Abstract: The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where A, U, V, W, X, Y, Z, R1, R2, R3, R4 and R5 have the meanings defined herein. Such compounds are modulators of RXFP1 and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions including heart failure, heart failure with preserved ejection fraction, heart failure with mid-range ejection fraction, heart failure with reduced ejection fraction, chronic kidney disease and acute kidney injury. The specification further relates to compositions comprising such compounds, intermediates useful in processes for preparing such compounds, and processes for preparing such compounds using such intermediates.
Abstract: The present invention relates to the calcium complex of (4RS)(4-carboxy-5,8,11-tris(carboxymethyl)-1-phenyl oxa-5,8,11-triazatridecan-13-oato(5-))pentahydrogen (BOPTA) in the form of a salt, to the process for its preparation and to a formulation comprising said salt.
Type:
Grant
Filed:
December 17, 2020
Date of Patent:
June 6, 2023
Assignee:
BRACCO IMAGING S.P.A.
Inventors:
Andrea Banin, Laura Galimberti, Roberta Napolitano, Roberta Fretta
Abstract: An HDAC6-specific inhibitor (i.e., a compound of Formula I or II) is shown to reduce the pathogenesis associated with polycystic disease. Administration of an HDAC6-specific inhibitor attenuated many of the symptoms characteristic of polycystic liver disease including cyst formation, cyst growth and cholangiocyte proliferation. Treatment with a HDAC6-specific inhibitor also increased the amount of bile duct acetylated tubulin and ?-catenin phosphorylation and/or acetylation while reducing bile duct ?-catenin synthesis. These results demonstrate that HDAC6 is overexpressed in cystic cholangiocytes and that its pharmacological inhibition reduces cholangiocyte proliferation and cyst growth.
Type:
Grant
Filed:
May 14, 2020
Date of Patent:
June 6, 2023
Assignee:
NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS) U.S. GOVERNMENT
Inventors:
Sergio A. Gradilone, Nicholas F. LaRusso
Abstract: The present application relates to a compound which may be useful for mediating NO production and improving L-arginine bioavailability in a subject. Pharmaceutical compositions comprising the compound and methods of using the compound are also provided.
Abstract: The invention relates to an aqueous pharmaceutical composition comprising: a) bilastine or a pharmaceutically acceptable salt or solvate thereof, b) mometasone, or a pharmaceutically acceptable derivative thereof, c) a suspending agent, and d) 2-hydroxypropyl-?-cyclodextrin; wherein the pH of the aqueous pharmaceutical composition is between 3.5 and 5.5, and wherein the content of 2-hydroxypropyl-?-cyclodextrin is less than 8.5% by weight. The invention also relates to said compositions for use in the treatment and/or prevention of a disorder or disease susceptible to amelioration by antagonism of H1 histamine receptor and/or of a corticosteroid-responsive disease through nasal administration. The invention also relates to a process for preparing the aqueous pharmaceutical composition above mentioned.
Type:
Grant
Filed:
October 15, 2018
Date of Patent:
May 9, 2023
Assignee:
FAES FARMA, S.A.
Inventors:
Gonzalo Hernández Herrero, Ana Gonzalo Gorostiza, Neftalí García Domínguez, Arturo Zazpe Arce, Pablo Morán Poladura, Tania González García
Abstract: Nasal formulations of metoclopramide, which remain stable and/or colorless upon storage over a period of time, are provided. Also provided are methods of treating disorders treatable with metoclopramide, comprising administering the nasal solutions to patients in need thereof.
Type:
Grant
Filed:
November 20, 2020
Date of Patent:
April 18, 2023
Assignee:
Evoke Pharma, Inc.
Inventors:
Matthew J. D'Onofrio, David A. Gonyer, Shirish A. Shah, Stuart J. Madden
Abstract: The present disclosure discloses a composition for relieving skin itch or irritation, which contains thymol trimethoxycinnamate or a stereoisomer, salt, hydrate or solvate thereof as an active ingredient, and a method for relieving skin itch or skin irritation by administering the composition to a subject in need of reliving of skin itch or irritation. The composition according to an aspect of the present disclosure has a superior effect of relieving skin itch or skin irritation by inhibiting the voltage-gated sodium channel Nav1.7 without side effects.
Abstract: The present invention relates to a composition comprising ethyl vanillin or a pharmaceutically acceptable salt thereof as an effective ingredient for preventing or treating muscle disease or for improving a muscle function. Having the capability of upregulating the expression of a protein associated with muscle protein synthesis and muscle mass increase in myocytes and downregulating at an mRNA level the expression of an enzyme involved in muscle protein degradation, ethyl vanillin can exhibit effects of muscle differentiation, muscle regeneration, and muscle strengthening through an increase in muscle mass against muscle diseases attributed to muscle function decrease, muscle consumption, or muscle degradation and can suppress sarcopenia. Thus, ethyl vanillin can be used for preventing or treating muscle diseases or for promoting muscle differentiation, muscle regeneration and muscle strengthening, muscle mass increase, or muscle generation or for improving muscle function.
Type:
Grant
Filed:
July 17, 2018
Date of Patent:
February 14, 2023
Assignee:
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY
Abstract: The invention provides compounds for use in inhibiting a microbial alternative oxidase (AOX) and/or cytochrome bc1 complex. The invention extends to the use of such inhibitors in agrochemicals and in pharmaceuticals, for treating microbial infections, including fungal infections.
