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70 条记录 (耗时 0.026 秒)

    Use of neboglamine (CR 2249) as an antipsychotic and neuroprotective
    31.
    发明授权
    Use of neboglamine (CR 2249) as an antipsychotic and neuroprotective 失效
    使用神经酰胺（CR 2249）作为抗精神病药和神经保护剂

    公开(公告)号：US07737180B2

    公开(公告)日：2010-06-15

    申请号：US11569545

    申请日：2005-05-23

    申请人： Francesco Makovec ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Lucio Claudio Rovati

    IPC分类号： A61K31/195

    CPC分类号： A61K31/196 ,  A61K31/13

    摘要： Use of neboglamine, (S)-4-amino-N-(4,4-dimethylcyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), of the racemate thereof or of a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment of schizophrenia.

    摘要翻译： 在其外消旋物或其药学上可接受的盐中使用神经酰胺，（S）-4-氨基-N-（4,4-二甲基环己基）谷氨酸（CR 2249）（CAS登记号163000-63-3） 制备用于治疗精神分裂症的药物。

    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity
    32.
    发明授权
    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity 失效
    具有抗炎和免疫抑制活性的苯甲脒衍生物

    公开(公告)号：US07560591B2

    公开(公告)日：2009-07-14

    申请号：US12112299

    申请日：2008-04-30

    申请人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    IPC分类号： C07C335/16 ,  A61K31/17

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “—A—NH—” group.

    摘要翻译： 可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自具有1至3个碳的烷基 原子和氨基，未取代或被硝基或甲基取代，R 2独立地选自氢，具有1至4个碳原子的烷基，甲氧基，乙氧基，丙氧基，单 - ，双 - 或具有5至12个碳原子的三环环烷烃残基，未被取代或被甲基，甲氧基，羟基，氨基或卤素基团取代的金刚烷基，芳基，萘基或杂环基，R3和R4独立地选自氢和烷基 具有1至3个碳原子的基团，R 5表示独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n为0至6的整数，并且脒基为t 他相对于“-A-NH-”组的对位或间位。

    Novel Benzamidine Derivatives Having Anti-Inflammatory and Immunosuppressive Activity
    33.
    发明申请
    Novel Benzamidine Derivatives Having Anti-Inflammatory and Immunosuppressive Activity 失效
    具有抗炎和免疫抑制活性的新型苯甲脒衍生物

    公开(公告)号：US20080207764A1

    公开(公告)日：2008-08-28

    申请号：US12112299

    申请日：2008-04-30

    申请人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    IPC分类号： A61K31/155 ,  C07C257/10

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH-” group.

    摘要翻译： 可以由以下通式（I）表示的化合物：其中：A独立地选自甲酰胺基，硫代羧酰胺基和羰基，R 1选自 具有1至3个碳原子的烷基和未被取代或被硝基或甲基取代的氨基，R 2独立地选自氢，具有1至4个碳的烷基 原子，甲氧基，乙氧基，丙氧基，具有5至12个碳原子的单环，双环或三环环烷烃残基，金刚烷基，芳基，萘基或杂环基，未取代或被甲基，甲氧基，羟基， 氨基或卤素基团，R 3和R 4独立地选自氢和具有1至3个碳原子的烷基，R 5， 代表独立地选自氢和甲基，甲氧基和羟基的一个或两个取代基，n是a 整数为0至6，脒基为相对于“-A-NH-”基的对位或间位。

    Method for the preparation of crystalline dexloxiglumide and products obtained
    34.
    发明授权
    Method for the preparation of crystalline dexloxiglumide and products obtained 失效
    制备结晶脱氧氟沙星和所得产品的方法

    公开(公告)号：US07662994B2

    公开(公告)日：2010-02-16

    申请号：US10562013

    申请日：2004-06-21

    申请人： Francesco Makovec ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Lucio Claudio Rovati

    IPC分类号： C07C229/00

    CPC分类号： C07C237/22

    摘要： The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product with morphological and particle-size characteristics such as to favor its use in the preparation of oral pharmaceutical forms on an industrial scale.

    摘要翻译： 本发明描述了一种通过从异丙醚中结晶来纯化脱氧氟沙星的新方法，其允许以可再现的方式产生具有形态和粒度特征的产物，例如有利于其用于制备口服药物形式 工业规模。

    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity
    35.
    发明授权
    Benzamidine derivatives having anti-inflammatory and immunosuppressive activity 有权
    具有抗炎和免疫抑制活性的苯甲脒衍生物

    公开(公告)号：US07202277B2

    公开(公告)日：2007-04-10

    申请号：US10467624

    申请日：2002-02-06

    申请人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    发明人： Francesco Makovec ,  Simona Zanzola ,  Roberto Artusi ,  Lucio Claudio Rovati

    IPC分类号： A61K31/17

    CPC分类号： C07D213/40 ,  C07C257/14 ,  C07C279/18 ,  C07C279/36 ,  C07C335/20 ,  C07C2601/14 ,  C07C2603/74 ,  C07D209/14 ,  C07D209/40 ,  C07D277/48

    摘要： Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta position relative to the “-A-NH—” group.

    摘要翻译： 可以由通式（I）表示的化合物如下所示：

    Derivatives of glutamic acid and aspartic acid
    36.
    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。