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12 条记录 (耗时 0.021 秒)

    Sub-type selective amides of diazabicycloalkanes
    1.
    发明授权
    Sub-type selective amides of diazabicycloalkanes 失效
    二氮杂双环烷烃的亚型选择性酰胺

    公开(公告)号：US08268860B2

    公开(公告)日：2012-09-18

    申请号：US12723790

    申请日：2010-03-15

    申请人： Anatoly A. Mazurov ,  Lan Miao ,  Yun-De Xiao ,  Philip S. Hammond ,  Craig H. Miller ,  Srinivisa Rao Akireddy ,  V. Srinivasa Murthy ,  Regina C. Whitaker ,  Scott R. Breining ,  Matt S. Melvin

    发明人： Anatoly A. Mazurov ,  Lan Miao ,  Yun-De Xiao ,  Philip S. Hammond ,  Craig H. Miller ,  Srinivisa Rao Akireddy ,  V. Srinivasa Murthy ,  Regina C. Whitaker ,  Scott R. Breining ,  Matt S. Melvin

    IPC分类号： A61K43/42 ,  A01N31/44

    CPC分类号： C07D487/04 ,  C07D471/08

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. The compounds can: (i) alter the number of nicotinic cholinergic receptors of the brain of the patient, (ii) exhibit neuroprotective effects, and (iii) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).

    摘要翻译： 公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。 这些化合物是可以由某些杂芳基羧酸和某些二氮杂双环烷烃制备的酰胺化合物。 该化合物对中枢神经系统（CNS）中α4和bgr2亚型的神经元烟碱受体表现出选择性并且以高亲和力结合。 化合物和组合物可用于治疗和/或预防多种病症或病症，特别是CNS疾病。 化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示神经保护作用，和（iii）当以有效量使用时，不会产生明显的副作用（例如副作用 因为血压和心率的显着增加，对胃肠道的显着的负面影响和对骨骼肌的显着影响）。

    Pharmaceutical Compositions and Methods for Relieving Pain and Treating Central Nervous System Disorders
    2.
    发明申请
    Pharmaceutical Compositions and Methods for Relieving Pain and Treating Central Nervous System Disorders 审中-公开
    减轻疼痛和治疗中枢性神经系统疾病的药物组合物和方法

    公开(公告)号：US20080242693A1

    公开(公告)日：2008-10-02

    申请号：US12123530

    申请日：2008-05-20

    申请人： Scott R. Breining ,  Balwinder S. Bhatti ,  Gregory D. Hawkins ,  Lan Miao ,  Anatoly Mazurov ,  Craig H. Miller

    发明人： Scott R. Breining ,  Balwinder S. Bhatti ,  Gregory D. Hawkins ,  Lan Miao ,  Anatoly Mazurov ,  Craig H. Miller

    IPC分类号： A61K31/439 ,  A61P25/30

    CPC分类号： C07D221/22 ,  C07D401/04

    摘要： Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

    摘要翻译： 特征在于正常神经递质释放（如多巴胺释放（如帕金森综合征，帕金森氏病，图雷特氏综合征，注意缺陷障碍或精神分裂症））改变的中枢神经系统疾病易患或患有疾病的患者是 通过施用如本文所述的式1或2的化合物进行治疗。 式1和式2化合物也可用于治疗疼痛，治疗药物成瘾，尼古丁成瘾和/或肥胖症。 该化合物可作为单独的立体异构体，外消旋混合物，非对映异构体等存在。

    (3-(5-ethoxypyridin)yl)-alkenyl 1 amine compounds
    6.
    发明授权
    (3-(5-ethoxypyridin)yl)-alkenyl 1 amine compounds 失效
    （3-（5-乙氧基吡啶）基） - 烯基1胺化合物

    公开(公告)号：US5616716A

    公开(公告)日：1997-04-01

    申请号：US631762

    申请日：1996-04-23

    申请人： Gary M. Dull ,  William S. Caldwell ,  Craig H. Miller

    发明人： Gary M. Dull ,  William S. Caldwell ,  Craig H. Miller

    IPC分类号： A61K31/44 ,  C07D213/65 ,  C07D213/02

    CPC分类号： C07D213/65 ,  A61K31/44

    摘要： Patients susceptible to or suffering from central nervous system disorders are treated by administering an effective amount of an aryl substituted olefinic amine compound. Exemplary compounds are (E)-4-[3-(5-ethoxypyridin)yl]-3-butene-1-amine, (E)-N-methyl-4-[3-(5-ethoxyrindin)yl]-3-buten-1-amine.

