公开(公告)号：US08247402B2

公开(公告)日：2012-08-21

申请号：US12012932

申请日：2008-02-05

申请人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

发明人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

IPC分类号： C07D477/20 ,  A61K31/407 ,  A61P31/04

CPC分类号： C07D477/20 ,  C07B2200/13

摘要： Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)p yrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) and a crystal of said compound having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

摘要翻译： 提供具有优异稳定性的吡咯烷基硫代碳青霉烯衍生物的新型晶体。 根据本发明，（+） - （4R，5S，6S）-6 - [（1R）-1-羟乙基] -4-甲基-7-氧代-3 [[（3S，5S） 具有衍射图案的5-（氨磺酰氨基甲基）吡咯烷-3-基]硫] -1-氮杂双环[3.2.0]庚-2-烯-2-羧酸，其衍射图在粉末X射线衍射中具有衍射角 2），约13.04,14.98,15.C，16.62,20.62,21.06,22.18,29.90,26.08,28.22和28.98（度），所述化合物的晶体在粉末X射线衍射中具有在衍射峰上具有主峰的衍射图案 提供约6.62,13.04,15.44,16.58,17.64,20.88,23.26,25.02和25.52（度）的角度（2＆amp;）。

公开(公告)号：US20080207586A1

公开(公告)日：2008-08-28

申请号：US12012932

申请日：2008-02-05

申请人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

发明人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

IPC分类号： A61K31/407 ,  C07D487/04 ,  A61P31/00

CPC分类号： C07D477/20 ,  C07B2200/13

摘要： A novel crystal of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction preferably having main peaks at diffraction angles (2θ)=13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) is provided.

摘要翻译： 提供了具有优异稳定性的吡咯烷基硫代碳青霉烯衍生物的新型结晶。 根据本发明，（+） - （4R，5S，6S）-6 - [（1R）-1-羟乙基] -4-甲基-7-氧代-3 [[（3S，5S） 在粉末X射线衍射中具有衍射图案的5-（氨磺酰氨基甲基）吡咯烷-3-基]硫] -1-氮杂双环[3.2.0]庚-2-烯-2-羧酸优选在衍射角 2θ）= 13.04,14.98,15.C，16.62,20.62,21.06,22.18,23.90,26.08,28.22和28.98（度）。

公开(公告)号：US20130059831A1

公开(公告)日：2013-03-07

申请号：US13585611

申请日：2012-08-14

申请人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

发明人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

IPC分类号： A61K31/407 ,  A61P31/00 ,  C07D487/04

CPC分类号： C07D477/20 ,  C07B2200/13

摘要： Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2θ) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

公开(公告)号：US20070060562A1

公开(公告)日：2007-03-15

申请号：US11595348

申请日：2006-11-10

申请人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

发明人： Izumi Saitoh ,  Masayuki Takahira ,  Toshio Kawakita ,  Yasuyuki Yoshioka

IPC分类号： C07D487/04 ,  A61K31/407

CPC分类号： C07D477/20 ,  C07B2200/13

摘要： A novel crystal of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3 [[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction preferably having main peaks at diffraction angles (2θ)=13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) is provided.

摘要翻译： 提供了具有优异稳定性的吡咯烷基硫代碳青霉烯衍生物的新型结晶。 根据本发明，（+） - （4R，5S，6S）-6 - [（1R）-1-羟乙基] -4-甲基-7-氧代-3 [[（3S，5S） 在粉末X射线衍射中具有衍射图案的5-（氨磺酰氨基甲基）吡咯烷-3-基]硫] -1-氮杂双环[3.2.0]庚-2-烯-2-羧酸优选在衍射角 2θ）= 13.04,14.98,15.C，16.62,20.62,21.06,22.18,23.90,26.08,28.22和28.98（度）。

公开(公告)号：US5346977A

公开(公告)日：1994-09-13

申请号：US52293

申请日：1993-04-26

申请人： Yoshio Sakai ,  Izumi Saitoh

发明人： Yoshio Sakai ,  Izumi Saitoh

IPC分类号： A61K8/00 ,  A61K8/81 ,  A61Q17/00 ,  C08F20/10 ,  C08F220/10

CPC分类号： A61Q17/00 ,  A61K8/8152 ,  A61K2800/75

摘要： A method of applying a skin-protective composition which comprises an acrylic copolymer which comprises(A) 40 to 85% by weight of an alkyl acrylate,(B) 5 to 50% by weight of an alkyl methacrylate, and(C) 10 to 30% by weight of a mono-ethylenically unsaturated monomer having a carboxyl group, and a medium, which can effectively block irritative materials and be easily removed from a skin.

