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    Arylbicyclo[3.1.0]hexylamines and methods and compositions for their preparation and use
    2.
    发明授权
    Arylbicyclo[3.1.0]hexylamines and methods and compositions for their preparation and use 有权
    芳基二环[3.1.0]己胺及其制备和使用的方法和组合物

    公开(公告)号：US08138377B2

    公开(公告)日：2012-03-20

    申请号：US11936016

    申请日：2007-11-06

    申请人： Phil Skolnick ,  Zhengming Chen ,  Ji Yang

    发明人： Phil Skolnick ,  Zhengming Chen ,  Ji Yang

    IPC分类号： C07C211/00

    CPC分类号： C07C211/41 ,  C07C2602/18

    摘要： The invention provides novel arylbicyclo[3.1.0]hexylamines, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including but not limited to depression and anxiety.

    摘要翻译： 本发明提供新的芳基双环[3.1.0]己胺，以及用于制备这些化合物的相关方法和中间体，以及使用这些化合物治疗和/或预防中枢神经系统（CNS）障碍的组合物和方法，包括但不限于 局限于抑郁和焦虑。

    Compositions and Methods for Treatment of Chronic Pain Conditions
    3.
    发明申请
    Compositions and Methods for Treatment of Chronic Pain Conditions 审中-公开
    治疗慢性疼痛病症的组合物和方法

    公开(公告)号：US20080014272A1

    公开(公告)日：2008-01-17

    申请号：US11775721

    申请日：2007-07-10

    申请人： Phil Skolnick ,  Warren Stern

    发明人： Phil Skolnick ,  Warren Stern

    IPC分类号： A61K31/403 ,  A61K31/19 ,  A61K31/44 ,  A61K9/00 ,  A61P19/00 ,  A61P19/02

    CPC分类号： A61K31/19 ,  A61K9/0053 ,  A61K31/403 ,  A61K31/44

    摘要： The present invention relates to methods, pharmaceutical compositions and kits for treating osteoarthritis associated pain, inflammation and improving function in a patient comprising a first therapeutic agent which comprises bicifadine or a pharmaceutically acceptable salt, enantiomer, solvate, hydrate, polymorph or prodrug thereof and a second therapeutic agent which comprises a non-steroidal anti-inflammatory drug or derivative thereof.

    摘要翻译： 本发明涉及用于治疗患有骨关节炎相关疼痛，炎症和改善功能的患者的方法，药物组合物和试剂盒，其包含第一治疗剂，其包含二十八烷或其药学上可接受的盐，对映体，溶剂化物，水合物，多晶型物或前药，以及 第二治疗剂，其包含非甾体抗炎药或其衍生物。

    2-Pyridinyl[7-(substituted-pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones
    4.
    发明申请
    2-Pyridinyl[7-(substituted-pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones 审中-公开
    2-吡啶基[7-（取代吡啶-4-基）吡唑并[1,5-a]嘧啶-3-基]甲酮

    公开(公告)号：US20050277639A1

    公开(公告)日：2005-12-15

    申请号：US11070394

    申请日：2005-03-01

    申请人： Phil Skolnick

    发明人： Phil Skolnick

    IPC分类号： A01N43/00 ,  A61K31/33 ,  A61K31/519 ,  A61K31/5377 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： The present invention provides novel 2-pyridinyl[7(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones with at least one substituent on the 4-pyridinyl ring having the chemical structure of formula I: The invention further provides compositions and methods employing the novel 2-pyridinyl[7-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidin-3-yl]methanones of formula I in to modulate GABA and GABA receptor physiology to elicit therapeutic responses in mammalian subjects to alleviate neurological or psychiatric disorders, including stroke, head trauma, epilepsy, pain, migraine, mood disorders, anxiety, post traumatic stress disorder, obsessive compulsive disorders, mania, bipolar disorders, schizophrenia, seizures, convulsions, tinnitus, neurodegenerative disorders including Alzheimer's disease, amyotrophic lateral sclerosis and Parkinson's disease, Huntington's chorea, depression, bipolar disorders, mania, trigeminal and other neuralgia, neuropathic pain, hypertension, cerebral ischemia, cardiac arrhythmia, myotonia, substance abuse, myoclonus, essential tremor, dyskinesia and other movement disorders, neonatal cerebral hemorrhage, and spasticity, as well as other psychiatric and neurological disorders mediated by GABA and/or GABA receptors.

