Multivalente Arzneistoffe mit kombinierter antioxidativer Wirkung und antagonistischen Effekten an 5-HT2-Rezeptor-Subtypen zur Behandlung von fibrotischem Organumbau.
HOROWSKI, REINHARD, DR.,Reinhard, Dr. Horowski,PALLA, HEINZ, DR.,Heinz, Dr. Palla,TACK, JOHANNES, DR.,Johannes, Dr. Tack
申请号：
DE102010051391
公开号：
DE102010051391A1
申请日:
2010.11.11
申请国别(地区):
DE
年份:
2012
代理人:
摘要：
Die vorliegende Erfindung beschreibt die Verwendung von 5-HT2-Rezeptor-Antagonisten und besonders von 8-α-Ergolinen wie Lisurid, Tergurid und deren Derivaten als 5-HT2B- und 5-HT2A-Rezeptor-Antagonisten und Antioxidantien in höher dosierten und bevorzugt kontinuierlichen Anwendungsformen zur Therapie. Progressionsprophylaxe und generellen Prophylaxe von nicht primär vaskulär verursachten Organfibrosen und anderem, durch mesenchymale Proliferation verursachtem pathologischem Organumbau.Lisuride (I), terguride (II) or a 1,1-diethyl-3-(R)-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-yl-urea derivative (III) is new, where (I)-(III) is useful for treating and/or preventing of fibrotic changes of organ and other vascular structure in human or animal for arresting and/or for remodeling of fibrotic changes of organs and their vascular structure. Lisuride (I), terguride (II) or a 1,1-diethyl-3-(R)-4,6,6a,7,8,9,10,10a-octahydro-indolo[4,3-fg]quinolin-9-yl-urea derivative of formula (III) is new, where (I)-(III) is useful for treating and/or preventing of fibrotic changes of organ and other vascular structure in human or animal for arresting and/or for remodeling of fibrotic changes of organs and their vascular structure. R 1> : alkyl or alkynyl R 2> : C 2H 5, n-propyl, isopropyl or alkyl R 3> : H, CH 3, C 2H 5, isopropyl or CH 2OH and dotted line : single or double bond. [Image] ACTIVITY : Hypotensive Respiratory-Gen. Cardiant Anti-HIV Fungicide Antibacterial Antiparasitic Antiinflammatory. MECHANISM OF ACTION : 5-Hydroxytryptamine 2A receptor antagonist 5-Hydroxytryptamine 2B receptor antagonist. The 5-hydroxytryptamine 2A receptor antagonistic activity of (I) was tested. The results showed that lisuride exhibited an IC 5 0value of 1 mmole/l.
