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48 条记录 (耗时 0.057 秒)

    SPIROINDOLINONE DERIVATIVES
    44.
    发明申请
    SPIROINDOLINONE DERIVATIVES 失效
    螺吲哚啉酮衍生物

    公开(公告)号：US20080293723A1

    公开(公告)日：2008-11-27

    申请号：US12101206

    申请日：2008-04-11

    申请人： Jin-Jun Liu ,  Zhuming Zhang

    发明人： Jin-Jun Liu ,  Zhuming Zhang

    IPC分类号： A61K31/53 ,  C07D487/20

    CPC分类号： C07D471/20

    摘要： There are provided spiroindolinone derivatives of the formula and pharmaceutically acceptable salts and esters thereof wherein R1, R2, R3, R4 and R are as herein described. The compounds exhibit anticancer activity.

    摘要翻译： 提供下式的螺二吲哚啉酮衍生物及其药学上可接受的盐和酯，其中R1，R2，R3，R4和R如本文所述。 该化合物具有抗癌活性。

    Substituted 1,5-naphthyridine azolinones
    46.
    发明申请
    Substituted 1,5-naphthyridine azolinones 失效
    取代的1,5-二氮杂萘唑啉酮

    公开(公告)号：US20060223843A1

    公开(公告)日：2006-10-05

    申请号：US11368936

    申请日：2006-03-06

    申请人： Jin-Jun Liu

    发明人： Jin-Jun Liu

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07D471/04

    摘要： Substituted 1,5-naphthyridine azolinones inhibit Cdk1 and are selective against Cdk2 and Cdk4. These compounds and their pharmaceutically acceptable salts have antiproliferative activity and are useful as anti-cancer agents.

    摘要翻译： 取代的1,5-萘啶唑啉酮抑制Cdk1并对Cdk2和Cdk4有选择性。 这些化合物及其药学上可接受的盐具有抗增殖活性，可用作抗癌剂。

    Pyrazolobenzodiazepines
    47.
    发明授权
    Pyrazolobenzodiazepines 失效
    吡唑并苯并二氮杂

    公开(公告)号：US06440959B1

    公开(公告)日：2002-08-27

    申请号：US09548091

    申请日：2000-04-12

    申请人： Qingjie Ding ,  Jin-Jun Liu ,  Vincent Stewart Madison ,  Giacomo Pizzolato ,  Chung-Chen Wei ,  Peter Michael Wovkulich

    发明人： Qingjie Ding ,  Jin-Jun Liu ,  Vincent Stewart Madison ,  Giacomo Pizzolato ,  Chung-Chen Wei ,  Peter Michael Wovkulich

    IPC分类号： A61K31551

    CPC分类号： C07D487/04 ,  C07D243/22

    摘要： Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer, more particularly, the treatment or control of breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.

    摘要翻译： 公开了具有下式的新的吡唑并苯并二氮杂类及其药学上可接受的盐，其中R 1，R 2，R 3和R 4如本文所定义。 这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。 这些化合物及其药学上可接受的盐和所述化合物的前药是可用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂，更特别地，治疗或控制乳腺癌，结肠癌，肺癌和前列腺肿瘤 。 还公开了含有式I化合物的药物组合物以及可用于制备式I化合物的中间体。

    Intermediates for preparation of taxols
    48.
    发明授权
    Intermediates for preparation of taxols 失效
    用于制备紫杉醇的中间体

    公开(公告)号：US5274137A

    公开(公告)日：1993-12-28

    申请号：US902390

    申请日：1992-06-23

    申请人： K. C. Nicolaou ,  Chan-Kou Hwang ,  Erik J. Sorensen ,  Jin-Jun Liu

    发明人： K. C. Nicolaou ,  Chan-Kou Hwang ,  Erik J. Sorensen ,  Jin-Jun Liu

    IPC分类号： C07C43/178 ,  C07C69/00 ,  C07C69/013 ,  C07C69/757 ,  C07D305/14 ,  C07D317/72 ,  C07D319/08 ,  C07D493/08 ,  C07F7/18

    CPC分类号： C07D317/72 ,  C07C43/1788 ,  C07C69/757 ,  C07D305/14 ,  C07D319/08 ,  C07D493/08 ,  C07F7/1852 ,  C07C2101/16 ,  Y02P20/55

    摘要： A taxol intermediate selected from the group consisting of: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each selected from hydrogen, hydroxyl, or a protected hydroxyl; or R.sup.1 and R.sup.2 together form an oxo or a protected oxo; R.sup.3 is formyl, a protected formyl, or --CH(X)--OY wherein X is hydrogen or a monovalent metal and Y is hydrogen or a hydroxyl protecting group; and R.sup.4 and R.sup.5 are different and each selected from chloro or cyano; or R.sup.4 and R.sup.5 together form an oxo or a protected oxo, with the proviso that R.sup.1 and R.sup.2 are not both hydroxyl; R.sup.6 is hydroxyl or a protected hydroxyl; R.sup.7 is hydrogen, hydroxyl, or a protected hydroxyl; R.sup.8 is carboxyl, hydroxylmethyl, or a protected hydroxylmethyl; or R.sup.7 and R.sup.8 when taken together with carbon atoms 3 and 4, form an oxetane ring; or R.sup.6 and R.sup.8 when taken together with carbon atoms 1 and 4, form a bridged lactone; R.sup.9 is hydrogen or a hydroxyl protecting group; R.sup. 10 is hydroxyl or a protected hydroxyl; or R.sup.8 and R.sup.10 when taken together with carbon atoms 4 and 5, form a .gamma.-butyrolactone ring; R.sup.11 is alkoxycarbonyl, formyl, a protected formyl, hydroxylmethyl or a protected hydroxylmethyl; or R.sup.6 and R.sup.11 when taken together with carbon atoms 1 and 6, form a 2,2-dimethyl-1,3-dioxane ring; and the dotted line between the 2- and 3-positions of the six-membered ring represents an optional bond.

    摘要翻译： 选自以下的紫杉醇中间体：其中R 1和R 2相同或不同，并且各自选自氢，羟基或被保护的羟基; 或R 1和R 2一起形成氧代或受保护的氧代; R3是甲酰基，被保护的甲酰基或-CH（X）-OY，其中X是氢或一价金属，Y是氢或羟基保护基; 并且R 4和R 5不同，各自选自氯或氰基; 或R 4和R 5一起形成氧代或受保护的氧代，条件是R 1和R 2不是羟基; R6是羟基或被保护的羟基; R7是氢，羟基或被保护的羟基; R8是羧基，羟甲基或被保护的羟甲基; 或者当与碳原子3和4一起形成时，R 7和R 8形成氧杂环丁烷环; 或R6和R8与碳原子1和4一起形成桥连的内酯; R9是氢或羟基保护基; R 10是羟基或被保护的羟基; 或与R8和R10一起与碳原子4和5一起形成γ-丁内酯环; R11为烷氧基羰基，甲酰基，被保护的甲酰基，羟甲基或被保护的羟甲基; 或者R6和R11与碳原子1和6一起形成2,2-二甲基-1,3-二恶烷环; 并且六元环的2-位和3-位之间的虚线表示任选的键。