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111. 发明授权

US4983602A 3'-hydroxybenzoxazinorifamycin derivative, process for preparing the same and antibacterial agent containing the same 失效
标题翻译： 3'-羟基苯并恶嗪利福霉素衍生物，其制备方法和含有该抗体的抗菌剂
公开(公告)号：US4983602A
公开(公告)日：1991-01-08
申请号：US407995
申请日：1989-09-14
申请人： Takehiko Yamane , Takuji Hashizume , Katsuji Yamashita , Kazunori Hosoe , Fumiyuki Kuze , Kiyoshi Watanabe
发明人： Takehiko Yamane , Takuji Hashizume , Katsuji Yamashita , Kazunori Hosoe , Fumiyuki Kuze , Kiyoshi Watanabe
IPC分类号： C07D498/18
CPC分类号： C07D498/18
摘要： A rifamycin derivative having the formula (I): ##STR1## wherein A is a group having the formula: ##STR2## in which R.sup.1 is an alkyl group having 4 or 5 carbon atoms or an alkenyl group having 3 to 5 carbon atoms, or a group having the formula: in which n is 3 or 4; or a pharmaceutically acceptable salt thereof. The rifamycin derivative (I) exhibits a strong antibacterial activity against Gram-positive bacteria and acid-fast bacteria, and also exhibits a strong antibacterial activity against tubercle bacilli.

112. 发明授权

US4962300A Preheating control apparatus for diesel engines 失效
标题翻译：柴油机预热控制装置
公开(公告)号：US4962300A
公开(公告)日：1990-10-09
申请号：US239608
申请日：1981-03-02
申请人： Kiyoshi Watanabe
发明人： Kiyoshi Watanabe
IPC分类号： F02B3/06 , F02P19/02
CPC分类号： F02P19/025 , F02B3/06
摘要： A preheating control apparatus for diesel engines of the present invention is provided wherein the voltage developed across a sensing resistor connected in series with a glow plug, which voltage is indicative of the temperature of the glow plug, is amplified by an amplifier. The amplified voltage is compared with a predetermined reference voltage to control the preheating current through the glow plug so that the temperature of the glow plug can be precisely controlled without increasing the resistance value of the sensing resistor. Further, a protection circuit may be provided to end the preheating current to the glow plug in response to an abnormal change in the voltage applied to the glow plug.
摘要翻译：提供了本发明的柴油发动机的预热控制装置，其中跨越与电热塞串联的感测电阻器产生的电压被放大器放大，该电热塞指示电热塞的温度。将放大的电压与预定的参考电压进行比较，以控制通过电热塞的预热电流，使得可以精确地控制电热塞的温度而不增加感测电阻器的电阻值。此外，可以提供保护电路以响应于施加到电热塞的电压的异常变化而将预热电流结束到电热塞。

113. 发明授权

US4863530A Fc-Pt-Nb permanent magnet with an ultra-high coercive force and a large maximum energy product, and method for producing the same 失效
标题翻译：具有超高矫顽力和大的最大能量积的Fc-Pt-Nb永磁体及其制造方法
公开(公告)号：US4863530A
公开(公告)日：1989-09-05
申请号：US278346
申请日：1988-12-01
申请人： Hakaru Masumoto, deceased , by Hiroshi Matushima, executor , Kiyoshi Watanabe
发明人： Hakaru Masumoto, deceased , by Hiroshi Matushima, executor , Kiyoshi Watanabe
IPC分类号： C21D6/00 , C22C30/00 , C22C38/00 , C22F1/14 , H01F1/04
CPC分类号： C21D6/00 , C22C30/00 , C22F1/14 , H01F1/04
摘要： The disclosed permanent magnet has a coercive force of larger than 500 Oe, a residual magnetic flux density of larger than 5 kG, and a maximum energy product of larger than 2 MGOe, and it consisting essentially of 48.about.66.9 Atm % of iron, 33.about.47 Atm % of platinum, and 0.1.about.10 Atm % of niobium. It includes a crystal structure of an incomplete single .gamma.1 phase of a face-centered tetragonal system due to either the composition thereof or heat treatment applied thereto. The permanent magnet are made by heating an alloy of the above main composition at 900.degree..about.1,400.degree. for one minute to ten hours and quenching the alloy at a high speed of faster than 30.degree. C./minute but slower than 2,000.degree. C./sec.
摘要翻译：所公开的永磁体具有大于500Oe的矫顽力，大于5kG的剩余磁通密度和大于2MGOe的最大能量乘积，并且其基本上由48差异66.9％的铁，33％差异47铂的百分比，和0.1的差异10 Atm％的铌。由于其组成或施加于其上的热处理，它包括面心四方系的不完全单一γ1相的晶体结构。永久磁铁是通过将上述主要组合物的合金在900℃-140℃下加热1分钟至10小时而制成的，并以高于30℃/分钟但低于2000℃的高速淬火该合金。 /秒。

