公开(公告)号：US08222231B2

公开(公告)日：2012-07-17

申请号：US12851166

申请日：2010-08-05

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 ,  A61K31/715 ,  A61P39/00

CPC分类号： C08B37/0075

摘要： Partially desulfated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. These glycosaminoglycan derivatives exhibit antiangiogenic 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基团具有说明书中所示含义的式（I）化合物。 这些糖胺聚糖衍生物表现出抗血管生成活性并且没有抗凝血活性。

公开(公告)号：US07728039B2

公开(公告)日：2010-06-01

申请号：US11993184

申请日：2006-05-31

申请人： Claudio Pisano ,  Giuseppe Giannini ,  Loredana Vesci ,  Franco Zunino ,  Sabrina Dallavalle ,  Lucio Merlini ,  Sergio Penco

发明人： Claudio Pisano ,  Giuseppe Giannini ,  Loredana Vesci ,  Franco Zunino ,  Sabrina Dallavalle ,  Lucio Merlini ,  Sergio Penco

IPC分类号： A61K31/185 ,  C07C259/06

CPC分类号： C07C259/06 ,  C07C259/10 ,  C07C2603/74 ,  C07D319/18

摘要： Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumor, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumors.

摘要翻译： 具有抗肿瘤活性的异羟肟基的联苯和苯基萘基化合物和抗血管生成活性因此，这些化合物特别可用于治疗耐药性肿瘤。

公开(公告)号：US20050137167A1

公开(公告)日：2005-06-23

申请号：US10489359

申请日：2001-09-12

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

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

IPC分类号： A61K47/36 ,  A61K31/727 ,  A61K45/00 ,  A61P1/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/04 ,  A61P11/06 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/04 ,  A61P37/00 ,  C08B37/00 ,  C08B37/10 ,  C07H5/04

CPC分类号： A61K31/727 ,  C08B37/0075 ,  C08B37/0078

摘要： Partially desulphated glycosaminoglycan derivatives are described, particularly heparin, and more particularly formula (I) compounds where the U, R and R1 groups have the meanings indicated in the description. Said glycosaminoglycan derivatives are endowed with antiangiogenic and heparanase-inhibiting activity ans 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所示含义的式（I）化合物。 所述糖胺聚糖衍生物具有抗血管生成和乙酰肝素酶抑制活性，没有抗凝活性。

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：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：US20110160147A1

公开(公告)日：2011-06-30

申请号：US12993738

申请日：2009-09-02

申请人： Alma Dal Pozzo ,  Emiliano Esposito ,  Minghong Ni ,  Sergio Penco ,  Claudio Pisano ,  Massimo Castorina ,  Loredana Vesci

发明人： Alma Dal Pozzo ,  Emiliano Esposito ,  Minghong Ni ,  Sergio Penco ,  Claudio Pisano ,  Massimo Castorina ,  Loredana Vesci

IPC分类号： A61K38/12 ,  C07K7/52 ,  A61P35/00 ,  A61P35/04

CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07K5/06026 ,  C07K7/64

摘要： The present invention relates to dual-targeting cytotoxic compounds of formula (I) and to their preparation. The described compounds are endowed with tumour specific action, incorporating three functional units: a tumour recognition moiety and a tumour selective enzymatic substrate sequence connected together by means of a spacer. These conjugates are designed to guarantee serum stability and, at the same time, the desired action inside the tumour cells as a result of enzymatic cleavability. [(L-D)nE]m-F-D-PI-SI-CT Formula (I).

摘要翻译： 本发明涉及式（I）的双靶向细胞毒性化合物及其制备。 所述化合物具有肿瘤特异性作用，并结合三个功能单元：通过间隔物连接在一起的肿瘤识别部分和肿瘤选择性酶底物序列。 这些缀合物被设计用于保证血清稳定性，并且同时由于酶切割性而在肿瘤细胞内所需的作用。 [（L-D）nE] m-F-D-PI-SI-CT式（I）。

公开(公告)号：US07105492B2

公开(公告)日：2006-09-12

申请号：US10388587

申请日：2003-03-17

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： A61K31/44 ,  A61K31/70 ,  C07H15/24 ,  C07D498/22

CPC分类号： C07D491/22

摘要： Camptothecin derivatives of camptothecin of formula (I) exhibit antitumor activity and show a good therapeutic index and are used in the treatment of tumors, viral infections and antiplasmodium falciparum.

摘要翻译： 式（I）喜树碱喜树碱衍生物具有抗肿瘤活性，显示出良好的治疗指标，用于治疗肿瘤，病毒感染和恶性疟原虫。

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：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。