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    Novel Compounds
    1.
    发明申请
    Novel Compounds 失效
    新型化合物

    公开(公告)号：US20070270435A1

    公开(公告)日：2007-11-22

    申请号：US11743824

    申请日：2007-05-03

    申请人： William Brown ,  Christopher Walpole ,  Niklas Plobeck ,  Thomas Hudzik

    发明人： William Brown ,  Christopher Walpole ,  Niklas Plobeck ,  Thomas Hudzik

    IPC分类号： A61K31/496 ,  A61P25/24 ,  A61P43/00 ,  C07D295/00

    CPC分类号： C07D295/155 ,  C07D233/24 ,  C07D307/52 ,  C07D333/20

    摘要： The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof, at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.

    摘要翻译： 本发明涉及至少一种通式I的化合物，其中R 1是苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基或吡啶N-氧化物，其中每个R 0 > 1苯基和R 1 - 杂芳环可以任选地和独立地被1,2或3个选自CF 3，甲基，碘，溴， 氟和氯; R 2独立地选自乙基和异丙基; R 3是氢或氟; R 4是-NH 2或-NHSO 2 R 5; 和R 5是氢，-CF 3或C 1 -C 6烷基，或其药学上可接受的盐 至少一种根据式I制备至少一种化合物的方法; 用至少一种根据式I的化合物治疗至少一种δ受体相关病症的方法; 和包含至少一种根据式I的化合物的至少一种药物组合物。

    Hydroxyphenyl-piperazinyl-methyl-benzamide derivatives for the treatment of pain
    2.
    发明授权
    Hydroxyphenyl-piperazinyl-methyl-benzamide derivatives for the treatment of pain 失效
    羟苯基 - 哌嗪基 - 甲基 - 苯甲酰胺衍生物用于治疗疼痛

    公开(公告)号：US06696447B2

    公开(公告)日：2004-02-24

    申请号：US10240037

    申请日：2002-09-27

    申请人： William Brown ,  Niklas Plobeck ,  Christopher Walpole

    发明人： William Brown ,  Niklas Plobeck ,  Christopher Walpole

    IPC分类号： A61K31496

    CPC分类号： C07D295/155 ,  C07D307/52 ,  C07D333/20

    摘要： The present application describes compounds of general formula I where R1 is selected from any one of pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; and where each R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the heteroaromatic ring may take place in any position on the ring system. The invention also includes enantiomers, salts and pharmaceutical compositions containing the compounds. The compounds may be used in treating patients for pain.

    摘要翻译： 本申请描述了通式I的化合物，其中R 1选自吡啶基，噻吩基，呋喃基，咪唑基和三唑基中的任一个;并且其中每个R 1杂芳环可以任选和独立地被1,2取代 或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基。 杂芳环上的取代可以在环系统上的任何位置进行。 本发明还包括含有这些化合物的对映异构体，盐和药物组合物。 该化合物可用于治疗患者的疼痛。

    Compounds
    4.
    发明授权
    Compounds 失效
    化合物

    公开(公告)号：US07915413B2

    公开(公告)日：2011-03-29

    申请号：US11743824

    申请日：2007-05-03

    申请人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    发明人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    IPC分类号： C07D295/155 ,  C07D233/64 ,  C07D333/20 ,  C07D307/52

    CPC分类号： C07D295/155 ,  C07D233/24 ,  C07D307/52 ,  C07D333/20

    摘要： The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof, at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.

    摘要翻译： 本发明涉及至少一种通式I的化合物，其中R 1是苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基或吡啶N-氧化物，其中每个R 1苯基和R 1杂芳环可任选地和独立地是 被1,2或3个选自CF 3，甲基，碘，溴，氟和氯的取代基取代; R2独立地选自乙基和异丙基; R3是氢或氟; R4是-NH2或-NHSO2R5; 和R 5是氢，-CF 3或C 1 -C 6烷基或其药学上可接受的盐，至少一种用于制备至少一种根据式I的化合物的方法; 用至少一种根据式I的化合物治疗至少一种δ受体相关病症的方法; 和包含至少一种根据式I的化合物的至少一种药物组合物。

    Piperazine-containing compounds useful in the treatment of pain
    9.
    发明授权
    Piperazine-containing compounds useful in the treatment of pain 失效
    可用于治疗疼痛的含有哌嗪的化合物

    公开(公告)号：US06784181B2

    公开(公告)日：2004-08-31

    申请号：US10149911

    申请日：2002-10-21

    申请人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    发明人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    IPC分类号： A61K31496

    CPC分类号： C07D401/12 ,  C07D215/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12

    摘要： The present invention is directed to a compound of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl; each phenyl ring and heteroaromatic ring optionally and independently being further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo, as well as their pharmaceutically acceptable salts. The invention includes pharmaceutical compositions comprising these compounds and the use of the compounds in therapy, in particular in the management of pain.

    摘要翻译： 本发明涉及通式（I）的化合物，其中R 1选自苯基，吡啶基，噻吩基，呋喃基，咪唑基; 每个苯环和杂芳环任选和独立地被1,2或3个选自直链和支链C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴和碘的取代基取代，以及 其药学上可接受的盐。 本发明包括包含这些化合物的药物组合物和化合物在治疗中的用途，特别是用于治疗疼痛。

    4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
    10.
    发明授权
    4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders 失效
    4-（苯基 - 哌嗪基 - 甲基）苯甲酰胺衍生物及其用于治疗疼痛，焦虑或胃肠道疾病的用途

    公开(公告)号：US08022074B2

    公开(公告)日：2011-09-20

    申请号：US12911167

    申请日：2010-10-25

    申请人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    发明人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    IPC分类号： A61K31/496

    CPC分类号： C07D295/155 ,  C07D233/24 ,  C07D307/52 ,  C07D333/20

    摘要： The invention relates to at least one compound of general formula I wherein R1 is phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, or pyridine N-oxide, where each R1 phenyl and R1 heteroaromatic ring may optionally and independently be substituted by 1, 2 or 3 substituents selected from CF3, methyl, iodo, bromo, fluoro, and chloro; R2 is independently selected from ethyl and isopropyl; R3 is hydrogen or fluoro; R4 is —NH2 or —NHSO2R5; and R5 is hydrogen, —CF3, or C1-C6 alkyl, or pharmaceutically acceptable salts thereof; at least one process for making at least one compound in accordance with Formula I; at least one method for treating at least one δ receptor associated condition with at least one compound in accordance with Formula I; and at least one pharmaceutical composition comprising at least one compound in accordance with Formula I.

    摘要翻译： 本发明涉及至少一种通式I的化合物，其中R 1是苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基或吡啶N-氧化物，其中每个R 1苯基和R 1杂芳环可任选地和独立地是 被1,2或3个选自CF 3，甲基，碘，溴，氟和氯的取代基取代; R2独立地选自乙基和异丙基; R3是氢或氟; R4是-NH2或-NHSO2R5; 和R 5是氢，-CF 3或C 1 -C 6烷基，或其药学上可接受的盐; 至少一种制备根据式I的至少一种化合物的方法; 用至少一种根据式I的化合物治疗至少一种δ受体相关病症的方法; 和包含至少一种根据式I的化合物的至少一种药物组合物。