114. 发明授权

US4812406A Process for preparing optically active hydantoins 失效
标题翻译：制备光学活性乙内酰脲的方法
公开(公告)号：US4812406A
公开(公告)日：1989-03-14
申请号：US775090
申请日：1985-09-12
申请人： Satomi Takahashi , Yukio Yamada , Yasuyoshi Ueda , Yasuhiro Katayama , Yoshio Shimada , Kiyoshi Watanabe
发明人： Satomi Takahashi , Yukio Yamada , Yasuyoshi Ueda , Yasuhiro Katayama , Yoshio Shimada , Kiyoshi Watanabe
IPC分类号： C07D233/72 , C07D233/74 , C07D311/68 , C07D317/60 , C07D405/06 , C07D491/10 , C12P17/02 , C12P17/10 , C12P17/18 , C12P41/00 , C12R1/01 , C12R1/07 , C12R1/15 , C12R1/365 , C12P13/04
CPC分类号： C07D405/06 , C07D233/74 , C07D311/68 , C07D317/60 , C07D491/10 , C12P17/02 , C12P17/10 , C12P17/18 , C12P41/009
摘要： A process for preparing optically active hydantoins having the general formula (II): ##STR1## wherein R.sup.1 and R.sup.2, which are different from each other, are independently alkyl group, aralkyl group, aryl group, substituted alkyl group, substituted aralkyl group, or substituted aryl group, or R.sup.1 and R.sup.2 form an asymmetric cyclic compound, characterized in that one configuration of racemic N-carbamoyl-.alpha.-amino acid having the general formula (I): ##STR2## wherein R.sup.1 and R.sup.2 are as above, is enzymatically converted into the corresponding hydantoins.The present invention provides a process for an optical resolution with a high efficiency which can be used for the synthesis of (S)-6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione (USAN; Sorbinil), which is an optically active hydrantoins attracting public attention as a preventive or a remedy for the particular chronic symptoms of diabetes such as cataract and neuropathy, and (S)-.alpha.-methyl-3,4-dihydroxyphenylalanine (L-methyldopa), which is an optically active amino acid widely used as antihypertensives. Further, the present invention provides a novel finding that N-carbamoyl-.alpha.-amino acid having no hydrogen atom on its .alpha.-carbon atom can be biochemically converted into hydantoins by an enzymatic cyclization reaction.
摘要翻译：制备具有通式（II）的光学活性乙内酰脲的方法：其中R1和R2彼此不同，其独立地为烷基，芳烷基，芳基，取代的烷基，取代的芳烷基基团或取代的芳基，或R 1和R 2形成不对称环状化合物，其特征在于具有通式（I）的外消旋N-氨基甲酰基-α-氨基酸的一种构型：其中R1和R2 如上所述，被酶转化成相应的乙内酰脲。本发明提供了可用于（S）-6-氟 - 螺 - [苯并二氢吡喃-4,4'-咪唑烷] -2'，5'-二酮的合成的高效光学拆分方法。（USAN; Sorbinil）是一种光学活性的水解素，引起公众的注意，作为预防或治疗糖尿病的特殊慢性症状如白内障和神经病，以及（S）-α-甲基-3,4-二羟基苯丙氨酸（L 甲基多巴），其是广泛用作抗高血压药物的光学活性氨基酸。此外，本发明提供了一种新的发现，其α-碳原子上不具有氢原子的N-氨基甲酰基-α-氨基酸可以通过酶环化反应生物化学转化成乙内酰脲。

