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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 6594. Отображено 100.
07-06-2012 дата публикации

Rare-earth complex and uses thereof

Номер: US20120140439A1

The rare-earth complex of the present invention has high luminous efficiency, since it has a structure represented by the following general formula (I):

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23-08-2012 дата публикации

Photoelectric conversion device and solar cell using the same

Номер: US20120211082A1
Принадлежит: Mitsubishi Chemical Corp

There is provides a photoelectric conversion device material which can be used as an electrode buffer material for a solar cell or the like and can improve durability while maintaining the interaction with an electrode and mobility; a photoelectric conversion device using the photoelectric conversion device material; and a solar cell using the photoelectric conversion device. A photoelectric conversion device containing a buffer layer and an active layer, wherein the buffer layer contains a compound represented by the following general formula (I), the active layer contains an n-type semiconductor, and the n-type semiconductor is a compound having a solubility in toluene of 0.5% by weight or more at 25° C. and having an electron mobility of 1.0×10 −6 cm 2 /Vs or more.

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17-01-2013 дата публикации

Frustrated Lewis Pair Compositions

Номер: US20130018207A1
Принадлежит: Stephan Consulting Corp

A compound having the formula (I) where each of R 1 , R 2 , R 3 and R 4 is independently C 6 -C 18 aryl-, C 5 -C 8 cycloalkyl-, C 6 -C 18 aryl having at least one C 1 -C 20 alkyl substituent, C 5 -C 8 cycloalkyl having at least one C 1 -C 20 alkyl sυbstituent, C 4 -C 20 branched alkyl-, C 16 -C 20 linear alkyl-, RO—, —NRR′, —PRR′, —SR, fluoro substituted forms thereof, and perfluoro forms thereof: and R 5 is C 6 -C 18 aryl-, C 5 -C 8 cycloalkyl-, C 6 -C 18 aryl having at least one C 1 -C 20 alkyl substituent, C 5 -C 8 cycloalkyl having at least one C 1 -C 20 alkyl substituent, C 3 -C 20 branched alkyl-, C 2 -C 30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; where R and R′ are each independently C 6 -C 18 aryl-, C 5 -C 8 cycloalkyl-, C 6 -C 18 aryl having at least one C 1 -C 20 alkyl substituent, C 5 -C 8 cycloalkyl having at least one C 1 -C 20 alkyl substituent, C 4 -C 20 branched alkyl-, C 2 -C 30 linear alkyl-, fluoro substituted forms thereof, and perfluoro forms thereof; A is N, P, S, or O with the proviso that when A is S, R 2 is a nullity; and M is B, Al, Ga or In.

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28-03-2013 дата публикации

Phosphonium-based ionic liquids and their use in the capture of polluting gases

Номер: US20130078170A1
Принадлежит: UT Battelle LLC

An ionic liquid composition having the following chemical structural formula: wherein R 1 , R 2 , R 3 , and R 4 are independently selected from hydrocarbon groups containing at least 1 and up to 20 carbon atoms, and X − is a cyclic anion that possesses a negatively-charged group reactive with a gaseous electrophilic species, particularly carbon dioxide or sulfur dioxide. Methods for capturing a gaseous electrophilic species, such as CO 2 or SO 2 , by contacting the gaseous electrophilic species with an ionic liquid according to Formula (1) are also described.

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16-05-2013 дата публикации

HIGHLY EFFICIENT CARBAZOLE-BASED COMPOUND, AND ORGANIC ELECTROLUMINESCENCE DEVICE COMPRISING SAME

Номер: US20130119367A1

The present invention relates to a highly efficient carbazole-based compound and to an organic electroluminescence device including the same. According to the present invention, provided are a compound for an organic electroluminescence device and an organic electroluminescence device including the compound, in which a carbazole-based phosphine oxide compound, which is a compound intended for an organic electroluminescence device, is employed to overcome the problems of conventional compounds for organic electroluminescence devices, i.e. those of instable thermal stability and low efficiency, and particularly, the compound of the present invention exhibits superior efficiency in pure-blue phosphorescent devices. 2. The compound of claim 1 , wherein in Chemical Formula 1 claim 1 , Ar represents a substituted or unsubstituted phenyl group having 6 to 34 carbons claim 1 , a substituted or unsubstituted biphenyl group claim 1 , a substituted or unsubstituted terphenyl group claim 1 , a substituted or unsubstituted naphthyl group claim 1 , a substituted or unsubstituted anthryl group claim 1 , a substituted or unsubstituted pyrenyl group claim 1 , substituted or unsubstituted dibenzofuran claim 1 , substituted or unsubstituted dibenzothiophene claim 1 , substituted or unsubstituted dibenzophosphole claim 1 , substituted or unsubstituted dibenzophosphole oxide claim 1 , substituted or unsubstituted benzofuran claim 1 , substituted or unsubstituted benzothiophene claim 1 , substituted or unsubstituted carbazole claim 1 , substituted or unsubstituted phenylcarbazole claim 1 , substituted or unsubstituted indole claim 1 , substituted or unsubstituted phenylindole claim 1 , substituted or unsubstituted pyridine claim 1 , substituted or unsubstituted pyridazine claim 1 , or substituted or unsubstituted pyrimidine claim 1 ,{'sup': 1', '5, 'Yto Yare an oxygen atom,'}{'sup': 1', '10, 'Arto Arare identical or different substituents and each represent a substituted or unsubstituted ...

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06-06-2013 дата публикации

In Vivo Mitochondrial Labeling Using Positively-CHarged Nitroxide Enhanced and Gadolinum Chelate Enhanced Magnetic Resonance Imaging

Номер: US20130142735A1
Принадлежит: Individual

A system and method for acquiring MR imaging data from a subject includes administering positively-charged nitroxides or gadolinium chelates for in vivo mitochondrial labeling, acquiring MR imaging data from the subject, and reconstructing an image of the subject having enhanced contrast in areas including metabolic and/or mitotic activity.

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11-07-2013 дата публикации

FLUOROALKYLFLUOROPHOSPHORANE ADDUCTS

Номер: US20130178628A1
Принадлежит: Merck Patent GmBH

The invention relates to fluoroalkylfluorophosphorane adducts and the use thereof for masking OH groups in organic compounds. 1. Compounds of the formula I{'br': None, 'sub': f', 'n', '5-n, 'sup': '−', '[P(R)FD]\u2003\u2003I,'}{'sub': 'f', 'where Rin each case, independently of one another, denotes a straight-chain or branched fluoroalkyl group having 1 to 8 C atoms,'}n denotes 1, 2 or 3 andD denotes a Lewis base which contains at least one N atom, O atom or at least one P atom and the at least one N, O or P atom has a free electron pair or which contains at least one N—C(═O) group which coordinates to the P atom via the oxygen, and/or tautomers or stereoisomers, including mixtures thereof in all ratios.2. Compounds of the formula I according to claim 1 , characterised in that D denotes an aromatic amine claim 1 , a dialkyl ether claim 1 , an aromatic or aliphatic tertiary phosphine claim 1 , a dialkylformamide claim 1 , dialkylacetamide or N-alkyl-2-pyrrolidone claim 1 , where the said alkyl groups have claim 1 , in each case independently of one another claim 1 , 1 to 8 C atoms.3. Compounds of the formula I according to claim 1 , characterised in that D denotes 4-dimethylaminopyridine or dimethylformamide.4. Process for the preparation of the compounds of the formula I according to claim 1 , characterised in that a fluoroalkylfluorophosphorane of the formula II{'br': None, 'sub': f', 'n', '5-1, '(R)PF\u2003\u2003II,'}{'sub': 'f', 'where Rin each case, independently of one another, denotes a straight-chain or branched fluoroalkyl group having 1 to 8 C atoms and n denotes 1, 2 or 3, is reacted with a Lewis base D, where the Lewis base contains at least one N atom, O atom or at least one P atom and the at least one N, O or P atom has a free electron pair, or contains at least one N—C(═O) group which coordinates to the P atom via the oxygen.'}5. Process according to claim 4 , characterised in that the perfluoroalkylfluorophosphorane or the Lewis base is employed in ...

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01-08-2013 дата публикации

FUNCTIONALIZED FLUOROALKYL FLUOROPHOSPHATE SALTS

Номер: US20130197228A1

The present invention relates to functionalised fluoroalkylfluorophosphate salts, in particular as ionic liquids, to the preparation thereof and to the use thereof. 1. Compounds of the formula I{'br': None, 'sup': z+', '−, 'i': 'z', 'sub': f', 'n', '5-n, 'Kt[P(R)FX]\u2003\u2003I,'}{'sub': 'f', 'where Rin each case, independently of one another, denotes a straight-chain or branched fluoroalkyl group having 1 to 8 C atoms,'}X denotes OR, Ac, OAr or OHet, {'br': None, 'i': x', 'y, 'sup': z+', '2−, 'sub': f', 'n', '5-n', '5-n', 'f', 'n, '[Kt][(R)PF(OC(O)—R′—C(O)O)FP(R)]\u2003\u2003Ib,'}, 'Ac denotes a carboxyl group OC(O)R, also including carboxyl groups of an aliphatic dicarboxylic acid resulting in compounds having the formula Ib'}wherex denotes 2 and y denotes 1 if z denotes 1,x denotes 1 and y denotes 1 if z denotes 2,x denotes 2 and y denotes 3 if z denotes 3 andx denotes 1 and y denotes 2 if z denotes 4 and R′ denotes a single bond or an alkylene group having 1 to 4 C atoms,{'sub': 2', '2', '2', '3, 'Ar denotes an aryl group having 6 to 12 C atoms, which may be unsubstituted or substituted by Hal, NH, NAlk, NHAlk, NO, CN, SOH or OR,'}Alk denotes a straight-chain or branched alkyl group having 1 to 12 C atoms,{'sub': 2', '2', '2', '3, 'Het denotes a heteroaryl group having 5 to 13 C atoms, which may be unsubstituted or substituted by Hal, NH, NAlk, NHAlk, NO, CN, SOH or OR,'}{'sub': 2', '2', '2', '3', '2, 'R denotes H, a straight-chain or branched alkyl group having 1 to 20 C atoms, which may be partially substituted by Hal, NH, NHAlk, NAlk, OH, NO, CN or SOH, or denotes a straight-chain or branched alkenyl group having 2 to 20 C atoms, which may contain a plurality of double bonds, where one or two non-adjacent carbon atoms of the alkyl or alkenyl group which are not bonded to the heteroatom may be replaced by atoms and/or atom groups selected from the group —O—, —S—, —S(O)—, —SO—, NH, —C(O)—, —O—C(O)— or —C(O)—O—'}andKt denotes a stabilised proton, a metal cation ...

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08-08-2013 дата публикации

Synthesis of Drug Conjugates Via Reaction With Epoxide-Containing Linkers

Номер: US20130203998A1
Принадлежит: UNIVERSITY OF SOUTHERN CALIFORNIA

The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases. 1. A compound of the formula: CH[O]CH(CH)R ,{'sub': '1', 'comprising a C3 or longer alkyl chain where one end is an oxirane that can be conjugated to a compound or drug, and the other, a group Rthat can be conjugated to a second compound; and wherein the resulting compound may be used to link a compound or drug to another drug, modify a moiety, link a compound or drug to a bead, link a compound or drug to a support, or link a compound or drug to an imaging label.'}2. The compound of wherein the tertiary oxirane carbon is racemic.3. The compound of wherein the tertiary oxirane carbon is substantially pure as and R or S isomer.4. The compound of wherein n is 1-12 and Ris an amino claim 1 , hydroxyl claim 1 , halogen claim 1 , or other reactive group.5. The compound of wherein n is 1 and Ris NH2.6. The compound of wherein n is 1 and Ris a protected amino group.7. The compound of wherein n is 1 and Ris NHtBOC.8. The compound of wherein n is 2 and Ris an oxirane group.9. A method of synthesizing a linkable compound comprising reacting the compound of with a second compound containing a group capable of reacting with an oxirane.10. The method of wherein n is 1 and Ris NHtBOC claim 9 , and the tBOC protecting group is removed after formation of the conjugate by reaction with trifluoroacetic acid in water claim 9 , aqueous DMF claim 9 , or aqueous MeOH.11. A method of preparing the compound of comprising:{'sub': 2', 'n', '1', '1, '(a) reacting an alkene comprising CH═CH—(CH2)Rwith a reagent to protect Rand;'}(b) oxidizing the alkene group to an oxirane using meta-chloroperbenzoic acid.12. The method of wherein n is 1 and Ris NHtBOC.13. A method of preparing a linker conjugate compound comprising:{'sub': 2', '2', '1, '(a) ...

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22-08-2013 дата публикации

Anti-corrosion conformal coating comprising modified porous silica fillers for metal conductors electrically connecting an electronic component

Номер: US20130213707A1
Принадлежит: International Business Machines Corp

A conformal coating comprising modified porous silica particles is disclosed. A porous silica particle, such as MCM-14 or SBA-15 is modified with a sulfur gettering functionality, such as a phosphine compound, covalently bonded to silicon atoms in the porous silica particle. The conformal coating comprising the modified porous silica particles may be applied to metallic wiring areas of a circuit component, with the sulfur gettering functionality preventing sulfur from atmospheric gasses from penetrating the conformal coating to the metallic wiring.

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14-11-2013 дата публикации

METHOD AND SUBSTANCES FOR PREPARATION OF N-SUBSTITUTED PYRIDINIUM COMPOUNDS

Номер: US20130303768A1
Принадлежит: ROCHE DIAGNOSTICS OPERATIONS, INC.

A method for the synthesis of N-substituted 3-acylated pyridinium compounds by reacting a pentamethine precursor with a primary amine. 2. The method according to claim 1 , wherein R1 is methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl or isopropyl.3. The method according to claim 1 , wherein R2 claim 1 , R3 claim 1 , R4 and R5 are methyl.4. The method according to claim 1 , wherein the primary amine of Formula II is 3-Amino-5-[(phosphonooxy)methyl]-1 claim 1 ,2-cyclo-pentanediol.5. The method according to claim 1 , wherein the primary amine of Formula II is (1R claim 1 ,2S claim 1 ,3R claim 1 ,5R)-3-Amino-5-[(phosphono-oxy)methyl]-1 claim 1 ,2-cyclo-pentanediol.6. The method according to claim 1 , wherein the primary amine of Formula II is (1R claim 1 ,2S claim 1 ,3R claim 1 ,4R)-2 claim 1 ,3-Dihydroxy-4-hydroxymethyl-1-aminocyclopentane.7. The method according to claim 1 , wherein R6 is linear C1-C6 alkyl.8. The method according to claim 1 , wherein R6 is substituted branched C3-C6 alkyl.9. The method according to claim 1 , wherein R6 is substituted cyclic C5-C6 alkyl.10. The method according to claim 1 , wherein R6 is a furanosyl or a cyclopentyl residue.12. The compound according to claim 11 , wherein R1 is C1-C10 alkyl.13. The compound according to claim 11 , wherein R1 is selected from the group consisting of methyl claim 11 , ethyl claim 11 , propyl claim 11 , butyl and isopropyl.14. The compound according to claim 13 , wherein R1 is methyl. This application is a continuation of International Application No. PCT/EP2012/050996, filed Jan. 24, 2012, which claims the benefit of European Patent Application No. 11152201.7, filed Jan. 26, 2011, the disclosures of which are hereby incorporated by reference in their entirety.Pyridinium compounds are of interest in drug design or as general intermediates for organic syntheses, e.g., especially in natural product synthesis. (Cheng, W.-C. and Kurth, M. J., Organic Preparations and Procedures International 34 (2002 ...

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21-11-2013 дата публикации

N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS

Номер: US20130310344A1
Принадлежит: AstraZeneca AB

The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-Xactivities and may be used for the treatment of cancer. 2. A compound of Formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , as claimed in claim 1 , wherein claim 1 ,{'sup': '1', 'Ris OH;'}{'sup': '2', 'sub': 2', '3, 'Ris —S(O)CF;'}{'sup': 3', '40, 'sub': 1-2', '1-2, 'Ris Calkyl, wherein said Calkyl is optionally substituted with one or more R;'}{'sup': 4', '40, 'sub': 1-2', '1-2, 'Ris Calkyl, wherein said Calkyl is optionally substituted with one or more R;'}{'sup': 40', '40a, 'sub': '2', 'Rin each occurrence is selected from —ORand —OP(═O)(OH); and'}{'sup': '40a', 'Ris H.'}4. A compound of Formula (I) claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , as claimed in claim 3 , wherein the compound is 4-(4-((R)-(4′-chlorobiphenyl-2-yl)(hydroxy)methyl)piperidin-1-yl)-N-(4-((R)-4-((2-hydroxyethyl)(methyl)amino)-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonyl)benzamide.5. A compound of Formula (I) claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , as claimed in claim 3 , wherein the compound is 2-(((R)-3-(4-(N-(4-(4-((R)-(4′-chlorobiphenyl-2-yl)(hydroxy)methyl)piperidin-1-yl)benzoyl)sulfamoyl)-2-(trifluoromethylsulfonyl)phenylamino)-4-(phenylthio)butyl)(methyl)amino)ethyl dihydrogen phosphate.6. A compound of Formula (I) claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , as claimed in claim 3 , wherein the compound is 4-(4-((R)-(4′-chlorobiphenyl-2-yl)(hydroxy)methyl)piperidin-1-yl)-N-(4-((R)-4-(ethyl(2-hydroxyethyl)amino)-1-(phenylthio)butan-2-ylamino)-3-(trifluoromethylsulfonyl)phenylsulfonyl)benzamide.7. A compound of Formula (I) claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , as claimed in claim 3 , wherein the compound is 2-(((R)-3-(4-(N-(4-(4-((R)-(4′- ...

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19-12-2013 дата публикации

Mitochondria targeted cationic anti-oxidant compounds for prevention, therapy or treatment of hyper-proliferative disease, neoplasias and cancers

Номер: US20130338110A1

The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.

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16-01-2014 дата публикации

Protein affinity tag and uses thereof

Номер: US20140017797A1

This invention concerns isotopically coded or non-isotopically coded affinity-tags for analysis of certain target molecules in complex samples, in particular for mass spectrometric analysis of proteomic samples. The affinity-tags have the following general formula X-SPACER-OPO 3 H 2 , wherein X is a functional group or moiety capable of reacting with a functional group of a protein, peptide, DNA, lipid, sugar and/or steroid. These phosphate affinity tags (‘PTAG’) are capable of high but reversible binding to metal-oxides like TiO 2 . Due to this property, tagged sample fractions can be isolated from non-tagged sample fraction by affinity chromatography. The binding of organophosphate to metal-oxides remains intact during multiple washings of preferably acidic solutions to remove non-specifically bound components. PTAG's are also envisaged wherein X is selected such that it is capable of binding proteins, peptides, nucleic acid molecules, lipids, carbohydrates, steroids and the like.

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13-02-2014 дата публикации

Phosphonate Compounds

Номер: US20140045794A1

The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like. 2. The compound of claim 1 , wherein Ris hydrogen and B is guanin-9-yl.3. The compound of claim 1 , wherein Ris alkylglycerol.4. The compound of claim 1 , wherein Ris 1-S-alkylthioglycerol.5. The compound of claim 1 , wherein Ris alkoxyalkanol.6. The compound of claim 5 , wherein Ris alkoxyethanol.7. The compound of claim 5 , wherein Ris alkoxypropanol.8. The compound of claim 7 , wherein Ris hexadecyloxypropanol.9. The compound of claim 7 , wherein Ris octadecyloxypropanol.10. The compound of claim 1 , wherein Ris —CHOH and B is cytosin-1-yl.11. The compound of claim 10 , wherein Ris alkylglycerol.12. The compound of claim 10 , wherein Ris 1-S-alkylthioglycerol.13. The compound of claim 10 , wherein Ris alkoxyalkanol.14. The compound of claim 13 , wherein Ris alkoxyethanol.15. The compound of claim 13 , wherein Ris alkoxypropanol.16. The compound of claim 15 , wherein Ris hexadecyloxypropanol.17. The compound of claim 15 , wherein Ris octadecyloxypropanol.18. A pharmaceutical composition comprising an effective amount of the compound of and a pharmaceutically acceptable carrier.19. The pharmaceutical composition of claim 18 , wherein the composition is formulated as a solid dosage form.20. The pharmaceutical composition of claim 18 , wherein the composition is formulated as a capsule claim 18 , tablet claim 18 , aerosol claim 18 , solution claim 18 , or suspension claim 18 , or is a topical formulation or a solution. This application is a divisional application of U.S. application Ser. No. 13/645,105 filed Oct. 4, 2012, now pending; which is a continuation application of U.S. application Ser. No. 13/220,548 filed Aug. 29, 2011, now issued as U.S. Pat. No. 8,309,565; which is a continuation ...

