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1. 发明授权

US5418230A Benzylidene derivatives 失效
标题翻译：亚苄基衍生物
公开(公告)号：US5418230A
公开(公告)日：1995-05-23
申请号：US142146
申请日：1993-10-28
申请人： Saichi Matsumoto , Tatsuo Tsuri , Masanao Inagaki , Hirokuni Jyoyama
发明人： Saichi Matsumoto , Tatsuo Tsuri , Masanao Inagaki , Hirokuni Jyoyama
IPC分类号： C07D275/02 , C07D291/06 , C07D417/10 , A61K31/54
CPC分类号： C07D275/02 , C07D291/06 , C07D417/10
摘要： Benzylidene derivatives having anti-inflammatory activities, are shown by the following formula I: ##STR1## wherein A is -CH.sub.2 - or -CH.sub.2 CH.sub.2 -; B is a bond or -CH.sub.2 -, -CHOH-, -CO-, -O-, or A and B may taken together form -CH=CH-; D is >N- or >CH-; R.sup.1 and R.sup.2 each independently is hydrogen, lower alkyl or lower alkoxy; R.sup.3 is hydrogen, lower alkyl, cycloalkyl, lower alkoxy, arylalkyloxy, heteroarylalkyloxy, lower alkylcarbonyl, arylcarbonyl, substituted or unsubstituted carbamoyl, or a group of the formula:-(CH.sub.2).sub.n -R.sup.4wherein R.sup.4 is hydrogen, hydroxy, substituted or unsubstituted amino, aryl, heteroaryl, hydroxycarbonyl or lower alkyloxycarbonyl; n is an integer of 0-3.
摘要翻译：具有抗炎活性的亚苄基衍生物由下式I表示：键或-CH 2 - ， - CHOH - ， - CO - ， - O-或A和B可以一起形成-CH = CH-; D是> N-或> CH-; R 1和R 2各自独立地为氢，低级烷基或低级烷氧基; R 3是氢，低级烷基，环烷基，低级烷氧基，芳基烷氧基，杂芳基烷氧基，低级烷基羰基，芳基羰基，取代或未取代的氨基甲酰基或下列基团： - （CH 2）n -R 4其中R 4是氢，羟基，取代或未取代的氨基，芳基，杂芳基，羟基羰基或低级烷氧基羰基; n为0-3的整数。

2. 发明授权

US5463052A Method for producing benzylidene derivatives 失效
标题翻译：亚苄基衍生物的制备方法
公开(公告)号：US5463052A
公开(公告)日：1995-10-31
申请号：US246494
申请日：1994-05-20
申请人： Nobuhiro Haga , Masanao Inagaki , Saichi Matsumoto , Susumu Kamata
发明人： Nobuhiro Haga , Masanao Inagaki , Saichi Matsumoto , Susumu Kamata
IPC分类号： C07D207/26 , C07D265/02 , C07D275/02 , C07D279/02 , C07D281/02 , C07D281/18 , C07D291/00 , C07D291/04 , C07D291/06
CPC分类号： C07D275/02 , C07D265/02 , C07D291/06 , Y02P20/55
摘要： A selective and high-yield method is described for producing stereoisomeric benzylidene derivatives of the formula III: ##STR1## wherein R.sup.1 and R.sup.2 each independently is lower alkyl, lower alkoxy or halogen; Y is SO.sub.2, SO or CO; --A-- is optionally substituted lower alkylene; --B-- is --CH.sub.2 -- or --O--; or --A-- and --B-- taken together may form optionally substituted phenylene or optionally substituted lower alkenylene; and R is hydrogen, optionally substituted lower alkyl, cycloalkyl, lower alkoxy, hydroxy, optionally substituted aryl, optionally substituted arylalkyl; optionally substituted arylalkyloxy, heterocyclic ring or N-protecting groups, which comprises reacting a compound of the formula I: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and X is lower alkoxy or halogen with a compound of the formula II: ##STR3## wherein Y, --A--, --B-- and R are as defined above in the presence of a base.
摘要翻译：描述了用于制备式III的立体异构亚苄基衍生物的选择性和高产率方法：其中R 1和R 2各自独立地为低级烷基，低级烷氧基或卤素; Y是SO2，SO或CO; -A-是任选取代的低级亚烷基; -B-是-CH 2 - 或-O-; 或-A-和-B-可以一起形成任选取代的亚苯基或任选取代的低级亚烯基; 并且R是氢，任选取代的低级烷基，环烷基，低级烷氧基，羟基，任选取代的芳基，任选取代的芳基烷基; 任选取代的芳基烷氧基，杂环或N-保护基，其包括使式I化合物：其中R 1和R 2如上所定义，X是低级烷氧基或卤素与式II化合物反应：图像II其中Y，-A-，-B-和R如上所定义，在碱的存在下。

