Patent ID: 11857637
Assignee: R.P. SCHERER TECHNOLOGIES, LLC
Field: Pharmaceuticals (Chemistry)
Classification: CPC C  A | IPC A  C

Claim 0:
1. A conjugate of formula (I):, wherein
Z is CR4 or N;
R1 is selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
R2 and R3 are each independently selected from hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl, acyloxy, acyl amino, amino acyl, alkylamide, substituted alkylamide, sulfonyl, thioalkoxy, substituted thioalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl, or R2 and R3 are optionally cyclically linked to form a 5 or 6-membered heterocyclyl;
each R4 is independently selected from hydrogen, halogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, acyl, acyloxy, acyl amino, amino acyl, alkylamide, substituted alkylamide, sulfonyl, thioalkoxy, substituted thioalkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, substituted cycloalkyl, heterocyclyl, and substituted heterocyclyl;
L is a linker comprising (T1-V1)a-(T2-V2)b-(T3-V3)c, wherein a, b, and c are 1;
T1, is selected from (C1-C12)alkyl and substituted (C1-C12)alkyl;
T2 is 4-amino-piperidine (4AP) having the structure:, T3 is selected from (C1-C12)alkyl and substituted (C1-C12)alkyl;
V1, V2, and V3 are each —CO—;
each f is independently an integer from 0 to 12;
each n is independently an integer from 0 to 30;
W1 is a maytansinoid;
W2 is an anti-CD25 antibody comprising a heavy chain comprising complementarity determining regions (CDRs) of SYRMH (SEO ID NO: 6), YINPSTGYTEYNQKFKD (SEQ ID NO: 7) and GGGVFDY (SEQ ID NO: 8); and a light chain comprising the CDRs of SASSSISYMH (SEQ ID NO: 9), YTSILHS (SEQ ID NO: 10), and QQGNTLPWT (SEQ ID NO: 11);
and wherein the anti-CD25 antibody comprises at the C-terminus of the heavy chain constant region a sequence of formula (II):

X1(FGly′)X2Z20X3Z30  (II)

wherein FGly′ is the amino acid residue coupled to the linker;
Z20 is either a proline or alanine residue;
Z30 is a basic amino acid or an aliphatic amino acid;
X may be present or absent and, when present, can be any amino acid;
X2 and X3 are each independently any amino acid.