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13-02-2014 дата публикации

MITOCHONDRIAL COMPOSITIONS AND USES THEREOF

Номер: US20140045798A1
Автор: Khan Shaharyar
Принадлежит: Gencia Corporation

The present invention provides a compound of Formula Ia, wherein Ris H or phosphate and the double bond is between Nand Cor between Nand C; Ris a mitochondrial targeting moiety; Ran alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; Ris H or an alkyl, aryl, or heteroaryl group; and Ris alkyl, aryl, or heteroaryl; or NC, and Ntogether form a heterocyclic ring containing at least 5 atoms, wherein N, N, and R-Rare as defined above, or Nand Rtogether form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof. 2. The compound of wherein the mitochondrial targeting moiety comprises a lipophilic cation.3. The compound of wherein the lipophilic cation comprises triphenylphosphonium.4. The compound of wherein the mitochondrial targeting moiety comprises polyarginine or polylysine.5. The compound of wherein the spacer group comprises a cleavable linkage.6. The compound of wherein the cleavable linkage is an ester linkage.9. The compound of claim 1 , wherein the compound is (triphenylphosphonio)methyl N-[amino(iminio)methyl]-N-methylglycinate or a pharmaceutically acceptable salt or prodrug thereof.10. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable excipient.11. A method for increasing levels of phosphocreatine in a host comprising administering to the host the compound of any one of .12. A method for treating mitochondrial myopathy comprising administering to a host having or suspected of having a mitochondrial myopathy the compound of .13. The method of wherein the compound is administered in an amount effective to increase phosphocreatine levels in the host relative to a control.14. The method of wherein the increase in phosphocreatine levels occurs in mitochondria of the host.15. The method of wherein the mitochondrial myopathy is selected from the group consisting of Kearns-Sayre syndrome claim 12 , Leigh's syndrome claim 12 , mitochondrial DNA ...

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10-04-2014 дата публикации

COLD MENTHOL RECEPTOR-1 ANTAGONISTS

Номер: US20140100194A1
Принадлежит: Janssen Pharmaceutica, NV

The invention is directed to TRPM8 antagonists of Formula (I). More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating TRPM8-mediated disorders. Pharmaceutical and veterinary compositions and methods of treating pain and various other disease states or conditions using compounds of the invention are also described. 2. (canceled)37-. (canceled)8. The compound of wherein X is O claim 1 , S claim 1 , or S(O).923-. (canceled)24. The compound of wherein L is absent claim 1 , —(CH)— claim 1 , —OCH— claim 1 , or ═CH—; and n is 1 or 2.25. The compound of wherein L is —(CH)— claim 24 , —OCH— claim 24 , or ═CH—; and n is 1.26. The compound of wherein L is —(CH)—; and n is 1.2737-. (canceled)4344-. (canceled)45. A method of treating or preventing a disease or condition in a mammal which disease or condition is affected by antagonism of TRPM8 claim 1 , which method comprises administering to a mammal in need of such treatment or prevention a therapeutically effective amount of a compound claim 1 , salt or solvate of .46. The method of wherein said therapeutically effective amount comprises a dose range of from about 0.1 mg to about 1 claim 45 ,000 mg.47. The method of wherein said therapeutically effective amount comprises a dose range of from about 50 mg to about 1000 mg.48. The method of wherein said therapeutically effective amount comprises a dose range of from about 100 mg to about 1000 mg.49. A method for treating a TRPM8-mediated disorder comprising the step of administering to a mammal in need of such treatment a therapeutically effective amount of a compound claim 1 , salt or solvate of .50. The method of wherein the TRPM8-mediated disorder is selected from the group consisting of inflammatory pain claim 49 , inflammatory hypersensitivity condition claim 49 , neuropathic pain claim 49 , anxiety claim 49 , and depression.51. The method of ...

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06-01-2022 дата публикации

PHOSPHATE COMPOUNDS FOR DETECTING NEUROLOGICAL DISORDERS

Номер: US20220001033A1
Принадлежит:

Provided herein are compounds, methods and compositions for determining whether a patient has a neurological disease or disorder is provided, comprising detecting the presence of a detectable target protein, or an accumulated mass thereof, for example, amyloid beta protein or phosphorylated tau protein, or an accumulated mass thereof, in a tissue or a sample of the patient. The detecting may comprise contacting the target protein with a compound described herein. 124.-. (canceled)27. The compound of claim 25 , wherein each X is independently O.33. The compound of as a sodium salt claim 30 , potassium salt claim 30 , lithium salt claim 30 , calcium salt claim 30 , magnesium salt claim 30 , zinc salt claim 30 , diisopropylamine salt claim 30 , triethylamine salt claim 30 , diethylamine salt claim 30 , ammonium salt claim 30 , diammonium salt claim 30 , tri(iso-propyl)amine salt claim 30 , tri(n-propyl)amine salt claim 30 , ethanolamine salt claim 30 , 2-dimethylaminoethanol salt claim 30 , piperazine salt claim 30 , piperidine salt claim 30 , morpholine salt claim 30 , N-ethylpiperidine salt claim 30 , or a mixed alkyl and aryl amine salt.34. The compound of claim 31 , as a sodium salt claim 31 , potassium salt claim 31 , lithium salt claim 31 , calcium salt claim 31 , magnesium salt claim 31 , zinc salt claim 31 , diisopropylamine salt claim 31 , triethylamine salt claim 31 , diethylamine salt claim 31 , ammonium salt claim 31 , diammonium salt claim 31 , tri(iso-propyl)amine salt claim 31 , tri(n-propyl)amine salt claim 31 , ethanolamine salt claim 31 , 2-dimethylaminoethanol salt claim 31 , piperazine salt claim 31 , piperidine salt claim 31 , morpholine salt claim 31 , N-ethylpiperidine salt claim 31 , or a mixed alkyl and aryl amine salt.35. The compound of claim 32 , a sodium salt claim 32 , potassium salt claim 32 , lithium salt claim 32 , calcium salt claim 32 , magnesium salt claim 32 , zinc salt claim 32 , diisopropylamine salt claim 32 , triethylamine salt ...

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04-01-2018 дата публикации

PROCESS FOR THE PREPARATION OF ACYLPHOSPHANES

Номер: US20180002357A1
Принадлежит: ETH ZUERICH

The present invention provides a process for the preparation of mono- and bisacylphosphanes based on formula (I): 2. The process as recited in claim 1 , wherein{'sup': 8', '8', '8', '6', '7', '8', '4, 'claim-text': either not, once, twice or more than twice interrupted by non-successive functional groups selected from the group consisting of:', {'sub': 2', '2', '2', '2', '2', '2', '2, 'sup': 4', '4', '4', '4', '4', '4', '4', '4', '4', '5', '5', '5', '5, '—O—, —S—, —SO—, —SO—, —SONR—, NRSO—, —NR—, —CO—, —O(CO)—, (CO)O—, —O(CO)O—, —NR(CO)NR—, NR(CO)—, —(CO)NR—, —NR(CO)O—, —O(CO)NR—, —Si(R)—, —OSi(R)—, —OSi(R)O—, —Si(R)O—,'}, 'and,', 'either not, additionally or alternatively either once, twice or more than twice interrupted by bivalent residues selected from the group consisting of heterocyclo-diyl, and aryldiyl,', 'and,', 'either not, additionally or alternatively either once, twice or more than twice substituted by substituents selected from the group consisting of:', {'sub': 6', '14', '1', '8', '1', '8', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', 'y', '3-y', 'y', '3-y, 'sup': 5', '5', '4', '4', '5', '4', '4', '4', '5', '4', '4', '4', '5', '5', '5, 'oxo, hydroxy, halogen, cyano, azido, C-C-aryl, C-C-alkoxy, C-C-alkylthio, —SOM, —COOM, POM, —PO(N(R)), PO(OR), —SON(R), —N(R), —CON(R), —COR, —OCOR, —NR(CO)R, —(CO)OR, —NR(CO)N(R), —Si(OR)(R), —OSi(OR)(R), with y=1, 2 or 3.'}], 'wherein the alkyl, alkenyl, aryl, alkanediyl and alkenediyl substituents are'}, 'Rindependently of further substituents Rwhich may be present in the substituent of formulae (IIa) to (IId) is alkyl, alkenyl or aryl or two substituents Rirrespective of whether they are both part of a substituent Z or belong to different substituents selected from Z, Rand Rtogether are alkanediyl or alkenediyl or alternatively, where two substituents —(CO)Rare present within the substituent of formulae (IIa), are together —O— or —NR—,'}3. The process as recited in claim 1 , wherein if Mis 1/q ...

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13-01-2022 дата публикации

TORSEMIDE PHOSPHATE PRODRUG, PREPARATION METHOD AND COMPOSITION THEREOF

Номер: US20220009951A1
Принадлежит:

The present application relates to the technical field of biological medicine, in particular to a torsemide phosphate prodrug, a preparation method and a composition thereof. The torsemide prodrug N-hydroxymethyl-torsemide phosphate, and/or a pharmaceutical salt thereof provided by the present application have a better solubility than torsemide, and have the advantage of high druggability. 2. The torsemide phosphate prodrug or pharmaceutical salt thereof according to claim 1 , wherein the pharmaceutical salt of the torsemide phosphate prodrug comprises a pharmaceutically acceptable salt claim 1 , which is selected from a sodium salt claim 1 , a potassium salt claim 1 , a barium salt claim 1 , a magnesium salt claim 1 , a zinc salt claim 1 , a lithium salt claim 1 , a ferric salt claim 1 , a ferrous salt or an organic ammonium salt.3. The torsemide phosphate prodrug or pharmaceutical salt thereof according to claim 2 , wherein the pharmaceutical salt of the torsemide phosphate prodrug is selected from disodium salt claim 2 , dipotassium salt or organic ammonium salt of phosphate group.4. The torsemide phosphate prodrug or pharmaceutical salt thereof according to claim 3 , wherein the organic ammonium salt is selected from trimethylammonium salt claim 3 , triethylammonium salt claim 3 , tripropylammonium salt claim 3 , or tri-n-butylammonium salt.8. A pharmaceutical composition claim 1 , comprising a therapeutic amount of N-hydroxymethyl-torsemide phosphate and/or pharmaceutical salt thereof according to claim 1 , and a pharmaceutically acceptable excipient.9. A pharmaceutical composition claim 5 , comprising a therapeutic amount of N-hydroxymethyl-torsemide phosphate claim 5 , and/or pharmaceutical salt according to claim 5 , and a pharmaceutically acceptable excipient. The present application is a continuation application of PCT application No. PCT/CN2020/084803, filed on Apr. 14, 2020, which claims the priority of China patent application number CN 2019104359957, ...

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01-01-2015 дата публикации

Modified Creatine Compounds

Номер: US20150005258A1
Принадлежит: Genci Corporation

The invention discloses creatine derivatives that are represented by Formula (I), Formula (II), and Formula (III); wherein Z is a functional group; Y is a mitochondrial targeting agent, a cationic ammonium group, or a polypeptide containing at least one positively charged amino acid residue; each Ris independently hydrogen, alkyl, or a phosphate group; Ra linker; Ris a spacer group; Ris hydrogen, alkyl, aryl, or heterocyclic; or Rand R, or Rand R, together with the nitrogen atoms to which they are attached form a heterocyclic ring, and W is hydrogen or alkyl. 2. A compound of wherein{'sub': 5', '5', '5', '5', '5', '5', '1-6, 'Z is —C(═O)NR—, —OC(═O)NR—, —NRC(═O)O—, or —NRC(═O)NR—; wherein each Ris independently hydrogen, or Calkyl;'}Y is a cationic phosphonium group;{'sub': '1', 'each Ris independently hydrogen, alkyl, or a phosphate group;'}{'sub': '2', 'Ris alkyl, cycloalkyl, heterocycloalkyl, or alkylaryl;'}{'sub': '3', 'Ris alkyl, cycloalkyl, alkylcycloalkyl, heterocycloalkyl, alkylheterocycloalkyl, or alkylaryl;'}{'sub': 4', '1-6, 'Ris hydrogen, or Calkyl; and W is hydrogen.'}3. A compound of wherein Z is —C(═O)NR— claim 2 , and Ris hydrogen claim 2 , or Calkyl.4. A compound of wherein Z is —C(═O)NH—.5. A compound of wherein a cationic phosphonium group is selected from —P(R′)X claim 2 , wherein R′ is alkyl or aryl; and X is an anion.6. A compound of wherein R′ is phenyl; and X is chloride claim 5 , or trifluoroacetate.7. A compound of wherein each Ris hydrogen.8. A compound of wherein one Ris hydrogen claim 2 , the other Ris —POM claim 2 , wherein M is a cation having one or two position charges.9. A compound of wherein Ris straight or branched Calkyl.10. A compound of wherein Ris Calkyl.11. A compound of wherein Ris alkyl claim 2 , cycloalkyl claim 2 , alkylcycloalkyl claim 2 , heterocycloalkyl claim 2 , or alkylheterocycloalkyl claim 2 , wherein alkyl is straight or branched.12. A compound of wherein Ris Calkyl.13. A compound of wherein Ris Calkylcycloalkyl ...

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20-01-2022 дата публикации

PSILOCIN DERIVATIVES AS SEROTONERGIC PSYCHEDELIC AGENTS FOR THE TREATMENT OF CNS DISORDERS

Номер: US20220017549A1
Принадлежит:

The present application relates to psilocin derivatives of Formula (1), to processes for their preparation, to compositions comprising them and to their use in activation of a serotonin receptor in a cell, as well as to treating diseases, disorders or conditions by activation of a serotonin receptor in a cell. 2. The compound of claim 1 , wherein Ris selected from S(O)Rand SOR claim 1 , wherein all available hydrogen atoms are optionally substituted with a halogen atom and/or all available atoms are optionally substituted with an alternate isotope thereof.3. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , C-Calkyl claim 1 , C(O)R claim 1 , CORand C(O)N(R) claim 1 , wherein all available hydrogen atoms are optionally substituted with a halogen atom and/or all available atoms are optionally substituted with an alternate isotope thereof.4. The compound of claim 3 , wherein Ris selected from hydrogen claim 3 , deuterium claim 3 , CH claim 3 , CFand CD.5. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , CH claim 1 , CHCH claim 1 , CH(CH)and C(CH) claim 1 , wherein all available hydrogen atoms are optionally substituted with a halogen atom and/or all available atoms are optionally substituted with an alternate isotope thereof.6. The compound of claim 5 , wherein Ris selected from hydrogen and deuterium.7. The compound of claim 1 , wherein R claim 1 , R claim 1 , Rand Rare independently selected from hydrogen and C-Calkyl claim 1 , wherein at least one of R claim 1 , R claim 1 , Rand Ris deuterium or at least one of R claim 1 , R claim 1 , Rand Rcomprises deuterium and wherein all available hydrogen atoms are optionally substituted with a halogen atom and/or all available atoms are optionally substituted with an alternate isotope thereof.8. The compound of claim 7 , wherein R claim 7 , R claim 7 , Rand Rare independently selected from hydrogen claim 7 , deuterium claim 7 , CHand CD claim 7 , wherein at least one of R claim 7 , R ...

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03-01-2019 дата публикации

Electron Injection Layer for an Organic Light-Emitting Diode (OLED)

Номер: US20190006589A1
Принадлежит: NOVALED GMBH

The invention relates to Organic light emitting diode comprising at least one emission layer, an electron injection layer and at least one cathode electrode, wherein: 1. Organic light emitting diode comprising at least one emission layer , an electron injection layer and at least one cathode electrode , wherein:the electron injection layer comprises an organic phosphine compound, wherein the electron injection layer is free of a metal, metal salt, metal complex and metal organic compound;the cathode electrode comprises at least a first cathode electrode layer, whereinthe first cathode electrode layer comprises a first zero-valent metal selected from the group comprising alkali metal, alkaline earth metal, rare earth metal and/or a group 3 transition metal; andthe electron injection layer is arranged in direct contact to the first cathode electrode layer.3. The organic light emitting diode according to claim 1 , wherein the first cathode electrode layer is free of a metal halide and/or free of a metal organic complex.4. The organic light emitting diode according to claim 1 , wherein the first cathode electrode layer further comprises a second zero-valent metal claim 1 , wherein the second zero-valent metal is selected from a main group metal or a transition metal claim 1 , wherein the second zero-valent metal is selected different from the first zero-valent metal.5. The organic light emitting diode according to claim 1 , wherein the cathode electrode further comprises a second cathode electrode layer claim 1 , wherein the second cathode electrode layer comprises at least a third metal claim 1 , in form of a zero-valent metal claim 1 , alloy and/or as oxide claim 1 , wherein the third metal is selected from a main group metal claim 1 , transition metal and/or rare earth metal.6. The organic light emitting diode according to claim 1 , further comprising at least one electron transport layer comprising at least one matrix compound claim 1 , wherein the electron ...

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10-01-2019 дата публикации

SOLUBLE C5aR ANTAGONISTS

Номер: US20190010177A1
Принадлежит:

Compounds are provided to modulate the C5a receptor. The compounds have the following Formula (I): 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris selected from the group consisting of O—(CO)—Calkylene-NRR claim 1 , O—(CO)—Calkylene-NR(CO)—Calkylene-NRR claim 1 , O—P(O)OROR claim 1 , O—CH—O—P(O)ORORand O—(CO)—Carylene-Calkylene-Cheterocyclyl claim 1 , wherein the Cheterocyclyl is selected from the group consisting of piperidinyl claim 1 , piperazinyl claim 1 , pyrrolidinyl claim 1 , morpholinyl and azetidinyl and wherein the piperidinyl claim 1 , piperazinyl claim 1 , pyrrolidinyl claim 1 , morpholinyl and azetidinyl are optionally substituted with 1 to 6 Rgroups.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —CH—O—P(O)ORORand —P(O)OROR.12. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —(CO)—Calkylene- NRR claim 1 , —(CO)—O—Calkylene-O—P(O)OROR claim 1 , —P(O)ORO(CO)—Calkyl claim 1 , —P(O)ORNRR claim 1 , —(CO)—O—Calkylene-O—(CO)—Calkenylene-COH claim 1 , —(CO)—Calkylene-NR(CO)—Calkylene- NRRwherein the Calkylene- NRRmay be optionally substituted by with NRR claim 1 , —(CO)—O—Calkylene-O—(CO)—Calkylene-NRR claim 1 , and —(CO)—O—Calkylene-Caryl-O—P(O)ORORwherein the Caryl is optionally substituted with 1 to 5 Rwhich can be the same or different.15. The compound of any one of to claim 1 , to and to claim 1 , which is in the form of a pharmaceutically acceptable salt.16. The compound of wherein the pharmaceutically acceptable salt is selected from the group consisting of ammonium claim 15 , calcium claim 15 , magnesium claim 15 , potassium claim 15 , sodium claim 15 , zinc claim 15 , arginine claim 15 , betaine claim 15 , caffeine claim 15 , choline claim 15 , N claim 15 ,N′-dibenzylethylenediamine claim 15 , diethylamine claim 15 , 2-diethylaminoethanol claim 15 , 2- ...

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12-01-2017 дата публикации

COMPOUND, MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENTS, ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE

Номер: US20170012209A1
Принадлежит: IDEMITSU KOSAN CO., LTD.

A high-performance organic electroluminescence device and an electronic equipment provided with the organic electroluminescence device are provided. Also, a compound for achieving the organic electroluminescence device and the electronic equipment is provided. Specifically, a compound having a specific structure having a triphenylene skeleton, an organic electroluminescence device using the compound and an electronic equipment provided with the organic electroluminescence device are provided. 2. The compound according to claim 1 , wherein one of Rto Ris a group represented by the general formula (2).4. The compound according to claim 1 , wherein the substituents of the pair in Rto Rcombine to form a ring claim 1 , and the ring is a substituted or unsubstituted aromatic ring or a substituted or unsubstituted heteroaromatic ring.8. The compound according to claim 7 , wherein Rand Rto Rin the general formulae (1-1′) and (1-2′) are all independent from each other and do not combine to form a ring.10. The compound according to claim 1 , wherein at least one of Arand Aris a substituted or unsubstituted aryl group having 6 to 60 ring carbon atoms.11. The compound according to claim 10 , wherein Arand Arare both a substituted or unsubstituted aryl group having 6 to 60 ring carbon atoms.12. The compound according to claim 11 , wherein Arand Arare both a substituted or unsubstituted aryl group having 6 to 13 ring carbon atoms.13. The compound according to claim 11 , wherein Arand Arare each independently a substituted or unsubstituted phenyl group claim 11 , a substituted or unsubstituted naphthyl group claim 11 , a substituted or unsubstituted biphenylyl group or a substituted or unsubstituted fluorenyl group.14. The compound according to claim 1 , wherein X is an oxygen atom or a sulfur atom.15. The compound according to claim 1 , wherein Lis a direct bond.16. The compound according to claim 1 , wherein Lis a phenylene group claim 1 , a naphthylene group claim 1 , an ...

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26-01-2017 дата публикации

ONO Pincer Ligands and ONO Pincer Ligand Comprising Metal Complexes

Номер: US20170022230A1
Принадлежит:

Embodiments of the invention are directed to ONO pincer ligands that can be in a trianionic, protonated or protonated equivalent form. The ONO pincer ligand can be combined with a metal comprising compound to form an ONO pincer ligand comprising transition metal complex. By choice of the ONO pincer ligand structure, the steric and electronic properties of the metal complexes therefrom can be controlled. The ONO pincer ligands comprise a central nitrogen atom that is disubstituted with a pair of three atom comprising bridges where the three atoms are a pair of sphybridized carbons and an sphybridized carbon. 3. A method of preparing an ONO pincer ligand precursor according to claim 1 , comprising condensing a nucleophilic oxygen or nucleophilic nitrogen comprising compound with an electrophilic carbon comprising compound further comprising the bridge structure of the resulting ONO pincer ligand.4. A trianionic ONO pincer ligand comprising metal complex comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one ONO trianionic pincer ligand derived from the ONO trianionic pincer ligand precursor of ; and'}a metal.5. The trianionic ONO pincer ligand comprising metal complex of claim 4 , wherein the metal is a transition metal from group III through group X of the periodic table.13. The method of preparing an ONO pincer ligand comprising metal complex of claim 11 , wherein the precursor metal compound further comprises a metal alkylidyne claim 11 , further comprising adding the OH or NH of the ONO pincer ligand precursor across the metal alkylidyne to form the anionic ONO pincer ligand comprising metal complex. This application is a divisional of U.S. application Ser. No. 14/077,822, filed Nov. 12, 2013, which is a continuation-in-part of International Patent Application No. PCT/US2012/037302, filed May 10, 2012, which claims the benefit of U.S. Provisional Application Ser. No. 61/484,793, filed May 11, 2011, the disclosures of which are hereby ...

