Compound and application thereof in filtering ultraviolet rays and / or high-energy visible light

Abstract

The invention provides a compound of formula (II) or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein Z1a, X1a, Ar1, X2a, W1a, Y1a, R1a, R2a, R3a and R4a have the same meaning as the meanings defined in the description and the claims. The invention also provides these compounds for filtering ultraviolet (UV) and high energy visible light. The invention also relates to compositions comprising said compounds. The invention also relates to consumer products and packaging materials comprising said compounds. # imgabs0 #

Description

Technical Field

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

[0002] High-energy light from the sun and artificial light sources, such as UV light and high-energy visible light, is known to cause cellular damage. This light ranges primarily from 290-320 nm (UVB), 320-400 nm (UVA), and 400-450 nm (HEV). Photons within this energy range can be absorbed by many biological, pharmaceutical, and cosmetic molecules, causing direct photodegradation or transferring the energy to oxygen, triggering a cascade of oxidative reactions. In living tissue, UV and high-energy visible light can damage key 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 UV and high-energy visible light can also degrade key pharmaceutical ingredients, such as the sunscreen active ingredient avobenzone, which typically requires photostabilizers to maintain its UVA protection. Foods are also susceptible to damage from UV and high-energy visible light, particularly unsaturated fatty acids such as olive oil and the essential amino acid tryptophan in proteins, which are susceptible to oxidation by photoexcited molecules and oxygen.

[0003] Therefore, molecules that absorb UV and high-energy visible light and dissipate this energy as energy are highly desirable. Such filters are particularly useful if they are: photostable, allowing them to be used more economically; low fluorescence, allowing them to dissipate most of their energy as energy; fully biodegradable, allowing them to not persist in the environment or tissues; and poorly absorbed through the skin, allowing them to remain on the surface to provide protection and prevent significant tissue mobility via biodegradation pathways. Many UV filters currently approved for use as sunscreen actives in the United States fail one or more of these tests, remaining in the environment as unchanged or stable xenobiotic degradation products that are also readily absorbed through the skin and accumulate in serum. These sunscreen actives also show disturbing evidence that they effectively mimic hormones in tissues and cause environmental damage to sensitive marine ecosystems.

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

[0005] The present invention relates to a compound of formula (I):

[0006]

[0007] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0008] Ar 1 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R za replace;

[0009] Each R za 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0010] 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; wherein said alkyl, said haloalkyl, said alkylcarbonyl, said Each of the alkenyl, the alkynyl, the aryl, the heterocyclyl, the heteroaryl, the cycloalkyl, the aryl-alkylene, the aryl-alkenylene, the aryl-alkynylene, the heteroaryl-alkylene, the heteroaryl-alkenylene, the heteroaryl-alkynylene, the heterocyclyl-alkylene, the heterocyclyl-alkenylene, the heterocyclyl-alkynylene, the cycloalkyl-alkylene, the cycloalkyl-alkenylene and the cycloalkyl-alkynylene may be unsubstituted or substituted with one or more R za1 Replace; wherein each Rza1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl;

[0011] R h selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0012] R a1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0013] R b1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0014] R c1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0015] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0016] X 1a Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0017] Z 1a Selected from the group consisting of 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;

[0018] X 2a For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3;

[0019] Each R c and Rd 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;

[0020] R e selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0021] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0022] R g Selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0023] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0024] Z 2a Selected from the group consisting of 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;

[0025] Y 1a Select from -OR a 、-R a or -NR a R b , or Y 1a is a moiety having formula (A);

[0026]

[0027] in

[0028] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0029] Each Rzb are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0030] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0031] Z 1b Selected from the group consisting of: 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;

[0032] X 2b For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; and

[0033] Y 1b Select from -OR a 、-NR b R a or -R a ;

[0034] The condition is

[0035] no and

[0036] Provided that the compound is not:

[0037] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0038] 4-(2-Acetylaminophenyl)-2-amino-4-oxobutanoic acid;

[0039] 2-Acetylamino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0040] (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;

[0041] (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);

[0042] 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;

[0043] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid methyl ester;

[0044] 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0045] 2-Acetylamino-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0046] (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-acetyl triacetate;

[0047] 2-Amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid.

[0048] In some embodiments, the present invention relates to a compound of formula (I):

[0049]

[0050] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0051] Ar 1 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R za replace;

[0052] Each R za 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0053] Each R a 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;

[0054] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0055] X 1a Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0056] Z 1a Selected from the group consisting of 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;

[0057] X 2a For-(CR c R d ) n -; n is an integer selected from 1, 2 or 3;

[0058] Each R c and R d 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;

[0059] R e selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0060] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0061] R g Selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0062] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0063] Z 2a Selected from the group consisting of 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;

[0064] Y 1a is a moiety having formula (A), or Y 1a Select from -OR a 、-R a or -NR a R b ;

[0065]

[0066] in

[0067] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0068] Each R zb are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0069] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0070] Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-Re -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;

[0071] X 2b For-(CR c R d ) m -; m is an integer selected from 1, 2 or 3; and

[0072] Y 1b Select from -OR a 、-NR b R a or -R a ;

[0073] Provided that the compound is not:

[0074] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0075] 4-(2-Acetylaminophenyl)-2-amino-4-oxobutanoic acid;

[0076] 2-Acetylamino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0077] (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;

[0078] 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

[0079] Methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate.

[0080] In some embodiments, the present invention relates to a compound of formula (II):

[0081]

[0082] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0083] R 1a 、R 2a 、R 3a and R 4a Each independently is R za ;

[0084] Each R za 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0085] 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, cycloalkyl-alkynylene, and -R f1 -R g1 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 may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h、 -NR a1 R b1 、-R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl and alkynyl; wherein 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 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0086] R f1 is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0087] R g1 is hydrogen or alkyl;

[0088] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0089] X 1a -NR b -;

[0090] Z 1a Selected from the group consisting of 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;

[0091] X 2a For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3;

[0092] Each R c and R dindependently 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;

[0093] R e selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0094] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0095] R g is selected from hydrogen, alkyl, N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0096] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0097] Z 2a Selected from the group consisting of 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;

[0098] Y 1a Select from -OR a 、-R a or -NR a R b , or Y 1a is a moiety having formula (A);

[0099]

[0100] in

[0101] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0102] Each Rzb are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0103] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0104] Z 1b Selected from the group consisting of: 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;

[0105] X 2b For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; and

[0106] Y 1b Select from -OR a 、-NR b R a or -R a ;

[0107] Provided that the compound is not:

[0108] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0109] (R)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0110] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0111] 4-(2-Acetylaminophenyl)-2-amino-4-oxobutanoic acid;

[0112] 2-Acetylamino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0113] (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;

[0114] 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;

[0115] (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;

[0116] (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;

[0117] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid methyl ester;

[0118] 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0119] 2-Acetylamino-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0120] (S)-2-Acetylamino-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;

[0121] (R)-2-Acetylamino-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;

[0122] (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-acetyl triacetate;

[0123] 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0124] (S)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0125] (R)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0126] 5-(2-aminophenyl)-5-oxopentanoic acid;

[0127] 4-(2-aminophenyl)-4-oxobutanoic acid;

[0128] Methyl 6-(2-aminophenyl)-6-oxohexanoate;

[0129] Methyl 4-(2-aminophenyl)-2-((tert-butoxycarbonyl)amino)-4-oxobutanoate;

[0130] Butyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate;

[0131] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid ethyl ester;

[0132] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid diacetate;

[0133] (R)-2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0134] (S)-2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0135] 2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0136] 2-Acetylamino-4-(2-acetylaminophenyl)-4-oxobutanoic acid methyl ester;

[0137] 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;

[0138] 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-D-bioside); 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;

[0139] 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-d-glycoside;

[0140] 2-amino-4-(2-formylamino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0141] 2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid;

[0142] (R)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid;

[0143] (S)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid;

[0144] 2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid;

[0145] (R)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid;

[0146] (S)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid;

[0147] 2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid;

[0148] (R)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid;

[0149] (S)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid;

[0150] 2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid;

[0151] (R)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid;

[0152] (S)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid;

[0153] 2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid;

[0154] (R)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid;

[0155] (S)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid;

[0156] 2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid;

[0157] (R)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid;

[0158] (S)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid;

[0159] 2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid;

[0160] (R)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid;

[0161] (S)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid;

[0162] 2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid;

[0163] (R)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid;

[0164] (S)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid;

[0165] 2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid;

[0166] (R)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid;

[0167] (S)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid;

[0168] 2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid;

[0169] (S)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid;

[0170] (R)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid;

[0171] 2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid;

[0172] (S)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid;

[0173] (R)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid;

[0174] 2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0175] (R)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0176] (S)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0177] 2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid;

[0178] (R)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid;

[0179] (S)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid;

[0180] 2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0181] (R)-2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0182] (S)-2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0183] 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid;

[0184] (S-)2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid;

[0185] (R-)2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid;

[0186] (S-)methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate;

[0187] 2-amino-4-(2-aminophenyl)-4-oxobutanamide;

[0188] (R)-2-amino-4-(2-aminophenyl)-4-oxobutanamide;

[0189] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanamide;

[0190] (S)-2-Acetylamino-4-(2-acetylaminophenyl)-4-oxobutanoic acid;

[0191] (S)-2-Formylamino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0192] 4-(2-Aminophenyl)-4-oxo-2-phenylbutanamide.

[0193] The 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.

[0194] The present invention is based on the unexpected discovery that the compounds described herein are compounds that absorb UV and / or high-energy visible light. These compounds may be particularly useful for filtering UV and / or high-energy visible light. These compounds may be particularly useful for dissipating this energy into heat, specifically absorbing UV light from solar radiation on the skin, which would otherwise penetrate into living tissue and cause cell damage, leading to cancer, erythema, and accelerated aging. These compounds may also be used to protect body parts from UV damage. Therefore, these compounds may be used to prevent cancer, erythema, and / or accelerated aging.

[0195] The compounds can also be used for light protection of hair, food, plants, and for making light protection materials (such as food packaging plastics). The compounds can also be used in food packaging to protect food from UV and / or high energy visible radiation damage.

[0196] The compounds can absorb UV and / or high-energy visible light and can be used to prevent photodegradation of ingredients such as pharmaceuticals and cosmetic ingredients. The compounds can also be used to prevent color spots caused by absorption of high-energy visible light.

[0197] In some embodiments, the compound has the additional advantage of being biodegradable, having a high extinction coefficient, high photostability, low fluorescence, and low singlet oxygen production, and having the advantage of not being easily absorbed through the skin.

[0198] In some embodiments, the compounds herein may function as antioxidants and may also be effective in preventing damage from hydroxyl radicals that may be formed due to pollution and UV radiation.

[0199] The present invention therefore also relates to the use of at least one compound according to the invention as UV-absorbing filter and / or high-energy visible light filter.

[0200] The present invention furthermore relates to the use of at least one compound according to the invention for protection against UV and / or high-energy visible radiation.

[0201] The compounds are useful for photoprotection in pharmaceutical and cosmetic formulations, such as cosmetic skin formulations.

[0202] The present invention also relates to the use of at least one compound according to the invention as light stabilizer for protecting ingredients against photolytic degradation.

[0203] The present invention also relates to the use of at least one compound according to the invention as UV and / or high-energy visible light absorbing filter in consumer products or in packaging.

[0204] The present invention also encompasses a consumer product comprising at least one compound according to the invention.

[0205] The present invention also encompasses a packaging material comprising at least one compound according to the invention.

[0206] The above and other characteristics, features and advantages of the present invention will be apparent from the following detailed description, which illustrates, by way of example, the principles of the invention. BRIEF DESCRIPTION OF THE DRAWINGS

[0207] Figure 1 is a line graph showing the absorbance spectrum of compound 1. It shows that absorbance is still present up to 410 nm, and thus it can be used to provide high-energy visible light protection.

[0208] Figure 2 is a line graph showing the absorbance spectrum of Compound 2. The figure shows strong absorbance in the UVB region.

[0209] Figure 3 is a line graph showing the combined absorbance spectra of compounds 1 and 2. The absorbance spectra of these two compounds can be combined to provide broad spectrum UVB and UVA protection.

[0210] Figure 4 It is a line graph showing the absorbance spectrum of compound 4.

[0211] Figure 5is a line graph showing the absorbance spectrum of Compound 5.

[0212] Figure 6 is a line graph showing the hydroxyl radical antioxidant capacity (HORAC) test of compound 4.

[0213] Figure 7 It is a line graph showing the absorbance spectrum of compound 42.

[0214] Figure 8 It is a line graph showing the absorbance spectrum of compound 43.

[0215] Figure 9 It is a line graph showing the absorbance spectrum of compound 44.

[0216] Figure 10 It is a line graph showing the absorbance spectrum of compound 45.

[0217] Figure 11 It is a line graph showing the absorbance spectrum of compound 46.

[0218] Figure 12 It is a line graph showing the absorbance spectrum of Compound 6.

[0219] Figure 13 is a line graph showing the absorbance spectrum of compound 47.

[0220] Figure 14 It is a line graph showing the absorbance spectrum of compound 48.

[0221] Figure 15 It is a line graph showing the absorbance spectrum of compound 49.

[0222] Figure 16 It is a line graph showing the absorbance spectrum of compound 50.

[0223] Figure 17 are photographs showing the protective effect of compound 42 against skin damage caused by UV. DETAILED DESCRIPTION

[0224] When describing the present invention, the terms used are to be interpreted in accordance with the following definitions, unless the context indicates otherwise.

[0225] Unless otherwise defined, all terms (including technical and scientific terms) used in disclosing the present invention have the meaning commonly understood by those of ordinary skill in the art to which the invention belongs. For further guidance, definitions of terms used in the specification 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 will be interpreted according to the following definitions unless the context indicates otherwise.

[0226] 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.

[0227] In the following paragraphs, different aspects of the present invention are defined in more detail. Unless clearly indicated to the contrary, each aspect so defined can be combined with any one or more other aspects. Specifically, any feature indicated as preferred or advantageous can be combined with any one or more other features indicated as preferred or advantageous.

[0228] As used herein, the terms "comprising," "comprises," and "comprised of" are synonymous with "including," "includes," or "containing," "contains," and are inclusive or open-ended and do not exclude additional, unrecited members, elements, or method steps. The terms "comprising," "comprises," and "comprised of" also encompass the term "consisting of."

[0229] The recitation of numerical ranges by endpoints includes all integers and, where appropriate, fractions within the range (e.g., 1 to 5 when referring to, for example, a plurality of elements, may include 1, 2, 3, 4, and when referring to, for example, a measurement result, may also 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 range recited herein is intended to include all subranges subsumed therein.

[0230] The term "about" is used herein to mean approximately, roughly, around, or in the region thereof. When the term "about" is used in conjunction with a numerical range, the term modifies the range by extending the boundaries above and below the stated numerical values. Generally, the term "about" is used herein to modify the numerical value above and below the stated value by a variation of 10% above or below (higher or lower).

[0231] As used herein, the term "and / or" should be understood as explicitly disclosing each of the two specified features or components with or without the other. Thus, the term "and / or" as used herein in phrases such as "A and / or B" is intended to include "A and B," "A or B," "A" (alone), and "B" (alone). Similarly, the term "and / or" as used in phrases such as "A, B, and / or C" is intended to cover each of the following: 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).

