公开(公告)号：EP1812449A1

公开(公告)日：2007-08-01

申请号：EP05810702.0

申请日：2005-10-24

申请人： Antibioticos S.p.A.

发明人： POZZI, Giovanni ,  GHETTI, Paolo ,  BALSAMO, Gaetano ,  ALPEGIANI, Marco ,  CABRI, Walter

IPC分类号： C07D501/00

CPC分类号： C07D501/00

摘要： The invention relates to crystalline Cefdinir ammonium salt of formula (I).

公开(公告)号：EP1572699B1

公开(公告)日：2007-02-14

申请号：EP03789109.0

申请日：2003-12-01

申请人： Antibioticos S.p.A.

发明人： POZZI, Giovanni ,  MARTIN, Gomez, Patricio ,  ALPEGIANI, Marco ,  CABRI, Walter

IPC分类号： C07D501/22

CPC分类号： C07D501/22

摘要： Cefdinir crystalline salts of formula (I), in which n ranges from 1 to 3, the preparation and use thereof for the preparation and purification of cefdinir is herein disclosed. The salts of formula (I) can be obtained from cefdinir intermediates or crude cefdinir by treatment with phosphoric acid.

公开(公告)号：EP1178991A1

公开(公告)日：2002-02-13

申请号：EP00935029.9

申请日：2000-05-16

申请人： Antibioticos S.p.A.

发明人： SIVIERO, Enrico ,  CABRI, Walter ,  TERRASSAN, Daniele, Mario

IPC分类号： C07D501/00 ,  C12P35/02

CPC分类号： C12P35/02 ,  C07D501/00

摘要： A process for the preparation of Cefuroxime acid (I), which comprises the following steps: (1) Extraction of deacetyl 7-glutaryl ACA (II) aqueous solution at acid pH with organic solvents (for example according to the procedures disclosed in US 5,801,241); (2) drying the resulting solution while preventing lactonization of the intermediate; (3) carbamoylation of the hydroxymethyl group at the 3- position by reaction with chlorosulfonyl isocyanate or similar products; (7) extraction of the carbamoyl derivative from step 3 with water at neutral pH; (8) enzymatic hydrolysis of the amide at the 7- position of the cephalosporanic ring with glutaryl acylase; (6) acylation of the amino group by condensation with 2-furanyl(sin-methoxyimino)acetic acid chloride or mixed anhydride.

摘要翻译： 制备头孢呋辛酸（I）的方法，其包括以下步骤：（1）用有机溶剂在酸性pH下萃取脱乙酰-7-戊二酰基ACA（II）水溶液（例如根据US 5,801,241 ）; （2）干燥所得溶液，同时防止中间体的内酯化; （3）通过与异氰酸氯磺酰酯或类似产物反应使3-位羟甲基氨基甲酰化; （7）用中性pH的水萃取步骤3的氨基甲酰基衍生物; （8）用戊二酰基酰化酶在头孢菌素环的7-位酶促水解酰胺; （6）通过与2-呋喃基（sin-甲氧基亚氨基）乙酰氯或混合酸酐缩合将氨基酰化。

公开(公告)号：EP1485382A2

公开(公告)日：2004-12-15

申请号：EP03717204.6

申请日：2003-03-10

申请人： Antibioticos S.p.A.

发明人： CABRI, Walter ,  PAISSONI, Paolo ,  ROLETTO, Jacopo ,  FONTE, Piera ,  OLMO, Sara

IPC分类号： C07D457/02 ,  C07D457/04

CPC分类号： C07D457/04 ,  C07D457/02

摘要： A process for the synthesis of pergolide (Formula(I)) (D-6-n-propyl-8β­methylmercaptomethylergo line) from acid 9,10-dihydrolysergic is herein disclosed. The process can be carried out without isolating most intermediates and is particularly convenient both from the yield and safety standpoint. Moreover, pergolide thereby obtained is highly pure and can be conveniently transformed into pergolide mesylate.

公开(公告)号：EP1196420B1

公开(公告)日：2003-03-19

申请号：EP00945949.6

申请日：2000-07-24

申请人： Antibioticos S.p.A.

