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    Heteroaryl fused azapolycyclic compounds
    1.
    发明申请
    Heteroaryl fused azapolycyclic compounds 失效
    杂芳基稠合的氮杂多环化合物

    公开(公告)号：US20050020830A1

    公开(公告)日：2005-01-27

    申请号：US10889395

    申请日：2004-07-12

    申请人： Martin Allen ,  Jotham Coe ,  Spiros Liras ,  Christopher O'Donnell ,  Brian O'Neill

    发明人： Martin Allen ,  Jotham Coe ,  Spiros Liras ,  Christopher O'Donnell ,  Brian O'Neill

    IPC分类号： A61P25/34 ,  C07D471/08 ,  C07D498/08 ,  C07D487/14

    CPC分类号： C07D471/08

    摘要： The present invention provides a compound having the structure of formula I: wherein R1 is hydrogen, (C1-C6) alkyl, unconjugated (C3-C6) alkenyl, benzyl, YC(═O)(C1-C6) alkyl or —CH2CH2—O—(C1-C4) alkyl; X is CH2 or CH2CH2; Y is (C2-C6) alkylene; Z is (CH2)m, CF2, or C(═O), where m is 0, 1 or 2; R2 and R3 are selected independently from hydrogen, halogen, —(C1-C6) alkyl optionally substituted with from 1 to 7 halogen atoms, and —O(C1-C6) alkyl optionally substituted with from 1 to 7 halogen atoms, or R2 and R3 each together with the atom to which it is connected independently form C(═O), S→O, S(═O)2, or N→O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.

    摘要翻译： 本发明提供具有式I结构的化合物：其中R 1是氢，（C 1 -C 6）烷基，未结合的（C 3 -C 6）烯基，苄基，YC（= O）（C 1 -C 6）烷基或 -CH 2 CH 2 -O-（C 1 -C 4）烷基; X是CH 2或CH 2 CH 2; Y是（C 2 -C 6）亚烷基; Z是（CH 2）m，CF 2或C（= O），其中m是0,1或2; R 2和R 3独立地选自氢，卤素，任选被1至7个卤素原子取代的 - （C 1 -C 6）烷基和任选被1至7个取代的-O（C 1 -C 6）烷基 卤素原子或R 2和R 3各自与其连接的原子一起独立地形成C（= O），S-> O，S（= O）2或N-> O; 吡啶基，吡唑基，三唑基，吡嗪基，呋喃基，噻吩基，异恶唑基，噻唑基，恶唑基，异噻唑基，吡咯基，噌啉基，三嗪基，恶二唑基， 噻二唑基和呋咱基。

    4-Phenyl-piperidine compounds and their use as modulators of opioid receptors
    2.
    发明申请
    4-Phenyl-piperidine compounds and their use as modulators of opioid receptors 审中-公开
    4-苯基哌啶化合物及其作为阿片受体调节剂的用途

    公开(公告)号：US20050032837A1

    公开(公告)日：2005-02-10

    申请号：US10823026

    申请日：2004-04-13

    申请人： Stanton McHardy ,  Spiros Liras ,  Sara Guediche ,  Jotham Coe

    发明人： Stanton McHardy ,  Spiros Liras ,  Sara Guediche ,  Jotham Coe

    IPC分类号： A61K31/445 ,  A61P25/00 ,  C07D211/32 ,  C07D211/34 ,  C07D211/54 ,  C07D401/06 ,  C07D405/12 ,  C07D471/04

    CPC分类号： C07D211/34 ,  C07D401/06 ,  C07D405/12 ,  C07D471/04

    摘要： The subject invention relates to 4-phenyl-piperidine derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by an opioid receptor. The subject also particularly relates to using such derivatives to treat certain disease states, disorders and conditions, for example irritable bowel syndrome, drug addiction or dependency, including alcohol addiction, depression, anxiety, schizophrenia, anxiety, schizophrenia and eating disorders, among numerous other disease states, disorders and conditions as more fully described herein.

