JP5042839B2 - 腸疾患の予防及び/又は治療のための医薬 - Google Patents
腸疾患の予防及び/又は治療のための医薬 Download PDFInfo
- Publication number
- JP5042839B2 JP5042839B2 JP2007534461A JP2007534461A JP5042839B2 JP 5042839 B2 JP5042839 B2 JP 5042839B2 JP 2007534461 A JP2007534461 A JP 2007534461A JP 2007534461 A JP2007534461 A JP 2007534461A JP 5042839 B2 JP5042839 B2 JP 5042839B2
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- retinoid
- medicament
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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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
-
- 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
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
- A61P31/06—Antibacterial agents for tuberculosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
上記発明の好ましい態様によれば、腸疾患が炎症性腸疾患、過敏性腸症候群、十二指腸潰瘍、急性腸炎、蛋白漏出性腸症、大腸癌、イレウス、虫垂炎、出血性大腸炎、腸結核、腸ベーチェット、又は大腸憩室症である上記の医薬;腸疾患が炎症性腸疾患である上記の医薬;及び腸疾患がクローン病である上記の医薬が提供される。
より具体的には、非天然型のレチノイドとして、下記の一般式:B−X−A(式中、Bは置換基を有していてもよい芳香族基を示し、Xは連結基を示し、Aは置換基を有していてもよいカルボン酸置換芳香族基又はトロポロニル基を示す)で表されるレチノイドを用いることができる。
例1:Am80のラット炎症性腸疾患モデルでの評価
雄性又は雌性Wistarラット(200 g±5 g)を用いて、炎症性腸疾患モデルを作成した。24時間絶食の後、DNBS(2,4-dinitorobenzenesulfonic acid, 30 mg in 0.5 ml ethanol 30%)を肛門から注腸した。本発明の医薬として4-[(5,6,7,8-テトラヒドロ-5,5,8,8-テトラメチル-2-ナフタレニル)カルバモイル]安息香酸(Am80、一般名「タミバロテン」)を0.3 mg/kg、比較例(陽性対照薬)として市販の潰瘍性大腸炎治療薬であるサラゾスルファピリジン(SASP)を300 mg/kgとなるように、それぞれDNBS注腸24時間前及び2時間前、並びに注腸24時間後から1日1回、5日間投与した。タミバロテン及びSASPは0.5%カルボキシメチルセルロース(Carboxymethylcellulose)に懸濁して経口投与した。対照群には溶媒をSASPと同様なスケジュールで経口投与した。最後の投与から24時間後に剖検し、腸の炎症の度合いを観察した。タミバロテン投与群、SASP投与群、正常群、及び対照群につき、一群各5匹のラットを用いた。
腸潰瘍と炎症のスコア(巨視的)
スコア 観察所見
0:正常
1: 局部的な充血、潰瘍なし
2: 充血の無い潰瘍形成又は大腸壁肥厚
3: 1箇所の炎症と潰瘍形成
4: 2箇所以上の潰瘍と炎症
5: 主な損傷部位が大腸の長さ方向に1センチメートル以上伸延
6-10: 主な損傷部位が大腸の長さ方向に2センチメートル以上伸延するとき、2センチメートル以上の1センチメートルごとにつきスコアが1ずつ増加
雄性又は雌性Wistarラット(200 g±10 g)を用いて、炎症性腸疾患モデルを作成した。24時間絶食の後、DNBS(2,4-dinitorobenzenesulfonic acid, 30 mg in 0.5 ml ethanol 30%)を肛門から注腸した。本発明の医薬として4-[2,3-(2,5-ジメチル-2,5-ヘキサノ)ジベンゾ[b,f][1,4]チアゼピン-11-イル]安息香酸(HX630)を3 mg/kg、4-(5H-7,8,9,10-テトラヒドロ-5,7,7,10,10-ペンタメチルベンゾ-[e]ナフト[2,3-b][1,4]ジアゼピン-13-イル]安息香酸(LE135)を5 mg/kg、又はAm80 0.1 mg/kg及びHX630 3 mg/kg(併用)を用い、、比較例(陽性対照薬)として市販の潰瘍性大腸炎治療薬であるサラゾスルファピリジン(SASP)を300 mg/kgを用いて、それぞれDNBS注腸24時間前及び2時間前、並びに注腸24時間後から1日1回、5日間投与した。各薬物は0.5%カルボキシメチルセルロース(Carboxymethylcellulose)に懸濁して経口投与した。対照群には溶媒を同様なスケジュールで経口投与した。最後の投与から24時間後に剖検し、腸の炎症の度合いを観察した。各群につき一群各5匹のラットを用いた。
腸潰瘍と炎症のスコア(巨視的)
スコア 観察所見
0:正常
1: 局部的な充血、潰瘍なし
2: 充血の無い潰瘍形成又は大腸壁肥厚
3: 1箇所の炎症と潰瘍形成
4: 2箇所以上の潰瘍と炎症
5: 主な損傷部位が大腸の長さ方向に1センチメートル以上伸延
6-10: 主な損傷部位が大腸の長さ方向に2センチメートル以上伸延するとき、2センチメートル以上の1センチメートルごとにつきスコアが1ずつ増加
Claims (1)
- 炎症性腸疾患の予防及び/又は治療のための医薬であって、4-[(5,6,7,8-テトラヒドロ-5,5,8,8-テトラメチル-2-ナフタレニル)カルバモイル]安息香酸を有効成分として含む医薬。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2007534461A JP5042839B2 (ja) | 2005-09-09 | 2006-09-07 | 腸疾患の予防及び/又は治療のための医薬 |
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005261775 | 2005-09-09 | ||
JP2005261775 | 2005-09-09 | ||
PCT/JP2006/317720 WO2007029760A1 (ja) | 2005-09-09 | 2006-09-07 | 腸疾患の予防及び/又は治療のための医薬 |
JP2007534461A JP5042839B2 (ja) | 2005-09-09 | 2006-09-07 | 腸疾患の予防及び/又は治療のための医薬 |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010184584A Division JP5172911B2 (ja) | 2005-09-09 | 2010-08-20 | 癒着の予防及び/又は治療のための医薬 |
