US 11,834,423 B2
Small molecule prolactin receptor inhibitors, pharmaceutical compositions and treatment methods using such inhibitors
Nira Ben-Jonathan, Cincinnati, OH (US); Eric R. Hugo, Cincinnati, OH (US); Edward J. Merino, Cincinnati, OH (US); Abraham J. Domb, Jerusalem (IL); and Armen N. Akopian, Austin, TX (US)
Assigned to University of Cincinnati, Cincinnati, OH (US); University of Texas System, Austin, TX (US); and The Hebrew University of Jerusalem, Jerusalem (IL)
Filed by University of Cincinnati, Cincinnati, OH (US); The Hebrew University of Jerusalem, Jerusalem (IL); and University of Texas System, Austin, TX (US)
Filed on Sep. 30, 2021, as Appl. No. 17/491,452.
Application 17/491,452 is a division of application No. 16/331,728, granted, now 11,168,061, previously published as PCT/US2017/050586, filed on Sep. 8, 2017.
Claims priority of provisional application 62/410,907, filed on Oct. 21, 2016.
Claims priority of provisional application 62/385,948, filed on Sep. 9, 2016.
Prior Publication US 2022/0024881 A1, Jan. 27, 2022
Int. Cl. A61P 35/00 (2006.01); C07D 253/075 (2006.01); A61K 31/135 (2006.01); A61K 31/415 (2006.01); A61K 31/475 (2006.01); A61K 31/53 (2006.01); A61K 45/06 (2006.01); A61K 9/00 (2006.01); A61K 33/243 (2019.01); A61K 31/122 (2006.01); A61K 31/337 (2006.01); A61K 31/4184 (2006.01); A61K 31/437 (2006.01)
CPC C07D 253/075 (2013.01) [A61K 9/0019 (2013.01); A61K 9/0053 (2013.01); A61K 31/135 (2013.01); A61K 31/415 (2013.01); A61K 31/475 (2013.01); A61K 31/53 (2013.01); A61K 45/06 (2013.01); A61P 35/00 (2018.01); A61K 31/122 (2013.01); A61K 31/337 (2013.01); A61K 31/4184 (2013.01); A61K 31/437 (2013.01); A61K 33/243 (2019.01)] 5 Claims
 
1. A pharmaceutical composition comprising:
a small molecule prolactin receptor (PRLR) inhibitor according to Formula II or a pharmaceutical salt thereof; and
at least one pharmaceutically acceptable carrier,
wherein Formula II is structurally depicted as:

OG Complex Work Unit Chemistry
and wherein:
R1 is selected from —CY3, linear or cyclic alkyl, halogen, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and H;
X is selected from —NH2, halogen, —OH, —SH, —NO2, —COOH, —SO3H, and —SO2NH2;
n is 0 or an integer between 1 and 10; and
each Y is independently H or halogen selected from Cl, Br, F, and I.