2848-78-4Relevant academic research and scientific papers
INDOLINONES COMPOUNDS AND THEIR USE IN THE TREATMENT OF FIBROTIC DISEASES
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Page/Page column 33-34, (2017/07/14)
The present invention relates inter alia to a compound of formula (I) Wherein R1, R2, R3 and Z are as defined in the specification and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of fibrotic diseases or interstitial lung diseases, in particular idiopathic pulmonary fibrosis.
Fast alpha nucleophiles: Structures that undergo rapid hydrazone/oxime formation at neutral pH
Kool, Eric T.,Crisalli, Pete,Chan, Ke Min
supporting information, p. 1454 - 1457 (2014/04/03)
Hydrazones and oximes are widely useful structures for conjugate formation in chemistry and biology, but their formation can be slow at neutral pH. Kinetics studies were performed for a range of structurally varied hydrazines, and a surprisingly large variation in reaction rate was observed. Structures that undergo especially rapid reactions were identified, enabling reaction rates that rival orthogonal cycloaddition-based conjugation chemistries.
MACROCYCLIC LACTONE DERIVATIVES AND USES THEREOF
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Page/Page column 27; 28, (2014/08/19)
The present invention provides compounds represented by Formula 1: wherein, R' is as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the preparation of the compounds of Formula and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of inflammatory disorders and/or viral infections. The compounds and the pharmaceutical compositions of the present invention are also useful for the treatment of cancer.
FUSED HETEROCYCLIC COMPOUND
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Page/Page column 414-415, (2010/11/28)
A compound of the formula: wherein ring'' A is a 7-membered or 8-membered nitrogen- containing ring optionally further substituted, ring B is an optionally substituted aryl group or an optionally substituted heteroaryl group, X1 is a group represented by -NR3-Y1-, -0-, -S-, -SO-, -SO2- or -CHR3- wherein R3 is a hydrogen atom or'' an optionally substituted aliphatic hydrocarbon group, or R3 may be bonded to the carbon atom of ring B to form an optionally substituted ring structure, and Y1 is a bond or an optionally substituted C1-4 alkylene, R1 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom or a sulfur atom, the formula = shows a single bond or a double bond, when ===R2 is - R2, R2 is a hydrogen atom, or an optionally substituted group bonded via a carbon atom, a nitrogen atom, an oxygen atom or a sulfur atom, and when ===R2 is =R2, R2 is an oxo group, an optionally substituted alkylidene group, or an optionally, substituted imino group.
17β-O-aminoalkyloximes of 5β-androstane-3β, 14β-diol with digitalis- like activity: Synthesis, cardiotonic activity, structure-activity relationships, and molecular modeling of the Na+,K+-ATPase receptor
Cerri, Alberto,Almirante, Nicoletta,Barassi, Paolo,Benicchio, Alessandra,Fedrizzi, Giorgio,Ferrari, Patrizia,Micheletti, Rosella,Quadri, Luisa,Ragg, Enzio,Rossi, Roberto,Santagostino, Marco,Schiavone, Antonio,Serra, Fulvio,Zappavigna, Maria Pia,Melloni, Piero
, p. 2332 - 2349 (2007/10/03)
A series of digitalis-like compounds with a 17-aminoalkoxyiminoalkyl or -alkenyl substituent was synthesized and evaluated for inhibition of Na+,K+-ATPase and for inotropic activity. The highest inhibition was found with compounds having the substituent in configuration 17β and the amino group at a distance of 6 or 7 bonds from C(17) of the digitoxigenin skeleton. The presence of the oxime function strengthens the interaction with the receptor, more if α,β-unsaturated, thus mimicking the electronic situation of the unsaturated lactone in natural digitalis compounds. The most active compounds showed Na+,K+-ATPase inhibitory potencies (IC50) 17-25 times higher than the standards digitoxigenin and digoxin and 3-11 times higher inotropic potencies (EC50) in isolated guinea pig left atria. These features are supported by a molecular model suggesting the possible interactions of the groups described above with particular amino acid residues in the H1-H2 domains of Na+,K+-ATPase. Some interactions are the classical ones already described in the literature; a new, very strong interaction of the basic group with the Cys138 was found and adds new possibilities to design compounds interacting with this region of the receptor. The most interesting compounds were also studied in vivo in the anesthetized guinea pig for evaluating their inotropic effect versus the lethal dose. Compounds 9 and 12 showed a slightly higher safety ratio than digoxin and deserve further evaluation.
Rapid synthesis of [18F]SR46349B, a potent and selective 5-HT2 receptor antagonist
Tan,Fowler,Ding,Schlyer
, p. 719 - 728 (2007/10/02)
F-18 labeled SR46349B, a highly potent and selective 5-HT2 receptor antagonist, was synthesized as a potential radioligand for PET studies of brain 5-HT2 receptors. Nucleophilic aromatic substitution of trans-1-(2-nitrophenyl)-3-(4-m