Type:
Grant
Filed:
September 30, 2020
Date of Patent:
January 31, 2023
Assignee:
AlternOx Scientific Limited
Inventors:
Anthony Lennox Moore, Mary Susan Albury, Luke Edward Young, Catherine Elliott
Abstract: The instant invention is related to a novel solid form of ceftolozane sulfate (the DMAc solvate of ceftolozane sulfate (Form 3)), compositions comprising ceftolozane sulfate DMAc solvate (Form 3), synthesis of Form 3 and an improved crystallization process using Form 3 to prepare ceftolozane sulfate Form 2. Novel compositions also include ceftolozane sulfate solid Form 3 and/or other crystalline and amorphous solid forms of ceftolozane.
Type:
Grant
Filed:
June 1, 2017
Date of Patent:
January 3, 2023
Assignee:
Merck Sharp & Dohme LLC
Inventors:
Kevin Matthew Maloney, Eric M. Sirota, Richard J. Varsolona, Donald R. Gauthier, Jr., Hong Ren
Abstract: The present invention relates to applications of a novel thiazole derivative in treating ulcerative colitis and in the preparation of drugs for treating ulcerative colitis.
Type:
Grant
Filed:
May 17, 2017
Date of Patent:
December 27, 2022
Assignee:
EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY
Abstract: The present disclosure relates to compositions including a fatty acid soap/fatty acid mixture, and methods of use thereof. The compositions include a C5 to C12 fatty acid or mixtures thereof. The compositions show increased activity, e.g., insecticidal, soil removal, antimicrobial activity, at a controlled pH range of about 7.5 to about 9.0.
Type:
Grant
Filed:
March 20, 2018
Date of Patent:
December 27, 2022
Assignee:
Ecolab USA Inc.
Inventors:
Victor Fuk-Pong Man, Yvonne Marie Killeen, Michael Charles DeNoma, Kelly J. Herrera, S. John Barcay, William J. Pattison
Abstract: The disclosure provides a method comprising administering HIF stabilizing small molecule drugs to premature infants, whose survival is dependent upon mechanical ventilation and/or supplemental oxygen, to counteract the pathological effects of hyperoxia on lung development. Data in a mouse model of hyperoxia-induced neonatal lung disease supports a treatment with a HIF stabilizer during high oxygen exposure protects the lung. HIF stabilizers can be administered via various routes, including in an aerosolized state using a ventilator, intravenous, intraperitoneal or subcutaneous injection.
Abstract: Compounds for the treatment of brain cancer are provided herein. Pharmaceutical compositions comprised of those compounds for the treatment of brain cancer are also provided herein.
Type:
Grant
Filed:
May 2, 2019
Date of Patent:
November 22, 2022
Assignee:
ARRAY BIOPHARMA INC.
Inventors:
Patrice A. Lee, Shannon L. Winski, Kevin Koch
Abstract: The present invention provides a compound that have excellent harmful arthropod controlling effects, the compounds being represented by formula (I) [wherein R represents a C1-C6 chain hydrocarbon group etc., X represents a C1-C4 chain hydrocarbon group etc., G represents a C1-C4 chain hydrocarbon group etc., and n is 0, 1, 2, or 3], as well as a composition for controlling harmful arthropod comprising the same, and a method for controlling harmful arthropod comprising applying the same.
Abstract: Disclosed herein are compounds according to Formula I; a pharmaceutical composition including, consisting essentially of, or consisting of: a pharmaceutically acceptable compound of Formula I and a pharmaceutically acceptable carrier, diluent, or excipient; the use of compounds of Formula I in the preparation of a medicament; and a method including administering a pharmaceutical compositions comprising the compound of Formula I to a patient. The compounds, compositions, use, and methods are directed to the treatment of neurological, psychiatric disorders which are characterised by a fundamental disruption of social behaviour, and substance use disorders.
Type:
Grant
Filed:
June 12, 2019
Date of Patent:
November 8, 2022
Assignee:
Kinoxis Therapeutics Pty Ltd
Inventors:
Michael Kassiou, William Jorgensen, Eryn Werry, Tristan Reekie, Michael Bowen, Iain McGregor
Abstract: The present invention relates to co-crystals of tramadol and co-crystal formers selected from NSAIDs/coxibs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
Type:
Grant
Filed:
December 19, 2019
Date of Patent:
October 25, 2022
Assignee:
ESTEVE PHARMACEUTICALS, S.A.
Inventors:
Carlos-Ramón Plata-Salaman, Nicolas Tesson
Abstract: An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea.
Type:
Grant
Filed:
April 20, 2020
Date of Patent:
October 25, 2022
Assignee:
Dow Pharmaceutical Sciences, Inc.
Inventors:
Yunik Chang, Gordon J. Dow, Radhakrishnan Pillai
Abstract: Salts of cytisine have been prepared and incorporated in stable pharmaceutical compositions, including compositions comprising lactose. The salts are prepared by adding acid stock solutions to solutions of cytisine with heating, followed by cooling to ambient temperature. The salts and compositions are indicated in the treatment of nicotine addiction.
Type:
Grant
Filed:
July 24, 2018
Date of Patent:
October 4, 2022
Inventors:
Anthony Clarke, Richard Alistair Balfour Stewart
Abstract: Provided are an oral delivery composition including oxaliplatin, a water-soluble anticancer agent, and a preparation method thereof, including forming an ionic complex with a bile acid derivative, which is an oral absorption promoter, and oxaliplatin, and incorporating it into the inner aqueous phase of a water-in-oil-in-water (w/o/w) multiple nanoemulsions, thereby obtaining the oral delivery composition with improved oral bioavailability of oxaliplatin, a water-soluble anticancer agent, avoiding the inconvenience and problems of injection, improving patient compliance, and reducing medical costs.
Type:
Grant
Filed:
November 30, 2017
Date of Patent:
September 27, 2022
Assignee:
ICURE BNP CO., LTD.
Inventors:
Jin Woo Park, Young Ro Byun, Young Kweon Choi, Kwan Young Chang, Jae Bum Lee