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US 2026/0284243 A1Published application
Gastrin-releasing peptide receptor (grpr)-targeted compounds and uses thereof
AssigneeAlpha-9 Oncology, Inc.
InventorsJutta WANNER, Chengcheng ZHANG, Kaveh MATINKHOO, Stephen BARIGYE, Hsiou-Ting KUO
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Abstract
The present invention relates to gastrin-releasing peptide receptor (GRPR)-targeted compounds and their use for imaging and treatment of diseases or conditions characterized by expression of the gastrin-releasing peptide receptor.
Claims22
-85. (canceled)
A compound of Formula (I),
- (I)
- Rradn6-[linker]-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-
- Xaa7-Xaa8-[ψ-Xaa9-(Xaa10)m2]m1-R
- or a salt thereof, wherein:
- Xaa1 is an N-terminal amino acid residue selected from D-Phe, D-Cpa, D-Nal, or D-2-Nal;
- Xaa2 is Asp, Asn, Gln, or Glu;
- Xaa3 is Trp, Trp(Me), αMe-Trp, Trp(7-F), Trp(6-F), Trp(5-F), or Trp(4-F);
- Xaa4 is Ala or D-Ala;
- Xaa5 is Val or tert-leucine (Tle);
- Xaa6 is Gly or D-Ala;
- Xaa7 is Trp, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(7-Cl), Trp(6-Cl), Trp(5-Cl), Trp(4-Cl), Trp(7-Br), Trp(6-Br), Trp(5-Br), Trp(4-Br), Trp(7-I), Trp(6-I), Trp(5-I), Trp(4-I), Trp(5-OH), or αMe-Trp;
- Xaa8 is Leu;
- m1 is 1 and m2 is 0;
- Xaa9 is Pro, oxazolidine-4-carboxylic acid (4-oxa-L-Pro), or 4,4-difluoroproline (difluoroPro);
- R is —NH2;
- ψ represents a peptide bond or reduced peptide bond joining Xaa8 to Xaa9;
- the linker comprises p-aminomethylaniline-diglycolic acid (pABzA-DIG), 4-amino-(1-carboxymethyl)piperidine (Pip), 9-amino-4,7-dioxanonanoic acid (dPEG2), or 4-(2-aminoethyl)-1-carboxymethyl-piperazine (Acp), wherein the linker optionally comprises an albumin binder;
- n6 is 1;
- Rrad is a radiometal chelator;
- wherein the compound is optionally bound by a radiometal;
- and
- wherein Xaa1, Xaa2, Xaa3, Xaa4, Xaa5, Xaa6, Xaa7, Xaa8, or Xaa9 is each optionally N-methylated.
19 more elements
Dependencies are inferred from the claim text.