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：

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。

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。

公开(公告)号：US3957785A

公开(公告)日：1976-05-18

申请号：US493335

申请日：1974-07-31

申请人： Giuliana Arcari ,  Luigi Bernardi ,  Germano Bosisio ,  Maurizio Foglio ,  Alfredo Glasser ,  Aldemio Temperilli

发明人： Giuliana Arcari ,  Luigi Bernardi ,  Germano Bosisio ,  Maurizio Foglio ,  Alfredo Glasser ,  Aldemio Temperilli

IPC分类号： C07D457/02

CPC分类号： C07D457/02

摘要： Novel 8.beta.-pyrimidino-aminomethyl-10.alpha.-ergoline and 10.alpha.-methoxyergoline derivatives which possess a high and prolonged adrenolytic activity and a low toxicity, and some of which also possess hypotensive and analgesic activity are prepared by reacting a pyrimidine anion with an ergoline derivative in an aprotic solvent.

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。

公开(公告)号：US3972883A

公开(公告)日：1976-08-03

申请号：US436927

申请日：1974-01-28

申请人： Giuliana Arcari ,  Luigi Bernardi ,  Germano Bosisio ,  Alfredo Glasser ,  Innocenzio Sinatra

发明人： Giuliana Arcari ,  Luigi Bernardi ,  Germano Bosisio ,  Alfredo Glasser ,  Innocenzio Sinatra

IPC分类号： A61K31/48 ,  C07D457/02

CPC分类号： C07D457/02

摘要： Ergoline derivatives are disclosed having the general formula ##SPC1##Wherein R is selected from the group consisting of a lower alkyl radical having from 1 to 4 carbon atoms; an --NH-lower alkyl radical having from 1 to 4 carbon atoms; a free or substituted phenyl- or 2-furanoyl radical; the --O--CH.sub.2 --C.sub.6 H.sub.5 radical; a (3)- or (4)-pyridine radical free or substituted by a methyl radical or a chlorine or bromine atom; a pyrrole radical of formula ##SPC2##WhereinY is hydrogen, a lower alkyl radical having from 1 to 4 carbon atoms or phenyl;R.sub.1 is hydrogen or methyl;R.sub.2 is hydrogen, methyl or halogen; andR.sub.3 and R.sub.4 are the same or different and are hydrogen, halogen, a lower alkyl radical having from 1 to 4 carbon atoms, carbethoxy, or a lower alkyloxy radical having from 1 to 4 carbon atoms.Novel processes for the preparation of these compounds are also disclosed.

摘要翻译： 公开了具有通式为WHEREIN R选自具有1至4个碳原子的低级烷基的衍生物， 具有1至4个碳原子的-NH-低级烷基; 游离或取代的苯基或2-呋喃酰基; -O-CH 2 -C 6 H 5基团; （3） - 或（4） - 吡啶基自由或被甲基或氯或溴原子取代; 式WHEREIN Y的吡咯基是氢，具有1至4个碳原子的低级烷基或苯基; R1是氢或甲基; R2是氢，甲基或卤素; 并且R 3和R 4相同或不同，为氢，卤素，具有1至4个碳原子的低级烷基，乙氧羰基或具有1至4个碳原子的低级烷氧基。

公开(公告)号：US4252941A

公开(公告)日：1981-02-24

申请号：US72289

申请日：1979-09-04

申请人： Sergio Mantegani ,  Giuliana Arcari ,  Anna M. Caravaggi ,  Germano Bosisio

发明人： Sergio Mantegani ,  Giuliana Arcari ,  Anna M. Caravaggi ,  Germano Bosisio

IPC分类号： C07D457/04 ,  A61K31/48 ,  A61P9/12 ,  C07D457/02

CPC分类号： C07D457/02

摘要： Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents a methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl group, an alkyl or alkoxy group having from 1 to 4 carbon atoms, an amino group, a substituted amino group of the formula NHR' (wherein R' represents an alkyl group having from 1 to 4 carbon atoms, a cycloalkyl group, a benzyl group, or a phenyl group) or a substituted amino group of the formula NR" R"' (wherein R" and R"' both represent alkyl groups having from 1 to 4 carbon atoms);R.sub.2 represents a hydrogen atom, an alkyl group having from 1 to 4 carbon atoms, or a phenyl group;R.sub.3 represents a fluorine atom, a cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl, or sulphonamido group, an alkoxy group having from 1 to 4 carbon atoms, an acyl group having from 2 to 4 carbon atoms, or a benzoyl group;R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms;R.sub.5 represents a hydrogen atom or a methoxy group;R.sub.6 represents a hydrogen or halogen atom or a methyl group; andR.sub.7 represents a hydrogen atom or a methyl group.The 2-cyano derivatives are especially preferred.

