Epoxysuccinic acid derivatives

Details Epoxysuccinic acid derivatives Epoxysuccinic acid derivatives

1994-10-27

1996-09-17

Ramsuer, Robert W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142278, 514252, 514475, 544584, 544146, 544147, 544374, 549548, 549549, A61K 31535, C07D41312

Patent

active

055568530

ABSTRACT:
A compound of the general formula: ##STR1## wherein R.sup.1 represents a carboxyl group which may optionally be esterified or amidated; R.sup.2 represents a cyclic group which may optionally be substituted or a polar group; n is an integer of 0 to 6; R.sup.3 represents hydrogen or a hydrocarbon residue which may optionally be substituted; R.sup.4 represents (1) a hydrocarbon residue which is substituted by an optionally protected amino group or (2) an alkenyl group; or R.sup.3 and R.sup.4 may be combined with the adjacent nitrogen atom to form a heterocyclic group containing at least two hetero atoms, or a salt thereof.
The compound or a salt thereof of the present invention inhibits thiol proteases such as cathepsin L and B and serves well as a prophylactic/therapeutic agent for bone diseases such as osteoporosis.

REFERENCES:
patent: 4333879 (1982-06-01), Tamai et al.
patent: 4418075 (1983-11-01), Tamai et al.
patent: 4507297 (1985-03-01), Masaki et al.
patent: 4596803 (1986-06-01), Masaki et al.
Fukushima et al., "Metabolic Fate of Loxistatin in Rat" Xenobiotica, 1990, vol. 20, No. 10, 1043-1051.

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