- 专利标题： NOVEL COMPOUNDS FOR THE DIAGNOSIS, TREATMENT AND PREVENTION OF DISEASES ASSOCIATED WITH THE AGGREGATION OF ALPHA-SYNUCLEIN
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申请号： EP24166495.2申请日： 2020-11-19
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公开(公告)号： EP4368184A3公开(公告)日： 2024-07-31
- 发明人: GIESE, Armin , SCHMIDT, Felix , WECKBECKER, Daniel , LEONOV, Andrei , RYAZANOV, Sergey , GRIESINGER, Christian , PICHLER, Bernd , HERFERT, Kristina , MAURER, Andreas , KÜBLER, Laura , BUSS, Sabrina
- 申请人： Modag GmbH , Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
- 申请人地址： DE 55234 Wendelsheim Mikroforum Ring 3
- 专利权人： Modag GmbH,Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
- 当前专利权人： Modag GmbH,Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
- 当前专利权人地址： DE 55234 Wendelsheim Mikroforum Ring 3
- 代理机构： Vossius & Partner Patentanwälte Rechtsanwälte mbB
- 优先权： EP 210073 2019.11.19
- 分案原申请号： 20810960.3 2020.11.19
- 主分类号： C07D401/04
- IPC分类号： C07D401/04 ; C07D401/14 ; C07D403/04 ; C07D405/14 ; A61P25/16 ; A61P25/28 ; A61K31/4439 ; A61K31/444 ; A61K31/506
摘要：
The present invention relates to a compound represented by the general formula Ila or IIb
or a solvate or salt thereof, wherein
is selected from
and
is selected from
Y1, Y2, Y3, Y4, Y5, Y6, Y7 and Y8 are independently selected from CR3 and N, with the proviso that at least one of Y1, Y2, Y3, Y4, Y5, Y6, Y7 and Y8 is N and with the proviso that in the formulae la or Ib, at least one of Y1, Y3, Y4, and Y6 is N; R1 is independently selected from hydrogen, C1-4 alkyl and -(CH2)-O-P(=O)(OR)(OR), wherein C1-4 alkyl can be optionally substituted by one or more halogen; R2 is independently selected from hydrogen, halogen, and C1-4 alkyl, wherein C1-4 alkyl can be optionally substituted by one or more halogen; R is hydrogen or a cation; R3 is hydrogen; R4 and R5 are independently selected from H and C1-4 alkyl, wherein C1-4 alkyl can be optionally substituted by one or more halogen or wherein R4 and R5 together with the nitrogen atom to which they are bound form a piperazinyl ring which is substituted by one or more R6; and R6 is independently selected from halogen, C1-4 alkyl, OH and C1-4 alkoxy, wherein C1-4 alkyl and C1-4 alkoxy can be optionally substituted by one or more halogen; and Hal is halogen.
or a solvate or salt thereof, wherein
is selected from
and
is selected from
Y1, Y2, Y3, Y4, Y5, Y6, Y7 and Y8 are independently selected from CR3 and N, with the proviso that at least one of Y1, Y2, Y3, Y4, Y5, Y6, Y7 and Y8 is N and with the proviso that in the formulae la or Ib, at least one of Y1, Y3, Y4, and Y6 is N; R1 is independently selected from hydrogen, C1-4 alkyl and -(CH2)-O-P(=O)(OR)(OR), wherein C1-4 alkyl can be optionally substituted by one or more halogen; R2 is independently selected from hydrogen, halogen, and C1-4 alkyl, wherein C1-4 alkyl can be optionally substituted by one or more halogen; R is hydrogen or a cation; R3 is hydrogen; R4 and R5 are independently selected from H and C1-4 alkyl, wherein C1-4 alkyl can be optionally substituted by one or more halogen or wherein R4 and R5 together with the nitrogen atom to which they are bound form a piperazinyl ring which is substituted by one or more R6; and R6 is independently selected from halogen, C1-4 alkyl, OH and C1-4 alkoxy, wherein C1-4 alkyl and C1-4 alkoxy can be optionally substituted by one or more halogen; and Hal is halogen.
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