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1. 发明授权

US5342841A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5342841A
公开(公告)日：1994-08-30
申请号：US29069
申请日：1993-03-10
申请人： Fumio Suzuki , Junichi Shimada , Akira Karasawa , Hideaki Mizumoto , Hiroshi Kase , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Akira Karasawa , Hideaki Mizumoto , Hiroshi Kase , Hiromi Nonaka
IPC分类号： C07D473/06 , A61K31/52 , C07D473/02
CPC分类号： C07D473/06
摘要： A xanthine derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are substituted or unsubstituted alicyclic alkyl; m1 and m2 are the same or different and represent an integer of 0 to 2; and Q represents ##STR2## (in which R.sup.3 and R.sup.4 are the same or different and are substituted or unsubstituted alicyclic alkyl) or ##STR3## (in which n is 0 or 1, and Y is a single bond or alkylene); or a pharmaceutically acceptable salt thereof is disclosed.This derivative has diuretic activity and renal protecting activity.
摘要翻译：式（I）的黄嘌呤衍生物：其中R1和R2相同或不同，为取代或未取代的脂环族烷基; m1和m2相同或不同，表示0〜2的整数。和Q表示（其中R 3和R 4相同或不同，是取代或未取代的脂环族烷基）或（其中n为0或1，Y为单键或亚烷基）。或其药学上可接受的盐。该衍生物具有利尿活性和肾脏保护活性。

2. 发明授权

US5525607A Xanthine compounds 失效
标题翻译：黄嘌呤化合物
公开(公告)号：US5525607A
公开(公告)日：1996-06-11
申请号：US63684
申请日：1993-05-20
申请人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka , Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka , Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22 , A61K31/52 , C07D473/00
CPC分类号： C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22
摘要： Novel xanthine compounds represented by the following formula: ##STR1## wherein each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl;each of X.sup.1 and X.sup.2 independently represents oxygen or sulfur; and Q represents: ##STR2## The compounds are useful as a diuretic, a renal-protecting agent and bronchodilator.
摘要翻译：由下式表示的新型黄嘌呤化合物：其中R 1，R 2和R 3各自独立地表示氢或低级烷基; X1和X2各自独立地表示氧或硫; Q表示：该化合物可用作利尿剂，肾保护剂和支气管扩张剂。

3. 发明授权

US5068236A Xanthine derivatives 失效
标题翻译： XANTHINE DERIVATIVES
公开(公告)号：US5068236A
公开(公告)日：1991-11-26
申请号：US486831
申请日：1990-03-01
申请人： Fumio Suzuki , Junichi Shimada , Kazuhiro Kubo , Tetsuji Ohno , Akira Karasawa , Akio Ishii , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Kazuhiro Kubo , Tetsuji Ohno , Akira Karasawa , Akio Ishii , Hiromi Nonaka
IPC分类号： A61K31/52 , A61K31/522 , A61P7/10 , A61P9/08 , A61P9/12 , A61P13/02 , A61P15/00 , C07D473/04 , C07D473/06 , C07D473/08 , C07D473/10 , C07D473/12 , C07D473/20 , C07D473/22
CPC分类号： C07D473/04 , C07D473/06 , C07D473/22
摘要： Novel xanthine compounds represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof have a diuretic action, a renal-protecting action and a vasodilative action.The compounds are useful as a diuretic, a renal-protecting agent and an antihypertensive agent.

4. 发明授权

US5290782A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5290782A
公开(公告)日：1994-03-01
申请号：US839690
申请日：1992-02-24
申请人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Tetsuji Ohno , Akira Karasawa , Kazuhiro Kubo , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22 , C07D473/02 , A61K31/52
CPC分类号： C07D473/06 , C07D473/08 , C07D473/20 , C07D473/22
摘要： Novel xanthine compounds represented by the following formula: ##STR1## wherein each of X.sup.1 and X.sup.2 independently represents oxygen or sulfur; and Q represents; ##STR2## where ----- represents a single bond or a double bond; Y represents a single bond or alkylene, n represents 0 or 1, each of W.sup.1 and W.sup.2 independently represents hydrogen, lower alkyl or amino, Z represents --CH.sub.2 -, --O--, --S-- or --NH--; represents ##STR3## each of R.sup.1 and R.sup.2 independently represents hydrogen, lower alkyl, allyl or propargyl; and R.sup.3 represents hydrogen or lower alkyl, and when Q represents the groups other than ##STR4## each of R.sup.1, R.sup.2 and R.sup.3 independently represents hydrogen or lower alkyl;provided that when Q is ##STR5## then R.sup.1 R.sup.2 and R.sup.3 are notsimultaneously methyl; and pharmaceutically acceptable salts thereof have a diuretic effect, a renal-protecting effect and a bronchodilatory effect.
摘要翻译：由下式表示的新型黄嘌呤化合物：其中X1和X2各自独立地表示氧或硫; 和Q表示; 其中-----表示单键或双键; Y表示单键或亚烷基，n表示0或1，W1和W2各自独立地表示氢，低级烷基或氨基，Z表示-CH2 - ， - O - ， - S-或-NH-。 R1和R2各自表示氢，低级烷基，烯丙基或炔丙基; 且R 3表示氢或低级烷基，并且当Q表示除R1之外的基团时，R 1，R 2和R 3各自独立地表示氢或低级烷基; 条件是当Q为时，则R1 + L，R2和R3不同时为甲基; 及其药学上可接受的盐具有利尿作用，肾脏保护作用和支气管扩张作用。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明授权

