RU2016146581A - Макроциклические антибиотики широкого спектра действия - Google Patents

Макроциклические антибиотики широкого спектра действия Download PDF

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RU2016146581A
RU2016146581A RU2016146581A RU2016146581A RU2016146581A RU 2016146581 A RU2016146581 A RU 2016146581A RU 2016146581 A RU2016146581 A RU 2016146581A RU 2016146581 A RU2016146581 A RU 2016146581A RU 2016146581 A RU2016146581 A RU 2016146581A
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alkyl
optionally substituted
independently
aryl
cycloalkyl
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RU2016146581A
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RU2016146581A3 (OSRAM
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Такер Каррэн РОБЕРТС
Питер Эндрю Смит
Роберт И. ХАЙГУЧИ
Прасуна Параселли
Филиппе БЕРГЕРОН
Майкл Ф.Т. КЁЛЕР
Хуэйюн ХУ
Джейкоб Брэдли Шварц
Цуон ЛИ
Джеймс КРОФОРД
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АрКьюЭкс ФАРМАСЪЮТИКЛС, ИНК.
Дженентек, Инк.
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    • A61K31/407Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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RU2016146581A 2014-05-20 2015-05-19 Макроциклические антибиотики широкого спектра действия RU2016146581A (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462000980P 2014-05-20 2014-05-20
US62/000,980 2014-05-20
US201562142404P 2015-04-02 2015-04-02
US62/142,404 2015-04-02
PCT/US2015/031631 WO2015179441A2 (en) 2014-05-20 2015-05-19 Macrocyclic broad spectrum antibiotics

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RU2016146581A true RU2016146581A (ru) 2018-06-21
RU2016146581A3 RU2016146581A3 (OSRAM) 2018-12-20

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US (1) US10392422B2 (OSRAM)
EP (1) EP3145944B1 (OSRAM)
JP (2) JP6823588B2 (OSRAM)
KR (1) KR20170027721A (OSRAM)
CN (1) CN106661084B (OSRAM)
BR (1) BR112016027232A2 (OSRAM)
CA (1) CA2949681A1 (OSRAM)
MX (1) MX2016015218A (OSRAM)
RU (1) RU2016146581A (OSRAM)
WO (1) WO2015179441A2 (OSRAM)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10501493B2 (en) 2011-05-27 2019-12-10 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
RU2016146581A (ru) 2014-05-20 2018-06-21 АрКьюЭкс ФАРМАСЪЮТИКЛС, ИНК. Макроциклические антибиотики широкого спектра действия
EP3377474B1 (en) * 2015-11-20 2023-08-16 RQX Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
TWI725075B (zh) * 2015-11-20 2021-04-21 美商Rqx製藥公司 巨環廣效抗生素
JPWO2017122697A1 (ja) * 2016-01-13 2018-12-06 Jsr株式会社 感放射線性樹脂組成物、レジストパターン形成方法、酸拡散制御剤及び化合物
AU2017229591B2 (en) * 2016-03-09 2021-08-19 Blade Therapeutics Pty Ltd Calpain modulators and methods of production and use thereof
WO2017156071A1 (en) 2016-03-09 2017-09-14 Blade Therapeutics, Inc. Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof
WO2018009417A1 (en) 2016-07-05 2018-01-11 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
JP2020500207A (ja) 2016-09-28 2020-01-09 ブレード・セラピューティクス・インコーポレイテッド カルパインモジュレーター及びそれらの治療上の使用
EP3330260A1 (en) * 2016-12-01 2018-06-06 Enantia, S.L. Process for the preparation of an intermediate for the synthesis of i.a. carfilzomib
IL268483B2 (en) * 2017-02-15 2024-02-01 Rqx Pharmaceuticals Inc Macrocyclic broad spectrum antibiotics
CA3057443A1 (en) 2017-03-21 2018-09-27 The Scripps Research Institute Cu-and ni-catalyzed decarboxylative borylation reactions
CN106966947B (zh) * 2017-03-30 2019-09-03 河北医科大学 一种维格列汀的制备方法
JP7634988B2 (ja) * 2017-12-15 2025-02-25 メルク パテント ゲーエムベーハー 有機エレクトロルミネッセントデバイスに使用するための置換芳香族アミン
CN108806787B (zh) * 2018-07-06 2022-04-05 上海长海医院 面向临床手术的医用耗材智能监控系统
CN109355404B (zh) * 2018-08-30 2022-03-29 华南理工大学 基于聚合酶螺旋反应恒温检测单增李斯特菌的引物、试剂盒及检测方法
EP3852786A4 (en) * 2018-09-19 2022-09-28 Georgia Tech Research Corporation SELF-TITRATEING BACTERIAL PROTEASE-ACTIVATED PRODRUG
IL295889B2 (en) * 2019-05-28 2025-01-01 Hoffmann La Roche Broad-spectrum macrocyclic antibiotic
CN118063337B (zh) * 2024-02-19 2025-01-28 绵阳师范学院 一种(s)-3-氨基-2-戊酮盐酸盐的制备方法