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25-01-2018 дата публикации

Process for the preparation of esters by means of carbonylation of ethers

Номер: US20180022684A1
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to a process comprising the process steps of: a) initially charging an ether having from 3 to 30 carbon atoms; b) adding a phosphine ligand and a compound comprising Pd, or adding a comprising Pd and a phosphine ligand; c) feeding in CO; d) heating the reaction mixture, with conversion of the ether; wherein the phosphine ligand is a compound of formula (I) where m and n are each independently 0 or 1; R 1 , R 2 , R 3 , R 4 are each independently selected from —(C 1 -C 12 )-alkyl, —(C 3 -C 12 )-cycloalkyl, —(C 3 -C 12 )-heterocycloalkyl, —(C 6 -C 20 )-aryl, —(C 3 -C 20 )-heteroaryl; at least one of the R 1 , R 2 , R 3 , R 4 radicals is a —(C 3 -C 20 )-heteroaryl radical; and R 1 , R 2 , R 3 , R 4 , if they are —(C 1 -C 12 )-alkyl, —(C 3 -C 12 )-cycloalkyl, —(C 3 -C 12 )-heterocycloalkyl, —(C 6 -C 20 )-aryl or —(C 3 -C 20 )-heteroaryl, may each independently be substituted by one or more substituents selected from —(C 1 -C 12 )-alkyl, —(C 3 -C 12 )-cycloalkyl, —(C 3 -C 12 )-heterocycloalkyl, —O—(C 1 -C 12 )-alkyl, —O—(C 1 -C 12 )-alkyl-(C 6 -C 20 )-aryl, —O—(C 3 -C 12 )-cycloalkyl, —S—(C 1 -C 12 )-alkyl, —S—(C 3 -C 12 )-cycloalkyl, —COO—(C 1 -C 12 )-alkyl, —COO—(C 3 -C 12 )-cycloalkyl, —CONH—(C 1 -C 12 )-alkyl, —CONH—(C 3 -C 12 )-cycloalkyl, —CO—(C 1 -C 12 )-alkyl, —CO—(C 3 -C 12 )-cycloalkyl, —N—[(C 1 -C 12 )-alkyl] 2 , —(C 6 -C 20 )-aryl, —(C 6 -C 20 )-aryl-(C 1 -C 12 )-alkyl, —(C 6 -C 20 )-aryl-O—(C 1 -C 12 )-alkyl, —(C 3 -C 20 )-heteroaryl, —(C 3 -C 20 )heteroaryl-(C 1 -C 12 )-alkyl, —(C 3 -C 20 )-heteroaryl-O—(C 1 -C 12 )-alkyl, —COOH, —SO 3 H, —NH 2 , halogen; and wherein no alcohol is added to the reaction mixture.

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25-01-2018 дата публикации

Process for the alkoxycarbonylation of ethers

Номер: US20180022685A1
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to a process comprising the following process steps: a) introducing an ether having 3 to 30 carbon atoms; b) adding a phosphine ligand and a compound which comprises Pd, or adding a complex comprising Pd and a phosphine ligand; c) adding an alcohol; d) supplying CO; e) heating the reaction mixture, the ether being reacted for form an ester; where the phosphine ligand is a compound of formula (I) where m and n are each independently 0 or 1; R 1 , R 2 , R 3 , R 4 are each independently selected from —(C 1 -C 12 )-alkyl, —(C 3 -C 12 )-cycloalkyl, —(C 3 -C 12 )-heterocycloalkyl, —(C 6 -C 20 )-aryl, —(C 3 -C 20 )-heteroaryl; at least one of the R 1 , R 2 , R 3 , R 4 radicals is a —(C 3 -C 20 )-heteroaryl radical; and R 1 , R 2 , R 3 , R 4 , if they are —(C 1 -C 12 )-alkyl, —(C 3 -C 12 )-cycloalkyl, —(C 3 -C 12 )-heterocycloalkyl, —(C 6 -C 20 )-aryl or —(C 3 -C 20 )-heteroaryl, may each independently be substituted by one or more substituents selected from —(C 1 -C 12 )-alkyl, —(C 3 -C 12 )-cycloalkyl, —(C 3 -C 12 )-heterocycloalkyl, —O—(C 1 -C 12 )-alkyl, —O—(C 1 -C 12 )-alkyl-(C 6 -C 20 )-aryl, —O—(C 3 -C 12 )-cycloalkyl, —S—(C 1 -C 12 )-alkyl, —S—(C 3 -C 12 )-cycloalkyl, —COO—(C 1 -C 12 )-alkyl, —COO—(C 3 -C 12 )-cycloalkyl, —CONH—(C 1 -C 12 )-alkyl, —CONH—(C 3 -C 12 )-cycloalkyl, —CO—(C 1 -C 12 )-alkyl, —CO—(C 3 -C 12 )-cycloalkyl, —N—[(C 1 -C 12 )-alkyl] 2 , —(C 6 -C 20 )-aryl, —(C 6 -C 20 )-aryl-(C 1 -C 12 )-alkyl, —(C 6 -C 20 )-aryl-O—(C 1 -C 12 )-alkyl, —(C 3 -C 20 )-heteroaryl, —(C 3 -C 20 )-heteroaryl-(C 1 -C 12 )-alkyl, —(C 3 -C 20 )-heteroaryl-O—(C 1 -C 12 )-alkyl, —COOH, —OH, —SO 3 H, —NH 2 , halogen.

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10-02-2022 дата публикации

QUINONE METHIDE ANALOG SIGNAL AMPLIFICATION

Номер: US20220041633A1
Принадлежит:

Disclosed herein are novel quinone methide analog precursors and embodiments of a method and a kit of using the same for detecting one or more targets in a biological sample. The method of detection comprises contacting the sample with a detection probe, then contacting the sample with a labeling conjugate that comprises an enzyme. The enzyme interacts with a quinone methide analog precursor comprising a detectable label, forming a reactive quinone methide analog, which binds to the biological sample proximally to or directly on the target. The detectable label is then detected. In some embodiments, multiple targets can be detected by multiple quinone methide analog precursors interacting with different enzymes without the need for an enzyme deactivation step. 1. A method of detecting a first target in a biological sample , comprising:contacting the biological sample with a first detection probe specific to the first target;labeling the first target with a first enzyme through the first detection probe;contacting the biological sample with a first quinone methide analog precursor comprising a first enzyme recognition group and a first detectable label, anddetecting the first target by detecting the first detectable label.2. The method of claim 1 , wherein the first enzyme cleaves the first enzyme recognition group claim 1 , thereby converting the first quinone methide analog precursor into a first reactive quinone methide analog which covalently binds to the biological sample proximally to or directly on the first target.3. The method of claim 1 , wherein the first enzyme is a phosphatase claim 1 , phosphodiesterase claim 1 , esterase claim 1 , lipase claim 1 , amidase claim 1 , protease claim 1 , nitroreductase claim 1 , urease claim 1 , sulfatase claim 1 , cytochrome P450 claim 1 , alpha-glucosidase claim 1 , beta-glucosidase claim 1 , beta-lactamase claim 1 , alpha-glucoronidase claim 1 , beta-glucoronidase claim 1 , alpha-galactosidase claim 1 , beta- ...

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23-01-2020 дата публикации

NOVEL IMINES WITH TUNABLE NUCLEOPHILICITY AND STERIC PROPERTIES THROUGH METAL COORDINATION: APPLICATIONS AS LIGANDS AND METALLOORGANOCATALYSTS

Номер: US20200023344A1
Автор: HUANG Kuo-Wei, Zhao Qianyi
Принадлежит:

The invention describes phospho-amino pincer-type ligands, metal complexes thereof, and catalytic methods comprising such metal complexes for conversion of carbon dioxide to methanol, conversion of aldehydes into alcohols, conversion of aldehydes in the presence of a trifluoromethylation agent into trifluorinated secondary alcohols, cycloaddition of carbon dioxide to an epoxide to provide cyclic carbonates or preparation of an amide from the combination of an alcohol and an amine. 2. The composition of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each a alkyl claim 1 , each Z is CH and Ris a hydrogen atom.3. The composition of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , and Rare each a Calkyl.4. The composition of claim 2 , wherein Ris a methyl group or a hydrogen.5. The composition of claim 1 , wherein X is a hydride.6. The composition of claim 1 , wherein X is a halide.7. The composition of claim 1 , wherein the base is an organic base.8. The composition of claim 7 , wherein the organic base is an amine or an alkoxide.9. The composition of claim 8 , wherein the amine is an alkylamine comprising NRRR claim 8 , wherein R claim 8 , R claim 8 , and Rare each independently a hydrogen atom claim 8 , alkyl claim 8 , aryl claim 8 , aralkyl claim 8 , or a substituted version of any one of these groups claim 8 , wherein one or more of R claim 8 , R claim 8 , and Rcan form a ring or an aromatic amine.10. The composition of claim 9 , wherein the aromatic amine is pyridine. This International Application claims priority to U.S. Provisional Patent Application Ser. No. 62/049,022, filed Sep. 11, 2014, entitled “Novel Imines with tunable nucleophilicity and steric properties through metal coordination: Applications as ligands and Metalloorganocatalysts”, the contents of which are incorporated herein in their entirety for all purposes.The present invention relates generally to the field of chemistry and catalysis. More particularly, it relates to ...

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04-02-2016 дата публикации

18f-labeled psma-targeted pet imaging agents

Номер: US20160030605A1

Compounds of Marlush formula (I) described in the claims are useful in diagnostic methods for detecting and/or identifying cells presenting PSMA. Disclosed are also methods for preparing the compounds. Representative compounds according to the application are:

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29-01-2015 дата публикации

FORMYLPYRROLE-BASED HETEROCYCLES FOR NUCLEIC ACID ATTACHMENT TO SUPPORTS

Номер: US20150031833A1
Принадлежит:

A compound has Formula I: 2. The compound of claim 1 , wherein the protected aldehyde is selected from the group consisting of an acetal claim 1 , an aminal claim 1 , a dithioacetal claim 1 , a protected hemiaminal claim 1 , an alkene claim 1 , and a protected hemithioacetal.3. The compound of claim 1 , wherein W claim 1 , X claim 1 , Y claim 1 , and Z comprise a fused ring system selected from the group consisting of a benzene claim 1 , a pyridine claim 1 , a furan claim 1 , a thiophene claim 1 , a pyridazine claim 1 , a pyrazine claim 1 , and a pyrimidine.4. The compound of claim 3 , wherein W claim 3 , X claim 3 , Y claim 3 , and Z comprise a fused benzene ring.5. The compound of claim 1 , wherein A is hydrogen or methyl claim 1 , Q is a protected aldehyde claim 1 , Ris N-iPr claim 1 , and Ris OCHCHCN.6. The compound of claim 1 , wherein A is a hydroxyl claim 1 , alkoxy or hydroxyalkyl claim 1 , Q is a protected aldehyde claim 1 , Ris N-iPr claim 1 , and Ris OCHCHCN.8. The compound of claim 7 , wherein the protected aldehyde is selected from the group consisting of an acetal claim 7 , an aminal claim 7 , a dithioacetal claim 7 , a protected hemiaminal claim 7 , an alkene claim 7 , and a protected hemithioacetal.9. The compound of wherein W claim 7 , X claim 7 , Y claim 7 , and Z comprise a fused ring system selected from the group consisting of a benzene claim 7 , a pyridine claim 7 , a furan claim 7 , a thiophene claim 7 , a pyridazine claim 7 , a pyrazine claim 7 , and a pyrimidine.10. The compound of claim 9 , wherein W claim 9 , X claim 9 , Y claim 9 , and Z comprise a fused benzene ring.11. The compound of claim 7 , wherein A is hydrogen or methyl claim 7 , Q is a protected aldehyde claim 7 , Nu is selected from the group consisting of a 3′-phosphate-linked nucleic acid claim 7 , a 3′-thiophosphate-linked nucleic acid claim 7 , and a 3′-phosphate linked modified nucleic acid.12. The compound of claim 7 , wherein A is hydrogen or methyl claim 7 , Q is a ...

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04-02-2016 дата публикации

PHOTORESPONSIVE NUCLEOTIDE ANALOGUE HAVING PHOTOCROSSLINKING ABILITY

Номер: US20160031918A1

The present invention provides a new photoreactive compound which can be used in technologies for photoreactions of nucleic acid, and also provides a photoreactive crosslinking agent comprising the above photoreactive compound. A photoreactive compound represented by the following formula I can be used. 3. The compound according to claim 1 , wherein R3 is a hydrogen atom claim 1 , a hydroxy group claim 1 , a C1 to C3 alkoxy group claim 1 , a C1 to C3 alkylsulfanyl group claim 1 , a nitro group claim 1 , a fluorine atom claim 1 , a trifluoromethyl group claim 1 , a phenyl group claim 1 , a 2-naphthyl group claim 1 , a 2-indolyl group claim 1 , a benzimidazole-2-yl group or a benzothiophene-2-yl group.4. A photoreactive crosslinking agent comprising the compound according to .5. A method of forming photo crosslinking of a nucleobase having a pyrimidine ring to the compound according to .7. The compound according to claim 2 , wherein R3 is a hydrogen atom claim 2 , a hydroxy group claim 2 , a C1 to C3 alkoxy group claim 2 , a C1 to C3 alkylsulfanyl group claim 2 , a nitro group claim 2 , a fluorine atom claim 2 , a trifluoromethyl group claim 2 , a phenyl group claim 2 , a 2-naphthyl group claim 2 , a 2-indolyl group claim 2 , a benzimidazole-2-yl group or a benzothiophene-2-yl group.8. A photoreactive crosslinking agent comprising the compound according to .9. A photoreactive crosslinking agent comprising the compound according to .10. A method of forming photo crosslinking of a nucleobase having a pyrimidine ring to the compound according to .11. A method of forming photo crosslinking of a nucleobase having a pyrimidine ring to the compound according to . The present invention relates to a photoreactive nucleobase-like structure capable of crosslinking with nucleic acid and the like, a photoreactive crosslinking agent having an alternative structure of deoxyribose and a photoreactive nucleotide-like compound (photoreactive nucleotide analogue) having photo ...

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31-01-2019 дата публикации

ELECTROCHROMIC COMPOUND, ELECTROCHROMIC COMPOSITION, AND DISPLAY ELEMENT

Номер: US20190031694A1
Принадлежит:

To provide an electrochromic compound, represented by the following general formula 2. The electrochromic composition according to claim 1 , wherein the electroconductive or semiconductive nanostructure is composed of metal oxide particles claim 1 , and wherein the metal oxide particles are at least one selected from the group consisting of titanium oxide claim 1 , zinc oxide claim 1 , tin oxide claim 1 , alumina claim 1 , zirconium oxide claim 1 , iron oxide claim 1 , magnesium oxide claim 1 , indium oxide claim 1 , and tungsten oxide.3. The electrochromic composition according to claim 2 , wherein the metal oxide particles have an average primary particle diameter of 30 nm or smaller.5. The display element of claim 4 , wherein the display layer comprises an electrochromic composition comprising the electrochromic compound and an electroconductive or semiconductive nanostructure claim 4 , wherein the electrochromic compound is bonded to or adsorbed on the nanostructure. This is a divisional of application Ser. No. 14/433,176, filed Apr. 2, 2015, which is the National Stage of International application no. PCT/JP2013/080363, filed Nov. 1, 2013 which claimed priority to Japanese patent application nos. 2012-241679, filed Nov. 1, 2012, and 2013-096261, filed May 1, 2013, of which all of the disclosures are incorporated herein by reference in their entiretiesThe present invention relates to an electrochromic compound, and an electrochromic composition, both of which colors in cyan as they are colored, and relates to a display element using the electrochromic compound or the electrochromic composition.As for an electronic medium replacing paper, developments of electronic paper have been recently actively carried out.The electronic paper has characteristics that the display device thereof is used like paper, and therefore requires properties different from conventional display devices, such as CRT and LCD. For example, required properties thereof are being a reflective ...

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30-01-2020 дата публикации

FUNCTIONALIZED PHOSPHONATES VIA MICHAEL ADDITION

Номер: US20200031855A1
Принадлежит:

Provided herein are functionalized phosphonates and methods for making same via phosphite addition to an atom alpha to an electron withdrawing group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron-withdrawing group is selected from nitro claim 1 , cyano claim 1 , —C(O)OH claim 1 , —C(O)R claim 1 , —C(O)OR claim 1 , and —C(O)NHR.3. The method of claim 1 , further comprising a reduction step.4. The method of claim 1 , wherein each of Cyand Cyis phenyl.5. The method of claim 1 , wherein n is 0.6. A compound produced by the method of .8. The compound of claim 7 , wherein the electron-withdrawing group is selected from nitro claim 7 , cyano claim 7 , —S(O)R claim 7 , —SOR claim 7 , —P(O)(R) claim 7 , —P(O)(OR) claim 7 , —C(O)OH claim 7 , —C(O)R claim 7 , —C(O)OR claim 7 , and —C(O)NHR.9. The compound of claim 7 , wherein each of Cyand Cyis phenyl.10. The compound of claim 7 , wherein n is 0.12. The method of claim 11 , wherein each of Cyand Cyis phenyl.13. The method of claim 11 , wherein n is 0.14. The method of claim 11 , further comprising a reduction step.15. The method of claim 11 , wherein reacting is in the presence of a catalyst.17. The method of claim 11 , wherein Rand R claim 11 , together with the intervening atoms claim 11 , comprise a 5- or 6-membered cycloalkyl or a 5- or 6-membered heterocycloalkyl having 1 or 2 ring-members selected from O claim 11 , S claim 11 , and NR claim 11 , substituted with 0 claim 11 , 1 claim 11 , 2 claim 11 , or 3 groups independently selected from hydroxyl claim 11 , halogen claim 11 , oxo claim 11 , C1-C4 alkyl claim 11 , C1-C4 alkoxy claim 11 , —C(O)OH claim 11 , —C(O)R claim 11 , —C(O)OR claim 11 , and —C(O)NHR.20. A compound produced by the method of . This application is a continuation application of U.S. application Ser. No. 15/650,417, filed Jul. 14, 2017, which claims ...

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04-02-2021 дата публикации

ELECTROCHROMIC ELEMENT

Номер: US20210032531A1
Принадлежит:

An electrochromic element including: a first electrode; a second electrode disposed to face the first electrode with a gap between the first electrode and the second electrode; a first electrochromic layer disposed on or above the first electrode, including conductor or semiconductor nano-structures and an electrochromic compound; and an electrolyte layer including an electrolyte, disposed between the first electrochromic layer and the second electrode, wherein the electrochromic compound is a compound represented by General Formula 1, and an anion of the electrolyte is a monovalent anion having oxidation potential higher than reduction potential of a dication of General Formula 1 by 3.1 V or greater, 2. The electrochromic element according to claim 1 ,wherein the first electrochromic layer is a first electrochromic layer, in which the electrochromic compound is deposited on the nano-structures.4. The electrochromic element according to claim 3 ,wherein the electrolyte layer includes an electrolyte, and an anion of the electrolyte is a monovalent anion having an oxidation potential higher than a reduction potential of a dication of General Formula 1 by 3.1 V or greater.5. The electrochromic element according to claim 1 ,{'sub': 2', '2', '3', '2', '2', '4', '4', '6', '4, 'sup': −', '−', '−', '−', '−', '−, 'wherein the anion of the electrolyte of the electrolyte layer is one or more selected from the group consisting of (FSO)N, (CFSO)N, (CB)B, BF, PF, and ClO.'}6. The electrochromic element according to claim 1 ,{'sub': 1', '2', '1', '2, 'wherein Ror R, or both Rand Rof General Formula 1 are a phosphonic acid group, a phosphoric acid group, a carboxylic acid group, a sulfonyl group, a silyl group, or a silanol group.'}7. The electrochromic element according to claim 1 ,{'sub': 1', '2, 'wherein one of Rand Rof General Formula 1 is a phosphonic acid group, a phosphoric acid group, a carboxylic acid group, a sulfonyl group, a silyl group, or a silanol group, and the ...

