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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 2006. Отображено 100.
09-02-2012 дата публикации

Charge transport compositions and electronic devices made with such compositions

Номер: US20120032158A1
Автор: Daniel David Lecloux, YING Wang
Принадлежит: EI Du Pont de Nemours and Co

The present invention is directed to a photoactive device comprising an anode, a cathode, and a photoactive layer, which device further comprises an electron transport and/or anti-quenching layer which minimizes both electron transfer quenching and energy transfer quenching of the photoactive layer.

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Номер записи: 1
10-01-2013 дата публикации

2,4,5-triaminophenols and related compounds

Номер: US20130012681A1
Автор: Joachim C. Ritter, Rajiv Dhawan
Принадлежит: EI Du Pont de Nemours and Co

New triaminophenol compositions and related compounds are disclosed, as are processes for their preparation and for the preparation of novel salts and diacid complexes from such compounds. Polymers prepared from these compositions can be made into high strength fiber, film, and tape and are useful in applications such as protective apparel, aircraft, automotive components, personal electronics, and sports equipment.

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Номер записи: 2
18-04-2013 дата публикации

PROCESS FOR PREPARATION OF AMISULPRIDE

Номер: US20130096319A1
Автор: Chavan Yuvraj Atmaram, Deshpande Tushar Nandkumar, Kolekar Mahesh Ramkumar, Paghdar Dinesh Jayntibhai, Patil Suryaprakash Pandurang, Ray Purna Chandra, Singh Girij Pal
Принадлежит: Lupin Limited

The present invention is related to a novel process for the preparation of amisulpride (I) which involves: methylation of 4-amino-salicylic-acid (VI) with dimethyl sulphate and base, optionally in presence of TBAB to obtain 4-amino-2-methoxy methyl benzoate (VII) and (ii) oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) or 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) with oxidizing agent in the presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV) or 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) respectively. 1) A process for the preparation of amisulpride (I) which involves following steps:{'b': '1', ') methylation of 4-amino-salicylic-acid (VI) to 4-amino-2-methoxy methyl benzoate (VII), optionally in the presence of phase transfer catalyst,'}{'b': '2', ') conversion of 4-amino-2-methoxy methyl benzoate (VII) to 4-amino-2-methoxy-5-thiocyano methyl benzoate (VIII),'}{'b': '3', ') ethylation of 4-amino-2-methoxy-5-thiocyano methyl benzoate (VIII) to form 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X),'}the intermediate compound (X) is converted to amisulpiride (I) by two routes (a) or (b):Route (a):{'b': '4', 'i': 'a', ') hydrolysis of 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) to 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX),'}{'b': '4', 'i': 'b', ') oxidation of 4-amino-2-methoxy-5-ethyl thio benzoic acid (IX) with a suitable oxidizing agent in presence of sodium tungstate or ammonium molybdate to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid (IV),'}Route (b):{'b': '5', 'i': 'a', ') oxidation of 4-amino-2-methoxy-5-ethyl thio methyl benzoate (X) to 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) with a suitable oxidizing agent,'}{'b': '5', 'i': 'b', ') hydrolysis of 2-methoxy-4-amino-5-ethyl-sulfonyl methyl benzoate (XI) to give 2-methoxy-4-amino-5-ethyl-sulfonyl benzoic acid,(IV and;'}{'b': '6', ') coupling of 2-methoxy-4-amino-5-ethyl-sulfonyl ...

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Номер записи: 3
02-05-2013 дата публикации

ANTIMICROBIAL AGENTS

Номер: US20130109713A1
Автор: LaVoie Edmond J., Parhi Ajit, Pilch Daniel S.
Принадлежит:

The invention provides a compound of formula I:or a salt thereof, wherein R-Rand X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents. 2. The compound of wherein:{'sup': 1', 'y', 'y, 'sub': 1', '6, 'Ris Ror (C-C)alkyl that is substituted with one or more R;'}{'sup': 2', 'z', 'x, 'sub': 1', '6, 'Ris Ror (C-C)alkyl that is substituted with one or more R;'}{'sup': 4', '5', '6', '7', 'd', '4', '5', '6', '7', 'p', 'p', 'p', 'g', 'h', 'g', 'h', 'a', '4', '5', '6', '7', 'b, 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '3', '2', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'at least one of RRRand Ris aryl or heteroaryl wherein each aryl or heteroaryl is optionally substituted with one or more (e.g. 1, 2, 3, or 4) R; and the remainder of RRRand Rare each independently H, halo, cyano, nitro, hydroxy, carboxy, trifluoromethyl, trifluoromethoxy, (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkoxycarbonyl, (C-C)alkanoyloxy, aryl, heteroaryl, aryloxy, heteroaryloxy, (C-C)alkylthio, —S(O)R, —S(O)R, —S(O)R, —S(O)NRR, and —NRR; wherein any alkyl and any alkyl or alkanoyl portion of any aryl(C-C)alkyl, heteroaryl(C-C)alkyl, aryl(C-C)alkanoyl or heteroaryl(C-C)alkanoyl is optionally substituted with one or more (e.g. 1, 2, 3, or 4) R; and wherein any aryl, heteroaryl, or any aryl or heteroaryl portion of any aryl(C-C)alkyl, heteroaryl(C-C)alkyl, aryl(C-C)alkanoyl or heteroaryl(C-C)alkanoyl of RRRand Ris optionally substituted with one or more (e.g. 1, 2, 3, or 4) R;'}{'sup': 8', 'p', 'p', 'p', 'g', 'h', 'g', 'h', '8', 'a', '8', 'b, 'sub': 1', '6', '3', '6', '1', '6', '1', '6', '1', '6', '1', '6', '2', '3', '2, 'Ris H, halo, cyano, nitro, hydroxy, carboxy, trifluoromethyl, trifluoromethoxy, (C-C)alkyl, (C-C)cycloalkyl, (C-C)alkoxy, (C-C)alkoxycarbonyl, (C-C)alkanoyloxy, aryl, heteroaryl, aryloxy, ...

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Номер записи: 4
29-08-2013 дата публикации

NOVEL HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME (AS AMENDED)

Номер: US20130225596A1
Автор: Asahi Kentaro, Endoh Takeshi, Horiguchi Tohru, Jikihara Sae, Kai Hiroyuki
Принадлежит:

The present invention provides novel compounds having a P2Xand/or P2Xreceptor antagonistic effect. 2. The pharmaceutical composition having a P2Xand/or P2Xreceptor antagonistic effect according to claim 1 , comprising the compound wherein ring A is a substituted or unsubstituted cyclohexane ring claim 1 , a substituted or unsubstituted cyclohexadiene ring claim 1 , a substituted or unsubstituted cyclohexene ring claim 1 , a substituted or unsubstituted benzene ring claim 1 , a substituted or unsubstituted pyridine ring claim 1 , a substituted or unsubstituted dihydropyridine ring claim 1 , a substituted or unsubstituted tetrahydropyridine ring claim 1 , a substituted or unsubstituted pyrimidine ring claim 1 , a substituted or unsubstituted dihydropyrimidine ring claim 1 , a substituted or unsubstituted tetrahydropyrimidine ring claim 1 , a substituted or unsubstituted hexahydropyrimidine ring claim 1 , a substituted or unsubstituted piperidine ring claim 1 , a substituted or unsubstituted piperazine ring claim 1 , a substituted or unsubstituted pyrazine ring claim 1 , a substituted or unsubstituted dihydropyrazine ring claim 1 , a substituted or unsubstituted tetrahydropyrazine ring claim 1 , a substituted or unsubstituted pyridazine ring claim 1 , a substituted or unsubstituted dihydropyridazine ring claim 1 , a substituted or unsubstituted tetrahydropyridazine ring claim 1 , a substituted or unsubstituted indene ring claim 1 , a substituted or unsubstituted benzofuran ring claim 1 , a substituted or unsubstituted benzofuran ring claim 1 , a substituted or unsubstituted benzo(b)thiophene ring claim 1 , a substituted or unsubstituted benzo(c)thiophene ring claim 1 , a substituted or unsubstituted indoline ring claim 1 , a substituted or unsubstituted indole ring claim 1 , a substituted or unsubstituted benzimidazole ring claim 1 , a substituted or unsubstituted cyclopenta[b]pyridine ring claim 1 , a substituted or unsubstituted 1H-indazole ring claim 1 , a ...

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Номер записи: 5
05-09-2013 дата публикации

ROS-Activated Compounds as Selective Anti-Cancer Therapeutics

Номер: US20130230542A1
Автор: Bell-Horwath Tiffany, LI Guorui, Merino Edward J., Mulloy James C.
Принадлежит:

Provided are compounds according to the following Formula I: 2. The compound according to claim 1 , wherein said alkyl claim 1 , aryl claim 1 , and aralkyl substitutions are selected from the group consisting of alkoxyl claim 1 , halo claim 1 , OH claim 1 , CN claim 1 , carboxyl claim 1 , carboxyl ester claim 1 , and substituted or unsubstituted alkyl.3. The compound according to claim 1 , wherein Ris H or alkyl when Ris aryl or aralkyl claim 1 , and wherein Ris H or alkyl when Ris aryl or aralkyl.4. The compound according to claim 1 , wherein Rand Rare each independently selected from the group consisting of H claim 1 , substituted or unsubstituted C-Calkyl claim 1 , and substituted or unsubstituted phenyl; and Ris OH.5. The compound according to claim 1 , wherein the cancer is associated with production of elevated reactive oxygen species.6. The compound according to claim 5 , wherein the cancer is selected from the group consisting of leukemia claim 5 , renal cancer claim 5 , and cancers of the central nervous system.7. The compound according to claim 6 , wherein the leukemia is selected from the group consisting of acute myeloid leukemia claim 6 , acute lymphoblastic leukemia claim 6 , plasmacytoma claim 6 , myeloma claim 6 , myelogenous leukemia claim 6 , acute lymphocytic leukemia claim 6 , acute promyelocytic leukemia claim 6 , and multiple myeloma.9. A method of reducing proliferative capacity in a cell claim 1 , the method comprising contacting the cell with an effective amount of a compound according to .10. The method according to claim 9 , wherein the cell is a mammalian cell.11. The method according to claim 10 , wherein the cell is a cancer cell.12. A method of treating a cancer associated with elevated ROS comprising administering to a subject in need thereof an effective amount of a compound according to .13. The method according to claim 12 , wherein the subject is a mammal.14. The method according to claim 13 , wherein the cancer is selected from ...

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Номер записи: 6
20-02-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140051724A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 7
20-03-2014 дата публикации

METHODS OF SYNTHESIZING 2- SUBSTITUTED-1,4-BENZENEDIAMINE

Номер: US20140081049A1
Автор: ANDERSON James S., GARDLIK John Michael, GARRETT Garry Steven, Murphy Bryan Patrick, SHUMATE Robert Edward, Zhang Guiru
Принадлежит: The Proctor & Gamble Company

Disclosed is a method of making a 2-substituted-1,4-benzenediamine by nucleophilic aromatic substitution. 2. The method of wherein the suitable alkali alkoxide is selected from the group consisting of sodium methoxide claim 1 , lithium methoxide claim 1 , potassium methoxide claim 1 , sodium ethoxide claim 1 , lithium ethoxide claim 1 , potassium ethoxide claim 1 , sodium propoxide claim 1 , lithium propoxide claim 1 , potassium propoxide and mixtures thereof.3. The method of wherein the suitable alkali hydroxide is sodium hydroxide or potassium hydroxide.4. The method of wherein the method further comprises dissolving a 4-nitro-2- (or 3-) haloalkyl moiety substituted chlorobenzene in an alcohol selected from methanol claim 1 , ethanol and propanol to form a solution and then mixing the solution with an alkali alkoxide claim 1 , alkali hydroxide and mixtures thereof.5. The method of wherein the suitable alkali alkoxide claim 4 , alkali hydroxide and mixtures thereof is present in an amount from about 10% to about 30% by weight of the solution. The subject matter of the present application relates to the synthesis of a 2-substituted-1,4-benzenediamine such as a 2-methoxymethyl-1,4-benzenediamine and physiologically compatible salts thereof.2-Substituted-1,4-benzenediamine and physiologically compatible salts thereof may be useful as primary intermediates in oxidative hair color. For example, 2-methoxymethyl-1,4-benzenediamine and physiologically compatible salts thereof are useful as primary intermediates in oxidative hair color. A current process for synthesizing 2-methoxymethyl-1,4-benzenediamine may be accomplished as discussed in U.S. Pat. No. 4,997,451 and U.S. Pat. No. 6,648,923. Such a process is illustrated by the following reaction scheme:However, it is still desired to find alternative processes that reduce costs of manufacturing the desired product. As such, there still exists a need to utilize less expensive starting materials to arrive at the desired ...

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Номер записи: 8
02-01-2020 дата публикации

Photoredox-Catalyzed Direct C-H Functionalization of Arenes

Номер: US20200002284A1
Автор: Nicewicz David
Принадлежит:

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is F.48-. (canceled)12. (canceled)13. The method of claim 1 , wherein the fluoride is selected from ammonium fluoride claim 1 , cesium fluoride claim 1 , and triethylamine hydrofluoride.1415-. (canceled)16. The method of claim 1 , wherein the oxidant is molecular oxygen.17. The method of claim 1 , wherein the oxidant is 2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyl-1-piperidinyloxy radical (TEMPO).1820-. (canceled)21. The method of claim 1 , wherein Z is —CN.29. The method of claim 1 , wherein the compound is isotopically-labeled.30. The method of claim 25 , wherein the compound contains a radioactive isotope.31. The method of claim 1 , wherein the compound is not isotopically-labeled. This application is a continuation of U.S. application Ser. No. 15/826,092, filed Nov. 29, 2017, which is a continuation of International Application No. PCT/US2016/035549 with an international filing date of Jun. 2, 2016, which claims priority to U.S. Provisional Application No. 62/170,632 filed on Jun. 3, 2015, the contents of which are incorporated ...

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Номер записи: 9
12-01-2017 дата публикации

BLOCK COPOLYMER

Номер: US20170008992A1
Автор: Kim Jung Keun, Lee Je Gwon, Park No Jin, Yoon Sung Soo
Принадлежит: LG CHEM, LTD.

The present application provides the block copolymers and their application. The block copolymer has an excellent self assembling property and phase separation and various required functions can be freely applied thereto as necessary. 2. The block copolymer according to claim 1 , wherein the X is a single bond claim 1 , an oxygen atom claim 1 , —C(═O)—O— or —O—C(═O)—.3. The block copolymer according to claim 1 , wherein the X is —C(═O)—O—.4. The block copolymer according to claim 1 , wherein the chain comprises 8 to 20 chain-forming atoms.5. The block copolymer according to claim 1 , wherein the chain-forming atom is a carbon claim 1 , an oxygen claim 1 , a nitrogen or a sulfur.6. The block copolymer according to claim 1 , wherein the chain-forming atom is a carbon or an oxygen.7. The block copolymer according to claim 1 , wherein the chain is a linear hydrocarbon chain.8. The block copolymer according to claim 1 , wherein the cyclic structure is an aromatic structure and a alicyclic structure.9. The block copolymer according to claim 1 , wherein the chain of the Y is directly linked to the cyclic structure or is linked to the cyclic structure via a linker.10. The block copolymer according to claim 9 , wherein the linker is an oxygen atom claim 9 , a sulfur atom claim 9 , —NR— claim 9 , —S(═O)— claim 9 , an alkylene group claim 9 , an alkenylene group or an alkynylene group claim 9 , where the Ris hydrogen claim 9 , an alkyl group claim 9 , an alkenyl group claim 9 , an alkynyl group claim 9 , an alkoxy group or an aryl group.11. The block copolymer according to claim 1 , the Y is represented by Formula 2 below:{'br': None, '-P-Q-Z\u2003\u2003[Formula 2]'}{'sub': 3', '3, 'wherein the P is an arylene group, the Q is a single bond, an oxygen atom or —NR—, where the Ris hydrogen, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group or an aryl group and the Z is the chain having the 8 or more chain-forming atoms.'}13. The block copolymer according to ...

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Номер записи: 10
09-01-2020 дата публикации

METHOD OF TREATING CANCER USING SELECTIVE ESTROGEN RECEPTOR MODULATORS

Номер: US20200009084A1
Автор: McDonnell Donald P., Nelson Erik R., Wardell Suzanne E.
Принадлежит:

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM. 2. The method of claim 1 , wherein the cancer is Breast cancer brain metastases claim 1 , Astrocytoma claim 1 , Atypical Teratoid Rhabdoid Tumor (ATRT) claim 1 , Chondrosarcoma claim 1 , Choroid Plexus Carcinoma claim 1 , Craniopharyngioma claim 1 , Ependymoma claim 1 , Germ Cell Tumor claim 1 , Glioblastoma claim 1 , Glioma claim 1 , Hemangioma claim 1 , Juvenile Pilocytic Astrocytoma claim 1 , Medulloblastoma claim 1 , Meningioma claim 1 , Neurofibroma claim 1 , Neuronal and Mixed Neuronal-Glial Tumors claim 1 , Oligoastrocytoma claim 1 , Oligodendroglioma claim 1 , Pineal Tumor claim 1 , Pituitary Tumor claim 1 , PNET—(primitive neuroectodermal tumor) claim 1 , Schwannoma claim 1 , and Leptomeningeal metastases.5. The method of claim 4 , wherein the cancer is de novo resistant to the estrogen receptor modulator.6. The method of claim 4 , wherein the resistance to the estrogen receptor modulator is acquired.7. The method of claim 4 , wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM).8. The method of claim 7 , wherein the SERM is tamoxifen claim 7 , idoxifene claim 7 , raloxifene or ICI 182 claim 7 ,780.9. The method of any one of - claim 7 , wherein the cancer is breast claim 7 , endometrial or ovarian cancer.10. The method of any one of - claim 7 , wherein the cancer is breast cancer.11. The method of any one of - claim 7 , wherein Rand Rindependently represent a hydrogen atom claim 7 , a methyl group claim 7 , an ethyl group claim 7 , a n-propyl group claim 7 , an iso-propyl group claim 7 , a n-butyl group claim 7 , an iso-butyl group claim 7 , or a tert-butyl group.12. The method of any one of - claim 7 , wherein -T-Z— ...

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Номер записи: 11
10-01-2019 дата публикации

REDUNDANT POWER LINE CONTROL SYSTEMS

Номер: US20190013470A1
Автор: Bogdanovich Phillip
Принадлежит:

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture. 1. A system for controlling electronic devices located at a site , comprising: a processor; and', 'a memory coupled to the processor;', 'wherein the control apparatus is configured to couple to at least one conductor in a power line associated with an electronic device receiving power from the power line, and wherein the control apparatus is configured to redirect electrical power from the at least one conductor through the control apparatus and to the electronic device;, 'a plurality of control apparatus, wherein one or more of the control apparatus comprisewherein a first control apparatus and a second control apparatus are configured to establish a communication link to at least one electronic device located at the site, the communication link comprising at least one of a wireless communication link and a power line communication link; andwherein at least one of the first control apparatus and the second control apparatus is configured to monitor and control the at least one electronic device using the established communication link.2. The apparatus of claim 1 , wherein at least one of the first control apparatus and the second control apparatus are configured to establish a wireless communication link with a remote device.3. The apparatus of claim 2 , wherein the control apparatus having the wireless ...

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Номер записи: 12
21-01-2021 дата публикации

APPARATUS FOR COUPLING TO EXISTING POWER LINES

Номер: US20210021303A1
Автор: Bogdanovich Phillip
Принадлежит: Crius Technology Group, Inc.

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture. 1. A clamp , comprising:a non-conductive blade;a conductive blade, wherein the conductive blade is offset from the non-conductive blade;wherein the non-conductive blade is configured to sever a power line and disrupt power through the power line;wherein the conductive blade is configured to splice into the power line and redirect the power from the power line while also providing the power back to the power line.2. The clamp of claim 1 , wherein the conductive blade is configured to splice into the power line simultaneously with the non-conductive blade.3. The clamp of claim 1 , further comprising an insulated tube claim 1 , wherein a portion of the non-conductive blade and a portion of the conductive blade are positioned in the insulated tube.4. The clamp of claim 3 , further comprising a contact pad claim 3 , wherein a first portion of the contact pad is electrically connected to the conductive blade claim 3 , and wherein a second portion of the contact pad is electrically connected to an electronic device control apparatus.5. The clamp of claim 4 , wherein the contact pad facilitates flow of current from inside of the insulated tube to an area outside of the insulated tube.6. The clamp of claim 1 , wherein the non-conductive blade comprises a piercing surface configured to splice into the power line.7. ...

