Described herein are novel compounds that block the activity of LOX family members having good IC50 values, no cellular toxicity below 10 μM, induce sensitization of the cells to doxorubicin, strong activity in a recombinant LOX/LOXL2 activity, and a chemical structure that is drug-like and does not have a PAINS flag, as well as, methods of treatment using the compounds with respect to cancer, organ fibrosis, neurodegenerative and cardiovascular diseases.
Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives; and methods of treatment comprising administering such compounds and compositions.
Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt; ester and amide or derivatives; and methods of treatment comprising administering such compounds and compositions.
Tricyclicdicarboximides representatively prepared by the Diels-Alder condensation of a cyclic diene such as cycloheptatriene, cyclooctatetraene and the like with a dienophile such as substituted N-phenylmaleimide and the like are disclosed having pharmaceutical utility as minor tranquilizers and anti-convulsants. Also disclosed are processes for the preparation of such tricyclicdicarboximides; pharmaceutical compositions comprising such compounds and their salt, ester and amide derivatives; and methods of treatment comprising administering such compounds and compositions.
Monoazofarbstoffe, deren Herstellung und Verwendung
申请人:CIBA-GEIGY AG
公开号:EP0198796A2
公开(公告)日:1986-10-22
Die Monoazofarbstoffe der Formel
worin R, N-Aethylanilino oder durch C 2.5-Alkanoylamino substituiertes Anilino, R2 Wasserstoff oder C1-4-Alkyl und R3 Halogen oder C1-4-Alkyl ist, ergeben auf Polyamidfasermaterialien Färbungen und Drucke von guten Licht-und Nassechtheiten.
式中的单偶氮染料
其中 R 是 N-乙基苯胺基或被 C 2.5-烷酰氨基取代的苯胺基,R2 是氢或 C1-4-烷基,R3 是卤素或 C1-4 烷基,这些单偶氮染料和印花在聚酰胺纤维材料上具有良好的耐光牢度和耐湿牢度。