115204-74-5Relevant academic research and scientific papers
HYPOXANTHINE COMPOUND
-
Paragraph 0066, (2021/05/13)
The present invention aims to provide a novel compound which has prolyl hydroxylases (PHDs) inhibitory effect and which is useful for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. The present invention relates to hypoxanthine compound or a pharmaceutically acceptable salt thereof. The compounds of the present invention or pharmaceutically acceptable salts thereof have prolyl hydroxylase inhibitory effect and are useful as agents for the treatment of inflammatory bowel diseases such as ulcerative colitis and the like. In an embodiment, the present invention relates to a method for treating an inflammatory bowel disease, comprising administering a necessary amount of a pharmaceutical composition containing hypoxanthine compound or a pharmaceutically acceptable salt thereof, and pharmaceutical additive to a patient.
EGFR INHIBITORS, COMPOSITIONS AND METHODS THEREOF
-
Page/Page column 42; 43, (2020/07/31)
Provided are compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or inf
COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF DISEASE
-
Page/Page column 74; 83-84, (2020/09/19)
Disclosed are compounds and compositions for inhibiting the expression of a pattern recognition receptor (e.g., STING), and methods of use thereof.
Double-ring heterocyclic amines Hedgehog signal pathway inhibitor
-
Paragraph 0148-0151, (2018/06/14)
The invention relates to the field of biological medicine, and concretely relates to bicyclic heterocyclic amine compounds, and the compounds are a new Hedgehog inhibitor and pharmaceutically acceptable salts shown as a general formula (I). The compounds can be used as a Hedgehog signal conduction inhibitor applied to multiple medical applications.
Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1
Malínková, Veronika,?ezní?ková, Eva,Jorda, Radek,Gucky, Tomá?,Kry?tof, Vladimír
, p. 6523 - 6535 (2017/11/03)
Inhibition of protein kinases is a validated concept for pharmacological intervention in cancers. Many kinase inhibitors have been approved for clinical use, but their practical application is often limited. Here, we describe a collection of 23 novel 2,6,9-trisubstituted purine derivatives with nanomolar inhibitory activities against PDGFRα, a receptor tyrosine kinase often found constitutively activated in various tumours. The compounds demonstrated strong and selective cytotoxicity in the human eosinophilic leukemia cell line EOL-1, whereas several other cell lines were substantially less sensitive. The cytotoxicity in EOL-1, which is known to express the FIP1L1‐PDGFRA fusion gene encoding an oncogenic kinase, correlated significantly with PDGFRα inhibition. EOL-1 cells treated with the compounds also exhibited dose-dependent inhibition of PDGFRα autophosphorylation and suppression of its downstream signaling pathways with concomitant G1 phase arrest, confirming the proposed mechanism of action. Our results show that substituted purines can be used as platforms for preparing tyrosine kinase inhibitors with specific activity towards eosinophilic leukemia.
Discovery of 9H-purins as potential tubulin polymerization inhibitors: Synthesis, biological evaluation and structure?activity relationships
Zhou, Zhong-Zhen,Shi, Xiu-Dong,Feng, Hong-Fang,Cheng, Yu-Fang,Wang, Hai-Tao,Xu, Jiang-Ping
, p. 1126 - 1134 (2017/08/02)
Two series of N-(4-methoxyphenyl)-N-methyl-9H-purin-6-amines (9a-d and 10a-h) and 9-substituted benzyl-6-chloro-9H-purines (11a-h) were designed and synthesized. Their antiproliferative activities against human myelogenous leukemia (K562), human neuroblas
HETEROCYCLIC HYDROXAMIC ACIDS AS PROTEIN DEACETYLASE INHIBITORS AND DUAL PROTEIN DEACETYLASE-PROTEIN KINASE INHIBITORS AND METHODS OF USE THEREOF
-
Paragraph 00371; 00372, (2016/04/26)
The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mpsl kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mpsl k
Five-membered heteroaromatic ring fused-pyrimidine derivatives: Design, synthesis, and hedgehog signaling pathway inhibition study
Zhang, Liandi,Xin, Minhang,Shen, Han,Wen, Jun,Tang, Feng,Tu, Chongxing,Zhao, Xinge,Wei, Ping
supporting information, p. 3486 - 3492 (2014/07/22)
A series of novel five-membered heteroaromatic ring fused-pyrimidine derivatives including purines, pyrrolo[2,3-d]pyrimidines, pyrrolo[3,2-d] pyrimidines, thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and furo[3,2-d]pyrimidines have been identified to be potent inhibitors of hedgehog signaling pathway. The synthesis and SAR of these compounds are described. Among this new series of hedgehog signaling pathway inhibitors, most compounds exhibited significant inhibitory activity compared to vismodegib, indicating that the five-membered heteroaromatic ring fused-pyrimidines stand out as encouraging scaffolds among the currently reported structural skeletons for hedgehog signaling pathway inhibitors, deserving more exploration and further investigation.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
-
Paragraph 00922, (2013/03/26)
Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
TRICYCLIC HETEROCYCLES USEFUL AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS
-
Page/Page column 35, (2013/03/26)
The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
