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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 3585. Отображено 100.
19-01-2012 дата публикации

(2,5-dioxoimidazolidin-i-yl)-n-hydroxy-acetamides as metalloproteinase inhibitors

Номер: US20120015994A1
Автор: Bertil Samuelsson, Guo-Qiang Lin, Hans Wallberg, Kevin Parkes, Ming-Hua Xu, Piaoyang Sun, Tony Johnson, Xin-Sheng Lei
Принадлежит: Medivir AB

The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).

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Номер записи: 1
10-05-2012 дата публикации

Crystalline forms of an alkoxyimidazol-1-ylmethyl biphenyl carboxylic acid

Номер: US20120115920A1
Автор: Paul R. Fatheree, Venkat R. Thalladi
Принадлежит: Theravance Inc

The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension.

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Номер записи: 2
19-07-2012 дата публикации

Novel n-halamine acrylamide monomers and copolymers thereof for biocidal coatings

Номер: US20120183494A1
Автор: Hasan B. Kocer, Idris CERKEZ, Royall M. Broughton, Shelby D. Worley
Принадлежит: AUBURN UNIVERSITY

Novel acrylamide and methacrylamide hydantoin monomers which can be reacted with other acrylamide, methacrylamide, acrylate, and methacrylate monomers to form copolymers, which upon halogenation, provide oxidative coatings which are biocidal for use with various materials including, but not limited to, textiles, filters, and latex paints.

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Номер записи: 3
20-12-2012 дата публикации

Deuterated compounds useful for treating neurodegenerative diseases

Номер: US20120322799A1
Автор: GOPAL Damodara
Принадлежит: Pharmatrophix Inc

The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.

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Номер записи: 4
11-04-2013 дата публикации

ESTER COMPOUND AND USE THEREOF

Номер: US20130090363A1
Автор: Matsuo Noritada
Принадлежит: Sumitomo Chemical Company, Limited

An ester compound represented by formula (1): wherein Rrepresents hydrogen or methyl, Rrepresents hydrogen or C1-C4 alkyl, and Rrepresents hydrogen or C1-C4 alkyl; has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent. 2. The ester compound according to claim 1 , wherein a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).3. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration in formula (1).4. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , and a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration in formula (1).5. The ester compound according to claim 1 , wherein a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).6. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration and a relative configuration of the substituent of the 1′-position existing on the substituent at the 3-position of the cyclopropane ring is Z-configuration in formula (1).7. The ester compound according to claim 1 , wherein an absolute configuration of the 1-position of the cyclopropane ring is an R configuration claim 1 , a relative configuration of the substituent at the 1-position of the cyclopropane ring and the substituent at the 3-position of the cyclopropane ring is a trans configuration claim 1 , and a relative configuration of the substituent of the 1′-position existing on the substituent at ...

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Номер записи: 5
09-05-2013 дата публикации

Cyclic n,n'-diarylthioureas and n,n'-diarylureas - androgen receptor antagonists, anticancer agent, method for preparation and use thereof

Номер: US20130116269A1
Автор: Alexandre Vasilievich IVACHTCHENKO, Oleg Dmitrievich Mitkin
Принадлежит: IVACHTCHENKO ALEXANDRE VASILIEVICH DR, IVASHCHENKO ANDREY ALEXANDROVICH DR, SAVCHUK NIKOLAY FILIPPOVICH DR

The present invention relates to novel cyclic N,N′-diarylureas and N,N′-diarylthioureas—androgen receptor antagonists, anti-cancer agent, pharmaceutical composition, medicament, and method for treatment of cancerous diseases, among them prostate cancer. Cyclic N,N′-diarylthioureas or N,N′-diarylureas of the general formula 1, their optical (R)- and (S)-isomers and pharmaceutically acceptable salts thereof exhibiting properties of androgen receptor antagonists have been proposed, wherein: X represents oxygen or sulfur; m=0 or 1; R1 represents C 1 -C 3 alkyl; R2 and R3 represent hydrogen; or R2 and R3 together with C-atom they are attached to form C═O group; R4 and R5 represent hydrogen; or R4 represents hydrogen, R5 represents methyl; or R4 represents methyl, R5 represents CH 2 R6 group in which R6 represents C 1 -C 3 alkoxycarbonyl, carboxyl, hydroxyl group optionally substituted with methyl or benzyl; or R4 and R5 together with C-atom they are attached to form 5- or 6-membered heterocycle comprising at least one oxygen atom or nitrogen atom optionally substituted with methyl; or R4 and R5 together with C-atom they are attached to form NH group.

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Номер записи: 6
15-08-2013 дата публикации

COMPOUNDS AND COMPOSITIONS AS INHIBITORS OF CANNABINOID RECEPTOR 1 ACTIVITY

Номер: US20130210769A1
Автор: He Xiaohui, Lau Thomas, Liu Hong, Nguyen Truc Ngoc, Phillips Dean Paul, Wang Xing, Wu Baogen, Xie Yongping, Yang Kunyong, Zhu Xuefeng
Принадлежит: IRM LLC

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1). 2. The compound of in which Ris selected from cyano claim 1 , methyl-carbonyl-amino-sulfonyl-ethyl claim 1 , pyrrolidin-2-onyl-ethyl claim 1 , imidazolyl-ethyl claim 1 , oxazolidin-2-only-ethyl claim 1 , 1-pyrazolyl-ethyl claim 1 , cyano-methyl claim 1 , 4′-(4-chlorophenoxy)phenyl claim 1 , 1 claim 1 ,3-dioxanyl-ethyl claim 1 , allyl claim 1 , phenyl claim 1 , pyrazinyl claim 1 , piperazinyl-sulfonyl-ethyl claim 1 , azetidinyl-sulfonyl-ethyl claim 1 , morpholino-sulfonyl-ethyl claim 1 , pyrrolidinyl-sulfonyl-ethyl claim 1 , pyrrolidinyl-propyl claim 1 , pyrrolidinyl-ethyl claim 1 , piperazinyl-propyl claim 1 , piperidinyl-sulfonyl-ethyl claim 1 , pyridazinyl claim 1 , (5-(4-methoxyphenyl)-1 claim 1 ,2 claim 1 ,4-oxadiazol-3-yl)methyl claim 1 , isoxazolyl claim 1 , piperidinyl-carbonyl-methyl claim 1 , 3-(N claim 1 ,N-bis(4-methoxyphenyl)sulfamoyl)propyl claim 1 , methyl-phenyl-sulfonyl claim 1 , cyanomethyl claim 1 , 2-oxo-2-(piperidin-1-ylamino)ethyl claim 1 , propyl-amino-carbonyl-methyl claim 1 , 2-(carboxymethylamino)-2-oxoethyl) claim 1 , bis-hydroxyethyl-amino-sulfonyl-ethyl claim 1 , carboxy-methyl-amino-carbonyl-methyl claim 1 , amino-carbonyl-ethyl claim 1 , amino-sulfonyl-ethyl claim 1 , amino-sulfonyl-propyl claim 1 , methyl-amino-ethyl claim 1 , piperidinyl-ethyl claim 1 , piperazinyl-ethyl claim 1 , methyl-sulfonyl-ethyl claim 1 , carboxy-methyl claim 1 , tetrazole-methyl claim 1 , benzyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole-methyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazole-ethyl claim 1 , isoxazole-methyl claim 1 , 2-(2-hydroxyethylamino)-2-oxoethyl claim 1 , dimethylamino-ethyl-amino-carbonyl-methyl claim 1 , hydroxyl-ethyl claim 1 , methoxy-ethyl claim 1 , hydroxyl-ethyl- ...

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Номер записи: 7
22-08-2013 дата публикации

IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS N-FORMYL PEPTIDE RECEPTOR 2 MODULATORS

Номер: US20130217720A1
Автор: Beard Richard L., Donello John E., Garst Michael E., Viswanath Veena, Vuligonda Vidyasagar
Принадлежит: ALLERGAN, INC.

The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2). 2. A compound according to wherein:{'sup': '1', 'sub': 1-6', '2-6', '2-6', '3-8', '3-8', '6-10, 'Ris hydrogen, halogen, substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted Ccycloalkyl, substituted or unsubstituted Ccycloalkenyl substituted or unsubstituted heterocycle or substituted or unsubstituted Caryl; and'}{'sup': 2', '3, 'Rand Rform a substituted or unsubstituted 3 to 6 member ring heterocycle.'}3. A compound according to claim 1 , wherein:{'sup': '1', 'Ris hydrogen; and,'}{'sup': 2', '3, 'Rand Rform a substituted or unsubstituted 3 to 6 member ring heterocycle.'}4. A compound according to claim 1 , wherein:{'sup': 1', '2, 'Rtogether with Rforms an optionally substituted cyclobutyl or cyclopropyl; and,'}{'sup': '3', 'sub': 1-6', '2-6', '2-6', '3-8', '3-8', '6-10, 'Ris hydrogen, substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted Ccycloalkyl, substituted or unsubstituted Ccycloalkenyl, substituted or unsubstituted heterocycle, substituted or unsubstituted Caryl.'}5. A compound according to claim 1 , wherein:{'sup': 1', '2, 'Rtogether with Rforms an optionally substituted cyclobutyl or cyclopropyl; and,'}{'sup': '3', 'sub': '1-6', 'Ris H or substituted or unsubstituted Calkyl.'}6. A compound according to claim 1 , wherein:{'sup': '1', 'sub': 1-6', '2-6', '2-6', '3-8', '3-8', '6-10, 'Ris hydrogen, halogen, substituted or unsubstituted Calkyl, substituted or unsubstituted Calkenyl, substituted or unsubstituted Calkynyl, substituted or unsubstituted Ccycloalkyl, substituted or unsubstituted Ccycloalkenyl substituted or unsubstituted heterocycle or ...

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Номер записи: 8
12-12-2013 дата публикации

SPECIFIC DIARYLHYDANTOIN AND DIARYLTHIOHYDANTOIN COMPOUNDS

Номер: US20130331421A1
Автор: Gibbons Jacqueline A., JAIN Rajendra Parasmal
Принадлежит: MEDIVATION PROSTATE THERAPEUTICS, INC.

Compositions, such as pharmaceutical compositions, comprising specific diarylhydantoin and diarylthiohydantoin compounds, or salts or solvates thereof, are provided. Isolated and purified forms of the compounds are also described, as are unit dosage forms, compositions of substantially pure compound and kits comprising the compounds. The compounds and pharmaceutical compositions thereof may find use in the prevention and/or treatment of a variety of conditions, including prostate cancer, Parkinson's disease, Alzheimer's disease, and others. 2. The pharmaceutical composition of claim 1 , wherein X is S and Ris OH or NH.3. The pharmaceutical composition of claim 1 , wherein X is O and Ris OH claim 1 , NHor NHMe.10. The composition of claim 9 , wherein X is S and Ris OH or NH.11. The composition of claim 9 , wherein X is O and Ris OH claim 9 , NHor NHMe.1716. The composition of any of - claims 9 , wherein the composition contains less than about 10 weight percent impurity.19. The method of claim 18 , wherein X is S and Ris OH or NH.20. The method of claim 18 , wherein X is O and Ris OH claim 18 , NHor NHMe.2120. The method of any of - claims 18 , wherein the therapy is the treatment of prostate cancer.2220. The method of any of - claims 18 , wherein the therapy is the treatment of Parkinson's disease or Alzheimer's disease.24. The kit of claim 23 , wherein X is S and Ris OH or NH.25. The kit of claim 23 , wherein X is O and Ris OH claim 23 , NHor NHMe.2625. The kit of any of - claims 23 , wherein the kit further comprises instructions for use.27. The kit of any of claim 26 , wherein the instructions are for use of the compound in the treatment of prostate cancer.28. The kit of claim 26 , wherein the instructions are for use of the compound in the treatment of Parkinson's disease or Alzheimer's disease.30. The unit dosage form of claim 29 , wherein X is S and Ris OH or NH.31. The unit dosage form of claim 29 , wherein X is O and Ris OH claim 29 , NHor NHMe.33. The ...

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Номер записи: 9
26-12-2013 дата публикации

Process for preparing biphenyl imidazole compounds

Номер: US20130345437A1
Автор: Gene Timothy Fass, Pierre-Jean Colson, Weijiang Zhang
Принадлежит: Theravance Inc

The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R 1-3 are as defined in the specification.

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Номер записи: 10
23-01-2014 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20140024835A1
Автор: Allegretti Paul, Choi Seok-ki, Fatheree Paul R., Gendron Roland, Jendza Keith, McKinnell Robert Murray, McMurtrie Darren, Olson Brooke
Принадлежит: THERAVANCE, INC.

The invention is directed to compounds having the formula: 14-. (canceled)5. The process of claim 33 , wherein Ris selected from —COOH claim 33 , —SONHR claim 33 , and tetrazol-5-yl.6. (canceled)7. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —N— claim 33 , Q is —N— and W is a bond.8. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —CH— claim 33 , Q is —C(R)— and W is —C(O)—.9. The process of claim 33 , wherein Y represents —N— claim 33 , Z is —C(R)— claim 33 , Q is —C(R)— and W is a bond.10. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —CH— claim 33 , Q is —N— and W is a bond.11. The process of claim 33 , wherein Ris selected from H claim 33 , halo claim 33 , —Calkyl claim 33 , —Ccycloalkyl claim 33 , and —Calkylene-OR.12. The process of claim 33 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 33 , where Ris —Calkyl.1314-. (canceled)15. The process of claim 33 , wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; and —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—.16. The process of claim 15 , wherein X is selected from ...

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Номер записи: 11
06-02-2014 дата публикации

Oligomer-Containing Hydantoin Compounds

Номер: US20140039020A1
Автор: Allums-Donald Stephanie, Riggs-Sauthier Jennifer
Принадлежит: Nektar Therapeutics

The invention relates to (among other things) oligomer-containing hydantoin compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer. 1. A compound comprising a hydantoin residue covalently attached via a linkage to a water-soluble , non-peptidic oligomer.5. The compound of claim 1 , wherein the hydantoin residue is a residue of a hydantoin moiety selected from the group consisting of ethotoin claim 1 , mephenyloin claim 1 , phenyloin and fosphenyloin.6. The compound of claim 5 , wherein the hydantoin residue is a residue of phenyloin.7. The compound of claim 1 , wherein the water-soluble claim 1 , non-peptidic oligomer is a poly(alkylene oxide).8. The compound of claim 7 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).9. The compound of claim 1 , wherein water-soluble claim 1 , non-peptidic oligomer has from about 1 to about 30 monomers.10. The compound of claim 9 , wherein the water-soluble claim 9 , non-peptidic oligomer has from about 1 to about 10 monomers.11. The compound of claim 7 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.12. The compound of claim 1 , wherein a single water-soluble claim 1 , non-peptidic oligomer is attached to the hydantoin residue.13. The compound of claim 1 , wherein more than one water-soluble claim 1 , non-peptidic oligomer is attached to the hydantoin residue.14. The compound of claim 1 , wherein the linkage is a stable linkage.15. The compound of claim 1 , wherein the linkage is a releasable linkage.16. A composition comprising a compound comprising a hydantoin residue covalently attached via a linkage to a water-soluble claim 1 , non-peptidic oligomer claim 1 , and optionally claim 1 , a pharmaceutically acceptable excipient.17. A composition of matter comprising a compound comprising a hydantoin residue covalently attached via a linkage to a water- ...

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Номер записи: 12
27-02-2014 дата публикации

CIS-ALKOXY-SUBSTITUTED SPIROCYCLIC 1-H-PYRROLIDINE-2,4-DIONE DERIVATIVES

Номер: US20140058114A1
Автор: FISCHER Reiner, Himmler Thomas, Schatterer Albert
Принадлежит: Bayer Intellectual Property GmbH

Process for preparing cis-alkoxy-substituted spirocyclic 1-H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof. 2. The process according to claim 1 , where A represents C-C-alkyl.3. The process according to claim 1 , where A represents methyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , butyl or isobutyl.4. The process according to claim 1 , where A represents methyl.5. The process according to claim 1 , wherein lithium hydroxide claim 1 , sodium hydroxide claim 1 , potassium hydroxide claim 1 , cesium hydroxide claim 1 , magnesium hydroxide claim 1 , rubidium hydroxide claim 1 , calcium hydroxide or barium hydroxide is used.9. A hydrate of a compound of formula (cis-IV) according to . The present invention relates to processes for preparing cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof.Alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the general formula (I) having acaricidal, insecticidal and herbicidal action are known: EP-A 596 298, WO95/20572, WO 95/26954, WO 95/20572, EP-A 668 267, WO 96/25395, WO 96/35664, WO 97/01535, WO 97/02243, WO 97/36868, WO 98/05638, WO 99/43649, WO 99/48869, WO 99/55673, WO 01/74770, WO 01/96333, WO 03/035643, WO 04/007448, WO 04/065366, WO 04/111042, WO 05/066125, WO 05/049569, WO 05/044796, WO 05/092897, WO 06/056282, WO 06/056281, WO 06/029799, WO 07/096058, WO 08/067910, WO 08/138551, WO 10/102758.Such compounds are usually prepared starting with the corresponding cis-substituted hydantoins of the formula (cis-II).In the formulae (I), (II) and (cis-II),It is already known that in particular the cis-substituted compounds of the formula (I) have biologically advantageous properties (activity, toxicological profile) (WO2004/007448). Accordingly, there is an increased demand for cis-substituted hydantoins of the formula (cis-II) as starting materials.However, owing ...

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Номер записи: 13
04-01-2018 дата публикации

5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS

Номер: US20180002293A1
Автор: ALVEY Luke Jonathan, Amantini David, BREBION Franck Laurent, DE CEUNINCK Frédéric André, DEPREZ Pierre Marc Marie Joseph, Gosmini Romain Luc Marie, JARY Hélène Marie, PEIXOTO Christophe, POP-BOTEZ Iuliana Ecaterina, VARIN Marie Laurence Claire
Принадлежит:

The present invention discloses compounds according to Formula I: 3. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris H.4. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris Calkyl.5. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris Cmonocyclic cycloalkyl.7. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Ris Calkyl.9. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein each R claim 1 , and Ris independently selected from H or CH.10. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Cy is 6-10 membered aryl claim 1 , substituted with one or more independently selected Rgroups.11. The compound or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Cy is phenyl substituted with one or more independently selected Rgroups.12. The compound or pharmaceutically acceptable salt thereof claim 10 , according to claim 10 , wherein each Ris F claim 10 , Cl claim 10 , CN claim 10 , CH claim 10 , or NO.13. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is5-[3-[(3S)-4-(3-chloro-4-fluoro-phenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,5-[3-[(3S)-4-(3-chloro-5-fluoro-phenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,(5S)-5-cyclopropyl-5-[3-[(3S)-4-(3,4-dichlorophenyl)-3-methyl-piperazin-1-yl]-3-oxo-propyl]imidazolidine-2,4-dione,(5S)-5-cyclopropyl-5-[(2S)-3-[(3S)-4-(3,4-difluorophenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]imidazolidine-2,4-dione,5-[3-[(3S)-4-(4-chlorophenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,5-[3-[4-(3,4-difluorophenyl)piperazin-1-yl]-2- ...

