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1. 发明公开

US20240246898A1 CATIONIC LIPIDS FOR NUCLEIC ACID DELIVERY AND PREPARATION THEREOF 审中-公开
公开(公告)号：US20240246898A1
公开(公告)日：2024-07-25
申请号：US18489240
申请日：2023-10-18
申请人： RAMOT AT TEL-AVIV UNIVERSITY LTD.
发明人： Dan PEER , Srinivas RAMISHETTI
IPC分类号： C07C211/22 , A61K47/18 , A61K48/00 , A61P29/00 , A61P35/00 , C07C59/01 , C07C215/08 , C07C219/04 , C07C229/02 , C07C229/10 , C07C229/12 , C07C233/00 , C07C243/00 , C07C243/10 , C07C243/14 , C07C243/16 , C07C243/26 , C07C243/28 , C07C279/04 , C07C333/10 , C07D233/64 , C07D295/13 , C07D295/15 , C12N15/113
CPC分类号： C07C211/22 , A61K47/18 , A61K48/00 , A61P29/00 , A61P35/00 , C07C59/01 , C07C215/08 , C07C219/04 , C07C229/02 , C07C229/10 , C07C229/12 , C07C233/00 , C07C243/00 , C07C243/10 , C07C243/14 , C07C243/16 , C07C243/26 , C07C243/28 , C07C279/04 , C07C333/10 , C07D233/64 , C07D295/13 , C07D295/15 , C12N15/113 , C12N2310/14
摘要： The present invention provides cationic lipids and lipid nanoparticle formulations comprising these lipids, alone or in combination with other lipids. These lipid nanoparticles may be formulated with nucleic acids to facilitate their intracellular delivery both in vitro and for therapeutic applications. The present invention also provides methods of chemical synthesis of these lipids, lipid nanoparticle preparation and formulation with nucleic acids.

2. 发明申请

US20230100940A1 DNP and DNP Prodrug Treatment of Neuromuscular, Neurodegenerative, Autoimmune, Developmental, Traumatic Brain Injury, Concussion, Dry Eye Disease, Hearing Loss and/or Metabolic Diseases 有权
公开(公告)号：US20230100940A1
公开(公告)日：2023-03-30
申请号：US17840436
申请日：2022-06-14
申请人： MITOCHON PHARMACEUTICALS, INC. , BIOVENTURES, LLC
发明人： John Gerard Geisler , Robert Alonso , Peter Anthony Crooks , Narsimha Reddy Penthala , Zaineb Albayati
IPC分类号： A61K31/5375 , A61K31/4453 , A61K31/495 , A61K31/06 , A61K31/4409 , C07C323/58 , C07F9/12 , A61K31/40 , A61K31/265 , A61K31/27 , C07C205/37 , A61K31/223 , A61K31/4406 , A61K31/661 , C07F9/09 , A61K31/221 , C07C271/44 , C07C219/04 , C07C271/52 , C07C229/26 , A61K31/44 , A61K31/4402 , C07C229/08 , C07C229/22
摘要： A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.01 mg/kg of body weight to about 50 mg/kg of body weight of the patient in need of treatment. A dose of the composition for treatment of metabolic diseases may be from about 1 mg/70 kg of body weight to about 100 mg/70 kg of body weight of the patient in need of treatment, and a maximum dose per day is about 200 mg/70 kg of body weight of the patient in need of treatment.

