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    Method for the preparation of crystalline dexloxiglumide and products obtained
    21.
    发明申请
    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：US20060154987A1

    公开(公告)日：2006-07-13

    申请号：US10562013

    申请日：2004-06-21

    申请人： Francesco Makovec ,  Lucio Rovati

    发明人： Francesco Makovec ,  Lucio Rovati

    IPC分类号： A61K31/195 ,  C07C231/24

    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 favour 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。

    Oxygenated-alkyl derivatives of glutamic and aspartic acids with antagonistic activity to bio-active polypeptides and a method for their preparation
    22.
    发明授权
    Oxygenated-alkyl derivatives of glutamic and aspartic acids with antagonistic activity to bio-active polypeptides and a method for their preparation 失效
    对生物活性多肽具有拮抗活性的谷氨酸和天冬氨酸的加氧烷基衍生物及其制备方法

    公开(公告)号：US4769389A

    公开(公告)日：1988-09-06

    申请号：US942751

    申请日：1986-12-17

    申请人： Francesco Makovec ,  Rolando Chiste' ,  Lucio Rovati ,  Luigi Rovati

    发明人： Francesco Makovec ,  Rolando Chiste' ,  Lucio Rovati ,  Luigi Rovati

    IPC分类号： A61K31/195 ,  A61P1/00 ,  A61P25/08 ,  C07C233/30 ,  C07C233/45 ,  C07C237/22 ,  C07C103/84

    CPC分类号： A61K31/195 ,  C07C233/30 ,  C07C233/45

    摘要： New Orginal derivates of D,L-glutamic acid and D,L-aspartic acid are described having the formula: ##STR1## where n is 1 or 2, R.sub.1 is a mono- or di-substituted phenyl group substituted with halogens such as chlorine and fluorine or with a methyl group in the 3 and 4 positions and in which R.sub.2 consists of a linear or branched alkyl group with 4 to 7 carbon atoms (preferably a pentyl group) and R.sub.3 is an alkyl group having 3 to 6 carbon atoms overall and containing an oxygen atom in the form of an either linkage, such as for example the groups 2-ethoxyethyl, 3-methoxypropyl, 3-ethoxypropyl etc. or in the form of a hydroxyl group such as for example 3-hydroxypropyl etc.The compounds have antagonistic activity towards bio-active polypeptides and are usable particularly in the treatment of illnesses of the digestive tract, of the central nervous system and anorexia and of all those affections (for example tumours) in which exogenic or endogenic bio-active polypeptides are involved.

    摘要翻译： 描述了具有下式的D，L-谷氨酸和D，L-天冬氨酸的新的原始衍生物：其中n是1或2，R1是被卤素如氯取代的单或二取代的苯基 和氟或在3和4位具有甲基，其中R 2由具有4至7个碳原子的直链或支链烷基（优选戊基）组成，并且R 3是总共具有3至6个碳原子的烷基 并且含有二键形式的氧原子，例如2-乙氧基乙基，3-甲氧基丙基，3-乙氧基丙基等，或以羟基形式例如3-羟基丙基等。 化合物对生物活性多肽具有拮抗活性，并且特别可用于治疗消化道，中枢神经系统和厌食症以及所有这些感染（例如肿瘤）的疾病，其中外源性或内源性生物活性多肽是 涉及。

    Novel benzamidine derivatives having anti-inflammatory and immunosuppressive activity
    23.
    发明申请
    Novel benzamidine derivatives having anti-inflammatory and immunosuppressive activity 审中-公开
    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：US20070135523A1

    公开(公告)日：2007-06-14

    申请号：US11652675

    申请日：2007-01-12

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

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

    IPC分类号： A61K31/165 ,  A61K31/16 ,  C07C275/42

    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。

    Preparation with an acrylic-based, adhesive copolymeric matrix for the transdermal delivery of estradiol
    25.
    发明授权
    Preparation with an acrylic-based, adhesive copolymeric matrix for the transdermal delivery of estradiol 失效
    使用丙烯酸基粘合剂共聚物基质制备用于经皮递送雌二醇