摘要翻译： 一种施用皮肤保护性组合物的方法，其包含丙烯酸共聚物，其包含（A）40〜85重量％的丙烯酸烷基酯，（B）5〜50重量％的甲基丙烯酸烷基酯，（C）10〜 30重量％的具有羧基的单烯属不饱和单体和介质，其可以有效地阻挡刺激性材料并容易从皮肤上除去。

公开(公告)号：US4935241A

公开(公告)日：1990-06-19

申请号：US266894

申请日：1988-11-03

申请人： Izumi Saitoh ,  Kaori Ikeda ,  Shigeru Kido ,  Yoshio Doi ,  Shohei Egawa

发明人： Izumi Saitoh ,  Kaori Ikeda ,  Shigeru Kido ,  Yoshio Doi ,  Shohei Egawa

IPC分类号： A61K9/70 ,  A61K31/415 ,  A61K47/10 ,  A61K47/32 ,  A61K47/38 ,  A61P17/00

CPC分类号： A61K31/415 ,  A61K47/32 ,  A61K47/38 ,  A61K9/0014 ,  Y10S514/858 ,  Y10S514/964

摘要： A pharmaceutical preparation for the treatment of tinea pedis, containing as basic components about 0.1% to about 2.5% of croconazole hydrochloride and about 1%-15% of an ethyl acrylate-methyl methacrylate copolymer in an aqueous alcohol, and if necessary, about 0.1% to about 2.5% of a thickening agent and/or a plasticizer.

公开(公告)号：US4923893A

公开(公告)日：1990-05-08

申请号：US267284

申请日：1988-11-04

申请人： Izumi Saitoh ,  Shigeru Kido ,  Yoshio Doi ,  Shohei Egawa

发明人： Izumi Saitoh ,  Shigeru Kido ,  Yoshio Doi ,  Shohei Egawa

IPC分类号： A61K8/30 ,  A61K8/34 ,  A61K8/67 ,  A61K8/73 ,  A61K9/06 ,  A61K9/70 ,  A61K31/19 ,  A61K31/355 ,  A61K47/12 ,  A61K47/32 ,  A61K47/38 ,  A61P3/02 ,  A61P29/00

CPC分类号： A61K31/355 ,  A61K47/12 ,  A61K47/32 ,  A61K47/38 ,  A61K9/0014 ,  A61K9/7015 ,  Y10S514/887

摘要： External preparations consisting essentially of about 0.1% to about 5% of tocopherol acetate and/or about 0.05% to about 0.3% of glycyrrhetinic acid, about 1% to about 15% of a methacrylic acid-ethyl acrylate copolymer, and about 0.2% to about 3% of a thickening agent in an alcoholic solvent, wherein said copolymer is characterized by that the monomer ratio of ethyl acrylate to methacrylic acid is within a range from 75/25 to 95/5, with residual monomer being 50 ppm or less and with practically no surfactants.

