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    ISOXAZOLE-5-CARBOXAMIDE DERIVATIVES
    4.
    发明申请
    ISOXAZOLE-5-CARBOXAMIDE DERIVATIVES 审中-公开
    异佛唑-5-羧酰胺衍生物

    公开(公告)号：US20120095002A1

    公开(公告)日：2012-04-19

    申请号：US13256561

    申请日：2010-02-02

    申请人： Paul David Ratcliffe ,  Ronald Palin

    发明人： Paul David Ratcliffe ,  Ronald Palin

    IPC分类号： A61K31/5377 ,  C07D413/12 ,  C07D413/14 ,  A61P13/02 ,  A61K31/422 ,  A61P29/00 ,  A61P11/00 ,  C07D261/18 ,  A61K31/42

    CPC分类号： C07D261/08 ,  C07D261/10

    摘要： The present invention relates to isoxazole-5-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-5-carboxamide derivatives for the treatment of TRPV1 mediated disorders, such as acute and chronic pain disorders, acute and chronic neuropathic pain, acute and chronic inflammatory pain, respiratory diseases, and lower urinary tract disorders.

    摘要翻译： 本发明涉及具有通式（I）的异恶唑-5-甲酰胺衍生物或其药学上可接受的盐，其涉及包含该异构体的异恶唑-5-甲酰胺衍生物用于治疗 的TRPV1介导的疾病，例如急性和慢性疼痛障碍，急性和慢性神经性疼痛，急性和慢性炎症性疼痛，呼吸系统疾病和下尿路疾病。

    6-Mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block
    6.
    发明授权
    6-Mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block 有权
    6-巯基 - 环糊精衍生物：药物诱导的神经肌肉阻滞剂的逆转剂

    公开(公告)号：US06670340B1

    公开(公告)日：2003-12-30

    申请号：US10148307

    申请日：2002-08-19

    申请人： Mingiang Zhang ,  Ronald Palin ,  David Jonathan Bennett

    发明人： Mingiang Zhang ,  Ronald Palin ,  David Jonathan Bennett

    IPC分类号： A61K31715

    CPC分类号： C08B37/0012 ,  A61K31/724 ,  A61K45/06 ,  A61K2300/00

    摘要： Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

    摘要翻译： 公开了通式（I）的6-巯基 - 环糊精衍生物，其中m为0-7，n为1-8且m + n = 7或8; R为（C 1-6）亚烷基，任选被1-3个OH基取代，或（CH 2）邻 - 亚苯基 - （CH 2）p - o和p独立地为0-4; X是COOH，CONHR1，NHCOR2，SO2OH，PO（OH）2，O（CH2-CH2-O）q-H，OH或四唑-5-基; R1是H或（C1-3）烷基; R2是羧基苯基; q为1-3; 或其药学上可接受的盐。 6-巯基环糊精衍生物非常适合用于逆转药物诱导的神经肌肉阻滞。

    (Pyrrolidin-2-yl)phenyl derivatives
    7.
    发明授权
    (Pyrrolidin-2-yl)phenyl derivatives 有权
    （吡咯烷-2-基）苯基衍生物

    公开(公告)号：US08188123B2

    公开(公告)日：2012-05-29

    申请号：US12611468

    申请日：2009-11-03

    申请人： Simon James Anthony Grove ,  Ronald Palin ,  Ashvinkumar Dhirubhai Mistry ,  John Kinnaird Ferguson MacLean

    发明人： Simon James Anthony Grove ,  Ronald Palin ,  Ashvinkumar Dhirubhai Mistry ,  John Kinnaird Ferguson MacLean

    IPC分类号： A61K31/4439 ,  C07D401/10

    CPC分类号： C07D401/10

    摘要： The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula I wherein R1 is (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, or halo(C1-4)alkyloxy; R2 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; R3 is H, (C1-4)alkyl or halo(C1-4)alkyl; R4 is H, (C1-4)alkyl or halo(C1-4)alkyl; R5 is H, (C1-4)alkyl or halo-(C1-4)-alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C3-6)cycloalkyl group, optionally substituted with halogen; R6 is H, (C1-4)alkyl, halo(C1-4)alkyl, (C1-4)alkyloxy, halo(C1-4)alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

