Abstract: The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
Type:
Grant
Filed:
July 28, 2021
Date of Patent:
January 2, 2024
Assignee:
JAZZ PHARMACEUTICALS IRELAND LIMITED
Inventors:
Andrew Belfield, Clifford David Jones, Jean-François Margathe, Chiara Colletto
Abstract: The invention provides a novel class of therapeutics that are safe and effective inhibitors of Janus kinase 1 and pharmaceutical composition and methods of preparation and use thereof in the treatment of various diseases and disorders (e.g., inflammatory diseases, immune-mediated diseases or cancer).
Abstract: Iridium, rhodium, and platinum complexes suitable for use as phosphorescent emitters or as delayed fluorescent and phosphorescent emitters having the following structures:
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
December 26, 2023
Assignee:
Arizona Board of Regents on behalf of Arizona State University
Abstract: This invention relates to novel opioid derivatives of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R3, R4 and Z are as defined herein in the disclosure. The invention also relates to the use of such compounds for the treatment or prevention of, for example, pain.
Type:
Grant
Filed:
February 22, 2019
Date of Patent:
December 19, 2023
Assignee:
RHODES TECHNOLOGIES
Inventors:
Ping Chang, Raymond Glowaky, Michael David Rogers
Abstract: The invention provides compounds of formula (I): or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases and release an active metabolite in vivo. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory skin diseases and other diseases.
Type:
Grant
Filed:
September 27, 2021
Date of Patent:
December 19, 2023
Assignee:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Philip A. Gerken, Jianhua Chao, Daniel D. Long
Abstract: The present invention is directed to bicyclic pyridine N-oxide derivatives, stereoisomers, isotopologues, isotopomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing said compounds and the use of said compounds in the treatment and/or prophylaxis of thromboembolic disorders, inflammatory disorders and diseases or conditions in which plasma kallikrein activity is implicated.
Type:
Grant
Filed:
March 17, 2022
Date of Patent:
December 19, 2023
Assignee:
Janssen Pharmaceutica NV
Inventors:
Guozhang Xu, Zhijie Liu, Micheal D. Gaul
Abstract: The present disclosure discloses a quinoline-2,3-fused nine-membered ring scaffold compound, and a preparation method and application thereof as an effective component in a plant fungicide. The quinoline-2,3-fused nine-membered ring scaffold compound stated in the present disclosure is prepared by the following method including steps: mixing a quinoline-derived aniline compound and a formaldehyde compound, adding a solvent and a catalyst, controlling a system temperature, and reacting with stirring to obtain a quinoline-2,3-fused nine-membered ring compound. According to the present disclosure, a 1,6-hydride transfer/cyclization strategy is triggered by aldimine condensation, the quinoline-derived aniline compound and the formaldehyde compound are prepared into the quinoline-2,3-fused nine-membered ring compound with a wide substrate scope and a potential biological activity by a “one-pot synthesis method” quickly.
Type:
Grant
Filed:
February 8, 2023
Date of Patent:
December 12, 2023
Assignee:
QINGDAO AGRICULTURAL UNIVERSITY
Inventors:
Xiao-De An, Jian Xiao, Daying Shao, Bin Qiu
Abstract: Certain embodiments of the present disclosure provide liquid pharmaceutical formulations, suitable for oral administration, that contain glycerol and an amount of apixaban in the solution phase of the formulations of from 0.5 mg/ml to 6 mg/ml.
Abstract: There is provided a therapeutic agent for Alzheimer's disease and Lewy body dementia for combined use of (S)-7-(2-methoxy-3,5-dimethylpyridin-4-yl)-1-(tetrahydrofuran-3-yl)-1H-pyrazolo[4,3-c]quinoline-4(5H)-one represented by formula (1): or a pharmaceutically acceptable salt thereof, and donepezil represented by formula (II): or a pharmaceutically acceptable salt thereof.
Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.
Type:
Grant
Filed:
March 22, 2022
Date of Patent:
December 5, 2023
Assignee:
NUVATION BIO INC.
Inventors:
David Hung, Jayakanth Kankanala, Christopher Paul Miller, Jeremy David Pettigrew, Son Minh Pham, Ihab S. Darwish
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of diseases and conditions.
Type:
Grant
Filed:
May 7, 2021
Date of Patent:
November 28, 2023
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Mark Brewer, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Bryce A. Harrison, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
Abstract: The present invention concerns a compound of formula (I): or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity, in particular ERK2 activity.
