公开(公告)号：US08115017B2

公开(公告)日：2012-02-14

申请号：US12305157

申请日：2007-06-28

申请人： Hiroyuki Kakinuma ,  Takahiro Oi ,  Yohei Kobashi ,  Yuko Hashimoto ,  Hitomi Takahashi

发明人： Hiroyuki Kakinuma ,  Takahiro Oi ,  Yohei Kobashi ,  Yuko Hashimoto ,  Hitomi Takahashi

IPC分类号： C70D335/02

CPC分类号： C07D335/02 ,  C07H7/04

摘要： C-phenyl 1-thioglucitol compounds of the following formula (I) or pharmaceutically acceptable salts thereof or hydrates thereof: [wherein X represents a hydrogen atom or a C1-6 alkyl group, Y represents a C1-6 alkylene group or —O—(CH2)n- (wherein n represents an integer of 1 to 5), and Z represents —CONHRA or —NHCONHRB (provided that when Z represents —NHCONHRB, n is not 1), wherein RA represents a C1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and —CONH2, and RB represents a hydrogen atom or a C1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and —CONH2] are useful as prophylactic or therapeutic agents for diabetes, because of their suppressive effect on sugar (e.g., glucose) absorption through inhibition of SGLT1 activity, or alternatively, because of their suppressive effect on sugar (e.g., glucose) absorption and excretory effect on urinary sugars through inhibition of both SGLT1 and SGLT2 activities.

摘要翻译： 下式（I）的C-苯基-1-硫代葡萄糖醇化合物或其药学上可接受的盐或其水合物：[其中X表示氢原子或C1-6烷基，Y表示C1-6亚烷基或-O- （CH 2）n - （其中n表示1〜5的整数），Z表示-CONHRA或-NHCONHRB（条件是当Z表示-NHCONHRB时，n不为1），其中RA表示C1-6烷基取代 具有1〜3个选自羟基和-CONH 2的取代基，RB表示氢原子或被1〜3个选自羟基和-CONH 2的取代基取代的C 1-6烷基] 可用作糖尿病的预防或治疗剂，因为它们通过抑制SGLT1活性而对糖（例如葡萄糖）的吸收具有抑制作用，或者由于其对糖（例如葡萄糖）对尿液的吸收和排泄作用的抑制作用 糖 通过抑制SGLT1和SGLT2两种活性。