Publications (2)
Publication Number | Publication Date |
---|---|
JPWO2007029760A1 JPWO2007029760A1 (ja) | 2009-03-19 |
JP5042839B2 true JP5042839B2 (ja) | 2012-10-03 |
Family
ID=37835875
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007534461A Expired - Fee Related JP5042839B2 (ja) | 2005-09-09 | 2006-09-07 | 腸疾患の予防及び/又は治療のための医薬 |
JP2010184584A Expired - Fee Related JP5172911B2 (ja) | 2005-09-09 | 2010-08-20 | 癒着の予防及び/又は治療のための医薬 |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010184584A Expired - Fee Related JP5172911B2 (ja) | 2005-09-09 | 2010-08-20 | 癒着の予防及び/又は治療のための医薬 |
Country Status (5)
Country | Link |
---|---|
US (3) | US20080255069A1 (ja) |
EP (2) | EP1930001A4 (ja) |
JP (2) | JP5042839B2 (ja) |
CN (2) | CN102058571B (ja) |
WO (1) | WO2007029760A1 (ja) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8198329B2 (en) * | 2004-03-10 | 2012-06-12 | Research Foundation Itsuu Laboratory | Memory consolidation promoting agent and method of use |
CN102058571B (zh) | 2005-09-09 | 2012-09-19 | 有限会社肯菲思 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)氨基甲酰基]苯甲酸在制备用于预防及/或治疗肠疾病的药物中的应用 |
JPWO2009101684A1 (ja) * | 2008-02-14 | 2011-06-02 | 有限会社ケムフィズ | 内臓癒着の予防及び/又は治療のための医薬 |
EP2781225B1 (en) * | 2011-11-18 | 2019-10-09 | Nitto Denko Corporation | Intestinal fibrosis treatment agent |
RU2015106915A (ru) * | 2012-08-01 | 2016-09-20 | Мерк Шарп И Доум Корп. | МОДУЛЯТОРЫ α7 НИКОТИНОВОГО АЦЕТИЛХОЛИНОВОГО РЕЦЕПТОРА И ИХ ПРИМЕНЕНИЕ |
EP2969031A4 (en) | 2013-03-15 | 2017-03-08 | Avisenna Cosmetics LLC | Topical compositions for reducing aging effects |
CN104162167A (zh) * | 2014-07-18 | 2014-11-26 | 山东大学 | 他米巴罗汀环糊精或环糊精衍生物包合物及其制备方法 |
DE102014011699B4 (de) * | 2014-08-07 | 2023-11-02 | Fresenius Medical Care Deutschland Gmbh | Vorrichtung zur Ermittlung eines optimalen Dialysatflusses für eine extrakorporale Blutbehandlung mit einer extrakorporalen Blutbehandlungsvorrichtung |
GEP20207149B (en) | 2016-03-22 | 2020-09-10 | Merck Sharp & Dohme | Allosteric modulators of nicotinic acetylcholine receptors |
US10811126B2 (en) * | 2016-12-14 | 2020-10-20 | Tracy Warren | System and methods for developing and using a microbiome-based action component for patient health |
US11978543B2 (en) | 2016-12-14 | 2024-05-07 | Astarte Medical Partners Inc. | System and methods for developing and using a microbiome-based action component |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH07101857A (ja) * | 1993-10-04 | 1995-04-18 | Kuraray Co Ltd | ビタミンa酸亜鉛塩を有効成分とする抗潰瘍剤 |
Family Cites Families (18)
Publication number | Priority date | Publication date | Assignee | Title |
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JPS6176440A (ja) | 1984-09-19 | 1986-04-18 | Koichi Shiyudo | 安息香酸誘導体 |
JPS6122047A (ja) | 1984-07-07 | 1986-01-30 | Koichi Shiyudo | 安息香酸誘導体 |
EP0170105B1 (en) * | 1984-07-07 | 1990-10-17 | Koichi Prof. Dr. Shudo | Benzoic acid derivatives |
US5601579A (en) * | 1994-12-29 | 1997-02-11 | Medex, Inc. | Method for the treatment of bowel adhesions |
US5534261A (en) * | 1995-01-17 | 1996-07-09 | University Of Southern California | Retinoid-based compositions and method for preventing adhesion formation using the same |
JP3865829B2 (ja) | 1995-09-21 | 2007-01-10 | 株式会社医薬分子設計研究所 | レチノイド作用増強性化合物 |
