Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1996-07-10
1999-11-16
Tsang, Cecilia J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
514 17, 514 18, 530330, 530331, 562571, A61K 3805
Patent
active
059858389
ABSTRACT:
Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.
REFERENCES:
patent: 5055451 (1991-10-01), Krantz et al.
patent: 5374623 (1994-12-01), Zimmerman
patent: 5430128 (1995-07-01), Chapman
Dolle, R.E., et al. "P1 Aspartate-Based Peptide alpha-((2,6-Dichlorobenzoyl) oxy) methyl Ketones as Potent Time Dependent Inhibitors of Interleukin-1beta-Converting Enzyme," J. Med. Chem. 37, pp. 563-564 (1994).
Thornberry, N.A., et al. "Inactivation of Interleukin-1beta Converting Enzyme by Peptide (Acyloxy)methyl Ketones," Biochemistry 33, pp. 3934-3940 (1994).
Sleath, P.R. et al. "Substrate Specificity of the Protease That Processes Human Interleukin-1beta," J. Biol. Chem. 24, pp. 14526-14528 (1990).
Thornberry, N.A., et al. "A Novel Heterodimeric Cysteine Protease is Required for Interleukin-1beta Processing in Monocytes," Nature 356, pp. 768-774 (1992).
Krantz, A., 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," Biochemistry 30, pp. 4678-4687 (1991).
Ator Mark A.
Awad Mohamed M. A.
Chaturvedula Prasad V.
Dolle Roland E.
Hoyer Denton W.
Dixon Lisa A.
Haley, Jr. Esq. James F.
Lukton David
Tsang Cecilia J.
Vertex Pharmaceuticals Inc.
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