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Claims for Patent: 6,509,376

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Claims for Patent: 6,509,376

Title: Utilization of dialkyfumarates
Abstract:The present invention relates to the use of certain dialkyl fumarates for the preparation of pharmaceutical preparations for use in transplantation medicine or for the therapy of autoimmune diseases and said compositions in the form of micro-tablets or pellets. For this purpose, the dialkyl fumarates may also be used in combination with conventional preparations used in transplantation medicine and immunosuppressive agents, especially cyclosporines.
Inventor(s): Joshi; Rajendra Kumar (Zurich, CH), Strebel; Hans-Peter (Muri, CH)
Assignee: Fumapharm AG (Muri, CH)
Application Number:09/831,620
Patent Claims: 1. Pharmaceutical preparation in the form of microtablets or micropellets comprising one or more dialkyl fumarates of the formula ##STR2##

wherein R.sub.1 and R.sub.2, which may be the same or different, independently represent a linear, branched or cyclic, saturated or unsaturated C.sub.1-20 alkyl radical which may be optionally substituted with halogen (Cl, F, I, Br), hydroxy, C.sub.1-4 alkoxy, nitro or cyano, and optionally suitable carriers and excipients for use in transplantation medicine or for the therapy of autoimmune diseases such as polyarthritis, multiple sclerosis, juvenile-onset diabetes, Hashimoto's thyroiditis, Grave's disease, systemic Lupus erythematodes (SLE), Sjogren's syndrome, pernicious anaemia, chronic active (lupoid) hepatitis, psoriasis, psoriatic arthritis, neurodermatitis and enteritis regionalis Crohn.

2. A preparation according to claim 1 comprising dimethyl fumarate, diethyl fumarate or methylethyl fumarate.

3. A preparation according to claim 1 or 2 comprising an amount of the active ingredient corresponding to 10 to 300 mg of fumaric acid.

4. A preparation according to claim 1 wherein the one or more dialkylfumarates is diethylfumarate.

5. A preparation according to claim 1 wherein the one or more dialkylfumarates is dimethylfumarate.

6. A preparation according to claims 4 or 5 wherein the amount of dialkylfumarate in said preparation corresponds to 10 to 300 mg of fumaric acid.

7. A preparation according to any of claims 1, 2, 4 or 5 wherein the preparation is formulated into an oral preparation in which the microtablets or micropellets are in capsules or sachets.

8. A preparation according to any of claims 1, 2, 4 or 5 wherein the preparation is formulated into an oral preparation in which the microtablets or micropellets are in soft or hard gelatine capsules.

9. A preparation according to any of claims 1, 2, 4 or 5 wherein the microtablets or micropellets are provided with an enteric coating.

10. A preparation according to claim 1 wherein the preparation is formulated into an oral preparation in which the microtablets or micropellets are in capsules or sachets and wherein the amount of dialkylfumarate in said preparation corresponds to 10 to 300 mg of fumaric acid.

11. A preparation according to claim 1 wherein the preparation is formulated into an oral preparation in which the microtablets or micropellets are in soft or hard gelatine capsules and wherein the amount of dialkylfumarate in said preparation corresponds to 10 to 300 mg of fumaric acid.

12. A preparation according to claim 1 wherein the microtablets or micropellets are provided with an enteric coating and wherein the amount of dialkylfumarate in said preparation corresponds to 10 to 300 mg of fumaric acid.

13. A pharmaceutical composition in which the active ingredient consists of one or more dialkyl fumarates, said composition being in the form of microtablets or micropellets wherein the size or mean diameter, respectively of said microtablets or micropellets is 5,000 microns or less exclusive of any optional coating applied to said microtablets or micropellets.

14. The composition of claim 13 wherein said size or mean diameter is 2,000 microns or less.

15. The composition of claim 13 wherein said one or more dialkyl fumarates are of the formula ##STR3##

wherein R.sub.1 and R.sub.2, which may be the same or different, independently represent a linear, branched or cyclic, saturated or unsaturated C.sub.1-20 alkyl radical which may be optionally substituted with halogen (Cl, F, I, Br), hydroxy, C.sub.1-4 alkoxy, nitro or cyano.

16. The composition of claim 13 wherein said one or more dialkyl fumarates is dimethyl fumarate, or diethyl fumarate, or methylethyl fumarate, and wherein the amount thereof corresponds to 10 to 300 mg fumaric acid.
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