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Номер записи: 14
20-01-2022 дата публикации

DOCK1-INHIBITING COMPOUND AND USE THEREOF

Номер: US20220017486A1
Автор: FUKUI Yoshinori, KANAI Motomu, OISAKI Kounosuke, TSUTSUMI Ryosuke, URUNO Takehito
Принадлежит: Kyushu University, National University Corporation

Provided is a compound that is usable as an active ingredient of an anticancer agent. Preferably provided is a compound that has DOCK1-inhibiting activity and exerts an anticancer effect based on the activity. A compound represented by the following formula (A) or a salt thereof: 4. A compound selected from the group consisting of the following compounds:(A1) methyl 1-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrole-2-carboxylate;(A2) 2-(2-acetyl-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrol-1-yl)-1-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethane-1-one;(A3) 1-(1-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrol-2-yl)propan-1-one;(A4) N,N-dimethyl-1-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrole-2-carboxamide;(A5) 2-(2-(oxazol-2-yl)-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrol-1-yl)-1-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethan-1-one;(A6) methyl 1-(2-hydroxy-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrole-2-carboxylate;(A7) 2-(2-(hydroxymethyl)-4-(pyrrolidin-1-yl-sulfonyl)-1H-pyrrol-1-yl)-1-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethan-1-ol;(A8) 2-(pyrrolidin-1-yl-sulfonyl)-6-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)indolizin-8-yl acetate; and 'a salt thereof.', '(A9) 3-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)-5-((phenylsulfonyl)methyl)imidazolidine-2,4-dione; or'}8. A compound selected from the group consisting of the following compounds:(B1) 5-((4-(4-(anthracen-9-yl)phenyl)piperidin-1-yl)sulfonyl)-1-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)pyridin-2(1H)-one,(B2) 1-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl)-5-((4-(3′,4′,5′-trifluoro-[1,1′-biphenyl]-4-yl)piperidin-1-yl)sulfonyl)pyridin-2(1H)-one,(B3) 5-((4-([1,1′:4′,1″:4″,1′″-quaterphenyl]-4-yl)piperidin-1-yl)sulfonyl)-1-(2-oxo-2-(3′-(trifluoromethyl)-[1,1′-biphenyl]-4-yl)ethyl ...

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Номер записи: 15
12-01-2017 дата публикации

ETHYNYL DERIVATIVES

Номер: US20170008854A1
Автор: Biemans Barbara, Guba Wolfgang, Jaeschke Georg, Ricci Antonio, Rueher Daniel, Vieira Eric
Принадлежит: Hoffmann-La Roche Inc.

The present invention relates to compounds useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2. 3. A compound of formula I according to claim 1 , wherein the compound is3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-1-isopropyl-imidazolidine-2,4-dione(5RS)-3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-1-isopropyl-5-methyl-imidazolidine-2,4-dione3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-1-isopropyl-5,5-dimethyl-imidazolidine-2,4-dione3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-5,5-dimethyl-1-phenyl-imidazolidine-2,4-dione 1-tert-butyl-3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]imidazolidine-2,4-dione1-cyclopropyl-3-[2,6-difluoro-4-(2-phenylethynyl)phenyl]imidazolidine-2,4-dione or7-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-5-isopropyl-2-oxa-5,7-diazaspiro[3.4]octane-6,8-dione.5. A compound of formula I according to claim 1 , wherein the compound is(5RS,8aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-5-methyl-5,6,8,8a-tetrahydroimidazo[5,1-c][1,4]oxazine-1,3-dione(3aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-3a,4-dihydroimidazo[1,5-a]indole-1,3-dione(3aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-4,5-dihydro-3aH-imidazo[1,5-a]quinoline-1,3-dione(10aRS)-2-[2,6-difluoro-4-(2-phenylethynyl)phenyl]-10,10a-dihydro-5H-imidazo[1,5-b]isoquinoline-1,3-dione(5RS,8aRS)-2-[2-chloro-4-(2-phenylethynyl)phenyl]-5-methyl-6,7,8,8a-tetrahydro-5H-imidazo[1,5-a]pyridine-1,3-dione or(5RS,8aRS)-2-[2-chloro-6-fluoro-4-[2-(3-pyridyl)ethynyl]phenyl]-5-methyl-6,7,8,8a-tetrahydro-5H-imidazo[1,5-a]pyridine-1,3-dione.7. A pharmaceutical composition comprising a compound of formula I according to and a pharmaceutically acceptable excipient.8. A method for the treatment of Parkinson's disease claim 1 , anxiety claim 1 , emesis claim 1 , obsessive compulsive disorder claim 1 , autism claim 1 , neuroprotection claim 1 , cancer claim 1 , depression claim 1 , schizophrenia and diabetes type 2 of a ...

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Номер записи: 16
09-01-2020 дата публикации

COMPOUNDS USEFUL AS MODULATORS OF TRPM8

Номер: US20200010425A1
Автор: Boren Brant Clayton, Chumakov Volodymyr, Chumakova Lyudmyla, Hammaker Jeffrey Robert, Karanewsky Donald, Kimmich Rachel, Noncovich Alain, Patron Andrew, Priest Chad, Ung Jane, Zhao Wen
Принадлежит:

The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations. 2. The compound of claim 1 , wherein either Ror Ris C-Calkyl claim 1 , and the remaining Ror Ris selected from the group consisting of optionally substituted alkyl claim 1 , optionally substituted alkenyl claim 1 , optionally substituted alkynyl claim 1 , optionally substituted alkylaryl claim 1 , optionally substituted heteroalkyl claim 1 , optionally substituted carbocyclyl claim 1 , and optionally substituted heterocyclyl; or alternatively claim 1 , Rand R claim 1 , taken together with the atoms to which they are attached claim 1 , form an optionally substituted carbocyclic ring;{'sup': '1', 'X and Xare N;'}{'sup': 8', '9', '9', '9', '9, 'Ris selected from the group consisting of -alkylene-carbonyl-aryl, -alkylene-carbonyl-heteroaryl, -alkylene-carbonyl-(substituted aryl), -alkylene-carbonyl-(substituted heteroaryl), -alkylene-carbonyl-O-aryl, -alkylene-carbonyl-O-(substituted aryl), -alkylene-carbonyl-NR-aryl, -alkylene-carbonyl-NR-(substituted aryl), -alkylene-carbonyl-O-heteroaryl, -alkylene-carbonyl-O-(substituted heteroaryl), -alkylene-carbonyl-NR-heteroaryl, and -alkylene-carbonyl-NR-(substituted heteroaryl);'}{'sup': '9', 'Ris selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted acylamido, and optionally substituted diacylamido;'}A is O;{'sub': '2', 'B is CH, or C═O; and'}C is a covalent bond.4. The compound of claim 3 , wherein{'sup': 5', '6', '5', '6', '5', '6, 'sub': 1 ...

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Номер записи: 17
11-01-2018 дата публикации

Ionic Liquid, Lubricant, and Magnetic Recording Medium

Номер: US20180012623A1
Автор: Baghel Pankaj, Hatsuda Kouki, Kondo Hirofumi, Tano Nobuo
Принадлежит:

A lubricant including an ionic liquid including a conjugate base and a conjugate acid, wherein the conjugate acid includes a straight-chain hydrocarbon group having 6 or greater carbon atoms and a straight chain hydrocarbon group s having 6 or greater but 14 or less carbon atoms, and wherein a pKa of an acid that is a source of the conjugate base in acetonitrile is 10 or less. 1. A lubricant comprising:an ionic liquid including a conjugate base and a conjugate acid,wherein the conjugate acid includes a straight-chain hydrocarbon group having 6 or greater carbon atoms and a straight-chain hydrocarbon group having 6 or greater but 14 or less carbon atoms, andwherein a pKa of an acid that is a source of the conjugate base in acetonitrile is 10 or less.5. A magnetic recording medium comprising:a non-magnetic support;a magnetic layer disposed on the non-magnetic support; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the lubricant according to , disposed on the magnetic layer.'}6. An ionic liquid comprising:a conjugate base; anda conjugate acid,wherein the conjugate acid includes a straight-chain hydrocarbon group having 6 or greater carbon atoms and a straight-chain hydrocarbon group having 6 or greater but 14 or less carbon atoms, andwherein a pKa of an acid that is a source of the conjugate base in acetonitrile is 10 or less. The present invention relates to an ionic liquid, a lubricant containing the ionic liquid, and a magnetic recording medium using the lubricant.Conventionally, in a thin film magnetic recording medium, a lubricant is applied onto a surface of a magnetic layer for the purpose of reducing frictions between a magnetic head and the surface of the magnetic recording medium, or reducing abrasion. In order to avoid adhesion, such as sticktion, an actual film thickness of the lubricant is of a molecular order. Accordingly, it is not exaggeration to say that the most important thing for a thin film magnetic recording medium is to select a lubricant ...

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Номер записи: 18
21-01-2016 дата публикации

HETEROCYCLIC INHIBITORS OF THE SODIUM CHANNEL

Номер: US20160016939A1
Автор: Holland Richard, Lamontagne Jason, PAJOUHESH Hassan, Pajouhesh Hossein, Whelan Brendan, ZHANG Lingyun
Принадлежит:

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.

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Номер записи: 19
15-01-2015 дата публикации

IMIDAZOLIDINEDIONE DERIVATIVES

Номер: US20150018377A1
Автор: Alvaro Giuseppe, Decor Anne, FONTANA Stefano, HAMPRECHT Dieter, Large Charles, MARASCO Agostino
Принадлежит: AUTIFONY THERAPEUTICS LIMITED

The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy. 114-. (canceled) This application is a continuation of U.S. application Ser. No. 13/515,097 (U.S. Pat. No. 8,722,695 issued May 13, 2014), filed Jun. 11, 2012 (published as US 2012-0289526 A1), which is a U.S. national phase of International Application No. PCT/EP2010/068946 filed 6 Dec. 2010, which designated the U.S. and claims priority to GB 0921760.5 filed 11 Dec. 2009 and GB 1012924.5 filed 30 Jul. 2010, the entire contents of each of which are hereby incorporated by reference.This invention relates to novel compounds, pharmaceutical compositions containing them and their use in therapy, in particular as antipsychotic agents.The Kv3 voltage-gated potassium channel family includes four members, Kv3.1, Kv3.2, KV3.3, and Kv3.4. Genes for each of these subtypes can generate multiple isoforms by alternative splicing, producing versions with different C-terminal domains. Thirteen isoforms have been identified in mammals to date, but the currents expressed by these variants appear identical (Rudy and McBain, 2001, Trends in Neurosciences 24, 517-526). Kv3 channels are activated by depolarization of the plasma membrane to voltages more positive than −20 mV; furthermore, the channels deactivate rapidly upon repolarization of the membrane. These biophysical properties ensure that the channels open towards the peak of the depolarizing phase of the neuronal action potential to initiate repolarization. Rapid termination of the action potential mediated by Kv3 channels allows the neuron to recover more quickly to reach sub-threshold membrane potentials from ...

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Номер записи: 20
17-01-2019 дата публикации

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

Номер: US20190016669A1
Автор: BENENATO Kerry E., CORNEBISE Mark
Принадлежит:

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression. 2. The compound of claim 1 , wherein Ris selected from the group consisting of NH claim 1 , alkylamino claim 1 , and dialkylamino.3. The compound of claim 1 , wherein Ris selected from the group consisting of methylamino claim 1 , and dimethylamino.4. The compound of claim 1 , wherein Rand Rare the same.5. The compound of claim 4 , wherein Rand Rare Calkyl.6. The compound of claim 1 , wherein n is 3.8. The compound of claim 7 , wherein R′ is C9 alkyl.9. The compound of claim 7 , wherein l is 5.10. The compound of claim 7 , wherein o is 5.11. The compound of claim 7 , wherein Ris selected from the group consisting of NH claim 7 , alkylamino claim 7 , and dialkylamino.12. The compound of claim 7 , wherein Ris selected from the group consisting of methylamino and dimethylamino.14. A nanoparticle composition comprising a lipid component comprising a compound of .15. The nanoparticle composition of claim 14 , wherein the lipid component further comprises a phospholipid selected from the group consisting of 1 claim 14 ,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC) claim 14 , 1 claim 14 ,2-dimyristoyl-sn-glycero-phosphocholine (DMPC) claim 14 , 1 claim 14 ,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) claim 14 , 1 claim 14 ,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) claim 14 , 1 claim 14 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 14 , 1 claim 14 ,2-diundecanoyl-sn-glycero-phosphocholine (DUPC) claim 14 , 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) claim 14 , 1 claim 14 ,2-di-O-octadecenyl-sn ...

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Номер записи: 21
16-01-2020 дата публикации

HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING

Номер: US20200017449A1
Автор: Bredesen Dale E., John Varghese
Принадлежит:

In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. 2126.-. (canceled) This application is a continuation of U.S. Ser. No. 14/764,107, filed Jul. 28, 2015, which is a U.S. 371 National Phase of PCT/US2014/016100, filed Feb. 12, 2014, which claims benefit of and priority to U.S. Ser. No. 61/763,830, filed on Feb. 12, 2013, all of which are incorporated herein by reference in their entirety for all purposes.[Not Applicable]Amyloid beta peptide (Aβ) is a primary component of beta amyloid fibrils and plaques, which are regarded as having a role in an increasing number of pathologies. Examples of such pathologies include, but are not limited to, Alzheimer's disease, Down's syndrome, Parkinson's disease, memory loss (including memory loss associated with Alzheimer's disease and Parkinson's disease), attention deficit symptoms (including attention deficit symptoms associated with Alzheimer's disease, Parkinson's disease, and Down's syndrome), dementia (including pre-senile dementia, senile dementia, dementia associated with Alzheimer's disease, Parkinson's disease, and Down's syndrome), progressive supranuclear palsy, cortical basal degeneration, neurodegeneration, olfactory impairment (including olfactory impairment associated with Alzheimer's disease, Parkinson's disease, and Down's syndrome), β-amyloid angiopathy (including cerebral amyloid angiopathy), hereditary cerebral ...

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Номер записи: 22
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.

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Номер записи: 23
26-01-2017 дата публикации

NEPRILYSIN INHIBITORS

Номер: US20170020904A1
Автор: Fleury Melissa, Gendron Roland, Hughes Adam D.
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

In one aspect, the invention relates to compounds having the formula: 131-. (canceled)32: A compound selected from:(a) (2R,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(b) (2S,4S)-5-(2′-Fluorobiphenyl-4-yl)-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(c) (2S,4S)-5-(3′-Fluorobiphenyl-4-yl)-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(d) (2S,4S)-5-(3′-Fluorobiphenyl-4-yl)-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid ethyl ester;(e) (2S,4S)-5-(3′-Fluorobiphenyl-4-yl)-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-methoxy-ethyl ester;(f) (2S,4S)-5-(3′-Fluorobiphenyl-4-yl)-2-hydroxymethyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-(2-methoxy-ethoxy)-ethyl ester;(g) (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(1-hydroxy-1H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(h) (2S,4S)-5-(2′-Fluorobiphenyl-4-yl)-2-hydroxymethyl-4-[(1-hydroxy-1H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(i) (2S,4S)-5-(3′-Chloro-biphenyl-4-yl)-2-hydroxymethyl-4-[(1H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(j) (2S,4S)-5-(3′-Chloro-biphenyl-4-yl)-2-hydroxymethyl-4-[(1-hydroxy-1H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(k) (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(1H-[1,2,4]triazole-3-carbonyl)-amino]-pentanoic acid;(l) (S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(2H-[1,2,4]triazole-3-carbonyl)-amino]-pentanoic acid;(m) (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(5-methyl-2H-[1,2,4]triazole-3-carbonyl)-amino]-pentanoic acid;(n) (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(5-hydroxy-2H-[1,2,4]triazole-3-carbonyl)-amino]-pentanoic acid;(o) (2S,4S)-5-Biphenyl-4-yl-2-hydroxymethyl-4-[(5-hydroxy-2H-[1,2,4]triazole-3-carbonyl)-amino]-pentanoic acid ethyl ester;(p) (2S,4S)-4-[(5-Chloro-2H-[1,2,4]triazole-3-carbonyl)-amino]-5-(2′-fluorobiphenyl-4-yl)-2-hydroxymethyl-pentanoic acid;(q) (2S,4S)-5-Biphenyl-4- ...

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Номер записи: 24
25-01-2018 дата публикации

IMIDAZOLIDINEDIONE DERIVATIVES

Номер: US20180021336A1
Автор: Alvaro Giuseppe, Decor Anne, FONTANA Stefano, HAMPRECHT Dieter, Large Charles, MARASCO Agostino
Принадлежит:

The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy. 2. The method according to wherein Ris halo claim 1 , Calkyl or Calkoxy claim 1 , halo-Calkoxy claim 1 , or cyano and Ris H claim 1 , halo claim 1 , Calkyl and Calkoxy; with the proviso that when R2 is H claim 1 , R1 is not in the para position; or a pharmaceutically acceptable salt thereof.3. The method according to wherein Ris halo claim 1 , Calkyl or Calkoxy; or a pharmaceutically acceptable salt thereof.4. The method according to wherein Ris Calkyl claim 1 , Calkoxy claim 1 , or halo-Calkoxy; Ris H claim 1 , cyano or alkyl; X is N claim 1 , Y is N or CH claim 1 , Ris Calkyl claim 1 , and Ris Calkyl or H; or a pharmaceutically acceptable salt thereof.5. The method according to wherein Ris propyl claim 1 , butyl claim 1 , methoxy claim 1 , propoxy claim 1 , or trifluoromethoxy; Ris H claim 1 , cyano or methyl; X is N claim 1 , Y is N or CH claim 1 , Ris ethyl claim 1 , and Ris methyl or H; or a pharmaceutically acceptable salt thereof.6. The method according to wherein the compound of formula (Ia) selected from the group consisting of:(5R)-5-methyl-3-{4-[(3-methylphenyl)oxy]phenyl}-2,4-imidazolidinedione;(5R)-5-methyl-3-(4-{[3-(methyloxy)phenyl]oxy}phenyl)-2,4-imidazolidinedione;(5R)-3-(4-{[3-(ethyloxy)phenyl]oxy}phenyl)-5-methyl-2,4-imidazolidinedione;(5R)-3-{4-[(3-chloro-5-fluorophenyl)oxy]phenyl}-5-methyl-2,4-imidazolidinedione;(5R)-3-{4-[(3-chloro-4-fluorophenyl)oxy]phenyl}-5-methyl-2,4-imidazolidinedione;(5S)-3-{4-[(3-chloro-4-fluorophenyl)oxy]phenyl}-5-methyl-2,4-imidazolidinedione;(5R)-5-methyl-3-(4-{[2-methyl-5-(methyloxy)phenyl]oxy}phenyl)-2 ...

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Номер записи: 25
24-01-2019 дата публикации

Inhibitors of cellular necrosis and related methods

Номер: US20190023690A1
Автор: Dawei Ma, Junying Yuan, Shan QIAN, Yijun Zhou
Принадлежит: Harvard College, Shanghai Institute of Organic Chemistry of CAS

A compound having the following structure (I): or a pharmaceutically acceptable salt, prodrug, stereoisomer or tautomer thereof, is provided. Related compounds, methods for preparation of the same and uses of the compounds for treatment of various indications, including treatment of necrotic cell diseases and/or inflammation, are also provided.

