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1. 再颁专利

USRE34918E Azaazulene compounds which are useful as antiallergic and antiinflammatory agents 失效
公开(公告)号：USRE34918E
公开(公告)日：1995-04-25
申请号：US225761
申请日：1994-04-05
申请人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
发明人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
IPC分类号： A61K31/40 , A61K31/403 , A61K31/41 , A61K31/47 , A61K31/495 , A61P29/00 , A61P37/08 , C07D209/52 , C07D401/06 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14 , C07D209/02
CPC分类号： C07D401/06 , C07D209/52 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14
摘要： An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.

2. 发明授权

US5013736A Azaazulene compounds which are useful as antiallergic and antiinflammatory agents 失效
标题翻译：可用作抗过敏和抗炎剂的氮杂薁化合物
公开(公告)号：US5013736A
公开(公告)日：1991-05-07
申请号：US457125
申请日：1989-12-26
申请人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
发明人： Michiko Nagahara , Chikara Ieda , Mitsuo Mimura , Katsuhiro Uchida , Soichiro Sato , Makoto Okumura
IPC分类号： A61K31/40 , A61K31/403 , A61K31/41 , A61K31/47 , A61K31/495 , A61P29/00 , A61P37/08 , C07D209/52 , C07D401/06 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14
CPC分类号： C07D401/06 , C07D209/52 , C07D401/14 , C07D403/04 , C07D409/06 , C07D409/14
摘要： An azaazulene derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond or double bond; when the bond C N is single bond, R.sup.2 is 5-tetrazolyl group, R.sup.3 is taken together with carbon atom to form carbonyl group at the 2-position, and R.sup.4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: ##STR2## in which W is single bond or carbonyl group, oxygen atom, sulfur atom or --CH.dbd.CH--, n is an integer of 1 to 6, and R.sup.1', R.sup.2' and R.sup.3' are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group; when the bond C N is double bond, N at the 1-position has no substituent R.sup.4, R.sup.2 is cyano group, and R.sup.3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.

3. 发明授权

US4699925A Biphenylylpropionic acid derivative and pharmaceutical composition containing the same 失效
标题翻译：联苯基丙酸衍生物和含有它们的药物组合物
公开(公告)号：US4699925A
公开(公告)日：1987-10-13
申请号：US531535
申请日：1983-09-12
申请人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura , Kiyonoshin Ichikawa , Misako Matsumura
发明人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura , Kiyonoshin Ichikawa , Misako Matsumura
IPC分类号： C07D307/33 , A61K31/22 , A01N37/10 , A61K31/23 , A61K31/235
CPC分类号： C07D307/33
摘要： Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms and m is 0 or an integer of 1. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.
摘要翻译：其中R是烷基羰氧基烷基或具有下式的链烯基羰氧基烷基：其中R1是具有1至15个碳原子的烷基或具有2至8个碳原子的链烯基的双苯甲酰基丙酸衍生物和 m为0或整数1.化合物具有优异的抗炎，止痛和解热活性。此外，化合物无刺激，快速，长效，安全性高。

4. 发明授权

US4766148A Biphenylylpropionic acid derivative and pharmaceutical composition containing the same 失效
标题翻译：联苯基丙酸衍生物和含有它们的药物组合物
公开(公告)号：US4766148A
公开(公告)日：1988-08-23
申请号：US742147
申请日：1985-06-07
申请人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura
发明人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura
IPC分类号： C07C67/10 , A61K31/215 , A61K31/365 , A61P25/04 , A61P29/00 , A61P43/00 , C07C69/65 , C07D307/33 , A61K31/22 , C07C69/635
CPC分类号： C07D307/33 , Y10S514/886 , Y10S514/887 , Y10S514/96 , Y10S514/961 , Y10S514/962 , Y10S514/966 , Y10S514/969
摘要： Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is a lower alkyl group having 1 to 5 carbon atoms and R.sup.2 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms, or a lactone having the formula: ##STR3## wherein R.sup.3 and R.sup.4 are hydrogen atom or a lower alkyl group having 1 to 2 carbon atoms, and n is an integer of 1 or 2. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.
摘要翻译：其中R是烷基羰基氧基烷基或具有下式的烯基羰基氧基烷基：其中R 1是具有1至5个碳原子的低级烷基，R 2是具有1至15个碳原子的烷基基团的下式的双苯甲酰基丙酸衍生物碳原子或具有2-8个碳原子的烯基，或具有下式的内酯：其中R 3和R 4是氢原子或具有1至2个碳原子的低级烷基，n是整数1或该化合物具有优异的抗炎，止痛和解热活性。此外，化合物无刺激，快速，长效，安全性高。

