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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 6356. Отображено 100.
23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Автор: Hiroki Fukudome, Hiroshi Moritani, Takahiro Nigawara, Takeshi Hanazawa, Tomoaki Kawano, Yasuhiro Yonetoku
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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Номер записи: 1
07-06-2012 дата публикации

Proteasome inhibitors having chymotrypsin-like activity

Номер: US20120142917A1
Автор: Harshani Lawrence, Said M. Sebti, Wayne Guida, Yiyu Ge
Принадлежит: H Lee Moffitt Cancer Center and Research Institute Inc, UNIVERSITY OF SOUTH FLORIDA

Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl 4 . The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.

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Номер записи: 2
21-06-2012 дата публикации

Leaving substituent-containing compound, organic semiconductor material, organic semiconductor film containing the material, organic electronic device containing the film, method for producing film-like product, pi-electron conjugated compound and method for producing the pi-electron conjugated compound

Номер: US20120153271A1
Автор: Daisuke Goto, Keiichiro Yutani, Masataka Mohri, Masato Shinoda, Satoshi Yamamoto, Shinji Matsumoto, Takashi Okada, Takuji Kato, Toshiya Sagisaka
Принадлежит: Ricoh Co Ltd

A leaving substituent-containing compound including a partial structure represented by the following General Formula (I): where a pair of X 1 and X 2 or a pair of Y 1 and Y 2 each represent a hydrogen atom; the other pair each represent a group selected from the group consisting of a halogen atom and a substituted or unsubstituted acyloxy group having one or more carbon atoms; a pair of the acyloxy groups represented by the pair of X 1 and X 2 or the pair of Y 1 and Y 2 may be identical or different, or may be bonded together to form a ring; R 1 to R 4 each represent a hydrogen atom or a substituent; and Q 1 and Q 2 each represent a hydrogen atom, a halogen atom or a monovalent organic group, and may be bonded together to form a ring.

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Номер записи: 3
28-06-2012 дата публикации

Amino- and amido-aminotetralin derivatives and related compounds as mu opioid receptor antagonists

Номер: US20120165360A1
Автор: Daniel D. Long, Lan Jiang, Michael R. Leadbetter, Sabine Axt, Sean G. Trapp
Принадлежит: Theravance Inc

The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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Номер записи: 4
05-07-2012 дата публикации

Co-crystals of tramadol and coxibs

Номер: US20120172398A1
Автор: Carlos Ramon Plata Salaman, Nicolas Tesson
Принадлежит: Laboratorios del Dr Esteve SA

The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses in pharmaceutical formulations for the treatment of pain.

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Номер записи: 5
18-10-2012 дата публикации

Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors

Номер: US20120264736A1
Автор: Chad E. Bennett, Chad E. Knutson, David J. Cole, Dmitri A. Pissarnitski, Duane A. Burnett, Haiqun Tang, Hongmei Li, Hubert B. Josien, Jing Su, John W. Clader, Li Qiang, Mark D. Mcbriar, Martin S. Domalski, Mary Ann Caplen, Murali Rajagopalan, Ruo Xu, Thavalakulamgara K. Sasikumar, Theodros Asberom, Thomas A. Bara, Wen-Lian Wu, Zhiqiang Zhao
Принадлежит: Schering Corp

This invention discloses novel gamma secretase inhibitors of the formula: R 2 and R 3 , or R 2 and R 4 , or R 3 and R 4 , together with the atoms to which they are bound, can form a fused cycloalkyl or fused heterocycloalkyl ring. The cycloalkyl ring or the heterocycloalkyl ring can be optionally substituted with one or more substituents. One or more compounds of formula (I), or formulations comprising such compounds, may be useful, e.g. in treating Alzheimer's Disease.

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Номер записи: 6
25-04-2013 дата публикации

Novel Process for the Preparation of Nitrogen Substituted Aminotetralins Derivatives

Номер: US20130102794A1
Автор: Arnaud Schule, Celal Ates, David Vasselin, Ganesh Phadtare, Jean-Pierre Delatinne, Magali Palacio, Maria Luisa Escudero Hernandez, Nicolas Carly, Paul Deutsch, Swapnil Yerande, Véronique PINILLA
Принадлежит: UCB PHARMA GMBH

The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).

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Номер записи: 7
01-08-2013 дата публикации

Mglu 2/3 agonists

Номер: US20130197079A1
Автор: Barry Peter Clark, Christopher David Beadle, James Allen Monn, Lourdes Prieto, Stephen Richard Baker
Принадлежит: Eli Lilly and Co

The present invention provides novel mGlu2/3 agonists useful in the treatment of neurological or psychiatric disorders.

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Номер записи: 8
12-09-2013 дата публикации

4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS

Номер: US20130237573A1
Автор: Adam Michael Fivush, Bruce Anthony Dressman, Charles Howard Mitch, Eric George Tromiczak, Mark Donald Chappell, Paul Leslie Ornstein, Tatiana Natali Vetman
Принадлежит: Eli Lilly and Co

A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.

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Номер записи: 9
19-09-2013 дата публикации

Compound having hetero ring skeleton, and process for producing optically active compound using the aforementioned compound as asymmetric catalyst

Номер: US20130245257A1
Автор: Kazuo Murakami, Yoshiji Takemoto
Принадлежит: KYOTO UNIVERSITY, Sumitomo Chemical Co Ltd

The invention provides a compound having a heterocyclic skeleton of formula (I): wherein the substituents are as defined in the specification, as well as a tautomer thereof or a salt thereof. The invention also provides asymmetric synthesis methods involving the use of such a compound, tautomer thereof, or salt thereof, as a catalyst.

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Номер записи: 10
10-10-2013 дата публикации

Aromatic ketone synthesis with amide reagents and related reactions

Номер: US20130267712A1
Автор: Douglas A. Klumpp, Erum K. Raja
Принадлежит: Northern Illinois University

A method of preparing an aryl carbonyl or aryl thiocarbonyl compound, comprises reacting an N-(nitroaryl)-amide or N-(nitroaryl)-thioamide with an aromatic ring, with a superacid catalyst, to produce the aryl carbonyl or aryl thiocarbonyl compound. The superacid is present in an amount of at most 8 equivalents in proportion to the N-(nitroaryl)-amide or N-(nitroaryl)-thioamide. A method of preparing aryl amide or aryl thioamide, comprises reacting an N-(nitroaryl)-carbamide or N-(nitroaryl)-thiocarbamide with an aromatic ring, with a superacid catalyst, to produce the aryl amide or aryl thioamide.

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Номер записи: 11
06-02-2014 дата публикации

Compositions and processes of preparing and using the same

Номер: US20140039182A1
Автор: Changho HAN, David A. Colby, Mark V. RIOFSKI
Принадлежит: PURDUE RESEARCH FOUNDATION

The present invention relates to compositions, for example, the DBU/Hexafluoroacetone hydrate salt, and processes of preparing and using the same for the modification of chemical compounds via the release of trifluoroacetate. The DBU/Hexafluoroacetone hydrate salt can perform trifluoromethylation reactions on chemical compounds, such as carbonyl group-containing compounds.

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Номер записи: 12
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: 13
27-02-2014 дата публикации

Co-crystals of tramadol and coxibs

Номер: US20140057879A1
Автор: Carlos Ramon Plata Salaman, Nicolas Tesson
Принадлежит: Laboratorios del Dr Esteve SA

The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.

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Номер записи: 14
02-01-2020 дата публикации

TREATMENT OF CNS DISORDERS WITH trans 4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENAMINE

Номер: US20200000746A1
Автор: Currie Mark G, Fang Qun Kevin, Jerussi Thomas
Принадлежит: Sunovion Pharmaceuticals Inc.

Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful. 3. A method according to claim 1 , wherein the compound of formula PQ is (1S claim 1 ,4R)—N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine or a salt thereof.4. A method according to claim 1 , wherein the compound of formula PQ is (1R claim 1 ,4S)—N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine or a salt thereof.5. A method according to claim 1 , wherein the compound of formula PQ is (1S claim 1 ,4R)—N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine hydrochloride.6. A method according to claim 1 , wherein the compound of formula PQ is (1R claim 1 ,4S)—N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine hydrochloride. This application is a continuation application of co-pending U.S. application Ser. No. 15/873,540, filed Jan. 17, 2018. U.S. application Ser. No. 15/873,540 was a continuation of U.S. Ser. No. 15/299,186, filed Oct. 20, 2016, now U.S. Pat. No. 9,907,764. U.S. application Ser. No. 15/299,186 was a continuation application of U.S. application Ser. No. 14/727,260, filed Jun. 1, 2015, now U.S. Pat. No. 9,498,452. U.S. Ser. No. 14/727,260 was a continuation of U.S. application Ser. No. 14/152,377, filed on Jan. 10, 2014, now U.S. Pat. No. 9,072,699. U.S. application Ser. No. 14/152,377 was a continuation application of U.S. application Ser. No. 13/693,489, filed on Dec. 4, 2012, now U.S. Pat. No. 8,658,700. U.S. ...

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Номер записи: 15
13-01-2022 дата публикации

METHOD FOR PRODUCING HETEROCYCLIDENE ACETAMIDE DERIVATIVE

Номер: US20220009898A1
Автор: CAI Xiaofei, Chen Chuan, CHEN Yanliang, GE Yonghui, GU Xiaomin, Li Jie, LIN Jinguang, LUO Jian, SATOH Tsutomu, SHA Chunbo, Sun Baoquan, SUN Fenglai, UCHIDA Hideharu, YE Jiajie, ZHAO BIN
Принадлежит: MOCHIDA PHARMACEUTICAL CO., LTD.

The present invention provides, a novel method for producing a compound represented by formula (I) and a novel method for producing a compound represented by formula (B) or a salt thereof, which are intermediates in the production of formula (I). The present invention relates to a new method for producing (E)-2-(7-trifluoromethylchroman-4-ylidene)-N-((7R)-7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide represented by Formula (I) which is a heterocyclidene acetamide derivative. Furthermore, the present invention relates to a new method for producing (R)-8-amino-1,2,3,4-tetrahydronaphthalen-2-ol represented by Formula (B) or a salt thereof, which is an intermediate useful for producing the compound represented by Formula (I).(E)-2-(7-trifluoromethylchroman-4-ylidene)-N-((7R)-7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)acetamide represented by Formula (I) is a transient receptor potential vanilloid 1 (TRPV1) antagonist, and is anticipated as a preventive and/or therapeutic agent for diseases involving the TRPV1 receptor (for example, pain (for example, neuropathic pain, diabetic neuralgia, postoperative pain, osteoarthrosis, rheumatoid arthritis pain, inflammatory pain, cancer pain, migraine and the like), nervous disorders, nerve damage, neurodegeneration, chronic obstructive pulmonary disease, asthma, rhinitis, inflammation of mucous membranes such as in the eyes, nervous skin disease, inflammatory skin disease, allergic disease, urinary incontinence, urge incontinence, overactive bladder, cystitis, pruritus, and the like) (Patent Literature 1).WO 2007/010383 (Patent Literature 1) discloses a method for producing the compound represented by Formula (I). In the document, the compound represented by Formula (I) is produced in steps of to shown in the following (scheme A). A compound represented by Formula (IM-k) is obtained by performing a condensation reaction using 8-amino-3,4-dihydronaphthalen-2(1H)-one (Formula (IM-3)) produced ...

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Номер записи: 16
13-01-2022 дата публикации

METHODS AND INTERMEDIATES FOR PREPARING THERAPEUTIC COMPOUNDS

Номер: US20220009904A1
Автор: "OKeefe Brian Michael", Allan Kevin McCormack, Brizgys Gediminas, Dhar Sachin, Doxsee Ian James, GOLDBERG Alex, Heumann Lars V., Huang Zilin, Kadunce Nathaniel Thomas, Kazerani Shahrokh, Lew Willard, Ngo Vinh Xuan, Rainey Trevor James, Roberts Benjamin James, Shi Bing, Steinhuebel Dietrich P., Tse Winston C., Vandehey Amanda Lynn, Wagner Anna Michelle, Wang Xianghong, Wolckenhauer Scott Alan, Wong Chloe Yuyi, Zhang Jennifer R.
Принадлежит:

The present disclosure relates to methods and intermediates useful for preparing a compound of formula I. 1171.-. (canceled)173174.-. (canceled)175. The process of claim 172 , wherein HX is N-Boc-D-leucine or (−)-N-acetyl-D-leucine.176. (canceled)177. The process of claim 172 , wherein the solvent is selected from the group consisting of n-heptane claim 172 , ethyl acetate claim 172 , butyl acetate claim 172 , isobutylacetate claim 172 , diethyl ether claim 172 , methyl tert-butyl ether claim 172 , tetrahydrofuran claim 172 , 2-methyltetrahydrofuran claim 172 , 1 claim 172 ,4-dioxane claim 172 , benzene claim 172 , xylenes claim 172 , toluene claim 172 , dichloromethane claim 172 , dichloroethane claim 172 , chloroform claim 172 , methanol claim 172 , ethanol claim 172 , 2-propanol claim 172 , acetone claim 172 , methyl ethyl ketone claim 172 , methylisobutylketone claim 172 , N claim 172 ,N-dimethylformamide claim 172 , N claim 172 ,N-dimethylacetamide claim 172 , N-methylpyrrolidone claim 172 , dimethylsulfoxide claim 172 , acetonitrile claim 172 , propionitrile claim 172 , butyronitrile claim 172 , water claim 172 , and combinations thereof.178. The process of claim 172 , wherein the solvent is toluene.179180.-. (canceled)181. The process of claim 172 , wherein the compound of formula X is treated with a base selected from the group consisting of potassium hydroxide claim 172 , potassium carbonate claim 172 , potassium bicarbonate claim 172 , sodium carbonate claim 172 , sodium bicarbonate claim 172 , triethylamine claim 172 , ammonium hydroxide claim 172 , potassium phosphate dibasic claim 172 , potassium phosphate tribasic claim 172 , sodium phosphate dibasic claim 172 , and sodium phosphate tribasic in a first solvent selected from the group consisting of diethyl ether claim 172 , methyl tert-butyl ether claim 172 , 2-methyltetrahydrofuran claim 172 , tetrahydrofuran claim 172 , 1 claim 172 ,4-dioxane claim 172 , aromatic solvents claim 172 , dichloromethane ...

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Номер записи: 17
11-01-2018 дата публикации

Ligand-Enabled meta-C-H Activation Using a Transient Mediator

Номер: US20180009739A1
Автор: YU JIN-QUAN
Принадлежит:

An alternative approach to formation of a C-C bond at a meta-position of an aromatic compound is disclosed that employs an ethylenically unsaturated bicyclic compound as a transient mediator to achieve meta-selective C-H activation with a simple and common ortho-directing group. The use of a pyridine-based ligand assists in relaying the palladium catalyst to the meta-position by the unsaturated bicyclic compound following initial ortho-C-H activation. 2. The method according to claim 1 , wherein circled Ar is carbocyclic.3. The method according to claim 2 , wherein one or both of Vand Vare other than hydrido.4. The method according to claim 3 , wherein Z is C.5. The method according to claim 4 , wherein W is C and X is ═O.6. The method according to claim 4 , wherein Ris a 4-(CF)CFNH— group.7. The method according to claim 4 , wherein Ris H.8. The method according to claim 4 , wherein Ris HY.9. The method according to claim 4 , wherein Ris HR.10. The method according to claim 1 , wherein W is nitrogen that is a ring atom of an aromatic ring system that contains at least one additional nitrogen atom that is adjacent to W in the aromatic ring.11. The method according to claim 1 , wherein W is the carbon of a >CH— group claim 1 , X is a N-sulfonamido or N-carboxamido group claim 1 , and Ris a C-C-hydrocarbyl carboxylate group.12. The method according to claim 1 , wherein W is C and W claim 1 , X and Rtogether form a heteroaromatic ring structure that contains one ring or two fused rings that each contains 5- or 6-members and a total of one to four heteroatoms that are independently nitrogen claim 1 , oxygen or sulfur.13. The method according to claim 1 , wherein said reactive coupling agent is an aromatic claim 1 , benzylic or aliphatic bromide or iodide compound of the Formula R-Q claim 1 , wherein Ris an aromatic group claim 1 , a straight claim 1 , branched or cyclic aliphatic C-C-hydrocarbyl group claim 1 , or a benzylic group claim 1 , and Q is bromo or iodo.14. ...

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Номер записи: 18
18-01-2018 дата публикации

PREPARATION OF CHIRAL AMIDES AND AMINES

Номер: US20180016224A1
Автор: BAKALE Roger P., KOENIG Stefan G., SINGH Surendra, VANDENBOSSCHE Charles P., Wilkinson Harold Scott, ZHAO Hang
Принадлежит:

This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine sub structure. 151.-. (canceled) This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 60/787,837 filed Mar. 31, 2006, which application is incorporated herein by reference in its entirety for all purposes.This invention relates to processes suitable for the large-scale preparation of enantiomerically- or diastereomerically-enriched chiral amides and amines prepared by these processes.Enantiomerically-enriched chiral primary amines are commonly used as resolving agents for racemic acids, as chiral auxiliaries for asymmetric syntheses and as ligands for transition metal catalysts used in asymmetric catalysis. In addition, many pharmaceuticals, such as sertraline, contain chiral amine moieties. Effective methods for the preparation of such compounds are of great interest to the pharmaceutical industry. Particularly valuable are processes that allow for the preparation of each enantiomer or diastereomer, in enantiomeric or diastereomeric excess, as appropriate, from prochiral or chiral starting materials.Methods are available for the preparation of enantiomerically enriched amines. For example, the addition of organometallic reagents to imines or their derivatives is reported by Watanabe et al., . ...

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Номер записи: 19
22-01-2015 дата публикации

Methods and compositions for treatment of muscle wasting, muscle weakness, and/or cachexia

Номер: US20150024032A1
Автор: David J. Tweardy, Marvin X. Xu, Moses M. Kasembeli, Thomas Kristian Eckols
Принадлежит: Baylor College of Medicine

Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.

