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US 2008/0166364 A1Published application
Anti-angiogenic compounds
AssigneeCovx Technology Ireland, Ltd.
InventorsCurt Bradshaw, Abhijit Bhat, Jing Yu Lai, Venkata Doppalapudi
Life of this patent
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Abstract
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.
Claims94
A compound of the formula:
- R1-[AA targeting agent]-R2
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH2, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate, and
- wherein [AA targeting agent] comprises a peptide of the sequence:
- (SEQ ID NO:
- 193)
- R1-Q1 x2 Y3 Q4 x5 L6 D7 x8 x9 D10 x11 x12 x13 x14
- x15 x16 F17 x18 x19 Q20 Q21 G22-R2
- wherein one of Q1, x8, x9, x11, x12, x15, x16, x18, x19 or G22 is a linking residue comprising a nucleophilic side chain covalently linkable to the combining site of an antibody directly or via an intermediate linker, the linking residue being selected from the group comprising K, R, Y, C, T, S, homologs of lysine, homocysteine, homoserine, Dap, and Dab, or the N-terminus or C-terminus, and
- x2 is selected from the group consisting of K, N, R, H, AcK, Nick, CbcK and the linking residue, and
- x5 is selected from the group consisting of P, hP, dhP, or BnHP, and
- x9 is selected from the group consisting of L, I, ThA, AcK and the linking residue, and
- x8 is selected from the group consisting of E and the linking residue, and
- x11 is selected from the group consisting of Q, N, C, K, AcK, Dab, Dap and the linking residue, and
- x12 is selected from the group consisting of L, HL, Nva, I, HchA, HF, ThA, and
- x13 is selected from the group consisting of L, HL, Nva, I, HchA, HF, ThA, and
- x14 is selected from the group consisting of aromatic residues and the linking residue, and
- x15 is selected from the group consisting of D and the linking residue, and
- x16 is selected from the group consisting of Q, N and the linking residue, and
- x18 is selected from the group consisting of M and the linking residue, and.
- x19 is selected from the group consisting of L, I and the linking residue.
19 more elements
A peptide at least 90% homologous to a peptide selected from the group consisting of:
- SEQ ID NO:
- 22, SEQ ID NO:
- 34, SEQ ID NO:
- 41, SEQ ID NO:
- 43, SEQ ID NO:
- 44, SEQ ID NO:
- 48 and SEQ ID NO:
- 64.
5 more elements
A peptide at least 80% homologous to a peptide selected from the group consisting of:
- SEQ ID NO:
- 22, SEQ ID NO:
- 34, SEQ ID NO:
- 41, SEQ ID NO:
- 43, SEQ ID NO:
- 44, SEQ ID NO:
- 48 and SEQ ID NO:
- 64.
5 more elements
A peptide at least 70% homologous to a peptide selected from the group consisting of:
- SEQ ID NO:
- 22, SEQ ID NO:
- 34, SEQ ID NO:
- 41, SEQ ID NO:
- 43, SEQ ID NO:
- 44, SEQ ID NO:
- 48 and SEQ ID NO:
- 64.
5 more elements
A peptide selected from the group consisting of:
- R1-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- R1-QNY QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK D(AcK)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK DET LYD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(DHP)L DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(HP)L DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT IYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEI DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HChA)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HF)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (ThA)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (Nva)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HL)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT LFD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(NO2F)D QFM LQQ G-
- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(BPA)D QFM LQQ G-
- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(CO2H)FD QFM LQQ G-
- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT L(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT LFD QFM LQQ G- R2;
- DCB-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- DFB-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- PyC-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- Amido 2-PEG-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(ClBnCarbamateK)Y QPL DEL DKT LYD QFM LQQ G-
- R2;
- R1-Q(AcK)Y QPL DEL D(Dab)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL D(Dap)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT L(NO2F)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT L(BPA)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT L(CF)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT LYD QFM LQQ G-R2;
- R1-Q(Nick)Y QPL DEL DKT LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT L(CF)D QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DE(AcK) DK(0P)T LFD QFM LQQ G-R2;
- wherein:
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH2, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate.
39 more elements
A peptide selected from the group consisting of:
- R1-Q(AcK)Y QPL DELDKTLYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKTLYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DELDKTL(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEKDK(Ac)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DEK(Ac) DKLT LYD QFM LQQ G-R2;
- wherein
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(C2H2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate.
6 more elements
A peptide of the formula:
- R1-Q(AcK)Y QPL DEK(Ac) DKLT LYD QFM LQQ G-R2;
- wherein
- R1 is C(O)CH3 and R2 is NH2.
