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1. 发明授权

US12042541B2 Lipids and compositions for the delivery of therapeutics 有权
公开(公告)号：US12042541B2
公开(公告)日：2024-07-23
申请号：US18194540
申请日：2023-03-31
申请人： ARBUTUS BIOPHARMA CORPORATION
发明人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
IPC分类号： A61K47/44 , A61K9/127 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/11 , C12N15/113
CPC分类号： A61K47/44 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/111 , C12N15/113 , A61K2039/55555 , A61K2039/55561 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/30
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structure

wherein:

R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alkylhetrocycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).

2. 发明授权

US11952351B2 Lipid particle, composition comprising lipid particle, and method for delivering activators to cell 有权
公开(公告)号：US11952351B2
公开(公告)日：2024-04-09
申请号：US18059765
申请日：2022-11-29
申请人： KABUSHIKI KAISHA TOSHIBA
发明人： Mitsuko Ishihara , Eiichi Akahoshi , Katsuyuki Naito , Emi Nozaki , Saeko Saruwatari
IPC分类号： C07D243/08 , A61K9/127 , C07C229/30 , C07D211/14 , C07D233/02 , C07D241/04 , A61K31/7088
CPC分类号： C07D243/08 , A61K9/1271 , C07C229/30 , C07D211/14 , C07D233/02 , C07D241/04 , A61K31/7088
摘要： The present embodiment provides a compound represented by the formula (1):

Q-CHR2 (1)

(Q is a nitrogen-containing aliphatic group containing two or more tertiary nitrogens but no oxygen, and R is an aliphatic group containing a biodegradable group). From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

3. 发明申请

US20220162171A1 COMPOSITIONS AND METHODS FOR THE TREATMENT OF GASTROINTESTINAL POLYPS 有权
公开(公告)号：US20220162171A1
公开(公告)日：2022-05-26
申请号：US17457398
申请日：2021-12-02
申请人： Cellix Bio Private Limited
发明人： Mahesh Kandula
IPC分类号： C07D239/94 , C07C229/30 , C07C229/62 , C07C317/44
摘要： The disclosures herein provide compounds of formula I, formula II, formula III, formula IV, formula V and formula VI or its pharmaceutical acceptable salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, lozenge, spray, intravenous, oral solution, buccal mucosal layer tablet, parenteral administration, syrup, or injection. Such compositions may be used to treatment of gastrointestinal polyps or its associated complications.

4. 发明授权

US11246844B2 Methods for inhibiting conversion of choline to trimethylamine (TMA) 有权
公开(公告)号：US11246844B2
公开(公告)日：2022-02-15
申请号：US15609791
申请日：2017-05-31
申请人： The Procter & Gamble Company , The Cleveland Clinic Foundation
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):

5. 发明授权

US11081729B2 Non-aqueous electrolyte solution additive, and non-aqueous electrolyte solution for lithium secondary battery and lithium secondary battery which include the same 有权
公开(公告)号：US11081729B2
公开(公告)日：2021-08-03
申请号：US16340269
申请日：2018-07-06
申请人： LG Chem, Ltd.
发明人： Hyun Seung Kim , Sung Hoon Yu , Jeong Woo Oh , Chul Haeng Lee
IPC分类号： H01M10/0567 , C07C229/30 , C07D207/16 , C07D211/60 , C07D233/90 , C07D241/04 , C07D295/145 , H01M4/505 , H01M4/525 , H01M10/0525 , H01M10/0568 , H01M10/0569 , H01M4/02
摘要： The present invention relates to a non-aqueous electrolyte solution additive, and a non-aqueous electrolyte solution for a lithium-ion battery and a lithium-ion battery which include the same, and particularly, to a non-aqueous electrolyte solution, which may remove an acid generated by the decomposition of a lithium salt while being able to suppress the dissolution of metal impurities causing failure in the battery by using and including a Lewis base compound containing a propargyl group as a non-aqueous electrolyte solution additive for a lithium-ion battery, and a lithium secondary battery in which transition metal dissolution in a positive electrode and a low-voltage phenomenon are improved.