[0232] Throughout this specification, references to "one embodiment" or "an embodiment" mean that a particular feature, structure, or characteristic described in connection with the embodiment is included in at least one embodiment of the present invention. Thus, the appearances of the phrases "in one embodiment" or "in an embodiment" in various places throughout this specification do not necessarily all refer to the same embodiment, but may refer to the same embodiment. Furthermore, in one or more embodiments, the particular features, structures, or characteristics may be combined in any suitable manner, as will be apparent to those skilled in the art from this disclosure. Furthermore, while some embodiments described herein include some features and not others included in other embodiments, as will be appreciated by those skilled in the art, combinations of features from different embodiments are intended to be within the scope of the present invention and to form different embodiments. For example, in the claims and statements that follow, any of the embodiments described may be used in any combination.

[0233] Whenever the term "substituted" is used herein, it is meant to indicate that one or more hydrogen atoms on the indicated atom in the expression using "substituted" are replaced with a selection from the indicated group, provided that the normal valency of the indicated atom is not exceeded and that the substitution results in a chemically stable compound, i.e., a compound that is sufficiently stable to survive isolation from a reaction mixture.

[0234] The term "halo" or "halogen" as a group or part of a group refers generally to fluorine, chlorine, bromine, iodine.

[0235] As used herein, the term "hydroxy" or "hydroxyl" refers to the group -OH.

[0236] As used herein, the term "thio" or "thiol" refers to the group -SH.

[0237] The term "alkyl" as a group or part of a group refers to a group of formula C n H 2n+1wherein n is a number greater than or equal to 1, and has no sites of unsaturation. Alkyl groups may be straight or branched and may be substituted as indicated herein. In general, alkyl groups in the present invention contain from 1 to 20 carbon atoms, preferably from 1 to 10 carbon atoms, more preferably from 1 to 6 carbon atoms, and more preferably from 1 to 4 carbon atoms. When a subscript is used after a carbon atom in this document, the subscript refers to the number of carbon atoms that the named group may contain. For example, the term "C" as a group or part of a group 1-20 "Alkyl" refers to a group of formula C n H 2n+1 wherein 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, isopropyl, butyl and isomers thereof (e.g., n-butyl, isobutyl and tert-butyl); pentyl and isomers thereof, hexyl and isomers thereof, etc. 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, isopropyl, 2-methyl-ethyl, butyl and isomers thereof (e.g., n-butyl, isobutyl and tert-butyl), etc. In specific embodiments, the term alkyl refers to C 1-12 Alkyl (C 1-12 hydrocarbons), but more specifically C 1-9 Alkyl (C 1-9 hydrocarbons), but more specifically C 1-6 Alkyl (C 1-6 Non-limiting examples of alkyl groups include methyl, ethyl, 1-propyl (n-propyl), 2-propyl (iPr), 1-butyl, 2-methyl-1-propyl ( i 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-eicosyl.

[0238] When the suffix "ene" is used with an alkyl group, i.e., "alkylene," it means that the alkyl group, as defined herein, has two single bonds as points of attachment to other groups. As used herein, the term "alkylene," also known as "alkanediyl," by itself or as part of another substituent, refers to a divalent, i.e., an alkyl group having two monovalent radical centers derived by removing two hydrogen atoms from the same or two different carbon atoms of a parent alkane, i.e., having two single bonds for attachment to two other groups. An alkylene group may be straight or branched and may be substituted as described 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-butene (-CH2-CH2-CH2-CH2-), 2-methylbutene (-CH2-CH(CH3)-CH2-CH2-), 4-methylbutene (-CH2-CH2-CH2-CH(CH3)-), pentene and its chain isomers, hexene and its chain isomers.

[0239] The term "hydrocarbyl" is used herein according to the definition assigned by IUPAC: a univalent group formed by removing a hydrogen atom from a hydrocarbon (ie, a group containing only carbon and hydrogen).

[0240] The term "alkenyl" as a group or part of a group refers to an unsaturated hydrocarbon group which may be linear or branched and contains one or more, at least one site of unsaturation (usually 1 to 3, preferably 1), i.e. at least one sp 2 Carbon-sp 2 In general, the alkenyl groups of the present 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 after a carbon atom herein, 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 can be in cis or trans configuration.

[0241] When the suffix "ene" is used together with alkenyl, i.e. "alkenylene", it means that the alkenyl defined herein has two single bonds as the connection point with other groups. As used herein, the term "alkenylene" itself or as a part of another substituent refers to divalence, i.e. the alkenyl with two monovalent group centers, which are obtained by removing two hydrogen atoms from the same or two different carbon atoms of the parent alkene, i.e. having two single bonds for being connected to two other groups. Alkenylene can be straight or branched, and can be substituted as described herein. The non-limiting examples of alkenylene include-CH=CH- ,-C (CH )=CH- ,-C (CH )=C (CH )- ,-CH=CH-CH 2 - ,-CH 2 -C (CH )=CH- ,-CH 2 -CH=C (CH )- ,-CH 2 -CH 2=CH- etc.

[0242] The term "alkynyl" as a group or part of a group refers to a branched or straight chain hydrocarbon containing at least one site of unsaturation (usually 1 to 3, preferably 1), i.e., sp 1 Carbon-sp 1 In particular embodiments, the term alkynyl refers to a C 2-12 Alkynyl (C 2-12 Hydrocarbon), preferably C 2-9 Alkynyl (C 2-9 hydrocarbons), but more preferably refers to C 2-6 Alkynyl (C 2-6 hydrocarbons), as further defined above, having at least one site of unsaturation (typically 1 to 3, preferably 1), i.e. at least one sp 1 Carbon-sp 1 Examples of alkynyl groups include, but are not limited to, ethynyl (-C≡CH), 3-ethyl-cycloheptan-1-ynyl, and 1-propynyl (propargyl, -CH2C≡CH).

[0243] When the suffix "ene" is used with an alkynyl group, i.e., "alkynylene", it means that the alkynyl group as defined herein has 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 a divalent, i.e., alkynyl group having two single bonds for connecting two other groups. Alkynylenes can be straight or branched and can be substituted as described herein. Non-limiting examples of alkynylenes include -C≡C-, -CH2-C≡C-, -C≡C-CH2-, -CH2-CH2-C≡C-, etc.

[0244] The term "cycloalkyl" as a group or part of a group refers to a cyclic alkyl group, i.e., a monovalent saturated hydrocarbon group having one or more ring structures and containing 3 to 20 carbon atoms, more preferably 3 to 10 carbon atoms, more preferably 3 to 8 carbon atoms; more preferably 3 to 6 carbon atoms. Cycloalkyl groups include all saturated hydrocarbon groups containing one or more rings, including monocyclic, bicyclic or tricyclic rings. For example, a cycloalkyl group containing C 3-10 Monocyclic or C 7-18 Polycyclic saturated hydrocarbons such as cyclopropyl, cyclobutyl, cyclopentyl, cyclopropylethylene, methylcyclopropene, cyclohexyl, cycloheptyl, cyclooctyl, cyclooctylmethylene, norbornyl, fenchyl, trimethyltricycloheptyl, decalinyl, adamantyl, etc. The additional rings of the polycyclic cycloalkyl may be fused, bridged, and / or joined by one or more spiro atoms. When a subscript is used after a carbon atom in this document, the subscript refers to the number of carbon atoms that the named group may contain. For example, the term "C 3-10 "Cycloalkyl" refers to a cyclic alkyl group containing 3 to 10 carbon atoms. For example, the term "C 3-8 "Cycloalkyl" refers to a cyclic alkyl group containing 3 to 8 carbon atoms. For example, the term "C 3-6 "Cycloalkyl" refers to a cyclic alkyl group containing 3 to 6 carbon atoms. For the avoidance of doubt, a cycloalkyl ring-heterocyclic ring fused system is considered to be a heterocyclic ring, regardless of the ring bound to the core structure. A cycloalkyl ring-aryl ring fused system is considered to be an aryl ring, regardless of the ring bound to the core structure. A cycloalkyl ring-heteroaryl ring fused system is considered to be a heteroaryl ring, regardless of the ring bound to the core structure.

[0245] The term "cycloalkylalkylene" or "cycloalkyl-alkylene" as a group or part of a group refers to a group of formula R z R y A group in which R z is a cycloalkyl group, and R y is an alkylene group as defined herein.

[0246] The term "alkoxy" or "alkyloxy" as a group or part of a group refers to a radical of the formula -OR x A group in which R x is an alkyl group as defined herein. Suitable C 1-6 Non-limiting examples of alkoxy groups include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, sec-butoxy, tert-butoxy, pentyloxy, and hexyloxy.

[0247] The term "alkenyloxy" as a group or part of a group refers to a group of the formula -OR w A group in which R w is alkenyl as defined herein.

[0248] The term "alkynyloxy" as a group or part of a group refers to a group of the formula -OR v A group in which R v is an alkynyl group as defined herein.

[0249] The term "aryl" as a group or part of a group refers to a polyunsaturated aromatic hydrocarbon group having a single ring (i.e., phenyl) or multiple aromatic rings fused together or covalently linked (e.g., naphthyl), typically containing 6 to 20 atoms; preferably 6 to 10, at least one of which is aromatic. Typical aryl groups include, but are not limited to, one ring or two or three rings fused together derived from benzene, naphthalene, anthracene, biphenyl, etc. The aromatic rings may optionally include one to two additional rings. A fused system of an aryl ring with a cycloalkyl ring, a cycloalkenyl ring, or a cycloalkynyl ring is considered an aryl group, regardless of the ring to which the core structure is attached. A fused system of an aryl ring with a heterocyclic ring is considered a heterocyclic ring, regardless of the ring to which the core structure is attached. A fused system of an aryl ring with a heteroaryl group is considered a heteroaryl group, regardless of the ring to which the core structure is attached. Examples of suitable aryl groups include C 6-20 Aryl, preferably C 6-10 Aryl, more preferably C 6-9 Aryl. Non-limiting examples of aryl groups include phenyl, biphenyl, biphenylenyl, or 1- or 2-decalinyl; 1-, 2-, 3-, 4-, 5-, or 6-tetrahydronaphthyl (also known as "1,2,3,4-tetrahydronaphthenyl"); 1-, 2-, 3-, 4-, 5-, 6-, 7-, or 8-azepanyl, 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; 1-, 2-, 3-, 4-, or 5-pyrenyl.

[0250] The term "aryl-alkylene" as a group or part of a group refers to an alkyl group as defined herein in which at least one hydrogen atom is replaced by at least one aryl group as defined herein. Non-limiting examples of aryl-alkylene groups include benzyl, phenethyl, dibenzylmethyl, benzyl, 2-phenylethan-1-yl, 2-phenylethen-1-yl, naphthylmethyl, 2-naphthylethyl, and the like. The term "C 6-10 Aryl-C 1-6 "Alkylene" means an aryl-alkylene group where the alkylene portion can contain from 1 to 6 carbon atoms and the aryl portion from 6 to 10 carbon atoms.

[0251] The term "aryl-alkenylene" as a group or part of a group refers to an alkenylene group in which one of the hydrogen atoms bonded to a carbon atom is replaced by an aryl group. 6-10 Aryl C 2-6The term "alkenylene" refers to an arylalkenyl group of which the alkenylene portion may contain 2 to 6 carbon atoms and the aryl portion 6 to 10 carbon atoms.

[0252] The term "aryl-alkynylene" as a group or part of a group refers to an alkynylene group in which one of the hydrogen atoms bonded to a carbon atom is replaced by an aryl group. 6-10 Aryl C 2-6 "Alkyne" means that the alkenylene portion of the arylalkynyl group may contain 2 to 6 carbon atoms and the aryl portion 6 to 10 carbon atoms.

[0253] The term "haloalkyl" as a group or part of a group refers to an alkyl group having the meaning defined herein in which one or more hydrogen atoms are each replaced by 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.

[0254] As used herein, the term "glycosyl" refers to a chemical group obtained by replacing a hydroxyl group in a hemiacetal function of a monosaccharide, disaccharide, trisaccharide, oligosaccharide or polysaccharide. Glycosyl moieties having more than one monosaccharide may represent a linear or branched structure.

[0255] As used herein, the term "monosaccharide" refers to a simple form of sugar that is composed of a single sugar unit and cannot be further broken down into smaller sugar building blocks or parts. Common examples of monosaccharides include glucose (dextrose), fructose, galactose, mannose, and ribose. Monosaccharides can be linear or cyclic (i.e., can be referred to as furanose, pyranose). Monosaccharides can be classified according to the number of carbon atoms in the carbohydrate, namely: trioses with 3 carbon atoms, such as glyceraldehyde and dihydroxyacetone; tetroses with 4 carbon atoms, such as erythrose, threose and erythrulose; pentoses with 5 carbon atoms, such as arabinose, lyxose, ribose, xylose, ribulose and xylulose; hexoses with 6 carbon atoms, such as allose, altrose, galactose, glucose, gulose, idose, mannose, talose, fructose, psicose, sorbose and tagatose; heptoses with 7 carbon atoms, such as mannoheptulose and sedoheptulose; octose with 8 carbon atoms, such as 2-keto-3-deoxy-mannose-octanoate; nonoses with 9 carbon atoms, such as sialose; and decose with 10 carbon atoms. The above monosaccharides cover both D-monosaccharides and L-monosaccharides.

[0256] Alternatively, monosaccharide can be a monosaccharide derivative, wherein the sugar unit contains one or more substituents other than hydroxyl groups. Such derivatives can be, but are not limited to, ethers, esters, amides, acids, phosphates, and amines. Amine derivatives include, for example, glucosamine, galactosamine, fructosamine, and mannosamine. Amide derivatives include, for example, N-acetylated amine derivatives of sugars (e.g., N-acetylglucosamine, N-acetylgalactosamine).

[0257] As used herein, the term "disaccharide" refers to a molecular moiety containing two monosaccharides covalently bound to each other. Disaccharides include maltose [glucose-glucose], lactose [galactose-glucose], and sucrose [fructose-glucose].

[0258] As used herein, the term "trisaccharide" refers to a molecular moiety containing three monosaccharides covalently bound to each other.

[0259] As used herein, the term " oligosaccharide " refers to a molecular part containing at least 4 monosaccharides covalently bound to each other. Oligosaccharides include tetrasaccharides, pentasaccharides, hexasaccharides, heptasaccharides, octasaccharides, etc. The covalent bond for connecting sugars is generally composed of the glycosidic bond (i.e., C-O-C bond) formed from the hydroxyl group of adjacent sugars. Key can be present between the 1-carbon (anomeric carbon) and 4-carbon of adjacent sugars (i.e., 1-4 key), between the 1-carbon (anomeric carbon) and 3-carbon of adjacent sugars (i.e., 1-3 key), between the 1-carbon (anomeric carbon) and 6-carbon of adjacent sugars (i.e., 1-6 key) or between the 1-carbon (anomeric carbon) and 2-carbon of adjacent sugars (i.e., 1-2 key). Sugar can be connected in oligosaccharides so that the anomeric carbon is in α- or β-configuration. The oligosaccharides prepared according to the method of the present invention can also include the key between the carbon atoms except 1-, 2-, 3-, 4- and 6-carbon atoms.

[0260] As used herein, the term "polysaccharide" refers to a molecular moiety containing at least 9 monosaccharides covalently bound to each other. Polysaccharides include starch, hyaluronic acid, amylose, amylopectin, dextran, cyclodextrin, cellulose, agar, chitin, gum arabic and glycogen.

[0261] As will be understood by those skilled in the art, the term "O-glycosyl moiety" refers to a glycosyl moiety that is linked to another molecular moiety via an O-glycosidic bond. Similarly, an "S-glycosyl moiety" refers to a glycosyl moiety that is linked to another molecular moiety via an S-glycosidic bond, an "N-glycosyl moiety" refers to a glycosyl moiety that is linked to another molecular moiety via an N-glycosidic bond, and a "C-glycosyl moiety" refers to a glycosyl moiety that is linked to another molecular moiety via a C-glycosidic bond.

