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71. 发明授权

US4199571A Substituted anthracyclines, their preparation and use 失效
标题翻译：取代蒽环类，其制备和用途
公开(公告)号：US4199571A
公开(公告)日：1980-04-22
申请号：US941847
申请日：1978-09-13
申请人： Sergio Penco , Fausto Gozzi , Francesco Angelucci , Federico Arcamone
发明人： Sergio Penco , Fausto Gozzi , Francesco Angelucci , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07D303/32 , C07D319/08 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252 , C07D303/32 , C07D319/08 , Y10S514/908
摘要： Compounds having the formula: ##STR1## wherein (a) when R.sup.1 is --COCH.sub.3 or --COCH.sub.2 OH,R.sup.2 is --OH, R.sup.3 is --OCH.sub.3 and R.sup.4 is --H;(b) when R.sup.2 is --COCH.sub.3 or --COCH.sub.2 OH;R.sup.1 is --OH, R.sup.3 is --H and R.sup.4 is --OCH.sub.3 ;and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyl daunorubicin, a known compound.
摘要翻译：具有下式的化合物：其中（a）当R 1是-COCH 3或-COCH 2 OH时，R 2是-OH，R 3是-OCH 3，且R 4是-H; （b）当R 2为-COCH 3或-COCH 2 OH时; R1是-OH，R3是-H，R4是-OCH3; 并且其可用于治疗某些哺乳动物肿瘤，由已知化合物9,10-脱氢-N-三氟乙酰柔红霉素制备。

72. 发明授权

US4169142A Disaccharide analogs of antitumor anthracyclines, process for their preparation and use thereof 失效
标题翻译：抗癌蒽环类药物的二糖类似物，其制备方法和用途
公开(公告)号：US4169142A
公开(公告)日：1979-09-25
申请号：US851165
申请日：1977-11-14
申请人： Sergio Penco , Giuliano Franchi , Federico Arcamone
发明人： Sergio Penco , Giuliano Franchi , Federico Arcamone
IPC分类号： A61K31/65 , A61P35/00 , C07H15/252 , A61K31/70 , C07G11/00
CPC分类号： C07H15/252
摘要： Anthracycline disaccharides having antitumor activity are prepared by condensing N-trifluoroacetyldaunomycin with a 1-halosugar in the presence of a silver salt such as AgSO.sub.3 CF.sub.3 as catalyst to form a protected di-glycoside which upon mild alkaline hydrolysis yields the novel disaccharides.
摘要翻译：具有抗肿瘤活性的蒽环类二糖通过在银盐如AgSO 3 CF 3作为催化剂的存在下将N-三氟乙酰基青霉素与1-卤代糖缩合形成受保护的二糖苷，通过温和的碱水解产生新的二糖来制备。

73. 发明授权

US4112076A Epi-daunomycin and epi-adriamycin compounds and method of use 失效
标题翻译：依托霉素和表阿霉素化合物及其使用方法
公开(公告)号：US4112076A
公开(公告)日：1978-09-05
申请号：US675696
申请日：1976-04-09
申请人： Federico Arcamone , Alberto Bargiotti , Aurelio DI Marco , Sergio Penco
发明人： Federico Arcamone , Alberto Bargiotti , Aurelio DI Marco , Sergio Penco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , G04B37/00 , C07H15/24
CPC分类号： C07H15/252 , C07H5/06 , G04B37/0025 , Y02P20/55 , Y10S514/908
摘要： Disclosed is a process for preparing glycoside antitumor antibiotics, including the known compounds daunomycin, adriamycin, 4'-epi-daunomycin and 4'-epi-adriamycin and the novel antibiotics, 3',4'-epi-6'-hydroxydaunomycin, 3',4'-epi-6'-hydroxyadriamycin. 3',4'-epi-daunomycin, 3',4'-epi-adriamycin, 4-demethoxy-4'-epi-daunomycin and 4-demethoxy-4'-epi-adriamycin. Process involves reacting daunomycinone or 4-demethoxy-daunomycinone with a protected 1-halo derivative of 3,4-epi-6-hydroxydaunosamine, 3,4-epi-daunosamine or 4-epi-daunosamine in an inert solvent in the presence of a soluble silver salt catalyst to form a protected derivative of the glycoside antibiotic and removing the protecting groups.
摘要翻译：公开了一种制备糖苷抗肿瘤抗生素的方法，包括已知的化合物道诺霉素，阿霉素，4'-表柔比星霉素和4'-表阿霉素，以及新型抗生素3'，4'-表 - 6'-羟基天然霉素3 '，4'-表6-hydroxydriamycin。 3'，4'-表柔比星霉素，3'，4'-表阿霉素，4-脱甲氧基-4'-表柔比星霉素和4-脱甲氧基-4'-表阿霉素。方法包括使道诺霉素酮或4-脱甲氧基道诺霉素酮与3,4-外延-6-羟基丹酰胺，3,4-外延诺胺或4-外 - 柔红霉素的保护的1-卤代衍生物在惰性溶剂中，在可溶性银盐催化剂以形成糖苷抗生素的被保护的衍生物并除去保护基团。

