76872-75-8

Upstream product

• 4815-36-5 ethyl 2-amino-4-phenyl-thiophene-3-carboxylate 
• 151-50-8 potassium cyanide 
• 67171-55-5 2-amino-4-phenylthiophene-3-carboxylic acid methyl ester 
• 57-13-6 urea 
• 17277-47-3 (Z)-2-cyano-3-phenylbut-2-enoic acid ethyl ester 
• 98-86-2 acetophenone 

Downstream Products

• 76872-27-0 2,4-dichloro-5-phenyl-thieno[2,3-d]pyrimidine 
• 108311-88-2 (2,4-Dioxo-5-phenyl-1,4-dihydro-2H-thieno[2,3-d]pyrimidin-3-yl)-acetic acid ethyl ester 
• 64572-05-0 3-methyl-5-phenyl-1H-thieno[2,3-d]pyrimidine-2,4-dione 
• 76872-51-0 2-Chloro-5-phenyl-3,4-dihydro-thieno[2,3-d]pyrimidine 
• 1401985-61-2 (S)-1-{5-phenyl-4-[(pyridin-2-ylmethyl)amino]thieno[2,3-d]pyrimidin-2-yl}piperidine-3-carboxylic acid 
• 1401985-49-6 N-(2-hydroxyethyl)-1-{5-phenyl-4-[(pyridin-2-ylmethyl)amino]thieno[2,3-d]pyrimidin-2-yl}piperidine-3-carboxamide 
• 1401985-56-5 (3S)-N-(2-hydroxyethyl)-1-{5-phenyl-4-[(pyridin-2-ylmethyl)amino]thieno[2,3-d]pyrimidin-2-yl}piperidine-3-carboxamide 

Relevant academic research and scientific papers

ECTONUCLEOTIDE PYROPHOSPHATASE/PHOSPHODIESTERASE 1 (ENPP1) MODULATORS AND USES THEREOF

Provided herein are small molecule modulators of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Design, Synthesis, and SAR Studies of Heteroarylpyrimidines and Heteroaryltriazines as CB2R Ligands

Herein we describe the design and synthesis of a new series of heteroarylpyrimidine/heteroaryltriazine derivatives on the basis of quinazoline-2,4(1H,3H)-diones as CB2R-selective ligands using a bioisosterism strategy. An acetamide group was explored to displace the enamine linker of the lead compound for the purpose of stereoisomerism elimination and hydrophilicity increase. As a result, some of the synthesized compounds showed high bioactivity and selectivity for CB2R in calcium mobilization assays, and four displayed CB2R agonist activity, with EC50 values below 30 nm. The compound exhibiting the highest agonist activity toward CB2R (EC50=7.53±3.15 nm) had a selectivity over CB1R of more than 1328-fold. Moreover, structure–activity relationship (SAR) studies indicated that the substituents on the nucleus play key roles in the functionality of a ligand, with one such example demonstrating CB2R antagonist activity. Additionally, molecular docking simulations were conducted with the aim of better understanding of these new derivatives in relation to the structural requirements for agonists/antagonists binding to CB2R.

Heteroarylpyrimindinedione derivative and use thereof

The invention provides a heteroarylpyrimindinedione derivative and use thereof. The heteroarylpyrimindinedione derivative comprises a compound with a structure shown as general formula I, and a pharmaceutically acceptable salt or hydrate thereof. The derivative is obtained by chemical synthesis, and pharmacological experiments prove that the active ligand with cannabinoid type II receptor CB2 can be used for preparation of drugs for prevention and mitigation of CB2 receptor-mediated diseases, and the drug is cannabinoid CB2 receptor agonist's agonist, partial agonist, inverse agonist or antagonist. And the general structural formula I is shown as the specification.

THIENO [2, 3-D] PYRIMIDINE DERIVATIVES AND THEIR USE TO TREAT ARRHYTHMIA

The present invention relates to thienopyrimidine compounds which are potassium channel inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also described.

THIENO [2, 3 -D] PYRIMIDINE DERIVATIVES AND THEIR USE TO TREAT ARRHYTHMIA

The present invention relates to thienopyrimidine compounds which are potassium channel inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also described.

THIENOPYRIMIDINE DERIVATIVES AS POTASSIUM CHANNEL INHIBITORS

The present invention provides thienopyrimidine compounds which are potasium channels inhibitors. Pharmaceutical compositions comprising the compounds and their use in the treatment of arrhythmia are also provided.