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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 4697. Отображено 100.
02-02-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120027796A1
Автор: David Butler, Jayaprakash K. Narayanannair, Kallanthottathil G. Rajeev, Laxmab Eltepu, Muthiah Manoharan, Muthusamy Jayaraman
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures: (Formula (I) or (XXXV)).

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Номер записи: 1
19-04-2012 дата публикации

Novel lipids and compositions for the delivery of therapeutics

Номер: US20120095075A1
Автор: David Butler, Kallanthottathil G. Rajeev, Laxman Eltepu, Muthiah Manoharan, Muthusamy Jayaraman, Narayanannair K. Jayaprakash
Принадлежит: Alnylam Pharmaceuticals Inc

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure:

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Номер записи: 2
10-05-2012 дата публикации

Compound inhibiting in vivo phosphorus transport and medicine containing the same

Номер: US20120115851A1
Автор: Nobuaki Eto, Rika Nagao, Tetsuko Kazama
Принадлежит: Kyowa Hakko Kirin Co Ltd

An objective of the present invention is to provide compounds that can effectively suppress the concentration of phosphorus in serum to effectively prevent or treat diseases induced by an increase in concentration of phosphate in serum. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein A represents an optionally substituted five- to nine-membered unsaturated carbocyclic moiety or a five- to nine-membered unsaturated heterocyclic moiety, and represents a single bond or a double bond, R 5 represents optionally substituted aryl or the like, Z represents —N═CHR 6 R 7 or the like, R 6 and R 7 represent H, optionally substituted alkyl, optionally substituted aryl or the like, R 101 and R 102 together form ═O, and R 103 and R 104 represent H, or R 101 and R 104 together from a bond, and R 102 and R 103 together form a bond.

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Номер записи: 3
24-05-2012 дата публикации

Dual-acting antihypertensive agents

Номер: US20120129900A1
Автор: Daniel Marquess, Keith Jendza, Paul R. Fatheree, Robert M. McKinnell, Ryan Hudson, Seok-Ki Choi, Sharath Hegde, Vivek Sasikumar
Принадлежит: Theravance Inc

The invention is directed to compounds of formula I: wherein Ar, r, R 3 , X, and R 5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT 1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

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Номер записи: 4
25-10-2012 дата публикации

Aryl compounds as ppar ligands and their use

Номер: US20120271055A1
Автор: Heonjoong Kang, Jaehwan LEE, Jungwook Chin
Принадлежит: SEOUL NATIONAL UNIVERSITY INDUSTRY FOUNDATION

The present invention relates to a compound as a peroxisome proliferator activated receptor (PPAR) activator and a hydrate, a solvate, a stereoisomer and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition, a cosmetic composition, a muscle strengthening agent, a memory improving agent, a therapeutic agent for dementia and Parkinson's disease, a functional food and a feed composition containing the same.

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Номер записи: 5
20-12-2012 дата публикации

Method for Obtaining Novel Derivatives of Naphthalene for the In Vivo Diagnosis of Alzheimer's Disease

Номер: US20120321560A1
Автор: Alejandro Perera Pintado, Anais Prats Capote, Carlos Serafin Perez Martinez, Chryslaine Rodriguez-Tanty, Herman Velez Castro, Marquiza Sablon Carrazana, Pedro Valdes Sosa, Rafaela Perez Perera, Rosa Maria Lopez Barroso, Suchitil Rivera Marrero
Принадлежит: Alejandro Perera Pintado, Anais Prats Capote, Barroso Rosa Maria López, Carrazana Marquiza Sablón, Castro Hermán Vélez, Chryslaine Rodriguez-Tanty, Martínez Carlos Serafin Pérez, Rafaela Perez Perera, Sosa Pedro Valdés, Suchitil Rivera Marrero

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R 1 :-alkylenyl-C(O)NH-alkylenyl-R 3 , -alkylenyl-C(O)O—R 4 , R 3 :—COOH, —OH, —SH, —NH 2 , -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R 4 : H, succinimidyl group, R 2 : —H,-alkyl. In II: R 1 : -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R 2 : -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN) 2 , —HC═CHNO 2 , -alkylenyl-NH 2 , -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

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Номер записи: 6
20-12-2012 дата публикации

4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs

Номер: US20120322875A1
Автор: Aihua Wang, Alan R. DeAngelis, Gee-Hong Kuo, Rui Zhang
Принадлежит: Individual

The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.

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Номер записи: 7
27-12-2012 дата публикации

Method for preparing acrolein from glycerol or glycerine

Номер: US20120330049A1
Автор: Benjamin Katryniok, Franck Dumeignil, Mickael Capron, Sebastien Paul
Принадлежит: Adisseo France SAS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE CNRS, Universite De Lille 1 Sciences Et Technologies

The invention relates to a method for preparing acrolein from glycerol or glycerin, according to which dehydration of glycerol or glycerin is carried out in the presence of a catalyst which consists in at least one silica modified with zirconium dioxide, titanium dioxide or tungsten trioxide or any combination of these oxides, and a heteropolyacid. This method may be used for making 3-(methylthio)propionic aldehyde (MMP), 2-hydroxy-4-methylthiobutyronitrile (HMBTN), methionine or its analogs, from acrolein.

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Номер записи: 8
07-02-2013 дата публикации

Pyrrolysine analogs

Номер: US20130035478A1
Автор: Jennifer Jo Ottensen, Manoj Nair, Marianne Lee, Michael K. Chan, Tomasz Fekner, Xin Li
Принадлежит: Ohio State University

Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.

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Номер записи: 9
02-05-2013 дата публикации

BISPHENOL DERIVATIVE THERAPEUTICS AND METHODS FOR THEIR USE

Номер: US20130109758A1
Автор: Andersen Raymond J., Banuelos Carmen Adriana, Garcia Fernandez Javier, Mawji Nasrin R., Sadar Marianne D.
Принадлежит:

This invention provides compounds having a structure of Formula (I). Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provided. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein the at least one Z of the other aromatic ring is selected from: C-T; CF; CCl; CBr; CI; CG; CNH; and CNG.3. The compound or pharmaceutically acceptable salt of claim 1 , wherein the at least one Z of the other aromatic ring is selected from: C-T; and{'sup': '1', 'CG.'}4. The compound or pharmaceutically acceptable salt of claim 1 , wherein each of the remaining Z is independently selected from: N; CG; CH;CF; CCl; CBr; and CI.5. The compound or pharmaceutically acceptable salt of claim 1 , wherein each of the remaining Z is independently selected from: CG; CH; CCl; and CBr.6. The compound or pharmaceutically acceptable salt of claim 1 , wherein each of the remaining Z is independently selected from: CG; CH; and CBr.7. The compound or pharmaceutically acceptable salt of claim 1 , wherein CGis CCH.8. The compound or pharmaceutically acceptable salt of claim 7 , wherein each remaining Z is independently selected from: CCH; CH; and CBr.9. The compound or pharmaceutically acceptable salt of claim 1 , wherein J is selected from: O; S; SO; and SO.10. The compound or pharmaceutically acceptable salt of claim 1 , wherein J is selected from: O; and S.11. The compound or pharmaceutically acceptable salt of claim 1 , wherein J is O.12. The compound or pharmaceutically acceptable salt of claim 1 , wherein M is selected from: H; Cl; Br; CHCl; CHCl; CHBr; CHBr; CHOG; and C≡CH.13. The compound or pharmaceutically acceptable salt of claim 1 , wherein M is selected from: H; Cl; Br; CHCl; CHBr; CHOG; and C≡CH.14. The compound or pharmaceutically acceptable salt of claim 1 , wherein M is selected from: Cl; Br; CHCl; and CHBr.15. The compound or pharmaceutically acceptable salt of claim 1 ...

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Номер записи: 10
16-05-2013 дата публикации

ALLOSTERIC BINDING COMPOUNDS

Номер: US20130123326A1
Автор: Jensen Henrik Helligsø, Neubauer Henrik Amtoft, Wiborg Ove Kjaer
Принадлежит:

The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds. 2. The method according to claim 1 , comprising administering the compound of formula (I) wherein A is an aryl ring.35.-. (canceled)6. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 6-membered cycloalkyl claim 1 , aryl claim 1 , or heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.78.-. (canceled)9. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 5-membered heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.1011.-. (canceled)14. (canceled)15. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Lis selected from the group consisting of —O— claim 1 , —NH— claim 1 , and —NR—.16. The method according to claim 15 , wherein Ris Calkyl.17. The method according to claim 16 , wherein Ris selected from the group consisting of methyl claim 16 , ethyl claim 16 , propyl claim 16 , isopropyl claim 16 , butyl claim 16 , iso-butyl claim 16 , sec-butyl claim 16 , and tert-butyl.1821.-. (canceled)22. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Ris selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , and —NH—Calkyl claim 1 , where any of these optionally is substituted with one or more substituents.23. (canceled)24. The method according to claim 22 , wherein Ris Calkyl claim 22 , wherein the alkyl optionally is substituted with one or more substituents.2527.-. (canceled)29. The method according to claim 28 , wherein Lis selected from the group consisting of —O— and —S—.3038.-. (canceled)39. The method ...

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Номер записи: 11
16-05-2013 дата публикации

VINYLOGOUS CHALCONE DERIVATIVES AND THEIR MEDICAL USE

Номер: US20130123367A1
Автор: Brunhofer Gerda, Dirsch Verena, Erker Thomas, Heiss Elke, Jäger Ulrich, Vanura Katrina
Принадлежит: MEDIZINISCHE UNIVERSITAT WIEN

The present invention relates to vinylogous chalcone derivatives, in particular the compounds of formula (I) as described and defined herein, pharmaceutical compositions comprising these compounds, and their medical use, including their use in the treatment or prevention of cancer, in particular malignant hematological diseases/disorders. 2. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl) claim 1 , and Ris hydrogen.3. The compound of claim 1 , wherein Rand Rare mutually linked to form a group —CH═CH—.4. The compound of any of to claim 1 , wherein Ris hydrogen claim 1 , and Ris selected from hydrogen claim 1 , halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).5. The compound of any of to claim 1 , wherein Rand Rare mutually linked to form a group —CH— or —CH—CH—.6. The compound of any of to claim 1 , wherein Rand Rare each hydrogen.7. The compound of any of to claim 1 , wherein each Ris independently selected from halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).8. The compound of any of to claim 1 , wherein each Ris independently selected from halogen claim 1 , —NO claim 1 , —OH claim 1 , —O(Calkyl) claim 1 , —SH claim 1 , or —S(Calkyl).9. The compound of any of to claim 1 , wherein n is 1.10. The compound of any of to claim 1 , wherein m is 1 or 3.12. A pharmaceutical composition comprising the compound of any of to and a pharmaceutically acceptable excipient for use in the treatment or prevention of cancer.13. A method of treating or preventing cancer claim 1 , the method comprising the administration of the compound of any of to or the pharmaceutical composition of to a subject in need of such a treatment or prevention.14. The compound of any of to or the pharmaceutical composition of or the method of claim 1 , wherein the cancer is a malignant hematological ...

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Номер записи: 12
23-05-2013 дата публикации

SUPERACID FUNCTIONAL COMPOUNDS

Номер: US20130131201A1
Автор: Goldbach James T., Mountz David A., Wan Xiaobo
Принадлежит: Arkema Inc.

The invention relates to a novel synthesis method for forming superacid functional molecules that include monomers, as well as new polymers and copolymers formed from the monomers, and uses for these superacid molecules, polymers, and copolymers. The superacid molecules have an alpha,alpha-difluorosulfonic acid functionality that can be obtained by a reaction between various Grignard reagents and an alkyl(2-fluorosulfonyl)-1,1-difluoroacetate, such as methyl(2-fluorosulfonyl-1,1-difluoroacetate. The molecules, polymers and copolymers would be expected to have enhanced ion conductivity, and would be useful in a variety of applications, including as ion-conductive materials, surfactants, and ion exchange resins. 3. The composition of where one of the groups claim 2 , R claim 2 , is vinylic claim 2 , and the other groups Rare hydrogen.4. The composition of where Ris chosen from: sulfonate claim 1 , sulfinate claim 1 , or sulfonyl halide.5. The composition of where one of the groups claim 2 , R claim 2 , is vinylic claim 2 , the other groups Rare hydrogen claim 2 , and Ris sulfonyl halide or sulfonate.7. The composition of where the group claim 6 , Ris selected from the group consisting of: sulfonate claim 6 , sulfinate claim 6 , and sulfonyl halide.9. The copolymer of having a weight average molecular weight of 500 kg/mol or less.10. The copolymer of claim 8 , comprising three or more monomer units.14. A polymer blend comprising from 5 to 95 weight percent of said homopolymer or copolymer composition of claim 8 , with from 5 to 95 weight percent of a matrix polymer.15. The polymer blend of claim 13 , comprising a blend of at least two different sulfonated polyelectrolytes claim 13 , each comprising from 5 to 95 weight percent of said blend.16. The polymer blend of claim 13 , wherein said matrix polymer is fluorinated.17. The polymer blend of claim 15 , wherein said matrix polymer comprises a poly(vinylidene fluoride) homopolymer or copolymer.18. The polymer blend of ...

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Номер записи: 13
13-06-2013 дата публикации

Mercapto Benzophenone Compounds, Compositions and Preparation Method Thereof

Номер: US20130150479A1
Автор: HU Weijing, LI Jiaqi, LI Jing, MA Zhongli, WANG Yonglin, YAO Lixiu, Zhang Jue, ZHAO Wenchao
Принадлежит: Insight High Technology (Beijing) Co. Ltd.

The present invention provides a photocurable composition prepared using mercapto benzophenone compounds as key raw materials. The present invention aims to solve the problems existing in the prior photo-curing technology that low-molecular photoinitiators are easy to remain and migrate, while macromolecular photoinitiators has low initiation efficiency due to a low content of effective components and also has the problem of certain migration. The photocurable composition in the present invention can be easily prepared and has high addition efficiency with ethylenically unsaturated compounds, and the photocurable composition obtained by addition has no residual mercapto and has features of high initiation activity and zero migration rates when it is used in photocurable coatings, binder and ink formula. 3. The photocurable composition according to claim 2 , wherein: in the compound of said formula (I) claim 2 , R claim 2 , R claim 2 , R claim 2 , and Rare H claim 2 , and Ris methyl claim 2 , Cl claim 2 , or F; or R claim 2 , R claim 2 , R claim 2 , and Rare H claim 2 , and Ris methyl claim 2 , methoxy claim 2 , methylthio claim 2 , dimethylamino claim 2 , diethylamino claim 2 , F claim 2 , or phenyl; or R claim 2 , R claim 2 , and Rare H claim 2 , and Rand Rindependently of one another are Cl claim 2 , or methyl.43. The photocurable composition according to any one of - claims 1 , wherein component (a) is in an amount of 0.05-75% by weight relative to the total weight of said composition.53. The photocurable composition according to any one of - claims 1 , wherein component (b) includes acrylate compound claims 1 , allyl ether compound or mixture thereof.63. The photocurable composition according to any one of - claims 1 , wherein amine promotor compound can be added in said addition reaction.7. The photocurable composition according to claim 6 , wherein said amine promotor compound includes tertiary amine compound and/or active amine.8. The photocurable composition ...

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Номер записи: 14
13-06-2013 дата публикации

Benzoxazine-thiol adducts

Номер: US20130150545A1
Автор: Ilya Gorodisher, Robert J. DeVoe, Robert J. Webb
Принадлежит: 3M Innovative Properties Co

Novel benzoxazine-thiol adducts are described, which may be may be cured to produce compositions useful in coating, sealants, adhesive and many other applications.

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Номер записи: 15
04-07-2013 дата публикации

SULFUR-CONTAINING COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL USES THEREOF

Номер: US20130172355A1
Автор: CHAO Chih-Hua, SHEU Jyh-Horng, WEN Zhi-Hong
Принадлежит: NATIONAL SUN YAT-SEN UNIVERSITY

The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds. 2. The method according to claim 1 , wherein Ris selected from the group consisting of methyl claim 1 , ethyl claim 1 , and unsubstituted phenyl.6. The method according to claim 5 , wherein Ris selected from the group consisting of methyl claim 5 , ethyl claim 5 , and unsubstituted phenyl.9. The method according to claim 5 , wherein the disease is selected from the group consisting of inflammation claim 5 , atherosclerosis claim 5 , neuropathic pain claim 5 , inflammatory neointimal proliferation claim 5 , arthritis claim 5 , multiple sclerosis claim 5 , inflammatory pain claim 5 , and spinal cord injury.10. The method according to claim 5 , wherein the compound is administered by injection. This application is a Divisional of the pending U.S. patent application Ser. No. 12/172,633 filed on Jul. 14, 2008, all of which is hereby incorporated by reference in its entirety.Although incorporated by reference in its entirety, no arguments or disclaimers made in the parent application apply to this divisional application. Any disclaimer that may have occurred during the prosecution of the above-referenced application(s) is hereby expressly rescinded. Consequently, the Patent Office is asked to review the new set of claims in view of the entire prior art of record and any search that the Office deems appropriate.1. Field of the InventionThe invention relates to a novel sulfur-containing compound. Said sulfur-containing compound has ability to inhibit the function of inducible nitric oxide synthase (iNOS) and/or ...

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Номер записи: 16
15-08-2013 дата публикации

DITHIOAMINE REDUCING AGENTS

Номер: US20130211055A1
Автор: LUKESH John, RAINES Ronald T.
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

Dithioamine reducing agents useful for the reduction of disulfide bonds. The reducing agents of this invention are useful, for example, to reduce disulfide bonds, particularly in proteins, or to prevent the formation of disulfide bonds, particularly in proteins and other biological molecules. Reducing agents of this invention are useful and suitable for application in a variety of biological applications, particularly as research and synthetic reagents. The invention provides S-acylated dithioamines which can be selectively activated reducing agents by removal of the S-acyl groups enzymatically or chemically. The invention further provides dithiane precursors of thioamino reducing agents. The invention provides dithioamine reducing agents, S-acylated dithioamines and dithianes which are immobilized on surfaces, including among others, glass, quartz, microparticles, nanoparticles and resins. 2. The compound of wherein neither Ror Ris an —NHgroup.3. The compound of wherein R claim 1 , Rand Rare all hydrogens.4. The compound of wherein R claim 1 , R claim 1 , R claim 1 , Rand Rare all hydrogens.5. The compound of wherein both Rare hydrogens.6. The compound of wherein both of Rare acyl groups.7. The compound of wherein one of Ror Ris an acyl group.8. The compound of wherein both of Ror Rare hydrogens.9. The compound of wherein Ror Ris -M.10. The compound of wherein Ror Ris -L-T.11. The compound of wherein R-Rare all hydrogens.12. The compound of wherein R-Rare all hydrogens and each Ris a —CO—Rwherein Ris an alkyl group having 1-6 carbon atoms claim 1 , a halogen-substituted alkyl group having 1-6 carbon atoms claim 1 , a hydroxy-substituted alkyl group having 1 to 6 carbon atoms claim 1 , an optionally substituted phenyl group or an optionally substituted benzyl group.13. The compound of wherein R claim 1 , R claim 1 , Rand one of Ror Rare all hydrogens and the other of Ror Ris an optionally substituted alkyl group having 1-3 carbons atoms claim 1 , a halogen claim 1 , ...

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Номер записи: 17
29-08-2013 дата публикации

USE OF NITROANILINE DERIVATIVES FOR THE PRODUCTION OF NITRIC OXIDE

Номер: US20130224083A1
Автор: Conoci Sabrina, Petralia Salvatore, SORTINO Salvatore
Принадлежит: STMicroelectronics S.r.I.

