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27 条记录 (耗时 0.049 秒)

    Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
    22.
    发明申请
    Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof 审中-公开

    公开(公告)号：US20060111386A1

    公开(公告)日：2006-05-25

    申请号：US11284330

    申请日：2005-11-21

    申请人： Bruce Molino ,  Barry Berkowitz ,  Marlene Cohen

    发明人： Bruce Molino ,  Barry Berkowitz ,  Marlene Cohen

    IPC分类号： A61K31/4745

    CPC分类号： A61K31/4745

    摘要： The present invention relates to a method of treating disorders including cognition impairment, generalized anxiety disorder, acute stress disorder, social phobia, simple phobias, pre-menstrual dysphoric disorder, social anxiety disorder, major depressive disorder, eating disorders, obesity, anorexia nervosa, bulimia nervosa, binge eating disorder, substance abuse disorders, chemical dependencies, nicotine addiction, cocaine addiction, alcohol addiction, amphetamine addiction, Lesch-Nyhan syndrome, neurodegenerative diseases, late luteal phase syndrome, narcolepsy, psychiatric symptoms anger, rejection sensitivity, movement disorders, extrapyramidal syndrome, Tic disorder, restless leg syndrome, tardive dyskinesia, sleep related eating disorder, night eating syndrome, stress urinary incontinence, migraine, neuropathic pain, diabetic neuropathy, fibromyalgia syndrome, chronic fatigue syndrome, sexual dysfunction, premature ejaculation, and male impotence. This method involves administering to a patient in need of such treatment a therapeutically effective amount of a disclosed compound. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.

    NOVEL PROCESSES FOR STEREOSELECTIVE SYNTHESIS OF TRANS ISATX247
    23.
    发明申请
    NOVEL PROCESSES FOR STEREOSELECTIVE SYNTHESIS OF TRANS ISATX247 有权
    用于ISATX247的立体选择性合成的新方法

    公开(公告)号：US20080021197A1

    公开(公告)日：2008-01-24

    申请号：US11572833

    申请日：2005-07-26

    申请人： Bruce Molino ,  Zhicai Yang ,  Jun-Ho Maeng ,  David Manning

    发明人： Bruce Molino ,  Zhicai Yang ,  Jun-Ho Maeng ,  David Manning

    IPC分类号： C07K7/64

    CPC分类号： C07K7/645

    摘要： The present invention relates to a process for preparation of a trans ISATX247 compound of the formula: where R1═H or D; R2═H or D; and R3═H or D, by application of organozirconium chemistry. The process involves reacting an acetyl cyclosporin aldehyde with an organozirconium reagent to provide acetyl cyclosporin diene (the acetate of trans ISATX247) and deacetylating the acetyl cyclosporin diene to produce the trans-isomer of ISATX247. The present invention also relates to a process for preparing the same trans ISATX 247 compound, using olefin cross metathesis. The process involves: olefin cross metathesis of acetyl cyclosporin A to afford acetyl cyclosporin α,β-unsaturated aldehyde; Wittig reaction of the acetyl cyclosporin α,β-unsaturated aldehyde to provide acetyl cyclosporin diene; and deacetylation of the acetyl cyclosporin diene to produce the trans ISATX247 compound. Also disclosed are processes for preparing an acetyl cyclosporin α,β-unsaturated aldehyde compound and a cyclosporin triene analogue compound.

    摘要翻译： 本发明涉及制备下式的反式ISA 247化合物的方法：其中R 1 -H或D; R 2 -H或D; 和R 3 -H或D，通过应用有机锆化学。 该方法包括使乙酰环孢菌素醛与有机锆试剂反应以提供乙酰环孢菌素二烯（反式ISA 247的乙酸酯）和乙酰环己烷二烯的脱乙酰化产生ISA的反式异构体 TX 247。 本发明还涉及使用烯烃交叉复分解制备相同的反式异构体化合物247的方法。 该方法包括：乙酰环孢菌素A的烯烃交叉复分解，得到乙酰环孢菌素α，β-不饱和醛; 乙酰环孢菌素α，β-不饱和醛维甲酸反应提供乙酰环孢菌素二烯; 和乙酰环孢菌素二烯的脱乙酰化以产生反式ISAX 247化合物。 还公开了制备乙酰环孢菌素α，β-不饱和醛化合物和环孢菌素三烯类似物化合物的方法。

