Patents Issued in May 15, 2018
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Patent number: 9969702Abstract: A novel compound excellent in heat resistance, resistance to volatilization, and compatibility with a resin component and useful as a UV absorber and a synthetic resin composition containing the compound are provided. Specifically provided are a triazine compound of general formula (1), preferably general formula (2) and a synthetic resin composition containing 0.001 to 20 parts by mass of the compound per 100 parts by mass of a synthetic resin. The details of formulae (1) and (2) are as defined in the description.Type: GrantFiled: December 1, 2015Date of Patent: May 15, 2018Assignee: ADEKA CORPORATIONInventors: Yosuke Ishima, Mio Tanabe, Masahiro Oishi, Takashi Mutou
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Patent number: 9969703Abstract: The present invention discloses a triazine-containing photocurable resin and a preparation method thereof. The preparation method of the resin comprises the following steps of: (1) Dissolving the hexamethylolmelamine the unsaturated fatty acids and a catalyst in a solvent, keeping a reaction going, separating and extracting the reaction product after the reaction ends, obtaining triazine-containing fatty acid ester; (2) adding 50 wt % hydrogen peroxide, a catalyst and a solvent, namely methylbenzene, into the triazine-containing fatty acid ester prepared in step (1), keeping a reaction going, obtaining triazine-containing fatty acid ester epoxy resin; (3) adding a polymerization inhibitor and a catalyst into acrylic acid, dropping the triazine-containing fatty acid ester epoxy resin prepared in step (2), keeping a reaction going, and obtaining the triazine-containing photocurable resin.Type: GrantFiled: January 20, 2016Date of Patent: May 15, 2018Assignee: JIANGNAN UNIVERSITYInventors: Ren Liu, Xiaopeng Zhang, Zhiquan Li, Jingcheng Liu, Jing Luo, Xiaoya Liu
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Patent number: 9969704Abstract: A process for preparing materials derived from sugar alcohols such that the dehydration products exhibit better accountability and improved color to water-clear or near water-white appearance is described. In particular, the process involves employing a reducing Brnsted acid (e.g., phosphonic acid) for the catalysis of sugar alcohols to their corresponding dehydrated-cyclized products.Type: GrantFiled: November 19, 2014Date of Patent: May 15, 2018Assignee: Archer Daniels Midland CompanyInventors: Kenneth Stensrud, Erik Hagberg
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Patent number: 9969705Abstract: A fused heterocyclic compound having an enteropeptidase inhibitory action and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided. Specifically, a compound represented by the following formula (I): wherein each symbol is as defined herein, or a salt thereof and use of the compound as a medicament for treatment or prophylaxis of obesity, diabetes mellitus, etc., are provided.Type: GrantFiled: February 12, 2015Date of Patent: May 15, 2018Assignee: Takeda Pharmaceutical Company LimitedInventors: Minoru Sasaki, Keiko Kakegawa, Fumiaki Kikuchi, Zenichi Ikeda, Yoichi Nishikawa
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Patent number: 9969706Abstract: An improved method is described for making single isomers of synthetic benzoprostacyclin analog compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.Type: GrantFiled: February 23, 2017Date of Patent: May 15, 2018Assignee: Lung Biotechnology PBCInventors: Vijay Sharma, Hitesh Batra, Sudersan Tuladhar
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Patent number: 9969707Abstract: The present document describes a method for extracting anthocyanin derivatives from a plant source. The method comprises the step of separating a homogenized extract of plant source in a polar acidified solvent for obtaining a residual solid, and a filtrate mixed with the acidified polar solvent. The separation includes a coarse filtration done by centrifugation of the plant source extract, by a filtration with a first filter having a pore size of about 100 ?m, and a fine filtration is done using a second filter having a pore size of about 10 ?m. Then, the filtrate mixed with the acidified polar solvent is evaporated for substantially separating the acidified polar solvent from the filtrate to obtain a semi-solid extract of anthocyanin derivatives.Type: GrantFiled: December 14, 2012Date of Patent: May 15, 2018Inventors: Sylvain Savard, André Tremblay, Michel Arsenault
