Additional Hetero Ring Containing Patents (Class 546/256)
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Patent number: 12162863Abstract: The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.Type: GrantFiled: June 12, 2019Date of Patent: December 10, 2024Assignee: RYVU THERAPEUTICS S.A.Inventors: Monika Patrycja Dobrzanska, Magdalena Izabela Zawadzka, Adam Radzimierski, Grzegorz Witold Topolnicki, Grzegorz Wojciech Cwiertnia, Tushar Ravindra Mahajan, Charles-Henry Fabritius, Stefan Chmielewski, Karolina Maria Gluza, Jose Alvarez, Maciej Krzysztof Rogacki, Magdalena Mroczkowska
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Patent number: 12139479Abstract: Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.Type: GrantFiled: September 23, 2022Date of Patent: November 12, 2024Assignee: Basilea Pharmaceutica International AG, AllschwilInventors: Michael Trzoss, Jonathan Covel, Karen Joy Shaw, Peter Webb
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Patent number: 12075695Abstract: The present application relates to a compound of Chemical Formula 1 and an organic light emitting device including the same: wherein Ar1 to Ar3, L1 and L2 are described herein.Type: GrantFiled: March 23, 2023Date of Patent: August 27, 2024Assignee: LG Chem, Ltd.Inventors: Miyeon Han, Dong Hoon Lee, Jungoh Huh, Boonjae Jang, Minyoung Kang, Dong Uk Heo, Min Woo Jung
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Patent number: 11980091Abstract: An organic electroluminescence device of an embodiment includes a first electrode, a second electrode, and an emission layer between the first electrode and the second electrode, and the emission layer includes a compound represented by Formula 1 below, and thus the organic electroluminescence device may exhibit high luminous efficiency characteristics and improved service life characteristics.Type: GrantFiled: September 16, 2020Date of Patent: May 7, 2024Assignees: Samsung Display Co., Ltd., Lapto Co., Ltd.Inventors: Dongchan Lee, Eu-gene Oh, SeulOng Kim, Yunjee Park, Munsoo Kim, JuWan Maeng, Kap-jong Han
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Patent number: 11926614Abstract: The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), —CN, —NO2, —N(R)2, and —SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g.Type: GrantFiled: June 19, 2019Date of Patent: March 12, 2024Assignees: OSLO UNIVERSITETSSYKEHUS HF, FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITY OF OULUInventors: Stefan Krauss, Marc Nazare, Lari Lehtio, Jo Waaler, Anita Wegert, Ruben Gerardus George Leenders
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Patent number: 11905245Abstract: The present disclosure relates to a novel heterocyclic compound represented by the following Chemical Formula 1 and to an organic light emitting device comprising the same: wherein, R1, R2, R3, R4, R5, R6, m, n and o are described herein.Type: GrantFiled: December 3, 2019Date of Patent: February 20, 2024Assignee: LG Chem, Ltd.Inventors: Juhwan Kim, Jaechol Lee, Jaesoon Bae, Soyoung Yu, Young Kwang Kim, Daeho Kim
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Patent number: 11890275Abstract: The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of diseases mediated by aberrant cell signalling, such as inflammatory disorders, cancer and neoplastic disease. Particular compounds described herein exhibit selective inhibitory activity against CBP compared with BRD4.Type: GrantFiled: March 15, 2021Date of Patent: February 6, 2024Inventors: Lynnie Trzoss, Juan Manuel Betancort, Toufike Kanouni, Michael Brennan Wallace, Amogh Boloor
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Patent number: 11873300Abstract: Crystalline forms of Compound I: pharmaceutically acceptable salts thereof, and solvates and hydrates thereof are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.Type: GrantFiled: August 13, 2020Date of Patent: January 16, 2024Assignee: Vertex Pharmaceuticals IncorporatedInventors: Yi Shi, Kevin J. Gagnon, Jicong Li, Jennifer Lu, Ales Medek, Muna Shrestha, Michael Waldo, Beili Zhang, Carl L. Zwicker, Corey Don Anderson, Jeremy J. Clemens, Thomas Cleveland, Timothy Richard Coon, Bryan Frieman, Peter Grootenhuis, Sara Sabina Hadida Ruah, Jason McCartney, Mark Thomas Miller, Prasuna Paraselli, Fabrice Pierre, Sara E. Swift, Jinglan Zhou
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Patent number: 11814371Abstract: The present application relates to the field of medicine. Specifically, disclosed are a compound of formula (I), a preparation method therefor, and a pharmaceutical composition comprising the compound.Type: GrantFiled: March 4, 2021Date of Patent: November 14, 2023Assignee: MEDSHINE DISCOVERY INC.Inventors: Guanglong Sun, Chunli Shen, Chengde Wu, Shuhui Chen
