- Approach to the library of fused pyridine-4-carboxylic acids by combes-type reaction of acyl pyruvates and electron-rich amino heterocycles
-
A library of fused pyridine-4-carboxylic acids (including pyrazolo[3,4-b]pyridines, isoxazolo[5,4-b]pyridines, furo[2,3-b]pyridines, thieno[2,3-b]pyridines, and pyrido[2,3-d]pyrimidines) was generated by Combes-type reaction of acyl pyruvates and electron-rich amino heterocycles followed by hydrolysis of the ester. The library members were also demonstrated to undergo the standard combinatorial transformations including amide coupling and esterification, as well as less common heterocyclizations to 1,2,4-triazoles and 1,2,4-oxadiazoles.
- Volochnyuk, Dmitriy M.,Ryabukhin, Sergey V.,Plaskon, Andrey S.,Dmytriv, Yuri V.,Grygorenko, Oleksandr O.,Mykhailiuk, Pavel K.,Krotko, Dmitriy G.,Pushechnikov, Alexei,Tolmachev, Andrey A.
-
scheme or table
p. 510 - 517
(2010/09/05)
-
- Selective, high affinity A2B adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines
-
A series of N-1 monosubstituted 8-pyrazolyl xanthines have been synthesized and evaluated for their affinity for the adenosine receptors (AdoRs). We have discovered two compounds 18 (CVT-7124) and 28 (CVT-6694) that display good affinity for the A2B AdoR (Ki = 6 nM and 7 nM, respectively) and greater selectivity for the human A1, A2A, and A3 AdoRs (>1000-, >830-, and >1500-fold; >850-, >700-, and >1280-fold, respectively). CVT-6694 has been shown to block the release of interleukin-6 and monocyte chemotactic protein-1 from bronchial smooth muscle cells (BSMC), a process believed to be promoted by activation of A2B AdoR.
- Kalla, Rao V.,Elzein, Elfatih,Perry, Thao,Li, Xiaofen,Gimbel, Art,Yang, Ming,Zeng, Dewan,Zablocki, Jeff
-
p. 1397 - 1401
(2008/09/21)
-
- XANTHINE DERIVATIVES AS A2B ADENOSINE RECEPTOR ANTAGONISTS
-
Disclosed are compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
- -
-
-
- A2B adenosine receptor antagonists
-
Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
- -
-
-
- 1,3-Dialkyl-8-(p-sulfophenyl)xanthines: Potent Water-Soluble Antagonistst for A1- and A2-Adenosine Receptors
-
A series of 8-(substituted phenyl) derivatives of Theophylline and other 1,3-dialkylxanthines were evaluated for potency and selectivity as antagonists at A1- and A2-adenosine receptors in brain tissue.Theophylline has a similar pote
- Daly, J.W.,Padgett, W.,Shamim, M.T.,Butts-Lamb, P.,Waters, J.
-
p. 487 - 492
(2007/10/02)
-
- Method and pharmaceutical preparation for treating chronic obstructive airway disease and cardiac disease, and intermediates for the preparation of therapeutically active xanthine derivatives
-
A method for the treatment of chronic obstructive airway disease or cardiac disease, characterized by the administration of a compound of the formula STR1 wherein R is n-propyl, n-butyl or isobutyl or a therapeutically acceptable salt thereof.
- -
-
-