公开(公告)号：US12129222B2

公开(公告)日：2024-10-29

申请号：US16324758

申请日：2017-08-11

申请人： Julius-Maximilians-Universitaet Wuerzburg

发明人： Ralf Wyrwa ,  Claudia Rode ,  Thomas Seemann ,  Lorenz Meinel ,  Jennifer Ritzer ,  Matthias Schnabelrauch

IPC分类号： C07C237/04 ,  A61K47/18 ,  A61K47/54 ,  A61K47/65 ,  C07C231/12 ,  C07C233/07 ,  C07C269/04

CPC分类号： C07C237/04 ,  A61K47/186 ,  A61K47/54 ,  A61K47/65 ,  C07C231/12 ,  C07C233/07 ,  C07C269/04 ,  C07C231/12 ,  C07C237/20 ,  C07C231/12 ,  C07C237/36 ,  C07C269/04 ,  C07C271/28

摘要： It is an object of the present invention to introduce carboxylic acid-functionalities suitable for coupling into the denatonium structure by means of simple synthesis, namely the synthesis of bitter principle derivatives based on the denatonium structure according to formula 1:




For example, according to the invention, lidocaine derivatives may be reacted with carboxylated benzyl halogenides. The carboxylated denatonium derivatives of the present invention are especially applied in medicine, biology, medical engineering as well as cosmetics, the pharmaceutical, chemical, and foodstuff industry.

公开(公告)号：US20210061783A1

公开(公告)日：2021-03-04

申请号：US16734413

申请日：2020-01-06

申请人： Yunnan Xike Science & Technology Co., Ltd.

发明人： Zheng Chen ,  Yinghui Cao ,  Ningning Yan ,  Songfeng Wang ,  Yong Zhang ,  Yuefeng Chen ,  Zhennan Huang ,  Shenghong Yuan

IPC分类号： C07D401/04 ,  C07D207/04 ,  C07D241/04 ,  C07D233/58 ,  C07D235/06 ,  C07C25/08 ,  C07C233/07 ,  C07C53/02 ,  C07C53/08 ,  C07C59/265 ,  C07C59/08 ,  C07C53/126 ,  C07C57/10 ,  C07C57/12 ,  C07C63/06 ,  C07C59/185 ,  C07C237/22

摘要： A synthetic nicotine composition comprising synthetic nicotine, a synthetic nicotine salt and a synthetic nicotine derivative, wherein the synthetic nicotine, the synthetic nicotine salt, and the synthetic nicotine derivative are in mass percentage; the synthetic nicotine accounts for 1-20%, the synthetic nicotine salt accounts for 30-70%, and the synthetic nicotine derivative accounts for 20-50%; and the synthetic nicotine is one or more of S-nicotine and a mixture of R-nicotine containing a racemate and S-nicotine. The synthetic nicotine, synthetic nicotine salt and synthetic nicotine derivative according to the present invention are proportionally mixed to prepare an existing synthetic nicotine product, which relieves the problem of the impact of impurities in natural extracted nicotine products causing an unpleasant smell, a bitter taste and a strong volatility, and can be used in the fields of low temperature heat-not-burn products, snuff, electronic cigarettes, nicotine release patches, insecticides, herbicides, microbicides, drug synthesis, etc.

公开(公告)号：US20210047347A1

公开(公告)日：2021-02-18

申请号：US16941821

申请日：2020-07-29

申请人： Navitor Pharmaceuticals, Inc.

发明人： Kristina Michelle FETALVERO ,  Sridhar NARAYAN ,  David John O'NEILL ,  Eddine SAIAH ,  Shomit SENGUPTA

IPC分类号： C07F7/08 ,  A61K38/00 ,  A61K31/198 ,  A61K31/223 ,  C07C261/04 ,  C07C311/13 ,  C07C311/19 ,  C07C311/51 ,  C07C229/28 ,  C07C233/40 ,  C07C233/83 ,  C07C237/06 ,  C07C237/12 ,  C07C237/30 ,  A61K31/197 ,  A61K31/221 ,  A61K31/275 ,  A61K31/341 ,  A61K31/41 ,  A61K31/695 ,  A61K45/06 ,  C07C229/12 ,  C07C229/14 ,  C07C229/18 ,  C07C229/20 ,  C07C233/07 ,  C07C233/47 ,  C07C233/49 ,  C07C233/51 ,  C07C233/63 ,  C07C255/61 ,  C07C311/06 ,  C07C311/10 ,  C07C311/14 ,  C07D257/04 ,  C07D307/33

摘要： The present invention provides compounds, compositions thereof, and methods of using the same.

