公开(公告)号：US10174011B2

公开(公告)日：2019-01-08

申请号：US15124264

申请日：2015-03-09

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. ,  TOPHARMAN SHANDONG CO., LTD.

Inventor： Hualiang Jiang ,  Zhen Wang ,  Jianfeng Li ,  Rongxia Zhang ,  Yang He ,  Yongjian Liu ,  Minghao Bi ,  Zheng Liu ,  Guanghui Tian ,  Weiming Chen ,  Feipu Yang ,  Chunhui Wu ,  Yu Wang ,  Xiangrui Jiang ,  Jingjing Yin ,  Guan Wang ,  Jingshan Shen

IPC: C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  A61K31/496 ,  A61K31/519 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55

Abstract: The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.

公开(公告)号：US20150284351A1

公开(公告)日：2015-10-08

申请号：US14434563

申请日：2013-10-10

Applicant: TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  TOPHARMAN SHANDONG CO., LTD.

Inventor： Guan Wang ,  Xiangrui Jiang ,  Xudong Gong ,  Weiming Chen ,  Fuqiang Zhu ,  Rongxia Zhang ,  Xianguo Zhao

IPC: C07D307/33 ,  C07D413/12

CPC classification number: C07D307/33 ,  C07D413/12

Abstract: This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.

Abstract translation: 本发明公开了单一构型的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯及其制备方法和用途。 根据本发明的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯或其药学上可接受的盐，酯，前药或溶剂化物是各种抗 - 病毒和抗肿瘤活性成分。 通过酰化反应从（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯获得的化合物可以直接用于制备各种抗病毒和抗肿瘤药物。 根据本发明的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯化合物的手性合成方法和自发拆分方法具有以下优点：反应路线短而简单 产量高，成本低，适合工业应用。

公开(公告)号：US20170158680A1

公开(公告)日：2017-06-08

申请号：US15124264

申请日：2015-03-09

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SUZHOU VIGONVITA LIFE SCIENCES CO., LTD. ,  TOPHARMAN SHANDONG CO., LTD.

Inventor： Hualiang JIANG ,  Zhen WANG ,  Jianfeng LI ,  Rongxia ZHANG ,  Yang HE ,  Yongjian LIU ,  Minghao BI ,  Zheng LIU ,  Guanghui TIAN ,  Weiming CHEN ,  Feipu YANG ,  Chunhui WU ,  Yu WANG ,  Xiangrui JIANG ,  Jingjing YIN ,  Guan WANG ,  Jingshan SHEN

IPC: C07D409/12 ,  C07D495/04 ,  C07D471/04

CPC classification number: C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

Abstract: The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.

公开(公告)号：US09376410B2

公开(公告)日：2016-06-28

申请号：US14434563

申请日：2013-10-10

Applicant: TOPHARMAN SHANGHAI CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA , CHINESE ACADEMY OF SCIENCES ,  TOPHARMAN SHANDONG CO., LTD.

Inventor： Guan Wang ,  Xiangrui Jiang ,  Xudong Gong ,  Weiming Chen ,  Fuqiang Zhu ,  Rongxia Zhang ,  Xianguo Zhao

IPC: C07D307/00 ,  C07D307/33 ,  C07D413/12

CPC classification number: C07D307/33 ,  C07D413/12

Abstract: This invention disclose (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone in a single configuration and preparation method and use thereof. The (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone, or a pharmaceutically acceptable salt, an ester, a prodrug or a solvate thereof according to the invention are important intermediates of a variety of anti-viral and anti-tumor active ingredients. A compound obtained from (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone via an acylation reaction can be directly used for preparing various anti-viral and anti-tumor drugs. The Chiral synthesis method and the spontaneous resolution method of the compound of (2R)-2-deoxy-2,2-disubstituted-ribono-1,4-lactone according to the invention have the following advantages: the reaction routes are short and simple with high yield and low cost, which are suitable for industrial application.

Abstract translation: 本发明公开了单一构型的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯及其制备方法和用途。 根据本发明的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯或其药学上可接受的盐，酯，前药或溶剂化物是各种抗 - 病毒和抗肿瘤活性成分。 通过酰化反应从（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯获得的化合物可以直接用于制备各种抗病毒和抗肿瘤药物。 根据本发明的（2R）-2-脱氧-2,2-二取代 - 内酰基-1,4-内酯化合物的手性合成方法和自发拆分方法具有以下优点：反应路线短而简单 产量高，成本低，适合工业应用。