公开(公告)号：US12016836B2

公开(公告)日：2024-06-25

申请号：US18168128

申请日：2023-02-13

申请人： Lapix Therapeutics, Inc.

发明人： Anas M. Fathallah ,  Scott D. Larsen ,  Abdulraouf Ramadan

IPC分类号： A61K31/198 ,  A61K9/00 ,  A61K9/08 ,  A61K31/357 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/472 ,  A61K47/40 ,  A61P25/28 ,  A61P37/06 ,  C07C235/34 ,  C07D213/65 ,  C07D217/02 ,  C07D235/06 ,  C07D319/18

CPC分类号： A61K31/198 ,  A61K9/0053 ,  A61K9/08 ,  A61K31/357 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/472 ,  A61K47/40 ,  A61P25/28 ,  A61P37/06 ,  C07C235/34 ,  C07D213/65 ,  C07D217/02 ,  C07D235/06 ,  C07D319/18

摘要： Provided herein are compounds and their pharmaceutically acceptable salts, lipid particles comprising such compounds or pharmaceutically acceptable salts thereof and compositions of the foregoing that can be used to reduce immune intolerance in a subject, for example, to treat autoimmune disorders, or in combination with an antigenic therapy, such as a protein or gene therapy, to improve the efficacy of the antigenic therapy. The compounds have the following structural formula:




wherein values for the variables (e.g., Ring A, L, R1, R2, R3, m) are as described herein.

公开(公告)号：US12006293B1

公开(公告)日：2024-06-11

申请号：US18545056

申请日：2023-12-19

申请人： KING FAISAL UNIVERSITY

发明人： Saad Shaaban ,  Amr Negm

IPC分类号： C07D231/12 ,  A61K31/4155 ,  A61K31/4375 ,  C07D213/65 ,  C07D401/14

CPC分类号： C07D231/12 ,  A61K31/4155 ,  A61K31/4375 ,  C07D213/65 ,  C07D401/14

摘要： Diselenide organo compounds, their synthesis, and their use as deubiquitination signaling pathway modulators and anti-cancer agents.

公开(公告)号：US20240051975A1

公开(公告)日：2024-02-15

申请号：US18258346

申请日：2022-02-14

申请人： TSINGHUA UNIVERSITY

发明人： Gelin WANG ,  Yefeng TANG ,  Hong YAO ,  Minghui LIU ,  Leibo WANG ,  Chenyu LI ,  Ruoxi ZHANG ,  Yumeng ZU ,  Chuo WU ,  Feifei LI ,  Shuangquan CHEN

IPC分类号： C07F5/02 ,  C07C235/24 ,  C07D213/65 ,  C07C255/50 ,  C07C311/16 ,  C07C279/04 ,  A61P25/28

CPC分类号： C07F5/025 ,  C07C235/24 ,  C07D213/65 ,  C07C255/50 ,  C07C311/16 ,  C07C279/04 ,  A61P25/28 ,  C07C2601/16

摘要： The present invention provides a class of novel NAMPT enzyme agonist and preparation and use thereof, which has a structural formula as shown in formula I or formula II. The present invention screens the NAMPT agonist NAT from the chemical small molecule library, and the NAT exhibits a good cytoprotective effect and a good anti-neurodegeneration effect in animal models of neurodegeneration. We studied the binding of NAT to enzymes, and then carried out multiple rounds of structure optimization based on the chemical structure characteristics of NAT and its enzyme activity properties, and obtained a relatively defined structure-activity relationship. The present patent not only lays the foundation for developing innovative drugs for anti-aging and neurodegenerative diseases, but also theoretically provides a proof-of-concept that enhancing NAMPT enzyme activity plays an important role in neuroprotection.

公开(公告)号：US11883386B2

公开(公告)日：2024-01-30

申请号：US17815391

申请日：2022-07-27

申请人： Akebia Therapeutics, Inc.

发明人： Richard Masaru Kawamoto ,  Shengde Wu ,  Artem G. Evdokimov ,  Kenneth D Greis ,  Angelique Sun Boyer ,  Namal C. Warshakoon

IPC分类号： C07D213/81 ,  C07D213/65 ,  A61K31/4418 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D405/10 ,  C07D405/04 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D417/04 ,  A61K31/4433

CPC分类号： A61K31/4418 ,  A61K31/4433 ,  C07C235/60 ,  C07C237/42 ,  C07C255/57 ,  C07D213/65 ,  C07D213/81 ,  C07D295/192 ,  C07D401/04 ,  C07D401/10 ,  C07D405/04 ,  C07D405/10 ,  C07D417/04 ,  Y02A50/30

摘要： The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.

