Abstract: Described herein are compounds and pharmaceutical compositions of phenyl-pyrimidinyl-urea derivatives, which inhibit the activity of Olig2. An example of a phenyl-pyrimidinyl-urea derivative has the following structure: Also described herein are methods using the Olig2 inhibitors for treating cancer and other diseases. The Olig2 inhibitors may be used to treat glioblastoma.
Type:
Grant
Filed:
April 19, 2021
Date of Patent:
November 19, 2024
Assignee:
CURTANA PHARMACEUTICALS, INC.
Inventors:
Graham Beaton, Stanton F. McHardy, Ambrosio Lopez, Jr., Bismarck Campos, Hua-Yu Leo Wang
Abstract: The invention generally relates to solid forms of berberine ursodeoxycholate, and to pharmaceutical compositions, and methods of preparation and therapeutic use thereof. In particular, the invention relates to solid forms of berberine ursodeoxycholate and pharmaceutical compositions thereof useful in treating and/or preventing various diseases or disorders, including metabolic disorders, heart diseases, neurodegenerative diseases and liver diseases.
Abstract: A composition is prepared from a platinum-based antitumor compound and a novel compound, and the novel compound is sodium(S)-2-(dithiocarboxylate ((2S, 3R, 4R, 5R)-2,3,4,5,6-pentahydroxyhexyl)amino)-4-(methylthio)butyrate. The novel compound in the composition could effectively chelate the platinum-based antitumor compound and reduce the various adverse effects exhibited by the platinum-based compound. The dosage of the platinum-based antitumor compound can thus be increased, and the antitumor effect can be optimized. The novel compound itself is low-toxic and it has low chelating activities with essential metals in the human body; it would not impose significant adverse effects on the human body at given doses. The composition and its application as an antitumor drug overcome some technical drawbacks of platinum-based antitumor drugs, namely severe adverse effects and the development of drug resistance during administration.
Abstract: Novel pyrimido[6?,1?:2,3]imidazo[4,5-b][1,6]naphthyridine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrimido[6?,1?:2,3]imidazo[4,5-b][1,6]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
Abstract: Aqueous pharmaceutical compositions, suitable for topical ophthalmic administration to a mammal, that comprise a therapeutically effective amount of a prostaglandin, less than 0.3% w/v, and no added benzalkonium chloride, are provided. Such compositions are useful in methods comprising their topical administration to mammalian subjects, e.g., humans and reducing intraocular pressure and/or ocular hyperemia in the patient. Such compositions are also useful in methods comprising their topical administration to mammalian subjects, e.g., humans and promoting eyelash growth in the patient.
Abstract: The described compounds are of the class of cyclic nucleotides, both mono- and di-nucleotides, which play diverse roles in the prokaryotes and eukaryotes having the general formula which inhibit phosphodiesterases that inhibit cyclic mononucleotide or dinucleotides and/or both mononucleotide and dinucleotide. These compounds have potential diverse applications as antiviral, antibacterial, anti-inflammatory and anticancer agents, including cancer immunotherapy. Pharmaceutical compositions and methods for treating those kinase related diseases are within the scope of this invention.
Type:
Grant
Filed:
December 16, 2021
Date of Patent:
October 22, 2024
Assignee:
Purdue Research Foundation
Inventors:
Herman O. Sintim, George Naclerio, Caroline Karanja
Abstract: Disclosed in the present invention are a fused pyridone compound, and a preparation method therefor and a use thereof. Specifically, the present invention discloses a compound of formula (I-B), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.
Abstract: A sterile, ready-to-use pharmaceutical composition having hydralazine and/or a salt thereof at a concentration of less than about 20 mg/mL and a solvent comprising an organic co-solvent, wherein the hydralazine and/or salt thereof and the organic co-solvent are provided at a first weight ratio sufficient for the hydralazine and/or salt thereof to have a change in concentration of no more than about 10% after 2 months of storage at 60° C. Also described are methods of making and using the composition.
Type:
Grant
Filed:
December 27, 2022
Date of Patent:
October 8, 2024
Assignee:
ENDO OPERATIONS LIMITED
Inventors:
Kumaresh Soppimath, Tushar Hingorani, Hari A. Attluri, Harshil H. Jain
Abstract: The present technology provides triazolones, tetrazolones, and imidazolones, or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The triazolones, tetrazolones, and imidazolones or their pharmaceutically acceptable salts exhibit inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).
Type:
Grant
Filed:
April 21, 2022
Date of Patent:
October 8, 2024
Assignee:
Yuhan Corporation
Inventors:
Hee Jae Tak, Eun Kyung Kim, Hyok Jun Cho, Cheol Hee Lim
Abstract: The invention relates to crystalline tranilast salts. The crystalline tranilast salts, their preparation and their characterization are described and shown in the figures. The invention relates to pharmaceutical compositions containing a crystalline tranilast salt of the invention and a pharmaceutically acceptable carrier. The invention also relates to methods of treatment and the use of a therapeutically effective amount of a crystalline tranilast salt of the invention for treatment. The invention also relates to a method of preparing a liquid pharmaceutical composition comprising the step of dissolving a crystalline tranilast salt of the invention in a pharmaceutically acceptable solvent and to liquid pharmaceutical compositions prepared according to that method.
