Abstract:
Disclosed herein are compounds having antiviral activity, and, in particular, an inhibitory activity on the replication of Respiratory Syncytial Virus (RSV). Druggable target sites, including Px, in the RSV N protein are disclosed, as well as compounds targeting Px. The compounds can be used to treat patients with RSV infection.
Abstract:
Novel NH-substituted fused triazoles are inhibitors of the bacterial enzyme S aureus methionyl t RNA synthetase and are of use in treating bacterial infections.
Abstract:
The present invention relates to resorcinol derivatives of formula I, in which R is a (C3-C8)cycloalkyl ring or a (C5-C8)cycloalkenyl ring substituted by one of -N(R )SO2(CHR )nR and (C1-C6)alkyIN(R )SO2(CHR )nR , wherein R , R and n are as defined in the claims, and their use as skin lightening agents.
Abstract:
This invention provides a method for visualizing cellular organelles using cellular organelle and/or cytoskeleton crystallizing agents (e.g. tetrazolium violet), a method for isolating cellular organelles using cellular organelle and/or cytoskeleton crystallizing agents, a method for detecting dehydrogenase inhibitors using cellular organelle and/or cytoskeleton crystallizing agents, a method for treating cancer in mammals through cellular-organelle-crystallization-induced-death (herein defined as "Cocid"), a method for treating cancer using Cocid inducing agents, pharmaceutical compositions containing a therapeutically effective amount of cocid inducing agents, and compositions containing Cocid inducing agents in combination with a pharmaceutically acceptable carrier, diluent or excipient. Said Cocid inducing agents with or without a pharmaceutically acceptable carrier, diluent or excipient, are used in combination with surgery and/or non-surgical anti-tumor treatments.
Abstract:
A synthesis for preparing a tetraamido-macrocyclic ligand, such as 5,6-Benzo-3,8,11,13-tetraoxo-2,2,9,9-tetramethyl-12,12-diethyl-1,4,7,10-tetraazacyclotridecane, H4, in greatly improved yield and in a commercially viable manner, comprising the steps of dissolving a quantity of a 1,2-bis(2-aminoalkanamido)benzene in a solution comprised of methylene chloride and ethyl acetate to yield a first reaction solution; dissolving a quantity of a malonyl dihalide in an ethyl acetate solution to yield a second reaction solution; adding the first reaction solution and the second reaction solution to a reaction vessel containing a third reaction solution comprised of refluxing ethyl acetate solution and an acid scavenger to form a reaction mixture; and isolating a solid product comprised of the tetraamido-macrocycle directly from the reaction mixture by filtration.
Abstract:
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of formulas (I), (II), their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs and solvates thereof inhibit farnesyl protein transferase which is an enzyme involved in ras oncogene expression.
Abstract:
The present invention provides a fused heteroaryl compound having a CaMKII inhibitory action, which is expected to be useful as an agent for the prophylaxis or treatment of cardiac diseases (particularly catecholaminergic polymorphic ventricular tachycardia, postoperative atrial fibrillation, heart failure, fatal arrhythmia) and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
Abstract:
The present invention relates to compound of formula (I), their method of preparation and use thereof in particular in the fields of optoelectronic, photonic, photovoltaics and biology.