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公开(公告)号：EP4342892A1
公开(公告)日：2024-03-27
申请号：EP22832202.0
申请日：2022-06-30
申请人： Hangzhou Healzen Therapeutics Co., Ltd. , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： ZHOU, Xinglu , LI, Jia , LIU, Xingguo , ZHOU, Yubo , HU, Miao , LUO, Xiaomin , XIE, Jiangfeng , KAN, Weijuan , SU, Mingbo , WU, Yizhe
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , A61P35/00 , A61K31/4427
摘要： Disclosed are a Bruton's tyrosine kinase and a mutant degrader thereof, or a stereoisomer thereof, or a stereoisomer mixture thereof or a pharmaceutically acceptable salt thereof, and an application thereof in the preparation of a drug for treating diseases, disorders or conditions that would benefit from the degradation of the Bruton's tyrosine kinase and the mutant thereof. The compound of the present invention can degrade BTK protein, can degrade BTKC481S protein, has an anti-proliferation inhibiting effect on tumor cell strains Mino and OCI-LY10, shows good anti-tumor activity in an OCI-LY10 subcutaneous transplantation tumor model, has an inhibiting effect on B cell activation, and can be applied to B cell or plasma cell proliferative diseases and autoimmune diseases. The compound of the present invention has good oral absorption properties, and can be applied to oral treatment of human or animal B cell or plasma cell proliferative diseases and autoimmune diseases.
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公开(公告)号：EP4434980A1
公开(公告)日：2024-09-25
申请号：EP22895006.9
申请日：2022-11-22
申请人： Hangzhou HealZen Therapeutics Co., Ltd. , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： ZHOU, Xinglu , LI, Jia , LIU, Xingguo , ZHOU, Yubo , HU, Miao , LUO, Xiaomin , XIE, Jiangfeng , KAN, Weijuan , WU, Yizhe , HU, Xiaobei , SU, Mingbo
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , A61K31/497 , A61K31/5377 , A61K31/4427 , A61P35/00 , A61P37/00
CPC分类号： A61K31/4427 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , A61K31/5377 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , C07D401/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
摘要： Disclosed in the present invention are a Bruton's tyrosine kinase degrading agent, which has a structure represented by general formula 1, or a stereoisomer, a mixture of stereoisomers, or a pharmaceutically acceptable salt and a prodrug thereof, Further disclosed are the uses of the compound and a pharmaceutical composition containing same in the preparation of a drug for treating Bruton's tyrosine kinase-related diseases such as B cell or plasma cell proliferative diseases, The compound of the present invention has potent cell proliferation inhibitory activity, effectively degrades Bruton's tyrosine kinase, and has a good liver particle metabolism stability and good oral absorption properties. The compound can be used alone in drugs or in combination with other drugs for treating a disease, disorder or condition that benefits from the inhibition of the Bruton's tyrosine kinase activity or degradation of the Bruton's tyrosine kinase.
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公开(公告)号：EP3127903B1
公开(公告)日：2017-08-23
申请号：EP15774232.1
申请日：2015-03-27
发明人： NAN, Fajun , LI, Jia , XIE, Xin , GONG, Chaojun , ZHOU, Yubo , CHAI, Hui , ZHANG, Yangming , SU, Mingbo
IPC分类号： C07D277/56 , C07D277/60 , C07D417/04 , A61K31/428 , A61K31/427 , A61P37/02 , A61P35/00 , A61P35/02
CPC分类号： C07D277/56 , C07D277/60 , C07D277/66 , C07D417/04 , C07D417/14
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公开(公告)号：EP3257856B1
公开(公告)日：2020-04-08
申请号：EP16748699.2
申请日：2016-02-03
发明人： LIU, Hong , WANG, Jian , LI, Jian , LI, Jia , LI, Jingya , ZHOU, Shengbin , SU, Mingbo , JIANG, Hualiang , LUO, Xiaomin , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10
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公开(公告)号：EP3530657A1
公开(公告)日：2019-08-28
申请号：EP17870509.1
申请日：2017-11-08
发明人： LIU, Tao , LI, Jia , HU, Yongzhou , ZHOU, Yubo , DONG, Xiaowu , GAO, Anhui , SONG, Pinrao , WANG, Peipei , TONG, Lexian , HU, Xiaobei , SU, Mingbo
IPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D409/14 , C07D405/14 , A61K31/506 , A61P35/00
摘要： The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chkl inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chkl kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chkl kinase inhibitory activity, and are promising Chkl inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I:
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公开(公告)号：EP2786998B1
公开(公告)日：2018-07-25
申请号：EP12853993.9
申请日：2012-10-23
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Cisen Pharmaceutical Co., Ltd.
