JP2020500875A - 統合失調症または統合失調感情障害を処置するためのバルベナジンの使用 - Google Patents
統合失調症または統合失調感情障害を処置するためのバルベナジンの使用 Download PDFInfo
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- JP2020500875A JP2020500875A JP2019529533A JP2019529533A JP2020500875A JP 2020500875 A JP2020500875 A JP 2020500875A JP 2019529533 A JP2019529533 A JP 2019529533A JP 2019529533 A JP2019529533 A JP 2019529533A JP 2020500875 A JP2020500875 A JP 2020500875A
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- Prior art keywords
- pyrido
- hexahydro
- isobutyl
- dimethoxy
- isoquinolin
- 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.)
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
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- 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
- A61K9/20—Pills, tablets, discs, rods
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- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Description
バルベナジン、(S)−2−アミノ−3−メチル−酪酸(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−1,3,4,6,7,11b−ヘキサヒドロ−2H−ピリド[2,1−a]イソキノリン−2−イルエステル、ジヒドロテトラベナジンの(+)−α−異性体の精製プロドラッグも、小胞モノアミン輸送体2系(VMAT2)の阻害剤である。
本明細書において説明されている本開示の理解を容易にするため、多数の用語が下記に定義されている。
処置の方法ならびに医薬調製物および組成物
医薬組成物
経口投与
非経口投与
局所的投与
修飾放出
マトリックス制御放出デバイス
浸透圧制御放出デバイス
多微粒子制御放出デバイス
標的化送達
投与量
薬物動態特性
Claims (16)
- (S)−2−アミノ−3−メチル−酪酸(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−1,3,4,6,7,11b−ヘキサヒドロ−2H−ピリド[2,1−a]イソキノリン−2−イルエステル、もしくはその同位体変種、またはその薬学的に許容される塩もしくは多形体を投与することを含む、統合失調症または統合失調感情障害を処置する方法。
- (S)−2−アミノ−3−メチル−酪酸(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−1,3,4,6,7,11b−ヘキサヒドロ−2H−ピリド[2,1−a]イソキノリン−2−イルエステル、もしくはその同位体変種、またはその薬学的に許容される塩もしくは多形体を投与することを含む、統合失調症または統合失調感情障害と関連する行動問題を処置する方法。
- 前記(S)−2−アミノ−3−メチル−酪酸(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−1,3,4,6,7,11b−ヘキサヒドロ−2H−ピリド[2,1−a]イソキノリン−2−イルエステル、もしくはその同位体変種、またはその薬学的に許容される塩もしくは多形体が、(S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)、もしくはその同位体変種、またはその多形体である、請求項1または2に記載の方法。
- 陽性症状を処置する、請求項1から3のいずれかに記載の方法。
- 陰性症状を処置する、請求項1から3のいずれかに記載の方法。
- (S)−2−アミノ−3−メチル−酪酸(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−1,3,4,6,7,11b−ヘキサヒドロ−2H−ピリド[2,1−a]イソキノリン−2−イルエステル、もしくはその同位体変種、またはその薬学的に許容される塩もしくは多形体が、投与単位の形態である、請求項1から5のいずれかに記載の方法。
- 前記投与単位が、25mgから100mgの(S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)、もしくはその同位体変種、またはその多形体を含有する、請求項6に記載の方法。
- 前記投与単位が、40mgの(S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)、もしくはその同位体変種、またはその多形体を含有する、請求項7に記載の方法。
- 前記投与単位が、80mgの(S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)、もしくはその同位体変種、またはその多形体を含有する、請求項8に記載の方法。
- 前記投与単位が、錠剤またはカプセル剤である、請求項6から8のいずれかに記載の方法。
- 統合失調症または統合失調感情障害を処置することにおける使用のための、化合物(S)−2−アミノ−3−メチル−酪酸(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−1,3,4,6,7,11b−ヘキサヒドロ−2H−ピリド[2,1−a]イソキノリン−2−イルエステル、もしくはその同位体変種、またはその薬学的に許容される塩もしくは多形体。
- 前記化合物が、経口投与のために製剤化される、請求項11に記載の使用のための化合物。
- 前記化合物が、単一剤形として製剤化される、請求項11または12に記載の使用のための化合物。
- 前記剤形が、錠剤またはカプセル剤である、請求項13に記載の使用のための化合物。
- 前記剤形が、40mgの(S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)、もしくはその同位体変種、またはその多形体を含有する、請求項13または14に記載の使用のための化合物。
- 前記剤形が、80mgの(S)−(2R,3R,11bR)−3−イソブチル−9,10−ジメトキシ−2,3,4,6,7,11b−ヘキサヒドロ−1H−ピリド[2,1−a]イソキノリン−2−イル2−アミノ−3−メチルブタノエートジ(4−メチルベンゼンスルホネート)、もしくはその同位体変種、またはその多形体を含有する、請求項13または14に記載の使用のための化合物。
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TW202345829A (zh) | 2023-12-01 |
EP4400171A2 (en) | 2024-07-17 |
US20200078352A1 (en) | 2020-03-12 |
JP2023015405A (ja) | 2023-01-31 |
TW201827051A (zh) | 2018-08-01 |
EP3548027A1 (en) | 2019-10-09 |
WO2018102673A1 (en) | 2018-06-07 |
US20210113553A1 (en) | 2021-04-22 |
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