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: 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: 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: 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
Abstract: The invention relates to novel methods of preparing cell-binding agent-cytotoxic agent conjugates, wherein the cytotoxic agent is an imine-containing cytotoxic agent bearing a maleimide group. In some embodiments, the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an engineered Cys, such as an engineered Cys in the heavy chain CH3 domain, at a position corresponds to the EU/OU numbering position 442 (or C442) on an antibody CBA. The invention also provides conjugates prepared by the methods of the present invention, compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.
Type:
Grant
Filed:
September 17, 2020
Date of Patent:
February 7, 2023
Assignee:
IMMUNOGEN, INC.
Inventors:
Scott A. Hilderbrand, Benjamin M. Hutchins
Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including infectious disease, autoimmune disease, diabetes, and a chronic inflammatory disease.
Type:
Grant
Filed:
October 20, 2020
Date of Patent:
February 7, 2023
Assignee:
Landos Biopharma, Inc.
Inventors:
Josep Bassaganya-Riera, Adria Carbo Barrios, Richard Gandour, Julian D. Cooper, Raquel Hontecillas
Abstract: The present disclosure provides a compound that exerts an anticancer action based on CHK1 inhibition. The present disclosure was completed by finding that a compound represented by formula (1) or a pharmaceutically acceptable salt thereof exhibits an excellent antitumor action by having a potent inhibitory action against CHK1: wherein R1, R2, L, V, W, and Q are as defined herein, X, Y, and Z each independently represent CR8 or a nitrogen atom, wherein X, Y, and Z are not simultaneously CR8, and R8 is as defined herein.
Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.
Abstract: The invention provides compounds having the general formula I: and pharmaceutically acceptable salts thereof, wherein the variables R1, R2, R3, R4, subscript m and n, have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Type:
Grant
Filed:
July 9, 2020
Date of Patent:
January 24, 2023
Assignee:
ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
Inventors:
Sidney Hecht, Omar Khdour, Sandipan Roy Chowdhury, Nishant P. Visavadiya
Abstract: The present invention relates to oxopiperazines that mimic helix ?B of the C-terminal transactivation domain of HIF1?. Also disclosed are pharmaceutical compositions containing these oxopiperazines and methods of using these oxopiperazines (e.g., to reduce gene transcription, treat or prevent disorders mediated by interaction of HIF1? with CREB-binding protein and/or p300, reduce or prevent angiogenesis in a tissue, induce apoptosis, and decrease cell survival and/or proliferation).
Type:
Grant
Filed:
August 3, 2020
Date of Patent:
January 24, 2023
Assignee:
NEW YORK UNIVERSITY
Inventors:
Paramjit S. Arora, Brooke Bullock Lao, Richard Bonneau, Kevin Drew
Abstract: The invention relates to compounds of the formula (I) or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.
Type:
Grant
Filed:
March 25, 2019
Date of Patent:
January 3, 2023
Assignee:
NOVARTIS AG
Inventors:
Luca Arista, Christina Hebach, Gregory John Hollingworth, Philipp Holzer, Patricia Imbach-Weese, Rainer Machauer, Niko Schmiedeberg, Anna Vulpetti, Thomas Zoller
Abstract: The present invention relates to heterobifunctional compounds (degraders), compositions and methods for treating diseases or conditions mediated by Interleukin Receptor-Associated Kinases (IRAKs).
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:
April 22, 2022
Date of Patent:
December 27, 2022
Assignee:
Deciphera Pharmaceuticals, LLC
Inventors:
Rodrigo Ruiz Soto, Oliver Rosen, Jama Pitman
Abstract: The present invention provides compounds of formula (I) that are PDE1 enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.
Type:
Grant
Filed:
December 19, 2018
Date of Patent:
December 27, 2022
Assignee:
H. Lundbeck A/S
Inventors:
Jan Kehler, Lars Kyhn Rasmussen, Morten LanggÄrd, Mikkel Jessing, Paulo Jorge Vieira Vital, Karsten Juhl, Mauro Marigo