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21. 发明申请

US20080051567A1 Derivatives of partially desulphated glycosaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect 有权
标题翻译：部分脱硫的糖胺聚糖衍生物作为乙酰肝素酶抑制剂，具有抗血管生成活性，无抗凝作用
公开(公告)号：US20080051567A1
公开(公告)日：2008-02-28
申请号：US11882978
申请日：2007-08-08
申请人： Benito Casu , Giangiacomo Torri , Anna Naggi , Giuseppe Giannini , Claudio Pisano , Sergio Penco
发明人： Benito Casu , Giangiacomo Torri , Anna Naggi , Giuseppe Giannini , Claudio Pisano , Sergio Penco
IPC分类号： C08B37/10 , C07H5/04
CPC分类号： A61K31/727 , A61K31/737 , C07H5/04 , C08B37/0063
摘要： Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly a compound of formula (I) where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives have antiangiogenic and heparanase-inhibiting activity and are devoid of anticoagulant activity.
摘要翻译：描述了部分脱硫的糖胺聚糖衍生物，特别是肝素，更具体地，其中U，R和R 1个基团具有说明书中指出的含义的式（I）化合物。这些糖胺聚糖衍生物具有抗血管生成和乙酰肝素酶抑制活性，并且没有抗凝血活性。

22. 发明申请

US20070232639A1 Camptothecin Derivatives Conjugated in Position 20 with Integrin Antagonists 审中-公开
标题翻译：喜树碱衍生物与20位整合素拮抗剂共轭
公开(公告)号：US20070232639A1
公开(公告)日：2007-10-04
申请号：US11596189
申请日：2005-05-04
申请人： Claudio Pisano , Giuseppe Giannini , Maria Ornella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
发明人： Claudio Pisano , Giuseppe Giannini , Maria Ornella Tinti , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini , Franco Zunino
IPC分类号： A61K31/437 , A61K31/4375 , C07D405/14
CPC分类号： A61K47/64
摘要： Compounds or formula (I) are described, in which the R and R1 groups are as defined here below and include the condensation of the camptothecin molecule in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
摘要翻译：描述了化合物或式（I），其中R和R 1个基团如下文所定义，并且包括20位的喜树碱分子与含有RGD序列的环肽的缩合。所述化合物赋予对整联蛋白受体α和β5β5的高亲和力，并与在微摩尔浓度下对人肿瘤细胞系的选择性细胞毒活性。

23. 发明申请

US20070225311A1 7-T-Butoxyiminomethylcamptothecin Conjugated in Position 20 With Integrin Antagonists 失效
标题翻译： 7-T-Butoxyiminomethylcamptothecin缀合在20位与整合素拮抗剂
公开(公告)号：US20070225311A1
公开(公告)日：2007-09-27
申请号：US11596016
申请日：2005-04-28
申请人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini
发明人： Claudio Pisano , Giuseppe Giannini , Loredana Vesci , Domenico Alloatti , Sergio Penco , Alma Dal Pozzo , Ni Minghong , Sabrina Dallavalle , Lucio Merlini
IPC分类号： A61K31/435 , C07D405/14
CPC分类号： A61K47/64
摘要： Compounds of Formula (I) are described: in which the R1 group is as defined in the specification and includes the condensation of 7-t-butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors αvβ3 and αvβ5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
摘要翻译：描述了式（I）的化合物：其中R 1 H 1基团如说明书中所定义，并且包括位置20上的7-叔丁氧基亚氨基甲基喜树碱与含有RGD序列的环肽的缩合。所述化合物赋予对整联蛋白受体α和β5β5的高亲和力，并与在微摩尔浓度下对人肿瘤细胞系的选择性细胞毒活性。

24. 发明授权

US06887883B2 Use of natural chrysanthone compounds having antiangiogenic activity 失效
标题翻译：使用具有抗血管生成活性的天然菊花素化合物
公开(公告)号：US06887883B2
公开(公告)日：2005-05-03
申请号：US10220184
申请日：2001-03-12
申请人： Sergio Penco
发明人： Sergio Penco
IPC分类号： C07D221/08 , A61K31/352 , A61K31/473 , A61P9/00 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/04 , C07D311/92 , A61K31/44 , A61K31/35
CPC分类号： A61K31/352 , A61K31/473
摘要： A series of compounds of natural origin are described, as useful agents for the treatment of diseases characterised by abnormal angiogenesis. These compounds are: chrysanthone A having formula (I); chrysanthone B having formula (II); and chrysanthone C having formula (III).
摘要翻译：描述了一系列天然来源的化合物作为用于治疗以异常血管发生为特征的疾病的有用试剂。这些化合物是：具有式（I）的菊花A; 菊酯B具有式（II）; 和具有式（III）的菊花C。