[0262] In some embodiments, preferred saccharides can be selected from the group comprising glucosyl, allosyl, altrosyl, galactosyl, gulosyl, idosyl, mannosyl, talosyl, fructosyl, psicosyl, sorbosyltagatosyl, sucrose, maltosyl, lactosyl, cellobiosyl, mannotriosyl, raffinose, melezitosyl, amylopectin saccharides, sialyl Lewis X (SiaLex), preferably glucosyl.

[0263] The term "carbonyl" as a group or part of a group refers to the group C(=O)-, also written as -CO-.

[0264] The term "alkylcarbonyl" as a group or part of a group refers to a group of the formula -C(=O)R x A group in which R x is alkyl as defined herein.

[0265] 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, for example, a 3-7 membered monocyclic ring, a 7-14 membered bicyclic ring, preferably containing a total of 3 to 10 ring atoms (3-10 membered heterocyclyl), more preferably 3 to 8 atoms (4-6 membered heterocyclyl), but more preferably 3 to 5 atoms (3-5 membered heterocyclyl). Each ring of the heterocycle or heterocyclyl group may have 1, 2, 3 or 4 heteroatoms selected from N, O, P and / or S, wherein the N and S heteroatoms may be optionally oxidized and the N heteroatom may be optionally quaternized; and wherein at least one carbon atom of the heterocyclyl group may be oxidized to form at least one C=O. The heterocyclyl group may be attached to any heteroatom or carbon atom of the ring or ring system, where valence permits. Polycyclic heterocyclyls or heterocyclic rings may be fused, bridged, and / or joined through one or more spiro atoms. A fused system of a heterocycle or heterocyclyl with an aryl ring is considered a heterocycle or heterocyclyl, regardless of the ring to which the core structure is attached. A fused system of a heterocycle or heterocyclyl with a heteroaryl ring is considered a heteroaryl, regardless of the ring to which the core structure is attached.

[0266] Non-limiting example heterocycles or heterocyclic groups include piperidinyl, piperazinyl, s-piperazinyl, morpholinyl, tetrahydropyranyl, tetrahydrofuranyl, pyrrolidinyl, aziridinyl, oxirane, thiopyranyl, acridinyl, oxetanyl, thietanyl, imidazolinyl, pyrazolidinyl, imidazolidinyl, oxazolinyl, isoxazolinyl, oxazolidinyl, isoxazolidinyl, tetrahydrothiazolyl, isotetrahydrothiazolyl, succinimidyl, indolinyl, isoindolinyl, chromanyl (also known as 3,4-dihydrobenzo[b]pyranyl), 2H-pyrrolyl, pyrrolinyl (e.g., 1-pyrrolinyl, 2-pyrrolinyl, 3-pyrrolinyl), 4H-quinolizinyl, 2-oxopiperazinyl, pyrazolinyl (e.g., 2-pyrazolinyl, 3-pyrazolinyl), tetrahydro-2H -pyranyl, 2H-pyranyl, 4H-pyranyl, dihydro-2H-pyranyl, 3-dioxanyl, 1,4-dioxinyl, 2,5-dioximidazolidinyl, 2-oxopiperidinyl, 2-oxopyrrolidinyl, indolinyl, tetrahydrothiophene, tetrahydroquinolinyl, tetrahydroisoquinolin-1-yl, tetrahydroisoquinolin-2-yl, tetrahydroisoquinolin-3-yl, tetrahydroisoquinolinyl thiomorpholin-4-yl, thiomorpholin-4-yl sulfoxide, thiomorpholin-4-yl sulfone, 1,3-dioxanyl, 1,4-oxathianyl, 1,4-dithianyl, 1,3,5-trioxanyl, 1H-pyrrolizinyl, tetrahydro-1,1-dioxythiophene, N-formylpiperazinyl, thiomorpholinyl, dihydrofuranyl, dihydrothiophenyl, tetrahydrothiophenyl, dihydropyrazolyl, dihydroimidazolyl, isothiazolinyl, thiazolinyl, triazolinyl, triazolidinyl, oxadiazolinyl, oxadiazolidinyl, thiadiazolinyl, thiadiazolinyl, tetrazolinyl, tetrazolidinyl, dihydropyridinyl, tetrahydropyridinyl, 1,2,3,6-tetrahydropyridinyl, hexahydropyridinyl, dihydropyrimidinyl, tetrahydropyrimidinyl, 1,4,5,6-tetrahydropyridinyl Hydropyrimidinyl, dihydropyrazinyl, tetrahydropyrazinyl, dihydropyridazinyl, tetrahydropyridazinyl, dihydrotriazinyl, tetrahydrotriazinyl, hexahydrotriazinyl, 1,4-diazepanyl, dihydroindolinyl, indolinyl, tetrahydroindolinyl, dihydroindazolyl, tetrahydroindazolyl, dihydroisoindolyl, dihydrobenzofuranyl, tetrahydrobenzofuranyl, dihydrobenzothiophene, tetrahydrobenzothiophene yl, dihydrobenzimidazolyl, tetrahydrobenzimidazolyl, dihydrobenzoxazolyl, 2,3-dihydrobenzo[d]oxazolyl, tetrahydrobenzoxazolyl, dihydrobenzoxazinyl, 3,4-dihydro-2H-benzo[b][1,4]oxazinyl, tetrahydrobenzoxazinyl, benzo[1,3]dioxol, benzo[1,4]dioxinyl, dihydropurinyl, tetrahydropurinyl, dihydroquinolinyl, 1,2,3,4-tetrahydroquinolinyl, dihydroisoquinolinyl, 3,4-dihydroisoquinolinyl-(1H)-yl, tetrahydroisoquinolinyl, 1,2,3,4-tetrahydroisoquinolinyl, dihydroquinazolinyl, tetrahydroquinazolinyl, dihydroquinoxalinyl, tetrahydroquinoxalinyl, 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]oxazin-(2H)-yl, (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, hexahydro-pyrrolo[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-1 H-pyrrolo[1,2-a]indolyl, 1,3-dihydro-2H-isoindolyl, octahydro-2H-isoindolyl, 2,5-diazabicyclo[2.2.1]heptyl, 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-diazabicyclo[2.2.1]heptenyl, Heterospiro[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]octanyl, 1,4-dihydropyreno[1,2-c]pyrazolyl, dihydropyranyl, dihydropyridinyl, dihydroquinolinyl, 8H-pyreno[1,2-d]thiazolyl, tetrahydroimidazo[1,2-a] pyridyl, 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 "oxirane alkyl" includes oxirane-2-yl. As used herein, the term "thiopyranyl" includes thiopyran-2-yl. As used herein, the term "acridinyl" includes acridin-1-yl, acridin-2-yl and acridin-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 "tetrahydrothiophene" includes tetrahydrothiophene-2-yl and tetrahydrothiophene-3-yl. As used herein, the term "succinimidyl" includes succinimidyl-1-yl and succinimidyl-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 2,3-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 "dihydrothiophene" 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 2,3-dihydrothiophen-5-yl.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 "dioxanyl", also known as "1,3-dioxanyl", includes dioxan-2-yl, dioxan-4-yl and dioxan-5-yl. As used herein, the term "dioxo" is also known as "1,3-dioxanyl".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-oxazolin-2-yl, 2-oxazolin-4-yl, 2-oxazolin-5-yl, 3-oxazolin-2-yl, 3-oxazolin-4-yl, 3-oxazolin-5-yl, 4-oxazolin-2-yl, 4-oxazolin-3-yl, 4-oxazolin-4-yl and 4 -oxazolin-5-yl. As used herein, the term "isoxazolinyl" includes 2-isoxazolin-3-yl, 2-isoxazolin-4-yl, 2-isoxazolin-5-yl, 3-isoxazolin-3-yl, 3-isoxazolin-4-yl, 3-isoxazolin-5-yl, 4-isoxazolin-2-yl, 4-isoxazolin-3-yl, 4-isoxazolin-4-yl and 4-isoxazolin-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 isothiazolidin-2-yl, isothiazolidin-3-yl, isothiazolidin-4-yl and isothiazolidin-5-yl. As used herein As used herein, the term "thiazolinyl" includes 2-thiazolin-2-yl, 2-thiazolin-4-yl, 2-thiazolin-5-yl, 3-thiazolin-2-yl, 3-thiazolin-4-yl, 3-thiazolin-5-yl, 4-thiazolin-2-yl, 4-thiazolin-3-yl, 4-thiazolin-4-yl and 4-thiazolin-5-yl. As used herein, the term "isothiazolinyl" includes 2-isothiazolin-3-yl, 2-isothiazolin-4-yl, 2-isothiazolin-5-yl, 3-isothiazolin-3-yl, 3-isothiazolin-4-yl, 3-isothiazolin-5-yl, 4-isothiazolin-2-yl, 4-isothiazolin-3-yl, 4-isothiazolin-4-yl and 4-isothiazolin-5-yl. As used herein , the term "piperidyl", also known as "piperidinyl", includes piperidin-1-yl, piperidin-2-yl, piperidin-3-yl and piperidin-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, 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 -tetrahydropyranyl, 1,2,3,6-tetrahydropyranyl, 1,2,3,6-tetrahydropyranyl, 1,2,3,6-tetrahydropyranyl, 1,2,3,6-tetrahydropyranyl, 2,3,4,5-tetrahydropyranyl-2-yl, 2,3,4,5-tetrahydropyranyl-3-yl, 2,3,4,5-tetrahydropyranyl-3-yl, 2,3,4,5-tetrahydropyranyl-4-yl, 2,3,4,5-tetrahydropyranyl-5-yl and 2,3,4,5-tetrahydropyranyl-6-yl. As used herein, the term "tetrahydropyranyl", also known as "oxa-yl" 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 "tetrahydrothiophene" includes tetrahydrothiophene-2-yl, tetrahydrothiophene-3-yl and tetrahydrothiophene-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 "piperidinyl", 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 "dioxa-yl" includes 1,2-dioxa-3-yl, 1,2-dioxa-4-yl, 1,3-dioxa-2-yl, 1,3-dioxa-4-yl, 1,3-dioxa-5-yl and 1,4-dioxa-2-yl. As used herein, the term "dithianyl" includes 1,2-dithiane-3-yl, 1,2-dithiane-4-yl, 1,3-dithiane-2-yl, 1,3-dithiane-4-yl, 1,3-dithiane-5-yl and 1,4-dithiane-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-trioxa-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 "piperazinyl" includes azepan-1-yl, azepan-2-yl, azepan-3-yl and azepan-4-yl. As used herein, the term "isopiperazinyl" includes isopiperazin-1-yl, isopiperazin-2-yl, isopiperazin-3-yl and isopiperazin-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 quinolizin-1-yl, quinolizin-2-yl, quinolizin-3-yl and quinolizin-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 quinolizin-1-yl, quinolizin-2-yl, quinolizin-3-yl and quinolizin-4-yl. As used herein, the term "quinolizinyl" includes quinolizin-1-yl, quinolizin-2-yl, quinolizin-3-yl and quinolizin-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.

[0267] The term "heterocycloalkylene" or "heterocyclyl-alkylene" as a group or part of a group refers to an alkylene group as defined herein wherein at least one hydrogen atom is replaced by at least one heterocyclyl group as defined herein and may be of the formula R y R r The group represents, wherein R y is an alkylene group, and R r The term "3 to 10 membered heterocyclyl-C 1-6 "Alkylene" refers to a heterocyclyl-alkylene group wherein 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 including at least one N, O, S or P.

[0268] The term "heterocycloalkenylene" or "heterocyclyl-alkenylene" as a group or part of a group refers to an alkenylene group as defined herein wherein at least one hydrogen atom is replaced by at least one heterocyclyl group as defined herein and may be of the formula R t R r The group represents, wherein R t is alkenylene, and R r The term "3 to 10 membered heterocyclyl-C 2-6 "Alkenylene" refers to a heterocyclyl-alkenylene group wherein 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 including at least one N, O, S or P.

[0269] The term "heterocycloalkynylene" or "heterocyclyl-alkynylene" as a group or part of a group refers to an alkynylene group as defined herein wherein at least one hydrogen atom is replaced by at least one heterocyclyl group as defined herein and may be of the formula R s R r The group represents, wherein R s is an alkynylene group, and R r The term "3 to 10 membered heterocyclyl-C 2-6 "Alkynylene" refers to a heterocyclyl-alkynylene group wherein 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 including at least one N, O, S or P.

[0270] The term "heteroaryl" refers to an aromatic ring system comprising 5 to 18 atoms including at least one N, O, S or P, containing 1 or 2 rings, preferably 5 to 14 atoms (5-14 membered heteroaryl), but more preferably 5 to 10 atoms (5-10 membered heteroaryl), which may be fused together or covalently linked, with each ring typically containing 5 to 6 atoms; at least one of the rings is aromatic, wherein the N and S heteroatoms may optionally be oxidized, and the N heteroatom may optionally be quaternized, and wherein at least one carbon atom of the heteroaryl group may be oxidized to form at least one C=O. A system of a heteroaryl ring fused to a cycloalkyl ring, a cycloalkenyl ring or a cycloalkynyl ring is considered a heteroaryl, regardless of the ring attached to the core structure. A system of a heteroaryl ring fused to a heterocyclic ring is considered a heteroaryl, regardless of the ring attached to the core structure. A system of a heteroaryl ring fused to an aryl ring is considered a heteroaryl, regardless of the ring attached to the core structure.Non-limiting examples of such heteroaryl groups include pyridyl, pyrrolyl, thiophenyl (also known as 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, dioxazinyl, thiazinyl, triazinyl, pyranyl, thiopyranyl, imidazo[2,1-b][1,3]thiazolyl, thieno[3,2-b]furanyl, thieno[3 ,2-b]thienyl, thieno[2,3-d][1,3]thiazolyl, thieno[2,3-d]imidazolyl, tetrazolo[1,5-a]pyridinyl, indolyl, indolizinyl, isoindolyl, benzofuranyl, isobenzofuranyl, benzothienyl, isobenzothienyl, 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-benzoxazolyl oxadiazolyl, 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-benzodioxol, quinolyl, isoquinolyl, cinnoline 1H-pyrazolyl, 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.

