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Azolecarboxamide derivative

A technology of azole carboxamides and derivatives, which is applied in the field of azole carboxamide derivatives, can solve problems such as untouched and undisclosed, and achieve high safety, strong effect of improving urination symptoms, and avoiding side effects

Inactive Publication Date: 2009-05-06
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In addition to the above-mentioned Non-Patent Document 8 and Patent Documents 1 to 10, as a compound having a relatively similar structure, in Patent Document 11, a compound represented by the following general formula (XV) is disclosed as a c-fms kinase inhibitor, but it is completely No trkA receptor inhibition involved in the present invention
Furthermore, in this gazette, there is no specific disclosure about compounds having a thiazole or oxazole skeleton substituted at the 2-position except for examples.

Method used

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Examples

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Embodiment

[0440] Hereinafter, the compounds of the present invention will be further specifically described by way of examples. In addition, the production method of the raw material compound is described as a reference example. It should be noted that the production method of the compound of the present invention is not limited to the production method of the specific examples shown below, and it can also be produced by a combination of the above-mentioned production methods or a known production method.

[0441] The following abbreviations are used in Reference Examples and Examples.

[0442] Me: methyl; Et: ethyl; Ac: acetyl; Ms: methylsulfonyl; Ph: phenyl; Boc: tert-butoxycarbonyl; TBS: tert-butyldimethylsilyl; Tf: trifluoro Methanesulfonyl; HOBt: 1-hydroxybenzotriazole; WSC HCl: 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide hydrochloride; DCC: dicyclohexylcarbodiimide imine; CDI: carbonyldiimidazole; DPPA: diphenylphosphoryl azide; DEPC: diethyl cyanophosphonate; THF: tetrahydro...

reference example 1

[0444] 2,4-Difluoro-6-nitrophenyl triflate is produced by reacting trifluoromethanesulfonic anhydride and 2,4-difluoro-6-nitrophenol in pyridine.

reference example 8

[0446] 4-Chloro-3-nitrophenylmethylsulfoxide is produced by reacting m-chloroperbenzoic acid and 4-chloro-3-nitrophenylmethylsulfide in chloroform to oxidize thioether.

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PUM

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Abstract

To provide a therapeutic or prophylactic agent for frequent urination / strong urge to urinate or incontinence associated with overactive bladder, a lower urinary tract disease accompanied by a lower urinary tract pain such as interstitial cystitis and chronic prostatitis or a disease accompanied by a pain, which acts based on excellent trkA receptor-inhibiting activity. [MEANS FOR SOLVING PROBLEMS] Disclosed is a novel azolecarboxamide derivative having an azole ring (e.g., a thiazole or oxazole ring) bound to a benzene, pyridine or pyrimidine ring through a carboxamide. It is confirmed that the azolecarboxamide derivative has a potent trkA receptor-inhibiting activity. It is found that the azolecarboxamide derivative can be used as a very efficient, safe therapeutic or prophylactic agent for a lower urinary tract disease or a disease accompanied by a pain.

Description

technical field [0001] The present invention relates to a drug useful as a medicine, especially as a therapeutic drug for various diseases of urinary frequency, urgency, urinary incontinence, lower urinary tract pain and pain associated with various lower urinary tract diseases including overactive bladder. Azole carboxamide derivatives. Background technique [0002] An overactive bladder is a condition in which there is urgency regardless of the presence or absence of incontinence, usually accompanied by frequency and nocturnal frequency (Non-Patent Document 1). Currently, the treatment of overactive bladder mainly uses anticholinergic drugs, and has shown some therapeutic results. On the other hand, anticholinergics are known to cause side effects such as thirst, constipation, and blurred eyes, and there is a risk of urination, so it has been reported that patients with enlarged prostate and elderly patients should not use them. In addition, it is known that there are pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D263/34A61K31/427A61K31/438A61K31/454A61K31/4545A61K31/496A61K31/4985A61K31/501A61K31/506A61K31/5377A61K31/541A61K31/55A61K31/551A61K31/553A61P13/02A61P13/08A61P13/10A61P19/02A61P25/04A61P43/00C07D277/20C07D277/56C07D413/12C07D413/14C07D417/12C07D417/14C07D471/04C07D471/10C07D487/08C07D491/08
CPCC07D487/08C07D417/14C07D471/04C07D413/04C07D277/56C07D413/14C07D417/04C07D263/48C07D491/08C07D417/12C07D263/34C07D413/12C07D471/10A61P13/00A61P13/02A61P13/08A61P13/10A61P19/02A61P25/02A61P25/04A61P29/00A61P43/00A61K31/427
Inventor 菅泽形造川口贤一松泽崇穗濑尾龙志原田博规须贺亮阿部友亮蓟英范松本俊一郎进崇史棚桥正幸渡边亨
Owner ASTELLAS PHARMA INC
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