a disease or disorder characterized or mediated by aberrant ALK claim 1 , TRKA claim 1 , TRKB claim 1 , TRKC or ROS1 activity claim 1 , comprising administering a therapeutically effective amount of the compound of or a pharmaceutically acceptable salt or stereoisomer thereof claim 1 , to a subject in need thereof.37. The method of claim 36 , wherein the disease or disorder characterized or mediated by aberrant ALK activity.38. The method of claim 36 , wherein the disease or disorder is cancer.39. The method of claim 38 , wherein the cancer is a carcinoma claim 38 , ALK(+)-anaplastic large cell lymphoma claim 38 , non-small cell lung cancer claim 38 , or neuroblastoma.40. (canceled)41. (canceled)42. (canceled) This application claims the benefit of priority under 35 U.S.C. § 119(e) to U.S. Provisional Application No. 62/737,546, filed on Sep. 27, 2018 and to U.S. Provisional Application No. 62/882,181 ...

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17-04-2014 дата публикации

POLYHEDRAL CAGE-CONTAINING METALLOPORPHYRIN FRAMEWORKS, METHODS OF MAKING, AND METHODS OF USING

Номер: US20140107333A1
Принадлежит:

Embodiments of the present disclosure provide compositions including metal-organic polyhedrons, metalloporphyrin framework structures, methods of making these, methods of using these, and the like. 2. The composition of claim 1 , wherein the R1 claim 1 , R2 claim 1 , R3 claim 1 , and R4 are independently selected from: H claim 1 , a polycarboxylated ligand claim 1 , a polypyridyl ligand claim 1 , a polycyano ligand claim 1 , a polyphosphonate ligand claim 1 , a polyhydroxyl ligand claim 1 , a polysulfonate ligand claim 1 , a polyimidazolate claim 1 , ligand claim 1 , a polytriazolate ligand claim 1 , and a combination thereof claim 1 , wherein at least one of R1 claim 1 , R2 claim 1 , R3 claim 1 , and R4 is not H.3. The composition of claim 1 , wherein the two of R1 claim 1 , R2 claim 1 , R3 claim 1 , and R4 are H and the other two are independently selected the moiety.4. The composition of claim 3 , wherein the moiety is an aromatic dicarboxylic acid moiety.5. The composition of claim 1 , wherein R1 and R3 are H and R2 and R4 are an isophthalic acid moiety.6. The composition of claim 1 , wherein each of R1 claim 1 , R2 claim 1 , R3 claim 1 , and R4 are independently selected the moiety.7. The composition of claim 6 , wherein the moiety is an aromatic dicarboxylic acid moiety.8. The composition of claim 6 , wherein the moiety is an isophthalic acid moiety.9. The composition of claim 1 , wherein the secondary building unit includes a metal.10. The composition of claim 1 , wherein the secondary building unit is selected from the group consisting of: a dicopper paddlewheel secondary building unit claim 1 , a distorted dicobalt trigonal prism secondary building unit claim 1 , a dimetal secondary building unit claim 1 , a square paddlewheel secondary building unit claim 1 , a dimetal triangular paddlewheel secondary building unit claim 1 , a tetra-metal clusters secondary building unit claim 1 , and a single metal ion secondary building unit.11. The composition of claim ...

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24-01-2019 дата публикации

Nanofibrous Filter

Номер: US20190022570A1
Принадлежит:

There is provided a nanofibrous filter comprising a substrate and self-assembled nanofibers deposited on the substrate. The self-assembled nanofibers comprise π-conjugated molecules self-assembled by non-covalent interactions, wherein the π-conjugated molecules are phthalocyanine derivative molecules or diketopyrrolopyrrole derivative molecules. There is also provided a method of preparing the nanofibrous filter. 1. A nanofibrous filter comprising a substrate and self-assembled nanofibers deposited on the substrate , the self-assembled nanofibers comprising π-conjugated molecules self-assembled by non-covalent interactions , wherein the π-conjugated molecules are phthalocyanine derivative molecules or diketopyrrolopyrrole derivative molecules.2. The nanofibrous filter according to claim 1 , wherein the non-covalent interactions comprise π-π stacking claim 1 , intermolecular hydrogen bonding claim 1 , or a combination thereof.4. The nanofibrous filter according to claim 3 , wherein the Compound I is formed by cyclotetramerization of 4 claim 3 ,4″-bis(hydroxymethyl)-[1 claim 3 ,1′:2′ claim 3 ,1″-terphenyl]-4′ claim 3 ,5′-dicarbonitrile in 1-pentanol.6. The nanofibrous filter according to claim 1 , wherein the nanofibers have an average diameter of 100-300 nm.7. The nanofibrous filter according to claim 1 , wherein the nanofibrous filter has a filtration efficiency of ≥80% for PM 2.5 particles and ≥85% for PM 10 particles.8. The nanofibrous filter according to claim 1 , wherein the pressure drop across the filter is ≤400 Pa.9. A method of preparing the nanofibrous filter of claim 1 , wherein the method comprises:obtaining π-conjugated molecules, wherein the π-conjugated molecules are phthalocyanine derivative molecules or diketopyrrolopyrrole derivative molecules;dissolving the π-conjugated molecules in an organic solvent to form a solution comprising self-assembled nanofibers; anddepositing the solution on a surface of a substrate to form the nanofibrous filter.10. ...

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23-01-2020 дата публикации

SPECIFICALLY meso-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PHOTODYNAMIC THERAPY

Номер: US20200022955A1
Принадлежит:

Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, opthamological or urological disorders are provided as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso-substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT-efficacy. In other embodiments the nucleophilic substitution on pentafluorophenyl-substituted tetrapyrroles is used to obtain compounds with a high PDT-efficacy. In another embodiment substituents are identified that via their steric and/or electronic influence direct the dihydroxylation or reduction with diimine so that one isomer is favored. Another embodiment consists of formulating the desired tetrapyrrole photosensitizer into a pharmaceutical formulation to be injected into the body avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems. 2. The compound according to claim 1 , wherein X is O or NH claim 1 , and Ris CH(CHOH) claim 1 , CH—CH(OH)—CHOH claim 1 , or CH(OH)—CH(OH)—CH.3. A pharmaceutical composition comprising a compound according to or a pharmaceutically acceptable derivative thereof as an active ingredient.4. The pharmaceutical composition ...

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23-01-2020 дата публикации

RADIOPHARMACEUTICAL COMPLEXES

Номер: US20200024234A1
Принадлежит:

The invention provides compounds such as chelating agents useful in chelating metal ions, particularly radionuclides, to provide metal ion complexes. The invention also provides methods of using the compounds and complexes of the invention, such as in therapeutic and diagnostic applications. 183.-. (Canceled)85. The complex of claim 84 , wherein said radionuclide is thorium claim 84 , optionally thorium-227 or thorium-232.86. The complex of claim 84 , wherein each Rand Rare H.87. The complex of claim 84 , wherein Ris H or C claim 84 , C claim 84 , C claim 84 , C claim 84 , Cor Calkyl.88. The complex of claim 84 , wherein Ris methyl.89. The complex of claim 84 , wherein Ris selected from C claim 84 , C claim 84 , C claim 84 , C claim 84 , Cor Calkyl.90. The complex of claim 84 , wherein L claim 84 , L claim 84 , Land Lare independently selected from C claim 84 , C claim 84 , C claim 84 , C claim 84 , Cor Calkyl.91. The complex of claim 84 , wherein said Lis selected from substituted alkyl claim 84 , substituted heteroalkyl claim 84 , substituted aryl claim 84 , and substituted heteroaryl.92. The complex of claim 84 , wherein said X is a targeting moiety.93. The complex of claim 92 , wherein said targeting moiety is an antibody.94. The complex of claim 91 , wherein said antibody is a full-length antibody or an antibody fragment.95. The complex of claim 84 , wherein said X is a reactive functional group selected from the group consisting of: N-hydroxysuccinimide (NHS) esters claim 84 , sulfo-NHS esters claim 84 , maleimides and isothiocyanates.96. The complex of claim 84 , wherein said Ris Cor Calkyl.97. The complex of claim 84 , wherein said L claim 84 , L claim 84 , Land Lare independently selected from substituted or unsubstituted ethyl.98. The complex of claim 84 , wherein each said Z is O. This application is a Continuation of U.S. application Ser. No. 15/978,881 filed May 14, 2018, which is a Continuation of Ser. No. 12/977,957, filed Dec. 23, 2010, which claims ...

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31-01-2019 дата публикации

SYNTHESIS OF A 1,2,5,6-NAPHTHALENEDIIMIDE MONOMER

Номер: US20190031671A1
Автор: Nielsen Laura, Woody Kathy
Принадлежит: Phillips 66 Company

A method comprising converting 2,6-naphthalene diol to produce 2. The method of claim 1 , wherein the conversion does not contain cyanide containing reagents.5. The method of claim 4 , wherein the method occurs at temperatures less than 250° C.6. The method of claim 4 , wherein the conversion does not contain cyanide containing reagents.8. The method of claim 7 , wherein the method occurs at temperatures less than 250° C.9. The method of claim 7 , wherein the conversion does not contain cyanide.11. The method of claim 10 , wherein the method occurs at temperatures less than 250° C.12. The method of claim 10 , wherein the conversion does not contain cyanide containing reagents. This application is a non-provisional application which claims the benefit of and priority to U.S. Provisional Application Ser. No. 62/538,386 filed Jul. 28, 2017, entitled “Synthesis of a 1,2,5,6-Naphthalenediimide Monomer”, which is hereby incorporated by reference in its entirety.None.This invention relates to high performance wide-bandgap polymers for organic photovoltaics.Solar energy using photovoltaics requires active semiconducting materials to convert light into electricity. Currently, solar cells based on silicon are the dominating technology due to their high-power conversion efficiency. Recently, solar cells based on organic materials showed interesting features, especially on the potential of low cost in materials and processing.Organic photovoltaic cells have many potential advantages when compared to traditional silicon-based devices. Organic photovoltaic cells are light weight, economical in the materials used, and can be deposited on low cost substrates, such as flexible plastic foils. However, organic photovoltaic devices typically have relatively low power conversion efficiency (the ratio of incident photons to energy generated). This is, in part, thought to be due to the morphology of the active layer. The charge carriers generated must migrate to their respective ...