[0271] As used herein, the term "pyrrolyl" (also known as azo) includes pyrrol-1-yl, pyrrol-2-yl, and pyrrol-3-yl. As used herein, the term "furanyl" (also known as "furyl") includes furan-2-yl and furan-3-yl (also known as furan-2-yl and furan-3-yl). As used herein, the term "thiophenyl" (also known as "thienyl") includes thien-2-yl and thien-3-yl (also known as thien-2-yl and thien-3-yl). As used herein, the term "pyrazolyl" (also known as 1H-pyrazolyl and 1,2-oxadiazolyl) 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 imidazole-1-yl, imidazole-2-yl, imidazole-4-yl and imidazole-5-yl. As used herein, the term "oxazolyl" (also referred to as 1,3-oxazolyl) includes oxazol-2-yl, oxazol-4-yl and oxazol-5-yl. As used herein, the term "isoxazolyl" (also referred to as 1,2-oxazolyl) includes isoxazol-3-yl, isoxazol-4-yl and isoxazol-5-yl. As used herein, the term "thiazolyl" (also referred to as 1,3-thiazolyl) includes thiazolyl-2-yl, thiazolyl-4-yl and thiazolyl-5-yl (also referred to as 2-thiazolyl, 4-thiazolyl and 5-thiazolyl). As used herein, the term "isothiazolyl" (also referred to as 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 "pyridyl" (also referred to as "pyridyl") includes pyridin-2-yl, pyridin-3-yl and pyridin-4-yl (also referred to as 2-pyridinyl, 3-pyridinyl and 4-pyridinyl). As used herein, the term "pyrimidinyl" includes pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl and pyrimidin-6-yl. As used herein, the term "pyrazinyl" includes pyrazine-2-yl and pyrazine-3-yl. As used herein, the term "pyridazinyl" includes pyridazine-3-yl and pyridazine-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 "dioxazinyl" (also referred to as "1,4-dioxazinyl") includes 1,4-dioxazin-2-yl and 1,4-dioxazin-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]thienyl" 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 known as 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 known as 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]thiophenyl) 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 benzothiophen-2-yl, benzothiophen-3-yl, benzothiophen-4-yl, benzothiophen-5-yl, benzothiophen-6-yl, and benzothiophen-7-yl). As used herein, the term "isobenzothiophenyl" (also known as benzo[c]thiophenyl) includes isobenzothiophen-1-yl, isobenzothiophen-3-yl, isobenzothiophen-4-yl, isobenzothiophen-5-yl, isobenzothiophen-6-yl, and isobenzothiophen-7-yl.As used herein, the term "indazolyl" (also known as 1H-indazolyl or 2-azaindolyl) 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-benzoxazolyl-2-yl, 1,3-benzoxazolyl-4-yl, 1,3-benzoxazolyl-5-yl, 1,3-benzoxazolyl-6-yl, and 1,3-benzoxazolyl-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, 1,2-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-benzoxadiazolyl-4-yl, 2,1,3-benzoxadiazolyl-5-yl, 2,1,3-benzoxadiazolyl-6-yl, and 2,1,3-benzoxadiazolyl-7-yl. As used herein, the term "1,2,3-benzothiadiazolyl" includes 1,2,3-benzothiadiazolyl-4-yl, 1,2,3-benzothiadiazolyl-5-yl, 1,2,3-benzothiadiazolyl-6-yl, and 1,2,3-benzothiadiazolyl-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-benzodioxol" 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.

[0272] Heteroaryl and heterocycle or heterocyclic groups as used herein include, for example, but are not limited to, groups described in Paquette, Leo A. "Principles of Modern Heterocyclic Chemistry" (WA Benjamin, New York, 1968), specifically Chapters 1, 3, 4, 6, 7, and 9; "The Chemistry of Heterocyclic Compounds, Aseries of Monographs" (John Wiley & Sons, New York, 1950 to present), specifically Volumes 13, 14, 16, 19, and 28; Katritzky, Alan R., Rees, CW, and Scriven, E. "Comprehensive Heterocyclic Chemistry" (Pergamon Publishing Company, 1996). Press), 1996); and Journal of the American Chemical Society (J. Am. Chem. Soc.) (1960) 82:5566.

[0273] The term "heteroarylalkylene" or "heteroaryl-alkylene" as a group or part of a group refers to an alkylene group as defined herein wherein at least one hydrogen atom is replaced by at least one heteroaryl group as defined herein and may be of the formula R y R u The group represents, wherein R y is an alkylene group, and R u is a heteroaryl group as defined herein. 1-6 "Alkylene" refers to a heteroaryl-alkylene group wherein 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.

[0274] The term "heteroarylalkenylene" or "heteroaryl-alkenylene" as a group or part of a group refers to an alkenylene group as defined herein wherein at least one hydrogen atom is replaced by at least one heteroaryl group as defined herein and may be of the formula R t R u The group represents, wherein R t is alkenylene, and R u is a heteroaryl group as defined herein. 2-6"Alkenylene" refers to a heteroaryl-alkenyl group wherein 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.

[0275] The term "heteroarylalkynylene" or "heteroaryl-alkynylene" as a group or part of a group refers to an alkynylene group as defined herein wherein at least one hydrogen atom is replaced by at least one heteroaryl group as defined herein, and may be of the formula R s R u The group represents, wherein R s is an alkynylene group, and R u is a heteroaryl group as defined herein. 2-6 "Alkynylene" refers to a heteroaryl-alkynylene group wherein 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.

[0276] The name of any substituent found in more than one position in a compound of the invention should be selected independently.

[0277] Substituents are optionally named with or without a bond. Regardless of the orientation of the bond, if a substituent is multivalent (according to its position in the structure), any and all possible orientations of the substituent are intended.

[0278] Unless expressly stated otherwise, any reference to a "compound according to the invention" or a "compound of formula (I)" also includes isomers such as stereoisomers and tautomers, salts such as pharmaceutically and / or physiologically acceptable salts, hydrates, solvates, polymorphs of such compounds.

[0279] As used herein, the term "isomer" refers to all possible isomeric forms that the compounds of the formulae herein may possess, including tautomeric and stereochemical forms, but excluding positional isomers. In general, the structures shown herein illustrate only one tautomeric or resonance form of the compounds, but corresponding alternative configurations are also contemplated.

[0280] Depending on its substitution pattern, the compounds of the present invention may or may not have one or more optical stereo centers 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 indicated, the chemical name of the compound represents a mixture of all possible stereochemical isomeric forms, the mixture containing all diastereomers and enantiomers of the basic molecular structure (because the compound of the chemical formula herein can have at least one chiral center), as well as stereochemically pure or enriched compounds. More specifically, the stereocenter can have an R configuration or an S configuration, and multiple bonds can have a cis or trans configuration. The term R configuration or S configuration is used herein according to Chemical Abstracts nomenclature. The terms cis and trans are used herein according to Chemical Abstracts nomenclature and include the position of the substituent on the ring portion. Those skilled in the art can easily determine the absolute stereochemical configuration of the compound of the chemical formula described herein while using well-known methods, such as X-ray diffraction.

[0281] Separation of stereoisomers is accomplished by standard methods known to those skilled in the art. One enantiomer of a compound can be separated by methods such as forming diastereomers using an optically active resolving agent, substantially free of its opposite enantiomer (E. L. Eil, "Stereochemistry of Carbon Compounds," (1962), McGraw Hill; Lochmuller, CH, (1975) "Journal of Chromatography," 113: (3) 283-302). Separation of isomers in a mixture can be achieved by any suitable method, including: (1) forming ionic diastereomeric salts with chiral compounds and separating by fractional crystallization or other methods, (2) forming diastereomeric compounds with chiral derivatizing agents, separating the diastereomers and converting them into pure enantiomers, or (3) enantiomers can be separated directly under chiral conditions. In method (1), diastereomeric salts can be formed by reacting an enantiomerically pure chiral base (such as strychnine, quinine, ephedrine, strychnine, a-methyl-b-phenylethylamine (amphetamine), etc.) with an asymmetric compound having an acidic functional group (such as carboxylic acid and sulfonic acid). The diastereomeric salts can be induced to separate by fractional crystallization or ion chromatography. In order to separate the optical isomers of amino compounds, chiral carboxylic acids or sulfonic acids (such as camphorsulfonic acid, tartaric acid, mandelic acid or lactic acid) are added to form diastereomeric salts. Alternatively, by method (2), the substrate to be resolved can be reacted with one enantiomer of the chiral compound to form a diastereomeric pair (Eliel, E. and Wilen, S. (1994) Stereochemistry of Organic Compounds Compounds, John Wiley & Sons, p. 322). Diastereomeric compounds can be formed by reacting an asymmetric compound with an enantiomerically pure chiral derivatizing agent (e.g., a menthyl derivative), followed by separation of the diastereomers and hydrolysis to produce the free enantiomerically enriched compound. Methods for determining optical purity include preparing a chiral ester of the racemic mixture, such as the menthyl or Mosher esters, α-methoxy-α-(trifluoromethyl)phenyl acetate (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 by normal and reverse phase chromatography and by following the separation method for atropisomeric naphthylisoquinolines (Hoye, T., WO 96 / 15111).According to method (3), the racemic mixture of the two asymmetric enantiomers is separated by chromatography using a chiral stationary phase. Suitable chiral stationary phases are, for example, polysaccharides, in particular cellulose or amylose derivatives. A commercially available chiral stationary phase based on polysaccharides is ChiralCel. TM CA, OA, OB5, OC5, OD, OF, OG, OJ, OK, and Chiralpak TM AD, AS, OP(+) and OT(+). Suitable eluents or mobile phases for use in combination with the polysaccharide chiral stationary phase are hexane modified with an alcohol (e.g., ethanol, isopropanol, etc.). ("Chiral Liquid Chromatography" (1989) edited by W. J. Lough, 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", Journal of Chromatography 513: 375-378).

[0282] The term "salt" refers to any salt that a compound can form. The salt may be a cosmetically or pharmaceutically acceptable salt. Thus, the compounds of the present invention optionally include salts of the compounds herein, particularly cosmetically or pharmaceutically acceptable non-toxic salts, such as those containing Na + 、Li + , K + , Ca 2+ and Mg 2+. Such salts may include salts derived from a combination of suitable cations (such as alkali and alkaline earth metal ions or ammonium and quaternary amino ions) with an acid anion moiety (typically a carboxylic acid). The compounds of the present invention may carry multiple positive or negative charges. The net charge of the compounds of the present invention may be positive or negative. Any relevant counterions are generally determined by the synthesis and / or separation methods used to obtain the compound. 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, isopropylamine, trimethylamine, diethylamine, triethylamine, tripropylamine, ethanolamine, and the like. It should be understood that the identity of any associated counterion is not a key feature of the present invention, and the present invention encompasses compounds associated with any type of counterion. Furthermore, since 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 counterions (e.g., dry salts), but also forms not associated with counterions (e.g., aqueous or organic solutions). Metal salts are typically prepared by reacting metal hydroxides with the compounds of the present invention. Examples of metal salts prepared in this manner are Li-containing + 、Na + and K + Salts of. By adding a suitable metal compound, a metal salt with lower solubility can be precipitated from a salt solution with higher solubility. In addition, salts can be formed by acid addition of certain organic and inorganic acids with a basic center (usually an amine) or an acidic group. Examples of such suitable acids include, for example, inorganic acids (such as hydrohalic acids), such as hydrochloric acid or hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, etc.; or organic acids, such as acetic acid, propionic acid, glycolic acid, 2-hydroxypropionic acid, 2-oxopropionic acid, lactic acid, pyruvic acid, oxalic acid (i.e., oxalic 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, cyclamic acid, salicylic acid (i.e., 2-hydroxybenzoic acid), p-aminosalicylic acid, etc. In addition, this term also includes solvates that the compounds of the chemical formula herein and their salts can form, such as hydrates, alcoholates, etc. Finally, it should be understood that the compositions herein can comprise the compounds of the present invention in their unionized and zwitterionic forms, as well as in the form of hydrates in combination with a stoichiometric amount of water.

[0283] Also included within the scope of the present invention are salts of the compounds with one or more amino acids, particularly naturally occurring amino acids found as components of proteins. Amino acids are typically amino acids with side chains having basic or acidic groups (e.g., lysine, arginine, or glutamic acid) or neutral groups (e.g., glycine, serine, threonine, alanine, isoleucine, or leucine).

[0284] 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 salts derived from appropriate bases, such as alkali metals (e.g., sodium) and alkaline earth metals (e.g., magnesium), ammonium and NX4 + (wherein X is a C1-C4 alkyl group). 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 aminosulfonic acid). Physiologically acceptable salts of compounds containing hydroxyl groups include salts of anions of the compound with, for example, Na + and NX4 + However, salts of acids or bases that are not physiologically acceptable may also be used, for example, in the preparation or purification of physiologically acceptable compounds.

[0285] All salts, whether or not derived from physiologically acceptable acids or bases, are within the scope of the present invention. Non-limiting examples of suitable such salts include, but are not limited to, acid addition salts formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like; or with organic acids such as 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, carboxylic acid, benzoic acid, benzoyl ... Cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethanedisulfonic acid, 2-hydroxyethylsulfonic acid, 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, tert-butylacetic acid, lauryl sulfuric 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, decanoate, camphorate, cyclamate, lauryl sulfate, oxalate, ethanesulfonate, isethionate, formate, galactonate, gentisate, glucoheptonate, glucuronate, oxoglutarate, hippurate, lactobionate, naphthalene disulfonate, cinafoate, nicotinate, oleate, orotate, oxalate, palmitate, Palmitate, siprate, pyroglutamate, p-aminosalicylate, sebacate, tannate, thiocyanate, undecenoate, etc.; or salts formed by replacement of an acidic proton in the parent compound by, for example, ammonia, arginine, phenethylbenzylamine, benzathine penicillin, calcium, choline, danol, diethanolamine, diethylamine, ethanolamine, ethyleneamine, meglumine, glycine, hydrazine penicillin, imidazole, lysine, magnesium, hydroxyethylmorpholine, piperazine, potassium, epolamine, sodium, triethanolamine, tromethamine, or zinc.

[0286] The scope of the present invention includes solvates of the compounds as defined herein. The term "solvate" refers to a crystalline solid formed from an active compound and a second component (solvent) that is in a separate form and is liquid at room temperature. 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; alcohol solvents such as methanol, ethanol or isopropanol; ether 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 the compound will be a hydrate.

[0287] 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 exhibit different biological properties such as activity. The present invention relates to amorphous and crystalline compounds of formula (I), mixtures of different crystalline states of the corresponding compounds of formula (I).

[0288] The term "polymorph" refers to a specific crystalline form of a compound that can crystallize into different crystalline forms with different molecular arrangements and / or conformations in the crystal lattice. Different crystal forms typically have different X-ray diffraction patterns, infrared spectra, melting points, density, hardness, crystal shape, optical and electrical properties, stability, and solubility. Although polymorphs may have the same chemical composition, they may also differ in composition due to the presence or absence of co-crystallized water or other molecules, and they may be weakly or strongly bound in the crystal lattice. Polymorphs may differ in chemical, physical, and biological properties such as crystal shape, density, hardness, color, chemical stability, melting point, hygroscopicity, suspension, dissolution rate, and bioavailability. Those skilled in the art will appreciate that a polymorph of a compound described herein may exhibit beneficial effects (e.g., suitability for preparing useful formulations, improved biological performance) relative to another polymorph or mixture of polymorphs of the same compound. The preparation and separation of a specific polymorph of a compound can be achieved by methods known to those skilled in the art, including, for example, using a selected solvent and temperature to carry out crystallization. Recrystallization solvent, crystallization rate, storage temperature, and other factors may cause a crystalline form to dominate. Various polymorphs of a compound can be prepared by crystallization under different conditions. For a comprehensive discussion of polymorphism, see "Polymorphism in the Pharmaceutical Industry," edited by Rolf Hilfiker, Wiley-VCH, Weinheim, 2006.

[0289] When referring to weight percentages of compositions and products and ingredients contained therein, it is understood that the total amount of ingredients according to the present invention does not exceed 100% (±1% due to rounding).

[0290] In this specification, the term "non-therapeutic" refers to a concept that does not include medical behavior, that is, treating the human body through medical means.

[0291] The preferred descriptions (features) and embodiments of the methods, compositions and uses of the present invention are listed below. Unless otherwise expressly stated, each statement and embodiment of the present invention as defined above may be combined with any other statement and / or embodiment. In particular, any feature indicated as preferred or advantageous may be combined with any other feature or statement indicated as preferred or advantageous. Thus, the present invention may be implemented in particular by any one or any combination of one or more of the following numbered statements and embodiments, as well as any other aspects and / or embodiments.