5. 发明授权

US4603217A Ester substituted alkyl-2-(2,6-dichloroanilino)phenyl acetates 失效
标题翻译：酯取代的烷基-2-（2,6-二氯苯胺基）苯基乙酸酯
公开(公告)号：US4603217A
公开(公告)日：1986-07-29
申请号：US634252
申请日：1984-07-25
申请人： Katsuhiro Uchida , Mitsuo Mimura , Shozo Masumoto , Makoto Okumura , Masao Tohno , Misako Matsumura
发明人： Katsuhiro Uchida , Mitsuo Mimura , Shozo Masumoto , Makoto Okumura , Masao Tohno , Misako Matsumura
IPC分类号： A61K31/215 , A61K31/403 , A61K31/404 , A61K31/405 , A61P25/04 , A61P29/00 , C07C67/00 , C07C227/00 , C07C227/18 , C07C229/42 , C07D209/28 , C07C101/453
CPC分类号： C07D209/28
摘要： A novel anti-inflammatory drug, which exhibits rapidly a pharmacological activity, maintains the activity for a long time, and is free from a side effect such as a gastrointestinal disorder or a central nervous disturbance is disclosed.The drug comprises a compound of an alkylcarbonyloxyalkylester or alkenylcarbonyloxyalkylester derivative of indolylacetic acid or anilinophenylacetic acid.The compound is prepared by an esterification reaction.
摘要翻译：显示出快速药理活性的新型抗炎药物长时间保持活性，并且没有副作用如胃肠病或中枢神经紊乱。该药物包括吲哚乙酸或苯胺基苯乙酸的烷基羰基氧基烷基酯或烯基羰基氧基烷基酯衍生物的化合物。该化合物通过酯化反应制备。

6. 发明授权

US5196567A Biphenylylpropionic acid derivative, process for preparing the same and pharmaceutical composition containing the same 失效
标题翻译：联苯基丙酸衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5196567A
公开(公告)日：1993-03-23
申请号：US204313
申请日：1988-06-09
申请人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura
发明人： Katsuhiro Uchida , Shozo Masumoto , Masao Tohno , Mitsuo Mimura , Makoto Okumura
IPC分类号： C07D307/33
CPC分类号： C07D307/33
摘要： Biphenylylpropionic acid derivatives of the formula: ##STR1## wherein R is an alkylcarbonyloxyalkyl group or an alkenylcarbonyloxyalkyl group having the formula: ##STR2## wherein R.sup.1 is a lower alkyl group having 1 to 5 carbon atoms and R.sup.2 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 8 carbon atoms, or a lactone having the formula: ##STR3## wherein R.sup.3 and R.sup.4 are hydrogen atom or a lower alkyl group having 1 to 2 carbon atoms, and n is an integer of 1 or 2. The compounds have excellent anti-inflammatory, analgesic and antipyretic activities. Moreover, the compounds have no irritation, rapid and long-acting, and high safety margin.
摘要翻译：其中R是烷基羰基氧基烷基或具有下式的烯基羰基氧基烷基：其中R 1是具有1至5个碳原子的低级烷基，R 2是具有1至15个碳原子的烷基基团的下式的双苯甲酰基丙酸衍生物碳原子或具有2-8个碳原子的烯基，或具有下式的内酯：其中R 3和R 4是氢原子或具有1至2个碳原子的低级烷基，n是整数1或该化合物具有优异的抗炎，止痛和解热活性。此外，化合物无刺激，快速，长效，安全性高。

