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1. 发明专利

SK278225B6 未知
公开(公告)号：SK278225B6
公开(公告)日：1996-04-03
申请号：SK95890
申请日：1990-02-28
申请人： CABRI WALTER , CANDIANI ILARIA , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO
发明人： CABRI WALTER , CANDIANI ILARIA , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO
IPC分类号： B01J31/12 , C07B61/00 , B01J27/128 , C07C46/00 , C07C49/423 , C07C49/727 , C07C50/36 , C07C50/38
摘要： METHOD FOR PREPARATION OF ANTHRACYCLINONES The preparation method of anthracyclinones of the general formula I, wherein R means group of the formula COOR1, in which R1 means a hydrogen atom or methyl, resides in following: in the first stage the 13-keto group of the 4-demethyl-3- -deoxydaunomycinone is protected by working up with the ethylene glycol; in the second stage the resultant 4-demethyl-13- -dioxolanyl-7-deoxydaunomycinone reacts with the sulphonatic agent of the formula R'-SO2-X, in which X means the halogene atom or the group of the formula -O-SO2-R' and R' means the trifluoromethyl, p-fluorophenyl or p-tolyl group; in the third stage the resultant 4-demethyl-13-dioxolanyl-7- -deoxydaunomycinone of the general formula V reacts with the nucleophilic agent of the general formula R1OH in which R1 has a meaning listed above, and with the carbon monoxyde under presence of the triethylamine and the catalitic amount of the palladium complex with chelating ligand; and in the fourth stage the resultant 4-demethyl-4-carboxyalkyl-7-deoxy-13- -dioxolanyldaunomycinone of the general formula VII reacts with the bromine solution in the carbon tetrachloride for introduction of the alpha-hydroxy group into the position 7 of the general formula VII compound, then the 13-dioxolanyl protective group is removal and, after chromatographic treatment the required pure compound of the general formula I is obtained.

2. 发明专利

SK278267B6 MANUFACTURING PROCESS OF 4-DEMETHOXYDAUNOMYCINONE 未知
公开(公告)号：SK278267B6
公开(公告)日：1996-06-05
申请号：SK215289
申请日：1989-04-07
申请人： CABRI WALTER , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO , PENCO SERGIO
发明人： CABRI WALTER , DE BERNARDINIS SILVIA , FRANCALANCI FRANCO , PENCO SERGIO
IPC分类号： B01J31/02 , C07D317/26 , B01J31/24 , C07B61/00 , C07C45/00 , C07C46/00 , C07C50/38 , C07C67/00 , C07H15/252
摘要： 4-demetoxydaunomycinone of a formula I is manufactured as follows: 4-demethyl-13-di-oxolanyldaunomycinone is brought, under presence of N,N-di-isopropylethylamine and catalytic amount of 4-dimethylaminopyridine, into reaction with sulfonyl compound of the general formula RSO2X, in which X means the group of the formula OSO2R, wherein R represents trifluoromethyl group; resultant sulfonated 4-demethyl-13-dioxolanyldaunomycinone is forced to react in a reduction medium in presence of a catalytic amount of a compound of the general formula MLnL°m, in which M means the transition metal atom, preferably palladium or nickel, L and L', which are the same or different, mean chloride or acetate anion, or chelatingly acted monophosphine, diphosphine, phosphite or diamine molecule, preferably 1,3-diphenylphosphinpropane or 1,1'-bis(diphenylphosphin)ferrocene and n and m mean numbers of from 0 to 4, and then the protective group on the 13-oxo group of resultant 4-demetoxy-13-dioxolanyldaunomycinone is removed by treatment with trifluoroacetic acid at ambient temperature.

3. 发明申请

WO9905103A3 2O(S)-7-ETHYL-9-(N-METHYL-N-PHENYL)AMIDINO-CAMPTOTHECIN, ITS PREPARATION AND ITS USE AS ANTITUMOR AGENT 审中-公开
标题翻译： 2O（S）-7-乙基-9-（N-甲基-N-苯基）氨基 - 角叉菜胶，其制备及其用作抗菌剂
公开(公告)号：WO9905103A3
公开(公告)日：1999-04-15
申请号：PCT/EP9804919
申请日：1998-07-20
申请人： PHARMACIA & UPJOHN SPA , BEDESCHI ANGELO , CABRI WALTER , CANDIANI ILARIA , CAPOLONGO LAURA
发明人： BEDESCHI ANGELO , CABRI WALTER , CANDIANI ILARIA , CAPOLONGO LAURA
IPC分类号： C07D491/22 , A61K31/47 , A61K31/4745 , A61P35/00 , C07D20060101
CPC分类号： C07D491/22
摘要： A water soluble camptothecin derivative which is 20(S)-7-ethyl-9-(N-methyl-N-phenyl)amidino-camptothecin (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them and a process for their preparation are described. The compound of the invention and its pharmaceutically acceptable salts are useful antitumor agents and are further characterised by having a remarkable therapeutic index.
摘要翻译： 20（S）-7-乙基-9-（N-甲基-N-苯基）脒基 - 喜树碱（I）及其药学上可接受的盐，含有它们的药物组合物及其制备方法的水溶性喜树碱衍生物是描述。本发明化合物及其药学上可接受的盐是有用的抗肿瘤剂，其特征还在于具有显着的治疗指标。

