公开(公告)号：EP0526642B1

公开(公告)日：1998-04-01

申请号：EP92900597.3

申请日：1991-12-13

申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA

发明人： FUJIMOTO, Masafumi ,  SAKURAI, Kensuke ,  MIHARA, Shinichi ,  NAKAMURA, Miharu ,  KONOIKE, Toshiro

IPC分类号： C07J63/00 ,  A61K31/705 ,  A61K35/78

CPC分类号： C07J63/008

公开(公告)号：EP0554455A1

公开(公告)日：1993-08-11

申请号：EP92910210.1

申请日：1992-05-14

申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA

发明人： KONOIKE, Toshiro ,  ARAKI, Yoshitaka

IPC分类号： C07F9/535 ,  C07F9/40 ,  C07C317/04 ,  C07F7/18 ,  C07D207/48

CPC分类号： C07F9/5352 ,  C07C315/04 ,  C07D207/48 ,  C07F7/1852 ,  C07F7/1856 ,  C07F7/1892 ,  C07F9/4006 ,  Y02P20/55 ,  C07C317/46

摘要： A process for synthesizing an optically active starting material, represented by general formula (I), for various medicines with a high optical purity in a good yield, wherein R¹ represents hydrogen or hydroxyl-protecting group: * represents an asymmetric carbon atom; R 2' represents hydrogen or optionally substituted lower alkyl; and Q represents -C=P(Ph)₃, -CH₂P(O)(OMe)₂ or -CN₂S(O)Me. More particularly, an intermediate for the synthesis of an optically active compound useful for inhibiting the activity of HMG-CoA reductase to thereby inhibit the biosynthesis of cholesterol; and a process for producing the intermediate.

摘要翻译： 用于以高收率合成具有高光学纯度的各种药物的由通式（I）表示的光学活性原料的方法，其中R 1表示氢或羟基保护基：*表示不对称碳原子 ; R 2表示氢或任选取代的低级烷基; Q表示-C = P（Ph）3，-CH 2 P（O）（OMe）2或-CN 2 S（O）Me。 更具体地说，涉及合成可用于抑制HMG-CoA还原酶活性从而抑制胆固醇生物合成的光学活性化合物的中间体; 和中间体的制造方法。

公开(公告)号：EP0554455B1

公开(公告)日：1997-12-17

申请号：EP92910210.1

申请日：1992-05-14

申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA

发明人： KONOIKE, Toshiro ,  ARAKI, Yoshitaka

IPC分类号： C07F9/535 ,  C07F9/40 ,  C07C317/04 ,  C07F7/18 ,  C07D207/48

CPC分类号： C07F9/5352 ,  C07C315/04 ,  C07D207/48 ,  C07F7/1852 ,  C07F7/1856 ,  C07F7/1892 ,  C07F9/4006 ,  Y02P20/55 ,  C07C317/46

摘要： A process for synthesizing an optically active starting material, represented by general formula (I), for various medicines with a high optical purity in a good yield, wherein R1 represents hydrogen or hydroxyl-protecting group: * represents an asymmetric carbon atom; R2' represents hydrogen or optionally substituted lower alkyl; and Q represents -C=P(Ph)¿3?, -CH2P(O)(OMe)2 or -CH2S(O)Me. More particularly, an intermediate for the synthesis of an optically active compound useful for inhibiting the activity of HMG-CoA reductase to thereby inhibit the biosynthesis of cholesterol; and a process for producing the intermediate.

公开(公告)号：EP0526642A1

公开(公告)日：1993-02-10

申请号：EP92900597.3

申请日：1991-12-13

申请人： SHIONOGI SEIYAKU KABUSHIKI KAISHA

发明人： FUJIMOTO, Masafumi ,  SAKURAI, Kensuke ,  MIHARA, Shinichi ,  NAKAMURA, Miharu ,  KONOIKE, Toshiro

IPC分类号： C07J63/00 ,  A61K31/705 ,  A61K35/78

CPC分类号： C07J63/008

摘要： A triterpene derivative represented by general formula (I), which has an antiendotheline activity and is useful for preventing and treating the diseases of the cardiovascular system, and a pharmaceutical composition thereof. In formula (I), R 1 represents hydrogen or a metabolic ester residue; R 3 represents an aryl or aromatic heterocyclic group which may be substituted; one of X and Y is hydroxy and the other is hydrogen, or alternatively X and Y are combined with each other to represent oxo; and Z represents oxygen or two hydrogen atoms.

摘要翻译： 由通式（I）表示的具有抗内丝素活性并可用于预防和治疗心血管系统疾病的三萜衍生物及其药物组合物。 在式（I）中，R 1表示氢或代谢酯残基; R 3表示可被取代的芳基或芳族杂环基; X和Y中的一个是羟基，另一个是氢，或者X和Y彼此结合以代表氧代​​; Z表示氧或两个氢原子。