214360-81-3Relevant articles and documents
Method of preparing Quinoline-5,8-dione derivatives for TGase 2 inhibitor
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Paragraph 0334-0336, (2020/04/28)
I Is -5,8- of the quinoline, dione derivative compound. of Formula I, or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the compound of Formula, TGase 2 has, inhibitory effects TGase 2, and thus the pharmaceutical composition may be useful for preventing or treating disorders or diseases mediated by TGase 2 or inhibiting. (by machine translation)
Quinoline-5,8-dione derivatives for TGase 2 inhibitor, and the pharmaceutical composition comprising the same
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Paragraph 0211-0213, (2019/10/29)
The present invention relates to a quinolin-5,8-dione derivative compound represented by chemical formula I, an optical isomer thereof or a pharmaceutically acceptable salt thereof. The compound represented by chemical formula I of the present invention has a TGase 2 inhibitory effect, and the pharmaceutical composition comprising the same can be usefully used for preventing or treating disorders or diseases mediated by TGase 2 or response to TGase 2 inhibition.COPYRIGHT KIPO 2020
Rational Design, Synthesis, and Pharmacological Characterization of Novel Ghrelin Receptor Inverse Agonists as Potential Treatment against Obesity-Related Metabolic Diseases
Daina, Antoine,Giuliano, Claudio,Pietra, Claudio,Wang, Junbo,Chi, Yushi,Zou, Zack,Li, Fugang,Yan, Zhonghua,Zhou, Yifan,Guainazzi, Angelo,Garcia Rubio, Silvina,Zoete, Vincent
, p. 11039 - 11060 (2018/10/24)
A new chemotype of ghrelin inverse agonists was discovered through chimeric design based on molecular scaffolds known as growth-hormone secretagogue receptor (GHSR) modulators but with divergent pharmacodynamic and pharmacokinetic properties. The structur
A novel protocol for the one-pot borylation/Suzuki reaction provides easy access to hinge-binding groups for kinase inhibitors
Hooper,Zambon,Springer
supporting information, p. 963 - 969 (2016/01/15)
The one-pot borylation/Suzuki reaction is a very efficient means of accessing cross-coupling products of two aryl-halide partners that generally requires the use of specific catalysts or ligands and/or relatively long reaction times. This new microwave-assisted method provides a quick one-pot borylation/Suzuki reaction protocol that we applied to the synthesis of various bi- or poly-aryl scaffolds, including a variety of aryl and heteroaryl ring systems and the core frameworks of kinase inhibitors vemurafenib and GDC-0879.
Polymerizable compound and its in the optical anisotropic body and the application of the liquid crystal display element
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Paragraph 0042; 0044; 0046-0048, (2018/02/04)
The invention relates to a polymerizable compound with general formula I, also provides a polymerizable liquid crystal composition containing the polymerizable compound and a liquid crystal display element containing the polymerizable compound, and especially provides a liquid crystal display element used for PS or PSA (polymer stabilized or polymer stably-aligned) liquid crystal displays. The polymerizable liquid crystal compound has the advantages of good solubility, good orientation effect, fast polymerization rate, complete polymerization and low residue, so the bad display problem can be greatly improved.
Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: Synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif
Krueger, A. Chris,Randolph, John T.,Degoey, David A.,Donner, Pamela L.,Flentge, Charles A.,Hutchinson, Douglas K.,Liu, Dachun,Motter, Christopher E.,Rockway, Todd W.,Wagner, Rolf,Beno, David W.A.,Koev, Gennadiy,Lim, Hock B.,Beyer, Jill M.,Mondal, Rubina,Liu, Yaya,Kati, Warren M.,Longenecker, Kenton L.,Molla, Akhteruzzaman,Stewart, Kent D.,Maring, Clarence J.
, p. 3487 - 3490 (2013/07/19)
The synthesis and structure-activity relationships of a novel aryl uracil series which contains a fused 5,6-bicyclic ring unit for HCV NS5B inhibition is described. Several analogs display replicon cell culture potencies in the low nanomolar range along with excellent rat pharmacokinetic values.
IMIDAZO [1, 2 - B] PYRIDAZINE - BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM, AND USES THEREOF
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Page/Page column 57, (2013/09/26)
Imidazo[1,2-b]pyridazine-based compounds of the formula (I): are disclosed, wherein R1, R2 and R3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by adaptor associated kinase 1 activity are also disclosed.
BIARYL PHOSPHODIESTERASE 1NHIBITORS
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Page/Page column 183-184, (2012/08/29)
Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions
2,3-DIHYDRO-1H-INDEN-1-YL-2,7-DIAZASPIRO[3.5] NONANE DERIVATIVES
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Page/Page column 26, (2011/10/10)
The present invention provides a compound of Formula (I) or a pharmaceutically salt thereof wherein R1, R2, Ra, L, Z, Z1 and Z2 are as defined herein, that act as Ghrelin antagonists or inverse agonists; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by the antagonism of the Ghrelin receptor.
URACIL OR THYMINE DERIVATIVE FOR TREATING HEPATITIS C
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Page/Page column 182-183, (2009/04/25)
Present application relates to the compounds of formula I useful to treat hepatitis C (HCV) infections. In the structure of the disclosed compounds is the uracil or thymine derivative linked via a phenylene into either fused 2-ring cyclic system (R6) or alternatively via additional two-atom linker (L) to a 5-6 membered monocycle (R6). Application further discloses polymorphs and pseudopolymorphs of two specific compounds: N-(6(3-t-butyl-5-(2>4-dioxo-3,4-dihydropyrimidin-1 (2H)- y!)2-methoxy-phenyl)naphthalen-2-yl)methanesulfonamide and (E)-N-(4(3-t- butyl-5-(2,4-dioxo-3)4-dihydropyrimidin-1 (2H)-yl)2-methoxy-styryl- phenyl)methanesulfonamide.