442685-53-2Relevant academic research and scientific papers
THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION
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Paragraph 0460-0461, (2019/02/13)
Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
Antagonists of the human A2A adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines
Gillespie, Roger J.,Bamford, Samantha J.,Botting, Ruth,Comer, Mike,Denny, Sarah,Gaur, Suneel,Griffin, Michael,Jordan, Allan M.,Knight, Anthony R.,Lerpiniere, Joanne,Leonardi, Stefania,Lightowler, Sean,McAteer, Steven,Merrett, Angela,Misra, Anil,Padfield, Antony,Reece, Mark,Saadi, Mona,Selwood, Daniel L.,Stratton, Gemma C.,Surry, Dominic,Todd, Richard,Tong, Xin,Ruston, Vicki,Upton, Rebecca,Weiss, Scott M.
experimental part, p. 33 - 47 (2011/04/19)
Antagonism of the human A2A receptor has been implicated as a point of therapeutic intervention in the alleviation of the symptoms associated with Parkinson's disease. This is thought to occur, at least in part, by increasing the sensitivity of the dopaminergic neurons to the residual, depleted levels of striatal dopamine. We herein describe a novel series of functionalized triazolo[4,5-d]pyrimidine derivatives that display functional antagonism of the A2A receptor. Optimization of these compounds has resulted in improvements in potency, selectivity, and the pharmacokinetic properties of key derivatives. These efforts have led to the discovery of 60 (V2006/BIIB014), which demonstrates strong oral activity in commonly used models of Parkinson's disease. Furthermore, this derivative has shown excellent preclinical pharmacokinetics and has successfully completed phase I clinical studies. This compound is presently undergoing further clinical evaluation in collaboration with Biogen Idec.
SUBSTITUTED PYRIDINONES
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, (2008/06/13)
Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
Purine derivatives as purinergic receptor antagonists
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, (2008/06/13)
Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO
