Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives
    1.
    发明授权
    Process for preparing 2-carbamoyloxyalkyl-1,4-dihydropyridine derivatives 失效
    2-氨基甲酰氧基烷基-1,4-二氢吡啶衍生物的制备方法

    公开(公告)号:US4958024A

    公开(公告)日:1990-09-18

    申请号:US230418

    申请日:1988-08-10

    IPC分类号: C07D211/90 C07D295/205

    CPC分类号: C07D295/205 C07D211/90

    摘要: A process for preparing a 2-carbamoylocxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives
    2.
    发明授权
    Certain intermediate 3-carbamoyloxyalkyl propiolic acid derivatives 失效
    某些中间体3-氨基甲酰氧基烷基丙炔酸衍生物

    公开(公告)号:US4914227A

    公开(公告)日:1990-04-03

    申请号:US863984

    申请日:1986-05-16

    IPC分类号: C07D211/90 C07D295/205

    CPC分类号: C07D295/205 C07D211/90

    摘要: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloxyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    3-amino-3-carbamoyloxyalkylacrylic acid intermediates to dihydropyridines
    3.
    发明授权
    3-amino-3-carbamoyloxyalkylacrylic acid intermediates to dihydropyridines 失效
    3-氨基-3-氨基甲酰氧基烷基丙烯酸中间体转化为二氢吡啶

    公开(公告)号:US4739106A

    公开(公告)日:1988-04-19

    申请号:US865654

    申请日:1986-05-16

    CPC分类号: C07D295/205 C07D211/90

    摘要: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.

    摘要翻译: 一种制备由以下通式表示的2-氨基甲酰氧基烷基-1,4-二氢吡啶衍生物的方法:(I),其包括:(a)使由以下通式表示的3-氨基-3-氨基甲酰氧基烷基丙烯酸衍生物: (II)与通式(III)表示的亚苄基化合物反应:(b)使通式II的3-氨基-3-氨基甲酰氧基烷基丙烯酸衍生物与通式 (IV)和由通式R4-CO-CH2-COOR2(V)表示的β-酮酯化合物(c)(c)使由以下通式表示的3-氨基甲酰氧基烷基丙酸衍生物反应: (VI)与通式Ⅲ的亚苄基化合物和氨或其盐; 或(d)使通式VI的3-氨基甲酰基烷基丙酸衍生物与通式IV的醛化合物,通式V的β-酮酯化合物和氨或其盐反应。

    2-Substituted or unsubstituted aminocarbonyloxyalkyl-1,4-dihydropyridines
    4.
    发明授权
    2-Substituted or unsubstituted aminocarbonyloxyalkyl-1,4-dihydropyridines 失效
    2-取代或未取代的氨基羰氧基烷基-1,4-二氢吡啶

    公开(公告)号:US4404378A

    公开(公告)日:1983-09-13

    申请号:US366137

    申请日:1982-04-06

    CPC分类号: C07D211/90

    摘要: Novel compounds having vasodilation and hypotensive effects are represented by the formula ##STR1## where R.sup.1 is halogen, nitro, cyano or lower alkoxy; each of R.sup.2 and R.sup.3 is lower alkyl, lower haloalkyl, lower alkoxyalkyl, aralkyloxyalkyl, aryloxyalkyl, lower alkenoxyalkyl, N,N-di-lower alkylaminoalkyl, N-lower alkyl-N-aralkylaminoalkyl, piperidylalkyl, 4-lower alkyl piperazinylalkyl, norpholinoalkyl or 1-pyrrolidinylalkyl; R.sup.4 is lower alkyl; A is lower alkylene; and R.sup.5 is hydrogen, lower alkyl, cycloalkyl of 3 to 7 carbon atoms, or aryl unsubstituted or substituted by one or two substituents selected from halogen, nitro, lower alkyl, lower alkoxy, di-lower alkylamino and cyano.Also disclosed are processes for their preparation.

    摘要翻译: 具有血管扩张和降血压作用的新型化合物由式(I)表示,其中R 1是卤素,硝基,氰基或低级烷氧基; R2和R3各自为低级烷基,低级卤代烷基,低级烷氧基烷基,芳烷氧基烷基,芳氧基烷基,低级烷氧基烷基,N,N-二 - 低级烷基氨基烷基,N-低级烷基-N-芳烷基氨基烷基,哌啶基烷基,4-低级烷基哌嗪基烷基, 1-吡咯烷基烷基; R4是低级烷基; A是低级亚烷基; 或R 5为氢,低级烷基,3-7个碳原子的环烷基,或未被取代或被一个或两个选自卤素,硝基,低级烷基,低级烷氧基,二低级烷基氨基和氰基的取代基取代的芳基。 还公开了它们的制备方法。

    Substituted fusaric acid derivatives
    5.
    发明授权
    Substituted fusaric acid derivatives 失效
    取代的镰孢酸衍生物

    公开(公告)号:US3935221A

    公开(公告)日:1976-01-27

    申请号:US461595

    申请日:1974-04-17

    IPC分类号: C07D213/81 C07D213/56

    CPC分类号: C07D213/81

    摘要: Halo-fusaric acid amides having the formula ##SPC1##Wherein X represents halogen or hydrogen, Y represents halogen and R.sub.1 and R.sub.2 are same or different and represent hydrogen or a lower alkyl group (C.sub.1-4) which are characterized by significant activity in the treatment of hypertension.

