Anilino-pyrimidine phenyl and benzothiophene analogs
申请人:Hu Yongbo
公开号:US20070244140A1
公开(公告)日:2007-10-18
The present invention relates to compounds of formula III:
wherein R
2
, R
3
, R
5
and R
6
are as defined herein.
本发明涉及以下式III的化合物:
其中R2、R3、R5和R6如本文所定义。
Synthesis and evaluation of 6-methylene-bridged uracil derivatives. Part 2: Optimization of inhibitors of human thymidine phosphorylase and their selectivity with uridine phosphorylase
A series of novel 6-methylene-bridged uracil derivatives have been optimized for clinical use as the inhibitors of human thymidine phosphorylase (TP). We describe their synthesis and evaluation. Introduction of a guanidino or an amidino group enhanced the in vitro inhibitory activity of TP comparing with formerly reported inhibitor 1. Their selectivity for TP based on uridine phosphorylase inhibitory
CRYSTALLINE POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS D-GLUCORONATE SALTS
申请人:Mirmehrabi Mahmoud
公开号:US20080262010A1
公开(公告)日:2008-10-23
The present invention relates to methods for preparing one or more crystalline polymorphs of a compound of formula I:
and structurally related compounds. The present invention is also directed to methods for converting one polymorph to other different polymorphs of formula I and structurally related compounds.
HEXAHYDRO-PYRAZINO[1,2-A]PYRIMIDINE-4,7-DIONE DERIVATIVES SUBSTITUTED WITH AMINO ACIDS
申请人:Lennig Petra
公开号:US20070197539A1
公开(公告)日:2007-08-23
The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments
[DE] MIT AMINOSÄUREN SUBSTITUIERTE HEXAHYDRO-PYRAZINO[1,2-A]PYRIMIDIN-4, 7-DIONDERIVATE<br/>[EN] HEXAHYDRO-PYRAZINO[1,2-A]PYRIMIDINE-4, 7-DIONE DERIVATIVES SUBSTITUTED WITH AMINO ACIDS<br/>[FR] DERIVES D'HEXAHYDRO-PYRAZINO[1,2-A]PYRIMIDIN-4,7-DIONE SUBSTITUES PAR DES AMINOACIDES, LEUR PROCEDE DE PRODUCTION, ET LEUR UTILISATION EN TANT QUE MEDICAMENTS
申请人:SANOFI AVENTIS DEUTSCHLAND
公开号:WO2006024390A1
公开(公告)日:2006-03-09
Die Erfindung betrifft substituierte Hexahydro-pyrazino[1,2-a]pyrimidin-4,7-dionderivate sowie deren physiologisch verträgliche Salze und physiologisch funktionelle Derivate. Es werden Verbindungen der Formel (I), worin die Reste die angegebenen Bedeutungen haben, sowie deren physiologisch verträglichen Salze und Verfahren zu deren Herstellung beschrieben. Die Verbindungen eignen sich z.B. als Anorektika.