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Kv1.3抑制劑及其醫學應用
专利权人:
4SC DISCOVERY GMBH
发明人:
TASLER, STEFAN,塔斯勒 司提分,KRIMMELBEIN, ILGA,克立美柏因 伊加,塔斯勒 司提分,克立美柏因 伊加
申请号:
TW105107666
公开号:
TW201639857A
申请日:
2016.03.11
申请国别(地区):
TW
年份:
2016
代理人:
摘要:
The present invention relates to a compound of the general formula (III) or a salt, solvate or prodrug thereof, as well as medical uses involving them, wherein A1 is selected from the group consisting of N and C-R8; A2 is selected from the group consisting of N and C-R3; A3 is selected from the group consisting of N and C-R9; A4 and A5 and A6 are independently selected from the group consisting of N and C-R1; R1 is selected from the group consisting of hydrogen, (C1-C3)alkyl, halogen, (C1-C3)alkoxy and (C1-C3)haloalkyl; R2 is selected from the group consisting of hydrogen, halogen and (C1-C3)alkyl; R3 is selected from the group consisting of hydrogen, (C1-C3)alkyl, NR4R5, (C1-C3)alkyl-NR4R5 and cyano; wherein R4 and R5 are independently selected from the group consisting of hydrogen, (C3-C5)cycloalkyl, (C3-C5)heterocycloalkyl, (C1-C3)alkyl, or R4 and R5 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring optionally comprising in addition to the aforementioned nitrogen atom a further heteroatom group selected from the group consisting of O and NR6, wherein R6 is selected from the group consisting of hydrogen, methyl, acetyl and formyl; Y is selected from the group consisting of O and S; R7 is selected from the group consisting of hydrogen, and (C1-C3)alkyl; R8 is selected from the group consisting of (C1-C4)alkyl, (C3-C5)cycloalkyl, and (C3-C5)heterocycloalkyl; and R9 is selected from the group consisting of hydrogen, (C1-C3)alkyl, (C1-C3)alkoxy, and methods for producing such compounds.本發明涉及一種具有通式(III)之化合物或其鹽、溶劑化物或前藥,連同它們參與的醫學用途,其中A1選自由以下各項組成之群組:N和C-R8;A2選自由以下各項組成之群組:N和C-R3;A3選自由以下各項組成之群組:N和C-R9;A4和A5和A6獨立地選自由以下各項組成之群組:N和C-R1;R1選自由以下各項組成之群組:氫、(C1-C3)烷基、鹵素、(C1-C3)烷氧基以及(C1-C3)鹵代烷基;R2選自由以下各項組成之群組:氫、鹵素以及(C1-C3)烷基;R3選自由以下各項組成之群組:氫、(C1-C3)烷基、NR4R5、(C1-C3)烷基-NR4R5以及氰基;其中R4和R5獨立地選自由以下各項組成之群組:氫、(C3-C5)環烷基、(C3-C5)雜環烷基、(C1-C3)烷基,或者R4和R5與它們所附接的氮原子一起形成5員至7員雜環,該雜環除前述氮原子之外,還視情況包括另外的雜原子基團,該基團選自由以下各項組成之群組:O和NR6,其中R6選自由以下各項組成
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