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1. 发明授权

US5532218A 3'-aziridino-anthracycline derivatives 失效
标题翻译： 3'-氮丙啶基 - 蒽环类衍生物
公开(公告)号：US5532218A
公开(公告)日：1996-07-02
申请号：US345450
申请日：1994-11-21
申请人： Alberto Bargiotti , Michele Caruso , Maria Grandi , Marina Ripamonti , Antonino Suarato
发明人： Alberto Bargiotti , Michele Caruso , Maria Grandi , Marina Ripamonti , Antonino Suarato
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , C07H17/02 , C07H15/24
CPC分类号： C07H15/252 , C07H17/02
摘要： Anthracycline glycosides of general formula 1 and 2: ##STR1## wherein R.sub.1 is hydrogen or a methoxy group; R.sub.2 is hydrogen, a hydroxy group or represents an acyloxy residue of formula 3 --O--COR.sub.5 wherein R.sub.5 is a linear or branched C.sub.1 -C.sub.8 alkyl, an aryl group or a heterocyclic mono or bicyclic ring, each of which may be unsubstituted or substituted with (a) an amino group NR.sub.6 R.sub.7 in which R.sub.6 and R.sub.7 are independently hydrogen or C.sub.1 -C.sub.4 alkyl or (b) a carboxy group; R.sub.3 and R.sub.4 both represent hydrogen or one of R.sub.3 and R.sub.4 is hydrogen and the other is hydroxy group or a group of formula --OSO.sub.2 R.sub.8 in which R.sub.8 may be a linear or branched alkyl group containing from 1 to 6 carbon atoms or an aryl group unsubstituted or substituted by 1 to 3 substituents each of which may independently be a linear or branched alkyl or alkoxy group of from 1 to 6 carbon atoms, a halogen atom or a nitro group; and pharmaceutically acceptable salts thereof; are active as antitumor agents.
摘要翻译：通式1和2的蒽环酸苷：其中R 1是氢或甲氧基; R2是氢，羟基或代表式3-COR5的酰氧基残基，其中R5是直链或支链C1-C8烷基，芳基或杂环单环或双环，其各自可以是未取代或取代的与（a）氨基NR 6 R 7，其中R 6和R 7独立地是氢或C 1 -C 4烷基或（b）羧基; R 3和R 4均代表氢或R 3和R 4之一是氢，另一个是羟基或式-OSO 2 R 8基团，其中R 8可以是含有1至6个碳原子的直链或支链烷基或未取代的芳基或被1〜3个取代基取代，各自可以独立地为具有1-6个碳原子的直链或支链烷基或烷氧基，卤素原子或硝基; 及其药学上可接受的盐; 作为抗肿瘤剂有活性。

2. 发明授权

US4684629A 3'-deamino-3'-hydroxy-4'-deoxy-4'-amino doxorubicin and related daunorubicin 失效
标题翻译： 3'-脱氨基-3'-羟基-4'-脱氧-4'-氨基多柔比星及相关的柔红霉素
公开(公告)号：US4684629A
公开(公告)日：1987-08-04
申请号：US843264
申请日：1986-03-24
申请人： Alberto Bargiotti , Michele Caruso , Antonino Suarato , Sergio Penco , Fernando Giuliani
发明人： Alberto Bargiotti , Michele Caruso , Antonino Suarato , Sergio Penco , Fernando Giuliani
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , A61P35/00 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of general formula (I) ##STR1## wherein R is hydrogen or hydroxy, and pharmaceutically acceptable salts thereof, are anti-tumor agents.
摘要翻译：通式（I）的蒽环酸苷是抗肿瘤剂，其中R是氢或羟基，及其药学上可接受的盐。

3. 发明授权

US5496808A Mono and bis alkylamino-anthracyclines 失效
标题翻译：单和双烷基氨基蒽环类
公开(公告)号：US5496808A
公开(公告)日：1996-03-05
申请号：US904650
申请日：1992-06-26
申请人： Alberto Bargiotti , Michele Caruso , Daniela Faiardi , Antonino Suarato , Nicola Mongelli
发明人： Alberto Bargiotti , Michele Caruso , Daniela Faiardi , Antonino Suarato , Nicola Mongelli
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H20060101 , C07H15/252 , C07H15/24
CPC分类号： A61K31/70 , C07H15/252
摘要： An anthracycline glycoside of general formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy group, A and B both represent hydrogen or one of A and B is hydrogen and the other is hydroxy or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is C1-C4 alkyl or aryl optionally substituted by C1-C4 alkyl, nitro, amino, methoxy or halogen; R.sub.3 is a hydrogen atom or a group of formula 2 and R.sub.4 is a group of formula 2--(CH.sub.2).sub.n --X 2in which n is 2 or 3 and X is hydroxy group, a halogen or a group of formula --OSO.sub.2 R.sub.5 in which R.sub.5 is as defined above and with the proviso that if R.sub.2, X and A are an hydroxy group and R.sub.3 .dbd.H, n must be 3; or a pharmaceutically acceptable salt thereof.Compounds of the invention have activity as antitumor agents. Processes for their preparation and pharmaceutical composition containing them are also disclosed.
摘要翻译：通式1的蒽环类苷：oup; R2是氢或羟基，A和B都代表氢或A和B之一是氢，另一个是羟基或式-OSO 2 R 5基团，其中R 5是任选被C 1 -C 4烷基取代的C 1 -C 4烷基或芳基，硝基，氨基，甲氧基或卤素; R3是氢原子或式2的基团，R4是式2 - （CH2）nX2的基团，其中n是2或3，X是羟基，卤素或式-OSO2R5基团，其中R5 条件是如果R2，X和A是羟基，R3 = H，则n必须为3; 或其药学上可接受的盐。本发明的化合物具有作为抗肿瘤剂的活性。还公开了其制备方法和含有它们的药物组合物。

