51509-98-9Relevant academic research and scientific papers
Pseudosaccharin amines as potent and selective KV1.5 blockers
Lloyd, John,Finlay, Heather J.,Kover, Alexander,Johnson, James,Pi, Zulan,Jiang, Ji,Neels, James,Cavallaro, Cullen,Wexler, Ruth,Conder, Mary Lee,Shi, Hong,Li, Danshi,Sun, Huabin,Chimalakonda, Anjaneya,Huang, Christine,Salvati, Mark,Levesque, Paul
, p. 4983 - 4986 (2015/03/30)
Phenethyl aminoheterocycles like compound 1 were known to be potent IKur blockers although they lacked potency in vivo. Modification of the heterocycle led to the design and synthesis of pseudosaccharin amines. Compounds such as 14, 17d and 21c were found to be potent KV1.5 blockers and selective over other cardiac ion channels. These compounds had potent pharmacodynamic activity, however, they also showed off-target activities such as hemodynamic effects.
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression
Wu, Yong-Jin,He, Huan,Bertekap, Robert,Westphal, Ryan,Lelas, Snjezana,Newton, Amy,Wallace, Tanya,Taber, Matthew,Davis, Carl,MacOr, John E.,Bronson, Joanne
, p. 2217 - 2228 (2013/05/08)
This report describes the synthesis, structure-activity relationships and activity of piperidine, homopiperidine, and azocane derivatives combining NK1 receptor (NK1R) antagonism and serotonin reuptake transporter (SERT) inhibition. Our studies culminated in the discovery of piperidine 2 and homopiperidine 8 as potent dual NK1R antagonists-SERT inhibitors. Compound 2 demonstrated significant activity in the gerbil forced swimming test, suggesting that dual NK1R antagonists-SERT inhibitors may be useful in treating depression disorders.
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11β-HSD1 inhibitors
Sun, Daqing,Wang, Zhulun,Caille, Seb,Degraffenreid, Michael,Gonzalez-Lopez De Turiso, Felix,Hungate, Randall,Jaen, Juan C.,Jiang, Ben,Julian, Lisa D.,Kelly, Ron,McMinn, Dustin L.,Kaizerman, Jacob,Rew, Yosup,Sudom, Athena,Tu, Hua,Ursu, Stefania,Walker, Nigel,Willcockson, Maren,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 405 - 410 (2011/02/27)
The synthesis and SAR of a series of 4,4-disubstituted cyclohexylbenzamide inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, highly selective, and orally bioavailable inhibitors demonstrating efficacy in both rat and non-human primate ex vivo pharmacodynamic models.
SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES
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Page/Page column 51; 52, (2009/10/06)
The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
Spirocyclic Azaindole Derivatives
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Page/Page column 9, (2009/07/03)
The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.
Benzamide derivatives and uses related thereto
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Page/Page column 44, (2008/06/13)
Benzamide derivatives of formula I are described and have therapeutic utility, particularly in the treatment of diabetes, obesity and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, and n are as defined herein.
Fused heterocyclic compounds
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Page/Page column 18, (2010/02/14)
A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.
Carbocyclic potassium channel inhibitors
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, (2008/06/13)
The present invention relates to a class of carbocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists I.
Elliott, Jason M,Castro, Jose L,Chicchi, Gary G,Cooper, Laura C,Dinnell, Kevin,Hollingworth, Gregory J,Ridgill, Mark P,Rycroft, Wayne,Kurtz, Marc M,Shaw, Duncan E,Swain, Christopher J,Tsao, Kwei-Lan,Yang, Lihu
, p. 1755 - 1758 (2007/10/03)
A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action.
Benzamide potassium channel inhibitors
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, (2008/06/13)
This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related affl
