Patents Examined by Brian McDowell
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Patent number: 9975887Abstract: The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R1, R2, R3, R4, R5, Ra, Rb, n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (ROR?t). These compounds prevent, inhibit, or suppress the action of ROR?t and are therefore useful in the treatment of ROR?t mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.Type: GrantFiled: August 2, 2016Date of Patent: May 22, 2018Assignee: GLENMARK PHARMACEUTICALS S.A.Inventors: Sanjib Das, Laxmikant A. Gharat, Rajendra L. Harde, Sandeep Y. Shelke, Shailesh R. Pardeshi, Abraham Thomas, Neelima Khairatkar-Joshi, Daisy M. Shah, Malini Bajpai
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Patent number: 9975859Abstract: Provided is a method for preparing a nitrogen-containing aromatic compound through catalytic pyrolysis from organic materials. The method comprises: feeding organic materials and a catalyst into a reactor, to enable the organic material to undergo reactions in the presence of nitrogen and under heating conditions, so as to generate a reaction system flow containing one or more nitrogen-containing aromatic compounds.Type: GrantFiled: January 28, 2016Date of Patent: May 22, 2018Assignee: University of Science and Technology of ChinaInventors: Ying Zhang, Lujiang Xu, Qian Yao
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Patent number: 9963434Abstract: Compounds of the Formula wherein A, B, C, D, X, Y, Z, R1, R2, R2?, R3 and n are described herein, selectively negatively modulate NMDA receptors containing an NR2A subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.Type: GrantFiled: September 26, 2014Date of Patent: May 8, 2018Assignee: Luc Therapeutics, Inc.Inventors: David R Anderson, Robert A Volkmann
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Patent number: 9951060Abstract: [Problem] To provide a compound which is useful as an active ingredient for a pharmaceutical composition for preventing or treating urine storage dysfunction, voiding dysfunction, lower urinary tract dysfunction, and the like. [Means for Solution] The present inventors have found that a thiazole derivative substituted with pyrazinylcarbonylamino at the 2-position is an excellent muscarinic M3 receptor-positive allosteric modulator and is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, thereby completing the present invention. 2-Acylaminothiazole derivative or a salt thereof of the present invention is expected as an agent for preventing or treating bladder/urinary tract diseases associated with bladder contractions via a muscarinic M3 receptor, for example voiding dysfunction such as underactive bladder.Type: GrantFiled: June 5, 2015Date of Patent: April 24, 2018Assignee: Astellas Pharma Inc.Inventors: Taisuke Takahashi, Takanori Koike, Kenji Negoro, Hiroaki Tanaka, Jun Maeda, Kazuhiro Yokoyama, Hajime Takamatsu
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Patent number: 9938256Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, and Z? have one of the meanings as indicated in the specification or a pharmaceutically acceptable salt thereof, to the use of compounds of formula (I) as a medicament, to pharmaceutical composition comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).Type: GrantFiled: August 19, 2016Date of Patent: April 10, 2018Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Dieter Hamprecht, Joerg Kley
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Patent number: 9938235Abstract: The invention generally relates to compounds of formula (I) with neural protective effect, and preparation and uses thereof. The compounds have multiple mechanisms or functions, for example, inhibition of monoamine oxidase and cholinesterase, scavenging of free radicals, and protection of cells such as nerve cells. The compounds can be used for manufacture of medicaments of cell protection, for prevention and/or treatment of monoamine oxidase, cholinesterase and free radicals related diseases, for example, neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and stroke, and free-radical related diseases such as heart disease, myocardial ischemia, diabetes and other cardiovascular and cerebrovascular diseases.Type: GrantFiled: March 2, 2015Date of Patent: April 10, 2018Inventors: Yuqiang Wang, Moussa B. H. Youdim, Yewei Sun, Zaizun Zhang, Gaoxiao Zhang, Pei Yu, Peng Yi, Ming Lang, Wei Liu
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Patent number: 9889131Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.Type: GrantFiled: February 5, 2016Date of Patent: February 13, 2018Assignee: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Jaime M. Guidry Auvil, Milton L. Brown
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Patent number: 9884845Abstract: There are provided compounds of formula (I) as defined in the specification, which are p38 MAP kinase inhibitors for use as medicaments for the treatment inter alia of inflammatory diseases.Type: GrantFiled: February 13, 2015Date of Patent: February 6, 2018Assignee: Respivert LimitedInventors: Alistair Ian Longshaw, Euan Alexander Fraser Fordyce, Stuart Thomas Onions, John King-Underwood, Jennifer Diane Venable, Iain Walters
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Patent number: 9862685Abstract: The present invention is a compound of the formula or a pharmaceutically acceptable salt thereof. The compounds are useful as HDAC inhibitors.Type: GrantFiled: May 12, 2014Date of Patent: January 9, 2018Assignee: Karus Therapeutics LimitedInventors: Stephen J. Shuttleworth, Cyrille D. Tomassi, Alexander R. L. Cecil, Somhairle MacCormick, William J. Nodes, Franck A. Silva
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Patent number: 9855268Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: GrantFiled: February 10, 2014Date of Patent: January 2, 2018Assignee: MERCK PATENT GMBHInventors: Dieter Dorsch, Guenter Hoelzemann, Michel Calderini, Ansgar Wegener, Oliver Poeschke
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Patent number: 9843002Abstract: A novel organometallic complex having high color purity is provided. The organometallic complex includes a structure which includes iridium and a ligand and is represented by a general formula (G1). The ligand includes a pyrido[2,3-b]indole skeleton and a pyrimidine skeleton bonded to the 3-position of the pyrido[2,3-b]indole skeleton. The 2-position of the pyrido[2,3-b]indole skeleton and the pyrimidine skeleton are each bonded to the iridium. In the general formula (G1), R1 to R9 each independently represent any of hydrogen, a substituted or unsubstituted alkyl group having 1 to 6 carbon atoms, a substituted or unsubstituted aryl group having 6 to 13 carbon atoms, and a substituted or unsubstituted heteroaryl group having 3 to 12 carbon atoms.Type: GrantFiled: October 24, 2016Date of Patent: December 12, 2017Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Tomoya Yamaguchi, Hideko Inoue, Tatsuyoshi Takahashi
