1116136-36-7Relevant academic research and scientific papers
EIF4E-INHIBITING 4-OXO-3,4-DIHYDROPYRIDO[3,4-D]PYRIMIDINE COMPOUNDS
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Paragraph 0311-0312; 0378, (2021/01/23)
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X1, X2, X3, X4, X5, X6, Q, L1, L2, Y, R1, R2, R3, R4, R5, R6, R7, R8 and rings A, B and C are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4e and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
BIARYL KINASE INHIBITORS
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Page/Page column 195, (2017/07/31)
The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAKl (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.
4-Azaindole Derivatives
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Paragraph 0361-0363, (2015/04/15)
4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
4-AZAINDOLE DERIVATIVES
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Page/Page column 39; 40, (2015/04/22)
4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
Lead optimization of 1,4-azaindoles as antimycobacterial agents
Shirude, Pravin S.,Shandil, Radha K.,Manjunatha,Sadler, Claire,Panda, Manoranjan,Panduga, Vijender,Reddy, Jitendar,Saralaya, Ramanatha,Nanduri, Robert,Ambady, Anisha,Ravishankar, Sudha,Sambandamurthy, Vasan K.,Humnabadkar, Vaishali,Jena, Lalit K.,Suresh, Rudrapatna S.,Srivastava, Abhishek,Prabhakar,Whiteaker, James,McLaughlin, Robert E.,Sharma, Sreevalli,Cooper, Christopher B.,Mdluli, Khisi,Butler, Scott,Iyer, Pravin S.,Narayanan, Shridhar,Chatterji, Monalisa
supporting information, p. 5728 - 5737 (2014/08/05)
In a previous report, we described the discovery of 1,4-azaindoles, a chemical series with excellent in vitro and in vivo antimycobacterial potency through noncovalent inhibition of decaprenylphosphoryl-β-d-ribose-2′- epimerase (DprE1). Nevertheless, high mouse metabolic turnover and phosphodiesterase 6 (PDE6) off-target activity limited its advancement. Herein, we report lead optimization of this series, culminating in potent, metabolically stable compounds that have a robust pharmacokinetic profile without any PDE6 liability. Furthermore, we demonstrate efficacy for 1,4-azaindoles in a rat chronic TB infection model. We believe that compounds from the 1,4-azaindole series are suitable for in vivo combination and safety studies.
3' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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Page/Page column 140-141, (2009/04/25)
The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein Q, R1, R4, m and Ar are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
