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1. 发明专利

JP2010001291A Method for producing glycolipid derivative 有权
标题翻译：生产甘油衍生物的方法
公开(公告)号：JP2010001291A
公开(公告)日：2010-01-07
申请号：JP2009159985
申请日：2009-07-06
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61P35/00 , A61P37/04 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a glycolipid derivative of formula (e), having antitumor activity and immunoactivating effect, stable to glucosidase metabolism, acids and bases, and storable for a long period at room temperature.
SOLUTION: The method for producing the glycolipid derivative of formula (e) includes conducting a catalytic reduction of a compound of formula (d). In the formulas (d) and (e), R
0 is -OH, -NH
2 or -NHAc group; W is a 9-17C saturated or unsaturated hydrocarbon chain; X is a 11-25C saturated or unsaturated hydrocarbon chain; Z is -CO- or -SO
2 -; and b is an integer of 1-5.
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供一种具有抗肿瘤活性和免疫活化作用的式（e）的糖脂衍生物的制备方法，其对葡糖苷酶代谢，酸和碱稳定，并可在室温下长时间储存。解决方案：制备式（e）的糖脂衍生物的方法包括进行式（d）化合物的催化还原。在式（d）和（e）中，R 0是-SH，-NHC 2或-NHAc基团; W是9-17C饱和或不饱和烃链; X是11-25℃饱和或不饱和烃链; Z是-CO-或-SO- SB 2。 b为1-5的整数。版权所有（C）2010，JPO＆INPIT

2. 发明专利

JP2009263391A New glycolipid derivative and pharmaceutical preparation comprising the same as active component 有权
标题翻译：新型GLYCOLIPID衍生物和药物制剂，将其作为活性成分
公开(公告)号：JP2009263391A
公开(公告)日：2009-11-12
申请号：JP2009159984
申请日：2009-07-06
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/70 , A61P35/00 , A61P37/04 , C07H15/14
摘要： PROBLEM TO BE SOLVED: To provide a glycolipid derivative with an α-C-glycoside bond, having a powerful antitumor activity and immunostimulation action, stable to glucosidase metabolism, acids and bases, and stored for a long time at room temperature.
SOLUTION: There is provided the compound represented by general formula (I) or its pharmaceutically permissible salts, [wherein W is a 9-17C saturated or unsaturated hydrocarbon chain and further contains a hydroxy group in some cases, X is an 11-25C saturated or unsaturated hydrocarbon chain and further contains a hydroxy group in some cases. Y represents -(CH
2 )
a -CH=CH-(CH
2 )
a - or -(CH
2 )
a - (in the proviso that a, a' are each an integer of 0-5, and a+a'≤5), Z represents -CO- or -SO
2 -, R represents a -CH
2 OH, -CO
2 H, -CH
2 OCH
2 CO
2 H, or -CH
2 OSO
3 H group, and R
0 represents a -OH, -NH
2 , or -NHAc group].
COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：待解决的问题：提供具有强大的抗肿瘤活性和免疫刺激作用的具有α-C-糖苷键的糖脂衍生物，对葡糖苷酶代谢，酸和碱稳定，并在室温下长时间储存。提供由通式（I）表示的化合物或其药学上可允许的盐[其中W是9-17C饱和或不饱和烃链，并且在某些情况下还含有羟基，X是11 -25℃饱和或不饱和烃链，在某些情况下还含有羟基。 Y表示 - （CH 2 ） -CH = CH-（CH 2 （条件是a，a'分别为0-5的整数，a + a'≤5），Z表示-CO - 或 - -SO 2 - ， - R表示-CH 2 S 2，-CO 2 SBH 2， CH 2，OCH 2，SO 2，SO 2，CH 3，SO 2，CH 2，表示-OH，-NH SB 2或-NHAc基团]。版权所有（C）2010，JPO＆INPIT

3. 发明专利

JP2004217601A Preventive or therapeutic agent for autoimmune disease and immunosuppressant 有权
公开(公告)号：JP2004217601A
公开(公告)日：2004-08-05
申请号：JP2003009703
申请日：2003-01-17
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , NODA ATSUSHI , OKURA YASUSHI
IPC分类号： C07H15/14 , A61K31/351 , A61K31/70 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/06 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P17/14 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , A61P37/02 , A61P37/06 , A61P37/08 , C07D309/10
摘要： PROBLEM TO BE SOLVED: To obtain a prophylactic or therapeutic agent for autoimmune diseases and an immunosuppressant.
SOLUTION: The prophylactic or therapeutic agent for autoimmune diseases and the immunosuppressant comprise as an effective ingredient a compound represented by formula (I) [wherein W is a 9-17C saturated or unsaturated carbon chain optionally bearing a hydroxy group; X is a 11-25C saturated or unsaturated carbon chain optionally bearing a hydroxy group; Y is (CH
2 )
a -CH=CH-(CH
2 )
b , (CH
2 )
a (wherein (a) and (b) are each an integer of 0-5; and (a+b) is at most 5), S(O)
0-2 CH
2 or NHCH
2 ; Z is CO or SO
2 ; R is a CH
2 OH, CO
2 H, CO
2 OCH
2 CO
2 H or CH
2 OSO
3 H group; and R
0 is an OH, NH
2 or NHAc group] or a pharmacologically acceptable salt thereof.
COPYRIGHT: (C)2004,JPO&NCIPI

