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Topical compositions comprising ascomycinsRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Heterocyclic Carbon Compounds Containing A Hetero Ring Having Chalcogen (i.e., O,s,se Or Te) Or Nitrogen As The Only Ring Hetero Atoms DoaiTopical compositions comprising ascomycins description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060058279, Topical compositions comprising ascomycins. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This invention relates to topical compositions containing ascomycins for treatment of skin disorders, e.g. subacute and chronic inflammatory and hyperproliferative skin diseases, e.g. atopic dermatitis, vitiligo, psoriasis, lichenified skin diseases, e.g. lichen planus, a lichenified form of atopic dermatitis. [0002] Ascomycins have a variety of useful pharmacological actions, e.g. immunosuppression, and which may be administered topically. However, inter alia because of their physicochemical properties, e.g. high molecular weight and lipophilicity the ascomycins have posed problems for topical administration. [0003] Skin disorders also present difficulties in treatment, particularly lichenified skin diseases, e.g. psoriasis, where the skin is hyperproliferated and the skin barrier function and skin lipid composition may have changed. Topical compositions for use in lichenified skin diseases, e.g. psoriasis, containing an ascomycin present particular difficulties. [0004] After exhaustive testing it has now been surprisingly found that the compositions of the present invention serve to enhance penetration of active agent through human skin, e.g. for the treatment of lichenified skin diseases, e.g. psoriasis. These compositions show other particularly interesting properties, e.g. they are easily applied to large areas of the skin and are stable. [0005] In one aspect this invention provides a composition for topical administration of an ascomycin which composition comprises a carrier vehicle comprising [0006] (i) means to retain water in the outer skin layer, and [0007] (ii) means to hinder water evaporating from the skin. [0008] The ascomycin is hereafter referred to as active agent. Under "ascomycin" is to be understood ascomycin itself or a derivative, antagonist, agonist or analogue thereof, e.g. a compound of the FK 506 class. [0009] FK506 is a known macrolide antibiotic that is produced by Streptomyces tsukubaensis No 9993. It is also a potent immunosuppressant. The structure of FK506 is given in the appendix to the Merck Index, 11th Edition as item A5. Methods of preparing FK506 are described in EP 184162. [0010] Under "compound of the FK 506 class" is to be understood FK 506 itself or a derivative, antagonist, agonist or analogue thereof, which retain the basic structure and modulate at least one of the biological properties (for example immunological properties) of FK506. A large number of compounds of the FK 506 class are known. These compounds are described in for example EP 184162, EP 315978, EP 323042, EP 423714, EP 427680, EP 465426, EP 474126, WO 91/13889, WO 91/19495, EP 484936, EP 532088, EP 532089, EP 569337, EP 626385, WO 93/5059 and the like. [0011] It is also known (for example from EP 315978 and EP 474126) that ascomycin derivatives such as macrolactam compounds of the FK506 class are particularly useful in the topical treatment of inflammatory and hyperproliferative skin diseases and of cutaneous manifestations of immunologically-mediated illnesses. [0012] Thus examples of ascomycin derivatives suitable for use in the present invention include FK506; 33-epi-chloro-33-desoxy-ascomycin as disclosed in Example 66a in EP 427 680 (hereafter referred to as Compound A); [0013] {[1E-(1R,3R,4R)]1R,4S,5R,6S,9R,10E,13S,15S,16R,17S,19S,20S}-9-ethyl- -6,16,20-trihydroxy-4-[2-(4-hydroxy-3-methoxy-cyclohexyl)-1-methylvinyl]-1- 5,17-dimethoxy-5,11,13,19-tetramethyl-3-oxa-22-aza-tricyclo[18.6.1.0(1,22)- ] heptacos-10-ene-2,8,21,27-tetraone as disclosed in Examples 6d and 71 in EP 569 337 (hereafter referred to as Compound B); and [0014] {1R,5Z,9S,12S-[1E-(1R,3R,4R)],13R,14S,17R,18E,21S,23S,24R,25S,27R} 17-ethyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxy-cyclohexyl)-1-methylvi- nyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-aza-tricyclo[22- .3.1.0(4,9)] octacosa-5,18-diene-2,3,10,16-tetraone, also known as 5,6-dehydro-ascomycin as disclosed