32012-12-7Relevant articles and documents
Amine derivative, and preparation method and medical application thereof
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Paragraph 0179; 0180; 0181; 0184; 0185, (2021/09/15)
The present invention relates to a compound represented by formula (I), or a stereoisomer, a pharmaceutically acceptable salt and a medical use thereof. The compound shown in the formula (I) can be effectively combined with BRD4, and can be used as a BRD4 inhibitor for treating various diseases related to BRD4.
NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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Page/Page column 132-133, (2008/12/07)
The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1 ), and their use as pharmaceutical compositions.
Functionalized DL-Amino Acid Derivatives. Potent New Agents for the Treatment of Epilepsy
Conley, Judith D.,Kohn, Harold
, p. 567 - 574 (2007/10/02)
Structural analogues of the potent known anticonvulsant agent N-acetyl-DL-alanine N-benzylamide (1a) have been prepared (16 examples).The pharmacological activities of these products were evaluated in the maximal electroshock seizure (MES), the subcutaneous pentylenetetrazole seizure threshold (sc Met), and the rotorod (Tox) tests.The median effective doses (ED50) and the median toxic doses (TD50) for the most active compounds by both intraperitoneal and oral administration are reported.The most active compounds were N-acetyl-DL-phenylglycine N-benzylamide (1d) and N-acetyl-DL-alanine N-m-fluorobenzylamide (1m) along with the parent compound 1a.The ED50 values in the MES test for these three compounds compared well with phenobarbital, while their high TD50 values contributed to their large protective indexes, which approached that of phenytoin.When tested against four convulsant agents, compounds 1a and 1d displayed activity profiles significantly different from those reported for conventionally used antiepileptic drugs.