Novartis Ag

Other

Irm LLC

Xueshi Hao

Tetsuo Uno

Bernhard Hubert Geierstanger

Weijia Ou

Jan Grunewald

Qihui Jin

Susan E Cellitti

Hsien-Po Chiu

Tiffany Crossgrove

Jun Liu

Qiang Ding

Dirk Behnke

Yunho Jin

Juergen Klaus Maibaum

Timothy Z Hoffman

Barun Okram

Xu Wu

Yahua Liu

Yefen Zou

Jianwei Che

Jianfeng Pan

Yun Feng Xie

Cameron Lee

Arnaud Lacoste

S Frank Yan

Tingting Mo

Frada Berenshteyn

Yahu Liu

Xin Qu

Jan Tchorz

Shanshan Yan

Timothy Hoffman

The present invention is related to 6-6 Fused Bicyclic Heteroaryl Compounds of the Formula A2 or A1 and their Use as LATS Inhibitors, or a salt, stereoisomer or pharmaceutical composition thereof; wherein the variables are as defined herein. The present invention further relates to a method of LATS inhibition in a cell population using a compound of Formula A1, or a salt, stereoisomer or pharmaceutical composition thereof. The present invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, their use in the treatment and management of diseases or disorders.

6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors

Disclosed herein is pyrroline-carboxy-lysine (PCL), a pyrrolysine analog, which is a natural, biosynthetically generated amino acid, and methods for biosynthetically generating PCL. Also disclosed herein are proteins, polypeptides and peptides that have PCL incorporated therein and methods for incorporating PCL into such proteins, polypeptides and peptides. Also disclosed herein is the site-specific derivatization of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein. Also disclosed herein is the crosslinking of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein.

Biosynthetically generated pyrroline-carboxy-lysine and site specific protein modifications via chemical derivatization of pyrroline-carboxy-lysine and pyrrolysine residues

Disclosed herein is pyrroline-carboxy-lysine (PCL), a pyrrolysine analogue, which is a natural, biosynthetically generated amino acid, and methods for biosynthetically generating PCL. Also disclosed herein are proteins, polypeptides and peptides that have PCL incorporated therein and methods for incorporating PCL into such proteins, polypeptides and peptides. Also disclosed herein is the site-specific derivatization of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein. Also disclosed herein is the crosslinking of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein.

The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT3, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS, or combinations thereof.

Compounds and compositions as kinase inhibitors

Growing community of inventors

San Diego, CA, United States of America

Xueshi Hao