332099-35-1

Upstream product

• 934246-45-4 ethyl 2-azido-3-(4-bromo-2-thienyl)acrylate 
• 18791-75-8 4-Bromothiophen-2-aldehyde 

Downstream Products

• 332099-31-7 ethyl 3-chloro-4H-thieno[3,2-b]pyrrole-5-carboxylate 
• 332099-36-2 3-bromo-4H-thieno[3,2-b]pyrrole-5-carboxylic acid 
• 1450743-07-3 ethyl 3-bromo-4-(4-fluorophenyl)-4H-thieno[3,2-b]pyrrole-5-carboxylic acid 
• 1450743-14-2 ethyl 4-(4-fluorophenyl)-3-(trifluoromethyl)-4H-thieno[3,2-b]pyrrole-5-carboxylic acid 
• 1450743-08-4 3-bromo-N-(3,4-dichlorobenzyl)-N-(2-(dimethylamino)ethyl)-4-(4-fluorophenyl)-4H-thieno[3,2-b]pyrrole-5-carboxamide 
• 1450743-09-5 N-(3,4-dichlorobenzyl)-N-(2-(dimethylamino)ethyl)-4-(4-fluorophenyl)-4H-thieno[3,2-b]pyrrole-5-carboxamide 
• 1450743-10-8 N-(3,4-dichlorobenzyl)-N-(2-(dimethylamino)ethyl)-4-(4-fluorophenyl)-3-methyl-4H-thieno[3,2-b]pyrrole-5-carboxamide 
• 1450743-11-9 3-chloro-N-(3,4-dichlorobenzyl)-N-(2-(dimethylamino)ethyl)-4-(4-fluorophenyl)-4H-thieno[3,2-b]pyrrole-5-carboxamide 
• 1450743-06-2 ethyl 4-(4-fluorophenyl)-3-(trifluoromethyl)-4H-thieno[3,2-b]pyrrole-5-carboxylate 
• 1450743-12-0 N-(3,4-dichlorobenzyl)-N-(2-(dimethylamino)ethyl)-4-(4-fluorophenyl)-3-(trifluoromethyl)-4H-thieno[3,2-b]pyrrole-5-carboxamide 
• 1450743-13-1 3-cyano-N-(3,4-dichlorobenzyl)-N-(2-(dimethylamino)ethyl)-4-(4-fluorophenyl)-4H-thieno[3,2-b]pyrrole-5-carboxamide 
• 1450743-05-1 ethyl 3-bromo-4-(4-fluorophenyl)-4H-thieno[3,2-b]pyrrole-5-carboxylate 

Relevant academic research and scientific papers

Synthetic studies of centromere-associated protein-E (CENP-E) inhibitors: 1.Exploration of fused bicyclic core scaffolds using electrostatic potential map

Centromere-associated protein-E (CENP-E), a mitotic kinesin that plays an important role in mitotic progression, is an attractive target for cancer therapeutic drugs. For the purpose of developing novel CENP-E inhibitors as cancer therapeutics, we investigated a fused bicyclic compound identified by high throughput screening, 4-oxo-4,5-dihydrothieno[3,4-c]pyridine-6-carboxamide 1a. Based on this scaffold, we designed inhibitors for efficient binding at the L5 site in CENP-E utilizing homology modeling as well as electrostatic potential map (EPM) analysis to enhance CENP-E inhibitory activity. This resulted in a new lead, 5-bromoimidazo[1,2-a]pyridine 7, which showed potent CENP-E enzyme inhibition (IC50: 50 nM) and cellular activity with accumulation of phosphorylated histone H3 in HeLa cells. Our homology model and EPM analysis proved to be useful tools for the rational design of CENP-E inhibitors.

Synthesis and CHK1 inhibitory potency of Hymenialdisine analogues

A series of thieno[3,2-b]pyrroloazepinones derivatives related to Hymenialdisine were prepared and tested for CHK1 inhibitory activity. Nanomolar inhibitions were achieved when electron-withdrawing substituents were introduced at position 3 of the thiophene ring.

FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE

This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O?X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.

USE OF FUSED PYRROLE CARBOXYLIC ACIDS FOR THE TREATMENT OF NEURODEGENERATIVE AND PSYCHIATRIC DISEASES AS D-AMINO ACID OXIDASE INHIBITORS

The present invention provides the use of fused pyrrole carboxylic acids of formula (I) for the manufacture of a medicament to inhibit D-amino acid oxidase, particularly for the treatment of neurodegenerative and psychiatric disorders or diseases; certain

Heterocyclic compounds

Certain thienopyrrolyl and furanopyrrolyl compounds are disclosed as useful to treat or prevent disorders and conditions mediated by the histamine H4 receptor, including allergic rhinitis.

Bicyclic pyrrole derivatives as MCP-1 inhibitors

A pharmaceutical composition comprising a compound of formula (I): or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1 and wherein A and B together form an optionally substituted 5-member aromatic ring which includes at least one heteroatom; R1is an optionally substituted aryl or heteroaryl ring; R2is selected from a range of organic groups including carboxy, and R3is hydrogen, or a range of organic groups; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and these form a further aspect of the invention.