Benzene compounds as antiproliferative and cholesterol lowering agents
AssigneeTularik Inc.
InventorsJulio Cesar Medina, David Louis Clark, John A. Flygare, Terry J. Rosen, Bei Shan
Life of this patent
Estimating the term…
Abstract
The invention provides compounds, compositions and methods relating to novel electrophilic aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents. The compositions include compounds of the general Formula I:
Claims27
A method of treating or preventing a disease state characterized by abnormally high levels of low density lipoprotein particles or cholesterol in the blood, or by an abnormally high level of cell proliferation, which method comprises administering to a mammalian subject in need thereof a therapeutically effective amount of a composition containing a compound of formula I:
- or a pharmaceutically acceptable salt or produce thereof, wherein:
- n is 2;
- R1 is a member selected from the group consisting of hydrogen, (C1-C6)alkyl, halogen, OCF3, CF3, NO2, CN, and CO2—R8;
- R2 is a member selected from the group consisting of NO2, CN, CO2—R8 and SO2—R8;
- R4 is a member selectd from the group consisting of halogen and OCF3;
- R4 is a member selected from the group consisting of hydrogen, halogen, OCF3, CF3, NO2, CN, and CO2—R8;
- R5 is a member selected from the group consisting of hydrogen, (C1-C6)alkyl, halogen, OCF3, CF3, NO2, CN, and CO2—R8;
- Y is N(9);
- wherein R8 is selected from the group consisting of (C1-C6) alkyl and (C2-C6) heteroallyl and R9 is selected from the group consisting of hydrogen, substituted or usudtituted (C1-C10)alkyl, substituted or unsubstituted (C3-C6)alkenyl, subsituted or unsubstituted (C2-C6)heteroalyl, substituted or unsubstituted (C3-C6)heteroalkenyl, substituted or unsubstituted (C3-C6)alkynyl, substituted or uusubstituted (C3-C8)cycloalky;
- and
- Ar is a substituted or unsubstituted pheayl group,
- wherein said substituents are independently selected from the group consisting of OH, halogen, NH2, NH(C1-C6)alkyl, N((C1-C6)alkyl)2, (C1-C6)alkyl, and (C1-C6)alkoxy.
Dependencies are inferred from the claim text.