4. 发明授权

US5045534A 4-demethoxy-4'-amino-4'-deoxy-anthracycline derivatives 失效
标题翻译： 4-脱甲氧基-4'-氨基-4'-脱氧蒽环衍生物
公开(公告)号：US5045534A
公开(公告)日：1991-09-03
申请号：US501800
申请日：1990-03-30
申请人： Alberto Bargiotti , Maria Grandi , Antonino Suarato , Fernando Giuliani
发明人： Alberto Bargiotti , Maria Grandi , Antonino Suarato , Fernando Giuliani
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252
CPC分类号： C07H15/252
摘要： Antitumour anthracycline glycosides of formula I: ##STR1## wherein R.sub.1 is hydrogen or a hydroxyl group, and pharmaceutically acceptable acid addition salts thereof.
摘要翻译：式I的抗肿瘤蒽环酸苷：其中R 1是氢或羟基，及其药学上可接受的酸加成盐。

5. 发明授权

US5744454A Anthracycline derivatives 失效
标题翻译：蒽环类衍生物
公开(公告)号：US5744454A
公开(公告)日：1998-04-28
申请号：US635957
申请日：1996-05-06
申请人： Antonino Suarato , Michele Caruso , Alberto Bargiotti , Dario Ballinari , Jacqueline Lansen
发明人： Antonino Suarato , Michele Caruso , Alberto Bargiotti , Dario Ballinari , Jacqueline Lansen
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61P25/00 , A61P25/28 , C07H15/252 , C07H17/02 , C07H15/24
CPC分类号： A61K31/704 , C07H15/252
摘要： The present invention provides the new use in the manufacture of a medicament for use in the treatment of amyloidosis of an anthracycline of formula A: wherein R1, R2, R3 and X are appropriate substituents. Novel compounds of the formula A, processes for their production and pharmaceutical compositions containing them are also described.
摘要翻译： PCT No.PCT / EP95 / 03480第 371日期：1996年5月6日 102（e）日期1996年5月6日PCT提交1995年9月5日PCT公布。公开号WO96 / 07665 日期：1996年3月14日本发明提供了用于制备用于治疗式A的蒽环霉素的淀粉样变性的药物的新用途：其中R1，R2，R3和X是适当的取代基。还描述了式A的新型化合物，其制备方法和含有它们的药物组合物。

6. 发明授权

US5304687A Morpholinyl derivatives of doxorubicin and process for their preparation 失效
标题翻译：多柔比星的吗啉基衍生物及其制备方法
公开(公告)号：US5304687A
公开(公告)日：1994-04-19
申请号：US3684
申请日：1993-01-13
申请人： Alberto Bargiotti , Maria Grandi , Antonino Suarato , Daniela Faiardi
发明人： Alberto Bargiotti , Maria Grandi , Antonino Suarato , Daniela Faiardi
IPC分类号： C07C43/313 , C07H15/252 , C07C43/30
CPC分类号： C07H15/252 , C07C43/313
摘要： Morpholinyl derivatives of doxorubicin having the general formula A: ##STR1## in which X represents a linear or branched C.sub.2 -C.sub.6 alkyl group or a benzyl group --CH.sub.2 C.sub.6 H.sub.5 and which have (S) or (R) configuration at carbon atom C-2" of the morpholino ring, are antitumor agents.
摘要翻译：具有通式A的阿霉素的吗啉基衍生物：其中X表示直链或支链的C 2 -C 6烷基或苄基-CH 2 C 6 H 5，并且在碳原子C 2具有（S）或（R）构型） “吗啉环”是抗肿瘤剂。

