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17 条记录 (耗时 0.036 秒)

    2-(benzimidazol-1-yl)-acetamide bisaryl derivatives
    1.
    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。

    2-(Benzimidazol-1-Yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives
    2.
    发明申请
    2-(Benzimidazol-1-Yl)-N-(4-phenylthiazol-2-yl) acetamide derivatives 审中-公开
    2-（苯并咪唑-1-基）-N-（4-苯基噻唑-2-基）乙酰胺衍生物

    公开(公告)号：US20070105920A1

    公开(公告)日：2007-05-10

    申请号：US11593742

    申请日：2006-11-07

    申请人： Ronald Palin ,  Colin Gray

    发明人： Ronald Palin ,  Colin Gray

    IPC分类号： A61K31/427 ,  C07D417/02

    CPC分类号： C07D417/12

    摘要： The invention relates 2-(benzimidazol-1-yl)-N-(4-phenylthiazol-2-yl)acetamide derivatives having the general Formula I wherein R1 is H, (C1-4)alkyl, (C1-4)alkyloxy or halogen; R2 represents 1-3 substituents selected from H, (C1-4)alkyl (optionally substituted with 1 or more halogens), (C1-4)alkyloxy (optionally substituted with 1 or more halogens), 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)-N-(4-phenylthiazol-2-yl)acetamide 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）-N-（4-苯基噻唑-2-基）乙酰胺衍生物，其中R 1是H，（C 1 -4 C 1-4烷基，（C 1-4烷基）烷氧基或卤素; R 2表示1-3个选自H，（C 1-4烷基）烷基（任选被1个或多个卤素取代）的取代基，（C 1-4） 烷氧基（任选被1个或多个卤素取代），卤素，CF 3或氰基; 或其药学上可接受的盐; 涉及包含其的药物组合物和所述2-（苯并咪唑-1-基）-N-（4-苯基噻唑-2-基）乙酰胺衍生物在治疗TRPV1介导的病症中的用途。

    6-Mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block
    4.
    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
    5.
    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。

    6-mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block
    8.
    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。