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: 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: Described herein are methods of treating pyruvate kinase deficiency (PKD), sickle cell disease or thalassemia with mitapivat or a pharmaceutically acceptable salt thereof, or use of the drug for the treatment of these conditions, in combination with or in the absence of with a secondary drug, such as an inducer or an inhibitor of cytochrome P450. Various doses and dosing regimens of mitapivat in monotherapy and in concomitant medications are described.
Type:
Grant
Filed:
June 12, 2020
Date of Patent:
January 23, 2024
Assignee:
Agios Pharmaceuticals, Inc.
Inventors:
Varsha Venkatachalam Iyer, Chandra Agarwal Prakash, Hua Yang
Abstract: Bifunctional compounds, which find utility as modulators of non-receptor Leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
March 19, 2021
Date of Patent:
January 2, 2024
Assignee:
Arvinas Operations, Inc.
Inventors:
Erika Araujo, Michael Berlin, Steven M. Sparks, Jing Wang, Wei Zhang
Abstract: This disclosure relates to the field of formulations of SN-38 with a poly(amino acid) copolymer and methods of making and using thereof. Compositions herein are drug products suitable for the treatment of cancer.
Abstract: Among other aspects, provided herein is a mixed-acid salt of a water-soluble polymer-drug conjugate, along with related methods of making and using the same. The mixed-salt acid salt is stably formed, and appears to be more resistant to hydrolytic degradation than the corresponding predominantly pure acid salt or free base forms of the polymer-drug conjugate. The mixed acid salt is reproducibly prepared and recovered, and provides surprising advantages over non-mixed acid salt forms of the water-soluble polymer drug conjugate.
Type:
Grant
Filed:
October 2, 2020
Date of Patent:
December 5, 2023
Assignee:
Nektar Therapeutics
Inventors:
Antoni Kozlowski, Samuel P. McManus, Sachin Tipnis, Greg Lavaty, David Swallow, John R. Handley, Anthony G. Schaefer
Abstract: The present invention relates to novel compounds which are able to modulate b-raf kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
Abstract: This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.
Abstract: Disclosed are methods and compositions for treating cell proliferative diseases and disorders such as cancers. Particularly disclosed are methods and composition for treating cancers such as glioblastoma by administering a therapeutic agent that inhibits the biological activity of the autophagy related 4B cysteine peptidase (ATG4B) protein in conjunction with additional therapeutic agents or treatments.
Abstract: Disclosed herein is a method for the prevention, delay of progression or treatment of indolent or aggressive B-cell lymphomas in an individual in need thereof, comprising administering a Btk inhibitor (in particularly (S)-7-(1-actyloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo-[1,5-a]pyrimidine-3-carboxamide or a pharmaceutically acceptable salt thereof) in combination with an anti-PD-1 antibody. The potent and selective BTK inhibitor in combination with the anti-PD-1 antibody have a manageable toxicity profile in patients with indolent and aggressive lymphomas.
Type:
Grant
Filed:
November 29, 2018
Date of Patent:
October 17, 2023
Assignee:
BEIGENE SWITZERLAND GMBH
Inventors:
James Hilger, Xiaoping Zhang, Shibao Feng, Sunhee Ro, Jane Huang
Abstract: The disclosure provides a multi-arm multi-claw polyethylene glycol derivative suitable for click chemistry reactions of general formula I, wherein R is a polyethylene glycol residue having a linear-chain structure, a Y-type structure or a multi-branched structure, R1, R2 and R3 are linking groups, P is an terminal group of non-azido non-alkynyl group, D is —N3 or —C?CH, l is selected from an integer of 1 to 20, and m is selected from an integer of 0 to 19.
Abstract: A compound of formula (I) and its antitumor application are disclosed. The compounds of formula (I) have degradation and inhibitory effects on ALK target proteins. They are mainly composed of four parts: the first part, ALK-TKI, being compounds with ALK tyrosine kinase inhibitory activity; the second part, LIN, being different kinds of linker (Linker); the third part, the ULM, being a small molecule ligand (ULM, ubiquitin ligase binding moiety) with ubiquitination of VHL, CRBN or other proteases; and the fourth part, the group A, being a carbonyl group or absent, which covalently bond ALK-TKI to LIN, wherein LIN and ULM are covalently bonded. A series of compounds designed and synthesized by the present disclosure have wide pharmacological activities, have functions of degrading ALK protein and inhibiting ALK activity, and can be used for related tumor treatment.
Type:
Grant
Filed:
June 15, 2020
Date of Patent:
October 3, 2023
Assignee:
ShanghaiTech University
Inventors:
Xiaobao Yang, Biao Jiang, Xiaoling Song, Haifan Lin, Ning Sun, Jinju Chen, Xing Qiu, Chaowei Ren, Ying Kong
Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Type:
Grant
Filed:
June 30, 2021
Date of Patent:
September 26, 2023
Assignee:
Amgen Inc.
Inventors:
John Gordon Allen, Jennifer Rebecca Allen, Ana Elena Minatti, Qiufen Xue, Ryan Paul Wurz, Christopher M. Tegley, Alexander J. Pickrell, Thomas T. Nguyen, Vu Van Ma, Patricia Lopez, Longbin Liu, David John Kopecky, Michael J. Frohn, Ning Chen, Jian Jeffrey Chen, Aaron C. Siegmund, Albert Amegadzie, Nuria A. Tamayo, Shon Booker, Clifford Goodman, Mary Walton, Nobuko Nishimura, Youngsook Shin, Jonathan D. Low, Victor J. Cee, Anthony B. Reed, Hui-Ling Wang, Brian Alan Lanman
Abstract: A powdered pre-operative beverage composition has one or more carbohydrates and L-citrulline. The composition can further have a CNS stimulant, a sweetener, citric acid, L-theanine, zinc sulfate, sodium selenite, Vitamin A, and at least one flavor enhancing agent. The composition remains clear when mixed with water. The composition, when mixed with water has an osmolarity of about 265 milliosmole to about 300 milliosmole and a pH about 3.7 to about 4.5. A total energy available from the one or more carbohydrates in one serving of the composition is at least about 200 calories.
Abstract: The invention relates generally to the treatment of multiple myeloma. One embodiment of the invention provides a method of treating multiple myeloma (MM) in an individual, the method comprising: administering to the individual an effective amount of trichostatin A (TSA).
Type:
Grant
Filed:
August 26, 2019
Date of Patent:
August 29, 2023
Assignee:
VANDA PHARMACEUTICALS INC.
Inventors:
Mihael H. Polymeropoulos, Louis William Licamele, Christian Lavedan
Abstract: This disclosure generally relates to methods for reducing the risk of preterm birth in a pregnant human female patient that include subcutaneous administration of HPC. The disclosure relates in part to the discovery that subcutaneous administration of HPC is actually feasible and can result in sufficient plasma levels of HPC in pregnant patients that can reduce the risk of preterm birth.
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: The disclosure provides for prodrugs of Fingolimod that were designed to specifically prevent phosphorylation during circulation, hence avoiding bradycardia and lymphopenia. The disclosure further provides for the use of the prodrugs in the treatment of cancer and multiple sclerosis in subjects in need of treatment thereof.
Type:
Grant
Filed:
January 9, 2021
Date of Patent:
July 11, 2023
Assignee:
The Regents of the University of California
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.