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1. 发明申请

WO1995031460A1 PROCESS FOR PRODUCING XANTHINE DERIVATIVE 审中-公开
标题翻译：生产XANTHINE DERIVATIVE的方法
公开(公告)号：WO1995031460A1
公开(公告)日：1995-11-23
申请号：PCT/JP1995000929
申请日：1995-05-16
申请人： KYOWA HAKKO KOGYO CO., LTD. , SHIMADA, Junichi , EGUCHI, Tamotsu , MOCHIDA, Kenichi , HORIGUCHI, Akira , YASUZAWA, Tohru , KUSAKA, Hideaki , NONAKA, Hiromi , SUZUKI, Fumio
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D473/04
CPC分类号： C07D473/04 , C07D473/06 , C12P17/18
摘要： A process for converting a xanthine derivative represented by general formula (I) [compound (I)], (wherein R and R are the same or different from each other and each represents hydrogen or hydroxy-, oxo- or unsubstituted lower alkyl) into another xanthine derivative represented by general formula (II) [compound (II)], (wherein R and R are the same or different from each other and each represents hydrogen or hydroxy-, oxo- or unsubstituted lower alkyl; R and R are the same or different from each other and each represents hydrogen, hydroxy or oxo, provided when both of R and R are hydrogen, at least one of R and R is hydroxy- or oxo-substituted lower alkyl; and X and Y represent both hydrogen or they are combined together to represent a single bond) in the presence of an enzyme source which catalyzes the hydroxylation or carbonylation of compound (I) into compound (II).
摘要翻译：用于转化由通式（I）[化合物（I）]表示的黄嘌呤衍生物的方法，其中R 1和R 2彼此相同或不同，并且各自表示氢或羟基，或未取代的低级烷基）转化成由通式（II）表示的另一种黄嘌呤衍生物[化合物（II）]，（其中R 3和R 4彼此相同或不同，各自表示氢或羟基 - 羟基或未取代的低级烷基; R 5和R 6彼此相同或不同，并且各自表示氢，羟基或氧代，当R 5和R 6均为氢时，其为 R 3和R 4中的至少一个是羟基或氧代取代的低级烷基;并且X和Y代表氢或它们组合在一起代表单键）在酶源的存在下催化化合物（I）羟化或羰基化成化合物（II）。

2. 发明申请

WO1994019342A1 ADENOSINE INCORPORATION INHIBITOR 审中-公开
标题翻译：腺苷合成抑制剂
公开(公告)号：WO1994019342A1
公开(公告)日：1994-09-01
申请号：PCT/JP1994000229
申请日：1994-02-16
申请人： KYOWA HAKKO KOGYO CO., LTD. , FUJIWARA, Shigeki , MACHII, Daisuke , TAKAI, Haruki , NONAKA, Hiromi , KASE, Hiroshi , YAO, Kozo , KAWAKAGE, Michiyo , KUSAKA, Hideaki , KARASAWA, Akira
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D491/04
摘要： An adenosine incorporation inhibitor and a drug for protecting cardiac muscles or preventing or treating inflammatory edema, each containing as the active ingredient a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R represents hydrogen, (un)substituted lower alkyl, alkenyl or (un)substituted aralkyl; R , R , R and R represent each independently hydrogen, halogen, amino, mono- or di(lower alkyl) amino, lower alkanoyl amino, nitro, cyano, (un)substituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy or lower alkanoyloxy; R , R , R and R represent each independently hydrogen, hydroxy, (un)substituted lower alkoxy or aralkyloxy, or alternatively the two adjacent groups among them may be combined together to represent methylenedioxy; R represents hydrogen or lower alkyl; and Y and Z represent each independently N or C-R'', wherein R'' represents hydrogen, (un)substituted lower alkyl or halogen.
摘要翻译：一种腺苷并入抑制剂和用于保护心肌或预防或治疗炎症性水肿的药物，每种含有作为活性成分的通式（I）表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物或其中R 1表示氢，（取代的）取代的低级烷基，烯基或（未）取代的芳烷基; R 2，R 3，R 4和R 5各自独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰氨基，硝基，氰基，（取代）低级烷基，羟基，低级烷氧基，低级烷硫基，羧基，低级烷氧基羰基，低级烷酰基，芳烷氧基或低级烷酰氧基; R 6，R 7，R 8和R 9各自独立地表示氢，羟基，（未）取代的低级烷氧基或芳烷氧基，或者它们中的两个相邻基团可以组合在一起代表亚甲二氧基 ; R 10代表氢或低级烷基; 并且Y和Z各自独立地表示N或C-R“，其中R”表示氢，（un）取代的低级烷基或卤素。

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