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公开(公告)号：US06593303B1
公开(公告)日：2003-07-15
申请号：US09926055
申请日：2001-08-22
IPC分类号： A01N4304
CPC分类号： A61K31/704 , A61K31/335 , A61K31/555 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： There are provided the combined use of 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4′-methansulfonyl daunorubicin and an anti-neoplastic anti-mitotic compound and/or a platinum derivative in the treatment of tumors, as well as in the prevention or treatment of metastasis or in the treatment of tumors by inhibition of angiogenesis.
摘要翻译： 提供了4-脱甲氧基-3'-脱氨基-3'-吖啶基-4'-甲磺酰基柔红霉素或4-脱甲氧基-N，N-双（2-氯乙基）-4'-甲磺酰基柔红霉素和抗 - - 肿瘤抗有丝分裂化合物和/或铂衍生物用于治疗肿瘤，以及通过抑制血管发生来预防或治疗转移瘤或治疗肿瘤。
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2.发明授权Combined preparations comprising morpholine anthracyclines and anticancer agent 失效包含吗啉蒽环类抗生素和抗癌剂的组合制剂公开(公告)号：US06586428B2
公开(公告)日：2003-07-01
申请号：US10284144
申请日：2002-10-31
IPC分类号： A61K315377
CPC分类号： A61K45/06 , A61K31/675 , A61K31/70 , A61K2300/00
摘要： The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inihbitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.
摘要翻译： 本发明涉及一种组合制剂，其包含与选自烷基化剂，抗代谢物，拓扑异构酶II抑制剂，拓扑异构酶I抑制剂，抗有丝分裂药物和铂衍生物的组合抗癌剂中的吗啉基蒽环类药物，其是有用的抗癌治疗，特别是 在治疗原发性或转移性肝癌中。
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3.发明授权Combined preparations comprising morpholine anthracyclines and anticancer agent 失效包含吗啉蒽环类抗生素和抗癌剂的组合制剂公开(公告)号：US06537990B1
公开(公告)日：2003-03-25
申请号：US09926392
申请日：2001-10-25
IPC分类号： A61K315377
CPC分类号： A61K45/06 , A61K31/675 , A61K31/70 , A61K2300/00
摘要： The present invention relates to combined preparations comprising a morpholinyl anthracycline administered in combination anticancer agents chosen from an alkylating agent, an antimetabolite, a topoisomerase II inhibitor, a topoisomerase I inhibitor, an antimitotic drug and a platinum derivative, which are useful anticancer therapy, particularly in the treatment of a primary or metastatic liver cancer.
摘要翻译： 本发明涉及包含作为有用的抗癌治疗的选自烷化剂，抗代谢药物，拓扑异构酶II抑制剂，拓扑异构酶I抑制剂，抗有丝分裂药物和铂衍生物的组合抗癌剂中的吗啉基蒽环霉素的组合制剂，特别是 在治疗原发性或转移性肝癌中。
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4.发明授权Antitumor composition containing a synergistic combination of an anthracycline derivative with a camptothecin derivate 失效含有蒽环类衍生物与喜树碱衍生物的协同组合的抗肿瘤组合物公开(公告)号：US06403563B1
公开(公告)日：2002-06-11
申请号：US09646096
申请日：2000-09-20
IPC分类号： A61K3170
CPC分类号： A61K31/704 , A61K31/47 , A61K31/70 , A61K45/06 , A61K2300/00
摘要： The combination of 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin or 4-demethoxy-N,N-bis(2-chloroethyl)-4′-methansulfonyl daunorubicin together with an antineoplastic topoisomerase I inhibitor yields preparations exhibiting anti-cancer effects. These preparations can be used in the treatment of tumors and especially 4-demethoxy-3′-deamino-3′-aziridinyl-4′-methansulfonyl daunorubicin in the treatment of brain tumors.
摘要翻译： 4-脱甲氧基-3'-脱氨基-3'-氮杂环丙烷基-4'-甲磺酰基柔红霉素或4-脱甲氧基-N，N-双（2-氯乙基）-4'-甲磺酰基柔红霉素与抗肿瘤拓扑异构酶I抑制剂的组合 产生具有抗癌作用的制剂。 这些制剂可用于治疗肿瘤，特别是4-脱甲氧基-3'-脱氨基-3'-吖丙啶基-4'-甲磺酰柔红霉素治疗脑肿瘤。
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公开(公告)号：US06258786B1
公开(公告)日：2001-07-10
申请号：US09445443
申请日：1999-12-13
IPC分类号： A61K3170
CPC分类号： C07H15/252
摘要： The present invention relates to anthracycline glycosides, to a process for their preparation and to pharmaceutical compositions containing the same.
摘要翻译： 本发明涉及蒽环类苷，其制备方法和含有它们的药物组合物。
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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。
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公开(公告)号：US5532218A
公开(公告)日：1996-07-02
申请号：US345450
申请日：1994-11-21
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。
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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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