Compounds and their use in filtering ultraviolet and / or high-energy visible light

Abstract

The present invention provides a compound of formula (II) or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, wherein Z 1a , X 1a , Ar 1 , X 2a , W 1a , Y 1a , R 1a , R 2a , R 3a , and R 4a have the same meaning as defined in the description and claims. The invention also provides these compounds for use in filtering ultraviolet (UV) and high-energy visible light. The invention also relates to compositions comprising the compounds. The invention also relates to consumer products and packaging materials comprising the compounds. TIFF2025530565000162.tif6087

Description

[Technical Field]

[0001] The present invention relates to novel compounds and their use as ultraviolet (UV) and / or high-energy visible (HEV) light absorbers and / or filters. The present invention also relates to compositions comprising the compounds. The present invention also relates to consumer products and packaging materials comprising the compounds. [Background technology]

[0002] High-energy light from the sun, as well as artificial sources such as ultraviolet and high-energy visible light, are known to cause cell damage. This light is primarily in the 290-320 nm (UVB), 320-400 nm (UVA), and 400-450 nm (HEV) ranges. Photons in this energy range are absorbed by many biological, pharmaceutical, and cosmetic molecules, potentially causing direct photolysis or transferring their energy to oxygen, triggering a cascade of oxidative reactions. In living tissues, ultraviolet and high-energy visible light can damage important cellular components such as DNA and lipids, leading to mutations and cell death that can manifest as cancer, erythema, and accelerated skin aging. Absorption of ultraviolet and high-energy visible light can also degrade important pharmaceutical ingredients, such as the sunscreen active ingredient avobenzone, which typically requires photostabilizers to maintain UVA protection. Foods are also susceptible to UV and high-energy visible light damage, particularly unsaturated fatty acids, such as those in olive oil, and the essential amino acid tryptophan in proteins, which is easily oxidized by photoexcited molecules and oxygen.

[0003] Therefore, molecules that absorb ultraviolet and high-energy visible light and dissipate that energy as heat are desirable. Such filters are particularly useful if they are photostable so they can be used more sparingly, have low fluorescence so they dissipate most of their energy as heat, and are fully biodegradable so they do not persist in the environment or in our tissues, and are not easily absorbed through the skin so they can remain on the surface to provide protection and prevent significant loss through biodegradation pathways within tissues. Many UV filters currently approved as sunscreen actives in the United States fail one or more of these tests and persist in the environment unchanged or as stable xenobiotic breakdown products that are easily absorbed through the skin and accumulate in serum. These sunscreen actives also show dire evidence of effectively mimicking hormones in our tissues, causing environmental damage to sensitive marine ecosystems.

[0004] Therefore, there is a great need for ultraviolet and / or high energy visible light filtering compounds that can match the performance of existing ultraviolet filters and that are preferably biodegradable even by human cells. Summary of the Invention

[0005] The present invention relates to a compound of formula (I): [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, Ar 1 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R za may be replaced by Each R zaare independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: Each R aare independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Each of the alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl; R h is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R a1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R b1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R c1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; Each R bis independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2a But, -(CR c R d ) n and n is an integer selected from 1, 2, or 3; Each R c and R d are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R f is alkylene, which may be interrupted by one or more O or S; R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a But, -OR a , -R a , or -NR a R b or Y 1a is part of formula (A), [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -ORa , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c Rd ) m and m is an integer selected from 1, 2, or 3; Y 1b But, -OR a , -NR b R a , or -R a is selected from however, [ka] but, [ka] provided that it is not However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2-amino-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid), 2-amino-4-oxo-4-(2-(((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate, 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid.

[0006] In some embodiments, the present invention provides a compound of formula (I): [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, Ar 1 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R za may be replaced by Each R za are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR aR b , and -NR b C(O)R a and selected from the group comprising: Each R a are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Each R b is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X2a But, -(CR c R d ) n and n is an integer selected from 1, 2, or 3; Each R c and R d are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R f is alkylene, which may be interrupted by one or more O or S; R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a is a moiety of formula (A), or Y 1a But, -OR a , -R a , or -NR a R b is selected from [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -OR a , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a, -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c R d ) m and m is an integer selected from 1, 2, or 3; Y 1b But, -OR a , -NR b R a , or -R a is selected from However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-amino-4-oxo-4-(2-(((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, and methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate.

[0007] In some embodiments, the present invention provides a compound of formula (II): [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, In the formula, R 1a , R 2a , R 3a , and R 4a are each independently R za and Each R za are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NRa R b , and -NR b C(O)R a and selected from the group comprising: Each R a are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, and -R f1 -R g1 and wherein each of the alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl; R h is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R a1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R b1is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R c1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R f1 is alkylene, which may be interrupted by one or more O or S; R g1 is hydrogen or alkyl, Each R b is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2a But, -(CR c R d ) n and n is an integer selected from 1, 2, or 3; Each R c and R dare independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R f is alkylene, which may be interrupted by one or more O or S; R g is selected from hydrogen, alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a But, -OR a , -R a , or -NR a R b or Y1a is part of formula (A), [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -OR a , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c R d ) m and m is an integer selected from 1, 2, or 3; Y 1b But, -OR a , -NR b R a , or -R a is selected from However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-amino-4-oxo-4-(2-(((3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, (2S)-2-amino-4-oxo-4-(2-(((3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (S)-2-acetamido-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (R)-2-acetamido-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate, 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, 5-(2-aminophenyl)-5-oxopentanoic acid, 4-(2-aminophenyl)-4-oxobutanoic acid, methyl 6-(2-aminophenyl)-6-oxohexanoate, methyl 4-(2-aminophenyl)-2-((tert-butoxycarbonyl)amino)-4-oxobutanoate, butyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, ethyl (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoate, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid diacetate, (R)-2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, 2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, methyl 2-acetamido-4-(2-acetamidophenyl)-4-oxobutanoate, 4-(2-amino-3-(((2R,3S,4R,5R,6S)-3,4,5-trihydroxy-6-((((2S,3S,4R,5R,6S)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)methyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-D-diglucoside), 4-(2-amino-3-(((2R,3S,4R,5R,6S)-3,4-5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-d-glucoside, 2-amino-4-(2-formamido-5-hydroxyphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, 2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (R)-2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (S)-2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, (S-) 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, (R-) 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, methyl (S-)2-amino-4-(2-aminophenyl)-4-oxobutanoate, 2-amino-4-(2-aminophenyl)-4-oxobutanamide, (R)-2-amino-4-(2-aminophenyl)-4-oxobutanamide, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanamide, (S)-2-acetamido-4-(2-acetamidophenyl)-4-oxobutanoic acid, (S)-2-formamido-4-(2-formamidophenyl)-4-oxobutanoic acid, 4-(2-aminophenyl)-4-oxo-2-phenylbutanamide.

[0008] The present invention also relates to a cosmetic or pharmaceutical composition comprising at least one compound according to the invention and, optionally, at least one dermatologically or pharmaceutically acceptable carrier.

[0009] The present invention is based on the unexpected discovery that the compounds described herein are compounds that absorb ultraviolet and / or high-energy visible light. These compounds may be particularly useful for filtering ultraviolet and / or high-energy visible light. The compounds are particularly useful for dissipating the aforementioned energy as heat, absorbing ultraviolet light from solar irradiance on the skin that would otherwise penetrate living tissue and cause cell damage leading to, among other things, cancer, erythema, and accelerated aging. They may also be useful for protecting body parts from UV damage. Thus, these compounds may be used to prevent cancer, erythema, and / or accelerated aging.

[0010] The compounds may also be used in the photoprotection of hair, food, plants, and in the manufacture of photoprotective materials such as plastics for food packaging. They may also be useful in food packaging to protect foodstuffs from damaging ultraviolet and / or high-energy visible radiation.

[0011] They can absorb ultraviolet and / or high-energy visible light and can be used to prevent photodegradation of ingredients, such as pharmaceutical and cosmetic ingredients. They can also be used to prevent coloration due to absorption of high-energy visible light.

[0012] In some embodiments, the compounds have the additional advantage of being biodegradable. They also have high extinction coefficients, high photostability, low fluorescence, and low singlet oxygen yield. They also have the advantage of being unlikely to be readily absorbed through the skin.

[0013] In some embodiments, the compounds of the present invention can function as antioxidants and can also effectively prevent damage from hydroxyl radicals that can form from pollution and ultraviolet radiation.

[0014] The present invention therefore also relates to the use of at least one compound according to the invention as an ultraviolet absorbing filter and / or a high-energy visible light filter.

[0015] The present invention also relates to the use of at least one compound according to the invention for protection against ultraviolet and / or high-energy visible radiation.

[0016] The compounds may be used for photoprotection of pharmaceutical and cosmetic formulations, including cosmetic skin formulations.

[0017] The present invention also relates to the use of at least one compound according to the invention as a light stabilizer for protecting ingredients against photodegradation.

[0018] The present invention also relates to the use of at least one compound according to the invention as an ultraviolet and / or high-energy visible light absorbing filter in a consumer product or in packaging.

[0019] The present invention also encompasses consumer products comprising at least one compound according to the invention.

[0020] The present invention also includes packaging materials comprising at least one compound according to the present invention.

[0021] These and other characteristics, features and advantages of the present invention will become apparent from the following detailed description, which illustrates, by way of example, the principles of the invention. [Brief explanation of the drawings]

[0022] [Figure 1] 1 is a line graph showing the absorbance spectrum of Compound 1, which exhibits an absorbance maximum of 410 nm and is useful for providing high-energy visible light protection. [Figure 2] 1 is a line graph showing the absorbance spectrum of Compound 2, which shows strong absorbance in the UVB region. [Figure 3] 1 is a line graph showing the combined absorbance spectrum of compounds 1 and 2. The absorbance spectra of both compounds can be combined to provide broad spectrum UVB and UVA protection. [Figure 4]1 is a line graph showing the absorbance spectrum of Compound 4. [Figure 5] 1 is a line graph showing the absorbance spectrum of Compound 5. [Figure 6] 1 is a line graph showing the hydroxyl radical antioxidant capacity (HORAC) test of compound 4. [Figure 7] 1 is a line graph showing the absorbance spectrum of Compound 42. [Figure 8] 1 is a line graph showing the absorbance spectrum of Compound 43. [Figure 9] 1 is a line graph showing the absorbance spectrum of compound 44. [Figure 10] 1 is a line graph showing the absorbance spectrum of compound 45. [Figure 11] 1 is a line graph showing the absorbance spectrum of compound 46. [Figure 12] 1 is a line graph showing the absorbance spectrum of Compound 6. [Figure 13] 1 is a line graph showing the absorbance spectrum of compound 47. [Figure 14] 1 is a line graph showing the absorbance spectrum of compound 48. [Figure 15] 1 is a line graph showing the absorbance spectrum of Compound 49. [Figure 16] 1 is a line graph showing the absorbance spectrum of Compound 50. [Figure 17] 1 is a photograph showing the protective effect of Compound 42 against UV-induced skin damage. DETAILED DESCRIPTION OF THE INVENTION

[0023] When describing the present invention, the terms used should be construed in accordance with the following definitions, unless the context dictates otherwise.

[0024] Unless otherwise defined, all terms used in disclosing the present invention, including technical and scientific terms, have the meanings commonly understood by those skilled in the art to which the present invention belongs. For further guidance, definitions of terms used in the description are included to better understand the teachings of the present invention. When describing the compounds, processes, methods and uses of the present invention, the terms used should be construed in accordance with the following definitions, unless the context dictates otherwise.

[0025] As used herein, the singular forms "a," "an," and "the" include both singular and plural referents unless the context clearly dictates otherwise. For example, "a compound" means one compound or more than one compound.

[0026] In the following paragraphs, different aspects of the invention are defined in more detail. Each aspect so defined can be combined with any other aspect or aspects, unless expressly indicated to the contrary. In particular, any feature indicated as being preferred or advantageous may be combined with any other feature or features indicated as being preferred or advantageous.

[0027] As used herein, the terms "comprising," "comprises," and "comprised of" are synonymous with "including," "includes," or "containing," and "contains," and are inclusive or open-ended and do not exclude additional, unrecited elements, components, or method steps. The terms "comprising," "comprises," and "comprised of" include the term "consisting of."

[0028] The recitation of numerical ranges by endpoints includes all integers and, where appropriate, fractions subsumed within that range (e.g., 1 to 5, when referring to, for example, several elements, can include 1, 2, 3, 4, and, when referring to, for example, measurements, can include 1.5, 2, 2.75, and 3.80). The recitation of endpoints also includes the endpoint values ​​themselves (e.g., 1.0 to 5.0 includes both 1.0 and 5.0). Any numerical ranges recited herein are intended to include all sub-ranges subsumed therein.

[0029] The term "about" is used herein to mean approximately, roughly, around, or within a range thereof. When the term "about" is used in conjunction with a numerical range, it modifies that range by extending the boundaries above and below the stated numerical values. In general, the term "about" is used herein to modify a numerical value above or below the stated value by a variance of 10 percent, above or below (higher or lower).

[0030] The term "and / or," as used herein, should be understood as a specific disclosure of each of two particular features or components with or without the other. Thus, the term "and / or" used in phrases such as "A and / or B" herein is intended to include A and B, A or B, A (alone), and B (alone). Similarly, the term "and / or" used in phrases such as "A, B, and / or C" is intended to encompass each of the following aspects: A, B, and C; A, B, or C; A or C; A or B; B or C; A and C; A and B; B and C; A (alone); B (alone); and C (alone).

[0031] References throughout this specification to "one embodiment" or "an embodiment" mean that a particular feature, structure, or characteristic described in connection with that embodiment is included in at least one embodiment of the present invention. Thus, the appearances of the phrase "in one embodiment" or "in an embodiment" in various places throughout this specification do not necessarily all refer to the same embodiment, although they may. Furthermore, particular features, structures, or characteristics may be combined in any suitable manner in one or more embodiments, as would be apparent to one of ordinary skill in the art from this disclosure. Furthermore, some embodiments described herein may include some features but not other features included in other embodiments, and combinations of features from different embodiments are intended to be within the scope of the present invention and form different embodiments, as would be understood by one of ordinary skill in the art. For example, in the following claims and description, any of the embodiments may be used in any combination.

[0032] Whenever the term "substituted" is used herein, it is meant to indicate that one or more hydrogen atoms on the atom designated by the expression "substituted" are replaced by a selection from the designated group, provided that the normal valence of the designated atom is not exceeded and that the substitution results in a chemically stable compound, i.e., a compound that is sufficiently robust to survive isolation from a reaction mixture.

[0033] The term "halo" or "halogen" as a group or part of a group is generic to fluoro, chloro, bromo, iodo.

[0034] As used herein, the term "hydroxyl" or "hydroxy" refers to the group --OH.

[0035] As used herein, the term "thio" or "thiol" refers to the group --SH.

[0036] The term “alkyl” refers to a group or part of a group of the formula C n H 2n+1where n is a number greater than or equal to 1 and there are no sites of unsaturation. The alkyl groups can be linear or branched and can be substituted as indicated herein. Generally, alkyl groups of the present invention contain 1 to 20 carbon atoms, preferably 1 to 10 carbon atoms, more preferably 1 to 6 carbon atoms, and more preferably 1 to 4 carbon atoms. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms the named group may contain. For example, "C 1-20 The term "alkyl" refers to a group or part of a group of the formula C n H 2n+1 where n is a number ranging from 1 to 20. Thus, for example, "C 1-6 "Alkyl" includes all straight or branched chain alkyl groups having 1 to 6 carbon atoms, and thus includes methyl, ethyl, n-propyl, i-propyl, butyl and its isomers (e.g., n-butyl, i-butyl, and t-butyl), pentyl and its isomers, hexyl and its isomers. For example, C 1-4 Alkyl includes all straight or branched chain alkyl groups having 1 to 4 carbon atoms, and thus includes, for example, methyl, ethyl, n-propyl, i-propyl, 2-methyl-ethyl, butyl, and its isomers (e.g., n-butyl, i-butyl, and t-butyl). In certain embodiments, the term alkyl includes C 1-12 Alkyl (C 1-12 hydrocarbons), and more specifically C 1-9 Alkyl (C 1-9 and more particularly refers to C hydrocarbons as further defined herein above. 1-6 Alkyl (C 1-6 Non-limiting examples of alkyl include methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl ( i-Bu), 2-butyl (s-Bu), 2-dimethyl-2-propyl (t-Bu), 1-pentyl (n-pentyl), 2-pentyl, 3-pentyl, 2-methyl-2-butyl, 3-methyl-2-butyl, 3-methyl-1-butyl, 2-methyl-1-butyl, 1-hexyl, 2-hexyl, 3-hexyl, 2-methyl-2-pentyl, 3-methyl-2-pentyl, 4-methyl-2-pentyl , 3-methyl-3-pentyl, 2-methyl-3-pentyl, 2,3-dimethyl-2-butyl, 3,3-dimethyl-2-butyl, n-heptyl, n-octyl, n-nonyl, n-decyl, n-undecyl, n-dodecyl, n-tridecyl, n-tetradecyl, n-pentadecyl, n-hexadecyl, n-heptadecyl, n-octadecyl, n-nonadecyl, and n-icosyl.

[0037] When the suffix "ene" is used in conjunction with an alkyl group, i.e., "alkylene," this is intended to mean an alkyl group, as defined herein, having two single bonds as points of attachment to other groups. As used herein, the term "alkylene," also referred to as "alkanediyl," by itself or as part of another substituent, refers to an alkyl group that is divalent, i.e., has two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkane, i.e., has two single bonds for attachment to two other groups. Alkylene groups can be linear or branched and can be substituted as indicated herein. Non-limiting examples of alkylene groups include methylene (-CH2-), ethylene (-CH2-CH2-), methylmethylene (-CH(CH3)-), 1-methyl-ethylene (-CH(CH3)-CH2-), n-propylene (-CH2-CH2-CH2-), 2-methylpropylene (-CH2-CH(CH3)-CH2-), 3-methylpropylene (-CH2-CH2-CH(CH3)-), n-butylene (-CH2-CH2-CH2-CH2-), 2-methylbutylene (-CH2-CH(CH3)-CH2-CH2-), 4-methylbutylene (-CH2-CH2-CH2-CH(CH3)-), pentylene and chain isomers, and hexylene and chain isomers.