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31-01-2019 дата публикации

NOVEL 5-HT2CR AGONIST ANALOGS

Номер: US20190031672A1
Принадлежит:

The invention relates to the novel analogs of selective 5HTR agonist WAY163909, the preparation, and the use thereof. 4. The compound of claim 1 , wherein Ris a N-protecting group selected from the group consisting of CBz and —(CO)R claim 1 , wherein Ris alkyl or aryl.8. The compound of claim 1 , wherein Ris a fluorophore selected from the group consisting of:Alkyne cyanine dye 718,Alkyne MegaStokes dye 608,Alkyne MegaStokes dye 673,Alkyne MegaStokes dye 735,Azide cyanine dye 728,Azide-fluor 488,Azide-fluor 545,Azide-PEG3-biotin conjugate,Biotin-PEG4-alkyne,Cy3-alkyne,Cy3-azide,Cy5-azide,DBCO-Cy3,DBCO-Cy5,Dibenzocyclooctyne-fluor 488,Fluor 488-Alkyne,Fluor 545-Alkyne, andNVOC2-Q-rhodamine-5-PEG3-azide.10. A method of inducing 5-HTR-mediated intracellular calcium (Ca) release comprising contacting a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , with one or more cells. This application claims the benefit of U.S. Provisional Appl. No. 62/538,344, filed Jul. 28, 2017. The content of the aforesaid application is relied upon and is incorporated by reference herein in its entirety.This invention was made with government support under NIH/NIDA Grants Nos. P20 DA 024157 and P50 DA 033935 awarded by the National Institutes of Health (NIH) and National Institute on Drug Abuse (NIDA). The government has certain rights in the invention.The field of the invention relates to novel analogs of selective 5HTR agonist WAY163909, their preparation, and use thereof.This background information is provided for the purpose of making information believed by the applicant to be of possible relevance to the present invention. No admission is necessarily intended, nor should it be construed, that any of the information disclosed herein constitutes prior art against the present invention.Serotonin (5-hydroxytryptamine, 5-HT) receptors are implicated in a wide variety of physiological functions in both the central and peripheral nervous systems.5-HTreceptors have ...

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31-01-2019 дата публикации

MACROCYCLIC COMPOUNDS AS TRK KINASE INHIBITORS

Номер: US20190031684A1
Принадлежит:

Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, R, R, R, R, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases. 1. (canceled)5. The method of claim 2 , wherein Y is F.6. The method of claim 2 , wherein Ris H.7. The method of claim 2 , wherein Ris hydrogen.8. The method of claim 2 , wherein Rand Rare each hydrogen.9. The method of claim 2 , wherein W is CH.10. The method of claim 2 , wherein m is 0.11. The method of claim 2 , wherein m is 1.13. The method of claim 2 , wherein the Trk kinase is selected from the group consisting of TrkA claim 2 , TrkB claim 2 , and TrkC.14. The method of claim 2 , wherein the cancerous tumor is selected from the group consisting of: neuroblastoma claim 2 , ovarian claim 2 , pancreatic claim 2 , colorectal claim 2 , prostate claim 2 , melanoma claim 2 , head and neck cancer claim 2 , gastric carcinoma claim 2 , lung carcinoma claim 2 , breast cancer claim 2 , glioblastoma claim 2 , medulloblastoma claim 2 , secratory breast cancer claim 2 , salivary gland cancer claim 2 , and papillary thyroid carcinoma.15. The method of claim 2 , wherein the cancerous tumor exhibits overexpression of a Trk kinase.16. The method of claim 2 , wherein the cancerous tumor exhibits activation of a Trk kinase.17. The method of claim 2 , wherein the cancerous tumor exhibits amplification of a Trk kinase.18. The method of claim 2 , wherein the cancerous tumor exhibits mutation of a Trk kinase. The present invention relates to novel compounds, to pharmaceutical compositions comprising the compounds, to processes for making the compounds and to the use of the compounds in therapy. More particularly, it relates to certain macrocyclic compounds which exhibit Trk family protein tyrosine kinase inhibition, and which are useful in the treatment of pain, cancer, inflammation, ...

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04-02-2021 дата публикации

Organic electroluminescent materials and devices

Номер: US20210032225A1
Принадлежит: Universal Display Corp

Provided are novel organic molecules containing fused indole and benzimidazole moieties, or their boron containing analogs. Also provided are OLEDs and related consumer products that utilize these compounds containing the fused indole and benzimidazole moieties.

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04-02-2021 дата публикации

ANTIMICROBIAL AND ANTICANCER CATIONIC PHTHALOCYANINE COMPOUNDS

Номер: US20210032261A1
Автор: WIGHT Paul
Принадлежит:

Substituted phthalocyanines for the generation of singlet oxygen in which one or more of the substituents bear a cationically charged N-alkylated pyridine. 4. A compound according to claim 1 , wherein the compound absorbs electromagnetic radiation at a wavelength from 600 to 800 nm.5. An antimicrobial surface comprising the compound according to .6. The antimicrobial surface according to claim 5 , wherein the compound is contained in a polymer claim 5 , metal or textile comprised by the surface.7. A surface according to claim 6 , wherein the surface is an elastomer or nitrile latex surface.8. A nitrile glove comprising the compound according to .9. A method of manufacturing a nitrile glove according to claim 8 , wherein the method comprises dissolving the compound in an aqueous coagulant and then dipping in a nitrile dispersion.10. A nitrile glove obtainable by the method according to .11. A compound according to for use in a therapeutic method of treatment of a human or animal body.12. The compound according to claim 11 , wherein the method is for treatment of a skin or subcutaneous cancer.13. A process for removing stains on a surface claim 1 , wherein the method comprises contacting a stained surface with an aqueous composition of the compound according to claim 1 , and exposing the surface to light claim 1 , preferably sunlight claim 1 , during or after the contacting step.14. A process according to claim 13 , wherein the surface is of any of fabric claim 13 , cement claim 13 , stone claim 13 , brick or glass. The present invention relates to an antimicrobial compound, antimicrobial surfaces comprising the compound, medical gloves comprising the compound, and medical and non-medical uses of the compound.Singlet oxygen generators are known to destroy microorganisms, Singlet oxygen has a greater energy than ground-state, triplet oxygen. The singlet and triplet states of oxygen are distinguished by the singlet state having two electrons of anti-parallel spins and ...

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08-02-2018 дата публикации

SPECIFICALLY meso-SUBSTITUTED PORPHYRINS AND CHLORINS FOR PHOTODYNAMIC THERAPY

Номер: US20180036284A1
Принадлежит:

Biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PDT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, opthamological or urological disorders are provided as well as providing methods to obtain them in pharmaceutical quality. One embodiment consists of a method to synthesize a porphyrin with a defined arrangement of meso-substituents and then converting this porphyrin system to a chlorin system by dihydroxylation or reduction, and if more than one isomer is formed separate them by chromatography either on normal or reversed phase silica. In another embodiment the substituents on the porphyrin are selected to direct the reduction or dihydroxylation to the chlorin so that a certain isomer is selectively formed. Another embodiment is to provide amphiphilic compounds with a higher membrane affinity and increased PDT-efficacy. In other embodiments the nucleophilic substitution on pentafluorophenyl-substituted tetrapyrroles is used to obtain compounds with a high PDT-efficacy. In another embodiment substituents are identified that via their steric and/or electronic influence direct the dihydroxylation or reduction with diimine so that one isomer is favored. Another embodiment consists of formulating the desired tetrapyrrole photosensitizer into a pharmaceutical formulation to be injected into the body avoiding undesirable effects like solubility problems or delayed pharmacokinetics of the tetrapyrrole systems. 175-. (canceled)77. The tetrapyrrolic compound according to claim 76 , based on the formulas 1 claim 76 , 2 claim 76 , 3 claim 76 , 4 claim 76 , 5 or 6 claim 76 , wherein Ris CH(CHOH) claim 76 , CH—CH(OH)—CHOH claim 76 , or CH(OH)—CH(OH)—CH; and/or Ris a substituent either in the meta- or para-position of the phenyl ring ...

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31-01-2019 дата публикации

Organic electroluminescent materials and devices

Номер: US20190036059A1
Автор: Bin Ma, Zhiqiang Ji
Принадлежит: Universal Display Corp

Circulene compounds of Formula I or Formula II, and organic light emitting devices (OLED) that include an organic layer disposed between an anode and a cathode, wherein the organic layer includes a compound of Formula I or Formula II. In addition, the OLED can be incorporated into one or more of a consumer product, for example, an electronic component module, and/or a lighting panel.

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08-02-2018 дата публикации

PHTHALOCYANINE-BASED COMPLEX COMPOUND

Номер: US20180037740A1
Принадлежит: DEXERIALS CORPORATION

A phthalocyanine-based complex compound is represented by general formula (1) shown below, 2. The phthalocyanine-based complex compound of having an E1% 1 cm value of at least 300 at a wavelength of maximum absorption in a visible light region.3. The phthalocyanine-based complex compound of claim 1 , whereinthe phthalocyanine-based complex compound dissolves in water or ethylene glycol in an amount of at least 0.01 mass %.4. The phthalocyanine-based complex compound of claim 1 , whereinthe phthalocyanine-based complex compound dissolves as molecules or disperses as particles having a number average particle diameter of no greater than 3 μm in water or ethylene glycol.5. The phthalocyanine-based complex compound of claim 1 , whereinthe phthalocyanine-based complex compound forms a solution having a hydrogen ion concentration (pH) of 4 to 10 when dissolved in water in an amount of 0.1 mass %.6. A method of producing a phthalocyanine-based complex compound claim 1 , for use in producing the phthalocyanine-based complex compound of claim 1 , comprisingpreparing a raw material solution in which a raw material including a phthalocyanine derivative moiety is dissolved in a solvent and a compound solution in which a compound including a moiety that adsorbs onto a metal is dissolved in a solvent, and mixing the raw material solution and the compound solution to precipitate a phthalocyanine-based complex compound.7. The phthalocyanine-based complex compound of claim 2 , whereinthe phthalocyanine-based complex compound dissolves in water or ethylene glycol in an amount of at least 0.01 mass %.8. The phthalocyanine-based complex compound of claim 2 , whereinthe phthalocyanine-based complex compound dissolves as molecules or disperses as particles having a number average particle diameter of no greater than 3 μm in water or ethylene glycol.9. The phthalocyanine-based complex compound of claim 2 , whereinthe phthalocyanine-based complex compound forms a solution having a hydrogen ...

