	US 12,227,482 B2
	Compounds and compositions for the treatment of cancer
Csaba Peto, San Francisco, CA (US); Bhairavi Tolani, San Francisco, CA (US); Gavitt Woodard, San Francisco, CA (US); Tsze Tsang, El Cerrito, CA (US); Michael Mann, San Francisco, CA (US); David M. Jablons, San Francisco, CA (US); and Biao He, Foster City, CA (US)
Assigned to The Regents of the University of California, Oakland, CA (US); and Rascal Therapeutics, Inc., Los Altos Hills, CA (US)
Filed by The Regents of the University of California, Oakland, CA (US); and RasCal Therapeutics, Inc., Southlake, TX (US)
Filed on Dec. 5, 2022, as Appl. No. 18/075,198.
Application 18/075,198 is a division of application No. 16/305,377, granted, now 11,560,356, previously published as PCT/US2017/039806, filed on Jun. 28, 2017.
Claims priority of provisional application 62/356,261, filed on Jun. 29, 2016.
Prior Publication US 2023/0150942 A1, May 18, 2023
Int. Cl. C07D 231/06 (2006.01); C07D 405/04 (2006.01); C07D 409/04 (2006.01)

CPC C07D 231/06 (2013.01) [C07D 405/04 (2013.01); C07D 409/04 (2013.01)]

27 Claims

1. A method for treating a subject with a cancerous condition, the method comprising:

administering to the subject a therapeutically effective amount of a compound of formula (I):

wherein

X¹is N and X²is C, and the ring N forms a double bond with X²;

R¹is aryl or substituted aryl;

R²is aryl or substituted aryl;

R³is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;

R⁴is hydrogen, alkyl or substituted alkyl; and

R⁵is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkyl, substituted cycloalkyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl;

or a salt, a hydrate, a solvate, or a stereoisomer thereof, wherein the cancerous condition is characterized by expressing a GLI protein, and wherein the administering results in treatment of the subject.