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21. 发明授权

US5567697A 17-(4-pyridazinyl) -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-（4-哒嗪基）-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：US5567697A
公开(公告)日：1996-10-22
申请号：US458822
申请日：1995-06-02
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： Present invention relates to a group of 17-(4-pyridazinyl)-5.beta.,14.beta.-androstane derivates active on the cardiovascular system and to pharmaceutical compositions containing same.
摘要翻译：本发明涉及对心血管系统有活性的一组17-（4-哒嗪基）-5β，14β-雄甾烷衍生物以及含有它们的药物组合物。

22. 发明授权

US4675404A 8-pyridazinylcarbamoyl ergolines 失效
标题翻译： 8-哒嗪基氨基甲酰基麦角碱
公开(公告)号：US4675404A
公开(公告)日：1987-06-23
申请号：US885315
申请日：1986-07-14
申请人： Luigi Bernardi , Aldemio Temperilli , Germano Bosisio , Gabriella Traquandi , Rosanna Eccel , Alessandro Rossi , Patricia Salvati
发明人： Luigi Bernardi , Aldemio Temperilli , Germano Bosisio , Gabriella Traquandi , Rosanna Eccel , Alessandro Rossi , Patricia Salvati
IPC分类号： C07D457/02 , C07D457/06 , A61K31/48
CPC分类号： C07D457/06 , C07D457/02
摘要： Ergoline derivatives of formula: ##STR1## wherein n=0,1,2; R.sub.1 =H, CH.sub.3 ; R.sub.2 =H, CH.sub.3, halogen; R.sub.3 =H, OCH.sub.3 ; R.sub.4 =hydrocarbon group and R.sub.5 is a residue of general formula II, III, IV, V, VI, VII: ##STR2## wherein R.sub.6 =H, Cl, OCH.sub.3, NR.sub.11 R.sub.12, wherein R.sub.11 and R.sub.12 =H, lower alkyl; phenyl or are bonded together to form a heterocyclic ring, R.sub.7, R.sub.8 and R.sub.9 and R.sub.10 =H or C.sub.1 -C.sub.3 alkyl, with the proviso that if R.sub.5 is of formula II and R.sub.2 =R.sub.7 =R.sub.8 =H, then R.sub.4 is not methyl or n is not 0.Pharmaceutically acceptable acid addition salts are also provided. A method for their preparation is also provided.The compounds have anti-depressive, anti-hypertensive and antiprolactin activity.
摘要翻译：式：其中n = 0,1,2; R1 = H，CH3; R2 = H，CH3，卤素; R3 = H，OCH3; R4 =烃基，R5是通式Ⅱ，Ⅲ，Ⅳ，Ⅴ，Ⅵ，Ⅶ的残基：其中R6 = H，Cl，OCH3，NR11R12，其中R11和R12 = H，低级烷基; 苯基或键合在一起形成杂环，R 7，R 8和R 9和R 10 = H或C 1 -C 3烷基，条件是如果R 5为式II且R 2 = R 7 = R 8 = H，则R 4不是甲基或n不为0.还提供药学上可接受的酸加成盐。还提供了它们的制备方法。该化合物具有抗抑郁，抗高血压和抗催乳素活性。

23. 发明授权

US4632990A Ergoline carboxamides 失效
标题翻译：二氢吡啶甲酰胺
公开(公告)号：US4632990A
公开(公告)日：1986-12-30
申请号：US484477
申请日：1983-04-13
申请人： Luigi Bernardi , Enzo Brambilla , Laura Chiodini , Enrico di Salle , Daniela Ruggieri , Osvaldo Sapini , Aldemio Temperilli
发明人： Luigi Bernardi , Enzo Brambilla , Laura Chiodini , Enrico di Salle , Daniela Ruggieri , Osvaldo Sapini , Aldemio Temperilli
IPC分类号： A61K31/435 , A61P13/02 , A61P15/00 , A61P25/00 , A61P43/00 , C07D457/02 , C07D457/06 , A61K31/48 , C07D239/42
CPC分类号： C07D457/06 , C07D457/02
摘要： There are provided ergoline derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group, R.sub.2 represents a hydrogen or halogen atom or a methyl group, R.sub.3 represents a hydrogen atom or a methoxy group, R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; each of X and W independently represents a hydrogen atom, a methyl group, a chlorine atom or a methoxy group, and n is 0, 1 or 2. A method for their preparation is also provided. The compounds have strong antiprolactin activity.
摘要翻译：提供下式的麦角灵衍生物：其中R 1表示氢原子或甲基，R 2表示氢或卤原子或甲基，R 3表示氢原子或甲氧基，R 4表示烃具有1至4个碳原子的基团; X和W各自独立地表示氢原子，甲基，氯原子或甲氧基，n为0,1或2.也可以提供其制备方法。该化合物具有较强的抗孕激素活性。

