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公开(公告)号:US12076306B2
公开(公告)日:2024-09-03
申请号:US18144890
申请日:2023-05-09
发明人: Tarek A. Zeidan , Scott Duncan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC分类号: C07C235/88 , A61K31/225 , C07C219/08 , C07C229/16 , C07C233/18 , C07C233/91 , C07C317/18 , C07C317/28 , C07D207/06 , C07D207/40 , C07D209/52 , C07D211/06 , C07D211/38 , C07D295/088 , C07D491/113
CPC分类号: A61K31/225 , C07C219/08 , C07C229/16 , C07C233/18 , C07C233/91 , C07C235/88 , C07C317/18 , C07C317/28 , C07D207/06 , C07D207/40 , C07D209/52 , C07D211/06 , C07D211/38 , C07D295/088 , C07D491/113
摘要: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
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公开(公告)号:US20230348360A1
公开(公告)日:2023-11-02
申请号:US18100596
申请日:2023-01-24
发明人: Gaofeng ZHA , Yuexiao HU , Xinghua PENG , Wanyin FANG
IPC分类号: C07C219/08 , C07D211/62 , A61K47/28
CPC分类号: C07C219/08 , C07D211/62 , A61K47/28
摘要: The disclosure belongs to the technical field of medical chemistry, particularly relates to an amino lipid and their preparation method as well as an application thereof, and provides the ionizable amino lipids with a general formula as shown in Formula (I), or pharmaceutically acceptable salts thereof. The amino lipids of the disclosure can be used for delivering nucleic acids and small molecule drugs. The amino lipid compounds have two ester bonds, which obviously enhance the lysosome escape capability of the ionizable amino lipids, and are favorable for the release of delivery targets of a targeted drug or gene, etc., thus improving the delivery efficiency, and showing the good capability of delivering nucleic acids into cells in the in-vitro and in-vivo delivery study.
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公开(公告)号:US11377511B2
公开(公告)日:2022-07-05
申请号:US17414980
申请日:2020-12-29
申请人: CHANGZHOU UNIVERSITY
发明人: Wenyan Huang , Qiujie Sun , Bibiao Jiang , Xiaoqiang Xue , Hongjun Yang , Li Jiang , Qimin Jiang
IPC分类号: C08F212/08 , C08F220/14 , C08F220/18 , C07C219/08
摘要: A reducing agent monomer for preparing a styrene-acrylic emulsion by an oxidation-reduction reaction at room temperature and a synthesis method thereof are disclosed. Maleic anhydride (MAH) and dimethylethanolamine (DMEA) are used as raw materials to synthesize the reducing agent monomer: 4-(2-(dimethylamino)ethoxy)-4-oxobut-2-enoic acid, and the synthesis method involves inexpensive easily-available raw materials, simple synthesis conditions, and easy purification. With the synthesized reducing agent monomer as a reducing agent, potassium persulfate (KPS) as an oxidizing agent, water as a dispersion medium, sodium dodecyl sulfate (SDS) as an emulsifier, and styrene, butyl acrylate (BA), and methylmethacrylate (MMA) as comonomers, free-radical microemulsion polymerization is conducted at room temperature to obtain a styrene-acrylic emulsion. In the synthesis of the styrene-acrylic emulsion, a monomer conversion rate is high, and a styrene-acrylic emulsion with a high molecular weight and a branched structure can be obtained at room temperature.
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公开(公告)号:US11246844B2
公开(公告)日:2022-02-15
申请号:US15609791
申请日:2017-05-31
发明人: Stanley Leon Hazen , Jose Carlos Garcia-Garcia , George Franklin Gerberick , John August Wos , Xiaodong Gu , Michael Reilly , Mark Robert Sivik , Jodie Michelle Reed , David Blair Cody
IPC分类号: A61K31/14 , C07D303/36 , A61K31/275 , C07C237/06 , A61K31/04 , C07C229/30 , C07C217/40 , C07D211/46 , C07C215/40 , C07C229/12 , C07C219/08 , C07D451/02 , A61K31/205 , C07C255/24 , C07C211/63 , C07C229/22 , C07C11/02 , C07C11/22 , C07C13/04 , C07C69/003 , C07C69/01 , C07C211/62 , C07C233/02 , C07C255/07 , C07D303/04
摘要: A method of inhibiting the conversion of choline to trimethylamine (TMA) and lowering TMAO by providing a composition comprising a compound set forth in Formula (I):
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公开(公告)号:US11083703B2
公开(公告)日:2021-08-10
申请号:US16790849
申请日:2020-02-14
发明人: Tarek A. Zeidan , Scott Duncan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC分类号: C07C235/88 , A61K31/225 , C07D491/113 , C07C317/28 , C07D211/38 , C07D295/088 , C07D207/40 , C07D211/06 , C07D207/06 , C07D209/52 , C07C317/18 , C07C219/08 , C07C229/16 , C07C233/18 , C07C233/91
摘要: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
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公开(公告)号:US20210154117A1
公开(公告)日:2021-05-27
申请号:US17256821
申请日:2019-06-21
申请人: BASF SE
发明人: Sophia EBERT , Bjoern LUDOLPH , Dawid MARCZEWSKI
IPC分类号: A61K8/46 , A61K8/41 , A61Q5/02 , A61Q19/10 , C07C303/32 , C07C309/31 , C07C219/08 , C07C219/06 , C08G59/50 , C11D11/00 , C11D3/34
摘要: The present invention relates to an esteramine salt according to the general formula (I): The substituents R1, R2 and R3 are defined below.
