Abstract: A method of treating or preventing keratin hyperproliferation skin disorders is set forth. The method includes the administration of an mTOR inhibitor to a subject afflicted with the hyperproliferation disorder. The mTOR inhibitor can be administered to the subject via any means known in the art including oral, topical, and transdermal administration.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
April 4, 2023
Assignee:
PALVELLA THERAPEUTICS, INC.
Inventors:
Roger Louis Kaspar, Robyn Patricia Hickerson
Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.
Type:
Grant
Filed:
May 28, 2020
Date of Patent:
March 21, 2023
Assignees:
THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORK, CHEM-MASTER INTERNATIONAL INC.
Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer.
Type:
Grant
Filed:
October 14, 2020
Date of Patent:
March 21, 2023
Assignee:
Incyte Corporation
Inventors:
Oleg Vechorkin, Minh Nguyen, Chao Qi, Anlai Wang, Michael Witten, Yao Xu, Hai Fen Ye, Ke Zhang, Peng Zhao, Wenqing Yao
Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, diseases associated with over production of IL12/IL23, lysosomal storage disorders, filovirus infections, ischemia, and other complications associated with these diseases and disorders.
Abstract: Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.
Abstract: Provided herein are compounds of formula I, compositions comprising the compounds and method of treating various diseases with the compounds and compositions.
Type:
Grant
Filed:
March 6, 2020
Date of Patent:
March 7, 2023
Assignee:
Histogen, Inc.
Inventors:
Alfred P. Spada, Robert J. Temansky, Michael Mueller
Abstract: The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
Type:
Grant
Filed:
November 20, 2020
Date of Patent:
February 28, 2023
Assignee:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Christina Owens, Svitlana Kulyk, Steven D. E. Sullivan, Paul Allegretti, Mandy Loo, Jennifer Kozak, Erik Fenster, Adam D. Hughes
Abstract: A general and modular mechanophore platform that efficiently releases a cargo molecule via a mechanically triggered cascade reaction is described, along with methods of synthesis and use thereof. The mechanophore platform comprises a stable Diels-Alder adduct mechanophore comprising a 2-furylcarbinol derivative as its diene component, wherein the 2-furylcarbinol derivative is, in turn, pre-loaded with a covalently attached cargo molecule, and wherein the Diels-Alder adduct mechanophore is embedded into a polymer chain or polymer network, such that the mechanophore platform undergoes the retro [4+2] cycloaddition reaction under mechanical force to reveal the unstable 2-furylcarbinol derivative, which, in turn, easily decomposes under mild conditions to release its molecule cargo.
Abstract: The disclosure provides therapeutic compositions (i.e., therapeutic agents) and methods of preventing or treating Friedreich's ataxia in a mammalian subject, reducing risk factors, signs and/or symptoms associated with Friedreich's ataxia (e.g., Complex I deficiency), and/or reducing the likelihood or severity of Friedreich's ataxia. The disclosure further provides novel intermediates for the production of said therapeutic compositions and related reduced versions of said therapeutic compositions, which reduce forms may also be used as therapeutic agents (or prodrugs of the therapeutic agent(s)).
Type:
Grant
Filed:
October 2, 2020
Date of Patent:
February 21, 2023
Assignee:
STEALTH BIOTHERAPEUTICS INC.
Inventors:
Dennis Keefe, Guozhu Zheng, Pavels Arsenjans
Abstract: The invention relates to a method for the preparation of a 4,5-dihydroxyisoleucine derivative comprising the steps of asymmetric Claisen rearrangement of a Z-aminocrotyl-glycin ester and subsequent kinetic resolution of the product diastereomer mix by acylase, and subsequent Sharpless dihydroxylation of the resulting 2-amino-3-methylpent-4-enoic acid derivative.
