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US 8,710,047 B2Granted
5-HT3 receptor modulators, methods of making, and use thereof
AssigneeAlbany Molecular Research, Inc.
InventorsDavid D. Manning, Christopher L. Cioffi
Life of this patent
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Abstract
Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.
Claims10
A compound having the following formula:
- wherein:
- X is CH or N;
- each R1 is independently selected from the group consisting of H, halogen, —OR4, or C1-C6 alkyl, wherein C1-C6 alkyl is optionally substituted with from 1 to 3 substituents independently selected at each occurrence thereof from C1-C3 alkyl, halogen, —CN, —OR7, —NR7R8, and phenyl which is optionally substituted 1-3 times with halogen, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, —CN, —OR7, or —NR7R8;
- R2 is H;
- R4 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxyalkyl, C3-C6 cycloalkyl, C4-C7 cycloalkylalkyl, —C(O)R6, phenyl, or benzyl, wherein phenyl or benzyl is optionally substituted 1 to 3 times with halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, or C1-C4 alkoxy;
- R6 is C1-C4 alkyl, C1-C4 haloalkyl, or phenyl;
- R7 and R8 are each independently H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxyalkyl, C3-C6 cycloalkyl, C4-C7 cycloalkylalkyl, —C(O)R6, phenyl, or benzyl, wherein phenyl or benzyl is optionally substituted from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, and C1-C4 alkoxy;
- n is 1 or 2;
- and
- p is 0, 1, 2, or 3;
- or an oxide thereof or a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.