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1. 发明授权

US5538960A Hydrazono-5.beta., 14.beta.-androstane derivatives active on the cardiovascular system, and pharmaceutical compositions containing same 失效
标题翻译：对心血管系统有活性的肼基-5β，14β-雄甾烷衍生物和含有它们的药物组合物
公开(公告)号：US5538960A
公开(公告)日：1996-07-23
申请号：US106638
申请日：1993-08-16
申请人： Alberto Cerri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Elena Folpini , Piero Melloni
发明人： Alberto Cerri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Elena Folpini , Piero Melloni
IPC分类号： A61K31/565 , A61K31/58 , A61P9/00 , A61P9/12 , C07J31/00 , C07J41/00 , C07J43/00 , C07J75/00 , C07D43/00 , A61K31/57
CPC分类号： C07J41/0088 , C07J41/0005 , C07J41/0038 , C07J43/003
摘要： The present invention relates to new 17-hydrazonomethyl- and 17-hydrazono-14.beta.-hydroxy-5.beta.-androstane derivatives active on the cardiovascular system, to a process 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：本发明涉及在心血管系统上活性的新的17-亚肼基甲基和17-亚肼基-14β-羟基-5β-雄甾烷衍生物，其制备方法以及含有其用于治疗心血管疾病的药物组合物，如心力衰竭和高血压。

2. 发明授权

US4657914A Ergoline derivatives 失效
标题翻译：二元醇衍生物
公开(公告)号：US4657914A
公开(公告)日：1987-04-14
申请号：US488168
申请日：1983-04-25
申请人： Luigi Bernardi , Aldemio Temperilli , Sergio Mantegani , Gabriella Traquandi , Patricia Salvati
发明人： Luigi Bernardi , Aldemio Temperilli , Sergio Mantegani , Gabriella Traquandi , Patricia Salvati
IPC分类号： A61K31/48 , A61P9/12 , C07D457/02
CPC分类号： C07D457/02
摘要： There are provided ergoline compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a methyl group; R.sub.2 is a hydrogen or halogen atom, a methyl or thiomethyl group; R.sub.3 is a hydrogen atom or a methoxy group; R.sub.4 is a hydrocarbon group having from 1 to 4 carbon atoms; n is 1 or 2; each of R.sub.5 and R.sub.6 independently is a hydrogen atom, an alkyl group having from 1 to 3 carbon atoms, or a phenyl or hydroxy or alkoxy group having from 1 to 4 carbon atoms, and X is an oxygen atom or a group of the formula NR.sub.7 wherein R.sub.7 is selected from the group consisting of a hydrogen atom, an alkyl having from 1 to 4 carbon atoms and a phenyl group, or a group of the formula N.dbd.C--R.sub.8 wherein the carbon atom is positioned between the nitrogen atoms in the ring and R.sub.8 is an amino, substituted amino, methyl, phenyl, thiomethyl or mercapto group. The compounds have antihypertensive and antiprolactin activity.
摘要翻译：提供下式的麦角灵化合物：其中R 1是氢原子或甲基; R2是氢或卤素原子，甲基或硫代甲基; R3是氢原子或甲氧基; R4是具有1至4个碳原子的烃基; n为1或2; R 5和R 6各自独立地为氢原子，具有1至3个碳原子的烷基或具有1至4个碳原子的苯基或羟基或烷氧基，X为氧原子或式 NR7，其中R7选自氢原子，具有1至4个碳原子的烷基和苯基，或式N = C-R8的基团，其中碳原子位于氮原子之间环和R8是氨基，取代的氨基，甲基，苯基，硫代甲基或巯基。该化合物具有抗高血压和抗催乳素活性。

3. 发明授权

US4526569A Portable device for infusing insulin on the basis of glycemic measurements 失效
标题翻译：基于血糖测量法输入胰岛素的便携式装置
公开(公告)号：US4526569A
公开(公告)日：1985-07-02
申请号：US438785
申请日：1982-11-03
申请人： Luigi Bernardi
发明人： Luigi Bernardi
IPC分类号： A61M5/172 , A61M5/00
CPC分类号： A61M5/1723
摘要： The invention relates to a device made by a concentric dual lumen catheter, a pump, a small hemofilter, a glucose sensor which, by means of a microinfusion pump with a stepping motor controlled by a microprocessor can, through another concentric dual lumen catheter, inject insulin or glucose into the blood stream depending on glycemic levels.
摘要翻译：本发明涉及由同心双腔导管，泵，小型血液滤清器，葡萄糖传感器制成的装置，其通过具有由微处理器罐控制的步进电机的微注射泵通过另一同心双腔导管注射胰岛素或葡萄糖根据血糖水平进入血液。