    摘要翻译: 具有式WHEREIN X表示卤素或氢的卤代糠酸酰胺,Y表示卤素,R 1和R 2相同或不同,表示氢或低级烷基(C 1-4),其特征在于治疗高血压具有显着活性 。

    Process for production of 5-ene-3-one or 3,6-dione derivatives of sterols, processes for production of lipid metabolism improvers, foods, drinks, and animal feeds, and analytical method
    6.
    发明授权
    Process for production of 5-ene-3-one or 3,6-dione derivatives of sterols, processes for production of lipid metabolism improvers, foods, drinks, and animal feeds, and analytical method 有权
    甾醇的5-烯-3-酮或3,6-二酮衍生物的制备方法,脂质代谢改进剂的生产方法,食品,饮料和动物饲料,以及分析方法

    公开(公告)号:US08008040B2

    公开(公告)日:2011-08-30

    申请号:US11632072

    申请日:2005-07-12

    IPC分类号: C12P33/00

    CPC分类号: C12P33/00

    摘要: An object of the present invention is to provide a process according to which 5-ene-3-one or 3,6-dione derivatives of sterols can be synthesized with a better yield, as well as a process for production of lipid metabolism improvers, foods, drinks, and animal feeds containing the 5-ene-3-one or 3,6-dione derivatives of sterols.The process for production of 5-ene-3-one or 3,6-dione derivatives of sterols of the present invention involves preparing a culturing solution containing an Arthrobacter bacterium, which is a microorganism exhibiting a cholesterol oxidase activity, and then, adding to the culturing solution an equivalent amount of hexane so as to prepare a bilayer solution consisting of an aqueous layer and a hydrocarbon-based solvent layer. Thereafter, sterol, or a derivative thereof, is made as a substrate contained therein, a reaction performed with cholesterol oxidase at 30° C. for 2 days, and, ethanol then added to separate a hydrocarbon-based solvent layer. Thereafter, the layer is dried to a state of dryness by means of a vacuum dryer so as to obtain 5-ene-3-one or 3,6-dione derivatives.

    摘要翻译: 本发明的目的是提供可以以更好的产率合成甾醇的5-烯-3-酮或3,6-二酮衍生物的方法,以及脂质代谢改进剂的生产方法, 含有甾醇的5-烯-3-酮或3,6-二酮衍生物的食品,饮料和动物饲料。 制备本发明的甾醇的5-烯-3-酮或3,6-二酮衍生物的方法包括制备含有作为显示胆固醇氧化酶活性的微生物的节杆菌细菌的培养液,然后加入 培养液中加入等量的己烷,以制备由水层和烃基溶剂层组成的双层溶液。 此后,将固醇或其衍生物作为其中含有的底物,在30℃下用胆固醇氧化酶进行反应2天,然后加入乙醇以分离烃基溶剂层。 此后,通过真空干燥器将该层干燥至干燥状态,以获得5-烯-3-酮或3,6-二酮衍生物。

    Process for Production of 5-Ene-3-One or 3,6-Dione Derivatives of Sterols, Processes for Production of Lipid Metabolism Improvers, Foods, Drinks, and Animal Feeds, and Analytical Method
    7.
    发明申请
    Process for Production of 5-Ene-3-One or 3,6-Dione Derivatives of Sterols, Processes for Production of Lipid Metabolism Improvers, Foods, Drinks, and Animal Feeds, and Analytical Method 有权
    甾醇的5-烯-3-酮或3,6-二酮衍生物的制备方法,脂质代谢改良剂,食品,饮料和动物饲料的生产方法和分析方法

    公开(公告)号:US20080248520A1

    公开(公告)日:2008-10-09

    申请号:US11632072

    申请日:2005-07-12

    IPC分类号: C12P33/00 G01N30/02

    CPC分类号: C12P33/00

    摘要: An object of the present invention is to provide a process according to which 5-ene-3-one or 3,6-dione derivatives of sterols can be synthesized with a better yield, as well as a process for production of lipid metabolism improvers, foods, drinks, and animal feeds containing the 5-ene-3-one or 3,6-dione derivatives of sterols.The process for production of 5-ene-3-one or 3,6-dione derivatives of sterols of the present invention involves preparing a culturing solution containing an Arthrobacter bacterium, which is a microorganism exhibiting a cholesterol oxidase activity, and then, adding to the culturing solution an equivalent amount of hexane so as to prepare a bilayer solution consisting of an aqueous layer and a hydrocarbon-based solvent layer. Thereafter, sterol, or a derivative thereof, is made as a substrate contained therein, a reaction performed with cholesterol oxidase at 30° C. for 2 days, and, ethanol then added to separate a hydrocarbon-based solvent layer. Thereafter, the layer is dried to a state of dryness by means of a vacuum dryer so as to obtain 5-ene-3-one or 3,6-dione derivatives.

