forma cristalina, composição farmacêutica, e, método de tratamento de uma doença proliferativa

The present invention provides a process for preparing pyrrolotriazine compounds of formula (I) or a pharmaceutically acceptable salt thereof. Also provided are crystalline forms of the pyrrolotriazine compound [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methyl-pyrrolo[2, 1-f][1,2,4]triaz...

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Bibliographic Details
Main Authors JACK Z. GOUGOUTAS, JOHN D. DIMARCO, BHARAT P. PATEL
Format Patent
LanguagePortuguese
Published 06.09.2016
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:The present invention provides a process for preparing pyrrolotriazine compounds of formula (I) or a pharmaceutically acceptable salt thereof. Also provided are 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.
Bibliography:Application Number: BR2006PI11891