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1. 发明授权

US4266067A Process for preparing thiophene derivatives 失效
标题翻译：制备噻吩衍生物的方法
公开(公告)号：US4266067A
公开(公告)日：1981-05-05
申请号：US110331
申请日：1980-01-07
申请人： Tamotsu Fujisawa , Kiyoshi Kondo , Kunikazu Sakai
发明人： Tamotsu Fujisawa , Kiyoshi Kondo , Kunikazu Sakai
IPC分类号： C07D333/12 , C07D333/16 , C07D333/22 , C07D333/24 , C07D333/28
CPC分类号： C07D333/22 , C07D333/12 , C07D333/16 , C07D333/24 , C07D333/28
摘要： Process for the preparation of a series of thiophene derivatives, from which 2-thiopheneacetic acid derivatives can easily be prepared, in high yields and selectivity by using substituted or unsubstituted 2-acetylthiophenes as the starting materials by easy operations. 2-Thiopheneacetic acid derivatives are very useful compounds as the chemical modifier of penicillin and cephalosporin. In the course of the reaction, 2-(dihaloacetyl)thiophenes are formed which are valuable intermediates for the production of not only 2-thiopheneacetic acids but also thioprofenic acid which is known as an anti-inflammatory agent.
摘要翻译：通过使用取代或未取代的2-乙酰基噻吩作为起始原料，通过简单的操作，可以高产率和选择性制备可以容易地制备2-噻吩乙酸衍生物的一系列噻吩衍生物的方法。 2-噻吩乙酸衍生物作为青霉素和头孢菌素的化学修饰剂是非常有用的化合物。在反应过程中，形成了2-（二卤乙酰基）噻吩，它们是生产不仅2-噻吩乙酸的有价值的中间体，而且也被称为抗炎剂的硫代甲酸。

2. 发明授权

US4219659A Process for the preparation of thiophene derivatives and thiophene derivatives obtained therethrough 失效
标题翻译：制备噻吩衍生物和噻吩衍生物的方法
公开(公告)号：US4219659A
公开(公告)日：1980-08-26
申请号：US910290
申请日：1978-05-30
申请人： Tamotsu Fujisawa , Kunikazu Sakai , Akira Kurebayashi
发明人： Tamotsu Fujisawa , Kunikazu Sakai , Akira Kurebayashi
IPC分类号： C07D333/16 , C07D333/22 , C07D333/24 , C07D333/28
CPC分类号： C07D333/16 , C07D333/22 , C07D333/24
摘要： An .alpha.-(2-thienyl)propionic acid can easily be prepared in a high yield and high selectivity by reacting a 2-(dihaloacetyl)thiophene which is easily obtainable by acetylation and halogenation of a substituted or unsubstutitued thiophene, with a methylmetal compound and then reacting an alkali metal hydroxide with the reaction product. .alpha.-(2-Thienyl)propionic acids are useful compounds from which, for example, thioprofenic acid can easily be prepared. Thioprofenic acid is known as an anti-inflammatory agent. As reaction intermediates, 1-(2-thienyl)-1-dihalomethylethanols can be obtained. Which are novel and useful compounds.
摘要翻译：通过使易于获得的取代或未取代的噻吩的乙酰化和卤化的2-（二卤代乙酰基）噻吩与甲基金属化合物反应，可以以高产率和高选择性制备α-（2-噻吩基）丙酸，和然后使碱金属氢氧化物与反应产物反应。 α-（2-噻吩基）丙酸是有用的化合物，其中例如可以容易地制备硫代丙烯酸。硫代丙酸被称为抗炎剂。作为反应中间体，可以得到1-（2-噻吩基）-1-二卤代甲基乙醇。哪些是新颖有用的化合物。

3. 发明授权

US4431659A 1-(Aryl)thiocarbamoyl-2-(aryl)-3-pyrazolidinones and their nematicidal use 失效
标题翻译： 1-（芳基）硫代氨基甲酰基-2-（芳基）-3-吡唑烷酮及其杀线虫用途
公开(公告)号：US4431659A
公开(公告)日：1984-02-14
申请号：US426470
申请日：1982-09-29
申请人： Kunikazu Sakai , Minoru Suda , Kiyoshi Kondo
发明人： Kunikazu Sakai , Minoru Suda , Kiyoshi Kondo
IPC分类号： A01N47/38 , C07D231/08 , C07D231/06
CPC分类号： A01N47/38 , C07D231/08
摘要： Compounds of the general formula ##STR1## their method of preparation, and their use to control nematodes in agricultural crops are disclosed and exemplified.
摘要翻译：通式（Ⅰ）的化合物及其制备方法及其在农作物中控制线虫的用途被公开和例示。

