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Indole derivative and pharmacologically acceptable salt thereof

A kind of technology of pharmaceutically acceptable salt and compound, applied in the field of indole derivatives or pharmaceutically acceptable salts thereof, can solve the problems such as no suggestion or disclosure of receptor antagonism

Inactive Publication Date: 2012-06-13
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, there is no suggestion or disclosure that these compounds have EP 1 receptor antagonism

Method used

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  • Indole derivative and pharmacologically acceptable salt thereof
  • Indole derivative and pharmacologically acceptable salt thereof
  • Indole derivative and pharmacologically acceptable salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0143] Preferred embodiments of the present invention are as follows:

[0144] Y is methylene;

[0145] A is a benzene ring or a pyridine ring;

[0146] R 1 is a hydrogen atom;

[0147] R 2 is a phenyl group or a 5-membered aromatic heterocyclic group;

[0148] R 3 is methoxy or ethoxy; and

[0149] R N is a hydrogen atom.

[0150] Examples of specific compounds encompassed within this embodiment include the following compounds:

[0151] 6-(6-methoxy-2-phenyl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (Example 4-1), 3-(6-methoxy-2-benzene Base-1H-indol-3-ylmethyl)benzoic acid (Example 4-2), 3-(6-methoxy-2-thiophen-3-yl-1H-indol-3-ylmethyl ) benzoic acid (embodiment 4-12), 6-(6-ethoxy-2-phenyl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (embodiment 4-34), 6 -(6-methoxy-2-thiophen-3-yl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (Example 11-1), 6-[2-(3-fluorobenzene Base)-6-methoxy-1H-indol-3-ylmethyl]pyridine-2-carboxylic acid (Example 11-5), 6-(2-furan-3-...

Embodiment approach 2

[0153] Another preferred embodiment of the present invention is as follows:

[0154] Y is methylene;

[0155] A is a benzene ring or a pyridine ring;

[0156] R 1 is a hydrogen atom;

[0157] R 2 is unsubstituted phenyl;

[0158] R 3 is methoxy; and

[0159] R N is a hydrogen atom.

[0160] Examples of specific compounds encompassed within this embodiment include the following compounds:

[0161] 6-(6-methoxy-2-phenyl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (Example 4-1), 3-(6-methoxy-2-benzene Base-1H-indol-3-ylmethyl)benzoic acid (Example 4-2), 2-fluoro-3-(6-methoxy-2-phenyl-1H-indol-3-ylmethyl) Base) benzoic acid (Example 16-9), 6-(6-methoxy-5-methyl-2-phenyl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (Example 16-12), 6-(5-chloro-6-methoxy-2-phenyl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (embodiment 16-13), 6-( 5-fluoro-6-methoxy-2-phenyl-1H-indol-3-ylmethyl)pyridine-2-carboxylic acid (Example 16-16), and 2-fluoro-5-(6-methyl Oxy-2-phenyl-1H-i...

Embodiment approach 3

[0163] Another preferred embodiment of the present invention is as follows:

[0164] Y is methylene;

[0165] A is a benzene ring or a pyridine ring;

[0166] R 1 is a hydrogen atom;

[0167] R 2 is a substituted phenyl group;

[0168] R 3 is methoxy; and

[0169] R N is a hydrogen atom.

[0170] Examples of specific compounds encompassed within this embodiment include the following compounds:

[0171] 6-[2-(3-fluorophenyl)-6-methoxy-1H-indol-3-ylmethyl]pyridine-2-carboxylic acid (Example 11-5), 6-[2-(4 -fluorophenyl)-6-methoxy-1H-indol-3-ylmethyl]pyridine-2-carboxylic acid (Example 11-13), 6-[2-(3-chlorophenyl)-6 -Methoxy-1H-indol-3-ylmethyl]pyridine-2-carboxylic acid (Example 11-21), 6-[6-methoxy-2-(3-methoxyphenyl)- 1H-indol-3-ylmethyl]pyridine-2-carboxylic acid (Example 11-34), 6-[2-(3,4-difluorophenyl)-6-methoxy-1H-indole -3-ylmethyl]pyridine-2-carboxylic acid (Example 16-2), 6-[6-methoxy-2-(3,4,5-trifluorophenyl)-1H-indole-3 -ylmethyl]pyridine-2-carboxylic a...

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Abstract

Disclosed is a compound represented by general formula (I), which has EP1 receptor antagonist activity, or a pharmacologically acceptable salt thereof. (In general formula (I), A represents a benzene ring or the like; Y represents a C1-6 alkylene group or the like; RN represents a hydrogen atom or a C1-6 alkyl group; R1 represents a hydrogen atom, a C1-6 alkyl group or the like; R2 represents an optionally substituted phenyl group, an optionally substituted five-membered aromatic heterocyclic group, an optionally substituted six-membered aromatic heterocyclic group or the like; R3 represents a halogen atom, a C1-6 alkoxy group or the like; R4 represents a hydrogen atom or the like; and R5 represents a hydrogen atom or the like.) The compound of general formula (I) is able to be used as an agent for treatment or prevention of LUTS, in particular symptoms of OABS.

Description

technical field [0001] The present invention relates to a drug with EP that can be used as a medicine 1 An indole derivative or a pharmaceutically acceptable salt thereof with receptor antagonism, a pharmaceutical composition comprising the indole derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical application thereof. Background technique [0002] With the progress of an aging society and a stressful society, the number of patients suffering from lower urinary tract dysfunction (LUTD) has increased. LUTD is a collective term for retention disorders and dysuria, and these symptoms derived from LUTD are lower urinary tract symptoms (LUTS). One of the LUTS is overactive bladder syndrome (OABs). In some instances, OABs may be commonly referred to as overactive bladder (OAB). In any case, it is a disorder defined as "a symptom syndrome of predominantly urge to urinate, often accompanied by frequency and nocturnal frequency. Urgency incontinence is n...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/18A61K31/404A61K31/422A61K31/427A61K31/4439A61P13/02A61P43/00C07D401/04C07D401/06C07D401/14C07D405/04C07D405/06C07D405/14C07D409/04C07D409/06C07D409/14C07D413/14C07D417/06C07D417/14
CPCC07D417/06C07D209/18C07D413/14C07D401/06C07D405/04A61K31/427C07D409/14C07D409/06C07D405/06C07D401/14C07D417/14C07D409/04A61K31/4439C07D405/14A61K31/422A61K31/404C07D401/04A61P13/00A61P13/02A61P43/00A61K31/454
Inventor 近藤龙大近藤敦志田谷和也川村直裕
Owner KISSEI PHARMA
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