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1. 发明申请

US20220056003A1 NEBIVOLOL SYNTHESIS METHOD AND INTERMEDIATE COMPOUND THEREOF 有权
公开(公告)号：US20220056003A1
公开(公告)日：2022-02-24
申请号：US17465606
申请日：2021-09-02
申请人： ZHEJIANG AUSUN PHARMACEUTICAL CO., LTD.
发明人： Zhiguo ZHENG
IPC分类号： C07D311/76 , C07C41/18 , C07C41/20 , C07C41/30 , C07C41/22 , C07D311/58 , C07C43/23 , C07D303/22 , C07D301/14 , C07D301/19 , C07C43/225 , C07F7/08 , A61P9/08 , A61P9/12 , A61K31/353 , C07C43/295 , C07D303/36
摘要： The present invention relates to a nebivolol synthesis method and intermediate compound thereof. Specifically, the present invention relates to a method for synthesizing nebivolol, intermediate compound thereof, and a method for preparing the intermediate compound.

2. 发明授权

US09902682B2 5-bromo-2-(alpha-hydroxypentyl)benzoic acid sodium salts in different crystal forms, and preparation method thereof 有权
公开(公告)号：US09902682B2
公开(公告)日：2018-02-27
申请号：US14905199
申请日：2014-07-10
申请人： Zhejiang Ausun Pharmaceutical Co., Ltd.
发明人： Junbiao Chang , Chuanjun Song
IPC分类号： C07C63/70 , C07C51/09 , C07C51/60
CPC分类号： C07C63/70 , C07B2200/13 , C07C51/09 , C07C51/60 , C07C65/03
摘要： The present invention discloses 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt in different crystal forms and the preparation methods thereof, and belongs to the field of pharmaceutical chemistry. Said different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt include: amorphous 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, crystal form A of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, and crystal form B of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt. The different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt obtained according to the present invention have better stability and water-solubility than the mixed forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, thus is advantageous for pharmaceutical use. Moreover, the different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt possess much better therapeutic effect than 5-bromo-2-(α-hydroxypentyl)benzoic acid potassium salt.

3. 发明公开

US20230159549A1 METHOD FOR PREPARATION OF ASENAPINE 审中-公开
公开(公告)号：US20230159549A1
公开(公告)日：2023-05-25
申请号：US18057916
申请日：2022-11-22
申请人： ZHEJIANG AUSUN PHARMACEUTICAL CO., LTD.
发明人： Zhiguo ZHENG
IPC分类号： C07D491/044
CPC分类号： C07D491/044 , C07B2200/13
摘要： The present invention relates to a method for preparing Asenapine. In particular, the present invention relates to a method for preparing pharmaceutically acceptable Asenapine free base and new crystal form thereof, and also relates to methods for preparing the intermediate compounds used in said method.

4. 发明授权

US11535628B2 Method for preparation of Asenapine 有权
公开(公告)号：US11535628B2
公开(公告)日：2022-12-27
申请号：US16992961
申请日：2020-08-13
申请人： ZHEJIANG AUSUN PHARMACEUTICAL CO., LTD.
发明人： Zhiguo Zheng
IPC分类号： C07D491/044
摘要： The present invention relates to a method for preparing Asenapine. In particular, the present invention relates to a method for preparing pharmaceutically acceptable Asenapine free base and new crystal form thereof, and also relates to methods for preparing the intermediate compounds used in said method.

5. 发明授权

US10696643B2 Posaconazole, composition, intermediate, preparation method and use thereof 有权
公开(公告)号：US10696643B2
公开(公告)日：2020-06-30
申请号：US16081551
申请日：2016-03-04
申请人： Zhejiang Ausun Pharmaceutical Co., Ltd.
发明人： Zhiguo Zheng
IPC分类号： C07D263/26 , C07D405/14 , C07D405/06 , C07D413/06 , C07D407/06
摘要： The present invention relates to a compound of formula III, wherein, R is selected from the group consisting of C1-C4 alkyl, substituted or unsubstituted phenyl, and substituted or unsubstituted benzyl, preferably isopropyl; and two Ar groups may be the same or different, and are each independently selected from the group consisting of substituted or unsubstituted aryl groups, preferably substituted or unsubstituted phenyl, such as p-methoxyphenyl and the like, wherein the compound is preferably in a solid form.

