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11. 发明申请

US20190315783A1 PRODRUGS OF GLUTAMINE ANALOGS 审中-公开
公开(公告)号：US20190315783A1
公开(公告)日：2019-10-17
申请号：US16454853
申请日：2019-06-27
申请人： THE JOHNS HOPKINS UNIVERSITY , Ústav organické chemie a biochemie AV CR, v.v.i.
发明人： Barbara Slusher , Rana Rais , Lukas Tenora , Pavel Majer , Andrej Jancarik
IPC分类号： C07F9/24 , C07C227/14 , C07K5/083 , C07H19/207 , C07H15/203 , C07D317/40 , A61K31/404 , C07D317/38 , C07D473/34 , C07D263/04 , C07D309/10 , C07C245/18 , C07D211/90 , A61P35/00 , C07C271/22 , C07D209/18 , C07K5/062 , C07D263/18 , C07K5/078 , C07F9/6561 , C07D209/20
摘要： The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

12. 发明授权

US10443084B2 Naphthalene derived chromogenic enzyme substrates 有权
公开(公告)号：US10443084B2
公开(公告)日：2019-10-15
申请号：US15906667
申请日：2018-02-27
申请人： Glycosynth Limited
发明人： Hayley Jane Turner , Michael Burton
IPC分类号： C12Q1/34 , C07H15/20 , C07H15/203
摘要： Conjugates of 2,3-dihydroxynaphthalene and its derivatives with enzyme cleavable groups are chromogenic substrates that form colored compounds when complexed with metal ions, e.g. iron ions, on cleavage by enzymes, and are useful in microbial detection and identification. The cleavage products form purple or red-brown colored complexes, that can easily be observed by the naked eye. Microbes can be grown in the presence of the substrates and the metal salts that provide the metal ion for complexing with the 2,3-dihydroxynaphthalene product. Substituents in the naphthalene ring may affect the solubility of the substrates and also the diffusibility and color of the metal complexes. Some of the substrates yield soluble complexes on cleavage and are of particular value in liquid growth media. Other substrates produce less soluble complexes that are more suitable for use in solid agar media.Some substrates are new compounds, such as those having the general formula II wherein one of the following applies i) m=0, R4═R5=Z1═H, Y1 is selected from the group consisting of D-glucuronyl and D-ribofuranosyl; ii) m=2, each R6 is Br, R4═R5═H or Br, Z1═H, Y1 is glycosyl or phosphate; iii) m=1, R6 is —SO3X, X is H or M+ wherein M+ is an alkali metal cation or a non-metal cation, Y1 is glycosyl and R4═R5=Z1═H; iv) m=0, R4═NO2, R5═Z1═H, Y1=glycosyl. Methods of synthesizing the substrates are described.

13. 发明申请

US20190292212A1 Dicaffeoyl Spermidine Derivative Glycosides And Use Thereof 审中-公开
公开(公告)号：US20190292212A1
公开(公告)日：2019-09-26
申请号：US16070607
申请日：2017-01-13
申请人： Jinan University
发明人： Hao Gao , Xinsheng Yao , Rongrong He , Guodong Chen , Zhengqun Zhou , Chuanxi Wang , Dan Hu , Hongxia Fan
IPC分类号： C07H15/203 , A61P31/14 , A61P25/28 , C07H1/08
摘要： The present invention relates to dicaffeoyl spermidine derivative glycosides, a preparation method and a use thereof. The biological activity experiments show that the dicaffeoyl spermidine derivative glycosides of the present invention have anti-oxidative activity and antiviral activity, and their activity are even better than that of a positive control drug, thus can be used as an antioxidant for the prevention and/or treatment of neurodegenerative diseases such as Senile dementia, and as an antiviral agent for the prevention and/or treatment of viral infections.

14. 发明申请

US20190201428A1 COMPOSITION CONTAINING STILBENE GLYCOSIDE AND PREPARATION AND USES THEREOF FOR TREATING DIABETES 审中-公开
公开(公告)号：US20190201428A1
公开(公告)日：2019-07-04
申请号：US16297672
申请日：2019-03-10
申请人： Shiming Li
发明人： Shiming Li , Tao Long , Guliang Yang , Yin Xu , Xiaojian Lv , Jianfeng Zhan
IPC分类号： A61K31/7034 , A61K36/70 , A61P3/10 , C07H15/203
CPC分类号： A61K31/7034 , A61K36/70 , A61K2236/15 , A61K2236/333 , A61K2236/39 , A61K2236/51 , A61P3/10 , C07B2200/09 , C07H15/203
摘要： Disclosed is a method of processing Polygonum multiflorum, the method contains preparing a root extract solution and placing the solution under UV light for 1 to 24 hours. Also disclosed is a composition prepared from the method that can be for use in the prevention, treatment, and management of diabetes in human and animal subjects.

15. 发明申请

US20190144916A1 REAGENTS AND METHODS FOR SCREENING MPS I, II, IIIA, IIIB, IVA, VI, AND VII 审中-公开
公开(公告)号：US20190144916A1
公开(公告)日：2019-05-16
申请号：US16224001
申请日：2018-12-18
申请人： University of Washington through its Center for Commercialization
发明人： Michael H. Gelb , Arun Babu Kumar , Frances Hocutt , Zdenek Spacil , Mariana Natali Barcenas Rodriguez , Frantisek Turecek , C. Ronald Scott
IPC分类号： C12Q1/34 , C07H15/203
摘要： Reagents, methods, and kits for assaying enzymes associated with lysosomal storage diseases MPS-I, MPS-II, MPS-IIIA, MPS-IIIB, MPS-IVA, MPS-VI, and MPS VII.