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Номер записи: 26
24-01-2019 дата публикации

SHIP1 MODULATORS AND METHODS RELATED THERETO

Номер: US20190023709A1
Автор: Bogucki David, Harwig Curtis, Mackenzie Lloyd F., Pettigrew Jeremy D., Raymond Jeffery R.
Принадлежит:

Compounds of formula (I): 2. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is substituted with one hydrogen;C14 is substituted with one hydrogen;C15 is substituted with two hydrogens;{'sup': 1', '8', '9, 'Ris —R—OR;'}{'sup': 2', '8', '9, 'Ris —R—OR;'}{'sup': 4a', '4b', '7', '3, 'sub': 2', '2', '2', '2', '3', '3, 'Ris hydrogen or alkyl, Ris a direct bond to the carbon to which Ris attached, and Ris —CHNHor —CHN(H)C(O)(CH)CH;'}{'sup': '5', 'Ris alkyl;'}{'sup': '6', 'Ris hydrogen;'}{'sup': '7', 'Ris hydrogen;'}{'sup': '8', 'each Ris independently a direct bond or a straight or branched alkylene chain; and'}{'sup': '9', 'each Ris independently hydrogen, alkyl, haloalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heterocyclyl, optionally substituted heterocyclylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl.'}3. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is substituted with one hydrogen;C14 is substituted with one hydrogen;C15 is substituted with two hydrogens;{'sup': '1', 'Ris —OH;'}{'sup': '2', 'sub': '2', 'Ris —CH—OH;'}{'sup': 4a', '4b', '7', '3, 'sub': 2', '2', '2', '2', '3', '3, 'Ris hydrogen or methyl, Ris a direct bond to the carbon to which Ris attached, and Ris —CHNHor —CHN(H)C(O)(CH)CH;'}{'sup': '5', 'Ris methyl;'}{'sup': '6', 'Ris hydrogen; and'}{'sup': '7', 'Ris hydrogen.'}4. The compound of selected from:(1S,3S,4R)-4-((3aS,6S,7R,7aS)-7-(aminomethyl)-3,3a-dimethyl-3a,4,5,6,7,7a-hexahydro-1H-inden-6-yl)-3-(hydroxymethyl)-4-methylcyclohexanol; andN-(((3aR,6S,7R,7aS)-6-((1R,2S,4S)-4-hydroxy-2-(hydroxymethyl)-1-methylcyclohexyl)-3a-methyl-3a,4,5,6,7,7a-hexahydro-1H-inden-7-yl)methyl)pentanamide.6. The compound of wherein:C1, C4, C11 and C12 are each independently substituted with two hydrogens;C9 is ...

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Номер записи: 27
28-01-2021 дата публикации

N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE

Номер: US20210024516A1
Автор: Andre Patrick, Bergnes Gustave, CHA Jacob, CHEN Chun, HALCOMB Randall, HOM Timothy, JIANG Lan, JR. David John, Li Hui, Morgans
Принадлежит:

The invention relates to compounds of formula (I): 2. The compound of claim 1 , or a salt thereof claim 1 , wherein Ris a fused bicyclic C-Caryl optionally substituted by Ror a fused bicyclic 7- to 10-membered heteroaryl optionally substituted by R.3. The compound of or claim 1 , or a salt thereof claim 1 , wherein Ris a fused bicyclic 7- to 10-membered heteroaryl optionally substituted by R.4. The compound of claim 3 , or a salt thereof claim 3 , wherein Ris indazolyl optionally substituted by R claim 3 , benzimidazolyl optionally substituted by R claim 3 , or benzoxazolyl optionally substituted by R.5. The compound of claim 1 , or a salt thereof claim 1 , wherein Ris phenyl optionally substituted by R.6. The compound of claim 1 , or a salt thereof claim 1 , wherein Ris a monocyclic 5- or 6-membered heteroaryl optionally substituted by R.7. The compound of any one of to claim 1 , or a salt thereof claim 1 , wherein the -A-L-moiety is -A-L-.8. The compound of claim 7 , or a salt thereof claim 7 , wherein Ais C-Carylene optionally substituted by R.9. The compound of claim 7 , or a salt thereof claim 7 , wherein Ais C-Ccycloalkylene optionally substituted by R.10. The compound of claim 7 , or a salt thereof claim 7 , wherein Ais 5- to 10-membered heteroarylene optionally substituted by R.11. The compound of claim 7 , or a salt thereof claim 7 , wherein Ais 3- to 12-membered heterocyclylene optionally substituted by R.12. The compound of claim 7 , or a salt thereof claim 7 , wherein Ais selected from the group consisting of 1 claim 7 ,4-phenylene claim 7 , 1 claim 7 ,3-phenylene claim 7 , 1 claim 7 ,1-cyclopropylene claim 7 , 1 claim 7 ,2-cyclopropylene claim 7 , 1 claim 7 ,3-cyclobutylene claim 7 , 1 claim 7 ,4-cyclohexylene claim 7 , 1 claim 7 ,3-azetidinylene claim 7 , 1 claim 7 ,3-pyrrolidinylene claim 7 , and 2 claim 7 ,5-benzo[d]oxazolylene.13. The compound of any one of to claim 7 , or a salt thereof claim 7 , wherein Lis —O—Z— claim 7 , —O—Z—X— claim 7 , —O—Y— ...

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Номер записи: 28
28-01-2021 дата публикации

PSMA Imaging Agents

Номер: US20210024574A1
Автор: Chen Gang, Gangadharmath Umesh B., Kasi Dhanalakshmi, Kolb Hartmuth C., Liu Changhui, Mocharla Vani P., Sinha Anjana, Szardenings Anna Katrin, Walsh Joseph C., Wang Eric, Yu Chul, ZHANG Wei, Zhao Tieming
Принадлежит:

Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging. 2. The compound of claim 1 , wherein in Formula VI claim 1 , Xis N.3. The compound of claim 1 , wherein in Formula VI claim 1 , Xis H and Xis (CH)—Rwherein at least one CHof (CH)is replaced by CONH.4. The compound of claim 1 , wherein in Formula VI claim 1 , Xis H and Xis (CH)—Rwherein at least one CHof (CH)is replaced by CONH.5. The compound of claim 1 , wherein in Formula VI claim 1 , at least one CHof (CH)—Rof either Xor Xis replaced by triazole.6. The compound of claim 1 , wherein in Formula VI claim 1 , Ris a radioisotope.8. The compound of claim 7 , wherein in Formula VIII claim 7 , Xis CH.9. The compound of claim 7 , wherein in Formula VIII claim 7 , Xis CH.10. The compound of claim 7 , wherein in Formula VIII claim 7 , at least one CHof (CH)is optionally replaced by O.11. The compound of claim 7 , wherein in Formula VIII claim 7 , Xis N.12. The compound of claim 7 , wherein in Formula VIII claim 7 , Xis CH.14. The method of claim 13 , wherein in Formula VI claim 13 , Xis N.15. The method of claim 13 , wherein in Formula VI claim 13 , Xis H and Xis (CH)—Rwherein at least one CHof (CH)is replaced by CONH.16. The method of claim 13 , wherein in Formula VI claim 13 , Xis H and Xis (CH)—Rwherein at least one CHof (CH)is replaced by CONH.17. The method of claim 13 , wherein in Formula VI claim 13 , at least one CHof (CH)—Rof either Xor Xis replaced by triazole.18. The method of claim 13 , wherein in Formula VI claim 13 , Ris a radioisotope.19. The method of claim 13 , wherein in Formula VIII claim 13 , Xis CH.20. The method of claim 13 , wherein in Formula VIII claim 13 , Xis CH.21. The method of claim 13 , wherein in Formula VIII claim 13 , at least one CHof (CH)is optionally replaced ...

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Номер записи: 29
17-02-2022 дата публикации

METHOD FOR PRODUCING METHIONINE

Номер: US20220048855A1
Автор: BINDERNAGEL Ulf, HIEROLD Judith, Moussallem Imad, Renner Christian, ROTH Philipp, SUDHOFF Daniel
Принадлежит: EVONIK OPERATIONS GMBH

The present invention pertains to a method for producing methionine or salts or derivatives thereof from hydrogen cyanide (HCN), the method comprising a step of producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN), or a crude product mixture comprising MMP-CN, by contacting a hydrogen cyanide (HCN) process gas mixture prepared according to the Andrussow process from methane, ammonia and oxygen, with 3-methylmercaptopropionaldehyde (MMP), wherein the HCN process gas mixture is obtained from the crude HCN process gas mixture by adjusting the amount of ammonia to between 20% (v/v) and 60% (v/v) of the amount of the ammonia in the crude HCN process gas mixture. 17-. (canceled)8. A method for producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN) , comprising: contacting a hydrogen cyanide (HCN) process gas mixture prepared according to the Andrussow process from methane , ammonia and oxygen , with 3-methylmercaptopropionaldehyde (MMP) , wherein the HCN process gas mixture is obtained from a crude HCN process gas mixture by adjusting the amount of ammonia to between 20% (v/v) and 60% (v/v) of the amount of the ammonia in the crude HCN process gas mixture.9. The method of claim 8 , wherein the ammonia adjustment is performed using an ammonia scrubber equipped with a bypass stream.10. The method of claim 8 , wherein the ammonia adjustment is performed using an ammonia scrubber enabling a partial ammonia breakthrough.11. The method of claim 8 , wherein the amount of ammonia in the HCN process gas mixture is adjusted to a maximum of 40% (v/v) of the ammonia in the crude HCN process gas mixture by passing a maximum of 40% (v/v) of the crude HCN gas mixture from the ammonia scrubber.12. A method for producing methionine or salts or derivatives thereof from HCN claim 8 , the method comprising: producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN) claim 8 , or a crude product mixture comprising MMP-CN claim 8 , by contacting a hydrogen cyanide (HCN) process gas mixture ...

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Номер записи: 30
04-02-2021 дата публикации

PSMA Imaging Agents

Номер: US20210032286A1
Автор: Chen Gang, Gangadharmath Umesh B., Kasi Dhanalakshmi, Kolb Hartmuth C., Liu Changhui, Mocharla Vani P., Sinha Anjana, Szardenings Anna Katrin, Walsh Joseph C., Wang Eric, Yu Chul, ZHANG Wei, Zhao Tieming
Принадлежит:

Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging. 2. The method of claim 1 , wherein in Formula IV claim 1 , Xis NH.4. The method of claim 1 , wherein in Formula IV claim 1 , Xis an aryl.6. The method of claim 1 , wherein in Formula IV claim 1 , Xis a single bond.7. The method of claim 1 , wherein in Formula IV claim 1 , Ris a radioisotope.8. The method of claim 1 , wherein in Formula IV claim 1 , Xis C(O) and Xis a sugar.9. The method of claim 1 , wherein in Formula V claim 1 , Xis CH.10. The method of claim 1 , wherein in Formula V claim 1 , Xis N.11. The method of claim 1 , wherein in Formula V claim 1 , Xis CH.12. The method of claim 1 , wherein in Formula V claim 1 , Xis N.13. The method of claim 1 , wherein in Formula V claim 1 , wherein one CHis replaced by an aryl.14. The method of claim 1 , wherein Ris O.15. The method of claim 1 , wherein Ris S.17. The compound of claim 16 , wherein in Formula IV claim 16 , Xis NH.19. The compound of claim 16 , wherein in Formula IV claim 16 , Xis an aryl.21. The compound of claim 16 , wherein in Formula IV claim 16 , Xis a single bond.22. The compound of claim 16 , wherein in Formula IV claim 16 , Ris a radioisotope.23. The compound of claim 16 , wherein in Formula IV claim 16 , Xis C(O) and Xis a sugar.26. The compound of claim 25 , wherein in Formula V claim 25 , Xis CH.27. The compound of claim 25 , wherein in Formula V claim 25 , Xis N.28. The compound of claim 25 , wherein in Formula V claim 25 , Xis CH.29. The compound of claim 25 , wherein in Formula V claim 25 , Xis N.30. The compound of claim 25 , wherein in Formula V claim 25 , wherein one CHis replaced by an aryl.31. The compound of claim 25 , wherein Ris O.32. The compound of claim 25 , wherein Ris S. This Continuation application ...

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Номер записи: 31
05-02-2015 дата публикации

PROCESS FOR PREPARING BIPHENYL IMIDAZOLE COMPOUNDS

Номер: US20150038725A1
Автор: COLSON Pierre-Jean, Fass Gene Timothy, Zhang Weijiang
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention provides processes for preparing intermediates useful for preparing compounds of the formula: 115-. (canceled)17. (canceled)18. Crystalline 4′-(5-aminomethyl-2-ethoxy-4-ethylimidazol-1-ylmethyl)-3′-fluorobiphenyl-2-carboxylic acid t-butyl ester , characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 5.24±0.2 , 10.43±0.2 , 15.65±0.2 , 20.63±0.2 , and 31.91±0.2.19. The compound of claim 18 , wherein the compound is further characterized by comprising one or more additional diffraction peaks at 2θ values selected from 12.74±0.2 claim 18 , 14.90±0.2 claim 18 , 18.20±0.2 claim 18 , 21.71±0.2 claim 18 , 23.03±0.2 claim 18 , 23.96±0.2 claim 18 , and 24.86±0.220. The compound of claim 18 , wherein the compound is characterized by a powder x-ray diffraction pattern in which the peak positions are substantially in accordance with the peak positions of the pattern shown in .21. The compound of claim 18 , wherein the compound is characterized by a differential scanning calorimetry trace which has a melting point at about 76.0° C.22. The compound of claim 18 , wherein the compound is characterized by a differential scanning calorimetry trace substantially in accordance with that shown in .23. A process for preparing the crystalline compound of claim 18 , comprising:a) treating 4′-(5-aminomethyl-2-ethoxy-4-ethylimidazol-1-ylmethyl)-3′-fluorobiphenyl-2-carboxylic acid t-butyl ester with heptanes to complete dissolution;b) cooling to effect crystallization; and{'claim-ref': {'@idref': 'CLM-00018', 'claim 18'}, 'c) isolating the resulting solids to yield the crystalline compound of .'}24. Crystalline 4′-{5-[((S)-2-acetylsulfanyl-4-methylpentanoylamino)methyl]-2-ethoxy-4-ethylimidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid claim 18 , characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 5.24±0.2 claim 18 , 7.16±0.2 claim 18 , 13.68±0.2 claim 18 , and 15.98±0.2.25. The compound ...

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Номер записи: 32
19-02-2015 дата публикации

PACKAGED PRODUCT OF SOLID PREPARATION CONTAINING 5-HYDROXY-1H-IMIDAZOLE-4-CARBOXAMIDE OR SALT THEREOF, OR HYDRATE THEREOF

Номер: US20150051408A1
Автор: NAKANO Shumma
Принадлежит: FUJIFILM Corporation

The present invention provides a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, which comprises the solid preparation and an environment-controlling agent packaged together. The packaged product of present invention is useful as a packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof, or a hydrate thereof, with which discoloration of the solid preparation is suppressed, and superior storage stability of the solid preparation is obtained. 1. A packaged product of a solid preparation containing 5-hydroxy-1H-imidazole-4-carboxamide or a salt thereof , or a hydrate thereof , which comprises the solid preparation and an environment-controlling agent packaged together.2. The packaged product of the solid preparation according to claim 1 , wherein the environment-controlling agent is a desiccant claim 1 , a deoxidant that exhibits a deoxidation function in a dry atmosphere claim 1 , or a deoxidant having both a deoxidation function and a desiccation function.3. The packaged product of the solid preparation according to claim 1 , wherein the environment-controlling agent is a desiccant.4. The packaged product according to claim 2 , wherein the desiccant is silica gel.5. The packaged product according to claim 3 , wherein the desiccant is silica gel.6. The packaged product of the solid preparation according to claim 3 , wherein the deoxidant that exhibits a deoxidation function in a dry atmosphere is further packaged together.7. The packaged product of the solid preparation according to claim 4 , wherein the deoxidant that exhibits a deoxidation function in a dry atmosphere is further packaged together.8. The packaged product of the solid preparation according to claim 2 , wherein the deoxidant that exhibits a deoxidation function in a dry atmosphere is a deoxidant using oxidation of carbon-carbon unsaturated bond.9. The packaged product of ...

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Номер записи: 33
14-02-2019 дата публикации

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Номер: US20190047977A1
Автор: Dominguez Celia, Mitchell William, Prime Michael, Toledo-Sherman Leticia, Went Naomi
Принадлежит:

Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity. 133.-. (canceled)35. The method of claim 34 , wherein said condition or disorder involves a neurodegenerative pathology.36. The method of claim 34 , wherein said condition or disorder is Huntington's Disease.38. The method of claim 37 , wherein said condition or disorder involves a neurodegenerative pathology.39. The method of claim 37 , wherein said condition or disorder is Huntington's Disease. This application is a continuation of U.S. patent application Ser. No. 14/392,307, filed Dec. 23, 2015, which claims the benefit of priority under 35 U.S.C. § 371 of PCT International Application No. PCT/US2014/056887, filed Sep. 23, 2014, which in turn claims the benefit of priority to U.S. Provisional Application No. 61/882,813, filed Sep. 26, 2013, both of which are incorporated herein by reference ...

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Номер записи: 34
22-02-2018 дата публикации

NEPRILYSIN INHIBITORS

Номер: US20180050052A1
Автор: Fleury Melissa, Gendron Roland, Hughes Adam D.
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

In one aspect, the invention relates to compounds having the formula: 131-. (canceled)32: A compound selected from:(a) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid;(b) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid ethyl ester;(c) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester;(d) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-morpholin-4-yl-ethyl ester;(e) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-methoxy-ethyl ester;(f) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-(2-methoxy-ethoxy)-ethyl ester;(g) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-methanesulfonyl-ethyl ester;(h) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid isopropyl ester;(i) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-dimethylamino-ethyl ester;(j) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid butyl ester;(k) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid propyl ester;(l) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 2-piperidin-1-yl-ethyl ester;(m) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid 3-methyl-butyl ester;(n) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-4-[(3H-[1,2,3]triazole-4-carbonyl)-amino]-pentanoic acid pentyl ester;(o) (2S,4R)-5-biphenyl-4-yl-2-hydroxymethyl ...

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Номер записи: 35
26-02-2015 дата публикации

Antiviral Compounds and Uses Thereof

Номер: US20150056164A1
Автор: Betebenner David A., DeGoey David A., Donner Pamela L., FLENTGE Charles A., Hutchinson Douglas K., Kati Warren M., Krueger Allan C., Liu Dachun, Longenecker Kenton L., Maring Clarence J., Pratt John K., Randolph John T., Rockway Todd W., Tufano Michael D., Wagner Rolf
Принадлежит: AbbVie Inc.

