Patent ID: 11865114
Assignee: AURIGENE ONCOLOGY LIMITED
Field: Pharmaceuticals (Chemistry)
Classification: CPC A  C  G | IPC A  G

Claim 0:
1. A method of treating a prostate disease in a subject in need thereof comprising:
a) identifying the subject as a responder to treatment with at least one SMARCA2/4 degraders when at least one tumor specific alteration is present in the subject, wherein said tumor specific alteration is:
a mutation, an amplification, or an overexpression of Androgen Receptor (AR) gene;
a loss of function or a deleterious mutation in phosphatase and tensin homolog (PTEN); or
a genomic rearrangement that results in a translocation between a TMPRSS2 gene and an ERG gene; and

the SMARCA2/4 degrader is a compound of formula (I):, or a pharmaceutically acceptable salt thereof or a stereoisomer thereof; wherein,
R1 is hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, —COORa—CON(Ra)2, or aryl; wherein the aryl is optionally substituted independently with at least one of hydroxy, alkoxy, halo, alkyl, amino, —ONa, —COORa, or —OCORa; wherein Ra at each occurrence is hydrogen or alkyl;
R2 is —NR3R4 or —OR3; wherein, R3 and R4 are independently hydrogen or alkyl;
Ring A is a heterocycloalkyl ring or a heteroaryl ring, each optionally substituted independently with at least one of hydroxy, halo or alkyl;
L is a linker with a chemical structure of:, , wherein,
the left side of the linker is attached with ring A and the right side of the linker is attached with Targeting Ligand (TL);
Rb is hydrogen or alkyl;
Rc is alkyl;
n is 0 to 10; and
p is 1 to 5;
Targeting Ligand (TL) is, , wherein
R6 is hydrogen, alkyl, acyl, or haloalkyl;
R7 is —O—R5 or halo; wherein R5 is hydrogen, alkyl, acyl, or Na; and
R8 is hydrogen or alky; and
b) administering a therapeutically effective amount of at least one SMARCA2/4 degrader to the subject who is identified to respond to the treatment, thereby treating the prostate disease.