MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
发明人:
HANS DR. BUCHSTALLER,DIETER PETER - DR. DIPL.-CHEM. DORSCH
申请号：
ARP130103430
公开号：
AR092670A1
申请日:
2013.09.25
申请国别(地区):
AR
年份:
2015
代理人:
摘要：
These compounds are inhibitors of tankilase and can be used, among other things, in the treatment of cancer, cardiovascular disease, central nervous system injury and various flammable forms.R2 represents each independent,h. R: H, F, Cl, ch8323u och83323；X1,X2 stands for each individual,CH or N； And denotes A, Cyc or oxyranyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, piperazinyl, piperidinyl, morpholinyl, pyrrolidinyl, thiomorpholinyl or diazepanyl, which may not be substituted or may be mono- or disubstituted with = O, Hal, OH and / or A ； A denotes unbranched or branched C₁₋₄ alkyl, wherein a CH₂ group may be replaced by an O atom and / or an H atom may be replaced by OH； A denotes unbranched or branched C₂₋₁₀ alkyl, wherein two adjacent carbon atoms may form a double bond and / or one or two non-adjacent CH and / or CH₂ groups may be replaced by N atoms,O and / or s, where 1-7 atoms of H can be replaced by F, Cl and / or Oh； CYC is cyclo-c83231；Not replaced or only replaced by Oh, Hal or a； Hal means F, Cl, Br or I； provided that there is at least one R1,R2,R³ is not H, and provided that Y is not 4-isopropyl-1-piperazinyl, and its pharmaceutically acceptable salts, tautomers and stereoisomers, including mixtures thereof in all proportions.Los compuestos son inhibidores de Tankirasa y se pueden emplear, inter alia, para el tratamiento de enfermedades tales como cáncer, enfermedades cardiovasculares, lesión del sistema nervioso central y diferentes formas de inflamación. Reivindicación 1: Compuestos de la fórmula (1) en donde: R¹, R² denotan cada uno, de modo independiente entre sí, H, F o Cl； R³ denota H, F, Cl, CH₃ u OCH₃； X¹, X² denotan cada uno, de modo independiente entre sí, CH o N； Y denota A, Cyc u oxiranilo, oxetanilo, tetrahidrofuranilo, tetrahidropiranilo, piperazinilo, piperidinilo, morfolinilo, pirrolidinilo, tiomorfolinilo o diazepanilo, que puede no estar sustituido o que puede estar mono- o disustituido con =O, Hal, OH y/o A； A denota alqui
