JP2008546725A - 1−(3−クロロフェニル)−3−アルキルピペラジンを含む食欲障害治療用医薬組成物 - Google Patents
1−(3−クロロフェニル)−3−アルキルピペラジンを含む食欲障害治療用医薬組成物 Download PDFInfo
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Abstract
Description
で表され、トラゾドンのアルキル誘導体を製造するための中間体として1−(3−クロロフェニル)−3−アルキルピペラジンが記載されている。
で表される1−(3−クロロフェニル)−3−アルキルピペラジン及びその医薬として許容可能な有機酸又は無機酸の添加塩の医薬としての使用方法に関する。
で表される1−(3−クロロフェニル)−3−アルキルピペラジン又はその医薬として許容可能な有機酸もしくは無機酸の添加塩を治療上有効な量と、少なくとも1種の医薬として許容可能な賦形剤と含む医薬組成物に関する。
1.製造
本発明の化合物は当業者に既知の方法によって製造することができる。
体重が150〜250gになる雄のCDラットを用いた。
体重が300〜350gになる雄のCDラットを用いた。
4.1 錠剤
有効成分として本発明の化合物を含有する錠剤は、以下の組成を有する。
有効成分 50mg
ラクトース一水和物 161mg
第二リン酸カルシウム二水和物 161mg
微結晶性セルロース 95mg
トウモロコシデンプン 30mg
ナトリウム・カルボキシメチルアミド 24mg
ポビドン 11mg
ステアリン酸マグネシウム 3mg
バイアルには、有効成分として本発明の化合物を含有する5mlの注射溶液が含まれる。
前記溶液は以下の組成を有する。
有効成分 25mg
ソルビトール 等張溶液にするのに充分な量(q.s.f. isoosmotic solutions)
注射用滅菌水 5mlにするのに充分な量(q.s.f. 5ml)
薬包には有効成分として本発明の化合物を含む5.23gの水分散性顆粒が含まれる。前記顆粒は以下の組成を有する。
有効成分 50mg
マルチトール 1300mg
マンニトール 2700mg
スクロース 1000mg
クエン酸 15mg
アスパルテーム 15mg
人工香味料 150mg
Claims (18)
- 前記医薬としての使用方法が食欲障害の治療を含むことを特徴とする請求項1記載の使用方法。
- 前記食欲障害が、食欲過剰、過食症及び肥満からなる群より選択されることを特徴とする請求項2記載の使用方法。
- Rがメチル又はエチルであることを特徴とする請求項1〜3項のいずれか1項に記載の使用方法。
- Rがメチルであることを特徴とする請求項1〜3項のいずれか1項に記載の使用方法。
- 式(I)の化合物が(S)立体配置のエナンチオマーであることを特徴とする請求項1〜5項のいずれか1項に記載の使用方法。
- 前記有機酸がマレイン酸、メタンスルホン酸、パラトルエンスルホン酸、コハク酸及びクエン酸からなる群より選択されることを特徴とする請求項1〜6項のいずれか1項に記載の使用方法。
- 前記無機酸が、塩酸、臭化水素酸、リン酸及び硫酸からなる群より選択されることを特徴とする請求項1〜6項のいずれか1項に記載の使用方法。
- 前記酸が塩酸であることを特徴とする請求項1〜6項のいずれか1項に記載の使用方法。
- 前記酸が、L(+)乳酸及びL(+)酒石酸からなる群より選択されることを特徴とする請求項6記載の使用方法。
- Rがメチル又はエチルであることを特徴とする請求項11記載の医薬組成物。
- Rがメチルであることを特徴とする請求項11記載の医薬組成物。
- 式(I)の化合物が(S)立体配置のエナンチオマーであることを特徴とする請求項11〜13項のいずれか1項に記載の医薬組成物。
- 前記有機酸がマレイン酸、メタンスルホン酸、パラトルエンスルホン酸、コハク酸及びクエン酸からなる群より選択されることを特徴とする請求項11〜14項のいずれか1項に記載の医薬組成物。
- 前記無機酸が、塩酸、臭化水素酸、リン酸及び硫酸からなる群より選択されることを特徴とする請求項11〜14項のいずれか1項に記載の医薬組成物。
- 前記酸が塩酸であることを特徴とする請求項11〜14項のいずれか1項に記載の医薬組成物。
- 前記酸が、L(+)乳酸及びL(+)酒石酸からなる群より選択されることを特徴とする請求項11〜14項のいずれか1項に記載の医薬組成物。
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ITMI2005A001193 | 2005-06-24 | ||
IT001193A ITMI20051193A1 (it) | 2005-06-24 | 2005-06-24 | Uso farmaceutico di una 1-3-clorofenil-3-alchilpiperazina |
PCT/EP2006/005390 WO2006136284A1 (en) | 2005-06-24 | 2006-06-02 | Pharmaceutical composition comprising a 1-(3-chlorophenyl)-3-alkylpiperazine for treating apetite disorder |
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JP2008546725A true JP2008546725A (ja) | 2008-12-25 |
JP5142991B2 JP5142991B2 (ja) | 2013-02-13 |
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WO (1) | WO2006136284A1 (ja) |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
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US3253989A (en) * | 1963-02-11 | 1966-05-31 | American Cyanamid Co | Process for producing anorexia |
