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    PYRIDIN-2YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF
    3.
    发明申请
    PYRIDIN-2YL SULFANYL ACID ESTERS AND PROCESS FOR THE PREPARATION THEREOF 失效
    吡啶-2YL硫酸酯及其制备方法

    公开(公告)号：US20130131350A1

    公开(公告)日：2013-05-23

    申请号：US13811090

    申请日：2011-07-20

    申请人： Jadab Chandra Sarma ,  Dilip Chandra Bora ,  Paruchuri Gangadhar Rao ,  Balaram Ghosh ,  Sakshi Balwani

    发明人： Jadab Chandra Sarma ,  Dilip Chandra Bora ,  Paruchuri Gangadhar Rao ,  Balaram Ghosh ,  Sakshi Balwani

    IPC分类号： C07D213/70

    CPC分类号： C07D213/70

    摘要： The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.

    摘要翻译： 本发明涉及具有抗炎性质的吡啶-2-基硫基酸酯化合物。 本发明特别涉及具有通式1结构的吡啶-2-基硫烷基的新型抗炎杂环酸酯，它们已被筛选出其抗人活性的抑制作用，其中抑制嗜中性粒细胞分离自人外周血， 作为抑制细胞因子刺激的细胞粘附分子ICAM-1表达的结果，在人脐静脉内皮细胞（HU-VEC）的表面上。 发现化合物RS-Z，3-（吡啶-2-基硫烷基） - 丙酸戊酯（结构1a，R1 = H，R2 = H，R3 = CH2-COOC5H11）对ICAM-1和 发现嗜中性粒细胞粘附抑制被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似病症，如小鼠急性肺损伤和急性呼吸窘迫综合征。

    Pyridin-2yl sulfanyl acid esters and process for the preparation thereof
    4.
    发明授权
    Pyridin-2yl sulfanyl acid esters and process for the preparation thereof 失效
    吡啶-2-基硫基酸酯及其制备方法

    公开(公告)号：US08680288B2

    公开(公告)日：2014-03-25

    申请号：US13811090

    申请日：2011-07-20

    申请人： Jadab Chandra Sarma ,  Dilip Chandra Bora ,  Paruchuri Gangadhar Rao ,  Balaram Ghosh ,  Sakshi Balwani

    发明人： Jadab Chandra Sarma ,  Dilip Chandra Bora ,  Paruchuri Gangadhar Rao ,  Balaram Ghosh ,  Sakshi Balwani

    IPC分类号： C07D213/62 ,  A61K31/435

    CPC分类号： C07D213/70

    摘要： The present invention relates to Pyridin-2-yl sulfanyl acid ester compounds having antiinflammatory properties. The present invention particularly relates to novel anti-inflammatory heterocyclic acid esters of Pyridin-2-yl sulfanyl having the structure of general formula 1 which have been screened for their antiinflammatory activity with respect to inhibition of adhesion of neutrophils, isolated from human peripheral blood, onto the surface of human umbilical vein endothelial cells (HU-VEC) as a result of inhibition of the cytokine-stimulated expression of cell adhesion molecule ICAM-1. The compound RS—Z, 3-(Pyridin-2-yl sulfanyl)-propionic acid pentyl ester (structure 1a, R1=H, R2=H, R3=CH2-COOC5H11) was found to be most effective for ICAM-1 and neutrophil adhesion inhibition and was found to effectively alleviate inflammation mediated by excessive leukocyte infiltration leading to inflammatory disorders or like conditions, such as acute lung injury and acute respiratory distress syndrome in mice.

    摘要翻译： 本发明涉及具有抗炎性质的吡啶-2-基硫基酸酯化合物。 本发明特别涉及具有通式1结构的吡啶-2-基硫烷基的新型抗炎杂环酸酯，它们已被筛选出其抗人活性的抑制作用，其中抑制嗜中性粒细胞分离自人外周血， 作为抑制细胞因子刺激的细胞粘附分子ICAM-1表达的结果，在人脐静脉内皮细胞（HU-VEC）的表面上。 发现化合物RS-Z，3-（吡啶-2-基硫烷基） - 丙酸戊酯（结构1a，R1 = H，R2 = H，R3 = CH2-COOC5H11）对ICAM-1和 发现嗜中性粒细胞粘附抑制被发现有效缓解由过度白细胞浸润引起的炎症，导致炎症性疾病或类似病症，如小鼠急性肺损伤和急性呼吸窘迫综合征。