4-Phenyl-piperidine compounds and their use as modulators of opioid receptors
    1.
    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

    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。

    Heteroaryl fused azapolycyclic compounds
    2.
    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

    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。

    3-Azabicyclo[3.1.0]hexane derivatives
    3.
    发明申请
    3-Azabicyclo[3.1.0]hexane derivatives 审中-公开
    3-氮杂双环[3.1.0]己烷衍生物

    公开(公告)号:US20070054950A1

    公开(公告)日:2007-03-08

    申请号:US11366903

    申请日:2006-03-01

    摘要: The subject invention provides a compound of the formula 1, wherein X, Q, n, R1, R2, R3, R4, R5 R6, R7, R8, R9, and R10 are as defined. Compounds of formula I have activity as opioid receptor antagonists. The subject invention furthermore provides for pharmaceutical compositions and therapeutic methods comprising compounds of formula I.

    摘要翻译: 本发明提供式1化合物,其中X,Q,n,R 1,R 2,R 3,R 3, SUP 4,R 5,R 6,R 7,R 8,R SUP, > 9 ,并且R 10定义如上。 式I化合物具有作为阿片受体拮抗剂的活性。 本发明还提供包含式I化合物的药物组合物和治疗方法。

    Heteroaryl fused azapolycyclic compounds
    5.
    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

    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。