33038-04-9

Upstream product

• 705-15-7 1-(2-hydroxy-5-methoxyphenyl)ethan-1-one 
• 105-36-2 ethyl bromoacetate 
• 105-39-5 chloroacetic acid ethyl ester 

Downstream Products

• 81718-77-6 5-methoxy-3-methyl-benzofuran-2-carboxylic acid 
• 33038-06-1 2-(2-acetyl-4-methoxyphenoxy)acetic acid 
• 7182-30-1 5-methoxy-3-methyl-1-benzofuran 
• 77956-74-2 2,3,4,5-tetrahydro-7-methoxy-1-benzoxepin-3,5-dione 
• 3710-50-7 ethyl 5-methoxy-3-methyl-1-benzofuran-2-carboxylate 
• 142143-40-6 (2R,3S)-3-Hydroxy-5-methoxy-3-methyl-2,3-dihydro-benzofuran-2-carboxylic acid ethyl ester 
• 142143-40-6 (2S,3S)-3-Hydroxy-5-methoxy-3-methyl-2,3-dihydro-benzofuran-2-carboxylic acid ethyl ester 
• 7182-21-0 5-hydroxy-3-methylbenzo<1.2-b>furan 

Relevant academic research and scientific papers

Amide compound and its preparation method, pharmaceutical composition and use thereof

The present invention relates to amide compounds as shown by structural formula (I). The compounds are low absorbable TGR5 agonists and can be used to treat type II diabetes, obesity, liver or intestine chronic inflammatory diseases.

Structure-activity relationships for a novel series of dopamine D2-like receptor ligands based on N-substituted 3-aryl-8-azabicyclo[3.2.1]octan-3-ol

Discovering dopamine D2-like receptor subtype-selective ligands has been a focus of significant investigation. The D2R-selective antagonist 3-[4-(4-chlorophenyl)-4-hydroxypiperidinyl]methylindole (1, L741,626; K i(D2R/D3R) = 11.2:163 nM) has previously provided a lead template for chemical modification. Herein, analogues have been synthesized where the piperidine was replaced by a tropane ring that reversed the selectivity seen in the parent compound, in human hD2LR- or hD3R-transfected HEK 293 cells (31, Ki(D2R/D3R) = 33.4: 15.5 nM). Further exploration of both N-substituted and aryl ring-substituted analogues resulted in the discovery of several high affinity D2R/D3R ligands with 3-benzofurylmethyl-substituents (e.g., 45, Ki(D2R/D3R) = 1.7:0.34 nM) that induced high affinity not achieved in similarly N-substituted piperidine analogues and significantly (470-fold) improved D3R binding affinity compared to the parent ligand 1. X-ray crystallographic data revealed a distinctive spatial arrangement of pharmacophoric elements in the piperidinol vs tropine analogues, providing clues for the diversity in SAR at the D2 and D3 receptor subtypes.

NEW TRICYCLIC DERIVATIVES AS LTD4 ANTAGONISTS

Compounds of formula (I) and their pharmaceutically acceptable salts are provided as well as processes for the manufacture of such compounds. The compounds are useful in the treatment or prevention of inflammatory and allergic diseases.