Patent classifications
C07D295/16
AMINOXY ACID-BASED ANTIBACTERIAL COMPOUNDS AND METHODS THEREOF
The subject invention pertains to novel compounds, compositions containing the novel compounds, and methods for targeting gram-positive bacteria with the compounds or compositions of the subject invention. The subject invention further pertains to novel compounds, novel compositions, and methods for targeting gram-positive bacteria persister cells and gram-positive bacterial biofilms. The subject compounds and compositions can target gram-positive bacteria by modulating the proton motive force, calcium influx, autolysis, or any combination thereof. The novel compounds are synthetic, small molecules that can induce the death of gram-positive bacteria.
AMINOXY ACID-BASED ANTIBACTERIAL COMPOUNDS AND METHODS THEREOF
The subject invention pertains to novel compounds, compositions containing the novel compounds, and methods for targeting gram-positive bacteria with the compounds or compositions of the subject invention. The subject invention further pertains to novel compounds, novel compositions, and methods for targeting gram-positive bacteria persister cells and gram-positive bacterial biofilms. The subject compounds and compositions can target gram-positive bacteria by modulating the proton motive force, calcium influx, autolysis, or any combination thereof. The novel compounds are synthetic, small molecules that can induce the death of gram-positive bacteria.
Methods of treating heart failure
Methods of treating heart failure include administering to a subject having heart failure an effective amount of a triazole compound that is an agonist of the APJ receptor, a pharmaceutically acceptable salt of the compound, or a mixture thereof. Compounds particularly useful in such methods are provided herein.
DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
This invention is directed to compounds of formula (I):
##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE
This invention is directed to compounds of formula (I):
##STR00001##
where r, q, R, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b, R.sup.5c, R.sup.6a, R.sup.6b, R.sup.6c, R.sup.7, R.sup.8, and R.sup.9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A.sub.4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
Metabotropic Glutamate Receptor Positive Allosteric Modulators (PAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Metabotropic Glutamate Receptor Positive Allosteric Modulators (PAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Small molecules targeting androgen receptor nuclear localization and/or level in prostate cancer
A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: ##STR00001## wherein R.sup.20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R.sup.21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R.sup.22 is a moiety that includes at least one divalent amino radical; and R.sup.23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group.
COVALENT INHIBITORS OF KRAS G12C
Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
COVALENT INHIBITORS OF KRAS G12C
Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.