4. 发明授权

US06498164B1 Barbituric acid derivative and preventive and therapeutic agent for bone and cartilage containing the same 失效
标题翻译：巴比妥酸衍生物和含有相同的骨和软骨的预防和治疗剂
公开(公告)号：US06498164B1
公开(公告)日：2002-12-24
申请号：US09647280
申请日：2000-10-19
申请人： Kunikazu Sakai , Yusuke Satoh
发明人： Kunikazu Sakai , Yusuke Satoh
IPC分类号： A61K31515
CPC分类号： C07D409/06 , C07D239/62
摘要： A compound of the formula wherein the substituents are as defined in the specification and solvates and salts thereof useful for treating bone and cartilage diseases.
摘要翻译：取代基中的取代基的化合物如说明书中所定义，并且可用于治疗骨和软骨疾病的溶剂化物和盐。

5. 发明授权

US06177474B1 Polyhydroxyphenol derivatives and preventive and therapeutic agents for bone and cartilage diseases containing the same 失效
标题翻译：聚羟基苯酚衍生物以及含有其的骨和软骨疾病的预防和治疗剂
公开(公告)号：US06177474B1
公开(公告)日：2001-01-23
申请号：US09180756
申请日：1998-12-10
申请人： Kunikazu Sakai , Yusuke Satoh , Kazuyuki Doi , Kazuyuki Kitamura
发明人： Kunikazu Sakai , Yusuke Satoh , Kazuyuki Doi , Kazuyuki Kitamura
IPC分类号： A61K3112
CPC分类号： C07C49/84 , C07C45/00 , C07C45/46 , C07C45/512 , C07C45/62 , C07C45/68 , C07C45/71 , C07C49/713 , C07C49/743 , C07C49/747 , C07C49/825 , C07C49/83 , C07C49/835
摘要： Compounds useful as preventive and therapeutic agents for bone and cartilage diseases; and drug compositions containing the same. The compounds are polyhydroxyphenol derivatives of general formula (I) and quinione analogues derived therefrom (wherein R1 is alkyl, optionally substituted benzyl or optionally substituted aryl; R2 is hydrogen, alkyl, alkenyl or optionally substituted benzyl; R3 is hydrogen, alkyl, alkenyl, optionally substituted benzyl, hydroxyl, alkoxy, alkenyloxy or optionally substituted benzyloxy; R4 is hydrogen, alkyl, alkenyl, optionally substituted benzyl or hydroxyl; and R5 and R6 are each independently hydrogen, alkyl, alkenyl or optionally substituted benzyl). The polyhydroxyphenol derivatives and the quinone analogues exhibit a potent inhibitory activity against bone resorption and are useful as preventive and therapeutic agents for bone and cartilage diseases.
摘要翻译：用作骨和软骨疾病的预防和治疗剂的化合物; 和含有它们的药物组合物。化合物是通式（I）的多羟基苯酚衍生物和由其衍生的醌基类似物（其中R1是烷基，任意取代的苄基或任意取代的芳基; R 2是氢，烷基，烯基或任选取代的苄基; R 3是氢，烷基，链烯基，任选取代的苄基，羟基，烷氧基，烯氧基或任选取代的苄氧基; R 4是氢，烷基，烯基，任选取代的苄基或羟基;且R 5和R 6各自独立地为氢，烷基，烯基或任选取代的苄基。多羟基苯酚衍生物和醌类似物表现出对骨吸收的有效抑制活性，并且可用作骨和软骨疾病的预防和治疗剂。

6. 发明授权

US6100219A Plant growth accelerator 失效
标题翻译：植物生长促进剂
公开(公告)号：US6100219A
公开(公告)日：2000-08-08
申请号：US117937
申请日：1998-11-30
申请人： Kunikazu Sakai , Yasuo Kamuro , Hiroki Kuriyama
发明人： Kunikazu Sakai , Yasuo Kamuro , Hiroki Kuriyama
IPC分类号： A01N37/36 , A01N43/12 , A01N43/28 , A01N45/00 , A01N49/00 , A01N63/00 , A01N43/16 , A01N43/20
CPC分类号： A01N43/12 , A01N45/00 , A01N49/00
摘要： The present invention provides a plant growth promoter comprising an epoxycylohexane derivative represented by the general formula: ##STR1## (wherein by R.sup.1 represents a hydrogen atom, C1 to C6 alkyl group or C3 to C6 cycloalkyl group, and R.sup.2 and R.sup.3 are independently lower alkyl groups or are combined to form a polymethylene group which may be substituted with an alkyl group) and gibberellin as active ingredients.
摘要翻译： PCT No.PCT / JP97 / 00315 Sec。 371日期：1998年11月30日 102（e）1998年11月30日日期PCT 1997年2月7日提交PCT公布。公开号WO97 / 28690 日期：1997年8月14日本发明提供一种植物生长促进剂，其包含由通式表示的环氧环己烷衍生物（其中，R1表示氢原子，C1〜C6烷基或C3〜C6环烷基，R2和R3独立地表示低级烷基或被结合形成可被烷基取代的聚亚甲基）和赤霉素作为活性成分。