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Номер записи: 20
25-01-2018 дата публикации

COMPOUND, AND SEPARATION METHOD, SYNTHESIS METHOD AND USE THEREOF

Номер: US20180022688A1
Автор: Duan Zhenwen, Guo Shuren, Li Xuemei
Принадлежит:

The invention relates to new compounds as well as a separation method, a synthetic method and use thereof. It is demonstrated by an assay on activity that the compound has an activity of inhibiting an HMG-CoA reductase. In addition, the invention also relates to a derivative of the compound. 2. The compound according to claim 1 , wherein claim 1 ,{'sub': 1', '1', '3', '1', '3', '2', '1-3', '3', '6', '3', '6', '1', '3', '1', '3', '1', '3', '1', '3, 'Ris selected from H, C-Calkyl, halo C-Calkyl, (CH)OH, C-Ccycloalkyl, halo C-Ccycloalkyl, C-Calkoxy, halo C-Calkoxy, C-Calkylthio, halo C-Calkylthio, halogen, nitro, amino and cyano.'}3. The compound according to claim 1 , wherein claim 1 ,{'sub': 1', '1', '3', '1', '3', '2', '1-3, 'Ris selected from H, C-Calkyl, halo C-Calkyl, (CH)OH, halogen, nitro, amino and cyano.'}4. The compound according to claim 1 , wherein{'sub': 1', '1', '3', '2', '1-3, 'Ris selected from H, C-Calkyl, and (CH)OH.'}5. The compound according to claim 1 , wherein{'sub': 2', '1', '3', '1', '3', '2', '1-3', '6', '3', '6', '3', '6', '1', '3', '1', '3', '1', '3', '1', '3, 'Ris selected from H, C-Calkyl, halo C-Calkyl, (CH)OR, C-Ccycloalkyl, halo C-Ccycloalkyl, C-Calkoxy, halo C-Calkoxy, C-Calkylthio, halo C-Calkylthio, halogen, nitro, amino and cyano;'}{'sub': 6', '7', '2', '8', '9', '10', '11, 'wherein, Ris selected from H, —COR, —SOR, and —SiRRR;'}{'sub': 7', '1', '6', '1', '6', '8', '1', '6', '1', '6', '6', '10', '6', '10', '9', '10', '11', '1', '6, 'wherein, Ris selected from C-Calkyl, and halo C-Calkyl; Ris selected from C-Calkyl, optionally substituted C-Calkyl, C-Caryl, and optionally substituted C-Caryl; R, Rand Rare independently selected from C-Calkyl.'}6. The compound according to claim 1 , wherein{'sub': 2', '1', '3', '1', '3', '2', '1-3', '6', '3', '6', '3', '6', '1', '3', '1', '3', '1', '3', '1', '3, 'Ris selected from H, C-Calkyl, halo C-Calkyl, (CH)OR, C-Ccycloalkyl, halo C-Ccycloalkyl, C-Calkoxy, halo C-Calkoxy, C-Calkylthio, halo C- ...

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Номер записи: 21
28-01-2021 дата публикации

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20210024462A1
Автор: Last Stefaan Julien, Raboisson Pierre Jean-Marie Bernard, ROMBOUTS Geert, Vandyck Koen, Verschueren Wim Gaston
Принадлежит:

Inhibitors of HBV replication of Formula (I) 2. The compound according to claim 1 , wherein Rrepresents a 3-7 membered saturated ring claim 1 , containing one or more heteroatoms each independently selected from the group consisting of O claim 1 , S and N claim 1 , such 3-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halo claim 1 , C-Calkyloxy claim 1 , C(═O)—C-Calkyl claim 1 , C-Calkyl claim 1 , OH claim 1 , CN claim 1 , CFH claim 1 , CFH and CF;{'sub': 1', '2', '1', '4', '1', '3', '1', '4', '2', '2', '3, 'Or RRtogether with the Nitrogen to which they are attached form a 5-7 membered saturated ring, optionally containing one or more additional heteroatoms each independently selected from the group consisting of O, S and N, such 5-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen, halo, CCalkyloxy, oxo, C(═O)—C-Calkyl, C-Calkyl, OH, CN, CFH, CFH and CF.'}3. The compound according to wherein Rrepresents a 4-7 membered saturated ring containing carbon and one or more oxygen atoms claim 1 , such 4-7 membered saturated ring optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halo claim 1 , CCalkyloxy claim 1 , C(═O)—C-Calkyl claim 1 , C-Calkyl claim 1 , OH claim 1 , CN claim 1 , CFH claim 1 , CFH and CF.4. The compound according to claim 1 , wherein B represents phenyl or thiophene claim 1 , optionally being substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 1 , halogen claim 1 , C-Calkyl claim 1 , CN claim 1 , CFH claim 1 , CFH and CF.5. The compound according to claim 1 , wherein Rrepresents C-Calkyl-Ror a 4-7 membered saturated ring consisting of carbon atoms and one or more heteroatoms each independently ...

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Номер записи: 22
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: 23
04-02-2016 дата публикации

Cycloalkyl-dione derivatives and methods of their use

Номер: US20160031805A1
Автор: Amos B. Smith, Carlo Ballatore, John Q. Trojanowski, Kurt R. Brunden, Virginia M.Y. Lee, Xiaozhao Wang
Принадлежит: University of Pennsylvania Penn

The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R 1 is H or C 1-6 alkyl and R 2 is H, C 1-6 alkyl, C 1-6 alkaryl, aryl, or heteroaryl; and X is O or NH. Tautomers, enantiomers, and diastereomers, as well as pharmaceutically acceptable salt forms, of compounds of formula I are also within the scope of the invention. Methods of preparing and using the compounds of formula I are also described. wherein A is

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Номер записи: 24
01-02-2018 дата публикации

Isothiocyanate compound and application thereof

Номер: US20180029979A1
Автор: Yongliang Yang
Принадлежит: Drivingforce Therapeutics Co Ltd

The present invention provides an isothiocyanate compound and its application. The compound is an aryl-substituted isothiocyanate compound that has a structure of the general formula I. The isothiocyanate compound of the present invention has very good solubility in water, far better inhibitory activity for XPO1 protein than other non-aryl substituted congeneric compounds, little side effects, and good biological safety and bioavailability, and is quite suitable for clinical application. Therefore, the isothiocyanate compound would have tremendous potential market space and economic benefits.

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Номер записи: 25
01-02-2018 дата публикации

COMPOUNDS CONTAINING CARBON-CARBON LINKER AS GPR120 AGONISTS

Номер: US20180030031A1
Автор: BAJAJ Komal, GODSE Pallavi, Kumar Sanjay, MAHAJAN Vishal, Sharma Rajiv
Принадлежит:

The present invention relates to compound of Formula (I) containing carbon-carbon linker, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a prodrug, a polymorph, N-oxide, S-oxide, or a carboxylic acid isostere thereof; processes for their preparation; pharmaceutical compositions comprising said compounds; and their use for the treatment of the diseases or disorders mediated by GPR120 receptor. 2. The compound of Formula (I) according to claim 1 , wherein Ring A is unsubstituted or substituted 3- to 10-membered cycloalkyl or unsubstituted or substituted 5- to 12-membered heterocycloalkyl containing 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms independently selected from the group consisting of N claim 1 , O and S or unsubstituted or substituted (C-C)aryl or 5- to 12-membered heteroaryl containing 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms independently selected from the group consisting of N claim 1 , O and S or unsaturated or partially unsaturated (C-C)aryl or unsaturated or partially unsaturated 5- to 12-membered heteroaryl.4. The compound of Formula (I) according to claim 1 , wherein Ring B is unsubstituted or substituted (C-C)aryl or 5- to 12-membered heteroaryl containing 1 claim 1 , 2 or 3 heteroatoms independently selected from the group consisting of N claim 1 , O and S.5. The compound of Formula (I) according to claim 4 , wherein Ring B is unsubstituted or substituted phenyl.6. The compound of Formula (I) according to claim 5 , wherein Ring B is unsubstituted or substituted phenyl and Ris located at para position to Ring A and n is 1.7. The compound of Formula (I) according to claim 6 , wherein Ring B is phenyl and Ris halogen located at para position to Ring A and n is 1.8. The compound of Formula (I) according to claim 1 , wherein Ring C is unsubstituted or substituted (C-C)aryl or 5- to 12-membered heteroaryl containing 1 claim 1 , 2 or 3 heteroatoms independently selected from the group consisting of N ...

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Номер записи: 26
31-01-2019 дата публикации

TETRAHYDRONAPHTHALENE DERIVATIVE

Номер: US20190031605A1
Автор: INAGAKI Yuichi, KUSUMI Kensuke, WATANABE Toshihide
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

A compound represented by general formula (I-1): 3. The compound according to claim 1 , wherein Y is —CH— or —O— claim 1 , or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein ring 1 is a C3-10 carbocyclic ring claim 1 , or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein ring 3 is a C3-7 saturated carbocyclic ring which may be substituted with a C1-4 alkyl group claim 1 , or a 3- to 7-membered saturated heterocyclic ring which may be substituted with a C1-4 alkyl group claim 1 , or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein Z is a carboxyl group which may be substituted with a C1-8 alkyl group claim 1 , or a pharmaceutically acceptable salt thereof.7. A pharmaceutical composition comprising the compound represented by general formula (I-1) according to claim 1 , or a pharmaceutically acceptable salt thereof.8. The pharmaceutical composition according to claim 7 , which is an S1Pbinder and/or modulator.9. The pharmaceutical composition according to claim 7 , which is an agent for preventing and/or treating a S1P-mediated disease.10. The pharmaceutical composition according to claim 9 , wherein the S1P-mediated disease is neurodegenerative disease claim 9 , autoimmune disease claim 9 , infection or cancer.11. The pharmaceutical composition according to claim 10 , wherein the neurodegenerative disease is schizophrenia claim 10 , Binswanger's disease claim 10 , multiple sclerosis claim 10 , neuromyelitis optica claim 10 , Alzheimer's disease claim 10 , cognitive impairment claim 10 , amyotrophic lateral sclerosis or spinocerebellar ataxia.12. A method for preventing and/or treating a S1P-mediated disease claim 1 , comprising administering to a mammal an effective amount of the compound represented by general formula (I-1) according to claim 1 , or a pharmaceutically acceptable salt thereof.1314-. (canceled)15. The compound according to claim 2 ...

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Номер записи: 27
04-02-2021 дата публикации

Imaging histone deacetylases with a radiotracer using positron emission tomography

Номер: US20210030899A1
Автор: Changning Wang, Frederick Albert SCHROEDER, Jacob M. Hooker
Принадлежит: General Hospital Corp

wherein R1 is a moiety including a positron emitter; R2 represents hydrogen, or substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and n is an integer selected from 0 or 1. In one version of the compound of formula (I), R1 is a moiety including an adamantyl group.

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Номер записи: 28
18-02-2021 дата публикации

TREATMENT OF CNS DISORDERS WITH trans 4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-1-NAPHTHALENAMINE

Номер: US20210046021A1
Автор: Currie Mark G., Fang Qun Kevin, Jerussi Thomas
Принадлежит: Sunovion Pharmaceuticals Inc.

Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful. 3. A method according to claim 1 , wherein the compound of formula PQ is (1S claim 1 ,4R)-N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine or a salt thereof.4. A method according to claim 1 , wherein the compound of formula PQ is (1R claim 1 ,4S)-N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine or a salt thereof.5. A method according to claim 1 , wherein the compound of formula PQ is (1S claim 1 ,4R)-N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine hydrochloride.6. A method according to claim 1 , wherein the compound of formula PQ is (1R claim 1 ,4S)-N-[4-(3 claim 1 ,4-dichlorophenyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-1-naphthalenamine hydrochloride. This application is a continuation application of co-pending U.S. application Ser. No. 15/873,540, filed Jan. 17, 2018. U.S. application Ser. No. 15/873,540 was a continuation of U.S. Ser. No. 15/299,186, filed Oct. 20, 2016, now U.S. Pat. No. 9,907,764. U.S. application Ser. No. 15/299,186 was a continuation application of U.S. application Ser. No. 14/727,260, filed Jun. 1, 2015, now U.S. Pat. No. 9,498,452. U.S. Ser. No. 14/727,260 was a continuation of U.S. application Ser. No. 14/152,377, filed on Jan. 10, 2014, now U.S. Pat. No. 9,072,699. U.S. application Ser. No. 14/152,377 was a continuation application of U.S. application Ser. No. 13/693,489, filed on Dec. 4, 2012, now U.S. Pat. No. 8,658,700. U.S. ...

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Номер записи: 29
06-02-2020 дата публикации

Aromatic compounds

Номер: US20200039903A1
Автор: Christian Ehrenreich, Philipp Stoessel
Принадлежит: Merck Patent GmBH

The present invention relates to aromatic compounds suitable for preparation of asymmetric polydentate ligands. The present invention further describes a process for preparing asymmetric polydentate ligands and metal complexes comprising these ligands which are suitable for use as emitters in organic electroluminescent devices.

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Номер записи: 30
01-05-2014 дата публикации

Deuterated phenylpropionic acid derivative

Номер: US20140121407A1
Автор: Hideaki Muratake, Koichi Shudo, Takahiro Toda, Yohei Amano
Принадлежит: RESEARCH FOUNDATION ITSUU LABORATORY

A compound corresponding to 3-[4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]phenyl]propionic acid in which a part or all of hydrogen atoms in the ethylene group constituting the propionic acid moiety are replaced with deuterium atoms, a salt thereof, or an ester thereof, and a prodrug for releasing Am80 as an active medicament after being absorbed into a living body, which comprises the aforementioned compound, a salt thereof, or an ester thereof as an active ingredient.

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Номер записи: 31
14-02-2019 дата публикации

PRODRUG OF AMINO ACID DERIVATIVE

Номер: US20190047943A1
Автор: Hashihayata Takashi, Masuda Seiji, Matsuda Yohei, Otake Norikazu, Yamauchi Yuko
Принадлежит: TAISHO PHARMACEUTICAL CO., LTD.

Provided is an amino acid derivative prodrug represented by general formula (I-A) that is a prodrug form of an amino acid derivative which is a group 2 metabotropic glutamate receptor antagonist, or a pharmaceutically acceptable salt thereof. 120-. (canceled)22. The compound or pharmaceutically acceptable salt thereof according to claim 21 , wherein Ris a fluorine atom.23. The compound or pharmaceutically acceptable salt thereof according to claim 22 , wherein Ris a Calkyl group claim 22 , a Ccycloalkyl group optionally substituted by one to three Calkyl groups claim 22 , a Ccycloalkoxy group optionally substituted by one to three Calkyl groups and optionally having a Calkylene group crosslinking two different carbon atoms in the ring claim 22 , an adamantyl group optionally substituted by one to three Calkyl groups claim 22 , or a phenyl group.25. The compound or pharmaceutically acceptable salt thereof according to claim 21 , wherein Ris a hydrogen atom.27. The compound or pharmaceutically acceptable salt thereof according to claim 25 , wherein Ris a 4-fluorophenyl group or a 3 claim 25 ,4-difluorophenyl group.29. The compound or pharmaceutically acceptable salt thereof according to claim 25 , wherein Ris a methyl group.32. The compound or pharmaceutically acceptable salt thereof according to claim 30 , wherein Ris a methyl group.33. The compound or pharmaceutically acceptable salt thereof according to claim 21 , wherein the compound or pharmaceutically acceptable salt thereof is any of the following compounds:{'sup': '3,7', '(1R,2R,3R,5R,6R)-2-amino-6-fluoro-3-[(4-fluorophenyl)methoxy]-2-({(1S)-1-[(tricyclo[3.3.1.1]decane-1-carbonyl)oxy]ethoxy}carbonyl)bicyclo[3.1.0]hexane-6-carboxylic acid,'}{'sup': '3,7', '(1R,2R,3R,5R,6R)-2-amino-6-fluoro-3-[(4-fluorophenyl)methoxy]-2-({[(tricyclo[3.3.1.1]decane-1-carbonyl)oxy]methoxy}carbonyl)bicyclo[3.1.0]hexane-6-carboxylic acid,'}{'sup': '3,7', '(1R,2R,3R,5R,6R)-2-amino-3-[(3,4-difluorophenyl)methoxy]-6-fluoro-2-({(1S)-1 ...

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Номер записи: 32
25-02-2021 дата публикации

Novel thyromimetics

Номер: US20210053917A1
Автор: Bradley Backes, Thomas von Geldern
Принадлежит: Autobahn Therapeutics Inc

or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X1, X2, Q, R1, R2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.

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Номер записи: 33
25-02-2021 дата публикации

COMPOUNDS CONTAINING CARBON-CARBON LINKER AS GPR120 AGONISTS

Номер: US20210053938A1
Автор: BAJAJ Komal, GODSE Pallavi, Kumar Sanjay, MAHAJAN Vishal, Sharma Rajiv
Принадлежит:

The present invention relates to compound of Formula (I) 2. The compound of Formula (I) according to claim 1 , wherein Ring A is unsubstituted or substituted 3- to 10-membered cycloalkyl or unsubstituted or substituted 5- to 12-membered heterocycloalkyl containing 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms independently selected from the group consisting of N claim 1 , O and S claim 1 , or unsubstituted or substituted (C-C)aryl claim 1 , or 5- to 12-membered heteroaryl containing 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms independently selected from the group consisting of N claim 1 , O and S claim 1 , an or unsaturated or partially unsaturated (C-C)aryl or unsaturated or partially unsaturated 5- to 12-membered heteroaryl.4. The compound of Formula (I) according to claim 1 , wherein Ring B is selected from the group consisting of an unsubstituted or substituted (C-C)aryl and a 5- to 12-membered heteroaryl containing 1 claim 1 , 2 or 3 heteroatoms independently selected from the group consisting of N claim 1 , O and S.5. The compound of Formula (I) according to claim 4 , wherein Ring B is an unsubstituted or substituted phenyl.6. The compound of Formula (I) according to claim 4 , wherein Ring B is an unsubstituted or substituted phenyl and Ris located at a para position to Ring A and n is 1.7. The compound of Formula (I) according to claim 4 , wherein Ring B is phenyl and Ris a halogen located at a para position to Ring A and n is 1.8. The compound of Formula (I) according to claim 1 , wherein Ring C is selected from the group consisting of an unsubstituted or substituted (C-C)aryl and a 5- to 12-membered heteroaryl containing 1 claim 1 , 2 or 3 heteroatoms independently selected from the group consisting of N claim 1 , O and S.9. The compound of Formula (I) according to claim 8 , wherein Ring C is selected from the group consisting of an unsubstituted or substituted phenyl claim 8 , and an unsubstituted or substituted 5- to 6-membered heteroaryl.10. The compound of ...

