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    Peptide drugs for chronic lymphocytic leukemia (CLL) and other cancers
    3.
    发明申请
    Peptide drugs for chronic lymphocytic leukemia (CLL) and other cancers 审中-公开
    用于慢性淋巴细胞白血病（CLL）和其他癌症的肽药物

    公开(公告)号：US20060198832A1

    公开(公告)日：2006-09-07

    申请号：US11267828

    申请日：2005-11-03

    申请人： Arnold Satterthwait ,  Xiuwen Zhu ,  Shinichi Kitada ,  John Reed

    发明人： Arnold Satterthwait ,  Xiuwen Zhu ,  Shinichi Kitada ,  John Reed

    IPC分类号： A61K38/54 ,  C12N9/99

    CPC分类号： C07K14/4702 ,  A61K38/00 ,  C07K2319/01

    摘要： The present invention provides a modified BAD peptide or peptidomimetic which includes an amino acid sequence having at least 60% amino acid identity with SEQ ID NO: 1, where the modified BAD peptide or peptidomimetic has enhanced affinity for Bcl-2 as compared to wild type BAD peptide (SEQ ID NO: 1). Further provided herein is a composition containing a delivery agent and a modified BAD peptide or peptidomimetic which includes an amino acid sequence having at least 60% amino acid identity with SEQ ID NO: 1, where the modified BAD peptide or peptidomimetic has enhanced affinity for Bcl-2 as compared to wild type BAD peptide (SEQ ID NO: 1).

    摘要翻译： 本发明提供了一种修饰的BAD肽或肽模拟物，其包括与SEQ ID NO：1具有至少60％氨基酸同一性的氨基酸序列，其中与野生型相比，修饰的BAD肽或肽模拟物对Bcl-2具有增强的亲和力 BAD肽（SEQ ID NO：1）。 本文进一步提供的是含有递送剂和修饰的BAD肽或肽模拟物的组合物，其包含与SEQ ID NO：1具有至少60％氨基酸同一性的氨基酸序列，其中修饰的BAD肽或肽模拟物对Bcl具有增强的亲和力 -2与野生型BAD肽（SEQ ID NO：1）相比。

    CANNABINOID RECEPTOR MODULATORS
    7.
    发明申请
    CANNABINOID RECEPTOR MODULATORS 有权
    CANNABINOID受体调节剂

    公开(公告)号：US20130165412A1

    公开(公告)日：2013-06-27

    申请号：US13616918

    申请日：2012-09-14

    申请人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    发明人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    IPC分类号： C07F9/6558 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D231/54 ,  C07D403/04

    CPC分类号： C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

    摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

    摘要翻译： 本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。 本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于 与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏 异常性疼痛 炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受 骨质疏松症 多发性硬化相关性痉挛状态; 自身免疫性疾病 过敏反应; CNS炎症; 动脉粥样硬化 不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

    Cannabinoid receptor modulators
    9.
    发明授权
    Cannabinoid receptor modulators 有权
    大麻素受体调节剂

    公开(公告)号：US08778950B2

    公开(公告)日：2014-07-15

    申请号：US13392074

    申请日：2010-08-27

    申请人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    发明人： Robert M. Jones ,  Sangdon Han ,  Lars Thoresen ,  Jae-Kyu Jung ,  Sonja Strah-Pleynet ,  Xiuwen Zhu ,  Yifeng Xiong ,  Dawei Yue

    IPC分类号： A61K31/4965 ,  A01N43/56 ,  A61K31/415 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00 ,  C07D231/54 ,  C07D487/00

    CPC分类号： C07D231/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07F9/65583

    摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

    摘要翻译： 本发明涉及某些式Ia化合物及其药物组合物，其调节大麻素CB2受体的活性。 本发明还涉及某些式Ia化合物及其药物组合物，其调节CB1受体和CB2受体的活性。 本发明的化合物及其药物组合物涉及可用于治疗以下疼痛的方法：疼痛，例如骨和关节疼痛，肌肉疼痛，牙痛，偏头痛和其他头痛疼痛，炎性疼痛，神经性疼痛，疼痛发生于 与骨关节炎相关的治疗和疼痛的不利影响; 痛觉过敏 异常性疼痛 炎性痛觉过敏; 神经性痛觉过敏; 急性伤害感受 骨质疏松症 多发性硬化相关性痉挛状态; 自身免疫性疾病 过敏反应; CNS炎症; 动脉粥样硬化 不良免疫细胞活性和炎症; 年龄相关性黄斑变性; 咳嗽; 白血病; 淋巴瘤 CNS肿瘤; 前列腺癌; 阿尔茨海默氏病; 中风引起的损伤; 痴呆; 肌萎缩性侧索硬化和帕金森病。

    Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders
    10.
    发明授权
    Substituted tricyclic acid derivatives as S1P1 receptor agonists useful in the treatment of autoimmune and inflammatory disorders 有权
    取代的三环酸衍生物作为可用于治疗自身免疫性和炎症性疾病的S1P1受体激动剂

    公开(公告)号：US08415484B2

    公开(公告)日：2013-04-09

    申请号：US13060477

    申请日：2009-08-26

    申请人： Robert M. Jones ,  Daniel J. Buzard ,  Andrew M. Kawasaki ,  Sun Hee Kim ,  Lars Thoresen ,  Juerg Lehmann ,  Xiuwen Zhu

    发明人： Robert M. Jones ,  Daniel J. Buzard ,  Andrew M. Kawasaki ,  Sun Hee Kim ,  Lars Thoresen ,  Juerg Lehmann ,  Xiuwen Zhu

    IPC分类号： C07D403/02 ,  C07D487/00 ,  C07D471/14 ,  C07D487/12 ,  C07D401/00 ,  C07D403/14 ,  A61K31/44 ,  A61K31/415 ,  A61K31/40

    CPC分类号： C07D487/04 ,  C07D471/04

    摘要： The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.

    摘要翻译： 本发明涉及某些取代的式（I）的三环酸衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为S1P1受体的激动剂。 本发明还提供了含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗S1P1相关病症的方法，例如牛皮癣，类风湿性关节炎，克罗恩病，移植排斥反应，多发性 硬化症，系统性红斑狼疮，溃疡性结肠炎，I型糖尿病，痤疮，心肌缺血再灌注损伤，高血压肾病，肾小球硬化，胃炎，多发性肌炎，甲状腺炎，白癜风，肝炎，胆汁性肝硬化，微生物感染和相关疾病，病毒感染和相关疾病 ，由淋巴细胞介导的疾病和病症，自身免疫疾病，炎性疾病和癌症。