公开(公告)号：US20230097090A1

公开(公告)日：2023-03-30

申请号：US17634516

申请日：2020-08-14

申请人： ACUITAS THERAPEUTICS, INC.

发明人： Ying K. TAM ,  Paulo Jia Ching LIN ,  Sean SEMPLE ,  Christopher J. BARBOSA

IPC分类号： A61K9/51 ,  C07C235/08 ,  A61K31/7105

摘要： Lipid nanoparticles having improved properties are provided. Use of the lipid nanoparticles for delivery of a therapeutic agent to primates for treatment of various indications is also described.

公开(公告)号：US20220234997A1

公开(公告)日：2022-07-28

申请号：US17458976

申请日：2021-08-27

申请人： VMI Foundation

发明人： Tappey H. Jones

IPC分类号： C07C235/74 ,  A01N37/18 ,  A01N37/36 ,  A01N37/42 ,  C07C233/18 ,  C07C235/08

摘要： Methods and compositions for pest control, and more particularly for control of ants, e.g., of the subfamily Myrmicinae, using tyramides.

公开(公告)号：US11274073B2

公开(公告)日：2022-03-15

申请号：US16608841

申请日：2018-05-10

申请人： ANTALGENICS, S.L.

发明人： Isabel Devesa Giner ,  Armando Genazzani ,  Tracey Pirali ,  Asia Fernandez Carvajal ,  Antonio Vicente Ferrer Montiel

IPC分类号： C07C235/08 ,  C07C231/06 ,  A61P29/00 ,  A61P17/04

摘要： The present invention relates to TRPV1 modulator compounds of formula (I) or their pharmaceutically, veterinary or cosmetically acceptable salts, or their stereoisomers or mixtures thereof, wherein m is an integer selected from 1 to 3; R1, R2, R6 and R6′ are independently selected from H, (C1-C8)alkyl, unsaturated (C2-C8)hydrocarbon, and (C3-C6)cycloalkyl, being these groups optionally substituted; R3 is hydrogen or halogen; R4 is selected from H, (C1-C8)alkyl, unsaturated (C2-C8)hydrocarbon, (C3-C6)cycloalkyl, (C6-C12)aryl, and (C5-C12)heteroaryl, being these groups optionally substituted; and R5 is selected from (C3-C28)alkyl, unsaturated (C3-C28)hydrocarbon, (C6-C12)aryl, and (C5-C12)heteroaryl, being these groups optionally substituted. It also relates to a process for their preparation, to pharmaceutical, veterinary or cosmetic compositions containing them, and to their pharmaceutical, veterinary and cosmetic applications.

公开(公告)号：US11198898B2

公开(公告)日：2021-12-14

申请号：US16131798

申请日：2018-09-14

申请人： CORNELL UNIVERSITY

发明人： Jeremy Baskin ,  Timothy Bumpus ,  Dongjun Liang

IPC分类号： C12Q1/42 ,  C07C233/60 ,  C07C33/05 ,  C07C43/196 ,  C07C235/08 ,  C07D321/12 ,  C07D313/18

摘要： A method for detecting phospholipase D (PLD) activity in a cell, comprising: (i) stimulating endogenous PLD in said cell for said PLD to catalyze a transphosphatidylation reaction between phosphatidylcholine or a derivative thereof and an exogenous functionalized alcohol to form a phosphatidyl alcohol, wherein the functionalized alcohol possesses a first functional group that can react with and form a bond to a functionalized detectable label having a second functional group reactive with the first functional group, and said phosphatidyl alcohol contains said first functional group in available form; (ii) reacting said phosphatidyl alcohol with said functionalized detectable label under conditions where said functionalized detectable label reacts, via its second functional group, with the first functional group to form a linkage between said detectable label and said phosphatidyl alcohol so as to form a labeled phosphatidyl alcohol containing said detectable label; and (iii) detecting said labeled phosphatidyl alcohol.