公开(公告)号：US10919863B2

公开(公告)日：2021-02-16

申请号：US16319957

申请日：2017-07-28

申请人： Vectus Biosystems Limited

发明人： Karen Annette Duggan

IPC分类号： C07D239/26 ,  A61P11/00 ,  C07C39/15 ,  C07C215/54 ,  C07C233/11 ,  C07D207/408 ,  C07D213/56 ,  C07D237/08 ,  C07D261/14 ,  C07D263/44 ,  C07D277/30 ,  C07D401/10 ,  C07D403/10 ,  C07D333/24 ,  C07C233/07 ,  C07D231/56 ,  C07D235/26 ,  C07D235/06 ,  C07C59/52 ,  C07C275/42 ,  C07D213/73 ,  C07D277/68 ,  A61P11/06 ,  C07D231/12 ,  C07C211/29 ,  C07D207/38 ,  C07C255/00 ,  C07C271/28 ,  C07C217/48 ,  C07C261/04 ,  C07D241/12 ,  C07D309/10 ,  C07D233/78 ,  C07D261/08 ,  C07D209/48 ,  C07C237/20 ,  C07D207/327 ,  C07C237/22 ,  C07D307/54 ,  C07D249/18 ,  C07D209/34 ,  C07D263/38 ,  C07C307/10 ,  C07D207/26 ,  C07D207/444 ,  C07C235/34 ,  C07C311/03 ,  C07C311/08 ,  C07C239/20 ,  C07C235/78 ,  C07D209/18 ,  C07D263/58 ,  C07D215/14 ,  C07D207/40 ,  A61K45/06

摘要： The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

公开(公告)号：US20200048198A1

公开(公告)日：2020-02-13

申请号：US16492656

申请日：2018-03-21

申请人： The Regents of the University of California ,  Vybyl Holdings. Inc.

发明人： Nathan C Gianneschi ,  Paul A. Bertin

IPC分类号： C07D209/14 ,  C07C271/60 ,  C07C233/07 ,  A61K38/38

摘要： The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule histone deacetylase inhibitors (HDIs) that are chemically modified to have one or more moieties that include hydrophobic portions. In some aspects, the disclosure provides compositions that include such modified HDIs and a protein, such as albumin or albumin mimetics. Further, the disclosure provides various uses of these compounds and compositions.

公开(公告)号：US10179764B2

公开(公告)日：2019-01-15

申请号：US15745337

申请日：2016-07-23

申请人： DONGGUK UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION ,  KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION

发明人： Yongseok Choi ,  Jae-Hong Kim ,  Kyeong Lee ,  Hyo-Kyung Han ,  Jun Dong Wei ,  Jinsun Kwon ,  Ja-Il Goo

IPC分类号： C07C311/21 ,  C07D241/04 ,  C07C233/07 ,  C07D265/30 ,  C07D211/06 ,  C07C233/88 ,  C07C235/34 ,  C07C237/42 ,  C07C311/16 ,  C07D295/192 ,  C07D295/205 ,  A61P11/06 ,  A61P35/00 ,  C07C275/32 ,  C07D257/04 ,  C07D295/185

摘要： The present invention relates to a novel compound showing leukotriene B4 receptor 2 (BLT2) inhibitory activity and a pharmaceutical composition, for preventing or treating inflammatory diseases, having same as an active ingredient. The inventors identified a novel compound containing BTL2 inhibitory activity, and experimentally confirmed that the present novel compound had an excellent effect on the enhancement of the cancer cell death, on the inhibition of the metastasis and chemotactic mobility, and on the anti-asthma activity. Therefore, the present novel compound can be used as a very effective pharmaceutical component for treating the inflammatory-related diseases.

公开(公告)号：US09789086B1

公开(公告)日：2017-10-17

申请号：US15510755

申请日：2015-09-17

申请人： Industry-University Cooperation Foundation Hanyang University ERICA Campus

发明人： Jung-Mi Hah ,  Kyung Jin Jung

IPC分类号： A61K31/415 ,  C07D261/06 ,  C07C233/07 ,  C07C233/10

CPC分类号： A61K31/415 ,  C07C233/07 ,  C07C233/10 ,  C07D261/02 ,  C07D261/06 ,  C07D261/18 ,  C07D413/12

摘要： The present invention relates to N-(5-arylamido-2-methylphenyl)-5-methylisoquoxazole-4-carboxamide derivative, or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising same. The compound according to the present invention exhibits an FMS kinase inhibitory activity and thus can be used as pharmaceutical composition for preventing and treating diseases associated therewith.