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30-01-2020 дата публикации

PHOTOELECTRIC CONVERSION ELEMENT, OPTICAL SENSOR, AND IMAGING ELEMENT

Номер: US20200035932A1
Принадлежит: FUJIFILM Corporation

The present invention provides a photoelectric conversion element exhibiting excellent responsiveness, and excellent dark current characteristics in a case of high-speed photoelectric conversion film formation, an optical sensor, an imaging element, and a compound which include the photoelectric conversion element. The photoelectric conversion element of the present invention includes a conductive film, a photoelectric conversion film, and a transparent conductive film, in this order, in which the photoelectric conversion film contains a compound represented by Formula (1), and an n-type organic semiconductor having a predetermined structure. 2. The photoelectric conversion element according to claim 1 ,wherein the n-type organic semiconductor contains the compound represented by Formula (3).3. The photoelectric conversion element according to claim 1 ,wherein M represents Zn, Cu, Co, Ni, Pt, Pd, Mg, or Ca.4. The photoelectric conversion element according to claim 1 ,wherein M represents Zn.5. The photoelectric conversion element according to claim 1 ,wherein a maximum absorption wavelength of the compound represented by Formula (1) is within a range of 480 to 600 nm.6. The photoelectric conversion element according to claim 1 ,wherein in a case where the photoelectric conversion film has a maximum absorption wavelength within a range of 480 to 600 nm and light absorbance of the photoelectric conversion film in the maximum absorption wavelength is 1, each of relative values of the light absorbance of the photoelectric conversion film at 400 nm and at 650 nm is 0.10 or less.7. The photoelectric conversion element according to claim 1 ,wherein a molecular weight of the compound represented by Formula (1) is 400 to 1200.8. The photoelectric conversion element according to claim 1 ,wherein the photoelectric conversion film has a bulk hetero structure.9. The photoelectric conversion element according to claim 1 , further comprising one or more interlayers between the ...

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18-02-2021 дата публикации

Pyrimidine-based antiproliferative agents

Номер: US20210047328A1
Принадлежит: G1 Therapeutics Inc

This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

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18-02-2021 дата публикации

PHOTODYNAMIC CATIONIC PORPHYRIN COMPOSITES

Номер: US20210047477A1
Автор: Elshaer Mohammed R.
Принадлежит:

A photodynamic composite including a porphyrin having four quaternized nitrogens, wherein the porphyrin is covalently bonded to a polymer containing reactive amines covalently bonded to a solid-state support is claimed. A method for sanitizing contaminated water is claimed including exposing the contaminated water to the photodynamic composite, in the presence of light and oxygen, wherein, a sufficient quantity of singlet oxygen and super oxide anions is provided by the chemical reaction of the light and the photosensitizer to destroy the pollutants or pathogens present in the contaminated water and to oxidize organic contaminants into carbon dioxide and water; thereby rendering the water potable. 1. A photodynamic composite comprising:a porphyrin having four quaternized nitrogens, wherein the porphyrin is covalently bonded to a polymer containing reactive amines covalently bonded to a solid-state support.3. The photodynamic composite according to claim 1 , wherein the polymer containing reactive amines is polyethylenimine (PEI) or modified PEI.4. The photodynamic composite according to claim 3 , wherein the polymer containing reactive amines is modified PEI and the PEI is modified by acetylation claim 3 , acylation claim 3 , alkylation claim 3 , quaternization claim 3 , hydroxylation claim 3 , succinylation claim 3 , pegylation claim 3 , or combinations thereof.5. The photodynamic composite according to claim 1 , wherein the solid-state support is a metal oxide claim 1 , inert material claim 1 , or water insoluble salt.6. The photodynamic composite according to claim 5 , wherein the solid-state support is a metal oxide selected from the group consisting of ZnO claim 5 , MgO claim 5 , AlO claim 5 , SiO claim 5 , TiO claim 5 , and ZrO.7. The photodynamic composite according to claim 5 , wherein the solid-state support is SiO claim 5 , TiO claim 5 , activated carbon claim 5 , graphite claim 5 , graphene oxide claim 5 , charcoal claim 5 , clay claim 5 , zeolites claim ...

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01-05-2014 дата публикации

DISPIROPYRROLIDINE DERIVATIVES

Номер: US20140121196A1
Принадлежит: Daiichi Sankyo Company, Limited

A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R, R, R, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification. 6. A method of inhibiting Mdm2 comprising administering a compound according to or a salt thereof to a subject in need thereof.7. A method of inhibiting Mdm2 ubiquitin ligase comprising administering a compound according to or a salt thereof to a subject in need thereof.8. A method of inhibiting p53-Mdm2 binding comprising administering a compound according to or a salt thereof to a subject in need thereof.9. A method of inhibiting suppression of p53 transcription activity comprising administering a compound according to or a salt thereof to a subject in need thereof.10. A method of inhibiting p53 degradation comprising administering a compound according to or a salt thereof to a subject in need thereof.16. A method of inhibiting Mdm2 comprising administering a compound according to or a salt thereof to a subject in need thereof.17. A method of inhibiting Mdm2 ubiquitin ligase comprising administering a compound according to or a salt thereof to a subject in need thereof.18. A method of inhibiting p53-Mdm2 binding comprising administering a compound according to or a salt thereof to a subject in need thereof.19. A method of inhibiting suppression of p53 transcription activity comprising administering a compound according to or a salt thereof to a subject in need thereof.20. A method of inhibiting p53 degradation comprising administering a compound according to or a salt thereof to a subject in need thereof.26. A method of inhibiting Mdm2 comprising administering a compound ...

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01-05-2014 дата публикации

SUBSTITUTED METHYLFORMYL REAGENTS AND METHOD OF USING SAME TO MODIFY PHYSICOCHEMICAL AND/OR PHARMACOKINETIC PROPERTIES OF COMPOUNDS

Номер: US20140121367A1
Принадлежит:

The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent. 127.-. (canceled)29. A method according to claim 28 , wherein Y═R; or alternatively Y═Rand compound 1 claim 28 , is selected from the group comprising:i. chloromethyl isopropyl carbonate;ii. benzyl chloromethyl carbonate;iii. chloromethyl morpholinomethyl carbonate;iv. chloromethyl isobutyl carbonate;v. chloromethylmethyl carbonate;vi. (S)-sec-butyl chloromethyl carbonate;vii. (R)-sec-butyl chloromethyl carbonate;viii. chloromethyl((3S,5R)-3,5-dimethylmorpholino)methyl carbonate;ix. chloromethyl 2-methylcyclopropyl carbonate;x. chloromethyl2-methoxyethyl carbonate;xi. chloromethyl propyl carbonate;xii. chloromethyl cyclobutyl carbonate;xiii. chloromethyl cyclopropyl carbonate;xiv. chloromethyl 2,2-dimethylcyclobutyl carbonate;xv. chloromethyl cyclopentyl carbonate;xvi. chloromethyl oxetan-3-yl carbonate;xvii. (S)-chloromethyl tetrahydrofuran-3-yl carbonate;xviii. chloromethyl cyclohexylmethyl carbonate;xix. chloromethyl 3-methoxycyclohexyl carbonate;xx. (R)-chloromethyl tetrahydrofuran-3-yl carbonate;xxi. chloromethyl ethoxymethyl carbonate;xxii. chloromethyl oxepan-4-yl carbonate;xxiii. (1R,2S,4S)-bicyclo[2.2.1]heptan-2-yl chloromethyl carbonate;xxiv. chloromethyl 2,3-dihydro-1H-inden-1-yl carbonate;xxv. benzyl chloromethyl carbonate;xxvi. (S)-chloromethyl 1-phenylethyl carbonate;xxvii. chloromethyl cyclohexyl carbonate;xxviii. chloromethyl isobutyl carbonate;xxix. chloromethyl 4-methylcyclohexyl carbonate;xxx. chloromethyl 2-(methylthio)ethyl carbonate;xxxi. chloromethyl 3-methylcyclohexyl carbonate;xxxii. chloromethylpentan-2-yl carbonate;xxxiii. chloromethyl neopentyl carbonate;xxxiv. methyl 1-((chloromethoxy)carbonyloxy) ...

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19-02-2015 дата публикации

High-purity large-scale preparation of stannsoporfin

Номер: US20150051184A1
Принадлежит: Infacare Pharmaceutical Corp

Large scale (bulk) compositions comprising high-purity stannsoporfin are disclosed, as well as methods of synthesizing such compositions.

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23-02-2017 дата публикации

GA-NAPHTHALOCYANINE CHROMOPHORES WITH SHORT CHAIN ALKOXY AXIAL SUBSTITUENTS

Номер: US20170051166A1
Принадлежит: BASF SE

The present invention relates to specific Ga-naphthalocyanine chromophores with short chain alkoxy axial substituents, their use as almost colourless IR absorbers, for optical filter applications; especially for plasma display panels, or for laser welding of plastics. The compounds may be used in compositions for inks, paints and plastics, especially in a wide variety of printing systems and are particularly well-suited for security applications. 2. A compound according to wherein R is C-Calkyl.3. A compound according to claim 1 , wherein R is ethyl claim 1 , propyl or butyl.46-. (canceled)7. A printing ink formulation claim 1 , comprising: at least one compound of the formula (I) according to .8. A printing ink formulation according to claim 7 , further comprising:a polymeric binder,a solvent,optionally at least one colorant, andoptionally at least one further additive.9. The printing ink formulation according to claim 7 , comprisinga) 0.0001 to 25% by weight of at least one compound of the formula (I),b) 5 to 74% by weight of at least one polymeric binder,c) 1 to 94.9999% by weight of at least one solvent,d) 0 to 25% by weight of at least one colorant, ande) 0 to 25% by weight of at least one further additive,wherein the sum of components a) to e) adds up to 100%.10. A process for the manufacture of a security document claim 7 , the process comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'printing on a substrate a printing ink formulation according to .'}11. A security document claim 7 , comprising:a substrate; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one compound of the formula (I) according to .'}12. A security document according to claim 11 , which is obtained by a process comprising:printing a printing ink formulation that comprises the at least one compound of the formula (I) onto a substrate13. The security document according to claim 11 , which is in the form of a bank note claim 11 , a passport claim 11 , a check claim 11 ...

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25-02-2021 дата публикации

Photoelectric conversion element and imaging device

Номер: US20210057649A1
Принадлежит: Sony Corp, Sony Semiconductor Solutions Corp

A photoelectric conversion element according to an embodiment of the present disclosure includes: a first electrode; a second electrode disposed to be opposed to the first electrode; and a photoelectric conversion layer disposed to be opposed to and between the first electrode and the second electrode, in which the photoelectric conversion layer includes a first compound represented by the general formula and a second compound having a skeleton different from the first compound.