The present invention relates to the use of a nitroaniline derivative of Formula I for the production of nitric oxide and for the preparation of a medicament for the treatment of a disease wherein the administration of nitric oxide is beneficial. The present invention furthermore relates to a method for the production of NO irradiating a nitroaniline derivative of Formula I, a kit comprising a nitroaniline derivative of Formula I and a carrier and to a system comprising a source of radiations and a container associated to a nitroaniline derivative of Formula I. In Formula I, R and Rare each independently hydrogen or a C-Calkyl group; Ris hydrogen or an alkyl group. 2. The kit according to claim 1 , wherein:{'sup': II', 'III', 'IV', 'V', 'VI, 'sub': 2', '18', '2', '3', '3', '3, 'Ris Ak-Y, wherein Ak is a branched or unbranched C-Calkyl group optionally substituted with —OH or NH, and Y is a tail-group selected from the group consisting of hydrogen, halogen, —SH, —S—SR, —Si(OR), —Si—X, and —CH═CRR;'}{'sup': 'III', 'Ris selected from the group consisting of alkyl group, aryl group, aralkyl group, alkenyl group, alkynyl group and heterocyclic group;'}{'sup': 'III', 'Ris an alkyl group;'}{'sup': V', 'VI, 'Rand Rare independently hydrogen or alkyl group; and'}X is halogen.3. The kit according to claim 1 , wherein said nitroaniline derivative of Formula (I) is 4-nitro-3-(trifluoromethyl)aniline.4. The kit according to claim 1 , wherein said carrier has a minor molar absorptivity in the wavelength comprised between 300 and 500 nm.5. The kit according to claim 1 , wherein said carrier is a liquid solution.6. The kit according to claim 1 , wherein said carrier is a solid substrate selected from the group consisting of a metal; an inorganic oxide; and a plastic polymeric material.7. The kit according to claim 6 , wherein said nitroaniline derivative of Formula (I) is chemically bound to said solid substrate without forming an amide bond.8. The kit according to claim 7 , ...

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Номер записи: 18
12-09-2013 дата публикации

COPPER(I)-ION SELECTIVE FLUORESCENT PROBE, METHOD FOR PREPARING THE SAME, METHOD FOR DIAGNOSING MALIGNANT DISEASE AND DIAGNOSIS KIT USING THE PROBE

Номер: US20130236922A1
Автор: Cho Bong-Rae, CHUN Hoon-Jai
Принадлежит:

The present disclosure relates to a copper (I) ion-selective fluorescent probe, a method for preparing the same, and a method for diagnosing malignant disease and a diagnosis kit using the probe. The fluorescent probe according to the present disclosure is capable of detecting free copper (I) ions inside cells for a long time with high selectivity and sensitivity for copper (I) ion, with a penetration depth longer than 90 μm in living cells and tissues and without the problems of mistargeting and photobleaching. Accordingly, since a biological sample can be imaged for a long period of time with high resolution without damage, presence of malignance disease in the target biological sample can be diagnosed faster, more accurately and more easily. 2. The copper(I) ion-selective fluorescent probe of claim 1 , wherein Ris hydrogen claim 1 , methyl or methoxy.3. The copper(I) ion-selective fluorescent probe of claim 1 , wherein Ris hydrogen or methoxy.10. The method for diagnosing malignant disease as set forth in claim 8 , wherein the malignant disease is respiratory cancer claim 8 , gastrointestinal cancer or breast cancer.11. The method for diagnosing malignant disease as set forth in claim 8 , wherein the malignant disease is diagnosed when the ratio is between 1.657 and 2.169. This application claims priority under 35 U.S.C. §119 to Korean Patent Application Nos. 10-2011-0104150 and 10-2012-0015602, filed on Oct. 12, 2011 and Feb. 16, 2012, respectively, in the Korean Intellectual Property Office, the disclosure of which is incorporated herein by reference in its entirety.The present disclosure relates to a copper(I) ion-selective fluorescent probe, a method for preparing the same, and a method for diagnosing malignant disease and a diagnosis kit using the probe.Copper ion, existing either as oxidized copper(II) ion (Cu) or as reduced copper(I) ion (Cu), is the essential probing metal found in the organs of living organisms. It acts as cofactor in many reactions by ...

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Номер записи: 19
19-09-2013 дата публикации

RHEUMATOID ARTHRITIS TREATMENT

Номер: US20130245127A1
Автор: Feuerherm Astrid Jullumstro, Johansen Berit
Принадлежит: Avexxin AS

A compound of formula (I) 2. A compound of formula (II){'br': None, 'R-L1-CO—X \u2003\u2003(II)'}(wherein R and X are as hereinbefore defined;{'sub': '2', 'L1 is a linking group forming a bridge of 1 to 5 atoms between the R group and the carbonyl CO, the atoms forming the backbone of said linking group being selected from carbon and/or the heteroatoms N, O, S, SO, SO,'}{'sub': '2', 'wherein the linking group L1 comprises a ring within the backbone or is linear and the backbone atoms of the linking group are substituted with at least one side chain (in addition to any oxo group of SO or SO) or a salt thereof.'}3. A compound as claimed in having the formula (IV){'br': None, 'R—Y3-Y4-CO—X \u2003\u2003(IV)'}wherein R and X are as hereinbefore defined;Y3 and Y4 taken together form a 5 or 6 membered homo or heterocyclic, saturated, unsaturated or aromatic ring; or{'sub': '2', 'Y3 forms a 5 or 6 membered homo or heterocyclic, saturated, unsaturated or aromatic ring and Y4 is (CH)n;'}where n is 1 to 3, preferably 1.7. A compound as claimed in any preceding claim wherein the group X is CN claim 2 , phenyl claim 2 , CHal claim 2 , CHalH claim 2 , CHalHwherein Hal represents a halogen claim 2 , e.g. fluorine claim 2 , chlorine claim 2 , bromine or iodine claim 2 , preferably fluorine.8. A compound as claimed in any preceding claim wherein the group X is CF.9. A compound as claimed in any preceding claim wherein the L or L1 group comprises an S atom claim 2 , especially β to the carbonyl.10. A compound as claimed in any preceding claim wherein R contains 5 non conjugated double bonds.12. A method of treating rheumatoid arthritis comprising administering to an animal claim 2 , preferably a mammal claim 2 , e.g. human claim 2 , an effective amount of a compound as claimed in any preceding claim.13. Use of a compound as claimed in any one of to for use in the manufacture of a medicament for treating rheumatoid arthritis.14. A compound of formula (I){'br': None, 'R-L-CO—X \u2003\ ...

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Номер записи: 20
26-09-2013 дата публикации

6,7-DIHYDRO-5H-BENZO[7]ANNULENE DERIVATIVES, PROCESS FOR PREPARATION THEREOF, PHARMACEUTICAL PREPARATIONS COMPRISING THEM, AND THE USE THEREOF FOR PRODUCTION OF MEDICAMENTS

Номер: US20130252890A1
Автор: BIERER Donald, BOHLMANN Rolf, Bothe Ulrich, Kosemund Dirk, Möller Carsten, Nubbemeyer Reinhard, Ter Laak Antonius, Wintermantel Tim, Wortmann Lars, Zorn Ludwig
Принадлежит: Bayer Intellectual Property GmbH

The invention relates to selective oestrogen receptor modulators (SERM) and methods of production thereof, use thereof for the treatment and/or prophylaxis of diseases and use thereof for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception. 6. A Compound according to that is8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,4,4,4-pentafluorobutyl)sulphinyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,4,4,4-pentafluorobutyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{4-[(4,4,5,5,5-pentafluoropentyl)sulphinyl]butyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,3-trifluoropropyl)sulphinyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(3,3,3-trifluoropropyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(4,4,4-trifluorobutyl)sulphonyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphinyl]propyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-[6-(methyl{4-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]butyl}amino)hexyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-{6-[(2-hydroxy-2-methylpropyl) {3-[(3,3,3-trifluoropropyl)sulphinyl]propyl}amino]hexyl}-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-{6-[(2-hydroxy-2-methylpropyl) {3-[(3,3,3-trifluoropropyl)sulphonyl]propyl}amino]hexyl}-6,7-dihydro-5H-benzo[7]annulen-3-ol;8-(3,5-Difluorophenyl)-9-{6-[(2-hydroxy-2- ...

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Номер записи: 21
24-10-2013 дата публикации

INTERMEDIATES OF SITAGLIPTIN AND PREPARATION PROCESS THEREOF

Номер: US20130281695A1
Автор: Deng Fei, He Minhuan, Huang Mingwang, Li Weijin, Ma Tianhua, Pan Xianhua, Ruan Libo, Yu Wansheng, Zhang Qunhui
Принадлежит: ZHEJIANG HISOAR PHARMACEUTICAL CO., LTD.

Disclosed are intermediates of Sitagliptin, a preparation process thereof, and a process for synthesizing Sitagliptin using these intermediates. Sitagliptin is synthesized by using chiral amino compounds as a raw material, without having to build a chiral center with a chiral asymmetric catalytic hydrogenation, and high-pressure hydrogenation is avoided. 2. The aziridine compound (I) with absolute configuration R according to claim 1 , wherein claim 1 ,{'sup': 1', '3', '3', '1', '4', '4, 'sub': 2', '2, 'Ris —CHSR, wherein Ris methyl; or Ris —CHOR, wherein Ris selected from the group consisting of hydrogen, methoxymethyl, benzyl, p-nitrobenzyl, tert-butyldimethylsilyl and tert-butyldiphenylsilyl; and'}{'sup': '2', 'Ris selected from the group consisting of formate group, acyl, sulfonyl, benzyl and 4-methoxybenzyl, wherein the formate group is selected from the group consisting of methoxycarbonyl, tert-butoxycarbonyl, benzyloxycarbonyl and allyloxycarbonyl; the acyl is benzoyl; the sulfonyl is benzenesulfonyl or trifluoromethylsulfonyl.'}3. The aziridine compound (I) with absolute configuration R according to claim 1 , wherein claim 1 , Ris —CHSR claim 1 , wherein Ris methyl claim 1 , or Ris —CHOR claim 1 , wherein Ris selected from the group consisting of hydrogen claim 1 , benzyl and tert-butyldimethylsilyl; and Ris selected from the group consisting of tert-butoxycarbonyl claim 1 , benzyl and benzenesulfonyl.5. The process according to claim 4 , wherein claim 4 , Ris —CHSR claim 4 , wherein Ris methyl claim 4 , or Ris —CHOR claim 4 , wherein Ris selected from the group consisting of hydrogen claim 4 , benzyl and tert-butyldimethylsilyl; Ris selected from the group consisting of tert-butoxycarbonyl claim 4 , benzyl and benzenesulfonyl; Ris methanesulfonate or p-toluenesulfonate.6. The process according to claim 4 , wherein the alkali is organic alkali or inorganic alkali;wherein the inorganic alkali is one or more alkalis selected from the group consisting of sodium ...

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Номер записи: 22
31-10-2013 дата публикации

Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators

Номер: US20130289122A1
Автор: Alessandra Restivo, Cibele Sabido-David, Elena Colombo, Emanuela Izzo, Piero Melloni, Simona Francisconi
Принадлежит: Newron Pharmaceuticals SpA

Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.

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Номер записи: 23
28-11-2013 дата публикации

TREATMENT OF MECP-2 ASSOCIATED DISORDERS

Номер: US20130316961A1
Автор: Roux Jean-Christophe, Saudou Frédéric, Villard Laurent
Принадлежит:

The invention relates to the use of cystamine, cysteamine, or a salt thereof, or of calcineurin inhibitors for treating a MeCP2-associated disorder such as Rett syndrome. 1. Cystamine or cysteamine , or a salt thereof , for use in treating a MECP2-associated disorder in a patient.2. Cystamine or cysteamine for use in treating a MECP2-associated disorder according to claim 1 , wherein the MECP2-associated disorder is selected from the group consisting of Rett syndrome claim 1 , autism claim 1 , Pervasive development disorder claim 1 , non-syndromic mental retardation claim 1 , idiopathic neonatal encephalopathy and idiopathic cerebral palsy.3. Cystamine or cysteamine for use in treating a MECP2-associated disorder according to claim 2 , wherein the MECP2-associated disorder is Rett syndrome.4. Cystamine or cysteamine for use in treating a MECP2-associated disorder according to any of to claim 2 , for use in combination with another pharmaceutically active compound.5. A calcineurin inhibitor for use in treating a MECP2-associated disorder in a human patient.6. The calcineurin inhibitor for use in treating a MECP2-associated disorder according to claim 5 , which is a macrolide.7. The calcineurin inhibitor for use in treating a MECP2-associated disorder according to or claim 5 , which is selected from the group consisting of calcipressins claim 5 , tacrolimus and tacrolimus analogs claim 5 , cyclosporine A and cyclosporine A analogs claim 5 , LxPV proteins claim 5 , 2 claim 5 ,6-diaryl-substitued pyrimidine derivatives and FK506-binding proteins8. The calcineurin inhibitor for use in treating a MECP2-associated disorder according to claim 7 , which is selected from the group consisting of calcipressin 1 claim 7 , calcipressin 2 claim 7 , calcipressin 3 claim 7 , tacrolimus claim 7 , ascomycin claim 7 , sirolimus claim 7 , pimecrolimus claim 7 , cyclosporine A claim 7 , voclosporine claim 7 , LxPVc1 claim 7 , LxPVc2 claim 7 , LxPVc3 claim 7 , 6-(3 claim 7 ,4-dichloro- ...

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Номер записи: 24
05-12-2013 дата публикации

IMPLANT FOR TREATING OR PREVENTING AN ANEURYSM

Номер: US20130324521A1
Автор: Ghotbi Reza
Принадлежит:

A medical product () introducible into a blood vessel () comprising a drug () for the treatment of an aneurysm and of arteriosclerotic diseases. The drug () is a farnesyltransferase inhibitor. 1111212313313. A medical product ( , ) introducible into a blood vessel ( , ) comprising a drug ( , ) for the treatment or prevention of an aneurysm , characterised in that said drug ( , ) is a farnesyltransferase inhibitor.2. The medical product according to claim 1 , wherein the aneurysm is caused by a degeneration of a vascular wall claim 1 , in particular wherein said vascular wall is the aortic wall.3. The medical product according to or claim 1 , wherein the aneurysm is an Aneurysma verum an Aneurysma spurium claim 1 , an Aneurysma dissecans or a hybrid thereof claim 1 , in particular wherein said aneurysm in an Aneurysma verum.4. The medical product according to at least one of the to claim 1 , wherein the aneurysm is an aneurysm at the aorta claim 1 , at the Arteria carotis claim 1 , at an artery of an upper or lower limb claim 1 , the Arteria subclavia claim 1 , a renal artery claim 1 , an encephalic artery claim 1 , at the Arteria iliaca or at a coronary artery.5111212313313. A medical product ( claim 1 , ) introducible into a blood vessel ( claim 1 , ) comprising a drug ( claim 1 , ) for the treatment or prevention of an arteriosclerotic disease claim 1 , characterised in that the drug ( claim 1 , ) is a farnesyltransferase inhibitor.6111213. The medical product according to at least one of the preceding claims claim 1 , wherein said medical product () is an angioplasty-balloon with which the diseased area in the blood vessel () is treatable with the drug () claim 1 , farnesyltransferase inhibitor.7112312. The medical product () according to at least one of the preceding claims claim 1 , wherein said medical product () is implantable inside the blood vessel () claim 1 , wherein the drug () claim 1 , farnesyltransferase inhibitor claim 1 , is administrable by means ...

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Номер записи: 25
12-12-2013 дата публикации

STABLE HOMOGENEOUSLY MIXED NANOSCALE COATINGS DERIVED FROM UNIQUE MULTI-FUNCTIONAL AND MULTIDENTATE AROMATIC ADSORBATES

Номер: US20130327251A1
Автор: Frank Thomas, Lee T. Randall, Rittikulsittichai Supachai, Singhana Burapol
Принадлежит: THE UNIVERSITY OF HOUSTON SYSTEM

Novel tridentate-, bidentate-, and monodentate-based aromatic adsorbates including self-assembled monolayers (SAMs), especially, mixed multi-component SAMs, where the adsorbates comprise an aromatic ring including one head group or a plurality of dentate head groups and one tunable tail group or a plurality of tail groups and methods for making the same, and methods for using same, their use in the preparation of homogeneously mixed multi-component self-assembled monolayers (SAMs). The adsorbants and SAMs derived therefrom are ideally suited for biosensing, biosensing diagnostics, biological interfacial mimics, surface protections for nanoparticles, inert coatings for artificial implants, and corrosion-resistant coatings for microelectronics components. 1. A method for preparing homogeneously self-assembled monolayers (SAMs) comprising:adsorbing a mono-dentate absorbate, a bi-dentate absorbate, a tri-dentate absorbate or a mixture or combination thereof onto a surface of a substrate to form a SAM modified surface,where the adsorbates comprise an aromatic ring including one dentate head group or a plurality of dentate head groups and one tunable tail group or a plurality of tunable tail groups, andwhere the SAM exhibit: (1) homogenous lateral chain distributions, (2) no or substantially no phase separation or islanding across SAM modified surfaces, and (3) enhanced stability as compared to a corresponding linear alkyl thiol monodentate adsorbate.2. The method of claim 1 , wherein the surface comprises a metal surface.3. The method of claim 1 , wherein the absorbate or mixture thereof comprise one monodentate adsorbate or a mixture of monodentate absorbates.4. The method of claim 1 , wherein the absorbate or mixture thereof comprise one bidentate adsorbate or a mixture of bidentate absorbates.5. The method of claim 4 , wherein the bidentate adsorbate or the mixture of bidentate absorbates comprise a non-symmetrical spiroalkanedithiol or a mixture of non-symmetrical ...

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Номер записи: 26
12-12-2013 дата публикации

Novel Heterocyclic Compound, Method For Producing Intermediate Therefor, And Use Thereof

Номер: US20130330876A1
Автор: Eisei KANOH, Hirokazu Kuwabara, Kazuki NIIMI, Kazuo Takimiya, Yuichi Sadamitsu
Принадлежит: Nippon Kayaku Co Ltd

Provided are a novel heterocyclic compound represented by formula (1), and a field-effect transistor having a semiconductor layer comprising the aforementioned compound. Also provided is a method for producing an intermediate enabling the production of the aforementioned novel heterocyclic compound. (In the formula, R 1 and R 2 represent a hydrogen atom, a C 2-16 alkyl group or an aryl group. However, when R 1 each independently represents a C 2-16 alkyl group or an aryl group, R 2 represents a hydrogen atom or each independently represents an aryl group; and when R 1 represents a hydrogen atom, R 2 each independently represents an aryl group.)

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Номер записи: 27
12-12-2013 дата публикации

4-(PHENOXYALKYL)THIO)-PHENOXYACETIC ACIDS AND ANALOGS

Номер: US20130331453A1
Автор: DeAngelis Alan R., Kuo Gee-Hong, Wang Aihua, Zhang Rui
Принадлежит: Janssen Pharmaceutica NV

The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia. 195-. (canceled)97. The pharmaceutical composition of wherein the pharmaceutical composition is a tablet or a capsule.98. A method of treating a condition selected from the group consisting of diabetes claim 96 , cardiovascular diseases claim 96 , Metabolic X Syndrome claim 96 , hypercholesterolemia claim 96 , hypo-HDL-cholesterolemia claim 96 , hyper-LDL-cholesterolemia claim 96 , dyslipidemia claim 96 , atherosclerosis claim 96 , and obesity claim 96 , comprising administering to a patient in need of treatment a pharmaceutical composition of .100. The pharmaceutical composition of wherein the pharmaceutical composition is a tablet or a capsule.101. A method of treating a condition selected from the group consisting of diabetes claim 99 , cardiovascular diseases claim 99 , Metabolic X Syndrome claim 99 , hypercholesterolemia claim 99 , hypo-HDL-cholesterolemia claim 99 , hyper-LDL-cholesterolemia claim 99 , dyslipidemia claim 99 , atherosclerosis claim 99 , and obesity claim 99 , comprising administering to a patient in need of treatment a pharmaceutical composition of .103. The pharmaceutical composition of wherein the pharmaceutical composition is a tablet or a capsule.104. A method of treating a condition selected from the group consisting of diabetes claim 102 , cardiovascular diseases claim 102 , Metabolic X Syndrome claim 102 , hypercholesterolemia claim 102 , hypo-HDL-cholesterolemia claim 102 , hyper-LDL-cholesterolemia claim 102 , dyslipidemia claim 102 , atherosclerosis claim 102 , and obesity claim 102 , comprising administering to a patient in need of treatment a pharmaceutical composition of . This application claims priority to U.S. Provisional Patent Application No. 60/504,146, filed Sep. 19, 2003, which is hereby incorporated ...

