RU2013144579A - Ингибиторы киназы mst1 и способы их применения - Google Patents
Ингибиторы киназы mst1 и способы их применения Download PDFInfo
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Abstract
1. Соединение формулы:или его фармацевтически приемлемая соль, где:A представляет собой арил или 4-7-членный гетероцикл;X представляет собой N или CH;каждый Yи Yнезависимо представляет собой S, N или CH, при условии, что по меньшей мере один из Yи Yпредставляет собой N или CH;каждый Rнезависимо представляет собой R, -(R)SOR, -(R)SON(R), -(R)NRSOR, -(R)C(O)N(R)или -(R)NRC(O)R, или необязательно замещенный Cгидрокарбил или 2-12-членный гетерокарбил, при этом необязательное замещение производится одним или более R;каждый Rнезависимо является амино, алкоксилом, карбоксилом, циано, галогеном или гидроксилом;каждый Rнезависимо является Cгидрокарбилом, необязательно замещенным один или более из амино, алкоксила, карбоксила, циано, галогена или гидроксила;каждый Rнезависимо является водородом или необязательно замещенным Cгидрокарбилом или 2-12-членным гетерокарбилом, при этом необязательное замещение производится одним или более из амино, алкоксила, карбоксила, циано, галогена или гидроксила;Rи R, взятые вместе, формируют 5-7-членный гетероцикл, необязательно замещенный одним или более R, или:Rявляется водородом или Cалкилом; иRявляется водородом или необязательно замещенным Cгидрокарбилом или 2-12-членным гетерокарбилом, при этом необязательное замещение производится одним или несколькими R;каждый Rнезависимо является амино, алкоксилом, карбоксилом, циано, галогеном или гидроксилом;k представляет собой 0 или 1;m представляет собой 0-3;n представляет собой 0 или 1; иp представляет собой 0-2;при условии, что Rне является водородом, когда X является CH, Yявляется CH, Yявляется CH и Rявляется водородом.2. Соединение по п.1, где Rне является водородом.3. Соединение по п.1, которое име
Claims (26)
1. Соединение формулы:
или его фармацевтически приемлемая соль, где:
A представляет собой арил или 4-7-членный гетероцикл;
X представляет собой N или CH;
каждый Y1 и Y2 независимо представляет собой S, N или CH, при условии, что по меньшей мере один из Y1 и Y2 представляет собой N или CH;
каждый R1 независимо представляет собой R1A, -(R1B)nSOpR1C, -(R1B)nSOpN(R1C)2, -(R1B)nNR1CSOpR1C, -(R1B)nC(O)N(R1C)2 или -(R1B)nNR1CC(O)R1C, или необязательно замещенный C1-12 гидрокарбил или 2-12-членный гетерокарбил, при этом необязательное замещение производится одним или более R1A;
каждый R1A независимо является амино, алкоксилом, карбоксилом, циано, галогеном или гидроксилом;
каждый R1B независимо является C1-12 гидрокарбилом, необязательно замещенным один или более из амино, алкоксила, карбоксила, циано, галогена или гидроксила;
каждый R1C независимо является водородом или необязательно замещенным C1-12 гидрокарбилом или 2-12-членным гетерокарбилом, при этом необязательное замещение производится одним или более из амино, алкоксила, карбоксила, циано, галогена или гидроксила;
R2 и R3, взятые вместе, формируют 5-7-членный гетероцикл, необязательно замещенный одним или более R3A, или:
R2 является водородом или C1-4 алкилом; и
R3 является водородом или необязательно замещенным C1-12 гидрокарбилом или 2-12-членным гетерокарбилом, при этом необязательное замещение производится одним или несколькими R3A;
каждый R3A независимо является амино, алкоксилом, карбоксилом, циано, галогеном или гидроксилом;
k представляет собой 0 или 1;
m представляет собой 0-3;
n представляет собой 0 или 1; и
p представляет собой 0-2;
при условии, что R3 не является водородом, когда X является CH, Y1 является CH, Y2 является CH и R2 является водородом.
2. Соединение по п.1, где R2 не является водородом.
13. Соединение по любому из пп. 1-12, где X представляет собой N.
14. Соединение по любому из пп. 1-10 и 12, где Y1 представляет собой CH.
15. Соединение по любому из пп. 1-11, где Y2 представляет собой CH.
16. Соединение по любому из пп. 5-12, где Z представляет собой N.
17. Соединение по любому из пп. 5-12, где Z представляет собой CR1.
18. Соединение по любому из пп. 1-12, где R1 представляет собой (R1B)nSOpR1C, -(R1B)nSOpN(R1C)2, -(R1B)nNR1CSOpR1C, -(R1B)nC(O)N(R1C)2 или -(R1B)nNR1CC(O)R1C.
19. Соединение по п.18, где n=0.
20. Соединение по п.18, где p=2.
22. Состав, включающий соединение по любому из пп. 1-21 и фармацевтически приемлемые вспомогательные вещества или растворитель.
23. Применение соединения по любому из пп. 1-21 или состава по п.22 для ингибирования MST1.
24. Применение соединения по любому из пп. 1-21 или состава по п.22 для лечения, контроля или предотвращения воспалительного или аутоиммунного заболевания или нарушения.
25. Применение по п.24, где аутоиммунным заболеванием или нарушением является аутоиммунная ахлоргидрия, болезнь Аддисона, анкилозирующий спондилит, антифосфолипидный синдром, астма (например, бронхиальная астма), атопический дерматит, аутоиммунный атопический гастрит, болезнь Бехчета, глютеновая энтеропатия, болезнь Крона, синдром Кушинга, дерматомиозит, синдром Гудпасчера, реакция трансплантат против хозяина, болезнь Грейвса, тиреоидит Хашимото, гепатит (например, воспалительный и вызванный алкоголем), идиопатическая атрофия надпочечников, идиопатическая тромбоцитопения, синдром Кавасаки, синдром Ламберта-Итона, красная волчанка, рассеянный склероз, тяжелая миастения, пемфигоид, обыкновенная пузырчатка, пернициозная анемия, поллиноз, узелковый полиартериит, первичный биллиарный цирроз печени, первичный склерозирующий холангит, псориаз, псориатический артрит, синдром Рейно, синдром Рейтера, рецидивирующий полихондрит, ревматоидный артрит, синдром Шмидта, склеродермия, синдром Шегрена, симпатическая офтальмия, артериит Такаясу, темпоральный артериит, тиреотоксикоз, отторжение трансплантата (например, органа, клетки или костного мозга), диабет 1-го типа, язвенный колит, увеит и гранулематоз Вегенера.
26. Применение по п.25, где аутоиммунным заболеванием или нарушением является болезнь Крона, реакция трансплантат против хозяина, псориаз, ревматоидный артрит или язвенный колит.
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WO2019006512A1 (en) * | 2017-07-07 | 2019-01-10 | The University Of Queensland | REGENERATION OF CARDIOMYOCYTES |
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TW202202495A (zh) * | 2020-03-26 | 2022-01-16 | 匈牙利商羅特格登公司 | 作為gamma-胺基丁酸A受體次單元alpha 5受體調節劑之㖠啶及吡啶并〔3,4-c〕嗒𠯤衍生物 |
CN113528425B (zh) * | 2020-04-15 | 2023-05-30 | 合肥中科普瑞昇生物医药科技有限公司 | 一种用于乳腺上皮肿瘤细胞的培养基和培养方法 |
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