公开(公告)号：US08598384B2

公开(公告)日：2013-12-03

申请号：US12672099

申请日：2008-07-31

申请人： Walter Cabri ,  Mauro Marzi ,  Fabrizio Giorgi ,  Emanuela Tassoni

发明人： Walter Cabri ,  Mauro Marzi ,  Fabrizio Giorgi ,  Emanuela Tassoni

IPC分类号： C07C229/00 ,  A01N33/02

CPC分类号： C07C275/16

摘要： The present invention relates to a new crystalline form of R-4-trimethylammonium-3-(tetradecylcarbamoyl)-amino butyrate (also named crystalline Form I of ST 1326 or teglicar), a process for its preparation and pharmaceutical compositions containing same.

摘要翻译： 本发明涉及一种新的结晶形式的R-4-三甲基铵-3-（十四烷基氨基甲酰基） - 氨基丁酸酯（也称为ST1326的晶体形式I或晶体），其制备方法和含有它的药物组合物。

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。

公开(公告)号：US5047433A

公开(公告)日：1991-09-10

申请号：US135335

申请日：1987-12-21

申请人： Mauro Marzi ,  Maria O. Tinti ,  Romano Di Fabio ,  Domenico Misiti

发明人： Mauro Marzi ,  Maria O. Tinti ,  Romano Di Fabio ,  Domenico Misiti

IPC分类号： C07C217/74 ,  A61K31/13 ,  A61K31/135 ,  A61P9/12 ,  C07C67/00 ,  C07C213/00 ,  C07C213/02

CPC分类号： A61K31/13

摘要： N-alkyl derivatives of 2-amino-6,7-dimethoxy tetraline having general formula (I) ##STR1## wherein R is selected from hydrogen, ethyl, n-propyl and methyl cyclopropyl;R.sub.1 is selected from hydrogen, hydroxy and --OR.sub.3 wherein R.sub.3 is selected from methyl, ethyl and n-propyl; andR.sub.2 is selected from hydrogen, methyl, hydroxy, trifluoromethyl, fluoro and methoxy,are endowed with potent antihypertensive activity.

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。

公开(公告)号：US20100184972A1

公开(公告)日：2010-07-22

申请号：US11993185

申请日：2006-05-31

申请人： Mauro Marzi ,  Maria Di Marzo

发明人： Mauro Marzi ,  Maria Di Marzo

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： A process for the synthesis of deoxybiotinyl hexamethylenediamine0-DOTA is herein described. Said process comprises reacting biotinyl hexamithylenediamine with tri-t-butyl DOTA in the presence of benzotriazol-1-yl-oxytripyrrolidinophosphonium hexafluorophosphate, as the condensing agent, and triethylamine, as a base.

摘要翻译： 本文描述了合成脱氧生物基六亚甲基二胺-ODTA的方法。 所述方法包括在苯并三唑-1-基 - 氧三吡咯烷鏻六氟磷酸盐作为缩合剂和作为碱的三乙胺存在下，将生物素基六亚甲基二胺与三叔丁基DOTA反应。

公开(公告)号：USRE40861E1

公开(公告)日：2009-07-21

申请号：US11606322

申请日：2006-11-30

申请人： Fabio Giannessi ,  Mauro Marzi ,  Patrizia Minetti ,  Francesco De Angelis ,  Maria O. Tinti ,  Piero Chiodi ,  Arduino Arduini

发明人： Fabio Giannessi ,  Mauro Marzi ,  Patrizia Minetti ,  Francesco De Angelis ,  Maria O. Tinti ,  Piero Chiodi ,  Arduino Arduini

IPC分类号： A61K31/46 ,  C07D453/02

CPC分类号： C07D257/04 ,  C07C229/22 ,  C07C229/26 ,  C07C271/12 ,  C07C271/22 ,  C07C275/16 ,  C07C311/06 ,  C07C335/08 ,  C07D295/15 ,  C07D453/02 ,  C07F9/5407

摘要： Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

公开(公告)号：US20080207729A1

公开(公告)日：2008-08-28

申请号：US11917065

申请日：2006-05-31

申请人： Claudio Pisano ,  Gianfranco Battistuzzi ,  Maria Di Marzo ,  Giuseppe Giannini ,  Mauro Marzi ,  Loredana Vesci ,  Franco Zunino

发明人： Claudio Pisano ,  Gianfranco Battistuzzi ,  Maria Di Marzo ,  Giuseppe Giannini ,  Mauro Marzi ,  Loredana Vesci ,  Franco Zunino

IPC分类号： A61K31/404 ,  A61P35/00 ,  C07D209/04

CPC分类号： C07D209/18

摘要： Indole derivatives of Formula (I+A) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.