3. 发明授权

US5319100A 3-benzylidene-1-carbamoyl-2-pyrrolidone analogues 失效
标题翻译： 3-亚苄基-1-氨基甲酰基-2-吡咯烷酮类似物
公开(公告)号：US5319100A
公开(公告)日：1994-06-07
申请号：US33342
申请日：1993-03-18
申请人： Susumu Kamata , Takeshi Shiota , Nobuhiro Haga , Toshihiko Okada , Hirokuni Jyoyama , Saichi Matsumoto
发明人： Susumu Kamata , Takeshi Shiota , Nobuhiro Haga , Toshihiko Okada , Hirokuni Jyoyama , Saichi Matsumoto
IPC分类号： C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D275/02 , C07D275/03 , C07D277/34 , C07D207/12
CPC分类号： C07D275/03 , C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D277/34
摘要： The present invention relates to novel 3-benzylidene-1-carbamoyl-2-pyrroridone analogues having advantage anti-inflammatory activities, which is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is independently hydrogen, alkyl, alkoxy, or halogen; R.sup.3 is hydrogen or acyl; R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, cyano, or halogen; R.sup.5 and R.sup.6 each is independently hydrogen, alkyl, aryl, aralkyl, heterocyclic group, substituted or unsubstituted amino, or OR.sup.7 wherein R.sup.7 is hydrogen, alkyl, aryl, acyl, or aralkyl, or taken together with the adjacent nitrogen atom may form heterocyclic group which may contain N, O, and/or S, and X and Y each is independently O, S, substituted or unsubstituted imino, or substituted or unsubstituted methylene. In more detail, the present invention provides an anti-inflammatory agent which is useful for the treatment of chronic inflammation and has little side effect, e.g., stomach disease.
摘要翻译：本发明涉及具有抗炎活性优势的新型3-亚苄基-1-氨基甲酰基-2-吡咯酮类似物，其由下式表示：其中R 1和R 2各自独立地为氢，烷基，烷氧基或卤素 ; R3是氢或酰基; R4是氢，烷基，羟基，烷氧基，氰基或卤素; R 5和R 6各自独立地为氢，烷基，芳基，芳烷基，杂环基，取代或未取代的氨基或OR 7，其中R 7为氢，烷基，芳基，酰基或芳烷基，或与相邻氮原子一起形成杂环基其可以含有N，O和/或S，X和Y各自独立地为O，S，取代或未取代的亚氨基，或取代或未取代的亚甲基。更详细地，本发明提供一种抗炎剂，其可用于治疗慢性炎症并且具有很小的副作用，例如胃病。

4. 发明授权

US06743923B2 Antirheumatic agent 失效
标题翻译：抗风湿剂
公开(公告)号：US06743923B2
公开(公告)日：2004-06-01
申请号：US10309256
申请日：2002-12-04
申请人： Saichi Matsumoto , Hirokuni Jyoyama , Shinji Kakudo , Kohji Hanasaki , Kenzo Koizumi , Tsuneaki Sakata , Ryuji Suzuki
发明人： Saichi Matsumoto , Hirokuni Jyoyama , Shinji Kakudo , Kohji Hanasaki , Kenzo Koizumi , Tsuneaki Sakata , Ryuji Suzuki
IPC分类号： C07D27502
CPC分类号： C07D275/02 , C07D417/06
摘要： A novel antirheumatic agent comprising as an active ingredient a compound of formula I: or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：一种新颖的抗风湿剂，其包含式I化合物作为活性成分：或其药学上可接受的盐或水合物。