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10-03-2022 дата публикации

COMPOUNDS FOR ELECTRONIC DEVICES

Номер: US20220073531A1
Принадлежит:

The present invention relates to condensed N-heteroaromatic compounds, to processes for preparing these compounds, and to electronic devices containing said compounds. 2. The electronic device as claimed in claim 1 , wherein Tis —(C═O)(NAr)—.3. The electronic device as claimed in claim 1 , wherein Aris the same or different at each instance and is selected from the group consisting of phenyl claim 1 , biphenyl claim 1 , terphenyl claim 1 , quaterphenyl claim 1 , triphenylene claim 1 , naphthyl claim 1 , fluorenyl claim 1 , dibenzofuranyl claim 1 , dibenzothiophenyl claim 1 , carbazolyl claim 1 , benzofuranyl claim 1 , benzothiophenyl claim 1 , triazinyl claim 1 , pyrimidyl claim 1 , pyridyl claim 1 , quinazoline claim 1 , quinoxaline and quinoline claim 1 , where the groups mentioned may each be substituted by one or more Rradicals.4. The electronic device as claimed in claim 1 , wherein Zis the same or different at each instance and is selected from C and CR.5. The electronic device as claimed in claim 1 , wherein k is 0.6. The electronic device as claimed in claim 1 , wherein{'sup': ['1', '4'], '#text': 'Ris the same or different at each instance and is selected from H, aromatic ring systems having 6 to 40 aromatic ring atoms, and heteroaromatic ring systems having 5 to 40 aromatic ring atoms; where the aromatic ring systems and the heteroaromatic ring systems are each substituted by Rradicals; and'}{'sup': ['2', '4'], '#text': 'Ris the same or different at each instance and is selected from H, aromatic ring systems having 6 to 40 aromatic ring atoms, and heteroaromatic ring systems having 5 to 40 aromatic ring atoms; where the aromatic ring systems and the heteroaromatic ring systems are each substituted by Rradicals; and'}{'sup': ['3', '4'], '#text': 'Ris the same or different at each instance and is selected from H, aromatic ring systems having 6 to 40 aromatic ring atoms, and heteroaromatic ring systems having 5 to 40 aromatic ring atoms; where the aromatic ...

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03-03-2016 дата публикации

Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates

Номер: US20160060274A1
Принадлежит: Shionogi and Co Ltd, ViiV Healthcare Co

A synthesis approach providing an early ring attachment via a bromination to compound l-l yielding compound II-Il, whereby a final product such as AA can be synthesized. In particular, the 2,4-difluorophenyl-containing sidechain is attached before creation of the additional ring Q.

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21-02-2019 дата публикации

COMPOUNDS FOR TREATING DISORDERS MEDIATED BY METABOTROPIC GLUTAMATE RECEPTOR 5, AND METHODS OF USE THEREOF

Номер: US20190055204A1
Принадлежит:

Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein. 3. The compound of claim 1 , wherein Lis —C≡C— or —HC═CH—.4. The compound of claim 1 , wherein either Q and X or Q and G are both N.5. The compound of claim 2 , wherein Ris aryl.7. The compound of claim 2 , wherein Ris heteroaryl.9. The compound of claim 2 , wherein Ris cycloalkyl.11. The compound of claim 2 , wherein Ris lower alkyl.12. The compound of claim 11 , wherein Ris selected from methyl claim 11 , propyl claim 11 , cyclopropylmethyl claim 11 , isobutyl and sec-butyl.13. The compound of claim 2 , wherein Ris lower alkenyl.14. The compound of claim 11 , wherein Ris CH═CH—.15. The compound of claim 2 , wherein Ris heteroalkyl.17. The compound of claim 2 , wherein Ris cycloalkyl.19. The compound of claim 2 , wherein Ris heterocycloalkyl-lower alkyl.21. The compound of claim 2 , wherein Ris heteroarylalkyl.23. The compound of claim 2 , wherein Ris —C(O)OR.24. The compound of claim 23 , wherein Ris methyl.25. The compound of claim 2 , wherein Ris —CO—NR.26. The compound of claim 25 , wherein Ris ethyl.27. The compound of claim 2 , wherein Ris heterocycloalkyl.29. The compound of claim 2 , wherein Ris cycloalkyl.31. The compound of claim 2 , wherein Ris heteroalkyl.33. The compound of claim 2 , wherein Ris lower alkyl.34. The compound of claim 33 , wherein Ris isobutyl or sec-butyl.35. The compound of claim 2 , wherein Rand R claim 2 , together ...

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02-03-2017 дата публикации

CDK Inhibitors

Номер: US20170057971A1
Принадлежит: G1 THERAPEUTICS, INC.

Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. 12. The compound of claim 1 , wherein x is 1 or 2.13. The compound of claim 1 , wherein y is 0 claim 1 , 1 claim 1 , or 2.14. The compound of claim 1 , wherein Ris -(alkylene)-heterocyclo claim 1 , -(alkylene)-NRR claim 1 , -(alkylene)-C(O)—NRR; -(alkylene)-C(O)—O-alkyl claim 1 , or -(alkylene)-O—R.15. The compound of claim 1 , wherein Ris -(alkylene)-heterocyclo or -(alkylene)-heteroaryl.16. The compound of claim 1 , wherein Ris -(alkylene)-heterocyclo.17. The compound of claim 16 , wherein m is 0.18. The compound of claim 1 , wherein Ris substituted with one Rgroup.19. The compound of claim 1 , wherein Ris selected from alkyl claim 1 , cycloalkyl claim 1 , and heterocycle.20. The compound of claim 1 , wherein Ris absent.21. The compound of claim 1 , wherein both of X are N.22. The compound of claim 1 , wherein one X is N and the other is CH.23. The compound of claim 22 , wherein x is 1 or 2.24. The compound of claim 23 , wherein x is 2.25. The compound of claim 24 , wherein y is 0 claim 24 , 1 claim 24 , or 2.26. The compound of claim 25 , wherein Ris -(alkylene)-heterocyclo.27. The compound of claim 26 , wherein m is 0.28. The compound of claim 27 , wherein Ris substituted with one Rgroup.29. The compound of claim 28 , wherein Ris selected from alkyl claim 28 , cycloalkyl claim 28 , and heterocycle.30. The compound of claim 29 , wherein Ris absent.31. The compound of claim 30 , wherein y is 2.32. The compound of claim 31 , wherein two Rs on the same ring atom together with the ring atom to which they are attached form a 3-8-membered cycle.33. The compound of claim 32 , wherein the 3-8-membered cycle is a 6-membered cycle.35. The compound of claim 34 , wherein x is 1 or 2.36. The compound of claim 34 , wherein y is 0 claim 34 , 1 claim 34 , or 2.37. The compound of claim 34 , wherein Ris absent.38. The compound of claim 34 , wherein one X is N and the ...

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02-03-2017 дата публикации

LACTAM KINASE INHIBITORS

Номер: US20170057972A1
Принадлежит: G1 THERAPEUTICS, INC.

Compounds useful as kinase inhibitors are provided herein, as well as salts, pharmaceutical compositions, methods of medical treatment and methods of synthesis thereof. 2. The compound of claim 1 , wherein yy is 1.3. The compound of claim 1 , wherein yy is 2.4. The compound of claim 3 , wherein two Rs on adjacent ring atoms or on the same ring atom together with the ring atom(s) to which they are attached form a 3-8-membered cycle.5. The compound of claim 3 , wherein two Rs on the same ring atom together with the ring atom to which they are attached form a 3-8 membered cycle.6. The compound of claim 5 , wherein the 3-8 membered cycle is a 5 membered cycle.7. The compound of claim 5 , wherein the 3-8 membered cycle is a 6 membered cycle.9. The compound of claim 8 , wherein yy is 1.10. The compound of claim 8 , wherein yy is 2.11. The compound of claim 10 , wherein two Rs on adjacent ring atoms or on the same ring atom together with the ring atom(s) to which they are attached form a 3-8-membered cycle.12. The compound of claim 10 , wherein two Rs on the same ring atom together with the ring atom to which they are attached form a 3-8 membered cycle.13. The compound of claim 1 , wherein ZZ is selected from the group consisting of —CH— and —CHCH—.14. The compound of claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , iso-propyl claim 1 , cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , and cyclohexyl.15. The compound of claim 1 , wherein Ris selected from the group consisting of cis 4-hydroxycyclohexylamino claim 1 , trans 4-hydroxycyclohexylamino claim 1 , cyclohexylamino claim 1 , cyclopentylamino and straight chain C-Calkylamino.16. The compound of claim 15 , wherein yy is 2.17. The compound of claim 16 , wherein two Rs on adjacent ring atoms or on the same ring atom together with the ring atom(s) to which they are attached form a 3-8-membered cycle.18. The compound of claim 16 , wherein Ris ...

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20-02-2020 дата публикации

NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS FOR ORGANIC LIGHT EMITTING DEVICES

Номер: US20200058881A1
Принадлежит: IDEMITSU KOSAN CO., LTD.

A compound of formula (I), a material for an organic electroluminescence device comprising at least one compound of formula (I); an organic electroluminescence device which comprises an organic thin film layer between a cathode and an anode, wherein the organic thin film layer comprises one or more layers and comprises a light emitting layer, and at least one layer of the organic thin film layer comprises at least one compound of formula (I); an electronic equipment comprising the organic electroluminescence device; and a process for preparing the compound of formula (I). 6: The compound according to claim 1 , wherein:L is a single bond, a substituted or unsubstituted aromatic hydrocarbon group having 6 to 30 ring carbon atoms, or a substituted or unsubstituted heterocyclic group having to 30 ring atoms;l is 1 or 2, in the case that l is 2, L is the same or different in each occurrence; and{'sup': '1', 'Bis H; CN; a substituted or unsubstituted aromatic hydrocarbon group having 6 to 30 ring carbon atoms; or a substituted or unsubstituted heterocyclic group having 5 to 30 ring atoms.'}8: The compound according to claim 1 , wherein L is selected from the group consisting of a substituted or unsubstituted phenylene group claim 1 , a substituted or unsubstituted biphenylene group claim 1 , a substituted or unsubstituted terphenylene group.9: The compound according to claim 1 , wherein:L represents substituted or unsubstituted aryl group having 6 to 30 carbon atoms; and{'sup': '1', 'Brepresents CN.'}10: A material for an organic electroluminescence device claim 1 , the material comprising at least one compound according to .11: An organic electroluminescence device claim 1 , comprising an organic thin film layer between a cathode and an anode claim 1 , wherein:the organic thin film layer comprises one or more layers including a light emitting layer; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one layer of the organic thin film layer comprises at least ...

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08-03-2018 дата публикации

Compounds, compositions and methods useful for cholesterol mobilization

Номер: US20180064718A1
Принадлежит: Cerenis Therapeutics Holding SA

The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.

