- N-Methyl- N-phenylvinylsulfonamides for Cysteine-Selective Conjugation
-
Use of N-methyl-N-phenylvinylsulfonamides to perform chemoselective modification of cysteine-containing peptides and proteins is reported. Probes linked to the drug were applicable to prepare antibody-drug conjugates (ADCs). The drug-antibody ratio for AD
- Huang, Rong,Li, Zhihong,Sheng, Yao,Yu, Jianghui,Wu, Yue,Zhan, Yuexiong,Chen, Hongli,Jiang, Biao
-
-
Read Online
- BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors
-
The application of BN/CC isosterism is explored as a method of expanding the scope of core scaffolds in biologically active compounds. The viability of potential drug candidates incorporating BN-heteroaromatic moieties was investigated through the synthesis of BN-substituted analogs to known phosphodiesterase (PDE10A) inhibitors, namely MP10 and a selection of N-methylanilide analogs. These in some cases revealed unexpectedly potent and relatively stable derivatives, providing further support for the potential of BN-incorporation in medicinal chemistry.
- Vlasceanu, Alexandru,Jessing, Mikkel,Kilburn, John Paul
-
-
Read Online
- SUBSTITUTED QUINOLINES AND METHODS FOR TREATING CANCER
-
Substituted quinoline compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or ameliorate cancer are provided.
- -
-
Paragraph 0301
(2018/05/24)
-
- Analine derivatives as OSC inhibitors
-
The present invention relates to compounds of formula (I) wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
- -
-
-