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Beta-2 Adrenoceptor Agonists for Treating Connective Tissue Diseases of the Skin

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Beta-2 Adrenoceptor Agonists for Treating Connective Tissue Diseases of the Skin (19) & (11) EP 1 719 507 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/135 (2006.01) A61P 37/00 (2006.01) 14.07.2010 Bulletin 2010/28 A61P 37/06 (2006.01) A61P 19/04 (2006.01) (21) Application number: 06007632.0 (22) Date of filing: 12.04.2006 (54) Beta-2 adrenoceptor agonists for treating connective tissue diseases of the skin Beta-2 Adrenoceptor Agonisten zur Behandlung von Bindegewebserkrankungen der Haut Des agonistes de bêta-2 adrénocepteur pour le traitement de maladies des tissus conjonctifs de la peau (84) Designated Contracting States: (56) References cited: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR WO-A-03/088997 WO-A-03/092617 HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI WO-A-03/097073 WO-A-2004/073614 SK TR WO-A-2005/051293 WO-A-2005/079284 Designated Extension States: WO-A-2005/089741 WO-A-2006/027579 AL BA HR MK YU GB-A- 2 255 503 US-A- 5 648 386 US-A- 5 919 827 US-A- 6 068 833 (30) Priority: 13.04.2005 DK 200500529 US-A- 6 110 974 US-A1- 2004 220 153 US-B1- 6 254 882 (43) Date of publication of application: 08.11.2006 Bulletin 2006/45 • SLATTERY D ET AL: "LEVALBUTEROL HYDROCHLORIDE" PEDIATRIC (73) Proprietor: Astion Development A/S PULMONOLOGY, JOHN WILEY, NEW YORK, NY, 2100 Copenhagen (DK) US, vol. 33, no. 2, 2002, pages 151-157, XP009057490 ISSN: 8755-6863 (72) Inventor: Weidner, Morten Sloth • AGIS F. KYDONIEUS, JOHN J. WILLE: 2830 Virum (DK) "BIOCHEMICAL MODULATION of SKIN REACTIONS" 2000, CRC PRESS * page 10 - page (74) Representative: Plougmann & Vingtoft A/S 11 * Sundkrogsgade 9 • KALISH ET AL: "Sensitization of mice to topically P.O. Box 831 applied drugs: Albuterol, chlorpheniramine, 2100 Copenhagen Ø (DK) clonidine and nadolol" CONTACT DERMATITIS, vol. 35, no. 2, 1996, pages 76-82, Remarks: Thefile contains technical information submitted after the application was filed and not included in this specification Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 1 719 507 B1 Printed by Jouve, 75001 PARIS (FR) EP 1 719 507 B1 Description FIELD OF THE INVENTION 5 [0001] The present invention relates to the field of pharmacological science. There is provided a beta 2-adrenoceptor agonistas therapeutically active ingredientfor use as a dermatological medicament fortreating connectivetissue diseases of the skin, particularly cutaneous manifestations of Lupus Erythematosus in an individual by administering a beta 2-adren- oceptor agonist to the affected skin areas of the individual. Furthermore, the invention is directed to topically administrable compositions comprising a beta2-adrenoceptor agonist in enantiomeric enriched or pure form. 10 BACKGROUND OF THE INVENTION [0002] There is no permanent cure for connective diseases of the skin, such as cutaneous forms of Lupus Erythema- tosus. Today, the treatment of connective diseases includes topical treatment with strong steroids, sometimes in com- 15 bination with anti-malarial drugs or systemic immuno- suppressants. Unfortunately, the treatment with such drug agents has serious side effects and cannot be applied for prolonged periods. [0003] The present inventor has recognised the strong need for therapeutic agents that can effectively alleviate the symptoms of cutaneous forms of Lupus Erythematosus (LE) without exhibiting significant adverse effects. Quite sur- prising, the present inventor has found that the topical application of a beta2-adrenoceptor agonist effectively relieves 20 the clinical manifestations in cutaneous forms of Lupus Erythematosus. [0004] Cutaneous forms of Lupus Erythematosus (Cutaneous Lupus Erythematosus) encompass at least 10 to 15 different clinical presentations that usually can be divided into 3 categories, including (1) acute cutaneous lupus ery- thematosus (ACLE), (2) subacute cutaneous lupus erythematosus (SCLE), and (3) chronic cutaneous lupus erythema- tosus (CCLE). Some of the common types of cutaneous LE include chronic cutaneous lupus erythematosus (CCLE) 25 and various sub-types thereof. [0005] Current evidence indicates that cutaneous Lupus Erythematosus is a separate disease from systemic Lupus Erythematosus and not just a benign variant of systemic LE in that the two diseases seems to be genetically different diseases (Rook’s, Textbook of Dermatology, chapter 65, page 56.2, volume 3, 7th edition, edited by Tony Burns et al, Blackwell Science, 2004). Systemic Lupus Erythematosus (SLE) is the most common connective tissue disease and is 30 characterised by multi-organ inflammation, which most commonly affects the skin, joints and vasculature. Almost any organ or system of the body, including the lungs, kidneys, heart or brain may be affected by the inflammation. [0006] Beta2-adreneroceptor agonists are traditionally used in the treatment of respiratory diseases such as asthma, chronic bronchitis and nervous system injury. Beta 2-adrenoceptor agonists has also been found to interact with specific receptors on T-lymphocytes to mediate anti-inflammatory activities (Baramki D et al. Modulation of T-cell function by 35 (R)- and (S)-isomers of albuterol: anti-inflammatory influences of (R)-isomers are negated in the presence of the (S)-iso- mer. J Allergy Clin Immunol 2002 March;109(3):449-54) and Barnes PJ. Effect of beta-agonists on inflammatory cells. J Allergy Clin Immunol 1999 August;104(2 Pt 2):S10-S1)7. [0007] A numberof drug agents and combinations thereofhave been proposed for the treatment ofvarious inflammatory diseases including discoid Lupus Erythematosus, wherein a beta2-adrenoceptor agonist among other drug agents is 40 proposed to be administered as a secondary active drug agent. [0008] The patent GB2255503 (Sandoz Ltd) relates to the treatment of obstructive or inflammatory airways disease by topically administering selective beta2- sympathomimatic bronchodilator drugs. [0009] The patents US6068833 and US5919827 (Aberg et al) relates to the treatment of pulmonary disorders by administering R-isomers of beta2-adrenoceptor agonists. 45 [0010] The patent US6110974 (Barberich et al) relates to a method for improving health, survival and muscle growth rate of animals by topically administrating R-salmeterol. [0011] The patent US5648386 (Resemann et al) relates to a composition for animal husbandry comprising R- cimaterol. [0012] The patent US6254882 (Jerussi et al) relates to a composition inducing bronchodilation comprising S-salme- terol. 50 [0013] The patent application US2005192261 relates to topical treatment with combinations of an antihistamine or an antihistamine analogue and a corticosteroid. [0014] The patent application WO05051293 relates to topical treatment with Ibudilast or a related compound. [0015] The patent application US2004220153 relates to topical treatment with a selective serotonin reuptake inhibitors (SSRI). 55 [0016] The patent applications US2004224876 (Jost- Price Edward Royden et al. ) and WO2004073614 (Combinatorix Inc et al.) relate to topical treatment with a non-steroidal immunophilin-dependent immunosuppressant (NsIDI) and an NsIDI enhancer (NsIDIE). [0017] Notably, none of the above-mentioned patent application relates to the direct treatment of cutaneous forms of 2 EP 1 719 507 B1 LE with a beta 2-adrenoceptor agonist, neither as the sole therapeutically agent nor as the primary therapeutically agent. [0018] Furthermore, a number of treatment regimens have been proposed for the treatment of systemic LE. In these treatments, the primary therapeutically effective drug agent eventually may be co- administered with a beta 2-adrenoceptor agonist: 5 [0019] The patent application WO2005079284 relate to combinations of a serotonin norepinephrine reuptake inhibitor (SNRI) or noradrenaline reuptake inhibitor (NARI) or analog thereof, a corticosteroid and a beta2- adrenoceptor agonist for the treatment of inflammatory diseases, including systemic Lupus Erythematosus. [0020] The patent application WO2006027579 relates to the treatment of inflammatory diseases, including systemic lupus erythematosus by administrering S-clenbuterol, S-mabuterol, SR-rimiterol and SS-procaterol. 10 [0021] The patent application WO2003092617 relates to the treatment of an inflammatory skin disease, such as systemic Lupus Erythematosus, by topically administering a steroid and a beta-adrenergic receptor ligand. [0022] The patent application US2003236298A1 (Atherogenics Pharmaceuticals, Inc) relates to 1,3-bis-(substituted- phenyl)-2-propen-1-ones that are inhibitors of the expression of VCAM-1 for the treatment of patients with a disease mediated by VCAM-1, such as systemic Lupus Erythematosus. 15 [0023] The patent applications US2005130935 and WO 2003097073 (Astion Development A/S) relate to combinations of a beta 2-adrenoceptor agonist and an aminosugar for the treatment of inflammatory diseases, including systemic Lupus Erythematosus. [0024] The patent applications US20050176714 and WO2003104204 relate to pyridazine derivatives acting as phos- phodiesterase IV inhibitors for the treatment of autoimmune diseases, such as systemic Lupus Erythematosus. 20 [0025] Furthermore, unusual respiratory manifestations of systemic Lupus Erythematosus, "shrinking lungs" have been treated
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