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1,2,4-trinitrotoluene 2,4,5-tritin
专利权人:
BAYER PHARMA AKTIENGESELLSCHAFT;BAYER AKTIENGESELLSCHAFT;THE BROAD INSTITUTE, INC.;PRESIDENT AND FELLOWS OF HARVARD COLLEGE;THE GENERAL HOSPITAL CORPORATION
发明人:
GRADL, Stefan Nikolaus,NGUYEN, Duy,EIS, Knut,GUNTHER, Judith,STELLFELD, Timo,JANZER, Andreas,CHRISTIAN, Sven,MULLER, Thomas,SHEIKH, Sherif El,LIU, Kery,KROBER, Michael,MERZ, Claudia,NIEHUES, Michael,Z
申请号:
PE2019000896
公开号:
PE20191005A1
申请日:
2017.10.25
申请国别(地区):
PE
年份:
2019
代理人:
摘要:
A formula compound (I),characterized in that R1 is C5-C8 alkyl, C2-C8 haloalkyl, C4-C8 cycloalkyl, among others; R2 H, or halogen; R3 is C1-C6 alkyl; C3-C8 cycloalkyl, C1-C6 haloalkyl, among others; R4 optionally substituted C1-C6 alkyl, C3-C8 cycloalkyl or phenyl; R5 is halogen, C1-C6 alkyl, among others. 1,2,4-TRIAZOLONS are 2,4,5-trisubstituted compounds that inhibit dihydroorotate dehydrogenase (DHODH);A selected compound is 5-fluoro-4 - [3-methyl-5-oxo-4 - (propane-2-il) - 4,5-dihydro-1h-1,2,4-triazol-1-il] - N - (2-methylphenyl) - 2 - [2 (2S) - 1,1-trifluoropropane-2-il] oxygen. It also refers to the preparation method of these compounds, the effective intermediate compounds used to prepare these compounds, including the pharmacological synthesis and combination of these compounds, and the use of these compounds as a single preparation or mixing with other active ingredients, It is used to treat or prevent diseases, especially high spread diseases such as cancer.Referido a un compuesto de formula (I), caracterizado porque R1 es alquiloC5-C8, haloalquiloC2-C8, cicloalquilo C4-C8, entre otros; R2 H, o halogeno; R3 es alquilo C1-C6; cicloalquiloC3-C8, haloalquilo C1-C6, entre otros; R4 alquilo C1-C6 opcionalmente sustituido, cicloalquilo C3-C8 o fenilo; R5 es halogeno, alquilo C1-C6, ente otros. Son compuestos 1,2,4-TRIAZOLONAS 2,4,5-trisustituidas que inhiben la dihidroorotato deshidrogenasa (DHODH); un compuesto seleccionado es 5-fluoro-4-[3-metil-5-oxo-4-(propan-2-il)-4,5-dihidro-1H-1,2,4-triazol-1-il]-N-(2-metilfenil)-2-{[(2S)-1,1,1-trifluoropropan-2-il]oxi}benzamida. Tambien se refiere a metodos de preparacion de dichos compuestos, compuestos intermedios utiles para preparar dichos compuestos, composiciones farmaceuticas y combinaciones que comprenden dichos compuestos y el uso de dichos compuestos para preparar composiciones farmaceuticas como un unico agente o en combinacion con otros ingredientes activos, para el tratamiento o la profilaxis de enfermedade
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

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