Title:
フェニルシクロブチルアミド誘導体およびそれらの立体異性体、それらの調製方法ならびにそれらの使用
Document Type and Number:
Japanese Patent JP2011516506
Kind Code:
A
Abstract:
Phenylcyclobutylamide derivatives and their optical isomers, the preparing processes and the uses thereof, which includes the compounds of formula (I), their pure stereoisomers and their pharmaceutically acceptable salts. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t -butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The present novel compounds have pharmaceutical activity and are prepared by condensation reaction of racemic, levo- or dextro- demethyl Sibutramine and racemic or D/L isoleucine under a mild condition. It is demonstrated that the present compounds have effect of losing weight to obese mode rats in different level and the effect is better than Sibutramine by the animal experiments. So the medicaments prepared by the present compounds or the medicaments prepared by the compositions of the present compounds and other pharmaceutical activity compounds may be used for treating obesity.
Inventors:
Chao, Shu Chien
Wen, Shomin
Din, Hao
Yan, Yassy
Chen, Xiaoping
Wen, Shomin
Din, Hao
Yan, Yassy
Chen, Xiaoping
Application Number:
JP2011503327A
Publication Date:
May 26, 2011
Filing Date:
March 24, 2009
Export Citation:
Assignee:
BEIJING YINGU CENTURY PHARMACY CO., LTD.
International Classes:
C07C237/06; C07C231/20; C07C271/22
Domestic Patent References:
| JPH11506439A | 1999-06-08 | |||
| JP2003519675A | 2003-06-24 | |||
| JP2007500242A | 2007-01-11 | |||
| JP2003534312A | 2003-11-18 | |||
| JPH11506439A | 1999-06-08 | |||
| JP2003519675A | 2003-06-24 | |||
| JP2007500242A | 2007-01-11 | |||
| JP2003534312A | 2003-11-18 |
Foreign References:
| EP1964555A1 | 2008-09-03 | |||
| CN1557803A | 2004-12-29 | |||
| WO2000056311A1 | 2000-09-28 | |||
| EP1964555A1 | 2008-09-03 | |||
| CN1557803A | 2004-12-29 | |||
| WO2000056311A1 | 2000-09-28 |
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JPN6013000224; Ｌｕ， Ｂｒｕｃｅ Ｚ． ｅｔ ａｌ．: 'Ｃｏｎｔｒｏｌ ｏｆ Ｄｉａｓｔｅｒｅｏｓｅｌｅｃｔｉｖｉｔｙ ｂｙ Ｓｏｌｖｅｎｔ Ｅｆｆｅｃｔｓ ｉｎ ｔｈｅ Ａｄｄｉｔｉｏｎ ｏｆＧｒｉｇｎａｒｄ Ｒｅａｇｅｎｔｓ ｔｏ Ｅｎａｎｔｉｏｐｕｒ' Ｏｒｇａｎｉｃ Ｌｅｔｔｅｒｓ Ｖｏｌ．７， Ｎｏ．１３, 2005, ｐ．２５９９-２６０２
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JPN6013000224; Ｌｕ， Ｂｒｕｃｅ Ｚ． ｅｔ ａｌ．: 'Ｃｏｎｔｒｏｌ ｏｆ Ｄｉａｓｔｅｒｅｏｓｅｌｅｃｔｉｖｉｔｙ ｂｙ Ｓｏｌｖｅｎｔ Ｅｆｆｅｃｔｓ ｉｎ ｔｈｅ Ａｄｄｉｔｉｏｎ ｏｆＧｒｉｇｎａｒｄ Ｒｅａｇｅｎｔｓ ｔｏ Ｅｎａｎｔｉｏｐｕｒ' Ｏｒｇａｎｉｃ Ｌｅｔｔｅｒｓ Ｖｏｌ．７， Ｎｏ．１３, 2005, ｐ．２５９９-２６０２
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JPN6013000225; Ｌｉｎｋ， Ｍａｒｅｋ ｅｔ ａｌ．: 'Ｍｅｔａｂｏｌｉｔｅ ｐｒｏｆｉｌｅ ｏｆ ｓｉｂｕｔｒａｍｉｎｅ ｉｎ ｈｕｍａｎ ｕｒｉｎｅ： ａ ｌｉｑｕｉｄｃｈｒｏｍａｔｏｇｒａｐｈｙ-ｅｌｅｃｔｒｏｓｐｒａｙ ｉｏｎｉｚａｔｉｏｎ ｍａｓ' Ｊｏｕｒｎａｌ ｏｆ Ｍａｓｓ Ｓｐｅｃｔｒｏｍｅｔｒｙ Ｖｏｌ．４１， Ｎｏ．９, 2006, ｐ．１１７１-１１７８
JPN6013000224; Ｌｕ， Ｂｒｕｃｅ Ｚ． ｅｔ ａｌ．: 'Ｃｏｎｔｒｏｌ ｏｆ Ｄｉａｓｔｅｒｅｏｓｅｌｅｃｔｉｖｉｔｙ ｂｙ Ｓｏｌｖｅｎｔ Ｅｆｆｅｃｔｓ ｉｎ ｔｈｅ Ａｄｄｉｔｉｏｎ ｏｆＧｒｉｇｎａｒｄ Ｒｅａｇｅｎｔｓ ｔｏ Ｅｎａｎｔｉｏｐｕｒ' Ｏｒｇａｎｉｃ Ｌｅｔｔｅｒｓ Ｖｏｌ．７， Ｎｏ．１３, 2005, ｐ．２５９９-２６０２
JPN6013000225; Ｌｉｎｋ， Ｍａｒｅｋ ｅｔ ａｌ．: 'Ｍｅｔａｂｏｌｉｔｅ ｐｒｏｆｉｌｅ ｏｆ ｓｉｂｕｔｒａｍｉｎｅ ｉｎ ｈｕｍａｎ ｕｒｉｎｅ： ａ ｌｉｑｕｉｄｃｈｒｏｍａｔｏｇｒａｐｈｙ-ｅｌｅｃｔｒｏｓｐｒａｙ ｉｏｎｉｚａｔｉｏｎ ｍａｓ' Ｊｏｕｒｎａｌ ｏｆ Ｍａｓｓ Ｓｐｅｃｔｒｏｍｅｔｒｙ Ｖｏｌ．４１， Ｎｏ．９, 2006, ｐ．１１７１-１１７８
Attorney, Agent or Firm:
Katsuto Momii