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1. 发明申请

US20220202837A1 COMPOSITIONS AND METHODS FOR MODIFICATION OF BIOMOLECULES 有权
公开(公告)号：US20220202837A1
公开(公告)日：2022-06-30
申请号：US17672508
申请日：2022-02-15
申请人： The Regents of the University of California
发明人： Carolyn Ruth Bertozzi , Nicholas J. Agard , Jennifer A. Prescher , Jeremy Michael Baskin , Ellen May Sletten
IPC分类号： A61K31/655 , C07C45/29 , C07C45/51 , C07C45/63 , C07C49/457 , C07C49/753 , C07C59/72 , C07C63/66 , C07C69/708 , C07C69/76 , C07D207/416 , C07D207/452 , C07D249/16 , C07D495/04 , G01N33/531 , G01N33/68 , C07C63/74 , C07C57/26
摘要： The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

2. 发明申请

US20210363109A1 PHENYL CYCLOHEXANONE DERIVATIVES AND METHODS OF MAKING AND USING THEM 有权
公开(公告)号：US20210363109A1
公开(公告)日：2021-11-25
申请号：US17395433
申请日：2021-08-05
申请人： SPIRIFY PHARMA INC.
发明人： Irving W. WAINER
IPC分类号： C07D233/24 , C07C49/753 , C07C225/22 , C07C311/36 , C07C255/46 , C07C225/28 , C07D207/09 , C07D307/14
摘要： Phenyl cyclohexanone based active agents, pharmaceutical preparations containing such active agents, methods of modifying cellular activity by contacting cells with such active agents, and methods of treating various conditions by administering such active agents to a patient are described.

3. 发明授权

US10889556B2 Compositions and methods for inhibiting influenza RNA polymerase PA endonuclease 有权
公开(公告)号：US10889556B2
公开(公告)日：2021-01-12
申请号：US16125468
申请日：2018-09-07
申请人： The Regents of the University of California
发明人： Seth M. Cohen , Cy V. Credille , David T. Puerta
IPC分类号： C07D309/32 , C07D309/40 , C07D213/69 , C07D213/90 , C07D401/04 , C07D401/10 , C07D413/04 , C07C49/747 , C07C49/453 , C07C62/38 , C07C65/03 , C07C65/05 , C07C69/757 , A61P31/16 , C07C49/717 , C07C49/753
摘要： There are provided inter alia metalloenzyme inhibitors, such as inhibitors of influenza A RNA dependent RNA polymerase PA subunit endonuclease, and methods of synthesis and use of the same.

4. 发明申请

US20200148623A1 ANTICONVULSANT COMPOUNDS 审中-公开
公开(公告)号：US20200148623A1
公开(公告)日：2020-05-14
申请号：US16723630
申请日：2019-12-20
申请人： OWEN-BARRY PHARMACEUTICALS INC.
发明人： Michael Poulter , Tony Durst
IPC分类号： C07C69/78 , C07C49/603 , C07D211/08 , C07C255/40 , C07C321/28 , C07C317/24 , C07C235/84 , A61P25/08 , C07C49/683 , C07C49/697 , C07C49/753 , C07C65/32 , A61K31/166 , A61K31/4453 , A61K31/122 , A61K31/216 , A61K31/192 , C07C49/67 , C07D295/192 , C07C69/76 , C07C49/723 , C07C49/623 , C07C69/157 , C07C63/66
摘要： The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of chronic or acute pain.