[0038] The term "hydrocarbyl" group is used herein in accordance with the definition provided by IUPAC as follows: a monovalent group formed by removing a hydrogen atom from a hydrocarbon (i.e., a group containing only carbon and hydrogen).

[0039] The term "alkenyl" as a group or part of a group means an alkyl group having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., at least one sp 2 Carbon-sp 2 "Alkenyl" refers to an unsaturated hydrocarbyl group, which may be linear or branched, containing one or more carbon-carbon double bonds. Generally, alkenyl groups of this invention contain 2 to 20 carbon atoms, preferably 2 to 10 carbon atoms, preferably 2 to 8 carbon atoms, and more preferably 2 to 6 carbon atoms. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms that the named group may contain. 2-6 Examples of alkenyl groups are ethenyl, 2-propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and its isomers, 2-hexenyl and its isomers, 2,4-pentadienyl, etc. The double bond may be in the cis or trans configuration.

[0040] When the suffix "ene" is used in conjunction with an alkenyl group, i.e., "alkenylene," this is intended to mean an alkenyl group, as defined herein, having two single bonds as points of attachment to other groups. As used herein, the term "alkenylene," by itself or as part of another substituent, refers to an alkenyl group that is divalent, i.e., has two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkane, i.e., has two single bonds for attachment to two other groups. Alkenylene groups can be linear or branched and can be substituted as set forth herein. Non-limiting examples of alkenylene groups include -CH=CH-, -C(CH3)=CH-, -C(CH3)=C(CH3)-, -CH=CH-CH2-, -CH2-C(CH3)=CH-, -CH2-CH=C(CH3)-, -CH2-CH2-CH=CH-, and the like.

[0041] The term "alkynyl" as a group or part of a group means an alkynyl group having at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., sp 1 Carbon-sp 1 It refers to a branched or straight chain hydrocarbon containing a carbon-carbon triple bond. In certain embodiments, the term alkynyl refers to a C 2-12 Alkynyl (C 2-12 hydrocarbons), preferably C 2-9 Alkynyl (C 2-9 hydrocarbon), and even more preferably at least one unsaturated site (usually 1 to 3, preferably 1), i.e., at least one sp 1 Carbon-sp 1 C as further defined herein above, having a carbon-carbon triple bond 2-6 Alkynyl (C 2-6 Examples of alkynyl include, but are not limited to, ethynyl (—C≡CH), 3-ethyl-cyclohept-1-ynylene, and 1-propynyl (propargyl, —CHC≡CH).

[0042] When the suffix "ene" is used in conjunction with an alkynyl group, i.e., "alkynylene," this is intended to mean an alkynyl group, as defined herein, having two single bonds as points of attachment to other groups. As used herein, the term "alkynylene" by itself or as part of another substituent refers to an alkynyl group that is divalent, i.e., having two single bonds for attachment to two other groups. Alkynylene groups can be linear or branched and can be substituted as set forth herein. Non-limiting examples of alkynylene groups include -C≡C-, -CH2-C≡C-, -C≡C-CH2-, -CH2-CH2-C≡C-, and the like.

[0043] The term "cycloalkyl," as a group or part of a group, refers to a cyclic alkyl group having one or more ring structures and being a monovalent saturated hydrocarbyl group containing from 3 to 20 carbon atoms, more preferably from 3 to 10 carbon atoms, more preferably from 3 to 8 carbon atoms, more preferably from 3 to 6 carbon atoms. Cycloalkyl includes all saturated hydrocarbon groups containing one or more rings, including monocyclic, bicyclic, or tricyclic. For example, cycloalkyl includes C 3-10 Monocyclic or C 7-18 Polycyclic saturated hydrocarbons include, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylethylene, methylcyclopropylene, cyclohexyl, cycloheptyl, cyclooctyl, cyclooctylmethylene, norbornyl, fenchyl, trimethyltricycloheptyl, decalinyl, adamantyl, and the like. The additional rings of polycyclic cycloalkyls may be fused, bridged, and / or joined through one or more spiro atoms. When a subscript is used herein following a carbon atom, the subscript refers to the number of carbon atoms the named group may contain. For example, "C 3-10 The term "cycloalkyl" refers to a cyclic alkyl group containing 3 to 10 carbon atoms. For example, "C 3-8 The term "cycloalkyl" refers to a cyclic alkyl group containing 3 to 8 carbon atoms. For example, "C 3-6The term "cycloalkyl" refers to a cyclic alkyl group containing from 3 to 6 carbon atoms. For the avoidance of doubt, a fused system of a cycloalkyl ring with a heterocyclic ring is considered to be heterocyclic, regardless of the ring attached to the core structure. A fused system of a cycloalkyl ring with an aryl ring is considered to be aryl, regardless of the ring attached to the core structure. A fused system of a cycloalkyl ring with a heteroaryl ring is considered to be heteroaryl, regardless of the ring attached to the core structure.

[0044] The term “cycloalkylalkylene” or “cycloalkylene” refers to a group or part of a group of the formula R z R y R refers to the group z is cycloalkyl, and R y is alkylene as defined herein.

[0045] The term "alkoxy" or "alkyloxy" refers to a group or part of a group of the formula -OR x R refers to the group x is alkyl as defined herein. 1-6 Non-limiting examples of alkoxy include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy, pentyloxy, and hexyloxy.

[0046] The term "alkenyloxy" refers to a group or part of a group having the formula -OR w R refers to the group w is alkenyl as defined herein.

[0047] The term "alkynyloxy" as a group or part of a group has the formula -OR v R refers to the group v is alkynyl as defined herein.

[0048] The term "aryl," as a group or part of a group, refers to a polyunsaturated aromatic hydrocarbyl group having a single ring (i.e., phenyl) or multiple aromatic rings fused together (e.g., naphthyl) or covalently linked, typically containing 6 to 20 atoms, preferably 6 to 10 atoms, in which at least one ring is aromatic. Typical aryl groups include, but are not limited to, one ring, or two or three rings fused together, such as those derived from benzene, naphthalene, anthracene, biphenyl, etc. The aromatic ring may optionally contain one to two additional rings. A fused system of an aryl ring with a cycloalkyl, cycloalkenyl, or cycloalkynyl ring is considered aryl, regardless of the ring attached to the core structure. A fused system of an aryl ring with a heterocyclic ring is considered heterocyclic, regardless of the ring attached to the core structure. A fused system of an aryl ring with a heteroaryl is considered heteroaryl, regardless of the ring attached to the core structure. Examples of suitable aryls include C 6-20 Aryl, preferably C 6-10 Aryl, more preferably C 6-9 Non-limiting examples of aryl include phenyl, biphenylyl, biphenylenyl, or 1- or 2-naphthalenyl; 1-, 2-, 3-, 4-, 5-, or 6-tetralinyl (also known as "1,2,3,4-tetrahydronaphthalene"); 1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-azulenyl, 4-, 5-, 6-, or 7-indenyl; 4- or 5-indanyl; 5-, 6-, 7-, or 8-tetrahydronaphthyl; 1,2,3,4-tetrahydronaphthyl; and 1,4-dihydronaphthyl; and 1-, 2-, 3-, 4-, or 5-pyrenyl.

[0049] The term "aryl-alkylene," as a group or part of a group, refers to alkyl, as defined herein, wherein at least one hydrogen atom is replaced by at least one aryl, as defined herein. Non-limiting examples of aryl-alkylene groups include benzyl, phenethyl, dibenzylmethyl, benzyl, 2-phenylethan-1-yl, 2-phenylethan-1-yl, naphthylmethyl, 2-naphthylethyl, and the like. 6-10 Aryl-C 1-6 The term "alkylene" means that the alkylene portion of the aryl-alkylene group can contain 1 to 6 carbon atoms and the aryl portion is 6 to 10 carbon atoms.

[0050] The term "aryl-alkenylene," as a group or part of a group, refers to an alkenylene in which one of the hydrogen atoms bonded to a carbon atom is replaced with an aryl. 6-10 Aryl C 2-6 The term "alkenylene" means that the alkenylene portion of the arylalkenyl group can contain 2 to 6 carbon atoms and the aryl portion can contain 6 to 10 carbon atoms.

[0051] The term "aryl-alkynylene," as a group or part of a group, refers to an alkynylene in which one of the hydrogen atoms bonded to a carbon atom is replaced with an aryl. 6-10 Aryl C 2-6 The term "alkynylene" means that the alkenylene portion of the arylalkynyl group can contain 2 to 6 carbon atoms and the aryl portion can contain 6 to 10 carbon atoms.

[0052] The term "haloalkyl," as a group or part of a group, refers to an alkyl group having the meaning defined herein, wherein one or more hydrogen atoms are each replaced with a halogen, as defined herein. Non-limiting examples of such haloalkyl groups include chloromethyl, 1-bromoethyl, fluoromethyl, difluoromethyl, trifluoromethyl, 1,1,1-trifluoroethyl, and the like.

[0053] As used herein, the term "glycosyl" refers to a chemical group derived by replacing a hydroxyl group from a hemiacetal function of a monosaccharide, disaccharide, trisaccharide, oligosaccharide, or polysaccharide. A glycosyl moiety having two or more monosaccharides can represent a linear or branched structure.

[0054] As used herein, the term "monosaccharide" refers to a simple form of sugar consisting of a single sugar unit that cannot be further broken down into smaller sugar building blocks or moieties. Common examples of monosaccharides include glucose (dextrose), fructose, galactose, mannose, and ribose. Monosaccharides can be linear or cyclic (i.e., they can be called furanoses, pyranoses). Monosaccharides can be classified according to the number of carbon atoms in the carbohydrate, i.e., trioses with three carbon atoms, such as glyceraldehyde and dihydroxyacetone; tetraoses with four carbon atoms, such as erythrose, trace, and erythrulose; pentoses with five carbon atoms, such as arabinose, lyxose, ribose, xylose, ribulose, and xylulose; hexoses with six carbon atoms, such as allose, altrose, galactose, glucose, gulose, idose, mannose, talose, fructose, cyclose, sorbose, and tagatose; heptoses with seven carbon atoms, such as mannoheptulose and sedoheptulose; octooses with eight carbon atoms, such as 2-keto-3-deoxy-manno-octonate; nonoses with nine carbon atoms, such as sialose; and decoses with ten carbon atoms. The above monosaccharides include both D- and L-monosaccharides.

[0055] Alternatively, the monosaccharide may be a monosaccharide derivative, in which the sugar unit contains one or more substituents other than hydroxyl. Such derivatives may be, but are not limited to, ethers, esters, amides, acids, phosphates, and amines. Examples of amine derivatives include glucosamine, galactosamine, fructosamine, and mannosamine. Examples of amide derivatives include N-acetylated amine derivatives of sugars (e.g., N-acetylglucosamine, N-acetylgalactosamine).

[0056] As used herein, the term "disaccharide" refers to a molecular moiety containing two monosaccharides covalently linked to each other. Disaccharides include maltose (glucose-glucose), lactose (galactose-glucose), and sucrose (fructose-glucose).

[0057] As used herein, the term "trisaccharide" refers to a molecular moiety containing three monosaccharides covalently linked to each other.

[0058] As used herein, the term "oligosaccharide" refers to a molecular moiety containing at least four monosaccharides covalently linked to one another. Oligosaccharides include tetrasaccharides, pentasaccharides, hexasaccharides, heptasaccharides, octasaccharides, and the like. The covalent bond linking the sugars generally consists of a glycosidic bond (i.e., a COC bond) formed between the hydroxyl groups of adjacent sugars. The linkage can occur between a 1-carbon (anomeric carbon) and a 4-carbon adjacent sugar (i.e., a 1-4 bond), a 1-carbon (anomeric carbon) and a 3-carbon adjacent sugar (i.e., a 1-3 bond), a 1-carbon (anomeric carbon) and a 6-carbon adjacent sugar (i.e., a 1-6 bond), or a 1-carbon (anomeric carbon) and a 2-carbon adjacent sugar (i.e., a 1-2 bond). Sugars can be linked within an oligosaccharide so that the anomeric carbon is in the a or β configuration. Oligosaccharides prepared according to the methods of the present invention can also contain linkages between carbon atoms other than 1-, 2-, 3-, 4-, and 6-carbons.

[0059] As used herein, the term "polysaccharide" refers to a molecular moiety containing at least nine monosaccharides covalently linked to one another. Polysaccharides include starch, hyaluronic acid, amylose, amylopectin, dextran, cyclodextrin, cellulose, agar, chitin, gum arabic, and glycogen.

[0060] Those skilled in the art will understand that the term "O-glycosyl moiety" refers to a glycosyl moiety that is attached to another molecular moiety via an O-glycosidic bond. Similarly, an "S-glycosyl moiety" refers to a glycosyl moiety that is attached to another molecular moiety via an S-glycosidic bond, an "N-glycosyl moiety" refers to a glycosyl moiety that is attached to another molecular moiety via an N-glycosidic bond, and a "C-glycosyl moiety" refers to a glycosyl moiety that is attached to another molecular moiety via a C-glycosidic bond.

[0061] In some embodiments, preferred glycosyls can be selected from the group including glucosyl, allosyl, altrosyl, galactosyl, gulosyl, idosyl, mannosyl, talosyl, fructosyl, psicosyl, sorbosyl, tagatosyl, sucrosyl, maltosyl, lactosyl, cellobiosyl, mannotriosyl, raffinosyl, melezitosyl, amylopectinyl, Syalyl Lewis X (SiaLex), preferably glucosyl.

[0062] The term "carbonyl," as a group or part of a group, refers to the group --C(.dbd.O)--, also written --CO--.

[0063] The term "alkylcarbonyl" as a group or part of a group has the formula -C(=O)R x where R x is alkyl as defined herein.

[0064] As used herein, the term "heterocyclyl" refers to a non-aromatic, fully saturated, or partially unsaturated ring system containing 3 to 18 atoms, preferably 3 to 14 atoms (3-14-membered heterocyclyl), including at least one N, O, S, or P, e.g., a 3- to 7-membered monocyclic ring, a 7- to 14-membered bicyclic ring, preferably a total of 3 to 10 ring atoms (3- to 10-membered heterocyclyl), more preferably 3 to 8 atoms (4- to 6-membered heterocyclyl), and even more preferably 3 to 5 atoms (3- to 5-membered heterocyclyl). The heterocycle or each ring of the heterocyclyl can have 1, 2, 3, or 4 heteroatoms selected from N, O, P, and / or S; the N and S heteroatoms can optionally be oxidized; the N heteroatom can optionally be quaternized; and at least one carbon atom of the heterocyclyl can be oxidized to form at least one C=O. A heterocyclyl may be attached to any heteroatom or carbon atom of the ring or ring system, valence permitting. The rings of a polycyclic heterocyclyl or heterocycle may be fused, bridged, and / or joined through one or more spiro atoms. A heterocycle or heterocyclyl fused system with an aryl ring is considered a heterocycle or heterocyclyl, regardless of the ring attached to the core structure. A heterocycle or heterocyclyl fused system with a heteroaryl ring is considered a heteroaryl, regardless of the ring attached to the core structure.

