Abstract: The present invention relates to an improved asymmetric synthesis of azaspiro or diazaspiro compound (hereafter referred to as the compound 5, (5A) or (5N)) or their pharmaceutically acceptable salts and derivatives; through the formation of intermediate compounds 4, (4A) or (4N) respectively. The process comprises an unusual substrate specific highly diastereoselective as well as enantio-enriched 1-substituted 2-azaspiro[3.3]heptane or 1-substituted 2-diazaspiro[3.3]heptane compounds with high diastereoselectivity by addition of a cyclobutane carboxylate anion to a Davis-Ellman's imine, followed by reduction and cyclisation resulting in the selective formation of azaspiro or diazaspiro intermediate compound 4, (4A) or (4N); which on subsequently removing the sulfinyl group provides corresponding azaspiro or diazaspiro compound 5, (5A) or (5N) respectively.
Abstract: The present disclosure provides pharmaceutical combinations of orally administered docetaxel and a P-gp inhibitor. The pharmaceutical combinations are suitable for the treatment of cancer in a subject and for reducing or preventing toxicity, hypersensitivity-type infusion reactions, and other negative outcomes resulting from or associated with intravenously administered docetaxel (e.g., Taxotere® or docetaxel formulated with polysorbate 80) therapy in a subject suffering from cancer.
Type:
Grant
Filed:
October 29, 2020
Date of Patent:
July 19, 2022
Assignee:
Athenex HK Innovative Limited
Inventors:
Min-Fun Rudolf Kwan, E. Douglas Kramer, David Lawrence Cutler, Johnson Yiu-Nam Lau, Wing Kai Chan
Abstract: The present disclosure relates to a new salt of escitalopram and its solid state forms, processes for the preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: Described herein is the preparation of carbon phosphonitride pre-polymers that are soluble in organic solvents and can be further thermoset into carbon phosphonitride extended solids (i.e. films, monoliths, etc.) with an approximate empirical formula of C3N3P.
Type:
Grant
Filed:
July 27, 2021
Date of Patent:
July 19, 2022
Assignee:
The Government of the United States of America, as represented by the Secretary of the Navy
Inventors:
Brian L. Chaloux, Albert Epshteyn, Thomas J. Dabrow
Abstract: Disclosed is a method for preventing or treating sleep disorders using TRPV1 receptor antagonist, (R)—N-[1-(3,5-difluoro-4-methanesulfonylamino-phenyl)-ethyl]-3-(2-propyl-6-trifluoromethyl-pyridin-3-yl)-acrylamide. The method of the present invention can effectively and safely prevent or treat sleep disorders accompanying pruritus caused by atopic dermatitis.
Type:
Grant
Filed:
February 28, 2020
Date of Patent:
July 12, 2022
Assignee:
AMOREPACIFIC CORPORATION
Inventors:
Gyeyoung Choi, Hyunjin Nam, Miyoung Park, Kyoungmi Jung, Jihae Lee, Chang Soon Choi, Youngho Park, Jong Hwa Roh, Eunsil Park, Jaehong Park, Kwanghyun Shin, Byoung Young Woo, Kiwha Lee, Wonkyung Cho, Joonho Choi
Abstract: The present invention is directed to the preparation of phthalic anhydride compounds and the intermediate phthalide compounds. In particular, the invention is directed to an improved bio-based route from furanic compounds to phthalic anhydride compounds by reacting furfuryl alcohol (i.e. 2-hydroxymethylfuran) or an analogue thereof having a nucleophilic atom on the 2-methyl, with a dienophile comprising an ?,?-unsaturated carbonyl comprising an ??-leaving group. The inventions further involved preparation of phthalic anhydride compounds, phthalic acid compounds and reduction products of the intermediate phthalide compounds.
Type:
Grant
Filed:
August 29, 2019
Date of Patent:
July 12, 2022
Assignee:
Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO
Inventors:
Marc Crockatt, Johan Urbanus, Pieter Cornelis Antonius Bruijnincx, Christopher Stuart Lancefield, Bart Fölker
Abstract: An eye drop composition for treating glaucoma is disclosed. The eye drop composition includes a prostaglandin analogue, a thickening agent, and a solubilizing agent, wherein the thickening agent is carboxymethylcellulose or a salt thereof, and the solubilizing agent is tyloxapol.
Type:
Grant
Filed:
June 21, 2018
Date of Patent:
July 12, 2022
Assignee:
YS LIFE SCIENCE CO. LTD.
Inventors:
Areum Baek, Youngsik Chung, Hyun Ik Shin, Chang Young Oh, Kee Young Lee
Abstract: The present application relates to new coumarin compounds and their uses as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.
