Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A, X, Y, Z, R1, R2a, R2b and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
Abstract: Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, and G, are defined herein.
Type:
Grant
Filed:
June 13, 2019
Date of Patent:
June 22, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Tianbao Lu, Peter J. Connolly, Maxwell David Cummings, Joseph Kent Barbay, Kevin D. Kreutter, Tongfei Wu, Gaston Stanislas Marcella Diels, Jan Willem Thuring, Ulrike Philippar, James Patrick Edwards, Fang Shen
Abstract: The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-?-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.
Type:
Grant
Filed:
June 17, 2019
Date of Patent:
June 15, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Steven Goldberg, Connor L. Martin, Elizabeth G. Fennema, Ronald L. Wolin, Anne M. Fourie, Xiaohua Xue
Abstract: The present disclosure relates to fused N-arylsulfonamidyl-thienoisoquinoline compounds, derivatives and pharmaceutical compositions thereof, and methods and uses in inhibiting cancer cell growth, along with a supplemental anti-cancer agent. Centrosome targeting and microtubule depolymerisation are attractive in designing the present chemotherapeutic compounds. The various diseases and conditions treated include various types of cell cancers, and in vitro inhibition.
Abstract: In one aspect, compounds and compositions that modulate a bromodomain and methods of making and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with inhibition of a bromodomain such as, for example, cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Type:
Grant
Filed:
December 12, 2017
Date of Patent:
June 8, 2021
Assignee:
St. Jude Children's Research Hospital
Inventors:
R. Kip Guy, P. Jake Slavish, William Robert Shadrick, Brandon M. Young, Vincent A. Boyd, Nagakumar Bharatham, Jeanine E. Price, Anang Shelat
Abstract: This application relates to compounds prepared from cosmetically acceptable ingredients, methods of preparation thereof, and use thereof. Compounds are of formula (I) U—C—B, or salts thereof, wherein U, C and B are moieties of cosmetically acceptable ingredients U?, C? and B?. In living tissues, the compounds can release at least one of U?, C? and B?. The bond between C and U and/or between C and B is labile in living tissues. In particular, the compounds comprise moieties derived from salicylic acid, retinol and retinoic acid or nicotinic acid.
Abstract: Metal complexes comprising a compound of general formula (I) and at least one metal ion, for use in the treatment of diseases related to the accumulation of intracellular deposits and/or diseases related to defective autophagy and/or defective proteasome activity is disclosed. Compositions comprising said metal complexes comprising a compound of general formula (I) and at least one metal ion, for use in the treatment of diseases related to the accumulation of intracellular deposits and/or diseases related to defective autophagy and/or defective proteasome activity are also disclosed.
Type:
Grant
Filed:
July 3, 2018
Date of Patent:
May 25, 2021
Assignee:
BIONOS BIOTECH, S.L.
Inventors:
José Luis Mullor Sanjosé, Rafael Vázquez Manrique, David González Fernández
Abstract: The invention relates to pyrazole derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to HbS modulators of formula (I) or tautomers thereof, or pharmaceutically acceptable salts of said modulators or tautomers thereof, wherein X, Y, R2 and R3 are as defined in the description. HbS modulators are potentially useful in the treatment of a wide range of disorders, including sickle cell disease (SCD).
Type:
Grant
Filed:
November 26, 2019
Date of Patent:
May 25, 2021
Assignee:
Pfizer Inc.
Inventors:
Ariamala Gopalsamy, Arjun Venkat Narayanan, Agustin Casimiro-Garcia, Chulho Choi, David Hepworth, David Walter Piotrowski, Hatice Gizem Yayla, Jayasankar Jasti, Lee Richard Roberts, Lyn Howard Jones, Mihir Dineshkumar Parikh, Ming Zhu Chen, Olugbeminiyi Omezia Fadeyi, Ralph Pelton Robinson, Jr., Robert Lee Dow, Shawn Cabral
Abstract: The disclosure relates to compounds of formula (I), which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, and related diseases.
Type:
Grant
Filed:
June 8, 2018
Date of Patent:
May 18, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Pravin Sudhakar Shirude, Amit Kumar Chattopadhyay, Chandrasekhar Rachamreddy, Nicholas R. Wurtz, Ellen K. Kick
Abstract: The present invention relates to quinazolinones and related compounds which are inhibitors of PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.
