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1. 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.

2. 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。

3. 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。

4. 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。

5. 发明授权

US4500712A Ergoline derivatives 失效
标题翻译：二元醇衍生物
公开(公告)号：US4500712A
公开(公告)日：1985-02-19
申请号：US438259
申请日：1982-11-01
申请人： Luigi Bernardi , Aldemio Temperilli , Daniela Ruggieri , Giuliana Arcari , Patricia Salvati
发明人： Luigi Bernardi , Aldemio Temperilli , Daniela Ruggieri , Giuliana Arcari , Patricia Salvati
IPC分类号： A61K31/48 , A61P1/04 , A61P9/12 , C07D457/02 , C07D457/12 , C07D457/04
CPC分类号： C07D457/02 , C07D457/12
摘要： There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.
摘要翻译：提供式（Ⅰ）的麦角灵衍生物，其中R1 = H，CH3; R2 = H或卤素原子，或CH3，CN，烷基或苯基 - 硫基; R3 = H，OCH3; R4 = C1-C4烃基; X = O，S，NH; A = CO，SO2; B = C1-C4烃基，芳基，芳烷基，杂环基，烷氧基，芳氧基; n = 0,1,2; 及其药学上可接受的盐。还提供了制备所述化合物的方法。这些化合物显示出抗高血压活性，并且对胃肠系统有活性。

6. 发明授权

US5547667A Linker for bioactive agents 失效
标题翻译：生物活性剂接头
公开(公告)号：US5547667A
公开(公告)日：1996-08-20
申请号：US328697
申请日：1994-10-25
申请人： Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
发明人： Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K39/395 , A61K47/00 , A61K47/48 , A61P35/00 , C07H20060101 , C07H15/252 , C07H17/00 , C07H19/24 , A61K39/44 , C07K17/06 , C07K15/252 , C07K19/06
CPC分类号： C07H15/252 , A61K47/48176 , A61K47/48246 , A61K47/48407 , A61K47/48692 , A61K47/48715 , C07H19/24
摘要： Conjugates of general formula 1:[A--O--W--Z].sub.a --T 1wherein the moiety A--O-- is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.
摘要翻译：通式1的缀合物：[A-O-W-Z] a-T1，其中A-O-部分是式A-O-H的药物的残基，其中-O-H是伯或仲羟基; a为1〜30的整数; W是通式2的基团：其中b是1至4的整数，B表示C1-C3亚烷基，R1和R2各自独立地表示氢，卤素，烷基，苯基或取代的苯基; Z是间隔基，T是载体部分。

7. 发明授权

US4322412A Anthracycline glycosides, their preparation, use and compositions thereof 失效
标题翻译：蒽环类苷，其制备方法，用途及其组合物
公开(公告)号：US4322412A
公开(公告)日：1982-03-30
申请号：US168157
申请日：1980-07-14
申请人： Giuseppe Cassinelli , Salvatore Forenza , Maria C. Ripamonti , Daniela Ruggieri
发明人： Giuseppe Cassinelli , Salvatore Forenza , Maria C. Ripamonti , Daniela Ruggieri
IPC分类号： C07H15/252 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , A61P35/02 , C07H15/24 , A61K31/71
CPC分类号： C07H15/252
摘要： There are disclosed compounds which exhibit anti-tumor activity. These compounds are of the formula I: ##STR1## wherein R.sub.1 is hydrogen, hydroxy or methoxy, R.sub.2 is hydrogen or hydroxy, and each of R.sub.3 and R.sub.4 independently is hydrogen or methyl, with the proviso that R.sub.3 and R.sub.4 are not simultaneously hydrogen, and pharmaceutically acceptable acid addition salts thereof. Also disclosed are processes for producing and using said compounds and therapeutic compositions containing same.
摘要翻译：公开了表现出抗肿瘤活性的化合物。这些化合物具有式I：其中R 1是氢，羟基或甲氧基，R 2是氢或羟基，R 3和R 4各自独立地是氢或甲基，条件是R 3和R 4不同时为氢，及其药学上可接受的酸加成盐。还公开了生产和使用所述化合物和含有它们的治疗组合物的方法。