    摘要翻译： 通过施用有效量的芳基取代的烯烃胺化合物来治疗易患或患有中枢神经系统疾病的患者。 示例性化合物是（E）-4- [3-（5-乙氧基吡啶）基] -3-丁烯-1-胺，（E）-N-甲基-4- [3-（5-乙氧基茚啉）基] -3 丁烯-1-胺。

    ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF
    7.
    发明申请
    ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 有权
    阿维林霉素化合物及其制备和使用方法

    公开(公告)号：US20100267776A1

    公开(公告)日：2010-10-21

    申请号：US12683106

    申请日：2010-01-06

    申请人： Arielle Genevois-Borella ,  Craig H. Miller

    发明人： Arielle Genevois-Borella ,  Craig H. Miller

    IPC分类号： A61K31/4439 ,  A61P25/28 ,  A61P25/16 ,  A61P25/14 ,  A61P25/24 ,  A61P25/22 ,  A61P1/00 ,  A61P25/30 ,  A61P29/00

    CPC分类号： A61K31/506 ,  C07D405/14

    摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

    摘要翻译： 公开了式（I）的新型乙烯基氮杂环烷化合物。 这些化合物是各种nAChR的配体。 化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。 可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。 化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

    Arylvinylazacycloalkane compounds and methods of preparation and use thereof
    9.
    发明授权
    Arylvinylazacycloalkane compounds and methods of preparation and use thereof 有权

    公开(公告)号：US08067443B2

    公开(公告)日：2011-11-29

    申请号：US12683106

    申请日：2010-01-06

    申请人： Arielle Genevois-Borella ,  Craig H. Miller

    发明人： Arielle Genevois-Borella ,  Craig H. Miller

    IPC分类号： A61K31/351 ,  C07D401/02

    CPC分类号： A61K31/506 ,  C07D405/14

    摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

    Salt forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)y1]-4-penten 2-amine
    10.
    发明授权
    Salt forms of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)y1]-4-penten 2-amine 失效
    （2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）y1] -4-戊烯-2-胺的盐形式

    公开(公告)号：US08017785B2

    公开(公告)日：2011-09-13

    申请号：US12299925

    申请日：2007-05-08

    申请人： Caroline Ericsson ,  Martin Bohlin ,  Tesfai Sebhatu ,  Gary M. Dull ,  Julio A. Munoz ,  Craig H. Miller

    发明人： Caroline Ericsson ,  Martin Bohlin ,  Tesfai Sebhatu ,  Gary M. Dull ,  Julio A. Munoz ,  Craig H. Miller

    IPC分类号： A61P25/18 ,  A61P29/28 ,  A61P25/00

    CPC分类号： C07D213/65

    摘要： Phosphoric acid, edisylic acid (1,2-ethanedisulfonic acid), citric acid, orotic acid (uracil-6-carboxylic acid), R-mandelic acid, sulfuric acid, 1,5-naphthalenedisulfonic acid, D-aspartic acid, and lysine monohydrochloride salts of (2S)-(4E)-N-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine, and methods for their preparation, pharmaceutical compositions comprising said salts, and use, are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.

    摘要翻译： 磷酸，乙二酸（1,2-乙烷二磺酸），柠檬酸，乳清酸（尿嘧啶-6-羧酸），R-扁桃酸，硫酸，1,5-萘二磺酸，D-天冬氨酸和赖氨酸 （2S） - （4E）-N-甲基-5- [3-（5-异丙氧基吡啶）基] -4-戊烯-2-胺的单盐酸盐及其制备方法，包含所述盐的药物组合物和用途 ，被披露。 盐可以施用于易患或患有诸如中枢神经系统疾病的病症和障碍的患者，以治疗和/或预防这些疾病。