-
1.发明公开
公开(公告)号：KR1020120050841A
公开(公告)日：2012-05-21
申请号：KR1020100112296
申请日：2010-11-11
Applicant: 한국화학연구원
IPC: C07D403/06 , A61K31/496 , A61P25/00
Abstract: PURPOSE: A pyrazole butyl compound and a pharmaceutical composition containing the same are provided to ensure dopamine D4 receptor affinity and to prevent and treat central nervous system diseases. CONSTITUTION: A pyrazole butyl compound and pharmaceutically acceptable salt thereof are denoted by chemical formula 1. The salt includes inorganic acid salt, organic acid salt, amino acid salt, alkali metal salt, or ammonium salt. A method for preparing the pyrazole butyl compounds comprises: a step of performing reductive amination of pyrazole aldehyde compound of chemical formula 2 with heterocycle compounds of chemical formula 3 under the presence of reducing agent and base. A pharmaceutical composition for treating central nervous system diseases contains 1-(4-chlorophenyl)-4-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)piperazine(compound No. 33) or 1-(4-(1-phenyl-3-propyl-1H-pyrazole-5-yl)butyl)-4-(3-(trifluoromethyl)phenyl)piperazine(compound No. 36).
Abstract translation: 目的：提供吡唑丁基化合物和含有它们的药物组合物以确保多巴胺D4受体亲和力并预防和治疗中枢神经系统疾病。 构成：吡唑基丁基化合物及其药学上可接受的盐由化学式1表示。盐包括无机酸盐，有机酸盐，氨基酸盐，碱金属盐或铵盐。 制备吡唑丁基化合物的方法包括：在还原剂和碱的存在下，用化学式3的杂环化合物进行化学式2的吡唑醛化合物的还原胺化的步骤。 用于治疗中枢神经系统疾病的药物组合物含有1-（4-氯苯基）-4-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）哌嗪（化合物33）或 1-（4-（1-苯基-3-丙基-1H-吡唑-5-基）丁基）-4-（3-（三氟甲基）苯基）哌嗪（化合物36）。
-
2.发明授权
公开(公告)号：KR101246056B1
公开(公告)日：2013-03-26
申请号：KR1020100112296
申请日：2010-11-11
Applicant: 한국화학연구원
IPC: C07D403/06 , A61K31/496 , A61P25/00
Abstract: 본 발명은 피라졸부틸 화합물, 이의 제조방법 및 이를 함유하는 약학적 조성물에 관한 것이다. 본 발명의 피라졸부틸 화합물은 도파민 D
4 수용체 친화력이 우수하고, 중추신경계 질환, 구체적으로는 정신분열증, 주의력결핍 과잉행동장애, 우울증, 스트레스성 질환, 공황장애, 공포증, 강박장애, 외상후 스트레스장애, 인식장애, 알츠하이머병, 파킨슨병, 불안증, 망상분열증, 열광증, 경련장애, 인격장애, 편두통, 약물중독, 알코올 중독, 비만, 섭식 장애, 수면장애 등의 치료 및 예방제로 유용하다.
-
Search Results
2
records
(took 0.016 seconds)