[0065] Non-limiting exemplary heterocycles or heterocyclic groups include piperidinyl, piperazinyl, homopiperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, aziridinyl, oxiranyl, thiiranyl, azetidinyl, oxetanyl, thietanyl, imidazolinyl, pyrazolidinyl, imidazolidinyl, oxazolinyl, isoxazolinyl, oxazolidinyl, isoxazolidinyl, thiazolidinyl, isothiazolidinyl, succinimidyl, indolinyl, isoindolinyl, chromanyl (3, (also known as 4-dihydrobenzo[b]pyranyl), 2H-pyrrolyl, pyrrolinyl (1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl, etc.), 4H-quinolidinyl, 2-oxopiperazinyl, pyrazolinyl (2-pyrazolinyl, 3-pyrazolinyl, etc.), tetrahydro-2H-pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxolanyl, 1,4-dioxanyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolodinyl, indolinyl, tetrahydro Thiophenyl, tetrahydroquinolinyl, tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, thiomorpholin-4-yl, thiomorpholin-4-yl sulfoxide, thiomorpholin-4-yl sulfone, 1,3-dioxolanyl, 1,4-oxathianyl, 1,4-dithianyl, 1,3,5-trioxanyl, 1H-pyrrolidinyl, tetrahydro-1,1-dioxothiophenyl, N-formyl-piperazinyl, thio Morpholinyl, dihydrofuranyl, dihydrothienyl, tetrahydrothienyl, dihydropyrazolyl, dihydroimidazolyl, isothiazolinyl, thiazolinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolinyl, thiadiazolidinyl, tetrazolinyl, tetrazolidinyl, dihydro-pyridinyl, tetrahydro-pyridinyl, 1,2,3,6-tetrahydropyridinyl, hexahydro-pyridinyl, dihydro-pyrimidinyl, tetrahydro-pyrimidinyl, 1,4,5,6-Tetrahydropyrimidinyl, dihydro-pyrazinyl, tetrahydro-pyrazinyl, dihydro-pyridazinyl, tetrahydro-pyridazinyl, dihydro-triazinyl, tetrahydro-triazinyl, hexahydro-triazinyl, 1,4-diazepanyl, dihydro-indolyl, indolinyl, tetrahydro-indolyl, dihydro-indazolyl, tetrahydro-indazolyl, dihydro-isoindolyl, dihydro-benzofuranyl, tetrahydro-benzofuranyl, dihydro-benzothienyl, tetrahydro-benzothienyl, dihydro-benzyl benzimidazolyl, tetrahydro-benzimidazolyl, dihydro-benzoxazolyl, 2,3-dihydrobenzo[d]oxazolyl, tetrahydro-benzoxazolyl, dihydro-benzoxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, tetrahydro-benzoxazinyl, benzo[1,3]dioxolyl, benzo[1,4]dioxanyl, dihydro-purinyl, tetrahydro-purinyl, dihydro-quinolinyl, 1,2,3,4-tetrahydroquinolinyl, dihydro-isoquinolinyl, 3,4-dihydroisoquinolinyl quinolin-(1H)-yl, tetrahydro-isoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, dihydro-quinazolinyl, tetrahydro-quinazolinyl, dihydro-quinoxalinyl, tetrahydro-quinoxalinyl, 1,2,3,4-tetrahydroquinoxalinyl, 2,5-dihydro-1H-pyrrolyl, 4,5-dihydro-1H-imidazolyl, hexahydropyrrolo[3,4-b][1,4]oxazin-(2H)-yl, 3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazinyl, (cis)-octahydrocyclopenta[ c]pyrrolyl, hexahydropyrrolo[3,4-b]pyrrol-(1H)-yl, 5H-pyrrolo[3,4-b]pyridin-(7H)-yl, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridinyl, tetrahydro-1H-pyrrolo[3,4-b]pyridin-(2H,7H,7aH)-yl, hexahydro-1H-pyrrolo[3,4-b]pyridin-(2H)-yl, (octahydro-6H-pyrrolo[3,4-b]pyridinyl, hexahydropyrrolo[1,2-a]pyrazin-(1H)-yl, 3,4,6,7,8,8a-hexahydro-1H-pyrrolo[1,2-a]pyrazinyl, 2,3,4,9-tetrahydro-1H-carbazolyl, 1,2,3,4-tetrahydropyrazino[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, 1,3-dihydro-2H-isoindolyl, octahydro-2H-isoindolyl, 2,5-diazabicyclo[2.2.1]heptanyl, 2-azabicyclo[2.2.1]heptenyl, 3-azabicyclo[3.1.0]hexanyl, 3,6-diazabicyclo[3.1.0]hexanyl, 5-azaspiro[2.4]heptanyl, 4,7-diazaspiro[2.5] Octanyl, 2,6-diazaspiro[3.3]heptanyl, 2,5-diazaspiro[3.4]octanyl, 2,6-diazaspiro[3.4]octanyl, 2,7-diazaspiro[3.5]nonanyl, 2,7-diazaspiro[4.4]nonanyl, 2-azaspiro[4.5]decanyl, 2,8-diazaspiro[4.5]decanyl, 3,6-diazabicyclo[3.2.1]octyl, 1,4-dihydroindeno[1,2-c]pyrazolyl, dihydropyranyl, dihydropyridinyl, dihydroquinolinyl, 8H-indeno[1,2-d]thiazolyl, tetrahydroimidazo[1,2-a]pyridinyl, pyridin-2(1H)-one, 8-azabicyclo[3.2.1]oct-2-enyl. As used herein, the term "aziridinyl" includes aziridin-1-yl and aziridin-2-yl. As used herein, the term "oxiranyl" includes oxiranyl-2-yl. As used herein, the term "thiiranyl" includes thiiran-2-yl. As used herein, the term "azetidinyl" includes azetidin-1-yl, azetidin-2-yl, and azetidin-3-yl. As used herein, the term "oxetanyl" includes oxetan-2-yl and oxetan-3-yl. As used herein, the term "thietanyl" includes thietan-2-yl and thietan-3-yl. As used herein, the term "pyrrolidinyl" includes pyrrolidin-1-yl, pyrrolidin-2-yl, and pyrrolidin-3-yl. As used herein, the term "tetrahydrofuranyl" includes tetrahydrofuran-2-yl and tetrahydrofuran-3-yl. As used herein, the term "tetrahydrothiophenyl" includes tetrahydrothiophen-2-yl and tetrahydrothiophen-3-yl. As used herein, the term "succinimidyl" includes succinimide-1-yl and succinimide-3-yl. As used herein, the term "dihydropyrrolyl" includes 2,3-dihydropyrrol-1-yl, 2,3-dihydro-1H-pyrrol-2-yl, 2,3-dihydro-1H-pyrrol-3-yl, 2,5-dihydropyrrol-1-yl, 2,5-dihydro-1H-pyrrol-3-yl, and 2,5-dihydropyrrol-5-yl. As used herein, the term "2H-pyrrolyl" includes 2H-pyrrol-2-yl, 2H-pyrrol-3-yl, 2H-pyrrol-4-yl, and 2H-pyrrol-5-yl. As used herein, the term "3H-pyrrolyl" includes 3H-pyrrol-2-yl, 3H-pyrrol-3-yl, 3H-pyrrol-4-yl, and 3H-pyrrol-5-yl. As used herein, the term "dihydrofuranyl" includes 2,As used herein, the term "dihydrothiophenyl" includes 3-dihydrofuran-2-yl, 2,3-dihydrofuran-3-yl, 2,3-dihydrofuran-4-yl, 2,3-dihydrofuran-5-yl, 2,5-dihydrofuran-2-yl, 2,5-dihydrofuran-3-yl, 2,5-dihydrofuran-4-yl, and 2,5-dihydrofuran-5-yl. As used herein, the term "dihydrothiophenyl" includes 2,3-dihydrothiophen-2-yl, 2,3-dihydrothiophen-3-yl, 2,3-dihydrothiophen-4-yl, 2,3-dihydrothiophen-5-yl, 2,5-dihydrothiophen-2-yl, 2,5-dihydrothiophen-3-yl, 2,5-dihydrothiophen-4-yl, and 2,5-dihydrothiophen-5-yl. As used herein, the term "imidazolidinyl" includes imidazolidin-1-yl, imidazolidin-2-yl, and imidazolidin-4-yl. As used herein, the term "pyrazolidinyl" includes pyrazolidin-1-yl, pyrazolidin-3-yl, and pyrazolidin-4-yl. As used herein, the term "imidazolinyl" includes imidazolin-1-yl, imidazolin-2-yl, imidazolin-4-yl, and imidazolin-5-yl. As used herein, the term "pyrazolinyl" includes 1-pyrazolin-3-yl, 1-pyrazolin-4-yl, 2-pyrazolin-1-yl, 2-pyrazolin-3-yl, 2-pyrazolin-4-yl, 2-pyrazolin-5-yl, 3-pyrazolin-1-yl, 3-pyrazolin-2-yl, 3-pyrazolin-3-yl, 3-pyrazolin-4-yl, and 3-pyrazolin-5-yl. As used herein, the term "dioxolanyl," also known as "1,3-dioxolanyl," includes dioxolan-2-yl, dioxolan-4-yl, and dioxolan-5-yl. As used herein, "1,3-dioxolanyl" includes dioxolan-2-yl, dioxolan-4-yl, and dioxolan-5-yl.The term "dioxolyl," also known as "3-dioxolyl," includes dioxol-2-yl, dioxol-4-yl, and dioxol-5-yl. As used herein, the term "oxazolidinyl" includes oxazolidin-2-yl, oxazolidin-3-yl, oxazolidin-4-yl, and oxazolidin-5-yl. As used herein, the term "isoxazolidinyl" includes isoxazolidin-2-yl, isoxazolidin-3-yl, isoxazolidin-4-yl, and isoxazolidin-5-yl. As used herein, the term "oxazolinyl" includes 2-oxazolinyl-2-yl, 2-oxazolinyl-4-yl, 2-oxazolinyl-5-yl, 3-oxazolinyl-2-yl, 3-oxazolinyl-4-yl, 3-oxazolinyl-5-yl, 4-oxazolinyl-2-yl, 4-oxazolinyl-3-yl, 4-oxazolinyl-4-yl, and 4-oxazolinyl-5-yl. As used herein, the term "isoxazolinyl" includes 2-isoxazolinyl-3-yl, 2-isoxazolinyl-4-yl, 2-isoxazolinyl-5-yl, 3-isoxazolinyl-3-yl, 3-isoxazolinyl-4-yl, 3-isoxazolinyl-5-yl, 4-isoxazolinyl-2-yl, 4-isoxazolinyl-3-yl, 4-isoxazolinyl-4-yl, and 4-isoxazolinyl-5-yl. As used herein, the term "thiazolidinyl" includes thiazolidin-2-yl, thiazolidin-3-yl, thiazolidin-4-yl, and thiazolidin-5-yl. As used herein, the term "isothiazolidinyl" includes isothiazolin-2-yl, isothiazolin-3-yl, isothiazolin-4-yl, and isothiazolin-5-yl. As used herein, the term "thiazolinyl" refers to 2-thiazolinyl-2-yl,

[0023] As used herein, the term "isothiazolinyl" includes 2-isothiazolinyl-3-yl, 2-isothiazolinyl-4-yl, 2-thiazolinyl-5-yl, 3-thiazolinyl-2-yl, 3-thiazolinyl-4-yl, 3-thiazolinyl-5-yl, 4-thiazolinyl-2-yl, 4-thiazolinyl-3-yl, 4-thiazolinyl-4-yl, and 4-thiazolinyl-5-yl. As used herein, the term "isothiazolinyl" includes 2-isothiazolinyl-3-yl, 2-isothiazolinyl-4-yl, 2-isothiazolinyl-5-yl, 3-isothiazolinyl-3-yl, 3-isothiazolinyl-4-yl, 3-isothiazolinyl-5-yl, 4-isothiazolinyl-2-yl, 4-isothiazolinyl-3-yl, 4-isothiazolinyl-4-yl, and 4-isothiazolinyl-5-yl. As used herein, the term "piperidyl," also known as "piperidinyl," includes piperid-1-yl, piperid-2-yl, piperid-3-yl, and piperid-4-yl. As used herein, the term "dihydropyridinyl" includes 1,2-dihydropyridin-1-yl, 1,2-dihydropyridin-2-yl, 1,2-dihydropyridin-3-yl, 1,2-dihydropyridin-4-yl, 1,2-dihydropyridin-5-yl, 1,2-dihydropyridin-6-yl, 1,4-dihydropyridin-1-yl, 1,4-dihydropyridin-2-yl, 1,4-dihydropyridin-3-yl, 1,4-dihydropyridin-4-yl, 2,3-dihydropyridin-2-yl, 2,3-dihydropyridin-3-yl, and the like. -yl, 2,3-dihydropyridin-4-yl, 2,3-dihydropyridin-5-yl, 2,3-dihydropyridin-6-yl, 2,5-dihydropyridin-2-yl, 2,5-dihydropyridin-3-yl, 2,5-dihydropyridin-4-yl, 2,5-dihydropyridin-5-yl, 2,5-dihydropyridin-6-yl, 3,4-dihydropyridin-2-yl, 3,4-dihydropyridin-3-yl, 3,4-dihydropyridin-4-yl, 3,4-dihydropyridin-5-yl, and 3,4-dihydropyridin-6-yl.As used herein, the term "tetrahydropyridinyl" includes 1,2,3,4-tetrahydropyridin-1-yl, 1,2,3,4-tetrahydropyridin-2-yl, 1,2,3,4-tetrahydropyridin-3-yl, 1,2,3,4-tetrahydropyridin-4-yl, 1,2,3,4-tetrahydropyridin-5-yl, 1,2,3,4-tetrahydropyridin-6-yl, 1,2,3,6-tetrahydropyridin-1-yl, 1,2,3,6-tetrahydropyridin-2-yl, 1,2,3,6-tetrahydropyridin- Examples of tetrahydropyridin-3-yl include 1,2,3,6-tetrahydropyridin-4-yl, 1,2,3,6-tetrahydropyridin-5-yl, 1,2,3,6-tetrahydropyridin-6-yl, 2,3,4,5-tetrahydropyridin-2-yl, 2,3,4,5-tetrahydropyridin-3-yl, 2,3,4,5-tetrahydropyridin-3-yl, 2,3,4,5-tetrahydropyridin-4-yl, 2,3,4,5-tetrahydropyridin-5-yl, and 2,3,4,5-tetrahydropyridin-6-yl. As used herein, the term "tetrahydropyranyl," also known as "oxanyl" or "tetrahydro-2H-pyranyl," includes tetrahydropyran-2-yl, tetrahydropyran-3-yl, and tetrahydropyran-4-yl. As used herein, the term "2H-pyranyl" includes 2H-pyran-2-yl, 2H-pyran-3-yl, 2H-pyran-4-yl, 2H-pyran-5-yl, and 2H-pyran-6-yl. As used herein, the term "4H-pyranyl" includes 4H-pyran-2-yl, 4H-pyran-3-yl, and 4H-pyran-4-yl. As used herein, the term "3,4-dihydro-2H-pyranyl" includes 3,4-dihydro-2H-pyran-2-yl, 3,4-dihydro-2H-pyran-3-yl, 3,4-dihydro-2H-pyran-4-yl, 3,4-dihydro-2H-pyran-5-yl, and 3,4-dihydro-2H-pyran-6-yl.As used herein, the term "3,6-dihydro-2H-pyranyl" includes 3,6-dihydro-2H-pyran-2-yl, 3,6-dihydro-2H-pyran-3-yl, 3,6-dihydro-2H-pyran-4-yl, 3,6-dihydro-2H-pyran-5-yl, and 3,6-dihydro-2H-pyran-6-yl. As used herein, the term "tetrahydrothiophenyl" includes tetrahydrothiophen-2-yl, tetrahydrothiophenyl-3-yl, and tetrahydrothiophenyl-4-yl. As used herein, the term "2H-thiopyranyl" includes 2H-thiopyran-2-yl, 2H-thiopyran-3-yl, 2H-thiopyran-4-yl, 2H-thiopyran-5-yl, and 2H-thiopyran-6-yl. As used herein, the term "4H-thiopyranyl" includes 4H-thiopyran-2-yl, 4H-thiopyran-3-yl, and 4H-thiopyran-4-yl. As used herein, the term "3,4-dihydro-2H-thiopyranyl" includes 3,4-dihydro-2H-thiopyran-2-yl, 3,4-dihydro-2H-thiopyran-3-yl, 3,4-dihydro-2H-thiopyran-4-yl, 3,4-dihydro-2H-thiopyran-5-yl, and 3,4-dihydro-2H-thiopyran-6-yl. As used herein, the term "3,6-dihydro-2H-thiopyranyl" includes 3,6-dihydro-2H-thiopyran-2-yl, 3,6-dihydro-2H-thiopyran-3-yl, 3,6-dihydro-2H-thiopyran-4-yl, 3,6-dihydro-2H-thiopyran-5-yl, and 3,6-dihydro-2H-thiopyran-6-yl. As used herein, the term "piperazinyl," also known as "piperazidinyl," includes piperazin-1-yl and piperazin-2-yl. As used herein, the term "morpholinyl" includes morpholin-2-yl, morpholin-3-yl, and morpholin-4-yl. As used herein, the term "thiomorpholinyl" includes thiomorpholin-2-yl, thiomorpholin-3-yl, and thiomorpholin-4-yl.As used herein, the term "dioxanyl" includes 1,2-dioxan-3-yl, 1,2-dioxan-4-yl, 1,3-dioxan-2-yl, 1,3-dioxan-4-yl, 1,3-dioxan-5-yl, and 1,4-dioxan-2-yl. As used herein, the term "dithianyl" includes 1,2-dithian-3-yl, 1,2-dithian-4-yl, 1,3-dithian-2-yl, 1,3-dithian-4-yl, 1,3-dithian-5-yl, and 1,4-dithian-2-yl. As used herein, the term "oxathianyl" includes oxathian-2-yl and oxathian-3-yl. As used herein, the term "trioxanyl" includes 1,2,3-trioxan-4-yl, 1,2,3-trioxan-5-yl, 1,2,4-trioxan-3-yl, 1,2,4-trioxan-5-yl, 1,2,4-trioxan-6-yl, and 1,3,4-trioxan-2-yl. As used herein, the term "azepanyl" includes azepan-1-yl, azepan-2-yl, azepan-3-yl, and azepan-4-yl. As used herein, the term "homopiperazinyl" includes homopiperazin-1-yl, homopiperazin-2-yl, homopiperazin-3-yl, and homopiperazin-4-yl. As used herein, the term "indolinyl" includes indolin-1-yl, indolin-2-yl, indolin-3-yl, indolin-4-yl, indolin-5-yl, indolin-6-yl, and indolin-7-yl. As used herein, the term "quinolizinyl" includes quinolizidin-1-yl, quinolizidin-2-yl, quinolizidin-3-yl, and quinolizidin-4-yl. As used herein, the term "isoindolinyl" includes isoindolin-1-yl, isoindolin-2-yl, isoindolin-3-yl, isoindolin-4-yl, isoindolin-5-yl, isoindolin-6-yl, and isoindolin-7-yl.As used herein, the term "3H-indolyl" includes 3H-indol-2-yl, 3H-indol-3-yl, 3H-indol-4-yl, 3H-indol-5-yl, 3H-indol-6-yl, and 3H-indol-7-yl. As used herein, the term "quinolizinyl" includes quinolizidin-1-yl, quinolizidin-2-yl, quinolizidin-3-yl, and quinolizidin-4-yl. As used herein, the term "quinolizinyl" includes quinolizidin-1-yl, quinolizidin-2-yl, quinolizidin-3-yl, and quinolizidin-4-yl. As used herein, the term "tetrahydroquinolinyl" includes tetrahydroquinolin-1-yl, tetrahydroquinolin-2-yl, tetrahydroquinolin-3-yl, tetrahydroquinolin-4-yl, tetrahydroquinolin-5-yl, tetrahydroquinolin-6-yl, tetrahydroquinolin-7-yl, and tetrahydroquinolin-8-yl. As used herein, the term "tetrahydroisoquinolinyl" includes tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolin-4-yl, tetrahydroisoquinolin-5-yl, tetrahydroisoquinolin-6-yl, tetrahydroisoquinolin-7-yl, and tetrahydroisoquinolin-8-yl. As used herein, the term "chromanyl" includes chroman-2-yl, chroman-3-yl, chroman-4-yl, chroman-5-yl, chroman-6-yl, chroman-7-yl, and chroman-8-yl. As used herein, the term "1H-pyrrolidine" includes 1H-pyrrolidin-1-yl, 1H-pyrrolidin-2-yl, 1H-pyrrolidin-3-yl, 1H-pyrrolidin-5-yl, 1H-pyrrolidin-6-yl, and 1H-pyrrolidin-7-yl. As used herein, the term "3H-pyrrolidine" includes 3H-pyrrolidin-1-yl, 3H-pyrrolidin-2-yl, 3H-pyrrolidin-3-yl, 3H-pyrrolidin-5-yl, 3H-pyrrolidin-6-yl, and 3H-pyrrolidin-7-yl.

