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1. 发明授权

US4927835A Acylphenol derivatives, useful as anti-inflammatory agents and pain suppressants 失效
标题翻译：酰基酚衍生物，可用作抗炎剂和止痛剂
公开(公告)号：US4927835A
公开(公告)日：1990-05-22
申请号：US317601
申请日：1989-03-01
申请人： Masahiro Kise , Yoshihiko Yoshimoto , Hiroshi Fujisawa , Yasuo Sasaki , Shoji Yasufuku
发明人： Masahiro Kise , Yoshihiko Yoshimoto , Hiroshi Fujisawa , Yasuo Sasaki , Shoji Yasufuku
IPC分类号： A61K31/13 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P29/00 , C07C20060101 , C07C225/16 , C07C225/18 , C07D207/32 , C07D207/333 , C07D211/40 , C07D295/10 , C07D295/112 , C07D307/46 , C07D307/56 , C07D333/22
CPC分类号： C07D207/333 , C07C225/16 , C07C225/18 , C07D295/112 , C07D307/46 , C07D333/22 , C07C2101/14
摘要： Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is cycloalkyl of 5 to 7 carbon atoms; aryl of 6 to 10 carbon atoms unsubstituted or substituted by straight or branched chain alkyl of 1 to 4 carbon atoms, halo or trifluoromethyl; or ##STR2## wherein A is oxygen, sulfur or NR.sup.5, wherein R.sup.5 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo, and R.sup.6 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo;R.sup.2 is straight or branched chain alkyl of 1 to 4 carbon atoms or cycloalkyl of 5 to 7 carbon atoms; andR.sup.3 and R.sup.4 are the same or different and each is hydrogen; straight or branched chain alkyl of 1 to 8 carbon atoms unsubstituted or substituted by hydroxy, acyloxy of 2 to 5 carbon atoms, carboxyl or carbamoyl;are useful for treating pain, inflammation and fever in humans and animals.

2. 发明授权

US5011831A Derivatives of quinolinecarboxylic acid 失效
标题翻译：喹啉羧酸的衍生物
公开(公告)号：US5011831A
公开(公告)日：1991-04-30
申请号：US267938
申请日：1988-11-07
申请人： Masahiro Kise , Masahiko Kitano , Masakuni Ozaki , Kenji Kazuno , Masahito Matsuda , Ichiro Shirahase , Yoshifumi Tomii
发明人： Masahiro Kise , Masahiko Kitano , Masakuni Ozaki , Kenji Kazuno , Masahito Matsuda , Ichiro Shirahase , Yoshifumi Tomii
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and ##STR2## is a 5- or 6-membered ring wherein the nitrogen atom is the only heteroatom or where there is a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, said 5- or 6-membered ring being unsubstituted or substituted by lower alkyl, amino or mono- or di-lower alkyl amino are useful for treating bacterial infections in humans and animals.

3. 发明授权

US4857515A Certain antihypertensive 1,4-dihydro-6-methyl-5-phosphonic acid-4-aryl-3-carboxylic acid-2-cyano diesters 失效
标题翻译：某些抗高血压的1,4-二氢-6-甲基-5-膦酸-4-芳基-3-羧酸-2-氰基二酯
公开(公告)号：US4857515A
公开(公告)日：1989-08-15
申请号：US115170
申请日：1987-10-30
申请人： Kiyoshi Kimura , Masahiro Kise , Iwao Morita , Toshio Tomita , Masami Tsuda
发明人： Kiyoshi Kimura , Masahiro Kise , Iwao Morita , Toshio Tomita , Masami Tsuda
IPC分类号： C07F9/58 , A61K31/675 , A61P9/08 , A61P9/12 , C07F9/59
CPC分类号： C07F9/597
摘要： A compound of formula (I): ##STR1## wherein R.sup.1 is alkenyl or alkyl or both of the depicted R.sup.1 groups together represent trimethylene and form a six-membered ring together with the depicted oxygen and phosphorus atoms, R.sup.2 is nitro, trifluoromethyl or halogen, R.sup.3 is alkyl, and R.sup.4 is dimethoxymethyl, formyl, hydroxymethyl or nitrile.
摘要翻译：式（I）的化合物：其中R 1是烯基或烷基或所描述的R 1基团两者一起表示三亚甲基，并与所描述的氧和磷原子一起形成六元环，R 2是硝基，三氟甲基或卤素，R 3是烷基，R 4是二甲氧基甲基，甲酰基，羟甲基或腈。