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Patent number: 9840479Abstract: The present disclosure provides polyamine-fatty acid derived lipidoids (e.g., compounds of Formula (I) or (II)) and methods of preparing the lipidoids. A described lipidoid includes R—C(?O)—O— moieties (where R is a lipid moiety), which may be hydrolyzed into non-toxic fatty acids. Also provided are compositions including a described lipidoid and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that involve the lipidoids or compositions for delivering an agent to a subject, tissue, or cell and/or for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, and metabolic disorders.Type: GrantFiled: July 1, 2015Date of Patent: December 12, 2017Assignee: Massachusetts Institute of TechnologyInventors: Owen Shea Fenton, Joseph Robert Dorkin, Daniel Griffith Anderson, Rebecca L. McClellan
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Patent number: 9834538Abstract: Provided herein are quinazolinone compounds of formula (I), and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Also provided herein are pharmaceutical compositions comprising the compounds, and methods of use thereof.Type: GrantFiled: January 25, 2017Date of Patent: December 5, 2017Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man
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Patent number: 9834550Abstract: The present invention provides a compound of Formula (I) being capable of modulating the activity of histone lysine demethylase (KDM), pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament. The compound of Formula (I) acts as KDM inhibitor with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to KDM dysregulation.Type: GrantFiled: October 27, 2015Date of Patent: December 5, 2017Assignee: DONG-A ST CO., LTD.Inventors: Myeong-seop Kim, Taesun Park, Taeyoung Yoon, Seung Min Yang, Hae-Sun Kim, Jun Gyu Kim
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Patent number: 9834558Abstract: The present invention relates to novel substituted bridged urea compounds of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding related analogs, pharmaceutical compositions and methods of use thereof. Sirtuin-modulating compounds of the present invention may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders, which include, but are not limited to, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. The present invention also related to compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: November 19, 2014Date of Patent: December 5, 2017Assignee: GLAXOSMITHKLINE LLCInventors: Charles A. Blum, Richard Dana Caldwell, Rebecca Casaubon, Jeremy S. Disch, Ryan Michael Fox, Karsten Koppetsch, William Henry Miller, Pui Yee Ng, Christopher Oalmann, Robert B. Perni, Bruce G. Szczepankiewicz, Brian White
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Patent number: 9828374Abstract: The present invention relates to compounds of formula of formula I wherein R, R1, R2 and L are as described herein, compositions containing compounds of formula I, methods of manufacture of compounds of formula I and methods of treating psychiatric, metabolic, cardiovascular or sleep disorders with compounds of formula I.Type: GrantFiled: February 8, 2017Date of Patent: November 28, 2017Assignee: Hoffmann-La Roche Inc.Inventors: Giuseppe Cecere, Guido Galley, Roger Norcross, Angelique Patiny-Adam, Philippe Pflieger
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Patent number: 9828393Abstract: Silylalkyloxyaryl compounds useful as anti-cancer agents. The compounds and pharmaceutical compositions containing them are particularly useful for the treatment of melanoma, colon, neuroblastoma, bladder, breast, lung, pancreatic, melanoma, sarcoma, lymphoma or gastric cancer.Type: GrantFiled: July 22, 2014Date of Patent: November 28, 2017Assignee: The Regents of the University of Colorado, a Body CorporateInventors: Lajos Gera, Robert S. Hodges, Peter Hegyes
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Patent number: 9828375Abstract: The invention belongs to the technical field of organic synthetic drugs, and particularly relates to a pyrazolopyrimidine derivative and a preparation method and medical uses thereof. The invention provides a new pyrazolopyrimidine derivative mainly having position 4 substituted, i.e., position substituted by Y in formula I. The pyrazolopyrimidine derivative of the invention has a structural formula I as follows: The invention provides a new pyrazolopyrimidine derivative and a simple, efficient and low-cost preparation method thereof. The pyrazolopyrimidine derivative of the invention has good inhibitory activity for multiple kinases, has inhibitory action on multiple solid tumors, leukemia and autoimmune diseases, provides a new effective choice for preparation of kinase inhibitors, medicines for autoimmune diseases, angiogenesis inhibitors and antitumor drugs, and has good application prospect.Type: GrantFiled: March 5, 2013Date of Patent: November 28, 2017Assignee: Guangxi Wuzhou Pharmaceuticals (Group) Co., Ltd.Inventors: Shengyong Yang, Yuquan Wei
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Patent number: 9822120Abstract: The present invention relates to a novel family of protein kinase inhibitors of Formula I: as well as to the processes of preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative, inflammatory, autoimmune or infectious diseases, disorders, or conditions in which protein kinase activity is implicated.Type: GrantFiled: November 20, 2014Date of Patent: November 21, 2017Assignee: Pharmascience Inc.Inventors: Alain Laurent, Yannick Rose
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Patent number: 9815813Abstract: The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4a, R4b, R5a, R5b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.Type: GrantFiled: January 16, 2015Date of Patent: November 14, 2017Assignee: Novartis AGInventors: Zhuoliang Chen, Michael Dore, Jorge Garcia Fortanet, Rajesh Karki, Mitsunori Kato, Matthew J. LaMarche, Lawrence Blas Perez, Sarah Williams, Martin Sendzik