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Bromodomain inhibitors and Uses Thereof
专利权人:
CONSTELLATION PHARMACEUTICALS; INC.
发明人:
申请号:
ARP110104481
公开号:
AR084070A1
申请日:
2011.12.01
申请国别(地区):
AR
年份:
2013
代理人:
摘要:
Compounds useful as inhibitors of the bromodomain protein content. Are also pharmaceutically acceptable compositions comprising these compounds and the use of such compositions in the treatment of various disorders.Claim 1: a compound of the formula (1) or a pharmaceutically acceptable Salt thereof, wherein: X is o or N; and o or N; where at least one of the X or y is o; r1 is H, alkyl, alquenilo, alquinilo, aralquilo, aryl, heteroaryl, Halo CN, prays, nrarb (RA), N (n or S) qrarb (RA, RB, C (o)) N (RA) C (o) nrarb, N (RA) C (o) or N (RA), C (S) nrarb, QRA, S (o) C (o) C (o) or ra, or ra, OC (o) C (o) nrarb; each ra is,Independently alquenilo optionally substituted alkyl, optionally substituted or alquinilo optionally replaced, each containing 0, 1, 2 or 3 heteroatoms selected from o, s or n aryl optionally substituted heteroaryl; Mind; optionally substituted Heterocyclic; u00edclico optionally substituted; carboc u00edclico Hydrogen or optionally substituted; each RB isIndependently alquenilo optionally substituted alkyl, optionally substituted or alquinilo optionally replaced, each containing 0, 1, 2 or 3 heteroatoms selected from o, s or N; optionally substituted aryl, heteroaryl heteroc u00ed optionally substituted; CLICO optionally substituted; carboc u00edclico Hydrogen or optionally substituted or ra and RB.Along with the Atoms to which each of them is United, Can form a heterocicloalquilo or a heteroaryl; each of which is optionally substituted; ring a is aryl or heteroaryl, cycloalkyl, heterocicloalquilo; RC is alkyl, cycloalkyl, alquenilo, alquinilo, Ari So, heterocicloalquilo or heteroaryl,Each of which is optionally substituted with 1 - 5 R4 selected independently and, when L1 is not a Covalent Bond, RC is selected in each h, R2 and R3 are independently h, halogen, alkyl, optionally substituted, optionally replacing alquenilo Gone, alquinilo optionally substituted, optionally substituted aryl,Aralquilo optionally substituted cycloalkyl, optionally subst
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