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Номер записи: 34
21-02-2019 дата публикации

ASYMMETRIC CATALYTIC DECARBOXYLATIVE ALKYL ALKYLATION USING LOW CATALYST CONCENTRATIONS AND A ROBUST PRECATALYST

Номер: US20190055182A1
Автор: Craig Robert A., Duquette Douglas, Kim Kelly E., Liniger Marc, Marziale Alexander N., Numajiri Yoshitaka, Stoltz Brian M.
Принадлежит:

This invention provides efficient and scalable enantioselective methods that yield 2-alkyl-2-allylcycloalkyanone compounds with quaternary stereogenic centers. Methods include the method for the preparation of a compound of formula (I): 140-. (canceled)45. The method of claim 44 , wherein the sum of m and n is 0 claim 44 , 1 claim 44 , 2 claim 44 , or 3.46. The method of claim 44 , wherein each occurrence of W claim 44 , B claim 44 , D claim 44 , and E is each independently —CRR— claim 44 , or —CR— claim 44 , or —C(O)—.47. The method of claim 46 , wherein one occurrence of W claim 46 , B claim 46 , D claim 46 , and E is —CRR— or —C(O)— claim 46 , and the remaining three are —CRR—;{'sup': 7', '8, 'optionally wherein Rand R, independently for each occurrence, are selected from hydrogen, hydroxyl, halo, alkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryl)alkyl, (5- to 10-membered heterocyclyl)alkyl, 5- to 10-membered heterocyclyl, alkenyl, alkynyl, amino, alkoxy, aryloxy, arylalkoxy, alkylamino, and amido.'}48. The method of claim 44 , wherein at least two adjacent occurrences of W claim 44 , B claim 44 , D claim 44 , and E are —CR—.49. The method of claim 48 , wherein W and B are each —CR— and m is 1;{'sup': '7', 'optionally wherein Ris independently selected for each occurrence from hydrogen, hydroxyl, halo, alkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, aralkyl, 5- to 10-membered heteroaryl heteroaryl, (5- to 10-membered heteroaryl)alkyl, (5- to 10-membered heterocyclyl)alkyl, 5- to 10-membered heterocyclyl, alkenyl, alkynyl, amino, alkoxy, aryloxy, alkylamino, amido, and acylamino; or'}{'sup': 7', '7, 'the occurrence of Ron W and the occurrence of Ron B are taken together to form an optionally substituted aryl, 5- to 10-membered heteroaryl, cycloalkenyl, or (5- to 10-membered heterocyclyl)alkenyl.'}50. The method of claim 44 , wherein at least one occurrence of W claim 44 , B claim 44 , D claim 44 , and E is ...

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Номер записи: 35
01-03-2018 дата публикации

CARBAMATE DERIVATIVE COMPOUNDS, PROCESSES FOR PREPARING THEM AND THEIR USES

Номер: US20180057449A1
Автор: Choi Yong Moon
Принадлежит:

The present invention relates to a pharmaceutical composition for treating or preventing CNS disorders containing a carbamate derivative compound and/or pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or prevention CNS disorders comprising administering a carbamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or prevention of CNS disorders. 2. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , wherein R claim 1 , R claim 1 , Rand Rare each independently selected from the group consisting of hydrogen claim 1 , F claim 1 , Br claim 1 , Cl and I; and if R claim 1 , R claim 1 , Rand Rare hydrogen claim 1 , l+m is not 1.4. The compound or a pharmaceutically acceptable salt thereof according to or claim 1 , wherein Rand Rare each independently selected from the group consisting of hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , iso-propyl claim 1 , t-butyl claim 1 , cyclopropyl claim 1 , cyclohexyl claim 1 , bicycloheptanyl claim 1 , phenyl and benzyl.5. The compound or a pharmaceutically acceptable salt thereof according to or claim 1 , Ris selected from hydrogen claim 1 , trimethyl silyl claim 1 , triethyl silyl claim 1 , triisopropyl silyl claim 1 , t-butyl dimethyl silyl claim 1 , trimethylsilylethoxymethyl (SEM) claim 1 , methoxymethyl (MOM) claim 1 , methoxyethoxymethyl (MEM) claim 1 , ethoxyethyl (EE) claim 1 , therahydropyranyl (THP) methylthiomethyl (MTM) and benzyloxymethyl (BOM).6. The compound or a pharmaceutically acceptable salt thereof according to or claim 1 , wherein Rand Rare each independently selected from the group consisting of hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , iso-propyl and t-butyl; and{'sup': '7', 'Ris selected from hydrogen, methyl, ethyl, propyl, iso-propyl, t-butyl and methoxymethyl (MOM); and'}l and m are independently an ...

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Номер записи: 36
04-03-2021 дата публикации

NOVEL PRECATALYST SCAFFOLDS FOR CROSS-COUPLING REACTIONS, AND METHODS OF MAKING AND USING SAME

Номер: US20210061834A1
Автор: HAZARI Nilay, HRUSZKEWYCZ Damian, Melvin Patrick
Принадлежит:

The present invention provides novel transition-metal precatalysts that are useful in preparing active coupling catalysts. In certain embodiments, the precatalysts of the invention are air-stable and moisture-stable. The present invention further provides methods of making and using the precatalysts of the invention. 114-. (canceled)16. The precatalyst of claim 15 ,wherein L is a bidentate ligand, and (i) X is present and coordinates to M or', '(ii) X is absent or X does not coordinate to M., 'wherein'}17. (canceled)18. The precatalyst of claim 15 , wherein M is selected from the group consisting of Pd claim 15 , Ni and Pt.19. (canceled)20. The precatalyst of claim 15 , wherein X is a weakly coordinating ligand.21. The precatalyst of claim 15 , wherein X is selected from the group consisting of halide claim 15 , trifluoromethanesulfonate (triflate) claim 15 , tosylate claim 15 , mesylate claim 15 , tetrafluoroborate claim 15 , tetraphenylborate claim 15 , hexafluorophosphine claim 15 , acetate claim 15 , trifluoroacetate claim 15 , acetonitrile claim 15 , tetrahydrofuran claim 15 , dichloromethane and water.22. The precatalyst of claim 15 , wherein the 5-membered ring is substituted with at least one R.23. The precatalyst of claim 15 , wherein the 5-membered ring is substituted with at least one R selected from the group consisting of methyl claim 15 , isopropyl and tert-butyl.24. The precatalyst of claim 15 , wherein:(i) the 1- or 3-position of the 5-membered ring is substituted with R, or(ii) the 2-position of the 5-membered ring is substituted with R.25. (canceled)26. (canceled)27. The precatalyst of claim 15 , wherein L is selected from the group consisting of:(i) a ligand selected from the group consisting of 1,3-bis(2,6-diisopropyl phenyl)-1,3-dihydro-2H-imidazol-2-ylidene and 1,3-bis(2,6-bis-(diphenylmethyl)-4-methoxyphenyl)imidazol-2-ylidene;(ii) a monodentate phosphine ligand; and(iii) a bidentate phosphine ligand.28. (canceled)29. The precatalyst of claim ...

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Номер записи: 37
20-02-2020 дата публикации

PROCESS FOR THE PREPARATION OF ALPH-FUNCTIONALIZED KETONES

Номер: US20200055806A1
Автор: Loerzer Thomas, Sommerlade Reinhard
Принадлежит:

The present invention refers to a process for the preparation of an α-functionalized ketone, an α-functionalized ketone obtained by said process, a photopolymerizable composition comprising the α-functionalized ketone and at least one photopolymerizable unsaturated compound, a method of preparing an article, an article obtained by said method, as well as the use of the α-functionalized ketone or the photopolymerizable composition as photoinitiator. 2. The process according to claim 1 , wherein Rand Rare the same.3. The process according to claim 2 , wherein Rand Rare selected from H and linear or branched C-C-alkyl.4. The process according to claim 1 , wherein Rand Rare different and are independently selected from H and linear or branched C-C-alkyl.5. The process according to claim 1 , wherein Rand Rform C-C-cycloalkyl together with the connecting C atom.6. The process according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rand Rare the same.7. The process according to claim 6 , wherein R claim 6 , R claim 6 , R claim 6 , Rand Rare selected from H and linear or branched C-C-alkyl.8. The process according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , Rand Rare different and at least one of them is selected from linear or branched C-C-alkyl claim 1 , linear or branched C-C-alkenyl claim 1 , C-C-alkoxy claim 1 , C-C-alkenyloxy claim 1 , C-C-alkenylarylalkoxy or N(R)or SRwith Rbeing selected from linear or branched C-C-alkyl or linear or branched C-C-alkenyl or Rform a C-C-alicyclic system together with the connecting N atom.9. The process according to claim 1 , wherein one of R claim 1 , R claim 1 , R claim 1 , Rand Ris linear or branched C-C-alkenyl C-C-alkoxy claim 1 , C-C-alkenyloxy claim 1 , C-C-alkenylarylalkoxy claim 1 , or N(R)or SRwith Rbeing selected from linear or branched C-C-alkyl or linear or branched C-C-alkenyl or Rform a C-C-alicyclic system together with the connecting N atom; and the remaining ones are independently selected ...

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Номер записи: 38
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: 39
27-02-2020 дата публикации

MICROBIOCIDAL PHENYLAMIDINE DERIVATIVES

Номер: US20200060275A1
Автор: Matthias WEISS, Sarah SULZER-MOSSE
Принадлежит: SYNGENTA PARTICIPATIONS AG

Compounds of the formula (I), wherein R, R, R, Rand Rare as defined in claim . Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi. 2. A compound according to wherein Rand Rare each independently selected from C-Calkyl and C-Ccycloalkyl.3. A compound according to wherein Ris hydrogen claim 1 , halogen claim 1 , C-Calkyl or C-Ccycloalkyl.4. A compound according to wherein Ris C-Chaloalkyl.5. A compound according to wherein Ris C-Ccycloalkyl wherein the cycloalkyl is substituted with 1 to 3 substituents independently selected from cyano claim 1 , halogen claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , C-Ccycloalkyloxy claim 1 , C-Calkenyloxy claim 1 , C-Calkynyloxy claim 1 , phenyloxy claim 1 , ═N—OR; or Ris C-Calkyl wherein the alkyl is substituted with 1 to 2 substituents independently selected from cyano claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , C-Ccycloalkyloxy claim 1 , C-Calkenyloxy claim 1 , C-Calkynyloxy claim 1 , phenyloxy (wherein the phenyl is optionally substituted with one to three Rgroups) claim 1 , pyridinyloxy (wherein the pyridinyl is optionally substituted with one or two Rgroups) claim 1 , Si(C-Calkyl)C-Calkoxy claim 1 , phenyl(C-C)alkyloxy (wherein the phenyl is optionally substituted with one to three Rgroups) claim 1 , ═N—OR claim 1 , —O—N═C(R)(R) claim 1 , —N(OR)R claim 1 , wherein each Ris independently selected from fluoro claim 1 , chloro claim 1 , cyano claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Ccycloalkyl claim 1 , C-Chalocycloalkyl claim 1 , C-Calkoxy claim 1 , C-Chaloalkoxy claim 1 , C-Ccycloalkyloxy claim 1 , C-Calkylthio claim 1 , C-Chaloalkylthio claim 1 , C- ...

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Номер записи: 40
28-02-2019 дата публикации

ALPHA-TRUXILLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF

Номер: US20190062261A1
Автор: Deutsch Dale, Elmes Matthew, Hu Kongzhen, Kaczocha Martin, Ojima Iwao, TONG Simon, Yan Su
Принадлежит: The Research Foundation for The State University of New York

The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure: Formula (I) 3. The compound of claim 1 , wherein when one of Ror Ris —C(═O)OH and R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each H claim 1 , then the other of Ror Ris other than —C(═O)ORwhere Ris tolyl claim 1 , 1-naphthalene or 2-naphthalene claim 1 , or —C(═O)O-alkyl-Rwhere the alkyl is a branched Calkyl and the Ris phenyl.4. The compound of claim 1 , wherein when one of Ror Ris —C(═O)OH and the other of Ror Ris —C(═O)ORwhere Ris 1-naphthalene or 2-naphthalene claim 1 , then one of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris other than —H; or{'sub': 1', '2', '1', '2', '13', '13', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12, 'wherein when one of Ror Ris —C(═O)OH and the other of Ror Ris —C(═O)ORwhere Ris 1-naphthalene or 2-naphthalene, then two of R, R, R, R, R, R, R, R, Rand Ris other than —H; or'}{'sub': 1', '2', '1', '2', '13', '13', '3', '4', '5', '6', '7', '8', '9', '10', '11', '12, 'herein when one of Ror Ris —C(═O)OH and the other of Ror Ris —C(═O)ORwhere Ris 1-naphthalene or 2-naphthalene, then four of R, R, R, R, R, R, R, R, Rand Ris other than —H.'}56.-. (canceled)7. The compound of claim 1 ,wherein{'sub': 1', '2', '13, 'claim-text': {'sub': '13', 'wherein Ris cycloalkyl, aryl or heteroaryl; and'}, 'one of Ror Ris —C(═O)OR,'}{'sub': 1', '2, 'the other of Ror Ris —C(═O)OH.'}8. The compound of claim 1 ,wherein{'sub': 1', '2', '14, 'claim-text': {'sub': 14', '3, 'wherein Ris CF, cycloalkyl, aryl or heteroaryl; and'}, 'one of Ror Ris —C(═O)O-alkyl-R,'}{'sub': 1', '2, 'the other of Ror Ris —C(═O)OH.'}910.-. (canceled)117. The compound of claim 1 , wherein the aryl or heteroaryl is a substituted aryl or heteroaryl claim 1 , wherein ...

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Номер записи: 41
17-03-2022 дата публикации

PLASMA ETCHING METHOD AND PLASMA ETCHING APPARATUS

Номер: US20220084835A1
Автор: Fukumizu Hiroyuki, IINO Daiki, KUBOI Shuichi
Принадлежит: Kioxia Corporation

A plasma etching method according to an embodiment is a method for etching a silicon-containing film by using plasma of a fluorocarbon gas. The fluorocarbon gas includes at least one selected from a first fluorocarbon which has a main chain of six or more carbons bonded in a linear manner, the main chain having a structure of single bond and double bond alternately joined, a second fluorocarbon which has a main chain of six or more carbons bonded in a linear manner, the main chain having a structure of single bond and triple bond alternately joined, and a third fluorocarbon which has a main chain of five or more carbons bonded in a linear manner, the main chain having a structure which includes double bond and triple bond. 1. A plasma etching method , comprising:etching a silicon-containing film by using plasma of a fluorocarbon gas, whereinthe fluorocarbon gas includes a fluorocarbon which has a main chain of six or more carbons bonded in a linear manner, the main chain having a structure of single bond and double bond alternately joined or single bond and triple bond alternately joined.2. The method according to claim 1 , whereina ratio of carbon to fluorine of the fluorocarbon is equal to or larger than 0.75.3. The method according to claim 1 , whereinthe fluorocarbon gas includes the fluorocarbon which has the main chain of six or more carbons bonded in the linear manner, the main chain having the structure of single bond and double bond alternately joined, and{'sub': x1', 'y1, 'b': 1', '1', '1', '1', '1, 'the fluorocarbon has, regarding carbon and fluorine, a composition represented by a general formula: CF, wherein x and y are numbers satisfying x≥6 and y≥x+2.'}5. The method according to claim 1 , whereinthe fluorocarbon gas includes the fluorocarbon which has the main chain of six or more carbons bonded in the linear manner, the main chain having the structure of single bond and triple bond alternately joined, and{'sub': x2', '2, 'b': 2', '2', '2', '2, 'the ...

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Номер записи: 42
29-05-2014 дата публикации

Penta/hexamethyl-3,4,5,8-tetrahydro-1(2h)-naphthalenone derivatives with aromatic notes

Номер: US20140148376A1
Автор: Charles Fehr
Принадлежит: FIRMENICH SA

The present invention relates to compounds of Formula (I), wherein the dotted line represents a carbon-carbon single or double bond and R represents a hydrogen atom or a methyl group; which are useful perfuming ingredients to impart odor notes of the musky-earthy and woody, aromatic-fresh type.

