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。

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。

公开(公告)号：US20110136857A1

公开(公告)日：2011-06-09

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

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。

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。

公开(公告)号：US07728140B2

公开(公告)日：2010-06-01

申请号：US11020793

申请日：2004-12-23

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： C07D471/02

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。

公开(公告)号：US20100210476A1

公开(公告)日：2010-08-19

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： 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。

公开(公告)号：US20050209269A1

公开(公告)日：2005-09-22

申请号：US11020794

申请日：2004-12-23

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

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

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

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。

公开(公告)号：US20050256151A1

公开(公告)日：2005-11-17

申请号：US11020793

申请日：2004-12-23

申请人： Barbara Salom ,  Matteo D'Anello ,  Maria Brasca ,  Patrizia Giordano ,  Katia Martina ,  Francesco Angelucci ,  Frederick Brookfield ,  William Trigg ,  Edward Boyd ,  Jonathan Larard

发明人： Barbara Salom ,  Matteo D'Anello ,  Maria Brasca ,  Patrizia Giordano ,  Katia Martina ,  Francesco Angelucci ,  Frederick Brookfield ,  William Trigg ,  Edward Boyd ,  Jonathan Larard

IPC分类号： C07D471/04 ,  G01N33/53 ,  A61K31/4745 ,  C07D471/02

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.

公开(公告)号：US06245742B1

公开(公告)日：2001-06-12

申请号：US08930616

申请日：1997-10-15

申请人： Carlo Battistini ,  Patrizia Giordano ,  Sabrina De Rosa ,  Fabio Corradi ,  Paolo Comoglio ,  Alberto Bardelli

发明人： Carlo Battistini ,  Patrizia Giordano ,  Sabrina De Rosa ,  Fabio Corradi ,  Paolo Comoglio ,  Alberto Bardelli

IPC分类号： A61K3800

CPC分类号： C07K5/0827 ,  C07K5/0202 ,  C07K5/1016 ,  C07K5/1027 ,  C07K14/71

摘要： The present invention relates to peptides and peptidomimetic compounds and pharmaceutical compositions containing them as useful pharmacological agents in the control or treatment of proliferative diseases such as cancer, against tumor growing and/or tumoral metastasis, and psoriasis and in the control or treatment of inflammatory, allergic, autoimmune, viral, and cardiovascular diseases. These new compounds have the unique property to inhibit the recognition of several phosphotyrosine containing motifs within all the cellular receptors and cytosolic transducers by a wide spectrum of SH2 domains contained in cytosolic transducers and other effector proteins laying along different pathways of the signal transduction process and with a particularly high affinity for the SH2 domain of the adaptor transducer Grb2, a key element along the pathway to mitogenesis and motogenesis, this last activity leading to invasiveness and to metastasis. The invention also relates to methods for production of the compounds and methods of treatment employing the compounds.

摘要翻译： 本发明涉及肽和拟肽化合物和药物组合物，其含有它们作为控制或治疗增殖性疾病如癌症，抗肿瘤生长和/或肿瘤转移以及牛皮癣以及控制或治疗炎症， 过敏性，自身免疫性，病毒性和心血管疾病。 这些新化合物具有独特的性质，可以通过广泛的SH2结构域抑制所有细胞受体和细胞溶质转导体中识别的含有多种含磷酸酪氨酸基序，这些SH2结构域包含在信号转导过程不同途径的细胞溶质转导和其他效应蛋白中， 对于适应器传感器Grb2的SH2结构域特别高的亲和力，Grb2是沿着有丝分裂和发育的途径的关键因素，这是导致侵袭和转移的最后一个活动。 本发明还涉及化合物的制备方法和使用该化合物的处理方法。