788799-69-9Relevant articles and documents
Bis(vinylsulfonyl)piperazines as efficient linkers for highly homogeneous antibody-drug conjugates
Huang, Rong,Sheng, Yao,Wei, Ding,Yu, Jianghui,Chen, Hongli,Jiang, Biao
, (2020/02/04)
Disulfide re-bridging strategy has demonstrated significant advantages in the construction of homogeneous antibody drug conjugates (ADCs). However, a major issue that disulfide scrambling at the hinge region of antibody leads to the formation of “half-antibody” has appeared for many re-bridging linkers. We present bis(vinylsulfonyl)piperazines (BVP) as efficient linkers to selectively re-bridge disulfides at the antigen-binding fragment (Fab) regions and produce highly homogeneous conjugates with a loading of two drugs without disulfide scrambling. We also found that optically active (S)-configuration linkers led to more sufficient conjugation compared with (R)-configuration. The BVP-linked ADCs demonstrated superior efficacy and antigen-selectivity in vitro cytotoxicity.
PYRAZOLOPYRIDINE KINASE INHIBITORS
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Page/Page column 42-43, (2011/08/21)
The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, co
PIPERAZINES AS ANTI-OBESITY AGENTS
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Page/Page column 26, (2009/07/17)
The present invention relates to new compounds of formula (I), to pharmaceutical compositions comprising these compounds, to processes for their preparation, and to the use of these compounds as leptin receptor modulator mimetics in the preparation of medicaments against conditions associated with weight gain, type 2 diabetes and dyslipidemias.