Polymer-oligonucleotide conjugates
AssigneePrimelink Biotherapeutics (Suzhou) Co., Ltd. Ltd.
InventorsMao YIN, Yingdong LU, Xiaohe SHI, Ganyuan XIAO, Ling XIN, Ya ZHANG, Qing ZHANG, Haitao PAN
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Abstract
A polymeric scaffold useful for conjugating with a targeting moiety to form a targeting moiety-polymer-oligonucleotide conjugate is described herein. Also disclosed is a targeting moiety-polymer-oligonucleotide conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their composition are also described.
Claims70
A polymeric scaffold of Formula (I) or Formula (II) 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 or —NH— 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 G1 and Za;
- each Za is independently an endosomal-lysosomal escaping moiety or a conjugation moiety;
- each ON is independently an oligonucleotide;
- 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 (III) or Formula (IV):
- 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 or —NH— moiety;
- Ba is branching moiety comprising a functional group WM connecting to —NH— moiety;
- each G′ is independently a functional group connecting LP to the linear polyglycerol;
- each LP is independently a drug release mechanism between G′ and Za;
- each Za is independently a lysosomal escaping moiety or a conjugation moiety;
- each ON is independently an oligonucleotide;
- 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.