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1. 发明申请

US20220380304A1 NOVEL METHOD FOR PRODUCING PERAMIVIR TRIHYDRATE, AND WATER-BASED DRYING THEREOF 有权
公开(公告)号：US20220380304A1
公开(公告)日：2022-12-01
申请号：US17622322
申请日：2020-07-02
申请人： CKD BIO CORPORATION
发明人： Hee Un KIM , In Kyu KIM , Myeong Seok LEE , Heung Mo KANG , Sae Jin KIM , In Suk CHOI
IPC分类号： C07C277/08
摘要： The present invention relates to a method for producing peramivir trihydrate, which is an inhibitor of neuraminidase infection, as an anti-influenza agent. According to the production method of the present invention, peramivir trihydrate can be produced with high yield and stability through a process suitable for producing excellent pharmaceuticals and quality control standards (GMP) without using highly-toxic methanol and activated carbon.

2. 发明申请

US20220362176A1 CATIONIC ANTIMICROBIAL OLIGO-GUANIDINIUM DENDRIMERS AND COMPOSITIONS 有权
公开(公告)号：US20220362176A1
公开(公告)日：2022-11-17
申请号：US17744470
申请日：2022-05-13
申请人： Hyun Ho Chung
发明人： Hyun Ho Chung
IPC分类号： A61K31/155 , C07C277/08 , A61P31/04 , A01N47/44 , A01P1/00 , A61K47/55
摘要： A new synthesized non-peptide cationic oligo-guanidinium dendrimers containing a number of positive charges, 6, 9, 12, and 18 for use as antimicrobial agents and a method for synthesizing non-peptide cationic oligo-guanidinium dendrimers G12 and G18. These designed and synthesized dendrimers exhibit antimicrobial activities as well as biofilm disrupting activity against various pathogens such as Gram-negative bacteria, Gram-positive bacteria, and fungi. The application of these dendrimers are very broad, which includes application to pharmaceutical compounds that are covalently or non-covalently complexed. These combinations are important in helping the body reach the proper immune balance required for maximized function and/or optimal health.

3. 发明申请

US20220213030A1 AMINOGUANIDINE HYDRAZONES AS RETROMER STABILIZERS USEFUL FOR TREATING NEUROLOGICAL DISEASES 有权
公开(公告)号：US20220213030A1
公开(公告)日：2022-07-07
申请号：US17599694
申请日：2020-04-01
申请人： OSPEDALE SAN RAFFAELE SRL
发明人： Gianvito MARTINO , Luca MUZIO , Nilo RIVA , Davide GORNATI , Pierfausto SENECI , Simona Carmen ELEUTERI
IPC分类号： C07C281/18 , A61P25/28 , C07C277/08 , C07D295/192 , C07C311/08 , C07C311/21 , C07D233/88
摘要： The present invention relates to novel aminoguanidine hydrazone-derivatives of Formula (I) which are effective as retromer stabilizers and useful as neuroprotecting drugs. The invention also relates to pharmaceutical compositions comprising the compounds and their use in therapy and diagnostic.

4. 发明申请

US20220017459A1 COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS 有权
公开(公告)号：US20220017459A1
公开(公告)日：2022-01-20
申请号：US17387478
申请日：2021-07-28
申请人： Lantheus Medical Imaging, Inc.
发明人： Ajay Purohit , Pedro Benites , Heike S. Radeke , Joel Lazewatsky , L. Veronica Lee
IPC分类号： C07C303/30 , A61K51/04 , C07B59/00 , C07C53/06 , C07C217/58 , C07C255/54 , C07C279/10 , C07C279/24 , C07C309/65 , C07C309/66 , C07C309/73 , C07C277/08 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C303/28 , C07C309/04 , C07C309/30
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.

5. 发明申请

US20200123099A1 Structure and Synthesis of Highly Fluorinated Amino Acid Derivatives 审中-公开
公开(公告)号：US20200123099A1
公开(公告)日：2020-04-23
申请号：US16483636
申请日：2018-02-20
申请人： The Board of Regents for Oklahoma State University
发明人： Jimmie Dean Weaver , Kip Allen Teegardin , Amandeep Arora
IPC分类号： C07C227/18 , C07C319/12 , C07C277/08 , C07D207/16 , C07D233/64 , C07D209/20
摘要： Methods of synthesizing polyfluorinated amino acid derivatives are disclosed, along with polyfluorinated amino acid derivatives produced from said methods, as well as compositions containing same. The synthesis methods utilize an oxazolone and a perfluoroarene to produce the polyfluorinated amino acid derivatives.

6. 发明授权

US10414875B2 Catalyst containing guanidine groups 有权
公开(公告)号：US10414875B2
公开(公告)日：2019-09-17
申请号：US15572331
申请日：2016-05-10
申请人： SIKA TECHNOLOGY AG
发明人： Rita Cannas , Urs Burckhardt
IPC分类号： C08G77/46 , C07C277/08 , C08K5/31 , C08G65/336 , C08J3/24 , C09D183/12 , C09J183/12
摘要： The use of a catalyst of the formula (I) for the crosslinking of a curable composition. The catalyst of the formula (I) contains at least one aliphatic guanidine group. It is substantially odorless and nonvolatile at room temperature and accelerates the crosslinking of curable compositions very efficiently, without impairing the storage stability thereof. It is particularly suitable for compositions based on polymers containing silane groups, where it has very good compatibility, as a result of which such compositions do not have a tendency to separation or migration or evaporation of the catalyst.

7. 发明申请

US20190269719A1 POLYGUANIDINE POLYMERS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20190269719A1
公开(公告)日：2019-09-05
申请号：US16411703
申请日：2019-05-14
申请人： Sealife Pharma GmbH
发明人： Alexander PRETSCH , Michael NAGL , Christoph WIESNER , Ralph HOLLAUS , Miroslav GENOV
IPC分类号： A61K31/785 , C07C277/08 , A61K31/155 , A61K45/06 , A01N47/44 , C08G73/00 , C07D213/42 , C07C279/00 , C08G73/06
摘要： Polyguanidines and methods of use thereof are described. In particular, polyguanidines of formula (I), formula (II), and formula (III) are described. The polyguanidines can be used to treat infection, such as bacterial, viral or fungal infection, and as an ex vivo microbial agent.

8. 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.

9. 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.

10. 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。

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