Title:
CB1-アンタゴニスト作用、アゴニスト作用または部分アゴニスト作用を有するチアゾール誘導体
Document Type and Number:
Japanese Patent JP2005529855
Kind Code:
A
Abstract:
The present invention relates to a group of thiazole derivatives which are potent antagonists, agonists or partial agonists of the cannabinoid CB1-receptor. The compounds have the general formula (I) wherein R and R1-R4 have the meanings given in the specification
Inventors:
Lange, Josephus H.M.
Kruze, Cornelis G
Heremance, Arnoldus HJ
Ban Stuibenberg, Hermann H
De Eaksman, Jessica A.R.
McCreeley, Andrew Sea
Kruze, Cornelis G
Heremance, Arnoldus HJ
Ban Stuibenberg, Hermann H
De Eaksman, Jessica A.R.
McCreeley, Andrew Sea
Application Number:
JP2003576419A
Publication Date:
October 06, 2005
Filing Date:
March 17, 2003
Export Citation:
Assignee:
Solvay Pharmaceuticals B.V.
International Classes:
A61K31/425; A61K31/426; A61K31/427; A61K31/454; A61K31/5377; A61K31/55; A61P1/00; A61P1/04; A61P1/08; A61P1/12; A61P1/14; A61P3/04; A61P3/10; A61P7/00; A61P9/00; A61P9/10; A61P11/00; A61P11/06; A61P25/00; A61P25/02; A61P25/04; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P25/36; A61P27/06; A61P31/04; A61P31/12; A61P35/00; A61P41/00; A61P43/00; C07D277/56; C07D277/68; C07D417/12; C07D277/20; (IPC1-7): C07D277/20; A61K31/426; A61K31/427; A61K31/454; A61K31/5377; A61K31/55; A61P1/00; A61P1/04; A61P1/08; A61P1/12; A61P1/14; A61P3/04; A61P3/10; A61P7/00; A61P9/00; A61P9/10; A61P11/00; A61P11/06; A61P25/00; A61P25/02; A61P25/04; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P25/36; A61P27/06; A61P31/04; A61P31/12; A61P35/00; A61P41/00; A61P43/00; C07D277/56; C07D417/12
Domestic Patent References:
| JPH05345772A | 1993-12-27 | |||
| JPH0327370A | 1991-02-05 | |||
| JPH10504542A | 1998-05-06 | |||