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24-02-2022 дата публикации

UV-CURABLE PHOSPHONIUM SMALL MOLECULES AS ANTIMICROBIAL COATINGS AND SURFACE ACTIVE ADDITIVES

Номер: US20220056058A1
Принадлежит:

The attachment and proliferation of antibiotic resistant, biofilm-forming bacteria to oft-handled material surfaces has emerged as a growing concern, particularly in the biomedical, healthcare and food packaging industries. UV-curable phosphoniums bearing benzophenone anchors have been synthesized with a variety of alkyl, aryl, and fluoroalkyl functional groups at phosphorus to probe their efficacy as thermally stable antimicrobial additives in plastics or as surface coatings. In an embodiment, a phosphonium compound having the following formula has been synthesized: 2. The phosphonium compound according to claim 1 , wherein the alkyl has a general formula CHwherein n is an integer ranging between 1 and 18.3. The phosphonium compound according to claim 1 , wherein the substituted alkyl has a general formula CXwherein X is hydrogen and/or one or more of substituents claim 1 , and n is an integer ranging between 1 and 18.4. The phosphonium compound according to claim 1 , wherein the substituted alkyl has a number of carbon atoms in a range between 1 and 18.5. The phosphonium compound according to claim 3 , wherein the substituents comprise fluorine.6. The phosphonium compound according to claim 1 , wherein the substituted aryl has substituents at any one claim 1 , or more of claim 1 , ortho claim 1 , meta and para positions.7. The phosphonium compound according to claim 6 , wherein the substituents comprise an alkyl or a heteroalkly claim 6 , wherein the alkyl backbone is optionally substituted.8. The phosphonium compound according to claim 7 , wherein the alkyl backbone is substituted with fluorine.11. The phosphonium compound according to claim 10 , combined as an additive with a polymer for forming an antimicrobial composite material.12. The antimicrobial composite material according to claim 11 , wherein said polymer is a thermoplastic polymer claim 11 , and wherein said phosphonium compound (2) is covalently bound to the thermoplastic polymer lattice.13. The ...

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12-02-2015 дата публикации

Fluorescent phospholipid ether compounds, compositions, and methods of use

Номер: US20150044142A1
Принадлежит: Cellectar Inc

The invention generally relates to novel fluorescent phospholipid compounds, compositions comprising these compounds, and diagnostic methods utilizing these compounds. A preferred compound of the present invention has the following structural formula:

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15-02-2018 дата публикации

Nitrogen-containing heterocyclic derivative having 2-imino group and pest control agent including the same

Номер: US20180042233A1
Принадлежит: Meiji Seika Pharma Co Ltd

Provided is a nitrogen-containing heterocyclic derivative having a 2-imino group, which is represented by the following Formula (I). [in the formula, Ar represents a phenyl group which may be substituted, a 5- to 6-membered heterocycle which may be substituted, or a 4- to 10-membered heterocycloalkyl group, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1 to C6 alkyl group which may be substituted with a halogen atom, a C1 to C6 alkyloxy group which may be substituted with a halogen atom, a cyano group, or a nitro group, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z).]

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15-02-2018 дата публикации

PRODRUGS OF PYRIDONE AMIDES USEFUL AS MODULATORS OF SODIUM CHANNELS

Номер: US20180044361A1
Принадлежит:

The invention relates to prodrug compounds of formula I: 2. The compound according to claim 1 , wherein Ris hydrogen claim 1 , Cl or CF.3. The compound according to or claim 1 , wherein Ris hydrogen claim 1 , Cl claim 1 , CFor CFCF.4. The compound according to any one of to claim 1 , wherein Ris hydrogen claim 1 , Cl claim 1 , F claim 1 , CH claim 1 , OCHor OCF.5. The compound according to any one of to claim 1 , wherein 127 is hydrogen claim 1 , fluorine or OCF.6. The compound according to any one of to claim 1 , wherein X is —PO(OH).8. The compound according to claim 7 , wherein Ris CF claim 7 , Cl or CFCF.9. The compound according to or claim 7 , wherein Ris F claim 7 , CHor OCH.10. The compound according to any one of to claim 7 , wherein Ris F.11. The compound according to any one of to claim 7 , wherein X is —PO(OH).12. The compound according to any one of to claim 7 , wherein X is —PO(OH)OM claim 7 , —PO(O).2M claim 7 , or —PO(O).D; M is Li claim 7 , Na or K and D is Mg or Ca.13. The compound according to claim 7 , wherein the compound is (4-(2-(4-fluoro-2-methylphenoxy)-4-(trifluoromethyl)benzamido)-2-oxopyridin-1(2H)-yl)methyl dihydrogen phosphate.14. The compound according to claim 7 , wherein the compound is (4-(2-(4-fluoro-2-methoxyphenoxy)-4-(perfluoroethyl)benzamido)-2-oxopyridin-1(2H)-yl)methyl dihydrogen phosphate.15. The compound according to claim 7 , wherein the compound is (4-(4-chloro-2-(4-fluoro-2-methylphenoxy)benzamido)-2-oxopyridin-1(2H)-yl)methyl dihydrogen phosphate.17. The compound according to claim 16 , wherein the compound is (4-(2-(4-fluoro-2-methylphenoxy)-5-(trifluoromethyl)benzamido)-2-oxopyridin-1(2H)-yl)methyl dihydrogen phosphate.19. The compound according to claim 18 , wherein the compound is (4-(2-(4-fluorophenoxy)-5-(trifluoromethyl)benzamido)-2-oxopyridin-1(2H)-yl)methyl dihydrogen phosphate.21. The compound according to claim 20 , wherein the compound is (4-(4 claim 20 ,5-dichloro-2-(4-fluoro-2-me thoxyphenoxy)benzamido)-2- ...

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15-02-2018 дата публикации

ELECTROCHROMIC COMPOUND, ELECTROCHROMIC COMPOSITION, ELECTROCHROMIC ELEMENT, AND ELECTROCHROMIC DIMMING ELEMENT

Номер: US20180044581A1
Принадлежит:

To provide an electrochromic compound represented by the following general formula (1) where Xand Xare each independently a carbon atom or a nitrogen atom, R, Rand Rare each independently a halogen atom, a substituted or unsubstituted alkyl group, or a substituted or unsubstituted alkoxy group, x is an integer selected from 0 through 3, y and z are each independently an integer selected from 0 through 4, and at least one of Land Lis a monovalent functional group bonded to a nitrogen atom of a pyridinium ring directly, or via a divalent substituent. 2. The electrochromic compound according to claim 1 ,{'sup': 1', '3', '1', '2, 'wherein at least one selected from the group consisting of Rto Rand Land Lcomprises a functional group capable of directly or indirectly bonding to a hydroxyl group.'}3. The electrochromic compound according to claim 2 ,{'sup': 1', '2, 'wherein at least one of Land Lcomprises a functional group capable of directly or indirectly bonding to a hydroxyl group.'}4. The electrochromic compound according to claim 2 ,wherein the functional group is a phosphonic acid group, a phosphoric acid group, a carboxylic acid group, a silyl group, or a silanol group.5. An electrochromic composition claim 2 , comprising:a conductive or semiconductive nanostructure; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the electrochromic compound according to ,'}wherein the electrochromic compound is optionally bonded to or adsorbed on the conductive or semiconductive nanostructure.7. The electrochromic element according to claim 6 ,wherein the first electroactive layer comprises a mixture of:{'sup': 1', '2, 'the electrochromic compound, where both Land Lcomprise a monovalent functional group bonded to a nitrogen atom of a pyridinium ring directly, or via a divalent substituent, and'}{'sup': 1', '2, 'the electrochromic compound, where either Lor Lcomprises a monovalent functional group bonded to a nitrogen atom of a pyridinium ring directly, or via a divalent ...

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25-02-2016 дата публикации

Biological buffers with wide buffering ranges

Номер: US20160052868A1
Автор: Thomas P. Daly
Принадлежит: TPAT IP LLC

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability.

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25-02-2016 дата публикации

BIS(6-METHYL-3-SULPHOPHENYL)PHENYLPHOSPHINE, AMMONIUM SALT THEREOF, AND METHOD FOR PRODUCING SAME

Номер: US20160052947A1
Принадлежит:

Provided are a water-soluble triarylphosphine for a palladium catalyst, which has high selectivity in a telomerization reaction and can be recovered with efficiency, an ammonium salt thereof, and a method for efficiently producing the same. Specifically, provided are bis(6-methyl-3-sulphophenyl)phenylphosphine; a bis(6-methyl-3-sulphonatophenyl)phenylphosphine diammonium salt obtained by reacting the phosphine with a tertiary amine having a total of 3 to 27 carbon atoms in groups bonded to one nitrogen atom; and a method for producing the same. 1. Bis(6-methyl-3-sulphophenyl)phenylphosphine.2. A bis(6-methyl-3-sulphonatophenyl)phenylphosphine diammonium salt obtained by a process comprising: reacting the bis(6-methyl-3-sulphophenyl)phenylphosphine of with a tertiary amine comprising a total of 3 to 27 carbon atoms in groups bonded to one nitrogen atom.3. The bis(6-methyl-3-sulphonatophenyl)phenylphosphine diammonium salt of claim 2 , wherein the tertiary amine is trimethylamine claim 2 , triethylamine claim 2 , tripropylamine claim 2 , triisopropylamine claim 2 , tributylamine claim 2 , triisobutylamine claim 2 , tri-s-butylamine claim 2 , tri-t-butylamine claim 2 , tripentylamine claim 2 , triisopentylamine claim 2 , trineopentylamine claim 2 , trihexylamine claim 2 , triheptylamine claim 2 , trioctylamine claim 2 , triphenylamine claim 2 , tribenzylamine claim 2 , N claim 2 ,N-dimethylethylamine claim 2 , N claim 2 ,N-dimethylpropylamine claim 2 , N claim 2 ,N-dimethylisopropylamine claim 2 , N claim 2 ,N-dimethylbutylamine claim 2 , N claim 2 ,N-dimethylisobutylamine claim 2 , N claim 2 ,N-dimethyl-s-butylamine claim 2 , N claim 2 ,N-dimethyl-t-butylamine claim 2 , N claim 2 ,N-dimethylpentylamine claim 2 , N claim 2 ,N-dimethylisopentylamine claim 2 , N claim 2 ,N-dimethylneopentylamine claim 2 , N claim 2 ,N-dimethylhexylamine claim 2 , N claim 2 ,N-dimethylheptylamine claim 2 , N claim 2 ,N-dimethyloctylamine claim 2 , N claim 2 ,N-dimethylnonylamine claim 2 , ...

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25-02-2016 дата публикации

BIS(6-METHYL-3-SULPHOPHENYL)(2-METHYLPHENYL)PHOSPHINE, AMMONIUM SALT THEREOF, AND METHOD FOR PRODUCING SAME

Номер: US20160052948A1
Принадлежит:

Provided are a water-soluble triarylphosphine for a palladium catalyst, which has high selectivity in a telomerization reaction and is easily recovered with efficiency, an ammonium salt thereof, and a method for efficiently producing the same. Specifically, provided are bis(6-methyl-3-sulphophenyl)(2-methylphenyl)phosphine; a bis(6-methyl-3-sulphonatophenyl)(2-methylphenyl)phosphine diammonium salt obtained by reacting the phosphine with a tertiary amine having a total of 3 to 27 carbon atoms in groups bonded to one nitrogen atom; and a method for producing the same. 21. A bis(6-methyl-3-sulphonatophenyl)(2-methylphenyl)phosphine diammonium salt obtained by reacting the bis(6-methyl-3-sulphophenyl)(2-methylphenyl)phosphine of claim with a tertiary amine having a total of 3 to 27 carbon atoms in groups bonded to one nitrogen atom.3. The bis(6-methyl-3-sulphonatophenyl)(2-methylphenyl)phosphine diammonium salt of claim 2 ,wherein the tertiary amine is trimethylamine, triethylamine, tripropylamine, triisopropylamine, tributylamine, triisobutylamine, tri-s-butylamine, tri-t-butylamine, tripentylamine, triisopentylamine, trineopentylamine, trihexylamine, triheptylamine, trioctylamine, triphenylamine, tribenzylamine, N,N-dimethylethylamine, N,N-dimethylpropylamine, N,N-dimethylisopropylamine, N,N-dimethylbutylamine, N,N-dimethylisobutylamine, N,N-dimethyl-s-butylamine, N,N-dimethyl-t-butylamine, N,N-dimethylpentylamine, N,N-dimethylisopentylamine, N,N-dimethylneopentylamine, N,N-dimethylhexylamine, N,N-dimethylheptylamine, N,N-dimethyloctylamine, N,N-dimethylnonylamine, N,N-dimethyldecylamine, N,N-dimethylundecylamine, N,N-dimethyldodecylamine, N,N-dimethylphenylamine, N,N-dimethylbenzylamine, N,N-diethylmonomethylamine, N,N-dipropylmonomethylamine, N,N-diisopropylmonomethylamine, N,N-dibutylmonomethylamine, N,N-diisobutylmonomethylamine, N,N-di-s-butylmonomethylamine, N,N-di-t-butylmonomethylamine, N,N-dipentylmonomethylamine, N,N-diisopentylmonomethylamine, N,N- ...

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26-02-2015 дата публикации

FLUORINE-CONTAINING PHOSPHATE ESTER-AMIDE, AND FLAME RETARDANT RESIN, FLAME RETARDANT LIQUID AND FLAME RETARDANT SOLVENT FOR ORGANIC SYNTHESIS CONTAINING SAME

Номер: US20150053901A1
Принадлежит: TOSOH F- TECH, INC.

[Problem] To provide a fluorine-containing phosphate ester-amide which has high flame retardancy such as exhibiting flame retardant effects at a small quantity of addition, and sufficient hydrolysis resistance. 3. A flame retardant resin containing the fluorine-containing phosphate ester-amide represented by the general formula (1) and/or the fluorine-containing phosphate ester-amide represented by the general formula (2).4. A flame retardant liquid containing a fluorine-containing phosphate ester-amide represented by the general formula (1) and/or the fluorine-containing phosphate ester-amide represented by the general formula (2).5. A flame retardant solvent for organic synthesis claim 4 , consisting of the fluorine-containing phosphate ester-amide represented by the general formula (1) and/or the fluorine-containing phosphate ester-amide represented by the general formula (2) or the flame retardant liquid according to . The present invention relates to fluorine-containing phosphate ester-amides. More particularly, the present invention relates to a fluorine-containing phosphate ester-amide having high hydrolysis resistance and useful in applications such as flame retardants for resins, flame retardants for flammable liquids, flame retardant solvents for organic synthesis, flame retardant solvents for secondary battery electrolytes, flame retardant hydraulic fluids, flame retardant lubricants, flame retardant extractants, and flame retardant cleaning agents. The present invention also relates to a flame retardant resin, a flame retardant liquid, and a flame retardant solvent for organic synthesis, each of which contains the fluorine-containing phosphate ester-amide.Phosphate esters and other phosphate esters such as phosphate ester-amides have excellent flame retardancy and self-extinguishing properties resulting from phosphorus atoms and are therefore widely used as flame retardants for various resins (for example, Patent Literatures 1 to 3).As the flame ...

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13-02-2020 дата публикации

PHOSPHOROUS DERIVATIVES AS KINASE INHIBITORS

Номер: US20200048288A1
Принадлежит:

The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use. 2. The compound of in which Xis N.3. The compound of in which Xis N and Xis CR.4. The compound of in which Xis CRand Xis CR.5. The compound of in which Xis CR.6. The compound of in which Xis N and Xis CR.7. The compound of in which Xis CRand Xis CR.8. The compound of any of claim 5 , claim 5 , claim 5 , or in which Ris selected from Cl claim 5 , F claim 5 , C1-C4 alkyl claim 5 , trihaloalkyl claim 5 , cycloalkyl claim 5 , C2-C4 alkenyl claim 5 , and alkynyl.9. The compound of in which Xis CRand Xis CRwherein Rand R claim 1 , together with the atoms to which they are attached claim 1 , form a fused claim 1 , 5- claim 1 , 6- or 7-membered saturated claim 1 , partially saturated or unsaturated ring claim 1 , which contains 0-4 heteroatoms selected from N claim 1 , O and S(O) claim 1 , and which may bear up to four substituents.10. The compound of any of - in which s is 1 claim 1 , 2 claim 1 , 3 or 4 claim 1 , and each of the substituents Ris independently selected from halo claim 1 , —R claim 1 , —OR claim 1 , —NRRand —P(═O)(R) claim 1 , wherein each Rand Rmoiety may be further substituted or unsubstituted.11. The compound of in which at least one substituent Ris —ORand Ris selected from C1-C6 alkyl claim 10 , C1-C6 alkenyl claim 10 , and C2-C6 alkynyl.12. The compound of or in which at least one substituent Ris a 5- claim 10 , 6- or 7-membered heterocyclic or 5- or 6-membered heteroaryl moiety claim 10 , linked to Ring A either directly or by an ether bond claim 10 , and which may be further substituted with 1-3 substituents independently selected from halo claim 10 , —CN claim 10 , —NO claim 10 , —R claim 10 , —OR claim 10 , —O—NRR claim 10 , —NRR claim 10 , —NR—NRR claim 10 , —NR—OR claim 10 , —C(O)YR claim 10 , —OC(O)YR claim 10 , —NRC(O)YR claim 10 , —SC(O)YR claim 10 , —NRC(═S)YR claim 10 , —OC(═S)YR claim 10 , —C(═S)YR ...

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22-02-2018 дата публикации

Functionalized phosphonates via michael addition

Номер: US20180051044A1
Принадлежит: Nevada System of Higher Education NSHE

Provided herein are functionalized phosphonates and methods for making same via phosphite addition to an atom alpha to an electron withdrawing group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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10-03-2022 дата публикации

PREPARATION OF PSILOCYBIN, DIFFERENT POLYMORPHIC FORMS, INTERMEDIATES, FORMULATIONS AND THEIR USE

Номер: US20220073548A1
Принадлежит: COMPASS PATHFINDER LIMITED

This invention relates to the large-scale production of psilocybin for use in medicine. Move particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin. 130-. (canceled)31. A method of treating treatment resistant depression , the method comprising orally administering a therapeutically effective amount of an oral dosage form , wherein the oral dosage form comprises:a crystalline Hydrate A of psilocybin characterized by XRPD peaks at 8.9±0.1, 13.8±0.1, 19.4±0.1, 23.1±0.1 and 23.5±0.1 °2θ, wherein the psilocybin has a chemical purity of greater than 97% as determined by HPLC analysis anda pharmaceutically acceptable excipient.32. The method of claim 31 , wherein about 1 mg to about 40 mg of the crystalline Hydrate A of psilocybin is administered.33. The method of claim 31 , wherein about 10 mg to about 30 mg of the crystalline Hydrate A of psilocybin is administered.34. The method of claim 31 , wherein about 1 mg of the crystalline Hydrate A of psilocybin is administered.35. The method of claim 31 , wherein about 5 mg of the crystalline Hydrate A of psilocybin is administered.36. The method of claim 31 , wherein about 10 mg of the crystalline Hydrate A of psilocybin is administered.37. The method of claim 31 , wherein about 25 mg of the crystalline Hydrate A of psilocybin is administered.38. The method of claim 31 , wherein the oral dosage form is a capsule.39. The method of claim 31 , wherein the oral dosage form is a tablet.40. The method of claim 31 , wherein the Hydrate A is further characterized by at least one peak selected from the group consisting of 6.5±0.1 claim 31 , 12.2±0.1 claim 31 , 12.6±0.1 claim 31 , 16.2±0.1 claim 31 , 20.4±0.1 claim 31 , 20.8±0.1 claim 31 , and 21.5±0.1 °2θ.41. The method of claim 31 , wherein the psilocybin has no ...

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01-03-2018 дата публикации

IONIC LIQUID FOR FORWARD OSMOSIS PROCESS AND FORWARD OSMOSIS PROCESS

Номер: US20180056241A1

A forward osmosis process is provided, which includes separating a feed part and a draw solution part by a semi-permeable film. An ionic liquid is introduced into the draw solution part, and brine is introduced into the feed part. The brine has an osmotic pressure lower than that of the ionic liquid, so that pure water of the brine permeates through the semi-permeable film, enters the draw solution part, and mixes with the ionic liquid to form a draw solution. The draw solution was obtained out of the draw solution part to be left to stand at room temperature, so that the draw solution separated into a water layer and an ionic liquid layer. The ionic liquid includes 14-. (canceled)68-. (canceled)10. (canceled)12. (canceled)13. The forward osmosis process as claimed in claim 5 , further comprising introducing the ionic liquid layer into the draw solution part after the step of separating the draw solution into the water layer and the ionic liquid layer14. The forward osmosis process as claimed in claim 5 , wherein the step of introducing the brine into the feed part is continuously introducing seawater into the feed part.15. The forward osmosis process as claimed in claim 5 , further comprising a step of stirring the pure water and the ionic liquid in the draw solution part for mixing the pure water and the ionic liquid to form the draw solution. This application claims the benefit of U.S. Provisional Application No. 62/381,187 filed on Aug. 30, 2016, and claims priority from Taiwan Application Serial Number 105139655 filed on Dec. 1, 2016, the entirety of which are incorporated by reference herein.The technical field relates to a draw solute (ionic liquid) for a forward osmosis process.The technical principle of forward osmosis (FO) desalination process utilizes an osmosis pressure difference (between two solutions/solutes in two parts separated by a semi-permeable film) as a driving force. Water in a feed part with a lower osmosis pressure will permeate through a ...

