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US 2012/0189546 A1Published application
Radiolabelling Method Using Cycloalkyl Groups
AssigneeBayer Pharma Aktiengesellschaft
InventorsKeith Graham, Heribert Schmitt-Willich, Dominic Franck
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Abstract
This invention relates to novel cyclo alkyl compounds suitable for labeling by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
Claims17
A compound of Formula I
- wherein
- A=H, —O—, ═O, —S—, ═S, N, N(R′), NYR′, P(R′)(R″), P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′ C(O)R′R″, SO, SO2, or SO2NR′,
- B=H, —O—, ═O, S, ═S, N, N(R′), NYR′, P(R′)(R″), P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′, C(O)R′R″, SO, SO2, or SO2NR′,
- Y=N, NR′, O or S,
- C=H, Leaving Group (LG), or R′,
- D=H, Leaving Group (LG), or R′,
- E=absent, H, OR′, SR′, NR′, CR′p, —O—, ═O, —S—, ═S, N, N(R′), NYR′, P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′ C(O)R′R″, SO, SO2, SO2NR′, or W-Z, wherein W is a linker and Z is a targeting agent or vector,
- F=absent, H, OR′, SR′, NR′, CR′p, —O—, ═O, —S—, ═S, N, N(R′), NYR′, P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′ C(O)R′R″, SO, SO2, SO2NR′, or W-Z, wherein W is a linker and Z is a targeting agent or vector,
- p=1 to 3,
- R′=H, OH, NH, branched or linear C1-C6 alkyl, branched or linear O—C1-C6 alkyl, branched or linear C1-C6 alkoxy, branched or linear C1-C6 alkylene, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl, CO(CH2)n, [O(CH2)n—O(CH2)n]m, or —O(CH2)n, [O(CH2)n—O(CH2)n]m,
- n=1 to 6 and m=1 to 6,
- R″=H, OH, NH, branched or linear C1-C6 alkyl, branched or linear O—C1-C6 alkyl, branched or linear C1-C6 alkoxy, branched or linear C1-C6 alkylene, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl, CO(CH2)n, [O(CH2)n—O(CH2)n]m, or —O(CH2)n, [O(CH2)n—O(CH2)n]m,
- n=1 to 6 and m=1 to 6,
- X=(CH2)q or C(R′R″), and
- q=0 to 2,
- provided when A or B is O then E or F is absent
- or a pharmaceutical salt, diastereomere or enantiomere thereof.
14 more elements
A compound of formula II.
- wherein
- A=H, —O—, ═O, —S—, ═S, N, N(R′), NYR′, P(R′)(R″), P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′ C(O)R′R″, SO, SO2, or SO2NR′,
- B=H, —O—, ═O, S, ═S, N, N(R′), NYR′, P(R′)(R″), P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′, C(O)R′R″, SO, SO2, or SO2NR′,
- Y=N, NR′, O or S,
- Y=N, NR′, O or S,
- C=H, radioisotope, halogen or R′,
- D=H, radioisotope, halogen or R′,
- E=absent, H, OR′, SR′, NR′, CR′p, —O—, ═O, —S—, ═S, N, N(R′), NYR′, P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′ C(O)R′R″, SO, SO2, SO2NR′, or W-Z, wherein W is a linker and Z is a targeting agent,
- F=absent, H, OR′, SR′, NR′, CR′p, —O—, ═O, —S—, ═S, N, N(R′), NYR′, P(O)(R′)R″, C(R′)(R″), CR′R″, C(O), C(O)O, C(O)OR′ C(O)R′R″, SO, SO2, SO2NR′, or W-Z, wherein W is a linker and Z is a targeting agent,
- p=1 to 3,
- R′=H, OH, NH, branched or linear C1-C6 alkyl, branched or linear O—C1-C6 alkyl, branched or linear C1-C6 alkoxy, branched or linear C1-C6 alkylene, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl, CO(CH2)n, [O(CH2)n—O(CH2)n]m, or —O(CH2)n, [O(CH2)n—O(CH2)n]m,
- n=1 to 6 and m=1 to 6,
- R″=H, OH, NH, branched or linear C1-C6 alkyl, branched or linear O—C1-C6 alkyl, branched or linear C1-C6 alkoxy, branched or linear C1-C6 alkylene, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl, CO(CH2)n, [O(CH2)n—O(CH2)n]m, or —O(CH2)n, [O(CH2)n—O(CH2)n]m,
- n=1 to 6 and m=1 to 6,
- X=(CH2)q or C(R′R″), and
- q=0 to 2,
- provided when A or B is O then E or F is absent
- or a pharmaceutical salt, diastereomere or enantiomere thereof.
15 more elements
Dependencies are inferred from the claim text.