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1. 发明授权

US5294623A (Benzhydryloxyethylpiperidyl) aliphatic acid derivatives and their use in the treatment of allergies and asthma 失效
标题翻译：（二苯甲氧基乙基哌啶基）脂肪酸衍生物及其在治疗过敏和哮喘中的应用
公开(公告)号：US5294623A
公开(公告)日：1994-03-15
申请号：US995547
申请日：1992-12-22
申请人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
发明人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
IPC分类号： A61K31/445 , A61K31/452 , A61P11/00 , A61P11/08 , A61P37/08 , A61P43/00 , C07D211/34 , A01N41/02 , C07D211/18
CPC分类号： C07D211/34
摘要： Compounds of formula (I): ##STR1## in which: R.sup.1 and R.sup.2 are independently alkyl, alkoxy, trifluoromethyl, nitro or halogen; A is an aliphatic hydrocarbon group having from 2 to 8 carbon atoms whose chain contains at least 2 carbon atoms in a linear chain between the piperidine group and --COOH, said group optionally being unsaturated; and m and n are independently 0, 1, 2 or 3; and pharmaceutically acceptable salts and esters thereof have been found to have valuable anti-histamine properties without the usual side effects of anti-histamines. Methods of preparing the compounds are also provided.
摘要翻译：式（I）化合物：其中：R 1和R 2独立地是烷基，烷氧基，三氟甲基，硝基或卤素; A是具有2至8个碳原子的脂族烃基，其链在哌啶基和-COOH之间的直链中含有至少2个碳原子，所述基团任选是不饱和的; m和n分别为0,1,2或3; 已经发现其药学上可接受的盐和酯具有有价值的抗组胺性质而没有抗组氨胺的常见副作用。还提供了制备化合物的方法。

2. 发明授权

US5407933A Nitrogen-containing tetracyclic compounds having anti-allergic and anti-asthmatic activities and their use 失效
标题翻译：具有抗过敏和抗哮喘活性的含氮四环化合物及其用途
公开(公告)号：US5407933A
公开(公告)日：1995-04-18
申请号：US291347
申请日：1994-08-16
申请人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
发明人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
IPC分类号： A61K31/55 , C07D487/04 , C07D487/14
CPC分类号： C07D487/04 , C07D487/14
摘要： Compounds of formula (I): ##STR1## [wherein: A-- B is .dbd.C.dbd.CH--or a nitrogen atom; R.sup.1 is hydrogen, alkyl, aryl or aralkyl; and Z is alkylene] and pharmaceutically acceptable salts thereof are useful in the treatment and prevention of allergies and asthma.
摘要翻译：式（I）化合物：其中：A-B为= C = CH-或氮原子; R1是氢，烷基，芳基或芳烷基; 和Z是亚烷基]及其药学上可接受的盐可用于治疗和预防过敏和哮喘。

3. 发明授权

US5461051A Tetracyclic compounds having anti-allergic and anti-asthmatic activities and their use 失效
标题翻译：具有抗过敏和抗哮喘活性的四环化合物及其用途
公开(公告)号：US5461051A
公开(公告)日：1995-10-24
申请号：US267274
申请日：1994-06-28
申请人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
发明人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
IPC分类号： C07D213/06 , C07D213/60 , C07D223/14 , C07D241/42 , C07D471/14 , C07D487/04 , A61K31/55
CPC分类号： C07D471/14 , C07D487/04 , Y10S514/826
摘要： Compounds of formula (I): ##STR1## in which: Q is nitrogen or .dbd.CH--; R.sup.1 and R.sup.2 are hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl or halogen; and R.sup.3 is a substituted alkyl groups, or a pharmaceutically acceptable salt thereof have valuable anti-allergic and anti-asthmatic activities. The compounds are prepared by reacting a corresponding compound where R.sup.3 is replaced by a hydrogen atom with a compound to introduce the group R.sup.3.
摘要翻译：式（I）的化合物：其中：Q是氮或= CH-; R1和R2是氢，烷基，烷氧基，羟基，三氟甲基或卤素; 并且R 3是取代的烷基，或其药学上可接受的盐具有有价值的抗过敏和抗哮喘活性。通过使其中R3被氢原子代替的相应化合物与化合物反应以引入基团R3来制备化合物。