74. 发明授权

US4058519A Adriamycins and uses thereof 失效
标题翻译：阿霉素及其用途
公开(公告)号：US4058519A
公开(公告)日：1977-11-15
申请号：US560104
申请日：1975-03-19
申请人： Federico Arcamone , Aurelio Di Marco , Sergio Penco
发明人： Federico Arcamone , Aurelio Di Marco , Sergio Penco
IPC分类号： C07H15/24 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252
CPC分类号： C07H15/252 , Y02P20/55 , Y10S514/908
摘要： The known antitumor antibiotic adriamycin and its .beta.-anomer, and the novel compounds, 4'-epiadriamycin (both .alpha.- and .beta.-anomers) are prepared by condensing a novel, reactive protected derivative of adriamycinone with reactive intermediates which are 1-halo-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-lyxo (or arabino) hexopyranoses.
摘要翻译：已知的抗肿瘤抗生素阿霉素及其β-对映体，以及新型化合物4'-表阿霉素（α-和β-共聚物两者）均通过将一种新型的反应性保护的阿霉素衍生物与1-卤代 - 2,3,6-三脱氧-3-三氟乙酰氨基-4-三氟乙酰氧基-α--L-赖克（或阿拉伯）六吡喃糖。

75. 发明授权

US5998426A 9,10 disubstituted camptothecin derivatives with antitumor activity 失效
标题翻译： 9,10具有抗肿瘤活性的二取代喜树碱衍生物
公开(公告)号：US5998426A
公开(公告)日：1999-12-07
申请号：US913855
申请日：1997-09-29
申请人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini , Sergio Penco
发明人： Angelo Bedeschi , Walter Cabri , Ilaria Candiani , Franco Zarini , Sergio Penco
IPC分类号： A61K31/47 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to 9-amino-10-(1-naphthylsulfonyloxy)-20(S)-camptothecin, 9-amino-10-phenylsulfonyloxy-20(S)-camptothecin, 7-ethyl-9-amino-10-(p-toluensulfonyloxy)-20(S)-camptothecin, their pharmaceutically acceptable salts, a process for their preparation, pharmaceutically compositions comprising them and their use as antitumor agents.
摘要翻译： PCT No.PCT / EP97 / 00194 Sec。 371日期：1997年9月29日 102（e）1997年9月29日PCT PCT 1997年1月11日PCT公布。出版物WO97 / 28164 日期：1997年8月7日本发明涉及9-氨基-10-（1-萘磺酰氧基）-20（S） - 喜树碱，9-氨基-10-苯基磺酰氧基-20（S） - 喜树碱，7-乙基-9- 氨基-10-（对甲苯磺酰氧基）-20（S） - 喜树碱，它们的药学上可接受的盐，其制备方法，包含它们的药物组合物及其作为抗肿瘤剂的用途。

76. 发明授权

US5856333A Substituted camptothecin derivatives and process for their preparation 失效
公开(公告)号：US5856333A
公开(公告)日：1999-01-05
申请号：US776192
申请日：1997-01-27
申请人： Walter Cabri , Ilaria Candiani , Angelo Bedeschi , Franco Zarini , Sergio Penco
发明人： Walter Cabri , Ilaria Candiani , Angelo Bedeschi , Franco Zarini , Sergio Penco
IPC分类号： A61K31/435 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to substituted camptothecin derivatives of formula (I) wherein the symbol - - - - represents a single or double bond; R.sub.1, R.sub.2 and R.sub.3 are as defined under (a) or (b) below: (a) R.sub.1 and R.sub.2 are, each independently, hydrogen; C.sub.1 -C.sub.4 alkyl; C.sub.3 -C.sub.7 cycloalkyl; phenyl C.sub.1 -C.sub.6 alkyl; an optionally substituted phenyl ring; --NR.sub.5 R.sub.6 wherein one of R.sub.5 and R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl or benzyl and the other is hydrogen, C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted benzoyl, phenyl C.sub.1 -C.sub.6 alkanoyl, an optionally substituted C.sub.1 -C.sub.6 alkoxycarbonyl, an optionally substituted phenoxycarbonyl or phenyl C.sub.1 -C.sub.6 alkoxycarbonyl, or R.sub.5 and R.sub.6, combined together with the nitrogen atom to which they are linked, form a 4-7 membered saturated, optionally substituted, heteromonocyclic ring residue; COOR.sub.8 wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; or COR.sub.9 wherein Rg is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, phenyl C.sub.1 -C.sub.6 alkyl, an optionally substituted phenyl ring or NR.sub.10 R.sub.11 wherein R.sub.10 and R.sub.11 are, each independently, hydrogen or C.sub.1 -C.sub.6 alkyl; and R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl or an optionally substituted phenyl ring; or (b) R.sub.1 and R.sub.3, combined together, form a 5-8 membered, optionally substituted, carbomonocyclic ring, and R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl or phenyl C.sub.1 -C.sub.6 alkyl; X is hydrogen,C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.6 alkanoyloxy, benzoyloxy, amino, hydroxy, nitro, halogen or it is a methylenedioxy group linked to the positions 10 and 11 of the molecule, and the pharmaceutically acceptable salts thereof. The compounds according to the invention are useful in therapy as antitumor agents. ##STR1##

