# US 2018/0022804 A1 · HUMANIZED MONOCLONAL ANTIBODIES THAT TARGET VE-PTP (HPTP-Beta)

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- Number: US 2018/0022804 A1
- Document ID: US20180022804A1
- Status: Published application
- Kind: A1
- Application number: 15/654,289
- Filed: 2017-07-19
- Published: 2018-01-25
- Earliest claimed: 2016-07-20
- Assignees: Aerpio Therapeutics Inc.
- Applicants: Aerpio Therapeutics, Inc
- Inventors: Kevin Peters; Michael Allen Flynn
- Web page: https://patentgrep.com/patent/US20180022804A1

## CPC

- C07K 16/28: against receptors, cell surface antigens or cell surface determinants
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61P 35/00: Antineoplastic agents
- C07K 16/22: against growth factors {; against growth regulators}
- C07K 16/2896: {against molecules with a "CD"-designation, not provided for elsewhere}
- A61K 2039/505: {comprising antibodies}
- A61K 2039/507: {Comprising a combination of two or more separate antibodies}
- A61K 2039/54: {characterised by the route of administration}
- A61K 2039/545: {characterised by the dose, timing or administration schedule}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/33: Crossreactivity, e.g. for species or epitope, or lack of said crossreactivity
- C07K 2317/51: Complete heavy chain or Fd fragment, i.e. VH + CH1
- C07K 2317/515: Complete light chain, i.e. VL + CL
- C07K 2317/75: Agonist effect on antigen
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value
- 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)
- 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

## Abstract

The disclosure provides compositions and methods for the treatment of ocular conditions associated with angiogenesis comprising administering an antibody that targets a tyrosine phosphatase inhibitor in a subject.

## Claims

### Claim at position 1

1-56. (canceled)

### Claim 57

A compound comprising:
a) a heavy chain that comprises a sequence that is at least 80% identical to SEQ ID NO: 30; and
b) a light chain that comprises a sequence that is at least 80% identical to SEQ ID NO: 34.

### Claim 58 (depends on 57)

The compound of claim 57, wherein the heavy chain is at least 85% identical to SEQ ID NO: 30; and the light chain is at least 85% identical to SEQ ID NO: 34.

### Claim 59 (depends on 57)

The compound of claim 57, wherein the heavy chain is at least 90% identical to SEQ ID NO: 30; and the light chain is at least 90% identical to SEQ ID NO: 34.

### Claim 60 (depends on 57)

The compound of claim 57, wherein the heavy chain is at least 95% identical to SEQ ID NO: 30; and the light chain is at least 95% identical to SEQ ID NO: 34.

### Claim 61 (depends on 57)

The compound of claim 57, wherein the heavy chain is SEQ ID NO: 30 and the light chain is SEQ ID NO: 34.

### Claim 62 (depends on 57)

The compound of claim 57, wherein the compound inhibits a tyrosine phosphatase.

### Claim 63 (depends on 57)

The compound of claim 57, wherein the compound inhibits HPTP-β.

### Claim 64 (depends on 57)

The compound of claim 57, wherein the compound inhibits VE-PTP.

### Claim 65 (depends on 57)

The compound of claim 57, wherein the compound activates Tie2.

### Claim 66 (depends on 57)

The compound of claim 57, wherein the compound activates Akt.

### Claim 67 (depends on 57)

The compound of claim 57, wherein the compound binds an extracellular domain of HPTP-β.

### Claim 68 (depends on 57)

The compound of claim 57, wherein the compound binds the first FN3 repeat of an extracellular domain of HPTP-β.

### Claim 69 (depends on 68)

The compound of claim 68, wherein a binding affinity (KD) of the compound to the extracellular domain of HPTP-β is about 70 pM to about 70 nM.