4. 发明专利

JP2009062381A Glucolipid derivative, its manufacturing method and medicine containing it as effective component 有权
标题翻译：葡萄糖衍生物及其制造方法和药物作为有效成分
公开(公告)号：JP2009062381A
公开(公告)日：2009-03-26
申请号：JP2008263962
申请日：2008-10-10
申请人： Kotobuki Seiyaku Kk , 壽製薬株式会社
发明人： TOMIYAMA YASUSHI , YANAGISAWA TAKASHI , FUTAMURA MASAYUKI , NODA ATSUSHI , TOMIYAMA TAKESHI
IPC分类号： C07D309/10 , A61K31/351 , A61P35/00 , A61P35/04 , A61P37/04
摘要： PROBLEM TO BE SOLVED: To provide a glucolipid derivative having an α-S-glucosidic linkage which is useful as an antitumor medicine and an immunopotentiator, and its manufacturing method, and medicines containing it as an effective component. SOLUTION: This glucolipid derivative is a compound represented by general formula (I) (wherein W is a 9-17C saturated or unsaturated carbon chain and further in some case contains a hydroxy group, X is an 11-25C saturated or unsaturated carbon chain and further in some case contains a hydroxy group, Y represents -S(O) 0-2 CH 2 -, Z represents -CO- or -SO 2 -, R represents -CH 2 OH, -CO 2 H, -CO 2 OCH 2 CO 2 H, or -CH 2 OSO 3 H group, and R 0 represents -OH, -NH 2 , or -NHAc group), or its pharmaceutically permissible salts. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可用作抗肿瘤药和免疫增强剂的具有α-S-糖苷键的糖脂衍生物及其制备方法以及含有它作为有效成分的药物。解决方案：该糖脂衍生物为通式（I）表示的化合物（其中W为9-17C饱和或不饱和碳链，并且在某些情况下还含有羟基，X为11-25℃饱和或不饱和的碳链，并且在某些情况下还含有羟基，Y表示-S（O），S表示-CO-或-SO 2 - ，R表示-CH 2 OH，-CO 2 H，-CO 2 / SB> CO 2 H或-CH 2 OSO 3 H基，R SB 0表示-OH ，-NH 2 SBA或-NHAc基团）或其药学上允许的盐。版权所有（C）2009，JPO＆INPIT

5. 发明专利

JP2009046489A C-glycoside derivative or salt thereof 有权
标题翻译： C-GLYCOSIDE衍生物或其盐
公开(公告)号：JP2009046489A
公开(公告)日：2009-03-05
申请号：JP2008222927
申请日：2008-08-29
申请人： Astellas Pharma Inc , Kotobuki Seiyaku Kk , アステラス製薬株式会社 , 壽製薬株式会社
发明人： IMAMURA MASAKAZU , MURAKAMI TAKESHI , SHIRAKI RYOTA , IKUGAI KAZUHIRO , SUGANE TAKASHI , IWASAKI SHIRO , KUROSAKI HIDESHI , TOMIYAMA YASUSHI , NODA ATSUSHI , KITSUTA KAYOKO , KOBAYASHI YOSHINORI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/381 , A61K31/4025 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P5/50 , A61P43/00 , C07D207/06 , C07D333/12 , C07D333/16 , C07D333/54 , C07D405/04 , C07D405/10 , C07D407/04 , C07D407/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/10 , C07D493/04 , C07D495/04
CPC分类号： C07D495/04 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , C07D405/10 , C07D407/10 , C07D409/10 , C07D413/10 , C07D417/10
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as an agent for treating various types of diabetes such as non-insulin-dependent diabetes (type II diabetes) and insulin-dependent diabetes (type I diabetes) and in addition, various diabetes-related diseases including insulin-resistant diseases and obesity. SOLUTION: This compound is a C-glycoside derivative having hetero rings each containing at least one heteroatom selected from N, S, and O as a substituent or is a salt thereof. COPYRIGHT: (C)2009,JPO&INPIT
摘要翻译：待解决的问题：提供可用作治疗各种类型的糖尿病如非胰岛素依赖性糖尿病（II型糖尿病）和胰岛素依赖型糖尿病（I型糖尿病）的药剂的化合物，另外还可以使用各种糖尿病相关疾病，包括胰岛素抵抗疾病和肥胖。解决方案：该化合物是具有各自含有至少一个选自N，S和O的杂原子作为取代基的杂环的C-糖苷衍生物或其盐。版权所有（C）2009，JPO＆INPIT

6. 发明专利

JP2004359630A Difluorodiphenylmethane derivative and its salt 审中-公开
公开(公告)号：JP2004359630A
公开(公告)日：2004-12-24
申请号：JP2003161718
申请日：2003-06-06
申请人： Kotobuki Seiyaku Kk , Yamanouchi Pharmaceut Co Ltd , 壽製薬株式会社 , 山之内製薬株式会社
发明人： TOMIYAMA YASUSHI , NODA ATSUSHI , KITSUTA KAYOKO , KOBAYASHI YOSHINORI , IMAMURA MASAKAZU , KUROSAKI HIDESHI
IPC分类号： C07D309/10 , A61K31/351 , A61P3/04 , A61P3/10
摘要： PROBLEM TO BE SOLVED: To provide a compound useful as a Na
+ -glucose cotransporter inhibitor, particularly as a treatment or preventive agent for non-insulin-dependent diabetes mellitus (type 2 diabetes), insulin-dependent diabetes mellitus (type 1 diabetes), insulin resistant disorder, fatty liver or obesity.
SOLUTION: This compound is a difluorodiphenylmethane derivative in which a benzene ring bonds to another benzene ring through difluoromethylene (-CF
2 -) and the latter ring functions to directly bond to a saccharide residue. The Na
+ -glucose cotransporter inhibitor comprises the difluorodiphenylmethane derivative and its salt as effective components, and can particularly suitably be used as the treatment or preventive agent for diabetes.
COPYRIGHT: (C)2005,JPO&NCIPI

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