3. 发明授权

US11406642B2 DNP and DNP prodrug treatment of neuromuscular, neurodegenerative, autoimmune, developmental, traumatic brain injury, concussion, dry eye disease, hearing loss and/or metabolic diseases 有权
公开(公告)号：US11406642B2
公开(公告)日：2022-08-09
申请号：US16695653
申请日：2019-11-26
申请人： MITOCHON PHARMACEUTICALS, INC. , BIOVENTURES, LLC
发明人： John Gerard Geisler , Robert Alonso , Peter Anthony Crooks , Narsimha Reddy Penthala , Zaineb Albayati
IPC分类号： A61K31/5375 , A61K31/4453 , A61K31/495 , A61K31/06 , A61K31/4409 , C07C323/58 , C07F9/12 , A61K31/40 , A61K31/265 , A61K31/27 , C07C205/37 , A61K31/223 , A61K31/4406 , A61K31/661 , C07F9/09 , A61K31/221 , C07C271/44 , C07C219/04 , C07C271/52 , C07C229/26 , A61K31/44 , A61K31/4402 , C07C229/08 , C07C229/22 , C07D295/145 , C07D295/088 , C07D295/205 , C07D213/40 , C07D295/13
摘要： A composition and method of treatment of neuromuscular, neuromuscular degenerative, neurodegenerative, autoimmune, developmental, traumatic, hearing loss related, and/or metabolic diseases, including spinal muscular atrophy (SMA) syndrome (SMA1, SMA2, SMA3, and SMA4, also called Type I, II, III and IV), traumatic brain injury (TBI), concussion, keratoconjunctivitis sicca (Dry Eye Disease), glaucoma, Sjogren's syndrome, rheumatoid arthritis, post-LASIK surgery, anti-depressants use, Wolfram Syndrome, and Wolcott-Rallison syndrome. The composition is selected from the group consisting of 2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP, bipartite 2,3-dinitrophenol, 2,4-dinitrophenol, 2,5-dinitrophenol, 2,6-dinitrophenol, 3,4-dinitrophenol, or 3,5-dinitrophenol (2,3-DNP, 2,4-DNP, 2,5-DNP, 2,6-DNP, 3,4-DNP, or 3,5-DNP) prodrugs; Gemini prodrugs, bioprecursor molecules, and combinations thereof. A dose of the composition for treatment of neurodegenerative diseases may be from about 0.01 mg/kg of body weight to about 50 mg/kg of body weight of the patient in need of treatment. A dose of the composition for treatment of metabolic diseases may be from about 1 mg/70 kg of body weight to about 100 mg/70 kg of body weight of the patient in need of treatment, and a maximum dose per day is about 200 mg/70 kg of body weight of the patient in need of treatment.

4. 发明授权

US09624160B2 Reactive ionic liquids 有权
公开(公告)号：US09624160B2
公开(公告)日：2017-04-18
申请号：US14620861
申请日：2015-02-12
申请人： BASF SE
发明人： Michael Schmidt , Nikolai (Mykola) Ignatyev , William-Robert Pitner
IPC分类号： C07C229/12 , C07C211/63 , C07C219/04 , C07C225/06 , C07C309/06 , C07C309/65 , C07F9/28 , C07D207/08 , C07D211/14 , C07D263/04 , C07D295/037 , C07C229/08 , C07C255/25 , C07C311/48 , C07C317/04 , C07D295/088 , C07D295/108 , C07D295/145 , C07F9/54 , C07F9/6568 , H01B1/12 , H01M10/052 , H01M10/0569 , H01G11/06 , H01G11/58 , C07F9/30 , H01G11/60 , H01G11/62 , H01G11/64 , H01M10/0567 , H01M10/0568 , H01M10/0525
CPC分类号： C07C229/12 , C07C211/63 , C07C219/04 , C07C225/06 , C07C229/08 , C07C255/25 , C07C309/06 , C07C309/65 , C07C311/48 , C07C317/04 , C07D207/08 , C07D211/14 , C07D263/04 , C07D295/037 , C07D295/088 , C07D295/108 , C07D295/145 , C07F9/28 , C07F9/301 , C07F9/5428 , C07F9/65688 , H01B1/122 , H01G11/06 , H01G11/58 , H01G11/60 , H01G11/62 , H01G11/64 , H01M10/052 , H01M10/0525 , H01M10/0567 , H01M10/0568 , H01M10/0569 , Y02E60/122 , Y02E60/13
摘要： The invention relates to reactive ionic liquids containing organic cations with groups or substituents which are susceptible to electrochemical reduction and anions obtained from fluoroalkyl phosphates, fluoroalkyl phosphinates, fluoroalkyl phosphonates, acetates, triflates, imides, methides, borates, phosphates and/or aluminates, for use in electrochemical cells, such as lithium ion batteries and double-layer capacitors.

5. 发明申请

US20030203852A1 Acyl pseudodipeptides which carry a functionalised auxialiary arm 失效
标题翻译：载有官能化辅助臂的酰基假二肽
公开(公告)号：US20030203852A1
公开(公告)日：2003-10-30
申请号：US10169053
申请日：2002-08-28
发明人： Jacques Bauer , Olivier Richard Martin , Sylvain Rodriguez
IPC分类号： C07F009/22 , C07F009/28 , A61K038/04 , C07C39/13 , C07C219/04 , A61K031/255 , A61K031/66
CPC分类号： A61K38/04 , A61K39/385 , A61K47/6811 , A61K2039/6018 , A61K2039/6037 , C07C237/22 , C07C323/60 , C07F9/091 , C07K5/04 , Y02A50/412
摘要： The present invention is directed in particular to dipeptide-like compounds derived from functionally substituted amino acids, having fatty acid chains bound thereto through amidification of the amine functional groups of said dipeptide-like compounds, one end portion of which bears an accessory functional side chain spacer, with the other end portion being an acid group either in neutral or charged state. Compounds of the present invention have immunomodulating properties like adjuvants, In addition, compounds of the invention can be grafted on a given antigen in order to modulate or tune the immune response or can be equally grafted on a pharmaceutical carrier to enhance the therapeutic effect or targetting thereof. Accordingly, compounds of the invention find use in human and veterinary medicine both as immunogens and diagnostic tools.
摘要翻译：本发明特别涉及衍生自功能取代的氨基酸的二肽样化合物，其具有通过所述二肽类化合物的胺官能团的酰胺化而结合的脂肪酸链，其一个末端部分具有辅助功能性侧链间隔物，另一端部分为中性或带电状态的酸基。本发明的化合物具有如佐剂的免疫调节特性。此外，本发明的化合物可以接枝在给定的抗原上以调节或调节免疫应答，或者可以同样地接枝在药物载体上以增强治疗效果或靶向其中。因此，本发明的化合物可用作人和兽医学作为免疫原和诊断工具。

