Synthetic process, and crystalline forms of a pyrrolotriazine compound

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United States of America Patent

APP PUB NO 20060014741A1
SERIAL NO

11149525

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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.

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Patent Owner(s)

Patent OwnerAddress
BRISTOL-MYERS SQUIBB COMPANYROUTE 206 & PROVINCE LINE ROAD PRINCETON NJ 08543

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
DiMarco, John D East Brunswick, NJ 23 283
Gougoutas, Jack Z Princeton, NJ 29 627
Patel, Bharat P Pennington, NJ 4 12

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