77317-53-4Relevant academic research and scientific papers
DISUBSTITUTED DL ARYLOXYBENZOH ETERODI AZOLE COMPOUNDS
-
Paragraph 0173-0176; 0177-0179, (2021/07/24)
A disubstituted diaryloxybenzoheterodiazole compound having general formula (I): wherein: R1, R2 and R3, which are the same as or different from each other, represent a hydrogen atom; or represent a halogen atom such as, for example, chlorine, bromine, fluorine, iodine, preferably fluorine; or are selected from optionally halogenated linear or branched C1-C12, preferably C1-C8, alkyl groups, optionally substituted phenoxy groups, provided that at least one of R1, R2 and R3 is an optionally substituted phenoxy group and, if R3 is an optionally substituted phenoxy group, at least one of R1, R2 is different from hydrogen; R4, which are the same as or different from each other, represent a hydrogen atom; or are selected from -COOR groups wherein R is selected from linear or branched C1-C8, preferably C1-C4, alkyl groups. This disubstituted diaryloxybenzoheterodiazole compound having general formula (I) may advantageously be used as a spectrum converter in luminescent solar concentrators ("Luminescent Solar Concentrators" - LSCs) which, in turn, are capable of improving the performance of photovoltaic devices (or solar devices) selected, for example, from photovoltaic cells (or solar cells), photovoltaic modules (or solar modules), on either a rigid or flexible support.
SELECTIVE BTK IRREVERSIBLE INHIBITORS
-
, (2021/01/23)
The invention provides a series of conformationally stable and selective, irreversible kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds. The compounds herein are atropisomers having increased kinase selectivity and are for use in treating conditions that benefit from selective BTK kinase inhibition.
TYROSINE KINASE INHIBITORS
-
, (2017/04/19)
The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase ("BTK") inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, au
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase
Bourbeau, Matthew P.,Siegmund, Aaron,Allen, John G.,Shu, Hong,Fotsch, Christopher,Bartberger, Michael D.,Kim, Ki-Won,Komorowski, Renee,Graham, Melissa,Busby, James,Wang, Minghan,Meyer, James,Xu, Yang,Salyers, Kevin,Fielden, Mark,Véniant, Murielle M.,Gu, Wei
supporting information, p. 10132 - 10141 (2014/01/17)
Acetyl-CoA carboxylase (ACC) is a target of interest for the treatment of metabolic syndrome. Starting from a biphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed. Initial pharmacokinetic liabilities of the piperazine oxadiazoles were overcome by blocking predicted sites of metabolism, resulting in compounds with suitable properties for further in vivo studies. Compound 26 was shown to inhibit malonyl-CoA production in an in vivo pharmacodynamic assay and was advanced to a long-term efficacy study. Prolonged dosing with compound 26 resulted in impaired glucose tolerance in diet-induced obese (DIO) C57BL6 mice, an unexpected finding.
SUBSTITUTED IMIDAZOPYR- AND IMIDAZOTRI-AZINES
-
Page/Page column 52, (2009/12/05)
Fused pyridine-based bicyclic compounds having the structure of Formula I, as defined herein, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. This abstract does not define or limit the invention.
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis
Akama, Tsutomu,Baker, Stephen J.,Zhang, Yong-Kang,Hernandez, Vincent,Zhou, Huchen,Sanders, Virginia,Freund, Yvonne,Kimura, Richard,Maples, Kirk R.,Plattner, Jacob J.
scheme or table, p. 2129 - 2132 (2009/12/07)
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.
Conformational analyses of thiirane-based gelatinase inhibitors
Lee, Mijoon,Hesek, Dusan,Shi, Qicun,Noll, Bruce C.,Fisher, Jed F.,Chang, Mayland,Mobashery, Shahriar
, p. 3064 - 3067 (2008/12/23)
SB-3CT is a thiirane-containing inhibitor of the gelatinase class of matrix metalloprotease enzymes. In support of the mechanistic study of this inhibition, the conformational analyses of SB-3CT (and of two methyl-substituted derivatives) were undertaken using X-ray crystallography and molecular dynamics simulation.
Pyrrolopyrimidines as therapeutic agents
-
, (2008/06/13)
Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatiod arthritis, disorders of the immune system, trasplant refections and imflammatory disorders.
Novel brominated phenoxy compounds and processes for their preparation
-
, (2008/06/13)
Compounds of the formula wherein:, n = 0 or 1;, R1 and R2 are C1 to C3 alkyl groups, or R2 may be H when n = 0;, Y is selected from the group: or, wherein:, m = 1-6;, Z = SO2,S,C=O,CH2 or C(CH3)2;, and a process for their preparation are described.
