Title:
DIAZACARBAZOLES AND METHODS OF USE
Document Type and Number:
Japanese Patent JP2014196309
Kind Code:
A
Abstract:
PROBLEM TO BE SOLVED: To provide compounds which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1), thus useful as cancer therapeutics.SOLUTION: The invention relates to 1,5-diazacarbazole compounds of the following formula.
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Inventors:
HAZEL JOAN DYKE
EMANUELA GANCIA
GAZZARD LEWIS J
SIMON CHARLS GOODACRE
LYSSIKATOS JOSEPH P
CALUM MACLEOD
KAREN WILLIAMS
CHEN HUIFEN
EMANUELA GANCIA
GAZZARD LEWIS J
SIMON CHARLS GOODACRE
LYSSIKATOS JOSEPH P
CALUM MACLEOD
KAREN WILLIAMS
CHEN HUIFEN
Application Number:
JP2014103195A
Publication Date:
October 16, 2014
Filing Date:
May 19, 2014
Export Citation:
Assignee:
GENENTECH INC
International Classes:
C07D471/14; A61K31/496; A61K31/519; A61K45/00; A61P35/00; A61P35/02
Domestic Patent References:
| JP2003527394A | 2003-09-16 | |||
| JP2006517949A | 2006-08-03 | |||
| JP2008502693A | 2008-01-31 | |||
| JP5677945B2 | 2015-02-25 |
Foreign References:
| WO2007044779A1 | 2007-04-19 | |||
| WO2001083456A1 | 2001-11-08 |
Other References:
JPN6013057182; ＷＡＲＮＥＲ， Ｓ．Ｌ． ｅｔ ａｌ．: 'Ｉｄｅｎｔｉｆｉｃａｔｉｏｎ ｏｆ ａ ｌｅａｄ ｓｍａｌｌ-ｍｏｌｅｃｕｌｅ ｉｎｈｉｂｉｔｏｒ ｏｆ ｔｈｅ Ａｕｒｏｒａ ｋｉｎａｓｅｓ ｕｓｉｎｇ ａ ｓｔｒｕｃｔｕｒｅ-ａｓｓｉｓｔｅｄ，' Ｍｏｌｅｃｕｌａｒ Ｃａｎｃｅｒ Ｔｈｅｒａｐｅｕｔｉｃｓ ５（７）, 2006, ｐ．１７６４-１７７３
JPN6013057184; ＦＯＬＯＰＰＥ， Ｎ． ｅｔ ａｌ．: 'Ｉｄｅｎｔｉｆｉｃａｔｉｏｎ ｏｆ ｃｈｅｍｉｃａｌｌｙ ｄｉｖｅｒｓｅ Ｃｈｋ１ ｉｎｈｉｂｉｔｏｒｓ ｂｙ ｒｅｃｅｐｔｏｒ-ｂａｓｅｄ ｖｉｒｔｕａｌ ｓｃｒｅｅｎｉｎｇ' Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ １４（１４）, 2006, ｐ．４７９２-４８０２
