Abstract: Provided are methods for treating pancreatic cancer in a patient by administering liposomal irinotecan (MM-398) alone or in combination with additional therapeutic agents. In one embodiment, the liposomal irinotecan (MM-398) is co-administered with 5-fluorouracil and leucovorin.
Type:
Grant
Filed:
June 19, 2018
Date of Patent:
June 28, 2022
Inventors:
Eliel Bayever, Navreet Dhindsa, Jonathan Basil Fitzgerald, Peter Laivins, Victor Moyo, Clet Niyikiza, Jaeyeon Kim
Abstract: The present invention relates to cyano-substituted-heterocycles of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having utility in a variety of therapeutic areas including cancer and conditions involving mitochondrial dysfunction.
Type:
Grant
Filed:
October 4, 2017
Date of Patent:
June 28, 2022
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Martin Lee Stockley, Mark Ian Kemp, Andrew Madin
Abstract: Embodiments of prodrugs of PKC modulators that show efficacy coupled with low levels of toxicity and improved stability are provided. The prodrug compounds are useful in academic research (animal studies), as candidates for preclinical research, and as therapeutic agents. By taking advantage of a pharmacophore-based strategy, this design strategy provides access to prodrugs of PKC modulators of diverse scaffolds including tigliane diterpenes, ingenane diterpenes, daphnane diterpene orthoesters, diacylglycerols, and bryostatins, and analogs thereof. In particular, embodiments of the prodrug ingenane esters having substitutions at C20 and their use as therapeutic agents are provided.
Type:
Grant
Filed:
May 10, 2018
Date of Patent:
June 28, 2022
Assignee:
THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY
Inventors:
Paul A. Wender, Katherine N. Keenan, Nancy Lynn Benner, Jack Leider Sloane, Xiaoyu Zang
Abstract: The present invention relates to pyrazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle stimulating hormone receptor (FSHR).
Type:
Grant
Filed:
August 22, 2018
Date of Patent:
June 21, 2022
Assignee:
Merck Patent GmbH
Inventors:
Henry Yu, Marianne Donnelly, Ngan Nguyen, Xuliang Jiang
Abstract: Deuterated domperidone compositions, methods of synthesis, methods of use, and dosing formulations providing beneficial safety and other effects.
Type:
Grant
Filed:
June 28, 2018
Date of Patent:
June 21, 2022
Assignee:
CinRx Pharma, LLC
Inventors:
Catherine Pearce, Jon Isaacsohn, Piyush Patel
Abstract: The present invention provides a 2-aminoquinazolinone derivative. The present invention is a compound represented by formula (1) [wherein X1 represents CR or N, X2 represents CR2 or N, X3 represents CR3 or N, Y represents an optionally substituted C6-10 aryl or optionally substituted 6 to 10-membered heteroaryl, Z represents an optionally substituted C6-10 aryl, RA represents a hydrogen atom, halogen, cyano, optionally substituted C1-6 alkyl sulfonyl, optionally substituted C1-6 alkyl, or optionally substituted C1-6 alkoxy, and R1, R2, and R3 independently represent a hydrogen atom, halogen, optionally substituted C1-6 alkyl, or optionally substituted C1-6 alkoxy] or a pharmaceutically acceptable salt thereof.
Abstract: 2-Aminopyrimidine-substituted 2H-indazole compounds of formula (I), where R1 is hydrogen, and their prodrugs, where R1 is a metabolizable group under physiological conditions, as cyclin-dependent kinase (CDK) and cell-proliferation inhibitors, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, solvates, prodrugs, and pharmaceutical compositions thereof, are useful for treating diseases and disorders associated with activity of cyclin-dependent kinases, in particular CDK4/6, including but not limited to various cancers and inflammation-related diseases or conditions.
Type:
Grant
Filed:
January 29, 2019
Date of Patent:
June 7, 2022
Assignee:
BETA PHARMA, INC.
Inventors:
Michael Nicholas Greco, Michael John Costanzo, Jirong Peng, Don Zhang
Abstract: Provided are a novel pseudoceramide compound and a skin external composition comprising the same. The skin external composition comprising a pseudoceramide compound or a pharmaceutically acceptable salt or solvate thereof according to the present invention as an active ingredient has an excellent effect of improving a skin barrier function, thereby exhibiting an effect of improving inflammatory skin diseases, and also is excellent in the function of improving the skin barrier and the effect of enhancing skin moisture.