公开(公告)号：US20230212123A1

公开(公告)日：2023-07-06

申请号：US17920794

申请日：2021-04-20

申请人： THE REGENTS OF THE UNIVERSITY OF MICHIGAN

发明人： Scott D. Larsen ,  James A. Shayman ,  Michael William Wilson ,  Neil Moss

IPC分类号： C07D213/64 ,  C07D213/65 ,  C07D213/40 ,  C07D213/68 ,  C07D401/06 ,  C07D213/61 ,  A61K45/06

CPC分类号： C07D213/64 ,  A61K45/06 ,  C07D213/40 ,  C07D213/61 ,  C07D213/65 ,  C07D213/68 ,  C07D401/06

摘要： Glucosylceramide synthase inhibitors and compositions containing the same are disclosed. Methods of using the glucosylceramide synthase inhibitors in the treatment of diseases and conditions wherein inhibition of glucosylceramide synthase provides a benefit, like Gaucher disease and Fabry disease, also are disclosed.

公开(公告)号：US11572337B2

公开(公告)日：2023-02-07

申请号：US16978135

申请日：2019-03-06

申请人： Rutgers, The State University of New Jersey

发明人： Richard H. Ebright ,  Yon W. Ebright ,  Joel S. Freundlich ,  Ricardo Gallardo-Macias ,  Shao-Gang Li

IPC分类号： C07C235/60 ,  C07D239/34 ,  C07D213/65 ,  C07D213/56 ,  A61P31/04 ,  A01N43/54 ,  A01N43/40 ,  A01N37/44 ,  C07D213/30 ,  C07D213/68 ,  C07D295/096

摘要： The invention provides compounds of formula (I) or (II) and tautomers and salts thereof, wherein variables are as described in the specification, as well as compositions comprising a compound of formula (I) or (II) or a tautomer or salt thereof, methods of making a compound of formula (I) or (II) or a tautomer or salt thereof, and methods of using a compound of formula (I) or (II) or a tautomer or salt thereof as, e.g., inhibitors of bacterial RNA polymerase or as antibacterial agents.

公开(公告)号：US20220402873A1

公开(公告)日：2022-12-22

申请号：US17761830

申请日：2020-09-21

申请人： AUTOTAC INC. ,  SEOUL NATIONAL UNIVERSITY R&DB FOUNDATION

发明人： Yong Tae KWON ,  Chang Hoon JI ,  Hyun Tae KIM ,  Jeong Eun NA ,  Hee Yeon KIM ,  Min Ju LEE

IPC分类号： C07D213/64 ,  C07D213/69 ,  C07D239/34 ,  C07D213/74 ,  C07D207/335 ,  C07D333/32 ,  C07D307/58 ,  C07D307/52 ,  C07D213/65

摘要： Novel p62 ligand compounds, or a stereoisomer, a solvate, a hydrate, or a prodrug thereof are disclosed. The novel compounds, stereoisomer, solvate, hydrate, or prodrug activates selective autophagy in cells to selectively remove proteins, organelles, and coagulations in the body, and thus can be advantageously used as a pharmaceutical composition for preventing, ameliorating, or treating various proteinopathies. Compositions such as pharmaceutical composition or food compositions containing the novel p62 ligand compounds, stereoisomer, solvate, hydrate, or prodrug thereof as well as uses thereof are disclosed.

公开(公告)号：US20220396581A1

公开(公告)日：2022-12-15

申请号：US17228573

申请日：2021-04-12

申请人： Janssen BioPharma, Inc.

