C07D215/42

CASPASE INHIBITORS AND METHODS OF USE THEREOF
20230250067 · 2023-08-10 ·

Provided herein are compounds of formula I, compositions comprising the compounds and method of treating various diseases with the compounds and compositions.

COMPOUNDS FOR PREVENTING, INHIBITING, OR TREATING CANCER, AIDS AND/OR PREMATURE AGING

The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being:

##STR00001##

where: R independently represents a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a —CN group, a hydroxyl group, a —COOR.sub.1 group, a (C.sub.1-C.sub.3)fluoroalkyl group, a —NO.sub.2 group, a —NR.sub.1R.sub.2 group, or a (C.sub.1-C.sub.3)alkoxy group; R′ is a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a —NO.sub.2 group, a (C.sub.1-C.sub.3)alkoxy group, or a —NR.sub.1R.sub.2 group; and R.sub.1 and R.sub.2 are a hydrogen atom or a (C.sub.1-C.sub.3) alkyl group.

COMPOUNDS FOR PREVENTING, INHIBITING, OR TREATING CANCER, AIDS AND/OR PREMATURE AGING

The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being:

##STR00001##

where: R independently represents a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a —CN group, a hydroxyl group, a —COOR.sub.1 group, a (C.sub.1-C.sub.3)fluoroalkyl group, a —NO.sub.2 group, a —NR.sub.1R.sub.2 group, or a (C.sub.1-C.sub.3)alkoxy group; R′ is a hydrogen atom, a halogen atom, a (C.sub.1-C.sub.3)alkyl group, a —NO.sub.2 group, a (C.sub.1-C.sub.3)alkoxy group, or a —NR.sub.1R.sub.2 group; and R.sub.1 and R.sub.2 are a hydrogen atom or a (C.sub.1-C.sub.3) alkyl group.

DRUG CONJUGATE COMPRISING QUINOLINE DERIVATIVES

Disclosed are compounds having the formula (I):

##STR00001##

wherein R.sub.1 represents a group: —NH.sub.2, —NHCOR.sub.a, —NHCOOR.sub.b, —(C.sub.2-C.sub.6)alkenylene-CO—NH—OH, —(C.sub.2-C.sub.6)alkynylene-CO—NH—OH or —OH; R.sub.2 represents a group: —OCH.sub.3, —OCH.sub.2CH.sub.3, —SCH.sub.3, —SCH.sub.2CH.sub.3 or —OCHF.sub.2; R.sub.3 represents a hydrogen atom or a group: —CH.sub.3, —CN, —F, —Cl or —OR.sub.c; R.sub.4 represents a hydrogen atom or a group: —CH.sub.3, —CN, —F, —Cl or —OR.sub.d; R.sub.a represents a group: —(C.sub.1-C.sub.5)alkyl or —CF.sub.3; R.sub.b represents a group: —(C.sub.1-C.sub.5)alkyl or —CF.sub.3; R.sub.c represents a group: —(C.sub.1-C.sub.5)alkyl or —CF.sub.3; and R.sub.d represents a group: —(C.sub.1-C.sub.5)alkyl or —CF.sub.3; in the state of a base or acid or acid salts or base salts or in the form of hydrate or of solvate. Also disclosed are drug conjugates including such compounds.

Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase

Compounds of formula (VII), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pertaining to said compounds.

Compounds useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase

Compounds of formula (VII), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pertaining to said compounds.

Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof

Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A). ##STR00001##

Inhibitors of low molecular weight protein tyrosine phosphatase and uses thereof

Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A). ##STR00001##

Tetrahydroquinoline-based bromodomain inhibitors

In one aspect, compounds and compositions that modulate a bromodomain and methods of making and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with inhibition of a bromodomain such as, for example, cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Tetrahydroquinoline-based bromodomain inhibitors

In one aspect, compounds and compositions that modulate a bromodomain and methods of making and using same are disclosed. The disclosed compounds and compositions can be useful for disorders associated with inhibition of a bromodomain such as, for example, cancer. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.