发明人： LIU, Hong , LI, Jia , LI, Jian , LI, Jingya , WANG, Jiang , SU, Mingbo , LIAN, Jie , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61K31/55 , A61P3/10
CPC分类号： C07D495/04
摘要： Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
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7.发明公开THIENYL [3, 2-D]PYRIMIDIN-4-ONE COMPOUNDS, PREPARATION METHOD, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF 有权THIENYL [3，] 2-D PYRIMIDIN-4-ON-VERBINDUNGEN，HERSTELLUNGSVERFAHREN，PHARMAZEUTISCHE ZUSAMMENSETZUNGEN UND IHRE VERWENDUNG
公开(公告)号：EP2786998A1
公开(公告)日：2014-10-08
申请号：EP12853993.9
申请日：2012-10-23
发明人： LIU, Hong , LI, Jia , LI, Jian , LI, Jingya , WANG, Jiang , SU, Mingbo , LIAN, Jie , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61K31/55 , A61P3/10
CPC分类号： C07D495/04
摘要： Disclosed are new thienyl [3, 2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.
摘要翻译： 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 这些化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱发一系列生理作用来治疗II型糖尿病。 因此，这些化合物可以作为治疗糖尿病的新药物开发。
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8.发明公开
公开(公告)号：EP3530656A1
公开(公告)日：2019-08-28
申请号：EP17869906.2
申请日：2017-11-08
发明人： LIU, Tao , LI, Jia , HU, Yongzhou , ZHOU, Yubo , DONG, Xiaowu , GAO, Anhui , SONG, Pinrao , WANG, Peipei , TONG, Lexian , HU, Xiaobei , SU, Mingbo
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
摘要： A 2-substituted aromatic ring-pyrimidine derivative as shown in a general fomula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chkl inhibitors by using N -substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chkl kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chkl kinase inhibitory activity and are promising Chkl inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.
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公开(公告)号：EP3257856A1
公开(公告)日：2017-12-20
申请号：EP16748699.2
申请日：2016-02-03
发明人： LIU, Hong , WANG, Jian , LI, Jian , LI, Jia , LI, Jingya , ZHOU, Shengbin , SU, Mingbo , JIANG, Hualiang , LUO, Xiaomin , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10
摘要： The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.
摘要翻译： 本发明涉及化合物的晶型A. 本发明还公开了晶型A的制备方法和药物组合物。晶型A在体内具有强烈的降血糖活性，并且预期为用于治疗或预防II型糖尿病和/或并发症的新型药物活性成分 II型糖尿病。
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10.发明公开2,2'-TANDEM DITHIAZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF 有权2,2'-二苯并噻唑类化合物及其制备方法及其用途
公开(公告)号：EP3127903A1
公开(公告)日：2017-02-08
申请号：EP15774232.1
申请日：2015-03-27
发明人： NAN, Fajun , LI, Jia , XIE, Xin , GONG, Chaojun , ZHOU, Yubo , CHAI, Hui , ZHANG, Yangming , SU, Mingbo
IPC分类号： C07D277/56 , C07D277/60 , C07D417/04 , A61K31/428 , A61K31/427 , A61P37/02 , A61P35/00 , A61P35/02
CPC分类号： C07D277/56 , C07D277/60 , C07D277/66 , C07D417/04 , C07D417/14
摘要： The present invention relates to a thiazole-based compound, a preparation method therefor, and a use thereof. More specifically, the present invention relates to a 2,2'-bis-thiazole-based compound, a preparation method therefor, and a use of 2,2'-bis-thiazole-based compound a histone deacetylase inhibitor in the preparation of an antitumor medicament, a medicament for treating autoimmune diseases, a medicament for treating type II diabetes mellitus and complication thereof, or a medicament for treating neurodegenerative diseases.
摘要翻译： 噻唑系化合物及其制备方法及其用途技术领域本发明涉及噻唑系化合物及其制备方法及其用途。 更具体地说，本发明涉及2,2'-双噻唑类化合物，其制备方法，以及2,2'-双噻唑类化合物和组蛋白脱乙酰酶抑制剂在制备 抗肿瘤药物，用于治疗自身免疫疾病的药物，用于治疗II型糖尿病及其并发症的药物或用于治疗神经变性疾病的药物。
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