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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
Inventor： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Dakai CHEN , Lina ZHANG , Runtao ZHANG , Zhifu XIE
IPC: C07D471/04 , C12N9/12 , C07D211/78
CPC classification number: C07D471/04 , A61K31/437 , C07D211/78 , C12N9/12 , C12Y207/11031
Abstract: 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
Inventor： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Zhifu XIE , Jingtao WANG , Dongdong GUO
CPC classification number: C07C61/35 , A61K31/194 , C07C55/28 , C07C57/13 , C07C57/26 , C07C57/42 , C07C61/16 , C07C61/20 , C07C61/22 , C07C2601/08 , C07C2601/16 , Y02P20/55
Abstract: 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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公开(公告)号：US20190211005A1
公开(公告)日：2019-07-11
申请号：US16329336
申请日：2017-08-24
Inventor： Fajun NAN , Jia LI , Jian DING , Meiyu GENG , Yangming ZHANG , Yi CHEN , Yubo ZHOU , Chaojun GONG , Mingbo SU , Anhui GAO
IPC: C07D417/04 , A61P35/02
Abstract: 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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4.发明申请公开(公告)号：US20250122148A1
公开(公告)日：2025-04-17
申请号：US18728641
申请日：2023-01-10
Inventor： Fajun NAN , Zhaobing GAO , Wuheng DONG , Yueming ZHENG , Jintao WANG , Xiaoyu ZHOU , Huanan LIU , Haiyan XU
IPC: C07C269/04 , A61K31/27 , A61P21/00
Abstract: Disclosed are a high-selectivity KCNQ4 potassium channel agonist of formula I, a preparation method therefor and the use thereof. The compound further improves the KCNQ4 agonistic activity, and is still free of KCNQ2 agonistic activity, thus having excellent KCNQ4/KCNQ2 selectivity. The high-selectivity KCNQ4 agonist overcomes the defect of poor selectivity of existing potassium channel agonists, the activity is relatively increased, and the toxicity is remarkably reduced. The agonist also has a simpler structure and lower product cost, thereby having a better development prospect.
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5.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
Inventor： Fajun NAN , Xin XIE , Chenlu ZHANG , Shimeng GUO , Yangming ZHANG , Siwei WANG
IPC: C07J63/00
Abstract: 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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Patent Agency Ranking
公开(公告)号：US20200010492A1
公开(公告)日：2020-01-09
申请号：US16490837
申请日：2016-02-28
Inventor： Fajun NAN , Xin XIE , Linhai CHEN , Qing ZHANG , Yufeng XIAO , Hui YANG
IPC: C07F9/09 , C07F9/6561 , C07F9/6553 , C07F9/655
Abstract: 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
Inventor： Fajun NAN , Boliang LI , Yang ZHAN , Xiaowei ZHANG , Ying XIONG , Xichan HU , Yangming ZHANG
IPC: A61K31/4433 , A61K31/352 , C07D493/04
CPC classification number: A61K31/4433 , A61K31/352 , C07B37/04 , C07B49/00 , C07D493/04
Abstract: 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：US20240351966A1
公开(公告)日：2024-10-24
申请号：US18290268
申请日：2022-05-11
Inventor： Fajun NAN , Jingya LI , Zheng ZHANG , Yanan DUAN , Yangming ZHANG , Dandan CHEN , Chengqiu DAI
IPC: 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 classification number: 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
Abstract: 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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9.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
Inventor： Fajun NAN , Xin XIE , Yang LIU , Qing ZHANG , Linhai CHEN , Hui YANG
IPC: C07D239/60 , C07D239/52 , C07D213/69 , C07C49/825 , C07C39/19
CPC classification number: 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
Abstract: 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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10.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
Inventor： Fajun NAN , Min LI , Zhaobing GAO , Yangming ZHANG , Haining HU , Haiyan XU , Huanan LIU , Xiaoping PI
IPC: C07D307/24 , C07C237/48 , C07C275/64 , C07C235/16 , C07C271/28 , C07C333/08
CPC classification number: 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
Abstract: 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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