摘要:
Disclosed are novel conjugates and methods for the preparation thereof. One of the methods for the preparation of a conjugate comprises a step of: acting a compound of formula (I), with a thiol-containing molecule of formula (II), wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, a small molecule, an optionally substituted C1-C8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).
摘要:
The present invention provides IP4-4,6 substituted derivatives, their methods of synthesis and their uses. In some aspects, the IP4-4,6 derivative is a compound of formula I wherein R1, R3, R7, and R11 are OPO32−, and R5 and R9 are selected from the group consisting of —O(Alkyl)nX, —O(Alkyl)yCy(Alkyl2)y-Z, —O(Alkyl)yA(Alkyl)y-Z′, and their thiophosphate analogs. Also provided are methods, pharmaceutical compositions and formulations, methods of use, articles of manufacture, and kits for the treatment of diseases and conditions such as pathological crystallization-related diseases and conditions.
摘要:
Compounds of general formula I are disclosed. The meaning of individual substituents is described in the claims. The compounds are useful in treatment of cancers, due to their multi-modal mechanism of action.
摘要:
The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.
摘要:
The invention relates to copper(I) complexes of the formula A, in which X*═Cl, Br, I, CN and/or SCN (i.e. independently of one another); N*∩E=a bidentate ligand where E=phosphanyl/arsenyl group of the R2E form (where R=alkyl, aryl, alkoxyl, phenoxyl, or amide); N*=imine function, which is part of a N-heteroaromatic 5- or 6-membered ring, which is chosen from the group consisting of oxazole, imidazole, thiazole, isoxazole, isothiazole, pyrazole, 1,2,3-triazole, 1,2,3-oxadiazole, 1,2,5-oxadiazole, 1,2,3-thiadiazole and 1,2,5-thiadiazole, pyridine, pyrimidine, triazine, pyrazine and pyridazine; and “∩”=at least one carbon atom, which is likewise part of the aromatic group, wherein the carbon atom is directly adjacent to both the imine nitrogen atom and to the phosphorous or arsenic atom.
摘要:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要:
Disclosed are a novel phosphorylating reagent and related methods. Specifically disclosed is a compound represented by general formula (A). In the formula, WG1 and WG2 independently represent a cyano group, a nitro group, a halogen atom, an alkylsulfonyl group or an arylsulfonyl group; X1, X2, X3 and X4 independently represent CR or N; and R represents H, a methyl group, a halogen atom, a trifluoromethyl group, a cyano group, a nitro group, an alkoxycarbonyl group, a carbamoyl group, a monoalkylcarbamoyl group, a dialkylcarbamoyl group, a sulfamoyl group, a monoalkylsulfamoyl group, a dialkylsulfamoyl group, or an alkylsulfonyl group.
摘要:
The invention relates to a compound of formula (I) and the salts, N-oxides, quaternary amines, and stereoisomers thereof, wherein R1 to R8 are as defined in the claims. The invention further relates to intermediates and methods for the preparation of the compounds of formula (I). The invention also relates to the compounds of formula (I) for use as a medicament, particularly for the prevention or treatment of fungal infections.
摘要:
The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
摘要:
Nucleotide phosphonate esters characterized by the presence of an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise an ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.