Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lupus erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
Abstract: This invention relates to compounds of Formula (I) or a pharmaceutically acceptable salt thereof, in which R-groups R1 to R23, A, Q, U, V, W, X, Y, Z, n, p and q are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.
Type:
Grant
Filed:
July 29, 2020
Date of Patent:
January 11, 2022
Assignee:
Pfizer Inc.
Inventors:
Ping Chen, Sujin Cho-Schultz, Judith Gail Deal, Gary Michael Gallego, Mehran Jalaie, Robert Steven Kania, Sajiv Krishnan Nair, Sacha Ninkovic, Suvi Tuula Marjukka Orr, Cynthia Louise Palmer
Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
Type:
Grant
Filed:
June 1, 2020
Date of Patent:
January 4, 2022
Assignee:
Prelude Therapeutics, Incorporated
Inventors:
Juan Luengo, Hong Lin, Michael Hawkins, Rupa Shetty, Philip Pitis, Gisela Saborit Villarroya
Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
Type:
Grant
Filed:
August 5, 2020
Date of Patent:
December 28, 2021
Assignee:
Prelude Therapeutics Incorporated
Inventors:
Hong Lin, Juan Luengo, Rupa Shetty, Michael Hawkins
Abstract: This invention is directed to compositions, methods and kits that can be used for reducing cell viability, inducing cell apoptosis, and inhibiting cell proliferation, such as for the treatment of cancer. The invention is also directed to compositions, methods and kits that can be used for treating inflammatory conditions, such as by modulating inflammatory cytokines.
Type:
Grant
Filed:
April 29, 2019
Date of Patent:
December 28, 2021
Assignee:
GLAX LLC
Inventors:
Rakesh K Srivastava, Sharmila Shankar, Sushant Kumar Shrivastava, Anupam G. Banerjee
Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
Abstract: Tetrahydronaphthyridines of formula are disclosed. These compounds selectively inhibit ?V?3 without activating the ?V?3 receptor. They are useful for treating osteoporosis, acute myelogenous leukemia, sickle cell disease, focal segmental glomerulosclerosis, fibrosis, supravalvular aortic stenosis associated with Williams syndrome, tumors expressing ?V?3, tumor metastasis, bone resorption, T-cell lymphoma, retinal disease, age-related macular degeneration, diabetic retinitis, and herpes simplex virus infection. They may also be used for inhibiting tumor angiogenesis.
Type:
Grant
Filed:
July 5, 2017
Date of Patent:
December 7, 2021
Assignee:
THE ROCKEFELLER UNIVERSITY
Inventors:
Barry S. Coller, Marta Filizola, Michael Andrew Foley
Abstract: The present invention relates to the use of pyrimidine compounds of formula (I), or their agriculturally acceptable salts or derivatives as herbicides, wherein the variables are defined according to the description, specific pyrimidine compounds of formula (I), compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidal effective amount of at least one pyrimidine compounds of the formula (I) to act on plants, their seed and/or their habitat.
Type:
Grant
Filed:
July 10, 2017
Date of Patent:
November 23, 2021
Assignee:
BASF SE
Inventors:
Florian Vogt, Matthias Witschel, Tobias Seiser, Veronica Lopez Carrillo, Thomas Seitz, Gerd Kraemer, Klaus Kreuz, Trevor William Newton, Klaus Reinhard, Doreen Schachtschabel
Abstract: Provided are compounds that target plexin domain containing 2 (PLXDC2). The compounds can be used to treat conditions such as inflammatory or immune-mediated diseases, diabetes, infectious diseases, and cancers. The compounds can be used to treat such specific conditions as systemic lupus erythematosus, rheumatoid arthritis, multiple sclerosis, autoimmune encephalitis, diabetic nephropathy, diabetic retinopathy, psoriasis, and inflammatory bowel disease, among other conditions.
