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    Pro-Neurogenic Compounds
    6.
    发明申请
    Pro-Neurogenic Compounds 有权
    前神经源性化合物

    公开(公告)号：US20140057900A1

    公开(公告)日：2014-02-27

    申请号：US13974642

    申请日：2013-08-23

    申请人： Board of Regents of The University of Texas System

    发明人： Steven L. McKnight ,  Andrew A. Pieper ,  Joseph M. Ready ,  Enrique Fernandez

    IPC分类号： C07D471/04 ,  C07D403/06 ,  C07D209/90 ,  C07D405/06 ,  C07D223/24 ,  C07D487/04

    CPC分类号： C07D471/04 ,  A61K31/403 ,  A61K31/519 ,  A61K31/55 ,  C07D209/90 ,  C07D223/24 ,  C07D403/06 ,  C07D405/06 ,  C07D487/04

    摘要： Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.

    摘要翻译： 本文公开了用于刺激神经发生（例如，产后神经发生，包括产后海马和下丘脑神经发生）和/或保护神经细胞免于细胞死亡的化合物和方法。 体内活性测试表明，这些化合物可能在神经精神和/或神经变性疾病如精神分裂症，主要抑郁症，双相性精神障碍，正常衰老，癫痫，创伤性脑损伤，创伤后应激障碍，帕金森病，阿尔茨海默病， 唐氏综合征，脊髓小脑性共济失调，肌萎缩性侧索硬化，亨廷顿病，中风，放射治疗，慢性应激，神经活性药物滥用，视网膜变性，脊髓损伤，周围神经损伤，与各种病症相关的生理体重减轻 作为与正常老化，化学疗法等相关的认知衰退。

    Condensed indoline derivatives and their use as 5HT , in particular 5hHT2c, receptor ligands
    9.
    发明申请
    Condensed indoline derivatives and their use as 5HT , in particular 5hHT2c, receptor ligands 失效
    缩合二氢吲哚衍生物及其用作5HT，特别是5hHT2c受体配体

    公开(公告)号：US20070105889A1

    公开(公告)日：2007-05-10

    申请号：US11637042

    申请日：2006-12-12

    申请人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn ,  David Adams

    发明人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn ,  David Adams

    IPC分类号： A61K31/4745 ,  A61K31/403

    CPC分类号： C07D471/04 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4745 ,  C07D209/60 ,  C07D209/70 ,  C07D209/90 ,  C07D471/06 ,  C07D491/04 ,  C07D491/06 ,  C07D495/04 ,  C07D495/06

    摘要： A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2C receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    摘要翻译： 式（I）的化合物，其中R 1和R 2各自独立地选自氢和烷基; R 3是烷基; R 4和R 5选自氢和烷基; R 6和R 7独立地选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基亚砜基，硝基，腈 ，碳 - 烷氧基，碳 - 芳氧基和羧基; 并且A是任选地含有一个或多个杂原子的5-或6-元环，其中除了环A稠合的苯环的不饱和碳原子之外的环A的原子是饱和或不饱和的， 可接受的盐，加成化合物和前药; 以及其在治疗中的用途，特别是作为5HT受体，特别是5HT 2C受体的激动剂或拮抗剂，例如用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。

    Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands
    10.
    发明申请
    Condensed indoline derivatives and their use as 5HT, in particular 5HT2C, receptor ligands 失效
    缩合二氢吲哚衍生物及其用作5HT，特别是5HT2C受体配体

    公开(公告)号：US20070099981A1

    公开(公告)日：2007-05-03

    申请号：US11637082

    申请日：2006-12-12

    申请人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn

    发明人： Jonathan Richard Roffey ,  James Edward Davidson ,  Howard Mansell ,  Richard Hamlyn

    IPC分类号： A61K31/403

    CPC分类号： C07D471/04 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4745 ,  C07D209/60 ,  C07D209/70 ,  C07D209/90 ,  C07D471/06 ,  C07D491/04 ,  C07D491/06 ,  C07D495/04 ,  C07D495/06

    摘要： A chemical compound of formula (I) wherein R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 and R5 are selected from hydrogen and alkyl; R6 and R7 are independently selected from hydrogen, halogen, hydroxyl, alkyl, aryl, amino, alkylamino, dialkylamino, alkoxy, aryloxy, alkylthio, alkylsulfoxyl, nitro, carbonitrile, carbo-alkoxy, carbo-aryloxy and carboxyl; and A is a 5- or 6-membered ring optionally containing one or more heteroatoms wherein the atoms of the ring A, other than the unsaturated carbon atoms of the phenyl ring to which the ring A is fused, are saturated or unsaturated, and pharmaceutically acceptable salts, addition compounds and prodrugs thereof; and the use thereof in therapy, particularly as an agonist or antagonist of a 5HT receptor, particularly a 5HT2c receptor, for instance in the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity.

    摘要翻译： 式（I）的化合物，其中R 1和R 2各自独立地选自氢和烷基; R 3是烷基; R 4和R 5选自氢和烷基; R 6和R 7独立地选自氢，卤素，羟基，烷基，芳基，氨基，烷基氨基，二烷基氨基，烷氧基，芳氧基，烷硫基，烷基亚砜基，硝基，腈 ，碳 - 烷氧基，碳 - 芳氧基和羧基; 并且A是任选地含有一个或多个杂原子的5-或6-元环，其中除了环A稠合的苯环的不饱和碳原子之外的环A的原子是饱和或不饱和的， 其可接受的盐，加成化合物和前药; 以及其在治疗中的用途，特别是作为5HT受体，特别是5HT 2C受体的激动剂或拮抗剂，例如用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖。