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3. 发明专利

CA2526145A1 C-GLYCOSIDE DERIVATIVES AND SALTS THEREOF 未知
公开(公告)号：CA2526145A1
公开(公告)日：2004-09-23
申请号：CA2526145
申请日：2004-03-12
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： IMAMURA MASAKAZU , KUROSAKI EIJI , KITTA KAYOKO , KOBAYASHI YOSHINORI , IWASAKI FUMIYOSHI , SUGANE TAKASHI , IKEGAI KAZUHIRO , TOMIYAMA HIROSHI , SHIRAKI RYOTA , MURAKAMI TAKESHI , NODA ATSUSHI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , 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
摘要： A C-glycoside derivative represented by the following general formula (I) or its salt which is a compound useful as a Na+-glucose co-transportation inhibitor in a remedy for, e.g., diabetes, in particular, insulin-independen t diabetes (type 2 diabetes) and insulin-dependent diabetes (type 1 diabetes), as well as a remedy for insulin resistance diseases and various diseases relating to diabetes including obesity. This compound is characterized in th at the ring B is bonded to the ring A via -X- and the ring A is bonded directly to a sugar residue.

4. 发明专利

ES2567571T3 Derivados de C-glucósido y sales de los mismos 未知
公开(公告)号：ES2567571T3
公开(公告)日：2016-04-25
申请号：ES04720254
申请日：2004-03-12
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： IMAMURA MASAKAZU , MURAKAMI TAKESHI , SHIRAKI RYOTA , IKEGAI KAZUHIRO , SUGANE TAKASHI , IWASAKI FUMIYOSHI , KUROSAKI EIJI , TOMIYAMA HIROSHI , NODA ATSUSHI , KITTA KAYOKO , KOBAYASHI YOSHINORI
IPC分类号： A61K31/497 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D207/06 , C07D309/10 , 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
摘要： Un derivado de C-glucósido o una sal de los mismos, en la que el derivado de C-glicósido es al menos un compuesto seleccionado del grupo constituido por: (1S)-1,5-anhidro-1-[3-(1-benzotien-2-ilmetil)-fenil-D-gluctitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-2-hidroxifenil]-D-glucitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-2-metoxifenil]-D-glucitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-2-(2-hidroxietoxi)fenil]-D-glucitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-2-(metilamino)fenil]-D-glucitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-2-[(2-hidroxietil)amino]fenil}-D-glucitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-4-metoxifenil]-D-glucitol; (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-4-clorofenil]-D-glucitol; y (1S)-1,5-anhidro-1-[5-(1-benzotien-2-ilmetil)-4-fluorofenil]-D-glucitol.