Type:
Grant
Filed:
March 29, 2019
Date of Patent:
February 21, 2023
Assignee:
Heidelberg Pharma Research GmbH
Inventors:
Caroline Knittel, Mary-Ann Siegert, Roderich Süssmuth, Christoph Wink, Gerhard Jas
Abstract: The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
August 13, 2020
Date of Patent:
February 21, 2023
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Paul Angell, John E. Cochran, Benjamin J. Littler, David Siesel, Armando Urbina, Corey Don Anderson, Jeremy J. Clemens, Thomas Cleveland, Timothy Richard Coon, Bryan Frieman, Peter Grootenhuis, Sara Sabina Hadida Ruah, Jason McCartney, Mark Thomas Miller, Prasuna Paraselli, Fabrice Pierre, Sara E. Swift, Jinglan Zhou
Abstract: Disclosed in the invention are a type of compounds having aldolase selective inhibitory activity, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for inhibiting triglyceride and cholesterol synthesis, for reducing fatty acid synthesis, for preventing and/or treating obesity and type II diabetes, for preventing and/or treating tumor, for preventing and/or treating Parkinson's disease, for preventing and/or treating Alzheimer's disease or for prolonging the lifespan of mammals:
Abstract: Disclosed are compounds of formulas (I)-(IX) for treating or preventing a disease or disorder responsive to antagonism of a P2Y14R receptor agonist in a mammal in need thereof, wherein R1-R8, X, Y, Z, X?, Y?, Z?, and A are as defined herein, that are useful in treating an inflammatory such as asthma, cystic fibrosis, and sterile inflammation of the kidney.
Type:
Grant
Filed:
February 11, 2019
Date of Patent:
February 21, 2023
Assignee:
The United States of America, as represented by the Secretary, Department of Health and Human Services
Abstract: A compound is represented by Chemical Formula 1. The compound may be included in, a film, an infrared sensor, a combination sensor, and/or an electronic device. In Chemical Formula 1, X, Y1, Y2, Z1, Z2, Q, R1, and R2 are the same as described in the detailed description.
Type:
Grant
Filed:
August 20, 2021
Date of Patent:
February 14, 2023
Assignee:
Samsung Electronics Co., Ltd.
Inventors:
Ohkyu Kwon, Rae Sung Kim, Dong-Seok Leem, Changki Kim, Insun Park
Abstract: The present disclosure relates to compounds and methods which may be useful as inhibitors of KDM1A for the treatment or prevention of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation in cancer cells in a human or animal subject are also provided for treatment of disease such as acute myelogenous leukemia.
Type:
Grant
Filed:
May 13, 2019
Date of Patent:
February 14, 2023
Assignee:
Imago Biosciences. Inc.
Inventors:
Amy E. Tapper, Cassandra Celatka, Michael Clare, Hugh Y. Rienhoff, Jr.
Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating diseases or disorders in a subject where the subject is in need of an inhibitor of MEK where the compound is according to formula where R1, R2, R2a, R3, R3a, and X are as described herein.
Abstract: The present invention covers new quinoline compounds of general formula (I), in which A, R1, R2, R3, R4, R5, R6, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.
Type:
Grant
Filed:
May 7, 2019
Date of Patent:
February 7, 2023
Assignee:
Bayer Animal Health GmbH
Inventors:
Walter Hübsch, Nils Griebenow, Hans-Georg Schwarz, Daniel Kulke, Claudia Böhm, Kirsten Börngen, Bernd Alig, Wei Zhuang, Iring Heisler, Thomas Ilg, Johannes Köbberling, Adeline Köhler, Niels Lindner, Ulrich Görgens, Claudia Welz, Maike Hink
Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.
Type:
Grant
Filed:
December 11, 2020
Date of Patent:
January 31, 2023
Assignees:
Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.
Inventors:
D. Keith Hester, II, Robert J. Duguid, Martha J. Kelly, Anna Chasnoff, Gang Dong, Edwin L. Crow, Lianhe Shu, Ping Wang, Duk Soon Choi