Patent classifications
C07D213/58
Opioid receptor modulators and products and methods related thereto
Compounds are provided having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: ##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
3-SUBSTITUTED PHENYLAMIDINE COMPOUNDS, PREPARATION AND USE THEREOF
The present invention disclosed 3-substituted phenylamidine compounds of general formula (I), wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.4a, R.sup.4b, A and E have the same meanings as defined in description. The present invention further discloses methods for their preparation and use of the compounds of general formula (I) as a crop protection agent.
##STR00001##
INHIBITORS OF THE INTERACTION BETWEEN TRIP8B AND HCN CHANNELS AND USES THEREOF FOR TREATING NEUROLOGICAL DISEASES AND DISORDERS
Disclosed herein are substituted phenyl compounds of formula I as defined herein that may be utilized as inhibitors of the interaction between the subunits of hyperpolarization-activated cyclic-nucleotide gated (HCN) channels, such as HCN1, and an auxiliary subunit of HCN channels which is the tetratricopeptide repeat-containing Rab8b-interacting protein (TRIP8b). The disclosed compounds may be used in pharmaceutical compositions and methods for treating neurological diseases and disorders such as depression, and in particular Major Depressive Disorder (MDD).
INHIBITORS OF THE INTERACTION BETWEEN TRIP8B AND HCN CHANNELS AND USES THEREOF FOR TREATING NEUROLOGICAL DISEASES AND DISORDERS
Disclosed herein are substituted phenyl compounds of formula I as defined herein that may be utilized as inhibitors of the interaction between the subunits of hyperpolarization-activated cyclic-nucleotide gated (HCN) channels, such as HCN1, and an auxiliary subunit of HCN channels which is the tetratricopeptide repeat-containing Rab8b-interacting protein (TRIP8b). The disclosed compounds may be used in pharmaceutical compositions and methods for treating neurological diseases and disorders such as depression, and in particular Major Depressive Disorder (MDD).
GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:
##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO
GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:
##STR00001##
wherein R.sub.1a, R.sub.1b, R.sub.1c, R.sub.1d, R.sub.2, R.sub.2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO
Compounds are provided having the structure of Formula (I):
##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulare the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO
Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, B, L, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.8, m and n are as defined herein. Such compounds modulate the opioid receptor, particulate the mu-opioid receptor (MOR) and/or the kappa-opioid receptor (KOR), and/or the delta-opioid receptor (DOR). Products containing such compounds, as well as methods for their use and preparation, are also provided.
##STR00001##