4. 发明专利

SK279039B6 METHOD FOR PREPARATION OF ERGOLINE DERIVATIVES 未知
公开(公告)号：SK279039B6
公开(公告)日：1998-05-06
申请号：SK140193
申请日：1993-02-15
申请人： CANDIANI ILARIA , CABRI WALTER , BEDESCHI ANGELO , ZARINI FRANCO
发明人： CANDIANI ILARIA , CABRI WALTER , BEDESCHI ANGELO , ZARINI FRANCO
IPC分类号： A61K31/48 , A61P5/08 , A61P25/16 , C07D457/06
摘要： This patent describes the procedure related to the production of ergoline derivatives with a general formula (I), where R means C1-4 alkyl, cyclohexyl, phenyl or the group with the formula (CH2)nN(CH3)2, where n is integer, R2 means any group related to the symbol R1 or hydrogen, pyridyl, pyrimidyl, pyrazinyl, pyridazinyl, thiazolyl, or thiadiazol, R3 means C1-4 hydrocarbon, R4 means halogen, methylthio group or phenylthio group, R5 means hydrogen or methyl, while these derivatives are prepared based on the reaction of ergolinamide with a general formula (II) with isocyanate with a general formula (III), where the symbols R1, R2, R3, R4, R5 are explained in the patent description, while the metal catalyst together with phosphorus compounds is present. The ergoline derivatives are the compounds with anti-prolactinic effects and they can be applied when healing a Parkinson disease.

5. 发明申请

WO2004035800A3 INTERMEDIATE CEFDINIR SALTS 审中-公开
标题翻译：中间CEFDINIR销售
公开(公告)号：WO2004035800A3
公开(公告)日：2004-08-26
申请号：PCT/EP0310718
申请日：2003-09-26
申请人： ANTIBIOTICOS SPA , POZZI GIOVANNI , MARTIN GOMEZ PATRICIO , ALPEGIANI MARCO , CABRI WALTER
发明人： POZZI GIOVANNI , MARTIN GOMEZ PATRICIO , ALPEGIANI MARCO , CABRI WALTER
IPC分类号： C07D501/00 , C07D501/22
CPC分类号： C07D501/00 , Y02P20/55
摘要： Disclosed are salts of the general formula (I) wherein R1, R2 and as defined in the description and a process for the preparation thereof. These salts are useful intermediates for the preparation of cefdinir.
摘要翻译：公开了通式（I）的盐，其中R1，R2和如说明书中所定义的及其制备方法。这些盐是制备头孢地尼的有用中间体。

6. 发明申请

WO2006067092A2 STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN 审中-公开
标题翻译：立体选择性方法和结晶形式
公开(公告)号：WO2006067092A2
公开(公告)日：2006-06-29
申请号：PCT/EP2005056849
申请日：2005-12-16
申请人： SIGMA TAU IND FARMACEUTI , CARMINATI PAOLO , TINTI MARIA ORNELLA , MARZI MAURO , GIORGI FABRIZIO , CABRI WALTER , ALPEGIANI MARCO , VERGANI DOMENICO , GHETTI PAOLO
发明人： CARMINATI PAOLO , TINTI MARIA ORNELLA , MARZI MAURO , GIORGI FABRIZIO , CABRI WALTER , ALPEGIANI MARCO , VERGANI DOMENICO , GHETTI PAOLO
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（也称为吉马替康）的立体选择性方法。通过在适当的不同溶剂混合物中进行进一步的溶解和沉淀步骤，还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。