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Номер записи: 43
15-03-2018 дата публикации

Peptidomimetics and Methods of Using the Same

Номер: US20180072677A1
Автор: Bender Aaron, Harland Aubrie, Henry Sean, Montgomery Deanna, Mosberg Henry, Nastase Anthony
Принадлежит:

Disclosed herein are compounds useful for modulating the mu-opioid receptor (“MOR”) and/or delta-opioid receptor (“DOR”), and methods of using these compounds to treat diseases and conditions, such as pain. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: 2. The compound of claim 1 , wherein A is formula (B).38.-. (canceled)10. The compound of claim 1 , wherein A is formula (C).11. (canceled)1317.-. (canceled)19. The compound of claim 1 , wherein A is formula (D).20. The compound of claim 19 , wherein:{'sup': '1', '(a) at least one J is CR; or'}{'sup': '1', '(b) each J is CR; or'}{'sup': '3', '(c) at least one J is NR; or'}{'sup': 1', '3, '(d) at least one J is CRand at least one other J is NR.'}2129.-. (canceled)3133.-. (canceled)3538.-. (canceled)39. The compound of claim 1 , wherein A is formula (C) or formula (D) claim 1 , and Ris(a) H; or(b) methyl or propyl; or{'sub': 3', '0-3, 'sup': 4', '4', '4, '(c) CalkyleneC(O)R, or CalkyleneC(O)OR, and Ris methyl, ethyl, propyl, phenyl, or benzyl; or'}(d) absent.4044.-. (canceled)45. The compound of claim 1 , wherein:{'sup': '2', 'sub': '3', '(a) at least one Ris CH; or'}{'sup': '2', '(b) at least one Ris H; or'}{'sup': '2', '(c) each Ris H.'}4647.-. (canceled)48. The compound of claim 1 , wherein Ris H claim 1 , methyl claim 1 , or cyclopropyl.49. (canceled)50. The compound of claim 1 , wherein each Rindependently is H claim 1 , CH claim 1 , or Cl.51. (canceled)52. The compound of claim 1 , wherein Ris H claim 1 , OH claim 1 , OCH claim 1 , Cl claim 1 , or C(O)NH.53. (canceled)55. (canceled)56. A pharmaceutical formulation comprising the compound of and a pharmaceutically acceptable excipient.57. A method of modulating the MOR claim 1 , the DOR claim 1 , the KOR claim 1 , or any combination thereof in a cell claim 1 , comprising contacting the cell with the compound of claim 1 , in an amount effective to modulate MOR claim 1 , DOR claim 1 , KOR claim 1 , or any ...

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Номер записи: 44
05-03-2020 дата публикации

Method for Preparing Levobunolol Hydrochloride

Номер: US20200071259A1
Автор: Feng Dongxiang, Tao Lianzhi, XU Weiming, Zhang Pengfei
Принадлежит:

The present invention provides a method for preparing levobunolol hydrochloride. In the present invention S-1-tert-butyl-epoxy methylamine is subjected to a substitution reaction with 5-hydroxy-1-tetralone, and acidified to obtain the target product levobunolol hydrochloride. The method provided by the present invention greatly improves the regioselectivity of the reaction, avoids the occurrence of side reactions, and effectively improves the yield and optical purity of levobunolol hydrochloride, with the yield being 87.3%, and the ee value being over 99%. 1. A method for preparing levobunolol hydrochloride , comprising the following steps:mixing 5-hydroxy-1-tetralone with S-1-tert-butyl-epoxymethylamine, an alkaline agent and a solvent, to obtain S-5-(3′-tert-butylamino-2′-hydroxy)-propoxy-3,4-dihydro-1(2H)tetralone through a substitution reaction; andacidifying S-5-(3′-tert-butylamino-2′-hydroxy)-propoxy-3,4-dihydro-1(2H)tetralone to give levobunolol hydrochloride;wherein the method for preparing 5-hydroxy-1-tetralone comprises the following steps:mixing 1,5-dihydroxynaphthalene, a metal catalyst, a reducing agent and an alcohol-water solven to obtain 5-hydroxy-1-tetralone through a reduction reaction;wherein the reducing agent comprises one or more of ammonium formate, sodium formate, potassium formate, formic acid and hydrazine hydrate: and the molar ratio of the reducing agent to 1,5-dihydroxynaphthalene is (1-3):1.2. (canceled)3. The preparation method of claim 2 , wherein the metal catalyst comprises palladium on carbon or raney nickel; and the mass of the metal catalyst is 0.5% to 10% by mass of 1 claim 2 ,5-dihydroxynaphthalene.4. (canceled)5. The preparation method of claim 2 , wherein the alcohol compound in the alcohol-water solvent comprises one or more of methanol claim 2 , ethanol claim 2 , n-propanol claim 2 , isopropanol claim 2 , n-butanol claim 2 , isobutanol and sec-butanol; the mass ratio of the alcohol compound to water in the alcohol-water ...

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Номер записи: 45
05-03-2020 дата публикации

METHODS FOR MAKING QUINOLINYLDIAMINES

Номер: US20200071344A1
Автор: Canich Jo Ann M., Goryunov Georgy P., Hagadorn John R., SAMSONOV Oleg V., Sharikov Mikhail I., Titone Michelle E., Uborsky Dmitry Dmitry, VOSKOBOYNIKOV Alexander Z.
Принадлежит:

The present disclosure provides methods for making quinolinyldiamine products from quinolinyl starting materials. In addition, the quinolinyldiamines can be used as ligands or ligand precursors for catalysts, e.g. for use in olefin polymerization. 2. The method of claim 1 , wherein introducing comprises:mixing the acid solution with the compound represented by Formula C or Formula K to form a first mixture;mixing the nitrite with the first mixture to form a second mixture; andmixing the phosphorous oxoacid with the second mixture to form a third mixture.3. The method of claim 1 , further comprising contacting the compound represented by Formula D or Formula L with an organic solvent.4. The method of claim 3 , wherein the organic solvent is an alcohol.5. The method of claim 1 , wherein the acid solution is a 2M to 6M solution of HCl.6. The method of claim 1 , wherein the nitrite is sodium nitrite claim 1 , potassium nitrite claim 1 , or mixtures thereof.7. The method of claim 1 , wherein the phosphorous oxoacid is hypophosphorous acid.8. The method of claim 1 , further comprising:{'sub': '4', 'introducing TiCland an aniline to the compound represented by Formula D or Formula L.'}9. The method of claim 8 , wherein introducing comprises:{'sub': '4', 'mixing the TiClwith the aniline to form a fourth mixture;'}heating the fourth mixture at a temperature of from about 30° C. to about 120° C.;mixing the compound represented by Formula D or Formula L to form a fifth mixture;heating the fifth mixture at a temperature of from about 30° C. to about 120° C.; andobtaining a dried product from the fifth mixture.10. The method of claim 9 , further comprising introducing the dried product to a reducing agent and an acid.11. The method of claim 10 , wherein:{'sub': 4', '3', '4, 'the reducing agent is selected from NaBH, NaBHCN, and LiAlH, and'}the acid is acetic acid.13. The method of claim 12 , further comprising contacting the compound represented by Formula E or Formula M with an ...

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Номер записи: 46
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: 47
18-03-2021 дата публикации

BENZOANNULENE DERIVATIVES AS ANTIVIRAL AGENTS

Номер: US20210078937A1
Автор: Ahmed Syed Kaleem, Augelli-Szafran Corinne E., Pathak Ashish Kumar, Suto Mark J.
Принадлежит:

The present disclosure is concerned with benzoannulene compounds that are capable of inhibiting a viral infection and methods of treating viral infections such as, for example, chikungunya, Venezuelan equine encephalitis, dengue, influenza, and zika, using these compounds. 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 compound of claim 1 , wherein m is 0.3. The compound of claim 1 , wherein n is 0 and Ris not hydrogen.4. The compound of claim 1 , wherein each of m and n is 0.5. The compound of claim 4 , wherein Ris not hydrogen.6. The compound of claim 1 , wherein Ris selected from —OH and C1-C4 alkoxy.7. The compound of claim 1 , wherein Ris C2-C5 heteroaryl substituted with 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3 groups independently selected from halogen claim 1 , —CN claim 1 , —NH claim 1 , —OH claim 1 , C1-C4 alkyl claim 1 , C1-C4 haloalkyl claim 1 , C1-C4 cyanoalkyl claim 1 , C1-C4 hydroxyalkyl claim 1 , C1-C4 alkoxy claim 1 , C1-C4 alkylamino claim 1 , (C1-C4)(C1-C4) dialkylamino claim 1 , (C1-C4 alkyl)Ar claim 1 , and Ar.8. The compound of claim 7 , wherein Ris selected from pyrazolyl claim 7 , thiazolyl claim 7 , and pyridinyl.12. The compound of claim 1 , wherein each of Rand Rare covalently bonded together and claim 1 , together with the intermediate atoms claim 1 , comprise a 3- to 6-membered heterocycloalkyl substituted with 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3 groups independently selected from halogen claim 1 , —CN claim 1 , —NH claim 1 , —OH claim 1 , C1-C4 alkyl claim 1 , C1-C4 haloalkyl claim 1 , C1-C4 cyanoalkyl claim 1 , C1-C4 hydroxyalkyl claim 1 , C1-C4 alkoxy claim 1 , C1-C4 alkylamino claim 1 , and (C1-C4)(C1-C4) dialkylamino.18. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound of and a pharmaceutically acceptable carrier.19. A method for the treatment of a viral infection ...

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Номер записи: 48
14-03-2019 дата публикации

SUBSTITUTED BICYCLIC COMPOUNDS

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

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

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Номер записи: 49
22-03-2018 дата публикации

New bi-aromatic propynyl compounds, pharmaceutical and cosmetic compositions containing them and uses thereof

Номер: US20180079707A1
Автор: Thibaud Portal
Принадлежит: Galderma Research and Development SNC

The invention relates to new compounds of the general formula (I): as well as the use thereof in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, in particular), or in the use of cosmetic compositions.

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Номер записи: 50
25-03-2021 дата публикации

AMIDE PRODRUGS OF SMALL MOLECULE NUCLEAR RECEPTOR MODULATORS

Номер: US20210087137A1
Автор: FERRARA Skylar J., Scanlan Thomas S.
Принадлежит: OREGON HEALTH & SCIENCE UNIVERSITY

Provided herein are novel amide prodrug forms of pharmaceutically active agents useful for central nervous system disorders. 3. A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier or excipient.4. The pharmaceutical composition of claim 1 , wherein the compound is selected from the group of compounds in claim 1 , or a pharmaceutically acceptable salt thereof.5. The use of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in the preparation of a medicament.6. The use of claim 1 , wherein the compound used in the preparation of a medicament is selected from the group of compounds in claim 1 , or a pharmaceutically acceptable salt thereof. The present invention relates to novel amide prodrug forms of Central Nervous System drugs with enhanced ability to complete blood-brain barrier passage.Nuclear receptor modulators include receptors for steroid hormones, lipophilic vitamins, sterols, and bile acids are targets for an important class of therapeutics of great therapeutic interest, encompassing 10-15% of the new drugs approved by the U.S. Food and Drug Administration. Among the most significant areas of interest are central nervous system disorders, including Alzheimer's Disease, Parkinson's Disease, demylenation disorders, and glioblastomas.While nuclear receptor modulators exhibit potent therapeutic effects, many also feature deleterious effects from receptor engagement in the periphery. There remains a need for therapeutic compounds with blood-brain barrier passage ability.Provided herein are novel amide prodrugs of pharmaceutically active compounds useful in the treatment of central nervous system (CNS) disorders.Most nuclear receptor ligands are non-polar small molecules with functional groups for target engagement with the desired receptor. A common functional group is the carboxylic acid, ...

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Номер записи: 51
28-03-2019 дата публикации

FUNCTIONALIZED BENZAMIDE DERIVATIVES AS ANTIVIRAL AGENTS AGAINST HBV INFECTION

Номер: US20190092720A1
Автор: BLOCK Timothy M., Du Yanming, Guo Ju-Tao, Xu Xiaodong
Принадлежит:

Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as pregenomic RNA encapsidation inhibitors, useful for the treatment of Hepatitis B virus (HBV) infection. 2. The compound of claim 1 , wherein X is CH and n is 1.3. The compound of claim 1 , wherein X is S and n is 0.4. The compound of claim 1 , wherein m is 0.5. The compound of claim 1 , which is selected from the group consisting of:3,4-Dihydro-2H-benzo[b][1,4]dioxepine-6-carboxylic acid (3-chloro-phenyl)-amide;3,4-Dihydro-2H-benzo[b][1,4]dioxepine-6-carboxylic acid (3,4-difluoro-phenyl)-amide;3,4-Dihydro-2H-benzo[b][1,4]dioxepine-6-carboxylic acid (3-chloro-4-fluoro-phenyl)-amide;or a hydrate, solvate, or salt thereof.6. A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and at least one compound of .7. A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and at least one compound selected from the group consisting of:3,4-Dihydro-2H-benzo[b][1,4]dioxepine-6-carboxylic acid (3-chloro-phenyl)-amide;3,4-Dihydro-2H-benzo[b][1,4]dioxepine-6-carboxylic acid (3,4-difluoro-phenyl)-amide;3,4-Dihydro-2H-benzo[b][1,4]dioxepine-6-carboxylic acid (3-chloro-4-fluoro-phenyl)-amide;or a hydrate, solvate, or salt thereof.8. A method for treating or ameliorating a disease or disorder that involves pregenomic RNA encapsidation claim 1 , the method comprising administering to a subject a therapeutically effective amount of at least one compound of .9. The method of claim 8 , wherein the disease or disorder is hepatitis B.10. The method of claim 8 , wherein the at least one compound is administered as part of a pharmaceutical composition further comprising at least one pharmaceutically acceptable excipient.11. A method of treating or ameliorating hepatitis B in a subject infected with hepatitis B virus claim 1 , the method comprising administering to the subject a therapeutically amount of at least one ...

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Номер записи: 52
14-04-2016 дата публикации

N-(4-(bis(4-(dimethylamino)phenyl)methylene)-8-(dimethylamino)

Номер: US20160102048A1
Автор: Jack Arbiser
Принадлежит: EMORY UNIVERSITY

This disclosure relates to N-(4-(bis(4-(dimethylamino)phenyl)methylene)-8-(dimethylamino)naphthalen-1(4H)-ylidene)-N-methylmethanaminium, derivatives, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I. In certain embodiments, the disclosure relates to methods of treating or preventing Nox related diseases and conditions comprising administering an effective amount of compounds disclosed herein to a subject in need thereof. In certain embodiments, the Nox related disease or condition is cancer.

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Номер записи: 53
26-03-2020 дата публикации

POLYMERIZABLE ABSORBERS OF UV AND HIGH ENERGY VISIBLE LIGHT

Номер: US20200095187A1
Автор: Arnold Stephen C., Mahadevan Shivkumar, Maharvi Ghulam
Принадлежит:

Described are polymerizable high energy light absorbing compounds of formula I: 2. The compound of wherein the compound contains one —Y—Pgroup.3. The compound of wherein Ris —Y—P.4. The compound of wherein Rand Rare each H.5. The compound of wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each H.6. The compound of wherein X is CH claim 1 , O claim 1 , NH claim 1 , or NCH.7. The compound of wherein Y comprises: C-Calkylene claim 1 , alkyleneoxy claim 1 , C-Coxaalkylene claim 1 , C-Cthiaalkylene claim 1 , C-Calkylene-ester-C-Calkylene claim 1 , C-Calkylene-amide-C-Calkylene claim 1 , or C-Calkylene-amine-C-Calkylene.8. The compound of wherein Pcomprises: styryl claim 1 , vinyl carbonate claim 1 , vinyl ether claim 1 , vinyl carbamate claim 1 , N-vinyl lactam claim 1 , N-vinylamide claim 1 , (meth)acrylate claim 1 , or (meth)acrylamide.9. A compound of that is:2-((1-amino-8-oxo-5,6,7,8-tetrahydronaphthalen-2-yl)oxy)ethyl methacrylate;N-(2-((1-amino-8-oxo-5,6,7,8-tetrahydronaphthalen-2-yl)oxy)ethyl)methacrylamide;N-(2-((1-amino-8-oxo-5,6,7,8-tetrahydronaphthalen-2-yl)oxy)ethyl)-N-methylmethacrylamide;2-((5-amino-4-oxo-1,2,3,4-tetrahydroquinolin-6-yl)oxy)ethyl methacrylate;N-(2-((5-amino-4-oxo-1,2,3,4-tetrahydroquinolin-6-yl)oxy)ethyl)methacrylamide;N-(2-((5-amino-4-oxo-1,2,3,4-tetrahydroquinolin-6-yl)oxy)ethyl)-N-methylmethacrylamide;2-((5-amino-1-methyl-4-oxo-1,2,3,4-tetrahydroquinolin-6-yl)oxy)ethyl methacrylate;N-(2-((5-amino-1-methyl-4-oxo-1,2,3,4-tetrahydroquinolin-6-yl)oxy)ethyl)methacrylamide;N-(2-((5-amino-1-methyl-4-oxo-1,2,3,4-tetrahydroquinolin-6-yl)oxy)ethyl)-N-methylmethacrylamide;2-((5-amino-4-oxochroman-6-yl)oxy)ethyl methacrylate;N-(2-((5-amino-4-oxochroman-6-yl)oxy)ethyl)methacrylamide; orN-(2-((5-amino-4-oxochroman-6-yl)oxy)ethyl)-N-methylmethacrylamide.10. An ophthalmic device that is a free radical reaction product of a reactive mixture comprising: one or more monomers suitable for making the ophthalmic device; and a ...

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Номер записи: 54
08-04-2021 дата публикации

NOVEL REXINOID COMPOUNDS AND METHODS OF USING REXINOID COMPOUNDS FOR TREATING METABOLIC DISORDERS AND CANCER

Номер: US20210101861A1
Автор: Atigadda Venkatram Reddy, Brouillette Wayne J., Grubbs Clinton J., Kim Jeonga, Muccio Donald D.
Принадлежит: THE UAB RESEARCH FOUNDATION

Novel rexinoid compounds are provided herein. Also provided herein are methods of using the compounds to treat disorders, such as metabolic disorders, diabetes, insulin resistance, glucose intolerance, obesity, steatosis, inflammation, and/or cancer. 10. (canceled)1218-. (canceled)19. A pharmaceutical composition claim 1 , comprising a compound of and a pharmaceutically acceptable carrier.20. A method of treating or preventing a metabolic disorder in a subject claim 1 , comprising administering to a subject an effective amount of a compound of .21. The method of claim 20 , wherein administering the compound provides a glucose-lowering effect claim 20 , an insulin-sensitizing effect claim 20 , or a plasma triglyceride lowering effect.22. (canceled)23. (canceled)24. A method of treating or preventing insulin resistance claim 1 , glucose intolerance claim 1 , obesity claim 1 , steatosis or inflammation in a subject claim 1 , comprising administrating to a subject in thereof an effective amount of a compound of .25. The method of claim 20 , wherein the subject is a rodent or human claim 20 , obese claim 20 , morbidly obese claim 20 , pre-diabetic claim 20 , or diabetic.2629-. (canceled)30. The method of claim 20 , wherein the compound is administered orally claim 20 , topically claim 20 , intranasally claim 20 , intravenously claim 20 , subcutaneously claim 20 , intradermally claim 20 , transdermally intramucosally intramuscularly claim 20 , by inhalation spray claim 20 , rectally claim 20 , nasally claim 20 , sublingually claim 20 , buccally claim 20 , vaginally or via an implanted reservoir.31. (canceled)32. A method of treating or preventing cancer in a subject claim 1 , comprising administering to a subject an effective amount of a compound of .3336-. (canceled)37. A kit for treating a metabolic disorder claim 1 , insulin resistance claim 1 , glucose intolerance claim 1 , obesity claim 1 , steatosis claim 1 , inflammation claim 1 , or cancer claim 1 , wherein the ...

