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1. 发明专利

IL172561D0 NOVEL PROCESS FOR PREPARING PRAMIPEXOLE AND ITS OPTICAL ISOMERIC MIXTURE BY REDUCTION WITH SODIUM TRIACETOXYBOROHYDRIDE 未知
公开(公告)号：IL172561D0
公开(公告)日：2006-04-10
申请号：IL17256105
申请日：2005-12-13
申请人： CHEMAGIS LTD , MICHAEL BRAND , ODED ARAD , GUANGXIN XIA , YIFENG NIAN , TIEMA YAN , JIN SUO
IPC分类号： C07D20100101

2. 发明授权

US09278944B2 Nitrogen-containing saturated heterocyclic compound 有权
标题翻译：含氮饱和杂环化合物
公开(公告)号：US09278944B2
公开(公告)日：2016-03-08
申请号：US14005512
申请日：2012-03-15
申请人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie , Miki Hirai
发明人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie , Miki Hirai
IPC分类号： C07D241/36 , C07D265/30 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D471/04 , C07D231/56
CPC分类号： C07D265/30 , C07D231/56 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
摘要翻译：本发明提供式[I]的含氮饱和杂环化合物：其中R 1为环烷基等，R 22为任意取代的芳基等，R为低级烷基等，T为羰基，Z为-O-等，R3〜R6相同或不同，为氢原子等; 或药学上可接受的盐，其可用作肾素抑制剂。

3. 发明申请

US20100240644A1 MORPHOLINE DERIVATIVE 有权
标题翻译：吗啉衍生物
公开(公告)号：US20100240644A1
公开(公告)日：2010-09-23
申请号：US12664637
申请日：2008-06-16
申请人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： A61K31/538 , C07D265/30 , A61K31/5375 , C07D265/36 , C07D413/12 , A61K31/5377 , C07D409/12 , A61K31/5355 , A61P9/12
CPC分类号： C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.
摘要翻译：本发明提供式[I]的吗啉衍生物。其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。这些化合物可用作肾素抑制剂。

4. 发明授权

US09371292B2 Quinazoline derivative, preparation method therefor, intermediate, composition and application thereof 有权
标题翻译：喹唑啉衍生物，其制备方法，中间体，组成和应用
公开(公告)号：US09371292B2
公开(公告)日：2016-06-21
申请号：US14234514
申请日：2012-07-27
申请人： Guangxin Xia , Jingkang Shen , Yongping Yu , Wenteng Chen , Chunchun Zhang , Yu Hao , Jing Zhang , Bojun Li , Xuejun Liu
发明人： Guangxin Xia , Jingkang Shen , Yongping Yu , Wenteng Chen , Chunchun Zhang , Yu Hao , Jing Zhang , Bojun Li , Xuejun Liu
IPC分类号： C07D239/94 , A61K31/517 , A61P35/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.
摘要翻译：公开了由式（I）喹唑啉衍生物及其药学上可接受的盐，或其对映异构体，非对映异构体，互变异构体，外消旋物，溶剂合物，代谢前体或前体药物表示。还公开了其制备方法，中间体，具有喹唑啉衍生物的药物组合物及其应用。本发明的喹唑啉衍生物具有改善的抗肿瘤活性。

5. 发明授权

US08975252B2 Morpholine derivative 有权
标题翻译：吗啉衍生物
公开(公告)号：US08975252B2
公开(公告)日：2015-03-10
申请号：US12664637
申请日：2008-06-16
申请人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Hidenori Akatsuka , Hiroshi Sugama , Nobumasa Awai , Takayuki Kawaguchi , Yoichi Takahashi , Toru Iijima , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： A61K31/535 , C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D265/30 , C07D209/08 , C07D209/14 , C07D209/30 , C07D209/34 , C07D209/42 , C07D231/56 , C07D265/36 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention provides a morpholine derivative of the formula [I]; wherein R1 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; R2 is a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R3, R4, R5 and R6 are the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group; or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.
摘要翻译：本发明提供式[I]的吗啉衍生物。其中R1是取代的烷基，任选取代的芳基，任选取代的杂环基，环烷基或烷基; R 2是取代的烷基，任选取代的芳基，任选取代的杂环基，任选取代的烷基羰基，任选取代的芳基羰基，任选取代的杂环取代的羰基或环烷基羰基; T是亚甲基或羰基; R3，R4，R5和R6相同或不同，氢原子，任选取代的氨基甲酰基或任选取代的烷基; 或其药学上可接受的盐。这些化合物可用作肾素抑制剂。

