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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 3660. Отображено 100.
08-03-2012 дата публикации

Phosphonate Compounds

Номер: US20120058975A1
Автор: Ganesh D. Kini, James R. Beadle, Karl Y. Hostetler
Принадлежит: UNIVERSITY OF CALIFORNIA

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.

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Номер записи: 1
07-06-2012 дата публикации

Rare-earth complex and uses thereof

Номер: US20120140439A1
Автор: Kohei Miyata, Takuya Nakashima, Tetsuya Nakagawa, Tsuyoshi Kawai, Yasuchika Hasegawa
Принадлежит: Nara Institute of Science and Technology NUC

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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Номер записи: 2
23-08-2012 дата публикации

Photoelectric conversion device and solar cell using the same

Номер: US20120211082A1
Автор: Hitoshi Oota, Junya Kawai, Misako Okabe, Saika Ootsubo, Seiji Akiyama, Takaaki Niinomi, Takamichi Yokoyama, Yoshiko Moritake, Yuhei Ogomi
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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Номер записи: 3
20-09-2012 дата публикации

Triptolide prodrugs

Номер: US20120238529A1
Автор: Ashok K. Saluja, Ingrid Gunda Georg, Rohit Chugh, Satish Prakash Patil, Selwyn M. Vickers
Принадлежит: University of Minnesota

The invention provides compounds of formula (I): or a salt thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using the compounds of formula I.

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Номер записи: 4
15-11-2012 дата публикации

Novel compounds with high therapeutic index

Номер: US20120289471A1
Автор: V. Ravi Chandran
Принадлежит: Signature R&D Holdings LLC

The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.

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Номер записи: 5
25-04-2013 дата публикации

Curable polysiloxane coating composition

Номер: US20130101840A1
Автор: George G.I. Moore, Kanta Kumar, Larry D. Boardman, Michael A. Semonick, Michele A. Craton, Yu Yang
Принадлежит: 3M Innovative Properties Co

A curable composition comprises (a) at least one polydiorganosiloxane, fluorinated polydiorganosiloxane, or combination thereof comprising reactive silane functionality comprising at least two hydroxysilyl moieties; (b) at least one polydiorganosiloxane, fluorinated polydiorganosiloxane, or combination thereof comprising reactive silane functionality comprising at least two hydrosilyl moieties; and (c) at least one base selected from amidines, guanidines, phosphazenes, proazaphosphatranes, and combinations thereof; wherein at least one of the components (a) and (b) has an average reactive silane functionality of at least three.

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Номер записи: 6
25-04-2013 дата публикации

Curable-on-demand polysiloxane coating composition

Номер: US20130101841A1
Автор: George G.I. Moore, Larry D. Boardman, Michael A. Semonick, Michele A. Craton, Yu Yang
Принадлежит: 3M Innovative Properties Co

A curable composition comprises (a) at least one polydiorganosiloxane, fluorinated polydiorganosiloxane, or combination thereof comprising reactive silane functionality comprising at least two hydroxysilyl moieties; (b) at least one polydiorganosiloxane, fluorinated polydiorganosiloxane, or combination thereof comprising reactive silane functionality comprising at least two hydrosilyl moieties; and (c) at least one photoactivatable composition that, upon exposure to radiation, generates at least one base selected from amidines, guanidines, phosphazenes, proazaphosphatranes, and combinations thereof; wherein at least one of the components (a) and (b) has an average reactive silane functionality of at least three.

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Номер записи: 7
02-05-2013 дата публикации

Method of ameliorating oxidative stress and supplementing the diet

Номер: US20130108605A1
Автор: Boyd E. Haley, Niladri Narayan Gupta
Принадлежит: University of Kentucky Research Foundation

A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R 1 is an aromatic backbone and R 2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R 2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.

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Номер записи: 8
16-05-2013 дата публикации

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

Номер: US20130119367A1
Автор: Jang Sang Eok, Jeon Soon Ok, Lee Jun Yeob, Son Hyo Suk, Yook Kyoung Soo
Принадлежит: INDUSTRY ACADEMIC COOPERATION FOUNDATION, DANKOOK UNIVERSITY

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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Номер записи: 9
06-06-2013 дата публикации

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

Номер: US20130142735A1
Автор: Balaraman Kalyanaraman, Douglas Edward Prah, Joy Joseph, Kathleen Marie Schmainda, Marcos Lopez, Micael Joël Hardy
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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Номер записи: 10
20-06-2013 дата публикации

NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY

Номер: US20130157982A1
Автор: Cappiello John, Heidelbaugh Todd M., Nguyen Phong X.
Принадлежит: ALLERGAN, INC.

The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to claim 1 , wherein:{'sup': 1', '10, 'Ris N or C—R;'}{'sup': '2', 'Ris optionally substituted aromatic heterocycle or optionally substituted cycloalkenyl;'}{'sup': 3', '11', '12', '13', '14, 'Ris O, N—R, CH—Ror S, —CR═CR—, —C(O) or —C≡C—;'}{'sup': '4', 'Ris H, optionally substituted aromatic heterocycle, optionally substituted non-aromatic heterocycle, optionally substituted cycloalkyl, optionally substituted cycloalkenyl or optionally substituted aryl;'}{'sup': '5', 'sub': 1-3', '1-3, 'Ris H, halogen, hydroxyl, —OCalkyl, or Calkyl;'}{'sup': '6', 'sub': 1-3', '1-3, 'Ris H, Calkyl, halogen, hydroxyl or —OCalkyl;'}{'sup': '7', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': '8', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': 9', '15, 'sub': 3', '2', '2', '3-6', '2, 'Ris —OPOH, —COOH, —P(O)(OH), —Calkyl, —S(O)OH, —P(O)MeOH, —P(O)(H)OH or —OR;'}{'sup': '10', 'sub': 1-6', '1-3, 'Ris H, Calkyl, halogen, hydroxyl or —OCalkyl;'}{'sup': '11', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '12', 'sub': 1-3', '1-3, 'Ris H, Calkyl, halogen, hydroxyl, —OCalkyl or amino;'}{'sup': '13', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '14', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '15', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': 16', '17, 'L is CHR, O, S, NRor —C(O)—;'}a is 0, 1, 2, 3, 4 or 5;b is 0, 1, 2, 3, 4 or 5;c is 0 or 1;d is 0, 1, 2 or 3;{'sup': '16', 'sub': 1-3', '1-3, 'Ris H, Calkyl, —OCalkyl, halogen, hydroxyl or amino, and'}{'sup': '17', 'sub': '1-3', 'Ris H or Calkyl;'}with the provisos:{'sup': 3', '11', '17, 'a). when Ris O, N—R, or S, and b is 0 or 1 then L is not O, S, or NR; and'}{'sup': '9', 'sub': 3', '2', '2', '2, 'b). when Ris —OPOH, —COOH, —P(O)(OH), —S(O)OH, —P(O)MeOH or —P(O)(H)OH'}then d is not 0; and{'sup': 9', '15, 'c). when Ris ORthen d is not ...

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Номер записи: 11
20-06-2013 дата публикации

Prostaglandin-bisphosphonate conjugate compounds, methods of making same, and uses thereof

Номер: US20130157984A1
Автор: Anne Moreau, Monzur Morshad, Robert N. Young, Romelo Gibe, Stephen Arns
Принадлежит: SIMON FRASER UNIVERSITY

The invention provides in part, conjugate compounds. The invention also provides synthesis methods for making the compounds, and uses of the compounds.

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Номер записи: 12
19-09-2013 дата публикации

SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES

Номер: US20130244958A1
Автор: Bartkovitz David Joseph, Chu Xin-Jie, FISHLOCK Daniel, Vu Binh Thanh, Zhao Chunlin
Принадлежит: Hoffmann-La Roche Inc.

There are provided compounds of the formula 3. The compound of whereinX is selected from H, F or Cl,Y is selected from H, F or Cl,{'sub': '1', 'Ris lower alkyl or substituted lower alkyl,'}{'sub': '3', 'Ris hydrogen or lower alkyl,'}{'sub': 5', '2', '2', 'n', '2', '2', 'n', '3, 'Ris selected from —(OCHCH)—OH or —(OCHCH)—OCHwherein n is from 45-55 and'}{'sub': '6', 'Ris hydrogen'}or a pharmaceutically acceptable salt thereof.5. A compound of selected from the group consisting of1-(Ethyl(isopropyl)carbamoyloxy)ethyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate,4-{[(2R,3S,4R,5S)-3-(3-Chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid di-tert-butoxy-phosphoryloxymethyl ester,4-{[(2R,3S,4R,5S)-3-(3-Chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid 1-[bis-(2-methoxy-ethyl)-carbamoyloxy]-ethyl ester,4-Methyl-piperazine-1-carboxylic acid 1-(4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoyloxy)-ethyl ester,1-Acetoxyethyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate,Rac-1-(isobutyryloxy)ethyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate,4-{[(2R,3S,4R,5S)-4-(4-Chloro-2-fluoro-phenyl)-3-(3-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid acetoxymethyl ester,1-(Cyclohexyloxycarbonyloxy)ethyl 4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxybenzoate,Rac-1-(isopropoxycarbonyloxy)ethyl 4-((2R,3S ...

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Номер записи: 13
26-09-2013 дата публикации

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

Номер: US20130251647A1
Автор: BOLLSCHWEILER Claus, PELZER Ralf, SIEGEL Wolfgang, Subkowski Thomas, WITTENBERG Jens
Принадлежит: BASF SE

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators. 123.-. (canceled)27. The method according to claim 27 , where claim 27 , in the compound of the formula (II) claim 27 , X is not a methylene or linear 1 claim 27 ,4-butylene bridge.28. The method according to claim 27 , in which claim 27 , in the compounds of the formula II claim 27 , R claim 27 , Rand Rare H and{'sub': 22', '23, 'Rand R, together with the carbon atoms to which they are bonded, form a methylenedioxy group.'}29. The method according to claim 27 , in which claim 27 , in the compounds of the formula II claim 27 , the radicals Rand R claim 27 , independently of one another claim 27 , are an in each case mononuclear aryl or heteroaryl radical or a C-C-cycloalkyl radical.31. The method according to claim 25 , where the receptor is brought into contact with at least one compound which claim 25 , in a cellular activity test using cells which recombinantly express the human TRPM8 receptor claim 25 , modulates the permeability of these cells for Ca ions.32. The method according to claim 25 , where the modulating compound has an agonistic or antagonistic effect on the cellular Ca ion permeability.33. The method according to claim 25 , where the modulating compound is a TRPM8 receptor agonist.34. The use of a compound according to the definition in for inducing a sensation of coldness in humans and/or animals claim 25 , in particular for non-therapeutic purposes.35. The use of a compound according to the definition in as active constituent of a pharmaceutical composition.36. The use of a compound according to the definition in for the treatment of prostate carcinomas claim 25 , for the treatment of bladder weakness or in pain therapy.37. The use of a compound ...

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Номер записи: 14
26-09-2013 дата публикации

Salts of prodrugs of piperazine and substituted piperidine antiviral agents

Номер: US20130253196A1
Автор: Chung-Pin H. Chen, David Kenneth Leahy, Dominique Thoraval, John F. Kadow, Kap-Sun Yeung, Kathia Levesque, Nachimuthu Soundararajan, Nicholas A. Meanwell, Pierre Sirard, Shawn K. Pack, Tao Wang, Timothy P. Connolly, Yasutsugu Ueda, Zhongxing Zhang
Принадлежит: BRISTOL-MYERS SQUIBB COMPANY

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R 1 does not exist; W is C or N with the proviso that when W is N, R 2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C 1 -C 6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

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Номер записи: 15
31-10-2013 дата публикации

Pantothenate derivatives for the treatment of neurologic disorders

Номер: US20130289001A1
Автор: Andrew Vaino, Marek BIESTEK, Martin SHKRELI
Принадлежит: Retrophin Inc

The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.

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Номер записи: 16
05-12-2013 дата публикации

SUBSTITUTED PYRROLIDINE-2-CARBOXAMIDES

Номер: US20130324531A1
Автор: Bartkovitz David Joseph, Chu Xin-Jie, Ehrlich George Kenneth, Liu Jin-Jun, Michel Hanspeter, Vu Binh Thanh, Zhao Chunlin
Принадлежит: Hoffmann-La Roche Inc.

