COMPOUNDS SELECTIVELY INHIBITING GAMMA 9 DELTA 2 T LYMPHOCYTES
    5.
    发明申请
    COMPOUNDS SELECTIVELY INHIBITING GAMMA 9 DELTA 2 T LYMPHOCYTES 审中-公开
    化合物选择性抑制GAMMA 9 DELTA 2 T LYMPHOCYTES

    公开(公告)号:WO00059916A1

    公开(公告)日:2000-10-12

    申请号:PCT/FR2000/000837

    申请日:2000-04-04

    摘要: The invention concerns compounds of formula CH3-R1-(CH2)2-R2 wherein: R1 is selected among a tertiary alcohol; a 1,2-diol; a halohydrine; an epoxide; an alkene; an aldehyde or an alpha -hydroxyaldehyde; and R2 is selected among a methylenediphosphonate; a difluoromethylenediphosphonate; or a monofluoromethylenediphosphonate. The invention also concerns the uses of said compounds as selective inhibitors of T gamma 9 delta 2 lymphocytes, and their uses, in particular for therapeutic purposes.

    摘要翻译: 本发明涉及式CH3-R1(CH2)2-R2的化合物,其中:R1选自叔醇; 1,2-二醇; 卤代水 环氧化物 烯烃 醛或α-羟基醛; 并且R2选自亚甲基二膦酸盐; 二氟亚甲基二膦酸盐; 或单氟亚甲基二膦酸盐。 本发明还涉及所述化合物作为Tγ9Δ2淋巴细胞的选择性抑制剂及其用途,特别是用于治疗目的的用途。

    BISPHOSPHONIC ACID DERIVATIVES
    6.
    发明申请
    BISPHOSPHONIC ACID DERIVATIVES 审中-公开
    二磷酸衍生物

    公开(公告)号:WO1996030378A1

    公开(公告)日:1996-10-03

    申请号:PCT/JP1996000888

    申请日:1996-04-01

    IPC分类号: C07F09/655

    摘要: Bisphosphonic acid derivatives having a partial structure of epoxysuccinic acid and showing the activity of inhibiting a cysteine protease, in particular, one represented by general formula (I) or its salt (wherein R represents hydrogen, alkyl or aralkyl; X represents -O-, -NR - or a divalent heterocyclic residue; A represents a single bond or an amino acid or dipeptide residue having the N-terminus on the right side; A represents a single bond or an amino acid or dipeptide residue having the N-terminus on the left side; L represents a divalent leaving group; and R , R , R , R and R independently represent each hydrogen, alkyl or aralkyl) which are useful as a remedy for bone diseases and in the treatment or prevention of diseases in association with the hyperfunction of cathepsins L and B.

    摘要翻译: 具有部分结构的环氧琥珀酸的双膦酸衍生物,显示抑制半胱氨酸蛋白酶的活性,特别是由通式(I)表示的二膦酸衍生物或其盐(其中R 1表示氢,烷基或芳烷基; X 1 >表示-O-,-NR 6 - 或二价杂环残基; A 1表示单键或位于右侧具有N末端的氨基酸或二肽残基; A 2表示单 键或左侧具有N末端的氨基酸或二肽残基; L 1表示二价离去基团; R 2,R 3,R 4,R 5和R 可以用作骨疾病的治疗方法,治疗或预防与组织蛋白酶L和B功能异常有关的疾病的各个氢,烷基或芳烷基。

    磷霉素氨盐的制备方法
    7.
    发明申请

    公开(公告)号:WO2014032363A1

    公开(公告)日:2014-03-06

    申请号:PCT/CN2012/084378

    申请日:2012-11-09

    发明人: 陈发普

    IPC分类号: C07F9/655

    CPC分类号: C07F9/65505

    摘要: 本发明公开了一种磷霉素氨盐的制备方法,其包含下列步骤:在有机溶剂中,将左磷右氨盐与异氰酸酯、异硫氰酸酯、烯酮、异氰酸酯的二聚体、异硫氰酸酯的二聚体、或者烯酮的二聚体,以及氨丁三醇进行反应;或者,在有机溶剂中,将磷霉素双氨丁三醇,与异氰酸酯、异硫氰酸酯、烯酮、异氰酸酯的二聚体、异硫氰酸酯的二聚体、或者烯酮的二聚体进行反应,即可。本发明的制备方法仅需一步反应即可完成,不需要低温离子交换柱,收率高,成本低,三废少,反应条件温和,能耗低,操作方便,适合于工业化。