公开(公告)号：US09233111B2

公开(公告)日：2016-01-12

申请号：US14130536

申请日：2012-07-07

Applicant: Richard Heng ,  Elizabeth Kate Hoegenauer ,  Guido Koch ,  Robert Alexander Pulz ,  Anna Vulpetti ,  Rudolf Waelchli

Inventor： Richard Heng ,  Elizabeth Kate Hoegenauer ,  Guido Koch ,  Robert Alexander Pulz ,  Anna Vulpetti ,  Rudolf Waelchli

IPC: C07D487/04 ,  A61K31/519 ,  A61P35/00

CPC classification number: A61K31/519 ,  C07D487/04

Abstract: The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.

Abstract translation: 本发明描述了与布鲁顿酪氨酸激酶（Btk）相互作用的新的吡咯并嘧啶衍生物及其药学上可接受的盐。 因此，新的吡咯并嘧啶可能有效治疗自身免疫疾病，炎性疾病，过敏性疾病，气道疾病如哮喘和慢性阻塞性肺疾病（COPD），移植排斥反应，癌症。 的造血起源或实体瘤。

公开(公告)号：US20150322060A1

公开(公告)日：2015-11-12

申请号：US14409878

申请日：2013-06-27

Applicant: Stefanie FLOHR ,  Ulrich HOMMEL ,  Edwige Liliane Jeanne LORTHIOIS ,  Jeurgen Klaus MAIBAUM ,  Nils OSTERMANN ,  Jean QUANCARD ,  Stefan Andreas RANDL ,  Olivier ROGEL ,  Anna VULPETTI

Inventor： Stefanie FLOHR ,  Ulrich HOMMEL ,  Edwige Liliane Jeanne LORTHIOIS ,  Jeurgen Klaus MAIBAUM ,  Nils OSTERMANN ,  Jean QUANCARD ,  Stefan Andreas RANDL ,  Olivier ROGEL ,  Anna VULPETTI

IPC: C07D471/04 ,  C07D403/14 ,  C07D403/06

CPC classification number: C07D471/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14

Abstract: The present invention provides a compound of formula (I) a method for manufacturing the compounds of the invention, and its therapeutic uses as a factor D inhibitor for the treatment of ophthalmic diseases. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明提供式（I）化合物，其制备本发明化合物的方法及其作为治疗眼科疾病的因子D抑制剂的治疗用途。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：US20150148349A1

公开(公告)日：2015-05-28

申请号：US14409911

申请日：2013-06-27

Applicant: Eva Altmann ,  Ulrich Hommel ,  Edwige Liliane Jeanne Lorthiois ,  Jeurgen Klaus Maibaum ,  Nils Ostermann ,  Jean Quancard ,  Stefan Andreas Randl ,  Olivier Rogel ,  Anna Vulpetti

Inventor： Eva Altmann ,  Ulrich Hommel ,  Edwige Liliane Jeanne Lorthiois ,  Jeurgen Klaus Maibaum ,  Nils Ostermann ,  Jean Quancard ,  Stefan Andreas Randl ,  Olivier Rogel ,  Anna Vulpetti

IPC: C07D209/52 ,  C07D487/04 ,  C07D403/06 ,  C07D403/14 ,  C07D471/04 ,  C07D401/14

CPC classification number: C07D209/52 ,  A61K45/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides a compound of formula (I): a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明提供式（I）化合物：本发明化合物的制备方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：US20150141455A1

公开(公告)日：2015-05-21

申请号：US14409871

申请日：2013-06-27

Applicant: Eva Altmann ,  Ulrich Hommel ,  Edwige Liliane Jeanne Lorthiois ,  Jeurgen Klaus Maibaum ,  Nils Ostermann ,  Jean Quancard ,  Stefan Andreas Randl ,  Olivier Rogel ,  Anna Vulpetti

Inventor： Eva Altmann ,  Ulrich Hommel ,  Edwige Liliane Jeanne Lorthiois ,  Jeurgen Klaus Maibaum ,  Nils Ostermann ,  Jean Quancard ,  Stefan Andreas Randl ,  Olivier Rogel ,  Anna Vulpetti

IPC: C07D403/06 ,  C07D491/056 ,  C07D471/04

CPC classification number: C07D403/06 ,  A61K31/416 ,  A61K31/4162 ,  A61K45/06 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

Abstract: The present invention provides a compound of formula I: (I) a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract translation: 本发明提供式I化合物：（I）制备本发明化合物的方法及其治疗用途。 本发明还提供药理活性剂和药物组合物的组合。

公开(公告)号：US20130338148A1

公开(公告)日：2013-12-19

申请号：US13972659

申请日：2013-08-21

Applicant: Gabriella Traquandi ,  Maria Gabriella Brasca ,  Roberto D'Alessio ,  Paolo Polucci ,  Fulvia Roletto ,  Anna Vulpetti ,  Paolo Pevarello ,  Achille Panzeri ,  Francesca Quartieri ,  Ron Ferguson ,  Paola Vianello ,  Daniele Fancelli

Inventor： Gabriella Traquandi ,  Maria Gabriella Brasca ,  Roberto D'Alessio ,  Paolo Polucci ,  Fulvia Roletto ,  Anna Vulpetti ,  Paolo Pevarello ,  Achille Panzeri ,  Francesca Quartieri ,  Ron Ferguson ,  Paola Vianello ,  Daniele Fancelli

IPC: A61K31/551 ,  C07D401/10 ,  C07D487/14 ,  A61K31/519 ,  A61K31/5377 ,  C07D231/56 ,  C07D487/04

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  C07D231/56 ,  C07D239/72 ,  C07D401/10 ,  C07D403/14 ,  C07D413/14 ,  C07D487/04

