# US 2020/0399350 A1 · Antibodies and antigen-binding fragments that specifically bind to microtubule-associated protein tau

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 2020/0399350 A1
- Document ID: US20200399350A1
- Status: Published application
- Kind: A1
- Application number: 16/514,770
- Filed: 2019-07-17
- Published: 2020-12-24
- Earliest claimed: 2014-06-26
- Assignees: Janssen Vaccines & Prevention B.V.
- Applicants: Janssen Vaccines & Prevention B.V.
- Inventors: Jehangir WADIA; Gabriel PASCUAL; Robert Anthony WILLIAMS; Katarina RADOSEVIC; Jaap GOUDSMIT
- Web page: https://patentgrep.com/patent/US20200399350A1

## CPC

- C07K 16/18: against material from animals or humans
- A61K 39/395: Antibodies (agglutinins A61K38/36 {; as drug carriers A61K47/50}); Immunoglobulins; Immune serum, e.g. antilymphocytic serum
- G01N 33/6896: {Neurological disorders, e.g. Alzheimer's disease}
- C07K 2317/21: from primates, e.g. man
- C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
- C07K 2317/30: characterized by aspects of specificity or valency
- C07K 2317/34: Identification of a linear epitope shorter than 20 amino acid residues or of a conformational epitope defined by amino acid residues
- C07K 2317/52: Constant or Fc region; Isotype
- C07K 2317/56: variable (Fv) region, i.e. VH and/or VL
- C07K 2317/565: Complementarity determining region [CDR]
- C07K 2317/567: Framework region [FR]
- C07K 2317/72: Increased effector function due to an Fc-modification
- C07K 2317/94: Stability, e.g. half-life, pH, temperature or enzyme-resistance
- G01N 2333/47: Assays involving proteins of known structure or function as defined in the subgroups
- G01N 2800/2821: Alzheimer
- 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)
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

The invention relates to antibodies and antigen-binding fragments that specifically bind to microtubule-associated protein tau. The invention also relates to diagnostic, prophylactic and therapeutic methods using anti-tau antibodies.

## Claims

### Claim 1

A monoclonal antibody, wherein the antibody binds tau deposits in human AD brain tissue,
wherein the antibody binds tau deposits in human AD brain tissue, but does not bind tau in normal human brain tissue and does not bind tau deposits in Progressive Supranuclear Palsy (“PSP”) brain tissue; and
wherein the antibody comprises an antigen-binding site of a VH of SEQ ID NO:87 and an antigen-binding site of a VL of SEQ ID NO:88.

### Claim 2 (depends on 1)

The antibody of claim 1, wherein the antibody comprises:
a naturally occurring human antigen-binding variable region that binds specifically to tau, and
a recombinant constant region of a human IgG1 antibody.

### Claim 3 (depends on 1)

The antibody of claim 1, wherein the antibody comprises:
naturally occurring human light and heavy chain variable regions from a human antibody, and
recombinant human IgG1 heavy and light chain constant regions.

### Claim 4 (depends on 1)

The antibody of claim 1, wherein the antibody comprises:
heavy and light chain variable regions from a naturally occurring human antibody, and recombinant human IgG1 heavy and light chain constant regions.

### Claim 5 (depends on 1)

The antibody of claim 1, wherein the antibody comprises:
heavy and light chain variable regions from a human antibody, and
recombinant human IgG1 heavy and light chain constant regions.

