Patent classifications
C07D209/14
NOVEL PRODRUGS AND CONJUGATES OF DIMETHYLTRYPTAMINE
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.8, R.sub.9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.
##STR00001##
NOVEL PRODRUGS AND CONJUGATES OF DIMETHYLTRYPTAMINE
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.8, R.sub.9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.
##STR00001##
Small molecule inhibitors of Ebola and Lassa fever viruses and methods of use
Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g., Ebola), cancer and obesity: ##STR00001##
wherein A is N or CR.sup.8; Z is ##STR00002## E is selected from optionally substituted alkyl, cycloalkyl, arylalkyl, cycloalkylalkyl, amino, alkoxy, cycloalkyloxy, and cycloalkylamino; R.sup.1 is selected from optionally substituted aryl and heteroaryl, R.sup.2 and R.sup.3 are independently selected from H, deutero, optionally substituted alkyl, haloalkyl, or R.sup.2 and R.sup.3, together with the carbon to which they are bound, combine to form a carbonyl; and R.sup.8 is selected from H, deutero, halo, hydroxyl, cyano, amino, alkyl, alkoxy, carboxy, alkoxycarbonyl, and aminocarbonyl,
provided that E is not ##STR00003##
Small molecule inhibitors of Ebola and Lassa fever viruses and methods of use
Disclosed herein are compounds having a structure of formula (I), compositions and methods useful for the treatment of a disease or infection, such as a viral infection (e.g., Ebola), cancer and obesity: ##STR00001##
wherein A is N or CR.sup.8; Z is ##STR00002## E is selected from optionally substituted alkyl, cycloalkyl, arylalkyl, cycloalkylalkyl, amino, alkoxy, cycloalkyloxy, and cycloalkylamino; R.sup.1 is selected from optionally substituted aryl and heteroaryl, R.sup.2 and R.sup.3 are independently selected from H, deutero, optionally substituted alkyl, haloalkyl, or R.sup.2 and R.sup.3, together with the carbon to which they are bound, combine to form a carbonyl; and R.sup.8 is selected from H, deutero, halo, hydroxyl, cyano, amino, alkyl, alkoxy, carboxy, alkoxycarbonyl, and aminocarbonyl,
provided that E is not ##STR00003##
INHIBITORS OF NLRP3 INFLAMMASOME
The present disclosure relates to compounds that act as inhibitors of NLRP3 inflammasomes; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with inflammation and inflammaging, including hearing loss and other diseases associated with aging.
PSMA-targeting compounds and uses thereof
Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.
PSMA-targeting compounds and uses thereof
Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.
N-SUBSTITUTED INDOLES
Disclosed herein are compounds of the formula
##STR00001##
as well as methods for their use in treating neurologic and brain disorders.
Water soluble novel cyanine fluorophore with tunable properties between near IR and SWIR region for in vivo imaging
Cyanine fluorophores including a nine-carbon polymethine bridge are disclosed. The cyanine fluorophores have absorbance and/or emission maxima in the near-infrared (NIR) and short-wave infrared (SWIR) wavelength ranges. Methods of making and using the cyanine fluorophores are also disclosed. The compounds are useful in fluorescence imaging, more particularly in cancer treatment. The compounds have generic formula (I): ##STR00001##
Cyanine dyes
The invention provides a novel class of cyanine dyes that are functionalized with sulfonic acid groups and a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.