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1. 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。

2. 发明授权

US3957785A B.beta.-Pyrimidino-aminomethyl-10.alpha.-ergoline and 10.alpha.-methoxyergoline derivatives 失效
标题翻译： B'-吡啶基 - 氨基甲酰基-10' - 麦芽糖和10'-麦芽糖衍生物
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.

3. 发明授权

US3972883A 1,6-Dimethyl-8.beta.-[2' or 3'-pyrroyloxyethyl or substituted pyrroyloxyethyl]-10.alpha.-methoxyergolene compounds 失效
标题翻译： 1,6-二甲基-8- {62 - {8 2 {40 {0或3 {40-吡咯氧基乙基或取代的吡咯氧基乙基{9-10 {60-甲氧基己烯基化合物
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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 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。

9. 发明授权

US4861793A D-nor-7-ergoline derivatives having anti-Parkinson and antipsychosis activity and pharmaceutical compositions containing them 失效
标题翻译：具有抗帕金森综合征和抗精神病药物的D-去甲-7麦角灵衍生物和含有它们的药物组合物
公开(公告)号：US4861793A
公开(公告)日：1989-08-29
申请号：US32447
申请日：1987-03-31
申请人： Luigi Bernardi , Laura Chiodini , Aldemio Temperilli
发明人： Luigi Bernardi , Laura Chiodini , Aldemio Temperilli
IPC分类号： C07D487/04 , A61K31/40 , A61K31/415 , A61K31/505 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/26 , C07D487/06
CPC分类号： C07D487/06
摘要： Pharmaceutical compounds of the formula ##STR1## wherein R is H or CH.sub.3, R.sub.1 is H or OCH.sub.3, R.sub.2 is a C.sub.1 -C.sub.4 hydrocarbon group and X is an organic group. Also disclosed is a process for the preparation of these compounds. The compounds have dopamine agonist or antagonist activity.
摘要翻译：其中R为H或CH 3，R 1为H或OCH 3，R 2为C 1 -C 4烃基，X为有机基团。还公开了制备这些化合物的方法。该化合物具有多巴胺激动剂或拮抗剂活性。

10. 发明授权

US4690929A Ergolines exhibiting protactin secretion inhibition activity 失效
标题翻译： Ergolines表现出protactin分泌抑制活性
公开(公告)号：US4690929A
公开(公告)日：1987-09-01
申请号：US604041
申请日：1984-04-26
申请人： Luigi Bernardi , Laura Chiodini , Sergio Mantegani , Daniela Ruggieri , Aldemio Temperilli , Patricia Salvati
发明人： Luigi Bernardi , Laura Chiodini , Sergio Mantegani , Daniela Ruggieri , Aldemio Temperilli , Patricia Salvati
IPC分类号： C07D457/02 , C07D457/12 , A61K31/48 , C07D457/04
CPC分类号： C07D457/02 , C07D457/12
摘要： Compounds of formula I: ##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, cyano, C.sub.1 -C.sub.4 alkylthio or phenylthio group; R.sub.7 and R.sub.8 represent hydrogen atoms and R.sub.3 represents a hydrogen atom or a methoxy group, or R.sub.7 represents a hydrogen atom and R.sub.3 and R.sub.8 taken together represent a bond, or R.sub.3 represents a hydrogen atom or a methoxy group and R.sub.7 and R.sub.8 taken together represent a bond; R.sub.4 represents a hydrocarbon group having from 1 to 4 carbon atoms; R.sub.5 represents a hydrogen atom or a hydrocarbon group having from 1 to 4 carbon atoms or a phenyl group; X represents an oxygen or sulphur atom or an imino group, R.sub.9 represents a hydrogen atom and B represents a cyano, a C.sub.2 -C.sub.5 alkoxycarbonyl or carbamoyl group, or R.sub.9 and B taken together represent a ##STR2## group wherein W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.6, CH.sub.2 --CHR.sub.6 or CH.dbd.CR.sub.6 group wherein R.sub.6 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group; and n is 0, 1 or 2; and their pharmaceutically acceptable salts are disclosed, along with the use of these compounds as antiprolactinic and antihypertensive agents. The preparation of these compounds and pharmaceutical compositions containing them are also described.
摘要翻译：式I的化合物：其中R 1表示氢原子或甲基; R 2表示氢或卤素原子或甲基，氰基，C 1 -C 4烷硫基或苯硫基; R7和R8表示氢原子，R3表示氢原子或甲氧基，或R7表示氢原子，R3和R8表示一个键，或R3表示氢原子或甲氧基，R7和R8表示一个债券 R4表示具有1至4个碳原子的烃基; R5表示氢原子或碳原子数1〜4的烃基或苯基; X表示氧或硫原子或亚氨基，R9表示氢原子，B表示氰基，C2-C5烷氧基羰基或氨基甲酰基，或R9和B表示“IMA”基团，其中W表示氧原子或亚氨基; A表示式CHR 6，CH 2 -CHR 6或CH = CR 6基团的基团，其中R 6表示氢原子或C 1 -C 4烷基; 且n为0,1或2; 以及它们的药学上可接受的盐以及这些化合物作为抗孕激素和抗高血压药的用途。还描述了这些化合物的制备和含有它们的药物组合物。

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