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公开(公告)号：EP4112054A1
公开(公告)日：2023-01-04
申请号：EP21760664.9
申请日：2021-02-26
申请人： Shanghai Runshi Medical Technology Co., Ltd , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： ZHANG, Ao , GENG, Meiyu , AI, Jing , WANG, Caixia , PENG, Xia , ZHANG, Yang , DING, Jian
IPC分类号： A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/5377 , A61K31/506 , A61K31/4433 , C07D401/12 , C07D213/75 , C07D413/12 , C07D417/12 , C07D403/12 , C07D405/12 , A61P35/00
摘要： Use of a compound of general formula (A) which is a CFS-1R kinase inhibitor or a pharmaceutically acceptable salt thereof in the preparation of medicaments for treating diseases related to CSF-1R kinase signal transduction pathway or medicaments for regulating immunization. In vivo and in vitro studies show that the compound can significantly inhibit CSF-1R kinase activity; significantly inhibits the proliferation of a CSF-1/CSF-1R-driven mouse myeloid leukemia cell line, inhibits the survival of macrophages induced by CSF-1 and reverses M2 polarization phenotype of macrophages, and has an effect superior to that of the marketed medicament Pexidartinib. In a TAM enriched tumor model (MC38 model), the compound significantly antagonizes the tumor immunosuppressive microenvironment and exhibits significant anti-tumor efficacy. The compound has inhibitory effects on tumors that are not sensitive to immune checkpoint drugs, and can enhance the efficacy of immune checkpoint drugs, and has good clinical application prospects.
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公开(公告)号：EP3985007A1
公开(公告)日：2022-04-20
申请号：EP20823330.4
申请日：2020-06-12
发明人： ZHANG, Ao , MIAO, Zehong , XIONG, Chaodong , SONG, Shanshan , HE, Jinxue
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00 , A61P35/02
摘要： The present disclosure relates to triazolopyrimidine compounds and salts, compositions and uses thereof, and the triazolopyrimidine compounds have the structures represented by the formula (I):
the above-mentioned triazolopyrimidine compounds have good activity and high selectivity for NAE.-
3.发明授权
公开(公告)号：EP3546460B1
公开(公告)日：2020-07-08
申请号：EP17874613.7
申请日：2017-11-24
发明人： ZHANG, Ao , DING, Jian , XIE, Hua , SONG, Zilan , XUE, Yu , TONG, Linjiang , GENG, Meiyu
IPC分类号： C07D471/14 , C07D487/14 , A61K31/519 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/02
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公开(公告)号：EP3299014B1
公开(公告)日：2019-11-20
申请号：EP16795854.5
申请日：2016-05-13
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai Acebright Pharmaceuticals Co. Ltd.
发明人： GUO, Shiyan , GAN, Yong , ZHANG, Ao , MIAO, Zehong , GAO, Li , DING, Jian
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5.发明公开
公开(公告)号：EP3418277A1
公开(公告)日：2018-12-26
申请号：EP17752701.7
申请日：2017-02-17
发明人： ZHANG, Ao , GENG, Meiyu , XING, Li , AI, Jing , SONG, Zilan , PENG, Xia , GU, Wangting , DING, Jian
IPC分类号： C07D401/12 , C07D213/75 , C07D413/12 , C07D417/12 , C07D403/12 , C07D405/12 , A61K31/4427 , A61K31/44 , A61K31/4439 , A61K31/4545 , A61P35/00
CPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/4545 , C07D213/75 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.
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6.发明公开PIPERAZINOTRIZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF IN DRUG PREPARATION 审中-公开PIPERAZINOTRIZOLVERBINDUNG，生产方法和它们用于药品的生产
公开(公告)号：EP2881395A1
公开(公告)日：2015-06-10
申请号：EP13825341.4
申请日：2013-07-24
发明人： ZHANG, Ao , MIAO, Zehong , YE, Na , HUAN, Xiajuan , SONG, Zilan , CHEN, Chuanhuizi , CHEN, Yi , DING, Jian
IPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/502 , A61P9/10 , A61P25/28 , A61P35/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/502
摘要： Provided is a piperazinotriazole compound represented by general formula I or an isomer, a pharmaceutically acceptable salt, ester, prodrug or hydrate thereof. Also provided are a method for preparing the compound, a drug composition containing the compound, and a use thereof as a high-selectivity poly(ADP-ribose)polymerase-1 (PARP 1) inhibitor in the preparation of drugs for the prevention and / or treatment of PARP-related diseases.