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02-03-2017 дата публикации

Ether Compounds for Treatment of Medical Disorders

Номер: US20170057993A1
Принадлежит: Achillion Pharmaceuticals Inc

Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R 12 or R 13 on the A group is an ether substituent (R 32 ) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

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04-03-2021 дата публикации

Composition, Film, Laminate Structure, Light-Emitting Device, and Display

Номер: US20210061829A1
Автор: Mase Kentaro, Naito Shota
Принадлежит: Sumitomo Chemical Company, Limited

Provided is a composition having high thermal durability containing a perovskite compound. 2. The composition according to claim 1 , wherein the component (3) is at least one selected from the group consisting of a compound represented by the formula (X1) and a compound represented by the formula (X6).3. A film using the composition according to or .4. A laminated structure comprising the film according to .5. A light emitting device comprising the laminated structure according to .6. A display comprising the laminated structure according to . The present invention relates to a composition, a film, a laminate structure, a light emitting device, and a display.An LED backlight having a blue LED (light emitting diode) and a composition having luminescence has been developed. In recent years, perovskite compounds have attracting attention as a compound having luminescence contained in the composition (Non-Patent Document 1).However, when a composition containing a perovskite compound as described in Non-Patent Document 1 is used as a light emitting material, further improvement in thermal durability is required.The present invention has been made in view of the above-mentioned problem, and has an object of providing a composition having high thermal durability containing a perovskite compound.In order to solve the above problem, the present inventors have intensively studied, and resultantly reached the following present invention.That is, the present invention includes the following [1] to [6].[1] A composition comprising the following components (1), (2), and (3):(1) Component: perovskite compound having A, B, and X: (A indicates a component positioned at each vertex of a hexahedron having B at the center in a perovskite type crystal structure and is a monovalent cation.B indicates a component positioned at the centers of the hexahedron where A is disposed at each vertex and the octahedron where X is disposed at each vertex in the perovskite type crystal structure and ...

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05-03-2015 дата публикации

PHOSPHONATE DERIVATIVES AND METHODS OF USE THEREOF IN THE TREATMENT OF ALZHEIMER'S DISEASE

Номер: US20150065463A1
Принадлежит: University of Kansas

Benzothiazole phosphonate analogs and methods of using the same to inhibit the activity of Amyloid Binding Alcohol Dehydrogenase and in the amelioration or treatment of Alzheimer's disease are provided. 4. A pharmaceutical composition comprising the ABAD inhibitor of and a pharmaceutically acceptable carrier.5. A method for inhibiting the activity of Amyloid Binding Alcohol Dehydrogenase (ABAD) comprising contacting ABAD with an inhibitor of thereby inhibiting the activity of ABAD.6. A method for ameliorating or treating Alzheimer's Disease comprising administering to a subject in need thereof the pharmaceutical composition of thereby ameliorating or treating the subject's Alzheimer's Disease. This application is a continuation-in-part application of PCT/US2013/040707, filed May 13, 2013, which claims the benefit of priority from U.S. Patent Application Ser. No. 61/646,548, filed May 14, 2012, the content of which is incorporated herein by reference in its entirety.This invention was made with government support under Grant Nos. R01GM095355, R37AG037319, and PO1AG017490 awarded by National Institute of General Medical Sciences and the National Institute on Aging. The government has certain rights in the invention.Alzheimer's disease (AD) is one of the most common dementia showing slowly progressive cognitive decline. Alzheimer's brain is characterized by accumulation of amyloid beta peptide (Aβ) and the formation of neurofibrillary tangles. Aβ plays a central role in the development of AD pathology and contributes to neuronal, synaptic, and cognitive malfunction. Mitochondrial and synaptic dysfunction is an early pathological feature of Alzheimer's disease brain (Du, et al. (2010) 107:18670; Du, et al. (2011) . doi:10.1089/ars.2011.4277; Chen, et al. (2010) 20 Suppl 2: S569; Caspersen, et al. (2005) 19:2040; Reddy, et al. (2008) 14:45; Lin & Beal (2006) 12:1241). Studies have highlighted the significance of mitochondrial Aβ accumulation and synaptic mitochondrial ...

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05-03-2015 дата публикации

PHOSPHOROUS COMPOUND AND TRANSITION METAL COMPLEX THEREOF

Номер: US20150065738A1
Принадлежит: TAKASAGO INTERNATIONAL CORPORATION

The present invention provides a phosphorous compound represented by general formula (1), and transition metal complexes containing such phosphorous compounds as ligands: 2. The phosphorous compound according to claim 1 , wherein Z is selected from the group consisting of an oxy group claim 1 , a thio group claim 1 , imino groups optionally having substitutent(s) claim 1 , methylene groups optionally having substitutent(s) claim 1 , and ethylene groups optionally having substitutent(s).3. The phosphorous compound according to which is an optically active substance.4. The phosphorous compound according to claim 1 , wherein Y is a lone electron pair.5. A transition metal complex comprising the phosphorous compound according to as a ligand.6. The transition metal complex according to claim 5 , comprising a transition metal selected from the group consisting of iron claim 5 , cobalt claim 5 , nickel claim 5 , copper claim 5 , ruthenium claim 5 , rhodium claim 5 , palladium claim 5 , silver claim 5 , osmium claim 5 , iridium claim 5 , platinum claim 5 , and gold. The present invention relates to a novel phosphorous compound and a transition metal complex containing the phosphorous compound as a ligand.Today, various transition metal complexes composed of transition metal species and ligands are used as catalysts of organic synthesis reactions. It is well known that not only transition metal species but also ligands of complexes play important roles as factors of exhibiting the performance or activity of such catalysts. For this reason, heretofore, numerous coordination compounds including phosphorous compounds have been developed as ligands. Furthermore, when an organic synthesis reaction is carried out using a complex catalyst, it is possible to construct optimum catalysts for a variety of substrates by appropriately combining transition metal species and ligands. Hence, the research and development are still actively conducted at present. It is needless to say that the ...

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10-03-2016 дата публикации

PHOSPHORUS FUNCTIONAL ANTIMICROBIAL COATINGS FOR METAL SURFACES

Номер: US20160066579A1
Принадлежит:

The invention relates to quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, processes for preparing quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, antimicrobial coating compositions comprising quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds and method of treating a surface with said compositions to provide a durable, antimicrobial-treated surface. 1150.-. (canceled)152. The process of wherein Rand Rare methyl.153. The process of wherein R is ethyl.154. The process of wherein n is 1 or 2.155. The process of wherein m is 17.156. The process of wherein R claim 151 , Rand Rare the same and methyl.157. The process of wherein Z is chloro or triflate.158. The process of wherein X is bromo.160. The process of wherein R is the same and ethyl.161. The process of wherein Rand Rare methyl.162. The process of wherein n is 1 or 2.163. The process of wherein m is 17.164. The process of wherein Z is bromo.165. The process of wherein the alkali carbonate is potassium carbonate.167. The process of wherein R is the same and ethyl.168. The process of wherein n is 1 or 2.169. The process of wherein the polar claim 166 , aprotic solvent is selected from the group consisting of acetonitrile claim 166 , dimethylformamide and dichloromethane.171. The process of wherein R is ethyl.172. The process of wherein Rand Ris methyl.173. The process of wherein n is 1 or 2.174. The process of wherein p is 1 or 2.175. The process of wherein Z is bromo.176. The process of wherein the polar claim 170 , aprotic solvent is selected from the group consisting of acetonitrile claim 170 , dimethylformamide and dichloromethane.178. The coating composition of wherein: in formula (I) claim 177 , Rand Rare methyl claim 177 , in is 17 claim 177 , n is 1 or 2 and X is bromo; and in formulas (XIV) and (XXVIII) claim 177 , R is the same and hydrogen claim 177 , Rand Rare methyl claim 177 , in is 17 ...

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22-05-2014 дата публикации

TELOMERASE ACTIVATING COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20140142068A1

The present invention is directed to use of a series of compounds and compositions comprising the same for activating telomerase and treating diseases, disorders and/or conditions related thereto. 3. The method of claim 1 , wherein said cell or tissue is contacted with a pharmaceutical compound and a pharmaceutical acceptable carrier. This application is a Division of U.S. patent application Ser. No. 12/602,956, filed Jun. 17, 2010, which in turn is a 371 of PCT International Application No. PCT/IL2008/000756, filed Jun. 4, 2008, which claims the benefit of U.S. Provisional Application Nos. 60/924,875, filed Jun. 4, 2007, 60/929,524, filed Jul. 2, 2007, 60/929,525, filed Jul. 2, 2007 and 61/006,924, filed Feb. 6, 2008. The disclosures of all applications are herein incorporated by reference.The present invention is directed to use of a series of compounds and compositions comprising the same for enhancing expression and/or activating telomerase and for treating diseases, disorders and/or conditions related thereto.Telomerase is a ribonucleoprotein that catalyzes the addition of telomeric repeats to the ends of telomeres. Telomeres are long stretches of repeated sequences that cap the ends of chromosomes. In humans, telomeres are typically 7-10 kb in length and comprise multiple repeats. Telomerase is not expressed in most adult cells, and telomere length decreases with successive rounds of replicationTelomerase acts as reverse transcriptase in the elongation of telomeres, which prevent the loss of telomeres due to the end replication problems. Without telomerase the telomeres are shortened at each cell division which leads to senescence, apoptosis and cell death caused by chromosome instability. Telomerase is inactive in somatic cells but active in 90% of cancer cells, where telomerase is reactivated. Although telomerase activation may be dangerous, because it can mimic the cancer development process, telomerase enhancing agents may be theoretically applicable as ...

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22-05-2014 дата публикации

Cross-linking and stabilization of organic metal complexes in networks

Номер: US20140142258A1
Принадлежит: CYNORA GmbH

The invention relates to the preparation of an organic transition metal complex cross-linked into a multi-dimensional network, comprising the performance of a first reaction, which comprises a first reactant in the form of an organic metal complex and a second reactant for the formation of a multi-dimensional network, where the organic metal complex is cross-linked to form the multi-dimensional-network during the reaction.

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28-02-2019 дата публикации

IONIC TAGS FOR SYNTHESIS OF OLIGORIBONUCLEOTIDES

Номер: US20190062355A1
Принадлежит:

The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II): 15-. (canceled)6. An ionic tag linker comprising a photolabile moiety , an ionic moiety and a linker.7. The ionic tag linker of claim 6 , wherein the photolabile moiety is a nitrobenzyl derivative.9. The ionic tag linker of claim 6 , wherein the linker is alkyl claim 6 , glycol or functionalized alkyl.10. The ionic tag linker of claim 6 , wherein the ionic moiety is an imidazolium or phosphonium group; or wherein the ionic moiety comprises a halide; or wherein the ionic moiety comprises Br claim 6 , Cl or I.11. The ionic tag linker of claim 6 , wherein the photolabile moiety is cleavable by photolysis.12. The ionic tag linker of claim 6 , wherein the ionic tag linker is orthogonally cleavable.1356-. (canceled) This application is a Continuation of application Ser. No. 14/240,067 filed May 29, 2014, which is a 371 application of International PCT Application No. PCT/CA2012/000784 filed Aug. 23, 2012, which claims priority to U.S. Provisional Application No. 61/602,373 filed Feb. 23, 2012 and International PCT Application No. PCT/CA2011/000950 filed Aug. 23, 2011, all of which are hereby incorporated by reference in their entirety.The invention relates to the chemical synthesis of oligonucleotides, in particular oligoribonucleotides, in particular solution phase synthesis.The demand for synthetic oligonucleotides has grown exponentially as genome sequencing, functional genomics, and PCR-based detection methods consume enormous quantities of DNA oligonucleotides. In addition, the potential success of new DNA- and RNA-based therapeutic platforms (such as antisense and siRNA gene silencing strategies) currently undergoing clinical trials could result in an unprecedented demand for short synthetic DNA and RNA molecules.RNA interference (RNAi) as potential therapeutics represents a fundamentally new way to ...

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08-03-2018 дата публикации

Water soluble fluorescent or colored dyes comprising conjugating groups

Номер: US20180065998A1
Принадлежит: Sony Corp, Sony Corp of America

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , L 1 , L 3 , L 4 , L 6 , L 7 , L 8 , M 1 , M 2 , q, w and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

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11-03-2021 дата публикации

ENANTIOPURE TERPHENYLS WITH TWO ORTHO-ATROPISOMERIC AXES

Номер: US20210070785A1
Принадлежит:

Enantiopure terphenyl presenting two ortho-located chiral axes having the following structural formula (I): their process of synthesis and their use as mono or bidentate ligands for asymmetric organometallic reactions, as organocatalysts, as chiral base and as generator, with metal, of isolable chiral metallic complexes for applications in asymmetric catalysis and others. 2. The enantiopure terphenyl according to claim 1 , wherein{'sub': '1', 'claim-text': an halogen atom,', 'a substituted or unsubstituted branched or straight alkyl group or', 'a substituted or unsubstituted branched or straight alkoxy group or', {'sub': '3', 'a CFgroup,'}], 'Rrepresents'}{'sub': '2', 'claim-text': a hydrogen atom or', 'a substituted or unsubstituted branched or straight alkyl group, or', 'a substituted or unsubstituted branched or straight alkoxy group, 'Rrepresents'}{'sub': '3', 'claim-text': a substituted or unsubstituted branched or straight alkyl group or', 'a substituted or unsubstituted branched or straight alkoxy group,, 'Rrepresents'}{'sub': '4', 'claim-text': a hydrogen atom or', 'a halogen atom or', 'a substituted or unsubstituted branched or straight alkoxy group, or', 'a substituted or unsubstituted branched or straight alkyl group or', 'a aryl group or', {'sub': 2', '2', 'n+2, 'a CHF group, or a CHFgroup or —CnFgroup avec n=1 à 10, or'}], 'Rrepresents'}{'sub': '5', 'claim-text': [{'sub': a', 'a', '1', '4, 'a SORgroup with Rselected from a substituted or unsubstituted branched or straight-(C-C) alkyl group or a substituted or unsubstituted aryl group, or'}, 'a OH group, or', {'sub': a', 'd', 'a', 'd', 'a', 'd, '—PRnor a —P(O)Rnwith Rand Rindependently selected from a substituted or unsubstituted branched or straight alkyl group or a substituted or unsubstituted aryl group,'}], 'Rrepresents'}{'sub': '6', 'claim-text': a hydrogen atom,', 'a halogen atom or', {'sub': 1', '4, 'a substituted or unsubstituted branched or straight-(C-C) alkyl group or'}, {'sub': 1', '4, 'a ...

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11-03-2021 дата публикации

PHOSPHONIUM-BASED ZWITTERIONIC MONOMERS AND POLYMERS, AND COMPOSITIONS AND METHODS THEREOF

Номер: US20210070786A1
Принадлежит:

The invention provides novel zwitterionic monomers and polymers (including copolymers) with pendent phosphonium-based zwitterionic moieties, and compositions and products comprising same, as well as related methods and uses of the compositions, for example, as surfactants, coatings, and interlayer materials, biomedical materials or agents. 2. The compound of claim 1 , wherein Ris H.3. The compound of claim 1 , wherein Ris a methyl group.4. The compound of claim 1 , wherein each Ris a C-Calkyl group.5. The compound of claim 4 , wherein each Ris a C-Calkyl group.6. The compound of claim 4 , wherein each Ris a C-Calkyl group.7. The compound of claim 1 , wherein each Ris an aryl group.8. The compound of claim 7 , wherein each Ris a phenyl group.9. The compound of claim 1 , wherein the Rs are the same.10. The compound of claim 1 , wherein the Rs are not the same.11. The compound of claim 1 , wherein i is 1.12. The compound of claim 11 , wherein j is an integer selected from 0-3.1422-. (canceled)24. The polymer of claim 23 , wherein Ris H.25. The polymer of claim 23 , wherein Ris a methyl group.26. The polymer of claim 23 , wherein each Ris a C-Calkyl group.27. (canceled)28. (canceled)29. The polymer of claim 23 , wherein each Ris an aryl group.3032-. (canceled)33. The polymer of claim 23 , wherein i is 1.34. The polymer of claim 33 , wherein j is an integer selected from 0-3.3556-. (canceled) This application claims the benefit of priority to U.S. Provisional Application No. 62/897,479, filed Sep. 9, 2019, the entire content of each of which is incorporated herein by reference for all purposes.This invention was made with government support under Grant No. NSF-CHE-CCI-1740630 awarded by the National Science Foundation. The Government has certain rights in the invention.The invention generally relates to chemicals and polymers. More particularly, the invention relates to zwitterionic monomers and polymers (including copolymers) with pendent phosphonium-based zwitterionic ...

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17-03-2016 дата публикации

TAMOXIFEN DERIVATIVES FOR TREATMENT OF NEOPLASTIC DISEASES, ESPECIALLY WITH HIGH HER2 PROTEIN LEVEL

Номер: US20160075726A1
Принадлежит:

The subject of the invention are new mitochondrially targeted E/Z isomers of aliphatic triphenylphosphonium derivatives of tamoxifen where the aliphatic chain is alkyl or alkenyl, and their corresponding tertiary amine salts and/or their mixture (MitoTAX). Alkyl triphenylphosphonium derivatives of tamoxifen have the general formula (I), where n=8 to 12 and where Z is selected from the group of organic salts or inorganic salts. Alkenyl triphenylphosphonium derivatives of tamoxifen have the general formula IA, where n=6 to 10 and where Z has the above mentioned meaning. These compounds are applicable for the treatment of neoplastic disease, especially those with high HER2 protein levels. The drug for the treatment of neoplastic diseases according to the invention contains at least one E/Z isomer of aliphatic triphenylphosphonium derivatives of tamoxifen of the general formula (I) and/or IA or their corresponding salts of tertiary amine. 114.-. (canceled)16. The mitochondrially targeted E/Z isomer of an aliphatic triphenylphosphonium derivative of tamoxifen of general formula I or IA according to claim 15 , wherein Z is selected from the group consisting of citrate claim 15 , acetate claim 15 , lactate claim 15 , tartrate claim 15 , oxalate claim 15 , ascorbate claim 15 , mesylate claim 15 , tosylate claim 15 , sulphate claim 15 , halogenide claim 15 , phosphate claim 15 , and mixtures thereof.20. A method of treating neoplastic disease using the mitochondrially targeted E/Z isomer of an aliphatic triphenylphosphonium derivative of tamoxifen of general formula I or IA according to .21. The method according to claim 20 , wherein the neoplastic disease is selected from the group consisting of carcinoma claim 20 , sarcoma claim 20 , lymphoma and leukemia.22. The method according to claim 20 , wherein the neoplastic disease is selected from the group consisting of astrocytoma claim 20 , neuroblastoma claim 20 , glioblastoma claim 20 , mesothelioma claim 20 , breast cancer ...

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17-03-2016 дата публикации

RADICAL ORBITAL SWITCHING

Номер: US20160075732A1
Принадлежит: THE AUSTRALIAN NATIONAL UNIVERSITY

Described herein are distonic radical anion species of formula (I): RAD-L-NEG; wherein RAD is a group comprising a radical; NEG is a group comprising an anion, which is capable of bonding to a proton or other cation; L is a linker that links NEG to RAD; and the radical of RAD is not π-conjugated to the anion of NEG. 194-. (canceled)96. The structure of Formula (I) as defined in claim 95 , wherein the lowest Singly-Occupied Molecular Orbital (SOMO) of RAD is lower in energy than a Doubly-Occupied Molecular Orbital (DOMO) of NEG; and wherein the SOMO of RAD is higher in energy than the DOMOs of NEG when the negative point charge of NEG is neutralized.97. The structure of Formula (I) as defined in claim 95 , wherein NEG is a surface or structure capable of bearing and/or carrying a negative point charge claim 95 , and where the negative point charge is capable of being neutralised claim 95 , wherein the structure capable of bearing and/or carrying a negative point charge is optionally selected from the group comprising: an electrode claim 95 , a metallic or non-metallic structure claim 95 , or graphene.98. The structure of Formula (I) as defined in claim 95 , wherein the negative point charge is selected from the group comprising an electron claim 95 , an electric charge claim 95 , a negative potential claim 95 , or a negative coulombic charge; and where the negative point charge is capable of being neutralised by the substantial removal claim 95 , dissipation or inversion of that charge.99. The structure of Formula (I) as defined in claim 95 , wherein the negative point charge is a group comprising an anion claim 95 , which is capable of being neutralised by bonding to a proton or other cation claim 95 , wherein the anion optionally comprises a sterically and/or electronically destabilised anion.100. The structure of Formula (I) as defined in claim 99 , where neutralisation is achieved by:removal of the proton or other cation bonded to the anion of NEG;increasing the ...

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24-03-2022 дата публикации

INHIBITORS OF THE ENZYME ENOLASE FOR PRECISION ONCOLOGY

Номер: US20220089620A1

Provided herein are compounds of the formula: wherein the variables are defined herein. The present disclosure also provides pharmaceutical compositions comprising the compounds disclosed herein as well as methods of treatment using the compounds and/or compositions disclosed herein. Such compounds and compositions may be used, for example, for the inhibition of enolase enzymes. 5. The compound of claim 1 , wherein X is —O—.6. The compound of claim 1 , wherein Ris hydrogen.7. The compound according to any one of - claim 1 , wherein Ris acylor substituted acyl.8. The compound according to any one of - claim 1 , wherein Ris acyl.9. The compound according to any one of - claim 1 , wherein Ris acetyl.10. The compound according to any one of - claim 1 , wherein Ris hydrogen.11. The compound according to any one of - claim 1 , wherein Ris hydrogen.12. The compound according to any one of - claim 1 , wherein Ris aralkyl claim 1 , substituted aralkyl claim 1 , heteroaralkyl claim 1 , or substituted heteroaralkyl.13. The compound according to any one of - and claim 1 , wherein Ris heteroaralkylor substituted heteroaralkyl.14. The compound according to any one of - claim 1 , claim 1 , and claim 1 , wherein Ris substituted heteroaralkyl.15. The compound according to any one of - and - claim 1 , wherein Ris (5-nitrofuran-2-yl)methyl claim 1 , (1-methyl-2-nitro-1H-imidazol-5-yl)methyl claim 1 , or (5-nitrothiophen-2-yl)methyl.16. The compound according to any one of - claim 1 , wherein Ris alkylor substituted alkyl.17. The compound of claim 16 , wherein Ris substituted alkyl.18. The compound of claim 17 , wherein Ris 2-cyanoethyl.19. The compound according to any one of - claim 17 , wherein Ris acyloxy claim 17 , substituted acyloxy claim 17 , acylthio claim 17 , or substituted acylthio.20. The compound according to any one of - and claim 17 , wherein Ris acyloxyor substituted acyloxy.21. The compound according to any one of - claim 17 , claim 17 , and claim 17 , wherein Ris ...

