Abstract: The present invention relates to compounds of formula I as defined herein, and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity. The present invention also relates to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.
Type:
Grant
Filed:
April 29, 2021
Date of Patent:
September 26, 2023
Assignee:
Cancer Research Technology Limited
Inventors:
Emma L. Carswell, Mark David Charles, Chukuemeka Tennyson Ekwuru, Frederic Elustondo, Katherine M. Fowler, Gregory R. Ott, Jonathan R. Roffey, Joanna L. Brookfield, Daniel James Ford, Mathew L. Calder
Abstract: The present invention includes a method for the treatment of age-related macular degeneration, glaucoma, or diabetic retinopathy in a human that comprises administering to the human a therapeutically effective amount of N-acetylcysteine amide (NACA) or (2R,2R?)-3,3?-disulfanediyl bis(2-acetamidopropanamide) (diNACA) sufficient to treat or reduce the symptoms of the age-related macular degeneration, glaucoma, or diabetic retinopathy.
Abstract: The present invention relates to crystalline forms of the compound represented by Structural Formula I, and compositions comprising crystalline forms of the compound represented by Structural Formula I described herein. The crystalline forms of the compound of Structural Formula I and compositions comprising the crystalline forms of the compound of Structural Formula I provided herein, in particular, single crystalline Form A, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders associated with CRM1 activity, including cancer. Also described herein are methods for preparing the compound of Structural Formula I and its single crystalline forms.
Abstract: The present invention relates to crystalline forms of the compound represented by Structural Formula I, and compositions comprising crystalline forms of the compound represented by Structural Formula I described herein. The crystalline forms of the compound of Structural Formula I and compositions comprising the crystalline forms of the compound of Structural Formula I provided herein, in particular, single crystalline Form A, can be incorporated into pharmaceutical compositions, which can be used to treat various disorders associated with CRM1 activity, including cancer. Also described herein are methods for preparing the compound of Structural Formula I and its single crystalline forms.
Abstract: A synthetic route to scopolamine and/or atropine. In such context, the present invention identifies a method for preparing 6,7-dehydro atropine, which can be converted into either scopolamine and/or atropine, along with a method for converting a protected pyrrole into a tetrachlorobicylic compound, such as benzyl 3-oxo-8-azabicyclo[3.2.1]oct-6-ene-8-carboxylate.
Type:
Grant
Filed:
October 7, 2021
Date of Patent:
August 29, 2023
Assignee:
SOUTHWEST RESEARCH INSTITUTE
Inventors:
Shawn T. Blumberg, Paul W. Miguel, Daniel A. Hinojosa
Abstract: The present disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R4?, X1, Y1, Y2, Y3, Y4, n, and m are described herein.
Type:
Grant
Filed:
November 12, 2020
Date of Patent:
August 29, 2023
Assignee:
Valo Health, Inc.
Inventors:
Stephanos Ioannidis, Adam Charles Talbot, Bruce Follows, Alexandre Joseph Buckmelter, Minghua Wang, Ann-Marie Campbell, David R. Lancia, Jr.
Abstract: Provided herein are piperidine dione compounds having the following structure: wherein R1, R2, R3, R4, L, V, X, a and m are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
Type:
Grant
Filed:
June 23, 2021
Date of Patent:
August 29, 2023
Assignee:
Celgene Corporation
Inventors:
Matthew D. Alexander, Matthew D. Correa, Deepak Dalvie, Virginia Heather Sharron Grant, Joshua Hansen, Roy L. Harris, III, Evan J. Horn, Dehua Huang, Christopher Mayne, Stephen Norris, Veronique Plantevin-Krenitsky, John J. Sapienza, Lida Tehrani, Brandon W. Whitefield
Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1?-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.
Abstract: The present application provides bifunctional compounds of Formula (X): or an enantiomer, diastereomer, or stereoisomer thereof, or pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, which act as protein degradation inducing moieties for Bruton's tyrosine kinase (BTK). The present application also relates to methods for the targeted degradation of BTK through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to BTK which can be utilized in the treatment of disorders modulated by BTK.
Type:
Grant
Filed:
December 16, 2020
Date of Patent:
August 22, 2023
Assignee:
DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Nathanael S. Gray, Dennis Dobrovolsky, Hai-Tsang Huang
Abstract: Methods of treating of interstitial lung disease, reducing pulmonary function decline in a subject with interstitial lung disease (ILD), and increasing forced vital capacity (FVC) in a subject suffering from ILD are provided, wherein the methods include administration of treprostinil.
