Abstract: The invention relates to an acylated peptide, namely a compound of formula (I), wherein n is 0 to 15, X is oxalyl PTI is the bivalent radical of tyrosine or (preferably) the bivalent radical of phosphotyrosine or a phosphotyrosine mimetic, AA stands for a bivalent radical of a natural or unnatural amino acid, and Y is secondary amino group, or a salt thereof, said compound being useful for the treatment of diseases that respond to inhibition of the interaction of (a) protein(s) comprising (an) SH2 domain(s) and a protein tyrosine kinase or a modified version thereof.

Abstract: The present invention relates to non-phosphorus containing O-malonyltryrosyl compounds, derivatives thereof, uses of the O-malonyltryrosyl compounds in the synthesis of peptides, and O-malonyltryrosyl compound-containing peptides. The O-malonyltyrosyl malonyltyrosyl compounds and O-malonyltryrosyl compound-containing peptides of the present invention are uniquely stable to phosphotases, capable of crossing cell membranes, suitable for application to peptide synthesis of O-malonyltryrosyl compound-containing peptides, and amenable to prodrag defivatization for delivery into cells. The present invention also provides for O-malonyltryrosyl compound-containing peptides which exhibit inhibitory potency against binding interactions of receptor domains with phosphotyrosyl-containing peptide ligands.

Abstract: The present invention relates to a method of treating hyperproliferative epithelial lesions by topical administration. The method prevents growth and actively cross-links these aberrant cells, thereby killing the cells. The present invention is useful in control and prevention of hyperproliferative epithelial disorders, such as HPV-infected cell lesions, actinic keratosis, melanomas, and malignant and pre-malignant carcinomas.

Abstract: The disclosure is concerned with providing phosphonic acid-containing derivatives of phenylalanine and optically active isomers thereof, which are functionalized in a manner which makes them suitable for facile incorporation into peptides using standard solid-phase or solution-phase techniques.

Abstract: The disclosure is concerned with providing phosphonic acid-containing derivatives of phenylalanine and optically active isomers thereof, which are functionalized in a manner which makes them suitable for facile incorporation into peptides using standard solid-phase or solution-phase techniques. The disclosure is also concerned with providing an advantageous one-step reaction method for preparing benzylic .alpha.,.alpha.-difluorophosphonates from corresponding benzylic ketophosphonates.

Abstract: There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH.sub.2 --, --CHF--, --CF.sub.2, --CHOH-- or --C(O)--;R.sup.6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl;Fmoc is 9-fluorenylmethyloxycarbonyl; and* indicates a chiral carbon atom.The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R.sup.4 and R.sup.5 are C.sub.1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R.sup.4 and R.sup.5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.

Abstract: Fluorinated derivatives 3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoro-17-methylmorphinan ("fluorooxymorphone"; FOXY, compound 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoromorphin an (CYCLOFOXY, compound 18) are prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11, respectively. Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6.alpha.-triflate functions in 8 and 16. The synthetic procedures were suitable for the production of the corresponding positron emitting .sup.18 F-labeled analogs .sup.18 F-FOXY and .sup.18 F-CYCLOFOXY, which are useful for in vivo studies of the opioid receptor system using positron emission transaxial tomography. In addition, the tritiation of FOXY (10) to high specific activity is noted.