公开(公告)号：US5750544A

公开(公告)日：1998-05-12

申请号：US635318

申请日：1996-04-19

申请人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

发明人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

IPC分类号： C07D311/58 ,  C07D405/06 ,  C07D521/00 ,  A61K31/44

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D311/58 ,  C07D405/06

摘要： Fused phenol derivatives of the formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 each, independently, is H, halogen, trifluoromethyl, cyano, (substituted) alkyl, alkoxy, cycloalkyl, COOH, COOR.sup.6 (in which R.sup.6 is C1-6 alkyl), alkenyl or R.sup.1 and R.sup.2, taken together, is --CH.dbd.CH--CH.dbd.CH--, when R.sup.1 and R.sup.2 are ortho to each other; A is alkylene, alkenylene, oxyalkylene or ##STR2## (in which m is 1-6); B is a monocyclic hetero ring containing a nitrogen atom; G is --OR.sup.3A or --NR.sup.3B R.sup.3C (in which R.sup.3A, R.sup.3B and R.sup.3C each, independently, is H, alkyl, acyl, or alkoxyalkyl); R.sup.4 and R.sup.5 each, independently, is H, alkyl, or R.sup.4, R.sup.5 together with the carbon atom to which they are attached represent C4-7 cycloalkyl; and n is 1-3; non-toxic salts thereof, non-toxic acid addition salts thereof, and hydrates thereof. The compounds of the formula (I) have inhibitory activities on TXA.sub.2 synthetase and on 5-lipoxygenase and/or a scavenging activity on active oxygen species, and are useful for the prevention and/or the treatment of thrombosis, arteriosclerosis, ischemic heart diseases or brain diseases, bronchial asthma, renal inflammation, rheumatism, arthritis, gout, psoriasis, ulcerative colitis, trichophytosis, cardiac infarction, allergic diseases, etc.

摘要翻译： （I）的稠合酚衍生物：其中R 1和R 2各自独立地是H，卤素，三氟甲基，氰基，（取代的）烷基，烷氧基，环烷基，COOH，COOR 6（其中R 6 当R1和R2彼此邻位时，A是亚烷基，亚烯基，氧化烯或（IMAGE）（在C 1 -C 6烷基中），链烯基或R 1和R 2一起是-CH = CH-CH = CH- 其中m是1-6）; B是含有氮原子的单环杂环; G是-OR3A或-NR3BR3C（其中R3A，R3B和R3C各自独立地是H，烷基，酰基或烷氧基烷基）; R4 且R 5各自独立地为H，烷基或R 4，R 5与它们所连接的碳原子一起代表C4-7环烷基; n为1-3;其无毒盐，无毒酸加成盐 式（I）化合物对TXA2合成酶和5-脂氧合酶和/或对活性氧物质的清除活性具有抑制活性，可用于预防和/或治疗o 血栓形成，动脉硬化，缺血性心脏病或脑疾病，支气管哮喘，肾脏炎症，风湿病，关节炎，痛风，牛皮癣，溃疡性结肠炎，毛发症，心肌梗塞，过敏性疾病等。

公开(公告)号：US5534536A

公开(公告)日：1996-07-09

申请号：US294015

申请日：1994-08-23

申请人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

发明人： Shuichi Ohuchida ,  Fumio Nambu ,  Masaaki Toda

IPC分类号： C07D311/58 ,  C07D405/06 ,  C07D521/00 ,  A61K31/415

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D311/58 ,  C07D405/06

摘要： Fused phenol compounds of the formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 each, independently, is H, halogen, trifluoromethyl, cyano, (substituted) alkyl, alkoxy, cycloalkyl, COOH, COOR.sup.6 (in which R.sup.6 is C1-6 alkyl), alkenyl or R.sup.1 and R.sup.2, taken together, is --CH.dbd.CH--CH.dbd.CH--, when R.sup.1 and R.sup.2 are ortho to each other; A is alkylene, alkenylene, oxyalkylene or ##STR2## (in which m is 1-6); B is a monocyclic hetero ring containing a nitrogen atom; G is --OR.sup.3A or --NR.sup.3B R.sup.3C (in which R.sup.3A, R.sup.3B and R.sup.3C each, independently, is H, alkyl, acyl, or alkoxyalkyl); R.sup.4 and R.sup.5 each, independently, is H, alkyl, or R.sup.4, R.sup.5 together with the carbon atom to which they are attached represent C4-7 cycloalkyl; and n is 1-3; non-toxic salts thereof, non-toxic acid addition salts thereof, and hydrates thereof.The compounds of the formula (I) have inhibitory activities on TXA.sub.2 synthetase and on 5-lipoxygenase and/or a scavenging activity on active oxygen species, and are useful for the prevention and/or the treatment of thrombosis, arteriosclerosis, ischemic heart diseases or brain diseases, bronchial asthma, renal inflammation, rheumatism, arthritis, gout, psoriasis, ulcerative colitis, trichophytosis, cardiac infarction, allergic diseases, etc.

摘要翻译： 式（I）的稠合酚化合物：其中R 1和R 2各自独立地是H，卤素，三氟甲基，氰基，（取代的）烷基，烷氧基，环烷基，COOH，COOR 6（其中R 6 当R1和R2彼此邻位时，A是亚烷基，亚烯基，氧化烯或（IMAGE）（在C 1 -C 6烷基中），链烯基或R 1和R 2一起是-CH = CH-CH = CH- 其中m是1-6）; B是含有氮原子的单环杂环; G是-OR3A或-NR3BR3C（其中R3A，R3B和R3C各自独立地是H，烷基，酰基或烷氧基烷基）; R4 且R 5各自独立地为H，烷基或R 4，R 5与它们所连接的碳原子一起代表C4-7环烷基; n为1-3;其无毒盐，无毒酸加成盐 式（I）化合物对TXA2合成酶和5-脂氧合酶和/或对活性氧物质的清除活性具有抑制活性，可用于预防和/或治疗 血栓形成，动脉硬化，缺血性心脏病或脑疾病，支气管哮喘，肾脏炎症，风湿病，关节炎，痛风，牛皮癣，溃疡性结肠炎，毛发症，心肌梗塞，过敏性疾病等。