25. 发明授权

US06589939B2 Camptothecin derivatives having antitumor activity 有权
标题翻译：喜树碱衍生物具有抗肿瘤活性
公开(公告)号：US06589939B2
公开(公告)日：2003-07-08
申请号：US09741818
申请日：2000-12-22
申请人： Sergio Penco , Lucio Merlini , Paolo Carminati , Franco Zunino
发明人： Sergio Penco , Lucio Merlini , Paolo Carminati , Franco Zunino
IPC分类号： A61K3170
CPC分类号： C07D491/22
摘要： Camptothecin derivatives of camptothecin of formula (I): wherein the groups R1, R2 and R3 are as defined in the description are disclosed. The compounds of formula (I) are endowed with antitumor activity and show a good therapeutic index. Processes for the preparation of the compounds of formula (I) and their use in the preparation of medicaments useful in the treatment of tumors, viral infections and antiplasmodium falciparum are also disclosed.
摘要翻译：式（I）的喜树碱喜树碱衍生物：其中基团R 1，R 2和R 3如说明书中所定义。式（I）化合物具有抗肿瘤活性并具有良好的治疗指标。制备方法的式（I）化合物及其在制备用于治疗肿瘤，病毒感染和恶性疟原虫的药物中的用途。

26. 发明授权

US5138042A 6-deoxyanthracyclines 失效
标题翻译： 6-脱氧蒽环类
公开(公告)号：US5138042A
公开(公告)日：1992-08-11
申请号：US501870
申请日：1990-03-28
申请人： Francesco Angelucci , Sergio Penco , Ermes Vanotti , Federico Arcamone
发明人： Francesco Angelucci , Sergio Penco , Ermes Vanotti , Federico Arcamone
IPC分类号： C07C50/38 , C07D407/04 , C07H15/252
CPC分类号： C07D407/04 , C07C50/38 , C07H15/252
摘要： Anthracycline glycosides useful as antitumor agents of formula XV: ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group.
摘要翻译：可用作式XV抗肿瘤剂的蒽环糖苷：其中R1表示氢原子或羟基，R2和R3之一表示氢原子，R2和R3中的另一个表示氢原子或羟基， X是氢原子或三氟乙酰基。

27. 发明授权

US4766142A Poly-4-aminopyrrole-2-carboxamido derivatives and their use as antiuiral or antitumor agents 失效
标题翻译：聚-4-氨基吡咯-2-甲酰胺衍生物及其作为抗病毒或抗肿瘤剂的用途
公开(公告)号：US4766142A
公开(公告)日：1988-08-23
申请号：US783588
申请日：1985-10-03
申请人： Federico Arcamone , Nicola Mongelli , Sergio Penco
发明人： Federico Arcamone , Nicola Mongelli , Sergio Penco
IPC分类号： C07D207/34 , C07D403/14 , C07D405/14 , C07D413/14 , C07H15/26 , A61K31/40 , C07D403/12
CPC分类号： C07D403/14 , C07D207/34 , C07D405/14 , C07D413/14 , C07H15/26
摘要： Compound of the formula (I) ##STR1## wherein n is zero or an integer of 1 to 3;R is(a) --NHR.sub.3, wherein R.sub.3 is(a') --CON(NO)R.sub.4, in which R.sub.4 is C.sub.1 -C.sub.4 alkyl either unsubstituted or substituted by halogen; or(b') --CO(CH.sub.2).sub.m --R.sub.5, in which R.sub.5 is halogen, oxiranyl, methyloxiranyl, aziridinyl, a group ##STR2## or a group ##STR3## and m is zero or an integer of 1 to 4; or (b) ##STR4## wherein either R.sub.6 and R.sub.7 are the same and are each oxiranemethyl, aziridinemethyl, or C.sub.2 -C.sub.4 alkyl 2-substituted by halogen or by a group --OSO.sub.2 R.sub.8 wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl or phenyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is as defined above;each group R.sub.1 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group terminating with (i) a basic moiety chosen from an amino group, a mono- or di- C.sub.1 -C.sub.6 alkylamino group, an amidino group, a group ##STR5## imidazolyl, imidazolinyl, tetrahydropyrimidinyl and oxazolidinyl; or (ii) a carboxy group; or (iii) a free hydroxy group --OH or a glycosilated hydroxy group --OD wherein D is a glucose, mannose or ribose sugar residue or the daunosamine amino-sugar residue; with the proviso that n is different from one when R.sub.2 is ##STR6## and the pharmaceutically acceptable salts thereof. The compounds are useful as antiviral and antitumor agents.
摘要翻译：式（I）的化合物其中n为0或1〜3的整数; R是（a）-NHR 3，其中R 3是（a'）-CON（NO）R 4，其中R 4是未被取代或被卤素取代的C 1 -C 4烷基; 或（b'）-CO（CH 2）m -R 5，其中R 5为卤素，环氧乙烷基，甲基环氧乙烷基，氮丙啶基，基团或基团，并且m为0或1至4的整数; 或（b）其中R 6和R 7相同并且各自是环氧乙烷基，氮丙啶甲基或被卤素取代的C 2 -C 4烷基或基团-OSO 2 R 8，其中R 8是C 1 -C 4烷基或苯基，或一个 R6和R7是氢，另一个如上所定义; 每个基团R 1独立地是氢或C 1 -C 4烷基; R2是C1-C6烷基，其终止于（i）选自氨基，单或二C1-C6烷基氨基，脒基，基团咪唑基，咪唑啉基，四氢嘧啶基和恶唑烷基的碱性部分 ; 或（ii）羧基; 或（iii）游离羟基-OH或糖基化羟基-OD，其中D是葡萄糖，甘露糖或核糖糖残基或达诺明胺氨基糖残基; 条件是当R 2不为1时，n不同于其药学上可接受的盐。该化合物可用作抗病毒和抗肿瘤剂。

