Abstract: The present invention relates to 5-amino-3-phenylamino-6-phenylpyrazolo[3,4-d]pyrimidine derivatives of the general formula (I) or pharmaceutically acceptable salts or propharmacons thereof for use as BCRP inhibitors, wherein at least one hydrogen atom in at least one of the phenyl groups A and B is substituted by a substituent RH, which has a Hammett constant ?p greater than 0.23. For corresponding compounds, surprisingly a particularly high inhibitory activity against BCRP has been discovered which can be exploited for suppressing the multidrug resistance modulator BCRP, thus providing an improvement in efficacy of BCRP affected drugs. This has useful implications for cancer and HIV treatment.
Abstract: Methods are provided for the treatment of relapsed and/or refractory solid tumors (including neuroendocrine carcinomas (NEC)) and non-Hodgkin's lymphomas (NHLs) and the like, using substituted heterocyclic derivative compounds and pharmaceutical compositions comprising compounds useful for the inhibition of lysine specific demethylase-1 (LSD-1).
Abstract: The invention provides a metabolism improving agent containing a rare fatty acid such as hydroxylated fatty acid, oxo fatty acid and the like, and further, food, pharmaceutical product and the like containing the metabolism improving agent.
Abstract: Imipridones selectively modulate Class A G protein-coupled receptors (GPCRs), such as the D2-like subfamily of dopamine receptors, and are useful for treating conditions and disorders in need of such modulation, such as cancers. Specifically, the cancer is a midline glioma, a cancer having a histone H3 mutation, or both. In addition, methods of identifying whether a subject having these conditions, is likely to be responsive to a treatment regimen, such as imipridone administration, are provided. Furthermore, methods of assessing the effectiveness of a treatment regimen, such as imipridone administration, monitoring, or providing a prognosis for a subject with these condition are also provided.
Type:
Grant
Filed:
July 30, 2019
Date of Patent:
March 16, 2021
Assignee:
ONCOCEUTICS, INC.
Inventors:
Joshua E. Allen, Martin Stogniew, Varun Vijay Prabhu
Abstract: An ophthalmic composition is provided that includes rebamipide and a method for preparing the same. The ophthalmic composition of maintains its transparency for a long time even in a physiologically neutral to weakly basic pH range that does not injure the cornea and conjunctiva of a patient suffering from dry eye and has improved stability so as not to be re-dispersed.
Type:
Grant
Filed:
September 30, 2016
Date of Patent:
February 16, 2021
Assignee:
SAMJIN PHARMACEUTICAL CO., LTD.
Inventors:
Eui-Hwan Cho, Sung-Ju Choi, Sung-Woo Lee, Hee-Jong Shin, Min-Hyo Ki, Mee-Hwa Choi, Dong-Ha Lee
Abstract: The present disclosure is directed to compositions comprising oxymetazoline and methods of stabilizing oxymetazoline compositions for long term storage.
Abstract: Disclosed herein are methods for treating solid tumors by direct injection into the tumors of chemotherapeutic particles, methods for inhibiting tumor metastasis by administering chemotherapeutic particles to a subject having a tumor, and compositions that include chemotherapeutic particles, small amounts of a polysorbate, and a carrier.
Type:
Grant
Filed:
December 13, 2019
Date of Patent:
January 19, 2021
Assignee:
Crititech, Inc.
Inventors:
Mike Baltezor, Gere diZerega, Charles Decedue, Sam Campbell, Matt McClorey
Abstract: Embodiments of the present invention are directed to methods and articles of manufacture to treat skin to improve and/or increase hydration, pliability, and thickness for improved texture, feel and appearance. Embodiments feature applying an effective amount of an acetylation agent to natural dermal collagen under reaction conditions to react the natural dermal collagen with the acetylation agent to form a modified collagen. The modified collagen has a higher net charge and higher net charge density than natural dermal collagen. The modified collagen improves or increases one or more skin characteristics consisting of hydration, pliability and thickness.
Abstract: The invention provides compositions and methods for the induction of cell death, for example, cancer cell death. Combinations of compounds and related methods of use are disclosed, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells. The disclosed drug combinations can have lower neurotoxicity effects than other compounds and combinations of compounds.
Type:
Grant
Filed:
October 1, 2018
Date of Patent:
January 12, 2021
Assignees:
The Board of Trustees of the University of Illinois, Vanquish Oncology, Inc.