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Patent number: 11771688Abstract: Described herein are pyridine derivatives substituted by heterocycle and amino groups and pharmaceutical compositions comprising said compounds. The disclosed compounds are antifungal agents. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.Type: GrantFiled: June 24, 2019Date of Patent: October 3, 2023Assignee: AMPLYX PHARMACEUTICALS, INC.Inventors: Andrei W. Konradi, Jonathan A. Covel, Michael Grey
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Patent number: 11666563Abstract: The present invention aims to find a pharmaceutical preparation which treats or prevents glaucoma or ocular hypertension and is effective for patients with inadequate efficacies of glaucoma or ocular hypertension therapeutic agents. It has been found that omidenepag, an ester thereof, or a salt thereof has an excellent intraocular pressure lowering efficacy on patients with inadequate efficacies of other glaucoma or ocular hypertension therapeutic agents. Therefore, the omidenepag, the ester thereof, or the salt thereof of the present invention is useful as a pharmaceutical preparation which can treat or prevent glaucoma or ocular hypertension even in patients with inadequate efficacies of other glaucoma or ocular hypertension therapeutic agents.Type: GrantFiled: December 27, 2018Date of Patent: June 6, 2023Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hisashi Kawata, Noriko Kawabata, Naveed Shams
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Patent number: 11660309Abstract: The present embodiments relate to methods for the prevention and treatment of inflammatory conditions such as alcoholic liver disease (ALD). More specifically the present embodiments relate to the prevention and treatment of ALD through the administration of an Retinoic Acid Receptor (RAR) agonist. Some embodiments relate to use of tazarotene in the prevention and treatment of alcohol-induced liver injury, alcohol-related liver disease, fatty liver disease, hepatic steatosis, alcoholic hepatitis or alcoholic cirrhosis.Type: GrantFiled: February 22, 2021Date of Patent: May 30, 2023Assignee: GRI BIO, INC.Inventor: Vipin Kumar Chaturvedi
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Patent number: 11649226Abstract: The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula: Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.Type: GrantFiled: December 22, 2020Date of Patent: May 16, 2023Assignee: Bristol-Myers Squibb CompanyInventors: Bahar Inankur, Sergei Kolotuchin, Maxime C. D. Soumeillant, Daniel S. Treitler
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Patent number: 11564901Abstract: Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms or sequelae of disease. Chronic and acute conditions may be due to viral infections such as HIV and AIDS, neoplastic diseases stroke, kidney disease, urinary incontinence, autoimmune disorders, Parkinson's disease, prostate hypertrophy, aging, or the treatment of such diseases. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools against acute and chronic conditions in mammalian subjects.Type: GrantFiled: January 18, 2013Date of Patent: January 31, 2023Assignee: Biosuccess Biotech Co., Ltd.Inventors: Zheng Tao Han, Hung-Fong Chen
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Patent number: 11538999Abstract: A heterocyclic compound and an organic light-emitting device including the same are provided. The heterocyclic compound is represented by Formula 1: Details of R1, R2, R3, X1, L1, and a1 and b1 are provided in the disclosure.Type: GrantFiled: June 16, 2017Date of Patent: December 27, 2022Assignee: SAMSUNG DISPLAY CO., LTD.Inventors: Soobyung Ko, Haejin Kim, Mieun Jun, Youngkook Kim, Seokhwan Hwang
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Patent number: 11529341Abstract: The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation.Type: GrantFiled: March 13, 2019Date of Patent: December 20, 2022Inventors: Chandregowda Venkateshappa, Jeyaraj D A, Muralidhar Pendyala, Dhanalakshmi Sivanandhan, Sridharan Rajagopal
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Patent number: 11447453Abstract: 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: March 12, 2020Date of Patent: September 20, 2022Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTEInventors: Nicholas David Peter Cosford, Dhanya Raveendra-Panickar, Douglas J. Sheffler, John Howard Hutchinson, Reto Andreas Gadient
