Abstract: Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as cancer and tumors, as well as viral infections such as HIV.
Type:
Grant
Filed:
May 26, 2023
Date of Patent:
November 14, 2023
Assignee:
Recurium IP Holdings, LLC
Inventors:
Joseph Robert Pinchman, Peter Qinhua Huang, Kevin Duane Bunker, Rakesh Kumar Sit, Ahmed Abdi Samatar
Abstract: Compounds of Formula (I) are provided herein. Such compounds, as well as pharmaceutically acceptable salts and compositions thereof, are useful for treating diseases or conditions, including conditions characterized by excessive cellular proliferation, such as cancer and tumors, as well as viral infections such as HIV.
Type:
Grant
Filed:
March 28, 2022
Date of Patent:
November 14, 2023
Assignee:
RECURIUM IP HOLDINGS, LLC
Inventors:
Joseph Robert Pinchman, Peter Qinhua Huang, Kevin Duane Bunker, Rakesh Kumar Sit, Ahmed Abdi Samatar
Abstract: The present disclosure relates to compounds and compositions for inhibition of Bcr-Abl tyrosine kinases, methods of preparing said compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML).
Type:
Grant
Filed:
December 13, 2022
Date of Patent:
November 7, 2023
Assignee:
ENLIVEN INC.
Inventors:
Joseph P. Lyssikatos, Samuel Kintz, Li Ren
Abstract: The substituted indolizine dicarboxylates are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against tuberculosis mycobacteria. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Type:
Grant
Filed:
March 28, 2023
Date of Patent:
November 7, 2023
Assignee:
KING FAISAL UNIVERSITY
Inventors:
Katharigatta N. Venugopala, Bandar Aldhubiab, Mohamed A. Morsy, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Christophe Tratrat, Sandeep Chandrashekharappa, Melendran Pillay, Pran Kishore Deb, Sheena Shashikanth
Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
March 15, 2021
Date of Patent:
October 31, 2023
Inventors:
Joseph D. Panarese, Dexter Davis, Nathaniel Thomas Kenton, Samuel Bartlett, Yat Sun Or
Abstract: Disclosed herein are compounds of Formula I?: or a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising such compounds, and methods of treating disease by administering or contacting a subject with one or more of the above compounds.
Type:
Grant
Filed:
November 5, 2021
Date of Patent:
October 24, 2023
Assignee:
Aligos Therapeutics, Inc.
Inventors:
David Craig McGowan, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Jerome Deval, Leonid Beigelman
Abstract: The present disclosure is directed to solid and salt forms of inhibitors of the CBP/p300 family of bromodomains made up of salts and crystalline forms of Formula (I). The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains (e.g., certain forms of cancer), and methods of synthesis of these compounds.
Abstract: The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.
Abstract: The present invention relates to processes of preparing PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3?-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2?-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, or salts thereof, related synthetic intermediates, and salts of the intermediates, where the PD-1/PD-L1 inhibitor is useful in the treatment of various diseases including infectious diseases and cancer.
Type:
Grant
Filed:
November 5, 2021
Date of Patent:
October 10, 2023
Assignee:
Incyte Corporation
Inventors:
Jiacheng Zhou, Shili Chen, Zhongjiang Jia, Yi Li, Qiyan Lin, Pingli Liu, Yongchun Pan, Timothy Martin, Bo Shen, Chongsheng Eric Shi, Naijing Su, Yongzhong Wu, Michael Xia
Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
Type:
Grant
Filed:
October 18, 2021
Date of Patent:
September 26, 2023
Assignee:
Bristol-Myers Squibb Company
Inventors:
Guanglin Luo, Jie Chen, Carolyn Diane Dzierba, David B. Frennesson, Junqing Guo, Amy C. Hart, Xirui Hu, Michael C. Mertzman, Matthew Reiser Patton, Jianliang Shi, Steven H. Spergel, Brian Lee Venables, Yong-Jin Wu, Zili Xiao, Michael G. Yang
Abstract: The present disclosure relates to compounds and compositions for inhibition of Bcr-Abl tyrosine kinases, methods of preparing said compounds and compositions, and their use in the treatment of various cancers, such as chronic myeloid leukemia (CML).