4. 发明授权

US4267116A Novel daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：新型道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4267116A
公开(公告)日：1981-05-12
申请号：US38689
申请日：1979-05-14
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , C07C50/16
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is hydrogen or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

5. 发明授权

US4252948A Ergoline derivatives 失效
标题翻译：二元醇衍生物
公开(公告)号：US4252948A
公开(公告)日：1981-02-24
申请号：US21671
申请日：1979-03-19
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
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 aminopyridazine 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。

6. 发明授权

US4191756A Daunomycin derivatives, their aglycones and the use thereof 失效
标题翻译：道诺霉素衍生物，其糖苷配基及其用途
公开(公告)号：US4191756A
公开(公告)日：1980-03-04
申请号：US901359
申请日：1978-05-01
申请人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
发明人： Paolo Masi , Antonino Suarato , Luigi Bernardi , Federico Arcamone
IPC分类号： C07C50/38 , A61K31/65 , A61P31/04 , A61P35/00 , C07C45/00 , C07C67/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , Y10S514/908
摘要： Daunomycin derivatives of the formula: ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms and R is a hydrogen atom or a trifluoroacetyl group are useful in treating certain mammalian tumors.
摘要翻译：下式的道诺霉素衍生物：其中R1是具有1至4个碳原子的低级烷基，R是氢原子或三氟乙酰基可用于治疗某些哺乳动物肿瘤。

7. 发明授权

US4141899A 4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives 失效
标题翻译： 4,5,6,7-四氢咪唑并 - {8 4,5-c {9-吡啶衍生物
公开(公告)号：US4141899A
公开(公告)日：1979-02-27
申请号：US838844
申请日：1977-10-03
申请人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Fulvio Luini , Giorgio Palamidessi , Ugo Scarponi
发明人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Fulvio Luini , Giorgio Palamidessi , Ugo Scarponi
IPC分类号： C07D471/04
CPC分类号： Y10S514/926 , Y10S514/927
摘要： New 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine derivatives are disclosed, and more particularly derivatives of Formula I ##STR1## where R.sub.1 is hydrogen or an alkyl having from 1 to 4 carbon atoms;R.sub.2 is hydrogen, an alkyl having from 1 to 4 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, phenyl or a heterocycle;R.sub.3 is hydrogen, a saturated or unsaturated straight or branched alkyl having from 1 to 6 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, benzoyl or phenyl; andX is O, S or NR.sub.4 where R.sub.4 is hydrogen, an alkyl having from 1 to 4 carbon atoms, cyano, amino, nitro or acylamino;Or pharmaceutically acceptable acid addition salts thereof. Also disclosed is a process of preparing these compounds which comprises condensing an appropriate 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine with an appropriate alkyl isocyanate, alkyl isothiocyanate or substituted S-methyl thiourea, preferably in a solvent such as ethanol, acetonitrile or dioxane, usually under reflux for from 4 to 12 hours. The products can be isolated by crystallization as free bases or as salts of pharmaceutically acceptable acids. The new compounds have proved to be well tolerated and to inhibit both the number of experimental ulcers and the gastric secretion in experimental animals. Thus, they should prove useful in the therapy of gastric and duodenal ulcers in man.
摘要翻译：公开了新的4,5,6,7-四氢咪唑并[4,5-c] - 吡啶衍生物，更具体地，其中R 1是氢或具有1至4个碳原子的烷基的式I的衍生物; R 2是氢，具有1至4个碳原子的烷基，具有3至6个碳原子的环烷基，苯基或杂环; R3是氢，具有1至6个碳原子的饱和或不饱和直链或支链烷基，具有3至6个碳原子的环烷基，苯甲酰基或苯基; 且X为O，S或NR 4，其中R 4为氢，具有1至4个碳原子的烷基，氰基，氨基，硝基或酰氨基; 或其药学上可接受的酸添加剂。还公开了制备这些化合物的方法，其包括将合适的4,5,6,7-四氢咪唑并[4,5-c] - 吡啶与适当的烷基异氰酸酯，异硫氰酸烷基酯或取代的S-甲基硫脲缩合，优选在溶剂如乙醇，乙腈或二恶烷，通常在回流下4至12小时。可以通过结晶作为游离碱或药学上可接受的酸的盐分离产物。这些新化合物已被证明是良好的耐受性，并且在实验动物中抑制实验性溃疡的数量和胃分泌。因此，它们应该证明在治疗人和十二指肠溃疡方面是有用的。

