C07K5/06139

Functionalized peptides as antiviral agents

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: ##STR00001##
which inhibit coronavirus replication activity. The invention further relates to pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable slat thereof, and methods of treating or preventing a coronavirus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.

METHOD FOR MODIFYING AMINO GROUP IN MOLECULE WITH THE ZOLINIUM AND USE THEREOF
20220177515 · 2022-06-09 ·

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.

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Chiral specific boron-containing compounds and their use in treating cancer or amyloidosis
11325942 · 2022-05-10 · ·

Useful chiral specific boron-containing compounds, such as boronate, boronate esters, boranamines, borane diamines, boranamine thioesters, and boronic mono/di-thioesters, have been prepared. These compounds and compositions containing them are useful as anti-cancer or anti-amyloidosis agents.

COMPOSITIONS AND METHODS FOR ASSESSING EYE VASCULATURE
20220016269 · 2022-01-20 ·

Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.

BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Compositions and methods for assessing eye vasculature
11160880 · 2021-11-02 · ·

Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.

A GROUP OF PEPTIDE DERIVATIVE OMICSYNINS WITH ANTIVIRAL ACTIVITY AND USES THEREOF

This disclosure related to a group of peptide derivative Omicsynins with antiviral activity against influenza virus and coronavirus. It also related uses of these derivatives, the chemical formula of the peptide derivative Omicsynins is shown in formula (1):

##STR00001##

TABLE-US-00001 R1—R4 are shown in the following table. NO. substituent1 substituent2 substituent3 R.sub.1 [00002]embedded image [00003]embedded image [00004]embedded imageBasic amino-acid side chains including lysine, histidine, citrulline residues, and etc. R.sub.2 [00005]embedded image —CH(CH.sub.3).sub.2, —CH(CH.sub.3)CH.sub.2CH.sub.3 embedded image—CH.sub.2CH(CH.sub.3).sub.2 Neutral amino-acid side chain including tryptophan, serine, threonine, cysteine residues and etc. R.sub.3 [00006]embedded image [00007]embedded image [00008]embedded image[00009]embedded imageR.sub.3 including tyrosine, lysine, histidine, citrulline residues, and etc. R.sub.4 —CH.sub.2OH —CHO R.sub.4 including —CH.sub.2NH.sub.2, —CH═NH,— CH═NOH, —COOH, —COOR.sub.5 (R.sub.5 represents alkyl groups containing 1-3 carbons), -CONH.sub.2 and etc.

ENZYME INHIBITORS

The present invention provides compounds of formula (I): Formula (I) compositions comprising such compounds; the use of such compounds in therapy; and methods of treating patients with such compounds; wherein A, Y, n, R1, R2.sup.A, R2.sup.B, R3 and *1 are as defined herein.

##STR00001##

Bicyclic compound as a caspase inhibitor

A compound represented by formula (I), a pharmaceutically acceptable salt or tautomer thereof, and an application of the compound as a caspase inhibitor. ##STR00001##