Abstract: The invention provides immunoconjugates of Formula I comprising an anti-HER2 antibody linked by conjugation to one or more 8-Het-2-aminobenzazepine derivatives. The invention also provides 8-Het-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides immunoconjugates of Formula I comprising an anti-HER2 antibody linked by conjugation to one or more 8-phenyl-2-aminobenzazepine derivatives. The invention also provides 8-phenyl-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides immunoconjugates of Formula I comprising an anti-PD-L1 antibody linked by conjugation to one or more 8-Cyc-2-aminobenzazepine derivatives. The invention also provides 8-Cyc-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides immunoconjugates of Formula I comprising an antibody linked by conjugation to one or more thienoazepine derivatives. The invention also provides thienoazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides immunoconjugates of Formula I comprising a cell-binding agent linked by conjugation to one or more immunostimulatory moieties where the linker is a substrate for elastase. The invention also provides immunostimulant intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides immunoconjugates of Formula I comprising an antibody linked by conjugation to one or more pyrazoloazepine derivatives. The invention also provides pyrazoloazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides macromolecule-supported compounds of Formula I comprising a macromolecular support linked by conjugation to one or more thienoazepine derivatives. The invention also provides thienoazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the macromolecule-supported compounds through a linker or linking moiety. The invention further provides methods of treating cancer with the macromolecule-supported compounds.

Abstract: This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.

Abstract: The invention provides immunoconjugates of Formula I comprising an antibody linked by conjugation to one or more thienoazepine derivatives. The invention also provides thienoazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides immunoconjugates of Formula I comprising an antibody linked by conjugation to one or more 8-amido-2-aminobenzazepine derivatives. The invention also provides 8-amido-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides a method for producing an immunoconjugate, the method comprising combining one or more compounds of Formula I and an antibody construct of Formula II to provide the immunoconjugate of Formula III, wherein TA is a therapeutic agent, L is a linker, r is an integer from 1 to 50, Ar is an aromatic moiety comprising a substituent selected from PEG, —SO2CX3, —NR3+, —NO2, —SO3R, —SO2R, —CN, —CX3, —PO3R2, —OPO3R2, and salts thereof, each R independently is H, CX3, or C1-C4 alkyl, each X independently is hydrogen or a halogen, Y is CH2, PEG, or a bond, n is an integer from 1 to 4, and PEG has the formula: —(CH2CH2O)m-(CH2)p—, where p is an integer from 1 to 5 and m is an integer from 2 to 50. The invention also provides an immunoconjugate and a composition of immunoconjugates formed from said method.

Abstract: The application provides macromolecule-supported compounds of Formula I or III comprising a macromolecular support linked by conjugation to one or more aminobenzazepine derivatives. The application also provides aminobenzazepine derivative intermediate compositions of Formula II comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the macromolecule-supported compounds through a linker or linking moiety. The application further provides compositions comprising the macromolecule-supported compounds, as well as methods of treating cancer with the macromolecule-supported compounds.

Abstract: The invention provides immunoconjugates of Formula (I) comprising an antibody linked by conjugation to one or more aminoquinoline derivatives. The invention also provides aminoquinoline derivative intermediate compositions of Formula (III) comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides an immunoconjugate of formula (I) or (II). Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.

Abstract: The invention provides an immunoconjugate of formula (I) or (II). Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds human epidermal growth factor receptor 2 (“HER2”) linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract: The invention provides immunoconjugates of Formula I comprising an anti-CEA antibody linked by conjugation to one or more 8-Het-2-aminobenzazepine derivatives. The invention also provides 8-Het-2-aminobenzazepine derivative intermediate compositions comprising a reactive functional group. Such intermediate compositions are suitable substrates for formation of the immunoconjugates through a linker or linking moiety. The invention further provides methods of treating cancer with the immunoconjugates.

Abstract: The invention provides an immunoconjugate of formula (I) or (II) Antibody-adjuvant immunoconjugates of the invention, comprising an antibody construct that has an antigen binding domain that binds carcinoembryonic antigen (“CEA”) linked to one or more adjuvants, demonstrate superior pharmacological properties over conventional antibody conjugates. The invention further provides compositions comprising and methods of treating cancer with the immunoconjugate.

Abstract: The invention provides a macromolecule-supported compound of formula (I) or (II). Macromolecule-supported compounds of the invention, comprising macromolecular support linked to one or more TLR agonists, are recognized by TLRs (e.g., TLR7 and/or TLR8) with high affinity providing utility in therapeutics, diagnostics, and chemical assays. The invention further provides compositions comprising and methods of treating cancer with the macromolecule-supported compounds.

Abstract: The invention provides a method of treating a disease or condition in a mammal by administering a compound having the general formula I: or a pharmaceutically acceptable salt thereof, wherein the variables RAA, n, ring A, X1, L, m, X2, R2, R3, R4, R5, X, and R6 have the meaning as described herein.