[0066] The term “heterocyclylalkylene” or “heterocyclyl-alkylene,” as a group or part of a group, refers to an alkylene, as defined herein, in which at least one hydrogen atom is replaced by at least one heterocyclyl, as defined herein, and has the formula R y R r (In the formula, R y is alkylene and R r is heterocyclyl as defined herein). 1-6 The term "alkylene" refers to heterocyclyl-alkylene, where the alkylene portion contains 1 to 6 carbon atoms and the heterocyclyl portion is a non-aromatic, fully saturated, or partially unsaturated ring system of 3 to 10 atoms containing at least one N, O, S, or P.

[0067] The term “heterocyclylalkenylene” or “heterocyclyl-alkenylene,” as a group or part of a group, refers to an alkenylene, as defined herein, in which at least one hydrogen atom is replaced by at least one heterocyclyl, as defined herein, and has the formula R t R r (In the formula, R t is alkenylene, and R r is heterocyclyl as defined herein). 2-6 The term "alkenylene" refers to heterocyclyl-alkenylene, where the alkenylene portion contains 2 to 6 carbon atoms and the heterocyclyl portion is a non-aromatic, fully saturated, or partially unsaturated ring system of 3 to 10 atoms containing at least one N, O, S, or P.

[0068] The term “heterocyclylalkynylene” or “heterocyclyl-alkynylene,” as a group or part of a group, refers to alkynylene, as defined herein, in which at least one hydrogen atom is replaced by at least one heterocyclyl, as defined herein, and has the formula R s R r (In the formula, Rs is alkynylene and R r is heterocyclyl as defined herein). 2-6 The term "alkynylene" refers to heterocyclyl-alkynylene, where the alkynylene portion contains 2 to 6 carbon atoms and the heterocyclyl portion is a non-aromatic, fully saturated, or partially unsaturated ring system of 3 to 10 atoms containing at least one N, O, S, or P.

[0069] The term "heteroaryl" refers to an aromatic ring system containing at least one N, O, S, or P and 5-18 atoms containing one or two rings, which may be fused or covalently bonded together, preferably 5-14 atoms (5-14-membered heteroaryl), and even more preferably 5-10 atoms (5-10-membered heteroaryl), where each ring typically contains 5-6 atoms, at least one of the rings is aromatic, and where the N and S heteroatoms may be optionally oxidized, the N heteroatom may be optionally quaternized, and at least one carbon atom of the heteroaryl may be oxidized to form at least one C=O. Fused systems of heteroaryl rings with cycloalkyl, cycloalkenyl, or cycloalkynyl rings are considered heteroaryls, regardless of the ring attached to the core structure. Fused systems of heteroaryl rings with heterocycles are considered heteroaryls, regardless of the ring attached to the core structure. A fused system of heteroaryl rings with an aryl ring is considered heteroaryl, regardless of the ring attached to the core structure. Non-limiting examples of such heteroaryls include pyridinyl, pyrrolyl, thiophenyl (also called thienyl), furanyl, thiazolyl, isothiazolyl, thiadiazolyl, triazol-2-yl, 1H-pyrazol-5-yl, pyrazolyl, imidazolyl, oxazolyl, isoxazolyl, triazolyl, oxadiazolyl, tetrazolyl, oxatriazolyl, thiatriazolyl, pyrimidinyl, pyrazinyl, pyridazinyl, oxazinyl, dioxinyl, thiazinyl, triazinyl, pyranyl, thiopyranyl, imidazo[2,1-b] [1,3]thiazolyl, thieno[3,2-b]furanyl, thieno[3,2-b]thiophenyl, thieno[2,3-d][1,3]thiazolyl, thieno[2,3-d]imidazolyl, tetrazolo[1,5-a]pyridinyl, indolyl, indolizinyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothiophenyl, isobenzothiophenyl, indazolyl, benzimidazolyl, benzoxazolyl, 1,3-benzoxazolyl, 1,2-benzisoxazolyl, 2,1-benzisoxazolyl, 1,3-benzothiazolyl, 1,2-Benzisothiazolyl, 2,1-benzisothiazolyl, benzotriazolyl, 1,2,3-benzoxadiazolyl, 2,1,3-benzoxadiazolyl, benzo[c][1,2,5]oxadiazolyl, 1,2,3-benzothiadiazolyl, 2,1,3-benzothiadiazolyl, benzo[d]oxazol-2(3H)-one, 2,3-dihydro-benzofuranyl, thienopyridinyl, purinyl, 9H-purinyl, imidazo[1,2-a]pyridinyl, imidazo[1,2-a]pyrazinyl, imidazo[5,1-a]isoquinolinyl, imidazo[1,5-a]pyridinyl, 6-oxo-pyridazin-1(6H)-yl, 2-oxopyridin-1(2H)-yl, 1,3-benzo Examples of suitable quinolinyl groups include zodioxolyl, quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, quinoxalinyl, acridinyl, phthalazinyl, 1,4-dihydroindeno[1,2-c]-1H-pyrazolyl, 2,3-dihydro-1H-inden-1-one, 2,3-dihydro-1H-indenyl, 3,4-dihydroquinolin-2(1H)-one, 5,6-dihydroimidazo[5,1-a]isoquinolinyl, 8H-indeno[1,2-d]thiazolyl, benzo[d]oxazol-2(3H)-one, quinolin-2(1H)-one, quinazolin-4(1H)-one, quinazolin-2,4(1H,3H)-dione, benzo-[d]oxazolyl, and pyrazolo[1,5-a]pyridinyl.

[0070] As used herein, the term "pyrrolyl" (also called azolyl) includes pyrrol-1-yl, pyrrol-2-yl, and pyrrol-3-yl. As used herein, the term "furanyl" (also called "furyl") includes furan-2-yl and furan-3-yl (also called furan-2-yl and furan-3-yl). As used herein, the term "thiophenyl" (also called "thienyl") includes thiophen-2-yl and thiophen-3-yl (also called "thien-2-yl" and "thien-3-yl"). As used herein, the term "pyrazolyl" (also called 1H-pyrazolyl and 1,2-diazolyl) includes pyrazol-1-yl, pyrazol-3-yl, or 1H-pyrazol-5-yl, pyrazol-4-yl, and pyrazol-5-yl. As used herein, the term "imidazolyl" includes imidazol-1-yl, imidazol-2-yl, imidazol-4-yl, and imidazol-5-yl. As used herein, the term "oxazolyl" (also called 1,3-oxazolyl) includes oxazol-2-yl, oxazol-4-yl, and oxazol-5-yl. As used herein, the term "isoxazolyl" (also called 1,2-oxazolyl) includes isoxazol-3-yl, isoxazol-4-yl, and isoxazol-5-yl. As used herein, the term "thiazolyl" (also called 1,3-thiazolyl) includes thiazol-2-yl, thiazol-4-yl, and thiazol-5-yl (also called 2-thiazolyl, 4-thiazolyl, and 5-thiazolyl). As used herein, the term "isothiazolyl" (also called 1,2-thiazolyl) includes isothiazol-3-yl, isothiazol-4-yl, and isothiazol-5-yl.As used herein, the term "triazolyl" includes triazol-2-yl, 1H-triazolyl, and 4H-1,2,4-triazolyl; "1H-triazolyl" includes 1H-1,2,3-triazol-1-yl, 1H-1,2,3-triazol-4-yl, 1H-1,2,3-triazol-5-yl, 1H-1,2,4-triazol-1-yl, 1H-1,2,4-triazol-3-yl, and 1H-1,2,4-triazol-5-yl; "4H-1,2,4-triazolyl" includes 4H-1,2,4-triazol-4-yl and 4H-1,2,4-triazol-3-yl. As used herein, the term "oxadiazolyl" includes 1,2,3-oxadiazol-4-yl, 1,2,3-oxadiazol-5-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 1,2,5-oxadiazol-3-yl, and 1,3,4-oxadiazol-2-yl. As used herein, the term "thiadiazolyl" includes 1,2,3-thiadiazol-4-yl, 1,2,3-thiadiazol-5-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl, 1,2,5-thiadiazol-3-yl (also known as furazan-3-yl), and 1,3,4-thiadiazol-2-yl. As used herein, the term "tetrazolyl" includes 1H-tetrazol-1-yl, 1H-tetrazol-5-yl, 2H-tetrazol-2-yl, and 2H-tetrazol-5-yl. As used herein, the term "oxatriazolyl" includes 1,2,3,4-oxatriazol-5-yl and 1,2,3,5-oxatriazol-4-yl. As used herein, the term "thiatriazolyl" includes 1,2,3,4-thiatriazol-5-yl and 1,2,3,5-thiatriazol-4-yl. As used herein, the term "pyridinyl" (also called "pyridyl") includes pyridin-2-yl, pyridin-3-yl, and pyridin-4-yl (also called 2-pyridyl, 3-pyridyl, and 4-pyridyl).As used herein, the term "pyrimidyl" includes pyrimid-2-yl, pyrimid-4-yl, pyrimid-5-yl, and pyrimid-6-yl. As used herein, the term "pyrazinyl" includes pyrazin-2-yl and pyrazin-3-yl. As used herein, the term "pyridazinyl" includes pyridazin-3-yl and pyridazin-4-yl. As used herein, the term "oxazinyl" (also referred to as "1,4-oxazinyl") includes 1,4-oxazin-4-yl and 1,4-oxazin-5-yl. As used herein, the term "dioxinyl" (also referred to as "1,4-dioxinyl") includes 1,4-dioxin-2-yl and 1,4-dioxin-3-yl. As used herein, the term "thiazinyl" (also referred to as "1,4-thiazinyl") includes 1,4-thiazin-2-yl, 1,4-thiazin-3-yl, 1,4-thiazin-4-yl, 1,4-thiazin-5-yl, and 1,4-thiazin-6-yl. As used herein, the term "triazinyl" includes 1,3,5-triazin-2-yl, 1,2,4-triazin-3-yl, 1,2,4-triazin-5-yl, 1,2,4-triazin-6-yl, 1,2,3-triazin-4-yl, and 1,2,3-triazin-5-yl. As used herein, the term "imidazo[2,1-b][1,3]thiazolyl" includes imidazo[2,1-b][1,3]thiazol-2-yl, imidazo[2,1-b][1,3]thiazol-3-yl, imidazo[2,1-b][1,3]thiazol-5-yl, and imidazo[2,1-b][1,3]thiazol-6-yl. As used herein, the term "thieno[3,2-b]furanyl" includes thieno[3,2-b]furan-2-yl, thieno[3,2-b]furan-3-yl, thieno[3,2-b]furan-4-yl, and thieno[3,2-b]furan-5-yl. As used herein, the term "thieno[3,2-b]thiophenyl" includes thieno[3,2-b]thien-2-yl, thieno[3,2-b]thien-3-yl, thieno[3,2-b]thien-5-yl, and thieno[3,2-b]thien-6-yl.As used herein, the term "thieno[2,3-d][1,3]thiazolyl" includes thieno[2,3-d][1,3]thiazol-2-yl, thieno[2,3-d][1,3]thiazol-5-yl, and thieno[2,3-d][1,3]thiazol-6-yl. As used herein, the term "thieno[2,3-d]imidazolyl" includes thieno[2,3-d]imidazol-2-yl, thieno[2,3-d]imidazol-4-yl, and thieno[2,3-d]imidazol-5-yl. As used herein, the term "tetrazolo[1,5-a]pyridinyl" includes tetrazolo[1,5-a]pyridin-5-yl, tetrazolo[1,5-a]pyridin-6-yl, tetrazolo[1,5-a]pyridin-7-yl, and tetrazolo[1,5-a]pyridin-8-yl. As used herein, the term "indolyl" includes indol-1-yl, indol-2-yl, indol-3-yl, indol-4-yl, indol-5-yl, indol-6-yl, and indol-7-yl. As used herein, the term "indolizinyl" includes indolizin-1-yl, indolizin-2-yl, indolizin-3-yl, indolizin-5-yl, indolizin-6-yl, indolizin-7-yl, and indolizin-8-yl. As used herein, the term "isoindolyl" includes isoindol-1-yl, isoindol-2-yl, isoindol-3-yl, isoindol-4-yl, isoindol-5-yl, isoindol-6-yl, and isoindol-7-yl. As used herein, the term "benzofuranyl" (also called benzo[b]furanyl) includes benzofuran-2-yl, benzofuran-3-yl, benzofuran-4-yl, benzofuran-5-yl, benzofuran-6-yl, and benzofuran-7-yl. As used herein, the term "isobenzofuranyl" (also called benzo[c]furanyl) includes isobenzofuran-1-yl, isobenzofuran-3-yl, isobenzofuran-4-yl, isobenzofuran-5-yl, isobenzofuran-6-yl, and isobenzofuran-7-yl.As used herein, the term "benzothiophenyl" (also known as benzo[b]thienyl) includes 2-benzo[b]thiophenyl, 3-benzo[b]thiophenyl, 4-benzo[b]thiophenyl, 5-benzo[b]thiophenyl, 6-benzo[b]thiophenyl, and -7-benzo[b]thiophenyl (also known as benzothien-2-yl, benzothien-3-yl, benzothien-4-yl, benzothien-5-yl, benzothien-6-yl, and benzothien-7-yl). As used herein, the term "isobenzothiophenyl" (also known as benzo[c]thienyl) includes isobenzothien-1-yl, isobenzothien-3-yl, isobenzothien-4-yl, isobenzothien-5-yl, isobenzothien-6-yl, and isobenzothien-7-yl. As used herein, the term "indazolyl" (also known as 1H-indazolyl or 2-azandyl) includes 1H-indazol-1-yl, 1H-indazol-3-yl, 1H-indazol-4-yl, 1H-indazol-5-yl, 1H-indazol-6-yl, 1H-indazol-7-yl, 2H-indazol-2-yl, 2H-indazol-3-yl, 2H-indazol-4-yl, 2H-indazol-5-yl, 2H-indazol-6-yl, and 2H-indazol-7-yl. As used herein, the term "benzimidazolyl" includes benzimidazol-1-yl, benzimidazol-2-yl, benzimidazol-4-yl, benzimidazol-5-yl, benzimidazol-6-yl, and benzimidazol-7-yl. As used herein, the term "1,3-benzoxazolyl" includes 1,3-benzoxazol-2-yl, 1,3-benzoxazol-4-yl, 1,3-benzoxazol-5-yl, 1,3-benzoxazol-6-yl, and 1,3-benzoxazol-7-yl.As used herein, the term "1,2-benzisoxazolyl" includes 1,2-benzisoxazol-3-yl, 1,2-benzisoxazol-4-yl, 1,2-benzisoxazol-5-yl, 1,2-benzisoxazol-6-yl, and 1,2-benzisoxazol-7-yl. As used herein, the term "2,1-benzisoxazolyl" includes 2,1-benzisoxazol-3-yl, 2,1-benzisoxazol-4-yl, 2,1-benzisoxazol-5-yl, 2,1-benzisoxazol-6-yl, and 2,1-benzisoxazol-7-yl. As used herein, the term "1,3-benzothiazolyl" includes 1,3-benzothiazol-2-yl, 1,3-benzothiazol-4-yl, 1,3-benzothiazol-5-yl, 1,3-benzothiazol-6-yl, and 1,3-benzothiazol-7-yl. As used herein, the term "1,2-benzisothiazolyl" includes 1,2-benzisothiazol-3-yl, 1,2-benzisothiazol-4-yl, 1,2-benzisothiazol-5-yl, 1,3-benzothiazol-6-yl, and 1,3-benzothiazol-7-yl. ,2-benzisothiazol-5-yl, 1,2-benzisothiazol-6-yl, and 1,2-benzisothiazol-7-yl. As used herein, the term "2,1-benzisothiazolyl" includes 2,1-benzisothiazol-3-yl, 2,1-benzisothiazol-4-yl, 2,1-benzisothiazol-5-yl, 2,1-benzisothiazol-6-yl, and 2,1-benzisothiazol-7-yl. As used herein, the term "benzotriazolyl" includes benzotriazol-1-yl, benzotriazol-4-yl, benzotriazol-5-yl, benzotriazol-6-yl, and benzotriazol-7-yl. As used herein, the term "1,2,3-benzoxadiazolyl" includes 1,2,3-benzoxadiazol-4-yl, 1,2,3-benzoxadiazol-5-yl, 1,2,3-benzoxadiazol-6-yl, and 1,2,3-benzoxadiazol-7-yl. As used herein, the term "2,1,3-benzoxadiazolyl" includes 2,1,3-benzoxadiazol-4-yl, 2,1,3-benzoxadiazol-5-yl, 2,1,3-benzoxadiazol-6-yl, and 2,1,3-benzoxadiazol-7-yl. As used herein, the term "1,2,3-benzothiadiazolyl" includes 1,2,3-benzothiadiazol-4-yl, 1,2,3-benzothiadiazol-5-yl, 1,2,3-benzothiadiazol-6-yl, and 1,2,3-benzothiadiazol-7-yl. As used herein, the term "2,1,3-benzothiadiazolyl" includes 2,1,3-benzothiadiazol-4-yl, 2,1,3-benzothiadiazol-5-yl, 2,1,3-benzothiadiazol-6-yl, and 2,1,3-benzothiadiazol-7-yl. As used herein, the term "thienopyridinyl" includes thieno[2,3-b]pyridinyl, thieno[2,3-c]pyridinyl, thieno[3,2-c]pyridinyl, and thieno[3,2-b]pyridinyl. As used herein, the term "purinyl" includes purin-2-yl, purin-6-yl, purin-7-yl, and purin-8-yl.As used herein, the term "imidazo[1,2-a]pyridinyl" includes imidazo[1,2-a]pyridin-2-yl, imidazo[1,2-a]pyridin-3-yl, imidazo[1,2-a]pyridin-4-yl, imidazo[1,2-a]pyridin-5-yl, imidazo[1,2-a]pyridin-6-yl, and imidazo[1,2-a]pyridin-7-yl. As used herein, the term "1,3-benzodioxolyl" includes 1,3-benzodioxol-4-yl, 1,3-benzodioxol-5-yl, 1,3-benzodioxol-6-yl, and 1,3-benzodioxol-7-yl. As used herein, the term "quinolinyl" includes quinolin-2-yl, quinolin-3-yl, quinolin-4-yl, quinolin-5-yl, quinolin-6-yl, quinolin-7-yl, and quinolin-8-yl. As used herein, the term "isoquinolinyl" includes isoquinolin-1-yl, isoquinolin-3-yl, isoquinolin-4-yl, isoquinolin-5-yl, isoquinolin-6-yl, isoquinolin-7-yl, and isoquinolin-8-yl. As used herein, the term "cinnolinyl" includes cinnolin-3-yl, cinnolin-4-yl, cinnolin-5-yl, cinnolin-6-yl, cinnolin-7-yl, and cinnolin-8-yl. As used herein, the term "quinazolinyl" includes quinazolin-2-yl, quinazolin-4-yl, quinazolin-5-yl, quinazolin-6-yl, quinazolin-7-yl, and quinazolin-8-yl. As used herein, the term "quinoxalinyl" includes quinoxalin-2-yl, quinoxalin-5-yl, and quinoxalin-6-yl.

