Настройки

Укажите год
-

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 2166. Отображено 200.
10-11-2003 дата публикации

ПРОИЗВОДНЫЕ АМИНОМАСЛЯНОЙ, АМИНОПЕНТАНОВОЙ И АМИНОГЕКСАНОВОЙ КИСЛОТ

Номер: RU2215735C2

Изобретение относится к производным аминомасляной, аминопентановой и аминогексановой кислот общей формулы I где R1 - -COOR10; - (CH2)m-CONHOR10, -CONHNHR10, -(CH2)nSR50 или -Y-P (OR51)2; m = 0, 1, 2; n = 0-3; каждый из R2, R3, R4, R5, R6 и R7 независимо является водородом, С1-8 алкилом, С2-8 алкенилом, -OR11, -SR11, -NR12R13, Циклом 1, С1-8 алкилом, замещенным -OR11, -SR11, -NR12R13, -COR14, гуанидино или Циклом 1, или С2-8 алкенилом, замещенным -OR11, -SR11, -NR12R13, -COR14, гуанидино или Циклом 1, или R3 и R4, взятые вместе, представляют С1-8 алкилен, R5 и R6, взятые вместе, представляют С1-8 алкилен, R3 и R6, взятые вместе, представляют С1-8 алкилен, R2 и R3, взятые вместе, представляют С2-8 алкилен, R4 и R5, взятые вместе, представляют С2-8 алкилен или R6 и R7, взятые вместе, представляют С2-8 алкилен, или (1) R8 представляет собой 1) водород, 2) С1-8 алкил, 3) С1-8 алкоксикарбонил, 4) С1-8 алкил, замещенный -OR26, -SR26, -NR27R28 или -COR29, или 5) С1-8 алкоксикарбонил, замещенный ...

Подробнее
10-02-2014 дата публикации

СПОСОБ ПОЛУЧЕНИЯ АКТИВИРОВАННЫХ СЛОЖНЫХ ЭФИРОВ

Номер: RU2506258C2
Принадлежит: САНОФИ (FR)

Изобретение относится к способу получения активированного сложного эфира формулы (I):где R означает C-Cалкил, линейный или разветвленный, 6-членный гетероарил с одним атомом азота в качестве гетероатома; Alk означает C-Cалкил, линейный или разветвленный, заключающийся во взаимодействии соли дициклогексиламина Pи дисукцинимидилкарбоната (ДСК) (DSC) в растворителе, который представляет собой кетон, и в котором соль дициклогексиламина и N-гидроксисукцинимида Рвыпадает в осадок. Способ обеспечивает получение целевого продукта с хорошим выходом и хорошей степенью чистоты. 2 н. и 8 з.п. ф-лы, 1 ил., 2 пр.

Подробнее
10-08-2010 дата публикации

N-ЗАМЕЩЕННЫЕ ИМИДЫ КАК ИНИЦИАТОРЫ ПОЛИМЕРИЗАЦИИ

Номер: RU2396256C2

Изобретение относится к новым N-замещенным имидам формул I и II ! и ! где n означает 1; m означает 1; R1 и R2, R4 и R5 совместно со смежной группой -CO-N-CO- образуют 5- или 6-членное моноциклическое кольцо, необязательно насыщенное и возможно замещенное С1-18алкилом, конденсированную кольцевую систему, которая в дополнение к моноциклическому сердцевинному кольцу, определенному выше, содержит одно или два С6ароматических или С6алифатических кольца; R3 означает NR12R13, где R12 и R13 независимо друг от друга означают С1-18алкил, C5-12циклоалкил, каждый из которых может быть замещен С1-4алкилом; R6 означает С6-10арил, C1-18алкил, С6-10ар-С1-С18алкил, С5-С12циклоалкил, каждый из которых необязательно замещен С1-С4алкилом; R7 означает C1-С18алкил, С6-С10арил, С6-С10ар-С1-С18алкил, С5-С12циклоалкил, каждый из которых необязательно замещен С1-С4алкилом, которые используют в качестве инициаторов радикальной термической полимеризации (ТРИ) в отвердителе для покрытий, отверждаемых свободнорадикальной ...

Подробнее
20-04-2006 дата публикации

ПРОИЗВОДНЫЕ 2-ФЕНОКСИ И 2-ФЕНИЛСУЛЬФОНАМИДА С ССR3 АНТАГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ДЛЯ ЛЕЧЕНИЯ АСТМЫ И ДРУГИХ ВОСПАЛИТЕЛЬНЫХ ИЛИ ИММУНОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ

Номер: RU2005132616A
Принадлежит:

... 1. Производное бензолсульфонамида, имеющее формулу (I), его таутомерные и стереоизомерные формы и его соли где Х представляет О или S; R1 представляет водород, галоген, гидрокси, нитро, циано, С1-6алкоксикарбонил, амино, С1-6алкиламино, ди(С1-6алкил)амино, С1-6алканоил, фенил, С1-6алкил, необязательно замещенный одним, двумя или тремя галогенами, или С1-6алкокси, необязательно замещенный одним, двумя или тремя галогенами; R2 представляет водород, галоген, гидрокси, нитро, циано, С1-6алкоксикарбонил, С1-6алкиламино, ди(С1-6алкил)амино, С1-6 алканоил, фенил, С1-6алкил, необязательно замещенный одним, двумя или тремя галогенами, или С1-6алкокси, необязательно замещенный одним, двумя или тремя галогенами; R3 представляет водород, галоген, гидрокси, нитро, циано, амино, карбокси, тетразолил, С1-6алкокси, С1-6алкоксикарбонил, С1-6алканоил, С1-6 алканоиламино, С1-6алкил, необязательно замещенный одним, двумя или тремя галогенами или гидрокси; R4 представляет или где R40 представляет С1-6алкил, ...

Подробнее
30-09-1999 дата публикации

Arylphenylsubstituierte cyclische Ketoenole

Номер: DE0019813354A1
Принадлежит:

The invention relates to new aryl phenyl substituted ketoenols of formula (I), where X is halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkyl sulfinyl, alkyl sulfonyl, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro, cyano or possibly substituted phenyl, phenoxy, phenylthio, phenyl alkoxy or phenyl alkylthio; Z is possibly substituted cycloalkyl, aryl or hetaryl; W and Z independently of each other are hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro or cyano; and CKE is one of groups (1), (2), (3), (4), (5), (6), (7) or (8), where A, B, D, G and Q<1> to Q<6> have the meanings assigned in the description. The invention also relates to several methods for producing said ketoenols and to their use as pest control agents and herbicides.

Подробнее
30-01-1975 дата публикации

VERFAHREN ZUR HERSTELLUNG EINES SCHMIEROELADDITIVS

Номер: DE0002429826A1
Принадлежит:

Подробнее
19-01-1977 дата публикации

AQUATIC ORGANISM EXPELLANTS

Номер: GB0001462139A
Автор:
Принадлежит:

... 1462139 Anti-fouling compositions containing succinimide derivatives IHARA CHEMICAL KOGYO KK 21 Nov 1974 [23 July 1974 5 Aug 1974 9 Aug 1974] 50552/74 Headings C3P and C3Q [Also in Divisions C2 and C4] Paints and resinous solutions having aquatic organism expellant properties contain as active ingredient a compound of formula where both Xs are Br and (Y) n represents 3- or 4-methyl-; 2-methoxy-; 3,5-dimethyl-; 3- chloro-4-methyl-; H; 2- or 4-nitro, together with further additives such as A1 powder, red iron oxide, lead chromate, titanium white, chrome yellow, cyanine green, rosin, methyl isobutyl ketone and tricresyl phosphate.

Подробнее
10-12-1986 дата публикации

PYRROLIDINE-2 5-DIONE STABILIZERS

Номер: GB0008626982D0
Автор:
Принадлежит:

Подробнее
06-10-1999 дата публикации

Process for making maleic anhydride polymers which include maleamic acid and/or its cyclic imide repeat units

Номер: GB0009918315D0
Автор:
Принадлежит:

Подробнее
31-12-2007 дата публикации

Helix 12 directed non-steroidal antiandrogens

Номер: AP0200704276A0
Принадлежит:

Подробнее
31-01-1996 дата публикации

Estrogen agonists/antagonists

Номер: AP0009500774A0
Автор:
Принадлежит:

Подробнее
31-12-2007 дата публикации

Helix 12 directed non-steroidal antiandrogens

Номер: AP2007004276A0
Принадлежит:

Подробнее
30-11-1980 дата публикации

Method of preparation of cyclic tertiary amoebas.

Номер: OA0000004987A
Автор:
Принадлежит:

Подробнее
20-11-1986 дата публикации

Derived from the 1-hétéroaryl-4-/(2,5-pyrrolidinedion-1-yl) alkyl/piperazine.

Номер: OA0000007809A
Принадлежит:

Подробнее
30-03-1971 дата публикации

Method of preparation of new substituted pyrrolidines.

Номер: OA0000003563A
Автор:
Принадлежит:

Подробнее
31-12-2007 дата публикации

Helix 12 directed non-steroidal antiandrogens

Номер: AP0200704276D0
Принадлежит:

Подробнее
25-01-1982 дата публикации

PROCEDURES FOR the PRODUCTION OF NEW ONE, HETERO-CYCLIC SUBSTITUTED 5-SULFAMOYLBENZOESAEUREDERIVATEN AND YOUR SALTS

Номер: AT0000365568B
Автор:
Принадлежит:

Подробнее
26-01-1976 дата публикации

METHOD FOR PRODUCING NEW [...] AND THEIR sOUR ADDITION SALTS

Номер: AT0000327174B
Автор:
Принадлежит:

Подробнее
10-03-1989 дата публикации

PROCEDURE FOR the PRODUCTION OF 1-HETEROARYL-4 ((2,5-PYRROLIDINDION-1-YL) AKLYL) IPERAZIN DERIVATIVES

Номер: AT0000387773B
Автор:
Принадлежит:

Подробнее
15-04-1975 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN SULFAMIDEN UND DEREN SAUREADDITIONSSALZEN

Номер: ATA915074A
Автор:
Принадлежит:

Подробнее
15-04-1975 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN SULFAMIDEN UND DEREN SAUREADDITIONSSALZEN

Номер: ATA915174A
Автор:
Принадлежит:

Подробнее
15-08-1988 дата публикации

VERFAHREN ZUR HERSTELLUNG VON 1-HETEROARYL-4-((2,5-PYRROLIDINDION-1-YL)AKLYL) IPERAZIN-DERIVATEN

Номер: ATA291584A
Автор:
Принадлежит:

Подробнее
15-09-1979 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN HETEROCYCLISCH SUBSTITUIERTEN 5-SULFAMOYL- BENZOESAEUREDERIVATEN UND IHREN SALZEN

Номер: ATA316475A
Автор:
Принадлежит:

Подробнее
15-06-1981 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN, HETEROCYCLISCH SUBSTITUIERTEN 5-SULFAMOYLBENZOESAEUREDERIVATEN UND IHREN SALZEN

Номер: ATA267878A
Автор:
Принадлежит:

Подробнее
15-06-1981 дата публикации

PROCEDURES FOR the PRODUCTION OF NEW ONE, HETERO-CYCLIC SUBSTITUTED 5-SULFAMOYLBENZOESAEUREDERIVATEN AND YOUR SALTS

Номер: AT0000267878A
Автор:
Принадлежит:

Подробнее
10-04-1980 дата публикации

PROCEDURES FOR the PRODUCTION OF NEW HETERO-CYCLIC SUBSTITUTED 5-SULFAMOYL BENZOIC ACID DERIVATIVES AND YOUR SALTS

Номер: AT0000356091B
Автор:
Принадлежит:

Подробнее
15-08-1984 дата публикации

SUBSTITUTED SUCCINIC ACID IMIDES AND YOUR USE AS FUNGICIDES MEANS.

Номер: AT0000008882T
Принадлежит:

Подробнее
25-02-1975 дата публикации

[...] OF NEW [...]

Номер: AT0000320613B
Автор:
Принадлежит:

Подробнее
25-04-1975 дата публикации

METHOD FOR PRODUCING NEW [...] THEIR [...]

Номер: AT0000321889B
Автор:
Принадлежит:

Подробнее
26-01-1976 дата публикации

METHOD FOR PRODUCING NEW [...] AND THEIR sOUR ADDITION SALTS

Номер: AT0000327173B
Автор:
Принадлежит:

Подробнее
15-06-2005 дата публикации

BIPHENYLDERIVATE AND YOUR USE AS ACTIVATORS OF THE PPAR GAMMA RECEPTOR

Номер: AT0000297386T
Принадлежит:

Подробнее
15-03-2002 дата публикации

ÖSTROGEN AGONISTEN/ANTAGONISTEN

Номер: AT0000214382T
Принадлежит:

Подробнее
10-08-1971 дата публикации

Micro-biological procedure for the production of a new, insecticide effective substance

Номер: AT0000291896B
Автор:
Принадлежит:

Подробнее
13-04-1971 дата публикации

Procedure for the production of new Succinimidderivate and their salts

Номер: AT0000289095B
Автор:
Принадлежит:

Подробнее
15-01-2004 дата публикации

PROCEDURE AND REAGENT FUR N-ALKYLATING UREIDES

Номер: AT0000257153T
Принадлежит:

Подробнее
04-10-1973 дата публикации

CHEMICAL COMPOUNDS

Номер: AU0000470838B2
Автор:
Принадлежит:

Подробнее
28-02-2019 дата публикации

Compositions for the treatment of pulmonary fibrosis

Номер: AU2017301113A1
Принадлежит: Shelston IP Pty Ltd.

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

Подробнее
29-01-2015 дата публикации

Conjugates of cell binding molecules with cytotoxic agents

Номер: AU2012385228A1
Принадлежит:

A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a formula (I), wherein T, L, m, n, Y, R ...

Подробнее
07-07-2011 дата публикации

Method for preparing activated esters

Номер: AU2009334689A1
Принадлежит:

The invention relates to a method for preparing an activated ester of the formula (I), where R is a (C-C) alkyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, and ALK is a (C-C) alkylene group, said method consisting of reacting the dicyclohexylamine P salt and the disuccinimidyl carbonate (DSC) in a solvent in which the dicyclohexylamine salt of the N-hydroxysuccinimide P is precipitated. The invention also relates to products of the formula P.

Подробнее
13-12-2012 дата публикации

Copolymers for near-infrared radiation-sensitive coating compositions for positive-working thermal lithographic printing plates

Номер: AU2010273146A1
Принадлежит:

There is provided a copolymer having the general structure below, wherein a, b, and d are molar ratios varying between about 0.01 and about 0.90 and c is a molar ratio varying between about 0,01 and about 0.90; A1 represents monomer units comprising a cyano-containing pendant group in which the cyano is not directly attached to the backbone of the copolymer; A2 represents monomer units comprising two or more hydrogen bonding sites; A3 represents monomer units that increase solubility in organic solvents; and A4 represents monomer units that increase solubility in aqueous alkaline solutions. There is also provided a near-infrared radiation-sensitive coating composition comprising this copolymer as well as a positive-working thermal lithographic printing plate comprising a near-infrared radiation-sensitive coating comprising this copolymer, a method of producing such a printing plate, and finally a method of printing using such a printing plate. Formula (I) ...

Подробнее
24-05-2018 дата публикации

Nucleotide analogues

Номер: AU2016349457A1
Принадлежит: Spruson & Ferguson

The present invention provides methods, compositions, mixtures and kits utilizing deoxynucleoside triphosphates comprising a 3'-O position capped by a group comprising methylenedisulfide as a cleavable protecting group and a detectable label reversibly connected to the nucleobase of said deoxynucleoside. Such compounds provide new possibilities for future sequencing technologies, including but not limited to Sequencing by Synthesis.

Подробнее
20-05-2021 дата публикации

Sulphamoylpyrrolamide derivatives and the use thereof as medicaments for the treatment of Hepatitis B

Номер: AU2019236657B2
Принадлежит:

Abstract SULPHAMOYLPYRROLAMIDE DERIVATIVESAND THE USE THEREOF AS 5 MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B A method of preparing inhibitors of HBV replication of Formula (ID) Ra R b R6 0 X-N, /N-SH Rd 10 R U N R4 including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, Ra to Rd and R4 toR6 have the meaning as defined herein wherein such compound is not H 0 H 0 o N-O'CF3 11 T) N CI I N-S N H N-SC\ H 15 or - ...

Подробнее
29-08-1978 дата публикации

LACTAM COMPOUNDS AND CONJUGATES

Номер: CA0001037475A1
Принадлежит:

Подробнее
07-06-2011 дата публикации

CARBAMIC ACID COMPOUNDS COMPRISING AN AMIDE LINKAGE AS HDAC INHIBITORS

Номер: CA0002423868C
Принадлежит: TOPOTARGET UK LIMITED

This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (see above formula) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: -NR1C (=O) - and -C (=O) NR1-; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, and ethers, thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and to inhibit conditions such as cancer and psoriasis.

Подробнее
17-07-2008 дата публикации

PROCESS FOR PREPARING 5-BIPHENYL-4-AMINO-2-METHYL PENTANOIC ACID

Номер: CA0002674291A1
Принадлежит:

The present invention relates to pyrrolidin-2-ones according to the formu la (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting gr oup, methods for their preparation and their use in the preparation of NEP-i nhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S )-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or sa lt thereof.

Подробнее
29-12-2010 дата публикации

COPOLYMERS, POLYMERIC PARTICLES COMPRISING SAID COPOLYMERS AND COPOLYMERIC BINDERS FOR RADIATION-SENSITIVE COATING COMPOSITIONS FOR NEGATIVE-WORKING RADIATION-SENSITIVE LITHOGRAPHIC PRINTING PLATES

Номер: CA0002768722A1
Принадлежит:

There is provided a copolymer and polymeric particle comprising the copolymer, a method of producing a polymeric particle, a copolymeric binder, a method of producing a copolymeric binder, a near infrared radiation-sensitive coating composition, a negative working lithographic offset printing plate, a method of producing a negative working lithographic offset printing plate and methods of imaging the plate and printing with the imaged plate.

Подробнее
03-01-1978 дата публикации

N-(3-HYDROXYARYL-PROPYL)-IMIDES

Номер: CA0001023739A1
Автор: LIND HANNS
Принадлежит:

Подробнее
26-06-1990 дата публикации

2,5-PYRROLIDINEDIONE DERIVATIVES USEFUL AS ANTIARRHYTHMIC AGENTS

Номер: CA0001270833A1
Принадлежит:

Подробнее
20-01-2009 дата публикации

ARYL PHENYL SUBSTITUTED CYCLIC KETOENOLS

Номер: CA0002325526C
Принадлежит: BAYER AKTIENGESELLSCHAFT

The invention relates to new aryl phenyl substituted ketoenols of formula (I), where X is halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkyl sulfinyl, alkyl sulfonyl, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro, cyano or possibly substituted phenyl, phenoxy, phenylthio, phenyl alkoxy or phenyl alkylthio; Z is possibly substituted cycloalkyl, aryl or hetaryl; W and Z independently of each other are hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogen alkyl, halogen alkoxy, halogen alkenyloxy, nitro or cyano; and CKE is one of groups (1), (2), (3), (4), (5), (6), (7) or (8), where A, B, D, G and Q1 to Q6 have the meanings assigned in the description. The invention also relates to several methods for producing said ketoenols and to their use as pest control agents and herbicides.

Подробнее
16-01-2014 дата публикации

CONJUGATES OF CELL BINDING MOLECULES WITH CYTOTOXIC AGENTS

Номер: CA3102268A1
Принадлежит:

Подробнее
11-06-2002 дата публикации

RADIOACTIVE IODINE COMPOUND FOR LABELING AN ANTIBODY

Номер: CA0002056633C
Принадлежит: SHIONOGI & CO., LTD., SHIONOGI & CO

The radioactive iodine compound of this invention or an intermediate for preparing the compound is represented by the following formula (I): (see formula I) wherein R is H or 125I. The radioactive compound can readily intro- duce a radioactive isotope element such as 125I into an antibody molecule without damaging the activity of the antibody molecule. Therefore, the compound can prefera- bly be used to label an antibody of immunoradiometric assay, and allow a higher degree of measurement sensi- tivity.

