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1. 发明授权

US4317912A Tetracyclic indole derivatives 失效
标题翻译：四环吲哚衍生物
公开(公告)号：US4317912A
公开(公告)日：1982-03-02
申请号：US129333
申请日：1980-03-11
申请人： Aldemio Temperilli , Sergio Mantegani , Giuliana Arcari , Anna M. Caravaggi
发明人： Aldemio Temperilli , Sergio Mantegani , Giuliana Arcari , Anna M. Caravaggi
IPC分类号： C07D457/02 , A61K31/40 , A61K31/48 , A61P9/12 , C07D487/06 , A61K31/445 , A61K31/535 , C07D487/00
CPC分类号： C07D487/06
摘要： A compound is disclosed of the formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, or a carboxy, alkoxycarbonyl, piperidinocarbonyl, 1-pyrrolidinylcarbonyl, morpholinocarbonyl, carbamoyl or benzylcarbamoyl group, or an alkylcarbamoyl or dialkylcarbamoyl group in which the, or each, alkyl group has from 1 to 4 carbon atoms;R.sub.2 represents a hydrogen or fluorine atom, or a cyano, acetyl or carbamoyl group; andR.sub.3 represents a hydrogen atom or a methyl group; and represents a single or a double bond, with the proviso that R.sub.1 and R.sub.2 do not simultaneously represent hydrogen atoms;or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了式（I）的化合物：其中R 1表示氢原子，或羧基，烷氧基羰基，哌啶子基羰基，1-吡咯烷基羰基，吗啉代羰基，氨基甲酰基或苄基氨基甲酰基，或烷基氨基甲酰基或二烷基氨基甲酰基其中或每个烷基具有1至4个碳原子; R2表示氢或氟原子，或氰基，乙酰基或氨基甲酰基; 并且R 3表示氢原子或甲基; 并且表示单键或双键，条件是R1和R2不同时表示氢原子; 或其药学上可接受的盐。

2. 发明授权

US4252941A Ergot derivatives 失效
标题翻译： Ergot衍生物
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。

3. 发明授权

US4785001A Ergoline esters 失效
标题翻译：二甘醇酯
公开(公告)号：US4785001A
公开(公告)日：1988-11-15
申请号：US52380
申请日：1987-05-21
申请人： Aldemio Temperilli , Roberto Maj , Sergio Mantegani , Enzo Brambilla
发明人： Aldemio Temperilli , Roberto Maj , Sergio Mantegani , Enzo Brambilla
IPC分类号： A61K31/48 , A61P25/28 , C07D457/02 , C07D457/04
CPC分类号： C07D457/02
摘要： Ergoline Esters having the formula (I) ##STR1## in which R.sub.1 =H or CH.sub.3 ; R.sub.2 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.3 =H or OCH.sub.3 ; R.sub.4 =H or halogen; R.sub.5 =C.sub.1 -C.sub.4 alkyl and their pharmaceutically acceptable salts are active at the central nervous system level. A process for their preparation is described.
摘要翻译：具有式（I）的化合物酯（I）其中R 1 = H或CH 3; R2 = C1-C4烃; R3 = H或OCH3; R4 = H或卤素; R5 = C1-C4烷基及其药学上可接受的盐在中枢神经系统水平上是活性的。描述了其制备方法。

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

US4839363A Ergolinyl heterocycles for the treatment of Parkinson's disease and dyskinetic symptoms 失效
标题翻译：用于治疗帕金森氏病和运动障碍症状的二元杂环化合物
公开(公告)号：US4839363A
公开(公告)日：1989-06-13
申请号：US149012
申请日：1988-01-27
申请人： Enzo Brambilla , Sergio Mantegani , Lorenzo Pegrassi , Alessandro Rossi , Aldemio Temperilli
发明人： Enzo Brambilla , Sergio Mantegani , Lorenzo Pegrassi , Alessandro Rossi , Aldemio Temperilli
IPC分类号： A61K31/48 , A61P25/00 , C07D457/00 , C07D457/02
CPC分类号： C07D457/00 , C07D457/02
摘要： Ergoline derivatives of the 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;R.sub.3 represents a hydrocarbon group having from 1 to 4 carbon atoms;X represents a nitrogen atom and Y represents an oxygen atom, a ##STR2## group wherein R.sub.4 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl or a phenyl group, R.sub.5 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a phenyl, an amino or di(C.sub.1 -C.sub.4 alkyl)amino group and the nitrogen atom of the group ##STR3## is not joined to the nitrogen atom represented by X, or Y represents a nitrogen atom and X represents an oxygen atom or a ##STR4## group wherein R.sub.4 is as above defined; and the pharmaceutically acceptable salt thereof; are useful for treatment of Parkinsonism and dyskinetic symptoms.

