EA201270602A1 - N-((1r,2s,5r)-5-(трет-бутиламино)-2-((s)-3-(7-трет-бутилпиразоло[1,5-а][1,3,5]триазин-4-иламино)-2-оксопирролидин-1-ил)циклогексил)ацетамид в качестве двойного модулятора активности хемокиновых рецепторов, его кристаллические формы и способы получения - Google Patents

N-((1r,2s,5r)-5-(трет-бутиламино)-2-((s)-3-(7-трет-бутилпиразоло[1,5-а][1,3,5]триазин-4-иламино)-2-оксопирролидин-1-ил)циклогексил)ацетамид в качестве двойного модулятора активности хемокиновых рецепторов, его кристаллические формы и способы получения

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EA201270602A1
EA201270602A1 EA201270602A EA201270602A EA201270602A1 EA 201270602 A1 EA201270602 A1 EA 201270602A1 EA 201270602 A EA201270602 A EA 201270602A EA 201270602 A EA201270602 A EA 201270602A EA 201270602 A1 EA201270602 A1 EA 201270602A1
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Prior art keywords
tret
oxopyrrolidin
triazin
butylamino
compounds
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EA201270602A
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English (en)
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EA020486B1 (ru
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Перси Х. Картер
Роберт Дж. Черни
Виктор В. Россо
Хун Ли
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Бристол-Майерс Сквибб Кампани
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Publication of EA201270602A1 publication Critical patent/EA201270602A1/ru
Publication of EA020486B1 publication Critical patent/EA020486B1/ru

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Abstract

В настоящем изобретении предложен новый антагонист, N-((1R,2S,5R)-5-(трет-бутиламино)-2-((S)-3 -(7-терет-бутилпиразоло[1,5-а][1,3,5]триазин-4-иламино)-2-оксопирролидин-1-ил)циклогексил)ацетамидили его фармацевтически приемлемая соль, сольват или пролекарство, обладающий неожиданной двойной активностью в отношении рецепторов CCR-2 и CCR-5. В настоящем изобретении также предложены кристаллические формы, метаболиты, фармацевтические композиции, содержащие указанные соединения, и способы применения этих соединений в качестве агентов для лечения воспалительных заболеваний, аллергических, аутоиммунных, метаболических, раковых и/или сердечно-сосудистых заболеваний. В настоящем изобретении также предложены способы получения соединений формулы (I), таких, как предложено в изобретении, включая N-((1R,2S,5R)-5-(трет-бутиламино)-2-((S)-3-(7-трет-бутилпиразоло[1,5-а][1,3,5]триазин-4-иламино)-2-оксопирролидин-1-ил)циклогексил)ацетамид. В данном изобретении также предложены соединения, которые могут быть использованы в качестве промежуточных соединений в способе получения соединений согласно настоящему изобретению.
EA201270602A 2009-10-13 2010-10-12 N-((1R,2S,5R)-5-(ТРЕТ-БУТИЛАМИНО)-2-((S)-3-(7-ТРЕТ-БУТИЛПИРАЗОЛО[1,5-a][1,3,5]ТРИАЗИН-4-ИЛАМИНО)-2-ОКСОПИРРОЛИДИН-1-ИЛ)ЦИКЛОГЕКСИЛ)АЦЕТАМИД В КАЧЕСТВЕ ДВОЙНОГО МОДУЛЯТОРА АКТИВНОСТИ ХЕМОКИНОВЫХ РЕЦЕПТОРОВ, ЕГО КРИСТАЛЛИЧЕСКИЕ ФОРМЫ И СПОСОБ ПОЛУЧЕНИЯ EA020486B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25097809P 2009-10-13 2009-10-13
PCT/US2010/052288 WO2011046916A1 (en) 2009-10-13 2010-10-12 N-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes

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EA201270602A1 true EA201270602A1 (ru) 2012-10-30
EA020486B1 EA020486B1 (ru) 2014-11-28

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EA201270602A EA020486B1 (ru) 2009-10-13 2010-10-12 N-((1R,2S,5R)-5-(ТРЕТ-БУТИЛАМИНО)-2-((S)-3-(7-ТРЕТ-БУТИЛПИРАЗОЛО[1,5-a][1,3,5]ТРИАЗИН-4-ИЛАМИНО)-2-ОКСОПИРРОЛИДИН-1-ИЛ)ЦИКЛОГЕКСИЛ)АЦЕТАМИД В КАЧЕСТВЕ ДВОЙНОГО МОДУЛЯТОРА АКТИВНОСТИ ХЕМОКИНОВЫХ РЕЦЕПТОРОВ, ЕГО КРИСТАЛЛИЧЕСКИЕ ФОРМЫ И СПОСОБ ПОЛУЧЕНИЯ
EA201490744A EA201490744A1 (ru) 2009-10-13 2010-10-12 N-((1r,2s,5r)-5-(трет-бутиламино)-2-((s)-3-(7-трет-бутилпиразоло[1,5-a][1,3,5]триазин-4-иламино)-2-оксопирролидин-1-ил)циклогексил)ацетамид в качестве двойного модулятора активности хемокиновых рецепторов, его кристаллическая форма и способ получения

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CN106456641A (zh) * 2014-07-17 2017-02-22 参天制药株式会社 眼后段疾病的预防或治疗剂
KR102205368B1 (ko) 2016-09-14 2021-01-20 노파르티스 아게 Fxr 작용제의 신규 요법
JOP20190040A1 (ar) 2016-09-14 2019-03-10 Novartis Ag توليفة من ناهضات fxr
CA3070423A1 (en) 2017-07-20 2019-01-24 Bristol-Myers Squibb Company Process for the preparation of n-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide
AU2019209435A1 (en) * 2018-01-22 2020-09-17 Bristol-Myers Squibb Company Compositions and methods of treating cancer
JP2023501584A (ja) * 2019-11-13 2023-01-18 ラプト・セラピューティクス・インコーポレイテッド Ｃ－ｃケモカイン受容体４型アンタゴニストの結晶形態、およびその使用
JP2023538533A (ja) 2020-08-07 2023-09-08 ブリストル－マイヤーズ スクイブ カンパニー 線維症の処置のための、ｃｃｒ２／５拮抗剤と組み合わせたｆｇｆ２１
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