Granted Patent B2

US 12,540,115 · App. 17/635,891 · Granted Feb 3, 2026

Inventors: Arvin Gouw (San Francisco, CA); Steven R. Schow (Redwood City, CA); Robert J. Greenhouse (Newark, CA); Toni Kline (San Francisco, CA); Dean W. Felsher (San Mateo, CA)

Assignee: The Board of Trustees of the Leland Stanford Junior University

C07C311/08A61K31/41A61P3/00C07C311/14C07C311/51C07D213/79C07D401/04C07D493/04C07D493/10

Abstract

Claims (44)

1 . A method of treating a subject for cancer, the method comprising:

administering an effective dose of a GPAT inhibitor described by formula (IIAa):

comparing a lipogenesis profile obtained from a subject having a neoplasm with a reference lipogenesis profile to classify whether the neoplasm is lipogenesis-dependent; and

administering to the subject an effective amountof a GPAT inhibitor described by formula (IIAa):

wherein:

Z′″ is a heteroaryl or substituted heteroaryl;

R′ is an alkyl, substituted alkyl, cycloalkyl, or heterocycloalkyl, wherein alkyl moieties are optionally substituted with a group selected from OCH 3 , and CF 3 ;

R″ is hydrogen;

Y 1 is CR 1 ;

Y 2 is CR 2 ;

Y 3 is CR 3 ;

Y 4 is CR 4 ; and

R 1 -R 4 are hydrogen, when the neoplasm is classified as lipogenesis-dependent, to treat the subject for the lipogenesis-dependent neoplasm for a period of time sufficient to inhibit growth of the cancer.

2 . A method of treating a subject for cancer, the method comprising:

administering an effective dose of a GPAT inhibitor wherein the GPAT inhibitor has the structure:

for a period of time sufficient to inhibit growth of the cancer.

3 . A method of treating a subject for cancer, the method comprising:

administering an effective dose of a GPAT inhibitor described by formula (IIAa):

wherein:

Z′″ is

R′ is an alkyl, substituted alkyl, cycloalkyl, or heterocycloalkyl, wherein alkyl moieties are optionally substituted with a group selected from OCH 3 , and CF 3 ;

R″ is hydrogen;

Y 1 is CR 1 ;

Y 2 is CR 2 ;

Y 3 is CR 3 ;

Y 4 is CR 4 ; and

R 1 -R 4 are hydrogen;

for a period of time sufficient to inhibit growth of the cancer.

4 . The method of claim 3 , wherein the GPAT inhibitor is selected from

5 . A method of treating a metabolic syndrome related disease, the method comprising:

administering to a subject an effective dose of a GPAT inhibitor wherein the GPAT inhibitor has the structure:

for a period of time sufficient to reduce symptoms of the disease in the subject.

6 . A method of treating a metabolic syndrome related disease, the method comprising:

administering an effective dose of a GPAT inhibitor described by formula (IIAa):

wherein:

Z′″ is

R′ is an alkyl, substituted alkyl, cycloalkyl, or heterocycloalkyl, wherein alkyl moieties are optionally substituted with a group selected from OCH 3 , and CF 3 ;

R″ is hydrogen;

Y 1 is CR 1 ;

Y 2 is CR 2 ;

Y 3 is CR 3 ;

Y 4 is CR 4 ; and

R 1 -R 4 are hydrogen for a period of time sufficient to reduce symptoms of the disease in the subject.

7 . The method of claim 6 , wherein the GPAT inhibitor is selected from

Assignments (1)

Continuity (2)

References Cited (15)