6. 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。

7. 发明授权

US4859678A N-oxide ergolines as antihypertensive agents 失效
标题翻译： N-氧化物麦角醇作为抗高血压药
公开(公告)号：US4859678A
公开(公告)日：1989-08-22
申请号：US210420
申请日：1988-06-21
申请人： Sergio Mantegani , Enzo Brambilla , Aldemio Temperilli , Daniela Ruggieri , Patricia Salvati
发明人： Sergio Mantegani , Enzo Brambilla , Aldemio Temperilli , Daniela Ruggieri , Patricia Salvati
IPC分类号： A61K31/48 , A61P9/12 , C07D457/02 , C07D457/12
CPC分类号： C07D457/12 , C07D457/02
摘要： An ergoline derivative of the formula I: ##STR1## wherein R.sub.1 represents hydrogen or a methyl group; R.sub.2 represents hydrogen or a halogen atom, a methyl, cyano or phenyl group or an alkylthio group having from 1 to about 4 carbon atoms; R.sub.3 represents a hydrocarbon group having from 1 to about 4 carbon atoms; R.sub.4 represents hydrogen, a phenyl group or a hydrocarbon group having from 1 to about 4 carbon atoms; wherein either (a) R.sub.6 and R.sub.7 represent a valence bond or hydrogen atoms and R.sub.8 represents a hydrogen atom or a methoxy group, or (b) R.sub.6 represents a hydrogen atom and R.sub.7 and R.sub.8 taken together represent a valence bond; W represents an oxygen atom or an imino group; A represents a group of the formula CHR.sub.5, CH.dbd.CR.sub.5 or CH.sub.2 CHR.sub.5 wherein R.sub.5 represents a hydrogen atom or an alkyl group having from 1 to about 4 carbon atoms; X represents an oxygen or sulphur atom or an imino group; and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.

8. 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。

9. 发明授权

US4728649A 3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity 失效
标题翻译：具有抗癌剂活性的3-氧代 - 哌嗪-1-基 - 麦角酰胺
公开(公告)号：US4728649A
公开(公告)日：1988-03-01
申请号：US817135
申请日：1986-01-08
申请人： Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi , Lorenzo Pegrassi
发明人： Sergio Mantegani , Aldemio Temperilli , Gabriella Traquandi , Alessandro Rossi , Lorenzo Pegrassi
IPC分类号： A61K31/48 , A61P9/12 , A61P25/00 , A61P25/20 , C07D457/02 , C07D457/12 , A61K31/445
CPC分类号： C07D457/02
摘要： The invention relates to ergoline derivatives having the general formula (I): ##STR1## where R=H, CH.sub.3 ; R.sub.1 =H, halogen, CH.sub.3, phenylthio, C.sub.1 -C.sub.4 alkylthio; R.sub.2 =H, CH.sub.3 O, and R.sub.3 =H or R.sub.2 +R.sub.3 =chemical bond; R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon; R.sub.5, R.sub.6, R.sub.8, R.sub.9 independently=H, C.sub.1 -C.sub.4 alkyl, or R.sub.5, R.sub.8 independently=H, C.sub.1 -C.sub.4 alkyl and R.sub.6 +R.sub.9 =CH.sub.2 CH.sub.2, CH.sub.2 CH.sub.2 CH.sub.2 ; R.sub.7 =H, C.sub.1 -C.sub.4 alkyl, phenyl, NR'R"; R',R" independently=H, C.sub.1 -C.sub.4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H.sub.2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：本发明涉及具有通式（I）的麦角灵衍生物：其中R = H，CH 3; R1 = H，卤素，CH3，苯硫基，C1-C4烷硫基; R2 = H，CH3O，R3 = H或R2 + R3 =化学键; R4 = C1-C4烃; R5，R6，R8，R9独立地为H，C1-C4烷基或R5，R8独立地为H，C1-C4烷基和R6 + R9 = CH2CH2，CH2CH2CH2; R7 = H，C1-C4烷基，苯基，NR'R“ R'，R“独立地为H，C 1 -C 4烷基，酰基或NR'R”=杂环; W = 0，H2; n = 0,1,2及其药学上可接受的盐，这些具有抗高血压活性的化合物使它们成为抗焦虑药和抗精神病药。还描述了其制备方法和含有它们的药物组合物。

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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