PATENT CLAIM ANALYSIS

Application Number: 16017489
Application Type: Utility
Filing Date: 2018-06
Publication Date: 2018-10
Patent Classification: ["530", "387100"]

Abstract:
Provided herein are antibodies, or antigen-binding portions thereof, that bind to T-cell immunoglobulin and mucin-domain containing-3 (TIM3) protein. Also provided are uses of these antibodies, or antigen-binding portions thereof, in therapeutic applications, such as treatment of cancer. Further provided are cells that produce the antibodies, or antigen-binding portions thereof, polynucleotides encoding the heavy and/or light chain regions of the antibodies, or antigen-binding portions thereof, and vectors comprising the polynucleotides encoding the heavy and/or light chain regions of the antibodies, or antigen-binding portions thereof.

Claim (Index 54):
The antibody or antigen binding portion thereof, of any of  claims 1 - 53 , wherein the antibody or antigen binding portion thereof has one or more of the following properties:\n (1) binding to soluble human TIM3, e.g., with a KD of 10 nM or less (e.g., 0.01 nM to 10 nM), e.g., as measured by Biacore; (2) binding to soluble cynomolgus TIM3, e.g., with a KD of 100 nM or less (e.g., 0.01 nM to 100 nM), e.g., as measured by Biacore; (3) binding to membrane bound human TIM3, e.g., with an EC50 of 1 ug/mL or less (e.g., 0.01 ug/mL to 1 ug/mL), e.g., as measured by flow cytometry; (4) binding to membrane bound human TIM3, e.g., with a K D  of 1 nM or less (e.g., 0.01 nM to 10 nM), e.g., as measured by Scatchard analysis; (5) binding to membrane bound cynomolgus TIM3, e.g., with an EC50 of 20 ug/mL or less (e.g., 0.01 ug/mL to 20 ug/mL), e.g., as measured by flow cytometry; (6) binding to membrane bound cynomolgus TIM3, e.g., with a K D  of 1 nM or less (e.g., 0.01 nM to 10 nM), e.g., as measured by Scatchard analysis; (7) inducing or enhancing T cell activation (e.g., by blocking or reducing the inhibitory effect of TIM3), as evidenced by (i) increased IFN-\u03b3 production in TIM3-expressing T cells (e.g., Th1 cells or TILs) and/or (ii) enhanced proliferation of TIM3-expressing T cells (e.g., Th1 cells or TILs); (8) stimulating T cell proliferation in a mixed lymphocyte reaction (MLR) assay; (9) inhibiting the binding of phosphatidylserine to TIM3, e.g., as measured by PS-hTIM3 \u201cin-tandem\u201d blocking assay; (10) not internalizing or downregulating cell surface TIM3 when binding to TIM3 on cells; (11) binding to one of the following regions of human TIM3 extracellular domain (SEQ ID NO: 290): (a) CPVFECG (SEQ ID NO: 296); (b) RIQIPGIMND (SEQ ID NO: 298); (c) CPVFECG and RIQIPGIMND (SEQ ID NOs: 296 and 298, respectively); and (d) WTSRYWLNGDFR (SEQ ID NO: 297); (12) having reduced binding to human TIM3 in which one or more of amino acids L48, C58, P59, V60, F61, E62, C63, G64, W78, S80, R81, W83, L84, G86, D87, R89, D104, R111, Q113, G116, M118 and D120 (as numbered in SEQ ID NO: 286 ( FIG. 20 )) is substituted with another amino acid relative to binding to wildtype human TIM3; (13) competing in either direction or both directions for binding to human TIM3 with an antibody comprising VH and VL domains of any one of 13A3, 3G4, 17C3, 17C8, 9F6, 8B9, 8C4, or TIM3.7, TIM3.8, TIM3.10, TIM3.11, TIM3.12, TIM3.13, TIM3.14, TIM3.15, TIM3.16, TIM3.17, and TIM3.18; (14) binding to human TIM3 regions 49VPVCWGKGACPVFE 62  (SEQ ID NO: 367) and  111 RIQIPGIMNDEKFNLKL 127  (SEQ ID NO: 368) as determined by HDX-MS (15) having the heavy chain and/or light chain variable regions interact with at least 5, 10, 15, 20 or all of the following amino acids of human TIM3: P50, V51, C52, P59, V60, F61, E62, C63, G64, N65, V66, V67, L68, R69, D71, E72, D74, R111, Q113, G116, I117, M118, D120, and optionally T70 and/or I112, as determined by X-ray crystallography (e.g., described in the Examples; numbering per SEQ ID NO: 286 ( FIG. 20 )); and/or (16) (a) having reduced binding to human TIM3 in which 1, 2, 3, 4, 5, 6, 7, 8 or 9 of amino acids C58, P59, F61, E62, C63, R111, D120, and optionally D104 and Q113 (numbering per SEQ ID NO: 286 ( FIG. 20 )) are substituted with another amino acid relative to binding to wildtype human TIM3; (b) binding to  49 VPVCWGKGACPVFE 62  (SEQ ID NO: 367),  111 RIQIPGIMNDEKFNLKL 127  (SEQ ID NO: 368) and  119 NDEKFNLKL 127  (SEQ ID NO: 373), as determined by HDX-MS, as described in the Examples; and/or (c) competing with or cross-blocking with the binding to human TIM3 of 13A3 or TIM3.18.IgG1.3.

Metadata:
- Claim Count in Document: 45.0
- Percentile: 94.0
- Lexical Diversity: 2.08511
- Patent Class: 530.0
- Transitional Phrase Type: open
- Component Type: 1
- Foreign Priority: False
- Related Applications: ['15649380', '15520638', '13478786', '14732082', '15474731']

Analysis Scores:
- 35 USC 101 Eligibility (BERT): 0.737040181042121
- 35 USC 102 Novelty (BERT): 0.6966712511980573
- Combined Prediction Score: 0.7330032880577146
- Mean Citation Score: 596.4244480000001
- Max Citation Score: 837.39594
- Similarity Product: 695.1513689856005

Labels:
- Claim Label 101: 1
- Claim Label 102: 1
- Claim Label 103: 1
- Claim Label 112: 1
- Combined Label: 1
- Label 101 Adjusted: 0

Dataset: test