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Номер записи: 28
23-01-2014 дата публикации

Compositions, synthesis, and methods of using phenylcycloalkylmethylamine derivatives

Номер: US20140024679A1
Автор: Kouacou Adiey, Laxminarayan Bhat, Seema Rani Bhat
Принадлежит: Reviva Pharmaceuticals Inc

The present invention provides novel phenylcycloalkylmethylamine derivatives, and methods of preparing phenylcycloalkylmethylamine derivatives. The present invention also provides methods of using phenylcycloalkylmethylamine derivatives and compositions of phenylcycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.

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Номер записи: 29
20-02-2014 дата публикации

Lipophilic Curcumin Analogs And Methods Of Inhibiting HIV-1, Treating Latent HIV In The Brain, And Preventing HIV-Mediated Cognitive Decline And HIV Dementia

Номер: US20140051742A1
Автор: Kulkarni Amol, Nwulia Evaristus A.
Принадлежит:

Compounds having formulas (I) to (VIII), salts thereof, or combinations thereof and pharmaceutical compositions comprising one or more these compounds are described herein for the treatment of HIV and neurodegenerative effects caused by HIV. Also provided herein are methods and a kit for inhibiting HIV-1, treating latent HIV in the brain, and preventing HIV-mediated cognitive decline and HIV dementia comprising administering the compounds having the formulas (I) to (VIII) and pharmaceutical compositions comprising the compounds having these formulas. The compounds having formulas I through VIII are curcumin analogs which are advantageously characterized as having anti-retroviral, neuroprotective, anti-glucosidase, and anti-HIV integrase properties. In one aspect, the pharmaceutical composition is delivered intranasally. 2. The method according to claim 1 , wherein the pharmaceutical composition is intranasally administered.3. The method according to claim 1 , wherein the pharmaceutical composition further comprises an antiviral agent other than at least one compound of formulas (I) to (VIII).4. The method according to claim 3 , wherein the antiviral agent is selected from the group consisting of nucleoside reverse transcriptase inhibitors claim 3 , nonnucleoside reverse transcriptase inhibitors claim 3 , protease inhibitors claim 3 , integrase inhibitors claim 3 , fusion inhibitors claim 3 , chemokine receptor antagonists claim 3 , and combinations thereof.5. The method according to claim 1 , wherein the analog is dispersed into a pharmaceutically acceptable oil.8. A compound having any of formulas (II) to (VIII) as defined in .9. A pharmaceutical composition comprising at least one compound having any of formulas (II) through (VIII) as defined in .10. The pharmaceutical composition according to claim 9 , further comprising a pharmaceutically acceptable excipient claim 9 , diluent claim 9 , and/or carrier.11. The pharmaceutical composition according to claim 9 , ...

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Номер записи: 30
27-02-2014 дата публикации

Therapeutic polyamine compositions and their synthesis

Номер: US20140057877A1
Автор: Malachowski Mitchell R., Murphy Michael A.
Принадлежит:

This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicity of neurotoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be utilized to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure. 1. A method of treating degenerative diseases due to acquired mitochondrial DNA damage , redox damage to mitochondrial macromolecules and inherited mitochondrial genetic defects said method comprising the steps of:selecting a composition from a group consisting of predominantly linear tetraamines and polyamines linked by 1,3-propylene and/or ethylene groups, predominately branched tetraamines and polyamines linked by 1,3-propylene and/or ethylene groups, cyclic polyamines linked by 1,3-propylene and/or ethylene groups, combinations of linear, branched and cyclic polyamines linked by one or more 1,3-propylene and/or ethylene groups, substituted polyamines, polyamines derivatized to form tyrosine phosphatase inhibitor molecules with linear or branched chains attached, polyamine derivatives of 2,2′-diaminobiphenyl with linear or branched chains ...

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Номер записи: 31
10-04-2014 дата публикации

Fluorine-Containing Polymerizable Monomer and Polymer Compound Using Same

Номер: US20140100342A1
Автор: MATSUURA Makoto, Nakatsuji Junya, YAMANAKA Kazuhiro
Принадлежит: CENTRAL GLASS COMPANY, LIMITED

Disclosed in the present invention are a fluorine-containing polymerizable compound of the general formula (1) and a polymer compound obtained therefrom: 11. The polymer compound according to claim 5 , wherein at least a part of hydrogen atoms of OH sites of 2-hydroxy-1 claim 5 ,1 claim 5 ,1 claim 5 ,3 claim 5 ,3 claim 5 ,3-hexafluoroisopropyl groups is substituted with a glycidyl group.12. A composition comprising:{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, 'the polymer compound according to any ; and'}an epoxy compound.14. A cured product obtained by cross-linking of the glycidyl group of the polymer compound according to .15. A cured product obtained by cross-linking of the composition according to .16. The polymer compound according to claim 8 , wherein at least a part of hydrogen atoms of OH sites of 2-hydroxy-1 claim 8 ,1 claim 8 ,1 claim 8 ,3 claim 8 ,3 claim 8 ,3-hexafluoroisopropyl groups is substituted with a glycidyl group.17. A composition comprising:{'claim-ref': {'@idref': 'CLM-00008', 'claim 8'}, 'the polymer compound according to ; and'}an epoxy compound.19. A cured product obtained by cross-linking of the glycidyl group of the polymer compound according to .20. A cured product obtained by cross-linking of the composition according to . The present invention relates to a fluorine-containing polymerizable monomer and a polymer compound obtained therefrom, which are useful as resist materials for lithography in semiconductor manufacturing processes, coatings for flat panel displays, protection films for substrates in electronic circuit boards, protection films for semiconductors and the like.Bisphenols are useful as raw materials of engineering plastics. Polymers using bisphenols are suitable in a wide range of applications such as electronic components, separation films for water treatment, gas separation and hemodialysis etc. However, polyesters having bisphenol repeating units are difficult to dissolve in organic solvents and difficult to mold ...

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Номер записи: 32
05-01-2017 дата публикации

ADO-RESISTANT CYSTEAMINE ANALOGS AND USES THEREOF

Номер: US20170002004A1
Автор: Duffy Lorna, Gourdet Benoit, Phillips Timothy, Unitt John, Zankel Todd C.
Принадлежит: RAPTOR PHARMACEUTICALS INC.

The present disclosure is directed to methods for treating diseases for which cysteamine is indicated and compounds useful in such methods. 2. The method of claim 1 , wherein Rand Rare independently selected from the group consisting of H claim 1 , methyl claim 1 , and ethyl.3. The method of claim 1 , wherein Rand R claim 1 , taken together with the nitrogen atom to which they are attached claim 1 , form a 5-membered heterocyclic ring.4. The method of claim 1 , wherein Ris methyl claim 1 , optionally wherein Ris methyl.5. (canceled)6. The method of claim 1 , wherein Rand R claim 1 , taken together with the carbon atom to which they are attached claim 1 , form a 3-membered carbocyclic ring.7. The method of claim 1 , wherein Ris methyl claim 1 , optionally wherein Ris methyl.8. (canceled)9. The method of claim 1 , wherein Rand R claim 1 , taken together with the carbon atom to which they are attached claim 1 , form a 3-membered carbocyclic ring.10. The method of claim 1 , wherein G is —CRRNRR claim 1 , and Rand R claim 1 , taken together with the atoms to which they are attached claim 1 , form a 6-membered heterocyclic ring claim 1 , optionally wherein Ris methyl.11. (canceled)12. The method of claim 1 , wherein G is —NRR claim 1 , and Rand R claim 1 , taken together with the atoms to which they are attached claim 1 , form a 4- or 6-membered heterocyclic ring.13. (canceled)14. (canceled)17. (canceled)18. (canceled)20. The method of wherein L is a 3- claim 19 , 4- claim 19 , 5- claim 19 , 6- claim 19 , 7- claim 19 , or 8-membered cycloalkyl ring or a 6-membered aryl ring.21. The method of wherein L is Calkyl.22. (canceled)23. The method of wherein A is a 3- claim 19 , 4- claim 19 , 5- claim 19 , 6- claim 19 , 7- claim 19 , or 8-membered monocyclic heterocycloalkyl ring claim 19 , a 6- claim 19 , 7- claim 19 , or 8-membered bicyclic heterocycloalkyl ring claim 19 , or a 5- or 6-membered heteroaryl ring.25. (canceled)26. (canceled)27. (canceled)28. (canceled)29. The ...

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Номер записи: 33
07-01-2021 дата публикации

Compound, Photopolymerization Initiator Containing Said Compound, and Photosensitive Resin Composition Containing Said Photopolymerization Initiator

Номер: US20210002216A1
Автор: KUWABARA Hirokazu, TERADA Kiwamu
Принадлежит:

This compound, which absorbs long-wavelength active energy rays and generates with high-efficiency radicals and strong bases, and which has excellent reaction efficiency in a base generating chain reaction, is represented by formula (1), where, in formula (1), R, R, R, Rand Rindependently represent a hydroxy group, an alkoxy group, or an organic group other than those substituents, the R's independently represent an organic group including a thioether bond, and ‘A’ represents a substituent represented by formula (1-1) or (1-2), where, in formula (1-1), Rand Rindependently represent a hydrogen atom, an alkyl group or a heterocyclic group, and where, in formula (1-2), Rand Rindependently represent an amino group or a substituted amino group. A photopolymerization initiator can include said compound; and a photosensitive resin composition can include said photopolymerization initiator. 2. The compound according to claim 1 , wherein one of Ris the alkyl group having a thioether bond or the aryl group having a thioether bond claim 1 , and the other is the hydrogen atom claim 1 , the alkyl group having a thioether bond or the aryl group having a thioether bond.3. The compound according to claim 1 , wherein Ris the hydroxy group.4. A photopolymerization initiator containing the compound according to .5. A photosensitive resin composition containing the photopolymerization initiator according to and a polymer precursor capable of being polymerized by irradiation or by both of irradiation and heating in presence of a photopolymerization initiator.6. The photosensitive resin composition according to claim 5 , wherein the polymer precursor comprises at least one selected from the group consisting of a compound having a substituent selected from the group consisting of an epoxy group claim 5 , an isocyanate group claim 5 , an oxetane group claim 5 , an acryloyl group claim 5 , a methacryloyl group claim 5 , a maleimide group and a thiirane group; a polysiloxane precursor; a ...

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Номер записи: 34
07-01-2021 дата публикации

METHOD OF SYNTHESIS OF AN IONIZABLE CATIONIC LIPID

Номер: US20210002217A1
Автор: Chivukula Padmanabh, Payne Joseph E.
Принадлежит:

What is described is a method of synthesis of the compound of formula 1A, 2. The method of claim 1 , wherein the nucleic acid is an RNA.3. The method of claim 2 , wherein the RNA is siRNA claim 2 , mRNA claim 2 , or miRNA.4. The method of claim 1 , wherein the target cell is a lung epithelial cell.5. The method of claim 1 , wherein the target cell is a hepatocyte.6. The method of claim 1 , wherein the lipid formulation is a lipid nanoparticle or a liposome.7. The method of claim 6 , wherein 30-70% of the lipids in the lipid formulation are a compound having Formula IA.8. The method of claim 7 , wherein 5-30% of the lipids in the lipid formulation are a helper lipid.9. The method of claim 7 , wherein 20-40% of the lipids in the lipid formulation are cholesterol.10. The method of claim 1 , wherein the composition is administered in an aqueous solution to a subject via inhalation.11. The method of claim 10 , wherein the composition is administered to the subject via pulmonary inhalation.12. The method of claim 10 , wherein the aqueous solution is aerosolized claim 10 , atomized claim 10 , or nebulized.16. The method of claim 1 , wherein the nucleic acid is a mRNA and delivery of the mRNA into the target cell results in expression of the mRNA into a protein of interest.17. The method of claim 16 , wherein the protein of interest is an enzyme.18. The method of claim 16 , wherein the protein of interest is an antigen.19. The method of claim 1 , wherein the nucleic acid is an siRNA and delivery of the siRNA into the target cell results in reduced expression of a gene of interest.20. The method of claim 1 , wherein the nucleic acid comprises one or more modified nucleotides selected from phosphorothioates claim 1 , phosphoramidates claim 1 , methyl phosphonates claim 1 , 2′-O-methyl ribonucleotides claim 1 , and peptide-nucleic acids. This application is a continuation of U.S. patent application Ser. No. 15/925,670, filed Mar. 19, 2018, which is a continuation of U.S. ...

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Номер записи: 35
11-01-2018 дата публикации

Cleavable Lipids

Номер: US20180008543A1
Автор: DeRosa Frank, GUILD Braydon Charles, Heartlein Michael, Zhang Jerry Chi
Принадлежит:

Disclosed herein are novel compounds, pharmaceutical compositions comprising such compounds and related methods of their use. The compounds described herein are useful, e.g., as liposomal delivery vehicles to facilitate the delivery of encapsulated polynucleotides to target cells and subsequent iransfection of said target cells, and in certain embodiments are characterized as having one or more properties that afford such compounds advantages relative to other similarly classified lipids. 2. (canceled)3. The nanoparticle of claim 1 , wherein Ris imidazole.4. The nanoparticle of claim 1 , wherein{'sub': '1', 'Ris imidazole;'}andn is 1.5. The nanoparticle of claim 1 , wherein Ris guanidinium.6. The nanoparticle-of claim 1 , wherein{'sub': '1', 'Ris guanidinium;'}andn is 1.723.-. (canceled)2629.-. (canceled)30. The nanoparticle of claim 1 , further comprising one or more compounds selected from the group consisting of a cationic lipid claim 1 , a PEG-modified lipid claim 1 , a non-cationic lipid and a helper lipid.31. (canceled)32. The nanoparticle of claim 1 , wherein one or more of the polynucleotides comprises a chemical modification.33. The nanoparticle of claim 1 , wherein the one or more polynucleotides is selected from the group consisting of an antisense oligonucleotide claim 1 , siRNA claim 1 , miRNA claim 1 , snRNA claim 1 , snoRNA and combinations thereof.34. (canceled)35. The nanoparticle of claim 1 , wherein the one or more polynucleotides comprise DNA.36. The nanoparticle of claim 1 , wherein the one or more polynucleotides comprise RNA.37. (canceled)38. The nanoparticle of claim 36 , wherein the RNA encodes an enzyme.39. The nanoparticle of claim 38 , wherein the enzyme is selected from the group consisting of agalsidase alfa claim 38 , alpha-L-iduronidase claim 38 , iduronate-2-sulfatase claim 38 , N-acetylglucosamine-1-phosphate transferase claim 38 , N-acetylglucosaminidase claim 38 , alpha-glucosaminide acetyltransferase claim 38 , N- ...

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Номер записи: 36
14-01-2016 дата публикации

PHARMACEUTICAL USES OF SULFUR-CONTAINING COMPOUND

Номер: US20160009642A1
Автор: CHEN Chih-Yi, CHEN SHUO-CHUEH, CHIEN YI-CHUNG, HUANG CHIUNG-YAO, Pan Chun-Hsu, SHEU Jyh-Horng, Wu Chieh-Hsi
Принадлежит:

The invention relates to uses of the sulfur-containing compound in inhibiting activities of a factor related to cancer metastasis and/or growth. Preferably, the invention relates to uses of the sulfur-containing compound in inhibiting lung cancer metastasis and/or growth. 19-. (canceled)11. (canceled)12. (canceled)13. (canceled)14. The method according to claim 10 , wherein the lung cancer is non-small cell lung carcinoma.15. The method according to claim 10 , wherein the lung cancer is Lewis lung carcinoma.16. The method according to claim 10 , wherein the compound is administered by injection. 1. Field of the InventionThe invention relates to uses of a sulfur-containing compound. Said sulfur-containing compound has ability to inhibit activities of a factor related to cancer metastasis and/or growth and to inhibit lung cancer metastasis and/or growth.2. Description of the Related ArtNon-small cell lung cancer (NSCLC) is one of the main causes of cancer death, and its incidence is increasing. Surgery, radiotherapy, and chemotherapy are the major treatment methods to reduce lung cancer mortality (Saba, N. F.; Khuri, F. R. Chemoprevention strategies for patients with lung cancer in the context of screening. 2005, 7, 92-99), however, these treatments have harmful side effects on normal healthy cells in the human body. Therefore, it is important to discover new agents to treat lung cancer safely without affecting the body's healthy cells. The deregulation of signaling pathways such as PI3K/Akt is often implicated in the pathogenesis of NSCLC (Li, C. M.; Narayanan, R.; Lu, Y.; Hurh, E.; Coss, C. C.; Barrett, C. M.; Miller, D. D.; Dalton, J. T. 2-Arylthiazolidine-4-carboxylic acid amides (ATCAA) target dual pathways in cancer cells: 5′-AMP-activated protein kinase (AMPK)/mTOR and PI3K/Akt/mTOR pathways. 2010, 37, 1023-1030). Thus, the need for the accelerated development of effective NSCLC therapies is critical. At present, the design of new therapeutic strategies ...

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Номер записи: 37
14-01-2016 дата публикации

POTENT AND SELECTIVE INHIBITORS OF MONOAMINE TRANSPORTERS; METHOD OF MAKING; AND USE THEREOF

Номер: US20160009644A1
Автор: Cao Jianjing, Newman Amy Hauck, OKUNOLA-BAKARE OLUYOMI M
Принадлежит: THE UNITED STATES OF AMERICA, AS REPRESENTED BY TH SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICE

Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds. 2. A compound or salt of in which each of Rand Rindependently is an optionally substituted C-Caryl group.3. A compound or salt of in which Y is S or S(O).4. A compound or salt of any one of in which Z is O or 2H.5. A compound or salt of any one of wherein the substitution on Rand Rare independently chosen from halogen claim 1 , hydroxyl claim 1 , amino claim 1 , nitro claim 1 , cyano claim 1 , C-Calkyl claim 1 , —COOH claim 1 , —CHO claim 1 , —CONH claim 1 , C-Calkoxy claim 1 , C-Calkanoyl claim 1 , mono- or di-C-Calkylamino claim 1 , C-Chaloalkyl claim 1 , or C-Chaloalkoxy.6. A compound or salt of any one of wherein when Rand Rtogether with the adjacent nitrogen atom form a substituted heterocycloalkyl or substituted mono- or bicyclic heteroaryl claim 1 , each substitution is independently chosen from halogen claim 1 , hydroxyl claim 1 , amino claim 1 , nitro claim 1 , cyano claim 1 , C-Calkyl claim 1 , —COOH claim 1 , —CHO claim 1 , —CONH claim 1 , C-Calkoxy claim 1 , C-Calkanoyl claim 1 , mono- or di-C-Calkylamino claim 1 , C-Chaloalkyl claim 1 , or C-Chaloalkoxy.9. A compound or salt of in whichY is S or S(O);Z is 2H; and{'sub': '3', 'Ris ethyl, propyl, butyl, allyl, cyclopropylmethyl, 2-arylethyl, 3-arylpropyl, or 4-arylbutyl.'}11. A compound or salt of in which each of Rand Rindependently is an optionally substituted C-Caryl group;Y is S or ...

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Номер записи: 38
09-01-2020 дата публикации

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Номер: US20200009103A1
Автор: AHLMARK Marko, DIN BELLE David, KAUPPALA Mika, LUIRO Anne, MESSINGER Josef, PAJUNEN Taina, PYSTYNEN Jamo, TIAINEN Eija, VAISMAA Matti
Принадлежит:

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed. 127-. (canceled)29. The method of claim 28 , wherein the compound of formula I is (E)-4 claim 28 ,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile claim 28 , (E)-2-(3 claim 28 ,3-dimethylbut-1-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , (Z)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (E)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (Z)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile claim 28 , (E)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-vinylisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile claim 28 , 2-allyl-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4 claim 28 ,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile.30. The method of claim 28 , wherein the disease or condition is hypertension claim 28 , heart failure claim 28 , depression claim 28 , diabetic vascular dysfunction claim 28 , pain claim 28 , or restless leg syndrome.31. The method of claim 28 , wherein the mammal is a human. The present invention relates to pharmacologically active 2-substituted 4,5-dihydroxyisophthalonitriles, or pharmaceutically acceptable salts and esters thereof, as well as to pharmaceutical compositions containing them and to their use as inhibitors of the catechol O-methyltransferase (COMT) enzyme.Dopamine is deficient in the brain of patients suffering from Parkinson's disease. Levodopa is used orally in the treatment of Parkinson's disease. Levodopa is a dopamine precursor, which is ...

