Src family SH2 domain inhibitors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546292, 546297, 546314, 546315, A61K 3144, C07D21172, C07D21184, C07D21170, C07D21182

Patent

active

060544708

ABSTRACT:
This invention relates to compounds of formula (1): ##STR1## wherein Ring a, A, B, C, D, E, R and Q are defined herein. These compounds possess the ability to disrupt the interaction between regulatory proteins possessing one or more SH2 domains and their native ligands.

REFERENCES:
patent: 5580979 (1996-12-01), Bachovchin
Songyang, Zhou et al; SH2 Domains Recognize Specific Phosphopetide Sequences, Cell. vol. 72, 767-773, Mar. 12, 1993.
Gilmer, T. et al; Peptide Inhibitors of src SH3-SH2 Phosphoprotein Interactions, The Journal of Biological Chemistry vol. 269, No. 50 Issue of Dec. 16, pp. 31711-31719.
Ye, Bin et al; L-0-(2-Malonyl) tyrosine: a New Phosphotyrosyl Mimetic for the Preparation of Src Homology 2 Domain Inhibitory Peptides, J. Med. Chem. 1995, 38, 4270-4275.
Burke, Terrence R. Jr. et al; Conformationally Constrained Phosphotyrosyl Mimetics Designed as Monomeric Src Homology 2 Domain Inhibitors, J. Med. Chem. 1995, 38, 1386-1396.
Wange, Ronald J. et al; F.sub.2 (Pmp).sub.2 -TAM .zeta..sub.3 a Novel Competitive Inhibitor of the Binding of ZAP-70 to the T Cell Antigen Receptor, Blocks Early T Cell Signaling,.
Shahripour, A.. et al; Design, Synthesis and Structure Activity Studies of Peptidomimetic Ligands Targeting the pp60 src SH2 Domain, Parke-Davis, 211.sup.th ACS National Meeting Mar. 1996, Poster #194.
Para, K.S. et al; Design of Novel Peptidomimetic Ligands Targeting the pp60srcSH2 Domain: Transposed Sidechain and Rigid Scaffold Modifications, Parke-Davis, 211.sup.th ACS National Meeting Mar. 1996, Poster #195.
Jian Min Fu; Design and Synthesis of a Pyridone-Based Phosphotyrosine Mimetic, XP-002101974, Bioorganic & Medicinal Chemistry Letters 8, (1998), 2813-2816.

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