摘要翻译： 本发明提供一种由通式表示的异构体，药学上可接受的盐，酯，前药或水合物的I或其化合物piperazinotriazole。 这样提供了用于制备所述化合物，药物组合物含有该化合物，并且作为高选择性的聚（ADP-核糖）在制备药物用于预防聚合酶-1（PARP 1）抑制剂及其使用的方法和/ 或治疗的PARP有关的疾病。
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7.发明公开
公开(公告)号：EP3960743A1
公开(公告)日：2022-03-02
申请号：EP20794381.2
申请日：2020-04-24
发明人： ZHANG, Ao , DING, Jian , XIE, Hua , SONG, Zilan , XUE, Yu , XING, Li , TONG, Linjiang , GENG, Meiyu
IPC分类号： C07D471/14 , C07D487/14 , A61K31/519 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/02
摘要： The present invention relates to a pyrimido[5,4-b]pyrrolizin compound represented by general formula I, an optical isomer thereof, a preparation method therefor, a pharmaceutical composition containing same, and a use thereof. The compound according to the present invention has good inhibitory activity on the kinase BTK at both the molecular level and the cellular level. Meanwhile, the compound also has good anti-tumor activity and pharmacokinetic properties in vivo.
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8.发明公开
公开(公告)号：EP3381919A1
公开(公告)日：2018-10-03
申请号：EP16867946.2
申请日：2016-11-22
发明人： ZHANG, Ao , MIAO, Zehong , WANG, Pingyuan , SONG, Shanshan , SONG, Zilan , HUAN, Xiajuan , FAN, Zhoulong , DING, Jian
IPC分类号： C07D487/04 , C07D471/04 , A61K31/502 , A61K31/437 , A61K31/444 , A61P25/28 , A61P25/16 , A61P9/10 , A61P27/02 , A61P35/00
CPC分类号： C07D487/04 , A61K31/437 , A61K31/444 , A61K31/502 , A61P35/00 , C07D471/04
摘要： The present invention relates to a class of substituted triazolopiperazine compounds represented by formula ( I ), tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers.
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9.发明公开SOMCL-9112 SOLID DISPERSION AND PREPARATION METHOD THEREOF AND SOMCL-9112 SOLID PREPARATION CONTAINING SOMCL-9112 SOLID DISPERSION 审中-公开SOMCL-9112固体分散体及其制备方法和含有SOMCL-9112固体分散体的SOMCL-9112固体制剂
公开(公告)号：EP3299014A1
公开(公告)日：2018-03-28
申请号：EP16795854.5
申请日：2016-05-13
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai Acebright Pharmaceuticals Co. Ltd.
发明人： GUO, Shiyan , GAN, Yong , ZHANG, Ao , MIAO, Zehong , GAO, Li , DING, Jian
IPC分类号： A61K9/28 , A61K9/48 , A61K31/502 , A61K47/32 , A61K47/38 , A61K47/40 , A61K47/34 , A61P35/00
摘要： Disclosed is an SOMCL-9112 solid dispersion. The SOMCL-9112 solid dispersion is characterized by being prepared from the following raw materials in percentage by weight: 5 percent to 60 percent of SOMCL-9112, 5 percent to 90 percent of pharmaceutically acceptable matrix polymer, 0 percent to 20 percent of surfactant, 0 percent to 20 percent of flow aid and 0 percent to 20 percent of plasticizer. Also disclosed are a preparation method of the SOMCL-9112 solid dispersion, a solid medicinal preparation containing the solid dispersion and application of the solid dispersion for preparing a medicine for treating cancer.
摘要翻译： 公开了一种SOMCL-9112固体分散体。 SOMCL-9112固体分散体的特征是由以下重量百分比的原料制备而成：SOMCL-9112 5％-60％，药用基质聚合物5％-90％，表面活性剂0％-20％ 0％至20％的助流剂和0％至20％的增塑剂。 本发明还公开了SOMCL-9112固体分散体的制备方法，包含该固体分散体的固体药物制剂和该固体分散体在制备用于治疗癌症的药物中的应用。
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10.发明公开
公开(公告)号：EP3907221A1
公开(公告)日：2021-11-10
申请号：EP19907455.0
申请日：2019-12-31
发明人： ZHANG, Ao , GENG, Meiyu , DING, Chunyong , XIE, Zuoquan , DING, Jian , ZHANG, Yan , SHEN, Ancheng , WANG, Xiyuan
IPC分类号： C07D333/60 , C07D333/58 , C07D333/56 , C07D409/12 , A61K31/381 , A61P35/00
摘要： The present invention relates to fluorine-containing substituted benzothiophene compound, and a pharmaceutical composition and an application thereof. Specifically, the compound of the present invention has the structure as shown in formula I, wherein the definitions of each group and substituent are as described in the description. The present invention further discloses a preparation method of the compound and an anti-tumor application thereof.
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