1190312-40-3Relevant academic research and scientific papers
4-Azaindole Derivatives
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, (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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, (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
, 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.
[4[4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-(1H-PYRROLO-PYRIDIN-YL)-METHANONES AND SYNTHESIS THEREOF
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Page/Page column 51, (2011/07/09)
The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase including but not limited to for example asthma and other inflammatory diseases including age-related macular degeneration.
SPIROPIPERIDINE BENZYLAMINES AS BETA-TRYPTASE INHIBITORS
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Page/Page column 33; 34, (2011/07/09)
The present invention discloses and claims a series of substituted spiropiperidine benzylamines of formula (I) wherein R is as described herein. More specifically, the compounds of this invention are inhibitors of β-tryptase and are, therefore, useful as
