1015610-31-7Relevant articles and documents
Compound with pyrrolopyridine structure, preparation method and medical application
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, (2021/08/06)
The invention discloses a compound with a pyrrolopyridine structure, a preparation method and medical application. The compound with the pyrrolopyridine structure has obvious inhibitory activity on JAK family proteins, and is an effective JAK inhibitor, so that the compound has a prospect of being developed into drugs for inhibiting JAK and further treating diseases.
Compound of dipyrrolopyridine structure Preparation method and medical application
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, (2021/08/25)
The invention discloses a compound with a dipyrrolo-pyridine structure as well as a preparation method and medical application thereof. The compound provided by the invention has obvious inhibitory activity on JAK family proteins, is an effective JAK inhibitor, and has the prospect of being developed into drugs for inhibiting JAK and further treating diseases.
BICYCLIC HETEROAROMATIC COMPOUNDS
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, (2015/09/22)
Compounds of the formula I, in which X1, X2, X3, X4, X5, R1, R2, R3, R4, R5 and R6 have the meanings indicated in Claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
Fragment-based discovery of new highly substituted 1H-pyrrolo[2,3-b]- and 3H-imidazolo[4,5-b]-pyridines as focal adhesion kinase inhibitors
Heinrich, Timo,Seenisamy, Jeyaprakashnarayanan,Emmanuvel, Lourdusamy,Kulkarni, Santosh S.,Bomke, J?rg,Rohdich, Felix,Greiner, Hartmut,Esdar, Christina,Krier, Mireille,Gr?dler, Ulrich,Musil, Djordje
, p. 1160 - 1170 (2013/04/10)
Focal adhesion kinase (FAK) is considered as an attractive target for oncology, and small-molecule inhibitors are reported to be in clinical testing. In a surface plasmon resonance (SPR)-mediated fragment screening campaign, we discovered bicyclic scaffolds like 1H-pyrazolo[3,4-d]pyrimidines binding to the hinge region of FAK. By an accelerated knowledge-based fragment growing approach, essential pharmacophores were added. The establishment of highly substituted unprecedented 1H-pyrrolo[2,3-b]pyridine derivatizations provided compounds with submicromolar cellular FAK inhibition potential. The combination of substituents on the bicyclic templates and the nature of the core structure itself have a significant impact on the compounds FAK selectivity. Structural analysis revealed that the appropriately substituted pyrrolo[2,3-b]pyridine induced a rare helical DFG-loop conformation. The discovered synthetic route to introduce three different substituents independently paves the way for versatile applications of the 7-azaindole core.