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1. 发明授权

US4824842A Cinnamoyl piperidines and thiomorpholine and cerebral protection compositions 失效
标题翻译：肉桂酰哌啶和硫代吗啉和脑保护组合物
公开(公告)号：US4824842A
公开(公告)日：1989-04-25
申请号：US829382
申请日：1986-02-13
申请人： Joji Nakamura , Kazuhiro Kubo , Shunji Ichikawa , Hajime Takahashi , Keisuke Isozumi , Toyofumi Yamada
发明人： Joji Nakamura , Kazuhiro Kubo , Shunji Ichikawa , Hajime Takahashi , Keisuke Isozumi , Toyofumi Yamada
IPC分类号： A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P25/28 , C07D211/16 , C07D211/22 , C07D211/46 , C07D265/30 , C07D265/32 , C07D279/12 , C07D295/18 , C07D295/185
CPC分类号： C07D265/30 , C07D211/16 , C07D211/22 , C07D279/12 , C07D295/185
摘要： Compounds of the general formula ##STR1## wherein: X is halogen or trifluoromethyl;R.sub.1 is hydrogen, halogen or trifluoromethyl;R.sub.2 is hydrogen, methyl or hydroxymethyl;R.sub.3 is hydrogen or lower alkyl; andY is methylene, methylene substituted with a lower alkyl or hydroxyl group, sulfinyl, sulfonyl, oxygen or sulfur, exhibit a cerebral protective effect and are applicable to the treatment of cerebral ischaemia and cerebral hypoxia.The compounds may be made by acylating a suitable piperidine or morpholine with the appropriate cinnamoyl chloride, and if necessary oxidizing the reaction product.
摘要翻译：通式（I）的化合物其中：X为卤素或三氟甲基; R1是氢，卤素或三氟甲基; R2是氢，甲基或羟甲基; R3是氢或低级烷基; Y为亚甲基，被低级烷基或羟基取代的亚甲基，亚磺酰基，磺酰基，氧或硫，表现出脑保护作用，适用于治疗脑缺血和脑缺氧。可以通过用合适的肉桂酰氯将适当的哌啶或吗啉酰化，并且如果需要氧化反应产物，可以制备化合物。

2. 发明授权

US4962107A Agent for cerebral protection 失效
标题翻译：脑保护剂
公开(公告)号：US4962107A
公开(公告)日：1990-10-09
申请号：US321692
申请日：1989-03-10
申请人： Joji Nakamura , Kazuhiro Kubo , Shunji Ichikawa , Hajime Takahashi , Keisuke Isozumi , Toyofumi Yamada
发明人： Joji Nakamura , Kazuhiro Kubo , Shunji Ichikawa , Hajime Takahashi , Keisuke Isozumi , Toyofumi Yamada
IPC分类号： A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P25/28 , C07D211/16 , C07D211/22 , C07D211/46 , C07D265/30 , C07D265/32 , C07D279/12 , C07D295/18 , C07D295/185
CPC分类号： C07D265/30 , C07D211/16 , C07D211/22 , C07D279/12 , C07D295/185
摘要： Compounds of the general formula ##STR1## wherein: X is halogen or trifluoromethyl;R.sub.1 is hydrogen, halogen or trifluoromethyl;R.sub.2 is hydrogen methyl or hydroxymethyl;R.sub.3 is hydrogen or lower alkyl; andY is methylene, methylene substituted with a lower alkyl or hydroxyl group, sulfinyl, sulfonyl, oxygen or sulfur, exhibit a cerebral protective effect and are applicable to the treatment of cerebral ischaemia and cerebral hypoxia.The compounds may be made by acylating a suitable piperidine or morpholine with the appropriate cinnamoyl chloride, and if necessary oxidizing the reaction product.

3. 发明授权

US06576765B2 Process for preparing amic acid esters 有权
标题翻译：酰胺酸酯的制备方法
公开(公告)号：US06576765B2
公开(公告)日：2003-06-10
申请号：US09980103
申请日：2002-03-18
申请人： Keisuke Isozumi
发明人： Keisuke Isozumi
IPC分类号： C07D27764
CPC分类号： C07C269/04 , C07D277/64
摘要： The present invention provides a process for producing an amic acid ester represented by the following general formula (7) (wherein A is substituted or unsubstituted lower alkylene or the like; R1 is substituted or unsubstituted lower alkyl or the like; and R3 is hydrogen or lower alkyl), which process comprises reacting, in the presence of water, an amino acid represented by formula (1) with a halogenated carbonic acid ester represented by formula (2) (wherein X is halogen) to form an amide compound represented by formula (3), then reacting the amide compound with a halogenated carbonic acid ester represented by formula (4) (wherein R2 is substituted or unsubstituted lower alkyl or the like; and X is halogen) to form, in the system, a mixed acid anhydride represented by formula (5), and reacting the mixed acid anhydride with an amine compound represented by formula (6) (wherein Het is substituted or unsubstituted heterocyclic).
摘要翻译：本发明提供由以下通式（7）表示的酰胺酸酯的制造方法（其中A为取代或未取代的低级亚烷基等; R 1为取代或未取代的低级烷基等; R 3为氢或低级烷基），该方法包括在水存在下使由式（1）表示的氨基酸与由式（2）表示的卤代碳酸酯（其中X为卤素）反应以形成式（3），然后使酰胺化合物与由式（4）表示的卤代碳酸酯（其中R 2是取代或未取代的低级烷基等，X是卤素）反应，在体系中形成混合酸酐由式（5）表示，并使混合的酸酐与由式（6）表示的胺化合物（其中Het是取代或未取代的杂环）反应。

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