公开(公告)号：EP3115361A4

公开(公告)日：2017-04-26

申请号：EP15757771

申请日：2015-03-09

申请人： SHANGHAI INST MATERIA MEDICA CAS ,  SUZHOU VIGONVITA LIFE SCIENCES CO LTD ,  TOPHARMAN SHANDONG CO LTD

发明人： JIANG HUALIANG ,  WANG ZHEN ,  LI JIANFENG ,  ZHANG RONGXIA ,  HE YANG ,  LIU YONGJIAN ,  BI MINGHAO ,  LIU ZHENG ,  TIAN GUANGHUI ,  CHEN WEIMING ,  YANG FEIPU ,  WU CHUNHUI ,  WANG YU ,  JIANG XIANGRUI ,  YIN JINGJING ,  WANG GUAN ,  SHEN JINGSHAN

IPC分类号： C07D409/12 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/517 ,  A61K31/519 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

摘要： Provided are heterocyclic compounds represented by formula (I), stereoisomers or pharmaceutically acceptable salts of said compounds, a pharmaceutical composition of said compounds, and an application of said compounds in the preparation of a drug for the prevention and/or treatment of a central nervous system disease.

摘要翻译： 提供由式（I）表示的杂环化合物，所述化合物的立体异构体或药学上可接受的盐，所述化合物的药物组合物，以及所述化合物在制备用于预防和/或治疗中枢神经系统 系统疾病。

公开(公告)号：EP2746284A4

公开(公告)日：2015-01-14

申请号：EP12823704

申请日：2012-08-14

申请人： TOPHARMAN SHANGHAI CO LTD ,  SHANGHAI INST MATERIA MEDICA ,  TOPHARMAN SHANDONG CO LTD

发明人： LI JIANFENG ,  TIAN GUANGHUI ,  WANG ZHEN ,  SUO JIN ,  JIANG XIANGRUI ,  LIU ZHENG ,  YANG XIAOJUN ,  XIE ZHU ,  ZHAO XIANGUO ,  ZHU WEILIANG ,  JIANG HUALIANG ,  SHEN JINGSHAN

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P1/00 ,  A61P9/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/00 ,  A61P13/08 ,  A61P13/10 ,  A61P13/12 ,  A61P15/00 ,  A61P15/06 ,  A61P15/10 ,  A61P25/00 ,  A61P27/06 ,  A61P29/00 ,  A61P37/08

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.

公开(公告)号：EP2383262A1

公开(公告)日：2011-11-02

申请号：EP09831388.5

申请日：2009-12-10

申请人： Topharman Shanghai Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Topharman Shandong Co., Ltd.

发明人： LIU, Zheng ,  LI, Jianfeng ,  YANG, Xiaojun ,  WANG, Zhen ,  ZHANG, Jinfeng ,  ZHU, Yi ,  TIAN, Guanghui ,  JIN, Qing ,  SHEN, Jingkang ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D239/36 ,  A61K31/505 ,  A61P15/10

CPC分类号： A61K31/505 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07H15/26

摘要： The present invention relates to a class of phenylpyrimidone compounds, the pharmaceutical composition, the preparation method and the use thereof. More specifically, the present invention relates to a type of phenylpyrimidone compounds of the following formula I, the pharmaceutically acceptable salts or solvates thereof; and to the pharmaceutical composition as well as the preparation method of the said compounds. The said compounds of formula I according to the present invention can effectively inhibit type V phosphodiesterase (PDE5), and thus can be used for the treatment of various vascular disorders, such as male erectile dysfunction, pulmonary hypertension and the like.

摘要翻译： 本发明涉及一类苯基嘧啶酮化合物，药物组合物，其制备方法及用途。 更具体地，本发明涉及一种下式I的苯基嘧啶酮化合物，其药学上可接受的盐或溶剂合物; 和药物组合物以及所述化合物的制备方法。 所述根据本发明的式I化合物可有效抑制V型磷酸二酯酶（PDE5），因此可用于治疗各种血管疾病，如男性勃起功能障碍，肺动脉高压等。

公开(公告)号：EP3115361A1

公开(公告)日：2017-01-11

申请号：EP15757771.9

申请日：2015-03-09

申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences ,  Suzhou Vigonvita Life Sciences Co., Ltd. ,  Topharman Shandong Co., Ltd.

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

IPC分类号： C07D409/12 ,  C07D471/04 ,  C07D409/14 ,  C07D519/00 ,  C07D495/04 ,  C07D417/12 ,  C07D413/12 ,  A61K31/496 ,  A61K31/519 ,  A61K31/4709 ,  A61K31/517 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/55 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22

CPC分类号： C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00

摘要： Provided are heterocyclic compounds represented by formula (I), stereoisomers or pharmaceutically acceptable salts of said compounds, a pharmaceutical composition of said compounds, and an application of said compounds in the preparation of a drug for the prevention and/or treatment of a central nervous system disease.