16. 发明授权

US10196668B2 Reagents and methods for screening MPS I, II, IIIA, IIIB, IVA, VI, and VII 有权
公开(公告)号：US10196668B2
公开(公告)日：2019-02-05
申请号：US14916526
申请日：2014-09-05
申请人： University of Washington through its Center for Commercialization
发明人： Michael H. Gelb , Arun Babu Kumar , Frances Hocutt , Zdenek Spacil , Mariana Natali Barcenas Rodriguez , Frantisek Turecek , C. Ronald Scott
IPC分类号： C12Q1/34 , C07H15/203
摘要： Reagents, methods, and kits for assaying enzymes associated with lysosomal storage diseases MPS-I, MPS-II, MPS-IIIA, MPS-IIIB, MPS-IV A, MPS-VI, and MPS VII. In one aspect, the invention provides methods for assaying one or more enzymes associated with a lysosomal storage disease. In a first embodiment, the method includes: (a) contacting a sample with a first solution to provide a solution comprising one or more lysosomal enzymes; (b) contacting the one or more lysosomal enzymes in solution with an enzyme substrate for each lysosomal enzyme to be analyzed and incubating the substrates with the enzymes for a time sufficient to provide a solution comprising an enzyme product for each lysosomal enzyme present in the sample.

17. 发明授权

US10183908B2 Compositions for the treatment of kidney and/or liver disease 有权
公开(公告)号：US10183908B2
公开(公告)日：2019-01-22
申请号：US15558155
申请日：2016-03-18
申请人： VECTUS BIOSYSTEMS LIMITED
发明人： Karen Annette Duggan
IPC分类号： C07H15/203 , C07C235/34 , C07D231/12 , C07D333/24 , C07D239/26 , C07D261/08 , C07C237/20 , C07D207/327 , C07D277/30 , C07D213/56 , C07D307/54
摘要： The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of kidney and/or liver disease.

18. 发明申请

US20190016744A1 PHENYLPROPANOID COMPOUND AND PREPARATION METHOD AND USE THEREOF 审中-公开
公开(公告)号：US20190016744A1
公开(公告)日：2019-01-17
申请号：US16132506
申请日：2018-09-17
申请人： QIANJIN PHARMACEUTICAL CO., LTD.
发明人： Peng Zhang , Kaifeng Peng , Yun Gong , Fujun Li , Nifu Liu , Bohou Xia , Limei Lin
IPC分类号： C07H15/203 , C07H1/08 , A61P29/00
CPC分类号： C07H15/203 , A61K9/0019 , A61K9/16 , A61K9/20 , A61K9/48 , A61K31/7034 , A61K36/19 , A61K36/232 , A61K36/28 , A61K36/29 , A61K36/48 , A61K36/486 , A61K36/738 , A61K36/758 , A61K45/06 , A61K2300/00 , A61P29/00 , C07H1/08
摘要： The present invention provides a phenylpropanoid compound and a preparation method and use thereof. The phenylpropanoid compound has a structural formula shown as formula (I), and the pharmaceutically acceptable salt has a structural formula shown as formula (II), formula (III), formula (IV), or formula (V). The phenylpropanoid compound and the pharmaceutically acceptable salt thereof have an effect on inhibiting a content of an inflammatory cytokine NO and an expression of an inflammatory cytokine TNF-α, have an effect on inhibiting a hydroxyl radical (—OH), thereby have anti-inflammatory and antioxidant activities, and has a good application prospect in preparing of a medicine for treating an inflammatory disease related to the above factors, such as cervicitis, endometritis, pelvic inflammatory disease, mastitis, sphagitis and/or arthritis.

19. 发明申请

US20190016743A1 COMPOUNDS FOR INHIBITING CANCER AND VIRUS 审中-公开
公开(公告)号：US20190016743A1
公开(公告)日：2019-01-17
申请号：US16069100
申请日：2017-01-12
申请人： Taipei Medical University
发明人： Yun YEN , Jing-Ping LIOU , Yun-Ru LIU
IPC分类号： C07H15/203 , A61K31/7034 , C07C235/64 , A61K31/216 , C07D211/58 , A61K31/4545 , A61K31/166
摘要： The invention relates to compounds for inhibiting a cancer cell or a virus. Particularly, the invention provides compounds for inhibiting, treating and/or preventing cancer and Zika virus.

20. 发明授权

US10174132B2 Heparan sulfate synthesis 有权
公开(公告)号：US10174132B2
公开(公告)日：2019-01-08
申请号：US14754175
申请日：2015-06-29
申请人： UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.
发明人： Geert-Jan Boons , Andre Venot , Sailaja Arungundram , Kanar al-Mafraji
IPC分类号： C08B37/00 , C07H5/04 , C07H15/04 , C07H15/203 , C07H23/00
摘要： The invention provides an efficient modular chemical synthesis for heparan sulfate oligosaccharides based on orthogonal protection strategies. Modular disaccharide building blocks, themselves the product of a novel combinatorial synthesis, are combined in numerous ways to produce a range of oligosaccharides.

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