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41. 发明授权

US06700011B1 Process for the preparation of naproxene nitroxyalkylesters 有权
标题翻译：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。

42. 发明授权

US5480882A Benzoxazinone and benzothiazinone derivatives having cardiovascular activity 失效
标题翻译：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。

43. 发明授权

US5376673A Isoindoles having cardiovascular activity 失效
标题翻译：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。

44. 发明授权

US08101658B2 Nitric oxide donating prostamides 有权
标题翻译：一氧化氮捐赠前列腺酰胺
公开(公告)号：US08101658B2
公开(公告)日：2012-01-24
申请号：US12991855
申请日：2009-05-11
申请人： Francesca Benedini , Stefano Biondi , Valerio Chiroli , Wesley Kwan Mung Chong , Liming Dong , Achim Hans-Peter Krauss , Fabio Nicoli , Ganesh Prasanna , William Francois Vernier , Yi Yang
发明人： Francesca Benedini , Stefano Biondi , Valerio Chiroli , Wesley Kwan Mung Chong , Liming Dong , Achim Hans-Peter Krauss , Fabio Nicoli , Ganesh Prasanna , William Francois Vernier , Yi Yang
IPC分类号： A61K31/04 , A61K31/16 , C07C203/04 , C07C291/00
CPC分类号： C07C405/00 , C07C291/02 , C07C2601/02 , C07C2601/08
摘要： Nitroderivatives of prostaglandins 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的硝基衍生物。可用于治疗青光眼和高眼压症。

45. 发明申请

US20110092590A1 NITRIC OXIDE DONATING PROSTAMIDES 有权
标题翻译：硝酸氧化物引发剂
公开(公告)号：US20110092590A1
公开(公告)日：2011-04-21
申请号：US12991855
申请日：2009-05-11
申请人： Francesca Benedini , Stefano Biondi , Valerio Chiroli , Wesley Kwan Mung Chong , Liming Dong , Achim Hans-Peter Krauss , Fabio Nicoli , Ganesh Prasanna , William Francois Vernier , Yi Yang
发明人： Francesca Benedini , Stefano Biondi , Valerio Chiroli , Wesley Kwan Mung Chong , Liming Dong , Achim Hans-Peter Krauss , Fabio Nicoli , Ganesh Prasanna , William Francois Vernier , Yi Yang
IPC分类号： A61K31/21 , C07C203/04 , A61P27/02 , A61P27/06
CPC分类号： C07C405/00 , C07C291/02 , C07C2601/02 , C07C2601/08
摘要： Nitroderivatives of prostaglandins 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的硝基衍生物。可用于治疗青光眼和高眼压症。

46. 发明授权

US07723382B2 Process for preparing nitrooxyalkyl substituted esters of carboxylic acids, intermediates useful in said process and preparation thereof 失效
标题翻译：制备硝基氧基烷基取代的羧酸酯的方法，可用于所述方法的中间体及其制备方法
公开(公告)号：US07723382B2
公开(公告)日：2010-05-25
申请号：US10522986
申请日：2003-08-06
申请人： Piero del Soldato , Giancarlo Santus , Francesca Benedini
发明人： Piero del Soldato , Giancarlo Santus , Francesca Benedini
IPC分类号： A61K31/21 , A61K31/40 , C07C203/04 , C07C69/00
CPC分类号： C07C269/06 , C07C67/10 , C07C69/734 , C07C201/02 , C07C203/04 , C07C271/28 , C07C303/28 , C07C309/73
摘要： The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of a drug and R1-R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1-R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.
摘要翻译：本发明涉及制备通式（A）化合物的方法，如说明书所述，其中R为药物基团，R 1 -R 12为氢或烷基，m，n，o，q， r和s各自独立地为0〜6的整数，p为0或1，X为O，S，SO，SO 2，NR 13或PR 13或芳基杂芳基，所述方法包括使式 B）R-COOZ（B）其中R如上所定义，Z是氢或选自：Li +，Na +，K +，Ca ++，Mg ++，四烷基铵，四烷基鏻与式（C）化合物的阳离子，如其描述其中R1-R12和m，n，o，p，q，r，s如上所定义，Y是合适的离去基团。

47. 发明授权

US07629368B2 Nitroderivatives as drugs for diseases having an inflammatory basis 失效
标题翻译：硝基衍生物作为具有炎症基础的疾病的药物
公开(公告)号：US07629368B2
公开(公告)日：2009-12-08
申请号：US12099636
申请日：2008-04-08
申请人： Piero Del Soldato , Francesca Benedini , Patrizia Antognazza
发明人： Piero Del Soldato , Francesca Benedini , Patrizia Antognazza
IPC分类号： A61K31/44 , A61K31/21
CPC分类号： C07D213/30 , A61K31/21 , A61K31/44 , C07C203/04 , C07C233/25 , C07C317/46 , C07C323/60
摘要： Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, Having the following general formula (I): A—X1—L—(W)p—NO2 wherein A contains the radical of a drug, X1 and W are bivalent radicals, L is a covalent bond or oxygen, sulphur, NR1e wherein R1e is H or a C1-C5 linear or branched alkyl.
摘要翻译：具有以下通式（I）：A-X1-L-（W）p-NO2，其中A含有药物基团，X1和W是用于治疗具有炎性基础的化合物或其盐的疾病。二价基团，L为共价键或氧，硫，NR1e，其中R1e为H或C1-C5直链或支链烷基。

