AMINO ACID DERIVATIVES FUNCTIONALIZED ON THE N-TERMINUS CAPABLE OF FORMING DRUG ENCAPSULATING MICROSPHERES AND USES THEREOF

• Main Authors: Chen, Delai, Love, Kevin Thomas, Anderson, Daniel Griffith, Alabi, Akinleye, Zhang, Yunlong, Vegas, Arturo Jose, Langer, Robert S, Chen, Yi, Dong, Yizhou
• Format: Patent
• Language: English
• Published: 16.11.2023
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; BEER; BIOCHEMISTRY; CHEMISTRY; COMPOSITIONS THEREOF; CULTURE MEDIA; ENZYMOLOGY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; MICROBIOLOGY; MICROORGANISMS OR ENZYMES; MUTATION OR GENETIC ENGINEERING; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; PROPAGATING, PRESERVING OR MAINTAINING MICROORGANISMS; SPIRITS; VINEGAR; WINE

Described herein are compounds and compositions that are characterized by the Markush formulae (I), (II), (III), (IV), (V), and (VI) underneath, where at least one terminal amino group is further functionalized by bearing a group of type (i), (ii), or (iii). Such compounds are obtained by reacting a terminal or internal amino group with epoxides, acrylates, or aldehydes bearing lipophilic groups. The resulting amino acid, peptide, polypeptide-lipids (named "APPLs" in the application) are deemed useful as drug delivery systems including nucleotide delivery to cells. Formulae (i), (ii), and (iii). See Fig. 1. WO 2013/063468 PCT/US2012/062222 £~ ~ ~-L3-0>1O ... Z aLa-A C) gW a... zLV-A2$io a;9 9L3-NNO 0 -)i~ aL h'AVO aiLa->iiO 12Z a -ASO ZaLB-AAO z O-QALOid WL --- $L OOOG~id ... ZL3-AAO z v->mli E Zc a 3W Z L3>i Ad L Z aLB-ANd ZaLa-H z (01 a a-H Ca C-Z La-v joiaua [GAO- U191~d IIJ GaJUvGN SUBTITTE HEE (RLa26