ANTI-ANGIOGENIC COMPOUNDS
The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.
1 - 175 . (canceled)
176 . A compound of the formula:
wherein Z is of the formula:
wherein Antibody is an aldolase catalytic antibody, and v is 1, 2, 3, 4, or 5; w is 1, 2, 3, 4, or 5; and R b is hydrogen, substituted or unsubstituted C 1-10 alkyl, substituted or unsubstituted C 3-7 cycloalkyl-C 0-6 alkyl, or substituted or unsubstituted aryl-C 0-6 alkyl, and q is 0, 1, 2 or 3.
177 . A compound as claimed in claim 176 , wherein v is 1, w is 1, R b is hydrogen.
178 . A compound of the formula:
wherein Antibody is an aldolase catalytic antibody, and v is 1, 2, 3, 4, or 5; w is 1, 2, 3, 4, or 5; and R b is hydrogen, substituted or unsubstituted C 1-10 alkyl, substituted or unsubstituted C 3-7 cycloalkyl-C 0-6 alkyl, or substituted or unsubstituted aryl-C 0-6 alkyl, q is 0, 1, 2 or 3, and AAn-AA2-AA1-N is an Anti-Angiogenic peptide.
179 . A compound as claimed in claim 178 , wherein v is 1, w is 1, R b is hydrogen and q is 2.
180 . A compound as claimed in claim 176 , wherein said Antibody is selected from full length antibody, Fab, Fab′, F(ab′) 2 , F v , dsF v , scF v , V H , diabody, or minibody comprising V H and V L domains from h38c2.
181 . A compound according to claim 176 , wherein said Antibody comprises a variable light chain comprising SEQ ID NO:32 and a variable heavy chain comprising SEQ ID NO:33.
182 . A compound according to claim 176 , wherein said Antibody comprises a light chain comprising SEQ ID NO:40 and a heavy chain comprising SEQ ID NO:41.
183 . A compound as claimed in claim 178 , wherein said Antibody is selected from full length antibody, Fab, Fab′, F(ab′) 2 , F v , dsF v , scF v , V H , diabody, or minibody comprising V H and V L domains from h38c2.
184 . A compound according to claim 178 , wherein said Antibody comprises a variable light chain comprising SEQ ID NO:32 and a variable heavy chain comprising SEQ ID NO:33.
185 . A compound according to claim 178 , wherein said Antibody comprises a light chain comprising SEQ ID NO:40 and a heavy chain comprising SEQ ID NO:41.
186 . A compound of the formula:
187 . A method of synthesizing a compound according to claim 186 , comprising the following route:
188 . A compound of the formula:
189 . A use of a compound according to claim 188 in the manufacture of a compound of the formula:
190 . A compound of the formula:
191 . Use of a compound according to claim 190 in the manufacture of a compound of the formula: