Abstract: The present invention provides, inter alia, compounds capable of inhibiting NF-?B. Pharmaceutical compositions containing and methods of using the compounds are also provided herein. Also provided are methods and kits for treating cancer and solid tumors in a subject, as well as methods and kits for inducing cancer cell death and apoptosis of a cancer cell, all utilizing the NF-?B inhibitors described herein.
Abstract: The present invention relates to a drug that is for treating or preventing cancer, that is effective in the treatment of cancer, and that comprises a combination of an ALK inhibitor and a VEGF inhibitor. The present invention also relates to a method for treating or preventing cancer and a method for inhibiting tumor growth.
Abstract: Tetrahydroberberine (THB), isolated from the Chinese herb “Corydalis ambigua”, exhibits a variety of pharmacological effects, although mechanisms of action are unclear or entirely unknown. Described herein are novel methods of using tetrahydroberberine (THB), THB analogs or derivatives, tetrahydroprotoberberines (THPB). Tetrahydroberberine (THB) and analogs such as l-stepholidine (l-SPD) potently block functional KATP channels natively expressed on midbrain dopamine neurons. Further, THB also blocks pancreatic ?-cell KATP channels, and can be developed to a novel drugs for treating disease and/or conditions such as diabetes and Parkinson's disease.
Abstract: Disclosed are compositions for the treatment of emotional pain, physical pain, and insomnia comprising a compound comprising an opioid antagonist that treats pain by blocking Toll-like receptor 4 (TLR4). Examples of opioid antagonist include naltrexone and naloxone, and their use in the treatment, prevention, and reversal of pain.
Abstract: Disclosed are a compound represented by general formula I and a preparation method therefor. The compound can be used as indoleamine-2,3-dioxygenase inhibitor to prepare medicines for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
Type:
Grant
Filed:
September 15, 2015
Date of Patent:
July 6, 2021
Assignee:
Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences
Abstract: This invention discloses uses for sulindac in preparing anti-lung cancer products. This invention provides uses for sulindac in the preparation of products to treat lung cancer. From carrying out cancer drug repositioning for the FDA- and CFDA-approved drug sulindac, experiments for this invention show, based on screening of non-anti-cancer drugs for various cancer cell lines (tissue types) and mutation sites, that sulindac has a new use as an anti-lung cancer medication, thus achieving a new purpose for an old drug.
Abstract: Pharmaceutical compositions for intraocular injection are described, the compositions comprise therapeutically effective quantity of lyophilized preservative-free and sulfite-free epinephrine or adrenaline and a metal chelator. Methods for fabricating the compositions and using them for intraocular injections are also described.
Abstract: The present invention provides a prophylactic or therapeutic agent for Alzheimer's disease (AD) containing a combination of two or more compounds selected from the group consisting of compounds shown by compound Nos. 1 to 130. Since these compounds are existing drugs that have already been confirmed actually for safety and pharmacokinetics in human, they can be a means for a pre-emptive treatment of people at risk of AD and in a stage before developing mild cognitive impairment (MCI).
Abstract: The present invention relates to a compound which is (R)-3-(1,4-dimethyl-1H-benzo[d][1,2,3]triazol-5-yl)-3-(3-(((R)-2-ethyl-2,3-dihydropyrido[2,3-f][1,4]oxazepin-4(5H)-yl)methyl)-4-methylphenyl)propanoic acid (I), or a pharmaceutically acceptable salt thereof, in particular, the meglumine salt thereof, a pharmaceutical composition containing the compound and its use as an NRF2 activator.
Type:
Grant
Filed:
December 11, 2017
Date of Patent:
June 8, 2021
Assignee:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Abstract: The present application relates to strontium L-lactate compositions and methods of use. The methods and compositions disclosed herein are particularly useful for providing bioavailable strontium to mammals and treating or preventing symptoms of bone and/or cartilage disorders.
Abstract: The present invention provides compositions or formulations comprising the combination of a compound of 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione or a salt thereof or hydrate of the foregoing, and a cyclodextrin; or in further combination with an excipient comprising L-Arginine or other additives, wherein the compositions or formulations increases water solubility and oral bioavailability of 5-[3-(4-benzyloxyphenylthio)-fur-2-yl]-imidazolidin-2,4-dione and its related compounds. The method of making or using the compositions or formulations is also disclosed. Such compositions or formulations may be used in treatment of certain diseases including asthma through inhibition of matrix metalloproteinase-12.