JPH07503000A (ja) * | 1992-01-17 | 1995-03-30 | アンジェリーニ・リチェルケ・ソシエタ・ペル・アチオニ・ソシエタ・コンソルティレ | Cns活性を示すトラゾドンのアルキル誘導体 |
JP2003518096A (ja) * | 1999-12-22 | 2003-06-03 | アー カールッスン リサーチ アーベー | ドーパミン神経伝達の新規のモジュレーター |
WO2005016902A1 (en) * | 2003-06-20 | 2005-02-24 | Arena Pharmaceuticals, Inc. | N-phenyl-piperazine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3637705A (en) * | 1968-10-01 | 1972-01-25 | Abbott Lab | N-3 4-dihalo phenyl piperazines |
FR2201084B1 (ja) * | 1972-09-29 | 1975-10-31 | Bouchara Emile |
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2005
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2006
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- 2006-06-02 AU AU2006261296A patent/AU2006261296B9/en not_active Ceased
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Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3253989A (en) * | 1963-02-11 | 1966-05-31 | American Cyanamid Co | Process for producing anorexia |
JPH07503000A (ja) * | 1992-01-17 | 1995-03-30 | アンジェリーニ・リチェルケ・ソシエタ・ペル・アチオニ・ソシエタ・コンソルティレ | Cns活性を示すトラゾドンのアルキル誘導体 |
JP2003518096A (ja) * | 1999-12-22 | 2003-06-03 | アー カールッスン リサーチ アーベー | ドーパミン神経伝達の新規のモジュレーター |
WO2005016902A1 (en) * | 2003-06-20 | 2005-02-24 | Arena Pharmaceuticals, Inc. | N-phenyl-piperazine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
Non-Patent Citations (1)
Title |
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JPN6012022304; Giannangeli M et al: J Med Chem Vol.42, 1999, p.336-345 * |
Also Published As
Publication number | Publication date |
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EP1893208A1 (en) | 2008-03-05 |
US7879836B2 (en) | 2011-02-01 |
HK1111080A1 (en) | 2008-08-01 |
ATE431146T1 (de) | 2009-05-15 |
PL1893208T3 (pl) | 2009-10-30 |
AR054491A1 (es) | 2007-06-27 |
ES2325744T3 (es) | 2009-09-15 |
ITMI20051193A1 (it) | 2006-12-25 |
CN101171011B (zh) | 2011-04-13 |
JP5142991B2 (ja) | 2013-02-13 |
BRPI0611719A2 (pt) | 2012-07-31 |
IL186334A0 (en) | 2008-08-07 |
EA200800125A1 (ru) | 2008-04-28 |
AU2006261296A1 (en) | 2006-12-28 |
CA2604584A1 (en) | 2006-12-28 |
EP1893208B1 (en) | 2009-05-13 |
EA012443B1 (ru) | 2009-10-30 |
DK1893208T3 (da) | 2009-08-31 |
DE602006006827D1 (de) | 2009-06-25 |
IL186334A (en) | 2011-02-28 |
US20090054461A1 (en) | 2009-02-26 |
UA89236C2 (ru) | 2010-01-11 |
GEP20094787B (en) | 2009-09-25 |
AU2006261296B2 (en) | 2010-12-16 |
PT1893208E (pt) | 2009-06-26 |
MX2007014396A (es) | 2008-02-12 |
WO2006136284A1 (en) | 2006-12-28 |
KR20080026115A (ko) | 2008-03-24 |
CA2604584C (en) | 2013-07-16 |
KR101324689B1 (ko) | 2013-11-04 |
SI1893208T1 (sl) | 2009-10-31 |
CN101171011A (zh) | 2008-04-30 |
AU2006261296B9 (en) | 2011-01-20 |
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