5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives,
preparation thereof, intermediates thereof and drugs containing the same
    12.
    发明授权
    5H,10H-imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one derivatives, preparation thereof, intermediates thereof and drugs containing the same 失效
    5H,10H-咪唑并[1,2-a]茚并[1,2-e]吡嗪-4-酮衍生物,其制备方法,其中间体和含有它们的药物

    公开(公告)号:US5990108A

    公开(公告)日:1999-11-23

    申请号:US101428

    申请日:1998-07-09

    CPC分类号: C07D487/04 C07F9/6561

    摘要: Compounds of formula (I), wherein R is a hydrogen atom or a --COOH, -alk-COOH, --PO.sub.3 H.sub.2, --CH.sub.2 --PO.sub.3 H.sub.2, or --CH.dbd.CH--COOH radical, or a phenyl radical substituted by a carboxy radical, R.sub.1 is an alk-CN, -alk-COOH, -alk-Het, alk-PO.sub.3 H.sub.2 or -alk-CO--NH--SO.sub.2 R.sub.2 radical, R.sub.2 is an alkyl or phenyl radical, alk is an alkyl radical, Het is a saturated or unsaturated mono- or polycyclic heterocyclic ring containing 1-9 carbon atoms and one or more heteroatoms selected from O, S and N, said heterocyclic ring optionally being substituted by one or more alkyl, phenyl or phenylalkyl radicals, with the proviso that when R is a hydrogen atom or a --COOH or --PO.sub.3 H.sub.2 radical, R.sub.1 cannot be -alk-COOH, isomers, racemic mixtures, enantiomers and diastereoisomers thereof, salts thereof, the preparation thereof, intermediates thereof and drugs containing said compounds, are disclosed. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor, and specifically ligands for NMDA receptor glycine modulator sites. ##STR1##

    摘要翻译: PCT No.PCT / FR97 / 00019 Sec。 371日期:1998年7月9日 102(e)日期1998年7月9日PCT 1997年1月6日PCT PCT。 出版物WO97 / 25328 日期:1997年7月17日式(I)化合物其中R为氢原子或-COOH,-alk-COOH,-PO3H2,-CH2-PO3H2或-CH = CH-COOH基,或苯基取代 通过羧基,R 1是烷基-C CN,-alk-COOH,-alk-Het,alk-PO 3 H 2或-alk -CO-NH-SO 2 R 2基团,R 2是烷基或苯基, Het是含有1-9个碳原子和一个或多个选自O,S和N的杂原子的饱和或不饱和单环或多环杂环,所述杂环任选被一个或多个烷基,苯基或苯基烷基取代,其中 条件是当R是氢原子或-COOH或-PO 3 H 2基团时,R 1不能是-alk COOH,其异构体,外消旋混合物,对映异构体和非对映异构体,其盐,其制备,其中间体和含有所述化合物的药物, 被披露。 式(I)化合物具有有价值的药理学性质,也是也称为quisqualate受体的α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)受体的拮抗剂。 此外,式(I)化合物是N-甲基-D-天冬氨酸(NMDA)受体的非竞争性拮抗剂,特别是NMDA受体甘氨酸调节剂位点的配体。

    Styryl thiol/disulfide compound with a hydroxy(cyclo)alkylamino unit, process for lightening keratin materials using same
    15.
    发明授权
    Styryl thiol/disulfide compound with a hydroxy(cyclo)alkylamino unit, process for lightening keratin materials using same 有权
    具有羟基(环)烷基氨基单元的苯乙烯基硫醇/二硫化物化合物,使用其来减轻角蛋白材料的方法

    公开(公告)号:US07717964B2

    公开(公告)日:2010-05-18

    申请号:US12234001

    申请日:2008-09-19

    IPC分类号: A61Q5/10 C07C321/00

    摘要: The disclosure relates to the dyeing of keratin materials using styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dyes. Disclosed herein is a dye composition comprising a styryl hydroxy(cyclo)alkylamino thiol/disulfide fluorescent dye and a dyeing process with, for example, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are novel thiol/disulfide fluorescent dyes and the uses thereof in lightening keratin materials. This composition makes it possible to obtain a lightening effect which can be resistant and visible on dark keratin fibers.

