公开(公告)号：WO2017210134A1

公开(公告)日：2017-12-07

申请号：PCT/US2017/034806

申请日：2017-05-26

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： JONES, Philip ,  CZAKO, Barbara ,  CROSS, Jason ,  LEONARD, Paul ,  MSEEH, Faika ,  PARKER, Connon, Austin

IPC: A61K31/4162 ,  A61K31/4985 ,  C07D487/04

Abstract: The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease.

Abstract translation: 本发明涉及可用作PTPN11抑制剂用于治疗或预防癌症和其他PTP介导的疾病的化合物。 本文公开了基于吡唑并吡嗪的新化合物和化合物及其作为用于治疗疾病的药物的应用。

公开(公告)号：WO2018044808A1

公开(公告)日：2018-03-08

申请号：PCT/US2017/048941

申请日：2017-08-28

Applicant: BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM

Inventor： SOTH, Michael, J. ,  JONES, Philip ,  RAY, James ,  LIU, Gang ,  LE, Kang ,  CROSS, Jason

IPC: A61K31/44 ,  A61K31/4178 ,  C07D401/04

Abstract: Disclosed herein are compounds which inhibit the kinase activity of dual leucine zipper (DLK) kinase (MAP3K12), pharmaceutical compositions, and methods of treatment of DLK-mediated diseases, such as neurological diseases that result from traumatic injury to central nervous system and peripheral nervous system neurons (e.g. stroke, traumatic brain injury, spinal cord injury), or that result from a chronic neurodegenerative condition (e.g. Alzheimer's disease, frontotemporal dementia, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, spinocerebellar ataxia, progressive supranuclear palsy, Lewy body disease, Kennedy's disease, and other related conditions), from neuropathies resulting from neurological damage (chemotherapy -induced peripheral neuropathy, diabetic neuropathy, and related conditions) and from cognitive disorders caused by pharmacological intervention (e.g. chemotherapy induced cognitive disorder, also known as chemobrain).

Abstract translation: 本文公开了抑制双亮氨酸拉链（DLK）激酶（MAP3K12）的激酶活性的化合物，药物组合物以及治疗DLK介导的疾病例如由创伤引起的神经疾病的方法 中枢神经系统和外周神经系统神经元损伤（例如中风，创伤性脑损伤，脊髓损伤）或由慢性神经变性疾病（例如阿尔茨海默氏病，额颞叶痴呆，帕金森病，亨廷顿病，肌萎缩侧索硬化，脊髓小脑 共济失调，进行性核上性麻痹，路易体疾病，肯尼迪氏病和其它相关病症），神经病损伤（化学疗法诱导的周围神经病，糖尿病性神经病和相关病症）和由药理学干预（例如化学疗法 诱导认知障碍，也称为化学细胞）。