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1. 发明授权

US4558049A Antipsycotic benzoxazines 失效
标题翻译：抗精神病药物
公开(公告)号：US4558049A
公开(公告)日：1985-12-10
申请号：US493618
申请日：1983-05-11
申请人： Luigi Bernardi , Ettore Lazzari , Maria L. Malnati , Giuseppe Mazzini , Lorenzo Pegrassi , Alessandro Rossi
发明人： Luigi Bernardi , Ettore Lazzari , Maria L. Malnati , Giuseppe Mazzini , Lorenzo Pegrassi , Alessandro Rossi
IPC分类号： A61K31/535 , A61P25/18 , C07D211/52 , C07D498/10
CPC分类号： C07D211/52
摘要： There are provided compounds of formula 1: ##STR1## wherein R=halogen atom or CN, NH.sub.2 and NO.sub.2 group, and pharmaceutically acceptable salts thereof.The compounds are antipsycotic agents.
摘要翻译：提供式1化合物：其中R =卤素原子或CN，NH 2和NO 2基团，及其药学上可接受的盐。这些化合物是抗精神病药。

2. 发明授权

US3948890A 4H-1,3-benzoxazin-2-one-3-acetohydroxamic acid derivatives 失效
标题翻译： 4H-1,3-苯并恶嗪-2-酮-3-乙酰肟酸衍生物
公开(公告)号：US3948890A
公开(公告)日：1976-04-06
申请号：US319724
申请日：1972-12-29
申请人： Giselbert Karl Suchowsky, deceased , Luigi Bernardi , Severina Coda , Lorenzo Pegrassi
发明人： Giselbert Karl Suchowsky, deceased , Luigi Bernardi , Severina Coda , Lorenzo Pegrassi
IPC分类号： C07D265/18 , C07D87/08
CPC分类号： C07D265/18
摘要： Compounds of the formula: ##EQU1## wherein R and R' are lower alkyl groups having from 1 to 4 carbon atoms, eventually substituted by a hydroxyl group; n is an integer from 0 to 3 and R' together with the ##EQU2## group jointly represent the group ##EQU3## A process for the preparation of these compounds is also disclosed. The compounds of the invention display interesting pharmacological activities and may be usefully employed as antidepressants.
摘要翻译：下式的化合物：其中R和R'是具有1至4个碳原子的低级烷基，最后被羟基取代，其中R 1，R 2，R 3，R 3，组; n是0至3的整数，R'与R - （CH 2）n-N ANGLE R基团一起表示基团-CH 2 -CH 2 ANGLE N-CH 2 -CH 2 -OH。 -CH 2 -CH 2还公开了制备这些化合物的方法。本发明的化合物显示出有趣的药理活性，可用作抗抑郁药。

3. 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。

4. 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。

5. 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。

6. 发明授权

US5721227A 17-aryl and 17-heterocyclyl-14.beta.-5.alpha.-androstane, androstene and androstadiene derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing same 失效
标题翻译： 17-芳基和17-杂环基-14β-5α-雄甾烷，对心血管系统有活性的雄甾烯和雄二烯衍生物衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5721227A
公开(公告)日：1998-02-24
申请号：US552796
申请日：1995-11-03
申请人： Piero Melloni , Luigi Bernardi , Mara Ferrandi , Marco Frigerio , Marina Mauro , Luisa Quadri
发明人： Piero Melloni , Luigi Bernardi , Mara Ferrandi , Marco Frigerio , Marina Mauro , Luisa Quadri
IPC分类号： A61K31/565 , A61K31/575 , A61K31/58 , A61P9/00 , A61P9/12 , C07J1/00 , C07J9/00 , C07J17/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00
CPC分类号： C07J31/006 , C07J1/0011 , C07J17/00 , C07J31/003 , C07J33/002 , C07J41/0005 , C07J41/0055 , C07J41/0088 , C07J43/003 , C07J51/00 , C07J9/00
摘要： 17-Aryl -5.alpha.,14.beta.-androstane, androstene and androstadiene derivatives of formula (I): ##STR1## wherein the symbol --- represents a single or a double bond; when the double bond is not present in the 4 or 5 position, the hydrogen in position 5 has the .alpha. configuration; Y is oxygen or guanidinoimino, when --- in position 3 is a double bond; Y is hydroxy, OR.sup.2 or SR.sup.2, when in position 3 is a single bond and has an .alpha. or .beta. configuration; R is a substituted or unsubstituted aryl ring; and R.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.
摘要翻译： 17-芳基-5α，14β-雄甾烷，式（I）的雄甾烯和雄二醇和雄二醇衍生物：其中符号+ E，uns --- + EE表示单键或双键; 当双键不存在于4或5位时，位置5中的氢具有α构型; Y是氧或胍基亚氨基，当位置3的+ E，uns --- + EE是双键时; 当位置3为单键且具有α或β构型时，Y为羟基，OR2或SR2; R是取代或未取代的芳基环; 并且R 1是被OH或NR 4 R 5取代的氢，甲基，乙基或正丙基。