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Patent number: 11318145Abstract: The present invention relates to oral ready to use liquid pharmaceutical compositions of eslicarbazepine. It also relates to the processes for the preparation of said liquid compositions. The present invention provides liquid compositions of eslicarbazepine with desired technical attributes such as release profile, viscosity, pH, stability, and acceptable organoleptic properties. The prepared compositions are useful in patients having difficulties in swallowing tablets and provide the physician with providing a more convenient and less cumbersome posology.Type: GrantFiled: May 21, 2021Date of Patent: May 3, 2022Inventors: Indranil Nandi, Tusharmouli Mukherjee, Dinesh Kumar, Rakesh K. Singh, Saurabh Srivastava
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Patent number: 11117903Abstract: The invention relates to compound of formula (I) wherein R1 to R3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: December 20, 2019Date of Patent: September 14, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Beat Frei, Luca Gobbi, Uwe Grether, Fabienne Ricklin, Stephan Roever, Mark Rogers-Evans, Didier Rombach
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Patent number: 11040968Abstract: Disclosed in the present invention are a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and also disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.Type: GrantFiled: January 22, 2018Date of Patent: June 22, 2021Inventors: Chengde Wu, Tao Yu, Ning Li, Shuhui Chen
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Patent number: 10815208Abstract: Provided is a method for preparing 2-hydroxy-4-(2, 3-disubstituted benzyloxy)-5-substituted benzaldehyde derivative represented by formula (I). The method comprises the following steps: (1) preparing 3-aryl-2-substituted toluene derivative 2 by using 3-iodo-2-substituted toluene derivative 1 and aryl boronic acid 5 or aryl boronate as starting materials; (2) preparing a benzyl halide derivative 3 by using 3-aryl-2-substituted toluene derivative 2 as starting materials; and (3) preparing 4-(2, 3-disubstituted benzyloxy)-2-hydroxy-5-substituted benzaldehyde derivative (I) by using benzyl halide derivative 3 and 2,4-dihydroxy-5-substituted benzaldehyde 6.Type: GrantFiled: May 23, 2017Date of Patent: October 27, 2020Assignees: Institute of Materia Medica, Chinese Academy of Medical Sciences, Tianjin Chase Sun Pharmaceutical Co., LTDInventors: Zhiqiang Feng, Xiaoguang Chen, Yang Yang, Fangfang Lai
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Patent number: 10730830Abstract: A compound of general formula (I-1): wherein the symbols are defined in the specification, has a selective S1P5 receptor binding activity and modulates the function of an S1P5 receptor, and can therefore be a therapeutic agent for a S1P5-mediated disease, for example, neurodegenerative diseases such as schizophrenia, Binswanger's disease and the like.Type: GrantFiled: January 27, 2017Date of Patent: August 4, 2020Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Toshihide Watanabe, Kensuke Kusumi, Yuichi Inagaki
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Patent number: 10710982Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.Type: GrantFiled: February 12, 2020Date of Patent: July 14, 2020Assignee: Merck Sharp & Dohme Corp.Inventors: Pranav Gupta, Jiansheng Wan
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Patent number: 10577367Abstract: Provided are compounds of Formula I, or pharmaceutically acceptable salts thereof, and methods for their use and production.Type: GrantFiled: February 8, 2019Date of Patent: March 3, 2020Assignee: BIOGEN MA INC.Inventors: Timothy Chan, Kevin Guckian, Tracy Jenkins, Jermaine Thomas, Jeffery Vessels, Gnanasambandam Kumaravel, Robert Meissner, Joseph Lyssikatos, Brian Lucas, Irina Leaf, Jeremy Duffield
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Patent number: 10577348Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.Type: GrantFiled: December 14, 2015Date of Patent: March 3, 2020Assignee: MERCK SHARP & DOHME CORP.Inventors: Pranav Gupta, Jason Wan, Scott T. Trzaska
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Patent number: 10562850Abstract: Disclosed are compounds of formula I, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.Type: GrantFiled: September 30, 2016Date of Patent: February 18, 2020Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Pravin L. Kotian, Yarlagadda S. Babu, V. Satish Kumar, Weihe Zhang, Lakshminarayana Vogeti
