05-11-2015 дата публикации
Номер: US20150315182A1
Автор:
Baiazitov Ramil,
Cao Liangxian,
Davis Thomas W,
DU Wu,
Lee Chang-Sun,
Liu Ronggang,
Moon Young-Choon,
Paget Steven D.,
Ren Hongyu,
Sydorenko Nadiya,
Wilde Richard Gerald
Принадлежит:
Amine substituted reverse pyrimidine compounds and forms thereof that inhibit the function and reduce the level of B-cell specific Moloney murine leukemia virus integration site 1 (Bmi-1) protein and methods for their use to inhibit Bmi-1 function and reduce the level of Bmi-1 to treat a cancer mediated by Bmi-1 are described herein. 2. The compound of claim 1 , wherein Ris optionally substituted heteroaryl or heterocyclyl selected from 1H-pyrazolyl claim 1 , 1H-imidazolyl claim 1 , 1 claim 1 ,2-oxazolyl claim 1 , pyridinyl claim 1 , 1H-indolyl claim 1 , 2H-indazolyl claim 1 , 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-2H-indazolyl claim 1 , 1H-benzimidazolyl claim 1 , imidazo[2 claim 1 ,1-b][1 claim 1 ,3]thiazolyl claim 1 , pyrazolo[1 claim 1 ,5-a]pyridinyl claim 1 , pyrazolo[1 claim 1 ,5-c]pyrimidinyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , 5 claim 1 ,6 claim 1 ,7 claim 1 ,8-tetrahydroimidazo[1 claim 1 ,2-a]pyridinyl claim 1 , 1H-imidazo[4 claim 1 ,5-b]pyridinyl claim 1 , 1H-imidazo[4 claim 1 ,5-c]pyridinyl claim 1 , 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-3H-imidazo[4 claim 1 ,5-c]pyridinyl claim 1 , imidazo[1 claim 1 ,2-a]pyrazinyl claim 1 , imidazo[1 claim 1 ,2-a]pyrimidinyl claim 1 , 7H-purinyl or quinolinyl.3. The compound of claim 2 , wherein Ris optionally substituted heteroaryl selected from 1H-pyrazolyl claim 2 , 1H-indolyl claim 2 , 1H-benzimidazolyl claim 2 , pyrazolo[1 claim 2 ,5-a]pyridinyl claim 2 , imidazo[1 claim 2 ,2-a]pyridinyl claim 2 , 1H-imidazo[4 claim 2 ,5-b]pyridinyl claim 2 , imidazo[1 claim 2 ,2-a]pyrazinyl or imidazo[1 claim 2 ,2-a]pyrimidinyl.4. A compound or a form thereof selected from the group consisting of:N-(4-methoxyphenyl)-2-(2-methyl-1H-benzimidazol-1-yl)pyrimidin-4-amineN-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-(2-methylimidazo[1,2-a]pyridin-3-yl)pyrimidin-4-amine2-(2-methylimidazo[1,2-a]pyridin-3-yl)-N-[4-(trifluoromethyl)phenyl]pyrimidin-4-amineN-(4-methoxyphenyl)-2-(2-methylimidazo[1,2-a]pyridin-3-yl) ...
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