Abstract: Pharmaceutical compositions for intraocular injection are described, the compositions comprise therapeutically effective quantity of lyophilized preservative-free and sulfite-free epinephrine or adrenaline and a metal chelator. Methods for fabricating the compositions and using them for intraocular injections are also described.
Abstract: The present invention discloses an application of clofoctol for manufacturing a pharmaceutical product for treating human neuroglioma. The clofoctol is a pharmaceutical product for treating an upper respiratory tract infection. The clofoctol exerts a significant and specific inhibition of a glioma stem cell activity relative to a human neuroglioma cell or a normal human astroglia, human embryonic kidney cell, and human neural stem cell. A glioma stem cell treated with the clofoctol exhibited significantly reduced self-renewal, tumorsphere formation, and in vivo tumor formation in a nude rat. In vivo experiments using a zebrafish glioma transplantation model and a nude rat glioma transplantation model provided in vivo verification for the therapeutic efficacy of the pharmaceutical product against glioma.
Type:
Grant
Filed:
March 20, 2017
Date of Patent:
April 27, 2021
Assignee:
Institute of Medical Sciences, Chinese Academy of Medical Sciences
Inventors:
Xiaozhong Peng, Yan Hu, Wei Han, Boqin Qiang
Abstract: The present invention relates to methods, compositions and kits for treatment of ribosomal disorders and ribosomopathies, e.g. Diamond Blackfan anemia (DBA). In some embodiments, the invention relates to the use of novel classes of compounds, i.e. inhibitors of RSK (p90S6K); inhibitors of p70S6K; and inhibitors of rps6, to treat ribosomal disorders and ribosomopathies. In some embodiments, the invention relates to the use of specific Chk2 inhibitors and to the use of specific phenothiazine derivatives to treat ribosomal disorders and ribosomopathies, e.g. DBA.
Type:
Grant
Filed:
July 13, 2017
Date of Patent:
April 20, 2021
Assignees:
The Children's Medical Center Corporation, Dana-Farber Cancer Institute, Inc.
Inventors:
James Bradner, Jun Qi, Dennis Buckley, Leonard I. Zon, Elizabeth Macari
Abstract: Compounds, pharmaceutical compositions, and methods for reversing fosfomycin resistance are disclosed. Embodiments of the disclosed compounds inhibit fosfomycin-inhibiting enzymes. Some embodiments of the compounds are FosA inhibitors. The disclosed pharmaceutical compositions include (i) fosfomycin or a pharmaceutically acceptable salt thereof and (ii) a compound, or a pharmaceutically acceptable salt thereof, which inhibits a fosfomycin-inhibiting enzyme. A method of inhibiting growth of a fosfomycin-resistant bacterium includes contacting the bacterium with (i) fosfomycin or a pharmaceutically acceptable salt thereof and (ii) an effective amount of a disclosed compound or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 11, 2018
Date of Patent:
April 20, 2021
Assignees:
University of Pittsburgh—of the Commonwealth System of Higher Education, University of Maryland, Baltimore
Inventors:
Nicolas Paul Sluis-Cremer, Adam Daniel Tomich, Yohei Doi, Eric J. Sundberg, Erik H. Klontz, Steven Fletcher
Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
Abstract: To provide an inhibitor of melanin decomposition, which inhibits decomposition of melanin in keratinocytes to accelerate accumulation of melanin in skin and hair. An inhibitor of melanin decomposition in keratinocytes, comprising at least one selected from the group consisting of a plant extract containing berberine or a salt thereof, berberine or a salt thereof, proguanil or a salt thereof and phenformin or a salt thereof, as an active ingredient.
Abstract: A solid pharmaceutical composition comprising a solid dispersion of a BCS Class II drug in a solid carrier/hydrophilic carrier; and a pH modifier. The solid carrier/hydrophilic carrier has a melting point of between about 40° C. to about 60° C. and an HLB value of between about 10 and about 18. The BCS Class II drug may be telmisartan.
Abstract: This application relates to various crystalline forms of 5-bromo-2,6-di(1H-pyrazol-1-yl)pyrimidin-4-amine and salt thereof, as well as compositions and methods of using the same. In some embodiments the crystalline forms also contain water (“hydrates”). These materials are useful in the treatment of various diseases, including carcinomas, specifically lung cancer and more specifically non-small cell lung cancer.
Type:
Grant
Filed:
May 30, 2018
Date of Patent:
March 2, 2021
Assignees:
Novartis AG, Palobiofarma S.L.
Inventors:
Kai Cui, Julio Cesar Castro-Palomino Laria, Weiyong Kong