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    Alpha-aminoamide derivatives useful as analgesic agents
    7.
    再颁专利
    Alpha-aminoamide derivatives useful as analgesic agents 有权
    用作止痛剂的α-氨基酰胺衍生物

    公开(公告)号：USRE40259E1

    公开(公告)日：2008-04-22

    申请号：US11359982

    申请日：1998-12-12

    申请人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    发明人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    IPC分类号： A61K31/275 ,  A61K31/165 ,  C07C255/50 ,  C07C233/05

    CPC分类号： C07C237/06 ,  A61K31/165 ,  C07C255/54

    摘要： The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents.In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.Accordingly, one object of the present invention is to provide the use of a compound of formula (I) wherein: A is a —(CH2)m—, —(CH2)n—X— or —(CH2)v—O— group wherein m is an integer of 1 to 4, n is zero or an integer of 1 to 4, X is —S— or —NH—, and v is zero or an integer of 1 to 5; s is 1 or 2; R is a furyl, thienyl, or pyridyl ring or a phenyl ring optionally substituted by one or two substituents independently chosen from halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy and trifluoromethyl; R1 is hydrogen or C1-C4 alkyl; one of R2 and R3 is hydrogen and the other is hydrogen or C1-C4 alkyl optionally substituted by hydroxy or phenyl; or R2 and R3 taken together with the carbon atom to which they are linked form a C3-C6 cycloalkyl ring; or R2 and R3 are both methyl; R4 is hydrogen or C1-C4 alkyl.

    摘要翻译： 本发明涉及新的和已知的α-氨基酰胺化合物，其制备方法，含有它们的药物组合物及其作为治疗剂的用途。 特别地，本发明的化合物具有止痛特性，特别可用于治疗和缓解慢性和神经性疼痛。 因此，本发明的一个目的是提供式（I）化合物的用途，其中：A是 - （CH 2）n - ， - （ CH 2 - （CH 2）n -X - 或 - （CH 2）2 -O - ，其中m是 1〜4的整数，n为0或1〜4的整数，X为-S-或-NH-，v为0或1〜5的整数。 s为1或2; R是呋喃基，噻吩基或吡啶基环或任选被一个或两个独立地选自卤素，氰基，C 1 -C 4烷基的取代基取代的苯环，C C 1 -C 4烷氧基和三氟甲基; R 1是氢或C 1 -C 4烷基; R 2和R 3中的一个是氢，另一个是氢或任选地是C 1 -C 4 - 被羟基或苯基取代; 或R 2和R 3与它们所连接的碳原子一起形成C 3 -C 6 - 环烷基环; 或R 2和R 3均为甲基; R 4是氢或C 1 -C 4烷基。

    Alpha-aminoamide derivatives useful as analgesic agents
    8.
    发明授权
    Alpha-aminoamide derivatives useful as analgesic agents 有权
    用作止痛剂的α-氨基酰胺衍生物

    公开(公告)号：US06306903B1

    公开(公告)日：2001-10-23

    申请号：US09582198

    申请日：2000-08-29

    申请人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    发明人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    IPC分类号： A61K31275

    CPC分类号： C07C237/06 ,  A61K31/165 ,  C07C255/54

    摘要： The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain. Accordingly, one object of the present invention is to provide the use of a compound of formula (I) wherein: A is a —(CH2)m—, —(CH2)n—X— or —(CH2)v—O— group wherein m is an integer of 1 to 4, n is zero or an integer of 1 to 4, X is —S— or —NH—, and v is zero or an integer of 1 to 5; s is 1 or 2; R is a furyl, thienyl, or pyridyl ring or a phenyl ring optionally substituted by one or two substitutents independently chosen from halogen, cyano, C1-C4 alkyl, C1-C4 alkoxy and trifluoromethyl; R1 is hydrogen or C1-C4 alkyl; one of R2 and R3 is hydrogen and the other is hydrogen or C1-C4 alkyl optionally substituted by hydroxy or phenyl; or R2 and R3 taken together with the carbon atom to which they are linked form a C3-C6 cycloalkyl ring; or R2 and R3 are both methyl; R4 is hydrogen or C1-C4 alkyl.

    摘要翻译： 本发明涉及新的和已知的α-氨基酰胺化合物，其制备方法，含有它们的药物组合物及其作为治疗剂的用途。特别地，本发明的化合物具有止痛性质，特别是 对于治疗和缓解慢性和神经性疼痛有用。因此，本发明的一个目的是提供式（I）化合物的用途，其中：A是 - （CH 2）m - ， - （CH 2）n X - 或 - （CH 2）v O-基团，其中m为1至4的整数，n为0或1至4的整数，X为-S-或-NH-，v为0或1至 5; s是1或2; R是呋喃基，噻吩基或吡啶基环或任选被一个或两个独立地选自卤素，氰基，C 1 -C 4烷基，C 1 -C 4烷氧基和三氟甲基的取代基取代的苯环; R 1是 氢或C 1 -C 4烷基; R 2和R 3之一是氢，另一个是氢或任选地被H 5取代的C 1 -C 4烷基 羟基或苯基; 或者R 2和R 3与它们所连接的碳原子一起形成C 3 -C 6环烷基环; 或R 2和R 3均为甲基; R 4为氢或C 1 -C 4烷基。

    Substituted 2-benzylamino-2-phenyl-acetamide compounds
    9.
    发明授权
    Substituted 2-benzylamino-2-phenyl-acetamide compounds 失效
    取代的2-苄基氨基-2-苯基 - 乙酰胺化合物

    公开(公告)号：US06303819B1

    公开(公告)日：2001-10-16

    申请号：US09581254

    申请日：2000-09-11

    申请人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    发明人： Paolo Pevarello ,  Mario Varasi ,  Patricia Salvati ,  Claes Post

    IPC分类号： C07C23305

    CPC分类号： C07C237/20 ,  C07C2601/02

    摘要： Compounds which are substituted 2-benzylamino-2-phenyl-acetamide compounds of formula (I) wherein: n is zero, 1, 2 or 3; X is —O—, —S—, —CH2— or —NH—; each of R, R1, R2 and R3, independently, is hydrogen, C1-C6 alkyl, halogen, hydroxy, C1-C6 alkoxy or trifluoromethyl; each of R4 and R5, independently, is hydrogen, C1-C6 alkyl or C3-C7 cycloalkyl; or pharmaceutically acceptable salts thereof, are useful in treating conditions such as chronic or neuropathic pain.

    摘要翻译： 作为式（I）的取代的2-苄基氨基-2-苯基 - 乙酰胺化合物的化合物，其中：n为0,1,2或3; X为-O - ， - S - ， - CH 2 - 或-NH- R 1，R 2和R 3独立地是氢，C 1 -C 6烷基，卤素，羟基，C 1 -C 6烷氧基或三氟甲基; R 4和R 5各自独立地是氢，C 1 -C 6烷基或C 3 -C 7环烷基 ; 或其药学上可接受的盐可用于治疗诸如慢性或神经性疼痛的病症。