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公开(公告)号：US20170247371A1
公开(公告)日：2017-08-31
申请号：US15326310
申请日：2015-07-14
发明人： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Dakai CHEN , Lina ZHANG , Runtao ZHANG , Zhifu XIE
IPC分类号： C07D471/04 , C12N9/12 , C07D211/78
CPC分类号： C07D471/04 , A61K31/437 , C07D211/78 , C12N9/12 , C12Y207/11031
摘要： Provided are a class of pyrazolone compounds and a use thereof. In particular, a compound represented by formula I is provided, wherein the definition of each variable group is as described in the description. The compounds of formula (I) have a direct AMPK-activating activity and can significantly promote the phosphorylation of AMPK and ACC of L6 myocytes and HepG2 cells in a dose-dependent manner.
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公开(公告)号：US20190039989A1
公开(公告)日：2019-02-07
申请号：US16075528
申请日：2017-02-20
发明人： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Zhifu XIE , Jingtao WANG , Dongdong GUO
CPC分类号： C07C61/35 , A61K31/194 , C07C55/28 , C07C57/13 , C07C57/26 , C07C57/42 , C07C61/16 , C07C61/20 , C07C61/22 , C07C2601/08 , C07C2601/16 , Y02P20/55
摘要： The present invention relates to a class of fatty acid compounds, a preparation method thereof and use thereof. The fatty acid compounds have the structure of the formula I, which has the ability to activate APMK and inhibit the glucose output in mouse primary hepatocytes. The fatty acid compounds can be used in preparing a medicament for the treatment of obesity or diabetes.
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3.发明申请公开(公告)号：US20200231623A1
公开(公告)日：2020-07-23
申请号：US16648123
申请日：2018-09-17
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.
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公开(公告)号：US20200010492A1
公开(公告)日：2020-01-09
申请号：US16490837
申请日：2016-02-28
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.
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公开(公告)号：US20180064696A1
公开(公告)日：2018-03-08
申请号：US15556932
申请日：2016-03-03
发明人： Fajun NAN , Boliang LI , Yang ZHAN , Xiaowei ZHANG , Ying XIONG , Xichan HU , Yangming ZHANG
IPC分类号： A61K31/4433 , A61K31/352 , C07D493/04
CPC分类号： A61K31/4433 , A61K31/352 , C07B37/04 , C07B49/00 , C07D493/04
摘要： The present invention relates to a series of analogues of natural product Pyripyropene A represented by general formula I and a preparation method and use thereof. More particularly, the present invention relates to analogues of the natural product Pyripyropene A, a preparation method and use thereof as the acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors for the treatment of cardiovascular diseases such as atherosclerosis and the like.
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公开(公告)号：US20190211005A1
公开(公告)日：2019-07-11
申请号：US16329336
申请日：2017-08-24
发明人： Fajun NAN , Jia LI , Jian DING , Meiyu GENG , Yangming ZHANG , Yi CHEN , Yubo ZHOU , Chaojun GONG , Mingbo SU , Anhui GAO
IPC分类号： C07D417/04 , A61P35/02
摘要： The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.
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公开(公告)号：US20240351966A1
公开(公告)日：2024-10-24
申请号：US18290268
申请日：2022-05-11
发明人： Fajun NAN , Jingya LI , Zheng ZHANG , Yanan DUAN , Yangming ZHANG , Dandan CHEN , Chengqiu DAI
IPC分类号： C07C39/19 , A61K31/05 , A61K31/09 , A61K31/136 , A61K31/145 , A61K31/167 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/505 , C07C43/215 , C07C43/23 , C07C215/76 , C07C233/88 , C07D213/69 , C07D213/74 , C07D239/10 , C07D307/36 , C07D333/06 , C07D333/34
CPC分类号： C07C39/19 , A61K31/05 , A61K31/09 , A61K31/136 , A61K31/145 , A61K31/167 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/505 , C07C43/215 , C07C43/23 , C07C215/76 , C07C233/88 , C07D213/69 , C07D213/74 , C07D239/10 , C07D307/36 , C07D333/06 , C07D333/34
摘要： Provided are a class of alkylphenol compounds and a preparation method therefor. Specifically provided are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome.
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8.发明申请公开(公告)号：US20180237399A1
公开(公告)日：2018-08-23
申请号：US15772105
申请日：2016-11-01
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.
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9.发明申请公开(公告)号：US20170081301A1
公开(公告)日：2017-03-23
申请号：US15306971
申请日：2015-04-22
发明人： Fajun NAN , Min LI , Zhaobing GAO , Yangming ZHANG , Haining HU , Haiyan XU , Huanan LIU , Xiaoping PI
IPC分类号： C07D307/24 , C07C237/48 , C07C275/64 , C07C235/16 , C07C271/28 , C07C333/08
CPC分类号： C07D307/24 , A61K31/167 , A61K31/17 , A61K31/27 , A61K31/277 , A61K31/341 , C07C231/02 , C07C233/62 , C07C235/16 , C07C235/74 , C07C237/04 , C07C237/22 , C07C237/48 , C07C269/04 , C07C269/06 , C07C271/28 , C07C273/18 , C07C275/64 , C07C333/08 , C07C2601/02 , C07C2601/14
摘要： The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.
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10.发明申请2,2'-TANDEM DITHIAZOLE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF 有权2,2'-TANDEM DITHIAZOLE化合物，其制备方法及其用途公开(公告)号：US20170044119A1
公开(公告)日：2017-02-16
申请号：US15301763
申请日：2015-03-27
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。
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