公开(公告)号：KR1020030026803A

公开(公告)日：2003-04-03

申请号：KR1020017016484

申请日：2001-07-26

Applicant: 삼성전자주식회사

Inventor： 고성보 ,  오유진 ,  김언겸 ,  김원엽 ,  데니스더블유최 ,  라우라엘두간 ,  고재영 ,  원무호 ,  위명복

IPC: C07D293/10

Abstract: PURPOSE: Seleno compounds containing nitrone moiety, a preparation process thereof and the uses thereof as therapeutics are provided. The compounds have low toxicity and improved lipid peroxide inhibiting activity to effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The Seleno compounds containing nitrone moiety represented by formula(I) are provided, wherein R1 and R2 are the same or different, hydrogen, halogen, C1-4-alkyl, C1-4-alkoxy, hydroxy, trifluoromethyl, nitro or R1 and R2 are methylenedioxy together; and L is phenyl, C1-4 alkylphenyl, or an unsaturated or saturated heterocyclic group having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, benzothiazolyl, benzoimidazolyl, benzotriazolyl, triazinyl and triazolyl. The Seleno compounds containing nitrone moiety are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.

Abstract translation: 目的：提供含有硝酮部分的硒化合物，其制备方法及其作为治疗剂的用途。 该化合物具有低毒性和改善的脂质过氧化物抑制活性，有效抑制ROS（活性氧）和/或过量锌离子对脑神经元的死亡。 提供：含有由式（I）表示的硝酮部分的硒化合物，其中R 1和R 2相同或不同，为氢，卤素，C 1-4 - 烷基，C 1-4 - 烷氧基，羟基，三氟甲基，硝基或R 1 R2是亚甲二氧基; L是苯基，C 1-4烷基苯基或具有1至4个氮，氧和/或硫杂原子的不饱和或饱和杂环基，选自呋喃基，恶唑基，异恶唑基，噻吩基，噻唑基，异噻唑基，吡咯基 咪唑基，吡唑基，噻二唑基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并咪唑基，苯并三唑基，三嗪基和三唑基。 含有硝酮部分的硒化合物可用于治疗和预防由ROS引起的疾病和过量的锌离子，如中风，帕金森病和阿尔茨海默病。

公开(公告)号：KR100454649B1

公开(公告)日：2004-11-05

申请号：KR1020017016484

申请日：2001-07-26

Applicant: 삼성전자주식회사

Inventor： 고성보 ,  오유진 ,  김언겸 ,  김원엽 ,  데니스더블유최 ,  라우라엘두간 ,  고재영 ,  원무호 ,  위명복

IPC: C07D293/10

Abstract: PURPOSE: Seleno compounds containing nitrone moiety, a preparation process thereof and the uses thereof as therapeutics are provided. The compounds have low toxicity and improved lipid peroxide inhibiting activity to effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The Seleno compounds containing nitrone moiety represented by formula(I) are provided, wherein R1 and R2 are the same or different, hydrogen, halogen, C1-4-alkyl, C1-4-alkoxy, hydroxy, trifluoromethyl, nitro or R1 and R2 are methylenedioxy together; and L is phenyl, C1-4 alkylphenyl, or an unsaturated or saturated heterocyclic group having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, benzothiazolyl, benzoimidazolyl, benzotriazolyl, triazinyl and triazolyl. The Seleno compounds containing nitrone moiety are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.

Abstract translation: 目的：提供含有硝酮部分的硒化合物，其制备方法及其作为治疗剂的用途。 该化合物具有低毒性和改善的脂质过氧化物抑制活性，可有效抑制ROS（活性氧）和/或过量锌离子导致的脑神经元死亡。 构成：提供了式（I）代表的含硝酮部分的硒代化合物，其中R 1和R 2相同或不同，为氢，卤素，C 1-4烷基，C 1-4烷氧基，羟基，三氟甲基，硝基或R 1 和R2一起是亚甲二氧基; L为苯基，C 1-4烷基苯基或具有1-4个氮，氧和/或硫杂原子的不饱和或饱和杂环基，所述杂原子选自呋喃基，恶唑基，异恶唑基，噻吩基，噻唑基，异噻唑基，吡咯基 咪唑基，吡唑基，噻二唑基，吡啶基，嘧啶基，吡嗪基，哒嗪基，苯并噻唑基，苯并咪唑基，苯并三唑基，三嗪基和三唑基。 含有硝酮部分的Seleno化合物可用于治疗和预防由ROS和过量锌离子引起的疾病，例如中风，帕金森病和阿尔茨海默氏病。