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05-03-2020 дата публикации

Biological Buffers with Wide Buffering Ranges

Номер: US20200071582A1
Автор: Daly Thomas
Принадлежит:

Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. 2. The biological buffer and its salts of wherein A═D═—CH3 and m=1.3. The biological buffer and its salts of wherein A═D═—CH2OH and m=1.4. The biological buffer and its salts of wherein A═D—CH2O(CH2CH2CH2N)H and n=m=1.5. The biological buffer and its salts of wherein A═—CH2CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.6. The biological buffer and its salts of wherein A═—CH3 claim 1 , D═—CH2O(CH2CH2CH2N)H and n=m=1.7. The biological buffer and its salts of wherein A is —CH3 and D is —CH2CH3.9. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.10. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′═—CH3 and G═—H.11. The quaternary ammonium compound and its salts of wherein A═D═—CH3 claim 8 , E═—CH2OH claim 8 , R═R′═—CH3 and G═—CH2CH3.12. The quaternary ammonium compound and its salts of wherein A═D═E═—CH2OH claim 8 , R═R′=—CH3 and G═—CH2CH3. This is a continuation of U.S. application Ser. No. 15/649,869 filed Jul. 14, 2017 and other previous parent applications claimed in the Application Data Sheet. U.S. application Ser. No. 15/649,869 is hereby incorporated by reference in its entirety.The present invention relates generally to the field of amines and more particularly to a classes of amines used as buffers in biological systems.Amines are very useful compounds in the buffering of biological systems. Each class of amine has various limitations which require choosing an amine ...

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05-06-2014 дата публикации

HOMOLEPTIC RARE EARTH TRIARYL COMPLEXES

Номер: US20140155562A1
Принадлежит: ROCKWOOD LITHIUM GMBH

The invention relates to chelate-stabilized homleptic triaryl compounds based on phenylphosphoranes, to methods for preparing same and to the use thereof as catalysts. According to the invention, the object is achieved by homleptic rare earth triaryl complexes of the general formula (I), where SE=Sc, Y, La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb or Lu; X=O, CRR′; R, R=phenyl; R, R′=mutually independently H, alkyl with n=10 C atoms, phenyl or trimethylsilyl. 116-. (canceled)18. A homoleptic rare earth triaryl complex according to claim 17 , wherein if X=O claim 17 , SE=Sc claim 17 , Y claim 17 , Lu or Yb.19. A homoleptic rare earth triaryl complex according to claim 17 , wherein if X=CH claim 17 , RE=Sc claim 17 , Y claim 17 , Lu claim 17 , Sm claim 17 , Gd or Dy.20. A homoleptic rare earth triaryl complex according to selected from the group consisting of:{'sub': 6', '4', '6', '5', '2', '3, '[o-Sc(CH(CH)P=O)],'}{'sub': 6', '4', '6', '5', '2', '3, '[o-Y(CH(CH)P=O)],'}{'sub': 6', '4', '6', '5', '2', '3, '[o-Lu(CH(CH)P=O)],'}{'sub': 6', '4', '6', '5', '2', '3, '[o-Yb(CH(CH)P=O)],'}{'sub': 6', '4', '6', '5', '2', '2', '3, '[o-Y(CH(CH)P=CH)],'}{'sub': 6', '4', '6', '5', '2', '2', '3, '[o-SC(CH(CH)P=CH)],'}{'sub': 6', '4', '6', '5', '2', '2', '3, '[o-LU(CH(CH )P=CH)],'}{'sub': 6', '4', '6', '5', '2', '2', '3, '[o-Dy(CH(CH)P=CH)],'}{'sub': 6', '4', '6', '5', '2', '2', '3, '[o-Gd(CH(CH)P=CH)], and'}{'sub': 6', '4', '6', '5', '2', '2', '3, '[o-Sm(CH(CH)P=CH)].'}21. A method according of preparing a homoleptic rare earth triaryl complex according to claim 17 , wherein a triphenylphosphorane is reacted with a solvated rare earth metal halogenide or solvatized organo rare earth metal complex in the temperature range of −30° C. to 120° C.22. The method according to claim 21 , wherein the reaction is achieved by at least one of a salt elimination or hydrogen elimination.23. The method according to claim 21 , wherein the reaction is performed in situ as a one-pot ...

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05-06-2014 дата публикации

PROCESS FOR EXTRACTING MINERAL OIL USING SURFACTANTS BASED ON BUTYLENE OXIDE-CONTAINING ALKYL ALKOXYLATES

Номер: US20140155645A1
Принадлежит: BASF SE

A surfactant and a surfactant formulation comprising at least one ionic surfactant of the general formula R—O-(D)-(B)-(A)-XYM where Ris a linear or branched, saturated or unsaturated, aliphatic and/or aromatic hydrocarbon radical having 8 to 30 carbon atoms, A is ethyleneoxy, B is propyleneoxy, and D is butyleneoxy, l is from 0 to 99, m is from 0 to 99 and n is from 1 to 99, X is an alkyl or alkylene group having 0 to 10 carbon atoms, M is a cation, and Y is selected from the group of sulfate groups, sulfonate groups, carboxylate groups and phosphate groups. 1. A surfactant formulation comprising at least one ionic surfactant of the general formula{'br': None, 'sup': 1', '−', '+, 'sub': n', 'm', 'l, 'R—O-(D)-(B)-(A)-XYM, where'}{'sup': '1', 'Ris a linear or branched, saturated or unsaturated, aliphatic and/or aromatic hydrocarbon radical having 8 to 30 carbon atoms,'}A is ethyleneoxy,B is propyleneoxy, andD is butyleneoxy,l is from 0 to 99,m is from 0 to 99 andn is from 1 to 99,X is an alkyl or alkylene group having 0 to 10 carbon atoms,{'sup': '+', 'M is a cation, and'}{'sup': '−', 'claim-text': 'the A, B and D groups may be distributed randomly, alternatingly, or in the form of two, three, four or more blocks in any sequence, the sum of l+m+n is in the range from 3 to 99 and the proportion of 1,2-butylene oxide, based on the total amount of butylene oxide, is at least 80%.', 'Y is selected from the group of sulfate groups, sulfonate groups, carboxylate groups and phosphate groups, where'}2. The surfactant formulation according to claim 1 , whereinm is from 5 to 9 andn is from 2 to 10, and{'sup': '−', 'claim-text': {'sup': '1', 'the A, B and D groups are present to an extent of more than 80% in block form in the sequence D,B,A, beginning from R, the sum of l+m+n is in the range from 7 to 49, and the proportion of 1,2-butylene oxide, based on the total amount of butylene oxide in the molecule, is at least 90%.'}, 'Y is selected from the group of sulfate groups, ...

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05-03-2020 дата публикации

Thermally Activated Delayed Fluorescent Material Based on 9,10-Dihydro-9,9-dimethylacridine Analogues for Prolonging Device Longevity

Номер: US20200075868A1
Автор: Daijun FENG, JIAN Li
Принадлежит: Arizona Board of Regents of ASU

Thermally activated delayed fluorescent compounds and uses thereof are described. The thermally activated delayed fluorescent compounds are an analogues of 9,10-dihydro-9,9-dimethylacridine compounds.

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18-03-2021 дата публикации

Organic Electronic Device Comprising an Organic Semiconductor Layer

Номер: US20210083192A1
Принадлежит:

The present invention relates to compounds comprising a TAE structure, for use as a layer material for electronic devices, and to an organic electronic device comprising the layer material, and a method of manufacturing the same. 2. The compound according to claim 1 , whereinthe compound of formula I comprises at least 8 to 14 non-hetero aromatic rings.3. The compound according to claim 1 , wherein the compound of formula 1 comprises at least 8 to 14 non-hetero 6-member aromatic rings and is free of a hetero atom.4. The compound according to claim 1 , wherein{'sup': '1', 'the Argroup comprises at least 1 to 3 non-hetero aromatic 6 membered rings.'}9. The compound according to claim 1 , wherein Arcomprises at least one substituted or unsubstituted 1 claim 1 ,1 claim 1 ,2 claim 1 ,2-Tetraphenylethylene group.11. An organic electronic device comprising an organic semiconductor layer claim 1 , wherein at least one organic semiconductor layer comprises a compound of formula I according to .12. The organic electronic device according to claim 11 , wherein the organic semiconductor layer is arranged between a photoactive layer and a cathode layer.13. The organic electronic device according to claim 11 , wherein the at least one organic semiconductor layer further comprises at least one alkali halide or alkali organic complex.14. The organic electronic device according to claim 11 , wherein the electronic device comprises at least one organic semiconductor layer claim 11 , at least one anode layer claim 11 , at least one cathode layer and at least one emission layer.15. The organic electronic device according to claim 11 , wherein the electronic device is a light emitting device claim 11 , thin film transistor claim 11 , a battery claim 11 , a display device or a photovoltaic cell.16. The compound according to claim 1 , wherein the compound of formula I comprises at least 8 to 14 non-hetero aromatic 6-member rings.17. The compound according to claim 1 , wherein the compound ...

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12-06-2014 дата публикации

CYCLOPENTADIENYLIDENE-PHOSPHORANE CONSTRAINED GEOMETRY COMPLEXES OF RARE EARTH METALS

Номер: US20140163187A1
Принадлежит: ROCKWOOD LITHIUM GMBH

The invention relates to η:η-cyclopentadienylidene-phosphorane constrained geometry complexes of rare earth metals, abbreviated to η:η-CpPC-CGC, method for production and use of same. The η:η-CpPC-CGCs correspond to the general formula (1), wherein SE=Sc, Y, La, Ce, Pr, Nd, Pm, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb or Lu; X=independently of one another, a mono-anionic diorganoamido-, bistrimethylsilylamido-, halogenido-, alkyl-, aryl-, alkoxo-, aryloxo- or alkylaluminate (AlR) substituent; L=neutral ligand (PR, NR, pyridine), solvent molecule (THF, ether, DMF, DMSO, HMPT, tetrahydropyran THP, tetrahydrothiofuran THT); R=alkyl with up to 1-10 C atoms or mono- or polycyclical aryl with 6 to 20 C atoms; R, R=independently of one another H or methyl; R, R=independently of one another, H or methyl or tertiary butyl or together a substituted cycloalkyl group; R, R=methyl, n-butyl, tertiary butyl or phenyl; R, R=independently of one another H, trimethylsilyl, alkyl with 1-10 C atoms or mono- or polycyclical aryl with 6 to 20 C atoms, and m=0, 1, 2 or 3. 115-. (canceled)18. η:η-CpPC-CGC according to claim 16 , whereinSE=Sc, Y, La, Ce, Nd, Sm or Lu.19. η:η-CpPC-CGC according to claim 17 , whereinSE=Sc, Y, La, Ce, Nd, Sm or Lu.20. η:η-CpPC-CGC according to claim 16 , whereinX=hexamethylenedisilazanide, N,N-dimethylbenzylamine ortho-metallized, N,N, α-trimethylbenzylamine ortho-metallized.21. η:η-CpPC-CGC according to claim 17 , whereinX=hexamethylenedisilazanide, N,N-dimethylbenzylamine ortho-metallized, N,N, α-trimethylbenzylamine ortho-metallized.22. η:η-CpPC-CGC according to claim 16 , wherein the neutral ligand is PR claim 16 , NR claim 16 , pyridine claim 16 , wherein R=an alkyl with up to 1-10 carbon atoms or a mono- or polycyclic aryl with 6 to 20 carbon atoms claim 16 , and the dissolvent molecule is THF claim 16 , ether claim 16 , DMF claim 16 , DMSO claim 16 , HMPT claim 16 , tetrahydropyran claim 16 , tetrahydrothiofuran.23. η:η-CpPC-CGC according to claim 17 , ...

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12-03-2020 дата публикации

COMPOUNDS FOR TREATMENT OF SENESCENCE-RELATED DISORDERS

Номер: US20200079805A1
Принадлежит:

The present invention relates to compounds of general formula (I) in particular for use in the treatment of senescence-related diseases, such as idiopathic pulmonary fibrosis, sarcopenia, diabetes, obesity, osteoarthritis, chronic inflammations, glaucoma, cataracts, radiation-induced oral mucosis, renal transplantation, prostatic hyperplasia. 111.-. (canceled)13. The compound of claim 12 , wherein Z is a linear hydrocarbyl chain selected from the group consisting of alkylene claim 12 , alkenylene and alkynylene having 4 to 14 carbon atoms claim 12 , and{'sub': 1', '4', '1', '4', '2', '1', '4', '1', '4, 'where the linear hydrocarbyl chain can optionally be substituted by one or more substituents selected independently from the group consisting of C-Calkyl, N(H or C-Calkyl), OH, ═O, SH, ═S, F, Cl, Br, I, C-Calkoxy and C-Cmercapto, where alkyl is the same or different.'}14. The compound of claim 12 , wherein Z is a linear hydrocarbyl chain selected from the group consisting of alkylene claim 12 , alkenylene and alkynylene having 4 to 14 carbon atoms claim 12 ,where one or more carbon atoms in the linear hydrocarbyl chain are replaced by one or more heteroatoms selected from O, S and NH, and{'sub': 1', '4', '1', '4, 'where the linear hydrocarbyl chain can optionally be substituted by one or more substituents selected independently from the group consisting of OH, ═O, SH, ═S, C-Calkoxy and C-Cmercapto.'}15. The compound of claim 12 , wherein Z is a linear hydrocarbyl chain selected from the group consisting of alkylene claim 12 , alkenylene and alkynylene having 4 to 14 carbon atoms claim 12 ,where one or more carbon atoms in the linear hydrocarbyl chain are replaced by NH, and{'sub': 1', '4', '1', '4, 'where the linear hydrocarbyl chain can optionally be substituted by one or more substituents selected independently from the group consisting of OH, ═O, SH, ═S, C-Calkoxy and C-Cmercapto.'}16. The compound of claim 12 , wherein Z is a linear hydrocarbyl chain selected ...

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25-03-2021 дата публикации

PREPARATION OF PSILOCYBIN, DIFFERENT POLYMORPHIC FORMS, INTERMEDIATES, FORMULATIONS AND THEIR USE

Номер: US20210087212A1
Принадлежит: COMPASS PATHFINDER LIMITED

This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin. 130-. (canceled)31. A pharmaceutical composition , comprising crystalline Polymorph A of psilocybin and a pharmaceutically acceptable excipient , wherein the Polymorph A is characterized by X-ray powder diffraction (XRPD) peaks at 11.5±0.1 , 12.0±0.1 , 14.5±0.1 , 17.5±0.1 and 19.7±0.1°2θ ,wherein the psilocybin has a chemical purity of greater than 97% and no single impurity of greater than 1% as determined by HPLC analysis.32. The pharmaceutical composition of claim 31 , wherein the composition is a capsule.33. The pharmaceutical composition of claim 31 , wherein the composition is a tablet.34. The pharmaceutical composition of claim 31 , wherein the Polymorph A is further characterized by at least one peak selected from the group consisting of 20.4±0.1 claim 31 , 22.2±0.1 claim 31 , 24.3±0.1 claim 31 , and 25.7±0.1°2θ.35. The pharmaceutical composition of claim 31 , wherein the composition comprises about 5 mg of the crystalline Polymorph A of psilocybin.36. The pharmaceutical composition of claim 31 , wherein the composition comprises about 10 mg of the crystalline Polymorph A of psilocybin.37. The pharmaceutical composition of claim 31 , wherein the composition comprises about 25 mg of the crystalline Polymorph A of psilocybin.38. Crystalline Polymorph A of psilocybin claim 31 , wherein the Polymorph A is characterized by X-ray powder diffraction (XRPD) peaks at 11.5±0.1 claim 31 , 12.0±0.1 claim 31 , 14.5±0.1 claim 31 , 17.5±0.1 and 19.7±0.1°2θ claim 31 , wherein the psilocybin has a chemical purity of greater than 97% and no single impurity of greater than 1% as determined by HPLC analysis.39. The ...

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19-03-2020 дата публикации

AZIRIDINE CONTAINING DNA ALKYLATING AGENTS

Номер: US20200085786A1
Принадлежит:

Provided herein are compounds of formula (I)-(VI): 3. The compound of claim 2 , wherein Ris a non-hydrogen substituent claim 2 , Rand Rare hydrogen claim 2 , and Ris hydrogen or halo claim 2 , or Rand Rtogether form a 5 membered cycloalkyl group.4. The compound of claim 3 , wherein Ris hydrogen.5. The compound of claim 3 , wherein Ris halo.6. The compound of claim 3 , wherein Ris fluoro.7. The compound of claim 3 , wherein Ris NRR claim 3 , wherein each Rand Rindependently is hydrogen claim 3 , hydroxy claim 3 , C-Calkyl C-Calkenyl claim 3 , C-Calkynyl claim 3 , C-Ccycloalkyl claim 3 , C-Caryl claim 3 , 4-15 membered heterocycle claim 3 , 5-15 membered heteroaryl claim 3 , or —SO(C-Calkyl); or Rand Rtogether with the nitrogen atom they are bonded to form a 4-15 membered heterocycle or a 5-15 membered heteroaryl.8. The compound of claim 3 , wherein Ris a non-hydrogen substituent.9. The compound of claim 3 , wherein Ris a non-hydrogen substituent; Rand Rare hydrogen claim 3 , and Ris hydrogen or halo claim 3 , and Ris optionally substituted C-Calkyl.10. A pharmaceutical composition comprising the compound of and at least one pharmaceutically acceptable excipient.11. A method of treating cancer comprising administering to a patient in need thereof a therapeutically effective amount of the compound of . This application is a continuation application of U.S. application Ser. No. 15/736,285, filed on Dec. 13, 2017, which claims priority under 35 U.S.C. § 371 of International Application No. PCT/US2016/039092, filed Jun. 23, 2016, which claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application No. 62/184,129, filed Jun. 24, 2015, the content of which is hereby incorporated by reference in its entirety.The present invention provides compounds suitable as therapeutic agents, pharmaceutical compositions of such compounds and methods of treating cancer in cancer patients, and so relates to the fields of biology, chemistry, and medicine.Cancer is one of the major ...

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19-06-2014 дата публикации

DIPHOSPHINE LIGAND AND TRANSITION METAL COMPLEX USING THE SAME

Номер: US20140171655A1
Принадлежит: Takeda Pharmaceutical Company Limited

The present invention provides a novel ligand represented by the following formula and a novel transition metal complex having the ligand, which shows superior enantioselectivity and catalytic efficiency, particularly high catalyst activity, in various asymmetric synthesis reactions. 111-. (canceled)13. The compound of claim 12 , wherein R claim 12 , Rand Rare each a Calkyl group optionally having substituent(s). The present invention relates to a novel ligand, a transition metal complex having the novel ligand, and an asymmetric synthesis reaction using the transition metal complex.Known asymmetric synthesis reaction includes asymmetric reductions, asymmetric isomerizations, asymmetric hydrosilylations and the like, and transition metal complexes with rhodium, ruthenium, iridium and the like having an optically active compound as a ligand are mainly used. Conventionally, 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (hereinafter sometimes to be also abbreviated as BINAP) is generally used as an optically active phosphine. Since reactivity, steric selectivity, catalytic efficiency and the like are not sufficient depending on the kind of substrate, however, various optically active phosphines have been produced and reported (e.g., Handbook of Enantioselective Catalysis with Transition Metal Compounds, published by VCH Verlag GmbH, 1993). Of the optically active phosphines, optically active phosphines having a dialkylamino group as a substituent are described in WO03/048174 and WO02/040491.Of the compounds having a 1,1′-binaphthyl skeleton like BINAP, for example, JP-A-61-63690 describes that a ruthenium complex having 2,2′-bis(di(p-tolyl)phosphino)-1,1′-binaphthyl as a ligand is useful for the asymmetric reduction of a carbon-carbon double bond. JP-A-3-255090 describes that a ruthenium complex having 2,2′-bis(bis(3,5-dialkylphenyl)phosphino)-1,1′-binaphthyl as a ligand is useful for the asymmetric reduction of β-ketoester and JP-A-2004-196793 describes that a ruthenium ...

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05-04-2018 дата публикации

Compounds with phosphine oxide and amine functions, useful as uranium (vi) ligands, and uses thereof, in particular for extracting uranium(vi) from aqueous solutions of sulphuric acid

Номер: US20180094009A1

The invention relates to compounds which correspond to the general formula (I) below: in which: R 1 and R 2 represent, independently of one another, a C 4 to C 12 acyclic hydrocarbon group; R 3 represents H; a C 1 to C 12 acyclic hydrocarbon group with optionally one or more heteroatoms; a C 5 or C 6 cyclic hydrocarbon group; or a 5- or 6-membered heterocyclic group; R 4 represents H or a C 1 to C 12 acyclic hydrocarbon group with optionally one or more heteroatoms; R 5 and R 6 represent, independently of one another, H; a C 1 to C 12 acyclic hydrocarbon group with optionally one or more heteroatoms; a C 5 or C 6 cyclic hydrocarbon group; or a 5- or 6-membered heterocyclic group; on the condition however that R 5 and R 6 do not each represent H.

