公开(公告)号：WO2017196261A1

公开(公告)日：2017-11-16

申请号：PCT/SG2017/050248

申请日：2017-05-11

Applicant: NATIONAL UNIVERSITY OF SINGAPORE ,  ACADEMIA SINICA

Inventor： DYMOCK, Brian William ,  YANG, Eugene Guorong ,  YEN, Jong-Young ,  TAN, Eng Chong

IPC: C07D498/12 ,  A61K31/505 ,  A61P35/00 ,  A61P37/06

Abstract: The present disclosure described provides novel dual inhibition compounds that specifically target the JAK-STAT and HDAC pathways, two distinct cellular pathways that are useful in the treatment of various diseases and disorders. In certain aspects, the compounds described herein are useful in the treatment of cellular proliferative and inflammatory diseases or disorders, such as graft vs. host disease. In particular embodiments, the compounds described herein inhibit JAK2 and HDAC6.

Abstract translation: 所描述的本公开提供了特异性靶向JAK-STAT和HDAC途径的新型双重抑制化合物，两种不同的细胞途径可用于治疗各种疾病和病症。 在某些方面，本文所述的化合物可用于治疗细胞增殖性和炎性疾病或病症，例如移植物抗宿主病。 在具体的实施方案中，本文所述的化合物抑制JAK2和HDAC6。

公开(公告)号：WO2016200339A1

公开(公告)日：2016-12-15

申请号：PCT/SG2016/050269

申请日：2016-06-10

Applicant: NATIONAL UNIVERSITY OF SINGAPORE

Inventor： LEE, Sang Hyun ,  DYMOCK, Brian William ,  KITAGAWA, Mayumi ,  SEE, Cheng Shang

IPC: C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D519/00 ,  C07D471/04 ,  C07D495/14 ,  C07D405/14

CPC classification number: C07D401/06 ,  A61K31/4709 ,  A61K31/4725 ,  A61P35/00 ,  A61P39/00 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D495/14 ,  C07D519/00

Abstract: A compound of formula I, wherein the compound of formula I has the structure: wherein R 1 to R 5 , Y, L, Z and X 1 to X 7 have meanings given in the description, said compounds having utility in the treatment of hyperproliferative disease.

Abstract translation: 式I化合物，其中式I化合物具有以下结构：其中R1至R5，Y，L，Z和X1至X7具有说明书中给出的含义，所述化合物可用于治疗过度增殖性疾病。