C07D241/14

TRPML MODULATORS

The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

REGULATOR OF NITROGEN-CONTAINING HETEROAROMATIC DERIVATIVES, PREPARATION METHOD THEREFOR AND USE THEREOF
20210355105 · 2021-11-18 ·

The present invention relates to a regulator of nitrogen-containing heteroaromatic derivatives, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in the general formula (I), a preparation method therefor and a pharmaceutical composition containing the compound, and the use thereof as a protein tyrosine phosphatase-2C (SHP2) inhibitor in the treatment of diseases or conditions such as leukemia, neuroblastoma, melanoma, breast cancer, lung cancer and colorectal cancer, wherein the definition of each substituent in the general formula (I) is the same as that in the description.

(R)-8-(1-((3-fluorophenyl)amino)ethyl)-N-(2-hydroxyethyl)-2-morpholinoquinoxaline-6-carboxamide for inhibiting phosphoinositide-3-kinase activity

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) ##STR00001##
wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

(R)-8-(1-((3-fluorophenyl)amino)ethyl)-N-(2-hydroxyethyl)-2-morpholinoquinoxaline-6-carboxamide for inhibiting phosphoinositide-3-kinase activity

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) ##STR00001##
wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3Kβ inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

CGRP RECEPTOR ANTAGONISTS

The disclosures herein relate to novel compounds of formula

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

CGRP RECEPTOR ANTAGONISTS

The disclosures herein relate to novel compounds of formula

##STR00001##

wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

CGRP receptor antagonists

The disclosures herein relate to novel compounds of formula ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

CGRP receptor antagonists

The disclosures herein relate to novel compounds of formula ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

QUINOXALINE AND PYRIDOPYRAZINE DERIVATIVES AS A PI3KB INHIBITORS

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I)

##STR00001##

wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.

Quinoxaline and pyridopyrazine derivatives as PI3Kβ inhibitors

The present invention relates to substituted quinoxaline and pyridopyrazine derivatives of Formula (I) ##STR00001##
wherein the variables have the meaning defined in the claims. The compounds according to the present invention are useful as pI3K inhibitors. The invention further relates to pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.