115. 发明授权

US4748176A 7-hydroxyguanine compounds 失效
标题翻译： 7-羟基鸟嘌呤化合物
公开(公告)号：US4748176A
公开(公告)日：1988-05-31
申请号：US867032
申请日：1986-05-27
申请人： Kiyoto Ishii , Hajime Kawaharada , Kiyoshi Watanabe
发明人： Kiyoto Ishii , Hajime Kawaharada , Kiyoshi Watanabe
IPC分类号： A61K31/52 , A61K31/522 , A61P35/00 , C07D473/18 , C12P17/18 , C12R1/465
CPC分类号： C07D473/18
摘要： Novel 7-hydroxyguanine compounds of the formula: ##STR1## wherein R is hydrogen atom, tetrahydropyranyl group or tetrahydrofuryl group, and R.sub.2 is hydrogen atom, tetrahydropyranyl group or tetrahydrofuryl group, provided that when R.sub.1 is hydrogen atom, R.sub.2 is tetrahydropyranyl group or tetrahydrofuryl group, and a salt thereof, which have excellent anti-tumor activity, process for preparing the compounds, and anti-tumor agent containing said compound as an active ingredient.
摘要翻译：下式的新型7-羟基鸟嘌呤化合物：其中R是氢原子，四氢吡喃基或四氢呋喃基，R2是氢原子，四氢吡喃基或四氢呋喃基，条件是当R1是氢原子时，R2是四氢吡喃基基团或四氢呋喃基及其盐，其具有优异的抗肿瘤活性，制备该化合物的方法，以及含有所述化合物作为活性成分的抗肿瘤剂。

116. 发明授权

US4745066A Method for producing optically active glycol derivatives 失效
标题翻译：光学活性二醇衍生物的制备方法
公开(公告)号：US4745066A
公开(公告)日：1988-05-17
申请号：US846766
申请日：1986-04-01
申请人： Shigeki Hamaguchi , Takehisa Ohashi , Kiyoshi Watanabe
发明人： Shigeki Hamaguchi , Takehisa Ohashi , Kiyoshi Watanabe
IPC分类号： C07B31/00 , C07C67/00 , C07C301/00 , C07C303/22 , C07C309/72 , C12P11/00 , C12P41/00 , C12R1/01 , C12R1/38 , C12R1/66 , C12R1/785 , C12R1/845
CPC分类号： C12P41/004 , C07C309/00 , C12P11/00
摘要： A method for producing optically active glycol derivatives by biochemical resolution which comprises contacting a racemic ester of the general formula 1 ##STR1## (wherein R.sub.1 is an aliphatic hydrocarbon group of 1 to 16 carbon atoms, R.sub.2 is an aliphatic hydrocarbon group of 1 to 8 carbon atoms, and R.sub.3 is an aromatic hydrocarbon group such as phenyl, tolyl or naphtyl) with a microorganism- or animal organ-derived enzyme having stereoselective hydrolytic activity to asymmetrically hydrolyze said racemic ester of general formula 1 to produce an optically active alcohol of general formula 2* ##STR2## (wherein R.sub.1 and R.sub.3 have the same meanings as defined above) and an unreacted ester of the general formula 1* ##STR3## (wherein R.sub.1, R.sub.2 and R.sub.3 have the same meanings as defined hereinbefore), separating the optically active compounds from each other, hydrolyzing said ester of general formula 1* to give an optically active glycol derivative which is antipodal to the alcohol of general formula 2* and, then, isolating the same optically active glycol derivative. The invention provides a method for producing optically active glycol derivatives, which is expedient, does not require costly reagents and is suited to commercial scale production.
摘要翻译：一种通过生物化学拆分制备光学活性二醇衍生物的方法，其包括使通式1的外消旋酯1（其中R 1是1至16个碳原子的脂族烃基，R 2是1的脂族烃基， 8个碳原子，并且R 3是芳族烃基如苯基，甲苯基或萘基）与具有立体选择性水解活性的微生物或动物器官衍生的酶不对称地水解所述通式1的外消旋酯以产生光学活性的醇通式2 * 2 *（其中R 1和R 3具有与上述相同的含义）和通式1 *未反应的酯*（其中R 1，R 2和R 3具有与定义相同的含义）将光学活性化合物彼此分离，水解所述通式1 *的酯，得到对通式为醇的对映体的光学活性二醇衍生物 2 *，然后分离相同的光学活性二醇衍生物。本发明提供了一种制备光学活性二醇衍生物的方法，这是有利的，不需要昂贵的试剂并且适于商业规模生产。

