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Pub. No.:    WO/1998/049152    International Application No.:    PCT/US1998/007942
Publication Date: 05.11.1998 International Filing Date: 23.04.1998
Chapter 2 Demand Filed:    29.10.1998    
C07C 43/285 (2006.01), C07C 43/295 (2006.01), C07C 65/24 (2006.01), C07C 69/92 (2006.01), C07C 205/26 (2006.01), C07C 205/37 (2006.01), C07C 217/90 (2006.01), C07C 235/28 (2006.01), C07C 243/22 (2006.01), C07C 335/26 (2006.01), C07D 215/18 (2006.01), C07D 215/227 (2006.01), C07D 215/38 (2006.01), C07D 277/56 (2006.01), C07D 417/12 (2006.01), C07F 5/02 (2006.01)
Applicants: SMITHKLINE BEECHAM CORPORATION [US/US]; One Franklin Plaza, Philadelphia, PA 19103 (US) (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW only).
DesJARLAIS, Renee, Louise [US/US]; (US) (For US Only).
DUFFY, Kevin, James [GB/US]; (US) (For US Only).
HALBERT, Stacie, Marie [US/US]; (US) (For US Only).
KEENAN, Richard, McCulloch [US/US]; (US) (For US Only).
MICHAUD, Evelyne [FR/US]; (US) (For US Only).
THOMPSON, Scott, Kevin [US/US]; (US) (For US Only).
VEBER, Daniel, Frank [US/US]; (US) (For US Only)
Inventors: DesJARLAIS, Renee, Louise; (US).
DUFFY, Kevin, James; (US).
HALBERT, Stacie, Marie; (US).
KEENAN, Richard, McCulloch; (US).
MICHAUD, Evelyne; (US).
THOMPSON, Scott, Kevin; (US).
VEBER, Daniel, Frank; (US)
Agent: STERCHO, Yuriy, P.; SmithKline Beecham Corporation, Corporate Intellectual Property, UW2220, 709 Swedeland Road, P.O. Box 1539, King of Prussia, PA 19406-0939 (US)
Priority Data:
60/044,906 25.04.1997 US
Abstract: front page image
(EN)Compounds of formula (I), wherein Rl is an aromatic or a heteroaromatic ring; R2 and R3 are H, C1-C8alkyl, aryl, arylC1-C8alkyl, or heteroaryl; R4 is an aromatic or a heteroaromatic ring or an amine; W, X, Y, are independently selected from the group consisting of CH, N, S, or O, provided that at least one of W, X, and Y is a heteroatom, which inhibit protease, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease therewith.
(FR)L'invention concerne des composés de formule (I), dans laquelle R1 est un cycle aromatique ou hétéroaromatique, R2 et R3 sont H, alkyle C1-8, aryle, aryl-alkyleC1-8 ou hétéroaryle; R4 est un cycle aromatique ou hétéroaromatique ou une amine, W, X, Y sont choisis séparément dans le groupe constitué de CH, N, S ou O, à condition qu'au moins un parmi W, X et Y soit un hétéroatome, lesdits composés inhibant la protéase, dont la cathépsine K. L'invention porte aussi sur des compositions pharmaceutiques contenant lesdits composés, sur des méthodes de traitement à l'aide desdites compositions, de maladies se manifestant par une perte osseuse excessive ou une dégradation du cartilage ou de la matrice, dont l'ostéoporose, l'affection gingivale telle que la gingivite et la parodontose, l'arthrite, l'arthrose et la polyarthrite rhumatoïde, la maladie osseuse de Paget, l'hypercalcémie maligne et la maladie métabolique des os.
Designated States: AL, AU, BA, BB, BG, BR, CA, CN, CZ, EE, GE, HU, ID, IL, IS, JP, KP, KR, LC, LK, LR, LT, LV, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, SL, TR, TT, UA, US, UZ, VN, YU.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)