RU98102116A - (1S, 2S) -1- (4-HYDROXYPHENYL) -2- (4-HYDROXY-4-Phenylpiperidin-1-IL) -1-PROPANO LMETANSULPHONATE TRIHYDRATE - Google Patents

(1S, 2S) -1- (4-HYDROXYPHENYL) -2- (4-HYDROXY-4-Phenylpiperidin-1-IL) -1-PROPANO LMETANSULPHONATE TRIHYDRATE

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Publication number
RU98102116A
RU98102116A RU98102116/04A RU98102116A RU98102116A RU 98102116 A RU98102116 A RU 98102116A RU 98102116/04 A RU98102116/04 A RU 98102116/04A RU 98102116 A RU98102116 A RU 98102116A RU 98102116 A RU98102116 A RU 98102116A
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RU
Russia
Prior art keywords
disease
dopamine
agonists
mammal
effective amount
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RU98102116/04A
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Russian (ru)
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RU2140910C1 (en
Inventor
М.Андино Марта
Г.Синэй Терри
Ф.Физ Юджин
Original Assignee
Пфайзер Инк.
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Application filed by Пфайзер Инк. filed Critical Пфайзер Инк.
Priority claimed from PCT/IB1996/000592 external-priority patent/WO1997007098A1/en
Application granted granted Critical
Publication of RU98102116A publication Critical patent/RU98102116A/en
Publication of RU2140910C1 publication Critical patent/RU2140910C1/en

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Claims (12)

