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1. 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。

2. 发明申请

WO1996026940A1 IMIDAZOQUINAZOLINE DERIVATIVES 审中-公开
标题翻译：咪唑啉酮衍生物
公开(公告)号：WO1996026940A1
公开(公告)日：1996-09-06
申请号：PCT/JP1996000497
申请日：1996-03-01
申请人： KYOWA HAKKO KOGYO CO., LTD. , ONODA, Yasuo , SASAKI, Shin-ichi , MACHII, Daisuke , TAKAI, Haruki , OHNO, Tetsuji , YAMADA, Koji , ICHIMURA, Michio , KASE, Hiroshi
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Imidazoquinazoline derivatives represented by general formula (I) or pharmacologically acceptable salts thereof, wherein R represents hydrogen, optionally substituted lower alkyl, etc.; R and R are the same or different and each represents hydrogen, optionally substituted lower alkyl, optionally substituted aralkyl, optionally substituted aryl, etc., or R and R together form an optionally substituted nitrogenous heterocycle; R represents hydrogen or optionally substituted lower alkyl; X represents O or S; Y represents a single bond or O; and n is 0, 1, 2 or 3.
摘要翻译：由通式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，其中R 1表示氢，任选取代的低级烷基等; R 2和R 3相同或不同，各自表示氢，任选取代的低级烷基，任选取代的芳烷基，任选取代的芳基等，或R 2和R 3一起形成任选取代的含氮杂环 R 4表示氢或任选取代的低级烷基; X表示O或S; Y表示单键或O; n为0,1,2或3。

3. 发明申请

WO1995006648A1 IMIDAZOQUINAZOLINE DERIVATIVE 审中-公开
标题翻译：咪唑啉酮衍生物
公开(公告)号：WO1995006648A1
公开(公告)日：1995-03-09
申请号：PCT/JP1994001456
申请日：1994-09-02
申请人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , MATSUNO, Kenji , KINOSHITA, Iwao , NOMOTO, Yuji , TAKAI, Haruki , OHNO, Tetuji , NAGASHIMA, Ken , ISHIKAWA, Tomoko , YAMADA, Koji , ICHIMURA, Michio , KASE, Kiroshi
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： An imidazoquinazoline derivative represented by formula (I) or a pharmacologically acceptable salt thereof, wherein R andR may be the same or different from each other and each represents hydrogen, lower alkyl, lower alkenyl, aryl, etc.; R represents hydrogen, lower alkyl, cycloalkyl, lower alkenyl, aryl, etc.; and X represents O or S. This compound has a potent and selective cCMP-specific PDE inhibitor activity and is useful for treating or mitigating cardiovascular diseases such as thrombosis, angina pectoris, hypertension and arteriosclerosis, asthma, and so forth.
摘要翻译：由式（I）表示的咪唑并喹唑啉衍生物或其药理学上可接受的盐，其中R 1和R 2可以相同或不同，各自代表氢，低级烷基，低级烯基，芳基等; R 3表示氢，低级烷基，环烷基，低级烯基，芳基等; X表示O或S.该化合物具有有效和选择性的cCMP特异性PDE抑制剂活性，可用于治疗或缓解心血管疾病如血栓形成，心绞痛，高血压和动脉硬化，哮喘等。

4. 发明申请

WO1995019343A1 INDOLE DERIVATIVE 审中-公开
公开(公告)号：WO1995019343A1
公开(公告)日：1995-07-20
申请号：PCT/JP1995000019
申请日：1995-01-11
申请人： KYOWA HAKKO KOGYO CO., LTD. , MACHII, Daisuke , TAKAI, Haruki , KOSAKA, Nobuo , SEO, Hisakatsu , SUGIYAMA, Tomomi , NAKAMURA, Joji , ISHIDA, Hiroyuki , GOMI, Katsushige , SATO, Soichiro , UCHII, Masako
发明人： KYOWA HAKKO KOGYO CO., LTD.
IPC分类号： C07D209/42
CPC分类号： C07D209/42
摘要： An indole derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, wherein R and R may be the same or different and each represents hydrogen, lower alkyl, -(CH2)n-OR (R representing hydrogen or lower alkyl, and n representing an integer of 1 to 6), or -(CH2)m-NR R (wherein R and R may be the same or different and each represents hydrogen or lower alkyl, or alternatively R and R are combined to represent, together with the nitrogen atom to which they are bonded, an (un)substituted heteroalicyclic group, and m represents an integer of 2 to 6); R represents hydrogen, lower alkyl or -(CH2)p-NR R (wherein R and R may be the same or different and each represents hydrogen or lower alkyl, or alternatively R and R are combined to represent, together with the nitrogen atom to which they are bonded, an (un)substituted heteroalicyclic group, and p represents an integer of 2 to 6); and R and R may be the same or different and each represents hydrogen, lower alkyl, cycloalkyl, (un)substituted aryl or (un)substituted heterocycle, or alternatively R and R are combined to represent, together with the nitrogen atom to which they are bonded, an (un)substituted heteroalicyclic group.
摘要翻译：由通式（I）表示的吲哚衍生物或其药理学上可接受的盐，其中R 1和R 2可以相同或不同，各自表示氢，低级烷基， - （CH 2）n -OR 6 （R 6表示氢或低级烷基，n表示1〜6的整数）或 - （CH 2）m -NR 7 R 8（其中R 7和R 8可以相同或不同，各自表示氢或低级烷基，或者R 7和R 8与它们所键合的氮原子一起代表与（un）取代的杂脂环基，m 表示2〜6的整数）; R 3表示氢，低级烷基或 - （CH 2）p -NR NR 9 R 10（其中R 9和R 10可以相同或不同，各自表示氢或低级烷基，或或者R 9和R 10与它们所键合的氮原子一起代表（取代的）杂脂环基，p表示2〜6的整数）。 R 4和R 5可以相同或不同，各自表示氢，低级烷基，环烷基，（未）取代的芳基或（未）取代的杂环，或者R 4和R 5分别为与它们所键合的氮原子一起表示（（un）取代的杂脂环基。

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