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41. 发明授权

US5489582A 14-deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and pharmaceutical composition comprising same for treating cardiovascular disorders 失效
标题翻译： 14-脱氧-14α-硬骨苷脂3β-硫代衍生物和包含其的用于治疗心血管疾病的药物组合物
公开(公告)号：US5489582A
公开(公告)日：1996-02-06
申请号：US80525
申请日：1993-06-24
申请人： Mauro Gobbini , Luigi Bernardi , Mara Ferrandi , Piero Melloni , Luisa Quadri , Roberto Villa
发明人： Mauro Gobbini , Luigi Bernardi , Mara Ferrandi , Piero Melloni , Luisa Quadri , Roberto Villa
IPC分类号： A61K31/585 , A61P9/00 , A61P9/12 , C07J19/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07D405/12
CPC分类号： C07J43/003 , C07J19/00 , C07J31/003 , C07J41/0055 , C07J41/0088
摘要： 14-Deoxy-14.alpha.-cardenolides 3.beta.-thioderivatives and pharmaceutical compositions comprising same for treating cardiovascular disorders, such as heart failure and hypertension, are disclosed.
摘要翻译：公开了用于治疗心血管疾病如心力衰竭和高血压的14-脱氧-14α-硬骨苷脂3β-硫代衍生物和包含其的药物组合物。

42. 发明授权

US5298022A Wearable artificial pancreas 失效
标题翻译：可穿戴人造胰腺
公开(公告)号：US5298022A
公开(公告)日：1994-03-29
申请号：US238
申请日：1993-01-04
申请人： Luigi Bernardi
发明人： Luigi Bernardi
IPC分类号： A61B5/00 , A61M31/00
CPC分类号： A61B5/14865 , A61B5/14528
摘要： A device for the continuous quantitative determination of glucose in the blood of a diabetic patient over a period of 24-36 hours, comprises a container for a saline solution with heparin, a microdialyzing needle inserted into a vein of a diabetic patient, a pump for injecting the solution into the microdialyzing needle, a semipermeable hollow fiber membrane located externally of the needle whereby dialysis occurs between the blood and the solution and only glucose and other substances of low molecular weight below 100,000 daltons go through the membrane and the concentration of the glucose and other substances of low molecular weight below 100,000 daltons inside the needle is proportional to that of the external side of the membrane. The needle is provided with an outgoing conduit, the conduit leads to a sensor, which comprises an enzymatic membrane coupled with a Platinum-Silver electrode. The glucose goes into the conduit, oxidation of glucose to gluconic acid and hydrogen peroxide occurs and the hydrogen peroxide is decomposed to give H.sub.2 O and oxygen with the liberation of two electrons whereby electric current is produced and the concentration of glucose in the blood is determined by determining the amount of current produced.It is possible to vary the dilution ratio of the fluid circulating inside the microdialyzing needle by varying the pump speed so that it is possible to have a ratio of the glucose containing saline solution to the actual concentration of glucose in the blood of 1/2-1/20.
摘要翻译：用于在24-36小时内连续定量测定糖尿病患者血液中的葡萄糖的装置包括用于肝素盐溶液的容器，插入糖尿病患者静脉的微透析针，将溶液注入微型脱水针，位于针的外部的半透性中空纤维膜，其中血液和溶液之间发生透析，并且仅葡萄糖和低分子量低于100,000道尔顿的其它物质通过膜并且葡萄糖的浓度和低于100,000道尔顿内的低分子量的其他物质与膜的外侧成比例。针设置有输出导管，导管通向传感器，传感器包括与铂 - 银电极耦合的酶膜。葡萄糖进入导管，葡萄糖氧化成葡萄糖酸，过氧化氢发生，过氧化氢分解，得到H2O和氧，释放出两个电子，由此产生电流，血液中的葡萄糖浓度由确定产生的电流量。可以通过改变泵速来改变在微脱水针内循环的流体的稀释比，使得可以使含葡萄糖的盐溶液与血液中葡萄糖的实际浓度的比例为1 / 2- 1/20。