Type:
Grant
Filed:
January 13, 2023
Date of Patent:
November 28, 2023
Assignees:
AGV Discovery, Institut National de la Sante et de la Recherche Medicale (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), Université De Montpellier
Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Type:
Grant
Filed:
April 30, 2021
Date of Patent:
November 21, 2023
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, Trevor C. Sherwood, Brian K. Whiteley, John L. Gilmore, Sreekantha Ratna Kumar, Laxman Pasunoori, Pitani Veera Venkata Srinivas, Srinivasan Kunchithapatham Duraisamy, Subramanya Hegde, Rushith Kumar Anumula
Abstract: Disclosed herein are compounds that can prevent and treat C. difficile by inhibiting sporulation. Also disclosed herein are compositions and formulations comprising the compound disclosed herein. Methods of preventing and treating C. difficile comprising administering the compounds described herein are also disclosed.
Type:
Grant
Filed:
June 27, 2022
Date of Patent:
November 14, 2023
Assignee:
University of South Florida
Inventors:
Yu Chen, Michael Sacco, James Leahy, Elena Bray, Xingmin Sun, Xiujun Zhang
Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Type:
Grant
Filed:
July 13, 2021
Date of Patent:
November 7, 2023
Assignee:
BioCryst Pharmaceuticals, Inc.
Inventors:
Pravin L. Kotian, Yarlagadda S. Babu, V. Satish Kumar, Weihe Zhang, Lakshminarayana Vogeti
Abstract: A compound represented by Formula 1, a stereoisomer thereof or a pharmaceutically acceptable salt thereof may be used for treating or preventing an autoimmune disease or a cancer. The autoimmune disease may be any one selected from the group consisting of inflammatory bowel disease, multiple sclerosis, graft-versus-host disease, asthma, atopy, psoriasis, rheumatoid arthritis, systemic lupus erythematous and type 1 diabetes. The cancer may be selected from the group consisting of colon cancer, melanoma, liver cancer, gliocytoma, ovarian cancer, colorectal cancer, head and neck cancer, bladder cancer, kidney cell cancer, stomach cancer, breast cancer, metastatic cancer, prostate cancer, gallbladder cancer, pancreatic cancer, blood cancer, skin cancer and lung cancer.
Type:
Grant
Filed:
April 25, 2023
Date of Patent:
November 7, 2023
Assignee:
PARENCHYMA BIOTECH INC.
Inventors:
Su Kil Seo, Eun Hye Yoon, Soung Min Lee, Hae Jeong Won, Won Hee Jang, Chae Eun Kim
Abstract: Applicant discloses methods for treating a glucocorticoid receptor positive (GR+) neuroepithelial tumor in a subject, comprising administering a selective glucocorticoid receptor modulator (SGRM) in an amount effective to reduce the tumor load in subject. The GR+ neuroepithelial tumor may be a neurofibromatosis type 2 (NF 2) tumor; the GR+ neuroepithelial tumor may be a schwannoma, meningioma, or ependymoma. In embodiments, the GR+ neuroepithelial tumor is not an adrenocorticotropic hormone (ACTH)-secreting tumor. In embodiments, the SGRM comprises a steroidal backbone. In embodiments, the SGRM is mifepristone. In embodiments, the SGRM comprises a non-steroidal backbone, such as, e.g., a cyclohexyl pyrimidine, a fused azadecalin, a heteroaryl ketone fused azadecalin, or an octahydro fused azadecalin backbone. The SGRM may be administered orally. The SGRM may be administered alone. In embodiments, the SGRM is administered with at least one non-SGRM therapy, e.g.
Abstract: Disclosed are small molecule inhibitors of ?v?6 integrin, and methods of using them to treat a number of specific diseases or conditions.
Type:
Grant
Filed:
May 14, 2021
Date of Patent:
October 24, 2023
Assignee:
Morphic Therapeutic, Inc.
Inventors:
Bryce A. Harrison, Matthew G. Bursavich, Aleksey I. Gerasyuto, Kristopher N. Hahn, Kyle D. Konze, Fu-Yang Lin, Blaise S. Lippa, Alexey A. Lugovskoy, Bruce N. Rogers, Mats A. Svensson, Dawn M. Troast
Abstract: An organic light-emitting device includes: a first electrode; a second electrode; an organic layer between the first electrode and the second electrode and including an emission layer; and at least one organometallic compound represented by Formula 1.
Type:
Grant
Filed:
May 12, 2020
Date of Patent:
October 17, 2023
Assignee:
Samsung Display Co., Ltd.
Inventors:
Jaesung Lee, Sungbum Kim, Soobyung Ko, Haejin Kim, Sujin Shin, Eunsoo Ahn, Eunyoung Lee, Hyunjung Lee, Mina Jeon, Junghoon Han