公开(公告)号：US20230242572A1

公开(公告)日：2023-08-03

申请号：US17801514

申请日：2020-08-19

Applicant: JIANGXI NORMAL UNIVERSITY

Inventor： Junfeng ZHAO ,  Zhengning WANG ,  Xuewei WANG

IPC: 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 classification number: 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

Abstract: 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.

公开(公告)号：US20220204457A1

公开(公告)日：2022-06-30

申请号：US17441572

申请日：2020-03-20

Applicant: Cortexyme, Inc.

Inventor： Robert A. Galemmo ,  Andrei W. Konradi ,  Casey C. Lynch ,  Stephen S. Dominy

IPC: C07D239/34 ,  C07C279/28 ,  C07C279/24 ,  C07C279/12 ,  C07D213/68 ,  C07D213/82 ,  C07D261/12

Abstract: Therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A and arginine gingipain B, are disclosed, as well as the use thereof for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, Formula Ia, and Formula Ib, as described herein, and pharmaceutically acceptable salts thereof.

公开(公告)号：US20220017459A1

公开(公告)日：2022-01-20

申请号：US17387478

申请日：2021-07-28

Applicant: Lantheus Medical Imaging, Inc.

Inventor： Ajay Purohit ,  Pedro Benites ,  Heike S. Radeke ,  Joel Lazewatsky ,  L. Veronica Lee

IPC: 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

Abstract: 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.

公开(公告)号：US20190337909A1

公开(公告)日：2019-11-07

申请号：US16419596

申请日：2019-05-22

Applicant: FARMINGTON PHARMA DEVELOPMENT

Inventor： William F. BRUBAKER

IPC: C07D273/06 ,  C07C279/24 ,  C07D273/04 ,  C07C279/14 ,  C07D271/07

Abstract: The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof.

公开(公告)号：US10392341B2

公开(公告)日：2019-08-27

申请号：US16148822

申请日：2018-10-01

Applicant: ModernaTX, Inc.

Inventor： Kerry E. Benenato ,  Mark Cornebise

IPC: A61K9/51 ,  A61K9/00 ,  A61K48/00 ,  C12N15/63 ,  C07C229/12 ,  A61K9/127 ,  C07C271/20 ,  C07C279/12 ,  C07C279/28 ,  C07C279/32 ,  C07D233/72 ,  C07D249/04 ,  C07D263/20 ,  C07D265/33 ,  C07D271/06 ,  C07D271/10 ,  C07D207/27 ,  C07D277/38 ,  C07C275/14 ,  C07C279/24 ,  C07C311/05 ,  C07C229/16 ,  C07C335/08 ,  C07C233/36 ,  C07C235/10 ,  C07C255/24 ,  C07F9/09 ,  A61K9/16 ,  A61K38/18 ,  C07K14/505 ,  A61K47/54 ,  A61K47/69 ,  C07C227/16 ,  A61K31/7105 ,  A61K38/17 ,  C07C227/18

Abstract: The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.

公开(公告)号：US20180327364A1

公开(公告)日：2018-11-15

申请号：US15774962

申请日：2016-11-14

Applicant: Brandeis University

Inventor： Ann Parrinello Lawson ,  Jianjun Xue ,  Lizbeth K. Hedstrom ,  Rory T. Coffey

IPC: C07D239/49 ,  C07C279/24 ,  C07C271/20 ,  C07C279/30 ,  A61P35/00

CPC classification number: C07D239/49 ,  A61P35/00 ,  C07C271/20 ,  C07C279/24 ,  C07C279/30 ,  C12N9/12 ,  C12Y207/1101 ,  C12Y207/1102

Abstract: Disclosed are small molecule inhibitors of mammalian target of rapamycin (mTOR), and methods of using them.

公开(公告)号：US10004702B2

公开(公告)日：2018-06-26

申请号：US15517764

申请日：2015-10-09

Applicant: LEAD DISCOVERY SIENA S.R.L.

Inventor： Maurizio Botta ,  Giorgio Maccari ,  Stefania Sanfilippo ,  Filomena De Luca ,  Jean-Denis Docquier ,  Davide Deodato

IPC: A61K31/155 ,  C07C279/12 ,  C07C279/24 ,  C08K5/31 ,  C07C279/04 ,  A61K45/06 ,  A61K31/17

CPC classification number: A61K31/155 ,  A61K31/17 ,  A61K45/06 ,  C07C279/04 ,  C07C279/12 ,  C07C279/24 ,  C07C2601/02 ,  C08K5/31 ,  Y02A50/473 ,  A61K2300/00

Abstract: The present invention relates to linear guanidine derivatives, methods of preparation, uses and pharmaceutical compositions thereof. The compounds of Formulas 1 or 2 exhibit high antimicrobial activity against Gram positive and Gram negative bacteria.

