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1. 发明公开

US20230242572A1 a-CARBONYL ALKENYL ESTER PREPARATION METHOD THEREFOR AND APPLICATION THEREOF 审中-公开
公开(公告)号：US20230242572A1
公开(公告)日：2023-08-03
申请号：US17801514
申请日：2020-08-19
申请人： JIANGXI NORMAL UNIVERSITY
发明人： Junfeng ZHAO , Zhengning WANG , Xuewei WANG
IPC分类号： C07K1/06 , C07C69/145 , C07C67/08 , C07C69/753 , C07C69/78 , C07D307/68 , C07D231/56 , C07D333/70 , C07C69/618 , C07C69/606 , C07C229/22 , C07C227/18 , C07D209/20 , C07C233/05 , C07C231/12 , C07D233/64 , C07D207/16 , C07C279/24 , C07C277/08 , C07C231/14 , C07C233/11 , C07C233/09 , C07D295/185 , C07K5/062 , C07K5/065 , C07K7/06 , C07K1/22
CPC分类号： C07K1/064 , C07C69/145 , C07C67/08 , C07C69/753 , C07C69/78 , C07D307/68 , C07D231/56 , C07D333/70 , C07C69/618 , C07C69/606 , C07C229/22 , C07C227/18 , C07D209/20 , C07C233/05 , C07C231/12 , C07D233/64 , C07D207/16 , C07C279/24 , C07C277/08 , C07C231/14 , C07C233/11 , C07C233/09 , C07D295/185 , C07K5/0606 , C07K5/06043 , C07K5/06052 , C07K5/06078 , C07K5/06069 , C07K7/06 , C07K1/22
摘要： There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

2. 发明公开

US20230173082A1 ANTIBACTERIAL PRODUCTS 审中-公开
公开(公告)号：US20230173082A1
公开(公告)日：2023-06-08
申请号：US17855222
申请日：2022-06-30
申请人： UNIVERSITY OF LINCOLN
发明人： Ishwar SINGH , Edward TAYLOR
IPC分类号： A61K47/64 , C07C277/08 , A61K38/14 , C07C271/20 , C07C279/12 , A61K38/16 , C07H13/00 , A61K47/59 , A61P31/04 , A61K31/7034 , A61K31/7056
CPC分类号： A61K47/64 , A61K31/7034 , A61K31/7056 , A61K38/14 , A61K38/164 , A61K47/59 , A61P31/04 , C07C271/20 , C07C277/08 , C07C279/12 , C07H13/00
摘要： The invention provides a combination of an antibacterial agent and a delivery agent, in which the delivery agent is bonded, or capable of binding, to the antibacterial agent, and in which the delivery agent is capable of binding to one or more structures on a bacterial cell membrane. The invention further provides the use of such combinations in treating or preventing bacterial infections.