公开(公告)号：US11013696B2

公开(公告)日：2021-05-25

申请号：US16537934

申请日：2019-08-12

申请人： Novartis AG

发明人： Luis Brito ,  Delai Chen ,  Gabriel Grant Gamber ,  Andrew Geall ,  Kevin Love ,  Thomas Zabawa ,  Frederic Zecri

IPC分类号： C07D319/06 ,  C07C219/06 ,  C07C229/12 ,  C07D207/12 ,  C07D207/16 ,  C07D211/22 ,  C07D211/62 ,  C07C323/52 ,  A61K31/7105 ,  A61K31/713 ,  C07C219/16 ,  C07D233/60 ,  C07D295/088 ,  C12N15/88 ,  A61K9/51 ,  A61K9/127 ,  A61K47/18 ,  A61K38/18 ,  A61K38/22 ,  A61K39/12 ,  C07C235/08 ,  C07D211/06 ,  C07D211/46 ,  C07D233/64 ,  C07D295/13 ,  C12N7/00 ,  C12N15/113 ,  A61K39/00

摘要： This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R3, n, p, L1 and L2 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

公开(公告)号：US10995004B2

公开(公告)日：2021-05-04

申请号：US16336709

申请日：2017-09-29

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

发明人： Keir Cajal Neuman ,  Ganesh Shenoy ,  Chandrasekhar Mushti ,  Rolf E. Swenson

IPC分类号： C01B32/28 ,  C07C51/347 ,  C07C59/125 ,  C07C231/12 ,  C07C235/08 ,  C07C327/30 ,  C07D207/448 ,  C07D225/08 ,  C07D239/47 ,  C07D473/18 ,  B82Y30/00 ,  B82Y40/00

摘要： A method of increasing a density of carboxylic acids on a surface of a carbon nanoparticle is disclosed. The method includes contacting an oxygen-containing functional group on a surface of a carbon nanoparticle with a reducing agent to provide a hydroxyl group; reacting the hydroxyl group with a diazoacetate ester in the presence of a transition metal catalyst to provide an ester, the diazoacetate ester having the structure wherein R is a C1-8 hydrocarbyl, preferably tert-butyl, methyl, ethyl, isopropyl, allyl, benzyl, pentafluorophenyl, or N-succinimidyl; and cleaving the ester to provide a carboxylic acid group. Surface-functionalized carbon nanoparticles made by the method are also disclosed.

公开(公告)号：US10308594B2

公开(公告)日：2019-06-04

申请号：US14781242

申请日：2014-04-18

申请人： ADESSO ADVANCED MATERIALS WUXI CO., LTD.

发明人： Bing Qin ,  Xin Li ,  Bo Liang

IPC分类号： B32B27/26 ,  B32B27/38 ,  B32B27/04 ,  C08G59/50 ,  C08J5/24 ,  C07C43/30 ,  C07C235/00 ,  C07C235/08 ,  C07C243/00 ,  C07C243/24 ,  C07C243/26 ,  C07C243/28 ,  C07C243/38 ,  C07C217/84 ,  C08J11/16 ,  C08J11/26 ,  C07C201/12 ,  C07C213/02 ,  C07C241/02 ,  C08G59/14 ,  C08K7/06 ,  C08L63/00 ,  C09J9/00 ,  C09J163/00

摘要： The present invention provides, among others, compounds of Formula (I) or a salt thereof, methods for making these compounds, degradable polymers and reinforced composites made therefrom, and methods for degrading and/or recycling the degradable polymers and reinforced composites.