7. 发明授权

US4987126A 3'-deamino-4'-deoxy-4'-amino anthracyclines 失效
标题翻译： 3'-脱氨基-4'-脱氧-4'-氨基蒽环类
公开(公告)号：US4987126A
公开(公告)日：1991-01-22
申请号：US308449
申请日：1989-02-10
申请人： Alberto Bargiotti , Antonino Suarato , Pierangelo Zini , Maria Grandi , Gabriella Pezzoni
发明人： Alberto Bargiotti , Antonino Suarato , Pierangelo Zini , Maria Grandi , Gabriella Pezzoni
IPC分类号： A61K31/65 , A61P35/00 , C07D309/10 , C07D309/14 , C07H15/252
CPC分类号： C07H15/252 , C07D309/10 , C07D309/14
摘要： Anthracycline glycoside compounds of general formula I or II: ##STR1## wherein R.sub.1 is hydrogen or a hydroxy group and R.sub.2 is hydrogen or a methoxy group, and their pharmaceutically acceptable acid addition salts, are antitumor agents.

8. 发明授权

US5510469A 2-acyloxy-4-morpholinyl anthracyclines 失效
标题翻译： 2-酰氧基-4-吗啉基蒽环类
公开(公告)号：US5510469A
公开(公告)日：1996-04-23
申请号：US987281
申请日：1993-05-12
申请人： Daniela Faiardi , Alberto Bargiotti , Antonino Suarato
发明人： Daniela Faiardi , Alberto Bargiotti , Antonino Suarato
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61P35/00 , C07H15/252 , C07H19/24 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of formula 1: ##STR1## wherein R.sub.1 is hydrogen or methoxy group; R.sub.2 is hydrogen or hydroxy; both R.sub.3 and R.sub.4 represent hydrogen or one of R.sub.3 and R.sub.4 is hydroxy and the other of R.sub.3 and R.sub.4 a represents hydrogen; R.sub.5 represents hydrogen atom or an acyl residue--COX in which X is a C.sub.1 -C.sub.8 linear or branched alkyl chain, an aryl, an aryl lower alkyl, or a 5- or 6-membered heteroaromatic group are anti-tumour agents.
摘要翻译： PCT No.PCT / EP91 / 01506 Sec。 371日期：1993年5月12日 102（e）日期1993年5月12日PCT 1991年8月8日PCT PCT。出版物WO92 / 04362 1992年3月19日。式1的蒽环糖苷：其中R1是氢或甲氧基; R2是氢或羟基; R3和R4分别代表氢或R3和R4之一是羟基，R3和R4中的另一个代表氢; R5表示氢原子或其中X为C1-C8直链或支链烷基链，芳基，芳基低级烷基或5或6元杂芳族基团的酰基残基-COX为抗肿瘤剂。

9. 发明授权

US5412081A New 4'-epi-4'-amino anthracyclines 失效
标题翻译：新的4'-epi-4'-氨基蒽环类
公开(公告)号：US5412081A
公开(公告)日：1995-05-02
申请号：US1229
申请日：1993-01-06
申请人： Francesco Angelucci , Alberto Bargiotti , Daniela Faiardi , Stefania Stefanelli , Antonino Suarato
发明人： Francesco Angelucci , Alberto Bargiotti , Daniela Faiardi , Stefania Stefanelli , Antonino Suarato
IPC分类号： C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides having the general formula 1 and 2: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, fluorine, hydroxy or amino; R.sub.2 and R.sub.3 represent hydroxy or one of R.sub.2 and R.sub.3 is a hydrogen atom, a nitro or an amino group and the other of R.sub.2 and R.sub.3 is a HYDROXY group, exhibit activity against LoVo and LoVo/Dx in vitro.
摘要翻译：具有通式1和2的蒽环酸苷：其中R 1选自氢，氟，羟基或氨基; R2和R3代表羟基或R2和R3之一是氢原子，硝基或氨基，R2和R3中的另一个是羟基，体外表现出对LoVo和LoVo / Dx的活性。

10. 发明授权

US4672057A Morpholino derivatives of daunorubicin and doxorubicin 失效
标题翻译：柔红霉素和多柔比星的吗啉衍生物
公开(公告)号：US4672057A
公开(公告)日：1987-06-09
申请号：US839936
申请日：1986-03-17
申请人： Alberto Bargiotti , Pierangelo Zini , Sergio Penco , Fernando Giuliani
发明人： Alberto Bargiotti , Pierangelo Zini , Sergio Penco , Fernando Giuliani
IPC分类号： C07H19/24 , A61K31/535 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61P35/00 , A61P35/02 , C07D413/04 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： Anthracycline glycosides of the general formula (A): ##STR1## wherein X is hydrogen or hydroxy and R is hydrogen or a methyl or a hydroxymethyl group; and their pharmaceutically acceptable salts; are useful as antitumor agents.
摘要翻译：通式（A）的蒽环酸苷：其中X是氢或羟基，R是氢或甲基或羟甲基; 及其药学上可接受的盐; 作为抗肿瘤剂有用。

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