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

公开(公告)号：US08481585B2

公开(公告)日：2013-07-09

申请号：US13614499

申请日：2012-09-13

Applicant: Maria Gabriella Brasca ,  Raffaella Amici ,  Daniele Fancelli ,  Marcella Nesi ,  Paolo Orsini ,  Fabrizio Orzi ,  Patrick Roussel ,  Anna Vulpetti ,  Paolo Pevarello

Inventor： Maria Gabriella Brasca ,  Raffaella Amici ,  Daniele Fancelli ,  Marcella Nesi ,  Paolo Orsini ,  Fabrizio Orzi ,  Patrick Roussel ,  Anna Vulpetti ,  Paolo Pevarello

IPC: A61K31/4162 ,  A61K31/454 ,  C07D487/02 ,  C07D401/14

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10

Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.

公开(公告)号：US07482354B2

公开(公告)日：2009-01-27

申请号：US10557565

申请日：2004-04-27

Applicant: Gabriella Traquandi ,  Maria Gabriella Brasca ,  Roberto D'Alessio ,  Paolo Polucci ,  Fulvia Roletto ,  Anna Vulpetti ,  Paolo Pevarello ,  Achille Panzeri ,  Francesca Quartieri ,  Ron Ferguson ,  Paola Vianello ,  Daniele Fancelli

Inventor： Gabriella Traquandi ,  Maria Gabriella Brasca ,  Roberto D'Alessio ,  Paolo Polucci ,  Fulvia Roletto ,  Anna Vulpetti ,  Paolo Pevarello ,  Achille Panzeri ,  Francesca Quartieri ,  Ron Ferguson ,  Paola Vianello ,  Daniele Fancelli

IPC: A61K31/505 ,  A01N43/54 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/551 ,  C07D231/56 ,  C07D239/72 ,  C07D401/10 ,  C07D403/14 ,  C07D413/14 ,  C07D487/04

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract translation: 公开了说明书中定义的式（Ia）或（Ib）的吡唑并喹唑啉衍生物及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; 本发明的化合物可用于治疗与失调的蛋白激酶活性相关的疾病，如癌症。

公开(公告)号：US20070004705A1

公开(公告)日：2007-01-04

申请号：US10539145

申请日：2003-12-04

Applicant: Maria Brasca ,  Raffaella Amici ,  Daniele Fancelli ,  Marcell Nesi ,  Paolo Orsini ,  Fabrizio Orzi ,  Patrick Roussel ,  Anna Vulpetti ,  Paolo Pevarello

Inventor： Maria Brasca ,  Raffaella Amici ,  Daniele Fancelli ,  Marcell Nesi ,  Paolo Orsini ,  Fabrizio Orzi ,  Patrick Roussel ,  Anna Vulpetti ,  Paolo Pevarello

IPC: A61K31/551 ,  A61K31/496 ,  A61K31/4747 ,  A61K31/454 ,  A61K31/4162 ,  C07D487/10 ,  C07D487/02

CPC classification number: C07D487/04 ,  A61K31/4162 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61N5/10

Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.

Abstract translation: 通式（Ia）或（Ib）表示的化合物及其药学上可接受的盐及其药学上可接受的盐被公开，其中R 1和R 1'如说明书中所定义。 所述化合物可用于治疗细胞周期增殖性疾病，例如， 与改变的细胞周期依赖性激酶活性相关的癌症。

公开(公告)号：US07105535B2

公开(公告)日：2006-09-12

申请号：US10470859

申请日：2002-01-28

Applicant: Daniela Berta ,  Eduard Felder ,  Anna Vulpetti ,  Marzia Villa

Inventor： Daniela Berta ,  Eduard Felder ,  Anna Vulpetti ,  Marzia Villa

IPC: A61K31/302 ,  A61K31/338 ,  A61K31/375 ,  C07D471/04 ,  C07D471/06

CPC classification number: C07D413/04 ,  A61K31/4155 ,  A61K31/437 ,  C07D413/14

Abstract: Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.

Abstract translation: 化合物，如说明书中所定义的恶唑基 - 吡唑衍生物及其药学上可接受的盐; 可用于治疗由改变的蛋白激酶活性如癌症，细胞增殖性病症，病毒感染，自身免疫性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：US20060135508A1

公开(公告)日：2006-06-22

申请号：US10522253

申请日：2003-07-16

Applicant: Manuela Villa ,  Francesca Abrate ,  Daniele Fancelli ,  Mario Varasi ,  Anna Vulpetti

Inventor： Manuela Villa ,  Francesca Abrate ,  Daniele Fancelli ,  Mario Varasi ,  Anna Vulpetti

IPC: A61K31/55 ,  A61K31/4745 ,  C07D487/02 ,  C07D471/02

CPC classification number: C07D487/04 ,  A61K31/415 ,  A61K45/06 ,  C07D471/04 ,  A61K2300/00

Abstract: The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrrolo-pyrazole or pyrazolo-azepine. The invention also provides specific pyrrolo-pyrazoles and pyrazolo-azepines, useful intermediates, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.

Abstract translation: 本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，其包括向有需要的哺乳动物施用有效量的吡咯并吡唑或吡唑并氮。 本发明还提供特定的吡咯并吡唑和吡唑并氮杂，有用的中间体，包含其中至少两个的文库，其制备方法和含有它们的药物组合物，其可用于治疗由和/或 与改变的蛋白激酶活性如癌症，细胞增殖性病症，病毒感染，自身免疫疾病和神经变性疾病有关。