[EN] NOVEL RADIOMETAL-BINDING COMPOUNDS FOR DIAGNOSIS OR TREATMENT OF PROSTATE SPECIFIC MEMBRANE ANTIGEN-EXPRESSING CANCER<br/>[FR] NOUVEAUX COMPOSÉS DE LIAISON DE RADIOMÉTAUX POUR LE DIAGNOSTIC OU LE TRAITEMENT DU CANCER EXPRIMANT UN ANTIGÈNE MEMBRANAIRE SPÉCIFIQUE DE LA PROSTATE
申请人:BRITISH COLUMBIA CANCER AGENCY BRANCH
公开号:WO2019075583A1
公开(公告)日:2019-04-25
This application relates to compounds of Formula (I-a) or Formula (I-b), or is salts or solvates thereof. R1 is -(CH2)5CH3 or comprises 2-4 fused benzene rings. R2 is I, Br, F, Cl, H, OH, OCH3, NH2, NO2 or CH3. R3 is a peptide-bonded glycine, aspartate or glutamate or is glutamate peptide bonded through Cdelta. L is –CH2NH–, –(CH2)2NH–, –(CH2)3NH–, or –(CH2)4NH–. R4 is a radiometal chelator optionally bound by a radiometal. Variable 'n' is 1-3. The compounds may be useful for imaging prostate specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).
该应用涉及到Formula (I-a)或Formula (I-b)的化合物,或其盐或溶剂化合物。R1为-(CH2)5CH3或包含2-4个融合苯环。R2为I、Br、F、Cl、H、OH、OCH3、NH2、NO2或CH3。R3为肽键的甘氨酸、天冬酰胺或谷氨酸,或通过Cdelta连接的谷氨酸肽键。L为-CH2NH-、-(CH2)2NH-、-(CH2)3NH-或-(CH2)4NH-。R4为可选择地与放射金属结合的放射金属螯合剂。变量'n'为1-3。这些化合物可能用于成像前列腺特异性膜抗原(PSMA)表达组织或治疗PSMA表达疾病(例如癌症)。