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    N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF
    1.
    发明申请
    N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 失效
    N-ARYL DIAZASPIROCYCLIC化合物及其制备和使用方法

    公开(公告)号：US20060217406A1

    公开(公告)日：2006-09-28

    申请号：US11423471

    申请日：2006-06-12

    申请人： Balwinder Bhatti ,  Craig Miller ,  Jeffrey Schmitt

    发明人： Balwinder Bhatti ,  Craig Miller ,  Jeffrey Schmitt

    IPC分类号： C07D471/10 ,  A61K31/4747

    CPC分类号： C07D487/20 ,  C07D453/02 ,  C07D471/10 ,  C07D471/20 ,  C07D487/10

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。 化合物是N-芳基二氮杂螺环化合物，N-杂芳基二氮杂螺环化合物的桥连类似物，或这些化合物的前药或代谢物。 芳基可以是五元或六元杂环（杂芳基）。 化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。 其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。 化合物和组合物也可用于缓解疼痛。 化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（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以及对骨骼肌的显着影响）。

    N-ARYL AZASPIROALKENE AND AZASPIROALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF
    4.
    发明申请
    N-ARYL AZASPIROALKENE AND AZASPIROALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 失效
    N-ARYL AZASPIROALKENE和AZASPIROALKANE化合物及其制备和使用方法

    公开(公告)号：US20080242689A1

    公开(公告)日：2008-10-02

    申请号：US12117946

    申请日：2008-05-09

    申请人： Balwinder Bhatti ,  Scott R. Breining ,  Philip S. Hammond ,  Jozef Klucik ,  Yun-De Xiao

    发明人： Balwinder Bhatti ,  Scott R. Breining ,  Philip S. Hammond ,  Jozef Klucik ,  Yun-De Xiao

    IPC分类号： A61K31/4427 ,  A61P25/00 ,  A61K31/4439

    CPC分类号： C07D413/04 ,  C07D401/04

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。 化合物是N-芳基或杂芳基氮杂螺烯/烷烃化合物，这些化合物的前药或代谢物，或其药学上可接受的盐。 芳基可以是苯环或五元或六元杂环（杂芳基）。 化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。 其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。 化合物和组合物也可用于缓解疼痛。 化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（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以及对骨骼肌的显着影响）。

    Use of N-aryl diazaspiracyclic compounds in the treatment of addiction
    5.
    发明申请
    Use of N-aryl diazaspiracyclic compounds in the treatment of addiction 审中-公开
    使用N-芳基二氮杂环环化合物治疗成瘾

    公开(公告)号：US20060058328A1

    公开(公告)日：2006-03-16

    申请号：US11207102

    申请日：2005-08-18

    申请人： Balwinder Bhatti ,  Gregory Gatto ,  Jozef Klucik

    发明人： Balwinder Bhatti ,  Gregory Gatto ,  Jozef Klucik

    IPC分类号： A61K31/4747

    CPC分类号： A61K31/4747 ,  A61K31/435 ,  A61K31/438 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506

    摘要： Compounds, compositions and methods for treating drug addiction, nicotine addiction, and/or obesity are disclosed. The compounds are N-aryl diazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five- or six-membered heterocyclic ring (heteroaryl). The compounds are effective at inhibiting dopamine production and/or secretion, and accordingly are effective at inhibiting the physiological “reward” process that is associated with ingestion of nicotine and/or illicit drugs. The compounds and compositions can be administered in effective amounts to inhibit dopamine release, without resulting in appreciable adverse side effects (e.g., side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastro-intestinal tract, and significant effects upon skeletal muscle).

    摘要翻译： 公开了用于治疗药物成瘾，尼古丁成瘾和/或肥胖的化合物，组合物和方法。 化合物是N-芳基二氮杂螺环化合物，N-杂芳基二氮杂螺环化合物的桥连类似物，或这些化合物的前药或代谢物。 芳基可以是五元或六元杂环（杂芳基）。 这些化合物有效抑制多巴胺的产生和/或分泌，因此有效地抑制与摄取尼古丁和/或非法药物相关的生理“奖赏”过程。 化合物和组合物可以以有效量施用以抑制多巴胺释放，而不导致明显的不良副作用（例如，副作用，例如血压和心率的显着升高，对胃肠道的显着的负面影响，以及显着的 对骨骼肌的影响）。

    N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof
    8.
    发明授权
    N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof 失效
    N-芳基氮杂螺烯和氮杂环烷烃化合物及其制备方法和用途

    公开(公告)号：US07754708B2

    公开(公告)日：2010-07-13

    申请号：US12117946

    申请日：2008-05-09

    申请人： Balwinder Bhatti ,  Scott R. Breining ,  Philip S. Hammond ,  Jozef Klucik ,  Yun-De Xiao

    发明人： Balwinder Bhatti ,  Scott R. Breining ,  Philip S. Hammond ,  Jozef Klucik ,  Yun-De Xiao

    IPC分类号： A61K31/4406 ,  A61K31/4418 ,  A61K31/397 ,  A61P25/22 ,  A61P25/24

    CPC分类号： C07D413/04 ,  C07D401/04

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。 化合物是N-芳基或杂芳基氮杂螺烯/烷烃化合物，这些化合物的前药或代谢物，或其药学上可接受的盐。 芳基可以是苯环或五元或六元杂环（杂芳基）。 化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。 其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。 化合物和组合物也可用于缓解疼痛。 化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（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以及对骨骼肌的显着影响）。

    N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof
    9.
    发明申请
    N-aryl azaspiroalkene and azaspiroalkane compounds and methods of preparation and use thereof 失效
    N-芳基氮杂螺烯和氮杂环烷烃化合物及其制备方法和用途

    公开(公告)号：US20060074067A1

    公开(公告)日：2006-04-06

    申请号：US11230140

    申请日：2005-09-19

    申请人： Balwinder Bhatti ,  Scott Breining ,  Philip Hammond ,  Jozef Klucik ,  Yun-De Xiao

    发明人： Balwinder Bhatti ,  Scott Breining ,  Philip Hammond ,  Jozef Klucik ,  Yun-De Xiao

    IPC分类号： A61K31/4747 ,  C07D471/10

    CPC分类号： C07D413/04 ,  C07D401/04

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or a five- or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic cholinergic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. 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 gastro-intestinal 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。 化合物是N-芳基或杂芳基氮杂螺烯/烷烃化合物，这些化合物的前药或代谢物，或其药学上可接受的盐。 芳基可以是苯环或五元或六元杂环（杂芳基）。 化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。 其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。 化合物和组合物也可用于缓解疼痛。 化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（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以及对骨骼肌的显着影响）。