24. 发明授权

US4223146A 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[4,5-c] - 吡啶衍生物
公开(公告)号：US4223146A
公开(公告)日：1980-09-16
申请号：US959506
申请日：1978-11-13
申请人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Ugo Scarponi
发明人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Ugo Scarponi
IPC分类号： A61K31/4188 , A61K31/435 , A61K31/437 , A61P1/04 , A61P25/02 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/925
摘要： Compounds are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms; and R.sub.3 is a saturated or unsaturated straight or branched alkyl having from 1 to 4 carbon atoms. A process for making such compounds is also disclosed. These compounds are useful as antiulcer agents and as inhibitors of gastric secretion.
摘要翻译：公开了通式（I）的化合物：其中R 1是具有1至4个碳原子的低级烷基; R2是氢或具有1至4个碳原子的低级烷基; 并且R 3是具有1至4个碳原子的饱和或不饱和的直链或支链烷基。还公开了制备这些化合物的方法。这些化合物可用作抗溃疡剂和胃分泌抑制剂。

25. 发明授权

US4155911A Process for the production of substituted 4-thia-2,6-diaza[3.2.0]-2-heptene-7-one 失效
标题翻译：制备取代的4-硫杂-2,6-二氮杂{8 3.2.0 {9,2-庚烯-7-酮
公开(公告)号：US4155911A
公开(公告)日：1979-05-22
申请号：US820895
申请日：1977-08-01
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
CPC分类号： C07D513/04 , C07D205/08
摘要： A new process is disclosed for the preparation of compounds of structure: ##STR1## and are as defined herein characterized in that a compound of structure ##STR2## where R and R.sup.1 have the meanings given herein, 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 structure: ##STR3## where R and R.sup.1 have the meanings given herein, Hal is a halogen atom; THE INTERMEDIATE COMPOUND (III) in a suitable solvent is then reacted with an appropriate nucleophilic reagent to obtain the compound IV where Z replaces Hal, where Z is defined herein;The compound (IV) is then subjected to an allylic halogenation in a suitable solvent by reacting it with a haloamide either under the influence of light alone or by heating it in the presence of a free radical initiator, to give a compound of structure: ##STR4## where R, R.sup.1 and Hal and Z have the above meanings; THE INTERMEDIATE COMPOUND (V) is then reacted with a reducing agent to give finally the desired compound (I).
摘要翻译：公开了用于制备结构式（I）的化合物的新方法，其定义如下，其特征在于其中R和R 1具有本文给出的含义的结构式（II）的化合物在在金属氧化物或卤代酰胺的存在下，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，在金属氧化物的存在下，与卤代酰胺合适的溶剂，得到结构化合物（III）其中R和R1具有本文给出的含义，Hal是卤素原子; 然后将合适的溶剂中的中间体化合物（III）与合适的亲核试剂反应，得到Z代替Hal的化合物IV，其中Z在本文中定义; 然后使化合物（IV）在合适的溶剂中通过与单独的光的影响下的卤代酰胺反应或通过在自由基引发剂的存在下加热使其与卤代酰胺反应，得到结构式（V）其中R，R1，Hal和Z具有上述含义; 然后将中间体化合物（V）与还原剂反应，最终得到所需化合物（I）。

26. 发明授权

US4077969A Process for preparing azetidinone thiazolidine derivatives 失效
标题翻译：制备氮杂环丁酮噻唑烷衍生物的方法
公开(公告)号：US4077969A
公开(公告)日：1978-03-07
申请号：US587090
申请日：1975-06-16
申请人： Luigi Bernardi , Maurizio Foglio , Giovanni Francheschi
发明人： Luigi Bernardi , Maurizio Foglio , Giovanni Francheschi
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： A process is disclosed for preparing azetidonethiazolidines of the formula ##STR1## where R and V are defined herein below, wherein a compound of the structure ##STR2## dissolved in a suitable solvent, is treated at about 0.degree. C with a solution of preferably anhydrous hydrochloric acid in a lower aliphatic alcohol with a slight excess of sodium cyanoborohydride.
摘要翻译：公开了一种制备下式定义的式“IMAGE”的氮杂环丁烷的方法，其中R和V如下文定义，其中溶解在合适溶剂中的结构式“IMAGE”的化合物在约0℃下用优选无水溶液在低级脂族醇中加入盐酸，稍加过量氰基硼氢化钠。

27. 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。

28. 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。

29. 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。

30. 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。

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