3. 发明授权

US09884814B2 Acylguanidines for treating osteoarthritis 有权
公开(公告)号：US09884814B2
公开(公告)日：2018-02-06
申请号：US14760765
申请日：2013-12-16
申请人： Merck Patent GmbH
发明人： Christos Tsaklakidis , Markus Klein , Paul Czodrowski
IPC分类号： C07C279/22 , C07D309/14 , C07D317/58 , C07D317/60 , C07D333/20 , C07D333/28 , C07D233/61 , C07D335/02 , C07D249/08 , C07D257/04 , C07D271/06 , C07D207/16 , C07D271/113 , C07D207/267 , C07D207/273 , C07D277/28 , C07D209/48 , C07D285/06 , C07D211/58 , C07D295/15 , C07D213/40 , C07D213/56 , C07D213/61 , C07D307/68 , C07C311/46 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/36 , A61K31/381 , A61K31/382 , A61K31/401 , A61K31/4015 , A61K31/4035 , A61K31/41 , A61K31/4164 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4468 , A61K31/5375 , C07C53/18 , C07C277/08 , C07D207/12 , C07D211/98 , C07D213/58 , C07D231/12 , C07D233/58 , C07D271/10 , C07D309/06 , C07D323/02 , C07D333/24
CPC分类号： C07C279/22 , A61K31/165 , A61K31/18 , A61K31/19 , A61K31/216 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/36 , A61K31/381 , A61K31/382 , A61K31/401 , A61K31/4015 , A61K31/4035 , A61K31/41 , A61K31/4164 , A61K31/4196 , A61K31/4245 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4468 , A61K31/5375 , C07C53/18 , C07C277/08 , C07C311/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D207/16 , C07D207/267 , C07D207/273 , C07D209/48 , C07D211/58 , C07D211/98 , C07D213/40 , C07D213/56 , C07D213/58 , C07D213/61 , C07D231/12 , C07D233/58 , C07D233/61 , C07D249/08 , C07D257/04 , C07D271/06 , C07D271/10 , C07D271/113 , C07D277/28 , C07D285/06 , C07D295/15 , C07D307/68 , C07D309/06 , C07D309/14 , C07D317/58 , C07D317/60 , C07D323/02 , C07D333/20 , C07D333/24 , C07D333/28 , C07D335/02
摘要： The present invention relates to compounds of the formula (I) and in particular to medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of osteoarthritis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia.

4. 发明授权

US09650470B2 Method of making ligand functionalized substrates 有权
公开(公告)号：US09650470B2
公开(公告)日：2017-05-16
申请号：US14467651
申请日：2014-08-25
申请人： 3M INNOVATIVE PROPERTIES COMPANY
发明人： Catherine A. Bothof , Yi He , Jerald K. Rasmussen , Kannan Seshadri , Clinton P. Waller, Jr. , Douglas E. Weiss
IPC分类号： B32B27/00 , C08G69/48 , B01J20/285 , C07C279/12 , C07C281/16 , C08J7/18 , C08J9/28 , C08J9/42 , B01D39/16 , C07K1/34 , C12N7/00 , C07C277/08 , C07C279/14 , C08F259/08
CPC分类号： C07C279/12 , B01D39/1676 , B01J20/285 , C07C277/08 , C07C279/14 , C07C281/16 , C07K1/34 , C08F259/08 , C08F283/04 , C08G69/48 , C08J7/18 , C08J9/283 , C08J9/42 , C08J2327/16 , C08J2377/00 , C12N7/00 , Y02C10/08 , Y10T428/31855
摘要： Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.

5. 发明授权

US09567294B2 Bioactive polymers 有权
标题翻译：生物活性聚合物
公开(公告)号：US09567294B2
公开(公告)日：2017-02-14
申请号：US14763356
申请日：2014-01-22
申请人： Sealife Pharma GmbH
发明人： Alexander Pretsch , Michael Nagl , Christoph Wiesner , Heinz Burgmann
IPC分类号： C07C279/00 , C08G73/02 , A01N47/40 , C07C277/08 , C07C279/08
CPC分类号： C07C279/00 , A01N47/40 , C07C277/08 , C07C279/08 , C08G73/02
摘要： Polycondensation products of aminoguanidine and/or 1,3-diaminoguanidine with one or more diamines are provided including polyguanidine derivatives of the following formula (I) or a salt thereof: wherein X is selected from —NH2, aminoguanidino and 1,3-diaminoguanidino; Y is selected from —H and —R1—NH2; or X and Y together represent a chemical bond to give a cyclic structure; R1 is selected from divalent organic radicals having 2 to 20 carbon atoms, in which optionally one or more carbon atoms are replaced by O or N; a and b are each 0 or 1, wherein a+b≠2 if no 1,3-diaminoguanidine units are included; R2 is selected from —H and —NH2, wherein R2 is —NH2 if a+b=0, R2 is —H or —NH2 if a+b=1, and R2 is —H if a+b=2; and n≧2. Production methods and uses of the polyguanidine derivatives are also provided.
摘要翻译：提供氨基胍和/或1,3-二氨基胍与一种或多种二胺的缩聚产物，包括下式（I）的聚胍衍生物或其盐：其中X选自-NH 2，氨基胍基和1,3-二氨基鸟嘌呤; Y选自-H和-R1-NH2; 或X和Y一起表示化学键以产生环状结构; R1选自具有2至20个碳原子的二价有机基团，其中任选地一个或多个碳原子被O或N替代; a和b各自为0或1，其中a + b≠2，如果不包括1,3-二氨基胍单元; 如果a + b = 0，则R 2选自-H和-NH 2，其中如果a + b = 0，R 2为-NH 2，如果a + b = 1，则R 2为-H 2或如果a + b = 2，则R 2为-H。 n≥2。还提供了聚胍衍生物的生产方法和用途。