There are provided compounds of the formula 2. The compound of whereinX is selected from H, F or Cl,{'sub': '1', 'Y is selected from H, F or C,'}{'sub': '1', 'Ris lower alkyl or substituted lower alkyl,'}{'sub': 3', '2', '3', '2', '2', '2', 'n', '2', '2', 'n', '3', '2', '2', 'n', '4', '2', '2', '2', '2', 'n', '2', '2', '2', 'n', '3', '2', '2', 'n', '3', '2', '2', 'n', '2', '2', '2', 'n', '3', '5', '2', '5', '2', '2', '5', '2', '5', '2', '2', 'n', '2', '2', '2, 'Ris selected from the group consisting of lower alkoxy, substituted lower alkoxy, alkylamino, dialkylamino, glucuronic acid, hexoses, aminohexoses, pyranoses, aminoglycosides, natural and unnatural amino acids, —OCHC(O)N(CH), —(OCHCH)—OH, —(OCHCH)—OCH, —(OCHCH)—OP(O)(OR), —OCHC(O)—(OCHCH)—OH, —OCHC(O)—(OCHCH)—OCH, —NH(CHCHO)—CH, —NH(CHCHO)—H, —OCHC(O)NH(CHCHO)—CH, —O—R, —OCH—R, OCHCH—R, —OCHC(O)—R, —NH(OCHCH)—NHand —OCHCH-amino acid, wherein n is from 3 to 60,'}{'sub': '4', 'Ris hydrogen or benzyl,'}{'sub': '5', 'Ris selected from the group consisting of heterocycles, substituted heterocycles, dialkylamino, alkylamino and aminoalkyl alcohols,'}or a pharmaceutically acceptable salt or ester thereof.3. The compound of whereinX is selected from H, F or Cl,Y is selected from H, F or Cl,{'sub': '1', 'Ris lower alkyl or substituted lower alkyl,'}{'sub': 3', '2', '3', '2', '2', '2', 'n', '2', '2', 'n', '3', '2', '2', 'n', '4', '2', '2', '2', '2', 'n', '2', '2', '2', 'n', '3', '2', '2', 'n', '3', '2', '2', 'n', '2', '2', '2', 'n', '3', '5', '2', '5', '2', '2', '5', '2', '5', '2', '2', 'n', '2', '2', '2, 'Ris selected from the group consisting of lower alkoxy, substituted lower alkoxy, alkylamino, dialkylamino, glucuronic acid, hexoses, aminohexoses, pyranoses, aminoglycosides, natural and unnatural amino acids, —OCHC(O)N(CH), —(OCHCH)—OH, —(OCHCH)—OCH, —(OCHCH)—OP(O)(OR), —OCHC(O)—(OCHCH)—OH, —OCHC(O)—(OCHCH)—OCH, —NH(CHCHO)—CH, —NH(CHCHO)—H, —OCHC(O)NH(CHCHO)—CH, —O—R, —OCH—R, OCHCH—R, —OCHC(O)—R, —NH(OCHCH)—NHand — ...

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Номер записи: 17
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
Автор: Balaraman Kalyanaraman, David A. Zarling, Hirak S. Basu, Joy Joseph
Принадлежит: Colby Pharmaceutical Co, MEDICAL COLLEGE OF WISCONSIN

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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Номер записи: 18
16-01-2014 дата публикации

Protein affinity tag and uses thereof

Номер: US20140017797A1
Автор: Adrianus Petrus Josephus Maria De Jong, Geert Petrus Maria Mommen, Gijsbert Zomer, Hugo Derk Meiring, Martinus Richardus Jozef Hamzink
Принадлежит: De Staadt der Nederlanden vert doorde minister van VWS

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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Номер записи: 19
06-02-2014 дата публикации

ORGANOGOLD COMPLEXES AND METHODS FOR MAKING THE SAME

Номер: US20140039200A1
Автор: Bobin Mariusz, Gallop Christopher, Viseux Eddy Michel Elie
Принадлежит: The University of Sussex

The present invention relates to chiral ligands deriving from α- and β-amino acids, and from metal complexes formed from the same. The ligands are useful with catalytic gold complexes, particularly Au(I) complexes. 12. A compound as defined in any preceding claim , wherein the Au is Au(I).13. A compound as defined in any preceding claim wherein A denotes SOor C(═O).14. A compound as defined in any preceding claim wherein R denotes C-C-alkyl , C-C-fluoroalkyl; or phenyl optionally substituted with 1 to 5 R15. A compound as defined in any preceding claim wherein A-R denotes SOCH , SOC-C-perfluoroalkyl , SOCHMe , SOCHNOor COCHBr.16. A compound as defined in any preceding claim wherein A-R denotes SOCH , SOCF , SOCHMe , SOCHNOor COCHBr.17. A compound as defined in any preceding claim wherein L denotes P(R) , S(R)or N(R).18. A compound as defined in any preceding claim wherein L denotes P(R).19. A compound as defined in any preceding claim wherein L denotes P(R); and Rdenotes CH , CH; or phenyl optionally substituted with 1 to 5 R.20. A compound as defined in any preceding claim wherein L denotes P(R); and Rdenotes phenyl optionally substituted with 1 to 5 R.21. A compound as defined in any preceding claim wherein Rdenotes C-C-alkyl.22. A compound as defined in any preceding claim wherein Rdenotes methyl.23. A compound as defined in any preceding claim wherein Rdenotes C-C-alkyl.24. A compound as defined in any preceding claim wherein Rdenotes methyl25. A compound as defined in any preceding claim wherein Rdenotes H or C-C-alkyl26. A compound as defined in any preceding claim wherein v denotes 1; and t denotes an integer from 2 to 4.27. A compound as defined in any preceding claim wherein v denotes 1; and t denotes 2.2825. A compound as defined in any of - wherein v denotes 0.29. A compound as defined in any preceding claim wherein u denotes 0.3028. A compound as defined in any of - wherein u denotes 1.31. A compound as defined in any preceding claim wherein Rdenotes ...

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Номер записи: 20
13-02-2014 дата публикации

Phosphonate Compounds

Номер: US20140045794A1
Автор: Beadle James R., Hostetler Karl Y.
Принадлежит: The Regents of the University of California

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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Номер записи: 21
10-04-2014 дата публикации

COLD MENTHOL RECEPTOR-1 ANTAGONISTS

Номер: US20140100194A1
Автор: Colburn Raymond W, Dax Scott L., Flores Christopher M., Matthews Jay M.
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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Номер записи: 22
04-01-2018 дата публикации

Salts of prodrugs of piperazine and substituted piperidine antiviral agents

Номер: US20180000849A1
Автор: Chung-Pin H. Chen, David Kenneth Leahy, Dominique Thoraval, John F. Kadow, Kap-Sun Yeung, Kathia Levesque, Nachimuthu Soundararajan, Nicholas A. Meanwell, Pierre Sirard, Shawn K. Pack, Tao Wang, Timothy P. Connolly, Yasutsugu Ueda, Zhongxing Zhang
Принадлежит: ViiV Healthcare UK No 4 Ltd

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R 1 does not exist; W is C or N with the proviso that when W is N, R 2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C 1 -C 6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

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Номер записи: 23
04-01-2018 дата публикации

PROCESS FOR THE PREPARATION OF ACYLPHOSPHANES

Номер: US20180002357A1
Автор: Gruetzmacher Hansjoerg, MUELLER Georgina
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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Номер записи: 24
20-01-2022 дата публикации

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

Номер: US20220017549A1
Автор: Araujo Joseph, Slassi Abdelmalik
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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Номер записи: 25
03-01-2019 дата публикации

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

Номер: US20190006589A1
Автор: Ganier Jerome, Rothe Carsten, Senkovskyy Volodymyr
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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Номер записи: 26
20-01-2022 дата публикации

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Номер: US20220020937A1
Автор: AHN Heechoon, HWANG Seokhwan, JEON Mina, JUN Mieun, KIM Sungbum, Kim Youngkook, KO Soobyung
Принадлежит:

An organic light-emitting device includes a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, the organic layer including an emission layer. The emission layer includes at least one heterocyclic compound of Formula 1. The heterocyclic compound may be a host or a delayed fluorescent dopant. The organic light-emitting device including the heterocyclic compound may have a low driving voltage, high efficiency, high luminance, and a long lifespan. 2. The organic light-emitting device of claim 1 , whereina1, a2, b1, and b2 satisfy a1+b1=1 and a2+b2=1.3. The organic light-emitting device of claim 1 , whereinb1 and b2 satisfy b1+b2=0 or b1+b2=1.4. The organic light-emitting device of claim 1 , wherein claim 1 ,{'sub': 2', '1', '2', '19', '19', '20', '19', '20, 'when Yis O, Yis a single bond, S, SO, N(R), C(R)(R), or Si(R)(R).'}5. The organic light-emitting device of claim 1 , wherein{'sub': 1', '2', '6', '30', '2', '30, 'Arand Arare each independently a substituted or unsubstituted aromatic C-Ccarbocyclic group or a substituted or unsubstituted π electron-depleted nitrogen-containing C-Cheterocyclic group.'}6. The organic light-emitting device of claim 1 , wherein{'sub': 1', '4, 'Ato Aare each independently a benzene group, a pyridine group, or a pyrimidine group, and'}{'sub': 5', '8, 'Ato Aare each independently a benzene group, a pyridine group, or a pyrimidine group.'}7. The organic light-emitting device of claim 1 , wherein{'sub': 1', '2', '19', '19', '20', '19', '20, 'Yis a single bond, O, S, SO, N(R), C(R)(R), or Si(R)(R),'}{'sub': 2', '2', '19', '19', '20', '19', '20, 'Yis a single bond, O, S, SO, N(R), C(R)(R), or Si(R)(R), and'}{'sub': 3', '2', '19', '19', '20', '19', '20, 'Yis a single bond, O, S, SO, N(R), C(R)(R), or Si(R)(R),'}{'sub': 2', '3, 'provided that Yand Yare not both a single bond at the same time.'}9. The organic light-emitting device of claim 1 , wherein{'sub': ...

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Номер записи: 27
19-01-2017 дата публикации

Substituted bisphenyl butanoic phosphonic acid derivatives as nep inhibitors

Номер: US20170015688A1
Автор: David Weninger BARNES, Dean Franklin Rigel, Scott Louis COHEN
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

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Номер записи: 28
17-01-2019 дата публикации

Ultra bright dimeric or polymeric dyes

Номер: US20190016898A1
Автор: Michael VANBRUNT, Sharat Singh, Tracy Matray
Принадлежит: Sony Corp, Sony Corp of America

or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, L1, L2, L3, L4, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

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Номер записи: 29
16-01-2020 дата публикации

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

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

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

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Номер записи: 30
18-01-2018 дата публикации

Heterocyclic compound and organic light-emitting device including the same

Номер: US20180019410A1
Автор: Eunjae JEONG, Hyoyoung Lee, Junha PARK, Munki SIM, Seokhwan Hwang, Youngkook Kim
Принадлежит: Samsung Display Co Ltd

A heterocyclic compound and an organic light-emitting device including the same are provided, the heterocyclic compound being represented by <Formula 1>

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Номер записи: 31
26-01-2017 дата публикации

Butyl-bridged diphosphine ligands for alkoxycarbonylation

Номер: US20170022138A1
Автор: Dieter Hess, Dirk Fridag, Frank Geilen, Helfried Neumann, Kaiwu DONG, Katrin Marie Dyballa, Matthias Beller, Ralf Jackstell, Robert Franke, Xiangjie FANG
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to compounds of formula (I) where 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; and to the use thereof as ligands in alkoxycarbonylation.

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Номер записи: 32
26-01-2017 дата публикации

FERROCENE-BASED COMPOUNDS AND PALLADIUM CATALYSTS BASED THEREON FOR THE ALKOXYCARBONYLATION OF ETHYLENICALLY UNSATURATED COMPOUNDS

Номер: US20170022235A1
Автор: Beller Matthias, DONG Kaiwu, DYBALLA Katrin Marie, Franke Robert, Fridag Dirk, GEILEN Frank, HESS Dieter, Jackstell Ralf, NEUMANN Helfried
Принадлежит: EVONIK DEGUSSA GmbH

The invention relates to a compound of formula (I) 2. Compound according to claim 1 ,{'sup': 1', '3, 'where Rand Rare each independently selected from furyl, thienyl, 2-pyrrolyl, 4-imidazolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, pyrazolyl, furazanyl, tetrazolyl.'}3. Compound according to claim 1 ,{'sup': 1', '3, 'where Rand Rare each independently selected from furyl and thienyl.'}4. Compound according to claim 1 ,{'sup': 2', '4, 'sub': 1', '12', '3', '12', '6', '20, 'where Rand Rare each independently selected from —(C-C)-alkyl, —(C-C)-cycloalkyl and —(C-C)-aryl.'}5. Compound according to claim 1 ,{'sup': 2', '4, 'sub': 1', '12, 'where Rand Rare each —(C-C)-alkyl.'}6. Compound according to claim 1 ,{'sup': 1', '3, 'where Rand Rmay each independently be substituted by one or more substituents selected from'}{'sub': 1', '12', '3', '12', '1', '12', '1', '12', '6', '20', '3', '12', '6', '20', '6', '20', '1', '12', '6', '20', '1', '12, '—(C-C)-alkyl, —(C-C)-cycloalkyl, —O—(C-C)-alkyl, —O—(C-C)-alkyl-(C-C)-aryl, —O—(C-C)-cycloalkyl, —(C-C)-aryl, —(C-C)-aryl-(C-C)-alkyl, —(C-C)-aryl-O—(C-C)-alkyl.'}7. Compound according to claim 1 ,{'sup': 3', '4, 'sub': 1', '12', '3', '12', '3', '12', '6', '20, 'where Rand R, if they are —(C-C)-alkyl, —(C-C)-cycloalkyl, —(C-C)-heterocycloalkyl or —(C-C)-aryl,'}{'sub': 1', '12', '3', '12', '1', '12', '1', '12', '6', '20', '3', '12', '6', '20', '6', '20', '1', '12', '6', '20', '1', '12, 'may each independently be substituted by one or more substituents selected from —(C-C)-alkyl, —(C-C)-cycloalkyl, —O—(C-C)-alkyl, —O—(C-C)-alkyl-(C-C)-aryl, —O—(C-C)-cycloalkyl, —(C-C)-aryl, —(C-C)-aryl-(C-C)-alkyl, —(C-C)-aryl-O—(C-C)-alkyl.'}10. Complex comprising Pd and a compound according to .12. Process according to claim 11 ,wherein the ethylenically unsaturated compound is selected from ethene, propene, 1-butene, cis- and/or trans-2-butene, isobutene, 1,3-butadiene, 1-pentene, cis- and/or trans-2-pentene, 2-methyl-1-butene, 3-methyl-1- ...

