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13 条记录 (耗时 0.02 秒)

    Neuroactive steroids of the androstane and pregnane series
    4.
    发明授权
    Neuroactive steroids of the androstane and pregnane series 失效
    雄激素和孕烷系列的神经活性类固醇

    公开(公告)号：US5925630A

    公开(公告)日：1999-07-20

    申请号：US659192

    申请日：1996-06-06

    申请人： Ravindra B. Upasani ,  David B. Fick ,  Derk J. Hogenkamp ,  Nancy C. Lan

    发明人： Ravindra B. Upasani ,  David B. Fick ,  Derk J. Hogenkamp ,  Nancy C. Lan

    IPC分类号： A61K31/565 ,  A61K31/57 ,  A61P25/00 ,  C07J1/00 ,  C07J5/00 ,  C07J17/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  A61K31/56

    CPC分类号： C07J31/006 ,  C07J1/0007 ,  C07J1/0029 ,  C07J1/0055 ,  C07J1/0077 ,  C07J17/00 ,  C07J21/00 ,  C07J41/0005 ,  C07J41/005 ,  C07J43/003

    摘要： The invention relates to 3.alpha.-hydroxy, 17-(un)substituted derivatives of the androstane series and 3.alpha.-hydroxy, 21-substituted derivatives of the pregnane series. These derivatives are capable of acting at a recently identified site on the GRC, thereby modulating brain excitability in a manner that will alleviate stress, anxiety, insomnia, mood disorders that are amenable to GRC-active agents (such as depression) and seizure activity. The steroid derivatives of this invention are those having the general structural Formula: ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9 and R.sub.10 are further defined herein and the dotted lines are single or double bonds. The structure includes androstanes, pregnanes (R.sub.4 =methyl), 19-norandrostanes, and norpregnanes (R.sub.4 =H).

    摘要翻译： 本发明涉及雄甾烷基系列的3α-羟基，17-（未）取代衍生物和孕烷系列的3α-羟基，21-取代衍生物。 这些衍生物能够在最近确定的GRC位点起作用，从而以减轻压力，焦虑，失眠，舒适于GRC活性剂（如抑郁症）和癫痫发作活动的情绪障碍的方式调节脑兴奋性。 本发明的类固醇衍生物是具有以下结构式的化合物：其中R，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10在本文中进一步定义，虚线是单键或双键。 该结构包括雄甾烷，孕烷（R4 =甲基），19-去雄孕烷和诺孕烷（R4 = H）。

    Process for synthesis of steroidal allylic tert. alcohols
    5.
    发明授权
    Process for synthesis of steroidal allylic tert. alcohols 失效
    合成甾体烯丙基化合物的方法 醇类

    公开(公告)号：US5449795A

    公开(公告)日：1995-09-12

    申请号：US195719

    申请日：1994-02-14

    申请人： Derk J. Hogenkamp

    发明人： Derk J. Hogenkamp

    IPC分类号： C07J7/00 ,  C07J13/00 ,  C07J17/00 ,  C07J31/00 ,  C07J75/00

    CPC分类号： C07J31/006 ,  C07J13/007 ,  C07J17/00 ,  C07J7/002

    摘要： A method for the preparation of a steroidal allylic tertiary alcohol is disclosed which involves the deprotonation of a sulfoxide with a strong base which is capable of deprotonating the methine proton which is .alpha. to the sulfoxide, in an inert solvent to give the anion; reaction of the anion with a steroidal spiro-2'-oxirane to give a steroidal .gamma.-hydroxysulfoxide; and thermolysis in the presence of a base other than calcium carbonate to give the steroidal allylic tertiary alcohol.

    摘要翻译： 公开了一种制备甾族烯丙基叔醇的方法，该方法涉及一种具有强碱的亚砜的去质子化，所述强碱能够在惰性溶剂中使亚砜的亚甲基次甲基质子脱质子得到阴离子; 阴离子与甾体螺-2'-环氧乙烷的反应得到甾体γ-羟基亚砜; 并在除碳酸钙之外的碱存在下热解，得到甾族烯丙基叔醇。

    Aryl substituted pyrazoles, triazoles, and tetrazoles, and the use thereof
    10.
    发明授权
    Aryl substituted pyrazoles, triazoles, and tetrazoles, and the use thereof 有权
    芳基取代的吡唑，三唑和四唑，及其用途

    公开(公告)号：US07078426B2

    公开(公告)日：2006-07-18

    申请号：US09814123

    申请日：2001-03-22

    申请人： Derk J. Hogenkamp ,  Phong Nguyen ,  Ji Yang

    发明人： Derk J. Hogenkamp ,  Phong Nguyen ,  Ji Yang

    IPC分类号： A61K31/4155 ,  C07D231/10

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R8 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

    摘要翻译： 本发明涉及具有式I化合物或其药学上可接受的盐，前药或溶剂化物，其中Het和R 5 -R 8被定义在说明书中。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途 作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。