77. 发明授权

US5801167A Camptothecin derivatives and process for their preparation 失效
标题翻译：喜树碱衍生物及其制备方法
公开(公告)号：US5801167A
公开(公告)日：1998-09-01
申请号：US697125
申请日：1996-08-20
申请人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
发明人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
IPC分类号： A61K31/47 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to new camptothecin derivatives which display antitumor activity. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.
摘要翻译：本发明涉及显示抗肿瘤活性的新的喜树碱衍生物。本发明还提供了它们的制备方法以及含有它们的药物组合物。

78. 发明授权

US5639884A Arylidene-heterocyclic derivatives and process for their preparation 失效
标题翻译：亚芳基杂环衍生物及其制备方法
公开(公告)号：US5639884A
公开(公告)日：1997-06-17
申请号：US400113
申请日：1995-03-06
申请人： Franco Buzzetti , Silvia Fustinoni , Maria Gabriella Brasca , Sergio Penco
发明人： Franco Buzzetti , Silvia Fustinoni , Maria Gabriella Brasca , Sergio Penco
IPC分类号： A61K31/425 , A61K31/428 , A61K31/47 , A61K31/472 , A61P35/00 , A61P43/00 , C07D217/24 , C07D275/06 , C07D401/06 , C07D417/06 , C12N9/99
CPC分类号： C07D275/06 , C07D217/24 , C07D401/06 , C07D417/06
摘要： The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar)R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.
摘要翻译：本发明涉及式（I）的化合物，其中Ar是选自苯，萘，四氢萘，喹啉和吲哚的单环或双环体系; Het是R 1是氢或C 1 -C 6烷基的氢，卤素，羟基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3; R 1是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3如上所定义; R2是氢，卤素，羟基或C1-C6烷基; 其中当（Ar）R 1 R 2基团同时表示未取代的苯基或4-氯 - ，4-氰基 - ，4-氨基 - 或3,4-二甲氧基 - 苯基且Het为 4-高邻苯二甲酰亚胺基，则R不是氢，它们可用作抗增殖剂。

79. 发明授权

US5602141A Camptothecin derivatives and process for their preparation 失效
标题翻译：喜树碱衍生物及其制备方法
公开(公告)号：US5602141A
公开(公告)日：1997-02-11
申请号：US389190
申请日：1995-02-15
申请人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
发明人： Angelo Bedeschi , Franco Zarini , Walter Cabri , Ilaria Candiani , Sergio Penco , Laura Capolongo
IPC分类号： A61K31/47 , A61P35/00 , C07D491/22
CPC分类号： C07D491/22
摘要： The present invention relates to new camptothecin derivatives of the formula (I) ##STR1## wherein B is a group B' or B" ##STR2## wherein each of (x) and (y) is a single or double bond. The present invention also provides processes for their preparation as well as pharmaceutical compositions containing the same.
摘要翻译：本发明涉及式（I）的新喜树碱衍生物，其中B是B'或B“”B'“B”，其中（x）和（y）各自为单键或双键。本发明还提供了它们的制备方法以及含有它们的药物组合物。

80. 发明授权

US5587385A Arylidene-heterocyclic derivatives and process for their preparation 失效
标题翻译：亚芳基杂环衍生物及其制备方法
公开(公告)号：US5587385A
公开(公告)日：1996-12-24
申请号：US452288
申请日：1995-05-26
申请人： Franco Buzzetti , Silvia Fustinoni , Maria G. Brasca , Sergio Penco
发明人： Franco Buzzetti , Silvia Fustinoni , Maria G. Brasca , Sergio Penco
IPC分类号： C07D217/24 , C07D275/06 , C07D401/06 , C07D417/06 , A61K31/47 , A61K31/475 , C07D401/08
CPC分类号： C07D275/06 , C07D217/24 , C07D401/06 , C07D417/06
摘要： The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.
摘要翻译：本发明涉及式（I）的化合物，其中Ar是选自苯，萘，四氢萘，喹啉和吲哚的单环或双环体系; Het是R 3是氢或C 1 -C 6烷基的氢，卤素，羟基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3; R 1是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3如上所定义; R2是氢，卤素，羟基或C1-C6烷基; 并且其中当同时（Ar）R 1 R 2基团表示未取代的苯基或4-氯 - ，4-氰基 - ，4-氨基 - 或3,4-二甲氧基 - 苯基且Het为 4-高邻苯二甲酰亚胺基，则R不是氢，其可用作抗增殖剂。

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