4. 发明授权

US5476848A 14B(R) isomers of novel tetracyclic compounds having anti-allergic and anti-asthmatic activities, and their use 失效
标题翻译：具有抗过敏和抗哮喘活性的新型四环化合物的14B（R）异构体及其用途
公开(公告)号：US5476848A
公开(公告)日：1995-12-19
申请号：US197208
申请日：1994-02-16
申请人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
发明人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
IPC分类号： C07D471/14 , C07D487/04 , C07D487/14 , A61K31/55
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14
摘要： An optically active compound of formula (I): ##STR1## in which R.sup.3 represents groups of formula --A--COOR.sup.4, whereinA represents alkylene groups having 3 or 5 carbon atoms andR.sup.4 represents hydrogen or an alkyl group having 1 to 4 carbon atoms; or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的光学活性化合物：其中R 3表示式-A-COOR 4的基团，其中A表示具有3或5个碳原子的亚烷基，R 4表示氢或具有1至 4个碳原子; 或其药学上可接受的盐。

5. 发明授权

US5362725A Tetracyclic compounds having anti-allergic and anti-asthmatic activities and their use 失效
标题翻译：具有抗过敏和抗哮喘活性的四环化合物及其用途
公开(公告)号：US5362725A
公开(公告)日：1994-11-08
申请号：US962037
申请日：1992-10-15
申请人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
发明人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Yoshio Iizuka , Takeshi Yamaguchi
IPC分类号： C07D213/06 , C07D213/60 , C07D223/14 , C07D241/42 , C07D471/14 , C07D487/04 , A61K31/55
CPC分类号： C07D471/14 , C07D487/04 , Y10S514/826
摘要： Compounds of formula (I): ##STR1## in which: Q is nitrogen or .dbd.CH--; R.sup.1 and R.sup.2 are hydrogen, alkyl, alkoxy, hydroxy, trifluoromethyl or halogen; and R.sup.3 is a substituted alkyl groups or a pharmaceutically acceptable salt thereof have valuable anti-allergic and anti-asthmatic activities. The compounds are prepared by reacting a corresponding compound where R.sup.3 is replaced by a hydrogen atom with a compound to introduce the group R.sup.3.
摘要翻译：式（I）的化合物：其中：Q是氮或= CH-; R1和R2是氢，烷基，烷氧基，羟基，三氟甲基或卤素; 并且R 3是取代的烷基或其药学上可接受的盐具有有价值的抗过敏和抗哮喘活性。通过使其中R3被氢原子代替的相应化合物与化合物反应以引入基团R3来制备化合物。

6. 发明授权

US5470851A Thiazolidinecarboxylic acid amide derivatives and their therapeutic uses 失效
标题翻译：噻唑烷羧酸酰胺衍生物及其治疗用途
公开(公告)号：US5470851A
公开(公告)日：1995-11-28
申请号：US129774
申请日：1993-09-30
申请人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Takeshi Yamaguchi , Takeshi Oshima , Fumitoshi Asai , Yasuteru Iijima
发明人： Hiroshi Fukumi , Toshiaki Sakamoto , Mitsuo Sugiyama , Takeshi Yamaguchi , Takeshi Oshima , Fumitoshi Asai , Yasuteru Iijima
IPC分类号： C07D417/04 , C07D417/14 , C07D471/14 , C07D487/04 , C07D487/14 , A61K31/55
CPC分类号： C07D417/04 , C07D417/14 , C07D471/14 , C07D487/04 , C07D487/14
摘要： Thiazolidinecarboxylic acid amides having combined antiallergic and antiasthmatic activities with an antagonist activity against platelet Activating Factor and having the following general formula (I) ##STR1##
摘要翻译：具有抗血小板活化因子拮抗活性和具有下列通式（I）的组合抗过敏和抗哮喘活性的噻唑烷羧酸酰胺具有下列通式（I）：（VI）（VI）（六）