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Patent number: 10544133Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.Type: GrantFiled: June 15, 2018Date of Patent: January 28, 2020Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, John V. Duncia, John Hynes, Satheesh Kesavan Nair, William J. Pitts, Sreekantha Ratna Kumar, Daniel S. Gardner, Natesan Murugesan, Venkatram Reddy Paidi, Joseph B. Santella, Ramesh Kumar Sistla, Hong Wu
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Patent number: 10468256Abstract: A method of forming a material layer includes providing a substrate into a reaction chamber, providing a source material onto a substrate, the source material being a precursor of a metal or semimetal having a ligand, providing an ether-based modifier on the substrate, purging an inside of the reaction chamber, and reacting a reaction material with the source material to form the material layer.Type: GrantFiled: April 7, 2017Date of Patent: November 5, 2019Assignee: Samsung Electronics Co., Ltd.Inventors: Sun-min Moon, Youn-soo Kim, Han-jin Lim, Yong-jae Lee, Se-hoon Oh, Hyun-jun Kim, Jin-sun Lee
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Patent number: 10414740Abstract: Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.Type: GrantFiled: June 4, 2018Date of Patent: September 17, 2019Assignee: Agios Pharmaceuticals, Inc.Inventors: Rene M. Lemieux, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Jeremy Travins, Shunqi Yan
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Patent number: 10208023Abstract: The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (I)-(X) or Compounds (1)-(92) of Table 1) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotrophic lateral sclerosis, glaucoma, ischemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.Type: GrantFiled: February 27, 2014Date of Patent: February 19, 2019Inventor: Mark G. DeGiacomo
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3-(benzoimidazol-2-yl)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof
Patent number: 10183929Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: February 6, 2018Date of Patent: January 22, 2019Assignee: Samumed, LLCInventors: Sunil Kumar K C, John Hood -
Patent number: 10047225Abstract: Disclosed are styryl dyes of formula wherein R1, R2, R3, R?1, R?2 and R?3 independently of each other are hydrogen; —NH(CO)—C1-C5alkyl; —N(C1-C5alkyl)(C1-C5alkyl-CN); C1-C6alkoxy; a heterocyclic radical; or R1 and R2 or R?1 and R?2 together form a 5- to 10-membered, monocyclic, carbocyclic or heterocyclic ring; wherein at least one of R1, R2, R3, R?1, R?2 and R?3 is different from hydrogen; Q and Q? independently from each other are the direct bond; *—C(O)—*; *—C(O)O—*; *—OCO—*; *—N(R4)—*; ?*—C(O)N(R6)—*; or *—(R6)NC(O)—*; and R4, R5 and R6 independently from each other are hydrogen; C1-C14alkyl; C2-C14alkenyl; C6-C12aryl; C6-C12aryl-C1-C10alkyl; or C1-C10alkyl(C5-C12aryl); X and X? are *—(CH2)m—*; Y1 and Y2 independently from each other are C1-C10alkylene; C5-C10cycloalkylene; C5-C12arylene; or C5-C12arylene-(C1-C10alkylene); An? is an anion; m is a number from 1 to 8; n is 0, or 1; and p is 0, or 1.Type: GrantFiled: August 28, 2014Date of Patent: August 14, 2018Assignee: BASF SEInventors: Frank Bachmann, Christian Cremer, Markus Knobloch, Beate Fröhling, Werner Specker
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Patent number: 10035787Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.Type: GrantFiled: June 15, 2017Date of Patent: July 31, 2018Assignee: ELI LILLY AND COMPANYInventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
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Patent number: 9988385Abstract: This invention provides 1,4-dihydropyrrolo[3,2-b]pyrrole derivatives which can be used as strongly fluorescent compounds and a one-stage method for their synthesis from simple substrates.Type: GrantFiled: November 5, 2013Date of Patent: June 5, 2018Assignee: INSTYTUT CHEMII ORGANICZNEJ POLSKIEJ AKADEMII NAUKInventors: Anita Janiga, Maciej Krzeszewski, Daniel Gryko
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Patent number: 9962386Abstract: Disclosed are chemical entities which are compounds of formula (I): or pharmaceutically acceptable salts thereof; wherein Y, Ra, Ra?, Rb, Rc, X1, X2, X3, Rd, Z1, and Z2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.Type: GrantFiled: April 17, 2017Date of Patent: May 8, 2018Assignee: Millennium Pharmaceuticals, Inc.Inventors: Matthew O. Duffey, Dylan England, Brian Scott Freeze, Zhigen Hu, Steven Langston, Charles McIntyre, Hirotake Mizutani, Koji Ono, He Xu
