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 inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Abstract: Provided herein are compounds of Formula (I) and Formula (II) and stereoisomers, tautomers, and pharmaceutically acceptable salts or solvates thereof. Also provided are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition by using the compounds and pharmaceutical compositions.
Type:
Grant
Filed:
March 1, 2022
Date of Patent:
March 5, 2024
Assignee:
RECURSION PHARMACEUTICALS, INC.
Inventors:
Michael James Genin, Joseph Carpenter, Carl Brooks
Abstract: The present invention relates to a method for preventing transmission of influenza, wherein said method comprises administering an effective amount of a compound to a patient having an influenza virus infection, herein referred to as “index patient”, wherein the compound has one of the formulae (I) and (II), or its pharmaceutically acceptable salt. The compound to be used in the present invention reduces infectivity of the influenza virus of the index patient, and therefore, reduces the risk of the index patient to trigger an influenza epidemic or an influenza pandemic as compared to a control patient.
Type:
Grant
Filed:
December 23, 2021
Date of Patent:
February 27, 2024
Assignees:
Shionogi & Co., Ltd.
Inventors:
Takeshi Noshi, Takahiro Noda, Ryu Yoshida, Takao Shishido, Kaoru Baba, Aeron C. Hurt, Leo Yi Yang Lee, Steffen Wildum, Klaus Kuhlbusch, Barry Clinch, Jan Michal Nebesky, Annabelle Lemenuel, Wendy S. Barclay, Jean-Eric Charoin, Yoshinori Ando
Abstract: The present application provides tricyclic heteroaryl compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.
Abstract: Novel compounds having D3 receptor antagonistic activity are provided. A compound represented by formula (I): wherein ring A is a heterocycle, X1 is each independently CR4aR4b, X2 is each independently CR4cR4d, Y1 and Y2 are each independently a carbon atom or a nitrogen atom, L is —N(R6)—C(?O)— or the like, W is cyclyl or the like, R2 and R3 are each independently substituted or unsubstituted alkyl or the like, R1a, R1b, R4a to R4d, and R6 are each independently hydrogen atoms or the like, p is 1 or 2, q is an integer of 1 to 3, n is an integer of 1 to 4, s is an integer of 0 to 4, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 21, 2022
Date of Patent:
February 13, 2024
Assignee:
SHIONOGI & CO., LTD.
Inventors:
Hiroyuki Tobinaga, Koji Masuda, Masanao Inagaki, Manami Masuda
Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I): wherein A, D and Q are described herein.
Type:
Grant
Filed:
June 30, 2021
Date of Patent:
February 13, 2024
Assignee:
CARDIO THERAPEUTICS PTY LTD
Inventors:
Herbert Treutlein, Jun Zeng, Ian Dixon, Ian James, James T. Palmer
Abstract: Disclosed herein are compounds, compositions and methods for the treatment of neurological, psychiatric disorders which are characterized by a fundamental disruption of social behaviour, and substance use disorders. In particular, disclosed herein are compounds of Formula (I), or salts or prodrugs thereof. Methods of treating or preventing neurological, psychiatric disorders and substance use disorders, using compounds of Formula (I), or salts and prodrugs are also disclosed.
Type:
Grant
Filed:
May 7, 2021
Date of Patent:
February 6, 2024
Assignee:
Kinoxis Therapeutics Pty Ltd
Inventors:
Iain Stewart McGregor, Michael Kassiou, Michael Thomas Bowen, Callum Hicks, William Jorgensen
Abstract: Methods of selectively forming substituted pyrazines are provided. Methods of the present invention can include receiving a reaction solution including at least one carbon source and at least one nitrogen source, and heating the reaction solution to a reaction temperature and holding the reaction solution at the reaction temperature for a time sufficient to produce a reaction product comprising at least one substituted pyrazine. The carbon source can be selected from the group consisting of hydroxy ketone(s), sugar(s) treated with at least one buffer, and combinations thereof. Tobacco products incorporating substituted pyrazines are also provided.
Type:
Grant
Filed:
July 8, 2021
Date of Patent:
February 6, 2024
Assignee:
R.J. Reynolds Tobacco Company
Inventors:
Michael Francis Dube, William Monroe Coleman, III
Abstract: The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
Type:
Grant
Filed:
April 23, 2021
Date of Patent:
February 6, 2024
Assignee:
VALO HEALTH, INC.
Inventors:
Xiaozhang Zheng, Pui Yee Ng, Bingsong Han, Jennifer R. Thomason, Mary-Margaret Zablocki, Cuixian Liu, Heather Davis, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair, David S. Millan, Matthew W. Martin
Abstract: The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1P1 receptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
Type:
Grant
Filed:
July 14, 2021
Date of Patent:
January 30, 2024
Assignee:
Arena Pharmaceuticals, Inc.