1. Тригидрат метансульфоната (1S,2S)-1-(4-гидроксифенил)-2-(4-гидрокси-4-фенилпиперидин-1-ил)-1-пропанола.1. Methanesulfonate trihydrate (1S, 2S) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4-phenylpiperidin-1-yl) -1-propanol. 2. Фармацевтическая композиция для лечения заболевания, выбранного из группы, включающей дегенеративные заболевания ЦНС, такие как припадок, болезнь Альцгеймера, болезнь Паркинсона и болезнь Хантингтона, эпилепсию, состояние страха, церебральную ишемию, мышечные спазмы, слабоумие, вызванное множественными инфарктами, травматическое поражение головного мозга, боль, слабоумие, вызванное СПИДом, гипогликемию, мигрень, боковой амиотрофический склероз, зависимость от лекарств и алкоголя, синдромы отмены лекарств и алкоголя, психотические состояния и недержание мочи у млекопитающих, в том числе у человека, содержащая тригидрат мезилатной соли по п.1 в эффективном количестве, и фармацевтически приемлемый носитель. 2. A pharmaceutical composition for treating a disease selected from the group consisting of degenerative diseases of the central nervous system, such as a seizure, Alzheimer's disease, Parkinson's disease and Huntington's disease, epilepsy, a state of fear, cerebral ischemia, muscle cramps, dementia caused by multiple heart attacks, traumatic head injury brain, pain, dementia caused by AIDS, hypoglycemia, migraine, amyotrophic lateral sclerosis, drug and alcohol addiction, drug and alcohol withdrawal syndromes, psychotic standing and urinary incontinence in a mammal, including a human, comprising the trihydrate mesylate salt according to claim 1 in an effective amount and a pharmaceutically acceptable carrier. 3. Фармацевтическая композиция по п.2, отличающаяся тем, что эффективным количеством является количество, эффективное для антагонистического взаимодействия с NMDA рецепторами. 3. The pharmaceutical composition according to claim 2, characterized in that the effective amount is an amount effective for antagonistic interaction with NMDA receptors. 4. Фармацевтическая композиция по п.2, отличающаяся тем, что эффективным количеством является количество, эффективное для лечения каждого заболевания. 4. The pharmaceutical composition according to claim 2, characterized in that the effective amount is an amount effective to treat each disease. 5. Способ лечения заболевания, выбранного из группы, включающей дегенеративные заболевания ЦНС, такие как припадок, болезнь Альцгеймера, болезнь Паркинсона и болезнь Хантингтона, эпилепсию, состояние страха, церебральную ишемию, мышечные спазмы, слабоумие, вызванное множественными инфарктами, травматическое поражение головного мозга, боль, слабоумие, вызванное СПИДом, гипогликемию, мигрень, боковой амиотрофический склероз, зависимость от лекарств и алкоголя, синдромы отмены лекарств и алкоголя, психотические состояния и недержание мочи у млекопитающих, в том числе у человека, заключающийся во введении млекопитающему тригидрата мезилатной соли по п.1 в эффективном количестве. 5. A method of treating a disease selected from the group comprising degenerative diseases of the central nervous system, such as a seizure, Alzheimer's disease, Parkinson's disease and Huntington's disease, epilepsy, a state of fear, cerebral ischemia, muscle cramps, dementia caused by multiple heart attacks, traumatic brain damage, pain, AIDS-related dementia, hypoglycemia, migraine, amyotrophic lateral sclerosis, drug and alcohol addiction, drug and alcohol withdrawal syndromes, psychotic conditions and urinary incontinence in mammals, including humans, comprising administering to the mammal a mesylate salt trihydrate according to claim 1 in an effective amount. 6. Способ по п.5, отличающийся тем, что эффективным количеством является количество, оказывающее антагонистическое действие на NMDA рецепторы. 6. The method according to claim 5, characterized in that the effective amount is the amount that has an antagonistic effect on NMDA receptors. 7. Способ по п.5, отличающийся тем, что эффективным количеством является количество, эффективное для лечения каждого заболевания. 7. The method according to claim 5, characterized in that the effective amount is an amount effective to treat each disease. 8. Способ лечения болезни Паркинсона у млекопитающего, включающий введение указанному млекопитающему эффективного для лечения болезни Паркинсона количества синергического сочетания тригидрата мезилатной соли по п.1 (1S, 2S)-1-(4-гидроксифенил)-2-(4-гидрокси-4-фенил-пиперидин-1-ил)-1-пропанола и средства, способного восстанавливать баланс возбудительной обратной связи из вентрального латерального ядра таламуса в кору головного мозга. 8. A method of treating Parkinson’s disease in a mammal, comprising administering to said mammal a quantity of synergistic combination of mesylate salt trihydrate effective for treating Parkinson’s disease according to claim 1 (1S, 2S) -1- (4-hydroxyphenyl) -2- (4-hydroxy-4 -phenyl-piperidin-1-yl) -1-propanol and an agent capable of restoring the balance of excitatory feedback from the ventral lateral nucleus of the thalamus to the cerebral cortex. 9. Способ лечения болезни Паркинсона у млекопитающего, включающий лечение указанного млекопитающего эффективным для лечения болезни Паркинсона количеством синергического сочетания тригидрата мезилатной соли по п.1 и средства, повышающего возбудительную обратную связь, которое выбрано из группы, включающей агонисты допамина, агонисты допамина D1, агонисты допамина D2, агонисты взаимодействия допамин\ адренорецептор, агонисты взаимодействия допамин\ 5-НТ ингибитор поглощения\5-НТ-1А, агонисты взаимодействия допамин\ опиат, агонисты адренорецепторов, агонисты взаимодействия a2-адренорецептор\ допамин D2, ингибиторы поглощения допамина, ингибиторы моноаминоксидазы, ингибиторы моноаминоксидазы-В, ингибиторы СОМТ, ингибиторы трансфераз и леводопы. 9. A method of treating Parkinson’s disease in a mammal, comprising treating said mammal with an effective amount of a synergistic combination of mesylate salt trihydrate for treating Parkinson’s disease according to claim 1 and an excitatory feedback enhancer selected from the group consisting of dopamine agonists, dopamine D1 agonists, agonists dopamine D2, dopamine \ adrenoreceptor interaction agonists, dopamine \ 5-HT interaction agonists, 5-HT-1A absorption inhibitor, dopamine \ opiate interaction agonists, adrenor agonists receptors, a2-adrenoreceptor \ dopamine D2 interaction agonists, dopamine uptake inhibitors, monoamine oxidase inhibitors, monoamine oxidase-B inhibitors, COMT inhibitors, transferase and levodopa inhibitors. 10. Способ по п. 9, где указанный реагент, повышающий возбудительную обратную связь, представляет собой леводопу. 10. The method according to p. 9, where the specified reagent that increases the excitatory feedback, is a levodopa. 11. Способ по любому из пп.5-7, где заболевание, которое подлежит лечению, представляет собой болезнь Паркинсона. 11. The method according to any one of claims 5-7, wherein the disease to be treated is Parkinson's disease. 12. Способ по любому из пп.5-7, где заболевание, которое подлежит лечению, представляет собой травматическое поражение головного мозга или церебральную ишемию. 12. The method according to any one of claims 5 to 7, wherein the disease to be treated is a traumatic brain lesion or cerebral ischemia.
RU98102116A 1995-08-11 1996-06-20 (1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidine-1-yl)-1-propanol methanesulfonate trihydrate RU2140910C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US223895P 1995-08-11 1995-08-11
US60/002,238 1995-08-11
PCT/IB1996/000592 WO1997007098A1 (en) 1995-08-11 1996-06-20 (1s,2s)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanolmethanesulfonate trihydrate

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