专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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。

4. 发明授权

US4895836A Nor-cholanic acid derivatives, a process for their preparation, their use and pharmaceutical compositions containing them 失效
标题翻译：非胆酸衍生物，其制备方法及其用途和含有它们的药物组合物
公开(公告)号：US4895836A
公开(公告)日：1990-01-23
申请号：US133043
申请日：1987-10-29
申请人： Laura Chiodini , Mauro Gobbini , Sergio Mantegani , Daniel Ruggieri , Aldemio Temperilli , Gabriella Traquandi , Patrizia Ferrari
发明人： Laura Chiodini , Mauro Gobbini , Sergio Mantegani , Daniel Ruggieri , Aldemio Temperilli , Gabriella Traquandi , Patrizia Ferrari
IPC分类号： A61K31/575 , C07J1/00 , C07J41/00
CPC分类号： C07J41/0088 , C07J41/0055
摘要： ##STR1## Compounds I (either R
1 =OH, C
1 -C
4 alkoxy and R
2 =H, C
1 -C
4 alkyl, or R
1 +R
2 =a chemical bond; R
3 =an aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being α or β: and either R
4 =OH and R
5 =H or R
4 +R
5 =a chemical bond) and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP87 / 00006 Sec。 371日期1987年10月29日第 102（e）1987年10月29日PCT PCT 1987年1月7日PCT公布。出版物WO87 / 04166 日期1987年7月16日。化合物I（R1 = OH，C1-C4烷氧基和R2 = H，C1-C4烷基或R1 + R2 =化学键; R3 =氨基脱氧或氨基二脱氧或氨基歧氮 D和L系列的糖残基，糖苷键为α或β：R4 = OH和R5 = H或R4 + R5 =化学键）及其药学上可接受的盐可用作抗高血压药。还描述了它们的制备和用途以及含有它们的药物组合物。

5. 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。

6. 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。

7. 发明授权

US4882315A Aminoglycoside steroids, a process for their preparation, their use and pharmaceutical compositions containing them 失效
标题翻译：氨基糖苷类固醇，其制备方法及其用途和含有它们的药物组合物
公开(公告)号：US4882315A
公开(公告)日：1989-11-21
申请号：US133035
申请日：1987-10-29
申请人： Laura Chiodini , Mauro Gobbini , Sergio Mantegani , Daniel Ruggieri , Aldemio Temperilli , Gabriella Traquandi , Patrizia Ferrari
发明人： Laura Chiodini , Mauro Gobbini , Sergio Mantegani , Daniel Ruggieri , Aldemio Temperilli , Gabriella Traquandi , Patrizia Ferrari
IPC分类号： A61K31/58 , C07J1/00 , C07J71/00
CPC分类号： C07J71/001
摘要： ##STR1## Compounds I (either R
1 =OH, C
1 -C
4 alkoxy and R
2 =H, C
1 -C
4 alkyl, or R
1 +R
2 =a chemical bond; R
3 =an aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being α or β) and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP87 / 00004 Sec。 371日期1987年10月29日第 102（e）1987年10月29日PCT PCT 1987年1月7日PCT公布。出版物WO87 / 04167 日期1987年7月16日。化合物I（R1 = OH，C1-C4烷氧基和R2 = H，C1-C4烷基或R1 + R2 =化学键; R3 =氨基脱氧或氨基二脱氧或氨基歧氮 D和L系列的糖残基，糖苷键为α或β）及其药学上可接受的盐可用作抗高血压药。还描述了其制备和用途以及含有它们的药物组合物。

8. 发明授权

US4920099A Aminoglycoside steroids, a process for their preparation, their use and pharmaceutical compositions containing them 失效
标题翻译：氨基糖苷类固醇，其制备方法及其用途和含有它们的药物组合物
公开(公告)号：US4920099A
公开(公告)日：1990-04-24
申请号：US123855
申请日：1987-10-29
申请人： Laura Chiodini , Mauro Gobbini , Sergio Mantegani , Daniela Ruggieri , Aldemio Temperilli , Gabriella Traquandi , Patrizia Ferrari
发明人： Laura Chiodini , Mauro Gobbini , Sergio Mantegani , Daniela Ruggieri , Aldemio Temperilli , Gabriella Traquandi , Patrizia Ferrari
IPC分类号： A61K31/585 , C07J1/00 , C07J71/00
CPC分类号： C07J71/0057
摘要： ##STR1## Compounds I [R
1 =H or C
1 -C
3 alkyl, R
2 =an (alkyl-substituted) aminodeoxy or aminodideoxy or aminotrideoxy sugar residue of the D and L series, the glycosidic linkage being α or β] and their pharmaceutically acceptable salts are useful as antihypertensive agents. Their preparation and use as well as pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP87 / 00005 Sec。 371日期1987年10月29日第 102（e）1987年10月29日PCT PCT 1987年1月7日PCT公布。公开号WO87 / 04168 日期1987年7月16日。图像I化合物I [R1 = H或C1-C3烷基，R2 = D和L系列的（烷基取代的）氨基脱氧或氨基二脱氧或氨基三脱氧糖残基，糖苷键为α 或β]及其药学上可接受的盐可用作抗高血压药。还描述了它们的制备和用途以及含有它们的药物组合物。

9. 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.

10. 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。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式