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US 2016/0376568 A1Published application
Thienopyrrole compounds and uses thereof
AssigneePromega Corporation
InventorsSarah Duellman, Matthew B. Robers, Joel R. Walker, Wenhui Zhou, Chad Zimprich
Life of this patent
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Abstract
Thienopyrrole compounds that may inhibit Oplophorus-derived luciferases are disclosed, as well as compositions and kits comprising the thienopyrrole compounds, and methods of using the thienopyrrole compounds.
Claims33
A compound of formula (I), or a salt thereof:
- wherein:
- the dashed line represents the presence or absence of a bond;
- n is 0, 1, 2, 3, 4 or 5;
- X is CH, N, O, or S;
- wherein, when the dashed line represents the presence of a bond, X is CH or N, and
- when the dashed line represents the absence of a bond, X is O or S;
- A is an optionally substituted phenyl ring, or an optionally substituted 5- or 6-membered heteroaryl ring;
- R1 and R2 are each independently selected from the group consisting of hydrogen, optionally substituted C1-C8 alkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl, optionally substituted alkoxyalkyl and optionally substituted alkoxyalkoxyalkyl;
- and
- R3 and R4 are each independently selected from the group consisting of hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C3-C8-cycloalkyl, optionally substituted C3-C8-cycloalkylalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, and optionally substituted heterocyclylalkyl;
- or R3 and R4, together with the nitrogen atom to which they are attached, together form an optionally substituted ring.
8 more elements
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-34. (canceled)
A method of inhibiting an Oplophorus-derived luciferase, the method comprising contacting the Oplophorus-derived luciferase with a compound of formula (II):
- wherein:
- the dashed line represents the presence or absence of a bond;
- n is 0, 1, 2, 3, 4 or 5;
- X is CH, N, O, or S;
- wherein, when the dashed line represents the presence of a bond, X is CH or N, and
- when the dashed line represents the absence of a bond, X is O or S;
- A is an optionally substituted phenyl ring, or an optionally substituted 5- or 6-membered heteroaryl ring;
- R4 and R2 are each independently selected from the group consisting of hydrogen, optionally substituted C1-C8 alkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl, optionally substituted alkoxyalkyl and optionally substituted alkoxyalkoxyalkyl;
- Z is selected from the group consisting of —NR3R4 and —OR5;
- and
- R3, R4 and R5 are each independently selected from the group consisting of hydrogen, optionally substituted C1-C8 alkyl, optionally substituted C3-C8-cycloalkyl, optionally substituted C3-C8-cycloalkylalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, and optionally substituted heterocyclylalkyl;
- or R3 and R4, together with the nitrogen atom to which they are attached, together form an optionally substituted ring.
9 more elements
-68. (canceled)
Dependencies are inferred from the claim text.