Polymer-drug conjugates
AssigneePrimelink Biotherapeutics (Shenzhen) Co., Ltd
InventorsMao YIN, Yingdong LU, Xiaohe SHI, Ganyuan XIAO, Junqi ZHU, Qingli ZHOU, Ling XIN, Jinchen DONG, Yu SHEN, Jiani YU, Qing ZHANG
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Abstract
A polymeric scaffold is used for conjugating with a targeting moiety to form a targeting moiety-polymer-drug conjugate. A targeting moiety-polymer-drug conjugate is prepared from the scaffold. Compositions comprise the conjugate. Methods of treating various disorders with the conjugates or the composition comprise administering the conjugates or the composition.
Claims71
A polymeric scaffold of Formula (I) useful to conjugate with a targeting moiety:
- wherein:
- the polymeric scaffold comprises linear polyglycerol;
- L is a linking moiety comprising a functional group Wp that is capable of forming a covalent bond with the targeting moiety;
- Ma is a stretcher connecting L to Ba moiety;
- Ba is a branching moiety comprising a functional group WM connecting to —NH— moiety;
- each G1 is independently a functional group connecting LP to the linear polyglycerol;
- each LP is independently a drug release mechanism between a therapeutic agent moiety D and G1;
- each D is independently a therapeutic agent moiety;
- each G2 is independently a functional group capable of converting into a charged state;
- n is an integer from 0 to 1000;
- m is an integer from 0 to 1000;
- p is an integer from 0 to 1000;
- and
- q is an integer from 0 to 1000.
The polymeric scaffold of any one of preceding claims, wherein L is
A polymeric scaffold of Formula (II):
- wherein,
- the polymeric scaffold comprises linear polyglycerol;
- L is a linking moiety comprising a functional group Wp that is capable of forming a covalent bond with the targeting moiety;
- Ma is a stretcher connecting L to Ba moiety;
- Ba is a branching moiety comprising a functional group WM connecting to —NH— moiety;
- each G2 is independently a functional group capable of converting into a charged state;
- each G3 independently comprises a functional group capable of reacting with a reactive group in a drug release mechanism to connect the drug release mechanism to the linear polyglycerol;
- n is an integer from 0 to 1000;
- m is an integer from 0 to 1000;
- p is an integer from 0 to 1000;
- and
- q is an integer from 0 to 1000.
A polymeric scaffold of Formula (III):
- wherein,
- the polymeric scaffold comprises linear polyglycerol;
- PBRM is a targeting moiety;
- each La is independently a divalent moiety connecting the targeting moiety to Ma;
- each Ma is independently a stretcher connecting La to Ba moiety;
- Ba is branching moiety comprising a functional group WM connecting to —NH— moiety;
- each G1 is independently a functional group connecting LP to the linear polyglycerol;
- each LP is independently a drug release mechanism between a fragment of a therapeutic agent D and G1;
- each D is independently a fragment of a therapeutic agent;
- each G2 is independently a functional group capable of converting into a charged state;
- n is an integer from 0 to 1000;
- m is an integer from 0 to 1000;
- p is an integer from 0 to 1000;
- q is an integer from 0 to 1000;
- and
- s is an integer from 1 to 8.
Dependencies are inferred from the claim text.