Подробнее
22-04-1999 дата публикации

AMINOBUTANOIC ACID DERIVATIVES

Номер: CA0002305463A1
Принадлежит:

Aminobutanoic acid derivatives represented by general formula (I) and salts thereof (wherein each symbol is as defined in the description). The derivatives inhibit matrix metalloproteinases and are therefore useful for the prevention and/or treatment of rheumatism, osteoarthritis, pathologic bone resorption, osteoporosis, periodontal diseases, interstitial nephritis, arteriosclerosis, pulmonary emphysema, hepatic cirrhosis, corneal injury, diseases due to metastasis and infiltration of cancer cells or proliferation thereof, autoimmune diseases (such as Crohn's disease and Sjögren's disease), diseases due to transmigration of white blood cells or infiltration thereof, neovascularization, multiple sclerosis, aortic aneurysm, endometritis and so on.

Подробнее
15-07-1955 дата публикации

Procédé de préparation d'une succinimide.

Номер: CH0000308502A
Принадлежит: PARKE DAVIS & CO, PARKE, DAVIS & COMPANY

Подробнее
15-12-1955 дата публикации

Procédé de préparation d'une succinimide.

Номер: CH0000312042A
Принадлежит: PARKE DAVIS & CO, PARKE, DAVIS & COMPANY

Подробнее
15-12-1955 дата публикации

Procédé de préparation d'une succinimide.

Номер: CH0000312041A
Принадлежит: PARKE DAVIS & CO, PARKE, DAVIS & COMPANY

Подробнее
15-09-1976 дата публикации

Номер: CH0000579549A5
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Подробнее
30-09-1976 дата публикации

Номер: CH0000580069A5
Автор:

Подробнее
30-09-1976 дата публикации

Номер: CH0000580068A5
Автор:

Подробнее
29-10-1976 дата публикации

Номер: CH0000581306A5
Автор:
Принадлежит: OLIN CORP, OLIN CORP.

Подробнее
13-09-1974 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN SUCCINIMIDODERIVATEN.

Номер: CH0000553777A
Автор:

Подробнее
27-02-1976 дата публикации

Sulphamido-aralkylamine cpds - with vasodilatory, cardiac-stimulant, blood-pressure, and broncholytic activity

Номер: CH0000572905A5
Автор:

Title cpds. of formula (I):- (where R1 is H or lower alkyl and R2 is lower alkyl, or R1+R2 is -(CH2)1-5-; R3 is H or OH. R4 is H, Me or Et; and R5 is H or alkyl opt. substd. by a heterocyclic residue or is an aralkyl or aryloxyalkyl gp. in which the aryl moiety is opt. substd.), in the form of the racemates, diastereomeric racemates or optical antipodes, and their acid addn. salts, have peripheral vasodilatory activity and effects on blood pressure, and also increase cardiac efficiency (without increasing heart rate) and as broncholytic agents. (I) are also inters. for pharmaceuticals. They are pref. prepd. by removing the protecting gps. from a corresp. cpd. in which the omega-amino gp. is protected by a hydro(geno)lytically removable gp. and/or the phenolic OH gp. is protected by a gp. which is removable hydro(geno)lyticall, by re-esterificn. of by means of ether-eliminating agents.

Подробнее
15-03-2012 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20120065408A1
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

Подробнее
11-04-2013 дата публикации

Synthetic processes for the preparation of aminocyclohexyl ether compounds

Номер: US20130090483A1
Принадлежит: Cardiome Pharma Corp

This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R 3 , R 4 and R 5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

Подробнее
08-08-2013 дата публикации

PROCESS FOR PRODUCING COMPOUNDS COMPRISING NITRILE FUNCTIONS

Номер: US20130204001A1
Принадлежит: Rhodia Operations

The production of compounds comprising nitrile functions and of cyclic imide compounds is described. Further described, is the production of compounds comprising nitrile functions from compounds comprising carboxylic functions, optionally of natural and renewable origin, and from a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN). 1. A process for preparing at least one nitrile of general formula I{'br': None, 'sub': v', '1', 'w, '(NC)—R—(CN)\u2003\u2003(I)'} {'br': None, 'sub': x', '1', 'y, '(HOOC)—R—(COOH)\u2003\u2003(II)'}, 'and at least cyclic imides 3-methylglutarimide and 3-ethylsuccinimide, by reacting at least one carboxylic acid of general formula II'}and a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN),whereinx, y are equal to 0 or 1 with (x+y) equal to 1 or 2,v, w are equal to 0 or 1 with (v+w) equal to 1 or 2, and from 4 carbon atoms to 34 carbon atoms when (x+y) is equal to 2, and', 'from 2 carbon atoms to 22 carbon atoms when (x+y) is equal to 1., 'R1 represents a linear or branched, saturated or unsaturated hydrocarbon-based group which can comprise heteroatoms, comprising2. The process as defined in claim 1 , wherein the mixture N of dinitriles is a mixture resulting from the process for producing adiponitrile by double hydrocyanation of butadiene.3. The process as defined in claim 1 , wherein the mixture N of dinitriles has the following composition by weight:2-Methylglutaronitrile from 70% to 95%,2-Ethylsuccinonitrile from 5% to 30%, andAdiponitrile from 0% to 10%, andwherein the remaining portion of the composition is composed of various impurities.4. The process as defined in claim 1 , wherein the compound of formula II is derived from a renewable matter of vegetable or animal origin.5. The process as defined in claim 4 , wherein the compound of formula II is selected from the group consisting of a caproic acid ...

Подробнее
07-11-2013 дата публикации

Polymer

Номер: US20130295040A1
Принадлежит: Warwick Effect Polymers Limited

The application provides a method of producing a comb polymer comprising the steps of: (a) Providing: (i) a plurality of monomers which are linear, branched or star-shaped, substituted or non-substituted, and have an olefinically unsaturated moiety, the olefinically unsaturated moiety being capable of undergoing addition polymerisation; (ii) an initiator compound; the initiator compound comprising a homolytically cleavable bond. (iii) a catalyst capable of catalysing the polymerisation of the monomer; and (b) Causing the catalyst to catalyse, in combination with the initiator, the polymerisation of a plurality of the monomers to produce the comb polymer. Catalysts and polymers obtainable by the process are also provided. Preferably, the comb polymer is capable of binding proteins and may be produced from monomers which are alkoxy polyethers, such as poly(alkyleneglycol) or polytetrahydrofuran.

Подробнее
21-11-2013 дата публикации

Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions

Номер: US20130310555A1
Автор: Hyun-Soon Chong
Принадлежит: Illinois Institute of Technology

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.

Подробнее
02-01-2014 дата публикации

2-Phenoxy- and 2-Phenylsulfonamide Derivatives with CCR3 Antagonistic Activity for the Treatment of Inflammatory or Immunological Disorders

Номер: US20140005176A1
Принадлежит: Axikin Pharmaceuticals, Inc.

Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders. 117.-. (canceled)22. The method of claim 18 , wherein the compound claim 18 , its tautomeric or stereoisomeric form claim 18 , or a physiologically acceptable salt thereof claim 18 , is selected from the group consisting of:(R)—N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-5-cyano-2-(3,5-dichloro-phenoxy)-benzenesulfonamide;(S)—N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-5-cyano-2-(3,5-dichloro-phenoxy)-benzenesulfonamide;N-(1-aza-bicyclo[2.2.2]oct-3-yl)-2-(3,5-dichloro-phenylsulfanyl)-5-nitro-benzenesulfonamide; and(R)-5-cyano-2-(3,5-dichlorophenoxy)-N-(2-(2,5-dioxopyrrolidin-1-yl)ethyl)-N-(1-aza-bicyclo[2.2.2]oct-3-yl)benzenesulfonamide.23. The method of claim 18 , wherein the compound claim 18 , its tautomeric or stereoisomeric form claim 18 , or a physiologically acceptable salt thereof is formulated with one or more pharmaceutically acceptable excipients.24. The method of claim 23 , wherein the excipient is an inert substance selected from the group consisting of a carrier claim 23 , a diluent claim 23 , a flavoring agent claim 23 , a sweetener claim 23 , a lubricant claim 23 , a solubilizer claim 23 , a suspending agent claim 23 , a binder claim 23 , a tablet disintegrating agent and an encapsulating agent. The present invention relates to a benzenesulfonamide derivative, which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor 3) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of ...

Подробнее
07-01-2016 дата публикации

Methods and compositions for radiohalogen protein labeling

Номер: US20160002121A1
Принадлежит: Genentech Inc

Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [ 125 I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.

Подробнее
07-01-2016 дата публикации

PLANT GROWTH REGULATING COMPOUNDS

Номер: US20160002161A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds. 2. The compound according to wherein R1 and R2 are independently selected from H claim 1 , methyl claim 1 , ethyl claim 1 , halogen or methoxy or form a C6 cycloalkyl claim 1 , preferably unsubstituted.3. The compound according to wherein R1 and R2 are independently selected from H and methyl.4. The compound according to wherein R1 and R2 are both methyl.5. The compound according to wherein one of R1 and R2 is hydrogen and the other is methyl.6. The compound according to wherein R3 is selected from H claim 1 , C1-C6 alkyl optionally substituted by one to five R4 claim 1 , methoxy claim 1 , ethoxy claim 1 , cyano claim 1 , acetyl claim 1 , acetoxy claim 1 , cyclopropyl optionally substituted with R4 claim 1 , C1-C6 alkenyl optionally substituted by one to five R4 claim 1 , C1-C6 alkynyl optionally substituted by one to five R4; and wherein each R4 is preferably independently halogen claim 1 , methoxy or cyano.7. The compound according to wherein R3 is selected from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , butyl claim 1 , isopropyl claim 1 , trifluoromethyl claim 1 , trifluoroethyl claim 1 , methoxymethyl claim 1 , methoxyethyl claim 1 , methoxy claim 1 , ethoxy claim 1 , cyano claim 1 , acetyl claim 1 , acetoxy claim 1 , cyclopropyl claim 1 , allyl claim 1 , propargyl claim 1 , phenyl claim 1 , benzyl claim 1 , pyridyl or thiazolyl.8. The compound according to wherein X is selected from H claim 1 , methyl claim 1 , ethyl claim 1 , iso-propyl claim 1 , halogen claim 1 , alkoxy claim 1 , alkoxyalkyl claim 1 , haloalkyl claim 1 , cyano claim 1 , nitro claim 1 , acetylene claim 1 , acetoxy claim 1 , acetyl claim 1 , carboxyl claim 1 , methoxycarbonyl claim 1 , or from unsubstituted ...

Подробнее
07-01-2021 дата публикации

AMINOBENZOIC ACID DERIVATIVES FOR USE AS ANTI-INFLAMMATORY AGENTS, ANTI-METASTATIC AGENTS AND/OR ANTICANCER AGENTS

Номер: US20210002222A1
Принадлежит: 3R VALO, S.E.C.

There are provided compounds of formula (I) 113-. (canceled)1538-. (canceled)39. The method of claim 57 , wherein said cancer cell growth is inhibited by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to an untreated subject.40. (canceled)41. The method of claim 57 , wherein a relative STAT1 activation of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.42. The method of claim 57 , or wherein a relative STAT3 activation of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.43. The method of claim 57 , wherein a CD40 expression of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.44. The method of claim 57 , wherein a MHC-II expression of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.45. The method of claim 57 , wherein a production of NO of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.46. The method of claim 57 , wherein TNFα/NFκB and/or IL6/STAT3 signaling pathways of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 ...

Подробнее
02-01-2020 дата публикации

DIARYLAMINE-BASED COMPOUND, ANTI-AGING AGENT, AND POLYMER COMPOSITION

Номер: US20200002507A1
Принадлежит: ZEON CORPORATION

The present invention provides a diarylamine-based compound represented by General Formula (1): 5. The diarylamine-based compound according to claim 1 , wherein Aand Aare a 1 claim 1 ,4-phenylene group.8. The composition according to claim 7 , wherein Rand Reach independently represent a linear or branched Cto Calkyl group which may have a substituent claim 7 , or a phenyl group which may have a substituent.10. The composition according to claim 1 , wherein a weight ratio of the diarylamine-based compound to the condensed heterocyclic compound is 30:1 to 1:30 as “diarylamine-based compound:condensed heterocyclic compound”.11. An antioxidant comprising the diarylamine-based compound according to claim 1 , or the composition according to any one of to .12. The antioxidant according to claim 11 , wherein the antioxidant is an antioxidant for a polymer.13. A polymer composition comprising a polymer and the antioxidant according to .14. The polymer composition according to claim 13 , wherein the polymer is a synthetic resin.15. The polymer composition according to claim 13 , wherein the polymer is a rubber.16. The polymer composition according to claim 15 , wherein the rubber is an acrylic rubber.17. The polymer composition according to claim 13 , wherein a content of the antioxidant is 0.05 to 30 parts by weight relative to 100 parts by weight of the polymer.18. An antioxidant comprising the composition according to . The disclosure relates to a novel diarylamine-based compound which has an excellent antioxidant effect on polymer materials required to have high heat resistance (for example, heat resistance in a high temperature range of 190° C. or more) and can be suitably used as an antioxidant, and an antioxidant and a polymer composition comprising such a diarylamine-based compound.With development of petrochemistry, polymers composed of organic compounds have contributed to human development in a variety of forms such as plastics, rubber, fibers, and films. Because ...

Подробнее
04-01-2018 дата публикации

HYDROXYAROMATIC SUCCINIMIDE DETERGENTS FOR LUBRICATING COMPOSITIONS

Номер: US20180002630A1
Принадлежит:

A lubricating composition includes an oil of lubricating viscosity and an N-substituted hydroxyaromatic succinimide or a salt thereof. 1. A lubricating composition comprising:an oil of lubricating viscosity; andan N-substituted hydroxyaromatic succinimide or a salt thereof.2. The composition of claim 1 , wherein the hydroxyaromatic succinimide includes a hydrocarbyl group of at least 8 carbon atoms.3. The composition of claim 1 , wherein the hydrocarbyl group is attached to the succinimide ring.4. The composition of claim 1 , wherein the hydrocarbyl group is a linear alkyl or linear alkenyl group.5. The composition of claim 1 , wherein the hydroxyaromatic succinimide is a succinimide derivative of a hydroxyaromatic amine.6. The composition of claim 5 , wherein the hydroxyaromatic amine is an aminophenol.8. The composition of claim 7 , wherein Ris selected from hydrocarbyl groups of at least 10 or at least 12 claim 7 , or at least 14 claim 7 , or at least 16 claim 7 , or at least 18 carbon atoms.9. The composition of claim 7 , wherein Ris selected from hydrocarbyl groups of up to 30 carbon atoms claim 7 , or up to 28 carbon atoms claim 7 , or up to 26 carbon atoms claim 7 , or up to 24 carbon atoms claim 7 , or up to 22 carbon atoms.10. The composition of claim 7 , wherein Ris selected from alkyl and alkenyl groups of at least 10 carbon atoms claim 7 , or at least 12 carbon atoms claim 7 , or at least 14 carbon atoms claim 7 , or at least 16 carbon atoms claim 7 , or at least 18 carbon atoms.11. The composition of claim 7 , wherein Ris selected from alkyl and alkenyl groups of up to 30 carbon atoms claim 7 , or up to 28 carbon atoms claim 7 , or up to 26 carbon atoms claim 7 , or up to 24 carbon atoms claim 7 , or up to 22 carbon atoms.12. The composition of claim 7 , wherein Ris selected from linear alkyl and alkenyl groups.13. The composition of claim 7 , wherein n is 0.14. The composition of claim 7 , wherein n is at least 1 and Ris selected from alkyl and alkenyl ...

Подробнее
01-01-2015 дата публикации

METHOD FOR CONVERSION OF DIAMMONIUM SUCCINATE IN FERMENTATION BROTH TO 2-PYRROLIDONE AND N-METHYLPYRROLIDONE

Номер: US20150005510A1
Принадлежит: Myriant Corporation

This invention relates to a process for preparing 2-pyrrolidone (also called 2-pyrrolidinone) and N-methylpyrrolidone (also called N-methylpyrrolidinone) from diammonium succinate in fermentation broth. In the first stage of this invention, renewable carbon resources are utilized to produce diammonium succinate through biological fermentation. In the second stage of this present invention, diammonium succinate is converted into 2-pyrrolidone and N-methylpyrrolidone through a two step reaction. Both the steps of the reaction leading to the production of 2-pyrrolidone and N-methylpyrrolidone are carried out in a solvent phase to prevent the loss of succinimide through hydrolysis. 1. A process for preparing succinimide comprising the steps of:(a) providing a fermentation broth comprising diammonium succinate;(b) adding a polar organic solvent with boiling point higher than that of water to said fermentation broth;(c) evaporating water in said fermentation broth;(d) raising temperature of said fermentation broth to at least 120° C. to convert said diammonium succinate to succinimide.2. The Process according to claim 1 , wherein said fermentation broth is a concentrated fermentation broth.3. The process according to claim 1 , wherein said fermentation broth is subjected to ultrafiltration process before converting diammonium succinate to succinimide.4. The process according to claim 1 , wherein said fermentation broth is subjected to adsorption process to remove sugars and amino acids in the fermentation broth.5. The process according to claim 1 , wherein said polar organic solvent is selected from a group consisting of diglyme claim 1 , triglyme claim 1 , tetraglyme claim 1 , propylene glycol claim 1 , dimethylsulfoxide claim 1 , dimethylformamide claim 1 , dimethylacetamide claim 1 , dimethylsulfone claim 1 , sulfolane claim 1 , polyethylene glycol claim 1 , butoxytriglycol claim 1 , N-methylpyrrolidone claim 1 , 2-pyrrolidone claim 1 , gammabutyrolactone claim 1 , ...

Подробнее
12-01-2017 дата публикации

SYNTHESIS OF THERAPEUTIC AND DIAGNOSTIC DRUGS CENTERED ON REGIOSELECTIVE AND STEREOSELECTIVE RING OPENING OF AZIRIDINIUM IONS

Номер: US20170008863A1
Автор: Chong Hyun-Soon
Принадлежит:

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds. 2. The method of claim 1 , further comprising:converting a substituted β amino alcohol to a substituted alkylating agent;converting the substituted alkylating agent to the substituted aziridinium ion; andstereoselectively or regioselectively reacting the aziridinium ion with a nucleophile to obtain the compound.4. The method of claim 2 , further comprising:{'sub': 4', '2', '3', '3', '6', '4, 'converting the substituted alkylating agent to the aziridinium ion in the presence of halosequestering agent comprising AgClO, AgOTf, AgCO, AgOTs, AgNO, AgSbF, or AgBF; and'}stereoselectively or regioselectively reacting the aziridinium ion in situ with a nucleophile to obtain the compound.6. The method of claim 5 , further comprising:{'sub': 4', '2', '3', '3', '6', '4, 'converting the substituted alkylating agent to the aziridinium ion in the presence of halosequestering agent comprising AgClO, AgOTf, AgCO, AgOTs, AgNO, AgSbF, or AgBF; and'}stereoselectively or regioselectively reacting the aziridinium ion in situ with the nucleophile in the presence of a base to obtain the compound.7. The method of claim 5 , further comprising:converting a substituted β amino alcohol to a substituted alkylating agent;converting the substituted alkylating agent to the substituted aziridinium ion; andstereoselectively or regioselectively reacting the aziridinium ion with a nucleophile to obtain the compound, wherein the reaction occurs without isolation of any intermediate compound.9. The method of claim 8 , further comprising removing a protecting group comprising an amino claim 8 , a carboxyl claim 8 , or a hydroxyl protecting group from the compound using a deprotection reaction.10. The method of claim 9 , further comprising converting a nitro group in the compound to an amino ...

