RU2697393C2 - Кристаллическая твердая форма соли бензолсульфоновой кислоты и 2-[(4S)-6-(4-хлорфенил)-1-метил-8-(метилокси)-4H-[1,2,4]триазоло[4,3-a][1,4]бензодиазепин-4-ил]-N-этилацетамида, способ ее получения и фармацевтическая композиция, содержащая ее - Google Patents

Кристаллическая твердая форма соли бензолсульфоновой кислоты и 2-[(4S)-6-(4-хлорфенил)-1-метил-8-(метилокси)-4H-[1,2,4]триазоло[4,3-a][1,4]бензодиазепин-4-ил]-N-этилацетамида, способ ее получения и фармацевтическая композиция, содержащая ее Download PDF

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RU2697393C2
RU2697393C2 RU2017107760A RU2017107760A RU2697393C2 RU 2697393 C2 RU2697393 C2 RU 2697393C2 RU 2017107760 A RU2017107760 A RU 2017107760A RU 2017107760 A RU2017107760 A RU 2017107760A RU 2697393 C2 RU2697393 C2 RU 2697393C2
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ethylacetamide
triazolo
chlorophenyl
methyloxy
benzodiazepin
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RU2017107760A
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Russian (ru)
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RU2017107760A3 (enExample
RU2017107760A (ru
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Госсетт Августус КЭМПБЕЛЛ
Аса Элизабет ГЛАДВИН
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ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед
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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
RU2017107760A 2014-10-02 2015-09-30 Кристаллическая твердая форма соли бензолсульфоновой кислоты и 2-[(4S)-6-(4-хлорфенил)-1-метил-8-(метилокси)-4H-[1,2,4]триазоло[4,3-a][1,4]бензодиазепин-4-ил]-N-этилацетамида, способ ее получения и фармацевтическая композиция, содержащая ее RU2697393C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462058753P 2014-10-02 2014-10-02
US62/058,753 2014-10-02
PCT/EP2015/072515 WO2016050821A1 (en) 2014-10-02 2015-09-30 Compound

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RU2017107760A RU2017107760A (ru) 2018-11-02
RU2017107760A3 RU2017107760A3 (enExample) 2019-03-01
RU2697393C2 true RU2697393C2 (ru) 2019-08-14

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US (3) US9975901B2 (enExample)
EP (1) EP3201199A1 (enExample)
JP (1) JP2017530155A (enExample)
KR (1) KR20170055549A (enExample)
CN (1) CN106715439A (enExample)
AU (1) AU2015326910B2 (enExample)
BR (1) BR112017006342A2 (enExample)
CA (1) CA2960090A1 (enExample)
RU (1) RU2697393C2 (enExample)
WO (1) WO2016050821A1 (enExample)

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KR102438072B1 (ko) 2012-01-12 2022-08-31 예일 유니버시티 E3 유비퀴틴 리가아제에 의한 표적 단백질 및 다른 폴리펩티드의 증진된 분해를 위한 화합물 및 방법
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
RU2745999C1 (ru) * 2014-12-05 2021-04-05 Х. Ли Моффитт Кэнсер Сентер Энд Рисёч Инститьют, Инк. Ингибитор бромодомена в качестве адъюванта в противоопухолевой иммунотерапии
AU2016232705C1 (en) 2015-03-18 2021-06-17 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
EP3319944A4 (en) 2015-07-10 2019-04-24 Arvinas, Inc. MDM2-BASED MODULATORS OF PROTEOLYSIS AND RELATED USE METHODS
EP3337476A4 (en) 2015-08-19 2019-09-04 Arvinas, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
US20170281784A1 (en) 2016-04-05 2017-10-05 Arvinas, Inc. Protein-protein interaction inducing technology
RU2019117356A (ru) 2016-11-10 2020-12-10 Лосинь Фармасьютикал (Шанхай) Ко., Лтд. Азотсодержащее макроциклическое соединение, способ его получения, фармацевтическая композиция и применение
IL319363A (en) 2017-01-31 2025-05-01 Arvinas Operations Inc Cervalon ligands and bifunctional compounds containing them
JP2021512153A (ja) 2018-01-26 2021-05-13 イエール ユニバーシティ タンパク質分解のイミド系モジュレーターおよび使用方法
CA3095912A1 (en) 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same
WO2021127443A1 (en) 2019-12-19 2021-06-24 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
CN111533745A (zh) * 2020-05-20 2020-08-14 成都药明康德新药开发有限公司 叔丁基-3-(氨基甲基)二氢-5h-三唑并二氮杂卓-8(9h)-甲酸基酯制法
WO2025049555A1 (en) 2023-08-31 2025-03-06 Oerth Bio Llc Compositions and methods for targeted inhibition and degradation of proteins in an insect cell

Citations (4)

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EP0934940A1 (en) * 1996-06-12 1999-08-11 Japan Tobacco Inc. Cytokine production inhibitors, triazepine compounds, and intermediates thereof
EP2239264A1 (en) * 2007-12-28 2010-10-13 Mitsubishi Tanabe Pharma Corporation Antitumor agent
EA201290183A1 (ru) * 2009-11-05 2012-12-28 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Бензодиазепиновый ингибитор бромодомена
EA201290184A1 (ru) * 2009-11-05 2012-12-28 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Бензодиазепиновый ингибитор бромодомена

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GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
PT2773354T (pt) * 2011-11-01 2019-07-17 Resverlogix Corp Formulações orais de libertação imediata para quinazolinonas substituídas
US9492460B2 (en) * 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors

Patent Citations (4)

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Publication number Priority date Publication date Assignee Title
EP0934940A1 (en) * 1996-06-12 1999-08-11 Japan Tobacco Inc. Cytokine production inhibitors, triazepine compounds, and intermediates thereof
EP2239264A1 (en) * 2007-12-28 2010-10-13 Mitsubishi Tanabe Pharma Corporation Antitumor agent
EA201290183A1 (ru) * 2009-11-05 2012-12-28 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Бензодиазепиновый ингибитор бромодомена
EA201290184A1 (ru) * 2009-11-05 2012-12-28 ГЛАКСОСМИТКЛАЙН ЭлЭлСи Бензодиазепиновый ингибитор бромодомена

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CA2960090A1 (en) 2016-04-07
US9975901B2 (en) 2018-05-22
RU2017107760A3 (enExample) 2019-03-01
JP2017530155A (ja) 2017-10-12
EP3201199A1 (en) 2017-08-09
AU2015326910B2 (en) 2018-03-01
RU2017107760A (ru) 2018-11-02
US10450319B2 (en) 2019-10-22
BR112017006342A2 (pt) 2017-12-19
US20180305365A1 (en) 2018-10-25
WO2016050821A1 (en) 2016-04-07
US20190389870A1 (en) 2019-12-26
KR20170055549A (ko) 2017-05-19
CN106715439A (zh) 2017-05-24
US20170298071A1 (en) 2017-10-19
AU2015326910A1 (en) 2017-03-30

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