[0071] As used herein, heteroaryl and heterocycle or heterocyclyl include, by way of example and without limitation, those groups described in Paquette, Leo A. "Principles of Modern Heterocyclic Chemistry" (WA Benjamin, New York, 1968), particularly Chapters 1, 3, 4, 6, 7, and 9; "The Chemistry of Heterocyclic Compounds, A series of Monographs" (John Wiley & Sons, New York, 1950 to present), particularly Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, CW, and Scriven, E. "Comprehensive Heterocyclic Chemistry" (Pergamon Press, 1996); and J. Am. Chem. Soc. (1960) 82:5566.

[0072] The term “heteroarylalkylene” or “heteroaryl-alkylene,” as a group or part of a group, refers to an alkylene, as defined herein, in which at least one hydrogen atom is replaced by at least one heteroaryl, as defined herein, and has the formula R y R u (In the formula, R y is alkylene and R u is heteroaryl as defined herein). 1-6 The term "alkylene" refers to heteroaryl-alkylene, where the alkylene portion contains 1 to 6 carbon atoms and the heteroaryl portion is an aromatic ring system containing 5 to 10 atoms, including at least one N, O, S, or P atom.

[0073] The term “heteroarylalkenylene” or “heteroaryl-alkenylene,” as a group or part of a group, refers to an alkenylene, as defined herein, in which at least one hydrogen atom is replaced by at least one heteroaryl, as defined herein, and has the formula R t Ru (In the formula, R t is alkenylene, and R u is heteroaryl as defined herein). 2-6 The term "alkenylene" refers to heteroaryl-alkenyl, where the alkenylene portion contains 2 to 6 carbon atoms and the heteroaryl portion is an aromatic ring system containing 5 to 10 atoms, including at least one N, O, S, or P.

[0074] The term “heteroarylalkynylene” or “heteroaryl-alkynylene,” as a group or part of a group, refers to alkynylene, as defined herein, in which at least one hydrogen atom is replaced by at least one heteroaryl, as defined herein, and has the formula R s R u (In the formula, R s is alkynylene and R u is heteroaryl as defined herein). 2-6 The term "alkynylene" refers to heteroaryl-alkynylene, where the alkynylene portion contains 2 to 6 carbon atoms and the heteroaryl portion is an aromatic ring system containing 5 to 10 atoms, including at least one N, O, S, or P atom.

[0075] Any substituent designation found at more than one site in a compound of the invention is intended to be independently selected.

[0076] Substituents are optionally designated with or without a bond. Regardless of the designation of a bond, if a substituent is multivalent (based on its position in the referenced structure), any and all possible orientations of the substituent are intended.

[0077] Any reference to a "compound according to the invention" or a "compound of formula (I)" also includes isomers, such as stereoisomers and tautomers, salts, including pharmaceutically and / or physiologically acceptable salts, hydrates, solvates, polymorphs, etc. of such compounds, unless expressly stated otherwise.

[0078] As used herein, the term "isomer" refers to all possible isomeric forms, including tautomeric and stereochemical forms, which a compound of the formula herein may possess, but does not include positional isomers. Typically, the structures shown herein illustrate one tautomeric or resonance form of a compound, but the corresponding alternative configurations are also contemplated.

[0079] Depending on their substitution patterns, compounds of the present invention may or may not have one or more optical stereocenters and may or may not exist as different enantiomers or diastereomers. Any such enantiomers, diastereomers, or other optical isomers are encompassed within the scope of the present invention. Unless otherwise specified, the chemical names of compounds refer to mixtures of all possible stereochemically isomeric forms, including all diastereomers and enantiomers of basic molecular structures (since compounds of the formulae herein may have at least one chiral center), as well as stereochemically pure or enriched compounds. More specifically, stereocenters may have either the R- or S-configuration, and bonds may have either the cis- or trans-configuration. The terms R- and S-configuration are used herein in accordance with chemical information retrieval nomenclature. The terms cis and trans are used herein in accordance with chemical information retrieval nomenclature and include reference to the position of substituents on cyclic moieties. The absolute stereochemical configuration of compounds of the formulae described herein can be readily determined by those skilled in the art using well-known methods, such as, for example, X-ray diffraction.

[0080] Separation of stereoisomers is accomplished by standard methods known to those skilled in the art. One enantiomer of a compound can be separated substantially free of its opposite enantiomer by methods such as the formation of diastereomers using optically active resolving agents ("Stereochemistry of Carbon Compounds," (1962) by E.L. Eliel, McGraw Hill, Lochmuller, CH, (1975) J. Chromatogr., 113:(3) 283-302). Separation of isomers in a mixture can be achieved by any suitable method, including (1) the formation of ionic diastereomeric salts with chiral compounds and separation by fractional crystallization or other methods, (2) the formation of diastereomeric compounds with chiral derivatizing agents, separation of the diastereomers, and conversion to pure enantiomers, or (3) enantiomers can be separated directly under chiral conditions. In method (1), diastereomeric salts can be formed by reacting enantiomerically pure chiral bases, such as brucine, quinine, ephedrine, strychnine, and a-methyl-b-phenylethylamine (amphetamine), with asymmetric compounds containing acidic functionalities, such as carboxylic and sulfonic acids. Diastereomeric salts can be induced to separate by fractional crystallization or ion chromatography. For the separation of optical isomers of amino compounds, the addition of chiral carboxylic or sulfonic acids, such as camphorsulfonic acid, tartaric acid, mandelic acid, or lactic acid, can result in the formation of diastereomeric salts. Alternatively, in method (2), the substrate to be resolved can be reacted with one enantiomer of a chiral compound to form a diastereomeric pair (Eliel, E. and Wilen, S. (1994) Stereochemistry of Organic Compounds, John Wiley & Sons, Inc., p. 322). Diastereomeric compounds can be formed by reaction of the asymmetric compound with an enantiomerically pure chiral derivatizing reagent, such as a menthyl derivative, followed by separation and hydrolysis of the diastereomers to give the free enantiomerically enriched compound.A method for determining optical purity involves preparing a chiral ester of the racemic mixture, such as menthyl ester or Mosher ester, a-methoxy-a-(trifluoromethyl)phenylacetate (Jacob III. (1982) J. Org. Chem. 47:4165), and analyzing the NMR spectrum for the presence of two atropisomeric diastereomers. Stable diastereomers can be separated and isolated by normal-phase and reverse-phase chromatography, following methods for the separation of atropisomeric naphthyl-isoquinolines (Hoye, T., WO 96 / 15111). Under method (3), a racemic mixture of two asymmetric enantiomers is separated by chromatography using a chiral stationary phase. Suitable chiral stationary phases are, for example, polysaccharides, particularly cellulose or amylose derivatives. Commercially available polysaccharide chiral stationary phases include ChiralCeI™ CA, OA, OB5, OC5, OD, OF, OG, OJ, and OK, and Chiralpak™ AD, AS, OP(+), and OT(+). Suitable eluents or mobile phases for use in combination with these polysaccharide chiral stationary phases include hexane, modified with alcohols such as ethanol and isopropanol. ("Chiral Liquid Chromatography" (1989) W. J. Lough, Ed. Chapman and Hall, New York, Okamoto, (1990) "Optical resolution of dihydropyridine enantiomers by high-performance liquid chromatography using phenylcarbamates of polysaccharides as a chiral stationary phase", J. of Chromatogr. 513:375-378).

[0081] The term "salt" relates to any salt that the compound can form. They may be cosmetically or pharmaceutically acceptable. Thus, the compounds of the present invention may optionally be used in the form of salts of the compounds herein, in particular, for example, Na + , Li + , K.+ , Ca 2+ , and Mg 2+ These salts include cosmetically or pharmaceutically acceptable non-toxic salts containing the following: Such salts may include those derived from the combination of suitable cations, such as alkali and alkaline earth metal ions, or ammonium and quaternary amino ions, with an acidic anion moiety, typically a carboxylic acid. The compounds of the present invention may bear multiple positive or negative charges. The net charge of the compounds of the present invention may be either positive or negative. Any associated counterions are typically determined by the synthesis and / or isolation methods by which the compounds are obtained. Typical counterions include, but are not limited to, ammonium, sodium, potassium, lithium, halides, acetates, trifluoroacetates, and the like, and mixtures thereof. Organic bases from which salts can be derived include, for example, primary, secondary, and tertiary amines, substituted amines, including naturally occurring substituted amines, cyclic amines, basic ion exchange resins, and the like, specifically, for example, isopropylamine, trimethylamine, diethylamine, triethylamine, tripropylamine, ethanolamine, and the like. It will be understood that the identity of any associated counterion is not a critical feature of the present invention, and the present invention encompasses compounds associated with any type of counterion. Furthermore, because the compounds can exist in a variety of different forms, the present invention is intended to encompass not only forms of the compounds associated with a counterion (e.g., dry salts), but also forms not associated with a counterion (e.g., aqueous or organic solutions). Metal salts are typically prepared by reacting a metal hydroxide with the compounds of the present invention. Examples of metal salts prepared in this manner include Li + , Na + , and K +

[0033] Examples of suitable acids include inorganic acids such as hydrohalogen acids, e.g., hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like; and organic acids such as acetic acid, propanoic acid, hydroxyacetic acid, 2-hydroxypropanoic acid, 2-oxopropanoic acid, lactic acid, pyruvic acid, oxalic acid (i.e., ethanedioic acid), malonic acid, succinic acid (i.e., butanedioic acid), maleic acid, fumaric acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, cyclohexanesulfamic acid, salicylic (i.e., 2-hydroxybenzoic) acid, p-aminosalicylic acid, and the like.

[0034] In addition, salts can be formed from the acid addition of certain organic and inorganic acids to basic centers, typically amines, or acidic groups. Examples of suitable acids include inorganic acids such as hydrohalogen acids, e.g., hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like; and organic acids such as acetic acid, propanoic acid, hydroxyacetic acid, 2-hydroxypropanoic acid, 2-oxopropanoic acid, lactic acid, pyruvic acid, oxalic acid (i.e., ethanedioic acid), malonic acid, succinic acid (i.e., butanedioic acid), maleic acid, fumaric acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, cyclohexanesulfamic acid, salicylic (i.e., 2-hydroxybenzoic) acid, p-aminosalicylic acid, and the like. Furthermore, this term also includes solvates, such as hydrates, alcoholates, etc., which the compounds of the formulae herein and their salts are able to form. Finally, it is to be understood that the compositions herein may include the compounds of the invention in their non-ionized form, as well as their zwitterionic form, and in the case of hydrates, in combination with a stoichiometric amount of water.

[0082] Also included within the scope of the present invention are salts of compounds having one or more amino acids, particularly the naturally occurring amino acids found as protein components. Amino acids typically have side chains with basic or acidic groups, such as lysine, arginine, or glutamic acid, or neutral groups, such as glycine, serine, threonine, alanine, isoleucine, or leucine.

[0083] The compounds of the present invention also include physiologically acceptable salts thereof. Examples of physiologically acceptable salts of the compounds of the present invention include alkali metal (e.g., sodium), alkaline earth (e.g., magnesium), ammonium, and NX4 salts. +(wherein X is C1-C4 alkyl). Physiologically acceptable salts of hydrogen atoms or amino groups include salts of organic carboxylic acids such as acetic acid, benzoic acid, lactic acid, fumaric acid, tartaric acid, maleic acid, malonic acid, malic acid, isethionic acid, lactobionic acid, and succinic acid; organic sulfonic acids such as methanesulfonic acid, ethanesulfonic acid, benzenesulfonic acid, and p-toluenesulfonic acid; and inorganic acids such as hydrochloric acid, sulfuric acid, phosphoric acid, and sulfamic acid. Physiologically acceptable salts of compounds containing a hydroxy group include salts of Na + and NX4 + (wherein X is typically independently selected from -H or a C1-C4 alkyl group.) However, salts of acids and bases that are not physiologically acceptable may also find use, for example, in the preparation or purification of a physiologically acceptable compound.

[0084] All salts are within the scope of the present invention, whether or not derived from a physiologically acceptable acid or base. Non-limiting examples of suitable such salts include those formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, or with acetic acid, propionic acid, hexanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, 3-(4-hydroxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzoic ... Examples of suitable acid addition salts include, but are not limited to, those formed with organic acids such as benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, 4-methylbicyclo[2.2.2]-oct-2-ene-1-carboxylic acid, glucoheptonic acid, 3-phenylpropionic acid, trimethylacetic acid, tertiary butylacetic acid, laurylsulfonic acid, gluconic acid, glutamic acid, hydroxynaphthoic acid, salicylic acid, stearic acid, and muconic acid. Other salts include 2,2-dichloroacetate, adipate, alginate, ascorbate, aspartate, 2-acetamidobenzoate, caproate, caprate, camphorate, cyclamate, lauryl sulfate, edisylate, esylate, isethionate, formate, galactarate, gentisate, gluceptate, glucuronate, oxoglutarate, hippurate, lactobionate, napadisylate, xinafoate, nicotinate, oleate, orotate, oxalate, palmitate, embonate, pidophosphate, and p-aminobenzoate. Included are salicylates, sebacates, tannates, rhodanide salts, undecylenates, etc., or salts formed when an acidic proton present in the parent compound is replaced with, for example, ammonia, arginine, benethamine, benzathine, calcium, choline, deanol, diethanolamine, diethylamine, ethanolamine, ethylenediamine, meglumine, glycine, hydrabamine, imidazole, lysine, magnesium, hydroxyethylmorpholine, piperazine, potassium, epolamine, sodium, trolamine, tromethamine, or zinc.

[0085] The present invention includes within its scope solvates of the compounds defined herein. The term "solvate" refers to a crystal formed by an active compound and a second component (solvent) that is liquid at room temperature in isolated form. Such solvates can be formed with common organic solvents, for example, hydrocarbon solvents such as benzene or toluene, chlorinated solvents such as chloroform or dichloromethane, alcoholic solvents such as methanol, ethanol, or isopropanol, ethereal solvents such as diethyl ether or tetrahydrofuran, or ester solvents such as ethyl acetate. Alternatively, solvates of the compounds herein can be formed with water, in which case they will be hydrates.

[0086] The compounds of formula (I) may be amorphous or may exist in one or more different crystalline states (polymorphs) which may have different macroscopic properties, such as stability, or may exhibit different biological properties, such as activity. The present invention relates to amorphous and crystalline compounds of formula (I), and mixtures of different crystalline states of each compound of formula (I).

[0087] The term "polymorph" refers to a specific crystalline form of a compound that can crystallize in different crystalline forms, which have different arrangements and / or conformations of molecules within the crystal lattice. Different crystalline forms typically have different X-ray diffraction patterns, infrared spectra, melting points, densities, hardness, crystal shape, optical and electrical properties, stability, and solubility. While polymorphs can have the same chemical composition, they may also differ in composition due to the presence or absence of co-crystallized water or other molecules that may be weakly or strongly bound within the lattice. Polymorphs may differ in chemical, physical, and biological properties, such as crystal shape, density, hardness, color, chemical stability, melting point, hygroscopicity, suspendability, dissolution rate, and bioavailability. Those skilled in the art will understand that polymorphs of the compounds described herein may exhibit beneficial effects (e.g., suitability for the preparation of useful formulations, improved biological performance) compared to other polymorphs or mixtures of polymorphs of the same compound. The preparation and isolation of specific polymorphs of a compound can be achieved by methods known to those skilled in the art, including, for example, crystallization using selected solvents and temperatures. The recrystallization solvent, rate of crystallization, storage temperature, and other factors can cause one crystalline form to predominate. Various polymorphs of a compound can be prepared by crystallization under different conditions. For a comprehensive discussion of polymorphism, see Rolf Hilfiker, Ed., Polymorphism in the Pharmaceutical Industry, Wiley-VCH, Weinheim, 2006.

[0088] When referring to compositions and products and the weight percentages of ingredients contained therein, it is understood that in accordance with the present invention, the total amount of ingredients does not exceed 100% (±1% rounded).

[0089] As used herein, the term "non-therapeutic" refers to a concept that excludes medical intervention, i.e., the treatment of the human body with medical therapy.

[0090] Preferred descriptions (features) and embodiments of the methods, compositions, and uses of the present invention are set forth herein below. Each description and embodiment of the present invention so defined may be combined with any other description and / or embodiment, unless expressly indicated to the contrary. In particular, any feature indicated as being preferred or advantageous may be combined with any other feature or description indicated as being preferred or advantageous. The present invention is particularly incorporated herein by any one or any combination of one or more of the following numbered descriptions and embodiments, together with any other aspects and / or embodiments.

[0091] 1. A compound of formula (I), [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, wherein: Ar 1 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R za may be replaced by Each R za are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a Rb , and -NR b C(O)R a and selected from the group comprising: Each R a are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Each of the alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl; R h is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R a1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R b1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R c1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; Each R b is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2a But, -(CR c R d ) n and n is an integer selected from 1, 2, or 3; Each R c and R dare independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R f is alkylene, which may be interrupted by one or more O or S; R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a But, -OR a , -R a , or -NR a R b or Y 1ais part of formula (A), [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -OR a , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c R d ) m and m is an integer selected from 1, 2, or 3; Y 1b But, -OR a , -NR b R a , or -R a is selected from however, [ka] but, [ka] provided that it is not However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-amino-4-oxo-4-(2-(((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate, A compound, or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, provided that the compound is not 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid.

