Patent classifications
A61K31/4192
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
MODULATORS OF THE INTEGRATED STRESS RESPONSE PATHWAY
##STR00001##
The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates, tautomers or stereoisomers thereof, wherein R.sup.1, R.sub.2, R.sup.2a, R.sup.3, R.sup.a1, R.sup.a2, R.sup.a3, R.sup.a4, R.sup.a5, R.sup.a6, A.sup.1 and A.sup.2 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising said compounds, their use as medicament and in a method for treating and preventing of one or more diseases or disorders associated with integrated stress response.
NEW INHIBITORS FOR THE KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION
Described herein are compounds, compositions and methods useful for inhibiting Kelch-like ECH-associated protein 1 (KEAP1). The compounds, compositions and methods described herein are useful for treating diseases, disorders or conditions associated with KEAP1.
NEW INHIBITORS FOR THE KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION
Described herein are compounds, compositions and methods useful for inhibiting Kelch-like ECH-associated protein 1 (KEAP1). The compounds, compositions and methods described herein are useful for treating diseases, disorders or conditions associated with KEAP1.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where X, R.sup.a, R.sup.b, R.sup.2, and R.sup.7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
Neprilysin inhibitors
In one aspect, the invention relates to compounds having the formula: ##STR00001##
where X, R.sup.a, R.sup.b, R.sup.2, and R.sup.7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
OX2R compounds
Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
OX2R compounds
Methods and compositions for agonizing a type-2 orexin receptor (OX2R) in a cell determined to be in need thereof, including the general method of (a) administering to a subject a cyclic guanidinyl OX2R agonist and (b) detecting a resultant enhanced wakefulness or increased resistance to diet-induced accumulation of body fat, or abbreviated recovery from general anesthesia or jet lag.
Hepatitis B antiviral agents
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof:
X-A-Y-L-R (I)
which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.