This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions. 2. (canceled)3. The compound or salt of claim 1 , wherein Ris selected from the group consisting of hydrogen and methyl.45-. (canceled)7. The compound or salt of claim 6 , wherein m is 0.8. The compound or salt of claim 1 , wherein m is 1.9. The compound or salt of claim 6 , wherein m is 2.10. The compound or salt of claim 6 , wherein m is 3.11. The compound or salt of claim 6 , wherein Ris hydrogen.12. The compound or salt of claim 6 , wherein Ris phenyl.13. The compound or salt of claim 6 , wherein Ris C-C-alkyl.14. The compound or salt of claim 6 , wherein Ris C-C-alkyloxy-carbonyl.15. The compound or salt of claim 1 , wherein Ris selected from the group consisting of C-C-alkyl claim 1 , C-C-carbocyclyl claim 1 , and 5-6-membered heterocyclyl claim 1 , wherein:{'sub': 1', '4, '(a) the C-C-alkyl optionally is substituted with up to three substituents independently selected from the group consisting of halo, oxo, hydroxy, alkyloxy, and trimethylsilyl, and'}{'sub': 3', '6, '(b) the C-C-carbocyclyl and 5-6-membered heterocyclyl optionally are substituted with one or two substituents independently selected from the group consisting of alkyl, halo, and alkylsulfonylamino.'}16. The compound or salt of claim 1 , wherein Ris selected from the group consisting of halo claim 1 , alkyl claim 1 , and alkyloxy.17. The compound or salt of claim 1 , wherein Ris selected from the group consisting of tert-butyl claim 1 , perfluoroethyl claim 1 , trifluoromethyl claim 1 , and 5-6-membered heterocyclyl optionally substituted with methyl.18. The compound or salt ...

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Номер записи: 36
10-03-2022 дата публикации

MILD AND SITE-SELECTIVE 18F-LABELING OF SMALL MOLECULES AND/OR BIOMOLECULES VIA A THIOL-REACTIVE SYNTHON

Номер: US20220072163A1
Автор: Ma Gaoyuan, MURPHY Jennifer M.
Принадлежит: The Regents of the University of California

Site-selective conjugation to biomolecules via thiol-based chemistry is superior to the unselective modification of lysine residues, which produce a mixed product and can potentially interfere with binding affinity of the biomolecule. However, in physiological environments, the maleimide-thiol conjugation product which is the current gold-standard for site-selective thiol-conjugation can be susceptible to hydrolysis or a retro-Michael reaction via exchange with reactive thiols such as those in albumin or glutathione residues yet the degradation is relatively slow. Therefore, for in vivo studies, the maleimide-thiol conjugation proposes instability issues. The compositions and methods disclosed herein provide an alternative thiol-based linkage, one that overcomes the instability issues with conventional reagents and methods. The compositions and methods disclosed herein are useful in various contexts, for example, for F-labeling of peptides/proteins in the preparation of positron emission tomography (PET) probes. 3. The composition of or , wherein:the compound is in a powdered form;the compound comprises at least 90% of the composition; and/orthe composition is disposed within a container of a kit.4. The composition of claim 1 , further comprising an organic solvent.5. The composition of claim 1 , further comprising a [F]fluoride molecule.8. The composition of or claim 1 , further comprising a biomolecule having a —SH moiety.9. The composition of claim 8 , wherein the biomolecule comprises a peptide claim 8 , a protein claim 8 , antibody or a sugar.10. A method of making a F labelled vinyl sulfone comprising:{'sup': '18', 'claim-ref': [{'@idref': 'CLM-00001', '#text': 'claim 1'}, {'@idref': 'CLM-00002', '#text': 'claim 2'}], '#text': 'combining a [F]fluoride radionuclide with at least one compound of or ;'}{'sup': '18', '#text': 'performing a fluorination reaction so that a F labelled vinyl sulfone is made.'}11. A method of coupling a F moiety to a biomolecule to ...

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Номер записи: 37
02-03-2017 дата публикации

Apparatus for producing halohydantoin compound

Номер: US20170056786A1
Автор: Shinji Uchikoshi, Tomohiro Ikegami, Yukihiko Hanamura
Принадлежит: Nippoh Chemicals Co Ltd

A method of the present invention for producing a halohydantoin compound by refining, in a dryer ( 1 ), a composition containing at least one of water and elemental halogen, an organic solvent, and the halohydantoin compound, the method includes the steps of: (i) removing the organic solvent from the composition; and (ii) removing the at least one of the water and the elemental halogen from the composition refined in the step (i).

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Номер записи: 38
04-03-2021 дата публикации

NITROGEN RING LINKED DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20210061767A1
Автор: Ladner Robert D., Spyvee Mark
Принадлежит:

Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. 6. The compound of claim 1 , wherein Lis a bond.7. The compound of claim 1 , wherein Lis —C(R)—.9. A composition comprising a compound of and at least one pharmaceutically acceptable excipient or carrier.10. A method of inhibiting dUTPase claim 1 , wherein the method comprises contacting the dUTPase with an effective amount of the compound of .11. 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; wherein the cancer cell is selected from a colorectal cancer cell claim 1 , a breast cancer cell claim 1 , or a non-small cell lung cancer cell.12. The method of claim 11 , wherein the dUTPase-directed therapeutic is selected from fluoropyrimidines and antifolates.13. A method of treating cancer in a patient whose treatment is impeded by the expression or overexpression of dUTPase claim 1 , comprising administering a therapeutically effective amount of the compound of to the patient claim 1 , wherein the cancer is colorectal cancer claim 1 , breast cancer claim 1 , or non-small cell lung cancer.14. The method of claim 13 , further comprising detecting overexpression of dUTPase in a cell or tissue sample isolated from the patient.15. A method of treating colorectal claim 1 , breast claim 1 , or non-small cell lung cancer in a patient selected for treatment by overexpression of dUTPase in a sample isolated from the patient claim 1 , comprising administering to the patient a therapeutically effective amount of the compound of .16. A kit comprising a compound of claim 1 , and instructions for diagnostic or therapeutic use as described herein. This application is a continuation of U.S. patent application Ser. No. 16/462,173, ...

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Номер записи: 39
05-03-2015 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20150065543A1
Автор: Allegretti Paul, Choi Seok-ki, Fatheree Paul R., Gendron Roland, Jendza Keith, McKinnell Robert Murray, McMurtrie Darren, Olson Brooke
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention is directed to compounds having the formula: 12-. (canceled)5. The method of claim 4 , wherein Ris selected from —COOH claim 4 , —SONHR claim 4 , and tetrazol-5-yl.7. The method of claim 36 , wherein Y represents —C(R)— claim 36 , Z is —N— claim 36 , Q is —N— and W is a bond.8. The method of claim 36 , wherein Y represents —C(R)— claim 36 , Z is —CH— claim 36 , Q is —C(R)— and W is —C(O)—.9. The method of claim 36 , wherein Y represents —N— claim 36 , Z is —C(R)— claim 36 , Q is —C(R)— and W is a bond.10. The method of claim 36 , wherein Y represents —C(R)— claim 36 , Z is —CH— claim 36 , Q is —N— and W is a bond.11. The method of claim 36 , wherein Ris selected from H claim 36 , halo claim 36 , —Calkyl claim 36 , —Ccycloalkyl claim 36 , and —Calkylene-OR.12. The method of claim 36 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 36 , where Ris —Calkyl.13. The method of claim 12 , wherein Ris selected from —Calkyl and —O—Calkyl.14. The method of claim 36 , wherein X is —Calkylene- claim 36 , 1 to 4 —CH— moieties in the alkylene are replaced with a —NR—C(O)— or —C(O)—NR— moiety claim 36 , and Ris selected from H and —OH.15. The method of wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; ...

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Номер записи: 40
22-05-2014 дата публикации

Compositions for Topical Application Having Androgenic Actions

Номер: US20140142124A1
Автор: Bohn Manfred, Kraemer Karl Theodor
Принадлежит:

A composition comprising at least one physiologically tolerated film-forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I 2. A composition as claimed in claim 1 , wherein the compound of formula I is a compound in which:{'sup': '1', 'claim-text': [{'sub': '2', '2) —NOor'}, '3) a halogen;, 'Ris 1) —CN,'}{'sup': '2', 'sub': '3', 'claim-text': '2) a halogen;', 'Ris 1) —CFor'}{'sup': '3', 'claim-text': '2) ═S;', 'Ris 1) ═0 or'}X is the radical of formula II or III, or {'sup': '4', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'in which Ris as defined in ;'}, 'X and Y together form the group of formula IV,'} {'sup': '4', 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'in which Ris as defined in ; and'}, 'Y is the radical of formula VI,'}Z is the radical of formula VII.3. A composition as claimed in claim 1 , wherein the compound of formula I is a compound in which:{'sup': '1', 'Ris —CN;'}{'sup': '2', 'sub': '3', 'Ris —CF;'}{'sup': '3', 'Ris =0;'}X is the radical of formula II;{'sup': '4', 'Y is the radical of formula VI, in which Ris hydrogen; and'}Z is —O— or the radical of formula VII.4. A composition as claimed in claim 1 , wherein the compound of formula I is chosen from 4-[3-(4-hydroxybutyl)-4 claim 1 ,4-dimethyl-2 claim 1 ,5-dioxo-1-imidazolidinyl]-2-(trifluoromethyl)benzonitrile and 4-(5-methyl-2 claim 1 ,4-dioxo-5-trifluoromethyl)-oxazolidin-3-yl)-2-(trifluoromethyl)-benzonitrile.5. A composition as claimed in claim 1 , wherein the at least one plasticizer is chosen from ethoxylated compounds claim 1 , panthenol claim 1 , esters of adipic acid claim 1 , and esters of sebacic acid.6. A composition as claimed in claim 5 , wherein the at least one plasticizer is chosen from polyoxyethylated castor oil claim 5 , ethoxylated cholesterol claim 5 , and panthenol.7. A composition as claimed in claim 1 , wherein the at least one physiologically tolerated solvent is chosen from water and (C-C)-alcohols ...

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Номер записи: 41
17-03-2022 дата публикации

FUNCTIONALIZED MATERIALS AND COMPOUNDS

Номер: US20220081424A1
Автор: Glover Thomas Grant, West Kevin N.
Принадлежит: UNIVERSITY OF SOUTH ALABAMA

Processes for chemical functionalization of materials are described. The processes generally include chemical reaction between a thiol group of a first compound or material and an alkene group or alkyne group of a second compound or material. Also disclosed are functionalized materials and compounds suitable for functionalizing a material. The present application is a continuing application of co-pending U.S. patent application Ser. No. 17/288,122 filed Apr. 23, 2021, which is a U.S. national phase application of PCT application PCT/US2019/058022 filed Oct. 25, 2019, which claims the benefit of U.S. provisional application 62/751,082 filed Oct. 26, 2018.The present invention relates generally to processes for imparting one or more desirable functionalities to materials and compounds which prior to treatment according to the process essentially lack such functionality.It is known in the art to impart desirable characteristics or performance attributes to materials by applying chemical compounds thereto. For example, materials may be coated or treated with various chemical compositions that contain one or more ingredients that impart hydrophobicity, soil or stain resistance, antistat, UV antidegradant, antibacterial/biocidal or similar characteristics which are sought after in various product and end-use applications. A particular challenge for manufacturers in developing coatings or treatment compositions in this field resides in (i) identifying active ingredients that are rapidly and thoroughly soluble or dispersible in composition solvents or carriers, in particular in solvents that are often utilized today because of their environmentally friendly nature while (ii) maximizing the coating's or treatment's efficacy and efficacy duration. Despite best efforts, the nature of these coatings or treatments is that their efficacy will inevitably decrease over time.In order to improve efficacy duration, the art has investigated techniques that involve the chemical bonding ...

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Номер записи: 42
12-03-2015 дата публикации

SUBSTITUTED B-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

Номер: US20150073004A1
Автор: BARTONE BODOR Veronika, BATA Imre, BUZDER-LANTOS Péter, FERENCZY Gyorgy, SZAMOSVOLGYI Zsuzsanna, SZELECZKY Gabor, TOMOSKOZI Zsuzsanna, VASAS Attila
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 ...

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Номер записи: 43
15-03-2018 дата публикации

COMPOSITIONS FOR THE TREATMENT OF FIBROSIS AND FIBROSIS-RELATED CONDITIONS

Номер: US20180072682A1
Автор: Duggan Karen Annette
Принадлежит: VECTUS BIOSYSTEMS LIMITED

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions. 2. The compound according to claim 1 , wherein the saturated claim 1 , partly saturated or unsaturated 5- or 6-membered heterocyclyl contains one or more of N claim 1 , S or O claim 1 , optionally substituted with one or more oxo claim 1 , Calkyl claim 1 , amino claim 1 , hydroxyl or halo substituents.3. The compound according to claim 1 , wherein the saturated claim 1 , partly saturated or unsaturated 5- or 6-membered heterocyclyl is selected from pyrrolyl claim 1 , pyrazolyl claim 1 , imidazolyl claim 1 , triazolyl claim 1 , imidazolidinyl claim 1 , pyrrolidinyl claim 1 , pyrrolidinylidene claim 1 , dihydropyrrolyl claim 1 , isoxazolyl dihydrooxazolyl claim 1 , isoxazolidinyl claim 1 , oxazolidinyl and oxazolyl claim 1 , optionally substituted with one or more oxo claim 1 , Calkyl claim 1 , amino claim 1 , hydroxyl or halo substituents.4. The compound according to claim 1 , wherein the Calkoxyl amine is aminooxymethyl.5. The compound according to claim 1 , wherein the Calkyl amine is optionally substituted with one or more of Calkyl claim 1 , Chalo alkyl claim 1 , hydroxyl or halo claim 1 , preferably mono- claim 1 , di- or tri-substituted halo alkyl claim 1 , most preferably tri-fluoro methane.6. The compound according to claim 1 , wherein the Calkyl carboxylic acid is carboxylic acid.7. The compound according to claim 1 , wherein the Calkyl hydroxyl is methyl hydroxyl.8. The compound according to claim 1 , wherein the Calkyl bicyclic heterocyclyl is selected from indolyl claim 1 , isoindolyl claim 1 , insolinyl and isoindolinyl claim 1 , optionally substituted with one or more oxo claim 1 , preferably dioxo.9. The compound according to claim 1 , wherein the Calkoxyl bicyclic heterocyclyl is selected indolyl claim 1 , isoindolyl claim 1 , insolinyl and isoindolinyl claim 1 , optionally substituted with one or ...

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Номер записи: 44
14-03-2019 дата публикации

Substituted Imidazole Derivatives and Methods of Use Thereof

Номер: US20190076402A1
Автор: David Jones, Raju Bore Gowda, Rongyuan Xie
Принадлежит: vTvx Holdings I LLC

The present invention provides intermediates for methods for synthesizing compounds of Formula (I) and pharmaceutically acceptable salts thereof.

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Номер записи: 45
12-06-2014 дата публикации

MULTIPLE-COMPONENT SOLID PHASES CONTAINING AT LEAST ONE ACTIVE PHARMACEUTICAL INGREDIENT

Номер: US20140162989A1
Автор: Moulton Brian, Rodriguez-Hornedo Nair, Zaworotko Michael J.
Принадлежит:

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to binary phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions. 136-. (canceled)37. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a co-crystal comprising supramolecular synthons , each supramolecular synthon formed from stoichiometric amounts of at least one active pharmaceutical ingredient (API) and at least one co-former ,wherein the API has a first chemical functionality that permits formation of API homosynthons through non-covalent hydrogen bonding when the API is in its pure form,wherein the co-former has a second chemical functionality complimentary to the first chemical functionality via non-covalent hydrogen bonding,wherein said co-former is a solid at room temperature and atmospheric pressure when the co-former is in its pure form,wherein said co-former is not an API, andwherein supramolecular synthons are formed via non-covalent hydrogen bonding between the first chemical functionality of the API and the second chemical functionality of the co-former.38. The pharmaceutical composition of claim 37 , wherein the supramolecular synthon comprises a supramolecular heterosynthon dimer formed by non-covalent hydrogen bonding of the API to the co-former.39. The pharmaceutical composition of claim 37 , wherein the supramolecular synthon comprises a plurality of the API and a plurality of the co-former claim 37 , wherein the supramolecular synthon is a chain of supramolecular heterosynthons claim 37 , each supramolecular heterosynthon formed by non-covalent hydrogen bonding of one API to one co-former claim 37 , and wherein the supramolecular heterosynthons are bonded to one another by non-covalent hydrogen bonding.40. The pharmaceutical composition of claim 37 , ...

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Номер записи: 46
12-03-2020 дата публикации

Diarylhydantoin compounds

Номер: US20200079741A1
Автор: Charles L. Sawyers, Charlie D. Chen, Chris Tran, Derek Welsbie, Dongwon Yoo, John Wongvipat, Michael Jung, Samedy Ouk
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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Номер записи: 47
21-03-2019 дата публикации

NOVEL 5-SUBSTITUTED IMIDAZOLE DERIVATIVES

Номер: US20190082691A1
Автор: Bernier David, BRUNET Stephane, Coqueron Pierre-Yves, Dahmen Peter, Genix Pierre, HELMKE Hendrik, Hoffmann Sebastian, KENNEL Philippe, Meissner Ruth, MILLER Ricarda, NAUD Sebastien, Vors Jean-Pierre, Wachendorff-Neumann Ulrike, WITTROCK Sven
Принадлежит:

The present invention relates to novel 5-substituted imidazolylmethyl derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 2. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'sub': 1', '8', '1', '8', '2', '7', '2', '7', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '7, 'Rrepresents in each case optionally branched C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-haloalkenyl, or optionally halogen-, cyano-, C-C-alkyl-, C-C-haloalkyl-, C-C-alkoxy-, C-C-haloalkoxy-, C-C-alkylthio- or C-C-haloalkylthio-substituted C-C-cycloalkyl.'}3. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'sub': 1', '4', '1', '4', '2', '5', '2', '5', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '6, 'Rrepresents in each case optionally branched C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-haloalkenyl, or optionally halogen-, cyano-, C-C-alkyl-, C-C-haloalkyl-, C-C-haloalkoxy-, C-C-alkoxy-, C-C-alkylthio- or C-C-haloalkylthio-substituted C-C-cycloalkyl.'}4. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'sub': 1', '4', '1', '4', '1', '4, 'Rrepresents tert-butyl, isopropyl, 1-halocyclopropyl, 1-(C-C-alkyl)cyclopropyl, 1-(C-C-alkoxy)cyclopropyl or 1-(C-C-alkylthio)cyclopropyl.'}5. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'Rrepresents tert-butyl, isopropyl, 1-chlorocyclopropyl, 1-fluorocyclopropyl or 1-methylcyclopropyl.'}6. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'Rrepresents 1-chlorocyclopropyl or 1-fluorocyclopropyl ...

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Номер записи: 48
29-03-2018 дата публикации

Diarylhydantoin Compounds

Номер: US20180086718A1
Автор: Chen Charlie D., Jung Michael, Ouk Samedy, Sawyers Charles L., Tran Chris, Welsbie Derek, Wongvipat John, Yoo Dongwon
Принадлежит: The Regents of the University of California

The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer. 151.-. (canceled) The present invention relates to diarylhydantoin compounds including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer. This application is a continuation of U.S. application Ser. No. 14/496,973, filed Sep. 25, 2014, which is a continuation of U.S. application Ser. No. 14/137,991, filed Dec. 20, 2013, which is a continuation of U.S. application Ser. No. 13/448,964, filed Apr. 17, 2012, which is a continuation of U.S. application Ser. No. 12/708,523, filed Feb. 18, 2010, which is a divisional of U.S. application Ser. No. 11/433,829, filed May 15, 2006, which claims the benefit of U.S. Provisional Application No. 60/786,837, filed Mar. 29, 2006, U.S. Provisional Application No. 60/756,552, filed Jan. 6, 2006, U.S. Provisional Application No. 60/750,351, filed Dec. 15, 2005, and U.S. Provisional Application No. 60/680,835, filed May 13, 2005, the specifications of which are hereby incorporated by reference in their entirety.This invention was made with Government support under Grant No. W81XWH-04-1-0129 awarded by the United States Army, Medical Research and Materiel Command and under Grant No. CA092131 awarded by the National Institutes of Health. The Government has certain rights in the invention.Prostate cancer is the most common incidence of cancer and the second leading cause of cancer death in Western men. When the cancer is confined locally, the disease can be cured by surgery or radiation. However, 30% of such cancer relapses with distant metastatic disease and others have advanced disease at diagnoses. Advanced disease is treated by castration and/or administration of antiandrogens, the so-called androgen deprivation therapy. Castration lowers the circulating levels of ...