117. 发明授权

US4625042A Process for preparing 6-fluoro-4-chromanone using 3-(4-fluorophenoxy)propionitrile 失效
标题翻译：使用3-（4-氟苯氧基）丙腈制备6-氟-4-苯并二氢吡喃酮的方法
公开(公告)号：US4625042A
公开(公告)日：1986-11-25
申请号：US752439
申请日：1985-07-08
申请人： Satomi Takahashi , Yasuyoshi Ueda , Yoshio Shimada , Kiyoshi Watanabe
发明人： Satomi Takahashi , Yasuyoshi Ueda , Yoshio Shimada , Kiyoshi Watanabe
IPC分类号： B01J23/00 , B01J31/02 , C07B61/00 , C07C59/90 , C07C67/00 , C07C253/00 , C07C255/13 , C07C255/53 , C07D311/22 , C07D311/68 , C07C121/75
CPC分类号： C07C255/00 , C07D311/22
摘要： The present invention relates to 3-(4-fluorophenoxy)propionitrile having the formula (I): ##STR1## a process for preparing 3-(4-fluorophenoxy)propionitrile having the formula (I) which comprises reacting 4-fluorophenol and acrylonitrile in the presence of a tertiary amine, a process for preparing 6-fluoro-4-chromanone having the formula (II): ##STR2## which comprises reacting 3-(4-fluorophenoxy)propionitrile having the formula (I) with an acid, and a process for preparing 6-fluoro-4-chromanone having the formula (II) which comprises reacting 4-fluorophenol with acrylonitrile in the presence of a catalyst to give 3-(4-fluorophenoxy)propionitrile having the formula (I), which is then reacted with an acid. 6-Fluoro-4-chromanone is an important intermediate for the synthesis of (S)-2,3-dihydro-6-fluoro-spiro[4H-1-benzopyran-4,4'-imidazolidine]-2',5'dione (USAN: sorbinil).
摘要翻译：本发明涉及具有式（I）的3-（4-氟苯氧基）丙腈：（I）制备具有式（I）的3-（4-氟苯氧基）丙腈的方法，该方法包括使4-氟苯酚（II）的6-氟-4-苯并二氢吡喃酮的制备方法：包括使具有式（I）的3-（4-氟苯氧基）丙腈与式）和用于制备具有式（II）的6-氟-4-苯并二氢吡喃酮的方法，其包括在催化剂存在下使4-氟苯酚与丙烯腈反应，得到具有式（II）的3-（4-氟苯氧基）丙腈（I），然后与酸反应。 6-氟-4-苯并二氢吡喃酮是合成（S）-2,3-二氢-6-氟 - 螺[4H-1-苯并吡喃-4,4'-咪唑烷] -2'，5' 二酮（USAN：sorbinil）。

118. 发明授权

US4455637A Disc record player with automatic loading/unloading assembly 失效
标题翻译：光盘录音机带自动装卸装置
公开(公告)号：US4455637A
公开(公告)日：1984-06-19
申请号：US286467
申请日：1981-07-24
申请人： Hiroyuki Suzuki , Masayuki Taoka , Kiyoshi Watanabe
发明人： Hiroyuki Suzuki , Masayuki Taoka , Kiyoshi Watanabe
IPC分类号： G11B3/095 , G11B17/028 , G11B17/04 , G11B19/20 , G11B25/04 , G11B1/00 , G11B3/60 , G11B17/02
CPC分类号： G11B17/0284 , G11B17/0404 , G11B19/20 , G11B3/0955
摘要： A record player is disclosed which includes a turntable (35) movable at least between a first position for record loading and a second position for record unloading, a record support (10R) having at least a first position for removal of the record out of said player and a second position for mounting the record onto said turntable and a transmission device (13a) maintained in engaging relationship with said turntable for transmission of rotating torque from said turntable to said record support when said turntable is in the second position.
摘要翻译：公开了一种记录播放器，其包括至少在用于记录装载的第一位置和用于记录卸载的第二位置之间可移动的转盘（35），具有至少第一位置的记录支架（10R），用于从所述播放器和用于将记录安装到所述转盘上的第二位置和与所述转台保持啮合关系的传动装置（13a），用于当所述转盘处于第二位置时将转动扭矩从所述转台传递到所述记录支架。