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12-05-2022 дата публикации

Double alkoxycarbonylation of dienes as one-pot synthesis

Номер: US20220144750A1
Принадлежит: EVONIK OPERATIONS GMBH

Process for the double alkoxycarbonylation of dienes as one-pot synthesis.

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12-05-2022 дата публикации

METHOD FOR PURIFYING PHOSPHORUS-CONTAINING OLEFIN COMPOUND SALT AND METHOD FOR PRODUCING OLEFIN COMPOUND USING PURIFIED PRODUCT OBTAINED THEREBY

Номер: US20220144864A1
Принадлежит: DAIKIN INDUSTRIES, LTD.

Provided is a method for purifying a phosphorus-containing olefin compound salt as a raw material or an intermediate that is useful to increase the purity of a target product in a method for producing an olefin compound and that can be applied to the production method, and a method for producing an olefin compound using a purified product obtained thereby. 2. The purification method according to claim 1 , wherein the solvent is at least one member selected from the group consisting of ethyl acetate claim 1 , n-propyl acetate claim 1 , isopropyl acetate claim 1 , n-butyl acetate claim 1 , methanol claim 1 , ethanol claim 1 , propanol claim 1 , isopropanol claim 1 , and butanol.3. (canceled)4. The purification method according to claim 1 , further comprising extracting the purified product by suction filtration and/or pressure filtration.5. The purification method according to claim 1 , wherein the solid comprises at least one compound selected from the group consisting of:(trans-2-perfluoropropoxy-1,2-difluoroethen-1-yl)(tributyl) phosphonium tetrafluoroboranuide,(cis-2-perfluoropropoxy-1,2-difluoroethen-1-yl)(tributyl) phosphonium tetrafluoroboranuide, perfluoropropoxy vinyl ether,(2,2,3,3,3-pentafluoro-1-tributylphosphin-1-one) tetrafluoroboranuide,boron trifluoride tributylphosphine oxide,tetrafluoroboric acid,(1,2-difluoroethen-1-yl)(tributyl) phosphonium tetrafluoroboranuide),diethyl ether,dimethyl ether, and2-methoxy-2-methylpropane.6. The purification method according to claim 1 , wherein the purity of the phosphorus-containing olefin compound salt in the purified product is 95 mass % or more.7. A method for producing an olefin compound claim 1 , comprising reacting the purified product obtained by the purification method according to and a base to thereby obtain a reaction product containing a dephosphorized and hydrogenated olefin compound.8. The production method according to claim 7 , wherein the olefin compound is (E)-1 claim 7 ,2-difluoroethylene.9. The ...

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02-06-2022 дата публикации

PROGRAMMABLE POLYMERIC DRUGS

Номер: US20220168433A1
Принадлежит:

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R, R, R, R, R, L, L, L, L, L, M, m, and n are as defined herein. Methods associated with preparation and use of such compounds is also provided. 2. (canceled)49.-. (canceled)1114.-. (canceled)15. The compound of claim 1 , wherein at least one occurrence of Lcomprises an amide bond claim 1 , an ester bond claim 1 , a phosphodiester bond claim 1 , a disulfide bond claim 1 , a double bond claim 1 , a triple bond claim 1 , an ether bond claim 1 , a hydrazone claim 1 , an amino acid sequence claim 1 , a ketone claim 1 , a diol claim 1 , a cyano claim 1 , a nitro or combinations thereof.16. The compound of claim 15 , wherein Lcomprises an amino acid sequence recognized by a sortase enzyme.17. The compound of claim 16 , wherein the amino acid sequence is Leu-Pro-X-Thr-Gly claim 16 , wherein X is any amino acid residue.18. (canceled)19. (canceled)2127.-. (canceled)2934.-. (canceled)35. The compound of claim 1 , wherein at least one occurrence of Lcomprises a thioether bond.36. (canceled)3850.-. (canceled)52. (canceled)53. The compound of claim 1 , wherein the targeting moiety is an antibody claim 1 , cell surface receptor agonist claim 1 , or cell surface receptor antagonist.54. (canceled)55. The compound of claim 53 , wherein the targeting moiety is a monoclonal antibody claim 53 , wherein the monoclonal antibody is Abciximab claim 53 , Adalimumab claim 53 , Alemtuzumab claim 53 , Alirocumab claim 53 , Avibactam claim 53 , Basiliximab claim 53 , Benralizumab claim 53 , Bezlotoxumab claim 53 , Blinatumomab claim 53 , Brodalumab claim 53 , Burosumab claim 53 , Canakinumab claim 53 , Caplacizumab claim 53 , Certolizumab pegol claim 53 , Daclizumab claim 53 , Denosumab claim 53 , Dupilumab claim 53 , Eculizumab claim 53 , Emicizumab claim 53 , Erenumab claim 53 , Evolocumab claim 53 , Fremanezumab claim 53 , ...

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04-04-2019 дата публикации

METHOD FOR PRODUCING MONOMER FOR SINGLE-STRANDED NUCLEIC ACID MOLECULE

Номер: US20190100540A1
Автор: Ihara Hideki, SATO Kanako
Принадлежит: Sumitomo Chemical Company, Limited

A compound represented by formula (3): 2. The production method according to claim 1 , wherein the base is an alkali metal hydroxide.3. The production method according to claim 1 , wherein the condensing agent is 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride claim 1 , 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide claim 1 , N claim 1 ,N′-dicyclohexylcarbodiimide claim 1 , N claim 1 ,N′-diisopropylcarbodiimide claim 1 , 1 claim 1 ,1-carbonyldiimidazole claim 1 , 1-propylphosphonic anhydride cyclic trimer or 2-chloro-4 claim 1 ,6-dimethoxy-1 claim 1 ,3 claim 1 ,5-triazine.4. The production method according to claim 1 , wherein the additive is 1-hydroxybenzotriazole claim 1 , 1-hydroxy-7-azabenzotriazole claim 1 , N-hydroxysuccinimide claim 1 , ethyl (hydroxyimino)cyanoacetate or N claim 1 ,N′-disuccinimidyl carbonate.5. The production method according to claim 1 , wherein the coupling activator is diisopropylaminetetrazole salt claim 1 , 1H-tetrazole claim 1 , 5-(ethylthio)-1H-tetrazole claim 1 , 5-(benzylthio)-1H-tetrazole or 4 claim 1 ,5-dicyanoimidazole. The present invention relates to a method for producing a monomer used for producing a single-stranded nucleic acid molecule capable of suppressing the expression of a target gene.US2012/0035246 discloses a method for producing a single-stranded nucleic acid molecule capable of suppressing the expression of a target gene, and, as a monomer used for its production, production of a compound represented by formula (3)(hereinafter referred to as the compound (3)) and its enantiomer is described in Example A3.However, when the compound (3) obtained by the method described in US2012/0035246 is used, the yield of the single-stranded nucleic acid molecule is not necessarily sufficient.The present invention provides a method for producing the compound (3) capable of producing the single-stranded nucleic acid molecule with high yield.The present invention is as follows.reacting a compound represented by formula ...

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23-04-2015 дата публикации

METHOD OF TREATMENT WITH PRODRUGS OF 6-CYCLOHEXYL-1-HYDROXY-4-METHYLPYRIDIN IN-2-1H-ONE AND DERIVATIVES THEREOF

Номер: US20150111858A1
Принадлежит: The University of Kansas

A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, , and , candidiasis (moniliasis), , tinea () vesicolor, , acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma. 3. The method of claim 2 , the compound represented by a structure of Formula 2 or stereoisomer thereof or pharmaceutically acceptable salt thereof claim 2 , wherein R-Rare each independently a positive ion.8. (canceled)11. The method of claim 1 , wherein the pharmaceutical composition comprises the compound and a pharmaceutically acceptable carrier.12. The method of claim 1 , wherein the compound is administered in an effective amount to provide a therapeutically effective amount of 6-cyclohexyl-1-hydroxy-4-methylpyridin-2(1H)-one.13. The method of claim 12 , wherein the therapeutically effective amount is sufficient:for use in treatment of a fungus;for use in treatment of cancer;for use in treatment of acute myeloid leukemia or acute lymphoid leukemia;for use in treatment of chronic myelogenous leukemia, lymphoma or multiple myeloma.15. The method of claim 13 , comprising administering the compound in an effective amount sufficient for treatment of fungus.16. The method of claim 13 , comprising administering the compound in an effective amount sufficient for treatment of cancer.17. The method of claim 1 , comprising administering the compound in an amount sufficient:for use in treatment of acute myeloid leukemia or acute lymphoid leukemia; orfor use in treatment of chronic myelogenous leukemia, lymphoma or multiple myeloma.19. The method of claim 1 , comprising administering the compound in an effective amount sufficient for treatment of fungus.20. The method of claim 1 , ...

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29-04-2021 дата публикации

PENTAFLUOROPHOSPHATE DERIVATIVE, ITS USES AND AN APPROPRIATE MANUFACTURING METHOD

Номер: US20210122772A1
Принадлежит: FREIE UNIVERSITÄT BERLIN

It is provided a pentafluorophosphate derivative according to general formula (I): 2. The pentafluorophosphate derivative according to claim 1 , wherein the cycloalkyl or the aryl is substituted by a hydrocarbon chain comprising an amide function and/or a carboxyl function claim 1 , or by a substituent chosen from the group consisting of alkyl claim 1 , alkylamino claim 1 , alkylaminocarboxy claim 1 , halogen claim 1 , haloalkyl claim 1 , carboxy claim 1 , alkoxycarbonyl claim 1 , hydroxy claim 1 , N-morpholino claim 1 , N-morpholinoalkyl claim 1 , N-morpholinocarbonyl claim 1 , N-methyl-N-piperazinyl claim 1 , N-methyl-N-piperazinylalkyl claim 1 , N-methyl-N-piperazinylcarbonyl claim 1 , and sulfo.4. The pentafluorophosphate derivative according to claim 3 , wherein the alkyl claim 3 , the cycloalkyl or the aryl is substituted by a hydrocarbon chain comprising an amide function and/or a carboxyl function claim 3 , or by a substituent chosen from the group consisting of alkyl claim 3 , alkylamino claim 3 , alkylaminocarboxy claim 3 , halogen claim 3 , haloalkyl claim 3 , carboxy claim 3 , alkoxycarbonyl claim 3 , hydroxy claim 3 , N-morpholino claim 3 , N-morpholinoalkyl claim 3 , N-morpholinocarbonyl claim 3 , N-methyl-N-piperazinyl claim 3 , N-methyl-N-piperazinylalkyl claim 3 , N-methyl-N-piperazinylcarbonyl claim 3 , and sulfo.6. The pentafluorophosphate derivative according to claim 1 , wherein Rand Rdenote F.7. The pentafluorophosphate derivative according to claim 1 , wherein Rand Rdenote F claim 1 , and Rdenotes H.8. (canceled)9. (canceled)10. (canceled)11. A pharmaceutical composition claim 1 , comprising a pentafluorophosphate derivative according to as active compound.13. The method according to claim 12 , wherein step a) is carried out by reacting the diethyl phosphonate derivative with bromotrimethylsilane in an organic solvent and by purifying the resulting product with an ion-exchange resin.14. The method according to claim 12 , wherein step b) is ...

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28-04-2016 дата публикации

Alkoxyamines for the treatment of cancers

Номер: US20160115130A1

The present invention relates to alkoxyamines of general formula (I), and to compounds of general formula (IIa), (IIb), (IIc), (IId), IIe), (IIf) or (IIg), as such and for the treatment of cancers.

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30-04-2015 дата публикации

Novel Alkylated Imino Sugars Exhibiting Glucosidase Inhibition and Their Method of Use

Номер: US20150119366A1

Pharmaceutical compositions of the invention comprise alkylated imino sugars derivatives having a disease-modifying action in the treatment of diseases associated with glucosidase activity that include Viral hemorrhagic fevers, and any other diseases involving glucosidase activity.

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10-07-2014 дата публикации

Spirobenzylamine-Phosphine, Preparation Method Therefor And Use Thereof

Номер: US20140194638A1

The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R, R, R, R, R, R, R, Rand Rhaving a value as defined in claim . Starting from the substituted 7-trifluoromesyloxy-7′-diarylphosphino-1,1′-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization. 2. The compound of spirobenzylamine-phosphine according to claim 1 , wherein claim 1 , C-Calkyl described above can be methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl claim 1 , isobutyl sec-butyl claim 1 , tert-butyl claim 1 , pentyl claim 1 , isopentyl claim 1 , neopentyl claim 1 , sec-pentyl claim 1 , tert-pentyl claim 1 , hexyl claim 1 , isohexyl claim 1 , neohexyl claim 1 , sec-hexyl claim 1 , tert-hexyl claim 1 , heptyl claim 1 , isoheptyl claim 1 , neoheptyl claim 1 , sec-heptyl claim 1 , tert-heptyl claim 1 , octyl claim 1 , isooctyl claim 1 , neooctyl claim 1 , sec-octyl or tert-octyl;{'sub': 1', '8, 'C-Calkoxy described above can be methoxy, ethoxy, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-pentyloxy, isopentyl, neopentyl, sec-pentyloxy, tert-pentyloxy, n-hexyloxy, isohexyloxy, neohexyloxy, sec-hexyloxy, tert-hexyloxy, n-heptyloxy, isoheptyloxy, neoheptyloxy, sec-heptyloxy, tert-heptyloxy, n-octyloxy, iso-octyloxy, neooctyloxy, sec-octyloxy or a tert-octyloxy;'}{'sub': 1', '8, 'C-Cacyl described above can be formyl, acetyl, propionyl, n-butyryl, ...

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13-05-2021 дата публикации

OLIGONUCLEOTIDE ANALOGUES HAVING MODIFIED INTERSUBUNIT LINKAGES AND/OR TERMINAL GROUPS

Номер: US20210139897A1
Принадлежит:

Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3′ and/or 5′-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects. 34-. (canceled)5. The oligomer of claim 1 , wherein W and Y are each O at each occurrence.619-. (canceled)2124-. (canceled)26. The oligomer of claim 25 , wherein at least one of Ror Ris R.2728-. (canceled)3133-. (canceled)34. The oligomer of claim 30 , wherein Ris C-Caralkylcarbonyl.3561-. (canceled)62. The oligomer of claim 30 , wherein Ris a cell-penetrating peptide and Ris R.63. The oligomer of claim 30 , wherein Ris a cell-penetrating peptide and Ris R.6466-. (canceled)6870-. (canceled)7281-. (canceled)83. The oligomer of claim 82 , wherein Ris C-Caralkylcarbonyl.84. The oligomer of claim 82 , wherein Ris a cell-penetrating peptide and Ris R.85. The oligomer of claim 82 , wherein Ris a cell-penetrating peptide and Ris R. This application is a continuation of U.S. application Ser. No. 16/225,909, filed Dec. 19, 2018, which is a continuation of U.S. application Ser. No. 15/247,584, filed on Aug. 25, 2016, now issued as U.S. Pat. No. 10,202,602, which is a continuation of U.S. application Ser. No. 14/298,655 filed on Jun. 6, 2014, now issued as U.S. Pat. No. 9,469,664, which is a continuation of U.S. application Ser. No. 13/118,298 filed on May 27, 2011, now issued as U.S. Pat. No. 8,779,128 which claims the benefit under 35 U.S.C. § 119(e) of U.S. Provisional Patent Application No. 61/349,783 filed on May 28, 2010; U.S. Provisional Patent Application No. 61/361,878 filed on Jul. 6, 2010 and U.S. Provisional Patent Application No. 61/386,428 filed on Sep. 24, 2010, each of which are incorporated herein by reference in their entireties.The Sequence Listing associated with this application is provided in text format in lieu of a paper copy, and is hereby ...

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03-05-2018 дата публикации

Biaryl ligands for transition metal-catalyzed reactions

Номер: US20180117574A1
Принадлежит: UNIVERSITY OF CALIFORNIA

In one embodiment, the present application discloses ligands of the formula A, wherein the variables are as described herein, and methods for using the ligands in cross-coupling reactions in organic and polar media:

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25-04-2019 дата публикации

Phosphonate functional antimicrobial coatings for metal surfaces

Номер: US20190116798A1
Принадлежит: NANO SAFE COATINGS Inc

The invention relates to quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, processes for preparing quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds, antimicrobial coating compositions comprising quaternary ammonium multi-dentate mono-, bis-, tris- and tetrakis-phosphonate compounds and method of treating a surface with said compositions to provide a durable, antimicrobial-treated surface.

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25-04-2019 дата публикации

PREPARATION OF PSILOCYBIN, DIFFERENT POLYMORPHIC FORMS, INTERMEDIATES, FORMULATIONS AND THEIR USE

Номер: US20190119310A1
Принадлежит:

This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin. 1. Crystalline psilocybin in the form Polymorph A or Polymorph A′ , characterised by one or more of:a. peaks in an XRPD diffractogram at 11.5, 12.0 and 14.5°2θ±0.1°2θ;b. peaks in an XRPD diffractogram at 11.5, 12.0 and 14.5°2θ±0.1°2θ, further characterised by at least one further peak at 19.7, 20.4, 22.2, 24.3 or 25.7°2θ±0.1°2θ;{'figref': {'@idref': 'DRAWINGS', 'i': 'a', 'FIG. 7'}, 'b': '7', 'i': 'b', 'c. an XRPD diffractogram as substantially illustrated in or ; or'}{'figref': {'@idref': 'DRAWINGS', 'i': 'a', 'FIG. 8'}, 'b': '8', 'i': 'b.', 'd. an endothermic event in a DSC thermogram having an onset temperature of between 205 and 220° C. substantially as illustrated in or'}2. Crystalline psilocybin in the form Polymorph A or Polymorph A′ claim 1 , according to further characterised by an endothermic event in a DSC thermogram having an onset temperature of between 210 and 215° C.3. Crystalline psilocybin in the form Polymorph A claim 1 , according to characterised by one or more of:a. peaks in an XRPD diffractogram at 11.5, 12.0,14.5, and 17.5, °2θ±0.1°2θ;b. peaks in an XRPD diffractogram at 11.5, 12.0, 14.5 and 17.5, °2θ±0.1°2θ, further characterised by at least one further peak at 19.7, 20.4, 22.2, 24.3 or 25.7°2θ±0.1°2θ;{'figref': {'@idref': 'DRAWINGS', 'i': 'a', 'FIG. 7'}, 'c. an XRPD diffractogram as substantially illustrated in ; or'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 8'}, 'i': 'a.', 'd. an endothermic event in a DSC thermogram having an onset temperature of between 205 and 220° C. substantially as illustrated in'}4. Crystalline psilocybin in the form Polymorph A claim 3 , according to ...

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25-08-2022 дата публикации

PRODUCTION METHOD FOR BIFURCATED LIPID-LINKED OLIGONUCLEOTIDE, AND INTERMEDIATE

Номер: US20220267771A1
Принадлежит: Shionogi & Co., Ltd.

Provided are production methods capable of controlling quality of a bifurcated lipid-linked oligonucleotide, and intermediates which is useful for the production method, has good stability, and is easy to manage and analyze. Specifically, it is a method for producing a bifurcated lipid-linked oligonucleotide including a step of reacting a compound of formula (II): 6. The production method according to claim 5 , characterized in that{'sup': 'X1', 'Ris C8 to C30 alkyl or C8 to C30 alkenyl;'}{'sup': 'X2', 'Ris C1 to C29 alkyl or C2 to C29 alkenyl; and'}{'sup': X2', 'X1, 'the number of carbon atoms of the alkyl or alkenyl of Ris smaller than the number of carbon atoms of the alkyl or alkenyl of R.'}7. The method according to claim 4 , wherein the cleavage reagent and the deprotecting agent contain butylamine and/or benzylamine.8. The method according to claim 4 , comprising a step of washing the compound (V) with an organic solvent.9. A method for producing a double-stranded oligonucleotide claim 4 , comprising steps of:{'claim-ref': {'@idref': 'CLM-00004', 'claim 4'}, 'obtaining the compound (VII) by the method according to , and'}annealing an oligonucleotide comprising a sequence capable of hybridizing to an oligonucleotide of the compound (VII) to form a double strand.11. The method according to claim 5 , wherein the cleavage reagent and the deprotecting agent contain butylamine and/or benzylamine.12. The method according to claim 5 , comprising a step of washing the compound (V) with an organic solvent.13. A method for producing a double-stranded oligonucleotide claim 5 , comprising steps of:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'obtaining the compound (X) by the method according to , and'}annealing an oligonucleotide comprising a sequence capable of hybridizing to an oligonucleotide of the compound (X) to form a double strand. The present invention relates to methods for producing a bifurcated lipid-linked oligonucleotide. Further, the present invention ...

