Inhibitors of phospholipid synthesis and methods of use
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorsArvin Gouw, Steven R. Schow, Robert J. Greenhouse, Toni Kline, Dean W. Felsher
Life of this patent
Estimating the term…
Abstract
Inhibitors of Glycerol 3-Phosphate Acyltransferase (GPAT) are provided; and methods of use in the treatment of cancer; and treatment of conditions relating to metabolic syndrome, hyperlipidemia, infection and inflammation.
Claims7
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 OCH3, and CF3;
- R″ is hydrogen;
- Y1 is CR1;
- Y2 is CR2;
- Y3 is CR3;
- Y4 is CR4;
- and
- R1-R4 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.
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.
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 OCH3, and CF3;
- R″ is hydrogen;
- Y1 is CR1;
- Y2 is CR2;
- Y3 is CR3;
- Y4 is CR4;
- and
- R1-R4 are hydrogen;
- for a period of time sufficient to inhibit growth of the cancer.
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.
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 OCH3, and CF3;
- R″ is hydrogen;
- Y1 is CR1;
- Y2 is CR2;
- Y3 is CR3;
- Y4 is CR4;
- and
- R1-R4 are hydrogen for a period of time sufficient to reduce symptoms of the disease in the subject.
Dependencies are inferred from the claim text.