Abstract: The invention is related to an inositol polyphosphate oligo alkyl ether compound, or its pharmaceutically acceptable salt, for use in treatment or prevention of a disease associated with formation of calcium salt crystals.
Type:
Grant
Filed:
June 7, 2021
Date of Patent:
July 25, 2023
Assignees:
ETH Zurich, Universitat Bern
Inventors:
Anna Kletzmayr, Makoto Kuro-o, Hirosaka Hayashi, Mattias E. Ivarsson, Jean-Christophe Leroux
Abstract: The present invention relates to intermediate compounds for the synthesis of novel cannabinoids 1 and 2, synthesized from simple starting materials using a cascade sequence of allylic rearrangement, aromatization and, for tetracyclic cannabinoids, further highly stereoselective and regioselective cyclization. These synthesized cannabinoids can more easily be obtained at high purity levels than cannabinoids isolated or synthesized via known methods. The cannabinoids 2 are obtained containing very low levels of isomeric cannabinoids such as the undesirable ?8-tetrahydrocannabinol. The analogues with variation in aromatic ring substituents, whilst easily synthesized with the new methodology, would be much more difficult to make from any of the components of cannabis oil. Novel compounds of the formulas 3 and 6, useful as intermediates for the synthesis of the cannabinoids of advanced intermediates 4 and 5 as well as cannabinoids of the formulas 1 and 2, are disclosed.
Type:
Grant
Filed:
May 6, 2022
Date of Patent:
June 27, 2023
Assignee:
Bessor Pharma, LLC
Inventors:
Barry A. Berkowitz, Anthony G. Barrett, Daniel Elliott
Abstract: The present invention is directed to bicyclo[4.1.0]heptane pyrrolidine compounds which are agonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
Type:
Grant
Filed:
August 16, 2021
Date of Patent:
June 20, 2023
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Stephane L. Bogen, Dane James Clausen, Deodial Guy Guiadeen, Jinsong Hao, Shishi Lin, Michael T. Rudd, Lan Wei, Li Xiao, Dexi Yang
Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.
Abstract: The present invention relates to the unexpected discovery of novel monomer compounds capable of crosslinking interpenetrating polymer networks (IPNs). In certain embodiments, the monomer compounds of the invention each comprise at least one methacrylate functionality capable of forming polymeric bonds with other methacrylate and vinyl functionalities, and at least one epoxide functionality capable of forming polymeric bonds with epoxide functionalities, amine functionalities, and/or reactive oxygen species.
Type:
Grant
Filed:
August 13, 2019
Date of Patent:
June 6, 2023
Assignees:
Rowan University, The United States of America as represented by the Secretary of the Army
Inventors:
Alexander W. Bassett, Joseph F. Stanzione, III, John J. La Scala
Abstract: The present invention relates to technical field of chemical synthesis of drugs, and provides a preparation method of Macitentan and intermediate compound thereof. Adding THF solution containing compound II and 5-bromo-2-chloropyrimidine slowly into THF solution containing base to react, or adding THF solution containing compound II and THF solution containing 5-bromo-2-chloropyrimidine slowly at the same time into THF solution containing base to react and obtain Macitentan (shown as compound I), wherein the base is selected from sodium hydride, potassium hydride, lithium hydride or lithium bis(trimethylsilyl)amide. The selectivity of the preparation method is very good, which is suitable for industrial production. The obtained product Macitentan has good quality and high yield. And the product compound II also has good quality and high yield, its HPLC purity is up to 99.0%, the content of impurity A is less than 0.20%, the content of impurity B is less than 0.25%.
Abstract: Provided herein are indole compounds that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.
Type:
Grant
Filed:
July 20, 2021
Date of Patent:
June 6, 2023
Assignee:
NIDO BIOSCIENCES, INC.
Inventors:
Bakary-Barry Toure, Mark Andrew Gallop, Paul Andrew Barsanti
Abstract: The present disclosure relates generally to inhibitors of mycobacterial membrane protein MmpL3, compositions comprising the inhibitors, and methods of preparation and use thereof.
Type:
Grant
Filed:
November 20, 2019
Date of Patent:
May 23, 2023
Assignee:
SHANGHAITECH UNIVERSITY
Inventors:
Zihe Rao, Jun Li, Bing Zhang, Haitao Yang
Abstract: The present invention provides small-molecule inhibitors of BMP signaling and compositions and methods for inhibiting BMP signaling. These compounds and compositions may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds and compositions may also be used to treat subjects with Sjögren's syndrome, or diffuse intrinsic pontine glioma (DIPG).
Type:
Grant
Filed:
June 7, 2021
Date of Patent:
May 23, 2023
Assignees:
The Brigham and Women's Hospital, Inc., The United States of America, as Represented by the Secretary, Dept. of Health and Human Services
Inventors:
Paul B. Yu, Wenwei Huang, Philip Edward Sanderson, Jian-Kang Jiang, Khalida Shamim, Wei Zheng, Xiuli Huang, Gregory Tawa, Arthur Lee, Asaf Alimardanov, Junfeng Huang
Abstract: The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.
Abstract: The present invention provides a production method of a 3-cyanopyrrole compound possibly useful as an intermediate for pharmaceutical products. A production method of compound (II) including subjecting compound (I) to a reduction reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst. A production method of compound (III) including subjecting compound (I) to a reduction reaction followed by a cyclization reaction, in which the aforementioned reduction reaction is continuous hydrogenation reaction in a fixed bed reactor filled with a supported metal catalyst.
