公开(公告)号：US20230131121A1

公开(公告)日：2023-04-27

申请号：US17827479

申请日：2022-05-27

申请人： QUANTA BIODESIGN, LTD. ,  UNIVERSITY OF WASHINGTON

发明人： Paul D. DAVIS ,  D. Scott WILBUR

IPC分类号： C07D209/60 ,  C07C271/16 ,  C07C279/24 ,  C07D403/14 ,  C07C317/44 ,  C07C331/28 ,  C07K14/605 ,  C07D257/02 ,  C07C235/08 ,  C07C235/48 ,  C07D207/404 ,  C07D209/48 ,  C07K16/30 ,  C07K16/40 ,  A61K51/10 ,  A61K47/60

摘要： 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 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：US11628161B2

公开(公告)日：2023-04-18

申请号：US17665456

申请日：2022-02-04

申请人： Kangpu Biopharmaceuticals, Ltd.

发明人： Wen-Cherng Lee ,  Baisong Liao ,  Lei Zhang

IPC分类号： A61K31/473 ,  A61K31/4035 ,  A61K45/06 ,  C07D209/48 ,  C07D401/06 ,  C07D471/04 ,  A61K31/437 ,  A61K31/4439

摘要： Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α so as to effectively treat cancer and inflammatory diseases.

公开(公告)号：US20220356205A1

公开(公告)日：2022-11-10

申请号：US17760760

申请日：2021-02-18

申请人： NATIONAL UNIVERSITY CORPORATION HOKKAIDO UNIVERSITY

发明人： Shigeki MATSUNAGA ,  Tatsuhiko YOSHINO ,  Keitaro MATSUOKA ,  Mikako OGAWA

IPC分类号： C07J1/00 ,  C07D209/48 ,  C07C69/712 ,  C07D215/16 ,  C07D333/62 ,  C07D261/20

摘要： This method for producing an aromatic astatine compound comprises reacting an aromatic iodonium ylide with astatine to produce an aromatic astatine compound.

公开(公告)号：US11440881B2

公开(公告)日：2022-09-13

申请号：US16869749

申请日：2020-05-08

申请人： THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH

发明人： Yousef Al-Abed ,  Ahmad Altiti

IPC分类号： C07D209/48 ,  C07D403/12

摘要： Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.

公开(公告)号：US11440880B2

公开(公告)日：2022-09-13

申请号：US17083898

申请日：2020-10-29

申请人： The USA, as represented by the Secretary, Department of Health and Human Services ,  University Court of the University of Aberdeen

发明人： Nigel H. Greig ,  Weiming Luo ,  David Tweedie ,  Neil Vargesson ,  Shaunna Beedie ,  William Douglas Figg

IPC分类号： C07D209/44 ,  C07D401/14 ,  C07D401/04 ,  C07D417/04 ,  C07D499/80 ,  C07D209/48 ,  C07D209/52 ,  C07D209/46 ,  C07D401/12 ,  C07D413/04 ,  C07D471/04 ,  A61P29/00 ,  A61P35/00 ,  A61K31/4035 ,  A61K31/431 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/536 ,  A61K45/06 ,  A61K31/428

摘要： Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.

公开(公告)号：US20220259154A1

公开(公告)日：2022-08-18

申请号：US17539679

申请日：2021-12-01

申请人： Arvinas Operations, Inc.

发明人： Michael BERLIN ,  Andrew P. CREW ,  Craig M. CREWS ,  Hanqing DONG ,  Keith R. HORNBERGER ,  Lawrence B. SNYDER ,  Jing WANG ,  Kurt ZIMMERMANN

IPC分类号： C07D233/42 ,  A61K31/166 ,  C07D211/76 ,  C07D241/04 ,  C07D231/12 ,  C07D213/72 ,  C07D205/04 ,  C07D237/08 ,  C07D239/24 ,  C07D221/20 ,  A61K31/277 ,  A61K47/10 ,  A61K31/02 ,  A61K31/497 ,  C07D209/48 ,  C07D401/14 ,  A61K45/06 ,  A61K31/506 ,  A61K31/496 ,  A61K31/501 ,  C07D401/04

摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US11339146B2

公开(公告)日：2022-05-24

申请号：US16877291

申请日：2020-05-18

申请人： Ottawa Hospital Research Institute ,  University of Ottawa

发明人： Jean-Simon Diallo ,  Christopher Noyce Boddy ,  Mark Dornan ,  Ramya Krishnan ,  Rozanne Arulanandam ,  Fabrice Le Boeuf ,  Jeffrey Smith ,  Andrew Macklin

IPC分类号： A61K31/501 ,  C07D413/06 ,  C07D237/14 ,  C07D207/38 ,  C07D307/60 ,  C07D307/66 ,  C07D401/06 ,  C07D403/06 ,  C07D405/04 ,  C07D405/12 ,  C07D409/06 ,  C07D307/30 ,  C07D307/58 ,  C07D405/06 ,  A61K45/06 ,  C12N7/00 ,  C07D207/36 ,  C07D207/456 ,  C07D317/64 ,  C07D417/06 ,  C07D471/04 ,  A61P35/02 ,  C07D209/48 ,  C07D231/08 ,  A61K31/341

摘要： Provided are compounds of Formula (II) that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

公开(公告)号：US20220152002A1

公开(公告)日：2022-05-19

申请号：US17665456

申请日：2022-02-04

申请人： Kangpu Biopharmaceuticals, Ltd.

发明人： Wen-Cherng Lee ,  Baisong Liao ,  Lei Zhang

IPC分类号： A61K31/437 ,  A61K31/4035 ,  A61K31/4439 ,  A61K45/06 ,  C07D209/48 ,  C07D401/06 ,  C07D471/04

摘要： Disclosed are a novel isoindoline derivative, a pharmaceutical composition and use thereof. The compound of formula I, or the pharmaceutically acceptable salt, solvate, polymorph, co-crystal, stereoisomer, isotopic compound, metabolite or prodrug thereof disclosed in the invention can regulate the generation and/or activity of PDE4 and/or TNF-α, so as to effectively treat cancer and inflammatory diseases.

公开(公告)号：US11306072B2

公开(公告)日：2022-04-19

申请号：US16790611

申请日：2020-02-13

申请人： City of Hope ,  National and Kapodistrian University of Athens

发明人： Richard Jove ,  Sangkil Nam ,  David Horne ,  Jun Xie ,  Alexios Leandros Skaltsounis ,  Marina Kritsanida ,  Nicolas Gaboriaud-Kolar

IPC分类号： C07D403/14 ,  C07D401/04 ,  C07D209/40 ,  C07D209/48 ,  A61K45/06 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/496 ,  C07D401/14

摘要： Disclosed herein inter alia are compositions and methods for treating cancer using 5-Br-indirubin derivatives.

公开(公告)号：US11260046B2

公开(公告)日：2022-03-01

申请号：US17003238

申请日：2020-08-26

申请人： AMGEN INC.

发明人： George W. Muller ,  Peter H. Schafer ,  Hon-Wah Man ,  Chuansheng Ge

IPC分类号： C07C317/28 ,  A61K31/4035 ,  C07D209/48 ,  A61K45/06

摘要： Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (−) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-α or the inhibition of PDE4.