发明人： CABRI, Walter ,  SIVIERO, Enrico ,  DAVERIO, Paola, Luigia ,  LONGONI, Davide ,  FELISI, Claudio

IPC分类号： C07D501/04

CPC分类号： C07D501/00

摘要： A process for the preparation of Cefuroxime acid or of a corresponding pharmaceutically acceptable salt or ester, by reaction of a 3-hydroxymethylceph-3-em precursor thereof with activated isocyanates in carbonic acid esters.

公开(公告)号：EP1173166A1

公开(公告)日：2002-01-23

申请号：EP00920675.6

申请日：2000-04-07

申请人： Antibioticos S.p.A.

发明人： COLACCI, Annamaria ,  VACCARI, Monica ,  CABRI, Walter ,  BERNASCONI, Ermanno

IPC分类号： A61K31/385 ,  A61P35/04

CPC分类号： A61K31/385

摘要： The invention relates to the use of alpha lipoic acid, also known as lipoic acid, thioctic acid or 1,2-dithiolan-3-pentanoic acid,as well as derivatives thereof, in the control of tumour progression and in the antimetastatic therapy.

公开(公告)号：EP1282590B1

公开(公告)日：2005-11-02

申请号：EP01943338.2

申请日：2001-05-10

申请人： Antibioticos S.p.A.

发明人： PIZZAMIGLIO, Valentina ,  CABRI, Walter ,  MAPELLI, Elio

IPC分类号： C07C46/00 ,  C07C50/38 ,  C07C309/65

CPC分类号： C07C303/30 ,  C07C46/00 ,  C07C303/28 ,  C07C309/65 ,  C07C2603/44 ,  C07C50/38

公开(公告)号：EP1442029A1

公开(公告)日：2004-08-04

申请号：EP02802646.6

申请日：2002-11-05

申请人： Antibioticos S.p.A.

发明人： CABRI, Walter ,  ALPEGIANI, Marco ,  POZZI, Giovanni ,  MARTIN, Gomez, Patricio ,  OLIVA, Francesco ,  PIZZAMIGLIO, Valentina ,  PIANTA, Elena

IPC分类号： C07D277/20 ,  C07D501/06

CPC分类号： C07D277/587 ,  C07D501/00

摘要： A process for the preparation of salts of organic nitrogen bases with carboxylic acids of general formula (I), wherein Q and R have the meanings defined in the disclosure, useful for the preparation of cephalosporins side chains.

公开(公告)号：EP1425285A1

公开(公告)日：2004-06-09

申请号：EP02774564.5

申请日：2002-09-04

申请人： Antibioticos S.p.A.

发明人： LONGONI, Davide ,  ALPEGIANI, Marco ,  CABRI, Walter ,  FELISI, Claudio

IPC分类号： C07D501/00

CPC分类号： C07D501/00

摘要： The present invention relates to a process for the preparation of crystalline cefuroxime axetil with high purity lecel and optimal diastereomeric ratio. Said process, which comprises the use of a dimethyl carbonate for isolating crystallizing cefuroxime axetil, is particularly suitable for implementing on an industrial scale.

公开(公告)号：EP1282590A2

公开(公告)日：2003-02-12

申请号：EP01943338.2

申请日：2001-05-10

申请人： Antibioticos S.p.A.

发明人： PIZZAMIGLIO, Valentina ,  CABRI, Walter ,  MAPELLI, Elio

IPC分类号： C07C46/00 ,  C07C50/38 ,  C07C309/65

CPC分类号： C07C303/30 ,  C07C46/00 ,  C07C303/28 ,  C07C309/65 ,  C07C2603/44 ,  C07C50/38

摘要： The present invention discloses a process for the semi-synthesis of 4-demethoxydaunomycinone, (8s-cis)-acetyl-10-hydroxy-7,8,9,10-tetrahydro-6,8,11-trihydroxy-5,12-naphthacenedione, of formula (I).

摘要翻译： （8s-顺式） - 乙酰基-10-羟基-7,8,9,10-四氢-6,8,11-三羟基-5,12-二氢-5,7,8,9-四氢-2H-异喹啉酮的半合成方法本发明公开了一种半合成4-脱甲氧基还诺霉素酮的方法， （I）的萘并二酮。