7. 发明申请

US20140005393A1 SULFONAMIDE COMPOUNDS HAVING TRPM8 ANTAGONISTIC ACTIVITY 有权
标题翻译：具有TRPM8拮抗活性的磺酰胺化合物
公开(公告)号：US20140005393A1
公开(公告)日：2014-01-02
申请号：US14004911
申请日：2012-03-15
申请人： Yasuyuki Tsuzuki , Daisuke Sawamoto , Toshiaki Sakamoto , Taku Kato , Yasuki Miwa , Nobumasa Awai
发明人： Yasuyuki Tsuzuki , Daisuke Sawamoto , Toshiaki Sakamoto , Taku Kato , Yasuki Miwa , Nobumasa Awai
IPC分类号： C07D487/04 , C07D405/12 , C07D401/12 , C07D217/22 , C07D409/12
CPC分类号： C07D413/12 , C07D215/38 , C07D217/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: (I) wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.
摘要翻译：提供了具有TRPM8拮抗活性的磺酰胺化合物。式（I）的磺酰胺化合物或其药学上可接受的盐或其前药：（I）其中环A是由（a）吡啶组成的双环芳族杂环与苯稠合; 或（b）吡啶与单环芳族杂环稠合，环A与构成环A的吡啶环的氮原子相邻的碳原子上的磺酰基氨基部分结合，环B为（a）单环或双环芳烃; （b）单环或双环脂环烃; （c）单环或双环芳族杂环; 或（d）单环或双环非芳族杂环，环C为（a）苯; 或（b）单环芳族杂环，以及其他符号与说明书中所定义的相同。

8. 发明申请

US20110166135A1 AROMATIC NITROGEN-CONTAINING 6-MEMBERED RING COMPOUNDS AND THEIR USE 审中-公开
标题翻译：含有硝酸的六元环化合物及其用途
公开(公告)号：US20110166135A1
公开(公告)日：2011-07-07
申请号：US13062841
申请日：2009-09-09
申请人： Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
发明人： Hiroshi Morimoto , Toshiaki Sakamoto , Toshiyuki Himiyama , Eiji Kawanishi , Takehiko Matsumura
IPC分类号： A61K31/5377 , C07D401/14 , C07D487/04 , C07D413/14 , A61K31/517 , A61K31/506 , A61K31/497 , A61K31/519 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/16 , A61P25/28
CPC分类号： C07D401/14 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12
摘要： The present invention provides aromatic nitrogen-containing 6-membered ring compounds having excellent PDE10 inhibitory activity. The present invention relates to an aromatic nitrogen-containing 6-membered ring compound represented by the following formula [I0] or a pharmaceutically acceptable salt thereof, a method for preparing the same, and use of said compounds for PDE10 inhibitors, and a pharmaceutical composition comprising said compounds as an active ingredient: Formula [I0] wherein: X1, X2 and X3 each independently are N or CH, and at least two of X1, X2 and X3 are N; A is *—CH═CH—, *—C(Alk)=CH—, *—CH2—CH2— or *—O—CH2— (* is a bond with R1); Alk is a lower alkyl group; Ring B is an optionally substituted nitrogen-containing aliphatic heterocyclic group; R1 is an optionally substituted nitrogen-containing heterocyclic group, a nitrogen-containing heterocyclic moiety of which is a moiety selected from the group consisting of quinoxalinyl, quinolyl, isoquinolyl, quinazolinyl, pyrazinyl, pyrimidinyl and a moiety thereof fused with a 5 to 6-membered aliphatic ring thereto; Y0 is a group selected from the group consisting of the following (1) to (5): (1) an optionally substituted phenyl or an optionally substituted aromatic monocyclic 5 to 6-membered heterocyclic group; (2) an optionally substituted aminocarbonyl; (3) an optionally substituted amino lower alkyl; (4) —O—R2 wherein R2 is hydrogen, an optionally substituted lower alkyl, lower cycloalkyl, aliphatic monocyclic 5 to 6-membered heterocyclic group, or Formula [AA]; (5) mono- or di-substituted amino; provided that, when Y0 is mono- or di-substituted amino, the nitrogen-containing heterocyclic moiety of R1 is not quinoxalinyl or quinolyl.
摘要翻译：本发明提供具有优异的PDE10抑制活性的芳香族含氮6元环化合物。本发明涉及由下式[I0]表示的含芳族含氮的6元环化合物或其药学上可接受的盐，其制备方法以及所述化合物用于PDE10抑制剂的用途和药物组合物包括所述化合物作为活性成分：式[I0]其中：X1，X2和X3各自独立地为N或CH，X1，X2和X3中的至少两个为N; A是* -CH = CH-，* -C（Alk）= CH-，* -CH2-CH2-或* -O-CH2-（*是与R1的键）; Alk是低级烷基; 环B是任选取代的含氮脂族杂环基; R1是任选取代的含氮杂环基团，其含氮杂环部分是选自喹喔啉基，喹啉基，异喹啉基，喹唑啉基，吡嗪基，嘧啶基及其部分与5至6位稠合的部分，元环脂族环; Y0是选自下列（1）至（5）的基团：（1）任选取代的苯基或任选取代的芳族单环5至6元杂环基; （2）任选取代的氨基羰基; （3）任选取代的氨基低级烷基; （4）-O-R2，其中R2是氢，任选取代的低级烷基，低级环烷基，脂族单环5至6元杂环基或式[AA]; （5）单取代或二取代氨基; 条件是当Y 0是单取代或二取代的氨基时，R 1的含氮杂环部分不是喹喔啉基或喹啉基。

