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    • 7. 发明授权
    • Phosphonic diester derivatives
    • 膦酸二酯衍生物
    • US5985858A
    • 1999-11-16
    • US91946
    • 1998-06-26
    • Kazuyoshi MiyataYasuhiro SakaiYasuo ShojiYoshihiko TsudaYasuhide InoueKeigo SatoShinya Miki
    • Kazuyoshi MiyataYasuhiro SakaiYasuo ShojiYoshihiko TsudaYasuhide InoueKeigo SatoShinya Miki
    • C07F9/6509C07F9/6539C07F9/6553C07F9/6558C07F9/6561A61K31/67A61K31/675
    • C07F9/650964C07F9/6539C07F9/655345C07F9/65583C07F9/65586C07F9/6561
    • A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R.sup.1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the group consisting of a lower alkoxy group, a lower alkyl group, a halogen atom, a halogen-substituted lower alkyl group, a lower alkanoyl group, a nitro group, a benzoyl group, a cyano group, an N-lower alkylcarbamoyl group, an N-phenyl-lower alkylcarbamoyl group, an N-(halogen-substituted phenyl)carbamoyl group and an N,N-di-lower alkylcarbamoyl group; a 1,3,4-thiadiazol-2-yl group having a halogen-substituted lower alkyl group as a substituent; a thiazolyl group; a pyridyl group which may be substituted by a halogen atom; a benzothiazol-2-yl group having 1 to 2 lower alkoxy groups on the phenyl ring; or a 4,5-dihydrothieno[3,2-e]benzothiazol-2-yl group; R.sup.2 represents a hydrogen atom or a phenyl lower alkyl group; R.sup.3 and R.sup.4 each represents a lower alkyl group; and A represents a heterocyclic ring selected from the group consisting of a pyrazine ring, a thiophene ring and a phenyl-substituted thiazole ring; the derivative being of value as an agent for treating and preventing hyperlipidemia, diabetes and cataract, or as an antitumor agent.
    • PCT No.PCT / JP96 / 03775第 371日期:1998年6月26日 102(e)日期1998年6月26日PCT 1996年12月24日PCT公布。 公开号WO97 / 24360 PCT 日期:1997年7月10日由下式(1)表示的膦酸二酯衍生物:其中R1表示环烷基; 可以具有1〜3个选自低级烷氧基,低级烷基,卤素原子,卤素取代的低级烷基,低级烷酰基,硝基,苯甲酰基的取代基的苯基 ,氰基,N-低级烷基氨基甲酰基,N-苯基 - 低级烷基氨基甲酰基,N-(卤素取代的苯基)氨基甲酰基和N,N-二低级烷基氨基甲酰基; 具有卤素取代的低级烷基作为取代基的1,3,4-噻二唑-2-基; 噻唑基 可被卤素原子取代的吡啶基; 在苯环上具有1至2个低级烷氧基的苯并噻唑-2-基; 或4,5-二氢噻吩并[3,2-e]苯并噻唑-2-基; R2表示氢原子或苯基低级烷基; R3和R4各自表示低级烷基; A表示选自吡嗪环,噻吩环和苯基取代的噻唑环的杂环; 该衍生物作为治疗和预防高脂血症,糖尿病和白内障或作为抗肿瘤剂的药剂是有价值的。