公开(公告)号：KR1020030026801A

公开(公告)日：2003-04-03

申请号：KR1020017016481

申请日：2001-07-26

Applicant: 삼성전자주식회사

Inventor： 오유진 ,  고성보 ,  김경화 ,  장인규 ,  데니스더블유최 ,  라우라엘두간 ,  고재영 ,  신인재 ,  원무호

IPC: C07D213/74

Abstract: PURPOSE: Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their uses as therapeutics are provided. The compounds have low toxicity and improved lipid peroxidation(LPO) inhibiting activity, therefore they effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The dialkylhydroxybenzoic acid derivatives containing metal chelating groups are characteristically represented by formula(I), wherein R1 is hydrogen, or straight or branched alkyl; R2 is hydrogen or alkyl; R3 is CO2H, CONH2 or CONR4R5; R4 is hydrogen, alkyl, or aryl; and R5 is unsaturated or saturated heterocyclic having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl and tetrazolyl. The dialkylhydroxybenzoic acid derivatives are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.

Abstract translation: 目的：提供含有金属螯合基团的二烷基羟基苯甲酸衍生物及其作为治疗剂的用途。 这些化合物具有低毒性和改善的脂质过氧化（LPO）抑制活性，因此它们有效地通过ROS（活性氧）和/或过量的锌离子来有效地抑制脑神经元的死亡。 构成：含有金属螯合基团的二烷基羟基苯甲酸衍生物特征性地由式（I）表示，其中R 1是氢或直链或支链烷基; R2是氢或烷基; R3是CO2H，CONH2或CONR4R5; R4是氢，烷基或芳基; R5是具有1-4个氮，氧和/或硫杂原子的不饱和或饱和杂环，选自呋喃基，恶唑基，异恶唑基，噻吩基，噻唑基，异噻唑基，吡咯基，咪唑基，吡唑基，恶二唑基，噻二唑基，吡啶基 ，嘧啶基，吡嗪基，哒嗪基，三嗪基和四唑基。 二烷基羟基苯甲酸衍生物可用于治疗和预防由ROS引起的疾病和过量的锌离子，如中风，帕金森病和阿尔茨海默氏病。

公开(公告)号：KR1020030026802A

公开(公告)日：2003-04-03

申请号：KR1020017016482

申请日：2001-07-26

Applicant: 삼성전자주식회사

Inventor： 오유진 ,  고성보 ,  김원엽 ,  김경화 ,  데니스더블유최 ,  라우라엘두간 ,  강태천 ,  고재영 ,  김경미 ,  신인재

IPC: C07D213/74

Abstract: PURPOSE: N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups, a preparation process thereof and the uses thereof as therapeutics are provided. The compounds have low toxicity and improved lipid peroxidation(LOP) inhibiting activity, so that they can effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups represented by formula(I) are provided, wherein R1 is branched alkyl, aralkyl, aryl or substituted aryl; R2 is hydrogen or COR6 wherein R6 is alkyl or aryl; R3 is CO2H, CONH2 or CONR4R5; R4 is hydrogen, alkyl, or aryl; and R5 is unsaturated or saturated heterocyclic having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl and tetrazolyl. The N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.

Abstract translation: 目的：提供含有金属螯合基团的N-烷基-N-苯基羟胺化合物，其制备方法及其用途作为治疗剂。 这些化合物具有低毒性和改善的脂质过氧化（LOP）抑制活性，从而可以有效地抑制ROS（活性氧）和/或过量锌离子对脑神经元的死亡。 构成：提供含有由式（I）表示的金属螯合基团的N-烷基-N-苯基羟胺化合物，其中R 1是支链烷基，芳烷基，芳基或取代的芳基; R2是氢或COR6，其中R6是烷基或芳基; R3是CO2H，CONH2或CONR4R5; R4是氢，烷基或芳基; R5是具有1-4个氮，氧和/或硫杂原子的不饱和或饱和杂环，选自呋喃基，恶唑基，异恶唑基，噻吩基，噻唑基，异噻唑基，吡咯基，咪唑基，吡唑基，恶二唑基，噻二唑基，吡啶基 ，嘧啶基，吡嗪基，哒嗪基，三嗪基和四唑基。 含有金属螯合基团的N-烷基-N-苯基羟胺化合物可用于治疗和预防由ROS引起的疾病和过量的锌离子，如中风，帕金森病和阿尔茨海默病。

公开(公告)号：KR100454648B1

公开(公告)日：2004-11-05

申请号：KR1020017016482

申请日：2001-07-26

Applicant: 삼성전자주식회사

Inventor： 오유진 ,  고성보 ,  김원엽 ,  김경화 ,  데니스더블유최 ,  라우라엘두간 ,  강태천 ,  고재영 ,  김경미 ,  신인재