7. 发明申请

US20130150586A1 PROCESS FOR PRODUCING 1-TRIAZOLE-2-BUTANOL DERIVATIVES 有权
标题翻译：生产1-三唑-2-丁醇衍生物的方法
公开(公告)号：US20130150586A1
公开(公告)日：2013-06-13
申请号：US13818897
申请日：2011-08-31
申请人： Mitsuo Mimura , Masahito Watanabe , Nobuo Ishiyama , Takuya Yamada
发明人： Mitsuo Mimura , Masahito Watanabe , Nobuo Ishiyama , Takuya Yamada
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： An object is to provide a process for producing the compound of formula 1 in higher yield by the ring-opening addition reaction of epoxytriazole with amine under mild conditions without using a large excess of 4-methylenepiperidine. The process for producing (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol or an acid addition salt thereof comprises reacting (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]oxirane with an acid addition salt of 4-methylenepiperidine in a reaction solvent in the presence of a hydroxide of an alkali metal or an alkaline earth metal selected from the group consisting of lithium, sodium, calcium, and strontium, or a hydrate thereof.
摘要翻译：本发明的目的是提供一种通过在温和条件下环氧三唑与胺的开环加成反应而不使用大量过量的4-亚甲基哌啶，以更高的产率制备式1化合物的方法。（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H-1,2,4-三唑-1-基）丁烷 -2-醇或其酸加成盐包括使（2R，3S）-2-（2,4-二氟苯基）-3-甲基-2 - [（1H-1,2,4-三唑-1-基）甲基]环氧乙烷与4-亚甲基哌啶的酸加成盐在反应溶剂中，在选自锂，钠，钙和锶的碱金属或碱土金属的氢氧化物或其水合物存在下，。

8. 发明授权

US07343273B2 Piston design support program, design support method, and design support apparatus 失效
标题翻译：活塞设计支援计划，设计支援方式及设计支援设备
公开(公告)号：US07343273B2
公开(公告)日：2008-03-11
申请号：US10736846
申请日：2003-12-17
申请人： Yasutomo Kusunoki , Kazuhiro Tomizawa , Mitsuo Mimura
发明人： Yasutomo Kusunoki , Kazuhiro Tomizawa , Mitsuo Mimura
IPC分类号： G06G7/48
CPC分类号： G06F17/5095 , F02F3/00 , G06T19/20 , G06T2219/2021
摘要： According to this invention, a piston design support program for supporting design of a piston shape of an internal combustion engine, makes a computer execute an input step of inputting specification values associated with a piston shape, a verification step of verifying, based on the input specification values, whether or not gaps between the piston and its surrounding components are appropriate, a read step of reading out, when it is determined in the verification step that the gaps are appropriate, a three-dimensional piston model which can be deformed according to a predetermined rule from a database, and a deformation step of deforming the piston model on the basis of the specification values.
摘要翻译：根据本发明，一种用于支持内燃机活塞形状设计的活塞设计支撑程序，使得计算机执行输入与活塞形状相关联的规格值的输入步骤，验证步骤基于输入规定值，活塞及其周围部件之间的间隙是否合适;读取步骤，当在验证步骤中确定间隙合适时，读取步骤可以根据以下内容进行变形的三维活塞模型来自数据库的预定规则，以及基于规格值使活塞模型变形的变形步骤。