    摘要翻译: 本发明的目的是提供可以以更好的产率合成甾醇的5-烯-3-酮或3,6-二酮衍生物的方法,以及脂质代谢改进剂的生产方法, 含有甾醇的5-烯-3-酮或3,6-二酮衍生物的食品,饮料和动物饲料。 制备本发明的甾醇的5-烯-3-酮或3,6-二酮衍生物的方法包括制备含有节杆菌属细菌的培养液,其为显示胆固醇氧化酶活性的微生物,然后加入 培养液中加入等量的己烷,以制备由水层和烃基溶剂层组成的双层溶液。 此后,将固醇或其衍生物作为其中含有的底物,在30℃下用胆固醇氧化酶进行反应2天,然后加入乙醇以分离烃基溶剂层。 此后,通过真空干燥器将该层干燥至干燥状态,以获得5-烯-3-酮或3,6-二酮衍生物。

    Paper feeding apparatus in web threading apparatus
    8.
    发明授权
    Paper feeding apparatus in web threading apparatus 失效
    卷筒纸穿线装置中的送纸装置

    公开(公告)号:US5921453A

    公开(公告)日:1999-07-13

    申请号:US021003

    申请日:1998-02-09

    申请人: Kunio Suzuki

    发明人: Kunio Suzuki

    摘要: A paper feeding apparatus is provided for use in a web threading apparatus of a rotary press for threading a web along a web threading path by drawing a leading end of the web using a web threading member movably provided on an outside portion of the web threading path and along the web threading path. The paper feeding apparatus includes a pair of an upstream roller and a downstream roller extending substantially parallel to a width direction of the web in the web threading path, and a driving mechanism for driving the upstream and downstream rollers in a feeding direction of the web and for ensuring that a peripheral speed of the downstream roller is at least equal to a moving speed of the web threading member. The upstream and downstream rollers are offset on an upstream side and a downstream side in a direction of the web threading path so that the web is not nipped by both the upstream roller and the downstream roller. A peripheral surface of one of the upstream and downstream rollers contacts a first side surface of the web and a peripheral surface of the other of the upstream and downstream rollers contacts a second side surface of the web, in a manner such that slipping between the rollers and the web is increased in response to a lowering of a tension on the web and such that slipping between the rollers and the web is decreased in response to an increase of the tension on the web. In addition, the upstream roller is displaceable in accordance with a variation of the tension on the web so as to constantly apply a force against the tension.

    摘要翻译: 一种供纸装置,用于旋转印刷机的卷筒纸穿线装置中,用于通过使用可移动地设置在卷筒纸穿线路径的外侧部分上的卷筒纸穿纱件拉伸卷筒纸的前端,沿着卷筒纸穿线路径来卷绕纸卷 并沿着网络线程路径。 供纸装置包括一对上游辊和下游辊,该辊沿着幅材穿过路径中的幅材的宽度方向基本上平行延伸;以及驱动机构,用于沿纸幅的进给方向驱动上游辊和下游辊;以及 用于确保下游辊的圆周速度至少等于卷筒纸穿线构件的移动速度。 上游辊和下游辊在幅材穿线路径的方向上的上游侧和下游侧偏移,使得幅材不被上游辊和下游辊夹持。 上游辊和下游辊中的一个的周边表面接触幅材的第一侧表面,并且另一个上游辊和下游辊的外周表面以这样的方式接触纸幅的第二侧表面,使得在辊之间滑动 并且纤维网响应于纸幅上的张力的降低而增加,并且响应于幅材上的张力的增加,辊和纸幅之间的滑动减小。 此外,上游辊可以根据幅材上的张力的变化而移位,以便不断地施加抵抗张力的力。

    Anti-obesity agents
    9.
    发明授权
    Anti-obesity agents 失效
    抗肥胖剂

    公开(公告)号:US5846962A

    公开(公告)日:1998-12-08

    申请号:US897884

    申请日:1997-07-21

    CPC分类号: A61K31/575

    摘要: Anti-obesity agents which comprise 3-ketosteroid compounds as an active ingredient are provided. The anti-obesity agents of the present invention have a high anti-obesity effect with little or no side effects and toxicity. Food products which contain anti-obesity agents comprising 3-ketosteroid compounds as an active ingredient, pharmaceutical compositions which comprise 3-ketosteroid compounds as an active ingredient and pharmaceutically acceptable carriers, and methods for preventing and treating obesity which comprise administering an effective amount of a 3-ketosteroid compound to a human are also provided.

    摘要翻译: 提供了包含3-酮类固醇化合物作为活性成分的抗肥胖剂。 本发明的抗肥胖剂具有很高的抗肥胖作用,很少或没有副作用和毒性。 含有3-酮类固醇化合物作为活性成分的抗肥胖剂的食品,包含3-酮类固醇化合物作为活性成分的药物组合物和药学上可接受的载体,以及预防和治疗肥胖症的方法,其包括施用有效量的 还提供了3-酮类固醇化合物给人类。