# US 10,869,931 B2 · Polyethylene glycol-modified angiogenesis inhibitor HM-1 and application thereof

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- Number: US 10,869,931 B2
- Document ID: US10869931B2
- Status: Granted
- Kind: B2
- Application number: 16/090,251
- Filed: 2017-03-07
- Published: 2019-04-18
- Granted: 2020-12-22
- Earliest claimed: 2016-04-06
- Assignees: Nanjing Anji Biological Technology Co., Ltd.
- Applicants: Nanjing Anji Biological Technology Co.,Ltd
- Inventors: Hanmei Xu
- Web page: https://patentgrep.com/patent/US10869931B2

## CPC

- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 38/10: Peptides having 12 to 20 amino acids {(A61K38/043 - A61K38/046 take precedence)}
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 27/02: Ophthalmic agents
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- C07K 7/08: having 12 to 20 amino acids (gastrins C07K14/595; somatostatins C07K14/655; melanotropins C07K14/68)
- 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)

## Abstract

A polyethylene glycol-modified angiogenesis inhibitor HM-1 and its application are disclosed. The polypeptide sequence is mPEG-Arg-Gly-Ala-Asp-Arg-Ala-Gly-Gly-Gly-Gly-Arg-Gly-Asp (SEQ ID NO: 1), and mPEG . . . is chosen from mPEG-SC, mPEG2-NHS, mPEG-ALD or mPEG-bALD, with a molecular weight range of 500˜40000. The polypeptide has been modified by polyethylene glycol, has the capacity to inhibit vascular endothelial cell migration and integrin affinity and binding, and can be used for the prevention and treatment of tumors, various types of inflammation, and neovascular eye diseases. The polyethylene glycol-modified angiogenesis inhibitor disclosed by the present invention is prepared by a synthetic method.

## Claims

### Claim 1

A polyethylene glycol-modified angiogenesis inhibitor HM-1, comprising the sequence of mPEG-Arg-Gly-Ala-Asp-Arg-Ala-Gly-Gly-Gly-Gly-Arg-Gly-Asp (SEQ ID NO: 1), wherein the mPEG is mPEG-ALD, with molecular weight ranging from 500 to 40,000 Dalton.

### Claim 2 (depends on 1)

The polyethylene glycol-modified angiogenesis inhibitor HM-1 according to claim 1, comprising the following sequence:
mPEG-ALD20k-Arg-Gly-Ala-Asp-Arg-Ala-Gly-Gly-Gly-Gly-Arg-Gly-Asp (SEQ ID NO: 1).

### Claim 3 (depends on 2)

A medicament for treating tumors, comprising the polyethylene glycol-modified angiogenesis inhibitor HM-1 from claim 2.

### Claim 4 (depends on 3)

The medicament of claim 3, wherein the tumors comprise a primary or secondary cancer, melanoma, hemangiomas, and sarcomas originating from human head, neck, brain, thyroid, esophagus, pancreas, lung, liver, stomach, breast, kidney, gallbladder, colon or rectum, ovary, cervix, uterus, prostate, bladder, and testis.

### Claim 5 (depends on 1)

A medicament for treating tumors, comprising the polyethylene glycol-modified angiogenesis inhibitor HM-1 from claim 1.

### Claim 6 (depends on 5)

The medicament of claim 5, wherein the tumors comprise a primary or secondary cancer, melanoma, hemangiomas, and sarcomas originating from human head, neck, brain, thyroid, esophagus, pancreas, lung, liver, stomach, breast, kidney, gallbladder, colon or rectum, ovary, cervix, uterus, prostate, bladder, and testis.