6. 发明申请

US20170001954A1 GUANIDINIUM COMPOUNDS 审中-公开
标题翻译： GUANIDINIUM化合物
公开(公告)号：US20170001954A1
公开(公告)日：2017-01-05
申请号：US15178314
申请日：2016-06-09
申请人： NUtech Ventures
发明人： Stephen DiMagno , Bao Hu
IPC分类号： C07C279/08 , C07C277/08
CPC分类号： C07C279/08 , C07B59/001 , C07C277/08 , C07C279/06 , C07C309/06
摘要： The present application provides, inter alia, chemical compounds useful as synthesis intermediates, said compounds comprising one or more guanidinium moieties and a hypervalent iodine atom. Methods for making these compounds are also provided.
摘要翻译：本申请尤其提供了可用作合成中间体的化合物，所述化合物包含一个或多个胍部分和高价碘原子。还提供了制备这些化合物的方法。

7. 发明授权

US09388125B2 Compositions, methods, and systems for the synthesis and use of imaging agents 有权
标题翻译：用于合成和使用成像剂的组合物，方法和系统
公开(公告)号：US09388125B2
公开(公告)日：2016-07-12
申请号：US13697287
申请日：2011-05-11
申请人： Ajay Purohit , Pedro Benites , Edward H. Cheesman , Joel Lazewatsky , L. Veronica Lee , Richard R. Cesati , Richard J. Looby , Heike S. Radeke
发明人： Ajay Purohit , Pedro Benites , Edward H. Cheesman , Joel Lazewatsky , L. Veronica Lee , Richard R. Cesati , Richard J. Looby , Heike S. Radeke
IPC分类号： A61K51/00 , A61M36/14 , C07C277/08 , A61K51/04 , C07B59/00 , C07C53/06 , C07C217/58 , C07C255/54 , C07C279/10 , C07C279/24 , C07C309/65 , C07C309/66 , C07C309/73 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C303/28 , C07C303/30 , C07C309/04 , C07C309/30 , C07C277/00
CPC分类号： C07C303/30 , A61K51/00 , A61K51/04 , A61K51/0406 , C07B59/001 , C07B2200/05 , C07C53/06 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C217/58 , C07C255/54 , C07C277/00 , C07C277/08 , C07C279/10 , C07C279/24 , C07C303/28 , C07C309/04 , C07C309/30 , C07C309/65 , C07C309/66 , C07C309/73 , C07C279/08
摘要： The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
摘要翻译：本发明一般涉及可用于医学成像的新型合成方法，系统，试剂盒，盐和前体。在一些实施方案中，本发明提供了包含可以使用本文所述的合成方法形成的成像剂前体的组合物。可以使用本文所述的方法将成像剂转化成成像剂。在某些情况下，成像剂富集于18F。在一些情况下，包括盐形式的成像剂（例如抗坏血酸盐）可用于对受试者感兴趣的区域进行成像，包括但不限于心脏，心血管系统，心脏血管，脑和其他器官。