4. 发明授权

US5102882A Pyroglutamide derivatives 失效
标题翻译：吡咯烷酮衍生物
公开(公告)号：US5102882A
公开(公告)日：1992-04-07
申请号：US661523
申请日：1991-02-26
申请人： Koyishi Kimura , Shoichi Chokai , Toshio Tomita , Masahiro Kise , Kenichi Nakamura
发明人： Koyishi Kimura , Shoichi Chokai , Toshio Tomita , Masahiro Kise , Kenichi Nakamura
IPC分类号： C07D207/28 , C07D401/06 , C07D401/12 , C07D403/06 , C07D407/12 , C07D409/12
CPC分类号： C07D401/06 , C07D207/28 , C07D401/12 , C07D403/06 , C07D407/12 , C07D409/12
摘要： Pyroglutamide derivatives have been found to be useful as nootropic agents for administration to humans and animals.
摘要翻译：已经发现焦呋喃酰胺衍生物可用作用于给予人和动物的诱导剂。

5. 发明授权

US4843070A Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically acceptable salts thereof 失效
标题翻译：取代的噻唑并喹啉-3-羧酸及其药学上可接受的盐
公开(公告)号：US4843070A
公开(公告)日：1989-06-27
申请号：US49814
申请日：1987-05-13
申请人： Masahiro Kise , Masahiko Kitano , Masakuni Ozaki , Kenji Kazuno , Ichiro Shirahase , Yoshifumi Tomii , Jun Segawa
发明人： Masahiro Kise , Masahiko Kitano , Masakuni Ozaki , Kenji Kazuno , Ichiro Shirahase , Yoshifumi Tomii , Jun Segawa
IPC分类号： A61K31/47 , A61P31/04 , C07D513/04
CPC分类号： C07D513/04
摘要： Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: ##STR1## in which R.sup.1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R.sup.2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R.sup.3 is hydrogen or substituted or unsubstituted alkyl; R.sup.4 and R.sup.5 are the same or different and are alkyl or hydroxyalkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.
摘要翻译：式I的抗细菌和抗真菌化合物及其药学上可接受的盐：其中R 1是氢，烷基或取代或未取代的苯基; R2是氢，烷基，烷氧基，羟基，卤素，硝基或取代或未取代的氨基; R3是氢或取代或未取代的烷基; R 4和R 5相同或不同，并且是烷基或羟基烷基或R 4和R 5与它们所连接的氮原子一起形成具有所述氮原子作为唯一杂原子的未取代或取代的杂环，或可具有氮，氧或硫原子作为其它杂原子; X为卤素。

6. 发明授权

US5086049A 7[4-(5 methyl-2-oxo-1,3-dioxalen-4-yl)methyl 1-piperzinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acids 失效
标题翻译： 7（4-（5甲基-2-氧代-1,3-二氧戊环-4-基）甲基-1-哌嗪基）-4-氧代-4H-（1,3）噻唑并（3,2-A）喹啉-3 羧酸
公开(公告)号：US5086049A
公开(公告)日：1992-02-04
申请号：US682434
申请日：1991-04-08
申请人： Masahiro Kise , Masahiko Kitano , Masakuni Ozaki , Kenji Kazuno , Masahito Matsuda , Ichiro Shirahase , Jun Segawa
发明人： Masahiro Kise , Masahiko Kitano , Masakuni Ozaki , Kenji Kazuno , Masahito Matsuda , Ichiro Shirahase , Jun Segawa
IPC分类号： C07D513/04 , A61K31/47 , A61P31/04
CPC分类号： C07D513/04
摘要： Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and R.sup.3 is hydrogen, halo or straight or branch chain lower alkoxy, are useful for treating bacterial infections in humans and animals.

7. 发明授权

US4882328A Thiazetidine derivatives 失效
标题翻译：噻嗪替丁衍生物
公开(公告)号：US4882328A
公开(公告)日：1989-11-21
申请号：US247959
申请日：1988-09-22
申请人： Masahiro Kise , Masakuni Ozaki , Kenji Kazuno , Yoshifumi Tomii , Jun Segawa , Shoji Yasufuki
发明人： Masahiro Kise , Masakuni Ozaki , Kenji Kazuno , Yoshifumi Tomii , Jun Segawa , Shoji Yasufuki
IPC分类号： C07D513/14
CPC分类号： C07D513/14
摘要： Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or phenyl unsubstituted or substituted by one or two halo moieties, R.sup.2 is hydrogen or alkyl, A CX wherein X is halo, B is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.

