The present disclosure provides a method of preparing a compound of Formula I, wherein R.sup.1 is C.sub.1-C.sub.4 alkyl; R.sup.2 is C1-C4 alkyl; and R.sup.3 is selected from the group consisting of C.sub.1-C.sub.6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess.

##STR00001##

The present invention is directed to novel bifunctional CTI-CTI and CBI-CTI dimers of the formula:
F.sup.1-L.sup.1-T-L.sup.2-F.sup.2
where F.sup.1, L.sup.1, T, L.sup.2 and F.sup.2 are as defined herein, useful for the treatment for proliferative diseases, where the inventive dimers can function as stand-alone drugs, payloads in antibody-drug-conjugates (ADCs), and linker-payload compounds useful in connection with the production or administration of such ADCs; and to compositions including the aforementioned dimers, linker-payloads and ADCs, and methods for using these dimers, linker-payloads and ADCs, to treat pathological conditions including cancer.

The present disclosure relates to a method for modifying or marking an amino group in a molecule, wherein the amino group in the molecule is modified or marked with zolinium(s) shown in the following formula 1, wherein the molecule comprises amino acid ester, aminoamide, or peptide/protein. The method has advantages of economy and site selectivity, and has huge potential application value in the field such as pharmaceutical molecular synthesis, probe molecule and diagnostic marker reagent development.

The present disclosure concerns inhibitors of Norovirus protease that are suitable for use against any genotype of Norovirus, including at least GII.4 Norovirus proteases. In particular embodiments, specific compositions are encompassed, including their use for prevention or treatment of Norovirus infection in an individual.

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L, L.sup.1, L.sup.2, M and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

##STR00001##

Anti-lymphoma plant virus particles are described. The anti-lymphoma plant virus particles include a filamentous or rod-shaped plant virus particle linked to an antimitotic agent. A therapeutically effective amount of an anti-lymphoma plant virus particle can be administered to a subject to provide a method of treating lymphoma.

The present invention is to provide a method for producing a peptide containing an N-alkylamino acid, which comprises the following Steps (1) to (3). Step (1): a step of mixing an N-terminal protected amino acid or an N-terminal protected peptide with a carboxylic acid halide or a halogenated alkyl formate; Step (2): a step of mixing an amino acid or a peptide in which the N-terminal and the C-terminal are not protected with a trialkylsilylating agent; and Step (3): a step of mixing the product obtained in Step (1) with the product obtained in Step (2).

There is provided an α-carbonyl alkenyl ester and a preparation method therefor, and the α-carbonyl alkenyl ester is further used to react with a primary or secondary amine to prepare an amide. The two reactions are combined to develop an amide bond and peptide bond formation method that directly use carboxylic acids and amines as starting materials and allenones as a condensing reagent. The α-carbonyl alkenyl ester corresponding to an α-amino acid serves as a peptide synthesis building block and is used in solid phase peptide synthesis. The method is carried out under mild reaction conditions, simple to operate, and has a high yield. Compared with existing amide bond condensation reagents, the allenones have the advantages of being simple to prepare, having good stability, a low molecular weight, not racemizing when activating α-chiral carboxylic acids, and is a novel amide bond and peptide bond condensing reagent.

The present invention is directed to novel heteroaryl sulfone-based conjugation handles of the formula: ##STR00001##
(wherein R.sup.1, R.sup.2, Het, D, E, X, Y, Z, m, n, p, q, r, s and t are as defined herein), methods for their preparation, their use in synthesizing antibody drug conjugates, and the resulting antibody drug conjugates made with components having heteroaryl sulfone-based conjugation handles.

The present disclosure provides a method of preparing a compound of Formula I, wherein R.sup.1 is C.sub.1-C.sub.4 alkyl; R.sup.2 is C1-C4 alkyl; and R.sup.3 is selected from the group consisting of C.sub.1-C.sub.6 alkyl, (aryl)alkyl, and (heteroaryl)alkyl in >95% chemical purity and >95% enantiomeric excess. ##STR00001##