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1. (WO2007006714) CYSTEINE PROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/006714    International Application No.:    PCT/EP2006/063950
Publication Date: 18.01.2007 International Filing Date: 06.07.2006
IPC:
C07D 487/04 (2006.01), A61K 31/407 (2006.01), A61P 19/10 (2006.01)
Applicants: MEDIVIR AB [SE/SE]; Lunastigen 7, S-141 44 Huddinge (SE) (For All Designated States Except US).
KANGASMETSA, Jussi [SE/GB]; (GB) (For US Only).
HISCOCK, Stephen [GB/GB]; (GB) (For US Only).
JOHNSON, Tony [GB/GB]; (GB) (For US Only).
SAMUELSSON, Bertil [SE/SE]; (SE) (For US Only).
TOZER, Matt [GB/GB]; (GB) (For US Only).
GRABOWSKA, Urszula [GB/GB]; (GB) (For US Only)
Inventors: KANGASMETSA, Jussi; (GB).
HISCOCK, Stephen; (GB).
JOHNSON, Tony; (GB).
SAMUELSSON, Bertil; (SE).
TOZER, Matt; (GB).
GRABOWSKA, Urszula; (GB)
Agent: TEUTEN, Andrew; Sagittarius IPC Ltd, Taylor House, 39 High Street, Marlow, Buckinghamshire SL7 1AF (GB)
Priority Data:
0513841.7 07.07.2005 GB
Title (EN) CYSTEINE PROTEASE INHIBITORS
(FR) INHIBITEURS DE CYSTÉINE PROTÉASE
Abstract: front page image
(EN)Compounds of the formula II wherein R1 and R1, are halo; or one of R1 and R1, is halo, and the other is is H; R2 is R4, -C(=O)R4; -OC(=O)R4, -S(=O)nR4, -S(=O)nNRdRe; R3 is H, -OR4, -SR4; R3' is H; or R3 and R3' together define =O; R4 is -C1C6 alkyl, -C0-C3alkylenecarbocyclyl or -C0-C3alkyleneheterocyclyl, any of which is optionally substituted with up to three substituents selected from R7; R5 is -C1C5 alkyl, -CH2CR5'C3-C4-cycloalkyl; R5' is H; or R5 and R5' together with the carbon to which they are attached define C4-C6-cycloalkyl; R5' is H, C1C2 alkyl, C1C2 haloalkyl, hydroxyl, OC1C2alkyl, fluoro; E is -C(=O)-, -S(=O)m-, -NRaS(=O)m-, -NRaC(=O)-, -OC(=O)-, -CRbRc-; R6 is a stable, optionally substituted, monocyclic or bicyclic carbocycle or heterocycle, wherein the, or each, ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepisn K, such as osteoporosis, osteoarthritis, rhuematoid arthritis or bone metastases.
(FR)La présente invention a trait à des composés de formule II dans laquelle R1 et R1' sont halo; ou un parmi R1 et R1' est halo, et l'autre est H; R2 est R4, -C(=O)R4; -OC(=O)R4, -S(=O)nR4, -S(=O)nNRdRe; R3 est H, -OR4, -SR4; R3' est H; ou R3 et R3' ensemble représentent =O; R4 est -C1C6 alkyle, -C0-C3alkylènecarbocyclyle ou -C0-C3alkylènehétérocyclyle, dont un quelconque est éventuellement substitué par un jusqu'à trois substituants choisis parmi R7; R5 est -C1C5 alkyle, -CH2CR5'C3-C4-cycloalkyle; R5' est H; ou R5 et R5' ensemble avec le carbone auquel ils sont liés représentent C4-C6-cycloalkyle; R5' est H, C1C2 alkyle, C1C2 haloalkyle, hydroxyle, OC1C2alkyle, fluoro; E est -C(=O)-, -S(=O)m-, -NRaS(=O)m-, -NRaC(=O)-, -OC(=O)-, -CRbRc-; R6 est un carbocycle ou hétérocycle monocyclique ou bicyclique stable, éventuellement substitué, dans lequel le ou chaque noyau comprend 4, 5 ou 6 atomes cycliques et 0 à 3 hétéroatomes choisis parmi S, O et N. Lesdits composés sont utiles dans le traitement de troubles caractérisés par une expression anormale ou une activation de la cathepsine K, tels que l'ostéoporose, l'ostéoarthrite, la polyarthrite rhumatoïde ou les métastases osseuses.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)