Carboxamide derivatives as therapeutic agents
    42.
    发明授权
    Carboxamide derivatives as therapeutic agents 失效
    甲酰胺衍生物作为治疗剂

    公开(公告)号:US07776919B2

    公开(公告)日:2010-08-17

    申请号:US12019045

    申请日:2008-01-24

    摘要: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

    摘要翻译: 本发明提供某些化合物,其制备方法,包含该化合物的药物组合物及其在治疗人或动物疾病中的用途。 本发明的化合物可用作晚期糖基化终产物(RAGE)的受体与其配体如晚期糖基化终产物(AGE),S100 /钙粒蛋白/ EN-RAGE,淀粉样蛋白和 两性霉素,以及由RAGE引起的人类疾病的管理,治疗,控制或辅助治疗。 这些疾病或疾病状态包括急性和慢性炎症,糖尿病晚期并发症的发展,例如血管通透性增加,肾病,动脉粥样硬化和视网膜病变,阿尔茨海默病的发展,勃起功能障碍和肿瘤侵袭和转移。

    Aryl and heteroaryl compounds, compositions, and methods of use
    46.
    发明授权
    Aryl and heteroaryl compounds, compositions, and methods of use 失效
    芳基和杂芳基化合物,组合物和使用方法

    公开(公告)号:US07208601B2

    公开(公告)日:2007-04-24

    申请号:US11069521

    申请日:2005-03-01

    IPC分类号: C07D217/00

    摘要: This invention provides aryl and heteroaryl compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention may be useful as antagonists, or partial antagonist of factor IX and/or factor XI and thus, may be used to inhibit the intrinsic pathway of blood coagulation. The compounds may be useful in a variety of applications including the management, treatment and/or control of diseases caused in part by the intrinsic clotting pathway utilizing factor IX and/or XI.

    摘要翻译: 本发明提供芳基和杂芳基化合物,其制备方法,包含该化合物的药物组合物及其在治疗人或动物病症中的用途。 本发明的化合物可用作拮抗剂或因子IX和/或因子XI的部分拮抗剂,因此可用于抑制凝血的内在途径。 所述化合物可用于各种应用,包括通过利用因子IX和/或XI的部分凝血途径引起的疾病的管理,治疗和/或控制。

    Benzimidazole derivatives as therapeutic agents

    公开(公告)号:US07087632B2

    公开(公告)日:2006-08-08

    申请号:US10091609

    申请日:2002-03-05

    IPC分类号: A61K31/4184 C07D235/14

    摘要: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

    Heterocycle derivatives as PPAR-gamma agonists
    48.
    发明授权
    Heterocycle derivatives as PPAR-gamma agonists 失效
    杂环衍生物作为PPAR-γ激动剂

    公开(公告)号:US06462046B2

    公开(公告)日:2002-10-08

    申请号:US09734458

    申请日:2000-12-11

    IPC分类号: A61K31496

    摘要: Compounds having the structure are peroxisome proliferator-activated receptor-gamma (PPAR-gamma) selective agonists and as such are useful in the modulation of blood glucose and the increase of insulin sensitivity in mammals. This activity of the piperazine derivatives of the invention make them particularly useful in the treatment of those conditions selected from the group consisting of diabetes, atherosclerosis, hyperglycemia, hyperlipidemia, obesity, syndrome X, insulin resistance, hypertension, heart failure and cardiovascular disease in mammals.

    摘要翻译: 具有结构的化合物是过氧化物酶体增殖物激活受体-γ(PPAR-γ)选择性激动剂,因此可用于调节血糖和哺乳动物胰岛素敏感性的增加。 本发明的哌嗪衍生物的这种活性使得它们特别可用于治疗选自以下的那些病症:糖尿病,动脉粥样硬化,高血糖症,高脂血症,肥胖症,综合征X,胰岛素抵抗,高血压,心力衰竭和哺乳动物心血管疾病 。

    Nucleic acid molecules encoding rage fusion proteins
    49.
    发明授权
    Nucleic acid molecules encoding rage fusion proteins 失效
    编码狂犬病融合蛋白的核酸分子

    公开(公告)号:US08344120B2

    公开(公告)日:2013-01-01

    申请号:US13158748

    申请日:2011-06-13

    IPC分类号: C07H21/04

    摘要: Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to the N-terminus of an immunoglobulin CH2 domain. Also disclosed are RAGE fusion protein formulations and the use of the RAGE fusion proteins and RAGE fusion protein formulations as therapeutics for RAGE-mediated pathologies.

    摘要翻译: 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点的RAGE多肽结构域和直接连接到免疫球蛋白CH2结构域的N末端的域间连接。 还公开了RAGE融合蛋白制剂以及使用RAGE融合蛋白和RAGE融合蛋白制剂作为RAGE介导的病理学的治疗剂。