Abstract:
본 발명은 하기 화학식 1로 표시되는 신규 피롤로피리디논 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 함유하는 MCH 수용체-1(멜라닌 농축 호르몬) 관련 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 따른 유도체는 MCH 수용체-1에 대한 길항제로 작용함으로써 MCH가 MCH 수용체-1에 결합함으로써 유발되는 비만, 당뇨병, 대사장애, 불안증 및 우울증과 같은 MCH 수용체-1 관련 질환을 예방 또는 치료하는데 유용하게 사용할 수 있다.
Abstract:
PURPOSE: A 2-(2-oxo-2-phenylethylsulfanyl)-benzimidazole-4-carboximide derivative is provided to prevent or treat diseases caused by over-activation of poly(ADP-ribose)polymerase-1(PARP-1) and protect heart during surgery or drug therapy. CONSTITUTION: A 2-(2-oxo-2-phenylethylsulfanyl)-benzimidazole-4-carboximide derivative is denoted by chemical formula 1. The 2-(2-oxo-2-phenylethylsulfanyl)-benzimidazole-4-carboximide derivative is prepared by performing alkylation of a compound of chemical formula 2 with a compound of chemical formula 3 under the presence of basic catalyst or without the catalyst. A pharmaceutical composition for preventing or treating diseases caused by over-activation of poly(ADP-ribose)polymerase-1(PARP-1) contains the 2-(2-oxo-2-phenylethylsulfanyl)-benzimidazole-4-carboximide derivative or its pharmaceutically acceptable salt as an active ingredient. The disease is ischemic disease or neurodegenerative disease.
Abstract:
PURPOSE: A 2-benzylsulfanyl-benzimidazole-4-carboximide derivative is provided to ensure activity of suppressing poly(ADP-ribose)polymerase-1-(PARP-1) and to prevent or treat diseases caused by over-activation of the PARP-1. CONSTITUTION: A 2-benzylsulfanyl-benzimidazole-4-carboximide derivative is denoted by chemical formula 1. The 2-benzylsulfanyl-benzimidazole-4-carboximide derivative is prepared by performing alkylation of a compound of chemical formula 2 with a compound of chemical formula 3 at room temperature to boiling point under the presence of basic catalyst. The catalyst is carbonate, hydroxise, hydride, alkoxide, triethylamine, or pyridine. A pharmaceutical composition for preventing or treating diseases caused by over-activation of poly(ADP-ribose)polymerase-1(PARP-1) contains the 2-benzylsulfanyl-benzimidazole-4-carboximide derivative of chemical formula 1 or its pharmaceutically acceptable salt as an active ingredient.