公开(公告)号：US20150210711A1

公开(公告)日：2015-07-30

申请号：US14683726

申请日：2015-04-10

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

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

Abstract: 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.

Abstract translation: 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：US20200157110A1

公开(公告)日：2020-05-21

申请号：US16626254

申请日：2018-06-22

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Chunhao YANG ,  Linghua MENG ,  Haoyue XIANG ,  Jing LI ,  Xi ZHANG ,  Xiang WANG ,  Cun TAN ,  Qian HE ,  Jian DING ,  Yi CHEN

IPC: C07D487/04 ,  C07D519/00

Abstract: The present disclosure relates to 7-substituted pyrrolo[2,1-f][1,2,4]triazine compounds or pharmaceutically acceptable salts thereof, and preparation methods and uses thereof. These compounds show good PI3K inhibitory activity, can effectively inhibit the activity of PI3K kinase, and has significant enhancement and improvement of pharmacokinetic properties, such as bioavailability, due to the introduction of the 7-position group; furthermore, the compounds of the present disclosure exhibit an unpredictable high selectivity and strong inhibitory activity on PI3Kδ, and thus these compounds can be used for treating diseases related to PI3K pathway, especially for anti-cancer or for the treatment of tumors, leukemias and autoimmune diseases. After further optimizing and screening, the compounds are expected to be developed into a new type of anti-tumor drugs.

公开(公告)号：US20160193195A1

公开(公告)日：2016-07-07

申请号：US14888797

申请日：2014-05-04

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC: A61K31/4375

CPC classification number: A61K31/4375

Abstract: 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.

Abstract translation: 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

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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

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

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

Abstract: 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.

Abstract translation: 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：US20170044187A1

公开(公告)日：2017-02-16

申请号：US15109101

申请日：2014-12-29

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： 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: C07D519/00 ,  C07D451/04 ,  C07D401/14 ,  C07D409/14

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

Abstract: 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.

Abstract translation: 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。