Подробнее
03-02-2022 дата публикации

CRYSTAL FORM A OF 2-(2, 5-DIOXOPYRROLIDIN-1YL) ETHYL METHYL FUMARATE, PREPARATION METHOD THEREFOR AND USE THEREOF

Номер: US20220033355A1
Принадлежит:

A crystal form A of 2-(2, 5-dioxopyrrolidin-1yl)ethyl methyl fumarate has a good light irradiation stability, high-temperature stability and high-humidity stability. 1. A crystal form A of 2-(2 , 5-dioxopyrrolidin-1yl)ethyl methyl fumarate , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has characteristic peaks at 2θ diffraction angles of 13.5±0.2° , 17.9±0.2° , 23.0±0.2° and 27.3±0.2°.2. The crystal form A of claim 1 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 13.3±0.2° claim 1 , and 18.2±0.2°.3. The crystal form A of claim 2 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 19.3±0.2° claim 2 , and 19.6±0.2°.4. The crystal form A of claim 3 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 16.6±0.2° claim 3 , 20.9±0.2° claim 3 , 22.0±0.2° claim 3 , 24.3±0.2° claim 3 , 25.3±0.2° claim 3 , and 30.6±0.2°.5. The crystal form A of claim 4 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 6.92±0.2° claim 4 , 11.5±0.2° claim 4 , 16.1±0.2° claim 4 , 23.7±0.2° claim 4 , 26.9±0.2° claim 4 , and 31.1±0.2°.9. The crystal form A of claim 1 , wherein the crystal form A has an X-ray powder refraction pattern substantially as shown in .10. The crystal form A of claim 1 , wherein the crystal form A has a characteristic endothermic peak in a temperature range of 96.0° C.-107.0° C. measured by differential scanning calorimetry.11. The crystal form A of claim 1 , wherein the crystal form A has a differential scanning calorimetry curve substantially as shown in .12. The crystal form A of claim 1 , wherein the crystal form A has a weight loss of less than 0.01% before a temperature of 125° C. in its thermo gravimetric analysis curve.13. The ...

Подробнее
18-01-2018 дата публикации

PROCESSES FOR THE CONVERGENT SYNTHESIS OF CALICHEAMICIN DERIVATIVES

Номер: US20180016228A1
Принадлежит: WYETH LLC

This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates. 2. The process of wherein the purifying of step (e) comprises the use of reverse phase high performance liquid chromatography having a mobile phase of about pH 7.0 to 9.0 followed by normal phase chromatography.5. The process of wherein the purifying of step (e) comprises the use of a reverse phase high performance liquid chromatography having a mobile phase of about pH 7.0 to 9.0 followed with a normal phase chromatography.9. A process according to claim 1 , wherein Alkis an alkylene of 2 to 5 carbon atoms claim 1 , and Spis an oxygen atom.10. A process according to claim 9 , wherein Alkis an alkylene of 3 carbon atoms.11. A process according to claim 1 , wherein Zis alkyl of 1 to 3 carbon atoms.12. A process according to claim 1 , wherein Ar is 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- claim 1 , or 1 claim 1 ,4-phenylene claim 1 , or 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- claim 1 , 1 claim 1 ,4- claim 1 , 1 claim 1 ,5- claim 1 , 1 claim 1 ,6- claim 1 , 1 claim 1 ,7- claim 1 , 1 claim 1 ,8- claim 1 , 2 claim 1 ,3- claim 1 , 2 claim 1 ,6- claim 1 , or 2 claim 1 ,7-naphthylidene.13. A process according to claim 12 , wherein Ar is 1 claim 12 ,4-phenylene.14. A process according to claim 1 , wherein Q is —NNHCO—.15. A process according to claim 1 , wherein Sp is straight or branched-chain divalent or trivalent alkyl radical of 1 to 12 carbon atoms.16. A process according to claim 15 , wherein Sp is straight or branched-chain divalent or trivalent alkyl radical of 1 to 6 carbon atoms.17. The process according to claim 1 , wherein the alcohol solvent is methanol.18. The process according to claim 1 , wherein the inert solvent is acetonitrile.19. The process according to claim 1 , wherein alkyl carboxylic acid is acetic acid.20. The process according to claim 1 , wherein the inert organic solvent is ...

Подробнее
16-01-2020 дата публикации

Prodrugs of Fumarates and Their Use in Treating Various Diseases

Номер: US20200016111A1
Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 111-. (canceled)13. A pharmaceutical composition comprising the compound of claim 12 , or a pharmaceutically acceptable salt thereof.14. A method of treating multiple sclerosis in a subject in need thereof claim 12 , comprising administering to the subject a therapeutically effective amount of the compound of .15. A method of treating multiple sclerosis in a subject in need thereof claim 13 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 16/145,703, filed Sep. 28, 2018, which is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, now U.S. Pat. No. 10,117,846, issued Nov. 6, 2018, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use ...

Подробнее
16-01-2020 дата публикации

Hydantoin containing deoxyuridine triphosphatase inhibitors

Номер: US20200017481A1
Автор: Mark Spyvee
Принадлежит: Cv6 Therapeutics NI Ltd

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Подробнее
01-02-2018 дата публикации

Prodrugs of fumarates and their use in treating various diseases

Номер: US20180030063A1
Принадлежит: Alkermes Pharma Ireland Ltd

The present invention provides compounds of formula (I), wherein: R 1 is unsubstituted C 1 -C 6 alkyl; L a is substituted or unsubstituted C 1 -C 6 alkyl linker, substituted or unsubstituted C 3 -C 10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R 2 and R 3 are each, independently, H, substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 6 -C 10 aryl; or alternatively, R 2 and R 3 , together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

Подробнее
11-02-2016 дата публикации

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

Номер: US20160039753A1
Принадлежит: ExxonMobil Research and Engineering Co

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Подробнее
06-02-2020 дата публикации

ANTIFIBRINOLYTIC COMPOUNDS

Номер: US20200039921A1
Автор: Chibber Bakshy A.
Принадлежит:

The present invention provides novel antifibrinilytic compounds, processes for their preparation, pharmaceutical and veterinary compositions thereof, and their use in medicine, in particular for the treatment of bleeding. 1. A compound of formula III:{'br': None, 'sup': 1', '1', '5, 'sub': '2', 'R—CH—X—R\u2003\u2003(III)'} [{'sup': 1', '6', '6', '7', '+', '6', '7', '8', '+', '9', '10, 'sub': '2', 'Ris —NH, —NHR, NRR—NRRRor —SRR;'}, {'sup': 5', '12', '13', '14', '15, 'sub': '2', 'Ris —C(O)R, —SOR, —P(O)RR, nitro or nitroso;'}, {'sup': 6', '7', '9', '10', '6', '7, 'sub': 1', '4', '1', '4, 'R, R, R8, Rand Rare independently (C-C)alkyl or halo(C-C)alkyl, or Rand R, together with the N atom to which they are attached form an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, or pyrrolyl group;'}, {'sup': 12', '13', '14', '15, 'sub': 1', '4', '1', '4, 'R, R, Rand Rare independently hydroxyl, —O—(C-C)alkyl or —(C-C)alkyl; and'}, {'sup': '1', 'Xis trans cyclohexan-1,4-diyl;'}, {'sup': 1', '2, 'sub': '2', 'with the proviso that Rin not NHwhen Ris COOH, or'}, 'a pharmaceutically acceptable salt thereof., 'wherein2. The compound of claim 1 , of formula IIIa:{'br': None, 'sup': 9', '10', '+', '5, 'sub': '2', 'RRS—CH—X—R\u2003\u2003(IIIa)'}or a pharmaceutically acceptable salt thereof.3. The compound of claim 1 , of formula IIIb:{'br': None, 'sup': 9', '10', '+', '1', '12, 'sub': '2', 'RRS—CH—X—C(O)R\u2003\u2003(IIIb)'}or a pharmaceutically acceptable salt thereof.4. The compound of claim 1 , wherein Ris hydroxyl or —O—(C-C)alkyl or a pharmaceutically acceptable salt thereof.5. The compound of claim 4 , wherein Ris hydroxyl claim 4 , or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein. Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 1 , or a pharmaceutically acceptable salt thereof.7. The compound of claim 6 , wherein Rand Rare both methyl claim 6 , or a pharmaceutically acceptable salt thereof. This application claims priority ...

Подробнее
06-02-2020 дата публикации

SULPHAMOYLPYRROLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20200039931A1
Принадлежит:

Inhibitors of HBV replication of Formula (ID) 115-. (canceled)191. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound as claimed in claim and a pharmaceutically acceptable carrier.202. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound as claimed in claim and a pharmaceutically acceptable carrier.213. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound as claimed in claim and a pharmaceutically acceptable carrier.221. A method of treating an HBV infection comprising administering a therapeutically effective amount of at least one compound as claimed in claim .232. A method of treating an HBV infection comprising administering a therapeutically effective amount of at least one compound as claimed in claim .243. A method of treating an HBV infection comprising administering a therapeutically effective amount of at least one compound as claimed in claim .251. A pharmaceutical product comprising (a) a compound as claimed in claim and (b) an HBV inhibitor.262. A pharmaceutical product comprising (a) a compound as claimed in claim and (b) an HBV inhibitor.273. A pharmaceutical product comprising (a) a compound as claimed in claim and (b) an HBV inhibitor. The Hepatitis B virus (HBV) is an enveloped, partially double-stranded DNA (dsDNA) virus of the Hepadnavirus family (Hepadnaviridae). Its genome contains 4 overlapping reading frames: the precore/core gene; the polymerase gene; the L, M, and S genes, which encode for the 3 envelope proteins; and the X gene.Upon infection, the partially double-stranded DNA genome (the relaxed circular DNA; rcDNA) is converted to a covalently closed circular DNA (cccDNA) in the nucleus of the host cell and the viral mRNAs are transcribed. Once encapsidated, the pregenomic RNA (pgRNA), which also codes for core protein and Pol, serves as the template for reverse transcription, which regenerates ...

Подробнее
15-02-2018 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20180042881A1
Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 1. (canceled)3. A pharmaceutical composition comprising a crystalline form of and a pharmaceutically acceptable carrier.4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of a crystalline form of .5. A method of treating multiple sclerosis in a subject in need thereof claim 3 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including psoriasis (Joshi ...

Подробнее
26-02-2015 дата публикации

Reversible pegylated drugs

Номер: US20150057219A1
Принадлежит: Yeda Research and Development Co Ltd

Reversible pegylated drugs are provided by derivatization of free functional groups of the drug selected from amino, hydroxyl, mercapto, phosphate and/or carboxyl with groups sensitive to mild basic conditions such as 9-fluorenylmethoxycarbonyl (Fmoc) or 2-sulfo-9-fluorenylmethoxycarbonyl (FMS), to which group a PEG moiety is attached. In these pegylated drugs, the PEG moiety and the drug residue are not linked directly to each other, but rather both residues are linked to different positions of the scaffold Fmoc or FMS structure that is highly sensitive to bases and is removable under physiological conditions. The drugs are preferably drugs containing an amino group, most preferably peptides and proteins of low or medium molecular weight. Similar molecules are provided wherein a protein carrier or another polymer carrier replaces the PEG moiety.

Подробнее
10-03-2022 дата публикации

(2,5-DIOXOPYRROLIDIN-1-YL)(PHENYL)-ACETAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES

Номер: US20220073461A1
Принадлежит:

The first object of the invention is the compound of general formula (I) or pharmaceutically acceptable salts thereof. A second object of the invention is the use of compounds described by general formula (I) as active ingredient in pharmaceutical compositions for the treatment of epileptic seizures or neuropathic pain or migraine. 114.-. (canceled)17. The compound according to claim 15 , characterized in that the halogen atom is a fluorine or chlorine atom.18. The compound according to claim 15 , characterized in that the alkyl moiety in the carbon backbone contains from 1 to 4 carbon atoms claim 15 , wherein the alkyl moiety has a straight or branched chain and is selected from the group comprising of: methyl claim 15 , ethyl claim 15 , propyl claim 15 , isopropyl claim 15 , n-butyl claim 15 , sec-butyl claim 15 , tert-butyl.19. The compound according to claim 15 , characterized in that k=0.20. The compound according to claim 15 , characterized in that X is nitrogen.21. The compound according to claim 15 , characterized in that the substituent A is selected from the group comprising of: 5-benzothiophenyl claim 15 , 2-naphthyl claim 15 , 5-benzisoxazolyl substituents.22. The compound according to claim 15 , characterized in that the substituent A is selected from the group comprising of: phenyl claim 15 , phenyl substituted with at least one chlorine atom or —CF claim 15 , —CHF claim 15 , —OCF claim 15 , —CH claim 15 , —SCFor phenyl.23. The compound according to claim 15 , characterized in that the substituent B is selected from the group comprising of phenyl or phenyl substituted with one or two halogen atoms.24. The compound according to claim 15 , characterized in that it is selected from the group comprising of:1-(2-Oxo-1-phenyl-2-(4-phenylpiperazin-1-yl)ethyl) pyrrolidine-2,5-dione1-(2-(4-(3-Chlorophenyl)piperazin-1-yl)-2-oxo-1-phenylethyl)pyrrolidine-2,5-dione1-(2-(4-(3,5-Dichlorophenyl)piperazin-1-yl)-2-oxo-1-phenylethyl)pyrrolidine-2,5-dione 1-(2-Oxo-1- ...

Подробнее
05-03-2015 дата публикации

PROCESS FOR MICROWAVE ASSISTED SYNTHESIS OF N-METHYL PYRROLIDONE

Номер: US20150065731A1
Принадлежит:

The present invention relates to a process for microwave assisted synthesis of N-methyl pyrrolidone (NMP). Particularly the process relates to the synthesis of N-methyl succinimide or corresponding analogues by using microwave irradiation which on hydrogenation in the presence of a hydrogenating catalyst gives N-methyl pyrrolidone. Compared to the conventional heating microwave process requires less energy inputs and reduces the reaction time drastically from 5-6 h to 2-5 min. 1. A process for synthesis of N-methyl pyrrolidone , said process comprising the steps of:(a) reacting a dicarboxylic acid or corresponding anhydride with non-aqueous methylamine with a molar ratio in the range 1:1 to 1:10 in solid state using microwave irradiation in the range of 600-900 W for a period of 1 to 10 minutes to obtain an intermediate N-methyl imide;(b) separating and purifying the intermediate N-methyl imide thus formed; and(c) converting the intermediate N-methyl imide to N-methyl pyrrolidone.2. The process according to claim 1 , wherein said dicarboxylic acid or anhydride is selected from the group consisting of maleic acid claim 1 , maleic anhydride claim 1 , succinic acid claim 1 , succinic anhydride and an analog thereof.3. The process according to claim 1 , wherein said non aqueous methylamine is selected from the group consisting of anhydrous methylamine claim 1 , methylamine in THF and methylamine hydrochloride.4. The process according to claim 1 , wherein an organic solvent is used for separating the intermediate N-methyl imide thus formed.5. The process according to claim 4 , wherein the organic solvent is selected from the group consisting of chloroform claim 4 , ethyl acetate claim 4 , dichloromethane and toluene.6. The process according to claim 1 , wherein purifying the intermediate N-methyl imide comprises subjecting the intermediate N-methyl imide to a crystallization process.7. The process according to claim 1 , wherein converting the intermediate N-methyl imide ...

Подробнее
08-03-2018 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20180064673A1
Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 2. The composition of claim 1 , wherein Ris methyl.3. The composition of claim 1 , wherein Lis an unsubstituted C-Calkyl.4. The composition of claim 3 , wherein Lis an unsubstituted C-Calkyl.5. The composition of claim 4 , wherein Lis an unsubstituted Calkyl.6. The composition of claim 1 , wherein Ris an unsubstituted C-Calkyl claim 1 , unsubstituted C-Calkenyl claim 1 , or unsubstituted C-Calkynyl.7. The composition of claim 6 , wherein Ris an unsubstituted C-Calkyl.8. The composition of claim 7 , wherein Ris an unsubstituted C-Calkyl.9. The composition of claim 8 , wherein Ris an unsubstituted C-Calkyl.10. The composition of claim 9 , wherein Ris methyl. This application is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016 which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or ...

Подробнее
12-03-2015 дата публикации

SUBSTITUTED B-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

Номер: US20150073004A1
Принадлежит:

The present invention relates to compounds of formula 1 3. A compound according to claim 1 , wherein Rrepresents hydrogen.6. A compound according to claim 1 , wherein X represents an O atom.7. A compound according to claim 1 , wherein Y represents halogen or a —CH claim 1 , —CHor —OCHgroup.8. A compound according to claim 7 , wherein Y represents Cl claim 7 , F or a —CH claim 7 , —CHor —OCHgroup.9. A compound according to claim 1 , wherein Z represents a (CH) claim 1 , CHN(CH) or CH═N(CH) group.10. A compound according to claim 9 , wherein Z represents a (CH)group.11. A compound according to claim 1 , wherein{'sub': 1-4', '3-6, 'R represents hydrogen or a —Calkyl, —Ccycloalkyl or fluorophenyl group; and'}R′ represents hydrogen.15. A method for the preventive or therapeutic treatment of a CXCR3 receptor mediated disease or disorder claim 1 , the method comprising the administration to a patient in need thereof of a pharmaceutically effective amount of a compound according to .16. The method according to wherein the disease or disorder is selected from the group consisting of COPD claim 15 , psoriasis claim 15 , graft/transplant rejection claim 15 , ophthalmological disease claim 15 , celiac disease claim 15 , inflammatory bowel disease (IBD) claim 15 , type 1 diabetes claim 15 , myasthenia gravis (MG) claim 15 , multiple sclerosis (MS) and other neuroinflammatory diseases claim 15 , lupus claim 15 , rheumatoid arthritis (RA) and lichen planus.17. A pharmaceutical composition comprising at least one compound according to and at least one pharmaceutically acceptable excipient. The present invention relates to compounds that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines.Chemokines are a large family of small soluble proteins of about 8 to 10 kDa in size. One of the major roles of chemokines is to direct the migration of immune cells. The mechanism by which the ...

Подробнее
17-03-2016 дата публикации

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

Номер: US20160075648A1
Принадлежит: ExxonMobil Research and Engineering Co

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Подробнее
17-03-2016 дата публикации

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

Номер: US20160075649A1
Принадлежит: ExxonMobil Research and Engineering Co

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Подробнее
31-03-2022 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20220096419A1
Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 2. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof.3. A method of treating multiple sclerosis in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound of .4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of the composition of . This application is a continuation of U.S. application Ser. No. 16/790,849, filed Feb. 14, 2020, which is a continuation of U.S. application Ser. No. 16/524,498, filed Jul. 29, 2019, now U.S. Pat. No. 10,596,140, issued Mar. 24, 2020, which is a continuation of U.S. application Ser. No. 16/145,703, filed Sep. 28, 2018, now U.S. Pat. No. 10,406,133, issued Sep. 10, 2019, which is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, now U.S. Pat. No. 10,117,846, issued Nov. 6, 2018, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the conterts of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United ...

