C07D213/61

Kappa opioid agonists and uses thereof

Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. ##STR00001## The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. Kappa opioid agonists that exhibit full agonist properties at the kappa opioid receptor have been widely shown to be efficacious in preclinical models of pain, particularly visceral pain.

Kappa opioid agonists and uses thereof

Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof. ##STR00001## The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. Kappa opioid agonists that exhibit full agonist properties at the kappa opioid receptor have been widely shown to be efficacious in preclinical models of pain, particularly visceral pain.

Sulfonamide derivative or pharmaceutically acceptable acid addition salt thereof
09815787 · 2017-11-14 · ·

The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) ##STR00001##
wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Sulfonamide derivative or pharmaceutically acceptable acid addition salt thereof
09815787 · 2017-11-14 · ·

The present invention aims to provide a novel low-molecular-weight compound having an orexin agonist activity, which is expected to be useful as a superior agent for the treatment or prophylaxis of narcolepsy. The present invention provides a compound showing superior orexin agonist activity which is represented by the formula (I) ##STR00001##
wherein each symbol is as defined in the DESCRIPTION, and a pharmaceutically acceptable acid addition salt thereof, as well as an orexin agonist containing the compound or a pharmaceutically acceptable acid addition salt thereof.

Organic light emitting element

Provided is an organic light emitting element having stable performance in the air. The organic light emitting element includes: an anode; a cathode; and a first organic compound layer placed between the anode and the cathode, in which: the organic light emitting element further includes a first organic compound layer placed between the cathode and the emission layer, and a second organic compound layer placed between the emission layer and the first organic compound layer, and brought into contact with the first organic compound layer; the first organic compound layer contains a first organic compound; the second organic compound layer contains a second organic compound; and the first organic compound includes an organic compound represented by the following general formula [1], and the second organic compound includes an organic compound different from the first organic compound ##STR00001##

Organic light emitting element

Provided is an organic light emitting element having stable performance in the air. The organic light emitting element includes: an anode; a cathode; and a first organic compound layer placed between the anode and the cathode, in which: the organic light emitting element further includes a first organic compound layer placed between the cathode and the emission layer, and a second organic compound layer placed between the emission layer and the first organic compound layer, and brought into contact with the first organic compound layer; the first organic compound layer contains a first organic compound; the second organic compound layer contains a second organic compound; and the first organic compound includes an organic compound represented by the following general formula [1], and the second organic compound includes an organic compound different from the first organic compound ##STR00001##

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:

##STR00001##

wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:

##STR00001##

wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

HERBICIDAL COMPOUNDS

The present invention relates to a compound of formula (I) wherein: wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

##STR00001##

Method for producing 2,3-dichloro-5-(trichloromethyl)pyridine
09809543 · 2017-11-07 · ·

The present invention relates to a novel process for producing of 2,3-dichloro-5-(trichloromethyl)pyridine by using PCl as chlorinating agent at elevated temperature and pressure.