Abstract: Provided herein are compositions and methods for treating pulmonary arterial hypertension. In particular, provided herein are dry powder formulations of TMP for delivery to the lung.
Type:
Grant
Filed:
October 25, 2018
Date of Patent:
June 6, 2023
Assignee:
Arizona Board of Regents on Behalf of the University of Arizona
Inventors:
Heidi M. Mansour, Jason Yuan, Jian Wang, Alexan I. Gomez, Priyardarshini Muralidharan, Yali Gu
Abstract: Disclosed in the present invention is a new triptolide derivative as shown in formula (I). Also disclosed in the present invention are a preparation method for the compound and the medical use thereof in preparation of anti-cancer drugs. Triptolide acrylate of the present invention and a pharmaceutically acceptable salt thereof have anti-cancer activity, and after animal in-vivo experiments, can effectively inhibit tumor growth in animals. A plurality of in-vitro experiments proves that same can significantly increase the protein expression quantity of p53, promote the apoptosis of tumor cells, effectively inhibit the growth of the tumor cells, and have the effect of inhibiting metastasis of cancer cells. More importantly, the toxicity of the compound to normal cells is less than that of triptolide.
Type:
Grant
Filed:
December 30, 2019
Date of Patent:
May 30, 2023
Assignees:
Guangdong Provincial Hospital of TCM, The Second Affiliated Hospital Of Guangzhou University of Chinese Medicine, The Second Clinical College Of Guangzhou University of Chinese Medicine, Guangdong Provincial Academy Of Chinese Medical Sciences
Inventors:
Bo Liu, Xianzhang Huang, Zhimin Yang, Jun Li, Quanfu Chen, Liqiao Han, Hualun Liang, Yiqi Yang, Kai Wang, Xiaowan Wang, Ennian Li, Yi Wang, Runyue Huang, Yunshan Wu, Xiaodong Han, Jinlang Zhong, Bidan Zheng
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:
January 25, 2021
Date of Patent:
May 23, 2023
Assignees:
Novartis AG, Palobiofarma S.L.
Inventors:
Kai Cui, Julio Cesar Castro-Palomino Laria, Weiyong Kong
Abstract: In certain embodiments, this disclosure relates to KRAS agonists, pharmaceutical composition, and uses in managing cancer. In certain embodiments, the KRAS agonist is 4-(4-(2-bromoacetamido)butyl)benzoic acid, salt, prodrug, or derivative thereof. In certain embodiments, this disclosure relates to methods of treating cancer comprising administering an effective amount of a compound of Formula I, salt, prodrug, or derivative thereof, to a subject in need thereof, wherein, substituents are reported herein.
Abstract: A medicament comprising (I) brexpiprazole or a pharmaceutically acceptable salt thereof, and (II) nalmefene or a pharmaceutically acceptable salt thereof in combination, wherein brexpiprazole or a pharmaceutically acceptable salt thereof, and nalmefene or a pharmaceutically acceptable salt thereof are contained in a single preparation, or a pharmaceutical composition containing brexpiprazole or a pharmaceutically acceptable salt thereof and a pharmaceutical composition containing nalmefene or a pharmaceutically acceptable salt thereof are formulated for use in combination. The medicament is used for the prophylaxis or treatment of a substance-related disorder, preferably an alcohol-related disorder.
Type:
Grant
Filed:
August 13, 2020
Date of Patent:
May 9, 2023
Assignees:
Otsuka Pharmaceutical Co., Ltd., H. Lundbeck A/S
Abstract: Provided herein are methods of treating cancer in a subject, wherein the cancer is extrachromosomal DNA-positive (ecDNA-positive) or therapeutically resistant, the method comprising administering to the subject a therapeutically effective amount of a replication stress (RS) pathway agent alone or in combination with a targeted therapeutic.
Type:
Grant
Filed:
October 21, 2022
Date of Patent:
May 9, 2023
Assignee:
BOUNDLESS BIO, INC.
Inventors:
Christian Hassig, Ryan Hansen, Snezana Milutinovic, Jason Christiansen, Zachary Hornby, Sudhir Chowdhry, Anthony Celeste, Kristen Turner, Deepti Wilkinson
Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, progression, proliferation and metastasis in several cancer types.