8. 发明授权

US4276289A Antitumor glycosides, their preparation and use 失效
标题翻译：抗肿瘤糖苷，其制备及用途
公开(公告)号：US4276289A
公开(公告)日：1981-06-30
申请号：US131035
申请日：1980-03-17
申请人： Giuseppe Cassinelli , Daniela Ruggieri , Federico Arcamone , Aurelio di Marco
发明人： Giuseppe Cassinelli , Daniela Ruggieri , Federico Arcamone , Aurelio di Marco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the formula I ##STR1## wherein R is hydrogen or hydroxyl and the hydrochlorides thereof, and which are useful in treating certain mammalian tumors, are prepared by condensing daunomycinone with the novel sugar, 4-O-methyl-2,3,6-trideoxy-3trifluoroacetamidoribohexopyranosyl chloride in an inert organic solvent and in the presence of a soluble silver salt and a dehydrating agent to form 3', 4' -diepi-4'-O-methyl-N-trifluoroacetyl daunorubicin, and removing the N-trifluoroacetyl group therefrom. This gives the compound wherein R is hydrogen. The former is converted to the corresponding hydroxyl compound by conventional means.
摘要翻译：通过将道诺霉素酮与新的糖4-O-甲基-2,3,3-四氢呋喃缩合来制备其中R为氢或羟基的式I的蒽环酸苷及其盐酸盐，其可用于治疗某些哺乳动物肿瘤，6-三脱氧-3-三氟乙酰胺六溴代吡喃葡萄糖氯化物在惰性有机溶剂中，在可溶性银盐和脱水剂存在下反应形成3'，4'-二甲基-4'-O-甲基-N-三氟乙酰柔红霉素，并除去 N-三氟乙酰基。这得到其中R是氢的化合物。前者通过常规方法转化成相应的羟基化合物。

9. 发明授权

US5776458A Anthracycline-conjugates 失效
标题翻译：蒽环霉素共轭物
公开(公告)号：US5776458A
公开(公告)日：1998-07-07
申请号：US412220
申请日：1995-03-27
申请人： Francesco Angelucci , Daniela Ruggieri , Stefania Stefanelli , Antonino Suarato , Laura Bersani
发明人： Francesco Angelucci , Daniela Ruggieri , Stefania Stefanelli , Antonino Suarato , Laura Bersani
IPC分类号： A61K47/48 , C07H15/252 , A61K39/395 , A61K39/00 , C07K16/00 , C07K17/00
CPC分类号： C07H15/252 , A61K47/48407
摘要： The present invention provides anthracycline conjugates with carriers such as monoclonal polyclonal antibodies, proteins or peptides, or other synthetic carriers. These anthracycline conjugates provide pharmaceutical compositions which are useful for treating certain mammalian tumors. The compounds of the present invention have higher potency than anthracyclines, and improved therapeutic efficacy and reduced toxic effects.
摘要翻译：本发明提供了与载体例如单克隆多克隆抗体，蛋白质或肽或其它合成载体的蒽环霉素缀合物。这些蒽环霉素缀合物提供可用于治疗某些哺乳动物肿瘤的药物组合物。本发明的化合物具有比蒽环类药更高的效力，并且具有改善的治疗功效和降低的毒性作用。

10. 发明授权

US5387578A New linker for bioactive agents 失效
标题翻译：生物活性剂的新接头
公开(公告)号：US5387578A
公开(公告)日：1995-02-07
申请号：US842171
申请日：1992-04-03
申请人： Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
发明人： Francesco Angelucci , Laura Bersani , Michele Caruso , Marina Ripamonti , Daniela Ruggieri , Antonino Suarato
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K39/395 , A61K47/00 , A61K47/48 , A61P35/00 , C07H20060101 , C07H15/252 , C07H17/00 , C07H19/24 , A61K37/00 , C07H19/06 , C07K17/06
CPC分类号： C07H15/252 , A61K47/48176 , A61K47/48246 , A61K47/48407 , A61K47/48692 , A61K47/48715 , C07H19/24
摘要： Conjugate of general formula 1:[A--O--W-Z].sub.a -T 1wherein the moity A--O--is the residue of drug of formula A--O--H in which --O--H is a primary or secondary hydroxyl group; a is an integer of from 1 to 30; W is a group of general formula 2: ##STR1## wherein b is an integer of from 1 to 4, B represents a C.sub.1 -C.sub.3 alkylene group and R.sub.1 and R.sub.2 each independently represent hydrogen, halogen, alkyl, phenyl or substituted phenyl; Z is a spacer group and T is a carrier moiety.
摘要翻译： PCT No.PCT / EP91 / 01449 371日期：1992年4月3日 102（e）日期1992年4月3日PCT 1991年8月1日PCT PCT。公开号WO92 / 02255 通式1：[A-O-W-Z] a-T1的结合物，其中，A-O-是式A-O-H药物的残基，其中-O-H是伯或仲羟基; a为1〜30的整数; W是通式2的基团：其中b是1至4的整数，B表示C1-C3亚烷基，R1和R2各自独立地表示氢，卤素，烷基，苯基或取代的苯基; Z是间隔基，T是载体部分。

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