1788873-48-2Relevant academic research and scientific papers
Discovery of selective, orally bioavailable, N-linked arylsulfonamide Nav1.7 inhibitors with pain efficacy in mice
Roecker, Anthony J.,Egbertson, Melissa,Jones, Kristen L.G.,Gomez, Robert,Kraus, Richard L.,Li, Yuxing,Koser, Amy Jo,Urban, Mark O.,Klein, Rebecca,Clements, Michelle,Panigel, Jacqueline,Daley, Christopher,Wang, Jixin,Finger, Eleftheria N.,Majercak, John,Santarelli, Vincent,Gregan, Irene,Cato, Matthew,Filzen, Tracey,Jovanovska, Aneta,Wang, Ying-Hong,Wang, Deping,Joyce, Leo A.,Sherer, Edward C.,Peng, Xuanjia,Wang, Xiu,Sun, Haiyan,Coleman, Paul J.,Houghton, Andrea K.,Layton, Mark E.
, p. 2087 - 2093 (2017)
The voltage-gated sodium channel Nav1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a variety of painful disorders and loss-of-function mutations affording insensitivity to pain.
QUINAZOLINE COMPOUNDS, PREPARATION METHODS AND USES THEREOF
-
Paragraph 204; 209, (2022/01/12)
Provided herein are novel compounds, for example, compounds having a Formula (I), Formula (II), or Formula (III), or a pharmaceutically acceptable salt thereof. Also provided herein are methods of preparing the compounds and methods of using the compounds, for example, in inhibiting KRAS G12D in a cancer cell, and/or in treating various cancer such as pancreatic cancer, colorectal cancer, lung cancer or endometrial cancer.
BICYCLOAMINE-SUBSTITUTED-N-BENZENESULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
-
Paragraph 0189, (2015/06/11)
Disclosed are compounds of Formula (A-a), or a salt thereof, Where "B1" and "R1" through "R5" are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A-a) or their salts, and methods of treating neuropathic pain disorders using the same.
BICYCLOAMINE-SUBSTITUTED-N-BENZENESULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
-
Paragraph 0189, (2015/06/11)
Disclosed are compounds of Formula A-a, or a salt thereof: Where "B1" and "R1" through "R5" are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.
