Compositions useful for increasing lower esophageal sphincter pressure
OwnerSteven Landau, Theodore Ashburninventors
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Abstract
The present invention relates to a method of increasing the pressure of the lower esophageal sphincter in a subject in need thereof comprising administering to said subject a specified amount of a compound having 5-HT3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The subject in need of treatment is suffering from GERD, including nocturnal GERD.
Claims43
1-24. (canceled)
A method of increasing the pressure of the lower esophageal sphincter in a human subject in need thereof comprising administering to said subject from about 0.5 mg to about 50 mg per day of a compound represented by Formula I:
- wherein:
- R1 represents hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C3-C8 cycloalkyl group, a C6-C12 aryl group or a C7-C18 aralkyl group;
- R2 represents hydrogen, a C1-C6 alkyl group, halogen, hydroxyl, a C1-C6 alkoxy group, amino, a C1-C6 alkylamino group, nitro, mercapto or a C1-C6 alkylthio group;
- Y represents —O— or
- wherein R3 represents hydrogen or a C1-C6 alkyl group;
- and
- A is represented by
- wherein:
- n is an integer from 1 to about 4;
- R4 represents hydrogen, a C1-C6 alkyl group, a C3-C8 cycloalkyl group or a C7-C18 aralkyl group;
- or a pharmaceutically acceptable salt, solvate, hydrate or N-oxide derivative thereof.
A method of increasing the pressure of the lower esophageal sphincter in a human subject in need thereof comprising administering to said subject from about 1 mg to about 25 mg per day of a compound represented by Formula I:
- wherein:
- R1 represents hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C3-C8 cycloalkyl group, a C6-C12 aryl group or a C7-C18 aralkyl group;
- R2 represents hydrogen, a C1-C6 alkyl group, halogen, hydroxyl, a C1-C6 alkoxy group, amino, a C1-C6 alkylamino group, nitro, mercapto or a C1-C6 alkylthio group;
- Y represents —O— or
- wherein R3 represents hydrogen or a C1-C6 alkyl group;
- and
- A is represented by
- wherein:
- n is an integer from 1 to about 4;
- R4 represents hydrogen, a C1-C6 alkyl group, a C3-C8 cycloalkyl group or a C7-C18 aralkyl group;
- or a pharmaceutically acceptable salt, solvate, hydrate or N-oxide derivative thereof.
A method of increasing the pressure of the lower esophageal sphincter in a human subject in need thereof comprising administering to said subject about 1.5 mg per day of a compound represented by Formula V:
- or a pharmaceutically acceptable salt, solvate or hydrate thereof.
A method of increasing the pressure of the lower esophageal sphincter in a human subject in need thereof comprising administering to said subject about 2.5 mg per day of a compound represented by Formula V:
- or a pharmaceutically acceptable salt, solvate or hydrate thereof.
The method of claim 59, wherein the GERD is nocturnal GERD.
A method of increasing the pressure of the lower esophageal sphincter in a human subject in need thereof comprising administering to said subject about 4.0 mg per day of a compound represented by Formula V:
- or a pharmaceutically acceptable salt, solvate or hydrate thereof.
Dependencies are inferred from the claim text.