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09-03-2017 дата публикации

PORPHYRIN MOLECULAR CATALYSTS FOR SELECTIVE ELECTROCHEMICAL REDUCTION OF CO2 INTO CO

Номер: US20170067168A1
Принадлежит:

The present invention relates to porphyrins of formula (I): wherein Rto R, R to R, X, X′ Y and Y′ are as described in claim . The invention also relates to complexes of said porphyrins with transition metals, in particular iron, preferably as Fe(III) or Fe(0) complex, and salts thereof, use thereof as catalysts for the selective electrochemical reduction of COinto CO, electrochemical cells comprising said complexes, and a method for selectively reducing electrochemically COinto CO using said complexes. 2. The porphyrin of , wherein at least one of X , X{hacek over ( )} , Y or Y{hacek over ( )} represents CF , CNRRR , or NR , or at least one of R , R , R , R , R , R , R , R represents F or NRRR , with R , Rand Rare as described in , and preferably R , Rand Rrepresent a methyl group.4. The porphyrin of any of to , wherein X and X{hacek over ( )} independently represent CH or CF , preferably CF.6. The porphyrin of any of to , at least one of Y , Y{hacek over ( )} , X and X{hacek over ( )} is CNRRRor at least one of R , R , R , R , R , R , R , and R is NRRR , with R , Rand Ras described in any of to .8. A complex of a porphyrin according to any of to with a transition metal such as iron , preferably a Fe(III) or Fe(0) complex , and salts thereof.9. Use of the complex of as catalyst for the electrochemical reduction of COinto CO claim 8 , advantageously in combination with at least one proton donor selected from the group consisting of water (HO) claim 8 , trifluoroethanol claim 8 , phenol and acetic acid claim 8 , even more advantageously HO or phenol.11. The electrochemical cell of claim 8 , wherein the complex of is in a concentration claim 8 , in the electrolyte solution claim 8 , of between 0.0005 and 0.01 M claim 8 , preferably 0.001 M.12. The electrochemical cell of or claim 8 , wherein the electrolyte further comprises a proton donor selected from the group consisting of water (HO) claim 8 , trifluoroethanol claim 8 , phenol and acetic acid claim 8 , even more ...

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15-03-2018 дата публикации

DE NOVO SYNTHESIS OF BACTERIOCHLORINS

Номер: US20180072746A1
Принадлежит:

A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II 1. (canceled)3. The method of claim 2 , wherein Ris not cycloalkyl.4. The method of claim 2 , wherein Ris not methyl.5. The method of claim 2 , wherein Ris not H.6. The method of claim 2 , wherein Ris not H.7. The method of claim 2 , wherein Ris not methyl.8. The method of claim 2 , wherein M is present and is selected from the group consisting of Pd claim 2 , Pt claim 2 , Mg claim 2 , Zn claim 2 , Al claim 2 , Ga claim 2 , In claim 2 , Sn claim 2 , Cu claim 2 , Ni claim 2 , and Au.9. The method of claim 2 , wherein at least one of Rthrough Ris a linking group.10. The method of claim 2 , wherein at least one of R claim 2 , R claim 2 , or Ris a linking group.11. The method of claim 2 , wherein the compound is coupled to a hydrophilic group.12. The method of claim 2 , wherein the compound is coupled to a hydrophilic group at at least one of said R claim 2 , R claim 2 , or Rpositions.13. The method of claim 2 , wherein the compound is coupled to a targeting agent.14. The method of claim 2 , wherein the compound is coupled to a targeting agent at at least one of said R claim 2 , R claim 2 , or Rpositions.15. The method of claim 2 , wherein the compound is to an antibody.16. The method of claim 2 , wherein the compound is coupled to an antibody at at least one of said R claim 2 , R claim 2 , or Rpositions.17. The method of claim 2 , wherein the compound is coupled to a protein or peptide.18. The method of claim 2 , wherein the compound is coupled to a protein or peptide at at least one of said R claim 2 , R claim 2 , or Rpositions.19. The method of claim 2 , wherein the compound is coupled to a nucleic acid.20. The method of claim 2 , wherein the compound is coupled to a nucleic acid at at least one of said R claim 2 , R claim 2 , or Rpositions. This application claims priority to and is a divisional of U.S. patent application Ser. No. 14/162,201, filed Jan. 23, 2014, now ...

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24-03-2022 дата публикации

Photosensitizer compounds, methods of manufacture and application to plants

Номер: US20220089615A1
Принадлежит: Suncor Energy Inc

Provided herein are compounds of general Formula I:or agriculturally acceptable salts thereof. The compounds of Formula I can be used to improve the health of plants. For example, the compounds of Formula I can be used to inhibit a microbial pathogen of a plant, or to increase resistance of a plant to one or more abiotic stress. Methods of manufacturing the compounds of general Formula I, as well as synthetic intermediates are also provided.

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05-03-2020 дата публикации

TEXAPHYRIN-PT(IV) CONJUGATES AND COMPOSITIONS FOR USE IN OVERCOMING PLATINUM RESISTANCE

Номер: US20200069698A1
Принадлежит:

The present disclosure relates platinum(IV) and texaphyrin linked conjugates and compositions comprising a texaphyrin and a platinum(IV) agent. The present disclosure also provides pharmaceutical compositions of the conjugates and compositions. Also, provided herein are methods of using the instant compounds in the treatment of cancer such as a platinum resistant cancer. 3. (canceled)7. The compound of claim 6 , wherein o or p are 2 claim 6 , 3 claim 6 , or 4.812.-. (canceled)13. The compound of claim 2 , wherein X claim 2 , X claim 2 , X claim 2 , X claim 2 , or Xare alkylor substituted alkyl.14. (canceled)1620.-. (canceled)21. The compound of claim 15 , wherein Ais alkanediylor substituted alkanediyl.2224.-. (canceled)25. The compound of claim 15 , wherein Ris carboxy.26. The compound of claim 15 , wherein Lor Lare halide.2731.-. (canceled)32. The compound of claim 15 , wherein Land Lare taken together and are alkyldicarboxylate.33. (canceled)34. The compound of claim 15 , wherein Lis amino.35. The compound of claim 15 , wherein Land Lare taken together and are diaminocycloalkane.3649.-. (canceled)50. The compound of claim 2 , wherein M is gadolinium.51. (canceled)52. The compound of claim 2 , wherein Land Lare acetate or nitrate.5354.-. (canceled)55. A pharmaceutical composition comprising:(A) a pharmaceutically acceptable carrier; and{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, '(B) a compound of .'}5687.-. (canceled)88. A method of treating a disease in a patient comprising administering to the patient in need thereof a therapeutically effective amount of{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'a compound or pharmaceutical composition of .'}8991.-. (canceled)92. The method of claim 88 , wherein the cancer is ovarian cancer claim 88 , testicular cancer claim 88 , or bladder cancer.93144.-. (canceled)145. A compound comprising:(A) a texaphyrin; and(B) a high oxidation state metal chemotherapeutic complex, wherein the high oxidation state metal is ...

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16-03-2017 дата публикации

FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS

Номер: US20170073349A1
Автор: Guo Yunhang, Wang Zhiwei
Принадлежит: Beigene, Ltd.

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby. 6. The compound of wherein R4 is N-containing C1-C8 alkyl claim 5 , N-containing C3-C8 cycloalkyl and phenyl claim 5 , each optionally substituted.7. The compound of wherein R4 is methylamine claim 5 , aniline claim 5 , azetidine claim 5 , pyrrolidine claim 5 , piperidine claim 5 , azacycloheptenyl claim 5 , each N-substituted with a moietie selected from benzyl claim 5 , acyl claim 5 , acryloyl claim 5 , substituted-acryloyl claim 5 , propiolyl claim 5 , and substituted-propiolyl.9. The compound of wherein Ris 1-acryloylpiperidin-4-yl (compound 27) or 1-(but-2-ynoyl)piperidin-4-yl (compound 176).10. A compound of the examples herein claim 5 , or of Table I claim 5 , II or III claim 5 , stereoisomers thereof claim 5 , and pharmaceutically acceptable salts thereof.11. The compound of any of to claim 5 , having a Btk-inhibiting activity corresponding to an IC50 of 10 uM or less in a Btk Kinase Assay.12. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any of to in unit dosage form and one or more pharmaceutically acceptable carriers.13. A combination comprising a therapeutically effective amount of a compound of any of to and a different agent therapeutically active against an autoimmune and/or inflammatory disease or cancer.14. A method of treating a disease associated with undesirable Btk activity claim 5 , which comprises administering to a person in need thereof an effective amount of a compound of any of - claim 5 , an N-oxide thereof or a prodrug thereof claim 5 , wherein the disease is an allergic disease claim 5 , an autoimmune disease claim 5 , an inflammatory disease claim 5 , or ...

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19-03-2015 дата публикации

LITHIUM REAGENT COMPOSITION, AND METHOD AND DEVICE FOR DETERMINING LITHIUM ION AMOUNT USING SAME

Номер: US20150079687A1
Принадлежит: METALLOGENICS CO., LTD.

[Problem] To provide to a reagent composition used in quantitative measurement of lithium in aqueous solutions such as biological specimens and environmental liquid samples by a simple colorimeter or ultraviolet-visible light spectrophotometer immediately, a reagent composition which permits to measure a concentration of lithium by visual observation, and a method and apparatus for measuring lithium ion by using the reagent. 2. (canceled)3. The lithium reagent composition of claim 1 , in which said pH modifier is selected from acids including hydrochloric acid claim 1 , nitric acid claim 1 , acetic acid claim 1 , phosphoric acid claim 1 , citric acid claim 1 , carbonic acid claim 1 , bicarbonic acid claim 1 , oxalic acid and their salts claim 1 , alkali medicine including sodium hydroxide claim 1 , potassium hydroxide claim 1 , ammonia and their salts.4. The lithium reagent composition of claim 1 , in which said pH modifier is pH buffer.5. The lithium reagent composition of claim 4 , in which said pH buffer is selected from citric acid claim 4 , carbonic acid claim 4 , bicarbonic acid claim 4 , phosphoric acid claim 4 , succinic acid claim 4 , phthalic acid claim 4 , ammonium chloride claim 4 , sodium hydroxide claim 4 , potassium hydroxide claim 4 , MES as Good buffer claim 4 , Bis-Tris claim 4 , ADA claim 4 , PIPES claim 4 , ACES claim 4 , MOPSO claim 4 , BES claim 4 , MOPS claim 4 , TES claim 4 , HEPES claim 4 , DIPSO claim 4 , TAPSO claim 4 , POPSO claim 4 , HEPPSO claim 4 , EPPS claim 4 , Tricine claim 4 , Bicine claim 4 , TAPS claim 4 , CHES claim 4 , CAPSO claim 4 , CAPS and their salts6. The lithium reagent composition of claim 4 , in which the reagent composition develops a color reaction for lithium in a range from pH 5 to pH 11.7. The lithium reagent composition of claim 1 , including further a stabilizer.8. The lithium reagent composition of claim 1 , in which said stabilizer is nonionic surfactant and/or anionic surfactant.9. The lithium reagent ...

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18-03-2021 дата публикации

TRANSIENT PROTECTION OF HEMATOPOIETIC STEM AND PROGENITOR CELLS AGAINST IONIZING RADIATION

Номер: US20210077498A1
Принадлежит: G1 THERAPEUTICS, INC.

