Provided herein are small molecule compounds and methods inhibiting human sulfotransferase 1A3 (SULT1A3) using these small molecule compounds. Methods of manufacturing and treatment are also disclosed.

Provided herein are small molecule compounds and methods inhibiting human sulfotransferase 1A3 (SULT1A3) using these small molecule compounds. Methods of manufacturing and treatment are also disclosed.

The present invention relates to compounds of formula (A), wherein Z is NR.sup.10 or O. These compounds represent novel acridinium and xanthylium salts having an unprecedented substituted heterocyclic core. They are useful as fluorescent dyes or precursors thereof in different applications including various imaging and sensing techniques, and, in particular, as photosensitizers and hereby preferably as photocatalysts. The present invention further relates to processes for preparing the inventive compounds via 1,5-organodimetallic reagents from double directed ortho-metalation reactions or combined halogen-metal exchange/directed ortho-metalation reactions. ##STR00001##

The present invention relates to compounds of formula (A), wherein Z is NR.sup.10 or O. These compounds represent novel acridinium and xanthylium salts having an unprecedented substituted heterocyclic core. They are useful as fluorescent dyes or precursors thereof in different applications including various imaging and sensing techniques, and, in particular, as photosensitizers and hereby preferably as photocatalysts. The present invention further relates to processes for preparing the inventive compounds via 1,5-organodimetallic reagents from double directed ortho-metalation reactions or combined halogen-metal exchange/directed ortho-metalation reactions. ##STR00001##

The disclosure relates to a radioisotope-labelled compound having a structure according to formula I, wherein a wavy line indicates a single bond between a non-nodal carbon atom of a polycyclic aromatic system and an R.sup.1 substituent selected from a hydrogen; a halogen; a hydroxy; a protected hydroxy; a C.sub.1-4 alkoxy; a nitro group; an amino group; an amino group having 1 hydrogen replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogens replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogen atoms replaced with C.sub.2-5 alkylene to form a heterocyclic ring; a chain C.sub.1-6 carbon group; a chain C.sub.1-6 carbon group having a substituent selected from a halogen, carboxyl, a formyl, and a C.sub.1-4 alkanesulfonic; a phenyl group; a phenyl group having 1-5 substituents independently selected from halogens, a chain C.sub.1-6 carbon, a halogenated chain C.sub.1-6 carbon substituent, a hydroxy, a protected hydroxy, a C.sub.1-4 alkoxy, and an amino group having 1-2 atoms of hydrogen replaced with C.sub.1-6 alkyl; wherein R.sup.2 is a chain aliphatic substituent having: a total of 1-16 carbon atoms, an atom of .sup.18F fluorine radioisotope replacing a hydrogen atom at one of the carbon atoms, and a —CH.sub.2 fragment as a terminal member of a chain, wherein the chain connects to one of a hydrogen, a phenyl group, and a phenyl group having 1-3 substituents selected from halogens and C.sub.1-6 alkyl, and wherein if the chain contains at least 2 carbon atoms and there is a bivalent link between the chain carbon atoms, then the bivalent link is selected from the group consisting of an oxygen atom —O—, a sulfur atom —S—, and a C.sub.3-6 cycloalkylene; wherein R.sup.3 and R.sup.4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to adjacent non-nodal carbon atoms of a B ring to form an aromatic C ring fused with an A and B ring system, having R.sup.1 substituents at non-nodal carbon atoms; wherein n is an integer of 9; wherein X.sup.− is a pharmaceutically acceptable counter ion selected from: an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkane carboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid, a hydrate thereof, and a solvate thereof.

