发明公开
- 专利标题: 3H-PHENOXAZINE DERIVATIVES SUITABLE AS NEAR-INFRARED IMAGING AGENTS, PREPARATION AN USE THEREOF
- 专利标题(中): AS合适的近红外3H-嗪,生产和使用的手段
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申请号: EP04764213.7申请日: 2004-08-17
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公开(公告)号: EP1658294A1公开(公告)日: 2006-05-24
- 发明人: AUBERSON, Yves , GREMLICH, Hans-Ulrich , HINTERSTEINER, Martin , KINZY, Willy , KNEUER, Rainer
- 申请人: Novartis AG , Novartis Pharma GmbH
- 申请人地址: Lichtstrasse 35 4056 Basel CH
- 专利权人: Novartis AG,Novartis Pharma GmbH
- 当前专利权人: Novartis AG,Novartis Pharma GmbH
- 当前专利权人地址: Lichtstrasse 35 4056 Basel CH
- 代理机构: Roth, Peter Richard
- 优先权: US495921P 20030818
- 国际公布: WO2005016934 20050224
- 主分类号: C07D498/22
- IPC分类号: C07D498/22 ; C07D513/22 ; A61K49/00
摘要:
The present invention provides compounds of formula (I) wherein X and Y represent CH, CH2 or a divalent or trivalent heteroatom under the proviso that X and Y are not simultaneously CH or CH2; m and o represent independently of each other 0 or 1, with the proviso that if m is 0 then the dotted line between Y and the neighboring C atom represents a bond and Y is CH or a trivalent heteroatom, if m is 1 then the dotted line between Y and the neighboring C atom is absent and Y is CH2 or a divalent heteroatom, if o is 0 then the dotted line between X and the neighboring C atom represents a bond and X is CH or a trivalent heteroatom, if o is 1 then the dotted line between X and the neighboring C atom is absent and X is CH2 or a divalent heteroatom; A represents (CH3CR4)p and Q represents (CR9R10)n; n and p represent independently of each other 0 or 1; R6, R7, R13 and R14 denote independently of each other hydrogen, halogen, (C1-4)alkyl, (C1-4)alkylSO2, SO3H, carboxy, (C1-4)alkoxy carbonyl, (C1-4)alkoxy, OH or NR15R16; R1, R2, R3, R4, R9, R10, R11 and R12 denote independently of each other hydrogen, (C1-4)alkyl, carboxy, (C1-4)alkoxy carbonyl or (C1-4)alkoxy, or, when X is CH or CH2 then R1 and R2 can also be OH or NR15R16, or when Y is CH or CH2 then R11, R12 can also be OH or NR15R16; R5, R8, R15 and R16 are independently of each other hydrogen, (C1-4)alkyl, (C1-4)alkoxy, R17O-C(O)-(C1-4)alkyl or (reactive group)-(C1-4)alkyl; and R17 represents hydrogen or (C1-4)alkyl; compositions comprising such compounds, a process for the production of such compounds of formula (I), a method of labeling target structures, especially amyloid plaques, in the brain, a method for identifying Alzheimer's disease, use of a compound of formula I as a near-infrared imaging agent and a conjugate comprising a compound of formula (I) covalently linked to a biomolecule through a reactive group.
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