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1. 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。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明授权

US06316451B1 Heterocyclyl anthracyclinone derivatives 失效
标题翻译：杂环蒽环类衍生物
公开(公告)号：US06316451B1
公开(公告)日：2001-11-13
申请号：US09623859
申请日：2000-09-26
申请人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Jacqueline Lansen , Mario Varasi
发明人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Jacqueline Lansen , Mario Varasi
IPC分类号： C07D27742
CPC分类号： C07D417/04 , C07D233/88 , C07D277/40 , C07D277/42
摘要： A compound of formula (1) wherein R1 is hydrogen, hydroxy, a group of formula OR5 wherein R5 is C1-C6 alkyl, C2-C6 alkenyl or C3-C8 cycloalkyl, halogen, amino which may be unsubstituted or mono or disubstituted by C1-C6 alkyl, C2-C6 alkenyl, aralkyl, acyl or trifluoroacetyl; R2 is hydrogen, hydroxy, a group NR6R7 wherein R6 and R7 independently represent hydrogen, an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C3-C8 cycloalkyl or, taken together with the nitrogen atom, represent an optionally substituted C3-C8 heterocyclic ring; R3 is hydrogen, hydroxy, R4 is a 2-substituted thiazolyl or imidazolyl system and the pharmaceutically acceptable salt thereof, is useful in the treatment of amyloidosis. Processes for the preparation and pharmaceutical compositions are also described.
摘要翻译：式（1）的化合物，其中R 1是氢，羟基，式OR 5的基团，其中R 5是C 1 -C 6烷基，C 2 -C 6烯基或C 3 -C 8环烷基，卤素，可被未被取代或被C1单或二取代的氨基 C 6烷基，C 2 -C 6烯基，芳烷基，酰基或三氟乙酰基; R 2是氢，羟基，NR 6 R 7基团，其中R 6和R 7独立地表示氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基，C 3 -C 8环烷基或与氮原子一起代表任选取代的C 3 -C 8 杂环 R3是氢，羟基，R4是2-取代的噻唑基或咪唑基系统及其药学上可接受的盐，可用于治疗淀粉样变性。还描述了制备方法和药物组合物。

9. 发明授权

US5210194A Process for preparing ergoline derivatives 失效
标题翻译：制备葡萄糖衍生物的方法
公开(公告)号：US5210194A
公开(公告)日：1993-05-11
申请号：US761977
申请日：1991-09-25
申请人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Enzo Brambilla
发明人： Sergio Mantegani , Gabriella Traquandi , Tiziano Bandiera , Enzo Brambilla
IPC分类号： C07D457/00 , C07D457/02 , C07D457/12
CPC分类号： C07D457/12 , C07D457/02
摘要： Ergoline derivatives of the formula I: ##STR1## wherein R represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.1 represents hydrogen, chlorine, bromine or methyl; either R.sub.2 and R.sub.3 both represent hydrogen or together represent a chemical bond; R.sub.4 represents a C.sub.1 -C.sub.4 hydrocarbon group; each of R.sub.5, R.sub.6, R.sub.8 and R.sub.9 independently represents hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.7 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or C.sub.3 -C.sub.7 cycloalkyl and n is 0, 1 or 2; are prepared by reaction between compounds of the formulae II and III: ##STR2## and subsequent cyclization of the resultant compounds. The compounds of the formula I are known useful anxiolytic, antipsychotic and anti-parkinson agents.
摘要翻译： PCT No.PCT / EP91 / 00104 Sec。 371日期1991年9月25日 102（e）1991年9月25日PCT 1991年1月21日PCT PCT。第WO91 / 11447号公报 1991年8月8日。式I的喹啉衍生物：其中R表示氢或C 1 -C 4烷基; R1代表氢，氯，溴或甲基; R2和R3均表示氢或一起代表化学键; R4代表C1-C4烃基; R5，R6，R8和R9各自独立地表示氢或C1-C4烷基; R 7表示氢，C 1 -C 4烷基，苯基或C 3 -C 7环烷基，n为0,1或2; 通过式II和III的化合物与所得化合物的环化反应制备。式I的化合物是已知的有用的抗焦虑药，抗精神病药和抗帕金森药。

10. 发明授权

US08981089B2 Pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors 有权
标题翻译：吡唑并喹唑啉衍生物，其制备方法及其作为激酶抑制剂的用途
公开(公告)号：US08981089B2
公开(公告)日：2015-03-17
申请号：US13972659
申请日：2013-08-21
申请人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
发明人： Gabriella Traquandi , Maria Gabriella Brasca , Roberto D'Alessio , Paolo Polucci , Fulvia Roletto , Anna Vulpetti , Paolo Pevarello , Achille Panzeri , Francesca Quartieri , Ron Ferguson , Paola Vianello , Daniele Fancelli
IPC分类号： C07D487/04 , C07D403/14 , C07D413/14 , C07D487/14 , C07D231/56 , C07D239/72
CPC分类号： C07D487/14 , A61K31/519 , A61K31/5377 , A61K31/551 , C07D231/56 , C07D239/72 , C07D401/10 , C07D403/14 , C07D413/14 , C07D487/04
摘要： Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
摘要翻译：公开了说明书中定义的式（Ia）或（Ib）的吡唑并喹唑啉衍生物及其药学上可接受的盐，其制备方法和包含它们的药物组合物; 本发明的化合物在治疗中可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

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