Abstract: The present invention provides a composition having an antifungal activity without depending on conventional compositions having anticandidal activity or combinations of such compositions. The composition comprises a complex of lysozyme bonded to chitosan. The composition according to the present invention is applicable to candidiasis of the skin and mucous membranes, in particular, oral candidiasis and vagina candidiasis affecting a large number of patients and can ameliorate the symptoms of these diseases, heal the same and prevent infection of the same. The composition comprises a complex of lysozyme, which has been widely used as a highly safe natural food additive, with a polysaccharide and, therefore, can reassure patients who use the same and ease their burden. The composition according to the present invention comprises a complex of lysozyme, which is a highly safe natural food additive, with a polysaccharide and, therefore, can be safely used by patients without considering any risk.
Type:
Grant
Filed:
July 9, 2020
Date of Patent:
May 31, 2022
Assignees:
Wako Filter Technology Co., Ltd., Teikyo University
Abstract: The present invention relates to compounds of general formula (II), to compositions comprising these compounds and to methods of treating Enterobacteriaceae bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Enterobacteriaceae.
Type:
Grant
Filed:
November 2, 2018
Date of Patent:
May 31, 2022
Assignee:
Discuva Ltd.
Inventors:
Paul Meo, Mohammed Nawaz Khan, Cedric Charrier
Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts and esters thereof: which inhibit the Apoptosis signal-regulating kinase 1 (ASK-1), which associated with autoimmune disorders, neurodegenerative disorders, inflammatory diseases, chronic kidney disease, cardiovascular disease. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from ASK-1 related disease. The invention also relates to methods of treating an ASK-1 related disease in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention specifically relates to methods of treating ASK-1 associated with hepatic steatosis, including non-alcoholic fatty liver disease (NAFLD) and non-alcohol steatohepatitis disease (NASH).
Type:
Grant
Filed:
November 19, 2019
Date of Patent:
May 31, 2022
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Brett Granger, Guoqiang Wang, Ruichao Shen, Jing He, Yong He, Xuechao Xing, Jun Ma, Jiang Long, Bin Wang, Yat Sun Or
Abstract: Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Type:
Grant
Filed:
June 4, 2021
Date of Patent:
May 31, 2022
Assignee:
KINNATE BIOPHARMA INC.
Inventors:
Stephen W. Kaldor, John Tyhonas, Eric A. Murphy, Toufike Kanouni, Lee D. Arnold, Robert Kania, Jason M. Cox
Abstract: The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.
Type:
Grant
Filed:
November 19, 2019
Date of Patent:
May 31, 2022
Assignee:
Valo Health, Inc.
Inventors:
Jennifer Lee, Nicholas Barczak, Jaime A. Escobedo, Chiara Conti, Bingsong Han, David R. Lancia, Jr., Cuixian Liu, Matthew W. Martin, Pui Yee Ng, Aleksandra Rudnitskaya, Jennifer R. Thomason, Xiaozhang Zheng
Abstract: Novel compounds of Formula I are described, where the compounds are selective HDAC6 inhibitors suitable for treatment of diseases associated with HDAC6, where X, Y, Z, A1, A2, Q1 and Q2 are as described.
Type:
Grant
Filed:
December 23, 2020
Date of Patent:
May 24, 2022
Assignee:
OnKure, Inc.
Inventors:
Anthony D. Piscopio, Gan Zhang, Kevin Hunt
Abstract: There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
Type:
Grant
Filed:
August 25, 2017
Date of Patent:
May 24, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Emily Charlotte Cherney, Weifang Shan, Liping Zhang, Susheel Jethanand Nara, Audris Huang, James Aaron Balog
Abstract: The object of the present invention is to find a new application of isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate or a salt thereof. Isopropyl (6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl) aminometh yl}pyridin-2-ylamino) acetate or a salt thereof is useful as a therapeutic agent for a disease involving a greatly elevated intraocular pressure.
Type:
Grant
Filed:
March 11, 2020
Date of Patent:
May 17, 2022
Assignee:
SANTEN PHARMACEUTICAL CO., LTD.
Inventors:
Tomoko Kirihara, Atsushi Shimazaki, Najam A. Sharif
Abstract: A probiotic formulation is provided including one or more bacteria, bacterial strains or bacterial species of the genus Veillonella, genus Faecalibacterium, genus Phascolarctobacteria, genus Oscillospira, genus Ruminococcus, genus Bacteroides, genus Blautia, family Christensenellaceae, genus Dialister, or phylum cyanobacteria.
Type:
Grant
Filed:
August 6, 2021
Date of Patent:
May 10, 2022
Assignee:
President and Fellows of Harvard College