JPWO2006051797A1 - 間質性膀胱炎の治療薬 - Google Patents
間質性膀胱炎の治療薬 Download PDFInfo
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- JPWO2006051797A1 JPWO2006051797A1 JP2006544902A JP2006544902A JPWO2006051797A1 JP WO2006051797 A1 JPWO2006051797 A1 JP WO2006051797A1 JP 2006544902 A JP2006544902 A JP 2006544902A JP 2006544902 A JP2006544902 A JP 2006544902A JP WO2006051797 A1 JPWO2006051797 A1 JP WO2006051797A1
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- interstitial cystitis
- capsaicin
- acid derivative
- phenoxyacetic acid
- acceptable salt
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- 0 Cc(cc(CCN[C@@](*1)[C@@](c(cc2)ccc2O)O)c1c1)c1OCC(*)=O Chemical compound Cc(cc(CCN[C@@](*1)[C@@](c(cc2)ccc2O)O)c1c1)c1OCC(*)=O 0.000 description 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/22—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
- A61K31/222—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
- A61K31/24—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
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- Chemical & Material Sciences (AREA)
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- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
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- Neurology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Pain & Pain Management (AREA)
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- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Nutrition Science (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Description
これらのうち、カプサイシンやレジニフェラトキシンの作用機序はC−繊維、すなわちカプサイシン感受性知覚神経の脱感作と考えられており、ムスカリンM3受容体選択的結合作用を有するキヌクリジン−3’−イル 1−フェニル−1,2,3,4−テトラヒドロイソキノリン−2−カルボキシレートがカプサイシン感受性知覚神経抑制作用を有することが報告されている(特許文献1参照)。
排尿障害プラクティス、株式会社メディカルレビュー社、2004年、第12巻、第1号、
20%ウレタン0.15mLを腹腔内投与して麻酔した雌性Balb/cマウス(日本SLC社)に、ポリエチレンチューブPE50を用いて気管カニュレーションを施した。尿道を介してポリエチレンチューブPE10を膀胱内に挿入し、生理食塩水及び2等量の水酸化ナトリウムで溶解させた濃度10μM(−)−2−[4−[2−[[(1S,2R)−2−ヒドロキシ−2−(4−ヒドロキシフェニル)−1−メチルエチル]アミノ]エチル]−2,5−ジメチルフェノキシ]酢酸エチルの塩酸塩(以下「化合物1」という。)溶液を各種濃度に生理食塩水で希釈したものを注入した。注入から1時間後、0.1%DMSO及び0.1%ツイーン80を含む生理食塩水に溶解させたエバンスブルー(30mg/kg)及びカプサイシン(0.3mg/kg)の溶液(10mL/kg)を尾静脈投与した。投与から正確に5分後、頚椎脱臼させ、膀胱を摘出した。摘出した膀胱の尿、血液を取り除いた後、膀胱湿重量を測定し、あらかじめ各穴にホルムアミドを150μLずつ分注した96穴マイクロプレートに摘出した膀胱を各穴に入れた。一晩、ホルムアミドに膀胱を浸けた後、上清100μLを620nmの波長で吸光度を測定し膀胱組織内色素を定量した。さらに、膀胱湿重量1mg当たりのエバンスブルー色素量を算出した。なお、生理食塩水を膀胱内に注入し、カプサイシンを含まないエバンスブルー溶液を投与したマウスを正常対照とした。
結果を図1に平均値±標準偏差で示した。正常対照群とカプサイシン刺激群との群間の有意差は、student t-testで検定した。化合物1投与群と未投与群との群間の有意差を一元分散分析に続くDunnettの多群間比較で検定した。p<0.05を有意とした。
対照群と溶媒群との間でエバンスブルー色素量は溶媒群で有意に高かった(p<0.01)。また、化合物1は濃度依存的にエバンスブルー色素量を減少させた。特に、1μM投与群ではエバンスブルー色素量は有意に減少し(p<0.01)、対照群と同レベルであった。
試験例1において、化合物1に代えてトルテロジン(Tolterodine)を用い、生理食塩水及び2等量の水酸化ナトリウムに代えてハルトマン液を用いた以外は、試験例1と同様にして膀胱組織内色素を定量し、さらにエバンスブルー色素量を算出した。なお、ハルトマン液を膀胱内に注入し、カプサイシンを含まないエバンスブルー溶液を投与したマウスを正常対照とした。
対照群と溶媒群との間でエバンスブルー色素量は溶媒群で有意に高かった(p<0.01)。トルテロジン投与群と溶媒群ではエバンスブルー色素量に有意差が認められなかった。
Claims (3)
- フェノキシ酢酸誘導体が、(−)−2−[4−[2−[[(1S,2R)−2−ヒドロキシ−2−(4−ヒドロキシフェニル)−1−メチルエチル]アミノ]エチル]−2,5−ジメチルフェノキシ]酢酸エチルであることを特徴とする請求項1記載の間質性膀胱炎の治療薬。
- 一般式(I)で表されるフェノキシ酢酸誘導体若しくはその薬理学的に許容される塩又はその水和物若しくは溶媒和物を含有することを特徴とするカプサイシン感受性知覚神経抑制薬。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2006544902A JP4928272B2 (ja) | 2004-11-10 | 2005-11-09 | 間質性膀胱炎の治療薬 |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2004325992 | 2004-11-10 | ||
JP2004325992 | 2004-11-10 | ||
PCT/JP2005/020499 WO2006051797A1 (ja) | 2004-11-10 | 2005-11-09 | 間質性膀胱炎の治療薬 |
JP2006544902A JP4928272B2 (ja) | 2004-11-10 | 2005-11-09 | 間質性膀胱炎の治療薬 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2006051797A1 true JPWO2006051797A1 (ja) | 2008-05-29 |
JP4928272B2 JP4928272B2 (ja) | 2012-05-09 |
Family
ID=36317138