发明人： Guangyi WANG ,  Leonid BEIGELMAN ,  Anh TRUONG ,  Carmela NAPOLITANO ,  Daniele ANDREOTTI ,  Haiying HE

IPC分类号： C07D495/04 ,  A61K31/352 ,  A61K31/4196 ,  A61K31/4365 ,  C07C255/66 ,  C07D233/88 ,  C07D261/20 ,  C07D307/40 ,  C07D307/52 ,  C07D333/20 ,  C07D333/58 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/427 ,  A61K31/4375 ,  A61K31/4725 ,  C07D213/50 ,  C07D233/64 ,  C07D333/68 ,  C07D401/12 ,  C07D409/06 ,  A61K31/343 ,  A61K31/382 ,  A61K31/426 ,  A61K31/4418 ,  A61K31/4545 ,  C07C251/84 ,  C07D207/335 ,  C07D215/12 ,  C07D215/42 ,  C07D233/61 ,  C07D401/04 ,  C07D409/14 ,  A61K31/277 ,  A61K31/407 ,  A61K31/423 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  C07C243/34 ,  C07D209/20 ,  C07D209/86 ,  C07D233/38 ,  C07D233/60 ,  C07D277/64 ,  C07D307/81 ,  C07D405/10 ,  C07D417/04 ,  C07D417/12 ,  A61K31/165 ,  A61K31/40 ,  A61K31/4709 ,  C07C243/18 ,  C07D277/56 ,  C07D333/66 ,  C07D413/04 ,  C07D471/04 ,  C07D495/14 ,  A61K31/4427 ,  A61K31/5377 ,  C07D213/42 ,  C07D213/68 ,  C07D215/38 ,  C07D217/24 ,  C07D307/91 ,  C07D311/68 ,  C07D333/16 ,  C07D333/62 ,  C07D401/10 ,  C07D409/12 ,  A61K31/341 ,  A61K31/4164 ,  A61K31/428 ,  A61K31/444 ,  A61K31/4704 ,  A61K31/501 ,  A61K45/06 ,  C07C255/34 ,  C07D209/08 ,  C07D215/14 ,  C07D333/54 ,  C07D335/06 ,  C07D405/04 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D413/14 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/47 ,  A61K31/538 ,  C07C251/80 ,  C07D209/14 ,  C07D213/65 ,  C07D333/50 ,  C07D333/76

摘要： Disclosed herein are new antiviral compounds, together with pharmaceutical compositions that include one or more antiviral compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection with one or more small molecule compounds. Examples of paramyxovirus infection include an infection caused by human respiratory syncytial virus (RSV).

公开(公告)号：US20220204472A1

公开(公告)日：2022-06-30

申请号：US17691745

申请日：2022-03-10

申请人： OHIO STATE INNOVATION FOUNDATION

发明人： Christopher Hadad ,  Christopher Callam ,  Jeremy Beck ,  Qinggeng Zhuang ,  Andrew Franjesevic ,  Thomas Corrigan ,  Craig McElroy

IPC分类号： C07D401/06 ,  C07D213/65 ,  C07D401/14 ,  C07D413/06

摘要： Disclosed herein are compounds, compositions, and methods for reactivating or realkylating aged acetylcholinesterase inhibited by or conjugated to the organophosphorus compound. The organophosphorus compound can be a nerve agent. The acetylcholinesterase can be in the central nerve system (CNS) and/or the peripheral nervous system (PNS) of a subject. Accordingly, methods for ameliorating, diminishing, reversing, treating or preventing the toxic effects of an organophosphorus compound in a subject are provided herein. Methods for prophylactic or therapeutic treatment of exposure to an organophosphorus nerve agent are also provided.

公开(公告)号：US11236053B2

公开(公告)日：2022-02-01

申请号：US16634567

申请日：2018-07-26

申请人： Emory University ,  Mercer University ,  Howard University ,  Union University

发明人： Osman Güner ,  Bernard Lassegue ,  Kathy Griendling ,  Qian Xu ,  David Brown ,  J. Phillip Bowen ,  Amol Kulkarni ,  E. Blake Watkins

IPC分类号： C07D239/26 ,  C07D213/50 ,  C07D307/54 ,  C07D215/14 ,  C07D213/65

摘要： This disclosure relates to compounds and methods of treating or preventing a Nox related disease or condition comprising administering to a subject in need thereof a Nox inhibitor or pharmaceutical compositions comprising a Nox inhibitor disclosed herein, derivatives, or compounds disclosed herein optionally substituted with one or more substitutes including optional salt and prodrug forms. In certain embodiments, this disclosure relates to sulfonylurea compounds and uses reported herein.