Type:
Grant
Filed:
March 25, 2021
Date of Patent:
November 23, 2021
Inventors:
Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas, Nuria Tubau-Juni
Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
Type:
Grant
Filed:
October 17, 2019
Date of Patent:
November 16, 2021
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
Abstract: The present invention relates to stimulators and activators of soluble guanylate cyclase in combination with an inhibitor of neutral endopeptidase and/or angiotensin AII antagonists and the use thereof for the treatment and/or prophylaxis of cardiovascular disorders, for example heart failure with preserved ejection fraction or heart failure with reduced ejection fraction, renal disorders, for example chronic kidney failure, urological disorders, lung disorders, disorders of the central nervous system, for regulation of cerebral perfusion, for example in the event of vascular cerebral states of dementia, for the treatment and/or prophylaxis of fibrotic disorders and other disease symptoms (e.g. end organ damage affecting the brain, kidney or heart).
Type:
Grant
Filed:
July 15, 2016
Date of Patent:
November 9, 2021
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Tobias Marquardt, Markus Follmann, Johannes-Peter Stasch
Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of Kirsten rat sarcoma protein (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, accumulation, and/or overactivation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Type:
Grant
Filed:
April 4, 2019
Date of Patent:
November 2, 2021
Assignee:
ARVINAS OPERATIONS, INC.
Inventors:
Andrew P. Crew, Keith R. Hornberger, Jing Wang, Hanqing Dong
Abstract: The present invention provides RUT analogs with various biological activities. In particular, the biological activities comprise anti-inflammatory activity, vasodilator effects, migration/invasion-suppressive activities, ability against damage due to remodeling between the epithelium and endothelium, collagen deposition and cardiac fibrosis suppress, Snail protein inhibitory effect, etc., which may improve cardiac, vasodilation, and lung functions. The RUT analogs disclosed herein also exhibit a lower cytotoxicity comparing to RUT.
Type:
Grant
Filed:
September 25, 2019
Date of Patent:
October 26, 2021
Assignees:
TAIPEI MEDICAL UNIVERSITY, NATIONAL TAIPEI UNIVERSITY OF TECHNOLOGY
Abstract: The present invention relates to amide derivatives which have blocking activities of voltage gated sodium channels as the Nav1.7 and Nav1.8 channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
Abstract: The present invention relates to compounds suitable for treating, ameliorating and/or preventing neuromuscular disorders, including the reversal of drug-induced neuromuscular blockade. The compounds as defined herein preferably inhibit the CIC-1 ion channel.
Type:
Grant
Filed:
December 14, 2017
Date of Patent:
October 19, 2021
Assignee:
NMD PHARMA A/S
Inventors:
Lars J. S. Knutsen, Thomas Holm Pedersen, Martin Broch-Lipps, Claus Elsborg Olesen, Marc Labelle, Ole Baekgaard Nielsen
Abstract: The present invention relates to crystalline forms of (9E,10E)-2,7-bis((3,5-dimethylpiperidin-1-yl)sulfonyl)anthracene-9,10-dione dioxime, pharmaceutical compositions comprising the crystalline form, processes for preparing the crystalline form and methods of use therefore.
Abstract: Novel, antimitotic heteroaryl amides and pharmaceutically acceptable salts of Formula I where Ar, R5, R6, R8, R9, R11, X1, and X2 are as defined herein, as compounds for treatment and prevention of cancer and proliferative diseases and disorders.
Abstract: The present invention relates to a Rho-associated protein kinase inhibitor of formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and a use of the same in preventing or treating a disease mediated by Rho-associated protein kinase (ROCK).
Type:
Grant
Filed:
June 29, 2018
Date of Patent:
September 28, 2021
Assignee:
BEIJING TIDE PHARMACEUTICAL CO., LTD.
Inventors:
Yanping Zhao, Hongjun Wang, Gong Li, Yuanyuan Jiang, Xiang Li, Bin Liu, Weiting Zhong, Kai Liu, Fajie Li, Liying Zhou, Yanan Liu