	US 12,370,169 B2
	Small molecule Bcl-2 functional converters as cancer therapeutics
Siva K. Kolluri, Corvallis, OR (US); Prasad R. Kopparapu, Houston, TX (US); and Martin Pearce, Independence, OR (US)
Assigned to Oregon State University, Corvallis, OR (US)
Filed by Oregon State University, Corvallis, OR (US)
Filed on Aug. 19, 2022, as Appl. No. 17/821,146.
Application 17/821,146 is a continuation of application No. 16/465,971, granted, now 11,419,843, previously published as PCT/US2017/064335, filed on Dec. 1, 2017.
Claims priority of provisional application 62/428,864, filed on Dec. 1, 2016.
Prior Publication US 2023/0129487 A1, Apr. 27, 2023
Int. Cl. A61K 31/341 (2006.01); A61K 31/167 (2006.01); A61K 38/16 (2006.01); A61K 45/06 (2006.01)

CPC A61K 31/341 (2013.01) [A61K 31/167 (2013.01); A61K 38/16 (2013.01); A61K 45/06 (2013.01)]

3 Claims

1. A method of treating Bcl-2-expressing cancer, comprising targeting the Bcl-2 protein in a cancer cell of a subject by administering to the subject a therapeutically effective amount of a compound of formula (III):

or a tautomer, hydrate, or salt thereof,

wherein:

Ar¹is optionally substituted C6-C10 aryl or optionally substituted C5-C10 heteroaryl;

R¹and R²are independently H, halogen, optionally substituted C1-C8 alkyl, optionally substituted C1-C8 alkenyl, optionally substituted C1-C8 alkynyl, O (C1-C8 alkyl), or C (O) NHR, wherein R is optionally substituted C1-C8 alkyl, optionally substituted C6-C10 aryl, or optionally substituted C5-C10 heteroaryl; or together with the carbon atoms to which each is attached, R¹and R²form an optionally substituted 6-membered cycle;

Y is COOH, CONH₂, optionally substituted C6-C10 aryl, optionally substituted C5-C10 heteroaryl, or C (O) X; and

X is optionally substituted C6-C10 aryl, or optionally substituted C3-C10 heteroaryl.