[0092] 2. A compound of formula (I), [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, wherein: Ar 1 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R za may be replaced by Each R zaare independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: Each R a are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Each R b is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NR bselected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2a But, -(CR c R d ) n wherein n is an integer selected from 1, 2, or 3, preferably 1 or 2, and preferably n is 1; Each R c and R d are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R fis alkylene, which may be interrupted by one or more O or S; R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a is a moiety of formula (A), or Y 1a But, -OR a , -R a , or -NR a R b is selected from [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -OR a, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c R d )m and m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1; Y 1b But, -OR a , -NR b R a , or -R a is selected from however, [ka] but, [ka] provided that it is not However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-amino-4-oxo-4-(2-(((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, and methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate, A compound, or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, provided that the compound is not 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid.

[0093] 3. A compound of formula (II), [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, wherein: R 1a , R 2a , R 3a , and R 4a are each independently R za and Each R za are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: Each R aare independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, and -R f1 -R g1 and wherein each of the alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl; R h is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R a1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R b1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R c1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R f1is alkylene, which may be interrupted by one or more O or S; R g1 is hydrogen or alkyl, Each R b is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2a But, -(CR c R d ) n and n is an integer selected from 1, 2, or 3; Each R c and R dare independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R f is alkylene, which may be interrupted by one or more O or S; R g is selected from hydrogen, alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a But, -OR a , -R a , or -NR a R b or Y1a is part of formula (A), [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -OR a , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c R d ) m and m is an integer selected from 1, 2, or 3; Y 1b But, -OR a , -NR b R a , or -R a or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof selected from:

[0094] 4. A compound of formula (II), [ka] or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, wherein: R 1a , R 2a , R 3a , and R 4a are each independently R za and Each R zaare independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: Each R a are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, and -R f1 -R g1and wherein each of the alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl; R h is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R a1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R b1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R c1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R f1 is alkylene, which may be interrupted by one or more O or S; R g1 is hydrogen or alkyl, Each R b is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X 1a But, -NRb - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2a But, -(CR c R d ) n and n is an integer selected from 1, 2, or 3; Each R c and R d are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R e is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R f is alkylene, which may be interrupted by one or more O or S; R gis selected from hydrogen, alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W 1a But, -NR b Z 2a , -R a , or -OR a is selected from Z 2a But hydrogen, -CO-R a , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y 1a But, -OR a , -R a , or -NR a R b or Y 1a is part of formula (A), [ka] During the ceremony, Ar 2 is aryl or heteroaryl, each of which may be unsubstituted or may contain one or more R zb may be replaced by Each R zb are independently hydrogen, halo, alkyl, haloalkyl, -OR a, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and selected from the group comprising: X 1b But, -NR b selected from -, -O-, -S-, SO2-O-, or -SO-O-; Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X 2b But, -(CR c R d )m and m is an integer selected from 1, 2, or 3; Y 1b But, -OR a , -NR b R a , or -R a is selected from However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-amino-4-oxo-4-(2-(((3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, (2S)-2-amino-4-oxo-4-(2-(((3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (S)-2-acetamido-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (R)-2-acetamido-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate, 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, 5-(2-aminophenyl)-5-oxopentanoic acid, 4-(2-aminophenyl)-4-oxobutanoic acid, methyl 6-(2-aminophenyl)-6-oxohexanoate, methyl 4-(2-aminophenyl)-2-((tert-butoxycarbonyl)amino)-4-oxobutanoate, butyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, ethyl (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoate, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid diacetate, (R)-2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, 2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, methyl 2-acetamido-4-(2-acetamidophenyl)-4-oxobutanoate, 4-(2-amino-3-(((2R,3S,4R,5R,6S)-3,4,5-trihydroxy-6-((((2S,3S,4R,5R,6S)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)methyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-D-diglucoside), 4-(2-amino-3-(((2R,3S,4R,5R,6S)-3,4-5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-d-glucoside, 2-amino-4-(2-formamido-5-hydroxyphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, 2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (R)-2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (S)-2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, (S-) 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, (R-) 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, methyl (S-)2-amino-4-(2-aminophenyl)-4-oxobutanoate, 2-amino-4-(2-aminophenyl)-4-oxobutanamide, (R)-2-amino-4-(2-aminophenyl)-4-oxobutanamide, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanamide, (S)-2-acetamido-4-(2-acetamidophenyl)-4-oxobutanoic acid, (S)-2-Formamido-4-(2-formamidophenyl)-4-oxobutanoic acid, and 4-(2-aminophenyl)-4-oxo-2-phenylbutanamide, or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, provided that the compound is not 4-(2-aminophenyl)-4-oxo-2-phenylbutanamide.

[0095] 5. Ar 1 But C 6-10 aryl or 5- to 10-membered heteroaryl, each of which may be unsubstituted or may contain one or more R za and preferably, Ar 1 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R za and preferably, Ar 1 But C 6-10 aryl, or a 6-membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more R za and preferably, Ar 1 is phenyl, which may be unsubstituted or may contain one or more R za and preferably, Ar 1 is phenyl, Each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glucosyl, non-acylated or acylated-O-glucosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R za are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R zais hydrogen, Each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 Each alkynylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , Haro, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R h But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R a1 But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R b1 But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R c1 But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and preferably each R aare independently hydrogen, halo, C 1-18 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, 1-18 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , Haro, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 1-6 alkylcarbonyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R his hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 5- to 6-membered heterocyclyl containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, wherein the C 1-15 Alkyl, C 2-15 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 5- to 6-membered heterocyclyl containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6alkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, wherein the C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 4-membered heterocyclyl containing at least one O, and phenyl, 1-15 Alkyl, C2-8 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 4-membered heterocyclyl containing at least one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, oxiranyl, and C 1-8 alkylcarbonyl, 1-15 Alkyl, C 2-6 Alkenyl, oxiranyl, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl, and oxiranyl, 1-15 Alkyl, C 2-6 Alkenyl, oxiranyl, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-4 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, e.g., each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, and preferably each R a are independently hydrogen, halo, C 1-18 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 5- to 6-membered heterocyclyl containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3-4 membered heterocyclyl containing at least one O, and phenyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, oxiranyl, and C 1-8 alkylcarbonyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 selected from the group consisting of alkenyl, and oxiranyl; Each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 6-10 aryl, and preferably each R b are independently hydrogen, C 1-6 Alkyl and haloC 1-6 alkyl, and preferably each R b are independently hydrogen or C 1-6 alkyl, and preferably each R b is hydrogen, X 1a But, -NR b-, -O-, -S-, SO2-O-, or -SO-O-, preferably X 1a But, -NR b -, -O-, -S-, preferably X 1a But, -NR b -, or -O-, preferably X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6alkynylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 Alkylene, 5-6 membered heterocyclyl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f-Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one N or one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-C2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2a But, -(CR c R d ) n and preferably X 2a But, -(CR c H) n and preferably X 2a But -(CH2) n and preferably X 2a But -(CH2) n -, n is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably n is 1, and preferably X 2a is -CH2-, Each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each Rc and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 6-10 aryl, and preferably each R c and R d are independently hydrogen or C 1-6 alkyl, and preferably each R c and R d are independently hydrogen, R e But C 1-12 Alkylene, C 2-12 Alkenylene, C 2-12 Alkynylene, C 6-10 Arylene, 3- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylene, C 6-10 Arylene, 3- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 6-10 Arylene, 3- to 5-membered heterocyclylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, and C 3-6 cycloalkylene, preferably R e But C 1-4 Alkylene or C 2-4 alkenylene, preferably R e But C 2-4 Alkenylene or C 1-3 alkylene, preferably R e But C 2-4 alkenylene, preferably R eBut C 2-3 is alkenylene, R f But C 1-20 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-16 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-14 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-10 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 is alkylene, R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl, preferably R g is N-maleimidyl or N-maleimidyloxy, preferably R g is N-maleimidyl, W 1a But, -NR b Z 2a , -R a , or -OR a Preferably, W 1a But, -NR b Z 2a , or -R a Preferably, W 1a But, -NHZ 2a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a, Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a However, NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , C 1-6 Alkyl, C 1-6 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a and preferably W 1a But -NHCO-C 1-12 alkyl, preferably W 1a But -NHCO-C 1-10 alkyl, preferably W 1a But -NHCO-C 1-8 alkyl, preferably W 1a But -NHCO-C 1-6 is alkyl, Z 2a But hydrogen, -CO-R a , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, preferably Z 2a But hydrogen, -CO-R a , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-10 Alkyl, C 1-10 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, C1-8 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, preferably selected from the group consisting of Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But hydrogen, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But C 1-8 alkylcarbonyl, Y 1a is a moiety of formula (A), or -OR a , -R a , or -NR a R b is selected from [ka] Preferably, Y 1a is a moiety of formula (A), or -OR a or -NHR a and preferably, Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1a is part of formula (A), Ar 2 But C 6-10 aryl or 5- to 10-membered heteroaryl, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 But C 6-10aryl or 6-membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, Each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SRa , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glucosyl, non-acylated or acylated-O-glucosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R zb are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R zb is hydrogen, X 1b But, -NR b -, -O-, -S-, SO2-O-, or -SO-O-, preferably X 1b But, -NR b -, -O-, -S-, preferably X 1b But, -NR b -, or -O-, preferably X 1b But, -NR b - and Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g, Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one N or one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2b But, -(CR c R d ) m and preferably X 2b But, -(CR c H) m and preferably X 2b But -(CH2) m and preferably X 2b But -(CH2) m -, m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1, and preferably X 2b is -CH2-, Y 1b But, OR a , -NR b R a , or R a Preferably, Y 1b But, -OR a , or -NHR a and preferably, Y 1b However, -OH, -NH2, -OC 1-12Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1b However, -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1b But, -OC 1-10 Alkyl, or -NH-C 1-10 A compound according to statement 1 or 2, wherein the compound is alkyl.

[0096] 6. Ar 1 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R za and preferably the aryl or heteroaryl may be unsubstituted or may contain one, two, three, or four R za may be replaced by Y 1a is a moiety of formula (A), or -OR a , -R a , or -NR a R b is selected from Ar 2 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, the aryl or heteroaryl may be unsubstituted or may contain one, two, three, or four R zb may be replaced by In the formula, R za , R zb , R a , R b has the same meaning as defined in any one of statements 1 to 2, 5.

[0097] 7. Ar 1 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R za and preferably, Ar 1 But C 6-10 aryl, or a 6-membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more Rza and preferably, Ar 1 is phenyl, which may be unsubstituted or may contain one or more R za and preferably, Ar 1 is phenyl, Each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R za are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R za is hydrogen, Y 1a is a moiety of formula (A), or -OR a , -R a , or -NR a R b Preferably, Y 1a is part of formula (A), [ka] Ar 2 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 But C 6-10 aryl, or a 6-membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, Each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R zbare independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R zb is hydrogen.

[0098] 8. R 1a , R 2a , R 3a , and R 4a are each independently R za and Each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b-glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glucosyl, non-acylated or acylated-O-glucosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC1-6 Alkyl and haloC 1-6 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R za are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R za is hydrogen, Each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylene, and -Rf1 -R g1 wherein the C is selected from the group comprising 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 Each alkynylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , Haro, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and Rh But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R a1 But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R b1 But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R c1 But hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl, and C 2-6 alkynyl, and R f1 But C 1-20 alkylene, 1-20 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-20 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-18 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, and -R f1 -R g1 wherein the C is selected from the group comprising 1-18 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , Haro, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 1-6 alkylcarbonyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-10 alkylene, 1-10 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-10 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, and -R f1 -R g1 wherein the C is selected from the group comprising 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-8 alkylene, 1-8 The alkylene may be interrupted by one or more O or S, and Rg1 is hydrogen or C 1-8 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 5- to 6-membered heterocyclyl containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-15 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 5- to 6-membered heterocyclyl containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-6 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclyl containing at least one N or one O, C 5-6 Cycloalkyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-6 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Alkylcarbonyl, 3-4 membered heterocyclyl containing at least one O, phenyl, -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-8 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 4-membered heterocyclyl containing at least one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , Haro, C 1-6 Alkyl and haloC 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O, and R g1 is hydrogen or C 1-6 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C2-6 Alkenyl, oxiranyl, C 1-8 Alkylcarbonyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-6 Alkenyl, oxiranyl, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O, and R g1 is hydrogen or C 1-6 alkyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl, and oxiranyl, 1-15 Alkyl, C 2-6 Each of the alkenyl and oxiranyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-4 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O, and R g1 is hydrogen or C 1-4 alkyl, e.g., each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, and preferably each R a are independently hydrogen, halo, C 1-18 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 5- to 6-membered heterocyclyl containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3-4 membered heterocyclyl containing at least one O, and phenyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, oxiranyl, and C 1-8 alkylcarbonyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 selected from the group consisting of alkenyl, and oxiranyl; Each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 6-10 aryl, and preferably each R b are independently hydrogen, C 1-6 Alkyl and haloC 1-6 alkyl, and preferably each R b are independently hydrogen or C 1-6 alkyl, and preferably each R b is hydrogen, X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 Alkylene, 5-6 membered heterocyclyl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one N or one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2a But, -(CR c R d ) n and preferably X 2a But, -(CR c H) n and preferably X 2a But -(CH2) n and preferably X 2a But -(CH2) n-, n is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably n is 1, and preferably X 2a is -CH2-, Each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R c and R d are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 6-10 aryl, and preferably each R c and R d are independently hydrogen or C 1-6 alkyl, and preferably each R c and R d are independently hydrogen, R e But C 1-12 Alkylene, C 2-12 Alkenylene, C 2-12 Alkynylene, C 6-10 Arylene, 3- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylene, C 6-10 Arylene, 4- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 6-10 Arylene, 3- to 5-membered heterocyclylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, and C 3-6 cycloalkylene, preferably R e But C 1-4 Alkylene or C 2-4 alkenylene, preferably R e But C 2-4 Alkenylene or C 1-3 alkylene, preferably R e But C 2-4 alkenylene, preferably R e But C 2-3 is alkenylene, R f But C 1-20 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-16 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-14 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-10 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 is alkylene, R g But hydrogen, C 1-20 alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl, preferably R g But hydrogen, C 1-10 alkyl, N-maleimidyl, or N-maleimidyloxy, preferably R g But hydrogen, C 1-6 alkyl, N-maleimidyl, W 1a But, -NR b Z 2a , -R a , or -OR a Preferably, W 1a But, -NR b Z 2a , or -R a Preferably, W 1a But, -NHZ 2a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a However, NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , C 1-6 Alkyl, C 1-6Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a and preferably W 1a But -NHCO-C 1-12 alkyl, preferably W 1a But -NHCO-C 1-10 alkyl, preferably W 1a But -NHCO-C 1-8 alkyl, preferably W 1a But -NHCO-C 1-6 is alkyl, Z 2a But hydrogen, -CO-R a , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6 alkynylene, preferably Z 2a But hydrogen, -CO-Ra , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-10 Alkyl, C 1-10 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, preferably selected from the group consisting of Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But hydrogen, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But C 1-8alkylcarbonyl, Y 1a is a moiety of formula (A), or -OR a , -R a , or -NR a R b is selected from [ka] Preferably, Y 1a is a moiety of formula (A), or -OR a or -NHR a and preferably, Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1a is part of formula (A), Ar 2 But C 6-10 aryl or 5- to 10-membered heteroaryl, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 But C 6-10 aryl or 6-membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, Each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a, non-acylated or acylated glucosyl, non-acylated or acylated-O-glucosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R zb are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R zb is hydrogen, X 1b But, -NR b-, -O-, -S-, SO2-O-, or -SO-O-, preferably X 1b But, -NR b -, -O-, -S-, preferably X 1b But, -NR b -, or -O-, preferably X 1b But, -NR b - and Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclyl-C 2-6 Alkynylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, and C 3-6 Cycloalkyl-C 2-6alkynylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heteroaryl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f-Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one N or one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-C2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2b But, -(CR c R d ) m and preferably X 2b But, -(CR c H) m and preferably X 2b But -(CH2) m and preferably X 2b But -(CH2) m -, m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1, and preferably X 2b is -CH2-, Y 1b But, OR a , -NR b R a , or R a Preferably, Y 1b But, -OR a , or -NHR a and preferably, Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1b However, -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1b But, -OC 1-10 Alkyl, or -NH-C 1-10 A compound according to any one of statements 3 or 4, wherein:

[0099] 9. Y 1a is a moiety of formula (A), or -OR a , -R a , or -NR a R b is selected from Ar 2 But C 6-10 aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of which may be unsubstituted or may contain one or more R zband preferably, the aryl or heteroaryl may be unsubstituted or may contain one, two, three, or four R zb may be replaced by In the formula, R za , R zb , R a , R b has the same meaning as defined in any one of statements 1 to 8.

[0100] 10. Each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6Alkyl, and -OR a and preferably, each R za are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. za are independently hydrogen, halo, and C 1-4 alkyl, and preferably each R za are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R za is hydrogen, Y 1a is a moiety of formula (A), or -OR a , -R a , or -NR a R b is selected from Ar 2 But C 6-10 aryl or 5-6 membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 But C 6-10 aryl, or a 6-membered heteroaryl containing at least one N, each of which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, which may be unsubstituted or may contain one or more R zb and preferably, Ar 2 is phenyl, Each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , non-acylated or acylated glycosyl, non-acylated or acylated-O-glycosyl, non-acylated or acylated-NR b -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably, each R zb are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Preferably, each R is selected from the group including alkyoxy. zb are independently hydrogen, halo, and C 1-4alkyl, and preferably each R zb are independently selected from hydrogen, halo, or C 1-3 alkyl, and preferably, each R zb is hydrogen.

[0101] 11. Having the structural formula (II): [ka] In the formula, Y 1a is part of formula (B), or OR a , R a , N.R. a R b is selected from [ka] In the formula, R 1a , R 2a , R 3a , and R 4a are each independently R za and R 1b , R 2b , R 3b , and R 4b are each independently R zb and Z 1a , X 1a , X 2a , W 1a , Z 1b , X 1b , X 2b , Y 1b , R b , R za , and R zb has the same meaning as defined in any one of statements 1 to 4, Preferably, R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , and R 4b each independently represents hydrogen, halo, alkyl, haloalkyl, -OR a, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR a , -C(O)-R a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkynylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 2-6 Alkenylene, 5-10 membered heteroaryl-C 2-6 Alkynylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 2-6 Alkenylene, 3-10 membered heterocyclylC 2-6 Alkynylene, C 3-6 Cycloalkyl-C1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylene, -OR a , -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, -OR a , -SR a , -S(O)R a , -NR a R b , and -NR b C(O)R a and preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a , -NR a R b , and -NR b C(O)R aand preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and -OR a and preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl and haloC 1-6 Alkyoxy, preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, C 1-4 Alkyl, HaloC 1-4 Alkyl and haloC 1-4 Alkyoxy, preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, and C 1-4 alkyl, preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b are each independently hydrogen, halo, or C 1-3alkyl, preferably R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , R 4b is independently at each occurrence hydrogen.

