公开(公告)号：US20120220771A1

公开(公告)日：2012-08-30

申请号：US13505357

申请日：2010-10-27

Applicant: Matteo D'Anello ,  Marco Re

Inventor： Matteo D'Anello ,  Marco Re

IPC: C07D403/04 ,  C07D207/34

CPC classification number: C07D403/04 ,  C07D207/34

Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

Abstract translation: 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 该方法允许以高产率和纯度获得所需的产物。 合成起始于缩醛与β-酮酯的偶联; 将所得化合物乙酰化，然后与N，N-二甲基甲酰胺的二烷基缩醛反应，得到中间体，将其中环化为5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-基） 羧酸酯; 然后将羧酸酯水解，所得羧酸最终与适当形式的氨浓缩，得到所需的甲酰胺。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 该化合物可用于治疗各种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

公开(公告)号：US20110039934A1

公开(公告)日：2011-02-17

申请号：US12846341

申请日：2010-07-29

Applicant: Fausto PIVETTI ,  Maria Gioia Fornaretto ,  Marco Re

Inventor： Fausto PIVETTI ,  Maria Gioia Fornaretto ,  Marco Re

IPC: A61K31/19 ,  C07C51/08 ,  A61P25/28

CPC classification number: C07C253/30 ,  C07C51/09 ,  C07C253/14 ,  C07C61/40 ,  C07C255/35 ,  C07C255/46

Abstract: Compounds according to formula (IA): may be efficiently prepared by the disclosed process.

Abstract translation: 根据式（IA）的化合物：可以通过所公开的方法有效制备。

公开(公告)号：US08592583B2

公开(公告)日：2013-11-26

申请号：US13505357

申请日：2010-10-27

Applicant: Matteo D'Anello ,  Marco Re

Inventor： Matteo D'Anello ,  Marco Re

IPC: C07D401/00

CPC classification number: C07D403/04 ,  C07D207/34

Abstract: The invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. The process allows to obtain the desired products in high yields and purity. The synthesis is starting from the coupling of an acetal with a beta-ketoester; the resultant compound is acetylated and then reacted with a dialkyl acetal of N,N-dimethylformamide to give an intermediate which is cyclized to 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxylic ester; the carboxylic ester is then hydrolyzed and the resultant carboxylic acid is finally condensed with an appropriate form of ammonia to give the desired carboxamide. The compounds prepared according to the process of the invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.

Abstract translation: 本发明涉及制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法和该方法的有用的中间体化合物。 该方法允许以高产率和纯度获得所需的产物。 合成起始于缩醛与β-酮酯的偶联; 将所得化合物乙酰化，然后与N，N-二甲基甲酰胺的二烷基缩醛反应，得到中间体，将其中环化为5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-基） 羧酸酯; 然后将羧酸酯水解，所得羧酸最终与适当形式的氨浓缩，得到所需的甲酰胺。 根据本发明的方法制备的化合物具有蛋白激酶抑制活性，更具体地，赋予Cdc7或Cdc7 / Cdks抑制活性。 该化合物可用于治疗各种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

公开(公告)号：US20090061129A1

公开(公告)日：2009-03-05

申请号：US12229093

申请日：2008-08-20

Applicant: Marco Re Fraschini ,  Felice Ursino

Inventor： Marco Re Fraschini ,  Felice Ursino

IPC: B32B27/08 ,  B65B53/02 ,  B32B27/34

CPC classification number: B32B27/34 ,  B29C51/02 ,  B29C51/14 ,  B32B27/304 ,  B32B27/32 ,  B32B2307/518 ,  B32B2307/702 ,  B32B2307/7244 ,  B32B2307/736 ,  B32B2439/00 ,  Y10T428/1328 ,  Y10T428/31725 ,  Y10T428/31757

Abstract: A multi-layer, gas-barrier, biaxially oriented and heat-shrinkable film comprising a first outer heat-sealable layer a), an inner gas-barrier layer b), preferably of PVDC, and a second outer abuse resistant layer c), said film being characterized in that at least one layer of the structure, that can be an inner layer d) or, preferably, the second outer abuse resistant layer c), is a polyamide layer that comprises a major proportion of one or more amorphous polyamides. Preferably the amorphous polyamides of said polyamide layer have a Tg≦120° C., more preferably ≦110° C., and even more preferably ≦100° C. The invention also concerns the use of said films in a “thermoform-shrink” packaging process and the shrunk package obtained therefrom.

Abstract translation: 包含第一外部可热密封层a），内部阻气层b），优选PVDC和第二外部抗<！ - SIPO - >抗层c）的多层阻气双轴取向和热收缩膜， 所述膜的特征在于，可以是内层d）或优选地，第二外部抗滥用层c）的至少一层结构是聚酰胺层，其包含主要比例的一种或多种无定形聚酰胺 。 优选地，所述聚酰胺层的无定形聚酰胺的Tg <= 120℃，更优选<= 110℃，甚至更优选<= 100℃。本发明还涉及所述膜在“热成型 收缩“包装过程和从其获得的收缩包装。

公开(公告)号：US09056818B2

公开(公告)日：2015-06-16

申请号：US12846341

申请日：2010-07-29

Applicant: Fausto Pivetti ,  Maria Gioia Fornaretto ,  Marco Re

Inventor： Fausto Pivetti ,  Maria Gioia Fornaretto ,  Marco Re

IPC: C07C61/04 ,  C07C253/30 ,  C07C51/09 ,  C07C253/14

CPC classification number: C07C253/30 ,  C07C51/09 ,  C07C253/14 ,  C07C61/40 ,  C07C255/35 ,  C07C255/46

Abstract: Compounds according to formula (IA): may be efficiently prepared by the disclosed process.

Abstract translation: 根据式（IA）的化合物：可以通过所公开的方法有效制备。