# US 7,612,110 B2 · Utilization of dialkylfumarates > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 7,612,110 B2 - Document ID: US7612110B2 - Status: Granted - Kind: B2 - Application number: 11/765,563 - Filed: 2007-06-20 - Published: 2007-10-25 - Granted: 2009-11-03 - Earliest claimed: 1998-11-19 - Assignees: Biogen Idec International GmbH - Inventors: Rajendra Kumar Joshi; Hans-Peter Strebel - Web page: https://patentgrep.com/patent/US7612110B2 ## CPC - A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)} - A61K 9/1676: {having a drug-free core with discrete complete coating layer containing drug (adsorbates of liquid drug formulations on inert powders without simultaneous granulation step A61K9/141; with further drug-free outer coating A61K9/5078; drug conjugated to non-active particles A61K47/6921)} - A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 9/2072: {characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms (A61K9/0004, A61K9/0056, A61K9/0065 take precedence)} - A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} - A61K 9/284: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone} - A61K 9/2846: {Poly(meth)acrylates} - A61K 9/2853: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)} - A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/4808: {characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release (capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084)} - A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60) - A61K 31/225: Polycarboxylic acids - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61P 5/14: of the thyroid hormones, e.g. T3, T4 - A61P 5/16: for decreasing, blocking or antagonising the activity of the thyroid hormones - A61P 7/06: Antianaemics - A61P 17/00: Drugs for dermatological disorders - A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like - A61P 17/06: Antipsoriatics - A61P 19/02: for joint disorders, e.g. arthritis, arthrosis - A61P 25/00: Drugs for disorders of the nervous system - A61P 37/00: Drugs for immunological or allergic disorders - A61P 37/02: Immunomodulators - A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection - A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)} - A61K 9/2095: {Tabletting processes} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## 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. ## Claims ### Claim 1 A method of treating autoimmune polyarthritis but not treating psoriatic arthritis, comprising administering, to a patient in need of treatment for said polyarthritis but not for said psoriatic arthritis, an amount of a pharmaceutical preparation effective for treating said polyarthritis, the pharmaceutical preparation comprising at least one excipient or at least one carrier or a combination thereof and an active ingredient only consisting of dimethyl fumarate, methyl hydrogen fumarate, or a combination thereof. ### Claim 2 (depends on 1) The method of claim 1, wherein 10 mg to 300 mg of the active ingredient is administered. ### Claim 3 (depends on 1) The method of claim 1, wherein the active ingredient is provided in one or more capsules. ### Claim 4 (depends on 1) The method of claim 1, wherein the active ingredient consists of 50 mg of dimethyl fumarate. ### Claim 5 (depends on 1) The method of claim 1, wherein the active ingredient consists of 110 mg of dimethyl fumarate. ### Claim 6 (depends on 1) The method of claim 1, wherein the active ingredient consists of 120 mg of dimethyl fumarate. ### Claim 7 (depends on 1) The method of claim 1, wherein the active ingredient consists of methyl hydrogen fumarate. ### Claim 8 (depends on 7) The method of claim 7, wherein the active ingredient consists of 10 mg to 300 mg of methyl hydrogen fumarate. ### Claim 9 (depends on 1) The method of claim 1, wherein the active ingredient consists of dimethyl fumarate. ### Claim 10 (depends on 9) The method of claim 9, wherein the active ingredient consists of 10 mg to 300 mg of dimethyl fumarate. ### Claim 11 (depends on 9) The method of claim 9, wherein the active ingredient consists of 50 mg of dimethyl fumarate. ### Claim 12 (depends on 9) The method of claim 9, wherein the active ingredient consists of 110 mg of dimethyl fumarate. ### Claim 13 (depends on 9) The method of claim 9, wherein the active ingredient consists of 120 mg of dimethyl fumarate. ### Claim 14 (depends on 1) The method of claim 1, wherein the pharmaceutical preparation is formulated for oral administration. ### Claim 15 (depends on 1) The method of claim 1, wherein the pharmaceutical preparation is formulated as a solid dosage form. ### Claim 16 (depends on 1) The method of claim 1, wherein the pharmaceutical preparation is in the form of microtablets. ### Claim 17 (depends on 16) The method of claim 16, wherein the microtablets are provided in one or more capsules, each capsule containing at least 50 mg of dimethyl fumarate. ### Claim 18 (depends on 17) The method of claim 17, wherein each capsule contains at least 110 mg of dimethyl fumarate. ### Claim 19 (depends on 18) The method of claim 18, wherein each capsule contains at least 120 mg of dimethyl fumarate. ### Claim 20 (depends on 16) The method of claim 16, wherein the microtablets are enteric-coated. ### Claim 21 (depends on 16) The method of claim 16, wherein the microtablets have a mean diameter in the range of 0.3 mm to 2.0 mm, exclusive of any coating on the microtablets. ### Claim 22 (depends on 21) The method of claim 21, wherein the microtablets have a mean diameter of 2.0 mm, exclusive of any coating on the microtablets. ### Claim 23 (depends on 1) The method of claim 1, wherein the active ingredient consists of at least 50 mg of dimethyl fumarate. ### Claim 24 (depends on 1) The method of claim 1, wherein the active ingredient consists of at least 110 mg of dimethyl fumarate. ### Claim 25 (depends on 1) The method of claim 1, wherein the active ingredient consists of at least 120 mg of dimethyl fumarate. ### Claim 26 (depends on 1) The method of claim 1, wherein the pharmaceutical preparation comprises at least one carrier. ### Claim 27 (depends on 1) The method of claim 1, wherein the pharmaceutical preparation comprises at least one excipient. ### Claim 28 (depends on 1) The method of claim 1, wherein the active ingredient consists of only both dimethyl fumarate and methyl hydrogen fumarate. ### Claim 29 (depends on 1) The method of claim 1, wherein the pharmaceutical preparation comprises at least one excipient and at least one carrier.