以4-叔丁基苯胺为原料,通过酰化,取代和水解反应,合成了一系列的2,3-二甲基-4-(1-酰氧基)烷氧基-6-叔丁基-8-氟喹啉。并通过1 H NMR,13 C NMR和HRMS对其结构进行了表征。杀菌活性表明,化合物6c,6e和6f对短小镰刀菌具有优异的活性,EC 50值分别为38.62、6.77和50.35 mg / L。结果表明这种化合物的化学型值得作为有希望的杀真菌剂进行进一步的研究。
[EN] METHODS OF TREATMENT OF AMYLOIDOSIS USING ASPARTYL-PROTEASE INIHIBITORS<br/>[FR] PROCEDES DE TRAITEMENT D'AMYLOIDOSE UTILISANT DES INHIBITEURS DE PROTEASE ASPARTYLE
申请人:ELAN PHARM INC
公开号:WO2005070407A1
公开(公告)日:2005-08-04
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
The present invention relates to compounds of formula (I-VII)
or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R
6
, R
7
and R
8
are defined herein. The present invention also relates to methods of trating pain using these compounds and pharmaceutical compositions including these compounds.
[EN] SUBSTITUTED UREA AND CARBAMATE, PHENACYL-2-HYDROXY-3-DIAMINOALKANE, AND BENZAMIDE-2-HYDROXY-3-DIAMINOALKANE ASPARTYL-PROTEASE INHIBITORS<br/>[FR] UREE ET CARBAMATE SUBSTITUES, PHENACYL-2-HYDROXY-3-DIAMINOALCANE, ET BENZAMIDE-2-HYDROXY-3-DIAMINOALCANE INHIBITEURS D'ASPARTYL-PROTEASE
申请人:ELAN PHARM INC
公开号:WO2005087215A1
公开(公告)日:2005-09-22
The invention relates to acetyl 2-hydroxy-1,3-diaminospirocyclohexanes and derivatives thereof that are useful in treating at least one disease, disorder, and condition associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and condition associated with abnormal deposition of A-beta protein.
Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
本文提供了dUTPase抑制剂,包括这类化合物的组合物以及使用这类化合物和组合物的方法。
[EN] 1,4-DISUBSTITUTED ISOQUINILONE DERIVATIVES AS RAF-KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES<br/>[FR] DERIVES D'ISOQUINILONE 1,4-DISUBSTITUES EN TANT QU'INHIBITEURS DE RAF-KINASE UTILES POUR LE TRAITEMENT DE MALADIES PROLIFERANTES
申请人:NOVARTIS AG
公开号:WO2005028444A1
公开(公告)日:2005-03-31
This invention relates to compounds of formula (I) wherein the variable substituents are described herein. The compounds are useful for the treatment of conditions and diseases characterized by an aberrant MAP kinase signaling pathway, such as cancer.