Fatty acids analogous
    2.
    发明授权
    Fatty acids analogous 有权
    脂肪酸类似

    公开(公告)号:US07902399B2

    公开(公告)日:2011-03-08

    申请号:US10220502

    申请日:2001-03-02

    IPC分类号: A01N37/00 C07C57/02

    摘要: The present invention relates to novel fatty acid analogous of the general formula (I): R1—[xi—CH2]n—COOR2 wherein R1 is: a C6-C24 alkene with one or more double bonds and/or with one or more triple bonds, and/or a C6-C24 alkyne, and/or a C6-C24 alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein n is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, and with the proviso that if R1 is an alkye, then the carbon-carbon triple bond is positioned between the (ω-1) carbon and the (ω-2) carbon, or between the (ω-2) carbon and the (ω-3) carbon, or between the (ω-3) carbon and the (ω-4) carbon, a salt, prodrug or complex thereof, which can be used for the treatment and/or prevention of syndrome X, obesity, hypertension, fatty liver, diabetes, hyperglycaemia, hyperinsulinemia and stenosis. Further, the invention relates to a nutritional composition comprising said fatty acid analogues, and a method for reducing the total weight, or the amount of adipose tissue in an animal.

    摘要翻译: 本发明涉及类似于通式(I)的新型脂肪酸:R1- [xi-CH2] n-COOR2其中R1是:具有一个或多个双键的C6-C24烯烃和/或一个或多个三重键 键,和/或C 6 -C 24炔基,和/或在一个或多个位置被一个或多个选自以下的化合物取代的C 6 -C 24烷基:氟,氯,羟基,C 1 -C 4烷氧基,C 1 -C 4烷硫基 ,C 2 -C 5酰氧基或C 1 -C 4烷基,并且其中R 2表示氢或C 1 -C 4烷基,并且其中n是1至12的整数,并且其中i是奇数并且表示相对于COOR 2的位置,并且其中 彼此独立的X选自O,S,SO,SO 2,Se和CH 2的基团,条件是至少一个X 1不是CH 2,条件是如果R 1是烷基,则 碳 - 碳三键位于(ω-1)碳和(ω-2)碳之间,或(ω-2)碳和(ω-3)碳之间,或 -3)碳和(ω-4)碳,其盐,前药或复合物,其可用于治疗和/或预防综合征X,肥胖症,高血压,脂肪肝,糖尿病,高血糖症,高胰岛素血症和狭窄 。 此外,本发明涉及包含所述脂肪酸类似物的营养组合物,以及用于降低动物体内总重量或脂肪组织量的方法。

    Intermediates and processes for the preparation of optically active octanoic acid derivatives
    3.
    发明授权
    Intermediates and processes for the preparation of optically active octanoic acid derivatives 失效
    用于制备光学活性辛酸衍生物的中间体和方法

    公开(公告)号:US06333415B1

    公开(公告)日:2001-12-25

    申请号:US09700181

    申请日:2000-11-13

    申请人: Hisashi Yamamoto

    发明人: Hisashi Yamamoto

    IPC分类号: C07D27506

    摘要: Novel intermediates, i.e., N-(2S-(2-propenyl)octanoyl)-(1S)-(−)-2,10-camphorsultam, N-(2S-(2-propynyl)octanoyl)-(1S)-(−)-2,10-camphorsultam and N-(2R-(2-propyl)octanoyl)-(1S)-(−)-2,10-camphorsultam; processes for the preparation of the intermediates; and processes for the preparation of optically active 2S-(2-propenyl)octanoic acid, 2S-(2-propynyl)octanoic acid and 2R-propyloctanoic acid by using the same. Optically active 2R-propyloctanoic acid equivalent or superior to that prepared by the process of the prior art in optical purity can be efficiently prepared in shorter reaction steps.

    摘要翻译: 新型中间体,即N-(2S-(2-丙烯基)辛酰基) - (1S) - ( - ) - 2,10-樟脑磺胺,N-(2S-(2-丙炔基)辛酰基) - (1S) - - ) - 2,10-樟脑磺胺和N-(2R-(2-丙基)辛酰基) - (1S) - ( - ) - 2,10-樟脑磺酸钠; 制备中间体的方法; 以及通过使用它们制备光学活性的2S-(2-丙烯基)辛酸2S-(2-丙炔基)辛酸和2R-丙基辛酸的方法。 可以在较短的反应步骤中有效地制备光学活性的2R-丙酸辛酸当量或优于现有技术的光学纯度方法制备的。

