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1. 发明授权

US11884627B2 Compounds and compositions for treating conditions associated with LPA receptor activity 有权
公开(公告)号：US11884627B2
公开(公告)日：2024-01-30
申请号：US18322492
申请日：2023-05-23
申请人： Lhotse Bio, Inc.
发明人： Wei Huang , Hui Lei , Zhongmiao Xu , Haizhen Zhang , Qiong Zhang
IPC分类号： C07D211/66 , C07C229/18 , C07C229/28 , C07D309/14 , C07D317/54 , C07C61/39 , C07D407/12 , C07D317/58
CPC分类号： C07D211/66 , C07C61/39 , C07C229/18 , C07C229/28 , C07D309/14 , C07D317/54 , C07D317/58 , C07D407/12 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/08
摘要： The present disclosure provides LPA antagonists, as well as pharmaceutical compositions comprising the compounds disclosed herein. Also provided are methods for treating LPA-associated diseases, disorders, and conditions.

2. 发明授权

US10487045B2 Adamantane derivative and use thereof 有权
公开(公告)号：US10487045B2
公开(公告)日：2019-11-26
申请号：US16072586
申请日：2017-01-26
申请人： TOHOKU UNIVERSITY , Brain Innovation Co., Inc.
发明人： Shigeki Moriguchi , Koji Fukunaga , Yoshiharu Iwabuchi
IPC分类号： C07C229/28 , C07C247/14 , C07C233/47 , C07D213/40 , A61K31/198 , A61K31/221 , A61K31/223 , A61K31/655 , A61P25/28 , A61P3/10 , A61P25/16
CPC分类号： C07C229/28 , A61K31/198 , A61K31/221 , A61K31/223 , A61K31/655 , A61P3/10 , A61P25/16 , A61P25/28 , C07C233/47 , C07C247/14 , C07D213/40
摘要： The present invention provides a pharmaceutical composition for treating or preventing a cognitive disease or disorder, containing a compound represented by Formula (I), an enantiomer thereof, a diastereomer thereof, or a pharmaceutically acceptable salt thereof.

4. 发明申请

US20170096449A1 Compositions and Methods Relating to Ionic Salts of Peptides 审中-公开
公开(公告)号：US20170096449A1
公开(公告)日：2017-04-06
申请号：US15333654
申请日：2016-10-25
申请人： Thetis Pharmaceuticals LLC
发明人： Gary Mathias , Banavara L. Mylari , Frank C. Sciavolino
IPC分类号： C07K5/068 , A23L33/12 , C07D213/80 , C07C53/134 , C07C57/03 , C07C229/28
CPC分类号： C07K5/06086 , A23L33/12 , A23V2002/00 , C07C51/412 , C07C53/134 , C07C57/02 , C07C57/03 , C07C229/28 , C07C237/12 , C07C317/04 , C07C2601/14 , C07D213/80 , C07K5/06095 , C07K7/08 , C11C3/00
摘要： The present invention relates to compounds of Formula I, compositions containing same, and methods of use.

5. 发明申请

US20160114042A1 AMINE-CONTAINING LIPIDOIDS AND USES THEREOF 有权
标题翻译：含胺的脂质体及其用途
公开(公告)号：US20160114042A1
公开(公告)日：2016-04-28
申请号：US14987717
申请日：2016-01-04
申请人： Massachusetts Institute of Technology
发明人： Daniel Griffith Anderson , Kathryn Ann Whitehead , Joseph R. Dorkin , Arturo Jose Vegas , Yunlong Zhang , Robert S. Langer
IPC分类号： A61K47/22 , C07D241/04 , C12N15/113 , C07D295/13
CPC分类号： A61K47/22 , A61K9/1272 , A61K9/5123 , A61K31/225 , A61K31/357 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/4985 , A61K31/573 , A61K31/704 , A61K31/713 , A61K45/06 , A61K47/18 , A61K47/542 , A61K47/543 , A61K47/6925 , C07C225/06 , C07C229/12 , C07C229/14 , C07C229/24 , C07C229/26 , C07C229/28 , C07C229/34 , C07C2601/14 , C07D207/09 , C07D211/14 , C07D211/26 , C07D211/34 , C07D241/04 , C07D295/13 , C07D295/15 , C07D295/16 , C07D319/16 , C07D319/18 , C07D487/04 , C12N15/111 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2320/32 , A61K2300/00
摘要： Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.
摘要翻译：本文提供的是可以通过将烷基胺偶联加成丙烯酸酯制备的类脂。在一些实施方案中，提供的类脂质是可生物降解的并且可以用于多种药物递送系统中。考虑到类固醇的氨基部分，除了其它药剂之外，它们非常适合于递送多核苷酸。已经制备了含有本发明的类脂和多核苷酸的纳米颗粒，并且已显示其在递送siRNA方面是有效的。