[0102] 12. Each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, wherein the C 1-16 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, wherein the C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one N or one O, and phenyl, 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one N or one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl, and oxiranyl, 1-15 Alkyl, C 2-4 Each of alkenyl and oxiranyl is unsubstituted or has one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, For example, each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-10alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3-5 membered heterocyclyl containing at least one N or one O, and phenyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 selected from the group consisting of alkenyl, and oxiranyl; Each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-10 membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 aryl, and preferably each R b are independently hydrogen, C 1-6 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-4 Alkylene and haloC 1-6 alkyl, and preferably each R b are independently hydrogen, oxiranyl-C 1-2 Alkylene, or C 1-6 alkyl, and preferably each R b is hydrogen, X 1a But, -NR b - or -O-, preferably X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-R a , --CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkylcarbonyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, and C 2-4 alkenylcarbonyl; X 2a But, -(CR c H) n and preferably X 2a But -(CH2) n and preferably X 2a But -(CH2) n-, n is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably n is 1, and preferably X 2a is -CH2-, Each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 6-10 aryl, and preferably each Rc are independently hydrogen or C 1-6 alkyl, and preferably each R c is hydrogen, R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylene, C 6-10 Arylene, 3- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 6-10 Arylene, 3- to 5-membered heterocyclylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, and C 3-6 cycloalkylene, preferably R e But C 1-4 Alkylene or C 2-4 alkenylene, preferably R e But C 2-4 Alkenylene or C 1-3 alkylene, preferably R e But C 2-4 alkenylene, preferably R e But C 2-3 is alkenylene, R f But C 1-20 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-16 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-14 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-10alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 is alkylene, R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl, preferably R g is N-maleimidyl or N-maleimidyloxy, preferably R g is N-maleimidyl, W 1a But, -NR b Z 2a , or -R a Preferably, W 1a But, -NHZ 2a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a However, NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , C 1-6 Alkyl, C 1-6 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a and preferably W1a But -NHCO-C 1-12 alkyl, preferably W 1a But -NHCO-C 1-10 alkyl, preferably W 1a But -NHCO-C 1-8 alkyl, preferably W 1a But -NHCO-C 1-6 is alkyl, Z 2a But hydrogen, -CO-R a , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-10 Alkyl, C 1-10 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6cycloalkyl, preferably selected from the group consisting of Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But hydrogen, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But C 1-8 alkylcarbonyl, Y 1a is a moiety of formula (A) or (B), or -OR a or -NHR a and preferably, Y 1a is a moiety of formula (A) or (B), or Y 1a However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A), or -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1a is a moiety of formula (A) or (B), or Y 1a However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1a is part of formula (B), X 1b But, -NR b - or -O-, preferably X 1b But, -NR b - and Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6Alkyl, 3-4 membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, C 1-8 Alkyl, oxiranyl-C 1-4 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, oxiranyl-C 1-2 Alkylene, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2b But, -(CR c H) m and preferably X 2b But -(CH2) m and preferably X 2b But -(CH2) m -, m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1, and preferably X 2b is -CH2-, Y 1b But, -OR a , or -NHR a and preferably, Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1b However, -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10alkyl, preferably Y 1b But, -OC 1-10 Alkyl, or -NH-C 1-10 The compound according to any one of statements 1-2, 5-11, wherein R is alkyl.

[0103] 13. Each R a are independently hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, wherein the C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and Ra1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, wherein the C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl, 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and preferably each R a are independently hydrogen, halo, C 1-10 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, 1-10 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl, and oxiranyl,1-15 Alkyl, C 2-4 Each of the alkenyl and oxiranyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, e.g., each R a are independently hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 selected from the group consisting of alkenyl, and oxiranyl; Each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 10-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 aryl, and preferably each R b are independently hydrogen, C 1-6 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-4 Alkylene and haloC 1-6 alkyl, and preferably each R b are independently hydrogen, oxiranyl-C 1-2 Alkylene, or C 1-6 alkyl, and preferably each R b is hydrogen, X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a, -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , --CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-4 Alkylene-, C 1-8Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylene, C 6-10 Arylene, 3- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 6-10 Arylene, 3- to 5-membered heterocyclylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, and C 3-6 cycloalkylene, preferably R e But C 1-4 Alkylene or C 2-4 alkenylene, preferably R e But C 2-4 Alkenylene or C 1-3 alkylene, preferably R e But C 2-4 alkenylene, preferably R e But C 2-3 is alkenylene, R f But C 1-20 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-16alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-14 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-10 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 is alkylene, R g is selected from N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl, preferably R g is N-maleimidyl or N-maleimidyloxy, preferably R g is N-maleimidyl, X 2a But -(CH2) n and preferably X 2a But -(CH2) n -, n is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably n is 1, and preferably X 2a is -CH2-, W 1a But, -NHZ 2a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a However, NHCO-R a, hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , C 1-6 Alkyl, C 1-6 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a and preferably W 1a But -NHCO-C 1-12 alkyl, preferably W 1a But -NHCO-C 1-10 alkyl, preferably W 1a But -NHCO-C 1-8 alkyl, preferably W 1a But -NHCO-C 1-6 is alkyl, Z 2a But hydrogen, -CO-R a , C 1-10 Alkyl, C 1-10 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, and C 3-6 cycloalkyl, preferably selected from the group consisting of Z 2a But hydrogen, -CO-R a , C1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But hydrogen, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But C 1-8 alkylcarbonyl, Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC3-6 cycloalkyl, preferably Y 1a is a moiety of formula (B), or -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1a is a moiety of formula (B), or -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1a is part of formula (B), X 1b But, -NR b - and Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one O1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , --CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2bBut -(CH2) m and preferably X 2b But -(CH2) m -, m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1, and preferably X 2b is -CH2-, Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl and -NHC1-12 alkyl, preferably Y 1b However, -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1b But, -OC 1-10 Alkyl, or -NH-C 1-10 13. The compound according to any one of statements 1 to 12, wherein:

[0104] 14. Each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, and -R f1 -R g1 wherein the C is selected from the group comprising 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more Rza1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-20 alkylene, 1-20 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-20 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, and -R f1 -R g1 wherein the C is selected from the group comprising 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-15 alkylene, 1-15 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-15 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and -Rf1 -R g1 wherein the C is selected from the group comprising 1-16 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-10 alkylene, 1-10 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-10 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, C 5-6 Cycloalkyl, and -Rf1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-8 alkylene, 1-8 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-8 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one N or one O, phenyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one N or one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-6 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, 3-4 membered heterocyclyl containing at least one O, C 1-8 Alkylcarbonyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-16 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-Rh , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-4 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 Alkenyl, oxiranyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-4 Each of alkenyl and oxiranyl is unsubstituted or has one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-4 is alkyl, For example, each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3-5 membered heterocyclyl containing at least one N or one O, and phenyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 selected from the group consisting of alkenyl, and oxiranyl; Each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 1-6 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-10 membered heteroaryl, and C 3-6cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 aryl, and preferably each R b are independently hydrogen, C 1-6 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-4 Alkylene and haloC 1-6 alkyl, and preferably each R b are independently hydrogen, oxiranyl-C 1-2 Alkylene, or C 1-6 alkyl, and preferably each R b is hydrogen, X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -Rf -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g, -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, C 3-6Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-R a , --CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkylcarbonyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C1-2 Alkylene, and C 2-4 alkenylcarbonyl; X 2a But, -(CR c H) n and preferably X 2a But -(CH2) n and preferably X 2a But -(CH2) n -, n is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably n is 1, and preferably X 2a is -CH2-, Each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R c are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, and C 6-10 aryl, and preferably each R c are independently hydrogen or C 1-6 alkyl, and preferably each R c is hydrogen, R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylene, C 6-10 Arylene, 3- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 6-10 Arylene, 3- to 5-membered heterocyclylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, and C 3-6 cycloalkylene, preferably R e But C 1-4 Alkylene or C 2-4 alkenylene, preferably R e But C 2-4 Alkenylene or C 1-3 alkylene, preferably R e But C 2-4 alkenylene, preferably R e But C 2-3 is alkenylene, R f But C 1-20alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-16 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-14 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-10 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 is alkylene, R g But hydrogen, C 1-20 Alkyl, N-maleimidyl, N-maleimidyloxy, or hydrogen, C 1-10 alkyl, N-maleimidyloxycarbonyl, preferably R g But hydrogen, C 1-6 alkyl, N-maleimidyl, or N-maleimidyloxy, preferably R g But hydrogen, C 1-4 alkyl, N-maleimidyl, W 1a But, -NR b Z 2a , or -R a Preferably, W 1a But, -NHZ 2a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C6-10 aryl, preferably W 1a However, NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , C 1-6 Alkyl, C 1-6 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a and preferably W 1a But -NHCO-C 1-12 alkyl, preferably W 1a But -NHCO-C 1-10 alkyl, preferably W 1a But -NHCO-C 1-8 alkyl, preferably W 1a But -NHCO-C 1-6 is alkyl, Z 2a But hydrogen, -CO-R a , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-10 Alkyl, C 1-10 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, and C 3-6 cycloalkyl, preferably selected from the group consisting of Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But hydrogen, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But C 1-8 is alkylcarbonyl, Y 1a is a moiety of formula (A) or (B), or -OR a or -NHR a and preferably, Y 1a is a moiety of formula (A) or (B), or Y 1a However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1a is a moiety of formula (A) or (B), or Y 1a However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1a is part of formula (B), X 1b But, -NR b - or -O-, preferably X 1b But, -NR b - and Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -Rf -R g , Haro, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g, -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C3-6 Cycloalkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3-4 membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, C 1-8 Alkyl, oxiranyl-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, oxiranyl-C 1-2 Alkylene, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, C1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; X 2b But, -(CR c H) m and preferably X 2b But -(CH2) m and preferably X 2b But -(CH2) m -, m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1, and preferably X 2b is -CH2-, Y 1b But, -OR a , or -NHR a and preferably, Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1b However, -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1b But, -OC 1-10 Alkyl, or -NH-C 1-10 14. The compound according to any one of statements 1 to 13, wherein:

[0105] 15. Each R a are independently hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene, and -R f1 -R g1 wherein the C is selected from the group comprising 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-16 alkylene, 1-16 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-16 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and -R f1 -R g1wherein the C is selected from the group comprising 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-10 alkylene, 1-10 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-10 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, C5-6 Cycloalkyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-6 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, phenyl, and -R f1 -R g1 wherein the C is selected from the group comprising1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-6 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, 3-4 membered heterocyclyl containing at least one O, C 1-8 Alkylcarbonyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-6 alkylene, 1-6 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-6 alkyl, which may preferably be unsubstituted or may contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, and R f1 But C 1-4 alkylene, 1-4The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-4 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 Alkenyl, oxiranyl, and -R f1 -R g1 wherein the C is selected from the group comprising 1-15 Alkyl, C 2-4 Each of the alkenyl and oxiranyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, and R f1 But C 1-4 alkylene, 1-4 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-4 alkyl, e.g., each R a are independently hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, and preferably each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl, and preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, and preferably each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4selected from the group consisting of alkenyl, and oxiranyl; Each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N, 3- to 6-membered heterocyclyl-C containing at least one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R b are independently hydrogen, halo, C 1-6 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 aryl, and preferably each R b are independently hydrogen, C 1-6 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-4 Alkylene and haloC 1-6 alkyl, and preferably each R b are independently hydrogen, oxiranyl-C 1-2 Alkylene, or C 1-6 alkyl, and preferably each R b is hydrogen, X 1a But, -NR b - and Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1a But hydrogen, -CO-R a , --CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, C 1-8 Alkyl, -CO-C2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1a But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl; R e But C 1-6 Alkylene, C 2-6 Alkenylene, C 6-10 Arylene, 3- to 5-membered heterocyclylene, and C 3-6 cycloalkylene, preferably R e But C 1-6 Alkylene, C 2-6 Alkenylene, and C 3-6 cycloalkylene, preferably R e But C 1-4 Alkylene or C 2-4 alkenylene, preferably R e But C 2-4 Alkenylene or C 1-3 alkylene, preferably R e But C 2-4 alkenylene, preferably R e But C 2-3 is alkenylene, R f But C 1-20 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-16 alkylene, which may be interrupted by one or more O or S, preferably R f But C1-14 alkylene, which may be interrupted by one or more O or S, preferably R f But C 1-10 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 alkylene, which may be interrupted by one or more O, preferably R f But C 1-6 is alkylene, R g But hydrogen, C 1-20 alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl, preferably R g But hydrogen, C 1-10 alkyl, N-maleimidyl, or N-maleimidyloxy, preferably R g But hydrogen, C 1-6 alkyl, N-maleimidyl, X 2a But -(CH2) n and preferably X 2a But -(CH2) n -, n is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably n is 1, and preferably X 2a is -CH2-, W 1a But, -NHZ 2a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , Hydrogen, Halo, C 1-12 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a However, NHCO-Ra , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a , C 1-6 Alkyl, C 1-6 Alkylcarbonyl, and C 6-10 aryl, preferably W 1a But -NHCO-R a and preferably W 1a But -NHCO-C 1-12 alkyl, preferably W 1a But -NHCO-C 1-10 alkyl, preferably W 1a But -NHCO-C 1-8 alkyl, preferably W 1a But -NHCO-C 1-6 is alkyl, Z 2a But hydrogen, -CO-R a , C 1-10 Alkyl, C 1-10 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 2a But hydrogen, -CO-R a , C 1-8 Alkyl, C 1-8 Alkyl carbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, and C 3-6 cycloalkyl, preferably selected from the group consisting of Z 2a But hydrogen, -CO-R a, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But hydrogen, C 1-8 Alkyl, and C 1-8 alkylcarbonyl, preferably Z 2a But C 1-8 is alkylcarbonyl, Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1a is a moiety of formula (A) or (B), or is -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10Aryl, -OC 3-6 cycloalkyl, preferably Y 1a is a moiety of formula (B), or -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1a is a moiety of formula (B), or -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1a is part of formula (B), X 1b But, -NR b - and Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10 Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-6 membered heteroaryl-C 1-6 Alkylene, 3-6 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-10Alkyl, HaloC 1-6 Alkyl, C 1-10 Alkyl carbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl, 3- to 6-membered heterocyclyl-C 1-6 Alkylene, 5-6 membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene and 5-6 membered heteroaryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 3- to 6-membered heterocyclyl-C containing at least one N or one O 1-6 alkylene, 5-6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , -CO-R e -CO-OR b , -CO-R f -R g , -R f -R g , Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, C 1-8 Alkyl carbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6Cycloalkyl, 3-6 membered heterocyclyl-C containing at least one O 1-6 Alkylene, and C 6-10 Aryl-C 1-6 alkylene, preferably Z 1b But hydrogen, -CO-R a , --CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijil, Haro, C 1-8 Alkyl, HaloC 1-6 Alkyl, 3- to 5-membered heterocyclyl-C containing at least one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-6 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-R a , -CO-C 2-6 Alkenylene-CO-OR b , -CO-R f -Malaymijir, C 1-8 Alkyl, 3-4 membered heterocyclyl-C containing one O 1-6 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl, and C 2-4 alkenylcarbonyl, preferably Z 1b But hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimidyl, oxiranyl-C 1-2 Alkylene, C 1-8 Alkylcarbonyl, and C 2-4alkenylcarbonyl; X 2b But -(CH2) m and preferably X 2b But -(CH2) m -, m is an integer selected from 1, 2 or 3, preferably 1 or 2, preferably m is 1, and preferably X 2b is -CH2-, Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 2-12 Alkenyl, -OC 2-12 Alkynyl, -OC 6-10 Aryl, 3-10 membered-O-heterocyclyl, 5-10 membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5-10 membered heteroaryl-C 1-6 Alkylene-O-, 3- to 10-membered heterocyclyl-C 1-6 Alkylene-O- and C 3-6 Cycloalkyl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12 Alkyl, -NH-CO-C 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 alkylene-O-, preferably Y 1b However, -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 cycloalkyl, preferably Y1b However, -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 alkyl, preferably Y 1b However, -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 alkyl, preferably Y 1b But, -OC 1-10 Alkyl, or -NH-C 1-10 15. The compound according to any one of statements 3 to 14, wherein:

[0106] 16. Having the structural formula (IIB1) or (IIA1a): [ka] In the formula, Z 1a , X 1a , X 2a , W 1a , Z 1b , X 1b , X 2b , Y 1a , Y 1b , R b , R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , and R 4b has the same meaning as defined in any one of statements 1 to 15.

[0107] 17. Having the structural formula (IIA12), (IIA13), (IIA14), (IIA15), (IIA16), (IIA17), (IIA18), (IIB2), (IIB3), (IIB4), (IIB5), (IIB6), (IIB7), or (IIB8), [ka] [ka] In the formula, Z1a , X 1a , X 2a , Z 2a , W 1a , Z 1b , X 1b , X 2b , Y 1a , Y 1b , R a , R b , R 1a , R 2a , R 3a , R 4a , R 1b , R 2b , R 3b , and R 4b has the same meaning as defined in any one of statements 1 to 16.

[0108] 18. Having the structural formula (IIA19) or (IIB9): [ka] In the formula, Z 1a , Z 2a , R a , Y 1b , and Z 1b has the same meaning as defined in any one of statements 1 to 17.