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Patent number: 9969708Abstract: The present invention relates to a method for preparing a compound of the formula (I) with a specific definition of the substituent R3 a mixture and also a corresponding application/use.Type: GrantFiled: August 10, 2015Date of Patent: May 15, 2018Assignee: Construction Research & Technology, GmbHInventors: Nicolas Vautravers, Joaquim Henrique Teles, Heimo Woelfle, Markus Dierker, Dominik Ohlmann
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Patent number: 9969709Abstract: [Problem] To provide a compound which is useful as an agent for preventing and/or treating kidney diseases. [Means for Solution] The present inventors have studied compounds having a trypsin inhibitory activity, and have confirmed that a guanidinobenzoic acid ester compound has a trypsin inhibitory activity, thereby completing the present invention. The guanidinobenzoic acid ester compound of the present invention can be used as an agent for preventing and/or treating kidney diseases (for example, chronic kidney disease, acute glomerulonephritis, acute kidney injury, and the like) as an agent which will substitute low-protein diet therapy, and/or as an agent for preventing and/or treating trypsin-related diseases (for example, chronic pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like).Type: GrantFiled: March 13, 2014Date of Patent: May 15, 2018Assignee: Takeda Pharmaceutical Company LimitedInventors: Jiro Fujiyasu, Toru Asano, Susumu Yamaki, Osamu Kaneko, Yuka Koike, Tomoyoshi Imaizumi, Yasuharu Urano, Tomohki Satou, Satoshi Sasamura
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Patent number: 9969710Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.Type: GrantFiled: September 16, 2016Date of Patent: May 15, 2018Assignee: Merck Patent GmbHInventors: Catherine Jorand-Lebrun, Ruoxi Lan, Austin Chen, Ryan C. Clark
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Patent number: 9969711Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: GrantFiled: October 14, 2016Date of Patent: May 15, 2018Assignee: OPKO Health, Inc.Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
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Patent number: 9969712Abstract: Provided are processes for the preparation of isotopologues of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 2, 2017Date of Patent: May 15, 2018Assignee: Celgene CorporationInventor: John Fitzgerald Traverse
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Patent number: 9969713Abstract: Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed.Type: GrantFiled: August 7, 2017Date of Patent: May 15, 2018Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Benjamin M. Cohen, Ying Li, Jean Xu, William W. Leong
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Patent number: 9969714Abstract: The present invention provides compounds of Formula 1, or a pharmaceutically acceptable salts, thereof, where R, X, A, E, and G are as described herein, methods of preparing the compounds, and use of the compounds to treat pain and/or inflammation.Type: GrantFiled: October 22, 2015Date of Patent: May 15, 2018Assignee: Eli Lilly and CompanyInventors: Matthew Joseph Fisher, Steven Lee Kuklish, Katherine Marie Partridge, Jeremy Schulenburg York
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Patent number: 9969715Abstract: The present invention relates to a compound of formula (I): wherein A and A? independently represent a phenylene group or a pyridylene group; R2 is a hydrogen atom or a (C1-C4)alkyl group; R3 is a 2-pyridyl group, 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, a 4-pyrimidinyl group or a 5-pyrimidinyl group; R4 is a carbonyl group or a sulfonyl group; and R5 is a —NH—(CH2)a—NR6R7 group or a 4-methylpiperazinyl group, with a being an integer from 1 to 4, R6 and R7 representing independently a (C1-C4)alkyl group, or R6 and R7 together with the nitrogen atom to which they are linked forming a heterocycle group which is chosen among a 4-methylpiperazinyl group, a morpholino group, a pyrrolidinyl group and a piperidino group; or any one of its pharmaceutically acceptable salt.Type: GrantFiled: September 30, 2013Date of Patent: May 15, 2018Assignees: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIERInventors: Pierre Roux, Florence Mahuteau, Romain Najman, Gilles Gadea, Jamal Tazi, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