9. 发明授权

US5367150A Data processing system using IC card 失效
标题翻译：数据处理系统采用IC卡
公开(公告)号：US5367150A
公开(公告)日：1994-11-22
申请号：US917678
申请日：1992-07-22
申请人： Kenichi Kitta , Kunihiro Okada , Mitsuo Mimura , Makoto Ochiai , Naotake Nakamura
发明人： Kenichi Kitta , Kunihiro Okada , Mitsuo Mimura , Makoto Ochiai , Naotake Nakamura
IPC分类号： G06F1/00 , G06F21/57 , G07F7/10 , G07F7/12 , G06F15/30
CPC分类号： G07F7/1008 , G06F21/57 , G06Q20/341 , G06Q20/3552 , G06Q20/3578 , G07F7/08 , G07F7/12 , G07F7/122 , G06F2221/2153
摘要： An IC card (24) and a data memory card (23) are mounted to a terminal equipment (1) connected to a center computer (32) via a line. Confirmation information stored in the IC card is checked whether or not it coincides with confirmation information stored in an RAM (6) in the terminal equipment or confirmation information stored in the data memory card. After coincidence of the confirmation information is detected, the terminal equipment performs the processing to be conventionally performed by the center computer in place of the center computer. An IC card intake and outtake processing mechanism (104) in the terminal equipment does not send out the IC card to the outside of the terminal equipment when the power of the terminal equipment is shut down.
摘要翻译： PCT No.PCT / JP89 / 00970 Sec。 371日期1990年5月22日 102（e）日期1990年5月22日PCT提交1989年9月25日PCT公布。出版物WO90 / 03607 日期：1990年04月5日。IC卡（24）和数据存储卡（23）通过线路安装到连接到中心计算机（32）的终端设备（1）上。检查存储在IC卡中的确认信息，是否与存储在终端设备中的RAM（6）中的确认信息或存储在数据存储卡中的确认信息一致。在检测到确认信息的一致之后，终端设备执行常规地由中央计算机代替中央计算机进行的处理。当终端设备的电源关闭时，终端设备中的IC卡进出口处理机构（104）不将IC卡发送到终端设备的外部。

10. 发明授权

US08871942B2 Process for producing 1-triazole-2-butanol derivatives 有权
标题翻译： 1-三唑-2-丁醇衍生物的制备方法
公开(公告)号：US08871942B2
公开(公告)日：2014-10-28
申请号：US13818897
申请日：2011-08-31
申请人： Mitsuo Mimura , Masahito Watanabe , Nobuo Ishiyama , Takuya Yamada
发明人： Mitsuo Mimura , Masahito Watanabe , Nobuo Ishiyama , Takuya Yamada
IPC分类号： C07D401/06
CPC分类号： C07D401/06
摘要： An object is to provide a process for producing the compound of formula 1 in higher yield by the ring-opening addition reaction of epoxytriazole with amine under mild conditions without using a large excess of 4-methylenepiperidine. The process for producing (2R,3R)-2-(2,4-difluorophenyl)-3-(4-methylenepiperidin-1-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol or an acid addition salt thereof comprises reacting (2R,3S)-2-(2,4-difluorophenyl)-3-methyl-2-[(1H-1,2,4-triazol-1-yl)methyl]oxirane with an acid addition salt of 4-methylenepiperidine in a reaction solvent in the presence of a hydroxide of an alkali metal or an alkaline earth metal selected from the group consisting of lithium, sodium, calcium, and strontium, or a hydrate thereof.
摘要翻译：本发明的目的是提供一种通过在温和条件下环氧三唑与胺的开环加成反应而不使用大量过量的4-亚甲基哌啶，以更高的产率制备式1化合物的方法。（2R，3R）-2-（2,4-二氟苯基）-3-（4-亚甲基哌啶-1-基）-1-（1H-1,2,4-三唑-1-基）丁烷 -2-醇或其酸加成盐包括使（2R，3S）-2-（2,4-二氟苯基）-3-甲基-2 - [（1H-1,2,4-三唑-1-基）甲基]环氧乙烷与4-亚甲基哌啶的酸加成盐在反应溶剂中，在选自锂，钠，钙和锶的碱金属或碱土金属的氢氧化物或其水合物存在下，。

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