76 results about "5-HT4 receptor" patented technology

The invention provides novel quinolinone-carboxamide 5-HT₄ receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT₄ receptor activity, and processes and intermediates useful for preparing such compounds.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R<1 >represents a hydrogen atom or a halogen atom; R<2 >represents a hydrogen atom, etc.; R<3 >represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R<3 >is substituted by at least one substituent selected from the group consisting of substituents alpha; said substituents alpha is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents alpha, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R<1 >represents a hydrogen atom or a halogen atom; R<2 >represents a methyl group or an ethyl group; R<3 >represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R<3 >is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and protons pumps.

An indazole compound having a piperazinyl moiety in the structure thereof, which is a 5-HT.sub.4 receptor agonist which is useful in the treatment of digestive tract disorders.

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

[Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT_2B receptor and 5-HT₇ receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

[Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT_2B receptor and 5-HT₇ receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT_2B receptor and 5-HT₇ receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

The invention relates to methods and compositions for the prevention, treatment, or management of gastrointestinal disorders or symptoms thereof, employing two or more agents or compounds to provide a triple site action on 5-HT3 receptors, 5-HT4 receptors, and at least one of H2 receptors and proton pumps.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.

This invention relates to Compound A or a pharmaceutically acceptable salt thereof with 5-HT4 agonistic activities, which is useful in the treatment of gastrointestinal diseases. This invention also relates to a pharmaceutical composition for the treatment of gastrointestinal diseases which comprises a therapeutically effective amount of Compound A or a pharmaceutically acceptable salt thereof. Further this invention relates to a method for the treatment of gastrointestinal diseases in an animal subject including a mammalian subject, which comprises administering to the animal subject including a mammalian subject Compound A or a pharmaceutically acceptable salt thereof.

The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5 HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

The present invention relates to novel piperazine derivatives or pharmaceutically acceptable salts thereof, a process for preparing the same, and in particular, a high binding for Serotonin 1A(5-hydroxytryptamine; 5-HT1A) receptor, a pharmaceutical composition for treatment and/or prevention of depression and anxiety including an effective amount of the piperazine compound, and a method of treating depression, anxiety and other conditions related to 5-HT1A receptor in a mammal.

The present invention provides a novel benzamide derivative or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a 5-HT₄ receptor agonist containing the same as an active ingredient. Benzamide derivatives of the present invention have a superior affinity for 5-HT₄ receptors, a capability to reduce a gastric emptying time and a low toxicity, and consequently are therapeutically effective for the treatment of a variety of diseases associated with 5-HT₄ receptors.

The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds of Formula (I). The invention also provides pharmaceutical compositions comprising such compounds, the use such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds. Wherein; R¹ is hydrogen, halo, hydroxy, C_1-4 alkyl, or C_1-4 alkoxy; R² is C_3-4 alkyl, or C_3-6cycloalkyl; R³ is hydrogen or C_1-3 alkyl: R⁴ is S(O)₂R⁶ or C(O)R⁷; R⁵ is hydrogen, C_1-3alkyl, C_2-3 alkyl substituted with —OH or C_1-3 alkoxy, or —CH₂-pyrydyl; R⁶ is C_1-3 alkyl; or R⁵ and R⁶ taken together from C_3-4 alkylenyl; and R⁷ is hydrogen, C_1-3alkyl, or pyrydyl; or pharmaceutically-acceptable salt or solvate or stereoisomer thereof.