C07C311/16

Benzene disulfonamide for the treatment of cancer

The present invention relates to novel substituted benzene disulfonamides, as well as pharmaceutical compositions containing at least one of these substituted benzene disulfonamides together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said substituted benzene disulfonamides are binding to the prenyl binding pocket of PDE6 and therefore, are useful for the prophylaxis and treatment of cancer by inhibition of the binding of PDE6 to farnesylated Ras proteins and thereby, inhibition of oncogenic Ras signaling in cells.

TRNA SYNTHETASE INHIBITORS
20210053997 · 2021-02-25 ·

Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

DRUGS TO TREAT OCULAR DISORDERS

The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

DRUGS TO TREAT OCULAR DISORDERS

The present invention provides new prodrugs of therapeutically active loop diuretics, including oligomeric prodrugs, and compositions to treat medical disorders, for example, ocular disorders such as glaucoma, a disorder or abnormality related to an increase in intraocular pressure (IOP), a disorder requiring neuroprotection, age-related macular degeneration, or diabetic retinopathy.

IMAGING HISTONE DEACETYLASES WITH A RADIOTRACER USING POSITRON EMISSION TOMOGRAPHY

Disclosed herein are histone deacetylase imaging agents for positron emission tomography and related imaging methods using the histone deacetylase imaging agents. The histone deacetylase imaging agents may be a compound of formula (I):

##STR00001##

wherein R.sup.1 is a moiety including a positron emitter; R.sup.2 represents hydrogen, or substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and n is an integer selected from 0 or 1. In one version of the compound of formula (I), R.sup.1 is a moiety including an adamantyl group.

IMAGING HISTONE DEACETYLASES WITH A RADIOTRACER USING POSITRON EMISSION TOMOGRAPHY

Disclosed herein are histone deacetylase imaging agents for positron emission tomography and related imaging methods using the histone deacetylase imaging agents. The histone deacetylase imaging agents may be a compound of formula (I):

##STR00001##

wherein R.sup.1 is a moiety including a positron emitter; R.sup.2 represents hydrogen, or substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and n is an integer selected from 0 or 1. In one version of the compound of formula (I), R.sup.1 is a moiety including an adamantyl group.

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I)

##STR00001##

including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R.sub.1, R.sub.2 and R.sub.4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

SULFAMOYL-ARYLAMIDES AND THE USE THEREOF AS MEDICAMENTS FOR THE TREATMENT OF HEPATITIS B

Inhibitors of HBV replication of Formula (I)

##STR00001##

including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein B, R.sub.1, R.sub.2 and R.sub.4 have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.

HEAT SENSITIVE RECORDING MATERIAL AND COLOR DEVELOPER

The presently claimed invention relates to a color developer, a process for its manufacture and its use as a component in heat sensitive recording material. The heat sensitive recording material is useful for thermographic printing.

HEAT SENSITIVE RECORDING MATERIAL AND COLOR DEVELOPER

The presently claimed invention relates to a color developer, a process for its manufacture and its use as a component in heat sensitive recording material. The heat sensitive recording material is useful for thermographic printing.