Piperidine-based glycodendrons as protein N-glycan prosthetics
摘要:
The generation of homogeneously glycosylated proteins is essential for defining glycoform-specific activity and improving protein-based therapeutics. We present a novel glycodendron prosthetic which can be site-selectively appended to recombinant proteins to create 'N-glycosylated' glycoprotein mimics. Using computational modeling, we designed the dendrimer scaffold and protein attachment point to resemble the native N-glycan architecture. Three piperidine-melamine glycodendrimers were synthesized via a chemoenzymatic route and attached to human growth hormone and the F-c region of human IgG. These products represent a new class of engineered biosimilars bearing novel glycodendrimer structures. (C) 2016 Elsevier Ltd. All rights reserved.
Piperidine-based glycodendrons as protein N-glycan prosthetics
摘要:
The generation of homogeneously glycosylated proteins is essential for defining glycoform-specific activity and improving protein-based therapeutics. We present a novel glycodendron prosthetic which can be site-selectively appended to recombinant proteins to create 'N-glycosylated' glycoprotein mimics. Using computational modeling, we designed the dendrimer scaffold and protein attachment point to resemble the native N-glycan architecture. Three piperidine-melamine glycodendrimers were synthesized via a chemoenzymatic route and attached to human growth hormone and the F-c region of human IgG. These products represent a new class of engineered biosimilars bearing novel glycodendrimer structures. (C) 2016 Elsevier Ltd. All rights reserved.
The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
The invention relates to compounds of formula (I) and salts thereof:
wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
The invention relates to compounds of formula (I) and salts thereof:
wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
Verbindungen der Formel
worin X für Methylen, Imino, Sauerstoff oder Schwefel steht und R einen Rest
bezeichnet, worin n 0, 1 oder 2 bedeutet, mit der Massgabe, dass n nicht 0 bedeutet, wenn R in Position 2 gebunden ist, und Salze davon haben eine starke spezifische Hemmwirkung auf das Enzym Ornithindecarboxylase. Die Verbindungen der Formel I werden nach an sich bekannten Verfahren hergestellt.
式中 X 为亚甲基、亚氨基、氧或硫,R 为自由基,其中 n 为 0、1 或 2,但当 R 结合在位置 2 时,n 不为 0 的化合物及其盐类对鸟氨酸脱羧酶有很强的特异性抑制作用。 式 I 的化合物是通过本身已知的方法制备的。
PENICILLIN-BINDING PROTEIN INHIBITORS
申请人:VenatoRx Pharmaceuticals, Inc.
公开号:US20200102331A1
公开(公告)日:2020-04-02
Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds described herein inhibit penicillin-binding proteins. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.