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1. 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。

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

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。

4. 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.

5. 发明授权

US5336769A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5336769A
公开(公告)日：1994-08-09
申请号：US18209
申请日：1993-02-16
申请人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Shizuo Shiozaki
发明人： Fumio Suzuki , Junichi Shimada , Akio Ishii , Shizuo Shiozaki
IPC分类号： A61K31/52 , A61K31/522 , A61P25/28 , C07D473/04 , C07D473/06
CPC分类号： C07D473/04
摘要： A xanthine derivative of the formula (I): ##STR1## wherein R.sup.1 represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl;R.sup.2 represents --(CH.sub.2).sub.m --X, wherein m is 2 or 3, and X is ##STR2## wherein a is NH, O or S, b and d are the same or different and are CH or N, and R.sup.3 is lower alkyl, substituted or unsubstituted alicyclic alkyl, or substituted or unsubstituted phenyl, or ##STR3## wherein e, g and h are the same or different and are CH or N, and R.sup.3 is the same as defined above;Q represents substituted or unsubstituted alicyclic alkyl, ##STR4## wherein R.sup.4 and R.sup.5 are the same or different and are substituted or unsubstituted alicyclic alkyl, ##STR5## wherein Y is single bond or alkylene; and n is 0 or 1, ##STR6## wherein K-M is --CH.sub.2 --CH.sub.2 --or --CH.dbd.CH--, and Y is the same as defined above, or ##STR7## wherein Y is the same as defined above; or a pharmacologically acceptable salt thereof is disclosed.This derivative has anti-dementia activity.
摘要翻译：式（I）的黄嘌呤衍生物：其中R1表示取代或未取代的低级烷基，低级烯基，低级炔基，取代或未取代的脂环族烷基，取代或未取代的苯基或取代或未取代的苄基; R 2表示 - （CH 2）m X，其中m为2或3，并且X为H，其中a为NH，O或S，b和d相同或不同，为CH或N，且R 3为低级烷基，取代或未取代的脂环族烷基或取代或未取代的苯基，或其中e，g和h相同或不同，为CH或N，并且R 3与上述定义相同; Q表示取代或未取代的脂环族烷基，不同且为取代或未取代的脂环族烷基，其中Y为单键或亚烷基; 并且n为0或1，其中K-M为-CH 2 -CH 2 - 或-CH = CH-，Y为与上述定义相同的基团，或者其中Y与上述定义相同。或其药理学上可接受的盐。该衍生物具有抗痴呆活性。

6. 发明授权

US5587378A Therapeutic agent for Parkinson's disease 失效
标题翻译：帕金森病治疗剂
公开(公告)号：US5587378A
公开(公告)日：1996-12-24
申请号：US447885
申请日：1995-05-23
申请人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Joji Nakamura , Shizuo Shiozaki , Shunji Ichikawa , Akio Ishii , Hiromi Nonaka
发明人： Fumio Suzuki , Junichi Shimada , Nobuaki Koike , Joji Nakamura , Shizuo Shiozaki , Shunji Ichikawa , Akio Ishii , Hiromi Nonaka
IPC分类号： C07D473/06 , C07D473/08 , C07D473/12 , A61K31/52
CPC分类号： C07D473/08 , C07D473/06 , C07D473/12
摘要： Methods for the treatment of Parkinson's disease comprising administering to a patient an agent which contains, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 is cycloalkyl, --(CH.sub.2).sub.n --R.sup.5, wherein R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4, or ##STR2## wherein Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z is substituted or unsubstituted aryl, ##STR3## wherein R.sup.6 is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m is an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 are independently O or S.
摘要翻译：用于治疗帕金森病的方法包括向患者施用含有作为活性成分的黄嘌呤衍生物或其药学上可接受的盐的试剂。黄嘌呤衍生物由下式表示：其中R 1，R 2和R 3独立地是氢，低级烷基，低级链烯基或低级炔基; 并且R 4是环烷基， - （CH 2）n -R 5，其中R 5表示取代或未取代的芳基或取代或未取代的杂环基; n为0〜4的整数，或者，其中Y1和Y2独立地表示氢，卤素或低级烷基; Z是取代或未取代的芳基，其中R6是氢，羟基，低级烷基，低级烷氧基，卤素，硝基或氨基; m为1〜4的整数，或取代或未取代的杂环基; X1和X2独立地为O或S.