7. 发明授权

US5965488A Plant growth regulating composition comprising epoxycyclohexane derivatives and brassinosteroids as well as method of regulating plant growth comprising the application thereof 失效
标题翻译：包含环氧环己烷衍生物和油菜素类固醇的植物生长调节组合物以及调节植物生长的方法包括其应用
公开(公告)号：US5965488A
公开(公告)日：1999-10-12
申请号：US66805
申请日：1998-04-24
申请人： Kunikazu Sakai , Yasuo Kamuro , Suguru Takatsuto , Tsuyoshi Watanabe , Hiroki Kuriyama
发明人： Kunikazu Sakai , Yasuo Kamuro , Suguru Takatsuto , Tsuyoshi Watanabe , Hiroki Kuriyama
IPC分类号： A01N37/06 , A01N37/38 , A01N43/20 , A01N43/22 , A01N43/30 , A01N43/90 , A01P21/00 , C07D303/38 , C07D303/40 , C07D493/10 , C07J73/00
CPC分类号： C07D493/10 , A01N43/20 , A01N43/22 , A01N43/30 , A01N43/90 , C07D303/40
摘要： The present invention relates to a plant growth regulator comprising as an active ingredient an epoxycyclohexane derivative represented by general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or C.sub.3 -C.sub.6 cycloalkyl group, and R.sup.2 and R.sup.3 are independently C.sub.1 -C.sub.6 alkyl groups or are combined to form a C.sub.2 -C.sub.3 polymethylene group which may be substituted with a C.sub.1 -C.sub.6 alkyl group, as well as to a plant growth regulator comprising the epoxycyclohexane derivative and a brassinosteroid as active ingredients. The epoxycyclohexane derivatives exhibit a potent plant growth regulating action which is equivalent to or higher than that of abscisic acid, and are useful as plant growth regulators such as a plant growth accelerator, a germination growth accelerator, a transpiration and wilting inhibitor, a cold resistance enhancer, an accelerator for growing, thickening or maturing fruits, roots, stems or bulbs, etc. A synergistic effect is achieved by combination of the epoxycyclohexane derivative with a brassinosteroid.
摘要翻译：本发明涉及一种植物生长调节剂，其包含通式（1）表示的环氧环己烷衍生物作为活性成分：其中R1为氢原子，C1-C6烷基或C3-C6环烷基，R2和R3为独立地是C 1 -C 6烷基或被组合以形成可以被C 1 -C 6烷基取代的C 2 -C 3多亚甲基，以及包含环氧环己烷衍生物和油菜素内固体作为活性成分的植物生长调节剂。环氧环己烷衍生物表现出与脱落酸相当或更高的有效的植物生长调节作用，并且可用作植物生长调节剂如植物生长促进剂，发芽生长促进剂，蒸腾和萎ting抑制剂，耐寒性增强剂，用于生长，增稠或成熟果实，根，茎或鳞茎等的促进剂。通过环氧环己烷衍生物与油菜素内酯类固醇的组合来实现协同效应。

8. 发明授权

US4540794A Method for preparing 5-mercapto-1,2,3-thiadiazole salts 失效
标题翻译： 5-巯基-1,2,3-噻二唑盐的制备方法
公开(公告)号：US4540794A
公开(公告)日：1985-09-10
申请号：US532922
申请日：1983-09-16
申请人： Kunikazu Sakai , Daiei Tunemoto , Takeo Kobori , Kiyosi Kondo
发明人： Kunikazu Sakai , Daiei Tunemoto , Takeo Kobori , Kiyosi Kondo
IPC分类号： C07D249/04 , C07D249/06 , C07D285/06
CPC分类号： C07D285/06 , C07D249/04 , C07D249/06
摘要： A method for preparing a 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I) is disclosed: ##STR1## the method comprises the steps of: providing a sulfonylhydrazone derivative represented by the general formula (II): ##STR2## providing a sulfide represented by the general formula (III):M--S--M' (III)(wherein R is an aryl group, X is a chlorine or bromine atom, M is an alkali metal atom and M' is a hydrogen atom or an alkali metal atom);combining the sulfonylhydrazone derivative represented by the general formula (II) and the sulfide represented by the general formula (III) and allowing a reaction to occur; andobtaining the 5-mercapto-1,2,3-thiadiazole salt represented by the general formula (I).
摘要翻译：公开了制备由通式（I）表示的5-巯基-1,2,3-噻二唑盐的方法：（I）该方法包括以下步骤：提供由通式（I）表示的磺酰腙衍生物（II）：提供由通式（III）表示的硫化物的化合物（II）：MS-M'（III）（其中R是芳基，X是氯或溴原子，M是碱金属原子和M'是氢原子或碱金属原子）; 将由通式（II）表示的磺酰腙衍生物与由通式（III）表示的硫化物组合并进行反应; 得到通式（I）表示的5-巯基-1,2,3-噻二唑盐。

