Abstract: Provided is a compound of formula I or a pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, isotopic substituent, polymorph, prodrug, or metabolite thereof. Also provided is a method for preparing the compound of formula I. The compound of formula I has higher inhibitory activity against SHP2, and thus can be used to prevent or treat a disease related to SHP2.
Abstract: Provided herein are crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate. Pharmaceutical compositions comprising crystalline forms of (R)-5-carbamoylpyridin-3-yl-2-methyl-4-(3-(trifluoromethoxy)benzyl)piperazine-1-carboxylate are also disclosed.
Type:
Grant
Filed:
June 3, 2021
Date of Patent:
June 20, 2023
Assignees:
Celgene Corporation, Lundbeck La Jolla Research Center, Inc.
Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, m, n, and p 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:
December 7, 2020
Date of Patent:
June 13, 2023
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Dharmpal S. Dodd, Tasir Shamsul Haque, Louis J. Lombardo, John E. Macor, Christopher P. Mussari, Laxman Pasunoori, Sreekantha Ratna Kumar, Trevor C. Sherwood, Shoshana L. Posy, Ramesh Kumar Sistla, Subramanya Hegde, Anupama Kandhi Ramachandra Reddy
Abstract: A pharmaceutical composition containing palbociclib tosylate and letrozole, in which palbociclib tosylate and letrozole are in one dosage unit, and the particles of the active ingredient palbociclib tosylate and letrozole are not separated from each other, and the production of the pharmaceutical preparation, the granule containing palbociclib tosylate and letrozole, the use of the pharmaceutical preparation and special blister packaging that facilitates the use of a specific dosage regimen.
Abstract: Provided herein are methods of treating, managing and/or preventing viral infections. A particular method comprises administering to a subject in need thereof an effective amount of an adaptor associated kinase 1 inhibitor of the formula wherein R1, R2 and R3 are defined herein.
Type:
Grant
Filed:
April 19, 2021
Date of Patent:
June 6, 2023
Assignee:
LEXICON PHARMACEUTICALS, INC.
Inventors:
Suma Gopinathan, Praveen Tyle, Qi Melissa Yang
Abstract: The present disclosure relates to methods and compositions for treating cancer with a diaryl macrocycle in combination with an inhibitor of MAPK/ERK kinase-1 and -2 (MEK1 and MEK2; MAP2K1 and MAP2K2), such as trametinib.
Type:
Grant
Filed:
November 25, 2020
Date of Patent:
June 6, 2023
Assignee:
Turning Point Therapeutics, Inc.
Inventors:
Wei Deng, Dayong Zhai, Laura Rodon, Brion W. Murray, Jingrong J. Cui, Nathan V. Lee
Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.
Type:
Grant
Filed:
December 1, 2020
Date of Patent:
May 23, 2023
Assignee:
Imago Biosciences, Inc.
Inventors:
John M. McCall, Hugh Y. Rienhoff, Jr., Michael Clare
Abstract: Methods of treating glioblastoma are provided comprising: administering a therapeutically effective amount of azeliragon, or a pharmaceutically acceptable salt thereof, and co-administering an effective amount of radiation therapy (RT), to a patient who has been diagnosed with glioblastoma. In another aspect, methods are provided for treating grade I, grade II, and grade III gliomas, the method comprising administering a therapeutically effective amount of azeliragon, or a pharmaceutically acceptable salt thereof, and co-administering an effective amount of radiation therapy (RT), to a patient who has been diagnosed with glioma.
Abstract: Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
Type:
Grant
Filed:
June 5, 2020
Date of Patent:
May 9, 2023
Assignee:
H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.
Inventors:
Ernst Schönbrunn, Nicholas J. Lawrence, Harshani R. Lawrence
Abstract: Disclosed are a diazaindole derivative as shown in formula I and the use thereof in the preparation of a drug for treating Chk1-related diseases.
Abstract: The present invention relates to compounds for targeted immunotherapy, as well as compositions comprising the same. Further, the present invention relates to the use of the compounds in the treatment of diseases such as cancer.
Abstract: The present invention relates to compounds for targeted immunotherapy, as well as compositions comprising the same. Further, the present invention relates to the use of the compounds in the treatment of diseases such as cancer.
Abstract: The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention.
Abstract: The present technology provides an isolated compound of Formula I, compositions including such compounds, methods of inhibiting TGF-? signaling and/or TGF-? induced epithelial mesenchymal transitions (EMT), and treating certain cancers involving TGF-? signaling and/or EMT.
Type:
Grant
Filed:
December 15, 2020
Date of Patent:
April 4, 2023
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Timothy Bugni, Fan Zhang, Douglas Braun, Gene Ananiev, F. Michael Hoffmann
Abstract: The present disclosure provides, inter alia, Compounds of Formulae IA, IB, IC, IIA, IIB and IIC or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
Type:
Grant
Filed:
April 1, 2019
Date of Patent:
March 21, 2023
Assignee:
CHEMOCENTRYX, INC.
Inventors:
Pingchen Fan, Rebecca M. Lui, Rajinder Singh, Venkat Reddy Mali, Yibin Zeng, Penglie Zhang
Abstract: The invention relates to acid addition salts of piperazine derivatives, as well as solid forms, such as polymorphic forms, thereof, which are useful as pharmaceutical ingredients and, in particular, as glycosidase inhibitors.
Type:
Grant
Filed:
May 18, 2020
Date of Patent:
February 28, 2023
Assignee:
Asceneuron SA
Inventors:
Anna Quattropani, Santosh S. Kulkarni, Awadut Gajendra Giri, Dawn V. Toronto, David Malcolm Crowe
Abstract: Disclosed is a macrocyclic kinase inhibitor, wherein the compound, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof is as shown in formula I. Experiments show that the new compound as shown in formula I disclosed in the present invention exhibits an excellent TRK inhibitory activity, has a significant inhibitory effect on TRKA-mutant cell growth, and exhibits an excellent inhibitory effect on in vivo tumor growth, thus providing a new choice for the clinical treatment of diseases associated with abnormal TRK activity.
Abstract: Aspects of the invention relate to compounds, pharmaceutical compositions, methods for the manufacturing of compounds and methods for treatment of various disorders mediated at least in part by one or more galectins.
Type:
Grant
Filed:
August 3, 2018
Date of Patent:
February 21, 2023
Assignee:
GALECTIN SCIENCES, LLC
Inventors:
Raphael Nir, Eliezer Zomer, Peter G. Traber, Joseph M. Johnson, Ryan George, Sharon Shechter
Abstract: The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
May 3, 2022
Date of Patent:
February 14, 2023
Assignee:
Deciphera Pharmaceuticals, LLC
Inventors:
Rodrigo Ruiz Soto, Oliver Rosen, Jama Pitman