304477-85-8

Upstream product

• 2365-48-2 Methyl thioglycolate 
• 68-12-2 N,N-dimethyl-formamide 
• 99-02-5 3'-Chloroacetophenone 
• 107818-32-6 (Z)-3-Chloro-3-(3-chloro-phenyl)-acrylonitrile 

Downstream Products

• 354811-91-9 3-amino-5-(3-chlorophenyl)-2-thiophenecarboxamide 
• 917597-43-4 methyl 5-(3-chlorophenyl)-3-{[(1E)-(dimethylamino)methylidene]amino}-2-thiophenecarboxylate 
• 354811-90-8 3-Amino-5-(3-chlorophenyl)-2-thiophenecarboxylic acid 

Relevant academic research and scientific papers

EIF4E INHIBITORS AND USES THEREOF

The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.

Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: Structure-based optimization of a virtual screening hit

Rising resistance against current antibiotics necessitates the development of antibacterial agents with alternative targets. The "switch region" of RNA polymerase (RNAP), addressed by the myxopyronins, could be such a novel target site. Based on a hit can

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists

Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in

Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1

The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat diet-induced obesity of MCH KO mice has spurred considerable efforts to develop small molecule MCHR1 antagonists. Starting from a lead thienopyrimidinone series, structure-activity studies at the 3- and 6-positions of the thienopyrimidinone core afforded potent and selective MCHR1 antagonists with representative examples having suitable pharmacokinetic properties. Based on structure-activity relationships, a structural model for MCHR1 was constructed to explain the binding mode of these antagonists. In general, a good correlation was observed between pKas and activity in the right-hand side of the template, with Asp123 playing an important role in the enhancement of binding affinity. A representative example when evaluated chronically in diet-induced obese mice resulted in good weight loss effects. These antagonists provide a viable lead series in the discovery of new therapies for the treatment of obesity.

Novel Compounds

The invention relates to heteroaromatic carboxamides of formula (I), wherein A, R1, R2 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Cyclic regimens using cyclocarbamate and cyclic amide derivatives

This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: where A and B are ind

Cyclocarbamate and cyclic amide derivatives

This invention provides compounds of the formula: wherein A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N,