公开(公告)号：EP0638567A1

公开(公告)日：1995-02-15

申请号：EP94907052.8

申请日：1994-02-16

申请人： KYOWA HAKKO KOGYO KABUSHIKI KAISHA

发明人： FUJIWARA, Shigeki ,  MACHII, Daisuke ,  TAKAI, Haruki ,  NONAKA, Hiromi ,  KASE, Hiroshi ,  YAO, Kozo ,  KAWAKAGE, Michiyo ,  KUSAKA, Hideaki ,  KARASAWA, Akira

IPC分类号： C07D401/14 ,  C07D491/056 ,  A61K31/505

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 R¹ represents hydrogen, (un)substituted lower alkyl, alkenyl or (un)substituted aralkyl; R², R³, R⁴ and R⁵ 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; R⁶, R⁷, R⁸ and R⁹ 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; R¹⁰ 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： 一种腺苷结合抑制剂和保护心肌的药物或预防或治疗炎性水肿的药物，每种药物含有作为活性成分的由通式（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代表氢，（未）取代的低级烷基，烯基或（未）取代的芳烷基; （低级烷基）氨基，低级烷酰基氨基，硝基，氰基，（未）取代的低级烷基，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 8，R 8和R 8各自独立地代表氢，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结合在一起表示亚甲二氧基; R 10代表氢或低级烷基; Y和Z各自独立地代表N或C-R“，其中R”代表氢，（未）取代的低级烷基或卤素。

公开(公告)号：EP0919233A1

公开(公告)日：1999-06-02

申请号：EP97904570.5

申请日：1997-02-19

申请人： KYOWA HAKKO KOGYO KABUSHIKI KAISHA

发明人： FUJIWARA, Shigeki ,  OKAMURA, Yuko ,  TAKAI, Haruki ,  NONAKA, Hiromi ,  MORIYAMA, Takahiro ,  YAO, Kozo ,  KARASAWA, Akira

IPC分类号： A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

CPC分类号： C07D401/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55

摘要： Disclosed is a therapeutic agent for renal disease comprising a quinazoline derivative represented by formula (I):
(wherein R 1 represents hydrogen, lower alkyl, alkenyl, or aralkyl; R 2 , R 3 , R 4 , and R 5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyl, or the like; R 6 , R 7 , R 8 , and R 9 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, aralkyloxy, or lower alkanoyloxy, or the like, or any adjoining two of them are combined to form methylenedioxy or the like; R 10 represents hydrogen, lower alkyl, or the like; R 11 and R 12 are the same or different and represent hydrogen, lower alkyl, cycloalkyl, phenyl, or aralkyl, or R 11 and R 12 are combined together to form a heterocyclic group containing nitrogen atom; and n represents 0, 1 or 2) and pharmaceutically acceptable salts thereof as an active ingredient.
This therapeutic agent is useful for the prevention or treatment of renal diseases such as nephritis and diabetic nephropathy.

摘要翻译： 公开了一种肾病治疗剂，其包含由式（I）表示的喹唑啉衍生物：其中R 1表示氢，低级烷基，链烯基或芳烷基; R 2，R 3，R R 5和R 5相同或不同，表示氢，低级烷基，低级烷氧基，低级烷酰基等; R 6，R 7，R 8和R 9 >相同或不同，表示氢，低级烷基，低级烷氧基，芳烷氧基或低级烷酰氧基等，或者其中任意相邻的两个被结合形成亚甲二氧基等; R 10表示氢，低级烷基 等等; R 11和R 12相同或不同，代表氢，低级烷基，环烷基，苯基或芳烷基，或R 11和R 12组合在一起形成杂环基 含有氮原子的基团; n表示0,1或2）及其药学上可接受的盐作为活性成分。 该治疗剂可用于预防或治疗肾脏疾病如肾炎和糖尿病肾病。