5. 发明授权

US10112918B2 15-oxospiramilactone derivatives, preparation method and uses thereof 有权
公开(公告)号：US10112918B2
公开(公告)日：2018-10-30
申请号：US14785075
申请日：2014-04-21
申请人： Kunming Institute of Botany, The Chinese Academy of Sciences , The Key Laboratory of Chemistry for Natural Product of Guizhou Province & Chinese Academy of Science , Shanghai Institutes for Biological Sciences, CAS , Institute of Zoology, Chinese Academy of Sciences
发明人： Xiaojiang Hao , Chen Yan , Haiyang Liu , Lin Li , Xiaoli He , Quan Chen
IPC分类号： C07C69/16 , C07C69/18 , C07C69/26 , C07C69/30 , C07C69/63 , C07C69/78 , C07C49/743 , C07C62/38 , C07C205/57 , C07D295/116 , C07D295/185 , C07D333/40 , C07D311/78 , A61K31/366 , C07D311/94 , C07D407/12 , C07D221/28 , C07D327/10 , C07D409/12 , C07D493/08 , C07D493/10 , C07D495/04 , C07D498/08 , C07C309/66 , C07C49/753
摘要： The invention relates to a derivative of 15-oxospiramilacton, particularly to a compound of Formula I or II, or an isomer, a solvate or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the compound as pharmaceutically active ingredient, a method for preparing the same, and use thereof in manufacture of an anti-tumor agent. The derivative of 15-oxospiramilactone of the invention have an activity against multiple tumor cell lines, and the anti-tumor activity is positively correlated to an activity inhibiting the Wnt signaling pathway.

6. 发明授权

US10100028B2 Synthesis routes for prostaglandins and prostaglandin intermediates using metathesis 有权
公开(公告)号：US10100028B2
公开(公告)日：2018-10-16
申请号：US15026026
申请日：2014-09-30
申请人： IRIX PHARMACEUTICALS, INC.
发明人： George Petros Yiannikouros , Panos Kalaritis , Chaminda Priyapushpa Gamage , Denis Viktorovich Arefyev
IPC分类号： C07D313/00 , C07C49/753 , C07C49/743 , C07C41/28 , C07C43/196 , C07C45/70 , C07C67/08 , C07C69/604 , C07D311/94
摘要： Methods of synthesizing prostaglandins, prostaglandin analogs and their synthetic intermediates are described. The methods can comprise metal-catalyzed metathesis reactions. Also provided are synthetic intermediates that can be used in the synthesis of the prostaglandins and prostaglandin analogs.

7. 发明申请

US20180194715A1 ANTICONVULSANT COMPOUNDS 审中-公开
公开(公告)号：US20180194715A1
公开(公告)日：2018-07-12
申请号：US15866924
申请日：2018-01-10
申请人： OWEN-BARRY PHARMACEUTICALS INC.
发明人： Michael Poulter , TONY DURST
IPC分类号： C07C69/78 , C07C65/32 , C07C49/753 , C07C49/697 , C07C49/683 , C07C49/603 , C07C235/84 , C07C317/24 , C07C321/28 , C07C255/40 , C07D211/08 , A61P25/08
摘要： The present application relates to compounds and methods for reducing the severity of convulsant activity or epileptic seizures, or for the treatment of chronic or acute pain.

8. 发明授权

US09884801B2 Compounds from antrodia camphorata, method for preparing the same and use thereof 有权
公开(公告)号：US09884801B2
公开(公告)日：2018-02-06
申请号：US14984442
申请日：2015-12-30
申请人： ONENESS BIOTECH CO.,LTD.
发明人： Chiung-Lin Liu , Wei-Tse Tsai , Kai-Hsin Hsieh
IPC分类号： A61K31/122 , C07C49/753
CPC分类号： C07C49/753 , A61K31/22 , A61K36/00 , A61P35/00 , C07C2601/16 , A61K2300/00
摘要： The invention relates to bioactive compounds purified from mycelium of Antrodia camphorata and the manufacturing method thereof. A method for treatment of cancers by administrating an effective amount of the said compounds selected from the group consisting of AC006, AC007, AC009, AC011, AC012, AC007-H1, AC009-H1, and AC012-H1 wherein the cancers is liver cancer, brain cancer, prostate cancer, breast cancer, colorectal cancer, or melanoma.

