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：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

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：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：EP3059237A1

公开(公告)日：2016-08-24

申请号：EP14854084.2

申请日：2014-10-20

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

发明人： LIU, Zheng ,  WU, Chunhui ,  LIU, Yongjian ,  ZHANG, Rongxia ,  HE, Yang ,  TIAN, Guanghui ,  SHEN, Jingshan

IPC分类号： C07D409/12 ,  C07D333/70

CPC分类号： C07D409/12 ,  C07D333/54 ,  C07D333/70

摘要： The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.

摘要翻译： 本发明涉及一种用于制备brexpiprazole，所述类似物，关键中间体的方法，以及它们的盐，具体地，本发明涉及一种新的方法用于制备brexpiprazole，所述类似物，关键的中间体，以及它们的盐，以及关键中间体， 和盐在制备过程中它们提供。 该制备方法具有反应条件温和，稳定的中间，容易操作，并且使用便宜和容易获得的试剂，从而节省了合成成本，缩短生产周期，提高产量和产品质量，并且是适合于大规模 生产。

公开(公告)号：EP3192792A1

公开(公告)日：2017-07-19

申请号：EP15840920.1

申请日：2015-09-11

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

发明人： SHEN, Jingshan ,  LIU, Zheng ,  WANG, Zhen ,  TIAN, Guanghui ,  LI, Jianfeng ,  YANG, Xiaojun

IPC分类号： C07D261/20 ,  C07D307/77 ,  C07D209/14 ,  A61K31/381 ,  A61K31/33 ,  A61P25/08

CPC分类号： C07D495/04 ,  A61K31/33 ,  A61K31/381 ,  A61K31/415 ,  A61K31/42 ,  A61K31/425 ,  C07D209/14 ,  C07D231/56 ,  C07D261/20 ,  C07D275/04 ,  C07D307/77 ,  C07D333/20 ,  C07D333/46

摘要： Disclosed are an aminosulfonyl compound represented by general formula I or a tautomer, enantiomer, racemate or pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition and a use thereof. The compound can be used for treating epilepsy, convulsion, obesity and the like.

摘要翻译： 公开了由通式I表示的氨基磺酰基化合物或其互变异构体，对映异构体，外消旋体或药学上可接受的盐，其制备方法，药物组合物及其用途。 该化合物可用于治疗癫痫，惊厥，肥胖症等。

公开(公告)号：EP3812384A1

公开(公告)日：2021-04-28

申请号：EP19822932.0

申请日：2019-06-21

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

发明人： SHEN, Jingshan ,  HE, Yang ,  WANG, Zhen ,  LI, Jianfeng ,  LIU, Yongjian ,  SUO, Jin ,  TIAN, Guanghui ,  CHEN, Weiming ,  YANG, Feipu ,  WANG, Yu ,  JIANG, Xiangrui ,  ZHANG, Rongxia ,  JIANG, Hualiang

IPC分类号： C07D409/14 ,  C07D409/12

摘要： The present invention relates to a maleate salt of a benzothiophene compound, a crystalline form and use thereof. Specifically, the present invention relates to a compound of formula (I-A), a crystalline form A, a preparation method thereof and a pharmaceutical composition comprising the same, and a use thereof in the preparation of drugs for preventing or treating the central nervous system diseases. The compound of formula (I-A) and the crystalline form A thereof in the present invention have excellent physical and chemical properties, high oral bioavailability, and the best comprehensive properties for preparing into drugs and they are more suitable for making pharmaceutical preparations and more suitable for storage.

公开(公告)号：EP1961753A1

公开(公告)日：2008-08-27

申请号：EP06817839.1

申请日：2006-11-16

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

发明人： TIAN, Guanghui ,  LAI, Shunan ,  WANG, Zhen ,  ZHU, Yi ,  CHEN, Xinjian ,  JI, Yurong ,  ZHANG, Jinfeng ,  JIN, Weixi ,  LV, Heping ,  LIU, Jinping ,  WANG, Wei ,  JI, Ruyun ,  SHEN, Jingshan

IPC分类号： C07D487/04 ,  A61K31/519 ,  C07D239/00 ,  C07D231/00

CPC分类号： C07D487/04

摘要： The invention discloses a series of pyrazolopyrimidinone derivatives, which have the following chemical structure, their preparation methods and use,

It has been proved by pharmacological experiment that the said pyrazolopyrimidinone derivatives have high inhibitory activity against PDE5, and parts of them have a much stronger potency against PDE5 than against PDE6. Most of the compounds show low toxicity. The pyrazolopyrimidinone derivatives can be used in clinics for the palliative or curative treatment of symptoms or diseases relating to cardiovascular system, urinary system, especially for the palliative or curative treatment of erectile dysfunction.

摘要翻译： 本发明公开了一系列具有以下化学结构的吡唑并嘧啶酮衍生物及其制备方法和应用，已经通过药理实验证明，所述吡唑并嘧啶酮衍生物对PDE5具有高抑制活性，其部分药效更强 反对PDE5而不是PDE6。 大多数化合物显示低毒性。 吡唑并嘧啶酮衍生物可用于临床上用于缓解或治疗与心血管系统，泌尿系统有关的症状或疾病，特别是对于勃起功能障碍的姑息治疗或治疗性治疗。

公开(公告)号：EP4234557A1

公开(公告)日：2023-08-30

申请号：EP21885029.5

申请日：2021-10-21

申请人： Vigonvita Life Sciences Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Wuhan Institute Of Virology, Chinese Academy of Sciences

发明人： SHEN, Jingshan ,  XIE, Yuanchao ,  ZHANG, Leike ,  XIAO, Gengfu ,  WANG, Zhen ,  JIANG, Hualiang ,  XU, Huaqiang ,  HU, Tianwen ,  TIAN, Guanghui

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P31/14

摘要： The present disclosure pertains to the technical field of medicine, and relates to salt of nucleoside analog, and crystal form, pharmaceutical composition and use thereof. Specifically, the salt of nucleoside analog has a structure shown in formula I, wherein X is hydrogen or deuterium; Y is an acid, preferably hydrogen bromide, hydrogen chloride, nitric acid, methanesulfonic acid or maleic acid, n is 0.5 to 2, preferably 1. When X is hydrogen or deuterium, Y is hydrogen bromide, and n is 1, the salt of the nucleoside analog exists in the form of a crystal with crystal form I or crystal form A or exists in an amorphous form, which has good appearance as solid material, high stability, good solubility, low hygroscopicity, etc., and can be used in the preparation of medicaments for the treatment and/or alleviation of related diseases caused by viruses (especially SARS-CoV-2).