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Номер записи: 55
02-06-2022 дата публикации

Monocarbonyl ruthenium and osmium catalysts

Номер: US20220168720A1
Автор: Salvatore Baldino, Steven GIBOULOT, Walter Baratta
Принадлежит: Innovation Factory SRL, UNIVERSITÀ DEGLI STUDI DI UDINE

The invention relates to monocarbonyl complexes of ruthenium and osmium with bi- and tridentate nitrogen and phosphine ligands. The invention relates to methods for preparing these complexes and the use of these complexes, isolated or prepared in situ, as catalysts for reduction reactions of ketones and aldehydes both via transfer hydrogenation or hydrogenation with hydrogen.

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Номер записи: 56
18-04-2019 дата публикации

Synthetic retinoids for use in rar mediated conditions

Номер: US20190112272A1
Автор: Andrew Whiting, David Chisholm, Iain Greig, Peter MCCAFFERY, Roy Valentine, Thabat KHATIB
Принадлежит: HIGH FORCE RESEARCH Ltd, University of Aberdeen, University of Durham

There are described novel compounds of formula I: in which R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are each as herein defined, for use in the treatment or alleviation of an RAR miated condition: and methods related thereto.

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Номер записи: 57
13-05-2021 дата публикации

COMPOUNDS AND SYNTHETIC METHODS FOR THE PREPARATION OF RETINOID X RECEPTOR-SPECIFIC RETINOIDS

Номер: US20210139404A1
Автор: Chandraratna Roshantha A., Jacks Thomas, Thompson Andrew, Vuligonda Vidyasagar Pradeep, Wade Peter
Принадлежит:

Provided herein are compounds useful for the preparation of compounds that have retinoid-like biological activity. Also provided herein are processes for the preparation of compounds that have retinoid-like biological activity. 2. The method of claim 1 , wherein Ris C-alkyl claim 1 , C-alkenyl claim 1 , or C-aryl.5. The method of claim 4 , wherein Ris C-alkyl claim 4 , C-alkenyl claim 4 , or C-aryl.7. The method of claim 1 , wherein treatment of the compound of Formula I with KOt-Bu is carried out under an inert atmosphere.8. The method of claim 1 , wherein the added Compound 32 is in a tetrahydrofuran or ether solvent.9. The method of claim 1 , further comprising quenching the reaction with water.10. The method of claim 9 , further comprising extracting the compound of Formula II with ethyl acetate.13. The method of claim 11 , wherein treatment of compound 12 with KOt-Bu is carried out under an inert atmosphere.14. The method of claim 11 , wherein the added Compound 32 is in a tetrahydrofuran or ether solvent.15. The method of claim 11 , further comprising quenching the reaction with water.16. The method of claim 15 , further comprising extracting Compound 37 with ethyl acetate. This application is a continuation of U.S. patent application Ser. No. 16/799,176, filed Feb. 24, 2020, now U.S. Pat. No. 10______, which is a continuation of U.S. patent application Ser. No. 16/194,141, filed Nov. 16, 2018, now U.S. Pat. No. 10,590,059, which claims priority to U.S. Provisional Patent Application No. 62/671,137, filed on May 14, 2018, and U.S. Provisional Patent Application No. 62/588,163, filed on Nov. 17, 2017. The entire content of each of these applications is incorporated herein by reference.This invention was made with government support under Grant Number 2R44AI112512-02A1 awarded by the National Institutes of Health. The government has certain rights in the invention.Compounds which have retinoid-like biological activity have been described. Preclinical studies ...

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Номер записи: 58
03-05-2018 дата публикации

General purpose plasticizers based on naphthalic acid diesters

Номер: US20180118660A1
Автор: Christine A. Costello, Christopher M. Evans, James R. Lattner, Stephen T. COHN
Принадлежит: ExxonMobil Research and Engineering Co

A diester of a fused ring compound of the formula (I): wherein the R 1 to R 6 substituents are H or ester moieties having C 1 to C 20 alkyl chains, but when both fused rings are aromatic and R 3 and R 4 are ester moieties, the alkyl chains are not C 5 or C 8 , and polymer compositions containing the fused ring compound.

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Номер записи: 59
03-05-2018 дата публикации

MUTANT KRAS INHIBITORS

Номер: US20180118761A1
Автор: Houghten Richard A., Li Yangmei, Sebti Said M.
Принадлежит:

Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling. 1. A method for treating cancer in a subject , comprising administering to the subject a compound that inhibits the binding of GTP to oncogenic mutant KRas.2. The method of claim 1 , wherein the compound is an allosteric inhibitor of the ability of GTP to bind mutant KRas.4. The method of claim 3 , wherein Ris alkyl.5. The method of claim 3 , wherein Ris unsubstituted phenyl or phenyl substituted.8. The method of claim 3 , wherein Ris unsubstituted Calkyl or Calkyl substituted with hydroxyl claim 3 , guanidinyl claim 3 , phenyl claim 3 , phenol claim 3 , tolyl claim 3 , or heteroaryl.9. The method of claim 3 , wherein the compound is any one of the compounds in claim 3 , claim 3 , or .13. The compound of claim 12 , wherein Ris alkyl.14. The compound of claim 12 , wherein Ris unsubstituted phenyl or phenyl substituted.17. The compound of claim 12 , wherein Ris unsubstituted Calkyl or Calkyl substituted with hydroxyl claim 12 , guanidinyl claim 12 , phenyl claim 12 , phenol claim 12 , tolyl claim 12 , or heteroaryl.18. The compound of claim 12 , wherein the compound is any one of the compounds in claim 12 , claim 12 , or .21. A pharmaceutical composition claim 12 , comprising a therapeutically effective amount of a compound of in a pharmaceutically acceptable excipient. This application claims the benefit of priority to U.S. Provisional Application 62/152,333, filed Apr. 24, 2015, which is hereby incorporated by reference herein in its entirety.Ras activation is catalyzed by GEFs such as SOS that exchange bound GDP for GTP, whereas Ras inactivation is catalyzed by GAPs leading to the hydrolysis of GTP to GDP. Oncogenic mutations in KRas impair GTP hydrolysis, leading to a constitutively activated, GTP- ...

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Номер записи: 60
16-04-2020 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS OF USE

Номер: US20200115320A1
Автор: Booth Raymond G.
Принадлежит: University of Florida Research Foundation, Incorporated

The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs. 18-. (canceled)1014-. (canceled)16. (canceled)17. A composition comprising a compound of claim 15 , or salt hydrate or solvate thereof claim 15 , and a pharmaceutically acceptable carrier.18. A method of making a composition of comprising a compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , and a pharmaceutically acceptable carrier.19. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-halophenyl optionally substituted with 1 claim 15 , 2 claim 15 , or 3 independent halo claim 15 , alkoxy claim 15 , or CF.20. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-haloalkylphenyl optionally substituted with 1 claim 15 , 2 claim 15 , or 3 independent halo claim 15 , alkoxy claim 15 , or CF.21. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-alkoxyphenyl optionally substituted with 1 claim 15 , 2 claim 15 , or 3 independent halo claim 15 , alkoxy claim 15 , or CF.22. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-halophenyl claim 15 , 3-haloalkylphenyl claim 15 , or 3-alkoxyphenyl.23. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-halophenyl.24. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-haloalkylphenyl.25. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-alkoxyphenyl.26. The compound of claim 15 , or salt claim 15 , hydrate or solvate thereof claim 15 , wherein Ris 3-chlorophenyl.27. The compound of claim 15 , or salt claim 15 , ...

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Номер записи: 61
16-04-2020 дата публикации

TETRALIN AND INDANE DERIVATIVES AND USES THEREOF

Номер: US20200115333A1
Автор: Greenhouse Robert, Harris, III Ralph New, Jaime-Figueroa Saul, Kress James M., Repke David Bruce, Stabler Russell Stephen
Принадлежит: Roche Palo Alto LLC

The application discloses pharmaceutical compounds of formula I useful for treating CNS diseases wherein m, s, RR, Rand Rare as defined herein. 2. The method of wherein m is 0 claim 1 , s is 1 claim 1 , Ris 3-fluoro claim 1 , Ris hydrogen and Ris acetyl claim 1 , aminocarbonyl or methylsulfonyl or a pharmaceutically acceptable salt.3. The method of wherein the compound is (R)-[6-(3-fluoro-benzenesulfonyl)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydro-naphthalen-1-ylmethyl]-urea or a pharmaceutically acceptable salt.4. The method of claim 3 , wherein the central nervous system disease state is depression.5. The method of claim 3 , wherein the central nervous system disease state is a memory disorder.6. The method of claim 3 , wherein the central nervous system disease state is Parkinson's disease. This Application is a Continuation of U.S. application Ser. No. 15/597,478, filed May 17, 2017, which is a Continuation of U.S. application Ser. No. 14/531,465, filed Nov. 3, 2014, which is a Continuation U.S. application Ser. No. 13/314,525, filed on Dec. 8, 2011, which is a Continuation of U.S. application Ser. No. 11/985,459, filed on Nov. 15, 2007, which is a continuation of U.S. patent application Ser. No. 11/315,706, filed Dec. 21, 2005, which claims the benefit under Title 35 U.S.C. 119(e) of U.S. Provisional Patent Application Ser. No. 60/638,030, filed Dec. 21, 2004, the disclosure of which is incorporated herein by reference in its entirety.This invention relates to substituted indane and tetralin compounds, and associated compositions, methods for use as therapeutic agents, and methods of preparation thereof.The actions of 5-hydroxytryptamine (5-HT) as a major modulatory neurotransmitter in the brain are mediated through a number of receptor families termed 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HTS, 5-HT6, and 5-HT7. Based on a high level of 5-HT6 receptor mRNA in the brain, it has been stated that the 5-HT6 receptor may play a role in the pathology and treatment of ...

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Номер записи: 62
16-04-2020 дата публикации

POLYCARBONATE RESIN COMPOSITION, MOLDED ARTICLE, POLYCARBONATE RESIN, AND END-CAPPING AGENT FOR POLYCARBONATE RESIN

Номер: US20200115496A1
Автор: Maruyama Hiroyoshi, Nakao Kimitaka, NII Yuusuke, SHIBASAKI Yuji
Принадлежит: MITSUBISHI GAS CHEMICAL COMPANY, INC.

A polycarbonate resin composition, a molded article, a polycarbonate resin, and an end-capping agent for polycarbonate resins are provided. The polycarbonate resin composition contains: a polycarbonate resin having a terminal structure represented by Formula (A) and having a viscosity average molecular weight from 1×10to 5×10, and a stabilizer. In Formula (A), Ris selected from the group consisting of a hydrogen atom, halogen atoms, linear alkyl groups having from 1 to 9 carbons, branched alkyl groups having from 3 to 9 carbons, linear alkenyl groups having from 2 to 9 carbons, branched alkenyl groups having from 3 to 9 carbons, and aryl groups having from 6 to 12 carbons; and Rto Rare each independently selected from the group consisting of a hydrogen atom, alkyl groups having from 1 to 9 carbons, and alkoxy groups having from 1 to 9 carbons. 4. The polycarbonate resin composition according to claim 1 , wherein the stabilizer is at least one type selected from the group consisting of thermal stabilizers and antioxidants.5. A molded article formed from the polycarbonate resin composition described in . The present invention relates to a polycarbonate resin composition, a molded article, a polycarbonate resin, and an end-capping agent for polycarbonate resins.Polycarbonate resins, represented by aromatic polycarbonate resins, are resins having excellent heat resistance, mechanical properties, and electrical properties, and are widely used in, for example, automotive materials, electrical and electronic device materials, various household electrical device materials, housing materials, and other materials for component production in industrial fields. In particular, flame-retardant aromatic polycarbonate resin compositions have been suitably used as members for office automation/information-processing equipment, such as a computer, a notebook computer, a mobile phone, a printer, a copying machine, or the like.Typically, as a method for imparting flame retardancy to an ...

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Номер записи: 63
10-05-2018 дата публикации

Compounds and Methods for Modulating Serotonin Receptors in the Periphery

Номер: US20180125798A1
Автор: Raymond G. Booth
Принадлежит: Northeastern University Boston

This invention relates to, in part, compositions and methods that are useful for, inter alia, the treatment of various diseases, including those linked to binding at a serotonin receptor in the GI tract.

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Номер записи: 64
10-05-2018 дата публикации

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20180127361A1
Автор: Last Stefaan Julien, Raboisson Pierre Jean-Marie Bernard, ROMBOUTS Geert, Vandyck Koen, Verschueren Wim Gaston
Принадлежит:

Inhibitors of HBV replication of Formula (I) 113-. (canceled)15. The compound of claim 14 , wherein Ris hydrogen.16. The compound of claim 14 , wherein Ris a 4-7 membered saturated ring optionally containing one or more heteroatoms each independently selected from the group consisting of O claim 14 , S and N claim 14 , said 4-7 membered saturated ring optionally substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 14 , halogen claim 14 , C-Calkyloxy claim 14 , C-Calkyloxycarbonyl claim 14 , C(═O)—C-Calkyl claim 14 , C-Calkyl claim 14 , OH claim 14 , CN claim 14 , CFH claim 14 , CFH and CF.17. The compound of claim 14 , wherein Ris C-Ccycloalkyl.18. The compound of claim 14 , wherein B is imidazolyl or thiazolyl claim 14 , each optionally substituted with one or more substituents each independently selected from the group consisting of hydrogen claim 14 , halogen claim 14 , C-Calkyl claim 14 , CN claim 14 , CFH claim 14 , CFH and CF.19. A compound of claim 14 , wherein at least one Ris fluoro claim 14 , and one other Ris selected from the group consisting of C-Calkyl claim 14 , C-Calkenyl claim 14 , CHFand cyclopropyl.20. A compound of claim 14 , wherein one Ris fluoro and one other Ris selected from methyl or CHF claim 14 , and wherein the location of said fluoro is on the para position related to the nitrogen(*) claim 14 , and the location of said methyl or CHFis on the meta position related to the nitrogen(*).21. The compound of claim 14 , wherein each Ris hydrogen.23. A pharmaceutical composition comprising at least one compound of and a pharmaceutically acceptable carrier.24. A product containing (a) at least one compound of claim 14 , and (b) an HBV inhibitor claim 14 , as a combined preparation for simultaneous claim 14 , separate or sequential use in the treatment of HBV infection.25. A method of preventing or treating an HBV infection in a subject in need thereof claim 14 , comprising administering ...

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Номер записи: 65
10-05-2018 дата публикации

NITRATED HYDROCARBONS, DERIVATIVES, AND PROCESSES FOR THEIR MANUFACTURE

Номер: US20180127435A1
Автор: Green George D., James Richard L., Swedo Raymond J., Tomlinson Ian A., Trauth Daniel M.
Принадлежит:

Provided is a process for the formation of nitrated compounds by the nitration of hydrocarbon compounds with dilute nitric acid. Also provided are processes for preparing industrially useful downstream derivatives of the nitrated compounds, as well as novel nitrated compounds and derivatives, and methods of using the derivatives in various applications. 2. The compound of selected from formula I-1.3. The compound of claim 2 , wherein Rand Rare unsubstituted.4. The compound of claim 2 , wherein the compound is selected from the group consisting of 3-nitrodecane claim 2 , 4-nitrodecane claim 2 , 5-nitrodecane claim 2 , 4-nitrotridecane claim 2 , 5-nitrotridecane claim 2 , 7-nitrotridecane claim 2 , 2-nitrotetradecane claim 2 , 3-nitrotetradecane claim 2 , 4-nitrotetradecane claim 2 , 5-nitrotetradecane claim 2 , 6-nitrotetradecane claim 2 , 7-nitrotetradecane claim 2 , 2-nitropentadecane claim 2 , 3-nitropentadecane claim 2 , 4-nitropentadecane claim 2 , 5-nitropentadecane claim 2 , 6-nitropentadecane claim 2 , 7-nitropentadecane claim 2 , 8-nitropentadecane claim 2 , 3-nitrohexadecane claim 2 , 4-nitrohexadecane claim 2 , 5-nitrohexadecane claim 2 , 6-nitrohexadecane claim 2 , 7-nitrohexadecane claim 2 , 8-nitrohexadecane claim 2 , 2-nitroheptadecane claim 2 , 3-nitroheptadecane claim 2 , 4-nitroheptadecane claim 2 , 5-nitroheptadecane claim 2 , 6-nitroheptadecane claim 2 , 7-nitroheptadecane claim 2 , 8-nitroheptadecane claim 2 , 9-nitroheptadecane claim 2 , 3-nitrooctadecane claim 2 , 4-nitrooctadecane claim 2 , 5-nitrooctadecane claim 2 , 6-nitrooctadecane claim 2 , 7-nitrooctadecane claim 2 , 8-nitrooctadecane claim 2 , and 9-nitrooctadecane.5. The compound of selected from formula II-1.6. The compound of claim 5 , wherein Ris a linear C-Calkyl; and Ris H claim 5 , linear C-Calkyl claim 5 , or CHOH.7. The compound of claim 5 , wherein Ris H or linear C-Calkyl claim 5 , and the total number of carbons in Rand R claim 5 , together with the carbon to which they are ...