公开(公告)号：US09382193B2

公开(公告)日：2016-07-05

申请号：US14583850

申请日：2014-12-29

申请人： EMORY UNIVERSITY

发明人： Lanny S. Liebeskind ,  Wenting Wu ,  Zhihui Zhang ,  Hao Li ,  Angus A. Lamar

IPC分类号： C07F7/08 ,  C07C231/02 ,  C07C233/65 ,  C07C233/69 ,  C07C233/07 ,  C07D213/82 ,  C07D233/90 ,  C07D295/192 ,  C07D307/52 ,  C07F7/18 ,  C07H1/00 ,  C07H21/02 ,  C07K1/00 ,  C07K1/02 ,  C07K5/062 ,  C07K5/065 ,  C07K5/068 ,  C07K5/072 ,  C07K5/087

CPC分类号： C07C231/02 ,  C07C233/07 ,  C07C233/65 ,  C07C233/69 ,  C07D213/82 ,  C07D233/90 ,  C07D295/192 ,  C07D307/52 ,  C07F7/1804 ,  C07H1/00 ,  C07H21/02 ,  C07K1/003 ,  C07K1/02 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06086 ,  C07K5/06104 ,  C07K5/0812

摘要： The disclosure relates to methods for producing amide bonds and reagents related thereto. In some embodiments, the disclosure relates to methods of producing an amide comprising mixing an O-silylated thionoester and an amine under conditions such that an amide is formed. In another embodiment, the disclosure relates to mixing a thiolacid, a silylating agent, and an amine under conditions such that an amide is formed.

摘要翻译： 本公开涉及制备酰胺键的方法和与其相关的试剂。 在一些实施方案中，本公开涉及制备酰胺的方法，包括在形成酰胺的条件下混合O-甲硅烷基化的硫代酯和胺。 在另一个实施方案中，本公开涉及在形成酰胺的条件下混合硫醇酸，甲硅烷基化试剂和胺。

公开(公告)号：US20130065963A1

公开(公告)日：2013-03-14

申请号：US13551086

申请日：2012-07-17

申请人： Alan P. Kozikowski ,  Anatoly Dritschilo ,  Mira Jung ,  Pavel A. Petukhov ,  Bin Chen

发明人： Alan P. Kozikowski ,  Anatoly Dritschilo ,  Mira Jung ,  Pavel A. Petukhov ,  Bin Chen

IPC分类号： A61K31/16 ,  A61K31/17 ,  C07C275/40 ,  C07C275/26 ,  A61P25/00 ,  C07C233/06 ,  C07C233/07 ,  A61K31/167 ,  A61P35/00 ,  C07C275/24 ,  C07C275/28

CPC分类号： C07C271/02 ,  A61K31/19 ,  C07C259/06 ,  C07C275/24 ,  C07C275/26 ,  C07C275/40 ,  C07C323/44 ,  C07C323/60 ,  C07C2603/74 ,  C07D215/48 ,  C07D215/54

摘要： The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.

摘要翻译： 本发明提供了新型的HDAC抑制剂。 还提供了使癌细胞对放射治疗的细胞毒作用敏感的方法以及治疗癌症的方法和治疗神经疾病的方法。 另外，本发明还提供了包含本发明的HDAC抑制剂的药物组合物和包含含有本发明的HDAC抑制剂的容器的试剂盒。

公开(公告)号：US20100137401A1

公开(公告)日：2010-06-03

申请号：US12698261

申请日：2010-02-02

申请人： Wenqing Yao ,  Colin Zhang ,  Jincong Zhuo ,  Meizhong Xu ,  Konstantinos Agrios ,  Brian Metcalf

发明人： Wenqing Yao ,  Colin Zhang ,  Jincong Zhuo ,  Meizhong Xu ,  Konstantinos Agrios ,  Brian Metcalf

IPC分类号： A61K31/404 ,  C07C233/07 ,  A61K31/165 ,  C12N9/99 ,  C07D307/22 ,  A61K31/341 ,  C07D209/18 ,  C07D319/16 ,  A61K31/357 ,  C07C233/06 ,  C07C233/05 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P9/00 ,  A61P9/10

CPC分类号： C07C233/11 ,  C07C233/13 ,  C07C233/19 ,  C07C233/22 ,  C07C233/23 ,  C07C235/22 ,  C07C323/60 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/28 ,  C07C2602/42 ,  C07D209/14 ,  C07D209/16 ,  C07D307/22 ,  C07D319/20

摘要： The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

摘要翻译： 本发明涉及11-和bgr的抑制剂。 1型羟基类固醇脱氢酶，盐皮质激素受体（MR）的拮抗剂及其药物组合物。 本发明的化合物可用于治疗与11-bgr的表达或活性相关的各种疾病; 羟基类固醇脱氢酶1型和/或与醛固酮过量相关的疾病。