48. 发明授权

US07199258B2 Process for preparing nitrooxyderivatives of naproxen 失效
标题翻译：制备萘普生硝基氧化酶的方法
公开(公告)号：US07199258B2
公开(公告)日：2007-04-03
申请号：US10523722
申请日：2003-08-06
申请人： Piero Del Soldato , Giancarlo Santus , Francesca Benedini
发明人： Piero Del Soldato , Giancarlo Santus , Francesca Benedini
IPC分类号： C07C203/04
CPC分类号： C07C269/06 , C07C67/10 , C07C69/734 , C07C201/02 , C07C203/04 , C07C271/28 , C07C303/28 , C07C309/73
摘要： The present invention refers to a process for preparing a compound of general formula (A), as reported in the description, wherein R is a radical of naproxen or bromonaproxen and R1–R12 are hydrogen or alkyl groups, m, n, o, q, r and s are each independently an integer from 0 to 6, and p is 0 or 1, and and X is O, S, SO, SO2, NR13 or PR13 or an aryl, heteroaryl group, said process comprising reacting a compound of formula (B) R—COOZ (B) wherein R is as defined above and Z is hydrogen or a cation selected from: Li+, Na+, K+, Ca++, Mg++, tetralkylammonium, tetralkylphosphonium, with a compound of formula (C), as reported in the description, wherein R1–R12 and m, n, o, p, q, r, s are as defined above and Y is a suitable leaving group.
摘要翻译：本发明涉及制备通式（A）化合物的方法，如说明书中所报导的，其中R是萘普生或溴苯丙酮的基团，R 1 -R 12， / SUB>为氢或烷基，m，n，o，q，r和s各自独立地为0至6的整数，p为0或1，X为O，S，SO，SO NR 2，NR 13或NR 13或芳基杂芳基，所述方法包括使式

49. 发明授权

US06613784B1 Nitroxyderivatives having antinflammatory, analgesic and antithrombotic activity 失效
标题翻译：具有抗炎，镇痛和抗血栓形成活性的硝基衍生物
公开(公告)号：US06613784B1
公开(公告)日：2003-09-02
申请号：US09926095
申请日：2001-08-30
申请人： Francesca Benedini , Piero Del Soldato
发明人： Francesca Benedini , Piero Del Soldato
IPC分类号： C07D21330
CPC分类号： C07D213/30 , C07D401/12
摘要： Organic or inorganic salts of compounds of general formula: A—X1—N(O)z for use as medicaments having anti-inflammatory, analgesic and antithrombotic activity, wherein A is R(COXu)t wherein t is 0 or 1; u is 0 or 1 and X is O, NH, NR1c wherein R1c us a C1-C10 alkyl and R is, for example, (Ia) wherein R1 is acetoxy, preferably in ortho position with respect to —CO— and R2 is hydrogen or acetylsalicylsalicylic acid derivatives; and X1 is the formula (B), Y being a ring containing at least one salified nitrogen atom.
摘要翻译：用作具有抗炎，镇痛和抗血栓形成活性的药物的通式为A-X1-N（O）z的化合物的有机或无机盐，其中A为R（COXu）t，其中t为0或1; u为0或1，X为O，NH，NR1c，其中R1c为C1-C10烷基，R为例如（Ia），其中R1为乙酰氧基，优选为相对于-CO-的邻位，R2为氢或乙酰水杨基水杨酸衍生物; X1为式（B），Y为含有至少一个成盐氮原子的环。

50. 发明授权

US07465803B2 Nitroderivatives as drugs for diseases having an inflammatory basis 失效
标题翻译：硝基衍生物作为具有炎症基础的疾病的药物
公开(公告)号：US07465803B2
公开(公告)日：2008-12-16
申请号：US10398289
申请日：2001-10-09
申请人： Piero Del Soldato , Francesca Benedini , Patrizia Antognazza
发明人： Piero Del Soldato , Francesca Benedini , Patrizia Antognazza
IPC分类号： C07D211/70 , C07D213/55
CPC分类号： C07D213/30 , A61K31/21 , A61K31/44 , C07C203/04 , C07C233/25 , C07C317/46 , C07C323/60
摘要： Use for the treatment of diseases having an inflammatory basis of compounds or salts thereof, having the following general formula (I): A-X1-L-(W)p—NO2 wherein A contains the radical of a drug, X1 and W are bivalent radicals, p is an integer equal to 1 or 0, and L is a covalent bond, CO, oxygen, sulphur, or NR1C where R1C is H or a C1-C5 linear or branched alkyl.
摘要翻译：用于治疗具有以下通式（I）的化合物或其盐的炎症基础的疾病：A-X1-L-（W）p-NO2其中A含有药物基团，X1和W是二价基团，p是等于1或0的整数，L是共价键，CO，氧，硫或NR 1 C，其中R 1 C是H或C 1 -C 5直链或支链烷基。

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