[0292] 1. A compound of formula (I):

[0293]

[0294] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0295] Ar 1 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R za replace;

[0296] Each R za 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0297] 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; wherein said alkyl, said haloalkyl, said alkylcarbonyl, said Each of the alkenyl, the alkynyl, the aryl, the heterocyclyl, the heteroaryl, the cycloalkyl, the aryl-alkylene, the aryl-alkenylene, the aryl-alkynylene, the heteroaryl-alkylene, the heteroaryl-alkenylene, the heteroaryl-alkynylene, the heterocyclyl-alkylene, the heterocyclyl-alkenylene, the heterocyclyl-alkynylene, the cycloalkyl-alkylene, the cycloalkyl-alkenylene and the cycloalkyl-alkynylene may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl, and alkynyl;

[0298] R h selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0299] R a1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0300] R b1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0301] R c1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0302] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0303] X 1a Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0304] Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-ORb 、-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;

[0305] X 2a For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3;

[0306] Each R c and R d 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;

[0307] R e selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0308] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0309] R g Selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0310] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0311] Z 2a Selected from the group consisting of: 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;

[0312] Y 1a Select from -OR a 、-R a or -NR a R b , or Y 1a is a moiety having formula (A);

[0313]

[0314] in

[0315] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0316] Each R zb are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0317] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0318] Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-Re -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;

[0319] X 2b For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; and

[0320] Y 1b Select from -OR a 、-NR b R a or -R a ;

[0321] The condition is

[0322] no and

[0323] Provided that the compound is not:

[0324] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0325] 4-(2-Acetylaminophenyl)-2-amino-4-oxobutanoic acid;

[0326] 2-Acetylamino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0327] (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;

[0328] 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;

[0329] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid methyl ester;

[0330] 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0331] 2-Acetylamino-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0332] (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-acetyl triacetate;

[0333] 2-Amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid.

[0334] 2. A compound of formula (I):

[0335]

[0336] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0337] Ar 1 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R za replace;

[0338] Each R za 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0339] Each R aindependently 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;

[0340] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0341] X 1a Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0342] Z 1a Selected from the group consisting of: 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;

[0343] X 2a For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably n is 1;

[0344] Each R c and R d 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;

[0345] R eselected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0346] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0347] R g Selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0348] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0349] Z 2a Selected from the group consisting of: 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;

[0350] Y 1a is a moiety having formula (A), or Y 1a Select from -OR a 、-R a or -NR a R b ;

[0351]

[0352] in

[0353] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0354] Each R zb are independently selected from the group consisting of 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, unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0355] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0356] Z 1b Selected from the group consisting of 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;

[0357] X 2b For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably m is 1; and

[0358] Y 1b Select from -OR a 、-NR b R a or -R a ;

[0359] The condition is

[0360] no and

[0361] Provided that the compound is not:

[0362] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0363] 4-(2-Acetylaminophenyl)-2-amino-4-oxobutanoic acid;

[0364] 2-Acetylamino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0365] (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;

[0366] 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

[0367] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid methyl ester,

[0368] 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0369] 2-Acetylamino-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0370] (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-acetyl triacetate;

[0371] 2-Amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid.

[0372] 3. A compound of formula (II):

[0373]

[0374] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0375] R 1a 、R 2a 、R 3a and R 4a Each independently is R za ;

[0376] Each R zaare 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0377] 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, cycloalkyl-alkynylene, and -R f1 -R g1 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 may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl and alkynyl; wherein 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; Rb1 is selected from the group consisting of hydrogen, alkyl, alkenyl, and alkynyl; R c1 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0378] R f1 is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0379] R g1 is hydrogen or alkyl;

[0380] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0381] X 1a -NR b -;

[0382] Z 1a Selected from the group consisting of: 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;

[0383] X 2a For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3;

[0384] Each R c and R d 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;

[0385] R eselected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0386] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0387] R g is selected from hydrogen, alkyl, N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0388] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0389] Z 2a Selected from the group consisting of 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;

[0390] Y 1a Select from -OR a 、-R a or -NR a R b , or Y 1a is a moiety having formula (A);

[0391]

[0392] in

[0393] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0394] Each R zb are independently selected from the group consisting of 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, unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0395] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0396] Z 1b Selected from the group consisting of: 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;

[0397] X 2b For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; and

[0398] Y 1b Select from -OR a 、-NR b R a or -R a .

[0399] 4. A compound of formula (II):

[0400]

[0401] or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein

[0402] R 1a 、R 2a 、R 3a and R4a Each independently is R za ;

[0403] Each R za 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, cycloalkyl-alkynylene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0404] 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, cycloalkyl-alkynylene, and -R f1 -R g1 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 may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl and alkynyl; wherein Rh 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 selected from the group consisting of: hydrogen, alkyl, alkenyl, and alkynyl;

[0405] R f1 is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0406] R g1 is hydrogen or alkyl;

[0407] Each R b independently selected from the group comprising hydrogen, halo, alkyl, haloalkyl, alkylcarbonyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, aryl-alkylene, heteroaryl-alkylene, heterocyclyl-alkylene, and cycloalkyl-alkylene;

[0408] X 1a -NR b -;

[0409] Z 1a Selected from the group consisting of: 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;

[0410] X 2a For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3;

[0411] Each R c and R dindependently 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;

[0412] R e selected from the group comprising alkylene, alkenylene, alkynylene, arylene, heterocyclylene, heteroarylene, and cycloalkylene;

[0413] R f is an alkylene group, wherein the alkylene group may be interrupted by one or more O or S;

[0414] R g is selected from hydrogen, alkyl, N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl;

[0415] W 1a Selected from-NR b Z 2a 、-R a OR a ;

[0416] Z 2a Selected from the group consisting of 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;

[0417] Y 1a Select from -OR a 、-R a or -NR a R b , or Y 1a is a moiety having formula (A);

[0418]

[0419] in

[0420] Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb replace;

[0421] Each Rzb are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ;

[0422] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-;

[0423] Z 1b Selected from the group consisting of: 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;

[0424] X 2b For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; and

[0425] Y 1b Select from -OR a 、-NR b R a or -R a ;

[0426] Provided that the compound is not:

[0427] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0428] (R)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0429] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0430] 4-(2-Acetylaminophenyl)-2-amino-4-oxobutanoic acid;

[0431] 2-Acetylamino-4-(2-aminophenyl)-4-oxobutanoic acid;

[0432] (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;

[0433] 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;

[0434] (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;

[0435] (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;

[0436] 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid methyl ester;

[0437] 4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0438] 2-Acetylamino-4-(2-amino-3-(((3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)phenyl)-4-oxobutanoic acid;

[0439] (S)-2-Acetylamino-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;

[0440] (R)-2-Acetylamino-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;

[0441] (2R,3R,4S,5R)-2-(acetoxymethyl)-6-(2-amino-3-(4-methoxy-4-oxobutanoyl)phenoxy)tetrahydro-2H-pyran-3,4,5-acetyl triacetate;

[0442] 2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0443] (S)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0444] (R)-2-amino-4-(2-amino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0445] 5-(2-aminophenyl)-5-oxopentanoic acid;

[0446] 4-(2-aminophenyl)-4-oxobutanoic acid;

[0447] Methyl 6-(2-aminophenyl)-6-oxohexanoate;

[0448] Methyl 4-(2-aminophenyl)-2-((tert-butoxycarbonyl)amino)-4-oxobutanoate;

[0449] Butyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate;

[0450] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid ethyl ester;

[0451] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid diacetate;

[0452] (R)-2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0453] (S)-2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0454] 2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid;

[0455] 2-Acetylamino-4-(2-acetylaminophenyl)-4-oxobutanoic acid methyl ester;

[0456] 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;

[0457] 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-D-bioside); 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;

[0458] 4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid O-β-d-glycoside;

[0459] 2-amino-4-(2-formylamino-5-hydroxyphenyl)-4-oxobutanoic acid;

[0460] 2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid;

[0461] (R)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid;

[0462] (S)-2-amino-4-(2-amino-3-chlorophenyl)-4-oxobutanoic acid;

[0463] 2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid;

[0464] (R)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid;

[0465] (S)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid;

[0466] 2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid;

[0467] (R)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid;

[0468] (S)-2-amino-4-(2-amino-5-fluorophenyl)-4-oxobutanoic acid;

[0469] 2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid;

[0470] (R)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid;

[0471] (S)-2-amino-4-(2-amino-5-bromophenyl)-4-oxobutanoic acid;

[0472] 2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid;

[0473] (R)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid;

[0474] (S)-2-amino-4-(2-amino-5-methylphenyl)-4-oxobutanoic acid;

[0475] 2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid;

[0476] (R)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid;

[0477] (S)-2-amino-4-(2-amino-5-ethylphenyl)-4-oxobutanoic acid;

[0478] 2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid;

[0479] (R)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid;

[0480] (S)-2-amino-4-(2-amino-5-propylphenyl)-4-oxobutanoic acid;

[0481] 2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid;

[0482] (R)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid;

[0483] (S)-2-amino-4-(2-amino-5-isopropylphenyl)-4-oxobutanoic acid;

[0484] 2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid;

[0485] (R)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid;

[0486] (S)-2-amino-4-(2-amino-5-cyclohexylphenyl)-4-oxobutanoic acid;

[0487] 2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid;

[0488] (S)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid;

[0489] (R)-2-amino-4-(2-(methylamino)phenyl)-4-oxobutanoic acid;

[0490] 2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid;

[0491] (S)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid;

[0492] (R)-2-amino-4-(2-(dimethylamino)phenyl)-4-oxobutanoic acid;

[0493] 2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0494] (R)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0495] (S)-2-amino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0496] 2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid;

[0497] (R)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid;

[0498] (S)-2-amino-4-(2-amino-6-chlorophenyl)-4-oxobutanoic acid;

[0499] 2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0500] (R)-2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0501] (S)-2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid;

[0502] 2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid;

[0503] (S-)2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid;

[0504] (R-)2-amino-4-(2-amino-3-hydroxyphenyl)-4-oxobutanoic acid;

[0505] (S-)methyl 2-amino-4-(2-aminophenyl)-4-oxobutanoate;

[0506] 2-amino-4-(2-aminophenyl)-4-oxobutanamide;

[0507] (R)-2-amino-4-(2-aminophenyl)-4-oxobutanamide;

[0508] (S)-2-amino-4-(2-aminophenyl)-4-oxobutanamide;

[0509] (S)-2-Acetylamino-4-(2-acetylaminophenyl)-4-oxobutanoic acid;

[0510] (S)-2-Formylamino-4-(2-formylaminophenyl)-4-oxobutanoic acid; and

[0511] 4-(2-Aminophenyl)-4-oxo-2-phenylbutanamide.

[0512] 5. A compound according to any one of Statements 1 or 2, wherein

[0513] Ar 1 C 6-10 aryl or 5- to 10-membered heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 C 6-10 aryl or a 6-membered heteroaryl containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 is phenyl; wherein the phenyl group may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 is phenyl;

[0514] Each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl, C3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylidene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R za independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R za are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R za For hydrogen,

[0515] Each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkynylidene; wherein the C 1-20 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-20 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the C 6-10 Aryl-C 2-6 Alkenylene, the C 6-10 Aryl-C 2-6 Alkyne, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 5 to 10 membered heteroaryl-C 2-6 Alkenylene, the 5 to 10 membered heteroaryl-C 2-6 Alkyne, the 3 to 10 membered heterocyclic group-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 2-6 Alkenylene, the 3 to 10 membered heterocyclic group-C 2-6 Alkynylidene, the C 3-6 Cycloalkyl-C 1-6 Alkylene, the C 3-6 Cycloalkyl-C 2-6 Alkenylene and the C 3-6 Cycloalkyl-C 2-6 Each of the alkynylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halogenated, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R h Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C2-6 Alkenyl and C 2-6 Alkynyl; R a1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R b1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R c1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; wherein the C 1-18 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-18 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: COO-R h 、 -NR a1 R b1 , halogenated, C 1-6Alkyl, halogenated C 1-6 Alkyl and C 1-6 Alkylcarbonyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; wherein the C 1-16 Alkyl, the C 2-16 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 3 to 6 membered heterocyclic group, the 5 to 6 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 6 membered heteroaryl-C 1-6 Alkylene, the 3 to 6 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 5- to 6-membered heterocyclic group 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, the C 2-15 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 5- to 6-membered heterocyclic group containing at least one N or O, the 5- to 6-membered heteroaryl containing at least one N and the C 3-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; wherein the C 1-15 Alkyl, the C 2-10 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-10 Alkylcarbonyl, the phenyl, the 6-membered heteroaryl containing at least one N, the 3 to 5-membered heterocyclic group containing at least one N or one O, and the C 5-6Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 alkylcarbonyl, a 3- to 4-membered heterocyclic group containing at least one O, and a phenyl group; wherein said C 1-15 Alkyl, the C 2-8 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-8 Each of the alkylcarbonyl group, the 3- to 4-membered heterocyclic group containing at least one O, and the phenyl group may be unsubstituted or replaced by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, oxirane and C 1-8 Alkylcarbonyl; wherein the C 1-15 Alkyl, the C 2-6 alkenyl, the oxirane alkyl and the C1-8 Each of the alkylcarbonyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane alkyl; wherein said C 1-15 Alkyl, the C 2-6 alkenyl, the oxirane alkyl and the C 1-8 Each of the may be unsubstituted or replaced by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-4 Alkyl; R h Selected from hydrogen or C 1-4 Alkyl; R a1 Selected from hydrogen or C 1-4 Alkyl; R b1 Selected from hydrogen or C 1-4 Alkyl; R c1 Selected from hydrogen or C 1-4 Alkyl; for example, each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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-C2-6 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10Aryl, 5- to 6-membered heterocyclic group containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 alkylcarbonyl, 3 to 4 membered heterocyclic group containing at least one O and phenyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, oxirane and C 1-8 Alkylcarbonyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane;

[0516] Each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6-membered heterocyclic group containing at least one N, 5 to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 6-10 Aryl; preferably each R b independently selected from the group consisting of hydrogen, C 1-6 Alkyl and halogenated C 1-6 alkyl group; preferably each R b are independently selected from hydrogen or C 1-6 Alkyl; preferably each R b is hydrogen;

[0517] X 1a Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-; preferably X 1a Selected from-NR b -, -O-, -S-; preferably X 1a Selected from-NR b - or -O-; preferably X 1a -NR b -;

[0518] Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1aSelected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclic group containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6Alkylene-maleimide, oxirane-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0519] X 2a For-(CR c R d ) n -; preferably X 2a For-(CR c H) n -; preferably X 2a -(CH2) n -; preferably X 2a -(CH2) n -; wherein n is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably n is 1; preferably X 2a is -CH2-;

[0520] Each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 6-10 Aryl; preferably each R c and R d are independently selected from hydrogen or C 1-6 Alkyl; preferably each R c and R d are independently hydrogen;

[0521] R e Selected from the group consisting of: C 1-12 Alkylene, C 2-12 Alkenylene, C 2-12 Alkynylidene, C 6-10 Arylene, 3 to 6 membered heterocyclylene, 5 to 6 membered heteroarylene and C 3-6 Cycloalkylene; preferably R eSelected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylidene, C 6-10 Arylene, 3 to 6 membered heterocyclylene, 5 to 6 membered heteroarylene and C 3-6 Cycloalkylene; preferably R e Selected from the group consisting of: 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 Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene and C 3-6 Cycloalkylene; preferably R e C 1-4 Alkylene or C 2-4 Alkenylene; preferably R e C 2-4 Alkenylene or C 1-3 Alkylene; preferably R e C 2-4 Alkenylene; preferably R e C 2-3 alkenylene;

[0522] R f C 1-20 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-16 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-14 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-10 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 alkylene;

[0523] R g is selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl; preferably R g is N-maleimide or N-maleimideoxy; preferably R g is N-maleimide;

[0524] W 1aSelected from-NR b Z 2a 、-R a OR a Preferably W 1a Selected from-NR b Z 2a or -R a Preferably W 1a Selected from the group consisting of: -NHZ 2a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: -NHCO-R a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a 、C 1-6 Alkyl, C 1-6 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a Preferably W 1a -NHCO-C 1-12 Alkyl; preferably W 1a -NHCO-C 1-10 Alkyl; preferably W 1a -NHCO-C 1-8 Alkyl; preferably W 1a -NHCO-C 1-6 alkyl;

[0525] Z 2a Selected from the group consisting of: hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-10 Alkyl, C 1-10 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a、C 1-8 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl and C 1-8 Alkylcarbonyl; preferably Z 2a Selected from the group consisting of hydrogen, C 1-8 Alkyl and C 1-8 Alkylcarbonyl group; preferably Z 2a C 1-8 alkylcarbonyl;

[0526] Y 1a is a moiety having formula (A), or is selected from -OR a 、-R a or -NR a R b ;

[0527]

[0528] Preferably Y 1a is a moiety having formula (A), or is -OR a or -NHR a ; preferably Y 1a is a moiety having formula (A), or is selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -O-CO-C 1-12Alkyl, -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 having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1a is a moiety having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1a is a moiety having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1a is a moiety having formula (A),

[0529] Ar 2 C 6-10 aryl or 5- to 10-membered heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 C 6-10 aryl or a 6-membered heteroaryl containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl; wherein the phenyl group may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl;

[0530] Each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylidene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NRb C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R zb independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R zb are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R zb is hydrogen;

[0531] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-; preferably X 1b Selected from-NR b -, -O-, -S-; preferably X 1b Selected from-NR b - or -O-; preferably X 1b -NR b -;

[0532] Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1bSelected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6Alkylene-maleimide, oxirane-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0533] X 2b For-(CR c R d ) m -; preferably X 2b For-(CR c H) m -; preferably X 2b -(CH2) m -; preferably X 2b -(CH2) m -; wherein m is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably m is 1; preferably X 2b is -CH2-; and

[0534] Y 1b Selected from OR a 、-NR b R a or R a ; preferably Y 1b For-OR a or -NHR a ; preferably Y 1b Selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 Selected from the group consisting of: -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 Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1b For-OC 1-10 Alkyl or -NH-C 1-10 alkyl.

