C07D211/56

Enantiomerically pure adamantane carboxamides for the treatment of filovirus infection

The compounds of the invention as shown by general structure I, as shown below, are effective in treating filovirus infections. ##STR00001## X is selected from the group consisting of O and H; R.sup.1 is selected from (C.sub.6 to C.sub.10) aryl and (C.sub.2 to C.sub.9) heteroaryl, and R.sup.2 is selected from (C.sub.1 to C.sub.10) alkyl, (C.sub.1 to C.sub.10) alkenyl, (C.sub.1 to C.sub.10) alkynyl, (C.sub.3 to C.sub.10) cycloalkyl, and (C.sub.5 to C.sub.10) cycloalkenyl, and NR.sup.3aR.sup.3b is defined in the specification. These compounds are effective in treating filovirii infections including Ebolavirus and Marburg virus.

TRANSCRIPTIONAL ENHANCED ASSOCIATE DOMAIN (TEAD) TRANSCRIPTION FACTOR INHIBITORS AND USES THEREOF

Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, compositions, and mixtures thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.

##STR00001##

TRANSCRIPTIONAL ENHANCED ASSOCIATE DOMAIN (TEAD) TRANSCRIPTION FACTOR INHIBITORS AND USES THEREOF

Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, compositions, and mixtures thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.

##STR00001##

YAP1 inhibitors that target the interaction of YAP1 with Oct4

Binding of the transcriptional co-activator, YAP1, to the transcription factor Oct4, induces Sox2, which is a transcription actor necessary for the self-renewal of stem-like cells from non-small cell lung cancer. The WW domain of YAP1 binds to the PPxY motif of Oct4 to induce Sox2. Delivering a peptide corresponding to the WW domain could prevent the induction of Sox2 and stemness. Similarly, peptides and mimetics of the PPxY motif would be able to inhibit sternness. Disclosed are compounds that affect the Yap1:Oct4 interaction.

Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation

The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation. ##STR00001##

Bicyclic compounds as inhibitors of PD1/PD-L1 interaction/activation

The compounds of Formula I is described herein along with their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof. The compounds described herein, their polymorphs, stereoisomers, tautomers, prodrugs, solvates, and pharmaceutically acceptable salts thereof are bicyclic compounds that are inhibitors of PD-1/PD-L1 interaction/activation. ##STR00001##

P2X7R ANTAGONISTS
20220380310 · 2022-12-01 ·

A compound has Formula I:

##STR00001##

R.sub.1 is hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, aryl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; L is a bond, a heterocyclic bivalent group, a heteroaromatic bivalent group, or an aromatic bivalent group; M is a bond, alkyl, aryl, heterocyclic bivalent group, heteroaromatic bivalent group, or aromatic bivalent group; X is a bond, —O—, —S—, —SO.sub.2—, —CO—, —NR.sub.9—, —(CH.sub.2).sub.m—, or heterocyclic bivalent group, m is 1, 2, 3, 4, 5, or 6; Y is a bond, —NH—, heterocyclic bivalent group, heteroaromatic bivalent group, bivalent benzyl group, or aromatic bivalent group; and Z is hydrogen, halogen, alkyl, aryl, heterocyclyl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; R.sub.7, R.sub.8, and R.sub.9 are independently hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl; and R.sub.10 is —O-tert-butyl, —CH.sub.2CH.sub.2-phenyl, hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl.

P2X7R ANTAGONISTS
20220380310 · 2022-12-01 ·

A compound has Formula I:

##STR00001##

R.sub.1 is hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, aryl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; L is a bond, a heterocyclic bivalent group, a heteroaromatic bivalent group, or an aromatic bivalent group; M is a bond, alkyl, aryl, heterocyclic bivalent group, heteroaromatic bivalent group, or aromatic bivalent group; X is a bond, —O—, —S—, —SO.sub.2—, —CO—, —NR.sub.9—, —(CH.sub.2).sub.m—, or heterocyclic bivalent group, m is 1, 2, 3, 4, 5, or 6; Y is a bond, —NH—, heterocyclic bivalent group, heteroaromatic bivalent group, bivalent benzyl group, or aromatic bivalent group; and Z is hydrogen, halogen, alkyl, aryl, heterocyclyl, heteroaryl, —NR.sub.7R.sub.8, —CO—R.sub.10, or —NH—CO—R.sub.10; R.sub.7, R.sub.8, and R.sub.9 are independently hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl; and R.sub.10 is —O-tert-butyl, —CH.sub.2CH.sub.2-phenyl, hydrogen, hydroxy, halogen, nitro, amino, alkyl, alkoxy, alkylamino, cycloalkyl, cycloalkyamino, heterocyclyl, or heteroaryl.

Aryl-piperidine derivatives

An aryl-piperidine derivative of formula I, wherein the meaning of R.sub.3, X, Cz, and Cy is that specified in the description, for use as inhibitors of T cells. ##STR00001##

Aryl-piperidine derivatives

An aryl-piperidine derivative of formula I, wherein the meaning of R.sub.3, X, Cz, and Cy is that specified in the description, for use as inhibitors of T cells. ##STR00001##