C07D223/06

QUATERNARY AMMONIUM SALT COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF
20210107872 · 2021-04-15 ·

A compound is shown in formula I and can be in the form of a pharmaceutically acceptable salt, or a stereoisomer, or a solvate, or a prodrug, or a metabolite. The compound takes effect rapidly and has a long-time local anesthetic effect following a single dose, with the sensory nerve blocking time being greater than the motor nerve blocking time, has both a long-acting local anesthetic effect and a selective local anesthetic effect, significantly reduces side effects of the compositions QX314 and QX314 and a quaternary ammonium salt compound with surfactant structural characteristics, and is safer. The compound of formula I of the present invention and a pharmaceutically acceptable salt thereof can be used for preparing drugs that have a long-time local anesthetic effect and a selective local anesthetic effect.

PRODRUG COMPOUNDS ACTIVATED BY AKR1C3 AND THEIR USE FOR TREATING HYPERPROLIFERATIVE DISORDERS

AKR1C3-activated prodrugs of Formula (I), pharmaceutical compositions comprising prodrugs of Formula (I), and their use in the treatment of hyperproliferative diseases such as cancer and for cell ablation. The compounds of the invention are able to penetrate neoplasm tissue and be selectively reduced to an active (cytotoxic) form by contact with an AKR1C3 enzyme found in the neoplasm. This active form is therefore able to ablate AKR1C3-expressing target cells of the neoplasm and therefore has particular utility in the treatment of cancer and other hyperproliferative disorders.

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Nitrogen and/or oxygen-containing hydrofluoroolefins and methods of making and using the same

The present invention relates to an unsaturated fluorinated ether or amine compound of formula (I) with low global warming potential and method of making the compound (I), where R.sub.H.sup.1 is and R.sub.H.sup.2 are independently selected from H or CH.sub.3, wherein when R.sub.H.sup.1 is CH.sub.3 then R.sub.H.sup.2 is H and when R.sub.H.sup.2 is CH.sub.3, then R.sub.H.sup.1 is H; X is O or N and when X is O, then n is 1 and R.sub.f is a linear or branched perfluorinated alkyl group comprising 1-10 carbon atoms and optionally comprising at least one catenated O or N atom; X is N, then n is 2 and (i) each R.sub.f is independently selected from a linear or branched perfluorinated alkyl group comprising 1-8 carbon atoms and optionally comprising at least one catenated O or N atom, or (ii) the two R.sub.f's are bonded together to form a ring structure optionally comprising at least one catenated O or N atom, wherein the ring of the ring structure consists of 5-7 atoms, no more than 10 carbon atoms, and is perfluorinated. The applications of the compound include solvent cleaning, electrolyte solvents or additives, heat transfer, and vapour phase soldering.

ADO-resistant cysteamine analogs and uses thereof

The present disclosure is directed to methods for treating diseases for which cysteamine is indicated and compounds useful in such methods.

ADO-resistant cysteamine analogs and uses thereof

The present disclosure is directed to methods for treating diseases for which cysteamine is indicated and compounds useful in such methods.

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

Inhibitors of HBV replication of Formula (I)

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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)

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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.

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I):

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wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the -position, wherein R.sup.2 may optionally be further substituted.

The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

NOVEL SULFONAMIDE CARBOXAMIDE COMPOUNDS

The present invention relates to compounds of formula (I):

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wherein Q is selected from O or S; R.sup.1 is a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein R.sup.1 is attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein R.sup.1 may optionally be substituted; and R.sup.2 is a cyclic group substituted at the -position, wherein R.sup.2 may optionally be further substituted.

The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

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

Inhibitors of HBV replication of Formula (I)

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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.