7. 发明申请

WO2006053625A8 CRYSTALLINE FORM OF CEFDINIR AMMONIUM SALT AS AN INTERMEDIATE FOR THE PREPARATION OF PURE CEFDINIR 审中-公开
标题翻译： CEFDINIR AUMONIUM盐的晶体形式作为制备纯CEFDINIR的中间体
公开(公告)号：WO2006053625A8
公开(公告)日：2007-07-05
申请号：PCT/EP2005011385
申请日：2005-10-24
申请人： ANTIBIOTICOS SPA , POZZI GIOVANNI , GHETTI PAOLO , BALSAMO GAETANO , ALPEGIANI MARCO , CABRI WALTER
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).
摘要翻译：本发明涉及式（I）的结晶头孢地尼铵盐。

8. 发明申请

WO03040116A8 A PROCESS FOR THE PREPARATION OF CEPHALOSPORINS SIDE CHAINS 审中-公开
标题翻译：一种制备CEPHOROSPORINS侧链的方法
公开(公告)号：WO03040116A8
公开(公告)日：2004-06-17
申请号：PCT/EP0212328
申请日：2002-11-05
申请人： ANTIBIOTICOS SPA , CABRI WALTER , ALPEGIANI MARCO , POZZI GIOVANNI , MARTIN GOMEZ PATRICIO , OLIVA FRANCESCO , PIZZAMIGLIO VALENTINA , PIANTA ELENA
发明人： CABRI WALTER , ALPEGIANI MARCO , POZZI GIOVANNI , MARTIN GOMEZ PATRICIO , OLIVA FRANCESCO , PIZZAMIGLIO VALENTINA , PIANTA ELENA
IPC分类号： C07D277/20 , C07D277/40 , C07D501/00 , C07D501/06 , C07D501/22
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.
摘要翻译：一种制备有机氮碱的盐与通式（I）的羧酸的方法，其中Q和R具有本公开限定的含义，可用于制备头孢菌素侧链。

9. 发明申请

WO2016199076A3 POLYMORPHIC FORMS OF AFATINIB FREE BASE AND AFATINIB DIMALEATE 审中-公开
标题翻译： AFATINIB自由基和AFATINIB DIMALEATE的多形态
公开(公告)号：WO2016199076A3
公开(公告)日：2017-03-09
申请号：PCT/IB2016053420
申请日：2016-06-10
申请人： FRESENIUS KABI ONCOLOGY LTD , CABRI WALTER , LAHIRI SASWATA , MISHRA BHUWAN BHASKAR , AZIM ABUL , PANDA NILENDU , BHAVANAM POLI REDDY , RAY KRISHANU , KACHHADIA NIKUNJ , SINGH KUMBER
发明人： CABRI WALTER , LAHIRI SASWATA , MISHRA BHUWAN BHASKAR , AZIM ABUL , PANDA NILENDU , BHAVANAM POLI REDDY , RAY KRISHANU , KACHHADIA NIKUNJ , SINGH KUMBER
IPC分类号： C07D407/12 , A61K31/517 , A61P35/00
CPC分类号： C07D407/12
摘要： The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof.
摘要翻译：本发明涉及阿片素及其二马来酸盐的结晶形式。本发明还涉及制备阿拉非尼及其二马来酸盐的结晶形式的方法。本发明还涉及此类结晶形式的阿片素二马来酸二乙酯的药物组合物及其在治疗有需要的患者中的用途。

10. 发明申请

WO2012168213A3 NOVEL PROCESS FOR THE SYNTHESIS OF 7-CHLORO-4-(PIPERAZIN-1-YL)-QUINOLINE 审中-公开
标题翻译：合成7-氯代-4-（哌嗪-1-基） - 喹啉的新工艺
公开(公告)号：WO2012168213A3
公开(公告)日：2013-03-07
申请号：PCT/EP2012060553
申请日：2012-06-05
申请人： SIGMA TAU IND FARMACEUTI , CABRI WALTER , CASTAGNANI ROBERTO , ARMAROLI SILVIA , QUATTROCIOCCHI GIANANDREA , COLANGELI VINCENZO
发明人： CABRI WALTER , CASTAGNANI ROBERTO , ARMAROLI SILVIA , QUATTROCIOCCHI GIANANDREA , COLANGELI VINCENZO
IPC分类号： C07D215/46
CPC分类号： C07D215/46
摘要： The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.
摘要翻译：本发明提供了合成式I的7-氯-4-（哌嗪-1-基） - 喹啉的多晶型物的新方法。所述喹啉化合物基本上是纯的任何杂质。本发明还提供上述7-氯-4-（哌嗪-1-基） - 喹啉的多晶型物在合成哌啶或其药学上可接受的盐之一中的用途。

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