Abstract: The present invention relates to the compound of formula (1a) wherein p is 1 or 2, R1-R4 are hydrogen atom or the like, and a-d are 1 or 2, or a pharmaceutically acceptable salt thereof, which has an antitumor effect by inhibiting the binding between a MLL fusion protein that is infused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.
Abstract: Disclosed herein are compositions comprising an NSAID such as meloxicam and/or rizatriptan in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability or pharmacokinetics of the NSAID for the treatment of pain such as migraine, arthritis, and other conditions. Also disclosed herein are methods of treating pain, such as migraine, comprising administering meloxicam and rizatriptan to a human being suffering from pain, such as migraine. For migraine, these methods may be particularly useful when the meloxicam and rizatriptan are administered while the human being is suffering from an acute attack of migraine pain or migraine aura. In some embodiments, the combination of meloxicam and rizatriptan may be administered in a manner that results in a Tmax of meloxicam of 3 hours or less.
Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising a JAK inhibitor. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having, suspected of having, or at risk of developing Graft-Versus-Host Disease.
Type:
Grant
Filed:
April 11, 2019
Date of Patent:
June 28, 2022
Assignee:
Incyte Corporation
Inventors:
Michael D. Howell, Hao Liu, Michael A. Pratta
Abstract: The present invention relates generally to the use of gene mutations, whose presence or absence are useful for predicting a patient's response to treatment with an anti-proliferative agent, in particular a WEE1 inhibitor. The presence or absence of a mutation to the TP53 gene, can be used to predict response to treatment with a WEE1 inhibitor in a patient presenting with a cancerous condition.
Abstract: The invention relates generally crystalline mesylate salts, crystalline chloride salts and crystalline sulfate salts of the compound (S)-2-(3?-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4?-bipyridin]-2?-yl)-7,7-dimethyl-2,3,4,6,7,8-hexahydro-1H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one that is an inhibitor of Bruton's tyrosine kinase. In some aspects, the crystalline salts are single polymorphs.
Abstract: The present invention relates to an anticancer and metastasis inhibiting effect by treatment with chlorphenesin, chloroquine, and chloropyrazine alone or in combination. Chlorphenesin, chloroquine, or chloropyrazine show the effect of killing cancer cells and inhibiting proliferation, and metastasis of cancer cells and particularly, a combination thereof is identified to have synergism. Cancer can be effectively prevented or treated by administering chlorphenesin, chloroquine, and chloropyrazine alone or in combination thereof.
Abstract: The present invention relates to use of a composition comprising D-glyceric acid (DGA), DL-glyceric acid, L-glyceric acid, or hydroxypyruvatic acid and/or their salts or esters. Further, the invention relates to the use of said composition for enhancing direct and indirect mitochondrial metabolism, e.g. the ATP producing electron transport system (ETS), citric acid cycle or tricarboxylic acid cycle, (TCA), and beta oxidation, and also enhancing the shuttling of reducing equivalents from mitochondrial matrix into the cytosol and protein synthesis in the endoplasmic reticulum. Directly related to the above the use of DGA relates also to reducing the formation of reactive oxygen species (ROS). Alleviating, preventing and even healing effects towards extremely wide range of non-communicable diseases materializes.
Type:
Grant
Filed:
October 23, 2019
Date of Patent:
June 14, 2022
Assignee:
REPLICON HEALTH OY
Inventors:
Petteri Hirvonen, Peter Eriksson, Risto Kaksonen
Abstract: It has been found by the present inventors that agents that boost the expression of the opioid receptor kappa 1 (OPRK1) can enhance the cytotoxicity of chemotherapeutic agents in multiple cancer cell lines. Furthermore, the effect is dose dependent, where the greater the induced expression of OPRK1, the greater the cytotoxicity of the chemotherapeutic agent. The increase in overall cytotoxicity is independent of the cytotoxicity of the agent that increases the expression of OPRK1, which itself has no or minimal cytotoxic effect.
