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US 2010/0075976 A1Published application
Substituted piperazinyl pyrazines and pyridines as 5-ht7 receptor antagonists
AssigneeEli Lilly and Company
InventorsMichael Philip Cohen, Sarah Lynne Hellman, Sean Patrick Hollinshead, Sandra Ann Filla, Michael Wade Tidwell
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Abstract
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is —C(H)═ or —N═; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.
Claims24
A compound of the formula:
- where:
- A is —C(H)═ or —N═,
- R1 is selected from the group consisting of phenyl optionally substituted with methoxy or 1 to 3 independently selected chloro or fluoro substituents;
- pyrazol-4-yl optionally substituted with 1 to 3 methyl or ethyl groups;
- imidazolyl optionally substituted with 1 or 2 C1-C3 methyl or ethyl;
- pyridyl optionally substituted with fluoro or chloro;
- and thienyl;
- R2 is hydrogen or methyl;
- m is 0, 1, or 2;
- R3 is selected from the group consisting of hydrogen, fluoro, chloro, hydroxy, methoxy, hydroxymethyl, cyanomethyl, methoxymethyl, acetyl, methylcarbonylamino, methylcarbonylaminomethyl, pyrazol-1-ylmethyl, and triazolylmethyl, provided that when R3 is hydrogen, m is not 0;
- each R4 is independently selected from the group consisting of fluoro, chloro, methyl, and methoxy;
- or alternatively, two R4 groups together with the phenyl to which they are attached join to form an indol-4-yl group;
- or a pharmaceutically acceptable salt thereof.
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Dependencies are inferred from the claim text.