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99 条记录 (耗时 0.037 秒)

    Method of treatment and/or prevention of brain, spinal or nerve injury
    91.
    发明申请
    Method of treatment and/or prevention of brain, spinal or nerve injury 审中-公开
    治疗和/或预防脑，脊髓或神经损伤的方法

    公开(公告)号：US20060247240A1

    公开(公告)日：2006-11-02

    申请号：US11481216

    申请日：2006-07-05

    申请人： Torsten Hoffmann ,  Alan Nimmo ,  Andrew Sleight ,  Pierre Vankan ,  Robert Vink

    发明人： Torsten Hoffmann ,  Alan Nimmo ,  Andrew Sleight ,  Pierre Vankan ,  Robert Vink

    IPC分类号： A61K31/5377 ,  A61K31/496 ,  A61K31/455

    CPC分类号： A61K31/435

    摘要： The invention relates to a method of treatment and/or prevention of brain, spinal or nerve injury comprising administration to a person in need of such treatment, of a therapeutically effective amount of an NK-1 receptor antagonist compound of the formula wherein the meanings of R, R1, R2, R2, R3, and R4 are explained in the specification and the pharmaceutically acceptable acid addition salts and the prodrugs thereof either alone or in combination with a magnesium salt. Exemplified is the use of N-(3,5-bis-trifluoromethyl-benzyl)-N-methyl-6-(4-methyl-piperazin-1-yl)-4-o-tolyl-nicotinamide. The invention also relates to pharmaceutical composition comprising one or more such NK-1 receptor antagonists, optionally in combination with a magnesium salt, and a pharmaceutically acceptable excipient for the treatment and/or prevention of brain, spinal or nerve injury.

    摘要翻译： 本发明涉及一种治疗和/或预防脑，脊髓或神经损伤的方法，包括向需要这种治疗的人施用治疗有效量的下式的NK-1受体拮抗剂化合物，其中， R 1，R 2，R 2，R 2，R 3和R 4， SUP>在本说明书和药学上可接受的酸加成盐及其前药中单独或与镁盐组合进行说明。 举例说明了使用N-（3,5-双 - 三氟甲基 - 苄基）-N-甲基-6-（4-甲基 - 哌嗪-1-基）-4-邻甲苯基 - 烟酰胺。 本发明还涉及包含一种或多种这样的NK-1受体拮抗剂，任选与镁盐组合的药物组合物和用于治疗和/或预防脑，脊髓或神经损伤的药学上可接受的赋形剂。

    5-phenyl-pyrimidine derivatives
    93.
    发明授权
    5-phenyl-pyrimidine derivatives 失效
    5-苯基 - 嘧啶衍生物

    公开(公告)号：US06756380B1

    公开(公告)日：2004-06-29

    申请号：US09575789

    申请日：2000-05-22

    申请人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    发明人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    IPC分类号： C07D23932

    CPC分类号： C07D239/28 ,  C07D239/34 ,  C07D239/42 ,  C07D239/47 ,  C07D239/48

    摘要： Compounds of the general formula are described: wherein R1 is hydrogen or halogen; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; R3 is halogen, trifluoromethyl, lower alkoxy or lower alkyl; R4/R4′are each independently hydrogen or lower alkyl; R5 is lower alkyl, lower alkoxy, amino, hydroxy, hydroxy-lower alkyl, —(CH2)n-piperazinyl, optionally substituted by lower alkyl, —(CH2)n-morpholinyl, —(CH2)n+1-imidazolyl, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n—NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, or —O—(CH2)n+1N(R4″)2, wherein R4″ is hydrogen or lower alkyl; R6 is hydrogen; R2 and R6 or R1 and R6 may together be —CH═CH—CH═CH—, wherein R2 and R6 or R1 and R6, respectively, together with the two carbon ring atoms to which they are attached form a fused ring, with the proviso that n for R1 is 1; n is independently 0-2; and X is —C(O)N(R4″)— or —N(R4″)C(O)—; and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 描述通式的化合物：其中R 1是氢或卤素; R 2是氢，卤素，低级烷基或低级烷氧基; R 3是卤素，三氟甲基，低级烷氧基或低级烷基; R 4 R 5是氢或低级烷基; R 5是低级烷基，低级烷氧基，氨基，羟基，羟基 - 低级烷基， - （CH 2）n - 哌嗪基，任选被低级烷基取代， （CH2）n-吗啉基， - （CH2）n + 1-咪唑基，-O-（CH2）n + 1-吗啉基，-O-（CH2）n + 1-哌啶基，低级烷基 - ，苄基氨基，-NH-（CH 2）n + 1N（R 4“）2， - （CH 2）n -NH-（CH 2）n + 1N（R 4”）2， - （CH 2） n + 1N（R 4“）2或-O-（CH 2）n + 1N（R 4”）2，其中R 4“是氢或低级烷基; R 6' R 2和R 6或R 1和R 6可以一起为-CH = CH-CH = CH-，其中R 2和R 6或R 1为氢; 和R 6分别与它们所连接的两个碳环原子一起形成稠合环，条件是R 1的n为1; n独立地为0-2; 和X是-C（O）N（R“”） - 或-N（R“”）C（O） - ;及其药学上可接受的酸加成盐。

    Biphenyl derivatives
    99.
    发明授权
    Biphenyl derivatives 失效
    联苯衍生物

    公开(公告)号：US06291465B1

    公开(公告)日：2001-09-18

    申请号：US09513147

    申请日：2000-02-25

    申请人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    发明人： Michael Bös ,  Guido Galley ,  Thierry Godel ,  Torsten Hoffmann ,  Walter Hunkeler ,  Patrick Schnider ,  Heinz Stadler

    IPC分类号： C07C23300

    CPC分类号： C07D295/155 ,  C07C217/54 ,  C07C233/15 ,  C07C233/44 ,  C07C233/66 ,  C07C235/42

    摘要： The invention relates to compounds of the formula wherein R is hydrogen, lower alkyl, lower alkoxy halogen, amino, —N(R6)2 or trifluoromethyl; R1 is hydrogen lower alkoxy or halogen, R and R1 may be together —CH═CH—CH═CH—; R2 is halogen, lower alkyl or trifluoromethyl; R3 is hydrogen or lower alkyl; R4 is hydrogen or a cyclic tertiary amine, optionally substituted by lower alkyl; R5 is hydrogen, nitro, amino or —N(R6)2; R6 is hydrogen or lower alkyl, X is —C(O)N(R6)—, —(CH2)nO—, (CH2)nN(R6)—, —N(R6)C(O)— or —N(R6)(CH2)n—; and n is 1 or 2; and pharmaceutically acceptable acid addition salts thereof. The compounds of formula I may be used for the treatment of diseases related to the NK-1 receptor.

    摘要翻译： 本发明涉及式的化合物，其中R是氢，低级烷基，低级烷氧基卤素，氨基，-N（R6）2或三氟甲基; R1是氢低级烷氧基或卤素，R和R1可以一起是-CH = CH-CH = CH-; R 2为卤素，低级烷基或三氟甲基; R 3为氢或低级烷基; R 4为氢或环状叔胺，任选被低级烷基取代; R 5为氢，硝基，氨基或-N（R 6） X是-C（O）N（R6） - ， - （CH2）nO-，（CH2）nN（R6） - ， - （R6）C（O） - 或-N ）（CH 2）n - 和n为1或2;及其药学上可接受的酸加成盐。式I化合物可用于治疗与NK-1受体有关的疾病。