摘要:
An isoxazole compound having the following formula: wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 1; n is 1 to 6; ring A represents a phenyl ring or a naphthyl ring; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.
摘要:
An isoxazole compound having the following formula: ##STR1## wherein R.sup.1 represents hydrogen, halogen, alkyl, alkoxy, hydroxyl, alkylthio, amino, alkanoyl, alkanoylamino, alkanoyloxy, alkoxycarbonyl, carboxy, (alkylthio)thiocarbonyl, carbamoyl, nitro or cyano; R.sup.2 represents an amino; m is 2 or 3; n is 1 to 6; ring A represents a phenyl ring, a naphthyl ring or an aromatic heterocycle; and X represents oxygen or sulfur. The isoxazole compound has an excellent monoamine oxidase inhibitory activity, and is useful for treating Parkinson's disease, depression and Alzheimer's disease.
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要:
Pharmaceutical compositions and methods of treatment are provided for treating amyloidosis, containing, as an active ingredient, at least one nitrogen-containing heteroaryl compound represented by the following general formula or a pharmacologically permitted salt thereof; together with nitrogen-containing heteroaryl derivatives, and pharmacologically permitted salts thereof: where, R1, R2, Z1-Z5, and A are as defined herein.
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译:本发明涉及阿尔茨海默病的预防药物或补救剂,或淀粉样蛋白原纤维形成抑制剂,其包括作为活性成分的下列通式(I)的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药理学上允许的盐,其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的,或作为淀粉样蛋白原纤维形成抑制剂:(其中R 1, 和R 2是H或烷基; Z 1和Z 2是H,烷基,烷氧基,卤代烷基或卤代; Z 3 烷氧基,SH,烷硫基,NH 2,单或二烷基氨基,OH或卤素; Z 4和Z 5 >为H或卤素; A为4,6-嘧啶-1,3-二基,1,3,5-三嗪-2,6-二基等)。
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译:本发明涉及阿尔茨海默病的预防药物或补救剂,或淀粉样蛋白原纤维形成抑制剂,其包括作为活性成分的下列通式(I)的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐,其作为阿尔茨海默病的预防剂或治疗药物是有价值的,或作为淀粉样蛋白原纤维形成抑制剂:(其中,R 1和R 2, Z 1和Z 2是H,烷基,烷氧基,卤代烷基或卤代; Z 3是烷氧基,SH,烷硫基,NH 2,一或二烷基氨基,OH或卤素; Z 4和Z 5是H或卤素; A是4,6-嘧啶-1,3-二基,1,3,5-三嗪-2,6-二基等)。
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译:本发明涉及阿尔茨海默病的预防药物或补救剂,或淀粉样蛋白原纤维形成抑制剂,其包括作为活性成分的下列通式(I)的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐,其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的,或作为淀粉样蛋白原纤维形成抑制剂:(其中,R 1和R 2为H或烷基; Z 1 Z 2是H,烷基,烷氧基,卤代烷基或卤代; Z 3是烷氧基,SH,烷硫基,NH 2,一或二烷基氨基,OH或卤素; Z 4和Z 5是H或卤素; A是4,6- -1,3-二基,1,3,5-三嗪-2,6-二基等)。
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译:本发明涉及阿尔茨海默病的预防药物或补救剂,或淀粉样蛋白原纤维形成抑制剂,其包括作为活性成分的下列通式(I)的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐,其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的,或作为淀粉样蛋白原纤维形成抑制剂:(其中,R 1和R 2为H或烷基; Z 1 Z 2是H,烷基,烷氧基,卤代烷基或卤代; Z 3是烷氧基,SH,烷硫基,NH 2,一或二烷基氨基,OH或卤素; Z 4和Z 5是H或卤素; A是4,6- -1,3-二基,1,3,5-三嗪-2,6-二基等)。
摘要:
The present invention relates to preventives or remedies for Alzheimer's disease, or to amyloid protein fibril-formation inhibitors, which include as an active ingredient a compound of general formula (I) below or a pharmacologically permitted salt thereof; and also to nitrogen-containing heteroaryl derivatives having specific substituents, or pharmacologically permitted salts thereof, which are valuable as preventives or remedies for Alzheimer's disease, or as amyloid protein fibril-formation inhibitors: (where, R1 and R2 are H or alkyl; Z1 and Z2 are H, alkyl, alkoxy, haloalkyl or halogeno; Z3 is alkoxy, SH, alkylthio, NH2, mono- or di-alkylamino, OH or halogeno; Z4 and Z5 are H or halogeno; and A is 4,6-pyrimidine-1,3-diyl, 1,3,5-triazine-2,6-diyl, etc).
摘要翻译:本发明涉及阿尔茨海默病的预防药物或补救剂,或淀粉样蛋白原纤维形成抑制剂,其包括作为活性成分的下列通式(I)的化合物或其药理学允许的盐; 以及具有特定取代基的含氮杂芳基衍生物或其药学上允许的盐,其作为阿尔茨海默氏病的预防剂或治疗剂是有价值的,或作为淀粉样蛋白原纤维形成抑制剂:(其中,R 1和R 2为H或烷基; Z 1 Z 2是H,烷基,烷氧基,卤代烷基或卤代; Z 3是烷氧基,SH,烷硫基,NH 2,一或二烷基氨基,OH或卤素; Z 4和Z 5是H或卤素; A是4,6- -1,3-二基,1,3,5-三嗪-2,6-二基等)。