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Patent number: 9969716Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: GrantFiled: August 15, 2014Date of Patent: May 15, 2018Assignee: Constellation Pharmaceuticals, Inc.Inventors: Brian K. Albrecht, James Edmund Audia, Les A. Dakin, Martin Duplessis, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
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Patent number: 9969717Abstract: The present invention relates to a process for preparing substituted anthranilic acid derivatives of the formula (I) in which R1, R2, R3 and R4 are each as defined in the description, by conversion of compounds of the general formula (IV) in the presence of a palladium catalyst and carbon monoxide. The present invention likewise relates to compounds of the general formula (IV).Type: GrantFiled: April 20, 2017Date of Patent: May 15, 2018Assignee: Bayer Intellectual Property GmbHInventors: Thomas Himmler, Sergii Pazenok, Frank Volz, Norbert Lui
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Patent number: 9969718Abstract: Disclosed is an intermediate of bemaciclib (also referred to as abemaciclib) having a structure of Formula II, and preparation methods therefor. The preparation methods may comprise condensation, amidine reaction, cyclization and/or other unit reactions. Bemaciclib is obtained through a guanidination reaction and a cyclization reaction using the bemaciclib intermediate disclosed herein as a starting material. starting materials for the preparation methods disclosed herein are easily available, the procedures are simple, and the preparation methods are economical, environmentally friendly and suitable for industrial production.Type: GrantFiled: July 7, 2017Date of Patent: May 15, 2018Assignee: SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.Inventor: Xuenong Xu
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Patent number: 9969719Abstract: Disclosed is a substituted 2H-pyrazole derivative serving as a selective CDK4/6 inhibitor. Specifically, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt thereof which serves as a selective CDK4/6 inhibitor.Type: GrantFiled: March 10, 2016Date of Patent: May 15, 2018Assignees: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., MEDSHINE DISCOVERY INC.Inventors: Charles Z. Ding, Shuhui Chen, Baoping Zhao, Zhaobing Xu, Yingchun Liu, Ruibin Lin, Fei Wang, Jian Li
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Patent number: 9969720Abstract: This invention relates to compounds, as defined in the specification and as represented by the compound of formula (I): that are useful in the treatment of mycoses, to compositions containing them and to their use in therapy.Type: GrantFiled: November 9, 2016Date of Patent: May 15, 2018Assignee: PULMOCIDE LIMITEDInventors: Thomas Christopher Colley, Kazuhiro Ito, Peter Strong, Mihiro Sunose, Matthew McConville
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Patent number: 9969721Abstract: The present invention relates to an improved process for the preparation of vilazodone Hydrochloride and a process for preparation of novel pure amorphous form of vilazodone hydrochloride.Type: GrantFiled: April 5, 2013Date of Patent: May 15, 2018Assignee: Alembic Pharmaceuticals LimitedInventors: Venkat Raman Jayaraman, Dhiraj Rathod, Irfan Vohra, Vinayak Bhujade, Viral Modi, Mayur Budh, Ojas Gandhi
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Patent number: 9969722Abstract: The present disclosure relates to salts and polymorphs of aminoalkylfumagillol carbamates (e.g., fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate benzenesulfonic acid salt and fumagill-6-yl N-(trans-4-aminocyclohexyl)carbamate hydroxynaphthoic acid salt). The polymorphs are characterized by X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis, among other methods. The polymorphs and salts can be used as intermediates in the production of fumagillol derivatives (e.g., polymer-conjugated fumagillol derivatives) as well as therapeutic agents for the treatment of various diseases and conditions such as cancer.Type: GrantFiled: December 9, 2016Date of Patent: May 15, 2018Assignee: SynDevRx, Inc.Inventor: John S. Petersen
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Patent number: 9969723Abstract: The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs.Type: GrantFiled: October 1, 2015Date of Patent: May 15, 2018Assignee: HYUNDAI PHARM CO., LTDInventors: Jin Yang, Jin Woong Kim, Han Kyu Lee, Jae Hyun Kim, Chang Mo Son, kyu hwan Lee, Hyung-Ho Choi, daehoon Kim, Tae-Young Ha, Jaekeol Rhee