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Chiral synthesis of pyrrolidine core compounds en route to neuronal nitric oxide synthase inhibitors
Patent number: 9758507Abstract: A chiral synthesis of pyrrolidine compounds en route to selective neuronal nitric oxide synthase inhibitors, and representative inhibitor compounds heretofore unattainable.Type: GrantFiled: December 14, 2015Date of Patent: September 12, 2017Assignee: Northwestern UniversityInventors: Richard B. Silverman, Fengtian Xue -
Patent number: 9708291Abstract: The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: The present invention further relates to novel processes for preparing a crystalline compound, which is {2-[1-(3,5-bis-trifluoromethyl-benzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, Form IV.Type: GrantFiled: November 10, 2015Date of Patent: July 18, 2017Assignee: Vanda Pharmaceuticals Inc.Inventors: Michael Edward Kobierski, Michael E. Kopach, Pingyun Chen
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Patent number: 9650340Abstract: The present invention relates to 5-fluoro-N-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).Type: GrantFiled: November 12, 2013Date of Patent: May 16, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Lücking, Niels Böhnke, Arne Scholz, Philip Lienau, Gerhard Siemeister, Ulf Bömer, Dirk Kosemund, Rolf Bohlmann, Ludwig Zorn
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Patent number: 9617243Abstract: The present invention relates to novel aminopyridyloxypyrazole compounds that inhibit the activity of transforming growth factor beta receptor 1 (TGF?R1), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, preferably colon cancer, melanoma, hepatocellular carcinoma, renal cancer, glioblastoma, pancreatic cancer, myelodysplastic syndrome, lung cancer, and gastric cancer, and/or fibrosis, preferably liver fibrosis and chronic kidney disease.Type: GrantFiled: September 30, 2015Date of Patent: April 11, 2017Assignee: Eli Lilly and CompanyInventors: William T. McMillen, Sajan Joseph, Huaxing Pei, Jason Scott Sawyer, Gaiying Zhao, David A. Coates, Craig D. Wolfangel
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Patent number: 9598405Abstract: The invention provides certain thiazole-substituted aminopyridine compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, Cy, and the subscript t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).Type: GrantFiled: December 19, 2013Date of Patent: March 21, 2017Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Kaleen Konrad Childers, Maria Emilia Di Francesco, John Michael Ellis, Andrew M. Haidle, Yuan Liu, Alan B. Northrup, Brendan O'Boyle, Ryan D. Otte, Michael H. Reutershan, Dilrukshi Vitharana, Hyun Chong Woo
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Patent number: 9518041Abstract: Provided is (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof. Also provided is a drug containing as the active ingredient (+)-5-(3,4-difluorophenyl)-5-[(3-methyl-2-oxopyridin-1(2H)-yl)methyl]imidazolidine-2,4-dione or a salt thereof.Type: GrantFiled: June 6, 2014Date of Patent: December 13, 2016Assignee: KAKEN PHARMACEUTICAL CO., LTD.Inventors: Noriyuki Kamei, Daigo Kamimura, Yoshitake Sumikawa, Shota Tokuoka
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Patent number: 9499528Abstract: Methods for preparing 2,5-Bis(benzoxazol-2?-yl)benzene-1,4-diol derivatives (Zinhbo derivatives) are provided. Zinhbo derivatives are used to detect zinc ions and have particular application in vivo and in vitro. Zinhbo derivatives upon excitation give a florescence response emission that can be used to determine the presence of zinc cation in solution. Zinhbo derivatives complexed with zinc cations upon excitation can produce a florescence response emission in the visible and near infrared range. Zinhbo derivatives complexed with zinc cations exhibit a large stoke shift between the excitation and emission wavelengths.Type: GrantFiled: April 8, 2014Date of Patent: November 22, 2016Assignee: The University of AkronInventors: Yi Pang, Junfeng Wang