The present invention further relates to a process for preparing such an esteramine salt according to general formula (I), wherein a corresponding monocarboxylic acid or an ester thereof are reacted with an aminoalcohol and an at least equimolar amount of a sulfonic acid.-
公开(公告)号:US10723692B2
公开(公告)日:2020-07-28
申请号:US16132287
申请日:2018-09-14
发明人: Steven M. Ansell , Xinyao Du
IPC分类号: C07C229/24 , A61K9/127 , C07C219/10 , A61K47/18 , A61K47/22 , C07C219/06 , C07C219/08 , C07C229/16 , C07D295/13 , C08G65/333 , A61K38/48 , A61K47/24 , A61K47/28 , A61K48/00 , C07C235/06 , C07C227/16
摘要: Compounds are provided having the following structure: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5, R6, R7, R8, R9, L1, L2, a, b, c, d and e are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
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公开(公告)号:US20200016111A1
公开(公告)日:2020-01-16
申请号:US16524498
申请日:2019-07-29
发明人: Tarek A. Zeidan , Scott Duncan , Christopher P. Hencken , Thomas Andrew Wynn , Carlos N. Sanrame
IPC分类号: A61K31/225 , C07D491/113 , C07C317/28 , C07D211/38 , C07D295/088 , C07D207/40 , C07D211/06 , C07D207/06 , C07D209/52 , C07C317/18 , C07C219/08 , C07C229/16 , C07C233/18 , C07C233/91
摘要: The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.
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公开(公告)号:US20180369384A1
公开(公告)日:2018-12-27
申请号:US15596845
申请日:2017-05-16
发明人: Muthiah Manoharan , Kallanthottathil G. Rajeev , Muthusamy Jayaraman , David Butler , Mamta Kapoor , Rajesh Kumar Kainthan
IPC分类号: A61K47/18 , C12N15/88 , C07D491/10 , C07D317/72 , C07D317/44 , C07D317/28 , C07C323/25 , C07C271/20 , C07C271/12 , C07C251/40 , C07C229/12 , C07C219/08 , C07C217/08 , A61K47/22 , A61K31/713 , A61K31/7105
摘要: The present invention is based, in part, upon the discovery of charged lipids that provide advantages when used in lipid particles for the in vivo delivery of a therapeutic agent. As such, described herein are compounds useful for delivering a nucleic acid to a cell.
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公开(公告)号:US20180353434A1
公开(公告)日:2018-12-13
申请号:US15560854
申请日:2016-03-24
IPC分类号: A61K9/51 , A61K31/7088 , C07C219/08 , C07C211/63 , C07C215/08 , C07C217/28 , C07C271/16 , C07C229/06 , C07C233/20 , C07C237/08 , C07D451/14 , C12N15/113
CPC分类号: A61K9/5123 , A61K9/0019 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61P29/00 , A61P35/00 , C07C211/63 , C07C215/08 , C07C217/28 , C07C219/08 , C07C229/06 , C07C233/20 , C07C237/08 , C07C271/16 , C07D207/08 , C07D207/12 , C07D211/22 , C07D223/04 , C07D295/088 , C07D317/28 , C07D401/04 , C07D451/14 , C12N15/113 , C12N2310/14 , C12N2320/32 , C12N2320/51
摘要: The present invention provides nucleic acid-containing lipid nanoparticles containing a lipid (lipid A) which has a hydrophilic unit having a single quaternary ammonium group, and three independent, optionally substituted hydrocarbon groups, a lipid derivative or fatty acid derivative of a water-soluble polymer, and a nucleic acid.
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