Abstract: The disclosure includes compounds of Formula (A): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12, j, k, m, n, Y, W, W1, W2, W3, V, L, Z1, Q1, Q2, Q3, and Q4, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neurodegenerative disease with these compounds.
Abstract: The present invention relates to novel benzohydroxamic compounds of formula (I) and (II) and pharmaceutically acceptable salts, isomers and prodrugs thereof, exhibiting a high selective inhibitory activity against histone deacetylase 6 (HDAC6) enzyme.
Type:
Grant
Filed:
April 12, 2018
Date of Patent:
June 7, 2022
Assignee:
ITALFARMACO SPA
Inventors:
Barbara Vergani, Gianluca Caprini, Gianluca Fossati, Maria Lattanzio, Mattia Marchini, Gianfranco Pavich, Marcello Pezzuto, Chiara Ripamonti, Giovanni Sandrone, Christian Steinkühler, Andrea Stevenazzi
Abstract: YAP1 inhibitors and methods of treating a subject with a cancer that include administering a YAP1 inhibitor are disclosed. Also disclosed are methods for determining responsiveness to a YAP1 inhibitor in a subject, methods for diagnosing a tumor in a subject including determining the level of YAP1 expression, compositions that include YAP1 inhibitors, and methods of using those compositions.
Abstract: The present invention relates to a new compound and a preparation method thereof. The general structural formula of the compound is shown in Formula I. Animal experiments show that the compound has the effect of saving the memory of animal models. It is of high safety, has no mutagenicity, can remain in blood for several hours after oral or intravenous injection, and can enter the brain. The compound can be used for preparing a medicament for treating Alzheimer's disease.
Abstract: Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.
Type:
Grant
Filed:
August 19, 2021
Date of Patent:
May 10, 2022
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Maan T. Khayat, Dhaval Shah, Martin K. Safo, Azizah M. Malebari, Farid Ahmed
Abstract: Provided herein are timosaponin compounds of Formula I, II, III, I?, II? and III?, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are uses of said timosaponin compounds for preparing medicament for the treatment of diseases associated with beta-amyloid in hosts or subjects in need thereof.
Abstract: A polyfluoro-substituted aromatic heterocyclic derivative having the structure as represented by formula I or formula I?, wherein at least one of R1 and R2 is a fluorine atom, and at least two substituents of Rc, Rd, Re, and Rf are fluorine atoms; and an optical isomer of the derivative, or a pharmaceutically acceptable salt or solvate of the same, or a pharmaceutically acceptable salt or solvate of the optical isomer of the same. A composition containing the polyfluoro-substituted aromatic heterocyclic derivative and an application of the composition in preparing an anti-tumour medicament. The compound provides significant inhibitory effects with respect to Akt1 and demonstrates strong proliferation inhibitory activity with respect to tumour cell lines such as an ovarian cancer cell line, a colon cancer cell line, and a prostate cancer cell line.
Abstract: Crystalline molecular framework:small molecule compounds. The molecular framework is formed from guanidinium cations and organosulfonate anions and the guanidinium cations and organosulfonate anions are associated via one or more hydrogen bond. The small molecule(s) is/are encapsulated by the molecular framework. Methods for making crystalline molecular framework:small molecule compounds may include combining guanidinium cations, organosulfonate anions, and small molecules in a single step. The crystalline molecular framework:small molecule compounds can be used to determine the structure of the small molecule(s).
Type:
Grant
Filed:
June 7, 2019
Date of Patent:
April 26, 2022
Assignee:
New York University
Inventors:
Michael David Ward, Yuantao Li, Chunhua Tony Hu
Abstract: Therapeutic compounds containing a phenyl core and amide link(s). Also described are pharmaceutical compositions incorporating the therapeutic compounds and a method for treating cancer with the compounds. These compounds are cytotoxic to stomach, colon, breast, and leukemia cancer cell lines via dual inhibition of Src kinases and tubulin.
Type:
Grant
Filed:
August 19, 2021
Date of Patent:
April 26, 2022
Assignee:
King Abdulaziz University
Inventors:
Moustafa E. El-Araby, Abdelsattar M. Omar, Maan T. Khayat, Dhaval Shah, Martin K. Safo, Azizah M. Malebari, Farid Ahmed
Abstract: The present disclosure provides pharmaceutical compositions comprising 2-arylsulfonamido-N-arylacetamide derivatized Stat3 inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use.
Type:
Grant
Filed:
January 23, 2018
Date of Patent:
April 12, 2022
Assignee:
University of Hawaii
Inventors:
James Turkson, Peibin Yue, Marcus Tius, Christine Brotherton-Pleiss, Francisco Javier Lopez Tapia
Abstract: Disclosed herein are compounds of the formulas: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to inhibit ROR? and/or reduce the expression of IL-17. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or autoimmune disorders.
Type:
Grant
Filed:
December 16, 2017
Date of Patent:
April 5, 2022
Assignee:
REATA PHARMACEUTICALS, INC.
Inventors:
Xin Jiang, Christopher F. Bender, Melean Visnick, Martha R. Hotema, Zachary S. Sheldon, Chitase Lee, Bradley William Caprathe, Gary Bolton, Brian Kornberg
Abstract: The present invention relates to a compound of the general formula (I). The compounds of formula I are useful for treatment of a cardiac disease, disorder or condition in a mammal.
Abstract: The present disclosure provides certain tetrahydro-1H-cyclopenta[cd]indene compounds that are Hypoxia Inducible Factor 2? (HIF-2?) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of HIF-2?. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Abstract: Dried and or decarboxylated cannabis containing a known composition of cannabinoids is blended with other dried or decarboxylated cannabis of a known composition of cannabinoids and or mixed with other extracts of, isolates of, cannabisor synthetic cannabinoids to achieve a prescribed amount of cannabinoids in the blend. Decarboxylated cannabis is preferentially produced using controlled thin layer decarboxylation. Precision decarboxylation is optionally used to produce a precise pair ratio of acidic to neutral cannabinoid, eg THCA to THC or CBDA to CBD. Further a prescribed or selected terpene profile is mixed and applied to the blend. Once mixed the plant material is suitable for ingestion without further treatment and is dosed appropriately.
Abstract: The invention relates, in certain aspects, to developable forms of certain compounds that are useful to treat and/or prevent EBV infection and related conditions in a subject. The invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.
Type:
Grant
Filed:
May 16, 2019
Date of Patent:
February 8, 2022
Assignee:
The Wistar Institute
Inventors:
Troy E. Messick, Paul M. Lieberman, Garry R. Smith, Arlindo L. Castelhano
Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.
Type:
Grant
Filed:
July 31, 2019
Date of Patent:
February 1, 2022
Assignees:
Cancer Research Technology Limited, The Institute of Cancer Research, Vernalis (R&D) Limited
Inventors:
Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
Abstract: The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
Inventors:
Edward J. Brnardic, Carl A. Brooks, Brian Griffin Lawhorn, Guosen Ye, Linda S. Barton, Brian W. Budzik, Jay M. Matthews, John Jeffrey McAtee, Jaclyn R. Patterson, Joseph E. Pero, Robert Sanchez, Matthew Robert Sender, Lamont Roscoe Terrell, David J. Behm, James V. Thomas