C07D211/52

N-BENZYL-N-ARYLSULFONAMIDE DERIVATIVE AND PREPARATION AND USE THEREOF

The invention provides an N-benzyl-N-arylsulfonamide derivative, which is an N-benzyl-N-arylsulfonamide compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof. The N-benzyl-N-arylsulfonamide derivative is obtained by condensing a substituted nitrobenzene with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B), reducing the nitro group to an amino group, and subjecting the amino group to reductive amination, sulfonamidation; or by subjecting a substituted nitrobenzene to nitro reduction, reductive amination and sulfonamidation, and condensing the resultant intermediate with 5- or 6-membered nitrogen-containing aliphatic heterocycle (the ring B). It has been experimentally demonstrated that the N-benzyl-N-arylsulfonamide derivative of the invention can specifically bind to Kv1.3 potassium channel and inhibit or decrease its activity, and is useful in the treatment of autoimmune diseases caused by abnormal activation of the Kv1.3 potassium channel in human or animals. The invention further provides a medicament or a pharmaceutical composition comprising the N-benzyl-N-arylsulfonamide derivative.

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ANTIBIOTIC AMMONIUM COMPOUNDS AND METHODS FOR THE TREATMENT OF BACTERIAL INFECTIONS

The present disclosure provides ammonium compounds, e.g., compounds according to Formula I as set forth herein, which are useful as antimicrobial agents. Methods for the treatment of bacterial infections and associated conditions, e.g., gastrointestinal conditions, are also described, as well as methods for altering the microbiome of subjects such as humans.

ANTIBIOTIC AMMONIUM COMPOUNDS AND METHODS FOR THE TREATMENT OF BACTERIAL INFECTIONS

The present disclosure provides ammonium compounds, e.g., compounds according to Formula I as set forth herein, which are useful as antimicrobial agents. Methods for the treatment of bacterial infections and associated conditions, e.g., gastrointestinal conditions, are also described, as well as methods for altering the microbiome of subjects such as humans.

Analogs of pridopidine, their preparation and use

This invention provides an isolated compound having the structure: ##STR00001##
or a salt thereof, processes for making the same and to compositions comprising pridopidine with these compounds.

Analogs of pridopidine, their preparation and use

This invention provides an isolated compound having the structure: ##STR00001##
or a salt thereof, processes for making the same and to compositions comprising pridopidine with these compounds.

Substituted 3-Dialkylaminomethyl-Piperidin-4-yl-Benzamides and Methods of Making and Using Same

The invention relates to certain substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides, and compositions comprising the same, which in certain embodiments are useful for treating and/or preventing pain in a subject in need thereof.

BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS
20210022978 · 2021-01-28 ·

The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na.sup.+K.sup.+2Cl.sup.-cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis.

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BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS
20210022978 · 2021-01-28 ·

The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na.sup.+K.sup.+2Cl.sup.-cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis.

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PIPERIDINYL- AND PIPERAZINYL-SUBSTITUTED HETEROAROMATIC CARBOXAMIDES AS MODULATORS OF GPR6

Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R.sup.4, R.sup.5, R.sup.8, R.sup.10, R.sup.11, X.sup.1, X.sup.2, X.sup.3, X.sup.9, X.sup.12, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.

PIPERIDINYL- AND PIPERAZINYL-SUBSTITUTED HETEROAROMATIC CARBOXAMIDES AS MODULATORS OF GPR6

Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R.sup.4, R.sup.5, R.sup.8, R.sup.10, R.sup.11, X.sup.1, X.sup.2, X.sup.3, X.sup.9, X.sup.12, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.