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Номер записи: 66
27-05-2021 дата публикации

Organic Compound, Light-Emitting Element, Light-Emitting Device, Electronic Device, Display Device, and Lighting Device

Номер: US20210159410A1
Автор: Hashimoto Naoaki, KAWAKAMI Sachiko, SEO Satoshi, SUZUKI Tsunenori, TADA Anna, TAKITA Yusuke
Принадлежит: SEMICONDUCTOR ENERGY LABORATORY CO., LTD.

An object of one embodiment of the present invention is to provide a novel organic compound. The organic compound is a triarylamine derivative. The triarylamine derivative has an aryl group including a skeleton in which a naphthyl group is bonded to a naphthylene group. The other two aryl groups are each independently a phenyl group, a biphenyl group, or a terphenyl group. These groups may each have a substituent. As the substituent, an alkyl group having 1 to 6 carbon atoms or a cycloalkyl group having 3 to 6 carbon atoms can be selected. 5. A light-emitting device comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a hole-transport layer comprising the organic compound according to ;'}a light-emitting layer over the hole-transport layer; andan electron-transport layer over the light-emitting layer.6. An electronic device comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the light-emitting device according to ; and'}any one of a sensor, an operation button, a speaker and a microphone.7. Alighting device comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the light-emitting device according to ; and'}a housing. This application is a continuation of copending U.S. application Ser. No. 15/855,113, filed on Dec. 27, 2017 which is incorporated herein by reference.One embodiment of the present invention relates to a light-emitting element, a display module, a lighting module, a display device, a light-emitting device, an electronic device, and a lighting device. Note that one embodiment of the present invention is not limited to the above technical field. The technical field of one embodiment of the invention disclosed in this specification and the like relates to an object, a method, or a manufacturing method. Another embodiment of the present invention relates to a process, a machine, manufacture, or a composition of matter. Specific examples of the technical field of one embodiment of the present invention disclosed in this ...

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Номер записи: 67
10-05-2018 дата публикации

Antifungal Penicillium Strains, Fungicidal Extrolites Thereof, and Their Use

Номер: US20180127840A1
Автор: ANKE Heidrun, Jabs Thorsten, OPATZ Till, SANDJO Louis Pergaud, SCHUEFFLER Anja, SIEPE Isabella, THINES Eckhard
Принадлежит:

The present invention relates to fungal strains, which are a member of the genus and have antifungal activity, and to cell-free extracts of said strains, culture media obtainable by culturing said strains and extrolites produced by said strains, all of which have fungicidal activity. The present invention further relates to compositions comprising said strains, extracts, culture media and extrolites, and their uses in the agrochemical field and the field of controlling phytopathogenic fungi in particular. 1Penicillium. A strain selected from the group consisting of:a. strain IBWF104-06 as deposited with DSMZ under the deposit number DSM 27859; andb. strains having at least one identifying characteristic of said strain IBWF104-06.3Penicillium steckii. The strain of claim 1 , which is a strain.4. The strain of claim 3 , wherein the strain comprises an ITS sequence which is at least 95% identical to SEQ ID NO:1.5. The strain of claim 1 , which has antifungal activity.6Alternaria solani, Botrytis cinereaPhytophthora infestans.. The strain of claim 5 , which is active against a fungus selected from the group consisting of and7penicillium. A method of preparing the tanzawaic acid or salt of claim 1 , which method comprises culturing a strain selected from the group consisting of:a. strain IBWF104-06 as deposited with DSMZ under the deposit number DSM 27859; andb. strains having at least one identifying characteristic of said strain IBWF104-06.and recovering said tanzawaic acid or salt from the culture broth.8. A composition comprising the strain of .9. The composition of further comprising a pesticide.10. The composition of claim 9 , wherein the pesticide is a biopesticide.11. A method of controlling claim 1 , suppressing plant pathogens or preventing plant pathogen infection claim 1 , wherein the pathogens claim 1 , their habitat or the materials or plants to be protected against pathogen attack claim 1 , or the soil or propagation material are treated with an effective ...

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Номер записи: 68
17-05-2018 дата публикации

QUINONE COMPOUNDS FOR TREATING APE1 MEDIATED DISEASES

Номер: US20180133175A1
Автор: KELLEY Mark R., Wikel James H.
Принадлежит:

The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases. 129.-. (canceled)31. The compound of claim 30 , wherein R is methyl.32. The compound of claim 30 , wherein R is methoxy.33. The compound of claim 30 , wherein each Ris methyl or ethyl.34. The compound of claim 30 , wherein at least one Ris hydrogen.35. The compound of claim 30 , wherein at least one Ris alkyl.36. The compound of claim 30 , wherein one Ris alkyl claim 30 , and one Ris hydrogen.37. The compound of claim 30 , wherein Y is NROR.38. The compound of claim 30 , wherein Y is N(R).39. The compound of claim 30 , wherein both Rare methyl.40. The compound of claim 30 , wherein Ris C-Calkyl.41. The compound of claim 30 , wherein Ris Calkyl.42. The compound of claim 30 , wherein Ris n-nonyl.43. The compound of claim 30 , wherein Ris C-Calkyl.44. The compound of claim 30 , wherein Ris C-Calkyl.45. The compound of claim 30 , wherein Ris C-Calkyl.46. The compound of claim 30 , wherein Ris methyl.47. A pharmaceutical composition comprising one or more compounds of .48. The composition of claim 47 , further comprising one or more carriers claim 47 , or excipients claim 47 , or a combination thereof.49. A unit dose or unit dosage form composition comprising one or more compounds of for treating a disease responsive to Ape1 inhibition. This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 61/490,141, filed May 26, 2011, which is expressly incorporated by reference herein.The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.Apurinic/apyrimidic ...

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Номер записи: 69
17-05-2018 дата публикации

ACETYLENIC CYANOENONES AS THERAPEUTICS FOR INFLAMMATION AND CARCINOGENESIS

Номер: US20180134654A1
Автор: Dinkova-Kostova Albena, HONDA Tadashi, Li Wei, Zheng Suqing
Принадлежит:

The present invention provides a compound having the structure: 2. The compound of claim 1 , wherein{'sub': 1', '12', '2', '12', '2', '12, 'X is C-Calkyl, C-Calkenyl, C-Calkynyl, cyano, aryl, heteroaryl, alkylaryl, alkylheteroaryl, alkenylaryl, alkenylheteroaryl, alkynylaryl, alkynylheteroaryl, alkoxy, alkenyloxy, alkynyloxy, aryloxy, heteroaryloxy, acyl, alkylhydroxy, alkylamino, alkenylamino, alkynylamino, amido, carboxyl, or carboxyl ester, or forms an unsubstituted or substituted indane or tetralin with Y,'}Y is H or forms an unsubstituted or substituted indane or tetralin with X, or forms an unsubstituted or substituted monocycle with Z; and {'sub': 2', '2, 'wherein when X and Y are both H, then X is Calkenyl or Calkynyl,'}, 'Z is H or forms an unsubstituted or substituted monocycle with Y,'}or a salt or ester thereof.3. The compound of claim 1 , wherein{'sub': 1', '12', '2', '12', '2', '12, 'X is C-Calkyl, C-Calkenyl, C-Calkynyl, cyano, aryl, heteroaryl, alkylaryl, alkylheteroaryl, alkenylaryl, alkenylheteroaryl, alkynylaryl, alkynylheteroaryl, alkoxy, alkenyloxy, alkynyloxy, aryloxy, heteroaryloxy, acyl, alkylhydroxy, alkylamino, alkenylamino, alkynylamino, amido, carboxyl, or carboxyl ester, or forms an unsubstituted or substituted cyclobutyl; cyclopentyl, cyclohexyl or cycloheptyl with Y,'}Y is H or forms an unsubstituted or substituted cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl with X, or forms an unsubstituted or substituted monocycle with Z; and nm {'sub': 2', '2', '3', '2', '2', '2', '3', '3', '2', '3', '2, 'wherein when X and Y are both H, then X is Calkenyl or Calkynyl, and when Y is H forms a substituted cyclohexyl, cycloheptyl with X, the cyclohexyl is other than a trisubstituted cyclohexyl bearing CH, i-Pr and (CH)COCHgroups or CH, i-Pr and (CH)NH,'}, 'Z is H or forms an unsubstituted or substituted monocycle with Y,'}or a salt or ester thereof.4. The compound of claim 1 , wherein{'sub': 1', '12', '2', '12', '2', '12, 'X is C-Calkyl, C- ...

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Номер записи: 70
30-04-2020 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS

Номер: US20200131119A1
Автор: GÜVEN Nuri, NADIKUDI Monila, Smith Jason, WOOLLEY Krystel Lee
Принадлежит: University of Tasmania

The invention relates to compounds of Formula (I) and methods for their preparation. Also described are pharmaceutical compositions comprising a compound of Formula (I) and their use in the treatment or prevention of conditions associated with mitochondrial dysfunction. Formula (I) 2. A compound according to wherein Ris optionally substituted Caryl.3. A compound according to claim 1 , wherein Ris dimethoxy phenyl claim 1 , preferably 3 claim 1 ,4-dimethoxy phenyl.4. A compound according to wherein Ris H.5. A compound according to wherein Ris methyl.7. A pharmaceutical composition comprising a compound according to any one of the preceding claims.8. A pharmaceutical composition according to further comprising an additional active agent.9. A pharmaceutical composition according to wherein the additional active agent is an anti-diabetic agent.10. A method of treating or preventing a disease or disorder associated with mitochondrial dysfunction claim 8 , comprising administering to a person in need thereof claim 8 , a therapeutically effective amount of a compound according to or a pharmaceutical composition according to claim 8 ,wherein the disease or disorder associated with mitochondrial dysfunction is selected from the group consisting of Leber's hereditary optic neuropathy (LHON), dominant optic neuropathy (DOA), Leigh syndrome, Friedreich's ataxia, mitochondrial myopathy, encephalomyopathy, lactic acidosis, stroke-like symptoms (MELAS), myoclonic epilepsy with ragged red fibers (MERRF), myoneurogenic gastrointestinal encephalomyopathy (MNGIE), Kearns-Sayre syndrome, CoQ.10 deficiency, mitochondrial complex deficiencies, Neuropathy, ataxia, retinitis pigmentosa, and ptosis (NARP), spinocerebellar ataxias, ataxia telangiectasia, ataxia oculomotor apraxia 1 and 2 (AOA1 and 2), epileptic seizures, amyotrophic lateral sclerosis (ALS), motor neuron disease (MND), Parkinson's disease, Alzheimer's disease, Huntington's disease, stroke/reperfusion injury, or dementia, ...

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Номер записи: 71
26-05-2016 дата публикации

Quinone based nitric oxide donating compounds for ophthalmic use

Номер: US20160145192A1
Автор: Elena Bastia, Gael Ronsin, Laura Storoni, Nicoletta Almirante
Принадлежит: Nicox Science Ireland Ltd

The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.

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Номер записи: 72
26-05-2016 дата публикации

Aminomethyl-Biaryl Derivatives Complement Factor D inhibitors and uses thereof

Номер: US20160145247A1
Автор: Anna Vulpetti, Christine Fang GELIN, David Belanger, Donglei Liu, Edwoge Liliane Jeanne LORTHIOIS, James J. Powers, Keith Jendza, NAN Ji, Nello Mainolfi, Oliver Rogel, Rajeshri Ganesh Karki, Stefan Andreas Randi, Stefanie Flohr, Taeyoung Yoon
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I), a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

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Номер записи: 73
24-05-2018 дата публикации

METHODS FOR PREPARING BRIDGED BI-AROMATIC LIGANDS

Номер: US20180141883A1
Автор: Faler Catherine Anne, Ramirez Kevin P.
Принадлежит: UNIVATION TECHNOLOGIES, LLC

New methods for preparing bridged bi-aromatic ligands are disclosed. The methods employ aryl coupling of unprotected phenols. The ligands may be used to prepare transition metal compounds useful as catalysts in olefin polymerization. 6. A method according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris independently selected from the group consisting of hydride claim 1 , halide claim 1 , optionally substituted alkyl claim 1 , heteroalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , alkoxyl claim 1 , aryloxyl claim 1 , silyl claim 1 , boryl claim 1 , dialkylamino claim 1 , alkylthio claim 1 , arylthio claim 1 , and seleno.7. A method according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris independently selected from the group consisting of hydride claim 1 , halide claim 1 , optionally substituted alkyl claim 1 , heteroalkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , alkoxyl claim 1 , aryloxyl claim 1 , silyl claim 1 , dialkylamino claim 1 , alkylthio claim 1 , and arylthio.8. A method according to wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Ris independently selected from the group consisting of hydride claim 1 , and optionally substituted alkyl and aryl.9. A method according to wherein the bridging group A is selected from the group consisting of optionally substituted divalent hydrocarbyl and divalent heteroatom containing hydrocarbyl.10. A method according to wherein the bridging group A is selected from the group consisting of optionally substituted divalent alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , heteroalkyl claim 1 , heteroalkenyl claim 1 , heteroalkynyl claim 1 , carbocycle claim ...

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Номер записи: 74
24-05-2018 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20180141921A1
Автор: JURUTKA Peter, MARSHALL Pamela, WAGNER Carl
Принадлежит: Arizona Board of Regents on behalf of Arizona State University

The invention provides compounds and compositions that are useful for treating conditions including Alzheimer's disease, Parkinson's disease, diabetes, cancer, and psychotic disorders such as schizophrenia. This is a divisional application of U.S. Non-Provisional application Ser. No. 15/121,324, filed on 24 Aug. 2016, which is a National Stage Application under 35 USC371(c) of International Application No. PCT/US15/017832, having an International Filing Date of 26 Feb. 2015, and which claims the benefit of priority to U.S. Provisional Application No. 61/945,020, filed on 26 Feb. 2014. The entire content of the applications referenced above are hereby incorporated by reference herein.This invention was made with government support under R15 CA139364 awarded by the National Institutes of Health. The government has certain rights in the invention.The human retinoid X receptors (hRXRs) consist of three identified isoforms (a, (3, y) that function as transcription promoters often in partnership with other members of a larger nuclear receptor (NR) family of transcription regulators including the thyroid receptor (TR), the vitamin D receptor (VDR), the liver X receptor (LXR), the peroxisome proliferator-activated receptor (PPAR), and the retinoic acid receptor (RAR). While 9-cis-retinoic acid (9-cis-RA) and docosahexaenoic acid (DHA) have been shown to bind to hRXRs and promote RXR element (RXRE) regulated transcription (i.e. function as RXR agonists), it is still unclear if RXR has a bona fide endogenous molecular ligand. RXR has been described as the central NR regulator, because it often plays a critical role, either as a permissive or non-permissive partner, in heterodimer complexes that must be formed with the other NRs to regulate their respective response elements.Recent studies have identified several RXR-selective-binding molecular ligands (rexinoids) that can modulate not only RXRE regulated transcription but also the heterodimer regulated transcription of other ...

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Номер записи: 75
24-05-2018 дата публикации

MATERIALS FOR ORGANIC ELECTRLUMINESCENT DEVICES

Номер: US20180145260A1
Автор: Hayer Anna, Heil Holger, Joosten Dominik, MAIER-FLAIG Florian
Принадлежит:

The present invention relates to the fluorene derivatives and to organic electronic devices in which these Compounds are used as matrix material in the emitting layer and/or as hole transport material and/or as electron blocker or exciton blocker material and/or as electron transport material. 115.-. (canceled)17. The compound according to claim 16 , wherein{'sup': 1', '2', '3', '4', '1', '1', '2', '3', '4, 'A, A, A, Ais the same or different at each instance and is CR, with the proviso that not more than two of the A, A, A, Agroups in one cycle are N;'}{'sup': 1', '2', '3', '2', '1', '2', '3, 'V, V, Vis the same or different at each instance and is CR, with the proviso that not more than two of the V, V, Vgroups in one cycle are N;'}{'sup': 1', '2', '3', '3', '1', '2', '3, 'W, W, Wis the same or different at each instance and CR, with the proviso that not more than two of the W, W, Wgroups in one cycle are N;'}{'sup': 1', '2', '3', '4', '1', '2', '3, 'X, X, Xis the same or different at each instance and is CR, with the proviso that not more than two of the X, X, Xgroups in one cycle are N;'}19. The compound according to claim 16 , wherein the compound has a molecular weight of not more than 5000 g/mol.20. The compound according to claim 16 , wherein the compound has a molecular weight of not more than 1000 g/mol.21. The compound according to claim 16 , wherein the compound has a total of not more than 5 nitrogen atoms.22. The compound according to claim 16 , wherein the compound has a total of not more than 3 nitrogen atoms.23. The compound according to claim 16 , wherein the compound has a total of not more than 5 heteroatoms apart from fluorine.24. The compound according to claim 16 , wherein the compound is a hydrocarbon or a fluorinated hydrocarbon.25. The compound according to claim 16 , wherein the compound is a hydrocarbon.26. The compound according to claim 16 , wherein the compound is a wide band gap material.27. The compound according to claim 16 , ...

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Номер записи: 76
15-09-2022 дата публикации

Organic electroluminescent element and electronic device using same

Номер: US20220289704A1
Автор: HIROAKI Itoi, Satomi TASAKI, Taro YAMAKI, Yuki Nakano
Принадлежит: Idemitsu Kosan Co Ltd

An organic electroluminescence device comprising: a cathode, an anode, and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a compound represented by the following formula (1), and a compound A having a Stokes shift of 20 nm or smaller and an emission peak wavelength of 440 nm to 465 nm (at least one of Ar1 and Ar2 is a monovalent group having a structure represented by the following formula (2)).

