Steroidal glycosides for treating hypercholesterolemia
AssigneePfizer Inc.
InventorsMichael P. Deninno, Peter A. McCarthy
Life of this patent
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Abstract
The application discloses steroidal glycoside compounds, especially spirostanyl glycosides, which have a glycosyl group O-linked to the C-3 hydroxy radical of the steroid and where the moieties at the C-10 and C-11 positions of the steroid are the same or different and are selected from the group consisiting of methylene, hydroxy and carbonyl. These steroid glycosides are useful as hypocholesterolemic agents and anti-atherosclerosis agents.
Claims36
A spirostanyl glycoside of Formula IA ##STR43## wherein either (A):
- ##STR44## Q.sup.4 and Q.sup.3 are both methylene;
- C.sub.25 is (R);
- and wherein
- R.sup.1 is
- .beta.-D-glucopyranosyl,
- .beta.-D-glucopyranuronosyl,
- .beta.-D-2-acetamido-2-deoxy-glucopyranosyl,
- .beta.-D-galactopyranosyl,
- .beta.-D-fucopyranosyl,
- .beta.-L-fucopyranosyl,
- .beta.-D-xylopyranosyl,
- .beta.-L-xylopyranosyl,
- .alpha.-D-arabanopyranosyl,
- .alpha.-L-arabanopyranosyl,
- .alpha.-D-cellobiosyl,
- .beta.-D-cellobiosyl,
- .beta.-D-lactosyl,
- .beta.-D-maltosyl,
- .beta.-D-gentiobiosyl,
- 3-O-.beta.-D-galactopyrasnosyl-.alpha.-D-arabanopyranosyl or
- .beta.-D-maltotriosyl.
A method for treating hypercholesterolemia or atherosclerosis in a mammal comprising adminstering to a mammal suffering from hypocholesterolemia or atherosclerosis a hypercholesterolemia or atherosclerosis treating amount of a Formula I spirostanyl glycoside ##STR55## wherein either (A):
- ##STR56## Q.sup.4 and Q.sup.5 are both methylene;
- C.sub.25 is (R);
- and wherein
- R.sup.1 is
- .beta.-D-glucopyranosyl,
- .beta.-D-glucopyranuronosyl,
- .beta.-D-2-acetamido-2-deoxy-glucopyranosyl,
- .beta.-D-galactopyranosyl,
- .beta.-D-fucopyranosyl,
- .beta.-L-fucopyranosyl,
- .beta.-D-xylopyranosyl,
- .beta.-L-xylopyranosyl,
- .alpha.-D-arabanopyranosyl,
- .alpha.-L-arabanopyranosyl,
- .alpha.-D-cellobiosyl,
- .beta.-D-cellobiosyl,
- .beta.-D-lactosyl,
- .beta.-D-maltosyl,
- .beta.-D-gentiobiosyl,
- 3-O-.beta.-D-galactopyranosyl-.alpha.-D-arabanopyranosyl or
- .beta.-D-maltotriosyl.
Dependencies are inferred from the claim text.