US 12,458,705 B2
Antibody-oligonucleotide conjugates
Paul A. Jaminet, Cambridge, MA (US); Shou-Ching S. Jaminet, Cambridge, MA (US); and Edward Ha, Cambridge, MA (US)
Assigned to ANGIEX, INC., Cambridge, MA (US)
Appl. No. 17/251,316
Filed by ANGIEX, INC., Cambridge, MA (US)
PCT Filed Jun. 12, 2019, PCT No. PCT/US2019/036836
§ 371(c)(1), (2) Date Dec. 11, 2020,
PCT Pub. No. WO2019/241430, PCT Pub. Date Dec. 19, 2019.
Claims priority of provisional application 62/684,131, filed on Jun. 12, 2018.
Prior Publication US 2021/0260209 A1, Aug. 26, 2021
This patent is subject to a terminal disclaimer.
Int. Cl. C07K 16/00 (2006.01); A61K 45/06 (2006.01); A61K 47/68 (2017.01); A61P 35/00 (2006.01); C07K 16/28 (2006.01); C07K 19/00 (2006.01); C12N 15/113 (2010.01)
CPC A61K 47/6807 (2017.08) [A61K 45/06 (2013.01); A61K 47/6849 (2017.08); A61K 47/6855 (2017.08); A61P 35/00 (2018.01); C07K 16/28 (2013.01); C07K 19/00 (2013.01); C12N 15/113 (2013.01); C12N 15/1135 (2013.01); C12N 15/1137 (2013.01); C12N 15/1138 (2013.01); C07K 2317/55 (2013.01); C12N 2310/11 (2013.01); C12N 2310/14 (2013.01); C12N 2310/141 (2013.01); C12N 2310/3513 (2013.01); C12N 2320/32 (2013.01)] 12 Claims
 
1. A conjugate comprising an anti-TM4SF 1 antibody or an antigen binding fragment thereof conjugated to an oligonucleotide,
(1) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 94, 95, and 96, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 97, 98, and 99, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 92 and a light chain sequence of SEQ ID NO.: 93;
(2) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 1 and a light chain sequence of SEQ ID NO.: 2;
(3) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 6, 7, and 8, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 12, 13, and 14, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 3 and a light chain sequence of SEQ ID NO.: 9;
(4) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 18, 19, and 20, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 24, 25, and 26, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 15 and a light chain sequence of SEQ ID NO.: 21;
(5) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 30, 31, and 32, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 36, 37, and 38, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 27 and a light chain sequence of SEQ ID NO.: 33;
(6) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 54, 55, and 56, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 60, 61, and 62, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 51 and a light chain sequence of SEQ ID NO.: 57;
(7) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 66, 67, and 68, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 72, 73, and 74, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 63 and a light chain sequence of SEQ ID NO.: 69;
(8) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 78, 79, and 80, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 84, 85, and 86, respectively, and wherein optionally the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 75 and a light chain sequence of SEQ ID NO.: 81; or
(9) wherein the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 42, 43, and 44, respectively, and a light chain CDR1, CDR2, and CDR3 sequence of SEQ ID NO.: 48, 49, and 50, respectively, the anti-TM4SF1 antibody or an antigen binding fragment thereof comprises a heavy chain sequence of SEQ ID NO.: 39 and a light chain sequence of SEQ ID NO.: 45.