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Номер записи: 39
11-01-2018 дата публикации

Process for the preparation of a polyunsaturated ketone compound

Номер: US20180009745A1
Автор: Inger-Reidun AUKRUST, Marcel Sanderberg
Принадлежит: Avexxin AS

A process for the preparation of a polyunsaturated thiol comprising: (1) reacting a polyunsaturated alcohol in the presence of a compound of formula R 2 —SO 2 Hal wherein R 2 is a C 1-20 hydrocarbyl group, such an C 1-10 alkyl group, to form a polyunsaturated sulphonyl ester; (2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula − SC(═O)R 4 wherein R 4 is a C 1-20 hydrocarbyl group; (3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate. (4) reacting said polyunsaturated thiol with a compound (LG)R 3 COX wherein X is an electron withdrawing group and R 3 is an alkylene group carrying a leaving group (LG), such as LG-CH 2 — forming where X is an electron withdrawing group and LG is a leaving group; optionally in the presence of an antioxidant, so as to form a polyunsaturated ketone compound.

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Номер записи: 40
08-01-2015 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20150011597A1
Автор: Hegde Sharath, Marquess Daniel
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC.

The invention is directed to compounds of formula I: 136-. (canceled)37. A method for treating hypertension , comprising administering to a patient a therapeutically effective amount of a compound having both ATreceptor-antagonizing activity and neprilysin enzyme-inhibiting activity.38. The method of claim 37 , wherein the compound has a pKvalue for binding to an ATreceptor greater than or equal to about 5.0 and a pICvalue for the inhibition of the neprilysin enzyme greater than or equal to about 5.0.39. The method of claim 38 , wherein the compound has a pKvalue greater than or equal to about 6.0.40. The method of claim 39 , wherein the compound has a pKvalue within the range of about 8.0-10.0.41. The method of claim 38 , wherein the compound has a pICvalue greater than or equal to about 6.0.42. The method of claim 41 , wherein the compound has a pICvalue within the range of about 7.0-10.0.43. (canceled)44. A method for treating heart failure claim 41 , comprising administering to a patient a therapeutically effective amount of a compound having both ATreceptor-antagonizing activity and NEP enzyme-inhibiting activity.45. The method of claim 44 , wherein the compound has a pKvalue for binding to an ATreceptor greater than or equal to about 5.0 and a pICvalue for the inhibition of the neprilysin enzyme greater than or equal to about 5.0.46. (canceled)47. A method of treating a patient suffering from a disease or disorder that is treated by antagonizing the ATreceptor and/or inhibiting the NEP enzyme claim 44 , comprising administering to a patient a therapeutically effective amount of a compound having both ATreceptor-antagonizing activity and NEP enzyme-inhibiting activity.48. The method of claim 47 , wherein the compound has a pKvalue for binding to an ATreceptor greater than or equal to about 5.0 and a pICvalue for the inhibition of the neprilysin enzyme greater than or equal to about 5.0.4954-. (canceled) This application claims the benefit of U.S. Provisional ...

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Номер записи: 41
14-01-2021 дата публикации

LINKER OF BIOPROBES

Номер: US20210011012A1
Автор: CHEN YU-CHE, LI CHING-WEN
Принадлежит:

A linker of bioprobes, suitable for immobilizing a bioprobe on a chip substrate of a sensor, includes SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of 6 or more, m and n being integers greater than 1. When an average surface roughness (Ra) of the chip substrate is greater than 250 nm, coverage of the linker on the chip substrate is 40%-80%. A further linker of bioprobes, includes SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of less than 6, m and n being integers greater than 1. When an average surface roughness (Ra) of the chip substrate is less than 250 nm, coverage of the linker on the chip substrate is 65%-100%. The optimal carbon chain length of the linker and the coverage are realized for substrates of various roughnesses, and grasping ability of an electrochemical sensor chip for a detected object are enhanced. 1. A linker of bioprobes , suitable for immobilizing a bioprobe on a chip substrate of a sensor , comprising:SH—(CH)n-NH2, SH—(CH)n-COOH, SH—(CH)n-SH, (OH)m-(CH)n-COOH or (OH)m-(CH)n-NH2, having a carbon number of 6 or more, m and n being integers greater than 1,wherein when an average surface roughness (Ra) of the chip substrate is greater than 250 nm, a coverage of the linker on the chip substrate is in a range of 40% to 80%.2. The linker of bioprobes according to claim 1 , wherein a material of the chip substrate of the sensor is silicon claim 1 , glass claim 1 , graphene claim 1 , gold claim 1 , platinum or polymers.3. The linker of bioprobes according to claim 1 , wherein the chip substrate is subjected to surface treatment according to a proportion of 1 part of 98 wt % sulfuric acid and 3 parts of 33 wt % hydrogen peroxide claim 1 , and a specific roughness is obtained by different treatment time.4. The linker of bioprobes according to claim 1 , further comprising: soaking the chip substrate into a solution of a linker dissolved in 99.8 ...

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Номер записи: 42
15-01-2015 дата публикации

FUNGICIDAL PYRAZOLE MIXTURES

Номер: US20150018374A1
Автор: Bereznak James Francis, Long Jeffrey Keith, Taggi Andrew Edmund
Принадлежит:

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, 2. The composition of wherein component (a) comprises a compound of Formula 1 or salt thereof.3. The composition of wherein component (a) comprises a compound selected from the group consisting of4-(2-chloro-4-fluorophenyl)-N-(2-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-chloro-4-fluorophenyl)-N-(2-chlorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,N-(2-bromophenyl)-4-(2-chloro-4-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-chlorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-bromophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-chloro-4-fluorophenyl)-N-(2,6-difluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-chloro-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,N-(2-bromo-6-fluorophenyl)-4-(2-chloro-4-fluoromethyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2,6-difluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine,4-(2-bromo-4-fluorophenyl)-N-(2-chloro-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine, and4-(2-bromo-4-fluorophenyl)-N-(2-bromo-6-fluorophenyl)-1,3-dimethyl-1H-pyrazol-5-amine.4. The composition of further comprising (c) at least one additional compound or agent that is biologically active.5. The composition of wherein component (c) comprises at least one fungicidal compound selected from the group consisting of:(c1) methyl benzimidazole carbamate fungicides;(c2) dicarboximide fungicides;(c3) demethylation inhibitor fungicides;(c4) phenylamide fungicides;(c5) amine/morpholine fungicides;(c6) phospholipid biosynthesis inhibitor fungicides;(c7) carboxamide fungicides;(c8) hydroxy(2-amino-)pyrimidine fungicides;(c9) anilinopyrimidine fungicides;(c10) N-phenyl carbamate fungicides;(c11) quinone outside inhibitor fungicides;(c12) ...

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Номер записи: 43
21-01-2021 дата публикации

Polycyclic aromatic compounds and methods for making and using the same

Номер: US20210017110A1
Автор: Khagendra HAMAL, Paban SITAULA, Wenlong Yang, Wesley CHALIFOUX
Принадлежит: Nevada System of Higher Education NSHE

Disclosed herein are embodiments of polycyclic aromatic compounds and methods of making and using the same. Various different types of polycyclic ring systems are disclosed, including, but not limited to, polymeric aromatic compounds (e.g., nanographene compounds), pentacene-like compounds, chiral aromatic compounds, asymmetric arene compounds formed from naphthalene-, anthracene-, phenanthrene-, and pyrene-based starting compounds, and dimerized aromatic compounds. Also disclosed herein are novel benzannulation-based methods for making the disclosed polycyclic aromatic compounds.

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Номер записи: 44
28-01-2016 дата публикации

Perfluoroalkyl Composition with Reduced Chain Length

Номер: US20160023033A1
Автор: Martin Thomas Joseph
Принадлежит:

Novel fluorosurfactants are provided that contain perfluoroalkyl groups no longer than perfluorohexyl (C). The surfactants are useful in the preparation of aqueous film forming foams (AFFF) and alcohol-resistant film-forming foams (AR-AFFF) for firefighting. Unexpectedly, these compounds have activity in AFFF and AR-AFFF applications that is comparable and even superior to conventional surfactants that contain perfluoroalkyl groups that are perfluorooctyl (C) and longer. Also provided are methods of making the novel surfactants, as well as foam concentrates, methods of making foam and methods of fighting fires using foam containing the novel surfactants. 2. The composition according to wherein Ris CF(CF).3. The composition according to wherein A is —CHCH—S—.4. The composition according to wherein m is 4.5. The composition according to wherein X is —S—.6. The composition according to wherein the weight average molecular weight of said surfactant is 750-7500.8. The composition according to wherein p is 4-20.9. An aqueous firefighting composition concentrate comprising an effective amount of a composition according to claim 1 , wherein said firefighting composition is substantially free of any surfactant containing a perfluoroalkyl group containing more than 6 carbon atoms.10. (canceled)11. The composition according to claim 9 , wherein said composition further comprises an effective amount of one or more components selected from the group consisting of: an amphoteric hydrocarbon surfactant claim 9 , an anionic hydrocarbon surfactant claim 9 , a nonionic hydrocarbon surfactant claim 9 , a Cfluorochemical surfactant claim 9 , a foam aid claim 9 , a freeze protection composition claim 9 , a composition comprising ion sequestering claim 9 , buffer claim 9 , and anti-corrosion components claim 9 , a polymeric film forming composition claim 9 , a biocides and antimicrobial composition claim 9 , an electrolyte composition claim 9 , and a polysaccharide gum thickener.12. The ...

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Номер записи: 45
10-02-2022 дата публикации

Compositions for controlled release of cysteamine and systemic treatment of cysteamine sensitive disorders

Номер: US20220040127A1
Автор: Patrice P. RIOUX, Vincent P. Stanton, Jr.
Принадлежит: Thiogenesis Therapeutics Inc

The invention features compositions, methods, and kits containing (i) one or more cysteamine precursor compounds convertible to cysteamine in vivo, and (ii) optionally agents to enhance that conversion, formulated to produce a spectrum of pharmacokinetic profiles of cysteamine that can be tailored to individual patients and diseases. The invention also features varying modes of administration of the therapeutic substances in the treatment of cystinosis and other cysteamine sensitive disorders. In particular, formulations combining active ingredient(s) with pharmaceutical excipients that permit sustained cysteamine plasma concentrations are featured.

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Номер записи: 46
17-04-2014 дата публикации

SYNTHESIS AND GROWTH REGULATORY ACTIVITY OF A PROTOTYPE MEMBER OF A NEW FAMILY OF AMlNOTHIOL RADIOPROTECTORS

Номер: US20140107216A1
Автор: Fahl William E.
Принадлежит:

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule. 120.-. (canceled)21. A systemically administered radioprotector comprising a free thiol and a positively-charged backbone.22. The systemically administered radioprotector of wherein the positively-charged backbone comprises an amine.24. The systemically administered radioprotector of wherein administering systemically to a subject the systemically administered radioprotector does not cause a side effect of nausea claim 21 , vomiting claim 21 , hypotension claim 21 , or fainting in the subject.25. The systemically administered radioprotector of wherein the systemically administered radioprotector is sulfurous odor-free.26. A complex comprising the systemically administered radioprotector of bound to the positively-charged backbone of a DNA.27. The complex of wherein the systemically administered radioprotector displays the free thiol away from the DNA.28. A cell comprising the systemically administered radioprotector of .29. A cell comprising the complex of . This application claims priority to U.S. Pat. Appl. Ser. No. 61/713,050, which is incorporated herein by reference in its entirety.The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective ...

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Номер записи: 47
17-04-2014 дата публикации

SYNTHESIS AND GROWTH REGULATORY ACTIVITY OF A PROTOTYPE MEMBER OF A NEW FAMILY OF AMlNOTHIOL RADIOPROTECTORS

Номер: US20140107217A1
Автор: William E. Fahl
Принадлежит: Individual

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methyl-amino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule.

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Номер записи: 48
10-02-2022 дата публикации

PREPARATION OF SULFONAMIDE HERBICIDE PROCESS INTERMEDIATES

Номер: US20220041554A1
Автор: Devaraj Jayachandran, Gullo Michael, Hazari Amaruka, Kruper Will, Ober Matthias S., Ondari Mark E., Oppenheimer Jossian
Принадлежит: CORTEVA AGRISCIENCE LLC

Improved methods for preparing chemical precursors to sulfonyl chloride III, which are important intermediates in the preparation of pyroxsulam herbicide are provided. Specifically, these precursors are compounds of Formulas VII and/or VIII, and IX, wherein R is a C-Calkyl, Ris a C-Calkyl, X is Cl or OH, Y is halogen, OH, or OR, and Ris a C-Calkyl. 2. The method of claim 1 , further comprising preparing the compound of Formula IV by a method by combining an alkyl mercaptan RSH claim 1 , a haloacetonitrile Y—CHCN claim 1 , and a second base claim 1 , wherein R is a C-Calkyl claim 1 , and Y is a halogen.4. The method of claim 3 , wherein the acid is HSO claim 3 , HCl claim 3 , HBr claim 3 , HI or p-toluenesulfonic acid.5. The method of claim 3 , wherein the alcohol is a C-Calcohol.6. The method of claim 3 , wherein the alkoxide is a C-Csodium or potassium alkoxide.7. The method of claim 3 , wherein the dehydrative halogenating reagent is SOCl claim 3 , SOBr claim 3 , POCl claim 3 , POBr claim 3 , PCl claim 3 , PBr claim 3 , PClor PBr claim 3 , or oxalyl chloride claim 3 , and combinations thereof.8. The method of claim 3 , wherein the alcohol is methanol.9. The method of claim 3 , wherein the alkoxide is sodium methoxide or potassium methoxide.10. The method of claim 3 , wherein the combining includes the simultaneous combination of the acid and the alcohol with the compound of Formula VII or Formula VIII claim 3 , or mixtures thereof claim 3 , to provide the compound of Formula IX wherein R is a C-Calkyl claim 3 , and Y is OR claim 3 , wherein Ris a C-Calkyl.11. The method of claim 3 , wherein the combining includes the simultaneous combination of the acid and water with the compound of Formula VII or Formula VIII claim 3 , and mixtures thereof claim 3 , to provide the compound of Formula IX wherein R is a C-Calkyl claim 3 , and Y is OH.12. The method of claim 3 , wherein the combining includes the sequential combination of an acid that is HCl or HBr claim 3 , and ...

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Номер записи: 49
29-01-2015 дата публикации

METHODS FOR REDUCING TRIGLYCERIDE, TOTAL CHOLESTEROL AND LOW DENSITY LIPOPROTEIN BLOOD LEVELS

Номер: US20150031769A1
Автор: MATSUDA Kazuko
Принадлежит: MediciNova, Inc.

A compound of Formula (I): 4. The method of claim 1 , in which the subject is diagnosed with hypertriglyceridemia.5. The method of claim 1 , in which the compound is administered orally.6. The method of claim 1 , in which the compound is administered once daily claim 1 , twice daily claim 1 , or thrice daily.7. The method of claim 1 , in which the compound is administered as a liquid or solid dosage form.8. The method of claim 1 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form (“substantially free of other polymorphic forms”—mention in the specification but not in the claims).9. The method of claim 1 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 1 ,000 mg/day claim 1 , optionally divided into one claim 1 , two claim 1 , or three portions.10. The method of claim 1 , in which the compound is administered at a dosage of 50 mg claim 1 , 75 mg claim 1 , 100 mg claim 1 , 200 mg claim 1 , 500 mg claim 1 , 750 mg claim 1 , or 1 claim 1 ,000 mg once a day claim 1 , twice a day claim 1 , or three times a day.14. The method of claim 11 , in which the subject is diagnosed with hypercholesterolemia.15. The method of claim 11 , in which the compound is administered orally.16. The method of claim 11 , in which the compound is administered once daily claim 11 , twice daily claim 11 , or thrice daily.17. The method of claim 11 , in which the compound is administered as a liquid or solid dosage form.18. The method of claim 11 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form.19. The method of claim 11 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 11 ,000 mg/day claim 11 , optionally divided into one claim 11 , two claim 11 , or three portions.20. The method of claim 11 , in which the compound is administered at a dosage of 50 mg claim 11 , 75 mg claim 11 , 100 mg ...

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Номер записи: 50
17-02-2022 дата публикации

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Номер: US20220047540A1
Автор: AHLMARK Marko, DIN BELLE David, KAUPPALA Mika, LUIRO Anne, MESSINGER Josef, PAJUNEN Taina, PYSTYNEN Jarmo, TIAINEN Eija, VAISMAA Matti
Принадлежит:

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed. 127-. (canceled)29. The method of claim 28 , wherein the compound of formula I is (E)-4 claim 28 ,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile claim 28 , (E)-2-(3 claim 28 ,3-dimethylbut-1-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , (Z)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (E)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (Z)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile claim 28 , (E)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-vinylisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile claim 28 , 2-allyl-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4 claim 28 ,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile.30. The method of claim 28 , wherein the disease or condition is hypertension claim 28 , heart failure claim 28 , depression claim 28 , diabetic vascular dysfunction claim 28 , pain claim 28 , or restless leg syndrome.31. The method of claim 28 , wherein the mammal is a human. The present invention relates to pharmacologically active 2-substituted 4,5-dihydroxyisophthalonitriles, or pharmaceutically acceptable salts and esters thereof, as well as to pharmaceutical compositions containing them and to their use as inhibitors of the catechol O-methyltransferase (COMT) enzyme.Dopamine is deficient in the brain of patients suffering from Parkinson's disease. Levodopa is used orally in the treatment of Parkinson's disease. Levodopa is a dopamine precursor, Which is ...

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Номер записи: 51
31-01-2019 дата публикации

CATECHOL O-METHYLTRANSFERASE ACTIVITY INHIBITING COMPOUNDS

Номер: US20190029990A1
Автор: AHLMARK Marko, DIN BELLE David, KAUPPALA Mika, LUIRO Anne, MESSINGER Josef, PAJUNEN Taina, PYSTYNEN Jarmo, TIAINEN Eija, VAISMAA Matti
Принадлежит:

Compounds of formula (I), wherein Ris as defined in the claims, exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors. Methods of treatment and pharmaceutical dosage forms are also disclosed. 127-. (canceled)29. The method of claim 28 , wherein the compound of formula I is (E)-4 claim 28 ,5-dihydroxy-2-(pent-1-enyl)isophthalonitrile claim 28 , (E)-2-(3 claim 28 ,3-dimethylbut-1-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , (Z)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (E)-4 claim 28 ,5-dihydroxy-2-(prop-1-enyl)isophthalonitrile claim 28 , (Z)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-enyl)isophthalonitrile claim 28 , (E)-2-(but-2-enyl)-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(2-methylprop-1-enyl)isophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-vinylisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(prop-1-en-2-yl)isophthalonitrile claim 28 , 2-allyl-4 claim 28 ,5-dihydroxyisophthalonitrile claim 28 , 4 claim 28 ,5-dihydroxy-2-(3-methylbut-2-en-2-yl)isophthalonitrile or (E)-4 claim 28 ,5-dihydroxy-2-(4-methylpent-1-enyl)isophthalonitrile.30. The method of claim 28 , wherein the disease or condition is hypertension claim 28 , heart failure claim 28 , depression claim 28 , diabetic vascular dysfunction claim 28 , pain claim 28 , or restless leg syndrome.31. The method of claim 28 , wherein the mammal is a human. The present invention relates to pharmacologically active 2-substituted 4,5-dihydroxyisophthalonitriles, or pharmaceutically acceptable salts and esters thereof, as well as to pharmaceutical compositions containing them and to their use as inhibitors of the catechol O-methyltransferase (COMT) enzyme.Dopamine is deficient in the brain of patients suffering from Parkinson's disease. Levodopa is used orally in the treatment of Parkinson's disease. Levodopa is a dopamine precursor, which is ...

