Indazole-carboxamide compounds

A compound, alkyl technology, applied in the field of treatment or prevention of medical conditions mediated by 5-HT4 receptor activity to achieve good bioavailability

Inactive Publication Date: 2007-11-28
THERAVANCE INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Although medicinal agents modulate 5-HT 4 Broad-range utility for receptor activity, but little 5-HT at present 4 Agonist compounds for clinical use

Method used

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  • Indazole-carboxamide compounds
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Examples

Experimental program
Comparison scheme
Effect test

example A

[0376] Prepare hard gelatin capsules for oral administration as follows:

[0377] Ingredient quantity

[0378] Compound of the present invention 50mg

[0379] Lactose (spray dried) 200mg

[0380] Magnesium stearate 10mg

[0381] Representative procedure: The ingredients are fully blended and then packed in hard gelatin capsules (each capsule contains 260 mg of composition).

example B

[0383] Prepare hard gelatin capsules for oral administration as follows:

[0384] Ingredient quantity

[0385] The compound of the present invention 20mg

[0386] Starch 89mg

[0387] Microcrystalline cellulose 89mg

[0388] Magnesium stearate 2mg

[0389] Representative procedure: The ingredients are thoroughly blended and then passed through a 45 mesh U.S. sieve and filled into hard gelatin capsules (each capsule contains 260 mg of composition).

example C

[0391] The capsules for oral administration are prepared as follows:

[0392] Ingredient quantity

[0393] Compound of the present invention 10mg

[0394] Polyoxyethylene sorbitan monooleate 50mg

[0395] Starch powder 250mg

[0396] Representative procedure: The ingredients are fully blended and then packed in gelatin capsules (each capsule contains 310 mg of composition).

[0397] Formulation example D

[0398] The lozenges for oral administration are prepared as follows:

[0399] Ingredient quantity

[0400] Compound of the present invention 5mg

[0401] Starch 50mg

[0402] Microcrystalline cellulose 35mg

[0403] Polyvinylpyrrolidone (10wt.% in water) 4mg

[0404] Sodium carboxymethyl starch 4.5mg

[0405] Magnesium stearate 0.5mg

[0406] Talc 1mg

[0407] Representative procedure: Pass the active ingredients, starch and cellulose through a 45-mesh U.S. sieve and mix thoroughly. The solution of polyvinylpyrrolidone is mixed with the resulting powde...

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Abstract

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.

Description

Technical field [0001] The present invention relates to use as 5-HT 4 Indazole-carboxamide compounds as receptor agonists. The present invention also relates to a pharmaceutical composition comprising the compound, the use of the compound to treat or prevent 5-HT 4 Methods for medical conditions mediated by receptor activity, and methods and intermediates for preparing the compounds. Background technique [0002] Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter widely distributed throughout the body in both the central nervous system and the peripheral system. At least seven serotonin receptor subtypes have been identified and the interaction between serotonin and these different receptors is related to various physiological functions. Therefore, the industry is essentially interested in the development of therapeutic agents that target specific 5-HT receptor subtypes. [0003] Specifically, 5-HT 4 The characteristics of receptors and the identification of drugs that i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D451/04A61P9/00A61K31/46
CPCC07D451/04A61P1/00A61P1/04A61P1/10A61P1/12A61P43/00A61P9/00C07D451/02A61K31/46
Inventor 保罗·R·法瑟雷罗兰·根德龙亚当·戈德布卢姆丹尼尔·D·朗丹尼尔·马凯斯德里克·S·特纳崔锡基
Owner THERAVANCE INC
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