137581-63-6Relevant articles and documents
Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers
Chen, Xiaoling,Clark, Anderson,Crowley, Lindsey,Deselm, Lizbeth,Georgi, Katrin,Goutopoulos, Andreas,Haxell, Thomas,Heasley, Brian H.,Huck, Bayard,Jackson, Jennifer,Johnson, Theresa,Jones, Reinaldo,Lan, Ruoxi,Lin, Jing,Machl, Andreas,Mochalkin, Igor,Moore, Joseph,Neagu, Constantin,Potnick, Justin,Richardson, Thomas E.,Rohdich, Felix,Sherer, Brian,Sutton, Amanda,Tian, Hui,Wilker, Erik,Xiao, Yufang
, p. 14603 - 14619 (2021/10/20)
Herein, we report the discovery of a novel class of quinazoline carboxamides as dual p70S6k/Akt inhibitors for the treatment of tumors driven by alterations to the PI3K/Akt/mTOR (PAM) pathway. Through the screening of in-house proprietary kinase library, 4-benzylamino-quinazoline-8-carboxylic acid amide 1 stood out, with sub-micromolar p70S6k biochemical activity, as the starting point for a structurally enabled p70S6K/Akt dual inhibitor program that led to the discovery of M2698, a dual p70S6k/Akt inhibitor. M2698 is kinase selective, possesses favorable physical, chemical, and DMPK profiles, is orally available and well tolerated, and displayed tumor control in multiple in vivo studies of PAM pathway-driven tumors.
CEPHALOSPORIN HAVING CATECHOL GROUP
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Page/Page column 120-121, (2011/07/30)
The present invention provides Cephem compounds which have a wide antimicrobial spectrum and have potent antimicrobial activity against beta-lactamase producing Gram negative bacteria as follows: A compound of the formula: wherein, X is N, CH or C-Cl; T is S or the like; A and G are lower alkylene or the like; B is a single bond or the like; D is a single bond, -NR7-, -CO-, -CO-NR7-, -NR7-CO-, -NR7-CO-NR7-, or the like; E is optionally substituted lower alkylene; F is a single bond or optionally substituted phenylene; R3, R4, R5 and R6 each is independently hydrogen, halogene, nitrile, or the like; or an ester, a compound protected at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
DPP-IV INHIBITORS
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Page/Page column 44, (2010/02/14)
The invention relates to compounds of formula (I), Z-C(R1R 2)-C(R3NH2)-C(R4R5)-X-N(R 6R7), wherein Z, R1-7 and X have the meaning as cited in the description and the claims. Said compounds are useful as DPP-lV inhibitors. The invention also relates to the