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US 10,039,846 B2Granted
Compositions targeting bradykinin receptor B1 for medical imaging of cancer and other disorders
AssigneeBritish Columbia Cancer Agency Branch
InventorsKuo-shyan Lin, Francois Benard, Jinhe Pan, Felix Mesak, Zhengxing Zhang
Life of this patent
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Abstract
Bradykinin B1 receptor (B1R) targeting peptides and compounds are radiolabelled with radioisotopes that are suitable for imaging and/or radiotherapy. The radiolabelled peptides and compounds have utility in imaging tissues expressing or overexpressing B1R and/or treating diseases or conditions in which B1R is expressed or overexpressed, including cancer.
Claims11
A bradykinin B1 receptor (B1R) targeting compound that selectively binds to B1R, comprising:
- a peptidic compound having general Formula (I) or a non-peptidic compound having general Formula (III):
- B-L-Xaa1-Xaa2-Arg-Pro-Xaa3-Gly-Xaa4-Ser-Xaa5-Xaa6 (I)
- wherein:
- B is a radio-labelled moiety, radiometal chelating agent, N-succinimidyl-4-[18F]fluorobenzoate (SFB), D-Pra,
- L is a linker;
- Xaa1 is Lys or Sar;
- Xaa2 is Lys or D-Arg;
- Xaa3 is Pro or Hyp;
- Xaa4 is Phe, Cha, Thi, (α-Me)Phe, Igl or Cpg;
- Xaa5 is Pro, D-Tic, D-Hyp, D-βNal or D-Igl, and
- Xaa6 is Leu, Ile, D-Phe, Cpg or Oic [SEQ ID NO:
- 31], wherein Xaa6 is not peptide-bonded to Arg, and
- wherein when B is a radiometal chelating agent, it is optionally chelated to a radiolabel;
- wherein:
- R1, R4 and R5 are each independently H or Me;
- R2 is H or halo;
- R3 is H, Me, halo or OMe;
- ˜NR6R7 is:
- Y is (CH2)mNHR or
- R is (CH2)p;
- R8 is Me or Et;
- X is O or CH2;
- NR9R10 is
- n, m, p, q and t are each independently 0, 1 or 2, and
- u and v are each independently 1 or 2, and
- wherein F is optionally 18F.
23 more elements
Dependencies are inferred from the claim text.