Abstract: A method for treating a viral infection of a mammalian subject that comprises administering a virus-inhibiting amount of a halogenated xanthene, a pharmaceutically acceptable salt, an alkyl ester or amide or aromatic ester or amide derivative thereof as disclosed within, to that mammalian subject. A method of inducing a type I interferon response in a mammalian subject that presents with a microbial infection, cancerous tumor or hematological malignancy that comprises administering an amount of a halogenated xanthene as discussed above, effective to induce the type I interferon response. A method of enhancing a mammalian immunogen-specific immune response that comprises contacting mammalian cells, in vivo or present in a mammalian cell growth supporting medium, with an adjuvant-effective amount of a halogenated xanthene as discussed above, and an immunogen to which that response is to be enhanced.
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
May 7, 2024
Assignees:
Provectus Pharmatech, Inc., UTI Limited Partnership
Inventors:
Aru Narendran, Edward V. Pershing, Dominic Rodrigues, Bruce Horowitz, Eric A. Wachter
Abstract: Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
Type:
Grant
Filed:
July 29, 2021
Date of Patent:
April 23, 2024
Assignee:
SKYHAWK THERAPEUTICS, INC.
Inventors:
Michael Luzzio, Brian Lucas, Tiansheng Wang, Jun Feng
Abstract: The present invention relates to a process for the preparation of crystalline Bortezomib of formula (I) and its pharmaceutical acceptable salts thereof. The present invention relates to a process for the preparation of highly pure crystalline Bortezomib (I).
Abstract: The present invention is directed to compounds of formula IIa These compounds are considered useful for the treatment of diseases associated with leucine-rich repeat kinase 2 (LRRK2) such as Parkinson's disease. Furthermore, the invention relates to pharmaceutical compositions comprising said compounds.
Type:
Grant
Filed:
September 14, 2023
Date of Patent:
April 16, 2024
Assignee:
H. Lundbeck A/S
Inventors:
Thomas Jensen, Thomas Andersen, Mikkel Jessing, Jacob Nielsen, Henrik Daver, Christopher Richard Jones
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30).
Type:
Grant
Filed:
February 18, 2022
Date of Patent:
April 2, 2024
Assignee:
Mission Therapeutics Limited
Inventors:
Alison Jones, Mark Ian Kemp, Martin Lee Stockley, Michael David Woodrow
Abstract: A method of inducing a Type I interferon response in a mammalian subject that presents with a microbial infection, cancerous tumor or hematological malignancy that comprises administering an amount of a halogenated xanthene as discussed above, effective to induce the Type I interferon response. A method of enhancing a mammalian immunogen-specific immune response that comprises contacting mammalian cells, in vivo or present in a mammalian cell growth supporting medium, with an adjuvant-effective amount of a halogenated xanthene, and an immunogen to which that response is to be enhanced. A mammalian HX compound-adjuvanted vaccine composition that contains an immunogen present in a vaccine-effective amount along with an adjuvant-effective amount of a halogenated xanthene (HX) compound and one or more excipients present at about 0.001% by weight to 10% by weight of the vaccine composition dissolved or dispersed in a pharmaceutically acceptable diluent.
Type:
Grant
Filed:
September 29, 2021
Date of Patent:
March 26, 2024
Assignees:
Provectus Pharmatech, Inc., UTI Limited Partnership
Inventors:
Aru Narendran, Dominic Rodrigues, Edward V. Pershing, Bruce Horowitz
Abstract: The present invention provides solid forms of compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, methods of producing the same, and methods of using the same in the treatment of ACC-mediated diseases.
Abstract: The present invention relates to a novel route of synthesis for the opioid receptor antagonist Buprenorphine or a pharmaceutically acceptable salt thereof, starting from thebaine, wherein the route comprises the reaction of thebaine with a dienophile; forming an alkylated reaction product by reaction with a Grignard-reagent; formation of an cyanamide; deprotection of the cyanamide- and the phenolic-oxygen-moiety, wherein the cleavage of one or both groups is performed in the presence of an alkali or alkaline earth sulfide; followed by derivatization with a cyclopropyl-halogen and hydrogenation to yield Buprenorphine.
Abstract: The present invention relates to compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.
Abstract: The disclosure includes compounds of Formula (A), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11, h, j, m, n, k, v, s, g, V, W, L, Z1, Q1, Q2, Q3, Q4, Q5, Q6, and Q7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.
Abstract: The present disclosure relates to tricyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer.
Type:
Grant
Filed:
December 3, 2020
Date of Patent:
February 13, 2024
Assignee:
Incyte Corporation
Inventors:
Matthew S. McCammant, Evan Styduhar, Oleg Vechorkin, Robert Swyka, Wenqing Yao
Abstract: The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.
Abstract: Novel 5-substituted pyrido[3?,4?:4?,5?]pyrrolo[3?,2?:4,5]imidazo[1,2-a]pyrazine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 5-substituted pyrido[3?,4?:4?,5?]pyrrolo[3?,2?:4,5]imidazo[1,2-a]pyrazine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
Abstract: Novel pyrrolo[2,3-c][1,6]naphthyridine-8-carboxylic acid compounds, a method of synthesizing these compounds, a pharmaceutical composition comprising these compounds and a suitable carrier, and a method of using the compounds. The pyrrolo[2,3-c][1,6]naphthyridine-8-carboxylic acid compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
Abstract: The present invention relates to new compounds derived from marine actinomycetes Streptomyces, and the new compound according to the present invention has an inhibitory effect of NO production on BV-2 microglia stimulated with LPS, and thus can be utilized for the prevention and treatment of neuroinflammatory diseases.
Type:
Grant
Filed:
June 3, 2019
Date of Patent:
January 23, 2024
Assignee:
KOREA INSTITUTE OF OCEAN SCIENCE & TECHNOLOGY
Inventors:
Hee Jae Shin, Byeoung Kyu Choi, Hwa Sun Lee, Hyi Seung Lee, Yeon Ju Lee, Jong Seok Lee, Ji Hoon Lee
Abstract: This application relates to compounds of Formula (I): or pharmaceutically acceptable salts thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.
Type:
Grant
Filed:
January 27, 2021
Date of Patent:
January 16, 2024
Assignee:
Incyte Corporation
Inventors:
Xiaozhao Wang, Heeoon Han, Matthew S. McCammant, Liangxing Wu, Wenqing Yao, Zhiyong Yu, Le Zhao
Abstract: The present invention relates to a cocrystal of progesterone, which is formed by the active ingredient progesterone and a cocrystal former which is selected from isophthalic acid, 4-formylbenzeneboronic acid and 3-nitrophthalic acid. The present invention also relates to the method for preparing the cocrystal of progesterone and use thereof for increasing the thickness of endometrium, improving progesterone's solubility or increasing progesterone's permeation rate.
Type:
Grant
Filed:
March 4, 2021
Date of Patent:
January 9, 2024
Assignee:
NATIONAL INSTITUTES FOR FOOD AND DRUG CONTROL
Inventors:
Lan He, Jing Xiong, Xiangxiang Wu, Xin Zhu, Zhonglin Lu, Yan Shi, Na Zhang, Yang Liu