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112 条记录 (耗时 0.069 秒)

    Hydroxyalkanoyl aminopyrazoles and related compounds
    3.
    发明授权
    Hydroxyalkanoyl aminopyrazoles and related compounds 失效
    羟基烷酰基氨基吡唑及其相关化合物

    公开(公告)号：US07053220B2

    公开(公告)日：2006-05-30

    申请号：US10355700

    申请日：2003-01-31

    申请人： Jay S. Tung ,  Ashley C. Guinn ,  Eugene D. Thorsett ,  Michael A. Pleiss

    发明人： Jay S. Tung ,  Ashley C. Guinn ,  Eugene D. Thorsett ,  Michael A. Pleiss

    IPC分类号： C07D285/135

    CPC分类号： C07D233/80 ,  C07D233/74

    摘要： This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting β-amyloid peptide release and/or synthesis, a method for inhibiting γ-secretase activity and a method for treating neurological disorders associated with β-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.

    摘要翻译： 本发明涉及一类包括羟基烷酰基氨基吡唑，羟基烷酰基氨基噻二唑，羟基烷酰基氨基酸酯，羟基烷酰基氨基酸酰胺，羟基烷酰基氨基醇，羟基链烷酰基氨基酮，羟基链烷酰基氨基乙内酰脲，羟基烷酰基苯胺和羟基烷酰基衍生物 的特权结构。 本发明还涉及药物组合物，其包含药学上可接受的盐形式的这种化合物或其前体药物。 本发明进一步涉及一种抑制β-淀粉样蛋白肽释放和/或合成的方法，一种抑制γ-分泌酶活性的方法和一种治疗与β-淀粉样蛋白肽生产相关的神经障碍的方法。 该方法包括向宿主施用包含有效量的式I化合物的药物制剂。式I化合物可用于预防和治疗阿尔茨海默氏病。

    &agr;aminocetic acid derivatives- &agr;4&bgr;7 receptor antagonists
    6.
    发明授权
    &agr;aminocetic acid derivatives- &agr;4&bgr;7 receptor antagonists 失效
    α-氨基酸衍生物-α4β7受体拮抗剂

    公开(公告)号：US06545160B2

    公开(公告)日：2003-04-08

    申请号：US10147884

    申请日：2002-05-20

    申请人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett

    发明人： Andrei W. Konradi ,  Michael A. Pleiss ,  Eugene D. Thorsett

    IPC分类号： C07D26306

    CPC分类号： C07D295/205 ,  C07C271/44 ,  C07C2601/14 ,  C07D213/56 ,  C07D263/24

    摘要： Disclosed are compounds which bind &agr;4&bgr;7 integrin. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by &agr;4&bgr;7 integrin. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

    摘要翻译： 公开了结合α4β7整联蛋白的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由α4β7整联蛋白介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

    Substituted pyrimidine compositions and methods of use
    7.
    发明授权
    Substituted pyrimidine compositions and methods of use 失效
    取代的嘧啶组合物和使用方法

    公开(公告)号：US06518424B1

    公开(公告)日：2003-02-11

    申请号：US09438103

    申请日：1999-11-10

    申请人： Varghese John ,  Russell E. Rydel ,  Michael S. Dappen ,  Eugene D. Thorsett

    发明人： Varghese John ,  Russell E. Rydel ,  Michael S. Dappen ,  Eugene D. Thorsett

    IPC分类号： C07D23924

    CPC分类号： C07D239/36 ,  C07D239/42

    摘要： Substituted pyrimidines that have the general structure: in which the symbol R1 represents a C1-C6 alkyl, C1-C6 alkoxy or halogen atom; R2 represents a phenyl group, substituted phenyl group, benzyl moiety, substituted benzyl moiety, C3-C7 cycloalkyl, or substituted C3-C7 cycloalkyl; R3 represents a hydrogen or C1-C6 alkyl group, R4 represents —H, —OH, —N3 or —NHCOCH3; and R5 represents H are provided. These compounds have activity as inhibitors of phospholipase A2, and are useful in treating disorders mediated by phospholipase A2.

    摘要翻译： 具有一般结构的取代的嘧啶：其中符号R1表示C1-C6烷基，C1-C6烷氧基或卤素原子; R 2表示苯基，取代的苯基，苄基部分，取代的苄基部分，C 3 -C 7环烷基或取代的C 3 -C 7环烷基; R 3表示氢或C 1 -C 6烷基，R 4表示-H，-OH，-N 3或-NHCOCH 3; 并且R5表示H。 这些化合物作为磷脂酶A2的抑制剂具有活性，可用于治疗由磷脂酶A2介导的病症。