A compound having the formula:
- L-[AA targeting agent]
- wherein:
- [AA targeting agent] is a peptide antagonist of the angiopoietin 2 and
- L is a linker attached to amino end, the carboxy end, a K side chain, a Y side chain or a T side chain of the AA targeting agent, and is capable of forming a covalent bond with an amino acid side chain in a combining site of an antibody.
1 more element
A compound having the formula:
- L-[AA targeting agent]
- wherein:
- [AA targeting agent] is a peptide selected from the group consisting of:
- R1-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- R1-QNY QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK D(AcK)F LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK DET LYD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(DHP)L DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(HP)L DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT IYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEI DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HChA)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HF)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (ThA)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (Nva)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HL)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT LFD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(NO2F)D QFM LQQ G-
- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(BPA)D QFM LQQ G-
- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(CO2H)FD QFM LQQ G-
- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT L(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT LFD QFM LQQ G- R2;
- DCB-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- DFB-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- PyC-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- Amido 2-PEG-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(ClBnCarbamateK)Y QPL DEL DKT LYD QFM LQQ G-
- R2;
- R1-Q(AcK)Y QPL DEL D(Dab)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL D(Dap)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT L(NO2F)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT L(BPA)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT L(CF)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT LYD QFM LQQ G-R2;
- R1-Q(Nick)Y QPL DEL DKT LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT L(CF)D QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DE(AcK) DK(0P)T LFD QFM LQQ G-R2;
- wherein:
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH2, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate;
- and
- L is a linker moiety having the formula —X—Y-Z-, wherein:
- X is optionally present and when present is attached to the amino end, the carboxy end, a K side chain, a Y side chain or a T side chain of the AA targeting agent, is substituted or unsubstituted, and is selected from —R22—[CH2—CH2—O]t—R23—, —R22-cycloalkyl-R23—, —R22-aryl-R23—, or —R22-heterocyclyl-R23—, wherein:
- t=1-10;
- and the size of R22 and R23 are such that the backbone length of X remains about 200 atoms or less;
- Y is an optionally present recognition group comprising at least a ring structure;
- and
- Z is a reactive group that is capable of forming a covalent bond with an amino acid side chain in a combining site of an antibody.
50 more elements
The compound according to claim 30, wherein R23 is a substituted or unsubstituted, straight or branched chain C1-50 heteroalkylene.
A compound having the formula selected from the group consisting of:
- R1-Q(AcK)Y QPL DELDK(L)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DK(L)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DELDK(L)T L(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK(L) DK(Ac)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DEK(Ac) DK(L)T LYD QFM LQQ G-R2;
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6Hs, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH12, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2C3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate;
- and K(L) is a lysine reside attached to a linker L wherein L is capable of forming a covalent bond with an amino acid side chain in a combining site of an antibody.
6 more elements
A compound having the formula selected from the group consisting of:
- R1Q(AcK)Y QPL DELDK(L)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DK(L)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DELDK(L)T L(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK(L) DK(Ac)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DEK(Ac) DK(L)T LYD QFM LQQ G-R2;
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH2, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate;
- and
- K(L) is
- L is a linker moiety having the formula —X—Y-Z-, wherein:
- X is:
- wherein v and w are selected such that the backbone length of X is 6-12 atoms;
- Y is a recognition group comprising at least a ring structure;
- and
- Z is a reactive group that is capable of forming a covalent bond with an amino acid side chain in a combining site of an aldolase antibody.
13 more elements
A compound selected from the group consisting of:
A compound having the formula
A compound having the formula:
- Antibody[-L′-[AA targeting agent]]1 or 2
- wherein:
- [AA targeting agent] is a peptide Antagonist of the angiopoietin 2;
- and
- L′ is a linker attached to the amino end, the carboxy end, a K side chain, a Y side chain or a T side chain of the AA targeting agent and wherein L further comprises a covalent link to an amino acid side chain in a combining site of an antibody.