##STR00001##

The disclosure relates to a radioisotope-labelled compound having a structure according to formula I, wherein a wavy line indicates a single bond between a non-nodal carbon atom of a polycyclic aromatic system and an R.sup.1 substituent selected from a hydrogen; a halogen; a hydroxy; a protected hydroxy; a C.sub.1-4 alkoxy; a nitro group; an amino group; an amino group having 1 hydrogen replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogens replaced with a C.sub.1-C.sub.6 alkyl group; an amino group having 2 hydrogen atoms replaced with C.sub.2-5 alkylene to form a heterocyclic ring; a chain C.sub.1-6 carbon group; a chain C.sub.1-6 carbon group having a substituent selected from a halogen, carboxyl, a formyl, and a C.sub.1-4 alkanesulfonic; a phenyl group; a phenyl group having 1-5 substituents independently selected from halogens, a chain C.sub.1-6 carbon, a halogenated chain C.sub.1-6 carbon substituent, a hydroxy, a protected hydroxy, a C.sub.1-4 alkoxy, and an amino group having 1-2 atoms of hydrogen replaced with C.sub.1-6 alkyl; wherein R.sup.2 is a chain aliphatic substituent having: a total of 1-16 carbon atoms, an atom of .sup.18F fluorine radioisotope replacing a hydrogen atom at one of the carbon atoms, and a —CH.sub.2 fragment as a terminal member of a chain, wherein the chain connects to one of a hydrogen, a phenyl group, and a phenyl group having 1-3 substituents selected from halogens and C.sub.1-6 alkyl, and wherein if the chain contains at least 2 carbon atoms and there is a bivalent link between the chain carbon atoms, then the bivalent link is selected from the group consisting of an oxygen atom —O—, a sulfur atom —S—, and a C.sub.3-6 cycloalkylene; wherein R.sup.3 and R.sup.4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to adjacent non-nodal carbon atoms of a B ring to form an aromatic C ring fused with an A and B ring system, having R.sup.1 substituents at non-nodal carbon atoms; wherein n is an integer of 9; wherein X.sup.− is a pharmaceutically acceptable counter ion selected from: an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkane carboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid, a hydrate thereof, and a solvate thereof.

##STR00001##

The present invention provides novel aclidinium salt of the formula (I) and a process for the production of the aclidinium salt.

##STR00001##

wherein R.sup.1 is C1-C6 alkyl or C1-C6 alkyloxy; R.sup.2 is hydrogen or C1-C6 alkyloxy; R.sup.3 is hydrogen, halogen, C1-C6 alkyl or C1-C6 alkyloxy; R.sup.4 is hydrogen, C1-C6 alkyloxy, halo C1-C6 alkyloxy or C1-C6 alkylamino; R.sup.5 is C1-C3 alkyl; and X.sup.− is an anion.

A deep-red light thermally activated delayed fluorescent material and a synthesizing method thereof, and an electroluminescent device are described. The deep-red light thermally activated delayed fluorescent material is a target compound reacted and synthesized by an electron donor and an electron acceptor. The target compound is a D-A molecular structure or a D-A-D molecular structure, wherein the electron acceptor is a planar electron acceptor with an ultra-low triplet state energy level, and a triplet state energy level of the target compound ranges from 1.0 to 2.0 eV. The synthesized deep-red light thermally activated delayed fluorescent material provides high electroluminescent performance, the synthesis efficiency thereof is improved, and the preparation of the highly efficient organic electroluminescent device is realized.

A deep-red light thermally activated delayed fluorescent material and a synthesizing method thereof, and an electroluminescent device are described. The deep-red light thermally activated delayed fluorescent material is a target compound reacted and synthesized by an electron donor and an electron acceptor. The target compound is a D-A molecular structure or a D-A-D molecular structure, wherein the electron acceptor is a planar electron acceptor with an ultra-low triplet state energy level, and a triplet state energy level of the target compound ranges from 1.0 to 2.0 eV. The synthesized deep-red light thermally activated delayed fluorescent material provides high electroluminescent performance, the synthesis efficiency thereof is improved, and the preparation of the highly efficient organic electroluminescent device is realized.

Hydrophilic, high quantum yield, chemiluminescent acridinium compounds with increased light output, improved stability, fast light emission and decreased non specific binding are disclosed. The chemiluminescent acridinium esters possess hydrophilic, branched, electron-donating functional groups at the C2 and/or C7 positions of the acridinium nucleus.