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    Substituted imidazole derivatives having agonist-like activity at alpha 2B or 2B/2C adrenergic receptors
    3.
    发明公开
    Substituted imidazole derivatives having agonist-like activity at alpha 2B or 2B/2C adrenergic receptors 审中-公开
    在α2B或2B / 2C肾上腺素能受体上具有激动剂样活性的取代的咪唑衍生物

    公开(公告)号：EP1413576A2

    公开(公告)日：2004-04-28

    申请号：EP04001074.6

    申请日：1998-12-03

    申请人： Allergan, Inc.

    发明人： Chow, Ken ,  Gil, Daniel W. ,  Burke, James A. ,  Harcourt, Dale A. ,  Garst, Michael E. ,  Wheeler, Larry A. ,  Munk, Stephen A.

    IPC分类号： C07D233/06 ,  C07D233/84 ,  C07D263/28 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  A61K31/4166 ,  A61P5/00

    CPC分类号： C07D233/56 ,  C07D233/06 ,  C07D233/64 ,  C07D233/84 ,  C07D263/28 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/12 ,  C07D495/04

    摘要： Coumpounds having adrenergic activity which are selective agonists for one or both of the α 2B and α 2C adrenoceptor receptor subtypes in preference to the α 2A adrenoceptor receptor subtype; the active compound being selected from the group consisting of compounds having formula (I) wherein the dotted lines represent optional bonds provided that two double bonds may not share a common carbon atom; R is H or lower alkyl; X is S or C(H)R 1 , wherein R 1 is H or lower alkyl, but R 1 is absent when the bond between X and the ring represented by formula (a) is a double bond; Y is O, N, S, (CR 1 2 ) y , wherein y is an integer of from 1 to 3, -CH=CH- or -Y 1 CH 2 -, wherein Y 1 is O, N or S; x is an integer of 1 or 2, wherein x is 1 when R 2 , R 3 or R 4 is bound to a saturated carbon atom and x is 2 when R 2 , R 3 or R 4 is bound to a saturated carbon atom; R 2 is H, lower alkyl, halogen, hydroxy or lower alkoxy, or, when attached to a saturated carbon atom, R 2 may be oxo; R 3 and R 4 are, each, H, lower alkyl, hydroxy, lower alkoxy, or phenyl or, together, are -(C(R 2 )x)z-; -Y 1 (C(R 2 )x)z'-; -Y 1 (C(R 2 )x)yY 1 -; -(C(R 2 )x)-Y 1 -(C(R 2 )x)-; -(C(R 2 )x)-Y 1 -(C(R 2 )x)-(C(R 2 )x)- and -Y 1 -(C(R 2 )x)-Y 1 -(C(R 2 )x)- wherein z is an integer of from 3 to 5, z' is an integer of from 2 to 4 and x and y are as defined above, and further either end of each of these divalent moieties may attach at either R3 or R4 to form a condensed ring structure and the rings formed may be totally unsaturated, partially unsaturated, or totally saturated; and being useful for treating muscle spasticity including hyperactive micturition, diarrhea, diuresis, withdrawal syndromes, pain including neuropathic pain, neurodegenerative diseases, memory and cognition deficits, psychoses including manic disorders and anxiety, hypertension, cardiac ischemia, congestive heart failure, and nasal congestion without sedating or cardiovascular side effects.

    摘要翻译： 具有肾上腺素能活性的化合物优先于α2A肾上腺素受体受体亚型，它们是α2B和α2C肾上腺素受体受体亚型中的一种或两种的选择性激动剂; 所述活性化合物选自具有式（I）的化合物，其中虚线代表任选的键，条件是两个双键可以不共享共同的碳原子; R是H或低级烷基; X是S或C（H）R 1，其中R 1是H或低级烷基，但当X和式（a）所代表的环之间的键是双键时，R 1不存在; Y是O，N，S，（CR12）y，其中y是1至3的整数，-CH = CH-或-Y1CH2-，其中Y1是O，N或S; x是1或2的整数，其中当R2，R3或R4与饱和碳原子结合时，x是1，当R2，R3或R4与饱和碳原子结合时，x是2; R2是H，低级烷基，卤素，羟基或低级烷氧基，或者当连接到饱和碳原子时，R2可以是氧代; R3和R4各自为H，低级烷基，羟基，低级烷氧基或苯基或一起为 - （C（R2）x）z-; -Y1（C（R2）x）的Z'-; -Y1（C（R2）x）的yY1-; - （C（R 2）x）的-Y 1 - （C（R 2）X） - ; - （C（R2）x）-Y1-（C（R2）x） - （C（R2）x） - 和-Y1-（C（R2）x）-Y1- z为3至5的整数，z'为2至4的整数，且x和y如上所定义，并且这些二价部分中的每一个的另一端可以连接至R3或R4以形成缩合 环结构并且形成的环可以是完全不饱和的，部分不饱和的或完全饱和的; 并且可用于治疗肌肉痉挛状态，包括过度排尿，腹泻，利尿，戒断综合征，疼痛包括神经性疼痛，神经变性疾病，记忆和认知缺陷，包括躁狂症和焦虑的精神病，高血压，心脏缺血，充血性心力衰竭和鼻充血 没有镇静或心血管副作用。

    Treatment of pain and other alpha 2 adrenergic-mediated conditions
    9.
    发明公开
    Treatment of pain and other alpha 2 adrenergic-mediated conditions 审中-公开
    疼痛和其他α-2肾上腺素beeinflüsste状态的治疗

    公开(公告)号：EP2335734A3

    公开(公告)日：2012-01-11

    申请号：EP11157644.3

    申请日：2004-08-19

    申请人： Allergan, Inc.

    发明人： Donello, John E. ,  Gil, Daniel W.

    IPC分类号： A61K45/06 ,  A61K31/4168 ,  A61K31/498 ,  A61K31/135 ,  A61K31/517 ,  A61K31/506 ,  A61P29/00 ,  A61K31/137

    CPC分类号： A61K45/06 ,  A61K31/135 ,  A61K31/137 ,  A61K31/4168 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  A61K2300/00

    摘要： The present invention provides the following components a) and b) for use in the treatment or prevention of pain in a mammal by co-administration of the components:
    a) a first component comprising a compound whose activity results in direct or indirect stimulation of alpha 2 adrenergic receptor activity, and
    b) a second component comprising an alpha 1 adrenergic receptor antagonist;

    wherein the dosage of the first component necessary to provide a given level of analgesia is less than that for a similarly affected mammal administered with the first component as the sole analgesic agent, or wherein the amount of sedation caused by the administration of a dose of the first component effective to cause half maximal analgesia is less than that caused in a similarly affected mammal administered with the first component in a dose effective to cause half maximal analgesia in the absence of the second component.