94347-11-2Relevant articles and documents
Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors
Lopez-Tapia, Francisco,Brotherton-Pleiss, Christine,Yue, Peibin,Murakami, Heide,Costa Araujo, Ana Carolina,Reis Dos Santos, Bruna,Ichinotsubo, Erin,Rabkin, Anna,Shah, Raj,Lantz, Megan,Chen, Suzie,Tius, Marcus A.,Turkson, James
supporting information, p. 250 - 255 (2018/03/21)
The molecular determinants for the activities of the reported benzoic acid (SH4-54), salicylic acid (BP-1-102), and benzohydroxamic acid (SH5-07)-based STAT3 inhibitors were investigated to design optimized analogues. All three leads are based on an N-met
2-ARYLSULFONAMIDO-N-ARYLACETAMIDE DERIVATIZED STAT3 INHIBITORS
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Paragraph 00302, (2018/08/20)
The present disclosure provides pharmaceutical compositions comprising 2-arylsulfonamido-N-arylacetamide derivatized Stat3 inhibitors and certain pharmaceutically acceptable salts thereof, and methods of their use.
Synthesis of bifunctional chelating agents based on mono and diphosphonic derivatives of diethylenetriaminepentaacetic acid
Giovenzana, Giovanni B.,Guanci, Claudia,Demattio, Silvia,Lattuada, Luciano,Vincenzi, Veronica
, p. 4809 - 4813 (2014/06/24)
Bifunctional chelating agents (BFCAs) are small molecules containing a chelating unit, able to strongly coordinate a metal ion, and a reactive functional group, devised to form a stable covalent bond with another molecule. BFCAs are widely employed since their conjugation to a suitable biomolecule (e.g., a peptide or an antibody) allows the synthesis of diagnostic or therapeutic agents that specifically target diseased tissue with metals or radiometals. For this reason, BFCAs find application in diagnostic imaging, molecular imaging, and radiotherapy of cancer. The synthesis of new BFCAs based on a diethylenetriaminepentaacetic acid (DTPA) structure in which one or two carboxylic groups are replaced with phosphonic units is described. The phosphonic group, aside from being a classical isostere of the carboxylic acid in coordination chemistry, allows to modulate the physico-chemical properties of the ligands and of the corresponding complexes.
Targeting ketone drugs towards transport by the intestinal peptide transporter, PepT1
Foley, David,Bailey, Patrick,Pieri, Myrtani,Meredith, David
supporting information; scheme or table, p. 1064 - 1067 (2009/05/30)
Thiodipeptide prodrugs of the ketone nabumetone are shown to have affinity for, and be transported by, PepT1 in vitro. The Royal Society of Chemistry 2009.
The in vitro transport of model thiodipeptide prodrugs designed to target the intestinal oligopeptide transporter, PepT1
Foley, David,Pieri, Myrtani,Pettecrew, Rachel,Price, Richard,Miles, Stephen,Lam, Ho Kam,Bailey, Patrick,Meredith, David
supporting information; experimental part, p. 3652 - 3656 (2009/10/23)
A thiodipeptide carrier system is shown to be effective at enabling a range of covalently bound molecules, including benzyl, benzoyl and ibuprofen conjugates, to be transported via the intestinal peptide transporter PepT1, demonstrating its potential as a rational drug delivery target.
CONTRAST AGENTS ENDOWED WITH HIGH RELAXIVITY
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Page/Page column 39-40, (2008/06/13)
The present invention relates to a novel class of paramagnetic ion-based contrast agents of formula (I), wherein a chelating backbone moiety is highly functionalized by the presence of one or more polyhdroxylated chain, that show a pharmacokinetic profile analogous to that of the commonly used T1-general extravascular agents (NSA) but are further characterized by a higher relaxivity.
Carboxylic acid substituted heterocycles, derivatives thereof and methods of use
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, (2008/06/13)
Selected novel carboxylic acid substituted heterocycle compounds are effective for prophylaxis and treatment of inflammation, tissue degradation, cancer, fibrosis and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharm
Azepine or larger medium ring derivatives and methods of use
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, (2008/06/13)
Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of inflamation, tissue degradation and related diseases. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Novel ester linked glycosyl amino acids: Convenient building blocks for the synthesis of glycopeptide libraries
Tennant-Eyles, Richard J.,Fairbanks, Antony J.
, p. 391 - 401 (2007/10/03)
The completely orthogonally protected aspartic acid derivative FmocAsp(OBn)O'Bu is readily synthesized on a large scale. Deprotection of the β-carboxylic acid allows coupling to various sugar derivatives via free hydroxyl groups to produce novel glycosyl amino acids. Subsequent deprotection of either the α-acid or nitrogen is achieved cleanly to allow elaboration into an oligopeptide, whilst selective deprotection of PMB protected sugar hydroxyls is also readily achievable. Such novel glycosyl amino acid building blocks may be useful for the combinatorial synthesis of novel glycopeptide libraries.
The synthesis of pyrimidin-4-yI substituted a-amino acids. a versatile approach from alkynyl ketones
Adlington, Robert M.,Baldwin, Jack E.,Catterick, David,Pritchard, Garcth J.
, p. 855 - 866 (2007/10/03)
The reaction of amidines with a-amino acid alkynyl ketones is shown to be a versatile route to pyrimidin-4-yl substituted a-amino acids. This route is also applicable to a parallel synthesis approach and has allowed the formation of a range of pyrimidin-4-yl substituted a-amino acids, including the naturally occurring a-amino acid L-lathyrine 4.