公开(公告)号：US20180297938A1

公开(公告)日：2018-10-18

申请号：US15985614

申请日：2018-05-21

申请人： Nitto Denko Corporation

发明人： Yoshiro Niitsu ,  Joseph E. Payne ,  John A. Gaudette ,  Zheng Hou ,  Victor Knopov ,  Richard P. Witte ,  Mohammad Ahmadian ,  Loren A. Perelman ,  Yasunobu Tanaka ,  Violetta Akopian

IPC分类号： C07C237/22 ,  C07C235/48 ,  A61K47/55 ,  A61K9/127 ,  A61K31/713 ,  C07C233/21 ,  C07C235/08 ,  C12N15/113 ,  C07F9/10 ,  A61K31/07

摘要： Here described are compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including these compounds which are useful for the targeting and delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.

公开(公告)号：US09522192B2

公开(公告)日：2016-12-20

申请号：US14103463

申请日：2013-12-11

申请人： EPITECH GROUP S.r.l.

发明人： Antonio Calignano ,  Giuseppe D'Agostino ,  Sonia Laneri ,  Rosaria Meli ,  Carmine Ostacolo ,  Roberto Russo ,  Antonia Sacchi ,  Diana Tronino ,  Francesco Della Valle ,  Maria Federica Della Valle ,  Gabriele Marcolongo

IPC分类号： A61K31/164 ,  C07C235/08 ,  A61K47/48 ,  C07C231/12 ,  C07C235/20 ,  C08G59/00

CPC分类号： A61K47/48215 ,  A61K31/164 ,  A61K47/60 ,  C07C231/12 ,  C07C235/20 ,  C08G65/332 ,  C08G65/33324 ,  C08L2203/02

摘要： The synthesis of a series of Polyethylene glycol conjugates (esters and carbonates) of PEA and its analogous acylethanolamides, have higher water solubility and good hydrophilic/lipophilic balance, resulting in (i) improved accumulation in tissues (particularly skin and mucosae), (ii) prolonged release, and (iii) increased bioavailability. Improvement of PEA and analogous acylethanolamides levels in the tissues—particularly in the skin and mucosae—and their prolonged release is due to the improved bioavailability of related conjugates. Conjugates are able to extend the time frame in which PEA and analogous acylethanolamides exert their pharmacological effects.

摘要翻译： 一系列聚乙二醇共轭物（酯和碳酸酯）的一系列PEA及其类似的酰基乙醇酰胺的合成具有较高的水溶性和良好的亲水/亲油平衡，导致（i）改善组织（特别是皮肤和粘膜）中的积累，（ii ）延长释放，和（iii）增加的生物利用度。 组织中特别是皮肤和粘膜中PEA和类似的乙酰乙酰胺水平的改善及其延长的释放是由于相关缀合物的生物利用度得到改善。 共轭物能够延长PEA和类似的乙酰乙酰胺发挥其药理作用的时间框架。

公开(公告)号：US09458088B2

公开(公告)日：2016-10-04

申请号：US14631763

申请日：2015-02-25

申请人： Acucela Inc.

发明人： Ian L. Scott ,  Vladimir A. Kuksa ,  Mark W. Orme ,  Thomas L. Little, Jr. ,  Anna Gall ,  Feng Hong

IPC分类号： C09B11/02 ,  C07C217/20 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  C07C217/72 ,  C07C225/16 ,  C07C229/38 ,  C07C233/18 ,  C07C235/08 ,  C07C251/86 ,  C07C279/08 ,  C07C317/28 ,  C07C323/25 ,  C07D277/24 ,  C07D309/06 ,  C07C215/20 ,  C07C309/06 ,  C07C217/84 ,  C07C323/33

CPC分类号： A61K31/137 ,  A61K31/165 ,  A61K31/222 ,  C07C215/20 ,  C07C217/20 ,  C07C217/60 ,  C07C217/62 ,  C07C217/64 ,  C07C217/72 ,  C07C217/84 ,  C07C225/16 ,  C07C229/38 ,  C07C233/18 ,  C07C235/08 ,  C07C251/86 ,  C07C279/08 ,  C07C309/06 ,  C07C317/28 ,  C07C323/25 ,  C07C323/33 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/42 ,  C07D277/24 ,  C07D309/06

摘要： The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.