660416-41-1Relevant academic research and scientific papers
The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma
Zablocki, Jeff,Kalla, Rao,Perry, Thao,Palle, Venkata,Varkhedkar, Vaibhav,Xiao, Dengming,Piscopio, Anthony,Maa, Tenning,Gimbel, Art,Hao, Jia,Chu, Nancy,Leung, Kwan,Zeng, Dewan
, p. 609 - 612 (2007/10/03)
Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A2B AdoR antagonist with good selectivity (A2B AdoR Ki = 50 nM, selectivity A1 > 200: A2A > 200: A3 > 167).
NEW COMPOUNDS
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Page/Page column 45, (2010/11/30)
The present invention relates to new compounds of formula (I), wherein P, Q, X1, X2, X3, X4, R, R1, R2, R3, R4, R5, R6, R7, m, n, o, p and q are defined as in any one of claims 1 to 12, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
NEW COMPOUNDS
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Page 104-105, (2010/02/06)
The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
CVT-4325: A potent fatty acid oxidation inhibitor with favorable oral bioavailability
Elzein, Elfatih,Ibrahim, Prabha,Koltun, Dmitry O.,Rehder, Ken,Shenk, Kevin D.,Marquart, Timothy A.,Jiang, Bob,Li, Xiaofen,Natero, Reina,Li, Yuan,Nguyen, Marie,Kerwar, Suresh,Chu, Nancy,Soohoo, Daniel,Hao, Jia,Maydanik, Victoria Y.,Lustig, David A.,Zeng, Dewan,Leung, Kwan,Zablocki, Jeff A.
, p. 6017 - 6021 (2007/10/03)
New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325, a potent FOXi (IC50 = 380 nM, rat mitochondria) with favorable PK properties (F = 93%, t1/2 = 13.6 h, dog). New inhibitors of palmitoyl-CoA oxidation are based on the introduction of nitrogen heterocycles in the 'Western Portion' of the molecule. SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50 = 380 nM rat mitochondria) with favorable PK properties (F = 93%, t1/2 = 13.6 h, dog).
