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Claims for Patent: 5,665,772

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Claims for Patent: 5,665,772

Title: O-alkylated rapamycin derivatives and their use, particularly as immunosuppressants
Abstract:Novel derivatives of rapamycin, particularly 9-deoxorapamycins, 26-dihydro-rapamycins, and 40-0-substituted and 28,40-0,0-di-substituted rapamycins, are found to have pharmaceutical utility, particularly as an immunosuppressants.
Inventor(s): Cottens; Sylvain (Witterswil, CH), Sedrani; Richard (Basel, CH)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:08/416,673
Patent Claims: 1. A compound of the formula ##STR3## wherein R.sup.1 is hydroxy(C.sub.1-6)alkyl or hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl.

2. A compound according to claim 1 in which R.sup.1 is hydroxy(C.sub.1-3)alkyl or hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl.

3. A compound according to claim 1 in which R.sup.1 is hydroxy(C.sub.1-3)alkyl.

4. A compound according to claim 1 in which R.sup.1 is hydroxy(C.sub.1-3)alkoxy(C.sub.1-3)alkyl.

5. The compound according to claim 1 which is 40-O-(3-hydroxypropyl)-rapamycin.

6. The compound according to claim 1 which is 40-O-[2-(2-hydroxyethoxy)ethyl]-rapamycin.

7. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier therefor.

8. A method of inducing an immunosuppressant effect in a subject in need of immunosuppression, which comprises administering to said subject an immunosuppressant effective amount of a compound according to claim 1.

9. A method of preventing allograft rejection in a subject in need of such treatment, which comprises administering to said subject a compound according to claim 1 in an amount effective to prevent allograph rejection.

10. The compound according to claim 1 which is 40-O-(3-hydroxyethyl)-rapamycin.
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