Abstract: The present disclosure provides LPA antagonists, as well as pharmaceutical compositions comprising the compounds disclosed herein. Also provided are methods for treating LPA-associated diseases, disorders, and conditions.
Abstract: The present embodiments are directed, in part, to processes and compositions that can, for example, be used in the preparation compounds of Formula (I), or a pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
November 17, 2020
Date of Patent:
January 30, 2024
Assignee:
Trevena, Inc.
Inventors:
Brian H. Heasley, Jennifer Wilent, Patrick J. Koestler
Abstract: The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I): or pharmaceutically acceptable salts thereof wherein R, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein. The disclosure also relates to methods of making and using compounds of Formula (I) or pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
May 26, 2022
Date of Patent:
January 23, 2024
Assignee:
PETRA PHARMA CORPORATION
Inventors:
Erin Danielle Anderson, Sean Douglas Aronow, Nicholas A. Boyles, Xiaohong Chen, Surendra Dawadi, Eugene R. Hickey, Thomas Combs Irvin, Edward A. Kesicki, Gabrielle R. Kolakowski, Jennifer Lynn Knight, Manoj Kumar, Katelyn Frances Long, Christopher Glenn Mayne, Johnathan Alexander McLean, Gerit Maria Pototschnig, Hua-Yu Wang, Michael Brian Welch, Tien Widjaja
Abstract: Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.
Type:
Grant
Filed:
June 23, 2021
Date of Patent:
January 23, 2024
Assignee:
WisTa Laboratories Ltd.
Inventors:
Claude Michel Wischik, John Mervyn David Storey, Colin Marshall, James Peter Sinclair, Thomas Craven Baddeley
Abstract: Substituted pyridazinone compounds, conjugates, and pharmaceutical compositions for use in the treatment of neuromuscular diseases, such as Duchenne Muscular Dystrophy (DMD), are disclosed herein. The disclosed compounds are useful, among other things, in the treating of DMD and modulating inflammatory inhibitors IL-1, IL-6 or TNF-?.
Type:
Grant
Filed:
June 11, 2021
Date of Patent:
January 16, 2024
Assignee:
Edgewise Therapeutics, Inc.
Inventors:
Kevin Hunt, Kevin Koch, Alan Russell, Stephen Schlachter, Paul Winship, Chris Steele
Abstract: This invention is based on the discovery that many eye conditions associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The data show that in age-matched patients, the severity of age-related conditions correlates with the abundance of senescent cells, and that clearing senescent cells can help abrogate the condition. Small molecule drugs that remove senescent cells from affected tissue in the eye are provided that have special efficacy in treating ophthalmic conditions. They not only inhibit progression of the disease, they can also reverse some of the pathophysiology—such as neovascularization and vaso-obliteration—that lead to vision loss. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable ophthalmic conditions.
Type:
Grant
Filed:
August 25, 2021
Date of Patent:
January 9, 2024
Assignee:
Unity Biotechnology, Inc.
Inventors:
Pam Tsuruda, Jill Hopkins, Harry Sweigard, Yan Poon, Jamie Dananberg, Daniel Marquess, Nathaniel David
Abstract: The disclosure provides at least one entity chosen from compounds of Formula I, a tautomer thereof, a deuterated derivative of that compound or tautomer, and a pharmaceutically acceptable salt of any of the foregoing, compositions comprising the same, and methods of using the same, including uses in treating APOL1-mediated diseases, including pancreatic cancer, focal segmental glomerulosclerosis (FSGS), and/or non-diabetic kidney disease (NDKD).
Type:
Grant
Filed:
August 26, 2021
Date of Patent:
January 9, 2024
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Jun Myun Ahn, Samantha Angle, Michael Aaron Brodney, Jingrong Cao, John E. Cochran, Jon H. Come, Leslie A. Dakin, Elena Dolgikh, Brad D. Maxwell, Suganthini S. Nanthakumar, Hardwin O'Dowd, Jessica Howard Olsen, Timothy J. Senter, Akira Joseph Shimizu, Steven David Stone, Haoxuan Wang
Abstract: Disclosed herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, that are inhibitors of Polo Like Kinase 4 (PLK4). Also disclosed herein are pharmaceutical compositions comprising the compounds of Formula (I), or pharmaceutically acceptable salts thereof, and one or more pharmaceutically acceptable excipients. Further disclosed herein are methods of treating cancer in a subject in need thereof, comprising administering to the subject an amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 27, 2023
Date of Patent:
January 2, 2024
Assignee:
ORIC PHARMACEUTICALS, INC.