9. 发明申请

US20170210764A1 CYCLOBUTENEDIONE DERIVATIVE, NONAQUEOUS ELECTROLYTIC SOLUTION, AND LITHIUM ION SECONDARY BATTERY 审中-公开
公开(公告)号：US20170210764A1
公开(公告)日：2017-07-27
申请号：US15500459
申请日：2015-07-01
申请人： NEC Corporation
发明人： Katsumi MAEDA , Shizuka SATO , Mika HORIE
IPC分类号： C07F7/08 , C07C49/753 , C07C49/647 , C07C49/697 , C07D307/46 , C07D333/22 , H01M10/0525 , H01M10/0568 , H01M10/0567 , H01M10/0569 , H01M4/505 , H01M4/525 , H01M4/38 , H01M4/587 , C07C49/683
CPC分类号： C07F7/0803 , C07C49/647 , C07C49/683 , C07C49/697 , C07C49/753 , C07C2601/04 , C07D307/46 , C07D333/22 , H01M4/386 , H01M4/483 , H01M4/505 , H01M4/525 , H01M4/587 , H01M10/0525 , H01M10/0567 , H01M10/0568 , H01M10/0569 , H01M2300/0025 , H01M2300/0037 , Y02T10/7011
摘要： A nonaqueous electrolytic solution comprising a cyclobutenedione derivative represented by the following general formula (1): wherein R1 represents an organic group having a carbon-carbon double bond or a carbon-carbon triple bond in its structure, and R2 represents an alkyl group having 1-6 carbon atoms, an alkoxy group having 1-6 carbon atoms, a thioalkyl group having 1-6 carbon atoms, a substituted or unsubstituted thioaryl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heteroaryl group.

10. 发明授权

US09409845B2 Alpha-(3,5-dimethoxybenzylidene)-alpha′-hydrocarbyl methylene cyclic ketone and preparation method thereof 有权
标题翻译： α-（3,5-二甲氧基亚苄基）-α-烃基亚甲基环酮及其制备方法
公开(公告)号：US09409845B2
公开(公告)日：2016-08-09
申请号：US14723785
申请日：2015-05-28
申请人： PHARMAXYN LABORATORIES LTD.
发明人： Guizhen Ao , Jihua Nie , Huanqiu Li , Lingxuan Mo , Lei Chen , Heng Song , Shaohua Chen
IPC分类号： C07C45/00 , A61K31/00 , C07C49/753 , C07C317/24 , C07C225/22 , C07C45/45
CPC分类号： C07C49/753 , C07C45/45 , C07C225/22 , C07C317/24 , C07C2601/14
摘要： The present invention discloses a α-(3,5-dimethoxybenzylidene)-α′-hydrocarbyl methylene cyclic ketone with the following formula: wherein R is aryl or alkyl, its preparation method is: the cyclic ketone blended with morpholine are subjected to azeotropic dehydration to give enamine, the enamine is condensed with 3,5-dimethoxybenzaldehyde and then condensed with alkyl or aryl formaldehyde under acidic or basic conditions to give the product, the present invention further discloses an antitumor agent comprising α-(3,5-dimethoxybenzylidene)-α′-hydrocarbyl methylene cyclic ketone or medically acceptable salts and pharmaceutically acceptable carriers thereof. Through the above, the present invention providesα-(3,5-dimethoxybenzylidene)-α′-hydrocarbyl methylene cyclic ketone and preparation method thereof, the said compound is a high activity antitumor agent obtained by piecing and modifying the formulas of natural anti-tumor active ingredient resveratrol and curcumin, which has a good inhibitory effect on epidermal growth factor receptor.
摘要翻译：本发明公开了具有下式的α-（3,5-二甲氧基亚苄基）-α'-烃基亚甲基环酮，其中R是芳基或烷基，其制备方法是：与吗啉共混的环酮进行共沸脱水给予烯胺，烯胺与3,5-二甲氧基苯甲醛缩合，然后在酸性或碱性条件下与烷基或芳基甲醛缩合得到产物，本发明还公开了一种抗肿瘤剂，其包含α-（3,5-二甲氧基亚苄基） -α'-烃基亚甲基环酮或其医药上可接受的盐和药学上可接受的载体。通过上述，本发明提供α-（3,5-二甲氧基亚苄基）-α'-烃基亚甲基环酮及其制备方法，所述化合物是通过接头和改性天然抗肿瘤剂的方法得到的高活性抗肿瘤剂活性成分白藜芦醇和姜黄素，对表皮生长因子受体具有良好的抑制作用。

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