7. 发明授权

US5447933A Xanthine derivatives 失效
标题翻译：黄嘌呤衍生物
公开(公告)号：US5447933A
公开(公告)日：1995-09-05
申请号：US973959
申请日：1992-11-09
申请人： Fumio Suzuki , Junichi Shimada , Hiromasa Kato , Akio Ishii , Shizuo Shiozaki
发明人： Fumio Suzuki , Junichi Shimada , Hiromasa Kato , Akio Ishii , Shizuo Shiozaki
IPC分类号： C07D473/06 , A61K31/52
CPC分类号： C07D473/06
摘要： A novel xanthine derivative of the formula (I): ##STR1## wherein one of R.sup.1 and R.sup.2 represents substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, substituted or unsubstituted alicyclic alkyl, substituted or unsubstituted phenyl, or substituted or unsubstituted benzyl; and the other represents--(CH.sub.2).sub.m --Xwherein m is 2 or 3, and X is amino substituted phenyl.Q represents ##STR2## (wherein R.sup.3 and R.sup.4 are the same or different and are substituted or unsubstituted alicyclic alkyl), ##STR3## or a pharmacologically accetable salt thereof is disclosed. This derivative has anti-dementia activity.
摘要翻译：式（I）的新颖的黄嘌呤衍生物：取代或未取代的低级烷基，低级烯基，低级炔基，取代或未取代的脂环族烷基，取代或未取代的苯基或取代或未取代的苄基; 另一个表示 - （CH 2）m -X，其中m为2或3，X为氨基取代的苯基。 Q代表不同的并且是取代或未取代的脂环族烷基），IMA或其药理学上可接受的盐。该衍生物具有抗痴呆活性。

8. 发明授权

US5319085A Quinoline derivative having serotonin-3 receptor antagonizing activity 失效
标题翻译：具有5-羟色胺-3受体拮抗活性的喹啉衍生物
公开(公告)号：US5319085A
公开(公告)日：1994-06-07
申请号：US039131
申请日：1993-04-16
申请人： Fumio Suzuki , Hiroaki Hayashi , Yoshikazu Miwa , Takeshi Kuroda , Akio Ishii , Shunji Ichikawa , Ichiro Miki , Katsuichi Shuto
发明人： Fumio Suzuki , Hiroaki Hayashi , Yoshikazu Miwa , Takeshi Kuroda , Akio Ishii , Shunji Ichikawa , Ichiro Miki , Katsuichi Shuto
IPC分类号： C07D451/04 , C07D451/12 , C07D451/14 , C07D403/12 , C07D401/12
CPC分类号： C07D451/14 , C07D451/04 , C07D451/12
摘要： Quinoline derivatives represented by formula (I): ##STR1## wherein A-B-D represents --C(COO--Y).dbd.CH--C(OR).dbd. (wherein Y represents 8-methyl-8-azabicyclo[3.2.1]oct-3-yl group and R represents alkyl) or --C(OH).dbd.C(COX--Y)--CH.dbd. (wherein X represents --O-- or --NH--; and Y has the same meaning as described above), or a pharmaceutically acceptable salt thereof, possess potent 5HT.sub.3 antagonizing activity and are useful as antiemetic agents.
摘要翻译： PCT No.PCT / JP91 / 01758 Sec。 371日期：1993年04月16日 102（e）日期1993年4月16日PCT 1991年12月25日PCT公布。出版物WO92 / 12150 PCT （I）表示的喹啉衍生物：其中ABD表示-C（COO-Y）= CH-C（OR）=（其中Y表示8-甲基-8- 氮杂双环[3.2.1]辛-3-基，R代表烷基）或-C（OH）= C（COX-Y）-CH =（其中X表示-O-或-NH-; Y具有相同意义如上所述）或其药学上可接受的盐具有有效的5HT3拮抗活性，并且可用作止吐剂。

9. 发明授权

US4994463A Tricyclic thromboxane A.sub.2 antagonists 失效
标题翻译：三环血栓素A2拮抗剂
公开(公告)号：US4994463A
公开(公告)日：1991-02-19
申请号：US281545
申请日：1988-12-08
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
IPC分类号： C07D211/14 , C07D313/12 , C07D333/34 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10
CPC分类号： C07D405/06 , C07D211/14 , C07D313/12 , C07D333/34 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10
摘要： Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.

10. 发明授权

US5302602A Tricyclic thromboxane A.sub.2 antagonists 失效
标题翻译：三环血栓素A2拮抗剂
公开(公告)号：US5302602A
公开(公告)日：1994-04-12
申请号：US884208
申请日：1992-05-18
申请人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
发明人： Etsuo Oshima , Hiroyuki Obase , Akira Karasawa , Kazuhiro Kubo , Ichiro Miki , Akio Ishii , Hidee Ishii , Kenji Ohmori
IPC分类号： C07D211/14 , C07D313/12 , C07D333/34 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10 , A61K31/445 , C07D211/22
CPC分类号： C07D405/06 , C07D211/14 , C07D313/12 , C07D333/34 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D471/10
摘要： Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
摘要翻译：具有由式（I）表示的TXA2拮抗活性的新型三环化合物：具有对血栓素A2的有效拮抗作用，还具有抗过敏和/或抗组胺活性，并且预期对缺血性疾病具有预防和治疗作用脑血管疾病等

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