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Номер записи: 52
01-02-2018 дата публикации

DETERMINATION OF AQUEOUS NITRATE CONCENTRATION

Номер: US20180031536A1
Автор: Greenawalt Angella Nicholle, MacFarland Darren Kent
Принадлежит:

A method of measuring nitrate concentration in an aqueous sample includes mixing the aqueous sample with a water-soluble thioether chosen to reduce nitrate in the aqueous sample to nitrite in the presence of a water soluble catalyst, and a water soluble reagent system adapted to interact with nitrite to generate a color; measuring color generation, and correlating the color generation to nitrate concentration. 1. A method of measuring nitrate concentration in an aqueous sample , comprisinga. mixing the aqueous sample with a water-soluble thioether chosen to reduce nitrate in the aqueous sample to nitrite in the presence of a water soluble catalyst, and a water soluble reagent system adapted to interact with nitrite to generate a color,b. measuring color generation, andc. correlating the color generation to nitrate concentration.2. The method of wherein the water soluble thioether comprises a thioether-containing a five-membered claim 1 , aromatic heterocyclic compound claim 1 , a phenylalkyl thioether or a substituted phenylalkyl thioether.4. The method of wherein the hydrophilic polymer is a polyalkyleneoxide.5. The method of wherein at least one of R claim 3 , R claim 3 , R claim 3 , R claim 3 , and Ris —ORwherein Ris selected from the group consisting of H claim 3 , a C-Calkyl group claim 3 , a C-Csulfonate terminated alkyl group claim 3 , a phenyl group claim 3 , and a polyalkylene oxide group claim 3 , —NRRwherein RE and Rare selected independently from the group consisting of H claim 3 , a C-Calkyl group claim 3 , a C-Csulfonate terminated alkyl group claim 3 , and a polyalkylene oxide group claim 3 , a dihydroxybenzene group claim 3 , a phenyl diamine group claim 3 , a phenyl diether group claim 3 , a carboxy late group claim 3 , and a polyalkyleneoxide group; or Rand Rtogether form a chain of four or five members selected from the group of CH claim 3 , CH claim 3 , NH claim 3 , CC(O)OH or NR claim 3 , wherein Ris an C-Calkyl group or C-Csulfonate terminated ...

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Номер записи: 53
05-02-2015 дата публикации

CHROMENE COMPOUND

Номер: US20150034887A1
Автор: Izumi Shinobu, Momoda Junji, Shimizu Yasutomo
Принадлежит: TOKUYAMA CORPORATION

A novel photochromic compound which develops a color of a neutral tint (double peak characteristic) and has high color optical density, high fading speed and excellent durability. 2. A photochromic curable composition which comprises the chromene compound of and polymerizable monomers.3. A photochromic optical article having a polymer molded body containing the above chromene compound of dispersed therein as a constituent member.4. An optical article having an optical substrate at least one surface or all of which is covered with a polymer film containing the chromene compound of dispersed therein as a constituent member. The present invention relates to a novel chromene compound which is useful as a photochromic compound for photochromic spectacle lenses.Photochromism is the reversible function of a certain compound that it changes its color swiftly upon exposure to light including ultraviolet light such as sunlight or light from a mercury lamp and returns to its original color when it is put in the dark by stopping its exposure to light. A compound having this property is called “photochromic compound” and used as a material for photochromic plastic lenses.For the photochromic compound used for this purpose, the following properties are required: (I) the degree of coloration at a visible light range before ultraviolet light is applied (to be referred to as “initial coloration” hereinafter) should be low, (II) the degree of coloration upon exposure to ultraviolet light (to be referred to as “color optical density” hereinafter) should be high, (III) the speed from the time when the application of ultraviolet light is started to the time when the color optical density reaches saturation (to be referred to as “color development sensitivity” hereinafter) should be high; (IV) the speed from the stoppage of the application of ultraviolet light to the time when the compound returns to its original state (to be referred to as “fading speed” hereinafter) should be high, (V) ...

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Номер записи: 54
09-02-2017 дата публикации

PHENYL BENZYL ETHER DERIVATIVE AND PREPARATION METHOD AND APPLICATION THEREOF

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

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

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Номер записи: 55
24-02-2022 дата публикации

SULFINYLAMINOBENZAMIDE AND SULFONYLAMINOBENZAMIDE DERIVATIVES

Номер: US20220055985A1
Автор: FARAND Julie, KAPLAN Joshua A., Notte Gregory, OLEN Casey Lockwood, Sangi Michael, Sperandio David
Принадлежит:

Provided is a compound of Formula (I): 25-. (canceled)6. The method of claim 1 , wherein Ris selected from the group consisting of: Calkyl claim 1 , —NRR claim 1 , 6-10 membered aryl claim 1 , 5-10 membered heteroaryl claim 1 , Ccycloalkyl claim 1 , and 4-12 membered heterocyclyl claim 1 , wherein each Calkyl claim 1 , 6-10 membered aryl claim 1 , 5-10 membered heteroaryl claim 1 , Ccycloalkyl claim 1 , and 4-12 membered heterocyclyl is further substituted with one or more Rgroups.7. The method of claim 1 , wherein Ris selected from the group consisting of: —H claim 1 , —CN claim 1 , —F claim 1 , methyl claim 1 , methoxy and Chaloalkoxy.8. The method of claim 7 , wherein Ris selected from the group consisting of: —H and —F.9. The method of claim 1 , wherein Ris selected from the group consisting of: —H claim 1 , halo claim 1 , —OH claim 1 , —CN claim 1 , Calkyl claim 1 , Calkoxy claim 1 , Chydroxyalkyl claim 1 , Cheteroalkyl claim 1 , —SF claim 1 , —S(O)R claim 1 , —S(O)(NH)R claim 1 , —S(O)(NR)R claim 1 , —S(O)(NH)NRR claim 1 , —S(O)(NR)NRR claim 1 , —NRSOR claim 1 , —NRS(O)NRR claim 1 , —NRC(O)NRR claim 1 , —NRC(O)OR claim 1 , —C(O)R claim 1 , —C(O)OR claim 1 , —C(O)NRR claim 1 , and —NO claim 1 , wherein each of the Calkyl claim 1 , Calkoxy claim 1 , Chydroxyalkyl claim 1 , and Cheteroalkyl claim 1 , is further substituted with one or more Rgroups.10. The method of claim 9 , wherein Ris selected from the group consisting of: —H claim 9 , —F claim 9 , —Cl claim 9 , —OH claim 9 , —CN claim 9 , —S(O)R claim 9 , —C(O)R claim 9 , —SF claim 9 , —NO claim 9 , Calkyl claim 9 , and Calkoxy claim 9 , and wherein said Calkyl or Calkoxy is optionally substituted with one or more —F claim 9 , and Ris selected from the group consisting of Calkyl claim 9 , Ccycloalkyl claim 9 , Chydroxyalkyl claim 9 , Cheteroalkyl claim 9 , wherein the Calkyl claim 9 , Ccycloalkyl claim 9 , Chydroxyalkyl claim 9 , and Cheteroalkyl claim 9 , are optionally substituted with one or more Rgroups ...

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Номер записи: 56
06-02-2020 дата публикации

FATTY ACID CYSTEAMINE CONJUGATES AND THEIR USE AS ACTIVATORS OF AUTOPHAGY

Номер: US20200038342A1
Автор: Jirousek Michael R., Vu Chi B.
Принадлежит:

The invention relates to fatty acid cysteamine conjugates, compositions comprising a fatty acid cysteamine conjugate, and methods for using such conjugates and compositions to treat disease, such as a disease caused by dysregulation of autophagy. 2. The method of claim 1 , wherein the disease is cystic fibrosis.3. The method of claim 1 , wherein the disease is idiopathic pulmonary fibrosis (IPF)4. The method of claim 1 , wherein the disease is Duchenne's Muscular Dystrophy.5. (canceled)6. The method of claim 1 , wherein the subject is a human.8. The method of claim 7 , wherein the administering increases the ratio of light chain 3-II (LC3-II) to light chain 3-I (LC3-I) in the subject by at least 10%.9. The method of claim 7 , wherein the administering decreases the amount of p62 protein in the subject by at least 1% w/w.10. The method of claim 7 , wherein the subject has been diagnosed as having cystic fibrosis or idiopathic pulmonary fibrosis or Duchenne's Muscular Dystrophy.11. The method of claim 7 , wherein the subject is a human.12. The method of claim 1 , wherein the compound is a compound of Formula I or a pharmaceutically acceptable salt thereof.13. The method of claim 7 , wherein the compound is a compound of Formula I-A or a pharmaceutically acceptable salt thereof.1415-. (canceled)16. The method of claim 1 , wherein n* is 2.17. The method of claim 1 , wherein m* is 2.18. The method of claim 1 , wherein Yis a 6-membered heteroaryl optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of alkyl claim 1 , hydroxyl claim 1 , and alkoxyl.19. The method of claim 1 , wherein Yis pyridinyl or pyrimidinyl claim 1 , each of which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 substituents independently selected from the group consisting of alkyl claim 1 , hydroxyl claim 1 , and alkoxyl.2021-. (canceled)23. (canceled)25. (canceled)27. The method of claim 1 , wherein at least one pair of ...

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Номер записи: 57
12-02-2015 дата публикации

ALKYNYL PHENYL DERIVATIVE COMPOUNDS FOR TREATING OPHTHALMIC DISEASES AND DISORDERS

Номер: US20150045444A1
Автор: Gage Jennifer, Gall Anna, Hong Feng, Kuksa Vladimir Aleksandrovich, Little Thomas, Orme Mark W., Scott Ian Leslie
Принадлежит:

Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions. 190-. (canceled)92. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , wherein Ris alkyl.93. The compound of claim 92 , or a pharmaceutically acceptable salt thereof claim 92 , wherein m is 0.94. The compound of claim 93 , or a pharmaceutically acceptable salt thereof claim 93 , wherein Rand Rare each independently hydrogen or C-Calkyl.95. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , wherein Ris aryl.96. The compound of claim 95 , or a pharmaceutically acceptable salt thereof claim 95 , wherein m is 0.97. The compound of claim 96 , or a pharmaceutically acceptable salt thereof claim 96 , wherein Rand Rare each independently hydrogen or C-Calkyl.98. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , wherein Ris carbocyclyl.99. The compound of claim 98 , or a pharmaceutically acceptable salt thereof claim 98 , wherein m is 0.100. The compound of claim 99 , or a pharmaceutically acceptable salt thereof claim 99 , wherein Rand Rare each independently hydrogen or C-Calkyl.101. The compound of claim 91 , or a pharmaceutically acceptable salt thereof claim 91 , chosen from:3-amino-1-(3-(3-hydroxy-3-propylhex-1-ynyl)phenyl)propan-1-one oxime;4-((3-(2-aminoethylamino)-phenyl)ethynyl)heptan-4-ol;4-((3-(2-aminoethylthio)phenyl)ethynyl)heptan-4-ol;4-((3-(2-aminoethylsulfinyl)phenyl)ethynyl)heptan-4-ol; or4-((3-(2-aminoethylsulfonyl)phenyl)ethynyl)heptan-4-ol.1031. A pharmaceutical composition comprising a compound of Formula (A) claim 91 , or pharmaceutically acceptable salt thereof claim 91 , as described in claim claim 91 , and a pharmaceutically acceptable excipient.104. A pharmaceutical composition comprising a compound of ...

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Номер записи: 58
06-02-2020 дата публикации

Compositions and Methods for the Treatment of Xerostomia

Номер: US20200040003A1
Автор: Kandula Mahesh
Принадлежит:

The invention relates to the compounds or its pharmaceutical acceptable polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, formula II, formula III, formula IV and formula V and the methods for the treatment of xerostomia may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of oral mucosal inflammatory, dry mouth or oral dry mouth mediated infectious diseases. 6. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.7. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.8. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.9. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. A Pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.11. The pharmaceutical composition of claim 6 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 6 , delayed release or sustained release claim 6 , transmucosal claim 6 , syrup claim 6 , topical claim 6 , parenteral administration claim 6 , injection claim 6 , subdermal claim 6 , oral solution claim 6 , rectal administration claim 6 , buccal administration or transdermal administration.12. The pharmaceutical composition of claim 7 , which is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 7 , delayed release or sustained release claim 7 , transmucosal claim 7 , syrup claim 7 , topical claim 7 , parenteral administration claim 7 , injection claim 7 , ...

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Номер записи: 59
15-02-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180043009A1
Автор: Butler David, Eltepu Laxman, Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure 125-. (canceled)27. A lipid particle comprising a lipid of .28. The lipid particle of claim 27 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.29. The lipid particle of claim 27 , wherein the lipid particle consists essentially of{'claim-ref': {'@idref': 'CLM-00026', 'claim 26'}, 'a. a lipid of ;'}b. a neutral lipid selected from DSPC, DPPC, POPC, DOPE and SM;c. a sterol; andd. PEG-DMG or PEG-DMA,{'b': 26', '5', '25, 'in a molar ratio of about 20-60% lipid of claim :-% neutral lipid:25-55% stero1:0.5-15% PEG-DMG or PEG-DMA.'}30. The lipid particle of claim 27 , further comprising a therapeutic agent.31. The lipid particle of claim 30 , wherein the therapeutic agent is a nucleic acid.32. The lipid particle of claim 31 , wherein the nucleic acid is a plasmid.33. The lipid particle of claim 31 , wherein the nucleic acid is an immunostimulatory oligonucleotide.34. The lipid particle of claim 31 , wherein the nucleic acid is selected from the group consisting of an siRNA claim 31 , an antisense oligonucleotide claim 31 , a microRNA claim 31 , an antagomir claim 31 , an aptamer claim 31 , and a ribozyme.35. The lipid particle of claim 30 , wherein the therapeutic agent is siRNA.36. The lipid particle of claim 30 , wherein the therapeutic agent is mRNA.37. The lipid particle of claim 29 , wherein the sterol is cholesterol.38. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 27 , carrier claim 27 , or diluent.38. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically acceptable excipient claim 30 , carrier claim 30 , or diluent. This application is a Continuation application of U.S. application Ser. No. 14/629,991, ...

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Номер записи: 60
01-05-2014 дата публикации

LOW VISCOSITY LUBRICATING OIL BASE STOCKS AND PROCESSES FOR PREPARING SAME

Номер: US20140121143A1
Автор: Bodige Satish, Luo Shuji, Patil Abhimanyu Onkar
Принадлежит: EXXONMOBIL RESEARCH AND ENGINEERING COMPANY

A composition that includes one or more compounds represented by the formula 2. The composition of wherein Rand Rare selected from the residue of a mPAO dimer (C-C) claim 1 , trimer (C-C) claim 1 , tetramer (C-C) claim 1 , pentamer (C-C) claim 1 , and hexamer (C-C) claim 1 , or α-olefin (C-C) claim 1 , X is selected from the residue of 1 claim 1 ,2-ethanedithiol claim 1 , 3-mercaptopropionate claim 1 , pentaerythritoltetrakis(3-mercaptopropionate) claim 1 , and trimethylopropanetris(3-mercaptopropionate) claim 1 , a is a value from 1 to 4 claim 1 , and b is a value or 0 or 1.3. The composition of having a Noack volatility of no greater than 20 percent.4. The composition of which is selected from a heteroatom-containing mPAO dimer claim 1 , trimer claim 1 , tetramer claim 1 , pentamer claim 1 , hexamer and higher oligomer claim 1 , or one or more compounds represented by a formula of .5. A composition comprising me or more heteroatom-containing hydrocarbon compounds claim 1 , wherein said one or more heteroatom-containing hydrocarbon compounds are produced by a process comprising reacting a polyalphaolefin oligomer or α-olefin (C-C) with an aliphatic polythiol claim 1 , aromatic polythiol claim 1 , cycloaliphatic polythiol claim 1 , ester or acid containing thiol claim 1 , or ester or acid containing polythiol claim 1 , optionally in the presence of a catalyst claim 1 , under reaction conditions sufficient to produce said one or more heteroatom-containing hydrocarbon compounds.6. The composition of wherein the process is carried out under reaction conditions sufficient to couple the polyalphaolefin oligomer or α-olefin (C-C) with the aliphatic polythiol claim 5 , aromatic polythiol claim 5 , cycloaliphatic polythiol claim 5 , ester or acid containing thiol claim 5 , or ester or acid containing polythiol claim 5 , to produce said heteroatom-containing hydrocarbon compound.7. The composition of having a viscosity (Kv) from 2 to 30 at 100° C. claim 5 , a viscosity index ...

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Номер записи: 61
01-05-2014 дата публикации

LIPID CONTAINING FORMULATIONS

Номер: US20140121393A1
Автор: Akinc Akin, Jayaprakash Narayanannair K., Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, Rajeev Kallanthottathil G.
Принадлежит: TEKMIRA PHARMACEUTICALS CORPORATION

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 2. The compound of claim 1 , wherein Ris H claim 1 , methyl claim 1 , ethyl claim 1 , isopropyl claim 1 , or 2-hydroxyethyl and Ris H claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , or isopropyl.3. The compound of claim 1 , wherein both m and n are 1.4. The compound of claim 1 , wherein both Land Lare —OC(O)— or —C(O)O—.5. The compound of claim 1 , wherein both Land Lare —N(R)C(O)N(R)—.6. The compound of claim 1 , wherein both Land Lare —OC(O)N(R)— or —N(R)C(O)O—.7. The compound of claim 1 , wherein Lis —NRC(O)— and Lis —S—S—.8. The compound of claim 1 , wherein Lis —OC(O)— and Lis —S—S—.9. The compound of claim 1 , wherein Lis —OC(O)N(R) or —N(R)C(O)O— and Lis —S—S—.10. The compound of claim 1 , wherein Lis —N(R)C(O)N(R)— and L2 is —S—S—.11. The compound of claim 1 , wherein L-Rand L-Rare taken together to form an acetal claim 1 , a ketal claim 1 , or an orthoester.12. The compound of claim 1 , wherein both Rand Rare C-Calkyl.13. The compound of claim 12 , wherein each Land Lare independently —S—S— claim 12 , —OC(O)N(R)— or —N(R)C(O)O—.14. The compound of claim 1 , wherein each Rand Rare independently C-Calkenyl.19. A preparation comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof. This application is a divisional application of U.S. patent application Ser. No. 13/211,094, filed on Aug. 16, 2011, which is a continuation application of U.S. patent application Ser. No. 12/056,230, filed on Mar. 26, 2008, which application issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Patent Application No. PCT/US2007/080331, filed on Oct. 3, 2007, and claims priority to U.S. Provisional Application No. 60/828,022 filed on Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed on Dec. 18, 2006. The entire content ...

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Номер записи: 62
14-02-2019 дата публикации

DEUTERATED GFT-505

Номер: US20190047949A1
Автор: Tung Roger D.
Принадлежит:

This invention relates to novel deuterated forms of GFT-505, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are characterized by reduced PPAR-alpha and/or PPAR-delta activity.

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Номер записи: 63
25-02-2016 дата публикации

METAL-CATALYZED COUPLING OF ARYL AND VINYL HALIDES WITH ALPHA, ALPHA-DIFLUOROCARBONYL COMPOUNDS

Номер: US20160052854A1
Автор: CHAKADAJ Wojciech, GE Shaozhong, Hartwig John F.
Принадлежит:

The coupling of aryl, heteroaryl, and vinyl halides with α,α-difluoroketones or silyl ethers or siylenol ethers of α,α-difluoroketones and α,α-difluoroamides and esters are described. Further derivatization of the coupling products (such as ketone cleavage and Baeyer-Villiger oxidation) is also described. 2. The composition according to claim 1 , wherein said complex is present in said composition in an amount of less than 10 mol % relative to said α claim 1 ,α-difluoromethyl carbonyl compound.3. The composition according to claim 2 , wherein said complex is present in said composition in an amount of about 2 mol % to about 5 mol % relative to said α claim 2 ,α-difluoromethyl carbonyl compound.5. The composition according to claim 4 , wherein said complex is present in said composition in an amount of less than 10 mol % relative to said silyl enol ether.6. The composition according to claim 5 , wherein said complex is present in said composition in an amount of about 2 mol % to about 5 mol % relative to said silyl enol ether.76. The composition according to any one of - claims 4 , wherein said composition does not contain BuSnF.87. The composition according to any one of - claims 4 , wherein said composition does not contain an organotin reagent.98. The composition according to any one of - claims 4 , wherein R claims 4 , R claims 4 , and Rare independently selected from unsubstituted C claims 4 , C claims 4 , C claims 4 , C claims 4 , Cand Calkyl.10. The composition according to claim 9 , wherein one or more of R claim 9 , R claim 9 , and Rare methyl.11. The composition according to any preceding claim claim 9 , further comprising a solvent.12. The composition according to claim 11 , wherein said solvent is a non-polar claim 11 , organic solvent.13. The composition according to claim 12 , wherein said solvent is toluene.14. The composition according to any preceding claim claim 12 , wherein said base is a member selected from CsCOand KPO.17. The composition ...