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Номер записи: 13
28-01-2016 дата публикации

Method and apparatus for performing an energy audit

Номер: US20160025782A1
Автор: Phillip Bogdanovich
Принадлежит: Hyperion Energy Group LLC

Methods and apparatuses for performing an energy audit are disclosed, including using one or more current sensors clamped to an existing lighting system to measure one or more current or voltage signals over a first period of time; calculating a first power usage from the one or more current or voltage signals; replacing the existing lighting system with a replacement lighting system; using the one or more current sensors to measure one or more current or voltage signals of the replacement lighting system over a second period of time; calculating a second power usage from the one or more current or voltage signals; determining a power difference between the first power usage and the second power usage; using the power difference to estimate a cost savings between the first period of time and the second period of time; and generating an energy audit report. Other embodiments are described and claimed.

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Номер записи: 14
24-01-2019 дата публикации

Opsin-Binding Ligands, Compositions and Methods of Use

Номер: US20190023649A1
Автор: Berman Judd, Garvey David S., Quach Tan
Принадлежит: BIKAM PHARMACEUTICALS, INC.

Compounds and compositions are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed. 115-. (canceled)17. The method of claim 16 , wherein said visual cycle product is a toxic visual cycle product.18. The method of claim 17 , wherein said toxic visual cycle product is lipofuscin or N-retinylidene-N-retinylethanolamine (A2E).19. The method of claim 16 , wherein said compound reduces mislocalization of said opsin protein.20. The method of claim 16 , wherein said opsin protein is present in a cell.21. The method of claim 20 , wherein said cell is a cone cell or rod cell.22. The method of claim 20 , wherein said cell is present in a mammalian eye.23. A method of inhibiting the formation or accumulation of a visual cycle product claim 20 , comprising contacting an opsin protein with a compound selected from the group consisting of:3-(trifluoromethyl)-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline hydrochloride (Compound 1);3-methyl-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 2);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzamide (Compound 3);3-((2,6,6-trimethylcyclohex-1-enyl)methylamino)benzonitrile (Compound 4);3-chloro-N-((2,6,6-trimethylcyclohex-1-enyl)methyl)aniline (Compound 5);1-methyl-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 6);1-fluoro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 7);1-chloro-3-((2,6,6-trimethylcyclohex-1-enyl)methoxy)benzene (Compound 8);1-(trifluoromethyl)-3-((2,6,6-trimethylcyclohex- ...

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Номер записи: 15
29-01-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150031722A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 16
02-02-2017 дата публикации

TRIPHENYLAMINE DERIVATIVE AND ELECTROPHOTOGRAPHIC PHOTOSENSITIVE MEMBER

Номер: US20170031253A1
Автор: OKADA Hideki
Принадлежит: KYOCERA Document Solutions Inc.

A triphenylamine derivative is represented by general formula (1). In the general formula (1): R, R, R, R, R, R, R, R, R, and Reach represent, independently of one another, a hydrogen atom, an optionally substituted alkyl group having a carbon number of at least 1 and no greater than 6, an optionally substituted alkoxy group having a carbon number of at least 1 and no greater than 6, an optionally substituted alkenyl group having a carbon number of at least 2 and no greater than 6, or an optionally substituted aryl group having a carbon number of at least 6 and no greater than 14; m represents an integer of at least 1 and no greater than 3; and n represents an integer of at least 0 and no greater than 2. 3. The triphenylamine derivative according to claim 2 , wherein [{'sub': 1', '2', '3', '4', '5, 'R, R, R, R, and Reach represent a hydrogen atom,'}, {'sub': 11', '12', '13', '14', '15, 'R, R, R, R, and Reach represent, independently of one another, an hydrogen atom or an alkyl group having a carbon number of at least 1 and no greater than 6,'}, {'sub': 16', '17', '18', '19', '20, 'R, R, R, R, and Reach represent, independently of one another, a hydrogen atom or an alkyl group having a carbon number of at least 1 and no greater than 6,'}, 'm represents an integer of at least 1 and no greater than 3,', 'n represents 0 or 1, and', 'q represents 0 or 1., 'in the general formulas (1-1) and (1-2),'}4. The triphenylamine derivative according to claim 2 , that is represented by the general formula (1-2).5. The triphenylamine derivative according to claim 2 , whereinin the general formula (1-2), m represents 1 or 2 and q represents 1.6. The triphenylamine derivative according to claim 2 , whereinin the general formula (1-2), m represents 2 and q represents 1.7. The triphenylamine derivative according to claim 2 , whereinin the general formula (1-2), m represents 3 and n represents 1.9. An electrophotographic photosensitive member comprising a conductive substrate and a ...

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Номер записи: 17
17-02-2022 дата публикации

POLYMORPHIC FORMS OF RAD1901-2HCL

Номер: US20220048848A1
Автор: Bolger Joshua Kyle, CRUSKIE, Eberlin Alex, Edwards Richard, JR. Michael Paul, Markey Michael, McKenzie Jonathan Blake, Sheth Pratik
Принадлежит:

Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed. 121-. (canceled)23. The solid Form 2 of RAD1901-2HCl according to claim 22 , having an X-ray powder diffraction pattern comprising peaks claim 22 , in terms of 2-theta claim 22 , at 6.3 degrees 2θ±0.2 degree 2θ claim 22 , and 12.5 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.24. The solid Form 2 of RAD1901-2HCl according to claim 23 , having an X-ray powder diffraction pattern comprising peaks claim 23 , in terms of 2-theta claim 23 , at 6.3 degrees 2θ±0.2 degree 2θ claim 23 , 12.5 degrees 2θ±0.2 degree 2θ claim 23 , and 15.4 degrees 2θ±0.2 degree 2θ claim 23 , at about relative humidity 0%.25. The solid Form 2 of RAD1901-2HCl according to claim 24 , having an X-ray powder diffraction pattern further comprising a peak claim 24 , in terms of 2-theta claim 24 , at 18.3 degrees 2θ±0.2 degree 2θ claim 24 , and/or 13.4 degrees 2θ±0.2 degree 2θ claim 24 , at about relative humidity 0%.26. The solid Form 2 of RAD1901-2HCl according to claim 25 , having an X-ray powder diffraction pattern further comprising peaks claim 25 , in terms of 2-theta claim 25 , at 18.3 degrees 2θ±0.2 degree 2θ claim 25 , and 13.4 degrees 2θ±0.2 degree 2θ claim 25 , at about relative humidity 0%.27. The solid Form 2 of RAD1901-2HCl according to claim 26 , having an X-ray powder diffraction pattern substantially as shown in at about relative humidity 0% claim 26 , e.g.28. The solid Form 2 of RAD1901-2HCl according to claim 22 , having a differential scanning calorimetry (DSC) thermogram as shown in the bottom graph of .29. The solid Form 2 of RAD1901-2HCl according to claim 22 , having a thermogravimetric analysis (TGA) as shown in the top graph of .30. A pharmaceutical composition comprising the solid Form 2 of RAD1901-2HCl according to claim 22 , and one or more ...

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Номер записи: 18
09-02-2017 дата публикации

NITRIFICATION INHIBITORS

Номер: US20170036969A1
Автор: Dickhaut Joachim, EBENHOECH Johan, Nave Barbara, SISAY Mihiret Tekeste, WEIGELT Wolfgang, Wissemeier Alexander, ZERULLA Wolfram
Принадлежит:

The present invention relates to novel nitrification inhibitors of formula I. Moreover, the invention relates to the use of these novel nitrification inhibitors for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors. Further encompassed by the present invention are methods for reducing nitrification comprising the treatment of plants, soil and/or loci with said nitrification inhibitors, and methods for treating a fertilizer or a composition by applying said nitrification inhibitor. 116-. (canceled)18: The compound of claim 17 , wherein in said compound of formula I claim 17 , A is phenyl or a 6-membered hetaryl claim 17 , preferably phenyl claim 17 , wherein the aromatic ring may in each case be unsubstituted or may be partially or fully substituted by substituents claim 17 , which are independently of each other selected from R.19: The compound of claim 17 , wherein in said compound of formula I claim 17 , Rand Rboth represent hydrogen.20: The compound of claim 17 , wherein in said compound of formula I claim 17 , Ris hydrogen claim 17 , C-C-haloalkyl or ethinylhydroxymethyl claim 17 , and preferably Ris hydrogen.21: The compound of claim 17 , wherein in said compound of formula I claim 17 , R claim 17 , if present claim 17 , is{'sup': a', 'b', 'c', '1', 'c', '1', 'c', '1', 'c', '1', 'a', 'b', '2', '1', '2', '1', 'a', 'b', 'g', 'd', 'e', 'f, 'sub': 2', '2', '1', '6', '2', '6', '1', '4', '1', '4', '2', '4', '1', '2', '2', '4, '(i) halogen, CN, NRR, OR, C(═Y)R, C(═Y)OR, C(═Y)SR, C(═Y)NRR, YC(═Y)R, YC(═Y)NRR, NRN═C(R)(R), S(═O)R, NO, C-C-alkyl, C-C- C-C-haloalkyl, C-C-alkoxy, C-C-alkynyl-C-C-hydroxyalkyl, C-C-alkynyloxy;'}{'sub': 2', '4', '2', '4', '1', '4', '2', '4, 'sup': 1', 'c', '2', '1', 'c, '(ii) C-C-alkenylene-C(═Y)R, C-C-alkenylene-Y—C(═Y)R, wherein the C-C-alkylene or C-C-alkenylene chain may in each case be unsubstituted or may be partially or fully substituted by CN or halogen;'}{'sup': 'h', '( ...

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Номер записи: 19
09-02-2017 дата публикации

PHENYL BENZYL ETHER DERIVATIVE AND PREPARATION METHOD AND APPLICATION THEREOF

Номер: US20170037008A1
Автор: Cui Mengchao, GUO Yuzhi, Lin Chunping, Liu Boli, Zhang Zhiyong
Принадлежит:

Parts of compounds, after being labeled by radionuclide, of the phenyl benzyl ether derivative, are used as Aβ plaque imaging agent. The structural formula of the phenyl benzyl ether derivative is shown by formula (I). The present invention develops a kind of brand new phenyl benzyl ether derivative which has high affinity with Aβ plaques in brains of AD patients. The chemical structure of the phenyl benzyl ether derivative is different from that of compounds disclosed in the prior art and the phenyl benzyl ether derivative belongs to a brand new compound for diagnosing and treating AD. The obtained Aβ plaque imaging agent has the advantages that the in-vivo stability is good, the fat solubility is low, the removal speed for the brain is fast, the problem of removing the radionuclide in vivo does not exist, and the application prospect and the market value are great. 115-. (canceled)17. The phenyl benzyl ether derivative according to claim 16 , wherein Rand Rare o-substituents claim 16 , m-substituents or p-substituents.18. The phenyl benzyl ether derivative according to claim 16 , wherein the halogen is fluorine claim 16 , chlorine claim 16 , bromine or iodine; the alkoxy is C-Calkoxy claim 16 , preferably C-Calkoxy; the alkyl is C-Calkyl claim 16 , preferably C-Calkyl; the carbocyclic alkyl is three-membered to six-membered carbocyclic alkyl claim 16 , preferably cyclopropyl claim 16 , cyclopentyl or cyclohexyl; heterocyclic alkyl is three-membered to six-membered heterocyclic alkyl claim 16 , preferably piperidyl claim 16 , piperazinyl or morpholine cyclic group; the alkylamino is C-Calkylamino claim 16 , preferably C-Calkylamino claim 16 , more preferably N-methylamino claim 16 , dimethylamino claim 16 , diethylamino claim 16 , dipropylamino or diisopropylamino; the aryl is phenyl or naphthyl; the heteraryl is pyridyl claim 16 , furyl claim 16 , thienyl claim 16 , benzothiazolyl claim 16 , benzofuryl or benzoxazolyl; the arylalkoxy is C-Caryl C-Calkoxy claim 16 ...

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Номер записи: 20
04-02-2021 дата публикации

White light emitting material, preparation method thereof, and application thereof

Номер: US20210036234A1
Автор: Jieshun Cui, Xianglin Wang, Xiaomeng Li, Zhaoyu Zhang
Принадлежит: SOUTHWEST UNIVERSITY OF SCIENCE AND TECHNOLOGY

A white light emitting material having a chemical structural formula represented by formula (I), a preparation method thereof and application thereof. The preparation method comprises subjecting tris(4-iodophenyl)amine and 4-methoxyphenylacetylene or tris(4-iodophenyl)amine and methyl 4-ethynylbenzoate to a coupling reaction under protection of a protective gas and catalysis of a Pd/Cu mixed catalyst, to obtain the white light emitting material. A novel temperature-sensitive light emitting material is synthesized through a one-step method. The material is applied to the field of diode luminescence based on the temperature-sensitive characteristic. White light luminescence can be finally realized only by reasonably controlling the temperature and duration time during heating a substrate. Compared with the existing art, the method greatly saves raw material costs and manufacturing process costs, and provides a novel idea and strategy for use of a white organic light emitting diode.

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Номер записи: 21
12-02-2015 дата публикации

METHOD FOR PREPARING FLUORINE-18 ELUENT WITH ADJUSTED PH, AND METHOD FOR LABELLING FLUORINE-18 USING SAME

Номер: US20150045548A1
Автор: Kim Jae Seung, LEE Jong Jin, LEE Sang Ju, Moon Dae Hyuk, Oh Seung Jun, Ryu Jin Sook
Принадлежит:

The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [F]fluoride in a method for preparing an organic [F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [F]fluoride, wherein a [F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [F]fluoride or eluting a [F]fluoride using a [F]fluoride eluent with an adjusted pH, thereby stably obtaining a [F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies. 2. The method of claim 1 , wherein the alkyl group of Formula 1 is any one selected from the group consisting of a methyl group claim 1 , an ethyl group claim 1 , an isopropyl group claim 1 , a chloromethyl group claim 1 , a trifluoromethyl group claim 1 , and a chloroethyl group.3. The method of claim 1 , wherein the aryl group of Formula 1 is any one selected from the group consisting of a methylphenyl group claim 1 , an ethylphenyl group claim 1 , a chlorophenyl group claim 1 , a bromophenyl group claim 1 , a methoxyphenyl group claim 1 , and a nitrophenyl group.4. The method of claim 1 , wherein the ammonium of Formula 2 is selected from the group consisting of tetrabutylammonium claim 1 , benzyltrimethylammonium claim 1 , triethylammonium claim 1 , tributylammonium claim 1 , dibutylammonium claim 1 , dihexylammonium claim 1 , butylammonium claim 1 , and hexylammonium.5. An eluent of [F]fluoride prepared by the method of claim 1 , the eluent having a pH of 6-8 claim 1 , containing a metal salt or quaternary ammonium salt claim 1 , and ...

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Номер записи: 22
25-02-2016 дата публикации

NOVEL CURING AGENTS AND DEGRADEABLE POLYMERS AND COMPOSITES BASED THEREON

Номер: US20160052871A1
Автор: Li Xin, Liang Bo, Qin Bing
Принадлежит:

The present invention provides, among others, compounds of Formula (I) or a salt thereof, methods for making these compounds, degradable polymers and reinforced composites made therefrom, and methods for degrading and/or recycling the degradable polymers and reinforced composites. 2. The compound of claim 1 , wherein both m and n are 0.3. The compound of claim 1 , wherein both m and n are 1.4. The compound of claim 1 , wherein each of A and B claim 1 , independently claim 1 , is alkylene claim 1 , alkenylene claim 1 , arylene claim 1 , alkylene-arylene claim 1 , alkenylene-arylene claim 1 , alkynylene-arylene claim 1 , heteroarylene claim 1 , alkylene-heteroarylene claim 1 , alkenylene-heteroarylene claim 1 , or alkynylene-heteroarylene.5. The compound of claim 1 , wherein each of A and B claim 1 , independently claim 1 , is alkylene or arylene.6. The compound of claim 5 , wherein both A and B are claim 5 , at the same time claim 5 , alkylene or arylene.7. The compound of claim 6 , wherein both A and B are claim 6 , at the same time claim 6 , methylene claim 6 , ethylene claim 6 , or phenylene.8. The compound of claim 1 , wherein each of Rand R claim 1 , independently claim 1 , is hydrogen claim 1 , alkyl claim 1 , cycloalkyl claim 1 , heterocyclic claim 1 , heterocycloalkyl claim 1 , alkenyl claim 1 , cycloalkenyl claim 1 , aryl claim 1 , heteroaryl claim 1 , alkyl-hetero-alkyl claim 1 , alkynyl claim 1 , alkylene claim 1 , alkylene-hetero-alkylene claim 1 , alkenylene claim 1 , alkylene-hetero-alkenylene claim 1 , alkynylene claim 1 , or alkylene-hetero-alkynylene; or Rand R claim 1 , together with the carbon atom to which they are attached claim 1 , form a 3- to 7-membered saturated or unsaturated ring.9. The compound of claim 8 , wherein each of Rand R claim 8 , independently claim 8 , is hydrogen or alkyl claim 8 , or Rand R claim 8 , together with the carbon atom to which they are attached claim 8 , form a 3- to 7-membered saturated ring.10. The compound of ...

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Номер записи: 23
25-02-2016 дата публикации

Novel heterocyclic derivative and pharmaceutical composition comprising the same (as amended)

Номер: US20160052892A1
Автор: Hiroyuki Kai, Kentaro Asahi, Sae Jikihara, Takeshi Endoh, Tohru Horiguchi
Принадлежит: Shionogi and Co Ltd

The present invention provides novel compounds having a P2X 3 and/or P2X 2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X 3 and/or P2X 2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R 16 )— or the like; R 16 is hydrogen, substituted or unsubstituted alkyl or the like; R 7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q 1 and Q 2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R 6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R 2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.

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Номер записи: 24
23-02-2017 дата публикации

PROCESS FOR PREPARING SYMMETRIC PINCER LIGANDS FROM THE GROUP OF THE M-TERPHENYL COMPOUNDS

Номер: US20170050918A1
Автор: DYBALLA Katrin Marie, ELSLER Bernd, Franke Robert, Fridag Dirk, WALDVOGEL Siegfried R., WIEBE Anton
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a process for preparing compounds of the formula ABA 2. Process according to claim 1 ,characterized in thatthe electrochemical process step is conducted in such a way thataa) a mixture of at least one solvent and at least one conductive salt is produced,bb) the compounds to be converted are added to this mixture, with addition of the compound of the formula (A) in a molar excess based on the compound (B),cc) at least two electrodes are introduced into the reaction solution obtained in bb) and a voltage is applied to the electrodes,dd) the compounds (A) and (B) are converted to the compound (ABA),ee) the voltage is switched off, and optionallyff) the compound (ABA) is isolated and/or purified.3. Process according to claim 1 ,characterized in thatthe molar ratio of the compound (A) to the compound (B) is in the range from 1.5:1 to 4:1, preferably from 1.8:1 to 2.5:1 and more preferably 2:1.4. Process according to claim 1 ,characterized in thatcompounds of the formula (A) used are compounds in which X═NHR′.5. Process according to claim 1 ,characterized in that{'sub': '2', 'compounds of the formula (A) used are compounds in which X═—NH.'}6. Process according to claim 1 ,characterized in that{'sup': 6', '8, 'Rand Rare identical and are preferably hydrogen.'}7. Process according to claim 1 ,characterized in thatthe reaction is conducted in the presence of a solvent and the solvent used is a solvent from the group of acetonitrile, propylene carbonate, methyl carbonate, nitromethane, ethylene glycol dimethyl ether, methanesulphonic acid, benzene, toluene, water, methanol, ethanol, propanol, isopropanol, halogenated solvents or halogenated or non-halogenated acids or mixtures thereof.8. Process according to claim 7 ,characterized in thatsolvents used are methanol, formic acid, trifluoroacetic acid, hexafluoroisopropanol or mixtures thereof, preferably methanol, hexafluoroisopropanol or mixtures thereof, and preferably hexafluoroisopropanol.9. ...