    Use of cyclosporin alkene analogues for preventing or treating viral-induced disorders
    24.
    发明申请
    Use of cyclosporin alkene analogues for preventing or treating viral-induced disorders 审中-公开
    使用环孢菌素烯类似物来预防或治疗病毒性疾病

    公开(公告)号：US20070232532A1

    公开(公告)日：2007-10-04

    申请号：US11391027

    申请日：2006-03-28

    申请人： Bruce Molino

    发明人： Bruce Molino

    IPC分类号： A61K38/13

    CPC分类号： A61K38/13 ,  A61K38/212 ,  A61K2300/00

    摘要： The present invention relates to methods of preventing or treating a mammal with a viral-induced disorder. The method involves administering to the mammal a therapeutically effective amount of a compound represented by Formula I, as shown below: or a pharmaceutically acceptable salt thereof, with X, R0, R1, and R2 defined herein, under conditions effective to prevent or treat the viral-induced disorder.

    摘要翻译： 本发明涉及用病毒诱导的病症预防或治疗哺乳动物的方法。 该方法包括向哺乳动物施用治疗有效量的由式I表示的化合物，如下所示：或其药学上可接受的盐，其中X，R 0，R 1， 在本文定义的条件下，在有效预防或治疗病毒诱导的病症的条件下。

    Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof
    26.
    发明申请
    Novel 4-phenyl substituted tetrahydroisoquinolines and therapeutic use thereof 审中-公开
    新型4-苯基取代的四氢异喹啉及其治疗用途

    公开(公告)号：US20060111385A1

    公开(公告)日：2006-05-25

    申请号：US10994706

    申请日：2004-11-22

    申请人： Bruce Molino ,  Barry Berkowitz ,  Marlene Cohen

    发明人： Bruce Molino ,  Barry Berkowitz ,  Marlene Cohen

    IPC分类号： A61K31/4745

    CPC分类号： A61K31/4745

    摘要： The present invention relates to a method of treating disorders including cognition impairment, generalized anxiety disorder, acute stress disorder, social phobia, simple phobias, pre-menstrual dysphoric disorder, social anxiety disorder, major depressive disorder, eating disorders, obesity, anorexia nervosa, bulimia nervosa, binge eating disorder, substance abuse disorders, chemical dependencies, nicotine addiction, cocaine addiction, alcohol addiction, amphetamine addiction, Lesch-Nyhan syndrome, neurodegenerative diseases, late luteal phase syndrome, narcolepsy, psychiatric symptoms anger, rejection sensitivity, movement disorders, extrapyramidal syndrome, Tic disorder, restless leg syndrome, tardive dyskinesia, sleep related eating disorder, night eating syndrome, stress urinary incontinence, migraine, neuropathic pain, diabetic neuropathy, fibromyalgia syndrome, chronic fatigue syndrome, sexual dysfunction, premature ejaculation, and male impotence. This method involves administering to a patient in need of such treatment a therapeutically effective amount of a disclosed compound. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.

    摘要翻译： 本发明涉及一种治疗包括认知障碍，广泛性焦虑症，急性应激障碍，社交恐惧症，简单恐怖症，月经前焦虑症，社会焦虑症，重度抑郁症，进食障碍，肥胖症，神经性厌食症， 癫痫症，神经性贪食症，暴饮暴食症，药物滥用障碍，化学依赖性，尼古丁成瘾，可卡因成瘾，酒精成瘾，安非他明成瘾，Lesch-Nyhan综合征，神经变性疾病，晚黄体期综合征，发作性睡眠，精神症状愤怒，排斥反应，运动障碍 ，锥体外综合征，Tic障碍，不宁腿综合征，迟发性运动障碍，睡眠相关饮食障碍，夜间饮食综合征，压力性尿失禁，偏头痛，神经性疼痛，糖尿病性神经病，纤维肌痛综合征，慢性疲劳综合征，性功能障碍，早泄和男性 阳。 该方法包括向需要这种治疗的患者施用治疗有效量的所公开的化合物。 这样的化合物是如本文所述的具有式IA，IB，IIA，IIB，IIIA或IIIC的4-苯基取代的四氢异喹啉。