752222-79-0

Upstream product

• 63981-31-7 6-amino-1-ethyl-3-propylpyrimidine-2,4(1H,3H)-dione 
• 752222-78-9 N'-(3-ethyl-1,2,3,6-tetrahydro-2,6-dioxopyrimidin-4-yl)-N,N-dimethylformamidine 
• 41862-09-3 1-ethyl-6-aminouracil 
• 879328-64-0 6-[1-aza-2-(dimethylamino)vinyl]-1-ethyl-3-propyl-1,3-dihydropyrimidine-2,4-dione 

Downstream Products

• 752222-81-4 5,6-diamino-1-ethyl-3-propylpyrimidine-2,4(1H,3H)-dione 

Relevant academic research and scientific papers

Use of A2B Adenosine Receptor Antagonists for Treating Pulmonary Hypertension

This disclosure relates generally to treating patients having pulmonary hypertension, or symptoms associated therewith, by administering a therapeutically effective amount of an A2B receptor antagonist to the patient.

Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases

Recently, we have reported a series of new 1,3-symmetrically (R1 = R3) substituted xanthines (3 and 4) which have high affinity and selectivity for the human adenosine A2B receptors (hA 2B-AdoR). Unfortunately, this class of compounds had poor pharmacokinetic properties. This prompted us to investigate the effect of differential alkyl substitution at the N-1 and N-3 positions (N1-R ≠ N3-R) on A2B-AdoR affinity and selectivity; we had the dual objectives of enhancing affinity and selectivity for the A 2B-AdoR, as well as improving oral bioavailability. This effort has led to the discovery of compound 62, that displayed high affinity and selectivity for the hA2B-AdoR (Ki = 22 nM). In addition, compound 62 showed high functional potency in inhibiting the accumulation of cyclic adenosine monophosphate induced by 5′-N-ethylcarboxamidoadenosine in HEK-A2B-AdoR and NIH3T3 cells with KB values of 6 and 2 nM, respectively. In a single ascending-dose phase I clinical study, compound 62 had no serious adverse events and was well tolerated.

METHOD OF PREVENTING AND TREATING HEPATIC DISEASE USING A2B ADENOSINE RECEPTOR ANTAGONISTS

The invention is related to methods of preventing and treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method.

Method of wound healing using A2B adenosine receptor antagonists

The present invention relates to methods of wound healing using A2B adenosine receptor antagonists. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

METHOD OF PREVENTING AND TREATING AIRWAY REMODELING AND PULMONARY INFLAMMATION USING A2B ADENOSINE RECEPTOR ANTAGONISTS

The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.

A2B adenosine receptor antagonists

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