RYAN W. CHAU,COURTNEY A. CULLIS,MATTHEW O. DUFFEY,KRISTA E. GIPSON,YONGBO HU,GANG LI,MICHAEL D. SINTCHAK,TRICIA J. VOS
申请号:
ARP120104958
公开号:
AR089447A1
申请日:
2012.12.26
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
The compounds are inhibitors of PI3K and / or vps34 and therefore are useful for treating proliferative disorders, inflammatory and cardiovascular.Claim 1: a compound of formula (1) or one of its pharmaceutically acceptable salts, where both and are g u2075 g u2078 cr u00b3, or one of g u2075 and g u2078 is N and the other is cr u00b3 when one of g u2075 or g u2078 is n, r u00b3 is Hydrogen, halogen, - CN, - Z - r u2075, group or an optionally substituted. Aliphatic and cicloalif u00e1tico c u2081 u208b u2086 held from 3 to 10 members,Where: Z is selected from a Chain alquileno c u2081 u208b u2083 optionally substituted, - O -, N - (r u00b3 u1d43) -, - S, - S - S - (OR), (OR) u2082 -, - C (o) -, CO2 -, - C (o) nr u00b3 u1d43 -, - N (r u00b3 u1d43) C (o) -, - N (CO2 r u00b3 u1d43) - S (o) u2082nr u00b3 u1d43 -, - N (r u00b3 u1d43) - S (o) u2082, OC (o) n (n r u00b3 u1d43) -, - C (o) (r u00b3 u1d43) nr u00b3 u1d43 -, - N (r u00b3 u1d43 s () or () u2082n r u00b3 u1d43) - or - - r u00b3 u1d43 oC (; OR) is a c u2081 u208b u2084 aliphatic Hydrogen or optionally substituted,And r u2075 is Hydrogen or optionally substituted aliphatic Group Selected c u2081 u208b u2086, cicloalif u00e1tico 3 to 10 members, heterociclilo 4 to 10 members with 1 - 5 heteroatoms selected independently of Nitrogen, Oxygen, Sulfur or 6 to 10 members, aryl, or heter Oarilo 5 to 10 members with 1 - 5 independently of heteroatoms selected from Oxygen, nitrogenWhen g u2075 or Sulfur; and g u2078 are both cr u00b3, each occurrence of r u00b3 is independently Hydrogen, CN, or an optionally substituted aliphatic c u2081 u208b u2083; r u00b9 is - CN, - C (o) n (r u2074) u2082, - C (o) - C (or u2074, nr u2074) n ( u2082, r u2074) nhcor u2074 nhso u2082r u2074 -, -, - nhcon (r u2074) u2082 nhcoor u2074 nhso u2082n (-, -, - u2082, r u2074) - ch u2082or u2074, ch u2082n (r u2074) u2082, ch u2082nhc - (OR) - r u2074, so u2082nr u2074 u2082, conhc (= NH) - N - (r u2074) u2082, nhso u2082or u2074 or Cy