Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1992-01-21
1994-04-19
Tsang, Cecilia
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
548112, 548413, 548414, 548431, 548518, 548557, 548558, 558170, 558174, 562621, 562622, 562623, 562433, 562533, 564153, 514 79, 514 89, 514 91, 514119, 5142328, 5142372, 514296, 514321, 514326, 514422, 514426, 514428, 514575, 514616, 514825, 544126, 544130, 544141, 544157, 544168, 546 23, 546 24, 546200, 546208, C07F 928, C07F 906, C07C 9310, C07C25904, C07C25906, A61K 31675, A61K 3116, A61K 31185
Patent
active
053045491
ABSTRACT:
Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.5 is hydrogen or halogen and their pharmaceutically acceptable salts, which are useful for the control or prevention of degenerative joint diseases or for the treatment of invasive tumors, atherosclerosis or multiple sclerosis are described.
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Dayer J.-M. et al., Proc. Natl. Acad. Sci. USA, 73, 945 (1976).
Johnson-Wint, B., Anal. Biochem., 104, 175 (1980).
Broadhurst Michael J.
Brown Paul A.
Johnson William H.
Lawton Geoffrey
Gould George M.
Hoffmann-La Roche Inc.
Johnston George W.
Silverman Robert A.
Tsang Cecilia
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