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1. 发明授权

US5079364A t-alkyl ergoline derivatives 失效
标题翻译： T-ALKYL ERGOLINE DERIVATIVES
公开(公告)号：US5079364A
公开(公告)日：1992-01-07
申请号：US328518
申请日：1989-03-24
申请人： Aldemio Temperilli , Enzo Brambilla , Mauro Gobbini , Maria A. Cervini
发明人： Aldemio Temperilli , Enzo Brambilla , Mauro Gobbini , Maria A. Cervini
IPC分类号： A61K31/48 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： t-alkyl eroline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinynoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.

2. 发明授权

US4843073A 1-t-butyl ergolines useful in the treatment of cerebral insufficiency and senile dementia 失效
标题翻译：可用于治疗脑功能不全和老年痴呆的1-叔丁基麦角醇
公开(公告)号：US4843073A
公开(公告)日：1989-06-27
申请号：US065597
申请日：1987-06-23
申请人： Aldemio Temperilli , Enzo Brambilla , Mauro Gobbini , Maria A. Cervini
发明人： Aldemio Temperilli , Enzo Brambilla , Mauro Gobbini , Maria A. Cervini
IPC分类号： A61K31/48 , A61P25/28 , C07D457/02
CPC分类号： C07D457/02
摘要： t-Alkyl ergoline derivatives of formula I are produced ##STR1## wherein (R.sub.1 =H, OCH.sub.3 and R.sub.2 =H) or (R.sub.1 +R.sub.2 =a ring bond and R.sub.3 =H, optionally substituted nicotinoyl or 1-oxo-2-cyclopenten-3-yl); and their pharmaceutically acceptable salts.A process for the preparation of these derivatives from lysergol and a t-alkyl alcohol is also described, as are pharmaceutical compositions containing them.
摘要翻译：其中（R1 = H，OCH3和R2 = H）或（R1 + R2 =环键，R3 = H，任选取代的烟酰基或1-氧代-2-环戊烯 -3-基）; 及其药学上可接受的盐。还描述了从lycgol和t-烷基醇制备这些衍生物的方法，以及含有它们的药物组合物。

3. 发明授权

US5430031A Serotoninergic ergoline derivatives 失效
标题翻译：血清素能麦角因衍生物
公开(公告)号：US5430031A
公开(公告)日：1995-07-04
申请号：US169177
申请日：1993-12-20
申请人： Sergio Mantegani , Enzo Brambilla , Carla Caccia , Nicola Carfagna
发明人： Sergio Mantegani , Enzo Brambilla , Carla Caccia , Nicola Carfagna
IPC分类号： A61K31/48 , A61P1/08 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , A61P25/30 , A61P43/00 , C07D457/02 , C07D457/04 , C07D457/06 , C07D457/08 , C07D457/12 , A61K31/495 , A61K31/505 , C07D403/14
CPC分类号： C07D457/04 , C07D457/02 , C07D457/08 , C07D457/12
摘要： The present invention provides compounds of the formula (I) ##STR1## wherein A, R.sub.1, R.sub.2 and R.sub.3 are defined as in the specification, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmacetical compositions comprising them are also provided.
摘要翻译：本发明提供式（I）的化合物，其中A，R 1，R 2和R 3如说明书中所定义，或其药学上可接受的盐。还提供了其制备方法和包含它们的药物组合物。

4. 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.

5. 发明授权

US4801588A Tetracyclic indole derivatives for treating hypertension 失效
标题翻译：用于治疗高血压的四环吲哚衍生物
公开(公告)号：US4801588A
公开(公告)日：1989-01-31
申请号：US73438
申请日：1987-07-15
申请人： Aldemio Temperilli , Rosanna Eccel , Enzo Brambilla , Patricia Salvati
发明人： Aldemio Temperilli , Rosanna Eccel , Enzo Brambilla , Patricia Salvati
IPC分类号： C07D487/04 , A61K31/40 , A61P9/12 , C07D457/02 , C07D487/06 , A61K31/415 , C07D487/02
CPC分类号： C07D487/06
摘要： Compounds of the formula I: ##STR1## wherein R.sub.1 =H, CH.sub.3 ; m=0,1; R.sub.2 =R.sub.3 =H or R.sub.2, R.sub.3 =bond, R.sub.4 =C.sub.1 -C.sub.4 hydrocarbon, n=1 or 2 and their pharmaceutically acceptable salts are antihypertensive agents. Their preparation and pharmaceutical compositions containing them are also described.
摘要翻译：式I的化合物：其中R 1 = H，CH 3; m = 0,1; R2 = R3 = H或R2，R3 =键，R4 = C1-C4烃，n = 1或2，其药学上可接受的盐是抗高血压药。还描述了它们的制备方法和含有它们的药物组合物。

