Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Type:
Grant
Filed:
June 25, 2021
Date of Patent:
June 6, 2023
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Somasekhar Bhamidipati, Simon Shaw, Ihab Darwish, Jiaxin Yu, Rao Kolluri, Vanessa Taylor, Esteban Masuda, Mark Irving
Abstract: The present invention is directed to tetramaleimide linkers and use thereof, more specifically to the compounds represented by formula I and their use in the preparation of antibody-drug conjugates (ADCs). The ADCs obtained from the tetramaleimide linkers have high homogeneity and stability, and could be used effectively for the treatment of various diseases including tumors. The definition of the groups in formula I is the same as that in the description.
Type:
Grant
Filed:
April 18, 2018
Date of Patent:
June 6, 2023
Assignee:
NewBio Therapeutics, Inc.
Inventors:
Deqiang An, Nianhe Han, Peng Zhu, Di Zeng, Baoxiang Wang, Huali Li, Chun Yang
Abstract: Provided herein are heterocyclic compounds useful for imaging Granzyme B. Methods of imaging Granzyme B, combination therapies, and kits comprising the Granzyme B imaging agents are also provided.
Type:
Grant
Filed:
February 13, 2019
Date of Patent:
June 6, 2023
Assignee:
CytoSite Biopharma Inc.
Inventors:
Geoffrey Malcolm Bilcer, Terence Alfred Kelly
Abstract: The present invention pertains to a medicament for preventing or treating cough, including, as an active ingredient, a compound having P2X4 receptor antagonistic action, a tautomer, stereoisomer, or pharmaceutically acceptable salt of the compound, or a hydrate or solvate thereof.
Abstract: The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
February 8, 2021
Date of Patent:
June 6, 2023
Assignee:
AstraZeneca AB
Inventors:
Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan Po Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne Macritchie, Nicholas John Palmer
Abstract: The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
September 10, 2022
Date of Patent:
May 23, 2023
Assignee:
AstraZeneca AB
Inventors:
Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan Po Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne Macritchie, Nicholas John Palmer
Abstract: The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
September 10, 2022
Date of Patent:
May 23, 2023
Assignee:
AstraZeneca AB
Inventors:
Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan P O Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne MacRitchie, Nicholas John Palmer
Abstract: The present disclosure relates to certain (2S)—N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
September 9, 2022
Date of Patent:
May 23, 2023
Assignee:
AstraZeneca AB
Inventors:
Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan Po Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne Macritchie, Nicholas John Palmer
Abstract: The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
Type:
Grant
Filed:
September 10, 2022
Date of Patent:
May 23, 2023
Assignee:
AstraZeneca AB
Inventors:
Hans Roland Lönn, Stephen Connolly, Steven Swallow, Staffan Po Karlsson, Carl-Johan Aurell, John Fritiof Pontén, Kevin James Doyle, Amanda Jane Van De Poël, Graham Peter Jones, David Wyn Watson, Jaqueline Anne Macritchie, Nicholas John Palmer
Abstract: Disclosed herein are embodiments of a compound that inhibits c-Abl tyrosine kinase (also referred to herein as “c-Abl”). The compound embodiments described herein are novel c-Abl inhibitors that can bind to c-Abl at an allosteric site and inhibit its activity in various pathways. The compound embodiments also are capable of crossing the blood brain barrier and therefore are useful in inhibiting c-Abl activity as it affects pathways and/or proteins in the brain. The compound embodiments described herein are effective therapeutic agents for treating diseases involving c-Abl, such as cancers, motor neuron diseases, and neurodegenerative diseases. Also disclosed herein are embodiments of methods for making and using the c-Abl inhibitory compound embodiments.
Type:
Grant
Filed:
March 8, 2019
Date of Patent:
May 16, 2023
Assignees:
The United States of America, as represented by the Secretary, Department of Health and Human Services, Pontificia Universidad Catolica de Chile
Inventors:
Juan J. Marugan, Marc Ferrer, Noel T. Southall, Andres E. Dulcey, Xin Hu, Christopher R. Dextras, Daniel C. Talley, Alejandra Alvarez, Silvana Zanlungo, Rommy M. Von Bernhardi
Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I? and I?? or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
Type:
Grant
Filed:
December 28, 2020
Date of Patent:
May 16, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I? and I?? or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
Type:
Grant
Filed:
December 28, 2020
Date of Patent:
May 16, 2023
Assignee:
Achillion Pharmaceuticals, Inc.
Inventors:
Jason Allan Wiles, Avinash S. Phadke, Milind Deshpande, Atul Agarwal, Dawei Chen, Venkat Rao Gadhachanda, Akihiro Hashimoto, Godwin Pais, Qiuping Wang, Xiangzhu Wang, William Greenlee
Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
Type:
Grant
Filed:
November 19, 2020
Date of Patent:
May 9, 2023
Assignee:
Nocion Therapeutics, Inc.
Inventors:
Bridget McCarthy Cole, James Lamond Ellis
Abstract: The present invention is directed to compounds, compositions and methods for preventing, treating or curing Hepatitis B (HBV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment, prevention or eradication of HBV infection.
Type:
Grant
Filed:
August 20, 2020
Date of Patent:
April 18, 2023
Assignee:
Emory University
Inventors:
Raymond F. Schinazi, Sebastien Boucle, Franck Amblard, Ozkan Sari, Leda Bassit
Abstract: Disclosed is an advancement in provoked chemical cleavage. Thereby the invention provides the use of a diene as a chemically cleavable group attached to a Construct, and the use of a dienophile to provoke the release of the Construct by allowing the diene to react with a dienophile capable of undergoing an inverse electron demand Diels Alder reaction with the diene. The invention includes a kit for releasing a Construct CA bound to a Trigger TR, the kit having a tetrazine and a dienophile, wherein the Trigger is the tetrazine. The invention also includes the use of the formation of a pyridazine by reacting a tetrazine having a Construct CA bound thereto and a dienophile, as a chemical tool for the release, in a chemical, biological or physiological environment, of the Construct.
Inventors:
Marc Stefan Robillard, Wolter Ten Hoeve, Freek Johannes Maria Hoeben, Ronny Mathieu Versteegen, Hendricus Marie Janssen, Arthur Henry Antoon Marie Van Onzen, Raffaella Rossin
Abstract: Disclosed are methods and compositions for treating ore preventing a STAT5-mediated medical condition, e.g., rheumatoid arthritis, in a subject by administering to the subject a therapeutically effective amount of a compound, the compound being a STAT5 inhibitor, or a pharmaceutically acceptable salt of the STAT5 inhibitor, or a solvate of the STAT5 inhibitor, or a prodrug of the STAT5 inhibitor. In one example, the compound used in the methods and compositions is pimozide. In another example, the compound used in the methods and compositions is nicotinohydrazide.
Abstract: This disclosure generally relates to novel processes for the preparation of drug linker compounds and compositions comprising such drug linker compounds. The presently disclosed methods for synthesizing Fmoc-Val-Cit-PABOH and related compounds have also been found to minimize formation of diastereomeric impurities.
Abstract: The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
Type:
Grant
Filed:
November 12, 2020
Date of Patent:
March 14, 2023
Assignee:
Nocion Therapeutics, Inc.
Inventors:
Bridget McCarthy Cole, James Lamond Ellis
Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 15, 2020
Date of Patent:
February 28, 2023
Assignee:
Aligos Therapeutics, Inc.
Inventors:
Sandrine Vendeville, Pierre Jean-Marie Bernard Raboisson, Yannick Debing