Steroids and protein-conjugates thereof

A method for treating a disease, disorder, or condition associated with glucocorticoid receptor signaling comprising administering to a patient having said disease, disorder, or condition a therapeutically effective amount of a compound of Formula (A):

• or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivative thereof, wherein:
• R1 and R2 together form
• wherein R4 is linear or branched alkyl, aryl, arylalkyl, or an N-containing heterocycloalkyl,
• wherein the linear or branched alkyl, aryl, arylalkyl, and N-containing heterocycloalkyl are, independently in each instance, optionally substituted with —NRaRb;
• R3 is —NRaRb;
• R5 is, independently in each instance, —OH, halo, alkyl, or arylalkyl;
• Ra and Rb are, independently in each instance, —H, unsubstituted alkyl, or optionally substituted aryl or Ra and Rb, taken together form a 3-7 membered ring;
• and n is an integer from 0-19.

A method of delivering a compound of Formula (A):

• or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivative thereof, wherein:
• R1 and R2 together form
• wherein R4 is alkyl, aryl, arylalkyl, or an N-containing heterocycloalkyl, wherein the linear or branched alkyl, aryl, arylalkyl, and N-containing heterocycloalkyl are, independently in each instance, optionally substituted with —NRaRb;
• R3 is —NRaRb;
• R5 is, independently in each instance, —OH, halo, alkyl, or arylalkyl;
• Ra and Rb are, independently in each instance, —H, optionally substituted alkyl, or optionally substituted aryl or Ra and Rb, taken together form a 3-7 membered ring;
• and n is an integer from 0-19;
• to a cell comprising contacting said cell with a protein steroid conjugate of said compound, wherein said protein conjugate comprises an antibody or antigen binding fragment thereof that binds a surface antigen of said cell.

A linker-payload comprising a compound of Formula (A):

• or a pharmaceutically acceptable salt, solvate, stereoisomer, or derivative thereof, wherein:
• R1 and R2 together form
• wherein R4 is alkyl, aryl, arylalkyl, or an N-containing heterocycloalkyl, wherein the linear or branched alkyl, aryl, arylalkyl, and N-containing heterocycloalkyl are, independently in each instance, optionally substituted with —NRaRb;
• R3 is —NRaRb;
• R5 is, independently in each instance, —OH, halo, alkyl, or arylalkyl;
• Ra and Rb are, independently in each instance, —H, optionally substituted alkyl, or optionally substituted aryl or Ra and Rb, taken together form a 3-7 membered ring;
• and n is an integer from 0-19;
• linked to a reactive group, optionally via a linker.

A method for treating a disease, disorder, or condition associated with glucocorticoid receptor signaling comprising administering to a patient having said disease, disorder, or condition a therapeutically effective amount of a compound of Formula 1000:

• or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof, wherein:
• R1 and R2 together form
• either (a) or (b):
• (a) R3 is —NRaRb;
• and
• R4 is selected from the group consisting of -alkylene-NRaRb, —X-arylene-Y—NRaRb, —X-heteroarylene-Y—NRaRb, and N-containing heterocycloalkyl;
• wherein X is absent, —NH—, —CH2—, or —O—;
• wherein Y is absent or —CH2—;
• or
• (b) R3 is —NRaRb;
• and
• R4 is linear or branched alkyl;
• R5 is, independently in each instance, selected from a substituent in the group consisting of —OH, halo, and alkyl;
• n is an integer from 0-16;
• and each R5 is positioned on any ring atom;
• Ra and Rb are, independently in each instance, selected from the group consisting of —H and unsubstituted alkyl;
• or Ra and Rb cyclize to form cycloheteroalkyl with three to six ring atoms, including one hetero atom, which is the N to which they are attached.