Patent ID: 11857635
Assignee: JENKEM TECHNOLOGY CO., LTD. (TIANJIN)
Field: Pharmaceuticals (Chemistry)
Classification: CPC A | IPC A

Claim 0:
1. A polyethylene glycol-linker-drug conjugate, having a structure as follows:

(PEG-X-L-Y)n-D  (IX)

wherein, PEG is a polyethylene glycol residue,
X is a linking group of PEG and L, which is selected from one or a combination of several of —(CH2)a—, —(CH2)aCO—, —(CH2)aOCO—, —(CH2)aNHCO—, —NH(CH2)aCO—, —(CH2)aSO2—, —O(CH2)a—, —O(CH2)aCO—, —O(CH2)aOCO—, —O(CH2)aNHCO— and —O(CH2)aSO2—, and a is an integer of 0 to 10,
Y is a linking group of L and D, which is selected from one or a combination of several of —(CH2)r—,, , —(CH2)rO—, —(CH2)rCO—, —(CH2)rNH—, —(CH2)rCONH—, —(CH2)rNHCO—, —(CH2)rSH—,, , and r is an integer of 0 to 10,
R17 and R18 are independently selected from —H, C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkyl and C4-10 alkylene cycloalkyl,
D is a bioactive agent containing m amido groups, and m is an integer of 1 to 500,
n is an integer, and 1≤n≤m,
L is a linker, having a structure as follows:, wherein, 1 is an integer of 1 to 5,
in the linker L-a, A is —COCH2NH—, —COCH(CH3)NH— or —COCH(CH(CH3)2)NH—;
in the linker L-b and L-c, A is one or a combination selected from amino acid residues, polypeptide residues,, , —NHCO(CH2)i, —CONH(CH2)i—, —(CH2)iNH— and —CO(CR15R16)iNH—, and i is an integer of 0 to 6,
R1-7 and R9-11 are independently selected from —H, —F, —Cl, —Br, —I, C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkyl, C1-6 alkenyl, C6-12 aryl, C6-12 aralkyl, C3-12 aromatic or non-aromatic heterocyclyl, C3-12 heterocyclic alkyl and —(CH2)l—O—Z,
wherein Z is selected from —H, —CH3, —C(CH3)3, —CH2OCH3, —COCH3, —COC(CH3)3, —CH2CH═CH2, —Si(CH3)3,, R8 and R12 are independently selected from C1-6 alkyl,
R13-16 are independently selected from —H, and C1-6 alkyl, and
B is a linking group —B1—B2—,
wherein, B1 is selected from —(CH2)j—, —NHCO(CH2)j— and —CONH(CH2)j—, and j is an integer of 0 to 6, and
B2 is selected from —C═O, —C═S, —O—, —S—, —C(O)O—, —C(O)S—, —C(S)O— and —S—S—.