公开(公告)号：EP2746284A1

公开(公告)日：2014-06-25

申请号：EP12823704.7

申请日：2012-08-14

申请人： Topharman Shanghai Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Topharman Shandong Co., Ltd.

发明人： LI, Jianfeng ,  TIAN, Guanghui ,  WANG, Zhen ,  SUO, Jin ,  JIANG, Xiangrui ,  LIU, Zheng ,  YANG, Xiaojun ,  XIE, Zhu ,  ZHAO, Xianguo ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P15/10 ,  A61P9/12 ,  A61P15/00 ,  A61P15/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/00 ,  A61P9/10 ,  A61P9/04 ,  A61P13/12 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06 ,  A61P11/02 ,  A61P37/08 ,  A61P27/06 ,  A61P1/00 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.

摘要翻译： 本发明涉及由式（I），和药学上可接受的多晶型物，溶剂化物，水合物，脱水物，共结晶，无水，或其无定形形式，所述药物组合物和药物单位剂量形式含在代表pyrazolopyrimidinones的新的盐 同样，worin X darstellt有机或无机酸，马来酸优选，琥珀酸，甲磺酸，盐酸，等等。本发明还涉及pyrazolopyrimidinones和含有相同的药物组合物的化合物的共结晶或络合物。 因此，本发明涉及一种用于制备，使用其和含有盐或结晶形式的药物制剂。

公开(公告)号：EP2383262A4

公开(公告)日：2012-10-31

申请号：EP09831388

申请日：2009-12-10

申请人： TOPHARMAN SHANGHAI CO LTD ,  SHANGHAI INST MATERIA MEDICA ,  TOPHARMAN SHANDONG CO LTD

发明人： LIU ZHENG ,  LI JIANFENG ,  YANG XIAOJUN ,  WANG ZHEN ,  ZHANG JINFENG ,  ZHU YI ,  TIAN GUANGHUI ,  JIN QING ,  SHEN JINGKANG ,  ZHU WEILIANG ,  JIANG HUALIANG ,  SHEN JINGSHAN

IPC分类号： C07D239/36 ,  A61K31/505 ,  A61P15/10

CPC分类号： A61K31/505 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07H15/26

公开(公告)号：EP2746284B1

公开(公告)日：2017-04-12

申请号：EP12823704.7

申请日：2012-08-14

申请人： Topharman Shanghai Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Topharman Shandong Co., Ltd.

发明人： LI, Jianfeng ,  TIAN, Guanghui ,  WANG, Zhen ,  SUO, Jin ,  JIANG, Xiangrui ,  LIU, Zheng ,  YANG, Xiaojun ,  XIE, Zhu ,  ZHAO, Xianguo ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P15/10 ,  A61P9/12 ,  A61P15/00 ,  A61P15/06 ,  A61P13/08 ,  A61P13/10 ,  A61P13/00 ,  A61P9/10 ,  A61P9/04 ,  A61P13/12 ,  A61P29/00 ,  A61P11/00 ,  A61P11/06 ,  A61P11/02 ,  A61P37/08 ,  A61P27/06 ,  A61P1/00 ,  A61P9/00 ,  A61P25/00

CPC分类号： C07D487/04 ,  C07B2200/13

摘要： The present invention relates to new salts of pyrazolopyrimidinone represented by formula (I), and pharmaceutically acceptable polymorph, solvate, hydrate, dehydrate, co-crystallization, anhydrous, or amorphous form thereof, the pharmaceutical compositions, and a pharmaceutical unit dosage form containing the same, wherein x represents organic or inorganic acids, preferable maleic acid, succinic acid, methanesulfonic acid, hydrochloric acid, etc. The invention further relates to co-crystals or complexes of compounds of pyrazolopyrimidinone and pharmaceutical compositions containing the same. The present invention also relates to a process for the preparation, use thereof and pharmaceutical preparation containing the salts or crystalline forms.

公开(公告)号：EP2383262B1

公开(公告)日：2016-07-06

申请号：EP09831388.5

申请日：2009-12-10

申请人： Topharman Shanghai Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Topharman Shandong Co., Ltd.

发明人： LIU, Zheng ,  LI, Jianfeng ,  YANG, Xiaojun ,  WANG, Zhen ,  ZHANG, Jinfeng ,  ZHU, Yi ,  TIAN, Guanghui ,  JIN, Qing ,  SHEN, Jingkang ,  ZHU, Weiliang ,  JIANG, Hualiang ,  SHEN, Jingshan

IPC分类号： C07D239/36 ,  A61K31/505 ,  A61P15/10

CPC分类号： A61K31/505 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07H15/26