8. 发明授权

US4659734A Olinecarboxylic acid derivatives 失效
标题翻译：奥林酸衍生物
公开(公告)号：US4659734A
公开(公告)日：1987-04-21
申请号：US523329
申请日：1983-08-15
申请人： Hiroshi Enomoto , Masahiro Kise , Masakuni Ozaki , Masahiko Kitano , Iwao Morita
发明人： Hiroshi Enomoto , Masahiro Kise , Masakuni Ozaki , Masahiko Kitano , Iwao Morita
IPC分类号： C07D513/04 , A61K31/495 , C07D417/14
CPC分类号： C07D513/04
摘要： A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms;A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; andR.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 or R.sub.4 and R.sub.5 together may be alkylenedioxy of 1 to 5 carbon atoms which form a ring with the carbon atoms to which they are attached; or a pharmaceutically acceptable salt thereof.
摘要翻译：式（1）的化合物R1是氢，碱金属，碱土金属，低级烷基，新戊酰氧基甲基或苯酞; R 2，R 3，R 4和R 5相同或不同，为氢，卤素，低级烷氧基或者其中R 6和R 7为低级烷基或R 6和R 7与它们所连接的氮原子一起形成5- 含有所述氮原子作为唯一杂原子或含有氮，硫或氧作为额外的反应原子的七元未取代或取代的杂环; A是1至5个碳原子的饱和或不饱和烃链，未被取代或被低级烷基取代; 低级烷氧基低级烷硫基; 羟基; 卤素; 被卤素，氨基，低级烷氧基羰基，羧基，低级烷氧基，低级烷硫基，低级酰氧基或羟基取代的低级烷基; 低级烷基氨基; 羧基; 硝基氰基; 羰; 亚氨基或被取代或未取代的苯基，苯硫基，苯基氨基或苯氧基取代; 并且R 2和R 3或R 3和R 4或R 4和R 5一起可以是与其所连接的碳原子形成环的1至5个碳原子的亚烷基二氧基; 或其药学上可接受的盐。

9. 发明授权

US5036098A Butynylamine derivatives and their production 失效
标题翻译：丁炔胺衍生物及其生产
公开(公告)号：US5036098A
公开(公告)日：1991-07-30
申请号：US407228
申请日：1989-09-14
申请人： Kiyoshi Kimura , Masahiro Kise , Iwao Morita
发明人： Kiyoshi Kimura , Masahiro Kise , Iwao Morita
IPC分类号： C07C219/20 , C07C219/24 , C07C235/34 , C07D295/084 , C07D295/125 , C07D333/24
CPC分类号： C07D295/084 , C07C219/20 , C07C219/24 , C07C235/34 , C07D295/125 , C07D333/24 , C07C2101/08 , C07C2101/14
摘要： Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.

10. 发明授权

US4426381A Carboxylic acid derivatives 失效
标题翻译：羧酸衍生物
公开(公告)号：US4426381A
公开(公告)日：1984-01-17
申请号：US348184
申请日：1982-02-12
申请人： Shingo Matsumura, deceased , Masahiro Kise , Masakuni Ozaki , Shinichi Tada , Kenji Kazuno , Hisao Watanabe , Katsutoshi Kunimoto , Masami Tsuda
发明人： Shingo Matsumura, deceased , Masahiro Kise , Masakuni Ozaki , Shinichi Tada , Kenji Kazuno , Hisao Watanabe , Katsutoshi Kunimoto , Masami Tsuda
IPC分类号： A61K31/47 , A61P31/04 , C07D215/56 , C07D277/10 , C07D513/04 , C07D513/14 , C07D475/00 , A61K31/495
CPC分类号： C07D513/04 , C07D215/56 , C07D277/10 , C07D513/14
摘要： Quinolinecarboxylic acid derivatives, such as compound 7-fluoro-8-(4-methyl-1-piperazinyl)-5-oxo-1,2-dihydro-5H-thiazolo(3,2-a)-quinoline-4-carboxylic acid, a pharmaceutical composition containing the same and methods of treatment of bacterial and fungal infections using the same.
摘要翻译：喹啉羧酸衍生物，如7-氟-8-（4-甲基-1-哌嗪基）-5-氧代-1,2-二氢-5H-噻唑并（3,2-a） - 喹啉-4-羧酸，含有该组合物的药物组合物和使用其的治疗细菌和真菌感染的方法。

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