Подробнее
19-06-2014 дата публикации

Inhibitors of Mycobacterium Tuberculosis Malate Synthase, Methods of Making and Uses Thereof

Номер: US20140171444A1
Принадлежит: The Texas A&M University System

The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided. 2. The substituted diketo acid compound of claim 1 , wherein Ris a 2- or 3-thienyl or (3-methyl)-2-thienyl substituted with Rat C5 claim 1 , wherein Ris one or more of Rat C2 claim 1 , Rat C3 claim 1 , Rat C4 claim 1 , Rat C5 claim 1 , or Rat C6 claim 1 , phenoxyphenyl claim 1 , or 2-thienyl.3. The substituted diketo acid compound of claim 2 , wherein R claim 2 , R claim 2 , R claim 2 , R claim 2 , and Rindependently are H claim 2 , OH claim 2 , NO claim 2 , Calkyl claim 2 , Calkoxy claim 2 , O(Calkyl)O(Calkyl) claim 2 , Br claim 2 , F claim 2 , Cl claim 2 , I claim 2 , Ph claim 2 , PhBr claim 2 , PhF claim 2 , PhCH claim 2 , PhOCH claim 2 , Ph(CH) claim 2 , CF claim 2 , CHSO claim 2 , imidazolyl claim 2 , or wherein Rand Rtogether are benzothienyl claim 2 ,4. The substituted diketo acid compound of claim 3 , wherein one or more of R claim 3 , R claim 3 , R claim 3 , Ror Ris independently methoxy claim 3 , Br claim 3 , F claim 3 , Cl claim 3 , I claim 3 , or methyl and Ris OH or ...

Подробнее
01-04-2021 дата публикации

FRICTION ADJUSTING AGENT AND LUBRICATING OIL COMPOSITION

Номер: US20210095221A1
Принадлежит: IDEMITSU KOSAN CO.,LTD.

The present invention provides a compound represented by formula (1) (in formula (1), Rand Reach independently represent a group represented by formula (2) or NHR(where Rand Rare not simultaneously NHR), Rrepresents any one of hydrogen, an alkyl group having 1-20 carbon atoms, an alkenyl group having 2-30 carbon atoms, an aryl group having 6-30 carbon atoms, an alkylaryl group having 7-30 carbon atoms, and an arylalkyl group having 7-30 carbon atoms, each Rindependently represents hydrogen or a hydrocarbon group having 1-30 carbon atoms, l represents an integer of 0-4, m represents an integer of 1-4 (where m is an integer of 2-4 in the case where Rand Rare a group represented by formula (2)), and each n independently represents an integer of 0-4, and, in formula (2), Rrepresents a hydrocarbon group having 6-24 carbon atoms, and Xand Xeach independently represent an oxygen atom or a sulfur atom). 2: The compound according to claim 1 , wherein in formula (1) claim 1 , Rrepresents an alkyl group having 6 to 24 carbon atoms claim 1 , an alkenyl group having 6 to 24 carbon atoms claim 1 , an aryl group having 6 to 24 carbon atoms claim 1 , an alkylaryl group having 7 to 24 carbon atoms claim 1 , an alkenylaryl group having 7 to 24 carbon atoms claim 1 , an arylalkyl group having 7 to 24 carbon atoms or an arylalkenyl group having 7 to 24 carbon atoms.3: The compound according to claim 1 , wherein in formula (1) claim 1 , each Rindependently represents hydrogen claim 1 , an alkyl group having 1 to 20 carbon atoms claim 1 , an alkenyl group having 2 to 30 carbon atoms claim 1 , an aryl group having 6 to 30 carbon atoms claim 1 , an alkylaryl group having 7 to 30 carbon atoms or an arylalkyl group having 7 to 30 carbon atoms.4: A friction adjusting agent claim 1 , comprising the compound according to .5: A lubricating oil composition claim 4 , comprising a base oil and the friction adjusting agent according to .6: A lubricating oil composition for continuously variable ...

Подробнее
16-04-2015 дата публикации

SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES

Номер: US20150105438A1
Автор: Liu Julie F.
Принадлежит: CONCERT PHARMACEUTICALS, INC.

This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. 2. The compound of claim 1 , wherein Ris CHor CD; and Yis H.6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. The compound of claim 1 , wherein Ris CDCD.14. A compound of claim 13 , having predominantly the (S) configuration.15. A compound of claim 13 , having predominantly the (R) configuration.17. A compound of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.18. A composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt of said compound; and an acceptable carrier.19. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt of said compound; and an acceptable carrier claim 1 , wherein the composition is suitable for the treatment of a disease selected from the group consisting of septic shock claim 1 , sepsis claim 1 , endotoxic shock claim 1 , hemodynamic shock and sepsis syndrome claim 1 , post ischemic reperfusion injury claim 1 , malaria claim 1 , mycobacterial infection claim 1 , meningitis claim 1 , psoriasis claim 1 , sarcoidosis claim 1 , psoriatic arthritis claim 1 , Behçet's Disease claim 1 , prurigo nodularis claim 1 , lupus claim 1 , uveitis claim 1 , congestive heart failure claim 1 , fibrotic disease claim 1 , cachexia claim 1 , graft rejection claim 1 , cancer claim 1 , autoimmune disease claim 1 , opportunistic infections in AIDS claim 1 , ...

Подробнее
29-04-2021 дата публикации

Prodrugs of Fumarates and Their Use in Treating Various Diseases

Номер: US20210122758A1
Принадлежит:

The present invention provides compounds of formula (I), 2. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt thereof.3. A method of treating multiple sclerosis in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound of .4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 16/221,884, filed Dec. 17, 2018, which is a continuation of U.S. application Ser. No. 15/683,189, filed Aug. 22, 2017, now U.S. Pat. No. 10,189,855, issued Jan. 29, 2019, which is a divisional of U.S. application Ser. No. 14/744,325, filed Jun. 19, 2015, now abandoned, which is a continuation of U.S. application Ser. No. 14/180,687, filed Feb. 14, 2014, now U.S. Pat. No. 9,090,558, issued Jul. 28, 2015, which claims the benefit of U.S. Provisional Application No. 61/782,445, filed on Mar. 14, 2013. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including psoriasis (Joshi and Strebel, WO 1999/ ...

Подробнее
28-04-2016 дата публикации

Sulphamoylpyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b

Номер: US20160115125A1
Принадлежит: Janssen Sciences Ireland ULC

Inhibitors of HBV replication of Formula (ID) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein X, R a to R d and R 4 to R 6 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

Подробнее
27-04-2017 дата публикации

Inactivation Method

Номер: US20170114339A1
Принадлежит: Thermo Fisher Scientific Baltics UAB

The present invention relates to the field of thermostable enzymes, methods for their inactivation, and related uses, kits and reagents. In particular, the invention relates to a method for reversible inactivation of thermophilic enzymes by chemical modification under aqueous or non-aqueous conditions.

Подробнее
18-04-2019 дата публикации

Diesel Detergent Without A Low Molecular Weight Penalty

Номер: US20190112539A1
Принадлежит:

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 1. A composition comprising a quaternary ammonium salt , wherein the quaternary ammonium salt comprises the reaction product of: (i) at least one tertiary amino group, and', '(ii) a hydrocarbyl-substituent derived from a hydrocarbon having a number average molecular weight of from about 100 to about 500;, 'a) a compound comprising a non-quaternized amide and/or ester detergent havingb) a quaternizing agent suitable for converting the tertiary amino group of compound (a) to a quaternary nitrogen.2. The composition of claim wherein 1 component b) , the quaternizing agent suitable for converting the tertiary amino group of compound a) to a quaternary nitrogen , comprises:(a) dialkyl sulfates;(b) benzyl halides;(c) hydrocarbyl substituted carbonates;(d) hydrocarbyl epoxides;(e) esters of carboxylic acids and/or polycarboxylic acids;(f) any combination thereof;wherein the quaternizing agent may optionally be used in combination with an acid.3. A diesel fuel comprising the composition of .4. The diesel fuel of claim 3 , wherein the diesel fuel is ultra-low sulfur diesel fuel.5. The diesel fuel of claim 3 , wherein the quaternary ammonium salt is present from about 10 to about 500 ppm.6. A method of minimizing creation of internal diesel injector deposits while additionally reducing the level of pre-existing internal diesel injector deposits comprising the step of supplying to a diesel engine a diesel fuel composition comprising (A) diesel fuel; and (B) a composition according to .7. The method of wherein the diesel engine comprises common rail diesel injectors. This application is a continuation application of U.S. application Ser. No. 14/434,985 which claims priority to PCT Application Serial No. PCT/US2013/ ...

Подробнее
25-04-2019 дата публикации

New nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio)molecules; precursors and conjugates thereof

Номер: US20190119316A1
Принадлежит: Advanced Accelerator Applications SA

Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio) molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conformconform.torespective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.

Подробнее
12-05-2016 дата публикации

ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES

Номер: US20160130240A1
Принадлежит:

The present invention relates to aryl sulfoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulfide and aryl sulfoxide derivatives have the general structure (I) 3. The compound as claimed in in whichA and B together with the atoms to which they are attached represent a substructure selected from the group consisting of (I-A) to (I-D),where{'sup': 1', '2', '3, 'claim-text': {'sup': 11', '11, 'represent oxygen; sulfur, NRor a salt of NR;'}, 'V, Vand Veach independently of one another'}{'sup': 1', '1', '2, 'Qrepresents oxygen, sulfur, NRor CRR;'}{'sup': 2', '10', '8', '9, 'Qrepresents NRor CRR;'}{'sup': '1', 'claim-text': represents alkyl, cycloalkylalkyl, haloalkyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, aminoalkyl, alkoxycarbonylalkyl, alkylsulfanylalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, haloalkylsulfanylalkyl, haloalkylsulfinylalkyl, haloalkylsulfonylalkyl, alkoxyalkylsulfanylalkyl, alkoxyalkylsulfinylalkyl, alkoxyalkylsulfonylalkyl, phenylalkyl, phenoxyalkyl, phenylsulfanylalkyl, phenylsulfinylalkyl, phenylsulfonylalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkoxycarbonyl, aryloxycarbonyl, arylcarbamoyl, where the aforementioned radicals may each be saturated or unsaturated and/or optionally substituted; or', 'represents optionally substituted saturated or unsaturated cycloalkyl which may optionally be interrupted by one or more heteroatoms; or', 'represents haloalkylcarbonyl, hydroxyalkylcarbonyl, alkoxyalkylcarbonyl, phenylcarbonyl, hetarylcarbonyl, haloalkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, cycloalkylaminocarbonyl, dicycloalkylaminocarbonyl, cycloalkyl(alkyl)aminocarbonyl, arylaminocarbonyl, diarylaminocarbonyl, alkyl(aryl)aminocarbonyl, cycloalkyl(aryl)aminocarbonyl, alkylaminothiocarbonyl, dialkylaminothiocarbonyl or aminothiocarbonyl, where the aforementioned radicals may each be saturated ...

Подробнее
02-05-2019 дата публикации

AMINOBENZOIC ACID DERIVATIVES FOR USE AS ANTI-INFLAMMATORY AGENTS, ANTI-METASTATIC AGENTS AND/OR ANTICANCER AGENTS

Номер: US20190127325A1
Принадлежит:

There are provided compounds of formula (I) in which R, R, R, Rand Q can represent various different possibilities. These compounds can be useful as anticancer agents as well as anti-inflammatory agents, anti-proliferative agents and/or anti-metastatic agents. 3. The compound of claim 2 , wherein{'sub': '2', 'Ris H, unsubstituted member chosen from acetyl and propiolyl;'}{'sub': 'A', 'Q is Q;'}{'sub': '5', 'Ris H, unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': '6', 'Ris Boc, H, or an unsubstituted member chosen from acetyl and propiolyl.'}5. The compound of claim 4 , wherein{'sub': '2', 'Ris H, unsubstituted member chosen from acetyl and propiolyl;'}{'sub': 'A', 'Q is Q;'}{'sub': '5', 'Ris H, unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': '6', 'Ris Boc, H, or an unsubstituted member chosen from acetyl and propiolyl.'}7. The compound of claim 6 , wherein{'sub': '2', 'Ris H, unsubstituted member chosen from acetyl and propiolyl;'}{'sub': 'A', 'Q is Q;'}{'sub': '5', 'Ris H, unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': '6', 'Ris Boc, H, or an unsubstituted member chosen from acetyl and propiolyl.'}9. The compound of claim 8 , wherein{'sub': '2', 'Ris H or unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': 7', '1', '8', '3', '6, 'Ris an unsubstituted member chosen from C-Calkyl, C-Ccycloalkyl, phenyl, furanyl, thiophenyl, pyridinyl, naphthyl, quinolyl and isoquinolyl.'}11. The compound of claim 10 , wherein{'sub': '2', 'Ris H or an unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': 7', '1', '8', '3', '6, 'Ris an unsubstituted member chosen from C-Calkyl, C-Ccycloalkyl, phenyl, furanyl, thiophenyl, pyridinyl, naphthyl, quinolyl and isoquinolyl.'}1535-. (canceled)36. A method for treating cancer or at least one cancer chosen from melanoma claim 1 , breast cancer claim 1 , uterine cancer claim 1 , ovarian cancer claim 1 , prostate cancer and bladder cancer claim 1 , said ...

Подробнее
19-05-2016 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20160137660A1
Принадлежит:

The present invention provides compounds of formula (I), 2. The compound of claim 1 , wherein Ris methyl.3. The compound according to claim 1 , wherein Lis substituted or unsubstituted C-Calkyl linker.4. The compound according to claim 1 , wherein Ris substituted or unsubstituted C-Calkyl and Ris H.5. The compound according to claim 1 , wherein Rand R claim 1 , together with the nitrogen atom to which they are attached claim 1 , form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N claim 1 , O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N claim 1 , O and S.10. A method of treating a neurological disease by administering to a subject in need thereof a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt claim 1 , polymorph claim 1 , hydrate claim 1 , solvate or co-crystal thereof.11. The method of claim 10 , wherein the neurological disease is multiple sclerosis.12. The method of claim 10 , wherein the neurological disease is relapsing-remitting multiple sclerosis.13. The method of claim 1 , wherein the compound of formula (I) is a pharmaceutically acceptable salt.14. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) a therapeutically effective amount of a compound of ;'}and(ii) a pharmaceutically acceptable carrier or excipient.15. The composition of claim 14 , wherein the therapeutically effective amount is sufficient for the treatment of multiple sclerosis.16. (canceled) This application is a continuation of U.S. application Ser. No. 14/180,687, filed Feb. 14, 2014 which claims the benefit of U.S. Provisional Application No. 61/782,445, filed on Mar. 14, 2013. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to various prodrugs of monomethyl fumarate. In ...

Подробнее
17-05-2018 дата публикации

BISMALEIMIDE RESINS FOR ONE DROP FILL SEALANT APPLICATION

Номер: US20180134657A1
Принадлежит:

The present invention relates to curable novel bismaleimide resins and prepolymers, methods of manufacture. Particularly useful applications include one drop fill sealant used in liquid crystal assembly. In particular, the inventive polymers and compositions are useful in the assembly of LCD panels. The present invention relates to monomers and oligomers useful as sealants and particularly as one drop fill sealants for liquid crystal applications. In particular, the present invention permits assembly of LCD panels without migration of the sealant resin into the liquid crystal or vice versa during LCD assembly and/or curing of the resin.The one drop fill (“ODF”) process is becoming the mainstream process in the assembly of LCD panels in display applications, replacing the conventional vacuum injection technology to meet faster manufacturing process demands. In the ODF process, first, a sealant is dispensed on an electrode-equipped substrate to form a frame of a display element, and liquid crystals are dropped inside the depicted frame. In the next step of the assembly, another electrode equipped substrate is joined thereto under vacuum. Then, the sealant undergoes a curing process, either by a combination of UV and thermal or by thermal only process.The ODF method has a few problems in that the sealant material in the uncured state comes into contact with the liquid crystal during the assembly process. This could cause reduction in electro-optical properties of the liquid crystal by resin migration into the liquid crystal or vice versa, or because of ionic impurities that may be present. Hence, design of resin systems for sealant material that show good liquid crystal resistance (less contamination) along with good adhesion and moisture barrier properties has remained a challenge.The present invention relates to unique resins and ODF compositions made therefrom.In one aspect of the invention there is provided a resin comprising the structure I:In another aspect of ...

Подробнее
30-04-2020 дата публикации

ALKENYL SUCCINIMIDES AND USE AS NATURAL GAS HYDRATE INHIBITORS

Номер: US20200131429A1
Принадлежит:

Disclosed are succinimide-based compounds used in compositions and methods for inhibiting natural gas hydrate agglomerates. The succinimide-based compounds are reaction products of an alkenyl succinic anhydride and an amine or amine alcohol. 1. A composition comprising at least one succinimide-based compound to inhibit formation of natural gas hydrate agglomerates , the at least one succinimide-based compound formed by a reaction between an alkenyl succinic anhydride with an amine or amine alcohol.2. The composition of claim 1 , wherein the amine comprises primary claim 1 , secondary or tertiary amine.3. The composition of claim 1 , wherein the amine is a dibutylaminopropylenediamine claim 1 , a dibutylaminopropylenediamine with an additional aminopropylamino moiety claim 1 , or combination thereof.4. The composition of claim 1 , wherein succinimide-based compounds is from about 1 wt/v % to about 80 wt/v % based on the composition.5. The composition of claim 1 , wherein the composition further comprises one or more thermodynamic gas hydrate inhibitors claim 1 , kinetic gas hydrate inhibitors claim 1 , anti-agglomerants claim 1 , asphaltene inhibitors claim 1 , paraffin inhibitors claim 1 , scale inhibitors claim 1 , emulsifiers claim 1 , water clarifiers claim 1 , dispersants claim 1 , emulsion breakers claim 1 , or any combination thereof.6. A composition comprising:a fluid; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the at least one succinimide-based compounds of .'}7. The composition of claim 1 , wherein the succinimide-based compounds are about is about 1000 ppm to 50 claim 1 ,000 ppm.8. The composition of claim 1 , wherein the fluid comprises water claim 1 , natural gas claim 1 , and liquid hydrocarbon.10. A method of inhibiting formation of agglomerates of natural gas hydrates comprising:introducing into a fluid a composition comprising at least one succinimide-based compound to inhibit formation of agglomerates of natural gas hydrates, the at least ...

Подробнее
08-09-2022 дата публикации

RESIST UNDERLAYER FILM-FORMING COMPOSITION

Номер: US20220283501A1
Принадлежит: NISSAN CHEMICAL CORPORATION

A resist underlayer film forming composition contains a reaction product of an aromatic compound (A) having 6 to 60 carbon atoms and a compound represented by formula (B), and a solvent. (In the formula, X represent an oxygen atom or a nitrogen atom; Y represents a single bond, an oxygen atom or a nitrogen atom; X and Y may combine with each other to form a ring; and each of R, R, Rand Rindependently represents a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, a cyclic alkyl group having 3 to 8 carbon atoms or an aromatic group having 6 to 10 carbon atoms; provided that Ris present only in cases where X is a nitrogen atom, and Ris present only in cases where Y is a nitrogen atom.) 2. The resist underlayer film-forming composition according to claim 1 , wherein X and Y in formula (B) are each an oxygen atom or a nitrogen atom.4. The resist underlayer film-forming composition according to claim 1 , wherein the aromatic compound (A) comprises one or more benzene rings claim 1 , one or more naphthalene rings claim 1 , one or more anthracene rings claim 1 , one or more pyrene rings claim 1 , or a combination thereof.5. The resist underlayer film-forming composition according to claim 1 , wherein the aromatic compound (A) comprises two or more benzene rings claim 1 , two or more naphthalene rings claim 1 , two or more anthracene rings claim 1 , two or more pyrene rings claim 1 , or a combination thereof.6. The resist underlayer film-forming composition according to claim 1 , further comprising a crosslinking agent.7. The resist underlayer film-forming composition according to claim 1 , further comprising an acid and/or an acid generator.8. The resist underlayer film-forming composition according to claim 1 , wherein the solvent has a boiling point of 160° C. or higher.9. A resist underlayer film claim 1 , which is a baked product of a coating film comprising the resist underlayer film-forming composition according to .10. A method for manufacturing a ...

