453566-61-5

Upstream product

• 661458-28-2 methyl 3-cyano-5-methoxybenzoate 
• 71590-09-5 methyl 3-(chlorocarbonyl)-5-methoxybenzoate 
• 71590-08-4 5-methoxy-isophthalic acid monomethyl ester 
• 20319-44-2 dimethyl 5-methoxyisophthalate 
• 13036-02-7 Dimethyl 5-hydroxyisophthalate 
• 916343-75-4 methyl 3-methoxy-5-(trifluoromethanesulfonyloxy)benzoate 
• 19520-74-2 3-hydroxy-5-methoxy-benzoic acid methyl ester 

Relevant academic research and scientific papers

Rational design of inhibitors of the bacterial cell wall synthetic enzyme GlmU using virtual screening and lead-hopping

An aminoquinazoline series targeting the essential bacterial enzyme GlmU (uridyltransferase) were previously reported (Biochem. J. 2012, 446, 405). In this study, we further explored SAR through a combination of traditional medicinal chemistry and structure-based drug design, resulting in a novel scaffold (benzamide) with selectivity against protein kinases. Virtual screening identified fragments that could be fused into the core scaffold, exploiting additional binding interactions and thus improving potency. These efforts resulted in a hybrid compound with target potency increased by a 1000-fold, while maintaining selectivity against selected protein kinases and an improved level of solubility and protein binding. Despite these significant improvements no significant antibacterial activity was yet observed within this class.

DIHYDRO- 1H- PYRROLO [1,2-A] INDOL-1-YL CARBOXYLIC DERIVATIVES WHICH ACT AS S1P1 AGONISTS

The present invention relates to certain (1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-pyrrolo[1,2-a]indol-1-yl carboxylic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, sepsis, myocardial infarction, ischemic stroke, acne, microbial infections or diseases and viral infections or diseases.

NEW COMPOUNDS

The present invention relates to new compounds of formula I, wherein P Q X1 X2 X3 X4 X5 R R1 R2 R3 R4R5 G M1 M2 M3 m and n are defined as in formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.