Type:
Grant
Filed:
January 6, 2020
Date of Patent:
May 18, 2021
Assignee:
Ribon Therapeutics Inc.
Inventors:
Laurie B. Schenkel, Melissa Marie Vasbinder, Kevin Wayne Kuntz, Kerren Kalai Swinger
Abstract: Disclosed is a compound, prepared by extracting and separating from Limax. Also disclosed is a method for extracting and separating the compound, which is simple and easy to operate. The compound has sedative and hypnotic effects, and has significant effects on physiological or psychological dependent detoxification or detoxication. It has potential application value for preparing detoxification or detoxication drugs, and provides new ideas for the further development of detoxification drugs.
Abstract: The present application relates to certain substituted imidazole compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating pain, musculoskeletal inflammation, neuroinflammatory disorders, airway inflammation, itch, dermatitis, colitis and related conditions.
Type:
Grant
Filed:
December 27, 2019
Date of Patent:
May 4, 2021
Assignee:
Heptares Therapeutics Limited
Inventors:
John Graham Cumming, Frank Xinhe Wu, Karl Henrik Edman, Hongming Chen, Dean Gordon Brown, Roland Werner Burli, Shawn Donald Johnstone, Giles Albert Brown, Benjamin Gerald Tehan, Barry John Teobald, Miles Stuart Congreve
Abstract: Provided are compounds of the formula (I) which are suitable for controlling animal pests, including arthropods and in particular insects, arachnids and nematodes, and in which the structural elements R1, p, T and G have the meanings given in the description, as are processes for their preparation and their use as insecticides.
Type:
Grant
Filed:
April 16, 2018
Date of Patent:
May 4, 2021
Assignee:
BAYER AKTIENGESELLSCHAFT
Inventors:
Markus Heil, Laura Hoffmeister, Matthew Webber, Kerstin Ilg, Ulrich Goergens, Andreas Turberg
Abstract: A manufacturing method of a rhodamine dye oligomer, a solid color material, and a liquid crystal display device are provided. By oligomerization of rhodamine dyes, monodispersion of rhodamine dyes can be achieved, preventing the enhanced shoulder peak caused by aggregation of rhodamine dye molecules, Meanwhile, the purification of color gamut is achieved, and the thermal stability of rhodamine dyes is increased, thereby meeting the need of liquid crystal display devices. Moreover, applying the rhodamine dye oligomer to the solid color material and fabricating the solid color film for application in the liquid crystal display devices can prevent a great loss of brightness of display devices.
Type:
Grant
Filed:
November 13, 2019
Date of Patent:
April 27, 2021
Assignee:
TCL CHINA STAR OPTOELECTRONICS TECHNOLOGY CO., LTD.
Abstract: The invention provides compounds that inhibit FTO (fat mass and obesity), including pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof, particularly obesity, with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
Type:
Grant
Filed:
January 12, 2020
Date of Patent:
April 27, 2021
Assignee:
National Institute of Biological Sciences, Beijing
Abstract: Methods of making low odor choline salts of an organic compound, for example, choline ellagate compound(s), and uses and formulations thereof.
Abstract: 2-((1r,4r)-4-(imidazo[4,5-d]pyrrolo[2,3-b]pyridin-1(6H)-yl)cyclohexyl)acetonitrile compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them including methods for treating disease states, disorders, and conditions mediated by JAK, such as inflammatory bowel disease.
Type:
Grant
Filed:
December 15, 2017
Date of Patent:
April 20, 2021
Assignee:
Janssen Pharmaceutica NV
Inventors:
Genesis M. Bacani, Wenying Chai, Tatiana Koudriakova, Paul J. Krawczuk, Kevin D. Kreutter, Kristi Leonard, Michele C. Rizzolio, Mark Seierstad, Russell C. Smith, Mark S. Tichenor, Jennifer D. Venable, Aihua Wang
Abstract: The present invention is directed to 5-(pyridine-3-yl)oxaxole compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. 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 M4 muscarinic acetylcholine 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 M4 muscarinic acetylcholine receptors are involved.
Inventors:
Jianming Bao, Timothy J. Henderson, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Meng Na, Michael T. Rudd, David M. Tellers, Ling Tong