# US 2021/0330803 A1 · Protein-antiviral compound conjugates

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- Number: US 2021/0330803 A1
- Document ID: US20210330803A1
- Status: Published application
- Kind: A1
- Application number: 17/156,525
- Filed: 2021-01-23
- Published: 2021-10-28
- Earliest claimed: 2020-01-24
- Assignees: Regeneron Pharmaceuticals, Inc.
- Applicants: Regeneron Pharmaceuticals, Inc.
- Inventors: Alina BAUM; Thomas NITTOLI
- Web page: https://patentgrep.com/patent/US20210330803A1

## CPC

- A61K 47/6801: {Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent}
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems
- A61K 47/6803: {Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates}
- A61K 47/6839: {the antibody targeting material from viruses}
- A61K 47/6841: {the antibody targeting a RNA virus}
- 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)

## Abstract

Provided herein are compounds, compositions, and methods for the treatment of diseases and disorders associated with influenza, including VX-787 and derivatives thereof, baloxavir and derivatives thereof, and baloxavir marboxil and derivatives thereof, and protein (e.g., antibody) drug conjugates thereof.

## Claims

### Claim 1

An antibody-drug conjugate comprising an anti-influenza antibody or antigen-binding fragment thereof conjugated to an antiviral compound.

### Claim 2 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the anti-influenza antibody or antigen-binding fragment thereof is conjugated to the antiviral compound via a linker.

### Claim 3 (depends on 1)

The antibody-drug conjugate of claim 1 having the following structure
wherein Ab is an anti-influenza antibody or an antigen binding fragment thereof;
L is a linker;
P is an antiviral compound; and
k is an integer from one to thirty.

### Claim 4 (depends on 3)

The antibody-drug conjugate of claim 3, wherein P is an influenza inhibitor.

### Claim 5 (depends on 3)

The antibody-drug conjugate of claim 3, wherein P is a polymerase inhibitor.

### Claim 6 (depends on 3)

The antibody-drug conjugate of claim 3, wherein P is VX-787, a derivative thereof, or a residue thereof.

### Claim 7 (depends on 3)

The antibody-drug conjugate of claim 3, wherein P is baloxavir, a derivative thereof, or a residue thereof.

### Claim 8 (depends on 3)

The antibody-drug conjugate of claim 3, wherein Ab is an anti-hemagglutinin antibody or an antigen binding fragment thereof.

### Claim 9 (depends on 8)

The antibody-drug conjugate of claim 8, wherein P is an influenza inhibitor.

### Claim 10 (depends on 8)

The antibody-drug conjugate of claim 8, wherein P is a polymerase inhibitor.

### Claim 11 (depends on 8)

The antibody-drug conjugate of claim 8, wherein P is VX-787, a derivative thereof, or a residue thereof.

### Claim 12 (depends on 8)

The antibody-drug conjugate of claim 8, wherein P is baloxavir, a derivative thereof, or a residue thereof.

### Claim 13

A compound having the following structure
wherein
L is a linker;
BA is a binding agent; and
k is an integer from one to thirty.

### Claim 14 (depends on 13)

The compound of claim 13, selected from the group consisting of
wherein
BA is an antibody or an antigen binding fragment thereof; and
k is an integer from one to thirty.

### Claim 15 (depends on 13)

The compound of claim 13, wherein BA is an antibody or antigen-binding fragment thereof.

### Claim at position 16

16-24. (canceled)

### Claim 25 (depends on 3)

The antibody-drug conjugate of claim 3, wherein Ab or BA is mAb11729.

### Claim 26 (depends on 1)

A pharmaceutical composition comprising the antibody-drug conjugate or compound of claim 1, and a pharmaceutically acceptable excipient, carrier, or diluent.

### Claim 27

(canceled)

### Claim 28 (depends on 1)

A method for treatment, prophylaxis, reduction, or inhibition of a disease, disorder, or condition associated with an infection in a subject, comprising administering to the subject an effective amount of an antibody-drug conjugate of claim 1.

### Claim at position 21

29-34. (canceled)

### Claim 35 (depends on 1)

A method for treatment, prophylaxis, reduction, or inhibition of an influenza infection in a subject comprising administering to the subject an effective amount of an antibody-drug conjugate of claim 1.

### Claim at position 23

36-57. (canceled)

### Claim 58

A linker-antiviral compound having the following structure
or a pharmaceutically acceptable salt thereof, wherein
L is a linker; and
RG is a reactive moiety.

### Claim 59 (depends on 58)

The linker-antiviral compound of claim 58, wherein the linker-payload is
or a pharmaceutically acceptable salt thereof,
wherein
SP1 and SP2, when present, are spacer groups;
RG is a moiety reactive with an antibody or an antigen binding fragment thereof;
each AA is an amino acid; and
n is an integer from one to ten.

### Claim 60 (depends on 59)

The linker-antiviral compound of claim 59, selected from the group consisting of

### Claim 61 (depends on 58)

An antibody-drug conjugate comprising an antibody, or an antigen binding fragment thereof, where the antibody or antigen binding fragment thereof is conjugated to a compound of claim 58.

### Claim 62 (depends on 61)

The antibody-drug conjugate of claim 61, wherein the conjugated compound is selected from
wherein L is a linker.

### Claim 63 (depends on 58)

A method of preparing an antibody-drug conjugate comprising contacting a binding agent with a linker-antiviral compound of claim 58.

### Claim at position 30

64-72. (canceled)

### Claim 73 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the antibody or antigen binding fragment thereof comprises a LCVR further comprising an amino acid sequence set forth in SEQ ID NO: 26; and a HCVR further comprising an amino acid sequence set forth in SEQ ID NO: 18.

### Claim 74 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the antibody or antigen binding fragment thereof is the antibody mAb11729.

### Claim 75 (depends on 1)

The antibody-drug conjugate of claim 1, wherein the antibody comprises
(a) a HCDR1 that comprises an amino acid sequence set forth in SEQ ID NO: 20;
(b) a HCDR2 that comprises an amino acid sequence set forth in SEQ ID NO: 22;
(c) a HCDR3 that comprises an amino acid sequence set forth in SEQ ID NO: 24;
(d) a LCDR1 that comprises an amino acid sequence set forth in SEQ ID NO: 28;
(e) a LCDR2 that comprises an amino acid sequence set forth in SEQ ID NO: 30; and
(f) a LCDR3 that comprises an amino acid sequence set forth in SEQ ID NO: 32.