Epoxy-guaiane derivatives and treatment of cancer
AssigneeThe United States of America, as represented by the Secretary, Department of Health and Human Services
InventorsJohn A. Beutler, Ranjala Ratnayake, David Covell, Tanya R. Johnson
Life of this patent
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Abstract
Disclosed are englerins and derivatives (I) thereof useful in the treatment of a number of cancers, particularly renal cancer, as well as pharmaceutical compositions and method of treating a patient with the use of these derivatives. The englerins, for example Englerin A and Englerin B, can be isolated from the plant Phyllanthus engleri or produced by synthetic methods. An example of the englerin derivative is 2′-chloroenglerin A, which has the structure (II), wherein double bond ‘a’ is E, Z, or a mixture of E and Z.
Claims40
An isolated or purified compound of the formula:
A compound of the formula (I):
- or an epimer thereof;
- wherein
- Ar is an aryl group, optionally substituted with a C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 alkoxy, halo, or nitro;
- X is O, NH, or S;
- R2 and R3 are independently a C1-C6 alkyl;
- R1 is isopropyl or isopropylenyl;
- “a” is a single bond or a double bond;
- when “a” is a double bond, R4 is hydrogen, and R5 is halo or H;
- when “a” is a single bond, R4 is selected from the group consisting of halo, hydroxy, or C1-C6 alkoxy and R5 is halo or H;
- and R6 is C1-C6 alkyl or hydroxy C1-C6 alkyl.
Dependencies are inferred from the claim text.