Title:
キナーゼ調節因子および使用方法
Document Type and Number:
Japanese Patent JP2007534687
Kind Code:
A
Abstract:
The present invention relates to compounds of the Formula (I) and (II) wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
Inventors:
Anand, Neil K.
Blazei, Charles M.
Bowles, Owen Joseph
Basenius, yerck
Cannes, Banen Lin
Chan, Diva She-Min
Chen, Baili
Kor, Eric One
Costanzo, Simona
Defina, Stephen Charles
Dubenco, Larisa
Franzini, Maurizio
Fan pin
Jamarama Madaka, Vas
Corey, Richard George
Kim, moon fan
Klein, Let Ronald
Leh, donna tiger
Mac, Morrison Bee.
Eggplant, John M.
Parkes, Jason Jeverus
Rice, Kenneth Dee.
Tsang, Tse H.
Tsujako, Amy Lou
One, Yong
Shoe, way
Blazei, Charles M.
Bowles, Owen Joseph
Basenius, yerck
Cannes, Banen Lin
Chan, Diva She-Min
Chen, Baili
Kor, Eric One
Costanzo, Simona
Defina, Stephen Charles
Dubenco, Larisa
Franzini, Maurizio
Fan pin
Jamarama Madaka, Vas
Corey, Richard George
Kim, moon fan
Klein, Let Ronald
Leh, donna tiger
Mac, Morrison Bee.
Eggplant, John M.
Parkes, Jason Jeverus
Rice, Kenneth Dee.
Tsang, Tse H.
Tsujako, Amy Lou
One, Yong
Shoe, way
Application Number:
JP2007509678A
Publication Date:
November 29, 2007
Filing Date:
April 22, 2005
Export Citation:
Assignee:
Exelixis, Inc.
International Classes:
C07D473/34; A61K31/519; A61K31/52; A61K31/7076; A61P9/10; A61P9/12; A61P17/06; A61P19/02; A61P25/00; A61P27/02; A61P29/00; A61P35/00; A61P37/06; A61P43/00; C07D487/04
Domestic Patent References:
| JP2008525526A | 2008-07-17 | |||
| JP2002518394A | 2002-06-25 | |||
| JP2007503392A | 2007-02-22 | |||
| JP2007531721A | 2007-11-08 | |||
| JP2002518394A | 2002-06-25 | |||
| JP2007503392A | 2007-02-22 | |||
