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    Thienylazolylalcoxyethanamines, their preparation and their application as medicaments
    11.
    发明授权
    Thienylazolylalcoxyethanamines, their preparation and their application as medicaments 失效
    噻吩并噻唑基羟乙胺，它们的制备及其作为药物的应用

    公开(公告)号：US06410582B1

    公开(公告)日：2002-06-25

    申请号：US09673186

    申请日：2000-10-12

    Applicant: Ramon Merce-Vidal ,  Blas Andaluz-Mataro ,  Jordi Frigola-Constansa

    Inventor： Ramon Merce-Vidal ,  Blas Andaluz-Mataro ,  Jordi Frigola-Constansa

    IPC: A61K3141

    CPC classification number: A61K31/4155 ,  C07D409/04 ,  C07D409/06

    Abstract: The thienylazolylalkoxyethanamines (I) where R1 is a hydrogen atom, a halogen atom or a lower alkyl radical; R2, R3 and R4 represent, independently, a hydrogen atom or a lower alkyl radical; and Az represents a five-member nitrogenated hetercyclic aromatic group, N-methyl-substituted, that contains from one to three nitrogen atoms. They have analgesic activity in mammals, including humans. The compounds (I) can be obtained, for example, by reaction of a derivative of hydroxy-thienylazol (IV) with a derivative of a suitable N-(ethyl)amine. The compounds (IV) are useful intermediates in the synthesis of the compounds (I). The compounds (I) have an application in human and/or veterinary medicine.

    Abstract translation: 其中R 1是氢原子，卤素原子或低级烷基的噻吩基唑烷基乙胺（I） R2，R3和R4独立地表示氢原子或低级烷基; 并且Az表示含有一至三个氮原子的五元氮杂环芳族基团N-甲基取代基。 它们在哺乳动物，包括人类中具有止痛活性。 化合物（I）可以通过例如羟基噻吩唑（IV）的衍生物与合适的N-（乙基）胺衍生物的反应来获得。 化合物（IV）是化合物（I）的合成中的有用的中间体。 化合物（I）在人和/或兽医学中有应用。

    2-{4-[4-(4,5-dichloro-2-methylimidazol-1-yl)butyl]-1-piperazinyl}-5-fluoropyrimidine, its preparation and its therapeutic use
    12.
    发明授权
    2-{4-[4-(4,5-dichloro-2-methylimidazol-1-yl)butyl]-1-piperazinyl}-5-fluoropyrimidine, its preparation and its therapeutic use 失效
    2- {4- [4-（4,5-二氯-2-甲基咪唑-1-基）丁基] -1-哌嗪基} -5-氟嘧啶，其制备及其治疗用途

    公开(公告)号：US06303608B1

    公开(公告)日：2001-10-16

    申请号：US09445081

    申请日：2000-02-29

    Applicant: Ramon Merce-Vidal ,  Jordi Frigola-Constansa

    Inventor： Ramon Merce-Vidal ,  Jordi Frigola-Constansa

    IPC: C07D40314

    CPC classification number: C07D403/12

    Abstract: 2-{4-[4-(4,5-dichloro-2-methylimidazol-1-yl)butyl]-1-piperazinyl}-5-fluoropyrimidine, and its physiologically acceptable salts; pharmaceutical compositions containing these compounds, and a method of treating vertigo, travel sickness, nausea, depression, anxiety, gastric acid secretion, obsessive/compulsive disorders, panic attacks or sleep apnea using these compounds are disclosed.

    Abstract translation: 2- {4- [4-（4,5-二氯-2-甲基咪唑-1-基）丁基] -1-哌嗪基} -5-氟嘧啶及其生理上可接受的盐; 公开了含有这些化合物的药物组合物和使用这些化合物治疗眩晕，旅行病，恶心，抑郁，焦虑，胃酸分泌，强迫症/强迫症，恐慌发作或睡眠呼吸暂停的方法

    Process for the preparation of aryl (or heteroaryl) piperazinylbutylazole derivatives
    18.
    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

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

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

    IPC: 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 classification number: C07D207/325 ,  C07D231/12 ,  C07D231/16 ,  C07D233/56 ,  C07D233/68 ,  C07D249/08 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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）。

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