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59 条记录 (耗时 0.021 秒)

    Process for the preparation of naproxene nitroxyalkylesters
    51.
    发明授权
    Process for the preparation of naproxene nitroxyalkylesters 有权
    制备萘普生硝基烷基酯的方法

    公开(公告)号：US07238829B2

    公开(公告)日：2007-07-03

    申请号：US10625558

    申请日：2003-07-24

    申请人： Francesca Benedini ,  Erminio Oldani ,  Graziano Castaldi ,  Antonio Tarquini

    发明人： Francesca Benedini ,  Erminio Oldani ,  Graziano Castaldi ,  Antonio Tarquini

    IPC分类号： C07C203/10

    CPC分类号： C07C201/02 ,  C07C203/04

    摘要： A process for obtaining nitroxyalklesters of the 2(S)(6-methoxy-2-naphthyl)-propanoic acid having an enantiomeric excess higher than or equal to 95%, preferably higher than or equal to 98%, characterized in that an halide of the 2-(S)-(6 methoxy-2-naphthyl)propanoic acid of formula A-Hal, wherein A is the acid acyl residue, is reacted in an inert organic solvent with an aliphatic nitroxyalkanol HO—Y—ONO2, wherein Y is a C2-C20 alkylene or a cycloalkylene from 3 to 8 carbon atoms, or an alkylene as defined containing a cycloalkylene as defined, in the presence of an inorganic base.

    摘要翻译： 一种获得具有高于或等于95％，优选高于或等于98％的对映异构体过量的2（S）（6-甲氧基-2-萘基） - 丙酸的硝基螺旋体的方法，其特征在于， 其中A是酸酰基残基的式A-Hal的2-（S） - （6甲氧基-2-萘基）丙酸在惰性有机溶剂中与脂族硝基链烷醇HO-Y-ONO 2，其中Y是C 2 -C 20亚烷基或3至8个碳原子的亚环烷基，或如所定义的含有如所定义的亚环烷基的亚烷基 在无机碱存在下进行。

    Process for the preparation of naproxene nitroxyalkylesters
    52.
    发明授权
    Process for the preparation of naproxene nitroxyalkylesters 有权
    制备萘普生硝基烷基酯的方法

    公开(公告)号：US06700011B1

    公开(公告)日：2004-03-02

    申请号：US10031412

    申请日：2002-01-18

    申请人： Francesca Benedini ,  Erminio Oldani ,  Graziano Castaldi ,  Antonio Tarquini

    发明人： Francesca Benedini ,  Erminio Oldani ,  Graziano Castaldi ,  Antonio Tarquini

    IPC分类号： C07C20304

    CPC分类号： C07C201/02 ,  C07C203/04

    摘要： A process for obtaining nitroxyalkylesters of the 2-(S)-(6-methoxy-2-naphthyl)-propanoic acid having an enantiomeric excess higher than or equal to 95%, preferably higher than or equal to 98%, characterized in that an halide of the 2-(S)-(6-methoxy-2-naphthyl)-propanoic acid of formula A-Hal, wherein A is the acid acyl residue, is reacted in an inert organic solvent with an aliphatic nitroxyalkanol HO—Y—ONO2, wherein Y is a C2-C20 alkylene or a cycloalkylene from 3 to 8 carbon atoms, or an alkylene as defined containing a cycloalkylene as defined, in the presence of an inorganic base.

    摘要翻译： 一种获得具有高于或等于95％，优选高于或等于98％的对映体过量的2-（S） - （6-甲氧基-2-萘基） - 丙酸的硝基烷基酯的方法，其特征在于， 其中A是酸酰基残基的式A-Hal的2-（S） - （6-甲氧基-2-萘基） - 丙酸的卤化物在惰性有机溶剂中与脂族硝基链烷醇HO-Y- ONO 2，其中Y是C 3 -C 20亚烷基或3至8个碳原子的亚环烷基，或在无机碱存在下含有如定义的亚环烷基的亚烷基。

    Benzoxazinone and benzothiazinone derivatives having cardiovascular activity
    53.
    发明授权
    Benzoxazinone and benzothiazinone derivatives having cardiovascular activity 失效
    具有心血管活性的苯并嗪酮和苯并噻嗪酮衍生物

    公开(公告)号：US5480882A

    公开(公告)日：1996-01-02

    申请号：US347217

    申请日：1994-11-23

    申请人： Alberto Sala ,  Roberto Barani ,  Francesca Benedini ,  Giorgio Bertolini ,  Giancarlo Dona ,  Gianni Gromo ,  Silvio Levi

