Compounds that abrogate DNA-damage-induced cell cycle G2 checkpoint and/or augment the anti-cancer activity of DNA damaging treatments
    21.
    发明申请
    Compounds that abrogate DNA-damage-induced cell cycle G2 checkpoint and/or augment the anti-cancer activity of DNA damaging treatments 失效
    消除DNA损伤诱导的细胞周期G2检查点和/或增加DNA损伤治疗的抗癌活性的化合物

    公开(公告)号:US20040198727A1

    公开(公告)日:2004-10-07

    申请号:US10457029

    申请日:2003-06-06

    摘要: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.

    摘要翻译: 本发明提供抑制哺乳动物细胞(包括人细胞)中的细胞周期G2检查点,特别是DNA损伤诱导的G2检查点的组合物和方法。 具体地,本发明提供了通过废除细胞周期G2检查点来使细胞对DNA损伤剂敏感的组合物和方法。 本发明的化合物用于治疗增殖性疾病如癌症。 本发明提供了选择性地使G1检查点受损的癌细胞对DNA损伤剂和治疗敏感的组合物和方法。

    3-amino-2-mercaptobenzoic acid derivatives and processes for their preparation
    22.
    发明申请
    3-amino-2-mercaptobenzoic acid derivatives and processes for their preparation 有权
    3-氨基-2-巯基苯甲酸衍生物及其制备方法

    公开(公告)号:US20020040157A1

    公开(公告)日:2002-04-04

    申请号:US09963046

    申请日:2001-09-25

    发明人: Walter Kunz Beat Jau

    IPC分类号: C07C327/26 C07C321/26

    摘要: Compounds of the formula I 1 and disulfides thereof and salts thereof are important intermediate products for the preparation of compounds having a microbicidal and plant-immunizing action, of the formula III 2 In the compounds of the formulae I and III: X is halogen, n is 0,1,2 or 3; Z is CN, COnullA or CSnullA, A is hydrogen, halogen, OR1, SR2 and N(R3)R4; R1 to R4 are hydrogen, a substituted or unsubstituted, open-chain, saturated or unsaturated hydrocarbon radical containing not more than 8 carbon atoms, a substituted or unsubstituted cyclic, saturated or unsaturated hydrocarbon radical containing not more than 10 carbon atoms, substituted or unsubstituted benzyl or phenethyl, a substituted or unsubstituted alkanoyl group containing not more than 8 carbon atoms, a substituted or unsubstituted benzoyl group or a substituted or unsubstituted heterocyclyl radical; or R3 and R4, together with the nitrogen atom to which they are bonded, are a 5- or 6-membered, substituted or unsubstituted heterocyclic radical having 1-3 heteroatoms O, S and/or N. Processes for the preparation of compounds of the formula I are described.

    摘要翻译: 式I化合物及其二硫化物及其盐是制备具有式III的杀微生物和植物免疫作用的化合物的重要中间产物。在式I和III化合物中:X为卤素,n为0 ,1,2或3; Z是CN,CO-A或CS-A,A是氢,卤素,OR1,SR2和N(R3)R4; R 1至R 4为氢,取代或未取代的含有不超过8个碳原子的开链,饱和或不饱和烃基,取代或未取代的含有不多于10个碳原子的环状,饱和或不饱和烃基,取代或未取代的 苄基或苯乙基,取代或未取代的不超过8个碳原子的烷酰基,取代或未取代的苯甲酰基或取代或未取代的杂环基; 或R 3和R 4与它们所键合的氮原子一起是具有1-3个杂原子O,S和/或N的5或6元取代或未取代的杂环基。用于制备 描述了式I。

    Addition of sulfenyl halides to olefins and acetylenes
    28.
    发明授权
    Addition of sulfenyl halides to olefins and acetylenes 失效
    将烯基卤化物加入到烯烃和乙炔中

    公开(公告)号:US4003939A

    公开(公告)日:1977-01-18

    申请号:US594593

    申请日:1975-07-10

    摘要: Acylthiosulfenyl halides, phosphorylsulfenyl halides, and thiophosphorylsulfenyl halides are added to monoolefins, multiolefins and acetylenic compounds. 1,2-Markownikov oriented adducts are the principal products when conjugated diolefins are employed as the starting feedstock. Anti-Markownikov adducts are obtained as major products when unsymmetrical monoolefins and nonconjugated multiolefins are used as the starting material. The addition reactions are conducted at low temperatures.

    摘要翻译: 酰基硫代亚磺酰卤,磷酰硫基卤化物和硫代磷酰基硫基卤化物加入到单烯烃,多烯烃和炔属化合物中。 当使用共轭二烯烃作为起始原料时,1,2-Markownikov取向的加合物是主要产物。 当使用非对称单烯烃和非共轭多烯烃作为起始原料时,抗Markownikov加合物作为主要产品获得。 加成反应在低温下进行。