9. 发明授权

US5801123A Epoxycyclohexane derivative and plant growth regulator 失效
标题翻译：环氧环己烷衍生物和植物生长调节剂
公开(公告)号：US5801123A
公开(公告)日：1998-09-01
申请号：US809051
申请日：1997-03-13
申请人： Kunikazu Sakai , Yasuo Kamuro , Suguru Takatsuto , Tsuyoshi Watanabe , Hiroki Kuriyama
发明人： Kunikazu Sakai , Yasuo Kamuro , Suguru Takatsuto , Tsuyoshi Watanabe , Hiroki Kuriyama
IPC分类号： A01N37/06 , A01N37/38 , A01N43/20 , A01N43/22 , A01N43/30 , A01N43/90 , A01P21/00 , C07D303/38 , C07D303/40 , C07D493/10 , C07J73/00
CPC分类号： C07D493/10 , A01N43/20 , A01N43/22 , A01N43/30 , A01N43/90 , C07D303/40
摘要： The present invention relates to a plant growth regulator comprising as an active ingredient an epoxycyclohexane derivative represented by general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.6, alkyl group or C.sub.3 -C.sub.6 cycloalkyl group, and R.sup.2 and R.sup.3 are independently C.sub.1 -C.sub.6 alkyl groups or are combined to form a C.sub.2 -C.sub.3 polymethylene group which may be substituted with a C.sub.1 -C.sub.6, alkyl group, as well as to a plant growth regulator comprising the epoxycyclohexane derivative and a brassinosteroid as active ingredients. The epoxycyclohexane derivatives exhibit a potent plant growth regulating action which is equivalent to or higher than that of abscisic acid, and are useful as plant growth regulators such as a plant growth accelerator, a germination growth accelerator, a transpiration and wilting inhibitor, a cold resistance enhancer, an accelerator for growing, thickening or maturing fruits, roots, stems or bulbs, etc.. A synergistic effect is achieved by combination of the epoxycyclohexane derivative with a brassinosteroid.
摘要翻译： PCT No.PCT / JP95 / 01816 Sec。 371日期1997年3月13日 102（e）1997年3月13日PCT PCT 1995年9月13日PCT公布。公开号WO96 / 08481 日期：1996年3月21日本发明涉及一种植物生长调节剂，其包含作为活性成分的通式（1）表示的环氧环己烷衍生物：其中R1是氢原子，C1-C6烷基或C 3 -C 6环烷基，R 2和R 3独立地是C 1 -C 6烷基，或者被结合形成可被C 1 -C 6烷基取代的C 2 -C 3多亚甲基，以及植物生长调节剂包括环氧环己烷衍生物和油菜素类固醇作为活性成分。环氧环己烷衍生物表现出与脱落酸相当或更高的有效的植物生长调节作用，并且可用作植物生长调节剂如植物生长促进剂，发芽生长促进剂，蒸腾和萎ting抑制剂，耐寒性增强剂，用于生长，增稠或成熟果实，根，茎或球茎等的促进剂。通过环氧环己烷衍生物与油菜素内酯类固醇的组合来实现协同效应。

10. 发明授权

US5254694A Optically active epoxycyclohexane derivative and epoxycyclohexanone derivative, and process for the preparation thereof 失效
标题翻译：光学活性环氧环己烷衍生物和环氧环己酮衍生物及其制备方法
公开(公告)号：US5254694A
公开(公告)日：1993-10-19
申请号：US834547
申请日：1992-02-12
申请人： Kunikazu Sakai , Kyoko Takahashi
发明人： Kunikazu Sakai , Kyoko Takahashi
IPC分类号： C07C403/20 , C07D303/38 , C07D303/40 , C07D407/04 , C07D493/10 , C07D303/32 , C07D301/00
CPC分类号： C07D303/38 , C07D303/40 , C07D493/10
摘要： An optically active epoxycyclohexane derivative represented by the general formula: ##STR1## wherein R represents a 4-oxycarbonyl-1-hydroxy-3-methyl-3(Z)-buten-1-yl or 4-hydroxycarbonyl-3-methyl-1(E),3(Z)-butadien-1-yl group; and R.sup.1 and R.sup.2 each represent a lower alkoxy group or together form a 1,3-dioxolane ring together with the carbon atom to which they are bonded,and an enantiometer thereof.An optically active epoxycyclohexanone derivative represented by the general formula: ##STR2## wherein R.sup.3 represents a hydrogen atom or a lower alkyl, allyl, aralkyl or aryl group,and an enantiomer thereof.Further, the process for preparing these compounds, is also disclosed.

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