Подробнее
24-05-2018 дата публикации

SULPHAMOYLPYRROLAMIDE DERIVATIVES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Номер: US20180141905A1
Принадлежит:

Inhibitors of HBV replication of Formula (ID) 115-. (canceled)17. The method of claim 16 , wherein{'sup': 'a', 'Ris —CN;'}{'sup': b', 'c', 'd, 'R, Rand Rare each independently selected from the group consisting of hydrogen and fluoro;'}{'sup': '4', 'sub': 1', '3, 'Ris C-Calkyl;'}{'sup': '6', 'sub': 2', '6, 'Ris selected from the group consisting of C-Calkyl, optionally substituted with one or more fluoro; and'}{'sup': '7', 'Ris hydrogen.'}18. The method of claim 16 , wherein the compound is selected from the group consisting of:N-(4-fluoro-3-methyl-phenyl)-4-(isopropylsulfamoyl)-1H-pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-(isopropylsulfamoyl)-1-methyl-pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-[[(1R)-2-hydroxy-1-methyl-ethyl]sulfamoyl]-1-methyl-pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[(3-methyloxetan-3-yl)sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[[(1R)-1-methylpropyl]sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[(3-methyloxetan-3-yl)methylsulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[[(1S)-2,2,2-trifluoro-1-methyl-ethyl]sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[[(1R)-2,2,2-trifluoro-1-methyl-ethyl]sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-[[3-(hydroxymethyl)oxetan-3-yl]sulfamoyl]-1-methyl-pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[(3-methyltetrahydrofuran-3-yl)sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-[[1-(hydroxymethyl)cyclopropyl]sulfamoyl]-1-methyl-pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-1-methyl-4-[(1-methyl-5-oxo-pyrrolidin-3-yl)sulfamoyl]pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-[[3-(2-hydroxyethyl)oxetan-3-yl]sulfamoyl]-1-methyl-pyrrole-2-carboxamide;N-(4-fluoro-3-methyl-phenyl)-4-[(3-hydroxycyclobutyl)sulfamoyl]-1-methyl ...

Подробнее
02-06-2016 дата публикации

Quaternary ammonium compounds as fuel or lubricant additives

Номер: US20160152910A1
Принадлежит: Innospec Ltd

A quaternary ammonium compound which is the reaction product of: (a) a tertiary amine having a molecular weight of less than 1000; (b) an acid-activated alkylating agent; and (c) a diacid including an optionally substituted hydrocarbyl moiety having at least (5) carbon atoms.

Подробнее
17-06-2021 дата публикации

Synergistic Blends Of Anti-Agglomerant Gas Hydrate Inhibitors With Quaternary Alkyl Ammonium Compounds

Номер: US20210179916A1
Принадлежит: Clariant International, Ltd.

The present disclosure relates to a gas hydrate inhibitor composition comprising from an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1) 1. A gas hydrate inhibitor composition comprising [{'br': None, 'sup': 5', '1', '2', '3', '+', '−, '[R-L-N(R)(R)(R)]X\u2003\u2003(1)'}, 'wherein', {'sup': 1', '2', '1', '2, 'each of Rand Ris independently an alkyl group having from 1 to 5 carbon atoms; or wherein the nitrogen atom and the Rand Rgroups together form a substituted or unsubstituted heterocyclic group;'}, {'sup': '3', 'Ris present or not as hydrogen or an alkyl group having from 1 to 8 carbon atoms which optionally bears a hydroxy group or a carboxy group in the 2-position;'}, 'L is a linking moiety comprising an optionally substituted hydrocarbyl group having at least 2 adjacent carbon atoms, at least one heteroatom selected from nitrogen and oxygen, and optionally one or more further heteroatoms;', {'sup': '5', 'Ris a hydrocarbyl group having from 6 to 22 carbon atoms; and'}, {'sup': −', '3, 'X is present as an anion when Ris present; and'}], 'A) from 5 to 95 weight-% of an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1)'}{'sub': 8', '18, 'B) from 5 to 95 weight-% of a cationic surfactant which is selected from di(C-Calkyl)dimethyl ammonium salts.'}2. The gas hydrate inhibitor composition according to claim 1 , wherein Rand Rindependently are alkyl groups having from 3 to 5 carbon atoms.3. The gas hydrate inhibitor composition according to wherein Ris an alkyl or alkenyl group having between 8 and 20 carbon atoms.4. The gas hydrate inhibitor composition according to claim 1 , wherein Ris present as hydrogen or as a methyl group.5. The gas hydrate inhibitor according to claim 1 , wherein X is selected from the group consisting of hydroxide claim 1 , carboxylate claim 1 , halide claim 1 , ...

Подробнее
17-06-2021 дата публикации

Synergistic Blends Of Anti-Agglomerant Gas Hydrate Inhibitors With Alkoxylates Of Fatty Alcohols, Fatty Amines And Fatty Acids

Номер: US20210179920A1
Принадлежит: Clariant International, Ltd.

The present disclosure relates to a gas hydrate inhibitor composition comprising an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1) 1. A gas hydrate inhibitor composition comprising [{'br': None, 'sup': 5', '1', '2', '3', 'q+', '−, 'sub': 'q', '[R-L-N(R)(R)(R)][X]\u2003\u2003(1)'}, 'wherein', {'sup': 1', '2', '1', '2, 'each of Rand Ris independently an alkyl group having from 1 to 5 carbon atoms; or wherein the nitrogen atom and the Rand Rgroups together form a substituted or unsubstituted heterocyclic group;'}, {'sup': '3', 'Ris present or not as hydrogen or an alkyl group having from 1 to 8 carbon atoms which optionally bears a hydroxy group in the 2-position;'}, 'L is a linking moiety comprising an optionally substituted hydrocarbyl group having at least 2 adjacent carbon atoms, at least one heteroatom selected from nitrogen and oxygen, and optionally one or more further heteroatoms;', {'sup': '5', 'Ris a hydrocarbyl group having from 6 to 22 carbon atoms;'}, {'sup': −', '3, 'X is present as an anion when Ris present;'}, 'q is 0 or an integer from 1 to 7; and, 'A) from 5 to 95 weight-% of an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1)'}{'sub': 8', '18', '8', '18', '8', '18', '8', '18, 'B) from 5 to 95 weight-% of a nonionic surfactant which is selected from alkoxylated C-Cfatty alcohols, alkoxylated C-Cfatty amines, alkoxylated C-Cfatty acids and alkoxylated C-Cfatty acid amides.'}2. The gas hydrate inhibitor composition according to claim 1 , wherein Rand Rindependently are alkyl groups having from 3 to 5 carbon atoms claim 1 , more preferably 4 or 5 and most preferably 4 carbon atoms.3. The gas hydrate inhibitor composition according to claim 1 , wherein Ris an alkyl or alkenyl group having from 8 to 20 carbon atoms.4. The gas hydrate inhibitor composition according to claim 1 , ...

Подробнее
09-06-2016 дата публикации

QUATERNARY AMMONIUM COMPOUNDS AS FUEL OR LUBRICANT ADDITIVES

Номер: US20160160142A1
Принадлежит: INNOSPEC LIMITED

A quaternary ammonium compound of formula (X), wherein R, R, Rand Ris each individually an optionally substituted alkyl, alkenyl or aryl group and R includes an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms. 2. A quaternary ammonium compound which is the reaction product of:(a) a tertiary amine;(b) an acid-activated alkylating agent; and(c) an acid including an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms.3. A quaternary ammonium compound according to wherein component (b) is an epoxide.4. A quaternary ammonium compound according to wherein component (c) is selected from a monoacid claim 2 , diacid claim 2 , monoester of a diacid claim 2 , a polyacid or a partial ester of a polyacid.5. A quaternary ammonium compound according to wherein component (c) is selected from a monoacid claim 4 , diacid or a monoester of a diacid.7. A quaternary ammonium compound according to wherein component (c) is a monoester of a diacid.10. A method of preparing a quaternary ammonium salt claim 6 , the method comprising reacting (a) a tertiary amine with (b) an acid-derived alkylating agent in the presence of (c) acid including an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms.11. An additive composition comprising one or more quaternary ammonium compounds as claimed in and a diluent or carrier.12. A lubricating composition comprising as an additive one or more quaternary ammonium compounds as claimed in .13. A fuel composition comprising as an additive one or more quaternary ammonium compounds as claimed in .14. A fuel composition according to wherein the fuel is diesel fuel.15. A fuel composition according to which comprises one or more further detergents selected from:(i) an additional quaternary ammonium salt additive which is not one of the one or more quaternary ammonium compounds;(ii) the product of a Mannich reaction between an aldehyde, an amine and an optionally substituted phenol;(iii) the ...

Подробнее
08-06-2017 дата публикации

Conjugates of cell binding molecules with cytotoxic agents

Номер: US20170157262A1
Принадлежит: Hangzhou Dac Biotech Co Ltd

A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a formula (I), wherein T, L, m, n, Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 12 , and R 13 are defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.

Подробнее
08-06-2017 дата публикации

Process for the Preparation of 2-Alkoxymethyl-1,4-Benzenediamines

Номер: US20170158608A1
Принадлежит:

A process for synthesizing 2-methoxymethyl-1,4-benzenediamine (V-a), its derivatives of formula (V) and the salts thereof, which comprises a radical halogenation step of formula (II). The final product can be 2-methoxymethyl-1,4-benzenediamine of formula (IV-a). 6. The process according to claim 4 , wherein the amine protection step a) claim 4 , radical halogenation step b) claim 4 , alkylating step c) and deprotection step d) are performed successively. A process to synthesize 2-alkoxymethyl-1,4-benzenediamines (V), its derivatives, and salts thereof, comprising the protection of sensitive amine functionalities, radical halogenation mediated by halogenating agents, and alkoxylation. These compounds may be used as couplers and/or primary intermediates in compositions for dyeing keratin fibers.CA 2,576,189 discloses the application of combinations of 2-methoxymethyl-1,4-benzenediamine (V-a) with various couplers and primary intermediates in oxidative dyeing compositions. U.S. Pat. No. 2,273,564 discloses a process to synthesize substituted 1,4-benzenediamine compounds with a substituent on the 2 position. U.S. Pat. No. 6,648,923 B1 discloses a process to synthesize 2-methoxymethyl-1,4-benzenediamine and the salts thereof.The previous syntheses described above to reach 2-alkoxymethyl-1,4-benzenediamines, their derivatives, and salts thereof are not completely satisfactory.Therefore, there is a need for a simple, industrially applicable, efficient, not expensive and high yield process to synthesize 2-alkoxymethyl-1,4-benzenediamines, their derivatives of formula (V), and salts thereof.The key step of the process of this invention is a radical halogenation of the N-protected- or the N,N′diprotected-2-methyl-1,4-benzenediamine derivatives of formula (II) as key intermediates.A new process has now been developed to synthesize 2-alkoxymethyl-1,4-benzenediamines (V), its derivatives, and salts thereof, which permits a production of said compounds in a novel, high yield, ...

Подробнее
04-09-2014 дата публикации

Process for Preparing 5-biphenyl-4-amino-2-methyl Pentanoic Acid

Номер: US20140249320A1
Принадлежит:

The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, 3. A compound according to wherein the compound according to formula (2) claim 1 , or tautomer claim 1 , or salt thereof claim 1 , is in crystalline form.4. A compound according to wherein the compound according to formula (2-a) claim 2 , or tautomer claim 2 , or salt thereof claim 2 , is in crystalline form.5. A compound according to claim 1 , wherein in the compound of formula (2-a) R1 is hydrogen or a nitrogen protecting group selected from pivaloyl and t-butyloxycarbonyl (BOC).13. A process according to claim 6 , wherein R1 and R2 are hydrogen and R3 is an ethyl group. This application is a Divisional application of Ser. No. 13/333,437, filed Dec. 21, 2011, which is a Divisional application of Ser. No. 12/522,767, filed Jul. 10, 2009, which is a National Phase Application of PCT/EP2008/000142, filed Jan. 10, 2008, which claims benefit of EP 07/100,451.9, filed Jan. 10, 2008.The present invention relates to pyrrolidin-2-ones according to formula (1), or salts thereof,wherein R1 is hydrogen or a nitrogen protecting group, as defined herein, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester, or salt thereof.Endogenous atrial natriuretic peptides (ANP), also called atrial natriuretic factors (ANF), have diuretic, natriuretic and vasorelaxant functions in mammals. The natural ANF peptides are metabolically inactivated, in particular by a degrading enzyme which has been recognized to correspond to the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), which is also responsible for e.g. the metabolic inactivation of enkephalins.In the art biaryl substituted phosphonic acid derivatives are known which are useful as neutral endopeptidase (NEP) inhibitors, e.g. as inhibitors of the ANF-degrading enzyme in ...

Подробнее
15-06-2017 дата публикации

CONTINUOUS HIGH SHEAR REACTOR MELT PROCESSING METHODS TO SYNTHESIZE HETEROCYCLIC MONOMERS AND COMPOSITIONS THEREOF

Номер: US20170166537A1
Принадлежит:

The invention provides novel methods of synthesizing new monofunctional and/or multifunctional heterocyclic monomers and the formulation of new alloys of said monomers from base reactants via a continuous solvent-free, or alternatively in-solvent, one-step high shear reactor methodology designed to reduce the minor isomer formation and to eliminate the need for post-processing purification, as well as the ability to disperse reinforcements and additives while synthesizing such heterocyclic monomers and monomer alloys created and to the synthesis of related compositions. 5. A method to melt synthesize a monofunctional benzoxazine monomer , maleimide monomer , or both , from a known variant of at least one base reactant , the method comprising:utilizing in a reactor at least one base reactant from a batch of pre-blended reactants for the synthesis, wherein the at least one base reactant is a phenol, amine, paraformaldehyde, or a combination thereof, andforming the monofunctional benzoxazine monomer, maleimide monomer, or both, using a continuous, high shear reactor at a processing temperature of from about 90° C. to about 200° C. and a residence time of about 30 to about 60 seconds for benzoxazines and about 160° C. to about 300° C. and a residence time of about 90 seconds for maleimides,wherein the monofunctional benzoxazine monomer, maleimide monomer, or both, is a room temperature solid.6. The method of claim 5 , wherein the at least one base reactant is fed to the reactor independently from at least one other base reactant.7. The method of claim 6 , wherein the monofunctional benzoxazine monomer claim 6 , maleimide monomer claim 6 , or both claim 6 , is a room temperature liquid.8. The method of claim 5 , further comprising melt synthesizing the major isomer of the monofunctional benzoxazine monomer claim 5 , maleimide monomer claim 5 , or both claim 5 , wherein the monomer is a room temperature solid claim 5 , and minimizing the formation of any minor isomer.9. ...

Подробнее
18-09-2014 дата публикации

FUNCTIONALIZED POLYMERS CONTAINING POLYAMINE SUCCINIMIDE FOR ANTIFOULING IN HYDROCARBON REFINING PROCESSES

Номер: US20140262953A1

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon. 2. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises polypropylene.3. The compound of claim 2 , wherein the polypropylene is selected from the group consisting of atactic polypropylene claim 2 , isotactic polypropylene claim 2 , syndiotactic polypropylene claim 2 , amorphous polypropylene claim 2 , polypropylene including isotactic crystallizable units claim 2 , polypropylene including syndiotactic crystallizable units claim 2 , and polypropylene including meso diads constituting from about 30% to about 99.5% of the total diads of the polypropylene.4. The compound of claim 2 , wherein at least one of R claim 2 , R claim 2 , and Rhas a number-averaged molecular weight of from about 300 to about 30000 g/mol.5. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises polyethylene.6. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises poly(ethylene-co-propylene).7. The compound of claim 6 , wherein at least one of R claim 6 , R claim 6 , and Rcomprises from about 1 mole % to about 90 mole % of ethylene units and from about 99 mole % to about 10 mole % propylene units.8. The compound of claim 7 , wherein at least one of R claim 7 , R claim 7 , and Rcomprises from about 10 mole % to about 50 mole % of ethylene units.9. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises poly(higher alpha-olefin) claim 1 , the higher alpha-olefin including two or more carbon atoms on each side chain.10. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises polypropylene-co-higher alpha- ...

Подробнее
04-06-2020 дата публикации

Conjugates of cell binding molecules with cytotoxic agents

Номер: US20200172480A1
Принадлежит: Hangzhou Dac Biotech Co Ltd

A conjugate of a potent cytotoxic agent with a cell-binding molecule having a structure represented by Formula (I), wherein T, L, m, n, , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , and R 13 are as defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.

Подробнее
18-09-2014 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20140275048A1
Принадлежит: ALKERMES PHARMA IRELAND LIMITED

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 2. The compound of claim 1 , wherein Ris methyl.3. The compound according to claim 1 , wherein Lis an unsubstituted C-Calkyl linker.4. The compound according to claim 1 , wherein Rand Rtogether with the nitrogen to which they are attached form a heterocycle claim 1 , wherein the heterocycle is a morpholine ring claim 1 , a thiomorpholine ring claim 1 , a pyrrolidine ring claim 1 , a 2 claim 1 ,5-dihydropyrrole ring claim 1 , a 1 claim 1 ,2-dihydropyridine ring claim 1 , a piperazine ring claim 1 , a succinimide ring claim 1 , an isoindoline ring claim 1 , a 2 claim 1 ,5-dihydro-1H-tetrazole ring claim 1 , an azetidine ring claim 1 , a piperidine ring claim 1 , a hexahydropyrimidine ring claim 1 , a 2 claim 1 ,3 claim 1 ,3a claim 1 ,4 claim 1 ,7 claim 1 ,7a-hexahydro-1H-4 claim 1 ,7-epoxyisoindole ring claim 1 , a 3 claim 1 ,4-dihydroquinazoline ring claim 1 , a 1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroquinazoline ring claim 1 , an oxazolidine ring claim 1 , an oxazolidinone ring claim 1 , an imidazolidinone ring claim 1 , a 1 claim 1 ,3-dihydro-2H-imidazol-2-one ring claim 1 , an imidizolidine thione ring claim 1 , or an isothiazolidine ring claim 1 , wherein all of the rings may be optionally substituted one or more times with C-Calkyl claim 1 , CO(C-Calkyl) claim 1 , OH claim 1 , (CH)OH claim 1 , O(C-Calkyl) claim 1 , halo claim 1 , NH claim 1 , (CH)NH claim 1 , (CH)NH(C-Calkyl) claim 1 , (CH)N(C-Calkyl) claim 1 , carbonyl claim 1 , or thione.5. The compound according to claim 1 , wherein Rand R claim 1 , together with the nitrogen atom to which they are attached claim 1 , form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N claim 1 , O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N claim 1 , O and S.11. The ...

Подробнее
18-09-2014 дата публикации

Prodrugs of fumarates and their use in treating various diseases

Номер: US20140275205A1
Принадлежит: Alkermes Pharma Ireland Ltd

The present invention provides compounds of formula (I), wherein: R 1 is unsubstituted C 1 -C 6 alkyl; L a is substituted or unsubstituted C 1 -C 6 alkyl linker, substituted or unsubstituted C 3 -C 10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R 2 and R 3 are each, independently, H, substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 6 -C 10 aryl; or alternatively, R 2 and R 3 , together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

Подробнее
05-07-2018 дата публикации

HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20180186737A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 4. (canceled)7. (canceled)11. (canceled)12. The compound of claim 1 , wherein Lis —S(O)NR— wherein the sulfur is attached to L.14. (canceled)15. (canceled)16. (canceled)17. (canceled)19. (canceled)20. (canceled)21. A compound selected from Table 1 or Table 2.22. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient or carrier.23. A method ofa. one or more of inhibiting dUTPase or enhancing the efficacy of a dUTPase directed therapy, orb. reversing resistance to a dUTPase-directed therapy{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'comprising contacting the dUTPase with a therapeutically effective amount of the compound of .'}24. (canceled)25. A method of treating a disease in a patient whose treatment is impeded by the expression or over expression of dUTPase claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. administering to the patient in need of such treatment a therapeutically effective amount of the compound of ; or'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'b. screening a cell or tissue sample from the patient determining the expression level of dUTPase in the sample; and administering to a patient whose sample shows over expression of dUTPase, a therapeutically effective amount of the compound of .'}26. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of and a therapeutically effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.27. The method of claim 26 , wherein the cancer cell is selected from a colon cancer cell claim 26 , a colorectal cancer cell claim 26 , a gastric cancer cell claim 26 , a head and neck cancer cell claim 26 , a breast cancer cell claim 26 , a lung cancer cell or a blood cell ...

