726174-45-4Relevant academic research and scientific papers
COMPOUNDS FOR THE TREATMENT OF NEUROMUSCULAR DISORDERS
-
Paragraph 0157-0158, (2020/12/29)
The present disclosure relates to compounds suitable for treating, ameliorating and/or preventing neuromuscular disorders, including the reversal of drug-induced neuromuscular blockade. The compounds as defined herein can inhibit the CIC-1 ion channel.
NOVEL SMALL MOLECULE INHIBITORS OF TEAD TRANSCRIPTION FACTORS
-
Page/Page column 124; 126, (2020/10/09)
The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.
SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
-
Page/Page column 95, (2015/01/07)
The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
The discovery of indole full agonists of the neurotensin receptor 1 (NTSR1)
Di Fruscia, Paolo,He, Yuanjun,Koenig, Marcel,Tabrizifard, Sahba,Nieto, Ainhoa,McDonald, Patricia H.,Kamenecka, Theodore M.
supporting information, p. 3974 - 3978 (2014/10/15)
Neurotensin (NT) is an endogenous tridecapeptide found in the central nervous system (CNS) and in peripheral tissues. Neurotensin exerts a wide range of physiological effects and it has been found to play a critical role in a number of human diseases, suc
LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
-
Paragraph 0665, (2013/03/26)
Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.
Virtual screening and structure-based discovery of indole acylguanidines as potent β-secretase (BACE1) inhibitors
Zou, Yiquan,Li, Li,Chen, Wuyan,Chen, Tiantian,Ma, Lanping,Wang, Xin,Xiong, Bing,Xu, Yechun,Shen, Jingkang
, p. 5706 - 5722 (2013/06/27)
Proteolytic cleavage of amyloid precursor protein by β-secretase (BACE1) is a key step in generating the N-terminal of β-amyloid (Aβ), which further forms into amyloid plaques that are considered as the hallmark of Alzheimer's disease. Inhibitors of BACE1 can reduce the levels of Aβ and thus have a therapeutic potential for treating the disease. We report here the identification of a series of small molecules bearing an indole acylguanidine core structure as potent BACE1 inhibitors. The initial weak fragment was discovered by virtual screening, and followed with a hit-to-lead optimization. With the aid of co-crystal structures of two discovered inhibitors (compounds 19 and 25) with BACE1, we explored the SAR around the indole and aryl groups, and obtained several BACE1 inhibitors about 1,000-fold more potent than the initial fragment hit. Accompanying the lead optimization, a previously under-explored sub-site opposite the flap loop was redefined as a potential binding site for later BACE1 inhibitor design.
Synthesis and evaluation of indole aspartyl ketones as novel caspase-3 inhibitors
Sengupta,Rao, G.Venkateshwar,Dubey
scheme or table, p. 5517 - 5520 (2012/07/27)
Synthesis, biological evaluation and structure-activity relationships for a series of novel nonpeptide small molecule inhibitors of caspase-3 are described. Among the synthesized compounds, 2,3,5,6-tetrafluorophenoxymethyl ketone derivatives of indole-N-a
1-(Bicyclopiperazinyl)ethylindoles and 1-(homopiperazinyl)ethyl-indoles as highly selective and potent 5-HT7 receptor ligands
Isaac, Methvin B,Xin, Tao,O'Brien, Anne,St-Martin, David,Naismith, Angela,MacLean, Neil,Wilson, Julie,Demchyshyn, Lidia,Tehim, Ashok,Slassi, Abdelmalik
, p. 2451 - 2454 (2007/10/03)
A novel series of 1-(bicyclopiperazinyl)ethylindole and 1-(homopiperazinyl)ethyl-indole derivatives was synthesized and found to be potent and selective 5-HT7 receptor ligands.
