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1. 发明授权

US06956132B2 Process for producing 2-phenylacetophenone derivatives and precursors therefor 失效
标题翻译：制备2-苯基苯乙酮衍生物及其前体的方法
公开(公告)号：US06956132B2
公开(公告)日：2005-10-18
申请号：US10485615
申请日：2002-07-15
申请人： Takeshi Ohshima , Shigeyuki Nishimura , Takayoshi Ando
发明人： Takeshi Ohshima , Shigeyuki Nishimura , Takayoshi Ando
IPC分类号： C07C45/42 , C07C45/51 , C07C49/813 , C07C49/76 , C07C211/00
CPC分类号： C07C49/813 , C07C45/42 , C07C45/516
摘要： A process for producing 2-phenylacetophenone derivatives represented by the formula (I): (wherein X is an alkyl group or a haloalkyl group, and Y is a hydrogen atom, a halogen atom or an alkyl group which may be substituted), which comprises reacting a compound represented by the formula (II): (wherein X and Y are as defined above, and R is a hydrogen atom or an alkyl group) with an acid.
摘要翻译：一种制备由式（I）表示的2-苯基苯乙酮衍生物的方法：（其中X是烷基或卤代烷基，Y是氢原子，卤原子或可被取代的烷基），其包括与式（II）表示的化合物（其中X和Y如上定义，R是氢原子或烷基）与酸反应。

2. 发明授权

US08338612B2 Process for producing toluidine compound 有权
标题翻译：甲苯胺化合物的制备方法
公开(公告)号：US08338612B2
公开(公告)日：2012-12-25
申请号：US12671050
申请日：2008-07-29
申请人： Shigeo Murai , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
发明人： Shigeo Murai , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
IPC分类号： C07D213/74
CPC分类号： C07D213/72
摘要： Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.
摘要翻译：由于氟啶胺作为农药的有效成分是优异的，而且是非常有用的，因此希望能以低成本的环境友好的方式以简单的操作以适当的形式有效地生产。通过使用工业上有利的反应体系，通过使用包括（1）在碱组分，选自酮，腈的溶剂存在下使ACTF和DCDNBTF反应的步骤，以简单的操作获得所需产物，醚和酯和足够量的水以基本上溶解碱组分，（2）用酸中和或酸化反应混合物的步骤和（3）通过蒸馏从包含氟啶胺的混合物中除去溶剂的步骤为反应产物和反应溶剂使产物析出晶体。

3. 发明申请

US20100197930A1 PROCESS FOR PRODUCING TOLUIDINE COMPOUND 有权
标题翻译：生产托洛芬化合物的方法
公开(公告)号：US20100197930A1
公开(公告)日：2010-08-05
申请号：US12671050
申请日：2008-07-29
申请人： Shigeo Murai , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
发明人： Shigeo Murai , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
IPC分类号： C07D213/36
CPC分类号： C07D213/72
摘要： Because fluazinam is excellent as an active ingredient of pesticides and highly useful, it is desired to produce it efficiently in a proper form with simple operations at low cost in an environmentally friendly manner. The desired product is obtained in good yields with simple operations by using industrially advantageous reaction systems by a process comprising (1) a step of reacting ACTF and DCDNBTF in the presence of an alkali component, a solvent selected from the group consisting of ketones, nitriles, ethers and esters and a sufficient amount of water to substantially dissolve the alkali component, (2) a step of neutralizing or acidifying the reaction mixture with an acid and (3) a step of removing the solvent by distillation from the mixture containing fluazinam as the reaction product and the reaction solvent to precipitate crystals the product.
摘要翻译：由于氟啶胺作为农药的有效成分是优异的，而且是非常有用的，因此希望能以低成本的环境友好的方式以简单的操作以适当的形式有效地生产。通过使用工业上有利的反应体系，通过使用包括（1）在碱组分，选自酮，腈的溶剂存在下使ACTF和DCDNBTF反应的步骤，以简单的操作获得所需产物，醚和酯和足够量的水以基本上溶解碱组分，（2）用酸中和或酸化反应混合物的步骤和（3）通过蒸馏从包含氟啶胺的混合物中除去溶剂的步骤为反应产物和反应溶剂使产物析出晶体。