Подробнее
12-07-2018 дата публикации

HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20180194736A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 9. The compound of claim 1 , wherein Lis —S(O)NR— wherein the sulfur is attached to L.12. A compound selected from Table 1 or Table 2.13. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient or carrier.15. A method of treating a disease in a patient whose treatment is impeded by the expression or over expression of dUTPase claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. administering to the patient in need of such treatment a therapeutically effective amount of the compound of ; or'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'b. screening a cell or tissue sample from the patient; determining the expression level of dUTPase in the sample; and administering to a patient whose sample shows over expression of dUTPase, a therapeutically effective amount of the compound of .'}16. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of and a therapeutically effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.17. The method of claim 16 , wherein the cancer cell is selected from a colon cancer cell claim 16 , a colorectal cancer cell claim 16 , a gastric cancer cell claim 16 , a head and neck cancer cell claim 16 , a breast cancer cell claim 16 , a lung cancer cell or a blood cell.18. The method of claim 15 , wherein the disease is cancer.19. The method of claim 18 , wherein the cancer is selected from the group consisting of colon cancer claim 18 , colorectal cancer claim 18 , gastric cancer claim 18 , esophageal cancer claim 18 , head and neck cancer claim 18 , breast cancer claim 18 , lung cancer claim 18 , stomach cancer claim 18 , liver cancer claim 18 , gall bladder cancer claim 18 , pancreatic cancer and leukemia. ...

Подробнее
12-07-2018 дата публикации

Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage

Номер: US20180194740A1

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Подробнее
25-09-2014 дата публикации

CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

Номер: US20140288106A1
Принадлежит: SANOFI

The present invention relates to compounds of formula 1 3. A compound according to claim 1 , wherein R represents hydrogen.7. A compound according to claim 1 , wherein X represents —O—CH— claim 1 , —S—CH— or —CH—CH—.8. A compound according to claim 1 , wherein Y represents hydrogen claim 1 , Cl claim 1 , F claim 1 , methyl claim 1 , ethyl claim 1 , methoxy or —CH—OH.9. A compound according to claim 8 , wherein Y represents ethyl or methoxy.11. A compound according to claim 10 , wherein Z represents —(CH)— or —CH—N(CH)—.13. A compound according to selected from the group consisting oftrans-4-[([1-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid ethyl ester;trans-4-[([1-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]{4-[2-(2,5-dioxo-pyrrolidin-1-yl)ethoxy]-3-methoxybenzyl}amino)methyl]-cyclohexanecarboxylic acid;cis-4-[([1-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]{4-[2-(2,5-dioxo-pyrrolidin-1-yl)ethoxy]-3-methoxybenzyl}amino)methyl]-cyclohexanecarboxylic acid;trans-4-[([(R)-1-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(S)-1-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(S)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]cyclohexanecarboxylic acid;trans-4-[([(R)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(S)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methyl-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;cis-4-[([(S)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methyl-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(R)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin ...

Подробнее
18-06-2020 дата публикации

SUBSTITUTED SUCCINIMIDE DERIVATIVES AS PESTICIDES

Номер: US20200190073A1
Принадлежит: BASF SE

The invention relates to succinimide compounds of formula I 117-: (canceled)24: The compound of claim 18 , wherein Ris halomethyl.25: The compound of claim 18 , wherein Ris halogen claim 18 , NO claim 18 , CN claim 18 , CH claim 18 , fluoromethyl claim 18 , CF claim 18 , SCH claim 18 , or OCH claim 18 , and Ris H.26: The compound of claim 18 , wherein Ris H claim 18 , C-C-alkyl claim 18 , C-C-cycloalkyl claim 18 , C-C-alkenyl claim 18 , or C-C-alkynyl.27: The compound of claim 18 , wherein Ris C-C-alkyl which is unsubstituted or substituted with phenyl or C(═O)—C-C-alkoxy; or Ris C-C-alkyl claim 18 , C-C-haloalkyl claim 18 , C-C-cycloalkyl claim 18 , C-C-alkoxy claim 18 , C-C-haloalkoxy claim 18 , C-C-alkylamino claim 18 , and di-C-C-alkylamino.28: An agricultural or veterinary composition comprising at least one compound according to and/or at least one agriculturally or veterinarily acceptable salt thereof claim 18 , and at least one inert liquid and/or solid agriculturally or veterinarily acceptable carrier.29: An agricultural composition for combating animal pests comprising at least one compound as defined in and at least one inert liquid and/or solid acceptable carrier and claim 18 , if desired claim 18 , at least one surfactant.30: The composition according to claim 28 , comprising additionally a further active substance.31: A method for combating or controlling invertebrate pests claim 18 , which method comprises contacting said pest or its food supply claim 18 , habitat or breeding grounds with a pesticidally effective amount of at least one compound as defined in .32: A method for protecting growing plants from attack or infestation by invertebrate pests claim 18 , which method comprises contacting a plant claim 18 , or soil or water in which the plant is growing claim 18 , with a pesticidally effective amount of at least one compound as defined in .33: Seed treated with a compound as defined in claim 18 , or the enantiomers claim 18 , diastereomers or ...

Подробнее
19-07-2018 дата публикации

DEOXYURIDINE TRIPHOSPHATASE INHIBITORS CONTAINING CYCLOPROPANO LINKAGE

Номер: US20180201586A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 4. (canceled)6. (canceled)11. (canceled)12. The compound of claim 1 , wherein Lis —S(O)NH— wherein the sulfur is attached to L.13. (canceled)14. (canceled)15. (canceled)17. (canceled)19. A compound selected from Table 1.20. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient.22. (canceled)23. A method of treating a disease in a patient whose treatment is impeded by the expression or over expression of dUTPase claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. administering to the patient in need of such treatment a therapeutically effective amount of the compound of ; or'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'b. screening a cell or tissue sample from the patient determining the expression level of dUTPase in the sample; and administering to a patient whose sample shows over expression of dUTPase, a therapeutically effective amount of the compound of .'}24. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of claim 1 , and an effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.25. The method of claim 24 , wherein the cancer cell is selected from a colon cancer cell claim 24 , a colorectal cancer cell claim 24 , a gastric cancer cell claim 24 , a head and neck cancer cell claim 24 , a breast cancer cell claim 24 , a lung cancer cell or a blood cell.26. (canceled)27. The method of claim 23 , wherein the disease is cancer.28. The method of claim 27 , wherein the cancer is selected from the group consisting of colon cancer claim 27 , colorectal cancer claim 27 , gastric cancer claim 27 , esophageal cancer claim 27 , head and neck cancer claim 27 , breast cancer claim 27 , lung cancer claim 27 , stomach cancer ...

Подробнее
04-07-2019 дата публикации

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

Номер: US20190201367A1
Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 110-. (canceled)12. A pharmaceutical composition comprising the compound of claim 11 , or a pharmaceutically acceptable salt thereof.13. A method of treating multiple sclerosis in a subject in need thereof claim 11 , comprising administering to the subject a therapeutically effective amount of the compound of .14. A method of treating multiple sclerosis in a subject in need thereof claim 12 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including ...

Подробнее
02-08-2018 дата публикации

TREATMENT METHOD UTILIZING PYRROLIDINE-2, 5-DIONE DERIVATIVES AS IDO1 INHIBITORS

Номер: US20180214415A1
Принадлежит:

Uses of compound of Formula I: 2. The method according to claim 1 , wherein the brain cancer is selected from glioblastomas and medulloblastomas; the intraepithelial neoplasms is selected from Bowen's disease and Paget's disease; the oral cancer is squamous cell carcinoma; the ovarian cancer is selected from those arising from epithelial cells claim 1 , stromal cells claim 1 , germ cells and mesenchymal cells; the renal cancer is selected from adenocarcinoma and Wilms tumor; the sarcomas is selected from leiomyosarcoma claim 1 , rhabdomyosarcoma claim 1 , liposarcoma claim 1 , fibrosarcoma and osteosarcoma; the skin cancer is selected from melanoma claim 1 , Kaposi's sarcoma claim 1 , basocellular cancer and squamous cell cancer; the testicular cancer is selected from germinal tumors seminomas claim 1 , and non-seminomas selected from teratomas and choriocarcinomas; and the thyroid cancer is selected from thyroid adenocarcinoma and medullary carcinoma.3. The method according to claim 1 , wherein the lymphoid disorders are selected from acute lymphocytic leukemia and chronic lymphoproliferative disorders.4. The method according to claim 3 , wherein the chronic lymphoproliferative disorders are selected from lymphomas claim 3 , myelomas and chronic lymphoid leukemias.5. The method according to claim 4 , wherein the lymphomas are selected from Hodgkin's disease claim 4 , non-Hodgkin's lymphoma lymphomas claim 4 , and lymphocytic lymphomas; and the chronic lymphoid leukemias are selected from T cell chronic lymphoid leukemias and B cell chronic lymphoid leukemias.6. The method according to claim 1 , wherein Qrepresents H and X represents —NH—.7. The method according to claim 1 , wherein Rand Reach independently represent H or halo.8. The method according to claim 7 , wherein the halo is F.10. The method according to claim 9 , wherein the method comprises delivering approximately equal molar amounts of the compound of Formula I′ and the compound of Formula I″.11. The ...

Подробнее
11-08-2016 дата публикации

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Номер: US20160229819A1
Автор: Nguyen Mark Quang
Принадлежит:

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , tert-butyl claim 1 , phenyl claim 1 , benzyl claim 1 , (1 claim 1 ,3-dioxoisoindolin-2-yl) claim 1 , (2 claim 1 ,5-dioxopyrrolidin-1-yl) claim 1 , (2 claim 1 ,5-dioxopyrrol-1-yl) claim 1 , indol-1-yl claim 1 , morpholin-4-yl claim 1 , 1 claim 1 ,3-oxazinan-3-yl claim 1 , oxazolidin-3-yl claim 1 , (1-oxoisoindolin-2-yl) claim 1 , (2-oxomorpholin-4-yl) claim 1 , (4-oxo-1-piperidyl) claim 1 , (2-oxopyrrolidin-1-yl) claim 1 , (3-oxopyrrolidin-1-yl) claim 1 , 1-piperidyl claim 1 , tetrazol-1-yl claim 1 , triazol-1-yl claim 1 , 1 claim 1 ,2 claim 1 ,4-triazol-4-yl claim 1 , 1-benzoyloxyethyl claim 1 , benzoyloxymethyl claim 1 , (1 claim 1 ,3-dimethyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (1 claim 1 ,3-dimethyl-2-oxo-imidazolidin-4-yl) claim 1 , (2 claim 1 ,5-dioxoimidazolidin-4-yl) claim 1 , (2 claim 1 ,5-dioxopyrrolidin-3-yl) claim 1 , (1-methyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (3-methyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (1-methyl-2 claim 1 ,5-dioxo-pyrrolidin-3-yl) claim 1 , (5-methyl-2-oxo-1 claim 1 ,3-dioxol-4-yl)methyl claim 1 , (3-methyl-2-oxo-oxazolidin-4-yl) claim 1 , (3-methyl-2-oxo-oxazolidin-5-yl) claim 1 , (1-methyl-2-oxo-pyrrolidin-3-yl) claim 1 , (1-methyl-5-oxo-pyrrolidin-2-yl) claim 1 , (1-methyl-5-oxo-pyrrolidin-3-yl) claim 1 , 1-(2-methylpropanoyloxy)ethyl claim 1 , 2-methylpropanoyloxymethyl ...

Подробнее
26-08-2021 дата публикации

Linker, Antibody-Drug Conjugate Including Same and Use Thereof

Номер: US20210261505A1
Принадлежит:

Provided are a linker represented by Formula I or I′, an antibody-drug conjugate containing the same, and use of thereof, a pharmaceutical composition comprising the antibody-drug conjugate, and use of the antibody-drug conjugate for treating and/or preventing a disease. 711.-. (canceled)1518.-. (canceled)22. (canceled)26. A pharmaceutical composition claim 5 , which comprises at least one compound according to claim 5 , a salt or a solvate thereof claim 5 , and one or more pharmaceutically acceptable carriers or excipients.27. (canceled)28. A method for diagnosis claim 5 , prevention or treatment of a disease or condition or reducing a severity of the disease or condition claim 5 , the method comprising administering to a patient in need of such treatment an effective amount of the compound according to claim 5 , a salt or a solvate thereof claim 5 , wherein the disease or condition is selected from the group consisting of tumor claim 5 , infectious disease claim 5 , hematological disease claim 5 , metabolic disease and inflammation.29. (canceled)30. The compound according to claim 21 , a salt or a solvate thereof claim 21 , wherein MAB is selected from the group consisting of: anti-HER2 humanized monoclonal antibody mil40 claim 21 , trastuzumab (HERCEPTIN) claim 21 , pertuzumab (PERJETA) claim 21 , cetuximab (ERBITUX) claim 21 , panitumumab (VECTIBIX) claim 21 , rituximab (RITUXAN) claim 21 , alemtuzumab (CAMPATH) claim 21 , ibritumomab (ZEVALIN) claim 21 , tositumomab (BEXXAR) claim 21 , ofatumumab (ARZERRA) claim 21 , bevacizumab (AVASTIN) claim 21 , ipilimumab (YERVOY) claim 21 , denosumab (XGEVA) claim 21 , pembrolizumab (KEYTRUDA) claim 21 , nivolumab (Opdivo) claim 21 , Avelumab (Bavencio) claim 21 , Atezolizumab (Tecentriq) claim 21 , durvalumab (Imfinzi) claim 21 , sacituzumab claim 21 , rovalpituzumab claim 21 , and biological analogues thereof.31. The compound according to claim 5 , a salt or a solvate thereof claim 5 , wherein B is selected from the ...

Подробнее
10-09-2015 дата публикации

DIESEL DETERGENT WITHOUT A LOW MOLECULAR WEIGHT PENALTY

Номер: US20150252278A1
Принадлежит: THE LUBRIZOL CORPORATION

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 1. A composition comprising a quaternary ammonium salt , wherein the quaternary ammonium salt comprises the reaction product of: (i) at least one tertiary amino group, and', '(ii) a hydrocarbyl-substituent derived from a hydrocarbon having a number average molecular weight of from about 100 to about 500;, 'a) a compound comprising'}b) a quaternizing agent suitable for converting the tertiary amino group of compound (a) to a quaternary nitrogen.2. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group and at least one hydrocarbyl-substituent claim 1 , comprises:(I) the condensation product of an acylating agent substituted with the hydrocarbyl-substituent of a)ii) and a compound having an oxygen or nitrogen atom capable of condensing the acylating agent wherein the condensation product has at least one tertiary amino group;(II) an amine substituted with the hydrocarbyl-substituent of a)ii), wherein the amine has at least one tertiary amino group and the hydrocarbyl-substituent is a polyalkene-substituent;(III) a compound containing at least one hydrocarbyl-substituent of a)ii) and at least one tertiary amino group, wherein the hydrocarbyl-substituent is a polyester group;(IV) a compound containing at least one hydrocarbyl-substituent of a)ii) and at least one tertiary amino group, wherein the hydrocarbyl-substituent is a polyether group; or(V) any combination thereof.3. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group claim 1 , comprises the condensation product of a hydrocarbyl-substituted acylating agent and a compound having an oxygen or nitrogen atom capable of condensing with said ...

Подробнее
13-11-2014 дата публикации

METHODS FOR TREATING LEISHMANIASIS

Номер: US20140336187A1
Принадлежит:

Methods are provided to inhibit proliferation of parasites, and in particular with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can used to provide prophylaxis or treatment to a patient in need of treatment against leishmaniasis disease. 2Leishmania donovani. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone has in vitro toxicity against greater than Amphotericin B.3. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone has an in vitro selectivity index greater than Amphotericin B.4Leishmania donovani. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone has an ICvalue against promastigotes and amastigotes lower than Amphotericin B.5. (canceled)6. (canceled)9. The method according to claim 1 , wherein each R is aryl claim 1 , halo-substituted aryl claim 1 , aliphatic claim 1 , halo-substituted aliphatic claim 1 , or alkenyl.10. (canceled)11. The method according to claim 1 , wherein Q is an aryl-imido substituent.12. The method according to claim 1 , wherein each R is aryl claim 1 , optionally having halogen substitution.15. The method according to claim 14 , wherein Y is a meta-substitutent.16. The method according to claim 14 , wherein Y is an ortho-substitutent.17. The method according to claim 14 , wherein Y is a para-substitutent.18. The method according to claim 13 , wherein Y is bromo claim 13 , chloro or fluoro.19. The method according to claim 13 , wherein X is chloro.20. The method according to claim 19 , wherein X is chloro and Y is chloro.21. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone is selected from the group consisting of IMDNQ2 claim 1 , IMDNQ3 and IMDNQ4.22. The method according to claim 7 , wherein R is a C-Calkyl claim 7 , optionally having halogen substitution.23. The method according to claim 22 , wherein ...

Подробнее
24-09-2015 дата публикации

DIESEL DETERGENT WITHOUT A LOW MOLECULAR WEIGHT PENALTY

Номер: US20150267138A1
Принадлежит: THE LUBRIZOL CORPORATION

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 1. A composition comprising a quaternary ammonium salt , wherein the quaternary ammonium salt comprises the reaction product of: (i) at least one tertiary amino group, and', '(ii) a hydrocarbyl-substituent derived from a hydrocarbon having a number average molecular weight of from about 100 to about 500;, 'a) a compound comprising'}b) a quaternizing agent suitable for converting the tertiary amino group of compound (a) to a quaternary nitrogen.2. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group and at least one hydrocarbyl-substituent claim 1 , comprises:(I) the condensation product of an acylating agent substituted with the hydrocarbyl-substituent of a)ii) and a compound having an oxygen or nitrogen atom capable of condensing the acylating agent wherein the condensation product has at least one tertiary amino group;(II) an amine substituted with the hydrocarbyl-substituent of a)ii), wherein the amine has at least one tertiary amino group and the hydrocarbyl-substituent is a polyalkene-substituent;(III) a compound containing at least one hydrocarbyl-substituent of a)ii) and at least one tertiary amino group, wherein the hydrocarbyl-substituent is a polyester group; or(IV) any combination thereof.3. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group claim 1 , comprises the condensation product of a hydrocarbyl-substituted acylating agent and a compound having an oxygen or nitrogen atom capable of condensing with said acylating agent and further having at least one tertiary amino group; andwherein the hydrocarbyl-substituted acylating agent is polyisobutylene succinic anhydride and the ...