    摘要翻译： 本发明涉及4-苯基哌啶衍生物，包含这些衍生物的药物组合物和使用这些衍生物治疗由阿片受体介导的疾病状态，病症和病症的方法。 该专题还特别涉及使用这样的衍生物治疗某些疾病状态，病症和病症，例如肠易激综合征，药物成瘾或依赖性，包括酒精成瘾，抑郁，焦虑，精神分裂症，焦虑，精神分裂症和进食障碍 疾病状态，障碍和病症，如本文中更全面地描述的。

    Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline
    5.
    发明申请
    Tetrahydroisoquinolinyl derivatives of quinazoline and isoquinoline 失效
    喹唑啉和异喹啉的四氢异喹啉衍生物

    公开(公告)号：US20050182079A1

    公开(公告)日：2005-08-18

    申请号：US11062133

    申请日：2005-02-18

    申请人： Martin Allen ,  Thomas Chappie ,  John Humphrey ,  Spiros Liras

    发明人： Martin Allen ,  Thomas Chappie ,  John Humphrey ,  Spiros Liras

    IPC分类号： C07D401/04 ,  C07D491/04 ,  A61K31/517 ,  C07D43/02

    CPC分类号： C07D401/04 ,  C07D491/04

    摘要： The invention pertains to substituted quinazoline and isoquinoline compounds that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE-10. The invention also relates to intermediates for preparation of said compounds; pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.

    摘要翻译： 本发明涉及用作有效磷酸二酯酶（PDE）抑制剂的取代喹唑啉和异喹啉化合物。 特别地，本发明涉及作为PDE-10的选择性抑制剂的所述化合物。 本发明还涉及制备所述化合物的中间体; 包含所述化合物的药物组合物; 以及所述化合物在治疗某些中枢神经系统（CNS）或其它疾病的方法中的用途。

    Heteroaryl fused azapolycyclic compounds
    6.
    发明授权
    Heteroaryl fused azapolycyclic compounds 失效
    杂芳基稠合的氮杂多环化合物

    公开(公告)号：US07456177B2

    公开(公告)日：2008-11-25

    申请号：US10889395

    申请日：2004-07-12

    申请人： Martin P. Allen ,  Jotham W. Coe ,  Spiros Liras ,  Christopher J. O'Donnell ,  Brian T. O'Neill

    发明人： Martin P. Allen ,  Jotham W. Coe ,  Spiros Liras ,  Christopher J. O'Donnell ,  Brian T. O'Neill

    IPC分类号： A61K31/502 ,  C07D471/02

    CPC分类号： C07D471/08

    摘要： The present invention provides a compound having the structure of formula I: wherein R1 is hydrogen, (C1–C6) alkyl, unconjugated (C3–C6) alkenyl, benzyl, YC(═O)(C1–C6) alkyl or —CH2CH2—O—(C1–C4) alkyl; X is CH2 or CH2CH2; Y is (C2–C6) alkylene; Z is (CH2)m, CF2, or C(═O), where m is 0, 1 or 2; R2 and R3 are selected independently from hydrogen, halogen, —(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, and —O(C1–C6) alkyl optionally substituted with from 1 to 7 halogen atoms, or R2 and R3 each together with the atom to which it is connected independently form C(═O), S→O, S(═O)2, or N→O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.

    摘要翻译： 本发明提供具有式I结构的化合物：其中R 1是氢，（C 1 -C 6 -C 6）烷基，未缀合的 （C 3 -C 6）烯基，苄基，YC（-O）（C 1 -C 6 - ）烷基或-CH 2 CH 2 -O-（C 1 -C 4 - ）烷基; X是CH 2或CH 2 CH 2 CH 2; Y是（C 2 -C 6 -C 6）亚烷基; Z是（CH 2）2，CH 2或C（-O），其中m是0,1或2; R 2和R 3独立地选自氢，卤素， - （C 1 -C 6 -C 6）烷基 或任选被1至7个卤素原子取代的-O（C 1 -C 6 -C 6）烷基，或任选被1至7个卤素原子取代的-O（C 1 -C 6 -C 6）烷基， 2和R 3各自与其连接的原子一起独立地形成C（-O），S-> O，S（-O）2 或N-> O; 吡啶基，吡唑基，三唑基，吡嗪基，呋喃基，噻吩基，异恶唑基，噻唑基，恶唑基，异噻唑基，吡咯基，噌啉基，三嗪基，恶二唑基， 噻二唑基和呋咱基。