β-turn peptidomimetic cyclic compounds

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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Details

C530S330000, C530S331000

Reexamination Certificate

active

06881719

ABSTRACT:
Proteolytically stable small molecule β-turn peptidomimetic compounds have been identified as agonists or antagonists of neurotrophin receptors, such as TrkA. A compound of particular interest binds the immunoglobulin-like C2 region of the extracellular domain of TrkA, competes the binding of another TrkA ligand, affords selective trophic protection to TrkA-expressing cell lines and neuronal primary cultures, and induces the differentiation of primary neuronal cultures. The small β-turn peptidomimetic compounds of the invention can activate a tyrosine kinase neurotrophin receptor that normally binds a relatively large protein ligand. Such compounds that bind the extracellular domain of Trk receptors are useful pharmacological agents to address disorders where Trk receptors play a role, by targeting populations selectively.

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patent: WO 9521193 (1995-08-01), None
“Confirmations of Peptidomimetics Formed by SNAr Macrocyclizations: 13- to 16-Membered Ring Systems”, By Zhicheng Wang et al., Chem. Eur. Journal 1999, 5, No. 11, pp. 3273-3276.
“Stereochemical Implications on Diversity in β-Turn Peptidomimetic Libraries”, By Yangbo Feng et al., Journal Org. Chem. 1999, 64, pp. 9175-9177.
“SNAr Cyclizations to Form Cyclic Peptidomimetics of β-Turns”, By Yangbo Feng et al., Am. Chem. Soc. 1998, 120, pp. 10768-10769.
“Solid-Phase SNAr Macrocyclizations to Give Turn-Extended-Turn Peptidomimetics”, By Yangbo Feng et al., Chem. Eur. Journal, 1999, 5, No. 11, pp. 3261-3272.
“Resin Effects in Solid Phase SNAr and SN2 Macrocyclizations”, By Yangbo Feng et al., Biotechnology and Bioengineering (Combinatorial Chemistry), vol. 71, No. 1, Winter, 2000, pp. 1-8.
“A Designed Peptidomimetic Agonistic Ligand of TrkA Nerve Growth Factor Receptors”, By Sergei Maliartchouk et al., Mol. Pharmacol. 2000, vol. 57, No. 2, pp. 385-391.

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