公开(公告)号：US09500653B2

公开(公告)日：2016-11-22

申请号：US13992076

申请日：2011-12-06

申请人： Craig M. Crews ,  Hyun Seop Tae ,  Ashley R. Schneekloth ,  Taavi Neklesa ,  Thomas Sundberg

发明人： Craig M. Crews ,  Hyun Seop Tae ,  Ashley R. Schneekloth ,  Taavi Neklesa ,  Thomas Sundberg

IPC分类号： G01N33/573 ,  A61K47/48 ,  C07K1/13 ,  C12N9/14 ,  G01N33/50

CPC分类号： G01N33/573 ,  A61K47/48015 ,  A61K47/52 ,  C07K1/13 ,  C07K2319/20 ,  C07K2319/95 ,  C12N9/14 ,  G01N33/5008 ,  G01N2500/10

摘要： The present invention includes compounds that are useful in perturbing or disrupting the function of a transmembrane or intracellular protein, whereby binding of a compound to the transmembrane or intracellular protein induces proteasomal degradation of the transmembrane or intracellular protein. The present invention further includes a method of inducing proteasomal degradation of a transmembrane or intracellular protein. The present invention further includes a method of identifying or validating a protein of interest as a therapeutic target for treatment of a disease state or condition.

摘要翻译： 本发明包括可用于扰乱或破坏跨膜或细胞内蛋白质的功能的化合物，由此化合物与跨膜或细胞内蛋白质的结合诱导跨膜或细胞内蛋白质的蛋白酶体降解。 本发明还包括诱导跨膜或细胞内蛋白质的蛋白酶体降解的方法。 本发明还包括鉴定或验证感兴趣的蛋白质作为治疗疾病状态或病症的治疗靶标的方法。

公开(公告)号：US20110112309A1

公开(公告)日：2011-05-12

申请号：US12734500

申请日：2008-04-04

申请人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoe Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

发明人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoe Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

IPC分类号： C07D405/06 ,  C07D207/34 ,  C07D319/06

CPC分类号： C07D319/06 ,  C07D207/34 ,  C07D405/06

摘要： The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.

摘要翻译： 本发明涉及可用于合成阿托伐他汀的制备方法，更具体地说，一种制备阿托伐他汀的方法在治疗高脂血症方面是有效的，包括保护原料顺式叔丁基-6-取代的C3和C5位的二羟基 -3,5-二羟基己酸酯与原甲酸三烷基酯反应，将末端硝基或氰基还原成胺基，通过与4-氟苯-2-卤代乙酸乙酯和异丁酰氯依次反应进行N-烷基化，用JV，3-二苯基丙酰胺 ，进行脱保护和水解。

公开(公告)号：US08124790B2

公开(公告)日：2012-02-28

申请号：US12734500

申请日：2008-04-04

申请人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoi Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

发明人： Dong-Ock Cho ,  Younja Kwon ,  Kyeong-Hoi Cha ,  Yeongsook Kim ,  Hyun-Seop Tae

IPC分类号： C07D207/333 ,  C07D405/06 ,  C07D319/06

CPC分类号： C07D319/06 ,  C07D207/34 ,  C07D405/06

摘要： The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.

摘要翻译： 本发明涉及可用于合成阿托伐他汀的制备方法，更具体地说，一种制备阿托伐他汀的方法在治疗高脂血症方面是有效的，包括保护原料顺式叔丁基-6-取代的C3和C5位的二羟基 -3,5-二羟基己酸酯与原甲酸三烷基酯反应，将末端硝基或氰基还原成胺基，通过与4-氟苯-2-卤代乙酸乙酯和异丁酰氯依次反应进行N-烷基化，用JV，3-二苯基丙酰胺 ，进行脱保护和水解。