5. 发明专利

ES2363941T3 DERIVADOS DE C-GLUCOSIDO PARA EL TRATAMIENTO DE DIABETES. 未知
公开(公告)号：ES2363941T3
公开(公告)日：2011-08-19
申请号：ES08012499
申请日：2004-03-12
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： IMAMURA MASAKAZU , MURAKAMI TAKESHI , IKEGAI KAZUHIRO , IWASAKI FUMIYOSHI , SUGANE TAKASHI , KUROSAKI EIJI , TOMIYAMA HIROSHI , NODA ATSUSHI , KITTA KAYOKO , KOBAYASHI YOSHINORI , SHIRAKI RYOTA
IPC分类号： C07D405/10 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D207/06 , C07D309/10 , C07D333/12 , C07D333/16 , C07D333/54 , C07D405/04 , C07D407/04 , C07D407/10 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/10 , C07D493/04 , C07D495/04
摘要： Un derivado de C-glucósido de la siguiente fórmula (I) y sales de los mismos: en la que el anillo A representa un anillo de benceno, el anillo B representa un anillo hetero bicíclico saturado o insaturado de ocho a diez miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S, y O, y X representa metileno, con la condición de que cuando el anillo B sea un anillo hetero bicíclico saturado o insaturado de ocho a diez miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S y O incluyendo un anillo de benceno, X se una al anillo B en una parte distinta del anillo de benceno incluido en el anillo B; R 1 a R 4 individualmente representan un átomo de hidrógeno, un alquilo inferior, -C(=O)-alquilo inferior, o -alquilen inferior-arilo; y R 5 a R 11 individualmente representan, alquilo inferior, un cicloalquilo, un halógeno, un alquilo inferior sustituido con halógeno, -OH, =O, -NH2, alquil sulfonil inferior-, alquil sulfonil inferior sustituido con halógeno, aril sulfonil-, un arilo, un anillo hetero monocíclico saturado o insaturado de 5 ó 6 miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S, y O, -alquilen inferior-OH, alquilen inferior-O-alquilo inferior, -alquilen inferior-O-C(=O) alquilo inferior, -alquilen inferior-O-alquilen inferior-COOH, -alquilen inferior-O-alquilen inferior-C(=O)-O-alquilo inferior, -alquilen inferior-NH2, -alquilen inferior-NH-alquilo inferior, -alquilen inferior-N(alquilo inferior)2, -alquilen inferior-NH-C(=O)-alquilo inferior, -COOH, -CN, -C(=O)-O-alquilo inferior, -C(=O)-NH2, -C(=O)-NH-alquilo inferior, C(=O)-N(alquilo inferior)2, -O-alquilo inferior, -O-cicloalquilo, -O-alquilen inferior-OH, -O-alquilen inferior-O-alquilo inferior, -O-alquilen inferior-COOH, -O-alquilen inferior-C(=O)-O-alquilo inferior, -O-alquilen inferior-C(=O)-NH2, -O alquilen inferior-C(=O)-NH-alquilo inferior, -O-alquilen inferior-C(=O)-N(alquilo inferior)2, -O-alquilen inferior-CH(OH) CH2(OH), -O-alquilen inferior-NH2, -O-alquilen inferior-NH-alquilo inferior, -O-alquilen inferior-N(alquilo inferior)2, -Oalquilen inferior-NH-C(=O)-alquilo inferior, -NH-alquilo inferior, -N(alquilo inferior)2, -NH-SO2-alquilo inferior, alquilo inferior sustituido con -NH-SO2-halógeno, -NH-alquilen inferior-OH, -NH-C(=O)-alquilo inferior, -NH-C(=O)-NH2, -NH C(=O)-NH-alquilo inferior, -NH-C(=O)-N(alquilo inferior)2, o -NH-C(=O)-O-alquilo inferior; y R 7 a R 11 individualmente representan un átomo de hidrógeno, un alquilo inferior, un cicloalquilo, un halógeno, un alquilo inferior sustituido con halógeno, -OH, =O, -NH2, alquil sulfonil inferior-, alquil sulfonil inferior sustituido con halógeno-, aril sulfonil-, un arilo, un anillo hetero monocíclico saturado o insaturado de cinco o seis miembros que tiene de 1 a 4 heteroátomos seleccionados entre N, S y O, -alquilen inferior-OH, -alquilen inferior-O-alquilo inferior, alquilen inferior-O-C(=O)-alquilo inferior, -alquilen inferior-O-alquilen inferior-COOH, -alquilen inferior-O-alquilen inferior-C(=O)-O-alquilo inferior, -alquilen inferior-NH2, -alquilen inferior-NH-alquilo inferior, -alquilen inferior-N(alquilo inferior)2, -alquilen inferior-NH-C(=O)-alquilo inferior, -COOH, -CN, -C(=O)-O-alquilo inferior, -C(=O)-NH2, -C(=O) NH-alquilo inferior, -C(=O)-N(alquilo inferior)2, -O-alquilo inferior, -O-cicloalquilo, -O-alquilen inferior-OH, -O-alquilen inferior-O-alquilo inferior, -O-alquilen inferior-COOH, -O-alquilen inferior-C(=O)-O-alquilo inferior, -O-alquilen inferior C(=O)-NH2, -O-alquilen inferior-C(=O)-NH-alquilo inferior, -O-alquilen inferior-C(=O)-N(alquilo inferior)2, -O-alquilen inferior-CH(OH)-CH2(OH), -O-alquilen inferior-NH2, -O-alquilen inferior-NH-alquilo inferior, - O-alquilen inferior- N(alquilo inferior)2, -O-alquilen inferior-NH-C(=O)-alquilo inferior, -NH-alquilo inferior, -N(alquilo inferior)2, -NH-SO2alquilo inferior, -NH-SO2-alquilo inferior sustituido con halógeno, -NH-alquilen inferior-OH, -NH-C(=O)-alquilo inferior, -NH-C(=O)-NH2, -NH-C(=O)-NH-alquilo inferior, -NH-C(=O)-N(alquilo inferior)2 o -NH-C(=O)-O-alquilo inferior; donde el término "inferior" se refiere a una cadena de carbono lineal o ramificada que tiene de 1-6 átomos de carbono.

6. 发明专利

AU2003252370B2 Azulene derivatives and salts thereof 未知
公开(公告)号：AU2003252370B2
公开(公告)日：2008-11-06
申请号：AU2003252370
申请日：2003-08-04
申请人： KOTOBUKI PHARMACEUTICAL CO LTD , ASTELLAS PHARMA INC
发明人： KUROSAKI EIJI , IMAMURA MASAKAZU , KITTA KAYOKO , TOMIYAMA HIROSHI , IKEGAI KAZUHIRO , KOBAYASHI YOSHINORI , MURAKAMI TAKESHI , SUZUKI TAKAYUKI , NODA ATSUSHI
IPC分类号： C07D309/12 , A61P3/04 , A61P3/10 , A61P43/00 , C07D309/10
摘要： The present invention provides an azulene derivative and a salt thereof, wherein an azulene ring is bonded to a benzene ring directly or via a lower alkylene which may be substituted with a halogen atom and the benzene ring is directly bonded to the glucose residue, and it is usable as a Na -glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes-related diseases such as insulin-resistant diseases and obesity.