Type:
Grant
Filed:
October 4, 2021
Date of Patent:
September 26, 2023
Assignee:
ENLIVEN INC.
Inventors:
Joseph P. Lyssikatos, Samuel Kintz, Li Ren
Abstract: The present disclosure relates generally to various forms and compositions of N-(5-(5-((1R,2S)-2-fluorocyclopropyl)-1,2,4-oxadiazol-3-yl)-2-methylphenyl)imidazo[1,2-a]pyridine-3-carboxamide useful as a selective inhibitor of c-kit kinase and uses of the same in the treatment of c-kit kinase associated diseases.
Type:
Grant
Filed:
July 15, 2021
Date of Patent:
September 26, 2023
Assignee:
Third Harmonic Bio, Inc.
Inventors:
Gregg F. Keaney, Leonard Walter Rozamus, Jr., Jonathan James Loughrey, Jaclyn Raeburn, Yuxiang Song
Abstract: The present invention relates to crystalline forms of the PD-1/PD-L1 inhibitor (R)-1-((7-cyano-2-(3?-(3-(((R)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-ylamino)-2,2?-dimethylbiphenyl-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid, including methods of preparation thereof, and related synthetic intermediates, where the compound is useful in the treatment of various diseases including infectious diseases and cancer.
Abstract: The present invention is related to crystalline salts of N-(3-(5-((1-ethylpiperidin-4-yl)(methyl)amino)-3-(pyrimidin-5-yl)-1H-pyrrolo[3,2-b]pyridin-1-yl)-2,4-difluorophenyl)propane-1-sulfonamide, a RAF kinase Inhibitor, useful in the treatment of cancer and other diseases.
Type:
Grant
Filed:
March 11, 2022
Date of Patent:
September 12, 2023
Assignee:
Xynomic Pharmaceuticals, Inc.
Inventors:
Ulrike Werthmann, Gerd-Michael Maier, Bodo Betzemeier, Otmar Schaaf
Abstract: The present disclosure provides a compound of Formula (I) or pharmaceutically acceptable salt, stereoisomers thereof, a pharmaceutical composition comprising the compound, and a method for treating or preventing an inflammatory and autoimmune diseases, especially neuroinflammation diseases using the compound.
Type:
Grant
Filed:
September 14, 2021
Date of Patent:
September 5, 2023
Assignee:
1ST Biotherapeutics, Inc.
Inventors:
Jinhwa Lee, Suyeon Jo, Keonseung Lim, A Yeong Park, Gadhe Changdev Gorakshnath, Hwajung Nam, Yeonguk Jeon, Yejin Hwang, Jae Eun Kim, Misoon Kim, Inyoung Yang
Abstract: Disclosed are hydroquinone compounds, preparation methods therefor, and uses thereof in anti-tumor or immunomodulation. The structural formula of the hydroquinone compounds are shown by formula I, wherein X is C?O or CH2; Y is NH, O or absent; R is: a substituted or unsubstituted alkyl group having at least one carbon atom, a substituted or unsubstituted cycloalkyl group having at least three carbon atoms, a substituted or unsubstituted alkenyl group or alkynyl group having at least two carbon atoms; and a substituted or unsubstituted aryl group or heteroaryl group containing at least four carbon atoms. The compounds provided slowly release 2-tert-butyl-4-methoxyphenol in vivo and maintain stable plasma concentration of 2-tert-butyl-4-methoxyphenol (T1/2=12-24 h). The compounds provided by the present invention protect the phenolic hydroxyl group of 2-tert-butyl-4-methoxyphenol, avoids environmental oxidation and increase the environmental stability of drugs containing the compounds.
Type:
Grant
Filed:
August 7, 2020
Date of Patent:
August 29, 2023
Assignees:
BIOMEDICAL ANALYSIS CENTER, ACADEMY OF MILITARY MEDICAL SCIENCES, INSTITUTE OF PHARMACOLOGY AND TOXICOLOGY, ACADEMY OF MILITARY MEDICAL SCIENCES
Inventors:
Xuemin Zhang, Xinhua He, Tao Zhou, Zhenggang Liu, Tao Li
Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
Abstract: The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.
Abstract: Described herein are PHD inhibitors and pharmaceutical compositions comprising said inhibitors. The subject compounds and compositions are useful for the treatment of inflammatory bowel disease.