| JP2007531721A | 2007-11-08 | |||
| JP2008525526A | 2008-07-17 |
Foreign References:
| US20050197340A1 | 2005-09-08 | |||
| WO2005020897A2 | 2005-03-10 | |||
| US3457263A | 1969-07-22 | |||
| WO1991004254A1 | 1991-04-04 | |||
| WO2003031405A2 | 2003-04-17 | |||
| WO2004074287A1 | 2004-09-02 | |||
| WO2005020897A2 | 2005-03-10 | |||
| US3457263A | 1969-07-22 | |||
| WO1991004254A1 | 1991-04-04 | |||
| WO2003031405A2 | 2003-04-17 | |||
| WO2004074287A1 | 2004-09-02 | |||
| US20050197340A1 | 2005-09-08 |
Other References:
JPN6011013350; ＳＴＲＡＰＰＡＧＨＥＴＴＩ， Ｇ．， ｅｔ ａｌ．: '"Ａｄｅｎｏｓｉｎｅ ｒｅｃｅｐｔｏｒｓ： ｓｙｎｔｈｅｓｉｓ， ｓｔｒｕｃｔｕｒｅ-ａｃｔｉｖｉｔｙ ｒｅｌａｔｉｏｎｓｈｉｐｓ ａｎｄ ｂｉｏｌｏｇｉｃａｌ ａｃｔｉｖｉｔｙ ｏｆ ｎｅｗ ６-ａ' ＥＵＲＯＰＥＡＮ ＪＯＵＲＮＡＬ ＯＦ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．３３， ｎｏ．６, 1998, ｐｐ．５０１-５０８
JPN6011013351; ＲＥＧＮＩＥＲ， Ｇ．， ｅｔ ａｌ．: '"Ｄｅｐｒｅｓｓｅｕｒｓ ｄｕ ｓｙｓｔｅｍｅ ｎｅｒｖｅｕｘ ｃｅｎｔｒａｌ； Ｅｔｕｄｅ ｄｅ ｎｏｕｖｅａｕｘ ｄｅｒｉｖｅｓ ｄｅ ｌａ ｐｕｒｉｎｅ"' ＣＨＩＭＩＣＡ ＴＨＥＲＡＰＥＵＴＩＣＡ ｖｏｌ．７， ｎｏ．３, 1972, ｐｐ．１９２-２０５
JPN6011013347; ＨＡＳＡＮ， Ａ． ｅｔ ａｌ．: '"Ｓｔｕｄｉｅｓ ｉｎ Ｎｕｃｌｅｏｓｉｄｅｓ： Ｐａｒｔ ＸＶ． Ｓｙｎｔｈｅｓｉｓ ｏｆ ６-ｍｅｔｈｏｘｙ／ｍｅｔｈｙｌｔｈｉｏ-４-Ｎ-ｓｕｂｓｔｉｔｕｔｅｄ-１-（２-ｔ ｅｔｒａｈｙｄｒｏ' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＣＨＥＭＩＳＴＲＹ， ＳＥＣＴＩＯＮ Ｂ： ＯＲＧＡＮＩＣ ＣＨＥＭＩＳＴＲＹ ＩＮＣＬＵＤＩＮＧ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．２６Ｂ， ｎｏ．３, 1987, ｐｐ．２８４-２８６
JPN6011013348; ＰＲＡＢＨＡＫＡＲ， Ｙ． Ｓ．， ｅｔ ａｌ．: '"ＱＳＡＲ ｓｔｕｄｙ ｏｎ ｔｈｅ ａｎｔｉｖｉｒａｌ ａｃｔｉｖｉｔｙ ｏｆ ２，６，９-ｓｕｂｓｔｉｔｕｔｅｄ ｐｕｒｉｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ａｎａｌｏｇｕｅｓ"' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＢＩＯＣＨＥＭＩＳＴＲＹ ＆ ＢＩＯＰＨＹＳＩＣＳ ｖｏｌ．２７， ｎｏ．５, 1990, ｐｐ．３４２-３４７
JPN6011013349; ＬＥＴＴＲＥ， Ｈ．， ｅｔ ａｌ．: '"Ｎ-Ｐｕｒｙｌ-（６）-Ｄｅｒｉｖａｔｅ ｖｏｎ Ｄｉａｍｉｎｅｎ"' ＪＵＳＴＵＳ ＬＩＥＢＩＧＳ ＡＮＮＡＬＥＮ ＤＥＲ ＣＨＥＭＩＥ ｖｏｌ．６４９, 1961, ｐｐ．１２４-１３０