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Patent number: 9493488Abstract: The present invention is to provide highly solid state emissive fluorophores of the formula 1 and 2 useful for the solid state lighting. The formula 1 and 2 have good solid state emission in blue and green region respectively. The zinc complexes of formula 1A and 2A have yellow and red emission respectively in solid state. The present invention also provide high solid state emissive assay of formula 1 and 2 to convert UV light into visible light by coating the color tunable materials on the 365-nm emitting solid state LED. The present invention further provides carbazole end-capped bipyridine for screening of metal salts with different counterions in solutions. The discrimination of the various metal salts can be monitored by noting the fluorescence change in solution. The zinc salts with different counterions have different emission color in solution. The present invention also develop a new two photon active fluorescent Zn2+ specific probe for detecting Zn2+ in cellular environments.Type: GrantFiled: February 14, 2012Date of Patent: November 15, 2016Assignee: Council of Scientific & Industrial ResearchInventors: Ajayaghosh Ayyappanpillai, Divya Kizhumuri, Srinivasan Sampath
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Patent number: 9428488Abstract: To provide an industrially useful method for producing pharmaceutically useful 4-[5-(pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile, and an intermediate for producing the compound. The method for producing compound represented by formula (1) is represented by the following reaction scheme, and the intermediate is represented by the following formula (4).Type: GrantFiled: July 24, 2013Date of Patent: August 30, 2016Assignee: FUJIYAKUHIN CO., LTD.Inventors: Yoshiyuki Iwabuchi, Sachiho Miyata, Junichiro Uda, Osamu Nagata
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Patent number: 9353110Abstract: There is provided a compound having an excellent controlling effect on pests represented by the formula (1): wherein, A1 represents —NR7—, etc., A2 represents a nitrogen atom, etc., A3 represents a nitrogen atom, etc., R1 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R2, R3 and R4 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more halogen atoms, etc., R5 and R6 are the same or different and each represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group X, etc., R7 represents a C1-C6 chain hydrocarbon group optionally substituted by one or more atoms or groups selected from Group W, etc., n represents 0, 1 or 2, or an N-oxide thereof.Type: GrantFiled: July 17, 2015Date of Patent: May 31, 2016Assignee: Sumitomo Chemical Company, LimitedInventors: Masaki Takahashi, Takamasa Tanabe, Mai Ito, Yoshihiko Nokura
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Patent number: 9198420Abstract: The present invention relates to norbormide analogs having rodenticidal activity; rodenticidal compositions comprising the analogs; uses of the analogs as rodenticides; uses of the analogs in the manufacture of rodenticidal compositions; and methods for controlling rodents using the compositions.Type: GrantFiled: March 11, 2013Date of Patent: December 1, 2015Assignee: Landcare Research New Zealand LimitedInventors: Brian Hopkins, Margaret Anne Brimble, David Rennison, Sergio Bova, Maurizio Cavalli, Olivia Laita
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Patent number: 9187426Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: June 25, 2009Date of Patent: November 17, 2015Assignees: Novartis AG, Xenon PharmaceuticalsInventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
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Patent number: 9172051Abstract: Polyphenylene compounds such as compounds represented by Formulas 1-28 may be used in electronic devices such as organic light-emitting devices. For example, the compounds may be used as host material in an emissive layer.Type: GrantFiled: August 20, 2013Date of Patent: October 27, 2015Assignee: Nitto Denko CorporationInventors: Shijun Zheng, David T. Sisk, Liping Ma
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Patent number: 9131694Abstract: The invention disclosed in this document is related to the field of pesticides and their use in controlling pests. Novel pyridine compounds for use in controlling pests are disclosed.Type: GrantFiled: November 1, 2013Date of Patent: September 15, 2015Assignee: Dow AgroSciences LLCInventors: Noormohamed M. Niyaz, Francis E. Tisdell, Gerald B. Watson, James M. Renga, William C. Lo, Maurice C. H. Yap
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Patent number: 9051284Abstract: Compounds useful in porous films for light extraction and/or light scattering in electronic devices, such as light-emitting devices, are described herein. These compounds may be represented by Formula 1, as described herein.Type: GrantFiled: March 2, 2012Date of Patent: June 9, 2015Assignee: NITTO DENKO CORPORATIONInventors: Shijun Zheng, Jensen Cayas, David T. Sisk