365572-09-4Relevant articles and documents
Discovery of tertiary amine and indole derivatives as potent RORγt inverse agonists
Yang, Ting,Liu, Qian,Cheng, Yaobang,Cai, Wei,Ma, Yingli,Yang, Liuqing,Wu, Qianqian,Orband-Miller, Lisa A.,Zhou, Ling,Xiang, Zhijun,Huxdorf, Melanie,Zhang, Wei,Zhang, Jing,Xiang, Jia-Ning,Leung, Stewart,Qiu, Yang,Zhong, Zhong,Elliott, John D.,Lin, Xichen,Wang, Yonghui
supporting information, p. 65 - 68 (2014/02/14)
A novel series of tertiary amines as retinoid-related orphan receptor gamma-t (RORγt) inverse agonists was discovered through agonist/inverse agonist conversion. The level of RORγt inhibition can be enhanced by modulating the conformational disruption of H12 in RORγt LBD. Linker exploration and rational design led to the discovery of more potent indole-based RORγt inverse agonists.
Novel derivatives and analogues of galanthamin
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, (2008/06/13)
New compounds of general formula I 1
12H-[2]-benzothiepino[6,5a,5-bc]benzofuran: Synthesis of a sulfur-analog of galanthamine
Treu, Matthias,Jordis, Ulrich,Mereiter, Kurt
, p. 1727 - 1735 (2007/10/03)
An analog of the anti-Alzheimer drug galanthamine, carrying a SO2-moiety instead of an amino-functionality, has been synthesized as a racemic mixture using tandem cyclization techniques to form a new four membered heterocyclic ring system.
9-(Arylalkyl or aroylalkyl)-1-oxa-4,9-diazaspiro(5.5)undecan-3-ones
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, (2008/06/13)
Compounds useful in the prevention and/or treatment of hypertension, congestive heart failure, arrhythmia, migraine, vasospastic disorders, and asthma are represented by the formula STR1 wherein: R1 is STR2 wherein X is hydrogen, lower alkyl, lower alkoxy, halo, carboxamido or hydroxy; m is 1, 2 or 3; and n is 1, 2 or 3; R2, R3 and R4 are independently hydrogen or lower alkyl; and the pharmaceutically acceptable acid addition salts thereof.