    Antimycobacterial compounds and method of using same
    4.
    发明授权
    Antimycobacterial compounds and method of using same 失效
    抗分解细菌化合物及其使用方法

    公开(公告)号:US5837732A

    公开(公告)日:1998-11-17

    申请号:US766273

    申请日:1996-12-13

    摘要: The present invention provides a compound having the structure: ##STR1## wherein R is a branched or unbranched C1-C30 alkyl, alkenyl or alkynl; or a branched or unbranched C1-C30 alkyl, alkenyl or alkynl substituted with S, O, N, P, SO.sub.2, F, Cl, Br, or I, wherein S, O, N, P, or SO.sub.2 replaces at least one --CH.sub.2 --, and F, Cl, Br, or I replaces at least one H. The present invention also provides a pharmaceutical composition comprising the compound above, as well as a method for treating a mycobacterial disease or infection in a subject in need of such treatment by administering to the subject an effective amount of the compound above.

    摘要翻译: 本发明提供具有以下结构的化合物:其中R是支链或非支链C 1 -C 30烷基,烯基或炔烃; 或被S,O,N,P,SO 2,F,Cl,Br或I取代的支链或非支链C 1 -C 30烷基,链烯基或炔烃,其中S,O,N,P或SO 2取代至少一个 - CH 2 - 和F,Cl,Br或I取代至少一个H.本发明还提供了包含上述化合物的药物组合物,以及用于治疗需要这样的受试者的分枝杆菌病或感染的方法 通过向受试者施用有效量的上述化合物进行治疗。

    VPA-analogous antiepileptics
    5.
    发明授权
    VPA-analogous antiepileptics 失效
    VPA类似的抗癫痫药

    公开(公告)号:US5786380A

    公开(公告)日:1998-07-28

    申请号:US344810

    申请日:1994-11-23

    摘要: The invention provides compounds which are effective antiepileptics and at the same time display only a slight sedative and teratogenic effect and have the formula ##STR1## where the compounds of the formulae (I) and (II) can also be mono- or polyunsaturated, in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each, independently of one another, hydrogen or a C.sub.1 -C.sub.6 -alkyl group, R.sup.5 is hydrogen or a C.sub.1 -C.sub.2 -alkyl group, and at least one of the radicals R.sup.1 to R.sup.4 in the compounds of the formulae (I) and (II) is different from hydrogen, where the compounds of the formula (I), in the case where a center of asymmetry is present on the carbon atom in position 2, and the compounds of the formulae (II), (III) and (IV) are in the form of their racemate, their pure enantiomers or a mixture of their enantiomers which differs from the racemate, and pharmaceutically compatible salts thereof.

    摘要翻译: 本发明提供了有效的抗癫痫药物,同时仅显示出轻微的镇静作用和致畸作用,并具有式(Ⅰ)的化合物。 式(I)和(II)的化合物也可以是单或多不饱和的,其中R 1,R 2,R 3和R 4彼此独立地为氢或C 1 -C 6 - 烷基,R 5为氢 或者C 1 -C 2烷基,式(I)和(II)的化合物中的R 1〜R 4中的至少一个与氢不同,式(I)的化合物在这种情况下 其中不对称中心存在于位置2的碳原子上,式(II),(III)和(IV)的化合物是其外消旋体,其纯对映异构体或其对映异构体的混合物的形式, 不同于外消旋体及其药学上相容的盐。

    Processless diacetylenic salt films capable of developing a black image
    6.
    发明授权
    Processless diacetylenic salt films capable of developing a black image 失效
    能够显影黑色图像的无处理二乙炔盐膜

    公开(公告)号:US5731112A

    公开(公告)日:1998-03-24

    申请号:US652144

    申请日:1996-05-23

    摘要: This invention relates to a mixture of imageable polyacetylenic compounds which have similar photosensitivities and which are visually imageable in complementary colors combinable to provide a black image, which mixture contains at least one polyacetylenic metal salt which produces a color, preferably a metal salt of a diacetylene C.sub.6 to C.sub.48 mono- or dicarboxylic acid, which is complementary to a color produced by another polyacetylenic metal salt or non-metallic polyacetylenic compound contained in the mixture or in an another integral color forming layer. The invention also pertains to the use of said mixture and the manner of its preparation.