4. 发明授权

US5023336A Imidazole compound and process for preparing the same 失效
标题翻译：咪唑化合物及其制备方法
公开(公告)号：US5023336A
公开(公告)日：1991-06-11
申请号：US424630
申请日：1989-10-20
申请人： Itaru Shigehara , Toshio Nakajima , Shigeyuki Nishimura , Takeshi Ohshima
发明人： Itaru Shigehara , Toshio Nakajima , Shigeyuki Nishimura , Takeshi Ohshima
IPC分类号： A01N43/50 , C07D233/90 , C07F7/08
CPC分类号： C07D233/90 , C07F7/0812
摘要： An imidazole compound is disclosed, which is represented by formula (I): ##STR1## wherein: X represents a --COOT group, in which T represents a hydrogen atom, an alkyl group, a benzyl group, or a phenyl group; or a --CONH.sub.2 group,Y represents a hydrogen atom, a chlorine atom, or a bromine atom,Z represents an alkyl group containing from 2 to 6 carbon atoms, which may be substituted with one or more halogen atoms; or a phenyl group which may be substituted with one or more halogen atoms or alkyl groups, andQ represents a hydrogen atom; an --SO.sub.2 R.sup.1 group, in which R.sup.1 represents an alkyl group, a dialkylamino group, or a phenyl group which may be substituted with one or more alkyl groups; or a --CH(R.sup.2)(R.sup.3) group, in which R.sup.2 represents a hydrogen atom, a methyl group, or an alkoxy group, and R.sup.3 represents an alkoxy group, an --OCH.sub.2 CH.sub.2 Si (CH.sub.3) group, or a phenyl group which may be substituted with one or more alkyl groups or alkoxy groups,provided that when Y and Q each represents a hydrogen atom and Z represents a phenyl group, X represents a group other than a --COOH-phenyl group, and a --CONH.sub.2 group; and that when Y and Q each represents a hydrogen atom and Z represents an n--C.sub.5 H.sub.11 group, X represents a group other than a --COOH group and a --COOC.sub.2 H.sub.5 group.Processes for preparing imidazole compounds are also disclosed.The imidazole compounds are useful as an intermediate for production of biocides for controlling harmful organisms in the agricultural and horticultural areas, or medical and pharmaceutical fungicides.

5. 发明申请

US20110021774A1 METHOD FOR PRODUCING PYRIMIDINE COMPOUND 有权
标题翻译：生产吡啶化合物的方法
公开(公告)号：US20110021774A1
公开(公告)日：2011-01-27
申请号：US12933980
申请日：2009-04-16
申请人： Shigeo Murai , Ryoji Koto , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takao Awazu , Hisayoshi Jonishi , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
发明人： Shigeo Murai , Ryoji Koto , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takao Awazu , Hisayoshi Jonishi , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
IPC分类号： C07D401/12 , C07D239/42
CPC分类号： C07D239/42 , C07D239/52 , C07D401/12
摘要： To provide a method for producing pyrimidine compound useful as an intermediate for agricultural chemicals or pharmaceuticals, which is simple in operation, presents high yield and produces only a small amount of by-products.The method comprises reacting a compound represented by the formula (I) with a compound represented by the formula (II) in the presence of a pyridine compound to produce a compound represented by the formula (III), a compound represented by the formula (IV) or their mixture.
摘要翻译：提供一种制造用作农药或药物中间体的嘧啶化合物的方法，其操作简单，产率高，仅产生少量副产物。该方法包括使式（I）表示的化合物与式（II）表示的化合物在吡啶化合物的存在下反应，制得由式（III）表示的化合物，式（IV）表示的化合物）或它们的混合物。

6. 发明授权

US08440824B2 Method for producing pyrimidine compound 有权
标题翻译：制备嘧啶化合物的方法
公开(公告)号：US08440824B2
公开(公告)日：2013-05-14
申请号：US12933980
申请日：2009-04-16
申请人： Shigeo Murai , Ryoji Koto , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takao Awazu , Hisayoshi Jonishi , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
发明人： Shigeo Murai , Ryoji Koto , Hiroshi Yoshizawa , Takeshi Ohshima , Katsuyoshi Murakami , Takao Awazu , Hisayoshi Jonishi , Takayoshi Ando , Tadashi Nakamura , Norio Adachi , Akihiko Isogai
IPC分类号： C07D239/02
CPC分类号： C07D239/42 , C07D239/52 , C07D401/12
摘要： To provide a method for producing pyrimidine compound useful as an intermediate for agricultural chemicals or pharmaceuticals, which is simple in operation, presents high yield and produces only a small amount of by-products.The method comprises reacting a compound represented by the formula (I) with a compound represented by the formula (II) in the presence of a pyridine compound to produce a compound represented by the formula (III), a compound represented by the formula (IV) or their mixture.
摘要翻译：提供一种制造用作农药或药物中间体的嘧啶化合物的方法，其操作简单，产率高，仅产生少量副产物。该方法包括使式（I）表示的化合物与式（II）表示的化合物在吡啶化合物的存在下反应，制得由式（III）表示的化合物，式（IV）表示的化合物）或它们的混合物。

7. 发明授权

US6008224A Pyrimidine derivatives 失效
标题翻译：嘧啶衍生物
公开(公告)号：US6008224A
公开(公告)日：1999-12-28
申请号：US849725
申请日：1997-06-27
申请人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Hiroyuki Sonoki , Masami Shiratsuchi
发明人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Hiroyuki Sonoki , Masami Shiratsuchi
IPC分类号： C07D239/69 , C07D401/04 , A61K31/505
CPC分类号： C07D239/69
摘要： The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## [wherein R.sup.1 represents a lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要翻译： PCT No.PCT / JP95 / 02605 Sec。 371日期：1997年6月27日 102（e）日期1997年6月27日PCT 1995年12月19日PCT公布。公开号WO96 / 20177 PCT 日期：1996年7月4日本发明涉及下述式（1）所示的嘧啶衍生物或其衍生物的盐：其中R1表示低级烷基; R 2和R 3各自表示H，烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基，-OR 7或-NR 8 R 9; 并且n是0和3之间的数字（其中R7，R8和R9各自表示H，烷基，芳基，芳烷基，氨基，杂环等）]，以及含有该衍生物或盐作为活性成分。本发明化合物对内皮素具有强烈的结合抑制活性，具有强烈的血管收缩作用和细胞增殖作用。因此，该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。