Abstract: An effective therapeutic agent for the M2 channel comprising sulfonylamide or oxabicyclo structures effective for treating amantadine-resistant influenza A infections, and methods of treating amantadine-resistant influenza A infections through administration of the same.
Type:
Grant
Filed:
April 27, 2020
Date of Patent:
June 21, 2022
Assignees:
Thomas Jefferson University, Ramot At Tel-Aviv University LTD.
Inventors:
Nir Ben-Tal, Roger S. Armen, Laurence C. Eisenlohr, Jitendra Belani, Michael Miller, Inbar Fish, Ori Kalid
Abstract: Compounds described herein are inhibitors of retinoic add inducible P450 (CYP26) enzymes, and are useful for treating diseases that are responsive to retinoids. Certain compounds have retinoid activity, are resistant to CYP26-mediated catabolism, and are used for treating diseases that are responsive to retinoids.
Type:
Grant
Filed:
November 26, 2020
Date of Patent:
June 21, 2022
Assignee:
Queen's University at Kingston
Inventors:
Donald Andrew Cameron, Martin Petkovich, Toni Kristian Rantanen, Victor Snieckus, Johnathan Board, Suneel Singh, Ashishkumar Jayantilal Maheta
Abstract: The present disclosure relates to pharmaceutical compositions of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and corresponding methods of treating psoriatic arthritis.
Type:
Grant
Filed:
November 16, 2021
Date of Patent:
June 21, 2022
Assignee:
AbbVie Inc.
Inventors:
Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Ben Klünder, Aileen L. Pangan, Jaclyn Kay Anderson
Abstract: Disclosed are compounds having the formula: wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
Type:
Grant
Filed:
January 25, 2021
Date of Patent:
June 21, 2022
Assignee:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Inventors:
Adam Kenneth Charnley, Gren Z. Wang, Joseph J. Romano
Abstract: A means for treating cardiovascular disease, in particular chronic heart failure, especially in terms of a more specific treatment preventing or minimizing pathological hypertrophic signaling while leaving cardiac contractility largely intact. For this purpose the present invention provides a means for treating cardiovascular disease, in particular chronic heart failure, the means specifically inhibiting or causing inhibition of components of the ?1-AR/cAMP pathway generating cAMP resulting from activation of the ?1-adrenoceptor on the cardiomyocyte cell crest.
Abstract: Described herein are prodrugs of cysteamine and pharmaceutically acceptable salts, solvates, and esters thereof. Also described herein are pharmaceutical compositions comprising prodrugs of cysteamine, or pharmaceutically acceptable salts, solvates, and esters thereof, and methods of treatment comprising administering prodrugs of cysteamine, or pharmaceutically acceptable salts, solvates, and esters thereof.
Abstract: The present invention provides a production method for dicyanocyclohexane, including a step of obtaining dicyanocyclohexane by reacting cyclohexanedicarboxylic acid and/or a salt thereof, or a heated concentrate of an aqueous ammonia solution of cyclohexanedicarboxylic acid with ammonia in a solvent having a boiling point equal to or higher than a reaction temperature.
Abstract: The present disclosure discloses a rosin-based small molecular weight hydrogelator and an application thereof, and belongs to the fields of supramolecular chemistry, surfactant science and chemical utilization of rosin. The rosin-based small molecular hydrogel of the present disclosure can gel water at a very low concentration, and the critical gelling concentration is only 0.176 wt %. On average, each gelling agent molecule can hold 13,889 water molecules, which exhibits extremely high gel efficiency and the formed small molecular hydrogel also exhibits extremely high stability. This small molecule hydrogel is derived from the natural product rosin and has a mild nature. It can be used in the fields of drug sustained-release, tissue engineering, daily chemicals, medicine and so on.
Type:
Grant
Filed:
March 27, 2020
Date of Patent:
June 7, 2022
Assignee:
Jiangnan University
Inventors:
Binglei Song, Tingting Yan, Danping Wang, Zhenggang Cui
Abstract: A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic ?-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.
Type:
Grant
Filed:
December 22, 2020
Date of Patent:
May 31, 2022
Assignee:
MANNKIND CORP.
Inventors:
John J. Freeman, Otto Phanstiel, William Elliot Bay, Kelly Sullivan Kraft
Abstract: The present invention provides dibenzylamine salt of Lifitegrast (XV), and diphenylamine salt of Lifitegrast (XVI) and the use of the above salts in the purification process of Lifitegrast (I). The present invention relates to a process for the preparation of Lifitegrast (I).
Abstract: Provided herein are piperazine carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL. Furthermore, the subject compounds and compositions are useful for the treatment of pain.
Type:
Grant
Filed:
May 14, 2019
Date of Patent:
May 17, 2022
Assignee:
H. LUNDBECK A/S
Inventors:
Cheryl A. Grice, Daniel J. Buzard, Michael B. Shaghafi