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公开(公告)号：US20050119339A1
公开(公告)日：2005-06-02
申请号：US10625558
申请日：2003-07-24
IPC分类号： C07C201/02 , C07B53/00 , C07B61/00 , C07C203/04 , A61K31/21
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 orgariic 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。
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公开(公告)号：US07238829B2
公开(公告)日：2007-07-03
申请号：US10625558
申请日：2003-07-24
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。
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公开(公告)号：US06700011B1
公开(公告)日：2004-03-02
申请号：US10031412
申请日：2002-01-18
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。
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4.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
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。
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公开(公告)号：US07799784B2
公开(公告)日：2010-09-21
申请号：US12162529
申请日：2007-02-02
申请人： Francesca Benedini , Francesco Impagnatiello , Stefano Biondi , Ennio Ongini , Wesley Kwan Mung Chong
发明人： Francesca Benedini , Francesco Impagnatiello , Stefano Biondi , Ennio Ongini , Wesley Kwan Mung Chong
IPC分类号： A61K31/495
CPC分类号： C07D233/50 , C07D239/76
摘要： The present invention relates to alpha2-adrenergic receptor agonist nitrooxyderivatives, including the following structure, having improved pharmacological activity and enhanced tolerability. They can be employed for the treatment of ocular diseases, in particular high intraocular pressure and glaucoma.
摘要翻译： 本发明涉及具有改善的药理活性和增强的耐受性的α2-肾上腺素能受体激动剂硝基氧化酶，包括以下结构。 它们可用于治疗眼部疾病，特别是高眼内压和青光眼。
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公开(公告)号：US20080058392A1
公开(公告)日：2008-03-06
申请号：US11841628
申请日：2007-08-20
IPC分类号： A61K31/192 , A61K31/433 , A61P27/06 , C07C229/06
CPC分类号： C07C405/0016
摘要： Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
摘要翻译： 描述了具有改善的药理活性和增强的耐受性的前列腺素硝基衍生物。 可用于治疗青光眼和高眼压症。
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公开(公告)号：US20070060586A1
公开(公告)日：2007-03-15
申请号：US10581450
申请日：2004-12-01
IPC分类号： A61K31/5377 , A61K31/4704 , A61K31/405 , A61K31/34 , A61K31/21
CPC分类号： C07D285/10
摘要： The present invention relates to β-adrenergic blockers nitrooxyderivatives of general formula (I): A-(Y—ONO2)s and enantiomers and diastereoisomers and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them and their use for the treatment of hypertension, cardiovascular diseases, glaucoma, migraine headache and vascular diseases.
摘要翻译： 本发明涉及通式（I）的β-肾上腺素能阻断剂硝基氧基衍生物：其对映异构体和非对映异构体及其药学上可接受的盐， 含有它们的药物组合物及其用于治疗高血压，心血管疾病，青光眼，偏头痛和血管疾病的用途。
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公开(公告)号：US5589490A
公开(公告)日：1996-12-31
申请号：US254779
申请日：1994-06-06
申请人： Alberto Sala , Aldo Banfi , Francesca Benedini , Roberta Cereda
发明人： Alberto Sala , Aldo Banfi , Francesca Benedini , Roberta Cereda
IPC分类号： A61K31/165 , A61K31/22 , A61K31/235 , A61K31/34 , A61K31/341 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/425 , A61K31/426 , A61K31/4406 , A61K31/445 , A61P9/06 , A61P9/08 , A61P9/10 , A61P9/12 , C07C203/04 , C07C203/08 , C07C205/40 , C07C205/41 , C07C235/48 , C07C235/60 , C07C235/62 , C07C237/32 , C07C237/44 , C07C317/44 , C07D211/60 , C07D213/79 , C07D277/06 , C07D277/56 , C07D307/58 , C07D317/68 , C07D333/32 , A61K31/21
CPC分类号： C07C235/60 , C07C203/04 , C07C203/08 , C07C235/48 , C07C235/62 , C07D277/56 , C07C2101/14
摘要： ##STR1## Compounds of formula (I) wherein X, Y, R
1 and R
2 have the meanings specified in the specification, are endowed with cardiovascular activity.摘要翻译： （I）其中X，Y，R 1和R 2具有本说明书中规定的含义的式（I）化合物具有心血管活性。
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公开(公告)号：US20100234334A1
公开(公告)日：2010-09-16
申请号：US12525822
申请日：2008-01-28
申请人： Francesca Benedini , Stefano Biondi , Ennio Ongini
发明人： Francesca Benedini , Stefano Biondi , Ennio Ongini
IPC分类号： A61K31/58 , C07J71/00 , C07J5/00 , A61K31/573 , A61P29/00 , A61P11/00 , A61P1/02 , A61P1/04 , A61P19/02 , A61P17/00 , A61P27/00 , A61P9/00 , A61P5/00 , A61P3/10 , A61P35/00
CPC分类号： C07J41/005
摘要： The invention relates to nitrooxyderivative of corticosteriods of general formula (I) and pharmaceutical acceptable salts or stereoisomers thereof wherein R is the corticosteriod residue of formulas (II): The compounds are useful in the treatment of respiratory diseases, inflammatory diseases, dermatological disease and ocular diseases.
摘要翻译： 本发明涉及通式（I）的皮质类固醇和其药学上可接受的盐或立体异构体的硝基氧化酶，其中R是式（II）的皮质类固醇残基：该化合物可用于治疗呼吸系统疾病，炎性疾病，皮肤病和眼部 疾病
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公开(公告)号：US20100063035A1
公开(公告)日：2010-03-11
申请号：US12516460
申请日：2007-12-03
申请人： Francesca Benedini , Stefano Biondi , Ennio Ongini
发明人： Francesca Benedini , Stefano Biondi , Ennio Ongini
IPC分类号： A61K31/542 , A61K31/382 , C07D513/02 , C07D335/04 , A61P9/12 , A61P27/00 , A61P3/10
CPC分类号： C07D513/04 , C07D495/04
摘要： Nitroderivatives of dorzolamide and brinzolamide having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma, ocular hypertension, age-related macular degeneration, diabetic macular edema, diabetic retinopathy, hypertensive retinopathy and retinal vasculopathies.
摘要翻译： 描述了具有改善的药理活性和增强的耐受性的多佐胺和布林佐胺的硝基衍生物。 它们可用于治疗青光眼，高眼压症，年龄相关性黄斑变性，糖尿病性黄斑水肿，糖尿病性视网膜病变，高血压性视网膜病变和视网膜血管病变。
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