C07D498/08

Fluoroalkyl-oxadiazoles and uses thereof

Provided herein are compounds identified as inhibitors of HDAC6 activity having the formula: ##STR00001##
or a pharmaceutically acceptable salt thereof, that can be used to treat various diseases and disorders.

Inhibitors of LRRK2 kinase

Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.

Inhibitors of LRRK2 kinase

Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.

Proteasome inhibitors

Unique compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.

NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

##STR00001##

NOVEL SUBSTITUTED PIPERAZINE AMIDE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.

##STR00001##

KRas G12C inhibitors

The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.

METHOD FOR PRODUCING 5-HYDROXYPIPERIDINE-2-CARBOXYLIC ACID

A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below:

##STR00001##

the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below:

##STR00002##

(wherein P represents a protecting group, R.sup.3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below:

##STR00003##

(wherein R.sup.3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).

METHOD FOR PRODUCING 5-HYDROXYPIPERIDINE-2-CARBOXYLIC ACID

A method for producing (2S,5S)/(2R,5R)-5-hydroxypiperidine-2-carboxylic acid represented by the formula (10) below:

##STR00001##

the method including removing the protecting group from the hydroxyl group in a compound represented by formula (7) below:

##STR00002##

(wherein P represents a protecting group, R.sup.3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms) to synthesize a compound represented by formula (8) below:

##STR00003##

(wherein R.sup.3 represents an alkyl group containing 1 to 4 carbon atoms, and A represents an alkyl group containing 1 to 10 carbon atoms, an aryl group containing 6 to 12 carbon atoms, an alkyloxy group containing 1 to 4 carbon atoms, or an aralkyloxy group containing 7 to 20 carbon atoms).

COVALENT INHIBITORS OF CDK-7
20180008604 · 2018-01-11 ·

The disclosure includes compounds of Formula (I)

##STR00001## wherein R.sub.0, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.