JP2007519657A - マレイン酸イボパミン、その製造方法、及びそれを含む医薬組成物 - Google Patents
マレイン酸イボパミン、その製造方法、及びそれを含む医薬組成物 Download PDFInfo
- Publication number
- JP2007519657A JP2007519657A JP2006550016A JP2006550016A JP2007519657A JP 2007519657 A JP2007519657 A JP 2007519657A JP 2006550016 A JP2006550016 A JP 2006550016A JP 2006550016 A JP2006550016 A JP 2006550016A JP 2007519657 A JP2007519657 A JP 2007519657A
- Authority
- JP
- Japan
- Prior art keywords
- ibopamine
- pharmaceutical composition
- maleate
- salt
- same
- 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.)
- Granted
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C219/26—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
- C07C219/28—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton having amino groups bound to acyclic carbon atoms of the carbon skeleton
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/08—Mydriatics or cycloplegics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Ophthalmology & Optometry (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Description
マレイン酸イボパミンの調製
工程a)
水(10ml)に塩酸イボパミン(4g)を溶解させた溶液に、炭酸ナトリウムの飽和溶液を、沈殿物が更に生じなくなるまで加えた。
マレイン酸(674mg;0.005mol)のアセトン(5ml)溶液を、不活性雰囲気下、加熱することなく、室温で、イボパミン塩基(1.78g;0.005mol)のアセトン(10ml)溶液に加えた。
眼の忍容性
二種の水溶液を用いた。
Claims (11)
- マレイン酸イボパミン塩(1:1)。
- 眼用の医薬組成物において、医薬として許容できる少なくとも一種の賦形剤と共に、マレイン酸イボパミン(1:1)を含むことを特徴とする医薬組成物。
- 軟膏あるいは点眼剤の形態にあること特徴とする、請求項2に記載の医薬組成物。
- イボパミンの量が0.01重量%から6重量%の間であることを特徴とする、請求項2又は3に記載の医薬組成物。
- イボパミンの量が0.1重量%から5重量%の間であることを特徴とする、請求項2又は3に記載の医薬組成物。
- マレイン酸イボパミン塩(1:1)の製造方法であって、
適切な有機溶媒に溶解させたマレイン酸を、適切な有機溶媒に同じく溶解させたイボパミン塩基に、1:1のモル比で添加することを含むことを特徴とするマレイン酸イボパミン塩(1:1)の製造方法。 - 上述の添加を不活性ガス雰囲気下で行うことを特徴とする、請求項6に記載の方法。
- 上述の添加を室温で行うことを特徴とする、請求項6又は7に記載の方法。
- 前記生成した塩を沈殿及び濾過により分離することを特徴とする、請求項6〜8のいずれか一項に記載の方法。
- 上述の有機溶媒がアセトンであることを特徴とする、請求項6〜9のいずれか一項に記載の方法。
- エチルエーテルを加えることにより前記アセトン溶液から前記塩を沈殿させることを特徴とする、請求項10に記載の方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IT000146A ITMI20040146A1 (it) | 2004-01-30 | 2004-01-30 | Ibopamina maleato metodo per prepararlo e composizioni farmaceutiche che lo comprendono |
PCT/EP2005/000445 WO2005075409A1 (en) | 2004-01-30 | 2005-01-13 | Ibopamine maleate, method for preparing it and pharmaceutical compositions containing it |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007519657A true JP2007519657A (ja) | 2007-07-19 |
JP4646921B2 JP4646921B2 (ja) | 2011-03-09 |
Family
ID=34835573
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2006550016A Expired - Fee Related JP4646921B2 (ja) | 2004-01-30 | 2005-01-13 | マレイン酸イボパミンを含む医薬組成物及びその製造方法 |
Country Status (20)
Country | Link |
---|---|
US (1) | US7667069B2 (ja) |
EP (1) | EP1708988B1 (ja) |
JP (1) | JP4646921B2 (ja) |
KR (1) | KR101109566B1 (ja) |
CN (1) | CN100564351C (ja) |
AT (1) | ATE502004T1 (ja) |
AU (1) | AU2005211453B2 (ja) |
BR (1) | BRPI0507153A (ja) |
CA (1) | CA2551411C (ja) |
DE (1) | DE602005026909D1 (ja) |
DK (1) | DK1708988T3 (ja) |
EA (1) | EA009212B1 (ja) |
ES (1) | ES2361520T3 (ja) |
HK (1) | HK1093721A1 (ja) |
IL (1) | IL176431A (ja) |
IT (1) | ITMI20040146A1 (ja) |
PL (1) | PL1708988T3 (ja) |
PT (1) | PT1708988E (ja) |
SI (1) | SI1708988T1 (ja) |
WO (1) | WO2005075409A1 (ja) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PE20091156A1 (es) * | 2007-12-17 | 2009-09-03 | Astrazeneca Ab | Sales de (3-{[[3-(6-amino-2-butoxi-8-oxo-7,8-dihidro-9h-purin-9-il)propil](3-morfolin-4-ilpropil)amino]metil}fenil)acetato de metilo |
US20240065999A1 (en) * | 2020-11-09 | 2024-02-29 | The Board Of Trustees Of The Leland Stanford Junior University | Ophthalmic Formulation Containing a Dopaminergic Prodrug that may be Combined with One or More Agents |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5321130A (en) * | 1976-08-05 | 1978-02-27 | Simes | Novel epinine ester*process for preparation thereof and pharmaceutical composition |