JPN6011013347; ＨＡＳＡＮ， Ａ． ｅｔ ａｌ．: '"Ｓｔｕｄｉｅｓ ｉｎ Ｎｕｃｌｅｏｓｉｄｅｓ： Ｐａｒｔ ＸＶ． Ｓｙｎｔｈｅｓｉｓ ｏｆ ６-ｍｅｔｈｏｘｙ／ｍｅｔｈｙｌｔｈｉｏ-４-Ｎ-ｓｕｂｓｔｉｔｕｔｅｄ-１-（２-ｔ ｅｔｒａｈｙｄｒｏ' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＣＨＥＭＩＳＴＲＹ， ＳＥＣＴＩＯＮ Ｂ： ＯＲＧＡＮＩＣ ＣＨＥＭＩＳＴＲＹ ＩＮＣＬＵＤＩＮＧ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．２６Ｂ， ｎｏ．３, 1987, ｐｐ．２８４-２８６
JPN6011013348; ＰＲＡＢＨＡＫＡＲ， Ｙ． Ｓ．， ｅｔ ａｌ．: '"ＱＳＡＲ ｓｔｕｄｙ ｏｎ ｔｈｅ ａｎｔｉｖｉｒａｌ ａｃｔｉｖｉｔｙ ｏｆ ２，６，９-ｓｕｂｓｔｉｔｕｔｅｄ ｐｕｒｉｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ａｎａｌｏｇｕｅｓ"' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＢＩＯＣＨＥＭＩＳＴＲＹ ＆ ＢＩＯＰＨＹＳＩＣＳ ｖｏｌ．２７， ｎｏ．５, 1990, ｐｐ．３４２-３４７
JPN6011013349; ＬＥＴＴＲＥ， Ｈ．， ｅｔ ａｌ．: '"Ｎ-Ｐｕｒｙｌ-（６）-Ｄｅｒｉｖａｔｅ ｖｏｎ Ｄｉａｍｉｎｅｎ"' ＪＵＳＴＵＳ ＬＩＥＢＩＧＳ ＡＮＮＡＬＥＮ ＤＥＲ ＣＨＥＭＩＥ ｖｏｌ．６４９, 1961, ｐｐ．１２４-１３０
JPN6011013350; ＳＴＲＡＰＰＡＧＨＥＴＴＩ， Ｇ．， ｅｔ ａｌ．: '"Ａｄｅｎｏｓｉｎｅ ｒｅｃｅｐｔｏｒｓ： ｓｙｎｔｈｅｓｉｓ， ｓｔｒｕｃｔｕｒｅ-ａｃｔｉｖｉｔｙ ｒｅｌａｔｉｏｎｓｈｉｐｓ ａｎｄ ｂｉｏｌｏｇｉｃａｌ ａｃｔｉｖｉｔｙ ｏｆ ｎｅｗ ６-ａ' ＥＵＲＯＰＥＡＮ ＪＯＵＲＮＡＬ ＯＦ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．３３， ｎｏ．６, 1998, ｐｐ．５０１-５０８
JPN6011013351; ＲＥＧＮＩＥＲ， Ｇ．， ｅｔ ａｌ．: '"Ｄｅｐｒｅｓｓｅｕｒｓ ｄｕ ｓｙｓｔｅｍｅ ｎｅｒｖｅｕｘ ｃｅｎｔｒａｌ； Ｅｔｕｄｅ ｄｅ ｎｏｕｖｅａｕｘ ｄｅｒｉｖｅｓ ｄｅ ｌａ ｐｕｒｉｎｅ"' ＣＨＩＭＩＣＡ ＴＨＥＲＡＰＥＵＴＩＣＡ ｖｏｌ．７， ｎｏ．３, 1972, ｐｐ．１９２-２０５
JPN6011013351; ＲＥＧＮＩＥＲ， Ｇ．， ｅｔ ａｌ．: '"Ｄｅｐｒｅｓｓｅｕｒｓ ｄｕ ｓｙｓｔｅｍｅ ｎｅｒｖｅｕｘ ｃｅｎｔｒａｌ； Ｅｔｕｄｅ ｄｅ ｎｏｕｖｅａｕｘ ｄｅｒｉｖｅｓ ｄｅ ｌａ ｐｕｒｉｎｅ"' ＣＨＩＭＩＣＡ ＴＨＥＲＡＰＥＵＴＩＣＡ ｖｏｌ．７， ｎｏ．３, 1972, ｐｐ．１９２-２０５
JPN6011013347; ＨＡＳＡＮ， Ａ． ｅｔ ａｌ．: '"Ｓｔｕｄｉｅｓ ｉｎ Ｎｕｃｌｅｏｓｉｄｅｓ： Ｐａｒｔ ＸＶ． Ｓｙｎｔｈｅｓｉｓ ｏｆ ６-ｍｅｔｈｏｘｙ／ｍｅｔｈｙｌｔｈｉｏ-４-Ｎ-ｓｕｂｓｔｉｔｕｔｅｄ-１-（２-ｔ ｅｔｒａｈｙｄｒｏ' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＣＨＥＭＩＳＴＲＹ， ＳＥＣＴＩＯＮ Ｂ： ＯＲＧＡＮＩＣ ＣＨＥＭＩＳＴＲＹ ＩＮＣＬＵＤＩＮＧ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．２６Ｂ， ｎｏ．３, 1987, ｐｐ．２８４-２８６