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Номер записи: 25
03-03-2016 дата публикации

TRIARYLAMINE DERIVATIVE, ELECTROPHOTOGRAPHIC PHOTOSENSITIVE MEMEBER, AND IMAGE FORMING APPARATUS

Номер: US20160062253A1
Автор: Kojima Kensuke, MIYAMOTO Eiichi, OKADA Hideki, SUGAI Fumio, TSURUMI Hiroki, Yamamoto Yohei
Принадлежит: KYOCERA Document Solutions Inc.

A triarylamine derivative is represented by general formula (I). In general formula (I), Rand Reach represent, independently of one another, a chemical group selected from the group consisting of a halogen atom, an optionally substituted alkyl group having a carbon number of 1-6, an optionally substituted alkoxy group having a carbon number of 1-6, and an optionally substituted aryl group having a carbon number of 6-12. In general formula (I), k and l each represent an integer of at least 0 and no greater than 4. When k and l represent integers greater than 1, chemical groups Rbonded to the same aromatic ring and chemical groups Rbonded to the same aromatic ring may be the same or different to one another. In general formula (I), m and n each represent a different integer of at least 1 and no greater than 3. 2. The triarylamine derivative according to claim 1 , whereinin the general formula (I),{'sub': '1', 'Rrepresents a chemical group selected from the group consisting of an alkyl group having a carbon number of at least 1 and no greater than 6 and an alkoxy group having a carbon number of at least 1 and no greater than 6,'}{'sub': '2', 'Rrepresents an alkoxy group having a carbon number of at least 1 and no greater than 6, and'}k and l each represent 0 or 1.3. The triarylamine derivative according to claim 1 , whereinin the general formula (I), m represents 1 and n represents 2 or 3; or', 'm represents 2 or 3 and n represents 1, and, 'when k and l each represent 0when at least one of k and l represents an integer greater than 0, m and n each represent an integer of at least 1 and no greater than 3, and m and n represent different integers to one another.4. The triarylamine derivative according to claim 1 , whereinin the general formula (I),when k and l each represent 0, m represents 1 and n represents 2 or 3, andwhen at least one of k and l represents an integer greater than 0, m and n each represent an integer of at least 1 and no greater than 3, and m and n ...

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Номер записи: 26
03-03-2016 дата публикации

Triphenylamine derivative, electrophotographic photosensitive member, and image forming apparatus

Номер: US20160062254A1
Автор: Eiichi Miyamoto, Fumio Sugai, Hideki Okada, Hiroki TSURUMI, Kensuke Kojima, Yohei Yamamoto
Принадлежит: Kyocera Document Solutions Inc

A triphenylamine derivative is represented by general formula (1). In general formula (1), R 1 to R 7 each represent, independently of one another, a chemical group selected from the group consisting of a halogen atom, an optionally substituted alkyl group having a carbon number of at least 1 and no greater than 6, an optionally substituted alkoxy group having a carbon number of at least 1 and no greater than 6, and an optionally substituted aryl group having a carbon number of at least 6 and no greater than 12. Also, k, l, m, n, o, and p each represent, independently of one another, an integer of at least 0 and no greater than 4. When any of k, l, m, n, o, or p represents an integer greater than 1, chemical groups R 3 , R 4 , R 5 , R 6 , or R 7 bonded to the same aromatic ring may be the same or different.

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Номер записи: 27
05-03-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150065487A1
Автор: Anna Hazlewood, Ashvani Singh, Fred Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 28
27-02-2020 дата публикации

Polymorphic Forms of RAD1901-2HCL

Номер: US20200062694A1
Автор: Bolger Joshua Kyle, CRUSKIE, Eberlin Alex, Edwards Richard, JR. Michael Paul, Markey Michael, McKenzie Jonathan Blake, Sheth Pratik
Принадлежит:

Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed. 1. A solid form of RAD1901-2HCl , having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at 7.1 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.2. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising a peak claim 1 , in terms of 2-theta claim 1 , at 7.1 degrees 2θ±0.2 degree 2θ and/or 14.3 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.3. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least two peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ and 18.3 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.4. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least three peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ and 12.0 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.5. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least four peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ and 18.9 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.6. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least five peaks claim 1 , in terms of 2-theta claim 1 , selected from ...

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Номер записи: 29
18-03-2021 дата публикации

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

Номер: US20210077427A1
Автор: Gall Anna, Hong Feng, JR. Thomas L., Kuksa Vladimir A., Little, Orme Mark W., Scott Ian L.
Принадлежит:

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 137.-. (canceled)3953.-. (canceled)55. The method of claim 54 , wherein the retinal cell is a retinal neuronal cell.56. The method of claim 55 , wherein the retinal neuronal cell is a photoreceptor cell.58. (canceled)59. The method of claim 57 , wherein the lipofuscin is N-retinylidene-N-retinyl-ethanolamine (A2E).6068.-. (canceled) This application is a continuation of U.S. patent application Ser. No. 16/043,019, filed Jul. 23, 2018, which is a continuation of U.S. patent application Ser. No. 15/672,031, filed Aug. 8, 2017, which is a continuation of U.S. patent application Ser. No. 15/260,127, filed Sep. 8, 2016, which issued as U.S. Pat. No. 9,737,496 on Aug. 22, 2017, which is a continuation of U.S. patent application Ser. No. 14/631,763, filed Feb. 25, 2015, which issued as U.S. Pat. No. 9,458,088 on Oct. 4, 2016, and U.S. patent application Ser. No. 14/631,779, filed Feb. 25, 2015, now abandoned, both of which are a continuation of U.S. patent application Ser. No. 13/111,679, filed on May 19, 2011, which issued as U.S. Pat. No. 8,981,153 on Mar. 17, 2015, which is a continuation of U.S. patent application Ser. No. 12/287,039, filed on Oct. 3, 2008, which issued as U.S. Pat. No. 7,982,071 on Jul. 19, 2011, which claims the benefit of U.S. Provisional Application No. 60/977,957, filed Oct. 5, 2007; U.S. Provisional Application No. 61/066,353, filed Feb. 19, 2008; U.S. Provisional Application No. 61/043,127, filed Apr. 7, 2008; U.S. Provisional Application No. 61/051,657, filed May 8, 2008; and U.S. Provisional ...

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Номер записи: 30
05-06-2014 дата публикации

MAO-B INHIBITORS USEFUL FOR TREATING OBESITY

Номер: US20140155355A1
Автор: Chorvat Robert J., McElroy John Francis, Parthasarathi Rajagopalan
Принадлежит:

The invention provides novel compounds of formulae I and II: 113-. (canceled)1519-. (canceled)20. The method of claim 14 , wherein the disease is selected from obesity claim 14 , Type 2 diabetes claim 14 , hypertension claim 14 , dyslipidemia claim 14 , high blood pressure claim 14 , and insulin resistance.21. The method of claim 20 , wherein the compound is selected from Table A claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.22. The method of claim 20 , wherein the compound is selected from Table I claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.23. The method of claim 20 , wherein the compound is selected from Table IIa claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.24. The method of claim 20 , wherein the compound is selected from Table IIb claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.25. The method of claim 20 , wherein the compound is selected from Table IIIa claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.26. The method of claim 20 , wherein the compound is selected from Table IIIb claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.27. The method of claim 20 , wherein the compound is selected from Table IVa claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.28. The method of claim 20 , wherein the compound is selected from Table IVb claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.29. The method of claim 20 , wherein the compound is selected from Table IVc claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.30. The method of claim 20 , wherein the compound is selected from Table IVd claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.31. The method of claim 20 , wherein the compound is selected from Table V claim 20 , or a stereoisomer or pharmaceutically acceptable salt thereof.32. The method of claim 20 , wherein the ...

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Номер записи: 31
05-06-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140155431A1
Автор: Anna Hazlewood, Ashvani Singh, Fredrick Van Goor, Jason Mccartney, Jinglan Zhou, Peter Grootenhuis, Sara Hadida-Ruah
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 32
12-06-2014 дата публикации

HYDROLYSABLE LINKERS AND CROSS-LINKERS FOR ABSORBABLE POLYMERS

Номер: US20140163253A1
Автор: Bezwada Rao S.
Принадлежит: BEZWADA BIOMEDICAL, LLC

The present invention relates to the discovery of new class of linear and multiarmed hydrolysable linkers and cross linkers for use in the synthesis of biodegradable polymers such as, polyesters, polyurethanes, polyamides, polyureas and degradable epoxy amine resin. The linear and multiarmed hydrolysable linkers of the present invention include symmetrical and/or unsymmetrical ether carboxylic acids, amines, amide diols, amine polyols and isocyanates. 2. The linker of claim 1 , wherein:{'sub': 1-25', '1-6', '1-3', '2, 'R is a di-, tri, or tetra-radical derived from Calkyl, aryl, or aryl-(Calkyl)-, wherein from 1-3 of the CHgroups, within the alkyl chain are optionally independently replaced by O atoms, such that each of said O atoms is attached only to carbon atoms in the alkyl chain, with the proviso that the O atoms are separated from the di-, tri, or tetra-radical chain ends by at least one carbon atom and that multiple O in the di-, tri, tetra-radical chain must be separated from each other by at least two carbon atoms;'}{'sup': rd', 'rd', 'th', 'st', 'nd, 'provided that when R is a tri or tetra-radical, the 3or 3/4arms of formula X, XI, or XII are capped as shown for the 1and 2arms in formula X, XI, or XIII, respectively;'}{'sub': 2', '3', '2', '2', '2', '2', '2', '2', '2', '2, 'each X is independently: —OC(═O)CH—, —OC(═O)CH(CH)—, —OC(═O)CHOCHCH—, or —OC(═O)CHCHCHCHCH—;'}{'sup': '1', 'sub': 2', '3', '2', '2', '2', '2', '2', '2', '2', '2, 'each Xis independently: —CHC(═O)O—, —CH(CH)C(═O)O—, —CHCHOCHC(═O)O—, or —CHCHCHCHCHC(═O)O—;'}{'sub': 2', '3', '2', '2', '2', '2', '2', '2', '2', '2, 'each Y is independently: —OCHC(═O)—, —OCH(CH)C(═O)—, —OCHCHOCHC(═O)—, or —OCHCHCHCHCHC(═O)—;'}{'sup': '1', 'sub': 2', '3', '2', '2', '2', '2', '2', '2', '2', '2, 'each Yis independently: —C(═O)CHO—, —C(═O)CH(CH)O—, —C(═O)CHOCHCHO—, or —C(═O)CHCHCHCHCHO—.'}3. The linker of claim 2 , wherein:{'sub': 1-25', '1-6', '1-3', '2, 'R is a di-, tri, tetra-radical derived from Calkyl, aryl, ...

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Номер записи: 33
21-03-2019 дата публикации

METHOD OF TREATING CANCER USING SELECTIVE ESTROGEN RECEPTOR MODULATORS

Номер: US20190083421A1
Автор: McDonnell Donald P., Nelson Erik R., Wardell Suzanne E.
Принадлежит:

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM. 111.-. (canceled)13. A method of treating an estrogen receptor positive breast cancer in a subject , wherein the estrogen receptor positive breast cancer is resistant to an estrogen receptor modulator , the method comprising administering a composition comprising a salt of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5 ,6 ,7 ,8-tetrahydronaphthalen-2-ol.14. The method of claim 13 , wherein the estrogen receptor positive breast cancer is de novo resistant to the estrogen receptor modulator.15. The method of claim 13 , wherein the resistance to the estrogen receptor modulator is acquired.16. The method of claim 13 , wherein the estrogen receptor modulator is tamoxifen claim 13 , idoxifene claim 13 , raloxifene or ICI 182 claim 13 ,780.17. The method of claim 13 , wherein an effective amount of the composition is administered.18. The method of claim 17 , wherein the effective amount comprises a high dosage.19. The method of claim 18 , wherein the high dosage is more than about 20 mg/kg.20. The method of claim 17 , wherein the effective amount is from about 200 mg/day to about 500 mg/day.21. The method of claim 20 , wherein the effective amount is about 400 mg/day.22. The method of claim 13 , wherein the composition is administered by oral administration claim 13 , intravenous administration claim 13 , intradermal injection claim 13 , intramuscular injection or subcutaneous injection.23. The method of claim 13 , further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor) claim 13 , an antiestrogen claim 13 , a ligand of retinoic acid ...

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Номер записи: 34
29-03-2018 дата публикации

EBNA1 INHIBITORS AND THEIR METHOD OF USE

Номер: US20180086699A1
Автор: Lieberman Paul M., McDonnell Mark E., Messick Troy E., Reitz Allen B., Smith Garry R., Velvadapu Venkata, Zhang Yan
Принадлежит:

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection. 4. The method of claim 1 , wherein the compound is at least one selected from the group consisting of:3-{2-[3-(methylsulfamoyl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-3-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(3-methanesulfonamidophenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-[2-(3-sulfamoylphenyl)ethynyl]benzoic acid;3-[2-(3-carbamoylphenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-6-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(2-hydroxypyridin-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indazol-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[3-(3,3-dimethyl-2-oxoazetidin-1-yl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{3-[(2-carboxy-2,2-dimethylethyl)amino]phenyl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyrazin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-5-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-(2-{1H-pyrrolo[2,3-b]pyridin-5-yl}ethynyl)benzoic acid;3-[2-(1-methyl-1H-indol-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-methyl-1H-indol-5-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-benzothiophen-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-7-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[2-( ...

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Номер записи: 35
12-03-2020 дата публикации

METHODS AND SYSTEMS FOR WIRELESS TO POWER LINE COMMUNICATION

Номер: US20200083928A1
Автор: Bogdanovich Phillip
Принадлежит: Crius Technology Group, LLC

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture. 1. A system , comprising:a memory that stores instructions; and connecting a multifunction communication cube to a circuit;', 'recording, by utilizing the multifunction communication cube, signal noise from the circuit;', 'transmitting the signal noise to a remote device;', 'receiving, from the remote device, an identification a device connected to the circuit, wherein the device is identified based on a comparison of the signal noise to a first device waveform; and', 'generating a command signal associated with the device., 'a processor that executes the instructions to perform operations, the operations comprising2. The system of claim 1 , wherein the operations further comprise associating the command signal with the device.3. The system of claim 1 , wherein the operations further comprise facilitating determination of a second device waveform within the signal noise.4. The system of claim 3 , wherein the operations further comprise facilitating the identification of the device by determining that the second device waveform corresponds to the first device waveform.5. The system of claim 1 , wherein the operations further comprise controlling the device by utilizing the command signal.6. The system of claim 1 , wherein the operations further comprise interacting with the device by utilizing the command ...

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Номер записи: 36
05-04-2018 дата публикации

COMPOUNDS AND ORGANIC ELECTRONIC DEVICES

Номер: US20180097178A1
Автор: Buesing Arne, Montenegro Elvira, Mujica-Fernaud Teresa, Parham Amir Hossain, Voges Frank
Принадлежит:

The present invention relates to certain fluorenes, to the use of the compounds in an electronic device, and to an electronic device comprising at least one of these compounds. The present invention furthermore relates to a process for the preparation of the compounds and to a formulation and composition comprising one or more of the compounds. 122.-. (canceled) The present invention relates to novel organic compounds, to the use of the compounds in an electronic device, and to an electronic device comprising at least one of the compounds. The present invention furthermore relates to a process for the preparation of the compounds and to compositions and formulations comprising at least one of the compounds.The development of functional compounds for use in electronic devices is currently the subject of intensive research. The aim here is, in particular, the development of compounds with which improved properties of electroluminescent devices in one or more relevant points can be achieved, such as, for example, power efficiency, lifetime or colour coordinates of the emitted light.In accordance with the present invention, the term electronic device is taken to mean, inter alia, organic integrated circuits (OICs), organic field-effect transistors (OFETs), organic thin-film transistors (OTFTs), organic light-emitting transistors (OLETs), organic solar cells (OSCs), organic optical detectors, organic photoreceptors, organic field-quench devices (OFQDs), organic light-emitting electrochemical cells (OLECs), organic laser diodes (O-lasers) and organic electroluminescent devices (OLEDs).Of particular interest is the provision of compounds for use in the last-mentioned electronic devices called OLEDs. The general structure and the functional principle of OLEDs are well known to the person skilled in the art and are described, inter alia, in U.S. Pat. No. 4,539,507, U.S. Pat. No. 5,151,629, EP 0676461 and WO 1998/27136.Further improvements are still necessary with respect to ...

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Номер записи: 37
12-04-2018 дата публикации

PHENANTHRENE COMPOUNDS FOR ORGANIC ELECTRONIC DEVICES

Номер: US20180102479A1
Автор: Buesing Arne, KROEBER Jonas, Mujica-Fernaud Teresa, Voges Frank
Принадлежит:

The invention relates to specific phenanthrenes, the use of the compound in an electronic device, and an electronic device containing at least one of said compounds. The invention further relates to a method for producing the compound and a formulation and composition containing one or more of the compounds. 117.-. (canceled)24. The compound according to claim 23 , wherein Y is C(R)or NR.25. The compound according to claim 18 , wherein L is a single bond claim 18 , so that the amine group is bonded directly to the phenanthrene.26. The compound according to claim 18 , wherein the compound contains in total at least 26 ring atoms.27. The compound according to claim 18 , wherein the compound contains only one amine group.28. A process for the preparation of the compound according to which comprises a one-step Buchwald coupling by reaction of a phenanthrene derivative which contains a leaving group with Ar—NH—Ar.29. A process for the preparation of the compound according to which comprises a two-step Buchwald coupling by stepwise reaction of a phenanthrene derivative which contains a leaving group with (1) Ar—NHand (2) NH—Ar.30. An oligomer claim 18 , polymer or dendrimer containing one or more compounds according to claim 18 , where the bond(s) to the polymer claim 18 , oligomer or dendrimer is optionally localised at any desired positions in formula (1) which are substituted by R claim 18 , Ror R.31. A composition comprising one or more compound according to and at least one further organically functional material selected from the group consisting of fluorescent emitters claim 18 , phosphorescent emitters claim 18 , host materials claim 18 , matrix materials claim 18 , electron-transport materials claim 18 , electron-injection materials claim 18 , hole-conductor materials claim 18 , hole-injection materials claim 18 , electron-blocking materials and hole-blocking materials.32. A formulation comprising at least one compound according to and at least one solvent.33. An ...

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Номер записи: 38
03-07-2014 дата публикации

ANTI-AMYLOID COMPOUNDS AND METHODS

Номер: US20140187556A1
Автор: Banfield Scott C., BARDEN Christopher J., Reed Mark A., YADAV Arun
Принадлежит: Treventis Corporation

Anti-amyloid compounds are provided along with methods of use thereof. 2. The compound of in which the compound is according to Formula Ia.3. The compound of in which the compound is according to Formula Ib.4. The compound of in which the compound is according to Formula Ic.5. The compound of in which the compound is according to Formula Id.6. The compound of in which the compound is according to Formula Ie.7. The compound of in which the compound is according to Formula If.8. The compound of in which E is carbon.9. The compound of in which E is nitrogen.10. The compound of in which Ris nitro and Ris selected from the group consisting of ethanol-1-yl claim 3 , methanol claim 3 , 2 claim 3 ,2 claim 3 ,2-trifluoro-1-hydroxyethanol-1-yl claim 3 , and 2 claim 3 ,2 claim 3 ,2-trifluoroethanol-1-yl.11. The compound of in which the compound is 1-(3′-(benzylamino)-4′-nitro-[1 claim 10 ,1′-biphenyl]-3-yl)-2 claim 10 ,2 claim 10 ,2-trifluoroethanol.12. The compound of in which the compound is 1-(3′-(benzylamino)-4′-nitro-[1 claim 10 ,1′-biphenyl]-3-yl)-2 claim 10 ,2 claim 10 ,2-trifluoroethane-1 claim 10 ,1-diol.13. The compound of in which Ris nitro and Ris C-linked tetrazole.14. The compound of in which Ris nitro.15. The compound of in which Ris selected from the group consisting of sulfonamide claim 14 , alkylamide claim 14 , dialkylamide claim 14 , benzyl alkylamide claim 14 , N-pyrrolidinamide claim 14 , (N′-methanonylpiperazine)amide claim 14 , (N′-methylpiperazine)amide claim 14 , morphilinamide claim 14 , and piperidineamide.16. The compound of claim 1 , wherein compound inhibits the aggregation of an amyloidogenic protein.17. The compound of for use in the preparation of a pharmaceutically effective dosage form the treatment of amyloid diseases.18. The compound of claim 16 , wherein said amyloid disease is selected from the group consisting of Alzheimer's disease claim 16 , Parkinson's disease claim 16 , Huntington's disease claim 16 , and prion diseases.19. A ...