    发明人： Alberto Sala ,  Roberto Barani ,  Francesca Benedini ,  Giorgio Bertolini ,  Giancarlo Dona ,  Gianni Gromo ,  Silvio Levi

    IPC分类号： A61K31/535 ,  A61K31/536 ,  A61K31/54 ,  A61K31/5415 ,  A61P9/00 ,  A61P9/08 ,  A61P9/10 ,  C07D265/22 ,  C07D279/08 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D265/22 ,  C07D279/08

    摘要： Compounds of formula I ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, methylene-dioxy or phenyl, which may be substituted by one or two groups independently selected from hydroxy, halogen, nitro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, COOR.sub.3, --CONR.sub.4 R.sub.5, ##STR2## --OCONR.sub.4 R.sub.5, --OCOR.sub.3, --NR.sub.4 R.sub.5, --OCOOR.sub.6, --NR.sub.3 COR.sub.7, --NR.sub.CONR.sub.4 R.sub.5, --N.dbd.CH--NR.sub.4 R.sub.5, NO.sub.2, CN, OH, SR.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 and R.sub.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, with the proviso that R.sub.1 and R.sub.2 cannot be hydrogen at the same time; X is oxygen or sulphur; Y represents a C.sub.2 -C.sub.6 alkylene chain or a C.sub.5 -C.sub.7 cycloalkylene group; and their pharmaceutically acceptable salts are provided and their use in pharmaceutical compositions which may be used in the treatment of cardiovascular diseases.

    摘要翻译： 式I的化合物其中R表示氢，C1-C6烷基，C5-C7环烷基，亚甲基 - 二氧基或苯基，其可以被一个或两个独立地选自羟基，卤素，硝基，C1 -C 1-6烷基或C 1 -C 6烷氧基; R1和R2独立地表示氢，COOR3，-CONR4R5，-OCONR4R5，-OCOR3，-NR4R5，-OCOOR6，-NR3COR7，-NRCONR4R5，-N = CH-NR4R5，NO2，CN，OH，SR3，其中R3 是氢或C1-C6烷基，R4和R5独立地是氢或C1-C6烷基，R6是C1-C6烷基，R7是氢，C1-C6烷基或C1-C6烷氧基，条件是R1和R2不能 同时是氢; X是氧或硫; Y表示C2-C6亚烷基链或C5-C7亚环烷基; 及其药学上可接受的盐，并且它们可用于可用于治疗心血管疾病的药物组合物中。

    Isoindoles having cardiovascular activity
    54.
    发明授权
    Isoindoles having cardiovascular activity 失效
    异吲哚酮具有心血管活性

    公开(公告)号：US5376673A

    公开(公告)日：1994-12-27

    申请号：US117162

    申请日：1993-09-17

    申请人： Alberto Sala ,  Silvio Levi ,  Francesca Benedini ,  Roberta Cereda ,  Piero Soldato

    发明人： Alberto Sala ,  Silvio Levi ,  Francesca Benedini ,  Roberta Cereda ,  Piero Soldato

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61P9/08 ,  A61P9/10 ,  C07D209/48

    CPC分类号： C07D209/48

    摘要： Isoindole compounds of the formula (I) ##STR1## wherein R.sub.1 represents hydrogen; C.sub.1 -C.sub.6 alkyl; benzyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, methylenedioxy; C.sub.2 -C.sub.8 aliphatic acyl; benzoyl optionally substituted with halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyl, C.sub.2 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, trifluoromethyl, methylenedioxy;R.sub.2 -R.sub.3 are selected independently from hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; trifluoromethyl; hydroxy; nitro; amino; mono or di C.sub.1 -C.sub.4 alkylamino; cyano; C.sub.1 -C.sub.6 alkoxy; C.sub.2 -C.sub.6 alkoxycarbonyl;Y is ethylene, or a straight or branched alkylene chain containing from 3 to 6 carbon atoms, and the salts thereof of pharmaceutically acceptable acids. The compounds possess antianginal activity and are used in the preparation of medicaments for antianginal therapy.