2 more elements
A compound having the formula:
- Antibody [-L′-[AA targeting agent]]1 or 2
- wherein:
- [AA targeting agent] is a peptide selected from the group consisting of:
- R1-QKY QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- R1-QNY QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK D(AcK)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK DET LYD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(DHP)L DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(HP)L DEL DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT IYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEI DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HChA)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HF)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (ThA)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (Nva)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT (HL)YD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT LFD QFM LQQ G- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(NO2F)D QFM LQQ G-
- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(BPA)D QFM LQQ G-
- R2;
- R1-Q(AcK)Y Q(HP)L DE(ThA) DKT L(CO2H)FD QFM LQQ G-
- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT L(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT LFD QFM LQQ G- R2;
- DCB-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- DFB-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- PyC-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- Amido 2-PEG-Q(AcK)Y QPL DEL DKT LYD QFM LQQ G- R2;
- R1-Q(ClBnCarbamateK)Y QPL DEL DKT LYD QFM LQQ G-
- R2;
- R1-Q(AcK)Y QPL DEL D(Dab)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL D(Dap)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DKT L(NO2F)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT L(BPA)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT L(CF)D QFM LQQ G-R2;
- R1-QNY QPL DEL DKT LYD QFM LQQ G-R2;
- R1-Q(Nick)Y QPL DEL DKT LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DE(AcK) DKT L(CF)D QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DE(AcK) DK(0P)T LFD QFM LQQ G-R2;
- wherein R1 is CH3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)CH2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH2, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6H5, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate;
- and
- L′ is a linker moiety having the formula —X—Y-Z′-, wherein:
- X is optionally present and when present is attached to the amino end, the carboxy end, a K side chain, a Y side chain or a T side chain of the AA targeting agent, is substituted or unsubstituted, and is selected from —R22—[C2—CH2—O]t—R23—, —R22-cycloalkyl-R23—, —R22-aryl-R23—, or —R22-heterocyclyl-R23—, wherein:
- R22 and R23 are independently a covalent bond, —O—, —S—, —NRb—, substituted or unsubstituted straight or branched chain C1-50 alkylene, substituted or unsubstituted straight or branched chain C1-50 heteroalkylene, substituted or unsubstituted straight or branched chain C2-50 alkenylene, or substituted or unsubstituted C2-50 heteroalkenylene;
- Rb, at each occurrence, is independently hydrogen, substituted or unsubstituted C1-10 alkyl, substituted or unsubstituted C3-7 cycloalkyl-C0-6 alkyl, or substituted or unsubstituted aryl-C0-6 alkyl;
- t=2-50;
- and
- the size of R22 and R23 are such that the backbone length of X remains about 200 atoms or less;
- Y is an optionally present recognition group comprising at least a ring structure;
- and
- Z′ is an attachment moiety comprising a covalent link to an amino acid side chain in a combining site of an antibody.
53 more elements
A compound having the formula selected from the group consisting of:
- R1-Q(AcK)Y QPL DELDK(L′)T LYD QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEL DK(L′)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DELDK(L′)T L(NO2F)D QFM LQQ G- R2;
- R1-Q(AcK)Y QPL DEK(L′) DK(Ac)T LYD QFM LQQ G-R2;
- R1-Q(AcK)Y QPL DEK(Ac) DK(L′)T LYD QFM LQQ G-R2;
- wherein R1 is C1H3, C(O)CH3, C(O)CH3, C(O)CH2CH3, C(O)Cl2CH2CH3, C(O)CH(CH3)CH3, C(O)CH2CH2CH2CH3, C(O)CH(CH3)CH2CH3, C(O)C6H5, C(O)CH2CH2(CH2CH2O)1-5Me, dichlorobenzoyl (DCB), difluorobenzoyl (DFB), pyridinyl carboxlate (PyC) or amido-2-PEG, an amino protecting group, a lipid fatty acid group or a carbohydrate;
- and
- R2 is OH, NH2, NH(CH3), NHCH2CH3, NHCH2CH2CH3, NHCH(CH3)CH3, NHCH2CH2CH2CH3, NHCH(CH3)CH2CH3, NHC6Hs, NHCH2CH2OCH3, NHOCH3, NHOCH2CH3, a carboxy protecting group, a lipid fatty acid group or a carbohydrate;
- and K(L′) is
- L is a linker moiety having the formula —X—Y-Z′-, wherein:
- X is:
- wherein v and w are selected such that the backbone length of X is 6-12 atoms;
- Y is a recognition group comprising at least a ring structure;
- and
- Z′ is an attachment moiety comprising a covalent link to an amino acid side chain in a combining site of an antibody.
12 more elements
A compound having the structure:
- wherein Antibody is an antibody comprising the VH and VL domains from h38c2 and a constant domain selected from the group consisting of IgG1, IgG2, IgG3, and IgG4.
A compound having the structure:
- wherein Antibody is an antibody comprising the VH and VL domains from h38c2 and a constant domain selected from the group consisting of IgG1, IgG2, IgG3, and IgG4.
A compound having the structure:
- wherein Antibody is an antibody comprising the VH, and VL domains from h38c2 and a constant domain selected from the group consisting of IgG1, IgG2, IgG3, and IgG4.
A compound having the structure:
- wherein Antibody is an antibody comprising the VH and VL domains from h38c2 and a constant domain selected from the group consisting of IgG1, IgG2, IgG3, and IgG4.87.
A compound having a structure selected from the group consisting of:
- wherein Antibody is an antibody comprising the VH and VL domains from h38c2 and a constant domain selected from the group consisting of IgG1, IgG2, IgG3, and IgG4.
The pharmaceutical composition of claim 90, further comprising a therapeutically effective amount of one or more chemotherapeutic agents.
Dependencies are inferred from the claim text.