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    Small molecule inducers of GDNF as potential new therapeutics for neuropsychiatric disorders
    1.
    发明授权
    Small molecule inducers of GDNF as potential new therapeutics for neuropsychiatric disorders 有权

    公开(公告)号：US09988377B2

    公开(公告)日：2018-06-05

    申请号：US14240681

    申请日：2012-08-24

    申请人： Dalibor Sames ,  Xiaoguang Li ,  Shu Li ,  Andrew Kruegel ,  Richard Karpowicz ,  Ignacio Carrera ,  Souvik Rakshit

    发明人： Dalibor Sames ,  Xiaoguang Li ,  Shu Li ,  Andrew Kruegel ,  Richard Karpowicz ,  Ignacio Carrera ,  Souvik Rakshit

    IPC分类号： C07D453/06

    CPC分类号： C07D453/06

    摘要： This invention provides a compound having the structure wherein A is a ring structure, with or without substitution; Z is present or absent and when present is wherein n is 0, 1, 2, 3, or 4; Y is —(CR11R12)—, —NH(CR11R12)—, or —O(CR11R12)—, wherein R11 and R12 are each hydrogen or combine to form a carbonyl; R1, R2, R3, R4, R5 and R6 are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester or amide; α represents a bond, which is present or absent and when α is present, then R7 and R8 are absent; R7 and R8 are present when α is absent and are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester, amide or R5 and R7 combine to form a carbonyl or R6 and R8 combine to form a carbonyl; R9 and R10 are each hydrogen or combine to form a carbonyl; and when α is present, Z is  where n=1, Y is —(CR11R12)— where R11 and R12 are H, A is unsubstituted indole attached at the 3-position of the indole, R3, R4, R5, R6, R9 and R10 are each H, and one of R1 or R2 is H, then the other one of R1 or R2 is other than H or ethyl, or a pharmaceutically acceptable salt, diastereomer, or enantiomer thereof.

    SMALL MOLECULE INDUCERS OF GDNF AS POTENTIAL NEW THERAPEUTICS FOR NEUROPSYCHIATRIC DISORDERS
    2.
    发明申请
    SMALL MOLECULE INDUCERS OF GDNF AS POTENTIAL NEW THERAPEUTICS FOR NEUROPSYCHIATRIC DISORDERS 有权
    GDNF的小分子诱导因子作为神经缺血性疾病的潜在新的治疗方法

    公开(公告)号：US20150056699A1

    公开(公告)日：2015-02-26

    申请号：US14240681

    申请日：2012-08-24

    申请人： Dalibor Sames ,  Xiaoguang Li ,  Shu Li ,  Andrew Kruegel ,  Richard Karpowicz ,  Ignacio Carrera ,  Souvik Rakshit

    发明人： Dalibor Sames ,  Xiaoguang Li ,  Shu Li ,  Andrew Kruegel ,  Richard Karpowicz ,  Ignacio Carrera ,  Souvik Rakshit

    IPC分类号： C07D453/06

    CPC分类号： C07D453/06

    摘要： This invention provides a compound having the structure wherein A is a ring structure, with or without substitution; Z is present or absent and when present is wherein n is 0, 1, 2, 3, or 4; Y is —(CR11R12)—, —NH(CR11R12)—, or —O(CR11R12)—, wherein R11 and R12 are each hydrogen or combine to form a carbonyl; R1, R2, R3, R4, R5 and R6 are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester or amide; α represents a bond, which is present or absent and when α is present, then R7 and R8 are absent; R7 and R8 are present when α is absent and are independently H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroaryl, hydroxyl, amino, ester, amide or R5 and R7 combine to form a carbonyl or R6 and R8 combine to form a carbonyl; R9 and R10 are each hydrogen or combine to form a carbonyl; and when α is present, Z is where n=1, Y is —(CR11R12)— where R11 and R12 are H, A is unsubstituted indole attached at the 3-position of the indole, R3, R4, R5, R6, R9 and R10 are each H, and one of R1 or R2 is H, then the other one of R1 or R2 is other than H or ethyl, or a pharmaceutically acceptable salt, diastereomer, or enantiomer thereof.

    摘要翻译： 本发明提供具有以下结构的化合物，其中A是具有或不具有取代的环结构; Z存在或不存在，并且当存在时，其中n为0,1,2,3或4; Y是 - （CR 11 R 12） - ， - NH（CR 11 R 12） - 或-O（CR 11 R 12） - ，其中R 11和R 12各自是氢或结合形成羰基; R 1，R 2，R 3，R 4，R 5和R 6独立地为H，取代或未取代的烷基，取代或未取代的芳基，取代或未取代的杂烷基，取代或未取代的杂芳基，羟基，氨基，酯或酰胺; α表示存在或不存在且当存在α时的键，则R7和R8不存在; 当α不存在时，R 7和R 8存在，并且独立地为H，取代或未取代的烷基，取代或未取代的芳基，取代或未取代的杂烷基，取代或未取代的杂烷基，羟基，氨基，酯，酰胺或R 5和R 7结合形成羰基 或R 6和R 8结合形成羰基; R9和R10各自为氢或结合形成羰基; 当存在α时，Z是其中n = 1，Y是 - （CR11R12） - 其中R11和R12是H，A是在吲哚3位上连接的未取代的吲哚，R3，R4，R5，R6，R9 和R 10各自为H，R 1或R 2中的一个为H，则R 1或R 2中的另一个为H或乙基，或其药学上可接受的盐，非对映异构体或对映异构体。