This invention is in the area of improved compounds and methods for transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC), from the damage associated with ionizing radiation (IR) exposure using selective radioprotectants. 2. The method of claim 1 , wherein the cancer is selected from small cell lung cancer claim 1 , triple-negative breast cancer claim 1 , human papilloma virus (HPV)-positive head and neck cancer claim 1 , retinoblastoma claim 1 , retinoblastoma protein (Rb)-negative bladder cancer claim 1 , retinoblastoma protein (Rb)-negative prostate cancer claim 1 , osteosarcoma claim 1 , or cervical cancer.3. The method of claim 2 , wherein the cancer is small cell lung cancer.4. The method of claim 2 , wherein the cancer is triple-negative breast cancer.5. The method of claim 2 , wherein the cancer is human papilloma virus (HPV)-positive head and neck cancer.6. The method of claim 2 , wherein the cancer is retinoblastoma.7. The method of claim 2 , wherein the cancer is retinoblastoma protein (Rb)-negative bladder cancer.8. The method of claim 2 , wherein the cancer is retinoblastoma protein (Rb)-negative prostate cancer.9. The method of claim 2 , wherein the cancer is osteosarcoma.10. The method of claim 2 , wherein the cancer is cervical cancer.11. The method of claim 2 , wherein the CDK4/6 inhibitor is administered to the subject prior to exposure to the ionizing radiation such that the compound reaches peak serum levels during exposure to the ionizing radiation. This application is a continuation of U.S. patent application Ser. No. 16/268,317, filed on Feb. 5, 2019, which is a continuation of U.S. patent application Ser. No. 15/839,685, filed on Dec. 12, 2017, which is a continuation of U.S. patent application Ser. No. 15/232,366, filed on Aug. 9, 2016; which is a continuation of U.S. patent application Ser. No. 14/926,147, filed on Oct. 29, 2015; which is a continuation of U.S. patent application Ser. No. 14/ ...

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05-03-2020 дата публикации

METALLOPORPHYRIN 2D-SHEETS FOR EFFICIENT PHOTO- AND ELECTRO- CATALYTIC SPLITTING OF WATER

Номер: US20200071458A1
Принадлежит:

The present invention disclosed a novel squaraine linked metalloporphyrin based 2D-sheet polymer catalyst of formula (I), process for preparation thereof and use of said catalyst for efficient photo- and electro-catalytic splitting of water. 2. The compound as claimed in claim 1 , wherein said compound of formula (I) is monometallic 2D-sheet polymer.3. The compound as claimed in claim 1 , wherein said compound of formula (I) is bimetallic 2D-sheet polymer.6. The compound as claimed in claim 1 , wherein said compound of formula (I) is used for generation of oxygen and hydrogen by splitting water photo catalytically and electro catalytically.7. A one step process for the synthesis of novel squaraine linked metalloporphyrin based 2D-sheet polymer compound with basic unit of formula (I) as claimed in claim 1 , wherein said process comprises heating the reaction mixture of metal porphyrin and acid compound in suitable solvent at temperature in the range of 120 to 125° C. for the period of 2.5 to 3 days.8. The process as claimed in claim 7 , wherein said metal porphyrin is selected from the group consisting of zinc porphyrin claim 7 , cobalt porphyrin claim 7 , nickel porphyrin claim 7 , iron porphyrin claim 7 , manganese porphyrin claim 7 , molybdenum porphyrin or mixture thereof.10. The process as claimed in claim 7 , wherein said acid compound is squaric acid.11. The process as claimed in claim 7 , wherein said solvent is selected from the group consisting of n-butanol claim 7 , toluene or mixture thereof. The present invention relates to a novel metalloporphyrin based 2D-sheet polymer catalyst. More particularly, the present invention relates to a novel squaraine linked metalloporphyrin based 2D-sheet polymer catalyst of formula (I), process for preparation thereof and use of said catalyst for efficient photo- and electro-catalytic splitting of water.Water splitting driven by sunlight or renewable resource-derived electricity has attracted great attention for ...

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18-03-2021 дата публикации

MDM2 Inhibitors

Номер: US20210079007A1
Автор: Heng Li, Lei Yin, Zhenglin Yao
Принадлежит: Gan & Lee Pharmaceuticals

A compound capable of being used as a tumor inhibitor, a preparation method therefor, and application thereof. The compound has a structure represented by general formula I; a stereoisomer, an enantiomer, a raceme, a cis/trans isomer, a tautomer, and an isotopic variant of the compound are comprised; the compound can be used separately or in combination with other drugs for treating tumors or inflammatory diseases, or for treating other disorders or diseases mediated by the activity of MDM2 and/or MDM4, and shows prominent curative activity. 117.-. (canceled)19. The compound according to claim 18 , wherein Ris a 5- or 6-membered aromatic ring or aromatic heterocycle which is unsubstituted or substituted with 1 to 3 substituents independently selected from H claim 18 , (C-C)alkyl claim 18 , —O—(C-C)alkyl claim 18 , —S—(C-C)alkyl claim 18 , halogen claim 18 , haloalkyl claim 18 , haloalkoxy claim 18 , —CN claim 18 , —C(O)NRR claim 18 , —C(O)-morpholin-4-yl claim 18 , hydroxy-azetidin-1-yl-carbonyl claim 18 , —CHNRR claim 18 , —CHNR—C(O)R claim 18 , methyl-imidazolyl- claim 18 , —CHC(O)NRR claim 18 , —CHC(O)OH claim 18 , —C(O)OH claim 18 , —CHC(O)O—(C-C)alkyl claim 18 , —N(R)—C(O)—(C-C)alkyl claim 18 , —NRR claim 18 , —C(O)O—(C-C)alkyl claim 18 , —CHCN claim 18 , azetidin-1-yl and azetidin-1-yl substituted with one or more —OH claim 18 , or with —CHand —OH; wherein the alkyl is optionally substituted with 0 to 3 substituents independently selected from alkoxy having 1 to 4 carbon atoms claim 18 , hydroxyl claim 18 , sulfhydryl claim 18 , halogen claim 18 , —C(O)OH claim 18 , —C(O)O—(C-C)alkyl claim 18 , —C(O)NRR claim 18 , —NRRand methanesulfonyl; and{'sub': 5', '1', '6', '1', '6', '1', '6', '9', '10', '2', '9', '10', '2', '9', '10', '2', '2', '9', '10', '2', '2', '1', '4', '9', '1', '4', '9', '10', '3', '3', '1', '4', '9', '10', '9', '10, 'Ris a 5- or 6-membered aromatic ring or aromatic heterocycle which is unsubstituted or substituted by 1 to 3 substituents ...

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24-03-2016 дата публикации

Fused heterocyclic compounds as protein kinase inhibitors

Номер: US20160083392A1
Автор: Guo Yunhang, Wang Zhiwei
Принадлежит: Beigene, Ltd.

The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby. 6. The compound of wherein R4 is N-containing C1-C8 alkyl claim 5 , N-containing C3-C8 cycloalkyl and phenyl claim 5 , each optionally substituted.7. The compound of wherein R4 is methylamine claim 5 , aniline claim 5 , azetidine claim 5 , pyrrolidine claim 5 , piperidine claim 5 , azacycloheptenyl claim 5 , each N-substituted with a moiety selected from benzyl claim 5 , acyl claim 5 , acryloyl claim 5 , substituted-acryloyl claim 5 , propiolyl claim 5 , and substituted-propiolyl.1015-. (canceled)19. A compound of the examples herein claim 5 , or of Table I claim 5 , II or III claim 5 , or a stereoisomer thereof claim 5 , or a pharmaceutically acceptable salt thereof.20. The compound of claim 1 , having a Btk-inhibiting activity corresponding to an IC50 of 10 uM or less in a Btk Kinase Assay.21. A pharmaceutical composition comprising a therapeutically effective amount of a compound of in unit dosage form and one or more pharmaceutically acceptable carriers.22. A combination comprising a therapeutically effective amount of a compound of and a different agent therapeutically active against an autoimmune and/or inflammatory disease or cancer.23. A method of treating a disease associated with undesirable Btk activity claim 1 , which comprises administering to a person in need thereof an effective amount of a compound of claim 1 , an N-oxide thereof or a prodrug thereof claim 1 , wherein the disease is an allergic disease claim 1 , an autoimmune disease claim 1 , an inflammatory disease claim 1 , or cancer.24. The method of wherein the disease is a B-cell proliferative disorder claim 23 , selected from chronic lymphocytic lymphoma ...

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24-03-2016 дата публикации

TRICYCLIC GUANIDINE DERIVATIVE

Номер: US20160083400A1
Принадлежит:

Disclosed are compounds useful as inhibitors of Phosphodiesterase 1 (PDE1), compositions thereof, and methods of using the same. 4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein the compound is a compound of formula II-a II-b claim 3 , II-k claim 3 , II-l claim 3 , or II-m.5. The compound of or a pharmaceutically acceptable salt thereof wherein Ris(i) a hydrogen, or(ii) a phenyl (said group being optionally substituted with the same or different 1 to 4 group(s) selected from(a) a halogen,{'sub': '1-6', '(b) a Calkyl (said group being optionally substituted with the same or different 1 to 3 halogen), and'}{'sub': '1-6', '(c) a Calkoxy (said group being optionally substituted with the same or different 1 to 3 halogen)).'}6. The compound of claim 1 , wherein Lis a covalent bond.7. The compound of claim 1 , wherein Lis methylene.8. The compound of claim 1 , wherein Ris a hydrogen or Cy.9. The compound of claim 1 , wherein Ris a Ccycloaliphatic; a phenyl; a 5-6 membered monocyclic heteroaryl claim 1 , or a 4-8 membered saturated or partially unsaturated monocyclic heterocyclyl claim 1 , each of said group is optionally substituted with the same or different 1 to 4 group(s) selected from the group consisting of(a) a halogen,{'sub': '1-6', '(b) a Calkyl (said group being optionally substituted with the same or different 1 to 3 halogen),'}{'sub': '1-6', '(c) a Calkoxy (said group being optionally substituted with the same or different 1 to 3 halogen),'}(d) a hydroxy, and(e) a cyano.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris(i) a hydrogen,(ii) a halogen,{'sub': '1-6', '(iii) a Caliphatic (said group being optionally substituted with the same or different 1 to 4 group(s) selected from'}(a) a halogen,{'sub': '1-6', '(b) a Calkoxy (said group being optionally substituted with the same or different 1 to 3 halogen),'}(c) a hydroxy, and(d) an oxo), or(iv) 4-8 membered saturated or ...