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Номер записи: 33
25-01-2018 дата публикации

Ether compounds for treatment of complement mediated disorders

Номер: US20180022766A1
Автор: Akihiro Hashimoto, Atul Agarwal, Avinash S. Phadke, Dawei Chen, Godwin Pais, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Venkat Rao Gadhachanda, Xiangzhu Wang
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 (R 32 ) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

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Номер записи: 34
25-01-2018 дата публикации

Compounds for Treatment of Complement Mediated Disorders

Номер: US20180022767A1
Автор: Agarwal Atul, Chen Dawei, Deshpande Milind, Gadhachanda Venkat Rao, Hashimoto Akihiro, Pais Godwin, Phadke Avinash S., Wang Qiuping, Wang Xiangzhu, Wiles Jason Allan
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 are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. 7. The pharmaceutical composition of claim 6 , wherein Xis CRand Xis CR.8. The pharmaceutical composition of claim 7 , wherein Ris C-Calkyl.9. The pharmaceutical composition of claim 8 , wherein Ris hydrogen.10. The pharmaceutical composition of claim 8 , wherein C-Calkyl is methyl.11. The pharmaceutical composition of claim 10 , wherein Ris hydrogen.12. The pharmaceutical composition of claim 7 , wherein Rand Rare both hydrogen.17. The pharmaceutical composition of claim 1 , wherein the composition is suitable for delivery to a human.18. The pharmaceutical composition of claim 1 , wherein the composition is suitable for systemic delivery.19. The pharmaceutical composition of claim 1 , wherein the composition is suitable for topical delivery.20. The pharmaceutical composition of claim 1 , wherein the composition is suitable for ocular delivery.21. The pharmaceutical composition of claim 1 , wherein the composition is suitable for intravitreal delivery. This application is a continuation of U.S. application Ser. No. 14/631,828, filed Feb. 25, 2015, which claims the benefit of provisional U.S. Application No. 61/944,189 filed Feb. 25, 2014, provisional U.S. Application No. 62/022,916 filed Jul. 10, 2014, and provisional U.S. Application 62/046,783 filed Sep. 5, 2014. The entirety of each of ...

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Номер записи: 35
24-01-2019 дата публикации

ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS

Номер: US20190023729A1
Автор: Agarwal Atul, Chen Dawei, Deshpande Milind, Gadhachanda Venkat Rao, Hashimoto Akihiro, Pais Godwin, Phadke Avinash S., Wang Qiuping, Wang Xiangzhu, Wiles Jason Allan
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 Ror Ron the A group is an aryl, heteroaryl or heterocycle (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. 2. The process of claim 1 , wherein Rand R are independently chosen from hydrogen claim 1 , halogen claim 1 , and C-Calkyl.3. The process of claim 1 , wherein Ris hydrogen.5. The process of claim 1 , wherein Ris hydrogen.6. The process of claim 1 , wherein B is —(C-Calkyl)(aryl) or —(C-Calkyl)(heteroaryl); each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R claim 1 , and 0 or 1 substituents chosen from Rand R.7. The process of claim 1 , wherein B is —(C-Calkyl)(heteroaryl) which is unsubstituted or substituted with one or more substituents independently chosen from Rand R.8. The process of claim 1 , wherein Ris selected from halogen and C-Calkyl.14. The process of claim 13 , wherein Rand R are independently chosen from hydrogen claim 13 , halogen claim 13 , and C-Calkyl.15. The process of claim 14 , wherein Ris C-Calkanoyl.16. The process of claim 15 , wherein B is —(C-Calkyl)(heteroaryl); each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R.17. The process of claim 16 , wherein Ris hydrogen.18. The process of claim 17 , wherein Ris selected from halogen and C-Calkyl. This application is a continuation of U.S ...

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Номер записи: 36
28-01-2021 дата публикации

SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS

Номер: US20210023098A1
Автор: Chen Chung-Pin H., Connolly Timothy P., Kadow John F., LEAHY David Kenneth, LEVESQUE Kathia, Meanwell Nicholas A., PACK Shawn K., SIRARD Pierre, SOUNDARARAJAN Nachimuthu, THORAVAL Dominique, Ueda Yasutsugu, WANG TAO, Yeung Kap-Sun, Zhang Zhongxing
Принадлежит:

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. 1. The compound This application is a continuation application of U.S. Ser. No. 16/190,632, filed Nov. 14, 2018, now pending, which is a continuation application of U.S. Ser. No. 15/704,100, filed Sep. 14, 2017, now pending, which is a continuation application of U.S. Ser. No. 15/249,827, filed Aug. 29, 2016, abandoned, which is a continuation application of U.S. Ser. No. 14/704,183 filed May 5, 2015, abandoned, which is a continuation application of U.S. Ser. No. 14/249,638 filed Apr. 10, 2014, abandoned, which is a continuation application of U.S. Ser. No. 13/861,804 filed Apr. 12, 2013, now U.S. Pat. No. 8,871,771, which is a continuation application of U.S. Ser. No. 13/429,838 filed Mar. 26, 2012, now U.S. Pat. No. 8,461,333, which is a continuation application of U.S. Ser. No. 12/767,222 filed Apr. 26, 2010, now U.S. Pat. No. 8,168,615, which is a continuation application of U.S. Ser. No. 11/066,745 filed Feb. 25, 2005, now U.S. Pat. No. 7,745,625, which claims the benefit of U.S. Provisional Application Ser. No. 60/635,231 filed Dec. 10, 2004 and 60/553,320 filed Mar. 15, 2004, now expired. The entire teachings of the referenced applications are herein incorporated by reference in their entirety.This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with new prodrug derivatives with antiviral activity. More particularly, the present invention relates to compounds useful for the treatment of HIV and AIDS.HIV-1 (human immunodeficiency virus-1) infection remains a major medical problem, with an estimated 42 million people infected worldwide at the end of 2002. The number of cases of HIV and AIDS (acquired immunodeficiency syndrome) has risen rapidly. In 2002, ˜5.0 million new infections were reported, and 3.1 million people ...

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Номер записи: 37
23-01-2020 дата публикации

LIGHT EMITTING DEVICES AND COMPOUNDS

Номер: US20200028093A2
Автор: Wong Michael, Zysman-Colman Eli
Принадлежит:

Thermally Activated Delayed Fluorescence (TADF) compounds wherein two aromatic heterocyclic moieties are provided as acceptor groups, spaced apart from two donor moieties by an aromatic spacer ring, are described. Charged organic TADF species having a similar structure are also described. The TADF compounds and charged organic TADF species may be employed as emitter material in light emitting devices such as OLEDs and LEECs. Also described TADF compounds wherein at least one donor moiety is substituted by at least one substituent that is a phosphine oxide or a phosphine sulphide. 137-. (canceled)44. A light emitting device comprising a TADF compound according to .45. The light emitting device of claim 44 , wherein said light emitting device is an OLED.492. The TADF compound according to claim 46 , wherein the acceptor moieties Acc are claim 46 , independently for each occurrence selected from the group consisting of -Het as defined in claim claim 46 , —CN claim 46 , sulfone claim 46 , sulfoxide claim 46 , imine claim 46 , amide claim 46 , acridine claim 46 , acridinium claim 46 , carboxylate ester claim 46 , phosphine oxide claim 46 , phosphine sulfide claim 46 , ketone and aldehyde.52. A light emitting device comprising a TADF compound according to .53. The light emitting device of claim 52 , wherein said light emitting device is an OLED.57. The charged organic species according to claim 56 , wherein at least one linking group L is present and is independently for each occurrence claim 56 , a hydrocarbylene chain claim 56 , that may be substituted or unsubstituted claim 56 , hydrocarbylene or unsaturated hydrocarbylene.58. The charged organic species according to claim 57 , wherein the at least one linking group L is selected from substituted or unsubstituted cyclopentane-1 claim 57 ,3-diyl claim 57 , cyclohexane-1 claim 57 ,4-diyl claim 57 , 1 claim 57 ,4-phenylene and 4 claim 57 ,4′-biphenylene.60. The charged organic species according to claim 56 , wherein ...

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Номер записи: 38
29-01-2015 дата публикации

FORMYLPYRROLE-BASED HETEROCYCLES FOR NUCLEIC ACID ATTACHMENT TO SUPPORTS

Номер: US20150031833A1
Автор: Smith Randall, Smith Ryan Christopher, Zhao Xiaodong
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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Номер записи: 39
04-02-2016 дата публикации

PHOTORESPONSIVE NUCLEOTIDE ANALOGUE HAVING PHOTOCROSSLINKING ABILITY

Номер: US20160031918A1
Автор: Fujimoto Kenzo, Sakamoto Takashi, Tanaka Yuya
Принадлежит: JAPAN ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY

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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Номер записи: 40
01-02-2018 дата публикации

ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS

Номер: US20180030075A1
Автор: Agarwal Atul, Chen Dawei, Deshpande Milind, Gadhachanda Venkat Rao, Hashimoto Akihiro, Pais Godwin, Phadke Avinash S., Wang Qiuping, Wang Xiangzhu, Wiles Jason Allan
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 Ror Ron the A group is an aryl, heteroaryl or heterocycle (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. 12. The pharmaceutical composition of claim 1 , wherein B is —(C-Calkyl)(aryl) or —(C-Calkyl)(heteroaryl) each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R claim 1 , and 0 or 1 substituents chosen from Rand R.13. The pharmaceutical composition of claim 12 , wherein B is —(CH)(aryl) substituted with two substituents independently chosen from Rand R.14. The pharmaceutical composition of claim 13 , wherein Ris halogen.15. The pharmaceutical composition of claim 14 , wherein there are two Rsubstituents and one is chlorine and the other is fluorine.18. The pharmaceutical composition of claim 12 , wherein B is aryl or heteroaryl each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R.19. The pharmaceutical composition of claim 18 , wherein B is aryl.20. The pharmaceutical composition of claim 18 , wherein B is heteroaryl.21. The pharmaceutical composition of claim 20 , wherein heteroaryl is 2-pyridine.22. The pharmaceutical composition of claim 21 , wherein 2-pyridine is substituted with one substituent independent chosen from R.23. The pharmaceutical composition of claim 22 , wherein Ris halogen.31. The ...

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Номер записи: 41
31-01-2019 дата публикации

Compounds for treatment of complement mediated disorders

Номер: US20190031692A1
Автор: Akihiro Hashimoto, Atul Agarwal, Avinash S. Phadke, Dawei Chen, Godwin Pais, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Venkat Rao Gadhachanda, Xiangzhu Wang
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 are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

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Номер записи: 42
04-02-2021 дата публикации

Non-Aqueous Electrolyte Solution for Lithium Secondary Battery and Lithium Secondary Battery Including the Same

Номер: US20210036364A1
Автор: KIM Hyun Seung, Lee Chul Haeng, Lee Hyun Yeong, YU Sung Hoon
Принадлежит: LG CHEM, LTD.

