公开(公告)号：US20200231623A1

公开(公告)日：2020-07-23

申请号：US16648123

申请日：2018-09-17

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Fajun NAN ,  Xin XIE ,  Chenlu ZHANG ,  Shimeng GUO ,  Yangming ZHANG ,  Siwei WANG

IPC分类号： C07J63/00

摘要： Disclosed are a pentacyclic triterpene compound as shown in general formula (I) and a preparation method therefor. The compound has an effective antagonistic effect on FXR receptors.

公开(公告)号：US20200010492A1

公开(公告)日：2020-01-09

申请号：US16490837

申请日：2016-02-28

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Fajun NAN ,  Xin XIE ,  Linhai CHEN ,  Qing ZHANG ,  Yufeng XIAO ,  Hui YANG

IPC分类号： C07F9/09 ,  C07F9/6561 ,  C07F9/6553 ,  C07F9/655

摘要： The present invention relates to a GPR84 receptor antagonist and use thereof. The GPR84 receptor antagonist of the present invention has a structure as represented by formula (I), the definitions of R1, R2, R3, R4, L1, L2, L3, L4, L5, L6, Y, Z, and rings A, B, C, and D are as described in the description and claims. The GPR84 receptor antagonist of the present invention can competitively inhibit the activation of the receptor caused by an agonist of GPR84, and can be used in the preparation of a medicament for treating related diseases caused by high expression or high excitability of GPR84 receptor, the diseases including multiple sclerosis, inflammatory bowel disease, arthritis and the like.

公开(公告)号：US20150210711A1

公开(公告)日：2015-07-30

申请号：US14683726

申请日：2015-04-10

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Xin XIE ,  Xuechu ZHEN ,  Haifeng SUN ,  Jing LI ,  Liyuan ZHU ,  Zeng LI ,  Ying CHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC分类号： C07D491/153 ,  C07D491/056 ,  C07D217/20 ,  C07D311/20 ,  C07C231/14 ,  C07D455/03 ,  C07C69/736

CPC分类号： C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

摘要： The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

摘要翻译： 本发明涉及由通式（I）表示的新型六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋及其混合物，以及其药学上可接受的盐。 本发明还涉及一种制备该化合物的方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关的疾病具有良好的预防和治疗作用。 生物活性实验表明，该化合物预计将发展成为一种新颖有力的化学实体，用于治疗与多巴胺受体和5-羟色胺受体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等有关的疾病。

公开(公告)号：US20160193195A1

公开(公告)日：2016-07-07

申请号：US14888797

申请日：2014-05-04

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Xin XIE ,  Haifeng SUN ,  Jing LI ,  Fei ZHAO ,  Ying CHEN ,  Zeng LI ,  Yu ZHOU ,  Hualiang JIANG ,  Kaixian CHEN

IPC分类号： A61K31/4375

CPC分类号： A61K31/4375

摘要： Use of hexahydro-dibenzo[a,g]quinolizine compounds as shown in formula(I) in preparing a medicine for treating and/or preventing benign prostate hyperplasia diseases.

摘要翻译： 式（I）所示的六氢 - 二苯并[a，g]喹嗪化合物在制备治疗和/或预防良性前列腺增生疾病的药物中的用途。

公开(公告)号：US20140088130A1

公开(公告)日：2014-03-27

申请号：US14091979

申请日：2013-11-27

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： Hong LIU ,  Xin XIE ,  Xuechu ZHEN ,  Haifeng SUN ,  Jing LI ,  Liyuan ZHU ,  Zeng LI ,  Ying CHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC分类号： C07D491/147 ,  C07D491/22 ,  C07D455/03

CPC分类号： C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

摘要： The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

摘要翻译： 本发明涉及由通式（I）表示的新型六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋及其混合物，以及其药学上可接受的盐。 本发明还涉及一种制备该化合物的方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关的疾病具有良好的预防和治疗作用。 生物活性实验表明，该化合物预计将发展成为一种新颖有力的化学实体，用于治疗与多巴胺受体和5-羟色胺受体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等有关的疾病。

公开(公告)号：US20180237399A1

公开(公告)日：2018-08-23

申请号：US15772105

申请日：2016-11-01

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Fajun NAN ,  Xin XIE ,  Yang LIU ,  Qing ZHANG ,  Linhai CHEN ,  Hui YANG

IPC分类号： C07D239/60 ,  C07D239/52 ,  C07D213/69 ,  C07C49/825 ,  C07C39/19

CPC分类号： C07D239/60 ,  A61K31/505 ,  C07C39/08 ,  C07C39/19 ,  C07C49/825 ,  C07D213/69 ,  C07D239/48 ,  C07D239/52 ,  C07D239/54 ,  C07D239/545 ,  C07D239/56 ,  C07D251/20 ,  C07D309/38

摘要： The present invention relates to a class of compounds represented by the formula I, or pharmaceutically acceptable salts thereof, methods for their preparation, and application as small molecule tools that function as GPR84 agonists, and their use in preparing a medicament for the treatment of septicemia.

公开(公告)号：US20170044187A1

公开(公告)日：2017-02-16

申请号：US15109101

申请日：2014-12-29

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong LIU ,  Beili WU ,  Yongtang ZHENG ,  Xin XIE ,  Hualiang JIANG ,  Panfeng PENG ,  Ronghua LUO ,  Jing LI ,  Jian LI ,  Ya ZHU ,  Ying CHEN ,  Haonan ZHANG ,  Liumeng YANG ,  Yu ZHOU ,  Kaixian CHEN

IPC分类号： C07D519/00 ,  C07D451/04 ,  C07D401/14 ,  C07D409/14

CPC分类号： C07D519/00 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  C07D451/04 ,  A61K2300/00

摘要： Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

摘要翻译： 提供由式（I）表示的1-（3-氨基丙基）取代的环胺化合物，其药学上可接受的盐，对映体，非对映异构体，外消旋体及其混合物，以及合成所述1-（3-氨基丙基）取代的环胺 化合物采用芳香族杂环甲醛为原料。 所述化合物可用作治疗HIV感染的CCR5拮抗剂。

公开(公告)号：US20170044119A1

公开(公告)日：2017-02-16

申请号：US15301763

申请日：2015-03-27

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Fajun NAN ,  Jia LI ,  Xin XIE ,  Chaojun GONG ,  Yubo ZHOU ,  Hui CHAI ,  Yangming ZHANG ,  Mingbo SU

IPC分类号： C07D277/56 ,  C07D417/14 ,  C07D277/60

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： 本发明涉及一种噻唑类化合物及其制备方法及其应用。 更具体地说，本发明涉及2,2'-双噻唑类化合物及其制备方法，以及使用组氨酸脱乙酰酶抑制剂的2,2'-双噻唑类化合物制备 抗肿瘤药物，用于治疗自身免疫性疾病的药物，用于治疗II型糖尿病的药物及其并发症，或用于治疗神经变性疾病的药物。