JPN6011013348; ＰＲＡＢＨＡＫＡＲ， Ｙ． Ｓ．， ｅｔ ａｌ．: '"ＱＳＡＲ ｓｔｕｄｙ ｏｎ ｔｈｅ ａｎｔｉｖｉｒａｌ ａｃｔｉｖｉｔｙ ｏｆ ２，６，９-ｓｕｂｓｔｉｔｕｔｅｄ ｐｕｒｉｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ａｎａｌｏｇｕｅｓ"' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＢＩＯＣＨＥＭＩＳＴＲＹ ＆ ＢＩＯＰＨＹＳＩＣＳ ｖｏｌ．２７， ｎｏ．５, 1990, ｐｐ．３４２-３４７
JPN6011013349; ＬＥＴＴＲＥ， Ｈ．， ｅｔ ａｌ．: '"Ｎ-Ｐｕｒｙｌ-（６）-Ｄｅｒｉｖａｔｅ ｖｏｎ Ｄｉａｍｉｎｅｎ"' ＪＵＳＴＵＳ ＬＩＥＢＩＧＳ ＡＮＮＡＬＥＮ ＤＥＲ ＣＨＥＭＩＥ ｖｏｌ．６４９, 1961, ｐｐ．１２４-１３０
JPN6011013347; ＨＡＳＡＮ， Ａ． ｅｔ ａｌ．: '"Ｓｔｕｄｉｅｓ ｉｎ Ｎｕｃｌｅｏｓｉｄｅｓ： Ｐａｒｔ ＸＶ． Ｓｙｎｔｈｅｓｉｓ ｏｆ ６-ｍｅｔｈｏｘｙ／ｍｅｔｈｙｌｔｈｉｏ-４-Ｎ-ｓｕｂｓｔｉｔｕｔｅｄ-１-（２-ｔ ｅｔｒａｈｙｄｒｏ' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＣＨＥＭＩＳＴＲＹ， ＳＥＣＴＩＯＮ Ｂ： ＯＲＧＡＮＩＣ ＣＨＥＭＩＳＴＲＹ ＩＮＣＬＵＤＩＮＧ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．２６Ｂ， ｎｏ．３, 1987, ｐｐ．２８４-２８６
JPN6011013348; ＰＲＡＢＨＡＫＡＲ， Ｙ． Ｓ．， ｅｔ ａｌ．: '"ＱＳＡＲ ｓｔｕｄｙ ｏｎ ｔｈｅ ａｎｔｉｖｉｒａｌ ａｃｔｉｖｉｔｙ ｏｆ ２，６，９-ｓｕｂｓｔｉｔｕｔｅｄ ｐｕｒｉｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ａｎａｌｏｇｕｅｓ"' ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＢＩＯＣＨＥＭＩＳＴＲＹ ＆ ＢＩＯＰＨＹＳＩＣＳ ｖｏｌ．２７， ｎｏ．５, 1990, ｐｐ．３４２-３４７
JPN6011013349; ＬＥＴＴＲＥ， Ｈ．， ｅｔ ａｌ．: '"Ｎ-Ｐｕｒｙｌ-（６）-Ｄｅｒｉｖａｔｅ ｖｏｎ Ｄｉａｍｉｎｅｎ"' ＪＵＳＴＵＳ ＬＩＥＢＩＧＳ ＡＮＮＡＬＥＮ ＤＥＲ ＣＨＥＭＩＥ ｖｏｌ．６４９, 1961, ｐｐ．１２４-１３０
JPN6011013350; ＳＴＲＡＰＰＡＧＨＥＴＴＩ， Ｇ．， ｅｔ ａｌ．: '"Ａｄｅｎｏｓｉｎｅ ｒｅｃｅｐｔｏｒｓ： ｓｙｎｔｈｅｓｉｓ， ｓｔｒｕｃｔｕｒｅ-ａｃｔｉｖｉｔｙ ｒｅｌａｔｉｏｎｓｈｉｐｓ ａｎｄ ｂｉｏｌｏｇｉｃａｌ ａｃｔｉｖｉｔｙ ｏｆ ｎｅｗ ６-ａ' ＥＵＲＯＰＥＡＮ ＪＯＵＲＮＡＬ ＯＦ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ｖｏｌ．３３， ｎｏ．６, 1998, ｐｐ．５０１-５０８
JPN6011013351; ＲＥＧＮＩＥＲ， Ｇ．， ｅｔ ａｌ．: '"Ｄｅｐｒｅｓｓｅｕｒｓ ｄｕ ｓｙｓｔｅｍｅ ｎｅｒｖｅｕｘ ｃｅｎｔｒａｌ； Ｅｔｕｄｅ ｄｅ ｎｏｕｖｅａｕｘ ｄｅｒｉｖｅｓ ｄｅ ｌａ ｐｕｒｉｎｅ"' ＣＨＩＭＩＣＡ ＴＨＥＲＡＰＥＵＴＩＣＡ ｖｏｌ．７， ｎｏ．３, 1972, ｐｐ．１９２-２０５
Attorney, Agent or Firm:
Hidesaku Yamamoto
Takaaki Yasumura
Natsuki Morishita
Takaaki Yasumura
Natsuki Morishita