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1. 发明授权

US08592583B2 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：US08592583B2
公开(公告)日：2013-11-26
申请号：US13505357
申请日：2010-10-27
申请人： Matteo D'Anello , Marco Re
发明人： Matteo D'Anello , Marco Re
IPC分类号： C07D401/00
CPC分类号： C07D403/04 , C07D207/34
摘要： 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.
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。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。

2. 发明授权

US08394802B2 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one derivatives for the modulation of the activity of protein kinases 有权
标题翻译： 3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮衍生物，用于调节蛋白激酶的活性
公开(公告)号：US08394802B2
公开(公告)日：2013-03-12
申请号：US13119849
申请日：2009-09-17
申请人： Danilo Mirizzi , Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Ron Ferguson , Francesco Casuscelli
发明人： Danilo Mirizzi , Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Ron Ferguson , Francesco Casuscelli
IPC分类号： A61K31/495
CPC分类号： A61K31/4985 , A61K45/06 , C07D487/04
摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds with the formula or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：具有下式或其药学上可接受的盐的3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮化合物的4,7-二取代衍生物，其制备方法和包含它们的药物组合物是披露; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

3. 发明申请

US20120232085A1 3,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 有权
标题翻译：作为激酶抑制剂活化的3,4-二氢-2H-吡嗪并[1,2-A]吲哚-1-酮衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：US20120232085A1
公开(公告)日：2012-09-13
申请号：US13482626
申请日：2012-05-29
申请人： Giovanni CERVI , Matteo D'ANELLO , Gianluca Mariano Enrico PAPEO , Barbara SALOM
发明人： Giovanni CERVI , Matteo D'ANELLO , Gianluca Mariano Enrico PAPEO , Barbara SALOM
IPC分类号： A61K31/4985 , C12N9/99 , A61P35/04 , A61P37/00 , A61P25/28 , A61P31/12 , A61P31/18 , C07D487/04 , A61P35/02
CPC分类号： C07D487/04
摘要： Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了3,4-二氢-2H-吡嗪并[1,2-a]吲哚-1-酮衍生物或其药学上可接受的盐，其制备方法和包含它们的药物组合物的化合物。这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

4. 发明授权

US08198298B2 Pyrrolo[2,3-b]pyridine derivatives active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活性的吡咯并[2,3-b]吡啶衍生物
公开(公告)号：US08198298B2
公开(公告)日：2012-06-12
申请号：US13026789
申请日：2011-02-14
申请人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Dania Tesei , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
发明人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Dania Tesei , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
IPC分类号： A61K31/44
CPC分类号： C07D471/04
摘要： Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了吡咯并[2,3-b]吡啶衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病引起的和/或与其相关的疾病。还公开了在SPS条件下制备本发明化合物的方法和包含其中多个化合物的化学文库。

5. 发明授权

US07888508B2 Pyrrolo[2,3-B]pyridine derivatives active as kinase inhibitors 有权
标题翻译：作为激酶抑制剂活性的吡咯并[2,3-B]吡啶衍生物
公开(公告)号：US07888508B2
公开(公告)日：2011-02-15
申请号：US11020794
申请日：2004-12-23
申请人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Dania Tesei , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
发明人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Dania Tesei , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
IPC分类号： C07D471/02 , C07D498/02
CPC分类号： C07D471/04
摘要： Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了吡咯并[2,3-b]吡啶衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病引起的和/或与其相关的疾病。还公开了在SPS条件下制备本发明化合物的方法和包含其中多个化合物的化学文库。

6. 发明授权

US08513241B2 3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them 有权
标题翻译：作为激酶抑制剂活性的3,4-二氢-2H-吡嗪并[1,2-A]吲哚-1-酮衍生物，其制备方法和包含它们的药物组合物
公开(公告)号：US08513241B2
公开(公告)日：2013-08-20
申请号：US13482626
申请日：2012-05-29
申请人： Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Barbara Salom
发明人： Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Barbara Salom
IPC分类号： A61K31/5355 , A61K31/501 , C07D413/14 , C07D241/04
CPC分类号： C07D487/04
摘要： Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了3,4-二氢-2H-吡嗪并[1,2-a]吲哚-1-酮衍生物或其药学上可接受的盐，其制备方法和包含它们的药物组合物的化合物。这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