119. 发明授权

US4369177A Stable composition of S-adenosyl-L-methionine 失效
标题翻译： S-腺苷-L-甲硫氨酸的稳定组成
公开(公告)号：US4369177A
公开(公告)日：1983-01-18
申请号：US208842
申请日：1980-11-20
申请人： Yuichi Kozaki , Shingo Hata , Hajime Kawaharada , Kiyoshi Watanabe
发明人： Yuichi Kozaki , Shingo Hata , Hajime Kawaharada , Kiyoshi Watanabe
IPC分类号： C07H19/16 , A61K31/70
CPC分类号： C07H19/16 , Y10S514/97 , Y10S514/973
摘要： A stable composition of S-adenosyl-L-methionine is disclosed which includes a salt of S-adenosyl-L-methionine and a pharmaceutically acceptable, water-soluble salt of a bivalent or trivalent metal. The salt of S-adenosyl-L-methionine is, for example, a salt of S-adenosyl-L-methionine with hydrochloric acid, sulfuric acid, p-toluenesulfonic acid, phosphoric acid, formic acid, acetic acid, citric acid, tartaric acid, or maleic acid; or a double salt of S-adenosyl-L-methionine with the foregoing acids. The salt of a bivalent or trivalent metal is, for example, calcium chloride, ferric chloride, magnesium chloride, or magnesium sulfate. A process for preparing the composition is also disclosed. The composition is suitable for preparing pharmaceutical preparations of S-adenosyl-L-methionine.
摘要翻译：公开了S-腺苷-L-甲硫氨酸的稳定组合物，其包括S-腺苷-L-甲硫氨酸的盐和二价或三价金属的药学上可接受的水溶性盐。 S-腺苷-L-甲硫氨酸的盐例如是S-腺苷-L-甲硫氨酸与盐酸，硫酸，对甲苯磺酸，磷酸，甲酸，乙酸，柠檬酸，酒石酸的盐酸或马来酸; 或S-腺苷-L-甲硫氨酸与上述酸的双重盐。二价或三价金属的盐是例如氯化钙，氯化铁，氯化镁或硫酸镁。还公开了制备该组合物的方法。该组合物适用于制备S-腺苷-L-甲硫氨酸的药物制剂。

120. 发明授权

US4310635A Fermentative production of D(-)-.beta.-hydroxyisobutyric acid 失效
标题翻译：发酵生产D（ - ） - β-羟基异丁酸
公开(公告)号：US4310635A
公开(公告)日：1982-01-12
申请号：US201337
申请日：1980-10-27
申请人： Junzo Hasegawa , Masahiro Ogura , Shigeki Hamaguchi , Masami Shimazaki , Hajime Kawaharada , Kiyoshi Watanabe
发明人： Junzo Hasegawa , Masahiro Ogura , Shigeki Hamaguchi , Masami Shimazaki , Hajime Kawaharada , Kiyoshi Watanabe
IPC分类号： C12P7/42
CPC分类号： C12P7/42 , Y10S435/911 , Y10S435/913 , Y10S435/917 , Y10S435/921 , Y10S435/938 , Y10S435/94 , Y10S435/942
摘要： A process is disclosed wherein D(-)-.beta.-hydroxyisobutyric acid is produced fermentatively from isobutyric acid or methacrylic acid by the stereoselective action of microorganisms having the ability to convert isobutyric acid or methacrylic acid into D(-)-.beta.-hydroxyisobutyric acid in an aqueous medium, and D(-)-.beta.-hydroxyisobutyric acid is recovered from the aqueous medium.
摘要翻译：公开了一种方法，其中通过具有将异丁酸或甲基丙烯酸转化为D（ - ） - β-羟基异丁酸的能力的微生物的立体选择性作用，从（异）酸或甲基丙烯酸发酵得到D（ - ） - β-羟基异丁酸）从水介质中回收水性介质和D（ - ） - β-羟基异丁酸。

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