Derivatives heteroarilicos PI3K Kinase Inhibitors, Pharmaceutical compositions containing them and Use thereof for treating proliferative disorders, inflammatory and / or cardiovascular
SHI ZHAN,HIROSE MASAAKI,LEE HONG MYUNG,SELLS TODD B.,HU YONGBO,VYSKOCIL STEPAN,HU ZHIGEN,XU TIANLIN,FREEZE BRIAN S.
申请号：
ARP110102929
公开号：
AR082665A1
申请日:
2011.08.11
申请国别(地区):
AR
年份:
2012
代理人:
摘要：
Claim 1: a compound of formula (1) or (2), or Salt acceptable for pharmaceutical use of the same, where: s or Z, R1 is Cy, - C (o) n (R3) 2 OR3, - C (o) - C (o) o (NH) - C (= NH) nhoh, - C (o) nr3n (R3) 2 - (c = N - NH2) NH2, - C (= n) n (R3) 2, where C is a remainder formula (3), where: G2 = - n = N -, - (OR N R3).Where each occurrence of R3 and R3 are independently Hydrogen or optionally substituted aliphatic C1 - 6, where X1, X2, and X3 are each independently n, o, S, or nr3, CR4, always only one of X1, X2, and X3 can be o, S, or NR1； each occurrence of R4 is independently Hydrogen, halogen, - CN, - Z3 - R6, or an optionally substituted aliphatic Group selected from C1 - 6Or cicloalif u00e1tico 3 to 10 members: Z3 is selected, where a Chain of alquileno c1-3 optionally substituted, - O -, N - (R4A) -, - S, - S - S - (OR), (OR) 2, - C (o) -, CO2 - nr4a - C (o) n (R4A) -, - C (o) -, - N (CO2, R4A) - S (o) 2nr4a -, - N (s R4A) (OR) 2, CO (o) n (n R4A) -, - C (R4A) (o) nr4a -, - N (R4A) s (OR) 2N (R4A) - or - (or oC - R4A)； is a c1-4 aliphatic Hydrogen or optionally substituted,And R6 is Hydrogen or a group of selected optionally substituted aliphatic C1 - 6, cicloalif u00e1tico 3 to 10 members, heterociclilo 4 to 10 members with 1 to 5 heteroatoms selected irrespective of Nitrogen, Oxygen, Sulfur or 6 to 10 members, aryl or heteroaryl 5 10 members who have 1 to 5 independently heteroatoms selected from Oxygen, nitrogenOr Sulfur； or where two adjacent appearances of R3 or R4, taken together with the Atom to which they are FUSED together to form a group of selected optionally substituted aryl or heteroaryl 5 to 6 members, 5 to 6 members that have 1 to 5 regardless of heteroatoms selected Nitrogen, Oxygen or Sulfur； The Ring is a selected Group of cicloalif u00e1tico 3 to 10 members.Heterociclilo 4 to 10 members with 1 to 5 heteroatoms selected irrespective of Nitrogen, Oxygen, Sulfur or 6 to 10 members, aryl or heteroaryl, 5 to 10 members with 1 to 5 heteroatoms selec