7. 发明申请

US20120220771A1 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：US20120220771A1
公开(公告)日：2012-08-30
申请号：US13505357
申请日：2010-10-27
申请人： Matteo D'Anello , Marco Re
发明人： Matteo D'Anello , Marco Re
IPC分类号： C07D403/04 , C07D207/34
CPC分类号： C07D403/04 , C07D207/34
摘要： 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.
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。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。

8. 发明授权

US08106069B2 Pyrrolo[2,3-b]pyridine derivatives active as kinase inhibitors and pharmaceutical compositions comprising them 有权
标题翻译：作为激酶抑制剂活性的吡咯并[2,3-b]吡啶衍生物和包含它们的药物组合物
公开(公告)号：US08106069B2
公开(公告)日：2012-01-31
申请号：US12766230
申请日：2010-04-23
申请人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Francesco Angelucci , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
发明人： Barbara Salom , Matteo D'Anello , Maria Gabriella Brasca , Patrizia Giordano , Katia Martina , Francesco Angelucci , Frederick Arthur Brookfield , William John Trigg , Edward Andrew Boyd , Jonathan Anthony Larard
IPC分类号： A61K31/44 , A61K31/50 , A61K31/497 , A61K31/445
CPC分类号： C07D471/04
摘要： Compounds which are pyrrolo[2,3-b]pyridine derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases and neurodegenerative disorders; also disclosed is a process under SPS conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了吡咯并[2,3-b]吡啶衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病和神经变性疾病引起的和/或与其相关的疾病。还公开了在SPS条件下制备本发明化合物的方法和包含其中多个化合物的化学文库。

9. 发明申请

US20110251179A1 3,4-DIHYDRO-2H-PYRROLO[1,2-a]PYRAZIN-1-ONE DERIVATIVES 有权
标题翻译： 3,4-二氢-2H-吡喃并[1,2-a]吡嗪-1-酮衍生物
公开(公告)号：US20110251179A1
公开(公告)日：2011-10-13
申请号：US13119849
申请日：2009-09-17
申请人： Danilo Mirizzi , Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Ron Ferguson , Francesco Casuscelli
发明人： Danilo Mirizzi , Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Ron Ferguson , Francesco Casuscelli
IPC分类号： A61K31/4985 , C40B40/04 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P35/02 , C12N9/99 , A61P35/00 , A61P31/12 , A61P31/18 , A61P37/06 , A61P25/28 , C07D487/04 , A61K31/551
CPC分类号： A61K31/4985 , A61K45/06 , C07D487/04
摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮化合物的4,7-二取代衍生物或其药学上可接受的盐，其制备方法和包含它们的药物组合物。这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

10. 发明授权

US08981092B2 Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 有权
标题翻译：取代的3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮作为蛋白激酶活性的调节剂
公开(公告)号：US08981092B2
公开(公告)日：2015-03-17
申请号：US13747859
申请日：2013-01-23
申请人： Danilo Mirizzi , Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Ron Ferguson , Francesco Casuscelli
发明人： Danilo Mirizzi , Giovanni Cervi , Matteo D'Anello , Gianluca Mariano Enrico Papeo , Ron Ferguson , Francesco Casuscelli
IPC分类号： C07D241/38 , A61K31/4985 , C07D487/04 , A61K45/06
CPC分类号： A61K31/4985 , A61K45/06 , C07D487/04
摘要： Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了3,4-二氢-2H-吡咯并[1,2-a]吡嗪-1-酮化合物的4,7-二取代衍生物或其药学上可接受的盐，其制备方法和包含它们的药物组合物。这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

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