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Priority claimed from PCT/JP1995/000736external-prioritypatent/WO1995028177A1/en
Publication of KR970702037ApublicationCriticalpatent/KR970702037A/en
Medicines That Contain Protein Lipid Enzymes And Other Medicines
(AREA)
Abstract
포스포디에스테라아제에 대한 효소억제활성을 갖는 화합물을 유효성분으로서 함유하는 지발성 디스키네시아의 치료용 의약조성물을 제공한다. 유효성분으로서는 롤리프람이 바람직하다. 할로페리돌의 연속투여에 의하여 쥐에 유발되는 지발성 디스키네시아의 실험 모델에 롤리프람을 투여하면, 용량의존적으로 지발성 디스키네시아 증상이 억제되는 치료효과를 얻는다.Provided is a pharmaceutical composition for treating delayed dyskinesia containing a compound having an enzyme inhibitory activity against phosphodiesterase as an active ingredient. As an active ingredient, rolipram is preferable. Administration of rolipram in the experimental model of delayed dyskinesia induced by rats by continuous administration of haloperidol provides a therapeutic effect that suppresses delayed dyskinesia symptoms in a dose-dependent manner.
Description
지발성 디스키네시아의 치료용 의약 조성물과 이의 용도 기술분야Pharmaceutical compositions for the treatment of delayed dyskinesia and uses thereof
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.
Claims (6)
포스포디에스테라아제에 대한 효소억제 활성을 가지고 투여후에 혈액-뇌관문을 통과할 수 있는 화합물을 유효성분으로서 함유하고, 또한 유효성분용으로 제약학적으로 허용되는 담체를 조합하여 함유함을 특징으로 하는 지연성 디스키네시아의 치료용 의약 조성물.Delay characterized in that it contains a compound having an enzyme inhibitory activity against phosphodiesterase and capable of crossing the blood-brain barrier after administration as an active ingredient, and in combination with a pharmaceutically acceptable carrier for the active ingredient. Pharmaceutical composition for the treatment of sexual dyskinesia.제1항에 있어서, 고리형 아데노신-3′, 5′-일인산(cAMP)인 포스포디에스테라아제 IV에 대한 효소억제활성을 가지고 투여후에 혈액-뇌관문을 통과할 수 있는 화합물을 유효성분으로 함유하는 의약조성물.The compound according to claim 1, which has an enzyme inhibitory activity against phosphodiesterase IV, which is cyclic adenosine-3 ', 5'-monophosphate (cAMP), and which can pass through the blood-brain barrier after administration as an active ingredient. Pharmaceutical composition to say.제2항에 있어서, 포스포디에스테라아제 IV에 대한 효소억제 활성을 갖는 화합물이 롤리프람인 의약조성물.The pharmaceutical composition according to claim 2, wherein the compound having enzymatic inhibitory activity against phosphodiesterase IV is rolipram.뇌내의 도파민 신경계의 도파민 D2유용체에 대하여 길항제로서 작용하는 항정신병 약제, 특히 정신분열병 치료약제의 장기간 투여에 의하여 일어나는 지발성 디에스테라아제, 특히 포스포디에스테라아제 IV에 대한 효소억제 활성을 가지고 투여후에 혈액-뇌관문을 통과할 수 있는 화합물을 치료 유효량으로 투여하는 것으로 이루어지는 지발성 디스키네시아의 치료방법.After administration with enzymatic inhibitory activity against long-acting diasterases, in particular phosphodiesterase IV, caused by prolonged administration of antipsychotics, particularly schizophrenia drugs, which act as antagonists to dopamine D 2 useful substances in the dopamine nervous system in the brain A method of treating delayed dyskinesia, comprising administering a therapeutically effective amount of a compound capable of crossing the blood-brain barrier.지발성 디스키네시아 치료제의 제조에 있어서 포스포디에스테라아제에 대한 효소억제 활성을 가지고 투여후에 혈액-뇌관문을 통과할 수 있는 화합물의 용도.Use of a compound having enzymatic inhibitory activity against phosphodiesterase and capable of crossing the blood-brain barrier after administration in the preparation of a delayed dyskinesia therapy.포스포디에스테라아제에 대한 효소억제 활성을 가지고 투여후에 혈액-뇌관문을 통과할 수 있는 화합물을 제약학적으로 허용할 수 있는 고체 또는 액체상의 담체와 혼합하는 것으로 이루어지는, 지발성 디스키네시아의 치료용 의약조성물의 제조법.A medicament for the treatment of delayed dyskinesia, comprising mixing a compound capable of passing the blood-brain barrier after administration with a pharmaceutically acceptable solid or liquid carrier, with enzymatic inhibitory activity against phosphodiesterase. Preparation of the composition.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019960705701A1994-04-151995-04-14
Pharmaceutical compositions for the treatment of delayed dyskinesia and uses thereof
KR970702037A
(en)
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Use of GM₁monosialogangliosides and their internal ester derivatives in humans to prevent the development of resistance to the analgesic effects of morphine and homologues in humans