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Номер записи: 77
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: 78
31-05-2018 дата публикации

Magnetically separable iron-based heterogeneous catalysts for dehydrogenation of alcohols and amines

Номер: US20180147568A1
Автор: Dinesh Jagadeesan, Ekambaram Balaraman, Garima JAISWAL, Sanjay Pandurang Borikar
Принадлежит: Council of Scientific and Industrial Research CSIR

The present invention discloses an iron-based nitrogen doped graphene catalyst, process for preparation thereof and use of said catalyst in oxidant-free catalytic dehydrogenation of alcohols and amines to the corresponding carbonyl compounds, amines and N-heterocylic compounds with extraction of molecular hydrogen as the only by-product.

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Номер записи: 79
17-06-2021 дата публикации

Alpha-truxillic acid derivatives and pharmaceutical compositions thereof

Номер: US20210179535A1
Автор: Dale Deutsch, Iwao Ojima, Kongzhen HU, Martin Kaczocha, Matthew ELMES, Simon Tong, Su Yan
Принадлежит: Research Foundation of State University of New York

The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure: Formula (I)

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Номер записи: 80
07-06-2018 дата публикации

ARYL ETHERS AND USES THEREOF

Номер: US20180155279A1
Автор: DIXON Darryl David, GRINA Jonas, Josey John A., Rizzi James P., Schlachter Stephen T., Wallace Eli M., Wang Bin, WEHN Paul, Xu Rui, Yang Hanbiao
Принадлежит:

The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo. 164.-. (canceled)66. The method of claim 65 , wherein Ris phenyl or pyridyl claim 65 , wherein said phenyl or pyridyl is substituted with one or more substituents selected from the group consisting of halo claim 65 , C-Calkyl claim 65 , C-Calkoxy and cyano.67. The method of claim 65 , wherein Ris cyano claim 65 , fluoroalkyl claim 65 , sulfinyl claim 65 , sulfonamide claim 65 , sulfonyl or sulfoximinyl.68. The method of claim 65 , wherein Ris hydrogen.69. The method of claim 65 , wherein Ris hydroxy or amino and Ris hydrogen.70. The method of claim 65 , wherein Ris fluoro and n is 1 claim 65 , 2 or 3.73. The method of claim 72 , wherein Ris phenyl or pyridyl claim 72 , wherein said phenyl or pyridyl is substituted with one or more substituents selected from the group consisting of halo claim 72 , C-Calkyl claim 72 , C-Calkoxy and cyano.74. The method of claim 72 , wherein Ris cyano claim 72 , fluoroalkyl claim 72 , sulfinyl claim 72 , sulfonamide claim 72 , sulfonyl or sulfoximinyl.75. The method of claim 72 , wherein Ris hydrogen and Ris hydroxy or amino.76. The method of claim 72 , wherein the enantiomeric excess of said compound is at least about 80%.80. The method of claim 65 , wherein the cancer is hemangioblastoma claim 65 , pheochromocytoma claim 65 , a pancreatic neuroendocrine tumor claim 65 , renal cell carcinoma claim 65 , astrocytoma claim 65 , breast cancer claim 65 , cervical cancer claim 65 , colorectal cancer claim 65 , glioblastoma claim 65 , glioma claim 65 , head and neck cancer claim 65 , hepatocellular cancer claim 65 , non-small cell lung cancer claim 65 , melanoma claim 65 , neuroblastoma claim 65 , ovarian cancer or prostate cancer.81. The ...

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Номер записи: 81
23-05-2019 дата публикации

COMPOUNDS AND SYNTHETIC METHODS FOR THE PREPARATION OF RETINOID X RECEPTOR-SPECIFIC RETINOIDS

Номер: US20190152888A1
Автор: Chandraratna Roshantha A., Jacks Thomas, Thompson Andrew, Vuligonda Vidyasagar Pradeep, Wade Peter
Принадлежит:

Provided herein are compounds useful for the preparation of compounds that have retinoid-like biological activity. Also provided herein are processes for the preparation of compounds that have retinoid-like biological activity. 7. A composition comprising the compound of .8. A pharmaceutical composition comprising the compound of claim 1 , and a pharmaceutically acceptable excipient or carrier.9. A method of treating cancer comprising claim 1 , administering to a subject in need thereof the compound of claim 1 , at a therapeutically effective dose from about 0.1 to about 20 mg/m/day.10. The method of claim 9 , wherein the therapeutically effective dose of the rxr agonist is a dose below the retinoic acid receptor (RAR) activating threshold and at or above the RXR effective dose.11. The method of claim 9 , wherein the cancer is a hematologic malignancy claim 9 , lung cancer claim 9 , prostate cancer claim 9 , breast cancer claim 9 , pancreatic cancer claim 9 , colon cancer claim 9 , or cervical cancer.12. The method of claim 9 , wherein the treating further comprises administration of thyroid hormone.13. The method of claim 9 , wherein the compound has an enantiomeric excess of Compound A that essentially eliminates claim 9 , or reduces to an undetectable level claim 9 , RAR activation by Compound B.14. A method of treating a nervous system disorder claim 1 , a muscular disorder claim 1 , a demyelinating disease claim 1 , or an autoimmune disease in a subject in need thereof claim 1 , comprising claim 1 , administering to the subject a therapeutically effective amount of the compound of claim 1 , wherein the therapeutically effective amount is from 0.001 mg/kg/day to about 100 mg/kg/day.15. The method of claim 14 , wherein the nervous system disorder is Parkinson's disease claim 14 , Alzheimer's disease claim 14 , multiple sclerosis claim 14 , schizophrenia claim 14 , amyotrophic lateral sclerosis claim 14 , ischemic injury claim 14 , traumatic injury claim 14 , a ...

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Номер записи: 82
23-05-2019 дата публикации

Sulfonated Aromatic Compounds

Номер: US20190152902A1
Автор: GEIGLE Peter, HARTWIG Jan, KRAWCZYK Nastaran, LARIONOV Evgeny, MOELLER Alexander
Принадлежит: CMBLU PROJEKT AG

The present invention relates to novel lignin-derived compounds and compositions comprising the same and their use as redox flow battery electrolytes. The invention further provides a method for preparing said compounds and compositions as well as a redox flow battery comprising said compounds and compositions. Additionally, an assembly for carrying out the inventive method is provided. 2. The sulfonated low molecular weight aromatic compound according to claim 1 , wherein said compound is characterized by Formula (X) or (XI) and wherein Rand Rare independently selected from H or SOH claim 1 , Ris selected from H claim 1 , OH claim 1 , and C-Calkoxy claim 1 , preferably methoxy claim 1 , or SOH claim 1 , Ris selected from H claim 1 , OH and C-Calkoxy claim 1 , preferably methoxy.3. The sulfonated low molecular weight aromatic compound according to or claim 1 , wherein the compound is characterized by one of the following:{'sup': '4', 'sub': '3', 'a) Ris SOH;'}{'sup': 4', '3, 'sub': '3', 'b) Ris SOH, Ris methoxy;'}{'sup': 4', '2', '3, 'sub': '3', 'c) Ris SOH, Rand Rare methoxy;'}{'sup': 1', '4, 'sub': '3', 'd) Rand Rare SOH;'}{'sup': 1', '4', '3, 'sub': '3', 'e) Rand Rare SOH, Ris methoxy;'}{'sup': 1', '4', '2', '3, 'sub': '3', 'f) Rand Rare SOH, Rand Rare methoxy; or'}{'sup': 2', '4', '3, 'sub': '3', 'g) Rand Rare SOH, and Ris methoxy,'}{'sup': 1', '4, 'wherein each of the other of R-Ris OH or H, preferably H.'}4. The sulfonated low molecular weight aromatic compound according to claim 1 , wherein said compound is characterized by Formula (XII) or (XIII) claim 1 , wherein Rand Rare independently selected from H claim 1 , OH and C-Calkoxy claim 1 , preferably methoxy claim 1 , and R-Rare independently selected from H and SOH.5. The sulfonated low molecular weight aromatic compound according to claim 1 , wherein said compound is characterized by Formula (XIV) or (XV) and wherein R claim 1 , Rand Rare independently selected from H claim 1 , OH and C-Calkoxy claim 1 , ...

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Номер записи: 83
14-05-2020 дата публикации

DECARBOXYLATIVE CROSS-COUPLING AND APPLICATIONS THEREOF

Номер: US20200148668A1
Автор: MACMILLAN David W.C., ZUO Zhiwei
Принадлежит:

Methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. For example, methods described herein enable the production of numerous molecular species through decarboxylative cross-coupling via use of photoredox and transition metal catalysts. A method described herein, in some embodiments, comprises providing a reaction mixture including a photoredox catalyst, a transition metal catalyst, a coupling partner and a substrate having a carboxyl group. The reaction mixture is irradiated with a radiation source resulting in cross-coupling of the substrate and coupling partner via a mechanism including decarboxylation, wherein the coupling partner is selected from the group consisting of a substituted aromatic compound and a substituted aliphatic compound. 1. A method of cross-coupling comprising:providing a substrate including a carboxyl group;oxidizing the carboxyl group via a single electron transfer process, wherein the substrate subsequently undergoes decarboxylation to provide a substrate radical; andforming a C—C bond between the substrate radical and a coupling partner selected from the group consisting of a substituted aromatic compound and substituted aliphatic compound.2. The method of claim 1 , wherein the substrate is an aliphatic carboxylic acid.3. The method of claim 1 , wherein the aliphatic carboxylic acid is an amino acid.4. The method of claim 1 , wherein the aliphatic carboxylic acid is a fatty acid.5. The method of claim 1 , wherein the aliphatic carboxylic acid is of formula R—COH claim 1 , wherein Ris selected from the group consisting of -alkyl claim 1 , -cycloalkyl claim 1 , -heteroalkyl claim 1 , -heterocycloalkyl claim 1 , -alkenyl claim 1 , -cycloalkenyl claim 1 , -heteroalkenyl claim 1 , -heterocycloalkenyl claim 1 , -alkynyl claim 1 , -alkyl-aryl claim 1 , -alkyl-heteroaryl claim 1 , -alkyl-alkoxy claim 1 , -alkenyl-aryl claim 1 , - ...

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Номер записи: 84
24-06-2021 дата публикации

Onium salt compound, chemically amplified resist composition and patterning process

Номер: US20210188770A1
Автор: Kenichi Oikawa, Masahiro Fukushima, Takayuki Fujiwara, Tomohiro Kobayashi
Принадлежит: Shin Etsu Chemical Co Ltd

An onium salt having formula (1) serving as an acid diffusion inhibitor and a chemically amplified resist composition comprising the acid diffusion inhibitor are provided. When processed by lithography, the resist composition exhibits a high sensitivity, and excellent lithography performance factors such as CDU and LWR.

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Номер записи: 85
29-09-2022 дата публикации

Lipids for delivery of charged material, formulations thereof and method for making same

Номер: US20220304929A1
Автор: Joshua Zaifman, Marco A. Ciufolini, Sam Chen, Yuen Yi Tam
Принадлежит: Integrated Nanotherapeutics Inc, University of British Columbia

Disclosed herein is a lipid having a net charge at physiological pH, and being covalently attached to a lipid moiety. The lipid moiety comprises a hydrocarbon structure having two or more linked hydrocarbon chains, optionally having cis or trans C═C, at least one of said chains being covalently attached to the head group optionally via the linker region. The hydrocarbon chains are bonded to one another at a branch point at an internal carbon of the chain attached to the linker region, which branch point comprises a functional group having an electronegative atom. The hydrocarbon chains each have between 1 and 40 carbon atoms, wherein the hydrocarbon structure in total comprises between 10 and 150 carbon atoms. Advantageously, the hydrocarbon structure may assume a generally flared shape for enhanced delivery of cargo molecules. Further provided are delivery vehicles comprising the lipids.

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Номер записи: 86
21-05-2020 дата публикации

ENANTIOSELECTIVE SYNTHESIS OF ALPHA-QUATERNARY MANNICH ADDUCTS BY PALLADIUM-CATALYZED ALLYLIC ALKYLATION

Номер: US20200157020A1
Автор: Chiyoda Koji, Numajiri Yoshitaka, Pritchett Beau P., Stoltz Brian M.
Принадлежит:

This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): 163-. (canceled)65. The method of claim 64 , wherein the transition metal catalyst comprises a transition metal selected from palladium claim 64 , nickel claim 64 , and platinum.66. The method of claim 64 , wherein the transition metal catalyst further comprises a chiral ligand.67. The method of claim 64 , wherein the compound represented by formula (Ia) has about 80% ee or greater.68. The method of claim 64 , wherein the compound represented by formula (Ia) has about 85% ee or greater.69. The method of claim 64 , wherein the compound represented by formula (Ia) has about 90% ee or greater. This Application is a Continuation of U.S. patent application Ser. No. 14/972,475, filed Dec. 17, 2015, which claims the benefit of U.S. Provisional Application 62/093,982, filed Dec. 18, 2014, the contents of both of which are incorporated herein by reference.This invention was made with Government support under Grant Number R01GM080269, awarded by the National Institutes of Health. The Government has certain rights in the invention.The Mannich reaction, first discovered in the early 20th century, is among the most robust reactions known to produce nitrogen-containing compounds. In a classic intermolecular Mannich reaction, an aldehyde, an amine and an α-acidic carbonyl compound react to form a β-amino carbonyl compound. Recent progress in this area, including modified imine donors and well-explored catalyst systems, has made available a wide variety of asymmetric α-functionalizations of carbonyl compounds. However, to date, asymmetric Mannich-type reactions to establish α-quaternary carbonyl compounds have been limited to specialized substrate classes.There exists a need for methods that enable access to α-quaternary Mannich Adducts, particularly enantioselective ...

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Номер записи: 87
01-07-2021 дата публикации

HIGH PENETRATION PRODRUG COMPOSITIONS OF RETINOIDS AND RETINOIDS-RELATED COMPOUNDS

Номер: US20210196664A1
Автор: Yu Chongxi
Принадлежит:

The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate. 2. A method for screening a HPP of a retinoid or a retinoid-related compound for a desired character , comprising the following steps:1) covalently linking a functional unit comprising a retinoid or a retinoid-related compound to a transportational unit through a linker to form a test composition;2) administering the test composition to a biological subject or a biological barrier; and3) determining whether the test composition has a desired character.3. The method according to claim 2 , wherein the desired character is selected from the group consisting of:1) the ability of the test composition to penetrate the biological barriers;2) the ability of the test composition to convert to a parent drug or to an active agent;3) the penetration rate of the test composition;4) the efficiency of the test composition; and5) the efficacy of the test composition.4. A method for diagnosing a condition in a biological subject claim 2 , comprising the following steps:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, '1) administering a composition according to any one of ...

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Номер записи: 88
21-06-2018 дата публикации

CYCLOPROPANATION OF SUBSTITUTED ALKENES

Номер: US20180170830A1
Автор: BECKER Yigal, GARA Mohamad
Принадлежит:

Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent. 1. A cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane in the presence of (i) particulate metal Zn , (ii) catalytically effective amount of particulate metal Cu or a salt thereof , (iii) at least one haloalkylsilane , and (iv) at least one solvent; thereby producing a cyclopropane derivative of said compound.2. A cyclopropanation process according to claim 1 , wherein said alkene compound has at least two carbon-carbon double bonds.3. A cyclopropanation process according to claim 1 , wherein said at least one dihaloalkane is dibromomethane claim 1 , chlorobromomethane claim 1 , or a combination thereof.4. A cyclopropanation process according to claim 1 , wherein said particulate metal Zn has particle size of less than 10 μm.5. A cyclopropanation process according to claim 1 , wherein said particulate metal Cu has particle size of less than 50 μm.6. A cyclopropanation process according to claim 1 , wherein said haloalkylsilane is chlorotrialkyl silane.7. A cyclopropanation process according to claim 6 , wherein said chlorotrialkyl silane is selected from the group consisting of chlorotrimethylsilane claim 6 , chlorotriethylsilane claim 6 , chlorotributylsilane claim 6 , chlorotriisobutylsilane claim 6 , chlorotrihexylsilane claim 6 , and any combinations thereof.8. A cyclopropanation process according to claim 1 , wherein said at least one solvent is an ether solvent.9. A cyclopropanation process according to claim 8 , wherein said at least one ether solvent is selected from the group ...

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Номер записи: 89
28-06-2018 дата публикации

PROCESSES FOR PREPARING ANTIVIRAL COMPOUNDS

Номер: US20180179175A1
Автор: Allan Kevin M., Fujimori Shinji, Heumann Lars V., Huynh Grace May, Keaton Katie Ann, Levins Christopher M., Pamulapati Ganapati Reddy, Roberts Benjamin James, SARMA Keshab, Teresk Martin Gerald, Wang Xiang, Wolckenhauer Scott Alan
Принадлежит:

The present disclosure provides processes for the preparation of a compound of formula: 1134.-. (canceled)136. The compound of claim 135 , wherein Z is bromo.138. (canceled) This application is a continuation of U.S. application Ser. No. 15/582,224, filed Apr. 28, 2017, which is a continuation of U.S. application Ser. No. 14/733,139, filed Jun. 8, 2015, now U.S. Pat. No. 9,670,187, which claims priority to and the benefit of U.S. Provisional Application No. 62/010,813, filed Jun. 11, 2014, each of which is hereby incorporated by reference in its entirety.The present disclosure relates generally to the field of organic synthetic methodology for the preparation of antiviral compounds and the synthetic intermediates prepared thereby.Hepatitis C is recognized as a viral disease of the liver. Although drugs targeting the liver are in wide use and have shown effectiveness, toxicity and other side effects have limited their usefulness. Inhibitors of hepatitis C virus (HCV) are useful to limit the establishment and progression of infection by HCV as well as in diagnostic assays for HCV.The compound of Formula (A) is known to exhibit antiviral properties (WO 2013/075029). Processes suitable for its production are disclosed herein.The present disclosure provides processes for making a compound of formula (A):or a salt or solvate thereof.In one embodiment, provided is a process for preparing a compound of formula (A):or a salt or solvate thereof, comprising the steps of:(a) contacting a compound of formula (I), stereoisomer thereof, or mixture of stereoisomers thereof:with a compound of formula (J) or salt thereof:under conditions sufficient to yield a compound of formula (G), stereoisomer thereof, or mixture of stereoisomers thereof:(b) contacting the compound of formula (G) with a compound of formula (H) or salt thereof:under conditions sufficient to yield a compound of formula (B), stereoisomer thereof, or mixture of stereoisomers thereof:(c) cyclizing a compound of formula ...

