公开(公告)号：US07259155B2

公开(公告)日：2007-08-21

申请号：US10838297

申请日：2004-05-05

申请人： Yasuhiro Sakai ,  Kazuyoshi Miyata ,  Takahiro Tomoyasu ,  Akiyoshi Kuroda ,  Yasuhide Inoue ,  Akifumi Hagi ,  Shinya Miki ,  Norihiro Yoshinaga ,  Masako Doi ,  Yoshihiko Tsuda ,  Seiichirou Kanou

发明人： Yasuhiro Sakai ,  Kazuyoshi Miyata ,  Takahiro Tomoyasu ,  Akiyoshi Kuroda ,  Yasuhide Inoue ,  Akifumi Hagi ,  Shinya Miki ,  Norihiro Yoshinaga ,  Masako Doi ,  Yoshihiko Tsuda ,  Seiichirou Kanou

IPC分类号： A61K31/517 ,  A61K31/675 ,  A01N43/54 ,  C07D239/72 ,  C07D265/32 ,  C07D413/00 ,  C07F9/02 ,  C07D401/00 ,  C07D403/02 ,  C07F9/28 ,  C07F9/547

CPC分类号： C07F9/65586 ,  C07F9/65068 ,  C07F9/65583

摘要： The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; R5 is phenyl having on the phenyl ring 1–3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that R5 is not mono(lower alkoxy)pheny; and R6 is lower alkyl; and an ACAT-1 inhibitor containing the compound as an active ingredient.

摘要翻译： 本发明提供由通式其中R 1，R 2，R 3和R 4代表的膦酸二酯化合物， / SUB>相同或不同，代表氢，卤素，低级烷基或低级烷氧基; R 5是在苯环上具有1-3个选自低级烷基，卤素取代的低级烷基，低级烷氧基，卤素取代的低级烷氧基，苯氧基，苄氧基，羟基， 卤素，硝基，低级烷硫基，二（低级烷基）氨基，低级链烷氨基，吡咯烷基和苯基等，条件是R 5不是单（低级烷氧基）苯基; 和R 6是低级烷基; 和含有该化合物作为活性成分的ACAT-1抑制剂。

公开(公告)号：US20050256087A1

公开(公告)日：2005-11-17

申请号：US10838297

申请日：2004-05-05

申请人： Yasuhiro Sakai ,  Kazuyoshi Miyata ,  Takahiro Tomoyasu ,  Akiyoshi Kuroda ,  Yasuhide Inoue ,  Akifumi Hagi ,  Shinya Miki ,  Norihiro Yoshinaga ,  Masako Doi ,  Yoshihiko Tsuda ,  Seiichirou Kanou

发明人： Yasuhiro Sakai ,  Kazuyoshi Miyata ,  Takahiro Tomoyasu ,  Akiyoshi Kuroda ,  Yasuhide Inoue ,  Akifumi Hagi ,  Shinya Miki ,  Norihiro Yoshinaga ,  Masako Doi ,  Yoshihiko Tsuda ,  Seiichirou Kanou

IPC分类号： A61K31/675 ,  C07F9/6506 ,  C07F9/6509 ,  C07F9/6558

CPC分类号： C07F9/65586 ,  C07F9/65068 ,  C07F9/65583

摘要： The present invention provides a phosphonic acid diester compound represented by General Formula wherein R1, R2, R3 and R4 are the same or different, and represent hydrogen, halogen, lower alkyl or lower alkoxy; R5 is phenyl having on the phenyl ring 1-3 substituents selected from the group consisting of lower alkyl, halogen-substituted lower alkyl, lower alkoxy, halogen-substituted lower alkoxy, phenoxy, benzyloxy, hydroxyl, halogen, nitro, lower alkylthio, di(lower alkyl)amino, lower alkanolyamino, pyrrolidinyl and phenyl, or the like, provided that R5 is not mono(lower alkoxy)pheny; and R6 is lower alkyl; and an ACAT-1 inhibitor containing the compound as an active ingredient.

摘要翻译： 本发明提供由通式其中R 1，R 2，R 3和R 4代表的膦酸二酯化合物， / SUB>相同或不同，代表氢，卤素，低级烷基或低级烷氧基; R 5是在苯环上具有1-3个选自低级烷基，卤素取代的低级烷基，低级烷氧基，卤素取代的低级烷氧基，苯氧基，苄氧基，羟基， 卤素，硝基，低级烷硫基，二（低级烷基）氨基，低级链烷氨基，吡咯烷基和苯基等，条件是R 5不是单（低级烷氧基）苯基; 和R 6是低级烷基; 和含有该化合物作为活性成分的ACAT-1抑制剂。