Abstract: The present invention relates to compounds, to compositions comprising the same, to methods for preparing the compounds, and the use of these compounds in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.
Type:
Grant
Filed:
March 11, 2020
Date of Patent:
May 31, 2022
Assignees:
QUANTUM GENOMICS, INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, COLLEGE DE FRANCE
Abstract: The invention provides methods for modulating the activity of farnesoid X receptors (FXRs) using specific FXR agonists, in particular for treating or preventing liver diseases.
Type:
Grant
Filed:
February 20, 2017
Date of Patent:
May 31, 2022
Assignee:
Novartis AG
Inventors:
Bryan Laffitte, Michael Badman, Jin Chen, Sam Lindgren
Abstract: This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation.
Abstract: This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation.
Abstract: The present invention relates to methods of treating patients with advanced forms of cancer, such as unresectable or metastatic renal cell carcinoma or kidney cancer, in which X4P-001 or a pharmaceutically acceptable salt thereof is administered as monotherapy or in combination with an immune checkpoint inhibitor, such as nivolumab. The methods demonstrate surprising results, including regression of disease, with comparatively little toxicity.
Abstract: This disclosure relates to dosage forms containing an enantiomerically enriched or pure bupropion such as enantiomeric excess of (S)-bupropion, enantiomerically enriched (S)-bupropion, or enantiomerically pure (S)-bupropion and methods of using these dosage forms. These dosage forms may be administered to human beings in a reduced amount as compared to the amount of racemic bupropion that would be administered in the same situation.
Abstract: Pharmaceutical compositions of the invention comprise functionalized N,N-dialkylamino phenyl ethers derivatives having a disease-modifying action in the treatment of diseases associated with lysosomal storage dysfunction that include Gaucher's disease, and any disease or condition involving lysosomal storage dysfunction.
Type:
Grant
Filed:
November 20, 2018
Date of Patent:
May 10, 2022
Assignee:
Temple University—Of The Commonwealth System of Higher Education
Inventors:
Edward G. Melenski, Wayne E. Childers, Marlene A. Jacobson, Magid A. Abou-Gharbia
Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
September 20, 2021
Date of Patent:
May 10, 2022
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Ruichao Shen, Yong He, Xuechao Xing, Matthew C. Rhodes, Guoqiang Wang, Yat Sun Or
Abstract: Methods of treating tumors by administering compounds to a patient are provided. Compounds such as pro drugs, e.g., 5-aminolevulinic acid (5-ALA), may be administered to the patient orally, by injection, intravenously, or topically, which then accumulate preferentially as compounds such as protoporphyrin IX (PpIX) in tumor cells. After such accumulation, compounds such as PpIX are then activated in various aspects to treat tumors cells, thereby treating cancer. Cancers such as glioblastoma may be treated.
Type:
Grant
Filed:
August 11, 2021
Date of Patent:
May 3, 2022
Assignee:
Alpheus Medical, Inc.
Inventors:
Vijay Agarwal, Braden Eliason, Jeremy Ling
Abstract: Compositions for inhibiting the aggregation of a granin from a non-toxic low molecular weight form to a toxic high molecular weight aggregated form and/or dissociating a high molecular weight aggregated form to a low molecular weight form are provided. Such a composition typically includes one or more active compounds or agents, which may also be referred to herein as disaggregation compounds. Using the compounds and compositions described herein, methods of i) modulating, inhibiting or preventing the interaction of granins with metal ions, ii) modulating, inhibiting, preventing the aggregation of granins or dissociating aggregated granins, iii) reducing or inhibiting cell toxicity, iv) treating or preventing dementia or Alzheimer's disease, and v) preventing or treating Parkinson's and/or Huntington's diseases are also provided.
Abstract: Provided herein are methods of treating basal cell carcinoma or glioblastoma by administering coal tar or a coal tar product to a patient with basal cell carcinoma or glioblastoma. The coal tar or coal tar product may be administered as a standalone therapy or in combination with other treatments for basal cell carcinoma or glioblastoma.