A non-aqueous electrolyte solution and a lithium secondary battery including the same are disclosed herein. In some embodiments, a non-aqueous electrolyte solution includes a lithium salt, an organic solvent, and a compound represented by Formula 1 as an additive. The compound has an excellent effect of removing a decomposition product, such as HF and PF, generated from the lithium salt in the electrolyte solution. The lithium secondary battery has improved high-temperature storage characteristics by including the non-aqueous electrolyte solution. 2. The non-aqueous electrolyte solution for a lithium secondary battery of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Rto Rare each independently an unsubstituted or substituted alkylene group having 2 to 10 carbon atoms.3. The non-aqueous electrolyte solution for a lithium secondary battery of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Rto Rare each independently an unsubstituted or substituted alkylene group having 3 to 7 carbon atoms.4. The non-aqueous electrolyte solution for a lithium secondary battery of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Rto Reach independently comprise at least one selected from the group consisting of —CRH—CRH—CRH— claim 1 , —CRH—CRH—CRH—CRH— claim 1 , and —CRH—CRH—CRH—CRH—CRH— claim 1 , where Rto Rare each independently hydrogen or an alkyl group having 1 to 2 carbon atoms).5. The non-aqueous electrolyte solution for a lithium secondary battery of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Rto Reach independently comprise at least one selected from the group consisting of —CH—CH—CH— claim 1 , —CH—CH—CH—CH— claim 1 , and —CH—CH—CH—CH—CH—.7. The non-aqueous electrolyte solution for a lithium secondary battery of claim 1 , wherein the compound represented by Formula 1 is included in an amount of 0.1 wt % to 2.0 wt % based on a total weight of the non-aqueous electrolyte solution.8. The non-aqueous electrolyte solution for a lithium secondary battery of claim 7 ...

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Номер записи: 43
04-02-2021 дата публикации

MODIFIED IONIC LIQUIDS CONTAINING PHOSPHORUS

Номер: US20210036369A1
Автор: Abbate Luigi, Moganty Surya, Sinicropi John, Torres Gabriel, Wu Yue
Принадлежит: NOHMS Technologies, Inc.

The present disclosure is directed to a phosphorus-modified ionic liquid compound, the synthesis thereof and an electrochemical cell electrolyte containing the phosphorus-modified ionic liquid compound. 2. The compound of claim 1 , wherein either or both of A and B is CAT+.3. The compound of claim 1 , wherein either or both of Rand Ris phenyl claim 1 , wherein any of the carbon or hydrogen atoms therein are optionally further substituted with a halide claim 1 , alkyl claim 1 , alkenyl claim 1 , alkoxy claim 1 , aryl claim 1 , alkynyl claim 1 , alkylsiloxy claim 1 , phenyl claim 1 , benzyl claim 1 , silyl claim 1 , thioether claim 1 , sulfoxide claim 1 , azo claim 1 , amino or silane.4. The compound of claim 1 , wherein Y is S.6. The electrolyte of claim 5 , wherein the aprotic organic solvent comprises open-chain or cyclic carbonates claim 5 , carboxylic acid esters claim 5 , nitrites claim 5 , ethers claim 5 , sulfones claim 5 , ketones claim 5 , lactones claim 5 , dioxolanes claim 5 , glymes claim 5 , crown ethers claim 5 , siloxanes claim 5 , phosphoric acid esters claim 5 , phosphates claim 5 , phosphites claim 5 , mono- or polyphosphazenes or mixtures thereof.7. The electrolyte of claim 5 , wherein the additive comprises sulfur-containing compounds claim 5 , phosphorus-containing compounds claim 5 , boron-containing compounds claim 5 , silicon-containing compounds claim 5 , fluorine-containing compounds claim 5 , nitrogen-containing compounds claim 5 , compounds containing at least one unsaturated carbon-carbon bond claim 5 , carboxylic acid anhydrides or the mixtures thereof.8. The electrolyte of claim 5 , where either or both of A and B is CAT+.9. The electrolyte of claim 5 , where either or both of Rand Ris phenyl claim 5 , wherein any of the carbon or hydrogen atoms therein are optionally further substituted with a halide claim 5 , alkyl claim 5 , alkenyl claim 5 , alkoxy claim 5 , aryl claim 5 , alkynyl claim 5 , alkylsiloxy claim 5 , phenyl claim 5 , ...

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Номер записи: 44
12-02-2015 дата публикации

Fluorescent phospholipid ether compounds, compositions, and methods of use

Номер: US20150044142A1
Автор: Anatoly PINCHUK, Irawati Kandela, Jamey P. Weichert, Marc LONGINO, William R. Clarke
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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Номер записи: 45
18-02-2021 дата публикации

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

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

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

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Номер записи: 46
18-02-2016 дата публикации

NOVEL PYRROLE DERIVATIVES

Номер: US20160046576A1
Автор: Andrew Peter William, Damaso Mafalda Pires, Davies Mark William, Frickel Fritz-Frieder, Hamza Daniel, Hirst Simon Christopher, Lonnen Rana
Принадлежит:

There are provided inter alia compounds of formula (I) 2. The compound of wherein Rand Rare independently selected from —C(O)NRR claim 1 , —C(O)OR claim 1 , CN claim 1 , —C(O)R claim 1 , —C(O)NHC(O)R claim 1 , —NO claim 1 , —SOR claim 1 , —SOR claim 1 , —SOR claim 1 , —SONRR claim 1 , —SONH—C(O)ORand optionally substituted phenyl or heteroaryl.36-. (canceled)7. The compound of wherein Ris substituted phenyl or phenyl having a substituent in the meta or para positions relative to the pyrrole ring.8. The compound of wherein Ris phenyl substituted by one or more substituents independently selected from halo claim 7 , cyano claim 7 , hydroxyl claim 7 , C-Calkoxy claim 7 , C-Chydroxyalkoxy claim 7 , C-Cfluoroalkoxy claim 7 , C-Calkyl claim 7 , C-Cfluoroalkyl claim 7 , —C(O)NRR claim 7 , where Rand Rare independently selected from hydrogen and C-Calkyl; —O—Rwherein Ris —(CH)—P(O)(OR) claim 7 , where x is 0 claim 7 , 1 claim 7 , 2 claim 7 , 3 or 4 and Ris independently selected from hydrogen and C-Calkyl claim 7 , —(CH)—S(O)Me where y is 1 claim 7 , 2 claim 7 , 3 or 4 claim 7 , —C-Calkylheterocyclyl which heterocyclyl group may be optionally substituted by C-Calkyl claim 7 , —C-Calkylphenyl which phenyl group may be optionally substituted by C-Calkoxy claim 7 , or phenyl or 5- or 6-membered heteroaryl which phenyl or heteroaryl group may optionally be substituted by a group selected from C-Calkyl and halo; or —(O(CH))OR claim 7 , where each z claim 7 , which may be the same or different claim 7 , represents 2 or 3 claim 7 , p represents 1 claim 7 , 2 claim 7 , 3 claim 7 , 4 or 5 and Ris hydrogen or C-Calkyl; or two adjacent carbon atoms within Rmay be linked by —O—CH—O—.9. The compound of wherein Ris phenyl substituted by 1 claim 8 , 2 or 3 substituents independently selected from:{'sub': 1', '6', '2', 'x', '2', '1', '3', '2', 'y', '2, 'sup': 15', '15', '23', '23', '15, '(i) C-Calkoxy; —O—Rwherein Ris —(CH)—P(O)(OR), where x is 0, 1, 2, 3 or 4 and Ris independently ...

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Номер записи: 47
15-02-2018 дата публикации

PRODRUGS OF PYRIDONE AMIDES USEFUL AS MODULATORS OF SODIUM CHANNELS

Номер: US20180044361A1
Автор: Alcacio Tim Edward, Anderson Corey, Belmont Daniel T., Golec Julian Marian Charles, Hadida-Ruah Sara Sabina, Keshavarz-Shokri Ali, Littler Benjamin Joseph, Zhang Beili
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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Номер записи: 48
19-02-2015 дата публикации

Phosphonate Compounds

Номер: US20150051174A1
Автор: James R. Beadle, Karl Y. Hostetler
Принадлежит: UNIVERSITY OF CALIFORNIA

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.

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Номер записи: 49
13-02-2020 дата публикации

Salts of prodrugs of piperazine and substituted piperidine antiviral agents

Номер: US20200046743A1
Автор: Chung-Pin H. Chen, David Kenneth Leahy, Dominique Thoraval, John F. Kadow, Kap-Sun Yeung, Kathia Levesque, Nachimuthu Soundararajan, Nicholas A. Meanwell, Pierre Sirard, Shawn K. Pack, Tao Wang, Timothy P. Connolly, Yasutsugu Ueda, Zhongxing Zhang
Принадлежит: ViiV Healthcare UK No 4 Ltd

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R 1 does not exist; W is C or N with the proviso that when W is N, R 2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C 1 -C 6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

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Номер записи: 50
14-02-2019 дата публикации

ETHER COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS

Номер: US20190048033A1
Автор: Agarwal Atul, Chen Dawei, Deshpande Milind, Gadhachanda Venkat Rao, Hashimoto Akihiro, Pais Godwin, Phadke Avinash S., Wang Qiuping, Wang Xiangzhu, Wiles Jason Allan
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 Ror Ron the A group is an ether (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. 7. The compound of claim 6 , wherein Ris hydrogen claim 6 , and wherein B is —(C-Calkyl)(heteroaryl) or —(C-Calkyl)(biphenyl) each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R claim 6 , and 0 or 1 substituents chosen from Rand R.8. The compound of claim 7 , wherein B is substituted with 0 substituents chosen from Rand R.9. The compound of claim 8 , wherein B is substituted with 0 substituents chosen from R.10. The compound of claim 9 , wherein B is aryl claim 9 , heteroaryl claim 9 , or biphenyl.11. The compound of claim 10 , wherein Ris halogen.16. A pharmaceutical composition comprising an effective amount of a compound of or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable carrier.17. The pharmaceutical composition of claim 16 , wherein the composition is suitable for systemic delivery.18. The pharmaceutical composition of claim 16 , wherein the composition is suitable for topical delivery.19. The pharmaceutical composition of claim 16 , wherein the composition is suitable for ocular delivery.20. The pharmaceutical composition of claim 16 , wherein the composition is suitable for intravitreal delivery. This application is a continuation of U.S. patent ...

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Номер записи: 51
10-03-2022 дата публикации

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

Номер: US20220073548A1
Автор: Brown Christopher, LONDESBROUGH Derek John, MOORE GILLIAN, Nichols David E., Northen Julian Scott, PATIL HEMANT KASHINATH
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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Номер записи: 52
15-05-2014 дата публикации

Phosphoric Acid Ester Derivatives

Номер: US20140135292A1
Автор: Jun Chiba, Mamoru Otoyo, Nobuo Machinaga, Ryotaku Inoue, Ryuji Hashimoto
Принадлежит: Daiichi Sankyo Co Ltd

To provide a novel compound that has S1P lyase inhibitory ability and induces a reduction in the number of lymphocytes, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the compound or pharmaceutically acceptable salt thereof as an active ingredient. A compound represented by the general formula (I): or a pharmaceutically acceptable salt thereof.

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Номер записи: 53
02-03-2017 дата публикации

Ether Compounds for Treatment of Medical Disorders

Номер: US20170057993A1
Автор: Akihiro Hashimoto, Atul Agarwal, Avinash S. Phadke, Dawei Chen, Godwin Pais, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Venkat Rao Gadhachanda, Xiangzhu Wang
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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Номер записи: 54
10-03-2016 дата публикации

PHOSPHORUS FUNCTIONAL ANTIMICROBIAL COATINGS FOR METAL SURFACES

Номер: US20160066579A1
Автор: Foucher Daniel, POROSA Lukasz, WOLFAARDT Gideon
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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Номер записи: 55
08-03-2018 дата публикации

Ablative, renewable, multi-functional protective coating for dental surfaces

Номер: US20180064625A1
Автор: Denis Bendejacq, Robert Lee Reierson
Принадлежит: Rhodia Operations SAS

An oral care composition in the form of a toothpaste, tooth gel, dentifrice, tooth powder, prophy paste, mouthwash, rinse, tooth mousse, dental floss, chewing gum, soluble oral care strip or film for direct application or attachment to an oral surface, or lozenge for combating dental caries, erosion, hypersensitivity, and/or staining that includes an orally acceptable carrier and a copolymer of a first α, β-ethylenically unsaturated phosphate compound (A); and one or more α, β-ethylenically unsaturated co-monomers, at least one of which is other than an allyl-functional co-monomer, wherein (A) is an allyl phosphate compound of formula (A): [CH 2 ═CH—CH 2 —O(R 1 O) a (R 2 O) b ] x P(O)(OM) 3-x   (A) wherein, R 1 is a substituted or unsubstituted (C 2 -C 4 ) alkylene moiety; R 2 is a substituted or unsubstituted (C 2 -C 4 ) alkylene moiety; M is identical or different, hydrogen, alkali metal, ammonium, protonated alkyl amine, protonated alkanolamine, or protonated basic amino acid; X is 1 or 2, a is from 1 to 20; and b is from 0 to 20. Methods for combating dental caries, erosion, hypersensitivity, and/or staining are also provided.

