On September 23, 1999, Buchanan, John; Bohacek, Regine; Vu, Chi B.; Luke, George P. published a patent.Name: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Preparation of heterocyclyl phosphotyrosine derivatives as SH2-mediated signal transduction inhibitors. And the patent contained the following:
Heterocyclic phosphotyrosine derivatives were prepared for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by a PDGF receptor protein, EGF receptor protein, HER2/Neu receptor protein, fibroblast growth factor receptor protein, focal adhesion kinase protein, p130 protein, or p68 protein. For example, BOC-Tyr(PO3Bn2)-OH (BOC = tert-butoxycarbonyl; Bn = benzyl) and the thiazolylamine salt (I)·TFA (four step preparation given) were coupled, the phosphate deprotected, the amine acylated, and the carboxylic acid deprotected to form the title compound (II). In an assay for binding affinities to Src SH2, thirteen compounds of the invention were determined to have IC50 values of < 50μM. In an assay for binding affinities to Zap-70 SH2, fourteen compounds of the invention exhibited IC50 values of < 50μM. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds for proliferative disease, cancer, restenosis, osteoporosis, inflammation, allergies, cardiovascular disease, or immunosuppression. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Name: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
The Article related to peptide heterocyclyl phosphotyrosine preparation signal transduction inhibitor, antitumor heterocyclyl phosphotyrosine preparation antiosteoporotic antiinflammatory antiallergenic immunosuppressant, tyrosine phospho heterocyclyl preparation proliferative disease cardiovascular disease treatment and other aspects.Name: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
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