Inventors:
Paul J. Hergenrother, Rachel C. Botham, Timothy M. Fan, Mark J. Gilbert, Michael K. Handley, Howard S. Roth, Theodore M. Tarasow
Abstract: Disclosed herein are methods for treating solid tumors by direct injection into the tumors of chemotherapeutic particles, methods for inhibiting tumor metastasis by administering chemotherapeutic particles to a subject having a tumor, and compositions that include chemotherapeutic particles, small amounts of a polysorbate, and a carrier.
Type:
Grant
Filed:
December 13, 2019
Date of Patent:
December 29, 2020
Assignee:
CritlTech, Inc.
Inventors:
Mike Baltezor, Gere diZerega, Charles Decedue, Sam Campbell, Matt McClorey
Abstract: An antibacterial compound of formula I, wherein X is selected from fluoro or bromo, effective against Gram negative and Gram positive bacteria, and in particular against non-fermenting multiresistant bacteria affecting patients suffering from cystic fibrosis and which are responsible of severe hospital-acquired infections in immunodepressed patients; its preparation process and pharmaceutical composition comprising said compound.
Type:
Grant
Filed:
August 9, 2017
Date of Patent:
December 8, 2020
Assignees:
CONSEJO NACIONAL DE INVESTIGACIONES CIENTIFICAS Y TECNICAS (CONICENT), UNIVERSIDAD NACIONAL DE LA PLATA (UNLP), QUAID-I-AZAM UNIVERSITY
Abstract: Provided are methods of administering a vesicular monoamine transport 2 (VMAT2) inhibitor chosen from valbenazine and (+)-?-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol, or a pharmaceutically acceptable salt and/or isotopic variant thereof, to a patient in need thereof wherein the patient is also being administered digoxin.
Type:
Grant
Filed:
May 11, 2020
Date of Patent:
December 8, 2020
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Christopher F. O'Brien, Haig P. Bozigian
Abstract: Methods are provided for the treatment of relapsed and/or refractory solid tumors (including neuroendocrine carcinomas (NEC)) and non-Hodgkin's lymphomas (NHLs) and the like, using substituted heterocyclic derivative compounds and pharmaceutical compositions comprising compounds useful for the inhibition of lysine specific demethylase-1 (LSD-1).
Abstract: A nutraceutical composition comprising fullerene (e.g., C60), curcumin, and a medium chain triglyceride. Preferably, blackseed oil is used to provide medium chain triglyceride. The nutraceutical composition can be packaged in a mist-producing device and used as a nasal spray or an inhaler. Preferably, the nasal spray is substantially free of particles having a size greater than 0.2 ?m. The nutraceutical composition can be used to treat respiratory conditions (e.g., asthma, nasal polyps, etc.) or brain disorders through nasal spray, inhaling, or oral administration.
Abstract: Methods of treating a mental condition by administering to a subject in need thereof an effective amount of compound CDD-102A, [5-(3-ethyl-1,2,4-oxadiazol-5-yl)-1,4,5,6-tetrahydropyrimidine] are described.
Type:
Grant
Filed:
October 17, 2013
Date of Patent:
November 17, 2020
Assignees:
The University of Toledo, The Board of Trustees of the University of Illinois
Inventors:
William S. Messer, Jr., Michael E. Ragozzino
Abstract: Disclosed herein are therapeutic regimens for improving visual function in Retinitis Pigmentosa and other visual disorders associated with an endogenous retinoid deficiency in a subject by administering a therapeutically effective amount of a synthetic retinal derivative, for example a 9- or 11-cis retinyl ester, according to the therapeutic regimen which leads to local recovery of visual functions such as visual fields, visual acuity and retinal sensitivity, among others.
Abstract: The present invention relates to a pharmaceutical composition for preventing or treating AIDS, comprising a rhodanine derivative and a nucleoside reverse transcriptase inhibitor. A complex composition of the present invention exhibits a synergistic effect in terms of anti-HIV activity as compared with a case where each of the compounds is used as a single drug. Thus, the composition provides sufficient anti-HIV activity and exhibits an excellent effect of decreasing side effects such as toxicity even in a case where each compound is administered in a small amount. Accordingly, the present invention is expected to greatly contribute to treatment of AIDS patients.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
November 3, 2020
Assignee:
AVIXGEN INC.
Inventors:
Min Jung Kim, Jun Sub Choi, Hye Cheong Koo, Yi Yong Baek