首页> 外国专利> USE OF COMPOUND BINDING TO MSIN3B THAT SPECIFICALLY BINDS TO NEURON RESTRICTIVE SILENCER FACTOR (NRSF)

USE OF COMPOUND BINDING TO MSIN3B THAT SPECIFICALLY BINDS TO NEURON RESTRICTIVE SILENCER FACTOR (NRSF)

机译:复合绑定到特定神经元沉默沉默因子(NRSF)的MSIN3B的使用

摘要

The present invention identifies a compound which binds to the PAH1 domain of mSin3B that specifically binds to neural restrictive silencer factor NRSF, and uses the compound as a prophylactic and/or a therapeutic for diseases associated with abnormal expression of neural restrictive silencer factor NRSF/REST or abnormal expression of genes targeted by NRSF/REST, such as Huntington's disease, medulloblastoma and neuropathic pain.;The present invention provides a pharmaceutical composition comprising a substance capable of binding to the PAH1 domain of mSin3B, e.g., a compound represented by the following formula (I), a pharmacologically acceptable salt thereof, or a pharmacologically acceptable ester thereof:; embedded image ;wherein n represents 0 or 1; R1, R2, R3, R4 and R5 each independently represent a hydrogen atom, a hydrocarbon group or a functional group; Y represents a single bond, a carbonyl group, —CONH—, —NHCO— or a sulfonyl group; and Z represents a nitrogen-containing heterocyclic group which may have a substituent, an amino group which may have a hydrocarbon group or an aromatic hydrocarbon group, or a nitrogen and oxygen-containing heterocyclic group which may have a substituent.
机译:本发明鉴定了与mSin3B的PAH1结构域结合的化合物,所述PAH1域特异性结合神经限制性沉默因子NRSF,并且将该化合物用作与神经限制性沉默因子NRSF / REST异常表达有关的疾病的预防和/或治疗剂。或由NRSF / REST靶向的基因的异常表达,例如亨廷顿氏病,髓母细胞瘤和神经性疼痛。;本发明提供了一种药物组合物,其包含能够与mSin3B的PAH1域结合的物质,例如以下所示的化合物式(I),其可药用盐或其可药用酯: “嵌入式图像” ;其中n代表0或1; R 1 ,R 2 ,R 3 ,R 4 和R 5 独立地表示氢原子,烃基或官能团; Y表示单键,羰基,-CONH-,-NHCO-或磺酰基; Z表示可以具有取代基的含氮杂环基,可以具有烃基或芳香族烃基的氨基或可以具有取代基的氮和氧杂环基。

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