JP5478495B2 - アドレナリン作動性α−1受容体アンタゴニストの新規な治療的使用 - Google Patents
アドレナリン作動性α−1受容体アンタゴニストの新規な治療的使用 Download PDFInfo
- Publication number
- JP5478495B2 JP5478495B2 JP2010526392A JP2010526392A JP5478495B2 JP 5478495 B2 JP5478495 B2 JP 5478495B2 JP 2010526392 A JP2010526392 A JP 2010526392A JP 2010526392 A JP2010526392 A JP 2010526392A JP 5478495 B2 JP5478495 B2 JP 5478495B2
- Authority
- JP
- Japan
- Prior art keywords
- bladder
- alfuzosin
- adrenergic
- receptor antagonists
- inflammatory
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
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Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61P13/06—Anti-spasmodics
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Description
膀胱炎誘導のために、雄Sprague−DawleyラットおよびSwissマウスにCYP(150mg/kg、i.p.)またはこのビヒクル(0.9%NaCl)を投与した。48時間後に、膀胱を取り出し、運動応答測定のために器官浴に入れた。CYP投与から90分後に、悶え挙動および血漿中蛋白質血管外遊出を調べた。
ラット膀胱の切片を末端麻酔動物から採取し、器官浴中に設置し、平衡期間の後、アトロピン(1μM)の不存在下および存在下で、電場刺激(EFS、5Hz、1ms幅、10V)に対するeNANC収縮応答を調べる(Rigoni et al.,2003,Br J Pharmacol,138,977−85)。これらの実験条件におけるEFSによって生じた収縮は、一次感覚ニューロンの末端から放出されたSPおよびNKAによって全部が媒介されている。EFSに対するeNANC応答は60分の間隔で再現可能であった。EFSに対するeNANC応答についてのアルフゾシンまたはこのビヒクルの効果を平行実験で調べた。各実験の最初または最後において、組織をカルバコール(1μM)で検証した。アルフゾシンの効果を、シクロホスファミドで処理したラットから得られた膀胱片においても調べた。
シクロホスファミドの腹腔内投与(150mg/kg、48時間前)は、膀胱の能力および増大した排尿の頻度を減少させることが知られている(Maggi et al.,1992,J Auton Nerv Syst,38,201−8)。シクロホスファミドのこれらの効果は、成体としてのカプサイシンで予備処理されたラットにおいてなくなった(Maggi et al.,1992,J Auton Nerv Syst,38,201−8)。このようにして、シクロホスファミドに対する炎症性応答は、神経原性炎症メカニズムによって媒介される。
エバンスブルー色素を用いて、血漿血管外遊出を測定した。頚静脈での色素の注射(5秒間にわたる30mg/kg i.v.)直後に炎症性刺激物を与えた。エバンスブルーの注射後に必要に応じて、胸を10分間、または異なる時間間隔で開き、動物にリン酸緩衝液を3分間灌流した。膀胱、尿道および前立腺を取り出し、ブロットし、秤量した。次いで、組織を3mlのホルムアミド中に50℃にて18時間入れて、血管外遊出したエバンスブルー色素を抽出した。気管および気管支から血管外遊出したエバンスブルーの量を、分光光度計を用いて測定し、ng/mg湿潤重量として表した。
代表的な例として、錠剤の形態の本発明の化合物の単位投与形態は以下の成分を含むことができる。
アルフゾシン塩酸塩 5mg
ラクトース 122mg
マイクロクリスタリンセルロース 36.0mg
ナトリウムカルボキシメチル澱粉 7.0mg
ポリビドン 9mg
ステアリン酸マグネシウム 1.0mg
Claims (5)
- 炎症性膀胱の治療および/または予防用の医薬の調製のためのアルフゾシンまたはこの医薬的に許容される塩の使用。
- 前記炎症性膀胱が、間質性膀胱炎に由来するか、またはこれに関連する、請求項1に記載の使用。
- 該アルフゾシンが、アルフゾシン塩酸塩である、請求項1または2に記載の使用。
- 男性患者での治療および/または予防のための、請求項1から3のいずれか一項に記載の使用。
- 有効成分として、アルフゾシンまたはこの医薬的に許容される塩を含む、炎症性膀胱の治療および/もしくは予防のための医薬組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US97532407P | 2007-09-26 | 2007-09-26 | |
EP07291148A EP2042179A1 (en) | 2007-09-26 | 2007-09-26 | Novel therapeutic uses of adrenergic alpha-1 receptor antagonists |
EP07291148.0 | 2007-09-26 | ||
US60/975,324 | 2007-09-26 | ||
PCT/IB2008/003126 WO2009040671A1 (en) | 2007-09-26 | 2008-09-24 | Novel therapeutic uses of adrenergic alpha-1 receptor antagonists |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2010540511A JP2010540511A (ja) | 2010-12-24 |
JP2010540511A5 JP2010540511A5 (ja) | 2011-09-15 |
JP5478495B2 true JP5478495B2 (ja) | 2014-04-23 |
Family
ID=38754714
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2010526392A Expired - Fee Related JP5478495B2 (ja) | 2007-09-26 | 2008-09-24 | アドレナリン作動性α−1受容体アンタゴニストの新規な治療的使用 |
Country Status (15)
Country | Link |
---|---|
US (1) | US8492396B2 (ja) |
EP (2) | EP2042179A1 (ja) |
JP (1) | JP5478495B2 (ja) |
AR (1) | AR068825A1 (ja) |
AT (1) | ATE524185T1 (ja) |
CY (1) | CY1112203T1 (ja) |
DK (1) | DK2203170T3 (ja) |
ES (1) | ES2373354T3 (ja) |
HR (1) | HRP20110919T1 (ja) |
ME (1) | ME01259B (ja) |
PL (1) | PL2203170T3 (ja) |
PT (1) | PT2203170E (ja) |
RS (1) | RS52069B (ja) |
