Preformed Selenoesters Enable Rapid Native Chemical Ligation at Intractable Sites
作者:Thomas Durek、Paul F. Alewood
DOI:10.1002/anie.201105512
日期:2011.12.9
Pro–Cys ligation using a preformed prolyl selenoester is reported (see scheme; P=peptide). In a comparative study of peptide selenoesters in nativechemicalligation peptide α‐selenoesters are shown to be superior acyl donors and result in rate enhancements of at least two orders of magnitude when compared to the well‐established peptide α‐thioesters. This method permits rapidchemicalligation even at
转为亲:报道了使用预制的脯氨酰硒酸酯的第一个简便的Pro-Cys连接(请参阅方案; P =肽)。在天然化学连接中进行的肽硒酸酯的比较研究表明,与成熟的肽α-硫酯相比,肽α-硒酸酯是优异的酰基供体,其速率提高至少两个数量级。即使在以前难以治疗的部位,例如Pro-Cys,该方法也可以进行快速化学连接。
[EN] BIARYL DERIVATIVES AS GPR120 AGONISTS<br/>[FR] DÉRIVÉS DE BIARYLE EN TANT QU'AGONISTES DE GPR120
申请人:LG LIFE SCIENCES LTD
公开号:WO2014209034A1
公开(公告)日:2014-12-31
The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.
The compounds of Formula (I) wherein R1, R21, R22, R23, R24, Y and R3 have the meanings as given in the description, the salts thereof, the N-oxides of the compounds and the salts thereof and the stereoisomers of the compounds, the salts, the N-oxides of the compounds and the N-oxides of the salts thereof are effective inhibitors of the type 5 phosphodiesterase.
The invention relates to thiophene carboxanmides of formula (I). wherein A, R
1
, R
2
, R
3
, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
1