[EN] KV1.3 INHIBITORS AND THEIR MEDICAL APPLICATION<br/>[FR] INHIBITEURS DE KV1.3 ET LEUR APPLICATION MÉDICALE
申请人:4SC DISCOVERY GMBH
公开号:WO2016146583A1
公开(公告)日:2016-09-22
The present invention relates to a compound of the general formula (II) or a salt or solvate 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 and (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; 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 and (C1-C3)alkoxy; wherein certain particular compounds are excluded py proviso, and methods for producing such compounds.
本发明涉及一般式(II)的化合物或其盐或溶剂络合物,以及涉及它们的医药用途,其中A1从N和C-R8组成的组中选择;A2从N和C-R3组成的组中选择,A3从N和C-R9组成的组中选择;A4、A5和A6独立地从N和C-R1组成的组中选择;R1从氢、(C1-C3)烷基、卤素、(C1-C3)烷氧基和(C1-C3)卤代烷基组成的组中选择;R2从氢、卤素和(C1-C3)烷基组成的组中选择;R3从氢、(C1-C3)烷基、NR4R5、(C1-C3)烷基-NR4R5和氰基组成的组中选择,其中R4和R5独立地从氢、(C3-C5)环烷基、(C3-C5)杂环烷基和(C1-C3)烷基组成的组中选择,或者R4和R5与它们连接的氮原子一起形成一个5至7元杂环,该环可选地包括除上述氮原子外进一步选择的O和NR6等杂原子基团,其中R6从氢、甲基、乙酰基和甲酰基组成的组中选择;Y从O和S组成的组中选择;R8从(C1-C4)烷基、(C3-C5)环烷基和(C3-C5)杂环烷基组成的组中选择;R9从氢、(C1-C3)烷基和(C1-C3)烷氧基组成的组中选择;其中特定的某些化合物受限制,以及生产这种化合物的方法。