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    Novel Compounds
    11.
    发明申请
    Novel Compounds 失效
    新型化合物

    公开(公告)号：US20110039858A1

    公开(公告)日：2011-02-17

    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： A61K31/497 ,  A61P25/00

    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 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。

    4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders
    12.
    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：US07229994B2

    公开(公告)日：2007-06-12

    申请号：US10477642

    申请日：2002-05-16

    申请人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    发明人： William Brown ,  Christopher Walpole ,  Niklas Plobeck

    IPC分类号： A61K31/496 ,  A61K31/495

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

    摘要： Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; R2 is independently selected from ethyl and isopropyl; R3 is independently selected from hydrogen and fluoro; R4 is independently selected from —OH, —NH2 and —NHSO2R5; and R5 is independently selected from hydrogen, —CF3 and C1–C6 alkyl, or salts thereof or separate enantiomers and salts thereof; 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 said ring systems; are disclosed and claimed in the present application, as well as separate enantiomers of the compounds and salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

    摘要翻译： 通式I R 1的化合物选自苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基和吡啶N-氧化物中的任何一种; R 2独立地选自乙基和异丙基; R 3独立地选自氢和氟; R 4独立地选自-OH，-NH 2和-NHSO 2 R 5; 和R 5独立地选自氢，-CF 3 3和C 1 -C 6烷基，或盐 或其单独的对映体和盐; 其中每个R 1杂芳环可以任选和独立地被1,2或3个选自直链和支链C 1 -C 6的取代基取代。 烷基，NO 2，CF 3，C 1 -C 6烷氧基，氯，氟，溴， 和碘。 杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及包含新化合物的化合物和盐和药物组合物的分开的对映异构体及其在治疗中的用途，特别是在治疗疼痛，焦虑和功能性胃肠道疾病中的用途。

    4[piperidin-4-yliden-(3-carbamoylpheny)methyl]benzamide derivatives and their use for the treatment of pain spinal injuries or gastrointestinal disorders
    17.
    发明授权
    4[piperidin-4-yliden-(3-carbamoylpheny)methyl]benzamide derivatives and their use for the treatment of pain spinal injuries or gastrointestinal disorders 失效
    4 [哌啶-4-亚基 - （3-氨基甲酰基苯基）甲基]苯甲酰胺衍生物及其用于治疗疼痛脊髓损伤或胃肠道疾病

    公开(公告)号：US07205317B2

    公开(公告)日：2007-04-17

    申请号：US10491263

    申请日：2002-10-02

    申请人： William Brown ,  Christopher Walpole ,  Zhongyong Wei

    发明人： William Brown ,  Christopher Walpole ,  Zhongyong Wei

    IPC分类号： A61K31/4528 ,  A61K31/4535 ,  C07D211/08

    CPC分类号： C07D401/06 ,  C07D211/70 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

    摘要： Compounds of general formula (I) wherein R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl and triazolyl; where each R1 phenyl ring and 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 thephenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, inparticular in the management of pain.

    摘要翻译： 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，吡咯基和三唑基中的任一个; 其中每个R 1苯基环和R 1'杂芳环可以任选地和独立地被1,2或3个选自直链和支链C 1的取代基取代， C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷基，C 1 -C 6烷基， 烷氧基，氯，氟，溴和碘。 苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及它们的药学上可接受的盐和药物组合物，其包含新化合物及其在治疗中的用途，特别是在疼痛的管理中。

    4-(Phenyl-(piperidin-4-yl)-amino)-benzamide derivaties and their use for the treatment of pain, anxiety or gastrointestinal disorders
    19.
    发明授权
    4-(Phenyl-(piperidin-4-yl)-amino)-benzamide derivaties and their use for the treatment of pain, anxiety or gastrointestinal disorders 失效
    4-（苯基 - （哌啶-4-基） - 氨基） - 苯甲酰胺衍生物及其用于治疗疼痛，焦虑或胃肠道疾病

    公开(公告)号：US07064137B2

    公开(公告)日：2006-06-20

    申请号：US10477853

    申请日：2002-05-16

    申请人： William Brown ,  Andrew Griffin ,  Christopher Walpole

    发明人： William Brown ,  Andrew Griffin ,  Christopher Walpole

    IPC分类号： A61K31/4468 ,  C07D211/58

    CPC分类号： C07D401/06 ,  C07D211/58 ,  C07D405/06 ,  C07D409/06 ,  C07D417/06

    摘要： Compounds of general formula (I): R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and 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 phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.

    摘要翻译： 通式（I）的化合物：R 1选自苯基，吡啶基，噻吩基，呋喃基，咪唑基，吡咯基，三唑基，噻唑基和吡啶N-氧化物中的任何一种; 其中每个R 1苯基环和R 1'杂芳环可以任选地和独立地被1,2或3个选自直链和支链C 1的取代基取代， C 1 -C 6烷基，NO 2，CF 3，C 1 -C 6烷基，C 1 -C 6烷基， 烷氧基，氯，氟，溴和碘。 苯环上和杂芳环上的取代可以在所述环体系上的任何位置进行; 在本申请中公开和要求保护，以及包含新化合物的盐和药物组合物及其在治疗中的用途，特别是在治疗疼痛，焦虑和功能性胃肠道疾病中的用途。