公开(公告)号：US07795458B2

公开(公告)日：2010-09-14

申请号：US12545665

申请日：2009-08-21

申请人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

发明人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

IPC分类号： C07D303/48

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet) 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm−1.

摘要翻译： 本发明涉及用（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并改善储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱（KBr片剂）3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm-1的特征吸收带。

公开(公告)号：US20110003993A1

公开(公告)日：2011-01-06

申请号：US12880655

申请日：2010-09-13

申请人： Atsushi TENDO ,  Toshihiro TAKAHASHI ,  Tomio YAMAKAWA ,  Kazuki OKAI ,  Susumu NIHASHI

发明人： Atsushi TENDO ,  Toshihiro TAKAHASHI ,  Tomio YAMAKAWA ,  Kazuki OKAI ,  Susumu NIHASHI

IPC分类号： C07D295/02 ,  C07D303/48

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm×1.

摘要翻译： 本发明涉及用（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并改善储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱的特征吸收带（KBr片剂）：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm -1。

公开(公告)号：US08163942B2

公开(公告)日：2012-04-24

申请号：US12880655

申请日：2010-09-13

申请人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

发明人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

IPC分类号： C07D303/48

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm−1.

摘要翻译： 本发明涉及用（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并改善储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱（KBr片剂）的特征吸收带：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm-1。

公开(公告)号：US20090312563A1

公开(公告)日：2009-12-17

申请号：US12545665

申请日：2009-08-21

申请人： Atsushi TENDO ,  Toshihiro TAKAHASHI ,  Tomio YAMAKAWA ,  Kazuki OKAI ,  Susumu NIHASHI

发明人： Atsushi TENDO ,  Toshihiro TAKAHASHI ,  Tomio YAMAKAWA ,  Kazuki OKAI ,  Susumu NIHASHI

IPC分类号： C07D303/40

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet) 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm−1.

摘要翻译： 本发明涉及用（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并改善储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱（KBr片剂）3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm-1的特征吸收带。

公开(公告)号：US07585988B2

公开(公告)日：2009-09-08

申请号：US10553946

申请日：2004-04-22

申请人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

发明人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

IPC分类号： C07D303/48

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics:DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; andcharacteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm−1.

摘要翻译： 本发明涉及用（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并改善储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱（KBr片剂）的特征吸收带：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm-1。

公开(公告)号：US20060252826A1

公开(公告)日：2006-11-09

申请号：US10553946

申请日：2004-04-22

申请人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

发明人： Atsushi Tendo ,  Toshihiro Takahashi ,  Tomio Yamakawa ,  Kazuki Okai ,  Susumu Nihashi

IPC分类号： A61K31/336 ,  C07D303/02

CPC分类号： C07D303/48

摘要： The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm−1.

摘要翻译： 本发明涉及用（2S，3S）-3 - [[（1S）-1-异丁氧基甲基-3-甲基丁基]氨基甲酰基]环氧乙烷-2-羧酸[以下称为羧酸] 所述羧酸与选自哌嗪，金刚烷胺等的有机胺反应。 本发明还涉及提供羧酸的结晶钠盐。 钠盐可用作制备药物的材料并改善储存稳定性，具有以下特征：DSC：在170至175℃的温度范围内观察到的放热峰，重量减少; 和红外吸收光谱的特征吸收带（KBr片剂）：3255,2950,2860,1670,1630,1550,1460,1435,1395,1365,1310,1260,1110,890cm -1 。

公开(公告)号：US4339379A

公开(公告)日：1982-07-13

申请号：US194844

申请日：1980-10-07

申请人： Mitsuo Masaki ,  Toru Yamanaka ,  Mitsuko Yoshioka ,  Kazuki Okai

发明人： Mitsuo Masaki ,  Toru Yamanaka ,  Mitsuko Yoshioka ,  Kazuki Okai

IPC分类号： A61K31/415 ,  A61K38/00 ,  A61P1/04 ,  C07D233/54 ,  C07D233/64 ,  C07C103/52 ,  A61K37/02

CPC分类号： C07D233/64 ,  Y10S514/927

摘要： An N-acylcarnosine aluminum salt of the formula, ##STR1## wherein R represents a lower alkyl group having 1 to 6 carbon atoms is effective for use as an anti-ulcer agent.

摘要翻译： 下式的N-酰基肌氨酸铝盐，其中R表示碳原子数为1〜6的低级烷基，作为抗溃疡剂有效。