Abstract: Disclosed are phenyltetrazole derivatives of formula (I), wherein A, R1, R2, X, R?, R?, and n are as defined herein, and pharmaceutically acceptable salts thereof. Also disclosed are methods of using the phenyltetrazole derivatives for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.
Type:
Grant
Filed:
October 7, 2019
Date of Patent:
September 17, 2024
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Dieter Wiedenmayer, Andreas Gollner, Iain Lingard, Holger Wagner
Abstract: Synergistic drug combinations with the small molecule PAC-1 against uveal or cutaneous melanoma. There are no current targeted drug treatments for the mutations associated with uveal melanoma. Despite primary radiation or surgical therapy, up to 50% of patients eventually develop metastatic disease, for which there is no standard therapy nor treatment shown to improve overall survival. Drug combinations with PAC-1 allow the use of lower dosages of this compound that result in cancer cell death in uveal melanoma. Drug combinations of PAC-1 with the kinase inhibitor entrectinib have shown a synergistic effect against uveal melanoma cell lines. Specifically, PAC-1 and entrectinib are synergistic against wild-type and mutant uveal melanoma cell lines (e.g., GNAQ and GNA11).
Type:
Grant
Filed:
October 3, 2019
Date of Patent:
September 17, 2024
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
Paul J. Hergenrother, Matthew Wesley Boudreau
Abstract: The present application provides tricyclic urea compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer.
Type:
Grant
Filed:
March 16, 2023
Date of Patent:
September 10, 2024
Assignee:
Incyte Corporation
Inventors:
Cooper Taylor, Yanran Ai, Chunhong He, Ke Zhang, Eddy W. Yue
Abstract: In a method of producing aqueous solutions of N-bromotaurine (Taurine Bromanine, NBrT) with taurine with latter addition of NaOBr, and emulsions of these solutions with Stable Produced Olive Oil (S.P.O.O.), so to use against hyper-proliferative and abnormally differentiating cells of human and mammalian origin. In addition, due to the hyper-proliferation of keratinocytes in psoriatic skin, the methodology and subsequent use of the aqueous solutions and emulsions derived from this invention, containing NBrT and taurine, and S.P.O.O. against the lesions of psoriasis. With the method of this invention, the solutions derived and applied on cells in vitro beneficially provide maximization of NBrT anti-proliferative properties on abnormally differentiating and hyper-proliferating cells of human and mammalian origin by restoring NBrT anti-proliferative activity in a solution, whilst leaving unaffected the proliferation of normally dividing human fibroblasts.
Abstract: The present disclosure provides solid forms of 6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, and methods of preparing and using the same.
Type:
Grant
Filed:
December 16, 2022
Date of Patent:
June 18, 2024
Assignee:
Pfizer Inc.
Inventors:
Caroline Yvette Proulx-Lafrance, John C. Amedio, Jr., Erika Volckova
Abstract: A topical formulation for transdermal delivery of sub-acute does of doxycycline hyclate to treat pain and inflammation may include: a base suspension; and doxycycline hyclate. The doxycycline hyclate is mixed with the base suspension in a proportion such that the formulation lacks any antibiotic effect and the concentration of doxycycline hyclate is between 200 and 600 mg/g inclusive. A method of applying the formulation is also disclosed.
Abstract: In certain embodiments, the disclosure relates to heterocyclic flavone derivatives, such as those described by formula provided herein, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to methods of treating or preventing diseases or conditions related to BDNF and TrkB activity, such as depression, stroke, Rett syndrome, Parkinson's disease, and Alzheimer's disease by administering effective amounts of pharmaceutical compositions comprising compounds disclosed herein to a subject in need thereof.
Abstract: Provided herein are compounds of Formula (I). Methods for the preparation of the compounds of Formula (I) and intermediates useful in the preparation of the compounds of Formula (I) are described herein. The compounds of Formula (I) may be useful as inhibitors of the MYST family of lysine acetyltransferases (KATs) for the treatment of and/or prophylaxis of hyperproliferative diseases, disorders or conditions such as cancer. In particular, the compounds of Formula (I) are useful for the inhibition of KAT6A and KAT6B which are enzymes frequently mutated, overexpressed, amplified and/or translocated in cancer altering their normal expression, activity and function. The use of the compounds of Formula (I) in the manufacture of pharmaceutical compositions or for treating cancers is further described, including for treating cancer in combination with other anti-cancer agents.