C07D498/14

GROUP OF TETRAHYDROINDOLOQUINAZOLINE COMPOUNDS AND USE THEREOF

The disclosure relates to an indolo[2′,3′:3,4]pyrido[2,1-b]quinazoline compound represented by general formula (I) and use thereof in the manufacture of (1) a medicament for treating a cardiovascular and cerebrovascular disease, (2) a formulation for increasing expression of AMPK, ABCA1 and SR-BI, (3) a formulation for activating nuclear receptors (NRs), and inhibiting activity of NLRP3, IL-1β, NF-κB and MAPKs, (4) a formulation for promoting cellular cholesterol efflux; or (5) a medicament for anti-inflammation.

##STR00001##

GROUP OF TETRAHYDROINDOLOQUINAZOLINE COMPOUNDS AND USE THEREOF

The disclosure relates to an indolo[2′,3′:3,4]pyrido[2,1-b]quinazoline compound represented by general formula (I) and use thereof in the manufacture of (1) a medicament for treating a cardiovascular and cerebrovascular disease, (2) a formulation for increasing expression of AMPK, ABCA1 and SR-BI, (3) a formulation for activating nuclear receptors (NRs), and inhibiting activity of NLRP3, IL-1β, NF-κB and MAPKs, (4) a formulation for promoting cellular cholesterol efflux; or (5) a medicament for anti-inflammation.

##STR00001##

FUSED PYRIDONE COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20220389029 · 2022-12-08 ·

Disclosed in the present invention are a fused pyridone compound, and a preparation method therefor and a use thereof. Specifically, the present invention discloses a compound of formula (I-B), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.

##STR00001##

FUSED PYRIDONE COMPOUND, AND PREPARATION METHOD THEREFOR AND USE THEREOF
20220389029 · 2022-12-08 ·

Disclosed in the present invention are a fused pyridone compound, and a preparation method therefor and a use thereof. Specifically, the present invention discloses a compound of formula (I-B), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.

##STR00001##

BCL6 inhibitors

The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: ##STR00001##
wherein X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.30, R.sup.31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.

BCL6 inhibitors

The present invention relates to compounds of formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: ##STR00001##
wherein X.sub.1, X.sub.2, R.sup.1, R.sup.2, R.sup.30, R.sup.31 and Ring A are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.

CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
20220372042 · 2022-11-24 ·

The disclosure includes compounds of Formula (A) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, and R.sub.11, h, j, m, n, k, v, s, g, V, W, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6, and Q.sub.7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

##STR00001##

CONDENSED HETEROCYCLES AS BCL-2 INHIBITORS
20220372042 · 2022-11-24 ·

The disclosure includes compounds of Formula (A) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, and R.sub.11, h, j, m, n, k, v, s, g, V, W, L, Z.sub.1, Q.sub.1, Q.sub.2, Q.sub.3, Q.sub.4, Q.sub.5, Q.sub.6, and Q.sub.7, are defined herein. Also disclosed is a method for treating a neoplastic disease, an autoimmune disease, or a neorodegenerative disease with these compounds.

##STR00001##

AMINOPYRIMIDINE DERIVATIVES AS HOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
20220372046 · 2022-11-24 ·

The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula:

##STR00001##

where A, B, R.sub.1, X.sub.1, X.sub.2, and W are described herein.

AMINOPYRIMIDINE DERIVATIVES AS HOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
20220372046 · 2022-11-24 ·

The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula:

##STR00001##

where A, B, R.sub.1, X.sub.1, X.sub.2, and W are described herein.