公开(公告)号：US20170313656A1

公开(公告)日：2017-11-02

申请号：US15630986

申请日：2017-06-23

Applicant: Paul D. Davis ,  D. Scott Wilbur

Inventor： Paul D. Davis ,  D. Scott Wilbur

IPC: C07D209/60 ,  C07K16/30 ,  C07K14/605 ,  C07D403/14 ,  C07D257/02 ,  C07D209/48 ,  C07D207/404 ,  C07C331/28 ,  C07C317/44 ,  C07C279/24 ,  C07C271/16 ,  C07C235/48 ,  C07C235/08 ,  A61K51/10 ,  C07K16/40 ,  C07C2603/18

CPC classification number: C07D209/60 ,  A61K47/60 ,  A61K51/106 ,  C07C235/08 ,  C07C235/48 ,  C07C271/16 ,  C07C279/24 ,  C07C317/44 ,  C07C331/28 ,  C07C2603/18 ,  C07D207/404 ,  C07D209/48 ,  C07D257/02 ,  C07D403/14 ,  C07K14/605 ,  C07K16/3069 ,  C07K16/40

Abstract: Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

公开(公告)号：US09388125B2

公开(公告)日：2016-07-12

申请号：US13697287

申请日：2011-05-11

Applicant: Ajay Purohit ,  Pedro Benites ,  Edward H. Cheesman ,  Joel Lazewatsky ,  L. Veronica Lee ,  Richard R. Cesati ,  Richard J. Looby ,  Heike S. Radeke

Inventor： Ajay Purohit ,  Pedro Benites ,  Edward H. Cheesman ,  Joel Lazewatsky ,  L. Veronica Lee ,  Richard R. Cesati ,  Richard J. Looby ,  Heike S. Radeke

IPC: 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 classification number: 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

Abstract: 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.

Abstract translation: 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 。

公开(公告)号：US20140228441A1

公开(公告)日：2014-08-14

申请号：US14346538

申请日：2012-09-21

Applicant: Centre National De La Recherche Scientifique ,  Universite De Strasbourg

Inventor： Martial Ruat ,  Hélène Faure ,  Hermine Roudaut ,  Lucile Hoch ,  Angèle Schoenfelder ,  Maurizio Taddei ,  André Mann

IPC: C07C279/24 ,  G01N33/50 ,  G01N33/574

CPC classification number: C07C279/24 ,  C07C279/22 ,  G01N33/5011 ,  G01N33/5041 ,  G01N33/57492

Abstract: The invention relates to compounds of formula (I), and the use thereof as a drug, particularly for the treatment of tumors associated with hyperactivation of the hedgehog protein signaling pathway, treatment of neurodegenerative diseases, treatment of diseases related to cerebral development (holoprosencephaly), for stem cell monitoring treatment of cerebrovascular accidents and cardiovascular accidents, treatment of diseases involving oligodendrocytes and diseases involving neurolemmocytes, for application thereof in vitro for modulating human or animal stem cell renewal, and for the treatment of diabetes. The invention also relates to pharmaceutical compositions having a compound of formula (I). The invention also relates to a method for radio-marking compounds having formula (I), the marked compounds, and the use of the compounds as research tools, and method for screening and/or identifying ligands in the Smoothened receptor (Smo) binding sites, methods for identifying agonists and antagonists of the Smoothened receptor, and a method for identifying cells.

Abstract translation: 本发明涉及式（I）化合物及其作为药物的用途，特别是用于治疗与刺猬蛋白信号传导途径的高活化相关的肿瘤，治疗神经变性疾病，治疗与脑发育有关的疾病（脑畸形） 用于干细胞监测治疗脑血管意外和心血管事故，治疗涉及少突胶质细胞的疾病和涉及神经细胞的疾病，用于体外应用于调节人或动物干细胞更新和用于治疗糖尿病。 本发明还涉及具有式（I）化合物的药物组合物。 本发明还涉及用于放射性标记具有式（I）的化合物，标记的化合物和该化合物作为研究工具的用途的方法，以及用于筛选和/或鉴定平滑受体（Smo）结合位点中的配体的方法 用于鉴定Smoothened受体的激动剂和拮抗剂的方法以及鉴定细胞的方法。