8. 发明授权

US4077970A Methyl-.alpha.[3'acetoxy-1'isopropenyl]-3 substituted 1.alpha.,5x-4-thia 2,6 diaza[3,2,0]2-heptene-6 acetate 7-one 失效
标题翻译：甲基 - {60 {8 3 {40乙酰氧基-1 {40异丙烯基{9,3取代的1 {60,5x-4-硫杂-2,6-二氮杂{8 3,2,0 {9 2-庚烯-6-乙酸酯7- 一
公开(公告)号：US4077970A
公开(公告)日：1978-03-07
申请号：US603605
申请日：1975-08-11
申请人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
发明人： Maurizio Foglio , Antonino Suarato , Paolo Masi , Giovanni Franceschi , Giorgio Palamidessi , Luigi Bernardi
IPC分类号： C07D205/08 , C07D513/04 , C07D513/08
CPC分类号： C07D513/04 , C07D205/08
摘要： A process is disclosed for the preparation of a compound of the formula ##STR1## where R and R.sup.1 are defined herein below, wherein a compound of the structure; ##STR2## is reacted in a suitable solvent with a haloamide in the presence of a metal oxide or a haloamide in the presence of a free radical initiator under the influence of light or heat or alternatively with a halogen in the presence of a metal oxide, to give a compound of the structure; ##STR3## which compound, in a suitable solvent is reacted with a suitable nucleophilic reagent to obtain the compound; ##STR4## which compound is then subjected to allylic halogenation to give a compound of the structure; ##STR5## which is then reacted with a reducing agent to yield I.
摘要翻译：公开了用于制备下式化合物的方法，其中R和R 1如下文所定义，其中该结构的化合物; 在自由基引发剂的存在下，在光或热的作用下，或者在卤素存在下，在金属氧化物或卤代酰胺的存在下，在合适的溶剂中与卤代酰胺反应。，得到结构的化合物; 该化合物在合适的溶剂中与合适的亲核试剂反应得到化合物; 然后将该化合物进行烯丙基卤化，得到结构的化合物; 然后将其与还原剂反应以产生I.

9. 发明授权

US4024224A 14-Aminodaunomycins, their preparation and use 失效
标题翻译： 14-氨基诺乃霉素，其制备和用途
公开(公告)号：US4024224A
公开(公告)日：1977-05-17
申请号：US637170
申请日：1975-12-03
申请人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
发明人： Federico Arcamone , Luigi Bernardi , Bianca Patelli , Aurelio DI Marco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/22 , A61K31/71
CPC分类号： C07H15/252
摘要： 14-Aminodaunomycins, which are prepared by reacting 14-bromodaunomycin with an amine in a solvent at about 20.degree.-60.degree. C. are useful in treating certain tumors such as ascites Sarcoma 180 and solid Sarcoma 180.
摘要翻译：通过使14-溴原子素霉素与胺在溶剂中在约20-60℃下反应制备的14-氨基诺乃霉素可用于治疗某些肿瘤如腹水肉瘤180和固体肉瘤180。

10. 发明授权

US3966739A Pyrrole-carboxylic acids lumilysergol esters 失效
标题翻译：吡咯羧酸lumilysergol酯
公开(公告)号：US3966739A
公开(公告)日：1976-06-29
申请号：US232605
申请日：1972-03-07
申请人： Luigi Bernardi , Germano Bosisio , Gian Carlo Fregnan
发明人： Luigi Bernardi , Germano Bosisio , Gian Carlo Fregnan
IPC分类号： C07D457/02
CPC分类号： C07D457/02
摘要： Esters of 1-methyl-lumilysergol-10-methylether having the formula: ##SPC1##Wherein R is selected from the group consisting of 2-furanoyl and the pyrrole group of the formula: ##SPC2##Wherein Y is selected from the group consisting of hydrogen, lower alkyl having from 1 to 6 carbon atoms and phenyl; R.sub.1 is selected from the group consisting of hydrogen, methyl and carbonyl; R.sub.2 is selected from the group consisting of hydrogen, methyl, halogen and carbonyl, provided that only one of R.sub.1 and R.sub.2 can be carbonyl; R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen, halogen, alkyl, alkoxy having from 1 to 6 carbon atoms and carboethoxy; the pharmaceutically acceptable addition salts thereof with an organic acid and a process for the preparation thereof. The compounds possess adrenolytic, hypotensive, sedative and antiserotoninic activities.
摘要翻译：具有下式的1-甲基 - 亮片葡聚糖-10-甲醚的酯：

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