6. 发明授权

US10307378B2 Diester and triester based low molecular weight, biodegradeable cationic lipids for oligonucleotide delivery 有权
公开(公告)号：US10307378B2
公开(公告)日：2019-06-04
申请号：US15827162
申请日：2017-11-30
申请人： SIRNA THERAPEUTICS, INC.
发明人： Steven L. Colletti , Matthew G. Stanton
IPC分类号： A61K9/51 , C07F7/18 , A61K47/60 , C12N15/11 , A61K31/713 , C07C229/12 , C07C229/28 , C07C229/30 , C12N15/113
摘要： The instant invention provides for novel cationic lipids of Formula A that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain coupled with inclusion of hydrolysable functionality in the lipid chains to enhance the efficiency and tolerability of in vivo delivery of siRNA.

7. 发明申请

US20180346408A1 LIPID COMPOUNDS AND COMPOSITIONS AND THEIR OPTHALMIC USE 审中-公开
公开(公告)号：US20180346408A1
公开(公告)日：2018-12-06
申请号：US15779829
申请日：2016-11-30
申请人： BIOZEP AS
发明人： Anne Kristin Holmeide
IPC分类号： C07C229/22 , C07C229/30 , C07C323/52 , C07C323/54 , C07C323/58 , C07C59/76 , C07C59/60 , C07C59/56 , C07C57/52 , C07C57/03 , C07C233/09 , A61P27/12 , A61P27/06
CPC分类号： C07C229/22 , A61K31/16 , A61K31/202 , A61P27/06 , A61P27/12 , C07C57/02 , C07C57/03 , C07C57/52 , C07C59/42 , C07C59/56 , C07C59/58 , C07C59/60 , C07C59/76 , C07C229/30 , C07C233/09 , C07C323/52 , C07C323/54 , C07C323/58
摘要： The invention relates to lipid compounds of formula (I) and their pharmaceutically acceptable salts for the prevention and/or treatment of ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases: (I) (wherein R1 is either a C9 to C22 alkyl group, or a C9 to C22 alkenyl group having from 1 to 6 double bonds; R2 is selected from the group consisting of a halogen atom, a hydroxy group, an alkyl group, an alkoxy group, an alkylthio group, a carboxy group, an acyl group, an amino group, and an alkylamino group; R3 is a hydrogen atom, or a group R2; R4 is a carboxylic acid or a derivative thereof; and X is methylene (—CH2—), or an oxygen or sulfur atom).

8. 发明申请

US20180342769A1 ELECTROLYTIC SOLUTION, METHOD FOR PREPARING ESTER COMPOUND CONTAINED THEREIN AND LITHIUM SECONDARY CELL 审中-公开
公开(公告)号：US20180342769A1
公开(公告)日：2018-11-29
申请号：US16050544
申请日：2018-07-31
申请人： NEC Corporation
发明人： Masahiro SUGURO , Midori SHIMURA
IPC分类号： H01M10/0567 , C07D295/145 , C07C67/347 , C07C69/734 , C07C227/08 , C07C227/10 , H01M10/0525 , H01M4/134 , H01M4/133 , C07C67/31 , C07D295/14 , C07D211/10 , C07D207/20 , C07C229/30 , H01M4/587 , H01M4/38 , H01M4/02
摘要： Provided is a lithium secondary cell which has high capacity, suppresses deterioration in capacity and improves cycle characteristics particularly when used in high-temperature environments and has long lifespan. Provided is a lithium secondary cell including a positive electrode active material layer containing a positive electrode active material, a negative electrode active material layer containing a negative electrode active material and an electrolytic solution for immersing the positive and negative electrode active material layers, wherein the electrolytic solution contains at least one certain ester compound.