    摘要翻译： 式（I）的异吲哚化合物其中R 1表示氢; C1-C6烷基; 任选被卤素取代的苄基，羟基，C 1 -C 6烷氧基，亚甲二氧基; C 2 -C 8脂族酰基; 任选被卤素取代的苯甲酰基，羟基，C 1 -C 6烷氧基，C 2 -C 6烷酰基，C 2 -C 6烷酰氧基，C 1 -C 4烷基，三氟甲基，亚甲二氧基; R2-R3独立地选自氢; 卤素; C 1 -C 4烷基; 三氟甲基 羟基; 硝基 氨基; 单或二C1-C4烷基氨基; 氰基; C1-C6烷氧基; C2-C6烷氧基羰基; Y是乙烯，或含有3至6个碳原子的直链或支链亚烷基链及其药学上可接受的酸的盐。 该化合物具有抗心绞痛活性，并用于制备用于抗心绞痛治疗的药物。

    CRYSTALLINE FORMS OF ATORVASTATIN 4-(NITROOXY) BUTYL ESTER
    56.
    发明申请
    CRYSTALLINE FORMS OF ATORVASTATIN 4-(NITROOXY) BUTYL ESTER 审中-公开
    4-（硝基）丁酯酯的结晶形式

    公开(公告)号：US20100152274A1

    公开(公告)日：2010-06-17

    申请号：US12594511

    申请日：2008-03-19

    申请人： Francesca Benedini ,  Stefano Biondi ,  Annalisa Bonfanti ,  Fabio Nicoli

    发明人： Francesca Benedini ,  Stefano Biondi ,  Annalisa Bonfanti ,  Fabio Nicoli

    IPC分类号： A61K31/40 ,  C07D207/327 ,  A61P9/00 ,  A61P29/00 ,  A61P7/02 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16

    CPC分类号： C07D207/34

    摘要： The present invention relates to two crystalline forms designated as form A and form B, of (βR,δR)-2(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbon-yl]-1H-pyrrole-1-heptanoic acid 4-(nitrooxy)butyl ester (atorvastatin 4-(nitrooxy)butyl ester), represented by the formula (I), The invention also relates to processes for the preparation of the forms A and B, to pharmaceutical compositions comprising the two forms, and to their use for treating and/or preventing acute coronary syndromes, stroke, neurodegenerative disorders, such as Alzheimer's and Parkinson's disease as well as autoimmune diseases, such as multiple sclerosis.

    摘要翻译： 本发明涉及两种结晶形式，其命名为（＆bgr; R，δR）-2（4-氟苯基） - ，b-，δ-二羟基-5-（1-甲基乙基）-3-苯基的形式A和形式B -4 - [（苯基氨基）碳基] -1H-吡咯-1-庚酸4-（硝基氧基）丁酯（阿托伐他汀4-（硝基氧基）丁酯），由式（I）表示，本发明还涉及 用于制备形式A和B的方法，包含两种形式的药物组合物及其用于治疗和/或预防急性冠状动脉综合征，中风，神经变性疾病如阿尔茨海默病和帕金森病以及自身免疫疾病的用途 ，如多发性硬化症。

    Process for obtaining (nitroxymethyl)phenyl esters of salicylic acid derivatives
    58.
    发明授权
    Process for obtaining (nitroxymethyl)phenyl esters of salicylic acid derivatives 失效
    获得水杨酸衍生物的（硝基甲基）苯基酯的方法

    公开(公告)号：US06696591B1

    公开(公告)日：2004-02-24

    申请号：US10019316

    申请日：2002-01-09

    申请人： Graziano Castaldi ,  Erminio Oldani ,  Gabriele Razzetti ,  Francesca Benedini

    发明人： Graziano Castaldi ,  Erminio Oldani ,  Gabriele Razzetti ,  Francesca Benedini

    IPC分类号： C07C20304

    CPC分类号： C07C67/14 ,  C07C201/02 ,  C07C69/86 ,  C07C203/04

    摘要： A process for obtaining (nitroxymethyl)phenyl esters of salicylic acid derivatives of formula (I) wherein R1 is the OCOR3 group characterized in that it comprises the following steps: a) reaction of a halide of a salicylic acid derivative with hydroxybenzylacohol in the presence of a base: b) nutration of the obtained product in anhydrous conditions by a mixture of nitric acid with a different inorganic acid, or an organic acid, or an anhydride of one or two organic acids: c) recovery of the final product.

    摘要翻译： 一种获得式（I）的水杨酸衍生物（R 1为OCOR 3基团）的（硝基甲基）苯基酯的方法，其特征在于其包括以下步骤：a）水杨酸衍生物的卤化物与羟基苄基羟基醇在 碱：b）通过硝酸与不同无机酸或有机酸或一种或两种有机酸的酸酐的混合物在无水条件下使得到的产物营养化：c）回收最终产物。