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Номер записи: 56
09-03-2017 дата публикации

Pharmaceutical dosage form for immediate release of an indolinone derivative

Номер: US20170065529A1
Автор: Dirk Trommeshauser, Peter Lach, Peter Stopfer, Roman Messerschmid, Thorsten SOKOLIESS
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to a pharmaceutical dosage form delivering an immediate release profile containing the active substance 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate.

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Номер записи: 57
27-02-2020 дата публикации

ARYL, HETEROARYL, AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS

Номер: US20200062790A1
Автор: Agarwal Atul, Chen Dawei, Deshpande Milind, Gadhachanda Venkat Rao, Hashimoto Akihiro, Pais Godwin, Phadke Avinash S., Wang Qiuping, Wang Xiangzhu, Wiles Jason Allan
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 Ror Ron the A group is an aryl, heteroaryl or heterocycle (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. 6. The compound of claim 1 , wherein B is (C-Calkyl)(aryl) or (C-Calkyl)(heteroaryl) each of which B is unsubstituted or substituted with one or more substituents independently chosen from Rand R claim 1 , and 0 or 1 substituents chosen from Rand R.7. The compound of claim 6 , wherein Ris halogen.8. The compound of claim 6 , wherein B is 2-pyridine.12. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.13. A method for the treatment of a disorder mediated by complement factor D claim 1 , comprising administering an effective amount to a host in need thereof of a compound of or a pharmaceutically acceptable salt thereof claim 1 , optionally in a pharmaceutically acceptable carrier.14. The method of claim 13 , wherein the host is a human.15. The method of claim 14 , wherein the disorder is age-related macular degeneration (AMD) or retinal degeneration.16. The method of claim 14 , wherein the disorder is an ophthalmic disease.17. The method of claim 14 , wherein the disorder is paroxysmal nocturnal hemoglobinuria (PNH).18. The method of claim 14 , wherein the disorder is multiple sclerosis claim 14 , arthritis claim 14 , a respiratory ...

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Номер записи: 58
08-03-2018 дата публикации

Water soluble fluorescent or colored dyes comprising conjugating groups

Номер: US20180065998A1
Автор: C. Frederick Battrell, John C. Kumer, Kenneth FARBER, Michael VANBRUNT, Tracy Matray
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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Номер записи: 59
15-03-2018 дата публикации

ALKYNE COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS

Номер: US20180072762A1
Автор: Agarwal Atul, Chen Dawei, Deshpande Milind, Gadhachanda Venkat Rao, Hashimoto Akihiro, Pais Godwin, Phadke Avinash S., Wang Qiuping, Wang Xiangzhu, Wiles Jason Allan
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 Ror Ron the A group is an alkyne (R) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. 2. The compound of claim 1 , wherein the compound is a hydrochloride salt. This application is a continuation of U.S. application Ser. No. 14/631,090, filed Feb. 25, 2015, which claims the benefit of provisional U.S. Application No. 61/944,189, filed Feb. 25, 2014, provisional U.S. Application No. 62/022,916, filed Jul. 10, 2014, and provisional U.S. Application 62/046,783, filed Sep. 5, 2014. The entirety of each of these applications is hereby incorporated by reference for all purposes.The complement system is a part of the innate immune system which does not adapt to changes over the course of the host's life, but is recruited and used by the adaptive immune system. For example, it assists, or complements, the ability of antibodies and phagocytic cells to clear pathogens. This sophisticated regulatory pathway allows rapid reaction to pathogenic organisms while protecting host cells from destruction. Over thirty proteins and protein fragments make up the complement system. These proteins act through opsonization (enhancing phaogytosis of antigens), chemotaxis (attracting macrophages and neutrophils), cell lysis (rupturing membranes of foreign cells) and agglutination (clustering and binding of pathogens together).The complement system has three ...

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Номер записи: 60
16-03-2017 дата публикации

ORGANOMETALLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME

Номер: US20170077427A1
Автор: Ito Naoyuki, Jeong Hyein, KIM Jin, Kim Seulong, Kim Yeong-Eun, KIM Younsun, Lee Jungsub, Lee Yunho, Shin Dongwoo
Принадлежит:

An organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, the organic layer including an emission layer, wherein the organic layer includes a condensed cyclic compound represented by Formula 1. An organic light-emitting device including the organometallic compound according to the embodiments of the present disclosure may have high efficiency: 2. The organometallic compound of claim 1 , wherein M is copper (Cu).3. The organometallic compound of claim 1 , wherein Xis selected from P(R)(R) and N(R)(R); and Xis selected from P(R)(R) and N(R)(R).4. The organometallic compound of claim 1 , wherein CYand CYare each independently selectted from a benzene claim 1 , a naphthalene claim 1 , a fluorene claim 1 , a spiro-fluorene claim 1 , an indene claim 1 , a pyrrole claim 1 , a thiophene claim 1 , a furan claim 1 , an imidazole claim 1 , a pyrazole claim 1 , a thiazole claim 1 , an isothiazole claim 1 , an oxazole claim 1 , an isoxazole claim 1 , a triazole claim 1 , a pyridine claim 1 , a pyrazine claim 1 , a pyrimidine claim 1 , a pyridazine claim 1 , a quinoline claim 1 , an isoquinoline claim 1 , a benzoquinoline claim 1 , a quinoxaline claim 1 , a quinazoline claim 1 , a carbazole claim 1 , a benzoimidazole claim 1 , a benzofuran claim 1 , a benzothiophene claim 1 , an isobenzothiophene claim 1 , a benzoxazole claim 1 , an isobenzoxazole claim 1 , a triazole claim 1 , a tetrazole claim 1 , an oxadiazole claim 1 , a triazine claim 1 , a dibenzofuran claim 1 , a dibenzothiophene claim 1 , a benzofuropyridine claim 1 , and a benzothienopyridine.5. The organometallic compound of claim 1 , wherein CYand CYare each independently selected from a benzene claim 1 , a naphthalene claim 1 , an indene claim 1 , and a pyridine.6. The organometallic compound of claim 1 , wherein Z claim 1 , Z claim 1 , and Rto Rare each independently selected from:{'sub': 1', ...

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Номер записи: 61
14-03-2019 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

Номер: US20190076450A1
Автор: Dhar T.G. Murali, Dyckman Alaric J., Gilmore John L., Marcoux David, Xiao Hai-Yun, Xiao Zili, Yang Michael G.
Принадлежит:

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 116-. (canceled)19. The compound according to or a salt thereof claim 17 , wherein:{'sub': 2a', '2', '3', '3', '2', '5-6', '3', '2', '2', '3', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '2', '2', '4', '2', '2', '4', '3', '2', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '2', '2', '3', '3', '2', '1-3', '3', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '2', '2', '1-2', '3', '2', '2', '2', '2', '2', '2-3', '2', '2', '3-4', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '9', '3', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '3', '2', '3', '3', '2', '3', '3', '3', '3', '2', '1-6', '3', '3', '2', '2', '3', '2', '2', '3', '3', '3', '2', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '2', '3', '2', '2', '2', '2', '3', '2', '3', '2', '3', '2', '3', '2', '2', '2-4', '3', '2', '3', '2', '2', '2', '3', '2', '2', '2', '3', '3', '2', '2', '2', '3', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '1-2', '3', '2', '2', '2', '3', '2', '2', '3', '3', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '3', '3', '2', '2', '2', '3', '3', '2', '2', '2', '2', '4', '3', '2', '2', '4', '3', '3', '2', '4', '3', '2', '3', '2', '5', '3', '2', '2', '4-7', '3', '2', '2', '2', '2-4', '3', '2', '2', '2', '3', '2', '2', '2', '2-3', '3', '2', '2', '2', '2', '2', '2', '2', '3', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '2', '2-3', '3', ' ...

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Номер записи: 62
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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Номер записи: 63
22-03-2018 дата публикации

Novel substituted 6,7-dihydro-5h-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof

Номер: US20180079720A1
Автор: Bruno Filoche-Romme, Corinne Terrier, Fabienne Thompson, Frank Halley, Gary McCort, Laurent Schio, Maurice Brollo, Michel Tabart, Monsif Bouaboula, Victor Certal, Youssef El-Ahmad
Принадлежит: SANOFI SA

Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH) 2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH) 2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.

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Номер записи: 64
12-03-2020 дата публикации

ISOINDOLINONE INHIBITORS OF THE MDM2-P53 INTERACTION HAVING ANTICANCER ACTIVITY

Номер: US20200079761A1
Автор: BUCK lldiko Maria, CANO Celine Florence, Chessari Gianni, CONS Benjamin David, GOLDING Bernard Thomas, GRIFFIN Roger John, HARDCASTLE Ian Robert, HIRST Kim Louise, HOLVEY Rhian Sara, Howard Steven, Johnson Christopher Norbert, LEWIS Arwel, MILLER Duncan Charles, MITCHELL Dale Robert, NOBLE Martin Edward Mäntylä, OSBORNE James Daniel, PEACH Joanne, Rees David Charles, ST. DENIS Jeffrey David, TAMANINI Emiliano, WATSON David Wyn, WHITTAKER Benjamin Paul
Принадлежит:

The invention provides a compound of formula (I): 2. A compound according to claim 1 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris:{'sub': 1-4', '2-4', '1-4, '(i) halogen, hydroxy, nitrile, Calkyl, Calkynyl, or Calkoxy; or'}{'sub': 1-4', '1-4', '1-4', '2-6', '1-4', '1-4', '2-4', '2', 'v', '2', '0-1', '2', '1-4', '2', 'v', '1-4', '2', '2', 'd', '1-6', 'd', 'd', '2, 'sup': x', 'y', '8, '(ii) hydroxy, halogen, nitrile, Calkyl, haloCalkyl, hydroxyCalkyl, Calkenyl, Calkoxy, haloCalkoxy, Calkynyl, —(CH)—COH, —O—(CRR)—COCalkyl, —(CH)—CON(Calkyl), —P(═O)(R), —S(O)—Calkyl, —S(O)-heterocyclic group with 3 to 6 ring members or —S(O)—N(R).'}3. A compound according to claim 1 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1 and Ris chloro or nitrile.4. A compound according to claim 3 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 3 , wherein Ris chloro.5. A compound according to claim 1 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris:{'sub': 1-4', '2-6', '1-4, '(i) hydrogen, Calkyl, Calkenyl, or hydroxyCalkyl; or'}{'sup': X', 'y, 'sub': u', '2, '(ii) hydrogen or —(CRR)—COH.'}6. A compound according to claim 1 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —COOH claim 1 , —CHCOOH claim 1 , —CHCH—COH claim 1 , —(CH(CH))—COH or —(C(CH))—COH.7. A compound according to claim 1 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 3', 'x', 'y, 'sub': t', 'q', '3-6, '(i) Ris -(A)-(CRR)—X and A is either a Ccycloalkyl group or a heterocyclic group with 3 to 5 ring members; or'}{'sup': 3', 'x', 'y, 'sub': t', 'q, '(ii) Ris -(A)-(CRR)—X and A is a heterocyclic group with 3 to 5 ring members.'}8. A compound according to claim 1 , or a tautomer or a solvate or a pharmaceutically acceptable salt thereof claim 1 , ...

