C07D453/06

TETRAHYDROISOQUINOLINES AS SELECTIVE NADPH OXIDASE 2 INHIBITORS

Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein “custom-character” represents a single or double bond, R.sup.1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.a is hydrogen, —CH.sub.2R.sup.2, R.sup.3, or —SO.sub.2R.sup.4; R.sup.2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.4 is lower aliphatic, or substituted or unsubstituted aryl; and R.sup.5 is hydrogen, halogen, or lower aliphatic.

TETRAHYDROISOQUINOLINES AS SELECTIVE NADPH OXIDASE 2 INHIBITORS

Embodiments of bridged tetrahydroisoquinolines and methods for their use in selectively inhibiting nicotinamide adenine dinucleotide phosphate (NADPH) oxidase 2 are disclosed. The disclosed compounds have a structure according to general formula I or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein “custom-character” represents a single or double bond, R.sup.1 is hydrogen, halogen, lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.a is hydrogen, —CH.sub.2R.sup.2, R.sup.3, or —SO.sub.2R.sup.4; R.sup.2 is lower aliphatic, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.3 is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; R.sup.4 is lower aliphatic, or substituted or unsubstituted aryl; and R.sup.5 is hydrogen, halogen, or lower aliphatic.

COMPOSITIONS AND METHODS FOR PARASITE CONTROL

A compound of Formula I and formulations including such a compound may be used for the reduction of infestation with ectoparasites, in particular ectoparasites of the insect class, including fleas and mosquitoes, and/or ectoparasites of the arachnid class, including ticks and mites, etc. Methods for controlling ectoparasites and/or formulations including such compounds may include use as a repellent, and/or application to a mammal, e.g., a human, dog, cat, cattle, horse, or sheep, or to an object or a fabric. The form may be a topical formulation, a shampoo composition, a cleansing composition, or a treatment composition, preferably a lotion, cream, ointment, gel, foam, patch, powder, solid, sponge, tape, vapor, paste, tincture, or spray.

COMPOSITIONS AND METHODS FOR PARASITE CONTROL

A compound of Formula I and formulations including such a compound may be used for the reduction of infestation with ectoparasites, in particular ectoparasites of the insect class, including fleas and mosquitoes, and/or ectoparasites of the arachnid class, including ticks and mites, etc. Methods for controlling ectoparasites and/or formulations including such compounds may include use as a repellent, and/or application to a mammal, e.g., a human, dog, cat, cattle, horse, or sheep, or to an object or a fabric. The form may be a topical formulation, a shampoo composition, a cleansing composition, or a treatment composition, preferably a lotion, cream, ointment, gel, foam, patch, powder, solid, sponge, tape, vapor, paste, tincture, or spray.

Kv11.1-3.1 INHIBITING METHODS AND COMPOSITIONS

##STR00001##

Compounds of formula (I), formula (II), or formula (III) and their use with a neurological or psychiatric disorder, mediated by Kv11.1-3.1 containing potassium channels, including schizophrenia, are disclosed.

HPK1 ANTAGONISTS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

HPK1 ANTAGONISTS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

MUSCARINIC ACETYLCHOLINE M1 RECEPTOR ANTAGONISTS

Provided herein are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M.sub.1 (mAChR M.sub.1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

SUBSTITUTED 1,2,3,4,5,6-HEXAHYDROAZEPINO[4,5-b]INDOLES FOR TREATING BRAIN DISORDERS
20230117791 · 2023-04-20 ·

The present invention provides azepino-indoles and other heterocycles and methods of using the compounds for treating brain disorders.

METHODS AND COMPOSITIONS FOR MODULATING SPLICING
20230067064 · 2023-03-02 ·

Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.