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175 条记录 (耗时 0.03 秒)

    Adamantyl containing 1,4-oxazinone derivatives
    58.
    发明授权
    Adamantyl containing 1,4-oxazinone derivatives 失效
    含有1,4-恶嗪酮衍生物的金刚烷基

    公开(公告)号：US4549014A

    公开(公告)日：1985-10-22

    申请号：US647787

    申请日：1984-09-06

    申请人： Vassil S. Georgiev ,  George B. Mullen

    发明人： Vassil S. Georgiev ,  George B. Mullen

    IPC分类号： C07D265/32 ,  C07D265/34

    CPC分类号： C07D265/32 ,  C07D265/34

    摘要： Antimicrobial or anti-inflammatory 1,4-oxazinone derivatives of the structure: ##STR1## wherein one of R and R.sup.1 is hydrogen and the other is --CH.sub.2 CO.sub.2 R.sup.6 (R.sup.6 =alkyl) or R and R.sup.1 together represent the group .dbd.CHCO.sub.2 R.sup.6, R.sup.2 and R.sup.3 are hydrogen, alkyl, substituted alkyl, phenyl or substituted phenyl or R.sup.2 and R.sup.3 together represent a single adamantyl group, and R.sup.4 and R.sup.5 are hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, or benzyl, are disclosed herein.

    摘要翻译： 下列结构的抗微生物或抗炎的1,4-恶嗪酮衍生物：其中R和R 1之一是氢，另一个是-CH 2 CO 2 R 6（R 6 =烷基）或R和R 1一起代表基团= CHCO 2 R 6，R 2和 R3是氢，烷基，取代的烷基，苯基或取代的苯基，或者R 2和R 3一起代表单一的金刚烷基，R4和R5是氢，烷基，取代的烷基，苯基，取代的苯基或苄基。

    Dopamine agonists and use thereof
    59.
    发明授权
    Dopamine agonists and use thereof 失效
    多巴胺激动剂及其用途

    公开(公告)号：US4540691A

    公开(公告)日：1985-09-10

    申请号：US600008

    申请日：1984-04-13

    申请人： Alan S. Horn

    发明人： Alan S. Horn

    IPC分类号： C07D265/00 ,  A61K31/535 ,  A61K31/55 ,  C07D265/34 ,  C07D265/36 ,  C07D267/00 ,  C07D267/12 ,  C07D267/14 ,  C07D409/00 ,  C07D413/02 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D265/34 ,  C07D267/12

    摘要： Compounds are disclosed having the formula: ##STR1## wherein: R.sub.1 is H, OH, --OCH.sub.3, --CH.sub.2 OH, --NH.sub.2, --NHMe, --NHEt, --NMe.sub.2, --NEt.sub.2, ##STR2## R.sub.2 is H, --CH.sub.3, or ##STR3## R.sub.3 is phenyl, benzyl, or 1-4 carbon alkyl; R.sub.4 is H, --CH.sub.3, --CH.sub.2 OH, --CH.sub.2 --CN, --CH.sub.2 --S--Me, CH.sub.2 --S--CN, or ##STR4## R.sub.5 is H, 1-4 carbon alkyl, alkenyl, or alkynyl, or aralkyl having a 1-4 carbon alkylene moiety; and A is --CH.sub.2 --or --CH.sub.2 CH.sub.2 --, and pharmaceutically-acceptable salts thereof. Pharmaceutical preparations using these compounds and a method for inducing a dopaminergic response by administering these compounds are also disclosed.

    摘要翻译： 公开了具有下式的化合物：其中：R1是H，OH，-OCH3，-CH2OH，-NH2，-NHMe，-NHEt，-NMe2，-NEt2，R2是H，-CH3或 R3是苯基，苄基或1-4个碳原子的烷基; R4是H，-CH3，-CH2OH，-CH2-CN，-CH2-S-Me，CH2-S-CN，或R5是H，1-4碳烷基，烯基或炔基，或具有 1-4碳亚烷基部分; 和A是-CH 2 - 或-CH 2 CH 2 - ，及其药学上可接受的盐。 还公开了使用这些化合物的药物制剂和通过施用这些化合物诱导多巴胺能反应的方法。

    Polysubstituted 2-morpholones
    60.
    发明授权
    Polysubstituted 2-morpholones 失效

    公开(公告)号：US4528370A

    公开(公告)日：1985-07-09

    申请号：US367631

    申请日：1982-04-12

    申请人： John T. Lai

    发明人： John T. Lai

    IPC分类号： C07D265/32 ,  C07D265/34 ,  C07D273/00 ,  C07D295/02 ,  C07D295/023 ,  C07D295/027

    CPC分类号： C07D273/00 ,  C07D265/32 ,  C07D265/34 ,  C07D295/023 ,  C07D295/027

    摘要： An essentially single stage reaction has been discovered in which a disubstituted ethanolamine, that is, a 2,2'-substituted-2-aminoethanol, may be reacted with a haloform and a carbonyl containing compound selected from the group consisting of monoketones and benzaldehyde, in the presence of an alkali metal hydroxide, and optionally in the presence of a phase transfer catalyst, to produce an alkali metal hydroxyethylaminoacetate ("HEAA") which has N-adjacent C atoms on which there are a total of at least three substituents (hence "polysubstituted"), and one or both pairs of substituents on each N-adjacent C atom may be cyclized. The HEAA may be cyclized by the action of a mineral acid to produce a 2-morpholone hydrochloride which is characterized by having a total of at least three substituents on the N-adjacent C atoms of the ring. The 2-morpholone so produced may be reduced to a polysubstituted aminodiol. The aminodiol so produced may be cyclized with an alkane sulfonic acid to yield a polysubstituted morpholine which could not otherwise have been made. The aminodiol may also be alkylated to produce diethers with polysubstituted N-adjacent C atoms. If the aminodiol is tosylated, a polysubstituted crown ether is produced with plural polyalkylene groups. The foregoing HEAA and related compounds are used as u-v light stabilizers in novel compositions in which a small but effective amount of one or more of the HEAA and related compounds is incorporated, in an amount sufficient to produce desirable stabilization against degradation by u-v light in a wide variety of organic materials.