公开(公告)号：US20110136857A1

公开(公告)日：2011-06-09

申请号：US13026789

申请日：2011-02-14

Applicant: 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

Inventor： 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: A61K31/437 ,  A61K31/4545 ,  A61P35/00 ,  A61P25/28 ,  A61P31/12 ,  A61P37/00 ,  A61P17/06 ,  A61P9/10 ,  A61P19/02 ,  A61P17/14 ,  C12N9/99 ,  C40B40/04

CPC classification number: C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20110040090A1

公开(公告)日：2011-02-17

申请号：US12989518

申请日：2009-04-30

Applicant: Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

Inventor： Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

IPC: C07D403/04 ,  C07D207/416

CPC classification number: C07D403/04

Abstract: 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.

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。 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。

公开(公告)号：US20100210476A1

公开(公告)日：2010-08-19

申请号：US12766230

申请日：2010-04-23

Applicant: 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

Inventor： 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: C40B40/04 ,  A61K31/437 ,  A61K31/5377 ,  A61K31/496 ,  A61P35/00 ,  A61P25/28 ,  A61P31/12 ,  A61P13/08 ,  A61P17/06 ,  A61P9/10 ,  A61P19/02 ,  A61P35/04 ,  A61P37/06 ,  A61P17/14

CPC classification number: C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07511136B2

公开(公告)日：2009-03-31

申请号：US10490189

申请日：2002-09-19

Applicant: Raffaella Amici ,  Matteo D'Anello ,  Katia Martina ,  Barbara Salom ,  Anna Vulpetti

Inventor： Raffaella Amici ,  Matteo D'Anello ,  Katia Martina ,  Barbara Salom ,  Anna Vulpetti

IPC: C07D413/00 ,  C07D231/00

CPC classification number: C07D231/56 ,  C07D403/04 ,  C07D403/12

Abstract: Compounds which are 3-aminoindazole derivatives or pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compositions 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.

Abstract translation: 公开了3-氨基吲唑衍生物或其药学上可接受的盐以及包含它们的药物组合物的化合物; 这些化合物或组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。

公开(公告)号：US20050209269A1

公开(公告)日：2005-09-22

申请号：US11020794

申请日：2004-12-23

Applicant: Barbara Salom ,  Matteo D'Anello ,  Maria Brasca ,  Patrizia Giordano ,  Katia Martina ,  Dania Tesei ,  Frederick Brookfield ,  William Trigg ,  Edward Boyd ,  Jonathan Larard

Inventor： Barbara Salom ,  Matteo D'Anello ,  Maria Brasca ,  Patrizia Giordano ,  Katia Martina ,  Dania Tesei ,  Frederick Brookfield ,  William Trigg ,  Edward Boyd ,  Jonathan Larard

IPC: C07D471/04 ,  A61K31/4745 ,  C07D471/02

CPC classification number: C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06284887B1

公开(公告)日：2001-09-04

申请号：US09588339

申请日：2000-06-06

Applicant: Achille Panzeri ,  Matteo D'Anello ,  Antonio Longo ,  Marcella Nesi

Inventor： Achille Panzeri ,  Matteo D'Anello ,  Antonio Longo ,  Marcella Nesi

IPC: C07J4300

CPC classification number: C07J73/005

Abstract: A process for producing a compound of formula (I): wherein the dotted lines - - - independently represent a single or double bond and R, R1, R2 and R3 are each hydrogen or an organic radical, comprises treating the corresponding 17&bgr;-carbonylimidazole intermediates with anhydrous acids in the presence of an amine and, optionally, hydrogenating the resulting compound.

Abstract translation: 一种制备式（I）化合物的方法：其中虚线 - - - 独立地表示单键或双键，R，R 1，R 2和R 3各自为氢或有机基团，包括处理相应的17β-羰基咪唑中间体 与无水酸在胺的存在下，并任选地氢化所得化合物。

公开(公告)号：US5254680A

公开(公告)日：1993-10-19

申请号：US691089

申请日：1991-04-25

Applicant: Marco Alpegiani ,  Pierluigi Bissolino ,  Matteo D'Anello ,  Ettore Perrone

Inventor： Marco Alpegiani ,  Pierluigi Bissolino ,  Matteo D'Anello ,  Ettore Perrone

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  A61P43/00 ,  C07D501/00 ,  C07D501/04

CPC classification number: C07D501/00

Abstract: There is provided a process for preparing a compound of the formula (I): ##STR1## wherein R.sub.1 is an organic residue, R.sub.2 is a hydrogen or a chlorine atom, a methoxy, ethoxy or an acetoxy group, and n represents 0, 1 or 2.The process comprises reacting a compound of the formula (II): ##STR2## wherein R.sub.2 and n are as defined above, with an inorganic or organic nitrite, in an alcohol R.sub.1 OH, wherein R.sub.1 is as defined above, or in a mixture R.sub.1 OH-organic solvent in the presence of an inorganic or organic acid.The compounds of the formula (I) are known intermediates in the synthesis of human leucocyte elastase inhibitors (HLE).

Abstract translation: 提供了制备式（I）化合物的方法：其中R1是有机残基，R2是氢或氯原子，甲氧基，乙氧基或乙酰氧基，n表示 该方法包括使式（II）化合物：其中R2和n如上所定义的化合物与无机或有机亚硝酸盐在醇R 1 OH中反应，其中R 1为 或在无机或有机酸存在下，在混合物中的R1OH-有机溶剂中。 式（I）的化合物是合成人类白细胞弹性蛋白酶抑制剂（HLE）的已知中间体。

公开(公告)号：US20130137696A1

公开(公告)日：2013-05-30

申请号：US13747859

申请日：2013-01-23

Applicant: Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

Inventor： Danilo Mirizzi ,  Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Ron Ferguson ,  Francesco Casuscelli

IPC: A61K31/4985 ,  A61K45/06 ,  C07D487/04

CPC classification number: A61K31/4985 ,  A61K45/06 ,  C07D487/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08399668B2

公开(公告)日：2013-03-19

申请号：US12989518

申请日：2009-04-30

Applicant: Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

Inventor： Matteo D'Anello ,  Carlo Battistini ,  Maria Gioia Fornaretto ,  Ermes Vanotti

IPC: C07D403/04

CPC classification number: C07D403/04

Abstract: 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.

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。 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。

公开(公告)号：US08207165B2

公开(公告)日：2012-06-26

申请号：US12934422

申请日：2009-03-27

Applicant: Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Barbara Salom

Inventor： Giovanni Cervi ,  Matteo D'Anello ,  Gianluca Mariano Enrico Papeo ,  Barbara Salom

IPC: A61K31/5355 ,  A61K31/501 ,  C07D413/14 ,  C07D241/04 ,  C40B40/04

CPC classification number: C07D487/04

Abstract: 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.

Abstract translation: 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。