Type:
Grant
Filed:
April 10, 2020
Date of Patent:
April 25, 2023
Assignee:
Boise State University
Inventors:
Cheryl Jorcyk, Don Warner, Matthew David King, Lisa Warner
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: The present application relates to an anti-tumor compound and a preparation method and use thereof, and in particular to a compound or a tautomer, a mesomer, a racemate, an enantiomer or a diastereoisomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, and a preparation method and use thereof.
Abstract: In a method of treating a patient having low blood flow that may be caused by diffused plaque and/or a plaque mass associated with Peyronie's disease in a penile region, a predetermined amount of carbon dioxide is injected into affected corpus cavernosum at a location that is adjacent to, but spaced away from the plaque mass. In addition, either before and/or after the injection of the carbon dioxide, a decalcifying agent(s) may be injected directly into the plaque mass.
Abstract: The present invention relates to the cosmetic use of at least one compound of general formula (I): in which: R1 represents a methyl or ethyl radical; R2 represents a hydrogen atom or a methyl or ethyl radical; R3 represents a linear C1-C6 or branched C3-C6 alkyl radical, or a linear C2-C6 or branched C3-C6 alkenyl radical; and X represents ?O or —OH, as an agent for reducing and/or delaying the signs of skin ageing.
Abstract: The present invention provides a compound of formula (Ia) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, solid forms, combinations of pharmacologically active agents, pharmaceutical compositions and methods of using such compounds and solid forms thereof to treat or prevent parasitic diseases, for example malaria.
Type:
Grant
Filed:
October 21, 2020
Date of Patent:
March 7, 2023
Assignee:
Novartis AG
Inventors:
Nicole Alice Blaquiere, Richard Yichong Huang, Thomas Martin Kirrane, Jr., Andreas Kordikowski, Anne-Catherine Mata, Christopher Ronald Sarko, Benjamin Robert Taft, Grace Lamprecht Waldron, Fumiaki Yokokawa, Tingying Zhu
Abstract: The present invention is directed to compositions and methods of treating or preventing diseases or disorders with inhibitors of SHP2, alone, and in combination with other therapeutic agents such as RAS pathway inhibitors (e.g., MEK inhibitors); methods of establishing appropriate treatment plans for subjects based upon the expression of one or more biomarker indicative of SHP2 inhibitor sensitivity; and methods of determining sensitivity to a SHP2 inhibitor based on a phosphorylation status of SHP2.
Type:
Grant
Filed:
March 5, 2020
Date of Patent:
March 7, 2023
Assignee:
Revolution Medicines, Inc.
Inventors:
Robert J. Nichols, Mark A. Goldsmith, Christopher Schulze, Jacqueline Smith, David E. Wildes, Stephen Kelsey, Mallika Singh
Abstract: The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.
Abstract: In one aspect, the present disclosure provides analogs of thailanstatin of the formula wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein.
Type:
Grant
Filed:
June 8, 2017
Date of Patent:
February 21, 2023
Assignee:
William Marsh Rice University
Inventors:
Kyriacos C. Nicolaou, Derek Rhoades, Soundarapandian M. Kumar, Manas R. Pattanayak, Manjunath Lamani
Abstract: Provided herein are combination therapies comprising an ATP competitive AKT inhibitor, fulvestrant, and CDK4/6 inhibitor for use in treating hormone receptor positive and HER2 negative locally advanced unresectable or metastatic breast cancer.
Abstract: Provided herein are methods of treating cancer in a subject, wherein the cancer is extrachromosomal DNA-positive (ecDNA-positive) or therapeutically resistant, the method comprising administering to the subject a therapeutically effective amount of a replication stress (RS) pathway agent alone or in combination with a targeted therapeutic.
Type:
Grant
Filed:
January 4, 2022
Date of Patent:
January 10, 2023
Assignee:
BOUNDLESS BIO, INC.
Inventors:
Christian Hassig, Ryan Hansen, Snezana Milutinovic, Jason Christiansen, Zachary Hornby, Sudhir Chowdhry, Anthony Celeste, Kristen Turner, Deepti Wilkinson