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1. 发明公开

EP2036901A1 C-PHENYL 1-THIOGLUCITOL COMPOUND 有权
标题翻译： C-苯基1-硫代胡萝卜醇化合物
公开(公告)号：EP2036901A1
公开(公告)日：2009-03-18
申请号：EP07767824.1
申请日：2007-06-28
申请人： TAISHO PHARMACEUTICAL CO., LTD
发明人： KAKINUMA, Hiroyuki , OI, Takahiro , KOBASHI, Yohei , HASHIMOTO, Yuko , TAKAHASHI, Hitomi
IPC分类号： C07D335/02 , A61K31/382 , A61P3/10 , A61P43/00
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 C 1-6 alkyl group,
Y represents a C 1-6 alkylene group or -O-(CH 2 )n- (wherein n represents an integer of 1 to 5), and
Z represents -CONHR A or -NHCONHR B (provided that when Z represents -NHCONHR B , n is not 1),
wherein
R A represents a C 1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and -CONH 2 , and
R B represents a hydrogen atom or a C 1-6 alkyl group substituted with 1 to 3 substituents selected from the group consisting of a hydroxyl group and -CONH 2 ] 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代表氢原子或C1-6烷基，Y代表C1-6亚烷基或-O- （CH 2）n - （式中，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至3个选自羟基和-CONH 2的取代基，RB表示氢原子或被1至3个选自羟基和-CONH 2的取代基取代的C 1-6烷基] 由于它们通过抑制SGLT1活性而抑制糖（例如葡萄糖）的吸收，或者由于它们对糖（例如葡萄糖）的吸收和对泌尿的排泄效果的抑制作用，因此可用作糖尿病的预防剂或治疗剂糖通过抑制剂 SGLT1和SGLT2活动。

2. 发明公开

EP2607360A1 4-ISOPROPYL-6-METHOXYPHENYL GLUCITOL COMPOUND 失效
标题翻译： 4-异丙基-6-甲氧基苯基葡萄糖醇-Verbindung
公开(公告)号：EP2607360A1
公开(公告)日：2013-06-26
申请号：EP11818240.1
申请日：2011-08-19
申请人： Taisho Pharmaceutical Co., Ltd.
发明人： KAKINUMA, Hiroyuki , KOBASHI, Yohei , CHONAN, Tomomichi , SHIOZAWA, Fumiyasu , IWATA, Yuki , OI, Takahiro , KAWABE, Kenichi
IPC分类号： C07D309/10 , A61K31/351 , A61P3/10 , A61P43/00
CPC分类号： A61K31/7034 , A61K31/351 , C07D309/10
摘要： A compound, which inhibits SGLT1 (sodium-dependent glucose transporter 1) activity to suppress absorption of glucose or the like, thereby suppressing abnormal glucose tolerance or postprandial hyperglycemia in diabetes, is provided. Specifically, a 4-isopropyl-6-methoxyphenyl glucitol compound represented by the following formula (I), or a pharmaceutically acceptable salt thereof, is provided:
摘要翻译：提供抑制SGLT1（钠依赖性葡萄糖转运体1）活性以抑制葡萄糖等的吸收，从而抑制糖尿病中的异常葡萄糖耐量或餐后高血糖的化合物。具体地，提供由下式（I）表示的4-异丙基-6-甲氧基苯基硬糖醇化合物或其药学上可接受的盐：

3. 发明公开

EP2103607A1 1-PHENYL 1-THIO-D-GLUCITOL DERIVATIVE 审中-公开
标题翻译： 1-苯基1-硫代-D-山梨醇衍生物
公开(公告)号：EP2103607A1
公开(公告)日：2009-09-23
申请号：EP07850604.5
申请日：2007-12-14
申请人： TAISHO PHARMACEUTICAL CO., LTD
发明人： KAKINUMA, Hiroyuki , OI, Takahiro , HASHIMOTO, Yuko , TAKAHASHI, Hitomi , KOBASHI, Yohei , IWATA, Yuki , KAWABE, Kenichi , TAKAHASHI, Masato
IPC分类号： C07D335/02 , A61K31/382 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/10 , A61P9/04 , A61P9/10 , A61P9/12 , A61P13/12 , A61P19/06 , A61P25/00 , A61P27/02 , A61P31/04 , A61P43/00
CPC分类号： C07D335/02
摘要： A 1-phenyl 1-thio-D-glucitol compound represented by formula (I) or the like:

