C07D243/08

Diamine Compound, Polyimide Precursor and Polyimide Film Using the Same, and Use Thereof
20220389165 · 2022-12-08 ·

Provided a diamine compound, a polyimide precursor and a polyimide film using the same, and a use thereof. The diamine compound may be very useful as a monomer for manufacturing a polyimide film having excellent transparency, high heat resistance, and low retardation.

Substituted pyrrolo[1,2-a]pyrazines and pyrrolo[1,2-a][1,4]diazepines as TREX1 inhibitors

The present invention provides compounds of Formula I: ##STR00001##
wherein ##STR00002##
X, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the TREX1 protein and thus can be used as medicaments for treating or preventing disorders affected by the inhibition of TREX1.

LIPID PARTICLE, COMPOSITION COMPRISING LIPID PARTICLE, AND METHOD FOR DERIVERING ACTIVATORS TO CELL

The present embodiment provides a compound represented by the formula (1):


Q-CHR.sub.2  (1)

(Q is a nitrogen-containing aliphatic group containing two or more tertiary nitrogens but no oxygen, and R is an aliphatic group containing a biodegradable group). From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

LIPID PARTICLE, COMPOSITION COMPRISING LIPID PARTICLE, AND METHOD FOR DERIVERING ACTIVATORS TO CELL

The present embodiment provides a compound represented by the formula (1):


Q-CHR.sub.2  (1)

(Q is a nitrogen-containing aliphatic group containing two or more tertiary nitrogens but no oxygen, and R is an aliphatic group containing a biodegradable group). From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.

Biphenyl compound or salt thereof

The present invention provides a compound represented by Formula (I) or a salt thereof; an LSD1 inhibitor that contains the compound or a salt thereof as an active ingredient; a pharmaceutical composition that contains the compound or a salt thereof; and an antitumor agent that contains the compound or a salt thereof as an active ingredient.

ROR-GAMMA-T INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF

An RORγt inhibitor, a preparation method thereof and uses thereof. The invention also relates to a pharmaceutical composition of the compound, a method for preparing the pharmaceutical composition, and use of the compound or the pharmaceutical composition in treating or preventing cancer, inflammation, or autoimmune diseases mediated by RORγt in mammals.

Prodrug compounds activated by AKR1C3 and their use for treating hyperproliferative disorders

AKR1C3-activated prodrugs of Formula (I), pharmaceutical compositions comprising prodrugs of Formula (I), and their use in the treatment of hyperproliferative diseases such as cancer and for cell ablation. The compounds of the invention are able to penetrate neoplasm tissue and be selectively reduced to an active (cytotoxic) form by contact with an AKR1C3 enzyme found in the neoplasm. This active form is therefore able to ablate AKR1C3-expressing target cells of the neoplasm and therefore has particular utility in the treatment of cancer and other hyperproliferative disorders. ##STR00001##

Methods and Compositions for Targeting Tregs using CCR8 Inhibitors
20230159446 · 2023-05-25 ·

The present invention provides compounds of Formula (I) which can be used as CCR8 inhibitors, which can be used as treatment or prevention of cancer using CCR8 inhibitors targeted tumor specific T regulatory cells.

##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##

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##