4027-35-4Relevant academic research and scientific papers
GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 001498; 001505; 001508; 001509, (2021/01/22)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 001540; 001541; 001548; 001550; 0015518; 001552, (2019/07/17)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme glycolate oxidase (GO). Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
CARBOXAMIDE DERIVATIVES
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Paragraph 0453-0454, (2015/12/17)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Acid-labile ester monomer having spirocyclic structure, polymer, resist composition, and patterning process
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, (2014/08/06)
An acid-labile ester monomer of spirocyclic structure has formula (1) wherein Z is a monovalent group having a polymerizable double bond, X is a divalent group which forms a cyclopentane, cyclohexane or norbornane ring, R2 is H or monovalent hydrocarbon, R3 and R4 are H or monovalent hydrocarbon, or R3 and R4, taken together, stand for a divalent group which forms a cyclopentane or cyclohexane ring, and n is 1 or 2. A polymer obtained from the acid-labile ester monomer has so high reactivity in acid-catalyzed elimination reaction that the polymer may be used to formulate a resist composition having high resolution.
Novel S1P1 receptor agonists - Part 2: From bicyclo[3.1.0] hexane-fused thiophenes to isobutyl substituted thiophenes
Bolli, Martin H.,Velker, J?rg,Müller, Claus,Mathys, Boris,Birker, Magdalena,Bravo, Roberto,Bur, Daniel,De Kanter, Ruben,Hess, Patrick,Kohl, Christopher,Lehmann, David,Meyer, Solange,Nayler, Oliver,Rey, Markus,Scherz, Michael,Steiner, Beat
supporting information, p. 78 - 97 (2014/02/14)
Previously, we reported on the discovery of a novel series of bicyclo[3.1.0]hexane fused thiophene derivatives that serve as potent and selective S1P1 receptor agonists. Here, we discuss our efforts to simplify the bicyclohexane fused thiophene
Inhibitors Of The Influenza A Virus M2 Proton Channel
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Page/Page column 8; 10, (2012/02/06)
Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
Molecular dynamics simulation directed rational design of inhibitors targeting drug-resistant mutants of influenza A virus M2
Wang, Jun,Ma, Chunlong,Fiorin, Giacomo,Carnevale, Vincenzo,Wang, Tuo,Hu, Fanghao,Lamb, Robert A.,Pinto, Lawrence H.,Hong, Mei,Klein, Michael L.,Degrado, William F.
supporting information; experimental part, p. 12834 - 12841 (2011/10/08)
Influenza A virus M2 (A/M2) forms a homotetrameric proton selective channel in the viral membrane. It has been the drug target of antiviral drugs such as amantadine and rimantadine. However, most of the current virulent influenza A viruses carry drug-resistant mutations alongside the drug binding site, such as S31N, V27A, and L26F, etc., each of which might be dominant in a given flu season. Among these mutations, the V27A mutation was prevalent among transmissible viruses under drug selection pressure. Until now, V27A has not been successfully targeted by small molecule inhibitors, despite years of extensive medicinal chemistry research efforts and high throughput screening. Guided by molecular dynamics (MD) simulation of drug binding and the influence of drug binding on the dynamics of A/M2 from earlier experimental studies, we designed a series of potent spirane amine inhibitors targeting not only WT, but also both A/M2-27A and L26F mutants with IC50s similar to that seen for amantadine's inhibition of the WT channel. The potencies of these inhibitors were further demonstrated in experimental binding and plaque reduction assays. These results demonstrate the power of MD simulations to probe the mechanism of drug binding as well as the ability to guide design of inhibitors of targets that had previously appeared to be undruggable.
ACID-LABILE ESTER MONOMER HAVING SPIROCYCLIC STRUCTURE, POLYMER, RESIST COMPOSITION, AND PATTERNING PROCESS
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, (2010/12/29)
An acid-labile ester monomer of spirocyclic structure has formula (1) wherein Z is a monovalent group having a polymerizable double bond, X is a divalent group which forms a cyclopentane, cyclohexane or norbornane ring, R2 is H or monovalent hydrocarbon, R3 and R4 are H or monovalent hydrocarbon, or R3 and R4, taken together, stand for a divalent group which forms a cyclopentane or cyclohexane ring, and n is 1 or 2. A polymer obtained from the acid-labile ester monomer has so high reactivity in acid-catalyzed elimination reaction that the polymer may be used to formulate a resist composition having high resolution.
SPIRO COMPOUNDS AND PHARMACEUTICAL USE THEREOF
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Page/Page column 41; 42, (2009/07/17)
The Spiro compound represented by the following general formula [Ia], its pharmaceutically acceptable salt or a solvate thereof
Hydrogenated Benzo (C) Thiophene Derivatives as Immunomodulators
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Page/Page column 27-28, (2008/12/07)
The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.
