4-substitued-3-[1 or 2 amino acid residue]-azetidin-2-one deriva

Details 4-substitued-3-[1 or 2 amino acid residue]-azetidin-2-one deriva 4-substitued-3-[1 or 2 amino acid residue]-azetidin-2-one deriva

1997-09-08

1999-11-16

Tsang, Cecilia

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548920, 514210, 514 19, 540200, C07D20500

Patent

active

059861088

ABSTRACT:
Disclosed herein are azetidin-2-one compounds which exhibit excellent cysteine proteinase inhibitory activity. The compounds are 4-substituted-3-{1 or 2 amino acid residue}-azetidin-2-ones of forumula I ##STR1## wherein AAR is a 1 or 2 acid residue, and R.sub.1 and R.sub.2 are as defined herein. The compounds can be used in the treatment of various diseases such as muscular dystrophy, bone resorption disorders, myocardial infarction and cancer metastasis.

REFERENCES:
Firestone, Raymond A. et al, "Monocyclic .beta.-Lactam Inhibitors of Human Leukocyte Elastase," Tetrahedron, vol. 46, No. 7, pp. 2255-2262, 1990.
2-Azetidinecarboxylic acid, 3-[[[[(4-butyl-2,3-dioxo-1-piperazinyl) carbonyl] amino] phenylacetyl] amino]-4-oxo-, methyl ester, [2R-[2.alpha., 3.alpha.(R*)]]-, RN 84237-30-9.
Allen Krantz, et al, Peptidyl (Acyloxy)methyl Ketones and the Quiescent Affinity Label Concept: The Departing Group as a Variable Structural Element in the Design of Inactivators of Cysteine Proteinases, Biochemisty 1991, 30, 4678-4687.
Dieter Hoppe and Thomas Hilpert, "Enantioselective Total Synthesis of the Fungicide .beta.-Lactam Antibiotic (-)-(2S,5S)-2(2-Hydroxyethyl) Clavam and its (+)-(2S,5S)-Epimer", Tetrahedon, vol. 43, No. 11, pp. 2467-2474, 1987.
Toshiyuki Konosu and Sadao Oida, Enantiocontrolled Synthesis of the Antifungal .beta.-Lactam (2R,5S)-2-(Hydroxymethyl)clavam, Chem. Pharm. Bull. 39(9) pp. 2212-2215, (1991).
J.C. Arnould, P. Boutron, M.J. Pasquet, "Synthesis and Antibacterial Acitviity of C4 Substituted Monobactams", Eur. J. Med Chem. (1992) 27; pp. 131-140.
Hans-Ulrich Demuth"Recent Developments In Inhibiting Cysteine and Serine Proteases", J. Enzyme Inhib. 1990, vol. 3, pp. 249-278.
C.M. Cimarusti et al, "4-Alkylated Monobactams", Tetrahedon, (1983), vol. 39, No. 15, pp. 2577-2589.

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