    摘要翻译： 本发明涉及具有通式I的（吡咯烷-2-基）苯基衍生物，其中R 1是（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基或卤代（C 1-4） 烷氧基 R 2是H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; R3是H，（C1-4）烷基或卤代（C1-4）烷基; R4是H，（C1-4）烷基或卤代（C1-4）烷基; R5是H，（C1-4）烷基或卤代（C1-4） - 烷基; 或R 4和R 5在与相同碳原子键合时可与碳原子一起形成任选被卤素取代的螺（C 3-6）环烷基; R 6为H，（C 1-4）烷基，卤代（C 1-4）烷基，（C 1-4）烷氧基，卤代（C 1-4）烷氧基或卤素; 或其药学上可接受的盐，包含其的药物组合物，以及这些（吡咯烷-2-基）苯基衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

    2-(benzimidazol-1-yl)-acetamide bisaryl derivatives
    9.
    发明申请
    2-(benzimidazol-1-yl)-acetamide bisaryl derivatives 失效
    2-（苯并咪唑-1-基） - 乙酰胺双芳基衍生物

    公开(公告)号：US20070112034A1

    公开(公告)日：2007-05-17

    申请号：US11593741

    申请日：2006-11-07

    申请人： Ronald Palin ,  Colin Gray

    发明人： Ronald Palin ,  Colin Gray

    IPC分类号： A61K31/4439 ,  A61K31/427 ,  A61K31/422 ,  A61K31/42 ,  A61K31/4184 ,  C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D235/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

    摘要： The invention relates to 2-(benzimidazol-1-yl)-acetamide bisaryl derivative having the general Formula I wherein n is 0 or 1; Ar1 represents a diradical derived from a 5- or-6-membered aromatic ring, optionally comprising 1-3 heteroatoms selected from N, O and S, said ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy, halogen, CF3 or cyano; Ar2 represents a 6-membered aryl ring, optionally comprising 1-3 nitrogen atoms, said ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), di(C1-4)alkylamino, halogen, CF3 or cyano; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same and to the use of said 2-(benzimidazol-1-yl)-acetamide bisaryl derivatives in the treatment of TRPV1 mediated disorders.

    摘要翻译： 本发明涉及具有通式I的2-（苯并咪唑-1-基） - 乙酰胺双芳基衍生物，其中n为0或1; Ar 1代表衍生自5或6元芳环的二价基团，任选地包含1-3个选自N，O和S的杂原子，所述环任选被（C 1 -C 6） 1-4 C 1-4烷基，（C 1-4烷基）烷氧基，卤素，CF 3或氰基; Ar 2表示任选地包含1-3个氮原子的6元芳环，所述环任选被1-3个选自（C 1-4 - ）烷基的取代基取代， 烷基（任选被1个或多个卤素取代），（C 1-4 - ）烷氧基（任选被1个或多个卤素取代），二（C 1-4 - 烷基）烷基 ，卤素，CF 3或氰基; 或其药学上可接受的盐; 包括其的药物组合物和所述2-（苯并咪唑-1-基） - 乙酰胺双芳基衍生物在治疗TRPV1介导的病症中的用途。

    6-mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block
    10.
    再颁专利
    6-mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block 有权
    6-巯基 - 环糊精衍生物：用于药物诱导的神经肌肉阻滞剂的逆转剂

    公开(公告)号：USRE44733E1

    公开(公告)日：2014-01-28

    申请号：US13432742

    申请日：2012-03-28

    申请人： Mingiang Zhang ,  Ronald Palin ,  Jonathan Bennett

    发明人： Mingiang Zhang ,  Ronald Palin ,  Jonathan Bennett

    IPC分类号： A61K31/724 ,  A61K31/715 ,  A61K31/537 ,  A61K31/452 ,  A61K31/225 ,  A61P25/00 ,  C08B37/16

    摘要： Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.

    摘要翻译： 公开了通式（I）的6-巯基 - 环糊精衍生物，其中m为0-7，n为1-8且m + n = 7或8; R为（C 1-6）亚烷基，任选被1-3个OH基取代，或（CH 2）邻 - 亚苯基 - （CH 2）p - o和p独立地为0-4; X是COOH，CONHR1，NHCOR2，SO2OH，PO（OH）2，O（CH2-CH2-O）q-H，OH或四唑-5-基; R1是H或（C1-3）烷基; R2是羧基苯基; q为1-3; 或其药学上可接受的盐。 6-巯基环糊精衍生物非常适合用于逆转药物诱导的神经肌肉阻滞。