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Patent number: 9969724Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: GrantFiled: April 10, 2015Date of Patent: May 15, 2018Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.Inventors: Isao Sakurada, Tomokazu Hirabayashi, Yoshitaka Maeda, Hiroshi Nagasue, Takashi Mizuno, Jiayi Xu, Ting Zhang, Cameron Smith, Dann Parker
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Patent number: 9969725Abstract: The invention is directed to pharmaceutically acceptable salts of suvorexant, which is an antagonist of orexin receptors. The pharmaceutically acceptable salts of suvorexant are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is further directed to pharmaceutical compositions comprising pharmaceutically acceptable salts of suvorexant.Type: GrantFiled: April 16, 2015Date of Patent: May 15, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Michael McNevin, Sachin Lohani
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Patent number: 9969726Abstract: Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.Type: GrantFiled: June 9, 2015Date of Patent: May 15, 2018Assignee: SANFORD-BURNHAM MEDICAL RESEARCH INSTITUTEInventors: Nicholas David Peter Cosford, Dhanya Raveendra-Panickar, Douglas J. Sheffler
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Patent number: 9969727Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: January 5, 2016Date of Patent: May 15, 2018Assignee: Array BioPharma Inc.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunawardana, Peter J. Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Patent number: 9969728Abstract: A series of substituted 5,6,7,8-tetrahydroimidazo[1,2-?]pyridine derivatives, being potent modulators of human TNF? activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: December 8, 2014Date of Patent: May 15, 2018Assignee: UCB BIOPHARMA SPRLInventors: Sabine Defays, Jag Paul Heer, Victoria Elizabeth Jackson, James Andrew Johnson, Boris Kroeplien, John Robert Porter
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Patent number: 9969729Abstract: A series of substituted 1H imidazo[4,5-b]pyridine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.Type: GrantFiled: December 8, 2014Date of Patent: May 15, 2018Assignee: UCB BIOPHARMA SPRLInventors: Victoria Elizabeth Jackson, Fabien Claude Lecomte, John Robert Porter
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Patent number: 9969730Abstract: Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.Type: GrantFiled: September 16, 2016Date of Patent: May 15, 2018Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Anantha Sudhakar, Jeff Jacobs, Ahmad Hashash, Sean Ritchie, Hengqin Cheng
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Patent number: 9969731Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.Type: GrantFiled: December 22, 2016Date of Patent: May 15, 2018Assignee: Lupin LimitedInventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
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Patent number: 9969732Abstract: Described herein are tetrahydroisoquinoline compounds with estrogen receptor modulation activity or function having the Formula I structure: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituent and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.Type: GrantFiled: April 7, 2017Date of Patent: May 15, 2018Assignee: Genentech, Inc.Inventors: Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Maia Vinogradova, Xiaojing Wang, Jason Zbieg, Birong Zhang, Tao Wang
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Patent number: 9969734Abstract: A process for making certain spiroheterocyclic pyrrolidine dione derivatives.Type: GrantFiled: July 11, 2014Date of Patent: May 15, 2018Assignee: Syngenta Participations AGInventors: Edouard Godineau, Tomas Smejkal, Sophie Pelletier, Michel Muehlebach, Regis Jean Georges Mondiere, Helmars Smits, Jochen Weckesser, Alan James Robinson
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Patent number: 9969735Abstract: Processes are described for the preparation of tricyclic lactam compound of Formula (I), having the structure and intermediates useful for the preparation of (I).Type: GrantFiled: July 18, 2017Date of Patent: May 15, 2018Assignee: GENENTECH, INC.Inventors: Ngiap-Kie Lim, Haiming Zhang, Chong Han
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Patent number: 9969736Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.Type: GrantFiled: June 14, 2017Date of Patent: May 15, 2018Assignee: Hydra Biosciences, Inc.Inventors: Bertrand L. Chenard, Randall J. Gallaschun
