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Indazole compound

A compound, the technology of ethylindazole, applied in the direction of active ingredients of silicon compounds, organic chemistry, drug combination, etc., can solve the problems such as no suggestion, no disclosure of β3 adrenergic receptor selective stimulation, no teaching, etc.

Inactive Publication Date: 2011-08-31
ASAHI KASEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] However, Patent Document 3 does not suggest an advantage of a drug capable of preferentially stimulating the β3 adrenergic receptor compared to the case of targeting the α1 adrenoceptor, nor does it teach that a compound having a specific structure is compatible with a drug targeting the α1 adrenoceptor. content that even preferentially stimulates the β3 adrenoceptors compared to the
[0015] In addition, Patent Documents 4 and 5 describe compounds [the following general formula (5) or (6)] having a β3 adrenergic receptor stimulating effect, but there is no disclosure about β3 adrenoceptor stimulation compared with α1 adrenoceptor stimulation. Selective stimulation of adrenergic receptors

Method used

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Examples

Experimental program
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Embodiment

[0613] The present invention will be further described based on examples, reference examples, and test examples, but the scope of the present invention is not limited to the following examples.

[0614] In the following examples, various analyzes were performed as follows.

[0615] (1) Precoated silica gel 60F254 (manufactured by Merck, product number 5715-1M) was used for thin layer chromatography (TLC). After developing with chloroform:methanol (1:0~1:1) or ethyl acetate:hexane (1:0~0:1), irradiate with UV (254nm or 365nm), pass iodine solution, potassium permanganate Confirm the color development of aqueous solution, phosphomolybdic acid (ethanol solution), ninhydrin or dinitrophenylhydrazine hydrochloric acid solution.

[0616] (2) Column chromatography was performed by the following method.

[0617] For the case described as "COLUMN-A", use Multi Prep YFLC (manufactured by Yamazensha), and use Hi-Flash made by the company for the column TM Column-Silicagel series.

...

Embodiment 6

[0664]

Embodiment 19

[0666]

[0667] (R)-N-(2-fluoro-5-(2-iodo-1-(triethylsilyloxy)ethyl)phenyl)methylsulfonamide: International Publication Patent No. WO97 / 25311 ( Cited here) Intermediate 101

[0668]

[0669] (R)-N-(2-Chloro-5-(2-iodo-1-(triethylsilyloxy)ethyl)phenyl)methylsulfonamide: International Patent No. WO97 / 25311 Intermediate 107

[0670]

[0671] 1-Benzyl-3-methylindazol-6-ol: Reference Example 11 of International Laid-Open Patent No. WO03 / 035620

[0672]

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PUM

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Abstract

Disclosed are a compound represented by general formula (A-1) or a salt thereof and a compound represented by general formula (1) or a salt thereof. The compound represented by general formula (A-1) or the salt thereof and the compound represented by general formula (1) or the salt thereof have an agonistic activity on a belta3 adrenergic receptor, and are therefore useful as therapeutic and prophylactic agents for diabetes, obesity, hyperlipemia, depression, gallstone, diseases associated with increased movement of the biliary tract, diseases associated with hyperfunction of the digestive tract, interstitial cystitis, overactive bladder or urinary incontinence or therapeutic and prophylactic agents for diseases associated with decreased tears.

Description

technical field [0001] The present invention relates to an indazole compound having β3 adrenoreceptor stimulating effect, a pharmaceutical composition containing the indazole compound, and their use. Background technique [0002] Norepinephrine and epinephrine are known to exhibit various actions on nerves, smooth muscles, and the like as neurotransmitters and hormones in vivo. Therefore, adrenergic receptors coupled to and responsive to the neurotransmitter / hormone are considered to be target molecules of important drugs in various treatments. [0003] Adrenoceptors belong to the family of G protein-coupled receptors and are classified into three subfamilies, α 1 、α 2 and β-adrenergic receptors. That is, it is known that the adrenergic receptor subfamily is activated by the coupling of norepinephrine and epinephrine, and then utilizes different intracellular signaling pathways, and it has been suggested in the literature that the increase in calcium ions is caused by the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/56A61K31/416A61P13/00A61P43/00
CPCA61K31/695A61K31/416C07D303/08C07D231/56C07D405/04A61P13/00A61P13/10A61P43/00
Inventor 中野诚志岩并泰资山西庆和田康弘森本晃史
Owner ASAHI KASEI PHARMA
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