Abstract: The present disclosure concerns methods of detecting injury to a tissue and/or organ in a subject. In some aspects, the subject is the recipient of a transplant, such as a liver transplant. In some aspects, the subject is undergoing treatment with an immunosuppressant. In some aspects, the present disclosure concerns the identification of aberrant mitochondria in the subject to identify injury to the tissue and/or organ of the subject. Detecting aberrant mitochondria allows for remedial and/or corrective action to prevent or avoid significant injury.
Abstract: This disclosure relates to low molecular weight substituted imidazoles that inhibit the TGF-b signaling pathway. More specifically, this disclosure relates to methods of using said imidazoles for the treatment of diseases related to the TGF-b signaling pathways including, but not limited to, atherosclerosis, Marfan syndrome, Loeys-Dietz syndrome, obesity, diabetes, multiple sclerosis, keratoconus, idiopathic pulmonary fibrosis, Alzheimer's Disease, chronic kidney disease, and scleroderma.
Abstract: Disclosed is a method of treating in a subject hair loss disorders that are beneficially treated by administering a JAK1 and/or JAK2 inhibitor. The method comprises administering to the subject an amount in the range of about 4 mg to about 50 mg of Compound (I): or a pharmaceutically acceptable salt thereof. This invention also provides compositions comprising Compound (I) and the use of such compositions in the described methods.
Type:
Grant
Filed:
December 5, 2019
Date of Patent:
September 3, 2024
Assignee:
Sun Pharmaceuticals Industries, Inc.
Inventors:
Amanda T. Wagner, James V. Cassella, Philip B. Graham, Virginia Braman, Vinita Uttamsingh, Jana Von Hehn, Colleen E. Hamilton
Abstract: The present invention provides methods and compositions for modulating molecular markers, and hence treating or preventing breast cancer (e.g., triple-negative breast cancer) and melanoma with a pharmaceutically effective amount of S-equol or a pharmaceutical composition comprising S-equol. The S-equol may be administered alone or in combination with one or more cytotoxic or immunotherapeutic compound or molecule.
Type:
Grant
Filed:
November 24, 2021
Date of Patent:
August 27, 2024
Assignee:
Board of Regents, The University of Texas System
Abstract: A method for catalytically synthesizing furaneol, which uses a specific peptide to function as a catalyst, uses rhamnose to function as a raw material, and uses an organic solvent and a phosphate buffer to function as a reaction solvent to be co-heated to prepare furaneol.
Type:
Grant
Filed:
September 20, 2021
Date of Patent:
August 27, 2024
Assignee:
Xiamen Oamic Biotech Co., Ltd.
Inventors:
Chupei Xu, Zhou Zhu, Shunchuan Ke, Yibin Zhang, Gang Liu
Abstract: The present disclosure is related to processes for preparing baricitinib, salts thereof, and related synthetic intermediate compounds and salts thereof.
Type:
Grant
Filed:
July 11, 2022
Date of Patent:
August 27, 2024
Assignee:
Incyte Corporation
Inventors:
Jiacheng Zhou, Shili Chen, Zhongjiang Jia, Pingli Liu, David Meloni, Yongchun Pan, Naijing Su, Michael Xia
Abstract: The present disclosure provides compounds according to Formula I or a pharmaceutically acceptable salt thereof: wherein each variable is as defined and described herein, compositions thereof, and methods of using the same for the inhibition of CDK2, and the treatment of CDK2 related diseases and disorders.
Type:
Grant
Filed:
January 28, 2022
Date of Patent:
August 20, 2024
Assignee:
Cedilla Therapeutics, Inc.
Inventors:
Louise Clare Kirman, Carl Eric Schwartz, Wojtek Michowski, Dale A. Porter, Jr., Justin Ripper, John Feutrill, John Paul Sherrill, Thomas P. Blaisdell
Abstract: A composition containing a compound of formula I or a pharmaceutically acceptable salt, dimer or trimer thereof, and a tyrosine kinase activity inhibitor is provided. A method of preventing and/or treating cancer by administering a subject in need thereof the composition is provided. The combination of Sotagliflozin and a tyrosine kinase activity inhibitor may exhibit a synergistic inhibitory effect on tumors, and the efficacy of the combination is significantly better than that of a single drug.
Type:
Grant
Filed:
August 19, 2020
Date of Patent:
July 30, 2024
Assignee:
NEWISH TECHNOLOGY (BEIJING) CO., LTD.
Inventors:
Hailong Qi, Xiaofang Wang, Zhongjie Sun
Abstract: Provided herein are novel conjugates of TGF-beta inhibitors and bisphosphonates, pharmaceutical compositions comprising the conjugates, methods of preparing the conjugates, and methods of using the conjugates, for example, for the treatment of a bone disease or disorder, such as osteoarthritis.
Abstract: The present disclosure provides processes for the purification of 2,5-furandicarboxylic acid (FDCA). The present disclosure further provides crystalline preparations of purified FDCA, as well as processes for making the same. In addition, the present disclosure provides mixtures used in processes for the purification of FDCA.
Type:
Grant
Filed:
November 30, 2021
Date of Patent:
July 30, 2024
Assignee:
Stora Enso Oyj
Inventors:
Henricus Johannes Cornelis Den Ouden, Valery Sokolovskii, Thomas R. Boussie, Gary M. Diamond, Eric L. Dias, Guang Zhu, Staffan Torssell, Vincent J. Murphy