43. 发明授权

US5176632A Wearable artificial pancreas 失效
标题翻译：佩戴人造皮革
公开(公告)号：US5176632A
公开(公告)日：1993-01-05
申请号：US527129
申请日：1990-05-22
申请人： Luigi Bernardi
发明人： Luigi Bernardi
IPC分类号： A61B5/00
CPC分类号： A61B5/14865 , A61B5/14528
摘要： A device for the continuous quantitative determination of glucose in the blood of a diabetic patient over a period of 24-36 hours, comprises a container for a saline solution with heparin, a microdialyzing needle inserted into a vein of a diabetic patient, a pump for injecting the solution into the microdialyzing needle, a semipermeable hollow fiber membrane located externally of the needle whereby dialysis occurs between the blood and the solution and only glucose and other substances of low molecular weight below 100,000 daltons go through the membrane and the concentration of the glucose and other substances of low molecular weight below 100,000 daltons inside the needle is proportional to that of the external side of the membrane. The needle is provided with an outgoing conduit, the conduit leads to a sensor, which comprises an enzymatic membrane coupled with a Platinum-Silver electrode. The glucose goes into the conduit, oxidation of glucose to gluconic acid and hydrogen peroxide occurs and the hydrogen peroxide is decomposed to give H.sub.2 O and oxygen with the liberation of two electrons whereby electric current is produced and the concentration of glucose in the blood is determined by determining the amount of current produced.

44. 发明授权

US4746666A Ergoline compounds useful as antiparkinson agents 失效
标题翻译：可用作抗帕金森病药物的魔芋醇化合物
公开(公告)号：US4746666A
公开(公告)日：1988-05-24
申请号：US874413
申请日：1986-06-16
申请人： Luigi Bernardi , Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi
发明人： Luigi Bernardi , Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi
IPC分类号： A61K31/48 , A61K31/50 , A61K31/505 , A61P25/00 , C07D457/02 , C07D457/04
CPC分类号： C07D457/02
摘要： Ergoline derivatives of the formula I ##STR1## wherein R.sub.1 =H,CH.sub.3 ; R.sub.2 =H, halogen, CH.sub.3, CN, C.sub.1 -C.sub.4 alkylthio or phenylthio; R.sub.3 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.4 =H, OCH.sub.3 ; R.sub.5 =H and R.sub.6 =--CH.dbd.CH--CONHR.sub.7 or R.sub.5 and R.sub.6 =.dbd.CH--CONHR.sub.7 ; R.sub.7 =2-thiazolyl, 3-pyridazinyl, 1,3,4-thiadiazol-2-yl or 4-pyrimidinyl group optionally substituted, and pharmaceutically acceptable salts thereof, display activity on the Central Nervous System and are useful as antiprolactinic agents. Their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：式I的吡咯啉衍生物其中R 1 = H，CH 3; R2 = H，卤素，CH3，CN，C1-C4烷硫基或苯硫基; R3 = C1-C4烃; R4 = H，OCH3; R5 = H，R6 = -CH = CH-CONHR7或R5和R6 = CH-CONHR7; R7 = 2-噻唑基，3-哒嗪基，1,3,4-噻二唑-2-基或任选取代的4-嘧啶基及其药学上可接受的盐，在中枢神经系统上显示活性，并且可用作抗孕激素。还描述了它们的制备方法和含有它们的药物组合物。

45. 发明授权

US4558049A Antipsycotic benzoxazines 失效
标题翻译：抗精神病药物
公开(公告)号：US4558049A
公开(公告)日：1985-12-10
申请号：US493618
申请日：1983-05-11
申请人： Luigi Bernardi , Ettore Lazzari , Maria L. Malnati , Giuseppe Mazzini , Lorenzo Pegrassi , Alessandro Rossi
发明人： Luigi Bernardi , Ettore Lazzari , Maria L. Malnati , Giuseppe Mazzini , Lorenzo Pegrassi , Alessandro Rossi
IPC分类号： A61K31/535 , A61P25/18 , C07D211/52 , C07D498/10
CPC分类号： C07D211/52
摘要： There are provided compounds of formula 1: ##STR1## wherein R=halogen atom or CN, NH.sub.2 and NO.sub.2 group, and pharmaceutically acceptable salts thereof.The compounds are antipsycotic agents.
摘要翻译：提供式1化合物：其中R =卤素原子或CN，NH 2和NO 2基团，及其药学上可接受的盐。这些化合物是抗精神病药。