EP0906907B1 (en) * | 1995-09-21 | 2002-03-06 | Institute of Medicinal Molecular Design, Inc. | Compounds potentiating retinoid |
CA2295807A1 (en) * | 1997-07-29 | 1999-02-11 | Bristol-Myers Squibb Company | Use of selective rxr agonists to prevent surgical adhesions |
US5776915A (en) * | 1997-08-12 | 1998-07-07 | Clarion Pharmaceuticals Inc. | Phosphocholines of retinoids |
EP0908179A1 (en) * | 1997-08-23 | 1999-04-14 | Werner Bollag | Treatment of cell-mediated immune diseases |
CA2482147A1 (en) * | 2002-04-22 | 2003-10-30 | Research Foundation Itsuu Laboratory | Medicament for therapeutic treatment of vascular disease |
US20050205086A1 (en) * | 2002-10-25 | 2005-09-22 | Foamix Ltd. | Retinoid immunomodulating kit and composition and uses thereof |
WO2005087129A1 (en) | 2004-03-08 | 2005-09-22 | Dentsply International Inc. | Energy assisted delivery of dental materials from a cartridge |
US8198329B2 (en) * | 2004-03-10 | 2012-06-12 | Research Foundation Itsuu Laboratory | Memory consolidation promoting agent and method of use |
CN102058571B (zh) * | 2005-09-09 | 2012-09-19 | 有限会社肯菲思 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)氨基甲酰基]苯甲酸在制备用于预防及/或治疗肠疾病的药物中的应用 |
JP2008081427A (ja) * | 2006-09-27 | 2008-04-10 | R&R Inc | 分泌障害性疾患の予防及び/又は治療のための医薬 |
JP2008184396A (ja) * | 2007-01-29 | 2008-08-14 | St Marianna Univ School Of Medicine | 神経損傷に起因する身体機能障害の予防及び治療のための医薬 |
US7902260B2 (en) * | 2007-02-28 | 2011-03-08 | Kemphys Ltd. | Medicament for preventive and/or therapeutic treatment of lower urinary tract symptom |
-
2006
- 2006-09-07 CN CN2011100294139A patent/CN102058571B/zh not_active Expired - Fee Related
- 2006-09-07 EP EP06797596A patent/EP1930001A4/en not_active Withdrawn
- 2006-09-07 WO PCT/JP2006/317720 patent/WO2007029760A1/ja active Application Filing
- 2006-09-07 US US12/065,099 patent/US20080255069A1/en not_active Abandoned
- 2006-09-07 CN CN2006800329648A patent/CN101262861B/zh not_active Expired - Fee Related
- 2006-09-07 EP EP10176936A patent/EP2286807A3/en not_active Withdrawn
- 2006-09-07 JP JP2007534461A patent/JP5042839B2/ja not_active Expired - Fee Related
-
2009
- 2009-09-14 US US12/559,268 patent/US8168677B2/en not_active Expired - Fee Related
-
2010
- 2010-08-20 JP JP2010184584A patent/JP5172911B2/ja not_active Expired - Fee Related
- 2010-08-31 US US12/872,171 patent/US8071647B2/en not_active Expired - Fee Related
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH07101857A (ja) * | 1993-10-04 | 1995-04-18 | Kuraray Co Ltd | ビタミンa酸亜鉛塩を有効成分とする抗潰瘍剤 |
Also Published As
Publication number | Publication date |
---|---|
CN101262861B (zh) | 2011-04-06 |
EP2286807A2 (en) | 2011-02-23 |
JPWO2007029760A1 (ja) | 2009-03-19 |
JP2010265315A (ja) | 2010-11-25 |
US8168677B2 (en) | 2012-05-01 |
US20100004203A1 (en) | 2010-01-07 |
US20100324134A1 (en) | 2010-12-23 |
EP1930001A1 (en) | 2008-06-11 |
EP1930001A4 (en) | 2010-07-21 |
EP2286807A3 (en) | 2012-08-29 |
US8071647B2 (en) | 2011-12-06 |
CN102058571A (zh) | 2011-05-18 |
CN102058571B (zh) | 2012-09-19 |
WO2007029760A1 (ja) | 2007-03-15 |
CN101262861A (zh) | 2008-09-10 |
US20080255069A1 (en) | 2008-10-16 |
JP5172911B2 (ja) | 2013-03-27 |
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