or a pharmaceutically acceptable salt thereof or a hydrate thereof, or a pharmaceutical preparation comprising the same as an active ingredient is useful as a novel type of prophylactic or therapeutic agent for diabetes, diabetes-related diseases or diabetic complications, which inhibits both SGLT1 and SGLT2 activities to achieve not only suppression of glucose absorption from the digestive tract but also excretion of urinary sugars.
摘要翻译：由式（I）等表示的1-苯基1-硫代-D-山梨醇化合物或其药学上可接受的盐或其水合物或包含其作为活性成分的药物制剂可用作新型的糖尿病相关疾病或糖尿病并发症的预防或治疗剂，其抑制SGLT1和SGLT2活性以不仅实现消化道中葡萄糖吸收的抑制，而且实现尿糖的排泄。

4. 发明授权

EP2607360B1 4-Isopropyl-6-methoxyphenyl glucitol compound 失效
标题翻译： 4-异丙基-6-甲氧基苯基葡萄糖醇化合物
公开(公告)号：EP2607360B1
公开(公告)日：2015-08-19
申请号：EP11818240.1
申请日：2011-08-19
申请人： Taisho Pharmaceutical Co., Ltd.
发明人： KAKINUMA, Hiroyuki , KOBASHI, Yohei , CHONAN, Tomomichi , SHIOZAWA, Fumiyasu , IWATA, Yuki , OI, Takahiro , KAWABE, Kenichi
IPC分类号： C07D309/10 , A61K31/351 , A61P3/10 , A61P43/00
CPC分类号： A61K31/7034 , A61K31/351 , C07D309/10

5. 发明授权

EP2076503B1 C-PHENYL GLYCITOL COMPOUND FOR THE TREATMENT OF DIABETES 有权
标题翻译： C-PHENYLGLYCITOLVERBINDUNG用于治疗糖尿病
公开(公告)号：EP2076503B1
公开(公告)日：2013-07-17
申请号：EP07744087.3
申请日：2007-05-18
申请人： TAISHO PHARMACEUTICAL CO., LTD
发明人： KAKINUMA, Hiroyuki , KOBASHI, Yohei , HASHIMOTO, Yuko , OI, Takahiro , TAKAHASHI, Hitomi , AMADA, Hideaki , IWATA, Yuki
IPC分类号： C07D309/12 , C07D405/10 , A61K31/351 , A61P3/10
CPC分类号： C07D405/10 , C07D309/12

6. 发明授权

EP2036901B1 C-PHENYL 1-THIOGLUCITOL COMPOUND 有权
标题翻译： C-苯基1-硫代胡萝卜醇化合物
公开(公告)号：EP2036901B1
公开(公告)日：2013-05-01
申请号：EP07767824.1
申请日：2007-06-28
申请人： TAISHO PHARMACEUTICAL CO., LTD
发明人： KAKINUMA, Hiroyuki , OI, Takahiro , KOBASHI, Yohei , HASHIMOTO, Yuko , TAKAHASHI, Hitomi
IPC分类号： C07H7/04 , C07D335/02 , A61K31/382 , A61P3/10 , A61K31/7034
CPC分类号： C07D335/02 , C07H7/04