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Номер записи: 39
29-04-2021 дата публикации

Amphiphilic and Mesogenic Organic Dyes for Tailor-Made Reflective Low-Dimensional Materials

Номер: US20210122742A1
Автор: Dupeyre Grégory, Laine Philippe, Marvaud Valerie, Poulard Laurélie
Принадлежит:

The present invention relates to a compound of the following formula (I): 2. The compound according to claim 1 , wherein R═R′.5. The compound according to any one of to claim 1 , wherein Rrepresents a halogen atom claim 1 , a (C-C)alkyl claim 1 , (C-C)haloalkyl claim 1 , (CH)OR claim 1 , (CH)SR claim 1 , OR claim 1 , SRor NRRgroup claim 1 , wherein m and m′ are claim 1 , independently of each other claim 1 , equal to 1 claim 1 , 2 or 3 claim 1 , preferably 1.6. The compound according to any one of to claim 1 , wherein:{'sub': 4', '1', '20', '1', '20', '2', 'm', '24', '2', 'm', '25', '26', '27', '28', '29, 'Rrepresents a halogen atom, a (C-C)alkyl, (C-C)haloalkyl, (CH)OR, (CH)SR, OR, SRor NRRgroup wherein m and m′ are, independently of each other, equal to 1, 2 or 3, preferably 1;'}or{'sub': 4', '42', '43', '2', 'n', '44', '45', '2', '2, 'claim-text': Y and Y′ each represent, independently of each other, O, S or NH,', 'n is equal to 2 or 3,', {'sub': 42', '43', '1', '6, 'Rand R, each represent, independently of each other, a (C-C)alkyl group, and'}, {'sub': 44', '45', '1', '6, 'Rand Reach represent, independently of each other, a (C-C)alkyl group.'}], 'both Rgroups form together a bond or a chain selected from the group consisting of —C(RR)—, —(CH)—, —Si(RR)— and —Y—CH—CH—Y′—, wherein7. The compound according to any one of to claim 1 , wherein L represents a bond.8. The compound according to any one of to claim 1 , wherein Rand Reach represent claim 1 , independently of each other claim 1 , a hydrogen atom claim 1 , a halogen atom claim 1 , a (C-C)alkyl or (C-C)haloalkyl group claim 1 , notably a hydrogen atom or a (C-C)alkyl group claim 1 , preferably Rand Rboth represent a hydrogen atom.9. The compound according to any one of to claim 1 , wherein R═Rand/or R═Rand/or R═R.11. The compound according to any one of to claim 1 , wherein A represents a hexafluorophosphate claim 1 , tetrafluoroborate claim 1 , tetraphenylborate claim 1 , 2 claim 1 ,3-dichloro-5 claim 1 ,6- ...

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Номер записи: 40
26-04-2018 дата публикации

POLYMERIC AMINE SYNERGIST

Номер: US20180112037A1
Автор: Lane Gregg A., STRAMEL Rodney David, Zhou Zhang-Lin
Принадлежит:

A polymeric amine synergist is disclosed herein. An example of the polymeric amine synergist includes an aniline moiety, a polyethylene glycol chain, and an ether linkage attaching one end of the polyethylene glycol chain to the aniline moiety. The polymeric amine synergist may be included in a photo curable ink composition. 1. A polymeric amine synergist , comprising:an aniline moiety;a polyethylene glycol chain; andan ether linkage attaching one end of the polyethylene glycol chain to the aniline moiety.3. The polymeric amine synergist as defined in claim 1 , further comprising an additional aniline moiety attached to an opposed end of the polyethylene glycol chain through an additional ether linkage.5. The polymeric amine synergist as defined in wherein:the polyethylene glycol chain is a first polyethylene glycol chain; second and third polyethylene glycol chains; and', 'second and third aniline moieties;, 'the polymeric amine synergist further comprisesthe second polyethylene glycol chain is attached to an opposed end of the first polyethylene glycol chain and the second aniline moiety is attached to the second polyethylene glycol chain through a second ether linkage; andthe third polyethylene glycol chain is attached to the opposed end of the first polyethylene glycol chain and the third aniline moiety is attached to the third polyethylene glycol chain through a third ether linkage.7. The polymer amine synergist as defined in claim 5 , further comprising:a fourth polyethylene glycol chain attached to the opposed end of the first polyethylene glycol chain; anda fourth aniline moiety attached to the fourth polyethylene glycol chain through a fourth ether linkage.9. The polymeric amine synergist as defined in wherein the polymeric amine synergist is stable in water at a pH ranging from about 7 to about 14.10. The polymeric amine synergist as defined in wherein the polymeric amine synergist has a water solubility of at least 0.05 wt %.11. A photo curable ink ...

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Номер записи: 41
02-04-2020 дата публикации

CONTROLLING ZONES OF ELECTRONIC DEVICES ASSOCIATED WITH POWER LINES

Номер: US20200106479A1
Автор: Bogdanovich Phillip
Принадлежит: Crius Technology Group, LLC

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture. 1. A system , comprising:a first control apparatus comprising:a memory that stores instructions; determining which control apparatus of a plurality of control apparatuses including the first control apparatus has a strongest communication link with a remote device; and', 'facilitating relaying of data from the plurality of control apparatuses to the remote device through the control apparatus having the strongest communication link., 'a processor that executes the instructions to perform operations, the operations comprising2. The system of claim 1 , wherein the operations further comprise establishing a communication link between the control apparatus having the strongest communication link and at least one other control apparatus of the plurality of control apparatuses.3. The system of claim 1 , wherein the first control apparatus is configured to couple to a conductor in a power line associated with an electronic device receiving power from the power line.4. The system of claim 3 , wherein the operations further comprise redirecting the power from the conductor through the first control apparatus and to the electronic device.5. The system of claim 1 , wherein the operations further comprise determining claim 1 , after a period of time claim 1 , that a different control apparatus of the plurality of ...

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Номер записи: 42
13-05-2021 дата публикации

COMPOUNDS FOR TREATMENT OF CARDIAC ARRHYTHMIAS AND HEART FAILURE

Номер: US20210139429A1
Автор: BOATMAN Douglas, Sibrian-Vazquez Martha, THAINASHMUTHU Josephrajan
Принадлежит: Elex Biotech, Inc.

This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca-induced (or Ca-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof. 2. The compound according to claim 1 , wherein Ris —Y—X—(CR)—N(R)R.4. The compound according to claim 3 , wherein the compound has a structure according to Formula II claim 3 , and X is N(R) where Ris aliphatic.5. The compound according to claim 3 , wherein the compound has a structure according to formula III claim 3 , and Y is an imidazolyl claim 3 , pyrazolyl claim 3 , triazolyl claim 3 , tetrazolyl claim 3 , oxazolyl claim 3 , isoxazolyl claim 3 , oxadiazolyl claim 3 , furazanyl claim 3 , thiazolyl claim 3 , isothiazolyl claim 3 , or thiadiazolyl group.6. (canceled)7. The compound according to claim 5 , wherein Y is a tetrazolyl or oxadiazolyl group.911-. (canceled)12. The compound according to claim 1 , wherein:{'sup': 4', '5, '(i) Rand Rare alkyl; or'}(ii) m is 2, or n is 1, or m is 2 and n is 1; or{'sup': 6', '7', '6', '7, '(iii) Ris H, or each Ris H, or Ris H and each Ris H; or'}(iv) any combination thereof.1318-. (canceled)19. The compound according to claim 1 , wherein:{'sup': A', '1', '2', '1', '2, 'Ris —N(R)Rwhere Ris H or aliphatic and Ris H or aliphatic;'}{'sup': 'B', 'Ris H, aliphatic, —O-aliphatic, —S-aliphatic, —O—C(O)-aliphatic, or halogen;'}{'sup': 'C', 'Ris H, aliphatic, —S-aliphatic, or —O—C(O)-aliphatic; and'}{'sup': 'D', 'sub': 2', 'q', '2', '2', 'q', '2', 'q', '3, 'Ris —(CH)NH, —(CH)OH, or —(CH)SOM where q is an integer from 1 to 10 and M is a monatomic cation.'}2022-. (canceled)23. The compound according to claim 1 , wherein the compound is:{'sup': 1', '2', '2, 'N-(4-amino-2-methoxybenzyl)-N,N-diethylethane-1,2-diamine;'}3-methoxy-4-(((2 ...

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Номер записи: 43
03-05-2018 дата публикации

AROMATIC AMINE DERIVATIVE, AND ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME

Номер: US20180123043A1
Автор: Fujiyama Takahiro, Kato Tomoki, Sado Takayasu
Принадлежит: IDEMITSU KOSAN CO., LTD.

An aromatic amine derivative represented by formula (1): 6. An organic electroluminescence device comprising an anode , a cathode , and at least one organic thin film layer disposed between the anode and the cathode , wherein:the at least one organic thin film layer comprises a light emitting layer; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one organic thin film layer comprises the aromatic amine derivative according to .'}7. The organic electroluminescence device according to claim 6 , wherein the at least one organic thin film layer comprises a hole injecting layer or a hole transporting layer claim 6 , and the hole injecting layer or the hole transporting layer comprises the aromatic amine derivative This application is a continuation application of prior U.S. application Ser. No. 14/424,656, filed Feb. 27, 2015, the disclosure of which is incorporated herein by reference in its entirety. U.S. application Ser. No. 14/424,656 is the National Stage of PCT/JP13/073187, filed Aug. 29, 2013, the disclosure of which is incorporated herein by reference in its entirety. U.S. application Ser. No. 14/424,656 claims priority to Japanese Application No. 2012-191939, filed Aug. 31, 2012, the disclosure of which is incorporated herein by reference in its entirety.The present invention relates to aromatic amine derivatives and organic electroluminescence devices using the aromatic amine derivatives. For example, the present invention relates to aromatic amine derivatives having a substituted or unsubstituted 9,9-diphenylfluorene skeleton and organic electroluminescence devices employing the aromatic amine derivative.Generally, an organic electroluminescence (EL) device includes an anode, a cathode, and at least one organic thin film layers which are interposed between the anode and the cathode. When applying a voltage between both electrodes, electrons are injected into an emission region from the cathode side and holes are injected into the emission region ...

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Номер записи: 44
23-04-2020 дата публикации

METHOD OF TREATING CANCER USING SELECTIVE ESTROGEN RECEPTOR MODULATORS

Номер: US20200121621A1
Автор: McDonnell Donald P., Nelson Erik R., Wardell Suzanne E.
Принадлежит:

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM. 112-. (canceled)13. A method of treating an estrogen receptor positive breast cancer in a subject , wherein the estrogen receptor positive breast cancer is resistant to an estrogen receptor modulator , the method comprising administering a composition comprising (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5 ,6 ,7 ,8-tetrahydronaphthalen-2-ol , or a salt thereof.14. The method of claim 13 , wherein the estrogen receptor positive breast cancer is de novo resistant to the estrogen receptor modulator.15. The method of claim 13 , wherein the resistance to the estrogen receptor modulator is acquired.16. The method of claim 13 , wherein the estrogen receptor modulator is tamoxifen claim 13 , idoxifene claim 13 , raloxifene or ICI 182 claim 13 ,780.17. The method of claim 13 , wherein an effective amount of the composition is administered.18. The method of claim 17 , wherein the effective amount comprises a high dosage.19. The method of claim 18 , wherein the high dosage is more than about 20 mg/kg.20. The method of claim 17 , wherein the effective amount is from about 200 mg/day to about 500 mg/day.21. The method of claim 20 , wherein the effective amount is about 400 mg/day.22. The method of claim 13 , wherein the composition is administered by oral administration claim 13 , intravenous administration claim 13 , intradermal injection claim 13 , intramuscular injection or subcutaneous injection.23. The method of claim 13 , further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor) claim 13 , an antiestrogen claim 13 , a ligand of ...

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Номер записи: 45
17-05-2018 дата публикации

Methods and Compositions for Inhibition of Bromodomain-Containing Proteins

Номер: US20180134715A1
Автор: Padia Janak Khimchand, Strovel Jeffrey W., Vankayalapati Hariprasad, Yoshioka Makoto
Принадлежит:

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders. 155-. (canceled)57. The method of claim 56 , wherein Ris substituted or unsubstituted aryl claim 56 , or substituted or unsubstituted heteroaryl.58. The method of claim 56 , wherein Lis —(CRR) claim 56 , wherein Rand Rare each hydrogen or methyl and nis 1 or 2.59. The method of claim 56 , wherein L-Ris methyl.60. The method of claim 56 , wherein Ris H.61. The method of claim 56 , wherein Ris H.62. The method of claim 56 , wherein Ris H.65. The method of claim 56 , wherein:{'sub': 1C', '10C', '11C', 'nC', '10C', '11C', 'C, 'Lis —(CRR)wherein Rand Rare independently selected from hydrogen and methyl; and nis 1 or 2;'}{'sub': 2C', '4C, 'L-Ris methyl;'}{'sub': 1C', '1-6, 'Ris Calkyl, halogen-substituted phenyl, unsubstituted phenyl, or unsubstituted 5-7 membered heteroaryl, wherein the heteroaryl includes 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur;'}{'sub': '2C', 'Ris hydrogen;'}{'sub': '3C', 'Ris hydrogen; and'}{'sub': '8C', 'Ris hydrogen.'}66. The method of claim 56 , wherein Ris selected from substituted or unsubstituted aryl claim 56 , or substituted or unsubstituted heteroaryl; Rand Rare hydrogen; Ris selected from substituted or unsubstituted aryl claim 56 , or substituted or unsubstituted heteroaryl; Ris selected from substituted or unsubstituted aryl claim 56 , or substituted or unsubstituted heteroaryl; Lis —(C—RR)— wherein Rand Rare independently selected from hydrogen and methyl and nis 1 or 2; and Lis —(CRR)— claim 56 , wherein n is 0 claim 56 , 1 claim 56 , 2 claim 56 , or 3.68. The method of claim 56 , wherein the compound is 4-(benzylamino)-6-(3 claim 56 ,5-dimethylisoxazol-4-yl)-1-methylquinolin-2(1H)-one ...

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Номер записи: 46
08-09-2022 дата публикации

Triaryl phosphine ligands, preparation method therefor, and use in catalysing coupling reactionsons

Номер: US20220281901A1
Автор: Fabin ZHOU, Jicheng Shi
Принадлежит: Dongguan Stephen Catalyst Co Ltd

Triaryl phosphine ligands, as shown in general formulae Ia and Ib, or a mixture thereof, and a preparation method therefor. The invention addresses the deficiencies of biaryl phosphine ligands invented by Buchwald et al. Also provided are a triaryl phosphine coordinated palladium complex, a system composed of triaryl phosphine ligand and a palladium salt or complex, and a use of the triaryl phosphine coordinated palladium complex in catalysing organic reactions, in particular a use in catalysis of coupling reactions involving (pseudo)halogenated aromatic hydrocarbon as substrate.

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Номер записи: 47
04-06-2015 дата публикации

CATIONIC PARA-PHENYLENEDIAMINES, COMPOSITION COMPRISING AT LEAST SUCH COMPOUNDS, IMPLEMENTATION PROCESS THEREFOR AND USE THEREOF

Номер: US20150150766A1
Автор: Fadli Aziz
Принадлежит:

The present invention relates to particular cationic paraphenylenediamine compounds of formula (I) below and also to the use thereof for dyeing keratin fibres, in particular human keratin fibres such as the hair. The invention also relates to a dye composition comprising, in a suitable dyeing medium, one or more cationic para-phenylenediamines as defined previously. Finally, the invention relates to a dyeing device using the said composition. 113-. (canceled)15. The cationic para-phenylenediamine of formula (I) according to claim 14 , wherein:{'sub': 1', '4, 'R is chosen from a hydrogen atom and a C-Calkyl radical,'}{'sub': 1', '6', '6', '1', '2, 'Zis chosen from an oxygen atom and a group NRwith Rrepresenting a hydrogen atom or a C-Calkyl radical,'}{'sub': 1', '1', '8, 'Ris chosen from a linear or branched C-Calkyl radical, substituted with a cationic radical; and a saturated, unsaturated or aromatic, 5- to 8-membered non-cationic ring substituted with a cationic radical, and'}{'sub': 1', '6', '1', '6, 'when Zrepresents NRthen Rand Rmay form, together with the nitrogen atom to which they are attached, a saturated or unsaturated cationic 5- to 8-membered heterocycle, it being possible for the heterocycle to contain one or more heteroatoms chosen from N or O; or a saturated or unsaturated non-cationic 5- to 8-membered heterocycle substituted with a cationic radical.'}16. The cationic para-phenylenediamine of formula (I) according to claim 14 , wherein the cationic radical is chosen from trimethylammonium claim 14 , trimethylammonium and tri-β-hydroxyethylammonium radicals.17. The cationic para-phenylenediamine of formula (I) according to claim 14 , wherein the cationic heterocycle is chosen from piperazinium claim 14 , pyrrolidinium claim 14 , morpholinium claim 14 , pyrrolidine claim 14 , piperidine claim 14 , morpholine and piperazine rings.18. The cationic para-phenylenediamine of formula (I) according to claim 14 , wherein:R is a hydrogen atom,{'sub': 1', '3, ' ...

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Номер записи: 48
08-09-2022 дата публикации

AROMATIC AMINE DERIVATIVE, AND ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME

Номер: US20220285620A1
Автор: Fujiyama Takahiro, Kato Tomoki, Sado Takayasu
Принадлежит: IDEMITSU KOSAN CO., LTD.

An aromatic amine derivative represented by formula (1): 5: The aromatic amine derivative according to claim 1 , wherein R claim 1 , Rand Rin formula (1) each independently represents a hydrogen atom claim 1 , a methyl group claim 1 , an ethyl group claim 1 , a n-propyl group claim 1 , an isopropyl group claim 1 , a n-butyl group claim 1 , an isobutyl group claim 1 , a s-butyl group claim 1 , a t-butyl group claim 1 , or a phenyl group.6: The aromatic amine derivative according to claim 1 , wherein R claim 1 , Rand Rin formula (1) represent hydrogen atoms.7: The aromatic amine derivative according to claim 1 , wherein Rin formula (16) for L in formula (1) represents a hydrogen atom.8: The aromatic amine derivative according to claim 1 , wherein Rin formulae (2) and (3) represents a hydrogen atom claim 1 , a phenyl group or a biphenylyl group.9: The aromatic amine derivative according to claim 1 , wherein Rin formulae (2) and (3) represents a hydrogen atom.10: The aromatic amine derivative according to claim 1 , wherein Rin formulae (7) to (11) represents a hydrogen atom claim 1 , a methyl group claim 1 , a t-butyl group claim 1 , or a phenyl group.11: The aromatic amine derivative according to claim 1 , wherein Rin formula (7) is a phenyl group.12: The aromatic amine derivative according to claim 1 , wherein Rin formulae (8) to (11) represents a hydrogen atom.13: The aromatic amine derivative according to claim 1 , wherein Rin formula (16) for L in formulae (10) and (11) represents a hydrogen atom.14: The aromatic amine derivative according to claim 2 ,{'sup': '1', 'claim-text': {'sup': '1', 'Rrepresents a hydrogen atom and m represents 4; and'}, 'wherein in (R)m of formula (7-2){'sup': '1', 'claim-text': {'sup': '1', 'Rrepresents a phenyl group and k represents 1.'}, 'wherein in (R)k of formula (7-2)15: An organic electroluminescence device comprising an anode claim 2 , a cathode claim 2 , and at least one organic thin film layer disposed between the anode and the ...