9. 发明授权

US09567422B2 Acetoacetoxy and enamine compounds and coatings therefrom 有权
标题翻译：乙酰乙酰氧基和烯胺化合物及其涂料
公开(公告)号：US09567422B2
公开(公告)日：2017-02-14
申请号：US13577039
申请日：2011-02-04
申请人： Dean C. Webster , Thomas J. Nelson , Xiao Pan
发明人： Dean C. Webster , Thomas J. Nelson , Xiao Pan
IPC分类号： C07C229/30 , C07H15/04 , C09D105/00 , C08G16/02 , C08G2/12 , C08G12/06 , C09D161/00
CPC分类号： C08G16/0212 , C08G2/12 , C08G12/06 , C09D161/00
摘要： The invention relates to enamine resins which are the reaction products of a) an acetoacetylated resin, and a C1-C20 alkyl amine or a mixture of C1-C20 alkyl amines. The acetoacetylated resin is the reaction product of a polyol having 4 or more hydroxyl groups; and at least one acetoacetate. The invention also relates to an acetoacetylated resin which is the reaction product of a polyol having 4 or more hydroxyl groups and at least one acetoacetate, where a portion of the hydroxyl groups of the polyol are replaced by acetoacetate groups and the remaining hydroxyl groups are replaced by a saturated monofunctional carboxylic acid ester, unsaturated monofunctional carboxylic acid ester, or a mixture thereof; as well as to enamine resins prepared from these acetoacetylated resins. The invention also relates to curable coating compositions containing such resins or a mixture of those resins, at least one metallic drier compound; and optionally one or more solvents.
摘要翻译：本发明涉及烯胺树脂，其是a）乙酰乙酰化树脂和C 1 -C 20烷基胺或C 1 -C 20烷基胺的混合物的反应产物。乙酰乙酰化树脂是具有4个以上羟基的多元醇的反应产物; 和至少一种乙酰乙酸酯。本发明还涉及乙酰乙酰化树脂，其是具有4个或更多个羟基和至少一个乙酰乙酸酯的多元醇的反应产物，其中多羟基的一部分羟基被乙酰乙酸酯基团取代并且剩余的羟基被替换饱和单官能羧酸酯，不饱和单官能羧酸酯或其混合物; 以及烯化由这些乙酰乙酰化树脂制备的树脂。本发明还涉及含有这些树脂的可固化涂料组合物或这些树脂的混合物，至少一种金属干燥剂化合物; 和任选的一种或多种溶剂。

10. 发明授权

US09518014B2 Process for synthesis of ezetimibe and intermediates used in said process 有权
标题翻译：合成所有方法中所用的依泽替米贝和中间体的合成方法
公开(公告)号：US09518014B2
公开(公告)日：2016-12-13
申请号：US14415891
申请日：2013-01-29
申请人： SHANGHAI INSTITUTE OF ORGANIC CHEMISTRY, CHINESE ACADEMY OF SCIENCES
发明人： Kuiling Ding , Xiaoming Wang , Zheng Wang
IPC分类号： C07C229/34 , C07D205/08 , C07D205/04 , C07C67/08 , C07C68/00 , C07C69/734 , C07C69/96 , C07C227/32 , C07C227/16 , C07F9/50 , C07F15/00 , C07C67/343 , C07C67/31 , C07C227/18 , C07C229/30
CPC分类号： C07D205/04 , C07C67/08 , C07C67/31 , C07C67/343 , C07C68/00 , C07C69/734 , C07C69/96 , C07C227/16 , C07C227/18 , C07C227/32 , C07C229/30 , C07C229/34 , C07C2601/16 , C07D205/08 , C07F9/5045 , C07F15/0033
摘要： A process for the production of ezetimibe and intermediates used in said process are disclosed. A kind of Morita-Baylis-Hillman adduct can be altered to chiral carboxylic acid derivatives of β-arylamino α-methylene with high activity and selectivity by means of ally lamination reaction, and the above carboxylic acid derivatives of β-arylamino α-methylene can be altered to the chiral intermediates of ezetimibe by means of simple conversion and further synthesized into the chiral drug ezetimibe. The synthesis route introduces chirality through the use of a chiral catalysis method, thereby avoiding the use of the chiral auxiliary oxazolidinone; and the route is economical and eco-friendly.
摘要翻译：公开了用于生产所述方法中使用的依泽替米贝和中间体的方法。一种Morita-Baylis-Hillman加合物可以通过烯丙基层压反应改变成具有高活性和选择性的β-芳基氨基α-亚甲基的手性羧酸衍生物，并且上述β-芳基氨基α-亚甲基的羧酸衍生物通过简单转化将其改变为依泽替米贝的手性中间体，并进一步合成为手性药物依泽替米贝。合成路线通过使用手性催化方法引入手性，从而避免使用手性辅助恶唑烷酮; 路线经济，环保。

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