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Номер записи: 49
29-03-2018 дата публикации

Biocidal coatings and methods for making same

Номер: US20180086740A1
Автор: Song Liu
Принадлежит: Exigence Technologies Inc

Methods for increasing biocidal activity of a substrate are provided. The methods can include attaching one or more ionic compounds to the substrate. The ionic compound can include a cationic moiety and at least one of an N-halamine precursor group or an N-halamine moiety.

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Номер записи: 50
19-03-2020 дата публикации

COMPOSITION FOR THE PREVENTION AND ELIMINATION OF ODORS

Номер: US20200085987A1
Автор: JOHNSTON Simon, Williams Jeffrey F.
Принадлежит: OXISCIENCE, LLC

Articles can be provided with odor resistance by applying a dispersion of a halogenated heterocyclic N-halamine in an inert liquid carrier onto the surface of the article and allowing the inert liquid carrier to penetrate into it. The N-halamine accordingly becomes deposited on the surface of the article after the inert liquid carrier penetrates into the article. This method can be used to provide odor resistance to a variety of substrates, including garbage bags. It can also be used to deposit other functional particulates onto the surface of substrates having sufficient porosity to take up the vehicle. For instance, such functional particles can be oxidants that display antimicrobial and/or enzyme inhibitory efficacy or particles having toxin interaction potentials through oxidative degradation or adsorption of toxic substances in air and/or water, such as fluoride uptake by metal oxide microparticles. 1. A method for manufacturing a medium for purifying fluids which comprises applying a dispersion of a micronized metal oxide in an inert liquid carrier to the surface of a substrate having a high surface area and allowing the inert liquid carrier to penetrate into the substrate leaving the micronized metal oxide stranded on the surface of the substrate.2. The method for manufacturing a medium for purifying fluids as specified in wherein the micronized metal oxide has a high affinity for sequestering contaminants.3. A method for manufacturing a medium for purifying fluids containing toxic compounds which comprises applying a dispersion of a halogenated heterocyclic N-halamine in an inert liquid carrier to the surface of a substrate having a high surface area and allowing the inert liquid carrier to penetrate into the substrate claim 1 , wherein the inert liquid carried does not react with halogen atoms in the halogenated heterocyclic N-halamine claim 1 , wherein the halogenated heterocyclic N-halamine is capable of destroying the toxic compound by oxidative action ...

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Номер записи: 51
19-03-2020 дата публикации

Salts for use in electrolyte compositions or as electrode additives

Номер: US20200087262A1
Автор: Antoine Lafleur-Lambert, Charlotte MALLET, Karim Zaghib, Shinichi Uesaka, Sylviane ROCHON
Принадлежит: HYDRO QUEBEC, Murata Manufacturing Co Ltd

Here are described compounds for use as electrode additives or as salts in electrolyte compositions, and their methods of preparation. Also described are electrochemical cells comprising the compounds as electrode additives or as salts in electrolyte compositions.

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Номер записи: 52
01-04-2021 дата публикации

Dyes for Analysis of Soluble Protein Aggregates or Misfolded Protein Oligomers

Номер: US20210094922A1
Автор: Liu Yu, Wolstenholme Charles, Zhang Xin
Принадлежит:

Dye and compositions to monitor the multistep protein aggregation process in both test tubes and live cells are provided. These dyes can detect misfolded protein oligomers and distinguish insoluble protein aggregates from misfolded oligomers. Applications of these dyes include measuring kinetics of protein aggregation, monitoring aggregation of specific proteins in intact live cells, monitoring aggregation of cellular proteome in intact live cells, and tracking the time course of protein aggregation in cells under stress conditions. 3. (canceled)4. A method for detecting at least one of aggregated protein , misfolded protein , and amyloid fiber in a protein of interest , comprising:performing a first measurement of fluorescence intensity of a protein of interest;adding to the protein of interest a fluorescent protein chromophore; andperforming a second measurement of fluorescence intensity of the protein of interest; wherein increased fluorescence is indicative of at least one of aggregation, misfolding, and amyloid fiber in the protein of interest.5. (canceled)6. The method of claim 4 , wherein the method is conducted in a cell in vivo.7. The method of claim 4 , wherein the method is conducted in vitro.8. The method of claim 4 , further comprising purifying the protein of interest prior to the first measurement.9. The method of claim 4 , wherein the fluorescent protein chromophore comprises a thioflavm-T guiding group or a tert-butyloxycarbonyl guiding group.10. The method for detecting at least one of aggregated protein claim 4 , misfolded protein claim 4 , and amyloid fiber in a protein of interest of claim 4 , said method comprising:performing a first measurement of fluorescence intensity of a standard protein;andcomparing the fluorescence intensity of the standard protein with the fluorescence intensity of the protein of interest, wherein increased fluorescence of the protein of interest relative to the fluorescence intensity of the standard protein is ...

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Номер записи: 53
05-04-2018 дата публикации

N-ACYL AMINO ACID COMPOUNDS AND METHODS OF USE

Номер: US20180093984A1
Автор: Andre Patrick, Bergnes Gustave, CHA Jacob, CHEN Chun, Halcomb Randall L., HOM Timothy, JIANG Lan, JR. David John, Li Hui, Morgans
Принадлежит:

The invention relates to compounds of formula (I): 2: The compound of claim 1 , or a salt thereof claim 1 , wherein Ris a fused bicyclic C-Caryl optionally substituted by Ror a fused bicyclic 7- to 10-membered heteroaryl optionally substituted by R.3: The compound of claim 1 , or a salt thereof claim 1 , wherein Ris a fused bicyclic 7- to 10-membered heteroaryl optionally substituted by R.4: The compound of claim 3 , or a salt thereof claim 3 , wherein Ris indazolyl optionally substituted by R claim 3 , benzimidazolyl optionally substituted by R claim 3 , or benzoxazolyl optionally substituted by R.5: The compound of claim 1 , or a salt thereof claim 1 , wherein Ris phenyl optionally substituted by R.6: The compound of claim 1 , or a salt thereof claim 1 , wherein Ris a monocyclic 5- or 6-membered heteroaryl optionally substituted by R.7: The compound of claim 1 , or a salt thereof claim 1 , wherein the -A-L-moiety is -A-L-.8: The compound of claim 7 , or a salt thereof claim 7 , wherein Ais C-Carylene optionally substituted by R.9: The compound of claim 7 , or a salt thereof claim 7 , wherein Ais C-Ccycloalkylene optionally substituted by R.10: The compound of claim 7 , or a salt thereof claim 7 , wherein Ais 5- to 10-membered heteroarylene optionally substituted by R.11: The compound of claim 7 , or a salt thereof claim 7 , wherein Ais 3- to 12-membered heterocyclylene optionally substituted by R.12: The compound of claim 7 , or a salt thereof claim 7 , wherein Ais selected from the group consisting of 1 claim 7 ,4-phenylene claim 7 , 1 claim 7 ,3-phenylene claim 7 , 1 claim 7 ,1-cyclopropylene claim 7 , 1 claim 7 ,2-cyclopropylene claim 7 , 1 claim 7 ,3-cyclobutylene claim 7 , 1 claim 7 ,4-cyclohexylene claim 7 , 1 claim 7 ,3-azetidinylene claim 7 , 1 claim 7 ,3-pyrrolidinylene claim 7 , and 2 claim 7 ,5-benzo[d]oxazolylene.14: The compound of claim 13 , or a salt thereof claim 13 , wherein Z is —CRR— where each of Rand Ris H.16: The compound of claim 7 , or a ...

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Номер записи: 54
16-04-2015 дата публикации

Heterocyclic aspartyl protease inhibitors

Номер: US20150105354A1
Автор: Andrew W. Stamford, Brian Mckittrick, Corey Strickland, Elizabeth M. Smith, Jared N. Cumming, Johannes H. Voigt, John Caldwell, Kurt W. Saionz, Lingyan Wang, Rachael C. Hunter, Robert D. Mazzola, Jr., Suresh D. Babu, Tao Guo, Thuy X.H. Le, Ulrich Iserloh, William J. Greenlee, Yuanzan C. Ye, Yusheng Wu, Zhaoning Zhu, Zhong-Yue Sun
Принадлежит: Merck Sharp and Dohme LLC, Pharmacopeia LLC

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O) 2 —, —C(═O)—, —O—, —C(R 6 )(R 7 )—, —N(R 5 )— or —C(═N(R 5 ))—; X is —O—, —N(R 5 )— or —C(R 6 )(R 7 )—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O) 2 —, —C(═O)— or —C(═NR 5 )—; U is a bond, —S(O)—, —S(O) 2 —, —C(O)—, —O—, —P(O)(OR 15 )—, —C(═NR 5 )—, —(C(R 6 )(R 7 )) b — or —N(R 5 )—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O) 2 —, —O—, or —N(R 5 )—, U is not —S(O)—, —S(O) 2 —, —O—, or —N(R 5 )—; provided that when X is —N(R 5 )— and W is —S(O)—, —S(O) 2 —, —O—, or —N(R 5 )—, then U is not a bond; and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , and R 7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.

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Номер записи: 55
23-04-2015 дата публикации

Diarylhydantoin compounds

Номер: US20150112082A1
Автор: Charles L. Sawyers, Charlie D. Chen, Chirs Tran, Derek Welsbie, Dongwon Yoo, John Wongvipat, Michael Jung, Samedy Ouk
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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Номер записи: 56
20-04-2017 дата публикации

HETEROCYCLIC INHIBITORS OF THE SODIUM CHANNEL

Номер: US20170107203A1
Автор: Holland Richard, Lamontagne Jason, PAJOUHESH Hassan, Pajouhesh Hossein, Whelan Brendan, ZHANG Lingyun
Принадлежит:

The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (1)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome. 3. The compound of claim 1 , wherein Ar is unsubstituted phenyl or Ar is phenyl having 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5 substituents selected independently from optionally substituted C1-C6 alkyl claim 1 , optionally substituted C1-C6 alkoxy claim 1 , O-(optionally substituted phenyl) claim 1 , optionally substituted phenyl claim 1 , —SO-(optionally substituted phenyl) claim 1 , —SO-(optionally substituted alkyl) claim 1 , and halogen.4. The compound of or claim 1 , wherein Ar comprises a halogen substituent.5. The compound of any of - claim 1 , wherein Rand Rare both H.6. The compound of claim 1 , wherein Rand Ar together form a dihydroindole moiety.7. The compound of claim 1 , wherein Rand Ar together form an indane moiety.8. The compound of any of - claim 1 , wherein m is 0 and n is 0.9. The compound of any of - claim 1 , wherein m is 1 and n is O.10. The compound of any of - claim 1 , wherein m is 0 and n is 1.11. The compound of any of - claim 1 , wherein m is 1 and n is 1.12. The compound of claim 1 , wherein said compound is selected from compounds 51-59 in Table 1.14. The compound of claim 13 , wherein Ris H.15. The compound of or claim 13 , wherein Lis an optionally substituted C1-C3 alkylene that is linear or branched.16. The compound of claim 15 , wherein said C1-C3 alkylene is unsubstituted.17. ...

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Номер записи: 57
30-04-2015 дата публикации

BIOCIDAL COMPOUNDS AND METHODS FOR USING SAME

Номер: US20150118179A1
Автор: Liu Song
Принадлежит: UNIVERSITY OF MANITOBA

Biocidally active cationic analogs of N-halamine having two biocidally active groups covalently bonded together in a single molecule and having general Formula (I). Compounds of Formula (I), and precursors thereof, can be in solution form immobilized onto a substrate via physical coating or covalent chemical bonding to functionalize surfaces or added into materials as additives so as to render them biocidal. The biocidal solutions and substrates comprising the compounds or precursors of the present invention can then be used to inactivate pathogenic microorganisms. N-halamine-L-QUAT (I) wherein: the N-halamine may be a cyclic or acyclic N-halamine; L is C-Calkyl, cyclic aromatic or non-aromatic ring, ether, ketone or any other organic linking structures, and QUAT has general formula (II): 1116-. (canceled)123. A precursor of the derivatized biocidal compound according to claim 121 , wherein each halo substituent in each N-halamine moiety is replaced with a hydrogen substituent claim 121 , and wherein halogenation of said substituent results in the biocidally active compound.127. A composition comprising a precursor of the biocidal compound according to and a substrate claim 125 , wherein the precursor is attached to the substrate claim 125 , and wherein each halo substituent in each N-halamine moiety of the biocidal compound is replaced with a hydrogen substituent claim 125 , and wherein halogenation of said substituent results in the biocidally active compound.129. The composition according to claim 125 , wherein said compounds or precursors thereof are covalently attached to the surface of the substrate.130. The composition according to claim 125 , wherein said compounds or precursors thereof are coated on the surface of the substrate.131. The composition according to claim 124 , wherein said compounds or precursors thereof are incorporated within the substrate.132. The composition according to claim 125 , wherein the substrate is a woven claim 125 , knit claim ...

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Номер записи: 58
27-04-2017 дата публикации

WATER-SOLUBLE TRIAZABUTADIENES

Номер: US20170114033A1
Автор: Jewett John C., Kimani Flora W.
Принадлежит:

Water-soluble triazabutadiene molecules and methods for producing and using such compounds. The triazabutadiene molecules may be more labile at pH levels below physiological pH, such as pH 7, pH 6, pH 5, etc. The triazabutadiene molecules and compounds may be used for depositing diazonium salt and/or cargo in a pH-sensitive manner. The triazabutadiene molecules may alternatively be cleaved in reducing conditions or as a light-catalyzed reaction. The compounds herein may be used for delivery of drugs, as part of detection systems, or for other applications such as underwater adhesive applications. 2. The triazabutadiene molecule of claim 1 , wherein the tri-substituted aryl group of Ycomprises a NHS-ester moiety; an oligonucleotide; a peptide; a fluorescence quencher; a pro-fluorophore; an alkyne; a triazene; or a combination thereof; and the optionally substituted aryl of Zcomprises a NHS-ester moiety; an oligonucleotide; a peptide; a fluorescence quencher; a pro-fluorophore; an alkyne; a triazene; a biologically active acid labile compound; a prodrug comprising a phenolic functional group; an aldehyde; an amine; an aminooxy; a halogen; or a combination thereof.3. The triazabutadiene molecule of claim 1 , wherein Xcomprises a moiety of the formula —R-Q claim 1 , wherein Rcomprises Calkylene claim 1 , and Qcomprises sulfate claim 1 , phosphate claim 1 , or a quaternary ammonium cation.4. The triazabutadiene molecule of claim 1 , wherein the molecule has half-life of at least 12 hours in a pH 7.4 buffer.56-. (canceled)7. The triazabutadiene molecule of claim 1 , wherein the triazabutadiene molecule is adapted to undergo an irreversible reaction yielding a diazonium species and a cyclic guanidine species.8. The triazabutadiene molecule of claim 7 , wherein the reaction occurs at a reaction rate claim 7 , and said reaction rate is increased when the triazabutadiene molecule is subjected to a lowered pH.9. The triazabutadiene molecule of claim 8 , wherein the lowered pH ...

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Номер записи: 59
03-05-2018 дата публикации

Neprilysin inhibitors

Номер: US20180118696A1
Автор: Adam D. Hughes, Anne-Marie Beausoleil, Daniel D. Long, Donna A.A. Wilton, Melissa Fleury
Принадлежит: Theravance Biopharma R&D Ip Llc

In one aspect, the invention relates to compounds having the formula I: where R 1 -R 6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

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Номер записи: 60
16-04-2020 дата публикации

Method for preparing methionine

Номер: US20200115334A1
Автор: Christian Kaiser, Daniel Fischer, Daniel SUDHOFF, Hans Joachim Hasselbach, Judith Hierold, Markus Held, Martin STEURENTHALER, Philipp Roth, Thorsten MERKER
Принадлежит: EVONIK DEGUSSA GmbH

The present invention relates to a method for preparing methionine or methionine salts. In particular, the invention describes the step of preparing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN) from 3-methylthiopropanal (MMP) and hydrogen cyanide (HCN) in the presence of ammonia by bringing a gaseous mixture comprising HCN and ammonia into contact with MMP.

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Номер записи: 61
12-05-2016 дата публикации

ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES

Номер: US20160130240A1
Автор: ALIG Bernd, Becker Angela, CEREZO-GALVEZ SILVIA, FISCHER Reiner, HAHN Julia Johanna, ILG Kerstin, KOEHLER Adeline, Portz Daniela, VOERSTE Arnd
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 ...

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Номер записи: 62
14-05-2015 дата публикации

CRYSTALLINE FORMS OF AN ALKOXYIMIDAZOL-1-YLMETHYL BIPHENYL CARBOXYLIC ACID

Номер: US20150133518A1
Автор: Fatheree Paul R., Thalladi Venkat R.
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention provides crystalline salt forms of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid. This invention also provides pharmaceutical compositions comprising the crystalline compounds, processes and intermediates for preparing the crystalline compounds, and methods of using the crystalline compounds to treat diseases such as hypertension. 111-. (canceled)12. The pharmaceutical composition of claim 23 , wherein the crystalline heminapadisylate salt is further characterized by having one or more additional diffraction peaks at 2θ values selected from 14.05±0.20 claim 23 , 18.65±0.20 claim 23 , 19.55±0.20 claim 23 , 20.21±0.20 claim 23 , 21.44±0.20 claim 23 , 23.48±0.20 claim 23 , 25.69±0.20 claim 23 , 26.65±0.20 claim 23 , 28.79±0.20 claim 23 , 29.63±0.20 claim 23 , and 30.52±0.20.13. The pharmaceutical composition of claim 23 , wherein the crystalline heminapadisylate salt is characterized by a powder x-ray diffraction pattern in which the peak positions are substantially in accordance with the peak positions of the pattern shown in .14. The pharmaceutical composition of claim 23 , wherein the crystalline heminapadisylate salt is characterized by a differential scanning calorimetry thermogram which has a melting point of about 181° C.15. The pharmaceutical composition of claim 23 , wherein the crystalline heminapadisylate salt is characterized by a differential scanning calorimetry thermogram substantially in accordance with that shown in .1622-. (canceled)23. A pharmaceutical composition comprising a blended mixture of a pharmaceutically acceptable carrier and a crystalline heminapadisylate salt of 4′-{2-ethoxy-4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid claim 23 , characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 4.84±0.20 claim 23 , 9.41±0.20 claim 23 , 10.82±0. ...

