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1. 发明授权

US5624926A Piperidinyl-dioxoquinazolines as adenosine reuptake inhibitors 失效
标题翻译：哌啶基 - 二氧喹唑啉作为腺苷再摄取抑制剂
公开(公告)号：US5624926A
公开(公告)日：1997-04-29
申请号：US318876
申请日：1994-10-17
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , A61K31/50 , A61K31/505
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译： PCT No.PCT / JP94 / 00229 Sec。 371日期：1994年10月17日 102（e）日期1994年10月17日PCT 1994年2月16日PCT PCT。 WO94 / 19342 PCT公开号日期：1994年9月1日本发明涉及一种腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物式（I）：其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，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 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

2. 发明授权

US5648353A Quinazolines and phthalazines having adenosine uptake inhibitor activity 失效
标题翻译：喹唑啉和具有腺苷摄取抑制剂活性的酞嗪酮
公开(公告)号：US5648353A
公开(公告)日：1997-07-15
申请号：US446235
申请日：1995-05-22
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , C07D401/04 , A61K31/445 , A61K31/50 , A61K31/505
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含由式（I）表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物：（I）其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，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 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

3. 发明授权

US5605900A Benzotriazines having adenosine uptake inhibitor activity 失效
标题翻译：具有腺苷摄取抑制剂活性的苯并三嗪
公开(公告)号：US5605900A
公开(公告)日：1997-02-25
申请号：US430227
申请日：1995-04-28
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , C07D401/04 , A61K31/445 , A61K31/50 , A61K31/53
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C-R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含由式（I）表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物：（I）其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，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 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

4. 发明授权

US5658917A Isoquinolines having adenosine uptake inhibitor activity 失效
标题翻译：具有腺苷摄取抑制剂活性的异喹啉
公开(公告)号：US5658917A
公开(公告)日：1997-08-19
申请号：US430234
申请日：1995-04-28
申请人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
发明人： Shigeki Fujiwara , Daisuke Machii , Haruki Takai , Hiromi Nonaka , Hiroshi Kase , Kozo Yao , Michiyo Kawakage , Hideaki Kusaka , Akira Karasawa
IPC分类号： C07D401/14 , C07D491/04 , A61K31/445 , A61K31/50 , A61K31/505
CPC分类号： C07D401/14 , C07D491/04
摘要： The present invention relates to an adenosine uptake inhibitor and an agent for the myocardium protection or the prevention or treatment of inflammatory edema, comprising a 1,2,3,4-tetrahydro-2,4-dioxoquinazoline derivative represented by formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, alkenyl, or substituted or unsubstituted aralkyl; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 independently represent hydrogen, halogen, amino, mono- or di(lower alkyl)amino, lower alkanoylamino, nitro, cyano, substituted or unsubstituted lower alkyl, hydroxy, lower alkoxy, lower alkylthio, carboxy, lower alkoxycarbonyl, lower alkanoyl, aralkyloxy, or lower alkanoyloxy; R.sup.6, R.sup.7, R.sup.8, and R.sup.9 independently represent hydrogen, hydroxy, substituted or unsubstituted lower alkoxy, or aralkyloxy, or any adjoining two of them are combined to form methylenedioxy; R.sup.10 represents hydrogen or lower alkyl; and Y and Z independently represent N or C--R.sup.11 (wherein R.sup.11 represents hydrogen, substituted or unsubstituted lower alkyl, or halogen),or a pharmaceutically acceptable salt thereof as an active ingredient.
摘要翻译：本发明涉及腺苷摄取抑制剂和用于心肌保护或预防或治疗炎性水肿的药剂，其包含由式（I）表示的1,2,3,4-四氢-2,4-二氧代喹唑啉衍生物：（I）其中R 1表示氢，取代或未取代的低级烷基，烯基或取代或未取代的芳烷基; R2，R3，R4和R5独立地表示氢，卤素，氨基，一或二（低级烷基）氨基，低级烷酰基氨基，硝基，氰基，取代或未取代的低级烷基，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 6，R 7，R 8和R 9独立地表示氢，羟基，取代或未取代的低级烷氧基或芳烷氧基，或者它们中的任何相邻的两个被结合形成亚甲二氧基; R 10表示氢或低级烷基; 并且Y和Z独立地表示作为活性成分的N或C-R11（其中R11表示氢，取代或未取代的低级烷基或卤素）或其药学上可接受的盐。

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