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39 条记录 (耗时 0.022 秒)

    Substituted aromatic ethers as inhibitors of glycine transport
    1.
    发明授权
    Substituted aromatic ethers as inhibitors of glycine transport 失效
    取代的芳香醚作为甘氨酸运输的抑制剂

    公开(公告)号：US06784299B2

    公开(公告)日：2004-08-31

    申请号：US10414736

    申请日：2003-04-16

    申请人： John A. Lowe, III

    发明人： John A. Lowe, III

    IPC分类号： C07D33202

    CPC分类号： C07D213/643 ,  C07C229/14 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/10 ,  C07D213/62 ,  C07D213/65 ,  C07D307/79 ,  C07D317/64 ,  C07D319/18

    摘要： This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

    摘要翻译： 本发明涉及一系列式I的取代芳醚，其中环A和X和Y如说明书中所定义，表现出作为甘氨酸转运抑制剂，其药学上可接受的盐，含有它们的药物组合物的活性及其用于 增强认知和治疗包括人类在内的哺乳动物精神分裂症和其他精神病的积极和消极症状。

    2-aminopyridines containing fused ring substituents
    3.
    发明授权
    2-aminopyridines containing fused ring substituents 失效
    含有稠环取代基的2-氨基吡啶

    公开(公告)号：US06211208B1

    公开(公告)日：2001-04-03

    申请号：US09504989

    申请日：2000-02-15

    申请人： John A. Lowe, III

    发明人： John A. Lowe, III

    IPC分类号： A61K3144

    CPC分类号： C07D213/73

    摘要： The present invention relates to 2-aminopyridine derivatives of the formula I: or pharmaceutically acceptable salts thereof, wherein A and B are each independently H, or together, A and B form a ring fused to the phenyl ring, said ring being saturated or unsaturated and containing from 5 to 7 ring member atoms, where said ring member atoms may optionally comprise from 1 to 2 heteroatoms selected independently from the group consisting of N, O or S, provided that no two adjacent ring members are heteroatoms; X is oxygen or a single bond; Y is (C1-C6)alkyl; R1 is hydrogen, (C1-C6)alkyl or a (C1-C6 alkyl) group substituted with —NR2R3 wherein R2 and R3 are either selected independently from the group consisting of H, alkyl, aryl, aralkyl or tetrahydronaphthalene, wherein said aryl group or said aryl moiety of said aralkyl group is phenyl or naphthyl, said alkyl group or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched, and said aryl group, said tetrahydronaphthalene or said aryl moiety of said aralkyl group is optionally substituted with from one to three of halogen, nitro, cyano, amino, (C1-C4)alkoxy and (C1-C4)alkylamino moieties, or R2 and R3 form, together with the nitrogen to which they are attached, a heterocyclic ring, or a cyclic or bicyclic ring which is saturated or unsaturated. The compounds of the invention have the ability to inhibit the activity of nitric oxide synthases (NOS), and hence, are useful in the treatment of diseases, conditions and disorders of the central nervous system, among others.

    摘要翻译： 本发明涉及式I的2-氨基吡啶衍生物或其药学上可接受的盐，其中A和B各自独立为H，或一起A和B形成稠合于苯环的环，所述环为饱和或不饱和的， 含有5至7个环成员原子，其中所述环成员原子可以任选地包含1至2个独立地选自N，O或S的杂原子，条件是没有两个相邻的环成员是杂原子; X是氧或一个 单键; Y是（C1-C6）烷基; R1是氢，（C1-C6）烷基或被-NR2R3取代的（C1-C6烷基）基团，其中R2和R3独立地选自H，烷基 芳基，芳烷基或四氢萘，其中所述芳烷基的所述芳基或所述芳基部分为苯基或萘基，所述烷基或所述芳烷基的所述烷基部分含有1至6个碳原子并且是直链或支链的， 说ar 所述四氢萘或所述芳烷基的所述芳基部分任选被1至3个卤素，硝基，氰基，氨基，（C 1 -C 4）烷氧基和（C 1 -C 4）烷基氨基部分取代，或R 2和R 3形式 与它们所连接的氮一起是杂环，或饱和或不饱和的环状或双环。 本发明的化合物具有抑制一氧化氮合酶（NOS）活性的能力，因此可用于治疗中枢神经系统的疾病，病症和病症等。

    NK-1 receptor antagonists for the treatment of neuronal injury and stroke
    8.
    发明授权
    NK-1 receptor antagonists for the treatment of neuronal injury and stroke 失效
    NK-1受体拮抗剂治疗神经元损伤和中风

    公开(公告)号：US06376507B1

    公开(公告)日：2002-04-23

    申请号：US09099289

    申请日：1998-06-18

    申请人： Robert B. Nelson ,  John A. Lowe, III

    发明人： Robert B. Nelson ,  John A. Lowe, III

    IPC分类号： A61K3144

    CPC分类号： A61K31/675 ,  A61K31/135 ,  A61K31/136 ,  A61K31/137 ,  A61K31/40 ,  A61K31/438 ,  A61K31/439 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/46 ,  A61K31/55

    摘要： The present invention relates to a method of treating or preventing a disorder selected from stroke, epilepsy, head trauma, spinal cord trauma, ischemic neuronal damage such as cerebral ischemic damage from stroke or vascular occlusion (e.g., during open heart surgery), excitotoxic neuronal damage (e.g., in stroke or epilepsy) and amyotrophic lateral sclerosis in mammals, including humans, using an NK-1 antagonist. It also relates to a method of treating or preventing such disorders in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds that are substance P receptor antagonists.

    摘要翻译： 本发明涉及一种治疗或预​​防选自中风，癫痫，头部创伤，脊髓创伤，缺血性神经元损伤如脑卒中或血管闭塞的脑缺血损伤（例如，开放心脏手术期间），兴奋性毒性神经元 使用NK-1拮抗剂的哺乳动物（包括人类）的损伤（例如中风或癫痫）和肌萎缩性侧索硬化。 它还涉及使用作为P受体拮抗剂的某些奎宁环衍生物，哌啶衍生物，吡咯烷衍生物，氮杂降冰片烷衍生物，乙二胺衍生物和相关化合物来治疗或预防哺乳动物包括人类的这种疾病的方法。