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Номер записи: 49
04-06-2015 дата публикации

Method For Preparing Methylated Amines

Номер: US20150152072A1
Автор: Cantat Thibault, Gomes Christophe, Jacquet Olivier
Принадлежит:

The present invention relates to a method for preparing methylated amines using carbon dioxide and to the use of the method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres and synthetic leathers, pesticides and fertilizers. The invention also relates to a method for manufacturing vitamins, pharmaceutical products, glues, acrylic fibres, synthetic leathers, pesticides and fertilizers, including a step of preparing methylated amines by the method according to the invention. The present invention also relates to a method for preparing marked methylated amines and to the uses thereof. 2. The process as claimed in claim 1 , wherein in the amine of formula (II) claim 1 , Rand Rrepresent claim 1 , independently of one another claim 1 , a hydrogen atom claim 1 , an alkyl group claim 1 , an aryl group or a heteroaryl group claim 1 , said alkyl claim 1 , aryl and heteroaryl groups optionally being substituted claim 1 , or{'sup': 1', '2, 'Rand R, taken together with the nitrogen atom to which they are bonded, form an optionally substituted heterocycle.'}3. The process as claimed in claim 1 , wherein the silane compound of formula (III) claim 1 , R claim 1 , Rand Rrepresent claim 1 , independently of one another claim 1 , a hydrogen atom claim 1 , an alkyl group claim 1 , an alkoxy group claim 1 , an aryl group claim 1 , a silyl group or a siloxy group claim 1 , said alkyl claim 1 , alkoxy claim 1 , silyl claim 1 , siloxy and aryl groups optionally being substituted.4. The process as claimed in claim 1 , wherein the catalyst is selected from the group consisting of organic catalysts and metal catalysts claim 1 , the metal catalysts being chosen from metal salts or metal complexes.5. The process as claimed in claim 4 , wherein the organic catalyst is:a secondary or tertiary amine selected from the group consisting of triazabicyclodecene (TBD), N-methyltriazabicyclodecene (MeTBD), 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), trimethylamine, triethylamine, ...

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Номер записи: 50
02-06-2016 дата публикации

Triarylamine derivative and electrophotographic photosensitive member

Номер: US20160152552A1
Автор: Fumio Sugai, Hideki Okada, Kensuke Kojima
Принадлежит: Kyocera Document Solutions Inc

A triarylamine derivative is represented by general formula (1) shown below. In general formula (1), R 1 , R 2 , and R 3 each represent, independently of one another, a halogen atom, an optionally substituted alkyl group having a carbon number of at least 1 and no greater than 6, an optionally substituted alkoxy group having a carbon number of at least 1 and no greater than 6, or an optionally substituted aryl group having a carbon number of at least 6 and no greater than 12. In general formula (1), o, p, and q each represent, independently of one another, an integer of at least 0 and no greater than 4, and m and n each represent, independently of one another, an integer of at least 1 and no greater than 2.

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Номер записи: 51
16-05-2019 дата публикации

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Номер: US20190144450A1
Автор: Grootenhuis Peter, Hadida-Ruah Sara, Hazlewood Anna, McCartney Jason, Singh Ashvani, Van Goor Fredrick, Zhou Jinglan
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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Номер записи: 52
31-05-2018 дата публикации

PHOTOREDOX-CATALYZED DIRECT C-H FUNCTIONALIZATION OF ARENES

Номер: US20180148414A1
Автор: Margrey Kaila, Nicewicz David, Romero Nathan, Tay Nicholas
Принадлежит:

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is a halogen.4. The method of claim 3 , wherein the halogen is selected from fluorine and chlorine.5. The method of claim 1 , wherein Z is selected from C1-C4 alkylamino claim 1 , C1-C4 dialkylamino claim 1 , arylamino claim 1 , diarylamino claim 1 , and C1-C4 alkarylamino.6. The method of claim 1 , wherein Z is —NH.7. The method of claim 1 , wherein Z is Ar.8. The method of claim 7 , wherein Aris selected from pyrazole claim 7 , 1 claim 7 ,2 claim 7 ,3-triazole claim 7 , 1 claim 7 , 2 claim 7 , 4-triazole claim 7 , benzotriazole claim 7 , imidazole claim 7 , and benzimidazole.12. The method of claim 1 , wherein the nucleophile is a halide.13. The method of claim 12 , wherein the halide is selected from ammonium fluoride claim 12 , cesium fluoride claim 12 , lithium chloride claim 12 , triethylamine hydrochloride claim 12 , and triethylamine hydrofluoride.14. The method of claim 1 , wherein the nucleophile is an amine.15. The method of claim 14 , wherein the amine is ammonium bicarbonate.16. The method of claim 1 , wherein the ...

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Номер записи: 53
08-06-2017 дата публикации

ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF-I

Номер: US20170158628A1
Автор: Avery Thomas, Giethlen Bruno, Harvey Andrew, HUFF Belinda, JOSEPH CHRISTOPHE, MORICE Christophe, Paul Dharam, Ripper Justin, Schaeffer Laurent, Singh Rajinder
Принадлежит: Merck Sharp & Dohme Corp.

The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases. 153-) (canceled)55) A compound according to claim 54 , or a pharmaceutically acceptable salt thereof claim 54 , wherein Rand Rare both C-Calkyl (preferably methyl) claim 54 , or Rand Rtogether form a C-Ccycloalkyl ring.56) A compound according to or a pharmaceutically acceptable salt thereof claim 54 , wherein Rand Rare both F.57) A compound according to or a pharmaceutically acceptable salt thereof claim 54 , wherein Rand Rare both methyl.58) A compound according to or a pharmaceutically acceptable salt thereof claim 54 , wherein Ris methyl claim 54 , and Ris hydrogen.59) A compound according to or a pharmaceutically acceptable salt thereof claim 54 , wherein Rand Rtogether form a C-Ccycloalkyl ring claim 54 , preferably cyclopentyl or cyclohexyl ring. The present invention relates to chemical compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (α7 nAChR). The invention also relates to the use of these compounds In the treatment or prevention of a broad range of diseases in which the positive modulation of α7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.The α7 nAChRs are rapidly desensitizing ligand-gated ion channels that are abundantly expressed in the cerebral cortex and the hippocampus, a limbic structure intimately linked to attention processing and memory formation. α7 nAChRs modulate neurotransmitter release and are responsible for ...

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Номер записи: 54
07-06-2018 дата публикации

ELECTROPHOTOGRAPHIC PHOTOSENSITIVE MEMBER

Номер: US20180157183A1
Автор: OKADA Hideki
Принадлежит: KYOCERA Document Solutions Inc.

An electrophotographic photosensitive member includes a conductive substrate and a photosensitive layer containing a charge generating material, a hole transport material, a quinone derivative, and a binder resin. The quinone derivative is represented by general formula (1) or (2), where R, R, R, R, and Reach represent, independently of one another, a hydrogen atom, an alkyl group having a carbon number of at least 1 and no greater than 12, an aryl group that has a carbon number of at least 6 and no greater than 14 and that may have an alkyl group having a carbon number of at least 1 and no greater than 6, an aralkyl group having a carbon number of at least 7 and no greater than 12, or a cycloalkyl group having a carbon number of at least 3 and no greater than 10. Z represents an oxygen atom or a sulfur atom. 2. The electrophotographic photosensitive member according to claim 1 , whereinin the general formula (1),{'sup': 1', '2', '3, 'R, R, and Reach represent, independently of one another, an alkyl group having a carbon number of at least 1 and no greater than 12 or an aryl group that has a carbon number of at least 6 and no greater than 14 and that is substituted with an alkyl group having a carbon number of at least 1 and no greater than 6,'}in the general formula (2),{'sup': 4', '5, 'Rand Reach represent, independently of one another, an alkyl group having a carbon number of at least 1 and no greater than 12 or an aryl group that has a carbon number of at least 6 and no greater than 14 and that is substituted with an alkyl group having a carbon number of at least 1 and no greater than 6, and'}Z represents a sulfur atom.4. The electrophotographic photosensitive member according to claim 1 , whereinthe photosensitive layer is a single-layer photosensitive layer.5. The electrophotographic photosensitive member according to claim 1 , whereinthe charge generating material is an X-form metal-free phthalocyanine pigment.7. The electrophotographic photosensitive member ...

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Номер записи: 55
16-06-2016 дата публикации

Biaryl derivatives as gpr120 agonists

Номер: US20160168096A1
Автор: Eun Sil Choi, Hyun Woo Joo, Sang Yun PARK, Young Kwan Kim
Принадлежит: LG Life Sciences Ltd

The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.

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Номер записи: 56
25-06-2015 дата публикации

SECONDARY AMINES AS THERAPEUTIC AGENTS

Номер: US20150175567A1
Автор: Ngo Vinh X., Old David W.
Принадлежит:

Compounds such as those represented by Formulas 1-6 can be used in topical liquids, creams, or other dosage forms such as solids, for reducing intraocular pressure, treating glaucoma, growing hair, or other medical uses. 2. The compound of claim 1 , wherein a is 1.3. The compound of claim 1 , wherein a is 2.4. The compound of claim 1 , wherein Ris H.5. The compound of claim 1 , wherein Ris H.6. The compound of claim 1 , wherein Ris H.7. The compound of claim 1 , wherein W is CH.8. The compound of claim 1 , wherein W is O.9. The compound of claim 1 , wherein X is NR.10. The compound of claim 9 , wherein Ris H.11. The compound of claim 9 , wherein Ris Calkyl claim 9 , or COCH.12. The compound of claim 1 , wherein X is O.13. The compound of claim 1 , wherein L is -A-OCH—.14. The compound of claim 1 , wherein A is interphenylene.15. The compound of claim 1 , wherein Q is COR.16. The compound of claim 1 , wherein Q is CHOH.17. The compound of claim 1 , wherein B is 3-fluorophenyl.19. An ophthalmic liquid comprising a compound according to .20. A solid dosage form comprising a compound according to .21. An ophthalmic liquid comprising a compound according to .22. A solid dosage form comprising a compound according to .23. A method of reducing intraocular pressure comprising administering a compound according to to a mammal in need thereof.24. A method or growing hair comprising administering a compound according to to a mammal in which hair growth is desirable. This application claims priority to and the benefit of U.S. Provisional Patent Application No. 61/919,557, filed Dec. 20, 2013, the disclosure of which is hereby incorporated by reference in its entirety.Ocular hypotensive agents are useful in the treatment of a number of various ocular hypertensive conditions, such as post-surgical and post-laser trabeculectomy ocular hypertensive episodes, glaucoma, and as pre-surgical adjuncts.Glaucoma is a disease of the eye characterized by increased intraocular pressure. On ...

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Номер записи: 57
23-06-2016 дата публикации

TRIARYLAMINE DERIVATIVE AND ELECTROPHOTOGRAPHIC PHOTOSENSITIVE MEMBER

Номер: US20160179020A1
Автор: Kojima Kensuke, OKADA Hideki, SUGAI Fumio
Принадлежит: KYOCERA Document Solutions Inc.

A triarylamine derivative is represented by general formula (1) shown below. 3. The triarylamine derivative according to claim 1 , wherein{'sub': 1', '2, 'in the general formula (1), at least one Ror Rrepresents a methyl group.'}4. An electrophotographic photosensitive member comprisinga conductive substrate and a photosensitive layer, wherein{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the photosensitive layer contains the triarylamine derivative according to .'}5. The electrophotographic photosensitive member according to whereinthe photosensitive layer is a single-layer type photosensitive layer in which a charge generating material, a hole transport material, an electron transport material, and a binder resin are contained in the same layer as one another, andthe hole transport material includes the triarylamine derivative.6. The electrophotographic photosensitive member according to claim 5 , whereinthe charge generating material includes Y-form titanyl phthalocyanine.7. An electrophotographic photosensitive member comprisinga conductive substrate and a photosensitive layer, wherein{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'the photosensitive layer contains the triarylamine derivative according to .'}8. The electrophotographic photosensitive member according to whereinthe photosensitive layer is a single-layer type photosensitive layer in which a charge generating material, a hole transport material, an electron transport material, and a binder resin are contained in the same layer as one another, andthe hole transport material includes the triarylamine derivative.9. The electrophotographic photosensitive member according to claim 8 , whereinthe charge generating material includes Y-form titanyl phthalocyanine.10. An electrophotographic photosensitive member comprisinga conductive substrate and a photosensitive layer, wherein{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'the photosensitive layer contains the triarylamine derivative according ...

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Номер записи: 58
28-06-2018 дата публикации

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

Номер: US20180177746A1
Автор: Gall Anna, Hong Feng, JR. Thomas L., Kuksa Vladimir A., Little, Orme Mark W., Scott Ian L.
Принадлежит:

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 168.-. (canceled)69. A method of modulating chromophore flux in a retinoid cycle comprising introducing into a subject a non-retinoid aromatic compound that inhibits 11-cis-retinol production with an ICof about 0.1 micromolar or less when assayed in vitro , the assay consisting of a homogenate of HEK293 cell clone expressing recombinant human RPE65 and LRAT as the source of visual enzyme , exogenous all-trans-retinol in the amount of about 20 μM , recombinant human CRALBP in the amount of about 80 μg/mL , about 10 mM pH 7.2 phosphate buffer , about 0.5% BSA and about 1 mM NaPPi , and wherein the amount of assay reaction product 11-cis-retinol being determined by HPLC analysis following heptane extraction of the assay reaction mixture and wherein the non-retinoid aromatic compound consists of a benzene core that is substituted with a first substituent , a second substituent , and an optional third substituent , wherein the first and second substituents are attached to the benzene core in a meta-substitution configuration , wherein the first substituent is a group selected from —CH(OH)CH(R)CHNHwherein R is H , CH , or —OH and the second substituent is an optionally substituted alkoxy group , and wherein the optional third substituent is a halogen or —OH.70. The method of claim 69 , wherein the R is H.71. The method of claim 69 , wherein the optionally substituted alkoxy group is —OR′ wherein R′ is optionally substituted C-Calkyl claim 69 , or optionally substituted carbocyclyalkyl.72. The method of claim 69 , wherein the ...

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Номер записи: 59
04-06-2020 дата публикации

NOVEL (POLY)AMINE COMPOUND, RESIN AND CURED PRODUCT

Номер: US20200172470A1
Автор: ECHIGO Masatoshi, MAKINOSHIMA Takashi, MATSUURA Yutaka, SHISHIMI Toru
Принадлежит:

A (poly)amine compound represented by the following formula (0): 5. The (poly)amine compound according to claim 4 , wherein{'sup': '3A′', 'R is any of a linear or branched, or cyclic alkyl group or alkoxy group having 1 to 30 carbon atoms and optionally having a substituent, an aryl group having 6 to 30 carbon atoms and optionally having a substituent, a crosslinking group having 2 to 30 carbon atoms and optionally having a substituent, a hydroxy group and a cyano group; and'}{'sup': 1', '3A′, 'when Ris a benzene ring or a naphthalene ring, R is any of a linear or branched, or cyclic alkyl group or alkoxy group having 1 to 30 carbon atoms and optionally having a substituent, an aryl group having 6 to 30 carbon atoms and optionally having a substituent, a crosslinking group having 2 to 30 carbon atoms and optionally having a substituent, a hydroxy group and a cyano group.'}12. The (poly)amine compound according to claim 1 , wherein X is an oxygen atom in the formulas (0) claim 1 , (1) claim 1 , (2) and (3).14. A resin comprising a monomer unit containing a unit derived from the (poly)amine compound according to .16. A cured product obtained by curing a curable compound with a curing agent claim 1 ,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the curing agent comprises the (poly)amine compound according to .'}20. The (poly)amine compound according to claim 2 , wherein X is an oxygen atom in the formulas (0) claim 2 , (1) claim 2 , (2) and (3).22. A resin comprising a monomer unit containing a unit derived from the (poly)amine compound according to .23. A cured product obtained by curing a curable compound with a curing agent claim 2 , wherein the curing agent comprises the (poly)amine compound according to . The present invention relates to a novel (poly)amine compound, resin and cured product.(Poly)amine compounds have been used as a raw material for functional resins such as polyurea, polyamide, polyimide, polyamideimide, benzoxazine and maleimide, and ...

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Номер записи: 60
05-07-2018 дата публикации

POLYMORPHIC FORMS OF RAD1901-2HCL

Номер: US20180186726A1
Автор: Bolger Joshua Kyle, CRUSKIE, Eberlin Alex, Edwards Richard, JR. Michael Paul, Markey Michael, McKenzie Jonathan Blake, Sheth Pratik
Принадлежит:

Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed. 1. A solid form of RAD1901-2HCl , having an X-ray powder diffraction pattern comprising a peak , in terms of 2-theta , at 7.1 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.2. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising a peak claim 1 , in terms of 2-theta claim 1 , at 7.1 degrees 2θ±0.2 degree 2θ and/or 14.3 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.3. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least two peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ and 18.3 degrees 2θ±0.2 degree 2θ at about relative humidity 0%.4. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least three peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ and 12.0 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.5. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least four peaks claim 1 , in terms of 2-theta claim 1 , selected from the group consisting of 7.1 degrees 2θ±0.2 degree 2θ claim 1 , 14.3 degrees 2θ±0.2 degree 2θ claim 1 , 18.3 degrees 2θ±0.2 degree 2θ claim 1 , 13.8 degrees 2θ±0.2 degree 2θ claim 1 , 12.0 degrees 2θ±0.2 degree 2θ claim 1 , 25.1 degrees 2θ±0.2 degree 2θ and 18.9 degrees 2θ±0.2 degree 2θ claim 1 , at about relative humidity 0%.6. The solid form of claim 1 , having an X-ray powder diffraction pattern comprising at least five peaks claim 1 , in terms of 2-theta claim 1 , selected from ...

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Номер записи: 61
20-06-2019 дата публикации

Alkoxy compounds for disease treatment

Номер: US20190183816A1
Автор: Anna Gall, Feng Hong, Ian L. Scott, Mark W. Orme, Thomas L. Little, Jr., Vladimir A. Kuksa
Принадлежит: Acucela Inc

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

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Номер записи: 62
11-06-2020 дата публикации

EBNA1 INHIBITORS AND THEIR METHOD OF USE

Номер: US20200181078A1
Автор: Lieberman Paul M., McDonnell Mark E., Messick Troy E., Reitz Allen B., Smith Garry R., Velvadapu Venkata, Zhang Yan
Принадлежит:

Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection. 122-. (canceled)25. The compound of claim 23 , wherein the compound is selected from the group consisting of:3-{2-[3-(methylsulfamoyl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-3-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(3-methanesulfonamidophenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-[2-(3-sulfamoylphenyl)ethynyl]benzoic acid;3-[2-(3-carbamoylphenyl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-6-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(2-hydroxypyridin-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indazol-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[3-(3,3-dimethyl-2-oxoazetidin-1-yl)phenyl]ethynyl}-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{3-[(2-carboxy-2,2-dimethylethyl)amino]phenyl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyrazin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-3-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;3-(2-{imidazo[1,2-a]pyridin-5-yl}ethynyl)-2-(1H-pyrrol-1-yl)benzoic acid;2-(1H-pyrrol-1-yl)-3-(2-{1H-pyrrolo[2,3-b]pyridin-5-yl}ethynyl)benzoic acid;3-[2-(1-methyl-1H-indol-4-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-methyl-1H-indol-5-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1-benzothiophen-6-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-[2-(1H-indol-7-yl)ethynyl]-2-(1H-pyrrol-1-yl)benzoic acid;3-{2-[2-( ...

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Номер записи: 63
23-07-2015 дата публикации

Dye composition comprising a cationic o-alkyl-substituted meta-phenylenediamine derivative

Номер: US20150202135A1
Автор: Aziz Fadli
Принадлежит: LOreal SA

The invention relates to a meta-phenylenediamine compound of formula (I) below, the addition salts thereof with an acid and the solvates thereof: in which: R represents a hydrogen or halogen atom; a C 1 -C 4 alkyl radical; a carboxyl radical or a (C 1 -C 4 ) alkoxycarbonyl radical, R 1 represents a linear C 1 -C 10 alkyl radical substituted with a cationic radical, said alkyl radical being optionally interrupted with one or more oxygen atoms and/or with one or more NR 6 groups, said cationic radical being optionally substituted with one or more radicals chosen from C 1 -C 4 alkoxy or C 1 -C 4 (hydroxy)alkyl; R 6 represents a hydrogen atom or a linear or branched C 1 -C 4 alkyl radical; An − represents an anion or a mixture of anions which are organic or inorganic and cosmetically acceptable.