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Номер записи: 64
15-05-2014 дата публикации

Quinone based nitric oxide donating compounds

Номер: US20140135389A1
Автор: Francesca Benedini, Gael Ronsin, Laura Storoni
Принадлежит: Nicox Sa

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 of pathological conditions where a deficit of NO plays an important role in their pathogenesis.

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Номер записи: 65
28-02-2019 дата публикации

Fungicidal pyrazoles

Номер: US20190059377A1
Автор: Andrew Edmund Taggi, Jeffrey Keith Long, Wonpyo Hong
Принадлежит: FMC Corp

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein Q 1 is a phenyl ring, naphthalenyl ring system, a 5- to 6-membered fully unsaturated heterocyclic ring or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; Q 2 is a phenyl ring, a naphthalenyl ring system, a 5- to 6-membered saturated, partially unsaturated or fully unsaturated heterocyclic ring, or an 8- to 10-membered heteroaromatic bicyclic ring system, each as described with optional substituents as defined in the disclosure; X is O, S(O) m , NR 4 , CR 15 R 16 , C(═O) or C(═S); and R 1 , R 1a , R 2 , R 4 , R 15 , R 16 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 2, including all geometric and stereoisomers, and salts thereof, wherein X is NH; and Q 1 , Q 2 and R 2 are as defined for Formula 1; which are useful as intermediates for preparing compounds of Formula 1.

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Номер записи: 66
28-02-2019 дата публикации

SMALL MOLECULES FOR IMMUNOGENIC TREATMENT OF CANCER

Номер: US20190062272A1
Автор: Chimmanamada Dinesh, Ying Weiwen
Принадлежит: Capten Therapeutics Inc.

The present invention relates to new compounds for immunogenic treatment of cancer. The compounds can be administered as a single agent or in combination with an anticancer drug including modulators of other immune pathways, especially immune checkpoint inhibitors that target CTLA-4, PD-1, and PD-L1 proteins. The compounds can produce neoantigens through irreversible protein binding in cancer cells and generate immune response. 3. The compound of claim 1 , wherein said targeting moiety (TM) is an antibody claim 1 , a folate receptor binding moiety claim 1 , a peptide claim 1 , a nanoparticle based delivery vehicle claim 1 , a selective tyrosine kinase inhibitor claim 1 , or an Hsp90 inhibitor.4. The compound of claim 1 , wherein said targeting moiety (TM) is a targeting moiety connected through a nitrogen atom (—N(TM)) or an oxygen atom (—O(TM)) of the targeting moiety.1158-. (canceled)59. The compound of claim 1 , wherein said compound isN-(2-((3,4-dimethoxyphenyl)thio)ethyl)propionamide;N-[2-(3,4-dihydroxyphenyl)sulfanylethyl]propenamide;N-[2-(2,5-dihydroxyphenyl)sulfanylethyl]propenamide;N-[2-(2,3-dihydroxyphenyl)sulfanylethyl]propenamide;4-(2-aminoethylsulfanyl)benzene-1,2-diol;N-[2-(3,4-dimethoxyphenyl) sulfanylethyl]heptanamide;N-[2-(3,4-dihydroxyphenyl)sulfanylethyl]heptanamide;N-[2-(3,4-dihydroxyphenyl)sulfanylethyl]undecanamide;N-[2-(3,4-dimethoxyphenyl)sulfanylethyl]undecanamide;N-[2-(3,4-dihydroxyphenyl)sulfanylethyl]undecanamide;N-[2-(3,4-dimethoxyphenyl)sulfanylethyl]undecanamide;N-[2-(3,4-dihydroxyphenyl)sulfanylethyl]pentanamide;3-(5,5-difluoro-1,3-dimethyl-dipyrrolo[3,1-c:2′,1′-g][1,3,2]diazaborinin-4-ium-7-yl)-N-[2-(3,4-dihydroxyphenyl)sulfanylethyl]propenamide;N-[2-(3,4-dihydroxyphenyl) sulfanylethyl]cyclopentanecarboxamide;3-pentadecylbenzene-1,2-diol;(4Z)-4-[(7-chloro-4-quinolyl)imino]-2-(diethylaminomethyl)cyclohexa-2,5-dien-1-one; or3-[(Z)-pentadec-10-enyl]benzene-1,2-diol.60. The compound of claim 1 , wherein said conjugate is an antibody drug ...

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Номер записи: 67
08-03-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180064807A1
Автор: Butler David, Eltepu Laxman, Jayaraman Muthusamy, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure: 2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. The cationic lipid of claim 1 , wherein X and Y are O.10. (canceled)11. The cationic lipid of claim 1 , wherein Ais —CH—.12. (canceled)13. (canceled)14. The cationic lipid of claim 1 , wherein Z′ is N(Q).15. (canceled)16. (canceled)17. The cationic lipid of claim 1 , wherein Z′ is alkyl.18. The cationic lipid of claim 1 , wherein Ris alkylamine.19. (canceled)20. (canceled)21. The cationic lipid of claim 1 , wherein Q is alkyl.22. (canceled)23. (canceled)24. (canceled)26. (canceled)27. (canceled)28. (canceled)29. (canceled)30. (canceled)31. (canceled)32. (canceled)33. (canceled)34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)41. (canceled)42. (canceled)43. A lipid particle comprising a compound of .44. (canceled)45. A lipid particle comprising a compound of .46. The lipid particle of claim 43 , wherein the particle further comprises a therapeutic agent.47. The lipid particle of claim 45 , wherein the particle further comprises a therapeutic agent.48. (canceled)49. The lipid particle of claim 46 , wherein the therapeutic agent is a nucleic acid.50. The lipid particle of claim 47 , wherein the therapeutic agent is a nucleic acid.51. (canceled)52. The lipid particle of claim 49 , wherein the nucleic acid is siRNA or mRNA.53. The lipid particle of claim 50 , wherein the nucleic acid is siRNA or mRNA.54. (canceled)55. A method of treating a disease or disorder in a subject in need thereof claim 46 , comprising administering to the subject the lipid particle of .56. A method of treating a disease or disorder in a subject in need thereof claim 47 , comprising administering to the subject the lipid particle of . This application ...

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Номер записи: 68
08-03-2018 дата публикации

LIPID CONTAINING FORMULATIONS

Номер: US20180065918A1
Автор: Akinc Akin, Jayaraman Muthusamy, MAIER Martin, Manoharan Muthiah, NAIR Jayaprakash K., Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

Compositions and methods useful in administering nucleic acid based therapies, for example association complexes such as liposomes and lipoplexes are described. 3. A preparation comprising a compound of .4. An association complex comprising a preparation of .5. An association complex comprising a preparation of .6. The association complex of claim 4 , further comprising a therapeutic agent.7. The association complex of claim 6 , wherein the therapeutic agent is nucleic acid.8. The association complex of claim 6 , wherein the therapeutic agent is siRNA.9. The association complex of claim 6 , wherein the therapeutic agent is mRNA.10. The association complex of claim 5 , further comprising a therapeutic agent.11. The association complex of claim 10 , wherein the therapeutic agent is nucleic acid.12. The association complex of claim 10 , wherein the therapeutic agent is siRNA.13. The association complex of claim 10 , wherein the therapeutic agent is mRNA.14. A method of treating a mammal comprising administering to said mammal a therapeutic amount of an association complex of .15. A method of treating a mammal comprising administering to said mammal a therapeutic amount of an association complex of . This application is a Continuation application of U.S. patent application Ser. No. 14/149,496, filed on Jan. 7, 2014, which is a Divisional application of U.S. patent application Ser. No. 13/211,094, filed on Aug. 16, 2011, issued as U.S. Pat. No. 8,642,076 on Feb. 4, 2014, which is a continuation application of U.S. patent application Ser. No. 12/056,230, filed on Mar. 26, 2008, issued as U.S. Pat. No. 8,034,376 on Oct. 11, 2011, which is a continuation application of International Patent Application No. PCT/US2007/080331, filed on Oct. 3, 2007, which claims priority to U.S. Provisional Application No. 60/828,022 filed on Oct. 3, 2006 and U.S. Provisional Application No. 60/870,457 filed on Dec. 18, 2006. The entire content of each of these applications is hereby ...

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Номер записи: 69
12-03-2015 дата публикации

Substituted 2,3-dihydro-1H-inden-1-one Retinoic acid-related orphan nuclear receptor Antagonists for Treating Multiple Sclerosis

Номер: US20150072980A1
Автор: Vankayalapati Hariprasad, Yerramreddy Venkatakrishnareddy
Принадлежит:

The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor γt (RORγt)/RORγ. The compounds of the present invention are useful for modulating RORγt)/RORγ activity and for treating diseases or conditions mediated by RORγt)/RORγ such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is O.3. The compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris.5. The compound according to claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , wherein Ris Calkyl optionally substituted with 1-6 independent halo substituents.11. A method of treatment of multiple sclerosis comprising the step of administering to a patient in need thereof an effective amount of a compound according to .12. A method of treatment of human autoimmune diseases comprising the step of administering to a patient in need thereof an effective amount of a compound according to .13. The method according to wherein the human autoimmune disease is Multiple Sclerosis (MS) claim 12 , Rheumatoid Arthritis (RA) claim 12 , Inflammatory Colitis claim 12 , Psoriasis claim 12 , Chronic Obstructive Pulmonary Disease (COPD) claim 12 , Pain claim 12 , Obesity claim 12 , Diabetes claim 12 , Dyslipidemia claim 12 , Osteoporosis claim 12 , Asthma claim 12 , Neurodegenerative diseases or Cancer.14. The method according to wherein the cancer is gastric cancer claim 13 , colon cancer claim 13 , chronic myelogenic leukemia (CML) claim 13 , acute myelogenic leukemia (AML) claim 13 , squamous cell or ...

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Номер записи: 70
12-03-2015 дата публикации

4-(3-BENZYLOXYPHENYLTHIO)-2-CHLORO-1-(3-NITROPROPYL)BENZENE CRYSTAL

Номер: US20150073178A1
Автор: SATO HIROYA, Tsubuki Takeshi
Принадлежит:

[Problem] For example, 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene (compound 1) is used as an intermediate for producing a 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride which has excellent immunosuppressive activity. This compound 1 is traditionally obtained only as an oil and thus handling and refining were difficult. 1. A crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene , wherein , in powder X-ray diffraction using CuKα radiation with 2θ representing a diffraction angle , a powder X-ray diffraction image including the following 2θ peaks is observed: 2θ: 9.7 , 12.9 , 16.4 , 16.8 , 17.6 , 19.5 , 21.7 , 22.6 , 22.9 , 23.3 , 24.5 , 24.8 , 26.0 , 26.4 , 27.2.2. A crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene , wherein a powder X-ray diffraction image substantially the same as an image in is obtained by powder X-ray diffraction using CuKα radiation with 2θ representing a diffraction angle.3. The crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene according to claim 1 , wherein a melting point of the crystal measured by a hot plate method is 46° C. to 49° C.4. The crystal of 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene according to claim 1 , wherein claim 1 , in thermogravimetric/differential thermal analysis (TG/DTA) of the crystal claim 1 , no reduction in weight is observed until 49° C. claim 1 , and a single endothermic peak is observed at around 50° C.5. A production method of the crystal according to claim 1 , the method including the step of mixing 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene with an alcohol.6. The production method of the crystal according to claim 5 , wherein the 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene is dissolved in a soluble solvent that can dissolve the compound to obtain a solution claim 5 , and the obtained solution of the 4-(3-benzyloxyphenylthio)-2-chloro-1-(3- ...

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Номер записи: 71
24-03-2022 дата публикации

3-SUBSTITUTED PHENYLAMIDINE COMPOUNDS, PREPARATION AND USE THEREOF

Номер: US20220089523A1
Автор: AUTKAR Santosh Shridhar, Garg Ruchi, GUMME Sachin Nagnath, KLAUSENER Alexander G.M., MAHAJAN Vishal A., NAIK Maruti, Rathod Kishor Singh, SIVAKUMAR S., VENKATESHA Hagalavadi M
Принадлежит: PI INDUSTRIES LTD.

The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R, R, R, R, R, R, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent. 2. The compound of formula (I) as claimed in claim 1 , wherein{'sup': '1', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '1', '6', '3', '5', '4', '8, 'Ris selected from the group consisting of C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, C-C-alkoxy, C-C-cycloalkyl and C-C-cycloalkylalkyl;'}{'sup': '2', 'sub': 1', '6', '2', '6', '2', '6', '3', '8', '1', '6, 'Ris selected from the group consisting of C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-cycloalkyl and C-C-haloalkyl;'}{'sup': 3', '4, 'sub': 1', '6', '2', '6', '2', '6', '1', '6', 'n', '3', '8, 'Rand Rare independently selected from the group consisting of X, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, N(R′R′″), OR″, S(O)R′″, (C═O)—R″ and C-C-cycloalkyl;'}{'sup': '5', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '3', '8, 'Ris selected from the group consisting of hydrogen, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl, C-C-cycloalkyl and OR′;'}{'sup': 6', '7, 'sub': 1', '4', '2', '4', '2', '4', '1', '4', '3', '4', 'm, 'Rand Rare independently selected from the group consisting of hydrogen, X, cyano, C-C-alkyl, C-C-alkenyl, C-C-alkynyl, C-C-haloalkyl and C-C-cycloalkyl; wherein one or more carbon atoms in cycloalkyl ring may be replaced by heteroatoms selected from the group consisting of N, O, S(O)and optionally including 1 to 3 ring members selected from the group consisting of C(═O) or C(═S);'}{'sub': 3', '10', '5', '10, 'sup': '8', 'ring E is selected from the group consisting of fused or non-fused C-C-carbocyclyl and C-C-heterocyclyl, which may optionally be substituted by one or more groups of R;'}or agriculturally acceptable salts, isomers/structural isomers, stereo ...

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Номер записи: 72
07-03-2019 дата публикации

POLYETHYLENE GLYCOL DERIVATIVE AND USE THEREOF

Номер: US20190071379A1
Автор: Bae Sung Min, Kim Dae Jin, Kwon Se Chang, Lee Jong Soo
Принадлежит: HANMI PHARM. CO., LTD.

The present invention relates to polyethylene glycol derivatives and use thereof. 2. The compound claim 1 , stereoisomer thereof claim 1 , or pharmaceutically acceptable salt of claim 1 , wherein Ris ortho-pyridyl disulfide claim 1 , thiol claim 1 , or iodine.3. The compound claim 1 , stereoisomer thereof claim 1 , or pharmaceutically acceptable salt of claim 1 , wherein Ris aldehyde.4. The compound claim 1 , stereoisomer thereof claim 1 , or pharmaceutically acceptable salt of claim 1 , wherein Rand Rhave mutually different functional groups.5. The compound claim 1 , stereoisomer thereof claim 1 , or pharmaceutically acceptable salt of claim 1 , {'br': None, 'sub': 2', 'j', '2', '2', 'n', '2', 'm', '2', 'k', '2, 'CHO—(CH)—O—(CHCH)—(CH)—NH(CO)—(CH)—R\u2003\u2003[Formula 2]'}, 'wherein the compound is represented by Formula 2 belowwherein, in Formula 2 above;n is an integer of 10 to 2400;each of j, m, and k is independently an integer of 1 to 6; and{'sub': '2', 'Ris ortho-pyridyl disulfide (OPSS), thiol, or halogen.'}7. A method for preparing a physiologically active polypeptide to which a polyethylene glycol compound is attached claim 1 , comprising reacting a polyethylene glycol compound according to any one of to with a physiologically active polypeptide.8. The method of claim 7 , wherein ortho-pyridyl disulfide (OPSS) claim 7 , thiol claim 7 , or halogen located at Rreacts with a thiol group located at the cysteine residue of the physiologically active polypeptide.9. The method of claim 7 , further comprising purifying the physiologically active polypeptide to which a polyethylene glycol compound is attached.10. The method of claim 7 , wherein the physiologically active polypeptide is selected from the group consisting of hormones claim 7 , cytokines claim 7 , enzymes claim 7 , antibodies claim 7 , growth factors claim 7 , transcription factors claim 7 , blood factors claim 7 , vaccines claim 7 , insulinotropic peptides claim 7 , neuropeptides claim 7 , pituitary ...

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Номер записи: 73
18-03-2021 дата публикации

ALKOXY COMPOUNDS FOR DISEASE TREATMENT

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

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

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Номер записи: 74
19-03-2015 дата публикации

6,7-Dihydro-5H-benzo[7]annulene derivatives, processes for their preparation, pharmaceutical products comprising them and their use for preparing medicaments

Номер: US20150080438A1
Автор: BOHLMANN Rolf, Bothe Ulrich, Moeller Carsten, Nubbemeyer Reinhard, Ter Laak Antonius, Wintermantel Tim, Wortmann Lars, Zorn Ludwig
Принадлежит: Bayer Intellectual Property GmbH

The invention relates to selective oestrogen receptor modulators (SERMs) and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception. 5. Compounds according to having the names9-[5-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphanyl]propyl}amino)pentyl]-8-phenyl-6,7-dihydro-5H-benzo[7]annulen-3-ol9-[5-(methyl{3-[(RS)-(4,4,5,5,5-pentafluoropentyl)sulphinyl]propyl}amino)pentyl]-8-phenyl-6,7-dihydro-5H-benzo[7]annulen-3-ol9-[5-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]propyl}amino)pentyl]-8-phenyl-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{3-[(RS)-(4,4,5,5,5-pentafluoropentyl)sulphinyl]propyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{3-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]propyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{4-[(RS)-(4,4,5,5,5-pentafluoropentyl)sulphinyl]butyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{4-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]butyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{5-[(RS)-(4,4,5,5,5-pentafluoropentyl)sulphinyl]pentyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{5-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]pentyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{6-[(RS)-(4,4,5,5,5-pentafluoropentyl)sulphinyl]hexyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[5-(methyl{6-[(4,4,5,5,5-pentafluoropentyl)sulphonyl]hexyl}amino)pentyl]-6,7-dihydro-5H-benzo[7]annulen-3-ol8-(3-hydroxyphenyl)-9-[6-(methyl{3-[(RS)-(4,4,5,5,5-pentafluoropentyl)sulphinyl]propyl}amino)hexyl]-6,7- ...

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Номер записи: 75
19-03-2015 дата публикации

METHODS FOR REDUCING TRIGLYCERIDE, TOTAL CHOLESTEROL AND LOW DENSITY LIPOPROTEIN BLOOD LEVELS

Номер: US20150080471A1
Автор: MATSUDA Kazuko
Принадлежит: MediciNova, Inc.