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Номер записи: 90
13-06-2019 дата публикации

Cyclopropanation of substituted alkenes

Номер: US20190177247A1
Автор: Mohamad GARA, Yigal Becker
Принадлежит: International Flavors and Fragrances Inc

Disclosed is a cyclopropanation process comprising the step of reacting an alkene compound having at least one carbon-carbon double bond with at least one dihaloalkane. The reaction is carried out in the presence of (i) particulate metal Zn, (ii) catalytically effective amount of particulate metal Cu or a salt thereof, (iii) at least one haloalkylsilane, and (iv) at least one solvent.

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Номер записи: 91
07-07-2016 дата публикации

Styrenyl Derivative Compounds for Treating Ophthalmic Diseases and Disorders

Номер: US20160193160A1
Автор: Anna Gall, Ian Leslie Scott, Jennifer Gage, Kevin F. Mcgee, Lana Michele Rossiter, Mark W. Orme, Qin Jiang, Ryo Kubota, Thomas L. Little, Jr., Vladimir Aleksandrovich 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 styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that 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: 92
12-07-2018 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS OF USE

Номер: US20180194716A1
Автор: Booth Raymond G.
Принадлежит:

The invention relates to protein biding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs. 1. A method of treating or preventing a GPCR-mediated disorder in a subject comprising administering to the subject identified as in need thereof a APT compound.2. The method of claim 1 , wherein the APT compound is a compound of Table 1.4. The method of claim 3 , wherein in the APT compound only one of Rand Ris H.5. The method of claim 4 , wherein in the APT compound only one of Rand Ris optionally substituted phenyl.6. The method of claim 1 , wherein the disorder is a neuropsychiatric disorder (e.g. claim 1 , obesity claim 1 , addiction claim 1 , anxiety claim 1 , depression claim 1 , schizophrenia claim 1 , and sleep disorders) claim 1 , a neurodegenerative disorder (e.g. claim 1 , Parkinson's Disease claim 1 , Alzheimer's Disease) claim 1 , a neurological disorder (e.g. claim 1 , epilepsy) claim 1 , a cardiovascular disorder (e.g. claim 1 , hypertension) claim 1 , a gastrointestinal disorder (e.g. claim 1 , irritable bowel syndrome) claim 1 , or a genitor-urinary tract disorder (e.g. claim 1 , bladder control).7. The method of claim 1 , wherein the disorder is cocaine addiction.8. The method of claim 1 , wherein the disorder is obesity claim 1 ,9. A method of inhibiting 5-HT2C in a subject identified as in need of such treatment claim 1 , comprising administering a APT compound.10. A method of treating obesity in a subject comprising administering to the subject identified as in need thereof a APT compound capable of selectively inhibiting the 5-HT2c relative to 5-HT2a or 5-HT2b.11. The method of claim 10 , wherein the binding interaction the for inhibiting 5-HT2c is at least 5-fold (alternatively at least 10-fold claim 10 , 15-fold claim 10 , 20-fold claim 10 , 50-fold claim 10 , 100-fold claim 10 ...

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Номер записи: 93
18-06-2020 дата публикации

COMPOUNDS AND SYNTHETIC METHODS FOR THE PREPARATION OF RETINOID X RECEPTOR-SPECIFIC RETINOIDS

Номер: US20200190008A1
Автор: Chandraratna Roshantha A., Jacks Thomas, Thompson Andrew, Vuligonda Vidyasagar Pradeep, Wade Peter
Принадлежит:

Provided herein are compounds useful for the preparation of compounds that have retinoid-like biological activity. Also provided herein are processes for the preparation of compounds that have retinoid-like biological activity. 3. The method of claim 1 , wherein the base is KCO.4. The method of claim 1 , wherein the reaction comprises a solvent comprising EtOH.6. The method of claim 5 , wherein the base is KCO.7. The method of claim 5 , wherein the reaction comprises a solvent comprising EtOH.9. The method of claim 8 , wherein the base is KCO.10. The method of claim 8 , wherein the reaction comprises a solvent comprising EtOH.11. The method of claim 8 , wherein the means for catalyzing a Suzuki reaction of compound 4 with compound 7 is Pd/C.12. The method of claim 8 , wherein the means for catalyzing a Suzuki reaction of compound 4 with compound 7 is not Pd(PPh).15. The method of claim 13 , wherein the base is KCO.16. The method of claim 13 , wherein the reaction comprises a solvent comprising EtOH.17. The method of claim 13 , wherein the means for catalyzing a Suzuki reaction of compound 4 with compound 7 is Pd/C.18. The method of claim 13 , wherein the means for catalyzing a Suzuki reaction of compound 4 with compound 7 is not Pd(PPh).19. The method of claim 8 , wherein the reaction comprises a solvent comprising EtOH claim 8 , wherein the base is KCO claim 8 , and wherein the means for catalyzing a Suzuki reaction of compound 4 with compound 7 is not Pd(PPh).20. The method of claim 19 , wherein the means for catalyzing a Suzuki reaction of compound 4 with compound 7 is Pd/C. This application is a continuation of U.S. patent application Ser. No. 16/194,141, filed Nov. 16, 2018, now U.S. Pat. No. 10,______,______, which claims priority to U.S. Provisional Patent Application No. 62/671,137, filed on May 14, 2018, and U.S. Provisional Patent Application No. 62/588,163, filed on Nov. 17, 2017. The entire content of each of these applications is incorporated herein by ...

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Номер записи: 94
19-07-2018 дата публикации

NOVEL REXINOID COMPOUNDS AND METHODS OF USING REXINOID COMPOUNDS FOR TREATING METABOLIC DISORDERS AND CANCER

Номер: US20180201565A1
Автор: Atigadda Venkatram Reddy, Brouillette Wayne J., Grubbs Clinton J., Kim Jeonga, Muccio Donald D.
Принадлежит: THE UAB RESEARCH FOUNDATION

Novel rexinoid compounds are provided herein. Also provided herein are methods of using the compounds to treat disorders, such as metabolic disorders, diabetes, insulin resistance, glucose intolerance, obesity, steatosis, inflammation, and/or cancer. 3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)14. (canceled)17. The compound of claim 16 , wherein Rand Rare not simultaneously methyl.19. A pharmaceutical composition claim 1 , comprising a compound of and a pharmaceutically acceptable carrier.20. A method of treating or preventing a metabolic disorder in a subject claim 1 , comprising administering to a subject an effective amount of a compound of .21. The method of claim 20 , wherein administering the compound provides a glucose-lowering effect claim 20 , an insulin-sensitizing effect claim 20 , or a plasma triglyceride lowering effect.22. (canceled)23. (canceled)24. A method of treating or preventing insulin resistance claim 1 , glucose intolerance claim 1 , obesity claim 1 , steatosis or inflammation in a subject claim 1 , comprising administrating to a subject in need thereof an effective amount of a compound of .25. The method of claim 20 , wherein the subject is a rodent or human claim 20 , obese claim 20 , morbidly obese claim 20 , pre-diabetic claim 20 , or diabetic.26. (canceled)27. (canceled)28. (canceled)29. (canceled)30. The method of claim 20 , wherein the compound is administered orally claim 20 , topically claim 20 , intranasally claim 20 , intravenously claim 20 , subcutaneously claim 20 , intradermally claim 20 , transdermally intramucosally intramuscularly claim 20 , by inhalation spray claim 20 , rectally claim 20 , nasally claim 20 , sublingually claim 20 , buccally claim 20 , vaginally or via an implanted reservoir.32. A method of treating or preventing cancer in a subject claim 1 , comprising administering to a subject an effective amount of a compound of .33. The method of claim 32 , ...

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Номер записи: 95
05-08-2021 дата публикации

METHODS AND DEVICES TO GENERATE [F-18]TRIFLYL FLUORIDE AND OTHER [F-18] SULFONYL FLUORIDES

Номер: US20210236659A1
Автор: Zhou Dong
Принадлежит: WASHINGTON UNIVERSITY

Described herein are methods and devices that allow the generation of [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides (such as [F-18]tosyl fluoride) in a manner that is suitable for radiosynthesis of F-18 labeled radiopharmaceuticals using currently available synthesis modules. 1. A method of making [F-18]sulfonyl fluoride without any evaporation step , the method comprising:a) passing an aqueous [F-18]fluoride solution or solvent through a solid phase extraction column comprising an anion-exchange resin so that the [F-18]fluoride is trapped on the resin;b) rinsing the resin with an organic solvent to eliminate residual water; and{'sub': 2', '2, 'sup': '1', 'c) eluting the [F-18]fluoride with an eluting solution to release the [F-18]fluoride from the anion-exchange resin as [F-18]RSOF which acts as a source of [F-18]fluoride for a labeling reaction, wherein the eluting solution comprises a compound having the formula RSORand an organic solvent, wherein'}R is selected from the group consisting of hydrocarbyl, substituted hydrocarbyl, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, arylalkenyl, substituted arylalkenyl, arylalkynyl, substituted arylalkynyl, heteroaryl, substituted heteroaryl, methyl, trifluoromethyl, and combinations thereof;{'sup': '1', 'Ris a leaving group; and'}wherein all method steps are performed with a single peristaltic pump.2. The method of claim 1 , wherein the eluting is done via a circulating method with the single peristaltic pump.3. The method of claim 1 , wherein the single peristaltic pump provides air flow to separate [F-18]sulfonyl fluoride from the reaction mixture.4. The method of claim 3 , wherein a separator is used to separate [F-18]triflyl fluoride from the reaction mixture using the air flow provided by the pump5. The method of claim 4 , wherein the ...

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Номер записи: 96
04-07-2019 дата публикации

SULFIDE ALKYL COMPOUNDS FOR HBV TREATMENT

Номер: US20190202780A1
Автор: BRAVO Yalda, Chen Austin, Clark Ryan C., Jacintho Jason, Pedram Bijan, Stock Nicholas
Принадлежит:

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention. 2. (canceled)3. (canceled)4. A composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , further comprising at least one pharmaceutically acceptable carrier.5. A method of treating an HBV infection in an individual in need thereof claim 1 , comprising administering to the individual a therapeutically effective amount of a compound according to .6. The method of claim 5 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of an HBV vaccine claim 5 , HBV polymerase inhibitor claim 5 , interferon claim 5 , pegylated interferon claim 5 , viral entry inhibitor claim 5 , viral maturation inhibitor claim 5 , BAY 41-4109 claim 5 , reverse transcriptase inhibitor claim 5 , a TLR-agonist claim 5 , AT-61 ((E)-N-(1-chloro-3-oxo-1-phenyl-3-(piperidin-1-yl)prop-1-en-2-yl)benzamide) claim 5 , and AT-130 ((E)-N-(1-bromo-1-(2-methoxyphenyl)-3-oxo-3-(piperidin-1-yl)prop-1-en-2-yl)-4-nitrobenzamide) claim 5 , and a combination thereof.7. The method of claim 6 , wherein the pegylated interferon is pegylated interferon alpha (IFN-α) claim 6 , pegylated interferon lambda (IFN-λ) claim 6 , or pegylated interferon gamma (IFN-γ).8. The method of claim 6 , wherein the reverse transcriptase inhibitor is at least one of Zidovudine claim 6 , Didanosine claim 6 , Zalcitabine claim 6 , ddA claim 6 , Stavudine claim 6 , Lamivudine claim 6 , Abacavir claim 6 , Emtricitabine claim 6 , Entecavir claim 6 , Apricitabine claim 6 , Atevirapine claim 6 , ribavirin claim 6 , acyclovir claim 6 , famciclovir claim 6 , valacyclovir claim 6 , ganciclovir claim 6 , valganciclovir claim 6 , Tenofovir claim 6 , Adefovir claim 6 , ...

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Номер записи: 97
02-08-2018 дата публикации

METHOD OF PRODUCING 2-HYDROXY-1,4-NAPHTHOQUINONE

Номер: US20180215693A1
Автор: KAKINUMA Seiji
Принадлежит: AGRO-KANESHO CO., LTD.

Provided is a method of producing 2-hydroxy-1,4-naphthoquinone in a large amount, a high yield, and inexpensively. This method comprises oxidizing 2-hydroxynaphthalene with hydrogen peroxide in (1) an alkaline aqueous solution or in (2) a mixture of an alkaline aqueous solution with an inert organic solvent incompatible with water, in the presence of a vanadium catalyst. 2. The method according to claim 1 , wherein the alkaline aqueous solution is an aqueous solution of sodium hydroxide or potassium hydroxide.3. The method according to claim 1 , wherein the vanadium catalyst is vanadium (V) oxide.4. The method according to claim 1 , wherein the organic solvent is an aliphatic hydrocarbon claim 1 , an aliphatic cyclic hydrocarbon claim 1 , or an aromatic hydrocarbon. The present invention relates to a method of producing 2-hydroxy-1,4-naphthoquinone. Specifically, the invention relates to a method of producing 2-hydroxy-1,4-naphthoquinone, which is useful as, for example, a raw material for producing a resin, an intermediate of a face wash, or an intermediate of a pharmaceutical or agricultural chemical, in a high yield and a high purity.As a method of producing 2-hydroxy-1,4-naphthoquinone using 2-hydroxynaphthalene (or 2-naphthol) as a raw material, there is disclosed a method of oxidizing 2-hydroxynaphthalene with gaseous oxygen in methanol in the presence of a cobalt catalyst and a caustic alkali. However, in this method, an expensive catalyst, such as a cobalt morpholine catalyst fixed to a polymer, must be used. In addition, the yield is insufficient. This method is described in the following non-patent document 1.As a method of producing 2-hydroxy-1,4-naphthoquinone using 1-hydroxynaphthalene as a raw material, there is disclosed a method of oxidizing 1-hydroxynaphthalene with hydrogen peroxide in an aqueous potassium hydroxide solution in the presence of a vanadium catalyst. However, in this method, 1-naphthol used as a raw material is expensive, and also the ...

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Номер записи: 98
02-08-2018 дата публикации

ENAMIDE PROCESS

Номер: US20180215702A1
Автор: Snoonian John R., Vandenbossche Charles
Принадлежит:

A convenient method for converting oximes into enamides is disclosed. The process produces enamides without the concomitant production of a large volume of metallic waste. 1. A process for converting an oxime to an enamide , said process comprising contacting said oxime with an acyl donor and a phosphine in the presence of an iron reagent that provides from 10 to 2000 ppm iron under conditions that convert said oxime to said enamide.2. The process according to wherein the acyl donor is acetic anhydride.3. The process according to wherein the phosphine is chosen from tri n-butylphosphine claim 1 , triethyl phosphine claim 1 , diphenylphosphinoethane and triphenyl phosphine.4. The process according to wherein the phosphine is triethyl phosphine.5. The process according to wherein the iron reagent is chosen from elemental iron and Fe(II) salts and Fe(III) salts wherein the counter ion is halide or alkanoate.5. The process according to wherein the iron reagent is chosen from FeCland Fe(OAc).6. The process according to wherein said iron reagent provides from 10 to 100 ppm iron.7. The process according to wherein said iron reagent provides from 10 to 50 ppm iron8. The process according to wherein said iron reagent provides from 25 to 100 ppm iron9. The process according to wherein said iron reagent provides from 500 to 2000 ppm iron10. The process according to wherein said process is carried out in a solvent at a temperature between 80° C. and 150° C.11. The process of wherein said solvent is toluene.12. The process according to wherein the oxime is an aliphatic ketone oxime.13. The process according to wherein the oxime is a tetralone oxime.14. A process for converting a ketone to an enamide claim 1 , said process comprising the sequential steps of:(a) reacting said ketone with hydroxylamine to provide an oxime; and(b) reacting said oxime with an acyl donor and a phosphine in the presence of an iron reagent that provides from 10 to 2000 ppm iron.15. A process for ...

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Номер записи: 99
02-08-2018 дата публикации

ROR-GAMMA MODULATORS AND USES THEREOF

Номер: US20180215707A1
Автор: MALI Sunil Vasantrao, SAHU Bichismita, Sharma Rajiv, SINGH DEEPAK
Принадлежит: Piramal Enterprises Limited

The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ. 6. The compound according to claim 1 ,wherein:L is —CO—;or an isotopic form, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof.7. The compound according to claim 1 ,wherein:{'sub': '2', 'L is —S(O)—;'}or an isotopic form, a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof.18. The compound according to selected from:2-(4-(Ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluoro-2-methoxypropan-2-yl)phenyl) acetamide;N-(1,1-Dioxido-4-oxothiochroman-6-yl)-2-(4-(ethylsulfonyl)phenyl)acetamide;2-(4-(Ethylsulfonyl)phenyl)-N-(4-oxothiochroman-6-yl)acetamide;N-(4-Cyclohexyl-2-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-2-(4-(ethyl sulfonyl)phenyl)acetamide;N-(4-(1-Cyanocyclopropyl)phenyl)-2-(4-(ethylsulfonyl)phenyl)acetamide;2-(4-(Ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluoro-2-(4-phenylbutoxy)propan-2-yl)phenyl)acetamide;2-(4-(Ethylsulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-2-methylphenyl)acetamide;2-(4-(Ethylsulfonyl)phenyl)-N-(3-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl) acetamide;2-(4-(Ethylsulfonyl)phenyl)-N-(4-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl) acetamide;2-(4-(Ethylsulfonyl)phenyl)-N-(4-(2,2,2-trifluoro-1-hydroxyethyl)phenyl)acetamide;N-(4-(2-(2-Cyclohexylethoxy)-1,1,1,3,3,3-hexafluoropropan-2-yl)phenyl)-2-(4-(ethyl sulfonyl)phenyl)acetamide;2-(4-(Ethyl sulfonyl)phenyl)-N-(4-(1,1,1,3,3,3-hexafluoro-2-(2-(piperidin-1-yl ...

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Номер записи: 100