    摘要翻译: 本公开涉及使用苯乙烯基羟基(环)烷基氨基硫醇/二硫化物荧光染料染色角蛋白材料。 本文公开了包含苯乙烯基羟基(环)烷基氨基硫醇/二硫化物荧光染料和染色方法的染料组合物,其使用所述组合物具有例如对角蛋白材料如头发的减轻作用。 本文公开的是新型硫醇/二硫化物荧光染料及其在减轻角蛋白材料中的用途。 该组合物可以获得在黑色角蛋白纤维上可以耐受和可见的减轻效果。

    Method of preparing an acylimidazolium-type reagent
    16.
    发明申请
    Method of preparing an acylimidazolium-type reagent 审中-公开
    制备酰基咪唑型试剂的方法

    公开(公告)号:US20060149051A1

    公开(公告)日:2006-07-06

    申请号:US10542249

    申请日:2004-01-14

    IPC分类号: C07H21/04 C07D233/91

    CPC分类号: C07D233/54

    摘要: The invention relates to a method of preparing an acylimidazolium-type reagent. More specifically, the invention relates to a salt of N-(benzyloxycarbonyl)-N′-methylimidazolium. The inventive method of preparing an acylimidazolium-type reagent is characterised in that it is obtained by: (i) reacting a reagent comprising a —COX group having formula (II) and an imidazole reagent having formula (III); and (ii) subsequently, adding a strong acid HY to the product thus obtained, said acid having a pKa of less than 1, which produces the desired reagent.

    摘要翻译: 本发明涉及一种制备酰基咪唑型试剂的方法。 更具体地说,本发明涉及N-(苄氧基羰基)-N'-甲基咪唑鎓盐。 制备酰基咪唑型试剂的本发明方法的特征在于:(i)使包含式(II)的-COX基团和具有式(III)的咪唑试剂的试剂反应; 和(ii)随后,向由此获得的产物中加入强酸HY,所述酸的pKa小于1,产生所需试剂。

    N-phenylglycinamide CCK antagonists and pharmaceutical compositions
containing them
    20.
    发明授权
    N-phenylglycinamide CCK antagonists and pharmaceutical compositions containing them 失效
    N-苯基甘氨酰胺CCK拮抗剂和含有它们的药物组合物

    公开(公告)号:US5475106A

    公开(公告)日:1995-12-12

    申请号:US924065

    申请日:1992-10-08

    CPC分类号: C07K5/06026 A61K38/00

    摘要: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom, an alkyl or alkoxycarbonyl radical or a phenyl radical, optionally substituted,R.sub.2 represents an alkoxy, optionally substituted cycloalkyloxy, cycloalkylalkyloxy, phenylalkyloxy, polyfluoroalkyloxy or cinnamyloxy radical or a radical --NR.sub.5 R.sub.6,R.sub.3 represents a phenylamino radical in which the phenyl ring is optionally substituted, an optionally substituted phenyl radical or a naphthyl, indolyl or quinolyl radical,R.sub.4 represents a substituted phenyl radical,R.sub.5 and R.sub.6, which may be identical or different, represent a hydrogen atom or an alkyl, optionally substituted phenyl, indanyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical, or alternatively R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocycle, their preparation and medicinal products containing them.

    摘要翻译: PCT No.PCT / FR91 / 00174 Sec。 371日期:1992年10月8日 102(e)日期1992年10月8日PCT 1991年3月5日PCT公布。 第WO91 / 13907号公报 1991年9月19日,化学式:其中R 1表示氢原子,烷基或烷氧基羰基或苯基,任意取代的式(I)化合物:R 2表示烷氧基,任选取代的环烷氧基,环烷基烷氧基,苯基烷氧基 ,多氟烷氧基或肉桂氧基或自由基-NR5R6,R3表示苯基氨基,其中苯环任选被取代,任选取代的苯基或萘基,吲哚基或喹啉基,R4表示取代的苯基,R5和R6, 其可以相同或不同,表示氢原子或烷基,任选取代的苯基,二氢化茚基,环烷基烷基,环烷基或苯基烷基,或者R5和R6与它们所连接的氮原子一起形成杂环,它们 制剂和含有它们的药用产品。