C07D277/48

AROMATIC 5-MEMBERED HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY
20170066759 · 2017-03-09 ·

The present invention is related to a compound represented by formula (I)

##STR00001##

wherein R.sup.1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is N(R.sup.3), O, or S; Y is C(R.sup.4), or N; Z is N(R.sup.7), O, or S; R.sup.2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: (CR.sup.2aR.sup.2b).sub.nR.sup.2c, wherein R.sup.2a is each independently a hydrogen atom, halogen, or the like; R.sup.2b is each independently a hydrogen atom, halogen, or the like; R.sup.2a and R.sup.2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R.sup.2a which are attached to the adjacent carbon atoms and/or two of R.sup.2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R.sup.2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R.sup.3 and R.sup.7 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; R.sup.4 and R.sup.5 are each independently a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like; R.sup.6 is a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like,
or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.

GUANIDINE COMPOUNDS AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I

##STR00001##

corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

GUANIDINE COMPOUNDS AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS

The present invention relates to guanidine compounds of the general formula I

##STR00001##

corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.

Alkylamidothiazoles, cosmetic or dermatological preparations containing said alkylamidothiazoles, and use thereof to combat or prevent undesired pigmentation of the skin

Alkylamidothiazoles of general formula (I), wherein R 1=C1-C24 alkyl (linear and branched), C1-C24 alkenyl (linear and branched), C1-C8 cycloalkyl, C1-C8 cycloalkyl-alkylhydroxy, C1-C24 alkylhydroxy (linear and branched), C1-C24 alkylamine (linear and branched), C1-C24 alkylaryl (linear and branched), C1-C24 alkylaryl-alkyl-hydroxy (linear and branched), C1-C24 alkyl-heteroaryl (linear and branched), C1-C24-alkyl-OC1-C24-alkyl (linear and branched), C1-C24 alkyl morpholino, C1-C24 alkyl piperidino, C1-C24 alkyl piperazino, C1-C24 alkyl-piperazino-N-alkyl, as well as cosmetic or dermatological preparations having an effective content of one or more alkylamidothiazoles, as well as the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation. ##STR00001##

Alkylamidothiazoles, cosmetic or dermatological preparations containing said alkylamidothiazoles, and use thereof to combat or prevent undesired pigmentation of the skin

Alkylamidothiazoles of general formula (I), wherein R 1=C1-C24 alkyl (linear and branched), C1-C24 alkenyl (linear and branched), C1-C8 cycloalkyl, C1-C8 cycloalkyl-alkylhydroxy, C1-C24 alkylhydroxy (linear and branched), C1-C24 alkylamine (linear and branched), C1-C24 alkylaryl (linear and branched), C1-C24 alkylaryl-alkyl-hydroxy (linear and branched), C1-C24 alkyl-heteroaryl (linear and branched), C1-C24-alkyl-OC1-C24-alkyl (linear and branched), C1-C24 alkyl morpholino, C1-C24 alkyl piperidino, C1-C24 alkyl piperazino, C1-C24 alkyl-piperazino-N-alkyl, as well as cosmetic or dermatological preparations having an effective content of one or more alkylamidothiazoles, as well as the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation. ##STR00001##

SMALL MOLECULE SIRTUIN INHIBITORS AND USES THEREOF
20250276953 · 2025-09-04 ·

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a 2-hydroxybenzoic acid structure which function as sirtuin (e.g., SIRT1, SIRT2, SIRT3, SIRT4, SIRT5, SIRT6, SIRT7) inhibitors and/or degraders which function as effective therapeutic agents for treating, ameliorating, and preventing disorders associated with sirtuin activity (e.g., melanoma, Ewing sarcoma, malignant peripheral nerve sheath tumor, non-small cell lung cancer). In addition, this invention also relates to a new class of proteolysis-targeting chimeras (PROTACs) (as defined herein) which function as sirtuin inhibitors and/or degraders within cancer and/or immune cells. Pharmaceutical compositions comprising said compounds are also within the scope of the present invention.

SMALL MOLECULE SIRTUIN INHIBITORS AND USES THEREOF
20250276953 · 2025-09-04 ·

This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a 2-hydroxybenzoic acid structure which function as sirtuin (e.g., SIRT1, SIRT2, SIRT3, SIRT4, SIRT5, SIRT6, SIRT7) inhibitors and/or degraders which function as effective therapeutic agents for treating, ameliorating, and preventing disorders associated with sirtuin activity (e.g., melanoma, Ewing sarcoma, malignant peripheral nerve sheath tumor, non-small cell lung cancer). In addition, this invention also relates to a new class of proteolysis-targeting chimeras (PROTACs) (as defined herein) which function as sirtuin inhibitors and/or degraders within cancer and/or immune cells. Pharmaceutical compositions comprising said compounds are also within the scope of the present invention.