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1. 发明授权

US06506785B2 Treating or preventing the early stages of degeneration of articular cartilage or subchondral bone in mammals using carprofen and derivatives 失效
公开(公告)号：US06506785B2
公开(公告)日：2003-01-14
申请号：US09283993
申请日：1999-04-01
申请人： Nigel A. Evans , Carolyn R. Kilroy , Kristin M. Lundy , Jean-Pierre Pelletier , Anthony P. Ricketts
发明人： Nigel A. Evans , Carolyn R. Kilroy , Kristin M. Lundy , Jean-Pierre Pelletier , Anthony P. Ricketts
IPC分类号： A61K3140
CPC分类号： A61K31/405
摘要： Treating or preventing the early stages of degeneration of articular cartilage or subchondral bone in the affected joint of a mammal is accomplished by administering a chondroprotective compound of Formula (I): where A is hydroxy, (C1-C4)alkoxy, amino, hydroxy-amino, mono-(C1-C2)alkylamino, di-(C1-C2)alkylamino; X and Y are independently H or (C1-C2)alkyl; and n is 1 or 2; R6 is halogen, (C1-C3)alkyl, trifluoromethyl, or nitro; R9 is H; (C1-C2)alkyl; phenyl or phenyl-(C1-C2)alkyl, where phenyl is optionally mono-substituted by fluoro or chloro; —C(═O)—R, where R is (C1-C2)alkyl or phenyl, optionally mono-substituted by fluoro or chloro; or —C(═O)—O—R′, where R1 is (C1-C2)alkyl. This treatment ameliorates, diminishes, actively treats, reverses or prevents any injury, damage or loss of articular cartilage or subchondral bone subsequent to said early stage of said degeneration. Whether or not a mammal needs such treatment is determined by whether or not it exhibits a statistically significant deviation from normal standard values in synovial fluid or membrane from the affected joint, with respect to at least five of the following substances: increased interleukin-1 beta (IL-1&bgr;); increased tumor necrosis factor alpha (TNF&agr;); increased ratio of IL-1&bgr; to IL-1 receptor antagonist protein (IRAP); increased expression of p55 TNF receptors (p55 TNF-R); increased interleukin-6 (IL-6); increased leukemia inhibitory factor (LIF); decreased insulin-like growth factor-1 (IGF-1); decreased transforming growth factor beta (TGF&bgr;); decreased platelet-derived growth factor (PDGF); decreased basic fibroblast growth factor (b-FGF); increased keratan sulfate; increased stromelysin; increased ratio of stromelysin to tissue inhibitor of metalloproteases (TIMP); increased osteocalcin; increased alkaline phosphatase; increased cAMP responsive to hormone challenge; increased urokinase plasminogen activator (uPA); increased cartilage oligomeric matrix protein; and increased collagenase.

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