C07C211/49

Serotonin 5-HT2A, 5-HT2B, and 5-HT2C Receptor Inverse Agonists
20240327353 · 2024-10-03 ·

4-phenyl-2-dimethylaminotetralin compounds, formulations, and methods are provided for selective modulation of serotonin 5-HT2A and 5-HT2C receptors without causing sedation at doses that are antipsychotic. Mechanisms for selective modulation are shown to involve inverse agonism at one or more of the 5-HT2A-2C receptors based on stereochemistry and substituents. The technology can be targeted to receptors inside or outside the central nervous system.

COMPOSITIONS AND METHODS FOR TREATING DISEASES AND CONDITIONS

A compound of Formula II, or a salt, ester, solvate, hydrate or prodrug thereof:

##STR00001##

where: X.sup.1 is a branched or unbranched C.sub.1-10 alkyl, (CH.sub.2).sub.sNH(CH.sub.2).sub.t, (CH.sub.2).sub.sO(CH.sub.2).sub.t, or (CH.sub.2).sub.sC(NH.sub.2)(CH.sub.2).sub.vNH(CH.sub.2).sub.t, where s, t and v are each, independently an integer from 1 to 5; A and B are each, independently, C.sub.6-10aryl, C.sub.6-10aryl-C.sub.1-6alkyl, C.sub.3-9 heteroaryl, or C.sub.3-9heteroaryl-C.sub.1-6alkyl, each optionally substituted with 1, 2 or 3 independently selected R.sup.g groups; C and D are each, independently, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-6alkyl, C.sub.3-7 heterocycloalkyl, C.sub.3-7 heterocycloalkyl-C.sub.1-6 alkyl, C.sub.6-10aryl, C.sub.6-10aryl-C.sub.1-6alkyl, C.sub.3-9 heteroaryl, or C.sub.3-9heteroaryl-C.sub.1-6alkyl, each optionally substituted with 1, 2 or 3 independently selected R.sup.g groups; each R.sup.g is, independently, halogen, C.sub.1-6 alkyl, C.sub.1-6 haloalkyl, hydroxyl, C.sub.1-6 alkoxy, C.sub.1-6 haloalkoxy, amino, C.sub.1-6 alkylamino, or di-C.sub.1-6alkylamino; and n.sup.1 and p.sup.1 are each, independently, integers from 1 to 10.

ORGANIC ELECTROLUMINESCENT DEVICE

An organic electroluminescent device of which emission life may be improved. The organic electroluminescent device includes an anode, an emission layer, and an anode-side hole transport layer provided between the anode and the emission layer and including an anode-side hole transport material. An electron accepting material is doped in the anode-side hole transport layer. An intermediate hole transport material layer is provided between the anode-side hole transport layer and the emission layer and includes an intermediate hole transport material, and an emission layer-side hole transport layer is provided between the intermediate hole transport material layer and the emission layer and adjacent to the emission layer. The emission layer-side hole transport layer includes an emission layer-side hole transport material represented by the following Formula 1.

##STR00001##

ORGANIC ELECTROLUMINESCENT DEVICE

An organic electroluminescent device of which emission life may be improved. The organic electroluminescent device includes an anode, an emission layer, and an anode-side hole transport layer provided between the anode and the emission layer and including an anode-side hole transport material. An electron accepting material is doped in the anode-side hole transport layer. An intermediate hole transport material layer is provided between the anode-side hole transport layer and the emission layer and includes an intermediate hole transport material, and an emission layer-side hole transport layer is provided between the intermediate hole transport material layer and the emission layer and adjacent to the emission layer. The emission layer-side hole transport layer includes an emission layer-side hole transport material represented by the following Formula 1.

##STR00001##

Tertiary amines for use in the treatment of cardiac disorders

The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure.

Tertiary amines for use in the treatment of cardiac disorders

The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure.

Cycloproplyamine derivatives useful as inhibitors of histone demethylases KDM1A

The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R.sup.1, and R.sup.2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy. ##STR00001##

Cycloproplyamine derivatives useful as inhibitors of histone demethylases KDM1A

The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R.sup.1, and R.sup.2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy. ##STR00001##

Organic electroluminescent device

An organic electroluminescent device of which emission life may be improved. The organic electroluminescent device includes an anode, an emission layer, and an anode-side hole transport layer provided between the anode and the emission layer and including an anode-side hole transport material. An electron accepting material is doped in the anode-side hole transport layer. An intermediate hole transport material layer is provided between the anode-side hole transport layer and the emission layer and includes an intermediate hole transport material, and an emission layer-side hole transport layer is provided between the intermediate hole transport material layer and the emission layer and adjacent to the emission layer. The emission layer-side hole transport layer includes an emission layer-side hole transport material represented by the following Formula 1. ##STR00001##

Organic electroluminescent device

An organic electroluminescent device of which emission life may be improved. The organic electroluminescent device includes an anode, an emission layer, and an anode-side hole transport layer provided between the anode and the emission layer and including an anode-side hole transport material. An electron accepting material is doped in the anode-side hole transport layer. An intermediate hole transport material layer is provided between the anode-side hole transport layer and the emission layer and includes an intermediate hole transport material, and an emission layer-side hole transport layer is provided between the intermediate hole transport material layer and the emission layer and adjacent to the emission layer. The emission layer-side hole transport layer includes an emission layer-side hole transport material represented by the following Formula 1. ##STR00001##