JPN5011005224; Ｍ． ＨＡＹＡＫＡＷＡ: 'ＳＹＮＴＨＥＳＩＳ ＡＮＤ ＢＩＯＬＯＧＩＣＡＬ ＥＶＡＬＵＡＴＩＯＮ ＯＦ ＰＹＲＩＤＯ［３'，２'：４，５］ＦＵＲＯ［３，２-Ｄ］ＰＹＲＩＭＩＤＩＮＥ 以下備考' ＢＩＯＯＲＧＡＮＩＣ ＆ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ＬＥＴＴＥＲＳ Ｖ１７, 2007, Ｐ２４３８-２４４２
JPN5011005225; Ｉ． Ａ． ＢＨＡＴＴＩ: 'ＰＹＲＯＬＹＳＩＳ ＯＦ １-ＳＵＢＳＴＩＴＵＴＥＤ ＰＹＲＡＺＯＬＥＳ ＡＮＤ ＣＨＬＯＲＯＦＯＲＭ ＡＴ ５５０℃： ＦＯＲＭＡＴＩＯＮ 以下備考' ＪＯＵＲＮＡＬ ＯＦ ＴＨＥ ＣＨＥＭＩＣＡＬ ＳＯＣＩＥＴＹ Ｖ１９９７, 1997, Ｐ３５８１-３５８５, ＰＥＲＫＩＮ ＴＲＡＮＳＡＣＴＩＯＮＳ Ｉ
JPN5011005226; Ｒ． Ｈ． ＢＡＫＥＨＡＲ: 'ＳＹＮＴＨＥＳＩＳ ＯＦ ３，８，９-ＴＲＩＳＵＢＳＴＩＴＵＴＥＤ-１，７，９-ＴＲＩＡＺＡ-ＦＬＵＯＲＥＮＥ-６-ＣＡＲＢＯＸＹＬＩＣ ＡＣＩＤ 以下備考' ＢＩＯＯＲＧＡＮＩＣ ＆ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ Ｖ１５, 2007, Ｐ５９５０-５９６４
JPN6013057179; ＳＭＩＴＨ， Ａ．Ｅ． ｅｔ ａｌ．: '（Ｄｉｍｅｔｈｏｘｙ- ａｎｄ ｄｉｈａｌｏｐｙｒｉｄｙｌ）ｂｏｒｏｎｉｃ ａｃｉｄｓ ａｎｄ ｈｉｇｈｌｙ ｆｕｎｃｔｉｏｎａｌｉｚｅｄ ｈｅｔｅｒｏａｒｙｌｐｙｒｉｄｉｎｅｓ ｂｙ Ｓｕｚｕｋｉ' Ｅｕｒｏｐｅａｎ Ｊｏｕｒｎａｌ ｏｆ Ｏｒｇａｎｉｃ Ｃｈｅｍｉｓｔｒｙ （８）, 200803, ｐ．１４５８-１４６３
JPN6013057180; Ａ．Ｍ．ＫＡＭＡＬ ＥＬ-ＤＥＡＮ， ｅｔ ａｌ．: 'Ｓｔｕｄｉｅｓ ｏｎ ｐｙｒｉｄａｚｉｎｅ ｄｅｒｉｖａｔｉｖｅｓ： ｓｙｎｔｈｅｓｉｓ ｏｆ ｐｙｒｒｏｌｏ［２，３-ｃ］ｐｙｒｉｄａｚｉｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ｃｏｍｐｏｕｎｄｓ' Ｂｕｌｌｅｔｉｎ ｏｆ ｔｈｅ Ｐｏｌｉｓｈ Ａｃａｄｅｍｙ ｏｆ Ｓｃｉｅｎｃｅｓ， Ｃｈｅｍｉｓｔｒｙ ４７（２）, 1999, ｐ．１３５-１４２
JPN6013057181; ＷＩＥＣＺＯＲＥＫ， Ｊ． ｅｔ ａｌ．: 'Ａｎｔｉｎｅｏｐｌａｓｔｉｃ ａｃｔｉｖｉｔｙ ｏｆ ａｚａｃａｒｂａｚｏｌｅｓ． ＩＩＩ． Ｓｙｎｔｈｅｓｉｓ ａｎｄ ａｎｔｉｔｕｍｏｒ ｅｖａｌｕａｔｉｏｎ ｏｆ ｓｅｌｅｃｔｅｄ ２-， ３-' Ａｒｃｈｉｖｕｍ Ｉｍｍｕｎｏｌｏｇｉａｅ ｅｔ Ｔｈｅｒａｐｉａｅ Ｅｘｐｅｒｉｍｅｎｔａｌｉｓ Ｖｏｌ．３４， Ｎｏ．３, 1986, ｐ．３２３-３２６
JPN6013057184; ＦＯＬＯＰＰＥ， Ｎ． ｅｔ ａｌ．: 'Ｉｄｅｎｔｉｆｉｃａｔｉｏｎ ｏｆ ｃｈｅｍｉｃａｌｌｙ ｄｉｖｅｒｓｅ Ｃｈｋ１ ｉｎｈｉｂｉｔｏｒｓ ｂｙ ｒｅｃｅｐｔｏｒ-ｂａｓｅｄ ｖｉｒｔｕａｌ ｓｃｒｅｅｎｉｎｇ' Ｂｉｏｏｒｇａｎｉｃ ＆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ １４（１４）, 2006, ｐ．４７９２-４８０２