6. 发明申请

US20160107985A1 Compositions and Methods Relating to Ionic Salts of Peptides 审中-公开
标题翻译：关于离子盐的组成和方法
公开(公告)号：US20160107985A1
公开(公告)日：2016-04-21
申请号：US14772320
申请日：2015-05-04
申请人： THETIS PHARMACEUTICALS LLC
发明人： Gary Mathias , Banavara L. Mylari , Frank C. Sciavolino
IPC分类号： C07C237/12 , C07D213/80 , C07C317/04 , C07C57/02
CPC分类号： C07K5/06086 , A23L33/12 , A23V2002/00 , C07C51/412 , C07C53/134 , C07C57/02 , C07C57/03 , C07C229/28 , C07C237/12 , C07C317/04 , C07C2601/14 , C07D213/80 , C07K5/06095 , C07K7/08 , C11C3/00
摘要： The present invention relates to compounds of Formula I, compositions containing same, and methods of use.
摘要翻译：本发明涉及式I化合物，含有其的组合物和使用方法。

7. 发明申请

US20160060380A1 HYDROPHILIC POLYASPARTIC ESTERS 审中-公开
标题翻译：水溶性聚酯酯
公开(公告)号：US20160060380A1
公开(公告)日：2016-03-03
申请号：US14836144
申请日：2015-08-26
申请人： Bayer MaterialScience AG
发明人： Hans-Josef Laas , Michael Grahl , Olaf Fleck , Hans-Ulrich Meyer-Westhues , Michèl La Faille
IPC分类号： C08G18/34 , C09D175/02 , C08G18/77
CPC分类号： C09D175/02 , C07C229/24 , C07C229/28 , C07C2601/08 , C07C2601/14 , C08G18/222 , C08G18/283 , C08G18/3821 , C08G18/73 , C08G18/755 , C08G18/7837
摘要： Disclosed are polyaspartic esters obtainable by reaction of at least one polyamine component A), comprising an amine compound of the formula (I), where X is a saturated or unsaturated, linear or branched, aliphatic or cycloaliphatic or aromatic organic radical which is substituted or unsubstituted and/or has heteroatoms in the chain, Y is a secondary amino group bonded to two carbon atoms, R1 and R2 independently of one another are saturated or unsaturated, linear or branched, aliphatic or cycloaliphatic or aromatic organic radicals having 1 to 18 carbon atoms, and are substituted or unsubstituted and/or have heteroatoms in the chain, and n is a natural number from 1 to 4, with at least one polyisocyanate component B), comprising a polyisocyanate which contains at least one chemically bonded, non-ionic, hydrophilic group, characterized in that the ratio of the number of secondary amino groups Y to the number of isocyanate groups in the polyisocyanate is from 250:1 to 3:1. Further disclosed is a method for producing a coating composition, a 2-component system, the use thereof for producing a coating on a substrate, and the substrates coated accordingly.
摘要翻译：公开了通过至少一种多胺组分A）的反应获得的聚天冬氨酸酯，其包含式（I）的胺化合物，其中X是饱和或不饱和的直链或支链的脂族或脂环族或芳族有机基团，其被取代或未取代的和/或在链中具有杂原子，Y是与两个碳原子键合的仲氨基，R 1和R 2彼此独立地是饱和或不饱和的直链或支链的具有1至18个碳原子的脂族或脂环族或芳族有机基团原子，并且是取代或未取代的和/或在链中具有杂原子，n是1至4的天然数，与至少一种多异氰酸酯组分B），其包含含有至少一个化学键合的非离子的多异氰酸酯亲水基团，其特征在于，多异氰酸酯中的仲氨基数Y与异氰酸酯基的数目的比例为250:1至3:1。进一步公开了一种制备涂料组合物，2-组分体系，其用于在基材上制备涂层的用途的方法，以及相应地涂布的基材。

