公开(公告)号：EP2818473A4

公开(公告)日：2015-04-15

申请号：EP13751296

申请日：2013-02-19

申请人： TAKEDA PHARMACEUTICAL

发明人： NAGAMIYA HIROYUKI ,  YOSHIDA MASATO ,  SETO MASAKI ,  MARUI SHOGO ,  ODA TSUNEO ,  ISHICHI YUJI ,  SUZUKI HIDEO ,  KUSUMOTO TOMOKAZU ,  YOGO TAKATOSHI ,  RHIM CHUL YUN ,  YOON CHEOLHWAN ,  LEE GIL NAM ,  KANG HYUN BIN ,  KIM KWANG OK ,  JEON HYE SUN

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61P1/04 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P29/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00

CPC分类号： C07D471/04 ,  C07D519/00

公开(公告)号：EP1302470A4

公开(公告)日：2005-04-06

申请号：EP01947999

申请日：2001-07-13

申请人： TAKEDA PHARMACEUTICAL

发明人： TERASHITA ZEN-ICHI ,  NAKAMURA MASAHIRA ,  MARUI SHOGO ,  OGINO MASAKI

IPC分类号： A61K31/00 ,  A61K31/343 ,  A61K31/352 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4433 ,  A61K31/453 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61P9/08 ,  A61P9/10 ,  A61P43/00 ,  C07D307/82 ,  C07D307/93 ,  C07D311/16 ,  C07D311/18 ,  C07D311/94 ,  C07D405/06 ,  C07D405/12 ,  C07D493/04

CPC分类号： C07D307/82 ,  A61K31/00 ,  A61K31/343 ,  A61K31/352 ,  A61K31/423 ,  A61K31/437 ,  A61K31/4433 ,  A61K31/453 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  C07D307/93 ,  C07D311/16 ,  C07D311/18 ,  C07D311/94 ,  C07D405/06 ,  C07D405/12 ,  C07D493/04

摘要： The present invention provides a lipid-rich plaque regressing agent comprising a compound represented by Formula: in which ring A is a cyclic hydrocarbon or the like; ring B is a heterocyclic ring or the like; each of X and Y is -NR - (in which R is a hydrocarbon or the like); D is a C1-3 alkylene group or the like; E is -NH- or the like; G is a bond or the like; and Ar is an aryl or the like; D may be taken together with a constituent atom of the ring B to form a ring, and R may be taken together with a constituent atom of the ring B to form a ring.

公开(公告)号：EP1650201A4

公开(公告)日：2009-02-18

申请号：EP04748264

申请日：2004-07-30

申请人： TAKEDA PHARMACEUTICAL

发明人： MARUI SHOGO ,  MIKI TAKASHI ,  MIURA SHOUTAROU ,  NISHIMOTO TOMOYUKI ,  NAKADA YOSHIHISA

IPC分类号： C07D267/14 ,  A61P1/18 ,  A61P3/00 ,  A61P3/06 ,  A61P3/10 ,  A61P5/14 ,  A61P7/00 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P19/00 ,  A61P19/10 ,  A61P21/00 ,  A61P25/28 ,  A61P43/00 ,  C07D417/06

CPC分类号： C07D413/06 ,  C07D267/14 ,  C07D417/06

摘要： A compound represented by the formula [I]: [I] (wherein ring A and ring B each represents an optionally substituted benzene ring; ring C represents an optionally further substituted aromatic ring; R1 represents a lower alkyl optionally substituted by optionally substituted hydroxy; X1a represents a bond or optionally substituted lower alkylene; X1b represents a bond or optionally substituted lower alkylene; X2 represents a bond, -O-, or -S-; X3 represents a bond or an optionally substituted divalent hydrocarbon group; and Y represents optionally esterified or amidated carboxy) or a salt of the compound. The compound of the formula [I] is safer and has more potent lipid-lowering activity such as squalene synthase inhibitory activity (cholesterol-lowering activity) and triglyceride-lowering activity. The compound is useful as a medicine for, e.g., the prevention of and treatments for hyperlipemia.

摘要翻译： 由式[I]表示的化合物：[I]（其中环A和环B各自表示任选取代的苯环;环C表示任选进一步取代的芳环; R 1表示任选被任选取代的羟基取代的低级烷基; X 1表示键或任选取代的低级亚烷基; X 1表示键或任选取代的低级亚烷基; X 2表示键，-O-或-S-; X 3表示键或任选取代的二价烃基;且Y表示任选 酯化或酰胺化的羧基）或该化合物的盐。 式[I]的化合物更安全，具有更强的降脂活性，如角鲨烯合成酶抑制活性（降胆固醇活性）和甘油三酯降低活性。 该化合物可用作例如预防和治疗高脂血症的药物。

公开(公告)号：EP1471064A4

公开(公告)日：2005-04-27

申请号：EP03701037

申请日：2003-01-09

申请人： TAKEDA PHARMACEUTICAL

发明人： TERASHITA ZEN-ICHI ,  NAKAMURA MASAHIRA ,  MARUI SHOGO ,  OGINO MASAKI

IPC分类号： A61K31/37 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10 ,  A61P25/28 ,  A61P43/00 ,  C07D209/94 ,  C07D261/14 ,  C07D271/10 ,  C07D277/42 ,  C07D311/12 ,  C07D333/36 ,  C07D405/10 ,  C07D311/18 ,  A61K31/352 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4709 ,  A61K31/4725 ,  C07D405/12 ,  C07D413/10 ,  C07D417/10

CPC分类号： C07D311/12 ,  C07D209/94 ,  C07D261/14 ,  C07D271/10 ,  C07D277/42 ,  C07D333/36 ,  C07D405/10

摘要： Compounds represented by the general formula [I] or salts thereof, which are useful as lipid-rich plaque inhibitors and/or ACAT inhibitors: [I] wherein R1 and R2 are each hydrogen, halogeno, an optionally substituted linear hydrocarbon group, or hydroxyl which may be substituted with an optionally substituted linear hydrocarbon group, or R1 and R2 together with the carbon atoms adjacent thereto may form an optionally substituted carbocyle or a dihydrofuran ring which may have an oxo group; A is a benzene ring which may be further substituted; B is an aromatic ring which may be substituted; X is a free valency or a spacer whose main chain has 1 to 6 atoms; Y is carboxyl which may be esterified, carbamoyl which may be substituted, cyano, or an optionally substituted heterocyclic group bearing a hydrogen atom capable of causing deprotonation.