Type:
Grant
Filed:
April 16, 2021
Date of Patent:
August 22, 2023
Assignee:
United Therapeutics Corporation
Inventors:
Leigh Peterson, Peter Smith, Chunqin Deng
Abstract: An 8-dihalomethyl berberine-type quaternary ammonium salt compound represented by general formula (I) or (II) and an application thereof in preparing a drug. The compound shows hydrophilicity and has antimicrobial, anti-inflammatory, anti-ulcerative colitis, and antitumor activities, while having no or low toxicity.
Type:
Grant
Filed:
October 17, 2019
Date of Patent:
August 15, 2023
Assignee:
INSTITUTE OF MATERIA MEDIC, CHINESE ACADEMY OF MEDICAL SCIENCES
Abstract: The present invention provides methods for treating cancer in a subject with a trisubstituted benzotriazole derivative with the formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2 and R3 are as defined herein.
Abstract: A method for the treatment a disease resulting from spondyloarthritis, such as axial spondyloarthritis, psoriatic arthritis and enteropathic arthritis, by administering, to a mammal in need of such treatment, a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof.
Abstract: Described herein are certain crystalline forms of Compound 3, as well as pharmaceutical compositions employing the crystalline forms. Also provided are particles (e.g., nanoparticles) comprising such crystalline forms or pharmaceutical compositions. In certain examples, the particles are mucus penetrating particles (MPPs). The present invention further relates to methods of treating or preventing diseases using crystalline forms or pharmaceutical compositions.
Type:
Grant
Filed:
March 10, 2021
Date of Patent:
August 1, 2023
Assignee:
Kala Pharmaceuticals, Inc.
Inventors:
Elizabeth Enlow, Minh Ngoc Nguyen, Winston Z. Ong
Abstract: This invention relates to methods of identifying, synthesizing, optimizing and profiling compounds that are inhibitors or activators of proteins, both naturally occurring endogenous proteins as well as certain variant forms of endogenous proteins, and novel methods of identifying such variants. The method accelerates the identification and development of compounds as potential therapeutically effective drugs by simplifying the pharmaceutical discovery and creation process through improvements in hit identification, lead optimization, biological profiling, and rapid elimination of toxic compounds. Implementation results in overall cost reductions in the drug discovery process resulting from the corresponding increases in efficiency.
Abstract: Forms of cerdulatinib and salts or co-crystals thereof were prepared and characterized in the solid state. Also provided are processes of manufacture and methods of using the forms cerdulatinib and salts or co-crystals thereof.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
August 1, 2023
Assignee:
Alexion Pharmaceuticals, Inc.
Inventors:
Anjali Pandey, Julian Scott Northen, Philippe Fernandes, Ying Chen, Yuelie Lu, Sami Karaborni, Gus Kodersha
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of ?-synuclein (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon. Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
August 20, 2019
Date of Patent:
July 25, 2023
Assignee:
Arvinas Operations, Inc.
Inventors:
Andrew P. Crew, Hanqing Dong, Michael Berlin, Steven M. Sparks
Abstract: Methods of using a phosphoinositide 3-kinase p110-delta inhibitor to treat, delay the onset, or slow the progression of an autoimmune disease or disorder in a subject, without suppressing the subject's B cell responses to exogenous antigens or rendering the subject immunocompromised, as well as pharmaceutical compositions containing phosphoinositide 3-kinase p110-delta inhibitors in amounts suitable for convenient and accurate administration within these therapeutic methods.
Type:
Grant
Filed:
January 7, 2019
Date of Patent:
July 18, 2023
Assignees:
NATIONAL INSTITUTES OF HEALTH (NCH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT NIH DIVISION OF EXTRAMURAL INVENTIONS AND TECHNOLOGY RESOURCES (DEITR), THE REGENTS OF THE UNIVERSITY OF COLORADO
Abstract: The present invention is directed to an aqueous composition comprising spirotetramat, pyriproxyfen, a solvent system comprising heavy aromatic naphtha, cottonseed oil and optionally, acetyl tributyl citrate, one or more poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) block copolymers and an acrylic type co-polymer having a backbone containing a carboxylated ethylenically unsaturated monomer and a non-carboxylated ethylenically unsaturated monomer and water. The present invention is further directed to methods of controlling pests by applying the compositions of the invention to an area in need thereof.
Abstract: This invention relates to methods of identifying, synthesizing, optimizing and profiling compounds that are inhibitors or activators of proteins, both naturally occurring endogenous proteins as well as certain variant forms of endogenous proteins, and novel methods of identifying such variants. The method accelerates the identification and development of compounds as potential therapeutically effective drugs by simplifying the pharmaceutical discovery and creation process through improvements in hit identification, lead optimization, biological profiling, and rapid elimination of toxic compounds. Implementation results in overall cost reductions in the drug discovery process resulting from the corresponding increases in efficiency.