摘要翻译： 描述了具有抗肿瘤和化学敏化活性的式（I + A）的吲哚衍生物。 还描述了含有上述化合物的药物组合物，用于治疗肿瘤。

公开(公告)号：US20060160778A1

公开(公告)日：2006-07-20

申请号：US10563480

申请日：2004-07-06

申请人： Giuseppe Giannini ,  Domenico Alloatti ,  Marcella Marcellini ,  Mauro Marzi ,  Teresa Riccioni ,  Maria Tinti

发明人： Giuseppe Giannini ,  Domenico Alloatti ,  Marcella Marcellini ,  Mauro Marzi ,  Teresa Riccioni ,  Maria Tinti

IPC分类号： A61K31/66 ,  C07F9/02 ,  A61K31/135

CPC分类号： C07C217/84 ,  C07C43/23 ,  C07F9/12

摘要： The present invention is related to new derivatives of Combretastatin, of Formula obtained by total synthesis. The strategy developed for each of the compounds is to i) replace a halogen (i.e. fluorine atom) to hydrogen on olefinic bound; ii) replace an aromatic ring in a natural product with an amino-aromatic ring. Said compounds recognize and bind the tubulin site: are useful for treating pathological states which arise from or are exacerbated by cell proliferation—as anticancer and/or antiangiogenic activity, in a mammal—to pharmaceutical compositions comprising these compounds.

公开(公告)号：US5272151A

公开(公告)日：1993-12-21

申请号：US854916

申请日：1992-03-20

申请人： Mauro Marzi ,  Patrizia Minetti ,  Piero Foresta ,  Maria O. Tinti

发明人： Mauro Marzi ,  Patrizia Minetti ,  Piero Foresta ,  Maria O. Tinti

IPC分类号： A61K31/505 ,  A61K31/519 ,  A61K38/00 ,  A61P31/04 ,  A61P35/00 ,  A61P37/00 ,  A61P37/04 ,  C07D487/04 ,  C07K5/04 ,  C07K5/06 ,  C07K5/08 ,  C07K5/10 ,  C07K7/06 ,  A61K31/495

CPC分类号： C07K5/06026 ,  C07K5/04 ,  A61K38/00

摘要： The present invention concerns aminoacyl and oligopeptidyl derivatives of allopurinol (1,5-dihydro-4H-pyrazolo-[3,4-d]-pyrimidin-4-one) of general formula (I), and related salts with ##STR1## pharmacologically-acceptable cations, in which n is an integer between 2 and 6, preferably 5, Y is H or CO--A, in which A is a racemic or chiral amino acid, dipeptide, tripeptide, tetrapeptide, or pentapeptide chosen, respectively, from the groups consisting of:a) arginine, aspartic acid, lysine, leucine;b) glycylaspartate, glycylglycine, aspartylarginine, leucylarginine, alanylglycine;c) arginyllysylaspartate, aspartyllysylarginine, lysylprolylarginine, prolylprolylarginine, lysylhistidylglycinamide, prolylphenylalanylarginine, phenylalanylprolylarginine;d) arginyllysylaspartylvaline, valylaspartyllysylarginine, threonylvalylleucylhistidine;e) arginyllysylaspartylvalyltyrosine.

公开(公告)号：US08053460B2

公开(公告)日：2011-11-08

申请号：US11917065

申请日：2006-05-31

申请人： Claudio Pisano ,  Gianfranco Battistuzzi ,  Maria Di Marzo ,  Giuseppe Giannini ,  Mauro Marzi ,  Loredana Vesci ,  Franco Zunino

发明人： Claudio Pisano ,  Gianfranco Battistuzzi ,  Maria Di Marzo ,  Giuseppe Giannini ,  Mauro Marzi ,  Loredana Vesci ,  Franco Zunino

IPC分类号： A61K31/404 ,  C07D209/10

CPC分类号： C07D209/18

摘要： Indole derivatives of Formula (I+A) having antitumor and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumors.

摘要翻译： 描述了具有抗肿瘤和化学敏化活性的式（I + A）的吲哚衍生物。 还描述了含有上述化合物的药物组合物，用于治疗肿瘤。