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Last Updated: February 18, 2020

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Patent: 6,506,785

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Summary for Patent: 6,506,785
Title: Treating or preventing the early stages of degeneration of articular cartilage or subchondral bone in mammals using carprofen and derivatives
Abstract: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): ##STR1## where A is hydroxy, (C.sub.1 -C.sub.4)alkoxy, amino, hydroxy-amino, mono-(C.sub.1 -C.sub.2)alkylamino, di-(C.sub.1 -C.sub.2)alkylamino; X and Y are independently H or (C.sub.1 -C.sub.2)alkyl; and n is 1 or 2; R.sup.6 is halogen, (C.sub.1 -C.sub.3)alkyl, trifluoromethyl, or nitro; R.sup.9 is H; (C.sub.1 -C.sub.2)alkyl; phenyl or phenyl-(C.sub.1 -C.sub.2)alkyl, where phenyl is optionally mono-substituted by fluoro or chloro; --C(.dbd.O)--R, where R is (C.sub.1 -C.sub.2)alkyl or phenyl, optionally mono-substituted by fluoro or chloro; or --C(.dbd.O)--O--R\', where R.sup.1 is (C.sub.1 -C.sub.2)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.beta.); increased tumor necrosis factor alpha (TNF.alpha.); increased ratio of IL-1.beta. 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.beta.); 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.
Inventor(s): Evans; Nigel A. (East Lyme, CT), Kilroy; Carolyn R. (Old Lyme, CT), Lundy; Kristin M. (Groton, CT), Pelletier; Jean-Pierre (St. Lambert, CA), Ricketts; Anthony P. (Stonington, CT)
Assignee: Pfizer, Inc. (New York, NY)
Application Number:09/283,993
Patent Claims:see list of patent claims

Details for Patent 6,506,785

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Smith And Nephew SANTYL collagenase OINTMENT;TOPICAL 101995 001 1965-06-04   Start Trial Pfizer, Inc. (New York, NY) 2018-05-22 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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