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1. (WO2007006716) CYSTEINE PROTEASE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/006716 International Application No.: PCT/EP2006/063952
Publication Date: 18.01.2007 International Filing Date: 06.07.2006
IPC:
C07D 471/04 (2006.01) ,A61K 31/407 (2006.01) ,A61P 19/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
407
condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19
Drugs for skeletal disorders
Applicants:
MEDIVIR AB [SE/SE]; Lunastigen 7 S-141 44 Huddinge, SE (AllExceptUS)
TICKLE, David [GB/GB]; GB (UsOnly)
PARKES, Kevin [GB/GB]; GB (UsOnly)
TOZER, Matt [GB/GB]; GB (UsOnly)
GRABOWSKA, Urszula [GB/GB]; GB (UsOnly)
Inventors:
TICKLE, David; GB
PARKES, Kevin; GB
TOZER, Matt; GB
GRABOWSKA, Urszula; GB
Agent:
TEUTEN, Andrew; Sagittarius IPC Ltd Taylor House 39 High Street Marlow Buckinghamshire SL7 1AF, GB
Priority Data:
0513839.107.07.2005GB
Title (EN) CYSTEINE PROTEASE INHIBITORS
(FR) INHIBITEURS DE CYSTEINE PROTEASE
Abstract:
(EN) A compound of the formula (II) wherein one of R1 and R2 is halo and the other is H or halo; R3 is -C1-C5 straight or branched chain, optionally fluorinated, alkyl or -CH2CR5C3-C4-Cycloalkyl; R4 is H; R5 is H, C1-C2 alkyl, C1-C2 haloalkyl, hydroxyl, OC1-C2alkyl, fluoro; R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle wherein the or each ring has 4, 5 or 6 ring atoms and 0 to 3 hetero atoms selected from S, O and N; Rb is haloalkyl; Rc is H or C1-C4 alkyl; and pharmaceutically acceptable salts, hydrates or N-oxides thereof have utility in the treatment of disorders characterised by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.
(FR) Composé de formule (II) sachant que R1 et R2 est halo et que l'autre est H ou halo ; R3 est une chaîne -C1-C5 droite ou ramifiée, éventuellement fluorée, alkyle -CH2CR5C3-C4-cycloalkyle; R4 est H; R5 est H, C1-C2 alkyle, C1-C2 haloalkyle, hydroxyle, OC1-C2alkyle, fluoro; R6 est un carbocycle ou hétérocycle monocyclique ou bicyclique stable, éventuellement substitué, et le cycle ou chaque cycle comporte 4, 5 ou 6 atomes de cycle et entre 0 et 3 hétéroatomes pouvant être S, O et N; est haloalkyle; Rc est H ou C1-C4 alkyle; y compris les sels, hydrates ou N-oxydes pharmaceutiquement acceptables d'un tel composé. Ce type de composé est utile pour le traitement de troubles dont la médiation est assurée par une expression ou activation inadéquate de la cathepsine K, du type ostéoporose, arthrose, polyarthrite rhumatoïde ou métastase osseuse.
front page image
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 (ARIPO) (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)
Also published as:
MXMX/a/2008/000201EP1899336BRPI0612568-9JP2009500376US20090023747CN101258153
CA2610817AU2006268752IN9335/DELNP/2007