C07D491/08

TRPML MODULATORS

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

INHIBITORS OF GLYCOGEN SYNTHASE 1 (GYS1) AND METHODS OF USE THEREOF

Provided herein are compounds of formula (I′):

##STR00001##

or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y.sup.2, Y.sup.3, L.sup.1, L.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Q.sup.1, R.sup.1, R.sup.2, R.sup.k, R.sup.m, and R.sup.n are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I′). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

INHIBITORS OF GLYCOGEN SYNTHASE 1 (GYS1) AND METHODS OF USE THEREOF

Provided herein are compounds of formula (I′):

##STR00001##

or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y.sup.2, Y.sup.3, L.sup.1, L.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Q.sup.1, R.sup.1, R.sup.2, R.sup.k, R.sup.m, and R.sup.n are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I′). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.

CYCLIC PEPTIDE COMPOUND HAVING KRAS INHIBITORY ACTION

The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.

Pyrazole MAGL inhibitors

Provided herein are pyrazole compounds and pharmaceutical compositions comprising the same. The compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the compounds and compositions are useful for the treatment of pain.

Pyrazole MAGL inhibitors

Provided herein are pyrazole compounds and pharmaceutical compositions comprising the same. The compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the compounds and compositions are useful for the treatment of pain.

MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

NAMPT MODULATORS

Provided are compounds of Formula (II) or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and p are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.

##STR00001##

NAMPT MODULATORS

Provided are compounds of Formula (II) or a pharmaceutically acceptable salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and p are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.

##STR00001##

SOS1 INHIBITORS

The present invention relates to methods of treating cancer using compounds that inhibit Son of sevenless homolog 1 (SOS1) activity and pharmaceutical compositions containing such compounds.