5. 发明授权

US5091569A Di-tert-butyl(hydroxy)phenylthio substituted hydroxamic acid derivatives 失效
标题翻译：二叔丁基（羟基）苯基取代的羟基酸衍生物
公开(公告)号：US5091569A
公开(公告)日：1992-02-25
申请号：US540625
申请日：1990-06-19
申请人： Saichi Matsumoto , Takuji Mizui , Masami Doteuchi
发明人： Saichi Matsumoto , Takuji Mizui , Masami Doteuchi
IPC分类号： A61K31/165 , A61K31/095 , A61P1/04 , A61P3/06 , A61P3/08 , A61P9/00 , A61P9/10 , A61P11/00 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C319/20 , C07C323/47 , C07C323/60
CPC分类号： C07C323/47 , C07C323/60
摘要： (Di-tert-butylhydroxyphenyl)thio substituted hydroxamic acid derivatives of the formula: ##STR1## wherein X is straight or branched C.sub.1 to C.sub.15 alkylene which may be attached to Y through phenylene, provided that X is not n-butylmethylene; Y is CO--N(OH) or N(OH)--CO; and R is hydrogen or straight or branched C.sub.1 to C.sub.9 alkyl, C.sub.3 to C.sub.9 cycloalkyl, aryl, or aralkyl, provided that R is not hydrogen when Y--R is N(OH)--CO--R; or a pharmaceutically acceptable salt thereof; useful in treating arteriosclerosis, ulcer, inflammation, allergy, or the like.

6. 发明授权

US5319099A 3-benzylidene-1-carbamoyl-2-pyrrolidone compounds useful as antiinflammatory agents 失效
标题翻译：可用作抗炎剂的3-亚苄基-1-氨基甲酰基-2-吡咯烷酮化合物
公开(公告)号：US5319099A
公开(公告)日：1994-06-07
申请号：US862761
申请日：1992-06-24
申请人： Susumu Kamata , Takeshi Shiota , Nobuhiro Haga , Toshihiko Okada , Hirokuni Jyoyama , Saichi Matsumoto
发明人： Susumu Kamata , Takeshi Shiota , Nobuhiro Haga , Toshihiko Okada , Hirokuni Jyoyama , Saichi Matsumoto
IPC分类号： C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D275/02 , C07D275/03 , C07D277/34 , C07D207/24 , A61K31/40 , A61K31/41 , C07D231/02 , C07D263/02 , C07D277/02
CPC分类号： C07D275/03 , C07D207/36 , C07D207/38 , C07D261/12 , C07D263/40 , C07D263/46 , C07D277/34
摘要： The present invention relates to novel 3-benzylidene-1-carbamoyl-2-pyrroridone analogues having advantage anti-inflammatory activities, which is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is independently hydrogen, alkyl, alkoxy, or halogen; R.sup.3 is hydrogen or acyl; R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, cyano, or halogen; R.sup.5 and R.sup.6 each is independently hydrogen, alkyl, aryl, aralkyl, heterocyclic group, substituted or unsubstituted amino, or OR.sup.7 wherein R.sup.7 is hydrogen, alkyl, aryl, acyl, or aralkyl, or taken together with the adjacent nitrogen atom may form heterocyclic group which may contain N, O, and/or S, and X and Y each is independently O, S, substituted or unsubstituted imino, or substituted or unsubstituted methylene. In more detail, the present invention provides an anti-inflammatory agent which is useful for the treatment of chronic inflammation and has little side effect, e.g., stomach disease.
摘要翻译： PCT No.PCT / JP92 / 00020 Sec。 371日期：1992年6月24日 102（e）日期1992年6月24日PCT提交1992年1月14日PCT公布。公开号WO92 / 12966 本发明涉及具有抗炎活性优势的新型3-亚苄基-1-氨基甲酰-2-吡咯烷酮类似物，其由下式表示：其中R 1和R 2各自独立地为氢烷基，烷氧基或卤素; R3是氢或酰基; R4是氢，烷基，羟基，烷氧基，氰基或卤素; R 5和R 6各自独立地为氢，烷基，芳基，芳烷基，杂环基，取代或未取代的氨基或OR 7，其中R 7为氢，烷基，芳基，酰基或芳烷基，或与相邻氮原子一起形成杂环基其可以含有N，O和/或S，X和Y各自独立地为O，S，取代或未取代的亚氨基，或取代或未取代的亚甲基。更详细地，本发明提供一种抗炎剂，其可用于治疗慢性炎症并且具有很小的副作用，例如胃病。

