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    Process for the preparation of aryl (or heteroaryl) piperazinylbutylazole derivatives
    3.
    发明授权
    Process for the preparation of aryl (or heteroaryl) piperazinylbutylazole derivatives 失效
    制备亚芳基（或杂芳基）哌嗪基吡唑衍生物的方法

    公开(公告)号：US5227486A

    公开(公告)日：1993-07-13

    申请号：US847625

    申请日：1992-03-06

    申请人： Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Juan Pares-Corominas

    发明人： Ramon Merce-Vidal ,  Jordi Frigola-Constansa ,  Juan Pares-Corominas

    IPC分类号： A61K31/40 ,  A61K31/435 ,  A61K31/495 ,  A61K31/496 ,  A61K31/505 ,  A61P9/12 ,  A61P25/00 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  C07D207/32 ,  C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D231/20 ,  C07D231/38 ,  C07D231/56 ,  C07D233/61 ,  C07D233/68 ,  C07D239/26 ,  C07D241/04 ,  C07D277/64 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04 ,  C07D521/00

    CPC分类号： C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D233/56 ,  C07D233/68 ,  C07D249/08 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04

    摘要： The present invention relates to a process for the preparation of aryl (or heteroaryl) piperazinyl-butylazole derivatives corresponding to the general formula I ##STR1## in which Ar denotes a nitrogenous or other aromatic radical chosen from differently substituted aryls, differently substituted 2-pyrimidine, 2-N-methyl-imidazole and 3-(1,2-benzisothiazole)Z.sub.1 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.1Z.sub.2 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.2Z.sub.4 denotes a nitrogen atom or an optionally substituted carbon atom which may be denoted by: C-R.sub.4 and R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which are identical or different and may also form a part of another ring, aromatic or otherwise, denote a hydrogen atom, a halogen, a lower alkyl radical, a nitro radical, a hydroxyl radical, an alkoxy radical, a cyano radical, a carboxylic radical, a carboxamido radical, an alkylcarboxylate radical, an aryl or substituted aryl radical, a sulfonic radical, a sulfonamido radical optionally substituted on the amino group or an amino or substituted amino radicalwherein ##STR2## in which Ar has the meanings referred to above and X denotes a halogen atom, is reacted with a compound of general formula III ##STR3## in which Z.sub.1, Z.sub.2, Z.sub.4 and R.sub.3 have the meanings referred to above.

    摘要翻译： 本发明涉及一种制备相应于通式I（I）的芳基（或杂芳基）哌嗪基 - 丁唑衍生物的方法，其中Ar表示选自不同取代的芳基的含氮或其它芳族基团， 2-嘧啶，2-N-甲基咪唑和3-（1,2-苯并异噻唑）Z1表示氮原子或任选取代的碳原子，可以用以下表示：C-R 1 Z 2表示氮原子或任选取代的 碳原子，其可以由以下表示：C-R 2 Z 4表示氮原子或任选取代的碳原子，其可以由以下表示：C-R 4和R 1，R 2，R 3和R 4，其相同或不同，并且也可以形成 另一个芳环或其它环的一部分表示氢原子，卤素，低级烷基，硝基，羟基，烷氧基，氰基，羧基，甲酰胺基，烷基羧酸根， 芳基或取代基 在氨基或氨基或取代的氨基上任选取代的磺酰基，磺酰氨基，其中Ar具有上述含义，X表示卤素原子的氨基或取代的氨基，与其反应，与 其中Z1，Z2，Z4和R3具有上述含义的通式III的化合物（III）。

    Utilization of derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain
    8.
    发明授权
    Utilization of derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain 有权
    四氢吡啶衍生物（或4-羟基哌啶） - 丁基二醇在制备用于治疗疼痛的药物中的应用

    公开(公告)号：US06384055B1

    公开(公告)日：2002-05-07

    申请号：US09743085

    申请日：2001-02-13

    申请人： Ramon Merce-Vidal ,  Jordi Frigola-Constansa

    发明人： Ramon Merce-Vidal ,  Jordi Frigola-Constansa

    IPC分类号： A61K31445

    CPC分类号： A61K31/454 ,  A61K31/4439

    摘要： Derivatives of tetrahydropyridines (or 4-hydroxypiperidines)-butylazols of formula (I), wherein R1, R2 and R3, which are similar or different, represent each of them hydrogen, halogen, alkyl C1-C4, trifluoromethyl, hydroxyl, alkoxyl, or two adjacent radicals can form a ring; A is a C atom and the dotted line represents an additional bond, or A is a C atom joined to a hydroxyl group and the dotted line represents absence of additional bond; Z1 is N or CR4; Z2 is N or CR5; Z4 is N or CR7; and R4, R5, R6 and R7, which different, represent hydrogen, halogen, alkyl C1-C4, aryl or substituted aryl, or two adjacent radicals can form part of another ring. These derivatives are useful for the treatment of acute pain, neuropathic pain or nociceptive pain in mammals, including human beings.

    摘要翻译： 式（I）的四氢吡啶（或4-羟基哌啶） - 丁基二醇的衍生物，其中相同或不同的R 1，R 2和R 3各自表示氢，卤素，C 1 -C 4烷基，三氟甲基，羟基，烷氧基或 两个相邻的基团可以形成环; A是C原子，虚线表示附加键，或A是连接到羟基的C原子，虚线表示不存在附加键; Z1是N或CR4; Z2为N或CR5; Z4是N或CR7; 和不同的代表氢，卤素，烷基C1-C4，芳基或取代的芳基或两个相邻基团的R4，R5，R6和R7可以形成另一个环的一部分。 这些衍生物可用于治疗哺乳动物（包括人类）的急性疼痛，神经性疼痛或伤害性疼痛。