Patent classifications
C07D213/57
METHOD FOR AROMATIC FLUORINATION
Disclosed is a fluorination method comprising providing an aryl fluorosulfonate and a fluorinating reagent to a reaction mixture; and reacting the aryl fluorosulfonate and the fluorinating reagent to provide a fluorinated aryl species. Also disclosed is a fluorination method comprising providing, a salt comprising a cation and an aryloxylate, and SO.sub.2F.sub.2 to a reaction mixture; reacting the SO.sub.2F.sub.2 and the ammonium salt to provide a fluorinated aryl species. Further disclosed a fluorination method comprising providing a compound having the structure ArOH to a reaction mixture; where A is an aryl or heteroaryl; providing SO.sub.2F.sub.2 to the reaction mixture; providing a fluorinating reagent to the reaction mixture; reacting the SO.sub.2F.sub.2, the fluorinating reagent and the compound having the structure ArOH to provide a fluorinated aryl species having the structure ArF.
CAFFEIC ACID DERIVATIVES AND USES THEREOF
In one aspect, the present disclosure provides caffeic acid derivatives of the formula:
##STR00001##
wherein the variables are as defined herein. In another aspect, the present disclosure provides pharmaceutical compositions and methods of using of the compounds disclosed herein, including for the treatment of cancer.
CAFFEIC ACID DERIVATIVES AND USES THEREOF
In one aspect, the present disclosure provides caffeic acid derivatives of the formula:
##STR00001##
wherein the variables are as defined herein. In another aspect, the present disclosure provides pharmaceutical compositions and methods of using of the compounds disclosed herein, including for the treatment of cancer.
Mcl-1 modulating compounds for cancer treatment
The invention relates to compounds of formula (I), and to their therapeutic use in the treatment of cancer: ##STR00001## Wherein Y.sub.1, Y.sub.2, Ar.sub.1, Ar.sub.2, R.sub.1, R.sub.2, i, j, k, l are as defined in claim 1.
Mcl-1 modulating compounds for cancer treatment
The invention relates to compounds of formula (I), and to their therapeutic use in the treatment of cancer: ##STR00001## Wherein Y.sub.1, Y.sub.2, Ar.sub.1, Ar.sub.2, R.sub.1, R.sub.2, i, j, k, l are as defined in claim 1.
Compound and organic electronic device using the same
Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): ##STR00001##
Compound and organic electronic device using the same
Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): ##STR00001##
AMYLOID TARGETING AGENTS AND METHODS OF USING THE SAME
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
AMYLOID TARGETING AGENTS AND METHODS OF USING THE SAME
Provided herein is the design and synthesis of novel molecular rotor fluorophores useful for detection of amyloid or amyloid like proteins. The fluorophores are designed to exhibit enhanced fluorescence emission upon associating with amyloid or amyloid like proteins as compared to unbound compound. Also disclosed herein are methods for treating diseases associated with amyloid or amyloid like proteins.
Phenyl-sulfamoyl.benzoyc acids as ERAP1 modulators
The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or hydrate thereof, wherein: the group XY is NHSO.sub.2 or SO.sub.2NH; Z is a monocyclic aryl or heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, cycloalkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.1 is H or alkyl; R.sub.2 is selected from COOH and a tetrazolyl group; R.sub.3 is selected from H, C land alkyl; R.sub.4 is selected from H and halo; R.sub.5 is selected from H, alkyl, haloalkyl, SO.sub.2-alkyl, Cl, alkoxy, OH, CN, hydroxyalkyl, alkylthio, heteroaryl, cycloalkyl, heterocycloalkyl and haloalkoxy; R.sub.6 is H; R.sub.7 is selected from H, CN, haloalkyl, halo, SO.sub.2-alkyl, SO.sub.2NR.sub.12R.sub.13, heteroaryl, CONR.sub.10R.sub.11 and alkyl, wherein said heteroaryl group is optionally substituted by one or more substituents selected from alkyl, halo, alkoxy, CN, haloalkyl and OH; R.sub.8 is selected from H, alkyl, haloalkyl and halo; and R.sub.9 is H, alkyl or halo; R.sub.10 and R.sub.11 are each independently H or alkyl; and R.sub.12 and R.sub.13 are each independently H or alkyl. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology and related applications. Another aspect of the invention relates to compounds of formulae (1a) and (1b). ##STR00001##