Abstract: Provided herein is a compound of Formula (I-I), or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g. in the treatment of CNS-related disorders.
Type:
Grant
Filed:
January 11, 2019
Date of Patent:
August 8, 2023
Assignee:
Sage Therapeutics, Inc.
Inventors:
Albert Jean Robichaud, Francesco G. Salituro, Maria Jesus Blanco-Pillado, Daniel La, Boyd L. Harrison
Abstract: The present invention concerns reagents for the reversible protection of biological molecules. It relates in particular to compounds derived from azaisatoic anhydride and their uses for the protection of biological molecules, particularly enzymes, in order to block their activity. The invention also relates to the biological molecules protected in this manner and to the methods for making use of these reagents.
Type:
Grant
Filed:
July 13, 2017
Date of Patent:
July 25, 2023
Assignees:
BIOMÉRIEUX, UNIVERSITÉ DE CAEN NORMANDIE
Inventors:
Sylvain Ursuegui, Alain Laurent, Ali Laayoun, Frédéric Fabis
Abstract: The invention relates to compounds of the formula: and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of inflammatory diseases, fibtrotic diseases and neoplastic diseases.
Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formulae I or Formula II: where R, L, X1, X2, X3, X4, X5, Y1, Y2, Y3, and Y4 are described herein.
Type:
Grant
Filed:
December 17, 2020
Date of Patent:
July 18, 2023
Assignee:
Valo Health, Inc.
Inventors:
Xiaozhang Zheng, Pui Yee Ng, Aleksandra Rudnitskaya, David R. Lancia, Jr.
Abstract: Provided herein are methods for treating uveal melanoma in a subject in need thereof by administering an effective amount of an agent that inhibits expression of FAK protein to the subject. In one aspect, the agent that inhibits expression of FAK protein comprises, or alternatively consists essentially of, or yet further consists of a gene editing agent, such as for example one or more of: RNA interference (RNAi), CRISPR/Cas, ZFN, and/or TALEN. In another aspect, the agent is VS-4718. Also described herein are kits comprising, or alternatively consisting essentially of, or yet further consisting of one or more of: agents that inhibit expression of FAK protein, siRNAs, shRNAs, miRNAs, nucleases and/or guide RNA sequences for carrying out the methods of this disclosure, and optional instructions for use.
Type:
Grant
Filed:
March 19, 2020
Date of Patent:
June 20, 2023
Assignee:
The Regents of the University of California
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 15, 2022
Date of Patent:
June 20, 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 invention relates to Ibogaine derivatives and related methods. It more specifically relates to deutero- and fluoro-derivatives of Ibogaine and related methods. In one aspect, the present invention provides a compound. The structure of the compound is shown as compound 1 in FIG. 1. In another aspect, the present invention provides a method of treating an addiction disorder. The method comprises administration of compound 1. In another aspect, the present invention provides a method of treating an anxiety-related disorder or impulse control disorder. The method comprises administration of compound 1.
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:
June 13, 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 invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin V1a and V2 antagonisms, and medical uses thereof. In the formula, R1 is optionally substituted C1-6 alkyl, etc.; L is —C(?O)—NH—, etc.; Ring A1 is a hydrocarbon ring, etc.; Ring A2 is a hydrocarbon ring, etc.; and each of Rings A1 and A2 may have at least one substituent.
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 16, 2022
Date of Patent:
June 13, 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 invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
Type:
Grant
Filed:
September 24, 2020
Date of Patent:
June 6, 2023
Assignees:
Novartis AG, Gilead Sciences, Inc.
Inventors:
Zef Konst, Yipin Lu, Robert Joseph Moreau, Naomi Samadara Rajapaksa, Galen Shearn-Nance, David Charles Tully, Michael Robert Turner, Joseph Michael Young, Qian Zhao, Britton K. Corkey, Samuel E. Metobo
Abstract: Disclosed are solid state forms of Rucaparib and of Rucaparib salts, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
December 15, 2020
Date of Patent:
June 6, 2023
Assignee:
ASSIA CHEMICAL INDUSTRIES LTD.
Inventors:
Dijana S. Samec, Jasna Dogan, Tomislav Biljan, Maja M. Skugor, Moris Mihovilovic, Tina Mundorfer, Nikolina Janton, Mihaela Tuksar, Sara M. Pipercic, Nea Baus Topic
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