Patent classifications
C07F9/62
ISOQUINOLINONE COMPOUND FOR INHIBITING SSAO/VAP-1, AND USE THEREOF
An isoquinolinone compound acts as an inhibitor of semicarbazide-sensitive oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1), and the use thereof, and further relates to a pharmaceutical composition containing the compound. The compound or the pharmaceutical composition can be used to prepare a drug for preventing, treating or ameliorating inflammation and/or inflammation-related diseases, diabetes and/or diabetes-related diseases in patients, and especially can be used to prepare a drug for preventing, treating or ameliorating non-alcoholic fatty liver diseases in patients.
COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.
Photo-cleavable primer compositions and methods of use
In one embodiment, the present application discloses a photo-cleavable surface binding compound of the Formula I and Formula II: ##STR00001##
wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound.
Photo-cleavable primer compositions and methods of use
In one embodiment, the present application discloses a photo-cleavable surface binding compound of the Formula I and Formula II: ##STR00001##
wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound.
SURFACE PRIMER COMPOSITIONS AND METHODS OF USE
In one embodiment, the present application discloses a surface binding compound of the Formula I or Formula II:
##STR00001##
wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound of the Formula I or Formula II.
SURFACE PRIMER COMPOSITIONS AND METHODS OF USE
In one embodiment, the present application discloses a surface binding compound of the Formula I or Formula II:
##STR00001##
wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound of the Formula I or Formula II.
STAT6 inhibitors
The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.
STAT6 inhibitors
The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer.
Surface primer compositions and methods of use
In one embodiment, the present application discloses a surface binding compound of the Formula I or Formula II: ##STR00001##
wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound of the Formula I or Formula II.
Surface primer compositions and methods of use
In one embodiment, the present application discloses a surface binding compound of the Formula I or Formula II: ##STR00001##
wherein the variables EG, EG1, SP1, SP2, SP3, Ar and BG are as defined herein. In another embodiment, the application discloses a method for forming a coating on a surface of a substrate using the surface binding compound of the Formula I or Formula II.