Inventors:
Anthony C. Blackburn, Ryan O. Castro, Mark Allen Hadd, You-An Ma, Antonio Garrido Montalban, Jaimie Karyn Rueter, Lee Alani Selvey, Sagar Raj Shakya, Marlon Carlos
Abstract: The present disclosure discloses a method for preparing caprolactam including: (1) contacting cyclohexanone oxime with a catalyst to carry out reaction in the presence of ethanol and under the condition of gas phase Beckmann rearrangement reaction of cyclohexanone oxime; (2) separating the reaction product obtained in step (1) to produce an ethanol solution of crude caprolactam, and then separating the ethanol solution of crude caprolactam to obtain ethanol and crude caprolactam; (3) removing impurities with boiling points lower than that of caprolactam in the crude caprolactam to obtain a light component removal product; (4) mixing the light component removal product with a crystallization solvent to carry out crystallization and solid-liquid separation to obtain a crystalline crystal; (5) subjecting the crystalline crystal to a hydrogenation reaction; wherein the crystallization solvent contains 0.1-2 wt % of ethanol.
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
January 30, 2024
Assignee:
ZHEJIANG HENGYI PETROCHEMICAL RESEARCH INSTITUTE CO., LTD.
Inventors:
Shibiao Cheng, Songlin Wang, Xi Li, Han Wang, Fei Shen, Xinping Zhang, Zhaobin Jiang, Zhimin Hu
Abstract: The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is bisphosphate hemihydrate, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the treatment of cancer and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of such a co-crystal.
Type:
Grant
Filed:
August 27, 2021
Date of Patent:
January 23, 2024
Assignee:
UNIVERSITY HEALTH NETWORK
Inventors:
Sze-Wan Li, Heinz W. Pauls, Peter Brent Sampson
Abstract: Compounds of Formula (I) shown below and a pharmaceutical composition containing one of the compounds: Each of the variables is defined herein. Also disclosed is a method of treating a condition associated with uncontrolled cell growth with a compound of Formula (I).
Abstract: The invention provides non-centrosymmetric organic crystals which show exceptional self-healing properties. More particularly, the present invention provides non-centrosymmetric substituted imidazole and Dialkyl 4,4?-methylenebis(azanediyl)dibenzoate Crystals and a process for preparation thereof. These highly crystalline materials, when broken into pieces, can self-propel and re-join in the blink of an eye and repair themselves so precisely that they become indistinguishable from the undisturbed materials.
Type:
Grant
Filed:
July 26, 2022
Date of Patent:
January 16, 2024
Assignee:
Indian Institute of Science Education and Research (IISER) Kolkata
Abstract: The present disclosure is a pharmaceutical composition for the prevention or treatment of sepsis containing a thiamine derivative or a pharmaceutically acceptable salt thereof, wherein the pharmaceutical composition of the present disclosure can be used for the prevention, alleviation, or treatment of sepsis by containing fursultiamine or allithiamine to inhibit the expressions of CD40, CD86, and TNF?.
Type:
Grant
Filed:
December 21, 2021
Date of Patent:
January 16, 2024
Assignees:
KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION, KYUNGPOOK NATIONAL UNIVERSITY HOSPITAL
Inventors:
In Kyu Lee, Eun Jung Choi, Chang Hyun Jeon, Tae-Hwan Kwon, Dong Ho Park
Abstract: Antiviral drugs targeting the N-terminal domain (NTD) of the spike receptor binding domain (RBD) and methods of treating a subject suffering from coronavirus.
Type:
Grant
Filed:
August 11, 2022
Date of Patent:
January 9, 2024
Assignees:
Southwest Research Institute, The Henry M. Jackson Foundation for the Advancement of Military Medicine, Inc., The Government of the United States, as Represented by the Secretary of the Army
Inventors:
Jonathan A. Bohmann, Nadean M. Gutierrez, Joseph A. McDonough, Robert Francis Campbell, Michael Gordon Joyce, Rekha Panchal, Rajeshwer Sankhala, Allen Duplantier
Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Type:
Grant
Filed:
March 8, 2021
Date of Patent:
January 9, 2024
Assignee:
Agios Pharmaceutical, Inc.
Inventors:
Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
Abstract: Provided herein are compounds useful for the treatment of various parasitic diseases. These compounds, as well as pharmaceutically acceptable salts thereof may be formulated in pharmaceutical compostions, veterinary compositions and may be used in methods of treatment and/or prophylaxis of diseases spread by parasites, including malaria and cryptosporidiosis.
Type:
Grant
Filed:
July 28, 2021
Date of Patent:
January 9, 2024
Assignees:
THE BROAD INSTITUTE, INC., PRESIDENT AND FELLOWS OF HARVARD COLLEGE
Inventors:
Eamon Comer, Nobutaka Kato, Marshall Morningstar, Bruno Melillo
Abstract: A combination of active agents for the treatment of Lowe Syndrome (LS) comprising a RhoA inhibitor and a mTOR inhibitor; a pharmaceutical composition comprising the combination and a pharmaceutically acceptable carrier; a combination of pharmaceutical compositions in which one composition comprises a RhoA inhibitor and the other composition comprises a mTOR inhibitor; and a method of treating a patient for LS.