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16-04-2020 дата публикации

Synthesis of bis(acyl)phosphines by activation of unreactive metal phosphides

Номер: US20200115402A1
Принадлежит: IGM Group BV

The present invention refers to a process for the preparation of a mono(acyl)phosphine of the general formula (I) and/or a bis(acyl)phosphine of the general formula (II), wherein R 1 , R 2 , R 3 , R 4 and R 5 are the same or different and are independently selected from H, halogen, linear or branched C 1 -C 20 -alkyl, linear or branched C 2 -C 8 -alkenyl, C 1 -C 8 -alkoxy, C 2 -C 8 -alkenyloxy, C 3 -C 8 -cycloalkyl, C 6 -C 12 -aryl, C 3 -C 8 -cycloalkoxy, C 7 -C 12 -arylalkoxy, C 9 -C 15 -alkenylarylalkoxy, nitro-, C 6 -C 12 -arylsulfonyl, 4-alkylaryl-sulfonyl, C 1 -C 20 -alkylcarboxy, C 1 -C 8 -alkoxycarbonyl, SR 14 , NIIR 14 or NR 14 R 15 with R 14 and R 15 being independently selected from H, linear or branched C 1 -C 20 -alkyl, linear or branched C 2 -C 8 -alkenyl and C 3 -C 8 -cycloalkyl, and an O-, S- or N-containing 5-or 6-membered heterocyclic ring; R 6 is H or R 6 is replaced by an alkaline earth metal cation or a mixed alkali metal/alkaline earth metal cation; Formula (II) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 7 , R 8 , R 9 , R 10 and R 11 are the same or different and are independently selected from H, halogen, linear or branched C 1 -C 20 -alkyl, linear or branched C 2 -C 8 -alkenyl, C 1 -C 8 -alkoxy, C 2 -C 8 -alkenyloxy, C 3 -C 8 -cycloalkyl, C 6 -C 12 -aryl, C 3 -C 8 -cycloalkoxy, C 7 -C 12 -arylalkoxy, C 9 -C 15 -alkenylarylalkoxy, nitro-, C 6 -C 12 -arylsulfonyl, 4-alkylarylsulfonyl, C 1 -C 20 -alkylcarboxy, C 1 -C 8 -alkoxycarbonyl, SR 14 , NHR 14 or NR 14 R 15 with R 14 and R 15 being independently selected from H, linear or branched C 1 -C 20 -alkyl, linear or branched C 2 -C 8 -alkenyl and C 3 -C 8 -cycloalkyl, and an O-, S- or N- containing 5- or 6-membered heterocyclic ring; as well as the mono(acyl)phosphine and/or bis(acyl)phosphine obtained by the process.

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27-05-2021 дата публикации

METHOD FOR PRODUCING PHOSPHINOBENZENE BORANE DERIVATIVE, METHOD FOR PRODUCING 1,2-BIS(DIALKYLPHOSPHINO)BENZENE DERIVATIVE, AND TRANSITION METAL COMPLEX

Номер: US20210155641A1
Автор: TAMURA Ken
Принадлежит: Nippon Chemical Industrial Co., Ltd.

A method for producing a phosphinobenzene borane derivative comprises a reaction step (A) of obtaining liquid A containing a 1,2-dihalogenobenzene represented by the following general formula (1): 2. The method for producing a phosphinobenzene borane derivative according to claim 1 , wherein the hydrogen-phosphine borane compound represented by the general formula (2) is an optically active substance having an asymmetric center on the phosphorus atom.3. The method for producing a phosphinobenzene borane derivative according to claim 1 , wherein Ris a t-butyl group claim 1 , a 1 claim 1 ,1 claim 1 ,3 claim 1 ,3-tetramethylbutyl group or an adamantyl group; and Ris a methyl group.4. The method for producing a phosphinobenzene borane derivative according to claim 2 , wherein a reaction temperature in the reaction step (A) is −80 to 30° C.6. The method for producing a 1.2-bis(dialkylphosphino)benzene derivative according to claim 5 , wherein the hydrogen-phosphine borane compound represented by the general formula (2) is an optically active substance having an asymmetric center on the phosphorus atom.11. A transition metal complex claim 7 , comprising: a transition metal; and a compound according to coordinating to the transition metal.12. The transition metal complex according to claim 11 , being used as a catalyst in an asymmetric synthesis reaction.13. A transition metal complex claim 8 , comprising: a transition metal; and a compound according to coordinating to the transition metal.14. A transition metal complex claim 9 , comprising: a transition metal; and a compound according to coordinating to the transition metal.15. A transition metal complex claim 10 , comprising: a transition metal; and a compound according to coordinating to the transition metal.16. The transition metal complex according to claim 13 , being used as a catalyst in an asymmetric synthesis reaction.17. The transition metal complex according to claim 14 , being used as a catalyst in an ...

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27-05-2021 дата публикации

PREPARATION OF PSILOCYBIN, DIFFERENT POLYMORPHIC FORMS, INTERMEDIATES, FORMULATIONS AND THEIR USE

Номер: US20210155642A1
Принадлежит: COMPASS PATHFINDER LIMITED

This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin. 130-. (canceled)31. A pharmaceutical composition , comprising crystalline Hydrate A of psilocybin and a pharmaceutically acceptable excipient , wherein the Hydrate A is characterized by X-ray powder diffraction (XRPD) peaks at 8.9±0.1 , 13.8±0.1 , 19.4±0.1 , 23.1±0.1 and 23.5±0.1 °2θ ,wherein the psilocybin has a chemical purity of greater than 97% and no single impurity of greater than 1% as determined by HPLC analysis.32. The pharmaceutical composition of claim 31 , wherein the composition is a capsule.33. The pharmaceutical composition of claim 31 , wherein the composition is a tablet.34. The pharmaceutical composition of claim 31 , wherein the crystalline Hydrate A is further characterized by at least one peak selected from the group consisting of 6.5±0.1 claim 31 , 12.2±0.1 claim 31 , 12.6±0.1 claim 31 , 16.2±0.1 claim 31 , 20.4±0.1 claim 31 , 20.8±0.1 claim 31 , and 21.5±0.1 °2θ.35. The pharmaceutical composition of claim 31 , wherein the composition comprises 1 mg to 40 mg of the crystalline Hydrate A of psilocybin.36. The pharmaceutical composition of claim 31 , wherein the composition comprises about 5 mg of the crystalline Hydrate A of psilocybin.37. The pharmaceutical composition of claim 31 , wherein the composition comprises about 10 mg of the crystalline Hydrate A of psilocybin.38. The pharmaceutical composition of claim 31 , wherein the composition comprises about 25 mg of the crystalline Hydrate A of psilocybin.39. Crystalline Hydrate A of psilocybin claim 31 , wherein the crystalline Hydrate A is characterized by X-ray powder diffraction (XRPD) peaks at 8.9±0.1 claim 31 , 13.8±0.1 claim ...

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27-05-2021 дата публикации

Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels

Номер: US20210155643A1
Принадлежит: Vertex Pharmaceuticals Inc

Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. The compounds have the formula (I) wherein R is H or CH 2 OPO(OH) 2 . Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.

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02-05-2019 дата публикации

CHARGED LINKERS AND THEIR USES FOR CONJUGATION

Номер: US20190127400A1
Принадлежит: HANGZHOU DAC BIOTECH CO., LTD.

Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided. 2. The compound of claim 1 , wherein the cell-binding agent is selected from the group consisting of antibodies claim 1 , proteins claim 1 , vitamins (folates) claim 1 , peptides claim 1 , polymeric micelles claim 1 , liposomes claim 1 , lipoprotein-based drug carriers claim 1 , nano-particle drug carriers claim 1 , dendrimers claim 1 , and combination thereof.3. The compound of claim 1 , wherein the cell-binding agent is an antibody claim 1 , a single chain antibody claim 1 , an antibody fragment that binds to the target cell claim 1 , a monoclonal antibody claim 1 , a single chain monoclonal antibody claim 1 , or a monoclonal antibody fragment that binds the target cell claim 1 , a chimeric antibody claim 1 , a chimeric antibody fragment that binds to the target cell claim 1 , a domain antibody claim 1 , a domain antibody fragment that binds to the target cell claim 1 , a resurfaced antibody claim 1 , a resurfaced single chain antibody claim 1 , or a resurfaced antibody fragment that binds to the target cell claim 1 , a humanized antibody or a resurfaced antibody claim 1 , a humanized single chain antibody claim 1 , or a humanized antibody fragment that binds to the target cell claim 1 , a lymphokine claim 1 , a hormone claim 1 , a vitamin claim 1 , a growth factor claim 1 , a colony stimulating factor claim 1 , or a nutrient-transport molecule.4. The compound of claim 1 , wherein the cell-binding agent binds to target cells which are selected from the group consisting of tumor cells claim 1 , virus infected cells claim 1 , microorganism infected cells claim 1 , parasite infected cells claim 1 , autoimmune cells claim 1 , activated cells claim 1 , myeloid cells claim 1 , activated T-cells claim 1 , B cells claim 1 , or melanocytes; cells expressing the CD19 claim 1 , CD20 claim 1 , CD22 claim 1 , CD30 claim 1 , CD33 claim 1 ...

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02-05-2019 дата публикации

CHARGED LINKERS AND THEIR USES FOR CONJUGATION

Номер: US20190127401A1
Принадлежит: HANGZHOU DAC BIOTECH CO., LTD.

Cell binding agent-drug conjugates comprising phosphinate-based charged linkers and methods of using such linkers and conjugates are provided. 2. The compound of claim 1 , wherein the Drug is selected from the group consisting of a toxin claim 1 , a chemotherapeutic agent claim 1 , a drug moiety claim 1 , an antibiotic claim 1 , a radioactive isotope claim 1 , and a nucleolytic enzyme.4. The compound of claim 1 , wherein Drug is selected from the group consisting of tubulysins claim 1 , calicheamicins claim 1 , auristatins claim 1 , maytansinoids claim 1 , CC-1065 compounds claim 1 , morpholinos doxorubicins claim 1 , taxanes claim 1 , cryptophycins claim 1 , epothilones claim 1 , and benzodiazepine dimers consisting of dimers of pyrrolobenzodiazepine claim 1 , tomaymycin claim 1 , indolinobenzodiazepines claim 1 , imidazobenzothiadiazepines claim 1 , and oxazolidinobenzodiazepines claim 1 , siRNA or a combination thereof claim 1 , and pharmaceutically acceptable salts claim 1 , or acids of any of the above.5. The compound of claim 1 , wherein the Drug is selected from the group consisting of tubulysins claim 1 , maytansinoids claim 1 , taxanoids claim 1 , CC-1065 compounds claim 1 , daunorubicin and doxorubicin compounds claim 1 , benzodiazepine dimers consisting of dimers of pyrrolobenzodiazepine claim 1 , tomaymycin claim 1 , anthramycin claim 1 , indolinobenzodiazepines claim 1 , imidazobenzothiadiazepines claim 1 , and oxazolidinobenzodiazepines claim 1 , calicheamicins and the enediyne antibiotics claim 1 , actinomycin claim 1 , azaserines claim 1 , bleomycins claim 1 , epirubicin claim 1 , tamoxifen claim 1 , idarubicin claim 1 , dolastatins/auristatins consisting of monomethyl auristatin E claim 1 , MMAE claim 1 , MMAF claim 1 , auristatin PYE claim 1 , auristatin TP claim 1 , auristatins 2-AQ claim 1 , 6-AQ claim 1 , EB (AEB) claim 1 , and EFP (AEFP) claim 1 , duocarmycins claim 1 , thiotepa claim 1 , vincristine claim 1 , hemiasterlins claim 1 , and ...

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23-04-2020 дата публикации

Phosphonium-ion tethered tetracycline drugs for treatment of cancer

Номер: US20200123182A1
Принадлежит: Oxford University Innovation Ltd

This invention relates to compounds that are useful as cancer therapies. The compounds comprise derivatives of tetracycline antibiotics, e.g. doxycycline, having a phosphonium cation tethered to the tetracycline tetracycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds.

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02-05-2019 дата публикации

OLIGONUCLEOTIDE COMPOSITIONS AND METHODS THEREOF

Номер: US20190127733A1
Принадлежит:

Among other things, the present disclosure relates to designed oligonucleotides, compositions, and methods thereof. In some embodiments, provided oligonucleotide compositions provide altered splicing of a transcript. In some embodiments, provided oligonucleotide compositions have low toxicity. In some embodiments, provided oligonucleotide compositions provide improved protein binding profiles. In some embodiments, provided oligonucleotide compositions have improved delivery. In some embodiments, provided oligonucleotide compositions have improved uptake. In some embodiments, the present disclosure provides methods for treatment of diseases using provided oligonucleotide compositions. 2. The composition of claim 1 , wherein the reference condition is absence of the composition claim 1 , and the pattern of backbone chiral centers comprises at least two chirally controlled centers independently selected from Rp and Sp.3. The composition of claim 2 , wherein the pattern of backbone linkages comprises one or more backbone linkages selected from phosphodiester claim 2 , phosphorothioate and phosphodithioate linkages.4. The composition of claim 3 , wherein oligonucleotides of the particular oligonucleotide type each further comprise one or more sugar modifications.5. The composition of claim 4 , wherein the sugar modifications comprise one or more modifications selected from: 2′-O-methyl claim 4 , 2′-MOE claim 4 , 2′-F claim 4 , morpholino and bicyclic sugar moieties.6. The composition of claim 5 , wherein the sugar modifications comprise one or more 2′-F sugar moieties.7. The composition of claim 5 , wherein the sugar modifications comprise one or more 2′-O-methyl sugar moieties.811-. (canceled)12. The composition of claim 2 , wherein the base sequence comprises a sequence having no more than 5 mismatches from a 20 base long portion of the dystrophin gene or its complement claim 2 , the length is no more than 50 bases claim 2 , the pattern of backbone chiral centers ...

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19-05-2016 дата публикации

FORMYLPYRROLE-BASED HETEROCYCLES FOR NUCLEIC ACID ATTACHMENT TO SUPPORTS

Номер: US20160137677A1
Принадлежит:

A compound has Formula I: 2. The compound of claim 1 , wherein the protected aldehyde is selected from the group consisting of an acetal claim 1 , an aminal claim 1 , a dithioacetal claim 1 , a protected hemiaminal claim 1 , an alkene claim 1 , and a protected hemithioacetal.3. The compound of claim 1 , wherein W claim 1 , X claim 1 , Y claim 1 , and Z comprise a fused ring system selected from the group consisting of a benzene claim 1 , a pyridine claim 1 , a furan claim 1 , a thiophene claim 1 , a pyridazine claim 1 , a pyrazine claim 1 , and a pyrimidine.4. The compound of claim 3 , wherein W claim 3 , X claim 3 , Y claim 3 , and Z comprise a fused benzene ring.5. The compound of claim 1 , wherein A is hydrogen or methyl claim 1 , Q is a protected aldehyde claim 1 , Ris N-iPr claim 1 , and Ris OCHCHCN.6. The compound of claim 1 , wherein A is a hydroxyl claim 1 , alkoxy or hydroxyalkyl claim 1 , Q is a protected aldehyde claim 1 , Ris N-iPr claim 1 , and Ris OCHCHCN.8. The compound of claim 7 , wherein the protected aldehyde is selected from the group consisting of an acetal claim 7 , an aminal claim 7 , a dithioacetal claim 7 , a protected hemiaminal claim 7 , an alkene claim 7 , and a protected hemithioacetal.9. The compound of wherein W claim 7 , X claim 7 , Y claim 7 , and Z comprise a fused ring system selected from the group consisting of a benzene claim 7 , a pyridine claim 7 , a furan claim 7 , a thiophene claim 7 , a pyridazine claim 7 , a pyrazine claim 7 , and a pyrimidine.10. The compound of claim 9 , wherein W claim 9 , X claim 9 , Y claim 9 , and Z comprise a fused benzene ring.11. The compound of claim 7 , wherein A is hydrogen or methyl claim 7 , Q is a protected aldehyde claim 7 , Nu is selected from the group consisting of a 3′-phosphate-linked nucleic acid claim 7 , a 3′-thiophosphate-linked nucleic acid claim 7 , and a 3′-phosphate linked modified nucleic acid.12. The compound of claim 7 , wherein A is hydrogen or methyl claim 7 , Q is a ...

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21-05-2015 дата публикации

PROCESS FOR THE PREPARATION OF TRIS(PERFLUOROALKYL)PHOSPHINE OXIDES AND BIS(PERFLUOROALKYL)PHOSPHINIC ACIDS

Номер: US20150141698A1
Принадлежит: Merck Patent GmBH

The invention relates to a method for producing tris(perfluoroalkyl)phosphine oxides and bis(perfluoroalkyl)phosphinic acids by reacting tris(perfluoroalkyl)difluorophosphorane or bis(perfluoroalkyl)trifluorophosphorane with non-metal oxides, metalloid oxides or organic compounds with basic oxygen residues. 1. Process for the preparation of compounds of the formula (I){'br': None, 'sub': x', '2x+1', 'n', '3-n, '(CF)P(O)(F)\u2003\u2003(I)'} {'br': None, 'sub': x', '2x+1', 'n', '3-n, '(CF)P(O)(OH)\u2003\u2003(II)'}, 'or of compounds of the formula (I) and compounds of the formula (II)'}where, in the formulae (I) and (II), x is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12 and n=2 or 3, {'br': None, 'sub': x', '2x+1', 'n', '5-n, '(CF)P(F)\u2003\u2003(III),'}, 'comprising at least the reaction of compounds of the formula (III)'}where x and n have one of the meanings indicated above,with non-metal oxides, semimetal oxides or organic compounds containing basic oxygen residues, where the reaction is optionally carried out in the presence of water.2. Process according to claim 1 , characterised in that compounds of the formula (III) where x denotes 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 or 6 are employed.3. Process according to claim 1 , characterised in that compounds of the formula (II) are selected from tris(pentafluoroethyl)difluorophosphorane claim 1 , tris(heptafluoropropyl)difluorophosphorane claim 1 , tris(nonafluorobutyl)difluorophosphorane claim 1 , tris(undecafluoropentyl)difluorophosphorane claim 1 , tris(tridecafluorohexyl)difluorophosphorane claim 1 , bis(heptafluoropropyl)trifluorophosphorane claim 1 , bis(nonafluorobutyl)trifluorophosphorane and bis(tridecafluorohexyl)trifluorophosphorane.4. Process according to claim 1 , characterised in that non-metal oxides or semimetal oxides are used.5. Process according to claim 1 , characterised in that SO claim 1 , POCl claim 1 , PO claim 1 , COor SeOis used.6. Process according to claim 1 , characterised in that SO claim 1 ...

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01-09-2022 дата публикации

LIGHT-EMITTING DEVICE AND ELECTRONIC APPARATUS INCLUDING THE SAME

Номер: US20220278296A1
Принадлежит:

Provided are a light-emitting device and an electronic apparatus including the same. The light-emitting device includes: a first electrode; a second electrode facing the first electrode; an interlayer located between the first electrode and the second electrode; and an electron transport capping layer located outside the second electrode, wherein the interlayer includes an emission layer and an electron transport region, one of the electron transport region and the electron transport capping layer includes a first compound represented by Formula 1, and the other one includes the first compound, a second compound represented by Formula 2, or a combination thereof, and the electron transport region further includes a metal dopant: 2. The light-emitting device of claim 1 , wherein the electron transport capping layer includes the first compound claim 1 , andthe electron transport region includes the second compound and the metal dopant.3. The light-emitting device of claim 1 , wherein the electron transport region includes an electron transport layer claim 1 , andthe electron transport layer includes the first compound, the second compound, or a combination thereof; and the metal dopant.4. The light-emitting device of claim 3 , wherein the electron transport layer includes the second compound and the metal dopant.5. The light-emitting device of claim 4 , wherein the metal dopant includes alkali metal claim 4 , alkaline earth metal claim 4 , rare earth metal claim 4 , or a combination thereof.6. The light-emitting device of claim 4 , wherein an amount of the metal dopant in the electron transport layer is 5 wt % or less.7. The light-emitting device of claim 3 , wherein the electron transport region further includes a hole-blocking layer claim 3 , an electron control layer claim 3 , an electron injection layer claim 3 , or any combination thereof.8. The light-emitting device of claim 3 , wherein the electron transport region consists of the electron transport layer.9. ...

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02-05-2019 дата публикации

Organic Light Emitting Diode Comprising an Organic Semiconductor Layer

Номер: US20190131531A1
Принадлежит:

The invention relates to an Organic light emitting diode comprising an anode electrode, a cathode electrode, at least one emission layer and an organic semiconductor layer, wherein the organic semiconductor layer is arranged between the anode electrode and the cathode electrode and the organic semiconductor layer comprises an alkali organic complex and a compound of formula 1 wherein X is selected from O, S or Se; and Rand Rare independently selected from the group consisting of Cto C, aryl group and Cto Cheteroaryl group, wherein each of Rand Rmay independently be unsubstituted or substituted with at least one Cto Calkyl group or Cto Calkoxy group, preferably Cto Calkyl group or Cto Calkoxy group; and each R, R, R, and Rare independently selected from the group consisting of H, Cto Calkyl group or Cto Calkoxy group, preferably H, Cto Calkyl group or Cto Calkoxy group; a method for preparing the same and the compound of Formula 1 comprised therein. 2. Organic light emitting diode according to claim 1 , wherein the compound of formula 1 the biphenylene group is attached to the adjacent phosphorous containing group and/or the adjacent anthracenylene group in meta-position.3. Organic light emitting diode according to claim 1 , wherein the organic semiconductor layer is arranged between the emission layer and the cathode electrode.4. Organic light emitting diode according to claim 1 , wherein the organic light emitting diode further comprises an electron transport layer arranged between the emission layer and the organic semiconductor layer.5. Organic light emitting diode according to claim 1 , wherein the cathode electrode comprises at least one substantially metallic cathode layer comprising a first zero-valent metal selected from the group consisting of alkali metal claim 1 , alkaline earth metal claim 1 , rare earth metal claim 1 , group 3 transition metal and mixtures thereof.6. Organic light emitting diode according to claim 5 , wherein the substantially metallic ...

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