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US 2019/0315689 A1Published application
Myeloperoxidase Imaging Agents
AssigneeThe General Hospital Corporation
InventorsJohn W. Chen, Cuihua Wang, Edmund J. Keliher
Life of this patent
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Abstract
Provided herein are compounds useful as imaging agents. Exemplary compounds provided herein are useful as myeloperoxidase imaging agents using positron emission tomography or fluorescence imaging techniques. Methods for preparing the compounds provided herein and diagnostic methods using radiolabeled and unlabeled compounds are also provided.
Claims53
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- L1 is selected from the group consisting of a bond, —C(O)—, —C(O)O—, —C(O)NRa1, —C(O)(C1-6 alkylene)-, and —C(O)(C1-6 alkyleneoxy)-;
- R1 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl, wherein each C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl is optionally substituted by 1, 2, 3, or 4 substituents independently selected from OH, halo, C1-6 alkoxy, and C1-6 haloalkyl;
- L2 is selected from the group consisting of —(C1-6 alkylene)-(C3-10 cycloalkylene)-, —(C1-6 alkylene)-(C6-10 arylene)-, —(C1-6 alkylene)-(4-10 membered heterocycloalkylene)-, —(C1-6 alkylene)-(5-10 membered heteroarylene)-, —C(O)—, —C(O)O—, —C(O)NRa2-, —C(O)(C1-6 alkylene)-, and —C(O)(C1-6 alkyleneoxy)-;
- R2 is selected from the group consisting of C1-6 alkoxy, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl, wherein each C1-6 alkoxy, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl is optionally substituted by 1, 2, 3, or 4 substituents independently selected from OH, halo, C1-6 alkoxy, and C1-6 haloalkyl;
- L3 is selected from the group consisting of a bond, —C(O)—, —C(O)O—, —C(O)NRa3, —C(O)(C1-6 alkylene)-, —C(O)(C1-6 alkyleneoxy)-, —C(O)N(Ra3)(C1-6 alkylene)-, —C(O)N(Ra3)(C1-6 alkylene)-di(C1-6 alkyl)amino, and —C(O)N(Ra3)(C1-6 alkyleneoxy)-;
- R3 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, and —C(O)N(Ra3)(C1-6 haloalkoxy), wherein each C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 alkoxy, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, and 5-10 membered heteroaryl, is optionally substituted by 1, 2, 3, or 4 substituents independently selected from OH, halo, C1-6 alkoxy, and C1-6 haloalkyl;
- or alternatively, -L3-R3 forms an oxo group;
- R4 is selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl;
- and each R1, Ra2, and Ra3 is independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, and C1-6 haloalkyl.
7 more elements
Dependencies are inferred from the claim text.