JPN5011005224; Ｍ． ＨＡＹＡＫＡＷＡ: 'ＳＹＮＴＨＥＳＩＳ ＡＮＤ ＢＩＯＬＯＧＩＣＡＬ ＥＶＡＬＵＡＴＩＯＮ ＯＦ ＰＹＲＩＤＯ［３'，２'：４，５］ＦＵＲＯ［３，２-Ｄ］ＰＹＲＩＭＩＤＩＮＥ 以下備考' ＢＩＯＯＲＧＡＮＩＣ ＆ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ ＬＥＴＴＥＲＳ Ｖ１７, 2007, Ｐ２４３８-２４４２
JPN5011005225; Ｉ． Ａ． ＢＨＡＴＴＩ: 'ＰＹＲＯＬＹＳＩＳ ＯＦ １-ＳＵＢＳＴＩＴＵＴＥＤ ＰＹＲＡＺＯＬＥＳ ＡＮＤ ＣＨＬＯＲＯＦＯＲＭ ＡＴ ５５０℃： ＦＯＲＭＡＴＩＯＮ 以下備考' ＪＯＵＲＮＡＬ ＯＦ ＴＨＥ ＣＨＥＭＩＣＡＬ ＳＯＣＩＥＴＹ Ｖ１９９７, 1997, Ｐ３５８１-３５８５, ＰＥＲＫＩＮ ＴＲＡＮＳＡＣＴＩＯＮＳ Ｉ
JPN5011005226; Ｒ． Ｈ． ＢＡＫＥＨＡＲ: 'ＳＹＮＴＨＥＳＩＳ ＯＦ ３，８，９-ＴＲＩＳＵＢＳＴＩＴＵＴＥＤ-１，７，９-ＴＲＩＡＺＡ-ＦＬＵＯＲＥＮＥ-６-ＣＡＲＢＯＸＹＬＩＣ ＡＣＩＤ 以下備考' ＢＩＯＯＲＧＡＮＩＣ ＆ ＭＥＤＩＣＩＮＡＬ ＣＨＥＭＩＳＴＲＹ Ｖ１５, 2007, Ｐ５９５０-５９６４
JPN6013057179; ＳＭＩＴＨ， Ａ．Ｅ． ｅｔ ａｌ．: '（Ｄｉｍｅｔｈｏｘｙ- ａｎｄ ｄｉｈａｌｏｐｙｒｉｄｙｌ）ｂｏｒｏｎｉｃ ａｃｉｄｓ ａｎｄ ｈｉｇｈｌｙ ｆｕｎｃｔｉｏｎａｌｉｚｅｄ ｈｅｔｅｒｏａｒｙｌｐｙｒｉｄｉｎｅｓ ｂｙ Ｓｕｚｕｋｉ' Ｅｕｒｏｐｅａｎ Ｊｏｕｒｎａｌ ｏｆ Ｏｒｇａｎｉｃ Ｃｈｅｍｉｓｔｒｙ （８）, 200803, ｐ．１４５８-１４６３
JPN6013057180; Ａ．Ｍ．ＫＡＭＡＬ ＥＬ-ＤＥＡＮ， ｅｔ ａｌ．: 'Ｓｔｕｄｉｅｓ ｏｎ ｐｙｒｉｄａｚｉｎｅ ｄｅｒｉｖａｔｉｖｅｓ： ｓｙｎｔｈｅｓｉｓ ｏｆ ｐｙｒｒｏｌｏ［２，３-ｃ］ｐｙｒｉｄａｚｉｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ｃｏｍｐｏｕｎｄｓ' Ｂｕｌｌｅｔｉｎ ｏｆ ｔｈｅ Ｐｏｌｉｓｈ Ａｃａｄｅｍｙ ｏｆ Ｓｃｉｅｎｃｅｓ， Ｃｈｅｍｉｓｔｒｙ ４７（２）, 1999, ｐ．１３５-１４２
JPN6013057181; ＷＩＥＣＺＯＲＥＫ， Ｊ． ｅｔ ａｌ．: 'Ａｎｔｉｎｅｏｐｌａｓｔｉｃ ａｃｔｉｖｉｔｙ ｏｆ ａｚａｃａｒｂａｚｏｌｅｓ． ＩＩＩ． Ｓｙｎｔｈｅｓｉｓ ａｎｄ ａｎｔｉｔｕｍｏｒ ｅｖａｌｕａｔｉｏｎ ｏｆ ｓｅｌｅｃｔｅｄ ２-， ３-' Ａｒｃｈｉｖｕｍ Ｉｍｍｕｎｏｌｏｇｉａｅ ｅｔ Ｔｈｅｒａｐｉａｅ Ｅｘｐｅｒｉｍｅｎｔａｌｉｓ Ｖｏｌ．３４， Ｎｏ．３, 1986, ｐ．３２３-３２６
Attorney, Agent or Firm:
Yoshitaka Sonoda
Yoshinori Kobayashi
Yoshinori Kobayashi
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