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    Certain alkylene diamine-substituted heterocycles
    7.
    发明授权
    Certain alkylene diamine-substituted heterocycles 失效
    某些亚烷基二胺取代的杂环

    公开(公告)号：US06696445B2

    公开(公告)日：2004-02-24

    申请号：US10291446

    申请日：2002-11-08

    申请人： Raymond F. Horvath ,  Jennifer N Tran ,  Stéphane De Lombaert ,  Kevin J. Hodgetts ,  Philip A. Carpino ,  David A. Griffith

    发明人： Raymond F. Horvath ,  Jennifer N Tran ,  Stéphane De Lombaert ,  Kevin J. Hodgetts ,  Philip A. Carpino ,  David A. Griffith

    IPC分类号： C07D40112

    CPC分类号： C07D213/73 ,  C07D215/46 ,  C07D239/48 ,  C07D471/04 ,  C07D471/14 ,  C07D473/34 ,  C07D475/08 ,  C07D487/04 ,  C07D495/04 ,  G01N2333/5755 ,  G01N2333/70571

    摘要： The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR14; W is S, O, or NR15; Y is N or CR3; E, F, and G are each, independently, CR3 or N; I and J are each, independently, C═O, S, O, CR3R16 or NR15 when single bonded to both adjacent ring atoms, or N, or CR3 when double bonded to an adjacent ring atom; K is N or CR3 when double bonded to L or J, or O, S, C═O, CR3R16, or NR15 when single bonded to both adjacent ring atoms, or N or CR3 when double bonded to an adjacent ring atom; L is N or CR16 when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; The 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C═O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR15. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.

    摘要翻译： 本发明还提供了通用方法，其中单环，双环或三环杂环可以被修饰以在NPY1受体上获得有效的拮抗剂。本发明提供NPY受体的新型有效的非肽拮抗剂，特别是 NPY1受体由选自单，双或三环杂环核心设计。本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。包含的新化合物 通过本发明是式I-XV的那些，其中X是N或CR 14; W是S，O或NR 15; Y是N或CR 3; E，F和G各自独立地为CR 3或N; 当单键结合到两个相邻的环原子上时，I和J各自独立地为C = O，S，O，CR 3 R 16或NR 15，当双键键合到 相邻的环原子;当双键连接到L或J或O，S，C = O，CR 3 R 16或NR 15时，K是N或CR 3。 当与相邻的环原子双键键合时，N或CR 3，当与其连接的所有原子单键键合时，L是N或CR 16，或当双键键合到K时，C（碳）; 含有I，J，K和L的6-或7-元环可以含有1至3个双键，0至2个杂原子和0至2个C = O基团，其中这些基团的碳原子 是环的一部分，氧原子是环上的取代基; Q是O或NR 15。这些化合物抑制神经肽Y在那些受体上的活性可用于治疗与过量神经肽Y相关的生理障碍， 包括进食障碍，例如肥胖和贪食症，以及某些心脏病 高血压等疾病。

    Certain alkylene diamine-substituted heterocycles
    9.
    发明授权
    Certain alkylene diamine-substituted heterocycles 失效
    某些亚烷基二胺取代的杂环

    公开(公告)号：US06506762B1

    公开(公告)日：2003-01-14

    申请号：US09676941

    申请日：2000-09-29

    申请人： Raymond F. Horvath ,  Jennifer Tran ,  Stéphane De Lombaert ,  Kevin J. Hodgetts ,  Philip A. Carpino ,  David A. Griffith

    发明人： Raymond F. Horvath ,  Jennifer Tran ,  Stéphane De Lombaert ,  Kevin J. Hodgetts ,  Philip A. Carpino ,  David A. Griffith

    IPC分类号： C07D48704

    CPC分类号： C07D213/73 ,  C07D215/46 ,  C07D239/48 ,  C07D471/04 ,  C07D471/14 ,  C07D473/34 ,  C07D475/08 ,  C07D487/04 ,  C07D495/04 ,  G01N2333/5755 ,  G01N2333/70571

    摘要： The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV. wherein X is N or CR14; W is S, O, or NR15; Y is N or CR3; E, F, and G are each, independently, CR3 or N; I and J are each, independently, C═O, S, O, CR3R16 or NR15 when single bonded to both adjacent ring atoms, or N, or CR3 when double bonded to an adjacent ring atom; K is N or CR3 when double bonded to L or J, or O, S, C═O, CR3R16, or NR15 when single bonded to both adjacent ring atoms, or N or CR3 when double bonded to an adjacent ring atom; L is N or CR16 when single bonded to all atoms to which it is attached, or C (carbon) when double bonded to K; the 6- or 7-membered ring that contains I, J, K, and L may contain from 1 to 3 double bonds, from 0 to 2 heteroatoms, and from 0 to 2 C═O groups, wherein the carbon atom of such groups are part of the ring and the oxygen atom is a substituent on the ring; Q is O or NR15. Such compounds inhibit the activity of neuropeptide Y at those receptors are useful in treating physiological disorders associated with an excess of neuropeptide Y, including eating disorders, such as, for example, obesity and bulimia, and certain cardiovascular diseases, for example, hypertension.

    摘要翻译： 本发明还提供了通用方法，其中单环，双环或三环杂环可以被修饰以在NPY1受体上获得有效的拮抗剂。本发明提供NPY受体的新型有效的非肽拮抗剂，特别是 NPY1受体由选自单，双或三环杂环核心设计。本发明涉及用于治疗与过量神经肽Y相关的生理紊乱的新化合物，组合物和方法。包含的新化合物 本发明是式I-XV的那些，其中X是N或CR 14; W是S，O或NR15; Y为N或CR 3; E，F和G各自独立地为CR 3或N; 当双键连接到相邻的环原子时，当单键连接到两个相邻的环原子，或N或CR 3时，I和J各自独立地为C = O，S，O，CR 3 R 16或NR 15;当双键键合时，K为N或CR 3 当与两个相邻的环原子单键键合时，或当与相邻环原子双键键合时为N或CR 3，L或J，或O，S，C = O，CR 3 R 16或NR 15;当单键连接到所有相邻环原子时，L为N或CR16 当与K键合时，其连接的原子或C（碳）;含有I，J，K和L的6-或7-元环可以含有1至3个双键，0至2个杂原子 和0〜2个C = O基团，其中这些基团的碳原子是环的一部分，氧原子是环上的取代基; Q是O或NR15。这些化合物抑制神经肽Y在这些受体上的活性可用于治疗与过量神经肽Y相关的生理紊乱，包括进食障碍，例如肥胖症和贪食症，以及某些心血管疾病， 例如高血压。