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1. 发明申请

US20110039934A1 PROCESS FOR THE PREPARATION OF DERIVATIVES OF 1-(2- HALOBIPHENYL-4-YL)-CYCLOPROPANECARBOXYLIC ACID 有权
标题翻译：制备1-（2-羟基乙酰基-4-基） - 环戊二羧酸的衍生物的方法
公开(公告)号：US20110039934A1
公开(公告)日：2011-02-17
申请号：US12846341
申请日：2010-07-29
申请人： Fausto PIVETTI , Maria Gioia Fornaretto , Marco Re
发明人： Fausto PIVETTI , Maria Gioia Fornaretto , Marco Re
IPC分类号： A61K31/19 , C07C51/08 , A61P25/28
CPC分类号： C07C253/30 , C07C51/09 , C07C253/14 , C07C61/40 , C07C255/35 , C07C255/46
摘要： Compounds according to formula (IA): may be efficiently prepared by the disclosed process.
摘要翻译：根据式（IA）的化合物：可以通过所公开的方法有效制备。

2. 发明授权

US09056818B2 Process for the preparation of derivatives of 1-(2-halobiphenyl-4-yl)-cyclopropanecarboxylic acid 有权
标题翻译：制备1-（2-卤代联苯-4-基） - 环丙烷羧酸衍生物的方法
公开(公告)号：US09056818B2
公开(公告)日：2015-06-16
申请号：US12846341
申请日：2010-07-29
申请人： Fausto Pivetti , Maria Gioia Fornaretto , Marco Re
发明人： Fausto Pivetti , Maria Gioia Fornaretto , Marco Re
IPC分类号： C07C61/04 , C07C253/30 , C07C51/09 , C07C253/14
CPC分类号： C07C253/30 , C07C51/09 , C07C253/14 , C07C61/40 , C07C255/35 , C07C255/46
摘要： Compounds according to formula (IA): may be efficiently prepared by the disclosed process.
摘要翻译：根据式（IA）的化合物：可以通过所公开的方法有效制备。

3. 发明授权

US08399668B2 Process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides 有权
标题翻译：制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺的方法
公开(公告)号：US08399668B2
公开(公告)日：2013-03-19
申请号：US12989518
申请日：2009-04-30
申请人： Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
发明人： Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
IPC分类号： C07D403/04
CPC分类号： C07D403/04
摘要： The present 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. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in WO2007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
摘要翻译：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。在WO2007110344中描述和要求保护5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺，其也公开了其制备方法。这些化合物可以有利地通过允许以高产率和纯度以及有限数量的步骤获得所需产物的方法制备。合成起始于氰基吡咯衍生物，其特征在于5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲腈的最终水解。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。因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

4. 发明授权

US08658662B2 Crystalline CDC7 inhibitor salts 有权
标题翻译：结晶CDC7抑制剂盐
公开(公告)号：US08658662B2
公开(公告)日：2014-02-25
申请号：US13508648
申请日：2010-11-05
申请人： Massimo Zampieri , Ermes Vanotti , Paola Civaroli , Maria Gioia Fornaretto
发明人： Massimo Zampieri , Ermes Vanotti , Paola Civaroli , Maria Gioia Fornaretto
IPC分类号： A01N43/54 , A61K31/505
CPC分类号： C07D403/04
摘要： The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide.
摘要翻译：本发明涉及CDC7或CDC7 / CDKs抑制剂的新结晶盐，相应游离碱的新结晶形式，其制备方法，这些新盐形式的水合物，溶剂化物和多晶型物的用途在治疗和含有它们的药物组合物。这样的结晶盐选自5-（2-氨基 - 嘧啶-4-基）-2-（2,4-二氯 - 苯基）-2-羟基丙酸的L-天冬氨酸盐，半富马酸盐，盐酸盐，马来酸盐，甲磺酸盐，硫酸盐，L-酒石酸盐或磷酸盐，苯基）-1H-吡咯-3-甲酸酰胺。

5. 发明申请

US20120041007A1 CDK INHIBITOR SALTS 有权
标题翻译： CDK抑制剂销售
公开(公告)号：US20120041007A1
公开(公告)日：2012-02-16
申请号：US13265918
申请日：2010-04-23
申请人： Massimo Zampieri , Annalisa Airoldi , Maria Gioia Fornaretto , Maria Gabriella Brasca
发明人： Massimo Zampieri , Annalisa Airoldi , Maria Gioia Fornaretto , Maria Gabriella Brasca
IPC分类号： A61K31/519 , A61P35/00 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.
摘要翻译：本发明涉及新型的水溶性盐和cdk抑制剂游离碱的结晶形式。这种结晶盐例如是富马酸盐，L-苹果酸盐，马来酸盐，琥珀酸盐，己二酸盐，丙二酸盐，乙醇酸盐，磷酸盐，甲磺酸盐，L-乳酸盐，盐酸盐，二盐酸盐，三盐酸盐。这种新盐形式的水合物和多晶型物，其制备方法，其在治疗中的用途和含有它们的药物组合物在本申请中也被要求保护和描述。