Type:
Grant
Filed:
June 17, 2021
Date of Patent:
May 16, 2023
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Takashi Ouchi, Giho Goh, Sunmi Kim, Jinsoon Choi, Hunsoo Park
Abstract: The present invention relates to technical field of chemical synthesis of drugs, and provides a preparation method of Macitentan and intermediate compound thereof. Adding THF solution containing compound II and 5-bromo-2-chloropyrimidine slowly into THF solution containing base to react, or adding THF solution containing compound II and THF solution containing 5-bromo-2-chloropyrimidine slowly at the same time into THF solution containing base to react and obtain Macitentan (shown as compound I), wherein the base is selected from sodium hydride, potassium hydride, lithium hydride or lithium bis(trimethylsilyl)amide. The selectivity of the preparation method is very good, which is suitable for industrial production. The obtained product Macitentan has good quality and high yield. And the product compound II also has good quality and high yield, its HPLC purity is up to 99.0%, the content of impurity A is less than 0.20%, the content of impurity B is less than 0.25%.
Abstract: The present invention belongs to the pharmaceutical technical field, and specifically relates to a haloallylamine compound represented by formula I, a pharmaceutically acceptable salt, an ester or a stereoisomer thereof, R1, R2, R3, R4, R5, R6, L1, Cy1, R7 are defined as in the specification; the present invention also relates to pharmaceutical preparations and pharmaceutical compositions containing these compounds, and their use in preventing and/or treating the SSAO/VAP-1 protein-related or SSAO/VAP-1 protein-mediated disease.
Abstract: Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
Type:
Grant
Filed:
November 19, 2021
Date of Patent:
May 9, 2023
Assignee:
ESCIENT PHARMACEUTICALS, INC.
Inventors:
Adam Yeager, Brandon Selfridge, Marcos Sainz, Esther Martinborough, Marcus Boehm, Liming Huang
Abstract: The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
Type:
Grant
Filed:
December 9, 2020
Date of Patent:
May 2, 2023
Assignees:
Massachusetts Institute of Technology, The General Hospital Corporation
Inventors:
Li-Huei Tsai, Stephen J. Haggarty, Debasis Patnaik, Ping-Chieh Pao
Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Type:
Grant
Filed:
February 22, 2021
Date of Patent:
May 2, 2023
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
Abstract: The present disclosure relates generally to antibody-drug conjugates comprising pyrrolo[2, 1-c][1, 4]benzodiazepine (PBD) drug moieties. The present disclosure also relates to methods of using these conjugates, e.g., as therapeutics and/or diagnostics.
Type:
Grant
Filed:
November 27, 2018
Date of Patent:
May 2, 2023
Assignee:
Mersana Therapeutics, Inc.
Inventors:
Joshua D. Thomas, Brian D. Jones, Timothy B. Lowinger, Shuyi Tang, Mao Yin, Aleksandr V. Yurkovetskiy
Abstract: The present disclosure relates to the use of silica-forming peptides (SFPs) Volp1 and Salp1 for protein fusion tags for protein purification, silica formation and self-encapsulation, and controlled release of biomolecules. After preparing a fusion protein containing the Volp1 or Salp1 peptide at the C-terminal of the protein, the adsorption conditions for silica (SiO2) surface were optimized. As a result, a high-purity fusion protein could be purified without an additional tag for purification. The fusion protein containing the silica-forming peptide was self-encapsulated and stably immobilized in the silica matrix through reaction with a silica precursor. The Volp1 and Salp1 peptides showed stronger adsorption ability for silica than the previously known R5 peptide. Using these characteristics, a silica complex wherein two proteins are encapsulated was prepared by mixing the R5 fusion protein with the Volp1 or Salp1 fusion protein.
Type:
Grant
Filed:
February 18, 2020
Date of Patent:
April 25, 2023
Assignee:
Korea University Research and Business Foundation, Sejong Campus
Inventors:
Seung Pil Pack, Mohamed Abdeltawab Abdallah Abdelhamid, Ki Baek Yeo, Mi Ran Ki
Abstract: Compositions of furan based surfactants derived from unsaturated carbon-containing molecules, such as fatty acids, as well as methods for forming furan based surfactants from unsaturated carbon-containing molecules, such as fatty acids, are disclosed herein. These compositions and methods can utilize long-chain (e.g., C14-C26) unsaturated carbon-containing molecules, for instance unsaturated fatty acids such as oleic acid or methyl oleate from soybean oil, to derive oleo-furan surfactants. To facilitate this, certain such embodiments include reaction steps that cleave the reactant molecule (e.g., methyl oleate) at the double bond and subsequently oxidize products to form a carboxylic acid molecule and a dicarboxylic acid molecule. In such embodiments, these two acids can be subsequently acylated with furan and functionalized to form surfactants.
Type:
Grant
Filed:
January 25, 2021
Date of Patent:
April 25, 2023
Assignee:
Sironix Renewables, Inc.
Inventors:
Shawn Eady, Connor Beach, Christoph Krumm
Abstract: The disclosure is directed to, in part, to BCL-2 inhibitors, pharmaceutical compositions comprising the same, as well as methods of their use and preparation.
Type:
Grant
Filed:
April 27, 2021
Date of Patent:
April 11, 2023
Assignee:
Prelude Therapeutics Incorporation
Inventors:
Jincong Zhuo, Andrew Paul Combs, Peng Wei, Jialiang Wang