6. 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。

7. 发明授权

US06284896B1 Abeo-ergoline derivatives as 5HT1A ligands 失效
标题翻译：二氢麦角灵衍生物作为5HT1A配体
公开(公告)号：US06284896B1
公开(公告)日：2001-09-04
申请号：US08998867
申请日：1997-12-29
申请人： Sergio Mantegani , Tiziano Bandiera , Enzo Brambilla , Carla Caccia , Nicola Carfagna
发明人： Sergio Mantegani , Tiziano Bandiera , Enzo Brambilla , Carla Caccia , Nicola Carfagna
IPC分类号： C07D48706
CPC分类号： C07D487/06
摘要： There are provided compounds of formula (I), wherein R1 is a hydrogen, chlorine or bromine atom or a methyl, methylthio, hydroxy, cyano or carboxamido group; R2 is C1-C3 alkyl or an alkyl group; R3 and R4 are independently a hydrogen atom, a C1-C5 alkyl group, a C3-C5 alkenyl group, a C5-C6 cycloalkyl C1-C3 alkyl group, a phenyl-C3-C5 alkenyl or phenyl group: which groups are optionally substituted by C1-C3 alkyl, C1-C3 alkoxy, triflouromethyl, hydroxy or amino group; or a group of formula (a), wherein R6 is hydrogen atom or a C1-C3 alkyl group and R7 is a phenyl group, a substituted phenyl group as described above or a heterocyclic ring, R5 is a hydrogen or bromine atom or an organic residue and R is H or an organic residue, or a pharmaceutically acceptable salt thereof. A process for their preparation and the pharmaceutical compositions comprising them are also provided.
摘要翻译：提供式（I）化合物，其中R 1是氢，氯或溴原子或甲基，甲硫基，羟基，氰基或甲酰氨基; R2是C1-C3烷基或烷基; R3和R4独立地是氢原子，C1-C5烷基，C3-C5烯基，C5-C6环烷基C1-C3烷基，苯基-C3-C5链烯基或苯基：这些基团是任选取代的 C 1 -C 3烷基，C 1 -C 3烷氧基，三氟甲基，羟基或氨基; 或式（a）的基团，其中R6是氢原子或C1-C3烷基，R7是苯基，如上所述的取代苯基或杂环，R5是氢或溴原子或有机残基，R为H或有机残基，或其药学上可接受的盐。还提供了其制备方法和包含它们的药物组合物。

8. 发明授权

US6060483A Antineurodegenerative ergoline derivatives 失效
标题翻译：抗神经变性麦角灵衍生物
公开(公告)号：US6060483A
公开(公告)日：2000-05-09
申请号：US147448
申请日：1998-12-28
申请人： Sergio Mantegani , Enzo Brambilla , Nicola Carfagna , Mario Varasi
发明人： Sergio Mantegani , Enzo Brambilla , Nicola Carfagna , Mario Varasi
IPC分类号： A61K31/48 , C07D457/02 , C07D457/10
CPC分类号： C07D457/10 , A61K31/48 , C07D457/02
摘要： The present invention provides the new use in the treatment of neurodegenerative diseases with ergoline derivatives of formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or C.sub.2 -C.sub.5 alkenyl group optionally substituted with a C.sub.3 -C.sub.7 cycloalkyl, a hydroxy group or a R.sub.3 -substituted phenyl group wherein R.sub.3 is a hydroxy or a hydroxymethyl group; R.sub.2 represents a hydrogen atom or a linear or branched C.sub.1 -C.sub.5 alkyl or a C.sub.2 -C.sub.5 alkenyl group optionally substituted with a hydroxy group, or a R.sub.3 -substituted phenyl group wherein R.sub.3 is as above defined, or with a C.sub.1 -C.sub.5 alkoxy group; the symbols--at positions 2,3 and 8, 9 independently denote a single or double chemical bond and Z represents a group (CH.sub.2).sub.n OH, wherein n is 0 or an integer from 1 to 3, or a group C(R.sub.4).sub.2 OH wherein R.sub.4 is a C.sub.1 -C.sub.5 alkyl or a phenyl group, or a pharmaceutically acceptable salt thereof. Some compounds of formula (I) are novel. Processes for their preparation and pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP97 / 02955 Sec。 371日期1998年12月28日第 102（e）日期1998年12月28日PCT提交1987年5月29日PCT公布。第WO98 / 00424号公报日本1998年1月8日本发明提供了用于治疗神经变性疾病的新用途，其中式（I）的麦角灵衍生物其中R 1表示氢原子或直链或支链C 1 -C 5烷基或C 2 -C 5烯基，任选被 C3-C7环烷基，羟基或R3-取代的苯基，其中R3是羟基或羟甲基; R2表示氢原子或任选被羟基取代的直链或支链C 1 -C 5烷基或C 2 -C 5烯基，或其中R 3如上所定义的R 3取代苯基，或与C 1 -C 5烷氧基 ; 位置2,3和8,9独立地表示单一或双重化学键，Z表示基团（CH 2）n OH，其中n为0或1至3的整数，或基团C（R 4）2 OH 其中R4是C1-C5烷基或苯基，或其药学上可接受的盐。一些式（I）化合物是新的。还描述了其制备方法和含有它们的药物组合物。

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

US5202325A Use of ergoline derivatives in treating emesis 失效
标题翻译： ERGOLINE衍生物在治疗EMESIS中的应用
公开(公告)号：US5202325A
公开(公告)日：1993-04-13
申请号：US499413
申请日：1990-07-12
申请人： Alessandro Rossi , Metilde Buonamici , Lorenzo Pegrassi , Enzo Brambilla
发明人： Alessandro Rossi , Metilde Buonamici , Lorenzo Pegrassi , Enzo Brambilla
IPC分类号： C07D457/02 , A61K31/48 , A61K31/495 , A61P1/08
CPC分类号： A61K31/495 , A61K31/48 , Y10S514/872
摘要： Compounds of the formula I ##STR1## wherein n is 1 or 2, R.sub.1 represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sub.2 represents a hydrogen atom and R.sub.3 represents a hydrogen atom or a hydroxy group or R.sub.2 and R.sub.3 together represent a chemical bond, R.sub.4 represents a hydrogen atom, or a phenyl or C.sub.1 -C.sub.4 alkyl group, R.sub.5 represents a C.sub.1 -C.sub.4 alkyl group or an alkyl group and R.sub.6 represents a hydrogen or halogen atom, and the pharmaceutically acceptable salt thereof, are useful for the manufacture of a pharmaceutical composition useful in the treatment of emesis.

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