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    BICYCLIC PYRAZOLO-HETEROCYCLES
    1.
    发明申请
    BICYCLIC PYRAZOLO-HETEROCYCLES 有权
    双相PYRAZOLO-HETEROCYCLES

    公开(公告)号：US20110144121A1

    公开(公告)日：2011-06-16

    申请号：US12816657

    申请日：2010-06-16

    申请人： Robert Zhiyong Luo

    发明人： Robert Zhiyong Luo

    IPC分类号： A61K31/497 ,  C07D231/00 ,  C07D401/14 ,  C07D471/04 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/437 ,  A61P25/00

    CPC分类号： C07D471/04 ,  C07D231/56 ,  C07D401/04 ,  C07D413/12 ,  C07D417/04 ,  C07D491/052

    摘要： The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

    摘要翻译： 本发明提供了具有式I的通式结构的取代的吡唑并 - 杂环。还提供式I化合物的药学上可接受的盐，酸式盐，水合物，溶剂化物和立体异构体。该化合物可用作大麻素受体的调节剂和预防 以及治疗大麻素受体相关疾病和病症，如疼痛，炎症和瘙痒。

    Bicyclic pyrazolo-heterocycles
    4.
    发明授权
    Bicyclic pyrazolo-heterocycles 有权
    双环吡唑并杂环

    公开(公告)号：US08211926B2

    公开(公告)日：2012-07-03

    申请号：US12816657

    申请日：2010-06-16

    申请人： Robert Zhiyong Luo

    发明人： Robert Zhiyong Luo

    IPC分类号： A61K31/425 ,  A61K31/42 ,  A61K31/415 ,  A61K31/40 ,  A61K31/35 ,  C07D277/00 ,  C07D413/12 ,  C07D487/04 ,  C07D207/06 ,  C07D311/94

    CPC分类号： C07D471/04 ,  C07D231/56 ,  C07D401/04 ,  C07D413/12 ,  C07D417/04 ,  C07D491/052

    摘要： The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

    摘要翻译： 本发明提供了具有式I的通式结构的取代的吡唑并 - 杂环。还提供式I化合物的药学上可接受的盐，酸式盐，水合物，溶剂化物和立体异构体。该化合物可用作大麻素受体的调节剂和预防 以及治疗大麻素受体相关疾病和病症，如疼痛，炎症和瘙痒。

    Uses of kappa opioid synthetic peptide amides
    6.
    发明授权
    Uses of kappa opioid synthetic peptide amides 有权
    使用κ阿片样物质合成肽酰胺

    公开(公告)号：US08906859B2

    公开(公告)日：2014-12-09

    申请号：US12868790

    申请日：2010-08-26

    申请人： Claudio D. Schteingart ,  Frederique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Robert Zhiyong Luo

    发明人： Claudio D. Schteingart ,  Frederique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Robert Zhiyong Luo

    IPC分类号： A61K38/07 ,  C07K5/107 ,  C07K7/02 ,  C07K5/103

    CPC分类号： A61K38/07 ,  A61K38/08 ,  C07K5/101 ,  C07K5/1016 ,  C07K5/1019 ,  C07K7/02

    摘要： The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-α, IL-β, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.

    摘要翻译： 本发明涉及使用作为κ阿片样物质受体的配体的合成肽酰胺在治疗和预防κ阿片受体相关疾病和病症中的使用方法; 特别是这些激动剂在预防，抑制和治疗与各种疾病，病症和病症相关的疼痛，炎症和瘙痒症中的用途。 通过本发明的方法可预防或治疗的炎症状态包括与升高的促炎细胞因子如TNF-α，IL-和bgr，IL-6，MMP-1和MMP-3水平相关的疾病和病症。 这些疾病和病症包括心血管炎症，神经炎症，骨骼炎症，肌肉炎症，胃肠道炎症，眼部炎症，耳炎，由于昆虫叮咬引起的炎症和由于伤口愈合引起的炎症; 动脉粥样硬化，局部缺血，再狭窄和血管炎; 哮喘，干燥综合征，肺部炎症，慢性气道炎症和慢性阻塞性肺病（COPD），过敏，牛皮癣，银屑病关节炎，湿疹，硬皮病，特应性皮炎和系统性红斑狼疮，关节炎，滑膜炎，骨髓炎，类风湿性关节炎，骨关节炎和 强直性脊柱炎; 败血病和败血性休克，糖尿病，葡萄糖不耐受，胰岛素抵抗和肥胖，结肠炎，溃疡性结肠炎，克罗恩病，IBD和IBS，以及由于肿瘤增殖，肿瘤转移或移植排斥引起的炎症疾病和病症。