    摘要翻译： 本发明提供了具有式I化学结构的4-吡啶基环上具有至少一个取代基的新的2-吡啶基[7（吡啶-4-基）吡唑并[1,5-a]嘧啶-3-基]甲酮 ：本发明还提供了使用式I的新型2-吡啶基[7-（吡啶-4-基）吡唑并[1,5-a]嘧啶-3-基]甲酮的组合物和方法来调节GABA和GABA受体生理学 在哺乳动物受试者中引发治疗反应以减轻神经或精神疾病，包括中风，头部创伤，癫痫，疼痛，偏头痛，情绪障碍，焦虑，创伤后应激障碍，强迫症，躁狂症，双相情感障碍，精神分裂症，癫痫发作，惊厥 ，耳鸣，包括阿尔茨海默病，肌萎缩性侧索硬化和帕金森病，亨廷顿舞蹈症，抑郁症，双相性精神障碍，躁狂症，三叉神经痛和其他神经痛，神经性疼痛，高血压，脑缺血，心脏的神经变性疾病 心律失常，肌强直，药物滥用，肌阵挛，原发性震颤，运动障碍和其他运动障碍，新生儿脑出血和痉挛状态，以及由GABA和/或GABA受体介导的其他精神和神经障碍。

    Methods and compositions for the treatment of urinary incontinence
    5.
    发明申请
    Methods and compositions for the treatment of urinary incontinence 审中-公开
    用于治疗尿失禁的方法和组合物

    公开(公告)号：US20080009538A1

    公开(公告)日：2008-01-10

    申请号：US11384219

    申请日：2006-03-17

    申请人： Phil Skolnick

    发明人： Phil Skolnick

    IPC分类号： A61K31/40 ,  A61P13/10

    CPC分类号： A61K45/06 ,  A61K31/403 ,  A61K2300/00

    摘要： Methods and compositions containing bicifadine are provided for the prevention and treatment of lower urinary tract disorders in mammalian subjects. The methods and compositions may be used to prevent or treat urinary incontinence, urinary urgency, nocturia, and enuresis associated with neurogenic and non-neurogenic overactive bladder, interstitial cystitis, prostatitis, prostadynia, and benign prostatic hyperplasia, among other conditions. Additional compositions and methods are provided which employ bicifadine in combination with a second anti-incontinence agent, or a different therapeutic agent to yield more effective anti-incontinence treatment tools, and/or dual activity therapeutic methods and formulations useful to prevent or reduce urinary incontinence and one or more additional symptoms such as urinary urgency, overflow, frequency, or pain in mammalian subjects.

    摘要翻译： 提供含有二西他汀的方法和组合物用于预防和治疗哺乳动物受试者中的下尿路障碍。 所述方法和组合物可用于预防或治疗与神经原性和非神经源性膀胱过度活动性膀胱，间质性膀胱炎，前列腺炎，前列腺症和良性前列腺增生等有关的尿失禁，尿急，夜尿和遗尿等。 提供了额外的组合物和方法，其使用二西他准与第二抗失禁药物或不同的治疗剂组合产生更有效的抗失尿治疗工具，和/或可用于预防或减少尿失禁的双重活性治疗方法和制剂 以及一种或多种另外的症状，例如哺乳动物受试者的尿急，溢流，频率或疼痛。

    Methods and compositions for the treatment of neuropathies and related disorders
    6.
    发明申请
    Methods and compositions for the treatment of neuropathies and related disorders 审中-公开
    用于治疗神经病和相关疾病的方法和组合物

    公开(公告)号：US20070082939A1

    公开(公告)日：2007-04-12

    申请号：US11492608

    申请日：2006-07-24

    申请人： Arnold Lippa ,  Phil Skolnick ,  Anthony Basile ,  Zhengming Chen ,  Joseph Epstein