8. 发明申请

US20150133519A1 NOVEL DIESTER AND TRIESTER BASED LOW MOLECULAR WEIGHT, BIODEGRADEABLE CATIONIC LIPIDS FOR OLIGONUCLEOTIDE DELIVERY 有权
标题翻译：新型柴油机和基于TRIESTER的低分子量，用于寡核苷酸交付的生物降解性阳离子脂肪
公开(公告)号：US20150133519A1
公开(公告)日：2015-05-14
申请号：US14395267
申请日：2013-04-16
申请人： SIRNA THERAPEUTICS, INC.
发明人： Steven L. Colletti , Matthew G. Stanton
IPC分类号： A61K9/51 , C12N15/113 , C07C229/28 , C07C229/30
CPC分类号： A61K9/5123 , A61K9/51 , A61K9/5146 , A61K31/713 , A61K47/60 , C07C229/12 , C07C229/28 , C07C229/30 , C07C2101/02 , C07C2601/02 , C07F7/1804 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2320/32 , C12N2320/51
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.
摘要翻译：本发明提供式A的新型阳离子脂质，其可以与其它脂质组分如胆固醇和PEG-脂质组合使用以与寡核苷酸形成脂质纳米颗粒。本发明的目的是提供一种阳离子脂质支架，由于肝中脂质水平降低，其表现出增强的功效以及较低的肝毒性。本发明使用具有一个短脂链的低分子量阳离子脂质，并在脂质链中加入可水解官能团，以提高siRNA体内递送的效率和耐受性。

9. 发明申请

US20150112084A1 PROCESS FOR PREPARATION OF (IS, 3S, 5S)-2-[(2S)-2-AMIN0-2-(3-HYDROXY-l-ADAMANTYL) ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE 有权
标题翻译：（1S，3S，5S）-2 - [（2S）-2-氨基-2-（3-羟基-1-亚氨基）乙酰基] -2-亚甲基] [3.1.0]异丙基-3-碳二烯的制备方法
公开(公告)号：US20150112084A1
公开(公告)日：2015-04-23
申请号：US14404686
申请日：2013-04-22
申请人： RAMAMOHAN RAO DAVULURI
发明人： Ponniah Ravi , Praveen Kumar Neela , Batthini Guruswamy , Sribashyam Ravikanth , Uppala Manikya Rao , Dongari Naresh , Mogili Ravindar
IPC分类号： C07D209/52 , C07C229/28 , C07C227/16 , C07C247/12 , C07C227/10
CPC分类号： C07D209/52 , C07C227/10 , C07C227/16 , C07C229/28 , C07C247/12
摘要： Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.
摘要翻译：提供了用于制备沙格列汀的新方法和用于制备萨格列汀的方法中使用的新型中间体。

10. 发明授权

US08492399B2 3-carboxypropyl-aminotetralin derivatives and related compounds as mu opioid receptor antagonists 有权
公开(公告)号：US08492399B2
公开(公告)日：2013-07-23
申请号：US13652808
申请日：2012-10-16
申请人： Michael R. Leadbetter , Pierre-Jean Colson , Miroslav Rapta , Ying Yu
发明人： Michael R. Leadbetter , Pierre-Jean Colson , Miroslav Rapta , Ying Yu
IPC分类号： A01N43/42
CPC分类号： C07C237/48 , A61K9/0075 , A61K9/2054 , A61K9/4858 , A61K31/197 , A61K31/485 , A61K45/06 , A61K47/02 , A61K47/12 , C07B2200/07 , C07C215/64 , C07C229/28 , C07C229/34 , C07C2601/14 , C07C2602/10 , Y10T436/173845
摘要： The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

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