46. 发明授权

US4500712A Ergoline derivatives 失效
标题翻译：二元醇衍生物
公开(公告)号：US4500712A
公开(公告)日：1985-02-19
申请号：US438259
申请日：1982-11-01
申请人： Luigi Bernardi , Aldemio Temperilli , Daniela Ruggieri , Giuliana Arcari , Patricia Salvati
发明人： Luigi Bernardi , Aldemio Temperilli , Daniela Ruggieri , Giuliana Arcari , Patricia Salvati
IPC分类号： A61K31/48 , A61P1/04 , A61P9/12 , C07D457/02 , C07D457/12 , C07D457/04
CPC分类号： C07D457/02 , C07D457/12
摘要： There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.
摘要翻译：提供式（Ⅰ）的麦角灵衍生物，其中R1 = H，CH3; R2 = H或卤素原子，或CH3，CN，烷基或苯基 - 硫基; R3 = H，OCH3; R4 = C1-C4烃基; X = O，S，NH; A = CO，SO2; B = C1-C4烃基，芳基，芳烷基，杂环基，烷氧基，芳氧基; n = 0,1,2; 及其药学上可接受的盐。还提供了制备所述化合物的方法。这些化合物显示出抗高血压活性，并且对胃肠系统有活性。

47. 发明授权

US4382940A Ercoline derivatives and therapeutic compositions having CNS affecting activity 失效
标题翻译：具有CNS影响活性的Ercoline衍生物和治疗组合物
公开(公告)号：US4382940A
公开(公告)日：1983-05-10
申请号：US211920
申请日：1980-12-01
申请人： Luigi Bernardi , Germano Bosisio , Sergio Mantegani , Alessandro Rossi , Aldemio Temperilli
发明人： Luigi Bernardi , Germano Bosisio , Sergio Mantegani , Alessandro Rossi , Aldemio Temperilli
IPC分类号： A61K31/48 , A61P9/12 , A61P25/20 , A61P25/24 , A61P25/26 , C07D457/02 , A61K31/55
CPC分类号： C07D457/02
摘要： Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group; R.sub.2 represents a hydrogen atom or a methoxy group;X represents an oxygen or sulphur atom or an NH or NCH.sub.3 group;R.sub.3 represents a hydrogen atom, a trifluoromethyl or phenyl group or a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.4 represents a hydrogen atom, a methyl or acetyl group or a hydrocarbon having from 1 to 4 carbon atoms, or R.sub.3 and R.sub.4 together represent a 3- or 4-membered carbon atom chain;Y represents an electron-withdrawing group such as a cyano, nitro, alkylsulphonyl or alkylsulprinyl group or a group of the formula COR.sub.5 wherein R.sub.5 represents an alkyl group having from 1 to 4 carbon atoms or a phenyl, alkoxy, amino or N-substituted amino group or R.sub.5 and R.sub.3 together represent a 2- or 3-membered carbon atom chain;R.sub.6 represents a hydrocarbon group having from 1 to 4 carbon atoms or a benzyl or phenethyl group; andR.sub.7 represents a hydrogen or halogen atom or a methyl or formyl group or a group of the formula SR.sub.8 wherein R.sub.8 represents a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group;and the pharmaceutically acceptable addition salts with organic or inorganic acids thereof. A process for producing these compounds is also disclosed.These compounds are useful antidepressant, anxiolytic and neuroleptic agents. They also display from moderate to good antiprolactinic and antihypertensive activity.
摘要翻译：公开了式（I）的化合物：其中R 1表示氢原子或甲基; R2表示氢原子或甲氧基; X表示氧或硫原子或NH或NCH 3基团; R3表示氢原子，三氟甲基或苯基或具有1至4个碳原子的烃基; R4表示氢原子，甲基或乙酰基或具有1至4个碳原子的烃，或R3和R4一起表示3-或4-元碳原子链; Y表示吸电子基团，例如氰基，硝基，烷基磺酰基或烷基磺基，或式COR5的基团，其中R5表示具有1至4个碳原子的烷基或苯基，烷氧基，氨基或N-取代的氨基基团或R 5和R 3一起表示2-或3-元碳原子链; R6表示具有1至4个碳原子的烃基或苄基或苯乙基; 并且R 7表示氢或卤素原子或甲基或甲酰基或式SR 8的基团，其中R 8表示具有1至4个碳原子的烃基或苯基; 和其药学上可接受的加成盐与其有机酸或无机酸。还公开了制备这些化合物的方法。这些化合物是有用的抗抑郁药，抗焦虑剂和抗精神病药。它们还显示从中度到良好的促乳素和抗高血压活性。