### Claim 6 (depends on 1)

The antibody of claim 1, wherein the antibody is selected from the group consisting of
a) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:175, a heavy chain CDR2 region comprising SEQ ID NO:176, and a heavy chain CDR3 region comprising SEQ ID NO:177, a light chain CDR1 region comprising SEQ ID NO:178, a light chain CDR2 region comprising SEQ ID NO:179 and a light chain CDR3 region comprising SEQ ID NO:180,
b) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:181, a heavy chain CDR2 region comprising SEQ ID NO:182, and a heavy chain CDR3 region comprising SEQ ID NO:183, a light chain CDR1 region comprising SEQ ID NO:172, a light chain CDR2 region comprising SEQ ID NO:173 and a light chain CDR3 region comprising SEQ ID NO:184,
c) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:185, a heavy chain CDR2 region comprising SEQ ID NO:186, and a heavy chain CDR3 region comprising SEQ ID NO:187, a light chain CDR1 region comprising SEQ ID NO:188, a light chain CDR2 region of comprising SEQ ID NO:173 and a light chain CDR3 region comprising SEQ ID NO:189,
d) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:190, a heavy chain CDR2 region comprising SEQ ID NO:191, and a heavy chain CDR3 region comprising SEQ ID NO:192, a light chain CDR1 region comprising SEQ ID NO:193, a light chain CDR2 region comprising SEQ ID NO:194 and a light chain CDR3 region comprising SEQ ID NO:195,
e) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:196, a heavy chain CDR2 region comprising SEQ ID NO:197, and a heavy chain CDR3 region comprising SEQ ID NO:198, a light chain CDR1 region comprising SEQ ID NO:199, a light chain CDR2 region comprising SEQ ID NO:173 and a light chain CDR3 region comprising SEQ ID NO:200,
f) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:213, a heavy chain CDR2 region comprising SEQ ID NO:214, and a heavy chain CDR3 region comprising SEQ ID NO:215, a light chain CDR1 region comprising SEQ ID NO:216, a light chain CDR2 region comprising SEQ ID NO:173 and a light chain CDR3 region comprising SEQ ID NO:217; NO:217,
g) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:213, a heavy chain CDR2 region comprising SEQ ID NO:214, and a heavy chain CDR3 region comprising SEQ ID NO:215, a light chain CDR1 region comprising SEQ ID NO:218, a light chain CDR2 region comprising SEQ ID NO:174 and a light chain CDR3 region comprising SEQ ID NO:217; NO:217, and
h) an antibody comprising a heavy chain CDR1 region comprising SEQ ID NO:219, a heavy chain CDR2 region comprising SEQ ID NO:220, and a heavy chain CDR3 region comprising SEQ ID NO:221, a light chain CDR1 region comprising SEQ ID NO:218, a light chain CDR2 region comprising SEQ ID NO:173 and a light chain CDR3 region comprising SEQ ID NO:217.

### Claim 7 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:95 and an antigen-binding site of a VL of SEQ ID NO:96.

### Claim 8 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:99 and an antigen-binding site of a VL of SEQ ID NO:100.

### Claim 9 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:103 and an antigen-binding site of a VL of SEQ ID NO:104.

### Claim 10 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:107 and an antigen-binding site of a VL of SEQ ID NO:108.

### Claim 11 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:111 and an antigen-binding site of a VL of SEQ ID NO:112.

### Claim 12 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:123 and an antigen-binding site of a VL of SEQ ID NO:124.

### Claim 13 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:127 and an antigen-binding site of a VL of SEQ ID NO:128.

### Claim 14 (depends on 1)

The antibody of claim 1, comprising an antigen-binding site of a VH of SEQ ID NO:131 and an antigen-binding site of a VL of SEQ ID NO:132.

### Claim 15 (depends on 1)

A method for the prophylaxis and/or treatment of a subject with Alzheimer's disease, or memory and/or cognitive disorders associated with tau, the method comprising utilizing the chimeric antibody of claim 1 or an antigen-binding fragment thereof for prophylaxis or treatment, or combination thereof, of Alzheimer's disease, or memory and/or cognitive disorders associated with tau.

### Claim 16 (depends on 1)

A method for diagnosing a subject for Alzheimer's disease, or memory and/or cognitive disorders associated with tau, the method comprising:
a) assaying the level of tau antigen in a biological sample from the subject utilizing the chimeric antibody of claim 1 or an antigen-binding fragment thereof.

### Claim 17 (depends on 16)

The method of claim 16, wherein the biological sample comprises peripheral blood, serum, plasma, urine, cerebrospinal fluid, tissue biopsy, surgical specimen, fine needle aspirates, autopsy material, cell culture supernatant, isolated cells, fermentation supernatant, or tissue homogenate.