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Номер записи: 63
16-04-2020 дата публикации

OLIGOMER AND LITHIUM BATTERY

Номер: US20200119359A1
Автор: Chern Chorng-Shyan, Pham Quoc Thai, Wang Fu-Ming
Принадлежит: National Taiwan University of Science and Technology

A oligomer and a lithium battery are provided. The oligomer is obtained by a polymerization reaction of a compound containing at least one ethylenically unsaturated group and a nucleophile compound. The compound containing at least one ethylenically unsaturated group is selected from a group consisting of a maleimide-based compound, an acrylate ester-based compound, a methacrylate ester-based compound, an acrylamide-based compound, a vinylamide-based compound and a combination thereof. The nucleophile compound is selected from a group consisting of monomaleimide, trithiocyanuric acid, hydantoin, hydantoin derivative, thiohydantoin, thiohydantoin derivative and a combination thereof. 1. An oligomer obtained by a polymerization reaction of a compound containing at least one ethylenically unsaturated group and a nucleophile compound , wherein the compound containing at least one ethylenically unsaturated group is selected from a group consisting of a maleimide-based compound , an acrylate ester-based compound , a methacrylate ester-based compound , an acrylamide-based compound , a vinylamide-based compound and a combination thereof , and the nucleophile compound is selected from a group consisting of monomaleimide , trithiocyanuric acid , hydantoin , hydantoin derivative , thiohydantoin , thiohydantoin derivative and a combination thereof.2. The oligomer of claim 1 , wherein a mole ratio of the compound containing at least one ethylenically unsaturated group and the nucleophile compound is between 1:5 and 5:1.3. The oligomer of claim 1 , wherein the maleimide-based compound comprises monomaleimide or bismaleimide.4. The oligomer of claim 1 , wherein the acrylate ester-based compound comprises bisphenol A diacrylate or bisphenol A ethoxylate diacrylate.5. The oligomer of claim 1 , wherein the methacrylate ester-based compound comprises bisphenol A dimethacrylate.6. The oligomer of claim 1 , wherein the acrylamide-based compound comprises bisacrylamide.7. The oligomer of ...

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Номер записи: 64
23-04-2020 дата публикации

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

Номер: US20200123100A1
Автор: BENENATO Kerry E., CORNEBISE Mark
Принадлежит:

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression. 1188.-. (canceled)190. The compound of claim 189 , wherein Rand Rare the same.191. The compound of claim 189 , wherein R′ is Calkyl.192. The compound of claim 189 , wherein n is 3.193. The compound of claim 189 , wherein 1 is 5 and m is 7.194. A nanoparticle composition comprising a lipid component comprising a compound of .195. The nanoparticle composition of claim 194 , wherein the lipid component further comprises a phospholipid selected from the group consisting of 1 claim 194 ,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC) claim 194 , 1 claim 194 ,2-dimyristoyl-sn-glycero-phosphocholine (DMPC) claim 194 , 1 claim 194 ,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) claim 194 , 1 claim 194 ,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) claim 194 , 1 claim 194 ,2-distearoyl-sn-glycero-3-phosphocholine (DSPC) claim 194 , 1 claim 194 ,2-diundecanoyl-sn-glycero-phosphocholine (DUPC) claim 194 , 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) claim 194 , 1 claim 194 ,2-di-O-octadecenyl-sn-glycero-3-phosphocholine (18:0 Diether PC) claim 194 , 1-oleoyl-2-cholesterylhemisuccinoyl-sn-glycero-3-phosphocholine (OChemsPC) claim 194 , 1-hexadecyl-sn-glycero-3-phosphocholine (C16 Lyso PC) claim 194 , 1 claim 194 ,2-dilinolenoyl-sn-glycero-3-phosphocholine claim 194 , 1 claim 194 ,2-diarachidonoyl-sn-glycero-3-phosphocholine claim 194 , 1 claim 194 ,2-didocosahexaenoyl-sn-glycero-3-phosphocholine claim 194 , 1 claim 194 ,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) claim 194 , 1 claim 194 ,2-diphytanoyl-sn- ...

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Номер записи: 65
23-04-2020 дата публикации

ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE

Номер: US20200123117A1
Автор: Virsik Peter, ZHOU Han-jie
Принадлежит:

The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer. 3. The compound of claim 2 , wherein C is 5- to 10-membered heteroaryl or aryl.4. The compound of claim 3 , wherein C is 5- to 7-membered heteroaryl comprising 1 claim 3 , 2 claim 3 , or 3 heteroatoms selected from O claim 3 , S claim 3 , or N as a ring member.5. The compound of claim 4 , wherein C claim 4 , which is substituted with (R)n3 claim 4 , is pyrazole claim 4 , imidazole claim 4 , oxazole claim 4 , oxadiazole claim 4 , oxazolone claim 4 , isoxazole claim 4 , thiazole claim 4 , pyridyl claim 4 , pyrazine claim 4 , furan or pyrimidyl.7. The compound of claim 6 , wherein Rand Rare each independently C claim 6 , —CN claim 6 , —CF claim 6 , —OH claim 6 , methyl claim 6 , methoxy claim 6 , or —CONH.8. The compound of claim 2 , wherein:A and B are phenyl;{'sup': 5', '6, 'sub': 't', 'X is —(CRR)—;'}Y and Z are each —O—;{'sub': 2', '2', '2, 'V is —CH— or —CHCH—;'}L is halogen;{'sup': 1', '2, 'sub': 3', '1', '6, 'Rand Rare each independently hydrogen, halogen, —CN, —CF, —OH, or optionally substituted C-Calkyl;'}{'sup': 5', '6, 'sub': 1', '3, 'Rand Rare each independently hydrogen, halogen, —OH, or C-Calkyl; and'}{'sup': '16', 'sub': 1', '3', '2', '3', '2', '3, 'Ris hydrogen, C-Calkyl, C-Calkenyl, or C-Calkynyl.'}9. The compound of claim 8 , wherein:{'sup': 5', '6, 'sub': 1', '3, 'Rand Rare each independently hydrogen, or C-Calkyl;'}{'sub': 2', '3, 'W is —CH— or —C(CH)H—;'}{'sub': 2', '2, 'V is —CHCH—; and'}{'sup': 1', '2, 'Rand Rare each independently hydrogen, halogen, or —CN.'}11. The compound of claim 10 , wherein:{'sup': 3', '3, 'sub': 1', '3', '2', '2', '3', '3', '2', '3', '2', '2', '3', '3', '2', '2', '3', '2', '3', '3', '1', '3', '2', '3', '2', '3', ...

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Номер записи: 66
26-05-2016 дата публикации

ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES

Номер: US20160145235A1
Автор: ALIG Bernd, Becker Angela, CEREZO-GALVEZ SILVIA, FISCHER Reiner, HAHN Julia Johanna, ILG Kerstin, KOEHLER Adeline, Portz Daniela, VOERSTE Arnd
Принадлежит:

The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I) 3. Compound according to in whichA and B together with the atoms to which they are bonded are a substructure selected from the group consisting of I-A to I-G;{'sup': '1', 'claim-text': [{'sub': 1', '6', '3', '6', '1', '6', '2', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6', '1', '6, 'is (C-C)alkyl, (C-C)cycloalkyl(C-C)alkyl, halo(C-C)alkyl, cyano(C-C)alkyl, hydroxy(C-C)alkyl, (C-C)alkoxy(C-C)alkyl, amino(C-C)alkyl, (C-C)alkoxycarbonyl(C-C)alkyl, (C-C)alkylsulphanyl(C-C)alkyl, (C-C)alkylsulphinyl(C-C)alkyl, (C-C)alkylsulphonyl(C-C)alkyl, halo(C-C)alkylsulphanyl(C-C)alkyl, halo(C-C)alkylsulphinyl(C-C)alkyl, halo(C-C)alkylsulphonyl(C-C)alkyl, (C-C)alkoxy(C-C)alkylsulphanyl(C-C)alkyl, (C-C)alkoxy(C-C)alkylsulphinyl(C-C)alkyl, (C-C)alkoxy(C-C)alkylsulphonyl(C-C)alkyl, phenyl(C-C)alkyl, phenoxy(C-C)alkyl, phenylsulphanyl(C-C)alkyl, phenylsulphinyl(C-C)alkyl, phenylsulphonyl(C-C)alkyl, hetaryl(C-C)alkyl, hetaryloxy(C-C)alkyl, hetarylsulphanyl(C-C)alkyl, hetarylsulphinyl(C-C)alkyl, hetarylsulphonyl(C-C)alkyl, where the aforementioned radicals may each optionally be substituted and/or, under the condition that, in the case of an unsaturated radical, the defined minimum number of carbon atoms is 2, the radicals may be saturated or unsaturated; or'}, {'sub': 3', '6, 'is optionally substituted saturated or unsaturated (C-C)cycloalkyl which may optionally be ...

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Номер записи: 67
10-06-2021 дата публикации

PROTEASOME INHIBITORS AND USES THEREOF

Номер: US20210171514A1
Автор: KIRKMAN Laura, Lin Gang, NATHAN Carl, Shi Lei, SINGH Pradeep K.
Принадлежит:

The compounds of the present invention are represented by the following compounds having Formula (I): 153.-. (canceled) This application claims the priority benefit of U.S. Provisional Patent Application Ser. No. 62/242,139 filed Oct. 15, 2015, which is hereby incorporated by reference in its entirety.The present invention relates to proteasome inhibitors and uses thereof.Proteasomes are highly conserved self-compartmentalizing proteases found in three kingdoms of life. A proteasome is a large, ATP-dependent, multi-subunit, barrel-shaped N-terminal nucleophile hydrolase present in the cytosol and nucleus of eukaryotic cells and is responsible for the degradation of the majority of cellular proteins (Baumeister et al., “The Proteasome: Paradigm of a Self-Compartmentalizing Protease,” 92(3):367-380 (1998); Goldberg A L., “Functions of the Proteasome:from Protein Degradation and Immune Surveillance to Cancer Therapy,” 35(Pt 1):12-17 (2007)). Through regulated degradation, a proteasome regulates protein homeostasis, the cell cycle, signal transduction, protein trafficking, immune responses, etc, which are important cellular functions. Degradation product oligopeptides are reservoirs of antigenic peptides for MHC class I antigen presentation.Proteasome inhibition interrupts many cellular pathways, particularly, the NF-kB activation pathway, the induction of unfolded protein response, and ER stress, while strongly inducing apoptosis. For this reason, highly specific proteasome inhibitors have been approved for the treatment of hematological cancer. Proteasome inhibitors can also markedly limit the overall supply of peptides for MHC class I molecules and thus block antigen presentation (Rock et al., “Protein Degradation and the Generation of MHC Class I-Presented Peptides,” 80:1-70 (2002)). As a result, proteasome inhibitors reduce immune response via multiple routes.: (), the most deadly of the human malarias, accounts for nearly 0.5 million deaths a year, primarily in ...

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Номер записи: 68
09-06-2016 дата публикации

HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING

Номер: US20160159746A1
Автор: Bredesen Dale E., John Varghese
Принадлежит:

In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. 2. The compound of claim 1 , wherein Ris C═NH claim 1 , or C═O.3. (canceled)5. (canceled)810-. (canceled)1213-. (canceled)1517-. (canceled)1920-. (canceled)21. The compound of claim 1 , wherein said compound binds to APP and/or to the enzyme BACE and/or to an APP/BACE complex.22. The compound of claim 1 , wherein said compound binds to APP and inhibits the enzyme BACE.23. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a compound of .2427-. (canceled)28. A method of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease claim 1 , said method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, "administering to a subject in need thereof a compound of in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease."}29. The method of claim 28 , wherein said method is a method of: ...

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Номер записи: 69
14-05-2020 дата публикации

HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING

Номер: US20200148648A1
Автор: Bredesen Dale E., John Varghese
Принадлежит:

In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. 2. The compound of claim 1 , wherein Ris C═NH or C═O.3. (canceled)5. (canceled)810.-. (canceled)1013.-. (canceled)1520.-. (canceled)12. The compound of claim 1 , wherein said compound binds to APP and/or to the enzyme BACE and/or to an APP/BACE complex.13. The compound of claim 1 , wherein said compound binds to APP and inhibits the enzyme BACE.14. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a compound of .1597.-. (canceled)98. A kit comprising one or more containers containing a compound of .99101.-. (canceled) This application is a divisional of U.S. Ser. No. 15/833,862 filed on 6 Dec. 2017, which is a divisional of U.S. Ser. No. 14/928,775 filed 30 Oct. 2015, which is a continuation of U.S. Ser. No. 14/179,310 filed 12 Feb. 2014, which claims the benefit of U.S. 61/763,830 filed 12 Feb. 2013. The entire disclosures of each of the above recited applications are incorporated herein by reference.[Not Applicable]Amyloid beta peptide (Aβ) is a primary component of beta amyloid fibrils and plaques, which are regarded as having a role in an increasing number of pathologies. Examples of such pathologies include, but are not limited to, Alzheimer's disease, Down's syndrome, Parkinson's disease, memory loss (including memory loss associated with Alzheimer's disease and Parkinson's disease ...

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Номер записи: 70
16-06-2016 дата публикации

Novel compounds

Номер: US20160168101A1
Автор: Carmelida CAPALDI, Elisabetta Armani, Jonathan Mark Sutton, Robert Andrew Heald
Принадлежит: Chiesi Farmaceutici SpA

Compounds of formula (I) described herein are imidazolone derivatives having human neutrophil elastase (HNE) inhibitory properties and are useful for the treatment of diseases and conditions in which HNE is implicated.

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Номер записи: 71
16-06-2016 дата публикации

INHIBITORS OF CELLULAR NECROSIS AND RELATED METHODS

Номер: US20160168128A1
Автор: Ma Dawei, Qian Shan, Yuan Junying, Zhou Yijun
Принадлежит:

A compound having the following structure (I): 5. The compound of claim 4 , wherein Ris H.6. The compound of claim 4 , wherein Ris F.7. The compound of claim 4 , wherein Ris F.8. The compound of claim 4 , wherein Ris F.9. The compound of claim 4 , wherein Ris F.10. The compound of claim 4 , wherein Rand Rare F.11. The compound of claim 4 , wherein Rand Rare F.13. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , prodrug or tautomer thereof claim 1 , and a pharmaceutically acceptable carrier claim 1 , diluent or excipient.14. A method for treating a necrotic cell disease claim 13 , the method comprising administering an effective amount of the composition of to a subject in need thereof.15. The method of claim 14 , wherein the necrotic cell disease is trauma claim 14 , ischemia claim 14 , stroke claim 14 , cardiac infarction claim 14 , infection claim 14 , Gaucher's disease claim 14 , Krabbe disease claim 14 , sepsis claim 14 , Parkinson's disease claim 14 , Alzheimer's disease claim 14 , amyotrophic lateral sclerosis claim 14 , Huntington's disease claim 14 , HIV-associated dementia claim 14 , retinal degenerative disease claim 14 , glaucoma claim 14 , age-related macular degeneration claim 14 , rheumatoid arthritis claim 14 , psoriasis claim 14 , psoriatic arthritis or inflammatory bowel disease.16. A method for treating an inflammatory disorder claim 13 , the method comprising administering an effective amount of the composition of to a subject in need thereof.17. The method of claim 16 , wherein the inflammatory disorder is inflammatory bowel disease.18. The method of claim 16 , wherein the inflammatory disorder is Crohn's disease or ulcerative colitis.24. The method of claim 22 , wherein the leaving group is halogen.25. The method of claim 24 , wherein halogen is bromine or iodine.26. The method of claim 22 , wherein Ris C-Calkyl.27. The method of claim 26 , wherein Ris methyl.28. The method of ...

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Номер записи: 72
30-05-2019 дата публикации

PTEN BINDING COMPOUNDS, FORMULATIONS, AND USES THEREOF

Номер: US20190161450A1
Автор: Cai Jianfeng, DAVÉ VRUSHANK G.
Принадлежит: UNIVERSITY OF SOUTH FLORIDA

Described herein are compounds and formulations thereof that can bind PTEN. Also described herein are methods of using the compounds and formulations thereof that can bind PTEN. In some embodiments, the method can include administering an amount of a compound or formulation described herein to a subject in need thereof. 3. The compound of any claim 1 , wherein the compound is effective to decrease the activity of PTEN.4. The compound of claim 1 , wherein the compound is effective to decrease the activity of PTEN by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 claim 1 , 9 claim 1 , 10 claim 1 , 12 claim 1 , 15 claim 1 , 20 claim 1 , 25 claim 1 , 30 claim 1 , 35 claim 1 , 40 claim 1 , 45 claim 1 , 50 claim 1 , 55 claim 1 , 60 claim 1 , 65 claim 1 , 70 claim 1 , 75 claim 1 , 90 claim 1 , 85 claim 1 , 90 claim 1 , 95 claim 1 , 100 claim 1 , 125 claim 1 , 150 claim 1 , 175 claim 1 , or 200 percent or more.6. The compound of claim 1 , wherein the compound is effective to increase the activity of PTEN.7. The compound of claim 1 , wherein the compound is effective to increase the activity of PTEN by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , 8 claim 1 , 9 claim 1 , 10 claim 1 , 12 claim 1 , 15 claim 1 , 20 claim 1 , 25 claim 1 , 30 claim 1 , 35 claim 1 , 40 claim 1 , 45 claim 1 , 50 claim 1 , 55 claim 1 , 60 claim 1 , 65 claim 1 , 70 claim 1 , 75 claim 1 , 90 claim 1 , 85 claim 1 , 90 claim 1 , 95 claim 1 , 100 claim 1 , 125 claim 1 , 150 claim 1 , 175 claim 1 , or 200 percent or more.10. The method of claim 9 , wherein the step of contacting occurs in vitro.11. The method of claim 9 , further comprising the step of administering the amount of the compound having a structure according to Formula 1 or pharmaceutical formulation thereof to a subject claim 9 , where the step of administering occurs prior to the step of contacting.12. The method of claim 11 , wherein the step of contacting occurs ...

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Номер записи: 73
25-06-2015 дата публикации

METHOD OF PRODUCTION OF A METHIONINE SALT

Номер: US20150175535A1
Автор: Gangadwala Jignesh, Gruener Christof P., Hanrath Franz H., Hasselbach Hans Joachim, Koerfer Martin, Krull Horst, Stock Juergen
Принадлежит: EVONIK DEGUSSA GmbH

A method for production of a methionine salt in a reactive rectification column containing a weir having a height of 100 mm or more is provided. 1. A method for continuous production of a methionine salt , comprising:reacting 3-methylmercaptopropionaldehyde and hydrogen cyanide or a component that can be produced therefrom, thereby obtaining a solution containing 5-(2-methylmercaptoethyl)-hydantoin;alkaline hydrolysing the 5-(2-methylmercaptoethyl)-hydantoin to a methionine salt in a reactive rectification column, wherein only the solution containing 5-(2-methylmercaptoethyl)-hydantoin is fed on a topmost plate of the reactive rectification column and an alkaline circulating solution is fed on a plate located under the topmost plate.2. The method according to claim 1 , wherein the alkaline circulating solution contains an alkali metal carbonate.3. The method according to claim 1 , wherein water claim 1 , ammonia and COare removed from the top of the reactive rectification column and the NHremoved is condensed completely or partially and used in the synthesis of 5-(2-methylmercaptoethyl)-hydantoin.4. The method according to claim 1 , wherein a concentration of ammonia at the bottom of the rectification column is less than 120 ppm.5. The method according to claim 1 , wherein the reaction to 5-(2-methylmercaptoethyl)-hydantoin is carried out in a reactive absorber and then in a second reactor.6. The method according to claim 1 , wherein the reaction to 5-(2-methylmercaptoethyl)-hydantoin is carried out in a reactive absorber and then in a second reactor designed as a flow tube.7. The method according to claim 1 , wherein the temperature of the reaction mixture at the outlet of the reactive-rectification column is in the range from 180° C. to 190° C.8. The method according to claim 1 , wherein the temperature of the gas phase at the top of the reactive-rectification column is in the range from 160° C. to 170° C.9. The method according to claim 1 , wherein alkaline ...