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12-03-2020 дата публикации

EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) TARGETED PHOTOSENSITIZERS

Номер: US20200078461A1
Принадлежит:

Compounds including a tetrapyrrolic or reduced tetrapyrrolic group/moiety and an epidermal growth factor receptor targeting group are disclosed. For example, a compound includes a tetrapyrrolic or reduced tetrapyrrolic group or moiety, a linker moiety, an epidermal growth factor receptor targeting group, and, optionally, a PET-active functional group. Uses of the compounds, for example, methods of treating a hyperproliferative tissue in an individual, and kits including one or more of the compounds are also provided. 1. A compound having the following structure:PS-L-E,wherein PS is a tetrapyrrolic or reduced tetrapyrrolic photosensitizer group or moiety,L is a linker moiety, andE is an erlotinib group or a group derived from an erlotinib analog.9. The compound of claim 1 , wherein the compound further comprises a functional group (FG) that is PET active.12. A composition comprising one or more compound of .13. The composition of claim 12 , wherein the composition further comprises a pharmaceutically acceptable carrier.14. A method for detecting the presence of a hyperproliferative tissue in an individual comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering to the individual an effective quantity of one or more compound of ; and'}imaging the individual or a portion thereof to detect the presence or absence of a hyperproliferative tissue in an individual.15. The method of claim 14 , wherein the imaging is fluorescence imaging and/or PET imaging.16. The method of claim 14 , wherein the method further comprises:exposing the individual with light of a wavelength to kill or impair the hyperproliferative tissue.17. A method of photodynamic therapy for treating hyperproliferative tissue in an individual claim 14 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) administering to the individual the compound of , and'}(ii) irradiating the individual with light of a wavelength to activate the compound, whereby the hyperproliferative ...

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31-03-2022 дата публикации

SPIRO-LACTAM AND BIS-SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF

Номер: US20220098211A1
Автор: Khan M. Amin
Принадлежит:

Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. 152-. (canceled)54. The compound of claim 53 , wherein Ris —C-Calkyl.55. The compound of claim 53 , wherein Ris methyl claim 53 , isobutyl claim 53 , or —CH-phenyl.61. A pharmaceutical composition comprising the compound of claim 53 , and a pharmaceutically acceptable excipient.62. A pharmaceutical composition comprising the compound of claim 59 , and a pharmaceutically acceptable excipient.63. A pharmaceutical composition comprising the compound of claim 60 , and a pharmaceutically acceptable excipient.64. A method of lessening or reducing one or more symptoms of depression claim 53 , Alzheimer's disease claim 53 , attention deficit disorder claim 53 , schizophrenia claim 53 , or anxiety claim 53 , in a patient in need thereof claim 53 , the method comprising administering to the patient a therapeutically effective amount of the compound of .65. A method of lessening or reducing one or more symptoms of a migraine claim 53 , neuropathic pain claim 53 , or traumatic brain injury in a patient in need thereof claim 53 , the method comprising administering to the patient a therapeutically effective amount of the compound of .66. A method of lessening or reducing one or more symptoms of depression claim 59 , Alzheimer's disease claim 59 , attention deficit disorder claim 59 , schizophrenia claim 59 , or anxiety claim 59 , in a patient in need thereof claim 59 , the method comprising administering to the patient a therapeutically effective amount of the compound of .67. A method of lessening or reducing one or more symptoms of a migraine claim 59 , neuropathic pain claim 59 , or traumatic brain injury in a patient in need thereof claim ...

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29-03-2018 дата публикации

Composition and Method for Detecting Hypoxia

Номер: US20180085475A1
Принадлежит: VANDERBILT UNIVERSITY

A compound and method for detecting hypoxic cells and tissue are provided. The compound includes a probe selected from the group consisting of a hypoxia sensitive 2-nitroimidazole containing fluorescence imaging probe, a hypoxia sensitive reversible ON-OFF fluorescence imaging probe, a hypoxia sensitive azo-based fluorescence imaging probe, and combinations thereof. The method includes contacting the cells or tissue with the probe of any one of claims 1 - 13 and detecting fluorescent intensity of the cell or tissue, wherein increased fluorescent intensity indicates that the cells or tissue is hypoxic. Also provided are a method of synthesizing the compound and a method for synthesizing a therapeutic agent including the compound.

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29-03-2018 дата публикации

FULLERENE DERIVATIVE AND LUBRICANT

Номер: US20180086771A1
Принадлежит:

A fullerene derivative, used as a lubricant, includes, in a molecule: a fullerene backbone; and n pyrrolidine rings each being condensed to the fullerene backbone, each of the pyrrolidine rings including one aryl group including a group including m perfluoropolyether chains, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5. 1. A fullerene derivative comprising , in a molecule:a fullerene backbone; andn pyrrolidine rings each being condensed to the fullerene backbone,each of the pyrrolidine rings including one aryl group including a group including m perfluoropolyether chains, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5.3. The fullerene derivative according to claim 2 , wherein the “R” is an alkyl group or an aryl group whose carbon number is less than or equal to 24.4. The fullerene derivative according to claim 1 , wherein the fullerene backbone is C.5. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains includes at least a partial structure selected from —(CF)O— in which “x” is an integer from 1 to 5.6. The fullerene derivative according to claim 5 , wherein the group including perfluoropolyether chains includes a partial structure expressed by —(CFCFO)(CFO)— in which each of “y” and “z” is an integer from 1 to 50.7. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains is configured only by a perfluoropolyether structure.8. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains is a straight-chain.9. A lubricant comprising the fullerene derivative according to .10. The lubricant according to claim 9 , further comprising a perfluoropolyether chemical compound that does not include a fullerene backbone. This application is a continuation-in-part application filed under 35 U.S.C. 111(a) claiming the benefit under 35 U.S.C. 120 and 365(c) of PCT International Application No. PCT ...

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21-03-2019 дата публикации

COMPOUND INCLUDING NITROGEN AND ORGANIC ELECTROLUMINESCENCE DEVICE INCLUDING THE SAME

Номер: US20190084992A1
Автор: SAKAMOTO Naoya
Принадлежит:

Provided are a compound including nitrogen, represented by Formula 1, and an organic electroluminescence device including the same. In Formula 1, Ato Aare each independently CRor N. The organic electroluminescence device may include a first electrode, a second electrode which is opposite to the first electrode, and a plurality of organic layers disposed between the first electrode and the second electrode, wherein the plurality of organic layers include an emission layer, and at least one organic layer among the organic layers includes the compound including nitrogen. 2. The compound including nitrogen of claim 1 , wherein the number of nitrogen atoms (N) among Ato Ais 0 claim 1 , 1 claim 1 , or 2.3. The compound including nitrogen of claim 1 , wherein Aand Aare the same.4. The compound including nitrogen of claim 1 , wherein at least one of Ato Ais CRor N claim 1 , and{'sub': '3', 'Ris a fluorine atom, a cyano group, a substituted or unsubstituted arylamino group, a substituted or unsubstituted triphenylsilyl group, a substituted or unsubstituted diphenylphosphine oxide group, a substituted or unsubstituted alkyl group having 1 to 5 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyridine group, a substituted or unsubstituted triazine group, a substituted or unsubstituted carbazole group, a substituted or unsubstituted dibenzofuran group, or a substituted or unsubstituted dibenzothiophene group.'}5. The compound including nitrogen of claim 1 , wherein Aand Aare nitrogen atoms (N).6. The compound including nitrogen of claim 1 , wherein Aand Aare each independently CR claim 1 , and{'sub': '3', 'Ris a hydrogen atom, a substituted or unsubstituted alkyl group having 1 to 5 carbon atoms, or a substituted or unsubstituted phenyl group.'}7. The compound including nitrogen of claim 1 , wherein a and b are 0.8. The compound including nitrogen of claim 1 , wherein at least one of a or b is 1 or more claim 1 , and{'sub': 1', '2, 'at ...

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02-04-2015 дата публикации

SYNTHETIC VOACANGINE

Номер: US20150094466A1
Автор: Moriarty Robert M.
Принадлежит: DEMERX, INC.

Synthetic voacangine, including in substantially enantiomerically enriched forms, and derivatives thereof are provided. 1. Synthetic voacangine or a salt thereof , which contains less than 1 ppt C.2. The synthetic voacangine of that is present as a racemic mixture claim 1 , or is present in a substantially enantiomerically enriched form.3. (+) Voacangine claim 1 , (+) ibogaine claim 1 , or (+) noribogaine claim 1 , which is present in a substantially enantiomerically enriched form. This application is a divisional application and claims priority to U.S. patent application Ser. No. 13/749,594 filed on Jan. 24, 2013, which claims the benefit under 35 U.S.C. 119(e) of U.S. Provisional Application Ser. Nos. 61/590,741 filed Jan. 25, 2012, and 61/591,200 filed Jan. 26, 2012, each of which is hereby incorporated by reference into this application in its entirety.This invention relates to processes for preparing synthetic voacangine, and salts thereof, intermediates thereto, and to compositions comprising the same.Voacangine is an alkaloid found in plants such as and , and has the following structure:It is an iboga alkaloid which can serve as a precursor for the semi-synthesis of ibogaine:which can be demethylated to provide noribogaine:Noribogaine and its pharmaceutically acceptable salts have recently received significant attention as a non-addictive alkaloid useful in treating drug dependency (U.S. Pat. No. 6,348,456) and as a potent analgesic (U.S. Pat. No. 7,220,737). Voacangine is a potential source for making noribogaine. However, plant derived voacangine is problematic because of its limited and unpredictable supply. Furthermore, plant derived voacangine may contain unwanted alkaloids which may find their way to the noribogaine produced from the plant derived voacangine.Accordingly, there is an ongoing need to provide synthetic voacangine, which can be intermediates in the synthesis noribogaine, preferably in an enantiomerically enriched form.This invention ...

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05-05-2022 дата публикации

SUPRAMOLECULAR PHOTOPROTECTION OF A PHOTOSENSITIZER

Номер: US20220133692A1
Принадлежит:

Disclosed herein are compositions comprising a water-soluble host-guest complex formed from a host receptor and a guest photosensitizer for the photoprotection of the photosensitizer. Also disclosed are methods of using the composition for generating reactive oxygen species, inhibiting the proliferation or killing of a cell, treating a subject with a cell proliferative disease or disorder.

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05-05-2022 дата публикации

HYDROXYPHEOPHORBIDE COMPOUNDS, METHODS AND USES THEREOF

Номер: US20220135580A1
Принадлежит:

The present disclosure relates to hydroxypheophorbide compounds with bioactivities towards obesity and obesity-related co-morbidities. Therefore, the present subject-matter discloses hydroxypheophorbide compounds or a pharmaceutically acceptable salt, hydrate, solvate, N-oxide, stereoisomer, diastereoisomer, enantiomer or atropisomer, polymorph for use in medicine comprising formula (I), wherein R is CHand n is an entire number multiple of 5. The compound of the present disclosure may be use in the therapy or treatment of obesity, an obesity-related disorder, an obesity related disease, being overweight, an obesity-related condition, or lipid obesity disorders.

