发明授权
- 专利标题: Use of anti-histaminics for acute reduction of elevated intracranial pressure
- 专利标题(中): 使用抗组胺药物急性降低颅内压升高
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申请号: US10494006申请日: 2002-11-22
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公开(公告)号: US07732437B2公开(公告)日: 2010-06-08
- 发明人: Frank Tegtmeier , Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jozef Leo Henri Van Reempts
- 申请人: Frank Tegtmeier , Frans Eduard Janssens , Joseph Elisabeth Leenaerts , Koenraad Arthur van Rossem , Manuel Jesús Alcázar-Vaca , Pedro Martínez-Jiménez , José Manuel Bartolomé-Nebreda , Antonio Gómez-Sánchez , Francisco Javier Fernández-Gadea , Jozef Leo Henri Van Reempts
- 申请人地址: BE Beerse
- 专利权人: Janssen Pharmaceutica, NV.
- 当前专利权人: Janssen Pharmaceutica, NV.
- 当前专利权人地址: BE Beerse
- 优先权: EP01204574 20011123
- 国际申请: PCT/EP02/13180 WO 20021122
- 国际公布: WO03/044023 WO 20030530
- 主分类号: A61P9/10
- IPC分类号: A61P9/10 ; A61P37/02 ; A61P37/08 ; A61K31/415 ; A61K31/425 ; C07D519/00 ; C07D487/04 ; C07D471/04
摘要:
The invention concerns a novel histamine receptor antagonist and the use of an histamine receptor antagonist for the reduction of intracranial pressure (ICP), in particular for the prevention and treatment of elevated intracranial pressure and/or secondary ischaemida, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury. The novel compounds comprise compounds according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6H-benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenyl-methyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2-α]benzimidazol-4(10H)-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof. Also claimed is the novel use of commercially available histamine H1-and H2-receptor antagonists for the reduction of intracranial pressure (ICP).
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