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Heteroaryl compounds and their use
专利权人:
АВИЛА ТЕРАПЬЮТИКС; ИНК. (US)
发明人:
СИНГХ Джасвиндер (US),ПЕТТЕР Рассел (US),ТЕСТЕР Ричланд Вэйн (US),КЛЮГ Артур Ф. (US),МАЗДИЯСНИ Хормоз (US),ВЕСТЛИН III Вильям Фредерик (US),НЮ Децян (US),ЦЯО Лисинь (US)
申请号:
RU2012123546/04
公开号:
RU2012123546A
申请日:
2010.12.29
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
1. A compound selected from the group consisting of si or a pharmaceutically acceptable salt thereof. A composition comprising a compound according to claim 1 and a pharmaceutically acceptable excipient, carrier or diluent. 3. The composition of claim 2 in combination with an additional therapeutic agent. The composition of claim 3, wherein the additional therapeutic agent is a chemotherapeutic agent. A method of inhibiting the activity of BTK kinase or its mutant in a patient or in a biological sample, comprising the step of administering to the specified patient or exposing the biological sample to the compound according to Claim 1.6. The method according to claim 5, characterized in that the activity of said BTK or its mutant is inhibited irreversibly. The method according to claim 6, characterized in that the activity of said BTK or its mutant is inhibited irreversibly due to covalent modification of Cys 481 of said BTK. A method for treating a disorder mediated by BTK in a patient in need of said treatment, comprising the step of administering to said patient a compound according to claim 1.9. The method of claim 8, wherein said violation is an autoimmune disease, heteroimmune disease, inflammatory disease, cancer, bone and joint disease, or thromboembolic complication. The method of claim 9, wherein said disorder is selected from rheumatoid arthritis, multiple sclerosis, diabetes, B-cell chronic lymphocytic leukemia, acute lymphocytic leukemia, fleecy leukemia, non-Hodgkin lymphoma, Hodgkin lymphoma, multiple myeloma, colorectal cancer, pancreas, bone cancer, bone metastasis, �1. Соединение, выбранное из группы, состоящей изи,или его фармацевтически приемлемая соль.2. Композиция, включающая соединение по п.1 и фармацевтически приемлемое вспомогательное вещество, носитель или разбавитель.3. Композиция по п.2 в комбинации с дополнительным терапевтическим агентом.4. Композиция по п.3, в которой дополнительным терапевтическим агентом является химиотерапевтическое
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