发明名称 3H-PHENOXAZINE DERIVATIVES SUITABLE AS NEAR-INFRARED IMAGINGAGENTS, PREPARATION AN USE THEREOF
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 th at 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 betwee n 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, carbox y, (C1-4)alkoxy carbonyl or (C1-4)alkoxy, or, when X is CH or CH2 then R1 and R 2 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, (C 1- 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 reactiv e group.
申请公布号 CA2535873(A1) 申请公布日期 2005.02.24
申请号 CA20042535873 申请日期 2004.08.17
申请人 NOVARTIS AG 发明人 KINZY, WILLY;HINTERSTEINER, MARTIN;KNEUER, RAINER;AUBERSON, YVES;GREMLICH, HANS-ULRICH
分类号 C07D498/22;A61K49/00;C07D498/14;C07D513/14;C07D513/22 主分类号 C07D498/22
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