Patent ID: 11920172
Assignee: YALE UNIVERSITY
Field: Pharmaceuticals (Chemistry)
Classification: CPC C  A | IPC A  C

Claim 0:
1. A compound according to the chemical formula consisting of:, Wherein UPA is a urokinase-type plasminogen activator (UPA);
UkBMB is a UPA-binding motif covalently or non-covalently bound to UPA via a UKBM group;
said UKBM is a group according to the chemical formula:, wherein T is a Re group or an amino acid group according to the chemical structure:, RAA is side chain of an amino acid;
Re is H or an electrophilic group which is reactive with a nucleophile in the active site of urokinase-type plasminogen activator (UPA) to produce a covalent bond or non-covalent bond interaction;
p1 is an integer from 0 to 25; and
Each (AA) is independently a single amino acid residue,
ABM is an antibody binding moiety comprising a hapten which is capable of binding to an antibody in a patient or subject comprising;
the hapten a group according to the chemical structure:
(a), Wherein X″ is O, CH2, NR1, S; and
R1 is H, a C1-C3 alkyl group or a —C(O)(C1-C3) group;
(b), Wherein Xb is a bond, O, CH2 or NR1 or S; and
R1 is the same as above;
(c) a group according to the chemical structure:, Wherein DNP is a dinitrophenyl group linked to the amino acid through an amine group or a thio group;
(d) A dinitrophenyl group according to the chemical structure:, Wherein Y′ is H or NO2;
X is O, CH2, NR1, S(O), S(O)2, —S(O)2O, —OS(O)2, or OS(O)2O; and
R1 is H, a C1-C3 alkyl group, or a —C(O)(C1-C3) group;
(e) A digalactose hapten moiety according to the chemical structure:, Wherein X′ is CH2, O, N—R1′ or S;
R1′ is H or C1-C3 alkyl; and
Z is a bond, a monosaccharide, disaccharide, oligosaccharide, glycoprotein or glycolipid; or
(f) A group according to the chemical structure:, Wherein XR is O or S; and
XM is O or S;
L1 is a linker molecule which chemically links UkBMB to ABM via CT and L2 in said compound;
L2 is a linker molecule which chemically links ABM to UkBMB via CT and L1 in said compound;
wherein L1 and L2 are each independently a group according to the chemical structure:, , (polyproline linker)
or, , (a collagen linker); or a
group according to the chemical structure:, , or
a polypropylene glycol or polypropylene-co-polyethylene glycol linker containing about 1 to 75 alkyleneglycol units;
Each m of L1 or L2 is independently an integer selected from 1 to 75;
Each n of L1 or L2 is independently an integer selected from 1 to 75;
CT is a bond or a connector molecule;
Each j is independently 0, 1, 2, 3, 4 or 5;
Each k is independently 0, 1, 2, 3, 4 or 5, with the proviso that k and/or j are other than 0 when CT is a bond; and
m of UkBMB is 1 and n of ABM is from 1 to 3; or
a pharmaceutically acceptable salt, stereoisomer, solvate or polymorph thereof suitable for combination with a pharmaceutically acceptable excipient.