Biaryl acetylenes as inhibitors of matrix metalloproteases
US5968795A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | May 15, 1997 |
| Grant date | Oct 19, 1999 |
| Priority date | — |
| Expiry date | May 15, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C59/84
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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 provid…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.