公开(公告)号：EP2236137A4

公开(公告)日：2014-01-01

申请号：EP09705558

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

CPC分类号： C07D309/10 ,  C07D409/10 ,  C07H7/04 ,  C07H15/203 ,  C07H15/26

公开(公告)号：EP1553094A4

公开(公告)日：2006-10-11

申请号：EP03766722

申请日：2003-08-04

申请人： ASTELLAS PHARMA INC ,  KOTOBUKI PHARMACEUTICAL CO LTD

发明人： TOMIYAMA HIROSHI ,  NODA ATSUSHI ,  KITTA KAYOKO ,  KOBAYASHI YOSHINORI ,  IMAMURA MASAKAZU ,  MURAKAMI TAKESHI ,  IKEGAI KAZUHIRO ,  SUZUKI TAKAYUKI ,  KUROSAKI EIJI

IPC分类号： C07D309/12 ,  A61K31/351 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07D309/10

CPC分类号： C07D309/12 ,  C07D309/10

摘要： Azulene derivatives represented by the following general formula (I) and salts thereof are useful as Na+-glucose cotransporter inhibitors in, for example, remedies for diabetes, etc., in particular, insulin-independent diabetes (type 2 diabetes), insulin-dependent diabetes (type 1 diabetes), etc., and remedies for various diabetes-related diseases such as insulin resistant disease and obesity. These compounds are characterized in that an azulene ring is bonded, either directly or via an optionally halogenated lower alkylene, to a benzene ring and the benzene ring is directly bonded to a sugar residue.

公开(公告)号：EP1609785A4

公开(公告)日：2008-10-22

申请号：EP04720254

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 ,  A61K31/49 ,  C07D407/10

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： 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-independent 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 that the ring B is bonded to the ring A via -X- and the ring A is bonded directly to a sugar residue.

公开(公告)号：EP1469071A4

公开(公告)日：2006-02-15

申请号：EP03703025

申请日：2003-01-22

申请人： ASTELLAS PHARMA INC

发明人： ENDOH HIDEKI ,  NAKANO RYOSUKE ,  KUROSAKI EIJI ,  KATO MIYUKI ,  YOKOTA HIROYUKI ,  INABE KAZUNORI

IPC分类号： A61P3/10 ,  C12N1/19 ,  C12N1/21 ,  C12N15/10 ,  C12N15/12 ,  C12Q1/68 ,  G01N33/566 ,  C07K14/705 ,  C07K16/18 ,  C12N15/62 ,  C12N15/81 ,  C12Q1/66

CPC分类号： G01N33/566 ,  C12N15/1055 ,  C12Q1/6897 ,  G01N2333/70567

摘要： It is intended to disclose a method of screening a protein which ligand-dependently interacts with PPAR and is highly useful as a tool for screening a drug improving insulin resistance. Using this method, a main effect ligand-dependent PPAR-binding molecule ECHLP, a main effect ligand-selective PPARgamma acting factor FLJ13111 and a side effect ligand-dependent PPAR-binding molecule AOP2 are obtained. It is also intended to disclose a screening system for a drug improving insulin resistance selectively exerting the main effect without causing any side effect which is constructed by using PPAR-interacting ECHLP, PPAR-interacting FLJ13111 and PPAR-interacting AOP2. It is furthermore intended to disclose a process for producing medicinal compositions for improving insulin resistance containing, as the active ingredient, a PPAR main effect promoter, a PPAR main effect-specific agonist, a PPAR-interacting ECHLP inhibitor promoting the main effect of PPAR, a substance regulating the side effect of PPARgamma, a PPAR-interacting AOP2 inhibitor regulating the side effect of PPARgamma, a PPAR-interacting FLJ1311 activator promoting the main effect of PPAR or an FLJ13111 expression accelerator which can be obtained by the above screening method.