9. 发明授权

US09540360B2 Sulfonamide compounds having TRPM8 antagonistic activity 有权
标题翻译：具有TRPM8拮抗活性的磺酰胺化合物
公开(公告)号：US09540360B2
公开(公告)日：2017-01-10
申请号：US14620360
申请日：2015-02-12
申请人： Yasuyuki Tsuzuki , Daisuke Sawamoto , Toshiaki Sakamoto , Taku Kato , Yasuki Niwa , Nobumasa Awai
发明人： Yasuyuki Tsuzuki , Daisuke Sawamoto , Toshiaki Sakamoto , Taku Kato , Yasuki Niwa , Nobumasa Awai
IPC分类号： A61K31/4709 , A61K31/4725 , A61K31/472 , C07D413/12 , C07D217/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D215/38
CPC分类号： C07D413/12 , C07D215/38 , C07D217/22 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.
摘要翻译：提供了具有TRPM8拮抗活性的磺酰胺化合物。式（I）的磺酰胺化合物或其药学上可接受的盐或其前药：其中环A是由（a）吡啶组成的双环芳族杂环与苯稠合; 或（b）吡啶与单环芳族杂环稠合，环A与构成环A的吡啶环的氮原子相邻的碳原子上的磺酰基氨基部分结合，环B为（a）单环或双环芳烃; （b）单环或双环脂环烃; （c）单环或双环芳族杂环; 或（d）单环或双环非芳族杂环，环C为（a）苯; 或（b）单环芳族杂环，以及其他符号与说明书中所定义的相同。

10. 发明授权

US5367787A Drying machine 失效
标题翻译：烘干机
公开(公告)号：US5367787A
公开(公告)日：1994-11-29
申请号：US102307
申请日：1993-08-05
申请人： Tomohiko Ikeda , Toshiaki Sakamoto
发明人： Tomohiko Ikeda , Toshiaki Sakamoto
IPC分类号： D06F43/08 , F26B11/18 , F26B21/10 , F26B25/00 , F26B19/00
CPC分类号： F26B21/10 , D06F43/086 , F26B11/181 , F26B25/006 , F26B25/009
摘要： A drying machine has a drying chamber for drying an article cleaned with an inflammable solvent as a detergent. A hot air supply channel communicates with the drying chamber and a heater is mounted in the hot air supply channel. A hot air evacuation channel communicates with the drying chamber and a hot air transfer device is mounted at a voluntary portion of the hot air supply channel and the hot air evacuation channel. A control device is provided for driving control of the heater. A first temperature sensor is mounted on the downstream side of the heater in the hot air supply channel and a second temperature sensor is mounted at a position shifted to the drying chamber in the hot air evacuation channel. The control device controls the heater so that the difference in the temperature detected by the first temperature sensor and the temperature detected by the second temperature sensor is kept within a safe temperature range.
摘要翻译：干燥机具有干燥室，用于干燥用易燃溶剂清洗的物品作为洗涤剂。热风供应通道与干燥室连通，并且加热器安装在热空气供应通道中。热空气排出通道与干燥室连通，热空气传送装置安装在热空气供应通道和热空气排出通道的自愿部分。提供控制装置用于驱动加热器的控制。第一温度传感器安装在热空气供应通道中的加热器的下游侧，并且第二温度传感器安装在位于热空气排出通道中的干燥室的位置。控制装置控制加热器，使得由第一温度传感器检测到的温度差和由第二温度传感器检测到的温度保持在安全的温度范围内。

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