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3128280A (en) 1959-10-23 1964-04-07 Searle & Co 1-(alkoxylated/halogenated phenyl)-3-pyridylmethylureas
US5204328A (en) 1990-06-26 1993-04-20 Merck & Co., Inc. Peptides having atrial natriuretic factor activity
EP0895999A1 (en) 1997-08-06 1999-02-10 Pfizer Products Inc. C-4" substituted macrolide antibiotics
GB9902399D0 (en) 1999-02-03 1999-03-24 Smithkline Beecham Plc Compounds
US6660832B1 (en) 1999-08-20 2003-12-09 Isis Pharmaceuticals, Inc. Macrocyclic compounds and preparation methods thereof
US6951840B2 (en) * 2001-08-31 2005-10-04 Eli Lilly And Company Lipoglycopeptide antibiotics
DE10226921A1 (de) 2002-06-17 2003-12-24 Bayer Ag Antibakterielle Amid-Makrozyklen
CA2530063A1 (en) 2003-06-26 2005-01-06 Migenix Inc. Compositions of lipopeptide antibiotic derivatives and methods of use thereof
DE10358824A1 (de) * 2003-12-16 2005-07-21 Bayer Healthcare Ag Antibakterielle Makrozyklen mit substituiertem Biphenyl
DE102005014247A1 (de) 2005-03-30 2006-10-05 Aicuris Gmbh & Co. Kg Antibakterielle Amid-Makrozyklen VI
DE102005014245A1 (de) 2005-03-30 2006-10-05 Aicuris Gmbh & Co. Kg Antibakterielle Amid-Makrozyklen V
BR112012021806A2 (pt) 2010-03-01 2015-09-08 Myrexis Inc compostos e seus usos terapêusticos.
BR112012021931A2 (pt) * 2010-03-09 2016-05-31 Merck Canada Inc composto, composição farmacêutica, método para tratar uma infecção bacteriana, e, uso de composto
WO2011120071A1 (en) 2010-04-01 2011-10-06 The University Of Queensland Oxytocin peptide analogues
KR20130105659A (ko) * 2010-09-15 2013-09-25 더 스크립스 리서치 인스티튜트 광범위 스펙트럼 항생제 아릴로마이신 유사체
WO2012166665A2 (en) * 2011-05-27 2012-12-06 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
US10501493B2 (en) 2011-05-27 2019-12-10 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
CA2867448A1 (en) * 2012-03-14 2013-09-19 Floyd E. Romesberg Broad spectrum antibiotic arylomycin analogs
CN103788176A (zh) 2012-10-31 2014-05-14 上海来益生物药物研究开发中心有限责任公司 一种arylomycin类化合物及其制备方法和应用
CA2892027A1 (en) * 2012-11-21 2014-05-30 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
RU2016146581A (ru) 2014-05-20 2018-06-21 АрКьюЭкс ФАРМАСЪЮТИКЛС, ИНК. Макроциклические антибиотики широкого спектра действия
ITUB20154591A1 (it) 2015-10-12 2017-04-12 Crestoptics S R L Apparato di microscopia confocale e relativo procedimento di acquisizione ed elaborazione di immagini
TWI725075B (zh) 2015-11-20 2021-04-21 美商Rqx製藥公司 巨環廣效抗生素
EP3377474B1 (en) 2015-11-20 2023-08-16 RQX Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics

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BR112016027232A2 (pt) 2018-06-26
JP6823588B2 (ja) 2021-02-03
CN106661084A (zh) 2017-05-10
EP3145944A2 (en) 2017-03-29
EP3145944A4 (en) 2018-01-03
RU2016146581A3 (OSRAM) 2018-12-20
CN106661084B (zh) 2021-08-31
WO2015179441A2 (en) 2015-11-26
CA2949681A1 (en) 2015-11-26
JP2017517567A (ja) 2017-06-29
KR20170027721A (ko) 2017-03-10
US20170088582A1 (en) 2017-03-30
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