Abstract: Provided in some embodiments are titration packages, kits, and methods of treating pulmonary arterial hypertension comprising prescribing and/or administering to a patient in need thereof 2-(((1r,4r)-4-(((4-chloropbenyl)(pbenyl)carbamoyloxy)methyl)cyclohexyi)methoxy)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, via a titration scheme that comprises the up-titration of Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, over a period of no more than about nine weeks until an optimized dose is administered.
Abstract: The invention provides a compound of formula (I): or a pharmaceutically-acceptable salt thereof, that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such compound, a crystalline form, methods of using such compound to treat inflammatory skin diseases and other diseases, and processes and intermediates useful for preparing such compound.
Type:
Grant
Filed:
March 30, 2021
Date of Patent:
August 23, 2022
Assignee:
THERAVANCE BIOPHARMA R&D IP, LLC
Inventors:
Jennifer Kozak, Ryan Hudson, Gary E. L. Brandt, Robert Murray McKinnell
Abstract: Described herein are embodiments of squarylium compounds for use as filters in light-emitting and/or display devices. One problem of known quarylium dyes is that strong nucleophiles can attack the electron-deficient cyclobutene ring which can lead to a loss of the dye's colour. Another potential drawback with squaraine dyes can be their tendency to form aggregates, which can lead to a substantial broadening of their absorption bands. Use of the present compounds in filters address these problems.
Abstract: The invention provides a method for treating a neurodegenerative disorder in a subject in need of such treatment, comprising administrating to said subject a compound with (substituted phenyl)-propenal moiety.
Abstract: Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
Type:
Grant
Filed:
January 7, 2021
Date of Patent:
August 16, 2022
Assignee:
THE FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
Abstract: The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3?: a C1-C6 alkyl group or the like.
Abstract: The present invention relates to a novel tryptophan hydroxylase inhibitor and a pharmaceutical composition including same, wherein the novel tryptophan hydroxylase inhibitor has an excellent inhibitory effect on TPH1, and thus can be usefully used for the prevention or treatment of disorders, such as metabolic disorders, cancer, digestive or cardiovascular system disorders, related to TPH1 activity. In particular, the novel tryptophan hydroxylase inhibitor has an excellent treatment effect on inflammatory bowel disorders, and thus can be usefully used for the treatment of inflammatory bowel disorder.
Type:
Grant
Filed:
August 24, 2018
Date of Patent:
August 9, 2022
Assignees:
Gwangju Institute of Science and Technolgy, Korea Advanced Institute of Science and Technology, KyungPook National University Industry-Academic Cooperation Foundation, Curacle Co., LTD.
Inventors:
Jin Hee Ahn, Hail Kim, Jaemyoung Suh, In-Kyu Lee, Kwang-eun Kim, Kun-Young Park, Eun Jung Bae, Ko Eun Shong, Suvarna Haus-habhau Pagire, Ajin Lim, Jae-Han Jeon, Haushabhau Shivaji Pagire, Haiying Zhang, Myung-Hwa Kim, Jung-In Pyo
Abstract: Bromine induced lactamization of vinyl acetohydroxamates facilitated syntheses of monocyclic ?-lactams suitable for incorporation of a thiomethyl and extended functionality at the C(4) position. Elaboration of the resulting substituted N-hydroxy-2-azetidinones allowed incorporation of functionalized ?-amino substituents appropriate for enhancement of antibiotic activity. Evaluation of antibacterial activity against a panel of Gram-positive and Gram-negative bacteria revealed structure-activity-relationships (SAR) and identification of potent new monobactam antibiotics. The corresponding bis-catechol conjugate, 42, has excellent activity against Gram-negative bacteria including carbapenemase and carbacephalosporinase producing strains of Acinetobacter baumannii which have been listed by the WHO as being of critical concern worldwide.
Type:
Grant
Filed:
October 2, 2018
Date of Patent:
August 2, 2022
Assignee:
University of Notre Dame du Lac
Inventors:
Marvin J. Miller, Serena Carosso, Rui Liu, Patricia Miller
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