Quaternaries of hydroxyalkylaminoalkylamides
    1.
    发明授权
    Quaternaries of hydroxyalkylaminoalkylamides 失效
    羟基烷基氨基烷基酰胺季铵盐

    公开(公告)号:US4146556A

    公开(公告)日:1979-03-27

    申请号:US814571

    申请日:1977-07-11

    IPC分类号: C23F11/14 C07C103/183

    CPC分类号: C23F11/145

    摘要: This invention relates to hydroxyalkylaminoalkylamides, the N-alkylated derivatives thereof, and the preparaton and uses thereof. This invention also relates to quaternaries of the abovementioned hydroxyalkylaminoalkylamides.

    摘要翻译: 本发明涉及羟烷基氨基烷基酰胺,其N-烷基化衍生物及其制备方法及用途。 本发明还涉及上述羟基烷基氨基烷基酰胺的季胺。

    Triiodinated aminoacetamido isophthalamide x-ray contrast agents
    3.
    发明授权
    Triiodinated aminoacetamido isophthalamide x-ray contrast agents 失效
    三碘代氨基乙酰氨基间苯二胺X射线造影剂

    公开(公告)号:US4283381A

    公开(公告)日:1981-08-11

    申请号:US167597

    申请日:1980-07-11

    CPC分类号: C07D209/48

    摘要: Compounds of the formula ##STR1## wherein X is alkylene, optionally substituted by hydroxy, methoxy or amino;R.sup.1 is hydrogen or C.sub.1-4 alkyl;R.sup.2 is hydrogen, C.sub.1-4 alkyl, or C.sub.2-4 -alkyl substituted by 1-3 OH groups;R.sup.3 is hydrogen, C.sub.1-4 alkyl, or C.sub.2-4 -alkyl substituted by 1-3 OH groups;R.sup.4 is hydrogen, C.sub.1-4 -alkyl, or C.sub.2-4 -alkyl substituted by 1-3 OH groups;R.sup.5 is C.sub.2-4 -alkyl substituted by 1-3 OH groups;R.sup.6 is hydrogen, C.sub.1-4 -alkyl or C.sub.2-4 -alkyl substituted by 1-3 OH groups; andR.sup.7 is C.sub.2-4 -alkyl substituted by 1-3 OH groups,or a salt thereof with an acidare useful as opaquing agents in x-ray contrast media.

    摘要翻译: 式(I)的化合物其中X为亚烷基,任选被羟基,甲氧基或氨基取代; R1是氢或C1-4烷基; R2是氢,C1-4烷基或被1-3个OH基取代的C2-4-烷基; R3是氢,C1-4烷基或被1-3个OH基取代的C2-4-烷基; R4是氢,C1-4烷基或被1-3个OH基取代的C2-4-烷基; R5是被1-3个OH基取代的C2-4-烷基; R6是氢,C1-4烷基或被1-3个OH基取代的C2-4烷基; 并且R 7为被1-3个OH基取代的C 2-4烷基,或其与酸的盐可用作x射线造影剂中的不透明剂。

    Olefinic derivatives of amino acids
    4.
    发明授权
    Olefinic derivatives of amino acids 失效
    氨基酸的烯烃衍生物

    公开(公告)号:US4039549A

    公开(公告)日:1977-08-02

    申请号:US664991

    申请日:1976-03-08

    CPC分类号: C07C237/00

    摘要: Novel compounds of the following general formula are useful pharmacologic agents: ##STR1## R is selected from hydrogen, alkylcarbonyl wherein the alkyl moiety contains from 1 to 4 carbon atoms, alkoxycarbonyl wherein the alkoxy moiety contains from 1 to 4 carbon atoms and may be a straight or branched, and ##STR2## wherein R.sub.10 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and .rho.-hydroxybenzyl; R.sub.2 is selected from hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, a lower alkylamino group wherein the alkyl moiety contains from 1 to 4 carbon atoms, and ##STR3## wherein R.sub.4 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl, and .rho.-hydroxybenzyl; R.sub.3 is selected from hydrogen, chlorine, bromine, and iodine; [A] is selected from ##STR4## AND --CH=CH-- wherein R.sub.1 is selected from hydrogen, lower alkyl of from 1 to 4 carbon atoms, phenyl and substituted phenyl wherein the substituents on the substituted phenyl may be attached at the ortho, meta or para positions of the phenyl ring and are selected from halogen, lower alkoxy of from 1 to 4 carbon atoms, and lower alkyl of from 1 to 4 carbon atoms; n is an integer of from 1 to 5; and the lactams of said compounds wherein [A] represents ##STR5## R and R.sub.1 represent hydrogen and n is the integer 2 or 3 and pharmaceutically acceptable salts and individual optical isomers thereof.