A compound of Formula (I): 4. The method of claim 1 , in which the subject is diagnosed with hypertriglyceridemia.5. The method of claim 1 , in which the compound is administered orally.6. The method of claim 1 , in which the compound is administered once daily claim 1 , twice daily claim 1 , or thrice daily.7. The method of claim 1 , in which the compound is administered as a liquid or solid dosage form.8. The method of claim 2 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form.9. The method of claim 1 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 1 ,000 mg/day claim 1 , optionally divided into one claim 1 , two claim 1 , or three portions.10. The method of claim 1 , in which the compound is administered at a dosage of 50 mg claim 1 , 75 mg claim 1 , 100 mg claim 1 , 200 mg claim 1 , 500 mg claim 1 , 750 mg claim 1 , or 1 claim 1 ,000 mg once a day claim 1 , twice a day claim 1 , or three times a day.14. The method of claim 11 , in which the subject is diagnosed with hypercholesterolemia.15. The method of claim 11 , in which the compound is administered orally.16. The method of claim 11 , in which the compound is administered once daily claim 11 , twice daily claim 11 , or thrice daily.17. The method of claim 11 , in which the compound is administered as a liquid or solid dosage form.18. The method of claim 12 , in which the compound is administered orally in a solid dosage form and is present in an orthorhombic crystalline form.19. The method of claim 11 , in which the compound is administered in an amount ranging from 50 mg/day to 5 claim 11 ,000 mg/day claim 11 , optionally divided into one claim 11 , two claim 11 , or three portions.20. The method of claim 11 , in which the compound is administered at a dosage of 50 mg claim 11 , 75 mg claim 11 , 100 mg claim 11 , 200 mg claim 11 , 500 mg claim 11 , 750 mg claim 11 , or 1 claim 11 ,000 mg once a day ...

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Номер записи: 76
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: 77
26-03-2015 дата публикации

ALKYL PHENYL SULFIDE DERIVATIVE AND PEST CONTROL AGENT

Номер: US20150087833A1
Автор: Bessho Junichiro, Domon Kei, Ito Seisuke, Kawamoto Kei, Komatsu Masaaki, Matsuda Takeshi, Ogawa Yutaka, Toriyabe Keiji, Watanabe Akira
Принадлежит:

An alkyl phenyl sulfide derivative represented by the general formula [I] or an agriculturally acceptable salt thereof, and a pest control agent containing the derivative or the salt as an active ingredient. 19-. (canceled)11. An alkyl phenyl sulfide derivative or an agriculturally acceptable salt thereof ,{'claim-ref': {'@idref': 'CLM-00010', 'claim 10'}, 'sup': '1', 'according to , wherein Rin the general formula [I] is a 2,2-difluoroethyl group, a 2,2,2-trifluoroethyl group, a 3,3,3-trifluoropropyl group, a pentafluoroethyl group, 1,2,2,2-tetrafluoroethyl group, 2-chloro-2,2-difluoroethyl group, a 2,2,3,3-tetrafluoropropyl group, a 2,2,3,3,3-pentafluoropropyl group, a 3,3-dichloroallyl group, a propargyl group, a cyclopropylmethyl group or a (2,2-difluorocyclopropyl)methyl group.'}12. An alkyl phenyl sulfide derivative or an agriculturally acceptable salt thereof claim 10 , according to claim 10 , wherein Rin the general formula [I] is a halogen atom claim 10 , a C˜Calkyl group claim 10 , a C˜Chaloalkyl group or a cyano group.13. An alkyl phenyl sulfide derivative or an agriculturally acceptable salt thereof claim 10 , according to claim 10 , wherein Rin the general formula [I] is a hydrogen atom claim 10 , a halogen atom or a C˜Calkyl group.14. A pest control agent which contains claim 10 , as an active ingredient claim 10 , an alkyl phenyl sulfide derivative or an agriculturally acceptable salt thereof claim 10 , according to .16. An alkyl phenyl sulfide derivative or an agriculturally acceptable salt thereof claim 15 , according to claim 15 , wherein R in the general formula [I′] is a 2 claim 15 ,2-difluoroethyl group claim 15 , a 2 claim 15 ,2 claim 15 ,2-trifluoroethyl group claim 15 , a 3 claim 15 ,3 claim 15 ,3-trifluoropropyl group claim 15 , a pentafluoroethyl group claim 15 , a 1 claim 15 ,2 claim 15 ,2 claim 15 ,2-tetrafluoroethyl group claim 15 , a 2-chloro-2 claim 15 ,2-difluoroethyl group claim 15 , a 2 claim 15 ,2 claim 15 ,3 claim 15 ,3- ...

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Номер записи: 78
31-03-2022 дата публикации

Thermally stable polythiol ligands with pendant solubilizing moieties

Номер: US20220098475A1
Автор: Austin Smith, David Olmeijer, Ravisubhash Tangirala
Принадлежит: Nanosys Inc

The present invention provides nanostructure compositions and methods of producing nanostructure compositions. The nanostructure compositions comprise a population of nanostructures comprising polythiol ligands with pendant moieties. The polythiol ligand with pendant moieties increase the solubility of the nanostructures in solvents and resins. The present invention also provides nanostructure films comprising the nanostructure compositions and methods of making nanostructure films using the nanostructure compositions.

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Номер записи: 79
25-03-2021 дата публикации

NOVEL CURCUMINOID-INSPIRED SYNTHETIC COMPOUNDS AS ANTI-TUMOR AGENTS

Номер: US20210087208A1
Автор: Laali Kenneth K.
Принадлежит: UNIVERSITY OF NORTH FLORIDA BOARD OF TRUSTEES

Novel CUR- and CUR-BFcompounds as well as novel bis and mono-NSAID/CUR-BFand NSAID/CUR hybrids exhibiting anti-tumor properties are presented. CUR compounds bearing fluorinated moieties with selective fluorine introduction into the α-carbonyl moiety as well as CUR-BFadducts and CURs with diverse substitution patterns in the phenyl rings including fluorinated substituents (SCF, OCF, and F) and/or bulky activating groups (OMe, OAc, and OBz) are presented. Fluorinated aryl-pyrazoles and isoxazoles as well as novel CUR and CUR-BFcompounds with monocyclic aromatic and bicyclic-heteroaromatic lateral rings, bearing fluorine(s), OCF, CF, and SCFgroups, and their alpha-carbonyl-fluorinated analogs, as well as their pyrazole and isoxazole derivatives are presented. The CUR-pyrazoles embody analogs that are fluorinated at the phenyl-pyrazole moiety. The hybrids, compounds, and their derivatives exhibited exceptional cytotoxic and anti-proliferative activity against several cancer cell-lines. The hybrid NSAID/CUR compounds also exhibited exceptional anti-inflammatory activity over NSAID or curcumin alone. 2. The composition of claim 1 , wherein Ris O associated with a difluoroboron adduct.3. The composition of claim 2 , wherein Ris O associated with a difluoroboron adduct.5. The method of claim 4 , wherein Ris O associated with a difluoroboron adduct.6. The method of claim 5 , wherein Ris O associated with a difluoroboron adduct.7. The method of claim 6 , wherein Ris p-OH.8. The method of claim 7 , wherein the at least one cancer cell is a colorectal cancer cell.10. The composition of claim 9 , further comprising at least one deuterated substituent on the aryl.11. The composition of claim 10 , wherein the at least one deuterated substitution is a plurality of deuterated substitutions.12. The composition of claim 11 , wherein the plurality of deuterated substitutions is at the meta positions. This application is a continuation in part of and claims priority to currently pending ...

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Номер записи: 80
31-03-2016 дата публикации

Derivatisation of biological molecules

Номер: US20160089445A1
Автор: Andrew Lennard Lewis, Antony Robert Godwin, Stephen James Brocchini, Yiqing Tang
Принадлежит: BIOCOMPATIBLES UK LTD

The present disclosure relates to a new polymerisation process in which ethylenically unsaturated monomers are polymerised by a living radical polymerisation process in the presence of an initiator and a catalyst. Polymers produced by this new process are also thought to be novel and may be used to derivatise biological molecules to improve their efficacy as therapeutic treatments. A preferred polymer is of formula The polymers are particularly suitable for derivatising proteins, such as interferon-α.

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Номер записи: 81
21-03-2019 дата публикации

4-sulfur pentafluoride phenol compound and preparation method therefor, and preparation method for sulfur pentafluoride substituted benzopyran compound

Номер: US20190084957A1
Автор: Chuang He, Jiantong GUAN, John J. Talley, Mickey D. TORTORELLA, Yanmei Zhang, Yican Wang, Yongjie LIN
Принадлежит: Guangzhou Institute of Biomedicine and Health of CAS

Provided are a 4-sulfur pentafluoride phenol compound and a preparation method therefor, and a preparation method for a sulfur pentafluoride substituted benzopyran compound. According to the present invention, sulfur pentafluoride salicylaldehyde with multiple substituent groups is synthesized through a plurality of steps by using sulfur pentafluoride phenol as a raw material, and then the sulfur pentafluoride substituted benzopyran compound is synthesized on this basis. The method is simple and convenient, and low in cost; overcomes the defects that, at present, the number of types of sulfur pentafluoride phenols is small, and the synthesis of various sulfur pentafluoride substituted benzopyran compounds cannot be met; and has wide industrial application prospects.

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Номер записи: 82
30-03-2017 дата публикации

Fluorine-Containing Polymerizable Monomer and Polymer Compound Using Same

Номер: US20170088666A1
Автор: Junya Nakatsuji, Kazuhiro Yamanaka, Makoto Matsuura
Принадлежит: Central Glass Co Ltd

Disclosed in the present invention are a fluorine-containing polymerizable compound of the general formula (1) and a polymer compound obtained therefrom: where A represents a single bond, an oxygen atom, a sulfur atom, SO 2 , CH 2 , CO, C(CH 3 ) 2 , C(CH 3 )(CH 2 CH 3 ), C(CF 3 ) 2 , C(CH 3 )(C 6 H 5 ), CH 2 —C 6 H 4 —CH 2 or a divalent organic group obtained by elimination of two hydrogen atoms from benzene, biphenyl, naphtharene, cyclohexene or fluorene; and a and b each independently represent an integer of 0 to 2 and satisfy a relationship of 1≦a+b≦4. The thus-obtained polymer compound combines adequate hydrophilicity and high transparency with low water adsorption of fluorine-containing compound.

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Номер записи: 83
05-05-2022 дата публикации

SUBSTITUTED AMINO-THIOL AND AMINO-DISULFIDE COMPOUNDS, AND USES THEREOF

Номер: US20220135524A1
Автор: Ballatore Carlo, Dohil Ranjan
Принадлежит:

The disclosure provides for new substituted cysteamine and cystamine compounds, pharmaceutical compositions made thereof, and methods thereof including the treatment of any disease or disorder in a subject that can benefit from one or more of the bioprotective effects of the compounds, including but not limited to, binding of cystine, reducing oxidative stress, increasing adiponectin levels and/or increasing brain-derived neurotrophic factors. Examples of such disease and disorders, include but are not limited to, cystinosis, and fatty liver diseases.

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Номер записи: 84
19-06-2014 дата публикации

2-MERCAPTO-5-METHYL-4-HEPTANONE AND ITS USE IN FLAVOR AND FRAGRANCE COMPOSITIONS

Номер: US20140171517A1
Автор: AGYEMANG David O., Bardsley Kathryn A., Chen Zhen, JANCZUK Adam Jan, Trinnaman Laurence
Принадлежит: International Flavors & Fragrances Inc.

The present invention is directed to a novel compound, 2-mercapto-5-methyl-4-heptanone, a process of augmenting, enhancing or imparting taste to a material selected from the group consisting of a foodstuff, a chewing gum, a medicinal product, and toothpaste comprising the step of incorporating an olfactory acceptable amount of 2-mercapto-5-methyl-4-heptanone, and a process of improving, enhancing or modifying a fragrance formulation through the addition of an olfactory acceptable amount of 2-mercapto-5-methyl-4-heptanone. 1. A compound , 2-mercapto-5-methyl-4-heptanone.2. A composition comprising an olfactory effective amount of 2-mercapto-5-methyl-4-heptanone.3. The composition of further comprising a material selected from the group consisting of foodstuff claim 2 , a chewing gum claim 2 , a dental or oral hygiene product claim 2 , and a medicinal product.4. The composition of claim 2 , wherein the olfactory effective amount is greater than about 0.5 parts per billion by weight.5. The composition of claim 2 , wherein the olfactory effective amount is from about 1 part per billion to about 1 part per million by weight.6. The composition of claim 2 , wherein the olfactory effective amount is from about 5 parts per billion to about 500 parts per billion by weight.7. A process of augmenting claim 2 , enhancing or imparting a taste to a material selected from the group consisting of foodstuff claim 2 , a chewing gum claim 2 , a dental or oral hygiene product claim 2 , and a medicinal product comprising the step of incorporating a composition comprising an olfactory effective amount of 2-mercapto-5-methyl-4-heptanone.8. The process of claim 7 , wherein the olfactory effective amount is greater than about 0.5 parts per billion by weight.9. The process of claim 7 , wherein the olfactory effective amount is from about 1 part per billion to about 1 part per million by weight.10. The process of claim 7 , wherein the olfactory effective amount is from about 5 parts per ...

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Номер записи: 85
19-03-2020 дата публикации

Polymerizable compound and liquid crystal composition

Номер: US20200087240A1
Автор: Ayaki Hosono, Masanao Hayashi
Принадлежит: DIC Corp

A compound represented by formula (i) has, as Ki1 in the formula (i), a structure represented by any one of formula (K-1) to formula (K-3). When used in a liquid crystal composition, it adheres to substrates which hold the liquid crystal composition (liquid crystal layer) therebetween, thereby permitting liquid crystal molecules to be maintained in the state of being aligned in the vertical direction. The liquid crystal composition using the compound enables liquid crystal molecules to be aligned even when the PI layer is not provided (vertical alignment of liquid crystal molecules is induced without the voltage applied and horizontal alignment of liquid crystal molecules is realized with the voltage applied). It is possible to provide a polymerizable compound being excellent in storability and capable of uniform vertical alignment of liquid crystal molecules with no PI layer provided.

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Номер записи: 86
05-04-2018 дата публикации

NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS

Номер: US20180092971A1
Автор: Ansell Steven, CHEN Jianxin, Eltepu Laxman, Jayaraman Muthusamy, Manoharan Muthiah, Rajeev Kallanthottathil G.
Принадлежит: Arbutus Biopharma Corporation

The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention 125-. (canceled)27. The lipid of claim 26 , wherein Ris ω-aminoalkyl claim 26 , ω-(substituted)aminoalkyl claim 26 , ω-phosphoalkyl claim 26 , or ω-thiophosphoalkyl.28. The lipid of claim 27 , wherein Ris ω-(substituted)aminoalkyl.29. The lipid of claim 26 , wherein Ris 2-(dimethylamino)ethyl claim 26 , 3-(diisopropylamino)propyl claim 26 , or 3-(N-ethyl-n-isopropylamino)-1-methylpropyl.30. The lipid of claim 26 , wherein Ris H claim 26 , optionally substituted C-Calkyl claim 26 , optionally substituted C-Calkenyl claim 26 , or optionally substituted C-Calkynyl.31. The lipid of claim 26 , wherein Ris alkylaminoalkyl claim 26 , dialkylaminoalkyl claim 26 , or alkylheterocycle.32. The lipid of claim 26 , wherein Rand Rare each optionally substituted C-Calkyl or optionally substituted C-Calkenyl.33. The lipid of claim 26 , wherein Rand Rare each linoleyl.34. A lipid particle comprising a lipid of .35. The lipid particle of claim 34 , wherein the particle further comprises a neutral lipid and a lipid capable of reducing aggregation.36. The lipid particle of claim 35 , wherein the lipid capable of reducing aggregation is a PEG-lipid.37. The lipid particle of claim 34 , further comprising a therapeutic agent.38. The lipid particle of claim 37 , wherein the therapeutic agent is a nucleic acid.39. The lipid particle of claim 38 , wherein the nucleic acid is selected from the group consisting of an siRNA and an antisense oligonucleotide.40. The lipid particle of claim 37 , wherein the nucleic acid is siRNA.41. The lipid particle of claim 37 , wherein the nucleic acid is mRNA.42. A pharmaceutical composition comprising a lipid of and a pharmaceutically acceptable excipient claim 26 , carrier claim 26 , or diluent.43. A pharmaceutical composition comprising a lipid particle of and a pharmaceutically ...

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Номер записи: 87
09-04-2015 дата публикации

Aryloxyurea compound and pest control agent

Номер: US20150099883A1
Автор: Asaho Nagagata, Daisuke Hanai, Hironori Furukawa, Jun Kanazawa, KATSUNORI Tanaka, Tetsuo Tamai
Принадлежит: Nippon Soda Co Ltd

The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R 1 represents an ethyl group or the like, R 2 represents a hydrogen atom or the like, R 3 and R 4 represents a methyl group or the like, X 1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X 2 represents a methyl group or the like, m2 is an integer of 0 to 3.

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Номер записи: 88
01-04-2021 дата публикации

LIGAND AND METHOD OF MANUFACTURING THE SAME, QUANTUM DOT FILM AND METHOD OF MANUFACTURING THE SAME, AND DISPLAY APPARATUS

Номер: US20210095194A1
Автор: MEI Wenhai
Принадлежит:

A ligand includes a molecular skeleton, a first coordinating group connected to the molecular skeleton, at least one initial group connected to the molecular skeleton, and a protecting group connected to an end of each initial group away from the molecular skeleton. Each initial group is capable of forming a second coordinating group after deprotection. 1. A ligand , comprising:a molecular skeleton;a first coordinating group connected to the molecular skeleton;at least one initial group connected to the molecular skeleton; anda protecting group connected to an end of each initial group away from the molecular skeleton; whereineach initial group is capable of forming a second coordinating group after deprotection.2. The ligand according to claim 1 , wherein for a same central atom claim 1 , a coordination capability of the second coordinating group to the central atom is stronger than a coordination capability of the first coordinating group to the central atom.3. The ligand according to claim 1 , whereinthe first coordinating group includes one of an amino group, an imino group, a carboxyl group, or a sulfhydryl group;or,the second coordinating group formed after each initial group is deprotected includes one of an amino group, an imino group, a carboxyl group, or a sulfhydryl group;or,the first coordinating group includes one of an amino group, an imino group, a carboxyl group or a sulfhydryl group, and the second coordinating group formed after each initial group is deprotected includes one of an amino group, an imino group, a carboxyl group, or a sulfhydryl group.4. The ligand according to claim 1 , wherein a decomposable bond formed between each initial group and the protecting group includes a photolytic chemical bond or a pyrolytic chemical bond; whereinthe photolytic chemical bond is capable of being broken under ultraviolet (UV) light irradiation; andthe pyrolytic chemical bond is capable of being broken by heating.5. The ligand according to claim 4 , ...

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Номер записи: 89
05-04-2018 дата публикации

POTENT AND SELECTIVE INHIBITORS OF MONOAMINE TRANSPORTERS; METHOD OF MAKING; AND USE THEREOF

Номер: US20180093947A1
Автор: Cao Jianjing, Newman Amy Hauck, Okunola-Bakare Oluyomi M.
Принадлежит:

Disclosed herein are bisarylmethylthioacetamides and bisarylmethylthioethylamines useful as inhibitors of monoamine transporters. The compounds are potent and/or selective inhibitors of dopamine (DA), serotonin (5-HT), and/or norepinephrine (NE) reuptake via their respective transporters, DAT, SERT and NET. Also disclosed are methods for eliciting a wake-promoting or cognitive or attention enhancing effect and for treating substance use disorders, attention deficit (hyperactivity) disorder, depressive disorders, bipolar disorder or other neuropsychiatric disorders sleep disorders or cognitive impairment using the compounds. 2. The method of claim 1 , wherein{'sub': 5', '2', '3', '2', '2, 'Ris 3-phenylpropyl, —CHCH(OH)CH, or —CHCH(OH)CHPh;'}{'sub': '3', 'each instance of X is located at the para or meta position and is fluoro, methyl, or CF;'}Y is S or S(O); andZ is O or 2H.3. The method of claim 1 , wherein a sulfoxide fragment has an (R)-configuration.4. The method of claim 1 , wherein a sulfoxide fragment has an (S)-configuration.5. The method of claim 1 , wherein{'sub': 5', '2', '3', '2', '2, 'Ris —CHCH(OH)CHor —CHCH(OH)CHPh wherein the carbon substituted with —OH is racemic, in the R configuration, or in the S configuration;'}{'sub': '3', 'each instance of X is located at the para or meta position and is fluoro, methyl, or CF;'}Y is S or S(O); andZ is 2H.6. The method of claim 5 , wherein a sulfoxide fragment has an (R)-configuration or an (S)-configuration.7. The method of claim 1 , wherein{'sub': 5', '2', '3', '2', '2, 'Ris —CHCH(OH)CHor —CHCH(OH)CHPh wherein the carbon substituted with —OH is racemic, in the R configuration, or in the S configuration;'}each instance of X is located at the para or meta position and is fluoro;Y is S or S(O); andZ is 2H.8. The method of claim 7 , wherein a sulfoxide fragment has an (R)-configuration or an (S)-configuration.9. The method of claim 1 , wherein the compound or salt thereof is formulated as a pharmaceutical ...