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Номер записи: 74
25-06-2015 дата публикации

3-O-HETEROARYL-INGENOL

Номер: US20150175622A1
Автор: Grue-Sørensen Gunnar, Högberg Thomas, Liang Xifu, Månsson Kristoffer, Nørremark Bjarne, Ryttersgaard Carsten
Принадлежит: Leo Laboratories Limited

The present invention relates to a compound according to formula (I) wherein Rrepresents optionally substituted heteroaryl, and pharmaceutically acceptable salts, hydrates, solvates or pharmaceutically acceptable and physiologically cleavable esters thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. diseases associated with hyperplasia, neoplasia or dysplasia, with said compounds, to methods of treatment of cosmetic indications with said compounds, and to the use of said compounds in the manufacture of medicaments. 3. The compound according to ; wherein{'sub': 1', '1', '1', '4, 'Rrepresents Gand wherein at least one of Xor Xis selected from the group consisting of N, NH, S and O;'}or{'sub': 1', '2', '1', '5, 'Rrepresents Gand wherein at least one of Yor Yrepresents N;'}or{'sub': 1', '3', '1', '3', '2, 'Rrepresents Gand wherein the point of attachment to 3-O-ingenol occurs through Xor Xand wherein Xis selected from the group consisting of N, NH, S and O;'}or{'sub': 1', '3', '2', '1', '3, 'Rrepresents Gand wherein the point of attachment to 3-O-ingenol occurs through Xand wherein at least one of Xand Xis selected from the group consisting of N, NH, S and O;'}or{'sub': 1', '4', '1', '2, 'Rrepresents Gand wherein the point of attachment to 3-O-ingenol occurs through Yand wherein Yrepresents N;'}or{'sub': 1', '4', '2', '1', '3, 'Rrepresents Gand wherein the point of attachment to 3-O-ingenol occurs through Yand wherein at least one of Yand Yrepresents N;'}or{'sub': 1', '5', '1', '2, 'Rrepresents Gand wherein the point of attachment to 3-O-ingenol occurs through Yand wherein Yrepresents N;'}or{'sub': 1', '5', '2', '1', '3, 'Rrepresents Gand wherein the point of attachment to 3-O-ingenol occurs through Yand wherein at least one of Yand Yrepresents N.'}4. The compound according to claim 2 , wherein ...

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Номер записи: 75
06-06-2019 дата публикации

Multiple-component solid phases containing at least one active pharmaceutical ingredient

Номер: US20190169130A1
Автор: Brian Moulton, Michael J. Zaworotko, Nair Rodriguez-Hornedo
Принадлежит: University of Michigan, UNIVERSITY OF SOUTH FLORIDA

The subject invention concerns a method for identifying complementary chemical functionalities to form a desired supramolecular synthon. The subject invention also pertains to multiple-component phase compositions comprising one or more pharmaceutical entities and methods for producing such compositions.

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Номер записи: 76
28-05-2020 дата публикации

Imidazolidinedione derivatives

Номер: US20200163964A1
Автор: Agostino Marasco, Anne DÉCOR, Charles Large, Dieter Hamprecht, Giuseppe Alvaro, Stefano Fontana
Принадлежит: Autifony Therapeutics Ltd

and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.

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Номер записи: 77
09-07-2015 дата публикации

DUAL-ACTING IMIDAZOLE ANTIHYPERTENSIVE AGENTS

Номер: US20150191435A1
Автор: Choi Seok-ki, Fatheree Paul R., Gendron Roland, McKinnell Robert Murray, Olson Brooke
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention is directed to compounds having the formula: 125-. (canceled)26. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.27. The pharmaceutical composition of further comprising a therapeutic agent selected from the group consisting of diuretics claim 26 , βadrenergic receptor blockers claim 26 , calcium channel blockers claim 26 , angiotensin-converting enzyme inhibitors claim 26 , ATreceptor antagonists claim 26 , neprilysin inhibitors claim 26 , non-steroidal anti-inflammatory agents claim 26 , prostaglandins claim 26 , anti-lipid agents claim 26 , anti-diabetic agents claim 26 , anti-thrombotic agents claim 26 , renin inhibitors claim 26 , endothelin receptor antagonists claim 26 , endothelin converting enzyme inhibitors claim 26 , aldosterone antagonists claim 26 , angiotensin-converting enzyme/neprilysin inhibitors claim 26 , vasopressin receptor antagonists claim 26 , and combinations thereof.2830-. (canceled)31. A method for causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of hypertension claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .32. A method for causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of heart failure claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .33. A method of causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of chronic kidney disease claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .3438-. (canceled)39. 4′-{4-ethyl-5-[((S)-2-mercapto-4-methylpentanoylamino)methyl]-2-propoxyimidazol-1-ylmethyl}-2′-fluorobiphenyl-2-carboxylic acid claim 39 , or a pharmaceutically acceptable salt thereof. This application claims the benefit of U.S. Provisional Application No. 60/925,931, filed on Apr. 24, 2007; the entire disclosure of which ...

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Номер записи: 78
15-07-2021 дата публикации

MATRIX METALLOPROTEINASE (MMP) INHIBITORS AND METHODS OF USE THEREOF

Номер: US20210214340A1
Автор: CHANG Kai-Wei, LIU Suying, TSAI Cheng-Han, Yang Wenjin
Принадлежит:

Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis. 2. The compound of claim 1 , wherein ring C is phenyl.3. The compound of claim 1 , wherein ring D is pyridinyl or phenyl.5. The compound of claim 1 , wherein each of R claim 1 , Rand Ris hydrogen.6. The compound of claim 1 , wherein X is S; Y is O; and Z is CH.7. The compound of claim 1 , wherein ring B is a five or six membered monocyclic heteroaryl having 1-2 heteroatoms independently selected from N claim 1 , S claim 1 , and O claim 1 , wherein the five or six membered monocyclic heteroaryl is optionally substituted with —CH.8. The compound of claim 7 , wherein ring B is pyridinyl claim 7 , thiophenyl claim 7 , imidazolyl claim 7 , pyrazolyl claim 7 , or oxazolyl claim 7 , wherein each of pyridinyl claim 7 , thiophenyl claim 7 , imidazolyl claim 7 , pyrazolyl claim 7 , and oxazolyl is optionally substituted with —CH.9. The compound of claim 7 , wherein ring B is pyridinyl.11. The compound of claim 7 , wherein ring B is thiophenyl.16. The compound of claim 15 , wherein each of R claim 15 , R claim 15 , and Ris hydrogen.18. The compound of claim 17 , or a pharmaceutically acceptable salt thereof.19. A pharmaceutical composition comprising the compound of claim 1 , and at least one pharmaceutically acceptable carrier.20. A method of inhibiting macrophage elastase (MMP-12) in a subject in need thereof claim 19 , the method comprising ...

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Номер записи: 79
12-07-2018 дата публикации

HYDANTOIN CONTAINING DEOXYURIDINE TRIPHOSPHATASE INHIBITORS

Номер: US20180194736A1
Автор: Shirude Pravin S., Spyvee Mark
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. ...

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Номер записи: 80
12-07-2018 дата публикации

HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING

Номер: US20180194737A1
Автор: Bredesen Dale E., John Varghese
Принадлежит:

In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. 2: The compound of claim 1 , wherein Ris C═NH claim 1 , or C═O.3. (canceled)5. (canceled)810-. (canceled)1213-. (canceled)1517-. (canceled)1920-. (canceled)21: The compound of claim 1 , wherein said compound binds to APP and/or to the enzyme BACE and/or to an APP/BACE complex.22: The compound of claim 1 , wherein said compound binds to APP and inhibits the enzyme BACE.23: A pharmaceutical formulation comprising a pharmaceutically acceptable carrier and a compound of .2427-. (canceled)28: A method of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , and/or ameliorating one or more symptoms of a pre-Alzheimer's condition and/or cognitive dysfunction claim 1 , or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease claim 1 , said method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, "administering to a subject in need thereof a compound of in an amount sufficient to prevent or delay the onset of a pre-Alzheimer's cognitive dysfunction, and/or to ameliorate one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or to prevent or delay the progression of a pre-Alzheimer's cognitive dysfunction to Alzheimer's disease."}29: The method of claim 28 , wherein said method is a method of: ...

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Номер записи: 81
12-07-2018 дата публикации

Deoxyuridine triphosphatase inhibitors containing amino sulfonyl linkage

Номер: US20180194740A1
Автор: Mark Spyvee, Pravin S. Shirude, Robert D. Ladner
Принадлежит: Cv6 Therapeutics NI Ltd, University of Southern California USC

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

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Номер записи: 82
25-09-2014 дата публикации

CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

Номер: US20140288106A1
Автор: BARTANE BODOR Veronika, BATA Imre, BÁTORI Sándor, BUZDER-LANTOS Péter, FERENCZY Gyorgy, PATEK Marcel, SMRCINA Martin, SZELECZKY Gabor, Thorpe David Squire, TOMOSKOZI Zsuzsanna, VASAS Attila, WEICHSEL Aleksandra
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 ...

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Номер записи: 83
19-07-2018 дата публикации

COMPOSITION FOR THE PREVENTION AND ELIMINATION OF ODORS

Номер: US20180200399A1
Автор: JOHNSTON Simon, Williams Jeffrey F.
Принадлежит: OXISCIENCE, LLC

Articles can be provided with odor resistance by applying a dispersion of a halogenated heterocyclic N-halamine in an inert liquid carrier onto the surface of the article and allowing the inert liquid carrier to penetrate into it. The N-halamine accordingly becomes deposited on the surface of the article after the inert liquid carrier penetrates into the article. This method can be used to provide odor resistance to a variety of substrates, including garbage bags. It can also be used to deposit other functional particulates onto the surface of substrates having sufficient porosity to take up the vehicle. For instance, such functional particles can be oxidants that display antimicrobial and/or enzyme inhibitory efficacy or particles having toxin interaction potentials through oxidative degradation or adsorption of toxic substances in air and/or water, such as fluoride uptake by metal oxide microparticles. 1. A method of manufacturing an odor resistant article which comprises applying a dispersion of a halogenated heterocyclic N-halamine in an inert liquid carrier to the surface of the article and allowing the inert liquid carrier to penetrate into the article , wherein the inert liquid carrier does not react with halogen atoms in the halogenated heterocyclic N-halamine , and wherein the halogenated heterocyclic N-halamine becomes deposited on the surface of the article after the inert liquid carrier penetrates into the article.2. The method of manufacturing an odor resistant article as specified in wherein the article is comprised of a solid porous substrate.4. The method of manufacturing an odor resistant article as specified in wherein the partially halogenated hydantoin is monochloro-5 claim 1 ,5-dimethyl hydantoin.5. The method of manufacturing an odor resistant article as specified in wherein the inert liquid carrier is a vegetable based ester.6. The method of manufacturing an odor resistant article as specified in wherein the inert liquid carrier is isopropyl ...

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Номер записи: 84
29-07-2021 дата публикации

INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE

Номер: US20210230123A1
Автор: Pellicciari Roberto
Принадлежит:

The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. 3. The compound of claim 1 , wherein:{'sup': '1', 'Xis 0;'}{'sup': 2', '2, 'Xis O, S, or SR;'}{'sub': 2', 'm', '2', 'p, 'L is —(CH)CH═CH(CH)— or phenyl;'}{'sup': '2', 'Yis O, NH or S;'}{'sup': 1', 'a', 'b', 'e, 'sub': 6', '10, 'Ris C-Caryl substituted with Rand R, and optionally substituted with one to two R;'}{'sup': '2', 'sub': 1', '4, 'Ris H or C-Calkyl;'}{'sup': a', 'f', 'x', 'f', 'x', 'f', 'Y, 'sub': 2', 'r', '2', '2', 'r', '2', '2', 'r', '6', '10, 'Ris H, —(C(R))COR, —O(C(R))COR, —(C(R))C-Caryl, or —OR, wherein the aryl is substituted with one to three substituents selected from halogen and OH;'}{'sup': b', 'f', 'x', 'f, 'sub': 2', 'r', '2', '2', 'r', '6', '10, 'Ris —O(C(R))COR, or —(C(R))C-Caryl, wherein the aryl is substituted with one to three substituents selected from halogen and OH;'}{'sup': 'c', 'Ris —CN;'}{'sup': 'd', 'each Ris independently at each occurrence absent, H, or methyl;'}{'sup': e', 'z, 'sub': 1', '6', '2', '6', '2', '6', '1', '6, 'each Ris independently at each occurrence C-Calkyl, C-Calkenyl, C-Calkynyl, halogen, C-Chaloalkyl, —NHR, —OH, or —CN;'}{'sup': 'f', 'sub': 1', '6, 'each Ris independently H or C-Calkyl;'}{'sup': 'x', 'sub': 1', '6, 'Ris H or C-Calkyl;'}{'sup': y', 'z, 'sub': 1', '6', '1', '6, 'each Rand Ris independently H, C-Calkyl, or C-Chaloalkyl;'}each m, p, and r is independently 0, 1 or 2;n is 0 or 1;o is 1, 2, 3, or 4; andthe dotted line is an optional double bond.4. The ...

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Номер записи: 85
20-07-2017 дата публикации

BIOCIDAL COATINGS AND METHODS FOR MAKING SAME

Номер: US20170204085A1
Автор: Liu Song
Принадлежит: Exigence Technologies Inc.

Biocidally active cationic analogs of N-halamine having two biocidally active groups covalently bonded together in a single molecule and having general Formula (I). Compounds of Formula (I), and precursurs thereof, can be in solution form or immobilized onto a substrate via physical coating or covalent chemical bonding to functionalize surfaces or added into materials as additives so as to render them biocidal. The biocidal solutions and substrates comprising the compounds or precursors of the present invention can then be used to inactivate pathogenic microorganisms. 5. A composition comprising a precursor of the biocidal compound according to and a substrate claim 4 , wherein the precursor is attached to the substrate claim 4 , and wherein each halo substituent in each N-halamine moiety of the biocidal compound is replaced with a hydrogen substituent claim 4 , and wherein halogenation of said substituent results in the biocidally active compound.7. The composition according to claim 5 , wherein said precursor is incorporated within the substrate.8. The composition according to claim 4 , wherein said compounds are covalently attached to the surface of the substrate.9. The composition according to claim 4 , wherein said compounds are coated on the surface of the substrate.10. The composition according to claim 4 , wherein the substrate is a woven claim 4 , knit claim 4 , or nonwoven substrate.11. A method to biofunctionalize a substrate comprising contacting the substrate with a compound of claim 1 , thereby biofunctionalizing the substrate.12. A method to biofunctionalize a substrate comprising contacting the substrate with a precursor of claim 3 , thereby biofunctionalizing the substrate.13. A method of disinfecting a substrate comprising contacting the substrate with a compound of claim 1 , thereby disinfecting the substrate.14. A method of disinfecting a substrate comprising contacting the substrate with a composition of claim 4 , thereby disinfecting the ...

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Номер записи: 86
19-07-2018 дата публикации

COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

Номер: US20180201572A1
Автор: BENENATO Kerry E.
Принадлежит:

The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression. 1. (canceled)3. (canceled)514.-. (canceled)15. The compound of claim 2 , wherein Ris unsubstituted methyl or —(CH)Q claim 2 , in which Q is OH claim 2 , —NHC(S)N(CH) claim 2 , —NHC(S)NH(CH) claim 2 , —NHC(O)NH(CH) claim 2 , or —NHC(O)N(CH).1644.-. (canceled)45. The compound of claim 2 , wherein Rand Rare the same.46. The compound of claim 2 , wherein Rand Rare Calkyl.4752.-. (canceled)53. The compound claim 2 , wherein Rand Rare different.54111.-. (canceled)112. The compound of claim 2 , wherein the compound is selected from the group consisting of Compounds 1-5 claim 2 , 7 claim 2 , 8 claim 2 , 19-20 claim 2 , 23 claim 2 , 28 claim 2 , 30 claim 2 , 32-47 claim 2 , 56-61 claim 2 , 96 claim 2 , 100 claim 2 , 104 claim 2 , 107-117 claim 2 , 122-124 claim 2 , 126-129 claim 2 , 131 claim 2 , 133-134 claim 2 , 143-147 claim 2 , 153 claim 2 , 168-170 claim 2 , 173-179 claim 2 , 181-182 claim 2 , 185 claim 2 , 186 claim 2 , 193 claim 2 , 194 claim 2 , 196-198 claim 2 , 200 claim 2 , 203-213 claim 2 , 215 claim 2 , 218-228 claim 2 , 230 claim 2 , and 231 claim 2 , and salts and isomers thereof.113115-. (canceled)117121.-. (canceled)123131.-. (canceled)132. A nanoparticle composition comprising a lipid component comprising a compound of .133. The nanoparticle composition of claim 132 , wherein the lipid component further comprises a phospholipid selected from the group consisting of 1 claim 132 ,2-dilinoleoyl-sn-glycero-3-phosphocholine (DLPC) claim 132 , 1 claim 132 ,2-dimyristoyl-sn-glycero-phosphocholine (DMPC) claim 132 , ...

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Номер записи: 87
06-08-2015 дата публикации

AGGRECANASE INHIBITORS

Номер: US20150218107A1
Автор: DURHAM Timothy Barrett, Marimuthu Jothirajah, WILEY Michael Robert
Принадлежит: Eli Lily and Company

The present invention provides compounds having the formula: wherein Ris selected from methyl, ethyl, propyl, cyclopropyl, and dimethyl, or a pharmaceutically acceptable salt thereof, along with methods and intermediates for their preparation, and uses thereof. 110-. (canceled)16. A pharmaceutical composition comprising a compound according to claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , and at least one of a pharmaceutically acceptable carrier claim 11 , excipient claim 11 , or diluent.17. The pharmaceutical composition of claim 16 , wherein said pharmaceutical composition is adapted for oral administration.18. A method of treating arthritis in a patient in need thereof claim 11 , said method comprising administering an effective amount of a compound according to claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , to said patient.19. The method of claim 18 , wherein said patient is administered at least one additional active agent.20. The method of claim 18 , wherein said patient is a human.21. The method of claim 18 , wherein said patient is a dog.22. The method of claim 18 , wherein said administration is oral administration.23. A method of inhibiting cartilage erosion in a patient in need thereof claim 11 , said method comprising administering an effective amount of a compound according to claim 11 , or a pharmaceutically acceptable salt thereof claim 11 , to said patient.24. The method of claim 23 , wherein said patient is administered at least one additional active agent.25. The method of claim 23 , wherein said patient is a human.26. The method of claim 23 , wherein said patient is a dog.27. The method of claim 23 , wherein said administration is oral administration. Connective tissue is a required component of all mammals. It provides rigidity, differentiation, attachments, and, in some cases, elasticity. Connective tissue components include, for example, collagen, elastin, proteoglycans, fibronectin, and laminin. These ...

