公开(公告)号：EP1694683A2

公开(公告)日：2006-08-30

申请号：EP04814139.4

申请日：2004-12-10

申请人： Bristol-Myers Squibb Company

发明人： SWAMINATHAN, Shankar ,  GAVAI, Ashvinikumar V. ,  FAN, Junying ,  PATEL, Bharat P. ,  NORRIS, Derek J. ,  CORBETT, Richard Michael ,  ZHENG, Bin

IPC分类号： C07D487/04 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D487/04

摘要： The present invention provides a process for preparing compounds of formula (I) ['insert chemical structure here'](I)or a pharmaceutically acceptable salt thereof. The compounds prepared by the process of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

公开(公告)号：EP1888590A2

公开(公告)日：2008-02-20

申请号：EP06784722.8

申请日：2006-06-09

申请人： Bristol-Myers Squibb Company

发明人： DIMARCO, John D. ,  GOUGOUTAS, Jack Z. ,  PATEL, Bharat P.

IPC分类号： C07D487/04 ,  A61K31/53

CPC分类号： C07D487/04

摘要： The invention provides crystalline forms of the pyrrolotriazine compound [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester and pharmaceutical compositions comprising at least one crystalline form, as well of methods of using the crystalline forms in the treatment of a proliferative disease, and methods for obtaining such crystalline forms. The compounds of formula (I), including [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamic acid, (3S)-3-morpholinylmethyl ester, are useful for inhibiting tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents for the treatment of cancer and other diseases.

摘要翻译： 本发明提供吡咯并三嗪化合物[4 - [[1-（3-氟苯基）甲基] -1H-吲唑-5-基氨基] -5-甲基 - 吡咯并[2,1-f] [1,2- 4]三嗪-6-基] - 氨基甲酸，（3S）-3-吗啉基甲基酯和包含至少一种晶型的药物组合物，以及使用该晶型治疗增殖性疾病的方法，以及用于 获得这种结晶形式。 式[I]化合物，包括[4 - [[1-（3-氟苯基）甲基] -1H-吲唑-5-基氨基] -5-甲基 - 吡咯并[2,1-f] [1,2， 4]三嗪-6-基] - 氨基甲酸（3S）-3-吗啉基甲基酯可用于抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使它们可用作抗增殖剂用于治疗 癌症和其他疾病。