[0535] 6. A compound according to any one of statements 1 to 2, 5, wherein

[0536] Ar 1 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R za Substituted, preferably the aryl or heteroaryl may be unsubstituted or substituted by one, two, three, four R za replace;

[0537] Y 1a is a moiety having formula (A), or is selected from -OR a 、-R a or -NR a R b ;Ar 2 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more Rzb Substituted; preferably, the aryl or heteroaryl may be unsubstituted or substituted by one, two, three, four R zb replace;

[0538] where R za 、R zb 、R a 、R b has the same meaning as defined in any one of Statements 1 to 2 and 5.

[0539] 7. A compound according to any one of statements 1 to 2, 5 to 6, wherein

[0540] Ar 1 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 C 6-10 aryl or a 6-membered heteroaryl containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 is phenyl; wherein the phenyl group may be unsubstituted or substituted by one or more R za Substituted; preferably Ar 1 is phenyl;

[0541] Each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R za independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R za are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R za For hydrogen,

[0542] Y 1a is a moiety having formula (A), or is selected from -OR a 、-R a or -NR a R b ; preferably Y 1a is a moiety having formula (A);

[0543]

[0544] Ar 2 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 C 6-10 aryl or a 6-membered heteroaryl containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl; wherein the phenyl group may be unsubstituted or substituted by one or more Rzb Substituted; preferably Ar 2 is phenyl;

[0545] Each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R zb independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R zbare independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R zb For hydrogen.

[0546] 8. A compound according to any one of Statements 3 or 4, wherein

[0547] R 1a 、R 2a 、R 3a and R 4a Each independently is R za ;

[0548] Each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylidene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each Rza Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R za independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R za are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R za For hydrogen,

[0549] Each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylidene and -R f1 -R g1 ; wherein said C 1-20 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-20 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the C 6-10 Aryl-C 2-6 Alkenylene, the C 6-10 Aryl-C 2-6 Alkyne, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 5 to 10 membered heteroaryl-C 2-6 Alkenylene, the 5 to 10 membered heteroaryl-C 2-6 Alkyne, the 3 to 10 membered heterocyclic group-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 2-6Alkenylene, the 3 to 10 membered heterocyclic group-C 2-6 Alkynylidene, the C 3-6 Cycloalkyl-C 1-6 Alkylene, the C 3-6 Cycloalkyl-C 2-6 Alkenylene and the C 3-6 Cycloalkyl-C 2-6 Each of the alkynylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halogenated, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R h Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R a1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R b1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R c1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R f1 C 1-20 Alkylene, wherein the C 1-20 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-20 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C1-6 Alkylene, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene and -R f1 -R g1 wherein said C 1-18 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-18 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halogenated, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 1-6 Alkylcarbonyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-10 Alkylene, wherein the C 1-10 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-10 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene and -R f1 -R g1 wherein said C 1-16 Alkyl, the C 2-16 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 3 to 6 membered heterocyclic group, the 5 to 6 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 6 membered heteroaryl-C 1-6 Alkylene, the 3 to 6 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-8 Alkylene, wherein the C 1-8 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-8 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, halogenated C 1-6Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 5- to 6-membered heterocyclic group 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 said C 1-15 Alkyl, the C 2-15 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 5- to 6-membered heterocyclic group containing at least one N or O, the 5- to 6-membered heteroaryl containing at least one N and the C 3-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3-5-membered heterocyclic group containing at least one N or one O, C 5-6 Cycloalkyl and -R f1 -R g1 wherein said C 1-15 Alkyl, the C 2-10 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-10Alkylcarbonyl, the phenyl, the 6-membered heteroaryl containing at least one N, the 3 to 5-membered heterocyclic group containing at least one N or one O, and the C 5-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, 3- to 4-membered heterocyclic group containing at least one O, phenyl, -R f1 -R g1 ; wherein said C 1-15 Alkyl, the C 2-8 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-8 Each of the alkylcarbonyl group, the 3- to 4-membered heterocyclic group containing at least one O, and the phenyl group may be unsubstituted or replaced by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 , halogenated, C 1-6 Alkyl and halogenated C 1-6 Alkyl; R h Selected from hydrogen or C 1-6Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O groups; R g1 is hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, oxirane alkyl, C 1-8 Alkylcarbonyl and -R f1 -R g1 wherein said C 1-15 Alkyl, the C 2-6 alkenyl, the oxirane alkyl and the C 1-8 Each of the alkylcarbonyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O groups; R g1 is hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane alkyl; wherein said C 1-15 Alkyl, the C 2-6 Each of the alkenyl group and the oxirane group may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-4 Alkyl; R h Selected from hydrogen or C 1-4 Alkyl; R a1 Selected from hydrogen or C 1-4 Alkyl; R b1 Selected from hydrogen or C 1-4 Alkyl; R c1 Selected from hydrogen or C 1-4 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O groups; R g1 is hydrogen or C 1-4 Alkyl; for example, each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, halogenated C 1-6 Alkyl, C 1-12Alkylcarbonyl, C 2-18 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C1-6 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; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-15 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 5- to 6-membered heterocyclic group containing at least one N or O, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 5-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-8 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 alkylcarbonyl, 3 to 4 membered heterocyclic group containing at least one O and phenyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C1-15 Alkyl, C 2-6 Alkenyl, oxirane and C 1-8 Alkylcarbonyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane;

[0550] Each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6-membered heterocyclic group containing at least one N, 5 to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 6-10 Aryl; preferably each R b independently selected from the group consisting of hydrogen, C 1-6 Alkyl and halogenated C 1-6 alkyl group; preferably each Rb are independently selected from hydrogen or C 1-6 Alkyl; preferably each R b is hydrogen;

[0551] X 1a -NR b -;

[0552] Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclic group containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1aSelected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0553] X 2a For-(CR c R d ) n -; preferably X 2a For-(CR c H) n -; preferably X 2a -(CH2) n -; preferably X 2a -(CH2) n -; wherein n is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably n is 1; preferably X 2a is -CH2-;

[0554] Each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl, C 3-6Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, C 6-10 Aryl-C 2-6 Alkenylene, C 6-10 Aryl-C 2-6 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R c and R d Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 6-10 Aryl; preferably each R c and R d are independently selected from hydrogen or C 1-6 Alkyl; preferably each R c and R d are independently hydrogen;

[0555] R e Selected from the group consisting of: C 1-12 Alkylene, C 2-12 Alkenylene, C 2-12 Alkynylidene, C 6-10 Arylene, 3 to 6 membered heterocyclylene, 5 to 6 membered heteroarylene and C 3-6 Cycloalkylene; preferably R e Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylidene, C 6-10 Arylene, 4- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene and C 3-6 Cycloalkylene; preferably R e Selected from the group consisting of: 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 Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene and C 3-6 Cycloalkylene; preferably R e C 1-4 Alkylene or C 2-4 Alkenylene; preferably R e C 2-4 Alkenylene or C 1-3 Alkylene; preferably R e C 2-4 Alkenylene; preferably R e C 2-3 alkenylene;

[0556] R f C1-20 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-16 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-14 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-10 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 alkylene;

[0557] R g Selected from hydrogen, C 1-20 alkyl, N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl; preferably R g For hydrogen, C 1-10 Alkyl, N-maleimido or N-maleimidooxy; preferably R g For hydrogen, C 1-6 Alkyl, N-maleimido;

[0558] W 1a Selected from-NR b Z 2a 、-R a OR a Preferably W 1a Selected from-NR b Z 2a or -R a Preferably W 1a Selected from the group consisting of: -NHZ 2a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: -NHCO-R a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: NHCO-R a , hydrogen, C 1-6Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a 、C 1-6 Alkyl, C 1-6 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a Preferably W 1a -NHCO-C 1-12 Alkyl; preferably W 1a -NHCO-C 1-10 Alkyl; preferably W 1a -NHCO-C 1-8 Alkyl; preferably W 1a -NHCO-C 1-6 alkyl;

[0559] Z 2a Selected from the group consisting of hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably Z 2a Selected from the group consisting of hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-10 Alkyl, C 1-10 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl and C 1-8 Alkylcarbonyl; preferably Z 2a Selected from the group consisting of hydrogen, C 1-8 Alkyl and C 1-8 Alkylcarbonyl group; preferably Z 2a C 1-8 alkylcarbonyl;

[0560] Y 1a is a moiety having formula (A), or is selected from -OR a 、-R a or -NR a R b ;

[0561]

[0562] Preferably Y 1a is a moiety having formula (A), or is -ORa or -NHR a ; preferably Y 1a is a moiety having formula (A), or is selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 having formula (A), or is selected from the group consisting of: -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 having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1a is a moiety having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1a is a moiety having formula (A), or is selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1a is a moiety having formula (A),

[0563] Ar 2 C6-10 aryl or 5- to 10-membered heteroaryl; wherein each of the aryl or heteroaryl groups may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 C 6-10 aryl or a 6-membered heteroaryl containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl; wherein the phenyl group may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl;

[0564] Each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylidene, -OR a , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b-glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4Alkoxy; preferably each R zb independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R zb are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R zb is hydrogen;

[0565] X 1b Selected from-NR b -, -O-, -S-, SO2-O- or -SO-O-; preferably X 1b Selected from-NR b -, -O-, -S-; preferably X 1b Selected from-NR b - or -O-; preferably X 1b -NR b -;

[0566] Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6Alkenylene and C 3-6 Cycloalkyl-C 2-6 Alkyne; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0567] X 2b For-(CR c R d ) m -; preferably X 2b For-(CR c H) m -; preferably X 2b -(CH2) m -; preferably X 2b -(CH2) m -; wherein m is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably m is 1; preferably X 2bis -CH2-; and

[0568] Y 1b Selected from OR a 、-NR b R a or R a ; preferably Y 1b For-OR a or -NHR a ; preferably Y 1b Selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 Selected from the group consisting of: -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 Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y1b For-OC 1-10 Alkyl or -NH-C 1-10 alkyl.

[0569] 9. A compound according to any one of Statements 1 to 8, wherein

[0570] Y 1a is a moiety having formula (A), or is selected from -OR a 、-R a or -NR a R b ;

[0571] Ar 2 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably, the aryl or heteroaryl may be unsubstituted or substituted by one, two, three, four R zb replace;

[0572] where R za 、R zb 、R a 、R b has the same meaning as defined in any one of Statements 1 to 8.

[0573] 10. A compound according to any one of Statements 1 to 9, wherein

[0574] Each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R zaIndependently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R za Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R za independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R za are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R za For hydrogen,

[0575] Y 1a is a moiety having formula (A), or is selected from -OR a 、-R a or -NR a R b ;

[0576] Ar 2 C 6-10 Aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of said aryl or said heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 C 6-10 aryl or a 6-membered heteroaryl containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl; wherein the phenyl group may be unsubstituted or substituted by one or more R zb Substituted; preferably Ar 2 is phenyl;

[0577] Each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; Preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably each R zb Independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably each R zb independently selected from hydrogen, halo and C 1-4 alkyl group; preferably each R zb are independently selected hydrogen, halo or C 1-3 Alkyl; preferably each R zb For hydrogen.

[0578] 11. A compound according to any one of Statements 1-10, which has structural formula (II);

[0579]

[0580] where Y 1a is a moiety having formula (B), or is selected from OR a 、R a NR a R b ,

[0581]

[0582] where R 1a 、R 2a 、R 3a and R 4a Each independently is R za ; and R 1b 、R 2b 、R 3b and R 4b Each independently is R zb ,and

[0583] where 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 of Statements 1 to 4;

[0584] Preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b and R 4b are each independently selected from the group consisting of 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 ; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b are each independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl, C 2-6 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 Alkyne, 5- to 10-membered heteroaryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 2-6 Alkenylene, 5 to 10 membered heteroaryl-C 2-6 Alkyne, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 3 to 10 membered heterocyclyl-C 2-6 Alkenylene, 3 to 10 membered heterocyclyl-C 2-6 Alkynylidene, C 3-6 Cycloalkyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 2-6 Alkenylene, C 3-6 Cycloalkyl-C 2-6 Alkynylidene, -OR a 、-SR a 、-S(O)R a 、-NR a R b and -NR b C(O)R a ; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4bare each independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, 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 ; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b are each independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, C 3-6 Cycloalkyl, -OR a 、-NR a R b and -NR b C(O)R a ; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b are each independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and -OR a ; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b are each independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and halogenated C 1-6 Alkoxy; preferably R 1a、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b are each independently selected from the group consisting of hydrogen, halo, C 1-4 Alkyl, halogenated C 1-4 Alkyl and halogenated C 1-4 Alkoxy; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b Each independently selected from hydrogen, halo and C 1-4 The group of alkyl groups; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b Each independently selected from hydrogen, halo or C 1-3 Alkyl; preferably R 1a 、R 2a 、R 3a 、R 4a 、R 1b 、R 2b 、R 3b 、R 4b are each independently hydrogen.