6. 发明申请

US20140206687A1 QUINAZOLINE DERIVATIVE, PREPARATION METHOD THEREFOR, INTERMEDIATE, COMPOSITION AND APPLICATION THEREOF 有权
标题翻译：喹诺酮衍生物，其制备方法，中间体，组合物及其应用
公开(公告)号：US20140206687A1
公开(公告)日：2014-07-24
申请号：US14234514
申请日：2012-07-27
申请人： Guangxin Xia , Jingkang Shen , Yongping Yu , Wenteng Chen , Chunchun Zhang , Yu Hao , Jing Zhang , Bojun Li , Xuejun Liu
发明人： Guangxin Xia , Jingkang Shen , Yongping Yu , Wenteng Chen , Chunchun Zhang , Yu Hao , Jing Zhang , Bojun Li , Xuejun Liu
IPC分类号： C07D239/94
CPC分类号： C07D239/94 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Disclosed are as represented by Formula (I) a quinazoline derivative and a pharmaceutical acceptable salt thereof, or, an enantiomer, a non-enantiomer, a tautomer, a racemate, a solvate, a metabolic precursor, or a prodrug of both. Also disclosed are a preparation method therefor, an intermediate, a pharmaceutical composition having the quinazoline derivative, and an application thereof. The quinazoline derivative of the present invention is provided with improved anti-tumor activity.
摘要翻译：公开了由式（I）喹唑啉衍生物及其药学上可接受的盐，或其对映异构体，非对映异构体，互变异构体，外消旋物，溶剂合物，代谢前体或前体药物表示。还公开了其制备方法，中间体，具有喹唑啉衍生物的药物组合物及其应用。本发明的喹唑啉衍生物具有改善的抗肿瘤活性。

7. 发明申请

US20060148866A1 Novel process for preparing pramipexole and its optical isomeric mixture by reduction with sodium triacetoxyborohydride 审中-公开
标题翻译：用三乙酰氧基硼氢化钠还原制备普拉克索及其光学异构体混合物的新方法
公开(公告)号：US20060148866A1
公开(公告)日：2006-07-06
申请号：US11299752
申请日：2005-12-13
申请人： Guangxin Xia , Yifeng Nian , Tiema Yan , Jin Suo , Michael Brand , Oded Arad
发明人： Guangxin Xia , Yifeng Nian , Tiema Yan , Jin Suo , Michael Brand , Oded Arad
IPC分类号： C07D277/82 , A61K31/428
CPC分类号： C07D277/82
摘要： A novel process is provided for producing pramipexole base or its optical isomeric mixture as defined hereinabove i.e. (R,S)-2-amino-6-propyl-4,5,6,7-tetrahydrobenzothiazole avoiding the use of borane tetrahydrofuran complex and using a more convenient reducing agent like sodium triacetoxyborohydride instead. The provided process comprises reacting the starting material (S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole or its optical isomeric mixture as defined hereinabove i.e. (R,S)-2,6-diamino-4,5,6,7-tetrahydrobenzothiazole with propionaldehyde in an organic solvent to obtain the respective enamine, which is subsequently reduced in situ, optionally without isolation, to obtain pramipexole or its optical isomeric mixture as defined hereinabove i.e. (R,S)-2-amino-6-propyl-4,5,6,7-tetrahydrobenzothiazole, and the acid addition salts thereof. The present invention also provides a process for purifying pramipexole dihydrochloride or the dihydrochloride salt of its optical isomeric mixture as defined hereinabove i.e. (R,S)-2-amino-6-propyl-4,5,6,7-tetrahydrobenzothiazole dihydrochloride by re-crystallization from a suitable solvent.
摘要翻译：提供了一种制备普拉克索碱或其如上所述的光学异构体混合物的新方法，即（R，S）-2-氨基-6-丙基-4,5,6,7-四氢苯并噻唑，避免使用硼烷四氢呋喃络合物并使用一种更方便的还原剂，如三乙酰氧基硼氢化钠。所提供的方法包括使起始原料（S）-2,6-二氨基-4,5,6,7-四氢苯并噻唑或其如上文所定义的光学异构体混合物即（R，S）-2,6-二氨基-4， 5,6,7-四氢苯并噻唑与丙醛在有机溶剂中反应，得到各自的烯胺，其随后可原位还原，任选不分离，得到如上所述的普拉克索或其旋光异构体混合物，即（R，S）-2- 氨基-6-丙基-4,5,6,7-四氢苯并噻唑及其酸加成盐。本发明还提供了纯化普拉克索二盐酸盐或其如上所述的光学异构体混合物的二盐酸盐的方法，即（R，S）-2-氨基-6-丙基-4,5,6,7-四氢苯并噻唑二盐酸盐， - 从合适的溶剂中结晶。

8. 发明申请

US20140011807A1 NITROGEN-CONTAINING SATURATED HETEROCYCLIC COMPOUND 有权
标题翻译：含氮饱和杂环化合物
公开(公告)号：US20140011807A1
公开(公告)日：2014-01-09
申请号：US14005512
申请日：2012-03-15
申请人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie
发明人： Toru Iijima , Hiroshi Sugama , Takayuki Kawaguchi , Jingkang Shen , Guangxin Xia , Jianshu Xie
IPC分类号： C07D265/30 , C07D403/12 , C07D231/56 , C07D413/14 , C07D405/12 , C07D413/12 , C07D471/04
CPC分类号： C07D265/30 , C07D231/56 , C07D403/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein R1 is a cycloalkyl group and the like, R22 is an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is —O— and the like, and R3 to R6 are the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.
摘要翻译：本发明提供式[I]的含氮饱和杂环化合物：其中R 1为环烷基等，R 22为任意取代的芳基等，R为低级烷基等，T为羰基，Z为-O-等，R3〜R6相同或不同，为氢原子等; 或药学上可接受的盐，其可用作肾素抑制剂。

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