1296202-59-9

Upstream product

• 45644-21-1 6-chloropyridin-2-amine 
• 800402-05-5 N-(6-chloro-3-iodopyridin-2-yl)-tert-butylamide 
• 800402-06-6 6-chloro-3-iodo-pyridin-2-ylamine 
• 800402-07-7 6-chloro-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid 
• 2393-23-9 4-methoxy-benzylamine 
• 86847-84-9 2,2-Dimethyl-N-(6-chloro-2-pyridinyl)propanamide 

Downstream Products

• 1296200-17-3 6-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylic acid 4-methoxybenzylamide 

Relevant academic research and scientific papers

6-chlorine-N-(substituted benzyl)-1H-pyrrolo[2,3-b]pyridine-2-amide compound and preparation method as well as application thereof

The invention discloses a 6-chlorine-N-(substituted benzyl)-1H-pyrrolo[2,3-b]pyridine-2-amide compound and a preparation method as well as application thereof, belonging to the field of HIV-1 integrase inhibitors. The compound is represented by a general formula (I), wherein R1 represents -F, -Me, -OMe and -H; R2 represents -H, -F, -Me, -OMe and -Cl; R3 represents -H, -F, -Me, -OMe, -Cl, -Br, -CF3 and -SO2Me. The preparation method of the compound comprises the steps of synthetising N-(6-chloropyridine-2-tertiary butyl) amide by using 6-chloropyridine-2-amine as a raw material and pivaloyl chloride, performing pyridine ring iodination, then hydrolyzing to obtain 6-chlorine-3-iodine pyridine-2-amine, cyclizing to obtain a compound with a carboxylic acid structure, and finally reacting with various substituted benzyls to obtain the compound disclosed by the invention.

Discovery and optimization of indoles and 7-azaindoles as Rho kinase (ROCK) inhibitors (part-I)

Rho kinase (ROCK) inhibitors are potential therapeutic agents to treat disorders such as hypertension, multiple sclerosis, cancers, and glaucoma. Here, we disclose the synthesis, optimization, biological evaluation of potent indole and 7-azaindole based ROCK inhibitors that have high potency on ROCK (IC 50 = 1 nM) with 740-fold selectivity over PKA (47). Moreover, 47 showed very good DMPK properties making it a good candidate for further development. Finally, docking studies with a homology model of ROCK-II were performed to rationalize the binding mode of these compounds and showed the compounds bound in both orientations to take advantage to H-bonds with Lys-121 of ROCK-II.

BICYCLIC HETEROARYLS AS KINASE INHIBITORS

The invention is directed to heteroaryl compounds useful as inhibitors of various kinase enzymes. In various embodiments, the invention provides a heteroaryl compound having inhibitory bioactivity with respect to a Rho kinase, an AKT kinase, a p70S6K kinase, a LIM kinase, an IKK kinase, a Flt kinase, an Aurora kinase, or a Src kinase, or any combination thereof. Compounds of the invention include bicyclic heteroaryl compounds of formula (I), which can contain a bridging nitrogen atom at a ring junction. The invention further provides methods of synthesis of compounds of the invention, pharmaceutical compositions, pharmaceutical combinations, and methods of treatment of malconditions using compounds of the invention.