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Номер записи: 64
30-07-2015 дата публикации

Process for the Synthesis of Arformoterol

Номер: US20150210629A1
Автор: HALDAVANEKAR Vaishali Vaman, KANKAN Rajendra Narayanrao, PRABHU Mangesh, RAO Dharmaraj Ramachandra
Принадлежит:

The present invention provides a process for preparing a compound of formula (VI) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of either (1) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein Rand Rare independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo. 2. The process according to claim 1 , wherein Ris benzyl.3. The process according to claim 1 , wherein Ris benzyl or 1-phenylethyl.4. The process according to claim 1 , wherein Ris benzyl and reductive amination produces compound (II) in racemic form claim 1 , and the process further comprises resolving the racemic compound (II) with a chiral acid claim 1 , to form the corresponding acid addition salt of compound (II) claim 1 , wherein the chiral acid is preferably (S)-mandelic acid.5. The process according to claim 1 , wherein Ris 1-phenylethyl claim 1 , and compound (VIII) is (R)-phenylethylamine claim 1 , and reductive amination produces the R-enantiomer of compound (II).6. The process according to claim 1 , wherein reductive amination is carried out in the presence of a reducing agent claim 1 , wherein the reducing agent is preferably selected from the group consisting of sodium borohydride claim 1 , sodium cyano borohydride claim 1 , sodium triacetoxyborohydride claim 1 , potassium borohydride and potassium ...

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Номер записи: 65
20-07-2017 дата публикации

Method of treating cancer using selective estrogen receptor modulators

Номер: US20170202823A1
Автор: Donald P. McDonnell, Erik R. Nelson, Suzanne E. Wardell
Принадлежит: Duke University

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM.

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Номер записи: 66
18-06-2020 дата публикации

REDUNDANT POWER LINE CONTROL SYSTEMS

Номер: US20200194672A9
Автор: Bogdanovich Phillip
Принадлежит:

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture. 1. A system for controlling electronic devices located at a site , comprising: a processor; and', 'a memory coupled to the processor;', 'wherein the control apparatus is configured to couple to at least one conductor in a power line associated with an electronic device receiving power from the power line, and wherein the control apparatus is configured to redirect electrical power from the at least one conductor through the control apparatus and to the electronic device;, 'a plurality of control apparatus, wherein one or more of the control apparatus comprisewherein a first control apparatus and a second control apparatus are configured to establish a communication link to at least one electronic device located at the site, the communication link comprising at least one of a wireless communication link and a power line communication link; andwherein at least one of the first control apparatus and the second control apparatus is configured to monitor and control the at least one electronic device using the established communication link.2. The apparatus of claim 1 , wherein at least one of the first control apparatus and the second control apparatus are configured to establish a wireless communication link with a remote device.3. The apparatus of claim 2 , wherein the control apparatus having the wireless ...

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Номер записи: 67
28-07-2016 дата публикации

DIPHENYLOXYALKYLAMINE DERIVATIVES AND ARYLOXYALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITION, USE OF SAID PHARMACEUTICAL COMPOSITION FOR TREATING, PREVENTING OR INHIBITING CHRONIC PULMONARY INFLAMMATORY DISEASES AND METHOD FOR TREATING OR PREVENTING SUCH DISEASES

Номер: US20160214926A1
Автор: DA COSTA Jorge Carlos Santos, DA SILVA Emerson Teixeira, DE SOUZA Marcus Vinicius Nora, FARIA Robson Xavier, MARTINS Marco Aurelio, SERRA Magda Fraguas
Принадлежит:

The present invention relates to diphenyloxyalkylamine derivatives and aryloxyalkylamine derivatives that are structurally analogous to mexiletine, said derivatives having important biological activity and not causing the undesired side effects observed with the prototype, as well as with other drugs from the same therapeutic class as the prototype. The derivatives of the present invention have formulas II and III and are used for treating, preventing or inhibiting pulmonary inflammatory diseases, for example, asthma and chronic obstructive pulmonary disease (COPD). 3. A pharmaceutical composition comprising at least one compound as defined in claim 1 , and a pharmaceutically acceptable carrier.4. The pharmaceutical composition according to claim 3 , in a form of a tablet claim 3 , a capsule claim 3 , a powder for reconstitution claim 3 , an oral solution claim 3 , an oral suspension or an inhalation solution.5. The pharmaceutical composition according to in the form of the tablet claim 4 , the capsule or the powder for reconstitution claim 4 , which further comprises at least one agent selected from the group consisting of a disintegrant claim 4 , a glidant claim 4 , a binder claim 4 , a diluent claim 4 , a flavoring claim 4 , a colorant claim 4 , a sweetener and a lubricant.6. The pharmaceutical composition according to in the form of the oral solution claim 4 , which further comprises at least one agent selected from the group consisting of an antioxidant claim 4 , a preservative claim 4 , a pH corrector claim 4 , a flavoring claim 4 , a colorant claim 4 , a sweetener claim 4 , a solubilizer and a solvent.7. The pharmaceutical composition according to in the form of the oral suspension claim 4 , which further comprises at least one agent selected from the group consisting of a suspender claim 4 , an antioxidant claim 4 , a preservative claim 4 , a pH corrector claim 4 , a sweetener claim 4 , a flavoring claim 4 , a colorant and a solvent.8. The pharmaceutical ...

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Номер записи: 68
09-10-2014 дата публикации

BIARYL PDE4 INHIBITORS FOR TREATING INFLAMMATORY, CARDIOVASCULAR AND CNS DISORDERS

Номер: US20140301999A1
Автор: BURGIN Alex, GURNEY Mark E., HAGEN Timothy, Hategan Georgeta, KISELYOV Alexander, Motta Adalie, Sandanayaka Vincent, Schiltz Gary, Singh Jasbir
Принадлежит:

The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula I: 56-. (canceled)7. A compound or salt according to wherein Ris an optionally substituted heterocycle chosen from pyrazole claim 1 , benzodioxole claim 1 , morpholine claim 1 , thiazole claim 1 , pyridine claim 1 , pyridine N-oxide claim 1 , pyrimidine claim 1 , thiene claim 1 , oxazolidine claim 1 , isoxazole claim 1 , azetidine claim 1 , piperazine claim 1 , pyrrolidine claim 1 , imidazole claim 1 , imidazolidine claim 1 , imidazolopyridine claim 1 , pyrazine claim 1 , 1 claim 1 ,2-thiazine-1 claim 1 ,1-dioxide claim 1 , benzimidazole claim 1 , thiadiazole claim 1 , benzotriazole claim 1 , benzoxazole claim 1 , oxadiazole claim 1 , triazole claim 1 , tetrazole claim 1 , isoindole claim 1 , pyrrolopyridine claim 1 , triazolopyridine and the dihydro and tetrahydro congeners thereof.89-. (canceled)10. A compound or salt according to wherein said substituted heterocycle is substituted with a substituent chosen from halogen claim 1 , haloalkyl claim 1 , alkyl claim 1 , acyl claim 1 , alkoxyalkyl claim 1 , hydroxyalkyl claim 1 , carbonyl claim 1 , phenyl claim 1 , heteroaryl claim 1 , benzenesulfonyl claim 1 , hydroxy claim 1 , alkoxy claim 1 , haloalkoxy claim 1 , oxaalkyl claim 1 , carboxy claim 1 , alkoxycarbonyl claim 1 , alkoxycarbonylamino claim 1 , alkoxycarbonylaminoalkyl claim 1 , carboxyalkylcarbonylamino claim 1 , carboxamido claim 1 , aminocarbonyloxy claim 1 , alkylaminocarbonyl claim 1 , dialkylaminocarbonyl claim 1 , aminocarbonylalkyl claim 1 , cyano claim 1 , acetoxy claim 1 , nitro claim 1 , amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , aminoalkyl claim 1 , (alkyl)(aryl)aminoalkyl claim 1 , alkylaminoalkyl claim 1 , dialkylaminoalkyl claim 1 , ...

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Номер записи: 69
04-07-2019 дата публикации

BIARYL COMPOUNDS AS ANTIMICROBIAL AND CHEMOTHERAPEUTIC AGENTS

Номер: US20190202774A1
Автор: CANNON Carolyn L, GAO HONGYIN, Kürti László, SHAH Kush, Shah Parth
Принадлежит:

In one aspect, the present disclosure provides diaryl compounds of the formula presented herein. The application also provides compositions and methods of treatment thereof. In some embodiments, these compounds are used in the treatment of bacterial infections or in the treatment of cancer. 12125-. (canceled)127. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) a compound of ; and'}(b) a pharmaceutically acceptable carrier.128133-. (canceled)135. The pharmaceutical composition of claim 134 , wherein M is a monovalent cation.136. (canceled)137. (canceled)138. The pharmaceutical composition of claim 134 , wherein R claim 134 , R claim 134 , R claim 134 , and Rare all chloro.139. The pharmaceutical composition of claim 134 , wherein R claim 134 , R claim 134 , R claim 134 , and Rare all bromo.141146-. (canceled)147. A method of treating a disease or disorder in a patient comprising administering to the patient in need thereof a therapeutically effective amount of a compound or composition of .148180-. (canceled) This application claims the benefit of U.S. Provisional Application No. 62/255,254 filed on Nov. 13, 2015, the entirety of which is hereby incorporated by reference.This disclosure relates to the fields of medicine, pharmacology, chemistry, antimicrobial activity, and oncology. In particular, new compounds, compositions, and methods of treatment comprising a biaryl core are disclosed.Infectious diseases are currently the second leading cause of death worldwide and the third leading cause of death in economically advanced countries despite the development of antibiotics (Nathan, 2004). Furthermore, the threatening emergence of bacterial resistance (US Department of Health and Human Services, Center of Disease Control and Prevention, 2013, www.cdc.gov/drugresistance/threat-report-2013/pdf/ar-threats-2013-508.pdf.) to many antibiotics presents a serious challenge for their clinical use. According to the 2013 estimates ...

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Номер записи: 70
27-08-2015 дата публикации

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

Номер: US20150239836A1
Автор: Gall Anna, Hong Feng, JR. Thomas L., Kuksa Vladimir A., Little, Orme Mark W., Scott Ian L.
Принадлежит:

The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. 119-. (canceled)21. The compound of claim 20 , or tautomer claim 20 , stereoisomer claim 20 , geometric isomer or a pharmaceutically acceptable solvate claim 20 , hydrate claim 20 , salt claim 20 , N-oxide or prodrug thereof claim 20 , wherein n is 0 and each Rand Ris hydrogen.22. The compound of claim 21 , or tautomer claim 21 , stereoisomer claim 21 , geometric isomer or a pharmaceutically acceptable solvate claim 21 , hydrate claim 21 , salt claim 21 , N-oxide or prodrug thereof claim 21 , wherein each R claim 21 , R claim 21 , Rand Ris hydrogen.23. The compound of claim 22 , or tautomer claim 22 , stereoisomer claim 22 , geometric isomer or a pharmaceutically acceptable solvate claim 22 , hydrate claim 22 , salt claim 22 , N-oxide or prodrug thereof claim 22 , wherein claim 22 ,{'sup': 31', '32, 'sub': 1', '5, 'Rand Rare each independently hydrogen, or C-Calkyl;'}{'sup': 16', '17, 'Rand R, together with the carbon atom to which they are attached, form a carbocyclyl; and'}{'sup': '18', 'Ris hydrogen, hydroxy, or alkoxy.'}24. The compound of claim 23 , or tautomer claim 23 , stereoisomer claim 23 , geometric isomer or a pharmaceutically acceptable solvate claim 23 , hydrate claim 23 , salt claim 23 , N-oxide or prodrug thereof claim 23 , wherein Rand R claim 23 , together with the carbon atom to which they are attached form cyclopentyl claim 23 , cyclohexyl or cycloheptyl and Ris hydrogen or hydroxy.25. The compound of claim 22 , or tautomer claim 22 , stereoisomer claim 22 , geometric isomer or a pharmaceutically ...

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Номер записи: 71
23-07-2020 дата публикации

NOVEL DEUTERIUM SUBSTITUTED POSITRON EMISSION TOMOGRAPHY (PET) IMAGING AGENTS AND THEIR PHARMACOLOGICAL APPLICATION

Номер: US20200230263A1
Автор: CHOI Seok Rye, Kung Hank F., LIU Futao, PLOESSL Karl, WU Zehui, ZHA Zhihao
Принадлежит: Five Eleven Pharma Inc.

The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof. 19-. (canceled)12. The compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein:{'sup': '2', 'Ris methyl and is optionally substituted with one or more deuterium atoms; and'}m is 3.13. The compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein Ris CD.14. The compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein Y is —[OCDCD]-.16. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ais N and X is F.17. The compound of claim 15 , or a pharmaceutically acceptable salt thereof claim 15 , wherein Ais CH and X is F.1834-. (canceled)35. The compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , wherein the deuterium enrichment for each designated deuterium atom is at least about 50% claim 10 , preferably at least about 80% claim 10 , more preferably at least about 90% claim 10 , and most preferably at least about 95%.36. A pharmaceutical composition comprising the compound of claim 10 , or a pharmaceutically acceptable salt thereof claim 10 , and a pharmaceutically acceptable carrier.37. A method for imaging a subject claim 10 , comprising{'claim-ref': {'@idref': 'CLM-00010', 'claim 10'}, 'administering the compound of or a pharmaceutically acceptable salt thereof to said subject; and'}obtaining an image of said subject or a portion of said subject. ...

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Номер записи: 72
13-11-2014 дата публикации

LIQUID CRYSTALLINE COMPOUND AND ELECTROLYTE MATERIAL

Номер: US20140336414A1
Автор: Kato Takashi, Soberats Bartolome, Yoshio Masafumi
Принадлежит: JAPAN SCIENCE AND TECHNOLOGY AGENCY

A liquid crystalline compound and an electrolyte material in which the conductivity switches between ion conductivity and non-ion conductivity depending on changes in temperature, and thus a switching function can be obtained are proposed. The liquid crystalline compound has a columnar liquid crystal phase in which an ammonium group is linked with an alkoxyphenyl group. A structural change thereof occurs depending on changes in temperature, and the conductivity switches between ion-conducting and non-ion-conducting, and thus the switching function can be obtained. 2. The liquid crystalline compound according to claim 1 , wherein a phase transition of liquid crystalline phases occurs from a rectangular columnar phase which is non-ion-conductive to a hexagonal columnar phase which is ion-conductive by heating.3. The liquid crystalline compound according to claim 1 , wherein a phase transition of liquid crystalline phases occurs from a hexagonal columnar phase which is ion-conductive to a rectangular columnar phase which is non-ion- conductive by lowering the temperature.4. The liquid crystalline compound according to claim 2 , wherein{'sup': −4', '−1, 'an ionic conductivity reaches 10Scmor more during the hexagonal columnar phase, and'}{'sup': −8', '−1, 'an ionic conductivity reaches 10Scmor less during the rectangular columnar phase.'}5. An electrolyte material comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the liquid crystalline compound according to ,'}wherein a phase transition of liquid crystalline phases of the liquid crystalline compound occurs depending on a change in temperature and a conductivity switches from ion-conducting to non-ion-conducting or from non-ion-conducting to ion-conducting.6. The liquid crystalline compound according to claim 3 , wherein{'sup': −4', '−1, 'an ionic conductivity reaches 10Scmor more during the hexagonal columnar phase, and'}{'sup': −8', '−1, 'an ionic conductivity reaches 10Scmor less during the rectangular ...

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Номер записи: 73
08-08-2019 дата публикации

METHOD FOR PRODUCING N-METHYL-PARA-ANISIDINE

Номер: US20190241500A1
Автор: BELYAKOV Nikolay Grigorievich, FROLOV Alexandr Yurievich
Принадлежит: IFOTOP Limited Liability Company

The invention relates to chemical engineering processes, and more particularly to liquid-phase catalytic methods for producing, in the presence of hydrogen, alkylated para-anisidine for use as a chemical substance or as a gasoline additive for increasing the octane rating of a gasoline. The technical result of the claimed group of inventions is an increase in the yield of N-methyl-para-anisidine and a decrease in the yield of a dimethyl derivative. A method for producing N-methyl-para-anisidine in a liquid phase includes alkylating para-anisidine with formalin as they are separately, simultaneously fed into a mixer disposed in a reactor, directly upstream of a catalytic reduction zone, thus producing an intermediate azomethine, and subsequently reducing same on a hydrogenation catalyst at a temperature of 20-120° C. in an environment of hydrogen at elevated pressure, and then isolating the target product, N-methyl-para-anisidine. 1: A method for producing N-methyl-para-anisidine in a liquid phase , comprising alkylating para-anisidine with formalin as they are separately , simultaneously fed into a mixer disposed in a reactor , directly upstream of a catalytic reduction zone , thus producing an intermediate azomethine-4-methoxy-(N-phenylmethanimine) , and subsequently reducing said intermediate on a hydrogenation catalyst at a temperature of 20-120° C. , in an environment of hydrogen at elevated pressure , and then separating the target product , N-methyl-para-anisidine , wherein para-anisidine is used in the form of a solution in a solvent selected from the group: ethanol , methanol , isopropanol.2: The method according to claim 1 , wherein the alkylation is carried out in a batch mode.3: The method according to claim 1 , wherein the alkylation is carried out on in a continuous mode.4. (canceled)5: The method according to claim 1 , wherein stabilizers are used during the alkylation in the form of tertiary aliphatic amines claim 1 , wherein said stabilizers are used ...

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Номер записи: 74
27-11-2014 дата публикации

ANILINE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION

Номер: US20140350019A1
Автор: Feutrill John, Leriche Caroline, Middlemiss David
Принадлежит: FOVEA PHARMACEUTICALS

The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C-C)alkyl or a CN; R1b represents H, an halogen or a (C-C)alkyl; R1c represents H or a (C-C)alkyl; R2 represents H, an halogen, an OH, an O—(C-C)alkyl or (C-C)alkyl; R3 represents H, an halogen, a (C-C)alkyl, an OH, an O—(C-C)alkyl, a CONHor CN; R4 represents H, an halogen or a (C-C)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C-C)alkyl, or one of its enantiomers. 2. The compound according to claim 1 , in which compounds of formula (I) are not:2-[2,4-difluoro-3-[[2-fluoro-3-(3-fluorophenyl)phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[3-(3-fluorophenyl)-2-methyl-phenyl]methylamino]phenoxy]acetic acid;2-[2-fluoro-3-[[2-fluoro-5-(3-fluoro-5-(3-fluorophenyl)phenyl]methylamino]phenoxy]acetic acid;2-[4-fluoro-3-[[2-fluoro-5-(3-fluorophenyl)phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[5-(3-fluorophenyl)-2-methoxy-phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[5-(3-fluorophenyl)-2-hydroxy-phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[3-(3-fluorophenyl)-2,5-dimethyl-phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[5-fluoro-3-(3-fluorophenyl)-2-methylphenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[2-fluoro-3-(3-fluorophenyl)-6-hydroxy-phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[2-fluoro-3-(3-fluorophenyl)-6-methoxy-phenyl]methylamino]phenoxy]acetic acid;2-[2,4-difluoro-3-[[3-(3-fluorophenyl)-5-isopropyl-phenyl]methylamino]phenoxy]acetic acid;2-[3-[[3-ethyl-5-(3-fluorophenyl)phenyl]methylamino]-2,4-difluoro-phenoxy]acetic acid;2-[2-ethyl-4-fluoro-3-[[2-fluoro-5-(3-fluorophenyl)phenyl]methylamino]phenoxy]acetic acid;2-[4-fluoro-3-[[2-fluoro-5-(3-fluorophenyl)phenyl]methylamino]-2-isopropyl-phenoxy]acetic acid;2-[2,4-difluoro-3-[[2-fluoro-5 ...