6. 发明申请

US20160168069A1 5-BROMO-2-(alpha-HYDROXYPENTYL)BENZOIC ACID SODIUM SALTS IN DIFFERENT CRYSTAL FORMS, AND PREPARATION METHOD THEREOF 有权
标题翻译：不同晶体形式的5-溴-2-（α-羟基苯甲酸）苯甲酸钠盐及其制备方法
公开(公告)号：US20160168069A1
公开(公告)日：2016-06-16
申请号：US14905199
申请日：2014-07-10
申请人： ZHEJIANG AUSUN PHARMACEUTICAL CO., LTD.
发明人： Junbiao Chang , Chuanjun Song
IPC分类号： C07C63/70 , C07C51/60
CPC分类号： C07C63/70 , C07B2200/13 , C07C51/09 , C07C51/60 , C07C65/03
摘要： The present invention discloses 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt in different crystal forms and the preparation methods thereof, and belongs to the field of pharmaceutical chemistry. Said different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt include: amorphous 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, crystal form A of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, and crystal form B of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt. The different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt obtained according to the present invention have better stability and water-solubility than the mixed forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, thus is advantageous for pharmaceutical use. Moreover, the different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt possess much better therapeutic effect than 5-bromo-2-(α-hydroxypentyl)benzoic acid potassium salt.
摘要翻译：本发明公开了不同结晶形式的5-溴-2-（α-羟基戊基）苯甲酸钠盐及其制备方法，属于药物化学领域。所述不同晶型的5-溴-2-（α-羟基戊基）苯甲酸钠盐包括：无定形5-溴-2-（α-羟基戊基）苯甲酸钠盐，5-溴-2-（ α-羟基戊基）苯甲酸钠盐和5-溴-2-（α-羟基戊基）苯甲酸钠盐的晶型B. 根据本发明得到的5-溴-2-（α-羟戊基）苯甲酸钠盐的不同晶体形式比5-溴-2-（α-羟基戊基）苯甲酸的混合形式具有更好的稳定性和水溶性酸性钠盐，因此对于药物使用是有利的。此外，5-溴-2-（α-羟基戊基）苯甲酸钠盐的不同晶体形式比5-溴-2-（α-羟基戊基）苯甲酸钾盐具有更好的治疗效果。

7. 发明公开

US20230398087A1 APPLICATION OF BZP IN TREATMENT OF ISCHEMIC CARDIOVASCULAR AND CEREBRAL VASCULAR DISEASES 审中-公开
公开(公告)号：US20230398087A1
公开(公告)日：2023-12-14
申请号：US18034144
申请日：2021-10-28
申请人： ZHEJIANG AUSUN PHARMACEUTICAL CO., LTD.
发明人： Zhiguo ZHENG
IPC分类号： A61K31/192 , A61P9/10
CPC分类号： A61K31/192 , A61P9/10
摘要： The present invention relates to an application of 5-bromo-2-(α-hydroxyamyl) sodium benzoate salt (BZP) in treatment of ischemic cardiovascular and cerebral vascular diseases, in particular to a BZP compound for treatment of ischemic stroke and a treatment method, and more specifically, relates to a treatment solution for treating mild and moderate acute ischemic stroke by using the BZP and a pharmaceutical composition comprising the BZP.

8. 发明授权

US11148991B2 5-bromo-2-(alpha-hydroxypentyl)benzoic acid sodium salts in different crystal forms, and preparation method thereof 有权
公开(公告)号：US11148991B2
公开(公告)日：2021-10-19
申请号：US16288863
申请日：2019-02-28
申请人： Zhejiang Ausun Pharmaceutical Co., Ltd.
发明人： Junbiao Chang , Chuanjun Song
IPC分类号： C07C63/70 , C07C51/09 , C07C51/60
摘要： The present invention discloses 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt in different crystal forms and the preparation methods thereof, and belongs to the field of pharmaceutical chemistry. Said different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt include: amorphous 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, crystal form A of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, and crystal form B of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt. The different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt obtained according to the present invention have better stability and water-solubility than the mixed forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, thus is advantageous for pharmaceutical use. Moreover, the different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt possess much better therapeutic effect than 5-bromo-2-(α-hydroxypentyl)benzoic acid potassium salt.

9. 发明授权

US10604471B2 5-bromo-2-(alpha-hydroxypentyl)benzoic acid sodium salts in different crystal forms, and preparation method thereof 有权
公开(公告)号：US10604471B2
公开(公告)日：2020-03-31
申请号：US16452905
申请日：2019-06-26
申请人： Zhejiang Ausun Pharmaceutical Co., Ltd.
发明人： Junbiao Chang , Chuanjun Song
IPC分类号： C07C63/70 , C07C51/09 , C07C51/60
摘要： The present invention discloses 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt in different crystal forms and the preparation methods thereof, and belongs to the field of pharmaceutical chemistry. Said different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt include: amorphous 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, crystal form A of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, and crystal form B of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt. The different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt obtained according to the present invention have better stability and water-solubility than the mixed forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, thus is advantageous for pharmaceutical use. Moreover, the different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt possess much better therapeutic effect than 5-bromo-2-(α-hydroxypentyl)benzoic acid potassium salt.

10. 发明申请

US20190194116A1 5-BROMO-2-(alpha-HYDROXYPENTYL)BENZOIC ACID SODIUM SALTS IN DIFFERENT CRYSTAL FORMS, AND PREPARATION METHOD THEREOF 审中-公开
公开(公告)号：US20190194116A1
公开(公告)日：2019-06-27
申请号：US16288863
申请日：2019-02-28
申请人： Zhejiang Ausun Pharmaceutical Co., Ltd.
发明人： Junbiao Chang , Chuanjun Song
IPC分类号： C07C63/70 , C07C51/60 , C07C51/09
CPC分类号： C07C63/70 , C07B2200/13 , C07C51/09 , C07C51/60 , C07C65/03
摘要： The present invention discloses 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt in different crystal forms and the preparation methods thereof, and belongs to the field of pharmaceutical chemistry. Said different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt include: amorphous 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, crystal form A of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, and crystal form B of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt. The different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt obtained according to the present invention have better stability and water-solubility than the mixed forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt, thus is advantageous for pharmaceutical use. Moreover, the different crystal forms of 5-bromo-2-(α-hydroxypentyl)benzoic acid sodium salt possess much better therapeutic effect than 5-bromo-2-(α-hydroxypentyl)benzoic acid potassium salt.

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