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。

公开(公告)号：US07612081B2

公开(公告)日：2009-11-03

申请号：US10564637

申请日：2004-07-06

申请人： Giuseppe Giannini ,  Claudio Pisano ,  Loredana Vesci ,  Maria Ornella Tinti ,  Lucio Merlini ,  Sergio Penco ,  Franco Zunino

发明人： Giuseppe Giannini ,  Claudio Pisano ,  Loredana Vesci ,  Maria Ornella Tinti ,  Lucio Merlini ,  Sergio Penco ,  Franco Zunino

IPC分类号： A61K31/4745 ,  C07D491/22

CPC分类号： C07D491/22 ,  Y02P20/55

摘要： Compounds are disclosed with the general formula in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime residue, such amine groups being in turn protected by suitable protective groups. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicaments for the treatment of tumors and viral and parasite infections.

摘要翻译： 公开了具有通式的化合物，其中基团如下文描述中所定义，并且其特征在于亚胺/肟残基上存在多胺取代基，此类胺基又被合适的保护基保护。 所述化合物具有有效的拓扑异构酶I抑制活性，因此可用作治疗肿瘤和病毒和寄生虫感染的药物。

公开(公告)号：US07351714B2

公开(公告)日：2008-04-01

申请号：US10546211

申请日：2004-03-10

申请人： Sabrina Dallavalle ,  Sergio Penco ,  Claudio Pisano ,  Franco Zunino

发明人： Sabrina Dallavalle ,  Sergio Penco ,  Claudio Pisano ,  Franco Zunino

IPC分类号： A61K31/4745 ,  C07D491/22

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： 公开了式（I）的喜树碱喜树碱衍生物，其中基团R 1，R 2和R 3 3如说明书中所定义。 式（I）化合物具有抗肿瘤活性，显示出良好的治疗指标。 还公开了制备式（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药物中的用途的方法。

公开(公告)号：US20070043067A1

公开(公告)日：2007-02-22

申请号：US10564637

申请日：2004-07-06

申请人： Giuseppe Giannini ,  Claudio Pisano ,  Loredana Vesci ,  Maria Omella Tinti ,  Lucio Merlini ,  Sergio Penco ,  Franco Zunino

发明人： Giuseppe Giannini ,  Claudio Pisano ,  Loredana Vesci ,  Maria Omella Tinti ,  Lucio Merlini ,  Sergio Penco ,  Franco Zunino

IPC分类号： A61K31/4745 ,  C07D491/14

CPC分类号： C07D491/22 ,  Y02P20/55

摘要： Compounds are disclosed with the general formula in which the groups are as defined in the description here below and characterized by the presence of polyamine substituents on the imine/oxime residue, such amine groups being in turn protected by suitable protective groups. Said compounds are endowed with potent topoisomerase I inhibiting activity and therefore are useful as medicaments for the treatment of tumours and viral and parasite infections.

摘要翻译： 公开了具有通式的化合物，其中基团如下文描述中所定义，并且其特征在于亚胺/肟残基上存在多胺取代基，此类胺基又被合适的保护基保护。 所述化合物具有有效的拓扑异构酶I抑制活性，因此可用作治疗肿瘤和病毒和寄生虫感染的药物。

公开(公告)号：US20060172968A1

公开(公告)日：2006-08-03

申请号：US11314736

申请日：2005-12-22

申请人： Benito Casu ,  Giangiacomo Torri ,  Anna Maria Naggi ,  Giuseppe Giannini ,  Claudio Pisano ,  Sergio Penco

发明人： Benito Casu ,  Giangiacomo Torri ,  Anna Maria Naggi ,  Giuseppe Giannini ,  Claudio Pisano ,  Sergio Penco