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006544902A Expired - Fee Related JP4928272B2 (ja) | 2004-11-10 | 2005-11-09 | 間質性膀胱炎の治療薬 |
Country Status (9)
Country | Link |
---|---|
US (1) | US7446128B2 (ja) |
EP (1) | EP1810673A4 (ja) |
JP (1) | JP4928272B2 (ja) |
KR (1) | KR20070084500A (ja) |
CN (1) | CN101056627B (ja) |
AR (1) | AR051665A1 (ja) |
CA (1) | CA2586459A1 (ja) |
TW (1) | TWI356699B (ja) |
WO (1) | WO2006051797A1 (ja) |
Families Citing this family (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2008155818A1 (ja) * | 2007-06-19 | 2008-12-24 | Kyorin Pharmaceutical Co., Ltd. | 頻尿及び尿失禁の予防又は治療剤 |
EP2818166A1 (en) * | 2013-06-26 | 2014-12-31 | Laboratorios del Dr. Esteve S.A. | Use of sigma receptor ligands for the prevention and treatment of pain associated to interstitial cystitis/bladder pain syndrome (IC/BPS) |
JP7223477B2 (ja) * | 2018-10-10 | 2023-02-16 | 花王株式会社 | Trpv4活性抑制剤 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000002846A1 (en) * | 1998-07-08 | 2000-01-20 | Kissei Pharmaceutical Co., Ltd. | Phenoxyacetic acid derivatives and medicinal compositions containing the same |
WO2003006019A1 (fr) * | 2001-07-10 | 2003-01-23 | Yamanouchi Pharmaceutical Co., Ltd. | Composition medicinale destinee au traitement de la cystite interstitielle |
WO2003024916A1 (fr) * | 2001-09-13 | 2003-03-27 | Kissei Pharmaceutical Co., Ltd. | Cristaux d'un derive d'hydroxynorephedrine |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE602004003172T2 (de) * | 2003-03-21 | 2007-09-27 | Dynogen Pharmaceuticals Inc., Waltham | Verfahren zur behandlung von erkrankungen der unteren harnwege mit antimuskarinika und mit modulatoren der alpha-2-delta untereinheit des kalziumkanals |
SI1620085T1 (sl) | 2003-05-05 | 2008-12-31 | Kissei Pharmaceutical | Uporaba derivatov fenoksiocetne kisline za zdravljenje hiperaktivnega sečnega mehurja |
-
2005
- 2005-11-01 TW TW094138235A patent/TWI356699B/zh not_active IP Right Cessation
- 2005-11-07 US US11/267,299 patent/US7446128B2/en not_active Expired - Fee Related
- 2005-11-09 JP JP2006544902A patent/JP4928272B2/ja not_active Expired - Fee Related
- 2005-11-09 KR KR1020077011690A patent/KR20070084500A/ko not_active Application Discontinuation
- 2005-11-09 CA CA002586459A patent/CA2586459A1/en not_active Abandoned
- 2005-11-09 EP EP05803324A patent/EP1810673A4/en not_active Withdrawn
- 2005-11-09 WO PCT/JP2005/020499 patent/WO2006051797A1/ja active Application Filing
- 2005-11-09 CN CN2005800381676A patent/CN101056627B/zh not_active Expired - Fee Related
- 2005-11-09 AR ARP050104682A patent/AR051665A1/es not_active Application Discontinuation
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000002846A1 (en) * | 1998-07-08 | 2000-01-20 | Kissei Pharmaceutical Co., Ltd. | Phenoxyacetic acid derivatives and medicinal compositions containing the same |
WO2003006019A1 (fr) * | 2001-07-10 | 2003-01-23 | Yamanouchi Pharmaceutical Co., Ltd. | Composition medicinale destinee au traitement de la cystite interstitielle |
WO2003024916A1 (fr) * | 2001-09-13 | 2003-03-27 | Kissei Pharmaceutical Co., Ltd. | Cristaux d'un derive d'hydroxynorephedrine |
Also Published As
Publication number | Publication date |
---|---|
CN101056627A (zh) | 2007-10-17 |
WO2006051797A1 (ja) | 2006-05-18 |
EP1810673A4 (en) | 2009-11-11 |
TWI356699B (en) | 2012-01-21 |
CN101056627B (zh) | 2010-06-16 |
KR20070084500A (ko) | 2007-08-24 |
US7446128B2 (en) | 2008-11-04 |
TW200621226A (en) | 2006-07-01 |
US20060100275A1 (en) | 2006-05-11 |
JP4928272B2 (ja) | 2012-05-09 |
CA2586459A1 (en) | 2006-05-18 |
EP1810673A1 (en) | 2007-07-25 |
AR051665A1 (es) | 2007-01-31 |
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