Inventors:
Chudi Ndubaku, Jared Thomas Moore, Paul Anthony Gibbons, Jae Hyuk Chang, F. Anthony Romero, Xiaohui Du, Hiroyuki Kawai, Stephane Ciblat, Hong Wang, Vincent Albert, Lea Constantineau-Forget, Hugo De Almeida Silva, Dilan Emine Polat, Amit Nayyar, Daniel Gordon Michael Shore, Kejia Wu, Joanne Tan
Abstract: Compounds having the structure of Formula (I): and pharmaceutically acceptable salts thereof, wherein X1, R1, R2, R3, R4, R5 and R6 are as defined in the specification; pharmaceutical compositions comprising such compounds and salts; use of such compounds and salts to treat or prevent Prolyl endopeptidase fibroblast activation protein (FAP)-mediated conditions; kits comprising such compounds and salts; and methods for manufacturing such compounds and salts.
Type:
Grant
Filed:
June 12, 2023
Date of Patent:
January 2, 2024
Assignee:
AstraZeneca
Inventors:
Jonas Brånalt, Maria Johansson, Anneli Nordqvist, Marianne Swanson
Abstract: The invention relates to a bromodomain inhibitor. The invention also provides compositions and formulations comprising such compounds, and methods of using and preparing such compounds.
Type:
Grant
Filed:
August 29, 2022
Date of Patent:
December 19, 2023
Assignee:
BETTA PHARMACEUTICALS CO., LTD.
Inventors:
Yan Xu, Xiaofeng Xu, Jiabing Wang, Lieming Ding
Abstract: The present invention relates to a pyrazine derivative, an application thereof in inhibiting SHP2, and a compound of formula (I) or pharmaceutically acceptable salts, esters, isomers, solvates, prodrugs or isotope labels thereof. The structure of the compound of formula (I) is as follows. The novel pyrazine derivative provided by the present invention has excellent inhibition of SHP2 activity and can be used to prevent and/or treat non-receptor protein tyrosine phosphatase-mediated or dependent diseases or disorders.
Type:
Grant
Filed:
January 25, 2023
Date of Patent:
November 28, 2023
Assignee:
SUZHOU GENHOUSE PHARMACEUTICAL CO., LTD
Inventors:
Haifeng Sun, Kuifeng Wang, Tao Zhang, Mengnan Ma, Jinchang Lu
Abstract: The subject invention pertains to compositions and methods for treating neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson's disease (PD), amyotrophic lateral sclerosis (ALS), Huntington's disease (HD), multiple sclerosis, epilepsy, stroke, alcohol withdrawal, progressive supranuclear palsy (PSP), Pick's disease (PiD), corticobasal degeneration (CBD), frontotemporal dementia or parkinsonism linked to chromosome 17 (FTDP-17). The methods of the subject invention further relate to methods of fermentation of bacterial cells and methods of tautomerization of the subject compounds.
Type:
Grant
Filed:
September 15, 2021
Date of Patent:
November 21, 2023
Assignees:
The Hong Kong University of Science and Technology, Southern Marine Science and Engineering Guangdong Laboratory (Guangzhou)
Abstract: The present disclosure relates to novel processes for the preparation of short acting benzodiazepines as well as to novel intermediates in this process. More particularly the disclosure relates to processes and intermediates for preparation of Methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate, commonly known as Remimazolam. The present disclosure also relates to solid state forms of Remimazolam salts, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.
Abstract: The present application relates to the field of medicine. Specifically, disclosed are a compound of formula (I), a preparation method therefor, and a pharmaceutical composition comprising the compound.
Abstract: A synthetic protocol to use a thiourea or urea compound and auric chloride as starting materials to obtain thiazole and benzothiazole derivatives. The synthesis can be conducted at room temperature and the final compound can result from cyclization of the thiourea or urea compound in the presence of an Au salt from the auric chloride.
Abstract: Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor.
Type:
Grant
Filed:
January 27, 2022
Date of Patent:
November 7, 2023
Assignee:
Novartis AG
Inventors:
David R. Anderson, Robert Volkmann, Frank Menniti, Christopher Fanger, Yuelian Xu
Abstract: The present invention provides a process for preparing a compound of the formula (II): wherein R2 is unsubstituted alkyl, characterized by reacting a compound of the formula (I): wherein R1 is hydrogen or a protecting group other than unsubstituted alkyl, with a compound of the formula: R2—OH, wherein R2 is as defined above, in the presence of a sodium salt and/or a magnesium salt.
Abstract: The aminocarbazole compounds 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 gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Abstract: Disclosed is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used to prepare a drug for treating diseases including obstructive airway diseases, bronchiectasis, cystic fibrosis, asthma, emphysema, and chronic obstructive pulmonary diseases.
Type:
Grant
Filed:
October 28, 2022
Date of Patent:
November 7, 2023
Assignee:
Haisco Pharmaceuticals Pte. Ltd.
Inventors:
Yao Li, Zongjun Shi, Guobiao Zhang, Lei Chen, Wenjing Wang, Xiaobo Zhang, Dengyu Zheng, Bo Xu, Xin Liu, Yajun Wang, Fei Ye, Pingming Tang, Jia Ni, Chen Zhang, Pangke Yan
Abstract: Novel first-in-class imidazothiazole- and imidazooxazole-based potent and selective HER4 kinase inhibitors for therapeutic formulations and methods for treating cancer.