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19-03-2020 дата публикации

TETRAPHENYLPORPHYRIN DERIVATIVE

Номер: US20200087315A1
Принадлежит: KYOTO UNIVERSITY

Provided is a ligand capable of stably bonding together interfaces composed of different types of nanoparticles, different bulk interfaces, or an interface composed of nanoparticles and a bulk interface. A tetraphenylporphyrin derivative represented by the following formula (I): 2. The tetraphenylporphyrin derivative according to claim 1 , wherein in formulas (II) to (VII) claim 1 ,X and Y are substituents having the ability to coordinate different surfaces;a first surface for which X has coordination ability and a second surface for which Y has coordination ability are different from each other; andeach of the first surface and the second surface is a surface comprising one or more members selected from the group consisting of metal nanoparticles, semiconductor nanoparticles, and organic matter nanoparticles, or a bulk interface comprising one or more members selected from the group consisting of metals, semiconductors, and organic matter.3. The tetraphenylporphyrin derivative according to claim 1 , wherein in formula (I) claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare all the same claim 1 , and are each any one of formulas (II) to (VII).5. The tetraphenylporphyrin derivative according to claim 2 , wherein in formulas (II) to (VII) claim 2 , X and Y are each any of formulas (E) and (F) claim 2 , formulas (F) and (K) claim 2 , formula (F) and an amino group claim 2 , an amino group and a catechol group claim 2 , formula (E) and an amino group claim 2 , formula (P) and a nitro group claim 2 , formula (P) and an amino group claim 2 , formulas (Q) and (R) claim 2 , formula (S) and an amino group claim 2 , formulas (S) and (U) claim 2 , and formulas (S) and (V).6. A complex comprising the tetraphenylporphyrin derivative according to and one or more nanoparticles selected from the group consisting of metals claim 1 , semiconductors claim 1 , and organic matter.7. A photoelectric conversion element having the complex according to . The present invention relates to ...

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01-04-2021 дата публикации

TROPOMYOSIN RECEPTOR KINASE INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: US20210094953A1
Принадлежит:

Disclosed in the present invention are a pyrazolo [1,5-a]pyrimidine derivative having a structure of formula (I), a pharmaceutical composition comprising the compound of formula (I), and use of the compound in the preparation of a medicament for preventing or treating diseases associated with tropomyosin receptor kinases, in particular for preventing or treating cancers associated with tropomyosin receptor kinases. Each substituent in formula (I) has the same definition as that in the description. 3. The compound according to claim 2 , wherein:{'sup': 1', '6', '8', '7', '7', '7', '7, 'sub': 1', '8', '3', '8', '2', '8', '2', '8', '2', '1', '8', '3', '8', '1', '8, 'Ris selected from H, C-Calkyl, C-Ccycloalkyl, C-Calkenyl or C-Calkynyl, and optionally further substituted with one or more substituents selected from deuterium, halogen, hydroxyl, cyano, —NRR, —NRCOR, —COR, —SOR, —SOR, C-Calkyl, C-Ccycloalkyl, C-Calkoxy, or a 4-10 membered heterocyclic group;'}{'sup': 2', '4', '6', '8', '6', '5', '5', '5', '5, 'sub': 1', '8', '3', '8', '2', '8', '2', '8', '2', '1', '8', '3', '8', '1', '8, 'Rand Rare each independently selected from H, C-Calkyl, C-Ccycloalkyl, C-Calkenyl or C-Calkynyl, and optionally further substituted with one or more substituents selected from deuterium, halogen, hydroxyl, cyano, —NRR, —NRCOR, —COR, —SOR, —SOR, C-Calkyl, C-Ccycloalkyl, C-Calkoxy, or a 4-10 membered heterocyclic group;'}{'sup': 5', '7', '8, 'sub': 1', '8', '3', '8, 'Rand Rare each independently selected from H, C-Calkyl, C-Ccycloalkyl, or —NR;'}{'sup': 6', '8, 'sub': 1', '8', '3', '8, 'Rand Rare each independently selected from H, C-Calkyl, or C-Ccycloalkyl;'}{'sup': 1', '2', '4, 'sub': 3', '8, 'alternatively, any two of R, Rand Rcan independently form a C-Ccycloalkyl group or a 4-10 membered heterocyclic group;'}{'sup': '3', 'Ris halogen; and'}X is selected from CH or N.4. The compound according to claim 3 , wherein:{'sup': 1', '6', '8', '6', '7', '7', '7', '7, 'sub': 1', '8', '3', '8', ...

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09-04-2015 дата публикации

CRYSTALLINE FORM OF 2-((1'-N-HEXYLOXY) ETHYL)-2-DIVINYL-PYROPHEOPHORBIDE-A AND METHOD FOR PREPARING THEREOF

Номер: US20150099873A1
Принадлежит:

The present invention provides a crystalline form of HPPH (2-((1′-n-hexyloxy)ethyl)-2-divinyl-pyropheophorbide-a). The crystalline form can be characterized by an X-ray powder diffraction (XRD) pattern and differential scanning calorimeter (DSC) pattern. The present invention also provides a method for preparing the crystalline form of HPPH. 1. A crystalline form of 2-((1′-n-hexyloxy)ethyl)-2-divinyl-pyropheophorbide-a (HPPH) , characterized by at least one of the features set forth below:(1) characteristic peaks (2θ) of X-ray powder diffraction (XRD) pattern being: (2θ±0.2) 5.46°, 6.02°, 13.95°, 18.03°, 24.01°, 24.49°;(2) characteristic peak of differential scanning calorimeter (DSC) pattern: a characteristic endothermic peak being at 201.2° C.2. The crystalline form of HPPH according to claim 1 , characterized in that the crystalline form further has XRD pattern characteristic peaks (2θ) are: (2θ±0.2) 8.66° claim 1 , 10.92° claim 1 , 12.04° claim 1 , 12.44° claim 1 , 13.31° claim 1 , 15.0° claim 1 , 16.90° claim 1 , 18.94° claim 1 , 25.03° claim 1 , 26.28° claim 1 , 27.21°.4. The crystalline form of HPPH according to claim 1 , characterized by the crystalline form having an XRD pattern as shown in .5. The crystalline form of HPPH according to claim 1 , characterized by the crystalline form having an DSC pattern as shown in .6. A method for preparing the crystalline form of HPPH according to claim 1 , comprising the four steps set forth below:1) dissolving an HPPH sample into a polar organic solvent;2) adding a non-polar solvent to promote crystallization of the HPPH;3) mixing well, then continuously stirring or sitting undisturbed for 1 to 8 hrs;4) isolating the obtained crystal,wherein, the polar solvent is selected from ethyl acetate or acetone, the non-polar solvent is selected from n-hexane or n-heptane, and the step of isolating comprises filtering and drying.7. The method according to claim 6 , characterized by the polar solvent being acetone.8. The method ...

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28-03-2019 дата публикации

ENERGETIC COMPOUNDS AND COMPOSITIONS

Номер: US20190092895A1

Energetic nitrogen-rich monomers represented by the general Formula I: 2. The mixture of claim 1 , wherein at least one of said polymerizable group of said first monomer is capable of forming a linking moiety with at least one of said polymerizable group of said second monomer claim 1 , thereby forming said polymer.3. The mixture of claim 2 , wherein said second monomer is represented by Formula I.5. The mixture of claim 4 , wherein R1 is amino claim 4 , each of R2 claim 4 , R3 and R4 is H and said guanidine moiety is 1-aminoguanidine.11. The mixture of claim 1 , wherein said second monomer is represented by Formula X:{'br': None, 'sub': 8', '9, 'R-A-R\u2003\u2003Formula X;'}wherein:A is selected from the group consisting of C1-6 alkyl, cycloalkyl, heteroalicyclic, aryl and heteroaryl, andeach of R8 and R9 is independently a polymerizable group selected from the group consisting of azido, cyano, diazonium, ethynyl, hydrazine, hydroxyl, hydrazide, amine, ethanolamine, isocyanate, cyanate, amide, imidate, ester, carboxyl and azo.12. The mixture of claim 11 , wherein said second monomer is selected from the group consisting of 1 claim 11 ,6-diisocyanatohexane claim 11 , 1 claim 11 ,4-dicyanobutane (adiponitrile) and dimethyl adipimidate.14. The mixture of claim 13 , wherein m is 1 claim 13 , and each of R10 claim 13 , R11 claim 13 , R12 and R13 is independently and Calkyl.15. The mixture of claim 14 , wherein said silane is selected from the group consisting of dimethoxydimethylsilane and diethoxydimethylsilane.16. A polymer derived from the mixture of monomers of such that at least a portion of the backbone units of the polymer are derived from said first monomer and said second monomer.17. An article of manufacturing comprising the polymer of .18. The article of claim 17 , forming a part of a system selected from the group consisting of a fire extinguishing system claim 17 , a safety airbag claim 17 , an inflatable device claim 17 , a buoy claim 17 , a flotation ...

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06-04-2017 дата публикации

DERIVATIZED CORROLES AND METALLOCORROLES AND THEIR USE AS IMAGING AND THERAPEUTIC AGENTS

Номер: US20170096434A1
Принадлежит:

The present invention is directed to derivatized corroles, methods of making and using the same as imaging and therapeutic agents. In certain embodiments, the corroles are compounds having a Structure (I-H) and (I-M): 2. The compound of claim 1 , having a Formula (I-H) or (I-M).3. The compound of claim 1 , having a Formula (I-M) or (II-M) claim 1 , where M is Al claim 1 , Cr claim 1 , Co claim 1 , Fe claim 1 , Ga claim 1 , Mn claim 1 , Rh claim 1 , Ru claim 1 , or Sn having 0 claim 1 , 1 claim 1 , or 2 axial nitrogen donor ligands.4. The compound of claim 1 , having a Formula (I-M) or (II-M) claim 1 , where M is Co claim 1 , Cr claim 1 , Fe claim 1 , Ga claim 1 , Ir claim 1 , Mn claim 1 , Rh claim 1 , Ru claim 1 , or Sn having 0 claim 1 , 1 claim 1 , or 2 axial phosphine ligands.5. The compound of claim 1 , having a Formula (I-M) claim 1 , where M is Al or Ga claim 1 , optionally coordinated to one or more ligands.6. The compound of claim 1 , having a Formula (I-M) claim 1 , where M is Ga(III) having 0 claim 1 , 1 claim 1 , or 2 axial tertiary or aromatic amine ligands.7. The compound of claim 1 , having a Formula (I-M) claim 1 , where M is Ga(III) having 0 claim 1 , 1 claim 1 , or 2 axial pyridine ligands claim 1 , preferably one axial pyridine ligand.8. The compound of claim 1 , wherein one of R claim 1 , R claim 1 , R claim 1 , and Ris —N(H)—(CH)—Y.9. A pharmaceutical composition comprising a pharmaceutically acceptable inert ingredient and a compound of .10. The pharmaceutical composition of claim 9 , wherein the composition is in a form suitable for local or systemic administration.11. The pharmaceutical composition of claim 9 , having a Formula (I-M) claim 9 , where M is Al or Ga claim 9 , optionally coordinated to one or more ligands.12. The pharmaceutical composition of claim 9 , having a Formula (I-M) claim 9 , where M is Ga(III) having 0 claim 9 , 1 claim 9 , or 2 axial tertiary or aromatic amine ligands.13. The pharmaceutical composition of claim 9 , ...

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