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25 条记录 (耗时 0.023 秒)

    Tetrahydro-Beta-Carbolin-Sulfonamide Derivatives as 5-Ht6 Ligands
    3.
    发明申请
    Tetrahydro-Beta-Carbolin-Sulfonamide Derivatives as 5-Ht6 Ligands 失效
    四氢-β-咔啉磺酰胺衍生物作为5-Ht6配体

    公开(公告)号：US20080280942A1

    公开(公告)日：2008-11-13

    申请号：US11997136

    申请日：2006-07-26

    申请人： Jose Luis Diaz-Fernandez ,  Ramon Merce-Vidal ,  Joerg Holenz

    发明人： Jose Luis Diaz-Fernandez ,  Ramon Merce-Vidal ,  Joerg Holenz

    IPC分类号： A61K31/437 ,  C07D471/14 ,  A61P3/00 ,  A61P25/22 ,  A61P25/28 ,  A61P25/18

    CPC分类号： C07D471/04

    摘要： The present invention relates to new tetrahydro-β-carbolin-sulfonamide derivatives of general formula (I), optionally in form of one of their stereoisomers, preferably enantiomers or diastereomers, their racemates or in form of a mixture of at least two of their stereoisomers, preferably enantiomers or diastereomers, in any mixing ratio, or corresponding physiologically acceptable salts or corresponding solvates. These compounds are suitable as pharmacologically active agents in a medicament for the prophylaxis and/or treatment of disorders or diseases related to 5-HT6 receptors. The invention also relates to two different methods for obtaining the mentioned compounds and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及通式（I）的新的四氢-β-咔啉 - 磺酰胺衍生物，任选地以其立体异构体之一的形式，优选对映异构体或非对映异构体，其外消旋体或其至少两种立体异构体的混合物的形式 ，优选对映异构体或非对映体，以任何混合比例，或相应的生理上可接受的盐或相应的溶剂化物。 这些化合物在用于预防和/或治疗与5-HT 6受体相关的疾病或疾病的药物中适合作为药理学活性剂。 本发明还涉及获得所述化合物和含有它们的药物组合物的两种不同方法。

    Utilization of derivatives of tetrahydropyridines(or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain
    8.
    再颁专利
    Utilization of derivatives of tetrahydropyridines(or 4-hydroxypiperidines)-butylazols in the preparation of a medicament for the treatment of pain 失效
    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：USRE39113E1

    公开(公告)日：2006-05-30

    申请号：US10355216

    申请日：1999-07-09

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

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

    IPC分类号： A61K31/445 ,  A61K31/44 ,  C07D211/06 ,  C07D401/00

    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 C3-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R 1，R 2，R 3， 类似或不同的，代表氢，卤素，烷基C 1 -C 4，三氟甲基，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; Z 1是N或CR 4; Z 2是N或CR 5; Z 4是N或CR 7; 和R 4，R 5，R 6和R 7，其不同表示氢，卤素，烷基 C 3 -C 4，芳基或取代的芳基或两个相邻的基团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。

    Thienylazolylalcoxyethanamines, their preparation and their application as medicaments
    9.
    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

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

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

    IPC分类号： A61K3141

    CPC分类号： A61K31/4155 ,  C07D409/04 ,  C07D409/06

    摘要： 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.

    摘要翻译： 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
    10.
    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

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

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

    IPC分类号： C07D40314

    CPC分类号： C07D403/12

    摘要： 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.

    摘要翻译： 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