[0585] 12. A compound according to any one of statements 1 to 2, 5 to 11, wherein

[0586] Each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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 1-6Alkylene; wherein the C 1-20 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-20 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0587] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; wherein the C 1-18 Alkyl, the C 2-18 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10aryl, the 3 to 6 membered heterocyclic group, the 5 to 6 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 6 membered heteroaryl-C 1-6 Alkylene, the 3 to 6 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0588] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group 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, the C 2-6 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 3 to 6 membered heterocyclic group containing at least one N or one O, the 5 to 6 membered heteroaryl containing at least one N and the C 3-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0589] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; wherein the C 1-15 Alkyl, the C 2-6 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-10 Alkylcarbonyl, the phenyl, the 6-membered heteroaryl containing at least one N, the 3 to 6-membered heterocyclic group containing at least one N or one O, and the C 5-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0590] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, 3 to 5 membered heterocyclic group containing at least one N or one O and phenyl; wherein said C 1-15 Alkyl, the C 2-6 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-8Each of the alkylcarbonyl group, the 3- to 5-membered heterocyclic group containing at least one N or one O, and the phenyl group may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0591] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, and C 1-8 Alkylcarbonyl; wherein the C 1-15 Alkyl, the C 2-6 alkenyl, the 3 to 4 membered heterocyclic group containing at least one O and the C 1-8 Each of the alkylcarbonyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0592] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane alkyl; wherein said C 1-15 Alkyl, the C 2-4 Each of the alkenyl group and the oxirane group may be unsubstituted or substituted by one or more R za1Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-4 Alkyl; R a1 Selected from hydrogen or C 1-4 Alkyl; R b1 Selected from hydrogen or C 1-4 Alkyl; R c1 Selected from hydrogen or C 1-4 alkyl;

[0593] For example, each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 alkylcarbonyl, 3 to 5 membered heterocyclic group containing at least one N or one O and phenyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, and C 1-8 Alkylcarbonyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane;

[0594] Each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 6-10 Aryl, 3 to 10 membered heterocyclyl, 3 to 6 membered heterocyclyl-C 1-6 Alkylene, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 3 to 6 membered heterocyclic group-C 1-6 Alkylene, 5- to 6-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclic group containing at least one O-C 1-6 Alkylene and C 6-10 Aryl; preferably each R b independently selected from the group consisting of hydrogen, C 1-6 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-4 Alkylene and halogenated C 1-6 Alkyl; preferably each R b independently selected from hydrogen, oxiranealkyl-C 1-2 Alkylene or C 1-6 Alkyl; preferably each R b is hydrogen;

[0595] X 1a Selected from-NR b - or -O-; preferably X 1a -NR b -;

[0596] Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-ORb 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclic group containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、--CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C1-6 Alkylene-maleimide, oxirane-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, C 1-8 Alkylcarbonyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene and C 2-4 alkenylcarbonyl;

[0597] X 2a For-(CR c H) n -; preferably X 2a -(CH2) n -; preferably X 2a -(CH2) n -; wherein n is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably n is 1; preferably X 2a is -CH2-;

[0598] Each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably each R cIndependently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 6-10 Aryl; preferably each R c are independently selected from hydrogen or C 1-6 Alkyl; preferably each R c is hydrogen;

[0599] R e Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylidene, C 6-10 Arylene, 3 to 6 membered heterocyclylene, 5 to 6 membered heteroarylene and C 3-6 Cycloalkylene; preferably R e Selected from the group consisting of: 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 Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene and C 3-6 Cycloalkylene; preferably R e C 1-4 Alkylene or C 2-4 Alkenylene; preferably R e C 2-4 Alkenylene or C 1-3 Alkylene; preferably R e C 2-4 Alkenylene; preferably R e C 2-3 alkenylene;

[0600] R f C 1-20 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-16 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-14 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably Rf C 1-10 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 alkylene;

[0601] R g is selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl; preferably R g is N-maleimide or N-maleimideoxy; preferably R g is N-maleimide;

[0602] W 1a Selected from-NR b Z 2a or -R a Preferably W 1a Selected from the group consisting of: -NHZ 2a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: -NHCO-R a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a 、C 1-6 Alkyl, C 1-6 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a Preferably W 1a -NHCO-C 1-12 Alkyl; preferably W 1a -NHCO-C 1-10 Alkyl; preferably W 1a -NHCO-C 1-8Alkyl; preferably W 1a -NHCO-C 1-6 alkyl;

[0603] Z 2a Selected from the group consisting of: hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-10 Alkyl, C 1-10 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl and C 1-8 Alkylcarbonyl; preferably Z 2a Selected from the group consisting of hydrogen, C 1-8 Alkyl and C 1-8 Alkylcarbonyl group; preferably Z 2a C 1-8 alkylcarbonyl;

[0604] Y 1a is a moiety having formula (A) or (B), or is -OR a or -NHRa ; preferably Y 1a is a moiety having formula (A) or (B), or Y 1a Selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 having formula (A) or (B), or is selected from the group consisting of: -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 having formula (A) or (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1a is a moiety having formula (A) or (B), or Y 1a Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1a is a moiety having formula (A) or (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1a is a moiety having formula (B),

[0605] X 1b Selected from-NR b - or -O-; preferably X 1b -NR b -;

[0606] Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1bSelected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 5 membered heterocyclyl containing at least one O-C1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 4 membered heterocyclic group containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, C 1-8 Alkyl, oxirane alkyl-C 1-4 Alkylene, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, oxirane-C 1-2 Alkylene, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0607] X 2b For-(CR c H) m -; preferably X 2b -(CH2) m -; preferably X 2b -(CH2)m -; wherein m is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably m is 1; preferably X 2b is -CH2-; and

[0608] Y 1b For-OR a or -NHR a ; preferably Y 1b Selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 Selected from the group consisting of: -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 Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1b For-OC1-10 Alkyl or -NH-C 1-10 alkyl.

[0609] 13. A compound according to any one of Statements 1 to 12, wherein

[0610] Each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; wherein the C 1-20 Alkyl, the C 2-20 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 3 to 6 membered heterocyclic group, the 5 to 6 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 6 membered heteroaryl-C 1-6 Alkylene, the 3 to 6 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0611] Preferably each R aIndependently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; wherein the C 1-18 Alkyl, the C 2-18 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 Aryl, the 3 to 6-membered heterocyclic group containing at least one N or one O, the 3 to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, the 5- to 6-membered heteroaryl containing at least one N and the C 3-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0612] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; wherein the C 1-16 Alkyl, the C 2-16 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-10Alkylcarbonyl, the phenyl, the 6-membered heteroaryl containing at least one N, the 3 to 6-membered heterocyclic group containing at least one N or one O, and the C 5-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0613] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 alkylcarbonyl, a 3- to 5-membered heterocyclic group containing at least one O, and a phenyl group; wherein said C 1-15 Alkyl, the C 2-10 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-8 Each of the alkylcarbonyl group, the 3- to 5-membered heterocyclic group containing at least one O, and the phenyl group may be unsubstituted or replaced by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 alkyl;

[0614] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, and C 1-8 Alkylcarbonyl; wherein the C 1-15 Alkyl, the C 2-6 alkenyl, the 3 to 4 membered heterocyclic group containing at least one O and the C 1-8 Each of the alkylcarbonyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-10 Alkyl, C 2-6 alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, and C 1-8 Alkylcarbonyl; wherein the C 1-10 Alkyl, the C 2-6 alkenyl, the 3 to 4 membered heterocyclic group containing at least one O and the C 1-8 Each of the alkylcarbonyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-4 Alkyl; R a1 Selected from hydrogen or C 1-4 Alkyl; R b1 Selected from hydrogen or C 1-4 Alkyl; R c1 Selected from hydrogen or C 1-4 alkyl;

[0615] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane alkyl; wherein said C 1-15 Alkyl, the C2-4 Each of the alkenyl group and the oxirane group may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-4 Alkyl; R a1 Selected from hydrogen or C 1-4 Alkyl; R b1 Selected from hydrogen or C 1-4 Alkyl; R c1 Selected from hydrogen or C 1-4 Alkyl; for example, each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, C 2-20 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-16 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; preferably each R aIndependently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-10 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 alkylcarbonyl, 3 to 5 membered heterocyclic group containing at least one O and phenyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, and C 1-8 Alkylcarbonyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane;

[0616] Each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclyl, 3 to 10 membered heterocyclyl-C 1-6 Alkylene, 5- to 6-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl; preferably each R b independently selected from the group consisting of hydrogen, C 1-6 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-4 Alkylene and halogenated C 1-6 Alkyl; preferably each R b independently selected from hydrogen, oxiranealkyl-C 1-2 Alkylene or C 1-6 Alkyl; preferably each R b is hydrogen;

[0617] X 1a -NRb -;

[0618] Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 3 to 6 membered heterocyclic group-C 1-6 Alkylene, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、--CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1aSelected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-4 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0619] R e Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene, C 2-6 Alkynylidene, C 6-10 Arylene, 3 to 6 membered heterocyclylene, 5 to 6 membered heteroarylene and C 3-6 Cycloalkylene; preferably R e Selected from the group consisting of: 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 Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene and C 3-6 Cycloalkylene; preferably R e C 1-4 Alkylene or C 2-4 Alkenylene; preferably R e C 2-4 Alkenylene or C 1-3 Alkylene; preferably R e C 2-4 Alkenylene; preferably R e C 2-3 alkenylene;

[0620] R f C 1-20 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-16 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably Rf C 1-14 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-10 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 alkylene;

[0621] R g is selected from N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl; preferably R g is N-maleimide or N-maleimideoxy; preferably R g is N-maleimide;

[0622] X 2a -(CH2) n -; preferably X 2a -(CH2) n -; wherein n is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably n is 1; preferably X 2a is -CH2-;

[0623] W 1a Selected from the group consisting of: -NHZ 2a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: -NHCO-R a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a 、C 1-6 Alkyl, C 1-6 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a-NHCO-R a Preferably W 1a -NHCO-C 1-12 Alkyl; preferably W 1a -NHCO-C 1-10 Alkyl; preferably W 1a -NHCO-C 1-8 Alkyl; preferably W 1a -NHCO-C 1-6 alkyl;

[0624] Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-10 Alkyl, C 1-10 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 3 to 6 membered heterocyclic group-C 1-6 Alkylene, 5- to 6-membered heteroaryl and C 3-6 Cycloalkyl; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl and C 1-8 Alkylcarbonyl; preferably Z 2a Selected from the group consisting of hydrogen, C 1-8 Alkyl and C 1-8 Alkylcarbonyl group; preferably Z 2a C 1-8 alkylcarbonyl;

[0625] Y 1a is a moiety having formula (A) or (B), or is selected from the group consisting of: -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, -OC2-12 Alkynyl, -OC 6-10 Aryl, 3- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 having formula (A) or (B), or is selected from the group consisting of: -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 having formula (A) or (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1a is a moiety having formula (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1a is a moiety having formula (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1a is a moiety having formula (B),

[0626] X 1b -NR b -;

[0627] Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g, halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 3 to 6 membered heterocyclic group-C 1-6 Alkylene, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N or one O, 3- to 6-membered heterocyclic group containing at least one N or one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 6 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、--CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimido, halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-4 Alkylene, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-C2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0628] X 2b -(CH2) m -; preferably X 2b -(CH2) m -; wherein m is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably m is 1; preferably X 2b is -CH2-; and

[0629] Y 1b Selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene-O-, 5- to 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 Selected from the group consisting of: -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 Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y1b Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1b Selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1b For-OC 1-10 Alkyl or -NH-C 1-10 alkyl.

[0630] 14. A compound according to any one of Statements 1 to 13, wherein

[0631] Each R a Independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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, C 3-6 Cycloalkyl-C 1-6 Alkylene and -R f1 -R g1 ; wherein said C 1-20 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-20 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-20 Alkylene, wherein the C 1-20 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-20 alkyl;

[0632] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene, C 3-6 Cycloalkyl-C 1-6 Alkylene and -R f1 -R g1 ; wherein said C 1-18 Alkyl, the C 2-18 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 3 to 6 membered heterocyclic group, the 5 to 6 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 Alkylene, the 5 to 6 membered heteroaryl-C 1-6 Alkylene, the 3 to 6 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-15 Alkylene, wherein the C 1-15 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-15 alkyl;

[0633] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and -R f1 -R g1 ; wherein said C 1-16 Alkyl, the C 2-6 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 6-10 aryl, the 3 to 6 membered heterocyclic group containing at least one N or one O, the 5 to 6 membered heteroaryl containing at least one N and the C 3-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-10 Alkylene, wherein the C 1-10 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-10 alkyl;

[0634] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclic group containing at least one N or one O, C 5-6 Cycloalkyl and -R f1 -R g1 ; wherein said C 1-15 Alkyl, the C 2-6 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-10 Alkylcarbonyl, the phenyl, the 6-membered heteroaryl containing at least one N, the 3 to 6-membered heterocyclic group containing at least one N or one O, and the C 5-6 Each of the cycloalkyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-8 Alkylene, wherein the C 1-8 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-8 alkyl;

[0635] Preferably each Ra Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, 3 to 5 membered heterocyclic group containing at least one N or one O, phenyl and -R f1 -R g1 ; wherein said C 1-15 Alkyl, the C 2-6 Alkenyl, the halogenated C 1-6 Alkyl, the C 1-8 Each of the alkylcarbonyl group, the 3- to 5-membered heterocyclic group containing at least one N or one O, and the phenyl group may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-6 alkyl;

[0636] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-6 alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, C 1-8 Alkylcarbonyl and -R f1 -R g1 ; wherein said C 1-16 Alkyl, the C 2-6 alkenyl, the 3 to 4 membered heterocyclic group containing at least one O and the C 1-8 Each of the alkylcarbonyl groups may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-Rh 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-6 Alkyl; R a1 Selected from hydrogen or C 1-6 Alkyl; R b1 Selected from hydrogen or C 1-6 Alkyl; R c1 Selected from hydrogen or C 1-6 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-4 alkyl;

[0637] Preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 Alkenyl, oxirane and -R f1 -R g1 ; wherein said C 1-15 Alkyl, the C 2-4 Each of the alkenyl group and the oxirane group may be unsubstituted or substituted by one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h 、 -NR a1 R b1 、-R f1 -R g1 and C 1-6 Alkyl; R h Selected from hydrogen or C 1-4 Alkyl; R a1 Selected from hydrogen or C 1-4 Alkyl; R b1 Selected from hydrogen or C 1-4 Alkyl; R c1 Selected from hydrogen or C 1-4 Alkyl; R f1 C 1-6 Alkylene, wherein the C 1-6 The alkylene group may be interrupted by one or more O or S groups; R g1 is hydrogen or C 1-4 alkyl;

[0638] For example, each R aIndependently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-20 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-18 Alkyl, C 2-18 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-16 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, phenyl, 6-membered heteroaryl containing at least one N, 3- to 6-membered heterocyclic group containing at least one N or one O, and C 5-6 Cycloalkyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 Alkenyl, halogenated C 1-6 Alkyl, C1-8 alkylcarbonyl, 3 to 5 membered heterocyclic group containing at least one N or one O and phenyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-6 alkenyl, a 3- to 4-membered heterocyclic group containing at least one O, and C 1-8 Alkylcarbonyl; preferably each R a Independently selected from the group consisting of hydrogen, halo, C 1-15 Alkyl, C 2-4 alkenyl and oxirane;

[0639] Each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 6-10 Aryl, 3 to 10 membered heterocyclyl, 3 to 6 membered heterocyclyl-C 1-6 Alkylene, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 3 to 6 membered heterocyclic group-C 1-6 Alkylene, 5- to 6-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R b Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl; preferably each R b independently selected from the group consisting of hydrogen, C 1-6 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-4 Alkylene and halogenated C 1-6 Alkyl; preferably each R b independently selected from hydrogen, oxiranealkyl-C1-2 Alkylene or C 1-6 Alkyl; preferably each R b is hydrogen;

[0640] X 1a -NR b -;

[0641] Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, C 3-6Cycloalkyl, 3 to 6 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of hydrogen, -CO-R a 、--CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, C 1-8 Alkyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-4 Alkylene-, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1a Selected from the group consisting of: hydrogen, C 1-8 Alkylcarbonyl, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, oxirane-C 1-2 Alkylene and C 2-4 alkenylcarbonyl;