    公开(公告)号：US6156335A

    公开(公告)日：2000-12-05

    申请号：US244132

    申请日：1994-07-15

    申请人： Luigi Rovati ,  Lucio Rovati ,  Francesco Makovec ,  Gunter Cordes ,  Wilfried Fischer

    发明人： Luigi Rovati ,  Lucio Rovati ,  Francesco Makovec ,  Gunter Cordes ,  Wilfried Fischer

    IPC分类号： A61K9/70 ,  A61K31/565 ,  C07J1/00 ,  A61F13/02

    CPC分类号： A61K9/7061 ,  A61K31/565

    摘要： The invention is represented by a transdermal medicated patch for the extended release of 17.beta.-estradiol to the skin. The transdermal patch is formed by an outer covering, a matrix containing from 1% to 5% (w/w) 17.beta.-estradiol, and a protective liner which is removed before use. The matrix is formed of pressure-sensitive adhesive acrylic copolymers, in which the active ingredient is dissolved or dispersed. The acrylic copolymers are obtained by radical copolymerization of 2-ethylhexyl acrylate, methyl acrylate, acrylic acid, vinyl acetate, hydroxyethyl acrylate or a mixture thereof. Optionally quantities of less than 0.5% (w/w) of other substances may be added.

    摘要翻译： PCT No.PCT / EP92 / 02704 Sec。 371日期1994年7月15日 102（e）日期1994年7月15日PCT 1991年11月24日PCT公布。 出版物WO93 / 10772 日期1993年6月10日本发明由用于将17β-雌二醇延长释放至皮肤的透皮药物贴剂代表。 透皮贴剂由外覆盖物，含有1％至5％（w / w）17β-雌二醇的基质和在使用前除去的保护性衬垫形成。 基质由粘合丙烯酸类共聚物形成，其中活性成分溶解或分散。 丙烯酸共聚物通过丙烯酸2-乙基己酯，丙烯酸甲酯，丙烯酸，乙酸乙烯酯，丙烯酸羟乙酯或其混合物的自由基共聚得到。 可选地，可以加入少于0.5％（w / w）的其它物质。

    Anthranyl derivatives having an anticholecystokinin activity (anti-cck-1), a process for their preparation, and pharmaceutical use thereof
    26.
    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。

    Pyrrole derivatives with angiotensin II antagonist activity
    29.
    发明授权
    Pyrrole derivatives with angiotensin II antagonist activity 有权
    具有血管紧张素II拮抗剂活性的吡咯衍生物

    公开(公告)号：US07906501B2

    公开(公告)日：2011-03-15

    申请号：US11568362

    申请日：2005-04-27

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

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

    IPC分类号： A61K31/41 ,  C07D293/00 ,  C07D257/04 ,  C07D403/10 ,  C07D295/04

    CPC分类号： C07D403/10

    摘要： Compounds which may be represented by the general formula (I) shown below and in which: R1 is a group independently selected from among: CHO, —COOH, —CH2OH R2 is hydrogen or a linear or branched C1-C6 alkyl group R3 is hydrogen or a halogen group selected from among Cl and Br R4 is a linear or branched C3-C5 alkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the AT1 receptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy.

    摘要翻译： 可以由下述通式（I）表示的化合物，其中：R 1是独立地选自：CHO，-COOH，-CH 2 OH的基团R 2是氢或直链或支链C 1 -C 6烷基R 3是氢 或选自Cl和Br R4中的卤素基团是直链或支链C 3 -C 5烷基及其药学上可接受的盐，例如钠盐或钾盐。 该化合物显示出有效和选择性的所有拮抗剂活性，并且可用于治疗其中AT1受体的全部或过表达的合成升高可能起主要病理学作用的任何障碍，如在动脉高血压，充血性心功能不全，血小板 与其相关的聚集和紊乱，例如心肌和脑梗死，肾缺血，静脉和动脉血栓形成，外周血管病变，肺动脉高压，糖尿病，糖尿病性神经病，青光眼和糖尿病性视网膜病变。