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Номер записи: 65
25-03-2021 дата публикации

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

Номер: US20210087212A1
Автор: Brown Christopher, LONDESBROUGH Derek John, MOORE GILLIAN, Nichols David E., Northen Julian Scott, PATIL HEMANT KASHINATH
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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Номер записи: 66
21-03-2019 дата публикации

Phosphonate compounds for treatment of complement mediated disorders

Номер: US20190085005A1
Автор: Akihiro Hashimoto, Atul Agarwal, Avinash Phadke, Dawei Chen, Godwin Pais, Jason Allan Wiles, Milind Deshpande, Qiuping Wang, Venkat Rao Gadhachanda, Xiangzhu Wang
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 R12 or R13 on the A group is a phosphonate (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

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Номер записи: 67
19-06-2014 дата публикации

DIPHOSPHINE LIGAND AND TRANSITION METAL COMPLEX USING THE SAME

Номер: US20140171655A1
Автор: Goto Mitsutaka, KAWAGUCHI Shinji, Kawakami Jun-ichi, YAMADA Masatoshi, Yamano Mitsuhisa
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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Номер записи: 68
12-05-2022 дата публикации

COMPOSITIONS AND METHODS OF USE COMPRISING SUBSTANCES WITH NEURAL PLASTICITY ACTIONS ADMINISTERED AT NON-PSYCHEDELIC/PSYCHOTOMIMETIC DOSAGES AND FORMULATIONS

Номер: US20220143051A1
Автор: ALIMONTI Andrea, BRUN Paola, Cavalli Andrea, De Martin Sara, Folli Franco, Giordano Giovanni, Inturrisi Charles E., Lodovichi Claudia, Manfredi Paolo L., Mattarei Andrea, Pappagallo Marco, Rolando Maurizio, Sgrignani Jacopo
Принадлежит:

Compositions and methods of use comprising serotonin (5-HT) receptor agonists and NMDAR modulating substances, including especially certain substances classified as 5-HT2A agonists presently disclosed to exert NMDAR modulating effects, administered as modulators of neural plasticity, at non-psychedelic/psychotomimetic dosages, posology and formulations, for treatment of diseases and conditions and for improving functions (neuroplastogens). 5. A method for preventing or treating diseases and conditions or improving functions in patients or subjects , the method comprising:{'claim-ref': [{'@idref': 'CLM-00001', 'claims 1'}, {'@idref': 'CLM-00004', '4'}], 'administration of a compound of any of - at doses, dosages, posology, or formulations devoid of clinically meaningful psychedelic or psychotomimetic actions or effects, and having clinical effects comparable to those exerted by human plasma psilocin Cmax of 4 ng/ml or less, or human 5-HT2A CNS receptor occupancy of 50% or less, or PD effects comparable to those exerted by human plasma psilocin Tmax in excess of 60 minutes.'}6. The method of claim 5 , wherein said clinical effects are comparable to those exerted by human plasma psilocin Cmax of 2 ng/ml or less or 5-HT2A human CNS receptor occupancy of 40% or less.7. The method of claim 5 , wherein said clinical effects are comparable to those exerted by human plasma psilocin Cmax of 1 ng/ml or less or 5-HT2A human CNS receptor occupancy of 30% or less.8. The method of claim 5 , wherein said PD effects are comparable to those exerted by human plasma psilocin Tmax in excess of 120 minutes.9. The method of claim 5 , wherein said PD effects are comparable to those exerted by human plasma psilocin Tmax in excess of 180 minutes.10. The method of claim 5 , wherein the administering of the compound occurs under conditions that may modulate NMDARs and their subunits in addition to modulate 5-HT2A receptors.11. The method of claim 5 , wherein the administering of the compound ...

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Номер записи: 69
12-05-2022 дата публикации

Double alkoxycarbonylation of dienes as one-pot synthesis

Номер: US20220144750A1
Автор: JI Yang, Malthias Beller, Ralf Jackstell, Robert Franke
Принадлежит: EVONIK OPERATIONS GMBH

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

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Номер записи: 70
01-04-2021 дата публикации

ULTRA BRIGHT DIMERIC OR POLYMERIC DYES WITH SPACING LINKER GROUPS

Номер: US20210096135A1
Автор: Matray Tracy, Singh Sharat
Принадлежит:

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): 2. The compound of claim 1 , wherein G comprises claim 1 , at each occurrence claim 1 , independently an aldehyde claim 1 , oxime claim 1 , hydrazone claim 1 , alkyne claim 1 , amine claim 1 , azide claim 1 , acylazide claim 1 , acylhalide claim 1 , nitrile claim 1 , nitrone claim 1 , sulfhydryl claim 1 , disulfide claim 1 , sulfonyl halide claim 1 , isothiocyanate claim 1 , imidoester claim 1 , activated ester claim 1 , ketone claim 1 , α claim 1 ,β-unsaturated carbonyl claim 1 , alkene claim 1 , maleimide claim 1 , α-haloimide claim 1 , epoxide claim 1 , aziridine claim 1 , tetrazine claim 1 , tetrazole claim 1 , phosphine claim 1 , biotin or thiirane functional group.3. The compound of claim 1 , wherein G comprises claim 1 , at each occurrence claim 1 , independently a reactive group capable of forming a functional group comprising an alkene claim 1 , ester claim 1 , amide claim 1 , thioester claim 1 , disulfide claim 1 , carbocyclic claim 1 , heterocyclic or heteroaryl group claim 1 , upon reaction with the complementary reactive group.4. The compound of claim 3 , wherein the heteroaryl is triazolyl.8. The compound of claim 1 , wherein Ris claim 1 , at each occurrence claim 1 ,{'sup': −', '5, 'sub': 'd', 'independently OH, O or ORand Ris, at each occurrence, oxo.'}9. The compound of claim 1 , wherein Ris H.10. The compound of claim 1 , wherein Rand Rare each independently OH or —OP(═R)(R)R.11. The compound of claim 10 , wherein Ris OL′.12. The compound of claim 11 , wherein L′ is a heteroalkylene linker to: Q claim 11 , a targeting moiety claim 11 , an analyte molecule claim 11 , a solid support claim 11 , a solid support residue claim 11 , a nucleoside or a further compound of structure (I).13. The compound of claim 11 , wherein L′ comprises an alkylene oxide or phosphodiester moiety claim 11 , or combinations thereof.15. The compound of claim 12 , ...

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Номер записи: 71
26-06-2014 дата публикации

COMPOUNDS AND COMPOSITIONS FOR USE IN THE TREATMENT AND PREVENTION OF LUNG AND BRAIN CANCER AND PRECANCEROUS CONDITIONS THEREOF

Номер: US20140178461A1
Автор: RIGAS Basil
Принадлежит:

Novel compounds and pharmaceutical compositions thereof administered by the respiratory route for prevention and/or treatment of lung and brain cancer and precancerous conditions thereof. 6. The method according to claim 1 , wherein Xis —NR— claim 1 , Ris hydrogen; B is —(CH)— claim 1 , and Z is represented by Formula Z-I claim 1 , Rand Rbeing identical C-alkyl substituents.7. (canceled)10. The method according to claim 1 , wherein said method is to prevent a precancerous lung lesion.11. The method according to any one of claim 1 , wherein said method is to prevent a precancerous brain lesion.12. The method according to claim 1 , wherein said method is to prevent or to treat lung cancer a precancerous lung lesion.13. The method according to claim 1 , wherein said method is to prevent or to treat brain cancer.14. The method according to claim 1 , wherein said method is to treat small cell or non-small cell lung cancer.15. The method according to claim 13 , wherein the brain cancer is glioma.16. The method according to claim 1 , wherein the compound is administered as a pharmaceutical composition comprising the compound and a pharmaceutically acceptable excipient.17. The method pharmaceutical composition according to claim 16 , comprising administering said composition to a human or animal by nasal administration.18. The method according to claim 16 , comprising administering said composition to a human or animal in the form of an aerosol.19. The method according to claim 16 , comprising administering said composition to a human or animal in the form of a dry powder aerosol.20. The method according to claim 16 , wherein said composition is formulated in form of nanoparticles.21. The method of claim 20 , wherein said nanoparticles are lipid or polymeric nanoparticles or a combination thereof.22. The method of claim 20 , wherein said nanoparticles are in form of a liposome claim 20 , submicron emulsion claim 20 , microemulsion claim 20 , nanoemulsion claim 20 , lipid ...

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Номер записи: 72
02-06-2022 дата публикации

PROGRAMMABLE POLYMERIC DRUGS

Номер: US20220168433A1
Автор: Battrell C. Frederick, Matray Tracy, Singh Sharat, VanBrunt Michael
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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Номер записи: 73
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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Номер записи: 74
02-06-2022 дата публикации

METHODS OF TREATING NEUROCOGNITIVE DISORDERS, CHRONIC PAIN AND REDUCING INFLAMMATION

Номер: US20220169668A1
Автор: Brown Christopher, CROAL Megan, ERIKSSON Hans Ake, GOLDSMITH George, HICKEY Molly Tabitha, HURLEY Shaun, LONDESBROUGH Derek John, MALIEVSKAIA Ekaterina, MARWOOD Lindsey, MCCULLOCH Drummond E-Wen Joe, MEDHURST Laurie Emma, MOORE GILLIAN, Nichols David E., Northen Julian Scott, PATIL HEMANT KASHINATH, POULSEN Nathan, SELIMBEYOGLU Aslihan, SHUXIANG Amanda Tan, SOULA Anais, VERAART Manon Cecile Elisabeth, WHELAN Tobias Patrick, WILDE Lars Christian, Wright Stephen
Принадлежит:

The disclosure provides methods for treating a subject in need thereof comprising administering to the subject a therapeutically-effective dose of psilocybin. The methods described herein may be used to treat a variety of diseases, disorders, and conditions. For example, the methods may be used to treat neurocognitive disorders (e.g., Alzheimer's disease, Parkinson's disease), ADHD, Epilepsy, Autism, Sleep-wake disorders, Chronic pain, Inflammatory Disorders, IBD, Stroke, ALS, and/or Multiple Sclerosis. 1. A method for treating one or more neurocognitive disorders in a subject in need thereof , the method comprising administering to the subject a therapeutically effective amount of psilocybin or an active metabolite thereof.2. The method of claim 1 , wherein the neurocognitive disorder is major neurocognitive disorder.3. The method of claim 1 , wherein the neurocognitive disorder is due to claim 1 , one or more of Alzheimer's disease claim 1 , Lewy Body Dementia claim 1 , Traumatic Brain Injury claim 1 , Prion Disease claim 1 , HIV Infection claim 1 , Parkinson's disease claim 1 , or Huntington's disease.4. The method of any one of - claim 1 , wherein the subject demonstrates an improvement in one or more of the following: the Mini-Mental State Exam (MMSE) claim 1 , the Mini-Cog test claim 1 , a CANTAB test claim 1 , a Cognigram test claim 1 , a Cognivue test claim 1 , a Cognition test claim 1 , or an Automated Neuropsychological Assessment Metrics test claim 1 , after the administration of psilocybin.5. The method of any one of - claim 1 , wherein the subject has at least one comorbidity claim 1 , and wherein administration of psilocybin ameliorates the comorbidity.6. The method of claim 5 , wherein the comorbidity is hypertension claim 5 , connective tissue disease claim 5 , depression claim 5 , diabetes claim 5 , or chronic pulmonary disease.7. A method for treating a Parkinsonian syndrome or symptom thereof in a subject in need thereof claim 5 , the method ...

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Номер записи: 75
21-04-2016 дата публикации

Semiconducting Material Comprising Aza-Substituted Phosphine Oxide Matrix and Metal Salt

Номер: US20160111654A1
Автор: Zoellner MIke
Принадлежит:

The present invention relates to a semiconducting material including at least one salt or complex of a metal cation and an aza-substituted phosphine oxide compound with improved electrical properties, and to a compound suitable for this organic semiconducting material and an electronic device utilizing the improved electrical properties of the semiconducting material. 2. The semiconducting material according to claim 1 , wherein the metal cation is a cation of a metallic element selected from the main groups of the Periodic Table.3. The semiconducting material according to claim 2 , wherein the metallic element is selected from the first or second main group of the Periodic Table.4. The semiconducting material according to claim 1 , wherein the spacer A is a divalent six-membered aromatic heterocyclic group.5. The semiconducting material according to claim 4 , wherein the spacer A is selected from azine-2 claim 4 ,4-diyl claim 4 , azine-2 claim 4 ,5-diyl claim 4 , azine-2 claim 4 ,6-diyl claim 4 , 1 claim 4 ,3-diazine-2 claim 4 ,4-diyl claim 4 , or 1 claim 4 ,3-diazine-2 claim 4 ,5-diyl.6. The semiconducting material according to claim 1 , wherein the electron transporting unit E is a C-C-aryl or a C-Cheteroaryl.8. The semiconducting material according to claim 7 , wherein at least two groups selected from Y claim 7 , Y claim 7 , Yand Yare H.9. The semiconducting material according to claim 1 , wherein the metal cation is selected from Li and Mg.10. The semiconducting material according to claim 1 , wherein the salt of the metal cation is selected from 8-hydroxyquinolinolate claim 1 , pyrazolylborate claim 1 , or phenolate substituted with a phosphine oxide group.11. An electronic device comprising a cathode claim 1 , an anode claim 1 , and the semiconducting material according to claim 1 , wherein the semiconducting material is arranged between the cathode and the anode.12. The electronic device according to claim 11 , further comprising an electron transporting ...