| JP2001114690A | 2001-04-24 | |||
| JPH11193281A | 1999-07-21 |
Other References:
JPN6009032192, Ａｋｉｔｏ Ｔａｎａｋａ, "Ａｎｔｉｐｌａｔｅｌｅｔ Ａｇｅｎｔｓ Ｂａｓｅｄ ｏｎ Ｃｙｃｌｏｏｘｙｇｅｎａｓｅ Ｉｎｈｉｂｉｔｉｏｎ ｗｉｔｈｏｕｔ Ｕｌｃｅｒｏｇｅｎｅｓｉｓ． Ｅｖａｌｕａｔｉｏｎ ａｎｄ Ｓｙｎｔｈｅｓ", Ｊ． Ｍｅｄ． Ｃｈｅｍ．, 1994, Ｖｏｌ．３７, １１８９−１１９９
JPN6009032194, Ｔａｋｅｈｉｒｏ Ｏｃｈｉ, "Ｄｉｆｆｅｒｅｎｔｉａｌ ｅｆｆｅｃｔ ｏｆ ＦＲ１２２０４７， ａ ｓｅｌｅｃｔｉｖｅ ｃｙｃｌｏ−ｏｘｙｇｅｎａｓｅ−１ ｉｎｈｉｂｉｔｏｒ， ｉｎ ｒａｔ ｃｈｒｏｎｉｃ ｍｏｄｅｌｓ ｏｆ ａ", Ｂｒｉｔｉｓｈ Ｊｏｕｒｎａｌ ｏｆ Ｐｈａｒｍａｃｏｌｏｇｙ, 200202, Ｖｏｌ．１３５, ７８２−７８８
JPN6009032196, Ｔａｋｅｈｉｒｏ Ｏｃｈｉ, "Ｔｈｅ ａｎａｌｇｅｓｉｃ ｅｆｆｅｃｔ ｐｒｏｆｉｌｅ ｏｆ ＦＲ１２２０４７， ａ ｓｅｌｅｃｔｉｖｅ ｃｙｃｌｏｏｘｙｇｅｎａｓｅ−１ ｉｎｈｉｂｉｔｏｒ， ｉｎ ｃｈｅｍｉｃａｌ ｎｏｃｉｃｅ", Ｅｕｒｏｐｅａｎ Ｊｏｕｒｎａｌ ｏｆ Ｐｈａｒｍａｃｏｌｏｇｙ, 2000, Ｖｏｌ．３９１, ４９−５４
JPN6009032197, Ｍｉｗａｋｏ Ｄｏｈｉ, "Ｔｈｅ ａｎｔｉ−ｐｌａｔｅｌｅｔ ａｃｔｉｏｎｓ ｏｆ ＦＲ１２２０４７， ａ ｎｏｖｅｌ ｃｙｃｌｏｏｘｙｇｅｎａｓｅ ｉｎｈｉｂｉｔｏｒ", Ｅｕｒｏｐｅａｎ Ｊｏｕｒｎａｌ ｏｆ Ｐｈａｒｍａｃｏｌｏｇｙ, 1993, Ｖｏｌ．２４３, １７９−１８４
JPN6009032198, Ｔｅｄ Ｔ． Ｓａｋａｉ, "Ｓｙｎｔｈｅｓｉｓ ａｎｄ Ｐｒｏｐｅｒｔｉｅｓ ｏｆ Ｓｏｍｅ Ｎｏｖｅｌ Ａｎｔｉ−ｃａｌｍｏｄｕｌｉｎ Ｄｒｕｇｓ", Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ, 1999, Ｖｏｌ．７, １５５９−１５６５
JPN6009032194, Ｔａｋｅｈｉｒｏ Ｏｃｈｉ, "Ｄｉｆｆｅｒｅｎｔｉａｌ ｅｆｆｅｃｔ ｏｆ ＦＲ１２２０４７， ａ ｓｅｌｅｃｔｉｖｅ ｃｙｃｌｏ−ｏｘｙｇｅｎａｓｅ−１ ｉｎｈｉｂｉｔｏｒ， ｉｎ ｒａｔ ｃｈｒｏｎｉｃ ｍｏｄｅｌｓ ｏｆ ａ", Ｂｒｉｔｉｓｈ Ｊｏｕｒｎａｌ ｏｆ Ｐｈａｒｍａｃｏｌｏｇｙ, 200202, Ｖｏｌ．１３５, ７８２−７８８
JPN6009032196, Ｔａｋｅｈｉｒｏ Ｏｃｈｉ, "Ｔｈｅ ａｎａｌｇｅｓｉｃ ｅｆｆｅｃｔ ｐｒｏｆｉｌｅ ｏｆ ＦＲ１２２０４７， ａ ｓｅｌｅｃｔｉｖｅ ｃｙｃｌｏｏｘｙｇｅｎａｓｅ−１ ｉｎｈｉｂｉｔｏｒ， ｉｎ ｃｈｅｍｉｃａｌ ｎｏｃｉｃｅ", Ｅｕｒｏｐｅａｎ Ｊｏｕｒｎａｌ ｏｆ Ｐｈａｒｍａｃｏｌｏｇｙ, 2000, Ｖｏｌ．３９１, ４９−５４
JPN6009032197, Ｍｉｗａｋｏ Ｄｏｈｉ, "Ｔｈｅ ａｎｔｉ−ｐｌａｔｅｌｅｔ ａｃｔｉｏｎｓ ｏｆ ＦＲ１２２０４７， ａ ｎｏｖｅｌ ｃｙｃｌｏｏｘｙｇｅｎａｓｅ ｉｎｈｉｂｉｔｏｒ", Ｅｕｒｏｐｅａｎ Ｊｏｕｒｎａｌ ｏｆ Ｐｈａｒｍａｃｏｌｏｇｙ, 1993, Ｖｏｌ．２４３, １７９−１８４
JPN6009032198, Ｔｅｄ Ｔ． Ｓａｋａｉ, "Ｓｙｎｔｈｅｓｉｓ ａｎｄ Ｐｒｏｐｅｒｔｉｅｓ ｏｆ Ｓｏｍｅ Ｎｏｖｅｌ Ａｎｔｉ−ｃａｌｍｏｄｕｌｉｎ Ｄｒｕｇｓ", Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ, 1999, Ｖｏｌ．７, １５５９−１５６５
Attorney, Agent or Firm:
Heikichi Odashima