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Номер записи: 75
04-12-2014 дата публикации

DYE COMPOSITION COMPRISING A CATIONIC PARA-AMINOPHENOL OXIDATION BASE

Номер: US20140352081A1
Автор: Fadli Aziz
Принадлежит: L'OREAL

The present invention relates to a para-aminophenol compound of formula (I) the addition salts thereof with an acid and the solvates thereof, dye composition comprising the latter and a dyeing process. 113-. (canceled)15. The compound according to claim 14 , wherein R1 is a saturated claim 14 , linear or branched C-Calkyl radical claim 14 , which is interrupted by at least one oxygen atom and/or by at least one group NR2 claim 14 , and/or substituted with at least one radical chosen from hydroxyl claim 14 , alkoxy or C-Chydroxyalkyl radicals; or a saturated claim 14 , unsaturated or aromatic cationic 5- to 8-membered heterocycle substituted with at least one radical chosen from C-Calkyl claim 14 , hydroxyl claim 14 , C-Calkoxy claim 14 , amino claim 14 , (C-C)alkylamino claim 14 , di(C-C)alkylamino claim 14 , thio claim 14 , (C-C)alkylthio claim 14 , carboxyl claim 14 , (C-C)alkylcarbonyl claim 14 , sulfonyl claim 14 , amido or C-Chydroxyalkyl radicals.16. The compound according to claim 14 , wherein when Z1 is R2 claim 14 , then R1 and R2 form claim 14 , together with the nitrogen atom to which they are attached claim 14 , a saturated or unsaturated cationic 5- to 8-membered heterocycle substituted with at least one radical chosen from C-Calkyl radicals and hydroxyl claim 14 , C-Calkoxy claim 14 , amino claim 14 , (C-C)alkylamino claim 14 , di(C-C)alkylamino claim 14 , thio claim 14 , (C-C)alkylthio claim 14 , carboxyl claim 14 , (C-C)alkylcarbonyl claim 14 , sulfonyl claim 14 , amido and C-Chydroxyalkyl radicals claim 14 , wherein the heterocycle includes at least one heteroatom chosen from N or O; or a saturated or unsaturated noncationic 5-to 8-membered heterocycle substituted with at least one radical chosen from C-Calkyl radicals and hydroxyl claim 14 , C-Calkoxy claim 14 , amino claim 14 , (C-C)alkylamino claim 14 , di(C-C)alkylamino claim 14 , thio claim 14 , (C-C)alkylthio claim 14 , carboxyl claim 14 , (C-C)alkylcarbonyl claim 14 , sulfonyl claim 14 , ...

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Номер записи: 76
01-10-2015 дата публикации

METHOD OF TREATING CANCER USING SELECTIVE ESTROGEN RECEPTOR MODULATORS

Номер: US20150274640A1
Автор: McDonnell Donald P., Nelson Erik R., Wardell Suzanne E.
Принадлежит:

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM. 1. A method of treating breast cancer brain metastasis in a subject , the method comprising administering a compound of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5 ,6 ,7 ,8-tetrahydronaphthalen-2-ol , wherein the breast cancer brain metastasis is resistant to an estrogen receptor modulator.2. The method of claim 1 , wherein an effective amount of the compound is administered.3. The method of claim 2 , wherein the effective amount comprises a high dosage.4. The method of claim 3 , wherein the high dosage is more than about 20 mg/kg.5. The method of claim 3 , wherein the high dosage is about 20 mg/kg to about 100 mg/kg.6. The method of claim 1 , wherein the compound is administered by oral administration claim 1 , intravenous administration claim 1 , intradermal injection claim 1 , intramuscular injection or subcutaneous injection.7. The method of claim 1 , further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor) claim 1 , an antiestrogen claim 1 , a ligand of retinoic acid or retinoxic X receptor claim 1 , an antiprogestin claim 1 , an antiandrogen claim 1 , vitamin D or metabolite thereof claim 1 , a farnesyl transferase inhibitor claim 1 , a PPARα or gamma agonist and a MAP kinase inhibitor.8. The method of claim 1 , wherein the breast cancer brain metastasis is de novo resistant to the estrogen receptor modulator.9. The method of claim 1 , wherein the resistance to the estrogen receptor modulator is acquired.10. The method of claim 1 , wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM ...

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Номер записи: 77
13-08-2020 дата публикации

New method for the synthesis of unsymmetrical tertiary amines

Номер: US20200255369A1
Автор: Christophe BOUR, Marie Jenny Jacqueline VAYER, Vincent Gandon
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite Paris Saclay

Disclosed is a new method for the synthesis of unsymmetrical tertiary amines using alcohol and an imine, and to new tertiary amines.

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Номер записи: 78
29-09-2016 дата публикации

Block copolymer

Номер: US20160280832A1
Автор: Eun Young Choi, Je Gwon Lee, Jeong Kyu Lee, Jung Keun Kim, Mi Sook Lee, No Jin Park, Se Jin Ku, Sung Joon Oh, Sung Soo Yoon
Принадлежит: LG Chem Ltd

The present application provides the block copolymers and their application. The present application may provide the block copolymers that have excellent self assembling and phase separation properties and therefore that can be effectively used in various applications. The present application may also provide applications of the block copolymers.

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Номер записи: 79
29-09-2016 дата публикации

Block copolymer

Номер: US20160280835A1
Автор: Je Gwon Lee, Jeong Kyu Lee, Jung Keun Kim, Sung Joon Oh, Sung Soo Yoon, Yeon Joo Kang
Принадлежит: LG Chem Ltd

The present application provides the block copolymers and their application. The present application may provide the block copolymers that have excellent self assembling and phase separation properties and therefore that can be effectively used in various applications. The present application may also provide applications of the block copolymers.

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Номер записи: 80
08-10-2015 дата публикации

N-MONOMETHYL-SUBSTITUTED ANILINES AS COMPONENTS INCREASING THE OXIDATIVE RESISTANCE OF PETROL

Номер: US20150284650A1
Автор: Frolov Alexander Yurievich, Ivanov Yuriy Alexandrovich
Принадлежит: ZAKRITOYE AKTSIONERNOE OBSHESTVO

The invention relates to application of N-monomethyl-4-methoxyaniline, N-monomethyl-4-ethoxyaniline and N-monomethyl aniline and their mixtures as oxidation-preventive additives for engine fuel. This invention may be used to improve their performance parameters. It also relates to fuel compositions containing the above-mentioned chemical compounds. 1. Application of N-monomethyl-4-methoxyaniline and/or N-monomethyl-4-ethoxyaniline as a component for petroleum prevention against oxidation.2. Fuel composition containing substances according to as an oxidation-preventive agent in amount 0.001-3 wt. %.3. Fuel composition containing substances according to and/or N-monomethyl aniline as an oxidation-preventive agent in amount 0.001-3 wt. %. The invention relates to the field of chemistry and chemical technology connected with application of chemical compounds as additives that prevent oxidation of the matters being stabilized by them. Invention may be used for engine fuel stabilization.The invention relates to chemistry, namely to oxidation-preventive additives to petrol brands; it may be used to improve their performance parameters.Hydrocarbon fuels produced mainly from oil and gas are subjected to oxidation by known, classic oxidation mechanism inherent to most hydrocarbon compounds, which comprise engine fuels, with certain kinetics of the oxidation process [clauses 1-7 of the List of references]. Hydroperoxides are initial oxidation products; they have low stability and are exposed to further transformations by different directions depending on the hydrocarbon being oxidized and oxidation conditions. At the same time, oxidation rate of hydrocarbons depends upon their molecular weight and structure.Moreover, the higher molecular weight of the hydrocarbon, the higher it oxidation rate.During oxidation of petrol brands, which are the mixture of hydrocarbons from different classes with different molecular weight, primary oxidation products may react among themselves. ...

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Номер записи: 81
12-10-2017 дата публикации

2,2' -DIAMINOBIARYLS HAVING ONE PRIMARY AND ONE SECONDARY AMINE

Номер: US20170291871A1
Автор: DYBALLA Katrin Marie, ELSLER Bernd, ENDERS Mathias, Franke Robert, Fridag Dirk, WALDVOGEL Siegfried R.
Принадлежит: EVONIK DEGUSSA GmbH

Novel 2,2′-diaminobiaryls having one primary and one secondary amine and an electrochemical process for preparation thereof. 2. Compound according to claim 1 ,{'sup': '1', 'where Xis selected fromtert-butyloxycarbonyl, methyloxycarbonyl, benzyloxycarbonyl, phenyloxycarbonyl, acetyl, trifluoroacetyl, benzoyl.3. Compound according to claim 1 ,{'sup': '2', 'where Xis selected fromtert-butyloxycarbonyl, methyloxycarbonyl, phenyloxycarbonyl, acetyl, trifluoroacetyl, benzoyl.4. Compound according to claim 1 ,{'sup': '2′', 'where X is selected fromtert-butyloxycarbonyl, methyloxycarbonyl, phenyloxycarbonyl, acetyl, trifluoroacetyl, benzoyl.5. Compound according to claim 1 ,{'sup': '3', 'where Xis selected fromtert-butyloxycarbonyl, methyloxycarbonyl, phenyloxycarbonyl, acetyl, trifluoroacetyl, benzoyl.6. Compound according to claim 1 ,{'sup': 1', '2', '3', '4', '1′', '2′', '3′, 'where R, R, R, R, R, R, R are selected from{'sub': 1', '12', '1', '12', '6', '20, '—H, —(C-C)-alkyl, —O—(C-C)-alkyl, —O—(C-C)-aryl, —S-alkyl, —S-aryl, halogen.'}7. Compound according to claim 1 ,{'sup': 5′', '6′', '7′', '8′', '9′', '10′, 'where R, R, R, R, R, R are selected from{'sub': 1', '12', '1', '12', '6', '20, '—H, —(C-C)-alkyl, —O—(C-C)-alkyl, —O—(C-C)-aryl, —S-alkyl, —S-aryl, halogen.'}8. Compound according to claim 1 ,{'sup': 5', '6', '7', '8', '9', '10, 'where R, R, R, R, R, Rare selected from{'sub': 1', '12', '1', '12', '6', '20, '—H, —(C-C)-alkyl, —O—(C-C)-alkyl, —O—(C-C)-aryl, —S-alkyl, —S-aryl, halogen.'}9. Compound according to claim 1 ,where the compound has the general structure (I).10. Compound according to claim 1 ,where the compound has the general structure (IIa) or (IIb).11. Compound according to claim 1 ,where the compound has the general structure (III). The invention relates to novel 2,2′-diaminobiaryls having one primary and one secondary amine and an electrochemical process for preparation thereof.The direct selective electrochemical C,C cross-coupling of differently ...

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Номер записи: 82
20-10-2016 дата публикации

MONOMER AND BLOCK COPOLYMER

Номер: US20160304653A1
Автор: Kim Jung Keun, Lee Je Gwon, Park No Jin, Yoon Sung Soo
Принадлежит: LG CHEM, LTD.

The present application relates to monomers, methods for preparing block copolymers, block copolymers and their applications. The monomers may form a block copolymer which has an excellent self assembling property and phase separation and to which various required functions can be freely applied as necessary. 2. The monomer according to claim 1 , wherein the R is hydrogen or an alkyl group having 1 to 4 carbon atoms.3. The monomer according to claim 1 , wherein the X is a single bond claim 1 , an oxygen atom claim 1 , —C(═O)—O— or —O—C(═O)—.4. The monomer according to claim 1 , wherein the X is —C(═O)—O—.5. The monomer according to claim 1 , wherein the chain comprises 8 to 20 chain-forming atoms.6. The monomer according to claim 1 , wherein the chain-forming atom is a carbon claim 1 , an oxygen claim 1 , a nitrogen or a sulfur.7. The monomer according to claim 1 , wherein the chain-forming atom is a carbon or an oxygen.8. The monomer according to claim 1 , wherein the chain is a linear hydrocarbon chain.9. The monomer according to claim 1 , wherein the cyclic structure is an aromatic structure and a alicyclic structure.10. The monomer according to claim 7 , wherein the chain of the Y is directly linked to the cyclic structure or is linked to the cyclic structure via a linker.11. The monomer according to claim 10 , wherein the linker is an oxygen atom claim 10 , a sulfur atom claim 10 , —NR— claim 10 , —S(═O)— claim 10 , an alkylene group claim 10 , an alkenylene group or an alkynylene group claim 10 , where the Ris hydrogen claim 10 , an alkyl group claim 10 , an alkenyl group claim 10 , an alkynyl group claim 10 , an alkoxy group or an aryl group.12. The monomer according to claim 10 , wherein the linker is an oxygen atom or —NR— claim 10 , where the Ris hydrogen claim 10 , an alkyl group claim 10 , an alkenyl group claim 10 , an alkynyl group claim 10 , an alkoxy group or an aryl group.13. The monomer according to claim 1 , the Y is represented by Formula 2 below ...

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Номер записи: 83
29-10-2015 дата публикации

HOLE-TRANSPORTING MATERIAL FOR INORGANIC/ORGANIC HYBRID PEROVSKITE SOLAR CELLS

Номер: US20150311440A1
Автор: JANGWON SEO, JEON Nam Joong, LEE HAK GUEN, LEE Jaemin, SEOK SANG II
Принадлежит:

Provided is a hole-transporting compound having a novel structure, and more particularly, a hole-transporting compound for an inorganic/organic hybrid perovskite solar cell. An inorganic/organic hybrid perovskite-based solar cell using the hole-transporting compound according to the present invention has significantly high power generation efficiency. 2. The hole-transporting compound of claim 1 , wherein Zto Zand Zto Zare each independently O or S; and{'sub': 1', '4', '11', '14, 'Rto Rand Rto Rare each independently (C1-C3)alkyl.'}3. The hole-transporting compound of claim 2 , wherein Zto Zare O; and{'sub': 1', '4, 'Rto Rare each independently (C1-C3)alkyl.'}6. The solar cell of claim 5 , wherein the hole transporting layer further contains a phthalocyanine derivative.8. The solar cell of claim 7 , wherein the phthalocyanine derivative is contained at a content of 0.1 to 15 parts by weight based on 100 parts by weight of the hole-transporting compound for an inorganic/organic hybrid perovskite solar cell.9. The solar cell of claim 5 , wherein it includes: a first electrode; a composite layer positioned on the first electrode and impregnated with a light harvester; a overlayer of light harvester positioned on the composite layer and made of the light harvester; the hole transporting layer positioned on the overlayer of light harvester; and a second electrode positioned on the hole transporting layer. This application claims priority under 35 U.S.C. §119 to Korean Patent Application No. 10-2014-0050995 filed on Apr. 28, 2014 and Korean Patent Application No. 10-2015-0057688 filed on Apr. 24, 2015 in the Korean Intellectual Property Office, the disclosure of which is incorporated herein by reference in its entirety.The following disclosure relates to a hole-transporting compound, and more particularly, to a hole-transporting compound having a novel structure, capable of being used in an inorganic/organic hybrid perovskite solar cell.In order to solve depletion of ...

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Номер записи: 84
27-10-2016 дата публикации

METHOD FOR DYEING KERATINOUS SUBSTANCES STARTING FROM COLOURED OLIGOMERS AND/OR POLYMERS RESULTING FROM META-PHENYLENEDIAMINES, COMPOSITION AND DYEING AGENT

Номер: US20160310383A1
Автор: Leduc Madeleine, Sabelle Stephane
Принадлежит:

A subject-matter of the invention is a) a method for dyeing keratinous substances starting from a dyeing agent chosen from coloured oligomers and polymers obtained from the polycondensation of i) meta-phenylenediamine (MPD) couplers in the presence of ii) one or more ingredients chosen from radical initiators and/or chemical oxidizing agents, b) a composition comprising one or more coloured oligomers and/or one or more coloured polymers as defined above and c) a coloured oligomeric or polymeric dyeing agent obtained by reaction between i) and ii) as defined above, and the use of the coloured oligomer(s) or polymer(s) for dyeing keratinous substances. The dyeing method and the composition according to the invention make it possible in particular to obtain a long-lasting colouration on keratinous fibres which is vivid, chromatic and/or homogeneous. 116.-. (canceled)17. A method for dyeing a keratinous substance , the method comprising:applying to the keratinous substances at least one dyeing agent obtained from the polycondensation between i) at least two meta-phenylenediamine couplers which react with one another in the presence of ii) at least one ingredient chosen from radical initiators and chemical oxidizing agents.20. The method according to claim 19 , wherein the couplers are chosen from those of formula (Ia) in which:{'sub': 1', '1', '6', '1', '6, 'Ris chosen from a hydrogen atom or a group chosen from (C-C)alkyl or (C-C)alkoxy optionally substituted by a hydroxyl group;'}{'sub': 2', '3', '1', '6', '1', '4', '3, 'Rand R, which are identical or different, are chosen from i) a hydrogen atom; ii) a (C-C)alkyl group optionally substituted by a group chosen from hydroxyl or guanidino; or iii) a (C-C)alkylcarbonyl group or acetyl CH—C(O)—;'}{'sub': 2', '3, 'or Rand Rform, together with the nitrogen atom which carries them, a saturated heterocycle chosen from pyrrolidino, piperidino, or morpholino;'}{'sub': '4', 'Rrepresents a hydrogen atom;'}{'sub': 5', '1', '6', '1 ...

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Номер записи: 85
27-10-2016 дата публикации

Block copolymer

Номер: US20160311960A1
Автор: Eun Young Choi, Je Gwon Lee, Jung Keun Kim, Mi Sook Lee, No Jin Park, Se Jin Ku, Sung Soo Yoon
Принадлежит: LG Chem Ltd

The present application provides the block copolymers and their application. The block copolymer has an excellent self assembling property and phase separation and various required functions can be freely applied thereto as necessary.

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Номер записи: 86
26-10-2017 дата публикации

2,2' -DIAMINOBIARYLS HAVING A PHTHALOYL GROUP OR SUCCINOYL GROUP

Номер: US20170305846A1
Автор: DYBALLA Katrin Marie, ELSLER Bernd, ENDERS Mathias, Franke Robert, Fridag Dirk, WALDVOGEL Siegfried R.
Принадлежит: EVONIK DEGUSSA GmbH

Novel 2,2′-diaminobiaryls having two secondary amines and an electrochemical process for preparation thereof. 8. Compound according to claim 1 ,{'sup': 1', '2', '3', '4', '1', '2', '3', '4, 'where R, R, R, R, R′, R′, R′, R′ are selected from{'sub': 1', '12', '1', '12', '6', '20, '—H, —(C-C)-alkyl, —O—(C-C)-alkyl, —O—(C-C)-aryl, —S-alkyl, —S-aryl, halogen.'}9. Compound according to claim 1 ,{'sup': 5', '6', '7', '8', '9', '10', '5', '6', '7', '8', '9', '10, 'where R′, R′, R′, R′, R′, R′, R, R, R, R, R, Rare selected from{'sub': 1', '12', '1', '12', '6', '20, '—H, —(C-C)-alkyl, —O—(C-C)-alkyl, —O—(C-C)-aryl, —S-alkyl, —S-aryl, halogen.'}10. Compound according to claim 1 ,{'sup': 1', '2', '3', '4, 'where X, X, X, Xare selected fromtert-butyloxycarbonyl, methyloxycarbonyl, benzyloxycarbonyl, phenyloxycarbonyl, acetyl, trifluoroacetyl, benzoyl, sulphonyl, sulphenyl.11. Compound according to claim 1 ,wherein the compound has the general structure (Ia) or (Ib).12. Compound according to claim 1 ,wherein the compound has the general structure (IIa), (IIb) or (IIc).13. Compound according to claim 1 ,wherein the compound has the general structure (IIIa) or (IIIb). The invention relates to novel 2,2′-diaminobiaryls having two secondary amines and to an electrochemical process for preparation thereof.The direct electrochemical C,C cross-coupling of differently protected aminoaryls is unknown to date. Although it is possible to prepare unsymmetric 2,2′-diaminobiaryls by a copper-catalysed C,C coupling, these are either unprotected (M. Smrcina, S. Vyskocil, B. Maca, M. Polasek, T. A. Claxton, A. P. Abbott, P. Kocovsky, J. Org. Chem. 1994, 59, 2156-2163) or both amino groups bear the same protecting group (J.-F. Cui, H. Huang, H. Wong, Synlett 2011, 7, 1018-1022. and W. Kalk, H.-S. Bien, K.-H. Schündehütle, Justus Liebigs Ann. Chem. 1977, 329-337.).There is likewise knowledge only of the synthesis of symmetrically protected 2,2′-diaminobiaryls having the same protecting group by an ...

