Patent classifications
C07C235/40
CYCLOPROPANE ANALOGUES OF N-(TRANS-4-HYDROXYCYCLOHEXYL)-6-PHENYLHEXANAMIDE AND RELATED COMPOUNDS
The present disclosure relates to compounds of Formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing diseases, disorders, or conditions (e.g., associated with mitochondria).
CYCLOPROPANE ANALOGUES OF N-(TRANS-4-HYDROXYCYCLOHEXYL)-6-PHENYLHEXANAMIDE AND RELATED COMPOUNDS
The present disclosure relates to compounds of Formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof. The present disclosure also relates to uses of the compounds, e.g., in treating or preventing diseases, disorders, or conditions (e.g., associated with mitochondria).
Sirtuin modulating compounds and applications thereof
In one aspect, compounds modulating sirtuin activity are described herein. Sirtuin modulation by compounds described herein includes sirtuin activation and sirtuin inhibition. Modulation of sirtuin activity includes sirtuin activation and/or sirtuin inhibition. In some embodiments, a sirtuin modulating compound and/or salt thereof is of Formula I described herein.
Sirtuin modulating compounds and applications thereof
In one aspect, compounds modulating sirtuin activity are described herein. Sirtuin modulation by compounds described herein includes sirtuin activation and sirtuin inhibition. Modulation of sirtuin activity includes sirtuin activation and/or sirtuin inhibition. In some embodiments, a sirtuin modulating compound and/or salt thereof is of Formula I described herein.
AMIDE DERIVATIVES OF POLYCAFFEOYLQUINIC ACIDS, PROCESS FOR PRODUCING SAME AND USES THEREOF
The present invention thus relates to amide derivatives of polysubstituted quinic acids (abbreviated to QPS), of general formula (IA): (IA), in which R.sub.1A and R.sub.2A are, independently of one another: H, with the proviso that R.sub.1A and R.sub.2A are not both a hydrogen atom, a butyl group, a C.sub.7-C.sub.30 alkyl group, a C.sub.7-C.sub.30 alkylaryl or arylalkyl group, or a C.sub.7-C.sub.18 aryl group; and Q.sub.1, Q.sub.3, Q.sub.4 and Q.sub.5 are, independently of one another, an OH, caffeoyl, maloyl, caffeoylmaloyl ou maloylcaffeoyl group, with the proviso that at least one of these radicals is not an OH group, or to a pharmaceutically acceptable salt or stereoisomer or hydrate thereof, and also to the process for producing same, to the use thereof as a medicament, in particular for the treatment and/or prevention of inflammation and of inflammatory diseases, and to the pharmaceutical, cosmetic and nutraceutical compositions containing same.
AMIDE DERIVATIVES OF POLYCAFFEOYLQUINIC ACIDS, PROCESS FOR PRODUCING SAME AND USES THEREOF
The present invention thus relates to amide derivatives of polysubstituted quinic acids (abbreviated to QPS), of general formula (IA): (IA), in which R.sub.1A and R.sub.2A are, independently of one another: H, with the proviso that R.sub.1A and R.sub.2A are not both a hydrogen atom, a butyl group, a C.sub.7-C.sub.30 alkyl group, a C.sub.7-C.sub.30 alkylaryl or arylalkyl group, or a C.sub.7-C.sub.18 aryl group; and Q.sub.1, Q.sub.3, Q.sub.4 and Q.sub.5 are, independently of one another, an OH, caffeoyl, maloyl, caffeoylmaloyl ou maloylcaffeoyl group, with the proviso that at least one of these radicals is not an OH group, or to a pharmaceutically acceptable salt or stereoisomer or hydrate thereof, and also to the process for producing same, to the use thereof as a medicament, in particular for the treatment and/or prevention of inflammation and of inflammatory diseases, and to the pharmaceutical, cosmetic and nutraceutical compositions containing same.
AMIDE DERIVATIVES OF POLYCAFFEOYLQUINIC ACIDS, PROCESS FOR PRODUCING SAME AND USES THEREOF
The present invention thus relates to amide derivatives of polysubstituted quinic acids (abbreviated to QPS), of general formula (IA): (IA), in which R.sub.1A and R.sub.2A are, independently of one another: H, with the proviso that R.sub.1A and R.sub.2A are not both a hydrogen atom, a butyl group, a C.sub.7-C.sub.30 alkyl group, a C.sub.7-C.sub.30 alkylaryl or arylalkyl group, or a C.sub.7-C.sub.18 aryl group; and Q.sub.1, Q.sub.3, Q.sub.4 and Q.sub.5 are, independently of one another, an OH, caffeoyl, maloyl, caffeoylmaloyl ou maloylcaffeoyl group, with the proviso that at least one of these radicals is not an OH group, or to a pharmaceutically acceptable salt or stereoisomer or hydrate thereof, and also to the process for producing same, to the use thereof as a medicament, in particular for the treatment and/or prevention of inflammation and of inflammatory diseases, and to the pharmaceutical, cosmetic and nutraceutical compositions containing same.
Screening methods for the binding affinity of chemical entities to biological molecules and NEDD4-1 inhibitors identified by the screening methods
Disclosed are methods for preparing and screening for an inhibitor of the activity of a biological molecule having a catalytic or non-catalytic cysteine residue. The methods including preparing a library of candidate inhibitor molecules by conjugating an electrophile to a plurality of drug molecules where the library of candidate inhibitor molecules thus formed react with cysteine residues. The library of candidate inhibitor molecules then may be reacted with the biological molecule to identify those inhibitor molecule that react with the catalytic or non-catalytic cysteine residue of the biological molecule in order to identify an inhibitor of the biological molecule.
Screening methods for the binding affinity of chemical entities to biological molecules and NEDD4-1 inhibitors identified by the screening methods
Disclosed are methods for preparing and screening for an inhibitor of the activity of a biological molecule having a catalytic or non-catalytic cysteine residue. The methods including preparing a library of candidate inhibitor molecules by conjugating an electrophile to a plurality of drug molecules where the library of candidate inhibitor molecules thus formed react with cysteine residues. The library of candidate inhibitor molecules then may be reacted with the biological molecule to identify those inhibitor molecule that react with the catalytic or non-catalytic cysteine residue of the biological molecule in order to identify an inhibitor of the biological molecule.
TERTIARY AMIDES AND METHOD OF USE
Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein G.sup.1, G.sup.2, G.sup.3, L.sup.1, L.sup.2, and L.sup.3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by the modulation of lysophosphatidic acid receptor 1. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
##STR00001##