6. 发明授权

US5798095A Hair treatment composition and method of making same 失效
标题翻译：头发处理组合物及其制造方法
公开(公告)号：US5798095A
公开(公告)日：1998-08-25
申请号：US648342
申请日：1996-05-15
申请人： Ernst Dieter Racky
发明人： Ernst Dieter Racky
IPC分类号： A61K8/00 , A61K8/04 , A61K8/34 , A61K8/36 , A61K8/365 , A61K8/368 , A61K8/40 , A61K8/41 , A61K8/49 , A61Q5/00 , A61Q5/02 , A61Q5/04 , A61Q5/06 , A61Q5/10 , C07C211/63 , C07C217/08 , C07C219/04 , C07C229/12 , C07D213/20 , C07D233/90 , C07D275/06 , A61K7/06
CPC分类号： A61K8/368 , A61K8/416 , A61K8/49 , A61Q5/00 , A61Q5/12
摘要： The hair treatment composition is free of anionic surfactant, has a pH of from 2 to 7 and includes a combination of 0.5 to 15 percent by weight of a surfactant component A) consisting of at least one water-soluble cationic surfactant and/or at least one water-soluble amphoteric surfactant and 0.05 to 5 percent by weight of a component B) consisting of benzoic acid or its physiologically compatible salts or saccharin or its physiologically compatible salts of saccharin with inorganic bases or a mixture of a physiologically compatible salt of saccharin and a physiologically compatible salt of benzoic acid. A weight ratio of surfactant component A) to component B) is from 2:1 to 1:10. A room-temperature method of making the hair treatment composition is also described. The viscosity of the hair treatment composition can be adjusted without difficulty. It improves the wet and dry combability of hair and reduces the electrostatic charge on dry hair without loading the hair after several applications.
摘要翻译：头发处理组合物不含阴离子表面活性剂，pH为2-7，包括0.5至15重量％的由至少一种水溶性阳离子表面活性剂组成的表面活性剂组分A）和/或至少一种水溶性两性表面活性剂和0.05至5重量％的组分B），其由苯甲酸或其生理相容的盐或糖精或其糖精的生理上相容的盐与无机碱或糖精的生理相容盐的混合物组成，生理上相容的苯甲酸盐。表面活性剂组分A）与组分B）的重量比为2:1至1:10。还描述了制备头发处理组合物的室温方法。毛发处理组合物的粘度可以毫无困难地调整。它改善了毛发的湿和干梳理性，并且减少了头发上的静电电荷，而不会在几次使用后加载头发。

7. 发明授权

US5008442A Surface-active compounds on the basis of arylated fatty substances and their use 失效
标题翻译：基于芳基化脂肪物质的表面活性化合物及其用途
公开(公告)号：US5008442A
公开(公告)日：1991-04-16
申请号：US854339
申请日：1986-04-21
申请人： Heinz Uhrig , Klaus Ehl , Reinhold Deubel
发明人： Heinz Uhrig , Klaus Ehl , Reinhold Deubel
IPC分类号： C07C69/66 , B01F17/00 , B01F17/42 , C07C41/00 , C07C41/02 , C07C43/178 , C07C43/20 , C07C43/205 , C07C51/00 , C07C59/125 , C07C67/00 , C07C219/04 , C07C227/00 , C07C229/12 , C07C301/00 , C07C305/10 , C07C309/03 , C07C309/62 , C08G65/26 , C09D7/45 , C11D1/72 , D06P1/60 , D06P1/613
CPC分类号： B01F17/0042 , B01F17/0028 , B01F17/0057 , C08G65/2615 , C09D7/02
摘要： A compound of the formulaA[(Y-O).sub.x - Y - Z].sub.min which A is the radical of an arylated fatty alcohol, Y are identical or different groups of the formulae--CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH(CH.sub.3)--,Z are identical or different radicals of the formulae --OH, --O--CO--CH.dbd.CH--COOM and --O--CO--CH.sub.2 --CH(SO.sub.3 M)--COOM,in whichM is a cation,x is an integer from 1 to 150, andm is a number from 1 to 7.

