Process for preparation of Irbesartan
    93.
    发明授权
    Process for preparation of Irbesartan 失效
    厄贝沙坦制备方法

    公开(公告)号:US07652147B2

    公开(公告)日:2010-01-26

    申请号:US11406919

    申请日:2006-04-19

    IPC分类号: C07D257/00 C07D403/00

    摘要: A process for the preparation of Irbesartan of formula (I) using the steps of: (i) reacting 4′ aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V) in an organic solvent and in the presence of an acid, without activating the —COOH group of compound of formula (V) to give 1-(2′cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII). converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).

    摘要翻译: 使用以下步骤制备式(I)的厄贝沙坦的方法:(i)使式(VI)的4'-氨基甲基-2-氰基联苯与式(V)的1-维拉酰氨基环戊烷羧酸在有机溶剂 并且在酸存在下,不活化式(Ⅴ)化合物的-COOH基,得到式(Ⅶ)的1-(2'-氰基联苯-4-基 - 甲基氨基羰基)-1-戊酰基氨基环戊烷。 通过使式(Ⅶ)化合物与叠氮化三丁基锡在邻二甲苯中反应,得到式(ⅰ)中得到的式(Ⅶ)化合物转化成式(I)所示的厄贝沙坦,得到式(I)的厄贝沙坦。

    DEUTERIUM-ENRICHED OSELTAMIVIR
    96.
    发明申请
    DEUTERIUM-ENRICHED OSELTAMIVIR 有权
    卓越的OSELTAMIVIR

    公开(公告)号:US20080319064A1

    公开(公告)日:2008-12-25

    申请号:US11765668

    申请日:2007-06-20

    CPC分类号: C07C233/52 C07B2200/05

    摘要: The present application describes deuterium-enriched oseltamivir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

    摘要翻译: 本申请描述了富含氘的奥司他韦,其药学上可接受的盐形式,以及使用其的治疗方法。

    PPAR ACTIVITY REGULATORS
    97.
    发明申请
    PPAR ACTIVITY REGULATORS 失效
    PPAR活性调节剂

    公开(公告)号:US20070276041A1

    公开(公告)日:2007-11-29

    申请号:US11753967

    申请日:2007-05-25

    IPC分类号: A61K31/198 C07C235/04

    摘要: The object of the present invention is to provide PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity.The present invention provides PPAR activity regulators which comprise an acylamide compound having the specific structure, prodrugs thereof, or pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明的目的是提供PPAR(过氧化物酶体增殖物激活受体)活性调节剂,其可广泛用于改善胰岛素抵抗和预防/治疗各种疾病如糖尿病,代谢综合征,高脂血症,高血压,血管 疾病,炎症,肝炎,脂肪肝,肝纤维化,NASH(非酒精性脂肪性肝炎)和肥胖症。 本发明提供了包含具有特定结构的酰基酰胺化合物,其前药或其药学上可接受的盐的PPAR活性调节剂。

    Process for preparation of Irbesartan
    98.
    发明申请
    Process for preparation of Irbesartan 失效
    厄贝沙坦制备方法

    公开(公告)号:US20070099973A1

    公开(公告)日:2007-05-03

    申请号:US11406919

    申请日:2006-04-19

    IPC分类号: A61K31/4188 C07D403/02

    摘要: A process for the preparation of Irbesartan of formula (I) using the steps of: (i) reacting 4′ aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V)  in an organic solvent and in the presence of an acid, without activating the —COOH group of compound of formula (V) to give 1-(2′cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII).  converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).

    摘要翻译: 使用以下步骤制备式(I)的厄贝沙坦的方法:(i)使式(VI)的4'-氨基甲基-2-氰基联苯与式(V)的1-维拉酰氨基环戊烷羧酸在有机溶剂 并且在酸存在下,不活化式(Ⅴ)化合物的-COOH基,得到式(Ⅶ)的1-(2'-氰基联苯-4-基 - 甲基氨基羰基)-1-戊酰基氨基环戊烷。 通过使式(Ⅶ)化合物与叠氮化三丁基锡在邻二甲苯中反应,得到式(ⅰ)中得到的式(Ⅶ)化合物转化成式(I)所示的厄贝沙坦,得到式(I)的厄贝沙坦。