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1.发明授权Camptothecins conjugated in position 7 to cyclic peptides as cytostatic agents 失效缀合在位置7的喜树碱与环肽作为细胞抑制剂公开(公告)号：US07705012B2
公开(公告)日：2010-04-27
申请号：US11596015
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： A61K31/4745 , C07D491/22
摘要： Compounds of Formula (I) are described in which the R1 group is as defined in the specification and includes the condensation of the camptothecin molecule in position 7 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基团如说明书中所定义，并且包括7位的喜树碱分子与含有RGD序列的环肽的缩合。 所述化合物对整联蛋白受体αv＆bgr 3和αv＆bgr 5具有高亲和力，并且在微摩尔浓度下对人肿瘤细胞系具有选择性细胞毒性活性。
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公开(公告)号：US20080161395A1
公开(公告)日：2008-07-03
申请号：US11815068
申请日：2006-02-13
申请人： Fabio Giannessi , Emanuela Tassoni , Maria Ornella Tinti , Roberto Conti , Natalina Dell'Uomo , Tiziana Brunetti
发明人： Fabio Giannessi , Emanuela Tassoni , Maria Ornella Tinti , Roberto Conti , Natalina Dell'Uomo , Tiziana Brunetti
IPC分类号： A61K31/21 , C07C229/02 , A61P3/10
CPC分类号： C07C275/16 , C07D211/90 , C07D213/82
摘要： The invention relates to a new class of compounds with action inhibiting carnitine palmitoyl transferase (CPT), pharmaceutical compounds which contain at least one new compound according to the invention, and their therapeutic use in the treatment of hyperglycaemic conditions such as diabetes and the pathologies associated with it, congestive heart failure and obesity.
摘要翻译： 本发明涉及具有抑制作用的肉碱棕榈酰转移酶（CPT）的新一类化合物，其含有至少一种本发明新化合物的药物化合物及其治疗用于治疗高血糖病症如糖尿病和相关病理 伴有它，充血性心力衰竭和肥胖。
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3.发明申请Camptothecin Derivatives Conjugated in Position 20 with Integrin Antagonists 审中-公开喜树碱衍生物与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。
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4.发明授权Esters of acyl L-carnitines and pharmaceutical compositions containing same for treating endotoxic shock 失效酰基L-肉碱的酯和含有其的用于治疗内毒素性休克的药物组合物公开(公告)号：US06180667B2
公开(公告)日：2001-01-30
申请号：US08827448
申请日：1997-03-28
IPC分类号： A61K31225
CPC分类号： C07C229/22 , A61K31/22
摘要： Esters of alkanoyl L-carnitines wherein the alkanoyl is a saturated or unsaturated, staight or branched alkanoyl having 2-26 carbon atoms, optionally &ohgr;-substituted with trialkylammonium, dialkylsulfonium, hydroxyl, carboxyl, halogen, methanesulfonyl and hydroxysulfonyl, are useful for preparing pharmaceutical compositions for the treatment of endotoxic shock.
摘要翻译： 烷酰基L-肉碱的酯，其中烷酰基是具有2-26个碳原子的饱和或不饱和的，稳定的或支链的烷酰基，任选被三烷基铵，二烷基锍，羟基，羧基，卤素，甲磺酰基和羟基磺酰基取代的烷酰基，可用于制备药物 用于治疗内毒素性休克的组合物。
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5.发明授权6,7-disubstituted-2-aminotetralines active as immunomodulators and pharmaceutical compositions containing same 失效作为免疫调节剂起作用的6,7-二取代-2-氨基三
线酯和含有它们的药物组合物公开(公告)号：US5962525A
公开(公告)日：1999-10-05
申请号：US871050
申请日：1997-06-09
申请人： Piero Foresta , Mauro Marzi , Maria Ornella Tinti
发明人： Piero Foresta , Mauro Marzi , Maria Ornella Tinti
IPC分类号： A61K31/135 , A61K31/216 , A61K31/675 , A61P37/00 , C07C211/38 , C07C217/74 , C07C219/26 , A61K31/225
CPC分类号： C07C219/26 , A61K31/135 , A61K31/216 , A61K31/675 , C07C2102/10
摘要： 6,7-disubstituted-2-aminotetralines of general formula (1) ##STR1## and their pharmacologically acceptable salts, wherein X and Y, identical or different are selected from the group consisting of methoxy, acetoxy and fluoro; and R and R.sub.1, identical or different, are selected from the group consisting of hydrogen, ethyl, propyl, cyclopropylmethyl, 2-hydroxy-2-phenylethyl, 2-hydroxy-2-(4-methylphenyl)ethyl and 2-hydroxy-3-(4-methoxyphenoxy)propyl are endowed with immunomodulator activity.
