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1.发明申请AMINO DERIVATIVES OF ANDROSTANES AND ANDROSTENES AS MEDICAMENTS FOR CARDIOVASCULAR DISORDERS 有权安非他明的氨基酸衍生物和作为心血管疾病药物的安慰剂公开(公告)号：US20110053902A1
公开(公告)日：2011-03-03
申请号：US12295497
申请日：2007-04-11
申请人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
发明人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
CPC分类号： C07J41/0038 , C07J41/0016 , C07J43/003
摘要： Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
摘要翻译： 式（I）化合物其中：所述基团如说明书中所定义，可用于制备用于治疗心血管疾病，特别是心力衰竭和高血压的药物。 这些化合物是Na +，K + -ATP酶的酶活性的抑制剂。 所述化合物用于制备用于治疗由内源性哇巴因的高血压作用引起的疾病的药物，例如常染色体显性多囊肾病（ADPKD）的肾衰竭进展，先兆子痫高血压和蛋白尿以及患者肾衰竭进展 与adducin多态性。
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2.发明授权Amino derivatives of androstanes and androstenes as medicaments for cardiovascular disorders 有权雄激素和雄激素的氨基衍生物作为心血管疾病的药物公开(公告)号：US08609644B2
公开(公告)日：2013-12-17
申请号：US12295497
申请日：2007-04-11
申请人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
发明人： Alberto Cerri , Marco Torri , Silvia Armaroli , Leonardo Banfi , Giuseppe Bianchi , Giulio Carzana , Patrizia Ferrari , Rosamaria Michaeletti , Simona Sputore , Maria Pia Zappavigna
IPC分类号： A61K31/566 , C07J41/00
CPC分类号： C07J41/0038 , C07J41/0016 , C07J43/003
摘要： Compounds of formula (I) wherein: the groups are as defined in the description, are useful for the preparation of medicaments for the treatment of cardiovascular disorders, in particular heart failure and hypertension. The compounds are inhibitors of the enzymatic activity of the Na+, K+-ATPase. Said compounds are used for the preparation of a medicament for the treatment of a disease caused by the hypertensive effects of endogenous ouabain, such as renal failure progression in autosomal dominant polycystic renal disease (ADPKD), preeclamptic hypertension and proteinuria and renal failure progression in patients with adducin polymorphisms.
摘要翻译： 式（I）化合物其中：所述基团如说明书中所定义，可用于制备用于治疗心血管疾病，特别是心力衰竭和高血压的药物。 这些化合物是Na +，K + -ATP酶的酶活性的抑制剂。 所述化合物用于制备用于治疗由内源性哇巴因的高血压作用引起的疾病的药物，例如常染色体显性多囊肾病（ADPKD）的肾衰竭进展，先兆子痫高血压和蛋白尿以及患者肾衰竭进展 与adducin多态性。
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公开(公告)号：US09127037B2
公开(公告)日：2015-09-08
申请号：US12094885
申请日：2006-11-23
申请人： Alberto Cerri , Silvia Armaroli , Marco Torri
发明人： Alberto Cerri , Silvia Armaroli , Marco Torri
IPC分类号： C07J17/00
CPC分类号： C07J17/00
摘要： New crystalline forms of 17β-(3-Furyl)-5-βandrostane-3β,14β,17α-triol are described together with pharmaceutical composition containing the same and methods for their preparation. In particular new Forms B, C, D, E and H are here described.
摘要翻译： 一起描述17＆bgr--（3-呋喃基）-5-＆bgr;雄甾烷-3和bgr，14＆bgr，17α-三醇的新结晶形式以及含有它们的药物组合物及其制备方法。 特别地，这里描述了新的形式B，C，D，E和H。
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公开(公告)号：US20080300228A1
公开(公告)日：2008-12-04
申请号：US12094885
申请日：2006-11-23
申请人： Alberto Cerri , Silvia Armaroli , Marco Torri
发明人： Alberto Cerri , Silvia Armaroli , Marco Torri
CPC分类号： C07J17/00
摘要： New crystalline forms of 17β-(3-Furyl)-5-βandrostane-3β,14β,17α-triol are described together with pharmaceutical composition containing the same and methods for their preparation. In particular new Forms B, C, D, E and H are here described.