SI (1) | SI2203170T1 (ja) |
WO (1) | WO2009040671A1 (ja) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN110933933B (zh) * | 2018-07-18 | 2022-12-27 | 温州医科大学 | 一种治疗近视的方法及制备药物的应用 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FR2582513B1 (fr) * | 1985-05-28 | 1988-08-05 | Synthelabo | Compositions pharmaceutiques contenant de l'alfuzosine |
US20020143007A1 (en) * | 1996-02-02 | 2002-10-03 | Garvey David S. | Nitrosated and nitrosylated alpha-adrenergic receptor antagonists, compositions and methods of use |
KR100541784B1 (ko) * | 1997-07-10 | 2006-01-10 | 테라코스, 인크. | 염증성 장 및 방광 질환을 치료하기 위한 치료제를 제조하는 방법 |
BR0206644A (pt) * | 2001-01-26 | 2004-02-25 | Schering Corp | Combinações de inibidor(es) de absorção de esteróis com agente(s) cardiovascular(es) para o tratamento de condições vasculares |
EP1364659B1 (en) * | 2001-02-08 | 2009-11-11 | Ono Pharmaceutical Co., Ltd. | Remedies for urinary diseases comprising lpa receptor controlling agents |
WO2002069906A2 (en) * | 2001-03-06 | 2002-09-12 | Cellegy Pharmaceuticals, Inc. | Compounds and methods for the treatment of urogenital disorders |
US20030060513A1 (en) * | 2001-09-27 | 2003-03-27 | Arneric Stephen P. | Pharmaceutical composition |
US20050261344A1 (en) * | 2002-08-14 | 2005-11-24 | Jones Charles R | Treatment of lower urinary tract symptoms associated with overactive bladder in men and women |
CA2530312A1 (en) * | 2003-07-02 | 2005-01-20 | F. Hoffmann-La Roche Ag | Arylamine-substituted quinazolinone compounds |
WO2007047282A1 (en) * | 2005-10-12 | 2007-04-26 | Lilly Icos Llc | Treatment of benign prostatic hypertrophy and lower urinary tract symptoms |
-
2007
- 2007-09-26 EP EP07291148A patent/EP2042179A1/en not_active Withdrawn
-
2008
- 2008-09-24 JP JP2010526392A patent/JP5478495B2/ja not_active Expired - Fee Related
- 2008-09-24 SI SI200830471T patent/SI2203170T1/sl unknown
- 2008-09-24 DK DK08833688.8T patent/DK2203170T3/da active
- 2008-09-24 PL PL08833688T patent/PL2203170T3/pl unknown
- 2008-09-24 ES ES08833688T patent/ES2373354T3/es active Active
- 2008-09-24 RS RS20110553A patent/RS52069B/en unknown
- 2008-09-24 EP EP08833688A patent/EP2203170B1/en active Active
- 2008-09-24 AR ARP080104131A patent/AR068825A1/es unknown
- 2008-09-24 ME MEP-2011-204A patent/ME01259B/me unknown
- 2008-09-24 PT PT08833688T patent/PT2203170E/pt unknown
- 2008-09-24 AT AT08833688T patent/ATE524185T1/de active
- 2008-09-24 WO PCT/IB2008/003126 patent/WO2009040671A1/en active Application Filing
-
2010
- 2010-03-24 US US12/730,559 patent/US8492396B2/en not_active Expired - Fee Related
-
2011
- 2011-12-06 HR HR20110919T patent/HRP20110919T1/hr unknown
- 2011-12-14 CY CY20111101243T patent/CY1112203T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
CY1112203T1 (el) | 2015-12-09 |
EP2203170B1 (en) | 2011-09-14 |
EP2203170A1 (en) | 2010-07-07 |
JP2010540511A (ja) | 2010-12-24 |
US8492396B2 (en) | 2013-07-23 |
WO2009040671A4 (en) | 2009-05-28 |
US20110009436A1 (en) | 2011-01-13 |
PL2203170T3 (pl) | 2012-02-29 |
ES2373354T3 (es) | 2012-02-02 |
HRP20110919T1 (hr) | 2012-01-31 |
DK2203170T3 (da) | 2012-01-16 |
PT2203170E (pt) | 2011-12-27 |
WO2009040671A1 (en) | 2009-04-02 |
SI2203170T1 (sl) | 2012-01-31 |
AR068825A1 (es) | 2009-12-09 |
RS52069B (en) | 2012-06-30 |
ATE524185T1 (de) | 2011-09-15 |
EP2042179A1 (en) | 2009-04-01 |
ME01259B (me) | 2013-06-20 |
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