摘要翻译： 通式（1）的6,7-二取代-2-氨基四氢萘酯及其药理学上可接受的盐，其中X和Y相同或不同选自甲氧基，乙酰氧基和氟; 和R和R 1相同或不同，选自氢，乙基，丙基，环丙基甲基，2-羟基-2-苯基乙基，2-羟基-2-（4-甲基苯基）乙基和2-羟基-3 - （4-甲氧基苯氧基）丙基具有免疫调节剂活性。
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公开(公告)号：US20100311783A1
公开(公告)日：2010-12-09
申请号：US12857743
申请日：2010-08-17
申请人： Paolo Carminati , Maria Ornella Tinti , Mauro Marzi , Fabrizio Giorgi , Walter Cabri , Marco Alpegiani , Domenico Vergani , Paolo Ghetti
发明人： Paolo Carminati , Maria Ornella Tinti , Mauro Marzi , Fabrizio Giorgi , Walter Cabri , Marco Alpegiani , Domenico Vergani , Paolo Ghetti
IPC分类号： A61K31/4375 , C07D491/22 , A61P35/00
CPC分类号： C07D491/22
摘要： A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.
摘要翻译： 本文公开了制备7 - [（E） - 叔丁氧基亚氨基甲基] - 喜树碱（也称为gimatecan）的立体选择性方法。 随着在合适的不同溶剂混合物中进一步溶解和沉淀步骤的添加，也可以通过使用相同的立体选择性方法获得四种新的结晶形式的gimatecan。
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7.发明授权Esters of L-carnitine of alkanoyl L-carnitines useful as cationic lipids for the intracellular delivery of pharmacologically active compounds 失效用作阳离子脂质的烷酰基L-肉碱的左旋肉碱的酯用于细胞内递送药理学活性化合物公开(公告)号：US07629003B2
公开(公告)日：2009-12-08
申请号：US10624645
申请日：2003-07-23
申请人： Claudio Pisano , Maria Ornella Tinti , Mosé Santaniello , Luciana Critelli , Giovanni Salvatori
发明人： Claudio Pisano , Maria Ornella Tinti , Mosé Santaniello , Luciana Critelli , Giovanni Salvatori
IPC分类号： A61K9/127
CPC分类号： C07C229/22 , A61K8/14 , A61K8/44 , A61K9/0019 , A61K9/127 , A61K9/1272 , A61K9/1277 , A61K9/19 , A61K31/225 , A61K48/00 , A61Q19/00
摘要： Esters of L-carnitine and alkanoyl L-carnitines are described which can be used as cationic lipids for the intracellular delivery of pharmacologically active compounds. New esters of L-carnitine and alkanoyl L-carnitines of formula (I) are also disclosed wherein the R groups are as defined in the description.
摘要翻译： 描述了左旋肉碱和烷酰基L-肉碱的酯，其可用作阳离子脂质用于药理学活性化合物的细胞内递送。 还公开了式（I）的L-肉碱和烷酰基L-肉毒碱的新酯，其中R基团如说明书中所定义。
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8.发明授权7-Polyaminoalkyl(oxy)iminomethylcamptothecins bearing protective groups 失效带有保护基团的7-聚氨基烷基（氧基）亚氨基甲基冠心病公开(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。
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9.发明申请Use of pamoic acid or one of its derivatives, or one of its analogues, for the preparation of a medicament for the treatment of diseases characterised by deposits of amyloid aggregates 审中-公开使用双羟萘酸或其衍生物之一或其类似物之一用于制备用于治疗以淀粉样蛋白聚集体沉积为特征的疾病的药物公开(公告)号：US20080293812A1
公开(公告)日：2008-11-27
申请号：US11979301
申请日：2007-11-01
申请人： Maria Grazia Gallo , Maria Grazia Cima , Fabrizio Giorgi , Maria Ornella Tinti , Paola Piovesan , Orlando Ghirardi
发明人： Maria Grazia Gallo , Maria Grazia Cima , Fabrizio Giorgi , Maria Ornella Tinti , Paola Piovesan , Orlando Ghirardi
IPC分类号： A61K31/216 , C07C69/76 , A61P25/28
CPC分类号： C07C229/22 , A61K31/221 , A61K31/222 , A61K31/223 , A61K31/235 , C07C65/11 , C07C229/08
摘要： Pamoic acid or its derivatives of formula (I) are used to treat diseases characterized by deposits of amyloid aggregates.
摘要翻译： 帕莫西酸或其式（I）的衍生物用于治疗以淀粉样蛋白聚集体沉积为特征的疾病。
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公开(公告)号：US06566552B2
公开(公告)日：2003-05-20
申请号：US09849363
申请日：2001-05-07
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.
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