PHOTOCLEAVABLE AND ACID CLEAVABLE LINKERS FOR COMBINATORIAL CHEMISTRY
    2.
    发明申请
    PHOTOCLEAVABLE AND ACID CLEAVABLE LINKERS FOR COMBINATORIAL CHEMISTRY 审中-公开
    用于组合化学的光电和酸性可清洗的连接器

    公开(公告)号:WO00005197A1

    公开(公告)日:2000-02-03

    申请号:PCT/US1999/016798

    申请日:1999-07-22

    摘要: A substrate for solid phase synthesis comprising a solid phase-linker combination of formula (I) is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediate useful therein. Among the novel intermediates are compounds of formula (II) wherein R is -NO2 or -CHO; R is -OCH3, -CHO or -H; R is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n = 1 or 3-12. A substrate of solid phase synthesis of formula (III) is also disclosed.

    摘要翻译: 公开了用于固相合成的底物,其包含式(I)的固相 - 连接体组合。 还公开了制备其中有用的基材和化学中间体的方法。 其中新的中间体是式(II)的化合物,其中R 1是-NO 2或-CHO; R 2是-OCH 3,-CHO或-H; R 3选自羟基,具有多个氨基的固体支持物的残基和酯的残基,n = 1或3-12。 还公开了式(III)的固相合成的底物。

    NOVEL BENZALDEHYDE DERIVATIVES FROM HERICEUM ERINACEUS
    3.
    发明申请
    NOVEL BENZALDEHYDE DERIVATIVES FROM HERICEUM ERINACEUS 审中-公开
    新的苯甲醛衍生物FROM HERICEUM刺猬

    公开(公告)号:WO1997036852A1

    公开(公告)日:1997-10-09

    申请号:PCT/EP1997001504

    申请日:1997-03-25

    IPC分类号: C07C59/90

    CPC分类号: C07C59/74 C12P7/42

    摘要: The present invention relates to a compound of formula (I) R to R are hydrogen or methyl, where two R to R on adjacent carbon atoms together with a C-C single bond may stand for a C-C double bond, provided that, in the carbon chain substituted by R to R , only one of the substituents R to R is methyl and only an adjacent pair of said substituents contribute to a C-C double bond, a process for its production and its use as a medicament, especially for treating diseases produced by an HIV infection.

    摘要翻译: 本发明涉及式(I)的化合物,其中R <1>至R <10>为氢或甲基,其中两个相邻碳原子上利用Dende,R <1>至R <10>与CC-单键用于一起 一个C-C双键的可自由基,条件是在其中R <1>至R <10>在每一种情况下的碳链仅取代基的一个R <1>至R <10>取代是甲基并且只有一对相邻的这些取代基的 有助于一个CC-双键,它们的制备方法和它们作为药物的用途的方法,尤其是用于由HIV感染引起的疾病的治疗。

    ORGANIC MOLECULES
    6.
    发明申请
    ORGANIC MOLECULES 审中-公开
    有机分子

    公开(公告)号:WO03087824A2

    公开(公告)日:2003-10-23

    申请号:PCT/GB0301505

    申请日:2003-04-07

    摘要: Compounds according to general formulae (Ia to Ie) wherein: X = O or S; Y is O, S or CH2, CHR, CRR, where R is C1-7 alkyl; Z is O or S; R1 is H or C1-7 alkyl; R2 is H or C1-7 alkyl; R4 is H or C1-7 alkyl at any vacant position on the aromatic ring; R3 is C1-7 alkyl-L1-R5-L2- R6-COOH, C3-10 cycloalkyl-L1-R5-L2- R6-COOH or Ar-C0-7 alkyl-L1-R5-L2- R6-COOH; each of L1 and L2 is absent or a suitable linker such as an amide CONH; or an ether -O-, or a thioether -S- or a sulphone -S02-; R5 is C1-7 alkyl, C3-1O cycloalkyl or Ar-C0-7 alkyl each of which is substituted with either NR8R9, where the nitrogen atom is capable of being protonated in solution to give N HR8R9; or a quaternary nitrogen atom N R8R9R10, such that R5 contains a positive charge; each of R8, R9 and R10 is independently C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl, or any two or more of R8, R9 and R10 together form an alicyclic or arylalicyclic ring system; R6 is C1-7 alkyl, C3-10 cycloalkyl or Ar-C0-7 alkyl; and their salts, hydrates, solvates, complexes or prodrugs are of use as linkers for conjugating an epitope to a carrier protein.

    摘要翻译: 根据通式(Ia至Ie)的化合物,其中:X = O或S; Y是O,S或CH 2,CHR,CRR,其中R是C 1-7烷基; Z是O或S; R1是H或C1-7烷基; R2是H或C1-7烷基; R4是芳环上任何空位的H或C 1-7烷基; R3是C1-7烷基-L1-R5-L2-R6-COOH,C3-10环烷基-L1-R5-L2-R6-COOH或Ar-C10-烷基-L1-R5-L2-R6-COOH; L1和L2各自不存在,或者合适的接头如酰胺CONH; 或醚-O-,或硫醚-S-或砜-S02-; R5是C1-7烷基,C3-1O环烷基或任选被NR8R9取代的Ar-C0-7烷基,其中氮原子能够在溶液中被质子化,得到N + HR8R9; 或季氮原子N + R 8 R 9 R 10,使得R 5含有正电荷; R 8,R 9和R 10各自独立地为C 1-7烷基,C 3-10环烷基或Ar-C 0-7烷基,或R 8,R 9和R 10中的任何两个或更多个一起形成脂环族或芳基脂环族环系; R 6是C 1-7烷基,C 3-10环烷基或Ar-C 0-7烷基; 并且它们的盐,水合物,溶剂合物,复合物或前药可用作将表位与载体蛋白缀合的接头。