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Claims for Patent: 6,423,722

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Claims for Patent: 6,423,722

Title: Crystalline macrolides and process for their preparation
Abstract:33-Epichloro-33-desoxyascomycin of formula I ##STR1## and various tautomeric or forms thereof, in crystalline form, such as Form A and Form B. Their preparation involves appropriately converting amorphous compound of formula I, or compound of formula I in other than Form A, or compound of formula I in other than Form B, respectively, from a solution thereof under crystallization-inducing conditions or conditions inducing preferential crystallization of Form A or B, respectively. Such crystals are particularly indicated for use in the preparation of topical galenical forms of the compound for pharmaceutical use, e.g. creams, emulsions and ointments.
Inventor(s): Dosenbach; Cornelia (Efringen-Kirchen, DE), Grassberger; Maximilian (Vienna, AT), Hartmann; Otto (Basel, CH), Horvath; Amarylla (Vienna, AT), Mutz; Jean-Paul (Blotzheim, FR), Penn; Gerhard (Oberwil, CH), Pfeffer; Sabine (Weil, DE), Wieckhusen; Dierk (Binzen, DE)
Assignee: Novartis AG (Basel, CH)
Application Number:09/690,404
Patent Claims: 1. The compound of formula I ##STR6##

or a tautomeric or solvated form thereof, in crystalline form.

2. The compound according to claim 1 in crystalline Form A.

3. The compound according to claim 1 in crystalline Form B.

4. A process for the preparation of a crystalline compound according to claim 1 which comprises appropriately converting amorphous compound of formula I from a solution thereof under crystallization-inducing conditions.

5. A process for the preparation of the crystalline compound according to claim 2 which comprises appropriately converting compound of formula I in other than Form A, or a tautomeric or solvated form thereof, from a solution thereof under conditions inducing preferential crystallization of Form A.

6. A process for the preparation of the crystalline compound according to claim 3 which comprises appropriately converting compound of formula I in other than Form B, or a tautomeric or solvated form thereof, from a solution thereof under conditions inducing preferential crystallization of Form B.

7. A pharmaceutical composition comprising a compound according to claim 1.

8. A method of treating inflammation or inducing immunosuppression or inhibiting cell proliferation, comprising administering to a patient in need of said treating a therapeutically effective amount of a compound according to claim 1.
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