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    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
    4.
    发明授权
    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
    碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途

    公开(公告)号：US06696442B2

    公开(公告)日：2004-02-24

    申请号：US10178477

    申请日：2002-06-25

    申请人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin

    发明人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin

    IPC分类号： A61K3117

    CPC分类号： C07D213/643 ,  A61K31/17 ,  A61K31/175 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07C281/12 ,  C07C281/14 ,  C07C2601/14 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/58 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones 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), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基-82-。 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来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），用于治疗和预防 涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

    Substituted quinazolines and analogs and use thereof
    6.
    发明授权
    Substituted quinazolines and analogs and use thereof 有权
    取代的喹唑啉和类似物及其用途

    公开(公告)号：US06465472B1

    公开(公告)日：2002-10-15

    申请号：US09654839

    申请日：2000-09-01

    申请人： Ravi Upasani ,  Sui X. Cai ,  Nancy C. Lan ,  Yan Wang ,  George Field ,  David B. Fick

    发明人： Ravi Upasani ,  Sui X. Cai ,  Nancy C. Lan ,  Yan Wang ,  George Field ,  David B. Fick

    IPC分类号： C07D23726

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/82 ,  C07D249/08 ,  C07D491/04

    摘要： The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus. Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

    摘要翻译： 本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的新型喹唑啉和杂环，以及其用于治疗，预防或改善与中风，全身和局灶性缺血，CNS创伤，低血糖和手术相关的神经元损失以及治疗 或改善神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病，帕金森病和唐氏综合征，治疗，预防或改善兴奋性氨基酸过度刺激的不良后果，治疗，预防或改善焦虑，精神病，惊厥，慢性 疼痛，青光眼，视网膜炎，尿失禁，肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏症如精神分裂症，肌阵挛的不良后果。 阿尔茨海默病和营养不良和神经发育不良，以及认知和学习增强剂。

    Substituted 5-oxo-5,6,7,8-tetrahydro-4H-1-benzopyrans and benzothiopyrans and the use thereof as potentiators of AMPA
    7.
    发明授权
    Substituted 5-oxo-5,6,7,8-tetrahydro-4H-1-benzopyrans and benzothiopyrans and the use thereof as potentiators of AMPA 失效
    取代的5-氧代-5,6,7,8-四氢-4H-1-苯并吡喃和苯并噻喃并将其作为AMPA的增效剂

    公开(公告)号：US06680332B1

    公开(公告)日：2004-01-20

    申请号：US09980628

    申请日：2002-05-20

    申请人： Christopher S. Konkoy ,  David B. Fick ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana

    发明人： Christopher S. Konkoy ,  David B. Fick ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana

    IPC分类号： A61K4364

    CPC分类号： C07D311/74

    摘要： Disclosed is a method for treating a disorder responsive to the positive modulation of AMPA receptors in animals suffering therefrom, comprising administering to an animal in need thereof a compound of Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is NH2, NHR, and NHCOR; Z is O and S; and R1, R2, R3, R4, and X are defined herein. These compounds can be used as cognitive enhancers, for the treatment of neurodegenerative diseases, including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, AIDS associated dementia and Down's syndrome as well as for the treatment of schizophrenia and myoclonus. Also disclosed are pharmaceutical compositions useful for treating disorders responsive to the positive modulation of AMPA receptors, and novel compounds of Formula I.

    摘要翻译： 本发明公开了一种治疗患有AMPA受体AMPA受体阳性调节的病症的方法，其包括向有需要的动物施用式I化合物或其药学上可接受的盐或前药，其中：Y为NH 2， NHR和NHCOR; Z是O和S; 并且R1，R2，R3，R4和X在本文中定义。 这些化合物可用作认知增强剂，用于治疗神经变性疾病，包括阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿舞蹈病，帕金森病，AIDS相关性痴呆和唐氏综合征，以及治疗精神分裂症和肌阵挛。 还公开了可用于治疗对AMPA受体的正调节起反应的病症的药物组合物和式I的新化合物。

    Substituted 2-aminoacetamides and the use thereof
    8.
    发明授权
    Substituted 2-aminoacetamides and the use thereof 有权
    取代的2-氨基乙酰胺及其用途

    公开(公告)号：US06500825B2

    公开(公告)日：2002-12-31

    申请号：US09933203

    申请日：2001-08-21

    申请人： Nancy C. Lan ,  Yan Wang ,  Sui Xiong Cai

    发明人： Nancy C. Lan ,  Yan Wang ,  Sui Xiong Cai

    IPC分类号： A61K31445

    CPC分类号： C07C233/05 ,  A61K31/165 ,  C07C237/06 ,  C07C237/08 ,  C07C2601/14 ,  C07D211/46 ,  C07D213/65 ,  C07D213/68 ,  C07D215/20 ,  C07D239/34 ,  C07D241/08 ,  C07D309/12 ,  C07D317/64

    摘要： This invention is related to substituted 2-aminoacetamides represented by Formula II: or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1, R2, R3 and R4 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R5, R6 and R7 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R5, is defined as above, and R6 and R7 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR8, CH2, C(O), NR8C(O), C(O)NR8, SO, SO2 or a covalent bond; where R8 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n is 0, 1, 2 or 3. The invention also is directed to the use substituted 2-aminoacetamides 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 pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

    摘要翻译： 本发明涉及由式II表示的取代的2-氨基乙酰胺或其药学上可接受的盐或前药，其中：R 1，R 2，R 3和R 4独立地为氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基， 羟烷基，烷氧基烷基或羧基烷基; R5，R6和R7独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基，或R5如上所定义，R 6和R 7与它们所在的氮原子一起 连接形成杂环，包括哌啶，哌嗪，吗啉; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR8，CH2，C（O），NR8C（O），C（O）NR8，SO，SO2或共价键; 其中R8是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 本发明还涉及使用取代的2-氨基乙酰胺用于治疗全身和局灶性缺血后的神经元损伤，用于治疗或预防神经变性病症如肌萎缩性侧索硬化（ALS） ，作为抗惊厥药，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的治疗，预防或改善。

    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
    9.
    发明授权
    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 有权
    碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途

    公开(公告)号：US06458843B1

    公开(公告)日：2002-10-01

    申请号：US09421403

    申请日：1999-10-21

    申请人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin ,  Eckard Weber

    发明人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin ,  Eckard Weber

    IPC分类号： A61K3117

    CPC分类号： C07D213/643 ,  A61K31/17 ,  A61K31/175 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07C281/12 ,  C07C281/14 ,  C07C2601/14 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/58 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones 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), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来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），用于治疗和预防 涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。