7. 发明授权

US5567697A 17-(4-pyridazinyl) -5.beta., 14.beta.-androstane derivatives active on the cardiovascular system, processes for their preparation and pharmaceutical compositions containing same 失效
标题翻译：对心血管系统有活性的17-（4-哒嗪基）-5β，14β-雄甾烷衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5567697A
公开(公告)日：1996-10-22
申请号：US458822
申请日：1995-06-02
申请人： Luisa Quadri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Piero Melloni , Loredana Valentino
发明人： Luisa Quadri , Luigi Bernardi , Giuseppe Bianchi , Patrizia Ferrari , Piero Melloni , Loredana Valentino
IPC分类号： A61K31/565 , A61K31/56 , A61K31/58 , A61K31/585 , A61P9/00 , A61P9/10 , A61P9/12 , C07J1/00 , C07J17/00 , C07J41/00 , C07J43/00 , C07J71/00
CPC分类号： C07J41/0005 , C07J17/00 , C07J41/0088 , C07J43/003 , C07J71/0021
摘要： Present invention relates to a group of 17-(4-pyridazinyl)-5.beta.,14.beta.-androstane derivates active on the cardiovascular system and to pharmaceutical compositions containing same.
摘要翻译：本发明涉及对心血管系统有活性的一组17-（4-哒嗪基）-5β，14β-雄甾烷衍生物以及含有它们的药物组合物。

8. 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。

9. 发明授权

US4223146A 4,5,6,7-Tetrahydroimidazo-[4,5-c]-pyridine derivatives 失效
标题翻译： 4,5,6,7-四氢咪唑并[4,5-c] - 吡啶衍生物
公开(公告)号：US4223146A
公开(公告)日：1980-09-16
申请号：US959506
申请日：1978-11-13
申请人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Ugo Scarponi
发明人： Giuliana Arcari , Luigi Bernardi , Giovanni Falconi , Ugo Scarponi
IPC分类号： A61K31/4188 , A61K31/435 , A61K31/437 , A61P1/04 , A61P25/02 , C07D471/04
CPC分类号： C07D471/04 , Y10S514/925
摘要： Compounds are disclosed of the general formula (I): ##STR1## wherein R.sub.1 is a lower alkyl having from 1 to 4 carbon atoms; R.sub.2 is hydrogen or a lower alkyl having from 1 to 4 carbon atoms; and R.sub.3 is a saturated or unsaturated straight or branched alkyl having from 1 to 4 carbon atoms. A process for making such compounds is also disclosed. These compounds are useful as antiulcer agents and as inhibitors of gastric secretion.
摘要翻译：公开了通式（I）的化合物：其中R 1是具有1至4个碳原子的低级烷基; R2是氢或具有1至4个碳原子的低级烷基; 并且R 3是具有1至4个碳原子的饱和或不饱和的直链或支链烷基。还公开了制备这些化合物的方法。这些化合物可用作抗溃疡剂和胃分泌抑制剂。

10. 发明授权

US4196288A Ergoline derivatives and a process for their preparation 失效
标题翻译：艾尔莫林衍生物及其制备方法
公开(公告)号：US4196288A
公开(公告)日：1980-04-01
申请号：US856536
申请日：1977-12-01
申请人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
发明人： Enzo Beacco , Luigi Bernardi , Enrico Di Salle , Giovanni Falconi , Bianca Patelli
IPC分类号： A61K31/48 , A61K31/495 , A61K31/505 , C07D457/02
CPC分类号： C07D457/02
摘要： New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle. The heterocycle may be a 5- or 6-membered ring which contains from 1 to 3 hetero atoms selected from the class consisting of nitrogen, oxygen and sulphur, and may be saturated or unsaturated, and unsubstituted or substituted by halogen, alkyl having from 1 to 3 carbon atoms, hydroxy, nitro, amino, CONHNH.sub.2 and COOH.
摘要翻译：公开了新的麦角灵衍生物，其是具有以下结构的式（I）的化合物：其中R 1是氢或甲氧基; R2是氢或甲基; 并且X是羟基，R 3 COO，S-R 4或NR 5 R 6，其中R 3是具有1至6个碳原子的直链或支链烷基，未取代或取代的苯基，所述取代基选自氯，溴，烷基或具有1至4个碳原子的烷氧基，含3至6个碳原子的环烷基或杂环; R 4是苯基或杂环，R 5和R 6是具有1至4个碳原子的烷基，或与它们相连的N原子一起形成杂环。杂环可以是含有1至3个选自氮，氧和硫的杂原子的5或6元环，并且可以是饱和或不饱和的，未取代的或被卤素取代的烷基，具有1个至3个碳原子，羟基，硝基，氨基，CONHNH 2和COOH。

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