US5173492A s-Triazolo(3,4-I)purine derivatives 失效
标题翻译：三唑并（3,4-I）嘌呤衍生物
公开(公告)号：US5173492A
公开(公告)日：1992-12-22
申请号：US752180
申请日：1991-08-23
申请人： Fumio Suzuki , Junichi Shimada , Kenji Ohmori , Haruhiko Manabe , Kazuihiro Kubo , Akira Karasawa , Tetsuji Ohno , Shizuo Shiozaki , Akio Ishii , Katsuichi Shuto
发明人： Fumio Suzuki , Junichi Shimada , Kenji Ohmori , Haruhiko Manabe , Kazuihiro Kubo , Akira Karasawa , Tetsuji Ohno , Shizuo Shiozaki , Akio Ishii , Katsuichi Shuto
IPC分类号： C07D471/14
CPC分类号： C07D471/14
摘要： There are disclosed s-triazolo[3,4-i]purine derivatives represented by formula: ##STR1## wherein Y-Z represents ##STR2## R.sub.4 represents hydrogen, alkyl, substituted or unsubstituted aromatic heterocyclic group or substituted or unsubstituted aryl; and X.sup.2 represents oxygen, sulfur or NH; each of R.sup.1 and R.sup.2 independently represents hydrogen, alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; R.sup.3 represents alkyl, cycloalkyl, aralkyl or substituted or unsubstituted aryl; X.sup.1 represents oxygen or sulfur; and represents a single bond or a double bond or pharmaceutically acceptable salts thereof.
摘要翻译：公开了由下式表示的三唑并[3,4-i]嘌呤衍生物：其中Y-Z表示R 4表示氢，烷基，取代或未取代的芳族杂环基或取代或未取代的芳基; X2表示氧，硫或NH; R 1和R 2各自独立地表示氢，烷基，环烷基，芳烷基或取代或未取代的芳基; R3表示烷基，环烷基，芳烷基或取代或未取代的芳基; X1表示氧或硫; 并且表示单键或双键或其药学上可接受的盐。

10. 发明授权

US5270316A Condensed purine derivatives 失效
标题翻译：凝血嘌呤衍生物
公开(公告)号：US5270316A
公开(公告)日：1993-12-14
申请号：US599758
申请日：1990-10-19
申请人： Fumio Suzuki , Junichi Shimada , Takeshi Kuroda , Kazuhiro Kubo , Akira Karasawa , Tetsuji Ohno , Kenji Ohmori
发明人： Fumio Suzuki , Junichi Shimada , Takeshi Kuroda , Kazuhiro Kubo , Akira Karasawa , Tetsuji Ohno , Kenji Ohmori
IPC分类号： A61K31/00 , A61K31/495 , A61K31/505 , A61K31/519 , A61K31/529 , A61P7/00 , A61P7/10 , A61P9/00 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/00 , A61P13/02 , A61P13/12 , A61P15/00 , C07D471/14 , C07D487/14 , A61K31/52
CPC分类号： C07D471/14 , C07D487/14
摘要： There are disclosed condensed purine derivatives represented by formula; ##STR1## in which R.sup.3 represents hydrogen, lower alkyl or benzyl; each of X.sup.1 and X.sup.2 independently represents hydrogen, lower alkyl, aralkyl or phenyl; and n is an integer of 0 or 1; R.sup.1 represents hydrogen, lower alkyl, alicyclic alkyl, noradamantan-3-yl, dicyclopropylmethyl or styryl; and R.sup.2 represents hydrogen, lower alkyl or alicyclic alkyl; or a pharmaceutically acceptable salt thereof. The derivatives and pharmaceutically acceptable salts are useful as diuretics, renal protecting agents, antiallergic agents and hypotensives.

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