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Номер записи: 76
18-04-2019 дата публикации

Salts of prodrugs of piperazine and substituted piperidine antiviral agents

Номер: US20190111066A1
Автор: Chung-Pin H. Chen, David Kenneth Leahy, Dominique Thoraval, John F. Kadow, Kap-Sun Yeung, Kathia Levesque, Nachimuthu Soundararajan, Nicholas A. Meanwell, Pierre Sirard, Shawn K. Pack, Tao Wang, Timothy P. Connolly, Yasutsugu Ueda, Zhongxing Zhang
Принадлежит: ViiV Healthcare UK No 4 Ltd

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R 1 does not exist; W is C or N with the proviso that when W is N, R 2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C 1 -C 6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

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Номер записи: 77
09-04-2020 дата публикации

WATER SOLUBLE FLUORESCENT OR COLORED DYES AND METHODS FOR THEIR USE

Номер: US20200109287A1
Автор: Battrell C. Frederick, Matray Tracy, Sherif Hesham
Принадлежит:

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): 12-. (canceled)613-. (canceled)14. The compound of claim 3 , wherein Ris OH.15. The compound of claim 3 , wherein Ris claim 3 , phosphate claim 3 , thiophosphate claim 3 , phospho claim 3 , thiophospho claim 3 , —Oalkylphospho claim 3 , —Oalkylthiophospho claim 3 , —Oalkyletherphospho claim 3 , —Oalkyletherthiophospho claim 3 , —Ophosphoalkyl claim 3 , —Ophosphoalkylether claim 3 , —Othiophosphoalkyl or —Othiophosphoalkylether optionally substituted with a substituent selected from —OH claim 3 , —NH claim 3 , and —SH.17. The compound of claim 3 , wherein Rand Rare each O and Rand Rare each oxo.1825-. (canceled)26. The compound of claim 3 , wherein n is an integer from 2 to 15.27. The compound of claim 3 , wherein n is an integer from 2 to 10.2856-. (canceled)57. The compound of claim 3 , wherein at least one Mis a dimethylaminostilbene claim 3 , quinacridone claim 3 , fluorophenyl-dimethyl-BODIPY claim 3 , his-fluorophenyl-BODIPY claim 3 , acridine claim 3 , terrylene claim 3 , sexiphenyl claim 3 , porphyrin claim 3 , benzopyrene claim 3 , (fluorophenyl-dimethyl-difluorobora-diaza-indacene)phenyl claim 3 , (bis-fluorophenyl-difluorobora-diaza-indacene)phenyl claim 3 , quaterphenyl claim 3 , bi-benzothiazole claim 3 , ter-benzothiazole claim 3 , bi-naphthyl claim 3 , bi-anthracyl claim 3 , squaraine claim 3 , squarylium claim 3 , 9 claim 3 , 10-ethynylanthracene or ter-naphthyl moiety.58. The compound of claim 3 , wherein at least one Mis p-terphenyl claim 3 , perylene claim 3 , azobenzene claim 3 , phenazine claim 3 , phenanthroline claim 3 , acridine claim 3 , thioxanthrene claim 3 , chrysene claim 3 , rubrene claim 3 , coronene claim 3 , cyanine claim 3 , perylene imide claim 3 , or perylene amide or derivative thereof.59. The compound of claim 3 , wherein at least one Mis a coumarin dye claim 3 , resorufin dye claim 3 , dipyrrometheneboron difluoride dye ...

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Номер записи: 78
13-05-2021 дата публикации

OLIGONUCLEOTIDE ANALOGUES HAVING MODIFIED INTERSUBUNIT LINKAGES AND/OR TERMINAL GROUPS

Номер: US20210139897A1
Автор: Cai Bao Zhong, Hanson Gunnar J., Rudolph Alexander Charles, Weller Dwight D., ZHOU MING
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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Номер записи: 79
25-04-2019 дата публикации

Phosphonate functional antimicrobial coatings for metal surfaces

Номер: US20190116798A1
Автор: Daniel Foucher, Gideon WOLFAARDT, Lukasz POROSA
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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Номер записи: 80
25-04-2019 дата публикации

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

Номер: US20190119310A1
Автор: Brown Christopher, LONDESBROUGH Derek John, MOORE GILLIAN, Northen Julian Scott, PATIL HEMANT KASHINATH
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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Номер записи: 81
25-08-2022 дата публикации

PRODUCTION METHOD FOR BIFURCATED LIPID-LINKED OLIGONUCLEOTIDE, AND INTERMEDIATE

Номер: US20220267771A1
Автор: FUKUI Nobuaki, OCHI Shunsuke, SEKIGUCHI Mitsuaki, TANINO Tetsuya
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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Номер записи: 82
03-05-2018 дата публикации

LIGHT EMITTING DEVICES AND COMPOUNDS

Номер: US20180123052A1
Автор: WONG Michael Yin, Zysman-Colman Eli
Принадлежит:

Thermally Activated Delayed Fluorescence (TADF) compounds wherein two aromatic heterocyclic moieties are provided as acceptor groups, spaced apart from two donor moieties by an aromatic spacer ring, are described. Charged organic TADF species having a similar structure are also described. The TADF compounds and charged organic TADF species may be employed as emitter material in light emitting devices such as OLEDs and LEECs. Also described TADF compounds wherein at least one donor moiety is substituted by at least one substituent that is a phosphine oxide or a phosphine sulphide. 137-. (canceled)44. A light emitting device comprising a TADF compound according to .45. The light emitting device of claim 44 , wherein said light emitting device is an OLED.492. The TADF compound according to claim 46 , wherein the acceptor moieties Acc are claim 46 , independently for each occurrence selected from the group consisting of -Het as defined in claim claim 46 , —CN claim 46 , sulfone claim 46 , sulfoxide claim 46 , imine claim 46 , amide claim 46 , acridine claim 46 , acridinium claim 46 , carboxylate ester claim 46 , phosphine oxide claim 46 , phosphine sulfide claim 46 , ketone and aldehyde.52. A light emitting device comprising a TADF compound according to .53. The light emitting device of claim 52 , wherein said light emitting device is an OLED.57. The charged organic species according to claim 56 , wherein at least one linking group L is present and is independently for each occurrence claim 56 , a hydrocarbylene chain claim 56 , that may be substituted or unsubstituted claim 56 , hydrocarbylene or unsaturated hydrocarbylene.58. The charged organic species according to claim 57 , wherein the at least one linking group L is selected from substituted or unsubstituted cyclopentane-1 claim 57 ,3-diyl claim 57 , cyclohexane-1 claim 57 ,4-diyl claim 57 , 1 claim 57 ,4-phenylene and 4 claim 57 ,4′-biphenylene.59. The charged organic species according to claim 57 , wherein the ...

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Номер записи: 83
27-05-2021 дата публикации

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

Номер: US20210155642A1
Автор: Brown Christopher, LONDESBROUGH Derek John, MOORE GILLIAN, Nichols David E., Northen Julian Scott, PATIL HEMANT KASHINATH
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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Номер записи: 84
27-05-2021 дата публикации

Deuterated pyridone amides and prodrugs thereof as modulators of sodium channels

Номер: US20210155643A1
Автор: Licong Jiang, Sara Sabina Hadida Ruah
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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Номер записи: 85
12-05-2016 дата публикации

Novel Pyrrole Derivatives

Номер: US20160130224A1
Автор: Andrew Peter William, Damaso Mafalda Pires, Davies Mark William, Frickel Fritz-Frieder, Hamza Daniel, Hirst Simon Christopher, Lonnen Rana
Принадлежит:

There are provided inter alia novel N-phenyl substituted pyrrole derivativesand theiruse in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections. 2. A compound according to selected from:2-(Dimethylcarbamoyl)-1-(4-methoxyphenyl)-5-(4-methylpiperazine-1-carbonyl)-1H-pyrrole-3,4-diyl bis(2-methylpropanoate),2-(D imethyl carbamo y1)-1-(4-methoxyphenyl)-5-(4-methylpiperazine-1-carbonyl)-1H-pyrrole-3,4-diyl bis(2-methylpropanoate) hydrochloride,2-(Dimethylcarbamoyl)-1-(4-methoxyphenyl)-5-(4-methylpiperazine-1-carbonyl)-1H-pyrrole-3,4-diyl bis(2,2-dimethylpropanoate),2-(Dimethylcarbamoyl)-1-(4-methoxyphenyl)-5-(4-methylpiperazine-1-carbonyl)-1H-pyrrole-3,4-diyl bis(2,2-dimethylpropanoate) hydrochloride,2,5-Bis(dimethylcarbamoyl)-1-(4-methoxyphenyl)-1H-pyrrole-3,4-diyl bis(3-((phosphonooxy)methyl)benzoate),Sodium ((((2,5-bis(dimethylcarbamoyl)-1-(4-methoxyphenyl)-1H-pyrrole-3,4-diyl)bis(oxy))bis(carbonyl))bis(3,1-phenylene))bis(methylene) bis(hydrogenphosphate),2-(Dimethylcarbamoyl)-5-(ethoxycarbonyl)-1-(4-methoxyphenyl)-1H-pyrrole-3,4-diyl bis(4-((phosphonooxy)methyl)benzoate), andSodium ((((2-(dimethylcarbamoyl)-5-(ethoxycarbonyl)-1-(4-methoxyphenyl)-1H-pyrrole-3,4-diyl)bis(oxy))bis(carbonyl))bis(4,1-phenylene))bis(methylene) bis(hydrogenphosphate).3. A pharmaceutical composition comprising a compound according to claim 1 , optionally in combination with one or more pharmaceutically acceptable diluents or carriers.4. A pharmaceutical composition according to comprising one or more other therapeutically active ingredients.5. (canceled)6. A compound according to for use in combination with one or more other therapeutically active ingredients.7. A method of treating bacterial infections caused by bacteria producing pore-forming toxins claim 1 , such as cholesterol dependent cytolysins claim 1 , in a subject claim 1 , the method comprising administering to the subject a therapeutically effective amount of a compound according to . ...

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Номер записи: 86
01-09-2022 дата публикации

Methods of Treating Psychological and Brain Disorders

Номер: US20220273680A1
Автор: Thompson Scott
Принадлежит: University of Maryland at Baltimore

Provided herein are methods for preventing or treating a psychological disorder. A serotonin agonist or an agonist of serotonin receptors is administered separately, sequentially or simultaneously in combination with a serotonin receptor 2A antagonist.

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Номер записи: 87
02-05-2019 дата публикации

NOVEL HYDROPHILIC LINKERS AND LIGAND-DRUG CONJUGATES THEREOF

Номер: US20190125894A1
Автор: GAI Shun, GUO Huihui, Huang Yuanyuan, JIA Junxiang, Li Wenjun, Li Xing, Lin Chen, QU Lan, SUN Sanxing, Xie Hongsheng, YANG Qingliang, YE Hangbo, ZHAO Robert Yongxin, ZHOU Xiaomai, ZHUO Xiaotao
Принадлежит: HANGZHOU DAC BIOTECH CO., LTD.

Hydrophilic linkers are useful for linking drugs to cell-binding ligands in ligand-drug conjugates, such as antibody-drug conjugates. The ligand-drug conjugate includes a cell-binding ligand capable of binding to a particular cell population, and a drug connected to the ligand by a hydrophilic linker. The hydrophilic linker includes one or more hydrophilic groups that render the linker hydrophilic. The hydrophilic linker may also include functional groups at the two termini for coupling to the drug and the cell-binding ligand respectively. 2. The compound of claim 1 , wherein V is —N(SOOH)—.3. The compound of claim 1 , wherein V is —N[PO(OH)]—.4. The compound of claim 1 , wherein n is an integer from 1 to 50.5. The compound of claim 1 , wherein n is an integer from 1 to 10.6. The compound of claim 1 , wherein n is 1. This application is a division of U.S. application Ser. No. 15/558,917, filed on Sep. 15, 2017, entitled “NOVEL HYDROPHILIC LINKERS AND LIGAND-DRUG CONJUGATES THEREOF,” which is a national stage of PCT/162015/052011, filed on Mar. 19, 2015, the entire content of each of the prior applications is hereby incorporated by reference.The present invention relates to novel hydrophilic linkers that are useful for linking drugs (e.g., cytotoxic drugs) to cell-binding ligands (e.g., antibodies). The use of the hydrophilic linkers of the invention increases the potency and therapeutic index of the ligand-drug conjugates (e.g., antibody-drug conjugates). This is particularly effective when the hydrophilic linkers are used as non-cleavable ones. The present invention further relates to methods for preparing the novel hydrophilic linkers and the ligand-drug conjugates thereof.In order to reduce systemic toxicities, a promising approach to achieve targeted delivery of cytotoxic drugs to tumor cells is to use antibody-drug conjugates (ADCs) or other types of ligand-drug conjugates as self-guided tumor-targeting drugs. Antibody-drug conjugates, which combine the ...

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Номер записи: 88
02-05-2019 дата публикации

Charged linkers and their uses for conjugation

Номер: US20190127399A1
Автор: Qingliang YANG, Robert Yongxin Zhao, Xing Li, Yuangyuang HUANG
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.

