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MEDICINAL COMPOSITION CONTAINING CARBAMOYLMETHYLUREA DERIVATIVE AND INTERMEDIATE FOR PRODUCING CARBAMOYLMETHYLUREA DERIVATIVE
MEDICINAL COMPOSITION CONTAINING CARBAMOYLMETHYLUREA DERIVATIVE AND INTERMEDIATE FOR PRODUCING CARBAMOYLMETHYLUREA DERIVATIVE
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机译:包含氨基甲酰脲类衍生物的中间体和用于生产氨基甲酰脲类衍生物的药物组合物
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摘要
PROBLEM TO BE SOLVED: To obtain a pharmaceutical preparation, containing a carbamoylmethylurea derivative having a strong affinity for a gastrin receptor and/or a central cholecystokinin receptor and useful as a therapeutic agent for gastric or duodenal ulcer, etc. ;SOLUTION: This pharmaceutical preparation comprises a compound of formula I (R1 is H or a lower alkyl; R2 is a lower alkoxy, a lower alkylamino, etc.; R3 is phenyl; R4 is phenyl, a cycloalkyl, an alkyl or a heterocyclic ring) or its pharmaceutically permissible salt. e.g. 2-[(tert- butoxycarbonylmethyl)-[3-(m-(carboxyphenyl) ureidomethylcarbonyl]]aminobenzophenone. The compound of formula I is obtained by reacting a compound of formula II (R9 is H or a carboxy-protecting group) with carbonyldiimidazole, reacting the resultant product with a compound of formula III (R10 is the same as R9) and using the prepared urea type compound of formula IV and a 2-substituted aniline derivative as starting raw materials.;COPYRIGHT: (C)1997,JPO
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机译:解决的问题:要获得药物制剂,该药物制剂含有对胃泌素受体和/或中央胆囊收缩素受体具有强亲和力的氨基甲酰基甲基脲衍生物,并可用作胃或十二指肠溃疡等的治疗剂;解决方案:该药物制剂包含式I的化合物(R 1 Sub>是H或低级烷基; R 2 Sub>是低级烷氧基,低级烷基氨基等; R 3 < / Sub>是苯基; R 4 Sub>是苯基,环烷基,烷基或杂环)或其药学上允许的盐。例如2-[(叔丁氧基羰基甲基)-[3-(间-(羧基苯基)脲基甲基羰基]]氨基二苯甲酮。式I化合物是通过使式II化合物(R 9 Sub>为H或羧基保护基)与羰基二咪唑反应,使所得产物与式Ⅲ化合物(R 10 Sub>与R 9 Sub>相同)反应,并使用制备的脲型化合物式Ⅳ的化合物和2-取代的苯胺衍生物为原料。版权所有:(C)1997,日本特许厅
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