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:
October 3, 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 application relates to a novel, cost-saving and efficient process for preparing 4-(2,2,3,3-tetrafluoropropyl)morpholine which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
January 15, 2020
Date of Patent:
September 19, 2023
Assignee:
ADVERIO PHARM GmbH
Inventors:
Peter Fey, Sergii Pazenok, Christian Funke, Natalya Pavlovna Kolesnik, Olexandr Ivanovich Guzyr, Yuriy Grigorievich Shermolovich
Abstract: The invention relates to compounds and methods of treating diseases including but not limited to, cancer, non-cancer proliferative disease, sepsis, autoimmune disease, viral infection, atherosclerosis. Type 1 or 2 diabetes, obesity, inflammatory disease, or Myc-dependent disorder including by modulating biological processes by the inhibition of cell cycle checkpoint targets CDKs, and/or PI3 kinase, and/or bromodomain protein binding to substrates, comprising the administration of a compound(s) of Formula 1-V1 (or pharmaceutically acceptable salts thereof) as defined herein.
Type:
Grant
Filed:
January 26, 2018
Date of Patent:
September 19, 2023
Assignee:
SignalRx Pharmaceuticals, Inc.
Inventors:
Guillermo A. Morales, Joseph R. Garlich, Donald L. Durden
Abstract: Compositions and methods for the treatment or prophylaxis of viral and other infections (e.g., coronavirus) are provided. The compositions typically comprise a quinoline derivative and an additional anti-viral agent. Incorporations of these agents into fabrics for use as filtration devices which forestall infection is also disclosed.
Abstract: Provided herein are alpha5-containing GABAA receptor agonists and pharmaceutical compositions and methods of treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders using them.
Type:
Grant
Filed:
December 15, 2020
Date of Patent:
September 12, 2023
Assignees:
UWM Research Foundation, Inc., Centre for Addiction and Mental Health, University of Belgrade—Faculty of Pharmacy
Inventors:
James M. Cook, Guanguan Li, Michael Ming-Jin Poe, Miroslav M. Savic, Etienne Sibille
Abstract: The present invention relates to Compounds of Formula (I) or Formula (II): or a pharmaceutically acceptable salt, solvate or enantiomer thereof, wherein A, B, R1, R2, R3, R4, Q and V are as defined herein. The present invention also relates to pharmaceutical compositions comprising a Compound of Formula (I) or Formula (II) and to their use in therapy.
Type:
Grant
Filed:
November 24, 2020
Date of Patent:
August 22, 2023
Assignee:
MSD International GMBH
Inventors:
Cyril B. Dousson, David Dukhan, Christophe C. Parsy, Stephane L. Bogen
Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.
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