    摘要翻译: 本发明涉及可成像的聚乙炔化合物的混合物,其具有相似的光敏性,并且可以互补的可视形态地形成可组合以提供黑色图像的混合物,该混合物含有至少一种产生颜色的聚乙炔性金属盐,优选为乙炔的金属盐 C6至C48单羧酸或二羧酸,其与由混合物中所含的另一种聚乙炔性金属盐或非金属聚乙炔化合物或另一整体成色层产生的颜色互补。 本发明还涉及所述混合物的用途及其制备方法。

    Biocidal esters of alkynoic acids
    7.
    发明授权
    Biocidal esters of alkynoic acids 失效
    炔酸的杀生物酯

    公开(公告)号:US4423064A

    公开(公告)日:1983-12-27

    申请号:US278721

    申请日:1981-06-29

    申请人: Thomas N. Wheeler

    发明人: Thomas N. Wheeler

    摘要: This invention relates to novel ester compounds derived from alkynoic acids and to their preparation. This invention is also directed to insecticidal and miticidal compositions comprising an acceptable carrier and an insecticidally or miticidally effective amount of a novel ester compound of this invention as well as a method of controlling pests by subjecting them to an insecticidally or miticidally effective amount of a novel ester compound of this invention.

    摘要翻译: 本发明涉及由炔酸衍生的新型酯化合物及其制备方法。 本发明还涉及包含可接受的载体和杀虫或杀螨有效量的本发明的新型酯化合物的杀虫剂和杀螨剂组合物,以及通过使其具有杀虫或杀螨有效量的新颖性的方法来控制害虫 酯化合物。

    Process for the preparation of cis-8-dodecen-1-ol acetate
    8.
    发明授权
    Process for the preparation of cis-8-dodecen-1-ol acetate 失效
    顺式-8-十二碳烯-1-醇乙酸酯的制备方法

    公开(公告)号:US3906035A

    公开(公告)日:1975-09-16

    申请号:US43769474

    申请日:1974-01-29

    发明人: HOLAN GEORGE

    摘要: An improved process for the manufacture of cis-8-dodecen-1-ol acetate, the sex pheromone of the oriental fruit moth Cydia molesta, comprises the steps of: i. reacting 1-chloro-6-iodohexane with pent-1-yne in liquid ammonia in the presence of lithium amide as a catalyst; ii. reacting the product of step (i) with an alkali metal cyanide in the presence of a metal iodide as catalyst; iii. subjecting the product of step (ii) to alkaline hydrolysis; iv. reducing the product of step (iii) with sodium bis(methoxyethoxy) aluminium hydride; v. acetylating the product of step (iv); and vi. reducing the product of step (v) with bis(sec-isoamyl)borane.

    摘要翻译: 顺丁-8-十二烯-1-醇乙酸酯的改进方法,东方水果蛾Cydia molesta的性信息素包括以下步骤:i。 在氨化氨作催化剂存在下,将液体氨中的1-氯-6-碘 - 己烷与戊-1-炔反应; ii。 在金属碘化物作为催化剂的存在下使步骤(i)的产物与碱金属氰化物反应; iii。 使步骤(ii)的产物进行碱水解; iv。 用二(甲氧基乙氧基)氢化铝钠还原步骤(ⅲ)的产物; v。乙酰化步骤(iv)的产物; 和vi。 用双(仲 - 异戊基)硼烷还原步骤(v)的产物。

    Photochemical process for preparing a bicyclic lactone
    10.
    发明授权
    Photochemical process for preparing a bicyclic lactone 失效
    用于制备双相乳液的光化学方法

    公开(公告)号:US3674663A

    公开(公告)日:1972-07-04

    申请号:US3674663D

    申请日:1969-11-28

    申请人: ZOECON CORP

    发明人: SIDDALL JOHN B

    摘要: Synthesis of cis 2-(1''-methyl-2''-isopropenylcyclobutyl)ethanol, a component of the boll weevil sex attractant, and intermediates therefor, in which 5-hydroxy-pent-2-ynoic acid or ethers thereof is methylated followed by cyclization to yield 3-methylpent-2eno-5-lactone which is irradiated in presence of ethylene to yield 2,3-cycloethylene-3-methylpentano-5-lactone which is cleaved and converted into 2-(1''-methyl-2''isopropenylcyclobutyl)ethanol.

    摘要翻译: 顺式2-(1'-甲基-2'-异丙烯基环丁基)乙醇的合成,其为5-位羟基 - 戊-2-炔酸或其醚甲基化,然后是其中的5-羟基 - 戊-2-炔酸或其醚, 在乙烯存在下照射3-甲基戊-2-烯-5-内酯,得到2,3-环亚乙基-3-甲基戊-5-烯酮,将其切割并转化为2-(1'-甲基 - 2'-异丙烯基环丁基)乙醇。