Abstract: In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
September 9, 2021
Date of Patent:
April 23, 2024
Assignees:
Memorial Sloan Kettering Cancer Center, St. Jude Children's Research Hospital
Inventors:
Jaeki Min, Daniel C. Scott, Deepak Bhasin, Brenda A. Schulman, Bhuvanesh Singh, Jared T. Hammill, R. Kiplin Guy
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:
June 15, 2022
Date of Patent:
April 16, 2024
Assignee:
Aligos Therapeutics, Inc.
Inventors:
Sandrine Vendeville, Pierre Jean-Marie Bernard Raboisson, David McGowan, Yannick Debing
Abstract: Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): wherein R1, R2, L1, and L2 are as defined herein.
Type:
Grant
Filed:
May 16, 2022
Date of Patent:
April 16, 2024
Assignee:
Agios Pharmaceuticals, Inc.
Inventors:
Giovanni Cianchetta, Tao Liu, Anil Kumar Padyana, Zhihua Sui, Zhenwei Cai, Dawei Cui, Jingjing Ji
Abstract: Provided are compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2A, R2B, R3, R4, and R5 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 4, 2022
Date of Patent:
April 9, 2024
Assignee:
CYTOKINETICS, INC.
Inventors:
Chihyuan Chuang, Bradley P. Morgan, Mark Vanderwal, Luke W. Ashcraft, Kevin Lau
Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small organic compound ligands that can raise LDL levels.
Type:
Grant
Filed:
September 14, 2020
Date of Patent:
April 2, 2024
Assignee:
SRX Cardio, LLC
Inventors:
Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
Abstract: The present disclosure concerns synthesis, anion binding features, liquid-liquid extraction of salts, and anti-corrosion character of aryl-triazole bicyclic macrocycles of Formula (I) and related compounds:
Type:
Grant
Filed:
May 22, 2019
Date of Patent:
March 26, 2024
Assignee:
Indiana University Research and Technology Corporation
Abstract: Provided herein are improved processes for the preparation of a compound of Formula IX (AG-10). Also provided herein are pharmaceutically acceptable salts of Formula I and Formula Ib as well as crystalline types of Formula IX (AG-10). The processes described herein provide improved yields and efficiency, while the pharmaceutically acceptable salts and crystalline forms provide unexpected pharmacokinetic properties. Other features and aspects of the present disclosure will be apparent to a person of skill in the art upon reading the remainder of the specification.
Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
Type:
Grant
Filed:
July 9, 2021
Date of Patent:
March 5, 2024
Assignee:
REATA PHARMACEUTICALS HOLDINGS, LLC
Inventors:
Eric Anderson, Xin Jiang, Melean Visnick
Abstract: The present invention provides methods and compositions for treating cancer, reducing side effects, and reducing postmenopausal symptoms comprising anordrin or analog thereof (such as anordrin) alone or in combination with at least one other agent selected from the group consisting of tamoxifen, raloxifene or functional equivalent thereof, and an aromatase inhibitor.
Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
Type:
Grant
Filed:
November 30, 2022
Date of Patent:
February 27, 2024
Assignees:
AMGEN INC., VIGIL NEUROSCIENCE, INC.
Inventors:
Lara C. Czabaniuk, Timothy Hopper, Jonathan B. Houze, Jane Panteleev, Gwenaella Rescourio, Vincent Santora, Haoxuan Wang, Ryan D. White, Alice R. Wong, Yongwei Wu, Maxence Bos, John Mancuso, Ivan Franzoni
Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.
Type:
Grant
Filed:
April 2, 2021
Date of Patent:
February 27, 2024
Assignee:
NOVARTIS AG
Inventors:
Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Le Grand, Katrin Spiegel
Abstract: The present invention relates to compositions and methods for the treatment of cancer and other diseases associated with mitochondrial dysfunction, including but not limited to, neurodegenerative disease, brain injuries, and certain non-neurological disorders, using a novel compound, 6-chloro-3-(2,4-dichloro-5-methoxyphenyl)-2-mercapto-7-methoxyquinazolin-4(3H)-one, and derivatives thereof.
Abstract: A carrier-free nanoparticle based on the self-assembly of curcumin-erlotinib conjugate (EPC) that exhibits stronger cell killing, better anti-migration effects, and anti-invasion effects for pancreatic cancer cells than the combination of free curcumin and erlotinib.
Abstract: The present invention relates to a process for the preparation of enantiomerically enriched 3-aminopiperidine, as in particular of its R-enantiomer (R)-3-aminopiperidine. The invention also relates to an enantiomerically enriched intermediate of said process and to specific acid-addition salts of 3-aminopiperidine (hereinafter also APIP) that are useful for obtaining a single enantiomer of APIP, and to crystalline (R)-3-aminopiperidine-dihydrochloride-monohydrate and crystalline (S)-3-aminopiperidine-dihydrochloride-monohydrate.
Type:
Grant
Filed:
September 9, 2022
Date of Patent:
February 13, 2024
Inventors:
Karl Reuter, Tobias Wedel, Viktor Meier, Mark Kantor, Vasyl Andrushko, Florian Stolz
Abstract: Method for preparing 3,7-bis(dimethylamino)phenothiazin-5-ylium iodide, the method resulting in a high purity while being very simple to implement and producing high yields. The method uses phenothiazine as a starting material and includes the following steps: a) treating phenothiazine with diiodine, b) treating the reaction medium directly obtained from step a) with dimethylamine.
Type:
Grant
Filed:
June 29, 2021
Date of Patent:
February 6, 2024
Assignee:
PROVEPHARM LIFE SOLUTIONS
Inventors:
Michel Feraud, Babak Sayah, Stéphane Queru, Marina Laurent
Abstract: The present invention provides in one aspect azabicyclo and diazepine derivatives useful as modulators of muscarinic receptors. In another aspect, the present invention provides pharmaceutical compositions for treating ocular diseases, the compositions comprising at least one muscarinic receptor modulator.
Abstract: Tri-component multi-functional boronated complexes (B-complexes), featuring reversible covalent bonds, are described, which incorporate a drug; a water-soluble moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins); and a targeting unit. A B-complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH). This platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate-receptor-positive MDA-MB-231 cancer cells, having an IC50 in the low nanomolar range.
Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
Type:
Grant
Filed:
November 30, 2022
Date of Patent:
January 30, 2024
Assignees:
AMGEN INC., VIGIL NEUROSCIENCE, INC
Inventors:
Lara C. Czabaniuk, Timothy Hopper, Jonathan B. Houze, Jane Panteleev, Gwenaella Rescourio, Vincent Santora, Haoxuan Wang, Ryan D. White, Alice R. Wong, Yongwei Wu, Maxence Bos, John Mancuso, Ivan Franzoni
Abstract: Imidazo[4,5-c]quinoline compounds of Formula (I) having a substituent that is attached at the N?1 position by a branched group, single enantiomers of the compounds, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in humans and animals, and in the treatment of diseases including infectious and neoplastic diseases are also disclosed.
Type:
Grant
Filed:
May 23, 2019
Date of Patent:
January 30, 2024
Assignee:
3M Innovative Properties Company
Inventors:
George W. Griesgraber, Hannah C. Cohen, Jana Ninkovic