# US 2019/0167804 A1 · Glucocorticoid receptor agonist and immunoconjugates thereof

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- Number: US 2019/0167804 A1
- Document ID: US20190167804A1
- Status: Published application
- Kind: A1
- Application number: 16/204,825
- Filed: 2018-11-29
- Published: 2019-06-06
- Earliest claimed: 2017-12-01
- Assignees: AbbVie Inc.
- Applicants: AbbVie Inc.
- Inventors: Adrian Hobson; Michael McPherson; Wendy Waegell; Christian Goess; Axel Hernandez, JR.; Lu Wang; Lu Wang; Christopher C. Marvin; Ling C. Santora
- Web page: https://patentgrep.com/patent/US20190167804A1

## CPC

- A61K 47/6803: {Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates}
- A61K 38/191: {Tumor necrosis factors [TNF], e.g. lymphotoxin [LT], i.e. TNF-beta}
- A61K 47/6845: {the antibody targeting a cytokine, e.g. growth factors, VEGF, TNF, a lymphokine or an interferon}
- A61K 47/6889: {Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment}
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- C07K 16/241: {Tumor Necrosis Factors}
- C07K 16/249: {Interferons}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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

Provided herein are glucocorticoid receptor agonist immunoconjugates, glucocorticoid receptor agonists, and methods of using the same.

## Claims

### Claim 1

An antibody drug conjugate comprising:
(a) an anti-TNFα antibody comprising a heavy chain set forth as SEQ ID NO: 3 and a light chain set forth as SEQ ID NO: 4; and
(b) a glucocorticoid receptor agonist comprising a radical represented by the formula:
wherein the antibody is conjugated to the glucocorticoid receptor agonist via a linker represented by the formula:

### Claim 2 (depends on 1)

The antibody drug conjugate of claim 1, according to the formula:
wherein A is the antibody and n is an integer from 1-10.

### Claim 3 (depends on 2)

The antibody drug conjugate of claim 2, wherein n is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10.

### Claim 4 (depends on 2)

The antibody drug conjugate of claim 2, wherein n is 4.

### Claim 5 (depends on 2)

The antibody drug conjugate of claim 2, wherein n is 2.

### Claim 6 (depends on 4)

A pharmaceutical composition comprising the antibody drug conjugate of claim 4 and a pharmaceutically acceptable carrier.

### Claim 7 (depends on 4)

A method of treating a condition selected from rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, plaque psoriasis, ulcerative colitis, adult Crohn's disease, pediatric Crohn's disease, uveitis, hidradenitis suppurativa, and juvenile idiopathic arthritis in a subject, comprising administering an effective amount of the antibody drug conjugate of claim 4 to the subject.

### Claim 8 (depends on 4, 6)

A kit comprising:
(a) a container comprising the antibody drug conjugate of claim 4 or the pharmaceutical composition of claim 6; and
(b) a label or package insert on or associated with the one or more containers, wherein the label or package insert indicates that the antibody drug conjugate or pharmaceutical composition is used for treating a condition selected from rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis, plaque psoriasis, ulcerative colitis, adult Crohn's disease, pediatric Crohn's disease, uveitis, hidradenitis suppurativa, and juvenile idiopathic arthritis.

### Claim 9 (depends on 4)

A method of delivering a glucocorticoid receptor agonist to a TNFα-expressing cell, comprising the step of contacting the cell with the antibody drug conjugate of claim 4.

### Claim 10

An antibody drug conjugate according to the formula:
wherein A is adalimumab and n is 4.

### Claim 11

An antibody drug conjugate according to the formula:
wherein A is adalimumab and n is 2.