146830-77-5

Upstream product

• 140396-42-5 5-nitroso-6-amino-3-benzyl-1,3-dihydropyrimidine-2,4-dione 
• 161419-60-9 6-amino-3-benzyl-1-butyl-5-nitrosouracil 
• 138895-24-6 6-amino-3-benzyl-1,3-dihydropyrimidine-2,4-dione 

Downstream Products

• 637334-90-8 N-[4-(1-benzyl-3-furan-3-ylmethyl-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-ylmethyl)-phenyl]-acetamide 
• 1019658-83-3 1-benzyl-8-[1-benzylpyrazol-4-yl]-1,3,7-trihydropurine-2,6-dione 

Relevant academic research and scientific papers

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.

Amide substituted xanthine derivatives

The present invention is a 1,3,8 substituted xanthine derivative of formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

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.

AMIDE SUBSTITUTED XANTHINE DERIVATIVES WITH GLUCONEOGENESIS MODULATING ACTIVITY

The present invention is a 1,3,8 substituted xanthine derivative of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (I) and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.

A2B adenosine receptor antagonists

Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

General synthesis and properties of 1-monosubstituted xanthines

A general convenient synthesis of 1-monosubstituted xanthines (7H-imidazo[4,5-d]pyrimidine-2,6(1H,3H)-diones), starting from 3-substituted 6-aminouracils, is described. After conversion of the 6-aminouracils to the corresponding 5,6-diaminouracils, reaction with formic acid, or with triethyl orthoformate, leads to the novel xanthines in good to excellent yields, while ring closure in alkaline medium, which is commonly used in xanthine synthesis, is not successful.