Small molecule inhibitors of the nuclear translocation of androgen receptor for the treatment of castration-resistant prostate cancer

US10980806B2 · kind B2 · utility

Assignee

• University of Pittsburgh—Of the Commonwealth System of Higher Education · US

Inventors

• Peter Wipf · Pittsburgh, US
• James K. Johnson · Ringwood, US
• Erin M. Skoda · Columbia, US
• Joel B. Nelson · Pittsburgh, US
• Zhou Wang · Aachen, DE
• Serene Tai · Pittsburgh, US
• Keita Takubo · Pittsburgh, US
• John Milligan · Philadelphia, US

Key dates

• Filing date: Sep 24, 2018
• Grant date: Apr 20, 2021
• Expiry date: Sep 24, 2038

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61K2300/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A compound, or a pharmaceutically acceptable salt or ester thereof, according to formula I: R20—(Z)b—(Y)c—(R21)a—(X)d—R22—R23 wherein R20 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; Z is alkanediyl, substituted alkanediyl, cycloalkanediyl, or substituted cycloalkanediyl; Y is S, O, S(═O), —S(═O)(═O)—, or NR10, wherein R10 is H or alkyl; R21 is alkanediyl, substituted alkanediyl, cycloalkanediyl, substituted cycloalkanediyl, alkadienyl, substituted alkadienyl, cycloalkenediyl, substituted cycloalkenediyl, alkatrienyl, substituted alkatrienyl; X is —C(═O)—, —S(═O)(═O)—, or —N(H)C(═O)—; R22 includes at least one divalent amino radical; R23 is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a thio-containing group, or a seleno-containing group; a, b, c, and d independently are 0 or 1.