# US 10,478,507 B2 · Peptide-based multiple-drug delivery vehicle

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- Number: US 10,478,507 B2
- Document ID: US10478507B2
- Status: Granted
- Kind: B2
- Application number: 15/752,909
- Filed: 2016-10-18
- Published: 2018-09-06
- Granted: 2019-11-19
- Earliest claimed: 2015-10-18
- Assignees: Ariel-University Research and Development Company Ltd.
- Applicants: Ariel-University Research and Development Company Ltd.
- Inventors: Gary Gellerman
- Web page: https://patentgrep.com/patent/US10478507B2

## CPC

- A61K 47/641: {Branched, dendritic or hypercomb peptides}
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 47/65: Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
- A61P 31/18: for HIV
- C07K 1/1077: {by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids}
- C07K 1/113: without change of the primary structure
- C07K 2/00: Peptides of undefined number of amino acids; Derivatives thereof
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- Y02A 50/30: Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)
- Y02A: TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE

## Abstract

A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

## Claims

### Claim 1

A process of preparing a molecular structure represented by Formula I:
wherein:
AA1 and AAn are each independently an amino acid residue;
n is an integer equal to or larger than 2 and denoting the number of said amino acid residues in the structure;
TM is a targeting moiety;
L0, L11, L12, Ln1 and Ln2 are each independently a linking moiety;
D1, Dn and Dn+1 are each independently a bioactive agent or absent, provided that at least two of D1, Dn and Dn+1 are each independently a bioactive agent; and
at least one bioactive agent of said D1, Dn and Dn+1 is different than at least one other bioactive agent of said D1, Dn and Dn+1, the process comprising:
binding a targeting moiety to a solid support;
linking said AA1 to said targeting moiety;
optionally attaching said D1 to said AA1;
linking AA2 to said AA1;
optionally attaching D2 to said AA2;
optionally attaching D2+1 to said AA2;
when n is larger than 2, linking said AAn to said AA2;
optionally attaching Dn to said AAn;
optionally attaching Dn+1 to said AAn; and
detaching said targeting moiety from said solid support to thereby obtain the molecular structure.

### Claim 2 (depends on 1)

The process of claim 1, wherein said linking and/or said attaching is effected via a functional group on said targeting moiety, or a functional group on a side chain of said amino acid, or on an alpha carbon of said amino acid.

### Claim 3 (depends on 2)

The process of claim 2, wherein said linking and/or said attaching to said functional group further includes removing a protection group on said functional group.