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Wo 2009/045539 A2 (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date PCT (10) International Publication Number 9 April 2009 (09.04.2009) WO 2009/045539 A2 (51) International Patent Classification: (74) Agents: WILSON, Mark, A. et al; Nektar Therapeutics, A61K 47148 (2006.01) 201 Industrial Road, San Carlos, California 94070 (US). (21) International Application Number: (81) Designated States (unless otherwise indicated, for every PCT/US2008/01 1523 kind of national protection available): AE, AG, AL, AM, AO, AT,AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, (22) International Filing Date: 3 October 2008 (03.10.2008) CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, (25) Filing Language: English IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY,MA, MD, ME, MG, MK, MN, MW, (26) Publication Language: English MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, (30) Priority Data: RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY,TJ, 60/997,835 5 October 2007 (05.10.2007) US TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW (71) Applicant {for all designated States except US):NEKTAR THERAPEUTICS AL, CORPORATION [US/US]; 490 (84) Designated States (unless otherwise indicated, for every Discovery Drive, Huntsville, Alabama 35806 (US). kind of regional protection available): ARIPO (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, (72) Inventors; and ZW), Eurasian (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM), (75) Inventors/Applicants (for US only): ZHANG, Wen European (AT,BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, [CN/US]; 142 Tottenham Way, Madison, Alabama 35758 FR, GB, GR, HR, HU, IE, IS, IT, LT,LU, LV,MC, MT, NL, (US). RIGGS-SAUTHIER, Jennifer [US/US]; 7917 NO, PL, PT, RO, SE, SI, SK, TR), OAPI (BF, BJ, CF, CG, Smoke Rise Road, Huntsville, Alabama 35802 (US). CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG). HARRIS, J., Milton [US/US]; 3309 Lookout Drive, Huntsville, Alabama 35801 (US). BENTLEY, Michael, Published: D. [US/US]; 4420 Choctaw Circle, Huntsville, Alabama — without international search report and to be republished 35801 (US). upon receipt of that report (54) Title: OLIGOMER-CORTICOSTEROID CONJUGATES (57) Abstract: The invention provides corticosteroids that are chemically modified by covalent attachment of a water soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits a reduced bio- logical membrane crossing rate as compared to the biological membrane crossing rate of the corticosteroid not attached to the water soluble oligomer. OLIGOMER-CORTICOSTEROID CONJUGATES CROSS REFERENCE TO RELATEDAPPLICATION [0001] This application claims the benefit of priority under 35 U.S.C. §119(e) to U.S. Provisional Patent Application No. 60/997,835, the disclosure of which is hereby incorporated by reference. FIELD OF THE INVENTION [0002] This invention comprises (among other things) chemically modified corticosteroids that possess certain advantages over corticosteroids lacking the chemical modification. The chemically modified corticosteroids described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry. BACKGROUNDOF THE INVENTION [0003] Corticosteroids represent a broad class of agents employed in the treatment of individuals suffering from a variety of disorders. In the treatment of an individual suffering from arthritis, for example, administration of a corticosteroid may reduce inflammation. In addition, individuals suffering autoimmune disorders often benefit from the administration of a corticosteroid. Other applications in which corticosteroids have been used include the treatment of individuals suffering from allergic reactions, ankylosing spondylitis, asthma, Crohn's disease dermatological disorders and psoriasis among others. As a class, corticosteroids represent an important and widely used tool in pharmacotherapy. [0004] Although corticosteroids serve an important role in treating patients, their use is sometimes associated with (among other things) CNS side effects, such as insomnia, eurphoria, mood changes, nervousness, personality changes, depression, nausea, headaches and convulsions. [0005] As a consequence, pharmacotherapy with corticosteroids would be improved if these and/or other side effects associated with their use could be decreased. [0006] The present invention seeks to address these and other needs in the art. SUMMARY OF THE INVENTION [0007] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached via a hydrazone linkage to a water-soluble, non-peptidic oligomer. [0008] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached via a hydrazone linkage to a water-soluble, non-peptidic oligomer, wherein the weight average molecular weight of the water-soluble, non-peptidic oligomer is less than 400 Daltons. [0009] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached (either directly or through one or more atoms) at a position other than through the 16 or 17 positions to a water-soluble, non-peptidic oligomer. [0010] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached (either directly or through one or atoms) at a position other than through D-ring atom positions to a water-soluble, non-peptidic oligomer. [0011] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached (either directly or through one or more atoms) at a position selected from the consisting of A-ring atom positions, B-ring atom positions, and C-ring atom positions to a water-soluble, non-peptidic oligomer. [0012] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached (either directly or through one or more atoms) at A-ring atom positions to a water-soluble, non-peptidic oligomer. [0013] In one or more embodiments of the invention, a compound is provided, the compound comprising a corticosteroid residue covalently attached at the 3 position to a water-soluble, non-peptidic oligomer. [0014] Exemplary compounds of the invention include those having the following structure: (Formula I-C) wherein: the dashed line independently represents an optional double bond; R1 is selected from the group consisting of halo (e.g., fluoro, chloro, bromo, iodo) and alkyl; either R2 is selected from the group consisting of hydroxy and alkyl and R3 is selected from the group consisting of hydroxy, alkyl, -OC(O)-alkyl, and -OC(O)- cyclo, or R2 and R3 combine to form a moiety selected from the group consisting of 4 R is selected from the group consisting Of-CH , -CH2-OH, -CH2-halo, -S-CH2-halo, -CH2-O-C(O)-CH3, -CH2-O-C(O)-CH2-CH3, -CH2-PO4, -CH2-O-C(O)-C(CH 3)3, -CH 2-O-C(O)-CH 2-CH 2-CH 2-CH 3 -CH 2-C(O)-O-CH 3 -CH 2-O-C(O)-CH 2-CH 2-C(O)-OH; either R5 is -H and R6 is selected from the group consisting of -H and hydroxy, or R5 and R combine to form carbonyl; R7 is halo; X is a spacer moiety; and POLY is a water-soluble, non-peptidic oligomer. [0015] The "corticosteroid residue" is a compound having a structure of a corticosteroid that is altered by the presence of one or more bonds, which bonds serve to attach (either directly or indirectly) one or more water-soluble, non-peptidic oligomers. In this regard, any compound having corticosteroid activity can be used. Exemplary corticosteroids have a structure encompassed by the structure defined herein as Formula I: (Formula I) wherein: the dashed line independently represents an optional double bond; R1 is selected from the group consisting of halo (e.g., fluoro, chloro, bromo, iodo) and alkyl; either R2 is selected from the group consisting of hydroxy and alkyl and R3 is selected from the group consisting of hydroxy, alkyl, -OC(O)-alkyl, and -OC(O)-cyclo, or R2 and R3 Λ O combine to form a moiety selected from the group consisting of 1 , O CH3 ° / 4 R is selected from the group consisting Of-CH , -CH2-OH, -CH2-halo, -S-CH2-halo, -CH2-O-C(O)-CH3, -CH2-O-C(O)-CH 2-CH3, -CH2-PO4, -CH2-O-C(O)-C(CH 3)3, -CH 2-O-C(O)-CH 2-CH 2-CH 2-CH 3 -CH 2-C(O)-O-CH 3 -CH 2-O-C(O)-CH 2-CH 2-C(O)-OH; either R5 is -H and R6 is selected from the group consisting of -H and hydroxy, or R5 and R6 combine to form carbonyl; and R7 is halo. [0016] In one or more embodiments of the invention, a composition is provided, the composition comprising a compound comprising a corticosteroid residue covalently attached via a stable or degradable linkage to a water-soluble and non-peptidic oligomer, and optionally, a pharmaceutically acceptable excipient. [0017] In one or more embodiments of the invention, a dosage form is provided, the dosage form comprising a compound comprising a corticosteroid residue covalently attached via a stable or degradable linkage to a water-soluble, non-peptidic oligomer, wherein the compound is present in a dosage form. [0018] In one or more embodiments of the invention, a method is provided, the method comprising covalently attaching a water-soluble, non-peptidic oligomer to a corticosteroid.
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