8. 发明授权

US4339391A Quaternary ammonium compounds 失效
标题翻译：季铵化合物
公开(公告)号：US4339391A
公开(公告)日：1982-07-13
申请号：US167202
申请日：1980-07-09
申请人： Erich Hoffmann , Wolfgang Wagemann , Gunther Tauber , Adolf May , Hans-Walter Bucking
发明人： Erich Hoffmann , Wolfgang Wagemann , Gunther Tauber , Adolf May , Hans-Walter Bucking
IPC分类号： C07C213/06 , C07C219/04 , C07C219/06 , C07C219/08 , C07C219/20 , C11D1/62 , C11D3/00 , D06M13/02 , D06M13/322 , D06M13/463 , C09F5/00
CPC分类号： C11D3/0015 , C11D1/62
摘要： Quaternary ammonium compounds of the formula 1 ##STR1## in which R is C.sub.8 -C.sub.30 -alkyl or alkenyl; R.sub.1 is alkyl, 2-hydroxyalkyl or alkenyl each having from 8 to 30 carbon atoms; R.sub.2 is C.sub.1 -C.sub.4 -alkyl or benzyl; A is a group of the formulae ##STR2## B is A or C.sub.1 -C.sub.4 -alkylene, X and Y are hydrogen or methyl with the proviso that X and Y are not simultaneously methyl; m is 1 or 2; n is a number of from 1 to 20; and A.sup.(-) is an anion; a process for the preparation thereof, and their use as fabric softeners.
摘要翻译：式1的季铵化合物（1）其中R是C 8 -C 30 - 烷基或链烯基; R1是具有8至30个碳原子的烷基，2-羟基烷基或烯基; R2是C1-C4烷基或苄基; A是下式的基团：B是A或C 1 -C 4 - 亚烷基，X和Y是氢或甲基，条件是X和Y不同时为甲基; m为1或2; n为1〜20的数; A（ - ）为阴离子; 其制备方法及其作为织物柔软剂的用途。

9. 发明授权

US4324739A Dimethylamino derivatives and their use 失效
公开(公告)号：US4324739A
公开(公告)日：1982-04-13
申请号：US135800
申请日：1980-03-31
申请人： Helmut Zondler , Roland Moser
发明人： Helmut Zondler , Roland Moser
IPC分类号： C08G59/00 , C07C67/00 , C07C213/00 , C07C217/08 , C07C217/12 , C07C219/04 , C07C239/00 , C07C253/00 , C07C255/13 , C07C255/17 , C07C269/00 , C07C271/28 , C07C275/04 , C07C275/14 , C07C275/16 , C07C275/28 , C08G59/40 , C08G59/44 , C08G59/50 , C08G59/52 , C09J163/00 , C07C121/417 , C07C121/46 , C07C121/52 , C07C121/66
CPC分类号： C07C275/28 , C07C275/14 , C07C275/16 , C08G59/4014 , C08G59/50 , C08G59/52
摘要： (Dimethylaminoalkyl)carboxylic and -carbamic acid esters and (dimethylaminoalkyl) ethers and ureas are compounds which are especially suitable for use as amine curing agents for polyepoxide compounds. They impart longer curing times to the curable mixtures and thus good processing properties, especially when the mixtures are used as adhesives. In addition, the mechanical properties are often improved. Further, these compounds afford advantages when used as curing agents on account of their low volatility.

10. 发明授权

US11420933B2 Lipids and lipid compositions for the delivery of active agents 有权
公开(公告)号：US11420933B2
公开(公告)日：2022-08-23
申请号：US17104294
申请日：2020-11-25
申请人： Novartis AG
发明人： Luis Brito , Delai Chen , Gabriel Gamber , Andrew Geall , Kevin Love , Thomas Zabawa , Frederic Zecri
IPC分类号： C07C229/12 , A61K47/18 , C07C229/38 , C07D205/04 , C07D265/30 , C07D207/12 , C07D207/16 , C07D211/22 , C07D295/088 , C07D211/46 , C07D211/60 , C07D211/62 , C07D295/15 , C07C271/20 , C07C219/04 , A61K9/127 , A61K9/51 , A61K31/7105 , A61K31/713 , A61K39/12 , A61K39/39 , C07C271/22 , C07D211/06 , C07D211/34 , C07D211/44 , A61K39/00
摘要： This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L1, n and p are defined herein. The compounds of formula (X) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.

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