C-PHENYL GLYCITOL COMPOUND
    1.
    发明申请
    C-PHENYL GLYCITOL COMPOUND 有权
    C-PHENYL GLYCITOL化合物

    公开(公告)号:US20100022460A1

    公开(公告)日:2010-01-28

    申请号:US12301463

    申请日:2007-05-18

    IPC分类号: A61K31/70 C07H1/00

    CPC分类号: C07D405/10 C07D309/12

    摘要: Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, —O—(CH2)n— (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is —NHC(═NH)NH2 or —NHCON(RB)RC, n is not 1, Z is —CONHRA, —NHC(═NH)NH2 or —NHCON(RB)RC,

    摘要翻译: 提供了可以通过抑制SGLT1活性和SGLT2活性而作为糖尿病的预防或治疗剂的新颖的C-苯基糖醇化合物,从而表现出葡萄糖吸收抑制作用和尿葡萄糖排泄作用。 由下式(I)表示的C-苯基糖醇化合物或其药学上可接受的盐或其水合物,其中R 1和R 2相同或不同,表示氢原子,羟基,C 1-6烷基, C 1-6烷氧基或卤原子,R 3为氢原子,C 1-6烷基,C 1-6烷氧基或卤素原子,Y为C 1-6亚烷基,-O-(CH 2)n - (n为1〜4的整数)或C 2-6亚烯基,条件是当Z为-NHC(-NH)NH 2或-NHCON(RB)RC时,n不为1,Z为-CONHRA, - NHC(-NH)NH 2或-NHCON(RB)RC,

    C-phenyl glycitol compound
    2.
    发明授权
    C-phenyl glycitol compound 有权
    C-苯基甘氨醇化合物

    公开(公告)号:US07973012B2

    公开(公告)日:2011-07-05

    申请号:US12301463

    申请日:2007-05-18

    CPC分类号: C07D405/10 C07D309/12

    摘要: Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action. A C-phenyl glycitol compound represented by Formula (I) below or a pharmaceutically acceptable salt thereof or a hydrate thereof wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, R3 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkoxy group or a halogen atom, Y is a C1-6 alkylene group, —O—(CH2)n- (n is an integer of 1 to 4) or a C2-6 alkenylene group, provided that when Z is —NHC(═NH)NH2 or —NHCON(RB)RC, n is not 1, Z is —CONHRA, —NHC(═NH)NH2 or —NHCON(RB)RC,

    摘要翻译: 提供了可以通过抑制SGLT1活性和SGLT2活性而作为糖尿病的预防或治疗剂的新颖的C-苯基糖醇化合物,从而表现出葡萄糖吸收抑制作用和尿葡萄糖排泄作用。 由下式(I)表示的C-苯基糖醇化合物或其药学上可接受的盐或其水合物,其中R 1和R 2相同或不同,表示氢原子,羟基,C 1-6烷基, C 1-6烷氧基或卤原子,R 3为氢原子,C 1-6烷基,C 1-6烷氧基或卤素原子,Y为C 1-6亚烷基,-O-(CH 2)n - (n为1〜4的整数)或C 2-6亚烯基,条件是当Z为-NHC(= NH)NH 2或-NHCON(RB)RC时,n不为1,Z为-CONHRA, - NHC(= NH)NH 2或-NHCON(RB)RC,

    C-phenyl 1-thioglucitol compound
    4.
    发明授权
    C-phenyl 1-thioglucitol compound 失效
    C-苯基1-硫代葡萄糖醇化合物

    公开(公告)号:US08115017B2

    公开(公告)日:2012-02-14

    申请号:US12305157

    申请日:2007-06-28

    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。

    C-PHENYL 1-THIOGLUCITOL COMPOUND
    5.
    发明申请
    C-PHENYL 1-THIOGLUCITOL COMPOUND 失效
    C-PHENYL 1-THIOGLUCITOL化合物

    公开(公告)号:US20100004465A1

    公开(公告)日:2010-01-07

    申请号:US12305157

    申请日:2007-06-28

    IPC分类号: C07D335/02

    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SGLT2两种活动。

    4-isopropylphenyl glucitol compounds as SGLT1 inhibitors
    6.
    发明授权
    4-isopropylphenyl glucitol compounds as SGLT1 inhibitors 有权
    4-异丙基苯基葡糖醇化合物作为SGLT1抑制剂

    公开(公告)号:US08466113B2

    公开(公告)日:2013-06-18

    申请号:US13202523

    申请日:2010-02-23

    CPC分类号: C07D309/10

    摘要: The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases.A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.

    摘要翻译: 本发明提供了通过抑制小肠中的葡萄糖吸收而不具有积累在体内的倾向而抑制SGLT1活性来抑制餐后高血糖(或葡萄糖耐量降低)的4-异丙基苯基甘醇醇化合物,其中, 可以抑制糖尿病和代谢综合征的发病,或者可以治疗这些疾病。 由下式(I)表示的4-异丙基苯基硬糖醇化合物或其药学上可接受的盐:其中R1表示氢原子等,R2表示甲基等,R3表示被 氨基等,R4表示氢原子等。

    4-ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS
    9.
    发明申请
    4-ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS 有权
    4-ISOPROPYLPHENYL GLUCITOL化合物作为SGLT1抑制剂

    公开(公告)号:US20110306759A1

    公开(公告)日:2011-12-15

    申请号:US13202523

    申请日:2010-02-23

    IPC分类号: C07H7/04 A61P3/10

    CPC分类号: C07D309/10

    摘要: The present invention provides 4-isopropylphenyl glucitol compounds which have no tendency to accumulate in the body and which inhibit SGLT1 activity to suppress postprandial hyperglycemia (or impaired glucose tolerance) through suppression of glucose absorption in the small intestine, whereby the compounds, for example, can suppress the onset of diabetes and metabolic syndrome or can treat these diseases.A 4-isopropylphenyl glucitol compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 represents a hydrogen atom, etc., R2 represents a methyl group, etc., R3 represents a C1-4 alkyl group substituted with an amino group(s), etc., and R4 represents a hydrogen atom, etc.

    摘要翻译: 本发明提供了通过抑制小肠中的葡萄糖吸收而不具有积累在体内的倾向而抑制SGLT1活性来抑制餐后高血糖(或葡萄糖耐量降低)的4-异丙基苯基甘醇醇化合物,其中, 可以抑制糖尿病和代谢综合征的发病,或者可以治疗这些疾病。 由下式(I)表示的4-异丙基苯基硬糖醇化合物或其药学上可接受的盐:其中R1表示氢原子等,R2表示甲基等,R3表示被 氨基等,R4表示氢原子等。