Biaryl acetylenes as inhibitors of matrix metalloproteases

Details Biaryl acetylenes as inhibitors of matrix metalloproteases Biaryl acetylenes as inhibitors of matrix metalloproteases

1997-05-15

1999-10-19

Witz, Jean C.

Chemistry: molecular biology and microbiology

Enzyme , proenzyme; compositions thereof; process for...

Enzyme inactivation by chemical treatment

435219, 514569, 562405, C12N 999, C12N 950, A01N 3710, C07C 6300

Patent

active

059687959

ABSTRACT:
Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## where R.sup.15 is selected from the group comprising: HOCH.sub.2, (n--Pr).sub.2 NCH.sub.2, CH.sub.3 CO.sub.2 CH.sub.2, EtOCO.sub.2 CH.sub.2, HO(CH.sub.2).sub.2, CH.sub.3 CO.sub.2 (CH.sub.2).sub.2, HO.sub.2 C(CH.sub.2).sub.2, OHC(CH.sub.2).sub.3, HO(CH.sub.2).sub.4, 3--HO--Ph, and PhCH.sub.2 OCH.sub.2 ; and R.sup.16 is ##STR2## These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempero mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.

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Child, et al., A New Non-steroidal Anti-inflammatory Analgesic: .gamma.-Oxo(1,1'-biphenyl)-4-butanoic Acid (Fenbufen), Arzneim.-Forsch., 30(4A), 695-702 (1980).
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Chiccarelli, et al., Disposition and Metabolism of Fenbufen in several Laboratory Animals, Arzneim.-Forsch., 30(4A), 707-715 (1980).

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