Isothiocyanate compounds and isothiocyanate XPO1 protein inhibitor drugs thereof
AssigneeDRIVINGFORCE THERAPEUTICS Co., Ltd.
InventorYongliang Yang
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Abstract
The present invention provides an isothiocyanate compound and its application. The compound is an aryl-substituted isothiocyanate compound that has a structure of the general formula I. The isothiocyanate compound of the present invention has very good solubility in water, far better inhibitory activity for XPO1 protein than other non-aryl substituted congeneric compounds, little side effects, and good biological safety and bioavailability, and is quite suitable for clinical application. Therefore, the isothiocyanate compound would have tremendous potential market space and economic benefits.
Claims5
An isothiocyanate compound of formula I:
- wherein R is selected from phenyl, a five- to six-membered mononuclear heteroaryl including 1-3 heteroatoms each independently selected from nitrogen, oxygen or sulfur, an eight- to ten-membered dinuclear aryl, an eight- to ten-membered dinuclear heteroaryl including 1-4 heteroatoms each independently selected from nitrogen, oxygen or sulfur, a ten- to fourteen-membered trinuclear aryl, or a ten- to fourteen-membered trinuclear heteroaryl including 1-4 heteroatoms each independently selected from nitrogen, oxygen or sulfur;
- wherein R is unsubstituted, or is optionally substituted with one or more independently selected W substituents,
- wherein the W substituent is selected from halogen, C1-4 alkoxy, C1-4 haloalkyl, a five- to six-membered mononuclear heteroaryl including 1-3 heteroatoms, each independently selected from nitrogen, oxygen or sulfur, a four- to seven-membered heterocycloalkyl, including 1-3 heteroatoms, each independently selected from nitrogen, oxygen or sulfur, or an eight- to ten-membered dinuclear heteroaryl including 1-4 heteroatoms, each independently selected from nitrogen, oxygen or sulfur;
- and
- wherein n is 0, 1 or 2.
Dependencies are inferred from the claim text.