公开(公告)号：US06911440B2

公开(公告)日：2005-06-28

申请号：US10723238

申请日：2003-11-26

申请人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

发明人： Guido Bold ,  Janet Dawson King ,  Jörg Frei ,  Richard Heng ,  Paul William Manley ,  Bernhard Wietfeld ,  Jeanette Marjorie Wood

IPC分类号： A61K31/502 ,  A61K31/506 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P13/12 ,  A61P17/06 ,  A61P19/02 ,  A61P25/04 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  A61P43/00 ,  C07D401/06 ,  C07D401/14 ,  A61K31/33 ,  A61K31/44 ,  C07D237/00 ,  C07D401/00 ,  C07D487/00

CPC分类号： C07D401/06 ,  A61K31/501 ,  A61K31/502 ,  C07D401/14

摘要： The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.

摘要翻译： 本发明涉及治疗炎症性疾病，特别是炎性类风湿病或风湿性疾病，和/或具有式I的VEGF受体酪氨酸激酶的活性抑制剂的疼痛，该说明书中定义的取代基; 以及新的酞嗪衍生物; 其制备方法，其用于治疗人或动物体的方法中的应用; 其用于治疗疾病，特别是由眼睛新生血管形成引起的疾病，例如年龄相关性黄斑变性或糖尿病性视网膜病，或其它对酪氨酸激酶（例如增殖性疾病）的抑制作用的疾病的用途; 哺乳动物治疗这种疾病的方法; 以及这种化合物用于制造特别是上述疾病的药物制剂的用途。