发明申请
US20090270399A1 NOVEL PYRIDAZINE DERIVATIVES AND MEDICINES CONTAINING THE SAME AS EFFECTIVE INGREDIENTS
审中-公开
基本信息:
- 专利标题： NOVEL PYRIDAZINE DERIVATIVES AND MEDICINES CONTAINING THE SAME AS EFFECTIVE INGREDIENTS
- 专利标题（中）：新的吡咯烷酮衍生物和含有相同成分的药物
- 申请号：US12497797 申请日：2009-07-06
- 公开(公告)号：US20090270399A1 公开(公告)日：2009-10-29
- 发明人： Masao OHKUCHI , Yoshinori Kyotani , Hiromichi Shigyo , Tomoyuki Koshi , Takahiro Kitamura , Tadaaki Ohgiya , Takayuki Matsuda , Yukiyoshi Yamazaki , Natsuyo Kumai , Kyoko Kotaki , Hideo Yoshizaki , Yuriko Habata
- 申请人： Masao OHKUCHI , Yoshinori Kyotani , Hiromichi Shigyo , Tomoyuki Koshi , Takahiro Kitamura , Tadaaki Ohgiya , Takayuki Matsuda , Yukiyoshi Yamazaki , Natsuyo Kumai , Kyoko Kotaki , Hideo Yoshizaki , Yuriko Habata
- 申请人地址： JP Aichi
- 专利权人： Kowa Co., Ltd.
- 当前专利权人： Kowa Co., Ltd.
- 当前专利权人地址： JP Aichi
- 优先权： JP9-318132 19971119; JP9-318133 19971119
- 主分类号： A61K31/50
- IPC分类号： A61K31/50 ; C07D237/14
摘要：
This invention relates to pyridazine derivatives represented by the formula (1): wherein R1 represents a (substituted) aryl group, R2 represents a phenyl group substituted at 4-position by a lower alkoxyl, group or a lower alkylthio group, R3 represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (substituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.
摘要（中）：
本发明涉及由式（1）表示的哒嗪衍生物：其中R1表示（取代）芳基，R2表示在4-位被低级烷氧基，低级烷硫基或低级烷硫基取代的苯基，R3表示低级 烷氧基，卤代低级烷基，低级环烷基，（取代）芳基，（取代）芳氧基，（取代）含氮杂环残基，（取代）氨基羰基或低级烷基羰基 A表示单键，低级亚烷基或低级亚烯基，X表示O或S，虚线表示4-位和5-位之间的碳 - 碳键为单键或 双键或其盐; 以及含有它们作为有效成分的药物。 这些化合物对白细胞介素-1β生产具有优异的抑制活性，可用作免疫系统疾病，炎性疾病，缺血性疾病等的预防药物和治疗剂。
IPC结构图谱:
| A | 人类生活必需 |
| --A61 | 医学或兽医学；卫生学 |
| ----A61K | 医用、牙科用或梳妆用的配制品 |
| ------A61K31/00 | 含有机有效成分的医药配制品 |
| --------A61K31/33 | .杂环化合物 |
| ----------A61K31/335 | ..仅有氧作为环杂原子的，例如制霉色基素 |
| ------------A61K31/40 | ...有仅以1个氮作为环杂原子的五元环的，例如舒必利、琥珀酰亚胺、托尔米丁、甲氧吡丁苯 |
| --------------A61K31/50 | ....哒嗪；氢化哒嗪 |