公开(公告)号：WO2022006340A1

公开(公告)日：2022-01-06

申请号：PCT/US2021/039995

申请日：2021-06-30

申请人： SILVERBACK THERAPEUTICS, INC.

发明人： SMITH, Sean W. ,  BAUM, Peter R. ,  DUBOSE, Robert ,  ODEGARD, Valerie ,  TAN, Philip ,  THOMPSON, Peter A. ,  STEVENS, Brenda ,  HUNT, Kevin W.

IPC分类号： C07D401/14 ,  C07K5/062 ,  C07K5/065 ,  C07K5/093 ,  C07K5/113 ,  C07K7/06 ,  A61K31/498 ,  A61K47/68 ,  A61P35/00 ,  A61K47/6803 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/0819 ,  C07K5/1021

摘要： ALK5 inhibitor compounds, conjugates, and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. Additionally, compounds incorporated into a conjugate with an antibody construct are described herein.The disclosed compoundsand conjugates are useful, among other things, in the treating of cancer and fibrosis and modulating ALK5.

公开(公告)号：WO2021222687A8

公开(公告)日：2021-11-04

申请号：PCT/US2021/030063

申请日：2021-04-30

申请人： MEDSTAR HEALTH ,  FISHBEIN, Thomas, M. ,  KHAN, Khalid, M. ,  KROEMER, Alexander, H.

发明人： FISHBEIN, Thomas, M. ,  KHAN, Khalid, M. ,  KROEMER, Alexander, H.

IPC分类号： C07K5/062 ,  C07K5/06 ,  C07D307/02 ,  C07D405/12 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06052

摘要： The invention relates to methods for treating COVID- 19 by targeting the inflammasome/caspase1/pyroptosi s axis as a key inflammatory pathway. In particular, the invention relates to treating a patient infected with SARS-CoV-2 with an effective amount of one or more compounds that directly or indirectly inhibit one or more pathways of the inflammasome/caspasel/pyroptosis axis.

公开(公告)号：WO2021260232A1

公开(公告)日：2021-12-30

申请号：PCT/EP2021/067754

申请日：2021-06-28

申请人： SYNAFFIX B.V.

发明人： VERKADE, Jorge Merijn Mathieu ,  VAN BERKEL, Sander Sebastiaan ,  VAN DELFT, Floris Louis

IPC分类号： C07C307/04 ,  C07D207/46 ,  A61K47/50 ,  A61K47/54 ,  A61K47/6889 ,  C07C2602/46 ,  C07D249/18 ,  C07D471/04 ,  C07D519/00 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/06156 ,  C07K5/0806

摘要： The present invention concerns a method for the preparation of an alkyne-linker-payload construct of structure Q-L-C (O)-NR3-D (1), comprising reacting (i) an alkyne compound of structure Q-L- C(O)-X (2), wherein Q is an alkyne moiety selected from the group consisting of terminal alkyne and (hetero)cycloalkyne; L is a linker, and X is a leaving group selected from halogen, SR1, O-succinimidyl, O-(hetero)aryl(R2)1-5, wherein R1 is selected from C1 - C6 alkyl and (hetero)aryl; and R2 is C1 - C6 alkyl, halogen or NO2; with (ii) a molecule of structure D-NHR3 (3), wherein D is a payload, and R3 is selected from hydrogen, optionally substituted C1 - C24 alkyl, optionally substituted aryl. The activated ester derivatives (2) are highly stable and provide for smooth and high-yielding attachment to a cytotoxic payload. The invention further concerns a method for preparing bioconjugates and alkyne compound of structure Q-L-C (O)-X (2).

公开(公告)号：WO2021207409A2

公开(公告)日：2021-10-14

申请号：PCT/US2021/026253

申请日：2021-04-07

申请人： ARIZONA BOARD OF REGENTS ON BEHALF OF THE UNIVERSITY OF ARIZONA

发明人： WANG, Jun ,  MA, Chunlong

IPC分类号： C07C271/32 ,  A61K38/05 ,  C07K5/06 ,  A61P31/12 ,  A61K31/00 ,  C07C2601/02 ,  C07C2601/14 ,  C07C317/28 ,  C07C323/60 ,  C07K5/06026 ,  C07K5/06052 ,  C07K5/06078 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/1016

摘要： This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical agents which function as inhibitors of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral replication and/or SARS-CoV-2 related viral 3CL protease (Mpro) activity. The invention further relates to methods of treating and/or ameliorating symptoms related to conditions caused by the SARS-CoV-2 virus (e.g., COVID-19), comprising administering to a subject (e.g., a human patient) a composition comprising one or more pharmaceutical agents which function as inhibitors of SARS-CoV-2 viral replication and/or inhibitors of SARS-CoV-2 related Mpro activity.