EA202191896A1 - Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2н-пиридо[1,2-]пиразин-7-карбоксамиды - ингибиторы интегразы вич, способы их получения и применения - Google Patents

Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2н-пиридо[1,2-]пиразин-7-карбоксамиды - ингибиторы интегразы вич, способы их получения и применения

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Publication number
EA202191896A1
EA202191896A1 EA202191896A EA202191896A EA202191896A1 EA 202191896 A1 EA202191896 A1 EA 202191896A1 EA 202191896 A EA202191896 A EA 202191896A EA 202191896 A EA202191896 A EA 202191896A EA 202191896 A1 EA202191896 A1 EA 202191896A1
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Eurasian Patent Office
Prior art keywords
dioxo
hydroxy
pyrazine
tetrahydro
carboxamide
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EA202191896A
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English (en)
Inventor
Андрей Александрович ИВАЩЕНКО
Александр Васильевич ИВАЩЕНКО
Николай Филиппович САВЧУК
Олег Дмитриевич МИТЬКИН
Original Assignee
Андрей Александрович ИВАЩЕНКО
Александр Васильевич ИВАЩЕНКО
Николай Филиппович САВЧУК
ИВАЩЕНКО, Алена Александровна
Алла Хем, Ллс
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Publication of EA202191896A1 publication Critical patent/EA202191896A1/ru

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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
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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Abstract

Изобретение относится к новому соединению, обладающему противовирусной активностью, в частности ингибиторной активностью в отношении интегразы вируса иммунодефицита человека (ВИЧ). Предметом настоящего изобретения является новый аннелированный 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2H-пиридо[1,2-]пиразин-7-карбоксамид, общей формулы 1 и 2, его стереоизомер, его фармацевтически приемлемая соль, его сольват, его кристаллическая или его поликристаллическая формагде кольцо A1 представляет собой необязательно замещенный метилом 5-7-членный насыщенный гетероцикл или гетеробицикл, кольцо A2 представляет собой 5-6-членный необязательно замещенный метилом насыщенный или частично насыщенный моноциклический гетероцикл, кольцо A3 представляет собой 5-6-членный моноциклический насыщенный циклоалкан и тетрагидро-2H-пиран, R представляет собой 5-7-членный необязательно замещенный одним, двумя или тремя необязательно одинаковыми заместителями моноциклический или бициклический гетероциклический радикал, включающий 1-4 гетероатома, выбранных из ряда O, S и N, исключая (2S,5R,11aS)-8-гидрокси-7,9-диоксо-N-{[3-(трифторметил)пиридин-2-ил]метил}-2,3,4,5,7,9,13,13a-октагидро-2,5-метанпиридо[1',2':4,5]пиразино[2,1-b][1,3]оксазепино-10-карбоксамид (формулы A4) и (1R,4S,12aR)-N-[(3,5-дифторпиридин-2-ил)метил]-7-гидрокси-6,8-диоксо-1,2,3,4,6,8,12,12a-октагидро-1,4-метанодипиридо[1,2-a:1',2'-d]пиразин-9-карбоксамид (формулы A5).
EA202191896A 2019-06-03 2020-03-05 Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2н-пиридо[1,2-]пиразин-7-карбоксамиды - ингибиторы интегразы вич, способы их получения и применения EA202191896A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2019117193A RU2717101C1 (ru) 2019-06-03 2019-06-03 Анелированные 9-гидрокси-1,8-диоксо-1,3,4,8-тетрагидро-2Н-пиридо[1,2-a]пиразин-7-карбоксамиды - ингибиторы интегразы ВИЧ, способы их получения и применения
PCT/RU2020/000118 WO2020246910A1 (ru) 2019-06-03 2020-03-05 АНЕЛИРОВАННЫЕ 9-ГИДРОКСИ- 1,8 - ДИОКСО- 1, 3,4, 8 -ТЕТРАГИДРО-2Н-ПИРИДО [1,2-α] ПИРАЗИН-7 - КАРБОКСАМИДЫ - ИНГИБИТОРЫ ИНТЕГРАЗЫ ВИЧ

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EA202191896A1 true EA202191896A1 (ru) 2021-10-12

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US (1) US20230020329A1 (ru)
EP (1) EP3978503A4 (ru)
CN (1) CN113710675A (ru)
BR (1) BR112021024439A2 (ru)
EA (1) EA202191896A1 (ru)
MX (1) MX2021010512A (ru)
RU (1) RU2717101C1 (ru)
WO (1) WO2020246910A1 (ru)

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RU2659388C1 (ru) 2017-02-28 2018-07-02 Васильевич Иващенко Александр Нуклеотиды, включающие N-[(S)-1-циклобутоксикарбонил]фосфорамидатный фрагмент, их аналоги и их применение
RU2665383C9 (ru) * 2017-06-22 2019-07-23 Общество с ограниченной ответственностью "Вириом" Фармацевтическая наносуспензия для терапии ВИЧ-инфекции
RU2674576C1 (ru) 2017-08-10 2018-12-11 Федеральное государственное автономное образовательное учреждение высшего образования "Крымский федеральный университет имени В.И. Вернадского" Рабочий орган культиватора

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EP3978503A1 (en) 2022-04-06
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