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US 9,844,554 B2Granted
Prodrugs of metopimazine
AssigneeNeurogastrx, Inc.
InventorsCyril De Colle, Pankaj Pasricha, David Wustrow
Life of this patent
Estimating the term…
Abstract
Provided herein are methods, compounds, compositions, and kits for the treatment of an enteric nervous system disorder. Such methods may comprise administering to a subject an effective amount of a phenothiazine compound, a peripherally restricted dopamine decarboxylase inhibitor, and/or a peripherally restricted dopamine D2 receptor antagonist that does not substantially inhibit hERG channels.
Claims20
A compound of Formula V:
- or a salt thereof, wherein:
- X′ is O or NH;
- R5 is C5-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, C4-C7 cycloalkyl, C3-C7 heterocycloalkyl, C6-C10 aryl, or C6-C10 heteroaryl each of which may be unsubstituted or substituted with one or more R6 groups;
- each R6 is independently —OR7, —SR7, —NR7R8, —COOR7, —CONR7R8, —OCOR7, —NR7—CO—R8, C1-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, C4-C7 cycloalkyl, C3-C7 heterocycloalkyl, C6-C10 aryl, or C6-C10 heteroaryl, wherein the alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl may be unsubstituted or substituted with one or more —OR7, —SR7, —NR7R8, —COOR7, —CONR7R8, —OCOR7, or —NR7—CO—R8 groups;
- and
- each of R7 and R8 is independently H, C1-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, C4-C7 cycloalkyl, C3-C7 heterocycloalkyl, C6-C10 aryl, or C6-C10 heteroaryl.
3 more elements
A compound of Formula VII:
- or a salt thereof, wherein:
- X is O or NH;
- R14 is C1-C4 linear or branched alkyl;
- and
- R15 is C1-C6 linear or branched alkyl, phenyl, or C4-C7 cycloalkyl.
2 more elements
A compound of Formula XI, or a salt thereof:
A compound of Formula V:
- or a salt thereof, wherein:
- X′ is O or NH;
- R5 is C1-C10 alkyl substituted with one R6 group selected from —NR7R8, —CONR7R8, and —NR7—CO—R8;
- and
- each of R7 and R8 is independently H, C1-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, C4-C7 cycloalkyl, C3-C7 heterocycloalkyl, C6-C10 aryl, or C6-C10 heteroaryl.
2 more elements
A compound of Formula V:
- or a salt thereof, wherein:
- X′ is O;
- and
- R5 is unsubstituted C2-C10 alkyl, C1-C10 alkenyl, or C1-C10 alkynyl.
1 more element
Dependencies are inferred from the claim text.