# US 11,433,140 B2 · Specific antibody drug conjugates (ADCs) having KSP inhibitors

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- Number: US 11,433,140 B2
- Document ID: US11433140B2
- Status: Granted
- Kind: B2
- Application number: 16/472,682
- Filed: 2017-12-18
- Published: 2019-12-05
- Granted: 2022-09-06
- Earliest claimed: 2016-12-21
- Assignees: Bayer Pharma Aktiengesellschaft
- Applicants: Bayer Pharma Aktiengesellschaft
- Inventors: Hans-Georg Lerchen; Anne-Sophie Rebstock; Beatrix Stelte-Ludwig; Dennis Kirchhoff; Sandra Berndt; Lisa Dietz; Stephan Märsch; Stefanie Hammer
- Web page: https://patentgrep.com/patent/US11433140B2

## CPC

- A61K 47/65: Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
- A61K 39/3955: {against proteinaceous materials, e.g. enzymes, hormones, lymphokines}
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61K 47/6803: {Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates}
- A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant}
- 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 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07K 16/2866: {against receptors for cytokines, lymphokines, interferons}
- A61K 2039/505: {comprising antibodies}
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/73: Inducing cell death, e.g. apoptosis, necrosis or inhibition of cell proliferation
- 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

Specific binder-drug conjugates (ADCs) of kinesin spindle protein inhibitors, effective metabolites of these ADCs, processes for preparing these ADCs, the use of these ADCs for the treatment and/or prevention of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases, are described.

## Claims

### Claim 1

An antibody-drug conjugate (ADC) of formula (I):
or a salt, a solvate, or a salt of the solvate thereof;
wherein:
n is 1 to 8;
AK is an anti-CD123 antibody comprising a variable region of the heavy chain (VH) comprising the variable CDR1 sequence of the heavy chain (H-CDR1), as shown by SEQ ID NO: 12, the variable CDR2 sequence of the heavy chain (H CDR2), as shown by SEQ ID NO: 13 and the variable CDR3 sequence of the heavy chain (H-CDR3), as shown by SEQ ID NO: 14, and a variable region of the light chain (VL) comprising the variable CDR1 sequence of the light chain (L CDR1), as shown by SEQ ID NO: 16, the variable CDR2 sequence of the light chain (L-CDR2), as shown by SEQ ID NO: 17 and the variable CDR3 sequence of the light chain (L-CDR3), as shown by SEQ ID NO: 18, or is an antigen-binding fragment thereof, wherein the antibody or the antigen-binding fragment thereof is attached via a sulfur atom of a cysteine side group.

### Claim 2 (depends on 1)

The antibody-drug conjugate according to claim 1, or a salt, a solvate, or a salt of the solvate thereof, wherein n is 2 to 8.

### Claim 3 (depends on 1)

The antibody-drug conjugate according to claim 1, or a salt, a solvate or a salt of the solvate thereof wherein n is 4 to 8.

### Claim 4 (depends on 1)

The antibody-drug conjugate according to claim 1, or a salt, a solvate, or a salt of the solvate thereof, wherein AK is an anti-CD123 antibody comprising a variable region of the heavy chain (VH) as shown in SEQ ID NO: 11 and a variable region of the light chain (VL) as shown in SEQ ID NO: 15, or is an antigen-binding fragment thereof.

### Claim 5 (depends on 1)

The antibody-drug conjugate according to claim 1, or a salt, a solvate, or a salt of the solvate thereof, wherein AK is an anti-CD123 antibody comprising a region of the heavy chain as shown in SEQ ID NO: 19 and a region of the light chain as shown in SEQ ID NO: 20, or is an antigen-binding fragment thereof.

### Claim 6 (depends on 1)

A pharmaceutical composition comprising at least one antibody-drug conjugate (ADC) according to claim 1, or a salt, a solvate, or a salt of the solvate thereof, in combination with an inert, non-toxic, pharmaceutically suitable auxiliary.

### Claim 7 (depends on 1)

A method for treatment of hyperproliferative and/or angiogenic disorders which overexpress CD123 or CXCR5, comprising administering to a patient in need thereof an effective amount of an antibody-drug conjugate according to claim 1, or a salt, a solvate, or a salt of the solvate thereof.

### Claim 8 (depends on 1)

A method for treatment of cancer and tumours which overexpress CD123 or CXCR5, comprising administering to a human in need thereof an effective amount of an antibody-drug conjugate according to claim 1, or a salt, a solvate, or a salt of the solvate thereof.

### Claim 9 (depends on 1)

A method for treatment of cancer and tumours which overexpress CD123 or CXCR5, comprising administering to a human in need thereof an effective amount of an antibody-drug conjugate according to claim 1, or a salt, a solvate, or a salt of the solvate thereof, in combination with one or more therapeutic approaches for cancer immunotherapy or with one or more active compounds directed against a molecular target of cancer immunotherapy.