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Patent number: 9969737Abstract: Chromogenic or fluorescent carbapenems according to formula I, wherein Ar is a mono or disubstituted carbocyclic aromatic group or an optionally mono or disubstituted heterocyclic aromatic group, are useful compounds for the detection of bacterial carbapenemase.Type: GrantFiled: February 29, 2016Date of Patent: May 15, 2018Assignee: Hans Rudolf PfaendlerInventor: Hans R. Pfaendler
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Patent number: 9969738Abstract: Novel compounds of Formula I and their use in therapeutic treatments.Type: GrantFiled: March 28, 2014Date of Patent: May 15, 2018Assignee: OGEDA SAInventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
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Patent number: 9969739Abstract: The present invention relates to a compound of general Formula (VIII), the compound having a bowl-shaped conformation, its formation and its use in asymmetric catalysis. In Formula (VIII), M is a metal selected from the group consisting of Group 1 to Group 14 metals, lanthanides and actinides; R is one of —COOR3, —R4COOR3, —R4CHO, —R4COR3, —R4CONR5R6, —R4COX, —R4OP(?O)(OH)2, —R4P(?O)(OH)2), —R4C(O)C(R3)CR5R6 and R4CO2C(R3)O, wherein R1, R2, R3, R4, R5 and R6 are as defined herein.Type: GrantFiled: October 30, 2015Date of Patent: May 15, 2018Assignee: Nanyang Technological UniversityInventors: Teck Peng Loh, Jian Xiao
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Patent number: 9969740Abstract: The present invention relates to solid state forms of a p-toluenesulfonic acid salt (PTSA) of the selective PI3K delta inhibitor (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one (TGR-1202). The present invention also relates to methods of preparing the same, pharmaceutical compositions containing them, and methods of treating a PI3K kinase mediated disease or disorder, such as cancer, by administering the same.Type: GrantFiled: May 26, 2015Date of Patent: May 15, 2018Assignee: RHIZEN PHARMACEUTICALS SAInventor: Swaroop K. Vakkalanka
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Patent number: 9969741Abstract: The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3 and R4 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.Type: GrantFiled: June 17, 2015Date of Patent: May 15, 2018Assignee: MASARYKOVA UNIVERZITAInventors: Jiri Damborsky, Fedor Nikulenkov, Alexandra Sisakova, Stepan Havel, Lumir Krejci, Benoit Carbain, Jan Brezovsky, Lukas Daniel, Kamil Paruch
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Patent number: 9969742Abstract: The present invention provides imidazotriazinone compounds which are inhibitors of phosphodiesterase 9 and pharmaceutically acceptable salt thereof. The present invention further provides processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of PDE9 associated diseases or disorders in mammals, including humans.Type: GrantFiled: December 21, 2016Date of Patent: May 15, 2018Assignee: Ironwood Pharmaceuticals, Inc.Inventors: Matthew Gregory Bursavich, Andrew J. McRiner, Amy Ripka, Gideon Shapiro
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Patent number: 9969743Abstract: Provided are compounds represented by the formula: In which: Y is an unbranched, saturated or unsaturated hydrocarbon chain with 2-5 hydrocarbon atoms R1=aryl R2=NR3R4 wherein R3 and R4 together form a heterocycle or R2=4-substitutedcyclohexyl, 1-substitutedpiperidine-4-yl or imidazo(1,2-a)azine-2-yl when Y is as defined above and R1 is a heterocycle other than benzothiophene pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, and mixtures thereof. The compounds can be used for treating a patient suffering from a condition that is capable of treatment with a partial agonist or antagonist of the dopamine D2/D3 receptors.Type: GrantFiled: March 20, 2017Date of Patent: May 15, 2018Assignee: SOUTHERN RESEARCH INSTITUTEInventor: Subramaniam Ananthan