[0642] X 2a For-(CR c H) n -; preferably X 2a -(CH2) n-; preferably X 2a -(CH2) n -; wherein n is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably n is 1; preferably X 2a is -CH2-;

[0643] Each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group containing at least one N or one O, 5 to 6 membered heteroaryl containing at least one N and C 3-6 Cycloalkyl; preferably each R c Independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 1-6 Alkyl and C 6-10 Aryl; preferably each R c are independently selected from hydrogen or C 1-6 Alkyl; preferably each R c is hydrogen;

[0644] R e Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene, C2-6 Alkynylidene, C 6-10 Arylene, 3 to 6 membered heterocyclylene, 5 to 6 membered heteroarylene and C 3-6 Cycloalkylene; preferably R e Selected from the group consisting of: 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 Selected from the group consisting of: C 1-6 Alkylene, C 2-6 Alkenylene and C 3-6 Cycloalkylene; preferably R e C 1-4 Alkylene or C 2-4 Alkenylene; preferably R e C 2-4 Alkenylene or C 1-3 Alkylene; preferably R e C 2-4 Alkenylene; preferably R e C 2-3 alkenylene;

[0645] R f C 1-20 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-16 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-14 Alkylene, wherein the alkylene may be interrupted by one or more O or S; preferably R f C 1-10 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 Alkylene, wherein the alkylene may be interrupted by one or more O; preferably R f C 1-6 alkylene;

[0646] R g Selected from hydrogen, C 1-20 Alkyl, N-maleimido, N-maleimidooxy or hydrogen, C 1-10 Alkyl, N-maleimidooxycarbonyl; preferably R g For hydrogen, C 1-6 Alkyl, N-maleimido or N-maleimidooxy; preferably R g For hydrogen, C 1-4 Alkyl, N-maleimido;

[0647] W 1a Selected from-NR b Z 2a or -R a Preferably W 1a Selected from the group consisting of: -NHZ 2a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: -NHCO-R a , hydrogen, halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a Selected from the group consisting of: NHCO-R a , hydrogen, C 1-6 Alkyl, C 1-12 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a 、C 1-6 Alkyl, C 1-6 Alkylcarbonyl and C 6-10 Aryl; preferably W 1a -NHCO-R a Preferably W 1a -NHCO-C 1-12 Alkyl; preferably W 1a -NHCO-C 1-10 Alkyl; preferably W 1a -NHCO-C 1-8 Alkyl; preferably W 1a -NHCO-C 1-6 alkyl;

[0648] Z 2a Selected from the group consisting of hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C 1-6 Alkyl, C 1-12 Alkylcarbonyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 5- to 10-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 10-membered heteroaryl-C 1-6Alkylene, 3 to 10 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-10 Alkyl, C 1-10 Alkylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl, C 1-8 Alkylcarbonyl, C 6-10 Aryl, 3 to 6 membered heterocyclic group, 5 to 6 membered heteroaryl and C 3-6 Cycloalkyl; preferably Z 2a Selected from the group consisting of: hydrogen, -CO-R a 、C 1-8 Alkyl and C 1-8 Alkylcarbonyl; preferably Z 2a Selected from the group consisting of hydrogen, C 1-8 Alkyl and C 1-8 Alkylcarbonyl group; preferably Z 2a C 1-8 alkylcarbonyl;

[0649] Y 1a is a moiety having formula (A) or (B), or is -OR a or -NHR a ; preferably Y 1a is a moiety having formula (A) or (B), or Y 1a Selected from the group consisting of: -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- to 10-membered-O-heterocyclyl, 5- to 10-membered-O-heteroaryl, -OC 3-6 Cycloalkyl, C 6-10Aryl-C 1-6 Alkylene-O-, 5- to 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 having formula (A) or (B), or is selected from the group consisting of: -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 having formula (A) or (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl, -NHC 1-12 Alkyl, -OC 6-10 Aryl, -OC 3-6 Cycloalkyl; preferably Y 1a is a moiety having formula (A) or (B), or Y 1a Selected from the group consisting of: -OH, -NH2, -OC 1-12 Alkyl and -NHC 1-12 Alkyl; preferably Y 1a is a moiety having formula (A) or (B), or is selected from the group consisting of: -OH, -NH2, -OC 1-10 Alkyl and -NHC 1-10 Alkyl; preferably Y 1a is a moiety having formula (B),

[0650] X 1b Selected from-NR b - or -O-; preferably X 1b -NR b -;

[0651] Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-12 Alkyl, halogenated C1-6 Alkyl, C 1-12 Alkylcarbonyl, C 2-10 Alkenylcarbonyl, C 2-12 Alkenyl, C 2-12 Alkynyl, C 6-10 Aryl, 3- to 10-membered heterocyclic group, 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; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 2-10 Alkenyl, C 2-10 Alkynyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C 1-6 Alkylene, 5- to 6-membered heteroaryl-C 1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and C 3-6 Cycloalkyl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-10 Alkyl, halogenated C 1-6 Alkyl, C 1-10 Alkylcarbonyl, C 2-8 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group, 5- to 6-membered heteroaryl, C 3-6 Cycloalkyl, C 6-10 Aryl-C1-6 Alkylene, 3 to 6 membered heterocyclyl-C 1-6 Alkylene and 5- to 6-membered heteroaryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, 3- to 6-membered heterocyclic group containing at least one N, 3- to 6-membered heterocyclic group containing at least one O-C 1-6 Alkylene, 5- to 6-membered heteroaryl containing at least one N, C 3-6 Cycloalkyl and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, C 1-8 Alkylcarbonyl, C 2-6 Alkenylcarbonyl, C 6-10 Aryl, C 3-6 Cycloalkyl, 3 to 5 membered heterocyclyl containing at least one O-C 1-6 Alkylene and C 6-10 Aryl-C 1-6 Alkylene; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g 、-R f -R g , halogenated, C 1-8 Alkyl, halogenated C 1-6 Alkyl, 3 to 4 membered heterocyclic group containing at least one O-C 1-6 Alkylene, C 1-8Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-C 2-6 Alkenylene-CO-OR b 、-CO-R f -Maleimide, C 1-8 Alkyl, 3- to 4-membered heterocyclic group containing one O-C 1-6 Alkylene, C 1-8 Alkylcarbonyl and C 2-6 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, C 1-8 Alkyl, oxirane alkyl-C 1-4 Alkylene, C 1-8 Alkylcarbonyl and C 2-4 Alkenylcarbonyl; preferably Z 1b Selected from the group consisting of hydrogen, oxirane-C 1-2 Alkylene, -CO-C 2-4 Alkenylene-CO-OC 1-4 Alkyl, -CO-C 1-6 Alkylene-maleimide, C 1-8 Alkylcarbonyl and C 2-4 alkenylcarbonyl;

[0652] X 2b For-(CR c H) m -; preferably X 2b -(CH2) m -; preferably X 2b -(CH2) m -; wherein m is an integer selected from 1, 2 or 3; preferably 1 or 2; preferably m is 1; preferably X 2b is -CH2-; and

[0653] Y 1b For-OR a or -NHR a ; preferably Y 1b Selected from the group consisting of: -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, -OC2-12 Alkynyl, -OC 6-10 Aryl, 3- to 10-membe...

Claims

1. A compound of formula (II) or a tautomer, stereoisomer, hydrate, solvate, salt or polymorph thereof, wherein R 1a , R 2a , R 3a and R 4a Each independently is R za ; Each R za are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated -C-glycosyl, unacylated or acylated -S-glycosyl, -SR a 、-S(O)R a 、-NR a R b and-NR b C(O)R a ; Each R a independently selected from the group consisting of 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 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 may be unsubstituted or substituted with one or more R za1 Replace; Each R za1 Independently selected from the group consisting of: -COO-R h , -NR a1 R b1 , -R f1 -R g1 , halo, alkyl, haloalkyl, alkylcarbonyl, alkenyl and alkynyl; wherein 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 an alkylene group, wherein the alkylene group may be interrupted by one or more O or S; R g1 is hydrogen or alkyl; Each R b 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 For-NR b -; Z 1a Selected from the group consisting of: 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 For-(CR c R d ) n -; wherein n is an integer selected from 1, 2 or 3; Each R c and R d 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 an alkylene group, wherein the alkylene group may be interrupted by one or more O or S; R g is selected from hydrogen, alkyl, N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl; W 1a Selected from -NR b Z 2a , -R a OR a ; Z 2a Selected from the group consisting of: 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 Select from -OR a , -R a or -NR a R b , or Y 1a is a moiety having formula (A); in Ar 2 is aryl or heteroaryl; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R zb replace; Each R zb are independently selected from the group consisting of 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 , unacylated or acylated glycosyl, unacylated or acylated -O-glycosyl, unacylated or acylated -NR b -glycosyl, unacylated or acylated-C-glycosyl, unacylated or acylated-S-glycosyl, -C(O)-R a 、-S(O)R a 、-NR a R b and-NR b C(O)R a ; X 1b Selected from -NR b -, -O-, -S-, SO2-O- or -SO-O-; Z 1b Selected from the group consisting of: 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 For-(CR c R d ) m -; wherein m is an integer selected from 1, 2 or 3; and Y 1b Select from -OR a 、-NR b R a or -R a ; Provided that the compound is not: 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-Acetylaminophenyl)-2-amino-4-oxobutanoic acid; 2-Acetylamino-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; 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid methyl ester; 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-Acetylamino-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-Acetylamino-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-Acetylamino-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-ceramyl 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; 2-amino-4-(2-aminophenyl)-4-oxobutanoic acid butyl ester; (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid ethyl ester; (S)-2-amino-4-(2-aminophenyl)-4-oxobutanoic acid diacetate; (R)-2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid; (S)-2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid; 2-amino-4-(2-formylaminophenyl)-4-oxobutanoic acid; 2-Acetylamino-4-(2-acetylaminophenyl)-4-oxobutanoic acid methyl ester; 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-bioside); 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-glycoside; 2-Amino-4-(2-formylamino-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-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid; (R)-2-Acetylamino-4-(2-amino-5-chlorophenyl)-4-oxobutanoic acid; (S)-2-Acetylamino-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; (S-) methyl 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-Acetylamino-4-(2-acetylaminophenyl)-4-oxobutanoic acid; (S)-2-Formylamino-4-(2-formylaminophenyl)-4-oxobutanoic acid; 4-(2-Aminophenyl)-4-oxo-2-phenylbutanamide.

2. The compound according to claim 1, wherein Y 1a is a moiety having formula (A), or is selected from -OR a , -R a or -NR a R b ; Ar 2 C 6-10 aryl or 5- to 6-membered heteroaryl, preferably containing at least one N; wherein each of the aryl or heteroaryl may be unsubstituted or substituted by one or more R zb replace; Where R za , R zb , R a , R b Has the same meaning as defined in claim 1.

3. The compound according to any one of claims 1 to 2, where Y 1a is a moiety having formula (B), or is selected from OR a , R a NR a R b , Where R 1a , R 2a , R 3a and R 4a Each independently is R za ; and R 1b , R 2b , R 3b and R 4b Each independently is R zb ,and Where 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 claim 1.

4. A compound according to any one of claims 1 to 3, wherein Each R a are independently selected from the group consisting of hydrogen, halo, C 1-20 Alkyl, halogenated C 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 1-20 Alkyl, the halogenated C 1-6 Alkyl, the C 1-12 Alkylcarbonyl, the C 2-20 Alkenyl, the C 2-12 Alkynyl, the C 6-10 aryl, the 3 to 10 membered heterocyclic group, the 5 to 10 membered heteroaryl, the C 3-6 Cycloalkyl, the C 6-10 Aryl-C 1-6 alkylene, the 5 to 10 membered heteroaryl-C 1-6 Alkylene, the 3 to 10 membered heterocyclic group-C 1-6 The alkylene group and the C 3-6 Cycloalkyl-C 1-6 Each of the alkylene groups may be unsubstituted or substituted with one or more R za1 Replace; wherein each R za1 Independently selected from the group consisting of: -COO-R h , -NR a1 R b1 , -R f1 -R g1 , halogenated, C 1-6 Alkyl, halogenated C 1-6 Alkyl, C 1-6 Alkylcarbonyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R h Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R a1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R b1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R c1 Selected from the group consisting of: hydrogen, C 1-6 Alkyl, C 2-6 Alkenyl and C 2-6 Alkynyl; R f1 C 1-20 Alkylene, wherein the C 1-20 The alkylene group may be interrupted by one or more O or S; R g1 is hydrogen or C 1-20 alkyl; Each R b are independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 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 Cycloalkyl; X 1a For-NR b -; Z 1a Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g , -R f -R g , halogenated, C 1-12 Alkyl, halogenated C 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 Alkylene; R e Selected from the group consisting of: C 1-12 Alkylene, C 2-12 Alkenylene, C 2-12 Alkynylidene, C 6-10 arylene, 5- to 6-membered heterocyclylene, 5- to 6-membered heteroarylene and C 3-6 Cycloalkylene; R f C 1-20 Alkylene, wherein the alkylene may be interrupted by one or more O or S; R g is selected from hydrogen, alkyl, N-maleimido, N-maleimidooxy or N-maleimidooxycarbonyl; X 2a For-(CR c H) n -; wherein n is an integer selected from 1, 2 or 3; Each R c are independently selected from the group consisting of hydrogen, halo, C 1-6 Alkyl, halogenated C 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 Alkylene; W 1a Selected from -NR b Z 2a or -R a ; Z 2a Selected from the group consisting of: hydrogen, -CO-R a , halogenated, C 1-12 Alkyl, halogenated C 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 Alkylene; Y 1a is a moiety having formula (A) or (B), or -OR a or -NHR a ; X 1b Selected from -NR b - or -O-; preferably X 1b For-NR b -; Z 1b Selected from the group consisting of: hydrogen, -CO-R a 、-CO-R e -CO-OR b 、-CO-R f -R g , -R f -R g , halogenated, C 1-12 Alkyl, halogenated C 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 Alkylene; X 2b For-(CR c H) m -; wherein m is an integer selected from 1, 2 or 3; and Y 1b For-OR a or -NHR a .

5. A compound according to any one of claims 1 to 4, which has the structural formula (IIA12), (IIA13), (IIA14), (IIA15), (IIA16), (IIA17), (IIA18), (IIB1), (IIB2), (IIB3), (IIB4), (IIB5), (IIB6), (IIB7) or (IIB8), Where 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. A compound selected from the group consisting of:

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 UV-absorbing filter and / or high-energy visible light filter.

9. Compounds according to any one of claims 1 to 6 or at least one pharmaceutical composition according to claim 7 for use as UV-absorbing filters and / or high-energy visible light filters.

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 UV and high-energy visible radiation.

11. Compound according to any one of claims 1 to 6 or at least one pharmaceutical composition according to claim 7 for use in protection against UV and high energy visible radiation.

12. Use of at least one compound according to any one of claims 1 to 6 as a light stabilizer in consumer products to protect ingredients from photolytic degradation.

13. 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 a UV and / or high-energy visible light absorbing filter in consumer products, preferably in cosmetics.

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

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

16. The consumer product according to claim 15, wherein the consumer product is a cosmetic; preferably wherein the cosmetic is selected from the group comprising: sunscreen, moisturizer, makeup, lip balm, shampoo and conditioner.

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

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

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

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

21. A method for protecting the skin from UV and / or high energy visible radiation, said method 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. A method for protecting a composition from oxidation or imparting antioxidant properties to a composition, said method comprising adding to said composition at least one compound according to any one of claims 1 to 6.

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