    摘要翻译: 以下通式的新型化合物是有用的药理学药剂:R选自氢,烷基部分含有1至4个碳原子的烷基羰基,其中烷氧基部分含有1至4个碳原子,可以是 直链或支链,和其中R10选自氢,1-4个碳原子的直链或支链低级烷基,苄基和对羟基苄基; R2选自羟基,1至8个碳原子的直链或支链烷氧基,其中烷基部分含有1至4个碳原子的低级烷基氨基,和其中R 4选自氢,直链或 具有1至4个碳原子的支链低级烷基,苄基和rho-羟基苄基; R3选自氢,氯,溴和碘; [A]选自和-CH = CH-,其中R 1选自氢,1至4个碳原子的低级烷基,苯基和取代的苯基,其中取代的苯基上的取代基可以在邻位, 苯环的间位或对位,并且选自卤素,1至4个碳原子的低级烷氧基和1至4个碳原子的低级烷基; n为1〜5的整数, 和所述化合物的内酰胺,其中[A]表示R并且R 1表示氢,n是整数2或3及其药学上可接受的盐和单独的光学异构体。

    Process for the production of carnitine amide
    6.
    发明授权
    Process for the production of carnitine amide 失效
    肉碱酰胺生产工艺

    公开(公告)号:US4443627A

    公开(公告)日:1984-04-17

    申请号:US341009

    申请日:1982-01-20

    CPC分类号: C07C237/00

    摘要: Process for the production of carnitine amide in the form of a chloride. The carnitine ethyl ester is obtained by reaction of 4-chloroacetoacetic acid ethyl ester with trimethyl amine and the subsequent hydrogenation is carried out with the help of a Pt/C catalyst. Such carnitine ethyl ester, without isolating it, is reacted with ammonia in an autoclave at -30.degree. to +10.degree. C. Everything is heated to 40.degree. to 80.degree. C. The mixture is stirred at such temperature at an ammoniac pressure of 8 to 24 atu. The product is filtered after cooling it to ambient temperature and counterbalancing the excess pressure. The product is then washed with alcohol and subsequently dried at 30.degree. to 50.degree. C. and at a pressure of 15 to 25 torr.

    摘要翻译: 以氯化物的形式生产肉碱酰胺的方法。 肉碱乙酯通过4-氯乙酰乙酸乙酯与三甲基胺的反应得到,随后在Pt / C催化剂的帮助下进行氢化。 将这样的肉碱乙酯在高压灭菌器中在-30〜+ 10℃下与氨反应,一切加热至40〜80℃。将混合物在氨压8℃下搅拌 到24阿库 将产物在冷却至环境温度后过滤,并平衡过剩的压力。 然后将产物用醇洗涤,然后在30至50℃和15至25托的压力下干燥。

    Cross-linking reagent for insulin synthesis
    8.
    发明授权
    Cross-linking reagent for insulin synthesis 失效
    用于胰岛素合成的交联剂

    公开(公告)号:US3996268A

    公开(公告)日:1976-12-07

    申请号:US502425

    申请日:1974-09-03

    摘要: Carbonyl-bis (L-methionine p-nitrophenyl ester) and its analogues are useful reagents for the intermolecular cross-linking of two chain peptide molecules such as occur in the hormone insulin. The cross-linking occurs across amino groups at preferred positions in the two peptide chains to fix the relative spacial position of the peptide chains and permit the oxidative formation of necessary disulfide bridges between the chains in high yields. The reagent is then removed from the linked chains to yield the insulin molecule. A method for preparation of the reagent is disclosed. Further, a procedure is disclosed by which the cross-linking reagent is used to specifically block certain amino groups on insulin to yield a cross-linked insulin which in turn is used to prepare isotopically labeled insulin and insulin analogues.

    摘要翻译: 羰基 - 双(L-甲硫氨酸对硝基苯酯)及其类似物是用于激素胰岛素中发生的两个链肽分子的分子间交联的有用试剂。 交联发生在两个肽链中优选位置的氨基上,以固定肽链的相对空间位置,并允许以高产率在链之间氧化形成必需的二硫键。 然后从连接的链中除去试剂以产生胰岛素分子。 公开了一种制备试剂的方法。 此外,公开了一种方法,通过该方法,交联剂用于特异性阻断胰岛素上的某些氨基,产生交联的胰岛素,其又用于制备同位素标记的胰岛素和胰岛素类似物。