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US 6,669,925 B1Granted
Sigma-2 receptors as biomarkers of tumor cell proliferation
AssigneeWake Forest University
InventorsRobert H. Mach, Kenneth T. Wheeler
Life of this patent
Estimating the term…
Abstract
The present invention provides novel sigma-2 ligands (labeled and unlabeled) and the use of the compounds in medical therapy or diagnosis.
Claims21
A compound of formula (I):
- wherein
- R is aryl-Y—;
- Y is (C2-C14)alkenyl,
- aryl is optionally substituted with one or more halo, OH, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)C(O), (C1-C6)alkyl-S, NH2, SH, N(Z)2;
- A is NH, O or S;
- B is NH, O, or S;
- C is O or S;
- D is CH;
- E is CH;
- F is CH;
- and
- X is (CH2)2, (CH2)3 or CH═CH;
- each Z is H or (C1-C6)alkyl;
- wherein the ring comprising F═D-E is optionally substituted with one or more halo, OH, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)C(O), (C1-C6)alkyl-S, NH2, SH, N(Z)2;
- wherein Z is H or (C1-C6)alkyl, or methylene dioxy (—OCH2O—);
- or a pharmaceutically acceptable salt thereof.
13 more elements
A compound of formula (I):
- wherein
- R is a —L-Det;
- L is a divalent (C2-C10)alkyl, (C2-C10)alkenyl, or (C2-C10)alkynyl chain optionally comprising one or more —O—, —S—, or N(Z) in the chain and optionally substituted on carbon with one or more oxo (═O);
- A is NH, O or S;
- B is NH, O, or S;
- C is O or S;
- D is CH;
- E is CH;
- F is CH;
- X is (CH2)2, (CH2)3 or CH═CH;
- wherein the ring comprising F═D—E is optionally substituted with one or more halo, OH, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)C(O), (C1-C6)alkyl-S, NH2, SH, N(Z)2;
- each Z is H or (C1-C6)alkyl;
- Det is
- wherein
- M is Technetium-99m or Rhenium-186;
- R1 and R2 are each independently H or together are oxo;
- or a pharmaceutically acceptable salt thereof.
14 more elements
A compound of formula (I):
- wherein
- R is a —L-Det;
- L is a divalent (C2-C10)alkyl, (C2-C10)alkenyl, or (C2-C10)alkynyl chain optionally comprising one or more —O—, —S—, or N(Z) in the chain and optionally substituted on carbon with one or more oxo (═O);
- A is NH, O or S;
- B is NH, O, or S;
- C is O or S;
- D is CH;
- E is CH;
- F is CH;
- X is (CH2)2, (CH2)3 or CH═CH;
- wherein the ring comprising F═D-E is optionally substituted with one or more halo, OH, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)C(O), (C1-C6)alkyl-S, NH2, SH, N(Z)2;
- Det is
- and each Z is H or (C1-C6)alkyl.
10 more elements
A compound of the formula:
Dependencies are inferred from the claim text.