Подробнее
15-08-2019 дата публикации

PREPARATION METHOD OF OLIGOMER ADDITIVE, OLIGOMER ADDITIVE, AND LITHIUM BATTERY

Номер: US20190248958A1

A preparation method of an oligomer additive including the following steps is provided. A compound (A) having a secondary amine and a basic compound (B) are reacted. Next, a product of the reaction and a compound (C) having an unsaturated carbon-carbon double bond are reacted in a solvent. When the oligomer additive prepared by the method is applied in the cathode of a lithium battery, the cathode electrode core structure can be effectively protected from an environment condition such as high temperature, droppage, or deformation by external force. Moreover, the lithium battery cycle life can be maintained. 1. A preparation method of an oligomer additive , comprising the steps of reacting a compound (A) having a secondary amine and a basic compound (B) are reacted. Next , the resulting product and a compound (C) having an unsaturated carbon-carbon double bond are reacted in a solvent.2. The preparation method of the oligomer additive of claim 1 , wherein a mass ratio of the compound (A) having the secondary amine and the basic compound (B) is between 1:5 and 1:20.3. The preparation method of the oligomer additive of claim 1 , wherein based on a total weight of 100 parts by weight of the oligomer additive claim 1 , an amount of the compound (A) having the secondary amine is 0.5 parts by weight to 5 parts by weight claim 1 , an amount of the basic compound (B) is 5 parts by weight to 50 parts by weight claim 1 , and an amount of the compound (C) having the unsaturated carbon-carbon double bond is 2 parts by weight to 20 parts by weight.4. The preparation method of the oligomer additive of claim 1 , wherein the compound (A) having the secondary amine has three or more than three secondary amines.5. The preparation method of the oligomer additive of claim 1 , wherein the basic compound (B) is dimethyl sulfoxide.7. An oligomer additive prepared by the preparation method of the oligomer additive of claim 1 , wherein a compound (A) having a secondary amine and a basic ...

Подробнее
06-08-2020 дата публикации

K-RAS MODULATORS

Номер: US20200247762A1
Принадлежит:

Provided herein, inter alia, are methods and compounds for modulating K-Ras treating cancer. 2. (canceled)5. The compound of claim 1 , wherein the compound is of Formula (I) claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:Ring A is phenyl;{'sup': 1', '1', '1', '1', '1D', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1A', '1B', '1C', '1C', '1A', '1B', '1D', '1A', '1D', '1A', '1C', '1A', '1C', '1A', '1C', '1', '1', '1, 'sub': 3', '2', '2', 'n1', 'v1', 'm1', '2', '3', '2', '2, 'Ris independently halogen, —CX, —CHX, —CHX, —CN, —SOR, —SONRR, —NHNRR, —ONRR, —NHC═(O)NHNRR, —NHC(O)NRR, —N(O), —NRR, —C(O)R, —C(O)—OR, —C(O)NRR, —OR, —NRSOR, —NRC(O)R, —NRC(O)OR, —NROR, —OCX, —OCHX, —OCHX, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted heterocycloalkyl; or'}{'sup': '1', 'two adjacent Rsubstituents may optionally be joined to form a substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;'}z1 is an integer from 0 to 4;{'sup': 2', '2', '2', '2', '2A', '2A', '2A', '2B, 'sub': 3', '2', '2, 'Ris independently hydrogen, —CX, —CHX, —CHX, —C(O)R, —C(O)OR, —C(O)NRR, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;'}{'sup': '1', 'Lis a bond, substituted or unsubstituted alkylene, or substituted or unsubstituted cycloalkylene;'}{'sup': 3', '3', '3', '3', '3', '3, 'sub': '2', 'Lis a bond, —S(O)—, —N(R)—, —O—, —S—, —C(O)—, —C(O)N(R)—, —N(R)C(O)—, —N(R)C(O)NH—, —NHC(O)N(R)—, —C(O)O—, —OC(O)—, substituted or unsubstituted alkylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted cycloalkylene, substituted or unsubstituted ...

Подробнее
13-08-2020 дата публикации

HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20200255385A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 2. The compound of claim 1 , wherein Yis H.3. The compound of claim 1 , wherein Lis an optionally substituted C-Calkylene claim 1 , wherein at least two geminal hydrogens are optionally substituted with cyclopropano or cyclobutano.4. The compound of claim 1 , wherein Lis an optionally substituted C-Calkenylene.5. The compound of claim 1 , wherein Lis an optionally substituted C-Cheteroalkylene.6. The compound of claim 1 , wherein Lis an optionally substituted C-Cheteroalkenylene.8. The compound of claim 1 , wherein Lis -L-L-L- claim 1 , wherein Lis attached to A.10. The compound of claim 1 , wherein Lis —S(O)NH— claim 1 , wherein the sulfur is attached to L.11. The compound of claim 1 , wherein Lis —NHS(O)— claim 1 , wherein the nitrogen is attached to L.12. The compound of claim 1 , wherein Lis a bond.15. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient or carrier.17. The method of claim 16 , wherein the disease is cancer.18. The method of claim 17 , wherein the cancer is selected from the group consisting of colon cancer claim 17 , colorectal cancer claim 17 , gastric cancer claim 17 , esophageal cancer claim 17 , head and neck cancer claim 17 , breast cancer claim 17 , lung cancer claim 17 , stomach cancer claim 17 , liver cancer claim 17 , gall bladder cancer claim 17 , pancreatic cancer and leukemia.19. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of ; and a therapeutically effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.20. The method of claim 19 , wherein the cancer cell is selected from a colon cancer cell claim 19 , a colorectal cancer cell claim 19 , a gastric cancer cell claim 19 , a head and neck cancer cell claim 19 ...

Подробнее
13-08-2020 дата публикации

Diesel Detergent Without A Low Molecular Weight Penalty

Номер: US20200255760A1
Принадлежит:

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 2. A diesel fuel comprising the composition of .3. The diesel fuel of claim 2 , wherein the diesel fuel is ultra-low sulfur diesel fuel.4. The diesel fuel of claim 2 , wherein the quaternary ammonium salt is present from about 10 to about 500 ppm.5. A method of minimizing creation of internal diesel injector deposits while additionally reducing the level of pre-existing internal diesel injector deposits comprising the step of supplying to a diesel engine a diesel fuel composition comprising (A) diesel fuel; and (B) a composition according to .6. The method of wherein the diesel engine comprises common rail diesel injectors.7. A gasoline fuel comprising the composition of . This application is a continuation application of U.S. application Ser. No. 16/223,485, which is a continuation of U.S. application Ser. No. 14/434,985 filed on Apr. 10, 2015, granted as U.S. Pat. No. 10,202,559 on Feb. 12, 2019, which claims priority to PCT Application Serial No. PCT/US2013/066135 filed on Oct. 22, 2013 which claims benefit of U.S. Provisional Application Ser. No. 61/717,161 filed on Oct. 23, 2012.The composition of the present invention is related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.It is well known that liquid fuel contains components that can degrade during engine operation and form deposits. These deposits can lead to incomplete combustion of the fuel resulting in higher emission and poorer fuel economy. Fuel additives, such as detergents, are well known additives in liquid fuels to help with control or minimize deposit formation. As ...

Подробнее
08-10-2015 дата публикации

New nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio) molecules; precursors and conjugates thereof

Номер: US20150284326A1
Принадлежит: Advanced Accelerator Applications SA

Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conform to respective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.

Подробнее
05-09-2019 дата публикации

COMPOSITIONS FOR THE TREATMENT OF PULMONARY FIBROSIS

Номер: US20190270712A1
Автор: Duggan Karen Annette
Принадлежит: VECTUS BIOSYSTEMS LIMITED

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions. 4. A method of prophylactically or therapeutically treating pulmonary fibrosis claim 1 , or a related condition in a subject with pulmonary fibrosis or at risk of developing pulmonary fibrosis claim 1 , the method comprising administering to the subject an effective amount of a compound according to .715-. (canceled)16. The method according to claim 4 , wherein the subject at risk of developing pulmonary fibrosis:has been exposed to gases, smoke, chemicals, asbestos fibres or dusts;has an autoimmune disorder, viral infection or bacterial infection of the lung;has received radiation therapy for lung or breast cancer;has a genetic predisposition; oris a cigarette smoker.17. The method according to claim 4 , wherein claim 4 , the related condition is selected from pulmonary hypertension claim 4 , right-sided heart failure claim 4 , respiratory failure claim 4 , hypoxia claim 4 , cough claim 4 , formation of blood clots claim 4 , pneumonia and lung cancer18. The method according to claim 4 , wherein the treatment:prevents, reduces or slows the progression of pulmonary fibrosis; orreduces established pulmonary fibrosis.19. The method according to claim 5 , wherein the subject at risk of developing pulmonary fibrosis:has been exposed to gases, smoke, chemicals, asbestos fibres or dusts;has an autoimmune disorder, viral infection or bacterial infection of the lung;has received radiation therapy for lung or breast cancer;has a genetic predisposition; oris a cigarette smoker.20. The method according to claim 5 , wherein claim 5 , the related condition is selected from pulmonary hypertension claim 5 , right-sided heart failure claim 5 , respiratory failure claim 5 , hypoxia claim 5 , cough claim 5 , formation of blood clots claim 5 , pneumonia and lung cancer21. The method according to claim 5 , wherein the treatment: ...

Подробнее
05-09-2019 дата публикации

PROCESS FOR THE SYNTHESIS OF AMIDE BONDS WITH THE AID OF NOVEL CATALYSTS

Номер: US20190270768A1
Принадлежит: Merck Patent GmBH

The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof. 1. Process for the production of an amide bond by reaction of an acid with a primary or secondary amine in the presence of a base with the aid of an amide linking reagent , characterised in that use is made of at least one amide linking reagent containing an anion of the formula (I) ,{'br': None, 'sub': n', '2n+1', 'y', '6-y, 'sup': '−', '[P(CF)F]\u2003\u2003(I),'}wheren stands on each occurrence, independently, for 1, 2, 3, 4, 5, 6, 7 or 8 andy stands for 1, 2, 3 or 4.2. Process according to claim 1 , in which use is made of amide linking reagents containing anions of the formula (I) in which the variable n stands on each occurrence claim 1 , independently claim 1 , for 2 claim 1 , 3 or 4.3. Process according to claim 1 , in which use is made of amide linking reagents containing anions of the formula (I) selected from the group [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] and [(CF)PF].4. Process according to claim 1 , characterised in that the cation of the amide linking reagent is a uronium claim 1 , thiouronium claim 1 , guanidinium claim 1 , aminium claim 1 , carbonium claim 1 , imidazolium or phosphonium cation.5. Process according to claim 1 , characterised in that a peptide bond is produced.7. Compounds according to claim 6 , where FAP stands for [(CF)PF] Or [(n-CF)PF]. The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents as catalysts, to the novel reagents, and to the preparation thereof.Modern standard processes for peptide synthesis use effective peptide linking reagents. The formation of amide bonds is likewise of importance for the ...

Подробнее
27-08-2020 дата публикации

DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20200270207A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 3. The compound of claim 1 , wherein Lis an optionally substituted C-Calkylene claim 1 , wherein at least two geminal hydrogens together with the carbon to which they are attached are optionally replaced with cyclopropano or cyclobutano.4. The compound of claim 1 , wherein Lis an optionally substituted C-Calkenylene.5. The compound of claim 1 , wherein Lis an optionally substituted C-Cheteroalkylene.6. The compound of claim 1 , wherein Lis an optionally substituted C-Cheteroalkenylene.8. The compound of claim 1 , wherein Lis -L-L-L- claim 1 , wherein Lis attached to A.10. The compound of claim 1 , wherein Lis —S(O)NH— claim 1 , wherein the sulfur is attached to L.11. The compound of claim 1 , wherein Lis —NHS(O)— claim 1 , wherein the nitrogen is attached to L.12. The compound of claim 1 , wherein Lis a bond.15. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient or carrier.17. The method of claim 16 , wherein the disease is cancer.18. The method of claim 17 , wherein the cancer is selected from the group consisting of colon cancer claim 17 , colorectal cancer claim 17 , gastric cancer claim 17 , esophageal cancer claim 17 , head and neck cancer claim 17 , breast cancer claim 17 , lung cancer claim 17 , stomach cancer claim 17 , liver cancer claim 17 , gall bladder cancer claim 17 , pancreatic cancer and leukemia.19. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of ; and a therapeutically effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.20. The method of claim 19 , wherein the cancer cell is selected from a colon cancer cell claim 19 , a colorectal cancer cell claim 19 , a gastric cancer cell claim 19 , a head and neck cancer cell ...

Подробнее
12-09-2019 дата публикации

Processes for the Preparation of Apalutamide and Intermediates Thereof

Номер: US20190276424A1
Принадлежит:

The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1). 3. The process of claim 2 , wherein R is selected from the group consisting of a substituted or unsubstituted aryl group having 6 to 10 ring carbon atoms claim 2 , and a substituted or unsubstituted arylalkyl group having 6 to 10 ring carbon atoms and 1 to 3 alkyl carbon atoms.4. The process of claim 3 , wherein the solvent (S5) is selected from the group consisting of amides claim 3 , dimethylsulfoxide and pyridine.5. The process of claim 1 , wherein the solvent (S5) is pyridine.6. The process of claim 5 , wherein G is OR and R is selected from the group consisting of C1-C4 alkyl and substituted phenyl claim 5 , wherein the phenyl substituent is selected from the group consisting of NO claim 5 , chloride and fluoride.7. The process of claim 6 , wherein G is methoxy.9. The process of claim 8 , wherein LGis halide claim 8 , and the displacement comprises reaction of the compound of Formula (2-A) with a halogenating agent selected from the group consisting of thionyl chloride claim 8 , phosphorous trichloride and phosphorous pentachloride.10. The process of claim 9 , wherein the halogenating agent is thionyl chloride.12. The process of claim 11 , wherein Gis OR.13. The process of claim 12 , wherein the carboxylic acid activating agent is selected from the group consisting of thionyl chloride claim 12 , pivaloyl chloride claim 12 , N claim 12 ,N′-dicyclohexylcarbodiimide (DCC) claim 12 , N claim 12 ,N′-diisopropylcarbodiimide (DIC) claim 12 , N-(3-dimethylaminopropyl)-W-ethylcarbodiimide (EDC) and N-(3-dimethylaminopropyl)-W-ethylcarbodiimide hydrochloride (EDC.HCl).14. The process of claim 13 , wherein the ...

Подробнее
10-09-2020 дата публикации

DEOXYURIDINE TRIPHOSPHATASE INHIBITORS CONTAINING CYCLOPROPANO LINKAGE

Номер: US20200283394A1
Принадлежит:

Provided herein are dUTPase inhibitors of Formula (I), compositions comprising such compounds and methods of using such compounds and compositions 2. The method of claim 1 , wherein the disease is cancer.3. The method of claim 2 , wherein the cancer is selected from the group consisting of colon cancer claim 2 , colorectal cancer claim 2 , gastric cancer claim 2 , esophageal cancer claim 2 , head and neck cancer claim 2 , breast cancer claim 2 , lung cancer claim 2 , stomach cancer claim 2 , liver cancer claim 2 , gall bladder cancer claim 2 , pancreatic cancer claim 2 , and leukemia.8. The method of claim 1 , wherein Lis —S(O)NH— wherein the sulfur is attached to L.16. The method of claim 15 , wherein the cancer cell is selected from a colon cancer cell claim 15 , a colorectal cancer cell claim 15 , a gastric cancer cell claim 15 , a head and neck cancer cell claim 15 , a breast cancer cell claim 15 , a lung cancer cell or a blood cell. This application is a divisional of U.S. patent application Ser. No. 15/741,205, filed Dec. 29, 2017, which is a national stage application under 35 U.S.C. § 371 of International Application No. PCT/IB2016/054092, filed Jul. 7, 2016, which in turn claims the benefit of Indian Application No. 739/KOL/2015, filed Jul. 8, 2015, the entire contents of each of which are incorporated herein by reference.Thymidylate metabolism is required for producing essential building blocks necessary to replicate DNA in dividing cells and has long been an important therapeutic target for cornerstone cancer drugs. Drugs targeting this pathway such as 5-fluorouracil (5-FU) inhibit the enzyme thymidylate synthase (TS) and are currently critical standard-of care therapies. TS-targeted agents are used for the treatment of a variety of cancers including colon, gastric, head and neck, breast, lung and blood related malignancies among others. Grem, J. L., 5-, J. De Vita, V. T., S. Hellman, and A. Rosenberg, Editors. 1988, J. B. Lippincott: Philadelphia, Pa. ...

Подробнее
10-09-2020 дата публикации

USES OF ISOBARIC TAGS IN MASS SPECTROMETRY

Номер: US20200286721A1
Принадлежит:

The present invention relates to use of an isobaric label in mass spectrometry (MS) analysis using data-independent acquisition (DIA), wherein said isobaric label comprises or consists of a group which fragments in the mass spectrometer (i) at an energy below the energy required for fragmenting analyte-derived precursor ions and/or a higher conversion rate than said precursor ions; and (ii) at said energy according to (i) and when coupled to a precursor ion, at a single site within said group, to yield a first moiety and a second moiety, said second moiety being coupled to said precursor ion. 1. Use of an isobaric label in mass spectrometry (MS) analysis using data-independent acquisition (DIA) , wherein said isobaric label comprises or consists of a group which fragments in the mass spectrometer(i) at an energy below the energy required for fragmenting analyte-derived precursor ions and/or a higher conversion rate than said precursor ions; and(ii) at said energy according to (i) and when coupled to a precursor ion, at a single site within said group, to yield a first moiety and a second moiety, said second moiety being coupled to said precursor ion.2. A method of analysis using a mass spectrometer claim 1 , said method comprising collecting precursor ions originating from different analytes in a data-independent manner claim 1 , wherein said precursor ions carry an isobaric label as defined in .3. Use of an isobaric label as defined in in mass spectrometry analysis using data-dependent acquisition (DDA).4. A method of analysis using a mass spectrometer claim 1 , said method comprising collecting precursor ions originating from different analytes in a data-dependent manner claim 1 , wherein said precursor ions carry an isobaric label as defined in .5. A method of operating a mass spectrometer comprising a detector claim 1 , said detector preferably being an Orbitrap detector or a TOF detector claim 1 , said method comprising claim 1 , in the time elapsing during the ...

Подробнее
25-10-2018 дата публикации

Synthesis of Succinimides and Quaternary Ammonium Ions for Use in Making Molecular Sieves

Номер: US20180305309A1
Принадлежит:

The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves. 115.-. (canceled)16. A process for producing a molecular sieve , the process comprising the steps of:{'sup': −', '+, '(i) preparing a synthesis mixture capable of forming a molecular sieve, said synthesis mixture comprising a source selected from a source of a tetravalent element Y, a source of a trivalent element X, or a mixture of a source of tetravalent element Y and a source of trivalent element X, and optionally a source of pentavelent element Z, optionally a source of hydroxide ions, optionally a source of halide ions W, and optionally a source of alkali metal ions M, the synthesis mixture further comprising a structure directing agent Q comprising a cation comprising a pyrrolidinium group in which the ring nitrogen is a quaternary ammonium nitrogen and in which at least one, and preferably both, of the 3- and the 4-positions on the pyrrolidinium ring is substituted with a substituent group other than hydrogen;'}(ii) heating said synthesis mixture under crystallization conditions for a time of from about 1 to about 100 days to form crystals of said molecular sieve; and(iii) recovering said crystals of the molecular sieve from the synthesis mixture.17. The process as claimed in claim 16 , wherein the synthesis mixture does not contain any pentavelent element Z.18. The process as claimed in claim 16 , wherein the synthesis mixture contains a pentavelent element Z claim 16 , preferably phosphorus.19. The process as claimed in or as claimed in claim 16 , ...