摘要翻译： 一起描述了17β-（3-呋喃基）-5-β雄甾烷-3β，14beta，17α-三醇的新结晶形式以及含有它们的药物组合物及其制备方法。 特别地，这里描述了新的形式B，C，D，E和H。
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5.发明授权公开(公告)号：US09206133B2
公开(公告)日：2015-12-08
申请号：US14123893
申请日：2012-06-05
申请人： Walter Cabri , Roberto Castagnani , Silvia Armaroli , Gianandrea Quattrociocchi , Vincenzo Colangeli
发明人： Walter Cabri , Roberto Castagnani , Silvia Armaroli , Gianandrea Quattrociocchi , Vincenzo Colangeli
IPC分类号： C07D401/04 , 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任何杂质的纯的。 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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6.发明授权Crystalline form II of 7-(dimethoxy-methyl) camptothecin, its use as intermediate and products obtained therefrom 有权7-（二甲氧基 - 甲基）喜树碱的结晶形式II，其用作中间体和由其获得的产物公开(公告)号：US08269007B2
公开(公告)日：2012-09-18
申请号：US12670905
申请日：2008-07-22
申请人： Walter Cabri , Mauro Marzi , Fabrizio Giorgi , Elena Badaloni , Silvia Armaroli , Giuseppe Marazzi
发明人： Walter Cabri , Mauro Marzi , Fabrizio Giorgi , Elena Badaloni , Silvia Armaroli , Giuseppe Marazzi
IPC分类号： C07D491/22 , C07D491/147
CPC分类号： C07D491/22
摘要： This invention relates to a process for preparing a crystalline form of (4S)-11(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3′4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing from methanol.
摘要翻译： 本发明涉及制备（4S）-11（二甲氧基甲基）-4-乙基-4-羟基-1H-吡喃并[3'4'：6,7]吲哚并[1,2-b] 喹啉-3,14（4H，12H） - 二酮，也称为7-（二甲氧基甲基）喜树碱）。 通过提供特定的结晶步骤，以合适的方式得到上述化合物的新结晶形式。 制备多晶型II的方法包括将喜树碱转化成相应的7-（二甲氧基 - 甲基）喜树碱，并从甲醇中结晶。
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7.发明申请Novel Process for the Synthesis of 7-Chloro-4-(piperazin-1-yl)-quinoline 有权用于合成7-氯-4-（哌嗪-1-基） - 喹啉的新方法公开(公告)号：US20140200346A1
公开(公告)日：2014-07-17
申请号：US14123893
申请日：2012-06-05
申请人： Walter Cabri , Roberto Castagnani , Silvia Armaroli , Gianandrea Quattrociocchi , Vincenzo Colangeli
发明人： Walter Cabri , Roberto Castagnani , Silvia Armaroli , Gianandrea Quattrociocchi , Vincenzo Colangeli
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任何杂质的纯的。 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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8.发明申请CRYSTALLINE FORM II OF 7-(DIMETHOXY-METHYL) CAMPTOTHECIN, ITS USE AS INTERMEDIATE AND PRODUCTS OBTAINED THEREFROM 有权7-（二甲氧基甲基）氨基甲酸酯的晶体形式II，作为中间体使用，并由其获得的产物公开(公告)号：US20100249414A1
公开(公告)日：2010-09-30
申请号：US12670905
申请日：2008-07-22
申请人： Walter Cabri , Mauro Marzi , Fabrizio Giorgi , Elena Badaloni , Silvia Armaroli , Giuseppe Marazzi
发明人： Walter Cabri , Mauro Marzi , Fabrizio Giorgi , Elena Badaloni , Silvia Armaroli , Giuseppe Marazzi
IPC分类号： C07D471/20
CPC分类号： C07D491/22
摘要： This invention relates to a process for preparing a crystalline form of (4S)-11-(dimethoxymethyl)-4-ethyl-4-hydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]qui-noline-3,14(4H,12H)-dione (also named 7-(dimethoxy-methyl)camptothecin). With the provision of a particular crystallization step, in appropriate way, a new crystalline form of the above compound is obtained. The process for the preparation of the polymorph Form II comprises transforming camptothecin to the corresponding 7-(dimethoxy-methyl)-camptothecin, and crystallizing it from methanol.
摘要翻译： 本发明涉及制备（4S）-11-（二甲氧基甲基）-4-乙基-4-羟基-1H-吡喃并[3'，4'：6,7]吲哚并[1,2- b]喹啉-3,14（4H，12H） - 二酮（也称为7-（二甲氧基 - 甲基）喜树碱）。 通过提供特定的结晶步骤，以合适的方式得到上述化合物的新结晶形式。 制备多晶型II的方法包括将喜树碱转化成相应的7-（二甲氧基 - 甲基）喜树碱，并将其从甲醇中结晶。
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