6. 发明授权

US08586598B2 CDK inhibitor salts 有权
标题翻译： CDK抑制剂盐
公开(公告)号：US08586598B2
公开(公告)日：2013-11-19
申请号：US13265918
申请日：2010-04-23
申请人： Massimo Zampieri , Annalisa Airoldi , Maria Gioia Fornaretto , Maria Gabriella Brasca
发明人： Massimo Zampieri , Annalisa Airoldi , Maria Gioia Fornaretto , Maria Gabriella Brasca
IPC分类号： A61K31/505 , C07D491/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel crystalline form(s) of water-soluble salts and of free base of a cdk inhibitor. Such crystal salts are for example fumarate, L-malate, maleate, succinate, adipate, malonate, glycolate, phosphate, mesylate, L-lactate, hydrochloride, di-hydrochloride, tri-hydrochloride. Hydrates and polymorphs of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.
摘要翻译：本发明涉及新型的水溶性盐和cdk抑制剂游离碱的结晶形式。这种结晶盐例如是富马酸盐，L-苹果酸盐，马来酸盐，琥珀酸盐，己二酸盐，丙二酸盐，乙醇酸盐，磷酸盐，甲磺酸盐，L-乳酸盐，盐酸盐，二盐酸盐，三盐酸盐。这种新盐形式的水合物和多晶型物，其制备方法，其在治疗中的用途和含有它们的药物组合物在本申请中也被要求保护和描述。

7. 发明申请

US20120245189A1 CRYSTALLINE CDC7 INHIBITOR SALTS 有权
标题翻译：晶体蛋白酶抑制剂SALTS
公开(公告)号：US20120245189A1
公开(公告)日：2012-09-27
申请号：US13508648
申请日：2010-11-05
申请人： Massimo Zampieri , Ermes Vanotti , Paola Civaroli , Maria Gioia Fornaretto
发明人： Massimo Zampieri , Ermes Vanotti , Paola Civaroli , Maria Gioia Fornaretto
IPC分类号： A61K31/506 , A61P35/00 , C07D403/04
CPC分类号： C07D403/04
摘要： The present invention relates to novel crystalline salts of a CDC7 or CDC7/CDKs inhibitor, to a novel crystal form of the corresponding free base, to a process for their preparation, to hydrates, solvates and polymorphs of such new salt forms, to their use in therapy and to pharmaceutical compositions containing them. Such crystal salts are selected from L-asparate, hemifumarate, hydrochloride, maleate, mesylate, sulfate, L-tartrate or phosphate salts of 5-(2-amino-pyrimidin-4-yl)-2-(2,4-dichloro-phenyl)-1H-pyrrole-3-carboxylic acid amide.
摘要翻译：本发明涉及CDC7或CDC7 / CDKs抑制剂的新结晶盐，相应游离碱的新结晶形式，其制备方法，这些新盐形式的水合物，溶剂化物和多晶型物的用途在治疗和含有它们的药物组合物。这样的结晶盐选自5-（2-氨基 - 嘧啶-4-基）-2-（2,4-二氯 - 苯基）-2-羟基丙酸的L-天冬氨酸盐，半富马酸盐，盐酸盐，马来酸盐，甲磺酸盐，硫酸盐，L-酒石酸盐或磷酸盐，苯基）-1H-吡咯-3-甲酸酰胺。

8. 发明申请

US20110040090A1 PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES 有权
标题翻译：制备5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-羧酸的方法
公开(公告)号：US20110040090A1
公开(公告)日：2011-02-17
申请号：US12989518
申请日：2009-04-30
申请人： Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
发明人： Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
IPC分类号： C07D403/04 , C07D207/416
CPC分类号： C07D403/04
摘要： The present 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. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in W02007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
摘要翻译：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。 5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲酰胺在WO2007110344中进行了描述和要求保护，其也公开了其制备方法。这些化合物可以有利地通过允许以高产率和纯度以及有限数量的步骤获得所需产物的方法制备。合成起始于氰基吡咯衍生物，其特征在于5-（2-氨基 - 嘧啶-4-基）-2-芳基-1H-吡咯-3-甲腈的最终水解。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。因此，这些化合物可用于治疗多种癌症，细胞增殖性疾病和与蛋白激酶相关的疾病。

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