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1. 发明授权

EP2251319B1 Process for preparing derivatives of benzoic acid 有权
标题翻译：一种用于苯甲酸衍生物的制备过程
公开(公告)号：EP2251319B1
公开(公告)日：2012-02-08
申请号：EP10174006.6
申请日：2006-09-01
申请人： Otsuka Pharmaceutical Co., Ltd.
发明人： Torisawa, Yasuhiro , Abe, Kaoru , Muguruma, Yasuaki , Fujita, Shigekazu , Ogawa, Hidenori , Utsumi, Naoto , Miyake, Masahiro
IPC分类号： C07C233/81
CPC分类号： C07D223/16 , C07C231/12 , C07C233/81

2. 发明授权

EP2261215B1 Process for preparing benzazepine compounds or salts thereof 有权
标题翻译：一种用于Benzazepineverbindungen或其盐的制备方法
公开(公告)号：EP2261215B1
公开(公告)日：2014-12-31
申请号：EP10174000.9
申请日：2006-09-01
申请人： Otsuka Pharmaceutical Co., Ltd.
发明人： Torisawa, Yasuhiro , Abe, Kaoru , Muguruma, Yasuaki , Fujita, Shigekazu , Ogawa, Hidenori , Utsumi, Naoto , Miyake, Masahiro
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07C231/12 , C07C233/81

3. 发明公开

EP2251319A3 Process for preparing derivatives of benzoic acid 有权
标题翻译： Verfahren zur Herstellung von Benzoesaure Derivaten
公开(公告)号：EP2251319A3
公开(公告)日：2011-03-09
申请号：EP10174006.6
申请日：2006-09-01
申请人： Otsuka Pharmaceutical Co., Ltd.
发明人： Torisawa, Yasuhiro , Abe, Kaoru , Muguruma, Yasuaki , Fujita, Shigekazu , Ogawa, Hidenori , Utsumi, Naoto , Miyake, Masahiro
IPC分类号： C07C233/81
CPC分类号： C07D223/16 , C07C231/12 , C07C233/81
摘要： This invention provides a process for preparing benzazepine compounds of the formula (1):

wherein X 1 is a halogen atom, R 1 and R 2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.
摘要翻译：本发明提供了制备式（1）的苯并氮杂化合物的方法：其中X 1为卤素原子，R 1和R 2为低级烷基，或其盐以及高产率和高的中间体苯甲酸化合物其可用作制备具有加压素拮抗活性的药学活性2,3,4,5-四氢-1H-1-苯并氮杂化合物的中间体。

4. 发明公开

EP2166368A1 Nuclear magnetic resonance measuring method for solid samples 审中-公开
标题翻译： Nukleares MagnetresonanzmessverfahrenfürFeststoffproben
公开(公告)号：EP2166368A1
公开(公告)日：2010-03-24
申请号：EP09179878.5
申请日：2005-07-27
申请人： OTSUKA PHARMACEUTICAL CO., LTD.
发明人： Miura, Iwao , Miyake, Masahiro
IPC分类号： G01R33/46 , G01R33/44
CPC分类号： G01R33/44 , G01R33/4641
摘要： In a nuclear magnetic resonance measuring method for solid samples, there are provided the steps of exciting a nuclear spin of a solid sample placed in a static magnetic field by allowing exciting pulses to pass through a receiver coil. A FID signal (Free Induction Decay signal) is received from the excited nuclear spin by applying reading pulses after a lapse of time τ after applying the exciting pulses is finished. An Inversion Recovery IR - Nuclear Magnetic Resonance NMR spectrum is obtained by subjecting the FID signal to a frequency conversion process. The estimation of a constituent ratio of constituent substances of the solid sample is achieved by acquiring a plurality of FID signals while changing the period of time τ, by calculating IR-NMR spectra based on these FID signals, by obtaining a longitudinal relaxation curve by plotting spectrum strength with respect to time τ in a specific frequency of the TR-NMR spectrum, and by making a regression analysis while regarding the longitudinal relaxation curve as a total sum of a plurality of longitudinal relaxation curves differing in longitudinal relaxation time.
摘要翻译：在固体样品的核磁共振测量方法中，提供了通过允许激发脉冲通过接收器线圈来激发置于静态磁场中的固体样品的核自旋的步骤。通过在施加激励脉冲之后的经过时间Ä之后施加读取脉冲从受激核反应接收FID信号（自由感应衰减信号）。通过对FID信号进行频率转换处理，获得反转恢复IR-核磁共振NMR光谱。通过基于这些FID信号计算IR-NMR光谱，通过绘制纵向弛豫曲线，通过获取多个FID信号同时改变时间段Ä来实现固体样品的构成物质的组成比的估计相对于TR-NMR光谱的特定频率的时间Ä的频谱强度，并且通过进行回归分析，同时关于纵向弛豫曲线作为纵向弛豫时间不同的多个纵向弛豫曲线的总和。

5. 发明公开

EP2261215A1 Process for preparing benzazepine compounds or salts thereof 有权
标题翻译： Verfahrenfürdie Zubereitung von Benzazepineverbindungen oder Salzen daraus
公开(公告)号：EP2261215A1
公开(公告)日：2010-12-15
申请号：EP10174000.9
申请日：2006-09-01
申请人： Otsuka Pharmaceutical Co., Ltd.
发明人： Torisawa, Yasuhiro , Abe, Kaoru , Muguruma, Yasuaki , Fujita, Shigekazu , Ogawa, Hidenori , Utsumi, Naoto , Miyake, Masahiro
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , C07C231/12 , C07C233/81
摘要： This invention provides a process for preparing benzazepine compounds of the formula (1):

wherein X 1 is a halogen atom, R 1 and R 2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.
摘要翻译：本发明提供了制备式（1）的苯并氮杂化合物的方法：其中X 1为卤素原子，R 1和R 2为低级烷基，或其盐以及高产率和高的中间体苯甲酸化合物其可用作制备具有加压素拮抗活性的药学活性2,3,4,5-四氢-1H-1-苯并氮杂化合物的中间体。

6. 发明公开

EP2251319A2 Process for preparing derivatives of benzoic acid 有权
标题翻译：一种用于苯甲酸衍生物的制备过程
公开(公告)号：EP2251319A2
公开(公告)日：2010-11-17
申请号：EP10174006.6
申请日：2006-09-01
申请人： Otsuka Pharmaceutical Co., Ltd.
发明人： Torisawa, Yasuhiro , Abe, Kaoru , Muguruma, Yasuaki , Fujita, Shigekazu , Ogawa, Hidenori , Utsumi, Naoto , Miyake, Masahiro
IPC分类号： C07C233/81
CPC分类号： C07D223/16 , C07C231/12 , C07C233/81
摘要： This invention provides a process for preparing benzazepine compounds of the formula (1):

wherein X 1 is a halogen atom, R 1 and R 2 are a lower alkyl group, or salts thereof as well as intermediate benzoic acid compounds in high yield and high purity on industrial scale, which are useful as an intermediate for preparing a pharmaceutically active 2,3,4,5-tetrahydro-1H-1-benzazepine compound having vasopressin antagonistic activity.

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