in Example 8 in EP 626 385 (hereafter referred to as Compound C); [0015] Imidazolylmethyloxyascomycin, as disclosed in Example 1 and as compound of formula I in WO 97/08182, contents of which are incorporated herein by reference (hereafter referred to as Compound D); [0016] 32-O-(1-hydroxyethylindol-5-yl)ascomycin, also known as Indolyl-ASC or L-732 531 as disclosed in Transplantation 65 (1998) 10-18, 18-26, on page 11, FIG. 1 (hereafter referred to as Compound E); and [0017] (32-deoxy-32-epi-N-1-tetrazolyl)ascomycin, also known as ABT-281 as disclosed in J. Inv. Derm. 112 (May 1999), 729-738, on page 730, FIG. 1 (hereafter referred to as Compound F). [0018] FK 506, Compounds A, B, C, D, E, and F are preferred ascomycins, particularly preferred are Compounds A, B, and C, especially Compound A. [0019] The active agent is e.g. present in the compositions of this invention in an amount of from 0.05 to 3% by weight, e.g. from 0.1 to 2% by weight, e.g. from 0.4 to 1% by weight based on the total weight of the composition. [0020] The active agent may be dissolved, e.g. partially dissolved in the vehicle. In a further aspect the active agent may be in suspension, e.g. partially in suspension in the vehicle. Preferably the active agent is partially dissolved in the vehicle. [0021] Preferably the active agent may be used in a micronized form. The suspension may contain particles of ascomycin of from 5, e.g. from 10, to about 90, preferably to about 25 microns in diameter. The particles of the ascomycin may be produced in conventional manner, e.g. by grinding or milling. [0022] If desired further active agents may be present. [0023] The carrier vehicle comprises means to retain water in the outer skin layer, e.g. moisturizers. [0024] Under "means to retain water in the outer skin layer" is to be understood, e.g. a pharmaceutically acceptable moisturizer, capable of e.g. penetrating and residing in the outer skin layer, e.g. the stratum corneum, and e.g. absorbing, holding and retaining moisture to increase the moisture content of the skin. [0025] Means to retain water in the outer skin layer, e.g. moisturizers, e.g. as described in Dermatika, Eds. R. Nieder, J. Ziegenmayer, Wissenschaftliche Verlagsgesellschaft Stuttgart 1992, 271-272, may be selected from a group comprising [0026] i) a urea, e.g. urea and its derivatives, e.g. monoacetyl urea, 1-dodecyl urea, 1,3-didodecyl urea, 1,3 diphenyl urea or cyclic urea derivatives, e.g. 1-methyl-4-imidazolin-2-one-3-methylenedecanoate. Urea may be commercially available from e.g. Merck, Germany; [0027] ii) an inorganic salt, e.g. sodium chloride, e.g. as known and commercially available from e.g. Merck, Germany; and [0028] iii) a carboxylic acid, e.g. a mono carboxylic acid or a cyclic carboxylic acid, salts and derivatives thereof. Particularly preferred are e.g. lactic acid; glycolic acid; lactic acid sodium and/or ammonium salt, e.g. sodium lactate, e.g. as known and commercially available from e.g. Merck, Germany; glycolic acid sodium and/or ammonium salt; lactamide; lactamidopropyl-triammonium chloride; sodium cocoyl lactylate; 2-pyrrolidone-5-carboxylate; 2-pyrrolidone-5-carboxylate sodium and/or calcium salt, e.g. sodium 2-pyrrolidone-5-carboxylate, e.g. as known and commercially available under the name Sodium PCA from A+E Connock, UK; 2-pyrrolidone-5-carboxylate derivatives of amino acids, e.g. lysin or arginin; or acyl esters, having e.g. a chain length of C.sub.1-C.sub.30, e.g. C.sub.3-C.sub.18, branched or unbranched, e.g 2-pyrrolidone-5-carboxylic laurate (Fiedler, H. P. "Lexikon der Hilfsstoffe fur Pharmazie, Kosmetik und angrenzende Gebiete", Editio Cantor Verlag Aulendorf, Aulendorf, 4th revised and expanded edition (1996), 1, p. 720; 2, p. 1013-1017; 2, p. 1303) [0029] Mixtures thereof may also be used. Continue reading about Topical compositions comprising ascomycins... Full patent description for Topical compositions comprising ascomycins Brief Patent Description - Full Patent Description - Patent Application Claims Click on the above for other options relating to this Topical compositions comprising ascomycins patent application. ###  How KEYWORD MONITOR works... a FREE service from FreshPatents1. Sign up (takes 30 seconds). 2. Fill in the keywords to be monitored. 3. Each week you receive an email with patent applications related to your keywords. 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