7. 发明专利

ES2541141T3 Composición farmacéutica para el tratamiento de las enfermedades del hígado graso 未知
公开(公告)号：ES2541141T3
公开(公告)日：2015-07-16
申请号：ES09705558
申请日：2009-01-29
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KUROSAKI EIJI , TAKASU TOSHIYUKI , MAEDA NORIAKI , YAMAZAKI SHUNJI
IPC分类号： A61K31/351 , A61K31/381 , A61P1/16 , C07D309/10 , C07D409/10 , C07H7/04 , C07H15/203 , C07H15/26
摘要： El compuesto (1S)-1,5-anhidro-1-[3-(1-benzotiofen-2-ilmetil)-4-fluorofenil]-D-glucitol o una sal farmacéuticamente aceptable del mismo para uso en un método de tratamiento de la enfermedad del hígado graso.

8. 发明专利

AU2004220222B2 C-glycoside derivatives and salts thereof 未知
公开(公告)号：AU2004220222B2
公开(公告)日：2009-10-01
申请号：AU2004220222
申请日：2004-03-12
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： KUROSAKI EIJI , KITTA KAYOKO , SHIRAKI RYOTA , IWASAKI FUMIYOSHI , IMAMURA MASAKAZU , KOBAYASHI YOSHINORI , MURAKAMI TAKESHI , SUGANE TAKASHI , NODA ATSUSHI , IKEGAI KAZUHIRO , TOMIYAMA HIROSHI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D207/06 , C07D333/12 , C07D333/16 , C07D333/54 , C07D405/04 , C07D405/10 , C07D407/04 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/10 , C07D493/04 , C07D495/04
摘要： The present invention provides C-glycoside derivatives (I) and salts thereof, wherein B ring is bonded to A ring via -X- and A ring is directly bonded to the glucose residue, and it is usable as a Na +- glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.

9. 发明专利

NO334799B1 C-glykosidderivat, farmasøytisk preparat derav og anvendelse av derivatet eller et salt der av for fremstilling av et antidiabetisk middel. 未知
公开(公告)号：NO334799B1
公开(公告)日：2014-05-26
申请号：NO20054713
申请日：2005-10-13
申请人： KOTOBUKI PHARMACEUTICAL CO LTD , ASTELLAS PHARMA INC
发明人： NODA ATSUSHI , KITTA KAYOKO , KOBAYASHI YOSHINORI , LMAMURA MASAKAZU , MURAKAMI TAKESHI , SHIRAKI RYOTA , IKEGAI KAZUHIRO , SUGANE TAKASHI , IWASAKI FUMIYOSHI , KUROSAKI EIJI , TOMIYAMA HIROSHI
IPC分类号： C07D309/10 , A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , 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
摘要： Et C-glykosidderivat representert ved følgende generelle formel (I) eller dets salt som er en forbindelse anvendelig som en Na+-glukose-ko-transportørinhibitor i et remedium mot for eksempel diabetes, spesielt insulinuavhengig diabetes (type 2 diabetes) og insulinavhengig diabetes (type I diabetes), så vel som et remedium mot insulinresistenssykdommer og forskjellige sykdommer relatert til diabetes, inkludert fedme. Denne forbindelsen er karakterisert ved at ring B er bundet til ring A via -X- og ring A er bundet direkte til en sukkerrest

10. 发明专利

NZ542399A C-glycoside derivatives and salts thereof 未知
公开(公告)号：NZ542399A
公开(公告)日：2009-01-31
申请号：NZ54239904
申请日：2004-03-12
申请人： ASTELLAS PHARMA INC , KOTOBUKI PHARMACEUTICAL CO LTD
发明人： IMAMURA MASAKAZU , MURAKAMI TAKESHI , SHIRAKI RYOTA , IKEGAI KAZUHIRO , SUGANE TAKASHI , IWASAKI FUMIYOSHI , KUROSAKI EIJI , TOMIYAMA HIROSHI , NODA ATSUSHI , KITTA KAYOKO , KOBAYASHI YOSHINORI
IPC分类号： A61K31/351 , A61K31/381 , A61K31/4035 , A61K31/404 , A61K31/41 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/4433 , A61K31/497 , A61K31/5377 , A61P3/04 , A61P3/10 , C07D207/06 , C07D309/10 , C07D333/12 , C07D333/16 , C07D333/54 , C07D405/04 , C07D405/10 , C07D407/04 , C07D409/04 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/10 , C07D493/04 , C07D495/04 , C07D403/10 , C07D407/10
摘要： Disclosed are compounds of formula (I), wherein the substituents are as defined in the specification. The compounds are Na+-glucose cotransporter inhibitors useful in the treatment of diabetes and obesity.

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