Pyrazolobenzodiazepines
    1.
    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

    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。

    Penam antibacterial compounds
    3.
    发明授权
    Penam antibacterial compounds 失效
    Penam抗菌化合物

    公开(公告)号:US5159077A

    公开(公告)日:1992-10-27

    申请号:US383783

    申请日:1989-07-21

    摘要: Antibacterial compounds of the formula ##STR1## in which R.sub.1 is a cyclic or secondary acyclic amino group which independently has antibacterial activity:R.sub.2 is hydrogen, lower alkoxy, lower alkylthio or formamido;R.sub.3 is hydrogen or an organic group bonded through carbon, oxygen, sulfur or nitrogen;R.sub.4 is an electronegative acidic group; or R.sub.3 and R.sub.4 together form a heterocycle; andR.sub.5 is a hydrogen or lower alkyl, except when R.sub.3 and R.sub.4 form a heterocycle, in which case R.sub.5 is hydrogen only; and methods of using same.

    摘要翻译: R1是具有独立具有抗菌活性的环状或次级无环氨基的式Ⅰ的抗菌化合物:R2是氢,低级烷氧基,低级烷硫基或甲酰氨基; R3是氢或通过碳,氧,硫或氮键合的有机基团; R4是电负性酸性基团; 或R3和R4一起形成杂环; 并且R 5是氢或低级烷基,除了当R 3和R 4形成杂环时,其中R 5仅为氢; 和使用方法。

    Antibacterial cephalosporin compounds
    4.
    发明授权
    Antibacterial cephalosporin compounds 失效
    抗生素CEPHOROSPORIN化合物

    公开(公告)号:US5189157A

    公开(公告)日:1993-02-23

    申请号:US189936

    申请日:1988-05-03

    摘要: There are presented antibacterial cephalosporins having broad antimicrobial activity as well as intermediates for their formation, such compounds having the formula ##STR1## wherein X is ##STR2## R is hydrogen or a carboxylic acid protecting group; R.sub.1 is hydrogen or an acyl group;R.sub.2 is hydrogen or lower alkoxy; andR.sub.3 is carbocyclic aryl or alkyl carbocyclic aryl substituted on the ring with two or more of hydroxy and/or lower alkanoyl ester groups, with halogen being an optional additional ring substituent;as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen.

    摘要翻译: 呈现具有广谱抗微生物活性的抗菌头孢菌素及其形成中间体,具有下式的化合物,其中X为氢或羧酸保护基; R1是氢或酰基; R2是氢或低级烷氧基; 并且R 3是在具有两个或多个羟基和/或低级烷酰基酯基团的环上被取代的碳环芳基或烷基碳环基,其中卤素是任选的另外的环取代基; 以及其中R是氢的这些化合物的相应的易水解的酯,药学上可接受的盐和水合物。

    Desulfurization of penicillins to prepare azetidinones
    7.
    发明授权
    Desulfurization of penicillins to prepare azetidinones 失效
    青霉素脱硫制备氮杂环丁酮

    公开(公告)号:US4461726A

    公开(公告)日:1984-07-24

    申请号:US379386

    申请日:1982-05-17

    CPC分类号: C07D205/085 B01J25/02

    摘要: A process for the Raney nickel desulfurization of penicillins is described. In the process of the invention, amino penicillanic acid or derivatives thereof are reacted with Raney nickel under controlled conditions of temperature and time to yield azetidinones which are useful as intermediates for the synthesis of monocyclic beta-lactam antibiotics.

    摘要翻译: 描述了青霉素的雷尼镍脱硫方法。 在本发明的方法中,氨基青霉烷酸或其衍生物在温度和时间的控制条件下与阮内镍反应,得到可用作合成单环β-内酰胺抗生素的中间体的氮杂环丁酮。