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Patent number: 9969744Abstract: Novel compounds for use in cognition improvement It relates to certain compounds having a polycyclic structure and a —(C?O)NRaRb moiety, wherein the polycyclic structure comprises at least three ring systems, wherein one ring system is a polycyclic ring system comprising from 2 to 4 rings; at least one ring is an aromatic ring; and wherein the structure comprises at least 3 nitrogen atoms and 1 oxygen atom. It also relates to pharmaceutical compositions containing them, and to their use in medicine, in particular in the treatment and/or prevention of neurological disorders coursing with a cognition deficit or impairment, or neurode-generative diseases.Type: GrantFiled: August 3, 2015Date of Patent: May 15, 2018Assignee: FUNDACIÓN LA INVESTIGACIÓN MÉDICA APLICADAInventors: María del Mar Cuadrado Tejedor, Ana María García Osta, Julen Oyarzabal Santamarina, Maria Obdulia Rabal Gracia, Juan Antonio Sánchez Arias, Ana Ugarte Baztán
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Patent number: 9969745Abstract: Novel compounds of Formula I methods of manufacturing the compounds and their use in therapeutic treatments are presented.Type: GrantFiled: November 9, 2017Date of Patent: May 15, 2018Assignee: OGEDA SAInventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
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Patent number: 9969746Abstract: The present invention relates to opioid compounds, especially to C14 esters and ethers of naltrexone and analogs thereof. The present invention also relates to compositions, methods and medical uses that employ such compounds. More specifically, the present invention pertains to compounds of formula: and to their use in the treatment of diseases and disorders including pain, hyperalgesia, addiction, substance abuse disorders, stress, anorexia, anxiety, depression, cough, asthma, hypertension, gastrointestinal motility disorder, water retention, cognitive disorders, and locomotor disorders.Type: GrantFiled: December 5, 2014Date of Patent: May 15, 2018Assignee: The University of BathInventors: John Lewis, Stephen Husbands, Lawrence Toll
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Patent number: 9969747Abstract: The present disclosure relates to a crystalline form of 2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide, which is useful as an inhibitor of bromodomain-containing proteins. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline form and methods of using said compositions in the treatment of various disorders.Type: GrantFiled: June 18, 2015Date of Patent: May 15, 2018Assignee: Constellation Pharmaceuticals, Inc.Inventor: Michael L. Hall
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Patent number: 9969748Abstract: A series of fused bicyclic heteroaromatic derivatives of formula (IA) or (IB), as defined herein, being selective inhibitors of phosphatidylinositol-4-kinase III? (PI4KIII?) activity, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases and malaria; and organ and cell transplant rejection.Type: GrantFiled: June 11, 2015Date of Patent: May 15, 2018Assignees: UCB Biopharma SPRL, Katholieke Universiteit Leuven, K.U. Leuven R&DInventors: Daniel James Ford, Qiuya Huang, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
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Patent number: 9969749Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.Type: GrantFiled: September 25, 2015Date of Patent: May 15, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brian M. Andresen, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. MacLean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Luis Torres
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Patent number: 9969750Abstract: A process for preparing a compound shown by formula (W6): wherein each Hal is independently chloro or bromo, using a novel process for preparing a pyridine derivative represented by formula (W2), wherein R6d is as defined herein.Type: GrantFiled: September 20, 2017Date of Patent: May 15, 2018Assignee: Shionogi and Co., Ltd.Inventors: Yukihito Sumino, Moriyasu Masui, Daisuke Yamada, Fumiya Ikarashi, Kazuya Okamoto
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Patent number: 9969751Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: GrantFiled: December 12, 2011Date of Patent: May 15, 2018Assignee: Techfields Pharma Co., Ltd.Inventors: Chongxi Yu, Lina Xu, Yuhua Chen, Binbing Yan, Shiqian Tu
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Patent number: 9969752Abstract: The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.Type: GrantFiled: September 23, 2015Date of Patent: May 15, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Jiaqiang Cai, Alejandro Crespo, Xiaoxing Du, Byron Gabriel Dubois, Deodialsingh Guiadeen, Shankaran Kothandaraman, Ping Liu, Rongqiang Liu, Weiguo Quan, Christopher Sinz, Liping Wang