191231-58-0Relevant articles and documents
Discovery of nonpeptide 3,4-dihydroquinazoline-4-carboxamides as potent and selective sst2 agonists
Betz, Stephen F.,Han, Sangdon,Kim, Sun Hee,Kusnetzow, Ana Karin,Nguyen, Julie,Rico-Bautista, Elizabeth,Scott Struthers, R.,Tan, Hannah,Wang, Shimiao,Zhao, Jian,Zhu, Yunfei
supporting information, (2020/07/21)
Nonpeptide sst2 agonists can provide a new treatment option for patients with acromegaly, carcinoid tumors, and neuroendocrine tumors. Our medicinal chemistry efforts have led to the discovery of novel 3,4-dihydroquinazoline-4-carboxamides as sst2 agonist
SOMATOSTATIN MODULATORS AND USES THEREOF
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Paragraph 00214, (2017/01/23)
Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or diso
Discovery of imidazo[1,2-b]pyridazines as IKKβ inhibitors. Part 2: Improvement of potency in vitro and in vivo
Shimizu, Hiroki,Yasumatsu, Isao,Hamada, Tomoaki,Yoneda, Yoshiyuki,Yamasaki, Tomonori,Tanaka, Shinji,Toki, Tadashi,Yokoyama, Mika,Morishita, Kaoru,Iimura, Shin
, p. 904 - 908 (2011/03/21)
We have increased the potency of imidazo[1,2-b]pyridazine derivatives as IKKβ inhibitors with two strategies. One is to enhance the activity in cell-based assay by adjusting the polarity of molecules to improve permeability. Another is to increase the affinity for IKKβ by the introduction of additional substituents based on the hypothesis derived from an interaction model study. These improved compounds showed inhibitory activity of TNFα production in mice.