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    OXAZOLE OREXIN RECEPTOR ANTAGONISTS
    2.
    发明申请
    OXAZOLE OREXIN RECEPTOR ANTAGONISTS 审中-公开

    公开(公告)号：US20170320865A1

    公开(公告)日：2017-11-09

    申请号：US15523247

    申请日：2015-10-27

    申请人： SCOTT D. KUDUK ,  NIGEL LIVERTON ,  YUNFU LUO

    发明人： SCOTT D. KUDUK ,  NIGEL LIVERTON ,  YUNFU LUO

    IPC分类号： C07D413/14 ,  C07D413/12 ,  C07D263/32

    CPC分类号： C07D413/14 ,  C07D263/32 ,  C07D413/12

    摘要： The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.

    Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors.
    5.
    发明申请
    Tricyclic Compounds as Allosteric Modulators of Metabotropic Glutamate Receptors. 审中-公开
    三环化合物作为代谢型谷氨酸受体的变构调节剂。

    公开(公告)号：US20130210807A1

    公开(公告)日：2013-08-15

    申请号：US13809579

    申请日：2011-07-09

    申请人： Nigel J Liverton ,  Christelle Boléa ,  Sylvain Celanire ,  Yunfu Luo

    发明人： Nigel J Liverton ,  Christelle Boléa ,  Sylvain Celanire ,  Yunfu Luo

    IPC分类号： C07D513/04 ,  A61K45/06 ,  A61K31/55 ,  A61K31/433 ,  C07D513/14 ,  A61K31/506

    CPC分类号： C07D513/04 ,  A61K31/433 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D513/14

    摘要： The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3′ are —H or methyl, or R3 and R3 taken together form a double bond, or R3′ is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.

    摘要翻译： 本发明描述并要求结构式I，结构式II或结构式III的化合物：其中R1，R2，R3和R3'是-H或甲基，或R3和R3一起形成双键，或R3 '是-H并且R 2和R 3一起形成螺环丙基取代基，R 4是-H或-F，且R 5是-H，甲基，-C 1或-Br，其中R 1是-H，乙基， 异丙基 - ，环丙基 - ，甲基或甲氧基 - ，R 4为-H或-F，“Y”为：（a）-CH 2 - ; （b）-CR6H-0-CR7R8-，其中R6，R7和R8独立地是-H或甲基; （c）-CR 6 H-N（R 9）-CR 7 R 8 - ，其中R 6，R 7和R 8独立地为-H或甲基; （d）-CH 2 -C（R 9）（R 10）-C（R 7）（R 8） - ，其中R 7，R 8，R 9和R 10独立地为-H或 - 甲基，或者R 7和R 8均为-F，R 9和 R 10独立地是-H或 - 甲基，或者R 9和R 10都是-F，或者R 9和R 10一起是（0 =），它们与它们所连接的碳一起形成羰基。