申请人:Ajinomoto Co., Inc.
公开号:EP1103544A2
公开(公告)日:2001-05-30
Use of a piperidine derivative of general formula (I) or of a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use as a 5HT2 antagonist in the treatment of ischaemic disorder, thrombosis, obstruction, arteriosclerosis, migraine or microcirculation failure, or for anti-platelet treatment:
wherein A1 represents an unsubstituted or substituted pyridyl, piperidyl, piperidino, morpholinyl, morpholino, thiomorpholinyl, thiomorpholino or piperazinyl group, a substituted alkyl group having 1 to 8 carbon atoms, a substituted cycloalkyl group having from 4 to 8 carbon atoms, or an unsubstituted or substituted alkoxy group having 1 to 8 carbon atoms,
X1 represents a hydrogen atom or a halogen atom,
Y1 represents one of the organic groups:
-CONH-, -NHCO-, -CONHCH2-, -(CH2)n-, -COO-,
wherein n is an integer of from 0 to 4, and
Z1 represents one of the organic groups:
-CH=CH-, -S-CH2-, -S-, -CH2-CH2-.
通式(I)的哌啶衍生物或其药学上可接受的盐在制造治疗缺血性疾病、血栓形成、阻塞、动脉硬化、偏头痛或微循环衰竭的5HT2拮抗剂或抗血小板治疗药物中的用途:
其中 A1 代表未取代或取代的吡啶基、哌啶基、哌啶基、吗啉基、吗啉基、 硫代吗啉基、硫代吗啉基或哌嗪基、具有 1 至 8 个碳原子的取代烷基、具有 4 至 8 个碳原子的取代环烷基或具有 1 至 8 个碳原子的未取代或取代烷氧基、
X1 代表氢原子或卤素原子、
Y1 代表有机基团之一:
-CONH-、-NHCO-、-CONHCH2-、-(CH2)n-、-COO-、
其中 n 为 0 至 4 的整数,以及
Z1 代表有机基团之一:
-ch=ch-、-s-ch2-、-s-、-ch2-ch2-。