7. 发明授权

US5084214A Phenolic thioethers, and their production and use 失效
标题翻译：酚醛树脂及其生产和使用
公开(公告)号：US5084214A
公开(公告)日：1992-01-28
申请号：US359718
申请日：1989-05-31
申请人： Toru Kita , Shuh Narumiya , Masayuki Narisada , Fumihiko Watanabe , Saichi Matsumoto , Masami Doteuchi
发明人： Toru Kita , Shuh Narumiya , Masayuki Narisada , Fumihiko Watanabe , Saichi Matsumoto , Masami Doteuchi
IPC分类号： A61K31/19 , A61K31/22 , A61K31/235 , A61P1/04 , A61P3/06 , A61P9/10 , A61P9/14 , A61P29/00 , A61P37/08 , C07C323/52 , C07C323/54 , C07C323/56
CPC分类号： C07C323/52 , Y02P20/55 , Y10S514/824
摘要： Phenolic thioethers of the formula: ##STR1## wherein R is a hydrogen atom or a protective group for carboxyl, X is a straight or branched C.sub.4 -C.sub.15 alkylene group, a straight or branched C.sub.1 -C.sub.15 alkylene group having a phenylene group or a straight or branched C.sub.2 -C.sub.15 alkenylene group, and their salts, which inhibit the denaturation of low density lipoproteins (LDL) and the incorporation of LDL by macrophages and are useful as anti-arteriosclerosis agents.

8. 发明授权

US4900749A Isoprenoidamine compounds useful as antiulcer agents 失效
标题翻译：异戊二烯类化合物可用作抗溃疡剂
公开(公告)号：US4900749A
公开(公告)日：1990-02-13
申请号：US837192
申请日：1986-03-10
申请人： Saichi Matsumoto , Masami Doteuchi , Takuji Mizui , Kentaro Hirai
发明人： Saichi Matsumoto , Masami Doteuchi , Takuji Mizui , Kentaro Hirai
IPC分类号： A61K31/16 , A61K31/165 , A61K31/17 , A61K31/22 , A61K31/335 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/495 , A61K45/08 , A61P1/04 , C07C67/00 , C07C231/00 , C07C233/05 , C07C233/65 , C07C275/20 , C07C275/24 , C07C275/28 , C07C275/30 , C07C313/00 , C07C317/44 , C07C323/62 , C07C325/00 , C07C327/40 , C07C327/46 , C07C327/50 , C07C331/22 , C07D207/34 , C07D209/18 , C07D209/28 , C07D209/30 , C07D209/42 , C07D213/40 , C07D213/54 , C07D213/56 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/83 , C07D233/54 , C07D233/60 , C07D233/61 , C07D241/12 , C07D241/24 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/68 , C07D317/58 , C07D333/38 , C07D521/00 , C08B37/16
CPC分类号： C07D213/40 , C07C275/20 , C07C275/24 , C07C275/28 , C07C275/30 , C07C331/22 , C07D207/34 , C07D209/28 , C07D209/30 , C07D213/54 , C07D213/74 , C07D213/75 , C07D213/81 , C07D213/82 , C07D213/83 , C07D231/12 , C07D233/56 , C07D233/64 , C07D241/24 , C07D249/08 , C07D295/13 , C07D295/15 , C07D295/215 , C07D307/68 , C07D317/58 , C07D333/38
摘要： Novel isoprenoidamine compounds (I) which show antiulcer activity are provided. ##STR1##
摘要翻译：提供了具有抗溃疡活性的新型异戊二烯酮化合物（I）。（一）

9. 发明授权

US06525081B1 Antirheumatic 失效
标题翻译：抗风湿性
公开(公告)号：US06525081B1
公开(公告)日：2003-02-25
申请号：US09530082
申请日：2000-04-24
申请人： Saichi Matsumoto , Hirokuni Jyoyama , Shinji Kakudo , Kohji Hanasaki , Kenzo Koizumi , Tsuneaki Sakata , Ryuji Suzuki
发明人： Saichi Matsumoto , Hirokuni Jyoyama , Shinji Kakudo , Kohji Hanasaki , Kenzo Koizumi , Tsuneaki Sakata , Ryuji Suzuki
IPC分类号： A61K31425
CPC分类号： C07D275/02 , C07D417/06
摘要： A novel antirheumatic agent comprising as an active ingredient a compound of formula I: or a pharmaceutically acceptable salt or hydrate thereof.
摘要翻译：一种新颖的抗风湿剂，其包含式I化合物作为活性成分：或其药学上可接受的盐或水合物。

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