C07D257/04

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

Provided herein is a compound of Formula (1-I): or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.11a, R.sup.11b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.18, X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (1-I) and methods of using the compounds, e.g, in the treatment of CNS-related disorders.

##STR00001##

Compounds with antimicrobial activity

This invention relates to compounds of formula 1, 2 or 3 ##STR00001##
a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

Compounds with antimicrobial activity

This invention relates to compounds of formula 1, 2 or 3 ##STR00001##
a pharmaceutically acceptable salt, or solvate thereof, wherein X.sub.1, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. The compounds are antimicrobial agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1, 2 or 3.

Anti-fibrotic compounds

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

Anti-fibrotic compounds

Provided herein are anti-fibrotic compounds, in particular those of Formula (I), that inhibit the TGF-beta signaling pathway. Also provided are pharmaceutical compositions comprising the anti-fibrotic compounds, and methods of treating diseases or conditions associated with fibrosis, inflammation, and benign or malignant neoplastic diseases in a subject by administering a compound or composition described herein.

Small Molecule Activators of Parkin Enzyme Function

The present disclosure relates to compounds for activating the enzymatic activity of an E3 ubiquitin ligase and methods for treating a disease or disorder in a subject with diminished E3 ubiquitin ligase enzymatic activity. In some embodiments, the present disclosure provides a compound of Formula I

##STR00001##

or a compound of Formula II.

##STR00002##

or pharmaceutically acceptable salts thereof.

Small Molecule Activators of Parkin Enzyme Function

The present disclosure relates to compounds for activating the enzymatic activity of an E3 ubiquitin ligase and methods for treating a disease or disorder in a subject with diminished E3 ubiquitin ligase enzymatic activity. In some embodiments, the present disclosure provides a compound of Formula I

##STR00001##

or a compound of Formula II.

##STR00002##

or pharmaceutically acceptable salts thereof.

LIPOSOMAL FORMULATIONS COMPRISING AT1 RECEPTOR BLOCKERS AND USES THEREOF
20230129331 · 2023-04-27 ·

The present disclosure provides liposomal formulations comprising a lipid membrane comprising at least one liposome forming phospholipid and a sterol; and an intraliposomal aqueous compartment encapsulating at least one ATI receptor blocker (ARB) and a pH-dependent ionizable anion; with the liposomes having an effect upon administration to a subject in need of said effect, without causing a reduction in mean blood pressure of said subject of more than 50% as compared to the administration of the same amount of ARB in free form. The liposomes can be for systemic administration, e.g. by injection or for pulmonary administration, e.g. by inhalation

LIPOSOMAL FORMULATIONS COMPRISING AT1 RECEPTOR BLOCKERS AND USES THEREOF
20230129331 · 2023-04-27 ·

The present disclosure provides liposomal formulations comprising a lipid membrane comprising at least one liposome forming phospholipid and a sterol; and an intraliposomal aqueous compartment encapsulating at least one ATI receptor blocker (ARB) and a pH-dependent ionizable anion; with the liposomes having an effect upon administration to a subject in need of said effect, without causing a reduction in mean blood pressure of said subject of more than 50% as compared to the administration of the same amount of ARB in free form. The liposomes can be for systemic administration, e.g. by injection or for pulmonary administration, e.g. by inhalation

Compounds which are inhibitors of Notum

A compound for use in the treatment of a disease ameliorated by the inhibition of Notum of formula (I): (I) ##STR00001##