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Tienotrizolodiazepinas acetamide and Uses Thereof
专利权人:
DANA-FARBER CANCER INSTITUTE; INC.
发明人:
BRADNER, James E.,QI, Jun,TANAKA, Minoru
申请号:
PE0003772018
公开号:
PE10862018A1
申请日:
2016.09.09
申请国别(地区):
PE
年份:
2018
代理人:
摘要:
The present Invention relates to trienotriazolodiazepinas Derivatives of formula (i) or a pharmaceutically acceptable Salt, or tautomero stereoisomer of the sameWhere: and it is as follows ra1 is H, halogen, alkyl, optionally substituted, among others carbociclilo RA2 is optionally substituted Halogen, RC is Halogen, among othersAlquenilo optionally replaced, among others RB is H, halogen, alkyl, optionally substituted, among others R2 is H, halogen, alkyl, optionally substituted,Among others, X1 is n or CR5 c is 0, 1, 2, 3 or 4 n is 0, 1, 2, 3 or 4 and the Ring C is aryl or heteroaryl.The compounds of formula (i) are bromodominios binding molecules and \/ or containing Proteins (e.g., bromodominios bromodomain proteins and extra terminal (BET).Also provided are methods and Kits, uses using the compounds and Pharmaceutical compositions for inhibiting activity (e.g.The increased activity of the bromodominios) and \/ or the bromodomain containing protein and to treat and \/ or prevent Diseases associated with a subject or bromodominios Protein contBromodomain have (e.g., proliferative diseases, cardiovascular diseases, Viral Infections, fibrotic diseases, Metabolic Diseases,Endocrine diseases and radiation poisoning). Compounds, Pharmaceutical compositions and kits are also useful for male ContraceptionLa presente invencion se refiere a derivados de trienotriazolodiazepinas de formula (I) o una sal, estereoisomero o tautomero farmaceuticamente aceptable de los mismos, en donde: Y es como se indica a continuacion RA1 es H, halogeno, alquilo opcionalmente sustituido, entre otros RA2 es carbociclilo opcionalmente sustituido, halogeno, entre otros Rc es halogeno, alquenilo opcionalmente sustituido, entre otros RB es H, halogeno, alquilo opcionalmente sustituido, entre otros R2 es H, halogeno, alquilo opcionalmente sustituido, entre otros X1 es N o CR5 c es 0, 1, 2, 3 o 4 n es 0, 1, 2, 3 o 4 y el anillo C es arilo o heteroarilo. Los compuestos de Formula (I) son moleculas
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