JPS63502270A (ja) * | 1984-12-27 | 1988-09-01 | ザンボン グループ ソシエタ ペル アチオニ | 散瞳作用を有する眼科用医薬組成物 |
JPH04501563A (ja) * | 1988-11-09 | 1992-03-19 | アツィエンデ キミケ リウニテ アンジェリーニ フランセスコ ア チ エッレ ア エッフェ ソシエタ ペル アチオニ | 水溶性イボパミン酸付加塩を含有する眼薬 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2400038A (en) * | 1944-09-07 | 1946-05-07 | Burroughs Wellcome Co | Esters of secondary phenolic amines |
IT1247508B (it) * | 1991-04-19 | 1994-12-17 | Zambon Spa | Composizioni farmaceutiche contenenti l'estere 4-(2 metilamminoetil)- 1,2- fenilenicodell`acido 2-metilpropanoico per il trattamento della neurootticopatia glaucomatosa |
-
2004
- 2004-01-30 IT IT000146A patent/ITMI20040146A1/it unknown
-
2005
- 2005-01-13 PT PT05706914T patent/PT1708988E/pt unknown
- 2005-01-13 EA EA200601117A patent/EA009212B1/ru not_active IP Right Cessation
- 2005-01-13 BR BRPI0507153-4A patent/BRPI0507153A/pt not_active IP Right Cessation
- 2005-01-13 KR KR1020067015322A patent/KR101109566B1/ko active IP Right Grant
- 2005-01-13 PL PL05706914T patent/PL1708988T3/pl unknown
- 2005-01-13 CA CA2551411A patent/CA2551411C/en not_active Expired - Fee Related
- 2005-01-13 JP JP2006550016A patent/JP4646921B2/ja not_active Expired - Fee Related
- 2005-01-13 CN CNB2005800030862A patent/CN100564351C/zh not_active Expired - Fee Related
- 2005-01-13 AT AT05706914T patent/ATE502004T1/de active
- 2005-01-13 WO PCT/EP2005/000445 patent/WO2005075409A1/en active Application Filing
- 2005-01-13 DE DE602005026909T patent/DE602005026909D1/de active Active
- 2005-01-13 EP EP05706914A patent/EP1708988B1/en active Active
- 2005-01-13 AU AU2005211453A patent/AU2005211453B2/en not_active Ceased
- 2005-01-13 SI SI200531293T patent/SI1708988T1/sl unknown
- 2005-01-13 ES ES05706914T patent/ES2361520T3/es active Active
- 2005-01-13 DK DK05706914.8T patent/DK1708988T3/da active
- 2005-01-13 US US10/586,865 patent/US7667069B2/en not_active Expired - Fee Related
-
2006
- 2006-06-20 IL IL176431A patent/IL176431A/en active IP Right Grant
- 2006-12-27 HK HK06114155.6A patent/HK1093721A1/xx not_active IP Right Cessation
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5321130A (en) * | 1976-08-05 | 1978-02-27 | Simes | Novel epinine ester*process for preparation thereof and pharmaceutical composition |
JPS63502270A (ja) * | 1984-12-27 | 1988-09-01 | ザンボン グループ ソシエタ ペル アチオニ | 散瞳作用を有する眼科用医薬組成物 |
JPH04501563A (ja) * | 1988-11-09 | 1992-03-19 | アツィエンデ キミケ リウニテ アンジェリーニ フランセスコ ア チ エッレ ア エッフェ ソシエタ ペル アチオニ | 水溶性イボパミン酸付加塩を含有する眼薬 |
Also Published As
Publication number | Publication date |
---|---|
WO2005075409A1 (en) | 2005-08-18 |
AU2005211453A1 (en) | 2005-08-18 |
BRPI0507153A (pt) | 2007-07-31 |
AU2005211453B2 (en) | 2011-06-30 |
DE602005026909D1 (de) | 2011-04-28 |
EA200601117A1 (ru) | 2006-10-27 |
IL176431A (en) | 2010-11-30 |
IL176431A0 (en) | 2006-10-05 |
ATE502004T1 (de) | 2011-04-15 |
CA2551411C (en) | 2012-04-24 |
CN100564351C (zh) | 2009-12-02 |
CN1910139A (zh) | 2007-02-07 |
DK1708988T3 (da) | 2011-06-27 |
EP1708988A1 (en) | 2006-10-11 |
ES2361520T3 (es) | 2011-06-17 |
US20080242724A1 (en) | 2008-10-02 |
EP1708988B1 (en) | 2011-03-16 |
KR101109566B1 (ko) | 2012-01-31 |
US7667069B2 (en) | 2010-02-23 |
HK1093721A1 (en) | 2007-03-09 |
PL1708988T3 (pl) | 2011-08-31 |
CA2551411A1 (en) | 2005-08-18 |
KR20060127940A (ko) | 2006-12-13 |
SI1708988T1 (sl) | 2011-06-30 |
EA009212B1 (ru) | 2007-12-28 |
PT1708988E (pt) | 2011-05-31 |
JP4646921B2 (ja) | 2011-03-09 |
ITMI20040146A1 (it) | 2004-04-30 |
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