Abstract: Disclosed herein are liquid diluents, formulations, and kits for preparing reconstituted suspensions of a proton pump inhibitor (e.g., omeprazole). The present disclosure also provides formulations for liquid diluents that do not have a tendency for gel formation following exposure to freeze-thaw cycles.
Abstract: Disclosed are a series of benzo 2-azaspiro[4.4]nonane compounds, and specifically disclosed are a compound as represented by formula (P) or a pharmaceutically acceptable salt thereof.
Abstract: The present invention includes pharmaceutical composition comprising (2R,2R?)-3,3?-disulfanediyl bis(2-acetamidopropanamide)(diNACA) or D3-N-acetyl cysteine amide, or a physiologically acceptable salt thereof, having a deuterium enrichment above the natural abundance of deuterium, and derivatives or solids thereof, and methods of using diNACA to treat eye diseases and other diseases associated with oxidative damage including, e.g., antivenom, beta-thallassemia, cataract, chronic obstructive pulmonary disease, macular degeneration, contrast-induced nephropathy, asthma, lung contusion, methamphetamine-induced oxidative stress, multiple sclerosis, Parkinson's disease, platelet apoptosis, Tardive dyskinesia, Alzheimer disease, HIV-1-associated dementia, mitochondrial diseases, myocardial myopathy, neurodegenerative diseases, pulmonary fibrosis, skin pigmentation, skin in need of rejuventation, antimicrobial infection, Friedreich's ataxia.
Abstract: Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III) and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.
Type:
Grant
Filed:
June 1, 2022
Date of Patent:
September 12, 2023
Assignee:
ACEA Therapeutics, Inc.
Inventors:
Long Mao, Xiao Xu, Namir Shaabani, Can Jin
Abstract: The present invention provides a compound of the formula I, a process for its preparation and the use of a medicament for the treatment of cancer. The compound of the present invention has an inhibitory effect on various cancer cells and can be biologically converted into the active drug Linifanib in vitro (in plasma) to inhibit the proliferation of tumor cells, especially liver cancer cells, at a lower dose.
Type:
Grant
Filed:
November 17, 2017
Date of Patent:
August 1, 2023
Assignee:
3D MEDICINES (BEIJING) CO., LTD.
Inventors:
John Gong, Yihui Lin, Fengqing Li, Fangqiang Tang
Abstract: Disclosed is an oral pharmaceutical composition for preventing or treating dry eye syndrome, which comprises rebamipide or a prodrug thereof, or a pharmaceutically acceptable salt thereof, as an active ingredient. The compounds can treat dry eye syndrome via oral route, and can be thus employed safely and conveniently compared to conventional eye drops.
Abstract: The present disclosure is directed to methods of treating fibrotic conditions by administration of TR? agonists. The disclosure provides methods wherein the abnormal deposition of extracellular matrix components, such as collagen, keratin, or elastin, is reduced, either through interaction of TR? agonists with TGF-?-dependent inflammatory pathways, or by other mechanisms, thereby ameliorating fibrotic symptoms.
Type:
Grant
Filed:
June 4, 2018
Date of Patent:
July 25, 2023
Assignee:
Viking Therapeutics, Inc.
Inventors:
Brian Lian, Hiroko Masamune, Geoffrey E. Barker
Abstract: Provided is a novel compound that has an excellent ?-lactamase inhibitory effect. More specifically, provided is a compound represented by formula (1a), (1b) or (11) having an excellent ?-lactamase inhibitory effect or a pharmaceutically acceptable salt thereof. By using this compound either in combination with a ?-lactam drug or alone, a useful preventive or therapeutic agent for bacterial infections is provided. Also provided are useful preventive or therapeutic agents for treating various diseases with the combined use of the aforesaid compound and ?-lactam drugs.
Type:
Grant
Filed:
April 26, 2019
Date of Patent:
July 18, 2023
Assignees:
Sumitomo Pharma Co., Ltd., THE KITASATO INSTITUTE
Abstract: The present invention provides methods for inhibiting Fyn kinase, using 5-3-pyridin-2-amine, 6-3-imidazo[1,2-a] pyrazine, 6-3-imidazo[1,2-b] pyridazine, N-(5-imidazo [2,1-b][1,3,4] thiadiazol-2-yl)-amine, 4-3-1H-pyrazolo[3,4-b] pyridine, and N-(3-imidazo [1,2-b] pyridazin-6-yl) amine compounds and methods of treatment, prevention, inhibition or amelioration of diseases and conditions associated with Fyn kinase using such compounds.
Abstract: The subject matter disclosed herein is directed to novel She inhibitors of Formula (II). These compounds are useful for treating impaired insulin sensitivity, glucose tolerance, obesity, diabetes, metabolic syndrome, NAFLD, NASH, PSC, PBC, or other metabolic syndrome component conditions.
Abstract: This disclosure relates to certain compounds that are effective in the treatment of a Rac-GTPase mediated disorder (e.g., acute lymphoblastic or chronic myelogenous leukemia), as well as methods for the manufacture of and the use of these compounds (e.g., for treating a Rac-GTPase mediated disorder).
