4,4-Disubstituted piperidines, and methods of use thereof

    公开(公告)号:US20070225331A1

    公开(公告)日:2007-09-27

    申请号:US11803670

    申请日:2007-05-14

    Inventor: Michael Hoemann

    CPC classification number: C07D211/26 C07D211/22

    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

    4,4-Disubstituted piperidines, and methods of use thereof
    13.
    发明授权
    4,4-Disubstituted piperidines, and methods of use thereof 有权
    4,4-二取代的哌啶类及其使用方法

    公开(公告)号:US07217823B2

    公开(公告)日:2007-05-15

    申请号:US10722114

    申请日:2003-11-25

    CPC classification number: C07D211/26 C07D211/22

    Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

    Abstract translation: 本发明的一个方面涉及杂环化合物。 本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体(包括多巴胺转运蛋白)的配体的用途。 本发明的化合物可用于治疗多种疾病,疾病,其包括但不限于成瘾,焦虑,抑郁,性功能障碍,高血压,偏头痛,阿尔茨海默病,肥胖,呕吐,精神病, 镇痛,精神分裂症,帕金森病,不宁腿综合征,睡眠障碍,注意缺陷多动障碍,肠易激综合征,早泄,月经性烦躁综合征,尿失禁,炎性疼痛,神经性疼痛,莱氏阴道炎,威尔逊氏病和图雷特综合征 。 本发明的另一方面涉及杂环化合物的组合文库的合成,以及用于生物活性的那些文库的筛选,例如在基于多巴胺转运蛋白的测定中。

    Hydroxylansoprazole methods
    15.
    发明授权

    公开(公告)号:US07098224B2

    公开(公告)日:2006-08-29

    申请号:US10685628

    申请日:2003-10-14

    Inventor: William E. Yelle

    CPC classification number: A61K31/4439

    Abstract: Methods and compositions are disclosed utilizing hydroxylansoprazole for the treatment of ulcers in humans. Hydroxylansoprazole exhibits a lessened liability toward drug-drug interactions than lansoprazole and a more predictable dosing regimen than lansoprazole. Hydroxylansoprazole is also useful for the treatment of gastroesophageal reflux and other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.

    Methods of using norfluoxetine
    17.
    发明授权
    Methods of using norfluoxetine 有权
    使用诺氟西汀的方法

    公开(公告)号:US07034059B2

    公开(公告)日:2006-04-25

    申请号:US10183472

    申请日:2002-06-28

    CPC classification number: A61K45/06 A61K31/137 A61K31/56 A61K2300/00

    Abstract: The invention encompasses methods of using racemic and enantiomerically pure norfluoxetine, as well as pharmaceutical compositions, pharmaceutical unit dosage forms, and kits comprising racemic and enantiomerically pure norfluoxetine. In particular, the invention encompasses a method of inhibiting or reducing the production of PGE2. The invention further encompasses a method of treating or preventing inflammation in a patient, as well as a method of treating or preventing a disease or disorder such as, but not limited to, autoimmune diseases, arthritis, neurologic diseases, inflammatory diseases, fibromyalgia, pain resulting from inflammation, neuropathic pain, and cancer.

    Abstract translation: 本发明包括使用外消旋和对映异构纯的去甲氟西汀以及药物组合物,药物单位剂型和包含外消旋和对映异构纯的去甲氟西汀的试剂盒的方法。 特别地,本发明包括抑制或降低PGE 2 2的产生的方法。 本发明还包括治疗或预防患者炎症的方法,以及治疗或预防疾病或病症的方法,所述疾病或病症例如但不限于自身免疫疾病,关节炎,神经系统疾病,炎性疾病,纤维肌痛,疼痛 由炎症,神经性疼痛和癌症引起。

    Method for treating gastric disorders using optically pure (−) pantoprazole
    19.
    发明授权
    Method for treating gastric disorders using optically pure (−) pantoprazole 失效
    使用光学纯( - )泮托拉唑治疗胃病的方法

    公开(公告)号:US06953808B2

    公开(公告)日:2005-10-11

    申请号:US10757059

    申请日:2004-01-14

    Applicant: Nancy M. Gray

    Inventor: Nancy M. Gray

    CPC classification number: A61K31/4439 A61K31/44

    Abstract: Methods and compositions are disclosed utilizing optically pure (−) pantoprazole for the treatment of ulcers in humans while substantially reducing the concomitant liability of adverse effects associated with the racemic mixture of pantoprazole. The optically pure (−) isomer is also useful for the treatment of gastroesophageal reflux. (−) Pantoprazole is an inhibitor of H+ release and is therefore useful in the treatment of other conditions related to gastric hypersecretion such as Zollinger-Ellison Syndrome.

    Abstract translation: 公开了使用光学纯的( - )泮托拉唑用于治疗人类溃疡的方法和组合物,同时显着降低与泮托拉唑的外消旋混合物相关的副作用的伴随的责任。 光学纯的( - )异构体也可用于治疗胃食管反流。 ( - )泮托拉唑是释放H +的抑制剂,因此可用于治疗与胃分泌异常有关的其他病症如Zollinger-Ellison综合征。

Patent Agency Ranking