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Номер записи: 88
25-06-2020 дата публикации

DIARYLHYDANTOIN COMPOUNDS AND METHODS OF USE THEREOF

Номер: US20200199098A1
Автор: BARDE Anup, CHAKRAVARTY Sarvajit, CHEN Jiyun, KANKANALA Jayakanth, Nayak Anjan Kumar, Pettigrew Jeremy D., Pham Son Minh, Pujala Brahmam
Принадлежит:

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation. 3. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein Q is S.4. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein Q is O.5. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein Rand Rare each independently hydrogen claim 1 , cyano claim 1 , halo claim 1 , or Calkyl which may be further substituted with —OH claim 1 , —NH claim 1 , halo claim 1 , or —OCH.6. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein or Rand Rjoin to form a Ccycloalkyl or 4-6-membered heterocyclyl.7. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein or Rand Rjoin to form a cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , or cyclohexyl.8. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein or Rand Rjoin to form a tetrahydrofuranyl or oxetanyl.13. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , solvate claim 1 , or tautomer thereof claim 1 , wherein t is 1 or 2.26. The compound of or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , mixture of stereoisomers claim 1 , ...

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Номер записи: 89
05-08-2021 дата публикации

Diarylhydantoin compounds

Номер: US20210238145A1
Автор: Charles L. Sawyers, Charlie D. Chen, Chris Tran, Derek Welsbie, Dongwon Yoo, John Wongvipat, Michael Jung, Samedy Ouk
Принадлежит: UNIVERSITY OF CALIFORNIA

The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.

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Номер записи: 90
11-07-2019 дата публикации

DIARYLHYDANTOIN COMPOUNDS

Номер: US20190210974A1
Автор: Chen Charlie D., Jung Michael, Ouk Samedy, Sawyers Charles L., Tran Chris, Welsbie Derek, Wongvipat John, Yoo Dongwon
Принадлежит: The Regents of the University of California

The present invention relates to diarylhydantoin compounds, including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer. 151.-. (canceled) This application is a continuation of U.S. application Ser. No. 15/655,458, filed Jul. 20, 2017, which is a continuation of U.S. application Ser. No. 14/496,973, filed Sep. 25, 2014, which is a continuation of U.S. application Ser. No. 14/137,991, filed Dec. 20, 2013, which is a continuation of U.S. application Ser. No. 13/448,964, filed Apr. 17, 2012, which is a continuation of U.S. application Ser. No. 12/708,523, filed Feb. 18, 2010, which is a divisional of U.S. application Ser. No. 11/433,829, filed May 15, 2006, which claims the benefit of U.S. Provisional Application No. 60/786,837, filed Mar. 29, 2006, U.S. Provisional Application No. 60/756,552, filed Jan. 6, 2006, U.S. Provisional Application No. 60/750,351, filed Dec. 15, 2005, and U.S. Provisional Application No. 60/680,835, filed May 13, 2005, the specifications of which are hereby incorporated by reference in their entirety.This invention was made with Government support under Grant No. W81XWH-04-1-0129 awarded by the United States Army, Medical Research and Materiel Command and under Grant No. CA092131 awarded by the National Institutes of Health. The Government has certain rights in the invention.The present invention relates to diarylhydantoin compounds including diarylthiohydantoins, and methods for synthesizing them and using them in the treatment of hormone refractory prostate cancer.Prostate cancer is the most common incidence of cancer and the second leading cause of cancer death in Western men. When the cancer is confined locally, the disease can be cured by surgery or radiation. However, 30% of such cancer relapses with distant metastatic disease and others have advanced disease at diagnoses. Advanced disease is treated by castration and/or administration of antiandrogens, the so- ...

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Номер записи: 91
20-08-2015 дата публикации

Process for Extracting Polyester from an Article

Номер: US20150232632A1
Автор: Walker Adam
Принадлежит: WORN AGAIN FOOTWEAR AND ACCESSORIES LIMITED

A process for extracting polyester from an article using a solvent system comprising a compound according to any of general Formula I to VI wherein Rand Rare each independently selected from: hydrogen, alkyl, alkenyl, alkynyl, aryl or alkoxy groups; Rto Rare each independently selected from: hydrogen, alkyl, alkenyl, alkynyl, aryl or alkoxy groups; X is selected from O or S; and each of a to e is a carbon atom, wherein the total linear chain length of a-b-c-d-e is in the range of 2 to 5 carbons; Rand Rare both independently aryl groups; R, R, R, Rand Rare each independently selected from hydrogen, alkyl, alkenyl, alkynyl or aryl groups; n is an integer in the range of 1 to 8; m is 3; and 1 is an integer in the range of 1 to 3; or combination thereof. 2. A process according to claim 1 , wherein the article is fabric.3. A process according to claim 1 , wherein the article is clothing.4. A process according to claim 1 , wherein the article is plastics bottles.5. A process according to claim 1 , wherein the polyester is selected from: Polyglycolic acid (PGA) claim 1 , Polylactic acid (PLA) claim 1 , Polycaprolactone (PCL) claim 1 , Polyethylene adipate (PEA) claim 1 , Polyhydroxyalkanoate (PHA) claim 1 , Polyethylene terephthalate (PET) claim 1 , Polybutylene terephthalate (PBT) claim 1 , Polytrimethylene terephthalate (PTT) claim 1 , Polyethylene naphthalate (PEN) or combination thereof.6. A process according to a claim 5 , wherein the polyester is polyethylene terephthalate.7. A process according to claim 1 , wherein the solvent system is homogeneous.8. A process according to claim 1 , wherein the solvent system comprises one or more compounds according to any of general formulae Ito VI in an amount in the range 30% to 100% by mass of the total mass of the composition.9. A process according to claim 8 , wherein the solvent system comprises one or more compounds according to any of general formulae I to VI in an amount of at least 90% by mass of the total mass of the ...

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Номер записи: 92
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 ...

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Номер записи: 93
11-08-2016 дата публикации

DEUTERATED COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISEASES

Номер: US20160229823A1
Автор: GOPAL Damodara
Принадлежит:

The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds. 145.-. (canceled)51. The compound of claim 50 , wherein X is oxygen and Ris hydrogen.54. A pharmaceutical composition comprising a compound of claim 46 , or a pharmaceutically acceptable salt claim 46 , solvate claim 46 , ester claim 46 , or prodrug thereof; and a pharmaceutically acceptable carrier.55. A method for treating a disorder involving degeneration or dysfunction of cells expressing p75 comprising administering to a patient in need of such treatment a pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt claim 46 , solvate claim 46 , ester claim 46 , or prodrug thereof.56. The method of wherein the disorder is a neurodegenerative disorder.57. The method of wherein the disorder is selected from the group consisting of Alzheimer's disease claim 55 , Huntington's disease claim 55 , Pick's disease claim 55 , amyotrophic lateral sclerosis claim 55 , epilepsy claim 55 , Parkinson's disease claim 55 , spinal cord injury claim 55 , stroke claim 55 , hypoxia claim 55 , ischemia claim 55 , brain injury claim 55 , diabetic neuropathy claim 55 , peripheral neuropathy claim 55 , nerve transplantation claim 55 , multiple sclerosis claim 55 , peripheral nerve injury claim 55 , retinal degeneration claim 55 , and hair loss.58. The method of wherein the disorder is selected from the group consisting of Alzheimer's disease claim 57 , Huntington's disease claim 57 , epilepsy claim 57 , spinal cord injury claim 57 , ischemia claim 57 , brain injury claim 57 , peripheral neuropathy claim 57 , retinal degeneration claim 57 , and hair loss. The present application is a U.S. national stage application under 35 U.S.C. §371 of International Application No. ...

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Номер записи: 94
19-08-2021 дата публикации

2-NAPHTHIMIDAMIDES, ANALOGUES THEREOF, AND METHODS OF TREATMENT USING SAME

Номер: US20210251942A1
Автор: Benam Kambez Hajipouran
Принадлежит:

The present invention relates in certain aspects to the discovery of novel 2-naphthimidamide compounds that are capable of binding Type II Transmembrane Serine Proteases (TTSPs). In certain embodiments, the compounds of the invention can be used to treat or prevent Influenza A viral infection in a mammal. 2. The compound of claim 1 , wherein each occurrence of heteroaryl or heterocyclyl is independently selected from the group consisting of pyridyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , isoxazolyl claim 1 , oxazolyl claim 1 , thiazolyl claim 1 , imidazolyl claim 1 , imidazolidin-2-one-1-yl claim 1 , 1 claim 1 ,5-dihydro-2H-imidazol-2-one-1-yl claim 1 , 2-pyrazolyl claim 1 , 1 claim 1 ,2 claim 1 ,3-triazolyl claim 1 , 1 claim 1 ,2 claim 1 ,4-triazolyl claim 1 , uracil claim 1 , thyminyl claim 1 , pyranyl claim 1 , furanyl claim 1 , and hydantoinyl.3. The compound of claim 1 , wherein each occurrence of alkyl claim 1 , alkoxy claim 1 , cycloalkyl claim 1 , phenyl claim 1 , heteroaryl claim 1 , or heterocyclyl is independently optionally substituted with at least one group selected from the group consisting of —CN claim 1 , —OR′ claim 1 , —NR′R′ claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , Calkyl claim 1 , Ccycloalkyl claim 1 , phenyl claim 1 , heteroaryl claim 1 , and heterocyclyl claim 1 , wherein each occurrence of R′ is independently selected from the group consisting of H and C-Calkyl.7. A pharmaceutical composition comprising the compound of claim 1 , further comprising at least one pharmaceutically acceptable carrier.8. The pharmaceutical composition of claim 7 , further comprising at least one additional therapeutic agent.9. The pharmaceutical composition of claim 8 , wherein the at least one additional therapeutic agent is an antiviral agent. The present application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Patent Application No. 62/683,480, filed Jun. 11, 2018, which application is incorporated herein by ...

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Номер записи: 95
09-07-2020 дата публикации

5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS

Номер: US20200216397A1
Автор: ALVEY Luke Jonathan, Amantini David, BREBION Franck Laurent, DE CEUNINCK Frédéric André, DEPREZ Pierre Marc Marie Joseph, Gosmini Romain Luc Marie, JARY Hélène Marie, PEIXOTO Christophe, POP-BOTEZ Iuliana Ecaterina, VARIN Marie Laurence Claire
Принадлежит:

The present invention discloses compounds according to Formula I: 118-. (canceled)19. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of a compound , wherein the compound is5-[3-[(3S)-4-(3-chloro-4-fluoro-phenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,5-[3-[(3S)-4-(3-chloro-5-fluoro-phenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,(5S)-5-cyclopropyl-5-[3-[(3S)-4-(3,4-dichlorophenyl)-3-methyl-piperazin-1-yl]-3-oxo-propyl]imidazolidine-2,4-dione,(5S)-5-cyclopropyl-5-[(2S)-3-[(3S)-4-(3,4-difluorophenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]imidazolidine-2,4-dione,5-[3-[(3S)-4-(4-chlorophenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,5-[3-[4-(3,4-difluorophenyl)piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-(methoxymethyl)imidazolidine-2,4-dione,5-[2-[4-(3,5-dichlorophenyl)piperazine-1-carbonyl]butyl]-5-methyl-imidazolidine-2,4-dione,(S)-5-((S)-3-((S)-4-(3-chloro-4-fluorophenyl)-3-methylpiperazin-1-yl)-2-methyl-3-oxopropyl)-5-(methoxymethyl) imidazolidine-2,4-dione,5-[3-[4-(3-chlorophenyl)piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,5-[3-[4-(3-chloro-2-methyl-phenyl)piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-cyclopropyl-imidazolidine-2,4-dione,tert-butyl N-[2-[4-[3-[4-(3,4-difluorophenyl) piperazin-1-yl]-2-methyl-3-oxo-propyl]-2,5-dioxo-imidazolidin-4-yl]ethyl]carbamate,(5S)-5-cyclopropyl-5-[3-[(3S)-4-(3,5-dichlorophenyl)-3-methyl-piperazin-1-yl]-3-oxo-propyl]imidazolidine-2,4-dione,5-[3-[(3S)-4-(3-chloro-4-fluoro-phenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-(2-pyridyl) imidazolidine-2,4-dione,5-cyclopropyl-5-[3-[4-(3,5-dichlorophenyl)piperazin-1-yl]-2-methyl-3-oxo-propyl]imidazolidine-2,4-dione,(5R)-5-[(2S)-3-[(3S)-4-(3-chloro-4-fluoro-phenyl)-3-methyl-piperazin-1-yl]-2-methyl-3-oxo-propyl]-5-methyl-imidazolidine-2,4- ...

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Номер записи: 96
18-08-2016 дата публикации

Method, device, and system for radio resource management measurement

Номер: US20160242083A1
Автор: David Jean-Marie Mazzarese, Lei GUAN, Lixia Xue
Принадлежит: Huawei Technologies Co Ltd

Embodiments provide a method for radio resource management measurement. The method includes: determining, by a UE according to a detected first reference signal, a first resource on which the detected first reference signal is located; determining, by the UE, a reference signal received power RSRP of a target cell according to a received power of the detected first reference signal carried on the first resource; determining, by the UE, a second resource; determining, by the UE, a received signal strength indicator RSSI of the target cell according to a total received power on the second resource; and determining, by the UE, reference signal received quality RSRQ or a signal to interference plus noise ratio SINR of the target cell or both according to the RSRP and RSSI. The method is applied to radio resource management measurement.

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Номер записи: 97
01-08-2019 дата публикации

Composition for the prevention and elimination of odors

Номер: US20190231915A1
Автор: Jeffrey F. Williams, Simon Johnston
Принадлежит: Oxiscience LLC

Articles can be provided with odor resistance by applying a dispersion of a halogenated heterocyclic N-halamine in an inert liquid carrier onto the surface of the article and allowing the inert liquid carrier to penetrate into it. The N-halamine accordingly becomes deposited on the surface of the article after the inert liquid carrier penetrates into the article. This method can be used to provide odor resistance to a variety of substrates, including garbage bags. It can also be used to deposit other functional particulates onto the surface of substrates having sufficient porosity to take up the vehicle. For instance, such functional particles can be oxidants that display antimicrobial and/or enzyme inhibitory efficacy or particles having toxin interaction potentials through oxidative degradation or adsorption of toxic substances in air and/or water, such as fluoride uptake by metal oxide microparticles.

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Номер записи: 98
01-08-2019 дата публикации

COMPOSITION FOR THE PREVENTION AND ELIMINATION OF ODORS

Номер: US20190231916A1
Автор: JOHNSTON Simon, Williams Jeffrey F.
Принадлежит: OXISCIENCE, LLC

Articles can be provided with odor resistance by applying a dispersion of a halogenated heterocyclic N-halamine in an inert liquid carrier onto the surface of the article and allowing the inert liquid carrier to penetrate into it. The N-halamine accordingly becomes deposited on the surface of the article after the inert liquid carrier penetrates into the article. This method can be used to provide odor resistance to a variety of substrates, including garbage bags. It can also be used to deposit other functional particulates onto the surface of substrates having sufficient porosity to take up the vehicle. For instance, such functional particles can be oxidants that display antimicrobial and/or enzyme inhibitory efficacy or particles having toxin interaction potentials through oxidative degradation or adsorption of toxic substances in air and/or water, such as fluoride uptake by metal oxide microparticles. 1. A garbage bag having walls which are comprised of polyethylene , wherein said walls of the garbage bag are coated with particles of a halogenated heterocyclic N-halamine having a particle size which is within the range of about 0.01 μm to 20 μm , and wherein the particles of the halogenated heterocyclic N-halamine are present only on the surface of the walls of the garbage bag.3. The garbage bag of wherein the partially halogenated hydantoin is monochloro-5 claim 2 ,5-dimethyl hydantoin.4. The garbage bag of wherein Rand Rrepresent an alkyl group containing from 1 to 4 carbon atoms.5. The garbage bag of wherein said halogen atoms are selected from the group consisting of chlorine atoms and bromine atoms.6. The garbage bag of wherein said halogen atoms are chlorine atoms.7. The garbage bag of wherein the partially halogenated hydantoin is selected from the group consisting of Cl-dimethyl hydantoin claim 2 , Cl-dimethyl hydantoin claim 2 , Cl-dimethyl hydantoin claim 2 , Cl-dimethyl hydantoin claim 2 , monochloro-5 claim 2 ,5-dimethyl hydantoin (MCDMH) claim 2 , Br ...

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Номер записи: 99
10-09-2015 дата публикации

INHIBITORS OF PEPTIDYL ARGININE DEIMINASE (PAD) ENZYMES AND USES THEREOF

Номер: US20150252006A1
Автор: Kotra Lakshmi, Moscarello Mario
Принадлежит:

The present application relates to imidazolidinecliones, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with the hypercitrullination of proteins by peptidyl arginine deiminase (PAD) enzymes. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: (I). 2. The compound of claim 1 , wherein Rand Rare independently Calkyl.3. (canceled)4. The compound of claim 1 , wherein Rand Rare independently CalkyleneR; wherein Ris selected from COOR claim 1 , Ph claim 1 , Ccycloalkyl and NHR; wherein Ris selected from H and Calkyl claim 1 , and Ris selected from H claim 1 , Ac and Bz.5. The compound of claim 4 , wherein Rand Rare independently selected from CHCOOCH claim 4 , CHCOOtBu claim 4 , CHCHCOOH claim 4 , CHCHCHCOOH claim 4 , CHPh claim 4 , CHCHPh claim 4 , CH-cyclohexyl claim 4 , CHCHNH claim 4 , CHCHCHNH claim 4 , CHCHNHAc claim 4 , CHCHNHBz claim 4 , CHCHCHNHAc and CHCHCHNHBz.9. (canceled)10. (canceled)11. (canceled)13. The compound of claim 1 , in the form of a pharmaceutically acceptable salt.14. (canceled)15. A pharmaceutical composition comprising one or more compounds of and a pharmaceutically acceptable carrier.17. The method of claim 16 , wherein Rand Rare independently Calkyl.18. (canceled)19. The method of claim 16 , wherein Rand Rare independently CalkyleneR; wherein Ris selected from COOR claim 16 , Ph claim 16 , Ccycloalkyl and NHR; wherein Ris selected from H and Calkyl claim 16 , and Ris selected from H claim 16 , Ac and Bz.20. The method of claim 19 , wherein Rand Rare independently selected from CHCOOCH claim 19 , CHCOOtBu claim 19 , CHCHCOOH claim 19 , CHCHCHCOOH claim 19 , CHPh claim 19 , CHCHPh claim 19 , CH-cyclohexyl claim 19 , CHCHNH claim 19 , CHCHCHNH claim 19 , CHCHNHAc claim 19 , CHCHNHBz claim 19 , CHCHCHNHAc and CHCHCHNHBz.24. (canceled)25. (canceled)26. (canceled)28. The method of claim ...

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Номер записи: 100