48. 发明授权

US4166911A Pyridazinyl-ergoline compounds having neuroleptic activity 失效
标题翻译：具有精神抑制活性的哒嗪基 - 麦角灵化合物
公开(公告)号：US4166911A
公开(公告)日：1979-09-04
申请号：US870095
申请日：1978-01-17
申请人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Alberto Bonsignori
发明人： Luigi Bernardi , Carlo Elli , Giovanni Falconi , Alberto Bonsignori
IPC分类号： C07D457/02 , A61K31/50
CPC分类号： C07D457/02 , Y10S514/823
摘要： Pyridazinyl-ergoline compounds having neuroleptic activity are obtained by reacting an 8.beta.-tosylmethyl ergoline with the sodium derivative of an amino-pyridazine or a mercaptopyridazine in a dipolar aprotic solvent.
摘要翻译：通过使8β-甲苯基甲基麦角灵与氨基哒嗪或巯基哒嗪的钠衍生物在偶极非质子溶剂中反应，得到具有精神抑制活性的哒嗪基 - 麦角灵化合物。

49. 发明授权

US3996228A Pyrimidinoaminoethyl ergoline derivatives 失效
标题翻译：嘧啶氨基乙基麦角灵衍生物
公开(公告)号：US3996228A
公开(公告)日：1976-12-07
申请号：US530617
申请日：1974-12-09
申请人： Giuliana Arcari , Luigi Bernardi , Germano Bosisio , Alfredo Glasser , Aldemio Temperilli
发明人： Giuliana Arcari , Luigi Bernardi , Germano Bosisio , Alfredo Glasser , Aldemio Temperilli
IPC分类号： C07D457/02
CPC分类号： C07D457/02
摘要： Pyrimidinoaminoethyl ergoline derivatives of the formula: ##STR1## wherein R is hydrogen or methyl; R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl having 1 to 3 carbon atoms, methoxy and phenyl;R.sub.3 is hydrogen, halogen, alkyl and alkoxy each having 1 to 3 carbon atoms, phenyl, nitro, amino, cyano, acylamino, carboxamido and carbalkoxy each having 1 to 3 carbon atoms, trifluoromethyl or --SO.sub.2 --Y wherein Y is hydroxyl, amino or methyl and R.sub.4 is hydrogen or methoxy are prepared by reacting an ergoline derivative of formula III and a 2-aminopyrimidine anion of formula II ##STR2##
摘要翻译：具有下式的嘧啶基氨基乙基麦角灵衍生物：其中R是氢或甲基; R 1和R 2独立地选自氢，具有1至3个碳原子的烷基，甲氧基和苯基; R3是氢，卤素，烷基和烷氧基，各自具有1至3个碳原子，苯基，硝基，氨基，氰基，酰氨基，甲酰胺基和碳烷氧基，各自具有1至3个碳原子，三氟甲基或-SO2-Y，其中Y是羟基，或甲基和R 4是氢或甲氧基通过使式III的麦角灵衍生物与式II的2-氨基嘧啶阴离子反应来制备。

50. 发明授权

US5591734A 17-(3-furyl)-5.beta., 14.beta.-androstane derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing same 失效
标题翻译：对心血管系统有活性的17-（3-呋喃基）-5β，14β-雄甾烷衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5591734A
公开(公告)日：1997-01-07
申请号：US106893
申请日：1993-08-16
申请人： Luisa Quadri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Piero Melloni , Loredana Valentino
发明人： Luisa Quadri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Piero Melloni , Loredana Valentino
IPC分类号： A61K31/565 , A61K31/56 , A61K31/58 , A61K31/585 , A61P9/00 , A61P9/10 , A61P9/12 , C07J1/00 , C07J17/00 , C07J41/00 , C07J43/00 , C07J71/00
CPC分类号： C07J41/0005 , C07J17/00 , C07J41/0088 , C07J43/003 , C07J71/0021
摘要： The present invention relates to a group of 17-(3-furyl)- and (4-pyridazinyl) 5.beta.,14.beta.-androstane derivatives, active on the cardiovascular system, to processes for their preparation and to pharmaceutical compositions containing same for the treatment of cardiovascular disorders such as heart failure and hypertension.
摘要翻译：本发明涉及对心血管系统有活性的一组17-（3-呋喃基） - 和（4-哒嗪基）5β，14β-雄甾烷衍生物，其制备方法和含有其的药物组合物治疗心血管疾病如心力衰竭和高血压。

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