公开(公告)号：US11214591B2

公开(公告)日：2022-01-04

申请号：US16576406

申请日：2019-09-19

Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

Inventor： Francis Yoshimoto

IPC: C07D221/18 ,  A61K31/473 ,  C07J73/00 ,  C07J9/00

Abstract: The present disclosure provides for a synthetic strategy to incorporate a C12α-hydroxy group from the methylene (—CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues.

公开(公告)号：US20210024572A1

公开(公告)日：2021-01-28

申请号：US16808085

申请日：2020-03-03

Applicant: Epirium Bio Inc.

Inventor： Sundeep DUGAR ,  Dinesh MAHAJAN ,  George Frederic SCHREINER

IPC: C07J73/00 ,  C07J1/00 ,  C07J3/00 ,  C07J7/00 ,  C07J17/00 ,  C07J41/00 ,  C07J43/00 ,  C07J9/00 ,  C07J51/00

Abstract: The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.

公开(公告)号：US20190350239A1

公开(公告)日：2019-11-21

申请号：US16524437

申请日：2019-07-29

Applicant: BASF SE

Inventor： Thomas SUBKOWSKI ,  Claus BOLLSCHWEILER ,  Jens WITTENBERG ,  Wolfgang SIEGEL ,  Ralf PELZER

IPC: A23L27/20 ,  A61Q19/00 ,  A61K8/49 ,  C07J63/00 ,  C07C49/675 ,  A61K8/35 ,  A61K8/55 ,  C07D339/08 ,  C07D339/06 ,  C07D495/10 ,  C07D493/10 ,  C07D311/94 ,  C07D311/78 ,  C07D405/06 ,  C07D209/48 ,  C07D471/04 ,  C07D495/20 ,  C07D491/20 ,  C07F9/572 ,  A23L27/00 ,  C07J73/00 ,  C07J33/00

Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

公开(公告)号：US20190255076A1

公开(公告)日：2019-08-22

申请号：US16298818

申请日：2019-03-11

Applicant: ZebraPeutics Inc.

Inventor： Xiao-Yan Wen ,  R. Loch MacDonald ,  Andrew Baker ,  Tom A. Schweizer

IPC: A61K31/585 ,  A61P9/00 ,  A61P9/14 ,  A61K31/58 ,  A61K31/567 ,  C07J1/00 ,  A61K31/4422 ,  A61K31/366 ,  A61K31/357 ,  C07J73/00 ,  A61K31/4545

Abstract: The described invention relates to small molecule therapeutic compounds capable of reducing the incidence of intracerebral hemorrhage and brain microhemorrhages identified using zebrafish and mouse models of intracerebral hemorrhage and brain microhemorrhages.

公开(公告)号：US10208083B2

公开(公告)日：2019-02-19

申请号：US15738328

申请日：2016-06-28

Applicant: GALENICA S.A. ,  ENERGONBIO TECHNOLOGIES S.A.

Inventor： Dimitrios Trafalis

IPC: A61P35/02 ,  C07J73/00

Abstract: Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.

公开(公告)号：US20180194800A1

公开(公告)日：2018-07-12

申请号：US15738328

申请日：2016-06-28

Applicant: GALENICA S.A. ,  ENERGONBIO TECHNOLOGIES S.A.

Inventor： Dimitrios TRAFALIS

IPC: C07J73/00 ,  A61P35/02

CPC classification number: C07J73/005 ,  A61P35/02

Abstract: Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.

公开(公告)号：US09809822B2

公开(公告)日：2017-11-07

申请号：US15100092

申请日：2013-12-11

Applicant: Hong Kong Baptist University

Inventor： Ge Zhang ,  Aiping Lu ,  Cheng Wang ,  Cheng Lu ,  Jun Lu ,  Biao Liu

IPC: C12N15/115 ,  A61K47/48 ,  A61K31/7088 ,  A61K31/585 ,  C07J73/00

CPC classification number: C12N15/115 ,  A61K31/585 ,  A61K31/7088 ,  A61K47/549 ,  C07J73/003 ,  C12N2310/16 ,  C12N2310/351 ,  C12N2320/30

Abstract: Tripyolide-nucleic acid aptamer derivatives, a preparation method and use thereof are shown. The structure of the triptolide-nucleic acid aptamer derivatives is as shown by formula I, wherein the definitions of R1-R7, G, A, B, M, Z and X are described. The present invention uses a nucleic acid aptamer and triptolide or modified compounds thereof as the starting materials, and introduces a linking group A at the C-14 hydroxyl group, epoxy groups and five-membered ring lactones in triptolide, then connects it to a nucleic acid aptamer B, and obtains the triptolide-nucleic acid aptamer derivatives. The triptolide-nucleic acid aptamer derivatives of the present invention have the characteristics of good targeting, a high anti-cancer activity, low toxicity and side effects, good water solubility and high bioavailability, and the preparation method of the present invention is scientific and reasonable and has a controllable quality and good repeatability, and is thereby suitable for production.

