DR. MARK M MITCHELL, M.D.
Anesthesiologist Assistant in San Diego, CA

2004026, Dec 30, 2004

Jun 23, 2004

10/875836

Elena Dovalsantos - San Diego CA, US
Erik Jon Flahive - San Diego CA, US
Brian Halden - San Diego CA, US
Mark Mitchell - San Diego CA, US
Wolfgang Reinhard Notz - La Jolla CA, US
Qingping Tian - San Diego CA, US

AGOURON PHARMACEUTICALS, INC.

A61K031/519, C07D487/02

514/264110, 544/280000

The invention relates to processes for the preparation of a GARFT inhibitor containing a methyl substituted thiophene core having the following structure: wherein each of Rand Rare independently a hydrogen atom or a moiety that together with the attached COforms a readily hydrolyzable ester group; from an intermediate of the formula wherein Ris a moiety that together with the attached COforms a readily hydrolyzable ester group; Pgis an amino protecting group; Ris H; or Pgcan optionally be taken together with Rand the nitrogen to which Pgand Rare attached to form (i) an imine; or (ii) a fused or bridged bicyclic ring or a spirocyclic ring, wherein said ring is saturated and contains from 5 to 12 carbon atoms in which up to 2 carbon atoms are optionally replaced with a hetero moiety selected from O, S(O)wherein j is an integer from 0 to 2, and —NR—, provided that two O atoms, two S(O)moieties, or an O atom and a S(O)moiety are not attached directly to each other; Ris selected from the group consisting of —C≡C— and —CH CH—; and Ris independently H or C-Calkyl; to form the compound of the formula (I) that is optically pure; and to processes for preparing intermediates thereof.

2005026, Dec 1, 2005

Mar 15, 2005

11/081708

Qiang Ye - San Diego CA, US
Scott Zook - San Diego CA, US
Michael Ouellette - Descanso CA, US
Don Hettinger - San Diego CA, US
Jayaram Srirangam - San Diego CA, US
Robert Kania - San Diego CA, US
Nabil Saeed - San Diego CA, US
Matthew Wightlin - San Diego CA, US
Mark Mitchell - San Diego CA, US

A61K031/4439, C07D043/14

514338000, 546275700

The invention provides several polymorphic forms and an amorphous form of 2,5-Dimethyl-2H-pyrazole-3-carboxylic acid {2-fluoro-5-[3-((E)-2-pyridin-2-yl-vinyl)-1H-indazol-6-ylamino]-phenyl}-amide, pharmaceutical compositions containing such polymorphic or amorphous forms, and methods of using such pharmaceutical compositions to treat disease states mediated by protein kinases, such as cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation.

7268126, Sep 11, 2007

Sep 21, 2005

11/233835

Jia Liu - San Diego CA, US
Naresh Nayyar - San Diego CA, US
Ming Guo - San Diego CA, US
Bennett Chaplin Borer - San Diego CA, US
Aparna Nadig Srirangam - San Diego CA, US
Mark Bryan Mitchell - San Diego CA, US
Yi Li - San Diego CA, US

Agouron Pharmaceuticals, Inc. - San Diego CA
Cancer Research Technology Ltd. - London

C07D 487/06, A61K 31/55, A61P 35/00, A61P 35/28

51421204, 540520

The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.