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    • 4. 发明授权
    • Quinolinone derivative, method for preparing the same, and anti-allergic
agent
    • 喹啉酮衍生物,其制备方法和抗过敏剂
    • US6136822A
    • 2000-10-24
    • US201662
    • 1998-12-01
    • Hidetsugu TakagakiShinobu YamaguchiMasayoshi AbeMitsuru SakaiOsamu Misumi
    • Hidetsugu TakagakiShinobu YamaguchiMasayoshi AbeMitsuru SakaiOsamu Misumi
    • C07D215/22A61K31/00A61K31/47A61K31/4704A61P37/00A61P37/08C07C235/16C07D215/38C07D215/40C07D215/48C07D401/12C07D405/04C07D405/06C07D215/16C07D215/20C07D215/36
    • C07D215/22C07C235/16C07D215/38C07D215/40C07D215/48C07D401/12C07D405/04C07D405/06
    • The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method; novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients. The quinolinone derivative is expressed by the following general formula (II); and the method is characterized in that an amide derivative, expressed by the following formula (I), is reacted with a basic agent, followed by intramolecular ring formation: ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group an alkenyl group, or an aryl group; R.sub.2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R.sub.3 represents a reactive carboxyl group; and R.sub.4 to R.sub.7 represent, respectively and independently, a hydrogen atom; a hydroxyl group; an alkyl group; an alkoxy group; an alkenyl group; an alkenyloxy group; an aryl group; an aryloxy group; an aralkyloxy group; a R.sub.8 R.sub.9 N group wherein R.sub.8 and R.sub.9 represent, respectively and independently, a hydrogen atom, an alkyl group, an alkenyl group an aralkyl group, or an acyl group; a nitro group; or a R.sub.10 OOC group wherein R.sub.10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; ##STR2## wherein R.sub.1, R.sub.2 and R.sub.4 to R.sub.7 represent, respectively, the same constituents as described in formula (I).
    • 本发明涉及一种制备喹啉酮衍生物的简单方法,其作为药物是有效的,例如用作治疗过敏性疾病等的药剂; 在该方法中作为中间体有效的新型酰胺衍生物; 按照该方法得到的新型喹啉酮衍生物; 以及含有与活性成分相同的喹啉酮衍生物和/或其生理盐的抗过敏剂。 喹啉酮衍生物由以下通式(II)表示; 该方法的特征在于将由下式(I)表示的酰胺衍生物与碱性试剂反应,然后分子内环形成:其中R 1表示氢原子,烷基,含有羟基的烷基 烯基或芳基; R2表示烷基,烯基,芳基或芳烷基; R3代表活性羧基; 和R 4至R 7分别独立地表示氢原子; 羟基; 烷基; 烷氧基 烯基; 烯氧基; 芳基; 芳氧基; 芳烷氧基; R8R9N基,其中R8和R9分别独立地表示氢原子,烷基,烯基,芳烷基或酰基; 硝基; 或R10OOC基,其中R10表示氢原子,烷基,烯基,芳基或芳烷基; 其中R1,R2和R4至R7分别表示与式(I)中所述相同的组分。
    • 6. 发明授权
    • Quinolinone derivative, method for preparing the same, and anti-allergic agent
    • 喹啉酮衍生物,其制备方法和抗过敏剂
    • US06271416B1
    • 2001-08-07
    • US09595909
    • 2000-06-20
    • Hidetsugu TakagakiShinobu YamaguchiMasayoshi AbeMitsuru SakaiOsamu Misumi
    • Hidetsugu TakagakiShinobu YamaguchiMasayoshi AbeMitsuru SakaiOsamu Misumi
    • C07C22900
    • C07D215/22C07C235/16C07D215/38C07D215/40C07D215/48C07D401/12C07D405/04C07D405/06
    • The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method, novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients. The quinolinone derivative is expressed by the following general formula (II); and the method is characterized in that an amide derivative, expressed by the following general formula (I), is reacted with a basic agent, followed by intramolecular ring formation: General Formula (I) [wherein, R1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group, an alkenyl group, or an aryl group; R2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R3 represents a reactive carboxyl group; and R4 to R7 represent, respectively and independently, a hydrogen atom, a hydroxyl group, an alkyl group, an alkoxy group, an alkenyl group, an alkenyloxy group, an aryl group, an aryloxy group, an aralkyloxy group, a R8R9N group (wherein, R8 and R9 represent, respectively and independently, a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, or an acyl group), a nitro group, or a R10OOC group (wherein, R10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group)]. General Formula (II) [wherein, R1, R2 and R4 to R7 represent, respectively, the same constituents as described in general formula (I)].
    • 本发明涉及一种制备喹啉酮衍生物的简单方法,其作为药物是有效的,例如用作治疗过敏性疾病等的药剂; 该方法中作为中间体有效的新型酰胺衍生物,按照该方法得到的新型喹啉酮衍生物; 以及含有与活性成分相同的喹啉酮衍生物和/或其生理盐的抗过敏剂。 喹啉酮衍生物由以下通式(II)表示; 该方法的特征在于将由以下通式(I)表示的酰胺衍生物与碱性试剂反应,然后分子内环形成:通式(I)[其中,R 1表示氢原子,烷基 基团,含有羟基,烯基或芳基的烷基; R2表示烷基,烯基,芳基或芳烷基; R3代表活性羧基; R 4〜R 7分别独立地表示氢原子,羟基,烷基,烷氧基,烯基,烯氧基,芳基,芳氧基,芳烷氧基,R8R9N基( 其中,R8和R9分别独立地表示氢原子,烷基,烯基,芳烷基或酰基),硝基或R10OOC基(其中,R10表示氢原子, 烷基,烯基,芳基或芳烷基)]通式(II)[其中,R1,R2和R4至R7分别表示与通式(I)中所述相同的组分] 。