Abstract: A crystal form of a pyrazin-2(1H)-one compound and a preparation method therefor. The present invention specifically related to a compound of formula (II) and a preparation method for a crystal form of the compound.
Abstract: Disclosed herein are compounds of Formula I?. Compounds of Formula I? inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
Abstract: This disclosure is in the field of medicinal chemistry, and relates to a new class of small-molecules having the Formula I, or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer, a mixture of enantiomers, a mixture of two or more diastereomers, or an isotopic variant thereof, wherein the variables Ring A, X, R1a, R1b, R2, R3, R4, m, n, and p are described herein, which function as dual inhibitors of EGFR proteins and PI3K proteins. The disclosure further relates to the use of the compounds described herein as therapeutics for the treatment of diseases and conditions mediated by EGFR proteins and/or PI3K proteins, such as cancer and other diseases.
Type:
Grant
Filed:
December 21, 2021
Date of Patent:
June 13, 2023
Assignee:
Mekanistic Therapeutics LLC
Inventors:
Christopher E. Whitehead, Judith S. Leopold
Abstract: The invention provides compounds that inhibit human MLKL, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
Type:
Grant
Filed:
August 26, 2019
Date of Patent:
June 6, 2023
Assignee:
National Institute of Biological Sciences, Beijing
Inventors:
Zhiyuan Zhang, Xiaodong Wang, Shaoqiang Huang, Bo Yan, Lei Liu, Huayi Wang, Jianguang Han, Zhi Huang, Weiye Cao
Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
Type:
Grant
Filed:
June 5, 2020
Date of Patent:
June 6, 2023
Assignee:
Servier Pharmaceuticals LLC
Inventors:
Janeta Popovici-Muller, Rene M. Lemieux, Jeremy Travins, Zhenwei Cai, Dawei Cui, Ding Zhou
Abstract: The present disclosure provides a crystal form of a compound and fumaric acid, an active pharmaceutical ingredient and a pharmaceutical composition containing the same, and a method for treating coronavirus-induced diseases a using the same. In particular, the crystal form of the present disclosure comprises the compound of Formula (I) and fumaric acid, and the X-ray powder diffraction pattern of the crystal form obtained using Cu-K? radiation includes at least three peaks selected from the group consisting of: 0.94°±0.2° 2?, 19.06°±0.2° 2?, 23.50°±0.2° 2?, and 24.66°±0.2° 2?. The crystal form of the present disclosure has a high purity, good stability, and a high melting point.
Type:
Grant
Filed:
October 12, 2022
Date of Patent:
May 23, 2023
Assignees:
BEIJING GRAND JOHAMU PHARMACEUTICAL COMPANY, LTD., NANJING GRITPHARMACO., LTD.
Inventors:
Weiye Wei, Jiannan Yang, Xiaotao Wu, Taotao Zhao, Hao Wang, Chao Li, Lei Qu, Bin Wang
Abstract: Disclosed herein are novel compounds for degrading Tau protein aggregates, pharmaceutical acceptable salts, enantiomers, non-enantiomers, tautomers, racemates, solvates, metabolic precursors, or prodrugs thereof. Also disclosed herein are uses of the compounds, pharmaceutical acceptable salts, enantiomers, non-enantiomers, tautomers, racemates, solvates, metabolic precursors, or prodrugs thereof in manufacture a medicament for treating a tauopathy, as well as method for aiding in the treatment of a tauopathy or treating a tauopathy in a subject.
Type:
Grant
Filed:
March 4, 2022
Date of Patent:
May 9, 2023
Assignee:
APRINOIA THERAPEUTICS LIMITED
Inventors:
Paul Tempest, Ming-Kuei Jang, Yih-Shyan Lin
Abstract: The present disclosure provides a compound of formula (I) targeting and degrading BCR-ABL protein and its use in the field of antitumor. The compound of formula (I) shows degradation and inhibitory effects on BCR-ABL target protein, which is mainly comprised of four moieties, wherein the first moiety (BCR-ABL-TKIs) is compound moiety with BCR-ABL tyrosine kinase inhibited activity; the second moiety (the LIN) is link units; the third moiety (the ULM) is a small molecule ligand for VHL or CRBN proteases with ubiquitination; and the four moiety (the group A) is carbonyl group that covalently binds to BCR-ABL-TKIs and LIN, and the LIN is further covalently bonded to ULM. A series of compounds designed and synthesized by the present disclosure shows extensive pharmacological effective, which function to degrade BCR-ABL protein and inhibit BCR-ABL effective, and can be utilized for treating relevant tumor.
Type:
Grant
Filed:
September 9, 2020
Date of Patent:
May 2, 2023
Assignee:
ShanghaiTech University
Inventors:
Xiaobao Yang, Biao Jiang, Qianqian Yin, Jinju Chen, Quanju Zhao, Chaowei Ren, Renhong Sun, Ning Sun, Xing Qiu, Ying Kong, Yan Li, Linyi Liu
Abstract: A compound of Formula I includes a stereoisomer thereof and/or a salt thereof; wherein R1 is a substituted alkane group, a heterocylic group, or a pyridine group; X is hydrogen, a halogen, an amino acid residue, a substituted amino acid residue, an alkyl group, or an ester.