Use of CRTH2 Antagonist Compounds
    1.
    发明申请
    Use of CRTH2 Antagonist Compounds 审中-公开
    使用CRTH2拮抗剂化合物

    公开(公告)号:US20110124683A1

    公开(公告)日:2011-05-26

    申请号:US12779638

    申请日:2010-05-13

    CPC分类号: A61K31/404

    摘要: The invention relates to compounds of general formula (I): wherein R1, R2, R3, R4 and R5 are as defined herein for the treatment of allergic conditions, wherein the treatment is by pulsed therapy which comprises a first period during which the compound is administered to the patient and a second period of at least seven days during which the compound is administered to the patient in a reduced amount. The invention also relates to compounds of general formula (I) for desensitizing the immune system of a subject to allergens, thus preventing or reducing the symptoms of allergic conditions such as allergic asthma, allergic rhinitis, or atopic dermatitis.

    摘要翻译: 本发明涉及通式(I)的化合物:其中R 1,R 2,R 3,R 4和R 5如本文所定义用于治疗过敏性疾病,其中所述治疗是通过脉冲疗法,其包括第一期间, 给予患者和第二期至少7天,其中化合物以减少的量施用给患者。 本发明还涉及使受试者的免疫系统对变应原脱敏的通式(I)化合物,从而预防或减少过敏性疾病如过敏性哮喘,过敏性鼻炎或特应性皮炎的症状。

    N-formyl hydroxylamine derivatives as antibacterial agents
    3.
    发明授权
    N-formyl hydroxylamine derivatives as antibacterial agents 失效
    N-甲酰羟胺衍生物作为抗菌剂

    公开(公告)号:US06476067B1

    公开(公告)日:2002-11-05

    申请号:US09868076

    申请日:2001-06-14

    IPC分类号: A61K3127

    摘要: Compounds of formula (I) are in the preparation of antibacterial agents, wherein: R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10(X)n—(ALK)— wherein R10 represents hydrogen, a C1-C6 alkyl, C2-C6 alkenyl, C1-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoyy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo, trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, which may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, and n is 0 or 1, R represents hydrogen or C1-C6 alkyl, R3 represents the characterising group or a natural or non-natural &agr; amino acid in which any functional groups may be protected; and R4 represents an ester or thioester group.

    摘要翻译: 式(I)化合物在制备抗菌剂中,其中:R1代表氢,C1-C6烷基或被一个或多个卤素原子取代的C1-C6烷基; R 2表示基团R 10(X)n-(ALK) - 其中R 10表示氢,C 1 -C 6烷基,C 2 -C 6烯基,C 1 -C 6炔基,环烷基,芳基或杂环基,其中任何一个可以是未取代的或 被(C 1 -C 6)烷基,(C 1 -C 6)烷基,羟基,巯基,(C 1 -C 6)烷硫基,氨基,卤素,三氟甲基,氰基,硝基,-COOH,-CONH 2,-COORA,-NHCORA - CONHRA,-NHRA,-NRARB或-CONRARB,其中RA和RB独立地为(C1-C6)烷基,ALK表示直链或支链二价C1-C6亚烷基,C2-C6亚烯基或C2-C6亚炔基 ,其可以被一个或多个不相邻的-NH-,-O-或-S-键中断,X表示-NH-,-O-或-S-,n为0或1,R表示氢或 C 1 -C 6烷基,R 3表示其中任何官能团可被保护的表征基团或天然或非天然α氨基酸; 并且R 4表示酯或硫酯基。