IPC: C07D213/74

Abstract: PURPOSE: N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups, a preparation process thereof and the uses thereof as therapeutics are provided. The compounds have low toxicity and improved lipid peroxidation(LOP) inhibiting activity, so that they can effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups represented by formula(I) are provided, wherein R1 is branched alkyl, aralkyl, aryl or substituted aryl; R2 is hydrogen or COR6 wherein R6 is alkyl or aryl; R3 is CO2H, CONH2 or CONR4R5; R4 is hydrogen, alkyl, or aryl; and R5 is unsaturated or saturated heterocyclic having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl and tetrazolyl. The N-alkyl-N-phenylhydroxylamine compounds containing metal chelating groups are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.

Abstract translation: 目的：提供含有金属螯合基团的N-烷基-N-苯基羟胺化合物，其制备方法及其作为治疗剂的用途。 该化合物具有低毒性和改善的脂质过氧化（LOP）抑制活性，因此它们可以有效地抑制ROS（活性氧）和/或过量的锌离子导致的脑神经元死亡。 构成：提供了由式（I）表示的含金属螯合基团的N-烷基-N-苯基羟胺化合物，其中R 1为支链烷基，芳烷基，芳基或取代芳基; R2是氢或COR6，其中R6是烷基或芳基; R3是CO2H，CONH2或CONR4R5; R4是氢，烷基或芳基; 并且R 5为具有1至4个选自呋喃基，恶唑基，异恶唑基，噻吩基，噻唑基，异噻唑基，吡咯基，咪唑基，吡唑基，恶二唑基，噻二唑基，吡啶基 ，嘧啶基，吡嗪基，哒嗪基，三嗪基和四唑基。 含有金属螯合基团的N-烷基-N-苯基羟胺化合物可用于治疗和预防由ROS和过量锌离子引起的疾病，例如中风，帕金森病和阿尔茨海默氏病。

公开(公告)号：KR100454647B1

公开(公告)日：2004-11-05

申请号：KR1020017016481

申请日：2001-07-26

Applicant: 삼성전자주식회사

Inventor： 오유진 ,  고성보 ,  김경화 ,  장인규 ,  데니스더블유최 ,  라우라엘두간 ,  고재영 ,  신인재 ,  원무호

IPC: C07D213/74

Abstract: PURPOSE: Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their uses as therapeutics are provided. The compounds have low toxicity and improved lipid peroxidation(LPO) inhibiting activity, therefore they effectively inhibit the death of cerebral neuron by ROS(reactive oxygen species) and/or excess zinc ion. CONSTITUTION: The dialkylhydroxybenzoic acid derivatives containing metal chelating groups are characteristically represented by formula(I), wherein R1 is hydrogen, or straight or branched alkyl; R2 is hydrogen or alkyl; R3 is CO2H, CONH2 or CONR4R5; R4 is hydrogen, alkyl, or aryl; and R5 is unsaturated or saturated heterocyclic having 1 to 4 nitrogen, oxygen and/or sulfur hetero atom, selected from the group consisting of furanyl, oxazolyl, isooxazolyl, thiophenyl, thiazolyl, isothiazolyl, pyrrolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, triazinyl and tetrazolyl. The dialkylhydroxybenzoic acid derivatives are useful for treatment and prevention of diseases caused by ROS and excessive zinc ion, such as stroke, Parkinson's disease and Alzheimer' disease.

Abstract translation: 目的：提供含有金属螯合基团的二烷基羟基苯甲酸衍生物及其作为治疗剂的用途。 该化合物具有低毒性和改善的脂质过氧化（LPO）抑制活性，因此它们有效地抑制ROS（活性氧）和/或过量锌离子导致的脑神经元死亡。 构成：含有金属螯合基团的二烷基羟基苯甲酸衍生物的特征在于式（I），其中R1是氢或直链或支链烷基; R2是氢或烷基; R3是CO2H，CONH2或CONR4R5; R4是氢，烷基或芳基; 并且R 5为具有1至4个选自呋喃基，恶唑基，异恶唑基，噻吩基，噻唑基，异噻唑基，吡咯基，咪唑基，吡唑基，恶二唑基，噻二唑基，吡啶基 ，嘧啶基，吡嗪基，哒嗪基，三嗪基和四唑基。 二烷基羟基苯甲酸衍生物可用于治疗和预防由ROS和过量锌离子引起的疾病，例如中风，帕金森病和阿尔茨海默氏病。