28. 发明授权

US4366149A Antitumor anthracycline glycosides, their preparation, intermediates therefor, and compositions and use thereof 失效
标题翻译：抗癌蒽环类苷，其制备方法，其中间体及其组合物和用途
公开(公告)号：US4366149A
公开(公告)日：1982-12-28
申请号：US316057
申请日：1981-10-29
申请人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
发明人： Alberto Bargiotti , Giuseppe Cassinelli , Sergio Penco , Federico Arcamone , Annamaria Casazza
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H13/04 , C07H15/04 , C07H15/252 , C07H5/06 , C07H15/24
CPC分类号： C07H13/04 , C07H15/04 , C07H15/252 , Y10S514/908
摘要： Novel antitumor anthracycline glycosides are prepared by condensing daunomycinone with 2,3,4,6-tetradeoxy-3,4-ditrifluoroacetamido-L-lyxo-[or L-arabino-]hexopyranosyl chloride.
摘要翻译：通过将道诺霉素酮与2,3,4,6-四脱氧-3,4-二三氟乙酰氨基-L-赖氨酸 - 或[L-阿拉伯糖]六吡喃葡萄糖氯化物缩合来制备新型抗肿瘤蒽环苷。

29. 发明授权

US4345070A Process for the preparation of 4'-deoxy-daunorubicin and 4'-deoxy-doxorubicin 失效
标题翻译： 4'-脱氧柔红霉素和4'-脱氧多柔比星的制备方法
公开(公告)号：US4345070A
公开(公告)日：1982-08-17
申请号：US270877
申请日：1981-06-05
申请人： Antonino Suarato , Sergio Penco , Federico Arcamone
发明人： Antonino Suarato , Sergio Penco , Federico Arcamone
IPC分类号： C07D309/14 , A61K31/65 , C07H15/252 , C07H15/24
CPC分类号： C07H15/252
摘要： A new process for the preparation of the known 4'-deoxydaunorubicin and 4'-deoxydoxorubicin is disclosed. The used starting material is 4'-eip-N-trifluoroacetyldaunorubicin which is converted into 4'-deoxy-4'-iodo-N-trifluoroacetyl-daunorubicin from which 4'-deoxy-daunorubicin can be reductively obtained and eventually transformed, by known methods, into 4'-deoxy-doxorubicin.
摘要翻译：公开了一种制备已知的4'-脱氧柔红霉素和4'-脱氧阿霉素的新方法。所使用的原料是4'-eip-N-三氟乙酰基柔红霉素，其被转化为4'-脱氧-4'-碘-N-三氟乙酰基柔红霉素，从其中可以还原获得4'-脱氧柔红霉素并最终通过已知的方法，进入4'-脱氧 - 多柔比星。

30. 发明授权

US4218440A Antitumordeoxy-anthracyclines and use thereof 失效
标题翻译：抗过氧 - 蒽环类抗生素及其用途
公开(公告)号：US4218440A
公开(公告)日：1980-08-19
申请号：US941920
申请日：1978-09-13
申请人： Sergio Penco , Giuliano Franchi , Federico Arcamone
发明人： Sergio Penco , Giuliano Franchi , Federico Arcamone
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P35/00 , C07H15/252 , A61K31/71 , C07H15/24
CPC分类号： C07H15/252
摘要： Compounds having the formula: ##STR1## wherein R is H or OH, and which are useful in treating certain mammalian tumors, are prepared from 9,10-anhydro-N-trifluoroacetyldaunorubicin, a known compound.
摘要翻译：具有下式的化合物：其中R是H或OH，可用于治疗某些哺乳动物肿瘤的化合物由已知化合物9,10-脱氢-N-三氟乙酰基柔红霉素制备。

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