[0109] 19. Each R a are independently hydrogen, halo, C 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C1-6 Alkylene, and -R f1 -R g1 wherein the C is selected from the group comprising 1-20 Alkyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5-10 membered heteroaryl-C 1-6 Alkylene, 3-10 membered heterocyclyl-C 1-6 Alkylene, and C 3-6 Cycloalkyl-C 1-6 Each alkylene can be unsubstituted or can have one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , -R f1 -R g1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, and R f1 But C 1-20 alkylene, 1-20 The alkylene may be interrupted by one or more O or S, and R g1 is hydrogen or C 1-20 is alkyl, Preferably, each R a are independently hydrogen, halo, C 1-20Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, wherein the C 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-18 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 cycloalkyl, wherein the C1-18 Alkyl, C 2-16 Alkenyl, HaloC 1-6 Alkyl, C 1-10 alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclyl containing at least one N or one O, and C 5-6 Each cycloalkyl can be unsubstituted or can contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl, 1-15 Alkyl, C 2-10 Alkenyl, HaloC 1-6 Alkyl, C 1-8 Each of alkylcarbonyl, 3- to 5-membered heterocyclyl containing at least one O, and phenyl can be unsubstituted or can be substituted with one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-6 alkyl, R h is hydrogen or C 1-6 alkyl, and R a1 is hydrogen or C 1-6 alkyl, and R b1 is hydrogen or C 1-6 alkyl, and R c1 is hydrogen or C 1-6 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 alkylcarbonyl, 1-15 Alkyl, C 2-4 alkenyl, 3-4 membered heterocyclyl containing at least one O, and C 1-8 Each alkylcarbonyl can be unsubstituted or contain one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-4 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, Preferably, each R a are independently hydrogen, halo, C 1-15 Alkyl, C 2-4alkenyl, and oxiranyl, 1-15 Alkyl, C 2-4 Each of alkenyl and oxiranyl is unsubstituted or has one or more R za1 and each R za1 But independently, -COO-R h , [ka] -NR a1 R b1 , and C 1-4 alkyl, R h is hydrogen or C 1-4 alkyl, and R a1 is hydrogen or C 1-4 alkyl, and R b1 is hydrogen or C 1-4 alkyl, and R c1 is hydrogen or C 1-4 alkyl, For example, each R a are independently hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, HaloC 1-6 Alkyl, C 1-12 Alkyl carbonyl, C 6-10 aryl, 3- to 6-membered heterocyclyl containing at least one N or one O, 5- to 6-membered heteroaryl containing at least one N, and C 3-6 cycloalkyl, and preferably each R a a...

Claims

1. A compound of formula (II), 【Chemical 1】 or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, In the formula, R １ａ , R ２ａ , R ３ａ , and R ４ａ are each independently R ｚａ and Each R ｚａ are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -OR ａ , non-acylated or acylated glycosyl, non-acylated or acylated -O-glycosyl, non-acylated or acylated -NR ｂ -glycosyl, non-acylated or acylated -C-glycosyl, non-acylated or acylated -S-glycosyl, -SR ａ , -S(O)R ａ , -NR ａ R ｂ , and -NR ｂ C(O)R ａ and selected from the group comprising: Each R ａ are independently hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, and -R ｆ１ -R ｇ１ wherein each of said alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene can be unsubstituted or can be substituted with one or more R ｚａ１ and each R ｚａ１ are independently -COO-R ｈ , 【Chemistry 2】 -NR ａ１ R ｂ１ , -R ｆ１ -R ｇ１ , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl; R ｈ is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R ａ１ is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R ｂ１ is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R ｃ１ is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R ｆ１ is alkylene, said alkylene being optionally interrupted by one or more O or S; R ｇ１ is hydrogen or alkyl, Each R ｂ is independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene; X １ａ But, -NR ｂ - and Z １ａ is hydrogen, -CO-R ａ , -CO-R ｅ -CO-O-R ｂ , -CO-R ｆ -R ｇ , -R ｆ -R ｇ , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X ２ａ But, -(CR ｃ R ｄ ) ｎ -, and n is an integer selected from 1, 2, or 3; Each R ｃ and R ｄ are independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; R ｅ is selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene; R ｆ is alkylene, said alkylene being optionally interrupted by one or more O or S; R ｇ is selected from hydrogen, alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; W １ａ But, -NR ｂ Z ２ａ , -R ａ , or -OR ａ is selected from Z ２ａ is hydrogen, -CO-R ａ , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; Y １ａ But, -OR ａ , -R ａ , or -NR ａ R ｂ or Y １ａ is the part of formula (A), 【Chemistry 3】 During the ceremony, Ar ２ is aryl or heteroaryl, each of which may be unsubstituted or may be one or more R ｚｂ may be replaced by Each R ｚｂ are independently hydrogen, halo, alkyl, haloalkyl, -OR ａ , alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, cycloalkyl-alkynylene, -SR ａ , non-acylated or acylated glycosyl, non-acylated or acylated -O-glycosyl, non-acylated or acylated -NR ｂ -glycosyl, non-acylated or acylated-C-glycosyl, non-acylated or acylated-S-glycosyl, -C(O)-R ａ , -S(O)R ａ , -NR ａ R ｂ , and -NR ｂ C(O)R ａ and selected from the group comprising: X １ｂ But, -NR ｂ -, -O-, -S-, SO ２ -O-, or -SO-O-; Z １ｂ is hydrogen, -CO-R ａ , -CO-R ｅ -CO-O-R ｂ , -CO-R ｆ -R ｇ , -R ｆ -R ｇ , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, aryl-alkenylene, aryl-alkynylene, heteroaryl-alkylene, heteroaryl-alkenylene, heteroaryl-alkynylene, heterocyclyl-alkylene, heterocyclyl-alkenylene, heterocyclyl-alkynylene, cycloalkyl-alkylene, cycloalkyl-alkenylene, and cycloalkyl-alkynylene; X ２ｂ But, -(CR ｃ R ｄ ) ｍ - and m is an integer selected from 1, 2, or 3; Y １ｂ But, -OR ａ , -NR ｂ R ａ , or -R ａ is selected from However, the compound is 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid, 4-(2-acetamidophenyl)-2-amino-4-oxobutanoic acid, 2-acetamido-4-(2-aminophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-amino-4-oxo-4-(2-(((3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, (2S)-2-amino-4-oxo-4-(2-(((3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)amino)phenyl)butanoic acid, (S)-2-amino-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (S)-2-acetamido-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (R)-2-acetamido-4-(2-amino-3-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-triyl triacetate, 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid, 5-(2-aminophenyl)-5-oxopentanoic acid, 4-(2-aminophenyl)-4-oxobutanoic acid, methyl 6-(2-aminophenyl)-6-oxohexanoate, methyl 4-(2-aminophenyl)-2-((tert-butoxycarbonyl)amino)-4-oxobutanoate, butyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate, ethyl (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoate, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid diacetate, (R)-2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, 2-amino-4-(2-formamidophenyl)-4-oxobutanoic acid, methyl 2-acetamido-4-(2-acetamidophenyl)-4-oxobutanoate, 4-(2-amino-3-(((2R,3S,4R,5R,6S)-3,4,5-trihydroxy-6-((((2S,3S,4R,5R,6S)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)methyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-D-diglucoside), 4-(2-amino-3-(((2R,3S,4R,5R,6S)-3,4-5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid, 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-d-glucoside, 2-amino-4-(2-formamido-5-hydroxyphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid, 2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid, 2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, (R)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, (S)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid, 2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (R)-2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, (S)-2-acetamido-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid, 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, (S-) 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, (R-) 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid, methyl (S-)2-amino-4-(2-aminophenyl)-4-oxobutanoate, 2-amino-4-(2-aminophenyl)-4-oxobutanamide, (R)-2-amino-4-(2-aminophenyl)-4-oxobutanamide, (S)-2-amino-4-(2-aminophenyl)-4-oxobutanamide, (S)-2-acetamido-4-(2-acetamidophenyl)-4-oxobutanoic acid, (S)-2-formamido-4-(2-formamidophenyl)-4-oxobutanoic acid, 4-(2-aminophenyl)-4-oxo-2-phenylbutanamide, or a tautomer, stereoisomer, hydrate, solvate, salt, or polymorph thereof, provided that the compound is not 4-(2-aminophenyl)-4-oxo-2-phenylbutanamide.

2. Y １ａ is a moiety of formula (A), or -OR ａ , -R ａ , or -NR ａ R ｂ is selected from Ar ２ But C ６－１０ aryl or 5-6 membered heteroaryl, preferably containing at least one N, each of said aryl or heteroaryl may be unsubstituted or may contain one or more R ｚｂ may be replaced by In the formula, R ｚａ , R ｚｂ , R ａ , R ｂ has the same meaning as defined in claim 1.

3. Y １ａ is a moiety of formula (B), or OR ａ , R ａ , N.R. ａ R ｂ is selected from 【Chemistry 4】 In the formula, R １ａ , R ２ａ , R ３ａ , and R ４ａ are each independently R ｚａ and R １ｂ , R ２ｂ , R ３ｂ , and R ４ｂ are each independently R ｚｂ and Z １ａ , X １ａ , X ２ａ , W １ａ , Z １ｂ , X １ｂ , X ２ｂ , Y １ｂ , R ｂ , R ｚａ , and R ｚｂ 3. A compound according to claim 1 or 2, wherein has the same meaning as defined in claim 1.

4. Each R ａ are independently hydrogen, halo, C １－２０ Alkyl, haloC １－６ Alkyl, C １－１２ Alkylcarbonyl, C ２－２０ Alkenyl, C ２－１２ Alkynyl, C ６－１０ aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C ３－６ Cycloalkyl, C ６－１０ Aryl-C １－６ alkylene, 5- to 10-membered heteroaryl-C １－６ alkylene, 3- to 10-membered heterocyclyl-C １－６ Alkylene, and C ３－６ Cycloalkyl-C １－６ alkylene, and -R ｆ１ -R ｇ１ wherein said C is selected from the group comprising １－２０ Alkyl, haloC １－６ Alkyl, C １－１２ Alkylcarbonyl, C ２－２０ Alkenyl, C ２－１２ Alkynyl, C ６－１０ aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C ３－６ Cycloalkyl, C ６－１０ Aryl-C １－６ alkylene, 5- to 10-membered heteroaryl-C １－６ alkylene, 3- to 10-membered heterocyclyl-C １－６ Alkylene, and C ３－６ Cycloalkyl-C １－６ Each alkylene can be unsubstituted or can contain one or more R ｚａ１ and each R ｚａ１ are independently -COO-R ｈ , 【Chemistry 5】 -NR ａ１ R ｂ１ , -R ｆ１ -R ｇ１ , Haro, C １－６ Alkyl, haloC １－６ Alkyl, C １－６ Alkylcarbonyl, C ２－６ Alkenyl, and C ２－６ alkynyl, and R ｈ But hydrogen, C １－６ Alkyl, C ２－６ Alkenyl, and C ２－６ alkynyl, and R ａ１ But hydrogen, C １－６ Alkyl, C ２－６ Alkenyl, and C ２－６ alkynyl, and R ｂ１ But hydrogen, C １－６ Alkyl, C ２－６ Alkenyl, and C ２－６ alkynyl, and R ｃ１ But hydrogen, C １－６ Alkyl, C ２－６ Alkenyl, and C ２－６ alkynyl, R ｆ１ But C １－２０ alkylene, １－２０ The alkylene may be interrupted by one or more O or S; R ｇ１ is hydrogen or C １－２０ is alkyl, Each R ｂ are independently hydrogen, halo, C １－６ Alkyl, haloC １－６ Alkyl, C １－６ Alkylcarbonyl, C ６－１０ Aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, and C ３－６ is selected from the group including cycloalkyl, X １ａ But, -NR ｂ - and Z １ａ is hydrogen, -CO-R ａ , -CO-R ｅ -CO-O-R ｂ , -CO-R ｆ -R ｇ , -R ｆ -R ｇ , Haro, C １－１２ Alkyl, haloC １－６ Alkyl, C １－１２ Alkylcarbonyl, C ２－１２ Alkenyl, C ２－１２ Alkynyl, C ６－１０ aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C ３－６ Cycloalkyl, C ６－１０ Aryl-C １－６ alkylene, 5- to 10-membered heteroaryl-C １－６ alkylene, 3- to 10-membered heterocyclyl-C １－６ Alkylene, and C ３－６ Cycloalkyl-C １－６ selected from the group including alkylene; R ｅ But C １－１２ Alkylene, C ２－１２ Alkenylene, C ２－１２ Alkynylene, C ６－１０ arylene, 5- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene, and C ３－６ is selected from the group comprising cycloalkylene; R ｆ But C １－２０ alkylene, which may be interrupted by one or more O or S; R ｇ is selected from hydrogen, alkyl, N-maleimidyl, N-maleimidyloxy, or N-maleimidyloxycarbonyl; X ２ａ But, -(CR ｃ H) ｎ -, and n is an integer selected from 1, 2, or 3; Each R ｃ are independently hydrogen, halo, C １－６ Alkyl, haloC １－６ Alkyl, C ６－１０ aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C ３－６ Cycloalkyl, C ６－１０ Aryl-C １－６ alkylene, 5- to 10-membered heteroaryl-C １－６ alkylene, 3- to 10-membered heterocyclyl-C １－６ Alkylene, and C ３－６ Cycloalkyl-C １－６ selected from the group including alkylene; W １ａ But, -NR ｂ Z ２ａ or -R ａ is selected from Z ２ａ is hydrogen, -CO-R ａ , Haro, C １－１２ Alkyl, haloC １－６ Alkyl, C １－１２ Alkylcarbonyl, C ６－１０ aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C ３－６ Cycloalkyl, C ６－１０ Aryl-C １－６ alkylene, 5- to 10-membered heteroaryl-C １－６ alkylene, 3- to 10-membered heterocyclyl-C １－６ Alkylene, and C ３－６ Cycloalkyl-C １－６ selected from the group including alkylene; Y １ａ is a moiety of formula (A) or (B), or -OR ａ Or -NHR ａ and X １ｂ But, -NR ｂ - or -O-, preferably X １ｂ But, -NR ｂ - and Z １ｂ is hydrogen, -CO-R ａ , -CO-R ｅ -CO-O-R ｂ , -CO-R ｆ -R ｇ , -R ｆ -R ｇ , Haro, C １－１２ Alkyl, haloC １－６ Alkyl, C １－１２ Alkylcarbonyl, C ２－１２ Alkenyl, C ２－１２ Alkynyl, C ６－１０ aryl, 3- to 10-membered heterocyclyl, 5- to 10-membered heteroaryl, C ３－６ Cycloalkyl, C ６－１０ Aryl-C １－６ alkylene, 5- to 10-membered heteroaryl-C １－６ alkylene, 3- to 10-membered heterocyclyl-C １－６ Alkylene, and C ３－６ Cycloalkyl-C １－６ selected from the group including alkylene; X ２ｂ But, -(CR ｃ H) ｍ - and m is an integer selected from 1, 2, or 3; Y １ｂ But, -OR ａ or -NHR ａ The compound according to any one of claims 1 to 3,

5. having the structural formula (IIA12), (IIA13), (IIA14), (IIA15), (IIA16), (IIA17), (IIA18), (IIB1), (IIB2), (IIB3), (IIB4), (IIB5), (IIB6), (IIB7), or (IIB8); 【Chemistry 6】 【Chemistry 7】 During the ceremony, Z １ａ , X １ａ , X ２ａ , W １ａ , Z １ｂ , X １ｂ , X ２ｂ , Y １ａ , Y １ｂ , R ａ , R ｂ , R １ａ , R ２ａ , R ３ａ , R ４ａ , R １ｂ , R ２ｂ , R ３ｂ , R ４ｂ has the same meaning as defined in any one of claims 1 to 4.

6. 【Chemical 8】 【Chemistry 9】 【Chemistry 10】 【Chemistry 11】 【Chemistry 12】 【Chemistry 13】 A compound selected from the group comprising:

7. A cosmetic or pharmaceutical composition comprising at least one compound according to any one of claims 1 to 6 and, optionally, at least one dermatologically or pharmaceutically acceptable carrier.

8. Non-therapeutic use of at least one compound according to any one of claims 1 to 6 or at least one cosmetic composition according to claim 7 as an ultraviolet absorbing filter and / or a high-energy visible light filter.

9. A compound according to any one of claims 1 to 6 or at least one pharmaceutical composition according to claim 7 for use as an ultraviolet absorbing filter and / or a high energy visible light filter.

10. Non-therapeutic use of at least one compound according to any one of claims 1 to 6 or at least one cosmetic composition according to claim 7 for protection against ultraviolet and high-energy visible radiation.

11. A compound according to any one of claims 1 to 6 or at least one pharmaceutical composition according to claim 7, for use in protecting against ultraviolet and high-energy visible radiation.

12. Use of at least one compound according to any one of claims 1 to 6 in a consumer product as a light stabilizer for protecting ingredients from photodegradation.

13. 10. Non-therapeutic use of at least one compound according to any one of claims 1 to 6 or at least one cosmetic composition according to claim 7 as an ultraviolet and / or high-energy visible light absorbing filter in a consumer product, preferably a cosmetic product.

14. A compound according to any one of claims 1 to 6 or at least one pharmaceutical composition according to claim 7 for use as an ultraviolet and / or high energy visible light absorbing filter in consumer products, preferably cosmetics.

15. A consumer product comprising at least one compound according to any one of claims 1 to 6.

16. 16. The consumer product of claim 15, wherein the consumer product is a cosmetic product, preferably the cosmetic product is selected from the group comprising sunscreens, moisturizers, make-up products, lip protectants, shampoos, and conditioners.

17. Use of at least one compound according to any one of claims 1 to 6 as an antioxidant.

18. Use of at least one compound according to any one of claims 1 to 6 as an ultraviolet and / or high-energy visible light absorbing filter in packaging.

19. Packaging material comprising at least one compound according to any one of claims 1 to 6.

20. 10. A method for protecting a substrate from ultraviolet and / or high-energy visible radiation, comprising applying onto the substrate at least one compound according to any one of claims 1 to 6, or the cosmetic or pharmaceutical composition according to claim 7.

21. 10. A method for protecting skin from ultraviolet and / or high-energy visible radiation, comprising the step of applying to the skin at least one compound according to any one of claims 1 to 6, or a cosmetic or pharmaceutical composition according to claim 7.

22. 10. A method for protecting a composition from oxidation or imparting antioxidant properties to a composition, comprising adding to said composition at least one compound according to any one of claims 1 to 6.

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