    发明人： Arnold Lippa ,  Phil Skolnick ,  Anthony Basile ,  Zhengming Chen ,  Joseph Epstein

    IPC分类号： A61K31/403

    CPC分类号： A61K31/403

    摘要： The present invention provides novel compositions and methods for treating symptoms associated with neuropathic disorders such as hyperalgesia, allodynia, and parasthesias, using a 1-aryl-3-azabicyclo[3.1.0] hexane. The invention further relates to the use of 1-aryl-3-azabicyclo[3.1.0] hexanes in pharmaceutical compositions and methods for treating neuropathic disorders and related symptoms in mammals. Patients amenable to treatment according to the invention include those suffering from diabetic neuropathies, post-herpetic neuralgia, trigeminal neuralgia, chronic lower back pain, sciatica, idiopathic and post-traumatic neuropathies, HIV-associated neuropathic pain, among many other neuropathic disorders and related symptoms.

    摘要翻译： 本发明提供了使用1-芳基-3-氮杂双环[3.1.0]己烷治疗与神经性疾病相关的症状的新颖的组合物和方法，所述神经性疾病例如痛觉过敏，异常性疼痛和副症状。 本发明还涉及1-芳基-3-氮杂双环[3.1.0]己烷在用于治疗哺乳动物神经病症和相关症状的药物组合物和方法中的用途。 根据本发明治疗的患者包括患有糖尿病性神经病，疱疹后神经痛，三叉神经痛，慢性下背痛，坐骨神经痛，特发性和创伤后神经病变，HIV相关神经性疼痛等许多其他神经病变和相关的患者 症状

    Methods and compositions for production, formulation and use of 1-aryl-3-azabicyclo[3.1.0]hexanes
    7.
    发明申请
    Methods and compositions for production, formulation and use of 1-aryl-3-azabicyclo[3.1.0]hexanes 审中-公开
    用于生产，配制和使用1-芳基-3-氮杂双环[3.1.0]己烷的方法和组合物

    公开(公告)号：US20060223875A1

    公开(公告)日：2006-10-05

    申请号：US11371178

    申请日：2006-03-07

    申请人： Phil Skolnick ,  Anthony Basile ,  Zhengming Chen

    发明人： Phil Skolnick ,  Anthony Basile ,  Zhengming Chen

    IPC分类号： A61K31/403 ,  C07D209/00

    CPC分类号： C07D209/52

    摘要： The invention provides novel 1-aryl-3-azabicyclo[3.1.0]hexanes that are active for modulating biogenic amine transport, along with compositions and methods for using these compounds to treat central nervous system disorders. Certain 1-aryl-3-azabicyclo[3.1.0]hexanes are provided that have at least one substituent on the aryl ring. In other embodiments 1-aryl-3-azabicyclo[3.1.0]hexanes are provided that have a substitution on the nitrogen at the ‘3’ position. In additional embodiments 1-aryl-3-azabicyclo[3.1.0]hexanes are provided which have one substitution on the aryl ring, as well as a substitution on the nitrogen at the ‘3’ position. The invention also provides novel methods of making aryl- and aza-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, including synthetic methods that form novel intermediate compounds of the invention for producing aryl- and aza-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes.

    摘要翻译： 本发明提供了用于调节生物胺转运的新型1-芳基-3-氮杂双环[3.1.0]己烷，以及使用这些化合物治疗中枢神经系统疾病的组合物和方法。 提供在芳基环上具有至少一个取代基的某些1-芳基-3-氮杂双环[3.1.0]己烷。 在其它实施方案中，提供1-氮杂双环[3.1.0]己烷，其在“3”位上在氮上具有取代基。 在另外的实施方案中，提供1-芳基-3-氮杂双环[3.1.0]己烷，其在芳基环上具有一个取代基，以及在“3”位置的氮上进行取代。 本发明还提供制备芳基和氮杂取代的1-芳基-3-氮杂双环[3.1.0]己烷的新方法，包括形成本发明的新型中间体化合物的合成方法，用于制备芳基和氮杂取代的1-芳基 -3-氮杂双环[3.1.0]己烷。