8. 发明申请

US20150246142A1 IMAGING AGENTS 审中-公开
标题翻译：成像代理
公开(公告)号：US20150246142A1
公开(公告)日：2015-09-03
申请号：US14428876
申请日：2013-09-25
申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN
发明人： David M. Raffel , Yong-Woon Jung , Keun-Sam Jang
IPC分类号： A61K51/04 , C07B59/00 , C07C279/08
CPC分类号： C07C279/08 , A61K31/155 , A61K51/04 , C07B59/001 , C07B59/002 , C07B2200/05 , C07C277/06 , C07C277/08 , C07C279/06
摘要： Provided herein is technology relating to imaging agents and particularly, but not exclusively, to methods of manufacturing fluorine-18-labeled phenethylguanidines and uses thereof.
摘要翻译：本文提供了涉及成像剂的技术，特别是但不排他地涉及制备氟-18-标记的苯乙基胍的方法及其用途。

9. 发明授权

US09035093B2 Methods for production of high concentration of arginine bicarbonate solution at high pressure 有权
标题翻译：在高压下生产高浓度精氨酸碳酸氢盐溶液的方法
公开(公告)号：US09035093B2
公开(公告)日：2015-05-19
申请号：US13515829
申请日：2010-12-13
申请人： Donghui Wu
发明人： Donghui Wu
IPC分类号： C07C277/08
CPC分类号： C07C277/08 , C07C279/14
摘要： Methods of producing arginine bicarbonate solutions in very high concentrations including reacting an arginine slurry containing a first portion of arginine with a source of carbon dioxide gas at elevated pressure and temperature, adding subsequent portions of arginine to the resulting solution and further reacting with compressed carbon dioxide until a final solution containing in excess of 50% by weight are provided which include preparing an arginine solution by subjecting an arginine water slurry to elevated pressure and temperature and reacting the arginine solution with a source of carbon dioxide gas to form a solution comprising arginine and bicarbonate anion and recovering arginine bicarbonate from the solution.
摘要翻译：以非常高的浓度生产精氨酸碳酸氢盐溶液的方法，包括在升高的压力和温度下使包含精氨酸的第一部分的精氨酸浆料与二氧化碳源一起在升高的压力和温度下反应，将后续部分精氨酸加入到所得溶液中，并与压缩的二氧化碳反应提供包含超过50重量％的最终溶液，其包括通过使精氨酸水浆料升高压力和温度来制备精氨酸溶液，并使精氨酸溶液与二氧化碳气体源反应以形成包含精氨酸和碳酸氢根阴离子并从溶液中回收精氨酸碳酸氢盐。

10. 发明授权

US08853276B2 Guanidine derivatives in cinnamic series 有权
标题翻译：肉桂系列中的胍衍生物
公开(公告)号：US08853276B2
公开(公告)日：2014-10-07
申请号：US13821093
申请日：2011-09-06
申请人： Sylvain Rault , Jean Charles Lancelot , Peggy Suzanne , Anne-Sophie Voisin-Chiret , Regis Pecquet , Jean-Christophe Joseph
发明人： Sylvain Rault , Jean Charles Lancelot , Peggy Suzanne , Anne-Sophie Voisin-Chiret , Regis Pecquet , Jean-Christophe Joseph
IPC分类号： A01N37/52 , A61K31/155 , C07C281/00 , C07C281/16 , C07C279/00 , C07D249/18 , A61K8/43 , C07D317/46 , A61Q19/08 , C07C243/34 , C07C277/08 , C07C243/32
CPC分类号： C07C281/16 , A61K8/43 , A61Q19/08 , C07C243/32 , C07C243/34 , C07C277/08 , C07C279/00 , C07D249/18 , C07D317/46
摘要： The invention relates to novel guanidine derivatives in the cinnamic series of general formula (I): The invention also relates to the process for preparing said guanidine derivatives and also to synthetic intermediates.Finally, the invention relates to the use of the guanidine derivatives for the preparation of compositions with anti-glycation properties, especially in cosmetology.
摘要翻译：本发明涉及通式（I）的肉桂系列中的新型胍衍生物：本发明还涉及制备所述胍衍生物以及合成中间体的方法。最后，本发明涉及胍衍生物用于制备具有抗糖化性质的组合物的用途，特别是在美容方面。

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