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Номер записи: 89
02-05-2019 дата публикации

CHARGED LINKERS AND THEIR USES FOR CONJUGATION

Номер: US20190127400A1
Автор: HUANG Yuangyuang, Li Xing, YANG Qingliang, ZHAO Robert Yongxin
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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Номер записи: 90
02-05-2019 дата публикации

CHARGED LINKERS AND THEIR USES FOR CONJUGATION

Номер: US20190127401A1
Автор: HUANG Yuangyuang, Li Xing, YANG Qingliang, ZHAO Robert Yongxin
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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Номер записи: 91
23-04-2020 дата публикации

Phosphonium-ion tethered tetracycline drugs for treatment of cancer

Номер: US20200123182A1
Автор: Alexandre Froidbise, Andrew Ratcliffe, Brett Stevenson, David Hallett, Edward COCHRANE, Franz LAGASSE, Gilbert Lassalle, Tim SPAREY
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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Номер записи: 92
19-05-2016 дата публикации

ABLATIVE, RENEWABLE, MULTI-FUNCTIONAL PROTECTIVE COATING FOR DENTAL SURFACES

Номер: US20160136081A1
Автор: BENDEJACQ Denis, REIERSON Robert Lee
Принадлежит: Rhodia Operations

An oral care composition in the form of a toothpaste, tooth gel, dentifrice, tooth powder, prophy paste, mouthwash, rinse, tooth mousse, dental floss, chewing gum, soluble oral care strip or film for direct application or attachment to an oral surface, or lozenge for combating dental caries, erosion, hypersensitivity, and/or staining that includes an orally acceptable carrier and a copolymer of a first α,β-ethylenically unsaturated phosphate compound (A); and one or more α,β-ethylenically unsaturated co-monomers, at least one of which is other than an allyl-functional co-monomer, wherein (A) is an allyl phosphate compound of formula (A): 1. An oral care composition in the form of a toothpaste , tooth gel , dentifrice , tooth powder , prophy paste , mouthwash , rinse , tooth mousse , dental floss , chewing gum , soluble oral care strip or film for direct application or attachment to an oral surface , or lozenge for combating dental caries , erosion , hypersensitivity , and/or staining comprising an orally acceptable carrier and a copolymer of a first α ,β-ethylenically unsaturated phosphate compound (A); and one or more α ,β-ethylenically unsaturated co-monomers , at least one of which is other than an allyl-functional co-monomer , wherein (A) is an allyl phosphate compound of formula (A){'br': None, 'sub': 2', '2', 'a', 'b', 'x', '3-x, 'sup': 1', '2, '[CH═CH—CH—O(RO)(RO)]P(O)(OM)\u2003\u2003(A)'}wherein{'sup': '1', 'sub': 2', '4, 'Ris a substituted or unsubstituted (C-C) alkylene moiety;'}{'sup': '2', 'sub': 2', '4, 'Ris a substituted or unsubstituted (C-C) alkylene moiety;'}M is identical or different, hydrogen, alkali metal, ammonium, protonated alkyl amine, protonated alkanolamine, or protonated basic amino acid;X is 1 or 2,a is from 1 to 20; andb is from 0 to 20.2. The oral care composition of wherein one or more instances of Rand/or R claim 1 , is substituted with a hydroxyl claim 1 , alkoxyl or aryloxyl moiety.3. The oral care composition of wherein the one or ...

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Номер записи: 93
19-05-2016 дата публикации

FORMYLPYRROLE-BASED HETEROCYCLES FOR NUCLEIC ACID ATTACHMENT TO SUPPORTS

Номер: US20160137677A1
Автор: Smith Randall, Smith Ryan Christopher, Zhao Xiaodong
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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Номер записи: 94
11-05-2017 дата публикации

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT USING SAME

Номер: US20170133602A1
Автор: CHOI Dae-Hyuk, CHOI Jin-Seok, EUM Sung-Jin, JUNG Su-Jin, Kang Sang-Kyu, KIM Dong-Jun, KIM Kee-Yong, LEE Joo-Dong, Lee Jung-hyun
Принадлежит: HEESUNG MATERIAL LTD.

The present specification relates to a novel hetero-cyclic compound, and an organic light emitting device using the same. 2. The compound of claim 1 , wherein the term “substituted or unsubstituted” means that there is substitution or no substitution is performed by one or more substituent groups selected from deuterium claim 1 , halogen claim 1 , —SiRR′R″ claim 1 , —P(═O)RR′ claim 1 , Cto Caryl claim 1 , and Cto Cheteroaryl claim 1 , or a substituent group where two or more substituent groups selected from the aforementioned substituent groups are connected claim 1 , and{'sub': 1', '60', '6', '60', '2', '60', '3', '60', '6', '60', '2', '60', '6', '60', '6', '60', '2', '60', '2', '60', '6', '60', '2', '60, 'R, R′, and R″ are the same as or different from each other, and are each independently hydrogen; Cto Cstraight-chain or branch-chain alkyl substituted or unsubstituted by one or more substituent groups selected from deuterium, halogen, Cto Cmonocyclic or polycyclic aryl, and Cto Cmonocyclic or polycyclic heteroaryl; Cto Cmonocyclic or polycyclic cycloalkyl substituted or unsubstituted by one or more substituent groups selected from deuterium, halogen, Cto Cmonocyclic or polycyclic aryl, and Cto Cmonocyclic or polycyclic heteroaryl; Cto Cmonocyclic or polycyclic aryl substituted or unsubstituted by one or more substituent groups selected from deuterium, halogen, Cto Cmonocyclic or polycyclic aryl, and Cto Cmonocyclic or polycyclic heteroaryl; or Cto Cmonocyclic or polycyclic heteroaryl substituted or unsubstituted by one or more substituent groups selected from deuterium, halogen, Cto Cmonocyclic or polycyclic aryl, and Cto Cmonocyclic or polycyclic heteroaryl.'}3. The compound of claim 1 , wherein X of Chemical Formula 1 is NR claim 1 , at least one of Y and Ris -(L)-(Z) claim 1 ,{'sub': 4', '5', 'm', 'n, 'X of Chemical Formula 1 is CRR, S, O, or Se, Y is -(L)-(Z),'}{'sub': 10', '6', '60', '2', '60', '1', '20', '6', '60', '2', '60, 'L is selected from the group ...

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Номер записи: 95
17-05-2018 дата публикации

Bicyclic aryl sphingosine 1-phosphate analogs

Номер: US20180133233A1
Автор: Arthur G. Taveras, Bin Ma, Edward Yin-Shiang Lin, Gnanasambandam Kumaravel, Guo Zhu Zheng, Jermaine Thomas, Kevin M. Guckian, Richard D. Caldwell, Xiaogao Liu
Принадлежит: Biogen MA Inc

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

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Номер записи: 96
01-09-2022 дата публикации

LIGHT-EMITTING DEVICE AND ELECTRONIC APPARATUS INCLUDING THE SAME

Номер: US20220278296A1
Автор: Bae Sungsoo, CHOI Hyewon, Hur Jaeweon, Jeong Hyein, Kim Seulong, KIM Soungwook
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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Номер записи: 97
17-05-2018 дата публикации

OXINDOLE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20180134659A1
Автор: BEESON Craig C., LINDSEY Christopher C., ROHRER Baerbel
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Provided herein are compounds of the formula (I) as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders. 2. The compound according to claim 1 , wherein Ris hydrogen.3. The compound according to claim 1 , wherein Ris lower alkyl or halogen.4. The compound according to claim 1 , wherein Ris methyl or chlorine.5. The compound according to claim 1 , wherein Ris hydrogen.6. The compound according to claim 1 , wherein Ris unsubstituted lower alkyl.7. The compound according to claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , pentyl claim 1 , butyl claim 1 , isobutyl claim 1 , isopentyl or methylpentyl.8. The compound according to claim 1 , wherein Ris trifluoroethyl.9. The compound according to claim 1 , wherein Ris unsubstituted phenyl.10. The compound according to claim 1 , wherein Ris phenyl mono- claim 1 , bi or trisubstituted independently with alkoxy or hydroxy.11. The compound according to claim 1 , wherein Ris phenyl bisubstituted independently with alkoxy claim 1 , hydroxy claim 1 , —OC(O)CH claim 1 , —OC(O)CHOCH claim 1 , —OC(O)-lower alkyl claim 1 , —OC(O)NHCHCHOCHCHOH claim 1 , —OSON(CH)or —OC(O)N(CH).12. The compound according to claim 1 , wherein Ris methyl-1H-indazolyl claim 1 , benzo[d][1 claim 1 ,3]dioxolyl claim 1 , benzo[d]imidazolyl claim 1 , benzoyl-1H-indolyl claim 1 , benzo[d]oxazolyl or oxazolo[4 claim 1 ,5-b]pyridinyl.13. The compound according to claim 1 , wherein Ris 6-membered heteroaryl group having one or more ring carbons replaced by N.14. The compound according to claim 13 , wherein Ris pyrimidinyl claim 13 , pyrazinyl claim 13 , pyridazinyl or pyridinyl.15. The compound according to claim 1 , wherein Ris hydrogen or hydroxy.16. The compound according to claim 1 , wherein Ris —ORor —NHR.17. The compound according to claim 1 , ...

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Номер записи: 98
17-05-2018 дата публикации

POLYCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT COMPRISING SAME

Номер: US20180138421A1
Автор: Cha Yongbum, Hong Sung Kil, Hong Wanpyo
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The present specification provides a multicyclic compound and an organic light emitting device including the same. 4. (canceled)5. The compound of claim 1 , wherein R4 and R5 are an alkyl group.10. (canceled)11. (canceled)13. (canceled)1517.-. (canceled)18. An organic light emitting device comprising:a first electrode;a second electrode; andone or more organic material layers disposed between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein one or more layers of the organic material layers comprise the compound of Chemical Formula 1 of .'}19. The organic light emitting device of claim 18 , wherein the organic material layer comprises at least one of an electron injection layer and an electron transfer layer claim 18 , and at least one of the electron injection layer and the electron transfer layer comprises the compound of Chemical Formula 1.20. The organic light emitting device of claim 18 , wherein the organic material layer comprises a light emitting layer claim 18 , and the light emitting layer comprises the compound of Chemical Formula 1 as a host of a light emitting layer.21. The organic light emitting device of claim 18 , wherein the organic material layer comprises an electron blocking layer claim 18 , and the electron blocking layer comprises the compound of Chemical Formula 1.22. The organic light emitting device of claim 18 , wherein the organic material layer comprises one or more layers of a hole injection layer claim 18 , a hole transfer layer claim 18 , and a layer carrying out hole injection and hole transfer at the same time claim 18 , and one of the layers comprises the compound of Chemical Formula 1.23. The organic light emitting device of claim 18 , wherein the organic material layer comprises the compound represented by Chemical Formula 1 as a host claim 18 , and comprises other organic compounds claim 18 , metals or metal compounds as a dopant.25. (canceled)2729.-. (canceled) The present ...

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Номер записи: 99
26-05-2016 дата публикации

STAT6 INHIBITORS

Номер: US20160145279A1
Автор: CORRY David B., KNIGHT Morgan, MANDAL Pijus Kumar, McMurray John S., MORLACCHI Pietro
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The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer. 28-. (canceled)9. The compound of claim 1 , wherein the compound has the formula IF or the formula IE; and wherein Ris —C(O)NRR claim 1 , Ris aryl claim 1 , and Ris —CH.10. The compound of claim 1 , wherein the bond between carbons 1 and 2 is a double bond.11. The compound of claim 1 , wherein Ris phosphate or —CF—P(O(OR)(OR).12. (canceled)13. The compound claim 12 , wherein Ror Ris —CHOC(O)C(CH).14. The compound of claim 13 , wherein Rand Ris —CHOC(O)C(CH).15. The compound of claim 1 , wherein Ris hydrogen.16. The compound of claim 1 , wherein Ris hydrogen or alkyl.17. (canceled)18. The compound of claim 17 , wherein Ris methyl.19. (canceled)20. The compound of claim 1 , wherein Ris hydrogen or —N(R)R.21. The compound of claim 20 , wherein Ris hydrogen or Ris hydrogen.22. (canceled)23. The compound of claim 20 , wherein Ris alkyl claim 20 , aryl claim 20 , or acyl.2425-. (canceled)264. The compound of claim claim 20 , wherein the compound has the formula IB claim 20 , and wherein Ris hydrogen or oxo.27. (canceled)28. The compound of claim 1 , wherein the compound has the formula IB claim 1 , and wherein Ris hydrogen or oxo.29. (canceled)30. The compound of claim 1 , wherein the compound has the formula IB claim 1 , and wherein n is 1 claim 1 , 2 claim 1 , or 3.3132-. (canceled)33. The compound of claim 1 , wherein Ris hydrogen claim 1 , alkyl claim 1 , or methyl.3435-. (canceled)36. The compound of claim 1 , wherein Ris hydrogen claim 1 , alkyl.3738-. (canceled)39. The compound of claim 1 , wherein Ris an alkylor methyl.40. (canceled)41. The compound of claim 1 , wherein R claim 1 , R claim 1 , and Rare hydrogen ...

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Номер записи: 100