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Номер записи: 90
12-05-2022 дата публикации

COMPOUND

Номер: US20220144759A1
Автор: ASATSU Yuji, KOBASHI Ai, OZAWA Shoichi
Принадлежит: Sumitomo Chemical Company, Limited

A compound having a molecular weight of 3000 or less and a partial structure represented by Formula (X) is provided: 3. The compound according to claim 2 , wherein at least one selected from Rand Ris a nitro group claim 2 , a cyano group claim 2 , a halogen atom claim 2 , —OCF claim 2 , —SCF claim 2 , —SF claim 2 , —SF claim 2 , a fluoroalkyl group claim 2 , a fluoroaryl group claim 2 , —CO—O—R claim 2 , —SO—R claim 2 , or —CO—R(Rrepresents a hydrogen atom claim 2 , an alkyl group having 1 to 25 carbon atoms which may have a substituent claim 2 , or an aromatic hydrocarbon group having 6 to 18 carbon atoms which may have a substituent).4. The compound according to claim 2 , wherein at least one selected from Rand Ris a nitro group claim 2 , a cyano group claim 2 , a fluorine atom claim 2 , a chlorine atom claim 2 , —OCF claim 2 , —SCF claim 2 , a fluoroalkyl group claim 2 , —CO—O—R claim 2 , or —SO—R(Rrepresents a hydrogen atom claim 2 , an alkyl group having 1 to 25 carbon atoms which may have a substituent claim 2 , or an aromatic hydrocarbon group having 6 to 18 carbon atoms which may have a substituent).5. The compound according to claim 2 , wherein at least one selected from Rand Ris a cyano group claim 2 , —CO—O—R claim 2 , or —SO—R(Rrepresents a hydrogen atom claim 2 , an alkyl group having 1 to 25 carbon atoms which may have a substituent claim 2 , or an aromatic hydrocarbon group having 6 to 18 carbon atoms which may have a substituent).6. The compound according to claim 2 , wherein at least one selected from Rand Ris a cyano group.7. The compound according to claim 2 , wherein Ris a cyano group claim 2 , Ris a cyano group claim 2 , —CO—O—R claim 2 , or —SO—R(Rrepresents a hydrogen atom claim 2 , an alkyl group having 1 to 25 carbon atoms which may have a substituent claim 2 , or an aromatic hydrocarbon group having 6 to 18 carbon atoms which may have a substituent).8. The compound according to claim 2 , wherein both Rand Rare a cyano group.9. The compound ...

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Номер записи: 91
28-03-2019 дата публикации

COMPOSITION INCLUDING BENZENE DIAMINE DERIVATIVE FOR PREVENTING OR TREATING DEGENERATIVE BRAIN DISEASES

Номер: US20190092728A1
Автор: Han Ho Seong, KIM Sang Tae, Lim Mi Hee
Принадлежит:

Provided are a compound represented by the following Formula I-1 or I-2, and a composition for preventing or treating dementia or Alzheimer's disease, the composition including the compound and a pharmaceutically acceptable carrier: 5. The method of claim of claim 1 , wherein Ais —SR.7. The method of claim 6 , wherein Ris hydrogen or a halogen.8. The method of claim 6 , wherein in Formula II claim 6 , Rand Rare each hydrogen.9. The method of claim of claim 6 , wherein in Formulae III and IV claim 6 , Rand Rare each independently a substituted or unsubstituted C-Calkyl group.1114-. (canceled) This application claims the benefit of Korean Patent Application No. 10-2017-0124527, filed on Sep. 26, 2017, in the Korean Intellectual Property Office, the disclosure of which is incorporated herein in its entirety by reference.The present disclosure relates to a benzene diamine derivate, or a solvate, stereoisomer, or pharmaceutically acceptable salt thereof, and a composition for preventing or treating degenerative brain diseases including the same as an active ingredient.Degenerative brain diseases are characterized by gradual occurrence of general impairment of mental or physical functions, which is caused by temporary or sustained damage to neurons due to a variety of causes. There are more than 70 diseases reported as degenerative brain diseases. Of them, dementia, Alzheimer's disease, Parkinson's disease, and frontotemporal degeneration are known as representative degenerative brain diseases.Among these, dementia is one of the diseases with high prevalence, and results from dysfunction of the cerebral cortex, in terms of memory, attention, language, and visual-spatial functioning, and thus patients with dementia suffer from many difficulties in their daily or social lives.The etiology of dementia has not yet been fully clarified, but Alzheimer's disease (AD) caused by cerebral deposition and aggregation of β-amyloid (Aβ) protein with aging, vascular dementia caused by ...

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Номер записи: 92
14-04-2016 дата публикации

Use of Cysteamine in Treating Infections caused by Yeasts/Moulds

Номер: US20160102052A1
Автор: "ONEIL Deborah", DUNCAN Vanessa
Принадлежит: NOVABIOTICS LIMITED

The present invention relates to compositions comprising cysteamine or a derivative thereof for use in treating infections caused by yeasts or moulds. 1. A composition comprising cysteamine or a derivative thereof for use in the treatment or prevention of an infection caused by yeasts and/or moulds.2CandidaC. albicansAspergillusEpidermophytonExophialaMicrosporumTrichophytonT. rubrumT. interdigitaleTineaBlastomycesBlastoschizomycesCoccidioidesCryptococcusCryptococcus neoformansHistoplasmaParacoccidiomycesSporotrixAbsidiaCladophialophoraFonsecaeaPhialophoraLacaziaArthrographisAcremoniumActinomaduraApophysomycesEmmonsiaBasidiobolusBeauveriaChrysosporiumConidiobolusCunninghamellaFusariumGeotrichumGraphiumLeptosphaeriaMalasseziaMalassezia furfurMucorNeotestudinaNocardiaNocardiopsisPaecilomycesPhomaPiedraiaPneumocystisPseudallescheriaPyrenochaetaRhizomucorRhizopusRhodotorulaSaccharomycesScedosporiumScopulariopsisSporobolomycesSyncephalastrumTrichodermaTrichosporonUlocladiumUstilagoVerticilliumWangiella. A composition according to wherein the infection is caused by one or more of the group consisting of: spp. claim 1 , (e.g. ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , (e.g and ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. (e.g. ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. (e.g ) claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. claim 1 , spp. c ...

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Номер записи: 93
08-04-2021 дата публикации

Process for the preparation of elafibranor and novel synthesis intermediates

Номер: US20210101866A1
Автор: Ilaria FERRANDO, Jiri Stohandl, Petr SEBESTA
Принадлежит: Advitech Advisory And Technologies Sa

The present invention relates to a process for the preparation of elafibranor and novel synthesis intermediates.

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Номер записи: 94
13-04-2017 дата публикации

IONIZABLE CATIONIC LIPID FOR RNA DELIVERY

Номер: US20170101370A1
Автор: Chivukula Padmanabh, Payne Joseph E.
Принадлежит:

What is described is a compound of formula I 2. The compound of claim 1 , wherein X is —CO—O—.3. The compound of claim 1 , wherein X is —O—CO—.4. The compound of claim 1 , wherein Y is S.5. The compound of claim 1 , wherein Y is O.6. The compound of claim 1 , wherein n is 1.7. The compound of claim 1 , wherein R is an alkenyl.8. The compound of claim 1 , wherein L is an alkylene.9. The compound of claim 1 , wherein L is an alkenylene.10. The compound of claim 1 , wherein L and R together have 14 to 20 carbons.11. The compound of claim 1 , wherein L and R together have 16 carbons.12. The compound of claim 1 , wherein Ris a C2 or a C3.13. The compound of claim 1 , wherein Rand Rtogether have 2 to 4 carbons.15. A composition of the compound of claim 1 , further comprising a lipid particle.16. A composition of the compound of claim 1 , further comprising an RNA claim 1 , wherein the RNA is encapsulated.17. A composition of the compound of claim 1 , further comprising a lipid conjugate.18. A composition of the compound of claim 1 , further comprising a non-cationic lipid. This application a divisional of U.S. patent application Ser. No. 14/707,796, filed May 8, 2015, which is a continuation-in-part and claims benefit under 35 U.S.C. §120 to U.S. patent application Ser. No. 14/546,105 filed on Nov. 18, 2014, which claims benefit under 35 U.S.C. §119(e) of Provisional U.S. Patent Application No. 61/905,724, filed Nov. 18, 2013, the contents of which are incorporated herein by reference in its entirety.The description of U.S. patent application Ser. No. 14/707,876, entitled “IONIZABLE CATIONIC LIPID FOR RNA DELIVERY,” filed May 8, 2015, now U.S. Pat. No. 9,365,610, issued Jun. 14, 2016, is hereby incorporated by reference in its entirety.A number of different types of nucleic acids are currently being developed as therapeutics for the treatment of a number of diseases. These nucleic acids include DNA in gene therapy, plasmids-based interfering nucleic acids, small ...

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Номер записи: 95
11-04-2019 дата публикации

CONTACT-KILLING, QAC FUNCTIONALIZED THERMOPLASTIC POLYURETHANE FOR CATHETER APPLICATIONS

Номер: US20190106525A1
Автор: BECKER Matthew L., CERCHIARI Alec, Chambers Sean, McROY Will, ZANDER Zachary K.
Принадлежит:

In various embodiments, the present invention provides a functionalized thermoplastic polyurethane (TPU) containing bulk incorporated or surface-grafted quaternary ammonium compounds (QAC)s for contact-killing of a variety of microbes, where the QACs are on the surface of TPU to provide a sterile surface material that prevents bacteria commonly involved in device-associated infections (DAIs) from proliferating. The functionalized TPUs of the present invention can be formed into a wide variety of 3-dimensional shapes, such as catheters, medical tubing, laryngeal or tracheal stents, sutures, prosthetics, wound dressings, and/or a coating for medical devices and contains the residue of either a QAC containing diol monomer or an alkene functional diol monomer, which then allows the TPU to be functionalized with a QAC containing disulfide or free thiol compound, to form a quaternary ammonium functionalized thermoplastic polyurethane compound having antimicrobial properties for use in medical devices. 1) A quaternary ammonium functionalized thermoplastic polyurethane compound having antimicrobial properties for use in medical devices comprising:a polyurethane polymer backbone;a plurality of side chains, said side chains extending from said polyurethane polymer backbone and comprising a quaternary ammonium functional group.2) The quaternary ammonium functionalized thermoplastic polyurethane compound of wherein:said polyurethane polymer backbone comprises the residues of one or more diisocyanates, one or more soft segment diols, one or more functionalized diols, and one or more diol chain extenders; andsaid plurality of side chains comprise a quaternary ammonium functional group connected to said polyurethane polymer backbone through said one or more functionalized diols.3) The quaternary ammonium functionalized thermoplastic polyurethane compound of wherein the residues of one or more functionalized diols comprises from 0.5 to 50 mole percent of said polyurethane polymer ...

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Номер записи: 96
28-04-2016 дата публикации

COMPOUND, ACTIVE LIGHT SENSITIVE OR RADIATION SENSITIVE RESIN COMPOSITION, RESIST FILM USING SAME, RESIST-COATED MASK BLANK, PHOTOMASK, PATTERN FORMING METHOD, METHOD FOR MANUFACTURING ELECTRONIC DEVICE, AND ELECTRONIC DEVICE

Номер: US20160116840A1
Автор: Tsuchimura Tomotaka
Принадлежит: FUJIFILM Corporation

Provided is an active light sensitive or radiation sensitive resin composition which contains a compound (A) represented by General Formula (I) or (II): 2. The active light sensitive or radiation sensitive resin composition according to claim 1 ,{'sub': 1', '2, 'sup': '1', 'wherein, in General Formula (I) or (II), Xor Xis a group which is represented by —NH— or —NR—.'}3. The active light sensitive or radiation sensitive resin composition according to claim 1 ,{'sub': 2', '2, 'wherein, in General Formula (I) or (II), Xor Xis a group which is represented by —S—.'}4. The active light sensitive or radiation sensitive resin composition according to claim 1 ,{'sub': 1', '2, 'wherein, in General Formula (I) or (II), Yor Yis an aryl group or a monovalent hydrocarbon group which has an alicyclic hydrocarbon structure having 5 or more carbon atoms.'}5. The active light sensitive or radiation sensitive resin composition according to claim 1 , further comprising:a compound (B) which has a phenolic hydroxyl group.8. The active light sensitive or radiation sensitive resin composition according to claim 1 , further comprising:an acid cross-linkable compound (C).9. The active light sensitive or radiation sensitive resin composition according to claim 8 ,wherein the compound (C) is a compound which has two or more hydroxymethyl groups or alkoxymethyl groups in a molecule.10. The active light sensitive or radiation sensitive resin composition according to claim 1 , which is used for exposure to electron beams or extreme ultraviolet light.11. A resist film formed using the active light sensitive or radiation sensitive resin composition according to .12. A resist-coated mask blank coated with the resist film according to .13. A photomask obtained by exposing and developing the resist-coated mask blank according to .14. A pattern forming method comprising:{'claim-ref': {'@idref': 'CLM-00011', 'claim 11'}, 'exposing the resist film according to ; and'}developing the exposed film.15. A ...

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Номер записи: 97
30-04-2015 дата публикации

BIODEGRADABLE COMPUTED TOMOGRAPHY CONTRAST AGENTS

Номер: US20150119706A1
Автор: Jin Erlei, Lu Zheng-Rong, Wu XiaoHui
Принадлежит:

Biodegradable computed tomography (CT) contrast agents comprising a polyiodinated aryl contrast agent that is crosslinked by an organic disulfide are described herein. The contrast agents can be used to image a tissue region by administering an effective amount of the biodegradable CT contrast agent to a subject, allowing a sufficient amount of time for the biodegradable CT contrast agent to enter the tissue region, and performing x-ray computed tomography imaging of the tissue region of the subject. 1. A biodegradable macromolecular computed tomography (CT) contrast agent comprising a polyiodinated aryl contrast agent crosslinked by an organic disulfide.4. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the polyiodinated aryl contrast agent is PEGylated.5. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the polyiodinated aryl contrast agent is 5-amino-2 claim 1 ,4 claim 1 ,6-triiodoisophthalic acid (ATIPA).6. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the organic disulfide is cystamine.8. The biodegradable macromolecular CT contrast agent of claim 1 , wherein the organic disulfide is cystine.10. A method for imaging a tissue region of a subject comprising:(a) administering an effective amount of a biodegradable macromolecular computed tomography (CT) contrast agent comprising a polyiodinated aryl contrast agent that is crosslinked by an organic disulfide to the subject;(b) allowing a sufficient amount of time for the macromolecular biodegradable CT contrast agent to enter the tissue region; and(c) performing x-ray computed tomography imaging of the tissue region of the subject.13. The method of claim 10 , wherein the polyiodinated aryl contrast agent is 5-amino-2 claim 10 ,4 claim 10 ,6-triiodoisophthalic acid (ATIPA).16. The method of claim 10 , wherein the tissue region is a blood vessel.17. The method of claim 10 , wherein the tissue region is a tumor.18. A method of making a ...

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Номер записи: 98
09-06-2022 дата публикации

CARBON QUANTUM DOT, A COMPOSITION THEREOF AND A METHOD FOR TREATING INFECTION BY USING SAME

Номер: US20220177412A1
Автор: CHEN Yuju, Huang ChihChing, Kuo WanChing, Lai PeiXin, Lin HanJia, Lin HanYou, Shen Fan
Принадлежит:

Provided is a carbon quantum dot having a graphite core and a surface including components, such as compounds derived from formula (I) and halogens, and having a positive charge for antibacterial purposes. Also provided are methods for preparing a carbon quantum dot and a composition containing the same. 2. The carbon quantum dot according to claim 1 , wherein Rin the compound of formula (I) is selected from the group consisting of C-Calkyl claim 1 , Calkylamine claim 1 , Calkyl polyamine claim 1 , 2-pentanol group and sulfide group.3. The carbon quantum dot according to claim 1 , wherein the halogen is derived from a chlorine compound claim 1 , a bromine compound claim 1 , or an iodine compound.4. The carbon quantum dot according to claim 3 , wherein the chlorine compound is hydrogen chloride claim 3 , ammonium chloride claim 3 , hypochlorous acid claim 3 , potassium chloride claim 3 , or sodium chloride.5. The carbon quantum dot according to claim 3 , wherein the bromine compound is hydrogen bromide or potassium bromide.6. The carbon quantum dot according to claim 3 , wherein the iodine compound is hydrogen iodide or potassium iodide.812.-. (canceled)13. The method according to claim 7 , wherein the temperature is between 150° C. and 300° C.14. The method according to claim 13 , wherein the temperature is between 150° C. and 180° C. claim 13 , between 180° C. and 210° C. claim 13 , between 210° C. and 240° C. claim 13 , between 240° C. and 270° C. claim 13 , or between 270° C. and 300° C.15. An antibacterial composition comprising the carbon quantum dot according to and a pharmaceutically acceptable carrier thereof.1621.-. (canceled)22. The antibacterial composition according to claim 15 , wherein the halogen has a weight percentage of between 15% and 40% in the antibacterial composition.2334.-. (canceled)35. The antibacterial composition according to claim 15 , wherein the carbon quantum dot has a diameter of from 1 nm to 8 nm.36. The antibacterial composition ...

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Номер записи: 99
27-04-2017 дата публикации

TETRADENTATE ORGANIC LIGAND H3-MN-16Bn CONTAINING LONG ALKYL GROUP, PRECURSOR THEREOF, AND METHOD FOR PREPARING THE SAME

Номер: US20170114009A1
Автор: Chang Yu, HSU CHENG-FANG, LU Kuei-Lin, TSAI JIA-DONG
Принадлежит:

A tetradentate organic ligand H-MN-16Bn containing a long alkyl group, a precursor thereof, and a method for preparing the same are revealed. A precursor of H-MN-16Bn, benzyl 16-bromohexadecanate, is obtained by esterification reaction of 16-bromohexadecanoic acid. Then bimolecular nucleophilic substitution reaction (S2) of Benzyl 16-bromohexadecanate with nitrogen sulfide (NS) is carried out to get H-MN-16Bn that is used as a standard hydrolysis metabolites of non-radioactive Re-complex compound. 2. A method for preparing a tetradentate organic ligand H-MN-16Bn containing a long alkyl group comprising the steps of:dissolving 16-bromohexadecanoic acid and thionyl chloride in a first solvent to get a first solution;heating the first solution under reflux;cooling the first solution, and concentrating the first solution by removing excess thionyl chloride and excess first solution to form a second solution;adding phenylmethanol into the second solution to form benzyl 16-bromohexadecanate in a solid form;{'sub': 2', '2, 'mixing the benzyl 16-bromohexadecanate, nitrogen sulfide (NS), a dehydrogenating agent, a molecular sieve and a second solvent to form a third solution;'}heating the third solution under reflux; and{'sub': '3', 'filtering the third solution to get a crude product and then purifying the crude product to get the tetradentate organic ligand H-MN-16Bn containing a long alkyl group.'}3. The method as claimed in claim 2 , wherein the first solvent is hexane.4. The method as claimed in claim 2 , wherein the second solvent is acetonitrile.5. The method as claimed in claim 2 , wherein the first solution is heated under reflux at 75˜85° C. for 2 hours in the step of heating the first solution under reflux.6. The method as claimed in claim 2 , wherein the first third solution is heated under reflux at 80˜90° C. for 48 hours in the step of heating the third solution under reflux.7. The method as claimed in claim 2 , wherein the dehydrogenating agent is potassium ...

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Номер записи: 100