公开(公告)号：US20170265510A1

公开(公告)日：2017-09-21

申请号：US15610958

申请日：2017-06-01

Applicant: BASF SE

Inventor： THOMAS SUBKOWSKI ,  Claus Bollschweiler ,  Jens Wittenberg ,  Wolfgang Siegel ,  Ralf Pelzer

IPC: A23L27/20 ,  A23L27/00 ,  A61K8/35 ,  A61K8/49 ,  A61K8/55 ,  A61Q19/00 ,  C07C49/665 ,  C07C49/675 ,  C07D209/48 ,  C07D311/78 ,  C07D311/94 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D471/04 ,  C07D491/20 ,  C07D493/10 ,  C07D495/10 ,  C07D495/20 ,  C07F9/572 ,  C07J33/00 ,  C07J63/00 ,  C07J73/00 ,  C07J11/00

CPC classification number: A23L27/2056 ,  A23L27/88 ,  A61K8/35 ,  A61K8/49 ,  A61K8/492 ,  A61K8/4926 ,  A61K8/498 ,  A61K8/4986 ,  A61K8/55 ,  A61K2800/244 ,  A61Q19/00 ,  C07C49/665 ,  C07C49/675 ,  C07C2603/26 ,  C07D209/48 ,  C07D311/78 ,  C07D311/94 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D471/04 ,  C07D491/20 ,  C07D493/10 ,  C07D495/10 ,  C07D495/20 ,  C07F9/5728 ,  C07J11/00 ,  C07J33/007 ,  C07J63/008 ,  C07J73/003

Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

公开(公告)号：US20170029460A1

公开(公告)日：2017-02-02

申请号：US15302983

申请日：2015-04-30

Applicant: JIMEI UNIVERSITY

Inventor： Hui NI ,  Huinong CAI ,  Yuanfan YANG ,  Qiufen GAO ,  Feng CHEN ,  Xiping DU ,  Gaoling HUANG ,  Ling WU ,  Anfeng XIAO

IPC: C07J73/00 ,  A23L33/105

CPC classification number: C07J73/00 ,  A23L33/105 ,  A23V2002/00 ,  C07J73/008

Abstract: A limonin extraction method, comprising the following steps: step one, raw material extracting or juicing: directly soaking raw material in water or using a presser to directly juice the raw material to obtain the extract; step two, adding salt and adjusting pH: adding a sulfate solid material or saturated sulfate solution to the extract; adjusting pH to 3-7; step three, heating and preserving heat: heating to 20° C.-100° C. and keeping at the temperature for 10 minutes-110 minutes; step four, centrifuging: centrifuging for 10 minutes at a rotational speed of 2500×g, and obtaining limonin precipitation. Compared with a traditional method, the raw material in the present invention can directly use the extract liquid or juicing liquid without drying, and recover most limonin in water using a precipitation method without complicated apparatus, and is easy to operate and has a low process cost.

Abstract translation: 一种柠檬苦素提取方法，包括以下步骤：第一步，原料提取或榨汁：将原料直接浸泡在水中或使用压榨机直接将原料榨汁获得提取物; 第二步，加盐调节pH：向提取物中加入硫酸固体物质或饱和硫酸盐溶液; 调节pH至3-7; 第三步，加热保温：加热至20°C-100°C，并保温10分钟至110分钟; 第四步，离心：以2500×g的转速离心10分钟，得到柠檬苦素沉淀。 与传统方法相比，本发明的原料可以直接使用提取液或榨汁液而不干燥，并且使用无复杂装置的沉淀法在水中回收大多数柠檬苦素，易于操作且工艺成本低 。

公开(公告)号：US08969617B2

公开(公告)日：2015-03-03

申请号：US13675574

申请日：2012-11-13

Applicant: Kaohsiung Medical University

Inventor： Chun-Nan Lin ,  Dravidum Maitraie ,  Jih-Pyang Wang ,  Chi-Feng Hung ,  Huang-Yao Tu ,  Ya-Ting Liou ,  Bai-Luh Wei ,  Shyh-Chyun Yang

IPC: C07C61/12 ,  C07C69/74 ,  C07D313/06 ,  A61K31/19 ,  A61K31/215 ,  A61K31/335 ,  C07D313/08 ,  C07J63/00 ,  C07J73/00 ,  C07C231/02 ,  C07C231/12

CPC classification number: C07D313/06 ,  A61K31/19 ,  A61K31/215 ,  A61K31/335 ,  C07C231/02 ,  C07C231/12 ,  C07D313/08 ,  C07J63/008 ,  C07J73/003

Abstract: The present invention provides a chemical compound having the structure being one selected from a group consisting of wherein R1 is one selected from a group consisting of COOCH3, COOCH2Ph, CONHCH(CH3)2 and CONHC6H5, R2 is one selected from a group consisting of H, CH3 and CH(CH3)2, R3 is one selected from a group consisting of H, CH3, CH(CH3)2 and CH2Ph, and R4 is one of CH(CH3)2 and C6H5.

Abstract translation: 本发明提供一种具有以下结构的化合物：其中R 1为选自COOCH 3，COOCH 2 Ph，CONHCH（CH 3）2和CONHC 6 H 5中的一个，R 2为选自H ，CH 3和CH（CH 3）2，R 3是选自H，CH 3，CH（CH 3）2和CH 2 Ph的一个，R 4是CH（CH 3）2和C 6 H 5之一。