    Bicyclic pyrazolo-heterocycles
    7.
    发明授权
    Bicyclic pyrazolo-heterocycles 有权
    双环吡唑并杂环

    公开(公告)号：US08653127B2

    公开(公告)日：2014-02-18

    申请号：US13126490

    申请日：2010-01-14

    申请人： Robert Zhiyong Luo

    发明人： Robert Zhiyong Luo

    IPC分类号： A61P29/00 ,  A61P17/04 ,  A61K31/437 ,  C07D403/04 ,  C07D487/04 ,  C07D491/04

    CPC分类号： A61K31/437 ,  C07D231/56 ,  C07D401/04 ,  C07D403/04 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/10

    摘要： The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

    摘要翻译： 本发明提供具有通式I的通式结构的取代的吡唑并 - 杂环环A和B以及取代基R a，R b和R c的结构在说明书中描述。 还提供了式I化合物的药学上可接受的盐，酸式盐，水合物，溶剂合物和立体异构体。该化合物可用作大麻素受体的调节剂和用于预防，治疗和抑制大麻素受体相关疾病和病症，例如 疼痛，炎症和瘙痒。

    USES OF KAPPA OPIOID SYNTHETIC PEPTIDE AMIDES
    8.
    发明申请
    USES OF KAPPA OPIOID SYNTHETIC PEPTIDE AMIDES 有权
    KAPPA OPIOID合成肽类药物的使用

    公开(公告)号：US20110212882A1

    公开(公告)日：2011-09-01

    申请号：US12868790

    申请日：2010-08-26

    申请人： Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Robert Zhiyong Luo

    发明人： Claudio D. Schteingart ,  Frédérique Menzaghi ,  Guangcheng Jiang ,  Roberta Vezza Alexander ,  Javier Sueiras-Diaz ,  Robert H. Spencer ,  Derek T. Chalmers ,  Robert Zhiyong Luo

    IPC分类号： A61K38/07 ,  A61P17/00 ,  A61P19/00 ,  A61P19/02 ,  A61P25/00 ,  A61P3/04 ,  A61P3/10 ,  A61P35/00 ,  A61P25/04

    CPC分类号： A61K38/07 ,  A61K38/08 ,  C07K5/101 ,  C07K5/1016 ,  C07K5/1019 ,  C07K7/02

    摘要： The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-α, IL-β, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.

    摘要翻译： 本发明涉及使用作为κ阿片样物质受体的配体的合成肽酰胺在治疗和预防κ阿片受体相关疾病和病症中的使用方法; 特别是这些激动剂在预防，抑制和治疗与各种疾病，病症和病症相关的疼痛，炎症和瘙痒症中的用途。 通过本发明的方法可预防或治疗的炎症状态包括与升高的促炎细胞因子如TNF-α，IL-和bgr，IL-6，MMP-1和MMP-3水平相关的疾病和病症。 这些疾病和病症包括心血管炎症，神经炎症，骨骼炎症，肌肉炎症，胃肠道炎症，眼部炎症，耳炎，由于昆虫叮咬引起的炎症和由于伤口愈合引起的炎症; 动脉粥样硬化，局部缺血，再狭窄和血管炎; 哮喘，干燥综合征，肺部炎症，慢性气道炎症和慢性阻塞性肺病（COPD），过敏，牛皮癣，银屑病关节炎，湿疹，硬皮病，特应性皮炎和系统性红斑狼疮，关节炎，滑膜炎，骨髓炎，类风湿性关节炎，骨关节炎和 强直性脊柱炎; 败血病和败血性休克，糖尿病，葡萄糖不耐受，胰岛素抵抗和肥胖，结肠炎，溃疡性结肠炎，克罗恩病，IBD和IBS，以及由于肿瘤增殖，肿瘤转移或移植排斥引起的炎症疾病和病症。