[EN] A METHOD OF PREPARING ENANTIOMERS OF INDOLE-2,3-DIONE-3-OXIME DERIVATIVES [FR] PROCEDE DE PREPARATION D'ENANTIOMERES DE DERIVES D'INDOLE-2,3-DIONE-3-OXIME
[EN] MULTICYCLIC PEPTIDES AND METHODS FOR THEIR PREPARATION<br/>[FR] PEPTIDES MULTICYCLIQUES ET LEURS PROCÉDÉS DE PRÉPARATION
申请人:STICHTING TECHNISCHE WETENSCHAPPEN
公开号:WO2018106112A1
公开(公告)日:2018-06-14
The invention relates to methods for preparing a compound comprising a peptide attached to a molecular scaffold whereby multiple peptide loops are formed, to compounds that can be obtained with such methods and uses thereof.
Structure-activity relationships of pyrimidine nucleotides containing a 5′-α,β-methylene diphosphonate at the P2Y6 receptor
作者:Paola Oliva、Mirko Scortichini、Clemens Dobelmann、Shanu Jain、Varun Gopinatth、Kiran S. Toti、Ngan B. Phung、Anna Junker、Kenneth A. Jacobson
DOI:10.1016/j.bmcl.2021.128137
日期:2021.8
highest human P2Y6R potency (MRS4554, 0.57 µM), and a 5-fluoro substitution of the cytosine ring in 28 similarly enhancedpotency, with >175- and 39-fold selectivity over human P2Y14R, respectively. However, 3-alkyl (31 – 33, 37, 38), β-D-arabinofuranose (39) and 6-aza (40) substitution prevented P2Y6R activation. Thus, we have identified new α,β -methylene bridged N4-extended CDP analogues as P2Y6R
Heteroaryl derivatives of monocyclic beta-lactam antibiotics
申请人:E. R. Squibb & Sons, Inc.
公开号:US05250691A1
公开(公告)日:1993-10-05
Compounds having the formula ##STR1## exhibiting antibacterial activity.
具有##STR1##分子式的化合物表现出抗菌活性。
Intermediates for the preparation of heteroaryl derivatives of
申请人:E. R. Squibb & Sons, Inc.
公开号:US05420277A1
公开(公告)日:1995-05-30
Antibacterial activity is exhibited by novel compounds having the formula ##STR1## where R.sub.1, R.sub.2, and M are as defined herein and X is --(CH.sub.2).sub.n -- wherein n is 0, 1, 2, 3 or 4 or CR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen, --CH.sub.3 or --C.sub.2 H.sub.5 or R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached form a 3, 4, 5, 6 or 7-membered cycloalkyl ring. Also described are various intermediates for the preparation of compounds of formula 1.