中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

49 records (took 0.031 seconds)

    Macrocyclic beta-secretase inhibitors for the treatment of Alzheimer's disease
    7.
    发明授权
    Macrocyclic beta-secretase inhibitors for the treatment of Alzheimer's disease 有权
    用于治疗阿尔茨海默氏病的大环β-分泌酶抑制剂

    公开(公告)号：US07329746B2

    公开(公告)日：2008-02-12

    申请号：US10568153

    申请日：2004-08-10

    Applicant: Craig A. Coburn ,  Shawn J. Stachel ,  Joseph P. Vacca

    Inventor： Craig A. Coburn ,  Shawn J. Stachel ,  Joseph P. Vacca

    IPC: C07D225/04 ,  C07D267/22 ,  A61K31/33 ,  A61K31/395 ,  A61P25/28

    CPC classification number: C07D267/00 ,  C07D225/08

    Abstract: The present invention is directed to compounds of formula I which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the beta-secretase enzyme is involved

    Abstract translation: 本发明涉及作为β-分泌酶的抑制剂并可用于治疗或预防其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式I化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及β-分泌酶的疾病中的用途

    Methods of preparation of camptothecin analogs
    8.
    发明授权
    Methods of preparation of camptothecin analogs 失效
    喜树碱类似物的制备方法

    公开(公告)号：US5391745A

    公开(公告)日：1995-02-21

    申请号：US2996

    申请日：1993-01-11

    Applicant: Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen ,  Craig A. Coburn

    Inventor： Samuel J. Danishefsky ,  William G. Bornmann ,  Wang Shen ,  Craig A. Coburn

    IPC: C07D491/14 ,  C07D491/147 ,  C07D491/22 ,  C07H17/00 ,  C07D491/52

    CPC classification number: C07D491/14 ,  C07H17/00

    Abstract: Substituted analoguss of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, acyl, or CN; X is H OH, or OR; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, alkoxy, hydroxyalkyl, or aminoalkoxy group, or an aryl or aryloxy group, or a C-glycal, or CO.sub.2 R, nitro, cyano, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12, or OR.sup.13 ; R is H, or a linear or branched chain alkyl, alkylaryl, or hydroxyalkyl group, or an aryl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, or a linear or branched chain alkyl, alkylaryl, hydroxyalkyl, or acyl group, or an aryl group; R.sup.13 is glycosyl; n is 0 or 1; with the proviso that when R.sup. 1 is ethyl, and n is 0, E, R.sup.2, R.sup.3, and R.sup.4 are not all H. Intermediate compounds leading to the camptothecin analogues comprise substituted tricyclic compounds which consist of rings C, D, and E fused together. Methods for preparing the analoguss involve condensation of such intermediates with variably substituted protected .alpha.-aminobenzaldehydes.

    Abstract translation: 具有一般结构的具有对癌细胞的细胞毒性活性的喜树碱的取代类似物：其中E是H，CO 2 R，CONH 2，CONHR，CONR 2，酰基或CN; X是H OH或OR; R 1，R 2，R 3和R 4独立地相同或不同，为H，或直链或支链烷基，烷基芳基或羟烷基或芳基; R 5，R 6，R 7，R 8和R 9独立地相同或不同，为H，或直链或支链烷基，烷基芳基，烷氧基，羟基烷基或氨基烷氧基，或芳基或芳氧基或C- ，或CO 2 R，硝基，氰基，Cl，F，Br，I，SR10，NR 11 R 12或OR 13; R为H或直链或支链烷基，烷基芳基或羟烷基或芳基; R 10，R 11和R 12独立地相同或不同，为H，或直链或支链烷基，烷基芳基，羟基烷基或酰基或芳基; R13是糖基; n为0或1; 条件是当R 1为乙基且n为0时，E，R 2，R 3和R 4不全为H.导致喜树碱类似物的中间体化合物包括取代的三环化合物，其由环C，D和E稠合 一起。 制备类似物的方法涉及这种中间体与可变取代的保护的α-氨基苯甲醛的缩合。

Patent Agency Ranking