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Номер записи: 87
17-09-2020 дата публикации

CONTROLLING ZONES OF ELECTRONIC DEVICES ASSOCIATED WITH POWER LINES

Номер: US20200295262A9
Автор: Bogdanovich Phillip
Принадлежит:

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture.

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Номер записи: 88
03-11-2016 дата публикации

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Номер: US20160318931A1
Автор: Grootenhuis Peter, Hadida-Ruah Sara, Hazlewood Anna, McCartney Jason, Singh Ashvani, Van Goor Fredrick, Zhou Jinglan
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. 313-. (canceled)1618-. (canceled)20. (canceled)2231-. (canceled)3739-. (canceled)4142-. (canceled)4445-. (canceled)49. (canceled)5155-. (canceled)5762-. (canceled)6467-. (canceled)68. A pharmaceutical composition comprising a compound of formula I according to and a pharmaceutically acceptable carrier or adjuvant.69. The composition according to claim 68 , wherein said composition comprises an additional agent selected from a mucolytic agent claim 68 , bronchodialator claim 68 , an anti-biotic claim 68 , an anti-infective agent claim 68 , an anti-inflammatory agent claim 68 , CFTR modulator claim 68 , or a nutritional agent.70. A method of modulating ABC transporter activity comprising the step of contacting said ABC transporter with a compound of formula I according to .7172-. (canceled)73. A kit for use in measuring the activity of a ABC transporter or a fragment thereof in a biological sample in vitro or in vivo claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) a composition comprising a compound of formula I according to ;'} a) contacting the composition with the biological sample;', 'b) measuring activity of said ABC transporter or a fragment thereof., '(ii) instructions for7475-. (canceled) The present application claims priority under 35 U.S.C. §119 to U.S. Provisional Application No. 60/582,676, filed Jun. 24, 2004 and entitled “MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS”, U.S. Provisional Application No. 60/630,127, filed Nov. 22, 2004 and entitled “MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS”, U.S. Provisional Application No. 60/635,674, filed Dec. 13, 2004 and entitled “MODULATORS OF ATP- ...

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Номер записи: 89
01-10-2020 дата публикации

AROMATIC AMINE DERIVATIVE, AND ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME

Номер: US20200313090A1
Автор: Fujiyama Takahiro, Kato Tomoki, Sado Takayasu
Принадлежит: IDEMITSU KOSAN CO., LTD.

An aromatic amine derivative represented by formula (1): 1. (canceled)3. The aromatic amine derivative according to claim 2 , wherein R claim 2 , Rand Rin formula (1) each independently represents a hydrogen atom claim 2 , a methyl group claim 2 , an ethyl group claim 2 , a n-propyl group claim 2 , an isopropyl group claim 2 , a n-butyl group claim 2 , an isobutyl group claim 2 , a s-butyl group claim 2 , or a t-butyl group.4. The aromatic amine derivative according to claim 2 , wherein Rin formula (30) represents a hydrogen atom claim 2 , a phenyl group or a biphenylyl group.5. The aromatic amine derivative according to claim 2 , wherein Rin formula (7-2) represents a hydrogen atom claim 2 , a phenyl group or a naphthyl group.6. The aromatic amine derivative according to claim 2 , wherein R′ claim 2 , Rand Rin formula (1) represent hydrogen atoms.7. The aromatic amine derivative according to claim 2 , wherein Rin formula (16) represents a hydrogen atom.8. The aromatic amine derivative according to claim 2 , wherein Rin formula (30) represents a hydrogen atom.9. The aromatic amine derivative according to claim 2 , wherein Rin formula (7-2) represents a hydrogen atom.10. The aromatic amine derivative according to claim 2 , wherein R claim 2 , Rand Rin formula (1) claim 2 , Rin formula (16) claim 2 , Rin formula (30) claim 2 , and Rin formula (7-2) represent hydrogen atoms.12. An organic electroluminescence device comprising an anode claim 2 , a cathode claim 2 , and at least one organic thin film layer disposed between the anode and the cathode claim 2 , wherein:the at least one organic thin film layer comprises a light emitting layer; and{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'at least one organic thin film layer comprises the aromatic amine derivative according to .'}13. The organic electroluminescence device according to claim 12 , wherein:the at least one organic thin film layer comprises a hole injecting layer or a hole transporting layer; andthe hole ...

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Номер записи: 90
08-10-2020 дата публикации

AROMATIC AMINE DERIVATIVE, AND ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME

Номер: US20200321526A1
Автор: Fujiyama Takahiro, Kato Tomoki, Sado Takayasu
Принадлежит: IDEMITSU KOSAN CO., LTD

An aromatic amine derivative represented by formula (1): 1. (canceled)3. The aromatic amine derivative according to claim 2 , wherein two Rrepresent methyl groups.4. The aromatic amine derivative according to claim 2 , wherein one of two Rrepresents a methyl group and the other represents a phenyl group.5. The aromatic amine derivative according to claim 2 , wherein two Rrepresent phenyl groups.7. The aromatic amine derivative according to claim 2 , wherein R claim 2 , Rand Rin formula (1) each independently represents a hydrogen atom claim 2 , a methyl group claim 2 , an ethyl group claim 2 , a n-propyl group claim 2 , an isopropyl group claim 2 , a n-butyl group claim 2 , an isobutyl group claim 2 , a s-butyl group claim 2 , or a t-butyl group.8. The aromatic amine derivative according to claim 2 , wherein Rin formula (30) represents a hydrogen atom or a phenyl group.9. The aromatic amine derivative according to claim 2 , wherein Rin formula (7) represents a hydrogen atom claim 2 , a methyl group claim 2 , a t-butyl group claim 2 , or a phenyl group.10. The aromatic amine derivative according to claim 2 , wherein R claim 2 , Rand Rin formula (1) represent hydrogen atoms.11. The aromatic amine derivative according to claim 2 , wherein Rin formula (16) represents a hydrogen atom.12. The aromatic amine derivative according to claim 2 , wherein Rin formula (30) represents a hydrogen atom.13. The aromatic amine derivative according to claim 2 , wherein Rin formula (7) represents a hydrogen atom.14. The aromatic amine derivative according to claim 2 , wherein R claim 2 , Rand Rin formula (1) claim 2 , Rin formula (16) claim 2 , Rin formula (30) claim 2 , and Rin formula (7) represent hydrogen atoms.16. An organic electroluminescence device comprising an anode claim 2 , a cathode claim 2 , and at least one organic thin film layer disposed between the anode and the cathode claim 2 , wherein:the at least one organic thin film layer comprises a light emitting layer; and{' ...

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Номер записи: 91
10-12-2015 дата публикации

Novel anticancer agent

Номер: US20150353473A1
Автор: Akito Tanaka, Tadashi Shimizu, Takashi Nakano, Takeshi Kanno, Tomoyuki Nishizaki
Принадлежит: KTN BIOTEC Inc

The present invention aims to provide a compound having an anticancer action comparable or superior to that of naftopidil. A compound represented by the formula (I) wherein each symbol is as defined in the SPECIFICATION, or a pharmaceutically acceptable salt thereof, particularly 1-((2-((2-methoxyphenyl)amino)ethyl)amino)-3-(1-naphthyloxy)propan-2-ol, or a pharmaceutically acceptable salt thereof. The compound shows a cell proliferation suppressive action on a wide range of cancer cells, is useful as an anti-cancer agent, and is useful for the prophylaxis and/or treatment of cancer.

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Номер записи: 92
07-11-2019 дата публикации

Organic Materials with Special Optical Effects

Номер: US20190337885A1
Автор: Grégory Dupeyre, Laurélie Poulard, Philippe Laine
Принадлежит: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite Paris Diderot Paris 7

The present invention relates to a compound of the following formula (I). The invention also relates to uses thereof as a chromophore as such or for building pigments displaying special optical effects, including metal-like reflection.

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Номер записи: 93
14-12-2017 дата публикации

SAFENING 4-AMINO-3-CHLORO-6-(4-CHLORO-2-FLUORO-3-METHOXYPHENYL)-5-FLUOROPYRIDINE-2-CARBOXYLIC ACID COMPOSITIONS IN BRASSICA SPECIES AND METHODS OF USE THEREOF

Номер: US20170354146A1
Автор: Gast Roger E., Satchivi Norbert M.
Принадлежит: DOW AGROSCIENCES LLC

Provided herein are safened herbicidal compositions for use in species susceptible to injury by 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid comprising (a) a herbicidally effective amount of 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid or an agriculturally acceptable salt or ester of thereof, and (b) a safener. The safener can be a herbicide or a herbicide safener capable of safening the species susceptible to injury by 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid. 1Brassica. A safened herbicidal composition for use in species susceptible to injury by 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid or an agriculturally acceptable salt or ester thereof comprising:a) a herbicidally effective amount of 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid or an agriculturally acceptable salt or ester thereof; and [{'i': 'Brassica', 'i. a herbicide capable of safening the 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid, or an agriculturally acceptable salt or ester thereof, to the species;'}, {'i': 'Brassica', 'ii. a herbicide safener capable of safening the 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylic acid, or an agriculturally acceptable salt or ester thereof, to the species; or'}, 'iii. mixtures thereof., 'b) a safener comprising2. The composition of claim 1 , wherein (a) is benzyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)-5-fluoropyridine-2-carboxylate.3. The composition of claim 1 , wherein the herbicide capable of safening is clopyralid claim 1 , quinclorac claim 1 , picloram claim 1 , aminopyralid claim 1 , or agriculturally acceptable salts claim 1 , esters claim 1 , and combinations thereof.4. The composition of claim 1 , wherein the herbicide capable of ...

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Номер записи: 94
14-11-2019 дата публикации

Methods and Compositions for Inhibition of Bromodomain-Containing Proteins

Номер: US20190345162A1
Автор: Padia Janak Khimchand, Strovel Jeffrey William, Vankayalapati Hariprasad, Yoshioka Makoto
Принадлежит:

The present invention relates to compounds that bind to and otherwise modulate the activity of bromodomain-containing proteins, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders. 155-. (canceled)57. The method of claim 56 , wherein the compound is 4-(benzylamino)-6-(3 claim 56 ,5-dimethylisoxazol-4-yl)-1-methylquinolin-2(1H)-one claim 56 , or a pharmaceutically acceptable salt thereof.58. The method of claim 56 , wherein the compound is 4-(benzylamino)-6-(3 claim 56 ,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one claim 56 , or a pharmaceutically acceptable salt thereof.59. The method of claim 56 , wherein the disease or condition is pancreatic cancer.60. The method of claim 56 , wherein the disease or condition is sarcoma.61. The method of claim 56 , wherein the disease or condition is breast cancer.62. The method of claim 56 , wherein the disease or condition is prostate cancer.64. The method of claim 63 , wherein the compound is 4-(benzylamino)-6-(3 claim 63 ,5-dimethylisoxazol-4-yl)-1-methylquinolin-2(1H)-one claim 63 , or a pharmaceutically acceptable salt thereof.65. The method of claim 63 , wherein the compound is 4-(benzylamino)-6-(3 claim 63 ,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one claim 63 , or a pharmaceutically acceptable salt thereof.67. The method of claim 66 , wherein the compound is 4-(benzylamino)-6-(3 claim 66 ,5-dimethylisoxazol-4-yl)-1-methylquinolin-2(1H)-one claim 66 , or a pharmaceutically acceptable salt thereof.68. The method of claim 66 , wherein the compound is 4-(benzylamino)-6-(3 claim 66 ,5-dimethylisoxazol-4-yl)quinolin-2(1H)-one claim 66 , or a pharmaceutically acceptable salt thereof.69. The method of claim 66 , wherein the disease or condition is fibrosis.70. The method of claim 69 , wherein the fibrosis is idiopathic pulmonary fibrosis.71. The method of claim 66 , wherein the disease or ...

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Номер записи: 95
31-12-2015 дата публикации

TRIARYLAMINE DERIVATIVE AND ELECTROPHOTOGRAPHIC PHOTOSENSITIVE MEMBER

Номер: US20150378268A1
Автор: Kojima Kensuke, OKADA Hideki, SUGAI Fumio
Принадлежит: KYOCERA Document Solutions Inc.

A triarylamine derivative is represented by general formula (I). In general formula (I), Rand Reach represent, independently of one another, a chemical group selected from the group consisting of a halogen atom, an optionally substituted alkyl group having a carbon number of at least 1 and no greater than 6, an optionally substituted alkoxy group having a carbon number of at least 1 and no greater than 6, and an optionally substituted aryl group having a carbon number of at least 6 and no greater than 12. In general formula (I), m and n each represent an integer of at least 0 and no greater than 4. When m and n represent integers greater than 1, chemical groups Rbonded to the same aromatic ring and chemical groups Rbonded to the same aromatic ring may be the same or different to one another. 2. The triarylamine derivative according to claim 1 , whereinin the general formula (I),{'sub': 1', '2, 'Rand Reach represent, independently of one another, a chemical group selected from the group consisting of an alkyl group having a carbon number of at least 1 and no greater than 6 and an alkoxy group having a carbon number of at least 1 and no greater than 6, and'}m and n each represent 0 or 1.3. The triarylamine derivative according to claim 1 , whereinin the general formula (I),n represents 1, and{'sub': '2', 'Ris located at an ortho or para position relative to a butadienyl group.'}5. An electrophotographic photosensitive member comprisinga photosensitive layer containing a charge generating material and a hole transport material, whereinthe photosensitive layer is either one of:a multi-layer photosensitive layer including a charge generating layer that contains the charge generating material and a charge transport layer that contains the hole transport material, and in which the charge transport layer is located on the charge generating layer; anda single-layer photosensitive layer containing the charge generating material and the hole transport material, and{'claim-ref ...

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Номер записи: 96
29-12-2016 дата публикации

DYE COMPOSITION COMPRISING A CATIONIC PARA-AMINOPHENOL OXIDATION BASE

Номер: US20160374913A1
Автор: Fadli Aziz
Принадлежит:

The present invention relates to a para-aminophenol compound of formula (I), the addition salts thereof with an acid and the solvates thereof: 113-. (canceled)15. The compound according to claim 14 , wherein R1 is a saturated claim 14 , linear or branched C-Calkyl radical claim 14 , which is interrupted by at least one oxygen atom and/or by at least one group NR2 claim 14 , and/or substituted with at least one radical chosen from hydroxyl claim 14 , alkoxy or C-Chydroxyalkyl radicals; or a saturated claim 14 , unsaturated or aromatic cationic 5- to 8-membered heterocycle substituted with at least one radical chosen from C-Calkyl claim 14 , hydroxyl claim 14 , C-Calkoxy claim 14 , amino claim 14 , (C-C)alkylamino claim 14 , di(C-C)alkylamino claim 14 , thio claim 14 , (C-C)alkylthio claim 14 , carboxyl claim 14 , (C-C)alkylcarbonyl claim 14 , sulfonyl claim 14 , amido or C-Chydroxyalkyl radicals.16. The compound according to claim 14 , wherein when Z1 is NR2 claim 14 , then R1 and R2 form claim 14 , together with the nitrogen atom to which they are attached claim 14 , a saturated or unsaturated cationic 5- to 8-membered heterocycle substituted with at least one radical chosen from C-Calkyl radicals and hydroxyl claim 14 , C-Calkoxy claim 14 , amino claim 14 , (C-C)alkylamino claim 14 , di(C-C)alkylamino claim 14 , thio claim 14 , (C-C)alkylthio claim 14 , carboxyl claim 14 , (C-C)alkylcarbonyl claim 14 , sulfonyl claim 14 , amido and C-Chydroxyalkyl radicals claim 14 , wherein the heterocycle includes at least one heteroatom chosen from N or O; or a saturated or unsaturated noncationic 5- to 8-membered heterocycle substituted with at least one radical chosen from C-Calkyl radicals and hydroxyl claim 14 , C-Calkoxy claim 14 , amino claim 14 , (C-C)alkylamino claim 14 , di(C-C)alkylamino claim 14 , thio claim 14 , (C-C)alkylthio claim 14 , carboxyl claim 14 , (C-C)alkylcarbonyl claim 14 , sulfonyl claim 14 , amido and C-Chydroxyalkyl radicals.17. The compound according ...

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Номер записи: 97
31-12-2015 дата публикации

MATERIAL FOR ORGANIC ELECTROLUMINESCENCE DEVICE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

Номер: US20150380656A1
Автор: SAKAMOTO Naoya
Принадлежит:

A compound for an organic electroluminescence device and an organic electroluminescence device, the compound being represented by the following Chemical Formula 1: 2. The compound for an organic electroluminescence device as claimed in claim 1 , wherein the aryl group having 10 or more ring carbon atoms includes a biphenyl group claim 1 , a naphthyl group claim 1 , a phenanthrenyl group claim 1 , or a triphenylenyl group.3. The compound for an organic electroluminescence device as claimed in claim 2 , wherein the aryl group having 10 or more ring carbon atoms includes the biphenyl group.4. The compound for an organic electroluminescence device as claimed in claim 1 , wherein the heteroaryl group having 10 or more ring carbon atoms includes a dibenzohetero group.6. The compound for an organic electroluminescence device as claimed in claim 1 , wherein Arto Arare each independently a substituted or unsubstituted aryl group having 10 or more ring carbon atoms or a substituted or unsubstituted heteroaryl group having 10 or more ring carbon atoms.8. The organic electroluminescence device as claimed in claim 7 , wherein the aryl group having 10 or more ring carbon atoms includes a biphenyl group claim 7 , a naphthyl group claim 7 , a phenanthrenyl group claim 7 , or a triphenylenyl group.9. The organic electroluminescence device as claimed in claim 8 , wherein the aryl group having 10 or more ring carbon atoms includes a biphenyl group.10. The organic electroluminescence device as claimed in claim 7 , wherein the heteroaryl group having 10 or more ring carbon atoms includes a dibenzohetero group.12. The organic electroluminescence device as claimed in claim 7 , wherein Arto Arare each independently a substituted or unsubstituted aryl group having 10 or more ring carbon atoms or a substituted or unsubstituted heteroaryl group having 10 or more ring carbon atoms.16. The organic electroluminescence device as claimed in claim 7 , wherein:the organic electroluminescence device ...

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Номер записи: 98
12-11-2020 дата публикации

REDUNDANT POWER LINE CONTROL SYSTEMS

Номер: US20200358477A1
Автор: Bogdanovich Phillip
Принадлежит: Crius Technology Group, Inc.

Methods, systems, and apparatus for monitoring and controlling electronic devices using wired and wireless protocols are disclosed. The systems and apparatus may monitor their environment for signals from electronic devices. The systems and apparatus may take and disambiguate the signals that are received from the devices in their environment to identify the devices and associate control signals with the devices. The systems and apparatus may use communication means to send control signals to the identified electronic devices. Multiple apparatuses or systems may be connected together into networks, including mesh networks, to make for a more robust architecture. 1. A system for controlling an electronic device located at a site , comprising: a memory; and', receiving device signal information, signal noise, a conflated device signal, or a combination thereof, from a circuit connected to the control apparatus and the electronic device;', 'identifying the electronic device by comparing the device signal information, the signal noise, the conflated device signal, or a combination thereof, to a device waveform associated with the electronic device;', 'establishing a communication link with the electronic device; and', 'transmitting a control signal for controlling the electronic device via the communication link., 'a processor coupled to the memory, wherein the processor performs operations comprising], 'a control apparatus, comprising2. The system of claim 1 , wherein the operations further comprise receiving power via the circuit.3. The system of claim 1 , wherein the operations further comprise associating a device control pathway with the electronic device.4. The system of claim 1 , wherein the operations further comprise generating the control signal for controlling the electronic device.5. The system of claim 1 , wherein the operations further comprise pinging all inputs available to a communications cube of the control apparatus.6. The system of claim 1 , wherein ...

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Номер записи: 99
19-11-2020 дата публикации

Polymorphic forms of rad1901-2hcl

Номер: US20200361853A1
Автор: Alex Eberlin, Jonathan Blake MCKENZIE, Joshua Kyle BOLGER, Michael MARKEY, Michael Paul CRUSKIE, JR., Pratik SHETH, Richard Edwards
Принадлежит: Radius Pharmaceuticals Inc

Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed.

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Номер записи: 100