Подробнее
03-11-2016 дата публикации

PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF ENZALUTAMIDE

Номер: US20160318875A1
Принадлежит:

The present invention provides processes for the preparation of enzalutamide. 4. The process according to or , wherein the reaction of the compound of Formula II with the compound of Formula III to give the compound of Formula IV is carried out in a solvent selected from the group consisting of water , dimethyl sulfoxide , esters , ethers , alcohols , hydrocarbons , halogenated hydrocarbons , amides , and mixtures thereof.5. The process according to or , wherein the reaction of the compound of Formula IV with the compound of Formula V is carried out in a solvent selected from the group consisting of water , dimethyl sulfoxide , esters , ethers , alcohols , hydrocarbons , halogenated hydrocarbons , and mixtures thereof.7. (canceled)8. The process according to claim 6 , wherein the reaction of the compound of Formula VI with the compound R—OH to give the compound of Formula V is carried out in the presence of a coupling agent selected from the group consisting of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride claim 6 , N claim 6 ,N′-dicyclohexylcarbodiimide claim 6 , thionyl chloride claim 6 , and oxalyl chloride.9. The process according to claim 6 , wherein the reaction of the compound of Formula VI with the compound R—OH to give the compound of Formula V is carried out in the presence of a solvent selected from the group consisting of water claim 6 , esters claim 6 , halogenated hydrocarbons claim 6 , ethers claim 6 , alcohols claim 6 , hydrocarbons claim 6 , amides claim 6 , and mixtures thereof.10. The process according to claim 6 , wherein the reaction of the compound of Formula VI with the compound R—OH to give the compound of Formula V is carried out in the presence of N claim 6 ,N-dimethylaminopyridine.13. Use of a compound of Formula IV for the preparation of enzalutamide.14. Use of a compound of Formula V for the preparation of enzalutamide.16. The process according to claim 14 , wherein the reaction of the compound of Formula V with the ...

Подробнее
02-11-2017 дата публикации

Branched Discrete PEG Constructs

Номер: US20170313656A1
Принадлежит:

Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues. 2. The substantially pure compound of claim 1 , wherein A comprises a preferential locator that binds with a biological moiety claim 1 , said preferential locator being one or more of a cell surface and matrix antigen claim 1 , transport protein claim 1 , or receptor protein.3. The substantially pure compound of claim 2 , wherein said preferential locator A is one or more of an antibody claim 2 , antibody fragment claim 2 , engineered antibody claim 2 , engineered fragment claim 2 , peptide substrate claim 2 , peptomimetic substrate claim 2 , cytokine claim 2 , aptamer claim 2 , siRNA claim 2 , vitamin claim 2 , or steroid.4. The substantially pure compound of claim 1 , wherein A is a nanoparticle claim 1 , microparticle claim 1 , engineered molecular scaffold that contains multiple functionalities claim 1 , or an engineered chemically reactable group.5. The substantially pure compound of claim 1 , wherein A is a chemically reactable moiety being one or more of an alkyl or aryl functionalized 1° or 2° amine claim 1 , hydroxyl claim 1 , aldehyde claim 1 , ketone claim 1 , carboxylate claim 1 , active carboxylate ester ...

Подробнее
10-11-2016 дата публикации

Radioiodinated compounds

Номер: US20160326109A1
Автор: Bao HU, Stephen Dimagno
Принадлежит: NuTech Ventures Inc

This disclosure relates to reagents and methods useful in the synthesis of aryl iodines, for example, in the preparation of iodine labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.

Подробнее
19-11-2015 дата публикации

Improved Synthesis Of Succinimides And Quaternary Ammonium Ions For Use In Making Molecular Sieves

Номер: US20150329487A1
Принадлежит:

The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves.

Подробнее
19-11-2015 дата публикации

PYRROLIDINE-2, 5-DIONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE AS IDO1 INHIBITORS

Номер: US20150329525A1
Принадлежит:

The present invention relates to compound of Formula I

Подробнее
10-10-2019 дата публикации

QUATERNARY AMMONIUM COMPOUNDS AS FUEL OR LUBRICANT ADDITIVES

Номер: US20190309234A1
Принадлежит: INNOSPEC LIMITED

A quaternary ammonium compound of formula (X): 1. A method of preparing a fuel composition , said method comprising: preparing a quaternary ammonium compound by reacting:{'sup': 1', '2', '3, '(a) a tertiary amine of formula RRRN with;'}(b) an epoxide; in the presence of(c) a monoester of a diacid including an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms;{'sup': 1', '2', '3, 'wherein R, Rand Rare each independently selected from an optionally substituted alkyl, alkenyl or aryl group; and mixing the quaternary ammonium compound into a fuel.'}2. A method according to wherein each of Rand Ris independently alkyl claim 1 , alkenyl or aryl group having from 1 to 50 carbon atoms optionally substituted with one or more groups selected from halo (especially chloro and fluoro) claim 1 , hydroxy claim 1 , alkoxy claim 1 , keto claim 1 , acyl claim 1 , cyano claim 1 , mercapto claim 1 , alkylmercapto claim 1 , dialkylamino claim 1 , nitro claim 1 , nitroso claim 1 , and sulphoxy.3. A method according to wherein Ris an alkyl or alkenyl group having from 1 to 50 carbon atoms optionally substituted with one or more substituents selected from halo (especially chloro and fluoro) claim 1 , hydroxy claim 1 , alkoxy claim 1 , keto claim 1 , acyl claim 1 , cyano claim 1 , mercapto claim 1 , alkylmercapto claim 1 , amino claim 1 , alkylamino claim 1 , nitro claim 1 , nitroso claim 1 , sulphoxy claim 1 , amido claim 1 , alkyamido claim 1 , imido and alkylimido.4. A method according to wherein Ris an alkyl or alkenyl group optionally substituted with alkoxy or hydroxy groups.5. A method according to wherein each of Rand Ris an unsubstituted alkyl group or a hydroxy substituted alkyl group.9. A method according to wherein each of R claim 1 , Rand Ris selected from an alkyl or hydroxyl alkyl group having 1 to 10 carbon atoms.10. A method according to wherein epoxide (b) is selected from styrene oxide claim 1 , ethylene oxide claim 1 , propylene oxide claim 1 , ...

Подробнее
08-10-2020 дата публикации

Branched Discrete PEG Constructs

Номер: US20200317612A1
Принадлежит:

Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues. 122-. (canceled)2310. A method of externally imaging an antibody , antibody fragment , or a peptide attached to an externally imagable radiolabel , which comprises attaching said imagable radiolabel to and said antibody , antibody fragment , or a peptide to the structure of claim , wherein RG is said radiolabel and A comprises said antibody , antibody fragment , or a peptide.24. The method of claim 23 , wherein said antibody has been generated against a tumor associated glycoprotein.25. The method of claim 24 , wherein said antibody comprises B72.3 claim 24 , CC49 claim 24 , V59 claim 24 , or 3E8.26. The method of claim 25 , wherein said antibody comprises CC49 claim 25 , domain deleted CC49 claim 25 , CC49 fragments claim 25 , including Fab′ claim 25 , CC49 diabodies claim 25 , CC49 scFv claim 25 , and single chains derived therefrom.27. The method of claim 23 , wherein said antibody comprises 3E8 claim 23 , domain deleted 3E8 claim 23 , 3E8 fragments claim 23 , 3E8 diabodies claim 23 , and single chains derived therefrom.2831-. (canceled) This application claims benefit of application Ser. No. 61/528,915 ...

Подробнее
23-11-2017 дата публикации

ANTIFIBRINOLYTIC COMPOUNDS

Номер: US20170334834A1
Автор: Chibber Bakshy A.
Принадлежит: THROMBOLYTICS, LLC

The present invention provides novel antifibrinilytic compounds, processes for their preparation, pharmaceutical and veterinary compositions thereof, and their use in medicine, in particular for the treatment of bleeding. 4. The compound of claim 1 , wherein Ris hydroxyl or —O—(C-C)alkyl claim 1 , or a pharmaceutically acceptable salt thereof.5. The compound of claim 4 , wherein Ris hydroxyl claim 4 , or a pharmaceutically acceptable salts thereof.6. The compound according to claim 1 , wherein Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 1 , or a pharmaceutically acceptable salts thereof.7. The compound of claim 6 , wherein Rand Rare both methyl claim 6 , or a pharmaceutically acceptable salts thereof.8. The compound according to claim 2 , wherein Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 2 , or a pharmaceutically acceptable salts thereof.9. The compound according to claim 3 , wherein .Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 3 , or a pharmaceutically acceptable salts thereof.10. The compound according to claim 4 , wherein .Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 4 , or a pharmaceutically acceptable salts thereof.11. The compound of claim 8 , wherein Rand Rare both methyl claim 8 , or a pharmaceutically acceptable salts thereof.12. The compound of claim 9 , wherein Rand Rare both methyl claim 9 , or a pharmaceutically acceptable salts thereof.13. The compound of claim 10 , wherein Rand Rare both methyl claim 10 , or a pharmaceutically acceptable salts thereof. The present invention relates to novel antifibrinolytic compounds, processes for their preparation, pharmaceutical compositions thereof, and their use in medicine, particularly for the treatment of bleeding.A major goal in surgery, as well as treatment of major tissue damage, is to avoid or minimize bleeding to ensure the formation of stable and secure haemostatic plugs that are not easily dissolved by fibrinolytic enzymes. It is of importance ...

Подробнее
15-10-2020 дата публикации

DEOXYURIDINE TRIPHOSPHATASE INHIBITORS CONTAINING AMINO SULFONYL LINKAGE

Номер: US20200325105A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 2. The compound of claim 1 , wherein Lis optionally substituted C-Calkylene.3. The compound of claim 1 , wherein Lis optionally substituted C-Cheteroalkylene.6. The compound of claim 1 , wherein Lis —NHS(O)— wherein the nitrogen is attached to L.7. The compound of claim 1 , wherein Lis —SONR— claim 1 , wherein the sulfur is attached to L.12. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient.13. A method of one or more of inhibiting dUTPase or enhancing the efficacy of a dUTPase directed therapy claim 1 , wherein the method comprises contacting the dUTPase with a therapeutically effective amount of the compound of .14. A method of reversing resistance to a dUTPase-directed therapy claim 1 , wherein the method comprises contacting the dUTPase with a therapeutically effective amount of the compound of .15. A method of treating a disease whose treatment is impeded by the expression or over expression of dUTPase claim 1 , comprising administering to a patient in need of such treatment a therapeutically effective amount of the compound of .16. The method of claim 15 , wherein the disease is cancer.17. The method of claim 16 , wherein the cancer is selected form the group consisting of colon cancer claim 16 , colorectal cancer claim 16 , gastric cancer claim 16 , esophageal cancer claim 16 , head and neck cancer claim 16 , breast cancer claim 16 , lung cancer claim 16 , stomach cancer claim 16 , liver cancer claim 16 , gall bladder cancer claim 16 , pancreatic cancer claim 16 , and leukemia.18. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of claim 1 , and an effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.19. The method of claim 18 , ...

Подробнее
22-11-2018 дата публикации

DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20180334431A1
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 4. (canceled)6. (canceled)11. (canceled)12. The compound of claim 1 , wherein Lis —S(O)NH— wherein the sulfur is attached to L.14. (canceled)15. (canceled)16. (canceled)17. (canceled)19. (canceled)20. (canceled)21. A compound selected from Table 1.22. A composition comprising a compound of claim 1 , and at least one pharmaceutically acceptable excipient.23. A method of:a. one or more of inhibiting dUTPase or enhancing the efficacy of a dUTPase directed therapy; orb. reversing resistance to a dUTPase-directed therapy;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the method comprises contacting the dUTPase with a therapeutically effective amount of the compound of .'}24. (canceled)25. A method of treating a disease in a patient whose treatment is impeded by the expression or over expression of dUTPase claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. administering to the patient in need of such treatment a therapeutically effective amount of the compound of ; or'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'b. screening a cell or tissue sample from the patient; determining the expression level of dUTPase in the sample; and administering to the patient whose sample shows over expression of dUTPase, a therapeutically effective amount of the compound of .'}26. A method of inhibiting the growth of a cancer cell comprising contacting the cell with a therapeutically effective amount of the compound of and an effective amount of a dUTPase directed therapeutic claim 1 , thereby inhibiting the growth of the cancer cell.27. The method of claim 26 , wherein the cancer cell is selected from a colon cancer cell claim 26 , a colorectal cancer cell claim 26 , a gastric cancer cell claim 26 , a head and neck cancer cell claim 26 , a breast cancer cell claim 26 , a lung cancer cell or a blood cell.28. (canceled ...

Подробнее
31-10-2019 дата публикации

CONJUGATES OF CELL BINDING MOLECULES WITH CYTOTOXIC AGENTS

Номер: US20190330149A1
Принадлежит: HANGZHOU DAC BIOTECH CO., LTD.

A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R, R, R, R, R, R, R, R, R, R, R, R, and Rare defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.

Подробнее
22-10-2020 дата публикации

Material for forming organic film, substrate for manufacturing semiconductor device, method for forming organic film, patterning process, and compound for forming organic film

Номер: US20200332062A1
Принадлежит: Shin Etsu Chemical Co Ltd

An object of the present invention is to provide: a compound containing an imide group which is not only cured under film formation conditions of inert gas as well as air, generates no by-product and has excellent heat resistance and properties of filling and planarizing a pattern formed on a substrate, but can also form an organic underlayer film with favorable adhesion to a substrate. The present invention provides a material for forming an organic film, including: (A) a compound for forming an organic film shown by the following general formula (1A) or (1B); and (B) an organic solvent, noting that in the general formula (1A), when W 1 represents any of R 1 does not represent any of

Подробнее
31-10-2019 дата публикации

COMPOUNDS AND METHOD FOR ENHANCED OIL RECOVERY USING SULFUR SURFACTANTS

Номер: US20190330515A1
Принадлежит:

A method of enhanced oil recovery wherein: (a) a flooding composition is delivered into a subterranean reservoir; (b) the flooding composition includes a sulfur surfactant; and (c) the fluid produced from the subterranean reservoir can also be analyzed to determine if the surfactant is present in the fluid. The surfactant preferably includes a sulfonate moiety or other sulfur-containing moiety. The presence of the surfactant in the fluid produced from the subterranean reservoir is preferably determined by X-ray fluorescence spectroscopy, HPLC-AES, or HPLC-ICP.

Подробнее
07-12-2017 дата публикации

METHOD FOR PRODUCING NITROGEN-CONTAINING PENTAFLUOROSULFANYLBENZENE COMPOUND

Номер: US20170349545A1
Принадлежит:

A method for producing a nitrogen-containing pentafluorosulfanylbenzene compound of formula (2a) or (2b): 3. The method according to claim 1 , wherein the nitrogenous nucleophile is at least one member selected from benzylamine compounds claim 1 , hydrazine compounds claim 1 , guanidine compounds claim 1 , hydroxylamines and alkali metal salts of phthalimide.4. The method according to claim 2 , wherein the reduction is carried out in the presence of hydrogen using Pd/C or Raney nickel as a catalyst.5. The method according to claim 2 , wherein the hydrolysis is carried out using an aqueous acid solution or an aqueous alkali solution.6. The method according to claim 1 , wherein an aprotic polar solvent is used as a solvent.7. The method according to claim 6 , wherein the aprotic polar solvent is dimethyl sulfoxide or N-methyl-2-pyrrolidone.8. The method according to claim 1 , wherein a base is used in the reaction of the halogeno-pentafluorosulfanylbenzene compound with the nitrogenous nucleophile. The present invention relates to a method for producing a nitrogen-containing pentafluorosulfanylbenzene compound, comprising reacting a halogenated aromatic compound with a nitrogenous nucleophile.Aromatic amine compounds like aniline are compounds that are useful mainly as base materials for pharmaceuticals, agricultural chemicals, and dyes.It was known that pentafluorosulfanylaniline compounds can be produced by reacting a disulfide compound with a fluorine gas (Patent Literature 1). This method was found to have some problems, because a fluorine gas which is problematic in handling must be used, and because with the progress of the fluorination of the benzene nucleus, the resulting nucleus fluorine compound becomes difficult to remove. For these reasons, it is difficult to produce these compounds by this method, and thus this method was hardly adopted as an industrial production method.Patent Literature 1: Japanese Patent No. JP 3964935An object of the present invention ...

Подробнее
22-12-2016 дата публикации

Reduction-triggered antibacterial sideromycins

Номер: US20160368878A1
Автор: CHENG JI, Marvin J. Miller
Принадлежит: University of Notre Dame

A compound is provided, comprising: an Fe(III)-binding or an Fe(III)-bound siderophore; one or more optional linker covalently bound to the siderophore; a drug; and an Fe(III) to Fe(II) reduction triggered linker bound to the drug and the linker or, if no linker is present, then bound to the drug and the siderophore. Compositions and methods including the compound are also provided.

Подробнее
21-11-2019 дата публикации

COMPOUND, SUBSTRATE FOR PATTERN FORMATION, PHOTODEGRADABLE COUPLING AGENT, PATTERN FORMATION METHOD, AND TRANSISTOR PRODUCTION METHOD

Номер: US20190352260A1
Принадлежит:

Provided is a compound represented by Formula (1). 2. The compound according to claim 1 , wherein Ror Rrepresents any of a methyl group claim 1 , an isopropyl group claim 1 , or a tert-butyl group.3. A substrate for pattern formation claim 1 , which has a surface chemically modified by the compound according to .4. A photodegradable coupling agent which is formed of the compound according to .5. A pattern formation method of forming a pattern on a surface of an object to be treated claim 1 , comprising:aminating at least a part of the surface of the object to be treated to form an aminated surface;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'chemically modifying the aminated surface using the compound according to ;'}irradiating the chemically modified surface to be treated with light in a predetermined pattern to generate a latent image formed of a hydrophilic region and a water-repellent region; anddisposing a pattern forming material in the hydrophilic region or the water-repellent region.6. The pattern formation method according to claim 5 ,wherein the predetermined pattern corresponds to a circuit pattern for an electronic device.7. The pattern formation method according to claim 5 ,wherein the pattern forming material contains a conductive material, a semiconductor material, or an insulating material.8. The pattern formation method according to claim 7 ,wherein the conductive material is formed of a conductive fine particle dispersion liquid.9. The pattern formation method according to claim 7 ,wherein the semiconductor material is formed of an organic semiconductor material dispersion liquid.10. A pattern formation method of forming a pattern on a surface of an object to be treated claim 7 , comprising:aminating at least a part of the surface of the object to be treated to form an aminated surface;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'chemically modifying the aminated surface using the compound according to ;'}irradiating the chemically ...

Подробнее
12-11-2020 дата публикации

Prodrugs of Fumarates and Their Use in Treating Various Diseases

Номер: US20200352893A1
Принадлежит:

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof. 111-. (canceled)13. A pharmaceutical composition comprising the compound of claim 12 , or a pharmaceutically acceptable salt thereof.14. A method of treating multiple sclerosis in a subject in need thereof claim 12 , comprising administering to the subject a therapeutically effective amount of the compound of .15. A method of treating multiple sclerosis in a subject in need thereof claim 13 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 16/524,498, filed Jul. 29, 2019, which is a continuation of U.S. application Ser. No. 16/145,703, filed Sep. 28, 2018, now U.S. Pat. No. 10,406,133, issued Sep. 10, 2019, which is a continuation of U.S. application Ser. No. 15/704,219, filed Sep. 14, 2017, now U.S. Pat. No. 10,117,846, issued Nov. 6, 2018, which is a continuation of U.S. application Ser. No. 15/295,370, filed Oct. 17, 2016, now U.S. Pat. No. 9,775,823, issued Oct. 3, 2017, which is a continuation of U.S. application Ser. No. 14/212,745, filed Mar. 14, 2014, now U.S. Pat. No. 9,505,776, issued Nov. 29, 2016, which claims the benefit of U.S. Provisional Application No. 61/934,365, filed Jan. 31, 2014 and U.S. Provisional Application No. 61/782,445, filed Mar. 14, 2013, the contents of which are incorporated herein by reference in their entireties.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range ...

Подробнее
05-12-2019 дата публикации

Assay plate and manufacturing method thereof

Номер: US20190366331A1
Автор: Feng-Di Lung
Принадлежит: Tunghai University

The present invention discloses an assay plate, which has a plate body made of polymeric material modified by coating a compound A thereon, and allows a molecule such as protein or peptide, or a group to bind to the plate body by hydrophobic bonding for use in biomedical assay.

Подробнее