Patent classifications
A61K31/444
Polycyclics as sigma receptor modulators
The present invention discloses a number of polycyclic amines that are useful as opioid receptor modulators. The compounds of the invention are useful in both therapeutic and diagnostic methods, including for treating pain, neurological disorders, cardiac disorders, bowel disorders, drug and alcohol addiction, drug overdose, urinary disorders, respiratory disorders, sexual dysfunction, psoriasis, graft rejection or cancer.
COMPOUNDS AND METHODS FOR THE TREATMENT OF MICROBIAL INFECTIONS
Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I):
##STR00001##
In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
COMPOUNDS AND METHODS FOR THE TREATMENT OF MICROBIAL INFECTIONS
Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I):
##STR00001##
In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
Substituted pyridines and methods of use
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
Substituted pyridines and methods of use
The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.
N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1),
##STR00001## wherein A.sup.1, Y and Z all represent rings.
N-(HETERO)ARYL, 2-(HETERO)ARYL-SUBSTITUTED ACETAMIDES FOR USE AS WNT SIGNALING MODULATORS
The present invention relates to methods for modulating the Wnt signaling pathway using compounds of Formula (1),
##STR00001## wherein A.sup.1, Y and Z all represent rings.
OCT3 ACTIVITY INHIBITOR CONTAINING IMIDAZOPYRIDINE DERIVATIVE AS ACTIVE COMPONENT, AND OCT3 DETECTION AGENT
To provide an OCT3 activity inhibitor having a different basic skeleton than that of conventional OCT3 activity inhibitors. This inhibitor of organic cation transporter 3 (OCT3) contains, as an active component, an imidazo[1,2-a]pyridine derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.
OCT3 ACTIVITY INHIBITOR CONTAINING IMIDAZOPYRIDINE DERIVATIVE AS ACTIVE COMPONENT, AND OCT3 DETECTION AGENT
To provide an OCT3 activity inhibitor having a different basic skeleton than that of conventional OCT3 activity inhibitors. This inhibitor of organic cation transporter 3 (OCT3) contains, as an active component, an imidazo[1,2-a]pyridine derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.
(S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOETHYL)-3-(METHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE COMPOSITIONS FOR PHARMACEUTICAL PREPARATIONS
The invention includes a granular composition comprising the active ingredient (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3- carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (5)-N-(3-(6-isopro-poxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-di-hydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide Form 1 HCl, about 10-30% (5)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base.