公开(公告)号：US4874830A

公开(公告)日：1989-10-17

申请号：US109619

申请日：1987-10-19

申请人： Izumi Saitoh ,  Shigeru Kido ,  Yoshio Sasaki ,  Syuichiro Shinohara

发明人： Izumi Saitoh ,  Shigeru Kido ,  Yoshio Sasaki ,  Syuichiro Shinohara

IPC分类号： A61K8/81 ,  A61Q17/00 ,  C08F220/18

CPC分类号： A61Q17/00 ,  A61K8/8152 ,  C08F220/18 ,  Y10S526/936

摘要： An acrylic copolymer of ethyl acrylate and methacrylic acid wherein the weight ratio of ethyl acrylate to methacrylic acid is in a range between 75:25 and 95:5, containing therein a residual monomer content of 50 ppm or less, but substantially no surfactants, and which is useful as agents for protecting the skin and manufactured from the following essential components:a. an acrylic copolymer of ethyl acrylate and methacrylic acid wherein the weight ratio of ethyl acrylate to methacrylic acid is in a range between 75:25 and 95:5, containing therein the residual monomers in an amount of 50 ppm or less, but substantially no surfactants . . . approximately 2 to 10%;b. cellulose derivative . . . approximately 0.2 to 2%; andc. a necessary amount of an aqueous alcohol to make the whole 100%.

摘要翻译： 丙烯酸乙酯和甲基丙烯酸的丙烯酸共聚物，其中丙烯酸乙酯与甲基丙烯酸的重量比在75:25至95:5的范围内，其中残留单体含量为50ppm以下，但基本上不含表面活性剂， 其可用作保护皮肤并由以下基本组分制成的试剂：a。 丙烯酸乙酯和甲基丙烯酸的丙烯酸共聚物，其中丙烯酸乙酯与甲基丙烯酸的重量比在75:25至95:5的范围内，其中残留单体的含量为50ppm或更低，但基本上不含表面活性剂 。 。 。 约2至10％; b。 纤维素衍生物。 。 。 约0.2〜2％; 和c。 必需量的含水酒精使整体达到100％。

公开(公告)号：US4915940A

公开(公告)日：1990-04-10

申请号：US271304

申请日：1988-11-15

申请人： Izumi Saitoh ,  Kaori Ikeda ,  Yoshio Doi ,  Shohei Egawa

发明人： Izumi Saitoh ,  Kaori Ikeda ,  Yoshio Doi ,  Shohei Egawa

IPC分类号： A61K9/70 ,  A61K31/27 ,  A61P31/04 ,  A61P31/10

CPC分类号： A61K31/27 ,  A61K9/7015

摘要： Film-formation-type antifungal preparations for external application, consisting essentially of about 0.1% to about 1.5% of tolnaphtate, about 10% to about 20% of a dimethylaminoethyl methacrylate-methacrylic acid ester copolymer and 0.5% to about 10% of a medium chain fatty acid ester in an alcoholic solvent but containing practically no water.

公开(公告)号：US4775667A

公开(公告)日：1988-10-04

申请号：US911151

申请日：1986-09-24

申请人： Izumi Saitoh ,  Hirokuni Jyoyama ,  Fujio Asanuma ,  Katsumi Hirose ,  Shohei Egawa

发明人： Izumi Saitoh ,  Hirokuni Jyoyama ,  Fujio Asanuma ,  Katsumi Hirose ,  Shohei Egawa

IPC分类号： A61K31/045 ,  A61K9/08 ,  A61K9/12 ,  A61K9/70 ,  A61K31/57 ,  A61K31/60 ,  A61P25/04 ,  A61P29/00 ,  A61P43/00 ,  A61K31/605

CPC分类号： A61K9/12

摘要： Topical analgesic anti-inflammatory compositions containing a corticosteroid in addition to the conventional efficacy-proven ingredients are disclosed. They may be embodied in an aerosol, a solution and any other type of composition being convenient for administration. More than the sum of effects of the individual ingredients has been proved. In other words, the effects of the salicylate esters and L-menthol are synergistically enhanced by the addition of the corticosteroid. Particularly, the persistency of the analgesic/anti-inflammatory effects of the conventional ingredients has been proved to be dependent upon the the concentration of the corticosteroid in the composition.

摘要翻译： 公开了除常规有效验证的成分之外含有皮质类固醇的局部止痛抗炎组合物。 它们可以以气溶胶，溶液和任何其它类型的组合物来实施，其方便施用。 超过了各种成分的影响总和已被证明。 换句话说，水杨酸酯和L-薄荷醇的作用通过添加皮质类固醇协同增强。 特别地，常规成分的镇痛/抗炎作用的持续性已被证明取决于组合物中皮质类固醇的浓度。