Isolated bacterial strain of Achromobacter sp. MTCC 5605 and a highly enantioselective epoxide hydrolase isolated therefrom
    5.
    发明授权
    Isolated bacterial strain of Achromobacter sp. MTCC 5605 and a highly enantioselective epoxide hydrolase isolated therefrom 有权
    无色杆菌的分离菌株 MTCC 5605和从其分离的高度对映选择性的环氧化物水解酶

    公开(公告)号:US09150840B2

    公开(公告)日:2015-10-06

    申请号:US14000730

    申请日:2012-08-27

    摘要: The present invention relates to a novel epoxide hydrolase enzyme which aims to achieve a high degree of resolution towards a broader range of substrates with high enantioselectivity and yields with minimal product inhibition. The invention further relates to a new bacterial strain Achromobacter sp. MTCC 5605 isolated from a petroleum-contaminated sludge sample, capable of producing the said enzyme. It is notable that the enzyme can be used as whole bacterial cell preparation, which allows continuous hydrolysis of substrates at even higher concentration and have an advantage of being recycled. The invention further relates to a process for the hydrolysis of different aryl epoxides which are potential synthons of intermediates for the synthesis of chiral amino alcohols and bioactive compounds like β-blockers.

    摘要翻译: 本发明涉及一种新的环氧化物水解酶,其目的是为具有高对映选择性的较宽范围的底物获得高度的分辨率,并以最小的产物抑制率得到产率。 本发明还涉及一种新的细菌菌株Achromobacter sp。 从能够产生所述酶的经石油污染的污泥样品中分离出的MTCC 5605。 值得注意的是,该酶可以用作整个细菌细胞制剂,其允许以更高浓度连续水解底物并且具有被回收的优点。 本发明还涉及用于水解不同芳基环氧化物的方法,它们是用于合成手性氨基醇和生物活性化合物(例如) - 阻滞剂的中间体的潜在合成子。

    Pyrrolo[2,1-c][1,4]naphthodiazepine Linked Piperazine Compounds and a Process for the Preparation Thereof
    6.
    发明申请
    Pyrrolo[2,1-c][1,4]naphthodiazepine Linked Piperazine Compounds and a Process for the Preparation Thereof 有权
    吡咯并[2,1-c] [1,4]萘并氮杂环丁哌嗪化合物及其制备方法

    公开(公告)号:US20130317211A1

    公开(公告)日:2013-11-28

    申请号:US13985510

    申请日:2012-01-10

    IPC分类号: C07D487/04

    CPC分类号: C07D487/04

    摘要: The present invention provides a compound of general formula A, useful as potential antitumour agents against five human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]naphthodiazepine linked substituted piperazine conjugates attached through different alkane spacers of general formula A. (Formula I) General formula A. Where R=R′=(Formula II). n=1-9 and R″=methyl, ethyl, acetyl, benzyl, piperinoyl, 4-fluorophenyl, 4-chlorophenyl, 4-methoxyphenyl, pyridyl, pyrimidyl

    摘要翻译: 本发明提供通式A的化合物,其可用作五种人癌细胞系的潜在抗肿瘤剂。 本发明还提供了制备通过不同的通式A的烷烃间隔物连接的吡咯并[2,1-c] [1,4]萘并氮杂的连接的取代的哌嗪共轭物的方法。(式I)通式A.其中R = R'=(式II)。 乙基,乙酰基,苄基,哌嗪基,4-氟苯基,4-氯苯基,4-甲氧基苯基,吡啶基,嘧啶基

    Pyrrolo[2,1-c][1,4]benzodiazepine compounds and processes for the preparation thereof
    10.
    发明授权
    Pyrrolo[2,1-c][1,4]benzodiazepine compounds and processes for the preparation thereof 有权
    吡咯并[2,1-c] [1,4]苯并二氮杂化合物及其制备方法

    公开(公告)号:US07312210B2

    公开(公告)日:2007-12-25

    申请号:US11367223

    申请日:2006-03-03

    IPC分类号: C07D405/14 A61K31/551

    CPC分类号: C07D487/04

    摘要: The present invention provides novel pyrrolo [2,1-c][1,4]benzodiazepine compounds. This invention also provides a process for the preparation of novel pyrrolo[2,1-c][1,4]benzodiazepine compounds. These novel pyrrolo [2,1-c][1,4]benzodiazepine compounds are useful as antitumor agents. It also provides a process for the preparation of 7-methoxy-8-{n-[4-(2-oxo-2H-4-chromenyl)piperazino]alkyl}-oxy-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]benzodiazepin-5-one and 7-methoxy-8-{n-[4-(7-alkoxy-8-methyl-2-oxo-2H-4-chromenyl)piperazino]alkyl}-oxy-(11aS)-1,2,3,11a-5H-pyrrolo[2,1-c][1,4]. benzodiazepine-5-one with aliphatic chain length variations for these compounds.

    摘要翻译: 本发明提供新的吡咯并[2,1-c] [1,4]苯并二氮杂化合物。 本发明还提供了制备新型吡咯并[2,1-c] [1,4]苯并二氮杂化合物的方法。 这些新的吡咯并[2,1-c] [1,4]苯并二氮杂化合物可用作抗肿瘤剂。 它还提供了制备7-甲氧基-8- {正 - [4-(2-氧代-2H-4-苯并吡喃基)哌嗪基]烷基} - 氧 - (11aS)-1,2,3,11a -5H-吡咯并[2,1-c] [1,4]苯并二氮杂-5-酮和7-甲氧基-8- {正 - [4-(7-烷氧基-8-甲基-2-氧代-2H- - 烯丙基)哌嗪基]烷基} - 氧基 - (11aS)-1,2,3,11a-5H-吡咯并[2,1-c] [1,4]。 苯并二氮杂-5-酮与这些化合物具有脂肪族链长度变化。