摘要翻译： 公开了化合物及其制备方法，具有式（I）的化合物：其中R 1表示甲基，苯基，哌啶子基，1-吡咯烷基，吗啉代或4-甲基-1-哌嗪基， 具有1至4个碳原子的烷基或烷氧基，氨基，式NHR'的取代氨基（其中R'表示具有1至4个碳原子的烷基，环烷基，苄基或 苯基）或式NR“R”'的取代氨基（其中R“和R”“均表示具有1至4个碳原子的烷基）; R2表示氢原子，具有1至4个碳原子的烷基或苯基; R 3表示氟原子，氰基，二氟甲基，二氟溴甲基，三氟甲基，甲硫基，甲磺酰基或磺酰胺基，具有1至4个碳原子的烷氧基，具有2至4个碳原子的酰基或苯甲酰基; R4表示具有1至4个碳原子的烃基; R5表示氢原子或甲氧基; R6表示氢或卤素原子或甲基; 并且R 7表示氢原子或甲基。 2-氰基衍生物是特别优选的。

公开(公告)号：US4321381A

公开(公告)日：1982-03-23

申请号：US188620

申请日：1980-09-19

申请人： Sergio Mantegani ,  Guiliana Arcari ,  Anna M. Caravaggi ,  Germano Bosisio

发明人： Sergio Mantegani ,  Guiliana Arcari ,  Anna M. Caravaggi ,  Germano Bosisio

IPC分类号： C07D457/04 ,  A61K31/48 ,  A61P9/12 ,  C07D457/02 ,  A61K31/495

CPC分类号： C07D457/02

摘要： Compounds and process for making same are disclosed, the compounds having the formula (I): ##STR1## wherein R.sub.1 represents methyl, phenyl, piperidino, 1-pyrrolidinyl, morpholino or 4-methyl-1-piperazinyl, alkyl or alkoxy having from 1 to 4 carbon atoms, amino, substituted amino of the formula NHR' (wherein R' is alkyl having from 1 to 4 carbon atoms, cycloalkyl, a benzyl, or phenyl) or substituted amino of the formula NR" R"' (wherein R" and R"' both represent alkyl having from 1 to 4 carbon atoms);R.sub.2 represents a hydrogen atom, alkyl having from 1 to 4 carbon atoms, or phenyl;R.sub.3 represents a fluorine atom, cyano, difluoromethyl, difluorobromomethyl, trifluoromethyl, methylthio, methylsulphonyl, sulphonamido, an alkoxy having from 1 to 4 carbon atoms, an alkanoyl having from 2 to 5 carbon atoms, or benzoyl;R.sub.4 represents a hydrocarbon having from 1 to 4 carbon atoms;R.sub.5 represents a hydrogen atom or methoxy;R.sub.6 represents a hydrogen or halogen atom or methyl; andR.sub.7 represents a hydrogen atom or methyl. The 2-cyano derivatives are especially preferred.The compounds are useful as antihypertensive agents.

公开(公告)号：US4526892A

公开(公告)日：1985-07-02

申请号：US448364

申请日：1982-12-09

申请人： Patricia Salvati ,  Anna M. Caravaggi ,  Aldemio Temperilli ,  Germano Bosisio ,  Osvaldo Sapini ,  Enrico di Salle

发明人： Patricia Salvati ,  Anna M. Caravaggi ,  Aldemio Temperilli ,  Germano Bosisio ,  Osvaldo Sapini ,  Enrico di Salle

IPC分类号： C07D457/06 ,  A61K31/48

CPC分类号： C07D457/06

摘要： Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.

摘要翻译： 通过8-羧基麦角灵与碳二亚胺的反应形成的具有降血压和抗抑素活性的新型麦角灵衍生物。