US 11,806,405 B1
Immunoconjugates and methods
Xiaojun Han, San Diego, CA (US); Suvi Tuula Marjukka Orr, San Diego, CA (US); Kevin Duane Bunker, Escondido, CA (US); Peter Qinhua Huang, San Diego, CA (US); and Kimberlee Fischer, San Diego, CA (US)
Assigned to Zeno Management, Inc., San Diego, CA (US)
Filed by Zeno Management, Inc., San Diego, CA (US)
Filed on Sep. 28, 2022, as Appl. No. 17/936,346.
Application 17/936,346 is a continuation in part of application No. 17/812,869, filed on Jul. 15, 2022.
Claims priority of provisional application 63/267,471, filed on Feb. 2, 2022.
Claims priority of provisional application 63/203,347, filed on Jul. 19, 2021.
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/68 (2017.01); A61K 31/4745 (2006.01); A61K 47/55 (2017.01); C07K 16/18 (2006.01); A61K 39/00 (2006.01)
CPC A61K 47/6803 (2017.08) [A61K 31/4745 (2013.01); A61K 47/55 (2017.08); A61K 47/6851 (2017.08); C07K 16/18 (2013.01); A61K 2039/505 (2013.01)] 42 Claims
 
1. An immunoconjugate having Formula (I),
Ab-[S-L1-L2-L3-L4-L5-L6-L7-D]n  (I)
wherein:
Ab is an antibody or an antigen-binding fragment thereof;
L1 is

OG Complex Work Unit Chemistry
L2 is absent,

OG Complex Work Unit Chemistry
Z1 and Z2 are each individually hydrogen, halogen, NO2, —O—(C1-C6 alkyl), or C1-C6 alkyl;
L3 is —(CH2)n1-C(═O)— or —(CH2CH2O)n1-(CH2)n1C(═O)—;
each n1 is independently an integer of 0 to 12;
L4 is a tetrapeptide residue;
L5 is absent or —[NH(CH2)n2]n3-;
n2 is an integer of 0 to 6;
n3 is an integer of 0 to 2;
L6 is absent or

OG Complex Work Unit Chemistry
L7 is absent,

OG Complex Work Unit Chemistry
D is a drug moiety; and
n is an integer from 1 to 10, wherein said antibody or binding fragment thereof is selected from:
an antibody or binding fragment thereof comprising:
a heavy chain comprising:
VHCDR 1 comprising an amino acid sequence of SEQ ID NO:29;
VHCDR 2 comprising an amino acid sequence of SEQ ID NO:30; and
VHCDR 3 comprising an amino acid sequence of SEQ ID NO:31; and
a light chain comprising:
VLCDR 1 comprising an amino acid sequence of SEQ ID NO:36;
VLCDR 2 comprising an amino acid sequence of DAS; and
VLCDR 3 comprising an amino acid sequence of SEQ ID NO:38;
wherein the antibody or antigen-binding fragment specifically binds to the extracellular domain of human receptor tyrosine kinase like orphan receptor 1 (ROR1).