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    Derivatives of glutamic acid and aspartic acid
    55.
    发明授权
    Derivatives of glutamic acid and aspartic acid 失效
    谷氨酸和天冬氨酸的衍生物

    公开(公告)号：US4791215A

    公开(公告)日：1988-12-13

    申请号：US746065

    申请日：1985-06-18

    申请人： Luigi Rovati ,  Francesco Makovec ,  Rolando Chiste' ,  Paolo Senin

    发明人： Luigi Rovati ,  Francesco Makovec ,  Rolando Chiste' ,  Paolo Senin

    IPC分类号： A23K1/16 ,  A61K31/195 ,  A61K31/445 ,  A61K31/535 ,  C07C233/12 ,  C07C255/49 ,  C07C255/51 ,  C07C255/56 ,  C07D295/18 ,  C07D295/185 ,  C07D307/66 ,  C07D309/32 ,  C07C121/52 ,  A61K31/275

    CPC分类号： C07D295/185 ,  C07C255/00 ,  C07D307/66 ,  C07D309/32

    摘要： New derivatives of D,L-glutamic acid and D,L-aspartic acid are described having the formulae: ##STR1## in which n is equal to 1 or 2, R.sub.1 is a phenyl group mono-, di- or tri-substituted with linear or branched C.sub.1 -C.sub.4 alkyl groups, which may be the same or different, or with halogens, with a cyano group or a trifluoromethyl group, and in which R.sub.2 is selected from the group consisting of morpholino, piperidino and amino with one or two linear, branched or cyclic alkyl group substituents containing from 1 to 8 carbon atoms, which may be the same or different, or a pharmaceutically-acceptable salt thereof.The compounds have an antagonistic activity towards bioactive polypeptides and are useful particularly in the treatment of illnesses of the digestive system and the central nervous system, as pain killers, and for the treatment of anorexia and all those affections (for example tumours) in which exogenous or endogenous bioactive polypeptides are involved.

    摘要翻译： 描述了D，L-谷氨酸和D，L-天冬氨酸的新衍生物，其具有下式：其中n等于1或2，其中R 1是苯基单 - 可以相同或不同的直链或支链C 1 -C 4烷基二取代或三取代，或与卤素一起用氰基或三氟甲基取代，并且其中R2选自 吗啉代，哌啶子基和氨基，其具有一个或两个含有1至8个碳原子的直链，支链或环状烷基取代基，其可以相同或不同，或其药学上可接受的盐。 这些化合物对生物活性多肽具有拮抗作用，特别用于治疗消化系统和中枢神经系统的疾病，作为止痛药，以及用于治疗厌食症和所有这些感染（例如肿瘤），其中外源性 或内源性生物活性多肽。

    Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof
    57.
    发明申请
    Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof 有权
    具有抗收缩功能活性的抗蒽醌衍生物（抗cck-1），其制备方法及其药物用途

    公开(公告)号：US20060111304A1

    公开(公告)日：2006-05-25

    申请号：US10523075

    申请日：2003-07-23

    申请人： Francesco Makovec ,  Antonio Varnavas ,  Lucia Lassiani ,  Lucio Rovati

    发明人： Francesco Makovec ,  Antonio Varnavas ,  Lucia Lassiani ,  Lucio Rovati

    IPC分类号： A61K38/04 ,  A61K31/405 ,  A61K31/381 ,  A61K31/343 ,  C07D333/66 ,  C07D307/87 ,  C07D209/18

    CPC分类号： C07D333/68 ,  C07D209/42 ,  C07D307/84

    摘要： Anthranylic compounds having anti-CCK activity of general formula (I) in which, n is a whole number lying between 0 and 7; R1 is chosen independently from the groups (II), in which X1 is chosen independently from, S, O, NR2 and X2 is a group chosen from: H, C1-C4 alkyl, F, Cl, CF3, OCH3, OC2H5, CN; R2 is chosen from H or CH3; R3 is chosen from H, CH3, F, Cl, CF3, OCH3; R4 is chosen from the groups: H, —S—(CH2)m-R5, —SO2—(CH2)m-R5 (n different from 0), a branched alkyl group, a cyclo alkyl, a cyclo alkenyl, the group 1 or 2 adamantile, a phenyl group optionally substituted; R5 is chosen from the groups: H, linear or branched alkyl, cyclo alkyl, the group 1 or 2 adamantile, a suitably substituted phenyl group.

    摘要翻译： 具有通式（I）的抗CCK活性的蒽醌化合物，其中n是0和7之间的整数; R 1独立地选自基团（II），其中X 1独立地选自S，O，NR 2和X H 2是选自以下的基团：H，C 1 -C 4烷基，F，Cl，CF 3， ，OCH 3，OC 2 H 5，CN; R 2选自H或CH 3; R 3选自H，CH 3，F，Cl，CF 3，OCH 3， R 4选自以下基团：H，-S-（CH 2）2，mR 5，-SO 2， （CH 2）m R 5（n不同于0），支链烷基，环烷基，环烯基，1或2族金刚烷基， 任选取代的苯基; R 5选自以下基团：H，直链或支链烷基，环烷基，第1或2族金刚烷基，适当取代的苯基。

    Stable compounds of glucosamine sulphate
    60.
    发明授权
    Stable compounds of glucosamine sulphate 失效
    硫酸氨基葡萄糖稳定化合物

    公开(公告)号：US4642340A

    公开(公告)日：1987-02-10

    申请号：US373542

    申请日：1982-04-30

    申请人： Paolo Senin ,  Francesco Makovec ,  Luigi Rovati

    发明人： Paolo Senin ,  Francesco Makovec ,  Luigi Rovati

    IPC分类号： A61K31/70 ,  A61K31/7008 ,  A61P29/00 ,  C07H5/06

    CPC分类号： C07H5/06

    摘要： The compound consists of a mixed salt of glucosamine sulphate and sodium chloride corresponding to the formula: ##STR1## and is in the form of a crystalline powder with a melting point above 300.degree. C. The salt is stable at ambient temperatures and humidities and has pharmacological properties practically identical to those of glucosamine sulphate.

    摘要翻译： 该化合物由硫酸氨基葡萄糖和氯化钠的混合盐组成，相应于下式：，为熔点高于300℃的结晶性粉末形式。该盐在环境温度和湿度下是稳定的并具有 药理学性质实际上与硫酸葡糖胺相同。