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    • 64. 发明授权
    • 4-(phenyl-piperazinyl-methyl)benzamide derivatives and their use for the treatment of pain, anxiety or gastrointestinal disorders
    • 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
    • US08022074B2
    • 2011-09-20
    • US12911167
    • 2010-10-25
    • William BrownChristopher WalpoleNiklas Plobeck
    • William BrownChristopher WalpoleNiklas Plobeck
    • A61K31/496
    • C07D295/155C07D233/24C07D307/52C07D333/20
    • 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.
    • 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。
    • 65. 发明申请
    • Novel Compounds
    • 新型化合物
    • US20110039858A1
    • 2011-02-17
    • US12911167
    • 2010-10-25
    • William BrownChristopher WalpoleNiklas Plobeck
    • William BrownChristopher WalpoleNiklas Plobeck
    • A61K31/497A61P25/00
    • C07D295/155C07D233/24C07D307/52C07D333/20
    • 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.
    • 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。
    • 68. 发明授权
    • 4(phenyl-piperazinyl-methyl) benzamide derivatives and their use for the treatment of pain anxiety or gastrointestinal disorders
    • 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
    • US07229994B2
    • 2007-06-12
    • US10477642
    • 2002-05-16
    • William BrownChristopher WalpoleNiklas Plobeck
    • William BrownChristopher WalpoleNiklas Plobeck
    • A61K31/496A61K31/495
    • C07D295/155C07D233/24C07D307/52C07D333/20
    • 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.
    • 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。