### Claim at position 15

70-95. (canceled)

### Claim 96

A method of treating a condition in a subject in need thereof, the method comprising administering to the subject a therapeutically-effective amount of a compound, the compound comprising:
a) a heavy chain that comprises a sequence that is at least 80% identical to SEQ ID NO: 30; and
b) a light chain that comprises a sequence that is at least 80% identical to SEQ ID NO: 34.

### Claim 97 (depends on 96)

The method of claim 96, wherein the condition is an ocular condition.

### Claim 98 (depends on 96)

The method of claim 96, wherein the condition is diabetic retinopathy.

### Claim 99 (depends on 96)

The method of claim 96, wherein the condition is neovascularization.

### Claim 100 (depends on 96)

The method of claim 96, wherein the condition is vascular leak.

### Claim 101 (depends on 96)

The method of claim 96, wherein the condition is increased intraocular pressure.

### Claim 102 (depends on 96)

The method of claim 96, wherein the condition is ocular edema.

### Claim 103 (depends on 96)

The method of claim 96, wherein the condition is diabetic macular edema.

### Claim 104 (depends on 96)

The method of claim 96, wherein the condition is ocular hypertension.

### Claim 105 (depends on 96)

The method of claim 96, wherein the condition is ocular inflammation.

### Claim 106 (depends on 96)

The method of claim 96, wherein the administration is to an eye of the subject.

### Claim 107 (depends on 96)

The method of claim 96, wherein the administration is intravitreal.

### Claim 108 (depends on 96)

The method of claim 96, wherein the administration is subcutaneous.

### Claim 109 (depends on 96)

The method of claim 96, wherein the administration is topical.

### Claim 110 (depends on 96)

The method of claim 96, wherein the subject is a human.

### Claim 111 (depends on 96)

The method of claim 96, wherein the therapeutically-effective amount of the compound is from about 0.25 mg to about 200 mg.

### Claim 112 (depends on 96)

The method of claim 96, wherein the therapeutically-effective amount of the compound is from about 1 mg/kg to about 10 mg/kg.

### Claim 113 (depends on 96)

The method of claim 96, wherein the therapeutically-effective amount of the compound is from about 1 mg to about 50 mg.

### Claim 114 (depends on 96)

The method of claim 96, wherein the therapeutically-effective amount of the compound is from about 50 mg to about 200 mg.

### Claim 115 (depends on 96)

The method of claim 96, wherein the heavy chain is at least 85% identical to SEQ ID NO: 30; and the light chain is at least 85% identical to SEQ ID NO: 34.

### Claim 116 (depends on 96)

The method of claim 96, wherein the heavy chain is at least 90% identical to SEQ ID NO: 30; and the light chain is at least 90% identical to SEQ ID NO: 34.

### Claim 117 (depends on 96)

The method of claim 96, wherein the heavy chain is at least 95% identical to SEQ ID NO: 30; and the light chain is at least 95% identical to SEQ ID NO: 34.

### Claim 118 (depends on 96)

The method of claim 96, wherein the heavy chain is SEQ ID NO: 30 and the light chain is SEQ ID NO: 34.

### Claim 119 (depends on 96)

The method of claim 96, wherein the method inhibits a tyrosine phosphatase.

### Claim 120 (depends on 96)

The method of claim 96, wherein the method inhibits HPTP-β.

### Claim 121 (depends on 96)

The method of claim 96, wherein the method inhibits VE-PTP.

### Claim 122 (depends on 96)

The method of claim 96, wherein the method activates Tie2.

### Claim 123 (depends on 96)

The method of claim 96, wherein the method activates Akt.

### Claim 124 (depends on 96)

The method of claim 96, wherein the compound binds an extracellular domain of HPTP-β.

### Claim 125 (depends on 96)

The method of claim 96, wherein the compound binds the first FN3 repeat of an extracellular domain of HPTP-β.

### Claim 126 (depends on 125)

The method of claim 125, wherein a binding affinity (KD) of the compound to the extracellular domain of HPTP-β is about 70 pM to about 70 nM.