8. 发明申请

US20080021018A1 (S)-(-)-1-(4-Fluoroisoquinolin-5-Yl)Sulfonyl-2-Methyl-1,4-Homopiperazine Hydrochloride Dihydrate 有权
标题翻译：（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐二水合物
公开(公告)号：US20080021018A1
公开(公告)日：2008-01-24
申请号：US11720288
申请日：2005-11-29
申请人： Takeshi Ohshima , Hiroyoshi Hidaka , Masami Shiratsuchi , Kazuhiro Onogi , Toshiaki Oda
发明人： Takeshi Ohshima , Hiroyoshi Hidaka , Masami Shiratsuchi , Kazuhiro Onogi , Toshiaki Oda
IPC分类号： A61K31/551 , A61P9/00 , C07D243/08
CPC分类号： C07D401/12
摘要： The present invention is directed to (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride dihydrate, to a method producing the dihydrate, and to a drug composition containing the dihydrate. The compound of the present invention has less hygroscopicity as compared with (S)-(−)-1-(4-fluoroisoquinolin-5-yl)sulfonyl-2-methyl-1,4-homopiperazine hydrochloride anhydrous crystals and thus, exhibits excellent chemical stability.
摘要翻译：本发明涉及（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐二水合物，生产二水合物的方法和药物含有二水合物的组合物。与（S） - （ - ） - 1-（4-氟异喹啉-5-基）磺酰基-2-甲基-1,4-高哌嗪盐酸盐无水晶体相比，本发明的化合物具有较少的吸湿性，化学稳定性。

9. 发明授权

US06730147B2 Surface treating agent for ligneous floorings and process for manufacturing the same 有权
标题翻译：木质地板用表面处理剂及其制造方法
公开(公告)号：US06730147B2
公开(公告)日：2004-05-04
申请号：US10016104
申请日：2001-12-17
申请人： Taizo Noda , Daijiro Ohtani , Takeshi Ohshima
发明人： Taizo Noda , Daijiro Ohtani , Takeshi Ohshima
IPC分类号： C09G108
CPC分类号： C09G1/08
摘要： There is provided a surface treating agent for ligneous floorings that makes the surface of a treated floor resistant to slipping and thus is capable of preventing tumbling. The surface treating agent for ligneous floorings contains a drying oil, Japan wax, candelilla wax, and powdery carnauba wax.
摘要翻译：提供了一种用于木质地板的表面处理剂，其使处理后的地板的表面具有滑动性，因此能够防止翻滚。用于木质地板的表面处理剂含有干性油，日本蜡，小烛树蜡和粉状巴西棕榈蜡。

10. 发明授权

US5883092A Pyrimidine derivatives as endothelin antagonists 失效
标题翻译：嘧啶衍生物作为内皮素拮抗剂
公开(公告)号：US5883092A
公开(公告)日：1999-03-16
申请号：US29244
申请日：1998-03-04
申请人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Tetsuya Ishikawa , Hiroyuki Sonoki , Masami Shiratsuchi
发明人： Mitsuteru Hirata , Takeo Deushi , Yoshio Takahashi , Masahiro Tamura , Takeshi Ohshima , Toshiaki Oda , Tetsuya Ishikawa , Hiroyuki Sonoki , Masami Shiratsuchi
IPC分类号： C07D403/04 , A61K31/506 , A61P9/00 , A61P9/12 , C07D213/00 , C07D239/52 , C07D239/545 , C07D295/00 , C07D401/14 , C07D413/04 , A61K31/505 , A61K31/535
CPC分类号： C07D239/52
摘要： The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## �wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.
摘要翻译： PCT No.PCT / JP96 / 02494 Sec。 371日期：1998年3月4日 102（e）1998年3月4日PCT PCT 1996年9月4日PCT公布。公开号WO97 / 09318 日期1997年3月13日本发明涉及下式（1）的嘧啶衍生物或衍生物的盐：其中R1表示羟基，低级烷氧基，苯氧基其可以具有取代基，可以具有取代基的芳烷氧基或-NR2R3; X表示氧原子或N-R4; m为2或3; n为1或2（式中，R2，R3各自相同或不同，表示氢原子，羟基，可具有取代基的低级烷基，可具有取代基的苯基，取代基，可以具有取代基的芳烷基或可以具有取代基的杂环基; R4表示低级烷基，苯基，甲酰基或低级烷氧基羰基）]以及药物含有衍生物或盐作为活性成分。该化合物对具有强烈血管收缩作用的内皮素表现出强烈的结合抑制活性。因此，该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。

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