IPC分类号： A61K31/727 ,  A61K31/737

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。

公开(公告)号：US20060167033A1

公开(公告)日：2006-07-27

申请号：US10546211

申请日：2004-03-10

申请人： Sabrina Dallavalle ,  Sergio Penco ,  Claudio Pisano ,  Franco Zunino

发明人： Sabrina Dallavalle ,  Sergio Penco ,  Claudio Pisano ,  Franco Zunino

IPC分类号： A61K31/4745 ,  C07D519/04

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： 公开了式（I）的喜树碱喜树碱衍生物，其中基团R 1，R 2和R 3 3如说明书中所定义。 式（I）化合物具有抗肿瘤活性，显示出良好的治疗指标。 还公开了制备式（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药物中的用途的方法。

公开(公告)号：US06566552B2

公开(公告)日：2003-05-20

申请号：US09849363

申请日：2001-05-07

申请人： Maria Ornella Tinti ,  Oreste Piccolo ,  Fausto Bonifacio ,  Cristina Crescenzi ,  Sergio Penco

发明人： Maria Ornella Tinti ,  Oreste Piccolo ,  Fausto Bonifacio ,  Cristina Crescenzi ,  Sergio Penco

IPC分类号： C07C22900

CPC分类号： C07C227/32 ,  C07C67/31 ,  C07C69/675 ,  C07C229/22

摘要： The present invention describes a process for the industrial production of L-carnitine, comprising the enantioselective reduction of an alkyl 4-chloro-3-oxobutyrate or 4-chloro-3-oxobutyramide. The optically active 3-hydroxy derivative thus obtained is reacted with trimethylamine, obtaining crude L-carnitine, which is then finally purified. The catalyst used for the reduction is a complex of ruthenium bound to a penta-atomic bis-heteroaromatic system. The reduction reaction, performed in controlled conditions of hydrogen pressure, substrate concentration, temperature, and substrate: catalyst molar ratio, enables 4-chloro-3-hydoxybutyrate or 4-chloro-hydroxybutyamide to be obtained in a high yield. The process described, which leads to L-carnitine being obtained, is easily applicable on an industrial scale.

公开(公告)号：US06242457B1

公开(公告)日：2001-06-05

申请号：US09507928

申请日：2000-02-22

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： A61K314761

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： 公开了式（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。 还公开了式（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药物中的用途。

公开(公告)号：US6130227A

公开(公告)日：2000-10-10

申请号：US125512

申请日：1998-08-20

申请人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

发明人： Lucio Merlini ,  Sergio Penco ,  Franco Zunino

IPC分类号： A61K31/00 ,  A61K31/435 ,  A61K31/47 ,  A61K31/4738 ,  A61K31/4745 ,  A61P35/00 ,  A61P43/00 ,  C07D209/00 ,  C07D221/00 ,  C07D311/00 ,  C07D491/22 ,  A61K31/4761 ,  C07D471/14 ,  C07D471/16

CPC分类号： C07D491/22

摘要： 20S-Camptothecin derivatives in which the 7-position bears as a substituent --CN, --CH(CN)R.sub.4, --CH.dbd.C(CN)R.sub.4, --C(.dbd.NOH)NH.sub.2, --C(.dbd.NH)NH.sub.2, --CH.dbd.C(NO.sub.2)R.sub.4, --CH(CN)R.sub.5, --CH(CH.sub.2 NO.sub.2)R.sub.5, tetrazol-5-yl, 4,5-dihydrooxazol-2-yl, or 1,2,4-oxadiazolin-3-yl-5-one. These compounds are active as topoisomerase I inhibitors, and can be used as antitumor drugs.

摘要翻译： PCT No.PCT / EP97 / 00786 Sec。 371日期：1998年8月20日 102（e）1998年8月20日PCT PCT 1997年2月19日PCT公布。 WO97 / 31003 PCT出版物 日期：1997年8月28日20 S- 7-位被作为取代基的喜树碱衍生物-CN，-CH（CN）R4，-CH = C（CN）R4，-C（= NOH）NH2，-C（= NH）NH2，-CH = C（NO2）R4，-CH（CN）R5，-CH（CH2NO2）R5，四唑-5-基，4,5-二氢恶唑-2-基或1,2,4- 恶二唑啉-3-基-5-酮。 这些化合物作为拓扑异构酶I抑制剂是有活性的，可用作抗肿瘤药物。

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。