1450642-51-9Relevant articles and documents
5-(1H-Pyrazol-4-yl)-1H-Pyrrolo[2,3-b]Pyridine Derivatives as Kinase Inhibitors
-
Paragraph 0183-0185, (2015/07/15)
The present application relates to novel 5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to prodrugs, derivatives, polymorphs, pharmaceutically acceptable salts and compositions comprising the said novel 5-(1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridine compounds and their derivatives and their use in the treatment of various disorders.
Discovery of 7-azaindole based anaplastic lymphoma kinase (ALK) inhibitors: Wild type and mutant (L1196M) active compounds with unique binding mode
Gummadi, Venkateshwar Rao,Rajagopalan, Sujatha,Looi, Chung-Yeng,Paydar, Mohammadjavad,Renukappa, Girish Aggunda,Ainan, Bharathi Raja,Krishnamurthy, Narasimha Rao,Panigrahi, Sunil Kumar,Mahasweta, Kumari,Raghuramachandran, Sangeetha,Rajappa, Manoj,Ramanathan, Anuradha,Lakshminarasimhan, Anirudha,Ramachandra, Murali,Wong, Pooi-Fong,Mustafa, Mohammad Rais,Nanduri, Srinivas,Hosahalli, Subramanya
, p. 4911 - 4918 (2013/09/02)
We have identified a novel 7-azaindole series of anaplastic lymphoma kinase (ALK) inhibitors. Compounds 7b, 7m and 7n demonstrate excellent potencies in biochemical and cellular assays. X-ray crystal structure of one of the compounds (7k) revealed a unique binding mode with the benzyl group occupying the back pocket, explaining its potency towards ALK and selectivity over tested kinases particularly Aurora-A. This binding mode is in contrast to that of known ALK inhibitors such as Crizotinib and NVP-TAE684 which occupy the ribose binding pocket, close to DFG motif.