Abstract:
The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
Abstract:
Methods and reagents for esterification of biological molecules including proteins, polypeptides and peptides. Diazo compounds of formula I: where R is hydrogen, an alkyl, an alkenyl or an alkynyl, RA represents 1-5 substituents on the indicated phenyl ring and RM is an organic group, which includes a label, a cell penetrating group, a cell targeting group, or a reactive group or latent reactive group for reaction to bond to a label, a cell penetrating group, or a cell targeting group, among other organic groups are useful for esterification of biological molecules. Also provided are diazo compounds which are bifunctional and trifunctional coupling reagents as well as reagents for the synthesis of compounds of formula I.
Abstract:
A method for making diazo-compounds, diazonium salts thereof and other protected forms of these compounds. Diaz-compounds are prepared by reaction of a tertiary phosphine reagent carrying a reactive carbonyl group with an azide. The reaction can also generate an acyl triazene which can be converted thermally or by addition of base to form the diazo-compound or the acyl triazene can be isolated. The method is particularly useful for conversion of azides carrying one or more electron withdrawing groups to diazo-compounds. The method can be carried out in aqueous medium under mild conditions and is particularly useful for conversion of azido sugars to diazo-compound and diazonium salts thereof under physiological conditions. Tertiary phosphine reagents, particularly those that are water-soluble, and precursors for preparation of the reagents are provided.
Abstract:
This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
Abstract:
A dye having a representative formula as follows and an ink providing waterfast printing having the dye, in which a surfactant is not essential: ##STR1##
Abstract:
A novel process for preparing 2-diazo-3-trisubstituted silyloxy-3-butenoates, synthons useful in the conversion of 3-substituted-4-acetoxy azetidinones and penicillin to thienamycin, imipenem and other carbapenem antibiotic compounds is provided, comprising the reaction of the appropriate diazo acetoacetate with the substituted silane, base and salt.
Abstract:
A positively operating radiation-sensitive mixture comprising a binder which is insoluble in water but soluble or at least swellable in aqueous alkaline solution, and as a photoactive component a polyfunctional .alpha.-diazo-.beta.-keto ester of the general formula I ##STR1## in which R.sup.1 denotes an aliphatic, cycloaliphatic or araliphatic or aromatic radical having 4 to 20 carbon atoms, in which individual CH.sub.2 groups can be replaced by oxygen or sulfur atoms or by ##STR2## or NH groups and/or contain keto groups, X denotes an aliphatic, cycloaliphatic, carbocyclic, heterocyclic or araliphatic radical having 2 to 22 carbon atoms, in which individual CH.sub.2 groups can be replaced by oxygen or sulfur atoms or by the groups --NR.sup.2 --, --C(O)--O--, --C(O)--NR.sup.2 --, --C(O)-- ##STR3## --NR.sup.2 --C(O)--NR.sup.3 --, --O--C(O)--NR.sup.2 --, --C(O)-- ##STR4## or --O--C(O)--O--, or CH groups can be replaced by ##STR5## in which R.sup.2 and R.sup.3 independently of one another represent hydrogen or an aliphatic, carbocyclic or araliphatic radical,m denotes an integer from 2 to 10 andn denotes an integer from 0 to 2, whereinm-n is .gtoreq.2,is described.The radiation-sensitive mixture is particularly suitable for exposure using radiation of wavelength 190 to 300 nm.
Abstract:
The present invention relates to a group of organic chelators whose affinity for calcium ion in solution is increased by electromagnetic radiation. Specifically, the chelators are related to BAPTA and utilize the addition of an electron-withdrawing group (e.g., diazocarbonyl) to a ring of BAPTA, para to the amino group. Photochemical rearrangement of the diazoacetyl group converts the group to the electron-donating carboxymethyl group, causing the calcium ion efficiency to increase 25 to 50 fold. These chelators when incorporated into rat fibroblasts either by microinjection or by incubation as the membrane-permeable, enzymatically-labile tetraacetoxymethyl ester and flash-photolyzed cause a drop in intracellular free calcine ion to or below resting valves of about 10.sup.-7 M. These chelators are used to generate controlled fast removal of intracellular free calcium ion to mimic or modulate a number of important cellular responses, especially in nerve or muscle.