7. 发明授权

EP1845095B1 1-THIO-D-GLUCITOL DERIVATIVES 有权
标题翻译： 1-硫代-D-山梨醇衍生物
公开(公告)号：EP1845095B1
公开(公告)日：2011-09-07
申请号：EP06711505.5
申请日：2006-01-10
申请人： TAISHO PHARMACEUTICAL CO., LTD
发明人： KAKINUMA, Hiroyuki , HASHIMOTO, Yuko , OI, Takahiro , TAKAHASHI, Hitomi
IPC分类号： C07D335/00 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D417/10 , C07D495/04 , A61K31/4178 , A61K31/382 , A61P3/10
CPC分类号： C07D409/14 , A61K31/382 , A61K31/7004 , A61K45/06 , C07D335/02 , C07D409/04 , C07D409/10 , C07D417/10 , C07D495/04 , A61K2300/00
摘要： It is intended to provide a 1-thio-D-glucitol compound represented by the following formula which shows an effect of inhibiting the activity of SGLT2, a pharmaceutically acceptable salt thereof or a hydrate thereof; and a drug containing such a compound as the active ingredient, in particular, a preventive or a remedy for diabetes, diabetes-associated diseases or diabetic complications. It is also intended to provide a method of producing the 1-thio-D-glucitol compound and an intermediate thereof.
摘要翻译：旨在提供下式所示的1-硫代-D-葡萄糖醇化合物，其显示出抑制SGLT2，其药学上可接受的盐或其水合物的活性的作用; 和含有这种化合物作为活性成分的药物，特别是用于糖尿病，糖尿病相关疾病或糖尿病并发症的预防剂或治疗剂。还意图提供一种生产1-硫代-D-葡萄糖醇化合物及其中间体的方法。

8. 发明公开

EP2076503A2 C-PHENYL GLYCITOL COMPOUND FOR THE TREATMENT OF DIABETES 有权
标题翻译： C-PHENYLGLYCITOLVERBINDUNG用于治疗糖尿病
公开(公告)号：EP2076503A2
公开(公告)日：2009-07-08
申请号：EP07744087.3
申请日：2007-05-18
申请人： TAISHO PHARMACEUTICAL CO., LTD
发明人： KAKINUMA, Hiroyuki , KOBASHI, Yohei , HASHIMOTO, Yuko , OI, Takahiro , TAKAHASHI, Hitomi , AMADA, Hideaki , IWATA, Yuki
IPC分类号： C07D309/12 , C07D405/10 , A61K31/351 , A61P3/10
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, Formula (A) or Formula (B).

9. 发明授权

EP2398786B1 4 -ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS 失效
标题翻译： 4-异丙基苯基硫酸酯化合物作为SGLT1抑制剂
公开(公告)号：EP2398786B1
公开(公告)日：2012-12-12
申请号：EP10708391.7
申请日：2010-02-23
申请人： Taisho Pharmaceutical Co., Ltd.
发明人： KAKINUMA, Hiroyuki , KOBASHI, Yohei , CHONAN, Tomomichi , OI, Takahiro , SHIOZAWA, Fumiyasu , IWATA, Yuki , KAWABE, Kenichi
IPC分类号： C07D309/10 , A61K31/351 , A61P3/10
CPC分类号： C07D309/10

10. 发明公开

EP2398786A1 4 -ISOPROPYLPHENYL GLUCITOL COMPOUNDS AS SGLT1 INHIBITORS 失效
标题翻译： 4-异丙基苯基硫酸酯化合物作为SGLT1抑制剂
公开(公告)号：EP2398786A1
公开(公告)日：2011-12-28
申请号：EP10708391.7
申请日：2010-02-23
申请人： Taisho Pharmaceutical Co., Ltd.
发明人： KAKINUMA, Hiroyuki , KOBASHI, Yohei , CHONAN, Tomomichi , OI, Takahiro , SHIOZAWA, Fumiyasu , IWATA, Yuki , KAWABE, Kenichi
IPC分类号： C07D309/10 , A61K31/351 , 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: [Chem. 1] wherein R
1 represents a hydrogen atom, etc., R
2 represents a methyl group, etc., R
3 represents a C
1-4 alkyl group substituted with an amino group(s), etc., and R
4 represents a hydrogen atom, etc.
摘要翻译：本发明提供了4-异丙基苯基葡萄糖醇化合物，其没有倾向于在体内累积并抑制SGLT1活性以通过抑制小肠中的葡萄糖吸收来抑制餐后高血糖（或葡萄糖耐量降低），由此该化合物，例如，可以抑制糖尿病和代谢综合征的发作或可以治疗这些疾病。由下式（I）表示的4-异丙基苯基山梨醇化合物或其药学上可接受的盐： 1]式中，R 1表示氢原子等，R 2表示甲基等，R 3表示被氨基取代的C 1-4烷基等，R 4表示氢原子等

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